CN101282960A - Raf抑制剂化合物和方法 - Google Patents

Raf抑制剂化合物和方法 Download PDF

Info

Publication number
CN101282960A
CN101282960A CNA2006800109351A CN200680010935A CN101282960A CN 101282960 A CN101282960 A CN 101282960A CN A2006800109351 A CNA2006800109351 A CN A2006800109351A CN 200680010935 A CN200680010935 A CN 200680010935A CN 101282960 A CN101282960 A CN 101282960A
Authority
CN
China
Prior art keywords
compound
pyridin
pyrazol
alkyl
cancer
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.)
Pending
Application number
CNA2006800109351A
Other languages
English (en)
Chinese (zh)
Inventor
埃伦·莱尔德
约瑟夫·P·利西卡托斯
迈克·韦尔奇
乔纳斯·格林纳
乔希·汉森
布雷德·纽豪斯
艾伦·奥利弗罗
乔治·托波拉夫
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Genentech Inc
Array Biopharma Inc
Original Assignee
Genentech Inc
Array Biopharma Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Genentech Inc, Array Biopharma Inc filed Critical Genentech Inc
Publication of CN101282960A publication Critical patent/CN101282960A/zh
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Communicable Diseases (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Virology (AREA)
CNA2006800109351A 2005-02-04 2006-02-02 Raf抑制剂化合物和方法 Pending CN101282960A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US65005005P 2005-02-04 2005-02-04
US60/650,050 2005-02-04

Publications (1)

Publication Number Publication Date
CN101282960A true CN101282960A (zh) 2008-10-08

Family

ID=36571626

Family Applications (1)

Application Number Title Priority Date Filing Date
CNA2006800109351A Pending CN101282960A (zh) 2005-02-04 2006-02-02 Raf抑制剂化合物和方法

Country Status (18)

Country Link
US (2) US7491829B2 (cg-RX-API-DMAC10.html)
EP (1) EP1846391A2 (cg-RX-API-DMAC10.html)
JP (1) JP2008530011A (cg-RX-API-DMAC10.html)
KR (1) KR20070107104A (cg-RX-API-DMAC10.html)
CN (1) CN101282960A (cg-RX-API-DMAC10.html)
AR (1) AR053014A1 (cg-RX-API-DMAC10.html)
AU (1) AU2006210626A1 (cg-RX-API-DMAC10.html)
BR (1) BRPI0607346A2 (cg-RX-API-DMAC10.html)
CA (1) CA2596973A1 (cg-RX-API-DMAC10.html)
CR (1) CR9365A (cg-RX-API-DMAC10.html)
IL (1) IL185024A0 (cg-RX-API-DMAC10.html)
MA (1) MA29310B1 (cg-RX-API-DMAC10.html)
MX (1) MX2007009405A (cg-RX-API-DMAC10.html)
NO (1) NO20074473L (cg-RX-API-DMAC10.html)
RU (1) RU2007133111A (cg-RX-API-DMAC10.html)
TW (1) TW200639163A (cg-RX-API-DMAC10.html)
WO (1) WO2006084015A2 (cg-RX-API-DMAC10.html)
ZA (1) ZA200707289B (cg-RX-API-DMAC10.html)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102666498A (zh) * 2009-08-28 2012-09-12 健泰科生物技术公司 Raf抑制剂化合物及其使用方法
WO2023098439A1 (zh) * 2021-11-30 2023-06-08 上海和誉生物医药科技有限公司 一种吡唑衍生物,其制备方法和在药学上的应用
WO2024022186A1 (zh) * 2022-07-29 2024-02-01 四川科伦博泰生物医药股份有限公司 甲基吡唑化合物、包含其的药物组合物及其制备方法和用途
CN117510491A (zh) * 2016-12-23 2024-02-06 阿尔维纳斯运营股份有限公司 用于迅速加速性纤维肉瘤多肽的靶向降解的化合物和方法

