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1. 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。

2. 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。

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

WO2006128803A1 PIPERIDIN-4-YL-AMIDE DERIVATIVES AND THEIR USE AS SST RECEPTOR SUBTYPE 5 ANTAGONISTS 审中-公开
标题翻译：哌啶-4-基酰胺衍生物及其作为SST受体亚型5拮抗剂
公开(公告)号：WO2006128803A1
公开(公告)日：2006-12-07
申请号：PCT/EP2006/062515
申请日：2006-05-23
申请人： F. HOFFMANN-LA ROCHE AG , BINGGELI, Alfred , CHRIST, Andreas , GREEN, Luke Gideon Granville , GUBA, Wolfgang , MAERKI, Hans-Peter , MARTIN, Rainer Eugen , MOHR, Peter
发明人： BINGGELI, Alfred , CHRIST, Andreas , GREEN, Luke Gideon Granville , GUBA, Wolfgang , MAERKI, Hans-Peter , MARTIN, Rainer Eugen , MOHR, Peter
IPC分类号： C07D401/14 , C07D413/14 , C07D401/12 , C07D211/58 , A61K31/4468 , A61K31/506 , A61K31/5375 , A61P3/10 , C07D407/12 , C07D401/10
CPC分类号： C07D211/58 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/14
摘要： This invention is concerned with compounds of the formula (1) wherein R 1 to R 5 , R 5' and A are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
摘要翻译：本发明涉及式（1）的化合物，其中R 1至R 5，R 5'和A如在说明书和权利要求书及其药学上可接受的盐。本发明还涉及含有这些化合物的药物组合物，其制备方法及其用于治疗和/或预防与调节SST受体亚型5相关的疾病的用途。

5. 发明申请

WO2006094682A1 BENZOTHIAZOLE, THIAZOLOPYRIDINE, BENZOOXAZOLE AND OXAZOLOPYRIDINE DERIVATIVES AS ANTIDIABETIC COMPOUNDS 审中-公开
标题翻译：苯并噻唑，噻唑啉，苯并唑和氧杂环丁啶衍生物作为抗菌化合物
公开(公告)号：WO2006094682A1
公开(公告)日：2006-09-14
申请号：PCT/EP2006/001843
申请日：2006-02-28
申请人： F. HOFFMANN-LA ROCHE AG , BINGGELI, Alfred , CHRIST, Andreas, Dominik , GREEN, Luke, Gideon, Granville , GUBA, Wolfgang , MAERKI, Hans-Peter , MARTIN, Rainer, Eugen , MOHR, Peter
发明人： BINGGELI, Alfred , CHRIST, Andreas, Dominik , GREEN, Luke, Gideon, Granville , GUBA, Wolfgang , MAERKI, Hans-Peter , MARTIN, Rainer, Eugen , MOHR, Peter
IPC分类号： C07D513/04 , C07D498/04 , C07D417/12 , C07D413/12 , C07D277/82 , C07D263/58 , A61K31/4468 , A61P3/10
CPC分类号： C07D413/14 , C07D263/58 , C07D277/82 , C07D413/12 , C07D417/12 , C07D417/14 , C07D513/04
摘要： This invention is concerned with compounds of the formula (I) wherein A, B 1 , B 2 , R 1 , R 2 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
摘要翻译：本发明涉及式（I）的化合物，其中A，B 1，B 2，R 1，R 2， G和G如说明书和权利要求书中所定义，及其药学上可接受的盐。本发明还涉及含有这些化合物的药物组合物，其制备方法及其用于治疗和/或预防与调节SST受体亚型5有关的疾病的用途。

6. 发明申请

WO2007025897A2 BENZOOXAZOLE, OXAZOLOPYRIDINE, BENZOTHIAZOLE AND THIAZOLOPYRIDINE DERIVATIVES 审中-公开
标题翻译：苯唑唑，氧杂吡咯烷，苯并噻唑和噻唑吡啶衍生物
公开(公告)号：WO2007025897A2
公开(公告)日：2007-03-08
申请号：PCT/EP2006/065522
申请日：2006-08-21
申请人： F. HOFFMANN-LA ROCHE AG , BINGGELI, Alfred , CHRIST, Andreas, D. , GREEN, Luke , GUBA, Wolfgang , MAERKI, Hans, P. , MARTIN, Rainer, E. , MOHR, Peter
发明人： BINGGELI, Alfred , CHRIST, Andreas, D. , GREEN, Luke , GUBA, Wolfgang , MAERKI, Hans, P. , MARTIN, Rainer, E. , MOHR, Peter
IPC分类号： C07D413/12 , C07D413/14 , C07D498/04 , C07D417/12 , C07D417/14 , A61P3/10
CPC分类号： C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： This invention is concerned with compounds of the formula (I) wherein X, A, B, R 1 , R 2 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to then- use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
摘要翻译：本发明涉及式（I）的化合物，其中X，A，B，R 1，R 2和G如说明书和权利要求中所定义，以及其药学上可接受的盐。本发明还涉及含有这些化合物的药物组合物，其制备方法，然后用于治疗和/或预防与调节SST受体亚型5有关的疾病。

