CO2022006858A2 - Inhibidores de pequeñas moléculas de mutante g12c de kras - Google Patents

Inhibidores de pequeñas moléculas de mutante g12c de kras

Info

Publication number
CO2022006858A2
CO2022006858A2 CONC2022/0006858A CO2022006858A CO2022006858A2 CO 2022006858 A2 CO2022006858 A2 CO 2022006858A2 CO 2022006858 A CO2022006858 A CO 2022006858A CO 2022006858 A2 CO2022006858 A2 CO 2022006858A2
Authority
CO
Colombia
Prior art keywords
pharmaceutically acceptable
compounds
kras
mutant
acceptable salts
Prior art date
Application number
CONC2022/0006858A
Other languages
English (en)
Inventor
Indu Bharathan
Symon Gathiaka
Thomas H Graham
Yongxin Han
Timothy Henderson
Elisabeth Hennessy
Xiaoshen Ma
Ryan Otte
Anandan Palani
David L Sloman
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 CO2022006858A2 publication Critical patent/CO2022006858A2/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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (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)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La divulgación proporciona compuestos de la fórmula (I) (I), o 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 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.
CONC2022/0006858A 2019-10-28 2022-05-24 Inhibidores de pequeñas moléculas de mutante g12c de kras CO2022006858A2 (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
CO2022006858A2 true CO2022006858A2 (es) 2022-06-10

Family

ID=73598936

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2022/0006858A CO2022006858A2 (es) 2019-10-28 2022-05-24 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 (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11932633B2 (en) 2018-05-07 2024-03-19 Mirati Therapeutics, Inc. KRas G12C inhibitors
JP2022517222A (ja) 2019-01-10 2022-03-07 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
CN114008037B (zh) * 2019-06-24 2024-06-21 广东新契生物医药科技有限公司 作为kras g12c抑制剂的杂环化合物
WO2021041671A1 (en) 2019-08-29 2021-03-04 Mirati Therapeutics, Inc. Kras g12d inhibitors
US11890285B2 (en) 2019-09-24 2024-02-06 Mirati Therapeutics, Inc. Combination therapies
MX2022007515A (es) 2019-12-20 2022-09-19 Mirati Therapeutics Inc Inhibidores de sos1.
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
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
JP2023530351A (ja) 2020-06-18 2023-07-14 レヴォリューション・メディスンズ，インコーポレイテッド Ｒａｓ阻害剤への獲得耐性を遅延させる、防止する、及び、治療する方法
IL301062A (en) 2020-09-03 2023-05-01 Revolution Medicines Inc Use of SOS1 inhibitors to treat malignancies with SHP2 mutations
TW202227438A (zh) * 2020-11-24 2022-07-16 大陸商杭州多域生物技術有限公司 一種芳香化合物、其製備方法及應用
US20230107642A1 (en) 2020-12-18 2023-04-06 Erasca, Inc. Tricyclic pyridones and pyrimidones
AU2021407827B2 (en) * 2020-12-21 2023-12-21 Abbisko Therapeutics Co., Ltd. Macrocyclic k-ras g12c inhibitor, preparation method therefor and use thereof
WO2022233316A1 (zh) * 2021-05-06 2022-11-10 南京明德新药研发有限公司 十二元大环类化合物
WO2022266206A1 (en) 2021-06-16 2022-12-22 Erasca, Inc. Kras inhibitor conjugates
EP4384275A1 (en) * 2021-08-12 2024-06-19 Merck Sharp & Dohme LLC Dosage regimen for administration of belzutifan
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

