公开(公告)号：EP1723144B1

公开(公告)日：2010-10-06

申请号：EP05802855.6

申请日：2005-02-15

申请人： AstraZeneca AB

发明人： EDWARDS, Louise ,  ISAAC, Methvin ,  JOHANSSON, Martin ,  KERS, Annika ,  MALMBERG, Johan ,  MCLEOD, Donald ,  MINIDIS, Alexander ,  STAAF, Karin ,  SLASSI, Abdelmalik ,  STEFANAC, Tomislav ,  STORMANN, Thomas ,  WENSBO, David ,  XIN, Tao ,  ARORA, Jalaj

IPC分类号： C07D413/12 ,  C07D413/14 ,  C07D487/04 ,  A61K31/519 ,  A61P25/28 ,  C07D413/06

CPC分类号： C07D487/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14

摘要： The present invention relates to new compounds of formula (I), to pharmaceutical formulations containing the compounds, and to the use of the compounds in the prevention and/or treatment of mGluR5 receptor-mediated disorders.

公开(公告)号：EP2132201B1

公开(公告)日：2016-11-16

申请号：EP08724190.7

申请日：2008-03-05

申请人： AstraZeneca AB

发明人： ARZEL, Erwan ,  SWAHN, Britt-Marie ,  WENSBO, David

IPC分类号： C07D405/04 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/501 ,  C07D409/04 ,  C07D471/04

CPC分类号： C07D405/04 ,  C07D409/04 ,  C07D471/04

公开(公告)号：EP2125800A1

公开(公告)日：2009-12-02

申请号：EP08705218.9

申请日：2008-01-21

申请人： AstraZeneca AB

发明人： VALLIN, Michaela ,  MALMSTRÖM, Jonas ,  PYRING, David ,  SLIVO, Can ,  WENSBO, David

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61K51/00 ,  A61P25/28 ,  A61K101/00

CPC分类号： C07D471/04 ,  A61K49/10 ,  A61K51/041 ,  A61K51/0453 ,  A61K51/0455 ,  A61K51/0459 ,  A61K51/0463

摘要： The present invention relates to novel heteroaryl substituted imidazopyridine derivatives, precursors thereof, and therapeutic uses of such compounds, having the structural formula (Ia) and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted imidazopyridine derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measureing clinical efficacy of Alzheimer's disease therapeutic agents.

公开(公告)号：EP1536790A2

公开(公告)日：2005-06-08

申请号：EP03749015.8

申请日：2003-08-08

申请人： AstraZeneca AB ,  NPS PHARMACEUTICALS, INC.

发明人： MCLEOD, Donald, A. ,  KERS, Annika ,  MALMBERG, Johan ,  OSCARSSON, Karin ,  EDWARDS, Louise ,  ISAAC, Methvin ,  SLASSI, Abdelmalik ,  STORMANN, Thomas, M. ,  XIN, Tao ,  ARORA, Jalaj ,  WENSBO, David ,  STEFANAC; Tomislav

IPC分类号： A61K31/4245 ,  C07D271/06 ,  C07D271/10 ,  C07D261/08 ,  A61P25/00 ,  C07D271/07 ,  C07D271/113 ,  C07D261/14 ,  C07D413/10 ,  C07D413/06 ,  C07D413/04 ,  C07D413/14

CPC分类号： C07D271/06 ,  C07D261/08 ,  C07D261/14 ,  C07D271/07 ,  C07D271/107 ,  C07D271/113 ,  C07D413/04 ,  C07D413/06 ,  C07D413/10 ,  C07D413/14

摘要： The present invention relates to new compounds of formula (I), wherein P, Q, X1, X2, X3, X4, R, R1, R2, R3, R4, R5, R6, R7, m, n, o, p and q are defined as in any one of claims 1 to 12, a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy. It has been found that the compounds according to the present invention, or salts therof, exhibit a high degree of potency and selectivity for individual metabotropic glutamate receptor (mGluR) subtypes. In particular there are compounds according to the present invention that are potent and selective for the mGluR Group I receptor and more particularly for mGluR5. Thus, it is expected that the compounds of the invention are well suited for the prevention and/or treatment of mGluR5 receptor-mediated disorders such as acute and chronic neurological and psychiatric disorders and chronic and acute pain disorders.

