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公开(公告)号：EP1313703B1
公开(公告)日：2008-02-13
申请号：EP01965201.5
申请日：2001-08-20
发明人： ALANINE, Alexander , BUETTELMANN, Bernd , FISHER, Holger , HEITZ NEIDHART, Marie-Paule , HUWYLER, Joerg , JAESCHKE, Georg , PINARD, Emmanuel , WYLER, Rene
IPC分类号： C07D211/42 , A61K31/445 , A61P25/28 , C07F9/59
CPC分类号： C07D211/42 , C07F9/591
摘要： The invention relates to compounds of the general formula (I) wherein R is a) -C(O)(CH2)nC(O)OH, b) wherein R1 is -N(R?2)(R3) and R2/R3¿ are independently from each other hydrogen or lower alkyl, or is a cyclic tertiary amine, optionally substituted by lower alkyl, c) -P(O)(OH)¿2?, or is d) -C(O)(CH)2)nNHC(O)(CH2)nN(R?2)(R3¿); and n is 1, 2, 3 or 4; and to pharmaceutically acceptable acid addition salts thereof. These compounds may be used as prodrugs for the parentcompound of formula (II) which are useful in the treatment of NMDA receptor-related diseases.
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公开(公告)号：EP1506190A1
公开(公告)日：2005-02-16
申请号：EP03752750.4
申请日：2003-05-16
IPC分类号： C07D403/06 , C07D409/14 , A61K31/505
CPC分类号： C07D403/06 , C07D409/14
摘要： The present invention relates to compounds of formula (I) wherein A is an unsubstituted cyclic group; and R is hydrogen or lower alkyl; and pharmaceutically acceptable acid addition salts thereof. It has been shown that the compounds of formulas IA and IB are good NMDA NR-2B receptor subtype specific blockers. Possible therapeutic indications for these compounds include acute forms of neurodegeneration caused, e.g., by stroke and brain trauma, and chronic forms of neurodegeneration such as Alzheimer's disease, Parkinson's disease, Huntington's disease, ALS(amyotrophic lateral sclerosis) and neurodegeneration associated with bacterial or viral infections and, in addition, depression and chronic and acute pain.
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公开(公告)号：EP0760819B1
公开(公告)日：2000-07-19
申请号：EP95920816.6
申请日：1995-05-16
发明人： BÜTTELMANN, Bernd , GODEL, Thierry , GROSS, Laurence , HEITZ NEIDHART, Marie-Paule , RIEMER, Claus , WYLER, René
IPC分类号： C07D487/04 , C07D471/04 , C07D498/04 , A61K31/505 , A61K31/435
CPC分类号： C07D471/04 , C07D487/04
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公开(公告)号：EP1358165A1
公开(公告)日：2003-11-05
申请号：EP02714095.3
申请日：2002-01-21
发明人： ALANINE, Alexander , BUETTELMANN, Bernd , HEITZ NEIDHART, Marie-Paule , JAESCHKE, Georg , PINARD, Emmanuel , WYLER, Rene
IPC分类号： C07D233/54 , C07D233/61 , C07D233/84 , C07D401/06 , A61K31/4164 , A61P25/28
CPC分类号： C07D233/64 , C07D231/12 , C07D233/56 , C07D233/84 , C07D249/08
摘要： The invention related to compounds of the general formula (I), wherein the substituents are defined in claim 1. These compounds have a good affinity to the NMDA (N-methyl-D-aspartate)-receptor subtype selective blockers, which have a key function in modulating neuronal activity and plasticity which makes them key players in mediating processes underlying development of CNS as well as learning and memory formation. These compounds are therefore suitable in the control or treatment of diseases, related to this receptor.
