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41. 发明授权

US5187179A Angiotensin II antagonists incorporating a substituted imidazo [1,2-b][1,2,4]triazole 失效
标题翻译：取代替咪唑（1,2-B）（1,2,4）三唑的ANGIOTENSIN II拮抗剂
公开(公告)号：US5187179A
公开(公告)日：1993-02-16
申请号：US673630
申请日：1991-03-22
申请人： Wallace T. Ashton , Steven M. Hutchins , Malcolm MacCoss
发明人： Wallace T. Ashton , Steven M. Hutchins , Malcolm MacCoss
IPC分类号： A61K31/415 , A61P9/12 , A61P27/02 , C07D249/08 , C07D487/04 , C07F9/6561
CPC分类号： C07D487/04 , C07F9/6561
摘要： There are disclosed substituted imidazo[1,2-b][1,2,4]triazole derivatives of Formula I which are useful as angiotensin II antagonists. ##STR1##

42. 发明授权

US4801710A Regioselective synthesis of 9-substituted purine acyclonucleoside derivatives 失效
标题翻译： 9-取代嘌呤非环酰核苷衍生物的区域选择性合成
公开(公告)号：US4801710A
公开(公告)日：1989-01-31
申请号：US153539
申请日：1988-02-02
申请人： Malcolm MacCoss , Richard L. Tolman , Arthur F. Wagner , John Hannah
发明人： Malcolm MacCoss , Richard L. Tolman , Arthur F. Wagner , John Hannah
IPC分类号： C07D473/00 , C07F9/6561 , C07F9/6574 , C07D473/18 , A61K31/52
CPC分类号： C07D473/00 , C07F9/65616 , C07F9/65742
摘要： A process for preparing 9-substituted guanine-containing acyclonucleosides comprising selective alkylation at the 9-position of the purine by utilizing a blocking group at the 6-position.
摘要翻译：一种制备9-取代的含鸟嘌呤的非循环核苷的方法，其包括在6-位上通过阻断基在嘌呤的9-位选择性烷基化。

43. 发明授权

US4670424A Cyclic pyrophosphates of purine and pyrimidine acyclonucleosides 失效
标题翻译：嘌呤和嘧啶非循环核苷的环状焦磷酸盐
公开(公告)号：US4670424A
公开(公告)日：1987-06-02
申请号：US533676
申请日：1983-09-19
申请人： Malcolm MacCoss , Richard Tolman
发明人： Malcolm MacCoss , Richard Tolman
IPC分类号： A61K31/70 , A61P31/12 , C07F9/6561 , C07F9/6574 , A61K31/52 , A61K31/505 , C07D239/55 , C07D473/18 , C07D473/34
CPC分类号： C07F9/65746 , C07F9/65616
摘要： A compound of the formula R--CH.sub.2 --O--W and its pharmaceutically acceptable salts wherein R is a purine, a substituted purine, a pyrimidine or a substituted pyrimidine, wherein the substituents on the purine or pyrimidine are selected from amino, hydroxyl, halogen, thiol or alkylthiol wherein the alkyl moiety of the alkylthiol has 1 to 6 carbon atoms; and W is ##STR1## The compounds have antiviral activity.
摘要翻译：式R-CH2-OW的化合物及其药学上可接受的盐，其中R是嘌呤，取代的嘌呤，嘧啶或取代的嘧啶，其中嘌呤或嘧啶上的取代基选自氨基，羟基，卤素，硫醇或烷基硫醇，其中烷基硫醇的烷基部分具有1至6个碳原子; 而这些化合物具有抗病毒活性。

