JPWO2019213526A5 - - Google Patents

Download PDF

Info

Publication number
JPWO2019213526A5
JPWO2019213526A5 JP2020560752A JP2020560752A JPWO2019213526A5 JP WO2019213526 A5 JPWO2019213526 A5 JP WO2019213526A5 JP 2020560752 A JP2020560752 A JP 2020560752A JP 2020560752 A JP2020560752 A JP 2020560752A JP WO2019213526 A5 JPWO2019213526 A5 JP WO2019213526A5
Authority
JP
Japan
Prior art keywords
alkyl
alkylene
heterocycloalkyl
heteroaryl
cycloalkyl
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
Application number
JP2020560752A
Other languages
English (en)
Japanese (ja)
Other versions
JP2021523099A (ja
JP7361722B2 (ja
Publication date
Application filed filed Critical
Priority claimed from PCT/US2019/030606 external-priority patent/WO2019213526A1/en
Publication of JP2021523099A publication Critical patent/JP2021523099A/ja
Publication of JPWO2019213526A5 publication Critical patent/JPWO2019213526A5/ja
Application granted granted Critical
Publication of JP7361722B2 publication Critical patent/JP7361722B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

JP2020560752A 2018-05-04 2019-05-03 Kras g12c阻害剤及び同一物の使用方法 Active JP7361722B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862667314P 2018-05-04 2018-05-04
US62/667,314 2018-05-04
PCT/US2019/030606 WO2019213526A1 (en) 2018-05-04 2019-05-03 Kras g12c inhibitors and methods of using the same

Publications (3)

Publication Number Publication Date
JP2021523099A JP2021523099A (ja) 2021-09-02
JPWO2019213526A5 true JPWO2019213526A5 (ru) 2022-04-25
JP7361722B2 JP7361722B2 (ja) 2023-10-16

Family

ID=66625266

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2020560752A Active JP7361722B2 (ja) 2018-05-04 2019-05-03 Kras g12c阻害剤及び同一物の使用方法

Country Status (8)

