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MA38398B1 - Composés biaryle amides en tant qu'inhibiteurs de kinase - Google Patents

Composés biaryle amides en tant qu'inhibiteurs de kinase

Info

Publication number
MA38398B1
MA38398B1 MA38398A MA38398A MA38398B1 MA 38398 B1 MA38398 B1 MA 38398B1 MA 38398 A MA38398 A MA 38398A MA 38398 A MA38398 A MA 38398A MA 38398 B1 MA38398 B1 MA 38398B1
Authority
MA
Morocco
Prior art keywords
compounds
kinase inhibitors
amide compounds
biaryl amide
biaryl
Prior art date
Application number
MA38398A
Other languages
English (en)
Other versions
MA38398A1 (fr
Inventor
Yan Lou
Matthew Burger
Gisele Nishiguchi
Alice Rico
Benjamin Taft
Huw Tanner
Robert Aversa
Paul A Barsanti
Michael Patrick Dillon
Alan Dipesa
Cheng Hu
Yue Pan
Valery Polyakov
Savithri Ramurthy
Lina Setti
Aaron Smith
Sharadha Subramanian
Lifeng Wan
Naeem Yusuff
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of MA38398A1 publication Critical patent/MA38398A1/fr
Publication of MA38398B1 publication Critical patent/MA38398B1/fr

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
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    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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Abstract

La présente invention concerne des composés de formule (i) tels que décrits ici, et leurs sels, et des utilisations thérapeutiques de ces composés pour le traitement de troubles associés à l'activité raf kinase. L'invention concerne en outre des compositions pharmaceutiques comprenant ces composés, et des compositions comprenant ces composés et un co-agent thérapeutique.
MA38398A 2013-03-14 2014-03-13 Composés biaryle amides en tant qu'inhibiteurs de kinase MA38398B1 (fr)

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Families Citing this family (114)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105050602B (zh) * 2013-01-12 2018-05-25 张大为 作为pi3激酶抑制剂的吡啶化合物
TWI627174B (zh) 2013-03-14 2018-06-21 比利時商健生藥品公司 P2x7調控劑
US10053463B2 (en) 2013-03-14 2018-08-21 Janssen Pharmaceutica Nv Substituted [1,2,4]triazolo[4,3-a]pyrazines as P2X7 modulators
EP3321266A1 (fr) 2013-03-14 2018-05-16 Janssen Pharmaceutica NV Modulateurs p2x7
PE20151727A1 (es) 2013-03-14 2015-12-17 Boehringer Ingelheim Int Acido 2-aza-biciclo[2.2.1]heptano-3-carboxilico (bencil-ciano-metil)-amidas sustituidas inhibidores de catepsina c
JO3773B1 (ar) 2013-03-14 2021-01-31 Janssen Pharmaceutica Nv معدلات p2x7
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
TWI771630B (zh) * 2013-10-18 2022-07-21 美商賽基昆堤塞爾研發公司 溴結構域(bromodomain)抑制劑
EP3094326A4 (fr) 2014-01-14 2017-07-26 Millennium Pharmaceuticals, Inc. Hétéroaryles et utilisations de ceux-ci
BR112016016289B1 (pt) * 2014-01-14 2023-02-07 Takeda Pharmaceutical Company Limited Heteroaris e usos dos mesmos
JOP20200094A1 (ar) 2014-01-24 2017-06-16 Dana Farber Cancer Inst Inc جزيئات جسم مضاد لـ pd-1 واستخداماتها
JOP20200096A1 (ar) 2014-01-31 2017-06-16 Children’S Medical Center Corp جزيئات جسم مضاد لـ tim-3 واستخداماتها
LT3116909T (lt) 2014-03-14 2020-02-10 Novartis Ag Antikūno molekulės prieš lag-3 ir jų panaudojimas
JP6636014B2 (ja) * 2014-09-12 2020-01-29 ノバルティス アーゲー Rafキナーゼ阻害剤としての化合物および組成物
