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1. 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。

2. 发明授权

US06683103B2 Sulfonamides for treatment of endothelin-mediated disorders 失效
标题翻译：磺酰胺用于治疗内皮素介导的疾病
公开(公告)号：US06683103B2
公开(公告)日：2004-01-27
申请号：US10029561
申请日：2001-12-20
申请人： Chengde Wu , Natalie Blok , Timothy Kogan , Karin Keller
发明人： Chengde Wu , Natalie Blok , Timothy Kogan , Karin Keller
IPC分类号： A61K3142
CPC分类号： C07D413/14 , C07D261/16 , C07D409/12 , C07D413/12 , C07D417/14
摘要： Thienylsulfonamides and their pharmaceutically acceptable derivatives, pharmaceutical compositions, articles of manufacture, combinations, lyophilized powders and methods for the treatment of endothelin diseases using these formulations and sulfonamides are provided. 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：提供噻吩磺酰胺及其药学上可接受的衍生物，药物组合物，制品，组合，冻干粉末以及使用这些制剂和磺酰胺治疗内皮素疾病的方法。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。

3. 发明授权

US06458805B2 Formulation of sulfonamides for treatment of endothelin-mediated disorders 失效
标题翻译：用于治疗内皮素介导的疾病的磺酰胺的制剂
公开(公告)号：US06458805B2
公开(公告)日：2002-10-01
申请号：US09792237
申请日：2001-02-23
申请人： Natalie Blok , Chengde Wu , Patricia Woodard , Karin Keller , Timothy Kogan
发明人： Natalie Blok , Chengde Wu , Patricia Woodard , Karin Keller , Timothy Kogan
IPC分类号： A61K3147
CPC分类号： C07D413/14 , C07D261/16 , C07D409/12 , C07D413/12 , C07D417/14
摘要： Formulations of pharmaceutically-acceptable salts of thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides using the formulations are provided. In particular, formulations of sodium salts of N-(isoxazolyl)-thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)-pyrrolylsulfonamides and methods using these sulfonamide salts for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide salt are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamide salts or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.
摘要翻译：提供噻吩基，呋喃基和吡咯基磺酰胺的药学上可接受的盐的制剂以及使用制剂调节或改变肽内皮素家族的活性的方法。特别地，N-（异恶唑基） - 噻吩基磺酰胺，N-（异恶唑基）呋喃基磺酰胺和N-（异恶唑基） - 吡咯烷磺酰胺的钠盐的制剂和使用这些磺酰胺盐的方法，用于通过接触来抑制内皮素肽与内皮素受体的结合提供了具有磺酰胺盐的受体。还提供了通过施用有效量的一种或多种这些抑制或增加内皮素活性的磺酰胺盐或其前体来治疗内皮素介导的病症的方法。

4. 发明授权

US06432994B1 Sulfonamides for treatment of endothelin-mediated disorders 有权
标题翻译：磺酰胺用于治疗内皮素介导的疾病
公开(公告)号：US06432994B1
公开(公告)日：2002-08-13
申请号：US09403599
申请日：2000-03-27
申请人： Chengde Wu , Natalie Blok , Timothy Kogan , Karin Keller , Patricia Woodard
发明人： Chengde Wu , Natalie Blok , Timothy Kogan , Karin Keller , Patricia Woodard
IPC分类号： A61K3142
CPC分类号： C07D413/14 , C07D261/16 , C07D409/12 , C07D413/12 , C07D417/14
摘要： Thienyl-, furyl- and pyrrolyl-sulfonamides, pharmaceutically-acceptable salts of sulfonamides, formulations of salts and the sulfonamides, and methods for modulating or altering the activity of the endothelin family of peptides using the formulations and sulfonamides are provided. In particular, formulations of sodium salts of N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides are provided. 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：提供噻吩基，呋喃基和吡咯基磺酰胺，磺酰胺的药学上可接受的盐，盐和磺酰胺的制剂，以及使用制剂和磺酰胺调节或改变肽的内皮素家族的活性的方法。特别地，提供了N-（异恶唑基）噻吩基磺酰胺，N-（异恶唑基）呋喃基磺酰胺和N-（异恶唑基）吡咯烷基磺酰胺的钠盐的配方。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

US06248767B1 Formulation of sulfonamides for treatment of endothelin-mediated disorders 失效
标题翻译：用于治疗内皮素介导的疾病的磺酰胺的制剂
公开(公告)号：US06248767B1
公开(公告)日：2001-06-19
申请号：US08938444
申请日：1997-09-26
申请人： Natalie Blok , Chengde Wu , Patricia Woodard , Karin Keller , Timothy Kogan
发明人： Natalie Blok , Chengde Wu , Patricia Woodard , Karin Keller , Timothy Kogan
IPC分类号： A61K3142
CPC分类号： C07D413/14 , C07D261/16 , C07D409/12 , C07D413/12 , C07D417/14
摘要： Formulations of pharmaceutically-acceptable salts of thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides using the formulations are provided. In particular, formulations of sodium salts of N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides and methods using these sulfonamide salts for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide salt are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamide salts or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.
摘要翻译：提供噻吩基，呋喃基和吡咯基磺酰胺的药学上可接受的盐的制剂以及使用制剂调节或改变肽的内皮素家族的活性的方法。特别地，N-（异恶唑基）噻吩基磺酰胺，N-（异恶唑基）呋喃基磺酰胺和N-（异恶唑基）吡咯烷磺酰胺的钠盐的制剂和使用这些磺酰胺盐通过使受体接触来抑制内皮素肽与内皮素受体结合的方法与磺酰胺盐。还提供了通过施用有效量的一种或多种这些抑制或增加内皮素活性的磺酰胺盐或其前体来治疗内皮素介导的病症的方法。

