CN102083804A - 具有抗肿瘤活性的调节hsp90的5-苯基-异噁唑-3-甲酰胺 - Google Patents

具有抗肿瘤活性的调节hsp90的5-苯基-异噁唑-3-甲酰胺 Download PDF

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Publication number
CN102083804A
CN102083804A CN2009801255931A CN200980125593A CN102083804A CN 102083804 A CN102083804 A CN 102083804A CN 2009801255931 A CN2009801255931 A CN 2009801255931A CN 200980125593 A CN200980125593 A CN 200980125593A CN 102083804 A CN102083804 A CN 102083804A
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Prior art keywords
isoxazole
phenyl
carboxylic acid
dihydroxy
chloro
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Pending
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CN2009801255931A
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Chinese (zh)
Inventor
G·简尼尼
W·卡布里
D·西蒙尼
R·巴鲁克谢罗
P·卡米纳蒂
C·皮萨诺
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Sigma-Tau Research Switzerland SA
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Sigma-Tau Research Switzerland SA
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D261/18—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D261/14—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
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  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Transplantation (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN2009801255931A 2008-07-04 2009-06-30 具有抗肿瘤活性的调节hsp90的5-苯基-异噁唑-3-甲酰胺 Pending CN102083804A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP08159692.6 2008-07-04
EP08159692 2008-07-04
PCT/EP2009/058205 WO2010000748A1 (en) 2008-07-04 2009-06-30 5-phenyl-isoxazole-3-carboxamides modulating hsp90 with antitumoral activities

Publications (1)

Publication Number Publication Date
CN102083804A true CN102083804A (zh) 2011-06-01

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CN2009801255931A Pending CN102083804A (zh) 2008-07-04 2009-06-30 具有抗肿瘤活性的调节hsp90的5-苯基-异噁唑-3-甲酰胺

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Country Link
US (1) US8383616B2 (enExample)
EP (1) EP2310377B1 (enExample)
JP (1) JP5640002B2 (enExample)
KR (1) KR20110050615A (enExample)
CN (1) CN102083804A (enExample)
AR (1) AR072793A1 (enExample)
AU (1) AU2009265745B2 (enExample)
BR (1) BRPI0913834A2 (enExample)
CA (1) CA2729710A1 (enExample)
EA (1) EA019793B1 (enExample)
IL (1) IL210200A0 (enExample)
MX (1) MX2010013913A (enExample)
MY (1) MY150604A (enExample)
NZ (1) NZ590861A (enExample)
SG (1) SG192464A1 (enExample)
TW (1) TWI450898B (enExample)
WO (1) WO2010000748A1 (enExample)
ZA (1) ZA201100007B (enExample)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103733069A (zh) * 2011-08-24 2014-04-16 浦项工科大学校产学协力团 筛选伴侣蛋白调节物的方法
CN103724269A (zh) * 2012-10-11 2014-04-16 中国科学院上海药物研究所 苯基1,2-异噁唑或苯基1,2-吡唑类化合物及其用途
CN104725329A (zh) * 2015-01-13 2015-06-24 陕西科技大学 一种具有抗肿瘤活性的异恶唑羧酸类化合物及其合成方法
CN104803934A (zh) * 2015-05-04 2015-07-29 陕西科技大学 一种具有抗肿瘤活性的苯基异恶唑羧酸类化合物及其合成方法与应用
CN117105880A (zh) * 2022-10-17 2023-11-24 上海康斯维克生物医药有限公司 用作诱发抗原特异性反应的脲类化合物、其荧光标记物及制备方法和用途

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US8236838B2 (en) * 2008-04-21 2012-08-07 Institute For Oneworld Health Compounds, compositions and methods comprising isoxazole derivatives
US8343976B2 (en) 2009-04-20 2013-01-01 Institute For Oneworld Health Compounds, compositions and methods comprising pyrazole derivatives
WO2012058271A2 (en) 2010-10-27 2012-05-03 Pixelligent Technologies, Llc Synthesis, capping and dispersion of nanocrystals
MA39483A (fr) * 2014-03-18 2015-09-24 Synta Pharmaceuticals Corp Agents thérapeutiques cibles
WO2016054560A1 (en) * 2014-10-02 2016-04-07 Flatley Discovery Lab Isoxazole compounds and methods for the treatment of cystic fibrosis
US10870651B2 (en) 2014-12-23 2020-12-22 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
CN107427521B (zh) 2015-03-27 2021-08-03 达纳-法伯癌症研究所股份有限公司 细胞周期蛋白依赖性激酶的抑制剂
IT201700081419A1 (it) 2017-07-18 2019-01-18 Rare Partners Srl Derivati isossazolici come induttori di emoglobina fetale in precursori eritroidi derivati da pazienti beta-talassemici
EP3810132A4 (en) * 2018-06-25 2022-06-22 Dana-Farber Cancer Institute, Inc. TAIRE FAMILY KINASE INHIBITORS AND RELATED USES
CN113164477A (zh) 2018-12-14 2021-07-23 达纳-法伯癌症研究所股份有限公司 C-jun-n-末端激酶的吡唑并吡啶抑制剂及其用途
EP3902542A4 (en) 2018-12-28 2022-09-07 Dana-Farber Cancer Institute, Inc. CYCLIN DEPENDENT KINASE 7 INHIBITORS AND USES THEREOF