US10150766B2 (en) 2014-09-12 2018-12-11 Janssen Pharmaceutica Nv P2X7 modulators
EA031376B1 (ru) 2014-09-12 2018-12-28 Бёрингер Ингельхайм Интернациональ Гмбх Спироциклические ингибиторы катепсина с
UY36294A (es) * 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
MA41044A (fr) 2014-10-08 2017-08-15 Novartis Ag Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer
EP4245376A3 (fr) 2014-10-14 2023-12-13 Novartis AG Molécules d'anticorps de pd-l1 et leurs utilisations
EP3233918A1 (fr) 2014-12-19 2017-10-25 Novartis AG Polythérapies
US10449211B2 (en) 2015-03-10 2019-10-22 Aduro Biotech, Inc. Compositions and methods for activating “stimulator of interferon gene”—dependent signalling
WO2017004133A1 (fr) * 2015-06-29 2017-01-05 Nimbus Iris, Inc. Inhibiteurs d'irak et utilisations de ceux-ci
EP4378957A3 (fr) 2015-07-29 2024-08-07 Novartis AG Traitements combinés comprenant des molécules d'anticorps qui se lient à pd-1
EP3878465A1 (fr) 2015-07-29 2021-09-15 Novartis AG Polythérapies comprenant des molécules d'anticorps tim-3
US20180340025A1 (en) 2015-07-29 2018-11-29 Novartis Ag Combination therapies comprising antibody molecules to lag-3
CN105153190B (zh) * 2015-08-21 2017-07-21 江西科技师范大学 含联芳基酰胺结构的杂环并嘧啶类化合物及其制备方法和应用
WO2017070708A1 (fr) 2015-10-23 2017-04-27 Array Biopharma, Inc. Composés de 2-pyridazin-3(2h)-one à substitution 2-aryle et 2-hétéroaryle utilisés en tant qu'inhibiteurs de fgfr tyrosine kinases
AU2016348388B2 (en) 2015-11-03 2023-11-30 Janssen Biotech, Inc. Antibodies specifically binding PD-1 and their uses
WO2017106656A1 (fr) 2015-12-17 2017-06-22 Novartis Ag Molécules d'anticorps anti-pd-1 et leurs utilisations
CN107021963A (zh) * 2016-01-29 2017-08-08 北京诺诚健华医药科技有限公司 吡唑稠环类衍生物、其制备方法及其在治疗癌症、炎症和免疫性疾病上的应用
JP6858984B2 (ja) 2016-02-19 2021-04-14 スプリント バイオサイエンス アクティエボラーグ がんおよび糖尿病の治療に有用な6−ヘテロシクリル−4−モルホリン−4−イルピリジン−2−オン化合物
PT3416945T (pt) * 2016-02-19 2020-09-11 Sprint Bioscience Ab Compostos de 6-aril-4-(morfolin-4-il)-1h-piridina-2-ona úteis para o tratamento do cancro e da diabetes
JP2019518426A (ja) 2016-04-15 2019-07-04 ジェネンテック, インコーポレイテッド がんの診断及び治療方法
BR112018075371A2 (pt) * 2016-06-10 2019-03-19 Novartis Ag usos terapêuticos de um inibidor de c-raf
US11098077B2 (en) 2016-07-05 2021-08-24 Chinook Therapeutics, Inc. Locked nucleic acid cyclic dinucleotide compounds and uses thereof
CN106831812B (zh) * 2016-08-09 2019-09-20 江西科技师范大学 含联芳基酰胺结构的杂环并嘧啶或吡嗪类化合物及其应用
WO2018049214A1 (fr) 2016-09-09 2018-03-15 Incyte Corporation Dérivés de pyrazolopyridine comme modulateurs de hpk1 et leurs utilisations pour le traitement du cancer
CA3036358A1 (fr) 2016-09-09 2018-03-15 Incyte Corporation Derives de pyrazolopyridine comme modulateurs de hpk1 et leurs utilisations pour le traitement du cancer
US10280164B2 (en) 2016-09-09 2019-05-07 Incyte Corporation Pyrazolopyridone compounds and uses thereof
US20180072741A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyrimidine compounds and uses thereof
CN109715163B (zh) * 2016-09-19 2022-11-22 诺华股份有限公司 包含raf抑制剂和erk抑制剂的治疗组合
EP3878850A1 (fr) 2016-12-22 2021-09-15 Boehringer Ingelheim International GmbH Nouvelles quinazolines substituées benzylamino et dérivés en tant qu'inhibiteurs de sos1
WO2018152220A1 (fr) 2017-02-15 2018-08-23 Incyte Corporation Composés de pyrazolopyridine et leurs utilisations