44. 发明授权

US4579849A N-alkylguanine acyclonucleosides as antiviral agents 失效
标题翻译： N-烷基鸟嘌呤非循环核苷作为抗病毒剂
公开(公告)号：US4579849A
公开(公告)日：1986-04-01
申请号：US597785
申请日：1984-04-06
申请人： Malcolm MacCoss , Richard L. Tolman , Robert A. Strelitz
发明人： Malcolm MacCoss , Richard L. Tolman , Robert A. Strelitz
IPC分类号： C07D473/18 , A61K31/52 , A61K31/522 , A61K31/675 , A61P31/12 , A61P31/22 , C07D473/00 , C07F9/6561
CPC分类号： C07D473/00 , C07F9/65616
摘要： Disclosed are compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof wherein R.sup.1 and R.sup.2 are independently alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl, each having 1 to 19 carbon atoms, or R.sup.2 is hydrogen; R.sup.3 is hydrogen, alkyl having 1 to 6 carbon atoms or hydroxyalkyl having 1 to 6 carbon atoms; R.sup.4 is hydrogen, halogen, amino or alkyl having 1 to 4 carbon atoms; R.sup.5, R.sup.6 and R.sup.7 are independently selected from hydrogen, hydroxy, alkyl having 1 to 6 carbon atoms, acyloxy having 1 to 8 carbon atoms, alkoxy having 1 to 6 carbon atoms, hydroxyalkyl having 1 to 6 carbon atoms, acyloxyalkyl having 1 to 12 carbon atoms, amino, alkylamino of 1 to 6 carbon atoms and --PO.sub.3.sup.=, or two of R.sup.5, R.sup.6 and R.sup.7 taken together form a group --OPO.sub.2 O.sup.- --, --CH.sub.2 OPO.sub.2 O.sup.- --, --CH.sub.2 OPO.sub.2 OPO.sub.2 O.sup.= --, or --OPO.sub.2 OPO.sub.2 O.sup.= --; A is O, S or CH.sub.2 and X is a pharmaceutically acceptable anion. The compounds have antiviral activity, especially against viruses of the herpes class.
摘要翻译：公开了下式的化合物及其药学上可接受的盐，其中R 1和R 2独立地为烷基，卤代烷基，烯基，卤代烯基，炔基或卤代炔基，各自具有1至19个碳原子，或R 2为氢; R3是氢，具有1至6个碳原子的烷基或具有1至6个碳原子的羟烷基; R4是氢，卤素，氨基或具有1至4个碳原子的烷基; R5，R6和R7独立地选自氢，羟基，具有1至6个碳原子的烷基，具有1至8个碳原子的酰氧基，具有1至6个碳原子的烷氧基，具有1至6个碳原子的羟烷基，具有1至12个碳原子的酰氧基烷基碳原子，氨基，1至6个碳原子的烷基氨基和-PO 3 =，或者R 5，R 6和R 7中的两个一起形成基团-OPO 2 O - ， - CH 2 OPO 2 - + 13，-CH 2 OPO 2 OPO 2 - =或 - - ; A是O，S或CH 2，X是药学上可接受的阴离子。这些化合物具有抗病毒活性，特别是抗疱疹病毒。

45. 发明授权

US4471113A Prodrugs based on phospholipid-nucleoside conjugates 失效
标题翻译：基于磷脂 - 核苷共轭物的前药
公开(公告)号：US4471113A
公开(公告)日：1984-09-11
申请号：US345442
申请日：1982-02-03
申请人： Malcolm MacCoss
发明人： Malcolm MacCoss
IPC分类号： C07H19/06 , C07H19/20 , C07H23/00 , C07H15/12 , C07H17/00
CPC分类号： C07H23/00 , C07H19/06 , C07H19/20
摘要： The invention relates to the production of a single diastereomeric form of a phospholipid araC conjugate as a prodrug.
摘要翻译：本发明涉及作为前体药物制备单一非对映体形式的磷脂araC缀合物。

46. 发明授权

US08440668B2 Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment of type 2 diabetes 有权
标题翻译： β-氨基杂环二肽基肽酶抑制剂用于治疗2型糖尿病
公开(公告)号：US08440668B2
公开(公告)日：2013-05-14
申请号：US13086563
申请日：2011-04-14
申请人： Scott D. Edmondson , Michael Fisher , Dooseop Kim , Malcolm MacCoss , Emma R. Parmee , Ann E. Weber , Jinyou Xu
发明人： Scott D. Edmondson , Michael Fisher , Dooseop Kim , Malcolm MacCoss , Emma R. Parmee , Ann E. Weber , Jinyou Xu
IPC分类号： A61K31/495 , A61K31/40
CPC分类号： A61K31/4985 , A61K31/498 , A61K38/28 , A61K45/06 , C07D487/04 , Y10S514/866 , A61K2300/00
摘要： The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译：本发明涉及作为二肽基肽酶-IV酶（“DP-IV抑制剂”）抑制剂的化合物，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病特别是2型糖尿病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。

47. 发明授权

US07879815B2 Nucleoside aryl phosphoramidates for the treatment of RNA-dependent RNA viral infection 有权
标题翻译：用于治疗RNA依赖性RNA病毒感染的核苷芳基氨基磷酸酯
公开(公告)号：US07879815B2
公开(公告)日：2011-02-01
申请号：US12223940
申请日：2007-02-12
申请人： Malcolm MacCoss , David B. Olsen , Monica Donghi , Cristina Gardelli , Steven Harper , Malte Meppen , Frank Narjes , Barbara Pacini
发明人： Malcolm MacCoss , David B. Olsen , Monica Donghi , Cristina Gardelli , Steven Harper , Malte Meppen , Frank Narjes , Barbara Pacini
IPC分类号： A01N43/04 , A61K31/70
CPC分类号： C07H19/06
摘要： The present invention provides nucleoside aryl phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside aryl phosphoramidates alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside aryl phosphoramidates of the present invention.
摘要翻译：本发明提供结构式（I）的核苷芳基氨基磷酸酯，其是RNA依赖性RNA病毒聚合酶抑制剂的前体。这些化合物是RNA依赖性RNA病毒复制抑制剂的前体，可用于治疗RNA依赖性RNA病毒感染。它们特别可用作丙型肝炎病毒（HCV）NS5B聚合酶抑制剂的前体，作为HCV复制抑制剂的前体和/或治疗丙型肝炎感染。本发明还描述了单独或与其它对RNA依赖性RNA病毒感染，特别是HCV感染有活性的试剂组合的含有这种核苷芳基氨基磷酸酯的药物组合物。还公开了本发明的核苷芳基氨基磷酸酯抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。

