JP2021020948A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2021020948A5 JP2021020948A5 JP2020179494A JP2020179494A JP2021020948A5 JP 2021020948 A5 JP2021020948 A5 JP 2021020948A5 JP 2020179494 A JP2020179494 A JP 2020179494A JP 2020179494 A JP2020179494 A JP 2020179494A JP 2021020948 A5 JP2021020948 A5 JP 2021020948A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 6
- PETFFVPRVBVQKQ-IBGZPJMESA-N CC(C)c1nccc(C)c1N(c(c(C(N(CC1)[C@@H](C)CN1C(OC(C)(C)C)=O)=N1)c2)nc(-c(c(F)ccc3)c3O)c2F)C1=O Chemical compound CC(C)c1nccc(C)c1N(c(c(C(N(CC1)[C@@H](C)CN1C(OC(C)(C)C)=O)=N1)c2)nc(-c(c(F)ccc3)c3O)c2F)C1=O PETFFVPRVBVQKQ-IBGZPJMESA-N 0.000 description 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022099389A JP7495444B2 (ja) | 2017-05-22 | 2022-06-21 | Kras g12c阻害剤及びその使用方法 |
| JP2024083128A JP7717224B2 (ja) | 2017-05-22 | 2024-05-22 | Kras g12c阻害剤及びその使用方法 |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762509629P | 2017-05-22 | 2017-05-22 | |
| US62/509,629 | 2017-05-22 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018097648A Division JP6785819B2 (ja) | 2017-05-22 | 2018-05-22 | Kras g12c阻害剤及びその使用方法 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022099389A Division JP7495444B2 (ja) | 2017-05-22 | 2022-06-21 | Kras g12c阻害剤及びその使用方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021020948A JP2021020948A (ja) | 2021-02-18 |
| JP2021020948A5 true JP2021020948A5 (enExample) | 2021-11-11 |
| JP7095052B2 JP7095052B2 (ja) | 2022-07-04 |
Family
ID=62620997
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018097648A Active JP6785819B2 (ja) | 2017-05-22 | 2018-05-22 | Kras g12c阻害剤及びその使用方法 |
| JP2020179494A Active JP7095052B2 (ja) | 2017-05-22 | 2020-10-27 | Kras g12c阻害剤及びその使用方法 |
| JP2022099389A Active JP7495444B2 (ja) | 2017-05-22 | 2022-06-21 | Kras g12c阻害剤及びその使用方法 |
| JP2024083128A Active JP7717224B2 (ja) | 2017-05-22 | 2024-05-22 | Kras g12c阻害剤及びその使用方法 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018097648A Active JP6785819B2 (ja) | 2017-05-22 | 2018-05-22 | Kras g12c阻害剤及びその使用方法 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022099389A Active JP7495444B2 (ja) | 2017-05-22 | 2022-06-21 | Kras g12c阻害剤及びその使用方法 |
| JP2024083128A Active JP7717224B2 (ja) | 2017-05-22 | 2024-05-22 | Kras g12c阻害剤及びその使用方法 |
Country Status (39)
Families Citing this family (259)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CR20190338A (es) | 2016-12-22 | 2019-09-09 | Amgen Inc | Inhibidores de kras g12c y métodos para su uso |
| UA127968C2 (uk) * | 2017-05-22 | 2024-02-28 | Емджен Інк. | Інгібітори g12c kras і способи їх застосування |
| US10640504B2 (en) | 2017-09-08 | 2020-05-05 | Amgen Inc. | Inhibitors of KRAS G12C and methods of using the same |
| BR112020020307A2 (pt) | 2018-04-04 | 2021-01-12 | Arvinas Operations, Inc. | Moduladores de proteólise e métodos de uso associados |
| MX2020010836A (es) * | 2018-05-04 | 2021-01-08 | Amgen Inc | Inhibidores de kras g12c y métodos para su uso. |
| EP3788053B1 (en) | 2018-05-04 | 2024-07-10 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| TW202012415A (zh) | 2018-05-08 | 2020-04-01 | 瑞典商阿斯特捷利康公司 | 化學化合物 |
| WO2019217691A1 (en) * | 2018-05-10 | 2019-11-14 | Amgen Inc. | Kras g12c inhibitors for the treatment of cancer |
| WO2019232419A1 (en) | 2018-06-01 | 2019-12-05 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| AU2019284472B2 (en) | 2018-06-11 | 2024-05-30 | Amgen Inc. | KRAS G12C inhibitors for treating cancer |
| JP7369719B2 (ja) | 2018-06-12 | 2023-10-26 | アムジエン・インコーポレーテツド | KRas G12C阻害剤及びそれを使用する方法 |
| SG11202012973RA (en) | 2018-06-27 | 2021-01-28 | Bristol Myers Squibb Co | Naphthyridinone compounds useful as t cell activators |
| CN112654621B (zh) | 2018-06-27 | 2024-05-14 | 百时美施贵宝公司 | 可作为t细胞活化剂的经取代萘啶酮化合物 |
| WO2020085504A1 (ja) | 2018-10-26 | 2020-04-30 | 大鵬薬品工業株式会社 | 光照射ザンドマイヤー反応を用いたクロロアゾールカルボキシレート誘導体の製造方法 |
| 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 |
| JP7454572B2 (ja) | 2018-11-19 | 2024-03-22 | アムジエン・インコーポレーテツド | Kras g12c阻害剤及びその使用方法 |
| US12503467B2 (en) * | 2018-12-10 | 2025-12-23 | Ideaya Biosciences, Inc. | 2-oxoquinazoline derivatives as methionine adenosyltransferase 2A inhibitors |
| CN111484477B (zh) * | 2019-01-29 | 2022-07-08 | 博瑞生物医药(苏州)股份有限公司 | 一种苯并吡啶酮杂环化合物及其用途 |
| CN113382774A (zh) * | 2019-02-12 | 2021-09-10 | 诺华股份有限公司 | 包含tno155和krasg12c抑制剂的药物组合 |
| ES3010507T3 (en) | 2019-03-05 | 2025-04-03 | Astrazeneca Ab | Fused tricyclic compounds useful as anticancer agents |
| ES3034869T3 (en) * | 2019-04-22 | 2025-08-25 | Univ Pittsburgh Commonwealth Sys Higher Education | Tg02 for use in treating gliomas in pediatric subjects |
| CN114025772B (zh) | 2019-04-24 | 2026-07-17 | 纪念斯隆凯特琳癌症中心 | 用于治疗ras突变体癌症的组合物和方法 |
| EP3964516A4 (en) * | 2019-04-28 | 2023-01-11 | Genfleet Therapeutics (Shanghai) Inc. | OXAAZACHUINAZOLINE-7( 8H)-KETONE COMPOUND, PROCESS FOR ITS PRODUCTION AND ITS PHARMACEUTICAL APPLICATION |
| EP3738593A1 (en) * | 2019-05-14 | 2020-11-18 | Amgen, Inc | Dosing of kras inhibitor for treatment of cancers |
| EP3972973A1 (en) * | 2019-05-21 | 2022-03-30 | Amgen Inc. | Solid state forms |
| US12252486B2 (en) | 2019-05-21 | 2025-03-18 | Amgen Inc. | Solid state forms |
| BR112021023136A2 (pt) | 2019-05-21 | 2022-01-04 | Inventisbio Co Ltd | Compostos heterocíclicos, métodos de preparação e usos dos mesmos |
| CN118745177A (zh) * | 2019-05-29 | 2024-10-08 | 上海翰森生物医药科技有限公司 | 含氮杂环类衍生物调节剂、其制备方法和应用 |
| CN112552294B (zh) * | 2019-09-10 | 2023-12-19 | 上海翰森生物医药科技有限公司 | 含哌嗪杂环类衍生物抑制剂、其制备方法和应用 |
| CN113396147B (zh) * | 2019-05-31 | 2024-06-18 | 上海翰森生物医药科技有限公司 | 芳香杂环类衍生物调节剂、其制备方法和应用 |
| AU2020308353B9 (en) * | 2019-06-24 | 2024-01-25 | Guangdong Newopp Biopharmaceuticals Co., Ltd. | Heterocyclic compounds as inhibitors of KRAS G12C |
| WO2020259573A1 (zh) * | 2019-06-25 | 2020-12-30 | 南京明德新药研发有限公司 | 作为kras g12c突变蛋白抑制剂的七元杂环类衍生物 |
| CN110256421A (zh) * | 2019-06-26 | 2019-09-20 | 微境生物医药科技(上海)有限公司 | Kras-g12c抑制剂 |
| WO2021000885A1 (zh) * | 2019-07-01 | 2021-01-07 | 江苏恒瑞医药股份有限公司 | 喹唑啉酮类衍生物、其制备方法及其在医药上的应用 |
| GB2606804B (en) | 2019-07-17 | 2023-12-27 | 2692372 Ontario Inc | Benzenesulfonamide derivatives and uses thereof |
| CN112300194B (zh) * | 2019-07-30 | 2022-01-14 | 上海凌达生物医药有限公司 | 一类稠环吡啶酮类化合物、制备方法和用途 |
| IL290276B2 (en) * | 2019-08-02 | 2026-05-01 | Shanghai Jemincare Pharmaceuticals Co Ltd | Tetracyclic compounds, method for their preparation and use |
| US20210040089A1 (en) * | 2019-08-07 | 2021-02-11 | Jacobio Pharmaceuticals Co., Ltd. | Kras mutant protein inhibitors |
| CN112390788A (zh) * | 2019-08-13 | 2021-02-23 | 苏州闻天医药科技有限公司 | 一种用于抑制krasg12c突变蛋白的化合物及其制备方法和用途 |
| CN112390797A (zh) * | 2019-08-15 | 2021-02-23 | 微境生物医药科技(上海)有限公司 | 新型螺环类K-Ras G12C抑制剂 |
| CN112390796B (zh) * | 2019-08-19 | 2023-06-27 | 贝达药业股份有限公司 | Kras g12c抑制剂及其在医药上的应用 |
| AR119821A1 (es) | 2019-08-28 | 2022-01-12 | Bristol Myers Squibb Co | Compuestos de piridopirimidinonilo sustituidos útiles como activadores de células t |
