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1. 发明授权

US5218139A Method for inhibiting IgE production 失效
标题翻译：抑制IgE产生的方法
公开(公告)号：US5218139A
公开(公告)日：1993-06-08
申请号：US892870
申请日：1992-06-03
申请人： Alan D. Levine , Paul W. Collins
发明人： Alan D. Levine , Paul W. Collins
IPC分类号： A61K31/557
CPC分类号： A61K31/557
摘要： A method is described for inhibiting IgE production which comprises administering, in an amount effective to inhibit IgE production, a prostaglandin of the formula: ##STR1## or a pharmaceutically acceptable non-toxic salt thereof, in which R is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.8 cycloalkyl, phenyl, or mono, di- or tri-substituted phenyl in which the substituents are selected form the group consisting of bromo, chloro, fluoro, iodo, C.sub.1 -C.sub.5 alkyl, hydroxy, nitro, acetyl, alkoxy, carboxy, acetoxy, amino, mono- or di- alkyl amino, amido and acetamido; R.sub.1 and R.sub.2 independently are hydrogen or C.sub.1 -C.sub.5 alkyl, n.sub.3, n.sub.4, n.sub.5, n.sub.6, n.sub.7, and n.sub.8 independently are zero or one; when n's are zeros, R.sub.3 and R.sub.4 together, R.sub.4 and R.sub.5 together, R.sub.5 and R.sub.6 together, and R.sub.7 and R.sub.8 together are double bonds; when n's are ones, R.sub.3, R.sub.5, R.sub.6 R.sub.7 and R.sub.8 independently are hydrogen, R.sub.4 is hydrogen or methyl, or R.sub.3 and R.sub.4 together, R.sub.4 and R.sub.5 together, or R.sub.5 and R.sub.6 together are methylene.
摘要翻译：描述了一种用于抑制IgE产生的方法，其包括以有效抑制IgE产生的量施用下式的前列腺素：其中R是氢，其中R是氢，C 1 -C 5烷基，其中取代基选自溴，氯，氟，碘，C 1 -C 5烷基，羟基，硝基，乙酰基，烷氧基，C 1 -C 5烷基，羧基，乙酰氧基，氨基，单或二烷基氨基，酰氨基和乙酰氨基; R 1和R 2独立地为氢或C 1 -C 5烷基，n 3，n 4，n 5，n 6，n 7和n 8独立地为0或1; 当n为零时，R 3和R 4一起，R 4和R 5一起，R 5和R 6一起，并且R 7和R 8一起是双键; 当n为1时，R 3，R 5，R 6 + L，R 7和R 8分别是氢，R 4是氢或甲基，或者R 3和R 4一起，R 4和R 5一起，或者R 5和R 6一起是亚甲基。

2. 发明授权

US5157052A Method for inhibiting IgE production 失效
标题翻译：阻止生产的方法
公开(公告)号：US5157052A
公开(公告)日：1992-10-20
申请号：US635000
申请日：1990-12-27
申请人： Alan D. Levine , Paul W. Collins
发明人： Alan D. Levine , Paul W. Collins
IPC分类号： A61K31/557 , A61K31/5575 , A61P37/00 , A61P37/08 , C07C405/00
CPC分类号： A61K31/557
摘要： A method is described for inhibiting IgE production which comprises administering, in an amount effective to inhibit IgE production, a prostaglandin of the formula: ##STR1## or a pharmaceutically acceptable non-toxic salt thereof, in which R is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.8 cycloalkyl, phenyl, or mono, di- or tri-substituted phenyl in which the substituents, are selected from the group consisting of bromo, chloro, fluoro, iodo, C.sub.1 -C.sub.5 alkyl, hydroxy, nitro, acetyl, alkoxy, carboxy, acetoxy, amino, mono- or di- alkyl amino, amido and acetamido; R.sub.1 and R.sub.2 independently are hydrogen or C.sub.1 -C.sub.5 alkyl, n.sub.3, n.sub.4, n.sub.5, n.sub.6, n.sub.7, and n.sub.8 independently are zero or one; when n's are zeros, R.sub.3 and R.sub.4 together, R.sub.4 and R.sub.5 together, R.sub.5 and R.sub.6 together, and R.sub.7 and R.sub.8 together are double bonds; when n's are ones, R.sub.3, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 independently are hydrogen, R.sub.4 is hydrogen or methyl, or R.sub.3 and R.sub.4 together, R.sub.4 and R.sub.5 together, or R.sub.5 and R.sub.6 together are methylene.

