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1. 发明申请

US20050054871A1 Process for the preparation of N-phosphonomethylglycine and derivatives thereof 有权
标题翻译： N-膦酰基甲基甘氨酸及其衍生物的制备方法
公开(公告)号：US20050054871A1
公开(公告)日：2005-03-10
申请号：US10924265
申请日：2004-08-23
申请人： James Coleman , Jerry Ebner , Eric Haupfear , Patrick Lennon , Joseph Schaper , Samuel Tremont , Serge Wolfson , Philip Brodsky
发明人： James Coleman , Jerry Ebner , Eric Haupfear , Patrick Lennon , Joseph Schaper , Samuel Tremont , Serge Wolfson , Philip Brodsky
IPC分类号： C07F9/28 , C07F9/38
CPC分类号： C07F9/3813 , Y02P20/582
摘要： N-phosphonomethylamines are produced by reaction of an amine substrate with a halomethylphosphonic acid or salt thereof, a hydroxymethylphosphonic acid or salt thereof, or a dehydrated self-ester dimer, trimer or oligomer of hydroxymethylphosphonic acid. Among the products that may be prepared according to the process are N-phosphonomethylaminocarboxylic acids such as (e.g.) glyphosate, N-phosphonomethylaminoalkanols such as (e.g.) hydroxyethlaminomethylphosphonic acid, and N-acylaminomethylphosphonic acids such as (e.g.) N-carbamylaminomethylphosphonic acid. Certain reactions are conducted with a substantial excess of amine reactant in order to drive the conversion while avoiding excessive formation of bis(N-phosphonomethyl)amine by-products. Other reactions use a secondary amine substrate (such as iminodiacetic acid) and can be conducted at substantial equimolar ratios of halomethylaminomethylphosphonic acid or hydroxyaminomethylphosphonic acid to secondary amine reactant without significant formation of bis(phosphonomethyl)amine by-products. Further disclosed is a process for the preparation of hydroxymethylphosphonic acid self-ester dimers, trimers and oligomers by azeotropic dehydration.
摘要翻译： N-膦酰基甲胺通过胺底物与卤甲基膦酸或其盐，羟甲基膦酸或其盐或羟甲基膦酸的脱水的自酯二聚物，三聚体或低聚物的反应来制备。可根据该方法制备的产物是N-膦酰基乙基氨基羧酸，例如（例如）草甘膦，N-膦酰基甲基氨基链烷醇如（例如）羟基乙基氨基甲基膦酸和N-酰基氨基甲基膦酸如（例如）N-氨基甲酰基氨基甲基膦酸。某些反应用大量过量的胺反应物进行，以驱动转化，同时避免过度形成双（N-膦酰基甲基）胺副产物。其他反应使用仲胺底物（例如亚氨基二乙酸），并且可以以基本上等摩尔比率的卤代甲基氨基甲基膦酸或羟基氨基甲基膦酸与仲胺反应物进行反应，而不显着形成双（膦酰基甲基）胺副产物。进一步公开了通过共沸脱水制备羟甲基膦酸自酯二聚体，三聚体和低聚物的方法。

2. 发明申请

US20050090543A1 Method for the preparation of tetrahydrobenzothiepines 审中-公开
标题翻译：四氢苯并噻吩的制备方法
公开(公告)号：US20050090543A1
公开(公告)日：2005-04-28
申请号：US10848566
申请日：2004-05-19
申请人： Kevin Babiak , Andrew Carpenter , Shine Chou , Pierre-Jean Colson , Farid Payman , Robert Hett , Christian Huber , Kevin Koeller , Jon Lawson , James Li , Eduardo Mar , Lawrence Miller , Vladislav Orlovski , James Peterson , Mark Pozzo , Claire Przybyla , Samuel Tremont , Jay Trivedi , Grace Wagner , Gerald Weisenburger , Benxin Zhi
发明人： Kevin Babiak , Andrew Carpenter , Shine Chou , Pierre-Jean Colson , Farid Payman , Robert Hett , Christian Huber , Kevin Koeller , Jon Lawson , James Li , Eduardo Mar , Lawrence Miller , Vladislav Orlovski , James Peterson , Mark Pozzo , Claire Przybyla , Samuel Tremont , Jay Trivedi , Grace Wagner , Gerald Weisenburger , Benxin Zhi
IPC分类号： C07D317/18 , A61K31/235 , A61K31/38 , A61K31/495 , A61K31/4995 , A61P3/06 , A61P43/00 , C07B53/00 , C07B55/00 , C07B57/00 , C07B61/00 , C07C201/12 , C07C205/35 , C07C315/02 , C07C315/04 , C07C317/24 , C07C317/36 , C07C319/14 , C07C321/28 , C07D337/08 , C07D409/12 , C07D487/08 , C07D337/16
CPC分类号： C07D409/12 , A61K31/235 , A61K31/38 , A61K31/495 , C07D337/08 , C07D487/08 , A61K2300/00
摘要： Among its several embodiments, the present invention provides an improved process for the preparation of tetrahydrobenzothiepine-1,1-dioxide compounds; the provision of a process for preparing a diastereomeric mixture of tetrahydrobenzothiepine-1,1-dioxide compounds from a single diastereomer of such compounds; the provision of a process for the preparation of 3-bromo-2-substituted propionaldehyde compounds; and the provision of a process for the preparation of 3-thio-2-substituted propionaldehyde compounds.
摘要翻译：在其几个实施方案中，本发明提供了一种制备四氢苯并噻吩一-1,1-二氧化物化合物的改进方法; 提供了由这种化合物的单一非对映异构体制备四氢苯并噻吩一-1,1-二氧化物化合物的非对映体混合物的方法; 提供了制备3-溴-2-取代的丙醛化合物的方法; 并提供了制备3-硫代-2-取代的丙醛化合物的方法。

