DK2776397T3 - QUINOLINES AS FGFR CHINA MODULATORS - Google Patents

QUINOLINES AS FGFR CHINA MODULATORS Download PDF

Info

Publication number
DK2776397T3
DK2776397T3 DK12794744.8T DK12794744T DK2776397T3 DK 2776397 T3 DK2776397 T3 DK 2776397T3 DK 12794744 T DK12794744 T DK 12794744T DK 2776397 T3 DK2776397 T3 DK 2776397T3
Authority
DK
Denmark
Prior art keywords
alkyl
substituted
cancer
formula
galkyl
Prior art date
Application number
DK12794744.8T
Other languages
Danish (da)
English (en)
Inventor
Valerio Berdini
Patrick Rene Angibaud
Steven John Woodhead
Gordon Saxty
Original Assignee
Astex Therapeutics Ltd
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 Astex Therapeutics Ltd filed Critical Astex Therapeutics Ltd
Application granted granted Critical
Publication of DK2776397T3 publication Critical patent/DK2776397T3/en

Links

Classifications

    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/38—Nitrogen atoms
    • 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
    • C07D401/02—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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
DK12794744.8T 2011-10-28 2012-10-26 QUINOLINES AS FGFR CHINA MODULATORS DK2776397T3 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161552880P 2011-10-28 2011-10-28
GBGB1118652.5A GB201118652D0 (en) 2011-10-28 2011-10-28 New compounds
PCT/GB2012/052666 WO2013061074A1 (en) 2011-10-28 2012-10-26 Quinolines as fgfr kinase modulators

Publications (1)

Publication Number Publication Date
DK2776397T3 true DK2776397T3 (en) 2018-02-26

Family

ID=45373580

Family Applications (1)

Application Number Title Priority Date Filing Date
DK12794744.8T DK2776397T3 (en) 2011-10-28 2012-10-26 QUINOLINES AS FGFR CHINA MODULATORS

Country Status (16)

Country Link
US (2) US9439896B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
EP (1) EP2776397B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
JP (1) JP6067725B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
KR (1) KR102072869B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CN (1) CN104011025B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
AU (1) AU2012328164B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
BR (1) BR112014010177B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CA (1) CA2853366C (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
DK (1) DK2776397T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
ES (1) ES2661003T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
GB (1) GB201118652D0 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
HU (1) HUE037458T2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
IN (1) IN2014MN00988A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
MX (1) MX353806B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
RU (1) RU2625303C2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
WO (1) WO2013061074A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
GB201020179D0 (en) 2010-11-29 2011-01-12 Astex Therapeutics Ltd New compounds
GB201118654D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118652D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118675D0 (en) 2011-10-28 2011-12-14 Astex Therapeutics Ltd New compounds
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
CA2888210C (en) 2012-10-16 2021-02-09 Janssen Pharmaceutica Nv Methylene linked quinolinyl modulators of ror-gamma-t
AU2013331493A1 (en) 2012-10-16 2015-04-09 Janssen Pharmaceutica Nv Heteroaryl linked quinolinyl modulators of RORyt
ES2628365T3 (es) 2012-10-16 2017-08-02 Janssen Pharmaceutica N.V. Moduladores de quinolinilo unidos a fenilo de ROR-GAMA-T
AR094812A1 (es) 2013-02-20 2015-08-26 Eisai R&D Man Co Ltd Derivado de piridina monocíclico como inhibidor del fgfr
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
EP3057949B1 (en) * 2013-10-15 2019-06-05 Janssen Pharmaceutica NV Secondary alcohol quinolinyl modulators of ror gamma t
US10555941B2 (en) 2013-10-15 2020-02-11 Janssen Pharmaceutica Nv Alkyl linked quinolinyl modulators of RORγt
US9328095B2 (en) 2013-10-15 2016-05-03 Janssen Pharmaceutica Nv Heteroaryl linked quinolinyl modulators of RORgammat
US9221804B2 (en) 2013-10-15 2015-12-29 Janssen Pharmaceutica Nv Secondary alcohol quinolinyl modulators of RORγt
US9346782B2 (en) * 2013-10-15 2016-05-24 Janssen Pharmaceutica Nv Alkyl linked quinolinyl modulators of RORγt
CA2927182A1 (en) * 2013-10-15 2015-04-23 Janssen Pharmaceutica Nv Quinolinyl modulators of ror.gamma.t
US9284308B2 (en) 2013-10-15 2016-03-15 Janssen Pharmaceutica Nv Methylene linked quinolinyl modulators of RORγt
US9403816B2 (en) 2013-10-15 2016-08-02 Janssen Pharmaceutica Nv Phenyl linked quinolinyl modulators of RORγt
BR112016022062B1 (pt) 2014-03-26 2023-04-11 Astex Therapeutics Limited Combinação, composição farmacêutica, uso de uma combinação ou de uma composição farmacêutica, e, produto farmacêutico
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
WO2015144804A1 (en) 2014-03-26 2015-10-01 Astex Therapeutics Ltd Combinations
MX369646B (es) 2014-08-18 2019-11-15 Eisai R&D Man Co Ltd Sal de derivado de piridina monociclico y su cristal.
JOP20200201A1 (ar) 2015-02-10 2017-06-16 Astex Therapeutics Ltd تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين
CN114984013A (zh) 2015-03-25 2022-09-02 国立癌症研究中心 胆管癌治疗剂
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer
BR112018005625B1 (pt) * 2015-09-23 2023-11-14 Janssen Pharmaceutica N.V Compostos derivados de quinolina, piridopirazina, naftiridina e quinazolinona, composições farmacêuticas que os compreende e uso dos mesmos
BR112018005637B1 (pt) 2015-09-23 2023-11-28 Janssen Pharmaceutica Nv Compostos derivados de quinoxalina, quinolina e quinazolinona,composições farmacêuticas que os compreende, e uso dos referidos compostos
CN108264510A (zh) * 2017-01-02 2018-07-10 上海喆邺生物科技有限公司 一种选择性抑制激酶化合物及其用途
KR20200135945A (ko) 2018-03-28 2020-12-04 에자이 알앤드디 매니지먼트 가부시키가이샤 간세포 암종 치료제
CN113087696A (zh) * 2019-12-23 2021-07-09 江苏开元药业有限公司 喹啉类化合物及其应用
WO2021146163A1 (en) * 2020-01-17 2021-07-22 Beta Pharma, Inc. Pyridazine and 1,2,4-triazine derivatives as fgfr kinase inhibitors

