IN2014KN02935A - - Google Patents
Info
- Publication number
- IN2014KN02935A IN2014KN02935A IN2935KON2014A IN2014KN02935A IN 2014KN02935 A IN2014KN02935 A IN 2014KN02935A IN 2935KON2014 A IN2935KON2014 A IN 2935KON2014A IN 2014KN02935 A IN2014KN02935 A IN 2014KN02935A
- Authority
- IN
- India
- Prior art keywords
- 6alkyl
- hydrogen
- 6alkoxy
- proviso
- hydroxy
- Prior art date
Links
Classifications
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- 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
- A61K31/40—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
-
- 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
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- 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
-
- 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)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Compounds of formula (I) wherein; R1 is hydrogen or C1-6alkyl; R2 is hydrogen, C1-6alkyl, perhalomethylC0-5alkyl-O-, or C1-6alkoxy; R3 is hydrogen, C1-6alkyl, or C1-6alkoxyC1-6alkyl; R4 is hydrogen, C1-6alkyl, perhalomethylC1-6alkyl; or unsubstituted C3-6cycloalkylC1-6alkyl; A is C-R5 or N; B is C-R6 or N; D is C-R7 or N; with the proviso that at least one of A, B, and D, is N; R5 is hydrogen or C1-6alkyl; R6 is hydrogen or C1-6alkyl; R7 is hydrogen, C1-6alkyl, C1-6alkoxy, or hydroxy; R8 is hydrogen or C1-6alkyl, with the proviso that one of R4 and R8 is hydrogen; R9 is hydrogen or hydroxy; R10 is hydrogen or C1-6alkyl; and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.
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 |
|---|---|
| IN2014KN02935A true IN2014KN02935A (en) | 2015-05-08 |
Family
ID=49996626
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IN2935KON2014 IN2014KN02935A (en) | 2012-07-26 | 2012-07-26 |
Country Status (22)
| Country | Link |
|---|---|
| US (4) | US9127003B2 (en) |
| EP (1) | EP2877467B1 (en) |
| JP (1) | JP6063567B2 (en) |
| KR (1) | KR101916443B1 (en) |
| CN (1) | CN104470919B (en) |
| AU (1) | AU2012386257B2 (en) |
| BR (1) | BR112015001545B1 (en) |
| CA (1) | CA2879341C (en) |
| CY (1) | CY1118524T1 (en) |
| DK (1) | DK2877467T3 (en) |
| ES (1) | ES2609126T3 (en) |
| HR (1) | HRP20161530T1 (en) |
| HU (1) | HUE033294T2 (en) |
| IN (1) | IN2014KN02935A (en) |
| LT (1) | LT2877467T (en) |
| PL (1) | PL2877467T3 (en) |
| PT (1) | PT2877467T (en) |
| RS (1) | RS55684B1 (en) |
| RU (1) | RU2611010C2 (en) |
| SI (1) | SI2877467T1 (en) |
| SM (1) | SMT201700052B (en) |
| WO (1) | WO2014015905A1 (en) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3298003B1 (en) * | 2015-05-21 | 2023-04-19 | GlaxoSmithKline Intellectual Property Development Limited | Benzoimidazole derivatives as pad4 inhibitors |
| AR107030A1 (en) * | 2015-12-09 | 2018-03-14 | Padlock Therapeutics Inc | AZA-BENCIMIDAZOL INHIBITORS OF PAD4 |
| AR107032A1 (en) * | 2015-12-09 | 2018-03-14 | Padlock Therapeutics Inc | PAD4 BICYCLIC INHIBITORS |
| SG11201807021UA (en) | 2016-02-23 | 2018-09-27 | Padlock Therapeutics Inc | Heteroaryl inhibitors of pad4 |
| CN107188867A (en) * | 2016-03-14 | 2017-09-22 | 中国科学院天津工业生物技术研究所 | The inhibitor of arginine deiminase 4 |
| WO2018022897A1 (en) * | 2016-07-27 | 2018-02-01 | Padlock Therapeutics, Inc. | Covalent inhibitors of pad4 |
| EP3510025B1 (en) * | 2016-09-12 | 2022-06-29 | Padlock Therapeutics, Inc. | Heteroaryl inhibitors of 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 (en) * | 2017-04-12 | 2022-10-18 | 中国科学院上海药物研究所 | 2-substituted sulfenyl acetamide compound and preparation method and application thereof |
