JP2018501285A5 - - Google Patents
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- Publication number
- JP2018501285A5 JP2018501285A5 JP2017536259A JP2017536259A JP2018501285A5 JP 2018501285 A5 JP2018501285 A5 JP 2018501285A5 JP 2017536259 A JP2017536259 A JP 2017536259A JP 2017536259 A JP2017536259 A JP 2017536259A JP 2018501285 A5 JP2018501285 A5 JP 2018501285A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- independently selected
- heterocyclyl
- independently
- 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 191
- 125000000623 heterocyclic group Chemical group 0.000 claims 84
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 45
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 33
- 229910052757 nitrogen Inorganic materials 0.000 claims 29
- 125000001072 heteroaryl group Chemical group 0.000 claims 24
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 24
- 125000003118 aryl group Chemical group 0.000 claims 19
- 150000003839 salts Chemical class 0.000 claims 19
- 125000004452 carbocyclyl group Chemical group 0.000 claims 17
- 125000000304 alkynyl group Chemical group 0.000 claims 15
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 14
- 125000000753 cycloalkyl group Chemical group 0.000 claims 13
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 13
- 125000006706 (C3-C6) 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 12
- 150000001875 compounds Chemical class 0.000 claims 11
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- -1 substituted Chemical group 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 241000239366 Euphausiacea Species 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N diethylenediamine Natural products C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 2
- 150000004885 piperazines Chemical class 0.000 claims 2
- 206010002383 Angina Pectoris Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 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
- 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
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 208000002815 pulmonary hypertension Diseases 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
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562101434P | 2015-01-09 | 2015-01-09 | |
| US62/101,434 | 2015-01-09 | ||
| PCT/US2016/012560 WO2016112236A1 (en) | 2015-01-09 | 2016-01-08 | Cyclic ureas as inhibitors of rock |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018501285A JP2018501285A (ja) | 2018-01-18 |
| JP2018501285A5 true JP2018501285A5 (OSRAM) | 2019-02-14 |
| JP6779214B2 JP6779214B2 (ja) | 2020-11-04 |
Family
ID=55310909
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017536259A Active JP6779214B2 (ja) | 2015-01-09 | 2016-01-08 | Ｒｏｃｋ阻害剤としての環状ウレア |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US10123993B2 (OSRAM) |
| EP (1) | EP3242873B1 (OSRAM) |
| JP (1) | JP6779214B2 (OSRAM) |
| CN (1) | CN107406426B (OSRAM) |
| AR (1) | AR103990A1 (OSRAM) |
| ES (1) | ES2815681T3 (OSRAM) |
| TW (1) | TW201630899A (OSRAM) |
| WO (1) | WO2016112236A1 (OSRAM) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW201630899A (zh) | 2015-01-09 | 2016-09-01 | 必治妥美雅史谷比公司 | 作為ｒｏｃｋ抑制劑的環狀脲類 |
| TW201706265A (zh) * | 2015-03-09 | 2017-02-16 | 必治妥美雅史谷比公司 | 做為Ｒｈｏ激酶（ＲＯＣＫ）抑制劑之內醯胺 |
| WO2017046739A1 (en) * | 2015-09-15 | 2017-03-23 | Glaxosmithkline Intellectual Property (No.2) Limited | Imidazolidinone derivatives as inhibitors of perk |
| TWI730032B (zh) | 2016-01-13 | 2021-06-11 | 美商必治妥美雅史谷比公司 | 作為ｒｏｃｋ抑制劑之螺庚烷水楊酸醯胺及相關化合物 |
| KR102457933B1 (ko) | 2016-05-27 | 2022-10-24 | 브리스톨-마이어스 스큅 컴퍼니 | Rock의 억제제로서의 트리아졸론 및 테트라졸론 |
| US10787450B2 (en) | 2016-07-07 | 2020-09-29 | Bristol-Myers Squibb Company | Spiro-fused cyclic ureas as inhibitors of rock |
| WO2018009622A1 (en) * | 2016-07-07 | 2018-01-11 | Bristol-Myers Squibb Company | Lactam, cyclic urea and carbamate, and triazolone derivatives as potent and selective rock inhibitors |
| KR102491994B1 (ko) | 2016-07-07 | 2023-01-25 | 브리스톨-마이어스 스큅 컴퍼니 | Rock의 억제제로서의 스피로락탐 |
| KR102511441B1 (ko) * | 2016-11-30 | 2023-03-16 | 브리스톨-마이어스 스큅 컴퍼니 | 트리시클릭 Rho 키나제 억제제 |
| US11306081B2 (en) | 2017-07-12 | 2022-04-19 | Bristol-Myers Squibb Company | Phenylacetamides as inhibitors of rock |
