JP6625551B2 - Ｆｇｆｒキナーゼ調節剤として有用なキノキサリン誘導体 - Google Patents

Ｆｇｆｒキナーゼ調節剤として有用なキノキサリン誘導体 Download PDF

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JP6625551B2
JP6625551B2 JP2016558669A JP2016558669A JP6625551B2 JP 6625551 B2 JP6625551 B2 JP 6625551B2 JP 2016558669 A JP2016558669 A JP 2016558669A JP 2016558669 A JP2016558669 A JP 2016558669A JP 6625551 B2 JP6625551 B2 JP 6625551B2
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cancer
compound
formula
alkyl
compounds
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Japanese (ja)
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JP2017511311A (ja
JP2017511311A5 (enExample
Inventor
ウィム、フェレメレン
スティーブン、アナ、ホスティン
フィリップ、アルベール、セリーヌ、キュイケン
ラッセル、マーク、ジョーンズ
ディエゴ、フェルナンド、ドメニコ、ブロッジーニ
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Astex Therapeutics Ltd
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Astex Therapeutics Ltd
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    • 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D403/14—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 three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2016558669A 2014-03-26 2015-03-26 Ｆｇｆｒキナーゼ調節剤として有用なキノキサリン誘導体 Active JP6625551B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14161820 2014-03-26
EP14161820.7 2014-03-26
PCT/EP2015/056507 WO2015144803A1 (en) 2014-03-26 2015-03-26 Quinoxaline derivatives useful as fgfr kinase modulators

Publications (3)

Publication Number Publication Date
JP2017511311A JP2017511311A (ja) 2017-04-20
JP2017511311A5 JP2017511311A5 (enExample) 2018-05-10
JP6625551B2 true JP6625551B2 (ja) 2019-12-25

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JP2016558669A Active JP6625551B2 (ja) 2014-03-26 2015-03-26 Ｆｇｆｒキナーゼ調節剤として有用なキノキサリン誘導体

Country Status (37)

Country Link
US (2) US9902714B2 (enExample)
EP (1) EP3122742B1 (enExample)
JP (1) JP6625551B2 (enExample)
KR (1) KR102469506B1 (enExample)
CN (1) CN106459010B (enExample)
AP (1) AP2016009536A0 (enExample)
AR (1) AR099854A1 (enExample)
AU (1) AU2015238300C1 (enExample)
BR (1) BR112016022060B1 (enExample)
CL (1) CL2016002382A1 (enExample)
CR (1) CR20160501A (enExample)
CY (1) CY1120969T1 (enExample)
DK (1) DK3122742T3 (enExample)
EA (1) EA032145B1 (enExample)
ES (1) ES2702450T3 (enExample)
HR (1) HRP20182073T1 (enExample)
HU (1) HUE041738T2 (enExample)
IL (1) IL247658B (enExample)
JO (1) JO3512B1 (enExample)
LT (1) LT3122742T (enExample)
MA (1) MA39783B1 (enExample)
MX (1) MX380829B (enExample)
MY (1) MY194074A (enExample)
NI (1) NI201600144A (enExample)
NZ (1) NZ724907A (enExample)
PH (1) PH12016501898B1 (enExample)
PL (1) PL3122742T3 (enExample)
PT (1) PT3122742T (enExample)
RS (1) RS58088B1 (enExample)
SG (1) SG11201607961QA (enExample)
SI (1) SI3122742T1 (enExample)
SM (1) SMT201800670T1 (enExample)
TR (1) TR201819138T4 (enExample)
TW (1) TWI686391B (enExample)
UA (1) UA117958C2 (enExample)
WO (1) WO2015144803A1 (enExample)
ZA (1) ZA201606942B (enExample)

Families Citing this family (43)