Families Citing this family (88)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2007305016B2 (en) 2006-10-02 2011-11-03 Novartis Ag Compounds and compositions as protein kinase inhibitors
CN101611016B (zh) * 2006-10-17 2012-01-25 斯蒂菲尔实验室公司 他拉罗唑代谢物
JP2010540451A (ja) * 2007-09-20 2010-12-24 ワイス・エルエルシー ピラゾロ[5,1−c][1,2,4]トリアジン、その調製法および使用法
CA2716947A1 (en) * 2008-02-29 2009-09-11 Array Biopharma Inc. Imidazo [4,5-b] pyridine derivatives used as raf inhibitors
AR072657A1 (es) * 2008-02-29 2010-09-15 Genentech Inc Compuestos inhibidores de raf y metodos para su uso
WO2009111260A1 (en) * 2008-02-29 2009-09-11 Wyeth Phenylsulfonamide-substituted, pyrazolo[1, 5-a]pyrimidines, methods for preparation and uses thereof
US20110003859A1 (en) * 2008-02-29 2011-01-06 Array Biopharma Inc. N- (6-aminopyridin-3-yl) -3- (sulfonamido) benzamide derivatives as b-raf inhibitors for the treatment of cancer
WO2009111278A2 (en) * 2008-02-29 2009-09-11 Array Biopharma Inc. Raf inhibitor compounds and methods of use thereof
WO2009108827A1 (en) * 2008-02-29 2009-09-03 Wyeth Fused tricyclic pyrazolo[1, 5-a]pyrimidines, methods for preparation and uses thereof
JP2009286773A (ja) * 2008-03-14 2009-12-10 Bayer Cropscience Ag 殺虫性縮環式アリール類
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
JP2011523646A (ja) 2008-05-21 2011-08-18 アリアド・ファーマシューティカルズ・インコーポレイテッド キナーゼ阻害剤としてのリン誘導体
EP2381777A4 (en) * 2008-12-12 2012-08-08 Ariad Pharma Inc AZAINDOL DERIVATIVES AS KINASEHEMMER
US8765747B2 (en) 2009-06-12 2014-07-01 Dana-Farber Cancer Institute, Inc. Fused 2-aminothiazole compounds
SG178854A1 (en) 2009-08-28 2012-04-27 Array Biopharma Inc Raf inhibitor compounds and methods of use thereof
EP2470538A1 (en) 2009-08-28 2012-07-04 Array Biopharma, Inc. Raf inhibitor compounds and methods of use thereof
CN102858754A (zh) 2009-08-28 2013-01-02 阵列生物制药公司 Raf抑制剂化合物及其使用方法
US20120157452A1 (en) 2009-08-28 2012-06-21 Genentech, Inc. 1h-pyrazolo[3,4-b] pyridine compounds for inhibiting raf kinase
SG178853A1 (en) 2009-08-28 2012-04-27 Array Biopharma Inc Raf inhibitor compounds and methods of use thereof
WO2011051478A1 (en) * 2009-10-30 2011-05-05 Domain Therapeutics Novel oxime derivatives and their use as allosteric modulators of metabotropic glutamate receptors
EP2937345B1 (en) 2009-12-29 2018-03-21 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
PH12012501361A1 (en) 2009-12-31 2012-10-22 Centro Nac De Investigaciones Oncologicas Cnio Tricyclic compounds for use as kinase inhibitors
US20120122928A1 (en) 2010-08-11 2012-05-17 Bayer Cropscience Ag Heteroarylpiperidine and -Piperazine Derivatives as Fungicides
US8759527B2 (en) 2010-08-25 2014-06-24 Bayer Cropscience Ag Heteroarylpiperidine and -piperazine derivatives as fungicides
EP2423210A1 (de) 2010-08-25 2012-02-29 Bayer CropScience AG Heteroarylpiperidin- und -piperazinderivate als Fungizide
EP2632922B1 (de) 2010-10-27 2019-02-27 Bayer CropScience Aktiengesellschaft Heteroarylpiperidin und -piperazinderivate als fungizide
CA2824028A1 (en) 2011-01-06 2012-07-12 Beta Pharma Canada Inc. Novel ureas for the treatment and prevention of cancer
WO2012098387A1 (en) 2011-01-18 2012-07-26 Centro Nacional De Investigaciones Oncológicas (Cnio) 6, 7-ring-fused triazolo [4, 3 - b] pyridazine derivatives as pim inhibitors
WO2012104273A1 (de) 2011-02-01 2012-08-09 Bayer Cropscience Ag Heteroarylpiperidin und -piperazinderivate als fungizide
