SMT201700052B - 2-(azaindol-2-il)benzimidazoli come inibitori di pad4 - Google Patents
2-(azaindol-2-il)benzimidazoli come inibitori di pad4Info
- Publication number
- SMT201700052B SMT201700052B SM201700052T SM201700052T SMT201700052B SM T201700052 B SMT201700052 B SM T201700052B SM 201700052 T SM201700052 T SM 201700052T SM 201700052 T SM201700052 T SM 201700052T SM T201700052 B SMT201700052 B SM T201700052B
- Authority
- SM
- San Marino
- Prior art keywords
- benzimidazols
- azaindol
- pad4 inhibitors
- pad4
- inhibitors
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/EP2012/064649 WO2014015905A1 (en) | 2012-07-26 | 2012-07-26 | 2 - (azaindol- 2 -yl) benz imidazoles as pad4 inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SMT201700052B true SMT201700052B (it) | 2017-03-08 |
Family
ID=49996626
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SM201700052T SMT201700052B (it) | 2012-07-26 | 2017-01-24 | 2-(azaindol-2-il)benzimidazoli come inibitori di pad4 |
Country Status (22)
| Country | Link |
|---|---|
| US (4) | US9127003B2 (it) |
| EP (1) | EP2877467B1 (it) |
| JP (1) | JP6063567B2 (it) |
| KR (1) | KR101916443B1 (it) |
| CN (1) | CN104470919B (it) |
| AU (1) | AU2012386257B2 (it) |
| BR (1) | BR112015001545B1 (it) |
| CA (1) | CA2879341C (it) |
| CY (1) | CY1118524T1 (it) |
| DK (1) | DK2877467T3 (it) |
| ES (1) | ES2609126T3 (it) |
| HR (1) | HRP20161530T1 (it) |
| HU (1) | HUE033294T2 (it) |
| IN (1) | IN2014KN02935A (it) |
| LT (1) | LT2877467T (it) |
| PL (1) | PL2877467T3 (it) |
| PT (1) | PT2877467T (it) |
| RS (1) | RS55684B1 (it) |
| RU (1) | RU2611010C2 (it) |
| SI (1) | SI2877467T1 (it) |
| SM (1) | SMT201700052B (it) |
| WO (1) | WO2014015905A1 (it) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2016264958B2 (en) * | 2015-05-21 | 2020-10-29 | Glaxosmithkline Intellectual Property Development Limited | Benzoimidazole derivatives as PAD4 inhibitors |
| AR107030A1 (es) * | 2015-12-09 | 2018-03-14 | Padlock Therapeutics Inc | Inhibidores aza-bencimidazol de pad4 |
| AR107032A1 (es) * | 2015-12-09 | 2018-03-14 | Padlock Therapeutics Inc | Inhibidores bicíclicos de pad4 |
| CA3015482A1 (en) * | 2016-02-23 | 2017-08-31 | Padlock Therapeutics, Inc. | Heteroaryl inhibitors of pad4 |
| CN107188867A (zh) * | 2016-03-14 | 2017-09-22 | 中国科学院天津工业生物技术研究所 | 精氨酸脱亚氨酶4的抑制剂 |
| EP3490989B1 (en) | 2016-07-27 | 2020-09-09 | Padlock Therapeutics, Inc. | Covalent inhibitors of pad4 |
| MA46193A (fr) * | 2016-09-12 | 2019-07-17 | Padlock Therapeutics Inc | Inhibiteurs hétéroaryles de pad4 |
| US11208386B2 (en) | 2016-12-02 | 2021-12-28 | University Of Massachusetts | Inhibitors of protein arginine deiminases (PADs) and methods of preparation and use thereof |
| CN108689946B (zh) * | 2017-04-12 | 2022-10-18 | 中国科学院上海药物研究所 | 2-取代硫基乙酰胺类化合物及其制备方法和应用 |
| BR112020005489A2 (pt) * | 2017-09-22 | 2020-09-24 | Jubilant Epipad Llc, | composto da fórmula (i), composto de fórmula (ii), composto de fórmula (iii), processo de preparação de compostos de fórmula (i), processo de preparação de compostos de fórmula (ii), processo de preparação de compostos de fórmula (iii), composição farmacêutica, método para inibir uma ou mais famílias pad em uma célula, método para tratar uma afeção mediada por um ou mais pads, utilização do composto, método para o tratamento e/ou prevenção de uma afeção mediada por um ou mais distúrbios da família pad, método para o tratamento de artrite reumatoide e método de tratamento de câncer |
