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1. 发明申请

US20100068176A1 HEPATITIS C VIRUS INHIBITORS 有权
标题翻译： HEPATITIS C病毒抑制剂
公开(公告)号：US20100068176A1
公开(公告)日：2010-03-18
申请号：US12536362
申请日：2009-08-05
申请人： Makonen Belema , Andrew C. Good , Jason Goodrich , Ramesh Kakarla , Guo Li , Omar D. Lopez , Van N. Nguyen , Jayne Kapur , Yuping Qiu , Jeffrey Lee Romine , Denis R. St. Laurent , Michael Serrano-Wu , Lawrence B. Snyder , Fukang Yang
发明人： Makonen Belema , Andrew C. Good , Jason Goodrich , Ramesh Kakarla , Guo Li , Omar D. Lopez , Van N. Nguyen , Jayne Kapur , Yuping Qiu , Jeffrey Lee Romine , Denis R. St. Laurent , Michael Serrano-Wu , Lawrence B. Snyder , Fukang Yang
IPC分类号： A61K38/20 , C07D403/14 , A61K31/4184 , A61K31/497 , A61K38/21 , A61K31/7088 , A61P31/12
CPC分类号： C07D235/20 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
摘要翻译：本公开涉及用于治疗丙型肝炎病毒（HCV）感染的化合物，组合物和方法。还公开了含有这些化合物的药物组合物和使用这些化合物治疗HCV感染的方法。

2. 发明授权

US07906655B2 Hepatitis C virus inhibitors 有权
标题翻译：丙型肝炎病毒抑制剂
公开(公告)号：US07906655B2
公开(公告)日：2011-03-15
申请号：US12536362
申请日：2009-08-05
申请人： Makonen Belema , Andrew C. Good , Jason Goodrich , Ramesh Kakarla , Guo Li , Omar D. Lopez , Van N. Nguyen , Jayne Kapur , Yuping Qiu , Jeffrey Lee Romine , Denis R. St. Laurent , Michael Serrano-Wu , Lawrence B. Snyder , Fukang Yang
发明人： Makonen Belema , Andrew C. Good , Jason Goodrich , Ramesh Kakarla , Guo Li , Omar D. Lopez , Van N. Nguyen , Jayne Kapur , Yuping Qiu , Jeffrey Lee Romine , Denis R. St. Laurent , Michael Serrano-Wu , Lawrence B. Snyder , Fukang Yang
IPC分类号： C07D403/14 , C07D217/08 , C07D211/32 , C07D239/04 , C07D413/14 , A61K31/47 , A61K31/497 , A61K31/445 , A61K31/5355 , A01N43/60
CPC分类号： C07D235/20 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
摘要翻译：本公开涉及用于治疗丙型肝炎病毒（HCV）感染的化合物，组合物和方法。还公开了含有这些化合物的药物组合物和使用这些化合物治疗HCV感染的方法。

3. 发明申请

US20110294819A1 Hepatitis C Virus Inhibitors 有权
标题翻译：丙型肝炎病毒抑制剂
公开(公告)号：US20110294819A1
公开(公告)日：2011-12-01
申请号：US12974069
申请日：2010-12-21
申请人： Omar D. Lopez , Denis R. St. Laurent , Jason Goodrich , Jeffrey Lee Romine , Michael Serrano-Wu , Fukang Yang , Ramesh Kakarla , Xuejie Yang , Yuping Qiu , Lawrence B. Snyder
发明人： Omar D. Lopez , Denis R. St. Laurent , Jason Goodrich , Jeffrey Lee Romine , Michael Serrano-Wu , Fukang Yang , Ramesh Kakarla , Xuejie Yang , Yuping Qiu , Lawrence B. Snyder
IPC分类号： A61K31/421 , C07D413/14 , C07D471/04 , C07D403/14 , C07D417/14 , C07D401/14 , C07D231/12 , C07D249/08 , C07D249/12 , C07D249/06 , C07D409/14 , C07D405/14 , A61K31/422 , A61K31/496 , A61K31/427 , A61K31/438 , A61K31/444 , A61K31/4545 , A61K31/4178 , A61K31/4725 , A61P31/14 , C07D263/32
CPC分类号： A61K31/415 , A61K31/4196 , A61K31/4245 , C07D231/12 , C07D233/58 , C07D233/64 , C07D249/06 , C07D249/08 , C07D249/12 , C07D263/32 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.
摘要翻译：本公开一般涉及抗病毒化合物，更具体地涉及可以抑制由丙型肝炎病毒（HCV）编码的NS5A蛋白的功能的化合物，包含这些化合物的组合物，以及用于抑制NS5A蛋白功能的方法。

