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5-PHENYL-ISOXAZOLE-3-CARBOXAMIDES MODULATING HSP90 WITH ANTITUMORAL ACTIVITIES
专利权人:
SIGMA-TAU RESEARCH SWITZERLAND S.A.
发明人:
GIANNINI, GIUSEPPE,CABRI, WALTER,SIMONI, DANIELE,BARUCHELLO, RICCARDO,CARMINATI, PAOLO,PISANO, CLAUDIO
申请号:
NZ59086109
公开号:
NZ590861A
申请日:
2009.06.30
申请国别(地区):
NZ
年份:
2012
代理人:
摘要:
Disclosed herein are aryl isoxazole derivatives of formula I wherein: X is halogen, alkyl, alkenyl, haloalkyl, aryl, heteroaryl, benzyl, amino, alkylamino, or aminocarbonyl Y and Z, the same or different, are halogen, nitro, haloalkyl, R3, OR3, amino, alkylamino, or aminocarbonyl R1 is NHC(=O)ER4, NHC(=S)ER4, or NR5R6 R2 is NR8R9 and additional substituents are define in the specification which exhibit inhibition of the molecular chaperone heat shock protein 90 (Hsp90) for use in the treatment of a neurodegenerative disease, inflammatory disease, cancer, autoimmune disease, cerebral ischemia, parasitemia including malaria. Examples of neurodegenerative diseases include Parkinson disease, Huntington disease, Alzheimer disease, dementia with Lewy bodies, amyotrophic lateral sclerosis, spinal and bulbar muscular atrophy or spinocerebellar ataxia. Examples of compounds claimed include: 4-acetylamino-5-(5-chloro-2,4-dihydroxy-phenyl)-isoxazole-3-carboxylic acid ethylamide 5-(5-chloro-2,4-dihydroxy-phenyl)-4-(2,2-dimethyl- propionylamino)-isoxazole-3-carboxylic acid ethylamide 1H-indole-6- carboxylic acid [5-(2,4-dihydroxy-5-isopropyl-phenyl)-3-ethyl carbamoyl- isoxazol-4-yl]-amide 4-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-5-(2,4-dihydroxy-5-isopropyl-phenyl)-isoxazole-3- carboxylic acid ethylamide and 5-(5-chloro-2,4-dihydroxy-phenyl)-4-(4-methoxy-benzoylaniino)-isoxazol-3-yl-(4-methylpiperazin-l-yl)-methanone.
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中国工程科技知识中心
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