JP2019520402A5 - - Google Patents
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- Publication number
- JP2019520402A5 JP2019520402A5 JP2019500450A JP2019500450A JP2019520402A5 JP 2019520402 A5 JP2019520402 A5 JP 2019520402A5 JP 2019500450 A JP2019500450 A JP 2019500450A JP 2019500450 A JP2019500450 A JP 2019500450A JP 2019520402 A5 JP2019520402 A5 JP 2019520402A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- independently
- heterocyclyl
- chr
- 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 95
- 125000000623 heterocyclic group Chemical group 0.000 claims 67
- 229910052799 carbon Inorganic materials 0.000 claims 44
- 229910052739 hydrogen Inorganic materials 0.000 claims 42
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 40
- 229910052794 bromium Inorganic materials 0.000 claims 37
- 229910052801 chlorine Inorganic materials 0.000 claims 37
- 229910052731 fluorine Inorganic materials 0.000 claims 37
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 27
- 229910052757 nitrogen Inorganic materials 0.000 claims 25
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 24
- 125000004452 carbocyclyl group Chemical group 0.000 claims 20
- 125000001072 heteroaryl group Chemical group 0.000 claims 19
- 229910052760 oxygen Inorganic materials 0.000 claims 19
- 125000003118 aryl group Chemical group 0.000 claims 17
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 16
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 claims 13
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 13
- 150000001875 compounds Chemical class 0.000 claims 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 11
- 125000006706 (C3-C6) carbocyclyl group Chemical group 0.000 claims 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- 125000003342 alkenyl group Chemical group 0.000 claims 9
- 125000000304 alkynyl group Chemical group 0.000 claims 9
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 9
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 208000035475 disorder Diseases 0.000 claims 5
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 229940124597 therapeutic agent Drugs 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
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease 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
- 230000001594 aberrant effect Effects 0.000 claims 1
- 239000004480 active ingredient Substances 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
- 238000004519 manufacturing process Methods 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 230000001613 neoplastic effect Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000000069 prophylactic effect 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**1C[U]C(C)=C(C=CC=C)NC1 Chemical compound C**1C[U]C(C)=C(C=CC=C)NC1 0.000 description 5
- GKPXXEFHTFXAFS-PLNGDYQASA-N CC([IH]SC1)=C1/C=C\C=C Chemical compound CC([IH]SC1)=C1/C=C\C=C GKPXXEFHTFXAFS-PLNGDYQASA-N 0.000 description 1
- AOCHNXXMYIQWEH-UHFFFAOYSA-N CC1N=C(C)OC1C Chemical compound CC1N=C(C)OC1C AOCHNXXMYIQWEH-UHFFFAOYSA-N 0.000 description 1
- DSGLHPOHLGFRGQ-SREVYHEPSA-N Cc1c(/C=C\C=C)nc(C)[n]1C Chemical compound Cc1c(/C=C\C=C)nc(C)[n]1C DSGLHPOHLGFRGQ-SREVYHEPSA-N 0.000 description 1
- LQZAPPYGONFIAQ-WAYWQWQTSA-N Cc1c(/C=C\C=C)nc(C)[o]1 Chemical compound Cc1c(/C=C\C=C)nc(C)[o]1 LQZAPPYGONFIAQ-WAYWQWQTSA-N 0.000 description 1
- GAUKCDPSYQUYQL-UHFFFAOYSA-N Cc1n[o]c2ccccc12 Chemical compound Cc1n[o]c2ccccc12 GAUKCDPSYQUYQL-UHFFFAOYSA-N 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021103777A JP7225317B2 (ja) | 2016-07-07 | 2021-06-23 | 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 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662359341P | 2016-07-07 | 2016-07-07 | |
| US62/359,341 | 2016-07-07 | ||
| PCT/US2017/040846 WO2018009622A1 (en) | 2016-07-07 | 2017-07-06 | Lactam, cyclic urea and carbamate, and triazolone derivatives as potent and selective rock inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021103777A Division JP7225317B2 (ja) | 2016-07-07 | 2021-06-23 | 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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019520402A JP2019520402A (ja) | 2019-07-18 |
| JP2019520402A5 true JP2019520402A5 (enExample) | 2020-08-13 |
| JP6903731B2 JP6903731B2 (ja) | 2021-07-14 |
Family
ID=59351142
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019500450A Active JP6903731B2 (ja) | 2016-07-07 | 2017-07-06 | 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 |
| JP2021103777A Active JP7225317B2 (ja) | 2016-07-07 | 2021-06-23 | 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 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021103777A Active JP7225317B2 (ja) | 2016-07-07 | 2021-06-23 | 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 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US10730858B2 (enExample) |
| EP (1) | EP3481816B1 (enExample) |
| JP (2) | JP6903731B2 (enExample) |
| KR (1) | KR102473481B1 (enExample) |
| CN (1) | CN110049977B (enExample) |
