Abstract:
4''-Deoxy derivatives of erythromycin having formula (I) and pharmaceutically acceptable salts thereof, which are enhancers of gastric motility but have minimal antibacterial activity, as well as pharmaceutical compositions containing the same and methods for their use and preparation.
Abstract:
Antibacterial compounds are disclosed having the formula and pharmaceutically acceptable salts thereof, wherein R1 is -NR4R6, where R4 and R6 are independently selected from the group consisting of hydrogen, loweralkyl and arylalkyl or, together, R4 and R6 form a nitrogen-containing heterocycle attached at the nitrogen atom; R2 is selected from the group consisting of hydrogen, -OH and, when R3 is methylene, oxygen so as to form an epoxide; and R3 is selected from the group consisting of -CH2OH, -NR4R6, -(CH2)nNR4R6 and, when R2 is oxygen, methylene so as to form an epoxide, where n is 1-4 and R4 and R6 are as previously defined, with the proviso that when R2 is -OH, R3 may not be -NR4R6; or R2 and R3 together are=CH2. Also disclosed are processes and intermediates useful in the preparation of the above compounds, as well as compositions containing the same and methods for their use.
Abstract:
Novel macrocyclic 13-membered ring-contracted compounds derived from erythromycins A and B having formula (I) and pharmaceutically acceptable salts thereof, wherein R, R , R , R and X are specifically defined, having use in treating gastrointestinal disorders associated with hypermotilinemia, pharmaceutical compositions thereof, a method of treating gastrointestinal disorders associated with hypermotilinemia with said pharmaceutical compositions, and processes for the preparation thereof.
Abstract:
Novel antifungal agents having formula (I), wherein R is hydrogen or -C(O)-R1 wherein R1 is alkenyl, C2-C12-alkyl, aryl, arylalkenyl, arylalkyl, aryl-aryl-, arylalkoxy-aryl-, aryloxyl-aryl-, aryl-aryl-aryl- or arylalkoxy-aryl-aryl-, or pharmaceutically acceptable salts, esters or prodrugs thereof, as well as (i) pharmaceutical compositions comprising such compounds, (ii) methods of treatment using such compounds, and (iv) methods and fungal cultures useful in making the same.
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:
Antibacterial compounds having formula (II) and pharmaceutically acceptable salts thereof, wherein Y is selected form (a), (b), and (c) and X is selected from the group consisting of -C(O)-, -C(S)-, CH2-, -CH2CH2- and -C(CH3)2-; also disclosed are processes and intermediates useful in the preparation of the above compounds, as well as compositions containing the same and methods for their use.
Abstract:
Antibacterial compounds are disclosed having the formula and pharmaceutically acceptable salts thereof, wherein R1 is -NR4R6, where R4 and R6 are independently selected from the group consisting of hydrogen, loweralkyl and arylalkyl or, together, R4 and R6 form a nitrogen-containing heterocycle attached at the nitrogen atom; R2 is selected from the group consisting of hydrogen, -OH and, when R3 is methylene, oxygen so as to form an epoxide; and R3 is selected from the group consisting of -CH2OH, -NR4R6, -(CH2)nNR4R6 and, when R2 is oxygen, methylene so as to form an epoxide, where n is 1-4 and R4 and R6 are as previously defined, with the proviso that when R2 is -OH, R3 may not be -NR4R6; or R2 and R3 together are=CH2. Also disclosed are processes and intermediates useful in the preparation of the above compounds, as well as compositions containing the same and methods for their use.
Abstract:
Novel macrocyclic 13-membered ring-contracted compounds derived from erythromycins A and B having formula (I) and pharmaceutically acceptable salts thereof, wherein R, R , R , R and X are specifically defined, having use in treating gastrointestinal disorders associated with hypermotilinemia, pharmaceutical compositions thereof, a method of treating gastrointestinal disorders associated with hypermotilinemia with said pharmaceutical compositions, and processes for the preparation thereof.
Abstract:
Novel antifungal agents having formula (I), wherein R is hydrogen or -C(O)-R1 wherein R1 is alkenyl, C2-C12-alkyl, aryl, arylalkenyl, arylalkyl, aryl-aryl-, arylalkoxy-aryl-, aryloxyl-aryl-, aryl-aryl-aryl- or arylalkoxy-aryl-aryl-, or pharmaceutically acceptable salts, esters or prodrugs thereof, as well as (i) pharmaceutical compositions comprising such compounds, (ii) methods of treatment using such compounds, and (iv) methods and fungal cultures useful in making the same.
Abstract:
Novel macrocyclic 13-membered ring-contracted compounds derived from erythromycins A and B having formula (I) and pharmaceutically acceptable salts thereof, wherein R, R?1, R2, R3¿ and X are specifically defined, having use in treating gastrointestinal disorders associated with hypermotilinemia, pharmaceutical compositions thereof, a method of treating gastrointestinal disorders associated with hypermotilinemia with said pharmaceutical compositions, and processes for the preparation thereof.