US20070244113A1 - Compounds and therapeutical use thereof - Google Patents

Compounds and therapeutical use thereof Download PDF

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Publication number
US20070244113A1
US20070244113A1 US11/680,843 US68084307A US2007244113A1 US 20070244113 A1 US20070244113 A1 US 20070244113A1 US 68084307 A US68084307 A US 68084307A US 2007244113 A1 US2007244113 A1 US 2007244113A1
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US
United States
Prior art keywords
alkyl
methyl
independently
halo
amine
Prior art date
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Abandoned
Application number
US11/680,843
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English (en)
Inventor
Sui Cai
Nilantha Sirisoma
Azra Pervin
John Drewe
Shailaja Kasibhatla
Songchun Jiang
Hong Zhang
Chris Pleiman
Vijay Baichwal
John Manfredi
Leena Bhoite
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Myrexis Inc
Cytovia Therapeutics LLC
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Myriad Genetics Inc
Cytovia Inc
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Application filed by Myriad Genetics Inc, Cytovia Inc filed Critical Myriad Genetics Inc
Priority to US11/680,843 priority Critical patent/US20070244113A1/en
Publication of US20070244113A1 publication Critical patent/US20070244113A1/en
Assigned to MYRIAD PHARMACEUTICALS, INC. reassignment MYRIAD PHARMACEUTICALS, INC. ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: MYRIAD GENETICS, INC.
Abandoned legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D239/95Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • 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
    • C07D403/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • 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
    • C07D403/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • C07D405/02Heterocyclic 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 containing two hetero rings
    • C07D405/12Heterocyclic 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 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32Nitrogen atom
    • C07D473/34Nitrogen atom attached in position 6, e.g. adenine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
US11/680,843 2003-07-03 2007-03-01 Compounds and therapeutical use thereof Abandoned US20070244113A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
US11/680,843 US20070244113A1 (en) 2003-07-03 2007-03-01 Compounds and therapeutical use thereof

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US48432503P 2003-07-03 2003-07-03
US49300603P 2003-08-07 2003-08-07
US55755604P 2004-03-29 2004-03-29
US57128804P 2004-05-14 2004-05-14
US10/885,903 US7618975B2 (en) 2003-07-03 2004-07-06 4-arylamino-quinazolines and analogs as activators of caspases and inducers of apoptosis and the use thereof
US11/680,843 US20070244113A1 (en) 2003-07-03 2007-03-01 Compounds and therapeutical use thereof

Related Parent Applications (1)

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US10/885,903 Continuation US7618975B2 (en) 2003-07-03 2004-07-06 4-arylamino-quinazolines and analogs as activators of caspases and inducers of apoptosis and the use thereof

Publications (1)

Publication Number Publication Date
US20070244113A1 true US20070244113A1 (en) 2007-10-18

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Family Applications (7)

Application Number Title Priority Date Filing Date
US10/885,903 Expired - Fee Related US7618975B2 (en) 2003-07-03 2004-07-06 4-arylamino-quinazolines and analogs as activators of caspases and inducers of apoptosis and the use thereof
US11/620,498 Abandoned US20070208044A1 (en) 2003-07-03 2007-01-05 Compounds and therapeutical use thereof
US11/680,843 Abandoned US20070244113A1 (en) 2003-07-03 2007-03-01 Compounds and therapeutical use thereof
US11/693,432 Abandoned US20070249601A1 (en) 2003-07-03 2007-03-29 Compounds and therapeutical use thereof
US11/779,086 Abandoned US20080032974A1 (en) 2003-07-03 2007-07-17 Compounds and therapeutical use thereof
US11/781,660 Abandoned US20080039479A1 (en) 2003-07-03 2007-07-23 Compounds and therapeutical use thereof
US15/081,530 Abandoned US20170050937A1 (en) 2003-07-03 2016-03-25 Compounds and therapeutical use thereof

Family Applications Before (2)

Application Number Title Priority Date Filing Date
US10/885,903 Expired - Fee Related US7618975B2 (en) 2003-07-03 2004-07-06 4-arylamino-quinazolines and analogs as activators of caspases and inducers of apoptosis and the use thereof
US11/620,498 Abandoned US20070208044A1 (en) 2003-07-03 2007-01-05 Compounds and therapeutical use thereof

Family Applications After (4)

Application Number Title Priority Date Filing Date
US11/693,432 Abandoned US20070249601A1 (en) 2003-07-03 2007-03-29 Compounds and therapeutical use thereof
US11/779,086 Abandoned US20080032974A1 (en) 2003-07-03 2007-07-17 Compounds and therapeutical use thereof
US11/781,660 Abandoned US20080039479A1 (en) 2003-07-03 2007-07-23 Compounds and therapeutical use thereof
US15/081,530 Abandoned US20170050937A1 (en) 2003-07-03 2016-03-25 Compounds and therapeutical use thereof

