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
phenyl
ethylamino
hydroxyl
methyl
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Pending
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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
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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Publication of CN1514833A publication Critical patent/CN1514833A/zh
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    • 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

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  • 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)

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

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

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US7081454B2 (en) * 2001-03-28 2006-07-25 Bristol-Myers Squibb Co. Tyrosine kinase inhibitors
AU2003218236B2 (en) 2002-03-01 2007-12-06 Bristol-Myers Squibb Company Transgenic non-human mammals expressing constitutively activated tyrosine kinase receptors
WO2003106452A2 (en) * 2002-06-12 2003-12-24 Millennium Pharmaceuticals, Inc. Antagonists of melanin concentrating hormone receptor
EP1575580A4 (en) * 2002-12-02 2009-06-10 Arqule Inc METHOD FOR TREATING CARCINOMA
WO2004063151A2 (en) 2003-01-03 2004-07-29 Bristol-Myers Squibb Company Novel tyrosine kinase inhibitors
WO2004069160A2 (en) * 2003-01-28 2004-08-19 Smithkline Beecham Corporation 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
JP2007514759A (ja) 2003-12-19 2007-06-07 タケダ サン ディエゴ インコーポレイテッド キナーゼ阻害剤
DE102004010207A1 (de) 2004-03-02 2005-09-15 Aventis Pharma S.A. Neue 4-Benzimidazol-2-yl-pyridazin-3-on-Derivate
CN1960993A (zh) 2004-04-02 2007-05-09 Osi制药公司 6,6-双环取代的杂双环蛋白激酶抑制剂
WO2006023931A2 (en) 2004-08-18 2006-03-02 Takeda San Diego, Inc. Kinase inhibitors
WO2006065946A1 (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
US7538113B2 (en) 2005-02-18 2009-05-26 Wyeth 4-substituted imidazo[4,5-c]pyridine antagonists of gonadotropin releasing hormone receptor
US7534796B2 (en) 2005-02-18 2009-05-19 Wyeth Imidazo[4,5-b]pyridine antagonists of gonadotropin releasing hormone receptor
US7582634B2 (en) 2005-02-18 2009-09-01 Wyeth 7-substituted imidazo[4,5-c]pyridine antagonists of gonadotropin releasing hormone receptor
US7531542B2 (en) 2005-05-18 2009-05-12 Wyeth Benzooxazole and benzothiazole antagonists of gonadotropin releasing hormone receptor
US7582636B2 (en) 2005-05-26 2009-09-01 Wyeth Piperazinylimidazopyridine and piperazinyltriazolopyridine antagonists of Gonadotropin Releasing Hormone receptor
WO2006130657A2 (en) 2005-05-31 2006-12-07 Bristol-Myers Squibb Company Stereoselective reduction process for the preparation of pyrrolotriazine compounds
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
ES2397275T3 (es) 2005-08-04 2013-03-05 Sirtris Pharmaceuticals, Inc. Derivados de imidazopiridina como agentes moduladores de la sirtuína
US8088928B2 (en) 2005-08-04 2012-01-03 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
WO2007027729A1 (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
ATE548363T1 (de) 2005-08-29 2012-03-15 Vertex Pharma 3,5-disubstituierte pyrid-2-one, die sich als inhibitoren der tec-familie von nicht-rezeptor- tyrosinkinasen eignen
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.
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
CA2712959C (en) * 2008-01-22 2015-06-23 Vernalis (R & D) Ltd Indolyl-pyridone derivatives having checkpoint kinase 1 inhibitory activity
EP2283020B8 (en) 2008-05-19 2012-12-12 OSI Pharmaceuticals, LLC Substituted imidazopyr-and imidazotri-azines
CN102388054B (zh) 2008-12-19 2015-03-04 西特里斯药业公司 噻唑并吡啶沉默调节蛋白调节剂的化合物
EP2421837A1 (en) 2009-04-20 2012-02-29 OSI Pharmaceuticals, LLC Preparation of c-pyrazine-methylamines
WO2011053779A2 (en) 2009-10-30 2011-05-05 Bristol-Myers Squibb Company Methods for treating cancer in patients having igf-1r inhibitor resistance
EP2635566B1 (en) * 2010-11-01 2018-05-16 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
CN105407888B (zh) 2013-06-21 2019-05-21 齐尼思表观遗传学有限公司 新双环溴结构域抑制剂
WO2015004534A2 (en) 2013-06-21 2015-01-15 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
JP6542212B2 (ja) 2013-07-31 2019-07-10 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キナゾリノン
WO2016016894A1 (en) 2014-07-30 2016-02-04 Yeda Research And Development Co. Ltd. Media for culturing pluripotent stem cells
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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
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
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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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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

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

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