PE20151776A1 - Compuestos de heteroarilo y sus usos - Google Patents

Compuestos de heteroarilo y sus usos

Info

Publication number
PE20151776A1
PE20151776A1 PE2015002022A PE2015002022A PE20151776A1 PE 20151776 A1 PE20151776 A1 PE 20151776A1 PE 2015002022 A PE2015002022 A PE 2015002022A PE 2015002022 A PE2015002022 A PE 2015002022A PE 20151776 A1 PE20151776 A1 PE 20151776A1
Authority
PE
Peru
Prior art keywords
diseases
optionally substituted
compounds
bivalent
halogen
Prior art date
Application number
PE2015002022A
Other languages
English (en)
Inventor
Laura Akullian D'agostino
Robert Tjin Tham Sjin
Deqiang Niu
Joseph John Mcdonald
Zhendong Zhu
Haibo Liu
Hormoz Mazdiyasni
Russell C Petter
Juswinder Singh
Matthieu Barrague
Alexandre Gross
Mark Munson
Darren Harvey
Andrew Scholte
Sachin Maniar
Original Assignee
Celgene Avilomics Res Inc
Sanofi Sa
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 Celgene Avilomics Res Inc, Sanofi Sa filed Critical Celgene Avilomics Res Inc
Publication of PE20151776A1 publication Critical patent/PE20151776A1/es

Links

Classifications

    • 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
    • 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
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/80—Oxygen atoms
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (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)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Reproductive Health (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epidemiology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

SE REFIERE A COMPUESTOS DE FORMULA I O SALES FARMACEUTICAMENTE ACEPTABLES DE LOS MISMOS, EN LOS CUALES X1 ES NH, N, CH2 o CH, ENTRE OTROS; X2 ES NH, N, CH2 o CH, ENTRE OTROS; X3 Y X4 SON INDEPENDIENTEMENTE N o CH, ENTRE OTROS; X5 ES N, C o CH; EN DONDE AL MENOS UNO DE X1, X2, X3, X4 o X5 ES N; G ES H, O, OH o NH2, ENTRE OTROS; A ES FENILO OPCIONALMENTE SUSTITUIDO, UN ANILLO CARBOCICLICO C3-8 OPCIONALMENTE SUSTITUIDO, O UN ANILLO HETEROCICLICO DE 4-7 MIEMBROS CONTENIENDO 1-4 HETEROATOMOS (O, N o S) OPCIONALMENTE SUSTITUIDO, ENTRE OTROS; R1 ES -L-Y, DONDE L ES UNA CADENA DE HIDROCARBURO C2-8 BIVALENTE, ENTRE OTROS, E Y ES H, HALOGENO, NO2 O CN, ENTRE OTROS; CADA R2 ES INDEPENDIENTEMENTE H, HALOGENO, OH, SH, CN, NO2, SO2H, C(O)H, C(O)OH, C(O)NH2, NH2, ENTRE OTROS; R3 ESTA AUSENTE, O ES H, ALQUENILO C2-6 O ALQUILO C1-6, ENTRE OTROS; Y ES O o NH, ENTRE OTROS; T ES UN ENLACE COVALENTE O UNA CADENA DE HIDROCARBURO C1-6 BIVALENTE, ENTRE OTROS; Y q ES 0-6. DICHOS COMPUESTOS SON INHIBIDORES DE UNA O VARIAS PROTEINAS CINASAS (EN PARTICULAR DE FGFR4) QUE CONTIENEN UN RESIDUO DE CISTEINA EN EL SITIO DE UNION A ATP, POR LO CUAL SON UTILES EN LA TERAPIA DE UNA VARIEDAD DE ENFERMEDADES, TRASTORNOS O AFECCIONES ASICOADAS CON RESPUESTAS CELULARES ANORMALES DESENCADENADAS POR EVENTOS MEDIADOS POR PROTEINAS CINASAS, PARTICULARMENTE PREVENIR EL CRECIMIENTO O INDUCIR LA APOPTOSIS DE TUMORES, EN ESPECIAL AL INHIBIR LA ANGIOGENESIS
PE2015002022A 2013-03-15 2014-03-14 Compuestos de heteroarilo y sus usos PE20151776A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361793113P 2013-03-15 2013-03-15
EP14305361 2014-03-13

