JP2010522184A5 - - Google Patents
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- JP2010522184A5 JP2010522184A5 JP2009554633A JP2009554633A JP2010522184A5 JP 2010522184 A5 JP2010522184 A5 JP 2010522184A5 JP 2009554633 A JP2009554633 A JP 2009554633A JP 2009554633 A JP2009554633 A JP 2009554633A JP 2010522184 A5 JP2010522184 A5 JP 2010522184A5
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- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- aryl
- alkyl
- heteroaryl
- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims description 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 10
- 206010028980 Neoplasm Diseases 0.000 claims description 6
- 201000011510 cancer Diseases 0.000 claims description 6
- 201000010099 disease Diseases 0.000 claims description 6
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 6
- 230000004770 neurodegeneration Effects 0.000 claims description 5
- 230000002265 prevention Effects 0.000 claims description 5
- 208000035475 disorder Diseases 0.000 claims description 4
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims description 3
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 206010003591 Ataxia Diseases 0.000 claims description 2
- 206010008111 Cerebral haemorrhage Diseases 0.000 claims description 2
- 206010067889 Dementia with Lewy bodies Diseases 0.000 claims description 2
- 208000012661 Dyskinesia Diseases 0.000 claims description 2
- 206010016212 Familial tremor Diseases 0.000 claims description 2
- 208000001799 Hereditary Optic Atrophies Diseases 0.000 claims description 2
- 208000023105 Huntington disease Diseases 0.000 claims description 2
- 208000009829 Lewy Body Disease Diseases 0.000 claims description 2
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 201000007737 Retinal degeneration Diseases 0.000 claims description 2
- 208000000323 Tourette Syndrome Diseases 0.000 claims description 2
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- 230000007850 degeneration Effects 0.000 claims description 2
- 201000006517 essential tremor Diseases 0.000 claims description 2
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- 229920000155 polyglutamine Polymers 0.000 claims description 2
- 108010040003 polyglutamine Proteins 0.000 claims description 2
- 230000000750 progressive effect Effects 0.000 claims description 2
- 230000001148 spastic effect Effects 0.000 claims description 2
- 208000002320 spinal muscular atrophy Diseases 0.000 claims description 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 20
- 125000003118 aryl group Chemical group 0.000 claims 17
- 229910052760 oxygen Inorganic materials 0.000 claims 16
- 125000000623 heterocyclic group Chemical group 0.000 claims 15
- 229910052739 hydrogen Inorganic materials 0.000 claims 14
- 150000002431 hydrogen Chemical group 0.000 claims 14
- 239000001257 hydrogen Substances 0.000 claims 14
- 229910052717 sulfur Inorganic materials 0.000 claims 14
- 125000000753 cycloalkyl group Chemical group 0.000 claims 11
- 229910052757 nitrogen Inorganic materials 0.000 claims 11
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical group 0.000 claims 10
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 9
- -1 amino, hydroxy Chemical group 0.000 claims 9
- 239000000651 prodrug Substances 0.000 claims 9
- 229940002612 prodrug Drugs 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 9
- 239000012453 solvate Substances 0.000 claims 9
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 9
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 125000002252 acyl group Chemical group 0.000 claims 7
- 125000003107 substituted aryl group Chemical group 0.000 claims 7
- 229910004013 NO 2 Inorganic materials 0.000 claims 6
- 125000003282 alkyl amino group Chemical group 0.000 claims 6
- 125000004663 dialkyl amino group Chemical group 0.000 claims 6
- 125000000547 substituted alkyl group Chemical group 0.000 claims 6
