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1. 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.

2. 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。

3. 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。

4. 发明授权

US5693770A 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：US5693770A
公开(公告)日：1997-12-02
申请号：US494194
申请日：1995-06-23
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 , C07H15/24
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. Novel 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。还公开了新的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。

5. 发明授权

US5552441A Leukotriene B4 antagonists 失效
标题翻译：白三烯B4拮抗剂
公开(公告)号：US5552441A
公开(公告)日：1996-09-03
申请号：US195951
申请日：1994-02-14
申请人： Robert D. Dillard , J. Scott Sawyer , Michael J. Sofia
发明人： Robert D. Dillard , J. Scott Sawyer , Michael J. Sofia
IPC分类号： C07C59/90 , C07C65/40 , C07C69/712 , C07C69/734 , C07C69/92 , C07D307/91 , C07D311/66 , C07D311/86 , A61K31/19 , C07C63/04
CPC分类号： C07D307/91 , C07C59/90 , C07C65/40 , C07C69/712 , C07C69/734 , C07C69/92 , C07D311/66 , C07D311/86
摘要： This invention provides certain 1,2,4,5 substituted benzene derivatives containing "acid" substituents derived from cyclic or heterocyclic moieties. These unique compounds are leukotriene B.sub.4 antagonists and formulations of these derivatives, and a method of using these derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
摘要翻译：本发明提供了含有衍生自环状或杂环部分的“酸”取代基的某些1,2,4,5取代的苯衍生物。这些独特的化合物是白三烯B4拮抗剂和这些衍生物的制剂，以及使用这些衍生物来治疗以白细胞三烯过度释放为特征的病症的方法。

6. 发明授权

US5462954A Substituted phenyl phenol leukotriene antagonists 失效
标题翻译：取代的苯酚白三烯拮抗剂
公开(公告)号：US5462954A
公开(公告)日：1995-10-31
申请号：US333122
申请日：1994-11-01
申请人： S. Richard Baker , Robert D. Dillard , Paul E. Floreancig , J. Scott Sawyer , Michael J. Sofia
发明人： S. Richard Baker , Robert D. Dillard , Paul E. Floreancig , J. Scott Sawyer , Michael J. Sofia
IPC分类号： C07C45/46 , C07C45/67 , C07C45/71 , C07C47/575 , C07C49/84 , C07C59/68 , C07C65/24 , C07C65/40 , C07C69/736 , C07C69/92 , C07C235/20 , C07C255/54 , C07C311/51 , C07C317/44 , C07C319/18 , C07C323/12 , C07C323/20 , C07C323/62 , C07D20060101 , C07D257/04 , C07D295/185 , C07D307/91 , C07D311/18 , C07D311/66 , C07D311/86 , A61K31/19 , A61K31/41 , C07D311/24
CPC分类号： C07D257/04 , C07C235/20 , C07C255/54 , C07C311/51 , C07C317/44 , C07C319/18 , C07C323/12 , C07C323/20 , C07C323/62 , C07C45/46 , C07C45/673 , C07C45/71 , C07C47/575 , C07C49/84 , C07C59/68 , C07C65/24 , C07C65/40 , C07C69/736 , C07C69/92 , C07D295/185 , C07D307/91 , C07D311/18 , C07D311/66 , C07D311/86
摘要： Antagonists having a substituted phenyl phenol or a substituted phenolic biphenyl structure, and various derivatives thereof, are specific leukotriene antagonists. Their structures, use and synthesis are disclosed. Also, pharmaceutical formulations are disclosed for use in applications treating diseases or conditions characterized by excessive release of leukotriene B.sub.4, one of the metabolites of arachidonic acid.The primary LTB.sub.4 antagonistic structures are represented as: ##STR1##
摘要翻译：具有取代苯基苯酚或取代的酚类联苯结构的拮抗剂及其各种衍生物是特异性白三烯拮抗剂。公开了它们的结构，用途和合成。此外，公开了用于治疗疾病或特征为过度释放白三烯B4（其是花生四烯酸的代谢物之一）的应用的药物制剂。主要的LTB4拮抗结构表示为：