WO2012145503A1 (en) 2011-04-21 2012-10-26 Novartis Ag Pharmaceutical combinations
AU2012250517B2 (en) 2011-05-04 2016-05-19 Takeda Pharmaceutical Company Limited Compounds for inhibiting cell proliferation in EGFR-driven cancers
BR112014002353B1 (pt) 2011-08-01 2022-09-27 Genentech, Inc Usos de antagonistas de ligação do eixo pd-1 e inibidores de mek, composições farmacêuticas, e kit
AU2012312515A1 (en) 2011-09-19 2014-03-13 Genentech, Inc. Combination treatments comprising c-met antagonists and B-raf antagonists
JP6106685B2 (ja) 2011-11-17 2017-04-05 ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド C−jun−n−末端キナーゼ(jnk)の阻害剤
US9408885B2 (en) 2011-12-01 2016-08-09 Vib Vzw Combinations of therapeutic agents for treating melanoma
ES2695233T3 (es) 2011-12-27 2019-01-02 Bayer Cropscience Ag Derivados de isoxazol
DK2797888T3 (en) * 2011-12-31 2016-09-19 Beigene Ltd Fused tricyclic compounds as RAF kinase inhibitors
JP6469567B2 (ja) 2012-05-05 2019-02-13 アリアド・ファーマシューティカルズ・インコーポレイテッド Egfr発動性がんの細胞増殖阻害用化合物
DK2884979T3 (da) 2012-08-17 2019-09-02 Hoffmann La Roche Kombinationsbehandlinger mod melanom omfattende indgivelse af cobimetinib og vemurafenib
EP2909194A1 (en) 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
USRE48175E1 (en) 2012-10-19 2020-08-25 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
US10000483B2 (en) 2012-10-19 2018-06-19 Dana-Farber Cancer Institute, Inc. Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
WO2014128235A1 (en) 2013-02-22 2014-08-28 F. Hoffmann-La Roche Ag Methods of treating cancer and preventing drug resistance
JO3383B1 (ar) * 2013-03-14 2019-03-13 Lilly Co Eli مثبطات cdc7
HK1214533A1 (zh) 2013-03-15 2016-07-29 基因泰克公司 治疗癌症和预防癌症耐药性的方法
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
WO2014206344A1 (en) 2013-06-28 2014-12-31 Beigene, Ltd. Fused tricyclic amide compounds as multiple kinase inhibitors
SMT202300039T1 (it) 2013-09-13 2023-03-17 Beigene Switzerland Gmbh Anticorpi anti-pd1 e loro uso come terapia e per diagnostica
US9629851B2 (en) 2013-09-20 2017-04-25 Stitching Het Nederlands Kanker Institut—Antoni Van Leeuwenhoek Ziekenhuis ROCK in combination with MAPK pathway
WO2015041534A1 (en) 2013-09-20 2015-03-26 Stichting Het Nederlands Kanker Instituut P90rsk in combination with raf/erk/mek
WO2015058126A1 (en) 2013-10-18 2015-04-23 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
AU2014337044A1 (en) 2013-10-18 2016-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
EP3122900A1 (en) 2014-03-24 2017-02-01 F. Hoffmann-La Roche AG Cancer treatment with c-met antagonists and correlation of the latter with hgf expression
US20170027940A1 (en) 2014-04-10 2017-02-02 Stichting Het Nederlands Kanker Instituut Method for treating cancer
US9862688B2 (en) 2014-04-23 2018-01-09 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
WO2015164614A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
WO2015178770A1 (en) 2014-05-19 2015-11-26 Stichting Het Nederlands Kanker Instituut Compositions for cancer treatment
WO2015191986A1 (en) 2014-06-13 2015-12-17 Genentech, Inc. Methods of treating and preventing cancer drug resistance
US20170114323A1 (en) 2014-06-19 2017-04-27 Whitehead Institute For Biomedical Research Uses of kinase inhibitors for inducing and maintaining pluripotency
TWI726608B (zh) 2014-07-03 2021-05-01 英屬開曼群島商百濟神州有限公司 抗pd-l1抗體及其作為治療及診斷之用途
