JP2019517475A5 - - Google Patents
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- Publication number
- JP2019517475A5 JP2019517475A5 JP2018562088A JP2018562088A JP2019517475A5 JP 2019517475 A5 JP2019517475 A5 JP 2019517475A5 JP 2018562088 A JP2018562088 A JP 2018562088A JP 2018562088 A JP2018562088 A JP 2018562088A JP 2019517475 A5 JP2019517475 A5 JP 2019517475A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- independently selected
- alkyl
- heterocyclyl
- 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 139
- 125000000623 heterocyclic group Chemical group 0.000 claims 72
- 229910052739 hydrogen Inorganic materials 0.000 claims 66
- 229910052799 carbon Inorganic materials 0.000 claims 53
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 29
- 229910052757 nitrogen Inorganic materials 0.000 claims 24
- 125000003118 aryl group Chemical group 0.000 claims 19
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 19
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 17
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 16
- 229910052717 sulfur Inorganic materials 0.000 claims 15
- -1 CN Inorganic materials 0.000 claims 14
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 claims 13
- 150000001875 compounds Chemical class 0.000 claims 13
- 125000001072 heteroaryl group Chemical group 0.000 claims 13
- 150000003839 salts Chemical class 0.000 claims 13
- 125000004452 carbocyclyl group Chemical group 0.000 claims 12
- 229910052760 oxygen Inorganic materials 0.000 claims 11
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- 125000006706 (C3-C6) carbocyclyl group Chemical group 0.000 claims 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 8
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 7
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 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
- 241000239366 Euphausiacea Species 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
- 208000006011 Stroke Diseases 0.000 claims 1
- 206010047163 Vasospasm Diseases 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 125000003277 amino group Chemical group 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
- 230000000694 effects Effects 0.000 claims 1
- 230000003176 fibrotic effect Effects 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 230000002981 neuropathic effect Effects 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 C*C(N1C(*)c2ccccc2)=NN(C(C)=CC=C(C=C)C(c2c(N)[n]cc2)=I[Tl])C1=Cl Chemical compound C*C(N1C(*)c2ccccc2)=NN(C(C)=CC=C(C=C)C(c2c(N)[n]cc2)=I[Tl])C1=Cl 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662342441P | 2016-05-27 | 2016-05-27 | |
| US62/342,441 | 2016-05-27 | ||
| PCT/US2017/034613 WO2017205709A1 (en) | 2016-05-27 | 2017-05-26 | Triazolones and tetrazolones as inhibitors of rock |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019517475A JP2019517475A (ja) | 2019-06-24 |
| JP2019517475A5 true JP2019517475A5 (OSRAM) | 2020-07-02 |
| JP6987792B2 JP6987792B2 (ja) | 2022-01-05 |
Family
ID=59009815
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018562088A Active JP6987792B2 (ja) | 2016-05-27 | 2017-05-26 | Ｒｏｃｋ阻害剤としてのトリアゾロンおよびテトラゾロン |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US10562887B2 (OSRAM) |
| EP (1) | EP3464262B1 (OSRAM) |
| JP (1) | JP6987792B2 (OSRAM) |
| KR (1) | KR102457933B1 (OSRAM) |
| CN (1) | CN109153663B (OSRAM) |
| ES (1) | ES2781309T3 (OSRAM) |
