WO2005003100A2 - 4-arylamino-quinazolines as activators of caspases and inducers of apoptosis - Google Patents

4-arylamino-quinazolines as activators of caspases and inducers of apoptosis Download PDF

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Publication number
WO2005003100A2
WO2005003100A2 PCT/US2004/021631 US2004021631W WO2005003100A2 WO 2005003100 A2 WO2005003100 A2 WO 2005003100A2 US 2004021631 W US2004021631 W US 2004021631W WO 2005003100 A2 WO2005003100 A2 WO 2005003100A2
Authority
WO
WIPO (PCT)
Prior art keywords
alkyl
methyl
independently
halo
phenyl
Prior art date
Application number
PCT/US2004/021631
Other languages
English (en)
French (fr)
Other versions
WO2005003100A3 (en
Inventor
Sui Xiong Cai
Nilantha Sudath Sirisoma
Azra Pervin
John A. Drewe
Shailaja Kasibhatla
Songchun Jiang
Hong Zhang
Chris Pleiman
Vijay Baichwal
John Manfredi
Leena Bhoite
Original Assignee
Myriad Genetics, Inc.
Cytovia, Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Myriad Genetics, Inc., Cytovia, Inc. filed Critical Myriad Genetics, Inc.
Priority to JP2006517854A priority Critical patent/JP5129957B2/ja
Priority to NZ544472A priority patent/NZ544472A/xx
Priority to CN2004800242058A priority patent/CN1984660B/zh
Priority to EP04785803A priority patent/EP1660092A2/en
Priority to CA002531327A priority patent/CA2531327A1/en
Priority to AU2004253967A priority patent/AU2004253967B2/en
Publication of WO2005003100A2 publication Critical patent/WO2005003100A2/en
Publication of WO2005003100A3 publication Critical patent/WO2005003100A3/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—Nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Cephalosporin Compounds (AREA)
PCT/US2004/021631 2003-07-03 2004-07-06 4-arylamino-quinazolines as activators of caspases and inducers of apoptosis WO2005003100A2 (en)

Priority Applications (6)

Application Number Priority Date Filing Date Title
JP2006517854A JP5129957B2 (ja) 2003-07-03 2004-07-06 カスパーゼの活性化因子およびアポトーシスの誘発因子としての４−アリールアミノ−キナゾリン
NZ544472A NZ544472A (en) 2003-07-03 2004-07-06 Compounds and therapeutical use thereof
CN2004800242058A CN1984660B (zh) 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
EP04785803A EP1660092A2 (en) 2003-07-03 2004-07-06 4-arylamino-quinazolines as activators of caspases and inducers of apoptosis
CA002531327A CA2531327A1 (en) 2003-07-03 2004-07-06 Compounds and therapeutical use thereof
AU2004253967A AU2004253967B2 (en) 2003-07-03 2004-07-06 4-arylamino-quinazolines as activators of caspases and inducers of apoptosis

Applications Claiming Priority (8)

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

Publications (2)

Publication Number Publication Date
WO2005003100A2 true WO2005003100A2 (en) 2005-01-13
WO2005003100A3 WO2005003100A3 (en) 2005-05-12

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PCT/US2004/021631 WO2005003100A2 (en) 2003-07-03 2004-07-06 4-arylamino-quinazolines as activators of caspases and inducers of apoptosis

Country Status (9)

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US (7) US7618975B2 (US20070244113A1-20071018-C00090.png)
EP (1) EP1660092A2 (US20070244113A1-20071018-C00090.png)
JP (2) JP5129957B2 (US20070244113A1-20071018-C00090.png)
KR (1) KR101218213B1 (US20070244113A1-20071018-C00090.png)
CN (1) CN1984660B (US20070244113A1-20071018-C00090.png)
AU (1) AU2004253967B2 (US20070244113A1-20071018-C00090.png)
CA (1) CA2531327A1 (US20070244113A1-20071018-C00090.png)
NZ (1) NZ544472A (US20070244113A1-20071018-C00090.png)
WO (1) WO2005003100A2 (US20070244113A1-20071018-C00090.png)

