专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US5660992A Sialic acid/fucose based assay reagents and assay methods 失效
标题翻译：唾液酸/岩藻糖基测定试剂和测定方法
公开(公告)号：US5660992A
公开(公告)日：1997-08-26
申请号：US464507
申请日：1995-06-05
申请人： Falguni Dasgupta , John Henry Musser
发明人： Falguni Dasgupta , John Henry Musser
IPC分类号： C07H3/06 , C07H11/00 , C07H15/04 , A61K51/00 , A61M36/14 , G01N33/53 , G01N33/567
CPC分类号： C07H3/06 , C07H11/00 , C07H15/04
摘要： Compounds that are synthetically inexpensive to make relative to the naturally occurring selectin ligands and that retain selectin binding activity are described that have a three-dimensionally stable configuration for sialic acid and fucose, or analogs or derivatives of these groups, such that sialic acid and fucose are separated by a non-carbohydrate linker that permits binding between those groups and the selectins, such compounds being represented by the following general structural formula I(a): ##STR1## wherein m and n are independently an integer of from 1 to 5, Y and Z are independently a connecting moiety selected from the group consisting of --CH.sub.2 --, --O--, --S--, --NR' and --NR'R"-- (wherein R' and R" are independently H or an alkyl containing 1 to 4 carbon atoms); X is a connecting moiety which is selected from the group consisting of --O--, --S--and --N--; and --R'" may be --R" or any moiety which does not interfere with the three-dimensional configuration of A or B so as to interfere with selectin binding and is preferably a moiety selected from the group consisting of --OR", --SR", --I, --N.sub.3, and --NR'R" and A is selected from the group consisting of .alpha. and .beta. forms of sialic acid, Kemp's acid, Quinic acid, Glyceric acid, Lactic acid and acetic acid, and esters thereof and B is selected from the group consisting of .alpha. and .beta. forms of L-Fucose and esters and substituted forms thereof wherein one or more of the --OH groups is independently --F, or --NR.sup.IV, R.sup.V wherein R.sup.IV and R.sup.V are independently an alkyl contain 1 to 5 carbons.
摘要翻译：描述了相对于天然存在的选择蛋白配体合成成本并且保留选择蛋白结合活性的化合物，其对于唾液酸和岩藻糖或这些基团的类似物或衍生物具有三维稳定的构型，使得唾液酸和岩藻糖由允许这些基团和选择素之间结合的非碳水化合物接头分开，这些化合物由以下通式结构式I（a）表示：其中m和n独立地为1至5的整数， Y和Z独立地是选自-CH 2 - ， - O - ， - S - ， - NR'和-NR'R“ - 的连接部分（其中R'和R”独立地是H或含有1至4个碳原子的烷基）; X是选自-O - ， - S-和-N-的连接部分; 和-R“可以是-R”或不干扰A或B的三维构型以干扰选择素结合的任何部分，并且优选是选自-OR'的部分， '，-SR“，-I，-N3和-NR'R”，A选自唾液酸，肯普酸，奎宁酸，甘油酸，乳酸和乙酸的α和β形式酸及其酯，B选自α-岩藻糖的α型和β型及其酯及其取代形式，其中一个或多个-OH基团独立地为-F，或-NRIV，RV，其中RIV和 RV独立地为含有1至5个碳的烷基。