BR112017000672A2 (pt) 2014-07-15 2017-11-14 Genentech Inc composições para tratamento de câncer utilizando antagonistas de ligação de eixo pd-1 e inibidores de mek
KR102524920B1 (ko) 2014-07-22 2023-04-25 아폴로믹스 인코포레이티드 항-pd-1 항체
SG10201901057UA (en) 2014-08-05 2019-03-28 Cb Therapeutics Inc Anti-pd-l1 antibodies
US10870651B2 (en) 2014-12-23 2020-12-22 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
CN107427521B (zh) 2015-03-27 2021-08-03 达纳-法伯癌症研究所股份有限公司 细胞周期蛋白依赖性激酶的抑制剂
AU2016248376B2 (en) 2015-04-15 2020-10-08 Beone Medicines I Gmbh Maleate salts of a B-RAF kinase inhibitor, crystalline forms, methods of preparation, and uses therefore
CA2986441A1 (en) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
WO2017044858A2 (en) 2015-09-09 2017-03-16 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
WO2017087851A1 (en) 2015-11-19 2017-05-26 Genentech, Inc. Methods of treating cancer using b-raf inhibitors and immune checkpoint inhibitors
WO2018007885A1 (en) 2016-07-05 2018-01-11 Beigene, Ltd. COMBINATION OF A PD-l ANTAGONIST AND A RAF INHIBITOR FOR TREATING CANCER
CN110087680B (zh) 2016-08-19 2024-03-19 百济神州有限公司 使用包含btk抑制剂的组合产品治疗癌症
IL266842B (en) 2016-12-01 2022-09-01 Arvinas Operations Inc History of tetrahydronaphthalene and tetrahydroisoquinoline as estrogen receptor antagonists
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
EP3573989A4 (en) 2017-01-25 2020-11-18 Beigene, Ltd. CRYSTALLINE FORMS OF (S) -7- (1- (BUT-2-YNOYL) PIPERIDIN-4-YL) -2- (4-PHENOXYPHENYL) -4, 5, 6, 7-TETRAHY DROPYRAZOLO [1, 5-A ] PYRIMIDINE-3-CARBOXAMIDE, PREPARATION AND ASSOCIATED USES
EP3579872A1 (en) 2017-02-10 2019-12-18 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of cancers associated with activation of the mapk pathway
EP3645569A4 (en) 2017-06-26 2021-03-24 BeiGene, Ltd. IMMUNOTHERAPY FOR LIVER CELL CARCINOMA
US11786529B2 (en) 2017-11-29 2023-10-17 Beigene Switzerland Gmbh Treatment of indolent or aggressive B-cell lymphomas using a combination comprising BTK inhibitors
CA3086765A1 (en) 2017-12-28 2019-07-04 Tract Pharmaceuticals, Inc. Stem cell culture systems for columnar epithelial stem cells, and uses related thereto
EP3810132A4 (en) 2018-06-25 2022-06-22 Dana-Farber Cancer Institute, Inc. TAIRE FAMILY KINASE INHIBITORS AND RELATED USES
CN113164477A (zh) 2018-12-14 2021-07-23 达纳-法伯癌症研究所股份有限公司 C-jun-n-末端激酶的吡唑并吡啶抑制剂及其用途
EP3902542A4 (en) 2018-12-28 2022-09-07 Dana-Farber Cancer Institute, Inc. CYCLIN DEPENDENT KINASE 7 INHIBITORS AND USES THEREOF
WO2021041348A1 (en) 2019-08-26 2021-03-04 Arvinas Operations, Inc. Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
WO2021120890A1 (en) * 2019-12-20 2021-06-24 Novartis Ag Pyrazolyl derivatives useful as anti-cancer agents
WO2022047145A1 (en) 2020-08-28 2022-03-03 Arvinas Operations, Inc. Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use
AU2021342287A1 (en) 2020-09-14 2023-04-13 Arvinas Operations, Inc. Crystalline forms of a compound for the targeted degradation of estrogen receptor
EP4237412A4 (en) * 2020-10-30 2024-04-10 Novartis AG NEW CRYSTALLINE FORMS OF A KRAS G12C INHIBITOR COMPOUND
US12371667B2 (en) 2021-05-13 2025-07-29 Washington University Enhanced methods for inducing and maintaining naive human pluripotent stem cells
EP4584258A1 (en) 2022-09-07 2025-07-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use

