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1. 发明申请

WO0027832A2 PPAR GAMMA LIGANDS 审中-公开
公开(公告)号：WO0027832A2
公开(公告)日：2000-05-18
申请号：PCT/EP9908477
申请日：1999-11-09
申请人： GLAXO GROUP LTD , COLLINS JON LOREN , HOLMES CHRISTOPHER PATRICK , LENHARD JAMES MARTIN , WILLSON TIMOTHY MARK
发明人： COLLINS JON LOREN , HOLMES CHRISTOPHER PATRICK , LENHARD JAMES MARTIN , WILLSON TIMOTHY MARK
IPC分类号： A61K31/425 , A61K31/426 , A61K31/427 , A61K31/443 , A61K31/4439 , A61P3/00 , A61P3/04 , A61P3/10 , A61P9/00 , A61P19/10 , A61P29/00 , A61P35/00 , A61P43/00 , C07D277/14 , C07D417/06 , C07D417/10 , C07D417/12 , G01N33/566
CPC分类号： A61K31/4439 , A61K31/426 , A61K31/443 , C07D277/14 , G01N33/566 , G01N2333/70567
摘要： The present invention discloses novel PPARgamma ligands of Formula (I) and pharmaceutically acceptable salts and solvates thereof. The present invention also discloses a method for treating osteoporosis by administration of a PPARgamma antagonist.
摘要翻译：本发明公开了式（I）的新型PPARγ配体及其药学上可接受的盐和溶剂化物。本发明还公开了一种通过施用PPARγ拮抗剂治疗骨质疏松症的方法。

2. 发明申请

WO2004009091A1 PURINE DERIVATIVES AS LIVER X RECEPTOR AGONISTS 审中-公开
标题翻译：作为肝脏X受体激动剂的嘌呤衍生物
公开(公告)号：WO2004009091A1
公开(公告)日：2004-01-29
申请号：PCT/US2003/016016
申请日：2003-05-20
申请人： GLAXO GROUP LIMITED , BOGGS, Sharon , COLLINS, Jon, L , FIVUSH, Adam , STEWART, Eugene, Lee , WILLSON, Timothy, Mark
发明人： BOGGS, Sharon , COLLINS, Jon, L , FIVUSH, Adam , STEWART, Eugene, Lee , WILLSON, Timothy, Mark
IPC分类号： A61K31/52
CPC分类号： A61K31/522 , A61K31/52 , A61K31/675 , C07D473/04 , C07D473/06
摘要： The invention relates to methods for the treatment or prevention of an LXR mediated disease or condition, including cariovascular disease and atherosclerosis, novel compounds for use in such methods and pharmaceutical compositions comprising compounds for use in such methods.
摘要翻译：本发明涉及用于治疗或预防LXR介导的疾病或病症的方法，包括心血管疾病和动脉粥样硬化，用于此类方法的新化合物和用于此类方法的化合物的药物组合物。

3. 发明申请

WO02070011A3 TREATMENT OF PPAR MEDIATED DISEASES 审中-公开
标题翻译：治疗PPAR介导的疾病
公开(公告)号：WO02070011A3
公开(公告)日：2003-04-24
申请号：PCT/US0203017
申请日：2002-01-31
申请人： SMITHKLINE BEECHAM CORP , WILLSON TIMOTHY MARK
发明人： WILLSON TIMOTHY MARK
IPC分类号： A61K38/17 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , G01N33/566 , A61K31/421 , A61K31/426
CPC分类号： G01N33/566 , A61K38/1783 , G01N2333/70567 , G01N2500/00
摘要： This invention provides a method for identifying a treatment regime for a compound or composition effective in treating a PPAR mediated disease or condition. The method includes determingin a treatment regime for the compound or composition that causes expression of a surrogate market for PPAR delta activity whereby the determined dose and route of administration identifies an effective treatment protocol.
摘要翻译：本发明提供了一种用于鉴定治疗PPAR介导的疾病或病症的化合物或组合物的治疗方案的方法。该方法包括确定化合物或组合物的治疗方案，其导致PPARδ活性的替代市场的表达，由此所确定的给药剂量和给药途径识别有效的治疗方案。

