JP2014512406A5 - - Google Patents
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- Publication number
- JP2014512406A5 JP2014512406A5 JP2014506888A JP2014506888A JP2014512406A5 JP 2014512406 A5 JP2014512406 A5 JP 2014512406A5 JP 2014506888 A JP2014506888 A JP 2014506888A JP 2014506888 A JP2014506888 A JP 2014506888A JP 2014512406 A5 JP2014512406 A5 JP 2014512406A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- het
- group
- aryl
- heteroaryl
- 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.)
- Ceased
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- 125000000217 alkyl group Chemical group 0.000 claims 81
- 125000003118 aryl group Chemical group 0.000 claims 53
- 125000001072 heteroaryl group Chemical group 0.000 claims 44
- 150000001875 compounds Chemical class 0.000 claims 31
- 125000001424 substituent group Chemical group 0.000 claims 24
- 239000003814 drug Substances 0.000 claims 20
- 125000000623 heterocyclic group Chemical group 0.000 claims 17
- 239000001257 hydrogen Substances 0.000 claims 17
- 229910052739 hydrogen Inorganic materials 0.000 claims 17
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 14
- 229940124597 therapeutic agent Drugs 0.000 claims 14
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 13
- 230000002265 prevention Effects 0.000 claims 11
- 230000000069 prophylactic effect Effects 0.000 claims 11
- 201000010099 disease Diseases 0.000 claims 10
- 125000001475 halogen functional group Chemical group 0.000 claims 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
- 125000003545 alkoxy group Chemical group 0.000 claims 8
- 125000000304 alkynyl group Chemical group 0.000 claims 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 8
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 239000001301 oxygen Substances 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 125000006647 (C3-C15) cycloalkyl group Chemical group 0.000 claims 5
- 206010020649 Hyperkeratosis Diseases 0.000 claims 5
- 201000001880 Sexual dysfunction Diseases 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 5
- 208000030533 eye disease Diseases 0.000 claims 5
- 231100000872 sexual dysfunction Toxicity 0.000 claims 5
- 206010006458 Bronchitis chronic Diseases 0.000 claims 4
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 4
- 208000010412 Glaucoma Diseases 0.000 claims 4
- 206010020772 Hypertension Diseases 0.000 claims 4
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 4
- 208000025865 Ulcer Diseases 0.000 claims 4
- 125000003282 alkyl amino group Chemical group 0.000 claims 4
- 208000006673 asthma Diseases 0.000 claims 4
- 206010006451 bronchitis Diseases 0.000 claims 4
- 208000007451 chronic bronchitis Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 229940079593 drug Drugs 0.000 claims 4
- 125000001188 haloalkyl group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 208000028774 intestinal disease Diseases 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 125000000168 pyrrolyl group Chemical group 0.000 claims 4
- 206010039083 rhinitis Diseases 0.000 claims 4
- 208000017520 skin disease Diseases 0.000 claims 4
- 125000003107 substituted aryl group Chemical group 0.000 claims 4
- 230000008719 thickening Effects 0.000 claims 4
- 125000001544 thienyl group Chemical group 0.000 claims 4
- 208000026533 urinary bladder disease Diseases 0.000 claims 4
- 206010016654 Fibrosis Diseases 0.000 claims 3
- 208000001126 Keratosis Diseases 0.000 claims 3
- 208000029162 bladder disease Diseases 0.000 claims 3