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
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
US5258389A (en) 1992-11-09 1993-11-02 Merck & Co., Inc. O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives
CA2148484A1 (en) 1992-11-13 1994-05-26 Stewart Lyman Novel cytokine designated elk ligand
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
CA2175215C (en) 1993-11-19 2008-06-03 Yat Sun Or Semisynthetic analogs of rapamycin (macrolides) being immunomodulators
BR9408323A (pt) 1993-12-17 1997-08-19 Sandoz Ag Derivados de rapamicina
JPH09512167A (ja) 1994-04-15 1997-12-09 アムジエン・インコーポレーテツド Ｈｅｋ５、ｈｅｋ７、ｈｅｋ８、ｈｅｋ１１、新規なｅｐｈ様受容体タンパク質チロシンキナーゼ
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
DK0821671T3 (da) 1995-04-20 2001-04-23 Pfizer Arylsulfonylhydroxamsyrederivater som MMP- og TNF-inhibitorer
KR100400620B1 (ko) 1995-06-09 2004-02-18 노파르티스 아게 라파마이신유도체
DK0780386T3 (da) 1995-12-20 2003-02-03 Hoffmann La Roche Matrixmetalloproteaseinhibitorer
AU735648B2 (en) 1996-07-12 2001-07-12 Ariad Pharmaceuticals, Inc. Materials and method for treating or preventing pathogenic fungal infection
ES2175415T3 (es) 1996-07-18 2002-11-16 Pfizer Inhibidores de metaloproteasas matriciales basados en fosfinato.
EA199900139A1 (ru) 1996-08-23 1999-08-26 Пфайзер, Инк. Производные арилсульфониламиногидроксамовой кислоты
PT950059E (pt) 1997-01-06 2004-10-29 Pfizer Derivados de sulfona ciclicos
EA002594B1 (ru) 1997-02-03 2002-06-27 Пфайзер Продактс Инк. Производные арилсульфониламиногидроксамовой кислоты
CA2279863A1 (en) 1997-02-07 1998-08-13 Pfizer Inc. N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases
JP3710489B2 (ja) 1997-02-11 2005-10-26 ファイザー・インク アリールスルホニルヒドロキサム酸誘導体
US6150395A (en) 1997-05-30 2000-11-21 The Regents Of The University Of California Indole-3-carbinol (I3C) derivatives and methods
EP1003720B1 (en) 1997-08-08 2004-03-31 Pfizer Products Inc. Aryloxyarylsulfonylamino hydroxamic acid derivatives
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
GB9801690D0 (en) 1998-01-27 1998-03-25 Pfizer Ltd Therapeutic agents
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
ATE260255T1 (de) 1998-11-05 2004-03-15 Pfizer Prod Inc 5-oxo-pyrrolidine-2-carbonsäure- hydroxamidderivate
GB9912961D0 (en) 1999-06-03 1999-08-04 Pfizer Ltd Metalloprotease inhibitors
AU783960B2 (en) 1999-06-07 2006-01-05 Immunex Corporation Tek antagonists
US6521424B2 (en) 1999-06-07 2003-02-18 Immunex Corporation Recombinant expression of Tek antagonists
EP1212331B1 (en) 1999-08-24 2004-04-21 Ariad Gene Therapeutics, Inc. 28-epirapalogs
US6727225B2 (en) 1999-12-20 2004-04-27 Immunex Corporation TWEAK receptor
AU4721901A (en) 2000-02-25 2001-09-03 Immunex Corp Integrin antagonists
US6861424B2 (en) 2001-06-06 2005-03-01 Schering Aktiengesellschaft Platelet adenosine diphosphate receptor antagonists
JP4755981B2 (ja) 2003-07-08 2011-08-24 ノバルティス アーゲー 骨減少の処置のための、ラパマイシンおよびラパマイシン誘導体の使用
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
WO2005016883A2 (en) 2003-08-14 2005-02-24 Icos Corporation Acrylamide derivatives as vla-1 integrin antagonists and uses thereof
WO2006021884A2 (en) 2004-08-26 2006-03-02 Pfizer Inc. Enantiomerically pure aminoheteroaryl compounds as protein kinase inhibitors
MX2007004489A (es) 2004-10-13 2007-09-21 Wyeth Corp Analogos de 17-hidroxiwortamina como inhibidores pi3k.
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
BRPI0616202A2 (pt) 2005-09-20 2011-06-14 Pfizer Prod Inc formas de dosagem e uso de um inibidor da tirosina quinase
AU2008298948B2 (en) 2007-09-12 2014-09-04 F. Hoffmann-La Roche Ag Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use
CN101909631B (zh) 2007-10-25 2012-09-12 健泰科生物技术公司 制备噻吩并嘧啶化合物的方法
US8278313B2 (en) 2008-03-11 2012-10-02 Abbott Laboratories Macrocyclic spiro pyrimidine derivatives
CA2766151A1 (en) 2009-06-24 2010-12-29 Genentech, Inc. Oxo-heterocycle fused pyrimidine compounds, compositions and methods of use
SG193327A1 (en) 2011-04-06 2013-10-30 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
US9688989B2 (en) 2012-06-08 2017-06-27 Sensorion H4 receptor inhibitors for treating tinnitus
CA2904612A1 (en) 2013-03-13 2014-10-09 The Regents Of The University Of Michigan Compositions comprising thienopyrimidine and thienopyridine compounds and methods of use thereof
