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1. 发明申请

WO2010062265A1 THERAPEUTIC MACROLIDE COMPOUNDS AND THEIR USE 审中-公开
标题翻译：治疗性大鼠化合物及其用途
公开(公告)号：WO2010062265A1
公开(公告)日：2010-06-03
申请号：PCT/SG2009/000446
申请日：2009-11-24
申请人： MERLION PHARMACEUTICALS PTE LTD , BOYCE, Rustum S. , SIHOMBING, Muhammad Sofian Asi , SONE, Hiroki
发明人： BOYCE, Rustum S. , SIHOMBING, Muhammad Sofian Asi , SONE, Hiroki
IPC分类号： C07D407/06 , A61K31/4427 , A61K31/551 , C07D413/14 , A61K31/365 , A61K31/4523 , A61K31/553 , A61K31/404 , A61K31/496 , A61P35/00 , A61K31/422 , A61K31/5377 , C07D407/14
CPC分类号： C07D407/06 , C07D403/14 , C07D405/14 , C07D413/14
摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain macrolide compounds (for convenience, collectively referred to herein as "MC compounds"), which, inter alia, are useful in treatment of cancer. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to treat proliferative conditions such as cancer, and in the treatment of diseases and conditions that are mediated by the regulation (e.g. inhibition) of cell proliferation, optionally in combination with another agent.
摘要翻译：本发明一般涉及治疗化合物的领域，更具体地涉及某些大环内酯类化合物（为方便起见，本文统称为“MC化合物”），其尤其可用于治疗癌症。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以治疗增殖性疾病如癌症，以及治疗由调节介导的疾病和病症（例如抑制）细胞增殖，任选与另一种试剂组合。

2. 发明申请

WO2010062264A1 LIPOPEPTIDE COMPOUNDS AND THEIR USE 审中-公开
标题翻译：利培酮化合物及其用途
公开(公告)号：WO2010062264A1
公开(公告)日：2010-06-03
申请号：PCT/SG2009/000444
申请日：2009-11-24
申请人： MERLION PHARMACEUTICALS PTE LTD , BOYCE, Rustum S. , CHERIAN, Joseph , CALANASAN, Cleofe , SIHOMBING, Muhammad Sofian Asi
发明人： BOYCE, Rustum S. , CHERIAN, Joseph , CALANASAN, Cleofe , SIHOMBING, Muhammad Sofian Asi
IPC分类号： C07K7/56 , A61K38/12 , A61P31/04
CPC分类号： C07K7/56 , A61K38/00
摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain lipopeptide compounds comprising a cyclic peptide bearing a lipid side chain (for convenience, collectively referred to herein as "LP compounds"), which, inter alia , are antimicrobial, particularly antibacterial. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to provide an antimicrobial function, particularly an antibacterial function, and in the treatment of diseases and conditions that are mediated by microbes, particularly bacteria, that are ameliorated by the antimicrobial function, particularly an antibacterial function, including bacterial diseases, optionally in combination with another agent, for example, another antibacterial agent.
摘要翻译：本发明一般涉及治疗化合物领域，更具体地涉及包含带有脂质侧链的环状肽（为了方便起见，统称为“LP化合物”）的某些脂肽化合物，其特别是抗微生物剂，特别是抗菌。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以提供抗微生物功能，特别是抗菌功能，以及用于治疗介导的疾病和病症特别是通过抗微生物功能改善的微生物，特别是细菌，特别是抗菌功能，包括细菌疾病，任选地与另一种试剂，例如另一种抗菌剂组合。