Family Cites Families (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1245283A (en) 1968-10-04 1971-09-08 Labaz Pyrazole derivatives
JP2753659B2 (ja) 1990-09-03 1998-05-20 株式会社大塚製薬工場 ピラゾール誘導体
US5356897A (en) 1991-09-09 1994-10-18 Fujisawa Pharmaceutical Co., Ltd. 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines
JPH05125079A (ja) 1991-11-05 1993-05-21 Otsuka Pharmaceut Factory Inc ピラゾロ[1,5−aピリミジン誘導体
EP0714898B1 (en) 1994-06-21 2001-11-14 Otsuka Pharmaceutical Factory, Inc. PYRAZOLO [1,5-a]PYRIMIDINE DERIVATIVE
US5486534A (en) 1994-07-21 1996-01-23 G. D. Searle & Co. 3,4-substituted pyrazoles for the treatment of inflammation
US5843951A (en) 1995-09-28 1998-12-01 Otsuka Pharmaceutical Factory Inc. Analgesic composition of pyrazolo(1,5-A) pyrimidines
JPH10101672A (ja) 1996-08-06 1998-04-21 Otsuka Pharmaceut Factory Inc アデノシン増強剤
JPH10101671A (ja) 1996-08-08 1998-04-21 Otsuka Pharmaceut Factory Inc 一酸化窒素合成酵素阻害剤
US5932576A (en) 1997-05-22 1999-08-03 G. D. Searle & Company 3(5)-heteroaryl substituted pyrazoles as p38 kinase inhibitors
US6514977B1 (en) 1997-05-22 2003-02-04 G.D. Searle & Company Substituted pyrazoles as p38 kinase inhibitors
JP2000153671A (ja) 1998-11-20 2000-06-06 Fuji Photo Film Co Ltd 感熱記録材料
AU4556800A (en) 1999-04-27 2000-11-10 Smithkline Beecham Plc Novel treatment
TWI271406B (en) 1999-12-13 2007-01-21 Eisai Co Ltd Tricyclic condensed heterocyclic compounds, preparation method of the same and pharmaceuticals comprising the same
JP4739632B2 (ja) 2000-02-05 2011-08-03 バーテックス ファーマシューティカルズ インコーポレイテッド Erkのインヒビターとして有用なピラゾール組成物
JP4783532B2 (ja) 2000-02-05 2011-09-28 バーテックス ファーマシューティカルズ インコーポレイテッド Erkのインヒビターとして有用なピラゾール組成物
EP1207864A2 (en) 2000-02-05 2002-05-29 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of erk
EP1263753B1 (en) 2000-03-06 2004-05-06 SmithKline Beecham plc Imidazol derivatives as raf kinase inhibitors
WO2002024680A1 (en) 2000-09-21 2002-03-28 Smithkline Beecham P.L.C. Imidazole derivatives as raf kinase inhibitors
AU2002226674B2 (en) 2000-12-28 2007-03-22 Ono Pharmaceutical Co., Ltd. Tricyclic and heterocyclic derivative compounds and drugs containing these compounds as the active ingredient
ES2296910T3 (es) 2001-01-22 2008-05-01 Sankyo Company, Limited Compuestos sustituidos con grupo amino biciclicos.
WO2002072576A1 (en) * 2001-03-09 2002-09-19 Pfizer Products Inc. Benzimidazole anti-inflammatory compounds
EP2048142A3 (en) * 2001-04-26 2009-04-22 Eisai R&D Management Co., Ltd. Nitrogen-containing condensed cyclic compound having a pyrazolyl group as a substituent group and pharmaceutical composition thereof
