CA2442428A1 - Novel tyrosine kinase inhibitors - Google Patents

Novel tyrosine kinase inhibitors Download PDF

Info

Publication number
CA2442428A1
CA2442428A1 CA002442428A CA2442428A CA2442428A1 CA 2442428 A1 CA2442428 A1 CA 2442428A1 CA 002442428 A CA002442428 A CA 002442428A CA 2442428 A CA2442428 A CA 2442428A CA 2442428 A1 CA2442428 A1 CA 2442428A1
Authority
CA
Canada
Prior art keywords
methyl
pyridin
hydroxy
ethylamino
phenyl
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.)
Abandoned
Application number
CA002442428A
Other languages
English (en)
French (fr)
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
Individual
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 Individual filed Critical Individual
Publication of CA2442428A1 publication Critical patent/CA2442428A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic 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
    • C07D231/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic 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
    • C07D233/56Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • 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
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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)
CA002442428A 2001-03-28 2002-03-26 Novel tyrosine kinase inhibitors Abandoned CA2442428A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US27932701P 2001-03-28 2001-03-28
US60/279,327 2001-03-28
PCT/US2002/009402 WO2002079192A1 (en) 2001-03-28 2002-03-26 Novel tyrosine kinase inhibitors

Publications (1)

Publication Number Publication Date
CA2442428A1 true CA2442428A1 (en) 2002-10-10

Family

ID=23068491

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002442428A Abandoned CA2442428A1 (en) 2001-03-28 2002-03-26 Novel tyrosine kinase inhibitors

Country Status (25)

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

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
WO2003073841A2 (en) 2002-03-01 2003-09-12 Bristol-Myers Squibb Company Transgenic non-human mammals expressing constitutively activated tyrosine kinase receptors
JP2005532368A (ja) * 2002-06-12 2005-10-27 アボット・ラボラトリーズ メラニン濃縮ホルモン受容体の拮抗薬
EP1575580A4 (en) * 2002-12-02 2009-06-10 Arqule Inc METHODS OF TREATING CANCERS
US7189716B2 (en) 2003-01-03 2007-03-13 Bristol-Myers Squibb Company 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
WO2005020921A2 (en) * 2003-08-29 2005-03-10 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
DK1740591T3 (da) 2004-04-02 2009-10-26 Osi Pharm Inc Heterobicykliske proteinkinaseinhibitorer substitueret med en 6,6-biocyclisk ring
AU2005316540A1 (en) * 2004-12-16 2006-06-22 Vertex Pharmaceuticals Incorporated Pyrid-2-ones useful as inhibitors of Tec family protein kinases for the treatment of inflammatory, proliferative and immunologically-mediated diseases
US7393667B2 (en) 2005-05-31 2008-07-01 Bristol-Myers Squibb Company Stereoselective reduction process for the preparation of pyrrolotriazine 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
DK1910384T3 (da) 2005-08-04 2012-12-17 Sirtris Pharmaceuticals Inc Imidazo [2,1-b] thiazol-derivater som sirtuinmodulerende forbindelser
US8093401B2 (en) 2005-08-04 2012-01-10 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
EP1919905B1 (en) * 2005-08-29 2011-02-23 Vertex Pharmaceuticals Incorporated 3,5-disubstituted pyrid-2-ones useful as inhibitors of tec family of non-recptor tyrosine kinases
AU2006284900A1 (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
US7691885B2 (en) 2005-08-29 2010-04-06 Vertex Pharmaceuticals Incorporated Pyridones useful as inhibitors of 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
WO2008144345A2 (en) 2007-05-17 2008-11-27 Bristol-Myers Squibb Company Biomarkers and methods for determining sensitivity to insulin growth factor-1 receptor modulators
CL2008001822A1 (es) 2007-06-20 2009-03-13 Sirtris Pharmaceuticals Inc Compuestos derivados de tiazolo[5,4-b]piridina; composicion farmaceutica que comprende a dichos compuestos; y uso del compuesto en el tratamiento de la resistencia a la insulina, sindrome metabolico, diabetes, entre otras.
JP2010531316A (ja) * 2007-06-25 2010-09-24 エフ.ホフマン−ラ ロシュ アーゲー キナーゼ阻害剤としてのベンズイミダゾールアミド誘導体
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
NZ586756A (en) 2008-01-22 2012-04-27 Vernalis R&D Ltd Indolyl-pyridone derivatives having checkpoint kinase 1 inhibitory activity
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
EP2376502B1 (en) 2008-12-19 2015-06-17 GlaxoSmithKline LLC Thiazolopyridine sirtuin modulating compounds
DE102010001064A1 (de) * 2009-03-18 2010-09-23 Bayer Schering Pharma Aktiengesellschaft Substituierte 2-Acetamido-5-Aryl-1,2,4-triazolone und deren Verwendung
MX2011011025A (es) 2009-04-20 2011-11-02 Osi Pharmaceuticals Llc Preparacion de c-piracin-metilaminas.
CN102459265A (zh) * 2009-05-27 2012-05-16 雅培制药有限公司 激酶活性的嘧啶抑制剂
EP2494070A2 (en) 2009-10-30 2012-09-05 Bristol-Myers Squibb Company Methods for treating cancer in patients having igf-1r inhibitor resistance
LT2624696T (lt) * 2010-10-06 2017-03-10 Glaxosmithkline Llc Benzimidazolo deriniai kaip pi3 kinazės inhibitoriai
JP5789888B2 (ja) * 2010-11-01 2015-10-07 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ロイコトリエン生成のベンゾイミダゾールインヒビター
US20140309229A1 (en) 2011-10-13 2014-10-16 Bristol-Myers Squibb Company Methods for selecting and treating cancer in patients with igf-1r/ir inhibitors
JP6461118B2 (ja) * 2013-06-21 2019-01-30 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新規の置換された二環式化合物
NZ714669A (en) 2013-06-21 2021-07-30 Zenith Epigenetics Ltd Novel bicyclic bromodomain inhibitors
EA201690087A1 (ru) 2013-07-31 2016-08-31 Зенит Эпидженетикс Корп. Новые квиназолиноны как ингибиторы бромодомена
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
US11920164B2 (en) 2014-07-30 2024-03-05 Yeda Research And Development Co. Ltd. Media for culturing naive human pluripotent stem cells
WO2016087936A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridinones as bromodomain inhibitors
CA2966449A1 (en) 2014-12-11 2016-06-16 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
CN107406438B (zh) 2014-12-17 2021-05-14 恒翼生物医药科技(上海)有限公司 溴结构域的抑制剂
AU2016249537B2 (en) * 2015-04-16 2020-01-30 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

