118288-67-8Relevant articles and documents
Pharmaceutical composition with improved dissolution property
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, (2008/06/13)
Pharmaceutical compositions with improved dissolution property, which are obtained by mixing and pulverizing benzothiepino[5,4-c]pyridazine compounds represented by the formula with starch(es) derived from various plants and/or derivative(s) thereof at a weight ratio of 1:4 - 2:1, preferably 1:2 - 2:1, followed by addition of additives normally used for pharmaceutical preparations and formulation thereof into preparations are disclosed. The pharmaceutical compositions of the invention exhibit superior dissolution-improving effect accompanied by enhancement of the solubility of the Compound (I) per se as compared with that when the Compound alone is dissolved.
Studies on the synthesis of condensed pyridazine derivatives. IV. Synthesis and anxiolytic activity of 2-aryl-5,6-dihydro-(1)benzothiepino[5,4-c]pyridazin-3(2H)-ones and related compound
Nakao,Obata,Kawakami,Morita,Tanaka,Morimoto,Takehara,Yakushiji,Tahara
, p. 2556 - 2563 (2007/10/02)
A series of 2-aryl-5,6-dihydro-(1)benzothiepino[5,4-c]pyridazin-3(2H)-ones and related compounds were synthesized and evaluated for their ability to displace 3H-diazepam from rat brain membranes in vitro, and to prevent bicuculline induced convulsions in mice in vivo. Compounds with a 4'-methoxyphenyl (36) or 4'-chlorophenyl group (37, 39-42) as 2-aryl substituents showed prominent activities in both the in vitro and in vivo tests. Among them, 2-(4'-chlorophenyl)-5,6-dihydro- (37) and 2-(4'-chlorophenyl)-5,6-dihydro-10-fluoro-(1)benzothiepino[5,4-c]pyrida zin-3(2H)-one 7-oxides (41) showed activity twice as potent as diazepam in an anticonflict test (Vogel type, rats) while exhibiting less muscle relaxation (rotarod test, mice) and augmentation of γ-aminobutyric acid-induced chloride current (I(cl)) in isolated frog sensory neurones than diazepam. Compound 37 (Y-23684) was selected from this series as a candidate for further development. The structure-activity relationships are discussed.
Anti-anxiety benzothiepino(5,4-c]pyridazines
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, (2008/06/13)
A benzothiepino 5,4-c]pyridazine compound of the formula: STR1 wherein R 1 and R 2 are the same or different and each is hydrogen, halogen, trifluoromethyl, hydroxy, amino, nitro, cyano, C 1-4 alkyl, C 1-4 alkoxy, or C 2-5 alkanoylamino, R 3 is hydrogen,