JP2020527560A5 - - Google Patents
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- JP2020527560A5 JP2020527560A5 JP2020501553A JP2020501553A JP2020527560A5 JP 2020527560 A5 JP2020527560 A5 JP 2020527560A5 JP 2020501553 A JP2020501553 A JP 2020501553A JP 2020501553 A JP2020501553 A JP 2020501553A JP 2020527560 A5 JP2020527560 A5 JP 2020527560A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- amino
- nicotinamide
- oxoethyl
- phenoxy
- 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 203
- DFPAKSUCGFBDDF-UHFFFAOYSA-N Nicotinamide Chemical compound NC(=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-UHFFFAOYSA-N 0.000 claims 66
- 125000003545 alkoxy group Chemical group 0.000 claims 48
- 125000000623 heterocyclic group Chemical group 0.000 claims 48
- 229960003966 nicotinamide Drugs 0.000 claims 33
- 235000005152 nicotinamide Nutrition 0.000 claims 33
- 239000011570 nicotinamide Substances 0.000 claims 33
- 229910052736 halogen Inorganic materials 0.000 claims 29
- 150000002367 halogens Chemical class 0.000 claims 28
- -1 2-Fluoro-4- (2-oxo-2-((5- (2-oxo-1,2-dihydropyridine-4-yl) benzo [d] thiazole-2-yl) amino) ethyl) phenoxy Chemical group 0.000 claims 25
- 229910052739 hydrogen Inorganic materials 0.000 claims 23
- 229910052799 carbon Inorganic materials 0.000 claims 19
- 229910052757 nitrogen Inorganic materials 0.000 claims 19
- 150000001875 compounds Chemical class 0.000 claims 16
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 16
- 125000005842 heteroatom Chemical group 0.000 claims 15
- 229910052760 oxygen Inorganic materials 0.000 claims 15
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 15
- 125000002947 alkylene group Chemical group 0.000 claims 12
- 229910052801 chlorine Inorganic materials 0.000 claims 12
- 229910052731 fluorine Inorganic materials 0.000 claims 12
- 229910052717 sulfur Inorganic materials 0.000 claims 12
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 11
- 229910004013 NO 2 Inorganic materials 0.000 claims 10
- 125000004432 carbon atom Chemical group C* 0.000 claims 9
- 125000003342 alkenyl group Chemical group 0.000 claims 7
- 125000000304 alkynyl group Chemical group 0.000 claims 7
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims 7
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 7
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 6
- 229910052794 bromium Inorganic materials 0.000 claims 6
- 125000002837 carbocyclic group Chemical group 0.000 claims 6
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 5
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 5
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 4
- 125000004414 alkyl thio group Chemical group 0.000 claims 4
