CR20220230A - Inhibidores de pequeñas moléculas de mutante g12c de kras - Google Patents

Inhibidores de pequeñas moléculas de mutante g12c de kras

Info

Publication number
CR20220230A
CR20220230A CR20220230A CR20220230A CR20220230A CR 20220230 A CR20220230 A CR 20220230A CR 20220230 A CR20220230 A CR 20220230A CR 20220230 A CR20220230 A CR 20220230A CR 20220230 A CR20220230 A CR 20220230A
Authority
CR
Costa Rica
Prior art keywords
sup
pharmaceutically acceptable
compounds
kras
mutant
Prior art date
Application number
CR20220230A
Other languages
English (en)
Inventor
Anandan Palani
Symon Gathiaka
Thomas H Graham
Xiaoshen Ma
Timothy Henderson
Elisabeth Hennessy
Indu Bharathan
David L Sloman
Yongxin Han
Ryan Otte
Original Assignee
Merck Sharp & Dohme
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 Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of CR20220230A publication Critical patent/CR20220230A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/22—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed systems contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

La divulgación proporciona compuestos de la fórmula (I): una de sus sales farmacéuticamente aceptables, en donde W1, W2, Y, Z, M, L, Cy, Cz, R1, R2,R3, R4, R2a, Ry, Rz y los subíndices m, n, q y r son como se describe en el presente documento. Los compuestos o sus sales farmacéuticamente aceptables pueden inhibir el mutante G12C de la proteína del sarcoma de rata de Kirsten (KRAS) y se espera que tengan utilidad como agentes terapéuticos, por ejemplo, para tratar el cáncer. La divulgación también proporciona<br /> composiciones farmacéuticas que comprenden compuestos de la fórmula (I) o sus sales farmacéuticamente aceptables. La divulgación también se refiere a métodos para el uso de los compuestos o sus sales farmacéuticamente aceptables en la terapia y profilaxis del cáncer y para preparar productos farmacéuticos para este propósito.
CR20220230A 2019-10-28 2020-10-27 Inhibidores de pequeñas moléculas de mutante g12c de kras CR20220230A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962926879P 2019-10-28 2019-10-28
US202063030014P 2020-05-26 2020-05-26
PCT/US2020/057496 WO2021086833A1 (en) 2019-10-28 2020-10-27 Small molecule inhibitors of kras g12c mutant

Publications (1)

Publication Number Publication Date
CR20220230A true CR20220230A (es) 2022-06-15

Family

ID=73598936

Family Applications (1)

Application Number Title Priority Date Filing Date
CR20220230A CR20220230A (es) 2019-10-28 2020-10-27 Inhibidores de pequeñas moléculas de mutante g12c de kras

Country Status (19)

