135206-76-7Relevant articles and documents
DIACYLGLYCEROL ACYLTRANSFERASE 2 INHIBITORS
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Page/Page column 110; 111, (2013/10/22)
Derivatives of purine, 3H-imidazo[4,5-b]pyrimidine and 1H- imidazo[4,5-d]pyrazine of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.
Pyrazolo-triazine derivatives as ligands for GABA receptors
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, (2008/06/13)
Compounds according to Formula (I): or a salt or prodrug thereof, have good affinity as ligands for the alpha2 and/or alpha3 subunit of the human GABAAreceptor and are useful for treatment of disorders of the central nervous system, including a
Optically active antifungal azoles. III. Synthesis and antifungal activity of sulfide and sulfonamide derivatives of (2R,3R)-2-(2,4-difluorophenyl)-3- mercapto-1-(1H-1,2,4-triazol-1-yl)-2-butanol
Tasaka,Teranishi,Matsushita,Tamura,Hayashi,Okonogi,Itoh
, p. 85 - 94 (2007/10/02)
In an effort to find potent antifungal agents, optically active sulfur- containing triazole derivatives, sulfides (3) and sulfonamides (4), were prepared and evaluated for antifungal activity against Candida albicans in vitro and in vivo. The sulfides (3) were prepared by the reaction of (2R,3R)- 2-(2,4-difluorophenyl)-3-mercapto-1-(1H-1,2,4-triazol-1-yl)-2-butanol (1) with various heteroarylmethyl chlorides in the presence of sodium methoxide. The sulfonamides (4) were synthesized starting from the disulfide (15) in three steps including oxidation of the corresponding sulfenamides (17). Some of the sulfur-containing triazole derivatives (3, 4) showed strong protective effects against candidosis in mice.
Heteroaryliumthio substituted carbapenem derivatives: Synthesis and in vitro activity of 1β-methyl-2-(dihydropyrrolotriazoliumthio)carbapenems
Wildonger,Ratcliffe
, p. 1866 - 1882 (2007/10/02)
The syntheses of five thiols, including three dihydropyrrolotriazoliumthiol salts, 1,4-dimethyl-5-mercaptomethyl-1,2,4-triazolium trifluoromethanesulfonate, and 6-mercapto-6,7-dihydro-5h-pyrazolo[1,2-a][1,2,4]triazolium chloride; and the addition of these thiols to 4-nitrobenzyl (IR,5R,6S)-2-(diphenylphosphono)oxy-6-[1(R)-hydroxyethyl]-1-methylcarbapen-2-cm -3-carboxylate and the subsequent hydrogenolysis of the addition products is described. The latter thiol provides a new route towards the preparation of L-627 (LJC 10,627). The compounds were evaluated in vitro against a panel of Gram-positive and Gram-negative bacteria and their antibacterial activities compared with imipenem. The compounds were measured for their hydrolytic stability to dehydropeptidase I (DHP-I) relative to imipenem. The five compounds generally had poorer Gram-positive and Pseudomonas activity than imipenem, although their Gram negative activity was variably improved. The monocyclic triazolium analog was nearly comparable in overall activity to the four bicyclic heterarylium analogs evaluated, including L-627 (LJC 10,627), All compounds were more stable to DHP-I than imipenem, although minor differences existed among them.
Substituted alkanediphosphonic acids and pharmaceutical use
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, (2008/06/13)
Alkanediphosphonic acids, in particular heteroarylalkanediphosphonic acids of formula STR1 wherein R1 is a 5-membered heteroaryl radical which may be fused with benzene or cyclohexene nuclei and which contains, as hetero atoms, 2 to 4 N-atoms or 1 or 2 N-atoms as well as 1 O- or S-atom, and which is unsubstituted or C-substituted by lower alkyl, phenyl or phenyl which is substituted by lower alkyl, lower alkoxy and/or halogen, or by lower alkoxy, hydroxy, di-lower alkylamino, lower alkylthio and/or halogen, and/or is N-substituted at a N-atom which is capable of substitution by lower alkyl, lower alkoxy and/or halogen, and R2 is hydrogen, hydroxy, amino, lower alkylthio or halogen, and salts thereof, have regulatory action on calcium metabolism and can be used as medicaments for the treatment of diseases associated with impairment of calcium metabolism. The compounds are obtained for example by converting, in a compound of formula STR2 wherein X1 is a functionally modified phosphono group and X2 is a free or functionally modified phosphono group, X1 and, if appropriate X2, into the free phosphono group.
1,2,4-TRIAZOLE-3,5-DIAMINE DERIVATIVES
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, (2008/06/13)
The invention relates to compounds of the formula (I) STR1 and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichR 1 and R 2 represent hydrogen, an aliphatic or cycloaliphatic group, or R 1 and R 2 together with the nitrogen atom form a 5 to 10 membered heterocyclic ring:Alk represents a straight or branched alkylene chain;Q represents furan, thiophen or benzene ring which is incorporated into the rest of the molecule; X represents--CH 2--, STR2--O--or--S--where R 6 represents hydrogen or methyl;n represents zero, 1 or 2; m represents 2, 3 or 4;R 3 represents hydrogen, a substituted or unsubstituted aliphatic or aryl group and;R 4 and R 5, which may be the same or different, each represent hydrogen, a substituted or unsubstituted aliphatic, aryl, or together with the nitrogen atom form a heterocyclic group.