- 125000003342 alkenyl group Chemical group 0.000 claims 5
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 5
- 125000004414 alkyl thio group Chemical group 0.000 claims 5
- 125000000304 alkynyl group Chemical group 0.000 claims 5
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 5
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 5
- 125000001931 aliphatic group Chemical group 0.000 claims 4
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 125000005017 substituted alkenyl group Chemical class 0.000 claims 4
- 125000004426 substituted alkynyl group Chemical class 0.000 claims 4
- 210000004027 cell Anatomy 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 230000002062 proliferating effect Effects 0.000 claims 3
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 101710113864 Heat shock protein 90 Proteins 0.000 claims 2
- 102100034051 Heat shock protein HSP 90-alpha Human genes 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 206010003571 Astrocytoma Diseases 0.000 claims 1
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- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
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- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
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- 208000006265 Renal cell carcinoma Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 206010044074 Torticollis Diseases 0.000 claims 1
- 206010046298 Upper motor neurone lesion Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 206010047741 Vulval cancer Diseases 0.000 claims 1
- 208000004354 Vulvar Neoplasms Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 230000005494 condensation Effects 0.000 claims 1
- 238000009833 condensation Methods 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 208000018197 inherited torticollis Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
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- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 208000003154 papilloma Diseases 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 230000001105 regulatory effect Effects 0.000 claims 1
- 208000015347 renal cell adenocarcinoma Diseases 0.000 claims 1
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 201000005102 vulva cancer Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 description 3
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- 208000010412 Glaucoma Diseases 0.000 description 2
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- 241000709661 Enterovirus Species 0.000 description 1
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- 201000011240 Frontotemporal dementia Diseases 0.000 description 1
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- 206010026749 Mania Diseases 0.000 description 1
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- 208000031888 Mycoses Diseases 0.000 description 1
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- 206010036105 Polyneuropathy Diseases 0.000 description 1
- 206010037075 Protozoal infections Diseases 0.000 description 1
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- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 1
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Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US89592107P | 2007-03-20 | 2007-03-20 | |
| US60/895,921 | 2007-03-20 | ||
| US1528807P | 2007-12-20 | 2007-12-20 | |
| US61/015,288 | 2007-12-20 | ||
| PCT/US2008/056396 WO2008115719A1 (en) | 2007-03-20 | 2008-03-10 | Fused amino pyridine as hsp90 inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010522184A JP2010522184A (ja) | 2010-07-01 |
| JP2010522184A5 true JP2010522184A5 (https=) | 2011-04-28 |
| JP5401329B2 JP5401329B2 (ja) | 2014-01-29 |
Family
ID=39766345
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009554633A Active JP5401329B2 (ja) | 2007-03-20 | 2008-03-10 | Ｈｓｐ９０インヒビターとしての縮合アミノピリジン |
Country Status (24)
| Country | Link |
