JP2019520398A5 - - Google Patents
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- JP2019520398A5 JP2019520398A5 JP2019500399A JP2019500399A JP2019520398A5 JP 2019520398 A5 JP2019520398 A5 JP 2019520398A5 JP 2019500399 A JP2019500399 A JP 2019500399A JP 2019500399 A JP2019500399 A JP 2019500399A JP 2019520398 A5 JP2019520398 A5 JP 2019520398A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- independently
- heterocyclyl
- independently selected
- 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 113
- 229910052739 hydrogen Inorganic materials 0.000 claims 49
- 229910052799 carbon Inorganic materials 0.000 claims 45
- 125000000623 heterocyclic group Chemical group 0.000 claims 41
- 229910052801 chlorine Inorganic materials 0.000 claims 35
- 229910052731 fluorine Inorganic materials 0.000 claims 35
- 229910052794 bromium Inorganic materials 0.000 claims 26
- 229910052757 nitrogen Inorganic materials 0.000 claims 25
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 13
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 13
- 125000004452 carbocyclyl group Chemical group 0.000 claims 12
- 229910052760 oxygen Inorganic materials 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 11
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 8
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 208000035475 disorder Diseases 0.000 claims 5
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 4
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000006706 (C3-C6) carbocyclyl group Chemical group 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 229910052717 sulfur Inorganic materials 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
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000002618 bicyclic heterocycle 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
- 239000003814 drug 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
- 125000005842 heteroatom Chemical group 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
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 0 *C(CN(C1=[C-])c(cc2)ncc2-c2c[n]nc2)C11N(*)c2ccccc2C1 Chemical compound *C(CN(C1=[C-])c(cc2)ncc2-c2c[n]nc2)C11N(*)c2ccccc2C1 0.000 description 14
- LNLXLSVOKURPPO-UHFFFAOYSA-N C/C(/N=C\N)=C/[Tl] Chemical compound C/C(/N=C\N)=C/[Tl] LNLXLSVOKURPPO-UHFFFAOYSA-N 0.000 description 1
- MJKPRSUXOAIASR-HYXAFXHYSA-N C/C=C(/C)\N=C/N Chemical compound C/C=C(/C)\N=C/N MJKPRSUXOAIASR-HYXAFXHYSA-N 0.000 description 1
- JTQKPDUJCGDXER-DAXSKMNVSA-N CC(/C=N\NC)=C Chemical compound CC(/C=N\NC)=C JTQKPDUJCGDXER-DAXSKMNVSA-N 0.000 description 1
- FKNQCJSGGFJEIZ-UHFFFAOYSA-N Cc1ccncc1 Chemical compound Cc1ccncc1 FKNQCJSGGFJEIZ-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662359354P | 2016-07-07 | 2016-07-07 | |
| US62/359,354 | 2016-07-07 | ||
| PCT/US2017/040850 WO2018009625A1 (en) | 2016-07-07 | 2017-07-06 | Spirolactams as inhibitors of rock |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2019520398A JP2019520398A (ja) | 2019-07-18 |
| JP2019520398A5 true JP2019520398A5 (OSRAM) | 2020-08-13 |
| JPWO2018009625A5 JPWO2018009625A5 (OSRAM) | 2022-03-15 |
| JP7113810B2 JP7113810B2 (ja) | 2022-08-05 |
Family
ID=59351143
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019500399A Active JP7113810B2 (ja) | 2016-07-07 | 2017-07-06 | Ｒｏｃｋ阻害剤としてのスピロラクタム |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US10696674B2 (OSRAM) |
| EP (1) | EP3481817B1 (OSRAM) |
| JP (1) | JP7113810B2 (OSRAM) |
| KR (1) | KR102491994B1 (OSRAM) |
| CN (1) | CN109689639B (OSRAM) |
| ES (1) | ES2821877T3 (OSRAM) |
| WO (1) | WO2018009625A1 (OSRAM) |
Families Citing this family (22)
| 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 |
| US10562887B2 (en) | 2016-05-27 | 2020-02-18 | Bristol-Myers Squibb Company | Triazolones and tetrazolones as inhibitors of ROCK |
| 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 |
| 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 |
