AU2020369569A1 - Pyridopyrimidine derivatives useful as KRAS G12C and KRAS G12D inhibitors in the treatment of cancer - Google Patents

Pyridopyrimidine derivatives useful as KRAS G12C and KRAS G12D inhibitors in the treatment of cancer Download PDF

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Publication number
AU2020369569A1
AU2020369569A1 AU2020369569A AU2020369569A AU2020369569A1 AU 2020369569 A1 AU2020369569 A1 AU 2020369569A1 AU 2020369569 A AU2020369569 A AU 2020369569A AU 2020369569 A AU2020369569 A AU 2020369569A AU 2020369569 A1 AU2020369569 A1 AU 2020369569A1
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compound
alkylene
cancer
alkyl
pharmaceutically acceptable
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Victor J. Cee
Hui-Ling Wang
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Amgen Inc
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Amgen Inc
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    • 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
    • C07D471/02—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
    • 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
    • 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

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  • 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)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2020369569A 2019-10-24 2020-10-22 Pyridopyrimidine derivatives useful as KRAS G12C and KRAS G12D inhibitors in the treatment of cancer Pending AU2020369569A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962925657P 2019-10-24 2019-10-24
US62/925,657 2019-10-24
PCT/US2020/056874 WO2021081212A1 (en) 2019-10-24 2020-10-22 Pyridopyrimidine derivatives useful as kras g12c and kras g12d inhibitors in the treatment of cancer

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AU2020369569A1 true AU2020369569A1 (en) 2022-04-14

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AU2020369569A Pending AU2020369569A1 (en) 2019-10-24 2020-10-22 Pyridopyrimidine derivatives useful as KRAS G12C and KRAS G12D inhibitors in the treatment of cancer

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US (1) US20240190862A1 (enExample)
EP (2) EP4048671B1 (enExample)
JP (1) JP7634003B2 (enExample)
AU (1) AU2020369569A1 (enExample)
CA (1) CA3155857A1 (enExample)
MX (1) MX2022004656A (enExample)
WO (1) WO2021081212A1 (enExample)