Family Cites Families (118)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2940972A (en) 1957-06-27 1960-06-14 Thomae Gmbh Dr K Tri-and tetra-substituted pteridine derivatives
US4666828A (en) 1984-08-15 1987-05-19 The General Hospital Corporation Test for Huntington's disease
US4683202A (en) 1985-03-28 1987-07-28 Cetus Corporation Process for amplifying nucleic acid sequences
US4801531A (en) 1985-04-17 1989-01-31 Biotechnology Research Partners, Ltd. Apo AI/CIII genomic polymorphisms predictive of atherosclerosis
US5272057A (en) 1988-10-14 1993-12-21 Georgetown University Method of detecting a predisposition to cancer by the use of restriction fragment length polymorphism of the gene for human poly (ADP-ribose) polymerase
US5192659A (en) 1989-08-25 1993-03-09 Genetype Ag Intron sequence analysis method for detection of adjacent and remote locus alleles as haplotypes
GB9125001D0 (en) 1991-11-25 1992-01-22 Ici Plc Heterocyclic compounds
EP0763537A3 (en) 1993-05-14 1997-10-22 Genentech Inc Non-peptides farnesyl transfer inhibitors
US5700823A (en) 1994-01-07 1997-12-23 Sugen, Inc. Treatment of platelet derived growth factor related disorders such as cancers
US6331555B1 (en) 1995-06-01 2001-12-18 University Of California Treatment of platelet derived growth factor related disorders such as cancers
US6218529B1 (en) 1995-07-31 2001-04-17 Urocor, Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate, breast and bladder cancer
WO1998004689A1 (en) 1995-07-31 1998-02-05 Urocor, Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate disease
TW472045B (en) 1996-09-25 2002-01-11 Astra Ab Protein kinase C inhibitor compounds, method for their preparation, pharmaceutical composition thereof and intermediate used for their preparation
DE69842151D1 (de) 1997-05-28 2011-04-14 Aventis Pharma Inc CHINOLIN UND CHINOXALINVERBINDUNGEN DIE DEN VON BLUTPLÄTTCHEN ABSTAMMENDEN FAKTOR UND/ODER p56Ick-TYROSINKINASE HEMMEN
UA71555C2 (en) 1997-10-06 2004-12-15 Zentaris Gmbh Methods for modulating function of serine/threonine protein kinases by 5-azaquinoline derivatives
JP2002534512A (ja) 1999-01-15 2002-10-15 ノボ ノルディスク アクティーゼルスカブ 非ペプチドｇｌｐ−１アゴニスト
IL148614A0 (en) 1999-09-15 2002-09-12 Warner Lambert Co Pteridinones as kinase inhibitors
DE10013318A1 (de) 2000-03-17 2001-09-20 Merck Patent Gmbh Formulierung enthaltend Chinoxalinderivate
WO2002076985A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
US7569592B2 (en) 2001-12-18 2009-08-04 Merck & Co., Inc. Heteroaryl substituted pyrazole modulators of metabotropic glutamate receptor-5
ATE446093T1 (de) 2001-12-24 2009-11-15 Astrazeneca Ab Substituierte chinazolin-derivate als aurora- kinase inhibitoren
JP2003213463A (ja) 2002-01-17 2003-07-30 Sumitomo Chem Co Ltd 金属腐食防止剤および洗浄液
CA2480800C (en) 2002-04-08 2008-09-23 Mark T. Bilodeau Inhibitors of akt activity
US7265378B2 (en) 2002-07-10 2007-09-04 E. I. Du Pont De Nemours And Company Electronic devices made with electron transport and/or anti-quenching layers
US7825132B2 (en) * 2002-08-23 2010-11-02 Novartis Vaccines And Diagnostics, Inc. Inhibition of FGFR3 and treatment of multiple myeloma
CA2500727A1 (en) 2002-10-03 2004-04-15 Targegen, Inc. Vasculostatic agents and methods of use thereof
AR043059A1 (es) 2002-11-12 2005-07-13 Bayer Pharmaceuticals Corp Derivados de indolil pirazinona utiles para el tratamiento de trastornos hiper-proliferativos
