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11. 发明公开

EP2513102A1 ETHYNYL DERIVATIVES 有权
标题翻译：乙炔衍生物
公开(公告)号：EP2513102A1
公开(公告)日：2012-10-24
申请号：EP10790960.8
申请日：2010-12-14
申请人： F.Hoffmann-La Roche AG
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-R 2; Z是CH或N; R 4是含有0,1或2个氮原子的6元芳族取代基，其任选被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为氢，低级烷基，低级烷氧基，羟基，低级羟烷基，低级环烷基或任选被羟基或烷氧基取代的杂环烷基; R 2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，外消旋混合物，或其相应的对映异构体和/或旋光异构体和/或立体异构体。现在令人惊讶地发现通式（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。

12. 发明公开

EP3049409A1 ETHYNYL DERIVATIVES 有权
标题翻译：乙炔衍生物
公开(公告)号：EP3049409A1
公开(公告)日：2016-08-03
申请号：EP14781474.3
申请日：2014-09-22
申请人： F.Hoffmann-La Roche AG
发明人： BIEMANS, Barbara , GUBA, Wolfgang , JAESCHKE, Georg , RICCI, Antonio , RUEHER, Daniel , VIEIRA, Eric
IPC分类号： C07D405/14 , C07D401/04 , C07D401/10 , C07D405/04 , C07D239/91 , C07D471/04 , C07D473/04 , C07D487/04 , C07D495/04 , C07D513/04 , A61K31/517 , A61P3/10 , A61P25/10 , A61P25/22 , A61P25/24
CPC分类号： C07D239/96 , C07D239/91 , C07D401/04 , C07D401/10 , C07D405/04 , C07D405/14 , C07D471/04 , C07D473/04 , C07D475/02 , C07D475/04 , C07D487/04 , C07D487/06 , C07D495/04 , C07D513/04
摘要： The present invention relates to compounds of formula I wherein Y is N or C-R
1' ; G is a 5 or 6-membered aromatic or heteroaromatic ring containing 0, 1, 2 or 3 heteroatoms, selected from the group consisting of phenyl, pyridinyl with different N-positions, imidazolyl, pyrazinyl, pyrimidinyl, thiophenyl, thiazolyl, pyrazolyl or thiadiazolyl, which are optionally substituted by 1, 2 or 3 substituents, selected from the group consisting of halogen, lower alkyl, lower alkoxy, lower alkoxy substituted by halogen or NRR'; R and R' are independently from each other hydrogen or lower alkyl, or may form together with the N atom to which they are attached a five or six membered saturated heterocyclic group which may contain an additional oxygen, NH, or N-lower alkyl group; R
1 is hydrogen, halogen or lower alkyl substituted by halogen; R
1' is hydrogen, halogen or lower alkyl substituted by halogen; R
2 is hydrogen, lower alkyl, lower alkoxyalkyl, cycloalkyl or heterocycloalkyl; or R
2 may form together with the closest carbon atom in group G a group (IA) for A being -CH
2 -, -CH
2 CH
2 , or -C(CH
3 )
2 -, R
3 is phenyl or pyridinyl, wherein the N atom in the pyridinyl group may be in different positions; 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 been surprisingly been found that the compounds of general formula I are positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGluR4), useful for the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.
摘要翻译：本发明涉及其中Y是N或C-R'的式I化合物; G是含有0,1,2或3个选自苯基，具有不同N-位的吡啶基，咪唑基，吡嗪基，嘧啶基，噻吩基，噻唑基，吡唑基或噻二唑基的5或6元芳族或杂芳族环其任选被1,2或3个选自卤素，低级烷基，低级烷氧基，被卤素或NRR'取代的低级烷氧基的取代基取代; R和R'彼此独立地为氢或低级烷基，或者可以与它们所连接的N原子一起形成可含有另外的氧，NH或N-低级烷基的五元或六元饱和杂环基 ; R 1是氢，卤素或被卤素取代的低级烷基; R 1'是氢，卤素或被卤素取代的低级烷基; R 2是氢，低级烷基，低级烷氧基烷基，环烷基或杂环烷基; 或者R 2可与G组中最接近的碳原子一起形成A为-CH 2 - ， - CH 2 CH 2或-C（CH 3）2 - ，R 3为苯基或吡啶基的基团（IA），其中吡啶基中的N原子可以位于不同的位置; 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/或旋光异构体和/或立体异构体。令人惊讶地发现，通式I的化合物是代谢型谷氨酸受体4（mGluR4）的正变构调节剂（PAM），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。