CN106866547B (zh) * 2017-03-15 2020-11-10 江苏省农用激素工程技术研究中心有限公司 2-乙氧基-4,6-二氯嘧啶的合成方法
UY37695A (es) 2017-04-28 2018-11-30 Novartis Ag Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo
TW201902517A (zh) * 2017-04-28 2019-01-16 美商石英醫療公司 Raf降解結合物化合物
IL311471A (en) * 2017-05-02 2024-05-01 Novartis Ag Combined treatment
EP3642240A1 (fr) 2017-06-22 2020-04-29 Novartis AG Molécules d'anticorps dirigées contre cd73 et utilisations correspondantes
JOP20200014A1 (ar) 2017-08-03 2022-10-30 Novartis Ag توليفة علاجية لمثبط كيناز تيروزين egfr من الجيل الثالث ومثبط raf
CN109384782A (zh) * 2017-08-04 2019-02-26 厦门大学 取代五元并六元杂环类化合物、其制备方法、药物组合及其用途
US10722495B2 (en) 2017-09-08 2020-07-28 Incyte Corporation Cyanoindazole compounds and uses thereof
KR20200041387A (ko) 2017-09-08 2020-04-21 에프. 호프만-라 로슈 아게 암의 진단 및 치료 방법
PT3728254T (pt) 2017-12-21 2023-05-02 Boehringer Ingelheim Int Piridopirimidinonas substituídos com benzilamino e derivados como inibidores de sos1
WO2019158579A1 (fr) 2018-02-13 2019-08-22 Vib Vzw Ciblage d'une maladie résiduelle minimale dans le cancer avec des antagonistes de rxr
WO2019164847A1 (fr) 2018-02-20 2019-08-29 Incyte Corporation Composés d'indazole et leurs utilisations
US10745388B2 (en) 2018-02-20 2020-08-18 Incyte Corporation Indazole compounds and uses thereof
PE20210397A1 (es) 2018-02-20 2021-03-02 Incyte Corp Derivados de n-(fenil)-2-(fenil)pirimidina-4-carboxamida y compuestos relacionados como inhibidores hpki para tratar el cancer
US11299473B2 (en) 2018-04-13 2022-04-12 Incyte Corporation Benzimidazole and indole compounds and uses thereof
CA3101117A1 (fr) * 2018-05-22 2019-11-28 Js Innomed Holdings Ltd. Composes heterocycliques utilises en tant qu'inhibiteurs de kinase, compositions comprenant le compose heterocyclique, et leurs procedes d'utilisation
TW202015726A (zh) 2018-05-30 2020-05-01 瑞士商諾華公司 Entpd2抗體、組合療法、及使用該等抗體和組合療法之方法
CN108863884B (zh) * 2018-07-26 2020-07-03 南京富润凯德生物医药有限公司 一种用dast试剂作为消除试剂合成共轭硝基烯取代系列衍生物的方法
US10899755B2 (en) 2018-08-08 2021-01-26 Incyte Corporation Benzothiazole compounds and uses thereof
US11111247B2 (en) 2018-09-25 2021-09-07 Incyte Corporation Pyrazolopyrimidine compounds and uses thereof
CN110950868B (zh) * 2018-09-27 2022-05-13 苏州锐明新药研发有限公司 吡唑并嘧啶化合物及制备方法与制备抗癌症药物的应用
EP3856178A1 (fr) 2018-09-28 2021-08-04 Janssen Pharmaceutica NV Modulateurs de la monoacylglycérol lipase
CA3111309A1 (fr) 2018-09-28 2020-04-02 Janssen Pharmaceutica Nv Modulateurs de la monoacylglycerol lipase
CN113453671A (zh) 2018-12-20 2021-09-28 诺华股份有限公司 用于治疗癌症的Raf抑制剂和CDK4/6抑制剂的组合疗法
US20230081390A1 (en) * 2019-03-22 2023-03-16 Kinnate Biopharma Inc. Inhibitors of raf kinases
WO2020227020A1 (fr) 2019-05-03 2020-11-12 Kinnate Biopharma Inc. Inhibiteurs de kinases raf
WO2020230028A1 (fr) * 2019-05-13 2020-11-19 Novartis Ag Nouvelles formes cristallines de n-(3-(2-(2-hydroxyéthoxy)-6-morpholinopyridin-4-yl)-4-méthylphényl)-2 (trifluorométhyl)isonicotinamide servant d'inhibiteurs de raf pour le traitement du cancer
CN114450276A (zh) 2019-08-06 2022-05-06 因赛特公司 Hpk1抑制剂的固体形式
WO2021027943A1 (fr) * 2019-08-14 2021-02-18 正大天晴药业集团南京顺欣制药有限公司 Dérivé de pyrimidinopyridazinone et son utilisation médicale
US10702525B1 (en) 2019-09-04 2020-07-07 United Arab Emirates University Pyrimidine derivatives as anti-diabetic agents
