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1. 发明授权

US08519095B2 Poly-beta-peptides from functionalized beta-lactam monomers and antibacterial compositions containing same 有权
标题翻译：来自功能化的β-内酰胺单体的聚-β-肽和含有它们的抗菌组合物
公开(公告)号：US08519095B2
公开(公告)日：2013-08-27
申请号：US12759998
申请日：2010-04-14
申请人： Shannon S. Stahl , Samuel H. Gellman , Sarah Lee , Mehmet F. Ilker , Bernard Weisblum , Denis Kissounko
发明人： Shannon S. Stahl , Samuel H. Gellman , Sarah Lee , Mehmet F. Ilker , Bernard Weisblum , Denis Kissounko
IPC分类号： A61K38/02 , C07K2/00 , A61P31/00
CPC分类号： C08G69/22 , A61K38/16 , C07D205/08 , C07D205/12 , C07K1/02
摘要： Disclosed is a method of making β-polypeptides. The method includes polymerizing β-lactam-containing monomers in the presence of a base initiator and a co-initiator which is not a metal-containing molecule to yield the product β-polypeptides. Specifically disclosed are methods wherein the base initiator is potassium t-butoxide, lithium bis(trimethylsilyl)amide (LiN(TMS)2), potassium bis(trimethyl-silyl)amide, and sodium ethoxide, and the reaction is carried out in a solvent such as chloroform, dichloromethane, dimethylsulfoxide, or tetrahydrofuran.
摘要翻译：公开了制备β-多肽的方法。该方法包括在碱基引发剂和不是含金属分子的共引发剂存在下聚合含β-内酰胺的单体以产生产物β-多肽。具体公开的是其中碱引发剂为叔丁醇钾，双（三甲基甲硅烷基）氨基锂（LiN（TMS）2），双（三甲基甲硅烷基）酰胺钾和乙醇钠的方法，反应在溶剂如氯仿，二氯甲烷，二甲基亚砜或四氢呋喃。

2. 发明授权

US09120892B2 Poly-β-peptides from functionalized β-lactam monomers and antibacterial compositions containing same 有权
标题翻译：来自功能化的β-内酰胺单体的聚合物和包含其的抗菌组合物
公开(公告)号：US09120892B2
公开(公告)日：2015-09-01
申请号：US13075218
申请日：2011-03-30
申请人： Shannon S. Stahl , Samuel H. Gellman , Sarah Lee , Bernard Weisblum , Denis Kissounko
发明人： Shannon S. Stahl , Samuel H. Gellman , Sarah Lee , Mehmet F. Ilker , Bernard Weisblum , Denis Kissounko
IPC分类号： C07K1/02 , C12P21/00 , C08G69/22 , C07D205/08 , C07D205/12
CPC分类号： C08G69/22 , A61K38/16 , C07D205/08 , C07D205/12 , C07K1/02
摘要： Disclosed is a method of making β-polypeptides. The method includes polymerizing β-lactam-containing monomers in the presence of a base initiator and a co-initiator which is not a metal-containing molecule to yield the product β-polypeptides. Specifically disclosed are methods wherein the base initiator is potassium t-butoxide, lithium bis(trimethylsilyl)amide (LiN(TMS)2), potassium bis(trimethyl-silyl)amide, and sodium ethoxide, and the reaction is carried out in a solvent such as chloroform, dichloromethane, dimethylsulfoxide, or tetrahydrofuran.
摘要翻译：公开了制备＆bgr-多肽的方法。该方法包括在碱性引发剂和不是含金属的分子的共引发剂存在下聚合并含有内含物的单体，以产生产物和多肽。具体公开的是其中碱引发剂为叔丁醇钾，双（三甲基甲硅烷基）氨基锂（LiN（TMS）2），双（三甲基甲硅烷基）酰胺钾和乙醇钠的方法，反应在溶剂如氯仿，二氯甲烷，二甲基亚砜或四氢呋喃。