| WO (1) | WO2017205709A1 (OSRAM) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY37073A (es) | 2016-01-13 | 2017-07-31 | Bristol-Myers Squibb Company Una Corporación Del Estado De Delaware | Salicilamidas espiroheptanos y compuestos relacionados como inhibidores de rock, y las composiciones que los contienen |
| JP6903731B2 (ja) | 2016-07-07 | 2021-07-14 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | 強力で選択的なｒｏｃｋ阻害剤としてのラクタム、環状尿素、およびカルバメート、およびトリアゾロン誘導体 |
| JP7113810B2 (ja) | 2016-07-07 | 2022-08-05 | 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ラクタム |
| JP7155102B2 (ja) | 2016-07-07 | 2022-10-18 | 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縮合環尿素 |
| ES2829400T3 (es) | 2016-11-30 | 2021-05-31 | Bristol Myers Squibb Co | Inhibidores tricíclicos de Rho cinasa |
| WO2019014304A1 (en) | 2017-07-12 | 2019-01-17 | Bristol-Myers Squibb Company | SPIROHEPTANYL HYDANTOIDS AS ROCK INHIBITORS |
| ES2894128T3 (es) | 2017-07-12 | 2022-02-11 | Bristol Myers Squibb Co | Inhibidores aminoheterocíclicos de cinco miembros y aminoheterocíclicos bicíclicos de 5,6 o 6,6 miembros de ROCK para el tratamiento de la insuficiencia cardíaca |
| EP3652164B1 (en) | 2017-07-12 | 2023-06-21 | Bristol-Myers Squibb Company | Phenylacetamides as inhibitors of rock |
| 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 |
| US12060341B2 (en) | 2017-07-12 | 2024-08-13 | Bristol-Myers Squibb Company | Spiroheptanyl hydantoins as ROCK inhibitors |
| EP3704121B1 (en) | 2017-11-03 | 2022-12-21 | Bristol-Myers Squibb Company | Diazaspiro rock inhibitors |
| US11034669B2 (en) | 2018-11-30 | 2021-06-15 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| WO2023041422A1 (en) | 2021-09-20 | 2023-03-23 | Basf Se | Heterocyclic compounds for the control of invertebrate pests |
| EP4431596A1 (en) | 2021-11-11 | 2024-09-18 | The Doshisha | Cryopreservation preparation for corneal endothelial cells and method for producing said cryopreservation preparation |
| TW202409023A (zh) | 2022-07-14 | 2024-03-01 | 美商富曼西公司 | 除草苯并𠯤 |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| CN119219603A (zh) * | 2023-06-28 | 2024-12-31 | 科辉智药(深圳)新药研究中心有限公司 | Sarm1酶活性抑制剂及其用途 |
| 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 |
| WO2025076010A1 (en) | 2023-10-01 | 2025-04-10 | Massachusetts Institute Of Technology | Site-selective conjugation of a pharmaceutical agent to an antibody using an affinity peptide |
| TW202530228A (zh) | 2023-10-12 | 2025-08-01 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2025111184A1 (en) | 2023-11-21 | 2025-05-30 | Fmc Corporation | Substituted tetrahydroquinoline and tetrahydroquinoxaline herbicides |
| 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 |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
Family Cites Families (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5747516A (en) | 1993-11-19 | 1998-05-05 | E. I. Du Pont De Nemours And Company | Dihydroazole compounds and their use for controlling fungal plant diseases |
| US20010020100A1 (en) * | 1994-06-14 | 2001-09-06 | G.D. Searle & Co. | N-substituted-1, 2, 4-triazolone compounds for treatment of cardiovascular disorders |
| US5607932A (en) * | 1994-07-12 | 1997-03-04 | Janssen Pharmaceutica N.V. | Heterocyclic derivatives of azolones |
| WO1996025410A1 (en) | 1995-02-17 | 1996-08-22 | Takeda Chemical Industries, Ltd. | Azole compounds, their production and use |
| TW318841B (OSRAM) * | 1995-02-17 | 1997-11-01 | Takeda Pharm Industry Co Ltd | |
| JP3056412B2 (ja) * | 1995-02-17 | 2000-06-26 | 武田薬品工業株式会社 | アゾール化合物およびその用途 |
| JP2771334B2 (ja) | 1995-05-16 | 1998-07-02 | イー・アイ・デユポン・ドウ・ヌムール・アンド・カンパニー | 殺菌・殺カビ性環状アミド類 |
| JP2007519754A (ja) | 2004-01-30 | 2007-07-19 | スミスクライン ビーチャム コーポレーション | 化合物 |
