4''-DEOXYERYTHROMYCIN DERIVATIVES
    1.
    发明申请
    4''-DEOXYERYTHROMYCIN DERIVATIVES 审中-公开
    4“ - 脱氧葡萄糖衍生物

    公开(公告)号:WO1993013780A1

    公开(公告)日:1993-07-22

    申请号:PCT/US1993000468

    申请日:1993-01-19

    CPC classification number: C07H17/08

    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 translation: 4' - 具有式(I)的红霉素的脱氧衍生物及其药学上可接受的盐,其是胃动力的增强剂但具有最小的抗菌活性,以及​​含有其的药物组合物及其使用和制备方法。

    ERYTHROMYCIN DERIVATIVES
    2.
    发明申请
    ERYTHROMYCIN DERIVATIVES 审中-公开
    红霉素衍生物

    公开(公告)号:WO1992019247A1

    公开(公告)日:1992-11-12

    申请号:PCT/US1992002891

    申请日:1992-04-09

    CPC classification number: A61K31/70 C07H17/08 Y02A50/473

    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.

    MACROCYCLIC 13-MEMBERED RING DERIVATIVES OF ERYTHROMYCINS A AND B
    3.
    发明申请
    MACROCYCLIC 13-MEMBERED RING DERIVATIVES OF ERYTHROMYCINS A AND B 审中-公开
    红霉素A和B的大环13-环状衍生物

    公开(公告)号:WO1997048713A1

    公开(公告)日:1997-12-24

    申请号:PCT/US1997007015

    申请日:1997-04-25

    CPC classification number: C07H17/08

    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 translation: 衍生自具有式(I)的红霉素A和B的新型大环13-环收缩的化合物及其药学上可接受的盐,其中R 1,R 2,R 3,R 3和X是具体定义的,其具有 用于治疗与高肌钙蛋白血症相关的胃肠道疾病,其药物组合物,用所述药物组合物治疗与高肌醇酐血症相关的胃肠道疾病的方法及其制备方法。

    ANTIFUNGAL FUSACANDINS
    4.
    发明申请
    ANTIFUNGAL FUSACANDINS 审中-公开
    抗真菌FUSACANDINS

    公开(公告)号:WO1996021670A2

    公开(公告)日:1996-07-18

    申请号:PCT/US1996000225

    申请日:1996-01-03

    CPC classification number: C07H15/10 A01N43/16

    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 translation: 具有式(I)的新型抗真菌剂,其中R是氢或-C(O)-R1,其中R 1是烯基,C 2 -C 12 - 烷基,芳基,芳基烯基,芳基烷基,芳基 - 芳基 - ,芳基烷氧基 - 芳基 - ,芳氧基 - 芳基 - ,芳基 - 芳基 - 芳基 - 或芳基烷氧基 - 芳基 - 芳基 - 或其药学上可接受的盐,酯或前药,以及(i)包含这些化合物的药物组合物,(ii)使用这些化合物的治疗方法, (iv)有用的方法和真菌培养物。

    AMINO-LIPOPEPTIDE ANTIFUNGAL AGENTS
    5.
    发明申请
    AMINO-LIPOPEPTIDE ANTIFUNGAL AGENTS 审中-公开
    氨基磷脂抗真菌药物

    公开(公告)号:WO1998006745A1

    公开(公告)日:1998-02-19

    申请号:PCT/US1997014053

    申请日:1997-08-11

    CPC classification number: C07K7/56 A61K38/00

    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。

    ERYTHROMYCIN DERIVATIVES
    6.
    发明申请
    ERYTHROMYCIN DERIVATIVES 审中-公开
    红霉素衍生物

    公开(公告)号:WO1995001794A1

    公开(公告)日:1995-01-19

    申请号:PCT/US1994007575

    申请日:1994-07-06

    CPC classification number: C07H17/08

    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 translation: 具有式(II)的抗菌化合物及其药学上可接受的盐,其中Y选自(a),(b)和(c)形式,X选自-C(O) - , - C ) - ,CH 2 - , - CH 2 CH 2 - 和-C(CH 3)2 - ; 还公开了可用于制备上述化合物的方法和中间体,以及含有该化合物的组合物及其使用方法。

    ERYTHROMYCIN DERIVATIVES
    7.
    发明公开
    ERYTHROMYCIN DERIVATIVES 失效
    红霉素。

    公开(公告)号:EP0583414A1

    公开(公告)日:1994-02-23

    申请号:EP92913526.0

    申请日:1992-04-09

    CPC classification number: A61K31/70 C07H17/08 Y02A50/473

    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.

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