Nippon Chemiphar Co., Ltd.

The Kitasato Institute

Eriko Nakata

Hiroshi Nagase

Hideaki Fujii

Masaaki Hirose

Isao Ooi

Kohei Hayashida

Akiyoshi Saitoh

Toshihiro Takahashi

Yoshikazu Watanabe

Daisuke Saito

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

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.

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 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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Saitama, Japan

Eriko Nakata