[go: up one dir, main page]

SMT201500191B - Derivati di benzopirazina sostituiti come inibitori delle chinasi fgfr per il trattamento di malattie tumorali - Google Patents

Derivati di benzopirazina sostituiti come inibitori delle chinasi fgfr per il trattamento di malattie tumorali

Info

Publication number
SMT201500191B
SMT201500191B SM201500191T SM201500191T SMT201500191B SM T201500191 B SMT201500191 B SM T201500191B SM 201500191 T SM201500191 T SM 201500191T SM 201500191 T SM201500191 T SM 201500191T SM T201500191 B SMT201500191 B SM T201500191B
Authority
SM
San Marino
Prior art keywords
benzopyrazine
treatment
kinase inhibitors
tumor diseases
derivatives substituted
Prior art date
Application number
SM201500191T
Other languages
English (en)
Inventor
Valerio Berdini
Gordon Saxty
Christopher William Murray
Gilbert Ebai Besong
Christopher Charles Frederick Hamlett
Steven John Woodhead
Yannick Aime Eddy Ligny
Patrick Rene Angibaud
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
Publication of SMT201500191B publication Critical patent/SMT201500191B/it

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/502Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
SM201500191T 2010-11-29 2015-08-06 Derivati di benzopirazina sostituiti come inibitori delle chinasi fgfr per il trattamento di malattie tumorali SMT201500191B (it)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US41774410P 2010-11-29 2010-11-29
GBGB1020179.6A GB201020179D0 (en) 2010-11-29 2010-11-29 New compounds
PCT/GB2011/052356 WO2012073017A1 (en) 2010-11-29 2011-11-29 Substituted benzopyrazin derivatives as fgfr kinase inhibitors for the treatment of cancer diseases

Publications (1)

Publication Number Publication Date
SMT201500191B true SMT201500191B (it) 2015-09-07

Family

ID=43500774

Family Applications (1)

Application Number Title Priority Date Filing Date
SM201500191T SMT201500191B (it) 2010-11-29 2015-08-06 Derivati di benzopirazina sostituiti come inibitori delle chinasi fgfr per il trattamento di malattie tumorali

Country Status (18)

Country Link
US (2) US9290478B2 (it)
EP (1) EP2646432B1 (it)
JP (1) JP5868992B2 (it)
KR (1) KR101914720B1 (it)
CN (1) CN103370314B (it)
AU (1) AU2011334624B2 (it)
BR (1) BR112013013435B1 (it)
CA (1) CA2819009C (it)
DK (1) DK2646432T3 (it)
ES (1) ES2541493T3 (it)
GB (1) GB201020179D0 (it)
HR (1) HRP20150692T8 (it)
HU (1) HUE025091T2 (it)
MX (1) MX2013005897A (it)
RU (1) RU2602233C2 (it)
SI (1) SI2646432T1 (it)
SM (1) SMT201500191B (it)
WO (1) WO2012073017A1 (it)

Families Citing this family (67)