4. 发明申请

WO2002061089A2 CRYSTALLIZED HNF4 GAMMA LIGAND BINDING DOMAIN POLYPEPTIDE AND SCREENING METHODS EMPLOYING SAME 审中-公开
标题翻译：结晶HNF4游离配体结合域多肽和筛选方法
公开(公告)号：WO2002061089A2
公开(公告)日：2002-08-08
申请号：PCT/US2002/002992
申请日：2002-01-31
申请人： SMITHKLINE BEECHAM CORPORATION , DAVIS, Roderick, Gerald , JOHNSON, Robert, Lloyd, Jr. , MILLER, Aaron, Bayne , MILLER, Ann, Brier , WAY, James, M. , WILLIAMS, Shawn, P. , WILLSON, Timothy, Mark , WISELY, George, Bruce
发明人： DAVIS, Roderick, Gerald , JOHNSON, Robert, Lloyd, Jr. , MILLER, Aaron, Bayne , MILLER, Ann, Brier , WAY, James, M. , WILLIAMS, Shawn, P. , WILLSON, Timothy, Mark , WISELY, George, Bruce
IPC分类号： C12N15/12
CPC分类号： C07K14/4702 , C07K2299/00
摘要： A solved three-dimensional crystal structure of an HNF4g ligand binding domain polypeptide is disclosed, along with a crystal form of the HNF4g ligand binding domain. Methods of designing modulators of the biological activity of HNF4g, and other HNF4 ligand binding domain polypeptides are also disclosed
摘要翻译：公开了HNF4g配体结合结构域多肽的解决的三维晶体结构以及HNF4g配体结合结构域的晶体形式。还公开了设计HNF4g和其他HNF4配体结合域多肽的生物学活性调节剂的方法

