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1. 发明授权

US06617324B1 Substituted pyrazoles as p38 kinase inhibitors 失效
标题翻译：取代的吡唑作为p38激酶抑制剂
公开(公告)号：US06617324B1
公开(公告)日：2003-09-09
申请号：US10114297
申请日：2002-04-02
申请人： Ashok S. Naraian , Michael Clare , Paul W. Collins , Joyce Zuowu Crich , Rajesh Devraj , Daniel L. Flynn , Lifeng Geng , Matthew J. Graneto , Cathleen E. Hanau , Gunnar J. Hanson , Susan J. Hartmann , Michael Hepperle , He Huang , Francis J. Koszyk , Shuyuan Liao , Suzanne Metz , Richard A. Partis , Thao D. Perry , Shashidhar N. Rao , Shaun Raj Selness , Michael S. South , Michael A. Stealey , John Jeffrey Talley , Michael L. Vazquez , Richard M. Weier , Xiangdong Xi , Ish K. Khanna , Yi Yu
发明人： Ashok S. Naraian , Michael Clare , Paul W. Collins , Joyce Zuowu Crich , Rajesh Devraj , Daniel L. Flynn , Lifeng Geng , Matthew J. Graneto , Cathleen E. Hanau , Gunnar J. Hanson , Susan J. Hartmann , Michael Hepperle , He Huang , Francis J. Koszyk , Shuyuan Liao , Suzanne Metz , Richard A. Partis , Thao D. Perry , Shashidhar N. Rao , Shaun Raj Selness , Michael S. South , Michael A. Stealey , John Jeffrey Talley , Michael L. Vazquez , Richard M. Weier , Xiangdong Xi , Ish K. Khanna , Yi Yu
IPC分类号： A61K31496
CPC分类号： C07D409/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D413/14 , C07D417/14 , C07D453/02 , C07D471/04 , C07D473/00 , C07D487/04
摘要： A class of pyrazole derivatives described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA wherein R1, R2, R3 and R4 are as described in the specification.
摘要翻译：一类描述用于治疗p38激酶介导的病症的吡唑衍生物。特别感兴趣的化合物由式IA定义，其中R1，R2，R3和R4如说明书中所述。

2. 发明授权

US06599934B1 3,4-diaryl thiopenes and analogs thereof having use as antiinflammatory agents 失效
标题翻译：具有用作抗炎剂的3,4-二芳基呋喃及其类似物
公开(公告)号：US06599934B1
公开(公告)日：2003-07-29
申请号：US09711737
申请日：2000-11-13
申请人： John J. Talley , Stephen R Bertenshaw , Paul W Collins , Thomas D. Penning , David B. Reitz , Roland S Rogers
发明人： John J. Talley , Stephen R Bertenshaw , Paul W Collins , Thomas D. Penning , David B. Reitz , Roland S Rogers
IPC分类号： C07D30702
CPC分类号： C07D307/38 , A61K31/341 , A61K31/365 , C07D307/58 , C07D333/16 , C07D333/18 , C07D333/28 , C07D333/38 , C07D409/04
摘要： A class of 3,4-diaryl substituted thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: wherein Y is selected from O, S and NR1; wherein R1 is selected from hydrido and lower alkyl; wherein X is one or two substituent selected from hydrido, halo, lower alkoxycarbonyl and carboxyl; wherein R2 and R3 are independently aryl or heteroaryl; and wherein R2 and R3 are optionally substituted at a substitutable position with one or more radicals selected from sulfamyl, alkylsulfonyl, halo, lower alkoxy and lower alkyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译：一类3,4-二芳基取代的噻吩，呋喃和吡咯衍生物及其类似物，含有它们的药物组合物和使用它们治疗炎症和炎症相关疾病的方法。特别感兴趣的化合物由式I定义：其中Y选自O，S和NR1; 其中R1选自氢和低级烷基; 其中X是一个或两个选自氢，卤素，低级烷氧基羰基和羧基的取代基; 其中R2和R3独立地是芳基或杂芳基; 并且其中R2和R3任选在可取代的位置被一个或多个选自磺酰胺基，烷基磺酰基，卤素，低级烷氧基和低级烷基的基团取代; 或其药学上可接受的盐。

