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EA027280B1 - Сульфамоил-ариламиды и их применение в качестве лекарственных препаратов для лечения гепатита b - Google Patents

Сульфамоил-ариламиды и их применение в качестве лекарственных препаратов для лечения гепатита b Download PDF

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Publication number
EA027280B1
EA027280B1 EA201590450A EA201590450A EA027280B1 EA 027280 B1 EA027280 B1 EA 027280B1 EA 201590450 A EA201590450 A EA 201590450A EA 201590450 A EA201590450 A EA 201590450A EA 027280 B1 EA027280 B1 EA 027280B1
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Eurasian Patent Office
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alkyl
group
independently selected
saturated ring
halogen
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EA201590450A
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EA201590450A1 (ru
Inventor
Коэн Вандик
Стефан Жюльен Ласт
Герт Ромбу
Вим Гастон Версхюэрен
Пьер Жан-Мари Бернар Рабуассон
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Янссен Сайенсиз Айрлэнд Юси
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    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
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Abstract

Сульфамоил-ариламиды и их применение в качестве лекарственных препаратов для лечения гепатита В. Ингибиторы репликации HBV формулы (I), в том числе их стереохимические изомерные формы, а также их соли, гидраты, сольваты, где В, R, Rи Rимеют значения, определенные в настоящем документе. Настоящее изобретение также относится к способам получения указанных соединений, содержащих их фармацевтических композиций, а также к их применению отдельно или в комбинации с другими ингибиторами HBV в терапии, активной в отношении HBV.

Description

С071) 277/16 (2006.01) (54) СУЛЬФАМОИЛ-АРИЛАМИДЫ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ЛЕКАРСТВЕННЫХ ПРЕПАРАТОВ ДЛЯ ЛЕЧЕНИЯ ГЕПАТИТА В
027280 Β1 (31) 12182076.5; 12185055.6; 12190837.0; 13157230.7; 13169574.4 (32) 2012.08.28; 2012.09.19; 2012.10.31; 2013.02.28; 2013.05.28 (33) ЕР (43) 2015.07.30 (86) РСТ/ЕР2013/067829 (87) \\О 2014/033176 2014.03.06 (71) (73) Заявитель и патентовладелец:
ЯНССЕН САЙЕНСИЗ АЙРЛЭНД ЮСи (ΙΕ)

Claims (12)

  1. ФОРМУЛА ИЗОБРЕТЕНИЯ или его стереоизомерная или таутомерная форма, где В представляет собой моноциклическое 5-6-членное ароматическое кольцо, необязательно содержащее один или несколько гетероатомов, каждый из которых независимо выбран из группы, состоящей из О, З и Ν, при этом такое 5-6-членное ароматическое кольцо необязательно замещено одним или несколькими заместителями, каждый из которых независимо выбран из группы, состоящей из водорода, галогена, С‘-С3алкила, СИ СРН2, СР2Н и СР3;
    Κ1 представляет собой водород;
    Κ2 представляет собой С‘-С6алкил, С‘-С6алкенил, С^С^лкил-И^ С(=О)-И5, СРН2, СР2Н, СР3, дигидроинденильный или тетрагидронафталенильный фрагмент, необязательно замещенный ОН, или 3-7членное насыщенное кольцо, необязательно содержащее один или несколько гетероатомов, каждый из которых независимо выбран из группы, состоящей из О, З и Ν, где каждый из 3-7-членного насыщенного кольца, С^С^лкил-Ю или С‘-С6алкила замещен одним или несколькими заместителями, каждый из которых независимо выбран из группы, состоящей из галогена, С‘-С4алкилокси, С‘-С4алкилоксикарбонила, оксо, С(=О)-С‘-С3алкила, С‘-С4алкила, СП СРН2, СР2Н и СР3; или
    Κ1 и Κ2 вместе с атомом азота, к которому они присоединены, образуют 6-10-членное бициклическое или мостиковое кольцо или 5-7-членное насыщенное кольцо, при этом такой фрагмент бициклического, мостикового или насыщенного кольца необязательно содержит один или несколько дополнительных гетероатомов, каждый из которых независимо выбран из группы, состоящей из О, З и Ν, и где 5-7членное насыщенное кольцо замещено одним или несколькими заместителями, каждый из которых независимо выбран из группы, состоящей из галогена, С‘-С4алкилоксикарбонила, оксо, С(=О)-С‘-С3алкила, С‘-С4алкила, ΟΝ, СРН2, СР2Н и СР3;
    каждый Κ4 независимо выбран из водорода, галогена, С‘-С4алкилокси, С‘-С4алкила, С‘-С4алкенила, ОН, С^ СРН2, СР2Н, СР3, НС=С и 3-5-членного насыщенного кольца, необязательно содержащего один или несколько гетероатомов, каждый из которых независимо выбран из группы, состоящей из О и Ν, где С‘-С4алкил необязательно замещен ОН и где по меньшей мере один Κ4 представляет собой фтор, а другой Κ4 выбран из группы, состоящей из С‘-С3алкила, С‘-С3алкенила, СНР2 или циклопропила;
    Κ5 представляет собой С‘-С6алкил, СРН2, СР2Н, СР3, фенил, пиридил или 3-7-членное насыщенное кольцо, необязательно содержащее один или несколько гетероатомов, каждый из которых независимо выбран из группы, состоящей из О, З и Ν, при этом такое 3-7-членное насыщенное кольцо необязательно замещено одним или несколькими заместителями, каждый из которых независимо выбран из группы, состоящей из галогена, С‘-С4алкилокси, С‘-С4алкилоксикарбонила, оксо, С(=О)-С‘-С3алкила, С‘С4алкила, ОН, ΟΝ, СРН2, СР2Н и СР3.
  2. 2. Соединение по п.1, где один Κ4 представляет собой фтор, а другой Κ4 выбран из группы, состоящей из метила или СНР2, и где указанный фтор находится в пара-положении, а указанный метил или СНР2 находится в мета-положении относительно азота(*).
  3. 3. Соединение по любому из пп.1, 2, где Κ2 представляет собой 4-7-членное насыщенное кольцо, содержащее атом углерода и один или несколько атомов кислорода, при этом такое 4-7-членное насыщенное кольцо замещено одним или несколькими заместителями, каждый из которых независимо выбран из группы, состоящей из галогена, С‘-С4алкилокси, С‘-С4алкилоксикарбонила, С(=О)-С‘-С3алкила, С‘-С4алкила, ΟΝ, СРН2, СР2Н и СР3.
  4. 4. Соединение по любому из пп.1-3, где Κ2 представляет собой 4-7-членное насыщенное кольцо, содержащее атом углерода и один или несколько атомов кислорода, при этом такое 4-7-членное насыщенное кольцо замещено одним или несколькими заместителями, каждый из которых независимо выбран из группы, состоящей из галогена, С‘-С4алкилоксикарбонила, С(=О)-С‘-С3алкила, С‘-С4алкила, С^ СРН2, СР2Н и СР3.
  5. 5. Соединение по любому из предыдущих пунктов, где В представляет собой фенил или тиофен, необязательно замещенный одним или несколькими заместителями, каждый из которых независимо выбран из группы, состоящей из галогена, С‘-С3алкила, С^ СРН2, СР2Н и СР3.
  6. 6. Соединение по любому из предыдущих пунктов, которое представлено формулой (Ш)
    - 92 027280 где Κ1, Κ2, Κ4 определены в любом из предыдущих пунктов и Κ3 выбран из группы, состоящей из водорода, галогена, С1-С3алкила, ΟΝ, СЕН2, СЕ2Н и СЕ3.
  7. 7. Соединение по любому из пп.1-3, которое представлено формулой (Ιά) где Κ1, Κ2, Κ4 определены в любом из предыдущих пунктов и Κ3 выбран из группы, состоящей из водорода, галогена, С1-С3алкила, ΟΝ, СЕН2, СЕ2Н, СЕ3.
  8. 8. Соединение по п.5 или 6, где Κ3 представляет собой водород.
  9. 9. Соединение по любому из предыдущих пунктов, которое представлено формулой (1с) где Κ1, Κ2, Κ4 определены в любом из предыдущих пунктов.
  10. 10. Применение соединения по любому из предыдущих пунктов в предупреждении или лечении инфекции НВУ у млекопитающего.
  11. 11. Фармацевтическая композиция, обладающая способностью ингибировать НВУ, содержащая терапевтически эффективное количество соединения по любому из пп.1-8 и фармацевтически приемлемый носитель.
  12. 12. Композиция, содержащая:
    (a) соединение формулы (I) по любому из пп.1-8 и (b) ингибитор НВУ, выбранный из интерферона-α (1ЕЫ-а), пегилированного интерферона-α, 3ТС и адефовира, причем указанная композиция пригодна в виде комбинированного препарата для одновременного, раздельного или последовательного применения в лечении инфекций, вызываемых НВУ.
