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公开(公告)号：US08815943B2
公开(公告)日：2014-08-26
申请号：US13032036
申请日：2011-02-22
IPC分类号： C07D307/33
CPC分类号： C07D307/33 , A61K31/365 , C07D307/32 , C07D309/30 , C07D333/32 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , C12N1/36 , Y02A50/471 , Y02A50/473
摘要： The present invention provides compounds and methods for modulation of the quorum sensing of bacteria. In an embodiment, the compounds of the present invention are able to act as replacements for naturally occurring bacterial quorum sensing ligands in a ligand-protein binding system; that is, they imitate the effect of natural ligands and produce an agonistic effect. In another embodiment, the compounds of the present invention are able to act in a manner which disturbs or inhibits the naturally occurring ligand-protein binding system in quorum sensing bacteria; that is, they produce an antagonistic effect. The compounds of the present invention comprise N-acylated-homoserine lactones (AHLs) comprised of a wide range of acyl groups.
摘要翻译： 本发明提供了用于调节细菌群体感应的化合物和方法。 在一个实施方案中，本发明的化合物能够作为配体 - 蛋白质结合系统中天然存在的细菌群感知配体的替代物; 也就是说，它们模拟天然配体的作用并产生激动作用。 在另一个实施方案中，本发明的化合物能够以扰乱或抑制群体感应细菌中天然存在的配体 - 蛋白质结合系统的方式起作用; 也就是说，它们产生对立效应。 本发明的化合物包含由广泛酰基组成的N-酰化高丝氨酸内酯（AHL）。
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公开(公告)号：US08227616B2
公开(公告)日：2012-07-24
申请号：US12815250
申请日：2010-06-14
IPC分类号： C07D211/78 , A61K31/44
CPC分类号： A61K31/122 , A61K31/4412 , C07C45/74 , C07C49/813 , C07C49/835 , C07C49/84 , C07D213/85 , C07D239/26 , C07D239/42 , C12Q1/18
摘要： The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use. For example, the present invention provides chalcone and cyanopyridine compounds, and derivatives thereof, exhibiting high antibacterial activities having multiple electron withdrawing group substituents, such as halogens and fluorinated alky groups, and optionally having hydroxyl and/or alkoxyl groups substituents.
摘要翻译： 本发明一般涉及提供抗菌治疗剂和制剂的化合物，以及使用和制备抗菌化合物的相关方法。 本发明的抗菌化合物包括查耳酮，烷基嘧啶，氨基嘧啶和氰基吡啶化合物及其在广泛使用中表现出与常规抗菌化合物类似或更少的最小抑制浓度（MIC）的衍生物。 例如，本发明提供查耳酮和氰基吡啶化合物及其衍生物，表现出具有多个吸电子基团取代基的高抗菌活性，例如卤素和氟化烷基，以及任选具有羟基和/或烷氧基取代基。
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3.发明申请COMPOUNDS AND METHODS FOR MODULATING COMMUNICATION AND VIRULENCE IN QUORUM SENSING BACTERIA 有权调节细菌感染细菌中通讯和毒力的化合物和方法公开(公告)号：US20100305182A1
公开(公告)日：2010-12-02
申请号：US12641056
申请日：2009-12-17
IPC分类号： A61K31/404 , C07D307/22 , C07D407/12 , A61K31/34 , A01N43/08 , A01N43/38 , B05D1/02 , B05D1/28 , A61P31/04 , A01P1/00
CPC分类号： C07D307/33
摘要： The present invention provides compositions and methods for modulating the communication and virulence of quorum sensing bacteria. In various exemplary embodiments, the invention provides a combinatorial library of quorum sensing compounds including synthetic analogs of naturally occurring and non-naturally occurring acyl-homoserine lactone (AHL) analogs, and methods of synthesizing and using these compounds.
摘要翻译： 本发明提供用于调节群体感应细菌的通讯和毒力的组合物和方法。 在各种示例性实施方案中，本发明提供了包括天然存在和非天然存在的酰基 - 高丝氨酸内酯（AHL）类似物的合成类似物的群体感应化合物的组合文库，以及合成和使用这些化合物的方法。
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公开(公告)号：US06414097B1
公开(公告)日：2002-07-02
申请号：US09919658
申请日：2001-07-31
IPC分类号： C08F426
CPC分类号： C07C269/06 , C07C41/30 , C07C67/475 , C07C69/78 , C07C69/007 , C07C69/16 , C07C43/166 , C07C43/1787
摘要： A method for the cross-metathesis of terminal olefins is disclosed. The method describes making disubstituted internal olefin products by contacting a first terminal olefin with another first terminal olefin to form a dimer and then contacting the dimer with a second terminal olefin in the presence of a catalyst having the formula where M may be Os or Ru, R and R1 may be the same or different and may be hydrogen or a substitutent group selected from C1-C20 alkyl, C2-C20 alkenyl, C2-C20alkynyl, aryl, C1C20 carboxylate, C1-C20 alkoxy, C2-C20 alkenyloxy, C2-C20 alkynyloxy, aryloxy, C2-C20 alkoxycarbonyl, C1-C20 alkylthio, C1-C20 alkylsulfonyl, and C1-C20 alkylsulfinyl. X and X1 may be the same or different and may be any anionic ligand. L and L1 may be the same or different and may be any neutral electron donor.