- 230000004761 fibrosis Effects 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- -1 nitro, amino Chemical group 0.000 claims 3
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 2
- 208000019901 Anxiety disease Diseases 0.000 claims 2
- 206010003011 Appendicitis Diseases 0.000 claims 2
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 2
- 208000020084 Bone disease Diseases 0.000 claims 2
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 2
- 206010010904 Convulsion Diseases 0.000 claims 2
- 208000011231 Crohn disease Diseases 0.000 claims 2
- 201000003883 Cystic fibrosis Diseases 0.000 claims 2
- 206010014561 Emphysema Diseases 0.000 claims 2
- 208000010228 Erectile Dysfunction Diseases 0.000 claims 2
- 208000005577 Gastroenteritis Diseases 0.000 claims 2
- 206010020751 Hypersensitivity Diseases 0.000 claims 2
- 206010058359 Hypogonadism Diseases 0.000 claims 2
- 241001465754 Metazoa Species 0.000 claims 2
- 206010061323 Optic neuropathy Diseases 0.000 claims 2
- 206010035664 Pneumonia Diseases 0.000 claims 2
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 2
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 2
- 208000018569 Respiratory Tract disease Diseases 0.000 claims 2
- 208000017442 Retinal disease Diseases 0.000 claims 2
- 208000007014 Retinitis pigmentosa Diseases 0.000 claims 2
- 206010038923 Retinopathy Diseases 0.000 claims 2
- 206010052779 Transplant rejections Diseases 0.000 claims 2
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 2
- 230000002159 abnormal effect Effects 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 2
- 125000004442 acylamino group Chemical group 0.000 claims 2
- 125000005907 alkyl ester group Chemical group 0.000 claims 2
- 125000004414 alkyl thio group Chemical group 0.000 claims 2
- 230000036506 anxiety Effects 0.000 claims 2
- 239000004202 carbamide Substances 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 201000009151 chronic rhinitis Diseases 0.000 claims 2
- 206010009887 colitis Diseases 0.000 claims 2
- 230000036461 convulsion Effects 0.000 claims 2
- MOXUSPIFBCWPHJ-UHFFFAOYSA-N diazidoamine Chemical compound [N-]=[N+]=NNN=[N+]=[N-] MOXUSPIFBCWPHJ-UHFFFAOYSA-N 0.000 claims 2
- 230000002526 effect on cardiovascular system Effects 0.000 claims 2
- 210000002615 epidermis Anatomy 0.000 claims 2
- AEOCXXJPGCBFJA-UHFFFAOYSA-N ethionamide Chemical compound CCC1=CC(C(N)=S)=CC=N1 AEOCXXJPGCBFJA-UHFFFAOYSA-N 0.000 claims 2
- 239000008187 granular material Substances 0.000 claims 2
- 125000000717 hydrazino group Chemical group [H]N([*])N([H])[H] 0.000 claims 2
- 208000009326 ileitis Diseases 0.000 claims 2
- 201000001881 impotence Diseases 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 208000003243 intestinal obstruction Diseases 0.000 claims 2
- 208000017169 kidney disease Diseases 0.000 claims 2
- 208000002780 macular degeneration Diseases 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 230000000414 obstructive effect Effects 0.000 claims 2
- 208000020911 optic nerve disease Diseases 0.000 claims 2
- 150000002923 oximes Chemical class 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 2
- 208000023504 respiratory system disease Diseases 0.000 claims 2
- 230000002207 retinal effect Effects 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 238000001356 surgical procedure Methods 0.000 claims 2
- 150000003573 thiols Chemical class 0.000 claims 2
- 206010044008 tonsillitis Diseases 0.000 claims 2
- 208000004371 toothache Diseases 0.000 claims 2
- 231100000397 ulcer Toxicity 0.000 claims 2
- 230000036269 ulceration Effects 0.000 claims 2
