Yamanouchi Pharmaceutical Company Ltd.

Merck Patent Gesellschaft MIT Beschrankter Haftung

Isao Yanagisawa

Mitsuaki Ohta

Keiji Miyata

Yoshio Ishii

Toshinari Tamura

Yasufumi Hirata

Takeshi Suzuki

Yuzo Matsumoto

Akira Matsuhisa

Masuo Murakami

Kenichi Tomioka

Hidenori Iwamoto

Masaaki Takeda

Noriyoshi Inukai

Tokuo Koide

Tomihisa Kawasaki

Seiji Kaku

Ryuji Tsuzuki

Wataru Uchida

Toru Yoden

Junya Ohmori

Seijiro Akamatsu

Masato Ichihara

Tetsuya Shiozaki, Deceased

Jun-ya Ohmori

Yasuo Isomura

Noriki Ito

Hiroyuki Koshio

Fukushi Hirayama

Masaharu Asano

Osamu Hasegawa

Kazuhisa Takayama

Akira Suga

Hideya Matsuda

Toshio Okazaki

Tetsuya Shiozaki

Shinichi Tsukamoto

Osamu Inagaki

Toshihiro Watanabe

Kazumi Kikuchi

Tetsuya Shizaoki

Tokuichi Takagi

Substituted amidinobenzene derivatives and medicinal compositions thereof

Amidinonaphthyl derivative or salt thereof

Benzamidine derivatives and pharmaceutical composition containing them

A novel thiazole derivative represented by general formula (I), which has a selected agonistic activity for 5-HT.sub.3 receptor, a pharmaceutical composition thereof, and a process for producing the same. In the said formula, R.sup.1 represents hydrogen or lower alkoxy; R.sup.2 and R.sup.3 are such that R.sup.2 represents hydrogen and R.sup.3 represents a group, --Y--Het, wherein Y represents a single bond or lower alkylene and Het represents a nitrogenous heterocyclic group, or alternatively R.sup.2 and R.sup.3 are combined together to form a group, --(CH.sub.2).sub.m --NR.sup.4 --(CH.sub.2).sub.n --, wherein m and n are each 1 or 2 and R.sup.4 represents lower alkyl; and X represents --NH--, --NHC(.dbd.O)NH--, --C(.dbd.O)NH-- or --NHC(.dbd.O)--.

Thiazole derivatives

A method is provided for the treatment of hypersensitive intestinal diseases (irritable bowel syndrome) comprising the administration of a tetrahydroimidazopyridine derivative of the formula: ##STR1## wherein either one of X and Y is nitrogen and the other one is a radical represented by the formula .dbd.C(R.sup.1)--; and R can be ##STR2## in which R.sup.1, R.sup.2 and R.sup.3 are same or different hydrogen atom or a lower alkyl group, and salts thereof.

Method of treatment of intestinal diseases

A process is provided for preparing a tetrahydrobenzimidazole derivative represented by Formula (Ib): ##STR1## wherein Het representa s heterocyclic group which may be substituted with 1 to 3 substituents selected from the group consisting of a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a cycloalkyl-lower alkyl group, an aralkyl group, a lower alkoxycarbonyl group, and a halogen atom; and X.sup.2 represents a single bond connected to the carbon atom of the heterocyclic ring as represented by Het. The process comprises reacting a heterocyclic compound represented by Formula (IIIa):

5-substituted tetrahydrobenzimidazole compounds

Pyrazolotriazole derivatives

Novel benzoxazine derivatives of the formula (I): ##STR1## are provided as well as their pharmaceutically acceptable salts and a method for their use as potassium channel activating agents 2-(3,4-Dihydro-2, 2-dimethyl-6-phenylsulfonyl-2H-1,4-benzoxazin-4-yl)pyridine N-oxide is illustrative of a benzoxazine derivative of formula (I). Also provided are intermediate compounds such as those of formula (II): ##STR2##

3,4-dihydro-2H-1,4-benzoxazine derivatives and pharmaceutical

A tetrahydrobenzimidazole derivative represented by formula (I): ##STR1## wherein Het represents a heterocyclic group which may be substituted with 1 to 3 substituents selected from the group consisting of a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a cycloalkyl-lower alkyl group, an aralkyl group, a lower alkoxy group, a nitro group, a hydroxyl group, a lower alkoxycarbonyl group, and a halogen atom; and X represents a single bond or --NH-- which is bonded to the carbon atom or nitrogen atom of the heterocyclic ring, or a pharmaceutically acceptable salt thereof. The compound of formula (I) and a salt thereof exhibits antagonism against 5-HT.sub.3 receptor.

Tetrahydrobenzimidazole derivatives and pharmaceutical compositions

Tetrahydroimidazopyridine derivatives and salts thereof

Oxazinobenzazole derivatives represented by the formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each independently represents a hydrogen atom or a lower alkyl group; R.sup.5 and R.sup.6 jointly form, in conjunction with the two adjacent carbon atoms, a substituted or unsubstituted 5- or 6-membered heterocyclic ring having at least two nitrogen atoms and optionally having one or more heteroatom(s) selected from the group consisting of an oxygen atom, a sulphur atom and a nitrogen atom; and m is an integer of 0 or 1, and pharmaceutically acceptable salts thereof. The compounds of the present invention are useful as antispasmodic medicaments.

Oxazinobenzazole compounds

4,5,6,7-Tetrahydrobenzimidazole derivatives represented by general formula (I) ##STR1## wherein groups represents the following: R.sup.1, R.sup.2, R.sup.3 : independently represent hydrogen atom, hydroxy group, a halogen atom, a lower alkyl group which may optionally be substituted with a halogen atom, a lower alkoxy group, a lower alkylthio group, an aralkyloxy group, an aryloxy group, a lower alkanoyl group, carboxy group, a lower alkoxycarbonyl group or nitro group;

4,5,6,7-tetrahydrobenzimidazole derivatives as 5HT.sub.3 -antagonists

A process is provided for producing a guanidinothiazole compound represented by the formula: ##STR1## wherein, R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen or an alkyl group having 1 to 3 carbon atoms; m represents 1 or 2; and n represents 2, 3 or 4. The process comprises reacting an aminothiazole compound of the formula: ##STR2## with a cyanamide or an amidinopyrazole, the compounds are useful as intermediates in the preparation of a gastric acid secretion inhibitor.

Process of producing guanidinothiazole derivatives

Novel 2-guanidinothiazoline compounds of the general formula ##STR1## wherein R represents a hydrogen atom or a lower alkyl group, and X represents a halogen atom, and the acid addition salts thereof; they are important intermediate compounds for preparing famotidine and thiotidine which are medicaments useful as gastric acid secretion inhibitors.

Novel 2-guanidinothiazoline compounds, and process for preparing them

Growing community of inventors

Tokyo, Japan

Isao Yanagisawa