Sankyo Company, Limited

Eiichi Kitazawa

Sadao Ishihara

Hiroshi Kogen

Teiichiro Koga

Akira Yoshida

Ichiro Hayakawa

Takao Yoshioka

Mitsuo Yamazaki

Nobufusa Serizawa

Takashi Kasai

Yoshio Iizuka

Hiroyuki Koike

Fujio Saito

Kiyoshi Hamano

Kozo Oda

Kousei Shimada

Taro Tokui

Koza Oda

Takashi Fujita

Kazuo Hasegawa

Yomoyuki Kurumada

Compounds of formula (I): ##STR1## wherein: R.sup.1 is alkyl; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are the same or different and each is hydrogen, optionally substituted alkyl or various other organic groups; R.sup.3 is alkyl; R.sup.4 is a group of formula (II), (III), (IV), (V), (VI), (VII), (VIII) or (IX): ##STR2## wherein: A.sup.1 is a single bond, alkylene or alkenylene; A.sup.2 is or alkenylene; A.sup.3 is a single bond, alkyleneor alkenylene; R.sup.5a and R.sup.5b are the same or different and each is hydrogen, alkyl or various other groups; R.sup.6 is alkyl or phenyl; R.sup.7 is hydrogen or alkyl; R.sup.8 is alkyl or various other groups; and n is 0 and pharmaceutically acceptable salts thereof have valuable inhibitory activity against acyl-CoA: cholesterol acyl transferase.

Urea derivatives having ACAT inhibitory activity, their preparation and

Compounds of formula (I): ##STR1## wherein: R.sup.1 is alkyl; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are the same or different and each is hydrogen, optionally substituted alkyl, --(C.dbd.O)--B.sup.1 (wherein B.sup.1 is hydrogen or alkyl), nitro, --NR.sup.c R.sup.d (wherein R.sup.c is hydrogen or alkyl and Rd is alkyl), hydroxy, protected hydroxy group, alkoxy, cyano, alkylthio, alkylsulfinyl, alkylsulfonyl or halogen; R.sup.3 is alkyl; R.sup.4 is a group of the formula (II) ##STR2## wherein A.sup.1 is a single bond, alkylene or alkenylene; R.sup.5a and R.sup.5b are the same or different and each is hydrogen, alkyl or --A.sup.4 R.sup.5.sub.c wherein A is a single bond, alkylene or alkenylene and R.sup.5.sub.c is alkoxy; and n is 0, and pharmaceutically acceptable salts thereof. Such compounds have valuable inhibitory activity against acyl-CoA (cholesterol acyl transferase).

Amide derivatives having ACAT inhibitory activity, their preparation and

Compounds of formula (I): ##STR1## wherein R.sup.1 represents a group of formula (II) or (III): ##STR2## R.sup.2 is alkyl, alkenyl or alkynyl; R.sup.3 and R.sup.4 are each hydrogen, alkyl, alkenyl or alkynyl; R.sup.5 is hydrogen or a carboxy-protecting group; R.sup.a is a group of formula --OR.sup.6 ; R.sup.6 is hydrogen; R.sup.6a and R.sup.6b 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.

Hexahydronaphthalene ester derivatives their preparation and their

Compounds of formula (I) are provided: ##STR1## wherein: R.sup.1 represents an alkyl group; or a group of formula (II), (III), (IV) or (V): ##STR2## and wherein the groups R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen or various organic groups; and pharmaceutically acceptable salts thereof; as well as methods for the preparation of such compounds and their use in the treatment and prophylaxis of hypercholesteremia and arteriosclerosis.

Amide and urea derivatives having anti-hypercholesteremic activity,

Substituted aromatic amides and ureas derivatives having

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.

Hexahydronaphthalene ester derivatives, their preparation and their

Compounds of formula (I): ##STR1## [wherein R.sup.1 represents a group of formula (II) or (III): ##STR2## R.sup.2 is alkyl, alkenyl or alkynyl; R.sup.3 and R.sup.4 are each hydrogen, alkyl, alkenyl or alkynyl; R.sup.5 is hydrogen or a carboxy-protecting group; R.sup.a is hydrogen or a group of formula and --OR.sup.6 ; R.sup.6, R.sup.6a and R.sup.6b are each hydrogen, a hydroxy-protecting group, alkyl, alkanesulfonyl, halogenated alkanesulfonyl or arylsulfonyl] 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.

Compounds of formula (I): ##STR1## (in which R.sup.1 -R.sup.7 are hydrogen or various organic groups, n is 1-10, Ar is an aromatic group, U is CH.sub.2 or a carbon atom doubly bonded to either one of its adjacent carbons, and W is &gt;CH.sub.2, &gt;C.dbd.O, &gt;CHOH, &gt;C.dbd.NOH or various derivatives thereof) have the ability to lower the levels of blood lipid peroxides and blood sugars and to inhibit the activity of aldose reductase; they may be used therapeutically for these purposes.

Thiazolidine derivatives, their preparation and use

Compounds formula (I): ##STR1## in which: R.sup.1 represents a hydrogen atom, an alkyl group, a substituted alkyl group, a C.sub.2 -C.sub.6 alkenyl group, an aryl group, a substituted aryl group or an alkoxycarbonyl group wherein the alkoxy part has from 1 to 6 carbon atoms; R.sup.2 represenets a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a C.sub.3 or C.sub.4 alkenyl group; R.sup.3 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group; R.sup.4 represents a hydroxy group, a C.sub.1 -C.sub.21 aliphatic acyloxy group or a carbocyclic aryl carboxylic aryloxy group; R.sup.5 represents a C.sub.1 -C.sub.12 alkyl group, a C.sub.1 -C.sub.6 alkoxy group, a hydroxy group, a C.sub.1 -C.sub.7 aliphatic acyloxy group or a carbocyclic aryl carboxylic acyloxy group; R.sup.6 represents a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a C.sub.1 -C.sub.6 alkoxy group; and n is 0, 1, or 2;

Lipid peroxide lowering 1,3-benzoxathiole derivative compositions and

Compounds formula (I): ##STR1## in which: R.sup.1 represents a hydrogen atom, an alkyl group, a substituted alkyl group, a C.sub.2 -C.sub.6 alkenyl group, an aryl group, a substituted aryl group or an alkoxycarbonyl group wherein the alkoxy part has from 1 to 6 carbon atoms; R.sup.2 represents a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a C.sub.3 or C.sub.4 alkenyl group; R.sup.3 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group; R.sup.4 represents a hydroxy group, a C.sub.1 -C.sub.21 aliphatic acyloxy group or a carbocyclic aryl carboxylic acyloxy group; R.sup.5 represents a C.sub.1 -C.sub.12 alkyl group, a C.sub.1 -C.sub.6 alkoxy group, a hydroxy group, a C.sub.1 -C.sub.7 aliphatic acyloxy group or a carbocyclic aryl carboxylic acyloxy group; R.sup.6 represents a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a C.sub.1 -C.sub.6 alkoxy group; and n is 0, 1, or 2; and pharmaceutically acceptable salts thereof are valuable in the treatment of circulatory disorders and allergies.

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Tokyo, Japan

Eiichi Kitazawa