公开(公告)号：US5514691A

公开(公告)日：1996-05-07

申请号：US142552

申请日：1993-10-21

申请人： Ming F. Chan ,  Bore G. Raju ,  Rosario S. Castillo ,  Adam Kois ,  Chengde Wu ,  Yalamoori Venkatachalapathi ,  Erik J. Verner ,  Vitukudi N. Balaji

发明人： Ming F. Chan ,  Bore G. Raju ,  Rosario S. Castillo ,  Adam Kois ,  Chengde Wu ,  Yalamoori Venkatachalapathi ,  Erik J. Verner ,  Vitukudi N. Balaji

IPC分类号： C07D261/14 ,  C07D261/16 ,  C07D261/20 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  A61K31/435 ,  C07D215/02 ,  C07D261/06

CPC分类号： C07D413/12 ,  C07D261/14 ,  C07D261/16 ,  C07D261/20 ,  C07D413/14 ,  C07D417/12

摘要： N-(4-halo-isoxazolyl)sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(4-halo-3-isoxazolyl)sulfonamides and N-(4-halo-5-isoxazolyl)benzenesulfonamides and methods for inhibiting the binding of an endothelin peptide to an endothelin receptor or increasing the activity of endothelin peptides by contacting the receptor with a 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 or increase the activity of endothelin are also provided.

摘要翻译： 提供N-（4-卤代 - 异恶唑基）磺酰胺和调节或改变肽内皮素家族的活性的方法。 特别地，N-（4-卤代-3-异恶唑基）磺酰胺和N-（4-卤代-5-异恶唑基）苯磺酰胺和用于抑制内皮素肽与内皮素受体结合或增加内皮素肽活性的方法 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或增加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。

公开(公告)号：US06372739B1

公开(公告)日：2002-04-16

申请号：US09897048

申请日：2001-07-02

申请人： Bernd M. Stein ,  David Wesley Anderson ,  Leah M. Gayo-Fung ,  Mary Doubleday ,  Graziella I. Shevlin ,  Adam Kois ,  Sak Khammungkhune ,  Ravi Kumar Jalluri ,  Shripad S. Bhagwat ,  Jeffrey A. McKie

发明人： Bernd M. Stein ,  David Wesley Anderson ,  Leah M. Gayo-Fung ,  Mary Doubleday ,  Graziella I. Shevlin ,  Adam Kois ,  Sak Khammungkhune ,  Ravi Kumar Jalluri ,  Shripad S. Bhagwat ,  Jeffrey A. McKie

IPC分类号： A61K315377

CPC分类号： C07D311/16 ,  C07D311/18 ,  C07D405/12

摘要： Compounds that modulate gene expression through the estrogen receptor (ER) are disclosed having the following structure, as well as pharmaceutical compositions containing the same: wherein R1, R2, R3, n and p are as defined here. Methods are also disclosed for modulating ER in cells and/or tissues expressing the same, such as bone, breast, prostate, uterus, CNS or the cardiovascular system. Methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, and adverse reproductive effects associated with exposure to environmental chemicals or natural hormonal imbalances.

摘要翻译： 公开了通过雌激素受体（ER）调节基因表达的化合物以及含有以下结构的药物组合物：其中R1，R2，R3，n和p如本文所定义。 还公开了用于在表达其的细胞和/或组织中调节ER的方法，例如骨，乳腺，前列腺，子宫，CNS或心血管系统。 还公开了治疗雌激素相关病症的方法，包括诸如乳腺癌，骨质疏松症，子宫内膜异位症，心血管疾病，高胆固醇血症，前列腺肥大，前列腺癌，肥胖症，潮热，皮肤效应，情绪波动，记忆丧失和不良 与暴露于环境化学品或天然荷尔蒙失衡相关的生殖影响。

公开(公告)号：US06331637B1

公开(公告)日：2001-12-18

申请号：US09274280

申请日：1999-03-22

申请人： Ming Fai Chan ,  Chengde Wu ,  Bore Gowda Raju ,  Timothy Kogan ,  Adam Kois ,  Erik Joel Verner ,  Rosario Silvestre Castillo ,  Venkatachalapathi Yalamoori ,  Vitukudi Narayanaiyengar Balaji

发明人： Ming Fai Chan ,  Chengde Wu ,  Bore Gowda Raju ,  Timothy Kogan ,  Adam Kois ,  Erik Joel Verner ,  Rosario Silvestre Castillo ,  Venkatachalapathi Yalamoori ,  Vitukudi Narayanaiyengar Balaji

IPC分类号： C07D26110

CPC分类号： C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： N-alkyl, N-alkenyl, N-alkynyl, N-aryl and N-fused bicyclo or tricyclo thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, (phenyl) and (phenoxy)thienylsulfonamides, (phenyl) and (phenoxy)furylsulfonamides, and (phenyl) and (phenoxy)pyrrolylsulfonamides and methods of 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 or increase the activity of endothelin are also provided.

