公开(公告)号：WO2008089307A3

公开(公告)日：2008-11-06

申请号：PCT/US2008051273

申请日：2008-01-17

Applicant: LEXICON PHARMACEUTICALS INC ,  BARBOSA JOSEPH ,  BAUGH SIMON D P ,  HAN QIANG ,  LOMBARDO VICTORIA K ,  NGUYEN HUY VAN ,  PABBA PRAVEEN K ,  TERRANOVA KRISTEN M

Inventor： BARBOSA JOSEPH ,  BAUGH SIMON D P ,  HAN QIANG ,  LOMBARDO VICTORIA K ,  NGUYEN HUY VAN ,  PABBA PRAVEEN K ,  TERRANOVA KRISTEN M

IPC: C07C211/60 ,  A61K31/137 ,  A61K31/416 ,  A61P3/04 ,  C07D231/56

CPC classification number: C07C211/59 ,  C07C211/44 ,  C07C211/60 ,  C07C237/40 ,  C07C255/52 ,  C07C275/30 ,  C07D209/08 ,  C07D213/74 ,  C07D215/38 ,  C07D215/44 ,  C07D215/60 ,  C07D217/06 ,  C07D217/22 ,  C07D231/56 ,  C07D233/64 ,  C07D237/28 ,  C07D237/34 ,  C07D239/94 ,  C07D261/20 ,  C07D275/04 ,  C07D277/82 ,  C07D295/135 ,  C07D307/85 ,  C07D311/08 ,  C07D311/68 ,  C07D333/20 ,  C07D333/66 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D403/04 ,  C07D403/06 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D413/04 ,  C07D413/06 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D473/34 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D498/04

Abstract: This invention relates to methods of treating, managing and preventing pain, inflammation, cancer, and ocular diseases and disorders, and to compounds and pharmaceutical compositions useful in such methods.

Abstract translation: 本发明涉及治疗，控制和预防疼痛，炎症，癌症和眼部疾病和病症的方法，以及可用于这些方法的化合物和药物组合物。

公开(公告)号：WO2008067121A3

公开(公告)日：2008-06-05

申请号：PCT/US2007/083623

申请日：2007-11-05

Applicant: LEXICON PHARMACEUTICALS, INC. ,  BARBOSA, Joseph ,  DONG, Li ,  FINK, Cynthia Anne ,  LANTHORN, Thomas Herbert ,  WANG, Jian Cheng ,  ZIPP, G. Gregory

Inventor： BARBOSA, Joseph ,  DONG, Li ,  FINK, Cynthia Anne ,  LANTHORN, Thomas Herbert ,  WANG, Jian Cheng ,  ZIPP, G. Gregory

IPC: A61K31/397 ,  A61K31/4025 ,  A61K31/407 ,  A61K31/426 ,  A61K31/435 ,  A61K31/437 ,  A61K31/439 ,  A61K31/4409 ,  A61K31/496 ,  A61K31/506 ,  A61K31/519 ,  A61K31/551 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  A61P43/00

Abstract: This invention relates to methods for treating, managing and preventing cognitive impairment associated with various diseases and disorders, age-associated memory impairment, and dementia.

公开(公告)号：WO2007024789A1

公开(公告)日：2007-03-01

申请号：PCT/US2006/032620

申请日：2006-08-22

Applicant: LEXICON GENETICS INCORPORATED ,  FINK, Cynthia, Ann ,  BARBOSA, Joseph ,  ZIPP, G., Gregory ,  WANG, Jiancheng

Inventor： FINK, Cynthia, Ann ,  BARBOSA, Joseph ,  ZIPP, G., Gregory ,  WANG, Jiancheng

IPC: A61K31/519 ,  A61K31/437 ,  C07D487/04 ,  C07D471/04 ,  A61P25/28

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/519 ,  C07D487/04

Abstract: Disclosed are pyrrolopyridine, pyrrolopyrimidine and pyrazolopyridine compounds, compositions comprising them, and methods of their use.

