KR102473481B1 - 강력하고 선택적인 rock 억제제로서의 락탐, 시클릭 우레아 및 카르바메이트, 및 트리아졸론 유도체 - Google Patents
강력하고 선택적인 rock 억제제로서의 락탐, 시클릭 우레아 및 카르바메이트, 및 트리아졸론 유도체 Download PDFInfo
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- KR102473481B1 KR102473481B1 KR1020197003126A KR20197003126A KR102473481B1 KR 102473481 B1 KR102473481 B1 KR 102473481B1 KR 1020197003126 A KR1020197003126 A KR 1020197003126A KR 20197003126 A KR20197003126 A KR 20197003126A KR 102473481 B1 KR102473481 B1 KR 102473481B1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/08—Vasodilators for multiple indications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Immunology (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Transplantation (AREA)
- Physical Education & Sports Medicine (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Neurosurgery (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Pyridine Compounds (AREA)
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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20190025960A KR20190025960A (ko) | 2019-03-12 |
| KR102473481B1 true KR102473481B1 (ko) | 2022-12-01 |
Family
ID=59351142
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020197003126A Active KR102473481B1 (ko) | 2016-07-07 | 2017-07-06 | 강력하고 선택적인 rock 억제제로서의 락탐, 시클릭 우레아 및 카르바메이트, 및 트리아졸론 유도체 |
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 (30)
| 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 |
| WO2017205709A1 (en) | 2016-05-27 | 2017-11-30 | 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 |
| WO2018009625A1 (en) | 2016-07-07 | 2018-01-11 | Bristol-Myers Squibb Company | Spirolactams as inhibitors of rock |
| ES2829400T3 (es) | 2016-11-30 | 2021-05-31 | Bristol Myers Squibb Co | Inhibidores tricíclicos de Rho cinasa |
| US12060341B2 (en) | 2017-07-12 | 2024-08-13 | Bristol-Myers Squibb Company | Spiroheptanyl hydantoins as ROCK inhibitors |
| WO2019014300A1 (en) | 2017-07-12 | 2019-01-17 | Bristol-Myers Squibb Company | PHENYLACETAMIDES AS ROCK INHIBITORS |
| 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 |
| CN110914257B (zh) | 2017-07-12 | 2023-05-26 | 百时美施贵宝公司 | 作为rock抑制剂的螺庚基乙内酰脲 |
| KR102680160B1 (ko) | 2017-07-12 | 2024-06-28 | 브리스톨-마이어스 스큅 컴퍼니 | 심부전의 치료를 위한 rock의 5원-아미노헤테로사이클 및 5,6- 또는 6,6-원 비시클릭 아미노헤테로시클릭 억제제 |
| CN111278825B (zh) | 2017-11-03 | 2023-05-02 | 百时美施贵宝公司 | 二氮杂螺rock抑制剂 |
| EA202191164A1 (ru) | 2018-11-06 | 2022-01-24 | Сервелло Терапьютикс, Ллк | Ингибиторы rock-киназы |
| US11248004B2 (en) | 2018-11-06 | 2022-02-15 | Cervello Therapeutics, Llc. | Substituted isoquinolines as rock kinase inhibitors |
| WO2021043245A1 (en) * | 2019-09-06 | 2021-03-11 | Ono Pharmaceutical Co., Ltd. | Hydantoin derivative |
| US11691971B2 (en) | 2020-06-19 | 2023-07-04 | Incyte Corporation | Naphthyridinone compounds as JAK2 V617F inhibitors |
| US11753413B2 (en) | 2020-06-19 | 2023-09-12 | Incyte Corporation | Substituted pyrrolo[2,1-f][1,2,4]triazine compounds as JAK2 V617F inhibitors |
| RS66978B1 (sr) | 2020-07-02 | 2025-07-31 | Incyte Corp | Triciklična jedinjenja uree kao inhibitori jak2 v617f |
| WO2022006456A1 (en) | 2020-07-02 | 2022-01-06 | Incyte Corporation | Tricyclic pyridone compounds as jak2 v617f inhibitors |
| US11661422B2 (en) | 2020-08-27 | 2023-05-30 | 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 |
| WO2022182839A1 (en) | 2021-02-25 | 2022-09-01 | Incyte Corporation | Spirocyclic lactams as jak2 v617f inhibitors |
| KR20240144096A (ko) | 2021-11-02 | 2024-10-02 | 플레어 테라퓨틱스 인크. | Pparg 역 효능제 및 그의 용도 |