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WO2007096194A1 (en) * 2006-02-27 2007-08-30 Novartis Ag Radio-labeled isoxazole derivatives useful for the labeling and diagnostic of hsp90 functionality

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KR101394245B1 (ko) * 2005-12-30 2014-05-14 에스케이바이오팜 주식회사 아이속사졸 유도체 및 이의 용도
ES2384906T3 (es) * 2007-03-01 2012-07-13 Novartis Ag Mesilato de etilamida del ácido 5-(2,4-dihidroxi-5-isopropil-fenil)-4-(4-morfolin-4-il-metil-fenil)-isoxazol-3-carboxílico, hidratos y polimorfos del mismo y formulaciones que comprenden estas formas

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WO2004072051A1 (en) * 2003-02-11 2004-08-26 Vernalis (Cambridge) Limited Isoxazole compounds as inhibitors of heat shock proteins
CN1771235A (zh) * 2003-02-11 2006-05-10 弗奈利斯(剑桥)有限公司 异噁唑化合物
WO2007096194A1 (en) * 2006-02-27 2007-08-30 Novartis Ag Radio-labeled isoxazole derivatives useful for the labeling and diagnostic of hsp90 functionality

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LAWRENCE A. REITER: "Synthesis of 4(5)-Acyl-, 1-Substituted 5-Acyl-, and 1-Substituted 4-Acyl-1H-imidazoles from 4-Aminoisoxazoles", 《J. ORG. CHEM.》 *
PAUL A. BROUGH，等: "4,5-Diarylisoxazole Hsp90 Chaperone Inhibitors: Potential Therapeutic Agents for the Treatment of Cancer", 《J. MED. CHEM.》 *

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103733069A (zh) * 2011-08-24 2014-04-16 浦项工科大学校产学协力团 筛选伴侣蛋白调节物的方法
US9260717B2 (en) 2011-08-24 2016-02-16 Postech Academy-Industry Foundation Method of screening for chaperonin modulator
CN103733069B (zh) * 2011-08-24 2016-06-08 浦项工科大学校产学协力团 筛选伴侣蛋白调节物的方法
CN103724269A (zh) * 2012-10-11 2014-04-16 中国科学院上海药物研究所 苯基1,2-异噁唑或苯基1,2-吡唑类化合物及其用途
WO2014056446A1 (zh) * 2012-10-11 2014-04-17 中国科学院上海药物研究所 苯基1,2-异噁唑或苯基1,2-吡唑类化合物及其用途
CN103724269B (zh) * 2012-10-11 2016-12-21 中国科学院上海药物研究所 苯基1,2-异噁唑或苯基1,2-吡唑类化合物及其用途
CN104725329A (zh) * 2015-01-13 2015-06-24 陕西科技大学 一种具有抗肿瘤活性的异恶唑羧酸类化合物及其合成方法
CN104803934A (zh) * 2015-05-04 2015-07-29 陕西科技大学 一种具有抗肿瘤活性的苯基异恶唑羧酸类化合物及其合成方法与应用
CN117105880A (zh) * 2022-10-17 2023-11-24 上海康斯维克生物医药有限公司 用作诱发抗原特异性反应的脲类化合物、其荧光标记物及制备方法和用途

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SG192464A1 (en) 2013-08-30
EP2310377B1 (en) 2015-09-16
MX2010013913A (es) 2011-03-03
ZA201100007B (en) 2011-10-26
IL210200A0 (en) 2011-03-31
WO2010000748A1 (en) 2010-01-07
JP2011526594A (ja) 2011-10-13
NZ590861A (en) 2012-08-31
EP2310377A1 (en) 2011-04-20
US20110245221A1 (en) 2011-10-06
MY150604A (en) 2014-01-30
JP5640002B2 (ja) 2014-12-10
AR072793A1 (es) 2010-09-22
KR20110050615A (ko) 2011-05-16
EA019793B1 (ru) 2014-06-30
US8383616B2 (en) 2013-02-26
TWI450898B (zh) 2014-09-01
CA2729710A1 (en) 2010-01-07
EA201170139A1 (ru) 2011-08-30
AU2009265745A1 (en) 2010-01-07
AU2009265745B2 (en) 2013-07-04
BRPI0913834A2 (pt) 2015-10-20
TW201012815A (en) 2010-04-01

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