JP7516029B2 - Kras g12c阻害剤化合物の重要な中間体の改良合成法 - Google Patents
Kras g12c阻害剤化合物の重要な中間体の改良合成法 Download PDFInfo
- Publication number
- JP7516029B2 JP7516029B2 JP2019205198A JP2019205198A JP7516029B2 JP 7516029 B2 JP7516029 B2 JP 7516029B2 JP 2019205198 A JP2019205198 A JP 2019205198A JP 2019205198 A JP2019205198 A JP 2019205198A JP 7516029 B2 JP7516029 B2 JP 7516029B2
- Authority
- JP
- Japan
- Prior art keywords
- fluoro
- formula
- compound
- composition
- methyl
- 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.)
- Active
Links
Images
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/01—Sulfonic acids
- C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
- C07C309/24—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of a carbon skeleton containing six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C67/00—Preparation of carboxylic acid esters
- C07C67/48—Separation; Purification; Stabilisation; Use of additives
- C07C67/52—Separation; Purification; Stabilisation; Use of additives by change in the physical state, e.g. crystallisation
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
- C07C69/76—Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
- C07C69/76—Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring
- C07C69/78—Benzoic acid esters
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D307/06—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B57/00—Separation of optically-active compounds
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Crystallography & Structural Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Furan Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024106605A JP2024127907A (ja) | 2018-11-16 | 2024-07-02 | Kras g12c阻害剤化合物の重要な中間体の改良合成法 |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862768802P | 2018-11-16 | 2018-11-16 | |
| US62/768,802 | 2018-11-16 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024106605A Division JP2024127907A (ja) | 2018-11-16 | 2024-07-02 | Kras g12c阻害剤化合物の重要な中間体の改良合成法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020090482A JP2020090482A (ja) | 2020-06-11 |
| JP2020090482A5 JP2020090482A5 (https=) | 2022-11-18 |
| JP7516029B2 true JP7516029B2 (ja) | 2024-07-16 |
Family
ID=68887130
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019205198A Active JP7516029B2 (ja) | 2018-11-16 | 2019-11-13 | Kras g12c阻害剤化合物の重要な中間体の改良合成法 |
| JP2024106605A Pending JP2024127907A (ja) | 2018-11-16 | 2024-07-02 | Kras g12c阻害剤化合物の重要な中間体の改良合成法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024106605A Pending JP2024127907A (ja) | 2018-11-16 | 2024-07-02 | Kras g12c阻害剤化合物の重要な中間体の改良合成法 |
Country Status (25)
| Country | Link |
|---|---|
| US (5) | US11299491B2 (https=) |
| EP (2) | EP3880670B1 (https=) |
| JP (2) | JP7516029B2 (https=) |
| KR (2) | KR20250164341A (https=) |
| CN (3) | CN113015724B (https=) |
| AR (1) | AR117101A1 (https=) |
| AU (2) | AU2019381817B2 (https=) |
| BR (1) | BR112021009384A2 (https=) |
| CA (1) | CA3117221A1 (https=) |
| CL (1) | CL2021001266A1 (https=) |
| DK (1) | DK3880670T3 (https=) |
| EA (1) | EA202191381A1 (https=) |
| ES (1) | ES2953752T3 (https=) |
| FI (1) | FI3880670T3 (https=) |
| HU (1) | HUE062656T2 (https=) |
| IL (2) | IL318601A (https=) |
| LT (1) | LT3880670T (https=) |
| MA (1) | MA54233A (https=) |
| MX (2) | MX2021005598A (https=) |
| PL (1) | PL3880670T3 (https=) |
| PT (1) | PT3880670T (https=) |
| SG (1) | SG11202104927QA (https=) |
| SI (1) | SI3880670T1 (https=) |
| TW (1) | TWI862525B (https=) |
| WO (1) | WO2020102730A1 (https=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2024127907A (ja) * | 2018-11-16 | 2024-09-20 | アムジエン・インコーポレーテツド | Kras g12c阻害剤化合物の重要な中間体の改良合成法 |
Families Citing this family (58)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110366550A (zh) | 2016-12-22 | 2019-10-22 | 美国安进公司 | 作为用于治疗肺癌、胰腺癌或结直肠癌的KRAS G12C抑制剂的苯并异噻唑、异噻唑并[3,4-b]吡啶、喹唑啉、酞嗪、吡啶并[2,3-d]哒嗪和吡啶并[2,3-d]嘧啶衍生物 |
| AU2018273356B2 (en) | 2017-05-22 | 2021-09-16 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
| AU2018329920B2 (en) | 2017-09-08 | 2022-12-01 | Amgen Inc. | Inhibitors of KRAS G12C and methods of using the same |
| EP3788053B1 (en) | 2018-05-04 | 2024-07-10 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| CA3098574A1 (en) | 2018-05-04 | 2019-11-07 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| MA52564A (fr) | 2018-05-10 | 2021-03-17 | Amgen Inc | Inhibiteurs de kras g12c pour le traitement du cancer |
| US11096939B2 (en) | 2018-06-01 | 2021-08-24 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
| MX2020012204A (es) | 2018-06-11 | 2021-03-31 | Amgen Inc | Inhibidores de kras g12c para tratar el cáncer. |
| US11285156B2 (en) | 2018-06-12 | 2022-03-29 | Amgen Inc. | Substituted piperazines as KRAS G12C inhibitors |
| AU2019384118B2 (en) | 2018-11-19 | 2025-06-12 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
