Toray Industries, Inc.

Naoki Izumimoto

Katsuhiko Iseki

Yasuhiro Morita

Shunsuke Iwano

Shuji Udagawa

Koji Kawai

Toshikazu Komagata

Tomoya Miyoshi

Yuji Osada

Tadamasa Arai

Kei Takahashi

Hidenori Mochizuki

Kuniaki Kawamura

Yuji Sugawara

Motohiro Shiraki

Chihiro Yoshida

Hirozumi Takahashi

Tetsuro Koreeda

Hidetoshi Noda

Masanori Murakami

Yoko Baba

Keiyu Oshida

Hiroshi Nagabukuro

Tadatoshi Hashimoto

Hideyuki Tsutsui

Morihiro Fujimura

Eriko Higashi

Hideyuki Tsutsiu

Toshiyuki Honda

A crystal of ethane disulfonate of (S)-1-(4-(dimethylamino)piperidin-1-yl)-3-hydroxy-3-(1-methyl-1H-imidazol-2-yl)propan-1-one, having peaks at diffraction angles 2&#x3b8;)(&#xb0; of 12.6&#xb1;0.2, 16.0&#xb1;0.2, 17.7&#xb1;0.2, 18.5&#xb1;0.2, and 21.3&#xb1;0.2 in powder X-ray diffraction; and the crystal of ethane disulfonate of (S)-1-(4-(dimethylamino)piperi din-1-yl)-3-hydroxy-3-(1-methyl-1H-imidazol-2-yl)propan-1-one, having an endothermic peak at 173&#xb0; C. to 177&#xb0; C. in simultaneous thermogravimetric-differential thermal analysis.

Crystals of cyclic amine derivative and pharmaceutical use thereof

Crystals of a compound that exhibits an analgesic action against neuropathic pain and/or fibromyalgia syndrome are useful as pharmaceuticals. The crystals may be of (S)-1-(4-(dimethylamino)piperidin-1-yl)-3-hydroxy-3-(1-methyl-1H-imidazol-2-yl)propan-1-one or a pharmacologically acceptable salt thereof.

A cyclic amine derivative represented by a general formula (I) or a pharmacologically acceptable salt thereof: wherein n represents 1 or 3, Rrepresents an alkyl group having 1 to 6 carbon atoms unsubstituted, substituted with a halogen atom or substituted with an alkyloxy group having 1 to 4 carbon atoms and Rrepresents a hydrogen atom or a halogen atom.

Cyclic amine derivative and pharmaceutical use thereof

A compound exerts an analgesic effect against pain, in particular, neuropathic pain and/or fibromyalgia syndrome. A cyclic amine derivative represented by the following general formula, or a pharmacologically acceptable salt thereof:  Methods using the compound including the cyclic amine derivative or a pharmacologically acceptable salt thereof to treat pain, neuropathic pain and fibromyalgia syndrome.

A compound exerts a strong analgesic effect against pain, in particular, neuropathic pain and/or fibromyalgia syndrome. A cyclic amine derivative represented by general formula or a pharmacologically acceptable salt thereof:  A method of treating neuropathic pain includes administering a therapeutically effective amount of the cyclic amine derivative to a mammal. A method of treating fibromyalgia syndrome includes administering a therapeutically effective amount of the cyclic amine derivative to a mammal.

A compound exerts a strong analgesic effect against pain, in particular, neuropathic pain and/or fibromyalgia syndrome. The cyclic amine derivative is represented by formula, a prodrug thereof or a pharmacologically acceptable salt thereof: wherein A represents a group represented by Formula (IIa), (IIb) or (IIc): wherein

A method treats or prevents neuropathic pain with a synergistically-enhanced analgesic effect at a dose at which a calcium channel &#x3b1;2&#x3b4; ligand does not produce any side effects as well as which agent does not produce any new side effects on the central nervous system. The therapeutic agent or a prophylactic agent used in the method includes as effective ingredients a cyclohexane derivative or a pharmaceutically acceptable salt thereof or a prodrug thereof, and a calcium channel &#x3b1;2&#x3b4; ligand.

Methods of treating or preventing neuropathic pain

A therapeutic agent or a prophylactic agent for neuropathic pain provides a synergistically-enhanced analgesic effect at a dose at which a calcium channel &#x3b1;2&#x3b4; ligand does not produce any side effects as well as which agent does not produce any new side effects on the central nervous system. The therapeutic agent or a prophylactic agent for neuropathic pain includes as effective ingredients a cyclohexane derivative, represented by the following formula, or a pharmaceutically acceptable salt thereof or a prodrug thereof, and a calcium channel &#x3b1;2&#x3b4; ligand. 

Therapeutic agent or prophylactic agent for neuropathic pain

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

A method relieves both nociceptive pain and neuropathic pain and has fewer side effects. The compound includes cyclohexane derivatives represented by the following compound, or pharmaceutically acceptable salts thereof or prodrugs thereof. 

Cyclohexane derivative and pharmaceutical use thereof

A compound has a strong analgesic action against both nociceptive pain and neuropathic pain and has less side effects, and is medically useful. The compound includes cyclohexane derivatives represented by the following compound, or pharmaceutically acceptable salts thereof or prodrugs thereof. 

An antitussive, which can be used for therapy or prophylaxis of coughing, is disclosed. The antitussive comprises as an effective ingredient a morphinan derivative having a nitrogen-containing cyclic substituent or a pharmaceutically acceptable acid addition salt thereof, having a specific structure, such as the compound below [N-(17-cyclopeopylmethyl-4,5&#x3b1;-epoxy-3,14-dihydroxy-morphinan-6&#x3b2;-yl)-3,4,5,6-tetrahydrophthalimide]. The antitussive has an excellent therapeutic or prophylactic effect against coughing and the side effects thereof are small. 

Antitussive agent

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.

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Kamakura, Japan

Naoki Izumimoto