JP2017524026A5 - - Google Patents
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- Publication number
- JP2017524026A5 JP2017524026A5 JP2017510314A JP2017510314A JP2017524026A5 JP 2017524026 A5 JP2017524026 A5 JP 2017524026A5 JP 2017510314 A JP2017510314 A JP 2017510314A JP 2017510314 A JP2017510314 A JP 2017510314A JP 2017524026 A5 JP2017524026 A5 JP 2017524026A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- methoxy
- pyrazol
- benzoyl
- 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
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- 125000000217 alkyl group Chemical group 0.000 claims 115
- 229910052799 carbon Inorganic materials 0.000 claims 56
- 125000000623 heterocyclic group Chemical group 0.000 claims 49
- -1 CN Inorganic materials 0.000 claims 46
- 229910052739 hydrogen Inorganic materials 0.000 claims 46
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 31
- KXDAEFPNCMNJSK-UHFFFAOYSA-N benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 31
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 30
- 125000004485 2-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])([H])C1([H])* 0.000 claims 29
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 25
- 229910052717 sulfur Inorganic materials 0.000 claims 21
- 229910052757 nitrogen Inorganic materials 0.000 claims 19
- 125000004433 nitrogen atoms Chemical group N* 0.000 claims 19
- 125000001072 heteroaryl group Chemical group 0.000 claims 18
- 229910052760 oxygen Inorganic materials 0.000 claims 15
- 150000001875 compounds Chemical class 0.000 claims 14
- 125000004452 carbocyclyl group Chemical group 0.000 claims 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 11
- 239000011780 sodium chloride Substances 0.000 claims 11
- 125000006706 (C3-C6) carbocyclyl group Chemical group 0.000 claims 9
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 9
- 125000005418 aryl aryl group Chemical group 0.000 claims 9
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 8
- 125000000304 alkynyl group Chemical group 0.000 claims 7
- BHXVSMHUOZGMQI-UHFFFAOYSA-N COC1=C(C=CC(=C1)C(=O)N1C(CCC1)C1=CC(=CC=C1)OC)C=1C=NNC=1 Chemical compound COC1=C(C=CC(=C1)C(=O)N1C(CCC1)C1=CC(=CC=C1)OC)C=1C=NNC=1 BHXVSMHUOZGMQI-UHFFFAOYSA-N 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 125000004432 carbon atoms Chemical group C* 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- NXICWAPFCXEPDV-UHFFFAOYSA-N COC1=C(C=CC(=C1)C(=O)N1C(CCC1)C1=CC=CC=C1)C=1C=NNC=1 Chemical compound COC1=C(C=CC(=C1)C(=O)N1C(CCC1)C1=CC=CC=C1)C=1C=NNC=1 NXICWAPFCXEPDV-UHFFFAOYSA-N 0.000 claims 4
- VTLSDDFCKSOXNK-HXUWFJFHSA-N CS(=O)(=O)C=1C=C(C=CC=1)[C@@H]1N(CCC1)C(=O)C1=CC(=C(C=C1)C=1C=NNC=1)OC Chemical compound CS(=O)(=O)C=1C=C(C=CC=1)[C@@H]1N(CCC1)C(=O)C1=CC(=C(C=C1)C=1C=NNC=1)OC VTLSDDFCKSOXNK-HXUWFJFHSA-N 0.000 claims 4
- WPYMKLBDIGXBTP-UHFFFAOYSA-M benzoate Chemical compound [O-]C(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-M 0.000 claims 4
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 4
- 239000003112 inhibitor Substances 0.000 claims 4
- 230000002401 inhibitory effect Effects 0.000 claims 4
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 3
- 102000000568 rho-Associated Kinases Human genes 0.000 claims 3
- 108010041788 rho-Associated Kinases Proteins 0.000 claims 3
- 206010003816 Autoimmune disease Diseases 0.000 claims 2
- XLTJRBJXUOGHKG-UHFFFAOYSA-N BrC=1C=C(C=CC=1)C1N(CCC1)C(=O)C1=CC(=C(C=C1)C=1C=NNC=1)OC Chemical compound BrC=1C=C(C=CC=1)C1N(CCC1)C(=O)C1=CC(=C(C=C1)C=1C=NNC=1)OC XLTJRBJXUOGHKG-UHFFFAOYSA-N 0.000 claims 2
- UGKKGFNXRUWUMD-FBLFFUNLSA-N C(C)C=1C=C(C(=O)N2CC(C[C@@H]2C2=C(C=CC=C2)F)O)C=CC=1C=1C=NNC=1 Chemical compound C(C)C=1C=C(C(=O)N2CC(C[C@@H]2C2=C(C=CC=C2)F)O)C=CC=1C=1C=NNC=1 UGKKGFNXRUWUMD-FBLFFUNLSA-N 0.000 claims 2
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| CN106924254A (zh) * | 2015-12-31 | 2017-07-07 | 中国医学科学院药物研究所 | 黄连碱在制备预防和/或治疗系统性红斑狼疮及其并发症药物中的应用 |
| AR107354A1 (es) | 2016-01-13 | 2018-04-18 | Bristol Myers Squibb Co | Salicilamidas espiroheptanos y compuestos relacionados como inhibidores de rock |
| KR102457933B1 (ko) | 2016-05-27 | 2022-10-24 | 브리스톨-마이어스 스큅 컴퍼니 | Rock의 억제제로서의 트리아졸론 및 테트라졸론 |
| US10730858B2 (en) | 2016-07-07 | 2020-08-04 | Bristol-Myers Squibb Company | Lactam, cyclic urea and carbamate, and triazolone derivatives as potent and selective rock inhibitors |
| US10696674B2 (en) | 2016-07-07 | 2020-06-30 | Bristol-Myers Squibb Company | Spirolactams as inhibitors of ROCK |
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2015
- 2015-08-20 CN CN201580044710.7A patent/CN107108581B/zh active Active
- 2015-08-20 WO PCT/US2015/046032 patent/WO2016028971A1/en active Application Filing
- 2015-08-20 US US15/503,419 patent/US10112939B2/en active Active
- 2015-08-20 EP EP15756322.2A patent/EP3183248B1/en active Active
- 2015-08-20 ES ES15756322T patent/ES2838573T3/es active Active
- 2015-08-20 JP JP2017510314A patent/JP6633618B2/ja active Active