5. 发明申请

WO1997031907A1 SUBSTITUTED 4-HYDROXY-PHENYLALCANOIC ACID DERIVATIVES WITH AGONIST ACTIVITY TO PPAR-GAMMA 审中-公开
标题翻译：具有激动剂活性的PPAR-GAMMA的取代的4-羟基 - 苯甲酸衍生物
公开(公告)号：WO1997031907A1
公开(公告)日：1997-09-04
申请号：PCT/EP1997000916
申请日：1997-02-26
申请人： GLAXO GROUP LIMITED , WILLSON, Timothy, Mark , MOOK, Robert, Anthony, Jr. , KALDOR, Istvan , HENKE, Brad, Richard , DEATON, David, Norman , COLLINS, Jon, Loren , COBB, Jeffrey, Edmond , BRACKEEN, Markus , SHARP, Matthew, Jude , O'CALLAGHAN, John, Mark , ERICKSON, Greg, Alan , BOSWELL, Grady, Evan
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D263/56
CPC分类号： C07D213/64 , A61K31/192 , A61K31/216 , A61K31/353 , A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/422 , A61K31/423 , A61K31/425 , A61K31/427 , A61K31/44 , A61K31/4402 , A61K31/4439 , A61K31/4453 , A61K31/454 , A61K31/495 , C07C229/36 , C07C229/56 , C07C237/40 , C07C255/54 , C07C323/12 , C07C2601/14 , C07C2601/16 , C07D207/08 , C07D213/65 , C07D213/70 , C07D213/74 , C07D231/12 , C07D233/64 , C07D235/12 , C07D237/14 , C07D249/08 , C07D261/08 , C07D263/32 , C07D263/56 , C07D277/24 , C07D277/42 , C07D311/22 , C07D333/36 , C07D401/04 , C07D405/04 , C07D413/04 , C07D413/12 , C07D417/04
摘要： A compound having formula (I), wherein A is selected from the group consisting of: (i) phenyl, wherein said phenyl is optionally substituted by one or more halogen atoms, C1-6alkyl, C1-3alkoxy, C1-3fluoroalkoxy, nitrile, or -NR R where R and R are independently hydrogen or C1-3alkyl; (ii) a 5- or 6-membered heterocyclic group containing at least one heteroatom selected from oxygen, nitrogen and sulfur; and (iii) a fused bicyclic ring (a), wherein ring C represents a heterocyclic group as defined in point (ii) above, which bicyclic ring is attached to group B via a ring atom of ring C; B is selected from the group consisting of: (iv) C1-6alkylene; (v) -MC1-6alkylene or C1-6alkyleneMC1-6alkylene, wherein M is O, S, or -NR wherein R represents hydrogen or C1-3 alkyl; (vi) a 5- or 6-membered heterocyclic group containing at least one nitrogen heteroatom and optionally at least one further heteroatom selected from oxygen, nitrogen and sulfur and optionally substituted by C1-3 alkyl; and (vii) Het-C1-6alkylene, wherein Het represents a heterocyclic group as defined in point (vi) above; Alk represents C1-3alkylene; R represents hydrogen or C1-3alkyl; Z is selected from the group consisting of: (viii) -(C1-3alkylene) phenyl, which phenyl is optionally substituted by one or more halogen atoms; and (ix) -NR R , wherein R represents hydrogen or C1-3alkyl, and R represents -Y-(C=O)-T-R , or -Y-(CH(OH))-T-R .
摘要翻译：具有式（I）的化合物，其中A选自：（i）苯基，其中所述苯基任选被一个或多个卤素原子取代，C 1-6烷基，C 1-3烷氧基，C 1-3氟烷氧基，腈，或-NR 7 R 8，其中R 7和R 8独立地是氢或C 1-3烷基; （ii）含有至少一个选自氧，氮和硫的杂原子的5-或6-元杂环基; 和（iii）稠合双环（a），其中环C表示如上述点（ii）中所定义的杂环基，该双环通过环C的环原子连接至基团B; B选自：（iv）C 1-6亚烷基; （v）-MC1-6亚烷基或C 1-6亚烷基亚甲基亚烷基，其中M是O，S或-NR 2，其中R 2表示氢或C 1-3烷基; （vi）含有至少一个氮杂原子和任选至少一个选自氧，氮和硫的另外的杂原子并任选被C 1-3烷基取代的5-或6-元杂环基; 和（vii）Het-C 1-6亚烷基，其中Het表示如上述（vi）中所定义的杂环基; Alk表示C1-3亚烷基; R 1表示氢或C 1-3烷基; Z选自：（ii） - （C 1-3亚烷基）苯基，该苯基任选被一个或多个卤素原子取代; 和（ix）-NR 3 R 4，其中R 3表示氢或C 1-3烷基，R 4表示-Y-（C = O）-TR 5或-Y- （CH（OH）） - TR <5>。

6. 发明申请

WO2003090745A1 FXR AGONISTS FOR HEPATOPROTECTION AND TREATMENT OF CHOLESTASIS 审中-公开
标题翻译： FXR激素用于治疗和治疗胆汁淤积
公开(公告)号：WO2003090745A1
公开(公告)日：2003-11-06
申请号：PCT/US2003/010519
申请日：2003-04-07
申请人： SMITHKLINE BEECHAM CORPORATION , KLIEWER, Steven, Anthony , WILLSON, Timothy, Mark
发明人： KLIEWER, Steven, Anthony , WILLSON, Timothy, Mark
IPC分类号： A61K31/42
CPC分类号： A61K31/4439 , A61K31/42
摘要： Methods for the treatment of cholestatic liver disease and reduction and prevention of hepatic injury resulting from cholestasis via administration of a FXR ligand are provided.
摘要翻译：提供了通过施用FXR配体治疗胆汁淤积性肝病和减少和预防胆汁淤积引起的肝损伤的方法。