3. 发明授权

US07220770B2 Heterocyclo-substituted imidazoles for the treatment of inflammation 失效
标题翻译：杂环取代的咪唑用于治疗炎症
公开(公告)号：US07220770B2
公开(公告)日：2007-05-22
申请号：US11183016
申请日：2005-07-15
申请人： Ish K. Khanna , Richard M. Weier , Paul W. Collins , Yi Yu , Xiangdong Xu , Richard A. Partis , Francis J. Koszyk , Renee M. Huff
发明人： Ish K. Khanna , Richard M. Weier , Paul W. Collins , Yi Yu , Xiangdong Xu , Richard A. Partis , Francis J. Koszyk , Renee M. Huff
IPC分类号： A61K31/44 , C07D213/53 , C07D401/04
CPC分类号： C07D233/64 , C07D233/32 , C07D233/90 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D419/04
摘要： A class of imidazolyl compounds is described for use in treating inflammation. Compounds of particular interest are defined by formula (V), wherein R3 is a radical selected from hydrido, alkyl, haloalkyl, aralkyl, heterocycloalkyl, heteroaralkyl, acyl, cyano, alkoxy, alkylthio, alkylthioalkyl, alkylsulfonyl, cycloalkylthio, cycloalkylthioalkyl, cycloalkylsulfonyl, cycloalkylsulfonylalkyl, haloalkylsulfonyl, arylsulfonyl, halo, hydroxyalkyl, alkoxyalkyl, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heterocyclocarbonyl, cyanoalkyl, aminoalkyl, alkylaminoalkyl, N-arylaminoalkyl, N-alkyl-N-arylaminoalkyl, carboxyalkyl, alkoxy-carbonylalkyl, alkoxycarbonyl, haloalkylcarbonyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, alkylaminocarbonylalkyl, heteroarylalkoxyalkyl, heteroaryloxyalkyl, heteroarylthioalkyl, aralkoxy, aralkylthio, heteroaralkoxy, heteroaralkylthio, heteroarylalkylthioalkyl, heteroaryloxy, heteroarylthio, arylthioalkyl, aryloxyalkyl, arylthio, aryloxy, aralkylthioalkyl, aralkoxyalkyl, aryl and heteroaryl; wherein R4 is a radical selected from hydrido, alkyl and halo; and wherein R13 and R14 are independently selected from aryl and heterocyclo, wherein R13 and R14 are optionally substituted at a substitutable position with one or more radicals independently selected from alkylsulfonyl, aminosulfonyl, halo, alkylthio, alkyl, cyano, carboxyl, alkoxycarbonyl, haloalkyl, hydroxyl, alkoxy, hydroxyalkyl, alkoxyalkyl, haloalkoxy, amino, alkylamino, arylamino and nitro; provided at least one of R13 and R14 is aryl substituted with alkylsulfonyl or aminosulfonyl; or a pharmaceutically-acceptable salt thereof
摘要翻译：描述了一类咪唑基化合物用于治疗炎症。特别感兴趣的化合物由式（V）定义，其中R 3是选自氢，烷基，卤代烷基，芳烷基，杂环烷基，杂芳烷基，酰基，氰基，烷氧基，烷硫基，烷硫基烷基，烷基磺酰基环烷硫基，环烷硫基烷基，环烷基磺酰基，环烷基磺酰基烷基，卤代烷基磺酰基，芳基磺酰基，卤素，羟基烷基，烷氧基烷基，烷基羰基，芳基羰基，芳烷基羰基，杂环羰基，氰基烷基，氨基烷基，烷基氨基烷基，N-芳基氨基烷基，N-烷基-N-芳基氨基烷基，羧基烷基，烷氧基 - 烷氧基羰基，卤代烷基羰基，羧基，氨基羰基，烷基氨基羰基，烷基氨基羰基烷基，杂芳基烷氧基烷基，杂芳氧基烷基，杂芳硫基烷基，芳烷氧基，芳烷硫基，杂芳烷氧基，杂芳烷硫基，杂芳基烷硫基烷基，杂芳氧基，杂芳硫基，芳硫基烷基，芳氧基烷基，芳硫基，芳氧基，芳烷硫基烷基，芳烷氧基烷基，芳基和杂芳基。其中R 4是选自氢，烷基和卤素的基团; 并且其中R 13和R 14独立地选自芳基和杂环，其中R 13和R 14是任选地在可取代的位置被一个或多个独立地选自烷基磺酰基，氨基磺酰基，卤素，烷硫基，烷基，氰基，羧基，烷氧基羰基，卤代烷基，羟基，烷氧基，羟基烷基，烷氧基烷基，卤代烷氧基，氨基，烷基氨基，芳基氨基和硝基的基团取代。只要R 13和R 14中的至少一个为被烷基磺酰基或氨基磺酰基取代的芳基; 或其药学上可接受的盐

