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1. 发明授权

US5843906A Meta-substituted phenylene sulphonamide derivatives 失效
标题翻译：元取代亚苯基磺酰胺衍生物
公开(公告)号：US5843906A
公开(公告)日：1998-12-01
申请号：US824626
申请日：1997-03-27
申请人： Nizal Chandrakumar , Michael Clare , Wendell Doubleday , Alan F. Gasiecki , Mark A. Russell
发明人： Nizal Chandrakumar , Michael Clare , Wendell Doubleday , Alan F. Gasiecki , Mark A. Russell
IPC分类号： A61K31/00 , A61K31/195 , A61K31/415 , A61K31/4164 , A61K31/4168 , A61K31/44 , A61K31/445 , A61P3/00 , A61P3/14 , A61P9/00 , A61P9/10 , A61P35/00 , A61P35/04 , A61P43/00 , C07C311/42 , C07C311/46 , C07C311/47 , C07D211/96 , C07D213/55 , C07D233/50 , C07D295/26 , A61K38/00
CPC分类号： C07D295/26 , C07C311/42 , C07C311/46 , C07C311/47 , C07D211/96 , C07D213/55 , C07D233/50
摘要： The present invention relates to a class of compounds represented by the Formula I ##STR1## or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the .alpha..sub.v .beta..sub.3 integrin.
摘要翻译：本发明涉及一类由式I表示的化合物或其药学上可接受的盐，包含式I化合物的药物组合物和选择性抑制或拮抗αvβ3整联蛋白的方法。

2. 发明授权

US06677308B1 Meta-substituted phenylene sulphonamide derivatives 失效
标题翻译：元取代亚苯基磺酰胺衍生物
公开(公告)号：US06677308B1
公开(公告)日：2004-01-13
申请号：US09141547
申请日：1998-08-28
申请人： Nizal Chandrakumar , Michael Clare , Wendell Doubleday , Alan F. Gasiecki , Mark A. Russell
发明人： Nizal Chandrakumar , Michael Clare , Wendell Doubleday , Alan F. Gasiecki , Mark A. Russell
IPC分类号： A61K3800
CPC分类号： C07D295/26 , C07C311/42 , C07C311/46 , C07C311/47 , C07D211/96 , C07D213/55 , C07D233/50
摘要： The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the &agr;v&bgr;3 integrin.
摘要翻译：本发明涉及一类由式I表示的化合物或其药学上可接受的盐，包含式I化合物的药物组合物，以及选择性抑制或拮抗阿尔茨海因3整联蛋白的方法。

3. 发明授权

US5773646A Meta-substituted phenylene derivatives 失效
标题翻译：元取代亚苯衍生物
公开(公告)号：US5773646A
公开(公告)日：1998-06-30
申请号：US825086
申请日：1997-03-27
申请人： Nizal Chandrakumar , Barbara B. Chen , Helen Y. Chen , Michael Clare , Alan F. Gasiecki , Richard A. Haack , James W. Malecha , Peter G. Ruminski , Mark A. Russell
发明人： Nizal Chandrakumar , Barbara B. Chen , Helen Y. Chen , Michael Clare , Alan F. Gasiecki , Richard A. Haack , James W. Malecha , Peter G. Ruminski , Mark A. Russell
IPC分类号： A61K31/00 , A61K31/195 , A61K31/196 , A61K31/215 , A61K31/216 , A61K31/415 , A61K31/4164 , A61K31/4168 , A61K31/4184 , A61K31/496 , A61K31/505 , A61P1/00 , A61P1/02 , A61P19/00 , A61P19/08 , A61P19/10 , A61P27/00 , A61P27/02 , A61P35/00 , A61P43/00 , C07C45/67 , C07C49/796 , C07C205/35 , C07C205/45 , C07C205/56 , C07C205/57 , C07C257/16 , C07C257/18 , C07C259/18 , C07C275/42 , C07C279/18 , C07C279/24 , C07C279/28 , C07C311/46 , C07C311/47 , C07C317/42 , C07C317/44 , C07C323/44 , C07C323/56 , C07C335/16 , C07C335/22 , C07C335/32 , C07D223/06 , C07D233/50 , C07D233/88 , C07D235/30 , C07D239/14 , C07D311/18 , C07D311/20 , C07D405/12 , C07C241/00 , C07C205/00 , C07C229/00 , C07C321/00
CPC分类号： C07C45/673 , C07C205/35 , C07C205/45 , C07C205/56 , C07C205/57 , C07C257/16 , C07C259/18 , C07C275/42 , C07C279/18 , C07C279/24 , C07C279/28 , C07C311/46 , C07C311/47 , C07C317/42 , C07C323/44 , C07C335/16 , C07C335/22 , C07C335/32 , C07C49/796 , C07D223/06 , C07D233/50 , C07D233/88 , C07D235/30 , C07D239/14 , C07D311/18 , C07D311/20 , C07D405/12
摘要： The present invention relates to a class of compounds represented by the Formula I ##STR1## or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the .alpha..sub.v .beta..sub.3 integrin.
摘要翻译：本发明涉及一类由式I表示的化合物或其药学上可接受的盐，包含式I化合物的药物组合物和选择性抑制或拮抗αvβ3整联蛋白的方法。

