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1. 发明授权

US5627270A Glycosylated steroid derivatives for transport across biological membranes and process for making and using same 失效
公开(公告)号：US5627270A
公开(公告)日：1997-05-06
申请号：US264488
申请日：1994-06-23
申请人： Daniel E. Kahne , Suzanne W. Kahne , Michael J. Sofia , Nicole T. Hatzenbuhler
发明人： Daniel E. Kahne , Suzanne W. Kahne , Michael J. Sofia , Nicole T. Hatzenbuhler
IPC分类号： C07J9/00 , C07J17/00 , C07J31/00 , C07J41/00 , C07J43/00 , C07J51/00 , C12N15/87 , C07H21/02 , C07H21/04
CPC分类号： A61K47/48092 , C07J17/005 , C07J31/006 , C07J41/0005 , C07J41/0011 , C07J41/0027 , C07J41/0061 , C07J43/003 , C07J51/00 , C07J9/005 , C12N15/87
摘要： Novel glycosylated steroid derivatives for facilitating the transport of compounds across biological membranes, either in admixture or as conjugates, are disclosed. A novel process for efficient synthesis of these glycosylated steroid derivatives, using activated glycosyl sulfoxide intermediates is provided. Methods for the permeabilization of membranes and the enhancement of the activity of predetermined compounds are also provided.

2. 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。

3. 发明授权

US06207820B1 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：US06207820B1
公开(公告)日：2001-03-27
申请号：US09394045
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： C07H100
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.
摘要翻译：结构上与霉酚霉素类抗生素有关的化合物的组合化学文库，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。

4. 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.

5. 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。

6. 发明授权

US5352690A 1,2,4-trioxygenated benzene derivatives useful as leukotriene antagonists 失效
标题翻译：可用作白三烯拮抗剂的1,2,4-三氧化苯衍生物
公开(公告)号：US5352690A
公开(公告)日：1994-10-04
申请号：US907492
申请日：1992-07-01
申请人： Michael J. Sofia
发明人： Michael J. Sofia
IPC分类号： A61K31/085 , A61K31/09 , A61K31/10 , A61K31/16 , A61K31/165 , A61K31/185 , A61K31/19 , A61K31/35 , A61K31/352 , A61K31/365 , A61K31/40 , A61K31/41 , A61K31/445 , A61K31/495 , A61P29/00 , A61P37/08 , A61P43/00 , C07D257/04 , C07D295/18 , C07D311/66 , C07D257/06 , A61K31/37 , C07D311/74
CPC分类号： C07D257/04 , C07D311/66
摘要： This invention provides 1,2,4-trioxygenated benzene derivatives which are leukotriene B.sub.4 antagonists, formulations of those derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
摘要翻译：本发明提供了作为白三烯B4拮抗剂的1,2,4-三氧化苯衍生物，这些衍生物的制剂，以及使用这些衍生物治疗以白细胞三烯过度释放为特征的病症的方法。

7. 发明授权

US5478857A Use of PLA.sub.2 inhibitors as treatment for alzheimer's disease 失效
标题翻译：使用PLA2抑制剂作为阿尔茨海默病的治疗
公开(公告)号：US5478857A
公开(公告)日：1995-12-26
申请号：US173544
申请日：1993-12-23
申请人： James A. Clemens , Michael J. Sofia , Diane T. Stephenson
发明人： James A. Clemens , Michael J. Sofia , Diane T. Stephenson
IPC分类号： C07D311/66 , A61K31/00 , A61K31/165 , A61K31/18 , A61K31/19 , A61K31/35 , A61K31/352 , A61K31/41 , A61K45/00 , A61P25/28 , A61P43/00 , C07C59/68 , C07C65/21 , C07C65/32 , C07C65/40 , C07C69/712 , C07C235/34 , C07C311/51 , C07D257/04 , C07D311/86 , A61K31/335
CPC分类号： A61K31/00 , A61K31/165 , A61K31/18 , A61K31/19 , A61K31/35 , A61K31/41
摘要： This invention provides methods for the treatment or prevention of Alzheimer's disease in a mammal which comprises administering to a mammal in need thereof an effective amount of an inhibitor of phospholipase A.sub.2. This invention also provides a series of compounds which are useful as inhibitors of phospholipases A.sub.2, especially cytosolic phospholipase A.sub.2.
摘要翻译：本发明提供了在哺乳动物中治疗或预防阿尔茨海默氏病的方法，其包括向有需要的哺乳动物施用有效量的磷脂酶A2抑制剂。本发明还提供一系列化合物，其可用作磷脂酶A2，特别是胞浆磷脂酶A2的抑制剂。

