Sankyo Company, Limited

Ube Industries, Inc.

Shinsaku Kobayashi

Akira Ogiso

Koichi Kojima

Hiroshi Mishima

Kiyoshi Sakai

Katsutoshi Fujii

Kazuo Koyama

Mikio Kojima

Shigeki Nagai

Takeo Honda

Takashi Kobayashi

Junya Ide

Shigeo Amemiya

Kiroku Oda

Katsuo Kamoshita

Hiroyuki Koike

Mitsuo Yamazaki

Yasuhiro Morisawa

Mitsuru Kataoka

Yasunobu Sato

Takashi Yusa

Seiji Kumakura

Kuniyuki Tomita

Compounds of formula (I): ##STR1## have valuable platelet-aggregation inhibitory activities and may be used for the prophylaxis and treatment of such diseases as thrombosis.

Carbacyclin derivatives, process for their preparation and compositions

Compounds of formula (Ic): ##STR1## having valuable platelet-aggregation inhibitory activities useful for the prophylaxis and treatment of such diseases as thrombosis and pharmaceutical compositions containing said compounds.

Carbacyclin compounds; pharmaceutical compositions and method of use

Compounds of formula (I): ##STR1## (wherein Q is oxygen or sulfur, the dotted line is a single or double bond, A is alkylene, and R.sup.1 -R.sup.5 are a variety of atoms or organic groups) have excellent ability to potentiate myocardial contractivity and a variety of other properties, and can be used to treat cardiac disorders.

Pyridazinone derivatives, their preparation and use

Carbacyclin derivatives with anti-ulcer activity comprise compounds of the general formula (I): ##STR1## (wherein R.sup.1 is selected from the group consisting of a hydrogen atom and an alkyl group having from 1 to 10 carbon atoms; R.sup.2 is selected from the group consisting of a hydrogen atom and a methyl group; and R.sup.3 is selected from the group consisting of a 3-butenyl group, a 4-pentenyl group and a 5-methyl-4-hexenyl group), and pharmaceutically acceptable salts thereof.

Carbacyclin derivatives

4-Anilinoquinazoline derivatives of formula (I): ##STR1## (in which: R.sup.1 represents a hydrogen atom, a halogen atom, a trifluoromethyl group or a nitro group;

4-Anilinoquinazoline compounds and pharmaceutical compositions thereof

Compounds of formula (I): ##STR1## (wherein: R.sup.1 represents a hydroxy group, a C.sub.1 -C.sub.8 alkoxy group, an aliphatic acyloxy group, a benzoyloxy group or a cinnamoyloxy group; p1 R.sup.2 represents a hydrogen atom, a C.sub.1 -C.sub.8 alkyl group, an aliphatic acyl group, a benzoyl group or a cinnamoyl group; and

Wound-healing promoters

Benzothiazocine and benzothiazonine derivatives of formula (I): ##STR1## in which: R.sup.1, R.sup.2 and R.sup.3 are the same or different and each represents a hydrogen atom or an alkyl group;

Benzothiazocine and benzothiazonine derivatives and use

A method of using 4-anilinoquinazoline derivatives of formula (I): ##STR1## (in which: R.sup.1 represents a hydrogen atom, a halogen, atom, a trifluoromethyl group or a nitro group;

Method of using 4-anilinoquinazoline derivatives as analgesic and

Prostacyclin derivatives of formula (I): ##STR1## (wherein R.sup.1 represents a hydrogen atom or a lower alkyl group; R.sup.2 represents an alkenyl group having from 8 to 12 carbon atoms; and n represents an integer of from 1 to 8, inclusive) and pharmaceutically acceptable salts thereof, are valuable pharmaceuticals, showing excellent thrombocyte agglutination inhibitory, coronary blood vessel dilatory and bronchodilatory effects, and may be prepared by introducing the .dbd.CH(CH.sub.2).sub.n COOR.sup.1 side chain onto an appropriate compound by means of a Wittig reaction.

Prostacyclin compounds

Polyprenyl derivatives having the formula ##STR1## in which R.sup.1 and R.sup.2 may be the same or different and each represents hydrogen atom, hydroxyl group, an alkoxy group having 1-8 carbon atoms, an aliphatic acyloxy group having 2-18 carbon atoms, an aromatic acyloxy group or an araliphatic acyloxy group having 2-3 carbon atoms in the aliphatic acyl moiety, R.sup.3 represents hydrogen atom, an alkyl group having 1-8 carbon atoms, an aliphatic acyl group having 2-18 carbon atoms, an aromatic acyl group or an araliphatic acyl group having 2-3 carbon atoms in the aliphatic acyl moiety, n is an integer of 1-4 and, when n is an integer of 2-4, R.sup.2 's may be the same or different; provided that, when n is 1 or 2, at least one of R.sup.1 and R.sup.2 's is hydroxyl group, an alkoxy group, an aliphatic acyloxy group, an aromatic acyloxy group or an araliphatic acyloxy group. These derivatives are useful as medicines for treating peptic ulcer.