Publications (1)

Publication Number Publication Date
PE20151776A1 true PE20151776A1 (es) 2015-12-11

Family

ID=50390019

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2015002022A PE20151776A1 (es) 2013-03-15 2014-03-14 Compuestos de heteroarilo y sus usos

Country Status (13)

Country Link
US (1) US9663524B2 (es)
EP (1) EP2968337B1 (es)
JP (1) JP6576325B2 (es)
KR (1) KR102219695B1 (es)
CN (2) CN111793068A (es)
AU (1) AU2014228746B2 (es)
BR (1) BR112015022191A8 (es)
EA (1) EA036160B1 (es)
MA (1) MA38393B1 (es)
MX (1) MX2015011514A (es)
PE (1) PE20151776A1 (es)
SG (1) SG11201507478VA (es)
WO (1) WO2014144737A1 (es)

Families Citing this family (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
GB201204384D0 (en) 2012-03-13 2012-04-25 Univ Dundee Anti-flammatory agents
PT3176170T (pt) 2012-06-13 2019-02-05 Incyte Holdings Corp Compostos tricíclicos substituídos como inibidores de fgfr
ES2916220T3 (es) 2012-07-11 2022-06-29 Blueprint Medicines Corp Inhibidores del receptor de factor de crecimiento de fibroblasto
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
MX2015011514A (es) 2013-03-15 2016-08-11 Celgene Avilomics Res Inc Compuestos de heteroarilo y sus usos.
TWI647220B (zh) 2013-03-15 2019-01-11 美商西建卡爾有限責任公司 雜芳基化合物及其用途
CA2907243C (en) 2013-03-15 2021-12-28 Celgene Avilomics Research, Inc. Substituted dihydropyrimidopyrimidinone compounds and pharmaceutical compositions thereof use fgfr4 inhibitor
SG10201708520YA (en) 2013-04-19 2017-12-28 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
UA116920C2 (uk) 2013-10-18 2018-05-25 ЕЙСАЙ Ар ЕНД Ді МЕНЕДЖМЕНТ КО., ЛТД. Інгібітори fgfr4
ES2924111T3 (es) 2013-10-25 2022-10-04 Blueprint Medicines Corp Inhibidores del receptor del factor de crecimiento de fibroblastos
PE20160546A1 (es) 2013-10-25 2016-05-26 Novartis Ag Compuestos derivados de piridilo biciclicos fusionados a anillo como inhibidores de fgfr4
US9695165B2 (en) 2014-01-15 2017-07-04 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
AU2015292818B2 (en) 2014-07-21 2020-01-16 Dana-Farber Cancer Institute, Inc. Imidazolyl kinase inhibitors and uses thereof
CA2954187C (en) 2014-07-21 2022-08-16 Dana-Farber Cancer Institute, Inc. Macrocyclic kinase inhibitors and uses thereof
AU2015300782B2 (en) 2014-08-08 2020-04-16 Dana-Farber Cancer Institute, Inc. Uses of salt-inducible kinase (SIK) inhibitors
ES2756748T3 (es) 2014-10-03 2020-04-27 Novartis Ag Uso de derivados de piridilo bicíclicos de anillo fusionado como inhibidores de fgfr4
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
TWI712601B (zh) 2015-02-20 2020-12-11 美商英塞特公司 作為fgfr抑制劑之雙環雜環
KR20170129757A (ko) 2015-03-25 2017-11-27 노파르티스 아게 Fgfr4 억제제로서의 포르밀화 n-헤테로시클릭 유도체
US9802917B2 (en) 2015-03-25 2017-10-31 Novartis Ag Particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide
MX2017013248A (es) 2015-04-14 2018-07-06 Eisai R&D Man Co Ltd Compuesto del inhibidor fgfr4 cristalino y usos del mismo.
US11357769B2 (en) 2016-05-10 2022-06-14 Eisai R&D Management Co., Ltd. Drug combinations for reducing cell viability and/or cell proliferation
KR20180002053A (ko) * 2016-06-28 2018-01-05 한미약품 주식회사 신규한 헤테로시클릭 유도체 화합물 및 이의 용도