| ES2829400T3 (es) | 2016-11-30 | 2021-05-31 | Bristol Myers Squibb Co | Inhibidores tricíclicos de Rho cinasa |
| 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 |
| 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 |
| EP3704121B1 (en) * | 2017-11-03 | 2022-12-21 | Bristol-Myers Squibb Company | Diazaspiro rock inhibitors |
| TWI833819B (zh) | 2018-10-05 | 2024-03-01 | 美商安尼波那生物公司 | 用於治療與apj受體活性相關的病狀的化合物及組成物 |
| US11248004B2 (en) | 2018-11-06 | 2022-02-15 | Cervello Therapeutics, Llc. | Substituted isoquinolines as rock kinase inhibitors |
| KR102882224B1 (ko) | 2018-11-06 | 2025-11-05 | 써벨로 테라퓨틱스, 엘엘씨 | Rock 키나아제 저해제 |
| EP3902805A4 (en) | 2018-12-28 | 2023-03-01 | SPV Therapeutics Inc. | CYCLINE-DEPENDENT KINASE INHIBITORS |
| EP4431596A1 (en) | 2021-11-11 | 2024-09-18 | The Doshisha | Cryopreservation preparation for corneal endothelial cells and method for producing said cryopreservation preparation |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| 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 |
| TW202530228A (zh) | 2023-10-12 | 2025-08-01 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| 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 (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1997023212A1 (en) | 1995-12-21 | 1997-07-03 | The Du Pont Merck Pharmaceutical Company | ISOXAZOLINE, ISOTHIAZOLINE AND PYRAZOLINE FACTOR Xa INHIBITORS |
| ES2232292B1 (es) | 2003-07-30 | 2006-11-01 | Laboratorios Del Dr. Esteve, S.A. | Compuestos sulfonamidicos derivados de benzoxazinona, su preparacion y uso como medicamentos. |
| ES2228267B1 (es) | 2003-07-30 | 2006-07-01 | Laboratorios Del Dr. Esteve, S.A. | Combinacion de sustancias activas conteniendo al menos un compuesto con afinidad por el receptor del neuropeptido y (npy) y al menos un compuesto con afinidad por el receptor 5-ht6. |
| 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 |
| WO2008096746A1 (ja) | 2007-02-06 | 2008-08-14 | Takeda Pharmaceutical Company Limited | スピロ化合物およびその用途 |
| WO2009133861A1 (ja) | 2008-04-28 | 2009-11-05 | 武田薬品工業株式会社 | 環状アミン化合物 |
| 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 |
| US9828345B2 (en) * | 2013-02-28 | 2017-11-28 | Bristol-Myers Squibb Company | Phenylpyrazole derivatives as potent ROCK1 and ROCK2 inhibitors |
| 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 |
| 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 |
| WO2015002926A1 (en) | 2013-07-02 | 2015-01-08 | Bristol-Myers Squibb Company | Tricyclic pyrido-carboxamide derivatives as rock inhibitors |
| 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 |
| WO2016065582A1 (en) * | 2014-10-30 | 2016-05-06 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| 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 |
| US10562887B2 (en) | 2016-05-27 | 2020-02-18 | Bristol-Myers Squibb Company | Triazolones and tetrazolones as inhibitors of ROCK |
| 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 |
| 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 |
| ES2829400T3 (es) | 2016-11-30 | 2021-05-31 | Bristol Myers Squibb Co | Inhibidores tricíclicos de Rho cinasa |
| 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 |
| WO2019014304A1 (en) | 2017-07-12 | 2019-01-17 | Bristol-Myers Squibb Company | SPIROHEPTANYL HYDANTOIDS AS ROCK INHIBITORS |
| 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 |
| EP3704121B1 (en) | 2017-11-03 | 2022-12-21 | Bristol-Myers Squibb Company | Diazaspiro rock inhibitors |
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2017
- 2017-07-06 JP JP2019500399A patent/JP7113810B2/ja active Active
- 2017-07-06 KR KR1020197003127A patent/KR102491994B1/ko active Active
- 2017-07-06 CN CN201780054599.9A patent/CN109689639B/zh active Active
- 2017-07-06 US US16/315,678 patent/US10696674B2/en active Active
- 2017-07-06 ES ES17740241T patent/ES2821877T3/es active Active
- 2017-07-06 WO PCT/US2017/040850 patent/WO2018009625A1/en not_active Ceased
- 2017-07-06 EP EP17740241.9A patent/EP3481817B1/en active Active