7. 发明申请

WO02061089A3 CRYSTALLIZED HNF4 GAMMA LIGAND BINDING DOMAIN POLYPEPTIDE AND SCREENING METHODS EMPLOYING SAME 审中-公开
标题翻译：结晶HNF4游离配体结合域多肽和筛选方法
公开(公告)号：WO02061089A3
公开(公告)日：2003-10-16
申请号：PCT/US0202992
申请日：2002-01-31
申请人： SMITHKLINE BEECHAM CORP , DAVIS RODERICK GERALD , JOHNSON ROBERT LLOYD JR , MILLER AARON BAYNE , MILLER ANN BRIER , WAY JAMES M , WILLIAMS SHAWN P , WILLSON TIMOTHY MARK , WISELY GEORGE BRUCE
发明人： DAVIS RODERICK GERALD , JOHNSON ROBERT LLOYD JR , MILLER AARON BAYNE , MILLER ANN BRIER , WAY JAMES M , WILLIAMS SHAWN P , WILLSON TIMOTHY MARK , WISELY GEORGE BRUCE
IPC分类号： C07K14/47 , C07K14/72 , C12N15/12 , G01N33/48 , G01N33/50 , G06F19/00 , G01N33/68
CPC分类号： C07K14/4702 , C07K2299/00
摘要： A solved three-dimensional crystal structure of an HNF4g ligand binding domain polypeptide is disclosed, along with a crystal form of the HNF4g ligand binding domain. Methods of designing modulators of the biological activity of HNF4g, and other HNF4 ligand binding domain polypeptides are also disclosed
摘要翻译：公开了HNF4g配体结合结构域多肽的解决的三维晶体结构以及HNF4g配体结合结构域的晶体形式。还公开了设计HNF4g和其他HNF4配体结合域多肽的生物学活性调节剂的方法

8. 发明申请

WO1997036579A1 USE OF AGONISTS OF THE PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA FOR TREATING OBESITY 审中-公开
标题翻译：使用过氧化物酶促反应物激活受体激素治疗肥胖
公开(公告)号：WO1997036579A1
公开(公告)日：1997-10-09
申请号：PCT/EP1997001552
申请日：1997-03-27
申请人： GLAXO GROUP LIMITED , WILLSON, Timothy, Mark
发明人： GLAXO GROUP LIMITED
IPC分类号： A61K31/00
CPC分类号： A61K31/196 , A61K31/00 , Y10S514/909
摘要： The use of agonists of the peroxisome proliferator activated receptor alpha (PPAR alpha ) for the manufacture of a medicament for the treatment of obesity and methods of treating obesity comprising the administration of a therapeutic amount of a PPAR alpha agonist.
摘要翻译：使用过氧化物酶体增殖物激活受体α（PPARα）的激动剂用于制备治疗肥胖症的药物和治疗肥胖症的方法，包括施用治疗量的PPARα激动剂。