EP4031578A1 (fr) 2019-09-18 2022-07-27 Novartis AG Anticorps d'entpd2, polythérapies, et procédés d'utilisation des anticorps et des polythérapies
WO2021064569A1 (fr) 2019-09-30 2021-04-08 Janssen Pharmaceutica Nv Ligands mgl pet radiomarqués
BR112022007612A2 (pt) 2019-10-24 2022-09-20 Kinnate Biopharma Inc Inibidores de raf quinases
US20230046018A1 (en) * 2019-12-06 2023-02-16 Medshine Discovery Inc. Biaryl compound as pan-raf kinase inhibitor
WO2021165849A1 (fr) 2020-02-18 2021-08-26 Novartis Ag Combinaisons thérapeutiques comprenant un inhibiteur de raf pour une utilisation dans le traitement du cpnpc mutant braf
JP2023516155A (ja) 2020-02-28 2023-04-18 ノバルティス アーゲー ダブラフェニブ、erk阻害剤及びraf阻害剤又はpd-1阻害剤を含む三重の医薬品の組合せ
AU2021241879A1 (en) 2020-03-26 2022-09-29 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators
EP4149472A1 (fr) 2020-05-12 2023-03-22 Novartis AG Combinaisons thérapeutiques comprenant un inhibiteur de craf
AU2021285032A1 (en) 2020-06-02 2022-12-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
CN113912591B (zh) * 2020-07-08 2023-10-20 齐鲁制药有限公司 联芳基化合物
CN111995623A (zh) * 2020-08-18 2020-11-27 上海毕得医药科技有限公司 一种7-溴-4-氯-1-甲基-1H-咪唑并[4,5-c]吡啶的合成方法
TW202227088A (zh) 2020-08-31 2022-07-16 瑞士商諾華公司 組合療法
WO2022060996A1 (fr) * 2020-09-18 2022-03-24 Kinnate Biopharma Inc. Inhibiteurs de raf kinases
US11377431B2 (en) 2020-10-12 2022-07-05 Kinnate Biopharma Inc. Inhibitors of RAF kinases
WO2022090481A1 (fr) 2020-11-02 2022-05-05 Boehringer Ingelheim International Gmbh 1h-pyrazolo[4,3-c]pyridines substituées et leurs dérivés utilisés comme inhibiteurs d'egfr
US20240051956A1 (en) 2020-12-22 2024-02-15 Qilu Regor Therapeutics Inc. Sos1 inhibitors and uses thereof
CN114591324B (zh) * 2021-03-30 2023-05-05 深圳微芯生物科技股份有限公司 一类吡嗪酮衍生物、其制备及其应用
EP4326256A1 (fr) * 2021-04-23 2024-02-28 Kinnate Biopharma Inc. Traitement du cancer avec un inhibiteur de raf
EP4326255A1 (fr) * 2021-04-23 2024-02-28 Kinnate Biopharma Inc. Formes à l?état solide de (s)-n-(3-(2-(((r)-1-hydroxypropan-2-yl)amino)-6-morpholinopyridin-4-yl)-4-méthylphényl)-3-(2,2,2-trifluoroéthyl)pyrrolidine-1-carboxamide et ses sels
US12065427B2 (en) 2021-04-29 2024-08-20 Boehringer Ingelheim International Gmbh Heterocyclic compounds capable of activating STING
CN117425650A (zh) * 2021-06-04 2024-01-19 齐鲁制药有限公司 一种raf激酶抑制剂的晶型及其制备方法
CN118201922A (zh) * 2021-11-12 2024-06-14 百极优棠(广东)医药科技有限公司 Drak2抑制剂及其制备方法和应用
CA3240980A1 (fr) 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh 2-amino-3-cyano thiophenes anneles et leurs derives pour le traitement du cancer
EP4441053A1 (fr) 2021-12-01 2024-10-09 Boehringer Ingelheim International GmbH 2-amino-3-cyano thiophènes annelés et leurs dérivés pour le traitement du cancer
CN118591540A (zh) 2021-12-01 2024-09-03 勃林格殷格翰国际有限公司 包含环状2-氨基-3-氰基噻吩的kras降解化合物
WO2023099608A1 (fr) 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh 2-amino-3-cyano thiophènes annelés et leurs dérivés pour le traitement du cancer
TW202340208A (zh) 2021-12-01 2023-10-16 德商百靈佳殷格翰國際股份有限公司 用於治療癌症之環狀2-胺基-3-氰基噻吩及衍生物
EP4441050A1 (fr) 2021-12-01 2024-10-09 Boehringer Ingelheim International GmbH 2-amino-3-cyano thiophènes annelés et leurs dérivés pour le traitement du cancer