US7098332B2 (en) 2002-12-20 2006-08-29 Hoffmann-La Roche Inc. 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones
CA2512646A1 (en) 2003-01-17 2004-08-05 Warner-Lambert Company Llc 2-aminopyridine substituted heterocycles as inhibitors of cellular proliferation
EP1620413A2 (en) 2003-04-30 2006-02-01 Cytokinetics, Inc. Compounds, compositions, and methods
US7244739B2 (en) 2003-05-14 2007-07-17 Torreypines Therapeutics, Inc. Compounds and uses thereof in modulating amyloid beta
RU2330851C9 (ru) 2003-05-23 2008-10-20 Центарис Гмбх ПИРИДО[2,3-b]ПИРАЗИНОВЫЕ ПРОИЗВОДНЫЕ, ЛЕКАРСТВЕННОЕ СРЕДСТВО ДЛЯ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЯ ИЛИ НАРУШЕНИЯ, КОТОРЫЕ ОБУСЛОВЛЕНЫ НЕПРАВИЛЬНО НАПРАВЛЕННЫМИ ПРОЦЕССАМИ КЛЕТОЧНОЙ СИГНАЛЬНОЙ ТРАНСДУКЦИИ, СПОСОБ ПОЛУЧЕНИЯ ЛЕКАРСТВЕННОГО СРЕДСТВА
DE10323345A1 (de) 2003-05-23 2004-12-16 Zentaris Gmbh Neue Pyridopyrazine und deren Verwendung als Kinase-Inhibitoren
WO2005007099A2 (en) 2003-07-10 2005-01-27 Imclone Systems Incorporated Pkb inhibitors as anti-tumor agents
CA2533417A1 (en) 2003-07-21 2005-02-03 Mitchell A. Avery Design and synthesis of optimized ligands for ppar
CN1829709A (zh) 2003-08-01 2006-09-06 健亚生物科技公司 对抗黄病毒的双环咪唑衍生物
WO2005039587A1 (en) 2003-10-17 2005-05-06 4 Aza Bioscience Nv Heterocycle-substituted pteridine derivatives and their use in therapy
US20050209247A1 (en) 2003-11-07 2005-09-22 Chiron Corporation Pharmaceutically acceptable salts of quinolinone compounds having improved pharmaceutical properties
EP1687277B1 (en) * 2003-11-20 2018-04-04 Janssen Pharmaceutica NV 6-alkenyl and 6-phenylalkyl substituted 2-quinolinones and 2-quinoxalinones as poly(adp-ribose) polymerase inhibitors
ES2670349T3 (es) * 2003-11-20 2018-05-30 Janssen Pharmaceutica Nv 2-Quinolinonas y 2-quinoxalinonas sustituidas con 6-alquenilo y 6-fenilalquilo como inhibidores de poli(ADP-ribosa) polimerasa
RU2377241C2 (ru) 2003-11-24 2009-12-27 Ф.Хоффманн-Ля Рош Аг Производные пиразоло-имидазопиримидина, обладающие антагонистической активностью в отношении кортикотропин-рилизинг фактора (crf)
PL1706385T3 (pl) 2003-12-23 2011-03-31 Astex Therapeutics Ltd Pochodne pirazolu jako modulatory kinazy białkowej
US7205316B2 (en) 2004-05-12 2007-04-17 Abbott Laboratories Tri- and bi-cyclic heteroaryl histamine-3 receptor ligands
US7098222B2 (en) 2004-05-12 2006-08-29 Abbott Laboratories Bicyclic-substituted amines having cyclic-substituted monocyclic substituents
MX2007002434A (es) 2004-08-31 2007-05-04 Astrazeneca Ab Derivados de quinazolinona y su uso como inhibidores de b-raf.
KR100875408B1 (ko) 2004-10-14 2008-12-23 에프. 호프만-라 로슈 아게 Ｃｄｋ1 항증식성 활성을 갖는 1,5-나프티리딘 아졸리디논
JP4966202B2 (ja) 2004-12-24 2012-07-04 スピニフェクス ファーマシューティカルズ ピーティーワイ リミテッド 治療または予防のための方法
CA2597447C (en) 2005-02-14 2014-03-25 Bionomics Limited Novel tubulin polymerisation inhibitors
EP1853261B1 (de) 2005-03-03 2017-01-11 Universität des Saarlandes Selektive hemmstoffe humaner corticoidsynthasen
JP2008540535A (ja) 2005-05-12 2008-11-20 メルク エンド カムパニー インコーポレーテッド チロシンキナーゼ阻害剤
BRPI0611521A2 (pt) 2005-05-18 2010-09-14 Wyeth Corp inibidores de 4,6-diamino-[1,7]naftiridina-3-carbonitrila de quìnase tpl2 e métodos de fabricação e uso dos mesmos
GB0513692D0 (en) 2005-07-04 2005-08-10 Karobio Ab Novel pharmaceutical compositions
ES2456000T3 (es) 2005-08-26 2014-04-21 Merck Serono Sa Derivados de pirazina y su uso como inhibidores de PI3K
