公开(公告)号：WO2011008312A2

公开(公告)日：2011-01-20

申请号：PCT/US2010/027931

申请日：2010-03-19

Applicant: ABBOTT LABORATORIES ,  SCHRIMPF, Michael R. ,  LEE, Chih-Hung ,  LI, Tao ,  GFESSER, Gregory A. ,  MORTELL, Kathleen H. ,  FAGHIH, Ramin ,  NERSESIAN, Diana L. ,  SIPPY, Kevin B. ,  BUNNELLE, William H. ,  SCANIO, Marc ,  SHI, Lei ,  GOPALAKRISHNAN, Murali ,  DONNELLY-ROBERTS, Diana L. ,  HU, Min

Inventor： SCHRIMPF, Michael R. ,  LEE, Chih-Hung ,  LI, Tao ,  GFESSER, Gregory A. ,  MORTELL, Kathleen H. ,  FAGHIH, Ramin ,  NERSESIAN, Diana L. ,  SIPPY, Kevin B. ,  BUNNELLE, William H. ,  SCANIO, Marc ,  SHI, Lei ,  GOPALAKRISHNAN, Murali ,  DONNELLY-ROBERTS, Diana L. ,  HU, Min

IPC: C07D487/18

CPC classification number: C07D471/18 ,  C07D487/18

Abstract: The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI) wherein a , R 1 , R 2 , R 3 , R 4 , R 5 , U, V, W, X, Y, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.

Abstract translation: 本申请涉及式（I），（II），（III），（IV），（V）或（VI）的吲哚和吲哚啉衍生物， R 1，R 2，R 3，R 4，R 5，R 5，R 5，R 4， U，V，W，X，Y和Z如说明书中所定义。 本申请还涉及包含此类化合物的组合物，以及使用此类化合物和组合物治疗疾病状况的方法以及鉴定此类化合物的方法。

公开(公告)号：WO2009149135A1

公开(公告)日：2009-12-10

申请号：PCT/US2009/046042

申请日：2009-06-03

Applicant: ABBOTT LABORATORIES ,  GOPALAKRISHNAN, Murali ,  JI, Jianguo ,  LEE, Chih-Hung ,  LI, Tao ,  SIPPY, Kevin, B.

Inventor： GOPALAKRISHNAN, Murali ,  JI, Jianguo ,  LEE, Chih-Hung ,  LI, Tao ,  SIPPY, Kevin, B.

IPC: C07D413/04 ,  C07D413/14 ,  A61K31/42 ,  A61P25/28

CPC classification number: C07D413/14 ,  C07D413/04

Abstract: The invention relates to isoxazole derivatives of formila (I), compositions comprising such compounds, and methods of preventing or treating conditions and disorders using such compounds and compositions.

Abstract translation: 本发明涉及甲醛（I）的异恶唑衍生物，包含这些化合物的组合物，以及使用这些化合物和组合物预防或治疗病症和障碍的方法。

公开(公告)号：WO2005066167A3

公开(公告)日：2005-07-21

申请号：PCT/US2004/041367

申请日：2004-12-10

Applicant: ABBOTT LABORATORIES ,  JI, Jianguo ,  LI, Tao

Inventor： JI, Jianguo ,  LI, Tao

IPC: C07D453/00

Abstract: Compounds of formula (I) or (II) , or pharmaceutically acceptable salts, esters, amides, or prodrugs thereof, wherein: A and G are each independently N or N + -O - ; m and n are each independently 0, 1, or 2; X 1 and X 3 are each independently O, S, and -N(R 1 )-; X 2 is O, S, -N(R 1 )-, -N(Ar 2 )-, and -N(R 2 )C(O)-; Ar 1 is a six-membered aromatic ring; Ar 2 is cyclohexyl or a mono- or bicyclic aromatic ring, and R 13 is hydrogen, alkyl, or halogen, as defined herein. The compounds are useful in treating conditions or disorders prevented by or ameliorated by nAChR ligands. Also disclosed are pharmaceutical compositions having compounds of formulas (I) and (II) and methods for using such compounds and compositions.

公开(公告)号：WO2011084433A2

公开(公告)日：2011-07-14

申请号：PCT/US2010/060343

申请日：2010-12-14

Applicant: ABBOTT LABORATORIES ,  SHI, Lei ,  BUNNELLE, William H. ,  LI, Tao ,  SCANIO, Marc J. ,  SCHRIMPF, Michael R. ,  LEE, CHIH-Hung

Inventor： SHI, Lei ,  BUNNELLE, William H. ,  LI, Tao ,  SCANIO, Marc J. ,  SCHRIMPF, Michael R. ,  LEE, CHIH-Hung

IPC: C07D471/18 ,  C07D487/18 ,  A61K31/407 ,  A61K31/439 ,  A61P25/28 ,  A61P25/18

CPC classification number: C07D471/18 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/4709 ,  C07D487/08

Abstract: The present application relates to indole and indoline derivatives of formula (I) wherein a, R 1 , R 2 , R 3 , h, i, j, m, n, L, Q, and X are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions.