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2710928C2 (ru) * 2014-07-31 2020-01-14 Инсерм (Институт Насьональ Де Ла Сант Эт Де Ла Решерш Медикаль) Антагонисты рецептора flt3

Families Citing this family (155)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2797123T3 (es) 2011-12-21 2020-12-01 Novira Therapeutics Inc Agentes antivirales para la hepatitis B
KR20210081451A (ko) 2012-08-28 2021-07-01 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 설파모일-아릴아미드 및 b형 간염 치료제로서의 그 용도
CA2896554C (en) * 2012-12-27 2019-11-05 Drexel University Novel antiviral agents against hbv infection
WO2014131847A1 (en) 2013-02-28 2014-09-04 Janssen R&D Ireland Sulfamoyl-arylamides and the use thereof as medicaments for the treatment of hepatitis b
US8993771B2 (en) 2013-03-12 2015-03-31 Novira Therapeutics, Inc. Hepatitis B antiviral agents
HUE033542T2 (en) 2013-04-03 2017-12-28 Janssen Sciences Ireland Uc Their use as medicaments for the treatment of N-phenylcarboxamide derivatives and hepatitis B
JO3603B1 (ar) 2013-05-17 2020-07-05 Janssen Sciences Ireland Uc مشتقات سلفامويل بيرولاميد واستخدامها كادوية لمعالجة التهاب الكبد نوع بي
AU2014267235B2 (en) 2013-05-17 2017-10-05 Janssen Sciences Ireland Uc Sulphamoylthiophenamide derivatives and the use thereof as medicaments for the treatment of hepatitis B
HUE039152T2 (hu) 2013-07-25 2018-12-28 Janssen Sciences Ireland Uc Glioxamiddal szubsztituált pirrolamid-származékok és alkalmazásuk hepatitisz B kezelésére szolgáló gyógyszerként
DK3060547T3 (en) 2013-10-23 2018-01-15 Janssen Sciences Ireland Uc CARBOXAMIDE DERIVATIVES AND USE THEREOF AS MEDICINES FOR TREATMENT OF HEPATITS B
US10392349B2 (en) 2014-01-16 2019-08-27 Novira Therapeutics, Inc. Azepane derivatives and methods of treating hepatitis B infections
US9181288B2 (en) 2014-01-16 2015-11-10 Novira Therapeutics, Inc. Azepane derivatives and methods of treating hepatitis B infections
US9169212B2 (en) 2014-01-16 2015-10-27 Novira Therapeutics, Inc. Azepane derivatives and methods of treating hepatitis B infections
KR20160128305A (ko) 2014-02-05 2016-11-07 노비라 테라퓨틱스, 인코포레이티드 Hbv 감염의 치료를 위한 병용 요법
EA035848B1 (ru) 2014-02-06 2020-08-20 Янссен Сайенсиз Айрлэнд Юси Производные сульфамоилпирроламида и их применение в качестве медикаментов для лечения гепатита b
EP3116316B1 (en) 2014-03-13 2019-07-10 Indiana University Research and Technology Corporation Hepatitis b core protein allosteric modulators
US9400280B2 (en) 2014-03-27 2016-07-26 Novira Therapeutics, Inc. Piperidine derivatives and methods of treating hepatitis B infections
US9765050B2 (en) 2014-12-30 2017-09-19 Novira Therapeutics, Inc. Pyridyl reverse sulfonamides for HBV treatment
MA41338B1 (fr) 2015-01-16 2019-07-31 Hoffmann La Roche Composés de pyrazine pour le traitement de maladies infectieuses
PL3097102T3 (pl) 2015-03-04 2018-04-30 Gilead Sciences Inc Związki 4,6-diamino-pirydo[3,2-d]pirymidyny modulujące działanie receptora toll-podobnego
WO2016149581A1 (en) 2015-03-19 2016-09-22 Novira Therapeutics, Inc. Azocane and azonane derivatives and methods of treating hepatitis b infections
WO2016161268A1 (en) 2015-04-01 2016-10-06 Enanta Pharmaceuticals, Inc. Hepatitis b antviral agents
WO2016183266A1 (en) 2015-05-13 2016-11-17 Enanta Pharmaceuticals, Inc. Ehpatitis b antiviral agents
US10875876B2 (en) 2015-07-02 2020-12-29 Janssen Sciences Ireland Uc Cyclized sulfamoylarylamide derivatives and the use thereof as medicaments for the treatment of hepatitis B
US10179131B2 (en) 2015-07-13 2019-01-15 Enanta Pharmaceuticals, Inc. Hepatitis B antiviral agents
US10301255B2 (en) 2015-07-22 2019-05-28 Enanta Pharmaceuticals, Inc. Hepatitis B antiviral agents
JP2018525412A (ja) 2015-08-26 2018-09-06 ギリアード サイエンシーズ， インコーポレイテッド 重水素化トール様受容体調節因子
TWI730985B (zh) 2015-09-15 2021-06-21 美商艾森伯利生物科學公司 B型肝炎核心蛋白質調節劑
AU2016330964B2 (en) 2015-09-29 2021-04-01 Novira Therapeutics, Inc. Crystalline forms of a hepatitis B antiviral agent
WO2017136403A1 (en) 2016-02-02 2017-08-10 Enanta Pharmaceuticals, Inc. Hepatitis b antiviral agents
KR102398439B1 (ko) 2016-03-07 2022-05-16 이난타 파마슈티칼스, 인코포레이티드 B형 간염 항바이러스제
BR112018071048A2 (pt) 2016-04-15 2019-05-07 Janssen Sciences Ireland Uc combinações e métodos que compreendem um inibidor da montagem de capsídeos
CN109153682B (zh) 2016-05-20 2021-05-25 豪夫迈·罗氏有限公司 用于治疗感染性疾病的具有氧、硫和氮连接基的新的吡嗪化合物
EP3463469B1 (en) 2016-05-27 2023-12-13 Gilead Sciences, Inc. Combination of ledipasvir and sofosbuvir for use in the treatment of hepatitis b virus infections in humans
BR102017010009A2 (pt) 2016-05-27 2017-12-12 Gilead Sciences, Inc. Compounds for the treatment of hepatitis b virus infection
JP2019521972A (ja) 2016-06-10 2019-08-08 エナンタ ファーマシューティカルズ インコーポレイテッド Ｂ型肝炎抗ウイルス剤
JP7051804B2 (ja) 2016-07-14 2022-04-11 エフ．ホフマン－ラ ロシュ アーゲー 感染症の治療のための６，７－ジヒドロ－４Ｈ－ピラゾロ［１，５－ａ］ピラジン化合物と６，７－ジヒドロ－４Ｈ－トリアゾロ［１，５－ａ］ピラジン化合物
EP3484883B1 (en) 2016-07-14 2020-04-15 H. Hoffnabb-La Roche Ag Novel tetrahydropyrazolopyridine compounds for the treatment of infectious diseases
WO2018011162A1 (en) 2016-07-14 2018-01-18 F. Hoffmann-La Roche Ag Carboxy 6,7-dihydro-4h-pyrazolo[1,5-a]pyrazine compounds for the treatment of infectious diseases
JOP20190024A1 (ar) 2016-08-26 2019-02-19 Gilead Sciences Inc مركبات بيروليزين بها استبدال واستخداماتها
WO2018045150A1 (en) 2016-09-02 2018-03-08 Gilead Sciences, Inc. 4,6-diamino-pyrido[3,2-d]pyrimidine derivaties as toll like receptor modulators
KR102268448B1 (ko) 2016-09-02 2021-06-22 길리애드 사이언시즈, 인코포레이티드 톨 유사 수용체 조정제 화합물
US10987360B2 (en) 2016-09-15 2021-04-27 Assembly Biosciences, Inc. Hepatitis B core protein modulators
EP4234691A3 (en) 2016-10-14 2023-10-18 Precision Biosciences, Inc. Engineered meganucleases specific for recognition sequences in the hepatitis b virus genome
AU2017353986B2 (en) 2016-11-07 2021-08-19 Arbutus Biopharma Corporation Substituted pyridinone-containing tricyclic compounds, and methods using same
WO2018086530A1 (zh) * 2016-11-08 2018-05-17 正大天晴药业集团股份有限公司 作为cccDNA抑制剂的磺酰胺类化合物
CN108264520B (zh) * 2017-01-03 2021-12-07 上海长森药业有限公司 用于治疗乙型肝炎的化合物及其用途
TWI714820B (zh) 2017-01-31 2021-01-01 美商基利科學股份有限公司 替諾福韋艾拉酚胺(tenofovir alafenamide)之晶型
JOP20180008A1 (ar) 2017-02-02 2019-01-30 Gilead Sciences Inc مركبات لعلاج إصابة بعدوى فيروس الالتهاب الكبدي b
CA3048278A1 (en) * 2017-02-07 2018-08-16 Janssen Pharmaceutica Nv Sulphamoylaryl derivatives and use thereof as medicaments for the treatment of liver fibrosis
RU2650610C1 (ru) 2017-02-28 2018-04-16 Васильевич Иващенко Александр Противовирусная композиция и способ ее применения
MX2019010404A (es) 2017-03-02 2019-11-21 Assembly Biosciences Inc Compuestos sulfamida cíclicos y métodos de uso de los mismos.