Country Link
US (3) US11697657B2 (es)
EP (1) EP4051678A1 (es)
JP (2) JP7340100B2 (es)
KR (1) KR20220106980A (es)
CN (1) CN114867726B (es)
AU (1) AU2020372881A1 (es)
BR (1) BR112022007783A8 (es)
CA (1) CA3158793A1 (es)
CO (1) CO2022006858A2 (es)
CR (1) CR20220230A (es)
DO (1) DOP2022000090A (es)
EC (1) ECSP22033597A (es)
IL (1) IL292438A (es)
JO (1) JOP20220101A1 (es)
MX (1) MX2022005053A (es)
PE (1) PE20221253A1 (es)
TW (1) TW202130645A (es)
WO (1) WO2021086833A1 (es)
ZA (1) ZA202205938B (es)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3790551A4 (en) 2018-05-07 2022-03-09 Mirati Therapeutics, Inc. KRAS G12C INHIBITORS
WO2020085493A1 (ja) 2018-10-26 2020-04-30 大鵬薬品工業株式会社 新規なインダゾール化合物又はその塩
EP3908283A4 (en) 2019-01-10 2022-10-12 Mirati Therapeutics, Inc. KRAS G12C INHIBITORS
EP3990448A4 (en) * 2019-06-24 2023-08-02 Guangdong Newopp Biopharmaceuticals Co., Ltd. HETEROCYCLIC COMPOUNDS AS INHIBITORS OF KRAS G12C
JP2022546043A (ja) 2019-08-29 2022-11-02 ミラティ セラピューティクス， インコーポレイテッド Ｋｒａｓ ｇ１２ｄ阻害剤
WO2021061749A1 (en) 2019-09-24 2021-04-01 Mirati Therapeutics, Inc. Combination therapies
CN115135315A (zh) 2019-12-20 2022-09-30 米拉蒂治疗股份有限公司 Sos1抑制剂
WO2021147965A1 (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
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
BR112022025550A2 (pt) 2020-06-18 2023-03-07 Revolution Medicines Inc Métodos para retardar, prevenir e tratar resistência adquirida aos inibidores de ras
MX2023002248A (es) 2020-09-03 2023-05-16 Revolution Medicines Inc Uso de inhibidores de sos1 para tratar neoplasias malignas con mutaciones de shp2.
WO2022111521A1 (zh) * 2020-11-24 2022-06-02 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
US20230107642A1 (en) 2020-12-18 2023-04-06 Erasca, Inc. Tricyclic pyridones and pyrimidones
KR20230088804A (ko) * 2020-12-21 2023-06-20 아비스코 테라퓨틱스 컴퍼니 리미티드 마크로시클릭 k-ras g12c 억제제, 이의 제조 방법 및 용도
CN117177980A (zh) * 2021-05-06 2023-12-05 上海齐鲁制药研究中心有限公司 十二元大环类化合物
US20240293558A1 (en) 2021-06-16 2024-09-05 Erasca, Inc. Kras inhibitor conjugates
CN118201609A (zh) * 2021-08-12 2024-06-14 默沙东有限责任公司 用于施用贝组替凡的给药方案
WO2024040131A1 (en) 2022-08-17 2024-02-22 Treeline Biosciences, Inc. Pyridopyrimidine kras inhibitors
WO2024112654A1 (en) 2022-11-21 2024-05-30 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras inhibitors
CN116063211B (zh) * 2023-02-14 2023-11-10 斯坦德药典标准物质研发(湖北)有限公司 一种Belzutifan的制备方法
WO2024206858A1 (en) 2023-03-30 2024-10-03 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof

Family Cites Families (176)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4034075A (en) 1972-07-03 1977-07-05 Allen & Hanburys Limited Quinaldic acid derivatives
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
PT98990A (pt) 1990-09-19 1992-08-31 American Home Prod Processo para a preparacao de esteres de acidos carboxilicos de rapamicina
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
US5118677A (en) 1991-05-20 1992-06-02 American Home Products Corporation Amide esters of rapamycin
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
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
DK0669929T3 (da) 1992-11-13 2007-01-29 Immunex Corp Elk-ligand, et cytokin
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
US5516658A (en) 1993-08-20 1996-05-14 Immunex Corporation DNA encoding cytokines that bind the cell surface receptor hek
WO1995014023A1 (en) 1993-11-19 1995-05-26 Abbott Laboratories Semisynthetic analogs of rapamycin (macrolides) being immunomodulators
JP3745772B2 (ja) 1993-12-17 2006-02-15 ノバルティス アクチエンゲゼルシャフト 免疫抑制剤として有用なラパマイシン誘導体
EP1464706A3 (en) 1994-04-15 2004-11-03 Amgen Inc., HEK5, HEK7, HEK8, HEK11, EPH-like receptor protein tyrosine kinases
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
EP0821671B1 (en) 1995-04-20 2000-12-27 Pfizer Inc. Arylsulfonyl hydroxamic acid derivatives as mmp and tnf inhibitors
DK0833828T3 (da) 1995-06-09 2003-03-17 Novartis Ag Rapamycinderivater
DK0780386T3 (da) 1995-12-20 2003-02-03 Hoffmann La Roche Matrixmetalloproteaseinhibitorer
EP0937082A2 (en) 1996-07-12 1999-08-25 Ariad Pharmaceuticals, Inc. Materials and method for treating or preventing pathogenic fungal infection
TR199900066T2 (xx) 1996-07-18 1999-04-21 Pfizer Inc. Matriks metalloproteazlar�n fosfinat bazl� inhibit�rleri
PL331895A1 (en) 1996-08-23 1999-08-16 Pfizer Arylosulphonylamino derivatives of hydroxamic acid
US6077864A (en) 1997-01-06 2000-06-20 Pfizer Inc. Cyclic sulfone derivatives
BR9807815A (pt) 1997-02-03 2000-03-08 Pfizer Prod Inc Derivados de ácido arilsulfonilamino-hidroxâmico
WO1998034915A1 (en) 1997-02-07 1998-08-13 Pfizer Inc. N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases
HUP0000657A3 (en) 1997-02-11 2000-10-30 Pfizer N-arylsulfonyl-piperidine, -morpholine hydroxamic acid derivatives and pharmaceutical compositions containing them
US6150395A (en) 1997-05-30 2000-11-21 The Regents Of The University Of California Indole-3-carbinol (I3C) derivatives and methods
EA002490B1 (ru) 1997-08-08 2002-06-27 Пфайзер Продактс Инк. Производные арилоксиарилсульфониламиногидроксамовой кислоты
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
GB9801690D0 (en) 1998-01-27 1998-03-25 Pfizer Ltd Therapeutic agents
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
US6114361A (en) 1998-11-05 2000-09-05 Pfizer Inc. 5-oxo-pyrrolidine-2-carboxylic acid hydroxamide derivatives
GB9912961D0 (en) 1999-06-03 1999-08-04 Pfizer Ltd Metalloprotease inhibitors
NZ516258A (en) 1999-06-07 2004-02-27 Immunex Corp Tek antagonists
US6521424B2 (en) 1999-06-07 2003-02-18 Immunex Corporation Recombinant expression of Tek antagonists
ES2219388T3 (es) 1999-08-24 2004-12-01 Ariad Gene Therapeutics, Inc. 28-epi-rapalogos.
US6727225B2 (en) 1999-12-20 2004-04-27 Immunex Corporation TWEAK receptor
DE60127656T2 (de) 2000-02-25 2007-12-20 Immunex Corp., Seattle Integrin antagonisten
US6861424B2 (en) 2001-06-06 2005-03-01 Schering Aktiengesellschaft Platelet adenosine diphosphate receptor antagonists
ES2316995T3 (es) 2003-07-08 2009-04-16 Novartis Ag Uso de rapamicina y derivados de rapamicida para el tratamiento de la perdida osea.
WO2005016252A2 (en) 2003-07-11 2005-02-24 Ariad Gene Therapeutics, Inc. Phosphorus-containing macrocycles
AR045134A1 (es) 2003-07-29 2005-10-19 Smithkline Beecham Plc Compuesto de 1h - imidazo [4,5-c] piridin-ilo, composicion farmaceutica que lo comprende, proceso para prepararla, su uso para preparar dicha composicion farmaceutica, combinacion farmaceutica, uso de la combinacion farmaceutica para la preparacion de un medicamento, procedimientos para preparar dic