48. 发明申请

US20080280842A1 Fluorinated Pyrrolo[2,3-D]Pyrimidine Nucleosides for the Treatment of Rna-Dependent Rna Viral Infection 审中-公开
标题翻译：用于治疗Rna依赖性Rna病毒感染的氟化吡咯并[2,3-D]嘧啶核苷
公开(公告)号：US20080280842A1
公开(公告)日：2008-11-13
申请号：US11664564
申请日：2005-10-17
申请人： Malcolm MacCoss , David B. Olsen , Joseph Leone , Philippe L. Durette
发明人： Malcolm MacCoss , David B. Olsen , Joseph Leone , Philippe L. Durette
IPC分类号： A61K31/7064 , C07H19/04 , A61P31/12
CPC分类号： C07H19/14
摘要： The present invention provides fluorinated pyrrolo[2,3,d]pyrimidine nucleoside compounds which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such fluorinated pyrrolo[2,3-d]pyrimidine nucleoside alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the fluorinated pyrrolo[2,3-d]pyrimidine nucleoside of the present invention.
摘要翻译：本发明提供了作为RNA依赖性RNA病毒聚合酶抑制剂的氟化吡咯并[2,3，d]嘧啶核苷化合物。这些化合物是RNA依赖性RNA病毒复制的抑制剂，可用于治疗RNA依赖性RNA病毒感染。它们特别可用作丙型肝炎病毒（HCV）NS5B聚合酶抑制剂的前体，作为HCV复制抑制剂的前体和/或治疗丙型肝炎感染。本发明还描述了含有这种氟化吡咯并[2,3-d]嘧啶核苷的药物组合物，或者与其它对RNA依赖性RNA病毒感染，特别是HCV感染有活性的试剂组合。还公开了本发明的氟化吡咯并[2,3-d]嘧啶核苷抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。

49. 发明申请

US20080021047A1 C-Purine Nucleoside Analogs As Inhibitors Of Rna-Dependent Rna Viral Polymerase 有权
标题翻译： C-嘌呤核苷类似物作为Rna依赖性Rna病毒聚合酶的抑制剂
公开(公告)号：US20080021047A1
公开(公告)日：2008-01-24
申请号：US11628513
申请日：2005-06-10
申请人： Gabor Butora , Malcolm MacCoss , Balkrishen Bhat , Anne Eldrup
发明人： Gabor Butora , Malcolm MacCoss , Balkrishen Bhat , Anne Eldrup
IPC分类号： A61K31/52 , A61K31/519 , A61P31/12 , C07D473/18 , C07D473/34 , C07D487/04 , C07D491/048 , C07D498/04
CPC分类号： C07D491/04 , C07D487/04 , C07H19/16 , C07H19/20
摘要： The present invention provides C-purine nucleoside analogs and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such C-nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the C-nucleoside compounds of the present invention.
摘要翻译：本发明提供作为RNA依赖性RNA病毒聚合酶抑制剂的C-嘌呤核苷类似物及其某些衍生物。这些化合物是RNA依赖性RNA病毒复制的抑制剂，可用于治疗RNA依赖性RNA病毒感染。它们特别可用作丙型肝炎病毒（HCV）NS5B聚合酶的抑制剂，作为HCV复制的抑制剂和/或用于治疗丙型肝炎感染。本发明还描述了单独或与其它对RNA依赖性RNA病毒感染，特别是HCV感染有活性的试剂组合的含有这种C-核苷化合物的药物组合物。还公开了本发明的C-核苷化合物抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。

50. 发明申请

US20070179114A1 Novel 2'-C methyl nucleoside derivatives 审中-公开
标题翻译：新型2'-C甲基核苷衍生物
公开(公告)号：US20070179114A1
公开(公告)日：2007-08-02
申请号：US11593381
申请日：2006-11-06
申请人： Mark Erion , K. Reddy , Malcolm MacCoss , David Olsen
发明人： Mark Erion , K. Reddy , Malcolm MacCoss , David Olsen
IPC分类号： A61K31/7076 , C07H19/20
CPC分类号： C07H19/04 , C07H19/20
摘要： Compounds of Formula I, stereoisomers, and pharmaceutically acceptable salts or prodrugs thereof, their preparation, and their uses for the treatment of hepatitis C viral infection are described:
摘要翻译：描述了式I化合物，立体异构体及其药学上可接受的盐或前药，其制备方法及其用于治疗丙型肝炎病毒感染的用途：

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