摘要翻译： 本发明涉及通式（I）的化合物，其中取代基如权利要求1所定义。这些化合物对NMDA（N-甲基-D-天冬氨酸） - 受体亚型选择性阻断剂具有良好的亲和力，其具有键 在调节神经元活动和可塑性方面起作用，这使得它们成为介导中枢神经系统发育过程以及学习和记忆形成过程的关键参与者。 因此这些化合物适用于控制或治疗与该受体有关的疾病。
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公开(公告)号：EP0760819A1
公开(公告)日：1997-03-12
申请号：EP95920816.0
申请日：1995-05-16
发明人： BÜTTELMANN, Bernd , GODEL, Thierry , GROSS, Laurence , HEITZ NEIDHART, Marie-Paule , RIEMER, Claus , WYLER, René
IPC分类号： A61K31 , A61P3 , A61P9 , A61P17 , A61P25 , A61P39 , C07D233 , C07D471 , C07D487 , C07D491 , C07D498
CPC分类号： C07D471/04 , C07D487/04
摘要： Compounds of general formulae (Ia), (Ib) and (II), wherein R?1 and R2¿ each independently signify hydrogen, lower alkyl, lower alkoxy, nitro, trifluoromethyl, amino, halogen, cyano or R?3R4NS(O)¿2- and R?3 and R4¿ signify lower alkyl, and R2 can additionally signify morpholino or thiomorpholino, a 5- or 6-membered heterocycle with 1-3 N atoms optionally substituted by lower alkyl, hydroxy, amino or the group -CH¿2?NHCH3, a bicyclic heterocycle with 1-3 N atoms or a group -NR?5R6 or -OR5¿ in which R?5 and R6¿ can be the same or different and signify hydrogen, lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, amino-lower alkyl or lower alkylamino-lower alkyl, and X in formula (II) signifies -CH=CH-, -CH=N-, -NH-, -CO- or -O-, as well as pharmaceutically usable salts of compounds of general formulae (Ia), (Ib) and (II). They can be used for the treatment or prevention of illnesses, especially for the treatment or prevention of ischemia, hypoglycaemia, hypoxia, cerebral vascular spasms, spasticity, trauma, hemorrhagia, infection (viral, bacterial, amoebic, prional), epileptic seizures, autoimmune diseases, withdrawal symptoms, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, intoxications, olivoponto-cerebellar atrophy, spinal cord injuries, schizophrenia, depressions, anxiety states, dependence, pains, autism and mental retardation.
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公开(公告)号：EP1358165B1
公开(公告)日：2009-03-11
申请号：EP02714095.3
申请日：2002-01-21
发明人： ALANINE, Alexander , BUETTELMANN, Bernd , HEITZ NEIDHART, Marie-Paule , JAESCHKE, Georg , PINARD, Emmanuel , WYLER, Rene
IPC分类号： C07D233/54 , C07D233/61 , C07D233/84 , C07D401/06 , A61K31/4164 , A61P25/28
CPC分类号： C07D233/64 , C07D231/12 , C07D233/56 , C07D233/84 , C07D249/08
摘要： The invention related to compounds of the general formula (I), wherein the substituents are defined in claim 1. These compounds have a good affinity to the NMDA (N-methyl-D-aspartate)-receptor subtype selective blockers, which have a key function in modulating neuronal activity and plasticity which makes them key players in mediating processes underlying development of CNS as well as learning and memory formation. These compounds are therefore suitable in the control or treatment of diseases, related to this receptor.
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公开(公告)号：EP1189886B1
公开(公告)日：2006-01-04
申请号：EP00936835.8
申请日：2000-05-31
发明人： ALANINE, Alexander , BURNER, Serge , BUETTELMANN, Bernd , HEITZ NEIDHART, Marie-Paule , JAESCHKE, Georg , PINARD, Emmanuel , WYLER, René
IPC分类号： C07D211/46 , C07D211/30 , A61K31/445 , A61P25/00
CPC分类号： C07D211/46 , C07D211/14
摘要： The invention relates to compounds of general formula (I) wherein R signify hydrogen or hydroxy; R2 signify hydrogen or methyl; and X signify -O- or -CH¿2?-; and their pharmaceutically acceptable acid addition salts. It has been shown that these compounds have a good affinity to the NMDA receptor and they are therefore useful in the treatment of diseases, wherein the therapeutic indications include acute forms of neurodegeneration caused, e.g., by stroke or brain trauma; chronic forms of neurodegeneration such as Alzheimer's disease, Parkinsons's disease, Huntington's disease or ALS (amyotrophic lateral sclerosis); neurodegeneration associated with bacterial or viral infections, and, diseases such as schizophrenia, anxiety, depression and chronic/acute pain.
