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1. 发明授权

US6103901A Process for preparing a 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol derivative 失效
标题翻译：制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇衍生物的方法
公开(公告)号：US6103901A
公开(公告)日：2000-08-15
申请号：US121446
申请日：1998-07-23
申请人： Humberto B. Arzeno , Eric R. Humphreys , Jim-Wah Wong , Christopher R. Roberts
发明人： Humberto B. Arzeno , Eric R. Humphreys , Jim-Wah Wong , Christopher R. Roberts
IPC分类号： C12N11/08 , C07D473/18 , C12N9/20 , C12N9/80 , C12P17/18 , C07B51/00
CPC分类号： C07D473/18 , Y02P20/55
摘要： Intermediates of Formula (III) ##STR1## wherein P.sup.1 is hydrogen or an amino-protecting group, R is lower alkyl, allyl or aralkyl, and Z is hydrogen, lower alkyl, aryl or aralkyl; and Formula (VI) ##STR2## wherein P.sup.1 is hydrogen or an amino-protecting group, P.sup.2 is an amino protecting group, and Z is hydrogen, lower alkyl, aryl or aralkyl, are useful in a novel process for preparing the mono-L-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol (ganciclovir). The mono-L-valine ester of ganciclovir and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.
摘要翻译：其中P1为氢或氨基保护基的式（III）中间体，R为低级烷基，烯丙基或芳烷基，Z为氢，低级烷基，芳基或芳烷基; 和式（VI）其中P1是氢或氨基保护基，P2是氨基保护基，Z是氢，低级烷基，芳基或芳烷基，可用于制备单-L-缬氨酸酯的新方法的2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇（更昔洛韦）。更昔洛韦的单-L-缬氨酸酯及其药学上可接受的盐具有改善吸收的抗病毒剂的价值。

2. 发明授权

US07365188B2 Process for producing N4-Acyl-5′-deoxy-5-fluorocytidine 有权
标题翻译：制备N4-酰基-5'-脱氧-5-氟胞苷的方法
公开(公告)号：US07365188B2
公开(公告)日：2008-04-29
申请号：US11021703
申请日：2004-12-22
申请人： Christopher R. Roberts , Jim-wah Wong
发明人： Christopher R. Roberts , Jim-wah Wong
IPC分类号： C07H19/06
CPC分类号： C07H19/067
摘要： The present invention provides a process for producing a N4-acyl-5′-deoxy-5-fluorocytidine compound of the formula: where R2 is alkyl, cycloalkyl, aralkyl, aryl, or alkoxy.
摘要翻译：本发明提供下式的N 4 - 酰基-5'-脱氧-5-氟胞苷化合物的制备方法：其中R 2是烷基，环烷基，芳烷基，芳基或烷氧基。

3. 发明授权

US5840890A Process for preparing a 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol derivative 失效
标题翻译：制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇衍生物的方法
公开(公告)号：US5840890A
公开(公告)日：1998-11-24
申请号：US775424
申请日：1997-01-09
申请人： Humberto B. Arzeno , Eric R. Humphreys , Jim-Wah Wong , Christopher R. Roberts
发明人： Humberto B. Arzeno , Eric R. Humphreys , Jim-Wah Wong , Christopher R. Roberts
IPC分类号： C12N11/08 , C07D473/18 , C12N9/20 , C12N9/80 , C12P17/18 , C07B51/00
CPC分类号： C07D473/18 , Y02P20/55
摘要： Process and novel intermediates for preparing the mono-L-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol ganciclovir) and its pharmaceutically acceptable salts. The present process and monoester intermediates provide for mono-esterification by an L-valine derivative, resulting in a monocarboxylate-monovalinate which is then selectively hydrolyzed under basic or enzymatic conditions to give the monovaline ester of ganciclovir in high yield and purity. These products are of value as antiviral agents with improved absorption.
摘要翻译：用于制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇更昔洛韦的单-L-缬氨酸酯的方法和新型中间体及其药学上可接受的盐。本方法和单酯中间体通过L-缬氨酸衍生物提供单酯化，得到单羧酸酯 - 单戊酸酯，然后在碱性或酶条件下选择性水解，以高产率和纯度得到更昔洛韦的单戊酸酯。这些产品具有改善吸收的抗病毒药物的价值。