Country Link
US (1) US11045484B2 (ru)
EP (1) EP3788053A1 (ru)
JP (1) JP7361722B2 (ru)
AU (1) AU2019262599B2 (ru)
CA (1) CA3099118A1 (ru)
MA (1) MA52496A (ru)
MX (1) MX2020011582A (ru)
WO (1) WO2019213526A1 (ru)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA124474C2 (ru) 2016-12-22 2021-09-22 Емджен Інк. Бензизотіазольні, ізотіазоло[3,4-b]піридинові, хіназолінові, фталазинові, піридо[2,3-d]піридазинові й піридо[2,3-d]піримідинові похідні як інгібітори g12c kras для лікування раку легені, раку підшлункової залози або колоректального раку
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
IL293443A (en) 2017-09-08 2022-07-01 Amgen Inc kras g12c inhibitors and methods of using them
JP7361722B2 (ja) 2018-05-04 2023-10-16 アムジエン・インコーポレーテツド Kras g12c阻害剤及び同一物の使用方法
US11090304B2 (en) 2018-05-04 2021-08-17 Amgen Inc. KRAS G12C inhibitors and methods of using the same
CA3099045A1 (en) 2018-05-10 2019-11-14 Amgen Inc. Kras g12c inhibitors for the treatment of cancer
JP7360396B2 (ja) 2018-06-01 2023-10-12 アムジエン・インコーポレーテツド Kras g12c阻害剤及び同一物の使用方法
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
MA55136A (fr) 2018-11-19 2022-02-23 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
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
US20220152026A1 (en) 2019-02-12 2022-05-19 Novartis Ag Pharmaceutical combination comprising tno155 and a krasg12c inhibitor
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
TW202132315A (zh) 2019-11-04 2021-09-01 美商銳新醫藥公司 Ras 抑制劑
CR20220243A (es) 2019-11-04 2022-08-04 Revolution Medicines Inc Inhibidores de ras
EP4054719A1 (en) 2019-11-04 2022-09-14 Revolution Medicines, Inc. Ras inhibitors
WO2021108683A1 (en) 2019-11-27 2021-06-03 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
IL299131A (en) 2020-06-18 2023-02-01 Revolution Medicines Inc Methods for delaying, preventing and treating acquired resistance to RAS inhibitors
IL301062A (en) 2020-09-03 2023-05-01 Revolution Medicines Inc Use of SOS1 inhibitors to treat malignancies with SHP2 mutations
EP4214209A1 (en) 2020-09-15 2023-07-26 Revolution Medicines, Inc. Indole derivatives as ras inhibitors in the treatment of cancer
BR112023022819A2 (pt) 2021-05-05 2024-01-16 Revolution Medicines Inc Compostos, composição farmacêutica, conjugados e métodos para tratar câncer em um sujeito, para tratar um distúrbio e para inibir uma proteína ras em uma célula
CR20230558A (es) 2021-05-05 2024-01-24 Revolution Medicines Inc Inhibidores de ras para el tratamiento del cáncer
WO2022266206A1 (en) 2021-06-16 2022-12-22 Erasca, Inc. Kras inhibitor conjugates
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
TW202327569A (zh) 2021-09-01 2023-07-16 瑞士商諾華公司 包含tead抑制劑的藥物組合及其用於癌症治療之用途
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
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
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
WO2023172940A1 (en) 2022-03-08 2023-09-14 Revolution Medicines, Inc. Methods for treating immune refractory lung cancer
WO2023199180A1 (en) 2022-04-11 2023-10-19 Novartis Ag Therapeutic uses of a krasg12c inhibitor
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2024102421A2 (en) 2022-11-09 2024-05-16 Revolution Medicines, Inc. Compounds, complexes, and methods for their preparation and of their use