EP4444429A1 (fr) * 2021-12-09 2024-10-16 Deciphera Pharmaceuticals, LLC Inhibiteurs de raf kinase et leurs méthodes d'utilisation
WO2023118250A1 (fr) 2021-12-23 2023-06-29 Boehringer Ingelheim International Gmbh 8-aza-quinazolines utilisés en tant qu'inhibiteurs de sos1 pénétrant dans le cerveau
US11814384B2 (en) 2022-02-03 2023-11-14 Kinnate Biopharma Inc. Inhibtors of Raf kinases
CN115947691B (zh) * 2022-03-01 2024-08-16 四川大学 哒嗪砜类衍生物及其用途
TW202342766A (zh) 2022-03-02 2023-11-01 瑞士商諾華公司 用於癌症治療之精準療法
TW202404581A (zh) 2022-05-25 2024-02-01 美商醫肯納腫瘤學公司 Mek抑制劑及其用途
WO2024033381A1 (fr) 2022-08-10 2024-02-15 Vib Vzw Inhibition de tcf4/itf2 dans le traitement du cancer
WO2024033703A1 (fr) 2022-08-10 2024-02-15 Novartis Ag Dispersions solides amorphes comprenant du naporafénib
US20240166629A1 (en) 2022-10-26 2024-05-23 Boehringer Ingelheim International Gmbh Heterocyclic compounds capable of activating sting
WO2024089006A1 (fr) 2022-10-26 2024-05-02 Boehringer Ingelheim International Gmbh Composés hétérocycliques capables d'activer sting
WO2024089008A1 (fr) 2022-10-26 2024-05-02 Boehringer Ingelheim International Gmbh Composés hétérocycliques capables d'activer le sting
WO2024166131A1 (fr) 2023-02-09 2024-08-15 Satyarx Pharma Innovations Private Limited Composés hétéroaryle en tant qu'inhibiteurs de pkmyt1
WO2024220470A1 (fr) 2023-04-17 2024-10-24 Ikena Oncology, Inc. Inhibiteurs de tead et leurs utilisations dans le traitement de troubles prolifératifs

Family Cites Families (110)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3707475A (en) 1970-11-16 1972-12-26 Pfizer Antiinflammatory imidazoles
DE3029376A1 (de) 1980-07-31 1982-03-18 Nepera Chemical Co. Inc., Harriman, N.Y. Verfahren zur herstellung von 2,4,5-tris-pyridylimidazolen
EP0149884B1 (fr) 1983-09-09 1992-12-16 Takeda Chemical Industries, Ltd. Dérivés de 5-pyridyle-1,3-thiazole, leur préparation et utilisation
JP2722586B2 (ja) 1989-01-13 1998-03-04 大正製薬株式会社 インドリルイミダゾール誘導体
JP2808460B2 (ja) 1989-11-16 1998-10-08 大正製薬株式会社 イミダゾール誘導体
US6358932B1 (en) 1994-05-31 2002-03-19 Isis Pharmaceticals, Inc. Antisense oligonucleotide inhibition of raf gene expression
US5717100A (en) 1995-10-06 1998-02-10 Merck & Co., Inc. Substituted imidazoles having anti-cancer and cytokine inhibitory activity
GB2306108A (en) 1995-10-13 1997-04-30 Merck & Co Inc Treatment of Raf-mediated cancers with imidazole derivatives
JP2001500482A (ja) 1996-08-27 2001-01-16 ノバルティス アクチェンゲゼルシャフト 除草性s置換1,2,4,6―チアトリアジン類
AU743024B2 (en) 1997-03-05 2002-01-17 Sugen, Inc. Formulations for hydrophobic pharmaceutical agents
AR012634A1 (es) 1997-05-02 2000-11-08 Sugen Inc Compuesto basado en quinazolina, composicion famaceutica que lo comprende, metodo para sintetizarlo, su uso, metodos de modulacion de la funcion deserina/treonina proteinaquinasa con dicho compuesto y metodo in vitro para identificar compuestos que modulan dicha funcion
GB9711650D0 (en) 1997-06-05 1997-07-30 Pfizer Ltd Compounds useful in therapy
GB9716557D0 (en) 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
US6022884A (en) 1997-11-07 2000-02-08 Amgen Inc. Substituted pyridine compounds and methods of use
US6211177B1 (en) 1998-11-24 2001-04-03 Cell Pathways, Inc. Method for treating neoplasia by exposure to substituted 2-aryl-benzimidazole derivatives