3. 发明申请

US20080318917A1 POLYETHYLENE GLYCOLATED SUPEROXIDE DISMUTASE MIMETICS 有权
标题翻译：聚乙烯甘油超氧化物歧化酶
公开(公告)号：US20080318917A1
公开(公告)日：2008-12-25
申请号：US11766221
申请日：2007-06-21
申请人： Daniela Salvemini , William L. Neumann , Samuel Tremont , Kishore Udipi , Amruta Reddy Poreddy
发明人： Daniela Salvemini , William L. Neumann , Samuel Tremont , Kishore Udipi , Amruta Reddy Poreddy
IPC分类号： A61K31/555 , A61P25/00 , A61P37/00 , C07D259/00
CPC分类号： A61K47/60
摘要： Compounds and methods for utilizing compounds comprising a superoxide dismutase mimetic covalently linked to polyethylene glycol. Methods are also provided for preparing a superoxide dismutase mimetic covalently linked to a polyethylene glycol, the methods comprising reacting an activated polyethylene glycol with a superoxide, dismutase mimetic, or alternatively, reacting a superoxide dismutase mimetic with an activated polyethylene glycol. A method is also provided for preventing or treating a disease or disorder in which superoxide anions are implicated, comprising administering to a subject in need thereof, a therapeutically effective amount of a compound comprising a superoxide dismutase mimetic covalently linked to a polyethylene glycol. Methods of determining the safety and efficacy of the compounds ere also provided. Methods for determining the safety and efficacy can include methods in lab animals and humans.
摘要翻译：用于利用包含与聚乙二醇共价连接的超氧化物歧化酶模拟物的化合物的化合物和方法。还提供了用于制备与聚乙二醇共价连接的超氧化物歧化酶模拟物的方法，所述方法包括使活化的聚乙二醇与超氧化物反应，模拟物歧化酶，或者将超氧化物歧化酶模拟物与活化的聚乙二醇反应。还提供了一种用于预防或治疗涉及超氧化物阴离子的疾病或病症的方法，包括向有需要的受试者施用治疗有效量的包含与聚乙二醇共价连接的超氧化物歧化酶模拟物的化合物。还提供了确定化合物的安全性和功效的方法。确定安全性和功效的方法可以包括实验动物和人类的方法。

4. 发明授权

US06740663B2 Mono- and di-fluorinated benzothiepine compounds as inhibitors of apical sodium co-dependent bile acid transport (ASBT) and taurocholate uptake 失效
标题翻译：单 - 和二 - 氟化苯并噻吩化合物作为顶端钠依赖性胆汁酸转运（ASBT）和牛磺胆酸摄取抑制剂
公开(公告)号：US06740663B2
公开(公告)日：2004-05-25
申请号：US10286987
申请日：2002-11-04
申请人： Samuel Tremont , Kevin J. Koeller
发明人： Samuel Tremont , Kevin J. Koeller
IPC分类号： A61K3144
CPC分类号： C07D409/12 , C07D337/08 , C07D487/08 , C07D495/04
摘要： Mono-flourinated and di-fluorinated benzothiepine apical sodium co-dependent bile acid transport (ASBT) inhibitors are disclosed together with methods of making the same, methods of using the same to treat hyperlipidemic conditions as well as pharmaceutical compositions containing the same compounds.
摘要翻译：公开了单粉化和二氟化苯并噻庚因顶端钠共依赖性胆汁酸转运（ASBT）抑制剂及其制备方法，使用该方法治疗高脂血症的方法以及含有相同化合物的药物组合物。

