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1. 发明申请

WO2011073172A1 ETHYNYL DERIVATIVES 审中-公开
标题翻译：乙炔衍生物
公开(公告)号：WO2011073172A1
公开(公告)日：2011-06-23
申请号：PCT/EP2010/069593
申请日：2010-12-14
申请人： F. HOFFMANN-LA ROCHE AG , GREEN, Luke , GUBA, Wolfgang , JAESCHKE, Georg , JOLIDON, Synese , LINDEMANN, Lothar , STADLER, Heinz , VIEIRA, Eric
发明人： GREEN, Luke , GUBA, Wolfgang , JAESCHKE, Georg , JOLIDON, Synese , LINDEMANN, Lothar , STADLER, Heinz , VIEIRA, Eric
IPC分类号： C07D471/04 , C07D487/04 , A61K31/4162 , A61P25/00
CPC分类号： C07D487/04 , C07D471/04
摘要： The present invention relates to ethynyl derivatives of formula (I) wherein X is N or C-R 1 ; Y is N or C-R 2 ; Z is CH or N; R 4 is a 6-membered aromatic substituent containing 0, 1 or 2 nitrogen atoms, optionally substituted by 1 to 3 groups, selected from halogen, lower alkyl, lower alkoxy or NRR'; R 1 is hydrogen, lower alkyl, lower alkoxy, hydroxy, lower hydroxyalkyl, lower cycloalkyl or is heterocycloalkyl optionally substituted with hydroxy or alkoxy; R 2 is hydrogen, CN, lower alkyl or heterocycloalkyl; R and R' are independently from each other hydrogen or lower alkyl; or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula (I) are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5) and they are therefore useful for the treatment of diseases related to this receptor.
摘要翻译：本发明涉及式（I）的乙炔基衍生物，其中X是N或C-R 1; Y是N或C-R2; Z是CH或N; R4是含有0,1或2个氮原子的6元芳族取代基，任选被1至3个选自卤素，低级烷基，低级烷氧基或NRR'的基团取代; R 1是氢，低级烷基，低级烷氧基，羟基，低级羟基烷基，低级环烷基或任选被羟基或烷氧基取代的杂环烷基; R2是氢，CN，低级烷基或杂环烷基; R和R'彼此独立地为氢或低级烷基; 或其药学上可接受的盐或酸加成盐，或其相应的对映异构体和/或其旋光异构体和/或立体异构体。现在惊奇地发现，通式（I）的化合物是代谢型谷氨酸受体亚型5（mGluR5）的正变构调节剂（PAM），因此它们可用于治疗与该受体有关的疾病。

2. 发明申请

WO2011128279A1 ARYLETHYNYL DERIVATIVES 审中-公开
标题翻译： ARYLETHYNYL衍生物
公开(公告)号：WO2011128279A1
公开(公告)日：2011-10-20
申请号：PCT/EP2011/055585
申请日：2011-04-11
申请人： F. HOFFMANN-LA ROCHE AG , GREEN, Luke , GUBA, Wolfgang , JAESCHKE, Georg , JOLIDON, Synese , LINDEMANN, Lothar , RICCI, Antonio , RUEHER, Daniel , STADLER, Heinz , VIEIRA, Eric
发明人： GREEN, Luke , GUBA, Wolfgang , JAESCHKE, Georg , JOLIDON, Synese , LINDEMANN, Lothar , RICCI, Antonio , RUEHER, Daniel , STADLER, Heinz , VIEIRA, Eric
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D413/04 , C07D413/14 , C07D498/04 , A61K31/506 , A61P25/18
CPC分类号： C07D471/04 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/04 , C07D413/14 , C07D491/107 , C07D498/04
摘要： The present invention relates to ethynyl derivatives of formula (I) as allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5). The variables in formula (I) are defined in the specification.
摘要翻译：本发明涉及式（I）的乙炔基衍生物作为代谢型谷氨酸受体亚型5（mGluR5）的变构调节剂。式（I）中的变量在说明书中定义。

