CN1514833A - 新型酪氨酸激酶抑制剂 - Google Patents

新型酪氨酸激酶抑制剂 Download PDF

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Publication number
CN1514833A
CN1514833A CNA028105168A CN02810516A CN1514833A CN 1514833 A CN1514833 A CN 1514833A CN A028105168 A CNA028105168 A CN A028105168A CN 02810516 A CN02810516 A CN 02810516A CN 1514833 A CN1514833 A CN 1514833A
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CN
China
Prior art keywords
pyridin
hydroxyl
phenyl
ethylamino
radicals
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.)
Pending
Application number
CNA028105168A
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English (en)
Chinese (zh)
Inventor
M��D����ά˹
M·D·维特曼
ղ���
N·巴拉苏布拉马尼安
ϣ
U·维拉帕特希
K·滋梅曼恩
M·G·索尼尔
�������ɭ
P·刘
���з�
X·尚
D·B·弗伦内森
K·M·斯托夫范
J·G·塔兰特
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
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Bristol Myers Squibb Co
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Filing date
Publication date
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of CN1514833A publication Critical patent/CN1514833A/zh
Pending legal-status Critical Current

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    • 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)
  • 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)
  • 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)
CNA028105168A 2001-03-28 2002-03-26 新型酪氨酸激酶抑制剂 Pending CN1514833A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US27932701P 2001-03-28 2001-03-28
US60/279,327 2001-03-28

Publications (1)

Publication Number Publication Date
CN1514833A true CN1514833A (zh) 2004-07-21

Family

ID=23068491

Family Applications (1)

Application Number Title Priority Date Filing Date
CNA028105168A Pending CN1514833A (zh) 2001-03-28 2002-03-26 新型酪氨酸激酶抑制剂

Country Status (25)

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

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101291926A (zh) * 2005-08-29 2008-10-22 沃泰克斯药物股份有限公司 可用作Tec家族非受体酪氨酸激酶抑制剂的3,5-二取代的吡啶-2-酮
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
CN103124496A (zh) * 2010-10-06 2013-05-29 葛兰素史密丝克莱恩有限责任公司 作为pi3激酶抑制剂的苯并咪唑衍生物
CN103864704A (zh) * 2009-03-18 2014-06-18 拜耳知识产权有限责任公司 取代的2-乙酰胺基-5-芳基-1,2,4-三唑酮和它的用途
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

Families Citing this family (47)

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US7081454B2 (en) * 2001-03-28 2006-07-25 Bristol-Myers Squibb Co. Tyrosine kinase inhibitors
EP1480514A4 (en) 2002-03-01 2008-08-13 Bristol Myers Squibb Co TRANSGENIC NON-HUMAN MAMMALS EXPRESS CONSTITUTIVELY ACTIVATED TYROSINE KINASE RECEPTORS
CA2488635C (en) * 2002-06-12 2012-10-23 Abbott Laboratories Antagonists of melanin concentrating hormone receptor
US7361691B2 (en) * 2002-12-02 2008-04-22 Arqule, Inc. Method of treating cancers using β-lapachone or analogs or derivatives thereof
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
EP1663204B1 (en) * 2003-08-29 2014-05-07 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
AP2139A (en) 2004-04-02 2010-08-21 Osi Pharm Inc 6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors.
EP1831168B1 (en) * 2004-12-16 2014-07-02 Vertex Pharmaceuticals Inc. 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
EP2388263A1 (en) 2005-08-04 2011-11-23 Sirtris Pharmaceuticals, Inc. Imidazo[2,1-b]thiazole derivatives as sirtuin modulators
US7855289B2 (en) 2005-08-04 2010-12-21 Sirtris Pharmaceuticals, Inc. Sirtuin modulating 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
EP1919906B1 (en) 2005-08-29 2011-10-12 Vertex Pharmaceuticals Incorporated 3, 5-disubstituted pyrid-2-ones useful as inhibitors of tec family of non-receptor tyrosine kinases
EP1919891B1 (en) 2005-08-29 2012-03-07 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
EP2145021A2 (en) 2007-05-17 2010-01-20 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.
US7956190B2 (en) 2007-06-25 2011-06-07 Hoffmann-La Roche Inc. Benzimidazole amido derivatives as kinase inhibitors
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
WO2009143051A1 (en) 2008-05-19 2009-11-26 Osi Pharmaceuticals, Inc. Substituted imidazopyr-and imidazotri-azines
BRPI0922435A2 (pt) 2008-12-19 2018-09-11 Sirtris Pharmaceuticals Inc "composto de tiazolopiridina moduladores de sirtuina, composição farmacêutica compreendendo o mesmo e seu uso."
BRPI1016245A2 (pt) 2009-04-20 2015-09-01 Osi Pharmaceuticals Llc Preparação de c-pirazina-metilaminas.
WO2011053779A2 (en) 2009-10-30 2011-05-05 Bristol-Myers Squibb Company Methods for treating cancer in patients having igf-1r inhibitor resistance
WO2012061169A1 (en) * 2010-11-01 2012-05-10 Boehringer Ingelheim International Gmbh Benzimidazole inhibitors of leukotriene production
WO2013056069A1 (en) 2011-10-13 2013-04-18 Bristol-Myers Squibb Company Methods for selecting and treating cancer in patients with igf-1r/ir inhibitors
SI3010503T1 (sl) 2013-06-21 2020-07-31 Zenith Epigenetics Ltd. Novi biciklični inhibitorji bromodomene
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
KR20160038008A (ko) 2013-07-31 2016-04-06 제니쓰 에피제네틱스 코포레이션 브로모도메인 억제제로서 신규 퀴나졸리논
JP2017525351A (ja) 2014-07-30 2017-09-07 イェダ リサーチ アンド ディベロップメント カンパニー リミテッドＹｅｄａ Ｒｅｓｅａｒｃｈ Ａｎｄ Ｄｅｖｅｌｏｐｍｅｎｔ Ｃｏ．Ｌｔｄ． 多能性幹細胞の培養用培地
CA2966298A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
EP3230277B1 (en) 2014-12-11 2019-09-18 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
EP3233846A4 (en) 2014-12-17 2018-07-18 Zenith Epigenetics Ltd. Inhibitors of bromodomains
JP6827954B2 (ja) * 2015-04-16 2021-02-10 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ ３−（１ｈ−ベンズイミダゾール−２−イル）−１ｈ−ピリジン−２−オン誘導体
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

