2-Halo-6-O-substituted ketolide derivatives
    2.
    发明授权
    2-Halo-6-O-substituted ketolide derivatives 失效
    2-卤代-6-O-取代的酮内酯衍生物

    公开(公告)号:US6124269A

    公开(公告)日:2000-09-26

    申请号:US154294

    申请日:1998-09-16

    IPC分类号: C07H17/08 A61K31/70

    CPC分类号: A61K31/7048 C07H17/08

    摘要: Novel 2-halo-6-O-substituted ketolide derivatives and pharmaceutically acceptable salts and esters thereof having antibacterial activity having a formula ##STR1## 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.

    摘要翻译: 具有抗菌活性的新型2-卤代-6-O-取代的酮内酯衍生物及其药学上可接受的盐和酯,其具有包含治疗有效量的本发明化合物与药学上可接受的载体的组合物的组合物,治疗细菌的方法 通过向哺乳动物施用含有治疗有效量的本发明化合物的药物组合物及其制备方法的感染。

    Anti-bacterial activity of 9-hydroxy derivatives of 6,11-bicyclolides
    3.
    发明授权
    Anti-bacterial activity of 9-hydroxy derivatives of 6,11-bicyclolides 有权
    6,11-双环氯化物的9-羟基衍生物的抗细菌活性

    公开(公告)号:US08383785B2

    公开(公告)日:2013-02-26

    申请号:US12437616

    申请日:2009-05-08

    摘要: The present invention discloses compounds of formula (I) or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit superior antibacterial properties, particularly against Haemophilus influenzae. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

    摘要翻译: 本发明公开了式(I)化合物或其药学上可接受的盐,酯或前药:其表现出优异的抗菌性,特别是抗流感嗜血杆菌。 本发明还涉及包含上述化合物的药物组合物,用于给予需要抗生素治疗的受试者。 本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的细菌感染的方法。 本发明还包括制备本发明化合物的方法。

    Processes for the preparation of O-[5-(4-amino-thiazol-2-yl)-pyridin-2-ylmethyl]-hydroxylamine
    4.
    发明授权
    Processes for the preparation of O-[5-(4-amino-thiazol-2-yl)-pyridin-2-ylmethyl]-hydroxylamine 有权
    制备O- [5-(4-氨基 - 噻唑-2-基) - 吡啶-2-基甲基] - 羟胺的方法

    公开(公告)号:US07842813B2

    公开(公告)日:2010-11-30

    申请号:US12437636

    申请日:2009-05-08

    IPC分类号: C07D417/04

    CPC分类号: C07D417/04

    摘要: The present invention relates generally to novel methods for the synthesis of O-[5-(4-amino-thiazol-2-yl)-pyridin-2-ylmethyl]-hydroxylamine which is an essential reagent in the synthesis of one of the bridged erythromycin derivatives and their respective pharmaceutically acceptable salts in PCT Application WO 03/097659 A1. In particular, the present invention relates to processes and intermediates for the preparation of a compound of formula (Ia):

    摘要翻译: 本发明一般涉及合成O- [5-(4-氨基 - 噻唑-2-基) - 吡啶-2-基甲基] - 羟胺的新方法,其是合成桥接的 红霉素衍生物及其各自的药学上可接受的盐在PCT申请WO 03/097659 A1中。 特别地,本发明涉及制备式(Ia)化合物的方法和中间体:

    USE OF BRIDGED MACROLIDES OR TYLOSIN DERIVATIVES IN TREATING INFLAMMATORY BOWEL DISEASES
    6.
    发明申请
    USE OF BRIDGED MACROLIDES OR TYLOSIN DERIVATIVES IN TREATING INFLAMMATORY BOWEL DISEASES 审中-公开
    桥梁加强剂或酪氨酸衍生物在治疗炎症性皮肤病中的应用

    公开(公告)号:US20090131343A1

    公开(公告)日:2009-05-21

    申请号:US12270967

    申请日:2008-11-14

    IPC分类号: A61K31/7048 A61P1/00

    CPC分类号: A61K31/70

    摘要: The invention provides methods utilizing bridged macrolide or tylosin derivatives for the treatment of patients with inflammatory bowel diseases. The methods of the invention provide for the administration to a patient of a therapeutically effective amount of a bridged macrolide or a tylosin derivative, pharmaceutically acceptable derivatives thereof, and combinations thereof for a period of time sufficient to obtain a desired alleviation of one or more symptoms of the inflammatory bowel disease.

