CY1117319T1 - Τρικυκλικα παραγωγα αμινης ως αναστολεις πρωτεϊνικης τυροσινης κινασης - Google Patents

Τρικυκλικα παραγωγα αμινης ως αναστολεις πρωτεϊνικης τυροσινης κινασης

Info

Publication number
CY1117319T1
CY1117319T1 CY20161100015T CY161100015T CY1117319T1 CY 1117319 T1 CY1117319 T1 CY 1117319T1 CY 20161100015 T CY20161100015 T CY 20161100015T CY 161100015 T CY161100015 T CY 161100015T CY 1117319 T1 CY1117319 T1 CY 1117319T1
Authority
CY
Cyprus
Prior art keywords
tysine
inspectors
amin
tricyclic
muscle
Prior art date
Application number
CY20161100015T
Other languages
English (en)
Inventor
Valerio Berdini
Gilbert Ebai Besong
Owen Callaghan
Maria Grazia Carr
Miles Stuart Congreve
Adrian Liam Gill
Charlotte Mary Griffiths-Jones
Andrew Madin
Christopher William Murray
Rajdeep Kaur Nijjar
Michael Alistair O'brien
Andrew Pike
Gordon Saxty
Richard David Taylor
Emma Vickerstaffe
Original Assignee
Astex Therapeutics Limited
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
Priority claimed from GB0625827A external-priority patent/GB0625827D0/en
Priority claimed from GB0719998A external-priority patent/GB0719998D0/en
Application filed by Astex Therapeutics Limited filed Critical Astex Therapeutics Limited
Publication of CY1117319T1 publication Critical patent/CY1117319T1/el

Links

Classifications

    • 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
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

Η εφεύρεση αναφέρεται σε νέες ενώσεις δικυκλικών ετεροκυκλυλικών παραγώγων του τύπου I, σε φαρμακευτικές συνθέσεις που περιλαμβάνουν τις εν λόγω ενώσεις και στη χρήση των εν λόγω ενώσεων στη θεραπεία ασθενειών, π.χ. του καρκίνου. Οι ενώσεις του τύπου I είναι αναστολείς των FGFR, VEGFR ή PDGFR.
CY20161100015T 2006-12-22 2016-01-11 Τρικυκλικα παραγωγα αμινης ως αναστολεις πρωτεϊνικης τυροσινης κινασης CY1117319T1 (el)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US87153806P 2006-12-22 2006-12-22
GB0625827A GB0625827D0 (en) 2006-12-22 2006-12-22 New compounds
US97958207P 2007-10-12 2007-10-12
GB0719998A GB0719998D0 (en) 2007-10-12 2007-10-12 New compounds
EP07848681.8A EP2121687B1 (en) 2006-12-22 2007-12-21 Tricyclic amine derivatives as protein tyrosine kinase inhibitors

Publications (1)

Publication Number Publication Date
CY1117319T1 true CY1117319T1 (el) 2017-04-26

Family

ID=39322759

Family Applications (1)

Application Number Title Priority Date Filing Date
CY20161100015T CY1117319T1 (el) 2006-12-22 2016-01-11 Τρικυκλικα παραγωγα αμινης ως αναστολεις πρωτεϊνικης τυροσινης κινασης

Country Status (12)

Country Link
US (1) US8513276B2 (el)
EP (1) EP2121687B1 (el)
JP (1) JP5442449B2 (el)
CN (1) CN101679409B (el)
AU (1) AU2007337895C1 (el)
CA (1) CA2672213C (el)
CY (1) CY1117319T1 (el)
HR (1) HRP20151398T1 (el)
MX (1) MX2009006704A (el)
NO (1) NO342865B1 (el)
PL (1) PL2121687T3 (el)
WO (1) WO2008078100A2 (el)