* 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
GB201118675D0 (en) 2011-10-28 2011-12-14 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
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
SI2861566T1 (sl) 2012-06-13 2017-03-31 F. Hoffmann-La Roche Ag Novi diazaspirocikloalkan in azaspirocikloalkan
PL2900669T3 (pl) 2012-09-25 2020-01-31 F. Hoffmann-La Roche Ag Pochodne heksahydropirolo[3,4-C]pirolu i związki pokrewne jako inhibitory autotaksyny (ATX) oraz inhibitory produkcji kwasu lizofosfatydowego (LPA) do leczenia np. chorób nerek
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
AU2014356583B2 (en) 2013-11-26 2019-02-28 F. Hoffmann-La Roche Ag New octahydro-cyclobuta (1,2-c;3,4-c')dipyrrol-2-yl
DK3102576T3 (da) 2014-02-03 2019-07-22 Vitae Pharmaceuticals Llc Dihydropyrrolopyridininhibitorer af ror-gamma
BR112016022056B1 (pt) 2014-03-26 2023-04-11 Astex Therapeutics Limited Combinação, composição farmacêutica, uso de uma combinação ou uma composição farmacêutica, e, produto farmacêutico
US10736900B2 (en) 2014-03-26 2020-08-11 Astex Therapeutics Ltd Combinations of an FGFR inhibitor and an IGF1R inhibitor
CR20160418A (es) 2014-03-26 2016-11-07 Hoffmann La Roche Nuevos compuestos biciclicos de 7 eslabones
MA50635A (fr) 2014-03-26 2020-08-12 Hoffmann La Roche Nouveaux composés bicycliques comme inhibiteurs de la production d'autotaxin (atx) et de l'acide lysophosphatidique
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
TWI719960B (zh) 2015-02-10 2021-03-01 英商阿斯迪克治療公司 新穎組成物
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer
MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
EP3331876B1 (en) 2015-08-05 2020-10-07 Vitae Pharmaceuticals, LLC Modulators of ror-gamma
EP3344619B1 (en) 2015-09-04 2020-10-28 H. Hoffnabb-La Roche Ag Phenoxymethyl derivatives
HUE050567T2 (hu) * 2015-09-23 2020-12-28 Janssen Pharmaceutica Nv Triciklusos heterociklusok rák kezelésére
WO2017050865A1 (en) * 2015-09-23 2017-03-30 Janssen Pharmaceutica Nv Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer
BR112018006080A2 (pt) 2015-09-24 2018-10-09 F. Hoffmann-La Roche Ag novos compostos bicíclicos como inibidores de dupla ação de atx/ca
MA42918A (fr) 2015-09-24 2018-08-01 Hoffmann La Roche Composés bicycliques utilisés en tant qu'inhibiteurs d'atx
WO2017050747A1 (en) 2015-09-24 2017-03-30 F. Hoffmann-La Roche Ag New bicyclic compounds as dual atx/ca inhibitors
AU2016328437A1 (en) 2015-09-24 2018-01-25 F. Hoffmann-La Roche Ag Bicyclic compounds as ATX inhibitors
EP3868750A1 (en) 2015-11-20 2021-08-25 Vitae Pharmaceuticals, LLC Modulators of ror-gamma
TWI757266B (zh) 2016-01-29 2022-03-11 美商維它藥物有限責任公司 ＲＯＲ－γ調節劑
EP3596060B1 (en) 2017-03-16 2023-09-20 F. Hoffmann-La Roche AG New bicyclic compounds as atx inhibitors
RU2019132254A (ru) 2017-03-16 2021-04-16 Ф. Хоффманн-Ля Рош Аг Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca
WO2019018975A1 (en) 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. INHIBITORS OF ROR GAMMA
CN115716826A (zh) 2017-07-24 2023-02-28 生命医药有限责任公司 RORγ的抑制剂
US12351571B2 (en) 2018-12-19 2025-07-08 Array Biopharma Inc. Substituted quinoxaline compounds as inhibitors of FGFR tyrosine kinases
WO2020131627A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
MX2021011926A (es) 2019-03-29 2021-11-03 Janssen Pharmaceutica Nv Inhibidores de fgfr tirosina cinasa para el tratamiento de carcinoma urotelial.
WO2020208592A1 (en) * 2019-04-12 2020-10-15 Dr. Reddy’S Laboratories Limited Process for preparation of erdafitinib, its purification and amorphous solid dispersion
CN117203202A (zh) * 2021-02-05 2023-12-08 黑钻治疗公司 喹喔啉衍生物及其用途
FI4288426T3 (fi) * 2021-02-05 2026-04-21 Black Diamond Therapeutics Inc Kinoksaliinijohdannaisia ja niiden käyttöjä

Family Cites Families (134)