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Publication number Priority date Publication date Assignee Title
US6162804A (en) * 1997-09-26 2000-12-19 Merck & Co., Inc. Tyrosine kinase inhibitors
NZ516348A (en) * 1999-06-23 2003-06-30 Aventis Pharma Gmbh Substituted benzimidazole
US7081454B2 (en) * 2001-03-28 2006-07-25 Bristol-Myers Squibb Co. Tyrosine kinase inhibitors

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101291926A (zh) * 2005-08-29 2008-10-22 沃泰克斯药物股份有限公司 可用作Tec家族非受体酪氨酸激酶抑制剂的3,5-二取代的吡啶-2-酮
CN103864704A (zh) * 2009-03-18 2014-06-18 拜耳知识产权有限责任公司 取代的2-乙酰胺基-5-芳基-1,2,4-三唑酮和它的用途
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
CN103124496A (zh) * 2010-10-06 2013-05-29 葛兰素史密丝克莱恩有限责任公司 作为pi3激酶抑制剂的苯并咪唑衍生物
CN103124496B (zh) * 2010-10-06 2016-03-30 葛兰素史密丝克莱恩有限责任公司 作为pi3激酶抑制剂的苯并咪唑衍生物
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

Also Published As

Publication number Publication date
CZ20032615A3 (en) 2004-03-17
YU84603A (sh) 2006-03-03
GEP20053660B (en) 2005-11-10
NO20034308D0 (no) 2003-09-26
HUP0400323A2 (hu) 2005-11-28
JP2004534010A (ja) 2004-11-11
EP1381598A4 (en) 2008-03-19
BR0208373A (pt) 2005-02-22
PL373300A1 (en) 2005-08-22
UY27234A1 (es) 2002-10-31
RU2003131693A (ru) 2005-05-10
EE200300475A (et) 2004-02-16
EP1381598A1 (en) 2004-01-21
IS6968A (is) 2003-09-26
NO20034308L (no) 2003-11-26
PE20021015A1 (es) 2002-11-10
BG108206A (bg) 2004-11-30
ZA200307466B (en) 2005-01-13
AR035804A1 (es) 2004-07-14
WO2002079192A1 (en) 2002-10-10
SK12002003A3 (en) 2004-10-05
MXPA03008690A (es) 2003-12-12
IL158041A0 (en) 2004-03-28
CA2442428A1 (en) 2002-10-10
KR20030083016A (ko) 2003-10-23
HRP20030844A2 (en) 2005-08-31

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