117279-73-9

Usage

InChI:InChI=1/C28H29ClN4S/c1-17(2)15-21-11-9-20(10-12-21)13-14-22-16-24-26(23-7-5-6-8-25(23)29)30-18(3)27-32-31-19(4)33(27)28(24)34-22/h5-12,16-18H,13-15H2,1-4H3/t18-/m1/s1

Upstream product

• 78-39-7 Triethyl orthoacetate 
• 117280-40-7 [5-(2-Chloro-phenyl)-7-[2-(4-isobutyl-phenyl)-ethyl]-3-methyl-1,3-dihydro-thieno[2,3-e][1,4]diazepin-(2Z)-ylidene]-hydrazine 
• 147598-20-7 4-(4-Isobutyl-phenyl)-butan-1-ol 
• 73120-67-9 4-(4-isobutylphenyl)-4-oxobutanoic acid 
• 538-93-2 1-phenyl-2-methylpropane 
• 127113-12-6 (+/-)-N-{3-(2-chlorobenzoyl)-5-[2-(4-isobutylphenyl)ethyl]-2-thienyl}-2-phthalimidopropanamide 
• 117280-38-3 5-(2-Chloro-phenyl)-7-[2-(4-isobutyl-phenyl)-ethyl]-3-methyl-1,3-dihydro-thieno[2,3-e][1,4]diazepin-2-one 
• 117280-39-4 5-(2-Chloro-phenyl)-7-[2-(4-isobutyl-phenyl)-ethyl]-3-methyl-1,3-dihydro-thieno[2,3-e][1,4]diazepine-2-thione 
• 127113-13-7 (+/-)-2-amino-N-{3-(2-chlorobenzoyl)-5-[2-(4-isobutylphenyl)ethyl]-2-thienyl}propionamide 
• 117280-04-3 2-amino-3-(2-chlorobenzoyl)-5-(2-(4-isobutylphenyl)ethyl)thiophene 
• 1041514-31-1 4-(4'-s-butylphenyl)butanoic acid 
• 117280-05-4 4-(4-isobutylphenyl)butyraldehyde 

Relevant academic research and scientific papers

Structural optimization of 4-(2-chlorophenyl)-9-methyl-6H-thieno [3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepines as antagonists for platelet activating factor: Pharmacological contribution of substituents at the 2- and 6-positions of a condensed ring system

A series of 4-(2-chlorophenyl)-9-methyl-6H-thieno [3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine derivatives bearing substituents at the 2- and 6-positions were synthesized, and evaluated in vitro for their inhibitory activity on rabbit platelet aggregation induced by platelet activating factor (PAF) and in vivo for their preventing effect on PAF-induced mortality in mice. The length of alkyl or arylalkyl side chain at the 2-position was responsible for enhancing the affinity for the PAF receptor. The simultaneous substitution at both the 2- and 6-positions resulted in a successful separation of the affinity for the PAF receptor from that for the benzodiazepine (BZ) receptor. Thus, (±)-4-(2-chlorophenyl)-2-[2-(4-isobutylphenyl)ethyl]- 6,9-dimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4] diazepine (Y-24180) was confirmed to be a specific antagonist for the PAF receptor and is currently under clinical trials.

Optically active thienotriazolodiazepine compounds

Stable crystals of an acid addition salt of an optically active thienotriazolodiazepine compound or its hydrate of the formula STR1 wherein R1 is hydrogen, R2 is 2-phenylethyl substituted by alkyl having 1 to 5 carbon atoms, 2-morpholinocarbonylethyl or alkyl having 6 to 12 carbon atoms, or R1 and R2 may combinedly form a saturated 5-membered ring having one substituent selected from the group consisting of morpholinomethyl, morpholinocarbonyl and N,N-dipropylcarbamoyl, R3 is halogen, alkyl having 1 to 5 carbon atoms or alkoxy having 1 to 5 carbon atoms, R4 is trifluoromethyl or alkyl having 1 to 5 carbon atoms, R5 is hydrogen or methyl, m is 1-2, and n is 0-2. The present invention provides optically active thienotriazolodiazepine compounds having strong PAF-antagonistic activity as markedly stable crystals which are excellent in crystalline property, permit purification by recrystallization, and have high chemical purity and optical purity, thereby rendering industrial large-scale synthesis attainable. In addition, crystallization thereof facilitates medicinal standardization and pharmaceutical formulation.

PAF-antagonistic thienotriazolodiazepine compounds and pharmaceutical uses thereof

A thienotriazolodiazepine compound of the formula: STR1 wherein A is alkylene or substituted alkylene and each other symbol is as defined in the specification and a pharmaceutically acceptable acid addition salt thereof, and pharmaceutical uses thereof.Sa