3. 发明授权

US5668161A Substituted thiazoles for the treatment of inflammation 失效
标题翻译：用于治疗炎症的取代的噻唑
公开(公告)号：US5668161A
公开(公告)日：1997-09-16
申请号：US679462
申请日：1996-07-09
申请人： John J. Talley , Jeffery S. Carter , Paul W. Collins , Steven W. Kramer , Thomas D. Penning , Donald J. Rogier, Jr. , Roland S. Rogers
发明人： John J. Talley , Jeffery S. Carter , Paul W. Collins , Steven W. Kramer , Thomas D. Penning , Donald J. Rogier, Jr. , Roland S. Rogers
IPC分类号： C07D277/24 , A61K31/425 , A61K31/426 , A61K31/44 , A61P3/00 , A61P29/00 , C07D277/20 , C07D277/26 , C07D277/28 , C07D277/30 , C07D277/32 , C07D277/34 , C07D277/40 , C07D277/42 , C07D277/50 , C07D277/52 , C07D277/56 , C07D417/04 , C07D417/12
CPC分类号： C07D417/04 , C07D277/26 , C07D277/30 , C07D277/42 , C07D277/56 , C07D417/12
摘要： A class of substituted thiazolyl compounds is described for use in treating inflammation disorders. Compounds are defined by Formula II ##STR1## wherein R.sup.1 is selected from hydrido, alkyl, haloalkyl, cyanoalkyl, alkylamino, aralkyl, arylamino, heteroarylsulfonylalkyl, heteroarylsulfonylhaloalkyl, aralkylamino, aryloxyalkyl, alkoxycarbonyl, aryl optionally substituted at a substitutable position with one or more radicals selected from halo and alkoxy, and heterocyclic optionally substituted at a substitutable position with one or more radicals selected from halo and alkyl; wherein R.sup.4 is selected from alkyl and amino; and wherein R.sup.5 is selected from aryl and heteroaryl; wherein R.sup.5 is optionally substituted at a substitutable position with one or more radicals selected from halo, alkyl and alkoxy; provided R.sup.5 is not phenyl at position 4 when R.sup.1 is .alpha.,.alpha.-bis(trifluoromethyl)methanol and R.sup.4 is methyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类用于治疗炎症的取代的噻唑基化合物。化合物由式II其中R 1选自氢，烷基，卤代烷基，氰基烷基，烷基氨基，芳烷基，芳基氨基，杂芳基磺酰基烷基，杂芳基磺酰基卤代烷基，芳烷基氨基，芳氧基烷基，烷氧基羰基，任选地在可取代的位置被取代的芳基与一个或多个选自卤素和烷氧基的基团和任选地在可取代的位置被一个或多个选自卤素和烷基的基团取代的杂环; 其中R 4选自烷基和氨基; 并且其中R 5选自芳基和杂芳基; 其中R 5任选在可取代的位置被一个或多个选自卤素，烷基和烷氧基的基团取代; 条件是当R 1为α时，R 5不在第4位为苯基，α-双（三氟甲基）甲醇，且R 4为甲基; 或其药学上可接受的盐。

