130311-72-7Relevant academic research and scientific papers
TRIAZOLO-1,4-DIAZEPINE DERIVATIVES AND THEIR USE IN PHARMACEUTICALS
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, (2008/06/13)
A triazolo-1,4-di-azepine compound of the below given formulas and a pharmacologically acceptable salt thereof are disclosed and useful in the pharmaceutical field, especially to allergic diseases. STR1 in which R1 and R2 are hydrogen or an alkyl, R3 is hydrogen or a halogen, R4 is hydrogen or an alkyl, X is--OCO--,--NHCO--,--CO--or others and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.
Structure-activity studies on triazolothienodiazepine derivatives as platelet-activating factor antagonists
Miyazawa,Okano,Shimomura,Clark,Kawahara,Asano,Yoshimura,Miyamoto,Sakuma,Muramoto,Obaishi,Harada,Kajima,Yamada,Tsunoda,Katayama,Abe,Asakawa,Souda,et al.
, p. 3215 - 3220 (2007/10/02)
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.
