JP6903731B2 - 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 - Google Patents
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 Download PDFInfo
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- JP6903731B2 JP6903731B2 JP2019500450A JP2019500450A JP6903731B2 JP 6903731 B2 JP6903731 B2 JP 6903731B2 JP 2019500450 A JP2019500450 A JP 2019500450A JP 2019500450 A JP2019500450 A JP 2019500450A JP 6903731 B2 JP6903731 B2 JP 6903731B2
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- substituted
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- 0 CCC*C(*C(NC1)=CC=C1C1=CC=CC=CC=CC=CC=CC=C1)=O Chemical compound CCC*C(*C(NC1)=CC=C1C1=CC=CC=CC=CC=CC=CC=C1)=O 0.000 description 5
- IFMORUNBRIRXLF-RZSVFLSASA-N C/N=C\C=C/C=C Chemical compound C/N=C\C=C/C=C IFMORUNBRIRXLF-RZSVFLSASA-N 0.000 description 1
- NNLOCKPMVPEAAF-QBJFVVIPSA-N CCN(C)C/C(/C=C\C)=C(\C)/C=C Chemical compound CCN(C)C/C(/C=C\C)=C(\C)/C=C NNLOCKPMVPEAAF-QBJFVVIPSA-N 0.000 description 1
- ZHHTYTDZEMZYOZ-UHFFFAOYSA-N CN(CCN1c(cc2)ccc2C(c2ccccc22)=NNC2=O)C1=O Chemical compound CN(CCN1c(cc2)ccc2C(c2ccccc22)=NNC2=O)C1=O ZHHTYTDZEMZYOZ-UHFFFAOYSA-N 0.000 description 1
- YIRAUZOICMUAQR-UHFFFAOYSA-N CN1N=C(c(cc2)ccc2N(CC(c2ccccc2)O2)C2=O)c(cccc2)c2C1=O Chemical compound CN1N=C(c(cc2)ccc2N(CC(c2ccccc2)O2)C2=O)c(cccc2)c2C1=O YIRAUZOICMUAQR-UHFFFAOYSA-N 0.000 description 1
- VIYQODYZRGGKJF-UHFFFAOYSA-N CN1N=C(c(cc2)ccc2N(CCC2C(N(C3)Cc4c3cccc4)=O)C2=O)c(cccc2)c2C1=O Chemical compound CN1N=C(c(cc2)ccc2N(CCC2C(N(C3)Cc4c3cccc4)=O)C2=O)c(cccc2)c2C1=O VIYQODYZRGGKJF-UHFFFAOYSA-N 0.000 description 1
- QUKKRSFVDPIFEL-UHFFFAOYSA-N COc1ccccc1NC(CCN1c(cc2)ccc2C(c2ccccc22)=NNC2=O)C1=O Chemical compound COc1ccccc1NC(CCN1c(cc2)ccc2C(c2ccccc22)=NNC2=O)C1=O QUKKRSFVDPIFEL-UHFFFAOYSA-N 0.000 description 1
- IPZUBKBAYXWIBL-UHFFFAOYSA-N Cc1cc(NC(CCN2c(cc3)ccc3C(c3ccccc33)=NNC3=O)C2=O)cc(OC)c1 Chemical compound Cc1cc(NC(CCN2c(cc3)ccc3C(c3ccccc33)=NNC3=O)C2=O)cc(OC)c1 IPZUBKBAYXWIBL-UHFFFAOYSA-N 0.000 description 1
- JAGCQTZNUQROMH-UHFFFAOYSA-N O=C(C(CC1)Nc2cc(OC(F)F)ccc2)N1c(cc1)ccc1C(c1ccccc11)=NNC1=O Chemical compound O=C(C(CC1)Nc2cc(OC(F)F)ccc2)N1c(cc1)ccc1C(c1ccccc11)=NNC1=O JAGCQTZNUQROMH-UHFFFAOYSA-N 0.000 description 1
- HDRNNUSDYFMXMS-UHFFFAOYSA-N O=C1N(c(cc2)ccc2C(c2ccccc22)=NNC2=O)N=CN1Cc1cc(OC(F)F)ccc1 Chemical compound O=C1N(c(cc2)ccc2C(c2ccccc22)=NNC2=O)N=CN1Cc1cc(OC(F)F)ccc1 HDRNNUSDYFMXMS-UHFFFAOYSA-N 0.000 description 1
- CWUQIEBYZXRBCI-UHFFFAOYSA-N O=C1N(c(cc2)ccc2C(c2ccccc22)=NNC2=O)N=CN1Cc1cccc(F)c1 Chemical compound O=C1N(c(cc2)ccc2C(c2ccccc22)=NNC2=O)N=CN1Cc1cccc(F)c1 CWUQIEBYZXRBCI-UHFFFAOYSA-N 0.000 description 1
- PHNXYQCFZAMNIX-UHFFFAOYSA-N O=C1OCC(c2ccccc2)N1c(cc1)ccc1C(c1ccccc11)=NNC1=O Chemical compound O=C1OCC(c2ccccc2)N1c(cc1)ccc1C(c1ccccc11)=NNC1=O PHNXYQCFZAMNIX-UHFFFAOYSA-N 0.000 description 1
Classifications
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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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- 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
-
- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- 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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- 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
- 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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- 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
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- 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
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- 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
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- 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
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- 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)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
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- Engineering & Computer Science (AREA)
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- General Chemical & Material Sciences (AREA)
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- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Immunology (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
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- Physical Education & Sports Medicine (AREA)