WO2005016883A2 (en) 2003-08-14 2005-02-24 Icos Corporation Acrylamide derivatives as vla-1 integrin antagonists and uses thereof
PL1786785T3 (pl) 2004-08-26 2010-08-31 Pfizer Enancjomerycznie czyste związki aminoheteroarylowe jako kinazy białkowe
TW200626610A (en) 2004-10-13 2006-08-01 Wyeth Corp Analogs of 17-hydroxywortmannin as PI3K inhibitors
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
ES2537352T3 (es) 2007-09-12 2015-06-05 Genentech, Inc. Combinaciones de compuestos inhibidores de fosfoinositida 3-cinasa y agentes quimioterapéuticos, y metodos para su uso
WO2009055730A1 (en) 2007-10-25 2009-04-30 Genentech, Inc. Process for making thienopyrimidine compounds
US8278313B2 (en) 2008-03-11 2012-10-02 Abbott Laboratories Macrocyclic spiro pyrimidine derivatives
EP2445346A4 (en) 2009-06-24 2012-12-05 Genentech Inc OXOHETEROCYCLIC FUSIONED PYRIMIDINE COMPOUNDS AND COMPOSITIONS AND METHOD FOR THEIR USE
MY163187A (en) 2011-04-06 2017-08-15 Taiho Pharmaceutical Co Ltd Novel imidazo-oxazine compound or salt thereof
AR090037A1 (es) 2011-11-15 2014-10-15 Xention Ltd Derivados de tieno y/o furo-pirimidinas y piridinas inhibidores de los canales de potasio
ES2683380T3 (es) 2012-06-08 2018-09-26 Sensorion Inhibidores del receptor H4 para tratar el tinnitus
KR20150130389A (ko) 2013-03-13 2015-11-23 더 리젠츠 오브 더 유니버시티 오브 미시간 티에노피리미딘 및 티에노피리딘 화합물을 포함하는 조성물 및 이의 사용 방법
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
EP3401314B1 (en) 2013-03-15 2023-11-08 Araxes Pharma LLC Covalent inhibitors of kras g12c
ES2617314T3 (es) 2013-04-05 2017-06-16 Dolby Laboratories Licensing Corporation Aparato de compresión y método para reducir un ruido de cuantización utilizando una expansión espectral avanzada
EP3586835B1 (en) 2013-09-09 2023-11-22 Peloton Therapeutics, Inc. Pharmaceutical compositions comprising aryl ethers
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Ｋｒａｓ ｇ１２ｃ之抑制劑
EP3055290B1 (en) 2013-10-10 2019-10-02 Araxes Pharma LLC Inhibitors of kras g12c
JP2017503783A (ja) 2013-12-19 2017-02-02 バイエル ファーマ アクチエンゲゼルシャフト アドレナリン受容体アルファ２ｃ拮抗薬としての置換されたビピペリジニル誘導体
WO2016049565A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Compositions and methods for inhibition of ras
EP3197870B1 (en) 2014-09-25 2020-08-19 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
WO2016164675A1 (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
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds 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.
WO2017058728A1 (en) 2015-09-28 2017-04-06 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
WO2017058805A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356359B1 (en) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10875842B2 (en) 2015-09-28 2020-12-29 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
EP3364977A4 (en) 2015-10-19 2019-09-04 Araxes Pharma LLC PROCESS FOR SCREENING INHIBITORS OF RAS
EP3365334B1 (en) 2015-10-21 2024-07-17 Otsuka Pharmaceutical Co., Ltd. Benzolactam compounds as protein kinase inhibitors
JP7015059B2 (ja) 2015-11-16 2022-02-15 アラクセス ファーマ エルエルシー 置換複素環式基を含む２－置換キナゾリン化合物およびその使用方法
US9988357B2 (en) 2015-12-09 2018-06-05 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
JP7039489B2 (ja) 2016-05-18 2022-03-22 ミラティ セラピューティクス， インコーポレイテッド Ｋｒａｓ ｇ１２ｃ阻害剤
JP6987843B2 (ja) 2016-07-27 2022-01-05 パドロック・セラピューティクス・インコーポレイテッドPadlock Therapeutics, Inc. Ｐａｄ４の共有結合性阻害剤
WO2018064510A1 (en) * 2016-09-29 2018-04-05 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
CN110312711A (zh) 2016-10-07 2019-10-08 亚瑞克西斯制药公司 作为ras抑制剂的杂环化合物及其使用方法
HUE056777T2 (hu) 2016-12-22 2022-03-28 Amgen Inc Benzizotiazol-, izotiazolo[3,4-b]piridin-, kinazolin-, ftálazin-, pirido[2,3-d]piridazin- és pirido[2,3-d]pirimidin-származékok mint KRAS G12C inhibitorok tüdõ-, hasnyálmirigy- vagy vastagbélrák kezelésére
