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1. 发明申请

US20100234348A1 COMPOSITIONS AND METHODS FOR POTENTIATING ANTIBIOTIC ACTIVITY 审中-公开
标题翻译：潜在的抗生素活性的组合物和方法
公开(公告)号：US20100234348A1
公开(公告)日：2010-09-16
申请号：US12376288
申请日：2007-08-02
申请人： Guillaume Cottarel , Timothy S. Gardner , Xiaoguang Lei , John Porco , Scott E. Schaus , Jamey Wierzbowski , Kollol Pal
发明人： Guillaume Cottarel , Timothy S. Gardner , Xiaoguang Lei , John Porco , Scott E. Schaus , Jamey Wierzbowski , Kollol Pal
IPC分类号： A61K31/4035 , C07D405/08 , C07D487/04 , C07D498/06 , C07C69/00 , C07D231/56 , A61K31/5025 , A61K31/553 , A61K31/22 , A61K31/416 , C12Q1/18 , C12Q1/68 , A61P31/00
CPC分类号： C07D405/04 , C07B2200/07 , C07C69/14 , C07D231/56 , C07D241/44 , C07D261/16 , C07D277/74 , C07D307/68 , C07D311/16 , C07D311/30 , C07D311/32 , C07D405/06 , C07D487/04 , C07D495/04 , C07J63/008 , C12Q1/18
摘要： The present invention provides compounds that potentiate the activity of antibiotic agents, particularly quinolones such as norflaxin. The invention further provides compositions, e.g., pharmaceutical compositions, comprising the inventive compounds. The invention also provides compositions comprising an antibiotic (e.g., a quinolone) and a compound that potentiates activity of the antibiotic. The invention further provides methods of treating a subject comprising administering any of the inventive compounds or compositions to the subject. The invention also provides screening methods to identify compounds that potentiate the activity of an antibiotic, e.g., a quinolone.
摘要翻译：本发明提供了增强抗生素剂，特别是喹诺酮类如诺氟沙星的活性的化合物。本发明还提供包含本发明化合物的组合物，例如药物组合物。本发明还提供包含抗生素（例如喹诺酮）和增强抗生素活性的化合物的组合物。本发明还提供了治疗受试者的方法，包括向受试者施用任何本发明化合物或组合物。本发明还提供了鉴定增强抗生素例如喹诺酮活性的化合物的筛选方法。

2. 发明申请

US20100029597A1 RECA INHIBITORS WITH ANTIBIOTIC ACTIVITY, COMPOSITIONS AND METHODS OF USE 有权
标题翻译：具有抗生物活性的RECA抑制剂，组合物和使用方法
公开(公告)号：US20100029597A1
公开(公告)日：2010-02-04
申请号：US12279243
申请日：2007-02-13
申请人： Guillaume Cottarel , Jamey Wierzbowski , Kollol Pal , Michael Kohanski , Daniel Dwyer , James Collins , Michael Almstetter , Michael Thormann , Andreas Treml
发明人： Guillaume Cottarel , Jamey Wierzbowski , Kollol Pal , Michael Kohanski , Daniel Dwyer , James Collins , Michael Almstetter , Michael Thormann , Andreas Treml
IPC分类号： A61K31/65 , A61K31/352 , A61K31/382 , A61K31/47 , A61P31/04
CPC分类号： A61K45/06 , A61K38/12 , C12Q1/18 , G01N33/5023 , A61K2300/00
摘要： The present invention is directed to the use of RecA inhibitors as antibiotic agents, and provides RecA inhibitors useful in treating infections. Also provided are various compositions and methods associated with RecA inhibition.
摘要翻译：本发明涉及使用RecA抑制剂作为抗生素，并提供可用于治疗感染的RecA抑制剂。还提供了与RecA抑制相关的各种组合物和方法。