US10954242B2 (en) * 2016-07-05 2021-03-23 The Broad Institute, Inc. Bicyclic urea kinase inhibitors and uses thereof
US11241435B2 (en) 2016-09-16 2022-02-08 The General Hospital Corporation Uses of salt-inducible kinase (SIK) inhibitors for treating osteoporosis
WO2018055503A1 (en) 2016-09-20 2018-03-29 Novartis Ag Combination comprising a pd-1 antagonist and an fgfr4 inhibitor
EP3534902B1 (en) 2016-11-02 2022-11-23 Novartis AG Combinations of fgfr4 inhibitors and bile acid sequestrants
US10968220B2 (en) * 2016-12-19 2021-04-06 Abbisko Therapeutics Co., Ltd. FGFR4 inhibitor, preparation method therefor and pharmaceutical use thereof
AU2018226771B2 (en) 2017-02-28 2023-11-23 Dana-Farber Cancer Institute, Inc. Uses of pyrimidopyrimidinones as SIK inhibitors
CN108503593B (zh) * 2017-02-28 2021-04-27 暨南大学 2-氨基嘧啶类化合物及其应用
WO2018213219A1 (en) * 2017-05-15 2018-11-22 University Of Houston System Pyrido[2,3-d]pyrimidin-7ones and related compounds as inhibitors of protein kinases
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
WO2019015593A1 (zh) * 2017-07-19 2019-01-24 江苏奥赛康药业股份有限公司 嘧啶并吡啶酮或者吡啶并吡啶酮类化合物及其应用
CN109384790B (zh) * 2017-08-08 2022-05-10 药捷安康(南京)科技股份有限公司 成纤维细胞生长因子受体抑制剂及其用途
CN109745325B (zh) * 2017-11-08 2022-02-15 上海翰森生物医药科技有限公司 Fgfr4抑制剂、其制备方法和用途
CN110386921A (zh) * 2018-04-23 2019-10-29 南京药捷安康生物科技有限公司 成纤维细胞生长因子受体抑制剂化合物
MA52493A (fr) 2018-05-04 2021-03-10 Incyte Corp Sels d'un inhibiteur de fgfr
US11466004B2 (en) 2018-05-04 2022-10-11 Incyte Corporation Solid forms of an FGFR inhibitor and processes for preparing the same
WO2019223766A1 (zh) * 2018-05-25 2019-11-28 上海和誉生物医药科技有限公司 一种fgfr抑制剂、其制备方法和在药学上的应用
CN110577524B (zh) * 2018-06-07 2022-01-28 北京大学深圳研究生院 一种激酶选择性抑制剂
CN111936493B (zh) * 2018-06-19 2023-05-26 上海和誉生物医药科技有限公司 一种高选择性FGFRi抑制剂及其制备方法和应用
MX2020013757A (es) 2018-09-14 2021-03-02 Abbisko Therapeutics Co Ltd Inhibidor del fgfr, metodo de preparacion y aplicacion del mismo.
WO2020177067A1 (en) 2019-03-05 2020-09-10 Bioardis Llc Aromatic derivatives, preparation methods, and medical uses thereof
EP3936509A4 (en) * 2019-03-08 2022-03-30 Shouyao Holdings (Beijing) Co., Ltd. FGFR4 KINASE INHIBITOR, METHOD FOR PREPARATION AND USE
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CA3157361A1 (en) 2019-10-14 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
GB201915828D0 (en) * 2019-10-31 2019-12-18 Cancer Research Tech Ltd Compounds, compositions and therapeutic uses thereof
WO2021108803A1 (en) 2019-11-26 2021-06-03 Theravance Biopharma R&D Ip, Llc Fused pyrimidine pyridinone compounds as jak inhibitors
JP2023505258A (ja) 2019-12-04 2023-02-08 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての三環式複素環
BR112022010664A2 (pt) 2019-12-04 2022-08-16 Incyte Corp Derivados de um inibidor de fgfr
KR20230160375A (ko) * 2021-03-26 2023-11-23 항저우 아펠로아 메디슨 리서치 인스티튜트 씨오.,엘티디. 이중환 헤테로고리 fgfr4 억제제, 이를 포함한 약물 조성물 및 제제 또한 그의 적용
EP4352059A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
CN113527311B (zh) * 2021-08-23 2022-05-06 中南大学湘雅医院 Fgfr4抑制剂、组合物及其在药物制备中的用途
WO2023039828A1 (en) * 2021-09-17 2023-03-23 Nutshell Biotech (Shanghai) Co., Ltd. Fused ring compounds as inhibitors of fgfr4 tyrosine kinases
CN113912602B (zh) * 2021-10-14 2023-05-05 温州医科大学 一种2-氧代-1,2-二氢-1,6-萘啶-7-基类化合物及其制备方法和用途