3. 发明申请

WO2011051201A1 POSITIVE ALLOSTERIC MODULATORS (PAM) 审中-公开
标题翻译：积极的独立调制器（PAM）
公开(公告)号：WO2011051201A1
公开(公告)日：2011-05-05
申请号：PCT/EP2010/066016
申请日：2010-10-25
申请人： F. HOFFMANN-LA ROCHE AG , GREEN, Luke , GUBA, Wolfgang , JAESCHKE, Georg , JOLIDON, Synese , LINDEMANN, Lothar , RICCI, Antonio , RUEHER, Daniel , STADLER, Heinz , VIEIRA, Eric
发明人： GREEN, Luke , GUBA, Wolfgang , JAESCHKE, Georg , JOLIDON, Synese , LINDEMANN, Lothar , RICCI, Antonio , RUEHER, Daniel , STADLER, Heinz , VIEIRA, Eric
IPC分类号： C07D213/74 , C07D239/34 , C07D239/42 , C07D401/06 , C07D405/12 , C07D413/06 , C07D493/08 , A61K31/44 , A61K31/4427 , A61K31/505 , A61K31/506
CPC分类号： C07D213/74 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/505 , A61K31/506 , C07D213/64 , C07D239/34 , C07D239/42 , C07D401/06 , C07D405/12 , C07D413/06 , C07D493/08
摘要： The present invention relates to phenylethynyl derivatives of formula (I) wherein R 1 is hydrogen, halogen, lower alkyl or lower alkyl substituted by halogen; R 2 is hydrogen, lower alkyl, =O, lower alkoxy, phenyl, hydroxy or lower alkyl substituted by hydroxy; X is N, CF or CH; L is -NR 3 -, -NHC(R 3 ) 2 -, -O-, -OC(R 3 ) 2 -, -CR 4 R 4' -; R 3 is hydrogen or lower alkyl; R 4 /R 4' are independently from each other hydrogen or lower alkyl; cyc is cycloalkyl or heterocycloalkyl, or is a non-aromatic bicycle selected from 7-oxa- bicyclo[2.2.1]hept-1-yl or bicyclo[2.2.1]hept-1-yl; n is 1, 2 or 3; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They are useful for the treatment of schizophrenia or cognitive diseases.
摘要翻译：本发明涉及式（I）的苯基乙炔基衍生物，其中R 1是氢，卤素，低级烷基或被卤素取代的低级烷基; R2是氢，低级烷基，= O，低级烷氧基，苯基，羟基或被羟基取代的低级烷基; X为N，CF或CH; L是-NR 3 - ， - NHC（R 3）2 - ， - O - ， - OC（R 3）2 - ， - CR 4 R 4' R3是氢或低级烷基; R4 / R4'彼此独立地为氢或低级烷基; 环是环烷基或杂环烷基，或是选自7-氧杂双环[2.2.1]庚-1-基或双环[2.2.1]庚-1-基的非芳族自行车; n为1,2或3; 或其药学上可接受的酸加成盐，或其相应的对映异构体和/或其旋光异构体和/或立体异构体。现在惊奇地发现通式I的化合物是代谢型谷氨酸受体亚型5（mGluR5）的正变构调节剂（PAM）。它们可用于治疗精神分裂症或认知疾病。