| JP7377679B2 (ja) | 2018-11-19 | 2023-11-10 | アムジエン・インコーポレーテツド | がん治療のためのkrasg12c阻害剤及び1種以上の薬学的に活性な追加の薬剤を含む併用療法 |
| EP3738593A1 (en) | 2019-05-14 | 2020-11-18 | Amgen, Inc | Dosing of kras inhibitor for treatment of cancers |
| AU2020277398B2 (en) | 2019-05-21 | 2026-01-29 | Amgen Inc. | Solid state forms |
| WO2020236947A1 (en) | 2019-05-21 | 2020-11-26 | Amgen Inc. | Solid state forms |
| JP2023501528A (ja) | 2019-11-14 | 2023-01-18 | アムジエン・インコーポレーテツド | Kras g12c阻害剤化合物の改善された合成 |
| JP7837865B2 (ja) | 2019-11-14 | 2026-03-31 | アムジエン・インコーポレーテツド | Kras g12c阻害剤化合物の改良合成法 |
| EP4065231A1 (en) | 2019-11-27 | 2022-10-05 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| EP4067343A4 (en) | 2019-11-29 | 2024-01-03 | Taiho Pharmaceutical Co., Ltd. | NEW PHENOLIC COMPOUND OR SALT THEREOF |
| TW202144345A (zh) | 2020-03-17 | 2021-12-01 | 大陸商北京加科思新藥研發有限公司 | Kras突變蛋白抑制劑 |
| CN114585624A (zh) * | 2020-06-02 | 2022-06-03 | 上海喆邺生物科技有限公司 | 一种手性中间体及其制备方法 |
| JP7808058B2 (ja) | 2020-06-02 | 2026-01-28 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | がんを治療するための縮合環化2-アミノ-3-シアノチオフェン及び誘導体 |
| IL299131A (en) | 2020-06-18 | 2023-02-01 | Revolution Medicines Inc | Methods for delaying, preventing and treating acquired resistance to RAS inhibitors |
| CN115942936A (zh) | 2020-06-24 | 2023-04-07 | 勃林格殷格翰国际有限公司 | 包含sos1抑制剂和kras g12c抑制剂的抗癌组合疗法 |
| CN113929676A (zh) * | 2020-07-14 | 2022-01-14 | 浙江海正药业股份有限公司 | 吡啶并杂环类衍生物及其制备方法和用途 |
| JP7584815B2 (ja) | 2020-08-02 | 2024-11-18 | 上▲海▼▲哲▼▲イェ▼生物科技有限公司 | 抗腫瘍薬物における芳香族化合物及びその用途 |
| EP4204412A4 (en) * | 2020-08-26 | 2024-10-09 | InventisBio Co., Ltd. | HETEROARYL COMPOUNDS, PRODUCTION PROCESSES AND USES THEREOF |
| US20250195521A1 (en) | 2020-09-03 | 2025-06-19 | Revolution Medicines, Inc. | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| DK4225755T3 (da) * | 2020-10-07 | 2026-04-07 | Amgen Inc | Fremgangsmåde til racemisering og isolering af atropisomerer af 7-chlor-6-fluor-1-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-d]pyrimidin-2,4(1 h,3 h)-dion |
| CA3201663A1 (en) * | 2020-11-20 | 2022-05-27 | Amgen Inc. | Process for preparing 7-chloro-6-fluoro-1-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-d]pyrimidine-2,4(1h,3h)-dione |
| JP2024514127A (ja) | 2021-04-09 | 2024-03-28 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 抗がん剤療法 |
| JP2024518845A (ja) | 2021-05-19 | 2024-05-07 | テバ・ファーマシューティカルズ・インターナショナル・ゲーエムベーハー | ソトラシブ及びその固体状態形態の調製のためのプロセス |
| US20240287066A1 (en) * | 2021-06-24 | 2024-08-29 | Sandoz Ag | Crystalline Form of Sotorasib |
| CN114605406B (zh) * | 2021-09-18 | 2023-05-26 | 都创(上海)医药开发有限公司 | Amg510化合物的晶型及其制备方法和用途 |
| WO2023099624A1 (en) | 2021-12-01 | 2023-06-08 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| WO2023117681A1 (en) | 2021-12-22 | 2023-06-29 | Boehringer Ingelheim International Gmbh | Heteroaromatic compounds for the treatment of cancer |
| CN116375746B (zh) * | 2021-12-23 | 2025-08-05 | 上海馨远医药科技有限公司 | 一种(2-氟-6-羟基苯基)三氟硼酸钾的制备方法 |
| KR20240156373A (ko) | 2022-03-07 | 2024-10-29 | 암젠 인크 | 4-메틸-2-프로판-2-일-피리딘-3-카르보니트릴의 제조 방법 |
| CN115466259B (zh) * | 2022-08-16 | 2023-12-05 | 山东大学 | 一种kras g12c抑制剂索托拉西布的制备方法 |
| AU2024241633A1 (en) | 2023-03-30 | 2025-11-06 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ras相關疾病或病症之組合療法 |
| EP4720678A1 (en) | 2023-05-31 | 2026-04-08 | Boehringer Ingelheim International GmbH | Survivin as a biomarker for predicting the responsiveness of cancer treatment |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| CN121773111A (zh) * | 2023-08-15 | 2026-03-31 | 劲方医药科技(上海)股份有限公司 | 吡嗪并萘啶二酮类化合物的制备方法及其中间体 |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| AU2024361909A1 (en) | 2023-10-20 | 2026-03-26 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras proteins |
| CN117430605A (zh) * | 2023-10-26 | 2024-01-23 | 广西天铭药业有限公司 | 一种kras g12c抑制剂amg-510中间体的合成方法 |
| US20250205238A1 (en) | 2023-12-20 | 2025-06-26 | Boehringer Ingelheim International Gmbh | Anti-cancer combination therapy |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| TW202547461A (zh) | 2024-05-17 | 2025-12-16 | 美商銳新醫藥公司 | Ras抑制劑 |
| WO2025255438A1 (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 |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (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 |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20180334454A1 (en) | 2017-05-22 | 2018-11-22 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| WO2019051291A1 (en) | 2017-09-08 | 2019-03-14 | Amgen Inc. | Inhibitors of kras g12c and methods of using the same |
| WO2019213516A1 (en) | 2018-05-04 | 2019-11-07 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
Family Cites Families (210)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4232027A (en) | 1979-01-29 | 1980-11-04 | E. R. Squibb & Sons, Inc. | 1,2-Dihydro-2-oxo-4-phenyl-3-quinolinecarbonitrile derivatives |
