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1. 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。

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

US5464853A N-(5-isoxazolyl)biphenylsulfonamides, N-(3-isoxazolyl)biphenylsulfonamides and derivatives thereof that modulate the activity of endothelin 失效
标题翻译： N-（5-异恶唑基）联苯磺酰胺，N-（3-异恶唑基）联苯磺酰胺及其衍生物，其调节内皮素的活性
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。

5. 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。

6. 发明授权

US5468778A Method of lowering intraocular pressure by administering a pharmaceutical composition containing 7-(5-substituted cyclopentyl) and 7-(5-substituted-cyclopentenyl) 5-heptenoic acids and derivatives 失效
标题翻译：通过施用含有7-（5-取代的环戊基）和7-（5-取代的环戊烯基）-5-庚烯酸和衍生物的药物组合物来降低眼内压的方法
公开(公告)号：US5468778A
公开(公告)日：1995-11-21
申请号：US950855
申请日：1992-09-24
申请人： Michael E. Garst , Robert M. Burk , Ming F. Chan , Michael B. Roof
发明人： Michael E. Garst , Robert M. Burk , Ming F. Chan , Michael B. Roof
IPC分类号： A61K31/557 , A61K31/19 , A61K31/215
CPC分类号： A61K31/557 , Y10S514/913
摘要： Intraocular pressure is lowered in the eye of a mammal by administration of a pharmaceutical composition containing as active ingredient a compound of the formula ##STR1## where the dotted line represents a bond or the absence of a bond, wavy lines connected to the olefinic bond represent cis or trans configuration about the olefinic bond; R.sub.1 represents H, or CO-R.sub.3 where R.sub.3 is lower alkyl of 1 to 6 carbons, carbocyclic aryl or heterocyclic aryl; or carbocyclic aryl or heteroaryl substituted lower alkyl group; R.sub.2 represents H or lower alkyl of 1 to 6 carbons, and n is an integer between 0 and 8.
摘要翻译：通过给药含有作为活性成分的式“IMAGE”的化合物的药物组合物，在哺乳动物的眼睛中降低眼内压，其中虚线表示键或不存在键，与烯键连接的波浪线代表关于烯键的顺式或反式构型; R1表示H或CO-R3，其中R3是1至6个碳的低级烷基，碳环芳基或杂环芳基; 或碳环芳基或杂芳基取代的低级烷基; R2表示H或碳原子数为1〜6的低级烷基，n为0〜8的整数。

7. 发明授权

US5238961A PGF 1-alcohols and their use as ocular hypotensives 失效
标题翻译： PGF 1-醇及其作为OCALAL HYPTENSIVES的用途
公开(公告)号：US5238961A
公开(公告)日：1993-08-24
申请号：US538204
申请日：1990-06-14
申请人： David F. Woodward , Ming F. Chan
发明人： David F. Woodward , Ming F. Chan
IPC分类号： A61K31/557 , A61K31/5575 , A61P9/12 , A61P27/02
CPC分类号： A61K31/557 , Y10S514/913
摘要： The invention relates to the use of alcohol derivatives of F-type prostaglandins as ocular hypotensives. The PGF derivatives used in accordance with the invention are encompassed by the following structural formula (I) ##STR1## wherein wherein wavy line attachments indicate either the alpha (.alpha.) or beta (b) configuration; hatched lines indicate .alpha. configuration, solid triangles are used to indicate b configuration, dashed bonds represent a double bond, the 5,6-double bond being in cis-configuration, or a single bond; R is hydrogen or a --(CO)R.sub.4 group; R.sub.1, R.sub.2, and R.sub.3 independently are hydroxyl, or --O(CO)R.sub.5 groups, wherein R.sub.4 and R.sub.5 independently stand for saturated or unsaturated acyclic hydrocarbon having from 1 to 20 carbon atoms, or --(CH.sub.2).sub.n R.sub.6 where n is 0-10 and R.sub.6 is an aliphatic, aromatic or heteroaromatic ring, R.sub.7 and R.sub.8 independently are hydrogen or alkyl of one to 6 carbon atoms or pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及使用F型前列腺素的醇衍生物作为眼部低血压。根据本发明使用的PGF衍生物包括以下结构式（I）其中波浪线附着物指示α（α）或β（b）构型; 阴影线表示α配置，实心三角形用于表示b构型，虚线键代表双键，5,6-双键处于顺式构型或单键; R是氢或 - （CO）R 4基团; R 1，R 2和R 3独立地是羟基或-O（CO）R 5基团，其中R 4和R 5独立地代表具有1至20个碳原子的饱和或不饱和的无环烃基，或 - （CH 2）n R 6，其中n是0- 10和R6是脂族，芳族或杂芳族环，R7和R8独立地是氢或1至6个碳原子的烷基或其药学上可接受的盐。