EP3601216B1 (en) 2017-03-21 2023-10-25 Arbutus Biopharma Corporation Substituted dihydroindene-4-carboxamides and analogs thereof, and methods using same for the treatment of hepatitis b virus infection
JOP20180040A1 (ar) 2017-04-20 2019-01-30 Gilead Sciences Inc مثبطات pd-1/pd-l1
RU2666727C1 (ru) * 2017-07-18 2018-09-12 Андрей Александрович Иващенко Ингибитор вируса гепатита В (ВГВ)
WO2019040102A1 (en) 2017-08-22 2019-02-28 Gilead Sciences, Inc. THERAPEUTIC HETEROCYCLIC COMPOUNDS
UY37861A (es) 2017-08-28 2019-03-29 Enanta Pharm Inc Agentes antivirales contra la hepatitis b
CN111448199A (zh) 2017-11-02 2020-07-24 艾库里斯有限及两合公司 具有抗乙型肝炎病毒(hbv)活性的新的高活性的氨基-噻唑取代的吲哚-2-甲酰胺
KR20200083552A (ko) 2017-11-02 2020-07-08 아이쿠리스 게엠베하 운트 코. 카게 B형 간염 바이러스 (hbv)에 활성인 신규 고활성 피라졸로-피페리딘 치환된 인돌-2-카르복스아미드
CN109879799B (zh) * 2017-12-06 2020-08-11 浙江司太立制药股份有限公司 含有4-羰氧基哌啶基的氨磺酰基苯甲酰胺类化合物及其制备方法
WO2019113173A1 (en) 2017-12-06 2019-06-13 Enanta Pharmaceuticals, Inc. Hepatitis b antiviral agents
US10723733B2 (en) 2017-12-06 2020-07-28 Enanta Pharmaceuticals, Inc. Hepatitis B antiviral agents
AU2018392212B9 (en) 2017-12-20 2021-03-18 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 2'3' cyclic dinucleotides with phosphonate bond activating the STING adaptor protein
US10966999B2 (en) 2017-12-20 2021-04-06 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3′3′ cyclic dinucleotides with phosphonate bond activating the sting adaptor protein
CN109988126B (zh) * 2017-12-29 2023-05-16 南京富润凯德生物医药有限公司 一种3-氨基-氧杂环丁烷衍生物及其制备方法和应用
US11058678B2 (en) 2018-01-22 2021-07-13 Enanta Pharmaceuticals, Inc. Substituted heterocycles as antiviral agents
WO2019154343A1 (zh) * 2018-02-09 2019-08-15 正大天晴药业集团股份有限公司 衣壳蛋白装配抑制剂、其药物组合物和用途
IL300572A (en) 2018-02-13 2023-04-01 Gilead Sciences Inc PD–1/PD–L1 inhibitors
CA3091142C (en) 2018-02-26 2023-04-11 Gilead Sciences, Inc. Substituted pyrrolizine compounds and uses thereof
TW202415645A (zh) 2018-03-01 2024-04-16 愛爾蘭商健生科學愛爾蘭無限公司 ２，４－二胺基喹唑啉衍生物及其醫學用途
CN111867582A (zh) 2018-03-14 2020-10-30 爱尔兰詹森科学公司 衣壳组装调节剂给药方案
US10729688B2 (en) 2018-03-29 2020-08-04 Enanta Pharmaceuticals, Inc. Hepatitis B antiviral agents
US10870691B2 (en) 2018-04-05 2020-12-22 Gilead Sciences, Inc. Antibodies and fragments thereof that bind hepatitis B virus protein X
TWI833744B (zh) 2018-04-06 2024-03-01 捷克科學院有機化學與生物化學研究所 3'3'-環二核苷酸
TWI818007B (zh) 2018-04-06 2023-10-11 捷克科學院有機化學與生物化學研究所 2'3'-環二核苷酸
TW202005654A (zh) 2018-04-06 2020-02-01 捷克科學院有機化學與生物化學研究所 ２，２，─環二核苷酸
US11142750B2 (en) 2018-04-12 2021-10-12 Precision Biosciences, Inc. Optimized engineered meganucleases having specificity for a recognition sequence in the Hepatitis B virus genome
WO2019204609A1 (en) 2018-04-19 2019-10-24 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
WO2019206072A1 (zh) * 2018-04-24 2019-10-31 浙江海正药业股份有限公司 磺酰胺芳基甲酰胺衍生物及其制备方法和用途
TW202014193A (zh) 2018-05-03 2020-04-16 捷克科學院有機化學與生物化學研究所 包含碳環核苷酸之2’3’－環二核苷酸
US11186579B2 (en) 2018-07-06 2021-11-30 Gilead Sciences, Inc. Therapeutic heterocyclic compounds
CA3103987C (en) 2018-07-06 2023-08-01 Gilead Sciences, Inc. Therapeutic heterocyclic compounds
KR20230159715A (ko) 2018-07-13 2023-11-21 길리애드 사이언시즈, 인코포레이티드 Pd-1/pd-l1 억제제
EP3597637A1 (en) * 2018-07-19 2020-01-22 Irbm S.P.A. Inhibitors of hepatitis b virus
TW202416959A (zh) 2018-07-27 2024-05-01 加拿大商愛彼特生物製藥公司 經取代四氫環戊[c]吡咯、經取代二氫吡咯𠯤，其類似物及使用其之方法
WO2020028097A1 (en) 2018-08-01 2020-02-06 Gilead Sciences, Inc. Solid forms of (r)-11-(methoxymethyl)-12-(3-methoxypropoxy)-3,3-dimethyl-8-0x0-2,3,8,13b-tetrahydro-1h-pyrido[2,1-a]pyrrolo[1,2-c] phthalazine-7-c arboxylic acid
MX2021003253A (es) 2018-09-21 2021-08-11 Enanta Pharm Inc Heterociclos funcionalizados como agentes antivirales.
JP2022508642A (ja) * 2018-10-05 2022-01-19 エモリー ユニバーシティ モノマーおよびマルチマー抗ｈｂｖ薬
CN113195055A (zh) 2018-10-22 2021-07-30 组装生物科学股份有限公司 用于hbv治疗的5元杂芳基甲酰胺化合物
EP3870566A1 (en) 2018-10-24 2021-09-01 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
KR102658602B1 (ko) 2018-10-31 2024-04-19 길리애드 사이언시즈, 인코포레이티드 Hpk1 억제 활성을 갖는 치환된 6-아자벤즈이미다졸 화합물
EP3873488A4 (en) 2018-10-31 2022-08-03 The University of Sydney COMPOSITIONS AND METHODS FOR THE TREATMENT OF VIRUS INFECTION
TW202136260A (zh) 2018-10-31 2021-10-01 美商基利科學股份有限公司 經取代之6-氮雜苯并咪唑化合物
UY38434A (es) 2018-11-02 2020-05-29 Aicuris Gmbh & Co Kg Nuevas 6,7-dihidro-4h-pirazolo[1,5-a]pirazin indol-2-carboxamidas activas contra el virus de la hepatitis b (hbv)
UY38436A (es) 2018-11-02 2020-05-29 Aicuris Gmbh & Co Kg Nuevas 6,7-dihidro-4h-pirazolo[1,5-a] pirazinindol-2-carboxamidas activas contra el virus de la hepatitis b (vhb)
CA3118339A1 (en) 2018-11-02 2020-05-07 Aicuris Gmbh & Co. Kg Novel urea 6,7-dihydro-4h-thiazolo[5,4-c]pyridines active against the hepatitis b virus (hbv)
UY38439A (es) 2018-11-02 2020-05-29 Aicuris Gmbh & Co Kg Novedosas urea 6,7-dihidro-4h-pirazolo[4,3-c]piridinas activas contra el virus de la hepatitis b (vhb)
AR117188A1 (es) 2018-11-02 2021-07-21 Aicuris Gmbh & Co Kg Derivados de urea 6,7-dihidro-4h-pirazolo[1,5-a]pirazinas activas contra el virus de la hepatitis b (vhb)
AR116948A1 (es) 2018-11-02 2021-06-30 Aicuris Gmbh & Co Kg Derivados de urea 6,7-dihidro-4h-pirazolo[1,5-a]pirazinas activas contra el virus de la hepatitis b (vhb)
AU2019385477A1 (en) 2018-11-21 2021-06-10 Enanta Pharmaceuticals, Inc. Functionalized heterocycles as antiviral agents
TW202415643A (zh) 2018-12-12 2024-04-16 加拿大商愛彼特生物製藥公司 經取代之芳基甲基脲類及雜芳基甲基脲類、其類似物及其使用方法
BR112021015618A2 (pt) 2019-02-22 2021-10-05 Janssen Sciences Ireland Unlimited Company Derivados de amida úteis no tratamento da infecção pelo hbv ou doenças induzidas pelo hbv
DK3934757T3 (da) 2019-03-07 2023-04-17 Inst Of Organic Chemistry And Biochemistry Ascr V V I 2'3'-cykliske dinukleotider og prodrugs deraf
WO2020178768A1 (en) 2019-03-07 2020-09-10 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator
KR20210137518A (ko) 2019-03-07 2021-11-17 인스티튜트 오브 오가닉 케미스트리 앤드 바이오케미스트리 에이에스 씨알 브이.브이.아이. 3'3'-사이클릭 다이뉴클레오티드 및 이의 프로드럭
TWI751516B (zh) 2019-04-17 2022-01-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
TW202212339A (zh) 2019-04-17 2022-04-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
KR20220003023A (ko) 2019-04-30 2022-01-07 아이쿠리스 게엠베하 운트 코. 카게 B형 간염 바이러스 (hbv)에 대해 활성인 신규 옥살릴 피페라진
WO2020221824A1 (en) 2019-04-30 2020-11-05 Aicuris Gmbh & Co. Kg Novel indolizine-2-carboxamides active against the hepatitis b virus (hbv)
MX2021013086A (es) 2019-04-30 2021-11-17 Aicuris Gmbh & Co Kg Nuevas fenil y piridil ureas activas contra el virus de la hepatitis b (vhb).