- 150000001721 carbon Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000004429 atom Chemical group 0.000 claims 3
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 1
- PYBNZXKOTHEYCW-UHFFFAOYSA-N 2-[2-chloro-4-[2-[[1-(cyclopropylmethyl)-4-fluorobenzimidazol-2-yl]amino]-2-oxoethyl]phenoxy]pyridine-3-carboxamide Chemical compound ClC1=C(OC2=C(C(=O)N)C=CC=N2)C=CC(=C1)CC(=O)NC1=NC2=C(N1CC1CC1)C=CC=C2F PYBNZXKOTHEYCW-UHFFFAOYSA-N 0.000 claims 1
- BVAWUHMTBUKGOL-UHFFFAOYSA-N 2-[2-chloro-4-[2-[[1-(cyclopropylmethyl)-5-fluorobenzimidazol-2-yl]amino]-2-oxoethyl]phenoxy]pyridine-3-carboxamide Chemical compound ClC1=C(OC2=C(C(=O)N)C=CC=N2)C=CC(=C1)CC(=O)NC1=NC2=C(N1CC1CC1)C=CC(=C2)F BVAWUHMTBUKGOL-UHFFFAOYSA-N 0.000 claims 1
- NMZNIDKIUYCRPN-UHFFFAOYSA-N 2-[4-[2-[[1-(2,2-difluoroethyl)-6-fluorobenzimidazol-2-yl]amino]-2-oxoethyl]-2-fluorophenoxy]pyridine-3-carboxamide Chemical compound FC(CN1C(=NC2=C1C=C(C=C2)F)NC(CC1=CC(=C(OC2=C(C(=O)N)C=CC=N2)C=C1)F)=O)F NMZNIDKIUYCRPN-UHFFFAOYSA-N 0.000 claims 1
- QRZOOGMNBAFQNM-UHFFFAOYSA-N 2-[4-[2-[[1-(cyclopropylmethyl)-4-fluorobenzimidazol-2-yl]amino]-2-oxoethyl]-2-fluorophenoxy]pyridine-3-carboxamide Chemical compound C1(CC1)CN1C(=NC2=C1C=CC=C2F)NC(CC1=CC(=C(OC2=C(C(=O)N)C=CC=N2)C=C1)F)=O QRZOOGMNBAFQNM-UHFFFAOYSA-N 0.000 claims 1
- ORACJASUMJXKPH-UHFFFAOYSA-N 2-[4-[2-[[1-(cyclopropylmethyl)-6-fluorobenzimidazol-2-yl]amino]-2-oxoethyl]-2-fluorophenoxy]pyridine-3-carboxamide Chemical compound C1(CC1)CN1C(=NC2=C1C=C(C=C2)F)NC(CC1=CC(=C(OC2=C(C(=O)N)C=CC=N2)C=C1)F)=O ORACJASUMJXKPH-UHFFFAOYSA-N 0.000 claims 1
- SMJDDHFPTIDCDR-UHFFFAOYSA-N 2-[4-[2-[[1-(cyclopropylmethyl)-6-phenylmethoxybenzimidazol-2-yl]amino]-2-oxoethyl]-2-fluorophenoxy]pyridine-3-carboxamide Chemical compound C(C1=CC=CC=C1)OC=1C=CC2=C(N(C(=N2)NC(CC2=CC(=C(OC3=C(C(=O)N)C=CC=N3)C=C2)F)=O)CC2CC2)C=1 SMJDDHFPTIDCDR-UHFFFAOYSA-N 0.000 claims 1
- AVYSMNTTWOATNF-UHFFFAOYSA-N 2-[4-[2-[[1-(cyclopropylmethyl)-7-fluorobenzimidazol-2-yl]amino]-2-oxoethyl]-2-fluorophenoxy]pyridine-3-carboxamide Chemical compound C1(CC1)CN1C(=NC2=C1C(=CC=C2)F)NC(CC1=CC(=C(OC2=C(C(=O)N)C=CC=N2)C=C1)F)=O AVYSMNTTWOATNF-UHFFFAOYSA-N 0.000 claims 1
- RNDXHQRUMYUJIR-UHFFFAOYSA-N 2-[4-[2-[[1-(cyclopropylmethyl)benzimidazol-2-yl]amino]-2-oxoethyl]-2-fluorophenoxy]pyridine-3-carboxamide Chemical compound C1(CC1)CN1C(=NC2=C1C=CC=C2)NC(CC1=CC(=C(OC2=C(C(=O)N)C=CC=N2)C=C1)F)=O RNDXHQRUMYUJIR-UHFFFAOYSA-N 0.000 claims 1
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 1
- 206010002383 Angina Pectoris Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- FHFJCUSWDYNRSI-UHFFFAOYSA-N C1(CC1)CN1C(=NC2=C1C=C(C=C2)OC)NC(CC1=CC(=C(OC2=C(C(=O)N)C=CC=N2)C=C1)F)=O Chemical compound C1(CC1)CN1C(=NC2=C1C=C(C=C2)OC)NC(CC1=CC(=C(OC2=C(C(=O)N)C=CC=N2)C=C1)F)=O FHFJCUSWDYNRSI-UHFFFAOYSA-N 0.000 claims 1