|---|---|
| US (10) | US8324240B2 (https=) |
| EP (1) | EP2069324B1 (https=) |
| JP (1) | JP5401329B2 (https=) |
| KR (1) | KR101313804B1 (https=) |
| CN (1) | CN101679347B (https=) |
| AU (1) | AU2008229216B2 (https=) |
| BR (1) | BRPI0808301B1 (https=) |
| CA (1) | CA2680778C (https=) |
| CY (1) | CY1114507T1 (https=) |
| DK (1) | DK2069324T3 (https=) |
| EA (1) | EA019103B1 (https=) |
| ES (1) | ES2430217T3 (https=) |
| HR (1) | HRP20130910T1 (https=) |
| IL (2) | IL200924A (https=) |
| MX (1) | MX2009009936A (https=) |
| MY (1) | MY148860A (https=) |
| NZ (1) | NZ579635A (https=) |
| PL (1) | PL2069324T3 (https=) |
| PT (1) | PT2069324E (https=) |
| RS (1) | RS52978B (https=) |
| SI (1) | SI2069324T1 (https=) |
| TW (1) | TWI471131B (https=) |
| WO (1) | WO2008115719A1 (https=) |
| ZA (1) | ZA200906371B (https=) |
Families Citing this family (64)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070129334A1 (en) * | 2001-10-30 | 2007-06-07 | Conforma Therapeutics Corporation | Orally Active Purine-Based Inhibitors of Heat Shock Protein 90 |
| US9403828B2 (en) | 2005-02-01 | 2016-08-02 | Sloan-Kettering Institute For Cancer Research | Small-molecule Hsp90 inhibitors |
| US7834181B2 (en) * | 2005-02-01 | 2010-11-16 | Slaon-Kettering Institute For Cancer Research | Small-molecule Hsp90 inhibitors |
| US10336757B2 (en) * | 2006-06-30 | 2019-07-02 | Sloan-Kettering Institute For Cancer Research | Treatment of neurodegenerative diseases through inhibition of HSP90 |
| EP2061772A4 (en) * | 2006-09-11 | 2011-06-29 | Curis Inc | MULTIFUNCTIONAL SMALL MOLECULES AS PROLIFERATION-ACTIVE ACTIVE SUBSTANCES |
| US20080234297A1 (en) * | 2007-03-20 | 2008-09-25 | Changgeng Qian | HSP90 Inhibitors Containing a Zinc Binding Moiety |
| JP5401329B2 (ja) * | 2007-03-20 | 2014-01-29 | キュリス，インコーポレイテッド | Ｈｓｐ９０インヒビターとしての縮合アミノピリジン |
| EP2469399B1 (en) | 2008-02-11 | 2019-09-11 | Idean Enterprises Oy | Layer-based user interface |
| US8017780B1 (en) | 2008-10-09 | 2011-09-13 | Myrexis, Inc. | Therapeutic compounds and uses thereof |
| CA2786715C (en) | 2009-01-16 | 2019-05-21 | Curis, Inc. | Fused amino pyridines for the treatment of brain tumors |
| TWI460177B (zh) | 2009-07-10 | 2014-11-11 | Taiho Pharmaceutical Co Ltd | An azabicyclo compound or a salt thereof |
| AR077405A1 (es) | 2009-07-10 | 2011-08-24 | Sanofi Aventis | Derivados del indol inhibidores de hsp90, composiciones que los contienen y utilizacion de los mismos para el tratamiento del cancer |
| FR2949467B1 (fr) | 2009-09-03 | 2011-11-25 | Sanofi Aventis | Nouveaux derives de 5,6,7,8-tetrahydroindolizine inhibiteurs d'hsp90, compositions les contenant et utilisation |
| WO2011044394A1 (en) * | 2009-10-07 | 2011-04-14 | Sloan-Kettering Institute For Cancer Research | Purine derivatives useful as hsp90 inhibitors |
| AU2013204109B2 (en) * | 2009-10-07 | 2016-05-05 | Sloan-Kettering Institute For Cancer Research | Purine derivatives useful as hsp90 inhibitors |
| EP2542687A1 (en) * | 2010-03-05 | 2013-01-09 | Baylor Research Institute | Involvement of androgen/androgen receptor pathway in fabry disease |
| WO2012131413A1 (en) * | 2011-03-25 | 2012-10-04 | Debiopharm Sa | Crystalline forms of fused amino pyridines as hsp90 inhibitors |
| ES2647889T3 (es) * | 2011-04-05 | 2017-12-27 | Sloan-Kettering Institute For Cancer Research | Inhibidores de la Hsp90 |
| WO2012138894A1 (en) | 2011-04-05 | 2012-10-11 | Sloan-Kettering Institute For Cancer Research | Hsp90 inhibitors |
| WO2012147084A2 (en) * | 2011-04-26 | 2012-11-01 | Rdd Pharma Ltd. | Oxymetazoline for the treatment of ano-rectal disorders |
| SMT201900660T1 (it) | 2012-02-09 | 2020-01-14 | Univ Kansas | Inibitori c-terminali di hsp90 |
| MX2014014188A (es) | 2012-05-25 | 2015-05-11 | Berg Llc | Metodos para tratar un sindrome metaboilico mediante la modulacion de la proteina de choque termico (hsp) 90-beta. |