13. 发明公开

EP2948446A1 FLUORO-[1,3]OXAZINES AS BACE1 INHIBITORS 审中-公开
标题翻译：氟 - [1,3]奥沙星ALS BACE1-HEMMER
公开(公告)号：EP2948446A1
公开(公告)日：2015-12-02
申请号：EP14700493.1
申请日：2014-01-15
申请人： F.Hoffmann-La Roche AG , Siena Biotech S.p.a.
发明人： WOLTERING, Thomas , GUBA, Wolfgang , HILPERT, Hans , KUGLSTATTER, Andreas , LIMBERG, Anja , OBST SANDER, Ulrike , PINARD, Emmanuel , WOSTL, Wolfgang
IPC分类号： C07D413/14 , C07D413/10 , C07D413/12 , A61K31/5355 , A61P25/28
CPC分类号： C07D413/14 , C07D413/04 , C07D413/10 , C07D413/12
摘要： The present invention provides a compound of formula I having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
摘要翻译：本发明提供具有BACE1抑制活性的式I化合物，其制备方法，含有它们的药物组合物及其作为治疗活性物质的用途。本发明的活性化合物可用于例如治疗和/或预防性治疗。阿尔茨海默氏病。

14. 发明公开

EP2686307A1 1,4-OXAZEPINES AS BACE1 AND/OR BACE2 INHIBITORS 审中-公开
标题翻译： 1,4-氧氮杂ALS BACE1-和/或BACE2，缝边
公开(公告)号：EP2686307A1
公开(公告)日：2014-01-22
申请号：EP12709616.2
申请日：2012-03-15
申请人： F.Hoffmann-La Roche AG , Siena Biotech S.p.a.
发明人： GABELLIERI, Emanuele , GUBA, Wolfgang , HILPERT, Hans , MAUSER, Harald , MAYWEG, Alexander V. , ROGERS-EVANS, Mark , ROMBACH, Didier , THOMAS, Andrew , WOLTERING, Thomas , WOSTL, Wolfgang
IPC分类号： C07D267/10 , C07D413/12 , A61K31/553 , A61P25/28 , A61P3/10
CPC分类号： C07D267/10 , C07D413/12
摘要： The present invention relates to 1,4-Oxazepines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.

15. 发明公开

EP2665713A1 1,4 OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS 审中-公开
标题翻译： 1,4恶唑作为BACE1和/或BACE2抑制剂
公开(公告)号：EP2665713A1
公开(公告)日：2013-11-27
申请号：EP12700341.6
申请日：2012-01-16
申请人： F.Hoffmann-La Roche AG , Siena Biotech S.p.a.
发明人： ANDREINI, Matteo , GABELLIERI, Emanuele , GUBA, Wolfgang , HILPERT, Hans , MAUSER, Harald , MAYWEG, Alexander V. , NARQUIZIAN, Robert , POWER, Eoin , TRAVAGLI, Massimiliano , WOLTERING, Thomas , WOSTL, Wolfgang
IPC分类号： C07D265/30 , C07D413/12 , A61K31/5375 , A61K31/5377 , A61P3/10
CPC分类号： C07D265/30 , C07D413/12
摘要： The present invention relates to 1,4 Oxazines of formula (I): having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
摘要翻译：本发明涉及式（I）的1,4嗪：具有BACE1和/或BACE2抑制活性，它们的制造方法，含有它们的药物组合物以及它们作为治疗活性物质的用途。本发明的活性化合物可用于例如治疗和/或预防性治疗。阿尔茨海默病和2型糖尿病。

16. 发明公开

EP2509965A1 2-AMINO-5, 5-DIFLUORO-5, 6-DIHYDRO-4H-OXAZINES AS BACE 1 AND/OR BACE 2 INHIBITORS 审中-公开
标题翻译： 2-氨基-5,5-二氟-5,6-二氢-4H-恶嗪AS BACE 1和/或2 BACE抑制剂
公开(公告)号：EP2509965A1
公开(公告)日：2012-10-17
申请号：EP10785437.4
申请日：2010-12-06
申请人： F.Hoffmann-La Roche AG , Siena Biotech S.p.a.
发明人： BANNER, David , GUBA, Wolfgang , HILPERT, Hans , MAUSER, Harald , MAYWEG, Alexander, V. , NARQUIZIAN, Robert , PINARD, Emmanuel , POWER, Eoin , ROGERS-EVANS, Mark , WOLTERING, Thomas , WOSTL, Wolfgang
IPC分类号： C07D265/08 , C07D413/12 , A61K31/535 , A61K31/5355
CPC分类号： C07D265/08 , C07D413/12
摘要： The present invention relates to 2-Amino-5,5-difluoro-5,6-dihydro-4H-[1,3]oxazin-4-yl)- phenyl]-amide derivatives of formula (I) having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.

