公开(公告)号：WO2009134726A1

公开(公告)日：2009-11-05

申请号：PCT/US2009/041848

申请日：2009-04-27

Applicant: ABBOTT LABORATORIES ,  LIU, Huaqing ,  DRIZIN, Irene ,  COWART, Marlon, D. ,  ALTENBACH, Robert, J.

Inventor： LIU, Huaqing ,  DRIZIN, Irene ,  COWART, Marlon, D. ,  ALTENBACH, Robert, J.

IPC: C07D239/70 ,  C07D403/12 ,  C07D471/04 ,  C07D491/048 ,  C07D513/04 ,  C07D519/00 ,  A61K31/517 ,  A61K31/519

CPC classification number: C07D491/048 ,  C07D239/70 ,  C07D403/12 ,  C07D471/04 ,  C07D513/04 ,  C07D519/00

Abstract: The present application describes substituted pyrimidine compounds of formula (I) wherein X, A 1 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , p, q, r, v, and w are defined in the specification, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions and disorders using such compounds and compositions.

Abstract translation: 本申请描述了式（I）的取代嘧啶化合物，其中X，A1，R1，R2，R3，R4，R5，R6，R7，R8，R9，p，q，r，v和w在本说明书中定义 ，包含这些化合物的组合物，制备该化合物的方法，以及使用这些化合物和组合物治疗和预防疾病进展，病症和病症的方法。

公开(公告)号：WO2009114575A1

公开(公告)日：2009-09-17

申请号：PCT/US2009/036728

申请日：2009-03-11

Applicant: ABBOTT LABORATORIES ,  LIU, Huaqing ,  KOENIG, John, R. ,  COWART, Marlon, D. ,  BLACK, Lawrence, A.

Inventor： LIU, Huaqing ,  KOENIG, John, R. ,  COWART, Marlon, D. ,  BLACK, Lawrence, A.

IPC: C07D239/95 ,  C07D471/10 ,  C07D487/10 ,  A61K31/517 ,  A61P25/00

CPC classification number: C07D239/95 ,  C07D471/10 ,  C07D487/10

Abstract: Macrocyclic spiro pyrimidine compounds, of formula (I) compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions, and disorders using such compounds and compositions are described herein. (I)

Abstract translation: 本文描述了包含这种化合物的式（I）组合物的大环螺嘧啶化合物，制备该化合物的方法，以及使用这些化合物和组合物治疗和预防疾病进展，病症和病症的方法。 （一世）

公开(公告)号：WO2007150010A2

公开(公告)日：2007-12-27

申请号：PCT/US2007/071849

申请日：2007-06-22

Applicant: ABBOTT LABORATORIES ,  LIU, Huaqing ,  BLACK, Lawrence A. ,  BENNANI, Youssef L. ,  COWART, Marlon D.

Inventor： LIU, Huaqing ,  BLACK, Lawrence A. ,  BENNANI, Youssef L. ,  COWART, Marlon D.

IPC: C07D207/06 ,  C07D401/10 ,  C07D403/10 ,  C07D417/10 ,  C07D495/04 ,  A61K31/4025 ,  A61K31/4439 ,  A61K31/455 ,  A61K31/501 ,  A61K31/506 ,  A61K31/4365 ,  A61K31/454 ,  A61K31/4196 ,  A61K31/397 ,  A61K31/55 ,  A61P25/00

CPC classification number: C07D207/06 ,  C07D401/10 ,  C07D403/10 ,  C07D417/10 ,  C07D495/04

Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).

