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1. 发明授权

US06262084B1 Compounds that inhibit the binding of integrins to their receptors 有权
标题翻译：抑制整联蛋白与其受体结合的化合物
公开(公告)号：US06262084B1
公开(公告)日：2001-07-17
申请号：US09417886
申请日：1999-10-14
申请人： Ronald J. Biediger , Vanessa O. Grabbe , George W. Holland , Jamal Kassir , Karin M. Keller , Timothy P. Kogan , Shuqun Lin , Robert V. Market , Bore G. Raju , Ian L. Scott , Chengde Wu
发明人： Ronald J. Biediger , Vanessa O. Grabbe , George W. Holland , Jamal Kassir , Karin M. Keller , Timothy P. Kogan , Shuqun Lin , Robert V. Market , Bore G. Raju , Ian L. Scott , Chengde Wu
IPC分类号： A61K31192
CPC分类号： C07D417/14 , C07D317/60 , C07D333/20 , C07D333/24 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14
摘要： A method for the inhibition of the binding of &agr;4&bgr;1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions thereof; and the use of the compounds either as above, or in formulations for the control or prevention of diseases states in which &agr;4&bgr;1 is involved.
摘要翻译：抑制α4β1整联蛋白与其受体结合的方法，例如VCAM-1（血管细胞粘附分子-1）和纤连蛋白; 抑制这种结合的化合物; 其药物活性组合物; 以及如上所述的化合物或用于控制或预防涉及α4β1的疾病状态的制剂中的用途。

2. 发明授权

US06194448B1 N, N-disubstituted amides that inhibit the binding of integrins to their receptors 有权
标题翻译：抑制整联蛋白与其受体结合的N，N-二取代酰胺
公开(公告)号：US06194448B1
公开(公告)日：2001-02-27
申请号：US09417857
申请日：1999-10-14
申请人： Ronald J. Biediger , Vanessa O. Grabbe , George W. Holland , Jamal M. Kassir , Timothy P. Kogan , Shuqun Lin , Robert V. Market , Bore G. Raju , Ian L. Scott , Chengde Wu
发明人： Ronald J. Biediger , Vanessa O. Grabbe , George W. Holland , Jamal M. Kassir , Timothy P. Kogan , Shuqun Lin , Robert V. Market , Bore G. Raju , Ian L. Scott , Chengde Wu
IPC分类号： A61K3138
CPC分类号： C07D417/14 , C07D317/60 , C07D333/20 , C07D333/24 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14
摘要： A method for the inhibition of the binding of &agr;4&bgr;1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of diseases states in which &agr;4&bgr;1 is involved.
摘要翻译：抑制α4β1整联蛋白与其受体结合的方法，例如VCAM-1（血管细胞粘附分子-1）和纤连蛋白; 抑制这种结合的化合物; 包含这些化合物的药物活性组合物; 以及使用上述化合物或在制剂中用于控制或预防涉及α4β1的疾病状态。

3. 发明授权

US5919768A Di- and trivalent small molecule selectin inhibitors 失效
标题翻译：二价和三价小分子选择蛋白抑制剂
公开(公告)号：US5919768A
公开(公告)日：1999-07-06
申请号：US981580
申请日：1998-02-11
申请人： Timothy P. Kogan , Brian Dupre , Ian L. Scott , Huong Bui , Kathy L. Wheeler , Karin M. Keller , Jamal M. Kassir
发明人： Timothy P. Kogan , Brian Dupre , Ian L. Scott , Huong Bui , Kathy L. Wheeler , Karin M. Keller , Jamal M. Kassir
IPC分类号： C07H15/203 , A61K31/35 , A61K31/70 , C07D309/10 , C07H15/00
CPC分类号： C07H15/203
摘要： The present invention provides compounds having structure (II), and the pharmaceutically acceptable salts, esters, amides and prodrugs thereof.
摘要翻译： PCT No.PCT / US96 / 11032 Sec。 371日期1998年2月11日 102（e）1998年2月11日PCT PCT 1996年6月26日PCT公布。第WO97 / 01335号公报日本1997年1月16日本发明提供具有结构（II）的化合物及其药学上可接受的盐，酯，酰胺和前药。

