138610-32-9

Upstream product

• 134290-58-7 2-(4'-Methoxyphenyl)-5,6-dihydro-(1)benzothiepino<5,4-c>pyridazin-3(2H)-one 
• 19501-58-7 4-methoxyphenylhydrazine hydrochloride 
• 118288-39-4 5-Oxo-2,3,4,5-tetrahydro-1-benzothiepin-4-acetic acid 
• 118258-07-4 2-(4'-Methoxyphenyl)-4,4a,5,6-tetrahydro-(1)benzothiepino<5,4-c>pyridazin-3(2H)-one 

Relevant academic research and scientific papers

Pharmaceutical composition with improved dissolution property

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

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.