4. 发明授权

US5620999A Benzenesulfonamide subtituted imidazolyl compounds for the treatment of inflammation 失效
标题翻译：苯磺酰胺取代的咪唑基化合物用于治疗炎症
公开(公告)号：US5620999A
公开(公告)日：1997-04-15
申请号：US281903
申请日：1994-07-28
申请人： Richard M. Weier , Paul W. Collins , Michael A. Stealey , Thomas E. Barta
发明人： Richard M. Weier , Paul W. Collins , Michael A. Stealey , Thomas E. Barta
IPC分类号： A61P29/00 , C07D233/54 , C07D233/84 , C07D401/04 , C07D401/12 , C07D405/04 , C07D409/04 , A61K31/415 , C07D233/58
CPC分类号： C07D233/64 , C07D233/84 , C07D401/04 , C07D401/12 , C07D405/04 , C07D409/04
摘要： A class of imidazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II ##STR1## wherein R.sup.1 is selected from lower alkyl, lower haloalkyl, lower hydroxyalkyl, lower aralkenyl, lower aryloxyalkyl, lower arylthioalkyl and heteroaryl; wherein R.sup.3 is selected from lower alkyl and amino; and wherein R.sup.4 is one or more radicals selected from hydrido, halo, lower alkyl and lower alkoxy; or where R.sup.4 together with the phenyl radical forms naphthyl or benzodioxolyl; provided R.sup.1 is not lower alkyl when R.sup.3 is methyl and when R.sup.4 is hydrido, methyl, methoxy or chloro; 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和炎症相关疾病。特别感兴趣的化合物由式II其中R 1选自低级烷基，低级卤代烷基，低级羟烷基，低级芳烯基，低级芳氧基烷基，低级芳硫基烷基和杂芳基构成。其中R3选自低级烷基和氨基; 并且其中R 4是一个或多个选自氢，卤素，低级烷基和低级烷氧基的基团; 或其中R4与苯基一起形成萘基或苯并二恶唑基; 当R 3为甲基且R 4为氢，甲基，甲氧基或氯时，R 1不为低级烷基; 或其药学上可接受的盐。

5. 发明授权

US5563165A 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：US5563165A
公开(公告)日：1996-10-08
申请号：US457059
申请日：1995-06-01
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 , A61K31/535
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##
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：（I）

6. 发明授权

US5504215A Substituted pyrazolyl benzenesulfonamide compounds for the treatment of inflammation 失效
公开(公告)号：US5504215A
公开(公告)日：1996-04-02
申请号：US458079
申请日：1995-06-01
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
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.

7. 发明授权

US5055569A N-(6)-substituted adenosine compounds 失效
标题翻译： N-（6） - 衍生的腺苷化合物
公开(公告)号：US5055569A
公开(公告)日：1991-10-08
申请号：US423923
申请日：1989-10-19
申请人： Daniel P. Becker , Paul W. Collins , Daniel L. Flynn
发明人： Daniel P. Becker , Paul W. Collins , Daniel L. Flynn
IPC分类号： C07H19/167 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61P1/00 , C07H19/16
CPC分类号： C07H19/16
摘要： The present invention relates to N-(6)-substituted adenosine compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein Z is an amine and R.sub.1 and R.sub.2 are independently hydrogen, hydroxyl, halogen, alkyl, phenyl, alkoxy, morpholino, piperidino, piperazino, phenoxy, thiophenoxy or amino optionally substituted by alkyl, aralkyl or phenyl.

8. 发明授权

US4820728A Tetraenyl prostaglandins 失效
标题翻译：四烯基前列腺素
公开(公告)号：US4820728A
公开(公告)日：1989-04-11
申请号：US68608
申请日：1987-06-30
申请人： Paul W. Collins , Alan F. Gasiecki
发明人： Paul W. Collins , Alan F. Gasiecki
IPC分类号： C07C405/00 , C07C177/00
CPC分类号： C07C405/00
摘要： This invention encompasses prostaglandins of the formula ##STR1## wherein R represents hydrogen or lower alkyl having 1 to 6 carbon atoms; R.sub.1 represents hydrogen, vinyl, or lower alkyl having 1 to 4 carbon atoms and the wavy line represents R or S stereochemistry; R.sub.2, R.sub.3, and R.sub.4 are hydrogen or lower alkyl having 1 to 4 carbom atoms or R.sub.2 and R.sub.3 together with carbon Y form a cycloalkenyl having 4 to 6 carbon atoms or R.sub.3 and R.sub.4 together with carbons X and Y form a cycloalkenyl having 4 to 6 carbons. Compounds of this invention have potent gastric antisecretory and cytoprotective properties with unexpectedly low diarrheogenic side effects.
摘要翻译：本发明包括式IMA的前列腺素，其中R表示氢或具有1至6个碳原子的低级烷基; R1表示氢，乙烯基或具有1至4个碳原子的低级烷基，波浪线表示R或S立体化学; R 2，R 3和R 4是氢或具有1至4个碳原子的低级烷基或R 2和R 3与碳Y一起形成具有4至6个碳原子的环烯基，或者R 3和R 4与碳一起形成X和Y形成具有4至 6个碳。本发明的化合物具有强烈的胃分泌和细胞保护性能，具有出乎意料的低泻药副作用。