| EP0090505B1 (en) | 1982-03-03 | 1990-08-08 | Genentech, Inc. | Human antithrombin iii, dna sequences therefor, expression vehicles and cloning vectors containing such sequences and cell cultures transformed thereby, a process for expressing human antithrombin iii, and pharmaceutical compositions comprising it |
| GB8827305D0 (en) | 1988-11-23 | 1988-12-29 | British Bio Technology | Compounds |
| JP2762522B2 (ja) | 1989-03-06 | 1998-06-04 | 藤沢薬品工業株式会社 | 血管新生阻害剤 |
| US5112946A (en) | 1989-07-06 | 1992-05-12 | Repligen Corporation | Modified pf4 compositions and methods of use |
| PT98990A (pt) | 1990-09-19 | 1992-08-31 | American Home Prod | Processo para a preparacao de esteres de acidos carboxilicos de rapamicina |
| US5892112A (en) | 1990-11-21 | 1999-04-06 | Glycomed Incorporated | Process for preparing synthetic matrix metalloprotease inhibitors |
| US5120842A (en) | 1991-04-01 | 1992-06-09 | American Home Products Corporation | Silyl ethers of rapamycin |
| US5100883A (en) | 1991-04-08 | 1992-03-31 | American Home Products Corporation | Fluorinated esters of rapamycin |
| US5118678A (en) | 1991-04-17 | 1992-06-02 | American Home Products Corporation | Carbamates of rapamycin |
| SG64322A1 (en) | 1991-05-10 | 1999-04-27 | Rhone Poulenc Rorer Int | Bis mono and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase |
| US5118677A (en) | 1991-05-20 | 1992-06-02 | American Home Products Corporation | Amide esters of rapamycin |
| NZ243082A (en) | 1991-06-28 | 1995-02-24 | Ici Plc | 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof |
| US5151413A (en) | 1991-11-06 | 1992-09-29 | American Home Products Corporation | Rapamycin acetals as immunosuppressant and antifungal agents |
| GB9125660D0 (en) | 1991-12-03 | 1992-01-29 | Smithkline Beecham Plc | Novel compound |
| GB9300059D0 (en) | 1992-01-20 | 1993-03-03 | Zeneca Ltd | Quinazoline derivatives |
| US5521184A (en) | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| ZA935112B (en) | 1992-07-17 | 1994-02-08 | Smithkline Beecham Corp | Rapamycin derivatives |
| ZA935111B (en) | 1992-07-17 | 1994-02-04 | Smithkline Beecham Corp | Rapamycin derivatives |
| US5256790A (en) | 1992-08-13 | 1993-10-26 | American Home Products Corporation | 27-hydroxyrapamycin and derivatives thereof |
| GB9221220D0 (en) | 1992-10-09 | 1992-11-25 | Sandoz Ag | Organic componds |
| JPH09509190A (ja) | 1992-10-13 | 1997-09-16 | ザ、プロクター、エンド、ギャンブル、カンパニー | 非水性液体洗剤組成物 |
| US5258389A (en) | 1992-11-09 | 1993-11-02 | Merck & Co., Inc. | O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives |
| WO1994011384A1 (en) | 1992-11-13 | 1994-05-26 | Immunex Corporation | Novel cytokine designated elk ligand |
| US5455258A (en) | 1993-01-06 | 1995-10-03 | Ciba-Geigy Corporation | Arylsulfonamido-substituted hydroxamic acids |
| US5629327A (en) | 1993-03-01 | 1997-05-13 | Childrens Hospital Medical Center Corp. | Methods and compositions for inhibition of angiogenesis |
| US5516658A (en) | 1993-08-20 | 1996-05-14 | Immunex Corporation | DNA encoding cytokines that bind the cell surface receptor hek |
| WO1995009847A1 (en) | 1993-10-01 | 1995-04-13 | Ciba-Geigy Ag | Pyrimidineamine derivatives and processes for the preparation thereof |
| US5656643A (en) | 1993-11-08 | 1997-08-12 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase |
| CA2175215C (en) | 1993-11-19 | 2008-06-03 | Yat Sun Or | Semisynthetic analogs of rapamycin (macrolides) being immunomodulators |
| SK78196A3 (en) | 1993-12-17 | 1997-02-05 | Sandoz Ag | Rapamycin demethoxy-derivatives, preparation method thereof and pharmaceutical agent containing them |
| US5700823A (en) | 1994-01-07 | 1997-12-23 | Sugen, Inc. | Treatment of platelet derived growth factor related disorders such as cancers |
| IL112248A0 (en) | 1994-01-25 | 1995-03-30 | Warner Lambert Co | Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them |
| IL112249A (en) | 1994-01-25 | 2001-11-25 | Warner Lambert Co | Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds |
| WO1995024190A2 (en) | 1994-03-07 | 1995-09-14 | Sugen, Inc. | Receptor tyrosine kinase inhibitors for inhibiting cell proliferative disorders and compositions thereof |
| EP0756627A1 (en) | 1994-04-15 | 1997-02-05 | Amgen Inc. | Hek5, hek7, hek8, hek11, new eph-like receptor protein tyrosine kinases |
| DE59500788D1 (de) | 1994-05-03 | 1997-11-20 | Ciba Geigy Ag | Pyrrolopyrimidinderivate mit antiproliferativer Wirkung |
| US6303769B1 (en) | 1994-07-08 | 2001-10-16 | Immunex Corporation | Lerk-5 dna |
| US5919905A (en) | 1994-10-05 | 1999-07-06 | Immunex Corporation | Cytokine designated LERK-6 |
| US6057124A (en) | 1995-01-27 | 2000-05-02 | Amgen Inc. | Nucleic acids encoding ligands for HEK4 receptors |
| US5863949A (en) | 1995-03-08 | 1999-01-26 | Pfizer Inc | Arylsulfonylamino hydroxamic acid derivatives |
| DE69536015D1 (de) | 1995-03-30 | 2009-12-10 | Pfizer Prod Inc | Chinazolinone Derivate |
| CA2214086C (en) | 1995-04-03 | 2008-07-29 | Novartis Ag | Pyrazole derivatives and processes for the preparation thereof |