Abstract translation: 式（I）化合物可用于治疗由组胺-3受体配体预防或改善的病症或病症。 还公开了包含组胺-3受体配体的药物组合物，使用这些化合物和组合物的方法，以及制备式（I）范围内的化合物的方法。

公开(公告)号：WO2005113536A2

公开(公告)日：2005-12-01

申请号：PCT/US2005/014866

申请日：2005-04-29

Applicant: ABBOTT LABORATORIES ,  ALTENBACH, Robert, J. ,  BLACK, Lawrence, A. ,  CHANG, Sou-jen ,  COWART, Marlon, D. ,  FAGHIH, Ramin ,  GFESSER, Gregory, A. ,  KU, Yi-yin ,  LIU, Huaqing ,  LUKIN, Kirill, A. ,  NERSESIAN, Diana, L. ,  PU, Yu-ming ,  CURTIS, Michael, P.

Inventor： ALTENBACH, Robert, J. ,  BLACK, Lawrence, A. ,  CHANG, Sou-jen ,  COWART, Marlon, D. ,  FAGHIH, Ramin ,  GFESSER, Gregory, A. ,  KU, Yi-yin ,  LIU, Huaqing ,  LUKIN, Kirill, A. ,  NERSESIAN, Diana, L. ,  PU, Yu-ming ,  CURTIS, Michael, P.

IPC: C07D401/00

CPC classification number: C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04

Abstract: Compounds of formula (I) wherein R 1 or R 2 is a tricyclic or bicyclic ring, each of which contains at least two heteroatoms, and R 1 , R 2 , R 3 , R 3a , R 3b , R 4 , R 5 , L, X, X', Y, Y', Z, and Z' are as defined herein, are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).

Abstract translation: 式（I）化合物其中R 1或R 2是三环或双环，其各自含有至少两个杂原子，R 1，R 2，R 3，R 3a，R 3b，R 4，R 5，L，X，X'，Y， Y'，Z和Z'如本文所定义，可用于治疗由组胺-3受体配体预防或改善的病症或病症。 还公开了包含组胺-3受体配体的药物组合物，使用这些化合物和组合物的方法，以及制备式（I）范围内的化合物的方法。

公开(公告)号：EP1751149B1

公开(公告)日：2012-06-06

申请号：EP05743943.2

申请日：2005-04-29

Applicant: Abbott Laboratories

Inventor： ALTENBACH, Robert, J. ,  BLACK, Lawrence, A. ,  CHANG, Sou-jen ,  COWART, Marlon, D. ,  FAGHIH, Ramin ,  GFESSER, Gregory, A. ,  KU, Yi-yin ,  LIU, Huaqing ,  LUKIN, Kirill, A. ,  NERSESIAN, Diana, L. ,  PU, Yu-ming ,  CURTIS, Michael, P.

IPC: C07D401/08 ,  C07D417/14 ,  C07D401/04 ,  C07D417/04 ,  C07D413/04 ,  C07D409/14 ,  C07D215/12 ,  C07D401/14 ,  A61K31/4709 ,  A61P25/28 ,  A61P25/00 ,  C07D413/14

CPC classification number: C07D215/12 ,  C07D401/04 ,  C07D401/08 ,  C07D401/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

Abstract: Compounds of formula (I) wherein R1 or R2 is an aromatic or non-aromatic ring directly joined or joined by a linker, as represented by L2 and L3, to a heteroaromatic core, and X, X', Y, Y', Z, Z', R1, R2, R3, R3a, R3b, R4, R5, L, L2, and L3 are as defined herein, are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).

公开(公告)号：EP1888523A2

公开(公告)日：2008-02-20

申请号：EP06771824.7

申请日：2006-06-01

Applicant: ABBOTT LABORATORIES

Inventor： LIU, Huaqing ,  HANCOCK, Arthur, A. ,  COWART, Marlon, D.

IPC: C07D207/06

CPC classification number: C07D207/06 ,  C07D401/10 ,  C07D403/10 ,  C07D417/10

Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).

公开(公告)号：EP1888523B1

公开(公告)日：2011-10-26

申请号：EP06771824.7

申请日：2006-06-01

Applicant: ABBOTT LABORATORIES

Inventor： LIU, Huaqing ,  HANCOCK, Arthur, A. ,  COWART, Marlon, D.