Country Status (9)

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US (7) US7618975B2 (US20070244113A1-20071018-C00204.png)
EP (1) EP1660092A2 (US20070244113A1-20071018-C00204.png)
JP (2) JP5129957B2 (US20070244113A1-20071018-C00204.png)
KR (1) KR101218213B1 (US20070244113A1-20071018-C00204.png)
CN (1) CN1984660B (US20070244113A1-20071018-C00204.png)
AU (1) AU2004253967B2 (US20070244113A1-20071018-C00204.png)
CA (1) CA2531327A1 (US20070244113A1-20071018-C00204.png)
NZ (1) NZ544472A (US20070244113A1-20071018-C00204.png)
WO (1) WO2005003100A2 (US20070244113A1-20071018-C00204.png)

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070244114A1 (en) * 2004-07-06 2007-10-18 Myriad Genetics, Incorporated Compounds and therapeutical use thereof
US20080004297A1 (en) * 2003-07-03 2008-01-03 Myriad Genetics, Inc. Compounds and therapeutical use thereof
US20080032974A1 (en) * 2003-07-03 2008-02-07 Myriad Genetics, Incorporated Compounds and therapeutical use thereof
US20080051398A1 (en) * 2005-01-03 2008-02-28 Myriad Genetics, Inc. Method of treating brain cancer
US20080319048A1 (en) * 2007-06-22 2008-12-25 Scidose Llc Solubilized formulation of docetaxel without tween 80
US7772274B1 (en) 2009-10-19 2010-08-10 Scidose, Llc Docetaxel formulations with lipoic acid
US20110092579A1 (en) * 2009-10-19 2011-04-21 Scidose Llc Solubilized formulation of docetaxel
US20110092580A1 (en) * 2009-10-19 2011-04-21 Scidose Llc Docetaxel formulations with lipoic acid and/or dihydrolipoic acid
US8309562B2 (en) 2003-07-03 2012-11-13 Myrexis, Inc. Compounds and therapeutical use thereof
US8912228B2 (en) 2009-10-19 2014-12-16 Scidose Llc Docetaxel formulations with lipoic acid

Families Citing this family (71)

* 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
AU2005249503B2 (en) 2003-11-10 2011-08-25 Vertex Pharmaceuticals Incorporated ICE inhibitors for the treatment of autoinflammatory diseases
US7750160B2 (en) 2003-11-13 2010-07-06 Ambit Biosciences Corporation Isoxazolyl urea derivatives as kinase modulators
US20060128696A1 (en) 2004-05-15 2006-06-15 Annamaria Vezzani Treating seizures using ice inhibitors
KR20060079121A (ko) * 2004-12-31 2006-07-05 에스케이케미칼주식회사 당뇨 및 비만 치료예방에 유효한 퀴나졸린 유도체
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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
EP1934377B1 (en) * 2005-09-02 2012-03-07 The University of Toledo Methods for identifying biomarkers useful in diagnosis of biological states
WO2007081517A2 (en) 2005-12-21 2007-07-19 Abbott Laboratories Anti-viral compounds
CN101443334A (zh) * 2005-12-21 2009-05-27 艾博特公司 抗病毒化合物
WO2007076034A2 (en) * 2005-12-21 2007-07-05 Abbott Laboratories Anti-viral compounds
PL2010496T3 (pl) * 2006-04-14 2011-01-31 Astrazeneca Ab 4-Anilinochinolino-3-karboksyamidy jako inhibitory kinazy CSF-1R
EP2079739A2 (en) * 2006-10-04 2009-07-22 Pfizer Products Inc. Pyrido[4,3-d]pyrimidin-4(3h)-one derivatives as calcium receptor antagonists
EP2094276A4 (en) 2006-12-20 2011-01-05 Abbott Lab ANTIVIRAL COMPOUNDS
CA2720987A1 (en) * 2007-04-10 2008-10-16 Myrexis, Inc. Dosages and methods for the treatment of cancer
WO2008124826A1 (en) * 2007-04-10 2008-10-16 Myriad Genetics, Inc. Methods for treating cancer
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
WO2008124828A1 (en) * 2007-04-10 2008-10-16 Myriad Genetics, Inc. Methods for treating vascular disruption disorders
US20090209536A1 (en) * 2007-06-17 2009-08-20 Kalypsys, Inc. Aminoquinazoline cannabinoid receptor modulators for treatment of disease
NZ590913A (en) * 2008-07-11 2012-09-28 Myrexis Inc (2-aminomethylquinazolin-4-yl)-(4-methoxyphenyl)methylamine for treating or ameliorating neoplasm or cancer
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
EA201101396A1 (ru) 2009-04-02 2012-09-28 Мерк Патент Гмбх Ингибиторы аутотаксина
CA2772642C (en) 2009-09-03 2017-08-29 Bristol-Myers Squibb Company Quinazolines as potassium ion channel inhibitors
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
CN109200296B (zh) 2010-02-08 2021-12-14 兰休斯医疗成像公司 用于合成显像剂和其中间体的方法和装置
WO2011151423A1 (en) 2010-06-04 2011-12-08 Exonhit S.A. Substituted isoquinolines and their use as tubulin polymerization inhibitors
WO2012061785A2 (en) 2010-11-05 2012-05-10 Brandeis University 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
PT3176170T (pt) 2012-06-13 2019-02-05 Incyte Holdings Corp Compostos tricíclicos substituídos como inibidores de 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
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TW201425307A (zh) 2012-09-13 2014-07-01 Glaxosmithkline Llc 作為激酶抑制劑之胺基-喹啉類
WO2014128622A1 (en) 2013-02-21 2014-08-28 Glaxosmithkline Intellectual Property Development Limited Quinazolines as kinase inhibitors
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EP2769722A1 (en) 2013-02-22 2014-08-27 Ruprecht-Karls-Universität Heidelberg Compounds for use in inhibiting HIV capsid assembly
PE20152033A1 (es) 2013-04-19 2016-01-21 Incyte Holdings Corp Heterociclos bicicliclos como inhibidores de fgfr
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
EP3617205B1 (en) 2015-02-20 2021-08-04 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
EP3283466A4 (en) 2015-04-16 2018-09-12 Icahn School of Medicine at Mount Sinai Ksr antagonists
JP2019527725A (ja) * 2016-08-15 2019-10-03 パデュー リサーチ ファウンデイション 4位置換アミノイソキノリン誘導体
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
WO2019006322A1 (en) * 2017-06-30 2019-01-03 The University Of North Carolina At Chapel Hill HETEROCROMATINE GENE REPRESSION INHIBITORS
CN112867716A (zh) 2018-05-04 2021-05-28 因赛特公司 Fgfr抑制剂的固体形式和其制备方法
CA3099116A1 (en) 2018-05-04 2019-11-07 Incyte Corporation Salts of an fgfr inhibitor
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
JOP20220083A1 (ar) 2019-10-14 2023-01-30 Incyte Corp حلقات غير متجانسة ثنائية الحلقة كمثبطات لـ fgfr
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
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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 (79)

