CN1984660B - 作为天冬氨酸特异性半胱氨酸蛋白酶活化剂和细胞程序死亡诱导剂的4-芳基氨基-喹唑啉 - Google Patents

作为天冬氨酸特异性半胱氨酸蛋白酶活化剂和细胞程序死亡诱导剂的4-芳基氨基-喹唑啉 Download PDF

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CN1984660B
CN1984660B CN2004800242058A CN200480024205A CN1984660B CN 1984660 B CN1984660 B CN 1984660B CN 2004800242058 A CN2004800242058 A CN 2004800242058A CN 200480024205 A CN200480024205 A CN 200480024205A CN 1984660 B CN1984660 B CN 1984660B
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alkyl
methyl
group
quinazoline
phenyl
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Expired - Fee Related
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Chinese (zh)
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CN1984660A (zh
Inventor
蔡遂雄
N·S·希里索玛
A·珀温
J·A·德鲁
S·卡希伯哈特拉
蒋松春
张红
C·普雷曼
V·巴驰沃尔
J·曼弗雷迪
L·博伊特
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Myrexis Inc
Cytovia Therapeutics LLC
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Cytovia Inc
Myriad Pharmaceuticals Inc
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen atoms
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07DHETEROCYCLIC COMPOUNDS
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    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/95Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
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    • 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
    • C07D401/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
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    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
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    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
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    • C07D471/02Heterocyclic 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
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    • C07D487/04Ortho-condensed systems
CN2004800242058A 2003-07-03 2004-07-06 作为天冬氨酸特异性半胱氨酸蛋白酶活化剂和细胞程序死亡诱导剂的4-芳基氨基-喹唑啉 Expired - Fee Related CN1984660B (zh)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US48432503P 2003-07-03 2003-07-03
US60/484,325 2003-07-03
US49300603P 2003-08-07 2003-08-07
US60/493,006 2003-08-07
US55755604P 2004-03-29 2004-03-29
US60/557,556 2004-03-29
US57128804P 2004-05-14 2004-05-14
US60/571,288 2004-05-14
PCT/US2004/021631 WO2005003100A2 (en) 2003-07-03 2004-07-06 4-arylamino-quinazolines as activators of caspases and inducers of apoptosis

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CN1984660A CN1984660A (zh) 2007-06-20
CN1984660B true CN1984660B (zh) 2010-12-15

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Families Citing this family (80)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7344702B2 (en) * 2004-02-13 2008-03-18 Bristol-Myers Squibb Pharma Company Contrast agents for myocardial perfusion imaging
US8309562B2 (en) 2003-07-03 2012-11-13 Myrexis, Inc. Compounds and therapeutical use thereof
CN1984660B (zh) * 2003-07-03 2010-12-15 美瑞德生物工程公司 作为天冬氨酸特异性半胱氨酸蛋白酶活化剂和细胞程序死亡诱导剂的4-芳基氨基-喹唑啉
WO2006074147A2 (en) * 2005-01-03 2006-07-13 Myriad Genetics, Inc. Nitrogen containing bicyclic compounds and therapeutical use thereof
US20050197371A1 (en) 2003-11-13 2005-09-08 Ambit Biosciences Corporation Urea derivatives as PDGFR modulators
MXPA06013256A (es) 2004-05-15 2007-02-08 Vertex Pharma Tratamiento de crisis convulsivas utilizando inhibidores ice.