WO2020221826A1 (en) 2019-04-30 2020-11-05 Aicuris Gmbh & Co. Kg Novel indole-2-carboxamides active against the hepatitis b virus (hbv)
CA3132554A1 (en) 2019-05-06 2020-11-12 Bart Rudolf Romanie Kesteleyn Amide derivatives useful in the treatment of hbv infection or hbv-induced diseases
EP3972695A1 (en) 2019-05-23 2022-03-30 Gilead Sciences, Inc. Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors
EP3975996A1 (en) 2019-05-24 2022-04-06 Assembly Biosciences, Inc. Pharmaceutical compositions for the treatment of hbv
JPWO2020241814A1 (ru) * 2019-05-29 2020-12-03
US11236111B2 (en) 2019-06-03 2022-02-01 Enanta Pharmaceuticals, Inc. Hepatitis B antiviral agents
WO2020247575A1 (en) 2019-06-04 2020-12-10 Enanta Pharmaceuticals, Inc. Hepatitis b antiviral agents
WO2020247561A1 (en) 2019-06-04 2020-12-10 Enanta Pharmaceuticals, Inc, Hepatitis b antiviral agents
WO2020255012A1 (en) 2019-06-18 2020-12-24 Janssen Sciences Ireland Unlimited Company Combination of hepatitis b virus (hbv) vaccines and capsid assembly modulators being sulfonamide derivatives
US20220241402A1 (en) 2019-06-18 2022-08-04 Janssen Sciences Ireland Unlimited Company Combination of hepatitis b virus (hbv) vaccines and quinazoline derivatives
US20220305115A1 (en) 2019-06-18 2022-09-29 Janssen Sciences Ireland Unlimited Company Combination of hepatitis b virus (hbv) vaccines and pyridopyrimidine derivatives
EP3990476A1 (en) 2019-06-25 2022-05-04 Gilead Sciences, Inc. Flt3l-fc fusion proteins and methods of use
WO2021007488A1 (en) 2019-07-11 2021-01-14 Enanta Pharmaceuticals, Inc. Substituted heterocycles as antiviral agents
US20220257619A1 (en) 2019-07-18 2022-08-18 Gilead Sciences, Inc. Long-acting formulations of tenofovir alafenamide
EP4017476A1 (en) 2019-08-19 2022-06-29 Gilead Sciences, Inc. Pharmaceutical formulations of tenofovir alafenamide
CA3153358A1 (en) * 2019-09-04 2021-03-11 Taigen Biotechnology Co., Ltd. Hepatitis b antiviral agents
WO2021055425A2 (en) 2019-09-17 2021-03-25 Enanta Pharmaceuticals, Inc. Functionalized heterocycles as antiviral agents
DK4037708T3 (da) 2019-09-30 2024-09-30 Gilead Sciences Inc HBV-vacciner og fremgangsmåder til at behandle HBV
EP4069729A1 (en) 2019-12-06 2022-10-12 Precision BioSciences, Inc. Optimized engineered meganucleases having specificity for a recognition sequence in the hepatitis b virus genome
WO2021130270A1 (en) 2019-12-24 2021-07-01 F. Hoffmann-La Roche Ag Pharmaceutical combination of antiviral agents targeting hbv and/or an immune modulator for treatment of hbv
CA3167114A1 (en) * 2020-02-11 2021-08-19 Romano Di Fabio Spirocyclic inhibitors of hepatitis b virus
US11802125B2 (en) 2020-03-16 2023-10-31 Enanta Pharmaceuticals, Inc. Functionalized heterocyclic compounds as antiviral agents
AR121620A1 (es) 2020-03-20 2022-06-22 Gilead Sciences Inc Profármacos de nucleósidos 4’-c-sustituidos-2-halo-2’-deoxiadenosina y métodos de preparación y uso de los mismos
CN113493441B (zh) * 2020-04-03 2024-07-09 广东东阳光药业股份有限公司 新型螺环类化合物及其在药物中的应用
CN111349056B (zh) * 2020-04-16 2022-08-02 南京安纳康生物科技有限公司 用于乙型肝炎病毒感染的抗病毒剂
CN111393391B (zh) * 2020-04-16 2022-07-26 南京安纳康生物科技有限公司 用于乙型肝炎病毒感染的抗病毒剂
WO2021216656A1 (en) 2020-04-22 2021-10-28 Assembly Biosciences, Inc. 5-membered heteroaryl carboxamide compounds for treatment of hbv
WO2021216661A1 (en) 2020-04-22 2021-10-28 Assembly Biosciences, Inc. Pyrazole carboxamide compounds for treatment of hbv
CN115916341A (zh) 2020-04-22 2023-04-04 组装生物科学股份有限公司 用于治疗hbv的吡唑甲酰胺化合物
WO2021216660A1 (en) 2020-04-22 2021-10-28 Assembly Biosciences, Inc. 5-membered heteroaryl carboxamide compounds for treatment of hbv
BR112023002164A2 (pt) 2020-08-07 2023-03-14 Gilead Sciences Inc Profármacos de análogos de nucleotídeos de fosfonamida e seu uso farmacêutico
TW202406932A (zh) 2020-10-22 2024-02-16 美商基利科學股份有限公司 介白素2-Fc融合蛋白及使用方法
CA3217107A1 (en) 2021-05-13 2022-11-17 Daniel J. CLOUTIER Combination of a tlr8 modulating compound and anti-hbv sirna therapeutics
CA3222277A1 (en) 2021-06-23 2022-12-29 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
EP4359389A1 (en) 2021-06-23 2024-05-01 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
CA3222439A1 (en) 2021-06-23 2022-12-29 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
AU2022297367A1 (en) 2021-06-23 2023-12-07 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
WO2023069547A1 (en) 2021-10-20 2023-04-27 Assembly Biosciences, Inc. 5-membered heteroaryl carboxamide compounds for treatment of hbv
WO2023069544A1 (en) 2021-10-20 2023-04-27 Assembly Biosciences, Inc. 5-membered heteroaryl carboxamide compounds for treatment of hbv
WO2023069545A1 (en) 2021-10-20 2023-04-27 Assembly Biosciences, Inc. 5-membered heteroaryl carboxamide compounds for treatment of hbv
WO2023164183A1 (en) 2022-02-25 2023-08-31 Assembly Biosciences, Inc. Benzothia(dia)zepine compounds for treatment of hbv and hdv
WO2023164186A1 (en) 2022-02-25 2023-08-31 Assembly Biosciences, Inc. Benzothia(dia)zepine compounds for treatment of hbv and hdv
WO2023164179A1 (en) 2022-02-25 2023-08-31 Assembly Biosciences, Inc. Benzothia(dia)zepine compounds for treatment of hbv and hdv
WO2023164181A1 (en) 2022-02-25 2023-08-31 Assembly Biosciences, Inc. Benzothia(dia)zepine compounds for treatment of hbv and hdv
CN115677545B (zh) * 2022-10-28 2024-03-15 潍坊医学院 一种抗hbv磺胺苯甲酰胺类衍生物及其制备方法和应用

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002064618A2 (en) * 2001-02-09 2002-08-22 Massachusetts Institute Of Technology Methods of identifying agents that mediate polypeptide aggregation
US20050239833A1 (en) * 2004-03-05 2005-10-27 Kazantsev Aleksey G Compositions and methods for modulating interaction between polypeptides
US20100016310A1 (en) * 2006-08-17 2010-01-21 Boehringer Ingelheim International Gmbh Methods of using aryl sulfonyl compounds effective as soluble epoxide hydrolase inhibitors
US20110009622A1 (en) * 2008-04-24 2011-01-13 Makoto Jitsuoka Long-chain fatty acyl elongase inhibitor comprising arylsulfonyl derivative as active ingredient
WO2013006394A1 (en) * 2011-07-01 2013-01-10 Institute For Hepatitis And Virus Research Sulfamoylbenzamide derivatives as antiviral agents against hbv infection
WO2013096744A1 (en) * 2011-12-21 2013-06-27 Novira Therapeutics, Inc. Hepatitis b antiviral agents

Family Cites Families (217)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US1359583A (en) * 1919-11-28 1920-11-23 James W Doolittle Force-feed oil-cup
US1359596A (en) * 1919-12-08 1920-11-23 Pressure Proof Piston Ring Com Piston-ring
US3843662A (en) 1971-12-09 1974-10-22 Pfizer 2-halo-5-(substituted piperidino sulfonyl)benzoic acids
AU1508183A (en) 1982-06-04 1983-12-08 Beecham Group Plc Benzamide and anilide derivatives of 8-azabicyclo-(3.2.1)- -octane
WO1984003281A1 (en) 1983-02-19 1984-08-30 Beecham Group Plc Azabicycloalkyl benzamide and anilide derivatives
JPS62142164A (ja) 1985-12-13 1987-06-25 Ishihara Sangyo Kaisha Ltd ４，５−ジクロロイミダゾ−ル系化合物及びそれらを含有する有害生物防除剤
IN164880B (ru) * 1986-01-30 1989-06-24 Ishihara Sangyo Kaisha