| CN114615981B (zh) | 2019-08-29 | 2024-04-12 | 米拉蒂治疗股份有限公司 | Kras g12d抑制剂 |
| US20220259150A1 (en) | 2019-09-11 | 2022-08-18 | Chiral Quest (Suzhou) Co., Ltd. | Synthesis method applied to kras inhibitor drug heterocyclic intermediate |
| US12122787B2 (en) | 2019-09-20 | 2024-10-22 | Shanghai Jemincare Pharmaceuticals Co., Ltd | Fused pyridone compound, and preparation method therefor and use thereof |
| CN116947885B (zh) * | 2019-09-20 | 2026-01-23 | 上海济煜医药科技股份有限公司 | 稠合吡啶酮类化合物及其制备方法和应用 |
| CN114761012B (zh) * | 2019-09-24 | 2025-03-21 | 米拉蒂治疗股份有限公司 | 组合疗法 |
| BR112022006394A2 (pt) | 2019-10-02 | 2022-07-26 | Tolremo Therapeutics Ag | Derivados heterocíclicos, composições farmacêuticas e seu uso no tratamento ou melhora do câncer |
| US20240139193A1 (en) | 2019-10-15 | 2024-05-02 | Amgen Inc. | Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers |
| AU2020369569B2 (en) * | 2019-10-24 | 2026-06-18 | Amgen Inc. | Pyridopyrimidine derivatives useful as KRAS G12C and KRAS G12D inhibitors in the treatment of cancer |
| CN112225734B (zh) * | 2019-10-25 | 2021-12-07 | 南京瑞捷医药科技有限公司 | Kras g12c抑制剂及其用途 |
| MD4051678T2 (en) * | 2019-10-28 | 2026-07-31 | Merck Sharp & Dohme Llc | Small molecule inhibitors of the KRAS G12C mutant |
| BR112022008375A2 (pt) * | 2019-10-30 | 2022-07-12 | Genfleet Therapeutics Shanghai Inc | Composto cíclico heterocíclico fundido substituído, método de preparação e uso farmacêutico deste |
| WO2021085653A1 (en) | 2019-10-31 | 2021-05-06 | Taiho Pharmaceutical Co., Ltd. | 4-aminobut-2-enamide derivatives and salts thereof |
| MX2022005359A (es) | 2019-11-04 | 2022-06-02 | Revolution Medicines Inc | Inhibidores de ras. |
| WO2021091956A1 (en) | 2019-11-04 | 2021-05-14 | Revolution Medicines, Inc. | Ras inhibitors |
| CN121471132A (zh) | 2019-11-04 | 2026-02-06 | 锐新医药公司 | Ras抑制剂 |
| CA3161156A1 (en) | 2019-11-14 | 2021-05-20 | Amgen Inc. | Improved synthesis of kras g12c inhibitor compound |
| EP4700030A3 (en) * | 2019-11-14 | 2026-03-18 | Amgen, Inc. | Improved synthesis of kras g12c inhibitor compound |
| WO2021093758A1 (zh) * | 2019-11-15 | 2021-05-20 | 四川海思科制药有限公司 | 一种嘧啶并环衍生物及其在医药上的应用 |
| CN114980976A (zh) | 2019-11-27 | 2022-08-30 | 锐新医药公司 | 共价ras抑制剂及其用途 |
| WO2021108682A1 (en) | 2019-11-27 | 2021-06-03 | Turning Point Therapeutics, Inc. | Combination therapy involving diaryl macrocyclic compounds |
| WO2021106231A1 (en) * | 2019-11-29 | 2021-06-03 | Taiho Pharmaceutical Co., Ltd. | A compound having inhibitory activity against kras g12d mutation |
| EP4067343A4 (en) | 2019-11-29 | 2024-01-03 | Taiho Pharmaceutical Co., Ltd. | NEW PHENOLIC COMPOUND OR SALT THEREOF |
| CN111377918B (zh) * | 2019-11-29 | 2021-03-02 | 苏州信诺维医药科技有限公司 | 一种kras抑制剂化合物 |
| WO2021104431A1 (zh) * | 2019-11-29 | 2021-06-03 | 苏州信诺维医药科技股份有限公司 | Kras g12c抑制剂化合物及其用途 |
| WO2021113595A1 (en) * | 2019-12-06 | 2021-06-10 | Beta Pharma, Inc. | Phosphorus derivatives as kras inhibitors |
| MX2022007051A (es) * | 2019-12-10 | 2022-12-06 | Univ Texas | Composiciones y metodos para analogos de 7-(piperazin-1-il)pirazol o[1,5-a]pirimidina sustituidos como inhibidores de kras. |
| US20230028414A1 (en) | 2019-12-16 | 2023-01-26 | Amgen Inc. | Dosing regimen of kras g12c inhibitor |
| WO2021120045A1 (en) | 2019-12-18 | 2021-06-24 | InventisBio Co., Ltd. | Heterocyclic compounds, preparation methods and uses thereof |
| CA3165238A1 (en) * | 2019-12-19 | 2021-06-24 | Jacobio Pharmaceuticals Co., Ltd. | Kras mutant protein inhibitors |
| WO2021120890A1 (en) | 2019-12-20 | 2021-06-24 | Novartis Ag | Pyrazolyl derivatives useful as anti-cancer agents |
| CA3162979A1 (en) | 2019-12-23 | 2021-07-01 | Upender Velaparthi | Substituted piperazine derivatives useful as t cell activators |
| AR120823A1 (es) | 2019-12-23 | 2022-03-23 | Bristol Myers Squibb Co | Compuestos bicíclicos sustituidos útiles como activadores de células t |
| IL294148A (en) | 2019-12-23 | 2022-08-01 | Bristol Myers Squibb Co | Substituted quinazolinyl compounds are useful as t-cell activators |
| WO2021139678A1 (zh) * | 2020-01-07 | 2021-07-15 | 广州百霆医药科技有限公司 | 吡啶并嘧啶类kras g12c突变蛋白抑制剂 |
| WO2021139748A1 (en) * | 2020-01-08 | 2021-07-15 | Ascentage Pharma (Suzhou) Co., Ltd. | Spirocyclic tetrahydroquinazolines |
| CN111205286B (zh) * | 2020-01-13 | 2022-12-13 | 中科苏州药物研究院 | 作为kras g12c突变蛋白抑制剂的腈甲基哌嗪类衍生物及其应用 |
| CN114671866A (zh) * | 2020-12-25 | 2022-06-28 | 苏州泽璟生物制药股份有限公司 | 芳基或杂芳基并吡啶酮或嘧啶酮类衍生物及其制备方法和应用 |
| WO2021150613A1 (en) | 2020-01-20 | 2021-07-29 | Incyte Corporation | Spiro compounds as inhibitors of kras |
| WO2021147967A1 (zh) * | 2020-01-21 | 2021-07-29 | 南京明德新药研发有限公司 | 作为kras抑制剂的大环类化合物 |
| GB202001344D0 (en) | 2020-01-31 | 2020-03-18 | Redx Pharma Plc | Ras Inhibitors |
| CN112159405B (zh) | 2020-02-04 | 2021-09-14 | 广州必贝特医药技术有限公司 | 吡啶并嘧啶酮类化合物及其应用 |
| US11618751B1 (en) | 2022-03-25 | 2023-04-04 | Ventus Therapeutics U.S., Inc. | Pyrido-[3,4-d]pyridazine amine derivatives useful as NLRP3 derivatives |
| CN113248521B (zh) * | 2020-02-11 | 2023-07-18 | 上海和誉生物医药科技有限公司 | 一种k-ras g12c抑制剂及其制备方法和应用 |
| EP4112606A4 (en) * | 2020-02-24 | 2024-04-10 | Shanghai Zheye Biotechnology Co., Ltd. | Aromatic compound and use thereof in preparing antineoplastic drugs |
| CN114901663B (zh) * | 2020-03-02 | 2024-07-02 | 上海喆邺生物科技有限公司 | 一类芳香杂环类化合物及其在药物中的应用 |
| 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 |
| JP7618684B2 (ja) | 2020-04-03 | 2025-01-21 | インテル コーポレイション | ビデオ復号エラーを識別する方法及び機器 |
| AU2021248363B2 (en) * | 2020-04-03 | 2024-02-15 | Medshine Discovery Inc. | Octahydropyrazinodiazanaphthyridine dione compounds |
| WO2021215544A1 (en) | 2020-04-24 | 2021-10-28 | Taiho Pharmaceutical Co., Ltd. | Kras g12d protein inhibitors |
| US12702658B2 (en) | 2020-04-24 | 2026-08-11 | Taiho Pharmaceutical Co., Ltd. | Anticancer combination therapy with N-(1-acryloyl-azetidin-3-yl)-2-((1H-indazol-3-yl)amino)methyl)-1H-imidazole-5-carboxamide inhibitor of KRAS-G12C |
| WO2021218939A1 (zh) * | 2020-04-28 | 2021-11-04 | 贝达药业股份有限公司 | 稠环化合物及其在医药上的应用 |
| WO2021231526A1 (en) | 2020-05-13 | 2021-11-18 | Incyte Corporation | Fused pyrimidine compounds as kras inhibitors |
| WO2021235812A1 (ko) | 2020-05-18 | 2021-11-25 | 웰마커바이오 주식회사 | Ron 돌연변이와 관련된 비소세포 폐암 예방 또는 치료용 약학 조성물 및 이를 이용한 방법 |
| CN112574199B (zh) * | 2020-05-20 | 2021-05-18 | 首药控股(北京)股份有限公司 | Kras-G12C抑制剂杂环化合物 |
| US20230183235A1 (en) * | 2020-05-20 | 2023-06-15 | Teva Pharmaceuticals International Gmbh | Solid state forms of amg-510 and process for preparation thereof |
| CN116034106B (zh) | 2020-06-02 | 2025-11-04 | 勃林格殷格翰国际有限公司 | 用于治疗癌症的环状2-氨基-3-氰基噻吩及衍生物 |
| WO2021244555A1 (zh) * | 2020-06-02 | 2021-12-09 | 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 |
| WO2021249563A1 (zh) * | 2020-06-12 | 2021-12-16 | 苏州泽璟生物制药股份有限公司 | 芳基或杂芳基并吡啶酮或嘧啶酮类衍生物及其制备方法和应用 |
| CN115916194A (zh) * | 2020-06-18 | 2023-04-04 | 锐新医药公司 | 用于延迟、预防和治疗针对ras抑制剂的获得性抗性的方法 |
| JP2023531049A (ja) | 2020-06-24 | 2023-07-20 | 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 | Sos1阻害剤及びkras g12c阻害剤を含む抗がん剤併用療法 |
