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1. 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）。

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

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）。

5. 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。

6. 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。

7. 发明申请

WO2018015235A1 ETHYNYL DERIVATIVES 审中-公开
标题翻译：乙炔衍生物
公开(公告)号：WO2018015235A1
公开(公告)日：2018-01-25
申请号：PCT/EP2017/067495
申请日：2017-07-12
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BIEMANS, Barbara , JAESCHKE, Georg , RICCI, Antonio , RUEHER, Daniel , O`HARA, Fionn
IPC分类号： C07D487/10 , A61K31/527 , A61P25/16
摘要： The present invention relates to compounds of formulas IA and IB IA IB 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. The compounds may be used in the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.
摘要翻译：本发明涉及式IA和IBA1B化合物或其药学上可接受的盐或酸加成盐，外消旋混合物或其相应的对映异构体和/或光学异构体和/或其立体异构体。这些化合物可用于治疗帕金森病，焦虑症，呕吐，强迫症，自闭症，神经保护，癌症，抑郁症和2型糖尿病。

8. 发明申请

WO2014060394A1 ETHYNYL DERIVATIVES AS MODULATORS OF MGLUR5 RECEPTOR ACTIVITY 审中-公开
标题翻译：作为MGLUR5受体活性调节剂的乙烯衍生物
公开(公告)号：WO2014060394A1
公开(公告)日：2014-04-24
申请号：PCT/EP2013/071493
申请日：2013-10-15
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： JAESCHKE, Georg , LINDEMANN, Lothar , RICCI, Antonio , RUEHER, Daniel , STADLER, Heinz , VIEIRA, Eric
IPC分类号： C07D213/81 , A61K31/44 , A61K31/444 , A61P25/24 , A61P25/16 , A61P1/00
CPC分类号： C07D213/81
摘要： The present invention relates to ethynyl derivatives of formula (I) 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 metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of anxiety and pain, depression, Fragile-X syndrom, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).
摘要翻译：本发明涉及式（I）的乙炔基衍生物或其药学上可接受的酸加成盐，涉及外消旋混合物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。现在令人惊奇地发现，通式（I）的化合物是代谢型谷氨酸受体拮抗剂（负变构调节剂），用于治疗焦虑和疼痛，抑郁症，脆性-X综合征，自闭症谱系障碍，帕金森病和胃食管反流病（GERD）。

9. 发明申请

WO2014060384A1 ETHYNYL DERIVATIVES AS MODULATORS OF MGLUR5 RECEPTOR ACTIVITY 审中-公开
标题翻译：作为MGLUR5受体活性调节剂的乙烯衍生物
公开(公告)号：WO2014060384A1
公开(公告)日：2014-04-24
申请号：PCT/EP2013/071476
申请日：2013-10-15
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： JAESCHKE, Georg , LINDEMANN, Lothar , RICCI, Antonio , RUEHER, Daniel , STADLER, Heinz , VIEIRA, Eric
IPC分类号： C07D213/81 , A61K31/44 , A61P25/24 , A61P25/16 , A61P1/00
CPC分类号： C07D213/81 , C07D239/28
摘要： The present invention relates to ethynyl derivatives of formula (I) wherein Y is N or CH R 1 is fluoro or chloro 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 metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of anxiety and pain, depression, Fragile-X syndrom, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD)
摘要翻译：本发明涉及式（I）的炔基衍生物，其中Y是N或CHR 1是氟或氯或可药用酸加成盐，与外消旋混合物或其相应的对映体和/或旋光异构体和/或其立体异构体。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拮抗剂（负变构调节剂），用于治疗焦虑和疼痛，抑郁症，脆性-X综合征，自闭症谱系障碍，帕金森病和胃食管反流病（GERD）

10. 发明申请

WO2020254546A1 NEW EGFR INHIBITORS 审中-公开
公开(公告)号：WO2020254546A1
公开(公告)日：2020-12-24
申请号：PCT/EP2020/067055
申请日：2020-06-19
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： DOLENTE, Cosimo , GOERGLER, Annick , HEWINGS, David Stephen , JAESCHKE, Georg , KUHN, Bernd , NAGEL, Yvonne Alice , NORCROSS, Roger David , OBST-SANDER, Christa Ulrike , RICCI, Antonio , RUEHER, Daniel , STEINER, Sandra
IPC分类号： A61P35/00 , C07D417/14 , A61K31/427
摘要： The invention provides novel compounds as described herein, compositions including the compounds and methods of using the compounds.

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