* 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
US3502681A (en) * 1968-04-10 1970-03-24 Roussel Uclaf 7- or 8-chloro-4-phenylamino-chloroquinolines
US3632761A (en) * 1969-08-08 1972-01-04 Upjohn Co Method of obtaining antihypertensive and antianxiety effects
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
US4322420A (en) * 1978-09-11 1982-03-30 Sankyo Company Limited Method of using 4-anilinoquinazoline derivatives as analgesic and anti-inflammatory agents
US4435003A (en) * 1980-01-31 1984-03-06 Ciba-Geigy Corporation Chromogenic quinazolines
US4510307A (en) * 1980-08-20 1985-04-09 Asahi Kasei Kogyo Kabushiki Kaisha 6-Quinazolinesulfonyl derivatives and process for preparation thereof
US4675047A (en) * 1980-07-01 1987-06-23 Alexander Serban Substituted phenylamine- and phenyloxy-quinazolines as herbicides
US5114939A (en) * 1988-01-29 1992-05-19 Dowelanco Substituted quinolines and cinnolines as fungicides
US5145843A (en) * 1988-01-29 1992-09-08 Dowelanco Quinoline and cinnoline fungicides
US5187168A (en) * 1991-10-24 1993-02-16 American Home Products Corporation Substituted quinazolines as angiotensin II antagonists
US5223505A (en) * 1989-04-21 1993-06-29 Imperial Chemical Industries Plc Pyrimidine derivatives
US5236925A (en) * 1991-10-24 1993-08-17 American Home Products Corporation Fused pyrimidines as angiotensin II antagonists
US5276148A (en) * 1991-05-23 1994-01-04 Basf Aktiengesellschaft Phenylazobenzenes or naphthylazobenzenes having a plurality of fiber-reactive groups
US5294622A (en) * 1988-01-29 1994-03-15 Dowelanco Substituted quinolines and cinnolines
US5330989A (en) * 1991-10-24 1994-07-19 American Home Products Corporation Heterocycles substituted with biphenyl-3-cyclobutene-1,2-dione derivatives
US5409930A (en) * 1991-05-10 1995-04-25 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5436233A (en) * 1992-07-15 1995-07-25 Ono Pharmaceutical Co., Ltd. 4-aminoquinazoline derivatives
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
US5604251A (en) * 1992-03-07 1997-02-18 Hoechst Aktiengesellschaft Imidazole derivatives with a biphenylsulfonylurea or biphenylsulfonylurethane side chain and their use as angitensin II receptors
US5618829A (en) * 1993-01-28 1997-04-08 Mitsubishi Chemical Corporation Tyrosine kinase inhibitors and benzoylacrylamide derivatives
US5618814A (en) * 1993-08-02 1997-04-08 Dr. Karl Thomae Gmbh Trisubstituted pyrimido [5,4-d] pyrimidines for modulating multi-drug resistance and pharmaceutical compositions containing these 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
US5654298A (en) * 1990-04-19 1997-08-05 Imperial Chemical Industries Amine derivatives
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
US5707989A (en) * 1994-09-07 1998-01-13 Dr. Karl Thomae Gmbh Pyrimido 5,4-D!pyrimidines, medicaments comprising these compounds, their use and processes for their preparation
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
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
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
US5739127A (en) * 1996-11-08 1998-04-14 Bayer Aktiengesellschaft 2,4'-bridged bis-2,4-diaminoquinazolines
US5747498A (en) * 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5747486A (en) * 1994-11-08 1998-05-05 Takeda Chemical Industries Thienopyridine or thienopyrimidine derivatives and their use
US5760230A (en) * 1996-10-11 1998-06-02 Bayer Aktiengesellschaft 4, 4'-bridged bis-2, 4-diaminoquinazolines
US5874438A (en) * 1996-10-11 1999-02-23 Bayer Aktiengesellschaft 2,2'-bridged bis-2,4-diaminoquinazolines
US5948819A (en) * 1994-04-06 1999-09-07 Shionogi & Co., Ltd α-substituted phenylacetic acid derivative, its production and agricultural fungicide containing it
US5952346A (en) * 1996-10-14 1999-09-14 Hoechst Marion Roussel Deutschland Gmbh Use of non-peptide bradykinin antagonists for the treatment or prevention of Alzheimer's disease
US6080748A (en) * 1999-03-05 2000-06-27 Parker Hughes Institute Therapeutic use of JAK-3 inhibitors
US6084095A (en) * 1994-01-25 2000-07-04 Warner-Lambert Company Substituted pyrido[3,2-d]pyrimidines capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
US6124330A (en) * 1996-06-27 2000-09-26 Janssen-Cilag S.A. N-[4-(Heteroarylmethyl)phenyl]-heteroarylamines
US6184226B1 (en) * 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