| WO2021260110A1 (en) | 2020-06-25 | 2021-12-30 | Tolremo Therapeutics Ag | Heterocyclic derivatives, pharmaceutical compositions and their use in the treatment, amelioration or prevention of fibrotic disease |
| AU2021298154A1 (en) * | 2020-06-25 | 2023-02-23 | Tolremo Therapeutics Ag | Combination of a CBP/p300 bromodomain inhibitor and a KRAS inhibitor for the treatment of cancer |
| 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 |
| CN113980032B (zh) * | 2020-07-27 | 2023-06-16 | 江苏恒瑞医药股份有限公司 | 稠合四环类衍生物、其制备方法及其在医药上的应用 |
| WO2022028346A1 (zh) | 2020-08-02 | 2022-02-10 | 上海喆邺生物科技有限公司 | 一种芳香类化合物及其在抗肿瘤药物中的应用 |
| CN114075195B (zh) * | 2020-08-21 | 2026-04-28 | 广东东阳光药业股份有限公司 | 嘧啶酮衍生物及其在药物中的应用 |
| CN116406363B (zh) * | 2020-08-21 | 2025-06-20 | 浙江海正药业股份有限公司 | 四环类衍生物、其制备方法及其医药上的用途 |
| CA3191279A1 (en) | 2020-08-28 | 2022-03-03 | Yi Liu | Heterocyclic compounds and uses thereof |
| WO2022047093A1 (en) * | 2020-08-28 | 2022-03-03 | Incyte Corporation | Vinyl imidazole compounds as inhibitors of kras |
| EP4208261A1 (en) | 2020-09-03 | 2023-07-12 | Revolution Medicines, Inc. | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| IL301298A (en) | 2020-09-15 | 2023-05-01 | Revolution Medicines Inc | Indole derivatives as RAS inhibitors in cancer therapy |
| WO2022066805A1 (en) | 2020-09-23 | 2022-03-31 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| WO2022072783A1 (en) | 2020-10-02 | 2022-04-07 | Incyte Corporation | Bicyclic dione compounds as inhibitors of kras |
| IL301517A (en) | 2020-10-07 | 2023-05-01 | Amgen Inc | A method for preparing the racemate and isolating atropisomers of 7-chloro-6-fluoro-1-(2-isopropyl-4-methylpyridin-3-yl)pyrido[3,2-D]pyrimidine-4,2(1H,3H)-dione |
| JP7654071B2 (ja) | 2020-10-20 | 2025-03-31 | アムジエン・インコーポレーテツド | 複素環スピロ化合物及び使用方法 |
| WO2022093856A1 (en) | 2020-10-27 | 2022-05-05 | Amgen Inc. | Heterocyclic spiro compounds and methods of use |
| KR102975432B1 (ko) * | 2020-11-13 | 2026-06-10 | 제넨테크, 인크. | 고형 종양 치료를 위한 krasg12c 억제제 및 vegf 억제제를 포함하는 방법 및 조성물 |
| MX2023005823A (es) | 2020-11-20 | 2023-05-31 | Amgen Inc | Procedimiento para preparar 7-cloro-6-fluoro-1-(2-isopropil-4-meti lpiridin-3-il)pirido[2,3-d]pirimidino-2,4(1h,3h)-diona. |
| WO2022109487A1 (en) | 2020-11-23 | 2022-05-27 | Merck Sharp & Dohme Corp. | Spirocyclic-substituted 6,7-dihydro-pyrano[2,3-d]pyrimidine inhibitors of kras g12c mutant |
| CN116390919B (zh) * | 2020-11-24 | 2025-12-23 | 杭州多域生物技术有限公司 | 一种芳香化合物、其制备方法及应用 |
| CN116390915B (zh) * | 2020-11-24 | 2026-02-10 | 杭州多域生物技术有限公司 | 一种芳香化合物、其制备方法及应用 |
| JP2023551006A (ja) * | 2020-11-26 | 2023-12-06 | 上▲海▼翰森生物医▲薬▼科技有限公司 | 窒素含有複素環誘導体の塩、結晶、並びにその調製方法、及び使用 |
| CN116171155B (zh) * | 2020-12-08 | 2024-09-17 | 上海和誉生物医药科技有限公司 | 吡啶并[2,3-d]嘧啶-2(1H)-酮衍生物及其制备方法和应用 |
| US20250195533A1 (en) * | 2020-12-11 | 2025-06-19 | Erasca, Inc. | Combination therapies for the treatment of cancer |
| WO2022127847A1 (zh) * | 2020-12-17 | 2022-06-23 | 广东东阳光药业有限公司 | 嘧啶酮衍生物及其在药物中的应用 |
| TWI795129B (zh) * | 2020-12-18 | 2023-03-01 | 大陸商正大天晴藥業集團股份有限公司 | 吡啶并嘧啶酮類化合物 |
| US20230107642A1 (en) | 2020-12-18 | 2023-04-06 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| US20240100172A1 (en) | 2020-12-21 | 2024-03-28 | Hangzhou Jijing Pharmaceutical Technology Limited | Methods and compounds for targeted autophagy |
| AU2021409816A1 (en) | 2020-12-22 | 2023-07-06 | Qilu Regor Therapeutics Inc. | Sos1 inhibitors and uses thereof |
| CN114685502A (zh) * | 2020-12-25 | 2022-07-01 | 由理生物医药(上海)有限公司 | 作为kras-g12c抑制剂的螺环类化合物 |
| WO2022150628A1 (en) | 2021-01-08 | 2022-07-14 | Amgen Inc. | Use of a kras g12c inhibitor in treating cancers |
| CN116964057A (zh) * | 2021-03-10 | 2023-10-27 | 贝达医药公司 | 作为kras抑制剂的吡啶并嘧啶衍生物 |
| US12697337B2 (en) | 2021-03-11 | 2026-08-04 | InventisBio Co., Ltd. | Solid dispersions |
| CN113018415B (zh) * | 2021-03-17 | 2022-07-01 | 遵义医科大学 | 一种药物组合及其应用 |
| WO2022204112A1 (en) | 2021-03-22 | 2022-09-29 | Incyte Corporation | Imidazole and triazole kras inhibitors |
| US11319319B1 (en) | 2021-04-07 | 2022-05-03 | Ventus Therapeutics U.S., Inc. | Compounds for inhibiting NLRP3 and uses thereof |
| CA3212085C (en) | 2021-04-07 | 2025-02-11 | Tolremo Therapeutics Ag | HETEROCYCLIC DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND THEIR USE IN THE TREATMENT OR RELIEF OF CANCER |
| 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 |
| US20240262842A1 (en) * | 2021-04-27 | 2024-08-08 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras g12c mutant |
| EP4329888A1 (en) | 2021-04-29 | 2024-03-06 | Amgen Inc. | 2-aminobenzothiazole compounds and methods of use thereof |
| PE20240088A1 (es) | 2021-05-05 | 2024-01-16 | Revolution Medicines Inc | Inhibidores de ras |
| IL308195A (en) | 2021-05-05 | 2024-01-01 | Revolution Medicines Inc | RAS inhibitors for cancer treatment |
| WO2022246069A1 (en) | 2021-05-19 | 2022-11-24 | Teva Pharmaceuticals International Gmbh | Process for preparation of sotorasib and solid state form thereof |
| AR125921A1 (es) * | 2021-05-19 | 2023-08-23 | Genentech Inc | Terapia de combinación |
| CN118076612A (zh) * | 2021-05-25 | 2024-05-24 | 医睿世康药业研发公司 | 含硫杂芳族三环kras抑制剂 |
| CA3221390A1 (en) * | 2021-05-25 | 2022-12-01 | Erasca, Inc. | Sulfur-containing heteroaromatic tricyclic kras inhibitors |
| WO2022266206A1 (en) | 2021-06-16 | 2022-12-22 | Erasca, Inc. | Kras inhibitor conjugates |
| AR126166A1 (es) * | 2021-06-18 | 2023-09-27 | Antengene Discovery Ltd | Combinación de un inhibidor de erk y un inhibidor de kras y usos de estos |
| TW202317100A (zh) | 2021-06-23 | 2023-05-01 | 瑞士商諾華公司 | 包含kras g12c抑制劑的藥物組合及其用於治療癌症之用途 |
| US20240287066A1 (en) | 2021-06-24 | 2024-08-29 | Sandoz Ag | Crystalline Form of Sotorasib |
| EP4227305A1 (en) | 2022-02-10 | 2023-08-16 | Sandoz AG | Crystalline form of sotorasib |
| WO2023283213A1 (en) | 2021-07-07 | 2023-01-12 | Incyte Corporation | Tricyclic compounds as inhibitors of kras |
| CA3224841A1 (en) | 2021-07-14 | 2023-01-19 | Zhenwu Li | Tricyclic compounds as inhibitors of kras |
| US20240417412A1 (en) * | 2021-08-10 | 2024-12-19 | Amgen Inc. | Heterocyclic compounds and methods of use |
| WO2023018812A1 (en) * | 2021-08-10 | 2023-02-16 | Amgen Inc. | Heterocyclic compounds and methods of use |
| CA3229855A1 (en) | 2021-08-31 | 2023-03-09 | Incyte Corporation | Naphthyridine compounds as inhibitors of kras |
| US20240374571A1 (en) | 2021-09-01 | 2024-11-14 | Novartis Ag | Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers |
| EP4389751A1 (en) | 2021-09-03 | 2024-06-26 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| 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 |
| US12030883B2 (en) | 2021-09-21 | 2024-07-09 | Incyte Corporation | Hetero-tricyclic compounds as inhibitors of KRAS |
| TWI876212B (zh) | 2021-10-01 | 2025-03-11 | 美商辛瑟拉股份有限公司 | 吖丁啶及吡咯啶parp1抑制劑及其用途 |
