公开(公告)号：WO2005113551A1

公开(公告)日：2005-12-01

申请号：PCT/US2005/014863

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: C07D417/14

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 R 1 or R 2 is an aromatic or non-aromatic ring directly joined or joined by a linker, as represented by L 2 and L 3 , to a heteroaromatic core, and X, X', Y, Y', Z, Z', R 1 , R 2 , R 3 , R 3a , R 3b , R 4 , R 5 , L, L 2 , and L 3 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）的化合物，其中R 1或R 2是通过由L 2和L 3表示的连接基直接连接或连接到杂芳族核心上的芳族或非芳族环，X，X'，Y，Y'，Z ，Z'，R1，R2，R3，R3a，R3b，R4，R5，L，L2和L3如本文所定义，可用于治疗组胺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：WO2004043458A1

公开(公告)日：2004-05-27

申请号：PCT/US2003/035365

申请日：2003-11-05

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 ,  SHARMA, Padam, N. ,  BENNANI, Youssef, L. ,  CURTIS, Michael, P.

IPC: A61K31/40

CPC classification number: C07C255/58 ,  C07D207/08 ,  C07D207/12 ,  C07D207/14 ,  C07D207/20 ,  C07D213/30 ,  C07D213/38 ,  C07D213/61 ,  C07D213/64 ,  C07D213/85 ,  C07D215/12 ,  C07D215/14 ,  C07D215/20 ,  C07D217/14 ,  C07D237/12 ,  C07D237/14 ,  C07D237/28 ,  C07D239/26 ,  C07D239/28 ,  C07D239/42 ,  C07D239/52 ,  C07D241/12 ,  C07D241/42 ,  C07D263/32 ,  C07D277/28 ,  C07D295/073 ,  C07D295/088 ,  C07D295/096 ,  C07D295/112 ,  C07D295/135 ,  C07D295/155 ,  C07D401/04 ,  C07D401/10 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04

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：WO2009137492A1

公开(公告)日：2009-11-12

申请号：PCT/US2009/042860

申请日：2009-05-05

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: C07D495/04 ,  C07D498/04 ,  A61K31/519 ,  A61P29/00

CPC classification number: C07D498/04 ,  C07D495/04

Abstract: Heteroaryl-fused macrocyclic 2,4-diaminopyrimidine compounds of formula (I) wherein W, G 1 , G 2 , A 1 and R 1 are defined in the description, 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.

Abstract translation: 其中W，G1，G2，A1和R1在说明书中定义的式（I）的杂芳基稠合的大环2,4-二氨基嘧啶化合物，包含这些化合物的组合物，制备该化合物的方法，以及治疗和预防进展的方法 使用这些化合物和组合物的疾病，病症和病症在本文中描述。

公开(公告)号：WO2009079225A1

公开(公告)日：2009-06-25

申请号：PCT/US2008/085622

申请日：2008-12-05

Applicant: ABBOTT LABORATORIES ,  LIU, Huaqing ,  BLACK, Lawrence A. ,  BENNANI, Youssef L. ,  COWART, Marlon D. ,  TIAN, Zhenping ,  BRACKEMEYER, Paul J.

Inventor： LIU, Huaqing ,  BLACK, Lawrence A. ,  BENNANI, Youssef L. ,  COWART, Marlon D. ,  TIAN, Zhenping ,  BRACKEMEYER, Paul J.

IPC: C07D295/14 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  A61K31/40 ,  A61K31/41 ,  A61K31/44 ,  A61P25/00

CPC classification number: C07D401/12 ,  C07D207/06 ,  C07D207/08 ,  C07D207/12 ,  C07D213/82 ,  C07D295/14 ,  C07D295/155 ,  C07D401/10 ,  C07D403/10 ,  C07D403/12 ,  C07D417/10 ,  C07D417/12 ,  C07D495/04

Abstract: Compounds of formula (I) wherein R 1 , R 2 , R 3 , R 3a , R 3b , R 4 , and R 5 are defined in the description, 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: 其中R1，R2，R3，R3a，R3b，R4和R5在说明书中定义的式（I）化合物可用于治疗组胺-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：WO2009036132A1

公开(公告)日：2009-03-19

申请号：PCT/US2008/075967

申请日：2008-09-11

Applicant: ABBOTT LABORATORIES ,  COWART, Marlon D ,  MARSH, Kennan C ,  LIU, Huaqing ,  LEE, Jae Yo ,  BECONI, Maria G ,  WETTER, Jill M ,  BLACK, Lawrence A ,  CUSTER, Thomas C

Inventor： COWART, Marlon D ,  MARSH, Kennan C ,  LIU, Huaqing ,  LEE, Jae Yo ,  BECONI, Maria G ,  WETTER, Jill M ,  BLACK, Lawrence A ,  CUSTER, Thomas C

IPC: C07D487/04 ,  A61K31/501 ,  A61P25/00

CPC classification number: C07D487/04

Abstract: The invention relates to octahydro-pyrrolo[3,4-b]pyrrole N-oxides as prodrugs of CNS-active compounds, compositions comprising such compounds, methods for making the compounds, salts, and polymorphs, and methods of treating conditions and disorders using such compounds and compositions. Octahydro-pyrrolo[3,4-b]pyrrole N-oxides of formula (I) are prodrugs of histamine-3 antagonists, and are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole N-oxide compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.