Abstract translation: 公开了吡咯并吡啶，吡咯并嘧啶和吡唑并吡啶化合物，包含它们的组合物及其用途。

公开(公告)号：WO2006124897A3

公开(公告)日：2006-11-23

申请号：PCT/US2006/018917

申请日：2006-05-12

Applicant: LEXICON GENETICS INCORPORATED ,  BARBOSA, Joseph ,  DONG, Li ,  FINK, Cynthia Ann ,  LANTHORN, Thomas Herbert ,  WANG, Jiancheng ,  ZIPP, G. Gregory

Inventor： BARBOSA, Joseph ,  DONG, Li ,  FINK, Cynthia Ann ,  LANTHORN, Thomas Herbert ,  WANG, Jiancheng ,  ZIPP, G. Gregory

IPC: A61K31/506 ,  A61K31/497 ,  A61K31/551 ,  A61K31/519 ,  A61K31/437 ,  A61K48/00 ,  A61P25/28

Abstract: This invention encompasses methods of improving cognitive performance and of treating, preventing and managing various diseases and disorders, such as Alzheimer's disease, autism, cognitive disorders, dementia, learning disorders, and short- and long-term memory loss.

公开(公告)号：WO02102313A3

公开(公告)日：2003-04-03

申请号：PCT/US0219097

申请日：2002-06-17

Applicant: SQUIBB BRISTOL MYERS CO ,  GUO JUNQING ,  BARBOSA JOSEPH ,  PITTS WILLIAM JOHN ,  CARLSEN MARIANNE ,  QUESNELLE CLAUDE ,  DODIER MARCO

Inventor： GUO JUNQING ,  BARBOSA JOSEPH ,  PITTS WILLIAM JOHN ,  CARLSEN MARIANNE ,  QUESNELLE CLAUDE ,  DODIER MARCO

IPC: C07D491/113 ,  A61K31/00 ,  A61K31/496 ,  A61K31/505 ,  A61K31/506 ,  A61K31/513 ,  A61K31/517 ,  A61K31/519 ,  A61K31/522 ,  A61K31/538 ,  A61K31/5513 ,  A61K45/00 ,  A61P1/00 ,  A61P1/04 ,  A61P3/10 ,  A61P5/14 ,  A61P9/10 ,  A61P11/00 ,  A61P11/04 ,  A61P11/06 ,  A61P17/04 ,  A61P17/06 ,  A61P17/14 ,  A61P19/00 ,  A61P19/02 ,  A61P21/04 ,  A61P25/00 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P37/06 ,  A61P43/00 ,  C07D403/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D473/00 ,  C07D473/16 ,  C07D487/04 ,  C07D491/10 ,  C07D498/10 ,  A61K31/55 ,  C07D239/42 ,  C07D403/04

CPC classification number: C07D417/14 ,  A61K31/00 ,  A61K31/505 ,  A61K31/506 ,  A61K31/513 ,  A61K31/517 ,  A61K31/519 ,  A61K31/522 ,  C07D403/12 ,  C07D417/12 ,  C07D471/04 ,  C07D473/00 ,  C07D473/16 ,  C07D487/04 ,  C07D491/10

Abstract: Pyrimidine phosphodiesterase 7 (PDE 7) inhibitors of the following formula [insert chemical structure here] wherein R1, R2, Z, J and L are described herein, and analogs thereof are provided which are useful in treating T-cell mediated diseases.

Abstract translation: 本文描述了其中R1，R2，Z，J和L的下式[插入化学结构]的嘧啶磷酸二酯酶7（PDE 7）抑制剂及其类似物可用于治疗T细胞介导的疾病。

公开(公告)号：WO2002087513A3

公开(公告)日：2002-11-07

申请号：PCT/US2002/014049

申请日：2002-05-01

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  PITTS, William ,  BARBOSA, Joseph ,  GUO, Junqing

Inventor： PITTS, William ,  BARBOSA, Joseph ,  GUO, Junqing

IPC: A61K31/55

Abstract: Fused heterocylic phosphodiesterase 7 (PDE 7) inhibitors of the following formula (I) wherein R 1 , R 2 , R 5 , Z, J 1 and J 2 are described herein, and analogs thereof are provided which are useful in treating T-cell mediated diseases.

