JP2017528481A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2017528481A5 JP2017528481A5 JP2017514486A JP2017514486A JP2017528481A5 JP 2017528481 A5 JP2017528481 A5 JP 2017528481A5 JP 2017514486 A JP2017514486 A JP 2017514486A JP 2017514486 A JP2017514486 A JP 2017514486A JP 2017528481 A5 JP2017528481 A5 JP 2017528481A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- het
- halo
- independently
- cycloalkyl
- Prior art date
- Legal status (The legal status 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 status listed.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims 234
- 125000001475 halogen functional group Chemical group 0.000 claims 77
- 125000001424 substituent group Chemical group 0.000 claims 37
- 150000001875 compounds Chemical class 0.000 claims 17
- 229910052757 nitrogen Inorganic materials 0.000 claims 16
- 125000005842 heteroatom Chemical group 0.000 claims 15
- 125000000753 cycloalkyl group Chemical group 0.000 claims 14
- 229910052760 oxygen Inorganic materials 0.000 claims 12
- 229910052717 sulfur Inorganic materials 0.000 claims 9
- 125000000623 heterocyclic group Chemical group 0.000 claims 8
- 239000000203 mixture Substances 0.000 claims 8
- 201000010099 disease Diseases 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 230000002265 prevention Effects 0.000 claims 4
- 238000003745 diagnosis Methods 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 2
- 208000009137 Behcet syndrome Diseases 0.000 claims 1
- 208000009766 Blau syndrome Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 101001109137 Homo sapiens Receptor-interacting serine/threonine-protein kinase 2 Proteins 0.000 claims 1
- 102000004877 Insulin Human genes 0.000 claims 1
- 108090001061 Insulin Proteins 0.000 claims 1
- 150000001204 N-oxides Chemical class 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 102100022502 Receptor-interacting serine/threonine-protein kinase 2 Human genes 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 208000010758 granulomatous inflammation Diseases 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 229940125396 insulin Drugs 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000002207 metabolite Substances 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 201000000306 sarcoidosis Diseases 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14185130 | 2014-09-17 | ||
| EP14185130.3 | 2014-09-17 | ||
| PCT/EP2015/071347 WO2016042087A1 (en) | 2014-09-17 | 2015-09-17 | Macrocyclic rip2 kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017528481A JP2017528481A (ja) | 2017-09-28 |
| JP2017528481A5 true JP2017528481A5 (enExample) | 2018-09-13 |
| JP6736545B2 JP6736545B2 (ja) | 2020-08-05 |
Family
ID=51687776
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017514486A Active JP6736545B2 (ja) | 2014-09-17 | 2015-09-17 | 大環状ｒｉｐ２キナーゼ阻害剤 |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US10676486B2 (enExample) |
| EP (1) | EP3194407B1 (enExample) |
| JP (1) | JP6736545B2 (enExample) |
| KR (1) | KR102563829B1 (enExample) |
| CN (1) | CN106687464B (enExample) |
| AU (1) | AU2015316799B2 (enExample) |
| BR (1) | BR112017004035B1 (enExample) |
| CA (1) | CA2958782C (enExample) |
| DK (1) | DK3194407T3 (enExample) |
| EA (1) | EA032872B1 (enExample) |
| ES (1) | ES2763344T3 (enExample) |
| HR (1) | HRP20192334T1 (enExample) |
| HU (1) | HUE048518T2 (enExample) |
| IL (1) | IL250544B (enExample) |
| LT (1) | LT3194407T (enExample) |
| MX (1) | MX376087B (enExample) |
| MY (1) | MY186523A (enExample) |
| PL (1) | PL3194407T3 (enExample) |
| PT (1) | PT3194407T (enExample) |
| SA (1) | SA517381087B1 (enExample) |
| SG (1) | SG11201701116XA (enExample) |
| SI (1) | SI3194407T1 (enExample) |
| TW (1) | TWI709563B (enExample) |
| UA (1) | UA121315C2 (enExample) |
| WO (1) | WO2016042087A1 (enExample) |
