公开(公告)号：WO2004037241A1

公开(公告)日：2004-05-06

申请号：PCT/US2003/033426

申请日：2003-10-22

Applicant: ABBOTT LABORATORIES

Inventor： BENNANI, Youssef, L. ,  CHANG, Sou-Jen ,  CHEMBURKAR, Sanjay, R. ,  DART, Michael, J. ,  FERNANADO, Dilinie, P. ,  GRIEME, Timothy, A.

IPC: A61K31/19

CPC classification number: A61K31/55 ,  A61K31/33 ,  A61K31/397 ,  A61K31/401 ,  A61K31/495 ,  A61K31/537 ,  A61K31/54 ,  C07C61/13 ,  C07C61/135 ,  C07C61/29 ,  C07C69/753 ,  C07C233/58 ,  C07C237/22 ,  C07C2602/18 ,  C07C2602/20 ,  C07C2602/22 ,  C07C2602/24 ,  C07C2603/08 ,  C07C2603/12 ,  C07C2603/62 ,  C07C2603/66

Abstract: The present invention relates to the use of compounds of formula (I) for the treatment of epilepsy, bipolar disorder, psychiatric disorders, migraine, pain, or movement disorders, and to provide neuroprotection.

Abstract translation: 本发明涉及式（I）化合物用于治疗癫痫，双相情感障碍，精神障碍，偏头痛，疼痛或运动障碍的用途，并提供神经保护作用。

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：WO2004101559A1

公开(公告)日：2004-11-25

申请号：PCT/US2004/013606

申请日：2004-05-03

Applicant: ABBOTT LABORATORIES ,  COWART, Marlon, D. ,  KU, Yin-Yin ,  CHANG, Sou-Jen ,  FERNANDO, Dilinie, P. ,  GRIEME, Timothy, A. ,  ALTENBACH, Robert, A.

Inventor： COWART, Marlon, D. ,  KU, Yin-Yin ,  CHANG, Sou-Jen ,  FERNANDO, Dilinie, P. ,  GRIEME, Timothy, A. ,  ALTENBACH, Robert, A.

IPC: C07D417/04

CPC classification number: C07D263/56 ,  C07D209/14 ,  C07D235/14 ,  C07D277/64 ,  C07D279/16 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D413/06 ,  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 comprising the histamine-3 receptor ligands and methods for using such compounds and compositions. X is O, S, NH, or N(alkyl); Y, and Y’ are each independently selected from the group consisting of CH, CF, and N; Z is C or N, provided that when X is O or S, Z is N; one of R 1 and R 2 is selected from the group consisting of aryl, heteroaryl, and heterocycle; the other of R 1 and R 2 is selected from the group consisting of hydrogen, alkyl, alkoxy, aryl, cycloalkyl, halo, cyano, and thioalkoxy; R 3 is absent when Z is N and, when present, R 3 is selected from the group consisting of hydrogen, methyl, alkoxy, halo and cyano; R 4 and R 5 are each independently selected from the group consisting of alkyl, haloalkyl, hydroxyalkyl, alkoxyalkyl, cycloalkyl, and cycloalkylalkyl, or R 4 and R 5 taken together with the nitrogen atom to which each is attached form a non-aromatic ring L is -[C(R 15 )(R 16 )]n-; m is an integer from 0-3; and n is an integer from 2-3.

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和使用这些化合物和组合物的方法。 X是O，S，NH或N（烷基）; Y和Y'各自独立地选自CH，CF和N; Z为C或N，条件是当X为O或S时，Z为N; R 1和R 2之一选自芳基，杂芳基和杂环; R 1和R 2中的另一个选自氢，烷基，烷氧基，芳基，环烷基，卤素，氰基和硫代烷氧基; 当Z为N时，R3不存在，并且当存在时，R 3选自氢，甲基，烷氧基，卤素和氰基; R 4和R 5各自独立地选自烷基，卤代烷基，羟烷基，烷氧基烷基，环烷基和环烷基烷基，或者R 4和R 5与各自连接的氮原子一起形成非芳香环L是 - C（R15）（R16）] N-; m是0-3的整数; n为2-3的整数。

公开(公告)号：WO2003027117A1

公开(公告)日：2003-04-03

申请号：PCT/US2002/028864

申请日：2002-09-11

Applicant: ABBOTT LABORATORIES

Inventor： KU, Yi-Yin ,  GRIEME, Timothy, A. ,  SHARMA, Padam, N. ,  RAJE, Prasad, S. ,  FITZGERALD, Mike, A. ,  MORTON, Howard, E.

IPC: C07D491/04

CPC classification number: C07D491/04

Abstract: The present invention relates to an efficient process for the preparation of 5-(substituted)-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-chromeno[3,4-f]quinolines.

Abstract translation: 本发明涉及制备5-（取代的）-10-甲氧基-2,2,4-三甲基-2,5-二氢-1H-色烯并[3,4-f]喹啉的有效方法。

公开(公告)号：EP1620434B1

公开(公告)日：2011-03-09

申请号：EP04751135.7

申请日：2004-05-03

Applicant: ABBOTT LABORATORIES

Inventor： COWART, Marlon, D. ,  KU, Yin-Yin ,  CHANG, Sou-Jen ,  FERNANDO, Dilinie, P. ,  GRIEME, Timothy, A. ,  ALTENBACH, Robert, A.