3. 发明申请

US20110196127A1 POLY-BETA-PEPTIDES FROM FUNCTIONALIZED BETA-LACTAM MONOMERS AND ANTIBACTERIAL COMPOSITIONS CONTAINING SAME 有权
标题翻译：来自功能化的BETA-LACTAM单体和含有其的抗菌组合物的聚-β-肽
公开(公告)号：US20110196127A1
公开(公告)日：2011-08-11
申请号：US13075218
申请日：2011-03-30
申请人： Shannon S. Stahl , Samuel H. Gellman , Sarah Lee , Mehmet F. Ilker , Bernard Weisblum , Denis Kissounko
发明人： Shannon S. Stahl , Samuel H. Gellman , Sarah Lee , Mehmet F. Ilker , Bernard Weisblum , Denis Kissounko
IPC分类号： C07K2/00
CPC分类号： C08G69/22 , A61K38/16 , C07D205/08 , C07D205/12 , C07K1/02
摘要： Disclosed is a method of making β-polypeptides. The method includes polymerizing β-lactam-containing monomers in the presence of a base initiator and a co-initiator which is not a metal-containing molecule to yield the product β-polypeptides. Specifically disclosed are methods wherein the base initiator is potassium t-butoxide, lithium bis(trimethylsilyl)amide (LiN(TMS)2), potassium bis(trimethyl-silyl)amide, and sodium ethoxide, and the reaction is carried out in a solvent such as chloroform, dichloromethane, dimethylsulfoxide, or tetrahydrofuran.
摘要翻译：公开了制备＆bgr-多肽的方法。该方法包括在碱性引发剂和不是含金属的分子的共引发剂存在下聚合并含有内含物的单体，以产生产物和多肽。具体公开的是其中碱引发剂为叔丁醇钾，双（三甲基甲硅烷基）氨基锂（LiN（TMS）2），双（三甲基甲硅烷基）酰胺钾和乙醇钠的方法，反应在溶剂如氯仿，二氯甲烷，二甲基亚砜或四氢呋喃。

4. 发明授权

US07951912B2 Poly-β-peptides from functionalized β-lactam monomers and antibacterial compositions containing same 有权
标题翻译：来自功能化的β-内酰胺单体的聚合物和包含其的抗菌组合物
公开(公告)号：US07951912B2
公开(公告)日：2011-05-31
申请号：US11510017
申请日：2006-08-25
申请人： Shannon S. Stahl , Samuel H. Gellman , Sarah Lee , Mehmet F. Ilker , Bernard Weisblum , Denis Kissounko
发明人： Shannon S. Stahl , Samuel H. Gellman , Sarah Lee , Mehmet F. Ilker , Bernard Weisblum , Denis Kissounko
IPC分类号： C12P21/06 , C07K1/02
CPC分类号： C08G69/22 , A61K38/16 , C07D205/08 , C07D205/12 , C07K1/02
摘要： Disclosed is a method of making β-polypeptides. The method includes polymerizing β-lactam-containing monomers in the presence of a base initiator and a co-initiator which is not a metal-containing molecule to yield the product β-polypeptides. Specifically disclosed are methods wherein the base initiator is potassium t-butoxide, lithium bis(trimethylsilyl)amide (LiN(TMS)2), potassium bis(trimethyl-silyl)amide, and sodium ethoxide, and the reaction is carried out in a solvent such as chloroform, dichloromethane, dimethylsulfoxide, or tetrahydrofuran.
摘要翻译：公开了制备＆bgr-多肽的方法。该方法包括在碱性引发剂和不是含金属的分子的共引发剂存在下聚合并含有内含物的单体，以产生产物和多肽。具体公开的是其中碱引发剂为叔丁醇钾，双（三甲基甲硅烷基）氨基锂（LiN（TMS）2），双（三甲基甲硅烷基）酰胺钾和乙醇钠的方法，反应在溶剂如氯仿，二氯甲烷，二甲基亚砜或四氢呋喃。

5. 发明申请

US20100222250A1 POLY-BETA-PEPTIDES FROM FUNCTIONALIZED BETA-LACTAM MONOMERS AND ANTIBACTERIAL COMPOSITIONS CONTAINING SAME 有权
标题翻译：来自功能化的BETA-LACTAM单体和含有其的抗菌组合物的聚-β-肽
公开(公告)号：US20100222250A1
公开(公告)日：2010-09-02
申请号：US12759998
申请日：2010-04-14
申请人： Shannon S. Stahl , Samuel H. Gellman , Sarah Lee , Mehmet F. Ilker , Bernard Weisblum , Denis Kissounko
发明人： Shannon S. Stahl , Samuel H. Gellman , Sarah Lee , Mehmet F. Ilker , Bernard Weisblum , Denis Kissounko
IPC分类号： A61K38/02 , C07K2/00 , A61P31/00
CPC分类号： C08G69/22 , A61K38/16 , C07D205/08 , C07D205/12 , C07K1/02
摘要： Disclosed is a method of making β-polypeptides. The method includes polymerizing β-lactam-containing monomers in the presence of a base initiator and a co-initiator which is not a metal-containing molecule to yield the product β-polypeptides. Specifically disclosed are methods wherein the base initiator is potassium t-butoxide, lithium bis(trimethylsilyl)amide (LiN(TMS)2), potassium bis(trimethyl-silyl)amide, and sodium ethoxide, and the reaction is carried out in a solvent such as chloroform, dichloromethane, dimethylsulfoxide, or tetrahydrofuran.
摘要翻译：公开了制备＆bgr-多肽的方法。该方法包括在碱性引发剂和不是含金属的分子的共引发剂存在下聚合并含有内含物的单体，以产生产物和多肽。具体公开的是其中碱引发剂为叔丁醇钾，双（三甲基甲硅烷基）氨基锂（LiN（TMS）2），双（三甲基甲硅烷基）酰胺钾和乙醇钠的方法，反应在溶剂如氯仿，二氯甲烷，二甲基亚砜或四氢呋喃。