4. 发明申请

WO2012143340A1 5-(PHENYL/PYRIDINYL-ETHINYL)-2-PYRIDINE/ 2-PYRIMIDINE-CARBORXAMIDES AS MGLUR5 MODULATORS 审中-公开
标题翻译：作为MGLUR5调节剂的5-（苯基/吡啶-2-基乙基）-2-吡啶-2-羧酸吡啶
公开(公告)号：WO2012143340A1
公开(公告)日：2012-10-26
申请号：PCT/EP2012/056966
申请日：2012-04-17
申请人： F. HOFFMANN-LA ROCHE AG , JAESCHKE, Georg , JOLIDON, Synese , LINDEMANN, Lothar , RICCI, Antonio , RUEHER, Daniel , STADLER, Heinz , VIEIRA, Eric
发明人： JAESCHKE, Georg , JOLIDON, Synese , LINDEMANN, Lothar , RICCI, Antonio , RUEHER, Daniel , STADLER, Heinz , VIEIRA, Eric
IPC分类号： C07D213/56 , C07D213/57 , C07D239/28 , C07D401/06 , C07D403/06 , C07D407/12 , C07D413/06 , A61P25/00 , A61P25/28 , A61K31/4427 , A61K31/445 , A61K31/506
CPC分类号： C07D213/56 , C07D213/57 , C07D239/28 , C07D401/06 , C07D403/06 , C07D407/12 , C07D413/06
摘要： The present invention relates to ethynyl derivatives of formula (I), wherein, Y is N or C-R 3 ;and R 3 is hydrogen, methyl, halogen or nitrile; R 1 is phenyl or pyridinyl, which are optionally substituted by halogen, lower alkyl or lower alkoxy; R 2 /R 2' are independently from each other hydrogen, lower alkyl or lower alkyl substituted by halogen, or R 2 and R 2' may form together with the N-atom to which they are attached a morpholine ring, a piperidine ring or an azetidine ring, which are unsubstituted or substituted one or more substituents selected from lower alkoxy, halogen, hydroxy or methyl; R 4 /R 4' are independently from each other hydrogen or lower alkyl, or R 4 and R 4' form together a C 3-5 cycloalkyl-, tetrahydrofuran- or an oxetane-ring; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula (I) are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5).
摘要翻译：本发明涉及式（I）的乙炔基衍生物，其中Y为N或C-R 3;且R 3为氢，甲基，卤素或腈; R 1是苯基或吡啶基，其任选被卤素，低级烷基或低级烷氧基取代; R 2 / R 2'彼此独立地为氢，低级烷基或被卤素取代的低级烷基，或者R 2和R 2'可以与它们所连接的N-原子一起形成吗啉环，哌啶环或氮杂环丁烷环，其为未取代或取代的一个或多个选自低级烷氧基，卤素，羟基或甲基的取代基; R4 / R4'彼此独立地为氢或低级烷基，或R4和R4'一起形成C3-5环烷基，四氢呋喃或氧杂环丁烷环; 或其药学上可接受的酸加成盐，或其相应的对映异构体和/或其旋光异构体和/或立体异构体。现在惊奇地发现通式（I）的化合物是代谢型谷氨酸受体亚型5（mGluR5）的正变构调节剂（PAM）。