| BR112020005489A2 (en) * | 2017-09-22 | 2020-09-24 | Jubilant Epipad Llc, | compound of formula (i), compound of formula (ii), compound of formula (iii), process of preparing compounds of formula (i), process of preparing compounds of formula (ii), process of preparing compounds of formula (iii), pharmaceutical composition, method for inhibiting one or more pad families in a cell, method for treating a condition mediated by one or more pads, use of the compound, method for treating and / or preventing a condition mediated by one or more more disorders of the pad family, method for treating rheumatoid arthritis and cancer treatment method |
| PT3697785T (en) * | 2017-10-18 | 2023-04-03 | Jubilant Epipad LLC | Imidazo-pyridine compounds as pad inhibitors |
| BR112020008851A2 (en) | 2017-11-06 | 2020-10-20 | Jubilant Prodel LLC | compound of formula i, process for preparing compounds of formula i, pharmaceutical composition, method for treating and / or preventing various diseases, use, method for treating cancer, method of treating cancer and method for treating and / or prevention of cancer and infectious diseases |
| JP7368369B2 (en) | 2017-11-24 | 2023-10-24 | ジュビラント・エピスクライブ・エルエルシー | Heterocyclic compounds as PRMT5 inhibitors |
| WO2019161803A1 (en) * | 2018-02-26 | 2019-08-29 | 南京药捷安康生物科技有限公司 | Peptidylarginine deiminase inhibitor and use thereof |
| WO2019175897A1 (en) | 2018-03-13 | 2019-09-19 | Jubilant Biosys Limited | Bicyclic compounds as inhibitors of pd1/pd-l1 interaction/activation |
| KR20210042932A (en) * | 2018-08-08 | 2021-04-20 | 브리스톨-마이어스 스큅 컴퍼니 | Substituted benzimidazole as a PAD4 inhibitor |
| WO2020033514A1 (en) * | 2018-08-08 | 2020-02-13 | Bristol-Myers Squibb Company | Benzimidazole inhibitors of pad enzymes |
| JP2021534108A (en) * | 2018-08-08 | 2021-12-09 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | PAD enzyme indole and azaindole inhibitors |
| CN112566916B (en) | 2018-08-08 | 2023-10-20 | 百时美施贵宝公司 | Substituted Thienopyrroles as PAD4 Inhibitors |
| CN109369513B (en) * | 2018-11-20 | 2020-08-25 | 都创(上海)医药科技有限公司 | Preparation method of FBDD common molecular fragment |
| JP7212781B2 (en) | 2018-12-19 | 2023-01-25 | ディスアーム セラピューティクス， インコーポレイテッド | Inhibitors of SARM1 in combination with neuroprotective agents |
| EP3994128A4 (en) * | 2019-07-03 | 2022-12-07 | University of Massachusetts | Inhibitors of protein arginine deiminase 1 and methods of preparation and use thereof |
| TW202115083A (en) * | 2019-09-27 | 2021-04-16 | 大陸商南京藥捷安康生物科技有限公司 | Peptidylarginine deiminase inhibitor and use thereof |
| KR20220137694A (en) * | 2020-02-06 | 2022-10-12 | 브리스톨-마이어스 스큅 컴퍼니 | Macrocyclic PAD4 inhibitors useful as immunosuppressants |
| TW202140477A (en) * | 2020-02-12 | 2021-11-01 | 美商必治妥美雅史谷比公司 | Heterocyclic pad4 inhibitors |
| CN111265526B (en) * | 2020-04-09 | 2021-03-19 | 黑龙江中医药大学 | Medicine for treating gastric cancer and preparation method thereof |
| CR20220550A (en) * | 2020-04-30 | 2022-12-15 | Gilead Sciences Inc | Macrocyclic inhibitors of peptidylarginine deiminases |
| KR20230093251A (en) | 2020-09-10 | 2023-06-27 | 프리시릭스 엔.브이. | Antibody fragment against FAP |
| WO2022059779A1 (en) | 2020-09-18 | 2022-03-24 | 大日本住友製薬株式会社 | Amine derivative |
| US11878965B2 (en) | 2020-12-22 | 2024-01-23 | Gilead Sciences, Inc. | Inhibitors of peptidylarginine deiminases |
| EP4433477A1 (en) | 2021-11-15 | 2024-09-25 | Regor Pharmaceuticals, Inc. | Pad4 inhibitors and use thereof |
| 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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| Publication number | Priority date | Publication date | Assignee | Title |