Family Cites Families (102)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5516931A (en) 1982-02-01 1996-05-14 Northeastern University Release tag compounds producing ketone signal groups
US4650750A (en) 1982-02-01 1987-03-17 Giese Roger W Method of chemical analysis employing molecular release tag compounds
US4709016A (en) 1982-02-01 1987-11-24 Northeastern University Molecular analytical release tags and their use in chemical analysis
US5650270A (en) 1982-02-01 1997-07-22 Northeastern University Molecular analytical release tags and their use in chemical analysis
DK0790997T3 (da) * 1994-11-14 2000-08-21 Warner Lambert Co 6-Aryl-pyrido[2,3-d]pyrimidiner og napthyridiner til hæmning af protein-tyrosin-kinase-fremkaldt celleproliferation
GB9508535D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivative
ES2301194T3 (es) * 1997-02-05 2008-06-16 Warner-Lambert Company Llc Pirido 2,3-d pirimidinas y 4-aminopirimidinas como inhibidores de la proliferacion celular.
DE19802377A1 (de) 1998-01-22 1999-08-19 Max Planck Gesellschaft Verwendung von Inhibitoren für die Behandlung von RTK-Überfunktions-bedingten Störungen, insbesondere von Krebs
CN1138778C (zh) 1998-05-26 2004-02-18 沃尼尔·朗伯公司 用作细胞增殖抑制剂的二环嘧啶及二环3,4-二氢嘧啶化合物及用途
AU769989B2 (en) 1998-10-23 2004-02-12 F. Hoffmann-La Roche Ag Bicyclic nitrogen heterocycles
US7169778B2 (en) 1999-09-15 2007-01-30 Warner-Lambert Company Pteridinones as kinase inhibitors
DE60032623T2 (de) 1999-10-21 2007-10-11 F. Hoffmann-La Roche Ag Alkylamino-substituierte bicyclische heterocyclen als p38 protein-kinase-inhibitoren
IL149100A0 (en) 1999-10-21 2002-11-10 Hoffmann La Roche Heteroalkylamino-substituted bicyclic nitrogen heterocycles as inhibitors of p38 protein kinase
MY141144A (en) 2000-03-02 2010-03-15 Smithkline Beecham Corp 1, 5-disubstituted-3,4-dihydro-1h-pyrimido 4,5-dipyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
CA2417942C (en) 2000-08-04 2010-06-29 Warner-Lambert Company 2-(4-pyridyl)amino-6-dialkoxyphenyl-pyrido[2,3-d]pyrimidin-7-ones
WO2002018379A2 (en) 2000-08-31 2002-03-07 F. Hoffmann-La Roche Ag 7-oxo pyridopyrimidines
AU9378401A (en) 2000-08-31 2002-03-13 Hoffmann La Roche 7-oxo pyridopyrimidines as inhibitors of a cellular proliferation
US6506749B2 (en) 2000-08-31 2003-01-14 Syntex (U.S.A.) Llc 7-oxo-pyridopyrimidines (I)
US6518276B2 (en) 2000-08-31 2003-02-11 Syntex (U.S.A.) Llc 7-oxo-pyridopyrimidines (II)
WO2002076985A1 (en) * 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
US7365205B2 (en) 2001-06-20 2008-04-29 Daiichi Sankyo Company, Limited Diamine derivatives
PA8577501A1 (es) 2002-07-25 2004-02-07 Warner Lambert Co Inhibidores de quinasas
AU2003250475A1 (en) 2002-08-13 2004-02-25 Warner-Lambert Company Llc 5,6-fused 3,4-dihydropyrimidine-2-one derivatives as matrix metalloproteinase inhibitors
US7084270B2 (en) 2002-08-14 2006-08-01 Hoffman-La Roche Inc. Pyrimido compounds having antiproliferative activity