* 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
GB1583753A (en) 1976-07-14 1981-02-04 Science Union & Cie Piperidine derivatives processes for their preparation and pharmaceutical compositions containing them
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
TW219935B (enExample) 1991-12-25 1994-02-01 Mitsubishi Chemicals Co Ltd
US5843941A (en) 1993-05-14 1998-12-01 Genentech, Inc. Ras farnesyl transferase 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
CA2744096C (en) 1996-07-31 2013-07-30 Laboratory Corporation Of America Holdings 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
ES2235331T3 (es) 1997-05-28 2005-07-01 Aventis Pharmaceuticals Inc Compuestos quinolina y quinoxalina que inhiben el factor de crecimiento derivado de plaquetas y/o tirosina quinasas p561ck.
US6235740B1 (en) 1997-08-25 2001-05-22 Bristol-Myers Squibb Co. Imidazoquinoxaline protein tyrosine kinase inhibitors
UA71555C2 (en) 1997-10-06 2004-12-15 Zentaris Gmbh Methods for modulating function of serine/threonine protein kinases by 5-azaquinoline derivatives
AU3033500A (en) 1999-01-15 2000-08-01 Agouron Pharmaceuticals, Inc. Non-peptide glp-1 agonists
DE60010448T2 (de) 1999-03-17 2005-04-07 Astrazeneca Ab Amid-derivate
JP2003509425A (ja) 1999-09-15 2003-03-11 ワーナー−ランバート・カンパニー キナーゼ阻害剤としてのプテリジノン
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
US20030114448A1 (en) 2001-05-31 2003-06-19 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
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
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
AU2002249275A1 (en) 2002-03-08 2003-09-22 Warner-Lambert Company Llc Oxo azabicyclic compounds
CA2480800C (en) 2002-04-08 2008-09-23 Mark T. Bilodeau Inhibitors of akt activity
US6962995B2 (en) 2002-07-10 2005-11-08 E. I. Du Pont De Nemours And Company Charge transport compositions and electronic devices made with such compositions
US7825132B2 (en) 2002-08-23 2010-11-02 Novartis Vaccines And Diagnostics, Inc. Inhibition of FGFR3 and treatment of multiple myeloma
MXPA05003477A (es) 2002-10-03 2005-07-22 Targegen Inc Agentes vasculo-estaticos y metodos de uso de los mismos.
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
EP1590341B1 (en) 2003-01-17 2009-06-17 Warner-Lambert Company LLC 2-aminopyridine substituted heterocycles as inhibitors of cellular proliferation
WO2004098494A2 (en) 2003-04-30 2004-11-18 Cytokinetics, Inc. Compounds, compositions, and methods
CN102584813B (zh) 2003-05-14 2016-07-06 Ngc药物公司 化合物及其在调节淀粉样蛋白β中的用途
WO2004104003A1 (de) 2003-05-23 2004-12-02 Zentaris Gmbh Neue pyridopyrazine und deren verwendung als modulatoren von kinasen
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
EP1646383A4 (en) 2003-07-21 2009-03-25 Bethesda Pharmaceuticals Inc DESIGN AND SYNTHESIS OF OPTIMIZED LIGANDS FOR PPAR
BRPI0413234A (pt) 2003-08-01 2006-10-03 Genelabs Tech Inc derivados de imidazola bicìclica contra flaviviridae
PT1673092E (pt) 2003-10-17 2007-11-23 4 Aza Ip Nv ''derivados de pteridina substituídos com heterociclos e sua utilização em terapia''
JP4823914B2 (ja) 2003-11-07 2011-11-24 ノバルティス バクシンズ アンド ダイアグノスティックス，インコーポレーテッド Ｆｇｆｒ３の阻害および多発性骨髄腫の治療
NZ546991A (en) 2003-11-20 2010-01-29 Janssen Pharmaceutica Nv 6-Alkenyl and 6-phenylalkyl substituted 2-quinolinones and 2-quinoxalinones as PARP inhibitors
BRPI0416853A (pt) 2003-11-24 2007-02-13 Hoffmann La Roche pirazolila e imidazolila pirimidinas
EP2228369A1 (en) 2003-12-23 2010-09-15 Astex Therapeutics Ltd. Pyrazole derivatives as protein kinase modulators