* 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
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
CN107245056A (zh) 2011-08-26 2017-10-13 润新生物公司 化学实体、组合物及方法
US9518029B2 (en) 2011-09-14 2016-12-13 Neupharma, Inc. Certain chemical entities, compositions, and methods
EP2757885B1 (en) 2011-09-21 2017-03-15 Neupharma, Inc. Certain chemical entites, compositions, and methods
WO2013049701A1 (en) 2011-09-30 2013-04-04 Neupharma, Inc. Certain chemical entities, compositions, and methods
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
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
US9670180B2 (en) 2012-01-25 2017-06-06 Neupharma, Inc. Certain chemical entities, compositions, and methods
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209613D0 (en) * 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
CN107652289B (zh) 2012-06-13 2020-07-21 因塞特控股公司 作为fgfr抑制剂的取代的三环化合物
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
WO2014044846A1 (en) 2012-09-24 2014-03-27 Evotec (Uk) Ltd. 3-(aryl- or heteroaryl-amino)-7-(3,5-dimethoxyphenyl)isoquinoline derivatives as fgfr inhibitors useful for the treatment of proliferative disorders or dysplasia
WO2014047648A1 (en) 2012-09-24 2014-03-27 Neupharma, Inc. Certain chemical entities, compositions, and methods
WO2014075077A1 (en) 2012-11-12 2014-05-15 Neupharma, Inc. Certain chemical entities, compositions, and methods
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
AR094812A1 (es) 2013-02-20 2015-08-26 Eisai R&D Man Co Ltd Derivado de piridina monocíclico como inhibidor del fgfr
KR102269032B1 (ko) 2013-04-19 2021-06-24 인사이트 홀딩스 코포레이션 Fgfr 저해제로서 이환식 헤테로사이클
GB201307577D0 (en) * 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
EP2924038A1 (en) 2014-03-24 2015-09-30 Evotec (UK) Ltd. Preparation of pyrrolo[2,3-b]pyrazine and pyrrolo[2,3-b]pyridine derivatives as FGFR inhibitors
RU2715236C2 (ru) 2014-03-26 2020-02-26 Астекс Терапьютикс Лтд Комбинации
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
HUE053653T2 (hu) 2014-03-26 2021-07-28 Astex Therapeutics Ltd FGFR inhibitor és IGF1R inhibitor kombinációi
ES2914072T3 (es) 2014-08-18 2022-06-07 Eisai R&D Man Co Ltd Sal de derivado de piridina monocíclico y su cristal
WO2016048833A2 (en) 2014-09-26 2016-03-31 Janssen Pharmaceutica Nv Use of fgfr mutant gene panels in identifying cancer patients that will be responsive to treatment with an fgfr inhibitor
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
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
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
PE20171514A1 (es) 2015-02-20 2017-10-20 Incyte Corp Heterociclos biciclicos como inhibidores de fgfr
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
JP6503450B2 (ja) 2015-03-25 2019-04-17 国立研究開発法人国立がん研究センター 胆管癌治療剤
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer
JP2018524010A (ja) * 2015-07-24 2018-08-30 デバイオファーム インターナショナル エスエイ Fgfr発現とfgfr阻害剤に対する感受性
ES2904513T3 (es) * 2015-09-23 2022-04-05 Janssen Pharmaceutica Nv 1,4-Benzodiazepinas biheteroarilo sustituidas y usos de las mismas para el tratamiento del cáncer
EP3353177B1 (en) 2015-09-23 2020-06-03 Janssen Pharmaceutica NV Tricyclic heterocycles for the treatment of cancer
MX382526B (es) 2015-10-23 2025-03-13 Array Biopharma Inc Compuestos de 2-piridazin-3(2h)-ona 2-aril sustituidas y 2-heteroaril sustituidas como inhibidores de las tirosina quinasas fgfr
MX384034B (es) 2015-12-17 2025-03-14 Eisai R&D Man Co Ltd Agente terapeutico para cancer de mama.
WO2018071348A1 (en) * 2016-10-10 2018-04-19 Development Center For Biotechnology Quinoxaline compounds as type iii receptor tyrosine kinase inhibitors
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
BR112020017922A2 (pt) 2018-03-28 2020-12-22 Eisai R&D Management Co., Ltd. Agente terapêutico para carcinoma hepatocelular
SG11202010636VA (en) 2018-05-04 2020-11-27 Incyte Corp Solid forms of an fgfr inhibitor and processes for preparing the same
BR112020022373A2 (pt) 2018-05-04 2021-02-02 Incyte Corporation sais de um inibidor de fgfr
CA3103335C (en) * 2018-09-14 2023-10-03 Abbisko Therapeutics Co., Ltd. Fgfr inhibitor, preparation method therefor and application thereof
JP2022515198A (ja) 2018-12-19 2022-02-17 アレイ バイオファーマ インコーポレイテッド FGFRチロシンキナーゼの阻害剤としての置換ピラゾロ[1,5-a]ピリジン化合物
US12351571B2 (en) 2018-12-19 2025-07-08 Array Biopharma Inc. Substituted quinoxaline compounds as inhibitors of FGFR tyrosine kinases
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
JP7198387B2 (ja) * 2019-08-08 2022-12-28 ▲ザン▼州片仔▲ファン▼薬業股▲フン▼有限公司 ピラジン-2(1h)-オン系化合物のc結晶形とe結晶形及びその製造方法
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076602A1 (en) 2019-10-14 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CN115151539A (zh) 2019-12-04 2022-10-04 因赛特公司 Fgfr抑制剂的衍生物
JP7720840B2 (ja) 2019-12-04 2025-08-08 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
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3205986A1 (en) 2020-12-30 2022-07-07 Tyra Biosciences, Inc. Indazole compounds as kinase inhibitors
CA3211124A1 (en) 2021-02-26 2022-09-01 Tyra Biosciences, Inc. Aminopyrimidine compounds and methods of their use
US12065494B2 (en) 2021-04-12 2024-08-20 Incyte Corporation Combination therapy comprising an FGFR inhibitor and a Nectin-4 targeting agent
CA3220155A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
AR126102A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
EP4547670A1 (en) 2022-06-29 2025-05-07 Tyra Biosciences, Inc. Polymorphic compounds and uses thereof
CN119731165A (zh) 2022-06-29 2025-03-28 泰拉生物科学公司 吲唑化合物
WO2024138112A1 (en) 2022-12-22 2024-06-27 Tyra Biosciences, Inc. Indazole compounds
TW202535368A (zh) 2023-12-15 2025-09-16 美商泰拉生物科學公司 吲唑化合物