US7129351B2 (en) 2002-11-04 2006-10-31 Hoffmann-La Roche Inc. Pyrimido compounds having antiproliferative activity
TW200413381A (en) 2002-11-04 2004-08-01 Hoffmann La Roche Novel amino-substituted dihydropyrimido [4,5-d]pyrimidinone derivatives, their manufacture and use as pharmaceutical agents
AU2003297431A1 (en) 2002-12-20 2004-07-22 Pharmacia Corporation Mitogen activated protein kinase-activated protein kinase-2 inhibiting compounds
US7098332B2 (en) * 2002-12-20 2006-08-29 Hoffmann-La Roche Inc. 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones
WO2004063195A1 (en) 2003-01-03 2004-07-29 Sloan-Kettering Institute For Cancer Research Pyridopyrimidine kinase inhibitors
KR100864393B1 (ko) 2003-04-10 2008-10-20 에프. 호프만-라 로슈 아게 피리미도 화합물
JP2006523638A (ja) 2003-04-16 2006-10-19 エフ．ホフマン−ラ　ロシュ　アーゲー キナゾリン化合物
BRPI0413005A (pt) 2003-07-29 2006-09-26 Irm Llc compostos e composições como inibidores da proteìna cinase
AU2004279427B2 (en) 2003-10-08 2008-07-03 Irm Llc Compounds and compositions as protein kinase inhibitors
AU2004312376A1 (en) 2003-12-19 2005-07-21 Five Prime Therapeutics, Inc. Fibroblast growth factor receptors 1, 2, 3, and 4 as targets for therapeutic intervention
EP2260849A1 (en) 2004-01-21 2010-12-15 Emory University Compositions and methods of use for tyrosine kinase inhibitors to treat pathogenic infection
WO2005105097A2 (en) 2004-04-28 2005-11-10 Gpc Biotech Ag Pyridopyrimidines for treating inflammatory and other diseases
GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds
US7655651B2 (en) 2004-08-31 2010-02-02 Hoffmann-La Roche Inc. Amide derivatives of 3-phenyl-dihydropyrimido[4,5-d]pyrimidinones, their manufacture and use as pharmaceutical agents
EP1789399A1 (en) 2004-08-31 2007-05-30 AstraZeneca AB Quinazolinone derivatives and their use as b-raf inhibitors
JP2008509964A (ja) 2004-08-31 2008-04-03 エフ．ホフマン−ラ ロシュ アーゲー ７−アミノ−３−フェニル−ジヒドロピリミド［４，５−ｄ］ピリミジノンのアミド誘導体、これらの製造、及びプロテインキナーゼ阻害剤としての使用
WO2006038112A1 (en) 2004-10-01 2006-04-13 Warner-Lambert Company Llc Use of kinase inhibitors to promote neochondrogenesis
US20070054916A1 (en) * 2004-10-01 2007-03-08 Amgen Inc. Aryl nitrogen-containing bicyclic compounds and methods of use
AU2005316668B2 (en) 2004-12-13 2012-09-06 Millennium Pharmaceuticals, Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as RAF kinase inhibitors
US20060142312A1 (en) * 2004-12-23 2006-06-29 Pfizer Inc C6-aryl and heteroaryl substituted pyrido[2,3-D] pyrimidin-7-ones
JP5079500B2 (ja) 2005-04-28 2012-11-21 協和発酵キリン株式会社 ２−アミノキナゾリン誘導体
RU2007147917A (ru) 2005-06-10 2009-07-20 Айрм Ллк (Bm) Соединения, поддерживающие плюрипотентность эмбриональных стволовых клеток
WO2006137421A1 (ja) 2005-06-21 2006-12-28 Kyowa Hakko Kogyo Co., Ltd. 局所投与剤
DE602006010874D1 (de) 2005-07-22 2010-01-14 Five Prime Therapeutics Inc Zusammensetzungen und verfahren zur behandlung von krankheiten mit fgfr-fusionsproteinen
AU2006272609A1 (en) 2005-07-26 2007-02-01 Vertex Pharmaceuticals Incorporated Abl kinase inhibition