| ES (1) | ES2814325T3 (enExample) |
| WO (1) | WO2018009622A1 (enExample) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR107354A1 (es) | 2016-01-13 | 2018-04-18 | Bristol Myers Squibb Co | Salicilamidas espiroheptanos y compuestos relacionados como inhibidores de rock |
| EP3464262B1 (en) | 2016-05-27 | 2020-02-26 | Bristol-Myers Squibb Company | Triazolones and tetrazolones as inhibitors of rock |
| ES2829550T3 (es) | 2016-07-07 | 2021-06-01 | Bristol Myers Squibb Co | Ureas cíclicas espiro-condensadas como inhibidores de ROCK |
| ES2821877T3 (es) | 2016-07-07 | 2021-04-28 | Bristol Myers Squibb Co | Espirolactamas como inhibidores de ROCK |
| CN110023291B (zh) | 2016-11-30 | 2023-07-18 | 百时美施贵宝公司 | 三环rho激酶抑制剂 |
| KR102680164B1 (ko) | 2017-07-12 | 2024-07-01 | 브리스톨-마이어스 스큅 컴퍼니 | Rock 억제제로서의 페닐아세트아미드 |
| 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 |
| KR102644889B1 (ko) | 2017-07-12 | 2024-03-06 | 브리스톨-마이어스 스큅 컴퍼니 | Rock 억제제로서의 스피로헵타닐 히단토인 |
| 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 |
| SI3877364T1 (sl) | 2018-11-06 | 2025-02-28 | Cervello Therapeutics, Llc | Inhibitorji rock kinaze |
| US11248004B2 (en) | 2018-11-06 | 2022-02-15 | Cervello Therapeutics, Llc. | Substituted isoquinolines as rock kinase inhibitors |
| TW202122382A (zh) * | 2019-09-06 | 2021-06-16 | 日商小野藥品工業股份有限公司 | 乙內醯脲衍生物 |
| WO2021257857A1 (en) | 2020-06-19 | 2021-12-23 | Incyte Corporation | Naphthyridinone compounds as jak2 v617f inhibitors |
| WO2021257863A1 (en) | 2020-06-19 | 2021-12-23 | Incyte Corporation | Pyrrolotriazine compounds as jak2 v617f inhibitors |
| US11767323B2 (en) | 2020-07-02 | 2023-09-26 | Incyte Corporation | Tricyclic pyridone compounds as JAK2 V617F inhibitors |
| TW202216713A (zh) | 2020-07-02 | 2022-05-01 | 美商英塞特公司 | 作為ｊａｋ２ ｖ６１７ｆ抑制劑之三環脲化合物 |
| WO2022046989A1 (en) | 2020-08-27 | 2022-03-03 | Incyte Corporation | Tricyclic urea compounds as jak2 v617f inhibitors |
| US11919908B2 (en) | 2020-12-21 | 2024-03-05 | Incyte Corporation | Substituted pyrrolo[2,3-d]pyrimidine compounds as JAK2 V617F inhibitors |
| EP4298099A1 (en) | 2021-02-25 | 2024-01-03 | Incyte Corporation | Spirocyclic lactams as jak2 v617f inhibitors |
| FI4426434T3 (fi) | 2021-11-02 | 2025-11-24 | Flare Therapeutics Inc | Pparg:n käänteisagonisteja ja niiden käyttöjä |
| JPWO2023085369A1 (enExample) | 2021-11-11 | 2023-05-19 | ||
| PE20251706A1 (es) | 2022-03-17 | 2025-07-02 | Incyte Corp | Compuestos de urea triciclica como inhibidores de v617f de jak2 |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| 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 |
| 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 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20080275062A1 (en) | 2004-01-30 | 2008-11-06 | David Harold Drewry | Chemical Compounds |
| JP2008514636A (ja) | 2004-09-28 | 2008-05-08 | アンジオン バイオメディカ コーポレイション | サイトカイン活性の低分子モジュレーター |
| SI2120579T1 (sl) * | 2006-12-28 | 2014-03-31 | Abbvie Inc. | Inhibitorji poli (adp-riboze)polimeraze |
| EA033220B1 (ru) * | 2013-01-18 | 2019-09-30 | Бристол-Майерс Сквибб Компани | Фталазиноны и изохинолиноны в качестве ингибиторов rock |
| WO2014134391A1 (en) | 2013-02-28 | 2014-09-04 | Bristol-Myers Squibb Company | Phenylpyrazole derivatives as potent rock1 and rock2 inhibitors |
| DK2986611T3 (da) | 2013-04-18 | 2019-05-06 | Shanghai Fochon Pharmaceutical Co Ltd | Bestemte proteinkinaseinhibitorer |
| 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 |
| CN105518005B (zh) | 2013-07-02 | 2018-07-20 | 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 |
| ES2838573T3 (es) | 2014-08-21 | 2021-07-02 | Bristol Myers Squibb Co | Derivados de benzamida ligados como inhibidores potentes de ROCK |
| ES2815681T3 (es) | 2015-01-09 | 2021-03-30 | Bristol Myers Squibb Co | Ureas cíclicas como inhibidores de ROCK |
| EP3268360B1 (en) | 2015-03-09 | 2019-04-24 | 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 |
| EP3464262B1 (en) | 2016-05-27 | 2020-02-26 | Bristol-Myers Squibb Company | Triazolones and tetrazolones as inhibitors of rock |
| ES2821877T3 (es) | 2016-07-07 | 2021-04-28 | Bristol Myers Squibb Co | Espirolactamas como inhibidores de ROCK |
| ES2829550T3 (es) | 2016-07-07 | 2021-06-01 | Bristol Myers Squibb Co | Ureas cíclicas espiro-condensadas como inhibidores de ROCK |
| CN110023291B (zh) | 2016-11-30 | 2023-07-18 | 百时美施贵宝公司 | 三环rho激酶抑制剂 |
-
2017
- 2017-07-06 EP EP17740240.1A patent/EP3481816B1/en active Active
- 2017-07-06 CN CN201780054580.4A patent/CN110049977B/zh active Active
- 2017-07-06 WO PCT/US2017/040846 patent/WO2018009622A1/en not_active Ceased
- 2017-07-06 KR KR1020197003126A patent/KR102473481B1/ko active Active
- 2017-07-06 ES ES17740240T patent/ES2814325T3/es active Active
- 2017-07-06 JP JP2019500450A patent/JP6903731B2/ja active Active
- 2017-07-06 US US16/315,674 patent/US10730858B2/en active Active
-
2021
- 2021-06-23 JP JP2021103777A patent/JP7225317B2/ja active Active
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