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1. 发明申请

WO2011019618A1 BORON-CONTAINING SMALL MOLECULES AS ANTIPROTOZOAL AGENTS 审中-公开
标题翻译：含有BORON的小分子作为抗真菌剂
公开(公告)号：WO2011019618A1
公开(公告)日：2011-02-17
申请号：PCT/US2010/044787
申请日：2010-08-06
申请人： ANACOR PHARMACEUTICALS, INC. , CHEN, Daitao , ORR, Matthew , SLIGAR, Jessica , JACOBS, Robert , PLATTNER, Jacob, J.
发明人： CHEN, Daitao , ORR, Matthew , SLIGAR, Jessica , JACOBS, Robert , PLATTNER, Jacob, J.
IPC分类号： A61K31/69 , C07F5/02 , A61P33/02
CPC分类号： C07F5/025 , A01N55/08 , A61K31/69
摘要： This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent. The compounds have the following formula: wherein X is selected from the group consisting of substituted phenyl, substituted or unsubstituted heteroaryl and unsubstituted cycloalkyl; R 3a is selected from the group consisting of H1 unsubstituted C 1 or C 2 or C 3 or C 4 or C 5 or C 6 alkyl and unsubstituted C 3 or C 4 or C 5 or C 6 cycloalkyl; R 3b is selected from the group consisting of H, unsubstituted C 1 or C 2 or C 3 or C 4 or C 5 or C 6 alkyl and unsubstituted C 3 or C 4 or C 5 or C 6 cycloalkyl; with the proviso that R 3a and R 3b , along with the atom to which they are attached, are optionally joined to form a 3 or 4 or 5 or 6 membered ring, with the proviso that R 3a and R 3b cannot both be H, or a salt thereof.
摘要翻译：本发明尤其提供了可用于治疗原生动物感染的新化合物，含有这些化合物的药物组合物，以及这些化合物与至少一种另外的治疗有效药物的组合。所述化合物具有下式：其中X选自取代的苯基，取代或未取代的杂芳基和未取代的环烷基; R3a选自H1未取代的C1或C2或C3或C4或C5或C6烷基和未取代的C3或C4或C5或C6环烷基; R3b选自H，未取代的C1或C2或C3或C4或C5或C6烷基和未取代的C3或C4或C5或C6环烷基; 条件是R3a和R3b与它们所连接的原子一起任选地连接形成3或4或5或6元环，条件是R 3a和R 3b不能都是H，或其盐。

2. 发明申请

WO2010045505A1 BORON-CONTAINING SMALL MOLECULES AS ANTI-PROTOZOAL AGENTS 审中-公开
标题翻译：含有BORON的小分子作为抗真菌剂
公开(公告)号：WO2010045505A1
公开(公告)日：2010-04-22
申请号：PCT/US2009/060917
申请日：2009-10-15
申请人： ANACOR PHARMACEUTICALS, INC , ZHOU, Huchen , DING, Dazhong , FENG, Yiqing , YE, Long , JACOBS, Robert , ORR, Matthew , WRING, Stephen , CHEN, Daitao , HERNANDEZ, Vincent, S. , ZHANG, Yong-Kang , PLATTNER, Jacob, J.
发明人： ZHOU, Huchen , DING, Dazhong , FENG, Yiqing , YE, Long , JACOBS, Robert , ORR, Matthew , WRING, Stephen , CHEN, Daitao , HERNANDEZ, Vincent, S. , ZHANG, Yong-Kang , PLATTNER, Jacob, J.
IPC分类号： A61K31/69 , C07F5/02
CPC分类号： C07F5/025 , A61K31/69 , Y02A50/411 , Y02A50/415
摘要： This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
摘要翻译：本发明尤其提供了可用于治疗原生动物感染的新化合物，含有这些化合物的药物组合物，以及这些化合物与至少一种另外的治疗有效药物的组合。

3. 发明申请

WO2011116348A1 BORON-CONTAINING SMALL MOLECULES AS ANTI-PROTOZOAL AGENT 审中-公开
标题翻译：含有BORON的小分子作为抗真菌剂
公开(公告)号：WO2011116348A1
公开(公告)日：2011-09-22
申请号：PCT/US2011/029088
申请日：2011-03-18
申请人： ANACOR PHARMACEUTICALS, INC. , JACOBS, Robert, T. , CHEN, Daitao , ORR, Matthew , PLATTNER, Jacob, J.
发明人： JACOBS, Robert, T. , CHEN, Daitao , ORR, Matthew , PLATTNER, Jacob, J.
IPC分类号： A61K31/69 , C07F5/02 , A61P33/02
CPC分类号： A61K31/69 , C07F5/025 , C07F5/04
摘要： This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent. The compounds are of the formula, wherein Y' is a halogen, Y is halosubstituted alkyl, or a salt thereof.
摘要翻译：本发明尤其提供了可用于治疗原生动物感染的新化合物，含有这些化合物的药物组合物，以及这些化合物与至少一种另外的治疗有效药物的组合。化合物具有下式，其中Y'是卤素，Y是卤代烷基或其盐。