EP1778221A2 (en) 2004-05-27 2007-05-02 Vertex Pharmaceuticals Incorporated Ice inhibitors for the treatment of autoinflammatory diseases
US20070244114A1 (en) * 2004-07-06 2007-10-18 Myriad Genetics, Incorporated Compounds and therapeutical use thereof
EP1844023A1 (en) * 2004-12-31 2007-10-17 Sk Chemicals Co., Ltd. Quinazoline derivatives for the treatment and prevention of diabetes and obesity
CA2592971A1 (en) * 2005-01-03 2006-07-13 Myriad Genetics Inc. Method of treating brain cancer
US8258145B2 (en) 2005-01-03 2012-09-04 Myrexis, Inc. Method of treating brain cancer
ES2551086T3 (es) * 2005-06-14 2015-11-16 Baylor University Análogos de combretastatina con actividad de unión a tubulina
CN101198312A (zh) * 2005-06-16 2008-06-11 美瑞德生物工程公司 药物组合物及其用途
JP2009501232A (ja) * 2005-07-15 2009-01-15 シェーリング コーポレイション 癌の処置に有用なキナゾリン誘導体
WO2007028162A2 (en) * 2005-09-02 2007-03-08 The University Of Toledo Methods and compositions for identifying biomarkers useful in diagnosis and/or treatment of biological states
WO2007076034A2 (en) * 2005-12-21 2007-07-05 Abbott Laboratories Anti-viral compounds
CN101443334A (zh) * 2005-12-21 2009-05-27 艾博特公司 抗病毒化合物
EP1971611B1 (en) 2005-12-21 2012-10-10 Abbott Laboratories Anti-viral compounds
RU2008144806A (ru) * 2006-04-14 2010-05-20 Астразенека Аб (Se) 4-анилинохинолин-3-карбоксамиды в качестве ингибиторов csf-1r киназы
EP2079739A2 (en) * 2006-10-04 2009-07-22 Pfizer Products Inc. Pyrido[4,3-d]pyrimidin-4(3h)-one derivatives as calcium receptor antagonists
US8236950B2 (en) 2006-12-20 2012-08-07 Abbott Laboratories Anti-viral compounds
CN101742910A (zh) * 2007-04-10 2010-06-16 美瑞德制药公司 治疗脑癌的方法
WO2008124823A1 (en) * 2007-04-10 2008-10-16 Myriad Genetics, Inc. Method of treating melanoma
AU2008236995A1 (en) * 2007-04-10 2008-10-16 Myrexis, Inc. Dosages and methods for the treatment of cancer
WO2008124828A1 (en) * 2007-04-10 2008-10-16 Myriad Genetics, Inc. Methods for treating vascular disruption disorders
CA2720989A1 (en) * 2007-04-10 2008-10-16 Myrexis, Inc. Methods for treating cancer
WO2008157500A1 (en) * 2007-06-17 2008-12-24 Kalypsys, Inc. Aminoquinazoline cannabinoid receptor modulators for treatment of disease
JP2010530872A (ja) * 2007-06-22 2010-09-16 サイドース・エルエルシー Tween80を含まないドセタキセル可溶化製剤
CN102088854A (zh) * 2008-07-11 2011-06-08 美瑞德生物工程公司 作为细胞毒素剂的药物化合物及其使用方法
US20100068197A1 (en) * 2008-07-11 2010-03-18 Myriad Pharmaceuticals, Inc. Pharmaceutical compounds as inhibitors of cell proliferation and the use thereof
CN101463014B (zh) * 2008-12-26 2013-07-10 复旦大学 二芳基苯并嘧啶类衍生物及其药物组合物和用途
AU2010230585B2 (en) 2009-04-02 2016-03-24 Merck Patent Gmbh Autotaxin inhibitors
WO2011028741A1 (en) 2009-09-03 2011-03-10 Bristol-Myers Squibb Company Quinazolines as potassium ion channel inhibitors
US8912228B2 (en) 2009-10-19 2014-12-16 Scidose Llc Docetaxel formulations with lipoic acid
US20110092579A1 (en) * 2009-10-19 2011-04-21 Scidose Llc Solubilized formulation of docetaxel
US8541465B2 (en) * 2009-10-19 2013-09-24 Scidose, Llc Docetaxel formulations with lipoic acid and/or dihydrolipoic acid
US7772274B1 (en) 2009-10-19 2010-08-10 Scidose, Llc Docetaxel formulations with lipoic acid
CN101716351B (zh) * 2009-12-08 2012-04-11 中国人民解放军军事医学科学院野战输血研究所 一类吡啶化合物在制备rna干涉增强剂中的应用
