Santen Pharmaceutical Co., Ltd.

Ken-ichi Fujimura

Hiroshi Suhara

Yoichi Kawashima

Takahiro Honda

Masakazu Ban

Kazuo Nishimura

Shiro Mita

Masashi Niwa

Masanori Hori

Nobuaki Miyawaki

Yuko Fujita

Eiko Matsumoto

Shin-ichi Kohno

Yaeko Osumi

Maki Tokai

Masato Horiuchi

Noriyoshi Yamamoto

Tadayuki Kobayashi

Junzo Matsumoto

Hiromi Matsumoto

Masahiro Okamoto

A method of treating pain or pruritis comprising administering to a patient in need thereof a pharmaceutically effective amount of a &#x3ba; opioid receptor agonist of the formula wherein R is an alkyl having an amino group as a substituent; and Ris acyl.

Method for treating pain or pruritis by administering &#x3ba;-opioid receptor agonist comprising 2-phenylbenzothiazoline derivative

A compound or a salt thereof having the following formula wherein Ris acyl, Ris hydrogen, halogen, unsubstituted alkyl or alkyl substituted by halogen; Ris halogen or alkoxy; Ris cycloalkyl, unsubstituted alkyl or alkyl substituted by cycloalkyl, aryl or hydroxyl or an ester thereof or alkoxy; Ris hydroxyl or an ester thereof, alkoxy or alkoxyalkyl; or Rand Rare bonded with each other to form a pyrrolidine ring substituted by hydroxyl or an ester thereof, alkoxy or alkoxyalkyl; Ris hydroxyl or an ester thereof, alkoxy, alkoxyalkoxy, alkoxyalkoxyalkoxy, mercapto or alkylthio; and Aand A, are the same or different, and are alkylene, provided that (i) when Rand Rare bonded to each other to form the pyrrolidine ring substituted by hydroxyl or an ester thereof, Ris halogen; (ii) when Rand Rare bonded to each other to form the pyrrolidine ring substituted by alkoxyalkyl, Ris hydrogen; (iii) when Ris hydroxyl or an ester thereof, Ris isopropyl.

&#x3ba; opioid receptor agonist comprising 2-phenylbenzothiazoline derivative

A compound having 3-oxo-3, 4-dihydro-2H-1, 4-thiazine 4-tetrahydropyrazine as a main skeleton. The compound is a chymase inhibitor and is represented by the following formula [I] and salts thereof:In the formula [I], X is S; Rand Rare H, alkyl, cycloalkyl or aryl; Rand Rare H, alkyl, cycloalkyl, aryl or an aromatic heterocycle; Ris H, alkyl, cycloalkyl, aryl or -A-A-R; Ris H, alkyl, cycloalkyl, hydroxy, alkoxy, aryl, aryloxy or an aromatic heterocycle; Ris H, alkyl, hydroxy, alkoxy, aryl, aryloxy, amino, alkylamino, arylamino, an aromatic heterocycle or a nonaromatic heterocycle; Ais alkylene; Ais carbonyl or sulfonyl; Ais alkylene; Ais carbonyl or oxalyl; and n is 0 or 1.

Thiazine derivatives

A compound which is a chymase inhibitor and which is represented by a formula &lsqb;I&rsqb; and salts thereof. In the formula &lsqb;I&rsqb;, X is R &mdash;(A ) &mdash;N, R and R are H, alkyl, cycloalkyl or aryl, R and R are H, alkyl, cycloalkyl, aryl or aromatic heterocycle, R is H, alkyl, cycloalkyl, aryl or &mdash;A &mdash;A &mdash;R , R is H, alkyl, cycloalkyl, OH, alkoxy, aryl, aryloxy or an aromatic heterocycle, R is H, alkyl, OH, alkoxy, aryl, aryloxy, amino, alkylamino, arylamino, an aromatic heterocycle or a nonaromatic heterocycle, A is alkylene, A is carbonyl or sulfonyl, A is alkylene, A is carbonyl or oxalyl and n is o or 1. The formula &lsqb;I&rsqb; is

Thiazine or pyrazine derivatives

Thiazolidine derivatives

The present invention relates to leukotriene A,hydrolase inhibitors containing compounds represented by the formula &lsqb;I&rsqb; or salts thereof as active ingredients,

Leukotriene A4 hydrolase inhibitors

1,3-dialkylurea derivative

1,3-dialkylurea derivatives having a hydroxyl group

A compound of the formula [I]. ##STR1## The compounds of this invention has excellent thymulin-line activities and expected to be useful for treatment of various diseases such as immunodeficiency and autoimmune diseases.

Bicyclic compounds

Growing community of inventors

Osaka, Japan

Ken-ichi Fujimura