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公开(公告)号：US06299897B1
公开(公告)日：2001-10-09
申请号：US09440880
申请日：1999-11-15
IPC分类号： A61K970
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 106 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.
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公开(公告)号：US5851988A
公开(公告)日：1998-12-22
申请号：US784854
申请日：1997-01-15
IPC分类号： C07C309/34 , C12Q1/34 , C12Q1/48 , G01N33/58 , A61K31/05 , A61K31/10 , A61K31/17 , A61K31/655
CPC分类号： G01N33/582 , C07C309/34 , C12Q1/34 , C12Q1/48 , G01N2333/62 , G01N2333/72 , G01N2333/9121 , Y10S514/866
摘要： Modulation of the activity of the insulin receptor, enhancement of glucose uptake by cells, and other effects significant in the control and management of diabetes are accomplished using compounds of the formula ##STR1## wherein each A is independently a proton-accepting substituent; each R is independently a noninterfering substituent; n is 0, 1, or 2; and each linker is independently an isostere of --NHCONH-- or of --N.dbd.N-- or of --NHCO--. Compounds in the genus of Formula (1) can also be used for structure activity studies to identify features responsible for the relevant activities.
摘要翻译： 胰岛素受体的活性的调节，细胞的葡萄糖摄取的增强以及在糖尿病的控制和治疗中显着的其它作用使用下式的化合物来实现：式（1）+ TR＆lt; IMAGE＆gt;其中每个A是 独立地是质子接受取代基; 每个R独立地是非干扰取代基; n为0,1或2; 并且每个连接体独立地是-NHCONH-或-N = N-或-NHCO-的等离子体。 式（1）属中的化合物也可用于结构活性研究，以鉴定负责相关活性的特征。
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公开(公告)号：US07071231B2
公开(公告)日：2006-07-04
申请号：US10237583
申请日：2002-09-06
申请人： Wayne R. Spevak , Songyuan Shi , Prasad V. V. S. V. Manchem , Michael R. Kozlowski , Steven R. Schow , Robert T. Lum
发明人： Wayne R. Spevak , Songyuan Shi , Prasad V. V. S. V. Manchem , Michael R. Kozlowski , Steven R. Schow , Robert T. Lum
IPC分类号： A61K31/18 , C12N5/06 , C07C309/01
CPC分类号： C07D257/04 , C07C309/51 , C07C311/47 , C07C335/16 , C07C335/18 , C07C335/32 , C07D211/96 , C07D213/76 , C07D233/36 , C07D239/42 , C07D241/20 , C07F9/4021
摘要： Compounds of formula I are useful for treating conditions associated with hyperglycemia, especially Type II diabetes. These compounds are useful in stimulating the kinase activity of the insulin receptor, activating the insulin receptor, and stimulating the uptake of glucose. Pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.
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公开(公告)号：USRE38915E1
公开(公告)日：2005-12-06
申请号：US09748665
申请日：2000-12-21
IPC分类号： C07C309/34 , C12Q1/34 , C12Q1/48 , G01N33/58 , A61K31/05 , A61K31/10 , A61K31/17 , A61K31/655
CPC分类号： G01N33/582 , C07C309/34 , C12Q1/34 , C12Q1/48 , G01N2333/62 , G01N2333/72 , G01N2333/9121 , Y10S514/866
摘要： Modulation of the activity of the insulin receptor, enhancement of glucose uptake by cells, and other effects significant in the control and management of diabetes are accomplished using compounds of the formula wherein each A is independently a proton-accepting substituent; each R is independently a noninterfering substituent; n is 0, 1, or 2; and each linker is independently an isostere of —NHCONH— or of —N═N— or of —NHCO—. Compounds in the genus of Formula (1) can also be used for structure activity studies to identify features responsible for the relevant activities.
摘要翻译： 胰岛素受体的活性调节，细胞葡萄糖摄取的增强以及糖尿病的控制和治疗中显着的其它作用使用下式的化合物来实现：其中每个A独立地是质子受体取代基; 每个R独立地是非干扰取代基; n为0,1或2; 并且每个接头独立地是-NHCONH-或-N-N-或-NHCO-的等排物。 式（1）属中的化合物也可用于结构活性研究，以鉴定负责相关活性的特征。
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公开(公告)号：US5985852A
公开(公告)日：1999-11-16
申请号：US250999
申请日：1999-02-16
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。
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公开(公告)号：US06479548B2
公开(公告)日：2002-11-12
申请号：US09872763
申请日：2001-05-31
申请人： John Patterson , Sophia Park , Robert T. Lum , Wayne R. Spevak
发明人： John Patterson , Sophia Park , Robert T. Lum , Wayne R. Spevak
IPC分类号： A61K31195
CPC分类号： C07C233/81 , C07C233/88 , C07C235/56 , C07C235/64 , C07C235/84 , C07C237/40 , C07C237/42 , C07C309/51 , C07C309/61 , C07D317/60
摘要： Compound of formula I activate the insulin receptor kinase. Pharmaceutical compositions comprising the compounds, and methods of treatment of hyperglycemia and other diseases involving imbalance of glucose levels, especially for the treatment of type II diabetes, by administering these compounds to mammalian hosts, and processes for their preparation, are also described.