摘要翻译： 公开了一种用于末端烯烃交叉复分解的方法。 该方法描述了通过使第一末端烯烃与另一个第一末端烯烃接触以形成二聚体制备二取代的内烯烃产物，然后在具有式I的催化剂存在下使二聚体与第二末端烯烃接触，M可以是Os或Ru，R 并且R 1可以相同或不同，并且可以是氢或选自C 1 -C 20烷基，C 2 -C 20烯基，C 2 -C 20炔基，芳基，C 1 -C 20羧酸酯，C 1 -C 20烷氧基，C 2 -C 20链烯氧基，C 2 -C 20 炔氧基，芳氧基，C 2 -C 20烷氧基羰基，C 1 -C 20烷硫基，C 1 -C 20烷基磺酰基和C 1 -C 20烷基亚磺酰基。 X和X 1可以相同或不同，并且可以是任何阴离子配体。 L和L1可以相同或不同，并且可以是任何中性电子给体。
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公开(公告)号：US08618327B2
公开(公告)日：2013-12-31
申请号：US13543572
申请日：2012-07-06
IPC分类号： C07C211/00 , A61K33/02
CPC分类号： A61K31/122 , A61K31/4412 , C07C45/74 , C07C49/813 , C07C49/835 , C07C49/84 , C07D213/85 , C07D239/26 , C07D239/42 , C12Q1/18
摘要： The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use. For example, the present invention provides chalcone and cyanopyridine compounds, and derivatives thereof, exhibiting high antibacterial activities having multiple electron withdrawing group substituents, such as halogens and fluorinated alkyl groups, and optionally having hydroxyl and/or alkoxyl groups substituents.
摘要翻译： 本发明一般涉及提供抗菌治疗剂和制剂的化合物，以及使用和制备抗菌化合物的相关方法。 本发明的抗菌化合物包括查耳酮，烷基嘧啶，氨基嘧啶和氰基吡啶化合物及其在广泛使用中表现出与常规抗菌化合物类似或更少的最小抑制浓度（MIC）的衍生物。 例如，本发明提供查耳酮和氰基吡啶化合物及其衍生物，其表现出具有多个吸电子基团取代基的高抗菌活性，例如卤素和氟化烷基，并且任选具有羟基和/或烷氧基取代基。
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公开(公告)号：US08367680B2
公开(公告)日：2013-02-05
申请号：US12412658
申请日：2009-03-27
IPC分类号： A61K31/165 , A61K31/505 , A61K31/4418 , A61P31/04 , C07C235/78 , C07D213/85 , C07D239/24 , C40B30/06
CPC分类号： C12Q1/18 , C07C235/20 , C07D213/85 , C07D239/26 , C07D239/42 , C40B30/06
摘要： The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use.
摘要翻译： 本发明一般涉及提供抗菌治疗剂和制剂的化合物，以及使用和制备抗菌化合物的相关方法。 本发明的抗菌化合物包括查耳酮，烷基嘧啶，氨基嘧啶和氰基吡啶化合物及其在广泛使用中表现出与常规抗菌化合物类似或更少的最小抑制浓度（MIC）的衍生物。
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公开(公告)号：US20110212860A1
公开(公告)日：2011-09-01
申请号：US13032036
申请日：2011-02-22
IPC分类号： C40B40/04 , C07D307/33 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12
CPC分类号： C07D307/33 , A61K31/365 , C07D307/32 , C07D309/30 , C07D333/32 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , C12N1/36 , Y02A50/471 , Y02A50/473
摘要： The present invention provides compounds and methods for modulation of the quorum sensing of bacteria. In an embodiment, the compounds of the present invention are able to act as replacements for naturally occurring bacterial quorum sensing ligands in a ligand-protein binding system; that is, they imitate the effect of natural ligands and produce an agonistic effect. In another embodiment, the compounds of the present invention are able to act in a manner which disturbs or inhibits the naturally occurring ligand-protein binding system in quorum sensing bacteria; that is, they produce an antagonistic effect. The compounds of the present invention comprise N-acylated-homoserine lactones (AHLs) comprised of a wide range of acyl groups.
摘要翻译： 本发明提供了用于调节细菌群体感应的化合物和方法。 在一个实施方案中，本发明的化合物能够作为配体 - 蛋白质结合系统中天然存在的细菌群感知配体的替代物; 也就是说，它们模拟天然配体的作用并产生激动作用。 在另一个实施方案中，本发明的化合物能够以扰乱或抑制群体感应细菌中天然存在的配体 - 蛋白质结合系统的方式起作用; 也就是说，它们产生对立效应。 本发明的化合物包含由广泛酰基组成的N-酰化高丝氨酸内酯（AHL）。
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公开(公告)号：US20100261763A1
公开(公告)日：2010-10-14
申请号：US12815250
申请日：2010-06-14
IPC分类号： A61K31/44 , C07C49/794 , A61K31/12 , C07D213/84 , A61P31/04
CPC分类号： A61K31/122 , A61K31/4412 , C07C45/74 , C07C49/813 , C07C49/835 , C07C49/84 , C07D213/85 , C07D239/26 , C07D239/42 , C12Q1/18
摘要： The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use. For example, the present invention provides chalcone and cyanopyridine compounds, and derivatives thereof, exhibiting high antibacterial activities having multiple electron withdrawing group substituents, such as halogens and fluorinated alky groups, and optionally having hydroxyl and/or alkoxyl groups substituents.