US20110224240A1 (en) * 2010-01-11 2011-09-15 Myrexis, Inc. Methods of treating cancer and related diseases
ES2651466T3 (es) 2010-02-08 2018-01-26 Lantheus Medical Imaging, Inc. Métodos para sintetizar agentes de formación de imágenes e intermediarios del mismo
WO2011151423A1 (en) 2010-06-04 2011-12-08 Exonhit S.A. Substituted isoquinolines and their use as tubulin polymerization inhibitors
EP2635906A4 (en) 2010-11-05 2014-04-02 Univ Brandeis ICE INHIBITING COMPOUNDS AND USES THEREOF
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
US9139590B2 (en) * 2011-02-04 2015-09-22 Duquesne University Of The Holy Spirit Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity and methods of treating a patient
CA2829131C (en) * 2011-03-04 2018-11-20 Glaxosmithkline Intellectual Property (No.2) Limited Amino-quinolines as kinase inhibitors
TWI547494B (zh) 2011-08-18 2016-09-01 葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之胺基喹唑啉類
BR112014030812B1 (pt) 2012-06-13 2022-11-08 Incyte Holdings Corporation Compostos tricíclicos substituídos como inibidores de fgfr, seus usos, composição farmacêutica e método para inibir uma enzima fgfr
AU2013203000B9 (en) 2012-08-10 2017-02-02 Lantheus Medical Imaging, Inc. Compositions, methods, and systems for the synthesis and use of imaging agents
AR092529A1 (es) 2012-09-13 2015-04-22 Glaxosmithkline Llc Compuesto de aminoquinazolina, composicion farmaceutica que lo comprende y uso de dicho compuesto para la preparacion de un medicamento
AR092530A1 (es) 2012-09-13 2015-04-22 Glaxosmithkline Llc Compuesto de amino-quinolina, composicion farmaceutica que lo comprende y uso de dicho compuesto para la preparacion de un medicamento
ES2654100T3 (es) 2013-02-21 2018-02-12 Glaxosmithkline Intellectual Property Development Limited Quinazolinas como inhibidores de quinasa
EP2769723A1 (en) 2013-02-22 2014-08-27 Ruprecht-Karls-Universität Heidelberg Compounds for use in inhibiting HIV capsid assembly
EP2769722A1 (en) 2013-02-22 2014-08-27 Ruprecht-Karls-Universität Heidelberg Compounds for use in inhibiting HIV capsid assembly
SG10201708520YA (en) 2013-04-19 2017-12-28 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
CN104130200B (zh) * 2014-07-01 2016-04-20 中山大学 一种2-取代苯基-4-芳胺基喹唑啉衍生物及其制备方法和应用
US10851105B2 (en) 2014-10-22 2020-12-01 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
AU2016219822B2 (en) 2015-02-20 2020-07-09 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
CA2981886A1 (en) 2015-04-16 2016-10-20 Icahn School Of Medicine At Mount Sinai Ksr antagonists
CA3033752C (en) 2016-08-15 2022-05-31 Purdue Research Foundation 4-substituted aminoisoquinoline derivatives
CN106380465B (zh) * 2016-09-05 2019-03-12 郑州大学 含1,2,3-三氮唑结构单元的2,4-二取代喹唑啉类化合物及其制备方法和用途
CN108239071B (zh) * 2016-12-27 2020-12-04 沈阳药科大学 酰胺及硫代酰胺类衍生物及其制备方法和应用
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
CA3068146A1 (en) * 2017-06-30 2019-01-03 The University Of North Carolina At Chapel Hill Heterochromatin gene repression inhibitors
SG11202010882XA (en) 2018-05-04 2020-11-27 Incyte Corp Salts of an fgfr inhibitor
KR20210018265A (ko) 2018-05-04 2021-02-17 인사이트 코포레이션 Fgfr 억제제의 고체 형태 및 이의 제조 방법
