Toray Industries, Inc.

Toshikazu Komagata

Naoki Izumimoto

Koji Kawai

Kuniaki Kawamura

Hiroshi Nagabukuro

Tadatoshi Hashimoto

Motohiro Shiraki

Masahiro Akimoto

Morihiro Fujimura

Akihiro Ando

Toshiyuki Honda

An analgesic which may be applied to wide variety of pain from various causes is disclosed. The analgesic comprises as an effective ingredient a specific morphinan derivative having a nitrogen containing heterocyclic group, such as compound 1: 

Analgesic and methods of treating pain

Crystalline particles of N-(17-cyclopropylmethyl-4,5&#x3b1;-epoxy-3,14-dihydroxy-morphinan-6&#x3b2;-yl)-phthalimide or a pharmaceutically acceptable salt thereof are disclosed. The crystalline particles have a particle diameter distribution in which a particle diameter (D50) at the point where cumulative frequency of volume distribution cumulatively calculated from particles having a smaller diameter reaches 50% is within a range of 1 to 30 &#x3bc;m, and a particle diameter (D90) at the point where cumulative frequency of volume distribution cumulatively calculated from particles having a smaller diameter reaches 90% is not more than 90 &#x3bc;m, which crystalline particles have a degree of crystallinity of not less than 80%. By the crystalline particles, bioavailability of the active substance may be increased while ensuring storage stability of the compound.

Crystalline micropowder particles

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

Growing community of inventors

Kamakura, Japan

Toshikazu Komagata