Families Citing this family (84)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0420722D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
AR059898A1 (es) 2006-03-15 2008-05-07 Janssen Pharmaceutica Nv Derivados de 3-ciano-piridona 1,4-disustituida y su uso como moduladores alostericos de los receptores mglur2
WO2008078091A1 (en) * 2006-12-22 2008-07-03 Astex Therapeutics Limited Bicyclic heterocyclic compounds as fgfr inhibitors
CA2672213C (en) 2006-12-22 2016-02-16 Astex Therapeutics Limited Bicyclic amine derivatives as protein tyrosine kinase inhibitors
TW200900065A (en) 2007-03-07 2009-01-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives
TW200845978A (en) 2007-03-07 2008-12-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
TW200922566A (en) 2007-09-14 2009-06-01 Ortho Mcneil Janssen Pharm 1,3 disubstituted 4-(aryl-X-phenyl)-1H-pyridin-2-ones
ES2356032T3 (es) 2007-09-14 2011-04-04 Ortho-Mcneil-Janssen Pharmaceuticals, Inc. 4-fenil-3,4,5,6-tetrahidro-2h,1'h-[1,4']bipiridinil-2'-onas 1,3'-disustituidas.
EA016969B1 (ru) 2007-09-14 2012-08-30 Аддекс Фарма С.А. 1,3-двузамещенные-4-фенил-1н-пиридин-2-оны
GB0720038D0 (en) 2007-10-12 2007-11-21 Astex Therapeutics Ltd New compounds
GB0720041D0 (en) 2007-10-12 2007-11-21 Astex Therapeutics Ltd New Compounds
US8785486B2 (en) 2007-11-14 2014-07-22 Janssen Pharmaceuticals, Inc. Imidazo[1,2-A]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors
WO2009085913A1 (en) * 2007-12-19 2009-07-09 Vertex Pharmaceuticals Incorporated PYRAZOLO [1,5-a] PYRIMIDINES USEFUL AS JAK2 INHIBITORS
GB0810902D0 (en) 2008-06-13 2008-07-23 Astex Therapeutics Ltd New compounds
WO2010017046A1 (en) 2008-08-05 2010-02-11 Merck & Co., Inc. Pyrazolo[1,5-a]pyridines as mark inhibitors
US8455477B2 (en) * 2008-08-05 2013-06-04 Merck Sharp & Dohme Corp. Therapeutic compounds
MX2011002042A (es) 2008-09-02 2011-06-20 Ortho Mcneil Janssen Pharm Derivados de 3-azabiciclo[3.1.o]hexilo como moduladores de los receptores del glutamato metabotropico.
MX2011003691A (es) 2008-10-16 2011-09-06 Ortho Mcneil Janssen Pharm Derivados de indol y benzomorfolina como moduladores de los receptores de glutamato metabotropico.
EP2373649B1 (en) * 2008-11-28 2013-01-23 Janssen Pharmaceuticals, Inc. Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors
GB0906472D0 (en) 2009-04-15 2009-05-20 Astex Therapeutics Ltd New compounds
GB0906470D0 (en) 2009-04-15 2009-05-20 Astex Therapeutics Ltd New compounds
MX2011011964A (es) 2009-05-12 2012-02-23 Janssen Pharmaceuticals Inc Derivados de 1,2,3-triazolo[4,3-a]piridina y su uso para el tratamiento o prevencion de trastornos neurologicos y psiquiatricos.
MY153913A (en) 2009-05-12 2015-04-15 Janssen Pharmaceuticals Inc 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
NZ596053A (en) 2009-05-12 2013-05-31 Janssen Pharmaceuticals Inc 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
US8486940B2 (en) 2009-09-11 2013-07-16 Probiodrug Ag Inhibitors
