公开(公告)号：WO2005100377A1

公开(公告)日：2005-10-27

申请号：PCT/US2005/014019

申请日：2005-04-06

Applicant: ABBOTT LABORATORIES ,  ZHAO, Chen ,  SUN, Minghua ,  COWART, Marlon, D. ,  BENNANI, Youssef, L.

Inventor： ZHAO, Chen ,  SUN, Minghua ,  COWART, Marlon, D. ,  BENNANI, Youssef, L.

IPC: C07J71/00

CPC classification number: C07J71/0042

Abstract: Azacyclosteroid histamine-3 receptor ligands, pharmaceutical compositions comprising such compounds, and methods for using such compounds and compositions are described herein.

Abstract translation: 氮杂环绕组胺胺受体配体，包含这些化合物的药物组合物和使用这些化合物和组合物的方法在本文中描述。

公开(公告)号：WO2004024707A2

公开(公告)日：2004-03-25

申请号：PCT/US2003/028396

申请日：2003-09-10

Applicant: ABBOTT LABORATORIES

Inventor： KU, Yi-Yin ,  PU, Yu-Ming ,  COWART, Marlon, D. ,  GRIEME, Timothy, A. ,  GUPTA, Ashok, K. ,  PLATA, Daniel, J.

IPC: C07D307/81

CPC classification number: C07D405/04 ,  C07C253/30 ,  C07C255/53 ,  C07D307/81

Abstract: The present invention relates to processes for preparing amine substituted benzofurans, and more particularly 4-(2-{2-[(2R)-2-methyl-1-pyrrolidinyl]ethyl}-1-benzofuran-5-yl)benzonitrile, and salts thereof. Compounds prepared by the processes of the invention have demonstrated activity as histamine-3 receptor ligands.

Abstract translation: 本发明涉及制备胺取代的苯并呋喃的方法，特别是4-（2- {2 - [（2R）-2-甲基-1-吡咯烷基]乙基} -1-苯并呋喃-5-基）苄腈，和 的盐。 通过本发明方法制备的化合物已经证明作为组胺-3受体配体的活性。

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：WO2007100990A3

公开(公告)日：2007-09-07

申请号：PCT/US2007/062329

申请日：2007-02-16

Applicant: ABBOTT LABORATORIES ,  COWART, Marlon, D. ,  ZHAO, Chen ,  SUN, Minghua ,  BLACK, Lawrence, A. ,  ZHENG, Guo Zhu ,  GREGG, Robert, J. ,  ZHANG, Geoff, G.Z. ,  SHEIKH, Ahmad, Y. ,  LOU, Xiaochun ,  HENRY, Rodger, F. ,  BARNES, David, M. ,  KOLACZKOWSKI, Lawrence ,  HAIGHT, Anthony, R. ,  CHANG, Sou-Jen ,  WITTENBERGER, Steven, J. ,  FICKES, Michael, G.

Inventor： COWART, Marlon, D. ,  ZHAO, Chen ,  SUN, Minghua ,  BLACK, Lawrence, A. ,  ZHENG, Guo Zhu ,  GREGG, Robert, J. ,  ZHANG, Geoff, G.Z. ,  SHEIKH, Ahmad, Y. ,  LOU, Xiaochun ,  HENRY, Rodger, F. ,  BARNES, David, M. ,  KOLACZKOWSKI, Lawrence ,  HAIGHT, Anthony, R. ,  CHANG, Sou-Jen ,  WITTENBERGER, Steven, J. ,  FICKES, Michael, G.

