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
-
- C—CHEMISTRY; METALLURGY
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- 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
- C07D403/02—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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- 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
-
- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
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- 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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- 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
-
- 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
-
- 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)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
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- Chemical Kinetics & Catalysis (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Immunology (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
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- Pulmonology (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Vascular Medicine (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen Condensed Heterocyclic Rings (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 (enExample) | 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 (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 (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| WO2017205709A1 (en) | 2016-05-27 | 2017-11-30 | 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 |
| 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 |
| EP3548468B1 (en) | 2016-11-30 | 2020-09-16 | Bristol-Myers Squibb Company | Tricyclic rho kinase inhibitors |
| 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 |
| JP7234201B2 (ja) | 2017-07-12 | 2023-03-07 | ブリストル－マイヤーズ スクイブ カンパニー | 心不全の治療のためのｒｏｃｋの５員アミノヘテロ環および５，６－または６，６員二環式アミノヘテロ環の阻害剤 |
| 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 |
| ES2937039T3 (es) | 2017-11-03 | 2023-03-23 | Bristol Myers Squibb Co | Inhibidores diazaespiro de ROCK |
| 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 |
| JP2022547777A (ja) * | 2019-09-06 | 2022-11-16 | 小野薬品工業株式会社 | ヒダントイン誘導体 |
| 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 |
| IL299612A (en) | 2020-07-02 | 2023-03-01 | Incyte Corp | Tricyclic urea 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 |
| CA3211748A1 (en) | 2021-02-25 | 2022-09-01 | Incyte Corporation | Spirocyclic lactams as jak2 v617f inhibitors |
| SMT202500447T1 (it) | 2021-11-02 | 2026-01-12 | Flare Therapeutics Inc | Agonisti inversi di pparg e loro usi |
| CA3238227A1 (en) | 2021-11-11 | 2023-05-19 | The Doshisha | Cryopreservation preparation for corneal endothelial cells and method for producing said cryopreservation preparation |
| IL315647A (en) | 2022-03-17 | 2024-11-01 | Incyte Corp | Tricyclic urea compounds as Jak2 and 617f inhibitors |
| KR20260019479A (ko) | 2023-05-04 | 2026-02-10 | 레볼루션 메디슨즈, 인크. | Ras 관련 질환 또는 장애를 위한 병용 요법 |
| CN121889155A (zh) | 2023-08-07 | 2026-04-17 | 锐新医药公司 | 用于治疗ras蛋白相关疾病或病症的rmc-6291 |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic 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 |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
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| 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 |
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