| BR112020007607A2 (pt) * | 2017-10-18 | 2020-09-29 | Jubilant Epipad LLC | compostos das fórmulas (i), (ii) e (iii); processos de preparação de compostos das fórmulas (i), (ii) e (iii); composição farmacêutica; compostos; método para a inibição de uma ou mais famílias de pad em uma célula; método de tratamento de uma afecção mediada por uma ou mais pad; composto da fórmula (i), fórmula (ii) e fórmula (iii); uso do composto; método para o tratamento e/ou prevenção de uma afecção; método para o tratamento de artrite reumatoide; e método de tratamento de câncer |
| AU2018362046B2 (en) | 2017-11-06 | 2023-04-13 | Jubilant Prodel LLC | Pyrimidine derivatives as inhibitors of PD1/PD-L1 activation |
| ES2979256T3 (es) | 2017-11-24 | 2024-09-25 | Jubilant Episcribe Llc | Compuestos heterocíclicos como inhibidores de prmt5 |
| EP3760628A4 (en) * | 2018-02-26 | 2021-10-13 | Nanjing Transthera Biosciences Co., Ltd. | PEPTIDYLARGININE DEIMINASE INHIBITOR AND ITS USES |
| SG11202008950PA (en) | 2018-03-13 | 2020-10-29 | Jubilant Prodel LLC | Bicyclic compounds as inhibitors of pd1/pd-l1 interaction/activation |
| JP7447080B2 (ja) | 2018-08-08 | 2024-03-11 | ブリストル－マイヤーズ スクイブ カンパニー | Ｐａｄ４阻害剤としての置換チエノピロール |
| US11524959B1 (en) * | 2018-08-08 | 2022-12-13 | Bristol-Myers Squibb Company | Indole and azaindole inhibitors of pad enzymes |
| BR112021002089A2 (pt) * | 2018-08-08 | 2021-05-04 | Bristol-Myers Squibb Company | benzimidazóis substituídos como inibidores de pad4 |
| ES2956090T3 (es) * | 2018-08-08 | 2023-12-13 | Bristol Myers Squibb Co | Inhibidores de bencimidazol de enzimas PAD |
| CN109369513B (zh) * | 2018-11-20 | 2020-08-25 | 都创(上海)医药科技有限公司 | 一种fbdd常用分子片段的制备方法 |
| CA3123215C (en) | 2018-12-19 | 2024-04-02 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 in combination with neuroprotective agents |
| US20230002328A1 (en) * | 2019-07-03 | 2023-01-05 | University Of Massachusetts | Inhibitors of protein arginine deiminase 1 and methods of preparation and use thereof |
| CN112574230B (zh) * | 2019-09-27 | 2022-10-28 | 药捷安康(南京)科技股份有限公司 | 肽酰精氨酸脱亚胺酶抑制剂及其用途 |
| JP2023512557A (ja) * | 2020-02-06 | 2023-03-27 | ブリストル－マイヤーズ スクイブ カンパニー | 免疫抑制剤として有用な大環状ｐａｄ４阻害剤 |
| TW202140477A (zh) * | 2020-02-12 | 2021-11-01 | 美商必治妥美雅史谷比公司 | 雜環ｐａｄ４抑制劑 |
| CN111265526B (zh) * | 2020-04-09 | 2021-03-19 | 黑龙江中医药大学 | 一种治疗胃癌的药物及其制备方法 |
| EP4143189A1 (en) | 2020-04-30 | 2023-03-08 | Gilead Sciences, Inc. | Macrocyclic inhibitors of peptidylarginine deiminases |
| KR20230093251A (ko) | 2020-09-10 | 2023-06-27 | 프리시릭스 엔.브이. | Fap에 대한 항체 단편 |
| CN116209441A (zh) | 2020-09-18 | 2023-06-02 | 住友制药株式会社 | 新型胺衍生物 |
| EP4267562A1 (en) | 2020-12-22 | 2023-11-01 | Gilead Sciences, Inc. | Inhibitors of peptidylarginine deiminases |
| TW202329941A (zh) | 2021-11-15 | 2023-08-01 | 大陸商上海齊魯銳格醫藥研發有限公司 | Ｐａｄ４抑制劑及其用途 |
| WO2023203135A1 (en) | 2022-04-22 | 2023-10-26 | Precirix N.V. | Improved radiolabelled antibody |
| WO2023213801A1 (en) | 2022-05-02 | 2023-11-09 | Precirix N.V. | Pre-targeting |
| WO2023230609A1 (en) * | 2022-05-26 | 2023-11-30 | Celgene Corporation | Heterocyclic pad4 inhibitors |
| WO2024109945A1 (en) * | 2022-11-24 | 2024-05-30 | Helios Huaming Biopharma Co., Ltd. | Selenium containing heterocycle compounds and use thereof |
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| AU570439B2 (en) | 1983-03-28 | 1988-03-17 | Compression Labs, Inc. | A combined intraframe and interframe transform coding system |
| CN1217654C (zh) | 1995-04-14 | 2005-09-07 | 史密丝克莱恩比彻姆公司 | 舒喘宁的计定剂量吸入器 |
| TW533865U (en) | 1997-06-10 | 2003-05-21 | Glaxo Group Ltd | Dispenser for dispensing medicament and actuation indicating device |
| JP2002527359A (ja) * | 1998-09-18 | 2002-08-27 | ビーエーエスエフ アクチェンゲゼルシャフト | キナーゼインヒビターとしての４−アミノピロリピリミジン |
| US6315112B1 (en) | 1998-12-18 | 2001-11-13 | Smithkline Beecham Corporation | Method and package for storing a pressurized container containing a drug |