3. 发明申请

US20090264342A1 COMPOSITIONS AND METHODS FOR ANTIBIOTIC POTENTIATION AND DRUG DISCOVERY 审中-公开
标题翻译：用于抗生素和药物发现的组合物和方法
公开(公告)号：US20090264342A1
公开(公告)日：2009-10-22
申请号：US12279237
申请日：2007-02-13
申请人： Guillaume Cottarel , Jamey Wierzbowski , Kollol Pal , Michael Kohanski , Daniel Dwyer , James Collins , Michael Almstetter , Michael Thormann , Andreas Treml
发明人： Guillaume Cottarel , Jamey Wierzbowski , Kollol Pal , Michael Kohanski , Daniel Dwyer , James Collins , Michael Almstetter , Michael Thormann , Andreas Treml
IPC分类号： A61K38/00 , C12Q1/68 , C12N5/02 , A61K31/70 , A61K31/435 , A61K31/352
CPC分类号： A61K45/06 , A61K38/12 , C12Q1/18 , G01N33/5023 , A61K2300/00
摘要： The present invention provides methods for identifying target genes whose partial or complete functional inactivation potentiates the activity of an antibiotic agent, e.g., a quinolone antibiotic. The invention further provides methods for identifying agents that modulate expression of target genes or that modulate activity of expression products of target genes. Agents identified according to various methods of the invention potentiate the activity of antibiotics such as quinolones, aminoglycosides, peptide antibiotics and β-lactams. Also provided are agents that suppress and/or retard resistance to antibiotics. The inventive methods provide potentiating agents and compositions comprising potentiating agents and antibiotics. Such agents and compositions can be used for inhibiting growth or survival of a microbial cell or of treating a subject suffering from or susceptible to a microbial infection.
摘要翻译：本发明提供用于鉴定其部分或完全功能失活增强抗生素试剂例如喹诺酮抗生素活性的靶基因的方法。本发明还提供用于鉴定调节靶基因表达或调节靶基因表达产物的活性的试剂的方法。根据本发明各种方法鉴定的药剂增强了抗生素如喹诺酮类，氨基糖苷类，肽类抗生素和β-内酰胺类的活性。还提供了抑制和/或延缓抗生素抗性的药剂。本发明的方法提供增效剂和包含增效剂和抗生素的组合物。这些药剂和组合物可用于抑制微生物细胞的生长或存活或治疗患有或易受微生物感染的受试者。

4. 发明授权

US09155792B2 RecA inhibitors with antibiotic activity, compositions and methods of use 有权
标题翻译：具有抗生素活性的RecA抑制剂，组合物和使用方法
公开(公告)号：US09155792B2
公开(公告)日：2015-10-13
申请号：US12279243
申请日：2007-02-13
申请人： Guillaume Cottarel , Jamey Wierzbowski , Kollol Pal , Michael Kohanski , Daniel Dwyer , James Collins , Michael Almstetter , Michael Thormann , Andreas Treml
发明人： Guillaume Cottarel , Jamey Wierzbowski , Kollol Pal , Michael Kohanski , Daniel Dwyer , James Collins , Michael Almstetter , Michael Thormann , Andreas Treml
IPC分类号： A61K49/00 , C07H19/16 , A61K38/00 , A61K45/06 , A61K38/12 , C12Q1/18 , G01N33/50
CPC分类号： A61K45/06 , A61K38/12 , C12Q1/18 , G01N33/5023 , A61K2300/00
摘要： The present invention is directed to the use of RecA inhibitors as antibiotic agents, and provides RecA inhibitors useful in treating infections. Also provided are various compositions and methods associated with RecA inhibition.
摘要翻译：本发明涉及使用RecA抑制剂作为抗生素，并提供可用于治疗感染的RecA抑制剂。还提供了与RecA抑制有关的各种组合物和方法。

5. 发明申请

US20100028334A1 COMPOSITIONS AND METHODS TO POTENTIATE COLISTIN ACTIVITY 审中-公开
标题翻译：组合物和方法来降低COLISTIN活性
公开(公告)号：US20100028334A1
公开(公告)日：2010-02-04
申请号：US12519336
申请日：2007-12-13
申请人： Guillaume Cottarel , Jamey Wierzbowski
发明人： Guillaume Cottarel , Jamey Wierzbowski
IPC分类号： A61K38/12 , A01N37/00 , A61K39/395 , A61P31/04 , C12Q1/68
CPC分类号： A61K31/16 , A61K31/47 , A61K38/12 , A61K45/06 , G01N2500/10 , Y02A50/401 , Y02A50/402 , Y02A50/469 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/48 , Y02A50/481 , A61K2300/00
摘要： A pharmaceutical composition comprising an antimicrobial agent and an enhancer of an antimicrobial agent, wherein the enhancer of an antimicrobial agent is an inhibitor of gene, that by inactivating the gene product potentiates the effectiveness of the antimicrobial agent. In some embodiments, the pharmaceutical composition further comprises a pharmaceutically acceptable carrier. In some embodiments, the antimicrobial agent is an antimicrobial peptide such as a polymyxin, for example but not limited to colistin. In some embodiments of the present invention provides methods to treat and/or prevent infection of a subject with a microorganism by administering a pharmaceutical composition comprising an antimicrobial agent and an enhancer of an antimicrobial agent. In some embodiments, the present invention provides methods to inhibit growth of a microorganism by administering a pharmaceutical composition comprising an antimicrobial agent and an enhancer of an antimicrobial agent.
摘要翻译：一种药物组合物，其包含抗微生物剂和抗微生物剂的增强剂，其中所述抗微生物剂的增强剂是基因抑制剂，通过灭活所述基因产物来增强所述抗微生物剂的有效性。在一些实施方案中，药物组合物还包含药学上可接受的载体。在一些实施方案中，抗微生物剂是抗微生物肽，例如多粘菌素，例如但不限于粘菌素。在本发明的一些实施方案中，提供了通过施用包含抗微生物剂和抗微生物剂增强剂的药物组合物来治疗和/或预防用微生物感染受试者的方法。在一些实施方案中，本发明提供了通过施用包含抗微生物剂和抗微生物剂增强剂的药物组合物来抑制微生物生长的方法。

