Abstract:
A process for the preparation of chiral 3-aminopyrrolidine of formula (I) and analogous bicyclic derivatives of formula (II) from dihydroxy olefins such as for the formula: HO-CH2-CH=CH-CH2-OAr by treatment with titanium isopropoxide, an optically active tartrate ester and tert-butyl hydroperoxide, followed by subsequent alkylation of the intermediate with an alkyl or alkenyl magnesium halide, then pyrrolidine ring formation by condensation with an arylmethylamine, subsequent chiral replacement of a ring hydroxyl group with an amino group with further protection thereof, optional additional substitution closing of the second ring, and hydrogenolysis to remove a ring-nitrogen protecting group.
Abstract:
Antimicrobial compounds having formula (II), (III), (IV), (IV-A) or (V) as well as pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compunds.
Abstract:
Antimicrobial compounds having formula (II), (III), (IV), (V), (VI), (VII), (VIII) and (IX) as well as the pharmaceutically acceptable salts, esters and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
Abstract:
Antibacterial compounds having formula (I) and the pharmaceutically acceptable salts, esters and amides thereof, selected preferred examples of which include those compounds wherein A is =CR -; R is cycloalkyl of from three to eight carbon atoms or substituted phenyl; R is selected from the group consisting of (a), (b), (c) and (d); R is halogen; R is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group; R is hydrogen, loweralkyl, halo(loweralkyl), or -NR R ; and R is halogen, loeralkyl, halo(loweralkyl), hydroxy-substituted loweralkyl, loweralkoxy(loweralkyl), loweralkoxy, or amino(loweralkyl), as well as pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.
Abstract translation:具有式(I)的抗菌化合物及其药学上可接受的盐,酯和酰胺,其选择的优选实例包括其中A = CR 6 - 的那些化合物; R 1是3至8个碳原子的环烷基或取代的苯基; R 2选自(a),(b),(c)和(d); R 3是卤素; R 4是氢,低级烷基,药学上可接受的阳离子或前药酯基; R 5是氢,低级烷基,卤代(低级烷基)或-NR 13 R 14; 和R 6是卤素,低级烷基,卤代(低级烷基),羟基取代的低级烷基,低级烷氧基(低级烷基),低级烷氧基或氨基(低级烷基),以及含有这些化合物的药物组合物及其在治疗中的用途 的细菌感染。
Abstract:
A process for preparing substituted 7-(piperazin-1-yl)-4-oxo-1,4-dihydro-3-quinoline carboxylic acid derivative antibacterial agents by reacting a carbamate protected piperazine derivative with a 7-halo-4-oxo-1,4-dihydro-quinoline carboxylic acid derivative.
Abstract:
A process for the preparation of a compound having formula (a) wherein R?1, R2, R3, R4, and R5¿ are defined, from an enamine by chain expansion and ring closure followed by additional derivatization, treatment with a 3-alkoxyl-acryloyl compound, another ring closure, and converting a hydroxyl group to a leaving group.
Abstract:
Novel 2-halo-6-O-substituted ketolide derivatives and pharmaceutically acceptable salts and esters thereof having antibacterial activity having formula (I) or (II), compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier, a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention, and processes for their preparation.
Abstract:
Antimicrobial compounds having formula (II), (III), (IV), (IV-A) or (V) as well as pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compunds.
Abstract:
Antimicrobial compounds having formula (II), (III), (IV), (V), (VI), (VII), (VIII) and (IX) as well as the pharmaceutically acceptable salts, esters and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
Abstract:
L'invention se rapporte à de la quinobenzoxazine, des quinobenzothiazines et des dérivés de pyrido-acridine, représentés par la formule (I), ainsi qu'à leurs sels, esters, amides, et pro-médicaments pharmaceutiquement acceptables. Dans la formule (I), R1 représente hydrogène ou un groupe protecteur de carboxy, R2 et R3 représentent des substituants, A représente oxygène, soufre ou carbone, Z représente un halogène ou un groupe contenant de l'azote, X représente hydrogène, halogène ou alkyle, et W représente hydrogène, alkyle, amino ou halogène. Ces composés ont un pouvoir antinéoplastique puissant.