2. 发明授权

US5962422A Inhibition of selectin binding 失效
标题翻译：抑制选择素结合
公开(公告)号：US5962422A
公开(公告)日：1999-10-05
申请号：US807428
申请日：1997-02-28
申请人： Jon O. Nagy , Wayne R. Spevak , Falguni Dasgupta , Carolyn Bertozzi
发明人： Jon O. Nagy , Wayne R. Spevak , Falguni Dasgupta , Carolyn Bertozzi
IPC分类号： A61K9/127 , A61K9/70 , A61K31/70 , A61K31/715 , A61K31/726 , A61K47/44 , A61K47/48 , A61P9/00 , A61P9/10 , A61P11/06 , A61P29/00 , A61P35/04 , A61P43/00 , G01N33/53
CPC分类号： A61K31/7024 , A61K9/1273
摘要： This invention provides a system for inhibiting the binding between two cells, one expressing P- or L-selectin on the surface and the other expressing the corresponding ligand. A covalently crosslinked lipid composition is prepared having saccharides and acidic group on separate lipids. The composition is then interposed between the cells so as to inhibit binding. Inhibition can be achieved at an effective oligosaccharide concentration as low as 10.sup.6 fold below that of the free saccharide. Since selectins are involved in recruiting cells to sites of injury, this system can be used to palliate certain inflammatory and immunological conditions.
摘要翻译：本发明提供了抑制两个细胞之间的结合的系统，一个在表面上表达P-或L-选择蛋白，另一个表达相应的配体。制备在单独的脂质上具有糖和酸性基团的共价交联的脂质组合物。然后将组合物置于细胞之间以抑制结合。可以在低于游离糖的106倍的有效寡糖浓度下实现抑制。由于选择素参与将细胞募集到损伤部位，因此该系统可用于缓解某些炎症和免疫条件。

3. 发明授权

US5985852A Inhibition of selectin binding 失效
标题翻译：抑制选择素结合
公开(公告)号：US5985852A
公开(公告)日：1999-11-16
申请号：US250999
申请日：1999-02-16
申请人： Jon O. Nagy , Wayne R. Spevak , Falguni Dasgupta , Caroline Bertozzi
发明人： Jon O. Nagy , Wayne R. Spevak , Falguni Dasgupta , Caroline Bertozzi
IPC分类号： A61K9/127 , A61K9/70 , A61K31/70 , A61K31/715 , A61K31/726 , A61K47/44 , A61K47/48 , A61P9/00 , A61P9/10 , A61P11/06 , A61P29/00 , A61P35/04 , A61P43/00 , C07H1/00
CPC分类号： A61K31/7024 , A61K9/1273
摘要： This invention provides compositions for inhibiting the binding between two cells, one expressing P- or L-selectin on the surface and the other expressing the corresponding ligand. A covalently crosslinked lipid composition is prepared having saccharides and acidic group on separate lipids. The composition is then interposed between the cells so as to inhibit binding. Inhibition can be achieved at an effective oligosaccharide concentration as low as 10.sup.6 fold below that of the free saccharide. Since selectins are involved in recruiting cells to sites of injury, these composition scan be used to palliate certain inflammatory and immunological conditions.
摘要翻译：本发明提供用于抑制两个细胞之间的结合的组合物，一个在表面上表达P-或L-选择蛋白，另一个表达相应的配体。制备在单独的脂质上具有糖和酸性基团的共价交联的脂质组合物。然后将组合物置于细胞之间以抑制结合。可以在低于游离糖的106倍的有效寡糖浓度下实现抑制。由于选择素参与将细胞募集到损伤部位，所以这些组合物扫描可用于缓解某些炎症和免疫条件。