Cited By (34)

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WO2005115362A1 (en) 2004-05-15 2005-12-08 Vertex Pharmaceuticals Incorporated Treating seizures using ice inhibitors
WO2007011618A1 (en) * 2005-07-15 2007-01-25 Schering Corporation Quinazoline derivatives useful in cancer treatment
EP1833511A2 (en) * 2005-01-03 2007-09-19 Myriad Genetics, Inc. Method of treating brain cancer
EP1833482A2 (en) * 2005-01-03 2007-09-19 Myriad Genetics, Inc. Compounds and therapeutical use thereof
EP1890677A2 (en) * 2005-06-16 2008-02-27 Myriad Genetics, Inc. Pharmaceutical compositions and use thereof
JP2008526734A (ja) * 2004-12-31 2008-07-24 エスケー ケミカルズ カンパニー リミテッド 糖尿及び肥満治療予防に有効なキナゾリン誘導体
WO2008157500A1 (en) * 2007-06-17 2008-12-24 Kalypsys, Inc. Aminoquinazoline cannabinoid receptor modulators for treatment of disease
JP2009521460A (ja) * 2005-12-21 2009-06-04 アボット・ラボラトリーズ 抗ウイルス化合物
JP2009521479A (ja) * 2005-12-21 2009-06-04 アボット・ラボラトリーズ 抗ウイルス化合物
JP2009533405A (ja) * 2006-04-14 2009-09-17 アストラゼネカ アクチボラグ Ｃｓｆ−１ｒキナーゼ阻害剤としての４−アニリノキノリン−３−カルボキサミド
EP2144887A1 (en) * 2007-04-10 2010-01-20 Myriad Pharmaceuticals, Inc. Dosages and methods for the treatment of cancer
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US7767670B2 (en) 2003-11-13 2010-08-03 Ambit Biosciences Corporation Substituted 3-carboxamido isoxazoles as kinase modulators
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EP2295054A1 (en) 2004-05-27 2011-03-16 Vertex Pharmaceuticals Incorporated Ice inhibitors for the treatment of autoinflammatory diseases
US7915411B2 (en) 2005-12-21 2011-03-29 Abbott Laboratories Anti-viral compounds
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
WO2011069335A1 (zh) * 2009-12-08 2011-06-16 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
WO2011151423A1 (en) 2010-06-04 2011-12-08 Exonhit S.A. Substituted isoquinolines and their use as tubulin polymerization inhibitors
US8236950B2 (en) 2006-12-20 2012-08-07 Abbott Laboratories Anti-viral compounds
US8258145B2 (en) 2005-01-03 2012-09-04 Myrexis, Inc. Method of treating brain cancer
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CN104130200A (zh) * 2014-07-01 2014-11-05 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
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US11661422B2 (en) 2020-08-27 2023-05-30 Incyte Corporation Tricyclic urea compounds as JAK2 V617F inhibitors
US11691971B2 (en) 2020-06-19 2023-07-04 Incyte Corporation Naphthyridinone compounds as JAK2 V617F inhibitors
US11753413B2 (en) 2020-06-19 2023-09-12 Incyte Corporation Substituted pyrrolo[2,1-f][1,2,4]triazine compounds as JAK2 V617F inhibitors
US11767323B2 (en) 2020-07-02 2023-09-26 Incyte Corporation Tricyclic pyridone compounds as JAK2 V617F inhibitors
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US11919908B2 (en) 2020-12-21 2024-03-05 Incyte Corporation Substituted pyrrolo[2,3-d]pyrimidine compounds as JAK2 V617F inhibitors
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AU2012225735B2 (en) 2011-03-04 2016-03-10 Glaxosmithkline Intellectual Property Development Limited Amino-quinolines as kinase inhibitors
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ME03300B (me) 2012-06-13 2019-07-20 Incyte Holdings Corp Supsтituisana triciklična jedinjenja као inhibiтori fgfr
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