- Pulmonology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Transplantation (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (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)
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 JP2019520402A5 (OSRAM) | 2020-08-13 |
| JP6903731B2 true JP6903731B2 (ja) | 2021-07-14 |
Family
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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 (OSRAM) |
| EP (1) | EP3481816B1 (OSRAM) |
| JP (2) | JP6903731B2 (OSRAM) |
| KR (1) | KR102473481B1 (OSRAM) |
| CN (1) | CN110049977B (OSRAM) |
| ES (1) | ES2814325T3 (OSRAM) |
| WO (1) | WO2018009622A1 (OSRAM) |
Families Citing this family (30)
| 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 |
| WO2018009625A1 (en) | 2016-07-07 | 2018-01-11 | Bristol-Myers Squibb Company | Spirolactams as inhibitors of rock |
| 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 |
| CN110869361B (zh) | 2017-07-12 | 2023-06-02 | 百时美施贵宝公司 | 用于治疗心力衰竭的rock的五元氨基杂环和5,6元或6,6元双环氨基杂环抑制剂 |
| US12060341B2 (en) | 2017-07-12 | 2024-08-13 | Bristol-Myers Squibb Company | Spiroheptanyl hydantoins 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 |
| ES2878054T3 (es) | 2017-07-12 | 2021-11-18 | Bristol Myers Squibb Co | Espiroheptanil hidantoínas como inhibidores de ROCK |
| WO2019089868A1 (en) | 2017-11-03 | 2019-05-09 | Bristol-Myers Squibb Company | Diazaspiro rock inhibitors |
| US11248004B2 (en) | 2018-11-06 | 2022-02-15 | Cervello Therapeutics, Llc. | Substituted isoquinolines as rock kinase inhibitors |
| DK3877364T3 (da) | 2018-11-06 | 2024-09-23 | Cervello Therapeutics LLC | Rock-kinasehæmmere |
| US20220306640A1 (en) * | 2019-09-06 | 2022-09-29 | Ono Pharmaceutical Co., Ltd. | Hydantoin derivative |
| US11753413B2 (en) | 2020-06-19 | 2023-09-12 | Incyte Corporation | Substituted pyrrolo[2,1-f][1,2,4]triazine compounds as JAK2 V617F inhibitors |
| US11691971B2 (en) | 2020-06-19 | 2023-07-04 | Incyte Corporation | Naphthyridinone compounds as JAK2 V617F inhibitors |
| SI4175719T1 (sl) | 2020-07-02 | 2025-07-31 | Incyte Corporation | Triciklične sečninske spojine kot zaviralci jak2 v617f |
| US11767323B2 (en) | 2020-07-02 | 2023-09-26 | 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 |
| WO2022140231A1 (en) | 2020-12-21 | 2022-06-30 | Incyte Corporation | Deazaguaine compounds as jak2 v617f inhibitors |
| US11958861B2 (en) | 2021-02-25 | 2024-04-16 | Incyte Corporation | Spirocyclic lactams as JAK2 V617F inhibitors |
| TW202334089A (zh) | 2021-11-02 | 2023-09-01 | 美商夫雷爾醫療公司 | Ｐｐａｒｇ反向激動劑及其用途 |
| KR20240110954A (ko) | 2021-11-11 | 2024-07-16 | 학교법인 도시샤 | 각막 내피 세포의 냉동보존 제제 및 상기 냉동보존 제제를 생산하기 위한 방법 |
| US12084430B2 (en) | 2022-03-17 | 2024-09-10 | Incyte Corporation | Tricyclic urea compounds as JAK2 V617F inhibitors |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | 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 |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | 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 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| AU2005289560A1 (en) | 2004-09-28 | 2006-04-06 | Angion Biomedica Corp. | Small molecule modulators of cytokine activity |
| DK2698062T3 (en) * | 2006-12-28 | 2015-09-14 | Abbvie Inc | Poly (ADP-ribose) polymerase inhibitors |
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| 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 |
| KR102511441B1 (ko) | 2016-11-30 | 2023-03-16 | 브리스톨-마이어스 스큅 컴퍼니 | 트리시클릭 Rho 키나제 억제제 |
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- 2017-07-06 KR KR1020197003126A patent/KR102473481B1/ko active Active
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- 2017-07-06 JP JP2019500450A patent/JP6903731B2/ja active Active
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| CN110049977A (zh) | 2019-07-23 |
| EP3481816B1 (en) | 2020-06-24 |
| US10730858B2 (en) | 2020-08-04 |
| KR102473481B1 (ko) | 2022-12-01 |
| JP2021152061A (ja) | 2021-09-30 |
| EP3481816A1 (en) | 2019-05-15 |
| US20190300510A1 (en) | 2019-10-03 |
| JP7225317B2 (ja) | 2023-02-20 |
| JP2019520402A (ja) | 2019-07-18 |
| CN110049977B (zh) | 2022-01-18 |
| WO2018009622A1 (en) | 2018-01-11 |
| ES2814325T3 (es) | 2021-03-26 |
| KR20190025960A (ko) | 2019-03-12 |
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