4. 发明授权

US5585492A LTA.sub.4 Hydrolase inhibitors 失效
标题翻译： LTA4水解酶抑制剂
公开(公告)号：US5585492A
公开(公告)日：1996-12-17
申请号：US321183
申请日：1994-10-11
申请人： Nizal S. Chandrakumar , Barbara B. Chen , Michael Clare , Bipinchandra N. Desai , Stevan W. Djuric , Stephen H. Docter , Alan F. Gasiecki , Richard A. Haack , Chi-Dean Liang , Julie M. Miyashiro , Thomas D. Penning , Mark A,. Russell , Stella S. Yu
发明人： Nizal S. Chandrakumar , Barbara B. Chen , Michael Clare , Bipinchandra N. Desai , Stevan W. Djuric , Stephen H. Docter , Alan F. Gasiecki , Richard A. Haack , Chi-Dean Liang , Julie M. Miyashiro , Thomas D. Penning , Mark A,. Russell , Stella S. Yu
IPC分类号： C07D295/08 , A61K31/09 , A61K31/135 , A61K31/165 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/27 , A61K31/336 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/35 , A61K31/352 , A61K31/357 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4184 , A61K31/425 , A61K31/426 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/4468 , A61K31/46 , A61K31/495 , A61K31/535 , A61K31/55 , A61K31/695 , A61P17/00 , A61P29/00 , A61P43/00 , C07C217/16 , C07C217/18 , C07C229/08 , C07C229/12 , C07C237/06 , C07C271/44 , C07D207/06 , C07D207/08 , C07D207/12 , C07D207/16 , C07D209/12 , C07D209/52 , C07D211/34 , C07D211/58 , C07D211/60 , C07D211/62 , C07D211/74 , C07D213/30 , C07D213/55 , C07D213/56 , C07D213/61 , C07D213/69 , C07D213/73 , C07D213/74 , C07D213/75 , C07D215/12 , C07D223/02 , C07D225/02 , C07D235/08 , C07D277/20 , C07D277/24 , C07D277/34 , C07D295/092 , C07D295/12 , C07D295/14 , C07D295/18 , C07D295/185 , C07D295/215 , C07D295/22 , C07D295/26 , C07D303/02 , C07D307/42 , C07D307/81 , C07D311/58 , C07D317/54 , C07D333/16 , C07D333/32 , C07D401/04 , C07D401/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D417/12 , C07D451/02 , C07D471/04 , C07D471/08 , C07D473/00 , C07D473/28 , C07D491/048 , C07D491/107 , C07D207/10 , C07D207/14
CPC分类号： C07D295/185 , C07C217/16 , C07C229/12 , C07C237/06 , C07D277/24 , C07D295/088 , C07D295/215 , C07D295/26
摘要： The present invention provides compounds of the formula Ar.sup.1 --Q--Ar.sup.2 --Y--R--Z and pharmaceutically acceptable salts thereof wherein Ar.sup.1 and Ar.sup.2 are optionally substituted aryl moieties, Z is an optionally substituted nitrogen-containing moiety which may be an acyclic, cyclic or bicyclic amine or an optionally substituted monocyclic or bicyclic nitrogen-containing heteroaromatic moiety; Q is a linking group capable of linking two aryl groups; R is an alkylene moiety; Y is a linking moiety capable of linking an aryl group to an alkylene moiety and wherein Z is bonded to R through a nitrogen atom. The compounds and pharmaceutical compositions of the present invention are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD and asthma.
摘要翻译：本发明提供式Ar1-Q-Ar2-YRZ的化合物及其药学上可接受的盐，其中Ar1和Ar2是任选取代的芳基部分，Z是任选取代的含氮部分，其可以是无环的，环状的或双环的胺，或任选取代的单环或双环含氮杂芳基部分; Q是能够连接两个芳基的连接基团; R是亚烷基部分; Y是能够将芳基连接到亚烷基部分并且其中Z通过氮原子与R键合的连接部分。本发明的化合物和药物组合物可用于治疗由LTB4产生介导的炎性疾病，例如牛皮癣，溃疡性结肠炎，IBD和哮喘。