- YPUJMVQINMZCTE-UHFFFAOYSA-N C1(CC1)CN1C(=NC2=C1C=CC(=C2)OC)NC(CC1=CC(=C(OC2=C(C(=O)N)C=CC=N2)C=C1)F)=O Chemical compound C1(CC1)CN1C(=NC2=C1C=CC(=C2)OC)NC(CC1=CC(=C(OC2=C(C(=O)N)C=CC=N2)C=C1)F)=O YPUJMVQINMZCTE-UHFFFAOYSA-N 0.000 claims 1
- SLFMWHLMCWZYLM-UHFFFAOYSA-N C1(CC1)CN1C(=NC2=C1C=CC=C2OC)NC(CC1=CC(=C(OC2=C(C(=O)N)C=CC=N2)C=C1)F)=O Chemical compound C1(CC1)CN1C(=NC2=C1C=CC=C2OC)NC(CC1=CC(=C(OC2=C(C(=O)N)C=CC=N2)C=C1)F)=O SLFMWHLMCWZYLM-UHFFFAOYSA-N 0.000 claims 1
- RJSBIHPGPOANAQ-UHFFFAOYSA-N CC1=C(C=CC=2N1N=C(N=2)NC(CC1=CC(=C(OC2=C(C(=O)N)C=CC=N2)C=C1)F)=O)C Chemical compound CC1=C(C=CC=2N1N=C(N=2)NC(CC1=CC(=C(OC2=C(C(=O)N)C=CC=N2)C=C1)F)=O)C RJSBIHPGPOANAQ-UHFFFAOYSA-N 0.000 claims 1
- CYECZCLVAZKDKL-UHFFFAOYSA-N CC=1C(=CC=2N(C=1)N=C(N=2)NC(CC1=CC(=C(OC2=C(C(=O)N)C=CC=N2)C=C1)F)=O)C Chemical compound CC=1C(=CC=2N(C=1)N=C(N=2)NC(CC1=CC(=C(OC2=C(C(=O)N)C=CC=N2)C=C1)F)=O)C CYECZCLVAZKDKL-UHFFFAOYSA-N 0.000 claims 1
- DXEGJCVJSJSGAX-UHFFFAOYSA-N CP(=O)(C)C1=CC2=C(N(C(=N2)NC(CC2=CC(=C(OC3=C(C(=O)N)C=CC=N3)C=C2)F)=O)CC(F)(F)F)C=C1 Chemical compound CP(=O)(C)C1=CC2=C(N(C(=N2)NC(CC2=CC(=C(OC3=C(C(=O)N)C=CC=N3)C=C2)F)=O)CC(F)(F)F)C=C1 DXEGJCVJSJSGAX-UHFFFAOYSA-N 0.000 claims 1
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 1
- SQZOIPUKILNRFH-UHFFFAOYSA-N ClC1=C(OC2=C(C(=O)N)C=CC=N2)C=CC(=C1)CC(=O)NC1=NC2=C(N1CC(F)F)C=CC=C2F Chemical compound ClC1=C(OC2=C(C(=O)N)C=CC=N2)C=CC(=C1)CC(=O)NC1=NC2=C(N1CC(F)F)C=CC=C2F SQZOIPUKILNRFH-UHFFFAOYSA-N 0.000 claims 1
- UYZSOAJLURWTDZ-UHFFFAOYSA-N ClC1=C(OC2=C(C(=O)N)C=CC=N2)C=CC(=C1)CC(=O)NC1=NC2=C(N1CC1CC1)C=C(C=C2)F Chemical compound ClC1=C(OC2=C(C(=O)N)C=CC=N2)C=CC(=C1)CC(=O)NC1=NC2=C(N1CC1CC1)C=C(C=C2)F UYZSOAJLURWTDZ-UHFFFAOYSA-N 0.000 claims 1
- MTFQDPIPYZYBST-UHFFFAOYSA-N ClC1=C(OC2=C(C(=O)N)C=CC=N2)C=CC(=C1)CC(=O)NC1=NN2C(C=C(C=C2)OC)=N1 Chemical compound ClC1=C(OC2=C(C(=O)N)C=CC=N2)C=CC(=C1)CC(=O)NC1=NN2C(C=C(C=C2)OC)=N1 MTFQDPIPYZYBST-UHFFFAOYSA-N 0.000 claims 1
- BVWXXNYAYHRKGQ-UHFFFAOYSA-N ClC1=C(OC2=C(C(=O)N)C=CC=N2)C=CC(=C1)CC(=O)NC=1SC2=NC(=CC=C2N=1)OC(F)F Chemical compound ClC1=C(OC2=C(C(=O)N)C=CC=N2)C=CC(=C1)CC(=O)NC=1SC2=NC(=CC=C2N=1)OC(F)F BVWXXNYAYHRKGQ-UHFFFAOYSA-N 0.000 claims 1
- DSAUQYLXJQKSOA-UHFFFAOYSA-N FC(CN1C(=NC2=C1C=C(C=C2)OC)NC(CC1=CC(=C(OC2=C(C(=O)N)C=CC=N2)C=C1)F)=O)F Chemical compound FC(CN1C(=NC2=C1C=C(C=C2)OC)NC(CC1=CC(=C(OC2=C(C(=O)N)C=CC=N2)C=C1)F)=O)F DSAUQYLXJQKSOA-UHFFFAOYSA-N 0.000 claims 1
- WOKWTRLJJGXTKX-UHFFFAOYSA-N FC(CN1C(=NC2=C1C=C(C=C2)P(=O)(C)C)NC(CC1=CC(=C(OC2=C(C(=O)N)C=CC=N2)C=C1)F)=O)F Chemical compound FC(CN1C(=NC2=C1C=C(C=C2)P(=O)(C)C)NC(CC1=CC(=C(OC2=C(C(=O)N)C=CC=N2)C=C1)F)=O)F WOKWTRLJJGXTKX-UHFFFAOYSA-N 0.000 claims 1