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
JP2022552324A (ja) 2019-10-14 2022-12-15 インサイト・コーポレイション Fgfr阻害剤としての二環式複素環
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
EP4069695A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Derivatives of an fgfr inhibitor
WO2021257863A1 (en) 2020-06-19 2021-12-23 Incyte Corporation Pyrrolotriazine compounds as jak2 v617f inhibitors
WO2021257857A1 (en) 2020-06-19 2021-12-23 Incyte Corporation Naphthyridinone compounds as jak2 v617f inhibitors
CR20230057A (es) 2020-07-02 2023-08-15 Incyte Corp Compuestos tríciclicos de urea como inhibidores de jak2 v617f
WO2022006456A1 (en) 2020-07-02 2022-01-06 Incyte Corporation Tricyclic pyridone compounds as jak2 v617f inhibitors
WO2022046989A1 (en) 2020-08-27 2022-03-03 Incyte Corporation Tricyclic urea compounds as jak2 v617f inhibitors
US11919908B2 (en) 2020-12-21 2024-03-05 Incyte Corporation Substituted pyrrolo[2,3-d]pyrimidine compounds as JAK2 V617F inhibitors
AR126102A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
CN114436975B (zh) * 2022-01-26 2023-10-31 贵州省中国科学院天然产物化学重点实验室(贵州医科大学天然产物化学重点实验室) 2-三氟甲基-4-氨基喹唑啉类化合物及其应用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2052481A (en) * 1979-05-09 1981-01-28 Hoechst Ag 4-Substituted 5,6,7,8- tetrahydroquinolines, their preparation and use
US4322420A (en) * 1978-09-11 1982-03-30 Sankyo Company Limited Method of using 4-anilinoquinazoline derivatives as analgesic and anti-inflammatory agents
US5480883A (en) * 1991-05-10 1996-01-02 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase

Family Cites Families (108)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2883382A (en) 1957-08-29 1959-04-21 Parke Davis & Co Benzo-quinolylamino-2-[di(beta-chloroethyl)aminomethyl]-phenols
US3031450A (en) 1959-04-30 1962-04-24 Thomae Gmbh Dr K Substituted pyrimido-[5, 4-d]-pyrimidines
CH421972A (de) 1960-02-02 1966-10-15 Thomae Gmbh Dr K Verfahren zur Herstellung von basisch substituierten Pyrimidincarbonsäuren-(4) bzw. ihren Derivaten
US3502681A (en) 1968-04-10 1970-03-24 Roussel Uclaf 7- or 8-chloro-4-phenylamino-chloroquinolines
FR8491M (US20070244113A1-20071018-C00053.png) 1968-12-31 1973-07-27
BE754586A (fr) 1969-08-08 1971-02-08 Upjohn Co Preparations pharmaceutiques a base de p-(4-quinolylamino) benzamide etleur utilisation
US3971783A (en) 1973-03-07 1976-07-27 Pfizer Inc. 4-Aminoquinazoline derivatives as cardiac stimulants
US4025629A (en) 1974-01-07 1977-05-24 The Upjohn Company P-(trifluoromethylquinolylamino)benzamides, pharmaceutical dosage forms and method of treatment
FI70036C (fi) 1980-01-31 1986-09-12 Ciba Geigy Ag Kromogena kinazolinfoereningar
NZ197420A (en) 1980-07-01 1984-04-27 Ici Australia Ltd -(quinazolin-(2-or 4-)(oxy,ylthio or amino)phen(oxy or ylthio)alkanoic acid derivatives
US4510307A (en) 1980-08-20 1985-04-09 Asahi Kasei Kogyo Kabushiki Kaisha 6-Quinazolinesulfonyl derivatives and process for preparation thereof
DE3049207A1 (de) 1980-12-27 1982-07-29 Dr. Karl Thomae Gmbh, 7950 Biberach Neue trisubstituierte pyrimido (5,4-d) pyrimidine, ihre herstellung und ihre verwendung als arzneimittel
FR2498187A1 (fr) 1981-01-16 1982-07-23 Rhone Poulenc Sante Procede de preparation d'amino-4 chloro-7 quinoleines