3. 发明申请

WO2008017840A1 CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE IN THE TREATMENT OF BACTERIAL INFECTIOUS DISEASES 审中-公开
标题翻译：环磷酰胆碱衍生物及其在治疗细菌性感染性疾病中的应用
公开(公告)号：WO2008017840A1
公开(公告)日：2008-02-14
申请号：PCT/GB2007/003017
申请日：2007-08-08
申请人： MERLION PHARMACEUTICALS SA , MERLION PHARMACEUTICALS PTE LTD , ORCHARD, Michael Glen , BENGHEZAL, Mohammed , BRAILLARD, Stéphanie , BURN, Christine , DEUSCHEL, Christine , LUCAS, Aurore , VALENTINO, Emilio , JANSSEN, Christian , BOYCE, Rustum S.
发明人： ORCHARD, Michael Glen , BENGHEZAL, Mohammed , BRAILLARD, Stéphanie , BURN, Christine , DEUSCHEL, Christine , LUCAS, Aurore , VALENTINO, Emilio , JANSSEN, Christian , BOYCE, Rustum S.
IPC分类号： C07C229/46 , C07C233/58 , C07C233/59 , C07C233/60 , C07C233/63 , C07C255/60 , C07C311/46 , C07D235/16 , C07D277/82 , C07D295/182 , A61K31/192 , A61K31/196 , A61K31/165 , A61K31/428 , A61K31/4453
CPC分类号： C07C233/60 , C07B2200/07 , C07C229/46 , C07C233/58 , C07C233/59 , C07C233/63 , C07C255/60 , C07C311/46 , C07C2601/08 , C07D235/16 , C07D235/30 , C07D277/82 , C07D295/182
摘要： The invention relates to cyclopentanecarboxylic acid derivatives and related compounds of formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are as described in the specification, processes for the preparation thereof, pharmaceutical compositions containing the same, the use thereof optionally in combination with one or more other pharmaceutically active compounds as anti-bacterial agents for the therapy of infective diseases, and a method for the treatment of such diseases. The compounds of formula (I) are reducing selectively the pathogenicity of bacteria within the host, but without affecting the bacteria outside the host environment.
摘要翻译：本发明涉及环戊烷羧酸衍生物及其相应的式（I）化合物，其中R 1，R 2，R 3，R 3， 4，R 5和R 6如说明书中所述，其制备方法，含有它们的药物组合物，其用途可任选地在与一种或多种其它药学活性化合物的组合作为用于治疗感染性疾病的抗细菌剂，以及治疗这些疾病的方法。式（I）化合物选择性地降低宿主细菌的致病性，但不影响宿主环境外的细菌。

4. 发明申请

WO2010025906A2 HYBRID ANTIMICROBIAL COMPOUNDS AND THEIR USE 审中-公开
标题翻译：混合抗微生物化合物及其用途
公开(公告)号：WO2010025906A2
公开(公告)日：2010-03-11
申请号：PCT/EP2009/006359
申请日：2009-09-02
申请人： MERLION PHARMACEUTICALS PTE LTD , LABISCHINSKI, Harald , CHERIAN, Joseph , CALANASAN, Cleofe , BOYCE, Rustum S.
发明人： LABISCHINSKI, Harald , CHERIAN, Joseph , CALANASAN, Cleofe , BOYCE, Rustum S.
CPC分类号： C07D239/49 , C07D401/12 , C07D471/04
摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain antimicrobial compounds comprising pharmacophores based on or comprising benzyl pyrimidines and 4-quinolones or 4H-4-oxoquinolizines (for convenience, collectively referred to herein as "BP-4Q compounds"), which, inter alia , are antimicrobial, particularly antibacterial. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo , to provide an antimicrobial function, particularly an antibacterial function, and in the treatment of diseases and conditions that are mediated by microbes, particularly bacteria, that are ameliorated by the antimicrobial function, particularly an antibacterial function, including bacterial diseases, optionally in combination with another agent, for example, another antibacterial agent.
摘要翻译：本发明一般涉及治疗化合物领域，更具体地涉及包含基于或包含苄基嘧啶和4-喹诺酮或4H-4-氧代喹诺嗪的药效团的某些抗微生物化合物（为方便起见，本文统称为“BP-4Q 化合物“），其尤其是抗微生物剂，特别是抗菌剂。本发明还涉及包含这种化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以提供抗微生物功能，特别是抗菌功能，以及用于治疗介导的疾病和病症特别是通过抗微生物功能改善的微生物，特别是细菌，特别是抗菌功能，包括细菌疾病，任选地与另一种试剂，例如另一种抗菌剂组合。

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