4. 发明授权

US08362020B2 Hepatitis C virus inhibitors 有权
标题翻译：丙型肝炎病毒抑制剂
公开(公告)号：US08362020B2
公开(公告)日：2013-01-29
申请号：US12974069
申请日：2010-12-21
申请人： Omar D. Lopez , Denis R. St. Laurent , Jason Goodrich , Jeffrey Lee Romine , Michael Serrano-Wu , Fukang Yang , Ramesh Kakarla , Xuejie Yang , Yuping Qiu , Lawrence B. Snyder
发明人： Omar D. Lopez , Denis R. St. Laurent , Jason Goodrich , Jeffrey Lee Romine , Michael Serrano-Wu , Fukang Yang , Ramesh Kakarla , Xuejie Yang , Yuping Qiu , Lawrence B. Snyder
IPC分类号： A61K31/422 , A61K31/4025 , A61K31/496 , A61K31/427 , A61K31/438 , A61K31/444 , A61K31/4545 , C07D263/32 , C07D207/09 , C07D413/14 , C07D471/04 , C07D417/14
CPC分类号： A61K31/415 , A61K31/4196 , A61K31/4245 , C07D231/12 , C07D233/58 , C07D233/64 , C07D249/06 , C07D249/08 , C07D249/12 , C07D263/32 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.
摘要翻译：本公开一般涉及抗病毒化合物，更具体地涉及可以抑制由丙型肝炎病毒（HCV）编码的NS5A蛋白的功能的化合物，包含这些化合物的组合物，以及用于抑制NS5A蛋白功能的方法。

5. 发明授权

US08143288B2 Inhibitors of HCV replication 有权
标题翻译： HCV复制抑制剂
公开(公告)号：US08143288B2
公开(公告)日：2012-03-27
申请号：US11446788
申请日：2006-06-05
申请人： Michael Serrano-Wu , Makonen Belema , Lawrence B. Snyder , Nicholas A. Meanwell , Denis R. St. Laurent , Ramesh Kakarla , Van N. Nguyen , Yuping Qiu , Xuejie Yang , John E. Leet , Min Gao , Donald R. O'Boyle, II , Julie A. Lemm , Fukang Yang
发明人： Michael Serrano-Wu , Makonen Belema , Lawrence B. Snyder , Nicholas A. Meanwell , Denis R. St. Laurent , Ramesh Kakarla , Van N. Nguyen , Yuping Qiu , Xuejie Yang , John E. Leet , Min Gao , Donald R. O'Boyle, II , Julie A. Lemm , Fukang Yang
IPC分类号： A61K31/444 , A61K31/4439 , A61K31/42 , A61K31/416 , A61K31/4025 , C07D413/14 , C07D403/14 , C07D409/14
CPC分类号： C07D207/16 , C07D207/22 , C07D207/277 , C07D209/42 , C07D211/60 , C07D263/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： Compounds having the structure of formula I are described. The compounds can inhibit hepatitis C virus (HCV) replication, and in particular can inhibit the function of the HCV NS5A protein.
摘要翻译：描述具有式I结构的化合物。该化合物可以抑制丙型肝炎病毒（HCV）复制，特别是可以抑制HCV NS5A蛋白的功能。

6. 发明申请

US20060276511A1 Inhibitors of HCV replication 有权
标题翻译： HCV复制抑制剂
公开(公告)号：US20060276511A1
公开(公告)日：2006-12-07
申请号：US11446788
申请日：2006-06-05
申请人： Michael Serrano-Wu , Makonen Belema , Lawrence Snyder , Nicholas Meanwell , Denis St. Laurent , Ramesh Kakarla , Van Nguyen , Yuping Qiu , Xuejie Yang , John Leet , Min Gao , Donald O'Boyle , Julie Lemm , Fukang Yang
发明人： Michael Serrano-Wu , Makonen Belema , Lawrence Snyder , Nicholas Meanwell , Denis St. Laurent , Ramesh Kakarla , Van Nguyen , Yuping Qiu , Xuejie Yang , John Leet , Min Gao , Donald O'Boyle , Julie Lemm , Fukang Yang
IPC分类号： A61K31/444 , A61K31/4439 , A61K31/42 , A61K31/416 , A61K31/4025 , C07D413/14 , C07D403/14 , C07D409/14
CPC分类号： C07D207/16 , C07D207/22 , C07D207/277 , C07D209/42 , C07D211/60 , C07D263/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： Compounds having the structure of formula I are described. The compounds can inhibit hepatitis C virus (HCV) replication, and in particular can inhibit the function of the HCV NS5A protein.
摘要翻译：描述具有式I结构的化合物。该化合物可以抑制丙型肝炎病毒（HCV）复制，特别是可以抑制HCV NS5A蛋白的功能。