US6204267B1 (en) * 1997-05-02 2001-03-20 Sugen, Inc. Methods of modulating serine/thereonine protein kinase function with quinazoline-based compounds
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
US6242196B1 (en) * 1997-12-11 2001-06-05 Dana-Farber Cancer Institute Methods and pharmaceutical compositions for inhibiting tumor cell growth
US6251912B1 (en) * 1997-08-01 2001-06-26 American Cyanamid Company Substituted quinazoline derivatives
US6265425B1 (en) * 1997-12-19 2001-07-24 Janssen Pharmaceutica, N.V. Combination of a RAMBA and a tocopherol
US6284764B1 (en) * 1999-01-27 2001-09-04 Pfizer Inc. Substituted bicyclic derivatives useful as anticancer agents
US6344459B1 (en) * 1996-04-12 2002-02-05 Warner-Lambert Company Irreversible inhibitors of tyrosine kinases
USRE37650E1 (en) * 1991-05-10 2002-04-09 Aventis Pharmacetical Products, Inc. Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase
US20020048271A1 (en) * 1998-12-02 2002-04-25 Farzan Rastinejad Methods and composition for restoring conformational stability of a protein of the p53 family
US6384051B1 (en) * 2000-03-13 2002-05-07 American Cyanamid Company Method of treating or inhibiting colonic polyps
US6391874B1 (en) * 1996-07-13 2002-05-21 Smithkline Beecham Corporation Fused heterocyclic compounds as protein tyrosine kinase inhibitors
US20020082270A1 (en) * 2000-08-26 2002-06-27 Frank Himmelsbach Aminoquinazolines which inhibit signal transduction mediated by tyrosine kinases
US6432979B1 (en) * 1999-08-12 2002-08-13 American Cyanamid Company Method of treating or inhibiting colonic polyps and colorectal cancer
US6518283B1 (en) * 1999-05-28 2003-02-11 Celltech R&D Limited Squaric acid derivatives
US20030055068A1 (en) * 2000-12-21 2003-03-20 David Bebbington Pyrazole compounds useful as protein kinase inhibitors
US6552027B2 (en) * 1998-05-28 2003-04-22 Parker Hughes Institute Quinazolines for treating brain tumor
US6552055B2 (en) * 1996-12-11 2003-04-22 Dana-Farber Cancer Institute Methods and pharmaceutical compositions for inhibiting tumor cell growth
US20030087931A1 (en) * 2001-03-23 2003-05-08 Patrick Mailliet Chemical derivatives and their application as antitelomerease agent
US20030087908A1 (en) * 2001-04-11 2003-05-08 Geuns-Meyer Stephanie D. Substituted triazinyl amide derivatives and methods of use
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
US6562818B1 (en) * 1997-07-29 2003-05-13 Warner-Lambert Company Irreversible inhibitors of tyrosine kinases
US20030134836A1 (en) * 2001-01-12 2003-07-17 Amgen Inc. Substituted arylamine derivatives and methods of use
US20030144330A1 (en) * 1996-12-11 2003-07-31 Spiegelman Bruce M. Methods and pharmaceutical compositions for inhibiting tumor cell growth
US20030144506A1 (en) * 2001-11-30 2003-07-31 Pfizer Inc. Processes for the preparation of substituted bicyclic derivatives for the treatment of abnormal cell growth
US20030144178A1 (en) * 1998-06-30 2003-07-31 Parker Hughes Institute Method for inhibiting C-jun expression using JAK-3 inhibitors
US20030149045A1 (en) * 1999-08-20 2003-08-07 Fatih M Uckun Therapeutic compounds
US20030149062A1 (en) * 2002-02-05 2003-08-07 Boehringer Ingelheim Pharma Gmbh & Co. Kg Use of tyrosine kinase inhibitors for the treatment of inflammatory processes
US20040014774A1 (en) * 1991-05-10 2004-01-22 Myers Michael R. Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase
US20040034045A1 (en) * 2000-11-29 2004-02-19 Parker Hughes Institute Inhibitors of thrombin induced platelet aggregation
US20040034044A1 (en) * 2000-11-02 2004-02-19 Masahiko Okano Quinazoline derivatives and drugs
US20040038856A1 (en) * 2002-05-17 2004-02-26 Sarvajit Chakravarty Treatment of fibroproliferative disorders using TGF-beta inhibitors
US20040043388A1 (en) * 2001-03-02 2004-03-04 Come Jon H. Three hybrid assay system
US6740651B2 (en) * 2000-08-26 2004-05-25 Boehringer Ingelheim Pharma Kg Aminoquinazolines which inhibit signal transduction mediated by tyrosine kinases
US6883375B2 (en) * 2001-06-29 2005-04-26 Harold L. Dunegan Detection of movement of termites in wood by acoustic emission techniques
US6890924B2 (en) * 2000-06-22 2005-05-10 Pfizer Inc Substituted bicyclic derivatives for the treatment of abnormal cell growth
US20050137213A1 (en) * 2003-07-03 2005-06-23 Myriad Genetics, Incorporated Compounds and therapeutical use thereof
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