6. 发明授权

US09044392B2 Nylon-3 co-polymers and synthetic lung surfactant compositions containing same 有权
标题翻译：尼龙-3共聚物和含有它们的合成肺表面活性剂组合物
公开(公告)号：US09044392B2
公开(公告)日：2015-06-02
申请号：US13634576
申请日：2011-03-17
申请人： Samuel H. Gellman , Shannon S. Stahl , Brendan P. Mowery , Annelise Barron , Michelle Dohm
发明人： Samuel H. Gellman , Shannon S. Stahl , Brendan P. Mowery , Annelise Barron , Michelle Dohm
IPC分类号： C08G69/22 , A61K31/785 , A61P11/00 , C08G69/48 , A61K9/00 , A61K47/32 , C08L77/02
CPC分类号： A61K31/785 , A61K9/0082 , A61K47/32 , C08G69/22 , C08L77/02
摘要： Non-natural oligomers have recently shown promise as functional analogues of lung surfactant proteins Band C (SP-B and SP-C), two helical and amphiphilic proteins that are clitical for normal respiration. The generation of non-natural mimics of SP-B and SP-C has previously been restlicted to step-by-step, sequence-specific synthesis, which results in discrete oligomers that are intended to manifest specific structural attributes. Presented herein an alternative approach to SP-R mimicry that is based on sequence-random copolymers containing cationic and lipophilic subunits. These materials, members of the nylon-3 family, arc prepared by ling-opening polymelization of 13-lactams. The best of the nylon-3 polymers display promising in vitro surfactant activities in a mixed lipid film. Pulsating bubble surfactometry data indicate that films containing the most surface-active polymers attain adsorptive and dynamic-cycling properties that surpass those of discrete peptides intended to mimic SP-B.
摘要翻译：近来，非天然低聚物已经表现出作为肺表面活性蛋白质C（SP-B和SP-C）的功能类似物的前景，两种螺旋和两亲性蛋白质对于正常呼吸是关键的。 SP-B和SP-C的非天然模拟物的产生以前已经被逐步地排列为序列特异性合成，其导致旨在表现特定结构特征的离散低聚物。本文提出了基于含有阳离子和亲脂亚单元的序列无规共聚物的SP-R模拟的替代方法。这些材料是尼龙-3族的成员，通过开启13-内酰胺的多聚化来制备。最好的尼龙-3聚合物在混合脂质膜中显示出有希望的体外表面活性剂活性。脉冲气泡表面测量数据表明，含有最多表面活性聚合物的膜具有超过旨在模拟SP-B的离散肽的吸附和动态循环性能。

7. 发明申请

US20090299098A1 Catalytic Metathesis of Secondary Amides 有权
标题翻译：二级酰胺的催化复分解
公开(公告)号：US20090299098A1
公开(公告)日：2009-12-03
申请号：US12325484
申请日：2008-12-01
申请人： Christen Bell Smith , Denis A. Kissounko , Samuel H. Gellman , Shannon S. Stahl
发明人： Christen Bell Smith , Denis A. Kissounko , Samuel H. Gellman , Shannon S. Stahl
IPC分类号： C07C231/08
CPC分类号： C07C231/08 , C07C231/00
摘要： The invention provides methods and reagents for the metathesis of secondary amides via a transacylation mechanism employing catalytic quantities of an imide initiator and a Brønsted base. Equilibrium-controlled exchange between various amide reactant pairs is demonstrated for substrates bearing a variety of N-alkyl and N-aryl substituents.
摘要翻译：本发明提供了通过使用催化量的酰亚胺引发剂和布朗斯台德碱的转酰化机理来复溶次级酰胺的方法和试剂。对于具有多种N-烷基和N-芳基取代基的底物，证明了各种酰胺反应物对之间的平衡控制交换。