KR100832594B1 (ko) 2005-11-08 2008-05-27 한미약품 주식회사 다중저해제로서의 퀴나졸린 유도체 및 이의 제조방법
US7618982B2 (en) 2005-12-19 2009-11-17 Nerviano Medical Sciences S.R.L. Heteroarylpyrrolopyridinones active as kinase inhibitors
BRPI0620408B8 (pt) 2005-12-21 2021-05-25 Novartis Ag derivados de pirimidinil aril uréia sendo inibidores de fgf, seus usos, e preparação farmacêutica
BRPI0620151A2 (pt) 2005-12-22 2010-06-29 Wyeth Corp composto; composição farmacêutica; método de tratar ou inibir o crescimento de células tumorais cancerosas em um mamìfero que deste necessita; método; e processo
ATE499374T1 (de) 2006-05-11 2011-03-15 Irm Llc Verbindungen und zusammensetzungen als proteinkinase-hemmer
WO2007136465A2 (en) 2006-05-15 2007-11-29 Irm Llc Compositions and methods for fgf receptor kinases inhibitors
EP1914234A1 (en) 2006-10-16 2008-04-23 GPC Biotech Inc. Pyrido[2,3-d]pyrimidines and their use as kinase inhibitors
JP2010506902A (ja) 2006-10-16 2010-03-04 ジーピーシー・バイオテック・インコーポレーテッド ピリド［２，３−ｄ］ピリミジン類およびキナーゼ阻害剤としてのそれらの使用
WO2008150260A1 (en) 2007-06-06 2008-12-11 Gpc Biotech, Inc. 8-oxy-2-aminopyrido (2, 3-d) pyrimidin-7-one derivatives as kinase inhibitors and anticancer agents
US8129659B2 (en) 2006-10-20 2012-03-06 Swagelok Company Apparatus having DC arc start in parallel with welder power supply
CA2668731A1 (en) 2006-11-09 2008-05-15 Tobias Gabriel Kinase inhibitors and methods for using the same
US7737149B2 (en) 2006-12-21 2010-06-15 Astrazeneca Ab N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]-4-(3,5-dimethylpiperazin-1-yl)benzamide and salts thereof
CA2672172C (en) 2006-12-22 2016-05-03 Astex Therapeutics Limited Bicyclic heterocyclic compounds as fgfr inhibitors
RS51655B (en) * 2006-12-27 2011-10-31 Sanofi-Aventis Isoquinoline derivatives and isoquinolinone derivatives substituted by cycloalkylamine
DE602007013295D1 (de) 2006-12-27 2011-04-28 Sanofi Aventis Substituierte isochinoline und ihre verwendung als rho-kinase-inhibitoren
SI2168966T1 (sl) 2007-06-15 2017-03-31 Msd K.K. Derivat biciklo anilina
GB0720038D0 (en) 2007-10-12 2007-11-21 Astex Therapeutics Ltd New compounds
US7989465B2 (en) * 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
US8216783B2 (en) 2008-04-14 2012-07-10 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Over-expression and mutation of a tyrosine kinase receptor FGFR4 in tumors
EP2112150B1 (en) 2008-04-22 2013-10-16 Forma Therapeutics, Inc. Improved raf inhibitors
EP2269993B1 (en) 2008-04-23 2013-02-27 Kyowa Hakko Kirin Co., Ltd. 2-aminoquinazoline derivative
EP2282995B1 (en) * 2008-05-23 2015-08-26 Novartis AG Derivatives of quinolines and quinoxalines as protein tyrosine kinase inhibitors
US20100121052A1 (en) 2008-06-20 2010-05-13 Rama Jain Novel compounds for treating proliferative diseases
EP3549934A1 (en) 2008-06-27 2019-10-09 Celgene CAR LLC Heteroaryl compounds and uses thereof
RU2014150660A (ru) * 2008-09-05 2015-07-20 Селджен Авиломикс Рисерч, Инк. Алгоритм разработки необратимо действующих ингибиторов