| US12030884B2 (en) | 2021-10-01 | 2024-07-09 | Incyte Corporation | Pyrazoloquinoline KRAS inhibitors |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| KR20240101561A (ko) | 2021-10-14 | 2024-07-02 | 인사이트 코포레이션 | Kras의 저해제로서의 퀴놀린 화합물 |
| KR20240089594A (ko) | 2021-10-22 | 2024-06-20 | 지앙수 헨그루이 파마슈티컬스 컴퍼니 리미티드 | 질소 함유 테트라시클릭 화합물, 이의 제조 방법 및 이의 의학적 응용 |
| SMT202500447T1 (it) | 2021-11-02 | 2026-01-12 | Flare Therapeutics Inc | Agonisti inversi di pparg e loro usi |
| CN118139861A (zh) * | 2021-11-05 | 2024-06-04 | 苏州信诺维医药科技股份有限公司 | Kras突变体抑制剂的晶型、其制备方法及其应用 |
| US12275745B2 (en) | 2021-11-24 | 2025-04-15 | Genentech, Inc. | Therapeutic compounds and methods of use |
| US12110276B2 (en) | 2021-11-24 | 2024-10-08 | Genentech, Inc. | Pyrazolo compounds and methods of use thereof |
| CR20240233A (es) | 2021-12-01 | 2024-07-17 | Univ Vanderbilt | Tiofenos 2-amino-3-ciano anulados y derivados para el tratamiento del cáncer |
| TW202340214A (zh) | 2021-12-17 | 2023-10-16 | 美商健臻公司 | 做為shp2抑制劑之吡唑并吡𠯤化合物 |
| AU2022421224A1 (en) | 2021-12-22 | 2024-06-20 | The Regents Of The University Of California | Covalently binding inhibitors of g12s, g12d and/or g12e mutants of k-ras gtpase |
| CN118339153A (zh) | 2021-12-22 | 2024-07-12 | 勃林格殷格翰国际有限公司 | 用于治疗癌症的杂芳族化合物 |
| CN120081844A (zh) | 2022-01-21 | 2025-06-03 | 新特拉有限公司 | Parp1抑制剂及其用途 |
| EP4227307A1 (en) | 2022-02-11 | 2023-08-16 | Genzyme Corporation | Pyrazolopyrazine compounds as shp2 inhibitors |
| CN118715215A (zh) | 2022-02-16 | 2024-09-27 | 美国安进公司 | 作为突变kras蛋白抑制剂的喹唑啉化合物及其用途 |
| JP2025508702A (ja) | 2022-02-16 | 2025-04-10 | アムジエン・インコーポレーテツド | キナゾリン化合物、及び変異krasタンパク質の阻害剤としてのその使用 |
| KR20240156373A (ko) | 2022-03-07 | 2024-10-29 | 암젠 인크 | 4-메틸-2-프로판-2-일-피리딘-3-카르보니트릴의 제조 방법 |
| WO2023172940A1 (en) | 2022-03-08 | 2023-09-14 | Revolution Medicines, Inc. | Methods for treating immune refractory lung cancer |
| WO2023172737A1 (en) | 2022-03-11 | 2023-09-14 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| CA3244999A1 (en) | 2022-03-31 | 2025-06-13 | Eisai R&D Management Co., Ltd. | Pharmaceutical composition for treating tumors |
| EP4504203A1 (en) | 2022-04-04 | 2025-02-12 | Sanofi | Therapeutic combination of kras g12c inhibitor and tead inhibitor |
| WO2023199180A1 (en) | 2022-04-11 | 2023-10-19 | Novartis Ag | Therapeutic uses of a krasg12c inhibitor |
| EP4511128A1 (en) | 2022-04-20 | 2025-02-26 | Kumquat Biosciences Inc. | Macrocyclic heterocycles and uses thereof |
| PT4497438T (pt) | 2022-04-28 | 2025-10-31 | Xinthera Inc C/O Gilead Sciences Inc | Inibidores tricíclicos da parp1 e suas utilizações |
| IL316253A (en) | 2022-05-06 | 2025-01-01 | Chugai Pharmaceutical Co Ltd | A cyclic compound with selective KRAS inhibitory effect on HRAS and NRAS |
| EP4536364A1 (en) | 2022-06-10 | 2025-04-16 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| AU2023320565A1 (en) | 2022-08-05 | 2025-01-23 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| JP2025528836A (ja) | 2022-08-17 | 2025-09-02 | ツリーライン バイオサイエンシズ インコーポレイテッド | ピリドピリミジンKRas阻害剤 |
| GB202212641D0 (en) | 2022-08-31 | 2022-10-12 | Jazz Pharmaceuticals Ireland Ltd | Novel compounds |
| CN115368358A (zh) * | 2022-09-01 | 2022-11-22 | 浙江九洲药业股份有限公司 | 一种Sotorasib新晶型及其制备方法与应用 |
| US20260137665A1 (en) | 2022-10-11 | 2026-05-21 | Aadi Bioscience, Inc. | Combination therapies for the treatment of cancer |
| US12331048B2 (en) | 2022-10-31 | 2025-06-17 | Ventus Therapeutics U.S., Inc. | Pyrido-[3,4-d]pyridazine amine derivatives useful as NLRP3 inhibitors |
| AU2023377064A1 (en) | 2022-11-09 | 2025-05-22 | Revolution Medicines, Inc. | Compounds, complexes, and methods for their preparation and of their use |
| JP2025539080A (ja) | 2022-11-14 | 2025-12-03 | アムジエン・インコーポレーテツド | 大環状kras阻害剤及び使用方法 |
| KR20250109197A (ko) | 2022-11-21 | 2025-07-16 | 트리라인 바이오사이언시스, 인크. | 스피로환식 디하이드로피라노피리미딘 KRas 억제제 |
| PE20260006A1 (es) | 2023-01-26 | 2026-01-06 | Arvinas Operations Inc | Protacs degradadores de kras basados en cereblon y usos relacionados con los mismos |
| CN121487738A (zh) | 2023-03-30 | 2026-02-06 | 锐新医药公司 | 诱导ras gtp水解的组合物和其用途 |
| KR20250166103A (ko) | 2023-04-06 | 2025-11-27 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 종양 치료용 약제학적 조성물 |
| CN121487951A (zh) | 2023-04-07 | 2026-02-06 | 锐新医药公司 | 大环ras抑制剂 |
| WO2024211712A1 (en) | 2023-04-07 | 2024-10-10 | Revolution Medicines, Inc. | Condensed macrocyclic compounds as ras inhibitors |
| EP4695261A1 (en) | 2023-04-14 | 2026-02-18 | Revolution Medicines, Inc. | Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof |
| AU2024251341A1 (en) | 2023-04-14 | 2025-10-16 | Revolution Medicines, Inc. | Crystalline forms of a ras inhibitor |
| KR20260019479A (ko) | 2023-05-04 | 2026-02-10 | 레볼루션 메디슨즈, 인크. | Ras 관련 질환 또는 장애를 위한 병용 요법 |
| WO2024243441A1 (en) | 2023-05-24 | 2024-11-28 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| JP2026520494A (ja) | 2023-05-31 | 2026-06-23 | 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 | がん処置の応答性を予測するためのバイオマーカーとしてのサバイビン |
| JPWO2024248123A1 (enExample) | 2023-06-02 | 2024-12-05 | ||
| EP4724445A1 (en) | 2023-06-06 | 2026-04-15 | Kumquat Biosciences Inc. | Substituted heterocycles and uses thereof |
| EP4735451A1 (en) | 2023-06-30 | 2026-05-06 | Kumquat Biosciences Inc. | Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors |
| 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 |
| WO2025034849A1 (en) * | 2023-08-08 | 2025-02-13 | Theras, Inc. | Fused pyridazines for the treatment of cancer and other indications |
| WO2025064848A1 (en) | 2023-09-21 | 2025-03-27 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyridine kras inhibitors |
| KR20260104082A (ko) | 2023-09-29 | 2026-07-03 | 디3 바이오 (우씨) 컴퍼니, 리미티드 | 암의 치료에 사용하기 위한 wx-001 또는 그의 유도체와 kras g12c 억제제의 조합물 |
| CN122374018A (zh) | 2023-10-06 | 2026-07-10 | 美国安进公司 | 用于癌症治疗的组合疗法 |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| KR20260096846A (ko) | 2023-10-20 | 2026-06-24 | 머크 샤프 앤드 돔 엘엘씨 | Kras 단백질의 소분자 억제제 |
| 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 |
| TW202525793A (zh) * | 2023-12-08 | 2025-07-01 | 大陸商中山優理生物醫藥有限公司 | 一種并環類mat2a抑制劑、包含其的藥物組合物及其應用 |
| WO2025127968A2 (ru) * | 2023-12-14 | 2025-06-19 | Федеральное Государственное Бюджетное Учреждение "Российский Научный Центр Рентгенорадиологии" Министерства Здравоохранения Российской Федерации (Фгбу "Рнцрр" Минздрава России). | Ингибитор ras-гтфазы и его применение для лечения онкологических заболеваний |
| AU2023477424A1 (en) * | 2023-12-19 | 2026-05-21 | Amgen Inc. | Indazole containing compounds and methods of use |
| IL330174A (en) | 2023-12-20 | 2026-08-01 | Boehringer Ingelheim Int Gmbh | Combination cancer treatment using zongratinib and KRAS G12C inhibitor |
| CN122459678A (zh) | 2023-12-29 | 2026-07-24 | 百时美施贵宝公司 | KRAS抑制剂与Treg耗竭剂的组合疗法 |
| WO2025171055A1 (en) | 2024-02-06 | 2025-08-14 | Kumquat Biosciences Inc. | Heterocyclic conjugates and uses thereof |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| TW202602882A (zh) | 2024-03-14 | 2026-01-16 | 美商安進公司 | 作為kras調節劑的大環化合物及其用途 |