4. 发明申请

WO2010045503A1 BORON-CONTAINING SMALL MOLECULES AS ANTI-PROTOZOAL AGENTS 审中-公开
标题翻译：含硼的小分子作为抗原剂
公开(公告)号：WO2010045503A1
公开(公告)日：2010-04-22
申请号：PCT/US2009/060914
申请日：2009-10-15
申请人： ANACOR PHARMACEUTICALS, INC. , JACOBS, Robert , ORR, Matthew , WRING, Stephen , CHEN, Daitao , ZHOU, Huchen , DING, Dazhong , FENG, Yiqing , YE, Long , HERNANDEZ, Vincent, S. , ZHANG, Yong-Kang , PLATTNER, Jacob J.
发明人： JACOBS, Robert , ORR, Matthew , WRING, Stephen , CHEN, Daitao , ZHOU, Huchen , DING, Dazhong , FENG, Yiqing , YE, Long , HERNANDEZ, Vincent, S. , ZHANG, Yong-Kang , PLATTNER, Jacob J.
IPC分类号： A61K31/69 , C07F5/02
CPC分类号： C07F5/025 , A61K31/69 , Y02A50/409 , Y02A50/411 , Y02A50/414 , Y02A50/415
摘要： This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
摘要翻译：除其他之外，本发明提供了用于治疗原虫感染的新型化合物，含有这些化合物的药物组合物，以及这些化合物与至少一种另外的治疗有效药剂的组合。

5. 发明申请

WO2011019616A1 BORON-CONTAINING SMALL MOLECULES AS ANTIPROTOZOAL AGENTS 审中-公开
标题翻译：含有BORON的小分子作为抗真菌剂
公开(公告)号：WO2011019616A1
公开(公告)日：2011-02-17
申请号：PCT/US2010/044751
申请日：2010-08-06
申请人： ANACOR PHARMACEUTICALS, INC. , ORR, Matthew , JENKS, Matthew
发明人： ORR, Matthew , JENKS, Matthew
IPC分类号： A61K31/69 , C07F5/02 , A61P33/02
CPC分类号： A61K31/69
摘要： This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent. The compounds are of the following formula: wherein R 1 is a member selected from alkyl or aryl or heteroaryl, in which at least one substituent on said alkyl or said aryl or said heteroaryl is optionally substituted with a member selected from halogen, C 1 or C 2 or C 3 or C 4 or C 5 or C 6 unsubstituted alkyl, C 1 or C 2 or C 3 or C 4 or C 5 or C 6 unsubstituted alkoxy, halosubstituted C 1 or C 2 or C 3 or C 4 or C 5 or C 6 alkyl, halosubstituted C 1 or C 2 or C 3 or C 4 or C 5 or C 6 alkoxy, unsubstituted C 1 or C 2 or C 3 or C 4 or C 5 or C 6 alkylthio, unsubstituted phenyl; and X is aryl or heteroaryl, in which one substituent on said aryl or said heteroaryl is a member selected from halogen, unsubstituted C 1 or C 2 or C 3 or C 4 or C 5 or C 6 alkyl, unsubstituted C 1 or C 2 or C 3 or C 4 or C 5 or C 6 alkoxy, halosubstituted C 1 or C 2 or C 3 or C 4 or C 5 or C 6 alkyl, halosubstituted C 1 or C 2 or C 3 or C 4 or C 5 or C 6 alkoxy, unsubstituted C 1 or C 2 or C 3 or C 4 or C 5 or C 6 alkylthio, unsubstituted phenyl or a salt thereof.
摘要翻译：本发明尤其提供了可用于治疗原生动物感染的新化合物，含有这些化合物的药物组合物，以及这些化合物与至少一种另外的治疗有效药物的组合。所述化合物具有下式：其中R 1是选自烷基或芳基或杂芳基的成员，其中所述烷基或所述芳基或所述杂芳基上的至少一个取代基任选被选自卤素，C 1或C 2的成员或 C 3或C 4或C 5或C 6未取代的烷基，C 1或C 2或C 3或C 4或C 5或C 6未取代的烷氧基，卤素取代的C 1或C 2或C 3或C 4或C 5或C 6烷基，卤素取代的C 1或C 2或C 3或C 4或C 5或C 6烷氧基，未取代的C1或C2或C3或C4或C5或C6烷硫基，未取代的苯基; 并且X是芳基或杂芳基，其中所述芳基或所述杂芳基上的一个取代基是选自卤素，未取代的C1或C2或C3或C4或C5或C6烷基，未取代的C1或C2或C3或C4或C5或C6 烷氧基，卤素取代的C1或C2或C3或C4或C5或C6烷基，卤素取代C1或C2或C3或C4或C5或C6烷氧基，未取代的C1或C2或C3或C4或C5或C6烷硫基，未取代的苯基或其盐。