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公开(公告)号：EP1448547B1
公开(公告)日：2005-04-20
申请号：EP02787541.8
申请日：2002-11-02
发明人： ALANINE, Alexander , BUETTELMANN, Bernd , HEITZ NEIDHART, Marie-Paule , PINARD, Emmanuel , WYLER, René
IPC分类号： C07D401/04 , C07D498/02 , A61K31/535 , A61K31/47 , A61P25/00
CPC分类号： C07D401/04
摘要： The invention relates to compounds of formulas (IA) or (IB) wherein R1 and R2 are independently from each other hydrogen, lower alkyl, -(CH2)n-OH, -(CH2)n-N(R6)2, -NR6C(O)C(O)O-lower alkyl, -NR6-(CH2)n-OH, -NR6C(O)-lower alkyl, -NH-benzyl or NR6C(O)-(CH2)n-OH; R6 is independently from each other hydrogen or lower alkyl R' is hydrogen or lower alkyl; R3 is hydrogen or amino; R4 is hydrogen or lower alkyl; R5 is hydrogen or halogen; or R1 and R' may be together with the carbon atoms to which they are attached the group (CH2)4-; or R2 and R3 may be together with the carbon atoms to which they are attached the group -N(R6)-CH2-O-CH2-; n is 0, 1, 2 or 3; and to pharmaceutically acceptable acid addition salts thereof. It has been shown that these compounds have a good affinity to the NMDA receptor and they may therefore be used for the treatment of diseases, related to this receptor.
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公开(公告)号：EP1443926A1
公开(公告)日：2004-08-11
申请号：EP02782972.0
申请日：2002-10-22
发明人： ALANINE, Alexander , BUETTELMANN, Bernd , HEITZ NEIDHART, Marie-Paule , PINARD, Emmanuel , WYLER, René
IPC分类号： A61K31/44 , A61K31/381 , C07D213/73 , C07D213/74 , C07D409/04
CPC分类号： C07D213/73 , C07D213/38 , C07D213/53 , C07D213/74 , C07D213/79 , C07D213/84 , C07D409/04
摘要： The present invention relates to compounds of formulas (IA) or (IB) wherein R1/R2 independently from each other hydrogen, lower alkyl, -(CH2)nNR5R5' or -(CH2)n+1OH; R5 and R5' are independently from each hydrogen, lower alkyl; R3/R4 are independently from each other hydrogen, lower alkyl, lower alkoxy, halogen, trifluoromethyl or hydroxy; Ar is phenyl or thiophenyl; the dotted line is -CH2-CH2-, -CH2-CHR'-, wherein R' is lower alkyl or are two hydrogen atoms, not forming a bridge and; n is 0, 1 or 2; and to pharmaceutically acceptable acid addition salts thereof, with the exception of 6-styryl-pyridin-2-yl-amine. The compounds of the present invention are NMDA (N-methyl-D-aspartate)-receptor subtype blockers and may be used in the treatment of diseases related to this receptor.
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公开(公告)号：EP1506190B1
公开(公告)日：2006-06-14
申请号：EP03752750.4
申请日：2003-05-16
IPC分类号： C07D403/06 , C07D409/14 , A61K31/505
CPC分类号： C07D403/06 , C07D409/14
摘要： The present invention relates to compounds of formula (I) wherein A is an unsubstituted cyclic group; and R is hydrogen or lower alkyl; and pharmaceutically acceptable acid addition salts thereof. It has been shown that the compounds of formulas IA and IB are good NMDA NR-2B receptor subtype specific blockers. Possible therapeutic indications for these compounds include acute forms of neurodegeneration caused, e.g., by stroke and brain trauma, and chronic forms of neurodegeneration such as Alzheimer's disease, Parkinson's disease, Huntington's disease, ALS(amyotrophic lateral sclerosis) and neurodegeneration associated with bacterial or viral infections and, in addition, depression and chronic and acute pain.
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