6. 发明申请

US20050059803A1 Immunosuppressant target proteins 审中-公开
标题翻译：免疫抑制剂靶蛋白
公开(公告)号：US20050059803A1
公开(公告)日：2005-03-17
申请号：US10877320
申请日：2004-06-24
申请人： Vivian Berlin , Maria Chiu , Guillaume Cottarel , Veronique Damagnez
发明人： Vivian Berlin , Maria Chiu , Guillaume Cottarel , Veronique Damagnez
IPC分类号： G01N33/53 , C07K14/40 , C07K14/47 , C07K16/18 , C12N1/19 , C12N1/21 , C12N9/00 , C12N9/12 , C12N15/09 , C12N15/12 , C12N15/31 , C12N15/62 , C12N15/81 , C12P21/02 , C12Q1/25 , C12Q1/68 , G01N33/566 , G01N33/68 , G01N33/94 , C07K14/74
CPC分类号： G01N33/5091 , A01K2217/05 , C07K14/40 , C07K14/4702 , C07K2319/00 , C12N9/1205 , C12N9/93 , C12Q1/25 , C12Q1/6883 , C12Q1/6897 , C12Q2600/158 , G01N33/5005 , G01N33/5008 , G01N33/5011 , G01N33/502 , G01N33/68 , G01N33/6845 , G01N33/9493 , G01N2500/00
摘要： The present invention relates to the discovery of novel proteins of mammalian origin which are immediate downstream targets for FKBP/rapamycin complexes.
摘要翻译：本发明涉及哺乳动物来源的新型蛋白质的发现，其是FKBP /雷帕霉素复合物的即时下游靶标。

7. 发明授权

US06251585B1 Assay and reagents for identifying anti-proliferative agents 失效
标题翻译：用于鉴定抗增殖剂的测定和试剂
公开(公告)号：US06251585B1
公开(公告)日：2001-06-26
申请号：US08428762
申请日：1995-04-24
申请人： Giulio Draetta , Guillaume Cottarel , Veronique Damagnez
发明人： Giulio Draetta , Guillaume Cottarel , Veronique Damagnez
IPC分类号： C12Q168
CPC分类号： G01N33/5011 , C12N9/16
摘要： The present invention makes available assays and reagents for identifying anti-proliferative agents, such as mitotic and meiotic inhibitors. The present assay provides a simple and rapid screening test which relies on scoring for positive cellular proliferation as indicative of anti-mitotic or anti-meiotic activity, and comprises contacting a candidate agent with a cell which has an impaired cell-cycle checkpoint and measuring the level of proliferation in the presence and absence of the agent. The checkpoint impairment is such that it either causes premature progression of the cell through at least a portion of a cell-cycle or inhibition of normal progression of the cell through at least a portion of a cell-cycle, but can be off-set by the action of an agent which inhibits at least one regulatory protein of the cell-cycle in a manner which counter-balances the effect of the impairment.
摘要翻译：本发明提供用于鉴定抗增殖剂（如有丝分裂和减数分裂抑制剂）的测定和试剂。本测定提供了一种简单快速的筛选试验，其依赖于阳性细胞增殖的评分作为抗有丝分裂或抗减数分裂活性的指示，并且包括使候选试剂与具有受损的细胞周期检查点的细胞接触并测量药剂存在和不存在时的增殖水平。检查点受损使得其通过细胞周期的至少一部分或者通过细胞周期的至少一部分抑制细胞的正常进展来导致细胞过早进展，但是可以通过抑制细胞周期的至少一种调节蛋白的药物的作用，其以抵消该损伤的作用的方式。