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
US20090118261A1 (en) 2004-08-31 2009-05-07 Astrazeneca Ab Quinazolinone derivatives and their use as b-raf inhibitors
KR20080075235A (ko) 2004-10-14 2008-08-14 에프. 호프만-라 로슈 아게 Ｃｄｋ1 항증식성 활성을 갖는 1,5-나프티리딘 아졸리디논
CA2583096A1 (en) 2004-10-15 2006-04-20 Astrazeneca Ab Quinoxalines as b raf inhibitors
NZ555334A (en) 2004-12-24 2010-05-28 Spinifex Pharm Pty Ltd Method of treatment or prophylaxis of a neuropathic condition using AT2 receptor antagonist
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
AU2006247833A1 (en) 2005-05-12 2006-11-23 Merck & Co., Inc. Tyrosine kinase inhibitors
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
ZA200801822B (en) 2005-08-26 2009-09-30 Serono Lab Pyrazine derivatives and use as p13k inhibitors
AU2006313701B2 (en) 2005-11-11 2012-05-31 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
EP1790342A1 (de) 2005-11-11 2007-05-30 Zentaris GmbH Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege
RS55630B1 (sr) 2005-12-21 2017-06-30 Janssen Pharmaceutica Nv Triazolopiridazini kao modulatori tirozin kinaze
WO2007125405A2 (en) 2006-05-01 2007-11-08 Pfizer Products Inc. Substituted 2-amino-fused heterocyclic compounds
GB0609621D0 (en) 2006-05-16 2006-06-21 Astrazeneca Ab Novel co-crystal
WO2007135027A1 (de) 2006-05-24 2007-11-29 Boehringer Ingelheim International Gmbh Substituierte pteridine, die mit einem viergliedrigen heterocyclus substituiert sind
TWI398252B (zh) 2006-05-26 2013-06-11 諾華公司 吡咯并嘧啶化合物及其用途
AU2007271187A1 (en) 2006-07-03 2008-01-10 Vereniging Voor Christelijk Hoger Onderwijs, Wetenschappelijk Onderzoek En Patientenzorg Fused bicyclic compounds interacting with the histamine H4 receptor
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
RU2009122670A (ru) 2006-12-21 2011-01-27 Плекссикон, Инк. (Us) Соединения и способы для модуляции киназ и показания к их применению
CN101679408B (zh) 2006-12-22 2016-04-27 Astex治疗学有限公司 作为fgfr抑制剂的双环杂环化合物
CA2673003A1 (en) 2006-12-22 2008-07-03 Novartis Ag Quinazolines for pdk1 inhibition
KR20080062876A (ko) 2006-12-29 2008-07-03 주식회사 대웅제약 신규한 항진균성 트리아졸 유도체
TW200902008A (en) 2007-05-10 2009-01-16 Smithkline Beecham Corp Quinoxaline derivatives as PI3 kinase inhibitors
EP1990342A1 (en) 2007-05-10 2008-11-12 AEterna Zentaris GmbH Pyridopyrazine Derivatives, Process of Manufacturing and Uses thereof
EP2154965A4 (en) 2007-05-29 2011-08-17 Glaxosmithkline Llc NAPHTHYRIDINE DERIVATIVES AS P13 KINASE INHIBITORS
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
ES2442003T3 (es) 2007-06-20 2014-02-07 Mitsubishi Tanabe Pharma Corporation Nuevo derivado de sulfonamida de ácido malónico y uso farmacéutico del mismo
EP2170894A1 (en) 2007-06-21 2010-04-07 Janssen Pharmaceutica N.V. 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
JP2010532758A (ja) 2007-07-06 2010-10-14 オーエスアイ・ファーマスーティカルズ・インコーポレーテッド 組み合わせ抗癌療法
EP2188292B1 (en) 2007-08-08 2013-05-29 GlaxoSmithKline Intellectual Property Development Limited 2- [ (2-{phenylamino}-1h-pyrrolo [2, 3-d]pyrimidin-4-yl) amino]benzamide derivatives as igf-1r inhibitors for the treatment of cancer
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
WO2009019518A1 (en) 2007-08-09 2009-02-12 Astrazeneca Ab Pyrimidine compounds having a fgfr inhibitory effect
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
US20110129456A1 (en) 2008-05-05 2011-06-02 Yaolin Wang Sequential Administration of Chemotherapeutic Agents for Treatment of Cancer
AU2009248774B2 (en) 2008-05-23 2012-05-31 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