US5272167A (en) 1986-12-10 1993-12-21 Schering Corporation Pharmaceutically active compounds
JP2606720B2 (ja) * 1987-03-13 1997-05-07 石原産業株式会社 イミダゾール系化合物及びそれらを含有する有害生物防除剤
CA1339133C (en) 1987-03-13 1997-07-29 Rikuo Nasu Imidazole compounds and biocidal composition comprising the same for controlling harmful organisms
US5571821A (en) * 1993-05-20 1996-11-05 Texas Biotechnology Corporation Sulfonamides and derivatives thereof that modulate the activity of endothelin
GB8904174D0 (en) 1989-02-23 1989-04-05 British Bio Technology Compounds
US4962101A (en) 1989-08-21 1990-10-09 Merck & Co., Inc. 2-(Heterocyclylalkyl)phenyl carbapenem antibacterial agents
GB9023082D0 (en) 1990-10-24 1990-12-05 Schering Agrochemicals Ltd Fungicides
GB9109557D0 (en) 1991-05-02 1991-06-26 Wellcome Found Chemical compounds
US5308826A (en) 1993-04-22 1994-05-03 Zeneca Limited Herbicidal 4-substituted pyridyl-3-carbinols
GB9405347D0 (en) * 1994-03-18 1994-05-04 Agrevo Uk Ltd Fungicides
ATE235470T1 (de) 1994-05-27 2003-04-15 Black James Foundation Gastrin- und cck-antagonisten
US5795907A (en) 1994-05-27 1998-08-18 James Black Foundation Limited Gastin and CCK receptor ligands
KR0131723B1 (ko) * 1994-06-08 1998-04-14 김주용 반도체소자 및 그 제조방법
US5763618A (en) 1995-05-12 1998-06-09 Konica Corporation Manufacturing method of sulfides
US5723411A (en) 1995-10-31 1998-03-03 E. I. Du Pont De Nemours And Company Herbicidal pyridazinones
DE19540995A1 (de) 1995-11-03 1997-05-07 Hoechst Ag Substituierte Sulfonimidamide, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament oder Diagnostikum sowie sie enthaltendes Medikament
GB9612884D0 (en) 1996-06-20 1996-08-21 Smithkline Beecham Plc Novel compounds
US6025367A (en) 1996-06-25 2000-02-15 Smithkline Beecham Plc Sulfonamide derivatives as 5HT7 receptor antagonists
WO1998023285A1 (en) 1996-11-29 1998-06-04 Smithkline Beecham Plc Use of a combination of penciclovir and alpha-interferon in the manufacture of a medicament for the treatment of hepatitis b
US5939423A (en) 1997-04-16 1999-08-17 Sciclone Pharmaceuticals, Inc. Treatment of hepatitis B infection with thymosin alpha 1 and famciclovir
US5919970A (en) 1997-04-24 1999-07-06 Allergan Sales, Inc. Substituted diaryl or diheteroaryl methanes, ethers and amines having retinoid agonist, antagonist or inverse agonist type biological activity
US5994396A (en) * 1997-08-18 1999-11-30 Centaur Pharmaceuticals, Inc. Furansulfonic acid derivatives and pharmaceutical compositions containing the same
ES2317688T3 (es) 1998-01-29 2009-04-16 Amgen Inc. Moduladores ppar-gamma.
EP1072263A4 (en) 1998-03-26 2004-03-31 Japan Tobacco Inc AMID DERIVATIVES AND NOCICEPTINANT AGONISTS
US6251893B1 (en) 1998-06-15 2001-06-26 Nps Allelix Corp. Bicyclic piperidine and piperazine compounds having 5-HT6 receptor affinity
CA2359440C (en) 1999-01-15 2009-04-14 Beate Gutterer Phenylphenanthridines with pde-iv inhibiting activity
IL147150A0 (en) 1999-07-16 2002-08-14 Warner Lambert Co Method for treating chronic pain using mek inhibitors
AU1840101A (en) 1999-08-10 2001-03-05 Chancellor, Masters And Scholars Of The University Of Oxford, The Long chain n-alkyl compounds and oxo-derivatives thereof
EP1216228B1 (en) 1999-09-17 2008-10-29 Millennium Pharmaceuticals, Inc. BENZAMIDES AND RELATED INHIBITORS OF FACTOR Xa
AR025884A1 (es) 1999-10-01 2002-12-18 Takeda Pharmaceutical Compuestos de amina ciclica, su produccion y su uso
AU2018301A (en) 1999-12-28 2001-07-24 Pfizer Products Inc. Non-peptidyl inhibitors of vla-4 dependent cell binding useful in treating inflammatory, autoimmune, and respiratory diseases
AU2882801A (en) 2000-01-28 2001-08-07 Kaken Pharmaceutical Co., Ltd. Azepine derivatives
US6511980B2 (en) 2000-05-05 2003-01-28 Ortho Mcneil Pharmaceutical, Inc. Substituted diamine derivatives useful as motilin antagonists
EP1193268A1 (en) 2000-09-27 2002-04-03 Applied Research Systems ARS Holding N.V. Pharmaceutically active sulfonamide derivatives bearing both lipophilic and ionisable moieties as inhibitors of protein Junkinases
WO2002051410A2 (en) 2000-12-22 2002-07-04 Akzo Nobel N.V. Phenylthiazole and thiazoline derivatives and their use as antiparasitics
JPWO2002053566A1 (ja) 2000-12-27 2004-05-13 住友製薬株式会社 新規なカルバペネム化合物
US6650463B2 (en) 2001-03-13 2003-11-18 Seiko Epson Corporation Electrophoretic display device
KR100713137B1 (ko) 2001-06-28 2007-05-02 동화약품공업주식회사 신규의 2,4-디플루오로벤즈아미드 유도체
AU2002317377A1 (en) 2001-07-20 2003-03-03 Cancer Research Technology Limited Biphenyl apurinic/apyrimidinic site endonuclease inhibitors to treat cancer
DE10136043A1 (de) 2001-07-25 2003-02-13 Degussa Verfahren zur Herstellung von modifiziertem Ruß
US6956035B2 (en) 2001-08-31 2005-10-18 Inotek Pharmaceuticals Corporation Isoquinoline derivatives and methods of use thereof
JP2005514366A (ja) 2001-11-20 2005-05-19 イーライ・リリー・アンド・カンパニー ３−置換オキシインドールβ３アゴニスト
SE0201635D0 (sv) 2002-05-30 2002-05-30 Astrazeneca Ab Novel compounds
EP1512396A4 (en) 2002-06-05 2008-12-31 Inst Med Molecular Design Inc INHIBITORS OF AP-1 AND NFAT ACTIVATION
BR0312023A (pt) 2002-06-27 2005-03-22 Novo Nordisk As Composto, composto ativador da glicose cinase, método para evitar a hipoglicemia, uso de um composto, e, composição farmacêutica
CN1678311A (zh) 2002-06-27 2005-10-05 诺沃挪第克公司 用作治疗剂的芳基羰基衍生物
AU2003256923A1 (en) 2002-07-31 2004-02-16 Smithkline Beecham Corporation Substituted benzanilides as modulators of the ccr5 receptor
WO2004011427A2 (en) 2002-07-31 2004-02-05 Smithkline Beecham Corporation Substituted benzanilides as modulators of the ccr5 receptor
US7186735B2 (en) 2002-08-07 2007-03-06 Sanofi-Aventis Deutschland Gmbh Acylated arylcycloalkylamines and their use as pharmaceuticals
US7338956B2 (en) 2002-08-07 2008-03-04 Sanofi-Aventis Deutschland Gmbh Acylamino-substituted heteroaromatic compounds and their use as pharmaceuticals
WO2004014428A1 (ja) 2002-08-09 2004-02-19 Ajinomoto Co.,Inc. 腸疾患および内臓痛の治療薬
US20040110802A1 (en) * 2002-08-23 2004-06-10 Atli Thorarensen Antibacterial benzoic acid derivatives
MXPA05002575A (es) 2002-09-06 2005-09-08 Johnson & Johnson Compuestos heterociclicos.
SE0202838D0 (sv) 2002-09-24 2002-09-24 Astrazeneca Ab Chemical compounds
WO2004058709A1 (en) 2002-12-23 2004-07-15 Millennium Pharmaceuticals, Inc. Ccr8 inhibitors
US7320989B2 (en) 2003-02-28 2008-01-22 Encysive Pharmaceuticals, Inc. Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-II receptor antagonists
ATE524452T1 (de) 2003-03-27 2011-09-15 Cytokinetics Inc Sulfonamide zur behandlung von kongestivem herzversagen, deren zusammensetzungen und verwendungen.
JP2006525366A (ja) 2003-04-30 2006-11-09 ジ インスチチュート フォー ファーマシューティカル ディスカバリー、エルエルシー 複素環式カルボン酸置換基
JP2006528685A (ja) 2003-05-06 2006-12-21 スミスクライン ビーチャム コーポレーション 新規化合物
CL2004001011A1 (es) 2003-05-13 2005-03-18 Schering Corp Compuestos azabiciclicos derivados de n-arilsulfonilpiperidinas; inhibidores de la deposicion de la proteina beta amiloide; composicion farmaceutica; y su uso para el tratamiento del alzheimer y enfermedades neurodegenerativas.
