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1. 发明授权

US08772330B2 Inhibitor(s) of transporters or uptake of monoaminergic neurotransmitters 有权
标题翻译：转运蛋白的抑制剂或单胺能神经递质的摄取
公开(公告)号：US08772330B2
公开(公告)日：2014-07-08
申请号：US13355371
申请日：2012-01-20
申请人： James David White , David T. Wong , David B. Chan , Jongtae Yang , Rajan Juniku
发明人： James David White , David T. Wong , David B. Chan , Jongtae Yang , Rajan Juniku
IPC分类号： A61K31/381 , C07D333/16
CPC分类号： A61K31/381 , C07D333/16 , C07D333/20 , C07D333/24
摘要： The present disclosure concerns a compound, or a pharmaceutically acceptable salt thereof, having a formula: where at least one of R1-R4 is a heterocycle, at least one of R1-R4 is an aryl group coupled to the ring by a linker atom, functional group, or other moiety, or where none of R1-R4 is an amide, and any and all combinations thereof. Remaining R1-R4 substituents independently are aliphatic, substituted aliphatic, amine, substituted amine, aryl, substituted aryl, cyclic, substituted cyclic, halide, heteroaryl, substituted heteroaryl, heterocyclic, substituted heterocyclic, hydrogen or hydroxyl. A method for treating a subject also is provided comprising administering a disclosed compound or compounds, or a prodrug that is converted into the disclosed compound or compounds, or a composition comprising the compound, compounds, or prodrugs thereof, to a subject. A method for making disclosed compounds also is provided.
摘要翻译：本公开涉及具有下式的化合物或其药学上可接受的盐：其中R 1 -R 4中的至少一个是杂环，R 1 -R 4中的至少一个是通过连接原子与环偶联的芳基，官能团或其它部分，或者其中没有R 1 -R 4是酰胺，以及其任何和所有组合。残留的R 1 -R 4取代基独立地是脂族，取代的脂族，胺，取代的胺，芳基，取代的芳基，环状，取代的环状，卤素，杂芳基，取代的杂芳基，杂环，取代的杂环，氢或羟基。还提供了治疗受试者的方法，其包括向受试者施用公开的化合物或化合物，或将其转化为所公开的化合物或化合物的前体药物或包含其化合物，化合物或前药的组合物。还提供了制备公开化合物的方法。

2. 发明申请

US20120190725A1 INHIBITOR(S) OF TRANSPORTERS OR UPTAKE OF MONOAMINERGIC NEUROTRANSMITTERS 有权
标题翻译：运输商抑制剂或单宁神经递质的摄取
公开(公告)号：US20120190725A1
公开(公告)日：2012-07-26
申请号：US13355371
申请日：2012-01-20
申请人： James David White , David T. Wong , David B. Chan , Jongtae Yang , Rajan Juniku
发明人： James David White , David T. Wong , David B. Chan , Jongtae Yang , Rajan Juniku
IPC分类号： A61K31/381 , C07D333/20 , C07D333/16 , A61P25/24 , A61P25/22 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/08 , A61P25/18 , A61P13/00 , A61P25/06 , A61P3/04 , A61P3/00 , A61P25/30 , A61P25/32 , A61P25/36 , A61P25/34 , C07D333/24
CPC分类号： A61K31/381 , C07D333/16 , C07D333/20 , C07D333/24
摘要： The present disclosure concerns a compound, or a pharmaceutically acceptable salt thereof, having a formula: where at least one of R1-R4 is a heterocycle, at least one of R1-R4 is an aryl group coupled to the ring by a linker atom, functional group, or other moiety, or where none of R1-R4 is an amide, and any and all combinations thereof. Remaining R1-R4 substituents independently are aliphatic, substituted aliphatic, amine, substituted amine, aryl, substituted aryl, cyclic, substituted cyclic, halide, heteroaryl, substituted heteroaryl, heterocyclic, substituted heterocyclic, hydrogen or hydroxyl. A method for treating a subject also is provided comprising administering a disclosed compound or compounds, or a prodrug that is converted into the disclosed compound or compounds, or a composition comprising the compound, compounds, or prodrugs thereof, to a subject. A method for making disclosed compounds also is provided.
摘要翻译：本公开涉及具有下式的化合物或其药学上可接受的盐：其中R 1 -R 4中的至少一个是杂环，R 1 -R 4中的至少一个是通过连接原子与环连接的芳基，官能团或其它部分，或者其中没有R 1 -R 4是酰胺，以及其任何和所有组合。残留的R 1 -R 4取代基独立地是脂族，取代的脂族，胺，取代的胺，芳基，取代的芳基，环状，取代的环状，卤素，杂芳基，取代的杂芳基，杂环，取代的杂环，氢或羟基。还提供了治疗受试者的方法，其包括向受试者施用公开的化合物或化合物，或将其转化为所公开的化合物或化合物的前体药物或包含其化合物，化合物或前药的组合物。还提供了制备公开化合物的方法。