EP1140840B1 (fr) 1999-01-13 2006-03-22 Bayer Pharmaceuticals Corp. Diphenylurees a substituants -g(v)-carboxyaryles, inhibitrices de kinase raf
US6548529B1 (en) 1999-04-05 2003-04-15 Bristol-Myers Squibb Company Heterocyclic containing biphenyl aP2 inhibitors and method
JP2002541253A (ja) 1999-04-09 2002-12-03 スミスクライン・ビーチャム・コーポレイション トリアリールイミダゾール
BR0009721A (pt) 1999-04-15 2002-02-13 Bristol Myers Squibb Co Inibidores de tirosina quinase de proteìna cìclica
JP2000302680A (ja) 1999-04-23 2000-10-31 Takeda Chem Ind Ltd 脳保護剤
WO2001021598A1 (fr) 1999-09-23 2001-03-29 Astrazeneca Ab Composes therapeutiques de quinazoline
NZ518032A (en) 1999-11-22 2004-02-27 Smithkline Beecham Plc Substituted imidazole derivatives
EP1251849A1 (fr) 2000-01-18 2002-10-30 Vertex Pharmaceuticals Incorporated Inhibiteurs de la gyrase et utilisations de ces derniers
JP2003520233A (ja) 2000-01-18 2003-07-02 バーテックス ファーマシューティカルズ インコーポレイテッド ジャイレースインヒビターおよびそれらの使用
CO5271680A1 (es) 2000-02-21 2003-04-30 Smithkline Beecham Corp Compuestos
EP1263753B1 (fr) 2000-03-06 2004-05-06 SmithKline Beecham plc Derives imidazole utilises comme inhibiteurs de la raf kinase
GB0005357D0 (en) 2000-03-06 2000-04-26 Smithkline Beecham Plc Compounds
GB0007405D0 (en) 2000-03-27 2000-05-17 Smithkline Beecham Corp Compounds
AU2001244618A1 (en) 2000-03-30 2001-10-15 Takeda Chemical Industries Ltd. Substituted 1,3-thiazole compounds, their production and use
US6608053B2 (en) * 2000-04-27 2003-08-19 Yamanouchi Pharmaceutical Co., Ltd. Fused heteroaryl derivatives
US6949571B2 (en) 2000-06-12 2005-09-27 Eisai Co., Ltd. 1,2-dihydropyridine compounds, process for preparation of the same and use thereof
HUP0400651A2 (hu) 2000-11-07 2004-06-28 Bristol-Myers Squibb Company Szerin proteáz inhibitorokként alkalmazható savszármazékok és ezeket tartalmazó gyógyszerkészítmények
US20040053943A1 (en) 2000-11-20 2004-03-18 Adams Jerry L. Novel compounds
US7238813B2 (en) 2000-11-29 2007-07-03 Smithkline Beecham Corporation Chemical compounds
WO2002064136A2 (fr) 2001-01-26 2002-08-22 Chugai Seiyaku Kabushiki Kaisha Inhibiteurs de malonyl-coa decarboxylase utiles en tant que modulateurs metaboliques
US7199124B2 (en) 2001-02-02 2007-04-03 Takeda Pharmaceutical Company Limited JNK inhibitor
US20030009034A1 (en) 2001-03-22 2003-01-09 Neil Wishart Transition metal mediated process
JP2002338537A (ja) 2001-05-16 2002-11-27 Mitsubishi Pharma Corp アミド化合物およびその医薬用途
GB0112348D0 (en) 2001-05-19 2001-07-11 Smithkline Beecham Plc Compounds
GB0129260D0 (en) 2001-12-06 2002-01-23 Eisai London Res Lab Ltd Pharmaceutical compositions and their uses
US8299108B2 (en) 2002-03-29 2012-10-30 Novartis Ag Substituted benzazoles and methods of their use as inhibitors of raf kinase
AU2003226211B2 (en) 2002-03-29 2008-05-29 Novartis Vaccines And Diagnostics, Inc. Substituted benzazoles and use thereof as RAF kinase inhibitors
AR039241A1 (es) 2002-04-04 2005-02-16 Biogen Inc Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos
CA2498047C (fr) 2002-09-18 2009-05-19 Pfizer Products Inc. Composes d'imidazole utilises en tant qu'inhibiteurs du facteur de croissance transformant (tgf)
OA12926A (en) 2002-09-18 2006-10-13 Pfizer Prod Inc Novel oxazole and thiazole compounds as transforming growth factor (TGF) inhibitors.