9. 发明申请

WO1996011940A1 ACYL AMINO ACETAMIDE DERIVATIVES WITH AGONIST ACTIVITY FOR CCK-A RECEPTORS 审中-公开
标题翻译： ACYA氨基酰胺衍生物与CCK-A受体的激活活性
公开(公告)号：WO1996011940A1
公开(公告)日：1996-04-25
申请号：PCT/EP1995004026
申请日：1995-10-12
申请人： GLAXO WELLCOME INC. , DEZUBE, Milana , HIRST, Gavin, Charles , WILLSON, Timothy, Mark , SHERRILL, Ronald, George , SUGG, Elizabeth, Ellen , SZEWCZYK, Jerzy, Ryszard
发明人： GLAXO WELLCOME INC.
IPC分类号： C07K05/062
CPC分类号： C07D223/16 , A61K38/00 , C07D243/14 , C07D403/06 , C07D403/12 , C07K5/0222 , C07K5/06026 , C07K5/06078 , C07K5/06104 , C07K5/06139 , C07K5/06191 , C07K5/0821
摘要： A CCK-A agonist of the general formula (I) R R NCOCH2N(R )COR and physiologically acceptable salts thereof wherein, R is independently C3-6alkyl, C3-6cycloalkyl, C3-6alkenyl, phenyl, -(CH2)pCN or -(CH2)pCOO(C1-4alkyl) and R is independently C3-6alkyl, C3-6cycloalkyl, C3-6alkenyl, benzyl, phenyl or phenyl mono- or disubstituted independently with C1-3alkyl, cyano, hydroxy, dimethylamino, -O(C1-4alkyl), -O(CH2C6H5), -NH(C1-4alkyl), -COO(C1-4alkyl), -N(C1-4alkyl)2 pyrrolidino, morpholino, halogen or C1-3alkyl substituted by one or more fluorine atoms or R is C1-2alkyl and R is phenyl substituted at the 2- or 4-position with chloro, methyl, methoxy or methoxycarbonyl; or R and R together with the nitrogen atom to which they are attached represent the group of formula (II), wherein R is hydrogen or methyl, R represents hydrogen, hydroxy, fluoro dimethylamino, C1-4alkoxy or benzyloxy, and m is zero, 1 or 2; R represents a group selected from C1-6alkyl; phenyl or phenyl substituted by one or two groups independently selected from C1-3alkyl, C1-4alkoxy or halogen; or thiophenyl; R is a group of formula (III) or (IV).
摘要翻译：通式（I）R 1 R 2 NCOCH 2 N（R 3）COR 4的CCK-A激动剂及其生理学上可接受的盐，其中R 1独立地为C 3-6烷基， C 1-6烯基，苯基， - （CH 2）pCN或 - （CH 2）p COO（C 1-4烷基）和R 2独立地是C 3-6烷基，C 3-6环烷基，C 3-6烯基，苄基，氰基，羟基，二甲基氨基，-O（C 1-4烷基）， - O（CH 2 C 6 H 5），-NH（C 1-4烷基），-COO（C 1-4烷基）， - N（C 1-4烷基））2吡咯烷子基，吗啉代，卤素或被一个或多个氟原子取代的C 1-3烷基或R 1是C 1-2烷基，R 2是在2-或4-位被氯，甲基，甲氧基或甲氧羰基; 或R 1和R 2与它们所连接的氮原子一起代表式（II）的基团，其中R 7是氢或甲基，R 8表示氢，羟基，氟二甲基氨基，C 1-4烷氧基或苄氧基，m为0,1或2; R 3表示选自C 1-6烷基的基团; 苯基或被一个或两个独立地选自C 1-3烷基，C 1-4烷氧基或卤素的基团取代的苯基; 或噻吩基; R 4是式（III）或（IV）的基团。

10. 发明申请

WO2004009091A8 PURINE DERIVATIVES AS LIVER X RECEPTOR AGONISTS 审中-公开
标题翻译：作为肝脏X受体激动剂的嘌呤衍生物
公开(公告)号：WO2004009091A8
公开(公告)日：2004-12-29
申请号：PCT/US0316016
申请日：2003-05-20
申请人： GLAXO GROUP LTD , BOGGS SHARON , COLLINS JON L , FIVUSH ADAM , STEWART EUGENE LEE , WILLSON TIMOTHY MARK
发明人： BOGGS SHARON , COLLINS JON L , FIVUSH ADAM , STEWART EUGENE LEE , WILLSON TIMOTHY MARK
IPC分类号： C07D473/06 , A61K31/52 , A61K31/522 , A61K31/5377 , A61K31/541 , A61K31/55 , A61P3/06 , A61P9/00 , A61P9/10 , A61P43/00 , C07D473/04 , C07D473/08 , C07D273/04
CPC分类号： A61K31/522 , A61K31/52 , A61K31/675 , C07D473/04 , C07D473/06
摘要： The invention relates to methods for the treatment or prevention of an LXR mediated disease or condition, including cariovascular disease and atherosclerosis, novel compounds for use in such methods and pharmaceutical compositions comprising compounds for use in such methods.

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