DE3423092A1 (de) 1984-06-22 1986-01-02 Dr. Karl Thomae Gmbh, 7950 Biberach Neue 8-alkylthio-2-piperazino-pyrimido(5,4-d) pyrimidine, ihre herstellung und diese verbindungen enthaltende arzneimittel
IL88507A (en) * 1987-12-03 1993-02-21 Smithkline Beckman Intercredit 2,4-diaminoquinazolines, process for their preparation and pharmaceutical compositions comprising them
US5294622A (en) 1988-01-29 1994-03-15 Dowelanco Substituted quinolines and cinnolines
US5114939A (en) 1988-01-29 1992-05-19 Dowelanco Substituted quinolines and cinnolines as fungicides
IL89029A (en) 1988-01-29 1993-01-31 Lilly Co Eli Fungicidal quinoline and cinnoline derivatives, compositions containing them, and fungicidal methods of using them
IE63502B1 (en) * 1989-04-21 1995-05-03 Zeneca Ltd Aminopyrimidine derivatives useful for treating cardiovascular disorders
GB8910722D0 (en) 1989-05-10 1989-06-28 Smithkline Beckman Intercredit Compounds
CA2015981A1 (en) * 1989-05-10 1990-11-10 Thomas H. Brown Compounds
GB9008818D0 (en) 1990-04-19 1990-06-13 Ici Plc Amine derivatives
DE4029648A1 (de) * 1990-09-19 1992-03-26 Hoechst Ag 4-anilino-pyrimidine, verfahren zu ihrer herstellung, sie enthaltende mittel und ihre verwendung als fungizide
HUT64755A (en) * 1991-02-20 1994-02-28 Pfizer Process for the production of 2,4-diamino-quinazoline derivatives and of medical preparatives containing them
US5710158A (en) 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5721237A (en) 1991-05-10 1998-02-24 Rhone-Poulenc Rorer Pharmaceuticals Inc. Protein tyrosine kinase aryl and heteroaryl quinazoline compounds having selective inhibition of HER-2 autophosphorylation properties
ATE159009T1 (de) 1991-05-10 1997-10-15 Rhone Poulenc Rorer Int Bis mono- und bicyclische aryl- und heteroarylderivate mit inhibierender wirkung auf die egf und/oder pdgf-rezeptor tyrosinkinase
US6645969B1 (en) * 1991-05-10 2003-11-11 Aventis Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase
US5714493A (en) 1991-05-10 1998-02-03 Rhone-Poulenc Rorer Pharmaceuticals, Inc. Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase
USRE37650E1 (en) 1991-05-10 2002-04-09 Aventis Pharmacetical Products, Inc. Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase
DE4116785A1 (de) 1991-05-23 1992-11-26 Basf Ag Phenylazo- oder naphthylazobenzole mit mehreren reaktiven ankern
US5236925A (en) 1991-10-24 1993-08-17 American Home Products Corporation Fused pyrimidines as angiotensin II antagonists
US5187168A (en) 1991-10-24 1993-02-16 American Home Products Corporation Substituted quinazolines as angiotensin II antagonists
US5256781A (en) 1991-10-24 1993-10-26 American Home Products Corporation Substituted quinazolines as angiotensin II antagonists
US5330989A (en) 1991-10-24 1994-07-19 American Home Products Corporation Heterocycles substituted with biphenyl-3-cyclobutene-1,2-dione derivatives
GB9127252D0 (en) 1991-12-23 1992-02-19 Boots Co Plc Therapeutic agents
TW215434B (US20070244113A1-20071018-C00053.png) 1992-03-07 1993-11-01 Hoechst Ag
US5270466A (en) 1992-06-11 1993-12-14 American Cyanamid Company Substituted quinazoline fungicidal agents
JP2657760B2 (ja) 1992-07-15 1997-09-24 小野薬品工業株式会社 4−アミノキナゾリン誘導体およびそれを含有する医薬品