4. 发明授权

US5750508A Sialic acid/fucose based medicaments 失效
标题翻译：唾液酸/岩藻糖基药物
公开(公告)号：US5750508A
公开(公告)日：1998-05-12
申请号：US78949
申请日：1993-06-16
申请人： Falguni Dasgupta , John Henry Musser
发明人： Falguni Dasgupta , John Henry Musser
IPC分类号： C07H3/06 , C07H11/00 , C07H15/04 , A61K31/70 , C07H15/00
CPC分类号： C07H3/06 , C07H11/00 , C07H15/04
摘要： Compounds that are synthetically inexpensive to make relative to the naturally occurring selectin ligands and that retain selectin binding activity are described that have a three-dimensionally stable configuration for sialic acid and fucose, or analogs or derivatives of these groups, such that sialic acid and fucose are separated by a non-carbohydrate linker that permits binding between those groups and the selectins, such compounds being represented by the following general structure formula I(a): ##STR1## wherein m and n are independently an integer of from 1 to 5, Y and Z are independently a connecting moiety selected from the group consisting of --CH.sub.2 --, --O--, --S--, --NR'and --NR'R"--(wherein R' and R" are independently H or an alkyl containing 1 to 4 carbon atoms); X is a connecting moiety which is selected from the group consisting of --O--, --S-- and --N--; and --R" may be --R'" or any moiety which does not interfere with the three-dimensional configuration of A or B so as to interfere with selectin binding and is preferably a moiety selected from the group consisting of --OR", --SR", --I, --N.sub.3, and --NR'R", and A is selected from the group consisting of .alpha. and .beta. forms of sialic acid, Kemp's acid. Quinic acid, Glyceric acid, Lactic acid and acetic acid, and esters thereof and B is selected from the group consisting of .alpha. and .beta. forms of L-Fucose and esters and substituted forms thereof wherein one or more of the --OH groups is independently --F, or --NR.sup.IV, R.sup.V wherein R.sup.IV and R.sup.V are independently an alkyl contain 1 to 5 carbons.
摘要翻译：描述了相对于天然存在的选择蛋白配体合成成本并且保留选择蛋白结合活性的化合物，其对于唾液酸和岩藻糖或这些基团的类似物或衍生物具有三维稳定的构型，使得唾液酸和岩藻糖被允许这些基团和选择素之间的结合的非碳水化合物接头分开，这些化合物由以下通式I（a）表示：其中m和n独立地为1至5的整数， Y和Z独立地是选自-CH 2 - ， - O - ， - S - ， - NR'和-NR'R“ - 的连接部分（其中R'和R”独立地是H或含有1至4个碳原子的烷基）; X是选自-O - ， - S-和-N-的连接部分; 或者-R“可以是-R”或不干扰A或B的三维构型以干扰选择素结合的部分，优选为选自-OR'的部分， '，-SR“，-I，-N3和-NR'R”，A选自唾液酸，肯普酸的α和β形式。奎宁酸，甘油酸，乳酸和乙酸及其酯，B选自α-和β形式的L-岩藻糖及其酯及其取代形式，其中一个或多个-OH基团独立地为 - F或-NRIV，RV，其中RIV和RV独立地为含有1至5个碳的烷基。