Families Citing this family (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3048217A1 (en) 2016-12-22 2018-06-28 Amgen Inc. Kras g12c inhibitors and methods of using the same
ES2905676T3 (es) 2017-05-22 2022-04-11 Amgen Inc Inhibidores de KRAS G12C y métodos para su uso
CN111051306B (zh) 2017-09-08 2023-01-03 美国安进公司 Kras g12c的抑制剂及其使用方法
CN119569702A (zh) 2018-04-04 2025-03-07 阿尔维纳斯运营股份有限公司 蛋白水解调节剂及相关使用方法
MX2020010836A (es) 2018-05-04 2021-01-08 Amgen Inc Inhibidores de kras g12c y métodos para su uso.
ES2995514T3 (en) 2018-05-04 2025-02-10 Amgen Inc Kras g12c inhibitors and methods of using the same
WO2019217307A1 (en) 2018-05-07 2019-11-14 Mirati Therapeutics, Inc. Kras g12c inhibitors
AU2019278998B2 (en) 2018-06-01 2023-11-09 Amgen Inc. KRAS G12C inhibitors and methods of using the same
MX2020012204A (es) 2018-06-11 2021-03-31 Amgen Inc Inhibidores de kras g12c para tratar el cáncer.
CA3100390A1 (en) 2018-06-12 2020-03-12 Amgen Inc. Kras g12c inhibitors encompassing piperazine ring and use thereof in the treatment of cancer
JP2022500385A (ja) 2018-09-10 2022-01-04 ミラティ セラピューティクス， インコーポレイテッド 組み合わせ療法
ES3004338T3 (en) 2018-09-10 2025-03-12 Mirati Therapeutics Inc Combination therapies
WO2020055761A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
KR102871791B1 (ko) 2018-09-10 2025-10-15 미라티 테라퓨틱스, 인크. 병용 요법
TWI831855B (zh) 2018-10-26 2024-02-11 日商大鵬藥品工業股份有限公司 新穎吲唑化合物或其鹽
JP7516029B2 (ja) 2018-11-16 2024-07-16 アムジエン・インコーポレーテツド Ｋｒａｓ ｇ１２ｃ阻害剤化合物の重要な中間体の改良合成法
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのｋｒａｓｇ１２ｃ阻害剤及び１種以上の薬学的に活性な追加の薬剤を含む併用療法
CA3112129A1 (en) 2018-12-05 2020-06-11 Mirati Therapeutics, Inc. Combination therapies
JP7592601B2 (ja) 2019-01-10 2024-12-02 ミラティ セラピューティクス， インコーポレイテッド Ｋｒａｓ ｇ１２ｃ阻害剤
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
CN114144414B (zh) 2019-05-21 2025-11-07 美国安进公司 固态形式
CA3148745A1 (en) 2019-08-29 2021-03-04 Xiaolun Wang Kras g12d inhibitors
US12122787B2 (en) 2019-09-20 2024-10-22 Shanghai Jemincare Pharmaceuticals Co., Ltd Fused pyridone compound, and preparation method therefor and use thereof
CN114761012B (zh) 2019-09-24 2025-03-21 米拉蒂治疗股份有限公司 组合疗法
CA3158793A1 (en) 2019-10-28 2021-05-06 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
WO2021106230A1 (ja) 2019-11-29 2021-06-03 大鵬薬品工業株式会社 新規なフェノール化合物又はその塩
KR20220130126A (ko) 2019-12-20 2022-09-26 미라티 테라퓨틱스, 인크. Sos1 억제제
CN114671866A (zh) * 2020-12-25 2022-06-28 苏州泽璟生物制药股份有限公司 芳基或杂芳基并吡啶酮或嘧啶酮类衍生物及其制备方法和应用
WO2021244555A1 (zh) * 2020-06-02 2021-12-09 上海喆邺生物科技有限公司 一种手性中间体及其制备方法
WO2021249563A1 (zh) * 2020-06-12 2021-12-16 苏州泽璟生物制药股份有限公司 芳基或杂芳基并吡啶酮或嘧啶酮类衍生物及其制备方法和应用
KR20230042600A (ko) 2020-06-18 2023-03-28 레볼루션 메디슨즈, 인크. Ras 억제제에 대한 획득된 저항성을 지연, 예방, 및 치료하는 방법
CA3187757A1 (en) 2020-09-03 2022-03-24 Ethan AHLER Use of sos1 inhibitors to treat malignancies with shp2 mutations
US12286431B2 (en) 2020-09-11 2025-04-29 Mirati Therapeutics, Inc. Crystalline forms of a KRas G12C inhibitor