| WO2025194054A1 (en) | 2024-03-14 | 2025-09-18 | Amgen Inc. | Spirocyclic compounds as modulators of kras and uses thereof |
| WO2025217247A1 (en) | 2024-04-10 | 2025-10-16 | Amgen Inc. | Tethered spiro-heterocyclic inhibitors of kras g12c mutant proteins and uses thereof |
| WO2025230862A1 (en) | 2024-04-29 | 2025-11-06 | Amgen Inc. | Macrocyclic amino compounds as modulators of kras and uses therof |
| WO2025230878A1 (en) | 2024-04-29 | 2025-11-06 | Amgen Inc. | Macrocyclic compounds as modulators of kras and uses thereof |
| WO2025230971A1 (en) | 2024-04-30 | 2025-11-06 | Kumquat Biosciences Inc. | Macrocyclic heterocycles as anticancer agents |
| WO2025240582A1 (en) | 2024-05-14 | 2025-11-20 | Amgen Inc. | Macrocyclic compounds as modulators of kras and uses thereof |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025245127A1 (en) | 2024-05-21 | 2025-11-27 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| CN118745175A (zh) * | 2024-06-07 | 2024-10-08 | 南昌大学 | 一种氘代索托拉西布及其制备方法与应用 |
| 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 |
| WO2026015796A1 (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 |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| TW202615038A (zh) | 2024-08-07 | 2026-04-16 | 美商太斯萊特醫藥美國有限責任公司 | 包含拓樸異構酶有效載荷之靶向kras之共價誘導之藥物結合物 |
| WO2026035945A1 (en) | 2024-08-07 | 2026-02-12 | Tesseract Medicines Us, Llc | Covalent-induced drug conjugates targeting kras and comprising a topoisomerase payload |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026055477A1 (en) | 2024-09-06 | 2026-03-12 | Amgen Inc. | Macrocyclic compounds as modulators of kras and uses thereof |
| WO2026064520A1 (en) | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Covalent-induced drug conjugates targeting kras and comprising a tubulin inhibitor payload |
| WO2026064527A1 (en) | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Kras-targeting covalent-induced drug conjugates comprising a tubulin inhibitor payload |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
| WO2026090116A2 (en) | 2024-10-21 | 2026-04-30 | Revolution Medicines, Inc. | Ras inhibitors |
| US20260108528A1 (en) | 2024-10-22 | 2026-04-23 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2026090245A1 (en) | 2024-10-22 | 2026-04-30 | Revolution Medicines, Inc. | Use of ras inhibitors for treating cancer |
| WO2026106912A1 (en) | 2024-11-12 | 2026-05-21 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026112260A1 (en) | 2024-11-21 | 2026-05-28 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026122764A2 (en) | 2024-12-06 | 2026-06-11 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026128688A2 (en) | 2024-12-13 | 2026-06-18 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026161839A1 (en) | 2025-01-27 | 2026-07-30 | Revolution Medicines, Inc. | Ras inhibitors |
Family Cites Families (235)
| 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 |
| GB2116183B (en) | 1982-03-03 | 1985-06-05 | Genentech Inc | Human antithrombin iii dna sequences therefore 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 |
| GB8912336D0 (en) | 1989-05-30 | 1989-07-12 | Smithkline Beckman Intercredit | Compounds |
| 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 |
| CA2066898A1 (en) | 1991-04-29 | 1992-10-30 | Chuan Shih | Pharmaceutical compounds |
| DE69222637T2 (de) | 1991-05-10 | 1998-02-26 | Rhone Poulenc Rorer Int | Bis mono- und bicyclische aryl- und heteroarylderivate mit inhibierender wirkung auf die egf und/oder pdgf-rezeptor tyrosinkinase |
| 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 |
| AU661533B2 (en) | 1992-01-20 | 1995-07-27 | Astrazeneca Ab | 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 |
| US5258389A (en) | 1992-11-09 | 1993-11-02 | Merck & Co., Inc. | O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives |
| PT669929E (pt) | 1992-11-13 | 2007-04-30 | Immunex Corp | Ligando de elk, uma citoquina |
| 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 |
| AU693475B2 (en) | 1993-10-01 | 1998-07-02 | Novartis 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 |
| EP0729471A1 (en) | 1993-11-19 | 1996-09-04 | Abbott Laboratories | Semisynthetic analogs of rapamycin (macrolides) being immunomodulators |
| BR9408323A (pt) | 1993-12-17 | 1997-08-19 | Sandoz Ag | Derivados de rapamicina |
| 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 |
| ES2109796T3 (es) | 1994-05-03 | 1998-01-16 | Ciba Geigy Ag | Derivados de pirrolopirimidilo con efecto antiproliferante. |
| 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 |
| ATE446955T1 (de) | 1995-03-30 | 2009-11-15 | Pfizer Prod Inc | Chinazolinone derivate |
| JP4249804B2 (ja) | 1995-04-03 | 2009-04-08 | ノバルティス・アクチエンゲゼルシャフト | ピラゾール誘導体およびその製造法 |
| CA2218503C (en) | 1995-04-20 | 2001-07-24 | Pfizer Inc. | Arylsulfonyl hydroxamic acid derivatives |
| 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 |
| DE69624921T2 (de) | 1995-06-09 | 2003-09-11 | Novartis Ag, Basel | Rapamycinderivate |
| PL188959B1 (pl) | 1995-07-06 | 2005-05-31 | Novartis Ag | Pirolopirymidyny i sposoby ich wytwarzania |
| 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 |
| DK0780386T3 (da) | 1995-12-20 | 2003-02-03 | Hoffmann La Roche | Matrixmetalloproteaseinhibitorer |
| US6140317A (en) | 1996-01-23 | 2000-10-31 | 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 |
| DE59710417D1 (de) | 1996-03-15 | 2003-08-14 | Novartis Ag | N-7 HETEROCYCLYL-PYRROLO[ 2,3-d]PYRIMIDINE UND IHRE VERWENDUNG |
| CN100503580C (zh) | 1996-04-12 | 2009-06-24 | 沃尼尔·朗伯公司 | 酪氨酸激酶的不可逆抑制剂 |
| GB9607729D0 (en) | 1996-04-13 | 1996-06-19 | Zeneca Ltd | Quinazoline derivatives |
| BR9709959A (pt) | 1996-06-24 | 2000-05-09 | Pfizer | Derivados tricìclicos de fenilamino substituìdo para o tratamento de doenças hiperproliferativas |
| WO1998002441A2 (en) | 1996-07-12 | 1998-01-22 | Ariad Pharmaceuticals, Inc. | Non immunosuppressive antifungal rapalogs |
| 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 |
| US6391874B1 (en) | 1996-07-13 | 2002-05-21 | Smithkline Beecham Corporation | Fused heterocyclic compounds as protein tyrosine kinase inhibitors |
| AR007855A1 (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 medicinay composiciones farmaceuticas que los contienen |
| HRP970371A2 (en) | 1996-07-13 | 1998-08-31 | Kathryn Jane Smith | Heterocyclic compounds |
| EP0923585B1 (en) | 1996-07-18 | 2002-05-08 | Pfizer Inc. | Phosphinate based inhibitors of matrix metalloproteases |
| US6111090A (en) | 1996-08-16 | 2000-08-29 | Schering Corporation | Mammalian cell surface antigens; related reagents |
| DK0920505T3 (da) | 1996-08-16 | 2008-09-08 | Schering Corp | Pattedyrcelleoverfladeantigener og tilhörende reagenser |
| PT938486E (pt) | 1996-08-23 | 2008-03-27 | Novartis Ag | Pirrolopirimidinas substituídas e processos para a sua preparação |
| EP0922030A1 (en) | 1996-08-23 | 1999-06-16 | Pfizer Inc. | Arylsulfonylamino hydroxamic acid derivatives |