IPC: C07D207/06

CPC classification number: C07D207/06 ,  C07D401/10 ,  C07D403/10 ,  C07D417/10

Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).

Abstract translation: 式（I）化合物可用于治疗由组胺-3受体配体预防或缓解的病症或障碍。 还公开了包含组胺-3受体配体的药物组合物，使用这些化合物和组合物的方法以及制备式（I）范围内的化合物的方法。

公开(公告)号：EP2049472A2

公开(公告)日：2009-04-22

申请号：EP07784511.3

申请日：2007-06-22

Applicant: ABBOTT LABORATORIES

Inventor： LIU, Huaqing ,  BLACK, Lawrence A. ,  BENNANI, Youssef L. ,  COWART, Marlon D.

IPC: C07D207/06 ,  C07D401/10 ,  C07D403/10 ,  C07D417/10 ,  C07D495/04 ,  A61K31/4025 ,  A61K31/4439 ,  A61K31/455 ,  A61K31/501 ,  A61K31/506 ,  A61K31/4365 ,  A61K31/454 ,  A61K31/4196 ,  A61K31/397 ,  A61K31/55 ,  A61P25/00

CPC classification number: C07D207/06 ,  C07D401/10 ,  C07D403/10 ,  C07D417/10 ,  C07D495/04

Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).

Abstract translation: 式（I）化合物可用于治疗由组胺-3受体配体预防或缓解的病症或障碍。 还公开了包含组胺-3受体配体的药物组合物，使用这些化合物和组合物的方法以及制备式（I）范围内的化合物的方法。

公开(公告)号：EP1751149A1

公开(公告)日：2007-02-14

申请号：EP05743943.2

申请日：2005-04-29

Applicant: ABBOTT LABORATORIES

Inventor： ALTENBACH, Robert, J. ,  BLACK, Lawrence, A. ,  CHANG, Sou-jen ,  COWART, Marlon, D. ,  FAGHIH, Ramin ,  GFESSER, Gregory, A. ,  KU, Yi-yin ,  LIU, Huaqing ,  LUKIN, Kirill, A. ,  NERSESIAN, Diana, L. ,  PU, Yu-ming ,  CURTIS, Michael, P.

IPC: C07D417/14 ,  C07D401/04 ,  C07D417/04 ,  C07D413/04 ,  C07D409/14 ,  C07D413/14 ,  C07D215/12 ,  C07D401/14 ,  A61K31/4709 ,  A61P25/28 ,  A61P25/00

CPC classification number: C07D215/12 ,  C07D401/04 ,  C07D401/08 ,  C07D401/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

Abstract: Compounds of formula (I) wherein R1 or R2 is an aromatic or non-aromatic ring directly joined or joined by a linker, as represented by L2 and L3, to a heteroaromatic core, and X, X', Y, Y', Z, Z', R1, R2, R3, R3a, R3b, R4, R5, L, L2, and L3 are as defined herein, are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).

公开(公告)号：EP1124804B1

公开(公告)日：2005-08-24

申请号：EP99953259.1

申请日：1999-10-27

Applicant: ABBOTT LABORATORIES

Inventor： BLACK, Lawrence, A. ,  BASHA, Anwer ,  KOLASA, Teodozyj ,  KORT, Michael, E. ,  LIU, Huaqing ,  MCCARTY, Catherine, M. ,  PATEL, Meena, V. ,  ROHDE, Jeffrey, J. ,  COGHLAN, Michael, J. ,  STEWART, Andrew, O.

IPC: C07D237/14 ,  A61K31/50 ,  C07D405/04 ,  C07D409/04

CPC classification number: C07D405/04 ,  C07D237/14 ,  C07D409/04

Abstract: The present invention describes pyridazinone compounds of formula (I) which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2). COX-2 is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1) which is an important 'housekeeping' enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectively of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently marketed non-steroidal anti-inflammatory drugs (NSAIDs).