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1. 发明申请

WO2007120270A2 GLUCAGON RECEPTOR ANTAGONISTS, PREPARATION AND THERAPEUTIC USES 审中-公开
标题翻译：胰高血糖素受体拮抗剂，制剂和治疗用途
公开(公告)号：WO2007120270A2
公开(公告)日：2007-10-25
申请号：PCT/US2006/060976
申请日：2006-11-16
申请人： ELI LILLY AND COMPANY , CONNER, Scott, Eugene , HIPSKIND, Philip, Arthur , LI, Jianke , ZHU, Guoxin
发明人： CONNER, Scott, Eugene , HIPSKIND, Philip, Arthur , LI, Jianke , ZHU, Guoxin
CPC分类号： C07D257/06 , C07D257/04
摘要： The present invention discloses novel compounds of Formula (I), or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.
摘要翻译：本发明公开了具有胰高血糖素受体拮抗剂或反向激动剂活性的式（I）的新型化合物或其药学上可接受的盐，以及制备该化合物的方法。在另一个实施方案中，本发明公开了包含式（I）化合物的药物组合物以及使用它们治疗糖尿病和其他胰高血糖素相关代谢疾病等的方法。

2. 发明申请

WO2006086488A3 SUBSTITUTED THIOPHENE DERIVATIVES AS GLUCAGON RECEPTOR ANTAGONISTS, PREPARATION AND THERAPEUTIC USES 审中-公开
标题翻译：作为GLUCAGON受体拮抗剂，制备和治疗用途的替代的噻吩衍生物
公开(公告)号：WO2006086488A3
公开(公告)日：2006-12-14
申请号：PCT/US2006004461
申请日：2006-02-09
申请人： LILLY CO ELI , CHAPPELL MARK DONALD , CONNER SCOTT EUGENE , TRIPP ALLIE EDWARD , ZHU GUOXIN
发明人： CHAPPELL MARK DONALD , CONNER SCOTT EUGENE , TRIPP ALLIE EDWARD , ZHU GUOXIN
IPC分类号： C07D333/24 , A61K31/381 , A61P3/10
CPC分类号： C07D333/38 , C07D409/12
摘要： The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have glucagon receptor antagonist or inverse agonist activity, as well as methods of using these compounds and intermediates and methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.
摘要翻译：本发明公开了具有胰高血糖素受体拮抗剂或反向激动剂活性的新颖的式（I）化合物或其药学上可接受的盐，以及使用这些化合物和中间体的方法以及制备这些化合物的方法。在另一个实施方案中，本发明公开了包含式（I）化合物的药物组合物以及使用它们治疗糖尿病和其它与胰高血糖素相关的代谢紊乱等的方法。

3. 发明申请

WO2004063184A1 THIOPHENE DERIVATIVE PPAR MODULATORS 审中-公开
标题翻译：噻吩衍生物PPAR调节剂
公开(公告)号：WO2004063184A1
公开(公告)日：2004-07-29
申请号：PCT/US2003/039118
申请日：2003-12-31
申请人： ELI LILLY AND COMPANY , MANTLO, Nathan, Bryan , WANG, Xiaodong , ZHU, Guoxin
发明人： MANTLO, Nathan, Bryan , WANG, Xiaodong , ZHU, Guoxin
IPC分类号： C07D333/16
CPC分类号： C07D333/18 , C07D333/16
摘要： The present invention is directed to compounds represented by the following structural formula, Formula I: and stereoisomers, pharmaceutically acceptable salts, solvates and hydrates thereof, wherein: (a) X is selected from the group consisting of O, S, S(O)2, N, and a bond; (b) U is an aliphatic linker wherein one carbon atom of the aliphatic linker may be replaced with O, NH or S, and wherein such aliphatic linker is optionally substituted with R30; (c) Y is selected from the group consisting of C, O, S, NH and a single bond; and (d) E is C(R3)(R4)A or A.
摘要翻译：本发明涉及由以下结构式式I表示的化合物及其立体异构体，药学上可接受的盐，溶剂合物和水合物，其中：（a）X选自O，S，S（O） 2，N和键; （b）U是脂族连接体，其中脂族连接体的一个碳原子可被O，NH或S取代，并且其中这种脂族连接基任选被R 30取代; （c）Y选自C，O，S，NH和单键; 和（d）E是C（R3）（R4）A或A。