US5565472A (en) 1992-12-21 1996-10-15 Pfizer Inc. 4-aryl-3-(heteroarylureido)-1,2-dihydro-2-oxo-quinoline derivatives as antihypercholesterolemic and antiatherosclerotic agents
US5618829A (en) 1993-01-28 1997-04-08 Mitsubishi Chemical Corporation Tyrosine kinase inhibitors and benzoylacrylamide derivatives
DK60593D0 (da) 1993-05-26 1993-05-26 Novo Nordisk As Kemiske forbindelser, deres fremstilling og anvendelse
US6087160A (en) 1993-06-24 2000-07-11 The General Hospital Corporation Programmed cell death genes and proteins
DE4325900A1 (de) 1993-08-02 1995-02-09 Thomae Gmbh Dr K Trisubstituierte Pyrimido [5,4-d] pyrimidine zur Modulation der Multidrugresistenz, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
US5656643A (en) 1993-11-08 1997-08-12 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
IL112249A (en) * 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
US5654307A (en) 1994-01-25 1997-08-05 Warner-Lambert Company Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
CN1176918C (zh) 1994-04-06 2004-11-24 盐野义制药株式会社 具有农用杀菌活性的新型α-取代苯乙酸衍生物的中间体
US6313150B1 (en) 1994-04-06 2001-11-06 Shionogi & Co., Ltd. α-substituted phenylacetic acid derivative, its production and agricultural fungicide containing it
TW414798B (en) 1994-09-07 2000-12-11 Thomae Gmbh Dr K Pyrimido (5,4-d) pyrimidines, medicaments comprising these compounds, their use and processes for their preparation
CA2202985A1 (en) 1994-11-08 1996-05-17 Haruhiko Makino Thienopyridine or thienopyrimidine derivatives and their use
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US6232312B1 (en) 1995-06-07 2001-05-15 Cell Pathways, Inc. Method for treating patient having precancerous lesions with a combination of pyrimidopyrimidine derivatives and esters and amides of substituted indenyl acetic acides
DE69625709D1 (de) 1995-09-29 2003-02-13 Shionogi & Co Alpha-substituierte heterozyklische benzylderivate, zwischenverbindungen zu ihrer herstellung und pestizide die diese als aktiver bestandteil enthalten
JP3370340B2 (ja) 1996-04-12 2003-01-27 ワーナー―ランバート・コンパニー チロシンキナーゼの不可逆的阻害剤
PT907650E (pt) 1996-06-27 2003-04-30 Janssen Pharmaceutica Nv N-¬4-(heteroarilmetil)fenil|heteroarilaminasc
ATE227283T1 (de) 1996-07-13 2002-11-15 Glaxo Group Ltd Kondensierte heterozyklische verbindungen als protein kinase inhibitoren
US5874738A (en) * 1996-07-16 1999-02-23 Saint-Gobain Industrial Ceramics, Inc. Scintillation crystal modules and methods of making the same
CA2262692C (en) 1996-08-06 2002-06-11 Pfizer Inc. Substituted pyrido- or pyrimido-containing 6,6- or 6,7-bicyclic derivatives
US5874438A (en) 1996-10-11 1999-02-23 Bayer Aktiengesellschaft 2,2'-bridged bis-2,4-diaminoquinazolines
US5760230A (en) 1996-10-11 1998-06-02 Bayer Aktiengesellschaft 4, 4'-bridged bis-2, 4-diaminoquinazolines
ATE284692T1 (de) 1996-10-14 2005-01-15 Aventis Pharma Gmbh Verwendung von nicht-peptidischen bradykinin- antagonisten zur herstellung von arzneimitteln zur behandlung und prävention der alzheimerischen krankheit
US5739127A (en) 1996-11-08 1998-04-14 Bayer Aktiengesellschaft 2,4'-bridged bis-2,4-diaminoquinazolines