5. 发明申请

WO2012146551A1 ETHYNYL DERIVATIVES AS POSITIVE ALLOSTERIC MODULATORS OF THE MGLUR5 审中-公开
标题翻译：乙烯衍生物作为MGLUR5的阳性调节因子
公开(公告)号：WO2012146551A1
公开(公告)日：2012-11-01
申请号：PCT/EP2012/057335
申请日：2012-04-23
申请人： F. HOFFMANN-LA ROCHE AG , JAESCHKE, Georg , JOLIDON, Synese , LINDEMANN, Lothar , STADLER, Heinz , VIEIRA, Eric
发明人： JAESCHKE, Georg , JOLIDON, Synese , LINDEMANN, Lothar , STADLER, Heinz , VIEIRA, Eric
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , A61K31/44 , A61K31/4406 , A61K31/506 , A61K31/501 , A61K31/55 , A61P25/18 , A61P25/28 , A61P25/30
CPC分类号： C07D403/04 , A61K31/506 , C07D401/04 , C07D401/14 , Y02T10/7011
摘要： The present invention relates to ethynyl derivatives of formula I wherein X is N or C-R, wherein R is hydrogen or halogen; G is N or CH; with the proviso that maximum one of G or X can be nitrogen; R 1 is phenyl or pyridinyl, which are optionally substituted by halogen; R 2 is hydrogen, lower alkyl, hydroxy, lower alkoxy or C(O)O-benzyl; R 3 ,R 3' , R 4 , R 4 , R 6 , R 6' are independently from each other hydrogen or lower alkyl; or R 6 and R 4 may form together with the carbon atom to which they are attached a C 4-6 -cycloalkyl ring, if m is 0 and n is 1 or 2; R 5 is hydrogen or lower alkyl; n is 0, 1 or 2; m is 0 or 1; with the proviso that n and m are not simultaneously 0; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They may be used for the treatment of schizophrenia or cognitive disorders.
摘要翻译：本发明涉及式I的乙炔基衍生物，其中X是N或C-R，其中R是氢或卤素; G为N或CH; 条件是G或X中的最大一个可以是氮; R1是苯基或吡啶基，其任选被卤素取代; R2是氢，低级烷基，羟基，低级烷氧基或C（O）O-苄基; R3，R3'，R4，R4，R6，R6'彼此独立地为氢或低级烷基; 或者R 6和R 4可以与它们所连接的碳原子一起形成C4-6环烷基环，如果m是0且n是1或2; R5是氢或低级烷基; n为0,1或2; m为0或1; 条件是n和m不同时为0; 或其药学上可接受的酸加成盐，或其相应的对映体和/或其旋光异构体和/或立体异构体。现在令人惊奇地发现，通式I的化合物是代谢型谷氨酸受体亚型5（mGluR5）的正变构调节剂（PAM）。它们可用于治疗精神分裂症或认知障碍。

6. 发明申请

WO2012146552A1 PYRAZOLIDIN-3-ONE DERIVATIVES 审中-公开
标题翻译：吡唑啉-3-酮衍生物
公开(公告)号：WO2012146552A1
公开(公告)日：2012-11-01
申请号：PCT/EP2012/057336
申请日：2012-04-23
申请人： F. HOFFMANN-LA ROCHE AG , JAESCHKE, Georg , JOLIDON, Synese , LINDEMANN, Lothar , RICCI, Antonio , RUEHER, Daniel , STADLER, Heinz
发明人： JAESCHKE, Georg , JOLIDON, Synese , LINDEMANN, Lothar , RICCI, Antonio , RUEHER, Daniel , STADLER, Heinz
IPC分类号： C07D401/04 , C07D403/04 , C07D487/04 , A61K31/45 , A61P25/00
CPC分类号： C07D401/04 , C07D403/04 , C07D487/04
摘要： The present invention relates to ethynyl derivatives of formula I wherein X is N or CH; G is N or CH; with the proviso that maximum one of X or G can be nitrogen; R 1 is phenyl or pyridyl, which are optionally substituted by halogen, lower alkyl or lower alkoxy; R 2 is hydrogen, lower alkyl or may form together with R 4 a C 3 -C 6 -cycloalkyl; R 3 /R 3' /R 4 /R 4' are independently from each other hydrogen, lower alkyl or CF 3 ; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5).
摘要翻译：本发明涉及式I的乙炔基衍生物，其中X是N或CH; G是N或CH; 条件是X或G中的最大一个可以是氮; R 1是苯基或吡啶基，其任选被卤素，低级烷基或低级烷氧基取代; R 2是氢，低级烷基或可以与R 4一起形成C 3 -C 6环烷基; R3 / R3'/ R4 / R4'彼此独立地为氢，低级烷基或CF3; 或其药学上可接受的酸加成盐，或其相应的对映异构体和/或其旋光异构体和/或立体异构体。现在惊奇地发现通式I的化合物是代谢型谷氨酸受体亚型5（mGluR5）的正变构调节剂（PAM）。