| WO1998014449A1 (en) | 1996-10-02 | 1998-04-09 | Novartis Ag | Fused pyrazole derivatives and processes for their preparation |
| CA2266519C (en) | 1996-10-02 | 2007-01-23 | Novartis Ag | Pyrimidine derivatives and processes for the preparation thereof |
| 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 |
| US6077864A (en) | 1997-01-06 | 2000-06-20 | Pfizer Inc. | Cyclic sulfone derivatives |
| HUP0000852A2 (hu) | 1997-02-03 | 2001-05-28 | Pfizer Products Inc. | Aril-szulfonil-amino-hidroxámsav-származékok, valamint e vegyületeket tartalmazó gyógyászati készítmények |
| ES2301194T3 (es) | 1997-02-05 | 2008-06-16 | Warner-Lambert Company Llc | Pirido 2,3-d pirimidinas y 4-aminopirimidinas como inhibidores de la proliferacion celular. |
| 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 |
| NZ336836A (en) | 1997-02-11 | 2001-02-23 | Pfizer | Arylsulfonyl hydroxamic acid derivatives suitable for a broad range of medicinal treatments |
| 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 |
| WO1999007701A1 (en) | 1997-08-05 | 1999-02-18 | Sugen, Inc. | Tricyclic quinoxaline derivatives as protein tyrosine kinase inhibitors |
| TR200000368T2 (tr) | 1997-08-08 | 2000-07-21 | Pfizer Products Inc. | Ariloksiariarilsülfonilamino hidroksamik asit türevleri. |
| CA2308114A1 (en) | 1997-10-21 | 1999-04-29 | Human Genome Sciences, Inc. | Human tumor necrosis factor receptor-like proteins tr11, tr11sv1, and tr11sv2 |
| GB9725782D0 (en) | 1997-12-05 | 1998-02-04 | Pfizer Ltd | Therapeutic agents |
| RS49779B (sr) | 1998-01-12 | 2008-06-05 | Glaxo Group Limited, | Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze |
| GB9800575D0 (en) | 1998-01-12 | 1998-03-11 | Glaxo Group Ltd | Heterocyclic compounds |
| GB9801690D0 (en) | 1998-01-27 | 1998-03-25 | Pfizer Ltd | Therapeutic agents |
| JP2002502607A (ja) | 1998-02-09 | 2002-01-29 | ジェネンテク・インコーポレイテッド | 新規な腫瘍壊死因子レセプター相同体及びそれをコードする核酸 |
| DE69940808D1 (de) | 1998-03-04 | 2009-06-10 | Bristol Myers Squibb Co | Heterocyclen substituierte imidazopyrazine als protein- tyrosin-kinase-inhibitoren |
| 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 |
| KR100743287B1 (ko) | 1998-05-29 | 2007-07-26 | 수젠, 인크. | 피롤기로 치환된 2-인돌리논 단백질 인산화 효소 억제제 |
| 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 |
| AU747427B2 (en) | 1998-07-10 | 2002-05-16 | 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 |
| EP2298311B1 (en) | 1999-01-13 | 2012-05-09 | Bayer HealthCare LLC | w-Carboxy aryl substituted diphenyl ureas as p38 kinase inhibitors |
| ATE329596T1 (de) | 1999-03-30 | 2006-07-15 | Novartis Pharma Gmbh | Phthalazinderivate zur behandlung von entzündlicher erkrankungen |
| 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 |
| NZ516258A (en) | 1999-06-07 | 2004-02-27 | Immunex Corp | Tek antagonists |
| ATE376837T1 (de) | 1999-07-12 | 2007-11-15 | Genentech Inc | Stimulierung oder hemmung von angiogenese und herzvaskularisierung mit tumor nekrose faktor ligand/rezeptor homologen |
| IL147803A0 (en) | 1999-08-24 | 2002-08-14 | Ariad Gene Therapeutics Inc | 28-epirapalogs |
| PT1244647E (pt) | 1999-11-05 | 2006-10-31 | Astrazeneca Ab | Derivados de quinazolina como inibidores de vegf |
| JP5336686B2 (ja) | 1999-11-24 | 2013-11-06 | スージェン, インク. | 遊離酸または遊離塩基としてイオン化可能な医薬品のための処方 |
| 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 |
| US7074408B2 (en) | 2000-02-25 | 2006-07-11 | Immunex Corporation | Use of integrin antagonists to inhibit angiogenesis |
| AU7349801A (en) | 2000-07-19 | 2002-01-30 | Warner Lambert Co | Oxygenated esters of 4-iodo phenylamino benzhydroxamic acids |
| US6630500B2 (en) | 2000-08-25 | 2003-10-07 | Cephalon, Inc. | Selected fused pyrrolocarbazoles |
| MXPA03005696A (es) | 2000-12-21 | 2003-10-06 | Glaxo Group Ltd | Pirimidinaminas como moduladores de angiogenesis. |
| 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 |
| US6878714B2 (en) | 2001-01-12 | 2005-04-12 | Amgen Inc. | Substituted alkylamine derivatives and methods of use |
| US7105682B2 (en) | 2001-01-12 | 2006-09-12 | Amgen Inc. | Substituted amine derivatives and methods of use |
| US7102009B2 (en) | 2001-01-12 | 2006-09-05 | Amgen Inc. | Substituted amine derivatives and methods of use |
| JP2002233610A (ja) | 2002-02-18 | 2002-08-20 | Olympia:Kk | スロットマシン |
| 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 |
| WO2004063195A1 (en) | 2003-01-03 | 2004-07-29 | Sloan-Kettering Institute For Cancer Research | Pyridopyrimidine kinase inhibitors |
| AU2004244626A1 (en) | 2003-05-23 | 2004-12-09 | The Government Of The United States Of America As Represented By The Secretary, Department Of Health And Human Services | GITR ligand and GITR ligand-related molecules and antibodies and uses thereof |
| CA2531454C (en) | 2003-07-08 | 2011-10-25 | Novartis Ag | Use of rapamycin and rapamycin derivatives for the treatment of bone loss |
| EP1648900A4 (en) | 2003-07-11 | 2010-02-10 | Ariad Pharma Inc | PHOSPHORUS MACROCYCLES |
| EP1660126A1 (en) | 2003-07-11 | 2006-05-31 | 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 |
| TW200523262A (en) | 2003-07-29 | 2005-07-16 | Smithkline Beecham Corp | Inhibitors of AKT activity |
| JP2007503388A (ja) | 2003-08-22 | 2007-02-22 | アバニール・ファーマシューティカルズ | マクロファージ遊走阻止因子の阻害剤としての置換ナフチリジン誘導体、およびヒト疾患の治療におけるそれらの使用 |
| EP1692318A4 (en) | 2003-12-02 | 2008-04-02 | Genzyme Corp | COMPOSITIONS AND METHODS FOR DIAGNOSIS AND TREATMENT OF LUNG CANCER |
| GB0409799D0 (en) | 2004-04-30 | 2004-06-09 | Isis Innovation | Method of generating improved immune response |
| EP1765402A2 (en) | 2004-06-04 | 2007-03-28 | Duke University | Methods and compositions for enhancement of immunity by in vivo depletion of immunosuppressive cell activity |
| JP4242911B2 (ja) | 2004-08-26 | 2009-03-25 | ファイザー・インク | プロテインキナーゼ阻害薬としてのエナンチオピュアなアミノヘテロアリール化合物 |
| TW200626610A (en) | 2004-10-13 | 2006-08-01 | Wyeth Corp | Analogs of 17-hydroxywortmannin as PI3K inhibitors |
| JP4931823B2 (ja) | 2004-10-18 | 2012-05-16 | アムジエン・インコーポレーテツド | チアジアゾール化合物及び使用方法 |
| JP5238936B2 (ja) | 2005-03-25 | 2013-07-17 | ジーアイティーアール,インク. | Gitr結合分子およびその使用 |
| EP3530736A3 (en) | 2005-05-09 | 2019-11-06 | ONO Pharmaceutical Co., Ltd. | Human monoclonal antibodies to programmed death 1 (pd-1) and methods for treating cancer using anti-pd-1 antibodies alone or in combination with other immunotherapeutics |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| CN101267824A (zh) | 2005-09-20 | 2008-09-17 | 辉瑞产品公司 | 使用酪氨酸激酶抑制剂的治疗剂型和方法 |
| AU2007207743B2 (en) | 2006-01-18 | 2010-07-08 | Amgen Inc. | Thiazole compounds as protein kinase B (PKB) inhibitors |
| WO2007133822A1 (en) | 2006-01-19 | 2007-11-22 | Genzyme Corporation | Gitr antibodies for the treatment of cancer |
| PE20081679A1 (es) | 2006-12-07 | 2008-12-18 | Hoffmann La Roche | Compuestos del inhibidor de fosfoinositida 3-cinasa y metodos de uso |
| HRP20160350T1 (hr) | 2007-03-23 | 2016-05-06 | Amgen Inc. | Heterociklički spojevi i njihove uporabe |