7. 发明授权

US5324743A Leukotriene B.sub.4 antagonists 失效
标题翻译：白三烯B4拮抗剂
公开(公告)号：US5324743A
公开(公告)日：1994-06-28
申请号：US988615
申请日：1992-12-10
申请人： Robert D. Dillard , J. Scott Sawyer , Michael J. Sofia
发明人： Robert D. Dillard , J. Scott Sawyer , Michael J. Sofia
IPC分类号： C07C59/90 , C07C65/40 , C07C69/712 , C07C69/734 , C07C69/92 , C07D307/91 , C07D311/66 , C07D311/86 , A61K31/35 , C07D311/58
CPC分类号： C07D307/91 , C07C59/90 , C07C65/40 , C07C69/712 , C07C69/734 , C07C69/92 , C07D311/66 , C07D311/86
摘要： This invention provides certain 1,2,4,5 substituted benzene derivatives containing "acid" substituents derived from cyclic or heterocyclic moieties. These unique compounds are leukotriene B.sub.4 antagonists and formulations of these derivatives, and a method of using these derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
摘要翻译：本发明提供了含有衍生自环状或杂环部分的“酸”取代基的某些1,2,4,5取代的苯衍生物。这些独特的化合物是白三烯B4拮抗剂和这些衍生物的制剂，以及使用这些衍生物来治疗以白细胞三烯过度释放为特征的病症的方法。

8. 发明授权

US5276021A 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，新的中间体和方法
公开(公告)号：US5276021A
公开(公告)日：1994-01-04
申请号：US810099
申请日：1991-12-19
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 , C07F9/02 , C07C69/73 , A61K31/66
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 hypocholesterolemic 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.
摘要翻译：提供可用作胆固醇生物合成抑制剂，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（*化学结构*），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（三键）C - ， - CH 2 CH 2 CH 2 - 或-CH 2 O-（其中O与Z连接）; （*化学结构*）（*化学结构*）（*化学结构*）（*化学结构*）（*化学结构*）（*化学结构*）（*化学结构*）其中虚线表示任选的双键。

9. 发明授权

US5273969A Phosphorus-containing squalene synthetase inhibitors and method 失效
标题翻译：含磷角鲨烯合成酶抑制剂及方法
公开(公告)号：US5273969A
公开(公告)日：1993-12-28
申请号：US31512
申请日：1993-03-15
申请人： Scott A. Biller , Michael J. Sofia
发明人： Scott A. Biller , Michael J. Sofia
IPC分类号： C07F9/38 , C07F9/40 , C07F9/44 , A61K31/66
CPC分类号： C07F9/4469 , C07F9/3821 , C07F9/4012 , C07F9/4028 , C07F9/4037 , C07F9/4078
摘要： Compounds which are inhibitors of cholesterol biosynthesis (by inhibiting de novo squalene biosynthesis), and thus are useful as hypocholesterolemic agents and antiatherosclerotic agents are provided which have the structure ##STR1## wherein m is 0, 1, 2 or 3; n is 0, 1, 2, 3 or 4;Y.sup.1 and Y.sup.2 are H or halogen;R.sup.2, R.sup.3 and R.sup.4 may be the same or different and are independently H, metal ion, C.sub.1 to C.sub.8 alkyl or C.sub.3 to C.sub.12 alkenyl;X is O, S, NH or NCH.sub.2 R.sup.15 wherein R.sup.15 is H or C.sub.1 to C.sub.5 alkyl; andR.sup.1 is R.sup.5 --Q.sup.1 --Q.sup.2 --Q.sup.3 -- wherein R.sup.5, Q.sup.1, Q.sup.2 and Q.sup.3 are as defined herein;and when m is o, X is other than S; and if m is o and X is O, then n is 1, 2, 3 or 4; including all stereoisomers thereof.
摘要翻译：作为胆固醇生物合成抑制剂的化合物（通过抑制从头角鲨烯生物合成），因此可用作具有下列结构的降血胆固醇药和抗动脉粥样硬化剂：其中m为0,1,2或3; n为0,1,2,3或4; Y1和Y2是H或卤素; R 2，R 3和R 4可以相同或不同，并且独立地为H，金属离子，C 1至C 8烷基或C 3至C 12链烯基; X是O，S，NH或NCH 2 R 15，其中R 15是H或C 1至C 5烷基; 并且R1是R5-Q1-Q2-Q3-，其中R5，Q1，Q2和Q3如本文所定义; 而当m为o时，X不为S; 如果m为o，X为O，则n为1,2,3或4; 包括其所有的立体异构体。

10. 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。

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