Toray Industries, Inc.

Lenovo (singapore) Pte. Ltd.

Koji Kawai

Hiroshi Nagase

Takashi Endoh

Akira Mizusuna

Kuniaki Kawamura

Takashi Endo

Naoki Izumimoto

Shu Matsumoto

Shinya Ueno

Hibiki Ikegami

Jun Hayakawa

Izumi Nakatani

Hiroki Kondo

Kiyotaka Ohno

Satoshi Sakami

Hisanori Wakita

Junzo Kamei

Toshikazu Komagata

Masayuki Maeda

Yoshihiro Onoda

Morihiro Fujimura

Yutaka Hosono

Hideo Yoshiwara

Cuong Huy Truong

Yoshihito Nakagaki

Shinnosuke Takahashi

Takumi Aoki

Sayoko Kanie

Yuji Negishi

Toshiyuki Honda

Koji Ohshima

Hideaki Fujii

Yohei Noro

Yoshiaki Katsura

Kohei Arakawa

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An antitussive, which can be used for therapy or prophylaxis of coughing, is disclosed. The antitussive comprises as an effective ingredient a morphinan derivative having a nitrogen-containing cyclic substituent or a pharmaceutically acceptable acid addition salt thereof, having a specific structure, such as the compound below [N-(17-cyclopeopylmethyl-4,5&#x3b1;-epoxy-3,14-dihydroxy-morphinan-6&#x3b2;-yl)-3,4,5,6-tetrahydrophthalimide]. The antitussive has an excellent therapeutic or prophylactic effect against coughing and the side effects thereof are small. 

Antitussive agent

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

A method of inhibiting or reducing occurrence or intensity of pruritus including administering to a patient an effective amount of one or more of the morphinan derivative having a nitrogen-containing cyclic group of the Formula (Ia): wherein Ris cyclopropylmethyl; Rand Rare independently hydrogen, hydroxy, C-Calkoxy, C-Calkenyloxy, C-Caralkyloxy or C-Calkanoyloxy; and the Formula (Ia) includes (+), (&#x2212;) and (&#xb1;) isomers or the pharmaceutically acceptable acid addition salt thereof.

Anti-itching agent

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

Indole derivatives and use thereof in medicines

Antitussives

A morphinan derivative or its pharmacologically allowed acid addition salt represented with compound I,

Morphinan derivative and its pharmaceutical applications

A novel compound which is a &dgr;-opioid antagonist having high selectivity and activity, that exhibits immunosuppressive action, antiallergic action, anti-inflammatory action and brain cell-protecting action is disclosed. The compound according to the present invention is an indole derivative represented by the formula (I):

Indole derivatives process for producing the same and medicinal uses of the same

Novel morphinan derivatives and pharmaceutically acceptable acid addition salts thereof as compounds having abilities to bind to opioid &egr;-receptor, which have agonist or antagonist activities, are disclosed. The morphinan derivatives according to the present invention are represented by the formula (I).

Morphinane derivatives and medicinal use thereof

A morphinan derivative or its pharmaceutically acceptable acid addition salt represented with, for example,

Morphinan derivatives and pharmaceutical use thereof

Growing community of inventors

Kanagawa, Japan

Koji Kawai