| MX2009010050A (es) | 2007-03-23 | 2009-10-12 | Amgen Inc | Derivados de quinolina o quinoxalina 3-sustituidos y su uso como inhibidores de fosfotidilinositol 3-cinasa (p13k). |
| CA2680783C (en) | 2007-03-23 | 2012-04-24 | Amgen Inc. | Heterocyclic compounds and their uses |
| US8557830B2 (en) | 2007-06-07 | 2013-10-15 | Amgen Inc. | RAF kinase modulators and methods of use |
| PT2175884T (pt) | 2007-07-12 | 2016-09-21 | Gitr Inc | Terapias de combinação empregando moléculas de ligação a gitr |
| US7919504B2 (en) | 2007-07-17 | 2011-04-05 | Amgen Inc. | Thiadiazole modulators of PKB |
| US7897619B2 (en) | 2007-07-17 | 2011-03-01 | Amgen Inc. | Heterocyclic modulators of PKB |
| US7928140B2 (en) | 2007-08-02 | 2011-04-19 | Amgen Inc. | Benzothiazole PI3 kinase modulators for cancer treatment |
| BRPI0816769A2 (pt) | 2007-09-12 | 2016-11-29 | Hoffmann La Roche | combinações de compostos inibidores de fosfoinositida 3-cinase e agentes quimioterapêuticos, e métodos de uso |
| WO2009055730A1 (en) | 2007-10-25 | 2009-04-30 | Genentech, Inc. | Process for making thienopyrimidine compounds |
| US7820665B2 (en) | 2007-12-19 | 2010-10-26 | Amgen Inc. | Imidazopyridazine inhibitors of PI3 kinase for cancer treatment |
| AU2008343932B2 (en) | 2007-12-19 | 2013-08-15 | Amgen Inc. | Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors |
| ATE531372T1 (de) | 2008-04-07 | 2011-11-15 | Amgen Inc | Gem-disubstituierte und spirocyclische aminopyridine/pyrimidine als zellcyclus- inhibitoren |
| JP5599783B2 (ja) | 2008-05-30 | 2014-10-01 | アムジエン・インコーポレーテツド | Pi3キナーゼの阻害薬 |
| JP2011526794A (ja) | 2008-07-02 | 2011-10-20 | エマージェント プロダクト デベロップメント シアトル, エルエルシー | TGF−βアンタゴニスト多重標的結合性分子 |
| JPWO2010030002A1 (ja) | 2008-09-12 | 2012-02-02 | 国立大学法人三重大学 | 外来性gitrリガンド発現細胞 |
| WO2010083246A1 (en) | 2009-01-15 | 2010-07-22 | Amgen Inc. | Fluoroisoquinoline substituted thiazole compounds and methods of use |
| MX2011008674A (es) | 2009-02-18 | 2011-11-04 | Amgen Inc | Compuestos de indol/bencimidazol como inhibidores de quinasa mtor. |
| CA2755285C (en) | 2009-03-20 | 2014-02-11 | Yunxin Y. Bo | Inhibitors of pi3 kinase |
| UY32582A (es) | 2009-04-28 | 2010-11-30 | Amgen Inc | Inhibidores de fosfoinositida 3 cinasa y/u objetivo mamífero |
| CA2760778A1 (en) | 2009-05-13 | 2010-11-18 | Amgen Inc. | Heteroaryl compounds as pikk inhibitors |
| CN102625799A (zh) | 2009-06-25 | 2012-08-01 | 安姆根有限公司 | 杂环化合物及其用途 |
| CA2781865A1 (en) | 2009-06-25 | 2010-12-29 | Amgen Inc. | Polycyclic derivatives of pyridine and their use in the treatment of (inter alia) rheumatoid arthritis and similar diseases |
| JP2012531435A (ja) | 2009-06-25 | 2012-12-10 | アムジエン・インコーポレーテツド | PI3K阻害剤としての4H−ピリド[1,2−a]ピリミジン−4−オン誘導体 |
| EP2445902A2 (en) | 2009-06-25 | 2012-05-02 | Amgen, Inc | Heterocyclic compounds and their uses as inhibitors of pi3k activity |
| EP2266984A1 (en) * | 2009-06-26 | 2010-12-29 | Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts | Pyrido[2,3-d]pyrimidines as Wnt antagonists for treatment of cancer and arthritis |
| IN2015DN02826A (enExample) | 2009-09-03 | 2015-09-11 | Merck Sharp & Dohme | |
| NZ598758A (en) | 2009-09-11 | 2013-12-20 | Amgen Inc | N-4 (-((3-(2-amino-4 pyrimidinyl)-2-pyridinyl)oxy)phenyl)-4-(4-methyl-2-thienyl)-1-phthalazinamine for use in the treatment of antimitotic agent resistant cancer |
| GB0919054D0 (en) | 2009-10-30 | 2009-12-16 | Isis Innovation | Treatment of obesity |
| WO2011075747A1 (en) * | 2009-12-18 | 2011-06-23 | Glaxosmithkline Llc | Therapeutic compounds |
| US20130089554A1 (en) | 2009-12-29 | 2013-04-11 | Emergent Product Development Seattle, Llc | RON Binding Constructs and Methods of Use Thereof |
| US9133164B2 (en) | 2011-04-13 | 2015-09-15 | Innov88 Llc | MIF inhibitors and their uses |
| US20130108641A1 (en) | 2011-09-14 | 2013-05-02 | Sanofi | Anti-gitr antibodies |
| WO2013155223A1 (en) | 2012-04-10 | 2013-10-17 | The Regents Of The University Of California | Compositions and methods for treating cancer |
| CA2881279C (en) | 2012-08-07 | 2020-07-07 | Merck Patent Gmbh | Pyridopyrimidine derivatives as protein kinase inhibitors |
| TW201524952A (zh) | 2013-03-15 | 2015-07-01 | Araxes Pharma Llc | Kras g12c之共價抑制劑 |
| US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
| WO2014143659A1 (en) | 2013-03-15 | 2014-09-18 | Araxes Pharma Llc | Irreversible covalent inhibitors of the gtpase k-ras g12c |
| GB201312059D0 (en) | 2013-07-05 | 2013-08-21 | Univ Leuven Kath | Novel GAK modulators |
| MX380928B (es) * | 2013-10-10 | 2025-03-12 | Araxes Pharma Llc | Inhibidores de kras g12c. |
| TWI659021B (zh) | 2013-10-10 | 2019-05-11 | 亞瑞克西斯製藥公司 | Kras g12c之抑制劑 |
| GB201320729D0 (en) | 2013-11-25 | 2014-01-08 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| US9828363B2 (en) | 2014-01-20 | 2017-11-28 | Cleave Biosciences, Inc. | Fused pyrimidines as inhibitors of P97 complex |
| WO2016035008A1 (en) | 2014-09-04 | 2016-03-10 | Lupin Limited | Pyridopyrimidine derivatives as mek inhibitors |
| JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| WO2016049565A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Compositions and methods for inhibition of ras |
| US9862701B2 (en) | 2014-09-25 | 2018-01-09 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| US10011600B2 (en) | 2014-09-25 | 2018-07-03 | Araxes Pharma Llc | Methods and compositions for inhibition of Ras |
| WO2016161361A1 (en) * | 2015-04-03 | 2016-10-06 | Nantbioscience, Inc. | Compositions and methods of targeting mutant k-ras |
| AU2016245864C1 (en) | 2015-04-10 | 2021-09-09 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| ES2856880T3 (es) | 2015-04-15 | 2021-09-28 | Araxes Pharma Llc | Inhibidores tricíclicos condensados de KRAS y métodos de uso de los mismos |
| JP6869947B2 (ja) | 2015-07-22 | 2021-05-12 | アラクセス ファーマ エルエルシー | 置換キナゾリン化合物ならびにそのg12c変異kras、hrasおよび/またはnrasタンパク質の阻害剤としての使用 |
| US10975071B2 (en) | 2015-09-28 | 2021-04-13 | 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 |
| 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 |
| WO2017058768A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| US10730867B2 (en) | 2015-09-28 | 2020-08-04 | 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 |
| KR102932353B1 (ko) | 2015-11-16 | 2026-02-27 | 아락세스 파마 엘엘씨 | 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법 |
| WO2017100546A1 (en) | 2015-12-09 | 2017-06-15 | 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 |
| ES2863873T3 (es) | 2016-05-18 | 2021-10-11 | Mirati Therapeutics Inc | Inhibidores de KRAS G12C |
| 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 |
| JP2019529484A (ja) | 2016-09-29 | 2019-10-17 | 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阻害剤 |
| US10377743B2 (en) | 2016-10-07 | 2019-08-13 | Araxes Pharma Llc | Inhibitors of RAS and methods of use thereof |
| CR20190338A (es) | 2016-12-22 | 2019-09-09 | Amgen Inc | Inhibidores de kras g12c y métodos para su uso |