    摘要翻译: 本发明提供了利用桥联大环内酯或泰乐菌素衍生物治疗炎症性肠病患者的方法。 本发明的方法提供给予患者治疗有效量的桥联大环内酯或泰乐菌素衍生物,其药学上可接受的衍生物及其组合足以获得所需缓解一种或多种症状的时间 的炎性肠病。

    Bicyclic 9a-azalide derivatives
    7.
    发明授权
    Bicyclic 9a-azalide derivatives 失效
    双环9a-azalide衍生物

    公开(公告)号:US07402568B2

    公开(公告)日:2008-07-22

    申请号:US11236043

    申请日:2005-09-27

    IPC分类号: A61K31/70 C07H17/08

    CPC分类号: C07H17/08

    摘要: The present invention discloses compounds of formulae I and II, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

    摘要翻译: 本发明公开了式I和II的化合物或其药学上可接受的盐,酯或前药:其表现出抗菌性质。 本发明还涉及包含上述化合物的药物组合物,用于给予需要抗生素治疗的受试者。 本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的细菌感染的方法。 本发明还包括制备本发明化合物的方法。

    6-11 bicyclic ketolide derivatives
    8.
    发明授权
    6-11 bicyclic ketolide derivatives 有权
    6-11双环酮内酯衍生物

    公开(公告)号:US07189704B2

    公开(公告)日:2007-03-13

    申请号:US11154260

    申请日:2005-06-16

    IPC分类号: A61K31/70 C07H17/08

    摘要: The present invention discloses, inter alia, a compound of the following formula, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the aforementioned compounds. The invention further includes processes by which to make the compounds of the present invention.

    摘要翻译: 本发明尤其公开了下式的化合物或其药学上可接受的盐,酯或前药:其表现出抗菌性质。 本发明还涉及包含上述化合物的药物组合物,用于给予需要抗生素治疗的受试者。 本发明还涉及通过施用包含上述化合物的药物组合物来治疗受试者的细菌感染的方法。 本发明还包括制备本发明化合物的方法。

    Bicyclic macrolide derivatives
    9.
    发明授权
    Bicyclic macrolide derivatives 失效
    双环大环内酯衍生物

    公开(公告)号:US06790835B1

    公开(公告)日:2004-09-14

    申请号:US10455219

    申请日:2003-06-05

    IPC分类号: A61K3170

    CPC分类号: C07H17/08

    摘要: The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

    摘要翻译: 本发明公开了式I化合物或其药学上可接受的盐,酯或前药:其表现出抗菌性质。 本发明还涉及包含上述化合物的药物组合物,用于给予需要抗生素治疗的受试者。 本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的细菌感染的方法。 本发明还包括制备本发明化合物的方法。

    Tylosin derivatives having antibacterial activity
    10.
    发明授权
    Tylosin derivatives having antibacterial activity 失效
    泰乐菌素衍生物具有抗菌活性

    公开(公告)号:US06664240B2

    公开(公告)日:2003-12-16

    申请号:US10002918

    申请日:2001-11-15

    IPC分类号: A61K3170

    CPC分类号: C07H17/08

    摘要: There are described novel substituted tylosin analogs and pharmaceutically acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier. Also described is 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 the preparation of such compounds.

    摘要翻译: 描述了新型取代的泰乐菌素类似物和药学上可接受的组合物,其包含治疗有效量的本发明化合物与药学上可接受的载体的组合。 还描述了一种通过向哺乳动物施用含有治疗有效量的本发明化合物的药物组合物及其制备方法来治疗细菌感染的方法。