3. 发明授权

US08101732B2 Methods of producing validamycin A analogs and uses thereof 有权
标题翻译：生产有效霉素A类似物的方法及其用途
公开(公告)号：US08101732B2
公开(公告)日：2012-01-24
申请号：US12560283
申请日：2009-09-15
申请人： Taifo Mahmud , Zixin Deng , Linquan Bai , Hui Xu , Jongtae Yang
发明人： Taifo Mahmud , Zixin Deng , Linquan Bai , Hui Xu , Jongtae Yang
IPC分类号： C07H15/00
CPC分类号： C12N9/0004 , C07H15/22 , C12P19/46
摘要： This disclosure relates to validamycin A biosynthesis and in particular, to methods of producing validamycin A analogs and uses thereof. In a particular example, a method for making a validamycin A analog includes transforming a host cell with one or more recombinant DNA vectors to produce a valN-inactivated mutant; and culturing the valN-inactivated mutant in a culture medium to produce a validamycin A analog, such as 1,1′-bis-valienamine and validienamycin, and their conversion to valienamine. The present disclosure further relates to compositions including such compounds as well as methods of using the compositions, such as for antifungal agents.
摘要翻译：本公开涉及有效霉素A生物合成，特别涉及产生有效霉素A类似物的方法及其用途。在具体实例中，制备有效霉素A类似物的方法包括用一种或多种重组DNA载体转化宿主细胞以产生ValN失活的突变体; 并在培养基中培养valN灭活的突变体以产生有效霉素A类似物，例如1,1'-双 - 缬胺和有效霉素，以及它们转化为valienamine。本公开还涉及包含这些化合物的组合物以及使用组合物如抗真菌剂的方法。

4. 发明申请

US20100151528A1 METHODS OF PRODUCING VALIDAMYCIN A ANALOGS AND USES THEREOF 有权
标题翻译：生产喹哪啶霉素类似物的方法及其用途
公开(公告)号：US20100151528A1
公开(公告)日：2010-06-17
申请号：US12560283
申请日：2009-09-15
申请人： Taifo Mahmud , Zixin Deng , Linquan Bai , Hui Xu , Jongtae Yang
发明人： Taifo Mahmud , Zixin Deng , Linquan Bai , Hui Xu , Jongtae Yang
IPC分类号： C12P19/46 , C12P13/00 , C12N1/21 , C12N15/63 , C07H15/00
CPC分类号： C12N9/0004 , C07H15/22 , C12P19/46
摘要： This disclosure relates to validamycin A biosynthesis and in particular, to methods of producing validamycin A analogs and uses thereof. In a particular example, a method for making a validamycin A analog includes transforming a host cell with one or more recombinant DNA vectors to produce a valN-inactivated mutant; and culturing the valN-inactivated mutant in a culture medium to produce a validamycin A analog, such as 1,1′-bis-valienamine and validienamycin, and their conversion to valienamine. The present disclosure further relates to compositions including such compounds as well as methods of using the compositions, such as for antifungal agents.
摘要翻译：本公开涉及有效霉素A生物合成，特别涉及产生有效霉素A类似物的方法及其用途。在具体实例中，制备有效霉素A类似物的方法包括用一种或多种重组DNA载体转化宿主细胞以产生ValN失活的突变体; 并在培养基中培养valN灭活的突变体以产生有效霉素A类似物，例如1,1'-双 - 缬胺和有效霉素，以及它们转化为valienamine。本公开还涉及包含这些化合物的组合物以及使用组合物如抗真菌剂的方法。

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