5. 发明授权

US6030959A Gastro-specific prodrugs 失效
标题翻译：胃特异性前药
公开(公告)号：US6030959A
公开(公告)日：2000-02-29
申请号：US49992
申请日：1998-03-30
申请人： Samuel J. Tremont , Paul W. Collins
发明人： Samuel J. Tremont , Paul W. Collins
IPC分类号： C07F7/18 , C07F7/10 , A61K31/695
CPC分类号： C07F7/1852
摘要： A compound is disclosed having the formulaAW--SiR.sup.1 R.sup.2 R.sup.3wherein R.sup.1 and R.sup.2 are independently alkyl, cycloalkyl, alkenyl, alkynyl, aryl, aralkyl, alkaryl, or a hydrophilic non-neutral group; R.sup.3 is a hydrophilic non-neutral group; and AW is the covalently bonded form of a drug AWH, wherein W is O, CO.sub.2, NH, S, or an enolate group. This compound serves as a prodrug for the drug AWH. A method for preparing these compounds is also disclosed. Also disclosed is a method of treatment or prevention of gastric ulcers by administering the prodrug compounds.
摘要翻译：公开了具有式-SiR 1 R 2 R 3的化合物，其中R 1和R 2独立地为烷基，环烷基，烯基，炔基，芳基，芳烷基，烷芳基或亲水性非中性基团; R3是亲水性非中性基团; AW是药物AWH的共价键合形式，其中W是O，CO 2，NH，S或烯醇化物基团。该化合物用作药物AWH的前药。还公开了制备这些化合物的方法。还公开了通过施用前药化合物治疗或预防胃溃疡的方法。

6. 发明授权

US5760068A Substituted pyrazolyl benzenesulfonamides for the treatment of inflammation 失效
标题翻译：用于治疗炎症的取代的吡唑基苯磺酰胺
公开(公告)号：US5760068A
公开(公告)日：1998-06-02
申请号：US648113
申请日：1996-09-06
申请人： John J. Talley , Thomas D. Penning , Paul W. Collins , Donald J. Rogier, Jr. , James W. Malecha , Julie M. Miyashiro , Stephen R. Bertenshaw , Ish K. Khanna , Matthew J. Graneto , Roland S. Rogers , Jeffery S. Carter , Stephen H. Docter , Stella S. Yu
发明人： John J. Talley , Thomas D. Penning , Paul W. Collins , Donald J. Rogier, Jr. , James W. Malecha , Julie M. Miyashiro , Stephen R. Bertenshaw , Ish K. Khanna , Matthew J. Graneto , Roland S. Rogers , Jeffery S. Carter , Stephen H. Docter , Stella S. Yu
IPC分类号： A61K31/415 , A61K31/4155 , A61K31/416 , A61K31/4178 , A61K31/4245 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/505 , A61K31/506 , A61P5/14 , A61P9/00 , A61P19/02 , A61P25/04 , A61P25/06 , A61P29/00 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/18 , C07D231/54 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D495/04
CPC分类号： C07D495/04 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/54 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
摘要： A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: ##STR1## or a pharmaceutically-acceptable salt thereof.
摘要翻译： PCT No.PCT / US94 / 12720 Sec。 371日期1996年9月6日 102（e）日期1996年9月6日PCT 1994年11月14日PCT PCT。 WO95 / 15316 PCT出版物日期：1995年6月8日描述了一类吡唑基苯磺酰胺化合物用于治疗炎症和炎症相关疾病。特别感兴趣的化合物由式II定义：其中R 1，R 2，

7. 发明授权

US5466823A Substituted pyrazolyl benzenesulfonamides 失效
标题翻译：取代的吡唑基苯磺酰胺
公开(公告)号：US5466823A
公开(公告)日：1995-11-14
申请号：US160594
申请日：1993-11-30
申请人： John J. Talley , Thomas D. Penning , Paul W. Collins , Donald J. Rogier, Jr. , James W. Malecha , Julie M. Miyashiro , Stephen R. Bertenshaw , Ish K. Khanna , Matthew J. Graneto , Roland S. Rogers , Jeffery S. Carter
发明人： John J. Talley , Thomas D. Penning , Paul W. Collins , Donald J. Rogier, Jr. , James W. Malecha , Julie M. Miyashiro , Stephen R. Bertenshaw , Ish K. Khanna , Matthew J. Graneto , Roland S. Rogers , Jeffery S. Carter
IPC分类号： A61K31/415 , A61P11/06 , A61P17/06 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/54 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D495/04 , C07D413/10
CPC分类号： C07D405/04 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/54 , C07D401/04 , C07D403/04 , C07D409/04 , C07D495/04
摘要： A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: ##STR1## or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类吡唑基苯磺酰胺化合物用于治疗炎症和炎症相关疾病。特别感兴趣的化合物由式I定义：其中（I）或其药学上可接受的盐。

