CAS: 117279-73-9; 4-(2-Chlorophenyl)-2-(4-Isobutylphenethyl)-6,9-Dimethyl-6H-Thieno[3,2-F][1,2,4]Triazolo[4,3-A][1,4]Diazepine

上下游产品

[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 117280-40-7
5-(2-Chloro-Phenyl)-7-[2-(4-Isobutyl-Phenyl)-Ethyl]-3-Methyl-1,3-Dihydro-Thieno[2,3-E][1,4]Diazepine-2-Thione 117280-39-4
5-(2-Chloro-Phenyl)-7-[2-(4-Isobutyl-Phenyl)-Ethyl]-3-Methyl-1,3-Dihydro-Thieno[2,3-E][1,4]Diazepin-2-One 117280-38-3
(+/-)-N-{3-(2-Chlorobenzoyl)-5-[2-(4-Isobutylphenyl)Ethyl]-2-Thienyl}-2-Phthalimidopropanamide 127113-12-6
(+/-)-2-Amino-N-{3-(2-Chlorobenzoyl)-5-[2-(4-Isobutylphenyl)Ethyl]-2-Thienyl}Propionamide 127113-13-7

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参考文献: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
标题: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
摘要: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.
Doi:10.1016/0223-5234(96)85877-6

专利信息

专利号:US-2022233673-A1
优先权日:2019-06-04
标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF
发明人：BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M
权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND
摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.

专利号:US-5286858-A
优先权日:1990-10-12
标 题 :Optically active thienotriazolodiazepine compounds
发明人：MORIWAKI MINORU; YUASA SYUJI; KITANI HIROYUKI; TERASAWA MICHIO
权利人:YOSHITOMI PHARMACEUTICAL
摘要:Stable crystals of an acid addition salt of an optically active thienotriazolodiazepine compound or its hydrate of the formula ##STR1## wherein R 1 is hydrogen, R 2 is 2-phenylethyl substituted by alkyl having 1 to 5 carbon atoms, 2-morpholinocarbonylethyl or alkyl having 6 to 12 carbon atoms, or R 1 and R 2 may combinedly form a saturated 5-membered ring having one substituent selected from the group consisting of morpholinomethyl, morpholinocarbonyl and N,N-dipropylcarbamoyl, R 3 is halogen, alkyl having 1 to 5 carbon atoms or alkoxy having 1 to 5 carbon atoms, R 4 is trifluoromethyl or alkyl having 1 to 5 carbon atoms, R 5 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.