5. 发明授权

US5567683A Substituted lactose and lactosamine derivatives as cell adhesion inhibitors 失效
标题翻译：取代的乳糖和乳糖胺衍生物作为细胞粘附抑制剂
公开(公告)号：US5567683A
公开(公告)日：1996-10-22
申请号：US270874
申请日：1994-07-01
申请人： Mina A. Nashed , Falguni Dasgupta , Saeed A. Abbas , John H. Musser , Darwin S. Asa
发明人： Mina A. Nashed , Falguni Dasgupta , Saeed A. Abbas , John H. Musser , Darwin S. Asa
IPC分类号： C07H5/04 , A61K31/7008 , A61K31/7024 , A61K31/7028 , A61K31/7034 , A61K31/7042 , A61K31/715 , A61P29/00 , A61P37/06 , A61P37/08 , C07H3/06 , C07H5/10 , C07H13/04 , C07H15/20 , C07H17/00 , A61K31/70 , A61K38/00 , A61K38/16
CPC分类号： C07H3/06
摘要： Simple lactose or lactosamine related compounds which behave as ligands for the ELAM-1 and related receptors are described. These compounds are useful in the treatment of conditions characterized by excess inflammation. These compounds are of the formula ##STR1## wherein each R.sup.1 is independently H or lower alkyl (1-4C); R.sup.2 is H, lower alkyl (1-4C), alkylaryl or one or more additional saccharide residues;R.sup.3 and R.sup.4 are each independently H, alkyl(1-6C), aryl or R.sup.3 and R.sup.4, taken together, form a five- or six-membered ring optionally containing a heteroatom selected from the group consisting of O, S, and NR.sup.1 ;wherein said five- or six-membered ring may further be substituted by one or more substituents selected from the group consisting of (CHOR.sup.1).sub.m H wherein m is 1-4, OR.sup.1, OOCR.sup.1, NR.sup.1.sub.2, NHCOR.sup.1, and SR.sup.1 ;Y is H, OR.sup.1, OOCR.sup.1, NR.sup.1.sub.2, NCOR.sup.1 or SR.sup.1 ; andX is --CHR.sup.5 (CHOR.sup.1).sub.2 CHR.sup.6 OR.sup.1 wherein R.sup.5 and R.sup.6 are each independently H, lower alkyl(1-4C) optionally substituted with one or more F, or result in a five- or six-membered ring optionally containing a heteroatom selected from the group consisting of O, S, and NR.sup.1 ;said five- or six-membered ring optionally substituted with one substituent selected from the group consisting of R.sup.1, CH.sub.2 OR.sup.1, OR.sup.1, OOCR.sup.1, NR.sup.1.sub.2, NHCOR.sup.1, SR.sup.1 and F;or X is benzoyl or naphthoyl having 1-3 hydroxyl substituents,with the proviso that if X represents a hexose substituent R.sup.3 and R.sup.4, taken together, cannot provide a hexose substituent.
摘要翻译：描述了作为ELAM-1和相关受体的配体的简单的乳糖或乳糖胺相关化合物。这些化合物可用于治疗以过量炎症为特征的病症。这些化合物具有式“IMAGE”，其中每个R 1独立地是H或低级烷基（1-4C）; R2是H，低级烷基（1-4C），烷基芳基或一个或多个另外的糖残基; R 3和R 4各自独立地为H，烷基（1-6C），芳基或R 3和R 4一起形成任选含有选自O，S和NR 1的杂原子的五元或六元环; 其中所述五元或六元环可以进一步被一个或多个选自（CHOR1）mH的取代基取代，其中m是1-4，OR1，OOCR1，NR12，NHCOR1和SR1; Y是H，OR1，OOCR1，NR12，NCOR1或SR1; 并且X是-CHR 5（CHOR 1）2 CHR 6OR 1，其中R 5和R 6各自独立地为H，任选地被一个或多个F取代的低级烷基（1-4C），或者产生任选含有选自以下的杂原子的五元或六元环由O，S和NR1组成的组; 所述五元或六元环任选被一个选自由R 1，CH 2 OR 1，OR 1，OOCR 1，NR 12，NHCOR 1，SR 1和F的取代基取代; 或X是具有1-3个羟基取代基的苯甲酰基或萘甲酰基，条件是如果X表示己糖取代基R 3和R 4一起不能提供己糖取代基。

6. 发明授权

US08728453B2 Combinatorial polymeric compositions for drug delivery 有权
标题翻译：用于药物递送的组合聚合物组合物
公开(公告)号：US08728453B2
公开(公告)日：2014-05-20
申请号：US13407388
申请日：2012-02-28
申请人： Falguni Dasgupta
发明人： Falguni Dasgupta
IPC分类号： A61K31/74
CPC分类号： C08G75/28 , A61K47/59 , C08G75/04 , C08G75/045
摘要： The present invention is directed towards the synthesis of polymeric drug delivery compositions which would address some of the important and difficult to realize aspects of polymer based drug delivery systems by being, biocompatible, stable, capable of achieving desired drug loading, and safe from accidental release while being non-toxic, easy to fabricate and safe for the environment.
摘要翻译：本发明涉及聚合物药物递送组合物的合成，其通过生物相容性，稳定性，能够实现期望的药物加载并且避免意外释放来解决基于聚合物的药物递送系统的一些重要且难以实现的方面同时无毒，易于制造和安全的环境。