4. 发明授权

US06340756B1 Process for preparing a 2-(2-amino-1, 6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol derivative 有权
标题翻译：制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇衍生物的方法
公开(公告)号：US06340756B1
公开(公告)日：2002-01-22
申请号：US09497319
申请日：2000-02-03
申请人： Charles A. Dvorak , Douglas L. Wren , Lawrence E. Fisher , Steven D. Axt , Eric R. Humphreys , Humberto B. Arzeno , Colin C. Beard , Sam Linh Nguyen , Yeun-Kwei Han , Christopher R. Roberts , Jan P. Lund , Paul R. Fatheree
发明人： Charles A. Dvorak , Douglas L. Wren , Lawrence E. Fisher , Steven D. Axt , Eric R. Humphreys , Humberto B. Arzeno , Colin C. Beard , Sam Linh Nguyen , Yeun-Kwei Han , Christopher R. Roberts , Jan P. Lund , Paul R. Fatheree
IPC分类号： C07D47318
CPC分类号： C07D473/00 , C07D473/18 , Y02P20/55
摘要： wherein Z1 is hydrogen or an amino-protecting group selected from the group consisting of acyl of the formula R—C(O)—, wherein R is alkyl of 1-6 carbon atoms; trityl, optionally substituted with methoxy; and N-(9-fluorenylmethoxycarbonyl); Y1 is halo, aralkyloxy or acyloxy, wherein acyl is as defined above; and Y2 is aralkyloxy. These intermediates are useful in a novel process for preparing the mono-L-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl) methoxy-1,3-propanediol (ganciclovir). The mono-L-valine ester of ganciclovir and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.
摘要翻译：其中Z1是氢或选自式R-C（O） - 的酰基的氨基保护基，其中R是1-6个碳原子的烷基; 三苯甲基，任选被甲氧基取代; 和N-（9-芴基甲氧基羰基）; Y1是卤素，芳烷氧基或酰氧基，其中酰基如上所定义; 而Y2是芳烷氧基。这些中间体可用于制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇（更昔洛韦）的单-L-缬氨酸酯的新方法）。更昔洛韦的单-L-缬氨酸酯及其药学上可接受的盐具有改善吸收的抗病毒剂的价值。

5. 发明申请

US20110213082A1 INSULINOTROPIC PEPTIDE SYNTHESIS USING SOLID AND SOLUTION PHASE COMBINATION TECHNIQUES 审中-公开
标题翻译：使用固相和溶液相组合技术的胰岛素肽合成
公开(公告)号：US20110213082A1
公开(公告)日：2011-09-01
申请号：US13105435
申请日：2011-05-11
申请人： Christopher R. Roberts , Lin Chen , Yeun-Kwei Han
发明人： Christopher R. Roberts , Lin Chen , Yeun-Kwei Han
IPC分类号： C08G61/00 , C07K7/08
CPC分类号： C07K14/605 , A61K38/00
摘要： The present invention relates to the preparation of insulinotropic peptides that are synthesized using a solid and solution phase (“hybrid”) approach. Generally, the approach includes synthesizing three different peptide intermediate fragments using solid phase chemistry. Solution phase chemistry is then used to add additional amino acid material to one of the fragments. The fragments are then coupled together in the solid solution phase. The use of a pseudoproline in one of the fragments eases solid phase synthesis of that fragment and also eases subsequent solution phase coupling of this fragment to other fragments. The present invention is very useful for forming insulinotropic peptides such as GLP-1(7-36) and its natural and non-natural counterparts.
摘要翻译：本发明涉及使用固相和溶液相（“混合”）方法合成的促胰岛素肽的制备。通常，该方法包括使用固相化学合成三种不同的肽中间体片段。然后使用溶液相化学为其中一个片段添加另外的氨基酸材料。然后将片段在固溶相中偶联在一起。在其中一个片段中使用假脯氨酸使得该片段的固相合成减轻了该片段随后与其它片段的溶液相偶联。本发明对于形成促胰岛素肽如GLP-1（7-36）及其天然和非天然对应物非常有用。

