Nippon Chemiphar Co., Ltd.

University of Tsukuba

University of Texas System

The Kitasato Institute

Toray Industries, Inc.

Hiroshi Nagase

Hideaki Fujii

Masaaki Hirose

Kohei Hayashida

Toshihiro Takahashi

Yoshikazu Watanabe

Daisuke Saito

Koji Kawai

Masashi Yanagisawa

Kuniaki Kawamura

Takashi Endo

Takashi Endoh

Susumu Matsuda

Eriko Nakata

Isao Ooi

Akira Mizusuna

Shu Matsumoto

Yoshifumi Imamura

Yasushi Miyauchi

Akiyoshi Saitoh

Tsuyoshi Saitoh

Yoko Irukayama

Jun Hayakawa

Naoshi Yamamoto

Takashi Nagahara

Yoshihiro Onoda

Yasuyuki Nagumo

Noriki Kutsumura

Takeshi Saiki

Megumi Yashima

Makiko Tada

A method for therapeutic treatment of pain-associated anxiety or depression in a mammalian subject in need thereof, that includes administering to the subject an effective amount of a pharmaceutical composition containing a morphinan derivative that exhibits an opioid δ receptor agonist activity.

Use of morphinan derivatives for treatment of opioid delta receptor agonist-related disease

The present invention aims to provide a novel low-molecular-weight compound showing an orexin receptor agonist activity and expected to be useful as a prophylactic or therapeutic agent for narcolepsy and the like. The present invention provides a compound represented by the formula (I): wherein each symbol is as described in the description, or a pharmaceutically acceptable acid addition salt thereof, which has an orexin receptor agonist activity, and an orexin receptor agonist containing the compound or a pharmaceutically acceptable acid addition salt thereof.

Sulfonamide derivative or pharmaceutically acceptable acid-addition salt

A morphinan derivative represented by the following general formula (I): wherein Rrepresents hydrogen, Calkyl, cycloalkylalkyl where the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms, etc.; Rrepresents heterocyclic ring containing 1 to 4 heteroatoms selected from N, O and S and at least one carbon atom as ring-constituting atoms, containing at least one set of adjacent ring-constituting atoms bound by a double bond, and further substituted with at least one oxo group; Y binds to a carbon atom as a ring-constituting atom of R; R, R, and Rrepresent hydrogen, hydroxy, etc.; Rand Rrepresent hydrogen, etc.; Rand Rrepresent hydrogen, etc.; Rand R, which are the same or different, represent hydrogen, etc.; X represents O or CH; and Y represents C(&#x2550;O)); a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt thereof, or a solvate thereof is used as an anxiolytic drug, antidepressant, etc.

Morphinan derivative

The present invention relates to a pharmaceutical composition comprising a morphinan derivative that exhibits an opioid &#x3b4; receptor agonist activity. By administering the pharmaceutical composition provided by the present invention, opioid &#x3b4; receptor-related diseases (for example, headache) can be treated or prevented.

Use of morphinan derivative for therapeutic treatment of opioid delta receptor agonist-related disease

A morphinan derivative represented by the following general formula (I): wherein Rrepresents hydrogen, Calkyl, cycloalkylalkyl where the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms, etc.; Rrepresents heterocyclic ring containing 1 to 4 heteroatoms selected from N, O and S and at least one carbon atom as ring-constituting atoms, containing at least one set of adjacent ring-constituting atoms bound by a double bond, and further substituted with at least one oxo group; Y binds to a carbon atom as a ring-constituting atom of R; R, R, and Rrepresent hydrogen, hydroxy, etc.; Rand Rrepresent hydrogen, etc.; Rand Rrepresent hydrogen, etc.; Rand Rio, which are the same or different, represent hydrogen, etc.; X represents O or CH; and Y represents C(&#x2550;O)); a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt thereof, or a solvate thereof is used as an anxiolytic drug, antidepressant, etc.

The present invention relates to a nalfurafine-containing percutaneous absorption patch having a support, a drug layer and a control layer which are laminated successively, wherein the drug layer contains at least one kind of a drug selected from the group consisting of nalfurafine and a salt thereof, and capable of maintaining a given level of drug skin permeation amount without permeation of an excess amount of the drug through the skin in a short time even when applied to the skin in which the horny cell layer and the like are damaged and the skin barrier is insufficient.

Nalfurafine-containing percutaneous absorption patch

A morphinan derivative represented by the following general formula (I): (wherein Rrepresents hydrogen, Calkyl, cycloalkylalkyl where the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms, etc.,

The purpose of the present invention is to provide a compound useful as a prophylactic or therapeutic agent for various diseases and symptoms related to orexin receptors, and a medical usage of the same. The present invention provides a morphinan derivative represented by the general formula (I) below or a pharmaceutically acceptable acid addition salt thereof, the morphinan derivative having excellent selectivity for and antagonism against orexin receptors and excellent therapeutic and prophylactic effects on drug dependence, and an orexin receptor antagonist and a therapeutic or prophylactic agent for drug dependence each containing it as an active ingredient. 

Morphinan derivative and medical usage thereof

The present invention aims to provide a novel low-molecular-weight compound exhibiting an orexin receptor agonist activity and expected to be useful as a prophylactic or therapeutic agent for narcolepsy and the like. The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the description, or a pharmaceutically acceptable acid addition salt thereof, which has an orexin receptor agonist activity, and an orexin receptor agonist containing the compound or a pharmaceutically acceptable acid addition salt thereof.

Sulfonamide derivative and pharmaceutically acceptable acid addition salt thereof

A morphinan derivative represented by the following formula (I), a tautomer or a stereoisomer of the compound, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a medicament, an analgesic and an antipruritic drug including the same as an active ingredient: wherein R is selected from hydrogen and Calkyl, and n represents an integer of 0 to 2.

The present invention aims to provide a novel low-molecular-weight compound having an orexin agonist activity, which is expected to be useful as a superior agent for the treatment or prophylaxis of narcolepsy. The present invention provides a compound showing superior orexin agonist activity which is represented by the formula (I) wherein each symbol is as defined in the DESCRIPTION, and a pharmaceutically acceptable acid addition salt thereof, as well as an orexin agonist containing the compound or a pharmaceutically acceptable acid addition salt thereof.

Sulfonamide derivative or pharmaceutically acceptable acid addition salt thereof

The present invention relates to a morphinan derivative represented by the following general formula (I), wherein Rrepresents hydrogen, Calkyl, Caryl, etc., Rand R, which are the same or different, represent hydrogen, hydroxy, etc., Rand Rrepresent hydrogen, Calkyl, etc., Rrepresents hydrogen, hydroxy, Calkyl, etc., X represents O or CH, Y represents C&#x2550;O, C(&#x2550;O)O, etc., and m and n, which are the same or different, represent an integer of 0 to 2 (m and n are not 0 at the same time), a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt thereof, or a solvate thereof, as well as an analgesic, antianxiety drug, etc. containing the same as an active ingredient. 

A morphinan derivative represented by the following general formula (I): 

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Ibaraki, Japan

Hiroshi Nagase