Family Cites Families (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH421972A (de) 1960-02-02 1966-10-15 Thomae Gmbh Dr K Verfahren zur Herstellung von basisch substituierten Pyrimidincarbonsäuren-(4) bzw. ihren Derivaten
FR8491M (US20070244113A1-20071018-C00204.png) 1968-12-31 1973-07-27
DE2918591A1 (de) * 1979-05-09 1980-11-20 Hoechst Ag Neue 4-substituierte 5,6,7,8-tetrahydrochinoline, ihre herstellung und verwendung
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
GB8910722D0 (en) 1989-05-10 1989-06-28 Smithkline Beckman Intercredit Compounds
CA2015981A1 (en) * 1989-05-10 1990-11-10 Thomas H. Brown Compounds
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
BR9205645A (pt) * 1991-02-20 1994-06-07 Pfizer Derivados de 2,4-diaminoquinazolinas para aumentar a atividade antitumoral
US5256781A (en) 1991-10-24 1993-10-26 American Home Products Corporation Substituted quinazolines as angiotensin II antagonists
GB9127252D0 (en) 1991-12-23 1992-02-19 Boots Co Plc Therapeutic agents
US5270466A (en) 1992-06-11 1993-12-14 American Cyanamid Company Substituted quinazoline fungicidal agents
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
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
US6313150B1 (en) 1994-04-06 2001-11-06 Shionogi & Co., Ltd. α-substituted phenylacetic acid derivative, its production and agricultural fungicide containing it
WO1997012863A1 (en) 1995-09-29 1997-04-10 Shionogi & Co., Ltd. α-SUBSTITUTED BENZYL HETEROCYCLIC DERIVATIVES, INTERMEDIATES FOR PRODUCING THE SAME, AND PESTICIDES CONTAINING THE SAME AS ACTIVE INGREDIENT
US5874738A (en) * 1996-07-16 1999-02-23 Saint-Gobain Industrial Ceramics, Inc. Scintillation crystal modules and methods of making the same
JP3345021B2 (ja) 1996-08-06 2002-11-18 ファイザー インク. 置換ピリド―またはピリミド―含有6,6―または6,7―二環式誘導体
US6002008A (en) 1997-04-03 1999-12-14 American Cyanamid Company Substituted 3-cyano quinolines
WO1999009986A1 (fr) * 1997-08-22 1999-03-04 Kyowa Hakko Kogyo Co., Ltd. Derives de 4-aminoquinazoline
HUP0100079A2 (hu) 1997-10-10 2001-05-28 Cytovia, Inc. Új, fluoreszcens riportermolekulák és alkalmazásaik, többek között kaszpázok vizsgálatára
US20020025968A1 (en) * 1998-04-15 2002-02-28 Rifat Pamukcu Method for inhibiting neoplastic cells and related conditions by exposure to 4-aminoquinazoline derivatives
WO2000010981A1 (en) 1998-08-21 2000-03-02 Parker Hughes Institute Quinazoline derivatives
US6297258B1 (en) 1998-09-29 2001-10-02 American Cyanamid Company Substituted 3-cyanoquinolines
YU13200A (sh) 1999-03-31 2002-10-18 Pfizer Products Inc. Postupci i intermedijeri za dobijanje anti-kancernih jedinjenja
WO2002047690A1 (en) 2000-12-12 2002-06-20 Cytovia, Inc. Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators of caspases and inducers of apoptosis and the use thereof
WO2004078114A2 (en) * 2003-02-28 2004-09-16 Encysive Pharmaceuticals Inc. Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-ii receptor antagonists.
WO2006074147A2 (en) * 2005-01-03 2006-07-13 Myriad Genetics, Inc. Nitrogen containing bicyclic compounds and therapeutical use thereof
PL1678166T3 (pl) * 2003-10-14 2009-12-31 Univ Arizona Inhibitory kinaz białkowych