WO2010067886A1 (en) 2008-12-12 2010-06-17 Banyu Pharmaceutical Co.,Ltd. Dihydropyrimidopyrimidine derivative
EP2376494A4 (en) 2008-12-12 2012-07-11 Msd Kk DIHYDROPYRIMIDOPIRYMIDINE DERIVATIVES
WO2010080712A2 (en) 2009-01-06 2010-07-15 Dana Farber Cancer Institute Pyrimido-diazepinone kinase scaffold compounds and methods of treating disorders
NZ620174A (en) * 2009-09-16 2016-08-26 Celgene Avilomics Res Inc Protein kinase conjugates and inhibitors
UA109888C2 (uk) 2009-12-07 2015-10-26 ІЗОЛЬОВАНЕ АНТИТІЛО АБО ЙОГО ФРАГМЕНТ, ЩО ЗВ'ЯЗУЄТЬСЯ З β-КЛОТО, РЕЦЕПТОРАМИ FGF І ЇХНІМИ КОМПЛЕКСАМИ
AR079257A1 (es) 2009-12-07 2012-01-04 Novartis Ag Formas cristalinas de 3-(2,6-dicloro-3-5-dimetoxi-fenil)-1-{6-[4-(4-etil-piperazin-1-il)-fenil-amino]-pirimidin-4-il}-1-metil-urea y sales de las mismas
WO2011075620A1 (en) 2009-12-18 2011-06-23 Novartis Ag Method for treating haematological cancers
GB201007286D0 (en) * 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
CN103501610A (zh) * 2011-03-09 2014-01-08 西建阿维拉米斯研究公司 Pi3激酶抑制剂和其用途
JP2014516511A (ja) * 2011-04-07 2014-07-17 ジェネンテック， インコーポレイテッド 抗ｆｇｆｒ４抗体及び使用方法
PL2710007T3 (pl) 2011-05-17 2020-06-01 The Regents Of The University Of California Inhibitory kinazy
CN102887895B (zh) 2011-07-22 2016-08-24 山东轩竹医药科技有限公司 吡啶并嘧啶类mTOR抑制剂
CN104093717A (zh) 2011-11-04 2014-10-08 阿弗拉克西斯控股股份有限公司 用于治疗细胞增殖性障碍的pak抑制剂
US8461179B1 (en) 2012-06-07 2013-06-11 Deciphera Pharmaceuticals, Llc Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
CN104902895B (zh) 2012-06-07 2019-03-29 德西费拉制药有限责任公司 可用作用于治疗增生性疾病的激酶抑制剂的二氢萘啶和相关化合物
ES2916220T3 (es) * 2012-07-11 2022-06-29 Blueprint Medicines Corp Inhibidores del receptor de factor de crecimiento de fibroblasto
TWI629266B (zh) 2012-12-28 2018-07-11 藍印藥品公司 纖維母細胞生長因子受體之抑制劑
MX2015011514A (es) 2013-03-15 2016-08-11 Celgene Avilomics Res Inc Compuestos de heteroarilo y sus usos.
TWI647220B (zh) 2013-03-15 2019-01-11 美商西建卡爾有限責任公司 雜芳基化合物及其用途
EP2970231A1 (en) 2013-03-15 2016-01-20 Blueprint Medicines Corporation Piperazine derivatives and their use as kit modulators
CA2917667A1 (en) 2013-07-09 2015-01-15 Dana-Farber Cancer Institute, Inc. Kinase inhibitors for the treatment of disease
EP3027654B1 (en) 2013-07-30 2019-09-25 Blueprint Medicines Corporation Pik3c2g fusions
WO2015017533A1 (en) 2013-07-30 2015-02-05 Blueprint Medicines Corporation Ntrk2 fusions
DK3057969T3 (en) 2013-10-17 2018-09-24 Blueprint Medicines Corp COMPOSITIONS USED FOR TREATMENT OF DISEASES RELATED TO ENZYMETE KIT
WO2015058129A1 (en) 2013-10-17 2015-04-23 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
UA116920C2 (uk) 2013-10-18 2018-05-25 ЕЙСАЙ Ар ЕНД Ді МЕНЕДЖМЕНТ КО., ЛТД. Інгібітори fgfr4
ES2924111T3 (es) 2013-10-25 2022-10-04 Blueprint Medicines Corp Inhibidores del receptor del factor de crecimiento de fibroblastos
US9695165B2 (en) 2014-01-15 2017-07-04 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor

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