公开(公告)号：WO2008019276A2

公开(公告)日：2008-02-14

申请号：PCT/US2007/075022

申请日：2007-08-02

Applicant: LEXICON PHARMACEUTICALS, INC. ,  BARBOSA, Joseph ,  FINK, Cynthia Anne ,  GREEN, Michael Alan

Inventor： BARBOSA, Joseph ,  FINK, Cynthia Anne ,  GREEN, Michael Alan

IPC: A61K31/506 ,  A61P25/28 ,  C07D403/04

CPC classification number: C07D401/04

Abstract: Solid amorphous and crystalline forms of (3'-chlorobiphenyl-4-yl)(1-(pyrimidin-2-yl)piperidin-4-yl)methanone are disclosed, in addition to methods of their use in the treatment of various diseases and disorders.

Abstract translation: 除了它们的方法之外，还公开了（3'-氯联苯-4-基）（1-（嘧啶-2-基）哌啶-4-基）甲酮的固体无定形和结晶形式 用于治疗各种疾病和病症。

公开(公告)号：WO2006124748A3

公开(公告)日：2007-03-01

申请号：PCT/US2006018682

申请日：2006-05-12

Applicant: LEXICON GENETICS INC ,  BARBOSA JOSEPH ,  DONG LI ,  FINK CYNTHIA ANN ,  WANG JIANCHENG ,  ZIPP G GREGORY

Inventor： BARBOSA JOSEPH ,  DONG LI ,  FINK CYNTHIA ANN ,  WANG JIANCHENG ,  ZIPP G GREGORY

IPC: A61K31/506 ,  A61K31/496 ,  A61K31/551 ,  A61P25/28 ,  C07D239/42 ,  C07D277/42 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D451/02 ,  C07D487/04 ,  C07D487/08

CPC classification number: C07D239/42 ,  C07D277/42 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D417/04 ,  C07D451/02 ,  C07D471/08 ,  C07D487/04

Abstract: This invention relates to multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use in, for example, the treatment of cognitive disorders.

Abstract translation: 本发明涉及多环化合物，包含它们的药物组合物及其用于例如认知障碍治疗的方法。

公开(公告)号：WO2004043367A3

公开(公告)日：2004-05-27

申请号：PCT/US2003/035321

申请日：2003-11-06

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  BARBOSA, Joseph, ,  PITTS, William J, ,  GUO, Junqing

Inventor： BARBOSA, Joseph, ,  PITTS, William J, ,  GUO, Junqing

IPC: A61P1/00

Abstract: Fused heterocyclic compounds of the following Formula (I) wherein R 1 , R 2 , R 5 , Z, J 1 and J 2 are described herein, and analogs thereof are provided which are useful in treating leukocyte activation-associated disorders.

公开(公告)号：WO2003091252A1

公开(公告)日：2003-11-06

申请号：PCT/US2003/012898

申请日：2003-04-24

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  PITTS, William, J. ,  KIM, Soong-Hoon ,  BARBOSA, Joseph ,  VACCARO, Wayne

Inventor： PITTS, William, J. ,  KIM, Soong-Hoon ,  BARBOSA, Joseph ,  VACCARO, Wayne

IPC: C07D471/10

CPC classification number: C07D487/10

Abstract: Compound having the formula (I),wherein A, B and D are O or S; R 1a and R 1b are H, C 1-4 alkyl, C 2-4 alkenyl; X is-NR 2 -,-S-,-S(=O)-, or -S(O) 2 -; G 1 , G 2 and G 3 are together or separately selected from hetero, carbonyl, alkylene, and alkenylene groups and G 4 is optionally substituted methylene; R 2 is Q-Ar, wherein Q is a linker and Ar is substituted or substituted aryl or heteroaryl; and z is 0 or 1, are useful as inhibitors of MMPs, particularly MMP-13, aggrecanase, and/or TACE.

Abstract translation: 具有式（I）的化合物，其中A，B和D为O或S; R1a和R1b是H，C1-4烷基，C2-4链烯基; X是-NR 2 - ， - S - ， - S（= O） - 或-S（O）2 - ; G1，G2和G3一起或分别选自杂，羰基，亚烷基和亚烯基，G4是任选取代的亚甲基; R2是Q-Ar，其中Q是连接基，Ar是取代或取代的芳基或杂芳基; 和z为0或1，可用作MMP的抑制剂，特别是MMP-13，聚集蛋白聚糖蛋白聚糖酶和/或TACE。