MX2023003338A (es) 2020-09-23 2023-06-14 Erasca Inc Piridonas y pirimidonas tricíclicas.
US12398154B2 (en) 2020-12-15 2025-08-26 Mirati Therapeutics, Inc. Azaquinazoline pan-KRas inhibitors
EP4262803A4 (en) 2020-12-16 2025-03-12 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-kras inhibitors
US20230107642A1 (en) 2020-12-18 2023-04-06 Erasca, Inc. Tricyclic pyridones and pyrimidones
WO2022266206A1 (en) 2021-06-16 2022-12-22 Erasca, Inc. Kras inhibitor conjugates
WO2022266496A1 (en) * 2021-06-17 2022-12-22 Parker Institute For Cancer Immunotherapy Methods of treating kras mutation subtypes with cd40 agonist
WO2022271658A1 (en) * 2021-06-23 2022-12-29 Erasca, Inc. Tricyclic kras inhibitors
TW202330529A (zh) * 2021-08-10 2023-08-01 美商安進公司 雜環化合物及使用方法
EP4384177A4 (en) * 2021-08-10 2025-09-10 Amgen Inc HETEROCYCLIC COMPOUNDS AND METHODS OF USE
JP2024540935A (ja) 2021-10-20 2024-11-06 インシリコ メディシン アイピー リミテッド メチオニンアデノシルトランスフェラーゼ２ａ（ｍａｔ２ａ）阻害剤およびその使用
EP4436969A2 (en) 2021-11-24 2024-10-02 Genentech, Inc. Bicyclic therapeutic compounds and methods of use in the treatment of cancer
EP4436957A1 (en) 2021-11-24 2024-10-02 Genentech, Inc. Therapeutic indazole compounds and methods of use in the treatment of cancer
WO2023138524A1 (zh) * 2022-01-24 2023-07-27 贝达药业股份有限公司 Kras g12d降解剂及其在医药上的应用
CN121419983A (zh) 2023-01-26 2026-01-27 阿尔维纳斯运营股份有限公司 基于小脑蛋白的kras降解protac及其相关用途
AU2024241633A1 (en) 2023-03-30 2025-11-06 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
CN121712509A (zh) 2023-05-04 2026-03-20 锐新医药公司 用于ras相关疾病或病症的组合疗法
EP4720059A1 (en) 2023-05-24 2026-04-08 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
AU2024337913A1 (en) 2023-09-08 2026-03-26 Gilead Sciences, Inc. Pyrimidine-containing polycyclic derivatives as kras g12d modulating compounds
WO2025080593A1 (en) 2023-10-09 2025-04-17 Incyte Corporation Combination therapy using a kras g12d inhibitor and pd-1 inhibitor or pd-l1 inhibitor
AU2024358992A1 (en) 2023-10-09 2026-04-23 Incyte Corporation Combination comprising a kras g12d inhibitor and an egfr inhibitor for use in the treatment of cancer
IL327306A (en) 2023-10-12 2026-05-01 Revolution Medicines Inc Macrocyclic RAS inhibitors
WO2025085748A1 (en) 2023-10-20 2025-04-24 Merck Sharp & Dohme Llc Small molecule inhibitors of kras proteins
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer
WO2026090116A2 (en) 2024-10-21 2026-04-30 Revolution Medicines, Inc. Ras inhibitors
WO2026090245A1 (en) 2024-10-22 2026-04-30 Revolution Medicines, Inc. Use of ras inhibitors for treating cancer
US20260108528A1 (en) 2024-10-22 2026-04-23 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2026090323A1 (en) 2024-10-23 2026-04-30 Incyte Corporation Combination therapy using a kras g12d inhibitor, and a nucleoside analog, and/or a microtubule inhibitor and its use in the treatment of cancer
WO2026090333A1 (en) 2024-10-23 2026-04-30 Incyte Corporation Combination using a kras g12d inhibitor and chemotherapy combinations as well as their use in the treatment of cancer