DE69726182T2 (de) * 1996-12-11 2004-08-12 Dana-Farber Cancer Institute, Inc., Boston Methoden und pharmazeutische zusammenstellungen zur wachstumsverhinderung von tumorzellen enthaltend einen ppar-gamma agonisten und einen map kinase inhibitor
US6552055B2 (en) * 1996-12-11 2003-04-22 Dana-Farber Cancer Institute Methods and pharmaceutical compositions for inhibiting tumor cell growth
US6002008A (en) 1997-04-03 1999-12-14 American Cyanamid Company Substituted 3-cyano quinolines
AR012634A1 (es) 1997-05-02 2000-11-08 Sugen Inc Compuesto basado en quinazolina, composicion famaceutica que lo comprende, metodo para sintetizarlo, su uso, metodos de modulacion de la funcion deserina/treonina proteinaquinasa con dicho compuesto y metodo in vitro para identificar compuestos que modulan dicha funcion
ZA986732B (en) 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitiors of tyrosine kinases
US6251912B1 (en) 1997-08-01 2001-06-26 American Cyanamid Company Substituted quinazoline derivatives
WO1999009986A1 (fr) * 1997-08-22 1999-03-04 Kyowa Hakko Kogyo Co., Ltd. Derives de 4-aminoquinazoline
WO1999018856A1 (en) 1997-10-10 1999-04-22 Cytovia, Inc. Novel fluorescent reporter molecules and their applications including assays for caspases
US6242196B1 (en) 1997-12-11 2001-06-05 Dana-Farber Cancer Institute Methods and pharmaceutical compositions for inhibiting tumor cell growth
EP1037629B1 (en) 1997-12-19 2004-10-27 Janssen Pharmaceutica N.V. Combination of a retinoic acid metabolism blocking agent and a tocophereol
US20020025968A1 (en) * 1998-04-15 2002-02-28 Rifat Pamukcu Method for inhibiting neoplastic cells and related conditions by exposure to 4-aminoquinazoline derivatives
CA2333392A1 (en) 1998-05-28 1999-12-02 Parker Hughes Institute Quinazolines for treating brain tumor
US6800649B1 (en) * 1998-06-30 2004-10-05 Parker Hughes Institute Method for inhibiting c-jun expression using JAK-3 inhibitors
KR20010089171A (ko) 1998-08-21 2001-09-29 추후제출 퀴나졸린 유도체
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
US6297258B1 (en) 1998-09-29 2001-10-02 American Cyanamid Company Substituted 3-cyanoquinolines
IL143094A0 (en) * 1998-12-02 2002-04-21 Pfizer Prod Inc METHODS AND COMPOSITIONS FOR RESTORING CONFORMATIONAL STABILITY OF A PROTEIN OF THE p53 FAMILY
UA71945C2 (en) 1999-01-27 2005-01-17 Pfizer Prod Inc Substituted bicyclic derivatives being used as anticancer agents
US6080747A (en) 1999-03-05 2000-06-27 Hughes Institute JAK-3 inhibitors for treating allergic disorders
YU13200A (sh) 1999-03-31 2002-10-18 Pfizer Products Inc. Postupci i intermedijeri za dobijanje anti-kancernih jedinjenja
US6518283B1 (en) 1999-05-28 2003-02-11 Celltech R&D Limited Squaric acid derivatives
US6432979B1 (en) 1999-08-12 2002-08-13 American Cyanamid Company Method of treating or inhibiting colonic polyps and colorectal cancer
US20030149045A1 (en) * 1999-08-20 2003-08-07 Fatih M Uckun Therapeutic compounds
US7087613B2 (en) * 1999-11-11 2006-08-08 Osi Pharmaceuticals, Inc. Treating abnormal cell growth with a stable polymorph of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride
US6384051B1 (en) 2000-03-13 2002-05-07 American Cyanamid Company Method of treating or inhibiting colonic polyps