8. 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。

9. 发明授权

US5091378A Phosphorus-containing HMG-CoA reductase inhibitors, new intermediates and method 失效
标题翻译：含磷的HMG-CoA还原酶抑制剂，新中间体和方法
公开(公告)号：US5091378A
公开(公告)日：1992-02-25
申请号：US182710
申请日：1988-04-18
申请人： Donald S. Karanewsky , Michael C. Badia , Scott A. Biller , Eric M. Gordon , Michael J. Sofia
发明人： Donald S. Karanewsky , Michael C. Badia , Scott A. Biller , Eric M. Gordon , Michael J. Sofia
IPC分类号： C07F9/30 , C07F9/32 , C07F9/40 , C07F9/572 , C07F9/6503 , C07F9/6506
CPC分类号： C07F9/65062 , C07F9/301 , C07F9/302 , C07F9/303 , C07F9/306 , C07F9/3211 , C07F9/3217 , C07F9/3241 , C07F9/4006 , C07F9/5721 , C07F9/5722 , C07F9/5728 , C07F9/65033
摘要： Compounds which are useful as inhibitors of cholesterol biosynthesis and thus as hypocholesteroleumic agents are provided which have the structure ##STR1## wherein R is OH, or salts thereof or lower alkoxy; R.sup.x is H or alkyl;X is --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --CH.sub.2 CH.sub.2 CH.sub.2 -- or --CH.sub.2 O-- (where O is linked to Z);Z is a hydrophobic anchor, such as ##STR2## wherein the dotted lines represent optional double bonds. New intermediates used in preparing the above compounds, pharmaceutical compositions containing such compounds and a method for using such compounds to inhibit cholesterol biosynthesis are also provided.
摘要翻译：提供了可用作胆固醇生物合成抑制剂并因此作为低胆固醇血症药物的化合物，其具有其中R为OH的结构，或其盐或低级烷氧基; Rx是H或烷基; X是-CH 2 - ， - CH 2 -CH 2 - ， - CH = CH - ， - C 3BOND C - ， - CH 2 CH 2 CH 2 - 或-CH 2 O-（其中O与Z连接）; Z是疏水锚，例如其中虚线表示任选的双键。还提供了用于制备上述化合物的新中间体，含有这些化合物的药物组合物和使用这些化合物抑制胆固醇生物合成的方法。

10. 发明授权

US6017906A Polyamine conjugates for treatment of infection 失效
标题翻译：用于治疗感染的多胺缀合物
公开(公告)号：US6017906A
公开(公告)日：2000-01-25
申请号：US72182
申请日：1998-05-05
申请人： Clifford S. Mintz , Natan A. Kogan , Ramesh Kakarla , Helena R. Axelrod , Michael J. Sofia
发明人： Clifford S. Mintz , Natan A. Kogan , Ramesh Kakarla , Helena R. Axelrod , Michael J. Sofia
IPC分类号： A61K31/575 , A61K31/715 , A61K31/56
CPC分类号： A61K31/575
摘要： The present invention relates to methods of preventing or treating an infection or disease caused by an infectious agent. The present invention also relates to the augmentation of the efficacy of existing anti-infective agents by the co-administration of the compounds described herein.
摘要翻译：本发明涉及预防或治疗感染性疾病引起的感染或疾病的方法。本发明还涉及通过共同给予本文所述的化合物来增加现有抗感染剂的功效。

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