FR2950344B1 (fr) * 2009-09-18 2011-11-25 Sanofi Aventis Derives de 5-phenyl-pyrazolopyridine, leur preparation et leur aplication en therapeutique.
FR2950345B1 (fr) * 2009-09-18 2011-09-23 Sanofi Aventis Derives acetyleniques de 5-phenyl-pyrazolopyridine, leur preparation et leur application en therapeutique
EP2496574A1 (en) * 2009-11-02 2012-09-12 Abbott Laboratories Imidazopyridines as a novel scaffold for multi-targeted kinase inhibition
FR2953520B1 (fr) * 2009-12-04 2011-11-25 Sanofi Aventis Derives de diphenyl-pyrazolopyridines, leur preparation et leur application en therapeutique
EP2338888A1 (en) * 2009-12-24 2011-06-29 Almirall, S.A. Imidazopyridine derivatives as JAK inhibitors
UY33213A (es) * 2010-02-18 2011-09-30 Almirall Sa Derivados de pirazol como inhibidores de jak
EP2360158A1 (en) * 2010-02-18 2011-08-24 Almirall, S.A. Pyrazole derivatives as jak inhibitors
RU2012136643A (ru) * 2010-04-28 2014-06-10 Дайити Санкио Компани, Лимитед [5,6]- гетероциклическое соединение
WO2012058529A2 (en) * 2010-10-28 2012-05-03 Viamet Pharmaceuticals, Inc. Metalloenzyme inhibitor compounds
JP5852666B2 (ja) 2010-11-08 2016-02-03 ジヤンセン・フアーマシユーチカルズ・インコーポレーテツド １，２，４−トリアゾロ［４，３−ａ］ピリジン誘導体およびｍＧｌｕＲ２受容体のポジティブアロステリックモジュレーターとしてのそれらの使用
EP2649069B1 (en) 2010-11-08 2015-08-26 Janssen Pharmaceuticals, Inc. 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
US9012448B2 (en) 2010-11-08 2015-04-21 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of MGLUR2 receptors
EP2463289A1 (en) 2010-11-26 2012-06-13 Almirall, S.A. Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors
KR101974665B1 (ko) * 2010-12-13 2019-05-02 어레이 바이오파마 인크. 제ＩＩＩ형 수용체 티로신 키나제 억제제로서의 치환된 Ｎ-（１Ｈ-인다졸-４-일)이미다조［１,２-ａ］피리딘-３-카복스아마이드 화합물
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
EP2554544A1 (en) 2011-08-01 2013-02-06 Almirall, S.A. Pyridin-2(1h)-one derivatives as jak inhibitors
US8883819B2 (en) 2011-09-01 2014-11-11 Irm Llc Bicyclic heterocycle derivatives for the treatment of pulmonary arterial hypertension
UA111382C2 (uk) 2011-10-10 2016-04-25 Оріон Корпорейшн Інгібітори протеїнкінази
EA036592B1 (ru) 2012-06-13 2020-11-26 Инсайт Холдингс Корпорейшн Замещенные трициклические соединения как ингибиторы fgfr
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
AU2013324396B2 (en) 2012-09-28 2018-10-04 Vanderbilt University Fused heterocyclic compounds as selective BMP inhibitors
CN102898426B (zh) * 2012-11-15 2015-04-22 江苏先声药业有限公司 抑制igf-1r酪氨酸激酶活性的吡啶并吡唑类衍生物
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
TWI628176B (zh) * 2013-04-04 2018-07-01 奧利安公司 蛋白質激酶抑制劑
WO2014172644A2 (en) 2013-04-19 2014-10-23 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US9822418B2 (en) 2013-04-22 2017-11-21 Icahn School Of Medicine At Mount Sinai Mutations in PDGFRB and NOTCH3 as causes of autosomal dominant infantile myofibromatosis
JO3368B1 (ar) 2013-06-04 2019-03-13 Janssen Pharmaceutica Nv مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2