- 208000019553 vascular disease Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 208000022873 Ocular disease Diseases 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 230000007815 allergy Effects 0.000 claims 1
- GOPDFXUMARJJEA-UHFFFAOYSA-N amino(nitro)azanide Chemical compound N[N-][N+]([O-])=O GOPDFXUMARJJEA-UHFFFAOYSA-N 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 230000005549 barrier dysfunction Effects 0.000 claims 1
- 230000003915 cell function Effects 0.000 claims 1
- 230000004663 cell proliferation Effects 0.000 claims 1
- 208000015114 central nervous system disease Diseases 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 230000006378 damage Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 230000009610 hypersensitivity Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 230000000926 neurological effect Effects 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
- 208000002815 pulmonary hypertension Diseases 0.000 claims 1
- 238000007634 remodeling Methods 0.000 claims 1
- 239000011435 rock Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 210000000329 smooth muscle myocyte Anatomy 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 229940124530 sulfonamide Drugs 0.000 claims 1
- 150000003456 sulfonamides Chemical class 0.000 claims 1
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 claims 1
- 0 Cc1c2C(*)=CCC(*)=Cc2ccc1 Chemical compound Cc1c2C(*)=CCC(*)=Cc2ccc1 0.000 description 5
- RUOJZAUFBMNUDX-UHFFFAOYSA-N CC(CO1)OC1=O Chemical compound CC(CO1)OC1=O RUOJZAUFBMNUDX-UHFFFAOYSA-N 0.000 description 1
- HORRIHWEYDDYST-UHFFFAOYSA-N Nc(cc1)cc2c1[nH]nc2I Chemical compound Nc(cc1)cc2c1[nH]nc2I HORRIHWEYDDYST-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1107223.8A GB201107223D0 (en) | 2011-04-29 | 2011-04-29 | Novel rock inhibitors |
| GB1107223.8 | 2011-04-29 | ||
| PCT/EP2012/057785 WO2012146724A2 (en) | 2011-04-29 | 2012-04-27 | Novel rock inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014512406A JP2014512406A (ja) | 2014-05-22 |
| JP2014512406A5 true JP2014512406A5 (https=) | 2015-04-23 |
Family
ID=44202979
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014506888A Ceased JP2014512406A (ja) | 2011-04-29 | 2012-04-27 | 新規のｒｏｃｋ阻害剤 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US9073905B2 (https=) |
| EP (1) | EP2702053A2 (https=) |
| JP (1) | JP2014512406A (https=) |
| CN (1) | CN103534249A (https=) |
| AU (1) | AU2012247455A1 (https=) |
| BR (1) | BR112013027241A2 (https=) |
| CA (1) | CA2834387A1 (https=) |
| EA (1) | EA201370230A1 (https=) |
| GB (1) | GB201107223D0 (https=) |
| MX (1) | MX2013012555A (https=) |
| NZ (1) | NZ616300A (https=) |
| WO (1) | WO2012146724A2 (https=) |
| ZA (1) | ZA201307496B (https=) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113620933A (zh) | 2012-10-05 | 2021-11-09 | 卡德门企业有限公司 | Rho激酶抑制剂 |
| SG11201503134WA (en) * | 2012-10-31 | 2015-05-28 | Amakem Nv | Novel rock inhibitors |
| AR094929A1 (es) | 2013-02-28 | 2015-09-09 | Bristol Myers Squibb Co | Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2 |
| WO2014134391A1 (en) | 2013-02-28 | 2014-09-04 | Bristol-Myers Squibb Company | Phenylpyrazole derivatives as potent rock1 and rock2 inhibitors |
| CN103127249A (zh) * | 2013-03-02 | 2013-06-05 | 谭习达 | 一种治阑尾炎的药 |
| US20170114323A1 (en) | 2014-06-19 | 2017-04-27 | Whitehead Institute For Biomedical Research | Uses of kinase inhibitors for inducing and maintaining pluripotency |
| CN112969694B (zh) * | 2018-11-09 | 2023-06-13 | 北京泰德制药股份有限公司 | Rho相关蛋白激酶抑制剂、包含其的药物组合物及其用途 |