4. 发明申请

WO2004063155A1 FUSED HETEROCYCLIC DERIVATIVES AS PPAR MODULATORS 审中-公开
标题翻译：作为PPAR调节剂的熔融杂环衍生物
公开(公告)号：WO2004063155A1
公开(公告)日：2004-07-29
申请号：PCT/US2003/039120
申请日：2003-12-31
申请人： ELI LILLY AND COMPANY , CONNER, Scott, Eugene , MANTLO, Nathan, Bryan , ZHU, Guoxin
发明人： CONNER, Scott, Eugene , MANTLO, Nathan, Bryan , ZHU, Guoxin
IPC分类号： C07D209/10
CPC分类号： C07D209/10 , C07D235/18 , C07D263/57 , C07D277/60 , C07D277/66 , C07D413/12 , C07D417/12 , C07D471/04 , C07D513/04
摘要： The present invention is directed to compounds represented by the following structural formula, Formula I: wherein (a) X is selected from the group consisting of a single bond, O, S. S(O) 2 and N; (b) U is an aliphatic linker; (c) Y is selected from the group consisting of C, O, S, NH and a single bond; (d) E is C(R3) (R4)A or A and wherein (i) A is selected from the group consisting of carboxyl, tetrazole, C 1 -C 6 alkylnitrile, carboxamidek, sulfonamide and acylsulfonamide; (e) B is selected from the group consisting of S, O, C, and N; (f) Z is selected from the group consisting of N and C; with the proviso that when B is C then Z is N.
摘要翻译：本发明涉及由以下结构式（I）表示的化合物：其中（a）X选自单键，O，S，S（O）2和N; （b）U是脂族连接体; （c）Y选自C，O，S，NH和单键; （d）E是C（R3）（R4）A或A，其中（i）A选自羧基，四唑，C 1 -C 6烷基腈，甲酰胺，磺酰胺和酰基磺酰胺; （e）B选自S，O，C和N; （f）Z选自N和C; 条件是当B为C时，则Z为N.

6. 发明申请

WO2007123581A1 GLUCAGON RECEPTOR ANTAGONISTS, PREPARATION AND THERAPEUTIC USES 审中-公开
公开(公告)号：WO2007123581A1
公开(公告)日：2007-11-01
申请号：PCT/US2006/060857
申请日：2006-11-14
申请人： ELI LILLY AND COMPANY , LI, Jianke , ZHU, Guoxin
发明人： LI, Jianke , ZHU, Guoxin
IPC分类号： C07C233/83 , A61K31/166 , A61P3/10
CPC分类号： C07C233/83
摘要： The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.

7. 发明申请

WO2004063166A1 HETEROCYCLIC PPAR MODULATORS 审中-公开
标题翻译：杂环PPAR调节剂
公开(公告)号：WO2004063166A1
公开(公告)日：2004-07-29
申请号：PCT/US2003/039119
申请日：2003-12-31
申请人： ELI LILLY AND COMPANY , CONNER, Scott, Eugene , MA, Tianwei , MANTLO, Nathan, Bryan , MAYHUGH, Daniel, Ray , SCHKERYANTZ, Jeffrey, Michael , WARSHAWSKY, Alan, M. , ZHU, Guoxin
发明人： CONNER, Scott, Eugene , MA, Tianwei , MANTLO, Nathan, Bryan , MAYHUGH, Daniel, Ray , SCHKERYANTZ, Jeffrey, Michael , WARSHAWSKY, Alan, M. , ZHU, Guoxin
IPC分类号： C07D231/12
CPC分类号： C07D231/12 , C07D233/20 , C07D233/22 , C07D233/64 , C07D249/06 , C07D253/04 , C07D261/08
摘要： The present invention is directed to compounds represented by the following structural formula, Formula I: wherein: (a) X is selected from the group consisting of a single bond, O, S, S(O)2 and N; (b) U is an aliphatic linker; (c) Y is selected from the group consisting of O, C, S, NH and a single bond; (d) E is C(R3)(R4)A or A and wherein (i) A is selected from the group consisting of carboxyl, tetrazole, C1-C6 alkylnitrile, carboxamide, sulfonamide and acylsulfonamide; (e) Z1 and Z2 are each independently selected from the group consisting of N, O, and C with the proviso that at least one of Z1 and Z2 is N; (f) Z3 is selected from the group consisting of N, O, and C. (g) R8 is selected from the group consisting of hydrogen, C1-C6 alkyl, C1-C4 alkylenyl and halo; (h) R9 is selected from the group consisting of hydrogen, C1-C4 alkyl, C1-C4 alkylenyl, halo, aryl- C0-C4 alkyl, heteroaryl, C1-C6 allyl, and OR29.
摘要翻译：本发明涉及由以下结构式（I）表示的化合物：其中：（a）X选自单键，O，S，S（O）2和N; （b）U是脂族连接体; （c）Y选自O，C，S，NH和单键; （d）E是C（R3）（R4）A或A，其中（i）A选自羧基，四唑，C 1 -C 6烷基腈，甲酰胺，磺酰胺和酰基磺酰胺; （e）Z1和Z2各自独立地选自N，O和C，条件是Z1和Z2中的至少一个是N; （f）Z 3选自N，O和C.（g）R 8选自氢，C 1 -C 6烷基，C 1 -C 4亚烷基和卤素; （h）R 9选自氢，C 1 -C 4烷基，C 1 -C 4亚烷基，卤素，芳基-C 0 -C 4烷基，杂芳基，C 1 -C 6烯丙基和OR 29。