8. 发明授权

US5034413A Intraocular pressure reducing 9,11-diacyl prostaglandins 失效
标题翻译：眼内压降低9,11-二酰基前列腺素
公开(公告)号：US5034413A
公开(公告)日：1991-07-23
申请号：US585284
申请日：1990-09-18
申请人： Ming F. Chan , Charles Gluchowski , David F. Woodward
发明人： Ming F. Chan , Charles Gluchowski , David F. Woodward
IPC分类号： A61K31/557
CPC分类号： A61K31/557 , Y10S514/913
摘要： Certain 9,11-diacyl prostaglandins and their use for lowering intraocular pressure are disclosed herein.
摘要翻译：某些9,11-二酰基前列腺素及其用于降低眼压的用途在本文中公开。

9. 发明授权

US5312832A Ocular hypotensive 2-decarboxyl-2-acylthioalkyl prostaglandin derivatives 失效
标题翻译：眼低血压2-脱羧-2-酰硫烷基前列腺素衍生物
公开(公告)号：US5312832A
公开(公告)日：1994-05-17
申请号：US702220
申请日：1991-05-17
申请人： Ming F. Chan
发明人： Ming F. Chan
IPC分类号： A61K31/557 , A61K31/5575 , A61P9/12 , A61P27/02 , C07C405/00
CPC分类号： A61K31/557 , C07C405/0033
摘要： The present invention relates to 2-decarboxyl-2-acylthioalkyl prostaglandins that are potent ocular hypotentives, and are particularly suitable for the management of glaucoma.
摘要翻译：本发明涉及作为有效的眼睛低血糖素的2-癸羧-2-酰硫烷基前列腺素，特别适用于治疗青光眼。

10. 发明授权

US5288754A Polar C-1 esters of prostaglandins 失效
标题翻译：前列腺素的极性C-1酯
公开(公告)号：US5288754A
公开(公告)日：1994-02-22
申请号：US831023
申请日：1992-02-04
申请人： David F. Woodward , Ming F. Chan
发明人： David F. Woodward , Ming F. Chan
IPC分类号： A61K31/557 , C07C405/00
CPC分类号： C07C405/00 , A61K31/557
摘要： The present invention provides a method of treating ocular hypertension which comprises applying to the eye an amount sufficient to treat ocular hypertension of a compound of formula (I) ##STR1## wherein the wavy line attachments indicate either alpha (.alpha.) or beta (.beta.) configuration; hatched lines indicate .alpha. configuration, solid triangles are used to indicate .beta. configuration; the dashed bonds represent a single bond or a double bond which can be in the cis or trans configuration; X is selected from the group consisting of O, NH, S and NR, where R is an aliphatic hydrocarbon group of about 1 to about 6 carbon atoms; Y is a polar functional group; one of R.sub.1 and R.sub.2 is .dbd.O, --OH or a --O(CO)R.sub.4 group, and the other one is --OH or a --O(CO)R.sub.4 group or R.sub.1 is .dbd.O and R.sub.2 is is H; R.sub.3 is --OH or --O(CO)R.sub.4, wherein R.sub.4 is a saturated or unsaturated acyclic hydrocarbon group having from 1 to about 20 carbon atoms, or --(CH.sub.2).sub.n R.sub.5 wherein n is 0-10, and R.sub.5 is an aliphatic ring from about 3 to about 7 carbon atoms, or an aromatic or heteroaromatic ring; or a pharmaceutically acceptable salt thereof.Also disclosed are pharmaceutical compositions including an effective amount of the compound of formula I or a pharmaceutically-acceptable salt thereof, in admixture with a nontoxic pharmaceutical carrier and ophthalmic solutions comprising a compound of formula I packaged for metered application. Finally, novel compounds according to Formula I are disclosed.
摘要翻译：本发明提供一种治疗眼高血压的方法，其包括向眼睛施用足以治疗式（I）化合物（*化学结构*）（I）的眼高血压的量，其中波浪线附着物指示α（（ α））或β（（β））构型; 阴影线表示（α）配置，实心三角形用于指示（β）配置; 虚线键表示单键或双键，其可以是顺式或反式构型; X选自O，NH，S和NR，其中R是约1至约6个碳原子的脂族烃基; Y是极性官能团; R1和R2之一为= O，-OH或-O（CO）R4基团，另一个为-OH或-O（CO）R 4基团或R 1为= O且R 2为H; R3是-OH或-O（CO）R4，其中R4是具有1至约20个碳原子的饱和或不饱和的无环烃基，或 - （CH 2）n R 5，其中n是0-10，并且R 5是脂族环约3至约7个碳原子，或芳族或杂芳族环; 或其药学上可接受的盐。还公开了药物组合物，其包含有效量的式I化合物或其药学上可接受的盐与无毒药物载体的混合物和包含用于计量应用包装的式I化合物的眼用溶液。最后，公开了根据式I的新化合物。

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