Kyowa Hakko Kogyo Co., Ltd.

Kyowa Hakko Kogyo

Toshiaki Kumazawa

Hiroyuki Obase

Koji Yamada

Etsuo Ohshima

Tetsuji Ohno

Fumihiko Kanai

Shiro Shirakura

Hideyuki Sato

Tomoko Ishikawa

Masashi Yanase

Shiho Takahara

Kazuhiro Kubo

Katsuichi Shuto

Shoji Oda

Shigeru Aono

Hiroyuki Harakawa

Akira Karasawa

Akio Ishii

Shunji Ichikawa

Kenji Ohmori

Haruki Takai

Hiroshi Tanaka

Shigeto Kitamura

Haruhiko Manabe

Etsuo Oshima

Yoshimasa Oiji

Tadafumi Tamura

Hidee Ishii

Koji Suzuki

Tsuyoshi Yamagata

Kaoru Atsuki

Makoto Yoshida

Takashi Seishi

Eiko Oishi

Hirokazu Koshimura

Shizuo Otaki

Hitoshi Takami

Nobuyuki Kishibayashi

The present invention provides tricyclic compounds which are useful for the treatment of pollakiuria and urinary incontinence and which are represented by general formula (I):

Tricyclic compounds

Phenylpiperidine derivative

Disclosed is a tricyclic compound represented by formula (I): ##STR1## where X.sup.1 -X.sup.2 represents CH.dbd.CH--CH.dbd.CH, CH.dbd.CH--CH.dbd.N or S--CH.dbd.CH;

Tricyclic compounds having ACAT inhibiting activity

A tricyclic compound represented by the following formula (I): ##STR1## exhibits antagonism to angiotensin II receptors.

Tricyclic compounds on angiotensin II receptor antagonists

A tricyclic compound represented by the following formula (I): ##STR1## wherein R.sup.1 represents hydrogen, halogen or lower alkyl; A represents cyano, carboxyl, tetrazolyl, cyano-substituted phenyl, carboxyl-substituted phenyl or tetrazolyl-substituted phenyl; V represents --(CH.sub.2).sub.m --(wherein m is an integer of 0 to 2); W represents ##STR2## (wherein R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, halogen, lower alkyl, cycloalkyl, halogenated lower alkyl, hydroxy, lower alkoxy, amino, lower alkylamino, carboxyl or lower alkoxycarbonyl; and Q.sup.1 --Q.sup.2 --Q.sup.3 --Q.sup.4 represents N.dbd.CH--CH.dbd.CH; X.sup.1 --X.sup.2 --X.sup.3 represents CH.dbd.CH--CH.dbd.CH, S--CH.dbd.CH or CH.dbd.CH--S; Y represents a single bond, CH.sub.2, O, S, CH.sub.2 O, OCH.sub.2, CH.sub.2 S, SCH.sub.2, CH.sub.2 CH.sub.2 or CH.dbd.CH; and Z.sup.1 --Z.sup.2 represents C.dbd.CH, CH--CH.sub.2 or CH--CH(COOH)-- or a pharmaceutically acceptable salt thereof. The compound of the present invention exhibits antagonism to angiotensin II receptors.

Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6-alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 -O, CH.sub.2 -S(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.14 represents hydrogen or C1-6 alkyl) and Z represents oxygen or sulfur, or a pharmaceutically acceptable salt thereof. The compound possesses an acyl coenzyme A: cholesterol acyltransferase-inhibiting activity, and thus are expected to have preventive and therapeutic effects on hyperlipemia and arteriosclerosis.

Tricyclic compounds and intermediates thereof

A tricyclic compound represented by the following formula (I): ##STR1## wherein R.sup.1 represents hydrogen, halogen or lower alkyl; A represents cyano, carboxyl, tetrazolyl, cyano-substituted phenyl, carboxyl-substituted phenyl or tetrazolyl-substituted phenyl; V represents --(CH.sub.2).sub.m -- wherein m is an integer of 0 to 2; W represents ##STR2## and Q.sup.1 --Q.sup.2 --Q.sup.3 --Q.sup.4 represents N.dbd.CH--CH.dbd.CH, CH.dbd.CH--CH.dbd.CH or CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2, ##STR3## and Q represents N or CH; X.sup.1 --X.sup.2 --X.sup.3 represents CH.dbd.CH--CH.dbd.CH, S--CH.dbd.CH or CH.dbd.CH--S; Y represents CH.sub.2 CH.sub.2 ; and Z.sup.1 --Z.sup.2 represents N--(CH.sub.2).sub.n -- wherein n is an integer of 1 to 3 or a pharmaceutically acceptable salt thereof.

Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6 alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 --O, CH.sub.2 --(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.14 represents hydrogen or C1-6 alkyl) and Z represents oxygen or sulfur, or a pharmaceutically acceptable salt thereof. The compound possesses an acyl coenzyme A: cholesterol acyltransferase-inhibiting activity, and thus are expected to have preventive and therapeutic effects on hyperlipemia and arteriosclerosis.

The present invention provides Indole derivatives represented by the formula (I) ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 independently represent hydrogen or lower alkyl;

Indole derivatives which inhibit steroid 5.alpha. reductase

Novel dibenz[b,e]oxepin derivatives are employed in the treatment and control of allergic conditions such as allergic asthma and also employed in the treatment of inflammation.

Dibenz[b,e]oxepin derivative and pharmaceutical compositions thereof

A novel [1] benzepino[3,4-b]pyridine derivative having antiulcer activity is represented by the formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group, a halogenated alkyl group, an alkoxy group or a halogen atom; R.sup.2 represents ##STR2## wherein Y represents an amino group, a substituted amino group, a heterocyclic group or a substituted heterocyclic group; Z represents a hydrogen atom, an alkyl group or an acyl group; and m is an integer of 1-3, ##STR3## wherein Z' represents a hydrogen atom or an alkyl group; Y has the same meaning as defined above, and n is 0, 1 or 2; or ##STR4## wherein Z and n have the same meanings as defined above; X represents an oxygen atom or a sulfur atom. Also disclosed are pharmaceutically acceptable acid addition salts of the compound represented by the formula (I).

Antiulcer [1] benzepino[3,4-b]pyridine and compositions

Growing community of inventors

Shizuoka, Japan

Toshiaki Kumazawa