7. 发明申请

WO2013050460A1 ETHYNYL DERIVATIVES AS METABOTROPIC GLUTAMATE RECEPTOR MODULATORS 审中-公开
标题翻译：乙烯衍生物作为代谢型谷氨酸受体调节剂
公开(公告)号：WO2013050460A1
公开(公告)日：2013-04-11
申请号：PCT/EP2012/069605
申请日：2012-10-04
申请人： F. HOFFMANN-LA ROCHE AG , JAESCHKE, Georg , LINDEMANN, Lothar , RICCI, Antonio , RUEHER, Daniel , STADLER, Heinz , VIEIRA, Eric
发明人： JAESCHKE, Georg , LINDEMANN, Lothar , RICCI, Antonio , RUEHER, Daniel , STADLER, Heinz , VIEIRA, Eric
IPC分类号： C07D237/22 , C07D239/42 , A61K31/44 , A61K31/50 , A61K31/505
CPC分类号： C07D213/74 , C07D237/22 , C07D239/42
摘要： The present invention relates to ethynyl derivatives of formula I wherein Y is N or CH; with the proviso that Y can only be CH, if at least on of U, V or W are N; U is N or C-R 4 ; V and W are independently N or CH; with the proviso that only one of U, V or W can be simultaneously nitrogen; R 4 is hydrogen, methyl or halogen; R 1 is phenyl or heteroaryl, which are optionally substituted by halogen, lower alkyl or lower alkoxy; R is hydrogen or lower alkyl; R 2 is hydrogen, lower alkyl, lower alkoxy, CF 3 or S-lower alkyl; are independently from each other hydrogen, lower alkyl or lower alkoxy; or R 3 and R 3 form together a C 3-5 -cycloalkyl-, tetrahydrofuran- or an oxetane-ring; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
摘要翻译：本发明涉及式I的乙炔基衍生物，其中Y是N或CH; 条件是Y只能是CH，如果至少在U，V或W上是N; U是N或C-R4; V和W独立地为N或CH; 条件是U，V或W中只有一个可以同时为氮; R4是氢，甲基或卤素; R 1是苯基或杂芳基，其任选被卤素，低级烷基或低级烷氧基取代; R是氢或低级烷基; R2是氢，低级烷基，低级烷氧基，CF3或S-低级烷基; 彼此独立地为氢，低级烷基或低级烷氧基; 或R 3和R 3一起形成C 3-5 - 环烷基 - ，四氢呋喃 - 或氧杂环丁烷环; 或其药学上可接受的酸加成盐，或其相应的对映异构体和/或其旋光异构体和/或立体异构体。已经发现通式I的化合物是代谢型谷氨酸受体亚型5（mGluR5）的变构调节剂。