摘要翻译： 提供N-烷基，N-烯基，N-炔基，N-芳基和N-稠合双环或三环噻吩基，呋喃基和吡咯基磺酰胺以及调节或改变肽内皮素家族活性的方法。 特别地，（苯基）和（苯氧基）噻吩基磺酰胺，（苯基）和（苯氧基）呋喃基磺酰胺和（苯基）和（苯氧基）吡咯烷磺酰胺和使用这些磺酰胺抑制内皮素肽与内皮素受体结合的方法 提供了具有磺酰胺的受体。 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或其前体来治疗内皮素介导的病症的方法。

公开(公告)号：US06265428B1

公开(公告)日：2001-07-24

申请号：US09327661

申请日：1999-06-08

申请人： Ming Fai Chan ,  Vitukudi Narayanaiyengar Balaji ,  Rosario Silvestre Castillo ,  Adam Kois ,  Bore Gowda Raju ,  Chengde Wu

发明人： Ming Fai Chan ,  Vitukudi Narayanaiyengar Balaji ,  Rosario Silvestre Castillo ,  Adam Kois ,  Bore Gowda Raju ,  Chengde Wu

IPC分类号： A61K314164

CPC分类号： A61K31/506 ,  A61K31/192 ,  A61K31/36 ,  A61K31/505 ,  C07D239/60 ,  C07D317/64 ,  C07D405/14 ,  Y10S206/828

摘要： Methods, compositions, and compounds for modulating the activity of an endothelin peptide are provided. The methods use compositions that contain compounds of formula (1): where X and Y are selected from groups that include O, S, and NH; and Ar1, Ar2 and Ar3 are independently selected from substituted or unsubstituted groups that include 5 to 6 membered aryl groups and heteroaryl groups that contain one or two heteroatom(s). The methods are effected by contacting endothelin receptors with one or more of the compounds or with compositions containing one or more of the compounds prior to, simultaneously with, or subsequent to contacting the receptors with an endothelin peptide.

摘要翻译： 提供了调节内皮素肽活性的方法，组合物和化合物。 该方法使用含有式（1）化合物的组合物：其中X和Y选自包括O，S和NH的基团; 并且Ar 1，Ar 2和Ar 3独立地选自包含5至6元芳基的取代或未取代的基团和含有一个或两个杂原子的杂芳基。 所述方法通过使内皮素受体与一种或多种化合物或含有一种或多种化合物的组合物在使受体与内皮素肽接触之前，同时或之后接触来实现。

公开(公告)号：US5594021A

公开(公告)日：1997-01-14

申请号：US477223

申请日：1995-06-06

申请人： Ming F. Chan ,  Bore G. Raju ,  Adam Kois ,  Erik J. Verner ,  Chengde Wu ,  Rosario S. Castillo ,  Venkatachalapathi Yalamoori ,  Vitukudi N. Balaji

发明人： Ming F. Chan ,  Bore G. Raju ,  Adam Kois ,  Erik J. Verner ,  Chengde Wu ,  Rosario S. Castillo ,  Venkatachalapathi Yalamoori ,  Vitukudi N. Balaji

IPC分类号： C07D261/14 ,  C07D261/16 ,  C07D261/20 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  A61K31/42 ,  C07D261/10

CPC分类号： C07D413/12 ,  C07D261/14 ,  C07D261/16 ,  C07D261/20 ,  C07D413/14 ,  C07D417/12

摘要： Thienyl-, furyl- and pyrrolyl-sulfonamides 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 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 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以及调节或改变肽内皮素家族的活性的方法。 特别地，提供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，以及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。 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或其前体来治疗内皮素介导的病症的方法。

公开(公告)号：US5464853A

公开(公告)日：1995-11-07

申请号：US142159

申请日：1993-10-21

申请人： Ming F. Chan ,  Bore G. Raju ,  Rosario S. Castillo ,  Adam Kois ,  Chengde Wu ,  Vitukudi Balaji

发明人： Ming F. Chan ,  Bore G. Raju ,  Rosario S. Castillo ,  Adam Kois ,  Chengde Wu ,  Vitukudi Balaji

IPC分类号： C07D261/14 ,  C07D261/16 ,  C07D261/20 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D261/06 ,  A61K31/41

CPC分类号： C07D261/14 ,  C07D261/16 ,  C07D261/20 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： N-(5-isoxazolyl)biphenylsulfonamides and N-(3-isoxazolyl)biphenylsulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(5-isoxazolyl)biphenylsulfonamides and N-(3-isoxazolyl)biphenylsulfonamides and methods for inhibiting the binding of an endothelin peptide to an endothelin receptor or increasing the activity of endothelin peptides by contacting the receptor with a 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 or increase the activity of endothelin are also provided.

摘要翻译： 提供N-（5-异恶唑基）联苯磺酰胺和N-（3-异恶唑基）联苯磺酰胺和调节或改变肽内皮素家族活性的方法。 特别地，提供了N-（5-异恶唑基）联苯磺酰胺和N-（3-异恶唑基）联苯磺酰胺和通过使受体与磺酰胺接触来抑制内皮素肽与内皮素受体的结合或增加内皮素肽的活性的方法 。 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或其前体来治疗内皮素介导的病症的方法。