8. 发明授权

US06068982A Ubiquitin conjugating enzymes 失效
标题翻译：泛素缀合酶
公开(公告)号：US06068982A
公开(公告)日：2000-05-30
申请号：US767942
申请日：1996-12-17
申请人： Mark Rolfe , Maria Isabel Chiu , Guillaume Cottarel , Vivian Berlin , Veronique Damagnez , Giulio Draetta
发明人： Mark Rolfe , Maria Isabel Chiu , Guillaume Cottarel , Vivian Berlin , Veronique Damagnez , Giulio Draetta
IPC分类号： G01N33/48 , C07K16/40 , C12N9/00 , C12N15/00 , C12N15/09 , C12Q1/25 , C12Q1/68 , C12R1/91 , G01N33/53 , G01N33/68
CPC分类号： G01N33/6842 , C12N9/93 , C12Q1/25 , G01N33/68 , A01K2217/05
摘要： The present invention relates to drug screening assays which provide a systematic and practical approach for the identification of candidate agents able to inhibit ubiquitin-mediated degradation of a cell-cycle regulatory protein, such as p53, p27, myc, fos, MAT.alpha.2, or cyclins. The invention further relates to novel ubiquitin-conjugating enzymes, and uses related thereto.
摘要翻译：本发明涉及药物筛选测定法，其提供了用于鉴定能够抑制泛素介导的细胞周期调节蛋白如p53，p27，myc，fos，MATα2等的降解的候选试剂的系统和实用的方法。或细胞周期蛋白。本发明还涉及新的泛素结合酶及其相关用途。

9. 发明授权

US06509152B1 Immunosuppressant target proteins 失效
标题翻译：免疫抑制剂靶蛋白
公开(公告)号：US06509152B1
公开(公告)日：2003-01-21
申请号：US09012399
申请日：1998-01-23
申请人： Vivian Berlin , Maria Isabel Chiu , Guillaume Cottarel , Veronique Damagnez
发明人： Vivian Berlin , Maria Isabel Chiu , Guillaume Cottarel , Veronique Damagnez
IPC分类号： C12Q168
CPC分类号： G01N33/5091 , A01K2217/05 , C07K14/40 , C07K14/4702 , C07K2319/00 , C12N9/1205 , C12N9/93 , C12Q1/25 , C12Q1/6883 , C12Q1/6897 , C12Q2600/158 , G01N33/5005 , G01N33/5008 , G01N33/5011 , G01N33/502 , G01N33/68 , G01N33/6845 , G01N33/9493 , G01N2500/00
摘要： The present invention relates to the discovery of novel proteins of mammalian origin which are immediate downstream targets for FKBP/rapamycin complexes.
摘要翻译：本发明涉及哺乳动物来源的新型蛋白质的发现，其是FKBP /雷帕霉素复合物的即时下游靶标。

10. 发明授权

US5968761A Ubiquitin conjugating enzymes 失效
公开(公告)号：US5968761A
公开(公告)日：1999-10-19
申请号：US486663
申请日：1995-06-07
申请人： Mark Rolfe , Maria Isabel Chiu , Guillaume Cottarel , Vivian Berlin , Veronique Damagnez , Giulio Draetta
发明人： Mark Rolfe , Maria Isabel Chiu , Guillaume Cottarel , Vivian Berlin , Veronique Damagnez , Giulio Draetta
IPC分类号： G01N33/48 , C07K16/40 , C12N9/00 , C12N15/00 , C12N15/09 , C12Q1/25 , C12Q1/68 , C12R1/91 , G01N33/53 , G01N33/68 , C12Q1/48 , C12N9/10
CPC分类号： G01N33/6842 , C12N9/93 , C12Q1/25 , G01N33/68 , A01K2217/05
摘要： The present invention relates to drug screening assays which provide a systematic and practical approach for the identification of candidate agents able to inhibit ubiquitin-mediated degradation of a cell-cycle regulatory protein, such as p53, p27, myc, fos, MAT.alpha.2, or cyclins. The invention further relates to novel ubiquitin-conjugating enzymes, and uses related thereto.

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