130312-24-2

Upstream product

• 32161-06-1 1-acetyl-4-piperidinone 
• 40018-25-5 2-Chlorobenzoyl acetonitrile 

Downstream Products

• 342884-10-0 3-[6-acetyl-3-(2-chloro-benzoyl)-4,5,6,7-tetrahydro-thieno[2,3-c]pyridin-2-yl]-1,1-diethyl-urea 
• 130311-70-5 6-acetyl-2-(2-bromopropionylamino)-3-(2-chlorobenzoyl)-4,5,6,7-tetrahydro-thieno<2,3-c>pyridine 
• 342884-03-1 cyclopropanecarboxylic acid [6-acetyl-3-(2-chloro-benzoyl)-4,5,6,7-tetrahydro-thieno[2,3-c]pyridin-2-yl]-amide 
• 342884-02-0 N-[6-acetyl-3-(2-chloro-benzoyl)-4,5,6,7-tetrahydro-thieno[2,3-c]pyridin-2-yl]-isobutyramide 
• 342884-04-2 N-[6-acetyl-3-(2-chloro-benzoyl)-4,5,6,7-tetrahydro-thieno[2,3-c]pyridin-2-yl]-2,2-dimethyl-propionamide 
• 130310-40-6 (-)-6-(2-chlorophenyl)-3-cyclopropanecarbonyl-8,11-dimethyl-2,3,4,5-tetrahydro-8H-pyrido<4',3':4,5>thieno<3,2-f><1,2,4>triazolo<4,3><1,4>-diazepine 
• 130310-40-6 (+)-6-(2-chlorophenyl)-3-cyclopropanecarbonyl-8,11-dimethyl-2,3,4,5-tetrahydro-8H-pyrido<4',3':4,5>thieno<3,2-f><1,2,4>triazolo<4,3><1,4>-diazepine 
• 130311-74-9 6-(2-chlorophenyl)-3-thioacetyl-8,11-dimethyl-2,3,4,5-tetrahydro-8H-pyrido<4',3':4,5>thieno<3,2-f><1,2,4>triazolo<4,3-a><1,4>diazepine 

Relevant academic research and scientific papers

Synthesis and bioactivities of novel 4,5,6,7-tetrahydrothieno[2,3-c]pyridines as inhibitors of tumor necrosis factor-alpha (TNF-alpha) production.

Novel 4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivatives were synthesized and evaluated for their abilities to inhibit lipopolysaccharide (LPS)-stimulated production of TNF-alpha in rat whole blood. Several of these compounds exhibited potent inhibitory activity.

Hetrazepine compounds which have useful pharmaceutical utility

The invention relates to new hetrazepines of general formula STR1 wherein A, Z, n, X, Y, R 1, R 2, R 3 and R 4 have the meanings given in the specification.The new compounds are intended for use in treating pathological conditions and diseases in which PAF (platelet activating factor) is implicated.

Structure-activity studies on triazolothienodiazepine derivatives as platelet-activating factor antagonists

A series of triazolodiazepines was synthesized and evaluated for anti-platelet activating factor (PAF) activities. Structure-activity relationship (SAR) studies on this series revealed that the introduction of a methyl group into the 8-position of the thienodiazepine nucleus can lead to a lengthening of the duration of action. Introduction of a methyl group produced an asymmetric center and the enantiomers so formed were separated with an optical resolving column. In the in vitro assay system, the (+)-isomers displayed 50-200 times more potent anti-PAF activity than the (-)-isomers. After comparison of toxicology and pharmacokinetics, (+)-6-(2-chlorophenyl)-3-cyclopropanecarbonyl-8,11-dimethyl-2,3,4,5-tet rahydro-8H-pyrido[4',3':4,5]thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]dia zepine (35(+)-isomer, E6123) was selected from among the compounds synthesized as a candidate for clinical study.