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
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
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
ES2108120T3 (es) 1991-05-10 1997-12-16 Rhone Poulenc Rorer Int Compuestos bis arilicos y heteroarilicos mono- y biciclicos que inhiben tirosina quinasa receptora de egf y/o pdgf.
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
DE69334100T2 (de) 1992-11-13 2007-07-19 Immunex Corp., Seattle Elk ligand, ein cytokin
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
JPH08503971A (ja) 1993-10-01 1996-04-30 チバ−ガイギー アクチェンゲゼルシャフト ピリミジンアミン誘導体及びその調製のための方法
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
WO1995014023A1 (en) 1993-11-19 1995-05-26 Abbott Laboratories Semisynthetic analogs of rapamycin (macrolides) being immunomodulators
SK78196A3 (en) 1993-12-17 1997-02-05 Sandoz Ag Rapamycin demethoxy-derivatives, preparation method thereof and pharmaceutical agent containing them
US5700823A (en) 1994-01-07 1997-12-23 Sugen, Inc. Treatment of platelet derived growth factor related disorders such as cancers
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
WO1995024190A2 (en) 1994-03-07 1995-09-14 Sugen, Inc. Receptor tyrosine kinase inhibitors for inhibiting cell proliferative disorders and compositions thereof
CA2189028A1 (en) 1994-04-15 1995-10-26 Gary M. Fox 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
JP3088018B2 (ja) 1995-03-30 2000-09-18 ファイザー・インコーポレーテッド キナゾリン誘導体
DE69609602T2 (de) 1995-04-03 2001-04-12 Novartis Ag Pyrazolderivate und verfahren zu deren herstellung
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
US5650415A (en) 1995-06-07 1997-07-22 Sugen, Inc. Quinoline compounds
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
CA2219659C (en) 1995-06-09 2008-03-18 Novartis Ag Rapamycin derivatives
CZ1598A3 (cs) 1995-07-06 1998-04-15 Novartis Ag Pyrrolopyrimidiny a způsoby jejich přípravy
DE19534177A1 (de) 1995-09-15 1997-03-20 Merck Patent Gmbh Cyclische Adhäsionsinhibitoren
AR004010A1 (es) 1995-10-11 1998-09-30 Glaxo Group Ltd Compuestos heterociclicos
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
ATE225343T1 (de) 1995-12-20 2002-10-15 Hoffmann La Roche Matrix-metalloprotease inhibitoren
ATE217873T1 (de) 1996-01-23 2002-06-15 Novartis Erfind Verwalt Gmbh Pyrrolopyrimidinen und verfahren zu deren herstellung
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
CA2249739A1 (en) 1996-03-15 1997-09-25 Novartis Ag Novel n-7-heterocyclyl pyrrolo[2,3-d]pyridines and their use
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
CA2258548C (en) 1996-06-24 2005-07-26 Pfizer Inc. Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases
EP0937082A2 (en) 1996-07-12 1999-08-25 Ariad Pharmaceuticals, Inc. Materials and method for treating or preventing pathogenic fungal infection
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
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
TR199900048T2 (xx) 1996-07-13 1999-04-21 Glaxo Group Limited Protein tirozin kinaz inhibit�rleri olarak bisiklik heteroaromatik bile�ikler
DK0912559T3 (da) 1996-07-13 2003-03-10 Glaxo Group Ltd Kondenserede heterocykliske forbindelser som proteintyrosinkinaseinhibitorer
CZ11899A3 (cs) 1996-07-18 1999-11-17 Pfizer Inc. Fosfinátové sloučeniny, farmaceutické prostředky, způsob inhibice matričních metalloproteinas nebo produkce faktoru nekrosy nádorů a způsob léčení
US6111090A (en) 1996-08-16 2000-08-29 Schering Corporation Mammalian cell surface antigens; related reagents
CA2263129C (en) 1996-08-16 2007-01-09 Schering Corporation Mammalian cell surface antigens; related reagents
WO1998007726A1 (en) 1996-08-23 1998-02-26 Novartis Ag Substituted pyrrolopyrimidines and processes for their preparation
SK21499A3 (en) 1996-08-23 2000-05-16 Pfizer Arylsulfonylamino hydroxamic acid derivatives
AU720135B2 (en) 1996-10-02 2000-05-25 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
WO1998014449A1 (en) 1996-10-02 1998-04-09 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
WO1998030566A1 (en) 1997-01-06 1998-07-16 Pfizer Inc. Cyclic sulfone derivatives
US6303636B1 (en) 1997-02-03 2001-10-16 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
WO1998033798A2 (en) 1997-02-05 1998-08-06 Warner Lambert Company Pyrido[2,3-d]pyrimidines and 4-amino-pyrimidines as inhibitors of cell proliferation
AU5493598A (en) 1997-02-07 1998-08-26 Pfizer Inc. N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases
CA2280151C (en) 1997-02-11 2005-12-13 Pfizer Inc. Arylsulfonyl hydroxamic acid derivatives
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
US6150395A (en) 1997-05-30 2000-11-21 The Regents Of The University Of California Indole-3-carbinol (I3C) derivatives and methods
AU8689298A (en) 1997-08-05 1999-03-01 Sugen, Inc. Tricyclic quinoxaline derivatives as protein tyrosine kinase inhibitors