IPC: C07D487/04 ,  A61K31/407

Abstract: Octahydro-pyrrolo[3,4-b]pyrrole derivatives or a pharmaceutically acceptable salt, ester, amide, prodrug, or radiolabeled form thereof, wherein R 1 is alkyl, C 3 -C 5 cycloalkyl. or (C 3 -C 5 cycloalkyl)methyl; R 2a , R 2b , R 2c , R 2d , R 2e , and R 2f each are independently hydrogen, methyl, or fluoromethyl; R 3a , R 3b , R 3c , and R 3d each are independently hydrogen, alkyl, fluoroalkyl, fluoroalkoxy, alkoxy, thioalkoxy, halogen, or nitrile, with the proviso that when one or more of R 3a , R 3b , R 3c , and R 3d are alkyl, then at least one of R 3a , R 3b , R 3c , and R 3d is fluoroalkyl, fluoroalkoxy, alkoxy, thioalkoxy, halogen, or nitrile; L 1 is a bond, oxygen, sulfur, carbonyl, alkylene,. alkylcarbonyl, alkylamino, -C(=N-Oalkyl)-, NR 4 , -C(=O) NR 4 -, or -NR4C(=O)-; R 4 is hydrogen or alkyl; Cy 1 is aryl, cycloalkyl, cycloalkenyl, heteroaryl, or heterocycle; Z is a substituent R 6 or a group represented by -L 3 -Cy 3 ; R 6 is hydrogen, acyl, acyloxy, alkenyl, alkoxy, alkoxyalkoxy, alkoxyalkyl, alkoxycarbonyl, alkoxyimino, alkoxysulfonyl, alkyl, alkylcarbonyl, alkylsulfonyl, alkynyl, amido, carboxy, cyano, cycloalkyl, fiuoroalkoxy, haloalkoxy, haloalkyl, halogen, hydroxy, hydroxyalkyl, mercapto, nitro, alkylthio, amino, NHR 7 , NR 7 R 8 , -N(R 7 )C(=O)R 9 , -C(=O)NR 7 R 8 , or N(R 7 )SO 2 (R 10 ); L 3 is a bond, oxygen, sulfur, carbonyl, alkylene, alkylcarbonyl, alkylamino, -C(=N-Oalkyl)-, NR 11 , -C(=O) NR 11 -, or -NR 11 C(=O)-;Cy 3 is aryl, cycloalkyl, cycloalkenyl, heteroaryl, or heterocycle; R 7 , R 8 , R 9 , R 10 , and R 11 at each occurrence are independently hydrogen,C 1-4 alkyl, C 3 -C 4 cycloalkyl, or a (C 3 -C 4 cycloalkyl)amine; are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.

公开(公告)号：WO2003101994A1

公开(公告)日：2003-12-11

申请号：PCT/US2003/016878

申请日：2003-05-29

Applicant: ABBOTT LABORATORIES

Inventor： COWART, Marlon, D.

IPC: C07D491/04

CPC classification number: C07D471/04 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04

Abstract: The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.

Abstract translation: 本发明涉及式（I）化合物用于治疗性功能障碍的用途，以及含有式（I）化合物用于治疗性功能障碍的组合物的用途。

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：WO2007038074A1

公开(公告)日：2007-04-05

申请号：PCT/US2006/036422

申请日：2006-09-19

Applicant: ABBOTT LABORATORIES ,  COWART, Marlon, D. ,  SUN, Minghua ,  ZHAO, Chen ,  ZHENG, Guo Zhu

Inventor： COWART, Marlon, D. ,  SUN, Minghua ,  ZHAO, Chen ,  ZHENG, Guo Zhu

IPC: C07D417/04 ,  C07D417/08 ,  C07D417/12 ,  C07D277/64 ,  C07D487/04 ,  A61K31/428 ,  A61K51/04 ,  A61P9/10

CPC classification number: C07D277/64 ,  C07D417/04 ,  C07D417/08 ,  C07D417/12 ,  C07D487/04

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：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。

公开(公告)号：WO2010129242A3

公开(公告)日：2010-11-11

申请号：PCT/US2010/032488

申请日：2010-04-27

Applicant: ABBOTT LABORATORIES ,  COWART, Marlon, D. ,  HSIEH, Gin, C. ,  BRIONI, Jorge, D. ,  SULLIVAN, James, P.

Inventor： COWART, Marlon, D. ,  HSIEH, Gin, C. ,  BRIONI, Jorge, D. ,  SULLIVAN, James, P.

IPC: A61K31/395 ,  A61K31/41 ,  A61P29/00

Abstract: This invention discloses a method of treatment of osteoarthritis pain by administration of a histamine H 3 receptor antagonist, described herein, a salt thereof, or a composition comprising such compound or salt.

Abstract translation: 本发明公开了一种通过施用本文所述的组胺H 3 N受体拮抗剂，其盐或包含该化合物或盐的组合物治疗骨关节炎疼痛的方法

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。