6. 发明授权

US08227571B2 Insulinotropic peptide synthesis using solid and solution phase combination techniques 失效
标题翻译：使用固相和溶液相组合技术的胰岛素肽合成
公开(公告)号：US08227571B2
公开(公告)日：2012-07-24
申请号：US12316309
申请日：2008-12-11
申请人： Lin Chen , Yeun-Kwei Han , Christopher R. Roberts
发明人： Lin Chen , Yeun-Kwei Han , Christopher R. Roberts
IPC分类号： C07K14/00
CPC分类号： C07K14/605
摘要： The present invention relates to the preparation of insulinotropic peptides that are synthesized using a solid and solution phase (“hybrid”) approach. Generally, the approach includes synthesizing three different peptide intermediate fragments using solid phase chemistry. Solution phase chemistry is then used to add additional amino acid material to the third fragment which is then coupled to the second fragment and then the first fragment in solution. Alternatively, a different second fragment is coupled to the first fragment in the solid phase. Then, solution phase chemistry is then used to add additional amino acid material to a different third fragment. Subsequently, this different third fragment is coupled to the coupled first and different second fragment in the solution phase. The use of a pseudoproline in one of the fragments eases solid phase synthesis of that fragment and also eases subsequent solution phase coupling of this fragment to the other fragments. The present invention is very useful for forming insulinotropic peptides such as GLP-1(7-36) and its natural and non-natural counterparts.
摘要翻译：本发明涉及使用固相和溶液相（“混合”）方法合成的促胰岛素肽的制备。通常，该方法包括使用固相化学合成三种不同的肽中间体片段。然后使用溶液相化学为第三片段添加另外的氨基酸材料，然后将其与第二片段偶联，然后与溶液中的第一片段偶联。或者，不同的第二片段与固相中的第一片段偶联。然后，然后使用溶液相化学法将另外的氨基酸材料添加到不同的第三片段。随后，将该不同的第三片段与溶液相中的偶联的第一和不同的第二片段偶联。在其中一个片段中使用假脯氨酸使得该片段的固相合成减轻了该片段随后与其它片段的溶液相偶联。本发明对于形成促胰岛素肽如GLP-1（7-36）及其天然和非天然对应物非常有用。

7. 发明申请

US20080287649A1 Methods for the synthesis of cyclic peptides 审中-公开
标题翻译：合成环肽的方法
公开(公告)号：US20080287649A1
公开(公告)日：2008-11-20
申请号：US12004265
申请日：2007-12-20
申请人： Lin Chen , Yeun-Kwei Han , Christopher R. Roberts
发明人： Lin Chen , Yeun-Kwei Han , Christopher R. Roberts
IPC分类号： C07K2/00 , C07C69/616 , C07K5/12
CPC分类号： C07K1/04 , C07K5/06113 , C07K7/56 , C07K14/665
摘要： Methods for the synthesis of cyclic peptides are provided, as well as novel dipeptide compounds. The methods include the solid phase synthesis of a dipeptide, which is the coupled to a second peptide in a solid phase reaction. The peptide is then cyclized following the coupling reaction. The methods and dipeptides are particularly useful for the synthesis of MC-4 receptor agonist peptides.
摘要翻译：提供了合成环肽的方法，以及新型二肽化合物。所述方法包括在固相反应中与第二肽偶联的二肽的固相合成。然后在偶合反应后使肽环化。该方法和二肽特别可用于合成MC-4受体激动剂肽。

8. 发明授权

US06215017B1 Process for preparing a 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol derivative 有权
标题翻译：制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇衍生物的方法
公开(公告)号：US06215017B1
公开(公告)日：2001-04-10
申请号：US09497537
申请日：2000-02-03
申请人： Charles A. Dvorak , Douglas L. Wren , Lawrence E. Fisher , Steven D. Axt , Eric R. Humphreys , Humberto B. Arzeno , Colin C. Beard , Sam Linh Nguyen , Yeun-Kwei Han , Christopher R. Roberts , Jan P. Lund , Paul R. Fatheree
发明人： Charles A. Dvorak , Douglas L. Wren , Lawrence E. Fisher , Steven D. Axt , Eric R. Humphreys , Humberto B. Arzeno , Colin C. Beard , Sam Linh Nguyen , Yeun-Kwei Han , Christopher R. Roberts , Jan P. Lund , Paul R. Fatheree
IPC分类号： C07C67743
CPC分类号： C07D473/00 , C07D473/18 , Y02P20/55
摘要： Intermediates of Formula (III) wherein Y1 is acyloxy, wherein acyl is of the formula R—C(O)—, wherein R is alkyl of 1-6 carbon atoms, Y2 is aralkyloxy, and Z is benzoyloxy or acyloxy, wherein acyl is as defined above. Intermediates of formula (III) are useful in a novel process for preparing the mono-L-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol (ganciclovir). The mono-L-valine ester of ganciclovir and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.
摘要翻译：式（III）的中间体，其中Y1是酰氧基，其中酰基是式RC（O） - ，其中R是1-6个碳原子的烷基，Y2是芳烷氧基，Z是苯甲酰氧基或酰氧基，其中酰基如所定义式（III）的中间体可用于制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1的单-L-缬氨酸酯的新方法，3-丙二醇（更昔洛韦）。更昔洛韦的单-L-缬氨酸酯及其药学上可接受的盐具有改善吸收的抗病毒剂的价值。