Abstract translation: 本发明涉及作为CNS活性化合物前药的八氢吡咯并[3,4-b]吡咯N-氧化物，包含这些化合物的组合物，制备化合物，盐和多晶型物的方法，以及使用 这些化合物和组合物。 式（I）的八氢 - 吡咯并[3,4-b]吡咯N-氧化物是组胺-3拮抗剂的前药，可用于治疗组胺-3受体配体预防或改善的病症或病症。 八氢吡咯并[3,4-b]吡咯N-氧化物化合物，使用这些化合物的方法，制备它们的组合物，以及这些化合物的制备方法。

公开(公告)号：WO2008060767A3

公开(公告)日：2008-05-22

申请号：PCT/US2007/080133

申请日：2007-10-02

Applicant: ABBOTT LABORATORIES ,  ALTENBACH, Robert J ,  LIU, Huaqing ,  DRIZIN, Irene ,  COWART, Marlon D ,  WISHART, Neil ,  BABINSKI, David J ,  GREGG, Robert J ,  ESBENSHADE, Timothy A ,  HSIEH, Gin C ,  BRIONI, Jorge D ,  HONORE, Marie P ,  BLACK, Lawrence A ,  ZHAO, Chen ,  WAKEFIELD, Brian D.

Inventor： ALTENBACH, Robert J ,  LIU, Huaqing ,  DRIZIN, Irene ,  COWART, Marlon D ,  WISHART, Neil ,  BABINSKI, David J ,  GREGG, Robert J ,  ESBENSHADE, Timothy A ,  HSIEH, Gin C ,  BRIONI, Jorge D ,  HONORE, Marie P ,  BLACK, Lawrence A ,  ZHAO, Chen ,  WAKEFIELD, Brian D.

IPC: C07D491/04 ,  C07D493/04 ,  C07H17/04

Abstract: Macrocyclic benzofused pyrimidine compounds, 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.

公开(公告)号：WO2008060766A2

公开(公告)日：2008-05-22

申请号：PCT/US2007/080132

申请日：2007-10-02

Applicant: ABBOTT LABORATORIES ,  COWART, Marlon D ,  ALTENBACH, Robert J ,  LIU, Huaqing ,  DRIZIN, Irene ,  WISHART, Neil ,  BABINSKI, David J ,  GREGG, Robert J ,  ESBENSHADE, Timothy A ,  HSIEH, Gin C ,  BRIONI, Jorge D ,  HONORE, Marie P ,  BLACK, Lawrence A ,  ZHAO, Chen ,  WAKEFIELD, Brian D

Inventor： ALTENBACH, Robert J ,  LIU, Huaqing ,  DRIZIN, Irene ,  WISHART, Neil ,  BABINSKI, David J ,  GREGG, Robert J ,  ESBENSHADE, Timothy A ,  HSIEH, Gin C ,  BRIONI, Jorge D ,  HONORE, Marie P ,  BLACK, Lawrence A ,  ZHAO, Chen ,  WAKEFIELD, Brian D

CPC classification number: A61K31/506 ,  A61K31/417 ,  A61K31/496 ,  A61K45/06

Abstract: This invention discloses a method of treating pain by administering histamine H 4 receptor ligands and compositions comprising the same.

Abstract translation: 本发明公开了一种通过施用组胺H 4受体配体和包含其的组合物来治疗疼痛的方法。

公开(公告)号：WO2009123967A1

公开(公告)日：2009-10-08

申请号：PCT/US2009/038775

申请日：2009-03-30

Applicant: ABBOTT LABORATORIES ,  LIU, Huaqing ,  DRIZIN, Irene ,  KOENIG, John, R. ,  COWART, Marlon, D. ,  ZHAO, Chen ,  WAKEFIELD, Brian, D. ,  BLACK, Lawrence, A. ,  ALTENBACH, Robert, J.

Inventor： LIU, Huaqing ,  DRIZIN, Irene ,  KOENIG, John, R. ,  COWART, Marlon, D. ,  ZHAO, Chen ,  WAKEFIELD, Brian, D. ,  BLACK, Lawrence, A. ,  ALTENBACH, Robert, J.

IPC: C07D239/84 ,  C07D403/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  A61K31/517 ,  A61P11/06

CPC classification number: C07D401/04 ,  C07D239/70 ,  C07D239/84 ,  C07D239/88 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D453/02 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10

Abstract: Macrocyclic pyrimidine compounds, 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.

Abstract translation: 本文描述了大环嘧啶化合物，包含这些化合物的组合物，制备化合物的方法，以及使用这些化合物和组合物治疗和预防疾病，病症和病症进展的方法。

公开(公告)号：WO2009085945A1

公开(公告)日：2009-07-09

申请号：PCT/US2008/087413

申请日：2008-12-18

Applicant: ABBOTT LABORATORIES ,  BLACK, Lawrence A. ,  COWART, Marlon D. ,  GFESSER, Gregory A. ,  WAKEFIELD, Brian D. ,  ALTENBACH, Robert J. ,  LIU, Huaqing ,  ZHAO, Chen ,  HSIEH, Gin C.

Inventor： BLACK, Lawrence A. ,  COWART, Marlon D. ,  GFESSER, Gregory A. ,  WAKEFIELD, Brian D. ,  ALTENBACH, Robert J. ,  LIU, Huaqing ,  ZHAO, Chen ,  HSIEH, Gin C.

IPC: A61K31/423 ,  A61K31/428 ,  C07D413/14 ,  C07D417/14 ,  A61P25/00 ,  A61P3/10

CPC classification number: C07D417/14 ,  C07D413/04 ,  C07D417/04

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 of compounds of formula (I), methods for using such compounds and compositions, and a process for preparing the compounds.

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。 还公开了式（I）化合物的药物组合物，使用这些化合物和组合物的方法及其制备方法。

公开(公告)号：WO2006132914A2

公开(公告)日：2006-12-14

申请号：PCT/US2006/021257

申请日：2006-06-01

Applicant: ABBOTT LABORATORIES ,  LIU, Huaqing ,  HANCOCK, Arthur, A. ,  COWART, Marlon, D.

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

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。