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：EP3066091B1

公开(公告)日：2019-04-03

申请号：EP14802476.3

申请日：2014-10-30

申请人： Astrazeneca AB

发明人： NORDVALL, Gunnar ,  HÖGDIN, Katharina ,  MALMBORG, Per Jonas ,  KERS, Annika ,  WEIGELT, Dirk ,  BERNSTEIN, Peter ,  QUIRK, Michael ,  BALESTRA, Michael

IPC分类号： C07D401/14 ,  C07D401/12 ,  C07D213/40 ,  A61K31/4402 ,  A61K31/4439 ,  A61P25/24

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：EP3176172A1

公开(公告)日：2017-06-07

申请号：EP17150757.7

申请日：2011-12-21

申请人： Astrazeneca AB

发明人： CSJERNYIK, Gabor ,  KARLSTR M, Sofia ,  KERS, Annika ,  KOLMODIN, Karin ,  NYLÖF, Martin ,  ÖHBERG, Liselotte ,  RAKOS, Laszlo ,  SANDBERG, Lars ,  SEHGELMEBLE, Fernando ,  SÖDERMAN, Peter ,  SWAHN, Britt-Marie ,  VON BERG, Stefan

IPC分类号： C07D491/107 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/4439 ,  A61K31/506 ,  A61P25/28 ,  C07D401/04 ,  C07D235/02 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D491/20

摘要： The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aß-related pathologies such as Down's syndrome, ß- amyloid angiopathy such as, but not limited to, cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI ("mild cognitive impairment"), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease.

摘要翻译： 本发明涉及式（I）的化合物及其药物组合物。 此外，本发明涉及用于治疗和/或预防Aβ相关病症如唐氏综合症，β-淀粉样血管病例如但不限于脑淀粉样血管病或遗传性脑出血的疾病的治疗方法，与 认知障碍，诸如但不限于MCI（“轻度认知障碍”），阿尔茨海默病，记忆丧失，与阿尔茨海默病相关的注意力缺陷症状，与诸如阿尔茨海默病的疾病相关的神经变性或包括混合血管和退行性起源的痴呆在内的痴呆， 老年痴呆症，老年痴呆症和帕金森病相关的痴呆症。

公开(公告)号：EP2655378A1

公开(公告)日：2013-10-30

申请号：EP11850232.7

申请日：2011-12-21

申请人： AstraZeneca AB

发明人： CSJERNYIK, Gabor ,  KARLSTRÖM, Sofia ,  KERS, Annika ,  KOLMODIN, Karin ,  NYLÖF, Martin ,  ÖHBERG, Liselotte ,  RAKOS, Laszlo ,  SANDBERG, Lars ,  SEHGELMEBLE, Fernando ,  SÖDERMAN, Peter ,  SWAHN, Britt-Marie ,  VON BERG, Stefan

IPC分类号： C07D491/107 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/4439 ,  A61K31/506 ,  A61P25/28 ,  C07D401/04 ,  C07D235/02 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D491/20

CPC分类号： A61K31/497 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/506 ,  A61K45/06 ,  A61K2300/00 ,  C07D235/02 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D471/04 ,  C07D491/107 ,  C07D491/20

摘要： The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Αβ-related pathologies such as Down's syndrome, β- amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI ("mild cognitive impairment"), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease.

公开(公告)号：EP2217566A1

公开(公告)日：2010-08-18

申请号：EP08850659.7

申请日：2008-11-14

申请人： AstraZeneca AB

发明人： BYLUND, Johan ,  EK, Maria ,  HOLENZ, Jörg ,  JOHANSSON, Martin H ,  KERS, Annika ,  NÄRHI, Katja ,  NORDVALL, Gunnar ,  ÖHBERG, Liselotte ,  SOHN, Daniel ,  VIKLUND, Jenny ,  VON BERG, Stefan

IPC分类号： C07C311/51 ,  A61K31/145 ,  A61P19/00 ,  C07D209/42 ,  C07D213/04 ,  C07D213/78 ,  C07D231/14 ,  C07D263/57 ,  C07D277/56 ,  C07D277/64 ,  C07D307/68 ,  C07D307/79 ,  C07D333/38 ,  C07D405/04 ,  C07D409/06 ,  C07D417/04 ,  C07D498/04 ,  C07D333/52

CPC分类号： C07D209/08 ,  C07C311/51 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/42 ,  C07C2603/74 ,  C07D209/42 ,  C07D213/56 ,  C07D213/81 ,  C07D213/82 ,  C07D215/54 ,  C07D231/14 ,  C07D239/28 ,  C07D263/57 ,  C07D277/22 ,  C07D277/30 ,  C07D277/56 ,  C07D277/66 ,  C07D307/24 ,  C07D307/79 ,  C07D307/80 ,  C07D317/46 ,  C07D333/24 ,  C07D333/38 ,  C07D333/60 ,  C07D333/68 ,  C07D405/04 ,  C07D409/04 ,  C07D417/04 ,  C07D498/04 ,  C07D513/04

摘要： The invention provides compounds of formula wherein R1, R3, L1, L2, G1, G2, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.