US7915293B2 (en) 2003-05-30 2011-03-29 Rigel Pharmaceuticals, Inc. Ubiquitin ligase inhibitors
US20110275630A1 (en) 2003-06-02 2011-11-10 Abbott Laboratories Isoindolinone kinase inhibitors
EP1631559A4 (en) 2003-06-06 2008-08-27 Smithkline Beecham Corp IL-8 SB / SB RECEPTOR ANTAGONISTS
AR045047A1 (es) 2003-07-11 2005-10-12 Arena Pharm Inc Derivados arilo y heteroarilo trisustituidos como moduladores del metabolismo y de la profilaxis y tratamiento de desordenes relacionados con los mismos
GB0319151D0 (en) 2003-08-14 2003-09-17 Glaxo Group Ltd Novel compounds
US8084457B2 (en) 2003-09-15 2011-12-27 Lead Discovery Center Gmbh Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases
GB0325956D0 (en) 2003-11-06 2003-12-10 Addex Pharmaceuticals Sa Novel compounds
US7498050B2 (en) 2003-12-15 2009-03-03 Kraft Foods Global Brands Llc Edible spread composition and packaged product
DE102004009238A1 (de) 2004-02-26 2005-09-08 Merck Patent Gmbh Arylamid-Derivate
EP1758856A2 (en) 2004-05-04 2007-03-07 Novo Nordisk A/S Indole derivatives for the treatment of obesity
WO2005115374A1 (en) 2004-05-29 2005-12-08 7Tm Pharma A/S Crth2 receptor ligands for therapeutic use
EP1768667B1 (en) 2004-06-22 2009-09-30 Schering Corporation Cannabinoid receptor ligands
RU2470916C2 (ru) 2004-07-30 2012-12-27 Экселиксис, Инк. Производные пиррола как лекарственные вещества
DE102004042441A1 (de) 2004-08-31 2006-04-06 Sanofi-Aventis Deutschland Gmbh Mit Aminosäuren substituierte Hexahydro-pyrazino(1,2-a)pyrimidin-4,7-dionderivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
KR20070048798A (ko) 2004-08-31 2007-05-09 아스트라제네카 아베 퀴나졸리논 유도체 및 이것의 ｂ-ｒａｆ 억제제로서의 용도
WO2006044457A1 (en) 2004-10-13 2006-04-27 Wyeth N-benzenesulfonyl substituted anilino-pyrimidine analogs
JP2008517057A (ja) 2004-10-19 2008-05-22 ノバルティス ヴァクシンズ アンド ダイアグノスティクス， インコーポレイテッド インドールおよびベンゾイミダゾール誘導体
US7919487B2 (en) 2004-11-10 2011-04-05 Synta Pharmaceuticals Corporation Heteroaryl compounds
US20060122236A1 (en) 2004-12-06 2006-06-08 Wood Michael R Substituted biaryl-carboxylate derivatives
TW200635899A (en) 2004-12-22 2006-10-16 Astrazeneca Ab Chemical compounds
AR054183A1 (es) 2004-12-22 2007-06-06 Astrazeneca Ab Derivados de piridincarboxamida y su uso como agentes anticancerigenos. procesos de obtencion y composiciones farmaceuticas.
FI117653B (fi) 2005-02-21 2006-12-29 Eigenor Oy Menetelmä ja laitteisto liikkuvien kohteiden havaitsemiseksi tutkalla
GB0510141D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B3
US20070032493A1 (en) 2005-05-26 2007-02-08 Synta Pharmaceuticals Corp. Method for treating B cell regulated autoimmune disorders
WO2006128129A2 (en) 2005-05-26 2006-11-30 Synta Pharmaceuticals Corp. Method for treating cancer
US7790726B2 (en) 2005-08-16 2010-09-07 Chemocentryx, Inc. Monocyclic and bicyclic compounds and methods of use
DK1940786T3 (da) 2005-09-16 2010-11-08 Arrow Therapeutics Ltd Biphenylderivater og deres anvendelse ved behandling af hepatitis C
WO2007070556A2 (en) 2005-12-12 2007-06-21 Genelabs Technologies, Inc. N-(6-membered aromatic ring)-amido anti-viral compounds
MX2008008340A (es) 2005-12-21 2008-09-03 Schering Corp Tratamiento de enfermedad de higado graso no alcoholica usando agentes reductores de colesterol y/o antagonista/agonista inverso de receptor de histamina 3.
EP1981849A1 (en) 2005-12-29 2008-10-22 LEK Pharmaceuticals D.D. Heterocyclic compounds
EP2019830A4 (en) 2006-05-04 2011-01-19 Inst Hepatitis & Virus Res INHIBITORS OF THE SECRETION OF HEPATITIS B VIRUS ANTIGENS FOR THE TREATMENT OF A CHRONIC HEPATITIS VIRUS
US20080021063A1 (en) 2006-07-18 2008-01-24 Kazantsev Aleksey G Compositions and methods for modulating sirtuin activity
US8153803B2 (en) * 2006-07-18 2012-04-10 The General Hospital Corporation Compositions and methods for modulating sirtuin activity
FR2903985B1 (fr) 2006-07-24 2008-09-05 Sanofi Aventis Sa Derives de n-(amino-heteroaryl)-1h-indole-2-carboxamides, leur preparation et leur application en therapeutique
FR2904316B1 (fr) 2006-07-31 2008-09-05 Sanofi Aventis Sa Derives de n-(amino-heteroaryl)-1h-indole-2-carboxamides, leur preparation et leur application en therapeutique.
AU2007314521A1 (en) 2006-10-06 2008-05-08 Merck Sharp & Dohme Corp. Non-nucleoside reverse transcriptase inhibitors
US8808702B2 (en) 2006-12-13 2014-08-19 Temple University-Of The Commonwealth System Of Higher Education Sulfide, sulfoxide and sulfone chalcone analogues, derivatives thereof and therapeutic uses thereof
US8071779B2 (en) 2006-12-18 2011-12-06 Inspire Pharmaceuticals, Inc. Cytoskeletal active rho kinase inhibitor compounds, composition and use
US20100022517A1 (en) 2006-12-18 2010-01-28 Richards Lori A Ophthalmic formulation of rho kinase inhibitor compound
FR2910473B1 (fr) 2006-12-26 2009-02-13 Sanofi Aventis Sa Derives de n-(amino-heteroaryl)-1h-pyrrolopyridine-2- carboxamides, leur preparation et leur application en therapeutique.
JP2008179621A (ja) 2006-12-28 2008-08-07 Taisho Pharmaceutical Co Ltd 含窒素飽和複素環化合物
US9001047B2 (en) 2007-01-07 2015-04-07 Apple Inc. Modal change based on orientation of a portable multifunction device
JP2008184403A (ja) 2007-01-29 2008-08-14 Japan Health Science Foundation 新規ｃ型肝炎ウイルス阻害剤
MX2009009873A (es) 2007-03-15 2009-09-24 Novartis Ag Compuestos organicos y sus usos.
US8097728B2 (en) 2007-04-30 2012-01-17 Philadelphia Health & Education Corporation Iminosugar compounds with antiflavirus activity
CA2686382C (en) 2007-05-04 2013-09-17 Irm Llc Phenylaminopyrimidine derivatives and compositions thereof as c-kit and pdgfr kinase inhibitors
CN101328169B (zh) 2007-06-18 2011-05-25 张中能 一种乙氧碳酰基-取代噻唑二氢嘧啶
WO2009018219A2 (en) * 2007-07-28 2009-02-05 University Of Chicago Methods and compositions for modulating rad51 and homologous recombination
CA2695071A1 (en) 2007-08-02 2009-02-05 F. Hoffmann-La Roche Ag The use of benzamide derivatives for the treatment of cns disorders
CN101429166B (zh) 2007-11-07 2013-08-21 上海特化医药科技有限公司 喹唑啉酮衍生物及其制备方法和用途
WO2009086303A2 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
FR2926554B1 (fr) 2008-01-22 2010-03-12 Sanofi Aventis Derives de carboxamides azabicycliques, leur preparation et leur application en therapeutique
FR2926556B1 (fr) 2008-01-22 2010-02-19 Sanofi Aventis Derives de carboxamides n-azabicycliques, leur preparation et leur application en therapeutique
FR2926555B1 (fr) 2008-01-22 2010-02-19 Sanofi Aventis Derives bicycliques de carboxamides azabicycliques, leur preparation et leur application en therapeutique
FR2926553B1 (fr) 2008-01-23 2010-02-19 Sanofi Aventis Derives d'indole-2-carboxamides et d'azaindole-2- carboxamides substitues par un groupe silanyle, leur preparation et leur application en therapeutique
CU20080028A6 (es) 2008-02-29 2011-02-24 Ct Ingenieria Genetica Biotech Compuestos químicos obtenidos in silico para la preparación de composiciones farmacéuticas para atenuar o inhibir la infección por virus dengue y otros flavivirus
WO2009146013A1 (en) 2008-03-31 2009-12-03 Georgetown University Myosin light chain phosphatase inhibitors
US20100008968A1 (en) 2008-06-26 2010-01-14 Lampe John W Method for treating cardiovascular diseases using rho kinase inhibitor compounds
US8410147B2 (en) 2008-06-26 2013-04-02 Inspire Pharmaceuticals, Inc. Method for treating diseases associated with alterations in cellular integrity using Rho kinase inhibitor compounds
US20090325959A1 (en) 2008-06-26 2009-12-31 Vittitow Jason L Method for treating ophthalmic diseases using rho kinase inhibitor compounds
US8207195B2 (en) 2008-06-26 2012-06-26 Inspire Pharmaceuticals, Inc. Method for treating neurological and neuropathic diseases using rho kinase inhibitor compounds
WO2009158587A1 (en) 2008-06-26 2009-12-30 Inspire Pharmaceuticals, Inc. Method for treating pulmonary diseases using rho kinase inhibitor compounds
US20090325960A1 (en) 2008-06-26 2009-12-31 Fulcher Emilee H Method for treating inflammatory diseases using rho kinase inhibitor compounds
CN102149677A (zh) 2008-08-15 2011-08-10 霍夫曼-拉罗奇有限公司 联芳基氨基四氢化萘类
WO2010027996A1 (en) 2008-09-02 2010-03-11 Institute For Hepatitis And Virus Research Novel imino sugar derivatives demonstrate potent antiviral activity and reduced toxicity
US8143269B2 (en) * 2008-10-03 2012-03-27 Calcimedica, Inc. Inhibitors of store operated calcium release
WO2010043592A1 (en) 2008-10-15 2010-04-22 Revotar Biopharmaceuticals Ag Lipase inhibitors for use for the treatment of obesity
AR074199A1 (es) 2008-11-20 2010-12-29 Glaxosmithkline Llc Compuesto de 6-(4-pirimidinil)-1h-indazol, composiciones farmaceuticas que lo comprenden y su uso para preparar un medicamento util para el tratamiento o disminucion de la gravedad del cancer.