| US10201623B2 (en) | 2013-03-15 | 2019-02-12 | Memorial Sloan Kettering Cancer Center | HSP90-targeted cardiac imaging and therapy |
| TW201533043A (zh) * | 2013-04-18 | 2015-09-01 | Lundbeck & Co As H | 作爲ｌｒｒｋ２抑制劑的芳基吡咯并吡啶衍生化合物 |
| JP6539275B2 (ja) | 2013-08-16 | 2019-07-03 | メモリアル スローン ケタリング キャンサー センター | 選択的ｇｒｐ９４阻害剤およびその使用 |
| MX2016008418A (es) | 2013-12-23 | 2017-01-11 | Memorial Sloan Kettering Cancer Center | Metodos y reactivos para el radiomarcaje. |
| US10023864B2 (en) | 2014-06-06 | 2018-07-17 | Berg Llc | Methods of treating a metabolic syndrome by modulating heat shock protein (HSP) 90-beta |
| MX388516B (es) * | 2014-06-24 | 2025-03-20 | Univ Kansas | Bifenil amidas con grupos éter modificados como inhibidores de hsp90 e inductores de hsp70. |
| CN113521314A (zh) | 2014-09-17 | 2021-10-22 | 纪念斯隆-凯特琳癌症中心 | Hsp90-靶向炎症和感染成像及治疗 |
| LT3319959T (lt) | 2015-07-06 | 2021-12-27 | Alkermes, Inc. | Histono deacetilazės hetero-halogeno inhibitoriai |
| EP3319968A1 (en) | 2015-07-06 | 2018-05-16 | Rodin Therapeutics, Inc. | Heterobicyclic n-aminophenyl-amides as inhibitors of histone deacetylase |
| RS62959B1 (sr) | 2017-01-11 | 2022-03-31 | Alkermes Inc | Biciklični inhibitori histon-deacetilaze |
| ES2747768T3 (es) | 2017-03-20 | 2020-03-11 | Forma Therapeutics Inc | Composiciones de pirrolopirrol como activadores de quinasa de piruvato (PKR) |
| EP3600376A1 (en) | 2017-03-31 | 2020-02-05 | Alma Bio Therapeutics | Methods of treatment of hla-b27 related inflammatory diseases and compositions related to same |
| US11225475B2 (en) | 2017-08-07 | 2022-01-18 | Alkermes, Inc. | Substituted pyridines as inhibitors of histone deacetylase |
| JP7508375B2 (ja) | 2018-05-14 | 2024-07-01 | リアタ ファーマシューティカルズ インコーポレイテッド | 熱ショックタンパク質経路に関連する疾患の治療のための、修飾された糖基を有するビアリールアミド |
| ES2989438T3 (es) | 2018-09-19 | 2024-11-26 | Novo Nordisk Healthcare Ag | Activación de la piruvato cinasa R |
| US12053458B2 (en) | 2018-09-19 | 2024-08-06 | Novo Nordisk Health Care Ag | Treating sickle cell disease with a pyruvate kinase R activating compound |
| CA3125900A1 (en) | 2019-01-08 | 2020-07-16 | Kyorin Pharmaceutical Co., Ltd. | 15-pgdh inhibitor |
| US12304897B2 (en) | 2019-01-31 | 2025-05-20 | Kyorin Pharmaceutical Co., Ltd. | 15-PGDH inhibitors |
| US20220378756A1 (en) | 2019-09-19 | 2022-12-01 | Forma Therapeutics, Inc. | Activating pyruvate kinase r |
| GB202006382D0 (en) | 2020-04-30 | 2020-06-17 | Spermatech As | Use |
| US12128035B2 (en) | 2021-03-19 | 2024-10-29 | Novo Nordisk Health Care Ag | Activating pyruvate kinase R |
| WO2023006993A1 (en) | 2021-07-30 | 2023-02-02 | Atmosr | Fused amino pyridine or pyrimidine derivatives for the treatment of congenital central hypoventilation syndrome |
| WO2024076731A1 (en) * | 2022-10-06 | 2024-04-11 | Regranion, Llc | Methods and compositions for treating hidradenitis suppurativa |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| AU2024296650A1 (en) * | 2023-07-10 | 2026-02-19 | Regranion, Llc | Methods and compositions for treating atopic dermatitis |
| IL326136A (en) | 2023-08-07 | 2026-03-01 | Revolution Medicines Inc | RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein |
| WO2025080629A1 (en) * | 2023-10-10 | 2025-04-17 | Regranion, Llc | Methods and compositions for treating behçet's disease |
| WO2025080623A1 (en) * | 2023-10-10 | 2025-04-17 | Regranion, Llc | Methods and compositions for treating discoid lupus erythematosus, systemic lupus erythematosus, and subacute cutaneous lupus erythematosus |
| WO2025080645A1 (en) * | 2023-10-10 | 2025-04-17 | Regranion, Llc | Methods and compositions for treating bullous pemphigoid |
| 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 |
| WO2025217284A1 (en) * | 2024-04-09 | 2025-10-16 | Regranion, Llc | Methods and compositions for treating inflammatory and autoimmune disorders of the skin |
| 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 |
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