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1. 发明授权

US5571821A 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：US5571821A
公开(公告)日：1996-11-05
申请号：US247072
申请日：1994-05-20
申请人： Ming Fai Chan , Bore G. Raju , Adam Kois , Erik J. Verner , Chengde Wu , Rosario S. Castillo , Venkatachalapathi Yalamoori , Vitukudi N. Balaji , Kalyanaraman Ramnarayan
发明人： Ming Fai Chan , Bore G. Raju , Adam Kois , Erik J. Verner , Chengde Wu , Rosario S. Castillo , Venkatachalapathi Yalamoori , Vitukudi N. Balaji , Kalyanaraman Ramnarayan
IPC分类号： C07D261/14 , C07D261/16 , C07D261/20 , C07D413/12 , C07D413/14 , C07D417/12 , A61K31/47
CPC分类号： C07D413/12 , C07D261/14 , C07D261/16 , C07D261/20 , C07D413/14 , C07D417/12
摘要： Sulfonamides 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. The sulfonamides have formula I: ##STR1## in which Ar.sup.1 is a 3- or 5-isoxazolyl and Ar.sup.2 is selected from among alkyl, including straight and branched chains, aromatic rings, fused aromatic rings and heterocyclic rings, including 5-membered heterocycles with one, two or more heteroatoms and fused ring analogs thereof and 6-membered rings with one, two or more heteroatoms and fused ring analogs thereof. Ar.sup.2 is preferably thiophenyl, furyl, pyrrolyl, naphthyl, and phenyl. Compounds in which Ar.sup.1 is a 4-halo-substituted isoxazole are more active than the corresponding alkyl-substituted compound and compounds in which Ar.sup.1 is substituted at this position with a higher alkyl tend to exhibit greater affinity for ET.sub.B receptors than the corresponding lower alkyl-substituted compound.
摘要翻译：提供磺酰胺和使用这些磺酰胺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。磺酰胺具有式I：其中Ar 1是3-或5-异恶唑基，Ar 2选自烷基，包括直链和支链，芳环，稠合芳环和杂环，其中包括5- 与一个，两个或更多个杂原子及其稠环类似物和六元环与一个，两个或更多个杂原子和稠合环类似物结合。 Ar 2优选为噻吩基，呋喃基，吡咯基，萘基和苯基。其中Ar1是4-卤素取代的异恶唑的化合物比相应的烷基取代的化合物更有活性，其中Ar1在该位置被高级烷基取代的化合物倾向于对ETB受体表现出比相应的低级烷基取代的化合物更大的亲和力，取代的化合物。

2. 发明授权

US5591761A Thiophenyl-, furyl-and pyrrolyl-sulfonamides and derivatives thereof that modulate the activity of endothelin 失效
标题翻译：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：US5591761A
公开(公告)日：1997-01-07
申请号：US222287
申请日：1994-04-05
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： A61K31/415 , A61K31/42 , A61K31/422 , A61K31/423 , A61K31/425 , A61K31/427 , A61P1/00 , A61P9/00 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/08 , A61P13/02 , A61P15/00 , A61P27/02 , A61P27/06 , A61P29/00 , A61P35/00 , A61P43/00 , C07D261/14 , C07D261/16 , C07D261/20 , C07D413/12 , C07D413/14 , C07D417/12 , C07D261/10
CPC分类号： C07D413/12 , C07D261/14 , C07D261/16 , C07D261/20 , C07D413/14 , C07D417/12
摘要： Thiophenyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, isoxazolyl-thiophenyl-sulfonamides, isoxazolyl-furyl-sulfonamides and isoxazolyl-pyrrolyl-sulfonamides 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：提供了噻吩基，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，提供了异恶唑基 - 噻吩基 - 磺酰胺，异恶唑基 - 呋喃基 - 磺酰胺和异恶唑基 - 吡咯基磺酰胺，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。

3. 发明授权

US5594021A Thienyl-, furyl- and pyrrolyl sulfonamides and derivatives thereof that modulate the activity of endothelin 失效
标题翻译：调节内皮素活性的噻吩基，呋喃基和吡咯基磺酰胺及其衍生物
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。

4. 发明授权

US5514691A N-(4-halo-isoxazolyl)-sulfonamides and derivatives thereof that modulate the activity of endothelin 失效
标题翻译： N-（4-卤代异恶唑基） - 磺酰胺及其衍生物，其调节内皮素的活性
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。

