EP1381598A4 - NEW INHIBITORS OF TYROSINE KINASE - Google Patents

NEW INHIBITORS OF TYROSINE KINASE

Info

Publication number
EP1381598A4
EP1381598A4 EP02723631A EP02723631A EP1381598A4 EP 1381598 A4 EP1381598 A4 EP 1381598A4 EP 02723631 A EP02723631 A EP 02723631A EP 02723631 A EP02723631 A EP 02723631A EP 1381598 A4 EP1381598 A4 EP 1381598A4
Authority
EP
European Patent Office
Prior art keywords
tyrosine kinase
kinase inhibitors
novel tyrosine
novel
inhibitors
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
EP02723631A
Other languages
German (de)
English (en)
French (fr)
Other versions
EP1381598A1 (en
Inventor
Mark D Wittman
Neelakantan Balasubramanian
Upender Velaparthi
Kurt Zimmermann
Mark G Saulnier
Peiying Liu
Xiaopeng Sang
David B Frennesson
Karen M Stoffan
James G Tarrant
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bristol Myers Squibb Co
Original Assignee
Bristol Myers Squibb Co
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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of EP1381598A1 publication Critical patent/EP1381598A1/en
Publication of EP1381598A4 publication Critical patent/EP1381598A4/en
Withdrawn legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
EP02723631A 2001-03-28 2002-03-26 NEW INHIBITORS OF TYROSINE KINASE Withdrawn EP1381598A4 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US27932701P 2001-03-28 2001-03-28
US279327P 2001-03-28
PCT/US2002/009402 WO2002079192A1 (en) 2001-03-28 2002-03-26 Novel tyrosine kinase inhibitors

Publications (2)

Publication Number Publication Date
EP1381598A1 EP1381598A1 (en) 2004-01-21
EP1381598A4 true EP1381598A4 (en) 2008-03-19

Family

ID=23068491

Family Applications (1)

Application Number Title Priority Date Filing Date
EP02723631A Withdrawn EP1381598A4 (en) 2001-03-28 2002-03-26 NEW INHIBITORS OF TYROSINE KINASE

Country Status (25)

Country Link
EP (1) EP1381598A4 (pt)
JP (1) JP2004534010A (pt)
KR (1) KR20030083016A (pt)
CN (1) CN1514833A (pt)
AR (1) AR035804A1 (pt)
BG (1) BG108206A (pt)
BR (1) BR0208373A (pt)
CA (1) CA2442428A1 (pt)
CZ (1) CZ20032615A3 (pt)
EE (1) EE200300475A (pt)
GE (1) GEP20053660B (pt)
HR (1) HRP20030844A2 (pt)
HU (1) HUP0400323A2 (pt)
IL (1) IL158041A0 (pt)
IS (1) IS6968A (pt)
MX (1) MXPA03008690A (pt)
NO (1) NO20034308L (pt)
PE (1) PE20021015A1 (pt)
PL (1) PL373300A1 (pt)
RU (1) RU2003131693A (pt)
SK (1) SK12002003A3 (pt)
UY (1) UY27234A1 (pt)
WO (1) WO2002079192A1 (pt)
YU (1) YU84603A (pt)
ZA (1) ZA200307466B (pt)

Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7081454B2 (en) * 2001-03-28 2006-07-25 Bristol-Myers Squibb Co. Tyrosine kinase inhibitors
IL163515A0 (en) 2002-03-01 2005-12-18 Bristol Myers Squibb Co Transgenic non-human mammals
WO2003106452A2 (en) * 2002-06-12 2003-12-24 Millennium Pharmaceuticals, Inc. Antagonists of melanin concentrating hormone receptor
WO2004050033A2 (en) * 2002-12-02 2004-06-17 Arqule, Inc. Method of treating cancers
WO2004063151A2 (en) 2003-01-03 2004-07-29 Bristol-Myers Squibb Company Novel tyrosine kinase inhibitors
EP1590339A4 (en) * 2003-01-28 2007-07-25 Smithkline Beecham Corp CHEMICAL COMPOUNDS
US7312215B2 (en) 2003-07-29 2007-12-25 Bristol-Myers Squibb Company Benzimidazole C-2 heterocycles as kinase inhibitors
CA2536954C (en) 2003-08-29 2012-11-27 Exelixis, Inc. C-kit modulators and methods of use
US20050075358A1 (en) * 2003-10-06 2005-04-07 Carboni Joan M. Methods for treating IGF1R-inhibitor induced hyperglycemia
DE102004010207A1 (de) * 2004-03-02 2005-09-15 Aventis Pharma S.A. Neue 4-Benzimidazol-2-yl-pyridazin-3-on-Derivate
EP2168968B1 (en) 2004-04-02 2017-08-23 OSI Pharmaceuticals, LLC 6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors
US8101770B2 (en) * 2004-12-16 2012-01-24 Vertex Pharmaceuticals Incorporated Pyridones useful as inhibitors of kinases
WO2006130657A2 (en) 2005-05-31 2006-12-07 Bristol-Myers Squibb Company Stereoselective reduction process for the preparation of pyrrolotriazine compounds
US8093401B2 (en) 2005-08-04 2012-01-10 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
US8088928B2 (en) 2005-08-04 2012-01-03 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
US7855289B2 (en) 2005-08-04 2010-12-21 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
ES2431050T3 (es) 2005-08-04 2013-11-22 Sirtris Pharmaceuticals, Inc. Benzotiazoles y tiazolopiridinas como moduladores de la sirtuína
CA2620352A1 (en) 2005-08-29 2007-03-08 Vertex Pharmaceuticals Incorporated 3, 5-disubstituted pyrid-2-ones useful as inhibitors of tec family of non-receptor tyrosine kinases
JP5112317B2 (ja) * 2005-08-29 2013-01-09 バーテックス ファーマシューティカルズ インコーポレイテッド 非受容体型チロシンキナーゼのｔｅｃファミリーの阻害剤として有用な３，５−二置換ピリド−２−オン
CA2620269A1 (en) 2005-08-29 2007-03-08 Vertex Pharmaceuticals Incorporated 3,5-disubstituted pyrid-2-ones useful as inhibitors of tec family of non-receptor tyrosine kinases
WO2007026720A1 (ja) * 2005-08-31 2007-03-08 Taisho Pharmaceutical Co., Ltd. 縮環ピラゾール誘導体
US8575164B2 (en) 2005-12-19 2013-11-05 OSI Pharmaceuticals, LLC Combination cancer therapy
WO2007145203A1 (ja) * 2006-06-13 2007-12-21 Daiichi Fine Chemical Co., Ltd. 光学活性２－アミノ－１－（４－フルオロフェニル）エタノール
US8063225B2 (en) * 2006-08-14 2011-11-22 Chembridge Corporation Tricyclic compound derivatives useful in the treatment of neoplastic diseases, inflammatory disorders and immunomodulatory disorders
WO2008022747A1 (en) * 2006-08-21 2008-02-28 F. Hoffmann-La Roche Ag Tricyclic lactam derivatives, their manufacture and use as pharmaceutical agents
WO2008025526A1 (en) * 2006-08-31 2008-03-06 F. Hoffmann-La Roche Ag Indole derivatives, their manufacture and use as pharmaceutical agents
US8492328B2 (en) 2007-05-17 2013-07-23 Bristol-Myers Squibb Company Biomarkers and methods for determining sensitivity to insulin growth factor-1 receptor modulators
TW200916472A (en) 2007-06-20 2009-04-16 Sirtris Pharmaceuticals Inc Sirtuin modulating compounds
CN101687840A (zh) * 2007-06-25 2010-03-31 霍夫曼-拉罗奇有限公司 作为激酶抑制剂的苯并咪唑酰胺基衍生物
EP2065380A1 (en) * 2007-08-22 2009-06-03 F.Hoffmann-La Roche Ag Pyridoneamide derivatives as focal adhesion kinase (FAK) inhibitors and their use for the treatment of cancer
US7816540B2 (en) * 2007-12-21 2010-10-19 Hoffmann-La Roche Inc. Carboxyl- or hydroxyl-substituted benzimidazole derivatives
BRPI0906495B8 (pt) * 2008-01-22 2021-05-25 Vernalis R&D Ltd compostos derivados de indolil-piridona e composição farmacêutica
JP2011520970A (ja) 2008-05-19 2011-07-21 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 置換されたイミダゾピラジン類およびイミダゾトリアジン類
JP5628828B2 (ja) 2008-12-19 2014-11-19 サートリス ファーマシューティカルズ， インコーポレイテッド チアゾロピリジンサーチュイン調節化合物
DE102010001064A1 (de) * 2009-03-18 2010-09-23 Bayer Schering Pharma Aktiengesellschaft Substituierte 2-Acetamido-5-Aryl-1,2,4-triazolone und deren Verwendung
CA2752826A1 (en) 2009-04-20 2010-10-28 OSI Pharmaceuticals, LLC Preparation of c-pyrazine-methylamines
CA2763624A1 (en) * 2009-05-27 2010-12-02 Abbott Laboratories Pyrimidine inhibitors of kinase activity
US20120220594A1 (en) 2009-10-30 2012-08-30 Bristol-Meyers Squibb Company Methods for treating cancer in patients having igf-1r inhibitor resistance
MA34591B1 (fr) * 2010-10-06 2013-10-02 Glaxosmithkline Llc Dérivés de benzimidazole utilisés comme inhibiteurs de pi3 kinase
EP2635566B1 (en) * 2010-11-01 2018-05-16 Boehringer Ingelheim International GmbH Benzimidazole inhibitors of leukotriene production
EP2766497A1 (en) 2011-10-13 2014-08-20 Bristol-Myers Squibb Company Methods for selecting and treating cancer in patients with igf-1r/ir inhibitors
BR112015031073B1 (pt) 2013-06-21 2022-11-29 Zenith Epigenetics Ltd Compostos inibidores bicíclicos de bromodomínio e composição farmacêutica contendo os referidos compostos
US9636328B2 (en) 2013-06-21 2017-05-02 Zenith Epigenetics Ltd. Substituted bicyclic compounds as bromodomain inhibitors
CN105593224B (zh) 2013-07-31 2021-05-25 恒元生物医药科技(苏州)有限公司 作为溴结构域抑制剂的新型喹唑啉酮类化合物
CN103936719A (zh) * 2014-05-14 2014-07-23 中国药科大学 苯并咪唑类衍生物制备方法及用途
EP3194572B1 (en) 2014-07-30 2023-10-25 Yeda Research and Development Co. Ltd. Media for culturing pluripotent stem cells
US10710992B2 (en) 2014-12-01 2020-07-14 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
JP2017537946A (ja) 2014-12-11 2017-12-21 ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． ブロモドメイン阻害剤としての置換複素環
US10231953B2 (en) 2014-12-17 2019-03-19 Zenith Epigenetics Ltd. Inhibitors of bromodomains
US10179777B2 (en) * 2015-04-16 2019-01-15 Merck Patent Gmbh 3-(1H-benzimidazol-2-yl)-1H-pyridin-2-one derivatives
EP3914698A1 (en) 2019-01-23 2021-12-01 Yeda Research and Development Co. Ltd Culture media for pluripotent stem cells
CN117069696B (zh) * 2023-08-17 2024-04-26 中国药科大学 一种双靶点小分子抑制剂及其制备方法和应用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6162804A (en) * 1997-09-26 2000-12-19 Merck & Co., Inc. Tyrosine kinase inhibitors
WO2001000610A1 (de) * 1999-06-23 2001-01-04 Aventis Pharma Deutschland Gmbh Substituierte benzimidazole
WO2004031401A2 (en) * 2002-10-02 2004-04-15 Bristol-Myers Squibb Company Novel tyrosine kinases inhibitors