EP1631260A2 (fr) 2003-02-28 2006-03-08 Transform Pharmaceuticals, Inc. Compositions pharmaceutiques a base d'un co-cristal
US7531553B2 (en) 2003-03-21 2009-05-12 Amgen Inc. Heterocyclic compounds and methods of use
AR045944A1 (es) 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
JP4758349B2 (ja) 2003-10-08 2011-08-24 アイアールエム・リミテッド・ライアビリティ・カンパニー タンパク質キナーゼ阻害剤としての化合物および組成物
CN1889951A (zh) 2003-10-16 2007-01-03 希龙公司 取代的苯并唑及其用作raf激酶抑制剂的应用
WO2005047266A1 (fr) 2003-11-14 2005-05-26 Lorus Therapeutics Inc. Imidazoles d'aryle et leur utilisation comme agents anticancereux
BRPI0508397A (pt) 2004-03-05 2007-08-07 Taisho Pharmaceutical Co Ltd derivado de tiazol ou um sal farmaceuticamente aceitável do mesmo, inibidor de alk5, estimulador de proliferação de folìculo capilar, e, estimulador do crescimento capilar ou um agente de crescimento capilar
KR100749566B1 (ko) 2004-04-21 2007-08-16 이화여자대학교 산학협력단 Alk5 및/또는 alk4 억제제로 유효한 2-피리딜이치환된 이미다졸 유도체
WO2005105814A1 (fr) 2004-04-28 2005-11-10 Incyte Corporation Inhibiteurs tetracycliques de janus kinases
PE20060315A1 (es) 2004-05-24 2006-05-15 Irm Llc Compuestos de tiazol como moduladores de ppar
CN101001845A (zh) * 2004-06-15 2007-07-18 阿斯利康(瑞典)有限公司 作为抗癌药物的取代喹唑酮
US7453002B2 (en) 2004-06-15 2008-11-18 Bristol-Myers Squibb Company Five-membered heterocycles useful as serine protease inhibitors
GB0415364D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
GB0415367D0 (en) * 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
GB0415365D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
WO2006026306A1 (fr) 2004-08-31 2006-03-09 Biogen Idec Ma Inc. Pyrimidinylimidazoles utilises comme inhibiteurs de tgf-beta
WO2006038734A1 (fr) 2004-10-08 2006-04-13 Astellas Pharma Inc. Dérivés de la pyridazinone inhibiteurs de cytokines
WO2006044509A2 (fr) 2004-10-15 2006-04-27 Biogen Idec Ma Inc. Procede pour traiter des lesions vasculaires
GB0524814D0 (en) * 2005-12-05 2006-01-11 Glaxo Group Ltd Compounds
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
JP2007246520A (ja) 2006-02-15 2007-09-27 Takeda Yuichiro Rage阻害剤
CA2643968A1 (fr) * 2006-03-17 2007-09-27 Wyeth Derives de pyrazolo[1,5-a]pyrimidine et procedes d'utilisation de ceux-ci
EP2007393B1 (fr) 2006-04-07 2013-08-21 Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College Thiazole et thiophene analogues et leur utilisation pour traiter des maladies auto-immunes et des cancers
BRPI0714908B8 (pt) 2006-08-08 2021-05-25 Chugai Pharmaceutical Co Ltd derivados de pirimidina como inibidor de pi3k, composição farmacêutica e agente preventivo ou agente terapêutico de uma doença proliferativa que os compreende
WO2008071605A2 (fr) 2006-12-15 2008-06-19 F. Hoffmann-La Roche Ag Méthodes de traitement de maladies inflammatoires
JP5140154B2 (ja) 2007-06-27 2013-02-06 アストラゼネカ・アクチエボラーグ ピラジノン誘導体および肺疾患の処置におけるそれらの使用
JP2010532381A (ja) 2007-06-29 2010-10-07 サネシス ファーマシューティカルズ, インコーポレイテッド Rafキナーゼ阻害剤として有用な複素環式化合物
CL2008001933A1 (es) 2007-06-29 2009-09-25 Millennium Pharm Inc Compuestos derivados de pirimidina, inhibidores de la raf quinasa; compuestos intermediarios; procedimiento de preparacion; composicion farmaceutica; y su uso para tratar trastornos proliferativos, cardiacos, neurodegenerativos, inflamatorios, oseos, inmunologicos enfermedad viral, entre otros.