| ZA (1) | ZA201701331B (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102719387B1 (ko) * | 2017-01-26 | 2024-10-21 | 한미약품 주식회사 | 이미다조피리다진 화합물 |
| AR124556A1 (es) | 2020-01-31 | 2023-04-12 | Oncodesign Sa | Inhibidores macrocíclicos de rip2-cinasa |
| WO2024051631A1 (zh) * | 2022-09-07 | 2024-03-14 | 苏州朗睿生物医药有限公司 | 一种大环咪唑并[1,2-b]哒嗪衍生物及其制备方法和用途 |
| CN120500490A (zh) * | 2023-01-03 | 2025-08-15 | 广东新契生物医药科技有限公司 | 作为usp1抑制剂的大环化合物 |
| WO2025212514A2 (en) * | 2024-04-02 | 2025-10-09 | Interline Therapeutics, Inc. | Methods of treating inflammatory diseases |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IS2334B (is) | 1992-09-08 | 2008-02-15 | Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) | Aspartyl próteasi hemjari af nýjum flokki súlfonamíða |
| SK283569B6 (sk) | 1993-10-01 | 2003-09-11 | Astra Aktiebolag | Spôsob spracovania jemne deleného práškového liečiva, zariadenie na vykonávanie tohto spôsobu a aglomeráty vyrobené týmto spôsobom |
| US6043358A (en) | 1995-11-01 | 2000-03-28 | Merck & Co., Inc. | Hexahydro-5-imino-1,4-heteroazepine derivatives as inhibitors of nitric oxide synthases |
| GB9718913D0 (en) | 1997-09-05 | 1997-11-12 | Glaxo Group Ltd | Substituted oxindole derivatives |
| US6369087B1 (en) | 1999-08-26 | 2002-04-09 | Robert R. Whittle | Alkoxy substituted benzimidazole compounds, pharmaceutical preparations containing the same, and methods of using the same |
| US7750007B2 (en) * | 2006-11-06 | 2010-07-06 | Supergen, Inc. | Imidazo[1,2-beta]pyridazine and pyrazolo[1,5-alpha]pyrimidine derivatives and their use as protein kinase inhibitors |
| AR077468A1 (es) * | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| AU2011256380C1 (en) * | 2010-05-20 | 2016-09-08 | Array Biopharma Inc. | Macrocyclic compounds as Trk kinase inhibitors |
| WO2013001310A1 (en) | 2011-06-30 | 2013-01-03 | Centro Nacional De Investigaciones Oncológicas (Cnio) | Macrocyclic compounds and their use as cdk8 inhibitors |
| TWI547494B (zh) * | 2011-08-18 | 2016-09-01 | 葛蘭素史克智慧財產發展有限公司 | 作為激酶抑制劑之胺基喹唑啉類 |
| ES2583477T3 (es) | 2011-09-30 | 2016-09-21 | Ipsen Pharma S.A.S. | Inhibidores macrocíclicos de cinasa de LRRK2 |
| KR20140078710A (ko) * | 2011-09-30 | 2014-06-25 | 온코디자인 에스.에이. | 거대고리 flt3 키나제 억제제 |
-
2015
- 2015-09-17 WO PCT/EP2015/071347 patent/WO2016042087A1/en not_active Ceased
- 2015-09-17 BR BR112017004035-2A patent/BR112017004035B1/pt active IP Right Grant
- 2015-09-17 AU AU2015316799A patent/AU2015316799B2/en active Active
- 2015-09-17 HU HUE15766800A patent/HUE048518T2/hu unknown
- 2015-09-17 KR KR1020177010128A patent/KR102563829B1/ko active Active
- 2015-09-17 EA EA201790609A patent/EA032872B1/ru unknown
- 2015-09-17 PT PT157668005T patent/PT3194407T/pt unknown
- 2015-09-17 SI SI201531050T patent/SI3194407T1/sl unknown
- 2015-09-17 UA UAA201703558A patent/UA121315C2/uk unknown
- 2015-09-17 EP EP15766800.5A patent/EP3194407B1/en active Active
- 2015-09-17 PL PL15766800T patent/PL3194407T3/pl unknown
- 2015-09-17 DK DK15766800.5T patent/DK3194407T3/da active
- 2015-09-17 MY MYPI2017700447A patent/MY186523A/en unknown
- 2015-09-17 SG SG11201701116XA patent/SG11201701116XA/en unknown
- 2015-09-17 JP JP2017514486A patent/JP6736545B2/ja active Active
- 2015-09-17 HR HRP20192334TT patent/HRP20192334T1/hr unknown
- 2015-09-17 LT LTEP15766800.5T patent/LT3194407T/lt unknown
- 2015-09-17 CA CA2958782A patent/CA2958782C/en active Active
- 2015-09-17 ES ES15766800T patent/ES2763344T3/es active Active
- 2015-09-17 CN CN201580050163.3A patent/CN106687464B/zh active Active
- 2015-09-17 MX MX2017003469A patent/MX376087B/es active IP Right Grant
- 2015-09-17 TW TW104130751A patent/TWI709563B/zh active
- 2015-09-17 US US15/505,976 patent/US10676486B2/en active Active
-
2017
- 2017-02-09 IL IL250544A patent/IL250544B/en active IP Right Grant
- 2017-02-22 ZA ZA2017/01331A patent/ZA201701331B/en unknown
- 2017-03-14 SA SA517381087A patent/SA517381087B1/ar unknown