9. 发明授权

US4713477A Omega cycloalkyl prostaglandins 失效
标题翻译：欧米茄环烷基前列腺素
公开(公告)号：US4713477A
公开(公告)日：1987-12-15
申请号：US798197
申请日：1985-11-14
申请人： Paul W. Collins , Alan F. Gasiecki
发明人： Paul W. Collins , Alan F. Gasiecki
IPC分类号： C07C405/00 , C07C177/00
CPC分类号： C07C405/0025 , C07C405/00
摘要： This invention encompasses prostaglandins of the formula I ##STR1## wherein R represents hydrogen or lower alkyl containing 1 to 6 carbon atoms;X represents --CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --CH.sub.2 --C.tbd.C--, --CH.sub.2 --CH.dbd.CH-- --CH.sub.2 --CH.sub.2 --CH.sub.2, --CH.dbd.CH--CH.sub.2 --, --C.tbd.C--CH.sub.2 --; andR.sub.1 represents cyclopropyl, cyclobutyl, cyclopentyl, 1-methylcyclopropyl or 1-methylcyclobutyl or XR.sub.1 together represent 1-methyl-1-cyclopropylethyl or 1-methyl-1-cyclobutylethyl; and R.sub.2 is lower alkyl having 1 to 4 carbon atoms or vinyl or ethynyl; the wavy line represents optional R or S sterochemistryThese compounds are potent antisecretory agents.
摘要翻译：本发明包括式I的前列腺素，其中R表示氢或含有1至6个碳原子的低级烷基; X表示-CH 2 - ， - CH = CH - ， - C 3BOND C - ， - CH 2 -CH 3 CH-，-CH 2 -CH = CH- -CH 2 -CH 2 -CH 2，-CH = CH-CH 2 - ， - 3OND C-CH2-; R1代表环丙基，环丁基，环戊基，1-甲基环丙基或1-甲基环丁基或XR1一起代表1-甲基-1-环丙基乙基或1-甲基-1-环丁基乙基; 和R2是具有1至4个碳原子的低级烷基或乙烯基或乙炔基; 波浪线代表任选的R或S类固体化学这些化合物是有效的抗分泌剂。

10. 发明授权

US4689419A Novel intermediate compounds in a process for producing 16-phenoxy- and 16-substituted phenoxy-9-keto-prostatrienoic acid derivatives 失效
标题翻译：在制备16-苯氧基和16-取代的苯氧基-9-酮 - 前列腺烯酸衍生物的方法中的新型中间体化合物
公开(公告)号：US4689419A
公开(公告)日：1987-08-25
申请号：US930616
申请日：1986-11-14
申请人： Paul W. Collins , Richard M. Weier
发明人： Paul W. Collins , Richard M. Weier
IPC分类号： C07F7/18
CPC分类号： C07F7/1856
摘要： This invention relates to the production of novel intermediate compounds which are useful in the process for producing 16-phenoxy- and 16-substituted phenoxy-9-keto-prostatrienoic acid derivatives, the antisecretory agents of U.S. Pat. No. 4,178,457.
摘要翻译：本发明涉及可用于生产16-苯氧基 - 和16-取代的苯氧基-9-酮 - 前列腺烯酸衍生物的方法的新的中间体化合物的生产，美国专利No. 第4,178,457号。

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