7. 发明申请

US20120184682A1 BIOCOMPATIBLE AND BIODEGRADABLE POLYMERS FROM RENEWABLE NATURAL POLYPHENOLS 有权
标题翻译：可再生天然多酚的生物降解和生物降解聚合物
公开(公告)号：US20120184682A1
公开(公告)日：2012-07-19
申请号：US13498886
申请日：2010-09-30
申请人： Falguni Dasgupta
发明人： Falguni Dasgupta
IPC分类号： C08F8/00 , C07C68/00 , C07C49/255 , C08G18/28 , C07C43/215 , C07C41/01 , C08G64/16 , C08G18/67 , C07C69/96 , C07C45/68
CPC分类号： C08G64/06 , C07C43/215 , C07C49/225 , C07C69/96 , C08G18/3215 , C08G18/44 , C08G63/193 , C08G63/547 , C08G64/045 , C08G64/14 , C08G65/40 , C08G65/44 , C08G75/0227 , C08G75/045 , C08G75/28
摘要： This invention describes the use of resveratrol and curcumin, representatives of naturally occurring polyphenols, in their native form, after hydrogenation, and as their respective allyl derivatives, individually, in combination with themselves and other commercial monomers, to make representative varieties of polymers, e.g., polycarbonates (PC), polyurethanes (PU), co-polymers and biodegradable polymers.
摘要翻译：本发明描述了白藜芦醇和姜黄素，天然存在的多酚的代表，其天然形式，氢化之后，以及作为它们各自的烯丙基衍生物与本身和其它商业单体组合使用以制备代表性的聚合物，例如，聚碳酸酯（PC），聚氨酯（PU），共聚物和可生物降解的聚合物。

8. 发明授权

US5679321A Sialic acid/fucose based medicaments 失效
标题翻译：唾液酸/岩藻糖基药物
公开(公告)号：US5679321A
公开(公告)日：1997-10-21
申请号：US468788
申请日：1995-06-06
申请人： Falguni Dasgupta , John Henry Musser
发明人： Falguni Dasgupta , John Henry Musser
IPC分类号： G01N33/53 , G01N33/564 , G01N33/574 , A61K49/00 , A61K31/715 , G01N31/00 , G01N33/48
CPC分类号： G01N33/5308 , G01N33/564 , G01N33/57488 , G01N2333/4724
摘要： Compounds that are synthetically inexpensive to make relative to the naturally occurring selectin ligands and that retain selectin binding activity are described that have a three-dimensionally stable configuration for sialic acid and fucose, or analogs or derivatives of these groups, such that sialic acid and fucose are separated by a non-carbohydrate linker that permits binding between those groups and the selectins, such compounds being represented by the following general structural formula I(a): ##STR1## wherein m and n are independently an integer of from 1 to 5, Y and Z are independently a connecting moiety selected from the group consisting of --CH.sub.2 --, --O--, --S--, --NR' and --NR'R"-- (wherein R' and R" are independently H or an alkyl containing 1 to 4 carbon atoms); X is a connecting moiety which is selected from the group consisting of --O--, --S-- and --N--; and --R'" may be --R" or any moiety which does not interfere with the three-dimensional configuration of A or B so as to interfere with selectin binding and is preferably a moiety selected from the group consisting of --OR", --SR", --I, --N.sub.3, and --NR'R", and A is selected from the group consisting of .alpha. and .beta. forms of sialic acid, Kemp's acid, Quinic acid, Glyceric acid, Lactic acid and acetic acid, and esters thereof and B is selected from the group consisting of .alpha. and .beta. forms of L-Fucose and esters and substituted forms thereof wherein one or more of the --OH groups is independently --F, or --NR.sup.IV, R.sup.V wherein R.sup.IV and R.sup.V are independently an alkyl contain 1 to 5 carbons.
摘要翻译：描述了相对于天然存在的选择蛋白配体合成成本并且保留选择蛋白结合活性的化合物，其对于唾液酸和岩藻糖或这些基团的类似物或衍生物具有三维稳定的构型，使得唾液酸和岩藻糖由允许这些基团和选择素之间结合的非碳水化合物接头分开，这些化合物由以下通式结构式I（a）表示：其中m和n独立地为1至5的整数， Y和Z独立地是选自-CH 2 - ， - O - ， - S - ， - NR'和-NR'R“ - 的连接部分（其中R'和R”独立地是H或含有1至4个碳原子的烷基）; X是选自-O - ， - S-和-N-的连接部分; 和-R“可以是-R”或不干扰A或B的三维构型以干扰选择素结合的任何部分，并且优选是选自-OR'的部分， '，-SR“，-I，-N3和-NR'R”，A选自唾液酸，肯普酸，奎宁酸，甘油酸，乳酸和乙酸及其酯，B选自α-岩藻糖的α型和β型及其酯及其取代形式，其中一个或多个-OH基团独立地为-F，或-NRIV，RV，其中RIV 并且RV独立地为含有1至5个碳的烷基。