8. 发明申请

WO0228861A8 METHODS AND COMPOUNDS FOR TREATING PROLIFERATIVE DISEASES 审中-公开
标题翻译：用于治疗增殖性疾病的方法和化合物
公开(公告)号：WO0228861A8
公开(公告)日：2003-11-20
申请号：PCT/US0127728
申请日：2001-09-24
申请人： LILLY CO ELI , ENGLER THOMAS ALBERT , FURNESS KELLY WAYNE , MALHOTRA SUSHANT , BRIGGS STEPHEN LYLE , BROOKS HAROLD BURNS , CLAWSON DAVID KEYES , SANCHEZ-MARTINEZ CONCEPCION , ZHANG FAMING , ZHU GUOXIN
发明人： ENGLER THOMAS ALBERT , FURNESS KELLY WAYNE , MALHOTRA SUSHANT , BRIGGS STEPHEN LYLE , BROOKS HAROLD BURNS , CLAWSON DAVID KEYES , SANCHEZ-MARTINEZ CONCEPCION , ZHANG FAMING , ZHU GUOXIN
IPC分类号： A61P35/00 , C07D403/14 , C07D487/14 , A61K31/407
CPC分类号： C07D403/14 , C07D487/14
摘要： The compounds disclosed herein are indolocarbazoles of Formula (I), which are potent CDK4 inhibitors, and are useful in the treatment of cell proliferative disorders, including cancer. Formula (I).
摘要翻译：本文公开的化合物是式（I）的吲哚并唑，其是有效的CDK4抑制剂，并且可用于治疗包括癌症的细胞增殖性疾病。式（I）。

10. 发明申请

WO2003072102A1 PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR MODULATORS 审中-公开
标题翻译：过氧化物促进剂激活受体调节剂
公开(公告)号：WO2003072102A1
公开(公告)日：2003-09-04
申请号：PCT/US2003/002680
申请日：2003-02-13
申请人： ELI LILLY AND COMPANY , CONNER, Scott, Eugene , MANTLO, Nathan, Bryan , ZHU, Guoxin
发明人： CONNER, Scott, Eugene , MANTLO, Nathan, Bryan , ZHU, Guoxin
IPC分类号： A61K31/426
CPC分类号： C07D413/04 , C07D263/32 , C07D277/24 , C07D277/26 , C07D413/10 , C07D417/04 , C07D417/10
摘要： The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts thereof, Formula I: wherein:(a) R5 is selected from the group consisting of (C 1 -C 6 ) alkyl, (C 1 -C 6 ) alkenyl, substituted aryl(C 0 -C 4 )alkyl, substituted aryloxy(C 0 -C 4 )alkyl, substituted arylthio(C 0 -C 4 )alkyl, unsubstituted aryl(C 0 -C 4 )alkyl, unsubstituted aryloxy(C 0 -C 4 )alkyl, and unsubstituted arylthio(C 0 -C 4 )alkyl; (b) T1 is C or N;(c) Q is selected from the group consisting of O, a single bond, O(CH 2 ) q and C;(d) q is 1 or 2;(e) W is selected from the group consisting of O, S, (CH 2 ) r N(R20)(CH 2 ) k , NHSO 2 , C(O)N(R20)(CH 2 ) r , (CH 2 ) r N(R20)C(O), and SO 2 ;(f) X is C m H 2m ;(g) m is 0, 1 or 2;(h) A is an functional group selected from the group consisting of carboxyl, C1-C3 alkylnitrile, carboxamide, and (CH 2 ) n COOR19; and(i) R19 is selected from the group consisting of hydrogen, optionally substituted C1-C4alkyl and optionally substituted arylmethyl.
摘要翻译：本发明涉及由以下结构式表示的化合物及其药学上可接受的盐，式I：其中：（a）R 5选自（C 1 -C 6）烷基，（C 1 -C 6）烯基，取代的芳基（C 0 -C 4）烷基，取代的芳氧基（C 0 -C 4）烷基，取代的芳硫基（C 0 -C 4）烷基，未取代的芳基（C 0 -C 4）烷基，未取代的芳氧基（C 0 -C 4）烷基和未取代的芳硫基 1 -C 4）烷基; （b）T1是C或N;（c）Q选自O，单键，O（CH 2）q和C;（d）q是1或2;（e）W选自由O，S，（CH2）rN（R20）（CH2）k，NHSO2，C（O）N（R20）（CH2）r，（CH2）rN（R20）C（O）和SO2组成的组; （f）X是CmH2m;（g）m是0,1或2;（h）A是选自羧基，C 1 -C 3烷基腈，甲酰胺和（CH 2）n COOR 19的官能团; 和（i）R 19选自氢，任选取代的C 1 -C 4烷基和任选取代的芳基甲基。

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