5. 发明授权

US06949578B2 Cycloalkyl alkanoic acids as integrin receptor antagonists 失效
标题翻译：环烷基链烷酸作为整联蛋白受体拮抗剂
公开(公告)号：US06949578B2
公开(公告)日：2005-09-27
申请号：US10891361
申请日：2004-07-14
申请人： Ish Kumar Khanna , Michael Clare , Alan F. Gasiecki , Thomas Rogers , Barbara Chen , Mark Russell , Hwang-Fun Lu
发明人： Ish Kumar Khanna , Michael Clare , Alan F. Gasiecki , Thomas Rogers , Barbara Chen , Mark Russell , Hwang-Fun Lu
IPC分类号： A61K31/4168 , A61K31/4375 , A61K31/44 , A61K31/4402 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/5383 , A61P3/14 , A61P9/00 , A61P9/10 , A61P19/02 , A61P19/10 , A61P21/00 , A61P27/02 , A61P35/00 , A61P35/04 , C07D213/74 , C07D231/38 , C07D233/88 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D498/04 , A61K31/415 , A61K31/4172 , C07D233/38
CPC分类号： C07D213/74 , C07D231/38 , C07D233/88 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要： The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the αvβ3 and/or αvβ5 integrin.
摘要翻译：本发明涉及一类由式I表示的化合物或其药学上可接受的盐，包含式I化合物的药物组合物和选择性抑制或拮抗α > 3和/或α

6. 发明授权

US06531494B1 Gem-substituted &agr;v&bgr;3 antagonists 失效
标题翻译：宝石取代的alphavbeta3拮抗剂
公开(公告)号：US06531494B1
公开(公告)日：2003-03-11
申请号：US09942214
申请日：2001-08-29
申请人： Ish Kumar Khanna , Yi Yu , Balekudru Devadas , Hwang-Fun Lu , Nizal S Chandrakumar , Renee M. Huff , Bipinchandra N. Desai , Srinivasan Raj Nagarajan , Alan F. Gasiecki , Thomas D. Penning , Mark A. Russell , Mark L. Boys , Lori A. Schretzman , Barbara B. Chen , Thomas Rogers , John Adam Wendt , Albert Khilevich , Yaping Wang
发明人： Ish Kumar Khanna , Yi Yu , Balekudru Devadas , Hwang-Fun Lu , Nizal S Chandrakumar , Renee M. Huff , Bipinchandra N. Desai , Srinivasan Raj Nagarajan , Alan F. Gasiecki , Thomas D. Penning , Mark A. Russell , Mark L. Boys , Lori A. Schretzman , Barbara B. Chen , Thomas Rogers , John Adam Wendt , Albert Khilevich , Yaping Wang
IPC分类号： A61K3144
CPC分类号： C07D213/74 , C07D213/73 , C07D401/12 , C07D471/04
摘要： The present invention relates to a class of compounds represented by the Formula I. or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the &agr;V&bgr;3 and/or the &agr;V&bgr;5 integrin.
摘要翻译：本发明涉及一类由式I表示的化合物或其药学上可接受的盐，包含式I化合物的药物组合物，以及选择性抑制或拮抗αVβ3和/或αVβ5整联蛋白的方法。

7. 发明授权

US06900232B2 Cycloalkyl alkanoic acids as integrin receptor antagonists 失效
标题翻译：环烷基链烷酸作为整联蛋白受体拮抗剂
公开(公告)号：US06900232B2
公开(公告)日：2005-05-31
申请号：US09882186
申请日：2001-06-15
申请人： Ish Kumar Khanna , Michael Clare , Alan F. Gasiecki , Thomas Rogers , Barbara Chen , Mark Russell , Hwang-Fun Lu
发明人： Ish Kumar Khanna , Michael Clare , Alan F. Gasiecki , Thomas Rogers , Barbara Chen , Mark Russell , Hwang-Fun Lu
IPC分类号： A61K31/4168 , A61K31/4375 , A61K31/44 , A61K31/4402 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/5383 , A61P3/14 , A61P9/00 , A61P9/10 , A61P19/02 , A61P19/10 , A61P21/00 , A61P27/02 , A61P35/00 , A61P35/04 , C07D213/74 , C07D231/38 , C07D233/88 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D498/04 , C07D213/72
CPC分类号： C07D213/74 , C07D231/38 , C07D233/88 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要： The present invention relates to a class of compounds represented by the Formula I Wherein A1 is a pyridinyl of the formula optionally substituted by one or more Rk selected from the group consisting of hydroxy, alkyl, alkoxy, alkoxyalkyl, thioalkyl, haloalkyl, cyano, amino alkylamino, halogen, acylamino, sulfonamide and —COR; and R is hydroxy, alkoxy, alkyl or amino; and pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the αvβ3 and/or αvβ5 integrin.
摘要翻译：本发明涉及由式I表示的一类化合物，其中A 1是下式的吡啶基，其任选被一个或多个选自下组的R 0选自羟基，烷基，烷氧基，烷氧基烷基，硫代烷基，卤代烷基，氰基，氨基烷基氨基，卤素，酰氨基，磺酰胺和-COR; 且R为羟基，烷氧基，烷基或氨基; 和其药学上可接受的盐，包含式I化合物的药物组合物，以及选择性抑制或拮抗α3β3和/或α / 5> 5＆lt; 5＆gt;整联蛋白。