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6162804A (en) * 1997-09-26 2000-12-19 Merck & Co., Inc. Tyrosine kinase inhibitors
WO2001000610A1 (de) * 1999-06-23 2001-01-04 Aventis Pharma Deutschland Gmbh Substituierte benzimidazole
WO2004031401A2 (en) * 2002-10-02 2004-04-15 Bristol-Myers Squibb Company Novel tyrosine kinases inhibitors

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
KATZ B A ET AL: "A novel serine protease inhibition motif involving a multi-centered short hydrogen bonding network at the active site", JOURNAL OF MOLECULAR BIOLOGY, LONDON, GB, vol. 307, no. 5, 13 April 2001 (2001-04-13), pages 1451 - 1486, XP004466071, ISSN: 0022-2836 *
See also references of WO02079192A1 *

Also Published As

Publication number Publication date
HUP0400323A2 (hu) 2005-11-28
PE20021015A1 (es) 2002-11-10
CN1514833A (zh) 2004-07-21
ZA200307466B (en) 2005-01-13
IS6968A (is) 2003-09-26
NO20034308D0 (no) 2003-09-26
CZ20032615A3 (en) 2004-03-17
BR0208373A (pt) 2005-02-22
IL158041A0 (en) 2004-03-28
JP2004534010A (ja) 2004-11-11
BG108206A (bg) 2004-11-30
PL373300A1 (en) 2005-08-22
RU2003131693A (ru) 2005-05-10
GEP20053660B (en) 2005-11-10
AR035804A1 (es) 2004-07-14
UY27234A1 (es) 2002-10-31
YU84603A (sh) 2006-03-03
EE200300475A (et) 2004-02-16
SK12002003A3 (en) 2004-10-05
KR20030083016A (ko) 2003-10-23
NO20034308L (no) 2003-11-26
MXPA03008690A (es) 2003-12-12
CA2442428A1 (en) 2002-10-10
WO2002079192A1 (en) 2002-10-10
EP1381598A1 (en) 2004-01-21
HRP20030844A2 (en) 2005-08-31

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