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
MX364438B (es) 2013-03-15 2019-04-26 Araxes Pharma Llc Inhibidores covalentes de kras g12c.
CN114566183A (zh) 2013-04-05 2022-05-31 杜比实验室特许公司 使用高级频谱延拓降低量化噪声的压扩装置和方法
EP3043784B9 (en) 2013-09-09 2019-11-20 Peloton Therapeutics, Inc. Aryl ethers and uses thereof
EP3055290B1 (en) 2013-10-10 2019-10-02 Araxes Pharma LLC Inhibitors of kras g12c
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
US20160318866A1 (en) 2013-12-19 2016-11-03 Bayer Pharma Aktiengesellschaft Substituted bipiperidinyl derivatives
WO2016049524A1 (en) 2014-09-25 2016-03-31 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
BR112017021869A2 (pt) 2015-04-10 2018-12-11 Araxes Pharma Llc compostos quinazolina substituídos e métodos de uso dos mesmos
EP3283462B1 (en) 2015-04-15 2020-12-02 Araxes Pharma LLC Fused-tricyclic inhibitors of kras and methods of use thereof
EP3325447A1 (en) 2015-07-22 2018-05-30 Araxes Pharma LLC Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
EP3356354A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10882847B2 (en) 2015-09-28 2021-01-05 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
WO2017058807A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10858343B2 (en) 2015-09-28 2020-12-08 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058915A1 (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
JP2018533939A (ja) 2015-10-19 2018-11-22 アラクセス ファーマ エルエルシー Ｒａｓの阻害剤をスクリーニングするための方法
MA47013A (fr) 2015-10-21 2018-08-29 Otsuka Pharma Co Ltd Composés benzolactames utilisés en tant qu'inhibiteurs de protéine kinase
CN108779097A (zh) 2015-11-16 2018-11-09 亚瑞克西斯制药公司 包含取代的杂环基的2-取代的喹唑啉化合物及其使用方法
US9988357B2 (en) 2015-12-09 2018-06-05 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
WO2017172979A1 (en) 2016-03-30 2017-10-05 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
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
CN110036010A (zh) 2016-09-29 2019-07-19 亚瑞克西斯制药公司 Kras g12c突变蛋白的抑制剂
JP2019534260A (ja) 2016-10-07 2019-11-28 アラクセス ファーマ エルエルシー Ｒａｓの阻害剤としての複素環式化合物およびその使用方法
JOP20190154B1 (ar) 2016-12-22 2022-09-15 Amgen Inc بنز أيزو ثيازول، أيزو ثيازولو [3، 4-b] بيريدين، كينازولين، فثالازين، بيريدو [2، 3-d] بيريدازين ومشتقات بيريدو [2، 3-d] بيريميدين على هيئة مثبطات kras g12c لمعالجة سرطان الرئة، أو سرطان البنكرياس أو سرطان القولون والمستقيم
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole 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
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
US20200385364A1 (en) 2017-01-26 2020-12-10 Araxes Pharma Llc Fused n-heterocyclic compounds and methods of use thereof
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
JOP20190186A1 (ar) 2017-02-02 2019-08-01 Astellas Pharma Inc مركب كينازولين
CN110603258A (zh) 2017-05-11 2019-12-20 阿斯利康(瑞典)有限公司 抑制g12c突变型ras蛋白的杂芳基化合物
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
EP3630746A1 (en) 2017-05-25 2020-04-08 Araxes Pharma LLC Compounds and methods of use thereof for treatment of cancer
EP3630745A2 (en) 2017-05-25 2020-04-08 Araxes Pharma LLC Covalent inhibitors of kras
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
EP4141005B1 (en) 2017-09-08 2024-04-03 Amgen Inc. Inhibitors of kras g12c and methods of using the same
GB201715342D0 (en) 2017-09-22 2017-11-08 Univ Nottingham Compounds
EP3684767B1 (en) 2017-09-22 2024-04-24 Jubilant Epipad LLC Heterocyclic compounds as pad inhibitors
KR20200071752A (ko) 2017-10-18 2020-06-19 주빌런트 에피파드 엘엘씨 Pad 억제제로서의 이미다조-피리딘 화합물
CN111989321B (zh) 2017-11-15 2024-05-14 米拉蒂治疗股份有限公司 Kras g12c抑制剂
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
WO2019110751A1 (en) 2017-12-08 2019-06-13 Astrazeneca Ab Tetracyclic compounds as inhibitors of g12c mutant ras protein, for use as anti-cancer agents
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
JP7326305B2 (ja) 2018-03-02 2023-08-15 大塚製薬株式会社 医薬化合物
EP3774769A1 (en) 2018-03-28 2021-02-17 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
MA51848A (fr) * 2018-06-12 2021-04-21 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
IL280331B2 (en) 2018-07-24 2023-12-01 Otsuka Pharma Co Ltd Tricyclic compounds to inhibit the activity of SHP2
