发明名称 Substitued 4'-oxo-spiro[cyclopropane-1,6'-[2H]-indene] derivatives useful as antitumor agents
摘要 An 4'-oxo-spiro[cyclopropane-1,6'-[2H]-indene] derivative or a pharmaceutically acceptable salt thereof has the formula I which is useful for treating cancer wherein: R1 is hydrogen, hydroxy, mercapto, amino, halo, carboxy, nitro, or -(CH2)n-(X)-(Y); n is 0 to 4; X is oxy, thio, -N(Ra)-, or absent; Y is cycloalkyl, aryl, heteroaryl, a saccharide, an optionally protected amino acid, , OH, carboxy, a peptide, or an optionally branched optionally substituted optionally saturated 1 to 15 membered carbon chain optionally comprising 1, 2, or 3 non-peroxide oxy, thio or -N(Ra) -; R2 is carboxy, alkanoyl, alkoxycarbonyl, haloalkyl, -C(=O)NRdRe, a saccharide, an amino acid, a peptide, or optionally substituted alkyl; R3 is hydrogen, alkyl, alkoxy, alkylthio, aryl, heteroaryl, aryloxy, or heteroaryloxy; R4 is hydrogen or alkyl; and R5 is hydroxy, alkoxy, or alkanoyloxy; or R4 and R5 taken together are ethylenedioxy; R6 is hydrogen, carboxy, alkanoyl, alkoxycarbonyl, haloalkyl, -C(=O)NRfRg, a saccharide, an amino acid, a peptide, or optionally substituted alkyl and Ra, Rd, Re, Rf and Rg are each defined in the specification.
申请公布号 NZ506592(A) 申请公布日期 2003.07.25
申请号 NZ19990506592 申请日期 1999.02.19
申请人 THE REGENTS OF THE UNIVERSITY OF CALIFORNIA 发明人 MCMORRIS, TREVOR C;KELNER, MICHAEL J
分类号 A61K31/12;A61K31/16;A61K31/195;A61K31/25;A61K38/00;A61P35/00;C07C49/737;C07C49/753;C07C69/013;C07C69/16;C07C69/18;C07C323/58;C07C323/59;C07C323/60;C07D207/16;C07K5/02;C07K5/065;C07K5/083;C07K5/103;(IPC1-7):C07C49/497;C07C49/517;A61K38/05 主分类号 A61K31/12
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