公开(公告)号：EP2121655A1

公开(公告)日：2009-11-25

申请号：EP08724189.9

申请日：2008-03-05

申请人： AstraZeneca AB

发明人： ARZEL, Erwan ,  SWAHN, Britt-Marie ,  WENSBO, David

IPC分类号： C07D401/04 ,  A61K31/4439 ,  A61K31/497 ,  C07D403/04

CPC分类号： C07D401/04

摘要： The present invention relates to novel 2-heteroaryl substituted indole derivatives, precursors thereof, and therapeutic uses of such compounds, having the structural formula (Ia) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel 2-heteroaryl substituted indole derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measureing clinical efficacy of Alzheimer?s disease therapeutic agents.

公开(公告)号：EP1981883A1

公开(公告)日：2008-10-22

申请号：EP07709290.6

申请日：2007-01-25

申请人： AstraZeneca AB

发明人： GRAVENFORS, Ylva ,  JONASSON, Catrin ,  MALMSTRÖM, Jonas ,  NORDVALL, Gunnar ,  PYRING, David ,  SLIVO, Can ,  SOHN, Daniel ,  STRÖM, Peter ,  WENSBO, David

IPC分类号： C07D417/04 ,  A61K31/4436 ,  A61K31/496 ,  A61P25/28 ,  C07D417/14 ,  C07D513/04

CPC分类号： C07D417/04 ,  C07B59/002 ,  C07D513/04

摘要： The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: [Chemical formula should be inserted here. Please see paper copy] and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted benzothiazole derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measureing clinical efficacy of Alzheimer's disease therapeutic agents.

公开(公告)号：EP1723144A1

公开(公告)日：2006-11-22

申请号：EP05802855.6

申请日：2005-02-15

申请人： AstraZeneca AB ,  NPS PHARMACEUTICALS, INC.

发明人： EDWARDS, Louise ,  ISAAC, Methvin ,  JOHANSSON, Martin ,  KERS, Annika ,  MALMBERG, Johan ,  MCLEOD, Donald ,  MINIDIS, Alexander ,  STAAF, Karin ,  SLASSI, Abdelmalik ,  STEFANAC, Tomislav ,  STORMANN, Thomas ,  WENSBO, David ,  XIN, Tao ,  ARORA, Jalaj

IPC分类号： C07D413/12 ,  C07D413/14 ,  C07D487/04 ,  A61K31/519 ,  A61P25/28 ,  C07D413/06

CPC分类号： C07D487/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14

摘要： The present invention relates to new compounds of formula (I), to pharmaceutical formulations containing the compounds, and to the use of the compounds in the prevention and/or treatment of mGluR5 receptor-mediated disorders.

公开(公告)号：EP2132201A1

公开(公告)日：2009-12-16

申请号：EP08724190.7

申请日：2008-03-05

申请人： AstraZeneca AB

发明人： ARZEL, Erwan ,  SWAHN, Britt-Marie ,  WENSBO, David

IPC分类号： C07D405/04 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/501 ,  C07D409/04 ,  C07D471/04

CPC分类号： C07D405/04 ,  C07D409/04 ,  C07D471/04

摘要： The present invention relates to novel 2-heteroaryl substituted benzothiophene and benzofuran derivatives, precursors thereof, and therapeutic uses of such compounds, having the structural formula (Ia) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel 2-heteroaryl substituted benzothiophene and benzofuran derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measureing clinical efficacy of Alzheimer's disease therapeutic agents.

公开(公告)号：EP1581525A2

公开(公告)日：2005-10-05

申请号：EP03785076.5

申请日：2003-08-08

申请人： AstraZeneca AB ,  NPS PHARMACEUTICALS, INC.

发明人： WENSBO, David ,  XIN, Tao ,  STEFANAC, Thomislav ,  ARORA, Jalaj ,  EDWARDS, Louise ,  ISAAC, Methvin ,  SLASSI, Abdelmalik

IPC分类号： C07D413/14 ,  C07D417/14 ,  A61K31/4245 ,  A61P25/00

CPC分类号： C07D413/14 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14

摘要： The present invention relates to new compounds of formula I, wherein P Q X1 X2 X3 X4 X5 R R1 R2 R3 R4R5 G M1 M2 M3 m and n are defined as in formula I, a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.