17. 发明公开

EP2467368A1 3-AMINO-5-PHENYL-5,6-DIHYDRO-2H-[1,4]OXAZINE DERIVATIVES 审中-公开
标题翻译： 3-氨基-5-苯基-5,6-二氢-2H- [1,4]恶嗪衍生物
公开(公告)号：EP2467368A1
公开(公告)日：2012-06-27
申请号：EP10742166.1
申请日：2010-08-16
申请人： F.Hoffmann-La Roche AG , Siena Biotech S.p.a.
发明人： ANDREINI, Matteo , BANNER, David , GUBA, Wolfgang , HILPERT, Hans , MAUSER, Harald , MAYWEG, Alexander, V. , NARQUIZIAN, Robert , POWER, Eoin , ROGERS-EVANS, Mark , TRAVAGLI, Massimiliano , VALACCHI, Michela , WOLTERING, Thomas , WOSTL, Wolfgang , GABALLIERI, Emanuele
IPC分类号： C07D265/30 , C07D413/12 , A61K31/5377
CPC分类号： C07D413/12 , C07D265/30 , C07D413/14 , C07D417/12 , C07D471/04
摘要： The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[l,4]oxazine derivatives of formula (I) having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.

18. 发明授权

EP1532132B1 NOVEL BENZODIOXOLES 有权
标题翻译：新benzodioxoles
公开(公告)号：EP1532132B1
公开(公告)日：2008-03-19
申请号：EP03766236.8
申请日：2003-07-18
申请人： F.HOFFMANN-LA ROCHE AG
发明人： ALANINE, Alexander , BLEICHER, Konrad , GUBA, Wolfgang , HAAP, Wolfgang , KUBER, Dagmar , LUEBBERS, Thomas , PLANCHER, Jean-Marc , ROGERS-EVANS, Mark , SCHNEIDER, Gisbert , ZUEGGE, Jochen , ROCHE, Olivier
IPC分类号： C07D317/62 , C07D405/12 , C07D317/54 , C07D451/06 , A61K31/36
CPC分类号： C07D317/46 , C07D317/72 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D417/06 , C07D451/06 , C07D491/10
摘要： The present invention relates to compound of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, and X are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases, which are associated with the modulation of CB1 receptors.

19. 发明公开

EP1532132A1 NOVEL BENZODIOXOLES 有权
标题翻译：新型苯并二氧戊环
公开(公告)号：EP1532132A1
公开(公告)日：2005-05-25
申请号：EP03766236.8
申请日：2003-07-18
申请人： F.HOFFMANN-LA ROCHE AG
发明人： ALANINE, Alexander , BLEICHER, Konrad , GUBA, Wolfgang , HAAP, Wolfgang , KUBE, Dagmar , LUEBBERS, Thomas , PLANCHER, Jean-Marc , ROGERS-EVANS, Mark , SCHNEIDER, Gisbert , ZUEGGE, Jochen , ROCHE, Olivier
IPC分类号： C07D317/62 , C07D405/12 , C07D317/54 , C07D451/06 , A61K31/36
CPC分类号： C07D317/46 , C07D317/72 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D417/06 , C07D451/06 , C07D491/10
摘要： The present invention relates to compound of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, and X are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases, which are associated with the modulation of CB1 receptors.
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和X如说明书和权利要求书中所定义。这些化合物可用于治疗和/或预防与CB1受体调节有关的疾病。

20. 发明公开

EP2558457A1 ARYLETHYNYL DERIVATIVES 有权
标题翻译：基乙炔衍
公开(公告)号：EP2558457A1
公开(公告)日：2013-02-20
申请号：EP11713288.6
申请日：2011-04-11
申请人： F.Hoffmann-La Roche AG
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 compounds of formula I wherein R1, R2, R2′, R3, R3′, R4, R4′, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).

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