EP1790342A1 (de) 2005-11-11 2007-05-30 Zentaris GmbH Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege
CA2628039A1 (en) 2005-11-11 2007-05-18 Aeterna Zentaris Gmbh Novel pyridopyrazines and their use as modulators of kinases
US8217042B2 (en) 2005-11-11 2012-07-10 Zentaris Gmbh Pyridopyrazines and their use as modulators of kinases
ME02736B (me) 2005-12-21 2017-10-20 Janssen Pharmaceutica Nv Triazolopiridazini kao modulatori tirozin kinaze
EP2024342A2 (en) 2006-05-01 2009-02-18 Pfizer Products Incorporated Substituted 2-amino-fused heterocyclic compounds
GB0609621D0 (en) 2006-05-16 2006-06-21 Astrazeneca Ab Novel co-crystal
EP2029600B1 (de) 2006-05-24 2012-03-14 Boehringer Ingelheim International GmbH Substituierte pteridine, die mit einem viergliedrigen heterocyclus substituiert sind
JP2009541460A (ja) 2006-07-03 2009-11-26 ベレナギング ヴォー クリスタラク ホガー オンダーヴェイル ヴェーテンザパーリク オンダージーク エン パシェンテンゾーク ヒスタミンｈ４受容体と相互作用する縮合二環式化合物
JP2008127446A (ja) 2006-11-20 2008-06-05 Canon Inc １，５−ナフチリジン化合物及び有機発光素子
EP2104501B1 (en) 2006-12-13 2014-03-12 Merck Sharp & Dohme Corp. Methods of cancer treatment with igf1r inhibitors
MX2009006688A (es) 2006-12-21 2009-06-30 Plexxikon Inc Compuestos y metodos para modulacion de cinasas, e indicaciones para ello.
KR20090092287A (ko) 2006-12-22 2009-08-31 노파르티스 아게 Ｐｄｋ１ 억제를 위한 퀴나졸린
HRP20150642T1 (hr) 2006-12-22 2015-08-14 Astex Therapeutics Limited BICIKLIÄŚKE HETEROCIKLIÄŚKE TVARI KAO INHIBITORI FGFR-a
KR20080062876A (ko) 2006-12-29 2008-07-03 주식회사 대웅제약 신규한 항진균성 트리아졸 유도체
EP1990342A1 (en) 2007-05-10 2008-11-12 AEterna Zentaris GmbH Pyridopyrazine Derivatives, Process of Manufacturing and Uses thereof
JP2010526823A (ja) 2007-05-10 2010-08-05 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Ｐｉ３キナーゼ阻害物質としてのキノキサリン誘導体
JP2010529031A (ja) 2007-05-29 2010-08-26 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Ｐｉ３キナーゼ阻害剤としてのナフチリジン誘導体
AR066879A1 (es) 2007-06-08 2009-09-16 Novartis Ag Derivados de quinoxalina como inhibidores de la actividad de cinasa de tirosina de las cinasas janus
KR101251933B1 (ko) 2007-06-20 2013-04-09 미쓰비시 타나베 파마 코퍼레이션 신규한 말론산술폰아미드 유도체 및 그 의약 용도
WO2008155378A1 (en) 2007-06-21 2008-12-24 Janssen Pharmaceutica Nv Polymorphic and hydrate forms, salts and process for preparing 6-{difluoro[6-(1-methyl-1h-pyrazol-4-yl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl}quinoline
WO2009019518A1 (en) 2007-08-09 2009-02-12 Astrazeneca Ab Pyrimidine compounds having a fgfr inhibitory effect
JP2010535804A (ja) 2007-08-09 2010-11-25 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Ｐｉ３キナーゼ阻害薬としてのキノキサリン誘導体
US20090054304A1 (en) 2007-08-23 2009-02-26 Kalypsys, Inc. Heterocyclic modulators of tgr5 for treatment of disease
EA020777B1 (ru) 2007-11-16 2015-01-30 Инсайт Корпорейшн 4-пиразолил-n-арилпиримидин-2-амины, 4-пиразолил-n-пиразолилпиримидин-2-амины и 4-пиразолил-n-пиридилпиримидин-2-амины в качестве ингибиторов киназ janus
CA2722992A1 (en) 2008-05-05 2009-11-12 Schering Corporation Sequential administration of chemotherapeutic agents for treatment of cancer
CA2725185C (en) * 2008-05-23 2016-10-25 Novartis Ag Derivatives of quinolines and quinoxalines as protein tyrosine kinase inhibitors
EP2356116A1 (en) 2008-11-20 2011-08-17 OSI Pharmaceuticals, Inc. Substituted pyrroloý2,3-b¨-pyridines and-pyrazines
JP5662346B2 (ja) 2009-01-21 2015-01-28 バジリア ファルマスーチカ アーゲーＢａｓｉｌｅａ Ｐｈａｒｍａｃｅｕｔｉｃａ ＡＧ 新規二環式抗生物質
