Kyowa Hakko Kogyo Co., Ltd.

Kyowa Hakko Kirin Co., Limited

University of Pittsburgh

Kyowa Hakko Kogyo

Kyowa Hakko Kogyo K.k.

Tetsuji Ohno

Akira Karasawa

Kazuhiro Kubo

Yuji Nomoto

Fumio Suzuki

Junichi Shimada

Koji Yamada

Akio Ishii

Haruki Takai

Hiromi Nonaka

Tomoko Ishikawa

Takao Nakajima

Yoshisuke Nakasato

Hiroyuki Obase

Etsuo Ohshima

Michio Ichimura

Fumihiko Kanai

Toshiaki Kumazawa

Noriaki Uesaka

Shiro Shirakura

Masamori Sugawara

Hideyuki Sato

Tsuyoshi Yamagata

Kaoru Atsuki

Shin-ichi Uchida

Shiho Takahara

Hiroshi Kase

Kenji Ohmori

Daisuke Machii

Yasuo Onoda

Kenji Shibata

Motoo Yamasaki

Tadashi Hirata

Eiji Tsukuda

Katsuichi Shuto

Shizuo Shiozaki

Toshiyuki Suzawa

Takeshi Kuroda

Haruhiko Manabe

Kenji Matsuno

Takeo Tanaka

Iwao Kinoshita

Naoki Yoshimura

William C De Groat

Ken Nagashima

Shin-ichi Sasaki

Kazuihiro Kubo

Adrian Sculptoreanu

Shin-Ichi Uchida

Method of treating central nervous systems disease by administering wherein n is an integer of from 0 to 3; Ris a 5-membered aromatic heterocyclic group containing at least one oxygen atom; Ris &#x2014;COR(wherein Ris aryl); Ris hydrogen or lower alkyl; and Rrepresents cycloalkyl, aryl, aralkyl, alicyclic heterocyclic group, aromatic heterocyclic group, alicyclic hetocyclic-alkyl, or aromatic heterocyclic-alkyl, and R, R, Rand Rare individually optionally substituted.

Thiazole derivatives

Wherein n is an integer of from 0 to 3; Ris a 5-membered aromatic heterocyclic group containing at least one oxygen atom; Ris &#x2014;COR(wherein Ris aryl); Ris hydrogen or lower alkyl; and Rrepresents cycloalkyl, aryl, aralkyl, alicyclic heterocyclic group, aromatic heterocyclic group, alicyclic hetocyclic-alkyl, or aromatic heterocyclic-alkyl, and R, R, Rand Rare individually optionally substituted. 

(Wherein n is an integer of from 0 to 3; Ris substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, or a substituted or unsubstituted aromatic heterocyclic group; Ris halogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, a substituted or unsubstituted aromatic heterocyclic group, &#x2014;COR, or the like; Rand Rmay be the same or different, and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl, &#x2014;COR, or the like) For example, provided are adenosine Areceptor antagonists comprising, as the active ingredient, a thiazole derivative represented by a general formula (I), or a pharmaceutically acceptable salt thereof, and the like. 

The present invention provides a therapeutic agent for bladder irritative symptoms associated with benign prostatic hyperplasia comprising, as an active ingredient, a tricyclic compound represented by formula (I): [wherein Rrepresents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy or halogen;X-X-Xrepresents CR&#x2550;CR&#x2014;CR&#x2550;CR, N(O)&#x2550;CR&#x2014;CR&#x2550;CR, CR&#x2550;CR&#x2014;N(O)&#x2550;CR, CR&#x2550;CR&#x2014;CR&#x2550;N(O), CR&#x2550;CR&#x2014;O, CR&#x2550;CR&#x2014;S, O&#x2014;CR&#x2550;CR, S&#x2014;CR&#x2550;CRor O&#x2014;CR&#x2550;N;Y represents 13 CHS&#x2014;, &#x2014;CHSO&#x2014;, &#x2014;CHSO&#x2014;, &#x2014;CHO&#x2014;, &#x2014;CH&#x2550;CH&#x2014;, &#x2014;(CH)&#x2014;, &#x2014;SCH&#x2014;, &#x2014;SOCH&#x2014;, &#x2014;SOCH&#x2014; or &#x2014;OCH&#x2014;; andRrepresents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl, substituted or unsubstituted lower alkoxy, amino, mono(substituted or unsubstituted lower alkyl)-substituted amino, di(substituted or unsubstituted lower alkyl)-substituted amino, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aralkylamino, substituted or unsubstituted arylamino or a substituted or unsubstituted heteroalicyclic group] or a pharmaceutically acceptable salt thereof.

Therapeutic agent for bladder irritative symptoms associated with benign prostatic hyperplasia

The present invention provides a therapeutic agent for overactive bladder comprising, as an active ingredient, a tricyclic compound represented by formula (I): [wherein Rrepresents a hydrogen atom, substituted or unsubstituted lower alkyl, and the like;

Remedies for vesical hyperactivity

The present invention provides an agent for the treatment of bladder irritative symptoms accompanied by benign prostatic hyperplasia, comprising, as an active ingredient, a compound having a slowly-inactivating A-type Kchannel opening activity or a pharmaceutically acceptable salt thereof, and a method for screening agents for the treatment of bladder irritative symptoms accompanied by benign prostatic hyperplasia, comprising measuring a slowly-inactivating A-type Kchannel opening activity as an index.

Agent for the treatment of bladder irritative symptoms accompanied by benign prostatic hyperplasia

Imidazoquinazoline derivatives

Endothelin-antagonizing peptide

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

Tricyclic compounds on angiotensin II receptor antagonists

Novel xanthine compounds represented by the following formula: ##STR1## wherein each of R.sup.1, R.sup.2 and R.sup.3 independently represents hydrogen or lower alkyl;

Xanthine compounds

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.

Tricyclic compounds

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.

Novel xanthine compounds represented by the following formula: ##STR1## wherein each of X.sup.1 and X.sup.2 independently represents oxygen or sulfur; and Q represents; ##STR2## where ----- represents a single bond or a double bond; Y represents a single bond or alkylene, n represents 0 or 1, each of W.sup.1 and W.sup.2 independently represents hydrogen, lower alkyl or amino, Z represents --CH.sub.2 -, --O--, --S-- or --NH--; represents ##STR3## each of R.sup.1 and R.sup.2 independently represents hydrogen, lower alkyl, allyl or propargyl; and R.sup.3 represents hydrogen or lower alkyl, and when Q represents the groups other than ##STR4## each of R.sup.1, R.sup.2 and R.sup.3 independently represents hydrogen or lower alkyl; provided that when Q is ##STR5## then R.sup.1 R.sup.2 and R.sup.3 are not simultaneously methyl; and pharmaceutically acceptable salts thereof have a diuretic effect, a renal-protecting effect and a bronchodilatory effect.

Xanthine derivatives

Growing community of inventors

Shizuoka, Japan

Tetsuji Ohno