摘要翻译： 本发明一般涉及提供抗菌治疗剂和制剂的化合物，以及使用和制备抗菌化合物的相关方法。 本发明的抗菌化合物包括查耳酮，烷基嘧啶，氨基嘧啶和氰基吡啶化合物及其在广泛使用中表现出与常规抗菌化合物类似或更少的最小抑制浓度（MIC）的衍生物。 例如，本发明提供查耳酮和氰基吡啶化合物及其衍生物，表现出具有多个吸电子基团取代基的高抗菌活性，例如卤素和氟化烷基，以及任选具有羟基和/或烷氧基取代基。
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公开(公告)号：US20080312319A1
公开(公告)日：2008-12-18
申请号：US12051826
申请日：2008-03-19
IPC分类号： A61K31/365 , C12N1/20 , C40B40/04 , A61P31/00 , C07D307/33
CPC分类号： C07D307/33 , A61K31/365 , C07D307/32 , C07D309/30 , C07D333/32 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , C12N1/36 , Y02A50/471 , Y02A50/473
摘要： The present invention provides compounds and methods for modulation of the quorum sensing of bacteria. In an embodiment, the compounds of the present invention are able to act as replacements for naturally occurring bacterial quorum sensing ligands in a ligand-protein binding system; that is, they imitate the effect of natural ligands and produce an agonistic effect. In another embodiment, the compounds of the present invention are able to act in a manner which disturbs or inhibits the naturally occurring ligand-protein binding system in quorum sensing bacteria; that is, they produce an antagonistic effect. The compounds of the present invention comprise N-acylated-homoserine lactones (AHLs) comprised of a wide range of acyl groups.
摘要翻译： 本发明提供了用于调节细菌群体感应的化合物和方法。 在一个实施方案中，本发明的化合物能够作为配体 - 蛋白质结合系统中天然存在的细菌群感知配体的替代物; 也就是说，它们模拟天然配体的作用并产生激动作用。 在另一个实施方案中，本发明的化合物能够以扰乱或抑制群体感应细菌中天然存在的配体 - 蛋白质结合系统的方式起作用; 也就是说，它们产生对立效应。 本发明的化合物包含由广泛酰基组成的N-酰化高丝氨酸内酯（AHL）。
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公开(公告)号：US06306988B1
公开(公告)日：2001-10-23
申请号：US09491800
申请日：2000-01-26
IPC分类号： C08F426
CPC分类号： C07C269/06 , C07C41/30 , C07C67/475 , C07C69/78 , C07C69/007 , C07C69/16 , C07C43/166 , C07C43/1787
摘要： A method for the cross-metathesis of terminal olefins is disclosed. The method describes making disubstituted internal olefin products by contacting a first terminal olefin with another first terminal olefin to form a dimer and then contacting the dimer with a second terminal olefin in the presence of a catalyst having the formula where M may be Os or Ru, R and R1 may be the same or different and may be hydrogen or a substitutent group selected from C1-C20 alkyl, C2-C20 alkenyl,C2-C20 alkynyl, aryl, C1-C20 carboxylate, C1-C20 alkoxy, C2-C20 alkenyloxy, C2-C20 alkynyloxy, aryloxy, C2-C20 alkoxycarbonyl, C1-C20 alkylthio, C1-C20 alkylsulfonyl, and C1-C20 alkylsulfinyl. X and X1 may be the same or different and may be any anionic ligand. L and L1 may be the same or different and may be any neutral electron donor.
摘要翻译： 公开了一种用于末端烯烃交叉复分解的方法。 该方法描述了通过使第一末端烯烃与另一个第一末端烯烃接触以形成二聚体制备二取代的内烯烃产物，然后在具有式I的催化剂存在下使二聚体与第二末端烯烃接触，M可以是Os或Ru，R 并且R 1可以相同或不同，并且可以是氢或选自C 1 -C 20烷基，C 2 -C 20烯基，C 2 -C 20炔基，芳基，C 1 -C 20羧酸酯，C 1 -C 20烷氧基，C 2 -C 20链烯氧基， C 2 -C 20炔氧基，芳氧基，C 2 -C 20烷氧基羰基，C 1 -C 20烷硫基，C 1 -C 20烷基磺酰基和C 1 -C 20烷基亚磺酰基。 X和X 1可以相同或不同，并且可以是任何阴离子配体。 L和L1可以相同或不同，并且可以是任何中性电子给体。
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