4. 发明授权

US5783705A Process of preparing alkali metal salys of hydrophobic sulfonamides 失效
标题翻译：制备疏水性磺胺类碱金属盐的工艺
公开(公告)号：US5783705A
公开(公告)日：1998-07-21
申请号：US847797
申请日：1997-04-28
申请人： Natalie Blok , Chengde Wu , Karin Keller , Timothy P. Kogan
发明人： Natalie Blok , Chengde Wu , Karin Keller , Timothy P. Kogan
IPC分类号： A61P9/00 , A61P11/00 , C07D261/16 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/14 , C07D261/06 , C07D261/04 , C07D261/14
CPC分类号： C07D413/14 , C07D261/16 , C07D409/12 , C07D413/12 , C07D417/14
摘要： A process of preparing an alkali metal salt of a hydrophobic sulfonamide is provided. The process includes the step of dissolving a free sulfonamide in an organic solvent in the presence of a saturated alkali metal salt solution and recovering the formed sulfonamide salt from the organic phase.
摘要翻译：提供了制备疏水性磺酰胺的碱金属盐的方法。该方法包括在饱和碱金属盐溶液存在下将游离磺酰胺溶解在有机溶剂中并从有机相中回收所形成的磺酰胺盐的步骤。

5. 发明授权

US5444050A Binding of E-selectin or P-selectin to sialyl Lewis.sup.x or sialyl-Lewis.sup.a 失效
公开(公告)号：US5444050A
公开(公告)日：1995-08-22
申请号：US235293
申请日：1994-04-29
申请人： Timothy P. Kogan , Brian Dupre , Ian L. Scott , Karin Keller , Huong Dao , Pamela J. Beck
发明人： Timothy P. Kogan , Brian Dupre , Ian L. Scott , Karin Keller , Huong Dao , Pamela J. Beck
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61P1/00 , A61P9/00 , A61P11/08 , A61P17/00 , A61P29/00 , A61P35/00 , A61P37/06 , C07H15/18 , C07H15/203 , C07H15/20
CPC分类号： C07H15/18 , C07H15/203
摘要： This invention relates to compounds that inhibit the binding of E-selectin and/or P-selectin to sialyl-Lewis.sup.x or sialyl-Lewis.sup.a presented on a cell surface having the general structure ##STR1## wherein X is selected from the group consisting of --(CH.sub.2).sub.n CO.sub.2 H, --O(CH.sub.2).sub.m CO.sub.2 H, --(CH.sub.2).sub.n O(CH.sub.2).sub.m CO.sub.2 H, --CONH(CH.sub.2).sub.m CO.sub.2 H, --CH(OZ)(CO.sub.2 H), --CH(Z)(CO.sub.2 H), --(CH.sub.2).sub.n SO.sub.3 H, --(CH.sub.2).sub.n PO.sub.3 D.sub.1 D.sub.2, --NH(CH.sub.2).sub.m CO.sub.2 H, --CONH(CHR.sub.6)CO.sub.2 H, (1-H-tetrazolyl-5-alkyl-), and --OH;R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, alkyl, halogen, --OZ, --NO.sub.2, --NH.sub.2 and --NHZ;R.sub.3 is selected from the group consisting of hydrogen, halogen, alkyl, --OZ and --NHZ;R.sub.4 is selected from the group consisting of hydrogen, halogen, alkyl, hydroxyl, hydroxyl-O-sulfate and --OZ;R.sub.5 is selected from the group consisting of hydroxyl, --CN, --N.sub.3, --NH.sub.2, --NHNH.sub.2, --NE.sub.1 E.sub.2, --NHE.sub.1, --NHCO(CH.sub.2).sub.n CO.sub.2 H, --S(CH.sub.2).sub.m CO.sub.2 H and --NHCHNHNH.sub.2 ;R.sub.6 is selected from the group consisting of hydrogen, alkyl, aralkyl, hydroxyalkyl, aminoalkyl, alkyl carboxylic acid and alkyl carboxamide;wherein n is 0 to 6, m is 1 to 6, p is 0 to 6, b is 0 to 2, Z is alkyl, aryl or aralkyl, D.sub.1 and D.sub.2 are independantly hydrogen or alkyl, E.sub.1 is alkyl or --(CH.sub.2).sub.8 CO.sub.2 H, and E.sub.2 is alkyl, and the pharmaceutically acceptable salts, esters, amides, and prodrugs thereof. This invention also relates to methods of inhibiting the binding of E-selectin and/or P-selectin to sialyl-Lewis.sup.x or sialyl-Lewis.sup.a presented on a cell surface using said compounds and to pharmaceutically active compositions comprising compounds that inhibit the binding of E-selectin to sialyl-Lewis.sup.x and to methods of treatment of septic shock, ARDS, Crohn's disease, chronic inflammatory diseases, such as psoriasis and rheumatoid arthritis, and reperfusion injuries that occur following heart attacks, strokes and organ transplants.

