专利号:US-5827855-A 优先权日:1992-12-28 标题 :Hexahydronaphthalene ester derivatives their preparation and their therapeutic uses 发明人:KOGEN HIROSHI; ISHIHARA SADAO; KOGA TEIICHIRO; KITAZAWA EIICHI; SERIZAWA NOBUFUSA; HAMANO KIYOSHI 权利人:SANKYO CO 摘要:Compounds of formula (I): (I) wherein R1 represents a group of formula (II) or (III): (II) (III) R2 is alkyl, alkenyl or alkynyl; R3 and R4 are each hydrogen, alkyl, alkenyl or alkynyl; R5 is hydrogen or a carboxy-protecting group; Ra is a group of formula -OR6; R6 is hydrogen; R6a and R6b are each hydrogen, a hydroxy-protecting group, alkyl, alkanesulfonyl, halogenated alkanesulfonyl or arysulfonyl, and their salts and esters. Such compounds inhibit the synthesis of cholesterol, and can be used for the treatment and prophylaxis of hypercholesterolemia and of various cardiac disorders.
专利号:US-4996314-A 优先权日:1986-03-11 标题 :6-(disubstituted amino)carbapenem compounds 发明人:YOSHIOKA TAKEO; CHIDA NORITAKA; WATANABE AZUMA; FUKAGAWA YASUO; ISHIKURA TOMOYUKI 权利人:SANRAKU INC 摘要:A compound represented by the formula ##STR1## wherein R 1 represents a lower alkyl group or a lower haloalkyl group; R 2 represents a lower alkyl group, a lower haloalkyl group, an aralkyl group, or a group of the formula --COOR 4 or --SO 2 R 5 in which R 4 represents an aralkyl group or a substituted or unsubstituted alkyl group and R 5 represents an alkyl group or a substituted or unsubstituted aryl group; and R 3 represents a hydrogen atom or a carboxyl protecting group which can be easily split off. This compound is useful in the production of a 6-(disubstituted amino)carbapenem-series antibiotic. n The compounds of the formula ##STR2## wherein R 1 and R 2 are as defined above are important intermediates for the synthesis of the compounds of formula (I) and/or the aforesaid di-(substituted amino) carbapenem-series antibiotics.
专利号:US-3989685-A 优先权日:1972-06-29 标题 :Process for making a 2'-halopenicillin 发明人:TANIDA HIROSHI; TSUJI TERUJI 权利人:SHINOGI CO 摘要:A 2'-halopenicillin compound is prepared from a penicillin-1-oxide compound by the action of an acid halide in the presence of a base. The product on heating rearranges to a 3-halo-3-methylcepham compound which itself gives a 3-methyl-3-cephem compound on further heating. A 2'-halopenicillin compound gives a 3-methyl-3-cephem compound on heating. The 2'-halopenicillin compounds, 3-halo-3-methylcepham compound and 3-methyl-3-cephem compounds are antibacterials which are also useful as intermediates for the synthesis of other penicillins and cephalosporins.
专利号:US-5491167-A 优先权日:1993-01-29 标题 :Hexahydronaphthalene ester derivatives, their preparation and their therapeutic uses 发明人:ISHIHARA SADAO; KOGEN HIROSHI; KOGA TEIICHIRO; KITAZAWA EIICHI; SERIZAWA NOBUFUSA 权利人:SANKYO CO 摘要:Compounds of formula (I): ##STR1## and their salts and esters have the ability to inhibit the synthesis of cholesterol, and can thus be used for the treatment and prophylaxis of hypercholesterolemia and of various cardiac disorders.