8. 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.

9. 发明申请

US20090203690A1 5-SUBSTITUTED INDAZOLES AS KINASE INHIBITORS 有权
标题翻译：作为激素抑制剂的5-取代的吲哚美辛
公开(公告)号：US20090203690A1
公开(公告)日：2009-08-13
申请号：US12327991
申请日：2008-12-04
申请人： Irini Akritopoulou-Zanze , Brian D. Wakefield , Helmut Mack , Sean C. Turner , Alan F. Gasiecki , Vijaya J. Gracias , Kathy A. Sarris , Douglas M. Kalvin , Melissa J. Michmerhuizen , Qi Shuai , Jyoti R. Patel , Margaretha H.M. Bakker , Nicole Teusch , Eric F. Johnson , Peter J. Kovar , Stevan W. Djuric , Andrew J. Long , Anil Vasudevan , Dawn George , Lu Wang , Biqin Li , N. St. John Moore , Adrian D. Hobson , Keith W. Woods , Julie M. Miyashiro , Steven L. Swann, JR. , Thomas D. Penning
发明人： Irini Akritopoulou-Zanze , Brian D. Wakefield , Helmut Mack , Sean C. Turner , Alan F. Gasiecki , Vijaya J. Gracias , Kathy A. Sarris , Douglas M. Kalvin , Melissa J. Michmerhuizen , Qi Shuai , Jyoti R. Patel , Margaretha H.M. Bakker , Nicole Teusch , Eric F. Johnson , Peter J. Kovar , Stevan W. Djuric , Andrew J. Long , Anil Vasudevan , Dawn George , Lu Wang , Biqin Li , N. St. John Moore , Adrian D. Hobson , Keith W. Woods , Julie M. Miyashiro , Steven L. Swann, JR. , Thomas D. Penning
IPC分类号： A61K31/5377 , C07D403/04 , A61K31/4192 , C07D413/14 , C12N9/99 , A61P25/28 , A61P35/00
CPC分类号： C07D413/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中A，R 1，R 2，R 3和m在说明书中定义。本发明还涉及制备所述化合物的方法和含有所述化合物的组合物，其可用于抑制激酶例如糖原合成酶激酶3（GSK-3），Rho激酶（ROCK），Janus激酶（JAK），Cdc7，AKT ，PAK4，PLK，CK2，KDR，MK2，JNK1，极光，pim1和nek2。

10. 发明授权

US4754059A Omega cycloalkyl prostaglandins 失效
标题翻译：欧米茄环烷基前列腺素
公开(公告)号：US4754059A
公开(公告)日：1988-06-28
申请号：US669137
申请日：1984-11-07
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 I ##STR1## wherein X represents cis or trans --CH.dbd.CH--, --C.tbd.C--, methylene or ethylene;R.sub.1 represents a cycloalkyl group of the formula ##STR2## where m is 1 to 3 inclusive;R.sub.2 represents hydrogen or lower alkyl with the proviso that the sum of the carbon atoms in X and R.sub.1 is 7 or less;R' represents lower alkyl containing 1 to 6 carbon atoms, vinyl or ethynyl;wherein R'" represents hydroxymethyl, hydroxyacetyl or --CO.sub.2 R""wherein R"" represents hydrogen or lower alkyl containing 1 to 6 carbon atoms and the wavy line represents optional R or S stereochemistry.
摘要翻译：本发明包括式I的前列腺素，其中X代表顺式或反式-CH = CH-，-C 3位C，亚甲基或亚乙基; R1表示式为“IMAGE”的环烷基，其中m为1-3; R 2表示氢或低级烷基，条件是X和R 1中的碳原子之和为7或更小; R'表示含有1至6个碳原子的低级烷基，乙烯基或乙炔基; 其中R“表示羟甲基，羟基乙酰基或-CO 2 R”“，其中R”“表示氢或含有1至6个碳原子的低级烷基，波浪线表示任选的R或S立体化学。

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