Nippon Chemiphar Co., Ltd.

Kinki University

Isao Ooi

Masaaki Hirose

Hiroshi Nagase

Eriko Nakata

Kohei Hayashida

Hideaki Fujii

Akiyoshi Saitoh

Atsufumi Kawabata

Hiroto Tanaka

Toru Ogawa

Tsuyoshi Endo

Yuzo Mogi

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 compound represented by the following General Formula (I), a tautomer or a stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof, is used as a voltage-dependent T-type calcium channel blocker: 

Voltage-dependent t-type calcium channel blocker

A compound represented by General Formula (I), a tautomer, a stereoisomer, or a pharmaceutically acceptable salt of the compound, or a solvate thereof is used as a voltage-dependent T-type calcium channel inhibitor, 

Voltage-dependent T-type calcium channel inhibitor

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.,

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Saitama, Japan

Isao Ooi