8. 发明授权

US5177251A Halogenated tetraenyl prostaglandin derivatives 失效
标题翻译：卤代四烯基前列腺素衍生物
公开(公告)号：US5177251A
公开(公告)日：1993-01-05
申请号：US814750
申请日：1991-12-24
申请人： Paul W. Collins , Steven W. Kramer , Robert L. Shone
发明人： Paul W. Collins , Steven W. Kramer , Robert L. Shone
IPC分类号： C07C405/00
CPC分类号： C07C405/00
摘要： The present invention relates to a novel class of halogenated tetraenyl prostaglandin compounds represented by the following general formula ##STR1##or a pharmaceutically acceptable salt thereof, whereinY is --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --;R.sub.1 is H or a lower alkyl of 1 to 6 carbons;n is an integer from 0 to 3;m is an integer from 0 to 3 and n+m=3; X is Cl or F provided that when X is Cl, n is 2 and m is 1;R.sub.2 and R.sub.3 are independently H, lower alkyl from 1 to 6 carbons, Cl, --CH.sub.2 Cl, --CH.sub.2 F, --CHCl.sub.2, --CCl.sub.3, or taken together form a cycloalkyl of 3 to 6 carbons;R.sub.4 is H, lower alkyl from 1 to 6 carbons, Cl, F or taken together with R.sub.3 form a cycloalkenyl of 4 to 6 carbons; and provided that at least one of --CH.sub.n X.sub.m, R.sub.2, R.sub.3 and R.sub.4 includes a chlorine or fluorine atom.
摘要翻译：本发明涉及由以下通式表示的新一类卤代四烯基前列腺素化合物或其药学上可接受的盐，其中Y为-CH = CH-或-CH 2 -CH 2 - ; R1是H或1-6个碳原子的低级烷基; n为0〜3的整数。 m为0〜3的整数，n + m = 3; X是Cl或F，条件是当X是Cl时，n是2，m是1; R 2和R 3独立地是H，1-6个碳的低级烷基，Cl，-CH 2 Cl，-CH 2 F，-CHCl 2，-CCl 3，或一起形成3至6个碳的环烷基; R4是H，C1至6的低级烷基，C1，F或与R3一起形成4至6个碳的环烯基; 并且条件是-CH n X m，R 2，R 3和R 4中的至少一个包括氯或氟原子。

9. 发明授权

US5089524A Tetraenyl prostanoic acid derivatives as prodrugs for the treatment of peptic ulcer disease 失效
公开(公告)号：US5089524A
公开(公告)日：1992-02-18
申请号：US546218
申请日：1990-06-28
申请人： Paul W. Collins , Alan F. Gasiecki
发明人： Paul W. Collins , Alan F. Gasiecki
IPC分类号： C07C405/00
CPC分类号： C07C405/00
摘要： Tetraenyl Prostanoic Acid derivatives which are useful as prodrugs for the treatment of peptic ulcer disease and are represented by the following general formula ##STR1## are disclosed.

10. 发明授权

US4064350A 15,16-Dihydroxyprostaglandins 失效
标题翻译： 15,16-二氢前列地隐球菌素
公开(公告)号：US4064350A
公开(公告)日：1977-12-20
申请号：US744070
申请日：1976-11-22
申请人： Paul W. Collins , Raphael Pappo
发明人： Paul W. Collins , Raphael Pappo
IPC分类号： A61K31/20 , A61K31/215 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07C177/00
CPC分类号： C07C405/00
摘要： The present invention encompasses compounds of the formula: ##STR1## wherein one of A and B is methyl and the other is hydrogen, the wavy line represents R or S stereochemistry, n is 2-5, and R is hydrogen or lower alkyl having 1-7 carbon atoms.
摘要翻译：本发明包括下式的化合物：其中A和B之一是甲基，另一个是氢，波浪线代表R或S立体化学，n是2-5，R是氢或具有1个 -7个碳原子。

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