427885-95-8Relevant articles and documents
Discovery of a novel bicyclic compound, DS54360155, as an orally potent analgesic without mu-opioid receptor agonist activity
Arita, Tsuyoshi,Asano, Masayoshi,Kubota, Kazufumi,Domon, Yuki,Machinaga, Nobuo,Shimada, Kousei
supporting information, (2019/11/11)
We synthesized derivatives of a natural alkaloid, conolidine, and evaluated these derivatives in the acetic acid-induced writhing test and formalin test in ddY mice after oral administration. As a result, we identified (5S)-6-methyl-1,3,4,5,6,8-hexahydro-7H-2,5-methano[1,5]diazonino[7,8-b]indol-7-one sulfate salt, 15a (DS54360155), with a unique and original bicyclic skeleton, as an analgesic more potent than conolidine. Moreover, 15a did not exhibit mu-opioid receptor agonist activity.
ERYTHROPOIETIN PRODUCTION ACCELERATOR
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Page/Page column 19, (2008/06/13)
The present invention relates to a preventive or therapeutic agent for pathological conditions caused by reduced production of erythropoietin, or for anemia, or for chronic anemia, renal anemia, aplastic anemia, or pure red cell aplasia, the agent comprising, as an active ingredient, a cyclic amine compound represented by the following formula (1): wherein, ???R1, R2 and R3 each independently represent a hydrogen atom, a halogen atom, or hydroxy, alkyl, halogen-substituted alkyl, alkoxy, alkylthio, carboxyl, alkoxycarbonyl or alkanoyl group; ???W1 and W2 each independently represent N or CH; ???X represents O, NR4, CONR4 or NR4CO; ???R4 each represents a hydrogen atom, or an alkyl, alkenyl, alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aralkyl, or substituted or unsubstituted heteroaralkyl group; and ???l, m and n each represents a number of 0 or 1, or a salt thereof or a solvate thereof.
Cyclic amine compounds and pharmaceutical composition containing the same
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, (2008/06/13)
A cyclic amine compound by the following general formula (1): wherein, R1, R2and R3each independently represent a hydrogen atom or an alkoxy group W1and W2each independently represent N or CH; X represents O, NR4, CONR4or NR4CO; R4represents a hydrogen atom, or an alkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl group; and l, m and n each represents a number of 0 or 1, a salt thereof and a hydrate thereof are provided. These compounds have inhibitory effects on both cell adhesion and cell infiltration and are useful as anti-asthmatic agents, anti-allergic agents, anti-rheumatic agents, anti-arteriosclerotic agents, anti-inflammatory agents, anti-Sjogren's syndrome agents or the like.