Toa Eiyo Ltd.

Toa Eiyo Kagaku Kogyo Co. Ltd.

Sagami Chemical Research Center Toa Eiyo Ltd.

Shin-ichi Yamada

Kentaro Kogi

Sen-ichi Narita

Takao Goto

Atsuo Takahashi

Takaji Yamaguchi

Hiroyasu Sato

Senichi Narita

Masakatsu Shibasaki

Fumiya Yoneyama

Tuyoshi Aoki

Toshihisa Mashiko

Yukiko Oguchi

Kazuyuki Aihara

Tetsuo Kimura

Michiko Kudo

Kaoru Genkyou

Eiji Shimanuki

Sachiko Yoneyama

Tsuyoshi Aoki

Kaoru Gengyou

Sachiko Ishigami

Eizi Shimanuki

Toyoki Nishimata

Yoichi Manome

Takashi Satoh

Rie Yorita

Takahiro Yamaguchi

Tetsutaro Hayasaka

Takahashi Atsuo

Isamu Sato

Kazuyoshi Okutani

Jun Sasamori

Teruo Saito

Kuniro Saito

This invention relates to a cycloalka&lsqb;b&rsqb;pyridine-3-carbonylguanidine derivative represented by the following general formula (1):

Cycloalka&lsqb;b&rsqb;pyridine-3-carbonylguanidine derivatives, process for producing the same, and drugs containing the same

A substituted cyclic amine compound represented by the following general formula (1) ##STR1## wherein each of R.sup.1 to R.sup.5 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group or the like, A represents a carbonyl group or a sulfonyl group, B represents a methine moiety or a nitrogen atom, D represents a methine moiety, a nitrogen atom or .dbd.N(.fwdarw.O)-- and n is an integer of 2 to 3; and synthetic methods thereof. The inventive compound is useful in preventing and treating circulatory organ-related diseases such as hypertension, ischemic heart disease, cerebrovascular disease, peripheral circulatory disease and the like.

Substituted cyclic amine compound, production process thereof and

Provided are cycloheptenopyridine derivatives represented by the general formula ##STR1## [wherein R represents a hydrogen atom or lower alkyl group; R.sup.1 represents a hydrogen atom, halogen atom, lower cycloalkoxy group, amido group, substituted phenoxy group, substituted benzyloxy group, lower alkoxy group optionally containing halogen atoms(s), nitro group, hydroxyl group, lower alkenyloxy group, lower alkylthio group, or a group--NR.sup.4 R.sup.5 (wherein R.sup.4 and R.sup.5 may be the same or different and each represent a hydrogen atom or lower alkyl group, or R.sup.4 and R.sup.5 mutually combine together with the nitrogen atom adjacent thereto to form a 5- or 6-membered heterocyclic group); R.sup.2 represents a hydrogen atom, halogen atom, lower alkyl group optionally containing a halogen atom, lower alkoxy group optionally containing a halogen atom, hydroxyl group, acyl group, lower alkoxycarbonyl group, nitro group or amino group; R.sup.3 represents a hydrogen atom, a lower alkyl group, lower alkoxymethyl group, lower alkylcarbonyl group, lower alkoxycarbonyl group, carbamoyl group, lower alkylcarbamoyl group, lower alkylcarbonylmethyl group, lower alkoxycarbonyl group, lower acyloxymethyl group, lower alkylsulfonyl group, or physiologically acceptable protective group eliminatable in an acid medium or under a physiological condition; n represents 0 or 1; and A represents a methine carbon or nitrogen atom] or their salts. These derivatives and their salts are useful as antiulcer agents.

Cycloheptenopyridine derivatives, process for preparation thereof and

A cis-bicyclo[4.3.0]non-2-ene derivative of the formula: ##STR1## wherein R is a hydrogen atom, or a protecting group for a hydroxyl group, R.sup.1 is a hydrogen atom, A C.sub.1 -C.sub.12 straight or branched chain alkyl group, a substituted or unsubstituted phenyl group, a C.sub.6 -C.sub.12 aralkyl group containing a condensed aromatic ring or an aromatic hetero ring, or 1 equivalent of a cation, A is --CH.dbd.CH--CH.sub.2 --, or --CH.sub.2 --CH.sub.2 --O--, R.sup.2 is a C.sub.3 -C.sub.10 straight or branched chain alkyl group, a C.sub.1 -C.sub.3 alkyl group substituted by an aryloxy group which may be substituted, a C.sub.3 -C.sub.12 straight or branched chain alkenyl group, a C.sub.3 -C.sub.8 straight or branched chain alkynyl group, a C.sub.1 -C.sub.3 alkyl group substituted by a phenyl or phenoxy group which may be substituted, by a C.sub.1 -C.sub.6 alkoxy group or by a C.sub.5 -C.sub.8 cycloalkyl group, R.sup.3 is a hydrogen atom, a methyl group, or a vinyl group, and X is a halogen atom.

Cis-bicyclo[4,3.0]non-2-end derivatives

A 4,7-dihydroisothiazole[5,4-b]pyridine derivative represented by the general formula ##STR1## wherein R.sup.1 represents an alkyl group which may be substituted,

4,7-dihydroisothiazolo(5,4-b)pyridine derivatives and cardiovascular

Novel compounds, dibenzo[a,d]cycloheptene derivatives, of the general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, a halogen atom or a lower alkyl group, R.sub.2 and R.sub.3 each represent a hydrogen atom or a lower alkyl group, and Z represents a group of the formula ##STR2## These novel compounds are useful as non-steroidal anti-inflammatory agents free from gastrointestinal lesions. The compounds of formula (I) can be prepared, for example, by cyclizing a compound of the general formula ##STR3## wherein R.sub.1 and R.sub.2 are as defined above, X represents a hydroxyl group or a halogen atom, one Y represents a group of the formula --CH.sub.2 COX and the other Y represents a hydrogen atom; optionally hydrolyzing the cyclized product; and optionally esterifying the product, and/or etherifying its enol group.

Dibenzo[a,d]cycloheptene derivatives and process for production thereof

Growing community of inventors

Fukushima, Japan

Shin-ichi Yamada