US8716280B2 (en) 2009-01-21 2014-05-06 Basilea Pharmaceutica Ag Bicyclic antibiotics
WO2010088177A1 (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
CN102625804B (zh) 2009-06-12 2015-04-08 Abivax公司 用于治疗aids的化合物
DK2473504T3 (en) 2009-09-03 2015-03-16 Bioenergenix Heterocyclic Compounds for Inhibition of Passover
WO2011026579A1 (en) 2009-09-04 2011-03-10 Bayer Schering Pharma Aktiengesellschaft Substituted aminoquinoxalines as tyrosine threonine kinase inhibitors
WO2011047129A1 (en) 2009-10-15 2011-04-21 Southern Research Institute Treatment of neurodegenerative diseases, causation of memory enhancement, and assay for screening compounds for such
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
US8513421B2 (en) 2010-05-19 2013-08-20 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof
JP5894980B2 (ja) 2010-05-24 2016-03-30 インテリカイン， エルエルシー 複素環式化合物およびその使用
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
WO2012106556A2 (en) 2011-02-02 2012-08-09 Amgen Inc. Methods and compositons relating to inhibition of igf-1r
TWI592411B (zh) 2011-02-23 2017-07-21 英特爾立秦有限責任公司 激酶抑制劑之組合及其用途
WO2012118492A1 (en) 2011-03-01 2012-09-07 Array Biopharma Inc. Heterocyclic sulfonamides as raf inhibitors
JP2014519813A (ja) 2011-04-25 2014-08-21 オーエスアイ・ファーマシューティカルズ，エルエルシー 癌薬剤発見、診断、および治療におけるｅｍｔ遺伝子シグネチャーの使用
WO2012154760A1 (en) 2011-05-10 2012-11-15 Gilead Sciences, Inc. Fused heterocyclic compounds as sodium channel modulators
WO2013032951A1 (en) 2011-08-26 2013-03-07 Neupharma, Inc. Certain chemical entities, compositions, and methods
AU2012308238B2 (en) 2011-09-14 2017-05-25 Neupharma, Inc. Certain chemical entities, compositions, and methods
US9249110B2 (en) 2011-09-21 2016-02-02 Neupharma, Inc. Substituted quinoxalines as B-raf kinase inhibitors
EP2763994A4 (en) 2011-10-04 2015-08-26 Gilead Calistoga Llc NEW QUINOXALINE INHIBITORS OF THE PI3K PATH
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
JO3210B1 (ar) 2011-10-28 2018-03-08 Merck Sharp & Dohme مثبط منصهر لبروتين نقل الكوليسترليستير اوكسازوليدينون ثمائي الحلقة
GB201118652D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118654D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
SG11201401716XA (en) 2011-10-28 2014-05-29 Novartis Ag Novel purine derivatives and their use in the treatment of disease
KR20220017512A (ko) 2012-03-08 2022-02-11 아스테라스 세이야쿠 가부시키가이샤 신규 fgfr3 융합체
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
CA2898326C (en) 2013-01-18 2022-05-17 Foundation Medicine, Inc. Methods of treating cholangiocarcinoma
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
EP3027623A4 (en) 2013-08-02 2017-03-01 Ignyta, Inc. METHODS OF TREATING VARIOUS CANCERS USING AN AXL/cMET INHIBITOR ALONE OR IN COMBINATION WITH OTHER AGENTS
US9221804B2 (en) 2013-10-15 2015-12-29 Janssen Pharmaceutica Nv Secondary alcohol quinolinyl modulators of RORγt
US10736900B2 (en) 2014-03-26 2020-08-11 Astex Therapeutics Ltd Combinations of an FGFR inhibitor and an IGF1R inhibitor
BR112016022056B1 (pt) 2014-03-26 2023-04-11 Astex Therapeutics Limited Combinação, composição farmacêutica, uso de uma combinação ou uma composição farmacêutica, e, produto farmacêutico
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
TWI719960B (zh) 2015-02-10 2021-03-01 英商阿斯迪克治療公司 新穎組成物
SG11201706727XA (en) 2015-02-19 2017-09-28 Bioclin Therapeutics Inc Methods, compositions, and kits for treatment of cancer
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer

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