8. 发明授权

US07154004B2 Catalytic transamidation and amide metathesis under moderate conditions 有权
标题翻译：催化转酰胺和酰胺复分解在适度条件下
公开(公告)号：US07154004B2
公开(公告)日：2006-12-26
申请号：US10785301
申请日：2004-02-24
申请人： Shannon S. Stahl , Samuel H. Gellman , Sarah E. Eldred
发明人： Shannon S. Stahl , Samuel H. Gellman , Sarah E. Eldred
IPC分类号： C07C233/05
CPC分类号： C07C231/12 , C07C2601/14 , C07C233/58
摘要： Disclosed is a method of manipulating the carboxamide functionality in a catalytic manner. The method includes the steps of reacting amides with or without amines in the presence of various types of metal catalysts, at a temperature of about 250° C. or less.
摘要翻译：公开了以催化方式操作羧酰胺官能团的方法。该方法包括在各种类型的金属催化剂存在下，在约250℃或更低的温度下使酰胺与或不与胺反应的步骤。

9. 发明申请

US20130004453A1 NYLON-3 CO-POLYMERS AND SYNTHETIC LUNG SURFACTANT COMPOSITIONS CONTAINING SAME 有权
标题翻译：尼龙-3聚合物和含有同种异构体的合成肺表面活性剂组合物
公开(公告)号：US20130004453A1
公开(公告)日：2013-01-03
申请号：US13634576
申请日：2011-03-17
申请人： Samuel H. Gellman , Shannon S. Stahl , Brendan P. Mowery , Annelise Barron , Michelle Dohm
发明人： Samuel H. Gellman , Shannon S. Stahl , Brendan P. Mowery , Annelise Barron , Michelle Dohm
IPC分类号： C08G69/22 , A61K31/785 , A61P11/00 , C08G69/48
CPC分类号： A61K31/785 , A61K9/0082 , A61K47/32 , C08G69/22 , C08L77/02
摘要： Non-natural oligomers have recently shown promise as functional analogues of lung surfactant proteins Band C (SP-B and SP-C), two helical and amphiphilic proteins that are clitical for normal respiration. The generation of non-natural mimics of SP-B and SP-C has previously been restlicted to step-by-step, sequence-specific synthesis, which results in discrete oligomers that are intended to manifest specific structural attributes. Presented herein an alternative approach to SP-R mimicry that is based on sequence-random copolymers containing cationic and lipophilic subunits. These materials, members of the nylon-3 family, arc prepared by ling-opening polymelization of 13-lactams. The best of the nylon-3 polymers display promising in vitro surfactant activities in a mixed lipid film. Pulsating bubble surfactometry data indicate that films containing the most surface-active polymers attain adsorptive and dynamic-cycling properties that surpass those of discrete peptides intended to mimic SP-B.
摘要翻译：近来，非天然低聚物已经表现出作为肺表面活性蛋白质C（SP-B和SP-C）的功能类似物的前景，两种螺旋和两亲性蛋白质对于正常呼吸是关键的。 SP-B和SP-C的非天然模拟物的产生以前已经被逐步地排列为序列特异性合成，其导致旨在表现特定结构特性的离散低聚物。本文提出了基于含有阳离子和亲脂亚单元的序列无规共聚物的SP-R模拟的替代方法。这些材料是尼龙-3族的成员，通过开启13-内酰胺的多聚化来制备。最好的尼龙-3聚合物在混合脂质膜中显示出有希望的体外表面活性剂活性。脉冲气泡表面测量数据表明，含有最多表面活性聚合物的膜具有超过旨在模拟SP-B的离散肽的吸附和动态循环性能。

10. 发明授权

US08039669B2 Catalytic metathesis of secondary amides 有权
标题翻译：二级酰胺的催化复分解
公开(公告)号：US08039669B2
公开(公告)日：2011-10-18
申请号：US12325484
申请日：2008-12-01
申请人： Christen Bell Smith , Denis A. Kissounko , Samuel H. Gellman , Shannon S. Stahl
发明人： Christen Bell Smith , Denis A. Kissounko , Samuel H. Gellman , Shannon S. Stahl
IPC分类号： C07C231/08
CPC分类号： C07C231/08 , C07C231/00
摘要： The invention provides methods and reagents for the metathesis of secondary amides via a transacylation mechanism employing catalytic quantities of an imide initiator and a Brønsted base. Equilibrium-controlled exchange between various amide reactant pairs is demonstrated for substrates bearing a variety of N-alkyl and N-aryl substituents.
摘要翻译：本发明提供了通过使用催化量的酰亚胺引发剂和布朗斯台德碱的转酰化机理来复溶次级酰胺的方法和试剂。对于具有多种N-烷基和N-芳基取代基的底物，证明了各种酰胺反应物对之间的平衡控制交换。

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