Nippon Chemiphar Co., Ltd.

Kinki University

Kohei Hayashida

Isao Ooi

Hideaki Fujii

Hiroshi Nagase

Eriko Nakata

Masaaki Hirose

Akiyoshi Saitoh

Daisuke Saito

Atsufumi Kawabata

Hiroto Tanaka

Toru Ogawa

Provided is, for example, a method for producing a morphinan derivative represented by General Formula (II), including the step of: allowing metal sodium and ethylenediamine to act on a morphinan derivative represented by General Formula (I) in presence of an auxiliary solvent.

Method for producing morphinan derivative

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 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.,

Growing community of inventors

Saitama, Japan

Kohei Hayashida