GB0112348D0 (en) 2001-05-19 2001-07-11 Smithkline Beecham Plc Compounds
SI1397364T1 (sl) * 2001-05-24 2007-12-31 Lilly Co Eli Novi pirolni derivati kot farmacevtske uäśinkovine
US6875789B2 (en) 2001-08-03 2005-04-05 Vertex Pharmaceuticals Incorporated Pyrazole-derived kinase inhibitors and uses thereof
US6750239B2 (en) 2001-08-03 2004-06-15 Vertex Pharmaceuticals Incorporated Pyrazole-derived kinase inhibitors and uses thereof
GB0121494D0 (en) 2001-09-05 2001-10-24 Smithkline Beecham Plc Compounds
GB0121490D0 (en) 2001-09-05 2001-10-24 Smithkline Beecham Plc Ciompounds
US6897208B2 (en) 2001-10-26 2005-05-24 Aventis Pharmaceuticals Inc. Benzimidazoles
US20040010027A1 (en) * 2001-12-17 2004-01-15 Pharmacia & Upjohn Spa Hydroxphenyl-pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical comositions comprising them
JP4286146B2 (ja) * 2001-12-18 2009-06-24 メルク エンド カムパニー インコーポレーテッド メタボトロピックグルタミン酸受容体−5のヘテロアリール置換ピラゾール系調節剤
JP4399265B2 (ja) 2001-12-21 2010-01-13 ヴァーナリス(ケンブリッジ)リミテッド 3,4−ジアリールピラゾール、および癌の治療におけるそれらの使用
WO2003095455A2 (en) 2002-05-10 2003-11-20 Smithkline Beecham Corporation Substituted pyrazolopyrimidines
GB0217786D0 (en) 2002-07-31 2002-09-11 Glaxo Group Ltd Compounds
EP1539748A1 (en) 2002-07-31 2005-06-15 Smithkline Beecham Corporation 2-phenylpyridin-4-yl derivatives as alk5 inhibitors
AU2003256297A1 (en) 2002-08-09 2004-02-25 Eli Lilly And Company Benzimidazoles and benzothiazoles as inhibitors of map kinase
JP2006501263A (ja) 2002-09-09 2006-01-12 アムジエン・インコーポレーテツド 炎症治療用のTNF−αおよびインターロイキン低下剤としての1,4,5−置換1,2−ジヒドロ−ピラゾール−3−オンおよび3−アルコキシ−1H−ピラゾール誘導体
WO2004026871A1 (en) * 2002-09-17 2004-04-01 Eli Lilly And Company Novel pyrazolopyridine derivatves as pharmaceutical agents
WO2004026306A2 (en) 2002-09-18 2004-04-01 Pfizer Products Inc. Pyrazole derivatives as transforming growth factor (tgf) inhibitors
WO2004026302A1 (en) 2002-09-19 2004-04-01 Eli Lilly And Company Methods of inhibiting tgf beta with substituted pyrazoles
US7405299B2 (en) * 2002-11-27 2008-07-29 Eli Lilly And Company Compounds as pharmaceutical agents
US7176210B2 (en) 2003-02-10 2007-02-13 Pfizer Inc. Cannabinoid receptor ligands and uses thereof
CL2004000234A1 (es) 2003-02-12 2005-04-15 Biogen Idec Inc Compuestos derivados 3-(piridin-2-il)-4-heteroaril-pirazol sustituidos, antagonistas de aik5 y/o aik4; composicion farmaceutica y uso del compuesto en el tratamiento de desordenes fibroticos como esclerodermia, lupus nefritico, cicatrizacion de herid
GB0313915D0 (en) * 2003-06-16 2003-07-23 Smithkline Beecham Corp Compounds

