EA033197B1 - Замещенные 4-азаиндолы и их применение в качестве модуляторов рецептора glun2b - Google Patents
Замещенные 4-азаиндолы и их применение в качестве модуляторов рецептора glun2bInfo
- Publication number
- EA033197B1 EA033197B1 EA201890245A EA201890245A EA033197B1 EA 033197 B1 EA033197 B1 EA 033197B1 EA 201890245 A EA201890245 A EA 201890245A EA 201890245 A EA201890245 A EA 201890245A EA 033197 B1 EA033197 B1 EA 033197B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- azaindoles
- substituted
- receptor modulators
- nr2b
- glun2b receptor
- Prior art date
Links
Classifications
-
- 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
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Communicable Diseases (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Rheumatology (AREA)
- Addiction (AREA)
- Vascular Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562190416P | 2015-07-09 | 2015-07-09 | |
| PCT/US2016/041339 WO2017007938A1 (en) | 2015-07-09 | 2016-07-07 | Substituted 4-azaindoles and their use as glun2b receptor modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201890245A1 EA201890245A1 (ru) | 2018-06-29 |
| EA033197B1 true EA033197B1 (ru) | 2019-09-30 |
Family
ID=56497884
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201890245A EA033197B1 (ru) | 2015-07-09 | 2016-07-07 | Замещенные 4-азаиндолы и их применение в качестве модуляторов рецептора glun2b |
Country Status (25)
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT3180329T (pt) | 2014-08-15 | 2020-06-08 | Janssen Pharmaceuticals Inc | Triazóis como inibidores do recetor nr2b |
| USRE49517E1 (en) | 2014-08-15 | 2023-05-02 | Janssen Pharmaceuticals, Inc. | Pyrazoles |
| HRP20200410T1 (hr) * | 2015-07-09 | 2020-08-21 | Janssen Pharmaceutica Nv | Supstituirani 4-azaindoli i njihova upotreba kao modulatora glun2b receptora |
| CN109071488B (zh) | 2016-02-10 | 2021-08-13 | 詹森药业有限公司 | 取代的1,2,3-三唑作为nr2b-选择性nmda调节剂 |
| TW201819376A (zh) * | 2016-10-06 | 2018-06-01 | 比利時商健生藥品公司 | 經取代之１Ｈ－咪唑並［４，５－ｂ］吡啶－２（３Ｈ）－酮及其作為ＧＬＵＮ２Ｂ受體調節劑之用途 |
| US11447503B2 (en) | 2019-06-14 | 2022-09-20 | Janssen Pharmaceutica Nv | Pyridine carbamates and their use as GLUN2B receptor modulators |
| JP7346441B2 (ja) * | 2018-04-04 | 2023-09-19 | ヤンセン ファーマシューティカ エヌ．ベー． | 置換ピリジン及びピリミジン並びにｇｌｕｎ２ｂ受容体調節物質としてのそれらの使用 |
| TW202112774A (zh) * | 2019-06-14 | 2021-04-01 | 比利時商健生藥品公司 | 經取代之吡唑并－吡啶醯胺及其作為ｇｌｕｎ２ｂ受體調節劑之用途 |
| JP2022536424A (ja) * | 2019-06-14 | 2022-08-16 | ヤンセン ファーマシューティカ エヌ．ベー． | 置換ヘテロ芳香族ピラゾロピリジン及びｇｌｕｎ２ｂ受容体調節因子としてのそれらの使用 |
| CA3142998A1 (en) | 2019-06-14 | 2020-12-17 | Janssen Pharmaceutica Nv | Pyrazine carbamates and their use as glun2b receptor modulators |
| KR20220020917A (ko) * | 2019-06-14 | 2022-02-21 | 얀센 파마슈티카 엔.브이. | 치환된 피라졸로[4,3-b]피리딘 및 GLUN2B 수용체 조절제로서의 이들의 용도 |
| MX2021015500A (es) | 2019-06-14 | 2022-02-10 | Janssen Pharmaceutica Nv | Pirazolo-pirazinas sustituidas y su uso como moduladores del receptor glun2b. |
| PH12021552839A1 (en) | 2019-06-14 | 2022-10-03 | Janssen Pharmaceutica Nv | Substituted pyrazolo-pyridine amides and their use as glun2b receptor modulators |