EP2400969A4 (en) 2008-12-04 2012-05-16 Inspire Pharmaceuticals Inc METHOD FOR TREATING PULMONARY DISEASES USING RHO KINASE INHIBITORY COMPOUNDS
US8273754B2 (en) 2008-12-30 2012-09-25 Arqule, Inc. Substituted 1H-pyrazolo[3,4-D]pyrimidine-6-amine compounds
WO2010088000A2 (en) 2009-02-02 2010-08-05 Angion Biomedica Corp. Antifibrotic compounds and uses thereof
WO2010123139A1 (ja) * 2009-04-24 2010-10-28 持田製薬株式会社 スルファモイル基を有するアリールカルボキサミド誘導体
WO2010133336A1 (en) 2009-05-19 2010-11-25 Bayer Cropscience Ag Insecticidal arylpyrrolines
CN102480957A (zh) 2009-05-27 2012-05-30 Ptc医疗公司 治疗癌症及非肿瘤病症的方法
BRPI1009034A2 (pt) 2009-06-30 2019-09-24 Siga Tech Inc composição farmacêutica e método para o tratamento ou profilaxia de uma infecção viral ou doença associada a mesma
US8703938B2 (en) 2009-09-11 2014-04-22 Enanta Pharmaceuticals, Inc. Hepatitis C virus inhibitors
US8822700B2 (en) 2009-09-11 2014-09-02 Enanta Pharmaceuticals, Inc. Hepatitis C virus inhibitors
US20120252792A1 (en) 2009-09-17 2012-10-04 The Regents Of The University Of Michigan Methods and compositions for modulating rho-mediated gene transcription
US9051296B2 (en) 2009-11-16 2015-06-09 Raqualia Pharma Inc. Aryl carboxamide derivatives as TTX-S blockers
CN102093320B (zh) 2009-12-09 2013-08-28 扬子江药业集团上海海尼药业有限公司 一种可溶性环氧化物水解酶抑制剂
US9315454B2 (en) 2010-01-15 2016-04-19 Boehringer Ingelheim International Gmbh Compounds which modulate the CB2 receptor
WO2011088561A1 (en) 2010-01-20 2011-07-28 University Of Manitoba Anti-viral compounds and compositions
WO2011109237A2 (en) 2010-03-02 2011-09-09 Emory University Uses of noscapine and derivatives in subjects diagnosed with fap
EP2545042A1 (en) 2010-03-11 2013-01-16 Bristol-Myers Squibb Company Compounds for the treatment of hepatitis c
CN102206172B (zh) * 2010-03-30 2015-02-25 中国医学科学院医药生物技术研究所 一组取代双芳基化合物及其制备方法和抗病毒应用
JP2013523766A (ja) 2010-03-31 2013-06-17 グラクソ グループ リミテッド キナーゼ阻害剤としてのイミダゾリル‐イミダゾール
EP3246027A1 (en) 2010-05-07 2017-11-22 GlaxoSmithKline LLC Indole derivatives for the treatment of cancer
WO2011155898A1 (en) 2010-06-11 2011-12-15 Wadell Goeran New antiviral compounds
WO2011163593A2 (en) 2010-06-25 2011-12-29 Philadelphia Health & Education Corporation D/B/A Drexel Induction of immune response
AU2011279909A1 (en) 2010-07-19 2013-01-24 Inspire Pharmaceuticals, Inc. Bifunctional rho kinase inhibitor compounds, composition and use
EP2598478A2 (en) 2010-07-26 2013-06-05 Neurotherapeutics Pharma, Inc. Arylsulfonamide derivatives, compositions, and methods of use
CN103249305A (zh) 2010-07-27 2013-08-14 印斯拜尔药品股份有限公司 使用前药形式的激酶抑制剂化合物治疗眼科疾病的方法
WO2012016133A2 (en) 2010-07-29 2012-02-02 President And Fellows Of Harvard College Ros1 kinase inhibitors for the treatment of glioblastoma and other p53-deficient cancers
WO2012033956A1 (en) 2010-09-08 2012-03-15 Mithridion, Inc. Cognition enhancing compounds and compositions, methods of making, and methods of treating
WO2012047856A2 (en) 2010-10-04 2012-04-12 Institute For Hepatitis And Virus Research Novel inhibitors of secretion of hepatitis b virus antigens
GB201017345D0 (en) 2010-10-14 2010-11-24 Proximagen Ltd Receptor antagonists
ES2585396T3 (es) 2010-12-02 2016-10-05 VIIV Healthcare UK (No.5) Limited Alquilamidas como inhibidores de la unión del VIH
WO2012080050A1 (en) 2010-12-14 2012-06-21 F. Hoffmann-La Roche Ag Solid forms of a phenoxybenzenesulfonyl compound
GB201103419D0 (ru) 2011-02-28 2011-04-13 Univ Aberdeen
SI3330257T1 (sl) 2011-04-08 2020-07-31 Janssen Sciences Ireland Unlimited Company Derivati pirimidina za zdravljenje virusnih okužb
US8889716B2 (en) 2011-05-10 2014-11-18 Chdi Foundation, Inc. Transglutaminase TG2 inhibitors, pharmaceutical compositions, and methods of use thereof
AR089671A1 (es) 2012-01-06 2014-09-10 Janssen R & D Ireland 1,4-dihidropirimidinas 4,4-disustituidas y su uso como medicamentos para el tratamiento de la hepatitis b
US9657013B2 (en) * 2012-02-29 2017-05-23 Baruch S. Blumberg Institute Inhibitors of hepatitis B virus covalently closed circular DNA formation and their method of use
CN104144924B (zh) 2012-03-31 2016-02-24 弗·哈夫曼-拉罗切有限公司 用于治疗和预防乙型肝炎病毒感染的4-甲基-二氢嘧啶类
US20130267517A1 (en) 2012-03-31 2013-10-10 Hoffmann-La Roche Inc. Novel 4-methyl-dihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection
JP6140815B2 (ja) 2012-05-25 2017-05-31 ヤンセン・サイエンシズ・アイルランド・ユーシー ウラシルスピロオキセタンヌクレオシド
SG11201407970VA (en) 2012-06-01 2014-12-30 Univ Drexel Modulation of hepatitis b virus cccdna transcription
JO3300B1 (ar) 2012-06-06 2018-09-16 Novartis Ag مركبات وتركيبات لتعديل نشاط egfr
AR092348A1 (es) 2012-07-11 2015-04-15 Hoffmann La Roche DERIVADOS DE ARIL-SULTAMO COMO MODULADORES DE RORc
SG11201501360TA (en) 2012-08-28 2015-03-30 Janssen Sciences Ireland Uc Fused bicyclic sulfamoyl derivatives and the use thereof as medicaments for the treatment of hepatitis b
KR20210081451A (ko) 2012-08-28 2021-07-01 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 설파모일-아릴아미드 및 b형 간염 치료제로서의 그 용도
BR112015004113A2 (pt) 2012-09-10 2017-07-04 Hoffmann La Roche 6-aminoácido heteroarila diidropirimidinas para o tratamento e profilaxia da infecção pelo vírus da hepatite b
CA2896554C (en) * 2012-12-27 2019-11-05 Drexel University Novel antiviral agents against hbv infection
WO2014131847A1 (en) * 2013-02-28 2014-09-04 Janssen R&D Ireland Sulfamoyl-arylamides and the use thereof as medicaments for the treatment of hepatitis b
TWI622592B (zh) 2013-02-28 2018-05-01 衛材Ｒ＆Ｄ企管股份有限公司 四氫咪唑並［１，５－ｄ］［１，４］氧氮雜卓衍生物
US8993771B2 (en) 2013-03-12 2015-03-31 Novira Therapeutics, Inc. Hepatitis B antiviral agents
WO2014151958A1 (en) 2013-03-14 2014-09-25 VenatoRx Pharmaceuticals, Inc. Beta-lactamase inhibitors
HUE033542T2 (en) * 2013-04-03 2017-12-28 Janssen Sciences Ireland Uc Their use as medicaments for the treatment of N-phenylcarboxamide derivatives and hepatitis B
TW201512193A (zh) 2013-05-17 2015-04-01 Hoffmann La Roche 用於治療及防治ｂ型肝炎病毒感染之新穎６－橋聯雜芳基二氫嘧啶
AU2014267235B2 (en) 2013-05-17 2017-10-05 Janssen Sciences Ireland Uc Sulphamoylthiophenamide derivatives and the use thereof as medicaments for the treatment of hepatitis B
JO3603B1 (ar) 2013-05-17 2020-07-05 Janssen Sciences Ireland Uc مشتقات سلفامويل بيرولاميد واستخدامها كادوية لمعالجة التهاب الكبد نوع بي
US9688681B2 (en) 2013-05-28 2017-06-27 Bayer Cropscience Aktiengesellschaft Heterocyclic compounds as pest control agents
HUE035738T2 (en) 2013-05-28 2018-05-28 Astrazeneca Ab Chemical compounds
WO2014198880A1 (en) 2013-06-14 2014-12-18 Ferrer Internacional, S.A. 2-(2-aminophenoxy)-3-chloronaphthalene-1,4-dione compounds having orexin 2 receptor agonist activity
