- Crystals of morphinan derivative, manufacturing method thereof, and pharmaceutical composition using the same
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The present invention relates to a X-form crystal of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan hydrochloride and the manufacturing method thereof, wherein the X-form crystal of the compound has char
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- Design, synthesis, and structure-activity relationship of novel opioid κ-agonists
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By focusing on 4,5-epoxymorphinan, a traditional opioid skeleton but a new structure in the opioid κ-agonist research field, and by rationally applying the 'message-address concept' and 'accessory site hypothesis,' we discovered a new chemical class opioid κ-agonist, TRK-820 (1). Its development as an antipruritus is now in the final stage. Here, the full scope of its design, synthesis, and structure-activity relationship are described.
- Kawai, Koji,Hayakawa, Jun,Miyamoto, Toru,Imamura, Yoshifumi,Yamane, Shinichi,Wakita, Hisanori,Fujii, Hideaki,Kawamura, Kuniaki,Matsuura, Hirotoshi,Izumimoto, Naoki,Kobayashi, Ryosuke,Endo, Takashi,Nagase, Hiroshi
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experimental part
p. 9188 - 9201
(2009/04/06)
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- CRYSTALS OF MORPHINAN DERIVATIVE AND PROCESS FOR PRODUCING THE SAME
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The present invention is directed to provide 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan hydrochloride consistent in quality after production and having high purity. A crystal of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan hydrochloride including a A-form, B-form or C-form crystal thereof, and a process for producing the same are provided.
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Page/Page column 5; 6
(2008/06/13)
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