- HTOGGPPMVUMBCH-UHFFFAOYSA-N FC(CN1C(=NC2=C1C=CC=C2F)NC(CC1=CC(=C(OC2=C(C(=O)N)C=CC=N2)C=C1)F)=O)F Chemical compound FC(CN1C(=NC2=C1C=CC=C2F)NC(CC1=CC(=C(OC2=C(C(=O)N)C=CC=N2)C=C1)F)=O)F HTOGGPPMVUMBCH-UHFFFAOYSA-N 0.000 claims 1
- RTCILOYBMNRTPU-UHFFFAOYSA-N FC1=C(OC2=C(C(=O)N)C=CC=N2)C=CC(=C1)CC(=O)NC1=NC2=C(N1CCOC)C=C(C=C2)OC Chemical compound FC1=C(OC2=C(C(=O)N)C=CC=N2)C=CC(=C1)CC(=O)NC1=NC2=C(N1CCOC)C=C(C=C2)OC RTCILOYBMNRTPU-UHFFFAOYSA-N 0.000 claims 1
- IFRMGYMBGOCZMW-UHFFFAOYSA-N FC1=C(OC2=C(C(=O)N)C=CC=N2)C=CC(=C1)CC(=O)NC1=NC2=C(N1CCOC)C=CC=C2 Chemical compound FC1=C(OC2=C(C(=O)N)C=CC=N2)C=CC(=C1)CC(=O)NC1=NC2=C(N1CCOC)C=CC=C2 IFRMGYMBGOCZMW-UHFFFAOYSA-N 0.000 claims 1
- CRYOQJHRMIZCTK-UHFFFAOYSA-N FC1=C(OC2=C(C(=O)N)C=CC=N2)C=CC(=C1)CC(=O)NC1=NN2C(C(=CC=C2)F)=N1 Chemical compound FC1=C(OC2=C(C(=O)N)C=CC=N2)C=CC(=C1)CC(=O)NC1=NN2C(C(=CC=C2)F)=N1 CRYOQJHRMIZCTK-UHFFFAOYSA-N 0.000 claims 1
- SIXNHBNYNCBUMX-UHFFFAOYSA-N FC1=C(OC2=C(C(=O)N)C=CC=N2)C=CC(=C1)CC(=O)NC1=NN2C(C=CC(=C2)F)=N1 Chemical compound FC1=C(OC2=C(C(=O)N)C=CC=N2)C=CC(=C1)CC(=O)NC1=NN2C(C=CC(=C2)F)=N1 SIXNHBNYNCBUMX-UHFFFAOYSA-N 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000031481 Pathologic Constriction Diseases 0.000 claims 1
- 208000018262 Peripheral vascular disease Diseases 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 206010047163 Vasospasm Diseases 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 208000026106 cerebrovascular disease Diseases 0.000 claims 1
- 208000029078 coronary artery disease Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 208000002815 pulmonary hypertension Diseases 0.000 claims 1
- 102000000568 rho-Associated Kinases Human genes 0.000 claims 1
- 108010041788 rho-Associated Kinases Proteins 0.000 claims 1
- 210000002460 smooth muscle Anatomy 0.000 claims 1
- 208000037804 stenosis Diseases 0.000 claims 1
- 230000036262 stenosis Effects 0.000 claims 1
- 0 Cc1nnc(*)[s]1 Chemical compound Cc1nnc(*)[s]1 0.000 description 5
- RJOZPHCJUUTZPW-XQRVVYSFSA-N C/C=C\c1c(C=C)[nH]c(C)n1 Chemical compound C/C=C\c1c(C=C)[nH]c(C)n1 RJOZPHCJUUTZPW-XQRVVYSFSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762531624P | 2017-07-12 | 2017-07-12 | |
| US62/531,624 | 2017-07-12 | ||
| PCT/US2018/041559 WO2019014300A1 (en) | 2017-07-12 | 2018-07-11 | PHENYLACETAMIDES AS ROCK INHIBITORS |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020527560A JP2020527560A (ja) | 2020-09-10 |
| JP2020527560A5 true JP2020527560A5 (enExample) | 2021-08-19 |
| JP7206253B2 JP7206253B2 (ja) | 2023-01-17 |
Family
ID=63036481
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020501553A Active JP7206253B2 (ja) | 2017-07-12 | 2018-07-11 | Ｒｏｃｋ阻害剤としてのフェニルアセトアミド |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US11306081B2 (enExample) |