Polyprenyl derivatives

Polyprenyl derivatives having the formula ##STR1## [wherein A and B individually represent a group of the formula --CH.sub.2 OR.sup.1 (wherein R.sup.1 is hydrogen atom, an alkyl group having an intervening hetero atom in the carbon chain, carboxyl group on its salt or an aliphatic acyl group optionally having an intervening hetero atom in the carbon chain, an aromatic acyl group, a heterocyclic acyl group, an araliphatic acyl group, a heterocyclic aliphatic acyl group or a radical of an inorganic acid or its salt) or where one of A and B represents the group --CH.sub.2 OR.sup.1, the other represents a group of the formula --COOR.sup.2 (wherein R.sup.2 represents hydrogen atom, a metal atom capable of forming a salt, an organic base or an akyl group), a group of the formula ##STR2## or a group of the formula ##STR3## (wherein R.sup.3 and R.sup.4 may be the same or different and each represents hydrogen atom, an alkyl group optionally having a heterocyclic substituent, an aryl group or an aralkyl group or R.sup.3 and R.sup.4 may jointly form a ring optionally containing other hetero ring atom) and n is an integer of 0 to 4 inclusive, provided that when both A and B are the group --CH.sub.2 OR.sup.1, either of the R.sup.1 represents an alkyl group having an intervening hetero atom, carboxyl group or its salt, an aliphatic acyl group having an intervening hetero atom in the carbon chain, a heterocyclic acyl group, a heterocyclic aliphatic acyl group or a radical of an inorganic acid or its salt]. These derivatives are useful as medicines for treating peptic ulcer.

Higher polyalkenyl fatty acids and esters

Polyprenyl derivatives having the formula ##STR1## in which R.sup.1 and R.sup.2 may be the same or different and each represents hydrogen atom, hydroxyl group, an alkoxy group having 1-8 carbon atoms, an aliphatic acyloxy group having 2-18 carbon atoms, an aromatic acyloxy group or an araliphatic acyloxy group having 2-3 carbon atoms in the aliphatic acyl moiety, R.sup.3 represents hydrogen atom, an alkyl group having 1-8 carbon atoms, an aliphatic acyl group having 2-18 carbon atoms, an aromatic acyl group or an araliphatic acyl group having 2-3 carbon atoms in the aliphatic acyl moiety, n is an integer of 1-4 and, when n is an interger of 2-4, R.sup.2 's may be the same or different; provided that, when n is 1 or 2, at least one of R.sup.2 and R.sup.2 's is hydroxyl group, an alkoxy group, an aliphatic acyloxy group, an aromatic acyloxy group or an araliphatic acyloxy group. These derivatives are useful as medicines for treating peptic ulcer.

Polyprenyl derivatives having the formula ##STR1## [wherein A and B individually represent a group of the formula --CH.sub.2 OR.sup.1 (wherein R.sup.1 is hydrogen atom, an alkyl group having an intervening hetero atom in the carbon chain, carboxyl group on its salt or an aliphatic acyl group optionally having an intervening hetero atom in the carbon chain, an aromatic acyl group, a heterocyclic acyl group, an araliphatic acyl group, a heterocyclic aliphatic acyl group or a radical of an inorganic acid or its salt) or where one of A and B represents the group --CH.sub.2 OR.sup.1, the other represents a group of the formula --COOR.sup.2 (wherein R.sup.2 represents hydrogen atom, a metal atom capable of forming a salt, an organic base or an alkyl group), a group of the formula ##STR2## or a group of the formula ##STR3## (wherein R.sup.3 and R.sup.4 may be the same or different and each represents hydrogen atom, an alkyl group optionally having a heterocyclic substituent, an aryl group or an aralkyl group or R.sup.3 and R.sup.4 may jointly form a ring optionally containing other hetero ring atom) and n is an integer of 0 to 4 inclusive, provided that when both A and B are the group --CH.sub.2 OR.sup.1, either of the R.sup.1 represents an alkyl group having an intervening hetero atom, carboxyl group or its salt, an aliphatic acyl group having an intervening hetero atom in the carbon chain, a heterocyclic acyl group, a heterocyclic aliphatic acyl group or a radical of an inorganic acid or its salt]. These derivatives are useful as medicines for treating peptic ulcer.

Polyprenyl piperazines

Prostanoic acid derivatives having the formula ##STR1## wherein A represents ethylene group or cis-vinylene group, R.sup.1 and R.sup.2 may be the same or different and each represents hydrogen atom or an alkyl group having 1-3 carbon atoms, R.sup.3 and R.sup.4 may be the same or different and each represents an alkyl group having 1-3 carbon atoms and R.sup.5 represents hydrogen atom or hydroxyl group and the pharmaceutically acceptable salts thereof and a process for the preparation thereof. The compounds are useful as anti-ulcerogenic or bronchodilating agents and may be prepared by oxidizing 9.xi.-hydroxy-15.xi.-protected-hydroxy-20-alkylideneprost-13(trans)-enoic acid derivatives.

Growing community of inventors

Hiromachi, Japan

Shinsaku Kobayashi