| US6352152B1 (en) | 1998-12-18 | 2002-03-05 | Smithkline Beecham Corporation | Method and package for storing a pressurized container containing a drug |
| US6390291B1 (en) | 1998-12-18 | 2002-05-21 | Smithkline Beecham Corporation | Method and package for storing a pressurized container containing a drug |
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| EP1226119B1 (en) | 1999-10-19 | 2005-03-16 | MERCK & CO. INC. | Tyrosine kinase inhibitors |
| MXPA02006338A (es) | 1999-12-24 | 2002-12-13 | Aventis Pharma Ltd | Azaindoles. |
| GB0115393D0 (en) | 2001-06-23 | 2001-08-15 | Aventis Pharma Ltd | Chemical compounds |
| WO2003000690A1 (en) | 2001-06-25 | 2003-01-03 | Aventis Pharmaceuticals Inc. | Synthesis of heterocyclic compounds employing microwave technology |
| CN102028994B (zh) | 2003-11-03 | 2013-04-24 | 葛兰素集团有限公司 | 流体分配装置 |
| WO2005047289A1 (en) | 2003-11-17 | 2005-05-26 | Pfizer Products Inc. | Pyrrolopyrimidine compounds useful in treatment of cancer |
| FR2862971B1 (fr) * | 2003-11-28 | 2006-03-24 | Sod Conseils Rech Applic | Nouveaux derives de benzimidazole et d'imidazo-pyridine et leur utilisation en tant que medicament |
| US7429611B2 (en) | 2004-09-23 | 2008-09-30 | Bristol-Myers Squibb Company | Indole inhibitors of 15-lipoxygenase |
| US20100197657A1 (en) | 2007-09-25 | 2010-08-05 | Chang Ronald K | 2-aryl or heteroaryl indole derivatives |
| US20090311217A1 (en) | 2008-05-28 | 2009-12-17 | Wyeth | 3-substituted-1h-indole compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses |
| RU2011106786A (ru) * | 2008-07-23 | 2012-08-27 | Вертекс Фармасьютикалз Инкорпорейтед (Us) | Ингибиторы пиразолопиридинкиназы |
| SG10201401169QA (en) * | 2009-04-02 | 2014-05-29 | Merck Serono Sa | Dihydroorotate dehydrogenase inhibitors |
| US20100305093A1 (en) | 2009-04-09 | 2010-12-02 | Exelixis, Inc. | Inhibitors of mTOR and Methods of Making and Using |
-
2012
- 2012-07-26 LT LTEP12740581.9T patent/LT2877467T/lt unknown
- 2012-07-26 US US14/416,937 patent/US9127003B2/en active Active
- 2012-07-26 KR KR1020157005099A patent/KR101916443B1/ko active IP Right Grant
- 2012-07-26 RU RU2014152456A patent/RU2611010C2/ru active
- 2012-07-26 CA CA2879341A patent/CA2879341C/en active Active
- 2012-07-26 PT PT127405819T patent/PT2877467T/pt unknown
- 2012-07-26 HU HUE12740581A patent/HUE033294T2/en unknown
- 2012-07-26 WO PCT/EP2012/064649 patent/WO2014015905A1/en active Application Filing
- 2012-07-26 ES ES12740581.9T patent/ES2609126T3/es active Active
- 2012-07-26 BR BR112015001545-0A patent/BR112015001545B1/pt active IP Right Grant
- 2012-07-26 DK DK12740581.9T patent/DK2877467T3/en active
- 2012-07-26 PL PL12740581T patent/PL2877467T3/pl unknown
- 2012-07-26 AU AU2012386257A patent/AU2012386257B2/en active Active
- 2012-07-26 CN CN201280074868.5A patent/CN104470919B/zh active Active
- 2012-07-26 IN IN2935KON2014 patent/IN2014KN02935A/en unknown
- 2012-07-26 JP JP2015523426A patent/JP6063567B2/ja active Active
- 2012-07-26 EP EP12740581.9A patent/EP2877467B1/en active Active
- 2012-07-26 RS RS20170121A patent/RS55684B1/sr unknown
- 2012-07-26 SI SI201230769A patent/SI2877467T1/sl unknown
-
2015
- 2015-08-03 US US14/816,246 patent/US9518054B2/en active Active
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2016
- 2016-11-15 US US15/352,340 patent/US9833449B2/en active Active
- 2016-11-21 HR HRP20161530TT patent/HRP20161530T1/hr unknown
-
2017
- 2017-01-24 SM SM201700052T patent/SMT201700052B/it unknown
- 2017-01-27 CY CY20171100128T patent/CY1118524T1/el unknown
- 2017-11-20 US US15/817,562 patent/US10039755B2/en active Active
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| FR2997080B1 (fr) | Inhibiteurs de neprilysine |