| EP (1) | EP3652164B1 (enExample) |
| JP (1) | JP7206253B2 (enExample) |
| KR (1) | KR102680164B1 (enExample) |
| CN (1) | CN110869360B (enExample) |
| ES (1) | ES2951212T3 (enExample) |
| WO (1) | WO2019014300A1 (enExample) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2821877T3 (es) | 2016-07-07 | 2021-04-28 | Bristol Myers Squibb Co | Espirolactamas como inhibidores de ROCK |
| KR102511441B1 (ko) | 2016-11-30 | 2023-03-16 | 브리스톨-마이어스 스큅 컴퍼니 | 트리시클릭 Rho 키나제 억제제 |
| KR102680160B1 (ko) | 2017-07-12 | 2024-06-28 | 브리스톨-마이어스 스큅 컴퍼니 | 심부전의 치료를 위한 rock의 5원-아미노헤테로사이클 및 5,6- 또는 6,6-원 비시클릭 아미노헤테로시클릭 억제제 |
| JP7313331B2 (ja) | 2017-07-12 | 2023-07-24 | ブリストル－マイヤーズ スクイブ カンパニー | Ｒｏｃｋ阻害剤としてのスピロヘプタニルヒダントイン |
| US12060341B2 (en) | 2017-07-12 | 2024-08-13 | Bristol-Myers Squibb Company | Spiroheptanyl hydantoins as ROCK inhibitors |
| TW201908293A (zh) | 2017-07-12 | 2019-03-01 | 美商必治妥美雅史谷比公司 | 作為rock抑制劑之5員及雙環雜環醯胺 |
| WO2019089868A1 (en) | 2017-11-03 | 2019-05-09 | Bristol-Myers Squibb Company | Diazaspiro rock inhibitors |
| AU2019377087B2 (en) | 2018-11-06 | 2025-03-06 | Cervello Therapeutics, Llc | Rock kinase inhibitors |
| US11248004B2 (en) | 2018-11-06 | 2022-02-15 | Cervello Therapeutics, Llc. | Substituted isoquinolines as rock kinase inhibitors |
| CN114929345B (zh) * | 2019-11-01 | 2024-07-23 | 百时美施贵宝公司 | 作为toll受体抑制剂的经取代的吡唑化合物 |
| WO2023085369A1 (ja) | 2021-11-11 | 2023-05-19 | 学校法人同志社 | 角膜内皮細胞の凍結保存製剤およびその製造法 |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| WO2025034702A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Rmc-6291 for use in the treatment of ras protein-related disease or disorder |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200306819A (en) * | 2002-01-25 | 2003-12-01 | Vertex Pharma | Indazole compounds useful as protein kinase inhibitors |
| EP1558607B1 (en) * | 2002-10-30 | 2010-05-05 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of rock and other protein kinases |
| CA2664335C (en) | 2006-09-20 | 2014-12-02 | Boehringer Ingelheim International Gmbh | Rho kinase inhibitors |
| CL2007003874A1 (es) | 2007-01-03 | 2008-05-16 | Boehringer Ingelheim Int | Compuestos derivados de benzamida; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar enfermedades cardiovasculares, hipertension, aterosclerosis, reestenosis, ictus, insuficiencia cardiaca, lesion isquemica, hipertensio |
| MX2011002825A (es) * | 2008-09-18 | 2011-04-05 | Astellas Pharma Inc | Compuestos heterociclicos de carboxamida. |
| UY33726A (es) | 2010-11-15 | 2012-06-29 | Abbott Lab | Inhibidores de nampt y rock |
| CA2898440A1 (en) | 2013-01-18 | 2014-07-24 | Bristol-Myers Squibb Company | Phthalazinones and isoquinolinones as rock inhibitors |