| ES2153031T4 (es) | 1995-04-20 | 2001-05-16 | Pfizer | Derivados del acido arilsulfonil hidroxamico como inhibidores de mmp y tnf. |
| GB9508538D0 (en) | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quinazoline derivatives |
| US5747498A (en) | 1996-05-28 | 1998-05-05 | Pfizer Inc. | Alkynyl and azido-substituted 4-anilinoquinazolines |
| US5880141A (en) | 1995-06-07 | 1999-03-09 | Sugen, Inc. | Benzylidene-Z-indoline compounds for the treatment of disease |
| US5650415A (en) | 1995-06-07 | 1997-07-22 | Sugen, Inc. | Quinoline compounds |
| US5985890A (en) | 1995-06-09 | 1999-11-16 | Novartis Ag | Rapamycin derivatives |
| SI9620103A (sl) | 1995-07-06 | 1998-10-31 | Novartis Ag | Pirolopirimidini in postopki za njihovo pripravo |
| DE19534177A1 (de) | 1995-09-15 | 1997-03-20 | Merck Patent Gmbh | Cyclische Adhäsionsinhibitoren |
| AR004010A1 (es) | 1995-10-11 | 1998-09-30 | Glaxo Group Ltd | Compuestos heterociclicos |
| GB9523675D0 (en) | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| ATE225343T1 (de) | 1995-12-20 | 2002-10-15 | Hoffmann La Roche | Matrix-metalloprotease inhibitoren |
| AU1441497A (en) | 1996-01-23 | 1997-08-20 | Novartis Ag | Pyrrolopyrimidines and processes for their preparation |
| JP3406763B2 (ja) | 1996-01-30 | 2003-05-12 | 東レ・ダウコーニング・シリコーン株式会社 | シリコーンゴム組成物 |
| GB9603097D0 (en) | 1996-02-14 | 1996-04-10 | Zeneca Ltd | Quinazoline compounds |
| GB9603095D0 (en) | 1996-02-14 | 1996-04-10 | Zeneca Ltd | Quinazoline derivatives |
| DE19629652A1 (de) | 1996-03-06 | 1998-01-29 | Thomae Gmbh Dr K | 4-Amino-pyrimidin-Derivate, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| DE19608588A1 (de) | 1996-03-06 | 1997-09-11 | Thomae Gmbh Dr K | Pyrimido [5,4-d]pyrimidine, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| WO1997034895A1 (de) | 1996-03-15 | 1997-09-25 | Novartis Ag | NEUE N-7 HETEROCYCLYL-PYRROLO[2,3-d]PYRIMIDINE UND IHRE VERWENDUNG |
| EA001595B1 (ru) | 1996-04-12 | 2001-06-25 | Варнер-Ламберт Компани | Необратимые ингибиторы тирозинкиназ |
| GB9607729D0 (en) | 1996-04-13 | 1996-06-19 | Zeneca Ltd | Quinazoline derivatives |
| CA2258548C (en) | 1996-06-24 | 2005-07-26 | Pfizer Inc. | Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases |
| EP0818442A3 (en) | 1996-07-12 | 1998-12-30 | Pfizer Inc. | Cyclic sulphone derivatives as inhibitors of metalloproteinases and of the production of tumour necrosis factor |
| AU735648B2 (en) | 1996-07-12 | 2001-07-12 | Ariad Pharmaceuticals, Inc. | Materials and method for treating or preventing pathogenic fungal infection |
| HRP970371A2 (en) | 1996-07-13 | 1998-08-31 | Kathryn Jane Smith | Heterocyclic compounds |
| EA199900021A1 (ru) | 1996-07-13 | 1999-08-26 | Глаксо, Груп Лимитед | Бициклические гетероароматические соединения в качестве ингибиторов протеинтирозинкиназы |
| AR007857A1 (es) | 1996-07-13 | 1999-11-24 | Glaxo Group Ltd | Compuestos heterociclicos fusionados como inhibidores de proteina tirosina quinasa, sus metodos de preparacion, intermediarios uso en medicina ycomposiciones farmaceuticas que los contienen. |
| KR20000067904A (ko) | 1996-07-18 | 2000-11-25 | 디. 제이. 우드, 스피겔 알렌 제이 | 매트릭스 메탈로프로테아제의 포스피네이트계 억제제 |
| US6111090A (en) | 1996-08-16 | 2000-08-29 | Schering Corporation | Mammalian cell surface antigens; related reagents |
| ES2308787T3 (es) | 1996-08-16 | 2008-12-01 | Schering Corporation | Antigenos de superficie de celular de mamiferos; reactivos relacionados. |
| KR20000068248A (ko) | 1996-08-23 | 2000-11-25 | 디. 제이. 우드, 스피겔 알렌 제이 | 아릴설포닐아미노 하이드록삼산 유도체 |
| WO1998007726A1 (en) | 1996-08-23 | 1998-02-26 | Novartis Ag | Substituted pyrrolopyrimidines and processes for their preparation |
| US6251911B1 (en) | 1996-10-02 | 2001-06-26 | Novartis Ag | Pyrimidine derivatives and processes for the preparation thereof |
| AU4779897A (en) | 1996-10-02 | 1998-04-24 | Novartis Ag | Fused pyrazole derivatives and processes for their preparation |
| ID18494A (id) | 1996-10-02 | 1998-04-16 | Novartis Ag | Turunan pirazola leburan dan proses pembuatannya |
| EP0837063A1 (en) | 1996-10-17 | 1998-04-22 | Pfizer Inc. | 4-Aminoquinazoline derivatives |
| GB9621757D0 (en) | 1996-10-18 | 1996-12-11 | Ciba Geigy Ag | Phenyl-substituted bicyclic heterocyclyl derivatives and their use |
| JP3338064B2 (ja) | 1997-01-06 | 2002-10-28 | ファイザー・インク | 環状スルホン誘導体 |
| NZ336840A (en) | 1997-02-03 | 2001-01-26 | Pfizer Prod Inc | Arylsulfonylamino hydroxamic acid derivatives useful in the treatment of tumor necrosis factor and matrix metalloproteinase mediated diseases |
| WO1998033798A2 (en) | 1997-02-05 | 1998-08-06 | Warner Lambert Company | Pyrido[2,3-d]pyrimidines and 4-amino-pyrimidines as inhibitors of cell proliferation |
| JP2000507975A (ja) | 1997-02-07 | 2000-06-27 | ファイザー・インク | N−ヒドロキシ−β−スルホニルプロピオンアミド誘導体類及びそれらのマトリックスメタロプロテイナーゼ阻害薬としての使用 |