JP6928185B2 (ja) 2018-08-16 2021-09-01 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト 縮合環化合物
AR116604A1 (es) 2018-10-15 2021-05-26 Lilly Co Eli Inhibidores de kras g12c
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
UA127930C2 (uk) 2018-11-09 2024-02-14 Ф. Хоффманн-Ла Роше Аг Сполуки з конденсованими кільцями
AU2019384118A1 (en) 2018-11-19 2021-05-27 Amgen Inc. KRAS G12C inhibitors and methods of using the same
KR20210097715A (ko) 2018-11-29 2021-08-09 아락세스 파마 엘엘씨 암 치료용 화합물 및 이의 사용 방법
JP2022517222A (ja) 2019-01-10 2022-03-07 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
WO2020156285A1 (zh) 2019-01-29 2020-08-06 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
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
US20220251109A1 (en) 2019-04-28 2022-08-11 Genfleet Therapeutics (Shanghai) Inc. Oxaazaquinazoline-7(8h)-ketone compound, preparation method therefor and pharmaceutical application thereof
CA3141604A1 (en) 2019-05-20 2020-11-26 1200 Pharma Llc Kras g12c inhibitors and uses thereof
WO2020234103A1 (en) 2019-05-21 2020-11-26 Bayer Aktiengesellschaft Identification and use of kras inhibitors
CN112585129B (zh) 2019-05-21 2022-03-01 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
WO2020238791A1 (zh) 2019-05-24 2020-12-03 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
CA3139769A1 (en) 2019-05-29 2020-12-03 Shiqiang Liu Nitrogen-containing heterocyclic derivative regulator, preparation method therefor and application thereof
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
CN114008037B (zh) 2019-06-24 2024-06-21 广东新契生物医药科技有限公司 作为kras g12c抑制剂的杂环化合物
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
CN114040914A (zh) 2019-07-01 2022-02-11 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
AU2020325477A1 (en) 2019-08-02 2022-03-17 Jiangxi Jemincare Group Co., Ltd Tetracyclic compound, preparation method therefor and use thereof
CN112341457A (zh) 2019-08-07 2021-02-09 北京加科思新药研发有限公司 Kras突变蛋白抑制剂
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
WO2021031952A1 (zh) 2019-08-16 2021-02-25 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
WO2021037018A1 (zh) 2019-08-26 2021-03-04 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
CN114616232A (zh) 2019-09-06 2022-06-10 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
CA3155066A1 (en) 2019-09-20 2021-03-25 Shanghai Jemincare Pharmaceuticals Co., Ltd Fused pyridone compound, and preparation method therefor and use thereof
WO2021057832A1 (en) 2019-09-25 2021-04-01 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitor
US20220389021A1 (en) 2019-09-29 2022-12-08 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
WO2021081212A1 (en) 2019-10-24 2021-04-29 Amgen Inc. Pyridopyrimidine derivatives useful as kras g12c and kras g12d inhibitors in the treatment of cancer
KR20220106765A (ko) 2019-10-30 2022-07-29 젠플리트 테라퓨틱스 (상하이) 아이엔씨. 치환된 헤테로환형 융합된 환형 화합물, 이의 제조 방법 및 이의 약학적 용도
WO2021084765A1 (en) 2019-10-31 2021-05-06 Taiho Pharmaceutical Co., Ltd 4-aminobut-2-enamide derivatives and salts thereof
CN113286794B (zh) 2019-11-04 2024-03-12 北京加科思新药研发有限公司 Kras突变蛋白抑制剂
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
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
EP4067343A4 (en) 2019-11-29 2024-01-03 Taiho Pharmaceutical Co., Ltd. NOVEL PHENOLIC 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
PL3886991T3 (pl) 2019-12-11 2022-11-21 Eli Lilly And Company Inhibitory KRAS G12C
WO2021120045A1 (en) 2019-12-18 2021-06-24 InventisBio Co., Ltd. Heterocyclic compounds, preparation methods and uses thereof
US20230062486A1 (en) 2019-12-19 2023-03-02 Betta Pharmaceuticals Co., Ltd Kras g12c inhibitor and pharmaceutical use thereof
CN113651814B (zh) 2019-12-19 2022-06-17 北京加科思新药研发有限公司 Kras突变蛋白抑制剂
WO2021120890A1 (en) 2019-12-20 2021-06-24 Novartis Ag Pyrazolyl derivatives useful as anti-cancer agents
WO2021127404A1 (en) 2019-12-20 2021-06-24 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
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
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
EP4262803A1 (en) 2020-12-16 2023-10-25 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-kras inhibitors