Abstract translation: 本发明涉及式（I）的吲哚和二氢吲哚衍生物，其中a，R1，R2，R3，h，i，j，m，n，L，Q和X如说明书中所定义。 本申请还涉及包含这些化合物的组合物，以及使用这些化合物和组合物治疗疾病状况的方法。

公开(公告)号：WO2008073942A2

公开(公告)日：2008-06-19

申请号：PCT/US2007/087090

申请日：2007-12-12

Applicant: ABBOTT LABORATORIES ,  GOPALAKRISHNAN, Murali ,  HONORE, Marie, P. ,  LEE, Chih-hung ,  MALYSZ, John ,  JI, Jianguo ,  LI, Tao ,  SCHRIMPF, Michael, R. ,  SIPPY, Kevin, B. ,  ANDERSON, David, J.

Inventor： GOPALAKRISHNAN, Murali ,  HONORE, Marie, P. ,  LEE, Chih-hung ,  MALYSZ, John ,  JI, Jianguo ,  LI, Tao ,  SCHRIMPF, Michael, R. ,  SIPPY, Kevin, B. ,  ANDERSON, David, J.

IPC: A61K31/4245 ,  A61P25/28 ,  A61K45/06

CPC classification number: A61K31/4439 ,  A61K31/4245 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/444 ,  A61K31/4709 ,  A61K45/06 ,  C07D413/04 ,  C07D413/14 ,  G01N33/944 ,  G01N2333/70571 ,  A61K2300/00

Abstract: The invention relates to a composition comprising a neuronal nicotinic receptor ligand and an α4β2 positive allosteric modulator, a method of using the same, and a related article of manufacture.

Abstract translation: 本发明涉及包含神经元烟碱性受体配体和a4β2正变构调节剂的组合物，其使用方法和相关制品。

公开(公告)号：WO2007018738A2

公开(公告)日：2007-02-15

申请号：PCT/US2006/023091

申请日：2006-06-14

Applicant: ABBOTT LABORATORIES ,  JI, Jianguo ,  LI, Tao ,  MORTELL, Kathleen, H. ,  SCHRIMPF, Michael, R. ,  NERSESIAN, Diana, L. ,  PAN, Liping ,  BUNNELLE, William, H.

Inventor： JI, Jianguo ,  LI, Tao ,  MORTELL, Kathleen, H. ,  SCHRIMPF, Michael, R. ,  NERSESIAN, Diana, L. ,  PAN, Liping ,  BUNNELLE, William, H.

IPC: C07D453/02 ,  A61P25/28 ,  A61K31/439

CPC classification number: C07D453/02

Abstract: Compounds of formula (I) wherein n is 0, 1, or 2; A is N or N + -O - ; X is O, S, -NH-, and -N-alkyl-; Ar 1 is a 6-membered aromatic ring; and Ar 2 is a fused bicycloheterocycle. The compounds are useful in treating conditions or disorders prevented by or ameliorated by α7 nAChR ligands. Also disclosed are pharmaceutical compositions having compounds of formula (I) and methods for using such compounds and compositions.

Abstract translation: 其中n是0,1或2的式（I）化合物; A是N或N ^{+ < - > - - ; X是O，S，-NH-和-N-烷基 - ; Ar 1是6元芳族环; Ar 2是稠合双环杂环。 该化合物可用于治疗由α7nAChR配体阻止或改善的病症或障碍。 还公开了具有式（I）化合物的药物组合物和使用该化合物和组合物的方法。}

公开(公告)号：WO2011075487A1

公开(公告)日：2011-06-23

申请号：PCT/US2010/060346

申请日：2010-12-14

Applicant: ABBOTT LABORATORIES ,  SHI, Lei ,  BUNNELLE, William H. ,  LI, Tao ,  SCANIO, Marc J. ,  SCHRIMPF, Michael R. ,  LEE, CHIH-Hung

Inventor： SHI, Lei ,  BUNNELLE, William H. ,  LI, Tao ,  SCANIO, Marc J. ,  SCHRIMPF, Michael R. ,  LEE, CHIH-Hung

IPC: C07D471/18 ,  C07D487/18 ,  A61K31/407 ,  A61P25/28

CPC classification number: C07D471/18 ,  C07D487/18

Abstract: The present application relates to indole and indoline derivatives of formula (I), formula (II), formula (III), or formula (IV) wherein a, R 2 , R 3 , h, k, m, n, L, Q, X, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and their medicaments for treating neurodegeneration and neuropsychiatric disorders.