摘要翻译： 本发明提供下式的化合物，其中R1，R3，L1，L2，G1，G2，A和m如说明书和旋光异构体，外消旋体和互变异构体及其药学上可接受的盐所定义; 以及其制备方法，含有它们的药物组合物及其在治疗中的用途。 这些化合物是微粒体前列腺素E合酶-1的抑制剂。

公开(公告)号：EP2069364A1

公开(公告)日：2009-06-17

申请号：EP07835061.8

申请日：2007-09-27

申请人： AstraZeneca AB

发明人： JOHANSSON, Rolf ,  KARLSTRÖM, Sofia ,  KERS, Annika ,  NORDVALL, Gunnar ,  REIN, Tobias ,  SLIVO, Can

IPC分类号： C07D513/04 ,  A61K31/519 ,  A61P11/06 ,  A61P25/00 ,  A61P9/10

CPC分类号： C07D513/04

摘要： There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I) wherein R1, R2, R3, R4 and n are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.

公开(公告)号：EP4001272A1

公开(公告)日：2022-05-25

申请号：EP21196371.5

申请日：2014-10-30

申请人： Astrazeneca AB

发明人： NORDVALL, Gunnar ,  HÖGDIN, Katharina ,  MALMBORG, Per Jonas ,  KERS, Annika ,  WEIGELT, Dirk ,  BERNSTEIN, Peter ,  QUIRK, Michael ,  BALESTRA, Michael

IPC分类号： C07D401/14 ,  C07D401/12 ,  C07D213/40 ,  A61K31/4402 ,  A61K31/4439 ,  C07K5/068 ,  C07K5/078 ,  C07K5/065 ,  C07K5/072 ,  C07K5/062 ,  A61P25/24

摘要： Prodrugs of an NMDA antagonist, (S)-1-phenyl-2-(pyridin-2-yl)ethanamine, useful for the treatment of depression (particularly major depressive disorder) or pain; compositions comprising them, and methods of making them.

公开(公告)号：EP3176172B1

公开(公告)日：2020-01-29

申请号：EP17150757.7

申请日：2011-12-21

申请人： Astrazeneca AB

发明人： CSJERNYIK, Gabor ,  KARLSTRÖM, Sofia ,  KERS, Annika ,  KOLMODIN, Karin ,  NYLÖF, Martin ,  ÖHBERG, Liselotte ,  RAKOS, Laszlo ,  SANDBERG, Lars ,  SEHGELMEBLE, Fernando ,  SÖDERMAN, Peter ,  SWAHN, Britt-Marie ,  VON BERG, Stefan

IPC分类号： C07D491/107 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/4439 ,  A61K31/506 ,  A61P25/28 ,  C07D401/04 ,  C07D235/02 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D491/20

公开(公告)号：EP3066091A1

公开(公告)日：2016-09-14

申请号：EP14802476.3

申请日：2014-10-30

申请人： Astrazeneca AB

发明人： NORDVALL, Gunnar ,  HÖGDIN, Katharina ,  MALMBORG, Per Jonas ,  KERS, Annika ,  WEIGELT, Dirk ,  BERNSTEIN, Peter ,  QUIRK, Michael ,  BALESTRA, Michael

IPC分类号： C07D401/14 ,  C07D401/12 ,  C07D213/40 ,  A61K31/4402 ,  A61K31/4439 ,  A61P25/24

CPC分类号： C07D213/40 ,  A61K38/00 ,  C07D401/12 ,  C07D401/14 ,  C07K5/06043 ,  C07K5/06078 ,  C07K5/06095 ,  C07K5/06104 ,  C07K5/06139 ,  C07K5/06147

摘要： Prodrugs of an NMDA antagonist, (S)-1-phenyl-2-(pyridin-2-yl)ethanamine, useful for the treatment of depression (particularly major depressive disorder) or pain; compositions comprising them, and methods of making them.

摘要翻译： NMDA拮抗剂的前药，（S）-1-苯基-2-（吡啶-2-基）乙胺，可用于治疗抑郁症（特别是重度抑郁障碍）或疼痛; 包含它们的组合物及其制备方法。