| US11299488B2 (en) | 2017-07-12 | 2022-04-12 | Bristol-Myers Squibb Company | Five membered-aminoheterocycle and 5,6-or 6,6-membered bicyclic aminoheterocyclic inhibitors of rock for the treatment of heart failure |
| 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 |
| KR102644889B1 (ko) | 2017-07-12 | 2024-03-06 | 브리스톨-마이어스 스큅 컴퍼니 | Rock 억제제로서의 스피로헵타닐 히단토인 |
| US11192891B2 (en) | 2017-11-03 | 2021-12-07 | 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 |
| CN112759550A (zh) * | 2019-11-04 | 2021-05-07 | 上海科技大学 | 一种平滑受体拮抗剂 |
| JP2021183586A (ja) * | 2020-05-22 | 2021-12-02 | 武田薬品工業株式会社 | 複素環化合物 |
| CA3238227A1 (en) | 2021-11-11 | 2023-05-19 | The Doshisha | Cryopreservation preparation for corneal endothelial cells and method for producing said cryopreservation preparation |
| 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 |
| 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 |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | Revolution Medicines, Inc. | Ras inhibitors |
| CN120424050A (zh) * | 2024-02-05 | 2025-08-05 | 科辉智药(深圳)新药研究中心有限公司 | 作为sarm1酶活性抑制剂的吡啶类化合物及其应用 |
| 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 (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH07183769A (ja) * | 1993-12-22 | 1995-07-21 | Fuji Electric Co Ltd | ラッチ回路 |
| 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 |
| WO2006048727A1 (en) * | 2004-11-02 | 2006-05-11 | Pfizer Products Inc. | Piperazinylphenalkyl lactam/amine ligands for the 5ht1b receptor |
| US8211919B2 (en) * | 2005-09-02 | 2012-07-03 | Astellas Pharma Inc. | Amide derivatives as rock inhibitors |
| WO2009078992A1 (en) * | 2007-12-17 | 2009-06-25 | Amgen Inc. | Linear tricyclic compounds as p38 kinase inhibitors |
| EP2237852B1 (en) * | 2007-12-17 | 2013-11-20 | Peshina, William F. | Oval cage coupler for filter cages |
| WO2010036316A1 (en) * | 2008-09-24 | 2010-04-01 | Yangbo Feng | Urea and carbamate compounds and analogs as kinase inhibitors |
| WO2012054367A1 (en) * | 2010-10-19 | 2012-04-26 | Boehringer Ingelheim International Gmbh | Rho kinase inhibitors |
| JP6488239B2 (ja) | 2013-01-18 | 2019-03-20 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | Ｒｏｃｋ阻害剤としてのフタラジノンおよびイソキノリノン |
| CN105102448B (zh) * | 2013-02-28 | 2018-03-06 | 百时美施贵宝公司 | 作为rock1和rock2抑制剂的苯基吡唑衍生物 |
| AR094929A1 (es) * | 2013-02-28 | 2015-09-09 | Bristol Myers Squibb Co | Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2 |
| WO2014145022A1 (en) | 2013-03-15 | 2014-09-18 | President And Fellows Of Harvard College | Hybrid necroptosis inhibitors |
| WO2015002926A1 (en) | 2013-07-02 | 2015-01-08 | Bristol-Myers Squibb Company | Tricyclic pyrido-carboxamide derivatives as rock inhibitors |
| AR096788A1 (es) | 2013-07-02 | 2016-02-03 | Bristol Myers Squibb Co | Compuestos tricíclicos de carboxamida como inhibidores potentes de rock |
| WO2015014835A1 (en) | 2013-07-31 | 2015-02-05 | Basf Se | Luminescent diazabenzimidazole carbene metal complexes |
| US9682960B2 (en) | 2013-12-19 | 2017-06-20 | Endorecherche, Inc. | Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety |
| CN106061964B (zh) * | 2014-01-20 | 2019-10-25 | 豪夫迈·罗氏有限公司 | 能够刺激神经发生的n-苯基-内酰胺衍生物及其在神经性病症的治疗中的用途 |
| US9902702B2 (en) | 2014-07-15 | 2018-02-27 | Bristol-Myers Squibb Company | Spirocycloheptanes as inhibitors of rock |
| WO2016028971A1 (en) | 2014-08-21 | 2016-02-25 | Bristol-Myers Squibb Company | Tied-back benzamide derivatives as potent rock inhibitors |
| TW201630899A (zh) | 2015-01-09 | 2016-09-01 | 必治妥美雅史谷比公司 | 作為ｒｏｃｋ抑制劑的環狀脲類 |
| TW201706265A (zh) | 2015-03-09 | 2017-02-16 | 必治妥美雅史谷比公司 | 做為Ｒｈｏ激酶（ＲＯＣＫ）抑制劑之內醯胺 |
| TWI730032B (zh) | 2016-01-13 | 2021-06-11 | 美商必治妥美雅史谷比公司 | 作為ｒｏｃｋ抑制劑之螺庚烷水楊酸醯胺及相關化合物 |
-
2016
- 2016-01-08 TW TW105100631A patent/TW201630899A/zh unknown
- 2016-01-08 CN CN201680012270.1A patent/CN107406426B/zh active Active
- 2016-01-08 AR ARP160100053A patent/AR103990A1/es unknown
- 2016-01-08 EP EP16703378.6A patent/EP3242873B1/en active Active
- 2016-01-08 JP JP2017536259A patent/JP6779214B2/ja active Active
- 2016-01-08 ES ES16703378T patent/ES2815681T3/es active Active
- 2016-01-08 WO PCT/US2016/012560 patent/WO2016112236A1/en not_active Ceased
- 2016-01-08 US US15/541,725 patent/US10123993B2/en active Active
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