Family Cites Families (108)

* 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
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
EP0951541B1 (en) 1995-07-31 2005-11-30 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
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.
UA71555C2 (en) 1997-10-06 2004-12-15 Zentaris Gmbh Methods for modulating function of serine/threonine protein kinases by 5-azaquinoline derivatives
EP1147094A1 (en) 1999-01-15 2001-10-24 Novo Nordisk A/S Non-peptide glp-1 agonists
CN1373763A (zh) 1999-09-15 2002-10-09 沃尼尔·朗伯公司 作为激酶抑制剂的蝶啶酮
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
DE60223720T2 (de) 2001-12-18 2008-10-30 Merck & Co., Inc. Heteroaryl-substituierte pyrazol-modulatoren des metabotropen glutamatrezeptors-5
RU2323215C2 (ru) 2001-12-24 2008-04-27 Астразенека Аб Замещенные производные хиназолина как ингибиторы ауроракиназы
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
US20040097725A1 (en) 2002-07-10 2004-05-20 Norman Herron 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
BR0315053A (pt) 2002-10-03 2005-08-09 Targegen Inc Agentes vasculostáticos , composição, artigo e processo de preparação dos mesmos
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
DE602004021558D1 (de) 2003-01-17 2009-07-30 Warner Lambert Co 2-aminopyridin-substituierteheterocyclen als inhibitoren der zellulären proliferation
WO2004098494A2 (en) 2003-04-30 2004-11-18 Cytokinetics, Inc. Compounds, compositions, and methods
MXPA05012281A (es) 2003-05-14 2006-05-19 Torreypines Therapeutics Inc Compuestos y uso de los mismos en la modulacion beta amiloide.
AU2004240747B2 (en) 2003-05-23 2008-01-03 Zentaris Gmbh Novel pyridopyrazines and use thereof as kinase modulators
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
DK1673092T3 (da) 2003-10-17 2007-12-17 4 Aza Ip Nv Heterocyklylsubstituerede pteridinderivater og anvendelsen deraf i terapi
EP1682529A4 (en) 2003-11-07 2010-06-30 Novartis Vaccines & Diagnostic PROCESS FOR SYNTHESIS OF CHINOLINONE COMPOUNDS
AU2004295058B9 (en) 2003-11-20 2011-06-30 Janssen Pharmaceutica N.V. 6-alkenyl and 6-phenylalkyl substituted 2-quinolinones and 2-quinoxalinones as poly(ADP-ribose) polymerase inhibitors
WO2005054231A1 (en) 2003-11-24 2005-06-16 F.Hoffmann-La Roche Ag Pyrazolyl and imidazolyl pyrimidines
US8247576B2 (en) 2003-12-23 2012-08-21 Astex Therapeutics Limited Pyrazole derivatives as protein kinase modulators
US7098222B2 (en) 2004-05-12 2006-08-29 Abbott Laboratories Bicyclic-substituted amines having cyclic-substituted monocyclic substituents
US7205316B2 (en) 2004-05-12 2007-04-17 Abbott Laboratories Tri- and bi-cyclic heteroaryl histamine-3 receptor ligands
US20090118261A1 (en) 2004-08-31 2009-05-07 Astrazeneca Ab Quinazolinone derivatives and their use as b-raf inhibitors
CA2583192A1 (en) 2004-10-14 2006-04-20 F. Hoffmann-La Roche Ag 1,5-naphthyridine azolidinones having cdk1 antiproliferative activity
CN102049048B (zh) 2004-12-24 2013-12-25 西芬克斯医药有限公司 治疗或预防的方法
CA2597447C (en) * 2005-02-14 2014-03-25 Bionomics Limited Novel tubulin polymerisation inhibitors
US9271963B2 (en) 2005-03-03 2016-03-01 Universitat Des Saarlandes Selective inhibitors of human corticosteroid synthases
US20090156617A1 (en) * 2005-05-12 2009-06-18 Northrup Alan B Tyrosine kinase inhibitors
MX2007014258A (es) 2005-05-18 2008-01-22 Wyeth Corp Inhibidores de 4,6-diamino-[1,7]naftiridin-3-carbonitrilo de la tpl2 cinasa y metodos de fabricacion y uso de los mismos.
GB0513692D0 (en) 2005-07-04 2005-08-10 Karobio Ab Novel pharmaceutical compositions