Family Cites Families (148)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3381783D1 (de) 1982-03-03 1990-09-13 Genentech Inc Menschliches antithrombin iii, dns sequenzen dafuer, expressions- und klonierungsvektoren die solche sequenzen enthalten und damit transformierte zellkulturen, verfahren zur expression von menschlichem antithrombin iii und diese enthaltende pharmazeutische zusammensetzungen.
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
GB9300059D0 (en) 1992-01-20 1993-03-03 Zeneca Ltd 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
US5258389A (en) 1992-11-09 1993-11-02 Merck & Co., Inc. O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives
PT669929E (pt) 1992-11-13 2007-04-30 Immunex Corp Ligando de elk, uma citoquina
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
US5629327A (en) 1993-03-01 1997-05-13 Childrens Hospital Medical Center Corp. Methods and compositions for inhibition of angiogenesis
US5516658A (en) 1993-08-20 1996-05-14 Immunex Corporation DNA encoding cytokines that bind the cell surface receptor hek
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
PT734389E (pt) 1993-12-17 2000-09-29 Novartis Ag Derivados de rapamicina uteis como imunossupressores
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
AU702522B2 (en) 1994-04-15 1999-02-25 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
DE69536015D1 (de) 1995-03-30 2009-12-10 Pfizer Prod Inc Chinazolinone Derivate
JP4249804B2 (ja) 1995-04-03 2009-04-08 ノバルティス・アクチエンゲゼルシャフト ピラゾール誘導体およびその製造法
JP3053222B2 (ja) 1995-04-20 2000-06-19 ファイザー・インコーポレーテッド Ｍｍｐおよびｔｎｆ抑制剤としてのアリールスルホニルヒドロキサム酸誘導体
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
CZ292233B6 (cs) 1995-06-09 2003-08-13 Novartis Ag Deriváty rapamycinu a jejich použití jako léčiv
EP0836605B1 (en) 1995-07-06 2002-02-06 Novartis AG Pyrrolopyrimidines and processes for the preparation thereof
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
AU1441497A (en) 1996-01-23 1997-08-20 Novartis Ag Pyrrolopyrimidines and processes for their preparation
JP3406763B2 (ja) 1996-01-30 2003-05-12 東レ・ダウコーニング・シリコーン株式会社 シリコーンゴム組成物
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
GB9603097D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline compounds
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
US6051577A (en) 1996-03-15 2000-04-18 Novartis Ag N-7-heterocyclyl pyrrolo[2,3-D]pyrimidines and the use thereof
JP3370340B2 (ja) 1996-04-12 2003-01-27 ワーナー―ランバート・コンパニー チロシンキナーゼの不可逆的阻害剤
GB9607729D0 (en) 1996-04-13 1996-06-19 Zeneca Ltd Quinazoline derivatives
EP0907642B1 (en) 1996-06-24 2005-11-02 Pfizer Inc. Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases
US6258823B1 (en) 1996-07-12 2001-07-10 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
EA199900021A1 (ru) 1996-07-13 1999-08-26 Глаксо, Груп Лимитед Бициклические гетероароматические соединения в качестве ингибиторов протеинтирозинкиназы
DE69716916T2 (de) 1996-07-13 2003-07-03 Glaxo Group Ltd., Greenford Kondensierte heterozyklische verbindungen als protein kinase inhibitoren
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
CA2260898C (en) 1996-07-18 2002-05-14 Pfizer Limited Phosphinate based inhibitors of matrix metalloproteases
DE69738749D1 (de) 1996-08-16 2008-07-17 Schering Corp Zelloberflächen-antigen aus säugetieren und verwandte reagenzien
US6111090A (en) 1996-08-16 2000-08-29 Schering Corporation Mammalian cell surface antigens; related reagents
PL331895A1 (en) 1996-08-23 1999-08-16 Pfizer Arylosulphonylamino derivatives of hydroxamic acid
AU720429B2 (en) 1996-08-23 2000-06-01 Novartis Ag Substituted pyrrolopyrimidines and processes for their preparation
ES2239779T3 (es) 1996-10-02 2005-10-01 Novartis Ag Derivados de pirimidina y procedimientos para la preparacion de los mismos.
AU4779897A (en) 1996-10-02 1998-04-24 Novartis Ag Fused pyrazole derivatives and processes for their preparation
ID18494A (id) 1996-10-02 1998-04-16 Novartis Ag Turunan pirazola leburan dan proses pembuatannya
EP0837063A1 (en) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
GB9621757D0 (en) 1996-10-18 1996-12-11 Ciba Geigy Ag Phenyl-substituted bicyclic heterocyclyl derivatives and their use
DE69730151T2 (de) 1997-01-06 2005-08-04 Pfizer Inc. Cyclische sulfonderivate
AU721748B2 (en) 1997-02-03 2000-07-13 Pfizer Products Inc. Arylsulfonylamino hydroxamic acid derivatives
KR20000070751A (ko) 1997-02-05 2000-11-25 로즈 암스트롱, 크리스틴 에이. 트러트웨인 세포 증식 억제제로서의 피리도[2,3-ｄ]피리미딘 및 4-아미노피리미딘
CA2279863A1 (en) 1997-02-07 1998-08-13 Pfizer Inc. N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases
WO1998034918A1 (en) 1997-02-11 1998-08-13 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
WO1999007701A1 (en) 1997-08-05 1999-02-18 Sugen, Inc. Tricyclic quinoxaline derivatives as protein tyrosine kinase inhibitors