7. 发明授权

US06274716B1 Combinatorial library of moenomycin analogs and methods of producing same 失效
公开(公告)号：US06274716B1
公开(公告)日：2001-08-14
申请号：US09394044
申请日：1999-09-13
申请人： Nigel Mark Allanson , Tin Yau Chan , Nicole T. Hatzenbuhler , Rakesh K. Jain , Ramesh Kakarla , Rui Liang , Dashan Liu , Domingos J. Silva , Michael J. Sofia
发明人： Nigel Mark Allanson , Tin Yau Chan , Nicole T. Hatzenbuhler , Rakesh K. Jain , Ramesh Kakarla , Rui Liang , Dashan Liu , Domingos J. Silva , Michael J. Sofia
IPC分类号： C07H500
CPC分类号： C07H15/04 , C07H15/203 , C40B40/00
摘要： A combinatorial chemical library of compounds structurally related to the moenomycin class of antibiotics has the formula wherein D is a donor mono- or disaccharide, A is an acceptor monosaccharide, and P-R is a lipophosphoglycerate mimetic group. Members of the library have a glycosidic linkage between the anomeric carbon of D and the C2 carbon of A, and the D-A moiety is in turn covalently linked through the anomeric carbon of A to the P-R group. Members of the library exhibit their greatest structural diversity in terms of substitutions occurring at the C3 position of the A residue, substitutions at the C2 position of the D residue, and different P-R groups used in assembling the compounds. Members of the library are preferably synthesized by solid phase techniques involving stepwise coupling of the respective units to a support, functionalizing the A and/or D saccharides either before or after immobilizing them on the support, and cleaving the assembled compounds from the support. Preferred functionalities attached to the sugar residues are amides, carbamates, ureas, sulfonamides, substituted amines, esters, carbonates, and sulfates. Exemplary P-R groups are derivatives of homoserine, glyceric acid, salicylates and mandelic acid. Members of the library can be screened for anti-microbial activity by contacting them with a culture of microbes and monitoring the growth rate of the microbes.

8. 发明授权

US5864022A Process for the manufacture of 3-amino-substituted glycosylated bile acids 失效
标题翻译：制备3-氨基取代的糖基化胆汁酸的方法
公开(公告)号：US5864022A
公开(公告)日：1999-01-26
申请号：US822849
申请日：1997-03-24
申请人： Anna K. Chen , Ramesh Kakarla , Dashan Liu , Michael J. Sofia , Thomas C. Zebovitz
发明人： Anna K. Chen , Ramesh Kakarla , Dashan Liu , Michael J. Sofia , Thomas C. Zebovitz
IPC分类号： C07G3/00 , C07G99/00 , C07H15/18 , C07J3/00 , C07J9/00 , C07J17/00 , C07J31/00 , C07J41/00 , C07G17/00
CPC分类号： C07H15/18 , C07J17/005 , C07J31/006 , C07J41/0011 , C07J41/0027 , C07J9/005
摘要： The present invention relates to a process for the preparation and manufacture of 3-amino-substituted glycosylated bile acid derivatives. Intermediates and related compounds are also disclosed. In particular, the present invention permits the conversion of cholic acid esters to the 3-amino-7,12-bis(glucosyl)cholic acid esters via an azide intermediate. Conditions for the purification and isolation of the desired product is also disclosed to provide an overall manufacturing process suitable for large-scale production.
摘要翻译：本发明涉及制备和制备3-氨基取代的糖基化胆汁酸衍生物的方法。还公开了中间体和相关化合物。特别地，本发明允许通过叠氮化物中间体将胆酸酯转化为3-氨基-7,12-双（葡糖基）胆酸酯。还公开了所需产物的纯化和分离的条件，以提供适合于大规模生产的总体制造方法。