5. 发明授权

US5612895A Method of rational drug design based on ab initio computer simulation of conformational features of peptides 失效
标题翻译：基于从头计算机模拟肽构象特征的合理药物设计方法
公开(公告)号：US5612895A
公开(公告)日：1997-03-18
申请号：US427118
申请日：1995-04-21
申请人： Vitukudi N. Balaji , Chandra U. Singh
发明人： Vitukudi N. Balaji , Chandra U. Singh
IPC分类号： C07K16/00 , G06F17/50 , G06F19/16 , G06F15/42
CPC分类号： C07K16/00 , G06F19/16
摘要： A method of rational drug design includes simulating polypeptides in a way that predicts the most probable secondary and/or tertiary structures of a polypeptide, e.g., an oligopeptide, without any presumptions as to the conformation of the underlying primary or secondary structure. The method involves computer simulation of the polypeptide, and more particularly simulating a real-size primary structure in an aqueous environment, shrinking the size of the polypeptide isobarically and isothermally, and expanding the simulated polypeptide to its real size in selected time periods. A useful set of tools, termed Balaji plots, energy conformational maps, and probability maps, assist in identifying those portions of the predicted peptide structure that are most flexible or most rigid. The rational design of novel compounds, useful as drugs, e.g., bioactive peptidomimetic compounds, and constrained analogs thereof, is thus made possible using the simulation methods and tools of the described invention.
摘要翻译：合理药物设计的方法包括以预测多肽（例如寡肽）的最可能的次要和/或三级结构的方式来模拟多肽，而没有关于下面的一级或二级结构的构象的任何推定。该方法涉及多肽的计算机模拟，并且更具体地模拟水性环境中的实际一级结构，以等温和等温收缩多肽的大小，并在选定的时间段内将模拟多肽扩增至其实际大小。一组有用的工具，称为Balaji图，能量构象图和概率图，有助于确定最灵活或最刚性的预测肽结构的那些部分。因此，使用所述发明的模拟方法和工具可以合理地设计可用作药物的生物活性肽模拟化合物及其约束类似物的新化合物。

6. 发明授权

US5579250A Method of rational drug design based on AB initio computer simulation of conformational features of peptides 失效
标题翻译：基于AB初步计算机模拟肽的构象特征的合理药物设计方法
公开(公告)号：US5579250A
公开(公告)日：1996-11-26
申请号：US427987
申请日：1995-04-24
申请人： Vitukudi N. Balaji , Chandra U. Singh
发明人： Vitukudi N. Balaji , Chandra U. Singh
IPC分类号： C07K16/00 , G06F17/50 , G06F19/16
CPC分类号： C07K16/00 , G06F19/16
摘要： A method of rational drug design includes simulating polypeptides in a way that predicts the most probable secondary and/or tertiary structures of a polypeptide, e.g., an oligopeptide, without any presumptions as to the conformation of the underlying primary or secondary structure. The method involves computer simulation of the polypeptide, and more particularly simulating a real-size primary structure in an aqueous environment, shrinking the size of the polypeptide isobarically and isothermally, and expanding the simulated polypeptide to its real size in selected time periods. A useful set of tools, termed Balaji plots, energy conformational maps, and probability maps, assist in identifying those portions of the predicted peptide structure that are most flexible or most rigid. The rational design of novel compounds, useful as drugs, e.g., bioactive peptidomimetic compounds, and constrained analogs thereof, is thus made possible using the simulation methods and tools of the described invention.
摘要翻译：合理药物设计的方法包括以预测多肽（例如寡肽）的最可能的次要和/或三级结构的方式来模拟多肽，而没有关于下面的一级或二级结构的构象的任何推定。该方法涉及多肽的计算机模拟，并且更具体地模拟水性环境中的实际一级结构，以等温和等温缩小多肽的大小，并在选定的时间段内将模拟多肽扩增至其实际大小。一组有用的工具，称为Balaji图，能量构象图和概率图，有助于确定最灵活或最刚性的预测肽结构的那些部分。因此，使用所述发明的模拟方法和工具可以合理地设计可用作药物的生物活性肽模拟化合物及其约束类似物的新化合物。