8. 发明申请

WO2013050454A1 ETHYNYL DERIVATIVES AS MGLUR5 ALLOSTERIC MODULATORS 审中-公开
标题翻译：乙醇衍生物作为MGLUR5单独调制剂
公开(公告)号：WO2013050454A1
公开(公告)日：2013-04-11
申请号：PCT/EP2012/069599
申请日：2012-10-04
申请人： F. HOFFMANN-LA ROCHE AG , JAESCHKE, Georg , LINDEMANN, Lothar , RICCI, Antonio , RUEHER, Daniel , STADLER, Heinz , VIEIRA, Eric
发明人： JAESCHKE, Georg , LINDEMANN, Lothar , RICCI, Antonio , RUEHER, Daniel , STADLER, Heinz , VIEIRA, Eric
IPC分类号： C07D401/04 , C07D403/04 , C07D413/04 , A61K31/4439 , A61K31/506 , A61P25/18 , A61P25/08 , A61P25/28
CPC分类号： C07D401/04 , C07D403/04 , C07D413/04
摘要： The present invention relates to ethynyl derivatives of formula (I) wherein U is N or CH, R 8 is hydrogen, halogen, lower alkyl or lower alkoxy;Y is –N(R 4 )-, -O- or –C(R 5 R 5 ')-; wherein R4 is hydrogen or lower alkyl and R 5 /R 5' are independently hydrogen, hydroxy, lower alkyl or lower alkoxy; V is –N(R 6 )- or –C(R 7 R 7' ), wherein R6 is hydrogen or lower alkyl and R 7 /R 7' are independently from each other hydrogen, lower alkyl, CH 2 -lower alkoxy or may form together with the carbon atom to which they are attached a C 3 -C 6 -cycloalkyl; R 1 is phenyl or heteroaryl, which are optionally substituted by halogen, lower alkyl or lower alkoxy; m is 0 or 1; in case m is 1, R 3 /R 3' are independently from each other hydrogen, lower alkyl, CH 2 -lower alkoxy or may form together with the carbon atom to which they are attached a C 3 -C 6 -cycloalkyl; n is 0 or 1; in case n is 1, R 2 /R 2' are independently from each other hydrogen, lower alkyl, CH 2 -lower alkoxy or may form together with the carbon atom to which they are attached a C 3 -C 6 -cycloalkyl; or if m is 1 and n is 0, R 3 and R 7 may form together with the carbon atoms to which they are attached a C 4-6 -cycloalkyl; or if m is 1 and n is 1, R 2 and R 3 or R 3 and R 7 may form together with the carbon atoms to which they are attached a C 4-6 -cycloalkyl; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has been found that the compounds of general formula (I) are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
摘要翻译：本发明涉及式（I）的乙炔基衍生物，其中U是N或CH，R8是氢，卤素，低级烷基或低级烷氧基; Y是-N（R4） - ， - O-或-C（R5R5'） - ; 其中R4是氢或低级烷基，R5 / R5'独立地是氢，羟基，低级烷基或低级烷氧基; V是-N（R6） - 或-C（R7R7'），其中R6是氢或低级烷基，R7 / R7'彼此独立地是氢，低级烷基，CH2-低级烷氧基或可与碳原子一起形成它们与C 3 -C 6环烷基连接; R 1是苯基或杂芳基，其任选被卤素，低级烷基或低级烷氧基取代; m为0或1; 在m为1的情况下，R 3 / R 3'彼此独立地为氢，低级烷基，CH 2 - 低级烷氧基，或者可以与它们所连接的碳原子一起形成C 3 -C 6 - 环烷基; n为0或1; 在n为1的情况下，R 2 / R 2'彼此独立地为氢，低级烷基，CH 2 - 低级烷氧基，或者可以与它们所连接的碳原子一起形成C 3 -C 6 - 环烷基; 或者如果m为1且n为0，则R 3和R 7可以与它们所连接的碳原子一起形成C 4-6 - 环烷基; 或者如果m为1且n为1，则R2和R3或R3和R7可以与它们所连接的碳原子一起形成C 4-6 - 环烷基; 或其药学上可接受的酸加成盐，或其相应的对映异构体和/或其旋光异构体和/或立体异构体。已经发现通式（I）的化合物是代谢型谷氨酸受体亚型5（mGluR5）的变构调节剂。