| US20200385364A1 (en) | 2017-01-26 | 2020-12-10 | Araxes Pharma Llc | Fused n-heterocyclic compounds and methods of use thereof |
| UA127968C2 (uk) * | 2017-05-22 | 2024-02-28 | Емджен Інк. | Інгібітори g12c kras і способи їх застосування |
| WO2018218069A1 (en) | 2017-05-25 | 2018-11-29 | Araxes Pharma Llc | Quinazoline derivatives as modulators of mutant kras, hras or nras |
| US10640504B2 (en) | 2017-09-08 | 2020-05-05 | Amgen Inc. | Inhibitors of KRAS G12C and methods of using the same |
| MX2020010836A (es) | 2018-05-04 | 2021-01-08 | Amgen Inc | Inhibidores de kras g12c y métodos para su uso. |
| EP3788053B1 (en) | 2018-05-04 | 2024-07-10 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| WO2019217691A1 (en) | 2018-05-10 | 2019-11-14 | Amgen Inc. | Kras g12c inhibitors for the treatment of cancer |
| WO2019232419A1 (en) | 2018-06-01 | 2019-12-05 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| AU2019284472B2 (en) | 2018-06-11 | 2024-05-30 | Amgen Inc. | KRAS G12C inhibitors for treating cancer |
| JP7369719B2 (ja) | 2018-06-12 | 2023-10-26 | アムジエン・インコーポレーテツド | KRas G12C阻害剤及びそれを使用する方法 |
| AU2019291101A1 (en) | 2018-06-21 | 2021-01-07 | Janssen Pharmaceutica Nv | OGA inhibitor compounds |
| AU2019291099A1 (en) | 2018-06-21 | 2021-01-07 | Janssen Pharmaceutica Nv | Oga inhibitor compounds |
| 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 |
| JP7454572B2 (ja) | 2018-11-19 | 2024-03-22 | アムジエン・インコーポレーテツド | Kras g12c阻害剤及びその使用方法 |
| 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 |
| EP3738593A1 (en) | 2019-05-14 | 2020-11-18 | Amgen, Inc | Dosing of kras inhibitor for treatment of cancers |
| EP3972973A1 (en) | 2019-05-21 | 2022-03-30 | Amgen Inc. | Solid state forms |
| US12252486B2 (en) | 2019-05-21 | 2025-03-18 | Amgen Inc. | Solid state forms |
| AU2020369569B2 (en) | 2019-10-24 | 2026-06-18 | Amgen Inc. | Pyridopyrimidine derivatives useful as KRAS G12C and KRAS G12D inhibitors in the treatment of cancer |
| EP4700030A3 (en) | 2019-11-14 | 2026-03-18 | Amgen, Inc. | Improved synthesis of kras g12c inhibitor compound |
| CA3161156A1 (en) | 2019-11-14 | 2021-05-20 | Amgen Inc. | Improved synthesis of kras g12c inhibitor compound |
| US20230028414A1 (en) | 2019-12-16 | 2023-01-26 | Amgen Inc. | Dosing regimen of kras g12c inhibitor |
-
2018
- 2018-05-21 UA UAA201912099A patent/UA127968C2/uk unknown
- 2018-05-21 EP EP21201361.9A patent/EP3974429A1/en active Pending
- 2018-05-21 CN CN201880047910.1A patent/CN110997668B/zh active Active
- 2018-05-21 KR KR1020217028358A patent/KR102573230B1/ko active Active
- 2018-05-21 EP EP18731624.5A patent/EP3630761B1/en active Active
- 2018-05-21 TW TW111135162A patent/TWI834294B/zh active
- 2018-05-21 DK DK18731624.5T patent/DK3630761T3/da active
- 2018-05-21 US US15/984,855 patent/US10519146B2/en active Active
- 2018-05-21 PE PE2019002456A patent/PE20200733A1/es unknown
- 2018-05-21 PT PT187316245T patent/PT3630761T/pt unknown
- 2018-05-21 CN CN202211265391.0A patent/CN115626923B/zh active Active
- 2018-05-21 WO PCT/US2018/033714 patent/WO2018217651A1/en not_active Ceased
- 2018-05-21 RS RS20220019A patent/RS62800B1/sr unknown
- 2018-05-21 HR HRP20212017TT patent/HRP20212017T1/hr unknown
- 2018-05-21 MA MA48772A patent/MA48772B1/fr unknown
- 2018-05-21 LT LTEPPCT/US2018/033714T patent/LT3630761T/lt unknown
- 2018-05-21 SM SM20220053T patent/SMT202200053T1/it unknown
- 2018-05-21 SI SI201830527T patent/SI3630761T1/sl unknown
- 2018-05-21 CR CR20190534A patent/CR20190534A/es unknown
- 2018-05-21 KR KR1020237029215A patent/KR102690360B1/ko active Active
- 2018-05-21 BR BR112019024525-1A patent/BR112019024525B1/pt active IP Right Grant
- 2018-05-21 KR KR1020247025384A patent/KR20240119348A/ko active Pending
- 2018-05-21 EA EA201992781A patent/EA201992781A1/ru unknown
- 2018-05-21 PL PL18731624T patent/PL3630761T3/pl unknown
- 2018-05-21 JO JOJO/P/2019/0272A patent/JOP20190272B1/ar active
- 2018-05-21 SG SG10201913195RA patent/SG10201913195RA/en unknown
- 2018-05-21 HU HUE18731624A patent/HUE057632T2/hu unknown
- 2018-05-21 TW TW107117297A patent/TWI780154B/zh active
- 2018-05-21 CR CR20240126A patent/CR20240126A/es unknown
- 2018-05-21 AU AU2018273356A patent/AU2018273356B2/en active Active
- 2018-05-21 ES ES18731624T patent/ES2905676T3/es active Active
- 2018-05-21 NZ NZ758786A patent/NZ758786A/en unknown
- 2018-05-21 CA CA3063469A patent/CA3063469C/en active Active
- 2018-05-21 KR KR1020197037502A patent/KR102300499B1/ko active Active
- 2018-05-21 MX MX2019013858A patent/MX386189B/es unknown
- 2018-05-21 MY MYPI2019006806A patent/MY199303A/en unknown
- 2018-05-22 AR ARP180101353A patent/AR111882A1/es active IP Right Grant
- 2018-05-22 UY UY0001037744A patent/UY37744A/es active IP Right Grant
- 2018-05-22 JP JP2018097648A patent/JP6785819B2/ja active Active
-
2019
- 2019-10-23 US US16/661,907 patent/US20200055845A1/en not_active Abandoned
- 2019-11-07 IL IL270490A patent/IL270490B/en unknown
- 2019-11-18 PH PH12019502579A patent/PH12019502579A1/en unknown
- 2019-11-19 ZA ZA2019/07651A patent/ZA201907651B/en unknown
- 2019-11-20 CO CONC2019/0013010A patent/CO2019013010A2/es unknown
- 2019-11-20 MX MX2021011115A patent/MX2021011115A/es unknown
- 2019-11-21 CL CL2019003394A patent/CL2019003394A1/es unknown
- 2019-11-24 SA SA522432081A patent/SA522432081B1/ar unknown
- 2019-11-24 SA SA519410622A patent/SA519410622B1/ar unknown
-
2020
- 2020-09-17 CL CL2020002405A patent/CL2020002405A1/es unknown
- 2020-09-24 US US17/031,607 patent/US11905281B2/en active Active
- 2020-10-27 JP JP2020179494A patent/JP7095052B2/ja active Active
-
2021
- 2021-01-29 ZA ZA2021/00644A patent/ZA202100644B/en unknown
- 2021-06-28 AR ARP210101801A patent/AR122785A2/es active IP Right Grant
- 2021-06-28 AR ARP210101802A patent/AR122786A2/es active IP Right Grant
- 2021-06-28 AR ARP210101806A patent/AR122790A2/es active IP Right Grant
- 2021-06-28 AR ARP210101804A patent/AR122788A2/es active IP Right Grant
- 2021-06-28 AR ARP210101799A patent/AR122783A2/es unknown
- 2021-06-28 AR ARP210101803A patent/AR122787A2/es active IP Right Grant
- 2021-06-28 AR ARP210101800A patent/AR122784A2/es unknown
- 2021-06-28 AR ARP210101805A patent/AR122789A2/es active IP Right Grant
- 2021-10-06 AU AU2021245150A patent/AU2021245150C1/en active Active
-
2022
- 2022-01-27 CY CY20221100074T patent/CY1125289T1/el unknown
- 2022-02-07 IL IL290399A patent/IL290399B2/en unknown
- 2022-03-02 ZA ZA2022/02559A patent/ZA202202559B/en unknown
- 2022-03-02 ZA ZA2022/02558A patent/ZA202202558B/en unknown
- 2022-06-21 JP JP2022099389A patent/JP7495444B2/ja active Active
-
2023
- 2023-11-09 AU AU2023263502A patent/AU2023263502A1/en not_active Abandoned
- 2023-12-18 US US18/543,498 patent/US20240174660A1/en active Pending
-
2024
- 2024-05-22 JP JP2024083128A patent/JP7717224B2/ja active Active
-
2025
- 2025-08-26 AU AU2025223741A patent/AU2025223741A1/en active Pending