9. 发明授权

US06114309A Combinatorial library of moenomycin analogs and methods of producing same 失效
标题翻译：霉酚霉素类似物组合库及其生产方法
公开(公告)号：US06114309A
公开(公告)日：2000-09-05
申请号：US975229
申请日：1997-11-21
申请人： Nigel Mark Allanson , Tin Yau Chan , Nicole T. Hatzenbuhler , Rakesh K. Jain , Ramesh Kakarla , Rui Liang , Dashan Liu , Domingos J. Silva , Michael J. Sofia
发明人： Nigel Mark Allanson , Tin Yau Chan , Nicole T. Hatzenbuhler , Rakesh K. Jain , Ramesh Kakarla , Rui Liang , Dashan Liu , Domingos J. Silva , Michael J. Sofia
IPC分类号： C12Q1/02 , A61K31/7016 , A61K31/702 , A61P31/04 , C07B61/00 , C07H1/02 , C07H5/08 , C07H11/04 , C07H15/04 , C07H15/203 , A61K31/70 , C07H13/00
CPC分类号： C07H15/04 , C07H15/203 , C40B40/00
摘要： A combinatorial chemical library of compounds structurally related to the moenomycin class of antibiotics has the formula ##STR1## wherein D is a donor mono- or disaccharide, A is an acceptor monosaccharide, and P-R is a lipophosphoglycerate mimetic group. Members of the library have a glycosidic linkage between the anomeric carbon of D and the C2 carbon of A, and the D-A moiety is in turn covalently linked through the anomeric carbon of A to the P-R group. Members of the library exhibit their greatest structural diversity in terms of substitutions occurring at the C3 position of the A residue, substitutions at the C2 position of the D residue, and different P-R groups used in assembling the compounds. Members of the library are preferably synthesized by solid phase techniques involving stepwise coupling of the respective units to a support, functionalizing the A and/or D saccharides either before or after immobilizing them on the support, and cleaving the assembled compounds from the support. Preferred functionalities attached to the sugar residues are amides, carbamates, ureas, sulfonamides, substituted amines, esters, carbonates, and sulfates. Exemplary P-R groups are derivatives of homoserine, glyceric acid, salicylates and mandelic acid. Members of the library can be screened for anti-microbial activity by contacting them with a culture of microbes and monitoring the growth rate of the microbes.
摘要翻译：结构上与新霉素类抗生素相关的化合物的组合化学文库具有下式：其中D是供体单糖或二糖，A是受体单糖，P-R是脂磷酸甘油酸酯模拟组。文库成员在D的异头碳和A的C2碳之间具有糖苷键，D-A部分又通过A的端基异碳共价连接到P-R基团。关于在A残基的C3位置发生的取代，在D残基的C2位置的取代以及用于组装化合物的不同的P-R基团，图书馆的成员表现出最大的结构多样性。文库的成员优选通过固相技术合成，其包括将各单元逐步偶联到载体上，在将它们固定在载体上之前或之后将A和/或D糖功能化，并将载体化合物从载体上分离。附着于糖残基的优选功能是酰胺，氨基甲酸酯，脲，磺酰胺，取代的胺，酯，碳酸酯和硫酸酯。示例性的P-R基团是高丝氨酸，甘油酸，水杨酸盐和扁桃酸的衍生物。通过与微生物培养物接触并监测微生物的生长速率，可以筛选图书馆成员的抗菌活性。

10. 发明授权

US5731423A Process for preparing sulfoxides 失效
标题翻译：亚砜制备方法
公开(公告)号：US5731423A
公开(公告)日：1998-03-24
申请号：US619170
申请日：1996-03-21
申请人： Ramesh Kakarla , Michael J. Sofia
发明人： Ramesh Kakarla , Michael J. Sofia
IPC分类号： C07C315/02 , C07C317/04 , C07C317/14 , C07G3/00
CPC分类号： C07G3/00 , C07C315/02
摘要： A process is disclosed for making a compound having a sulfoxide group comprising providing a first compound having a sulfide group and contacting said first compound with an oxidizing agent in the presence of silica and a carboxylic acid anhydride. In a particular embodiment of the invention, the high yield preparation of glycoside moieties having anomeric sulfoxides at ambient temperature is described.
摘要翻译：公开了制备具有亚砜基的化合物的方法，包括提供具有硫化物基团的第一化合物，并在二氧化硅和羧酸酐的存在下使所述第一化合物与氧化剂接触。在本发明的一个具体实施方案中，描述了在环境温度下具有异构亚砜的糖苷部分的高产率制备。

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