6. 发明授权

US5712387A High yield stereospecific mannosylation 失效
标题翻译：高产量立体特异性甘露糖基化
公开(公告)号：US5712387A
公开(公告)日：1998-01-27
申请号：US650653
申请日：1996-05-20
申请人： Ian L. Scott , Timothy P. Kogan , Harold Meckler
发明人： Ian L. Scott , Timothy P. Kogan , Harold Meckler
IPC分类号： C07H13/02 , C07H13/04 , C07H15/18 , C07H113/02 , C07H1/00
CPC分类号： C07H13/04
摘要： A process of preparing mannosylated alcohols or phenols in high chemical yield and purity using tetra-O-pivaloylmannosylfluoride and a Lewis acid catalyst.
摘要翻译：使用四-E，非O + EE-新戊酰基甘露糖基氟化物和路易斯酸催化剂制备具有高化学产率和纯度的甘露糖化醇或酚的方法。

7. 发明授权

US06582928B1 Carbohydrate-directed cross-linking reagents 失效
标题翻译：碳水化合物导向的交联试剂
公开(公告)号：US06582928B1
公开(公告)日：2003-06-24
申请号：US09517876
申请日：2000-03-02
申请人： Avi J. Ashkenazi , Steven M. Chamow , Timothy P. Kogan
发明人： Avi J. Ashkenazi , Steven M. Chamow , Timothy P. Kogan
IPC分类号： G01N33567
CPC分类号： C07D207/452 , C07K1/1072 , C07K14/805 , Y10S435/96 , Y10S435/974 , Y10S436/829 , Y10S530/812
摘要： The invention provides heterobifunctional cross-linking reagents and methods of using the cross-linking reagents. The cross-linking reagents of the invention combine a nucleophilic hydrazide residue with an electrophilic maleimide residue allowing coupling of aldehydes to free thiols. In the methods of the invention, human immunodeficiency virus (HIV) infected cells can be detected using conjugates that include CD4 molecules conjugated to detectable markers via the disclosed cross-linking reagents.
摘要翻译：本发明提供异双功能交联试剂和使用交联试剂的方法。本发明的交联试剂将亲核酰肼残基与亲电子马来酰亚胺残基相结合，允许醛与游离硫醇偶合。在本发明的方法中，可以使用包含通过公开的交联试剂缀合到可检测标记的CD4分子的缀合物来检测人免疫缺陷病毒（HIV）感染的细胞。