7. 发明授权

US5543521A Compounds that modulate endothelin activity 失效
标题翻译：调节内皮素活性的化合物
公开(公告)号：US5543521A
公开(公告)日：1996-08-06
申请号：US180575
申请日：1994-01-12
申请人： Ming F. Chan , Vitukudi N. Balaji
发明人： Ming F. Chan , Vitukudi N. Balaji
IPC分类号： C07D487/04 , A61K31/495 , C07D207/16
CPC分类号： C07D487/04
摘要： Compounds of formula (I) and pharmaceutical compositions containing the compounds of formula (I): ##STR1## are provided. In formula (I): Ar is a substituted or unsubstituted aromatic or heterocyclic group; R is H or a substituted or unsubstituted straight or branched chain, cyclic or mixture of straight branched and cyclic alkyl, alkenyl, or alkynyl group having from 1-20 carbon atom; A is a functional group that bears a polar moiety; R.sub.1 is R, R--C=0, R substituted with one or more heteroatoms, a substituted or unsubstituted aryl group, or is aryl-(CH.sub.2).sub.n ; R.sub.2 is (CH.sub.2).sub.n, CHR, C(R).sub.2, COO, OCO, NHCO, CONH, SO, SO.sub.2 or NR; R.sub.3 and R.sub.4, which are the same or different or each may be absent, and are .dbd.O, H, O-aryl, OR, O-alkyl or alkyl, aryl, SR, S-aryl, NHR, NH-aryl, NR, or are other heteroaromatic groups; R.sub.5 is H, OH or R; E and F, which are the same or are different, are either N or (CH.sub.2).sub.p ; p is an integer or 0 between 0 and 5; m and n are integers or 0 between 0 and 10; T is O, S, NCOR or NR; U and V, which may be the same or different, are (CH.sub.2)n; W is CO, (CH.sub.2)n, (CH.sub.2).sub.n --CHR or CHR--(CH.sub.2).sub.n ; X and Y, which may be the same or different, are H, alkyl or aryl or X and Y form a saturated or unsaturated homocyclic or heterocyclic ring contain 3-15 members; and Z is H, SR, NHR or N(R).sub.2.
摘要翻译：式（I）化合物和含有式（I）化合物的药物组合物：取代或未取代的芳族或杂环基团; R是H或具有1-20个碳原子的直链或支链直链或支链，直链或环状的烷基，烯基或炔基的直链或支链的混合物; A是具有极性部分的官能团; R1是R，R-C = 0，被一个或多个杂原子取代的R，取代或未取代的芳基，或是芳基 - （CH 2）n; R2是（CH2）n，CHR，C（R）2，COO，OCO，NHCO，CONH，SO，SO2或NR; R 3和R 4相同或不同或各自不存在，并且为= O，H，O-芳基，OR，O-烷基或烷基，芳基，SR，S-芳基，NHR，NH-芳基，NR ，或其它杂芳族基团; R5是H，OH或R; E和F相同或不同，是N或（CH2）p; p是0或5之间的整数或0; m和n是整数，0是0和10之间; T为O，S，NCOR或NR; U和V可以相同或不同，是（CH 2）n; W是CO，（CH 2）n，（CH 2）n -CHR或CHR-（CH 2）n; X和Y可以相同或不同，是H，烷基或芳基，或X和Y形成含有3-15个成员的饱和或不饱和的杂环或杂环; 并且Z是H，SR，NHR或N（R）2。

8. 发明授权

US5331573A Method of design of compounds that mimic conformational features of selected peptides 失效
标题翻译：模拟所选肽的构象特征的化合物的设计方法
公开(公告)号：US5331573A
公开(公告)日：1994-07-19
申请号：US628111
申请日：1990-12-14
申请人： Vitukudi N. Balaji , Chandra U. Singh
发明人： Vitukudi N. Balaji , Chandra U. Singh
IPC分类号： C07K16/00 , G06F17/50 , G06F19/16 , G06F15/42
CPC分类号： C07K16/00 , G06F19/16
摘要： A method of rational drug design includes simulating polypeptides in a way that predicts the most probable secondary and/or tertiary structures of a polypeptide, e.g., an oligopeptide, without any presumptions as to the conformation of the underlying primary or secondary structure. The method involves computer simulation of the polypeptide, and more particularly simulating a real-size primary structure in an aqueous environment, shrinking the size of the polypeptide isobarically and isothermally, and expanding the simulated polypeptide to its real size in selected time periods. A useful set of tools, termed Balaji plots, energy conformational maps, and probability maps, assist in identifying those portions of the predicted peptide structure that are most flexible or most rigid. The rational design of novel compounds, useful as drugs, e.g., bioactive peptidomimetic compounds, and constrained analogs thereof, is thus made possible using the simulation methods and tools of the described invention.
摘要翻译：合理药物设计的方法包括以预测多肽（例如寡肽）的最可能的次要和/或三级结构的方式来模拟多肽，而没有关于下面的一级或二级结构的构象的任何推定。该方法涉及多肽的计算机模拟，并且更具体地模拟水性环境中的实际一级结构，以等温和等温收缩多肽的大小，并在选定的时间段内将模拟多肽扩增至其实际大小。一组有用的工具，称为Balaji图，能量构象图和概率图，有助于确定最灵活或最刚性的预测肽结构的那些部分。因此，使用所述发明的模拟方法和工具可以合理地设计可用作药物的生物活性肽模拟化合物及其约束类似物的新化合物。

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