| 摘要 |
<p>EP--79694 A 7-Oxabicycloheptane derivs. of formula (I) are new. In (I), A' is vinylene or (CH2)2; B' is vinylene, ethynylene or (CH2)2; m is 1-8; X is OH, 1H-tetrazol-5-yl, COOH, (1-12C)alkoxycarbonyl CONHZ; Z is H, 1-12C alkyl, aryl, SO2Q, COQ or OH; Q is 1-12C alkyl or aryl; Y is alkyl (provided that at least one of A' and B' is other than vinylene and X is other than COOH or alkoxycarbonyl), substd. alkyl, aryl-(1-12C)alkyl, alkenyl, alkynyl, aryl, pyridinyl-(1-12C)alkyl, opt. substd. pyridinyl, thienylalkyl, opt. substd. thienyl, opt. substd. cycloalkyl or opt. substd. cycloalkylalkyl; and the broken bond is an opt. double bond, provided that when it is a double bond, A is vinylene and B is vinylene or (CH2)2 and Y is not alkenyl or alkynyl. - (I) are cardiovascular agents esp. inhibitors of blood platelet aggregation for treating thrombolytic diseases, and they are selective inhibitors of thromboxane A2 synthetase e.g. they have a vasodilatory effect for treatment of myocardial ischemic disease such as angina pectoris. Dose is 1-100 mg/kg daily in mammals. EPAB- EP--79694 B 7-Oxabicycloheptane derivs. of formula (I) are new. In (I), A' is vinylene or (CH2)2; B' is vinylene, ethynylene or (CH2)2; m is 1-8; X is OH, 1H-tetrazol-5-yl, COOH, (1-12C)alkoxycarbonyl CONHZ; Z is H, 1-12C alkyl, aryl, SO2Q, COQ or OH; Q is 1-12C alkyl or aryl; Y is alkyl (provided that at least one of A' and B' is other than vinylene and X is other than COOH or alkoxycarbonyl), substd. alkyl, aryl-(1-12C)alkyl, alkenyl, alkynyl, aryl, pyridinyl-(1-12C)alkyl, opt. substd. pyridinyl, thienylalkyl, opt. substd. thienyl, opt. substd. cycloalkyl or opt. substd. cycloalkylalkyl; and the broken bond is an opt. double bond, provided that when it is a double bond, A is vinylene and B is vinylene or (CH2)2 and Y is not alkenyl or alkynyl. - (I) are cardiovascular agents esp. inhibitors of blood platelet aggregation for treating thrombolytic diseases, and they are selective inhibitors of thromboxane A2 synthetase e.g. they have a vasodilatory effect for treatment of myocardial ischemic disease such as angina pectoris. Dose is 1-100 mg/kg daily in mammals. (164pp) - EP--79694 B A compound having the structural formula (I) and including all stereoisomers thereof; wherein A and B may be the same or different and A is CH=CH or (CH2)2, B is CH=CH, C triple bond C or (CH2)2; m is 1 to 8, the group (CH2)m being optionally substituted with 1 or more lower alkyl radicals; X is CO2R1 wherein R1 is H or C1-C12 alkyl; Y is phenyl; phenyl-lower alkyl; substituted phenyl-lower alkyl wherein the substituent is lower alkyl, halogen, (Cl, Br or F) or lower alkoxy; cycloalkyl; cycloalkylalkyl; or substituted cycloalkyl or substituted cyclo alkylalkyl wherein the substituent is 1 or 2 halogen, lower alkyl and/or lower alkoxy radicals; the lower alkyl and lower alkoxy groups having up to 12 carbon atoms, and the cycloalkyl groups having from 3 to 12 carbon atoms; and (i) represents a single or double bond. (43pp) USAB- US4537904 A 7-Oxabicycloheptane and 7-oxabicycloheptene prostaglandin analogues of formula (I) are new. IN (I), A is CH=CH or (CH2)2; B is CH=CH C=C or (CH2)2; m is 1-8; X is OH, COOR1 where R1 is H or 1-12C alkyl or O-CNH-Z where Z is H, 1-12Calkyl or aryl, SO2=Q where Q is 1-12C-alkyl or aryl, O=C-Q or OR2 where R2 is H; Y is alkyl substd. halo, alkoxy, alkyl-aryl, haloalkyl, cycloalkyl or alkylaryl, alkylcycloalkyl, 3-6C-alkenyl or -alkynyl; aryl opt. substd. cycloalkyl opt. substd. cycloalkylalkyl or PhOMe and dotted line is single or double bond. (I) are prepd. from alkylester (VI) by reaction scheme involving Collins oxidn.</p> |