SK1362000A3 (en) 1997-08-08 2000-10-09 Pfizer Prod Inc Aryloxyarylsulfonylamino hydroxamic acid derivatives
WO2000012089A1 (en) 1998-08-31 2000-03-09 Merck & Co., Inc. Novel angiogenesis inhibitors
US6509173B1 (en) 1997-10-21 2003-01-21 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
GB9800569D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
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
IL137409A0 (en) 1998-02-09 2001-07-24 Genentech Inc Novel tumor necrosis factor receptor homolog and nucleic acids encoding the same
ATE430149T1 (de) 1998-03-04 2009-05-15 Bristol Myers Squibb Co Heterocyclen substituierte imidazopyrazine als protein- tyrosin-kinase-inhibitoren
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
WO1999061422A1 (en) 1998-05-29 1999-12-02 Sugen, Inc. Pyrrole substituted 2-indolinone protein kinase inhibitors
UA60365C2 (ru) 1998-06-04 2003-10-15 Пфайзер Продактс Інк. Производные изотиазола, способ их получения, фармацевтическая композиция и способ лечения гиперпролиферативного заболевания у млекопитающего
JP2002520324A (ja) 1998-07-10 2002-07-09 メルク エンド カムパニー インコーポレーテッド 新規な血管形成インヒビター
EP1004578B1 (en) 1998-11-05 2004-02-25 Pfizer Products Inc. 5-oxo-pyrrolidine-2-carboxylic acid hydroxamide derivatives
ES2377847T3 (es) 1999-01-13 2012-04-02 Bayer Healthcare Llc Difenil ureas sustituidas con omega-carboxi arilo como agentes inhibidores de la cinasa p38
AU775332B2 (en) * 1999-03-05 2004-07-29 Metabasis Therapeutics, Inc. Novel phosphorus-containing prodrugs
EP1165085B1 (en) 1999-03-30 2006-06-14 Novartis AG Phthalazine derivatives for treating inflammatory diseases
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
DK1187918T4 (da) 1999-06-07 2009-02-23 Immunex Corp TEK-antagonister
CA2378179A1 (en) 1999-07-12 2001-01-18 Genentech, Inc. Promotion or inhibition of angiogenesis and cardiovascularization by tumor necrosis factor ligand/receptor homologs
ES2219388T3 (es) 1999-08-24 2004-12-01 Ariad Gene Therapeutics, Inc. 28-epi-rapalogos.
AU769222B2 (en) 1999-11-05 2004-01-22 Genzyme Corporation Quinazoline derivatives as VEGF inhibitors
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
JP2003523768A (ja) 2000-02-25 2003-08-12 イミュネックス・コーポレーション インテグリンアンタゴニスト
US6630500B2 (en) 2000-08-25 2003-10-07 Cephalon, Inc. Selected fused pyrrolocarbazoles
ES2556946T3 (es) 2000-12-21 2016-01-21 Novartis Ag Pirimidinaminas como moduladores de la angiogénesis
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
US7102009B2 (en) 2001-01-12 2006-09-05 Amgen Inc. Substituted amine derivatives and methods of use
US7105682B2 (en) 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
US20020147198A1 (en) 2001-01-12 2002-10-10 Guoqing Chen Substituted arylamine derivatives and methods of use
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
US20040214798A1 (en) * 2003-04-22 2004-10-28 Longqin Hu Nitroaryl phosphoramide compositions and methods for targeting and inhibiting undesirable cell growth or proliferation
BRPI0410785A (pt) 2003-05-23 2006-06-20 Wyeth Corp molécula de ácido nucleico isolada, célula hospedeira, animal transgênico não humano, proteìna isolada, oligonucleotìdeo anti-sentido, molécula de sirna, anticorpo isolado, métodos de triagem quanto aos compostos de teste capazes de inibir, de intensificar ou imitar a interação do gitrl com o gitr, para diagnosticar doenças, para tratar um paciente em risco ou diagnosticado com uma doença, para induzir e para inibir a proliferação de uma população celular contendo células t efetoras, de bloquear a supressão e de supressão de uma população celular que inclua células t efetoras na presença de células t reguladoras cd4+cd25+, e para tratar uma doença, composição farmacêutica, e, adjuvante de vacina
PT1646634E (pt) 2003-07-08 2009-02-16 Novartis Ag Utilização de rapamicina e derivados de rapamicina para o tratamento de perda óssea
US20050048054A1 (en) 2003-07-11 2005-03-03 Shino Hanabuchi Lymphocytes; methods
WO2005016252A2 (en) 2003-07-11 2005-02-24 Ariad Gene Therapeutics, Inc. Phosphorus-containing macrocycles
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
UA87153C2 (ru) 2004-08-26 2009-06-25 Пфайзер Инк. Энантиомерно чистые аминогетероарильные соединения как ингибиторы протеинкиназы
TW200626610A (en) 2004-10-13 2006-08-01 Wyeth Corp Analogs of 17-hydroxywortmannin as PI3K inhibitors
PT1866339E (pt) 2005-03-25 2013-09-03 Gitr Inc Moléculas de ligação a gitr e suas utilizações
EP2418278A3 (en) 2005-05-09 2012-07-04 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
EP2114949A1 (en) 2006-12-07 2009-11-11 F.Hoffmann-La Roche Ag Phosphoinositide 3-kinase inhibitor compounds and methods of use
CA2693677C (en) 2007-07-12 2018-02-13 Tolerx, Inc. Combination therapies employing gitr binding molecules