摘要翻译： 配方化合物使胰岛素受体激酶活化。 还描述了包含该化合物的药物组合物，以及通过将哺乳动物宿主施用这些化合物及其制备方法来治疗高血糖症和涉及葡萄糖水平不平衡的其它疾病，特别是用于治疗II型糖尿病的方法。
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7.发明授权公开(公告)号：US06653321B1
公开(公告)日：2003-11-25
申请号：US09628206
申请日：2000-07-28
申请人： Wayne R. Spevak , Songyuan Shi , Prasad V. V. S. V. Manchem , Michael R. Kozlowski , Steven R. Schow , Robert T. Lum , Louise Robinson , Jeong Weon Park
发明人： Wayne R. Spevak , Songyuan Shi , Prasad V. V. S. V. Manchem , Michael R. Kozlowski , Steven R. Schow , Robert T. Lum , Louise Robinson , Jeong Weon Park
IPC分类号： A61K3150
CPC分类号： C07D241/44 , C07C237/42 , C07C309/51 , C07C309/59 , C07C311/13 , C07C311/21 , C07C311/29 , C07D213/81 , C07D213/82 , C07D215/48 , C07D307/68 , C07D307/85
摘要： Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptable salts, are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.
摘要翻译： 用新型萘磺酸和相关化合物治疗与高血糖相关的病症，特别是II型糖尿病的方法。 这些化合物作为单立体异构体或立体异构体的混合物或其药学上可接受的盐可用于刺激胰岛素受体的激酶活性，增强胰岛素对胰岛素受体的活化以及刺激葡萄糖摄入细胞的方法。 还公开了包含抗糖尿病化合物的各种抗糖尿病化合物和药物组合物。
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公开(公告)号：USRE39866E1
公开(公告)日：2007-10-02
申请号：US11167026
申请日：2005-06-23
IPC分类号： A61K31/655 , A61K31/17 , A61K31/10 , A61K31/015 , C07C245/00
CPC分类号： G01N33/582 , C07C309/34 , C12Q1/34 , C12Q1/48 , G01N2333/62 , G01N2333/72 , G01N2333/9121 , Y10S514/866
摘要： Modulation of the activity of the insulin receptor, enhancement of glucose uptake by cells, and other effects significant in the control and management of diabetes are accomplished using compounds of the formula wherein each A is independently a proton-accepting substituent; each R is independently a noninterfering substituent; n is 0, 1, or 2; and each linker is independently an isostere of —NHCONH— or of —N═N— or of —NHCO—. Compounds in the genus of Formula (1) can also be used for structure activity studies to identify features responsible for the relevant activities.
摘要翻译： 胰岛素受体的活性调节，细胞葡萄糖摄取的增强以及糖尿病的控制和治疗中显着的其它作用使用下式的化合物来实现：其中每个A独立地是质子受体取代基; 每个R独立地是非干扰取代基; n为0,1或2; 并且每个接头独立地是-NHCONH-或-N-N-或-NHCO-的等排物。 式（1）属中的化合物也可用于结构活性研究，以鉴定负责相关活性的特征。
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公开(公告)号：US06458998B1
公开(公告)日：2002-10-01
申请号：US09579279
申请日：2000-05-25
申请人： Wayne R. Spevak , Songyuan Shi , Prasad V. V. S. V. Manchem , Michael R. Kozlowski , Steven R. Schow , Robert T. Lum
发明人： Wayne R. Spevak , Songyuan Shi , Prasad V. V. S. V. Manchem , Michael R. Kozlowski , Steven R. Schow , Robert T. Lum
IPC分类号： C07C27300
CPC分类号： C07D257/04 , C07C309/51 , C07C311/47 , C07C335/16 , C07C335/18 , C07C335/32 , C07D211/96 , C07D213/76 , C07D233/36 , C07D239/42 , C07D241/20 , C07F9/4021
摘要： Compounds of formula I are useful for treating conditions associated with hyperglycemia, especially Type II diabetes. These compounds are useful in stimulating the kinase activity of the insulin receptor, activating the insulin receptor, and stimulating the uptake of glucose. Pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.
摘要翻译： 式I化合物可用于治疗与高血糖相关的病症，特别是II型糖尿病。 这些化合物可用于刺激胰岛素受体的激酶活性，激活胰岛素受体，并刺激葡萄糖摄取。 还公开了包含抗糖尿病化合物的药物组合物。
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公开(公告)号：US5962422A
公开(公告)日：1999-10-05
申请号：US807428
申请日：1997-02-28
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。
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