HUE039152T2 (hu) 2013-07-25 2018-12-28 Janssen Sciences Ireland Uc Glioxamiddal szubsztituált pirrolamid-származékok és alkalmazásuk hepatitisz B kezelésére szolgáló gyógyszerként
WO2015055764A1 (en) 2013-10-18 2015-04-23 Syngenta Participations Ag 3-methanimidamid-pyridine derivatives as fungicides
AU2014337298B2 (en) 2013-10-18 2018-12-06 Indiana University Research And Technology Corporation Hepatitis B viral assembly effectors
DK3060547T3 (en) 2013-10-23 2018-01-15 Janssen Sciences Ireland Uc CARBOXAMIDE DERIVATIVES AND USE THEREOF AS MEDICINES FOR TREATMENT OF HEPATITS B
ES2777248T3 (es) 2013-11-14 2020-08-04 Novira Therapeutics Inc Derivados de azepano y métodos de tratar infecciones por hepatitis B
JO3466B1 (ar) 2013-12-20 2020-07-05 Takeda Pharmaceuticals Co مواد ضابطة لتترا هيدرو بيريدوبيرازينات من gpr6
US9169212B2 (en) 2014-01-16 2015-10-27 Novira Therapeutics, Inc. Azepane derivatives and methods of treating hepatitis B infections
US9181288B2 (en) 2014-01-16 2015-11-10 Novira Therapeutics, Inc. Azepane derivatives and methods of treating hepatitis B infections
KR102331422B1 (ko) 2014-01-31 2021-11-25 카그니션 테라퓨틱스, 인코퍼레이티드 아이소인돌린 조성물 및 신경퇴행성 질환을 치료하는 방법
KR20160128305A (ko) 2014-02-05 2016-11-07 노비라 테라퓨틱스, 인코포레이티드 Hbv 감염의 치료를 위한 병용 요법
EA035848B1 (ru) 2014-02-06 2020-08-20 Янссен Сайенсиз Айрлэнд Юси Производные сульфамоилпирроламида и их применение в качестве медикаментов для лечения гепатита b
MY188114A (en) 2014-03-07 2021-11-21 Hoffmann La Roche Novel 6-fused heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection
EP3116316B1 (en) 2014-03-13 2019-07-10 Indiana University Research and Technology Corporation Hepatitis b core protein allosteric modulators
US9400280B2 (en) 2014-03-27 2016-07-26 Novira Therapeutics, Inc. Piperidine derivatives and methods of treating hepatitis B infections
MY196243A (en) 2014-03-28 2023-03-24 Sunshine Lake Pharma Co Ltd Dihydropyrimidine Compounds and Their Application In Pharmaceuticals
JP6710642B2 (ja) 2014-05-30 2020-06-17 チル ファーマシューティカル カンパニー リミテッド Ｈｂｖ阻害剤としてのジヒドロピリミジン縮環誘導体
JP2018504373A (ja) 2014-12-02 2018-02-15 ノヴィラ・セラピューティクス・インコーポレイテッド Ｈｂｖ治療用のスルフィドアルキル及びピリジルリバーススルホンアミド化合物
CA2972434A1 (en) 2014-12-30 2016-07-07 Novira Therapeutics, Inc. Derivatives and methods of treating hepatitis b infections
MA41338B1 (fr) 2015-01-16 2019-07-31 Hoffmann La Roche Composés de pyrazine pour le traitement de maladies infectieuses
WO2016149581A1 (en) 2015-03-19 2016-09-22 Novira Therapeutics, Inc. Azocane and azonane derivatives and methods of treating hepatitis b infections
WO2016161268A1 (en) 2015-04-01 2016-10-06 Enanta Pharmaceuticals, Inc. Hepatitis b antviral agents
WO2016168619A1 (en) 2015-04-17 2016-10-20 Indiana University Research And Technology Corporation Hepatitis b viral assembly effectors
WO2016183266A1 (en) 2015-05-13 2016-11-17 Enanta Pharmaceuticals, Inc. Ehpatitis b antiviral agents
US10875876B2 (en) 2015-07-02 2020-12-29 Janssen Sciences Ireland Uc Cyclized sulfamoylarylamide derivatives and the use thereof as medicaments for the treatment of hepatitis B
AU2016330964B2 (en) 2015-09-29 2021-04-01 Novira Therapeutics, Inc. Crystalline forms of a hepatitis B antiviral agent
CN109251212A (zh) 2017-07-14 2019-01-22 上海长森药业有限公司 内环硫醚酰胺-芳基酰胺类化合物及其治疗乙型肝炎的用途

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002064618A2 (en) * 2001-02-09 2002-08-22 Massachusetts Institute Of Technology Methods of identifying agents that mediate polypeptide aggregation
US20050239833A1 (en) * 2004-03-05 2005-10-27 Kazantsev Aleksey G Compositions and methods for modulating interaction between polypeptides
US20100016310A1 (en) * 2006-08-17 2010-01-21 Boehringer Ingelheim International Gmbh Methods of using aryl sulfonyl compounds effective as soluble epoxide hydrolase inhibitors
US20110009622A1 (en) * 2008-04-24 2011-01-13 Makoto Jitsuoka Long-chain fatty acyl elongase inhibitor comprising arylsulfonyl derivative as active ingredient
WO2013006394A1 (en) * 2011-07-01 2013-01-10 Institute For Hepatitis And Virus Research Sulfamoylbenzamide derivatives as antiviral agents against hbv infection
WO2013096744A1 (en) * 2011-12-21 2013-06-27 Novira Therapeutics, Inc. Hepatitis b antiviral agents

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
D. CAI, C. MILLS, W. YU, R. YAN, C. E. ALDRICH, J. R. SAPUTELLI, W. S. MASON, X. XU, J.-T. GUO, T. M. BLOCK, A. CUCONATI, H. GUO: "Identification of Disubstituted Sulfonamide Compounds as Specific Inhibitors of Hepatitis B Virus Covalently Closed Circular DNA Formation", ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, AMERICAN SOCIETY FOR MICROBIOLOGY., vol. 56, no. 8, 1 August 2012 (2012-08-01), pages 4277 - 4288, XP055059505, ISSN: 00664804, DOI: 10.1128/AAC.00473-12 *
LAMBENG, N. LEBON, F. CHRISTOPHE, B. BURTON, M. DE RYCK, M. QUERE, L.: "Arylsulfonamides as a new class of cannabinoid CB"1 receptor ligands: Identification of a lead and initial SAR studies", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, AMSTERDAM, NL, vol. 17, no. 1, 22 December 2006 (2006-12-22), AMSTERDAM, NL, pages 272 - 277, XP005812156, ISSN: 0960-894X, DOI: 10.1016/j.bmcl.2006.09.049 *
MAI S MABROUK: "Discovering best candidates for Hepatocellular Carcinoma (HCC) by in-silico techniques and tools", INT. J. BIOINFORMATICS RESEARCH AND APPLICATIONS, vol. 8, no. 1/2, 1 January 2012 (2012-01-01), pages 141 - 152, XP055059465, DOI: 10.1504/IJBRA.2012.045956 *
NAM DOO KIM; HAARIN CHUN; SANG JIN PARK; JAE WON YANG; JONG WOO KIM; SOON KIL AHN;: "Discovery of novel HCV polymerase inhibitors using pharmacophore-based virtual screening", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, AMSTERDAM, NL, vol. 21, no. 11, 4 April 2011 (2011-04-04), AMSTERDAM, NL, pages 3329 - 3334, XP028211474, ISSN: 0960-894X, DOI: 10.1016/j.bmcl.2011.04.010 *
ZHANG XIAOQIAN; SMITH DONNA L; MERIIN ANATOLI B; ENGEMANN SABINE; RUSSEL DEBORAH E; ROARK MARGO; WASHINGTON SHETIA L; MAXWELL MICH: "A potent small molecule inhibits polyglutamine aggregation in Huntington's disease neurons and suppresses neurodegeneration in vivo.", PROCEEDINGS NATIONAL ACADEMY OF SCIENCES PNAS, NATIONAL ACADEMY OF SCIENCES, US, vol. 102, no. 3, 18 January 2005 (2005-01-18), US, pages 892 - 897, XP009116402, ISSN: 0027-8424, DOI: 10.1073/pnas.0408936102 *

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Publication number Priority date Publication date Assignee Title
RU2710928C2 (ru) * 2014-07-31 2020-01-14 Инсерм (Институт Насьональ Де Ла Сант Эт Де Ла Решерш Медикаль) Антагонисты рецептора flt3

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