WO2009003998A2 (fr) 2007-07-02 2009-01-08 Boehringer Ingelheim International Gmbh Nouveaux composés chimiques
WO2009007749A2 (fr) 2007-07-09 2009-01-15 Astrazeneca Ab Composés 947
CA2695004C (fr) 2007-07-17 2016-01-19 Plexxikon, Inc. Composes et procedes pour la modulation des kinases et leurs indications
WO2009014637A2 (fr) 2007-07-19 2009-01-29 Schering Corporation Composés hétérocycliques d'amide en tant qu'inhibiteurs de protéine kinase
US20110190280A1 (en) 2007-08-29 2011-08-04 George Adjabeng Thiazole And Oxazole Kinase Inhibitors
TW200916458A (en) 2007-09-05 2009-04-16 Astrazeneca Ab Heterocyclic compounds and methods of use thereof
WO2009047163A1 (fr) 2007-10-10 2009-04-16 F. Hoffmann-La Roche Ag Procédés de traitement de maladies inflammatoires
TW200940537A (en) 2008-02-26 2009-10-01 Astrazeneca Ab Heterocyclic urea derivatives and methods of use thereof
US8865732B2 (en) 2008-03-21 2014-10-21 Novartis Ag Heterocyclic compounds and uses thereof
WO2009115572A2 (fr) 2008-03-21 2009-09-24 Novartis Ag Nouveaux composés hétérocycliques et leurs utilisations
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
BRPI0915205A2 (pt) 2008-06-11 2017-03-21 Dana Farber Cancer Inst Inc compostos e composições úteis para o tratamento de malária
EP2300466B1 (fr) * 2008-06-20 2014-08-06 Bristol-Myers Squibb Company Composés d'imidazopyridine et d'imidazopyrazine utilisés comme inhibiteurs de kinase
WO2010010154A1 (fr) 2008-07-24 2010-01-28 Nerviano Medical Sciences S.R.L. 3,4-diarylpyrazoles utilisés comme inhibiteurs de protéine kinase
WO2010048149A2 (fr) 2008-10-20 2010-04-29 Kalypsys, Inc. Modulateurs hétérocycliques de gpr119 pour le traitement d'une maladie
HUE036068T2 (hu) 2008-12-19 2018-06-28 Vertex Pharma ATR kináz gátlószereiként alkalmazható pirazinszármazékok
US8242260B2 (en) 2009-08-28 2012-08-14 Novartis Ag Compounds and compositions as protein kinase inhibitors
US20110130380A1 (en) 2009-09-04 2011-06-02 Barsanti Paul A Heteroaryl Kinase Inhibitors
WO2011059610A1 (fr) 2009-11-10 2011-05-19 Glaxosmithkline Llc Composés de benzènesulfonamide-thiazole et oxazole
US9315491B2 (en) 2009-12-28 2016-04-19 Development Center For Biotechnology Pyrimidine compounds as mTOR and PI3K inhibitors
EP2520575B1 (fr) 2009-12-28 2016-11-30 General Incorporated Association Pharma Valley Project Supporting Organisation Composé 1,3,4-oxadiazole-2-carboxamide
KR20110123657A (ko) 2010-05-07 2011-11-15 에스케이케미칼주식회사 피콜린아마이드 및 피리미딘-4-카복사미드 화합물, 이의 제조방법 및 이를 함유하는 약제학적 조성물
US20130096149A1 (en) 2010-06-25 2013-04-18 Novartis Ag Heteroaryl compounds and compositions as protein kinase inhibitors
CN101993415B (zh) 2010-09-15 2013-08-14 北京韩美药品有限公司 作为Hedgehog通路抑制剂的化合物以及包含该化合物的药物组合物及其应用
WO2012109075A1 (fr) 2011-02-07 2012-08-16 Plexxikon Inc. Composés et procédés de modulation de kinase, et leurs indications
EP2686317A4 (fr) * 2011-03-17 2014-08-20 Selexagen Therapeutics Inc Inhibiteurs des kinases raf
EP2739143B1 (fr) 2011-08-05 2018-07-11 Gary A. Flynn Préparation et procédés d'utilisation d'ortho-aryle hétéroaryle à 5 chaînons -carboxamide contenant des inhibiteurs de kinases multicibles
US8569283B2 (en) 2011-09-01 2013-10-29 Valentina Molteni Compounds and compositions as c-Kit kinase inhibitors
RU2616619C2 (ru) 2011-09-21 2017-04-18 Селлзоум Лимитед Морфолино-замещенные производные мочевины или карбамата в качестве ингибиторов mtor
EP2844655A1 (fr) 2012-05-02 2015-03-11 Lupin Limited Composés substitués de pyridine en tant que modulateurs de crac
MX2014013373A (es) 2012-05-15 2015-08-14 Novartis Ag Derivados de benzamida para inhibir la actividad de abl1, abl2 y bcr-abl1.
WO2014008214A1 (fr) 2012-07-02 2014-01-09 Biogen Idec Ma Inc. Composés contenant biaryle comme agonistes inverses de récepteurs ror-gamma
EP2903613B1 (fr) 2012-10-08 2017-11-22 Merck Sharp & Dohme Corp. Composés pyrazoliques utiles en tant qu'inhibiteurs d'activité d'irak4
US9242969B2 (en) * 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
JP6636014B2 (ja) 2014-09-12 2020-01-29 ノバルティス アーゲー Rafキナーゼ阻害剤としての化合物および組成物
CN107001329B (zh) 2014-09-12 2020-09-01 诺华股份有限公司 作为激酶抑制剂的化合物和组合物
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa

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