Also Published As

Publication number Publication date
PE20221253A1 (es) 2022-08-16
US20240043448A1 (en) 2024-02-08
CN114867726A (zh) 2022-08-05
WO2021086833A1 (en) 2021-05-06
ECSP22033597A (es) 2022-05-31
ZA202205938B (en) 2024-02-28
JP2023159395A (ja) 2023-10-31
TW202130645A (zh) 2021-08-16
US11697657B2 (en) 2023-07-11
WO2021086833A8 (en) 2022-07-14
CR20220230A (es) 2022-06-15
IL292438A (en) 2022-06-01
US20240083913A1 (en) 2024-03-14
KR20220106980A (ko) 2022-08-01
BR112022007783A8 (pt) 2023-04-11
DOP2022000090A (es) 2022-06-30
US20210122764A1 (en) 2021-04-29
MX2022005053A (es) 2022-05-18
CN114867726B (zh) 2023-11-28
EP4051678A1 (en) 2022-09-07
CA3158793A1 (en) 2021-05-06
JP2022553994A (ja) 2022-12-27
JOP20220101A1 (ar) 2023-01-30
JP7340100B2 (ja) 2023-09-06
AU2020372881A1 (en) 2022-06-09
BR112022007783A2 (pt) 2022-07-05

Similar Documents

Publication Publication Date Title
CO2022006858A2 (es) Inhibidores de pequeñas moléculas de mutante g12c de kras
CL2019000368A1 (es) Inhibidores de cdk2/4/6.
WO2021055728A8 (en) Small molecule inhibitors of kras g12c mutant
CY1124239T1 (el) Ενωσεις αμινο-τριαζολοπυριδινης και χρηση αυτων στην αγωγη του καρκινου
UY38553A (es) Inhibidores de cdk2
PE20190437A1 (es) Procesos para la preparacion de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidin-1-carboxamida y sales del mismo
CY1123627T1 (el) Παραγωγα διυδροϊμιδαζοπυραζινονης χρησιμα στη θεραπευτικη αντιμετωπιση του καρκινου
UA108926C2 (ru) LibreOffice? [2,3-D] +" +" !+
DOP2014000055A (es) Derivados de pirrolopirimidina y purina
CY1120378T1 (el) Υποκατεστημενα παραγωγα του διφαινυλο βουτανοϊκου φωσφονικου οξεος ως αναστολεις νερ (ουδετερης ενδοπεπτιδασης)
EA202090530A1 (ru) Производные 1-бензил-2-имино-4-фенил-5-оксоимидазолидина как ингибиторы протеазы вич
NZ630457A (en) Compounds useful as inhibitors of atr kinase
TR201802944T4 (tr) İlaç olarak azai̇ndazol veya di̇azai̇ndazol türünün türevleri̇
UY33491A (es) ?Derivados de sulfonamida y sus sales farmacéuticamente aceptables para uso en medicina?.
EA201001013A1 (ru) Бис(сульфониламино)производные для применения в терапии
AR047531A1 (es) Derivados 1h-tieno(2,3-c)pirazol utiles como inhibidores de quinasa
MX2019006843A (es) Inhibidor de cdk4/6.
MX2020010942A (es) Inhibidores dobles de atm y adn-pk para uso en terapias antitumorales.
ECSP22038478A (es) Heteroaril bifenil amidas para el tratamiento de enfermedades relacionadas con el ligando pd-l1
EA201990765A1 (ru) Азаиндазольные соединения для применения при повреждениях сухожилий и/или связок
CL2019001023A1 (es) Derivados de naftiridinona y su uso en el tratamiento de la arritmia.
CO2023017151A2 (es) Inhibidores de ripk1 de nicotinamida
MX2022005951A (es) Compuestos de pirrolotriazina que actuan como inhibidor de mnk.
ECSP23033180A (es) Derivados de pirazol como inhibidores de la ret-cinasa
ZA202201499B (en) Dual atm and dna-pk inhibitors for use in anti-tumor therapy