Patent Citations (99)

* 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
US3502681A (en) * 1968-04-10 1970-03-24 Roussel Uclaf 7- or 8-chloro-4-phenylamino-chloroquinolines
US3632761A (en) * 1969-08-08 1972-01-04 Upjohn Co Method of obtaining antihypertensive and antianxiety effects
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
US4322420A (en) * 1978-09-11 1982-03-30 Sankyo Company Limited Method of using 4-anilinoquinazoline derivatives as analgesic and anti-inflammatory agents
US4464375A (en) * 1978-09-11 1984-08-07 Sankyo Co., Ltd. 4-Anilinoquinazoline compounds and pharmaceutical compositions thereof
US4435003A (en) * 1980-01-31 1984-03-06 Ciba-Geigy Corporation Chromogenic quinazolines
US4675047A (en) * 1980-07-01 1987-06-23 Alexander Serban Substituted phenylamine- and phenyloxy-quinazolines as herbicides
US4510307A (en) * 1980-08-20 1985-04-09 Asahi Kasei Kogyo Kabushiki Kaisha 6-Quinazolinesulfonyl derivatives and process for preparation thereof
US5114939A (en) * 1988-01-29 1992-05-19 Dowelanco Substituted quinolines and cinnolines as fungicides
US5145843A (en) * 1988-01-29 1992-09-08 Dowelanco Quinoline and cinnoline fungicides
US5294622A (en) * 1988-01-29 1994-03-15 Dowelanco Substituted quinolines and cinnolines
US5240940A (en) * 1988-01-29 1993-08-31 Dowelanco Quinoline and cinnoline fungicide compositions
US5223505A (en) * 1989-04-21 1993-06-29 Imperial Chemical Industries Plc Pyrimidine derivatives
US5654298A (en) * 1990-04-19 1997-08-05 Imperial Chemical Industries Amine derivatives
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
US6057320A (en) * 1991-05-10 2000-05-02 Aventis Pharmaceuticals Products Inc. Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
USRE36256E (en) * 1991-05-10 1999-07-20 Rhone-Poulenc Rorer Pharmaceuticals, Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5409930A (en) * 1991-05-10 1995-04-25 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF 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
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
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
US20040014774A1 (en) * 1991-05-10 2004-01-22 Myers Michael R. 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
US5646153A (en) * 1991-05-10 1997-07-08 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5795889A (en) * 1991-05-10 1998-08-18 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5276148A (en) * 1991-05-23 1994-01-04 Basf Aktiengesellschaft Phenylazobenzenes or naphthylazobenzenes having a plurality of fiber-reactive groups
US5330989A (en) * 1991-10-24 1994-07-19 American Home Products Corporation Heterocycles substituted with biphenyl-3-cyclobutene-1,2-dione derivatives
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
US5604251A (en) * 1992-03-07 1997-02-18 Hoechst Aktiengesellschaft Imidazole derivatives with a biphenylsulfonylurea or biphenylsulfonylurethane side chain and their use as angitensin II receptors
US5436233A (en) * 1992-07-15 1995-07-25 Ono Pharmaceutical Co., Ltd. 4-aminoquinazoline derivatives
US5618829A (en) * 1993-01-28 1997-04-08 Mitsubishi Chemical Corporation Tyrosine kinase inhibitors and benzoylacrylamide derivatives
US5618814A (en) * 1993-08-02 1997-04-08 Dr. Karl Thomae Gmbh Trisubstituted pyrimido [5,4-d] pyrimidines for modulating multi-drug resistance and pharmaceutical compositions containing these compounds
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
US6713484B2 (en) * 1994-01-25 2004-03-30 Warner-Lambert Company Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
US6265410B1 (en) * 1994-01-25 2001-07-24 Warner-Lambert Company Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
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
US6521620B1 (en) * 1994-01-25 2003-02-18 Warner-Lambert Company Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
US6084095A (en) * 1994-01-25 2000-07-04 Warner-Lambert Company Substituted pyrido[3,2-d]pyrimidines capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
US5948819A (en) * 1994-04-06 1999-09-07 Shionogi & Co., Ltd α-substituted phenylacetic acid derivative, its production and agricultural fungicide containing it
US5707989A (en) * 1994-09-07 1998-01-13 Dr. Karl Thomae Gmbh Pyrimido 5,4-D!pyrimidines, medicaments comprising these compounds, their use and processes for their preparation
US5747486A (en) * 1994-11-08 1998-05-05 Takeda Chemical Industries Thienopyridine or thienopyrimidine derivatives and their use
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
US6344459B1 (en) * 1996-04-12 2002-02-05 Warner-Lambert Company Irreversible inhibitors of tyrosine kinases
US6602863B1 (en) * 1996-04-12 2003-08-05 Warner-Lambert Company Irreversible inhibitors of tyrosine kinases
US5747498A (en) * 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US6124330A (en) * 1996-06-27 2000-09-26 Janssen-Cilag S.A. N-[4-(Heteroarylmethyl)phenyl]-heteroarylamines
US6391874B1 (en) * 1996-07-13 2002-05-21 Smithkline Beecham Corporation Fused heterocyclic compounds as protein tyrosine kinase inhibitors