6. 发明申请

WO2011019612A1 BORON-CONTAINING SMALL MOLECULES AS ANTIPROTOZOAL AGENTS 审中-公开
标题翻译：含有BORON的小分子作为抗真菌剂
公开(公告)号：WO2011019612A1
公开(公告)日：2011-02-17
申请号：PCT/US2010/044727
申请日：2010-08-06
申请人： ANACOR PHARMACEUTICALS, INC. , ORR, Matthew , JENKS, Matthew
发明人： ORR, Matthew , JENKS, Matthew
IPC分类号： A61K31/69 , C07F5/02 , A61P33/02
CPC分类号： C07F5/025
摘要： This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent. The compounds are of formula (I), wherein Z is S or O; and X is selected from the group consisting of substituted phenyl, substituted or unsubstituted heteroaryl, and unsubstituted cycloalkyl, or a salt thereof.
摘要翻译：本发明尤其提供了可用于治疗原生动物感染的新化合物，含有这些化合物的药物组合物，以及这些化合物与至少一种另外的治疗有效药物的组合。化合物为式（I），其中Z为S或O; 并且X选自取代的苯基，取代或未取代的杂芳基和未取代的环烷基，或其盐。

7. 发明公开

EP2155204A1 ANDROSTANE AND PREGNANE STEROIDS WITH POTENT ALLOSTERIC GABA RECEPTOR CHLORIDE IONOPHORE MODULATING PROPERTIES 有权
标题翻译：雄甾烷和PREGNANSTEROID与调制GABA受体氯离子载体的有效性能
公开(公告)号：EP2155204A1
公开(公告)日：2010-02-24
申请号：EP08771137.0
申请日：2008-06-16
申请人： Cook, Kevin M. , Runyon, Scott P. , Rogawski, Michael , Kepler, John , Navarro, Hernan , Kaminski, Rafal , Orr, Matthew
发明人： RUNYON, Scott, P. , ROGAWSKI, Michael , KEPLER, John , NAVARRO, Hernan , KAMINSKI, Rafal , ORR, Matthew
IPC分类号： A61K31/56 , A61P25/02
CPC分类号： C07J41/0005 , C07J7/00 , C07J31/003
摘要： This invention describes compounds of Structures 1, 2, and 3 and their use as allosteric modulators of the GABA receptor chloride ionophore complex to alleviate stress, anxiety, mood disorders, seizures, depression, treatment of drug and alcohol abuse, memory, premenstrual disorders, and neural system damage.

8. 发明申请

WO2008157460A1 ANDROSTANE AND PREGNANE STEROIDS WITH POTENT ALLOSTERIC GABA RECEPTOR CHLORIDE IONOPHORE MODULATING PROPERTIES 审中-公开
标题翻译：安非他酮和前列腺素与耐药性GABA受体氯离子离子调节特性
公开(公告)号：WO2008157460A1
公开(公告)日：2008-12-24
申请号：PCT/US2008/067059
申请日：2008-06-16
申请人： COOK, Kevin, M. , RUNYON, Scott, P. , ROGAWSKI, Michael , KEPLER, John , NAVARRO, Hernan , KAMINSKI, Rafal , ORR, Matthew
发明人： RUNYON, Scott, P. , ROGAWSKI, Michael , KEPLER, John , NAVARRO, Hernan , KAMINSKI, Rafal , ORR, Matthew
IPC分类号： A61K31/56 , A61P25/02
CPC分类号： C07J41/0005 , C07J7/00 , C07J31/003
摘要： This invention describes compounds of Structures 1, 2, and 3 and their use as allosteric modulators of the GABA receptor chloride ionophore complex to alleviate stress, anxiety, mood disorders, seizures, depression, treatment of drug and alcohol abuse, memory, premenstrual disorders, and neural system damage.
摘要翻译：本发明描述了结构1,2和3的化合物及其作为GABA受体氯离子载体复合物的变构调节剂的用途，以缓解压力，焦虑，情绪障碍，癫痫发作，抑郁症，药物和酒精滥用的治疗，记忆，经前期障碍，和神经系统损伤。

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