Abstract translation: 本申请涉及式（I），式（II），式（III）或式（IV）的吲哚和二氢吲哚衍生物，其中a，R2，R3，h，k，m，n，L，Q，X ，Z如说明书中所定义。 本申请还涉及包含这些化合物的组合物及其用于治疗神经变性和神经精神障碍的药物。

公开(公告)号：WO2010138600A2

公开(公告)日：2010-12-02

申请号：PCT/US2010/036213

申请日：2010-05-26

Applicant: ABBOTT LABORATORIES ,  JI, Jianguo ,  LEE, Chih-Lung ,  SIPPY, Kevin, B. ,  LI, Tao ,  GOPALAKRISHNAN, Murali

Inventor： JI, Jianguo ,  LEE, Chih-Lung ,  SIPPY, Kevin, B. ,  LI, Tao ,  GOPALAKRISHNAN, Murali

IPC: A61K45/06 ,  A61P29/00 ,  A61P25/04 ,  A61K31/4245 ,  A61K31/4427

CPC classification number: A61K45/06 ,  A61K31/4245 ,  A61K31/4427 ,  A61K2300/00

Abstract: This invention discloses a method of treatment of osteoarthritis pain by administration of a composition containing a nicotinic acetylcholine receptor ligand and a nicotinic acetylcholine receptor subtype 4 2 allosteric modulator. The present application also relates to compositions comprising such compounds for use in treating pain and related disorders mediated by controlling neurotransmitter release in a subject.

Abstract translation: 本发明公开了一种通过施用含有烟碱型乙酰胆碱受体配体和烟碱型乙酰胆碱受体亚型4 2变构调节剂的组合物来治疗骨关节炎疼痛的方法。 本申请还涉及包含用于治疗疼痛和通过控制受试者中的神经递质释放介导的相关病症的化合物的组合物。

公开(公告)号：WO2006065233A1

公开(公告)日：2006-06-22

申请号：PCT/US2004/041471

申请日：2004-12-10

Applicant: ABBOTT LABORATORIES ,  JI, Jianguo ,  LI, Tao ,  MORTELL, Kathleen, H. ,  SCHRIMPF, Michael, R. ,  NERSESIAN, Diana, L. ,  PAN, Liping

Inventor： JI, Jianguo ,  LI, Tao ,  MORTELL, Kathleen, H. ,  SCHRIMPF, Michael, R. ,  NERSESIAN, Diana, L. ,  PAN, Liping

IPC: C07D453/02 ,  A61K31/439 ,  A61P25/28

CPC classification number: C07D453/02

Abstract: Compounds of formula (I) wherein n is 0, 1, or 2; A is N or N+-O-; X is O, S, -NH-, and -N-alkyl-; Ar1 is a 6-membered aromatic ring; and Ar2 is a fused bicycloheterocycle. The compounds are useful in treating conditions or disorders prevented by or ameliorated by a7 nAChR ligands. Also disclosed are pharmaceutical compositions having compounds of formula (I) and methods for using such compounds and compositions.

Abstract translation: 其中n为0,1或2的式（I）化合物; A是N或N + -O-; X是O，S，-NH-和-N-烷基 - ; Ar1是6元芳环; 并且Ar 2是稠合的双环杂环。 该化合物可用于治疗由α7nAChR配体预防或改善的病症或病症。 还公开了具有式（I）化合物的药物组合物和使用这些化合物和组合物的方法。

公开(公告)号：WO2005077899A2

公开(公告)日：2005-08-25

申请号：PCT/US2005/003578

申请日：2005-02-04

Applicant: ABBOTT LABORATORIES ,  SCHRIMPF, Michael, R. ,  SIPPY, Kevin, B. ,  JI, Jianguo ,  LI, Tao ,  PACE, Jennifer, M. ,  BRIGGS, Clark, A. ,  BUNELLE, William, H.

Inventor： SCHRIMPF, Michael, R. ,  SIPPY, Kevin, B. ,  JI, Jianguo ,  LI, Tao ,  PACE, Jennifer, M. ,  BRIGGS, Clark, A. ,  BUNELLE, William, H.

IPC: C07D207/08

CPC classification number: C07D207/08 ,  C07C211/31 ,  C07C217/24 ,  C07C2603/18 ,  C07C2603/26 ,  C07D205/04 ,  C07D207/12 ,  C07D207/14 ,  C07D209/88 ,  C07D211/22 ,  C07D211/46 ,  C07D243/08 ,  C07D295/104 ,  C07D307/91 ,  C07D311/86 ,  C07D333/76 ,  C07D451/06 ,  C07D453/02 ,  C07D487/04 ,  C07D487/08

Abstract: Compounds of formula (I) wherein A and B are amine-substituted sidechains, Y 1 and Y 2 form various tricyclic cores, X a and X b are C, CH, or N, as defined herein, and R x is an optional substituent. Compounds and compositions of formula (I) are contemplated as well as methods for treating conditions or disorders prevented by or ameliorated by α7 nAChR ligands that encompass compounds of formula (I) and other tricyclic derivatives. Methods of using amino-substituted tricyclic derivatives also are described herein.

Abstract translation: 其中A和B是胺取代的侧链，Y 1和Y 2形成各种三环核心的式（I）化合物， 如本文所定义，X和X是C，CH或N，并且R X是任选的取代基。 考虑式（I）化合物和组合物以及用于治疗由包含式（I）化合物和其他三环衍生物的α7nAChR配体阻止或改善的病症或障碍的方法。 本文还描述了使用氨基取代的三环衍生物的方法。