8. 发明授权

US06124435A Carbohydrate-directed cross-linking reagents 有权
标题翻译：碳水化合物导向的交联试剂
公开(公告)号：US06124435A
公开(公告)日：2000-09-26
申请号：US218408
申请日：1998-12-22
申请人： Avi J. Ashkenazi , Steven M. Chamow , Timothy P. Kogan
发明人： Avi J. Ashkenazi , Steven M. Chamow , Timothy P. Kogan
IPC分类号： C07D207/44 , C07D207/452 , C07K1/107 , C07K14/805 , C07K15/14
CPC分类号： C07D207/452 , C07K1/1072 , C07K14/805 , Y10S435/96 , Y10S435/974 , Y10S436/829 , Y10S530/812
摘要： The invention provides heterobifunctional cross-linking reagents and methods of using the cross-linking reagents. The cross-linking reagents of the invention combine a nucleophilic hydrazide residue with an electrophilic maleimide residue, allowing coupling of aldehydes to free thiols. In the methods of the invention, human immunodeficiency virus (HIV) infected cells can be detected using conjugates that include CD4 molecules conjugated to detectable markers via the disclosed cross-linking reagents.
摘要翻译：本发明提供异双功能交联试剂和使用交联试剂的方法。本发明的交联试剂将亲核酰肼残基与亲电马来酰亚胺残基相结合，使醛与游离硫醇偶联。在本发明的方法中，可以使用包含通过公开的交联试剂缀合到可检测标记的CD4分子的缀合物来检测人免疫缺陷病毒（HIV）感染的细胞。

9. 发明授权

US06713604B1 Process to inhibit binding of the integrin &agr;4&bgr;1 , to VCAM-1 fibronectin and cyclic peptides thereof 失效
标题翻译：抑制整合素α4β1与VCAM-1纤连蛋白及其环肽的结合的方法
公开(公告)号：US06713604B1
公开(公告)日：2004-03-30
申请号：US08646558
申请日：1996-05-08
申请人： Timothy P. Kogan , Kaijun Ren , Peter Vanderslice , Pamela J. Beck
发明人： Timothy P. Kogan , Kaijun Ren , Peter Vanderslice , Pamela J. Beck
IPC分类号： C07K1600
CPC分类号： C07K14/78 , A61K38/00
摘要： The present invention is directed to an isolated and purified cyclic peptide of from 5 to about 13 residues modeled after a portion of the CS1 peptide. A peptide of this invention preferably has the amino acid residue sequence of SEQ ID NO:2-14 or 16-42. The present invention is further directed to a process of selectively inhibiting the binding of &agr;4&bgr;1 integrin to a protein such as VCAM-1, fibronectin or invasin. In accordance with that process, a cell that expresses &agr;4&bgr;1 integrin is exposed to that protein in the presence of an effective inhibiting amount of such a peptide. The present invention is still further directed to a pharmaceutical composition containing a physiologically acceptable carrier and a cyclic peptide of the invention.
摘要翻译：本发明涉及在一部分CS1肽之后建模的分离和纯化的5至约13个残基的环肽。本发明的肽优选具有SEQ ID NO：2-14或16-42的氨基酸残基序列。本发明进一步涉及选择性抑制α4β1整联蛋白与蛋白质如VCAM-1，纤连蛋白或侵袭素结合的方法。根据该方法，在存在有效抑制量的这种肽的情况下，将表达α4β1整联蛋白的细胞暴露于该蛋白质。本发明还涉及含有本发明的生理学上可接受的载体和环肽的药物组合物。

10. 发明授权

US5929211A Carbohydrate-directed cross-linking reagents 失效
公开(公告)号：US5929211A
公开(公告)日：1999-07-27
申请号：US923590
申请日：1997-09-04
申请人： Avi J. Ashkenazi , Steven M. Chamow , Timothy P. Kogan
发明人： Avi J. Ashkenazi , Steven M. Chamow , Timothy P. Kogan
IPC分类号： C07D207/44 , C07D207/452 , C07K1/107 , C07K14/805 , C07K15/14
CPC分类号： C07D207/452 , C07K1/1072 , C07K14/805 , Y10S435/96 , Y10S435/974 , Y10S436/829 , Y10S530/812
摘要： The invention provides heterobifunctional cross-linking reagents and methods of using the cross-linking reagents. The cross-linking reagents of the invention combine a nucleophilic hydrazide residue with an electrophilic maleimide residue, allowing coupling of aldehydes to free thiols. In the methods of the invention, human immunodeficiency virus (HIV) infected cells can be detected using conjugates that include CD4 molecules conjugated to detectable markers via the disclosed cross-linking reagents.

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