| EP0960098A1 (en) | 1997-02-11 | 1999-12-01 | Pfizer Inc. | Arylsulfonyl hydroxamic acid derivatives |
| CO4950519A1 (es) | 1997-02-13 | 2000-09-01 | Novartis Ag | Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion |
| US6150395A (en) | 1997-05-30 | 2000-11-21 | The Regents Of The University Of California | Indole-3-carbinol (I3C) derivatives and methods |
| AU8689298A (en) | 1997-08-05 | 1999-03-01 | Sugen, Inc. | Tricyclic quinoxaline derivatives as protein tyrosine kinase inhibitors |
| CA2299355C (en) | 1997-08-08 | 2005-09-27 | Pfizer Products Inc. | Aryloxyarylsulfonylamino hydroxamic acid derivatives |
| US6323208B1 (en) * | 1997-09-05 | 2001-11-27 | Pfizer Inc | Atropisomers of 2,3-disubstituted-(5.6)-heteroaryl fused-pyrimidin-4-ones |
| JP2001520039A (ja) | 1997-10-21 | 2001-10-30 | ヒューマン ジノーム サイエンシーズ, インコーポレイテッド | ヒト腫瘍壊死因子レセプター様タンパク質、tr11,tr11sv1およびtr11sv2 |
| GB9725782D0 (en) | 1997-12-05 | 1998-02-04 | Pfizer Ltd | Therapeutic agents |
| GB9800575D0 (en) | 1998-01-12 | 1998-03-11 | Glaxo Group Ltd | Heterocyclic compounds |
| RS49779B (sr) | 1998-01-12 | 2008-06-05 | Glaxo Group Limited, | Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze |
| GB9801690D0 (en) | 1998-01-27 | 1998-03-25 | Pfizer Ltd | Therapeutic agents |
| AU2591599A (en) | 1998-02-09 | 1999-08-23 | Genentech Inc. | Novel tumor necrosis factor receptor homolog and nucleic acids encoding the same |
| CA2322311C (en) | 1998-03-04 | 2009-10-13 | Bristol-Myers Squibb Company | Heterocyclo-substituted imidazopyrazine protein tyrosine kinase inhibitors |
| PA8469501A1 (es) | 1998-04-10 | 2000-09-29 | Pfizer Prod Inc | Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico |
| PA8469401A1 (es) | 1998-04-10 | 2000-05-24 | Pfizer Prod Inc | Derivados biciclicos del acido hidroxamico |
| SK287132B6 (sk) | 1998-05-29 | 2009-12-07 | Sugen, Inc. | Farmaceutická kompozícia obsahujúca pyrolom substituovaný 2-indolinón, súprava obsahujúca uvedenú kompozíciu a použitie pyrolom substituovaného 2-indolinónu |
| UA60365C2 (uk) | 1998-06-04 | 2003-10-15 | Пфайзер Продактс Інк. | Похідні ізотіазолу, спосіб їх одержання, фармацевтична композиція та спосіб лікування гіперпроліферативного захворювання у ссавця |
| CA2336848A1 (en) | 1998-07-10 | 2000-01-20 | Merck & Co., Inc. | Novel angiogenesis inhibitors |
| CA2341409A1 (en) | 1998-08-31 | 2000-03-09 | Merck And Co., Inc. | Novel angiogenesis inhibitors |
| EP1004578B1 (en) | 1998-11-05 | 2004-02-25 | Pfizer Products Inc. | 5-oxo-pyrrolidine-2-carboxylic acid hydroxamide derivatives |
| EP1158985B1 (en) | 1999-01-13 | 2011-12-28 | Bayer HealthCare LLC | OMEGA-CARBOXY ARYL SUBSTITUTED DIPHENYL UREAS AS p38 KINASE INHIBITORS |
| CN1660840A (zh) | 1999-03-30 | 2005-08-31 | 诺瓦提斯公司 | 治疗炎性疾病的酞嗪衍生物 |
| GB9912961D0 (en) | 1999-06-03 | 1999-08-04 | Pfizer Ltd | Metalloprotease inhibitors |
| US6521424B2 (en) | 1999-06-07 | 2003-02-18 | Immunex Corporation | Recombinant expression of Tek antagonists |
| ATE324444T1 (de) | 1999-06-07 | 2006-05-15 | Immunex Corp | Tek-antagonisten |
| WO2001003720A2 (en) | 1999-07-12 | 2001-01-18 | Genentech, Inc. | Promotion or inhibition of angiogenesis and cardiovascularization by tumor necrosis factor ligand/receptor homologs |
| ATE264863T1 (de) | 1999-08-24 | 2004-05-15 | Ariad Gene Therapeutics Inc | 28-epirapaloge |
| KR100881105B1 (ko) | 1999-11-05 | 2009-02-02 | 아스트라제네카 아베 | Vegf 억제제로서의 퀴나졸린 유도체 |
| WO2001037820A2 (en) | 1999-11-24 | 2001-05-31 | Sugen, Inc. | Ionizable indolinone derivatives and their use as ptk ligands |
| US6515004B1 (en) | 1999-12-15 | 2003-02-04 | Bristol-Myers Squibb Company | N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases |
| US6727225B2 (en) | 1999-12-20 | 2004-04-27 | Immunex Corporation | TWEAK receptor |
| NZ521437A (en) | 2000-02-25 | 2004-04-30 | Immunex Corp | Integrin antagonists suitable as inhibitors of angiogenesis |
| US6630500B2 (en) | 2000-08-25 | 2003-10-07 | Cephalon, Inc. | Selected fused pyrrolocarbazoles |
| BR0116452A (pt) | 2000-12-21 | 2003-09-30 | Glaxo Group Ltd | Composto, composição farmacêutica, uso de um composto |
| US6878714B2 (en) | 2001-01-12 | 2005-04-12 | Amgen Inc. | Substituted alkylamine derivatives and methods of use |
| US7102009B2 (en) | 2001-01-12 | 2006-09-05 | Amgen Inc. | Substituted amine derivatives and methods of use |
| US7105682B2 (en) | 2001-01-12 | 2006-09-12 | Amgen Inc. | Substituted amine derivatives and methods of use |
| US20020147198A1 (en) | 2001-01-12 | 2002-10-10 | Guoqing Chen | Substituted arylamine derivatives and methods of use |
| US6995162B2 (en) | 2001-01-12 | 2006-02-07 | Amgen Inc. | Substituted alkylamine derivatives and methods of use |
| GB2382074A (en) | 2001-11-14 | 2003-05-21 | Basf Ag | Recovery of chiral tartaric acid resolving agents |
| US7307088B2 (en) | 2002-07-09 | 2007-12-11 | Amgen Inc. | Substituted anthranilic amide derivatives and methods of use |