EP3573971A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
WO2018140598A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Fused n-heterocyclic compounds and methods of use thereof
US11274093B2 (en) 2017-01-26 2022-03-15 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
EP3573967A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused hetero-hetero bicyclic compounds and methods of use thereof
US11358959B2 (en) 2017-01-26 2022-06-14 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
EP3573970A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer
JOP20190186A1 (ar) 2017-02-02 2019-08-01 Astellas Pharma Inc مركب كينازولين
TW201906848A (zh) 2017-05-11 2019-02-16 瑞典商阿斯特捷利康公司 化學化合物
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
WO2018218069A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant kras, hras or nras
JP2020521742A (ja) 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー Ｋｒａｓの共有結合性阻害剤
EP3630746A1 (en) 2017-05-25 2020-04-08 Araxes Pharma LLC Compounds and methods of use thereof for treatment of cancer
CN107556289A (zh) 2017-06-22 2018-01-09 天津国际生物医药联合研究院 一种氯苯‑吡啶类化合物及其应用
MA50077A (fr) 2017-09-08 2020-07-15 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
GB201715342D0 (en) 2017-09-22 2017-11-08 Univ Nottingham Compounds
RU2764243C2 (ru) 2017-09-22 2022-01-14 ДЖУБИЛАНТ ЭПИПЭД ЭлЭлСи Гетероциклические соединения в качестве ингибиторов PAD
PT3697785T (pt) 2017-10-18 2023-04-03 Jubilant Epipad LLC Compostos de imidazopiridina como inibidores de pad
AU2018369759B2 (en) 2017-11-15 2022-11-24 Array Biopharma Inc. KRas G12C inhibitors
US10647715B2 (en) 2017-11-15 2020-05-12 Mirati Therapeutics, Inc. KRas G12C inhibitors
WO2019099703A1 (en) 2017-11-16 2019-05-23 Sidecar Therapeutics, Inc. Apoptosis signal-regulating kinase 1 (ask 1) inhibitor compounds
TW201938561A (zh) 2017-12-08 2019-10-01 瑞典商阿斯特捷利康公司 化學化合物
TW201942116A (zh) 2018-02-09 2019-11-01 美商輝瑞股份有限公司 作為抗癌劑之四氫喹唑啉衍生物
SG11202006778TA (en) 2018-03-02 2020-08-28 Otsuka Pharma Co Ltd Pharmaceutical compounds
WO2019185525A1 (en) 2018-03-28 2019-10-03 Bayer Pharma Aktiengesellschaft 4-(3-amino-6-fluoro-1h-indazol-5-yl)-1,2,6-trimethyl-1,4-dihydropyridine-3,5-dic arbonitrile compounds for treating hyperproliferative disorders
CA3100390A1 (en) 2018-06-12 2020-03-12 Amgen Inc. Kras g12c inhibitors encompassing piperazine ring and use thereof in the treatment of cancer
MA53395A (fr) 2018-07-24 2021-06-02 Otsuka Pharma Co Ltd Composés hétérobicycliques pour inhiber l'activité de shp2
US11760744B2 (en) 2018-08-16 2023-09-19 Genentech, Inc. Fused ring compounds
TW202033518A (zh) 2018-10-15 2020-09-16 美商美國禮來大藥廠 Kras g12c 抑制劑
WO2020085493A1 (ja) 2018-10-26 2020-04-30 大鵬薬品工業株式会社 新規なインダゾール化合物又はその塩
PE20211504A1 (es) 2018-11-09 2021-08-11 Hoffmann La Roche Compuestos de anillo fusionado
MX2021005700A (es) 2018-11-19 2021-07-07 Amgen Inc Inhibidores de kras g12c y metodos de uso de los mismos.
EP3887373A1 (en) 2018-11-29 2021-10-06 Araxes Pharma LLC Compounds and methods of use thereof for treatment of cancer
EP3908283A4 (en) 2019-01-10 2022-10-12 Mirati Therapeutics, Inc. KRAS G12C INHIBITORS
EP3919483A4 (en) 2019-01-29 2022-02-09 Brightgene Bio-medical Technology Co., Ltd. HETEROCYCLIC BENZOPYRIDONE COMPOUND AND USE THEREOF
WO2020177629A1 (zh) 2019-03-01 2020-09-10 劲方医药科技(上海)有限公司 螺环取代的嘧啶并环类化合物，其制法与医药上的用途
US20220204527A1 (en) 2019-03-05 2022-06-30 Astrazeneca Ab Fused tricyclic compounds useful as anticancer agents
CN113767106B (zh) 2019-04-28 2024-02-20 劲方医药科技(上海)有限公司 氧杂氮杂喹唑啉-7(8h)-酮类化合物,其制法与医药上的用途
WO2020236940A1 (en) 2019-05-20 2020-11-26 California Institute Of Technology Kras g12c inhibitors and uses thereof
EP3972963A1 (en) 2019-05-21 2022-03-30 Bayer Aktiengesellschaft Identification and use of kras inhibitors
CN118359609A (zh) 2019-05-21 2024-07-19 益方生物科技(上海)股份有限公司 杂环化合物，其制备方法和用途