9. 发明申请

US20090292108A1 Insulinotropic peptide synthesis using solid and solution phase combination techniques 失效
标题翻译：使用固相和溶液相组合技术的胰岛素肽合成
公开(公告)号：US20090292108A1
公开(公告)日：2009-11-26
申请号：US12316309
申请日：2008-12-11
申请人： Lin Chen , Yeun-Kwei Han , Christopher R. Roberts
发明人： Lin Chen , Yeun-Kwei Han , Christopher R. Roberts
IPC分类号： C07K1/02 , C07K14/00 , C07K7/06
CPC分类号： C07K14/605
摘要： The present invention relates to the preparation of insulinotropic peptides that are synthesized using a solid and solution phase (“hybrid”) approach. Generally, the approach includes synthesizing three different peptide intermediate fragments using solid phase chemistry. Solution phase chemistry is then used to add additional amino acid material to the third fragment which is then coupled to the second fragment and then the first fragment in solution. Alternatively, a different second fragment is coupled to the first fragment in the solid phase. Then, solution phase chemistry is then used to add additional amino acid material to a different third fragment. Subsequently, this different third fragment is coupled to the coupled first and different second fragment in the solution phase. The use of a pseudoproline in one of the fragments eases solid phase synthesis of that fragment and also eases subsequent solution phase coupling of this fragment to the other fragments. The present invention is very useful for forming insulinotropic peptides such as GLP-1(7-36) and its natural and non-natural counterparts.
摘要翻译：本发明涉及使用固相和溶液相（“混合”）方法合成的促胰岛素肽的制备。通常，该方法包括使用固相化学合成三种不同的肽中间体片段。然后使用溶液相化学为第三片段添加另外的氨基酸材料，然后将其与第二片段偶联，然后与溶液中的第一片段偶联。或者，不同的第二片段与固相中的第一片段偶联。然后，然后使用溶液相化学法将另外的氨基酸材料添加到不同的第三片段。随后，将该不同的第三片段与溶液相中的偶联的第一和不同的第二片段偶联。在其中一个片段中使用假脯氨酸使得该片段的固相合成减轻了该片段随后与其它片段的溶液相偶联。本发明对于形成促胰岛素肽如GLP-1（7-36）及其天然和非天然对应物非常有用。

10. 发明授权

US06485451B1 Body cavity irrigation system 失效
标题翻译：体腔灌注系统
公开(公告)号：US06485451B1
公开(公告)日：2002-11-26
申请号：US09630884
申请日：2000-08-02
申请人： Christopher R. Roberts , Michael McMahon , Steven R. Slawson
发明人： Christopher R. Roberts , Michael McMahon , Steven R. Slawson
IPC分类号： A61M100
CPC分类号： A61M3/0283 , A61M1/0058 , A61M1/0064 , A61M2205/3368 , A61M2210/0662
摘要： A body cavity irrigation system includes a housing having at least one interior chamber which is connectable to a faucet or other continuous fluid supply which delivers liquid under pressure through an inlet port. A discharge port of the housing is fluidly interconnected to an irrigation syringe having an actuable valve to control the dispensing of liquid from the housing to a body cavity through a discharge opening under controlled pressure. The liquid being dispensed can be monitored to ensure that the liquid is at an preferred temperature for effectively cleaning the body cavity without patient discomfort, the housing including an antiscald valve which prevents liquid above a predetermined temperature from being dispensed and in which at least one indicator indicates to the user that the liquid is above a second predetermined temperature whereby the first and second temperatures define a suitable temperature range. The system removes discharged water from the body cavity through an insertion tip of the syringe along a return path extending to the housing which includes a venturi which removes the discharged water.
摘要翻译：体腔灌溉系统包括具有至少一个内室的壳体，所述至少一个内室可连接到水龙头或其它连续流体供应器，其通过入口端口在压力下输送液体。壳体的排出口流体地互连到具有致动阀的冲洗注射器，以控制通过控制压力下的排放口将液体从壳体分配到体腔。可以监测被分配的液体，以确保液体处于优选的温度以有效地清洁体腔而没有患者不适，该壳体包括防止在预定温度以上的液体被分配的止回阀，并且其中至少一个指示器向用户指示液体高于第二预定温度，由此第一和第二温度限定合适的温度范围。该系统通过注射器的插入端沿着延伸到壳体的返回路径从体腔中除去排出的水，其包括排出排出的水的文丘里管。

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