| CN114621125B (zh) * | 2020-12-14 | 2024-07-09 | 中国科学技术大学 | Nlrp3炎症小体抑制剂及其应用 |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003082868A1 (en) * | 2002-03-28 | 2003-10-09 | Eisai Co., Ltd. | 7-azaindoles as inhibitors of c-jun n-terminal kinases for the treatment of neurodegenerative disorders |
| US20070275965A1 (en) * | 2006-03-30 | 2007-11-29 | Chemocentryx, Inc. | CXCR4 modulators |
| US20080300239A1 (en) * | 2007-05-18 | 2008-12-04 | Adams Nicholas D | Quinoline derivatives as pi3 kinase inhibitors |
| WO2010043396A1 (en) * | 2008-10-16 | 2010-04-22 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc. | Indole and benzomorpholine derivatives as modulators of metabotropic glutamate receptors |
| WO2014124651A1 (en) * | 2013-02-15 | 2014-08-21 | Københavns Universitet | Pyrrolidine-2-carboxylic acid derivatives as iglur antagonists |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200604183A (en) | 2004-02-18 | 2006-02-01 | Astrazeneca Ab | Triazole compounds and their use as metabotropic glutamate receptor antagonists |
| US20060183758A1 (en) * | 2005-02-17 | 2006-08-17 | Cb Research And Development, Inc. | Method for synthesis of AZA-annelated pyrroles, thiophenes, and furans |
| KR20100017372A (ko) | 2007-05-25 | 2010-02-16 | 애보트 게엠베하 운트 콤파니 카게 | 향대사성 글루타메이트 수용체 2（ｍｇｌｕ2 수용체）의 포지티브 조절자로서의 헤테로사이클릭 화합물 |
| WO2009005821A1 (en) | 2007-07-03 | 2009-01-08 | Edward Scott Carlson | Support apparatus for climbing plants |
| EP2194045A4 (en) | 2007-08-30 | 2011-09-21 | Takeda Pharmaceutical | Substituted pyrazole derivative |
| EP2215073A4 (en) | 2007-10-31 | 2011-04-06 | Merck Sharp & Dohme | SLEEP MODULATION WITH NR2B RECEPTOR ANTAGONISTS |
| RU2499598C2 (ru) | 2008-03-27 | 2013-11-27 | Евотек Интернациональ Гмбх | Способы лечения нарушений с применением селективного антагониста nr2b-подтипа nmda рецепторов |
| WO2010016490A1 (ja) | 2008-08-05 | 2010-02-11 | 第一三共株式会社 | イミダゾピリジン－２－オン誘導体 |
| EP3037421A3 (en) | 2008-11-25 | 2016-11-30 | University Of Rochester | Mlk inhibitors and methods of use |
| TWI625121B (zh) * | 2009-07-13 | 2018-06-01 | 基利科學股份有限公司 | 調節細胞凋亡信號之激酶的抑制劑 |
| WO2011156245A2 (en) | 2010-06-09 | 2011-12-15 | Merck Sharp & Dohme Corp. | Positive allosteric modulators of mglur2 |
| WO2013130855A1 (en) | 2012-03-02 | 2013-09-06 | Takeda Pharmaceutical Company Limited | Indazole derivatives |
| EP2970200A1 (en) * | 2013-03-13 | 2016-01-20 | Abbvie Inc. | Pyridine cdk9 kinase inhibitors |
| RU2680100C9 (ru) * | 2013-03-15 | 2019-04-18 | Плексксикон Инк. | Гетероциклические соединения и их применения |
| CN103626767A (zh) * | 2013-12-04 | 2014-03-12 | 上海药明康德新药开发有限公司 | 区域选择性的氮杂吲哚及其合成方法 |
| PT3180329T (pt) | 2014-08-15 | 2020-06-08 | Janssen Pharmaceuticals Inc | Triazóis como inibidores do recetor nr2b |
| USRE49517E1 (en) | 2014-08-15 | 2023-05-02 | Janssen Pharmaceuticals, Inc. | Pyrazoles |
| HRP20200410T1 (hr) | 2015-07-09 | 2020-08-21 | Janssen Pharmaceutica Nv | Supstituirani 4-azaindoli i njihova upotreba kao modulatora glun2b receptora |
| CN109071488B (zh) | 2016-02-10 | 2021-08-13 | 詹森药业有限公司 | 取代的1,2,3-三唑作为nr2b-选择性nmda调节剂 |
| TW201819376A (zh) | 2016-10-06 | 2018-06-01 | 比利時商健生藥品公司 | 經取代之１Ｈ－咪唑並［４，５－ｂ］吡啶－２（３Ｈ）－酮及其作為ＧＬＵＮ２Ｂ受體調節劑之用途 |
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2016