CN113874374A (zh) 2019-05-24 2021-12-31 江苏恒瑞医药股份有限公司 氢化吡啶并嘧啶类衍生物、其制备方法及其在医药上的应用
TW202110843A (zh) 2019-05-29 2021-03-16 大陸商上海翰森生物醫藥科技有限公司 含氮雜環類衍生物調節劑、其製備方法和應用
WO2020239123A1 (zh) 2019-05-31 2020-12-03 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
EP3990448A4 (en) * 2019-06-24 2023-08-02 Guangdong Newopp Biopharmaceuticals Co., Ltd. HETEROCYCLIC COMPOUNDS AS INHIBITORS OF KRAS G12C
US20220372036A1 (en) 2019-06-25 2022-11-24 Medshine Discovery Inc. Seven-membered heterocyclic derivative acting as kras g12c mutant protein inhibitor
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
JP2022543767A (ja) 2019-08-02 2022-10-14 シャンハイ ジェミンケア ファーマシューティカルズ カンパニー、リミテッド 四環式化合物、その調製と使用の方法
TWI752580B (zh) 2019-08-07 2022-01-11 大陸商北京加科思新藥研發有限公司 Kras突變蛋白抑制劑
WO2021027943A1 (zh) 2019-08-14 2021-02-18 正大天晴药业集团南京顺欣制药有限公司 哒嗪酮并嘧啶类衍生物及其医药用途
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
CN114222743A (zh) 2019-08-16 2022-03-22 劲方医药科技(上海)有限公司 氧代六元环并嘧啶类化合物，其制法与医药上的用途
CN114269735B (zh) 2019-08-26 2024-02-23 南京创济生物医药有限公司 二氢或四氢喹唑啉类化合物及其中间体、制备方法和应用
WO2021043322A1 (zh) 2019-09-06 2021-03-11 正大天晴药业集团南京顺欣制药有限公司 氮杂环庚烷并嘧啶类衍生物及其医药用途
MX2022003401A (es) 2019-09-20 2022-07-13 Shanghai Jemincare Pharmaceuticals Co Ltd Compuesto de piridona fusionada y metodo de preparacion del mismo y uso del mismo.
US20210094919A1 (en) 2019-09-25 2021-04-01 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitors
WO2021058018A1 (en) 2019-09-29 2021-04-01 Beigene, Ltd. Inhibitors of kras g12c
CN112574224A (zh) 2019-09-30 2021-03-30 上海迪诺医药科技有限公司 Kras g12c抑制剂及其应用
CN112694475A (zh) 2019-10-23 2021-04-23 苏州泽璟生物制药股份有限公司 环烷基类和杂环烷基类抑制剂及其制备方法和应用
MX2022004656A (es) 2019-10-24 2022-05-25 Amgen Inc Derivados de piridopirimidina utiles como inhibidores de kras g12c y kras g12d en el tratamiento del cancer.
EP4328229A3 (en) 2019-10-30 2024-10-02 Genfleet Therapeutics (Shanghai) Inc. Substituted heterocyclic fused cyclic compound, preparation method therefor and pharmaceutical use thereof
WO2021084765A1 (en) 2019-10-31 2021-05-06 Taiho Pharmaceutical Co., Ltd 4-aminobut-2-enamide derivatives and salts thereof
WO2021088458A1 (en) 2019-11-04 2021-05-14 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitor
TWI760919B (zh) 2019-11-15 2022-04-11 大陸商四川海思科製藥有限公司 一種嘧啶並環衍生物及其在醫藥上的應用
CN112824410A (zh) 2019-11-21 2021-05-21 苏州泽璟生物制药股份有限公司 氮杂七元环类抑制剂及其制备方法和应用
US20230061083A1 (en) 2019-11-29 2023-03-02 Evopoint Biosciences Co., Ltd. Kras g12c inhibitor compound and use thereof
US20230049402A1 (en) 2019-11-29 2023-02-16 Taiho Pharmaceutical Co., Ltd. Novel phenol compound or salt thereof
JP7480298B2 (ja) 2019-12-02 2024-05-09 シャンハイ インリー ファーマシューティカル カンパニー リミテッド 酸素含有複素環化合物、その製造方法及び使用
WO2021113595A1 (en) 2019-12-06 2021-06-10 Beta Pharma, Inc. Phosphorus derivatives as kras inhibitors
AU2020402701B2 (en) 2019-12-11 2024-03-14 Eli Lilly And Company KRas G12C inhibitors
WO2021120045A1 (en) 2019-12-18 2021-06-24 InventisBio Co., Ltd. Heterocyclic compounds, preparation methods and uses thereof
PE20230161A1 (es) 2019-12-19 2023-02-01 Jacobio Pharmaceuticals Co Ltd Inhibidores de proteinas kras mutantes
US20230062486A1 (en) 2019-12-19 2023-03-02 Betta Pharmaceuticals Co., Ltd Kras g12c inhibitor and pharmaceutical use thereof
WO2021120890A1 (en) 2019-12-20 2021-06-24 Novartis Ag Pyrazolyl derivatives useful as anti-cancer agents
AU2020408562A1 (en) 2019-12-20 2022-06-23 Erasca, Inc. Tricyclic pyridones and pyrimidones
CN113045565A (zh) 2019-12-27 2021-06-29 微境生物医药科技(上海)有限公司 新型K-Ras G12C抑制剂
WO2021147965A1 (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
TW202144349A (zh) 2020-04-30 2021-12-01 大陸商上海科州藥物研發有限公司 作為ｋｒａｓ抑制劑的雜環化合物的製備及其應用方法
US20230357277A1 (en) 2020-09-22 2023-11-09 Mirati Therapeutics, Inc. Kras g12d inhibitors
WO2022133038A1 (en) 2020-12-16 2022-06-23 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-kras inhibitors

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