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| AU570439B2 (en) | 1983-03-28 | 1988-03-17 | Compression Labs, Inc. | A combined intraframe and interframe transform coding system |
| SI0820279T1 (en) | 1995-04-14 | 2002-12-31 | Smithkline Beecham Corporation | Metered dose inhaler for albuterol |
| TW533865U (en) | 1997-06-10 | 2003-05-21 | Glaxo Group Ltd | Dispenser for dispensing medicament and actuation indicating device |
| EP1114052B1 (en) * | 1998-09-18 | 2005-11-16 | Abbott GmbH & Co. KG | 4-aminopyrrolopyrimidines as kinase inhibitors |
| US6315112B1 (en) | 1998-12-18 | 2001-11-13 | 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 |
| US6119853A (en) | 1998-12-18 | 2000-09-19 | Glaxo Wellcome Inc. | 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 |
| ATE290865T1 (en) | 1999-10-19 | 2005-04-15 | Merck & Co Inc | TYROSINE KINASE INHIBITORS |
| CA2699568C (en) | 1999-12-24 | 2013-03-12 | Aventis Pharma Limited | 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 |
| CN1901958B (en) | 2003-11-03 | 2011-03-09 | 葛兰素集团有限公司 | A fluid dispensing device |
| CA2546192C (en) | 2003-11-17 | 2010-04-06 | Pfizer Products Inc. | Pyrrolopyrimidine compounds useful in treatment of cancer |
| FR2862971B1 (en) * | 2003-11-28 | 2006-03-24 | Sod Conseils Rech Applic | NOVEL BENZIMIDAZOLE AND IMIDAZO-PYRIDINE DERIVATIVES AND THEIR USE AS A MEDICINAL PRODUCT |
| US7429611B2 (en) | 2004-09-23 | 2008-09-30 | Bristol-Myers Squibb Company | Indole inhibitors of 15-lipoxygenase |
| EP2205085A1 (en) * | 2007-09-25 | 2010-07-14 | Merck Sharp & Dohme Corp. | 2-aryl or heteroaryl indole derivatives |
| JP2011521961A (en) | 2008-05-28 | 2011-07-28 | ワイス・エルエルシー | 3-substituted-1H-indole compounds, their use as mTOR kinase and PI3 kinase inhibitors, and their synthesis |
| RU2011106786A (en) * | 2008-07-23 | 2012-08-27 | Вертекс Фармасьютикалз Инкорпорейтед (Us) | PYRAZOLOPYRIDINKINASE INHIBITORS |
| EP2414328B1 (en) * | 2009-04-02 | 2021-05-26 | Merck Serono S.A. | 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 CA CA2879341A patent/CA2879341C/en active Active
- 2012-07-26 JP JP2015523426A patent/JP6063567B2/en active Active
- 2012-07-26 DK DK12740581.9T patent/DK2877467T3/en active
- 2012-07-26 LT LTEP12740581.9T patent/LT2877467T/en unknown
- 2012-07-26 US US14/416,937 patent/US9127003B2/en active Active
- 2012-07-26 KR KR1020157005099A patent/KR101916443B1/en active IP Right Grant
- 2012-07-26 PT PT127405819T patent/PT2877467T/en unknown
- 2012-07-26 CN CN201280074868.5A patent/CN104470919B/en active Active
- 2012-07-26 BR BR112015001545-0A patent/BR112015001545B1/en active IP Right Grant
- 2012-07-26 HU HUE12740581A patent/HUE033294T2/en unknown
- 2012-07-26 EP EP12740581.9A patent/EP2877467B1/en active Active
- 2012-07-26 SI SI201230769A patent/SI2877467T1/en unknown
- 2012-07-26 ES ES12740581.9T patent/ES2609126T3/en active Active
- 2012-07-26 RU RU2014152456A patent/RU2611010C2/en active
- 2012-07-26 IN IN2935KON2014 patent/IN2014KN02935A/en unknown
- 2012-07-26 PL PL12740581T patent/PL2877467T3/en unknown
- 2012-07-26 RS RS20170121A patent/RS55684B1/en unknown
- 2012-07-26 WO PCT/EP2012/064649 patent/WO2014015905A1/en active Application Filing
- 2012-07-26 AU AU2012386257A patent/AU2012386257B2/en active Active
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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/en unknown
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2017
- 2017-01-24 SM SM201700052T patent/SMT201700052B/en unknown
- 2017-01-27 CY CY20171100128T patent/CY1118524T1/en unknown
- 2017-11-20 US US15/817,562 patent/US10039755B2/en active Active
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