Abstract:
Compounds having formula (I), wherein -OR comprises alkanoyl or the C-13 side-chain of paclitaxel; R , R , and R can be oxygenated or hydrogen in various combinations; and R and R are acyl groups, as well as a process for the preparation thereof, pharmaceutical compositions containing the above compounds, and a method for their use in inhibiting tumor growth.
Abstract translation:具有式(I)的化合物,其中-OR 1包含烷酰基或紫杉醇的C-13侧链; R 2,R 3和R 6可以以各种组合进行氧化或氢化; R 4和R 5为酰基,以及其制备方法,含有上述化合物的药物组合物及其抑制肿瘤生长的方法。
Abstract:
Disclosed are novel antifungal agents having formula (I) or a pharmaceutically acceptable acid, ester or prodrug thereof, wherein preferred compounds include those compounds wherein R1 is selected from the group consisting of -NH2; R2 is selected from the group consisting of hydrogen, fluoro, and hydroxyl; R3 is selected from the group consisting of -CH2(p-C6H4)3O(CH2)3CH3, -CH2(p-C6H4)O(CH2)6CH3, -COO(p-C6H4)O(CH2)6CH3, -CO(Piperazinyl)(p-C6H4)2OCH3, -CO(p-C6H4)O(CH2)6CH3, -CO(p-C6H4)(Piperazinyl)(p-C6H4)O(CH2)4CH3, -CO(p-C6H4)(Piperazinyl)(p-C6H4)O(CH2)6CH3, -CO(p-C6H4)(Piperazinyl)(p-C6H4)OCH3, and -CO(p-C6H4)(Piperazinyl)O(CH2)6CH3; et R4 is selected from the group consisting of -CH(OH)CH3, -CH2OH, -CH2CH3, -CH2CH2CH2NH2, -CH2(CH2)NH2, -CH2NH2, -CH2(CH2)2(NH)C=(NH)-NH2, -CH3, -CH2(Ph)OH, hydrogen, -CH2CH2COOH, and -CH2COOH. Also disclosed are pharmaceutical compositions containing such compounds and the use of the same in the treatment of fungal infections.
Abstract translation:公开了具有式(I)的新型抗真菌剂或其药学上可接受的酸,酯或前药,其中优选的化合物包括其中R 1选自-NH 2; R2选自氢,氟和羟基; R 3选自-CH 2(对-C 6 H 4)3 O(CH 2)3 CH 3,-CH 2(对-C 6 H 4)O(CH 2)6 CH 3,-COO(对-C 6 H 4)O(CH 2)6 CH 3,-CO( 哌嗪基)(对-C 6 H 4)2 OCH 3,-CO(p-C 6 H 4)O(CH 2)6 CH 3,-CO(p-C 6 H 4)(哌嗪基)(对-C 6 H 4)O(CH 2)4 CH 3,-CO(p-C 6 H 4) (哌嗪基)(p-C6H4)O(CH2)6CH3,-CO(对-C6H4)(哌嗪基)(对-C 6 H 4)OCH 3和-CO(对-C 6 H 4)(哌嗪基)O(CH 2) 其中R 4选自-CH(OH)CH 3,-CH 2 OH,-CH 2 CH 3,-CH 2 CH 2 CH 2 NH 2,-CH 2(CH 2)NH 2,-CH 2 NH 2,-CH 2(CH 2)2(NH)C =(NH) NH 2,-CH 3,-CH 2(Ph)OH,氢,-CH 2 CH 2 COOH和-CH 2 COOH。 还公开了含有这些化合物的药物组合物及其在治疗真菌感染中的用途。
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:
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:
Novel multicyclic erythromycin compounds and pharmaceutically acceptable salts and esters thereof having antibacterial activity having a formula selected from the group consisting of (I), (II), (III), (IV) and (V), compositions comprising a therapeutically eff ective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier, as well as a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically effective amount of a compound of formulas (I)-(V).
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:
Compounds having formula (I), wherein -OR1 comprises alkanoyl or the C-13 side-chain of paclitaxel; R?2, R3, and R6¿ can be oxygenated or hydrogen in various combinations; and R?4 and R5¿ are acyl groups, as well as a process for the preparation thereof, pharmaceutical compositions containing the above compounds, and a method for their use in inhibiting tumor growth.
Abstract:
Novel 6,11-bridged erythromycin compounds 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:
Compounds having formula (I), wherein -OR1 comprises alkanoyl or the C-13 side-chain of paclitaxel; R?2, R3, and R6¿ can be oxygenated or hydrogen in various combinations; and R?4 and R5¿ are acyl groups, as well as a process for the preparation thereof, pharmaceutical compositions containing the above compounds, and a method for their use in inhibiting tumor growth.
Abstract translation:具有式(I)的化合物,其中-OR 1包含紫杉醇的烷酰基或C-13侧链; R 2,R 3和R 6可以是各种组合的氧化或氢; R 4和R 5是酰基的化合物及其制备方法,含有上述化合物的药物组合物,以及它们用于抑制肿瘤生长的方法。
Abstract:
Novel 6,11-bridged erythromycin compounds 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.