US5760230A (en) * 1996-10-11 1998-06-02 Bayer Aktiengesellschaft 4, 4'-bridged bis-2, 4-diaminoquinazolines
US5874438A (en) * 1996-10-11 1999-02-23 Bayer Aktiengesellschaft 2,2'-bridged bis-2,4-diaminoquinazolines
US5952346A (en) * 1996-10-14 1999-09-14 Hoechst Marion Roussel Deutschland Gmbh Use of non-peptide bradykinin antagonists for the treatment or prevention of Alzheimer's disease
US5739127A (en) * 1996-11-08 1998-04-14 Bayer Aktiengesellschaft 2,4'-bridged bis-2,4-diaminoquinazolines
US20030144330A1 (en) * 1996-12-11 2003-07-31 Spiegelman Bruce M. Methods and pharmaceutical compositions for inhibiting tumor cell growth
US6552055B2 (en) * 1996-12-11 2003-04-22 Dana-Farber Cancer Institute Methods and pharmaceutical compositions for inhibiting tumor cell growth
US20010014679A1 (en) * 1997-05-02 2001-08-16 Tang Peng C. Methods of modulating serine/threonine protein kinase function with quinazoline-based compounds
US6204267B1 (en) * 1997-05-02 2001-03-20 Sugen, Inc. Methods of modulating serine/thereonine protein kinase function with quinazoline-based compounds
US6562818B1 (en) * 1997-07-29 2003-05-13 Warner-Lambert Company Irreversible inhibitors of tyrosine kinases
US6251912B1 (en) * 1997-08-01 2001-06-26 American Cyanamid Company Substituted quinazoline derivatives
US6242196B1 (en) * 1997-12-11 2001-06-05 Dana-Farber Cancer Institute Methods and pharmaceutical compositions for inhibiting tumor cell growth
US6265425B1 (en) * 1997-12-19 2001-07-24 Janssen Pharmaceutica, N.V. Combination of a RAMBA and a tocopherol
US6552027B2 (en) * 1998-05-28 2003-04-22 Parker Hughes Institute Quinazolines for treating brain tumor
US20030144178A1 (en) * 1998-06-30 2003-07-31 Parker Hughes Institute Method for inhibiting C-jun expression using JAK-3 inhibitors
US20030069248A1 (en) * 1998-08-28 2003-04-10 Sarvajit Chakravarty Quinazoline derivatives as medicaments
US6184226B1 (en) * 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
US6277989B1 (en) * 1998-08-28 2001-08-21 Scios, Inc. Quinazoline derivatives as medicaments
US20020048271A1 (en) * 1998-12-02 2002-04-25 Farzan Rastinejad Methods and composition for restoring conformational stability of a protein of the p53 family
US6284764B1 (en) * 1999-01-27 2001-09-04 Pfizer Inc. Substituted bicyclic derivatives useful as anticancer agents
US6541481B2 (en) * 1999-01-27 2003-04-01 Pfizer Inc Substituted bicyclic derivatives useful as anticancer agents
US6177433B1 (en) * 1999-03-05 2001-01-23 Parker Hughes Institute JAK-3 inhibitors for treating allergic disorders
US6080748A (en) * 1999-03-05 2000-06-27 Parker Hughes Institute Therapeutic use of JAK-3 inhibitors
US6080747A (en) * 1999-03-05 2000-06-27 Hughes Institute JAK-3 inhibitors for treating allergic disorders
US6518283B1 (en) * 1999-05-28 2003-02-11 Celltech R&D Limited Squaric acid derivatives
US20030162799A1 (en) * 1999-05-28 2003-08-28 Langham Barry John 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
US6890924B2 (en) * 2000-06-22 2005-05-10 Pfizer Inc Substituted bicyclic derivatives for the treatment of abnormal cell growth
US20020082270A1 (en) * 2000-08-26 2002-06-27 Frank Himmelsbach Aminoquinazolines which inhibit signal transduction mediated by tyrosine kinases
US6740651B2 (en) * 2000-08-26 2004-05-25 Boehringer Ingelheim Pharma Kg Aminoquinazolines which inhibit signal transduction mediated by tyrosine kinases
US20040034044A1 (en) * 2000-11-02 2004-02-19 Masahiko Okano Quinazoline derivatives and drugs
US20040034045A1 (en) * 2000-11-29 2004-02-19 Parker Hughes Institute Inhibitors of thrombin induced platelet aggregation
US6727251B2 (en) * 2000-12-21 2004-04-27 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US20030055068A1 (en) * 2000-12-21 2003-03-20 David Bebbington Pyrazole compounds useful as protein kinase inhibitors
US20030105090A1 (en) * 2000-12-21 2003-06-05 David Bebbington Pyrazole compounds useful as protein kinase inhibitors
US20030134836A1 (en) * 2001-01-12 2003-07-17 Amgen Inc. Substituted arylamine derivatives and methods of use
US20040043388A1 (en) * 2001-03-02 2004-03-04 Come Jon H. Three hybrid assay system
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
US20030087931A1 (en) * 2001-03-23 2003-05-08 Patrick Mailliet Chemical derivatives and their application as antitelomerease agent
US20030087908A1 (en) * 2001-04-11 2003-05-08 Geuns-Meyer Stephanie D. Substituted triazinyl amide derivatives and methods of use
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
US20030144506A1 (en) * 2001-11-30 2003-07-31 Pfizer Inc. Processes for the preparation of substituted bicyclic derivatives for the treatment of abnormal cell growth
US20030149062A1 (en) * 2002-02-05 2003-08-07 Boehringer Ingelheim Pharma Gmbh & Co. Kg Use of tyrosine kinase inhibitors for the treatment of inflammatory processes
US20040038856A1 (en) * 2002-05-17 2004-02-26 Sarvajit Chakravarty Treatment of fibroproliferative disorders using TGF-beta inhibitors
US20050137213A1 (en) * 2003-07-03 2005-06-23 Myriad Genetics, Incorporated Compounds and therapeutical use thereof