6. 发明授权

US06686382B2 Sulfonamides and derivatives thereof that modulate the activity of endothelin 失效
标题翻译：调节内皮素活性的磺酰胺及其衍生物
公开(公告)号：US06686382B2
公开(公告)日：2004-02-03
申请号：US09751825
申请日：2000-12-29
申请人： Chengde Wu , Natalie Blok , George W. Holland
发明人： Chengde Wu , Natalie Blok , George W. Holland
IPC分类号： A61K3142
CPC分类号： C07D413/12 , C07D413/14
摘要： Thienyl-, furyl-, pyrrolyl- and phenylsulfonamides, formulations of pharmaceutically-acceptable derivatives thereof and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides, N-(isoxazolyl)pyrrolylsulfonamides and N-(isoxazolyl)phenylsulfonamides, formulations thereof and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or pharmaceutically acceptable derivatives thereof that inhibit the activity of endothelin are also provided.
摘要翻译：提供噻吩基，呋喃基，吡咯基和苯基磺酰胺，其药学上可接受的衍生物的制剂和调节或改变肽内皮素家族的活性的方法。特别地，N-（异恶唑基）噻吩基磺酰胺，N-（异恶唑基）呋喃基磺酰胺，N-（异恶唑基）吡咯烷基磺酰胺和N-（异恶唑基）苯基磺酰胺及其制剂及使用这些磺酰胺抑制内皮素肽与内皮素受体结合的方法通过使受体与磺酰胺接触。还提供了通过施用有效量的一种或多种这些抑制内皮素活性的磺酰胺或其药学上可接受的衍生物来治疗内皮素介导的病症的方法。

7. 发明授权

US06420567B1 N-heteroaryl aryl-substituted thienyl-furyl-and pyrrolyl-sulfonamides and derviatives thereof that modulate the activity of endothelin 失效
标题翻译： N-杂芳基芳基取代的噻吩基 - 呋喃基和吡咯基磺酰胺及其衍生物，其调节内皮素的活性
公开(公告)号：US06420567B1
公开(公告)日：2002-07-16
申请号：US08938325
申请日：1997-09-26
申请人： Chengde Wu , Bore Gowda Raju , Timothy Kogan , Natalie Blok
发明人： Chengde Wu , Bore Gowda Raju , Timothy Kogan , Natalie Blok
IPC分类号： C07D26104
CPC分类号： C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： Thienyl-, furyl- and pyrrolyl-sulfonamides, formulations of pharmaceutically-acceptable salts thereof and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides, formulations thereof and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit the activity of endothelin are also provided.
摘要翻译：提供噻吩基，呋喃基和吡咯基磺酰胺，其药学上可接受的盐的制剂和调节或改变肽内皮素家族的活性的方法。特别地，N-（异恶唑基）噻吩基磺酰胺，N-（异恶唑基）呋喃基磺酰胺和N-（异恶唑基）吡咯烷磺酰胺，其制剂和使用这些磺酰胺用于通过使受体与磺酰胺接触来抑制内皮素肽与内皮素受体结合的方法被提供。还提供了通过施用有效量的一种或多种这些抑制内皮素活性的磺酰胺或其前体来治疗内皮素介导的病症的方法。

8. 发明授权

US06632829B2 Sulfonamides and derivatives thereof that modulate the activity of endothelin 失效
标题翻译：调节内皮素活性的磺酰胺及其衍生物
公开(公告)号：US06632829B2
公开(公告)日：2003-10-14
申请号：US10011610
申请日：2001-11-05
申请人： Chengde Wu , Bore Gowda Raju , Timothy Kogan , Natalie Blok , Patricia Woodard
发明人： Chengde Wu , Bore Gowda Raju , Timothy Kogan , Natalie Blok , Patricia Woodard
IPC分类号： A61K3142
CPC分类号： C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： Thienyl-, furyl- and pyrrolyl-sulfonamides, formulations of pharmaceutically-acceptable salts thereof and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides, formulations thereof and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit the activity of endothelin are also provided.
摘要翻译：提供噻吩基，呋喃基和吡咯基磺酰胺，其药学上可接受的盐的制剂和调节或改变肽内皮素家族的活性的方法。特别地，N-（异恶唑基）噻吩基磺酰胺，N-（异恶唑基）呋喃基磺酰胺和N-（异恶唑基）吡咯烷磺酰胺，其制剂和使用这些磺酰胺用于通过使受体与磺酰胺接触来抑制内皮素肽与内皮素受体结合的方法被提供。还提供了通过施用有效量的一种或多种这些抑制内皮素活性的磺酰胺或其前体来治疗内皮素介导的病症的方法。

9. 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。

10. 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。

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