| MXPA06010253A (es) * | 2004-03-10 | 2007-02-16 | Janssen Pharmaceutica Nv | Aril piperidinas o piperazinas sustituidas con heterociclos de cinco miembros inhibidoras de la proteina de transferencia microsomal de trigliceridos. |
| AR049382A1 (es) | 2004-05-18 | 2006-07-26 | Fmc Corp | Derivados de la urea ciclica substituida |
| EP1778676B1 (en) * | 2004-07-16 | 2010-08-25 | Schering Corporation | Hydantoin derivatives for the treatment of inflammatory disorders |
| WO2006048727A1 (en) * | 2004-11-02 | 2006-05-11 | Pfizer Products Inc. | Piperazinylphenalkyl lactam/amine ligands for the 5ht1b receptor |
| CN101084201A (zh) * | 2004-12-21 | 2007-12-05 | 詹森药业有限公司 | 用作α2C－肾上腺素能受体拮抗剂的三唑酮、四唑酮和咪唑酮衍生物 |
| CA2620818A1 (en) * | 2005-09-02 | 2007-03-08 | Astellas Pharma Inc. | Amide derivatives as rock inhibitors |
| PE20140572A1 (es) * | 2008-06-05 | 2014-05-16 | Janssen Pharmaceutica Nv | Combinaciones de drogas que comprenden un inhibidor de dgat y un agonista de ppar |
| WO2010077582A1 (en) * | 2008-12-16 | 2010-07-08 | Merck Sharp & Dohme Corp. | Triazole derivatives for treatment of alzheimer's disease |
| US9409868B2 (en) * | 2012-01-24 | 2016-08-09 | H. Lee Moffin Cancer Center and Research Institute, Inc. | Inhibitors of rho associated protein kinases (ROCK) and methods of use |
| TW201443023A (zh) | 2013-01-18 | 2014-11-16 | 必治妥美雅史谷比公司 | 作爲ｒｏｃｋ抑制劑之酞□酮及異喹啉酮 |
| TW201444798A (zh) * | 2013-02-28 | 2014-12-01 | 必治妥美雅史谷比公司 | 作爲強效ｒｏｃｋ１及ｒｏｃｋ２抑制劑之苯基吡唑衍生物 |
| US9828345B2 (en) * | 2013-02-28 | 2017-11-28 | Bristol-Myers Squibb Company | Phenylpyrazole derivatives as potent ROCK1 and ROCK2 inhibitors |
| WO2015002926A1 (en) | 2013-07-02 | 2015-01-08 | Bristol-Myers Squibb Company | Tricyclic pyrido-carboxamide derivatives as rock inhibitors |
| TW201506024A (zh) | 2013-07-02 | 2015-02-16 | 必治妥美雅史谷比公司 | 作為有效ｒｏｃｋ抑制劑的三環甲醯胺衍生物 |
| CA2935270A1 (en) | 2014-01-20 | 2015-07-23 | F. Hoffmann-La Roche Ag | N-phenyl-lactam derivatives capable of stimulating neurogenesis and their use in the treatment of neurological disorders |
| 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 |
| CN107406426B (zh) * | 2015-01-09 | 2020-11-20 | 百时美施贵宝公司 | 作为rock抑制剂的环状脲类 |
| EP3268360B1 (en) | 2015-03-09 | 2019-04-24 | Bristol-Myers Squibb Company | Lactams as inhibitors of rock |
| UY37073A (es) | 2016-01-13 | 2017-07-31 | Bristol-Myers Squibb Company Una Corporación Del Estado De Delaware | Salicilamidas espiroheptanos y compuestos relacionados como inhibidores de rock, y las composiciones que los contienen |
| JP7113810B2 (ja) | 2016-07-07 | 2022-08-05 | 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ラクタム |
| JP6903731B2 (ja) | 2016-07-07 | 2021-07-14 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | 強力で選択的なｒｏｃｋ阻害剤としてのラクタム、環状尿素、およびカルバメート、およびトリアゾロン誘導体 |
| JP7155102B2 (ja) | 2016-07-07 | 2022-10-18 | 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縮合環尿素 |
| ES2829400T3 (es) | 2016-11-30 | 2021-05-31 | Bristol Myers Squibb Co | Inhibidores tricíclicos de Rho cinasa |
-
2017
- 2017-05-26 US US16/098,978 patent/US10562887B2/en active Active
- 2017-05-26 KR KR1020187037221A patent/KR102457933B1/ko active Active
- 2017-05-26 WO PCT/US2017/034613 patent/WO2017205709A1/en not_active Ceased
- 2017-05-26 CN CN201780031569.6A patent/CN109153663B/zh active Active
- 2017-05-26 JP JP2018562088A patent/JP6987792B2/ja active Active
- 2017-05-26 EP EP17728029.4A patent/EP3464262B1/en active Active
- 2017-05-26 ES ES17728029T patent/ES2781309T3/es active Active
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