| AR094929A1 (es) | 2013-02-28 | 2015-09-09 | Bristol Myers Squibb Co | Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2 |
| JP6423372B2 (ja) | 2013-02-28 | 2018-11-14 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | 強力なｒｏｃｋ１およびｒｏｃｋ２阻害剤としてのフェニルピラゾール誘導体 |
| EP3016950B1 (en) | 2013-07-02 | 2017-06-07 | Bristol-Myers Squibb Company | Tricyclic pyrido-carboxamide derivatives as rock inhibitors |
| CN105492444B (zh) | 2013-07-02 | 2018-09-07 | 百时美施贵宝公司 | 作为rock抑制剂的三环吡啶-甲酰胺衍生物 |
| US9902702B2 (en) | 2014-07-15 | 2018-02-27 | Bristol-Myers Squibb Company | Spirocycloheptanes as inhibitors of rock |
| JP6633618B2 (ja) | 2014-08-21 | 2020-01-22 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | 強力なｒｏｃｋ阻害剤としてのタイドバックのベンズアミド誘導体 |
| WO2016112236A1 (en) | 2015-01-09 | 2016-07-14 | Bristol-Myers Squibb Company | Cyclic ureas as inhibitors of rock |
| WO2016144936A1 (en) | 2015-03-09 | 2016-09-15 | Bristol-Myers Squibb Company | Lactams as inhibitors of rock |
| AR107354A1 (es) | 2016-01-13 | 2018-04-18 | Bristol Myers Squibb Co | Salicilamidas espiroheptanos y compuestos relacionados como inhibidores de rock |
| JP6987792B2 (ja) | 2016-05-27 | 2022-01-05 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | Ｒｏｃｋ阻害剤としてのトリアゾロンおよびテトラゾロン |
| ES2829550T3 (es) | 2016-07-07 | 2021-06-01 | Bristol Myers Squibb Co | Ureas cíclicas espiro-condensadas como inhibidores de ROCK |
| CN110049977B (zh) | 2016-07-07 | 2022-01-18 | 百时美施贵宝公司 | 作为强效和选择性rock抑制剂的内酰胺、环状脲和氨基甲酸酯及三唑酮衍生物 |
| ES2821877T3 (es) | 2016-07-07 | 2021-04-28 | Bristol Myers Squibb Co | Espirolactamas como inhibidores de ROCK |
| KR102511441B1 (ko) | 2016-11-30 | 2023-03-16 | 브리스톨-마이어스 스큅 컴퍼니 | 트리시클릭 Rho 키나제 억제제 |
| TW201908293A (zh) | 2017-07-12 | 2019-03-01 | 美商必治妥美雅史谷比公司 | 作為rock抑制劑之5員及雙環雜環醯胺 |
| JP7313331B2 (ja) | 2017-07-12 | 2023-07-24 | ブリストル－マイヤーズ スクイブ カンパニー | Ｒｏｃｋ阻害剤としてのスピロヘプタニルヒダントイン |
| KR102680160B1 (ko) | 2017-07-12 | 2024-06-28 | 브리스톨-마이어스 스큅 컴퍼니 | 심부전의 치료를 위한 rock의 5원-아미노헤테로사이클 및 5,6- 또는 6,6-원 비시클릭 아미노헤테로시클릭 억제제 |
| WO2019089868A1 (en) | 2017-11-03 | 2019-05-09 | Bristol-Myers Squibb Company | Diazaspiro rock inhibitors |
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2018
- 2018-07-11 JP JP2020501553A patent/JP7206253B2/ja active Active
- 2018-07-11 WO PCT/US2018/041559 patent/WO2019014300A1/en not_active Ceased
- 2018-07-11 ES ES18746509T patent/ES2951212T3/es active Active
- 2018-07-11 US US16/629,736 patent/US11306081B2/en active Active
- 2018-07-11 EP EP18746509.1A patent/EP3652164B1/en active Active
- 2018-07-11 KR KR1020207003732A patent/KR102680164B1/ko active Active
- 2018-07-11 CN CN201880045811.XA patent/CN110869360B/zh active Active