PE20090678A1 (es) 2007-09-12 2009-06-27 Genentech Inc Combinaciones de compuestos inhibidores de fosfoinositida 3-quinasa y agentes quimioterapeuticos y los metodos de uso
JP5348725B2 (ja) 2007-10-25 2013-11-20 ジェネンテック, インコーポレイテッド チエノピリミジン化合物の製造方法
CA2729810A1 (en) 2008-07-02 2010-01-07 Emergent Product Development Seattle, Llc Tgf-.beta. antagonist multi-target binding proteins
WO2010030002A1 (ja) 2008-09-12 2010-03-18 国立大学法人三重大学 外来性gitrリガンド発現細胞
AU2010289677B2 (en) 2009-09-03 2014-07-31 Merck Sharp & Dohme Llc Anti-GITR antibodies
GB0919054D0 (en) 2009-10-30 2009-12-16 Isis Innovation Treatment of obesity
WO2011090762A1 (en) 2009-12-29 2011-07-28 Emergent Product Development Seattle, Llc Heterodimer binding proteins and uses thereof
WO2012142498A2 (en) 2011-04-13 2012-10-18 Innovimmune Biotherapeutics, Inc. Mif inhibitors and their uses
US20130108641A1 (en) 2011-09-14 2013-05-02 Sanofi Anti-gitr antibodies
CN104379563B (zh) 2012-04-10 2018-12-21 加利福尼亚大学董事会 用于治疗癌症的组合物和方法
AU2014239542A1 (en) 2013-03-15 2015-10-01 Araxes Pharma Llc Covalent inhibitors of KRas G12C
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
GB201312059D0 (en) 2013-07-05 2013-08-21 Univ Leuven Kath Novel GAK modulators
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Kras g12c之抑制劑
AU2014331794C1 (en) 2013-10-10 2019-09-12 Araxes Pharma Llc Inhibitors of KRAS G12C
GB201320729D0 (en) 2013-11-25 2014-01-08 Cancer Rec Tech Ltd Therapeutic compounds and their use
CN106061984A (zh) * 2014-02-13 2016-10-26 配体药物公司 前药化合物及其用途
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
JP2017528498A (ja) 2014-09-25 2017-09-28 アラクセス ファーマ エルエルシー Kras g12c変異体タンパク質のインヒビター
WO2016049565A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Compositions and methods for inhibition of ras
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
CA2981530A1 (en) 2015-04-10 2016-10-13 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
US10428064B2 (en) 2015-04-15 2019-10-01 Araxes Pharma Llc Fused-tricyclic inhibitors of KRAS and methods of use thereof
WO2016209996A1 (en) * 2015-06-23 2016-12-29 University Of Oregon Phosphorus-containing heterocycles and a method for making and using
CA2993013A1 (en) 2015-07-22 2017-01-26 Araxes Pharma Llc Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins
EP3356359B1 (en) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10689356B2 (en) 2015-09-28 2020-06-23 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10875842B2 (en) 2015-09-28 2020-12-29 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10647703B2 (en) 2015-09-28 2020-05-12 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3356349A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058805A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356353A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
TW201726656A (zh) 2015-11-16 2017-08-01 亞瑞克西斯製藥公司 包含經取代雜環基團之2-經取代喹唑啉化合物及其使用方法
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
AU2017266911B2 (en) 2016-05-18 2021-09-02 Array Biopharma, 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
US10280172B2 (en) 2016-09-29 2019-05-07 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
UA124474C2 (ru) 2016-12-22 2021-09-22 Емджен Інк. Бензизотіазольні, ізотіазоло[3,4-b]піридинові, хіназолінові, фталазинові, піридо[2,3-d]піридазинові й піридо[2,3-d]піримідинові похідні як інгібітори g12c kras для лікування раку легені, раку підшлункової залози або колоректального раку
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
EP3630747A1 (en) 2017-05-25 2020-04-08 Araxes Pharma LLC Quinazoline derivatives as modulators of mutant kras, hras or nras
IL293443A (en) 2017-09-08 2022-07-01 Amgen Inc kras g12c inhibitors and methods of using them
US11090304B2 (en) 2018-05-04 2021-08-17 Amgen Inc. KRAS G12C inhibitors and methods of using the same
JP7361722B2 (ja) 2018-05-04 2023-10-16 アムジエン・インコーポレーテツド Kras g12c阻害剤及び同一物の使用方法
CA3099045A1 (en) 2018-05-10 2019-11-14 Amgen Inc. Kras g12c inhibitors for the treatment of cancer
JP7360396B2 (ja) 2018-06-01 2023-10-12 アムジエン・インコーポレーテツド Kras g12c阻害剤及び同一物の使用方法
EP4268898A3 (en) 2018-06-11 2024-01-17 Amgen Inc. Kras g12c inhibitors for treating cancer
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.
US20210130352A1 (en) 2018-06-21 2021-05-06 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
MA55136A (fr) 2018-11-19 2022-02-23 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
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
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
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
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
EP3972973A1 (en) 2019-05-21 2022-03-30 Amgen Inc. Solid state forms
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