| KR102819334B1 (ko) * | 2019-06-21 | 2025-06-10 | 광저우 오쿠순 옵탈믹 바이오테크놀로지 캄파니 리미티드 | Rock단백질 키나아제 억제제인 이소퀴놀리논의 유도체 및 그 응용 |
| US12371667B2 (en) | 2021-05-13 | 2025-07-29 | Washington University | Enhanced methods for inducing and maintaining naive human pluripotent stem cells |
| EP4431596A4 (en) | 2021-11-11 | 2026-01-14 | The Doshisha | CRYOCONSERVATION PREPARATION FOR CORNIAL ENDOTHELIAL CELLS AND PROCESS FOR PRODUCING SAID CRYOCONSERVATION PREPARATION |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| IL326136A (en) | 2023-08-07 | 2026-03-01 | Revolution Medicines Inc | RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | 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 |
| US20250375445A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| CN118304286B (zh) * | 2024-06-07 | 2024-09-10 | 四川省医学科学院·四川省人民医院 | 芥子碱硫氰酸盐在制备治疗视网膜新生血管相关疾病的药物中的应用 |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
Family Cites Families (15)
| 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 |
| 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 |
| US7217722B2 (en) | 2000-02-01 | 2007-05-15 | Kirin Beer Kabushiki Kaisha | Nitrogen-containing compounds having kinase inhibitory activity and drugs containing the same |
| ATE478865T1 (de) * | 2006-05-12 | 2010-09-15 | Vertex Pharma | Selektive rock-proteinkinasehemmer und ihre verwendung |
| WO2008049919A2 (en) * | 2006-10-26 | 2008-05-02 | Devgen N.V. | Rho kinase inhibitors |
| US20100022517A1 (en) | 2006-12-18 | 2010-01-28 | Richards Lori A | Ophthalmic formulation of rho kinase inhibitor compound |
| US8071779B2 (en) * | 2006-12-18 | 2011-12-06 | Inspire Pharmaceuticals, Inc. | Cytoskeletal active rho kinase inhibitor compounds, composition and use |
| US20090325959A1 (en) | 2008-06-26 | 2009-12-31 | Vittitow Jason L | Method for treating ophthalmic diseases using rho kinase inhibitor compounds |
| US20090325960A1 (en) | 2008-06-26 | 2009-12-31 | Fulcher Emilee H | Method for treating inflammatory diseases using rho kinase inhibitor compounds |
| EP2317849A4 (en) | 2008-06-26 | 2011-11-02 | Inspire Pharmaceuticals Inc | PROCESS FOR THE TREATMENT OF LUNG DISEASES WITH RHO KINASE INHIBITOR COMPOUNDS |
| US20100204210A1 (en) | 2008-12-04 | 2010-08-12 | Scott Sorensen | Method for treating pulmonary diseases using rho kinase inhibitor compounds |
| CA2781390A1 (en) * | 2009-12-14 | 2011-06-23 | Inspire Pharmaceuticals, Inc. | Bridged bicyclic rho kinase inhibitor compounds, composition and use |
| KR20130095263A (ko) * | 2010-07-27 | 2013-08-27 | 인스파이어 파마슈티컬스 인코퍼레이티드 | 전구약물 형태의 키나아제 저해제 화합물을 사용하여 안질환을 치료하는 방법 |
-
2011
- 2011-04-29 GB GBGB1107223.8A patent/GB201107223D0/en not_active Ceased
-
2012
- 2012-04-27 WO PCT/EP2012/057785 patent/WO2012146724A2/en not_active Ceased
- 2012-04-27 EA EA201370230A patent/EA201370230A1/ru unknown
- 2012-04-27 MX MX2013012555A patent/MX2013012555A/es unknown
- 2012-04-27 NZ NZ616300A patent/NZ616300A/en not_active IP Right Cessation
- 2012-04-27 EP EP12719645.9A patent/EP2702053A2/en not_active Withdrawn
- 2012-04-27 US US14/113,941 patent/US9073905B2/en not_active Expired - Fee Related
- 2012-04-27 CA CA2834387A patent/CA2834387A1/en active Pending
- 2012-04-27 BR BR112013027241A patent/BR112013027241A2/pt not_active IP Right Cessation
- 2012-04-27 AU AU2012247455A patent/AU2012247455A1/en not_active Abandoned
- 2012-04-27 CN CN201280020905.4A patent/CN103534249A/zh active Pending
- 2012-04-27 JP JP2014506888A patent/JP2014512406A/ja not_active Ceased
-
2013
- 2013-10-08 ZA ZA2013/07496A patent/ZA201307496B/en unknown
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