ID23668A (id) 1997-08-08 2000-05-11 Pfizer Prod Inc Turunan asam ariloksiarilsulfonilamino hidroksamat
WO1999020758A1 (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
JP2002502607A (ja) 1998-02-09 2002-01-29 ジェネンテク・インコーポレイテッド 新規な腫瘍壊死因子レセプター相同体及びそれをコードする核酸
ES2324846T3 (es) 1998-03-04 2009-08-17 Bristol-Myers Squibb Company Inhibidores de la proteina tirosina quinasa de imidazopirazina heterociclo-sustituida.
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
IL139934A0 (en) 1998-05-29 2002-02-10 Sugen Inc Pyrrole substituted 2-indolinone derivatives and pharmaceutical compositions containing the same
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
CA2336848A1 (en) 1998-07-10 2000-01-20 Merck & Co., Inc. Novel angiogenesis inhibitors
EP1109555A4 (en) 1998-08-31 2001-11-21 Merck & Co Inc Novel angiogenesis inhibitors
DK1004578T3 (da) 1998-11-05 2004-06-28 Pfizer Prod Inc 5-oxo-pyrrolidin-2-carboxylsyrehydroxamidderivater
CA2359244C (en) 1999-01-13 2013-10-08 Bayer Healthcare Llc .omega.-carboxy aryl substituted diphenyl ureas as p38 kinase inhibitors
JP4673977B2 (ja) 1999-03-30 2011-04-20 ノバルティス アーゲー 炎症性疾患治療用フタラジン誘導体
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
ATE324444T1 (de) 1999-06-07 2006-05-15 Immunex Corp Tek-antagonisten
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.
AU783158B2 (en) 1999-08-24 2005-09-29 Ariad Pharmaceuticals, Inc. 28-epirapalogs
CN100376567C (zh) 1999-11-05 2008-03-26 阿斯特拉曾尼卡有限公司 作为vegf抑制剂的喹唑啉衍生物
DK1233943T3 (da) 1999-11-24 2011-08-15 Sugen Inc Ioniserbare indolinon derivater og anvendelse deraf som PTK ligander
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
EP1259595B1 (en) 2000-02-25 2007-04-04 Immunex Corporation Integrin antagonists
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
US20020147198A1 (en) 2001-01-12 2002-10-10 Guoqing Chen Substituted arylamine 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
US7105682B2 (en) 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
US6995162B2 (en) 2001-01-12 2006-02-07 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
WO2005005434A1 (en) 2003-07-08 2005-01-20 Novartis Ag Use of rapamycin and rapamycin derivatives for the treatment of bone loss
US20050048054A1 (en) 2003-07-11 2005-03-03 Shino Hanabuchi Lymphocytes; methods
EP1648900A4 (en) 2003-07-11 2010-02-10 Ariad Pharma Inc PHOSPHORUS 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
WO2005055808A2 (en) 2003-12-02 2005-06-23 Genzyme Corporation Compositions and methods to diagnose and treat lung cancer
GB0409799D0 (en) 2004-04-30 2004-06-09 Isis Innovation Method of generating improved immune response
US20060002932A1 (en) 2004-06-04 2006-01-05 Duke University Methods and compositions for enhancement of immunity by in vivo depletion of immunosuppressive cell activity
GEP20104906B (en) 2004-08-26 2010-02-25 Pfizer Enantiomerically pure aminoheteroaryl compounds as protein kinase inhibitors
CN101039952A (zh) 2004-10-13 2007-09-19 惠氏公司 作为pi3k抑制剂的17－羟基渥曼青霉素类似物
AU2006230099B2 (en) 2005-03-25 2012-04-19 Gitr, Inc. GITR binding molecules and uses therefor
PL2161336T5 (pl) 2005-05-09 2017-10-31 Ono Pharmaceutical Co Ludzkie przeciwciała monoklonalne przeciwko białku Programmed Death 1 (PD-1) oraz sposoby leczenia raka z zastosowaniem samych przeciwciał anty-PD-1 lub w połączeniu z innymi środkami immunoterapeutycznymi
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
CA2622870A1 (en) 2005-09-20 2007-03-29 Pfizer Products Inc. Dosage forms and methods of treatment using a tyrosine kinase inhibitor
WO2007133822A1 (en) 2006-01-19 2007-11-22 Genzyme Corporation Gitr antibodies for the treatment of cancer
WO2008070740A1 (en) 2006-12-07 2008-06-12 F.Hoffmann-La Roche Ag Phosphoinositide 3-kinase inhibitor compounds and methods of use
CN101801413A (zh) 2007-07-12 2010-08-11 托勒克斯股份有限公司 采用gitr结合分子的联合疗法
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
EP2214675B1 (en) 2007-10-25 2013-11-20 Genentech, Inc. Process for making thienopyrimidine compounds
KR20110044992A (ko) 2008-07-02 2011-05-03 이머전트 프로덕트 디벨롭먼트 시애틀, 엘엘씨 ＴＧＦ-β 길항제 다중-표적 결합 단백질
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
PT3023438T (pt) 2009-09-03 2020-05-08 Merck Sharp & Dohme Anticorpos anti-gitr
GB0919054D0 (en) 2009-10-30 2009-12-16 Isis Innovation Treatment of obesity
SI2519543T1 (sl) 2009-12-29 2016-08-31 Emergent Product Development Seattle, Llc Beljakovine, ki se vežejo s heterodimeri in njihova uporaba
WO2013039954A1 (en) 2011-09-14 2013-03-21 Sanofi Anti-gitr antibodies
CA3048217A1 (en) 2016-12-22 2018-06-28 Amgen Inc. Kras g12c inhibitors and methods of using the same
ES2905676T3 (es) 2017-05-22 2022-04-11 Amgen Inc Inhibidores de KRAS G12C y métodos para su uso
CN111051306B (zh) 2017-09-08 2023-01-03 美国安进公司 Kras g12c的抑制剂及其使用方法

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