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102666498A (zh) * 2009-08-28 2012-09-12 健泰科生物技术公司 Raf抑制剂化合物及其使用方法
CN117510491A (zh) * 2016-12-23 2024-02-06 阿尔维纳斯运营股份有限公司 用于迅速加速性纤维肉瘤多肽的靶向降解的化合物和方法
WO2023098439A1 (zh) * 2021-11-30 2023-06-08 上海和誉生物医药科技有限公司 一种吡唑衍生物,其制备方法和在药学上的应用
CN117730075A (zh) * 2021-11-30 2024-03-19 上海和誉生物医药科技有限公司 一种吡唑衍生物,其制备方法和在药学上的应用
WO2024022186A1 (zh) * 2022-07-29 2024-02-01 四川科伦博泰生物医药股份有限公司 甲基吡唑化合物、包含其的药物组合物及其制备方法和用途

Also Published As

Publication number Publication date
MX2007009405A (es) 2007-09-25
BRPI0607346A2 (pt) 2009-09-01
WO2006084015A2 (en) 2006-08-10
JP2008530011A (ja) 2008-08-07
ZA200707289B (en) 2009-09-30
AR053014A1 (es) 2007-04-18
KR20070107104A (ko) 2007-11-06
CR9365A (es) 2008-01-15
RU2007133111A (ru) 2009-03-10
US20060189627A1 (en) 2006-08-24
US20090176809A1 (en) 2009-07-09
EP1846391A2 (en) 2007-10-24
MA29310B1 (fr) 2008-03-03
AU2006210626A1 (en) 2006-08-10
CA2596973A1 (en) 2006-08-10
WO2006084015A3 (en) 2006-11-23
NO20074473L (no) 2007-10-31
US7491829B2 (en) 2009-02-17
IL185024A0 (en) 2007-12-03
TW200639163A (en) 2006-11-16

Similar Documents

Publication Publication Date Title
US7491829B2 (en) RAF inhibitor compounds and methods
US7566716B2 (en) Imidazopyrazines as Raf inhibitor compounds
JP6312634B2 (ja) ピラゾロピリミジンjak阻害剤化合物及び方法
CN109952295B (zh) 一种cdk4/6抑制剂及其制备方法和应用
KR101749192B1 (ko) 트리아진, 피리미딘 및 피리딘 유사체 및 이의 치료제 및 진단 프로브로의 용도
JP5769199B2 (ja) ピラゾロピリミジンjak阻害剤化合物と方法
JP2023082088A (ja) Prmt5阻害剤としての置換イミダゾリジン-2-オン誘導体
KR20080052630A (ko) Raf 억제제 화합물 및 그의 사용 방법
JP2011525193A (ja) トリアゾロピリジンjak阻害剤化合物と方法
CN106573906A (zh) 哌啶‑二酮衍生物
JP2010538094A (ja) チロシンキナーゼ阻害剤としてのピラゾロピリジン類
KR20230154436A (ko) 아미노피리미딘 화합물 및 그의 사용 방법
KR101254546B1 (ko) 신규 메틸이소퀴놀리논 치환된 트리아졸로피리다진 유도체 또는 이의 약학적으로 허용 가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 이상세포 성장 질환의 예방 또는 치료용 약학적 조성물
JP2011522890A (ja) 置換されたピロール及び使用方法
HK40103326A (en) Aminopyrimidine compounds and methods of their use
HK40057478B (en) Hpk1 inhibitors and methods of using same
HK1159947A (en) Triazolopyridine jak inhibitor compounds and methods

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C02 Deemed withdrawal of patent application after publication (patent law 2001)
WD01 Invention patent application deemed withdrawn after publication

Open date: 20081008