| TWI329112B (en) | 2002-07-19 | 2010-08-21 | Bristol Myers Squibb Co | Novel inhibitors of kinases |
| EP1586551A4 (en) | 2003-01-16 | 2006-07-26 | Toray Finechemicals Co Ltd | METHOD FOR OBTAINING OPTICALLY ACTIVE DIACYLTARTIC ACIDS |
| US7618632B2 (en) | 2003-05-23 | 2009-11-17 | Wyeth | Method of treating or ameliorating an immune cell associated pathology using GITR ligand antibodies |
| US20060173033A1 (en) | 2003-07-08 | 2006-08-03 | Michaela Kneissel | Use of rapamycin and rapamycin derivatives for the treatment of bone loss |
| WO2005007190A1 (en) | 2003-07-11 | 2005-01-27 | Schering Corporation | Agonists or antagonists of the clucocorticoid-induced tumour necrosis factor receptor (gitr) or its ligand for the treatment of immune disorders, infections and cancer |
| WO2005016252A2 (en) | 2003-07-11 | 2005-02-24 | Ariad Gene Therapeutics, Inc. | Phosphorus-containing macrocycles |
| AR045134A1 (es) | 2003-07-29 | 2005-10-19 | Smithkline Beecham Plc | Compuesto de 1h - imidazo [4,5-c] piridin-ilo, composicion farmaceutica que lo comprende, proceso para prepararla, su uso para preparar dicha composicion farmaceutica, combinacion farmaceutica, uso de la combinacion farmaceutica para la preparacion de un medicamento, procedimientos para preparar dic |
| CN1839133A (zh) | 2003-08-22 | 2006-09-27 | 阿文尼尔药品公司 | 作为巨噬细胞移动抑制因子的抑制剂的取代的二氮杂萘衍生物及其在治疗人类疾病中的应用 |
| WO2005055808A2 (en) | 2003-12-02 | 2005-06-23 | Genzyme Corporation | Compositions and methods to diagnose and treat lung cancer |
| GB0409799D0 (en) | 2004-04-30 | 2004-06-09 | Isis Innovation | Method of generating improved immune response |
| US20060002932A1 (en) | 2004-06-04 | 2006-01-05 | Duke University | Methods and compositions for enhancement of immunity by in vivo depletion of immunosuppressive cell activity |
| DE602005020465D1 (de) | 2004-08-26 | 2010-05-20 | Pfizer | Enantiomerenreine aminoheteroaryl-verbindungen als proteinkinasehemmer |
| EP1799699A1 (en) | 2004-10-13 | 2007-06-27 | Wyeth | Analogs of 17-hydroxywortmannin as pi3k inhibitors |
| PT2343320T (pt) | 2005-03-25 | 2018-01-23 | Gitr Inc | Anticorpos anti-gitr e as suas utilizações |
| DK2439273T3 (da) | 2005-05-09 | 2019-06-03 | Ono Pharmaceutical Co | Humane monoklonale antistoffer til programmeret død-1(pd-1) og fremgangsmåder til behandling af cancer ved anvendelse af anti-pd-1- antistoffer alene eller i kombination med andre immunterapeutika |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| KR20080040007A (ko) | 2005-09-20 | 2008-05-07 | 화이자 프로덕츠 인크. | 티로신 키나제 억제제를 이용한 치료의 투여형 및 방법 |
| WO2007133822A1 (en) | 2006-01-19 | 2007-11-22 | Genzyme Corporation | Gitr antibodies for the treatment of cancer |
| MX2009005950A (es) | 2006-12-07 | 2009-10-12 | Genentech Inc | Compuestos inhibidores de fosfoinositido 3-quinasas y metodos de uso. |
| US8591886B2 (en) | 2007-07-12 | 2013-11-26 | Gitr, Inc. | Combination therapies employing GITR binding molecules |
| EP2205242B1 (en) | 2007-09-12 | 2015-04-15 | Genentech, Inc. | Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use |
| JP5348725B2 (ja) | 2007-10-25 | 2013-11-20 | ジェネンテック, インコーポレイテッド | チエノピリミジン化合物の製造方法 |
| CN101239913B (zh) | 2008-03-17 | 2011-03-16 | 广州辉宏生物医药科技有限公司 | 手性酒石酸类衍生物的制备方法 |
| NZ590667A (en) | 2008-07-02 | 2013-01-25 | Emergent Product Dev Seattle | Tgf-b antagonist multi-target binding proteins |
| CN102149820B (zh) | 2008-09-12 | 2014-07-23 | 国立大学法人三重大学 | 能够表达外源gitr配体的细胞 |
| KR101790802B1 (ko) | 2009-09-03 | 2017-10-27 | 머크 샤프 앤드 돔 코포레이션 | 항-gitr 항체 |
| GB0919054D0 (en) | 2009-10-30 | 2009-12-16 | Isis Innovation | Treatment of obesity |
| CA2785907A1 (en) | 2009-12-29 | 2011-07-28 | Emergent Product Development Seattle, Llc | Ron binding constructs and methods of use thereof |
| WO2012142498A2 (en) | 2011-04-13 | 2012-10-18 | Innovimmune Biotherapeutics, Inc. | Mif inhibitors and their uses |
| WO2013039954A1 (en) | 2011-09-14 | 2013-03-21 | Sanofi | Anti-gitr antibodies |
| EP2836482B1 (en) | 2012-04-10 | 2019-12-25 | The Regents of The University of California | Compositions and methods for treating cancer |
| US9745319B2 (en) | 2013-03-15 | 2017-08-29 | Araxes Pharma Llc | Irreversible covalent inhibitors of the GTPase K-Ras G12C |
| CA2904393A1 (en) | 2013-03-15 | 2014-09-25 | Araxes Pharma Llc | Covalent inhibitors of kras g12c |
| US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
| GB201312059D0 (en) | 2013-07-05 | 2013-08-21 | Univ Leuven Kath | Novel GAK modulators |
| JO3805B1 (ar) * | 2013-10-10 | 2021-01-31 | Araxes Pharma Llc | مثبطات كراس جي12سي |
| EP3055290B1 (en) * | 2013-10-10 | 2019-10-02 | Araxes Pharma LLC | Inhibitors of kras g12c |
| GB201320729D0 (en) | 2013-11-25 | 2014-01-08 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| EP3778584A1 (en) * | 2014-06-19 | 2021-02-17 | ARIAD Pharmaceuticals, Inc. | Production process of 2-chloro-4-heteroaryl-pyrimidine derivatives |
| JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| WO2016049568A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Methods and compositions for inhibition of ras |
| JP2017528498A (ja) | 2014-09-25 | 2017-09-28 | アラクセス ファーマ エルエルシー | Kras g12c変異体タンパク質のインヒビター |
| WO2016049565A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Compositions and methods for inhibition of ras |
| ES2898765T3 (es) | 2015-04-10 | 2022-03-08 | Araxes Pharma Llc | Compuestos de quinazolina sustituidos y métodos de uso de los mismos |
| US10428064B2 (en) | 2015-04-15 | 2019-10-01 | Araxes Pharma Llc | Fused-tricyclic inhibitors of KRAS and methods of use thereof |
| WO2017015562A1 (en) | 2015-07-22 | 2017-01-26 | Araxes Pharma Llc | Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins |
| US10144724B2 (en) * | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| TW201713630A (en) * | 2015-07-22 | 2017-04-16 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| EP3356347A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2017058902A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| WO2017058805A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| EP3356359B1 (en) | 2015-09-28 | 2021-10-20 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| EP3356349A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2017058728A1 (en) * | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| EP3356351A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| KR20180081596A (ko) | 2015-11-16 | 2018-07-16 | 아락세스 파마 엘엘씨 | 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법 |
| US9988357B2 (en) | 2015-12-09 | 2018-06-05 | Araxes Pharma Llc | Methods for preparation of quinazoline derivatives |
| WO2017172979A1 (en) | 2016-03-30 | 2017-10-05 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
| KR102444509B1 (ko) | 2016-05-18 | 2022-09-19 | 미라티 테라퓨틱스, 인크. | Kras g12c 억제제 |
| US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
| WO2018064510A1 (en) * | 2016-09-29 | 2018-04-05 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| EP3523289A1 (en) | 2016-10-07 | 2019-08-14 | Araxes Pharma LLC | Heterocyclic compounds as inhibitors of ras and methods of use thereof |
| CN110366550A (zh) | 2016-12-22 | 2019-10-22 | 美国安进公司 | 作为用于治疗肺癌、胰腺癌或结直肠癌的KRAS G12C抑制剂的苯并异噻唑、异噻唑并[3,4-b]吡啶、喹唑啉、酞嗪、吡啶并[2,3-d]哒嗪和吡啶并[2,3-d]嘧啶衍生物 |
| EP3573966A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Fused n-heterocyclic compounds and methods of use thereof |
| WO2018218069A1 (en) | 2017-05-25 | 2018-11-29 | Araxes Pharma Llc | Quinazoline derivatives as modulators of mutant kras, hras or nras |
| EP3788053B1 (en) | 2018-05-04 | 2024-07-10 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| MA52564A (fr) | 2018-05-10 | 2021-03-17 | Amgen Inc | Inhibiteurs de kras g12c pour le traitement du cancer |
| US11096939B2 (en) | 2018-06-01 | 2021-08-24 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
| MX2020012204A (es) | 2018-06-11 | 2021-03-31 | Amgen Inc | Inhibidores de kras g12c para tratar el cáncer. |
| US11285156B2 (en) | 2018-06-12 | 2022-03-29 | Amgen Inc. | Substituted piperazines as KRAS G12C inhibitors |
| CA3103048A1 (en) | 2018-06-21 | 2019-12-26 | Janssen Pharmaceutica Nv | Oga inhibitor compounds |
| JP2021528404A (ja) | 2018-06-21 | 2021-10-21 | ヤンセン ファーマシューティカ エヌ.ベー. | Oga阻害剤化合物 |
| JP7516029B2 (ja) * | 2018-11-16 | 2024-07-16 | アムジエン・インコーポレーテツド | Kras g12c阻害剤化合物の重要な中間体の改良合成法 |
| JP7377679B2 (ja) | 2018-11-19 | 2023-11-10 | アムジエン・インコーポレーテツド | がん治療のためのkrasg12c阻害剤及び1種以上の薬学的に活性な追加の薬剤を含む併用療法 |
| AU2019384118B2 (en) | 2018-11-19 | 2025-06-12 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
| EP3738593A1 (en) | 2019-05-14 | 2020-11-18 | Amgen, Inc | Dosing of kras inhibitor for treatment of cancers |
| WO2020236947A1 (en) | 2019-05-21 | 2020-11-26 | Amgen Inc. | Solid state forms |
| AU2020277398B2 (en) | 2019-05-21 | 2026-01-29 | Amgen Inc. | Solid state forms |
| EP4048671B1 (en) | 2019-10-24 | 2026-03-18 | Amgen Inc. | Pyridopyrimidine derivatives useful as kras g12c and kras g12d inhibitors in the treatment of cancer |
| JP2023501528A (ja) | 2019-11-14 | 2023-01-18 | アムジエン・インコーポレーテツド | Kras g12c阻害剤化合物の改善された合成 |
| JP7837865B2 (ja) | 2019-11-14 | 2026-03-31 | アムジエン・インコーポレーテツド | Kras g12c阻害剤化合物の改良合成法 |
| US20230028414A1 (en) | 2019-12-16 | 2023-01-26 | Amgen Inc. | Dosing regimen of kras g12c inhibitor |
| US11299281B2 (en) | 2020-08-03 | 2022-04-12 | Ami Industries, Inc. | Parachute assemblies with elastomeric inserts |
| DK4225755T3 (da) * | 2020-10-07 | 2026-04-07 | Amgen Inc | Fremgangsmåde til racemisering og isolering af atropisomerer af 7-chlor-6-fluor-1-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-d]pyrimidin-2,4(1 h,3 h)-dion |
| CA3201663A1 (en) * | 2020-11-20 | 2022-05-27 | Amgen Inc. | Process for preparing 7-chloro-6-fluoro-1-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-d]pyrimidine-2,4(1h,3h)-dione |