BR0111548A (pt) * 2000-06-22 2003-05-06 Pfizer Prod Inc Derivados bicìclicos substituìdos para o tratamento de crescimento de célula anormal
US6740651B2 (en) * 2000-08-26 2004-05-25 Boehringer Ingelheim Pharma Kg Aminoquinazolines which inhibit signal transduction mediated by tyrosine kinases
US20020082270A1 (en) * 2000-08-26 2002-06-27 Frank Himmelsbach Aminoquinazolines which inhibit signal transduction mediated by tyrosine kinases
ATE383860T1 (de) * 2000-11-02 2008-02-15 Nippon Shinyaku Co Ltd Chinazolinderivate und -arzneimittel
US20040034045A1 (en) * 2000-11-29 2004-02-19 Parker Hughes Institute Inhibitors of thrombin induced platelet aggregation
EP1351691A4 (en) * 2000-12-12 2005-06-22 Cytovia Inc SUBSTITUTED 2-ARYL-4-ARYLAMINOPYRIMIDINES AND ANALOGUES AS ACTIVATORS OF CASPASES AND APOPTOSIS INDUCERS, AND USE THEREOF
ES2272567T3 (es) * 2000-12-21 2007-05-01 Vertex Pharmaceuticals Incorporated Compuestos de pirazol utiles como inhibidores de proteina quinasas.
US20030134836A1 (en) * 2001-01-12 2003-07-17 Amgen Inc. Substituted arylamine derivatives and methods of use
DE60239097D1 (de) * 2001-03-02 2011-03-17 Gpc Biotech Ag Drei-hybrid-assaysystem
US6562319B2 (en) * 2001-03-12 2003-05-13 Yissum Research Development Company Of The Hebrew University Of Jerusalem Radiolabeled irreversible inhibitors of epidermal growth factor receptor tyrosine kinase and their use in radioimaging and radiotherapy
US6887873B2 (en) * 2001-03-23 2005-05-03 Aventis Pharma S.A. Triazine derivatives and their application as antitelomerase agents
US6864255B2 (en) * 2001-04-11 2005-03-08 Amgen Inc. Substituted triazinyl amide derivatives and methods of use
US6883375B2 (en) * 2001-06-29 2005-04-26 Harold L. Dunegan Detection of movement of termites in wood by acoustic emission techniques
AU2002337428A1 (en) * 2001-11-30 2003-06-10 Pfizer Products Inc. Processes for the preparation of substituted bicyclic derivatives for the treatment of abnormal cell growth
DE10204462A1 (de) * 2002-02-05 2003-08-07 Boehringer Ingelheim Pharma Verwendung von Tyrosinkinase-Inhibitoren zur Behandlung inflammatorischer Prozesse
WO2003097615A1 (en) * 2002-05-17 2003-11-27 Scios, Inc. TREATMENT OF FIBROPROLIFERATIVE DISORDERS USING TGF-β INHIBITORS
WO2004078114A2 (en) * 2003-02-28 2004-09-16 Encysive Pharmaceuticals Inc. Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-ii receptor antagonists.
CN1984660B (zh) * 2003-07-03 2010-12-15 美瑞德生物工程公司 作为天冬氨酸特异性半胱氨酸蛋白酶活化剂和细胞程序死亡诱导剂的4-芳基氨基-喹唑啉
WO2006074147A2 (en) * 2005-01-03 2006-07-13 Myriad Genetics, Inc. Nitrogen containing bicyclic compounds and therapeutical use thereof
US7326712B2 (en) * 2003-10-14 2008-02-05 Arizona Board Of Regents On Behalf Of The University Of Arizona Substituted tricyclic compounds as protein kinase inhibitors

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4322420A (en) * 1978-09-11 1982-03-30 Sankyo Company Limited Method of using 4-anilinoquinazoline derivatives as analgesic and anti-inflammatory agents
GB2052481A (en) * 1979-05-09 1981-01-28 Hoechst Ag 4-Substituted 5,6,7,8- tetrahydroquinolines, their preparation and use
US5480883A (en) * 1991-05-10 1996-01-02 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase

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