| 摘要 |
<p>EP--83172 A N-(Substd.-acetyl)-L-proline derivs. and analogues of formula (I) and their salts are new - R1CO-NH-CHR2-CH2-P(:O)(OR3)-A-CO-X (I) - Where R1 and R2 are H, 1-7C (halo)alkyl, (CH2)qC6H(5-p)(R13)p, (CH2)m-D or 1-7C aminoalkyl; D is cycloalkyl, furyl, thienyl or pyridinyl; A is (CH2)n-CHR21, NR22-CHR23 or O-CHR23; n is 0 or 1; q is 0-7; R21 is H, 1-7C (halo)alkyl, benzyl or phenethyl; R22 is H or 1-7C alkyl; R23 is H, 1-7C (halo)alkyl or (CH2)rD1; D1 is Ph, p-HOC6H4, 3,4-(HO)2C6H3, 3-indolyl, 4-imidazolyl, NH2, SH, 1-7C alkylthio, NH-C(:NH)NH2 or CONH2; X is substd.-azetidine, -pyrrolidine, -thiazolidine or -piperidine; m is 0-3; p is 1-3; R3 is H, 1-7C alkyl, PhCH2, Ph2CH or CHR17-O-COR18; R17 is H, 1-7C alkyl or Ph and R18 is H, 1-7C alkyl, 1-7C alkoxy or Ph; or R17 + R18 form (CH2)2, (CH2)3, ethynyl or o-phenylene. EPAB- EP--83172 B N-(Substd.-acetyl)-L-proline derivs. and analogues of formula (I) and their salts are new - R1CO-NH-CHR2-CH2-P(:O)(OR3)-A-CO-X (I) - Where R1 and R2 are H, 1-7C (halo)alkyl, (CH2)qC6H(5-p)(R13)p, (CH2)m-D or 1-7C aminoalkyl; D is cycloalkyl, furyl, thienyl or pyridinyl; A is (CH2)n-CHR21, NR22-CHR23 or O-CHR23; n is 0 or 1; q is 0-7; R21 is H, 1-7C (halo)alkyl, benzyl or phenethyl; R22 is H or 1-7C alkyl; R23 is H, 1-7C (halo)alkyl or (CH2)rD1; D1 is Ph, p-HOC6H4, 3,4-(HO)2C6H3, 3-indolyl, 4-imidazolyl, NH2, SH, 1-7C alkylthio, NH-C(:NH)NH2 or CONH2; X is substd.-azetidine, -pyrrolidine, -thiazolidine or -piperidine; m is 0-3; p is 1-3; R3 is H, 1-7C alkyl, PhCH2, Ph2CH or CHR17-O-COR18; R17 is H, 1-7C alkyl or Ph and R18 is H, 1-7C alkyl, 1-7C alkoxy or Ph; or R17 + R18 form (CH2)2, (CH2)3, ethynyl or o-phenylene. (180pp) USAB- US4716155 A Novel P-contg.. cpd. has formula (I), and opt. comprises its pharmaceutical salt. R1 and R2 are each e.g. H, opt. halo-substd. lower alkyl, substd. Ph(CH2)q, cycloalkyl(CH2)m, NH2-substd. lower alkyl, etc.; m is 0-3; q is 0-7; R3 and R6 are each e.g. H, lower alkyl, PhCH2, benzhydryl, etc.; R23 is e.g. H, opt. halo-substd. lower alkyl, etc.; X has e.g. formula (II) or (III) etc.; R7 is e.g. H, OH, halogen, keto, lower alkyl, etc.; and R8 is e.g. keto, halogen, O-lower alkyl, etc. - Pref. (I) is 1-((S)-2-(((2-(benzoylamino) -3-phenylpropyl)hydroxyphos phinyl)oxy) -1-oxopropyl)-L- proline.</p> |