JP5527972B2 (ja) 2005-11-11 2014-06-25 エテルナ ツェンタリス ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規のピリドピラジン及び前記ピリドピラジンをキナーゼのモジュレーターとして用いる使用
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
JP2009535393A (ja) 2006-05-01 2009-10-01 ファイザー・プロダクツ・インク 置換2−アミノ縮合複素環式化合物
GB0609621D0 (en) 2006-05-16 2006-06-21 Astrazeneca Ab Novel co-crystal
ATE549338T1 (de) 2006-05-24 2012-03-15 Boehringer Ingelheim Int Substituierte pteridine, die mit einem viergliedrigen heterocyclus substituiert sind
CA2657702A1 (en) 2006-07-03 2008-01-10 Vereniging Voor Christelijk Hoger Onderwijs Wetenschappelijk Onderzoek E N Patieentenzorg Quinazolines and related heterocyclic comp0unds, and their therapeutic use
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
WO2008076278A2 (en) 2006-12-13 2008-06-26 Schering Corporation Methods of cancer treatment with igf1r inhibitors
US7872018B2 (en) * 2006-12-21 2011-01-18 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
MX2009006706A (es) * 2006-12-22 2009-07-02 Astex Therapeutics Ltd Compuestos heterociclicos biciclicos como inhibidores del receptor del factor de crecimiento de fibroblastos.
US20100216767A1 (en) 2006-12-22 2010-08-26 Mina Aikawa 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
US20100179143A1 (en) 2007-05-29 2010-07-15 Smithkline Beecham Corporation 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
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
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
US8309718B2 (en) 2007-11-16 2012-11-13 Incyte Corporation 4-pyrazolyl-N-arylpyrimidin-2-amines and 4-pyrazolyl-N-heteroarylpyrimidin-2-amines as janus kinase inhibitors
WO2009137378A2 (en) 2008-05-05 2009-11-12 Schering Corporation 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
JP2012509342A (ja) 2008-11-20 2012-04-19 オーエスアイ・フアーマスーテイカルズ・インコーポレーテツド 置換ピロロ[2,3−b]−ピリジンおよび−ピラジン
CA2750047A1 (en) 2009-01-21 2010-07-29 Basilea Pharmaceutica Ag Novel bicyclic antibiotics
JP2012516847A (ja) 2009-02-02 2012-07-26 メルク・シャープ・エンド・ドーム・コーポレイション Akt活性の阻害剤
TW201041888A (en) * 2009-05-06 2010-12-01 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
MX353776B (es) 2009-06-12 2018-01-29 Abivax Compuestos utiles para tratar cancer.
ES2534226T3 (es) 2009-09-03 2015-04-20 Bioenergenix Compuestos heterocíclicos para la inhibición de PASK
US9340528B2 (en) 2009-09-04 2016-05-17 Bayer Pharma Aktiengesellschaft Substituted aminoquinoxalines as tyrosine threonine kinase inhibitors
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
WO2011149937A1 (en) 2010-05-24 2011-12-01 Intellikine, Inc. Heterocyclic compounds and uses thereof
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
AU2012213080B2 (en) 2011-01-31 2014-03-27 Novartis Ag Novel heterocyclic derivatives
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
CN107245056A (zh) 2011-08-26 2017-10-13 润新生物公司 化学实体、组合物及方法
US9518029B2 (en) 2011-09-14 2016-12-13 Neupharma, Inc. Certain chemical entities, compositions, and methods
EP2757885B1 (en) 2011-09-21 2017-03-15 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
PH12014500912A1 (en) 2011-10-28 2014-06-09 Novartis Ag Novel purine derivatives and their use in the treatment of disease
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
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
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
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
RU2715236C2 (ru) 2014-03-26 2020-02-26 Астекс Терапьютикс Лтд Комбинации
HUE053653T2 (hu) 2014-03-26 2021-07-28 Astex Therapeutics Ltd FGFR inhibitor és IGF1R inhibitor kombinációi
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

Also Published As

Publication number Publication date
ES2541493T3 (es) 2015-07-21
AU2011334624A1 (en) 2013-06-13
BR112013013435A2 (pt) 2016-10-11
HRP20150692T1 (hr) 2015-08-14
DK2646432T3 (en) 2015-07-13
EP2646432A1 (en) 2013-10-09
WO2012073017A1 (en) 2012-06-07
US9290478B2 (en) 2016-03-22
CA2819009C (en) 2020-02-25
GB201020179D0 (en) 2011-01-12
KR20130132509A (ko) 2013-12-04
RU2602233C2 (ru) 2016-11-10
AU2011334624B2 (en) 2016-09-15
RU2013129820A (ru) 2015-01-10
EP2646432B1 (en) 2015-04-08
US20130267525A1 (en) 2013-10-10
KR101914720B1 (ko) 2018-11-05
JP5868992B2 (ja) 2016-02-24
HK1187916A1 (en) 2014-04-17
CN103370314B (zh) 2015-10-21
CA2819009A1 (en) 2012-06-07
US9856236B2 (en) 2018-01-02
MX2013005897A (es) 2013-10-25
JP2013543883A (ja) 2013-12-09
CN103370314A (zh) 2013-10-23
HUE025091T2 (en) 2016-01-28
US20160031856A1 (en) 2016-02-04
BR112013013435B1 (pt) 2020-10-20
HRP20150692T8 (en) 2015-09-25
SI2646432T1 (sl) 2015-08-31

Similar Documents

Publication Publication Date Title
SMT201500191B (it) Derivati di benzopirazina sostituiti come inibitori delle chinasi fgfr per il trattamento di malattie tumorali
HUS2200017I1 (hu) Dihidronaftiridinek és rokon vegyületek, amelyek hasznosak kináz inhibitorokként proliferatív betegségek kezelésére
IL291000A (en) Benzimidazole derivatives as erbb tyrosine kinase inhibitors for cancer therapy
PT3418281T (pt) Pirazolo[1,5-a]pirimidinas úteis como inibidores da quinase atr para o tratamento de doenças de cancro
SMT201600220B (it) Derivati di eterociclile biciclici come inibitori di fgfr chinasi per uso terapeutico
HUE037154T2 (hu) Szubsztituált benzilindazol-származékok mint Bub1 kinázgátlók hiperproliferatív megbetegedések kezelésére
PL2927213T3 (pl) Pochodne piperydynonu jako inhibitory MDM2 do leczenia nowotworu
SMT201500195B (it) Derivati di chinolina e chinossalina quali inibitori delle chinasi
SMT201600108B (it) Derivato di pirazochinolina come inibitori di pde9
IL232128B (en) Tor kinase inhibitors for cancer treatment
UA111075C2 (uk) Триазолопіридинові сполуки як інгібітори кінази рім
BR112013008527A2 (pt) derivados de pirazolo-quinazolina substituídos como inibidores de cinase
IL234639B (en) Treatment of cancer with tor kinase inhibitors
EP2782579A4 (en) PYRAZINKINASEINHIBITOREN
EP2930167A4 (en) TINOSOLINE INHIBITOR USED AS COMPLETE INDOLKETONE DERIVATIVE
HRP20150752T1 (xx) Piridinil- i pirazinilmetoksiarilni derivati, korisni kao inhibitori slezenske tirozinske kinaze
SMT201600395B (it) Derivati di pantotenato per il trattamento di disturbi neurologici
IL238592B (en) Compounds for treatment of liver diseases
EP2817286A4 (en) KINASEHEMMER FOR THE TREATMENT OF CANCER
IT1400964B1 (it) Procedimento per la preparazione di derivati pteridinici
IL234686A0 (en) Methods of treating cancer using aurora kinase inhibitors
SMT201600268B (it) Composizione per il trattamento delle neuropatie
IL231448A0 (en) Phosphatidylinositol 3-kinase inhibitors for cancer treatment
AU2012901199A0 (en) Kinase inhibitors for the Treatment of Cancer