9. 发明授权

US5658880A Sialic acid/fucose based medicaments 失效
标题翻译：唾液酸/岩藻糖基药物
公开(公告)号：US5658880A
公开(公告)日：1997-08-19
申请号：US289715
申请日：1994-08-12
申请人： Falguni Dasgupta , John H. Musser , Daniel E. Levy , Peng Cho Tang
发明人： Falguni Dasgupta , John H. Musser , Daniel E. Levy , Peng Cho Tang
IPC分类号： G01N33/566 , A61K31/70 , A61K31/7028 , A61K49/00 , A61K51/00 , A61P29/00 , A61P31/04 , C07D309/10 , C07H3/06 , C07H11/00 , C07H15/04 , C07H15/18 , A61K31/715 , A61K38/14 , C07K2/00
CPC分类号： A61K31/7012 , C07D309/10 , C07H11/00 , C07H15/04 , C07H15/18 , C07H3/06
摘要： Compounds that exhibit selectin binding activity are described and have the following structural formula: ##STR1## where W is selected from a group including structures a-d below ##STR2## wherein p is an integer of from 0-2, q is an integer of from 0-3, and r is an integer of from 0-5;A is selected from the group consisting of .alpha. and .beta. forms of sialic acid, Kemp's acid, quinic acid, R and S forms of mandelic acid, R and S forms of glyceric acid, R and S forms of lactic acid, propionic and acetic acid, and esters and amides thereof, --SO.sub.3, sulfonate, --PO.sub.3, phosphonate, trifluoromethyl, diazine and triazine;B is selected from a group consisting of .alpha. and .beta. forms of fucose, arabinose and esters and substituted forms thereof wherein one or more of the OH groups is independently substituted with F, N.sub.3, NHAc, NHCOCF.sub.3. The remaining variable are described in the specification.
摘要翻译：描述具有选择素结合活性的化合物，并具有以下结构式：其中W选自包含以下结构的组（a）（b）（c）（d）其中p是0-2的整数，q是0-3的整数，r是0-5的整数; A选自唾液酸的α和β形式，肯普酸，奎尼酸，R和S形扁桃酸，R和S形式的甘油酸，R和S形式的乳酸，丙酸和乙酸，及其酯和酰胺，-SO 3，磺酸盐，-PO 3，膦酸盐，三氟甲基，二嗪和三嗪; B选自由岩藻糖，阿拉伯糖和酯及其取代形式的α和β形式组成的组，其中一个或多个OH基团独立地被F，N 3，NHAc，NHCOCF 3取代。剩余变量在说明书中描述。

10. 发明授权

US5138044A Synthesis of sialosides 失效
标题翻译：唾液酸苷的合成
公开(公告)号：US5138044A
公开(公告)日：1992-08-11
申请号：US566682
申请日：1990-08-13
申请人： Falguni Dasgupta
发明人： Falguni Dasgupta
IPC分类号： C07H15/10 , C07H15/14 , C07H15/18 , C07H23/00
CPC分类号： C07H15/10 , C07H15/14 , C07H15/18 , C07H23/00
摘要： Reaction schemes for carrying out a variety of chemical synthesis are disclosed. The reactions produce .alpha.-(X)-sialosides wherein X is O, S, N or another compatible electron donating atom or molecular moiety. The reaction schemes include a relatively small number of steps to provide a yield with a relatively small amount of undesired .beta.-configuration product. Compounds synthesized are encompassed by the following general structural formula I. ##STR1## wherein R, R' and R" are each independently H, CH.sub.3, acetyl, or a disaccharide which is preferably lactose.
摘要翻译：公开了用于进行各种化学合成的反应方案。反应产生α - （X）-sialosides，其中X是O，S，N或其他相容的电子供体原子或分子部分。反应方案包括相对少量的步骤以提供具有相对少量的不期望的β构型产物的产率。合成的化合物包括下列一般结构式I.其中R，R'和R“各自独立地为H，CH 3，乙酰基或二糖，其优选为乳糖。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式