Cited By (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7989462B2 (en) 2003-07-03 2011-08-02 Myrexis, Inc. 4-arylamin-or-4-heteroarylamino-quinazolines and analogs as activators of caspases and inducers of apoptosis and the use thereof
US20080004297A1 (en) * 2003-07-03 2008-01-03 Myriad Genetics, Inc. Compounds and therapeutical use thereof
US20080032974A1 (en) * 2003-07-03 2008-02-07 Myriad Genetics, Incorporated Compounds and therapeutical use thereof
US8309562B2 (en) 2003-07-03 2012-11-13 Myrexis, Inc. Compounds and therapeutical use thereof
US20070244114A1 (en) * 2004-07-06 2007-10-18 Myriad Genetics, Incorporated Compounds and therapeutical use thereof
US8258145B2 (en) 2005-01-03 2012-09-04 Myrexis, Inc. Method of treating brain cancer
US20080051398A1 (en) * 2005-01-03 2008-02-28 Myriad Genetics, Inc. Method of treating brain cancer
US20080319048A1 (en) * 2007-06-22 2008-12-25 Scidose Llc Solubilized formulation of docetaxel without tween 80
US20110092579A1 (en) * 2009-10-19 2011-04-21 Scidose Llc Solubilized formulation of docetaxel
US20110092580A1 (en) * 2009-10-19 2011-04-21 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
US8541465B2 (en) 2009-10-19 2013-09-24 Scidose, Llc Docetaxel formulations with lipoic acid and/or dihydrolipoic acid
US8912228B2 (en) 2009-10-19 2014-12-16 Scidose Llc Docetaxel formulations with lipoic acid

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US20050137213A1 (en) 2005-06-23
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US7618975B2 (en) 2009-11-17
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