- 2016-07-07 HR HRP20200410TT patent/HRP20200410T1/hr unknown
- 2016-07-07 CN CN201680052507.9A patent/CN108026094B/zh active Active
- 2016-07-07 AU AU2016291158A patent/AU2016291158B2/en active Active
- 2016-07-07 KR KR1020187003560A patent/KR20180026760A/ko not_active Withdrawn
- 2016-07-07 DK DK16741469.7T patent/DK3319963T3/da active
- 2016-07-07 JP JP2018500737A patent/JP6964576B2/ja active Active
- 2016-07-07 EP EP16741469.7A patent/EP3319963B1/en active Active
- 2016-07-07 EA EA201890245A patent/EA033197B1/ru not_active IP Right Cessation
- 2016-07-07 LT LTEP16741469.7T patent/LT3319963T/lt unknown
- 2016-07-07 SM SM20200134T patent/SMT202000134T1/it unknown
- 2016-07-07 MX MX2018000352A patent/MX2018000352A/es unknown
- 2016-07-07 PT PT167414697T patent/PT3319963T/pt unknown
- 2016-07-07 MA MA42397A patent/MA42397B1/fr unknown
- 2016-07-07 BR BR112018000468-5A patent/BR112018000468A2/pt not_active Application Discontinuation
- 2016-07-07 SI SI201630594T patent/SI3319963T1/sl unknown
- 2016-07-07 HU HUE16741469A patent/HUE047460T2/hu unknown
- 2016-07-07 CA CA2991765A patent/CA2991765C/en active Active
- 2016-07-07 PL PL16741469T patent/PL3319963T3/pl unknown
- 2016-07-07 WO PCT/US2016/041339 patent/WO2017007938A1/en not_active Ceased
- 2016-07-07 MD MDE20180505T patent/MD3319963T2/ro not_active IP Right Cessation
- 2016-07-07 ES ES16741469T patent/ES2781867T3/es active Active
- 2016-07-08 US US15/205,632 patent/US9963447B2/en active Active
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2018
- 2018-01-07 IL IL256758A patent/IL256758A/en unknown
- 2018-02-08 ZA ZA2018/00827A patent/ZA201800827B/en unknown
- 2018-03-20 US US15/926,440 patent/US10377753B2/en active Active
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2020
- 2020-03-24 CY CY20201100280T patent/CY1123007T1/el unknown
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2021
- 2021-08-27 JP JP2021138906A patent/JP7369743B2/ja active Active
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003082868A1 (en) * | 2002-03-28 | 2003-10-09 | Eisai Co., Ltd. | 7-azaindoles as inhibitors of c-jun n-terminal kinases for the treatment of neurodegenerative disorders |
| US20070275965A1 (en) * | 2006-03-30 | 2007-11-29 | Chemocentryx, Inc. | CXCR4 modulators |
| US20080300239A1 (en) * | 2007-05-18 | 2008-12-04 | Adams Nicholas D | Quinoline derivatives as pi3 kinase inhibitors |
| WO2010043396A1 (en) * | 2008-10-16 | 2010-04-22 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc. | Indole and benzomorpholine derivatives as modulators of metabotropic glutamate receptors |
| WO2014124651A1 (en) * | 2013-02-15 | 2014-08-21 | Københavns Universitet | Pyrrolidine-2-carboxylic acid derivatives as iglur antagonists |
Non-Patent Citations (1)
| Title |
|---|
| BUONARATI M H, TURTELTAUB K W, SHEN N H, FELTON J S: "Role of sulfation and acetylation in the activation of 2-hydroxyamino-1-methyl-6-phenyl-imidazo[4,5-b]pyridine to intermeidates which bind DNA", MUTATION RESEARCH LETTERS, ELSEVIER, NL, vol. 245, no. 3, 1 November 1990 (1990-11-01), NL, pages 185 - 190, XP002760909, ISSN: 0165-7992, DOI: 10.1016/0165-7992(90)90048-O * |
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