JO3367B1 (ar) 2013-09-06 2019-03-13 Janssen Pharmaceutica Nv مركبات 2،1، 4- ثلاثي زولو [3،4-a] بيريدين واستخدامها بصفة منظمات تفارغية موجبة لمستقبلات ميجلور 2
PE20160886A1 (es) 2013-12-06 2016-09-14 Genentech Inc Inhibidores de serina/treonina cinasa
KR102414246B1 (ko) 2014-01-21 2022-06-27 얀센 파마슈티카 엔.브이. 대사 조절형 글루탐산 작동성 수용체 제2아형의 양성 알로스테릭 조절제 또는 오르토스테릭 작동제를 포함하는 조합 및 그 용도
LT3431106T (lt) 2014-01-21 2021-02-10 Janssen Pharmaceutica Nv Deriniai, apimantys 2 potipio metabotropinio glutamaterginio receptoriaus teigiamus alosterinius moduliatorius arba ortosterinius agonistus, ir jų panaudojimas
WO2016011019A1 (en) * 2014-07-15 2016-01-21 The Brigham And Women's Hospital, Inc. Compositions and methods for inhibiting bmp
CA2956270C (en) 2014-08-18 2022-08-09 Eisai R&D Management Co., Ltd. Salt of monocyclic pyridine derivative and crystal thereof
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
WO2016134294A1 (en) 2015-02-20 2016-08-25 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
ES2895769T3 (es) 2015-02-20 2022-02-22 Incyte Corp Heterociclos bicíclicos como inhibidores de FGFR
JP2020511424A (ja) * 2017-01-18 2020-04-16 ヴァンダービルト ユニバーシティーＶａｎｄｅｒｂｉｌｔ Ｕｎｉｖｅｒｓｉｔｙ 選択的ｂｍｐ阻害としての縮合複素環式化合物
US10870637B2 (en) * 2017-03-23 2020-12-22 Orion Corporation Process for the preparation of a sulfonamide structured kinase inhibitor
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
KR102639231B1 (ko) 2017-10-30 2024-02-22 뉴로포레 테라피스, 인코포레이티드 치환된 페닐 설폰일 페닐 트리아졸 싸이온 및 이의 용도
CA3089769A1 (en) 2018-01-29 2019-08-01 Merck Patent Gmbh Gcn2 inhibitors and uses thereof
TWI816742B (zh) 2018-01-29 2023-10-01 美商維泰克斯製藥公司 Gcn2抑制劑及其用途
EP3765460A1 (en) 2018-03-14 2021-01-20 Vanderbilt University Inhibition of bmp signaling, compounds, compositions and uses thereof
JPWO2019189241A1 (ja) 2018-03-28 2021-03-18 エーザイ・アール・アンド・ディー・マネジメント株式会社 肝細胞癌治療剤
US11174257B2 (en) 2018-05-04 2021-11-16 Incyte Corporation Salts of an FGFR inhibitor
CA3099287A1 (en) 2018-05-04 2019-11-07 Incyte Corporation Solid forms of an fgfr inhibitor and processes for preparing the same
WO2020135878A1 (zh) * 2018-12-29 2020-07-02 南京明德新药研发有限公司 作为fgfr和vegfr双重抑制剂的咪唑并吡啶衍生物
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
EP3985005A4 (en) * 2019-06-14 2023-07-19 CGeneTech (Suzhou, China) Co., Ltd. FUSED RING COMPOUND AS DUAL FGFR AND VEGFR INHIBITOR
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
KR20220052939A (ko) * 2019-07-26 2022-04-28 메드샤인 디스커버리 아이엔씨. Fgfr 및 vegfr 이중 억제제로서의 피리딘 유도체
CR20220169A (es) 2019-10-14 2022-10-27 Incyte Corp Heterociclos bicíclicos como inhibidores de fgfr
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
BR112022010664A2 (pt) 2019-12-04 2022-08-16 Incyte Corp Derivados de um inibidor de fgfr
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2021146424A1 (en) * 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
EP4352059A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors

Family Cites Families (104)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4503050A (en) 1983-06-02 1985-03-05 Riker Laboratories, Inc. Substituted imidazo[1,2-c]pyrimidines
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
EP0308020A3 (en) 1987-09-18 1990-12-05 Merck & Co. Inc. 5-(aryl and heteroaryl)-6-(aryl and heteroaryl)-1,2-dihydro-2-oxo 3-pyridinecarboxylic acids and derivatives thereof
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
US5554630A (en) 1993-03-24 1996-09-10 Neurosearch A/S Benzimidazole compounds
EP0767790B1 (en) 1994-06-20 2001-12-12 Takeda Chemical Industries, Ltd. Condensed imidazole compounds, their production and use
AU5348396A (en) 1995-05-01 1996-11-21 Fujisawa Pharmaceutical Co., Ltd. Imidazo 1,2-a pyridine and imidazo 1,2-a pyridezine derivati ves and their use as bone resorption inhibitors
US6218529B1 (en) 1995-07-31 2001-04-17 Urocor, Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate, breast and bladder cancer
CA2262403C (en) 1995-07-31 2011-09-20 Urocor, Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate disease
AU6966696A (en) 1995-10-05 1997-04-28 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
EP1908764A1 (en) 1996-07-24 2008-04-09 Bristol-Myers Squibb Pharma Company Azolo triazines and pyrimidines
EP0984692A4 (en) 1997-05-30 2001-02-21 Merck & Co Inc ANGIOGENESIS INHIBITORS
US5990146A (en) 1997-08-20 1999-11-23 Warner-Lambert Company Benzimidazoles for inhibiting protein tyrosine kinase mediated cellular proliferation
US6465484B1 (en) 1997-09-26 2002-10-15 Merck & Co., Inc. Angiogenesis inhibitors
NZ505079A (en) 1998-01-28 2003-08-29 Du Pont Pharm Co Pyrazolotriazines and pyrazolopyrimidines useful as corticotropin releasing factor antagonists
CA2341409A1 (en) 1998-08-31 2000-03-09 Merck And Co., Inc. Novel angiogenesis inhibitors
US6245759B1 (en) 1999-03-11 2001-06-12 Merck & Co., Inc. Tyrosine kinase inhibitors
JP2003503354A (ja) 1999-06-30 2003-01-28 メルク エンド カムパニー インコーポレーテッド Ｓｒｃキナーゼ阻害剤化合物
ATE253915T1 (de) 1999-06-30 2003-11-15 Merck & Co Inc Src-kinase hemmende verbindungen
EP1206260A4 (en) 1999-06-30 2002-10-30 Merck & Co Inc SRC-KINASE INHIBITING COMPOUNDS
JP2001057292A (ja) 1999-08-20 2001-02-27 Toray Ind Inc 発光素子
GB9919778D0 (en) * 1999-08-21 1999-10-27 Zeneca Ltd Chemical compounds
GB9921150D0 (en) 1999-09-07 1999-11-10 Merck Sharp & Dohme Therapeutic agents
EP1214330A1 (en) 1999-09-21 2002-06-19 LION Bioscience AG Benzimidazole derivatives and combinatorial libraries thereof
GB9927687D0 (en) 1999-11-23 2000-01-19 Merck Sharp & Dohme Therapeutic agents
ATE414079T1 (de) * 2000-03-01 2008-11-15 Janssen Pharmaceutica Nv 2,4-disubstituierte thiazolyl derivate
JP2004500389A (ja) 2000-03-09 2004-01-08 アベンティス・ファーマ・ドイチユラント・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング Ｐｐａｒメディエーターの治療での使用
US20020041880A1 (en) 2000-07-05 2002-04-11 Defeo-Jones Deborah Method of treating cancer
DE60135854D1 (de) 2000-08-04 2008-10-30 Warner Lambert Co 2-(4-Pyridyl)amino-6-dialkoxyphenyl-pyrido(2,3-d)pyrimidin-7-one
AU2001295992A1 (en) 2000-10-24 2002-05-06 Sankyo Company Limited Imidazopyridine derivatives
GB0027561D0 (en) 2000-11-10 2000-12-27 Merck Sharp & Dohme Therapeutic agents
WO2002046168A1 (en) 2000-12-07 2002-06-13 Astrazeneca Ab Therapeutic benzimidazole compounds
US20020107262A1 (en) 2000-12-08 2002-08-08 3M Innovative Properties Company Substituted imidazopyridines
GB0103926D0 (en) 2001-02-17 2001-04-04 Astrazeneca Ab Chemical compounds
SE0100568D0 (sv) 2001-02-20 2001-02-20 Astrazeneca Ab Compounds
KR20030076688A (ko) 2001-02-20 2003-09-26 아스트라제네카 아베 Ｇｓｋ3-관련 장애의 치료를 위한 2-아릴아미노-피리미딘
SE0100567D0 (sv) 2001-02-20 2001-02-20 Astrazeneca Ab Compounds
TWI248936B (en) 2001-03-21 2006-02-11 Merck Sharp & Dohme Imidazo-pyrimidine derivatives as ligands for GABA receptors
DE10117183A1 (de) 2001-04-05 2002-10-10 Gruenenthal Gmbh Verwendung von substituierten Imidazo[1,2-a]-pyridinverbindungen als Arzneimittel
EP1382603B1 (en) 2001-04-26 2008-07-23 Eisai R&D Management Co., Ltd. Nitrogenous fused-ring compound having pyrazolyl group as substituent and medicinal composition thereof
AU2002317377A1 (en) 2001-07-20 2003-03-03 Cancer Research Technology Limited Biphenyl apurinic/apyrimidinic site endonuclease inhibitors to treat cancer
GB0128499D0 (en) 2001-11-28 2002-01-23 Merck Sharp & Dohme Therapeutic agents
US6900208B2 (en) 2002-03-28 2005-05-31 Bristol Myers Squibb Company Pyrrolopyridazine compounds and methods of use thereof for the treatment of proliferative disorders
CN100343255C (zh) 2002-04-23 2007-10-17 盐野义制药株式会社 吡唑并[1,5－a]嘧啶衍生物和含有该衍生物的NAD(P)H氧化酶抑制剂
JP2004002826A (ja) 2002-04-24 2004-01-08 Sankyo Co Ltd 高分子イミダゾピリジン誘導体
CA2483084A1 (en) 2002-05-02 2003-11-13 Merck & Co., Inc. Tyrosine kinase inhibitors
GB2398781B (en) 2002-05-23 2005-02-02 Cytopia Pty Ltd Kinase inhibitors
AUPS251402A0 (en) * 2002-05-23 2002-06-13 Cytopia Pty Ltd Kinase inhibitors
GB0212049D0 (en) 2002-05-24 2002-07-03 Merck Sharp & Dohme Therapeutic agents
GB0212048D0 (en) 2002-05-24 2002-07-03 Merck Sharp & Dohme Therapeutic agents
AU2003240488A1 (en) 2002-06-04 2003-12-19 Neogenesis Pharmaceuticals, Inc. Pyrazolo` 1,5a! pyrimidine compounds as antiviral agents
US7196090B2 (en) 2002-07-25 2007-03-27 Warner-Lambert Company Kinase inhibitors
EP1539756B1 (en) 2002-09-19 2007-11-14 Schering Corporation Imidazopyridines as cyclin dependent kinase inhibitors
GB0223349D0 (en) 2002-10-08 2002-11-13 Merck Sharp & Dohme Therapeutic agents
AU2003271185A1 (en) 2002-10-15 2004-05-04 Takeda Pharmaceutical Company Limited Imidazopyridine derivative, process for producing the same, and use
AU2003299651A1 (en) 2002-12-11 2004-06-30 Merck And Co., Inc. Tyrosine kinase inhibitors
AU2003298942A1 (en) 2002-12-11 2004-06-30 Merck And Co., Inc. Tyrosine kinase inhibitors
US7826979B2 (en) 2003-02-14 2010-11-02 Vertex Pharmaceuticals Incorporated Method of modeling complex formation between a query ligan and a target molecule
US7476670B2 (en) 2003-02-18 2009-01-13 Aventis Pharma S.A. Purine derivatives, method for preparing, pharmaceutical compositions and novel use
FR2851248B1 (fr) * 2003-02-18 2005-04-08 Aventis Pharma Sa Nouveaux derives de la purine, leur procede de preparation, leur application a titre de medicaments, compositions pharmaceutiques et nouvelle utilisation
US7157460B2 (en) 2003-02-20 2007-01-02 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
US7893096B2 (en) 2003-03-28 2011-02-22 Novartis Vaccines And Diagnostics, Inc. Use of small molecule compounds for immunopotentiation
US7885960B2 (en) 2003-07-22 2011-02-08 Microsoft Corporation Community mining based on core objects and affiliated objects
UA82395C2 (en) 2003-08-21 2008-04-10 Оси Фармасьютикалз, Инк. N-substituted benzimidazolyl c-kit inhibitors
AU2004268950A1 (en) 2003-08-21 2005-03-10 Osi Pharmaceuticals, Inc. N3-substituted imidazopyridine-derivatives as c-kit inhibitors
US7442709B2 (en) 2003-08-21 2008-10-28 Osi Pharmaceuticals, Inc. N3-substituted imidazopyridine c-Kit inhibitors
JP4808628B2 (ja) 2003-12-03 2011-11-02 ワイエム・バイオサイエンシズ・オーストラリア・ピーティーワイ・リミテッド アゾール系キナーゼ阻害剤
WO2005075470A1 (en) 2004-01-28 2005-08-18 Smithkline Beecham Corporation Thiazole compounds
TW200530236A (en) 2004-02-23 2005-09-16 Chugai Pharmaceutical Co Ltd Heteroaryl phenylurea
US7566781B2 (en) 2004-05-10 2009-07-28 Banyu Pharmaceutical Co., Ltd. Imidazopyridine compound
GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds
WO2006025567A1 (ja) * 2004-08-31 2006-03-09 Banyu Pharmaceutical Co., Ltd. 新規置換イミダゾール誘導体
EP1809294A4 (en) 2004-09-21 2008-08-06 Synta Pharmaceuticals Corp COMPOUNDS AGAINST INFLAMMATION AND IMMUNE-RELEVANT USES
WO2006038001A1 (en) 2004-10-06 2006-04-13 Celltech R & D Limited Aminopyrimidine derivatives as jnk inhibitors
BRPI0518794A2 (pt) * 2004-12-01 2008-12-09 Osi Pharm Inc composto, composiÇço, mÉtodo de tratamento de distérbio hiperproliferativo, e, biblioteca combinatorial
JPWO2006070943A1 (ja) 2004-12-28 2008-06-12 武田薬品工業株式会社 縮合イミダゾール化合物およびその用途
WO2006070198A1 (en) 2004-12-30 2006-07-06 Astex Therapeutics Limited Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases
DOP2006000051A (es) 2005-02-24 2006-08-31 Lilly Co Eli Inhibidores de vegf-r2 y métodos
CA2599987A1 (en) 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. Fused heterocyclic compounds and their use as sirtuin modulators
KR20080013886A (ko) 2005-04-05 2008-02-13 파마코페이아, 인코포레이티드 면역억제용 퓨린 및 이미다조피리딘 유도체
FR2884821B1 (fr) 2005-04-26 2007-07-06 Aventis Pharma Sa Pyrrolopyridines substitues, compositions les contenant, procede de fabrication et utilisation
US7572807B2 (en) 2005-06-09 2009-08-11 Bristol-Myers Squibb Company Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors
WO2007036732A1 (en) 2005-09-30 2007-04-05 Astrazeneca Ab Imidazo [1,2-a] pyridine having anti-cell-proliferation activity
AU2007227210A1 (en) 2006-03-20 2007-09-27 Synta Pharmaceuticals Corp. Benzoimidazolyl-parazine compounds for inflammation and immune-related uses
US8163777B2 (en) 2006-03-23 2012-04-24 Synta Pharmaceuticals Corp. Benzimidazolyl-pyridine compounds for inflammation and immune-related uses
ITVA20060041A1 (it) 2006-07-05 2008-01-06 Dialectica Srl Uso di composti derivati amminotiazolici, di loro composizioni farmaceutiche, nel trattamento di malattie caratterizzate dalla anormale repressione della trascrizione genica, particolarmente il morbo di huntington
TW200811134A (en) 2006-07-12 2008-03-01 Irm Llc Compounds and compositions as protein kinase inhibitors
EP1882475A1 (en) 2006-07-26 2008-01-30 Novartis AG Method of treating disorders mediated by the fibroblast growth factor receptor
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
CA2672213C (en) 2006-12-22 2016-02-16 Astex Therapeutics Limited Bicyclic amine derivatives as protein tyrosine kinase inhibitors
US8131527B1 (en) 2006-12-22 2012-03-06 Astex Therapeutics Ltd. FGFR pharmacophore compounds
WO2008078091A1 (en) 2006-12-22 2008-07-03 Astex Therapeutics Limited Bicyclic heterocyclic compounds as fgfr inhibitors
US7977336B2 (en) 2006-12-28 2011-07-12 Banyu Pharmaceutical Co. Ltd Aminopyrimidine derivatives as PLK1 inhibitors
UA101611C2 (ru) 2007-04-03 2013-04-25 Аррей Байофарма Инк. СОЕДИНЕНИЯ ИМИДАЗО[1,2-а]ПИРИДИНА КАК ИНГИБИТОРЫ ТИРОЗИНКИНАЗЫ РЕЦЕПТОРОВ
CA2934114A1 (en) 2007-06-12 2008-12-18 Achaogen, Inc. Antibacterial agents
CA2690192A1 (en) 2007-06-26 2008-12-31 Gilead Colorado, Inc. Imidazopyridinyl thiazolyl histone deacetylase inhibitors
GB0720038D0 (en) 2007-10-12 2007-11-21 Astex Therapeutics Ltd New compounds
GB0720041D0 (en) 2007-10-12 2007-11-21 Astex Therapeutics Ltd New Compounds
GB0810902D0 (en) 2008-06-13 2008-07-23 Astex Therapeutics Ltd New compounds
GB0906472D0 (en) 2009-04-15 2009-05-20 Astex Therapeutics Ltd New compounds
GB0906470D0 (en) 2009-04-15 2009-05-20 Astex Therapeutics Ltd New compounds

Also Published As

Publication number Publication date
US20100093718A1 (en) 2010-04-15
WO2008078100A3 (en) 2008-11-13
EP2121687B1 (en) 2015-10-14
JP2010513448A (ja) 2010-04-30
CN101679409B (zh) 2014-11-26
WO2008078100A2 (en) 2008-07-03
PL2121687T3 (pl) 2016-03-31
CA2672213A1 (en) 2008-07-03
AU2007337895C1 (en) 2014-07-31
HRP20151398T1 (hr) 2016-02-12
CA2672213C (en) 2016-02-16
EP2121687A2 (en) 2009-11-25
AU2007337895B2 (en) 2014-01-30
JP5442449B2 (ja) 2014-03-12
NO342865B1 (no) 2018-08-20
AU2007337895A1 (en) 2008-07-03
CN101679409A (zh) 2010-03-24
NO20092658L (no) 2009-09-17
MX2009006704A (es) 2009-06-30
US8513276B2 (en) 2013-08-20

Similar Documents

Publication Publication Date Title
CY1117319T1 (el) Τρικυκλικα παραγωγα αμινης ως αναστολεις πρωτεϊνικης τυροσινης κινασης
CY1118061T1 (el) Δικυκλικα παραγωγα heterocyclyl σαν καταστολεις κινασης (kinase) fgfr για θεραπευτικη χρηση
CY1121021T1 (el) Ιμιδαζοτριαζινες και ιμιδαζοπυριμιδινες ως αναστολεις κινασης
CY1114277T1 (el) ΕΝΩΣΕΙΣ ΙΜΙΔΑΖΟ[1,2-a]ΠΥΡΙΔΙΝΗΣ ΩΣ ΑΝΑΣΤΟΛΕΙΣ ΥΠΟΔΟΧΕΑ ΚΙΝΑΣΗΣ ΤΥΡΟΣΙΝΗΣ
CY1121299T1 (el) Υποκατεστημενες τρικυκλικες ενωσεις ως αναστολεις fgfr
CY1110962T1 (el) Τρικυκλικες ενωσεις και η χρηση τους ως διαμορφωτες του υποδοχεα γλυκοκορτικοειδων
CY1117820T1 (el) Δικυκλικες ετερο-κυκλικες ενωσεις σαν καταστολεις κινασης (kinase) πρωτεϊνης
CY1116847T1 (el) Ειδικοι ανταγωνιστες του υποδοχεα fgf-r4
EA201001143A1 (ru) Активаторы прокаспаз "исполнителей" 3, 6 и 7
CY1118362T1 (el) Ανταγωνιστες υποδοχεων cgrp αζαϊνδανιου καρβοξαμιδιου πιπεριδινονης
CY1112297T1 (el) Ετεροκυκλικοι αναστολεις της μεκ και μεθοδοι χρησης αυτων
CY1111757T1 (el) Παραγωγα ξανθινης ως εκλεκτικοι αναστολεις ημ74α
CY1114543T1 (el) Παραγωγο υποκατεστημενου οξινδολιου και χρηση αυτου ως συνδετηρα υποδοχεα αγγειοπιεσινης
EA200601697A1 (ru) Производные карболина, полезные в ингибировании ангиогенеза
DE60315677D1 (de) Pyrazolopyridin derivate als tgf beta hemmstoffe zur behandlung von krebs
CY1114272T1 (el) Υποκατεστημενες διυδροπυραζολονες για την θεραπευτικη αντιμετωπιση των καρδιαγγειακων και αιματολογικων παθησεων
EA200700982A1 (ru) Производные хинолина и изохинолина, замещённые в 5-ом положении, способ их получения и их применение в качестве противовоспалительных средств
DK1853602T3 (da) Kemiske forbindelser
DK1853588T3 (da) Kemiske forbindelser
ECSP088561A (es) Derivados de pirimidinil-aril-urea que son inhibidores de fgf
DE602006007037D1 (de) Pyrrolotriazin-kinasehemmer
CY1111789T1 (el) Ετεροκυκλικες ενωσεις
DOP2006000061A (es) Derivados de pirimidina para el tratamiento de trastornos hiperproliferativos
EA201200218A1 (ru) Новые бициклические соединения мочевины
CY1110190T1 (el) Παραγωγα πιπεραζινυλιου χρησιμα στην αγωγη των νοσων στις οποιες μεσολαβει ο υποδοχεας gpr38