5. 发明申请

US20120301403A1 POLYETHYLENE GLYCOLATED SUPEROXIDE DISMUTASE MIMETICS 审中-公开
标题翻译：聚乙烯甘油超氧化物歧化酶
公开(公告)号：US20120301403A1
公开(公告)日：2012-11-29
申请号：US13526111
申请日：2012-06-18
申请人： Daniela Salvemini , William L. Neumann , Samuel Tremont , Kishore Udipi , Amruta Reddy Poreddy
发明人： Daniela Salvemini , William L. Neumann , Samuel Tremont , Kishore Udipi , Amruta Reddy Poreddy
IPC分类号： A61K31/28 , A61P29/00 , A61P1/00 , A61P19/02 , A61P9/12 , A61P17/06 , A61P37/06 , A61P7/02 , A61P37/00 , A61P11/00 , A61P25/00 , A61P25/04 , A61P31/00 , A61K49/00 , C12Q1/18 , A61P9/10
CPC分类号： C12N9/0089 , A61K47/60 , C12Q1/26 , C12Q1/28 , G01N33/5014
摘要： Compounds and methods for utilizing compounds comprising a superoxide dismutase mimetic covalently linked to polyethylene glycol. Methods are also provided for preparing a superoxide dismutase mimetic covalently linked to a polyethylene glycol, the methods comprising reacting an activated polyethylene glycol with a superoxide dismutase mimetic, or alternatively, reacting a superoxide dismutase mimetic with an activated polyethylene glycol. A method is also provided for preventing or treating a disease or disorder in which superoxide anions are implicated, comprising administering to a subject in need thereof, a therapeutically effective amount of a compound comprising a superoxide dismutase mimetic covalently linked to a polyethylene glycol. Methods of determining the safety and efficacy of the compounds are also provided. Methods for determining the safety and efficacy can include methods in lab animals and humans.
摘要翻译：用于利用包含与聚乙二醇共价连接的超氧化物歧化酶模拟物的化合物的化合物和方法。还提供了制备与聚乙二醇共价连接的超氧化物歧化酶模拟物的方法，所述方法包括使活化的聚乙二醇与超氧化物歧化酶模拟物反应，或者使超氧化物歧化酶模拟物与活化的聚乙二醇反应。还提供了一种用于预防或治疗涉及超氧化物阴离子的疾病或病症的方法，包括向有需要的受试者施用治疗有效量的包含与聚乙二醇共价连接的超氧化物歧化酶模拟物的化合物。还提供了确定化合物的安全性和功效的方法。确定安全性和功效的方法可以包括实验动物和人类的方法。

6. 发明授权

US08217166B2 Polyethylene glycolated superoxide dismutase mimetics 有权
标题翻译：聚乙烯甘氨酸超氧化物歧化酶模拟物
公开(公告)号：US08217166B2
公开(公告)日：2012-07-10
申请号：US11766221
申请日：2007-06-21
申请人： Daniela Salvemini , William L. Neumann , Samuel Tremont , Kishore Udipi , Amruta Reddy Poreddy
发明人： Daniela Salvemini , William L. Neumann , Samuel Tremont , Kishore Udipi , Amruta Reddy Poreddy
IPC分类号： C07B47/00 , C07D487/22
CPC分类号： A61K47/60
摘要： Compounds and methods for utilizing compounds comprising a superoxide dismutase mimetic covalently linked to polyethylene glycol. Methods are also provided for preparing a superoxide dismutase mimetic covalently linked to a polyethylene glycol, the methods comprising reacting an activated polyethylene glycol with a superoxide dismutase mimetic, or alternatively, reacting a superoxide dismutase mimetic with an activated polyethylene glycol. A method is also provided for preventing or treating a disease or disorder in which superoxide anions are implicated, comprising administering to a subject in need thereof, a therapeutically effective amount of a compound comprising a superoxide dismutase mimetic covalently linked to a polyethylene glycol. Methods of determining the safety and efficacy of the compounds ere also provided. Methods for determining the safety and efficacy can include methods in lab animals and humans.
摘要翻译：用于利用包含与聚乙二醇共价连接的超氧化物歧化酶模拟物的化合物的化合物和方法。还提供了制备与聚乙二醇共价连接的超氧化物歧化酶模拟物的方法，所述方法包括使活化的聚乙二醇与超氧化物歧化酶模拟物反应，或者使超氧化物歧化酶模拟物与活化的聚乙二醇反应。还提供了一种用于预防或治疗涉及超氧化物阴离子的疾病或病症的方法，包括向有需要的受试者施用治疗有效量的包含与聚乙二醇共价连接的超氧化物歧化酶模拟物的化合物。还提供了确定化合物的安全性和功效的方法。确定安全性和功效的方法可以包括实验动物和人类的方法。

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