Family Cites Families (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
EP1194425B1 (de) * 1999-06-23 2005-08-10 Aventis Pharma Deutschland GmbH Substituierte benzimidazole
US7081454B2 (en) * 2001-03-28 2006-07-25 Bristol-Myers Squibb Co. Tyrosine kinase inhibitors

Also Published As

Publication number Publication date
PL373300A1 (en) 2005-08-22
KR20030083016A (ko) 2003-10-23
YU84603A (sh) 2006-03-03
IS6968A (is) 2003-09-26
CZ20032615A3 (en) 2004-03-17
HUP0400323A2 (hu) 2005-11-28
UY27234A1 (es) 2002-10-31
WO2002079192A1 (en) 2002-10-10
AR035804A1 (es) 2004-07-14
SK12002003A3 (en) 2004-10-05
JP2004534010A (ja) 2004-11-11
BG108206A (bg) 2004-11-30
NO20034308D0 (no) 2003-09-26
NO20034308L (no) 2003-11-26
HRP20030844A2 (en) 2005-08-31
EP1381598A4 (en) 2008-03-19
EE200300475A (et) 2004-02-16
RU2003131693A (ru) 2005-05-10
IL158041A0 (en) 2004-03-28
GEP20053660B (en) 2005-11-10
ZA200307466B (en) 2005-01-13
EP1381598A1 (en) 2004-01-21
PE20021015A1 (es) 2002-11-10
MXPA03008690A (es) 2003-12-12
BR0208373A (pt) 2005-02-22
CN1514833A (zh) 2004-07-21

Similar Documents

Publication Publication Date Title
CA2442428A1 (en) Novel tyrosine kinase inhibitors
US7081454B2 (en) Tyrosine kinase inhibitors
CA2534921C (en) Aminotriazole compounds useful as inhibitors of protein kinases
US7232826B2 (en) Tyrosine kinase inhibitors
US7470696B2 (en) Tyrosine kinase inhibitors
US8129403B2 (en) Chemical compounds
US6515004B1 (en) N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
KR20130028732A (ko) 4―아미노피리미딘 유도체 및 아데노신 a2a 수용체 안타고니스트로서의 이들의 용도
US9346795B2 (en) Substituted sulfonamides useful as antiapoptotic Bcl inhibitors
US20080113967A1 (en) Enzyme modulators and treatments
AU2004212421A1 (en) Heteroaryl substituted pyrolls useful as inhibitors of protein kinases
JP2011526616A (ja) 化学化合物
EA007968B1 (ru) N-замещённые производные пирролидина в качестве ингибиторов дипептидилпептидазы
MXPA04008807A (es) Derivados de 4-(imidazol-5-il)-2-(4-sulfonilanilino)pirimidina con actividad inhibidora de cdk.
US20100029643A1 (en) Heterocyclyc sulfonamides having edg-1 antagonistic activity
CA2547080A1 (en) Heterocyclic protein kinase inhibitors and uses thereof
CN115605463B (zh) 用于治疗疾病的受体相互作用蛋白激酶i的抑制剂
CA3079081A1 (en) Benzimidazole derivatives and their uses
CA2389280C (en) Triazoles as farnesyl transferase inhibitors
TW202220980A (zh) 新穎二唑系選擇性hdac6抑制劑
JP2003522174A (ja) サイクリン依存性キナーゼの3−アミノピラゾール阻害剤
AU2003251721A1 (en) Azole methylidene cyanide derivatives and their use as protein kinase modulators
AU2002254399A1 (en) Novel tyrosine kinase inhibitors

Legal Events

Date Code Title Description
FZDE Discontinued