| KR20240156373A (ko) | 2022-03-07 | 2024-10-29 | 암젠 인크 | 4-메틸-2-프로판-2-일-피리딘-3-카르보니트릴의 제조 방법 |
-
2019
- 2019-11-13 JP JP2019205198A patent/JP7516029B2/ja active Active
- 2019-11-15 AR ARP190103372A patent/AR117101A1/es unknown
- 2019-11-15 CN CN201980075080.8A patent/CN113015724B/zh active Active
- 2019-11-15 PT PT198209389T patent/PT3880670T/pt unknown
- 2019-11-15 CA CA3117221A patent/CA3117221A1/en active Pending
- 2019-11-15 DK DK19820938.9T patent/DK3880670T3/da active
- 2019-11-15 CN CN202411826907.3A patent/CN119638694A/zh active Pending
- 2019-11-15 EP EP19820938.9A patent/EP3880670B1/en active Active
- 2019-11-15 IL IL318601A patent/IL318601A/en unknown
- 2019-11-15 US US16/685,841 patent/US11299491B2/en active Active
- 2019-11-15 CN CN202411826898.8A patent/CN119638693A/zh active Pending
- 2019-11-15 ES ES19820938T patent/ES2953752T3/es active Active
- 2019-11-15 LT LTEPPCT/US2019/061815T patent/LT3880670T/lt unknown
- 2019-11-15 KR KR1020257037985A patent/KR20250164341A/ko active Pending
- 2019-11-15 EP EP23174717.1A patent/EP4234546B1/en active Active
- 2019-11-15 MX MX2021005598A patent/MX2021005598A/es unknown
- 2019-11-15 WO PCT/US2019/061815 patent/WO2020102730A1/en not_active Ceased
- 2019-11-15 PL PL19820938.9T patent/PL3880670T3/pl unknown
- 2019-11-15 IL IL282682A patent/IL282682B2/en unknown
- 2019-11-15 KR KR1020217017296A patent/KR20210093276A/ko active Pending
- 2019-11-15 MA MA054233A patent/MA54233A/fr unknown
- 2019-11-15 SG SG11202104927QA patent/SG11202104927QA/en unknown
- 2019-11-15 HU HUE19820938A patent/HUE062656T2/hu unknown
- 2019-11-15 BR BR112021009384-2A patent/BR112021009384A2/pt unknown
- 2019-11-15 SI SI201930601T patent/SI3880670T1/sl unknown
- 2019-11-15 EA EA202191381A patent/EA202191381A1/ru unknown
- 2019-11-15 TW TW108141509A patent/TWI862525B/zh active
- 2019-11-15 AU AU2019381817A patent/AU2019381817B2/en active Active
- 2019-11-15 FI FIEP19820938.9T patent/FI3880670T3/fi active
-
2021
- 2021-05-12 MX MX2023007748A patent/MX2023007748A/es unknown
- 2021-05-14 CL CL2021001266A patent/CL2021001266A1/es unknown
-
2022
- 2022-03-08 US US17/689,741 patent/US12391689B2/en active Active
-
2024
- 2024-07-02 JP JP2024106605A patent/JP2024127907A/ja active Pending
- 2024-12-19 US US18/987,568 patent/US12391691B2/en active Active
-
2025
- 2025-04-22 AU AU2025202772A patent/AU2025202772A1/en active Pending
- 2025-07-25 US US19/281,019 patent/US20250368642A1/en active Pending
- 2025-07-25 US US19/281,069 patent/US20250368643A1/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20180334454A1 (en) | 2017-05-22 | 2018-11-22 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| WO2019051291A1 (en) | 2017-09-08 | 2019-03-14 | Amgen Inc. | Inhibitors of kras g12c and methods of using the same |
| WO2019213516A1 (en) | 2018-05-04 | 2019-11-07 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
Non-Patent Citations (2)
| Title |
|---|
| JANES MATTHEW R ET AL,Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor,CELL,2018年,Vol.172(3),p.578-589 |
| STATSYUK ALEXANDER V,Let K-Ras activate its own inhibitor,NAT. STRUCT. MOL. BIOL.,2018年,Vol.25(6),p.435-437 |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2024127907A (ja) * | 2018-11-16 | 2024-09-20 | アムジエン・インコーポレーテツド | Kras g12c阻害剤化合物の重要な中間体の改良合成法 |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP7516029B2 (ja) | Kras g12c阻害剤化合物の重要な中間体の改良合成法 | |
| JP7360396B2 (ja) | Kras g12c阻害剤及び同一物の使用方法 | |
| US20260028339A1 (en) | Synthesis of KRAS G12C Inhibitor Compound | |
| TWI882037B (zh) | Kras g12c抑制劑化合物之改善的合成 | |
| KR102953492B1 (ko) | Kras g12c 억제제 화합물의 개선된 합성 | |
| HK40094419A (en) | Improved synthesis of key intermediate of kras g12c inhibitor compound | |
| HK40123166A (zh) | Kras g12c抑制剂化合物的关键中间体的改善合成 | |
| HK40050247B (en) | Improved synthesis of key intermediate of kras g12c inhibitor compound | |
| HK40050247A (en) | Improved synthesis of key intermediate of kras g12c inhibitor compound | |
| EA049102B1 (ru) | Улучшенный синтез соединения, представляющего собой ингибитор kras g12c | |
| KR20260056313A (ko) | Kras g12c 억제제 화합물의 개선된 합성 | |
| HK40079912B (zh) | Kras g12c抑制剂化合物的改善的合成 | |
| HK40055588B (zh) | Kras g12c抑制剂化合物的关键中间体的改善合成 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20200117 |
|
| AA79 | Non-delivery of priority document |
Free format text: JAPANESE INTERMEDIATE CODE: A24379 Effective date: 20200324 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20221110 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20221110 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20230926 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20231003 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20231215 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20240604 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20240703 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 7516029 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |