SG11202104927QA - Improved synthesis of key intermediate of kras g12c inhibitor compound - Google Patents

Improved synthesis of key intermediate of kras g12c inhibitor compound

Info

Publication number
SG11202104927QA
SG11202104927QA SG11202104927QA SG11202104927QA SG11202104927QA SG 11202104927Q A SG11202104927Q A SG 11202104927QA SG 11202104927Q A SG11202104927Q A SG 11202104927QA SG 11202104927Q A SG11202104927Q A SG 11202104927QA SG 11202104927Q A SG11202104927Q A SG 11202104927QA
Authority
SG
Singapore
Prior art keywords
kras
inhibitor compound
key intermediate
improved synthesis
synthesis
Prior art date
Application number
SG11202104927QA
Other languages
English (en)
Inventor
Andrew Thomas Parsons
Brian Mcneil Cochran
Powazinik, Iv
Marc Anthony Caporini
Original Assignee
Amgen Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Amgen Inc filed Critical Amgen Inc
Publication of SG11202104927QA publication Critical patent/SG11202104927QA/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/02Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/24Sulfonic acids having sulfo groups bound to acyclic carbon atoms of a carbon skeleton containing six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/76Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04Heterocyclic 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
    • C07D307/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs
SG11202104927QA 2018-11-16 2019-11-15 Improved synthesis of key intermediate of kras g12c inhibitor compound SG11202104927QA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862768802P 2018-11-16 2018-11-16
PCT/US2019/061815 WO2020102730A1 (en) 2018-11-16 2019-11-15 Improved synthesis of key intermediate of kras g12c inhibitor compound

Publications (1)

Publication Number Publication Date
SG11202104927QA true SG11202104927QA (en) 2021-06-29

Family

ID=68887130

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11202104927QA SG11202104927QA (en) 2018-11-16 2019-11-15 Improved synthesis of key intermediate of kras g12c inhibitor compound

Country Status (25)

Country Link
US (2) US11299491B2 (da)
EP (2) EP3880670B1 (da)
JP (1) JP2020090482A (da)
KR (1) KR20210093276A (da)
CN (1) CN113015724A (da)
AR (1) AR117101A1 (da)
AU (1) AU2019381817A1 (da)
BR (1) BR112021009384A2 (da)
CA (1) CA3117221A1 (da)
CL (1) CL2021001266A1 (da)
DK (1) DK3880670T3 (da)
EA (1) EA202191381A1 (da)
ES (1) ES2953752T3 (da)
FI (1) FI3880670T3 (da)
HU (1) HUE062656T2 (da)
IL (1) IL282682A (da)
LT (1) LT3880670T (da)
MA (1) MA54233A (da)
MX (2) MX2021005598A (da)
PL (1) PL3880670T3 (da)
PT (1) PT3880670T (da)
SG (1) SG11202104927QA (da)
SI (1) SI3880670T1 (da)
TW (1) TW202035354A (da)
WO (1) WO2020102730A1 (da)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2019007643A (es) 2016-12-22 2019-09-09 Amgen Inc Benzoisotiazol, isotiazolo[3,4-b]piridina, quinazolina, ftalazina, pirido[2,3-d]piridazina y derivados de pirido[2,3-d]pirimidina como inhibirores de kras g12c para tratar el cancer de pulmon, pancreatico o colorrectal.
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
SG11202001499WA (en) 2017-09-08 2020-03-30 Amgen Inc Inhibitors of kras g12c and methods of using the same
US11045484B2 (en) 2018-05-04 2021-06-29 Amgen Inc. KRAS G12C inhibitors and methods of using the same
US11090304B2 (en) 2018-05-04 2021-08-17 Amgen Inc. KRAS G12C inhibitors and methods of using the same
JP7361720B2 (ja) 2018-05-10 2023-10-16 アムジエン・インコーポレーテツド がんの治療のためのkras g12c阻害剤
MX2020012731A (es) 2018-06-01 2021-02-22 Amgen Inc Inhibidores de kras g12c y metodos para su uso.
MX2020012261A (es) 2018-06-12 2021-03-31 Amgen Inc Inhibidores de kras g12c que comprenden un anillo de piperazina y uso de estos en el tratamiento del cancer.
JP2020090482A (ja) 2018-11-16 2020-06-11 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
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
CN114980976A (zh) 2019-11-27 2022-08-30 锐新医药公司 共价ras抑制剂及其用途
WO2021185233A1 (en) 2020-03-17 2021-09-23 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitors
US20230212164A1 (en) 2020-06-02 2023-07-06 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
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
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
EP4171570A1 (en) 2020-06-24 2023-05-03 Boehringer Ingelheim International GmbH Anticancer combination therapy comprising a sos1 inhibitor and a kras g12c inhibitor
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
MX2023002248A (es) 2020-09-03 2023-05-16 Revolution Medicines Inc Uso de inhibidores de sos1 para tratar neoplasias malignas con mutaciones de shp2.
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
AR124105A1 (es) 2020-11-20 2023-02-15 Amgen Inc Procedimiento para preparar 7-cloro-6-fluoro-1-(2-isopropil-4-metilpiridin-3-il)pirido[2,3-d]pirimidino-2,4(1h,3h)-diona
CN117479942A (zh) 2021-04-09 2024-01-30 勃林格殷格翰国际有限公司 抗癌疗法
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
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
WO2023117681A1 (en) 2021-12-22 2023-06-29 Boehringer Ingelheim International Gmbh Heteroaromatic compounds for the treatment of cancer
TW202346267A (zh) 2022-03-07 2023-12-01 美商安進公司 用於製備4-甲基-2-丙-2-基-吡啶-3-甲腈之方法
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

Family Cites Families (203)

* Cited by examiner, † Cited by third party
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
CA2102780C (en) 1991-05-10 2007-01-09 Alfred P. Spada 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
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
ZA935111B (en) 1992-07-17 1994-02-04 Smithkline Beecham Corp Rapamycin derivatives
ZA935112B (en) 1992-07-17 1994-02-08 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
WO1994009101A1 (en) 1992-10-13 1994-04-28 The Procter & Gamble Company Non-aqueous liquid detergent compositions
US5258389A (en) 1992-11-09 1993-11-02 Merck & Co., Inc. O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives
ES2279508T3 (es) 1992-11-13 2007-08-16 Immunex Corporation Ligando elk, una 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
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
NZ277498A (en) 1993-12-17 1998-03-25 Novartis Ag Rapamycin derivatives
US5700823A (en) 1994-01-07 1997-12-23 Sugen, Inc. Treatment of platelet derived growth factor related disorders such as cancers
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
IL112248A0 (en) 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
AU2096895A (en) 1994-03-07 1995-09-25 Sugen, Incorporated 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
MX9707453A (es) 1995-03-30 1997-12-31 Pfizer Derivados de quinazolina.
WO1996031510A1 (en) 1995-04-03 1996-10-10 Novartis Ag Pyrazole derivatives and processes for the preparation thereof
ATE198326T1 (de) 1995-04-20 2001-01-15 Pfizer Arylsulfonamido-substituierte hydroxamsäure derivate als inhibitoren von mmp und 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
CN1124276C (zh) 1995-06-09 2003-10-15 诺瓦蒂斯有限公司 雷帕霉素衍生物
ES2172670T3 (es) 1995-07-06 2002-10-01 Novartis Ag Pirrolpirimidinas y procedimientos para su preparacion.
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
ES2183905T3 (es) 1995-12-20 2003-04-01 Hoffmann La Roche Inhibidores de metaloproteasa de matriz.
PT888349E (pt) 1996-01-23 2002-10-31 Novartis Ag Pirrolopirimidinas e processos para a sua preparacao
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
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
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
AU716383B2 (en) 1996-03-15 2000-02-24 Novartis Ag Novel N-7-heterocyclyl pyrrolo(2,3-d)pyrimidines and the use thereof
CA2249446C (en) 1996-04-12 2008-06-17 Warner-Lambert Company Irreversible inhibitors of tyrosine kinases
GB9607729D0 (en) 1996-04-13 1996-06-19 Zeneca Ltd Quinazoline derivatives
JP2000512990A (ja) 1996-06-24 2000-10-03 ファイザー・インク 過増殖性疾患を処置するためのフェニルアミノ置換三環式誘導体
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
EP0937082A2 (en) 1996-07-12 1999-08-25 Ariad Pharmaceuticals, Inc. Materials and method for treating or preventing pathogenic fungal infection
WO1998002437A1 (en) 1996-07-13 1998-01-22 Glaxo Group Limited Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors
JP4386967B2 (ja) 1996-07-13 2009-12-16 グラクソ、グループ、リミテッド プロテインチロシンキナーゼ阻害剤としての縮合複素環式化合物
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
IL127567A0 (en) 1996-07-18 1999-10-28 Pfizer Phosphinate based inhibitors of matrix metalloproteases
EP0920505B1 (en) 1996-08-16 2008-06-04 Schering Corporation Mammalian cell surface antigens; related reagents
US6111090A (en) 1996-08-16 2000-08-29 Schering Corporation Mammalian cell surface antigens; related reagents
CA2264284A1 (en) 1996-08-23 1998-02-26 Ralph P. Robinson Arylsulfonylamino hydroxamic acid derivatives
DK0938486T3 (da) 1996-08-23 2008-07-07 Novartis Ag Substituerede pyrrolopyrimidiner og fremgangsmåder til deres fremstilling
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
AU4779897A (en) 1996-10-02 1998-04-24 Novartis Ag Fused pyrazole derivatives and processes for their preparation
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
ES2224277T3 (es) 1997-01-06 2005-03-01 Pfizer Inc. Derivados de sulfonas ciclicas.
TR199901849T2 (xx) 1997-02-03 2000-02-21 Pfizer Products Inc. Arils�lfonilamino hidroksamik asit t�revleri.
CA2271157A1 (en) 1997-02-05 1998-08-06 Warner-Lambert Company Pyrido[2,3-d]pyrimidines and 4-aminopyrimidines as inhibitors of cellular proliferation
WO1998034915A1 (en) 1997-02-07 1998-08-13 Pfizer Inc. N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases
IL131123A0 (en) 1997-02-11 2001-01-28 Pfizer 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
WO1999007701A1 (en) 1997-08-05 1999-02-18 Sugen, Inc. Tricyclic quinoxaline derivatives as protein tyrosine kinase inhibitors
NZ502309A (en) 1997-08-08 2002-02-01 Pfizer Prod Inc Aryloxyarylsulfonylamino hydroxamic acid derivatives and pharmaceutical use
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
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
CA2319236A1 (en) 1998-02-09 1999-08-12 Genentech, Inc. Novel tumor necrosis factor receptor homolog and nucleic acids encoding the same
AU756838B2 (en) 1998-03-04 2003-01-23 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
EP2020408B1 (en) 1998-05-29 2013-06-26 Sugen, Inc. Pyrrole substituted 2-indolinone protein kinase inhibitor
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
WO2000002871A1 (en) 1998-07-10 2000-01-20 Merck & Co., Inc. Novel angiogenesis inhibitors
AU760020B2 (en) 1998-08-31 2003-05-08 Merck & Co., Inc. Novel angiogenesis inhibitors
PT1004578E (pt) 1998-11-05 2004-06-30 Pfizer Prod Inc Derivados hidroxamida do acido 5-oxo-pirrolidino-2-carboxilico
JP2002534468A (ja) 1999-01-13 2002-10-15 バイエル コーポレイション p38キナーゼ阻害剤としてのω−カルボキシアリール置換ジフェニル尿素
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
DE60027564T3 (de) 1999-06-07 2009-07-23 Immunex Corp., Thousand Oaks Tek-antagonisten
US6521424B2 (en) 1999-06-07 2003-02-18 Immunex Corporation Recombinant expression of Tek antagonists
PT1196186E (pt) 1999-07-12 2008-02-14 Genentech Inc Promoção ou inibição da angiogénese e da cardiovascularização com homólogos de ligandos/receptores do factor de necrose tumoral.
IL147803A0 (en) 1999-08-24 2002-08-14 Ariad Gene Therapeutics Inc 28-epirapalogs
ATE330954T1 (de) 1999-11-05 2006-07-15 Astrazeneca Ab Quinazolin-derivate als vegf-hemmer
PT1233943E (pt) 1999-11-24 2011-09-01 Sugen Inc Formulações para agentes farmacêuticos ionizáveis como ácidos livres ou bases livres
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
WO2001062905A2 (en) 2000-02-25 2001-08-30 Immunex Corporation Integrin antagonists
US6630500B2 (en) 2000-08-25 2003-10-07 Cephalon, Inc. Selected fused pyrrolocarbazoles
SI2311825T1 (sl) 2000-12-21 2016-02-29 Novartis Ag Pirimidinamini kot angiogenetski modulatorji
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
US20020147198A1 (en) 2001-01-12 2002-10-10 Guoqing Chen Substituted arylamine 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
US6878714B2 (en) 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
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
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
PT1646634E (pt) 2003-07-08 2009-02-16 Novartis Ag Utilização de rapamicina e derivados de rapamicina para o tratamento de perda óssea
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
EP1648900A4 (en) 2003-07-11 2010-02-10 Ariad Pharma Inc PHOSPHORUS MACROCYCLES
TW200523262A (en) 2003-07-29 2005-07-16 Smithkline Beecham Corp Inhibitors of AKT activity
CA2531506A1 (en) 2003-08-22 2005-03-10 Avanir Pharmaceuticals Substituted naphthyridine derivatives as inhibitors of macrophage migration inhibitory factor and their use in the treatment of human diseases
JP2007518399A (ja) 2003-12-02 2007-07-12 ジェンザイム コーポレイション 肺癌を診断および治療する組成物並びに方法
GB0409799D0 (en) 2004-04-30 2004-06-09 Isis Innovation Method of generating improved immune response
WO2006083289A2 (en) 2004-06-04 2006-08-10 Duke University Methods and compositions for enhancement of immunity by in vivo depletion of immunosuppressive cell activity
ATE463486T1 (de) 2004-08-26 2010-04-15 Pfizer Enantiomerenreine aminoheteroaryl-verbindungen als proteinkinasehemmer
TW200626610A (en) 2004-10-13 2006-08-01 Wyeth Corp Analogs of 17-hydroxywortmannin as PI3K inhibitors
ES2432091T5 (es) 2005-03-25 2022-03-18 Gitr Inc Moléculas de unión GITR y usos de las mismas
EP2161336B2 (en) 2005-05-09 2017-03-29 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
WO2007034327A1 (en) 2005-09-20 2007-03-29 Pfizer Products Inc. Dosage forms and methods of treatment using a tyrosine kinase inhibitor
US20110212086A1 (en) 2006-01-19 2011-09-01 Genzyme Corporation GITR Antibodies For The Treatment of Cancer
ES2544082T3 (es) 2006-12-07 2015-08-27 F. Hoffmann-La Roche Ag Compuestos inhibidores de fosfoinosítido 3-quinasa y métodos de uso
WO2009009116A2 (en) 2007-07-12 2009-01-15 Tolerx, Inc. Combination therapies employing gitr binding molecules
CL2008002687A1 (es) 2007-09-12 2009-01-16 Genentech Inc Uso de una combinacion farmaceutica de un compuesto derivado de tieno[3,2-d]pirimidina con un agente quimioterapeutico en el tratamiento de un trastorno hiperproliferativo; kit farmaceutico.
WO2009055730A1 (en) 2007-10-25 2009-04-30 Genentech, Inc. Process for making thienopyrimidine compounds
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
CN103951753B (zh) 2009-09-03 2018-01-12 默沙东公司 抗‑gitr抗体
GB0919054D0 (en) 2009-10-30 2009-12-16 Isis Innovation Treatment of obesity
LT2519543T (lt) 2009-12-29 2016-10-10 Emergent Product Development Seattle, Llc Heterodimerus rišantys baltymai ir jų panaudojimas
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
EP2836482B1 (en) 2012-04-10 2019-12-25 The Regents of The University of California Compositions and methods for treating cancer
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
EP2970121B1 (en) * 2013-03-15 2017-12-13 Araxes Pharma LLC Covalent inhibitors of kras g12c
GB201312059D0 (en) 2013-07-05 2013-08-21 Univ Leuven Kath Novel GAK modulators
KR20160076519A (ko) * 2013-10-10 2016-06-30 아락세스 파마 엘엘씨 Kras g12c 억제제
JO3805B1 (ar) * 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
GB201320729D0 (en) 2013-11-25 2014-01-08 Cancer Rec Tech Ltd Therapeutic compounds and their use
CN110526912B (zh) * 2014-06-19 2023-02-14 武田药品工业株式会社 用于激酶抑制的杂芳基化合物
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
US9862701B2 (en) 2014-09-25 2018-01-09 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
WO2016049565A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Compositions and methods for inhibition of ras
EA201792214A1 (ru) 2015-04-10 2018-01-31 Араксис Фарма Ллк Соединения замещенного хиназолина
EP3283462B1 (en) 2015-04-15 2020-12-02 Araxes Pharma LLC Fused-tricyclic inhibitors of kras and methods of use thereof
MX2018000777A (es) 2015-07-22 2018-03-23 Araxes Pharma Llc Compuestos de quinazolina sustituido y su uso como inhibidores de proteinas kras, hras y/o nras mutantes g12c.
TW201713630A (en) * 2015-07-22 2017-04-16 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
US10144724B2 (en) * 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
EP3356353A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10975071B2 (en) 2015-09-28 2021-04-13 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
EP3356351A1 (en) 2015-09-28 2018-08-08 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
EP3356354A1 (en) 2015-09-28 2018-08-08 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
KR20180081596A (ko) 2015-11-16 2018-07-16 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
US10822312B2 (en) 2016-03-30 2020-11-03 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
WO2017201161A1 (en) 2016-05-18 2017-11-23 Mirati Therapeutics, Inc. Kras g12c inhibitors
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
EP3519402A1 (en) 2016-09-29 2019-08-07 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
MX2019007643A (es) * 2016-12-22 2019-09-09 Amgen Inc Benzoisotiazol, isotiazolo[3,4-b]piridina, quinazolina, ftalazina, pirido[2,3-d]piridazina y derivados de pirido[2,3-d]pirimidina como inhibirores de kras g12c para tratar el cancer de pulmon, pancreatico o colorrectal.
US20200385364A1 (en) 2017-01-26 2020-12-10 Araxes Pharma Llc Fused n-heterocyclic compounds and methods of use thereof
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
CN110831933A (zh) 2017-05-25 2020-02-21 亚瑞克西斯制药公司 喹唑啉衍生物作为突变kras、hras或nras的调节剂
SG11202001499WA (en) 2017-09-08 2020-03-30 Amgen Inc Inhibitors of kras g12c and methods of using the same
US11045484B2 (en) 2018-05-04 2021-06-29 Amgen Inc. KRAS G12C inhibitors and methods of using the same
US11090304B2 (en) 2018-05-04 2021-08-17 Amgen Inc. KRAS G12C inhibitors and methods of using the same
JP7361720B2 (ja) 2018-05-10 2023-10-16 アムジエン・インコーポレーテツド がんの治療のためのkras g12c阻害剤
MX2020012731A (es) 2018-06-01 2021-02-22 Amgen Inc Inhibidores de kras g12c y metodos para su uso.
US20190375749A1 (en) 2018-06-11 2019-12-12 Amgen Inc. Kras g12c inhibitors and methods of using the same
MX2020012261A (es) * 2018-06-12 2021-03-31 Amgen Inc Inhibidores de kras g12c que comprenden un anillo de piperazina y uso de estos en el tratamiento del cancer.
AU2019291099A1 (en) 2018-06-21 2021-01-07 Janssen Pharmaceutica Nv Oga inhibitor compounds
AU2019291101A1 (en) 2018-06-21 2021-01-07 Janssen Pharmaceutica Nv OGA inhibitor compounds
JP2020090482A (ja) 2018-11-16 2020-06-11 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
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
JP2022532790A (ja) 2019-05-21 2022-07-19 アムジエン・インコーポレーテツド 固体形態
JP2022552873A (ja) 2019-10-24 2022-12-20 アムジエン・インコーポレーテツド がんの治療におけるkras g12c及びkras g12d阻害剤として有用なピリドピリミジン誘導体
WO2021126816A1 (en) 2019-12-16 2021-06-24 Amgen Inc. Dosing regimen of a kras g12c inhibitor

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