| 摘要 |
Heterocyclic oxime derivatives (I), their enantiomers, diastereomers and their acid or basic addition salts are new. Heterocyclic oxime derivatives of formula (I), their enantiomers, diastereomers and their acid or basic addition salts are new. A : 1-6C alkyl (where CH2 can be replaced by heteroatom (O or S)), NRa or a phenyl or naphthyl group; RaH or 1-6C alkyl; R1>, R2>, R, R1 : H, 1-6C ((hetero)aryl)alkyl, 2-6C ((hetero)aryl)alkenyl, 2-6C ((hetero)aryl)alkynyl, (hetero)aryl, 3-8C cycloalkyl-1-6C alkyl or polyhalo-1-6C alkyl; either R3>, R4>H, halo, R, OR or NRR1; or -C-R3>-R4>-C- : 5-6 membered ring (containing heteroatom (O, S or N); B1>1-6C alkyl, 2-6C alkenyl (both optionally substituted by -CHR5>R6> or R7>), -CHR5>R6> or R7>; R5>-C(=Z)-OR, -C(=Z)-NRR1, -N(R)-C(=Z)-R1 or -N(R)-C(=Z)-OR1; Z : O or S; R6>(hetero)aryl, (hetero)aryl-1-6C alkyl, CN, tetrazole, OR, NRR1, -N(R)-C(=Z)-R1, -N(R)-C(=Z)-OR1 or -N(R)-C(=Z)-R; R7>CN, tetrazole, -N(R)-C(=Z)-R1, -N(R)-C(=Z)-OR1 or -O-(CH2)n-C(R8>R9>)-COOR; n : 1-6; and R8>, R9>H or 1-6C alkyl. Provided that both R8> and R9> are not simultaneously H. Provided that (1) the oxime R1>-C(=N-OR2>)- can be the Z or E configuration; (2) the aryl are phenyl, naphthyl or biphenyl, which can be partially hydrogenated; (3) the heteroaryl are 5-10 membered mono or bicylic aromatic, where the bicyclics can partially be hydrogenated, and containing 1-3 heteroatom (O, N or S); and (4) the (hetero)aryl are optionally substituted by 1-3 of 1-6C (polyhalo)alkyl, 1-6C alkoxy, OH, carboxy, 1-6C alkoxycarbonyl, 1-6C acyloxy, formyl, 1-6C acyl, aryl, NRbRc, amido, nitro, CN or halo, where Rb, Rc are H, 1-6C alkyl or (hetero)aryl. Independent claims are included for: (1) the preparations of (I); (2) a composition (X) comprising (I) an antioxidant agent. [Image] - ACTIVITY : Antidiabetic; Antilipemic; Analgesic; Antianginal; Cardiant; Vasotropic; Cardiovascular-Gen.; Nephrotropic; Ophthalmological; Antipsoriatic; Gynecological; Osteopathic; Gastrointestinal-Gen.; Antiinflammatory; Antiarteriosclerotic; Anorectic; Anabolic; Eating-Disorders-Gen.; Neuroprotective; Cytostatic; Endocrine-Gen.; Neuroleptic. - MECHANISM OF ACTION : Angiogenesis inhibitor.
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