| US20250000083A1 (en) | 2021-11-11 | 2025-01-02 | The Doshisha | Cryopreservation preparation for corneal endothelial cells and method for producing said cryopreservation preparation |
| KR20240163688A (ko) | 2022-03-17 | 2024-11-19 | 인사이트 코포레이션 | Jak2 v617f 억제제로서의 삼환계 우레아 화합물 |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | 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 |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20140206686A1 (en) | 2013-01-18 | 2014-07-24 | Bristol-Myers Squibb Company | Phthalazinones and isoquinolinones as rock inhibitors |
| WO2016010950A1 (en) | 2014-07-15 | 2016-01-21 | Bristol-Myers Squibb Company | Spirocycloheptanes as inhibitors of rock |
| WO2016112236A1 (en) | 2015-01-09 | 2016-07-14 | Bristol-Myers Squibb Company | Cyclic ureas as inhibitors of rock |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1713775A4 (en) | 2004-01-30 | 2009-08-12 | Smithkline Beecham Corp | CHEMICAL COMPOUNDS |
| US7648978B2 (en) | 2004-09-28 | 2010-01-19 | Angion Biomedica Corp. | Small molecule modulators of cytokine activity |
| SI2698062T1 (sl) * | 2006-12-28 | 2015-12-31 | Abbvie Inc. | Inhibitorji poli (ADP-riboza) polimeraze |
| US9828345B2 (en) | 2013-02-28 | 2017-11-28 | Bristol-Myers Squibb Company | Phenylpyrazole derivatives as potent ROCK1 and ROCK2 inhibitors |
| CN106905316B (zh) | 2013-04-18 | 2021-06-01 | 上海复尚慧创医药研究有限公司 | 蛋白激酶抑制剂 |
| 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 |
| CN105492444B (zh) | 2013-07-02 | 2018-09-07 | 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 |
| CN107108581B (zh) | 2014-08-21 | 2020-06-23 | 百时美施贵宝公司 | 作为强效rock抑制剂的回接苯甲酰胺衍生物 |
| US10112929B2 (en) | 2015-03-09 | 2018-10-30 | 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 |
| WO2017205709A1 (en) | 2016-05-27 | 2017-11-30 | Bristol-Myers Squibb Company | Triazolones and tetrazolones as inhibitors of rock |
| WO2018009625A1 (en) | 2016-07-07 | 2018-01-11 | Bristol-Myers Squibb Company | Spirolactams 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 |
| ES2829400T3 (es) | 2016-11-30 | 2021-05-31 | Bristol Myers Squibb Co | Inhibidores tricíclicos de Rho cinasa |
-
2017
- 2017-07-06 CN CN201780054580.4A patent/CN110049977B/zh active Active
- 2017-07-06 ES ES17740240T patent/ES2814325T3/es active Active
- 2017-07-06 WO PCT/US2017/040846 patent/WO2018009622A1/en not_active Ceased
- 2017-07-06 JP JP2019500450A patent/JP6903731B2/ja active Active
- 2017-07-06 US US16/315,674 patent/US10730858B2/en active Active
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- 2017-07-06 KR KR1020197003126A patent/KR102473481B1/ko active Active
-
2021
- 2021-06-23 JP JP2021103777A patent/JP7225317B2/ja active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20140206686A1 (en) | 2013-01-18 | 2014-07-24 | Bristol-Myers Squibb Company | Phthalazinones and isoquinolinones as rock inhibitors |
| WO2016010950A1 (en) | 2014-07-15 | 2016-01-21 | Bristol-Myers Squibb Company | Spirocycloheptanes as inhibitors of rock |
| WO2016112236A1 (en) | 2015-01-09 | 2016-07-14 | Bristol-Myers Squibb Company | Cyclic ureas as inhibitors of rock |
Also Published As
| Publication number | Publication date |
|---|---|
| US10730858B2 (en) | 2020-08-04 |
| CN110049977A (zh) | 2019-07-23 |
| EP3481816A1 (en) | 2019-05-15 |
| JP2019520402A (ja) | 2019-07-18 |
| KR20190025960A (ko) | 2019-03-12 |
| JP2021152061A (ja) | 2021-09-30 |
| JP6903731B2 (ja) | 2021-07-14 |
| EP3481816B1 (en) | 2020-06-24 |
| JP7225317B2 (ja) | 2023-02-20 |
| CN110049977B (zh) | 2022-01-18 |
| ES2814325T3 (es) | 2021-03-26 |
| WO2018009622A1 (en) | 2018-01-11 |
| US20190300510A1 (en) | 2019-10-03 |
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