CA2750051A1 (en) 2009-02-02 2010-08-05 Merck Sharp & Dohme Corp. Inhibitors of akt activity
TW201041888A (en) 2009-05-06 2010-12-01 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
ES2736198T3 (es) * 2009-06-12 2019-12-26 Abivax Compuestos útiles para tratar el cáncer
NZ598294A (en) 2009-09-03 2013-07-26 Bioenergenix Heterocyclic compounds for the inhibition of pask
WO2011026579A1 (en) 2009-09-04 2011-03-10 Bayer Schering Pharma Aktiengesellschaft Substituted aminoquinoxalines as tyrosine threonine kinase inhibitors
US20110123545A1 (en) 2009-11-24 2011-05-26 Bristol-Myers Squibb Company Combination of vegfr2 and igf1r inhibitors for the treatment of proliferative diseases
EP2332939A1 (en) 2009-11-26 2011-06-15 Æterna Zentaris GmbH Novel Naphthyridine derivatives and the use thereof as kinase inhibitors
SG10201502484SA (en) 2010-03-30 2015-05-28 Verseon Corp Multisubstituted aromatic compounds as inhibitors of thrombin
GB201007286D0 (en) * 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
WO2011146591A1 (en) 2010-05-19 2011-11-24 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof
US9096590B2 (en) 2010-05-24 2015-08-04 Intellikine Llc Substituted benzoxazoles as PI3 kinase inhibitors
GB201020179D0 (en) * 2010-11-29 2011-01-12 Astex Therapeutics Ltd New compounds
CN102532141A (zh) 2010-12-08 2012-07-04 中国科学院上海药物研究所 [1，2，4]三唑并[4，3-b][1，2，4]三嗪类化合物、其制备方法和用途
WO2012104776A1 (en) 2011-01-31 2012-08-09 Novartis Ag Novel heterocyclic derivatives
EP2678018A4 (en) 2011-02-23 2015-09-30 Intellikine Llc COMBINATION OF CHINESE HEMMER AND USES THEREOF
WO2012118492A1 (en) 2011-03-01 2012-09-07 Array Biopharma Inc. Heterocyclic sulfonamides as raf inhibitors
CN104053442B (zh) 2011-08-26 2017-06-23 润新生物公司 某些化学实体、组合物及方法
CN108794411B (zh) 2011-09-14 2022-06-07 润新生物公司 某些化学实体、组合物及方法
WO2013043935A1 (en) 2011-09-21 2013-03-28 Neupharma, Inc. Certain chemical entites, compositions, and methods
EP2763994A4 (en) 2011-10-04 2015-08-26 Gilead Calistoga Llc NEW QUINOXALINE INHIBITORS OF THE PI3K PATH
GB201118675D0 (en) 2011-10-28 2011-12-14 Astex Therapeutics Ltd New compounds
CN104039790B (zh) 2011-10-28 2016-04-13 诺华股份有限公司 嘌呤衍生物及它们在治疗疾病中的应用
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118652D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
JO3210B1 (ar) 2011-10-28 2018-03-08 Merck Sharp & Dohme مثبط منصهر لبروتين نقل الكوليسترليستير اوكسازوليدينون ثمائي الحلقة
GB201118654D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
AU2013228389A1 (en) 2012-03-08 2014-09-25 Astellas Pharma Inc. Novel FGFR3 fusion product
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
US20150203589A1 (en) 2012-07-24 2015-07-23 The Trustees Of Columbia University In The City Of New York Fusion proteins and methods thereof
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
US9221804B2 (en) * 2013-10-15 2015-12-29 Janssen Pharmaceutica Nv Secondary alcohol quinolinyl modulators of RORγt
WO2015144804A1 (en) 2014-03-26 2015-10-01 Astex Therapeutics Ltd Combinations
BR112016022062B1 (pt) 2014-03-26 2023-04-11 Astex Therapeutics Limited Combinação, composição farmacêutica, uso de uma combinação ou de uma composição farmacêutica, e, produto farmacêutico
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
JOP20200201A1 (ar) 2015-02-10 2017-06-16 Astex Therapeutics Ltd تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer

Also Published As

Publication number Publication date
US20170000781A1 (en) 2017-01-05
EP2776397A1 (en) 2014-09-17
RU2014121494A (ru) 2015-12-10
US20140296236A1 (en) 2014-10-02
AU2012328164B2 (en) 2017-08-03
RU2625303C2 (ru) 2017-07-13
CN104011025B (zh) 2017-04-05
MX2014004857A (es) 2014-08-26
EP2776397B1 (en) 2017-11-29
CN104011025A (zh) 2014-08-27
BR112014010177A2 (pt) 2017-04-25
KR20140093665A (ko) 2014-07-28
JP6067725B2 (ja) 2017-01-25
WO2013061074A1 (en) 2013-05-02
JP2014530896A (ja) 2014-11-20
AU2012328164A1 (en) 2014-05-15
US10039759B2 (en) 2018-08-07
MX353806B (es) 2018-01-30
CA2853366A1 (en) 2013-05-02
IN2014MN00988A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 2015-04-24
HUE037458T2 (hu) 2018-09-28
KR102072869B1 (ko) 2020-03-02
CA2853366C (en) 2021-04-20
US9439896B2 (en) 2016-09-13
BR112014010177B1 (pt) 2023-01-31
ES2661003T3 (es) 2018-03-27
GB201118652D0 (en) 2011-12-07

Similar Documents

Publication Publication Date Title
DK2776397T3 (en) QUINOLINES AS FGFR CHINA MODULATORS
US10272087B2 (en) Pteridines as FGFR inhibitors
AU2012328167B9 (en) New compounds
AU2012328171B2 (en) Anticancer benzopyrazines via the inhibition of FGFR kinases
US9737544B2 (en) Compounds
AU2011334624B2 (en) Substituted benzopyrazin derivatives as FGFR kinase inhibitors for the treatment of cancer diseases
AU2012328170B2 (en) Anticancer pyridopyrazines via the inhibition of FGFR kinases