9. 发明申请

WO2013045380A2 PHARMACEUTICALLY ACCEPTABLE MGLUR5 POSITIVE ALLOSTERIC MODULATORS AND THEIR METHODS OF IDENTIFICATION 审中-公开
标题翻译：药物可接受的MGLUR5阳性免疫调节剂及其鉴定方法
公开(公告)号：WO2013045380A2
公开(公告)日：2013-04-04
申请号：PCT/EP2012/068737
申请日：2012-09-24
申请人： F. HOFFMANN-LA ROCHE AG , BIEMANS, Barbara , JAESCHKE, Georg , LINDEMANN, Lothar , MUSTER, Wolfgang , STADLER, Heinz , VIEIRA, Eric
发明人： BIEMANS, Barbara , JAESCHKE, Georg , LINDEMANN, Lothar , MUSTER, Wolfgang , STADLER, Heinz , VIEIRA, Eric
IPC分类号： A61K31/44 , A61K31/4439 , A61K31/4545 , A61K31/497 , A61K31/506 , A61K31/519 , A61P7/00 , A61P9/00 , A61P13/10 , A61P21/00 , A61P25/00 , A61P25/06 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/34 , A61P25/36 , A61P29/00 , A61P43/00
CPC分类号： A61K31/5377 , A61K31/44 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/497 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/5355 , G01N33/5041 , G01N33/5088 , G01N33/74 , G01N33/9406 , G01N2333/70571
摘要： The present invention relates to mGluR5 positive allosteric modulators (PAM) and methods for identifying pharmaceutically acceptable compounds with high tolerability and safety, which method comprises the use of at least one non-competitive mGluR5 allosteric modulator which has a shift factor measured at 10 uM glutamate concentration below 3.0.
摘要翻译：本发明涉及mGluR5阳性变构调节剂（PAM）以及用于鉴定具有高耐受性和安全性的药学上可接受的化合物的方法，该方法包括使用至少一种非竞争性mGluR5变构调节剂，其具有在10μM谷氨酸测量的移位因子浓度在3.0以下。

10. 发明申请

WO2011006910A1 IMIDAZOLE DERIVATIVES AS MGLUR5 ANTAGONISTS 审中-公开
标题翻译：咪唑衍生物作为MGLUR5拮抗剂
公开(公告)号：WO2011006910A1
公开(公告)日：2011-01-20
申请号：PCT/EP2010/060097
申请日：2010-07-14
申请人： F. HOFFMANN-LA ROCHE AG , JAESCHKE, Georg , LINDEMANN, Lothar , VIEIRA, Eric , WICHMANN, Juergen
发明人： JAESCHKE, Georg , LINDEMANN, Lothar , VIEIRA, Eric , WICHMANN, Juergen
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , A61K31/4439 , A61P25/00
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04
摘要： The present invention relates to imidazole derivatives of the general formula (I) wherein R 1 signifies halogen, lower alkyl or lower alkoxy; R 2 signifies lower alkyl, lower hydro xyalkyl or lower alkoxyalkyl; R 3 signifies hydrogen, lower alkyl, lower hydroxyalkyl or alkoxyalkyl; Q signifies either -N= or -CH=; R 4 is a group of formula IIa or lIb (formula IIa and IIb) wherein X, Y and Z independently are -CH= or -N=, and whereby only one of X or Y can be a nitrogen atom; R 5 and R 6 independently are hydrogen, lower alkyl, lower hydroxyalkyl, lower alkoxyalkyl, -(CH 2 ) m -(CO)O-lower alkyl, -(CH 2 ) m -S(O) 2 -lower alkyl, -(CH 2 ) m -C(O)-NR'R" and where m = 0-3 and R' and R'' are independently hydrogen or lower alkyl; as well as to pharmaceutically acceptable salts thereof. It has now surprisingly been found that the compounds of general formula (I) are metabotropic glutamate receptor antagonists. They can be used in the treatment or prevention of mGluR5 receptor mediated disorders.
摘要翻译：本发明涉及通式（I）的咪唑衍生物，其中R1表示卤素，低级烷基或低级烷氧基; R2表示低级烷基，低级羟基烷基或低级烷氧基烷基; R3表示氢，低级烷基，低级羟烷基或烷氧基烷基; Q表示-N =或-CH =; R4是式IIa或IIIb（式IIa和IIb）的基团，其中X，Y和Z独立地是-CH =或-N =，并且其中X或Y中只有一个可以是氮原子; （CH2）m-（CO）O-低级烷基， - （CH2）mS（O）2-低级烷基， - （CH2）mC（O））-NR'R“，其中m = 0-3，并且R'和R”独立地为氢或低级烷基;以及其药学上可接受的盐。现在令人惊奇地发现，通式（I ）是代谢型谷氨酸受体拮抗剂，可用于治疗或预防mGluR5受体介导的疾病。

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