Toray Industries, Inc.

Morihiro Fujimura

Koji Kawai

Naoki Izumimoto

Kuniaki Kawamura

Toshikazu Komagata

Sayoko Kanie

Yohei Noro

A method for therapy of diarrhea-predominant irritable bowel disorders comprising as an effective ingredient a morphinan derivative having a nitrogen-containing cyclic group or a pharmaceutically acceptable acid addition salt thereof is disclosed. The method for therapy of diarrhea-predominant irritable bowel disorders comprises as an effective ingredient a morphinan derivative or a pharmaceutically acceptable acid addition salt thereof, having a specific structure, such as N-(17-cyclopeopylmethyl-4,5&#x3b1;-epoxy-3,14-dihydroxy-morphinan-6&#x3b2;-yl)-3,4,5,6-tetrahydrophthalimide tartaric acid salt (Compound 10). 

Method for therapy of diarrhea-predominant irritable bowel disorders

The invention provides a morphinan derivative of the Formula (I): wherein Ris methyl, cyclopropylmethyl or the like; Rand Rare hydroxy, methoxy, acetoxy or the like; both Y and Z are valence bonds, &#x2014;C(&#x2550;O)&#x2014; or the like; X is C-Ccarbon chain (one of the carbon atoms may be substituted by oxygen, sulfur or nitrogen) constituting a part of the ring structure, or the like; (R)k is substituted or non-substituted benzene fused ring, carbonyl group or the like; Ris hydrogen or the like; Rand Rare bound to represent &#x2014;O&#x2014;, or the like, and Ris hydrogen or the like or a pharmaceutically acceptable acid addition salt thereof. The invention also provides a therapeutic or prophylactic agent for urinary frequency or urinary incontinence, comprising as an effective ingredient the morphinan derivative or the pharmaceutically acceptable acid addition salt thereof; a method for therapy or prophylaxis of the diseases.

Remedies or preventives for urinary frequency or urinary incontinence and morphinan derivatives having nitrogen-containing heterocyclic group

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Kanagawa, Japan

Morihiro Fujimura