Similar Documents

Publication Publication Date Title
JPWO2019213526A5 (ru)
JPWO2019217691A5 (ru)
JPWO2020106640A5 (ru)
JP2020528889A5 (ru)
JP2019512505A5 (ru)
CN114401952A (zh) 作为整合应激通路的调节剂的被取代的环烷基化合物
JP6173426B2 (ja) アミノ置換イミダゾピリダジン
JP2019518071A5 (ru)
JP2019519598A5 (ru)
CN112204009A (zh) 整合应激通路的调节剂
BR112016018633B1 (pt) Pirazolopirimidina-5,7-diaminas como inibidores de cdk, seus usos, composição farmacêutica e seu método de preparação, e método in vitro para inibir a função de quinase dependente de ciclina em uma célula
CA3082856A1 (en) Sulphur substituted 3-oxo-2,3-dihydropyridazine-4-carboxamides
JP2020510091A5 (ru)
JP2016510758A5 (ru)
RU2016137832A (ru) Соединения для лечения опосредованных комплементом нарушений
JP2017510642A5 (ru)
RU2018114518A (ru) Новые бициклические соединения в качестве двойных ингибиторов аутотаксина (atx)/карбоангидразы (ca)
JP2013521291A5 (ru)
JP2010523522A5 (ru)
JP2017531688A5 (ru)
JP2020521767A5 (ru)
JP2007501779A5 (ru)
JP7159440B2 (ja) ジカチオン化合物及びその製造方法と使用
JP2017525699A5 (ru)
CN112119072A (zh) 用于ido和tdo调节的化合物和方法,以及其适应症