IPC: C07D417/04 ,  C07D417/06 ,  C07D417/14 ,  C07D403/06 ,  C07D413/06 ,  A61P25/00 ,  A61K31/425 ,  A61K31/404 ,  A61K31/423

CPC classification number: C07D263/56 ,  C07D209/14 ,  C07D235/14 ,  C07D277/64 ,  C07D279/16 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D413/06 ,  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 comprising the histamine-3 receptor ligands and methods for using such compounds and compositions. X is O, S, NH, or N(alkyl); Y, and Y’ are each independently selected from the group consisting of CH, CF, and N; Z is C or N, provided that when X is O or S, Z is N; one of R1 and R2 is selected from the group consisting of aryl, heteroaryl, and heterocycle; the other of R1 and R2 is selected from the group consisting of hydrogen, alkyl, alkoxy, aryl, cycloalkyl, halo, cyano, and thioalkoxy; R3 is absent when Z is N and, when present, R3 is selected from the group consisting of hydrogen, methyl, alkoxy, halo and cyano; R4 and R5 are each independently selected from the group consisting of alkyl, haloalkyl, hydroxyalkyl, alkoxyalkyl, cycloalkyl, and cycloalkylalkyl, or R4 and R5 taken together with the nitrogen atom to which each is attached form a non-aromatic ring L is -[C(R15)(R16)]n-; m is an integer from 0-3; and n is an integer from 2-3.

公开(公告)号：EP1562575B1

公开(公告)日：2009-05-20

申请号：EP03777773.7

申请日：2003-10-22

Applicant: ABBOTT LABORATORIES

Inventor： BENNANI, Youssef, L. ,  CHANG, Sou-Jen ,  CHEMBURKAR, Sanjay, R. ,  DART, Michael, J. ,  FERNANADO, Dilinie, P. ,  GRIEME, Timothy, A.

IPC: A61K31/19 ,  A61P25/08 ,  C07C61/135 ,  C07C69/753 ,  C07C233/58 ,  C07C237/24 ,  C07C61/13

CPC classification number: A61K31/55 ,  A61K31/33 ,  A61K31/397 ,  A61K31/401 ,  A61K31/495 ,  A61K31/537 ,  A61K31/54 ,  C07C61/13 ,  C07C61/135 ,  C07C61/29 ,  C07C69/753 ,  C07C233/58 ,  C07C237/22 ,  C07C2602/18 ,  C07C2602/20 ,  C07C2602/22 ,  C07C2602/24 ,  C07C2603/08 ,  C07C2603/12 ,  C07C2603/62 ,  C07C2603/66

Abstract: The present invention relates to the use of compounds of formula (I) for the treatment of epilepsy, bipolar disorder, psychiatric disorders, migraine, pain, or movement disorders, and to provide neuroprotection.

Abstract translation: 本发明涉及使用式（I），用于癫痫，双相性精神障碍，精神障碍，偏头痛，疼痛，或运动障碍的治疗中的化合物，并提供神经保护。

公开(公告)号：EP1620434A1

公开(公告)日：2006-02-01

申请号：EP04751135.7

申请日：2004-05-03

Applicant: ABBOTT LABORATORIES

Inventor： COWART, Marlon, D. ,  KU, Yin-Yin ,  CHANG, Sou-Jen ,  FERNANDO, Dilinie, P. ,  GRIEME, Timothy, A. ,  ALTENBACH, Robert, A.

IPC: C07D417/04 ,  C07D417/06 ,  C07D417/14 ,  C07D403/06 ,  C07D413/06 ,  A61P25/00 ,  A61K31/425 ,  A61K31/404 ,  A61K31/423

CPC classification number: C07D263/56 ,  C07D209/14 ,  C07D235/14 ,  C07D277/64 ,  C07D279/16 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D413/06 ,  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 comprising the histamine-3 receptor ligands and methods for using such compounds and compositions. X is O, S, NH, or N(alkyl); Y, and Y’ are each independently selected from the group consisting of CH, CF, and N; Z is C or N, provided that when X is O or S, Z is N; one of R1 and R2 is selected from the group consisting of aryl, heteroaryl, and heterocycle; the other of R1 and R2 is selected from the group consisting of hydrogen, alkyl, alkoxy, aryl, cycloalkyl, halo, cyano, and thioalkoxy; R3 is absent when Z is N and, when present, R3 is selected from the group consisting of hydrogen, methyl, alkoxy, halo and cyano; R4 and R5 are each independently selected from the group consisting of alkyl, haloalkyl, hydroxyalkyl, alkoxyalkyl, cycloalkyl, and cycloalkylalkyl, or R4 and R5 taken together with the nitrogen atom to which each is attached form a non-aromatic ring L is -[C(R15)(R16)]n-; m is an integer from 0-3; and n is an integer from 2-3.

公开(公告)号：EP1562575A1

公开(公告)日：2005-08-17

申请号：EP03777773.7

申请日：2003-10-22

Applicant: Abbott Laboratories

Inventor： BENNANI, Youssef, L. ,  CHANG, Sou-Jen ,  CHEMBURKAR, Sanjay, R. ,  DART, Michael, J. ,  FERNANADO, Dilinie, P. ,  GRIEME, Timothy, A.

IPC: A61K31/19 ,  A61P25/08 ,  C07C61/135 ,  C07C69/753 ,  C07C233/58 ,  C07C237/24 ,  C07C61/13

CPC classification number: A61K31/55 ,  A61K31/33 ,  A61K31/397 ,  A61K31/401 ,  A61K31/495 ,  A61K31/537 ,  A61K31/54 ,  C07C61/13 ,  C07C61/135 ,  C07C61/29 ,  C07C69/753 ,  C07C233/58 ,  C07C237/22 ,  C07C2602/18 ,  C07C2602/20 ,  C07C2602/22 ,  C07C2602/24 ,  C07C2603/08 ,  C07C2603/12 ,  C07C2603/62 ,  C07C2603/66

Abstract: The present invention relates to the use of compounds of formula (I) for the treatment of epilepsy, bipolar disorder, psychiatric disorders, migraine, pain, or movement disorders, and to provide neuroprotection.