7. 发明申请

WO2011138293A1 2,5,6,7-TETRAHYDRO-[1,4]OXAZEPIN-3-YLAMINE OR 2,3,6,7-TETRAHYDRO-[1,4]OXAZEPIN-5-YLAMINE COMPOUNDS 审中-公开
标题翻译： 2,5,6,7-四氢 - [1,4]氧杂环己烯-3-基胺或2,3,6,7-四氢 - [1,4]氧杂环己烯-5-胺化合物
公开(公告)号：WO2011138293A1
公开(公告)日：2011-11-10
申请号：PCT/EP2011/056990
申请日：2011-05-03
申请人： F. HOFFMANN-LA ROCHE AG , SIENA BIOTECH S.P.A. , BANNER, David , GUBA, Wolfgang , HILPERT, Hans , HUMM, Roland , MAUSER, Harald , MAYWEG, Alexander, V. , NARQUIZIAN, Robert , POWER, Eoin , ROGERS-EVANS, Mark , ROMBACH, Didier , WOLTERING, Thomas , WOSTL, Wolfgang
发明人： BANNER, David , GUBA, Wolfgang , HILPERT, Hans , HUMM, Roland , MAUSER, Harald , MAYWEG, Alexander, V. , NARQUIZIAN, Robert , POWER, Eoin , ROGERS-EVANS, Mark , ROMBACH, Didier , WOLTERING, Thomas , WOSTL, Wolfgang
IPC分类号： C07D267/10 , C07D413/12 , C07D417/12 , A61K31/553 , A61P25/28
CPC分类号： C07D267/10 , C07D413/12 , C07D417/12
摘要： This invention relates to compounds of the formula (I), wherein A, B and R 1 to R 7 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE1 and/or BACE2 inhibitors and can be used as 5 medicaments for the therapeutic and/or prophylactic treatment of diseases such as Alzheimer's disease, diabetes, particularly type 2 diabetes, and other metabolic disorders.
摘要翻译：本发明涉及式（I）化合物，其中A，B和R 1至R 7如下所述，或其药学上可接受的盐。这些化合物是BACE1和/或BACE2抑制剂，可用作5种药物用于治疗和/或预防性治疗诸如阿尔茨海默病，糖尿病，特别是2型糖尿病和其它代谢疾病的疾病。

8. 发明申请

WO2009103626A1 4, 5-DIHYDRO-OXAZOL-2-YL AMINE DERIVATIVES 审中-公开
标题翻译： 4,5-二氢 - 氧杂-2-氨基胺衍生物
公开(公告)号：WO2009103626A1
公开(公告)日：2009-08-27
申请号：PCT/EP2009/051452
申请日：2009-02-09
申请人： F. HOFFMANN-LA ROCHE AG , SIENA BIOTECH S.P.A , ANDREINI, Matteo , GABELLIERI, Emanuele , GUBA, Wolfgang , MARCONI, Guido , NARQUIZIAN, Robert , POWER, Eoin , TRAVAGLI, Massimiliano , WOLTERING, Thomas , WOSTL, Wolfgang
发明人： ANDREINI, Matteo , GABELLIERI, Emanuele , GUBA, Wolfgang , MARCONI, Guido , NARQUIZIAN, Robert , POWER, Eoin , TRAVAGLI, Massimiliano , WOLTERING, Thomas , WOSTL, Wolfgang
IPC分类号： C07D263/28 , C07D413/10 , A61K31/422 , A61P25/28
CPC分类号： C07D263/28 , C07D413/10
摘要： The present invention relates to a compounds of formula I or a pharmaceutically active acid addition salts thereof. It has been found that the present compounds have Asp2 (β-sccretasc, BACE 1 or Mcmapsin-2) inhibitory activity and that the compounds may therefore be used in the treatment of diseases characterised by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.
摘要翻译：本发明涉及式I化合物或其药学活性的酸加成盐。已经发现本发明化合物具有Asp2（β-sccretasc，BACE1或Mcmapsin-2）的抑制活性，因此该化合物可用于治疗以β淀粉样蛋白升高或β-淀粉样蛋白沉积为特征的疾病，特别是阿尔茨海默病。

9. 发明申请

WO2012019966A1 1,4,5,6-TETRAHYDRO-PYRIMIDIN-2-YLAMINE COMPOUNDS 审中-公开
标题翻译： 1,4,5,6-四氢吡啶-2-基胺化合物
公开(公告)号：WO2012019966A1
公开(公告)日：2012-02-16
申请号：PCT/EP2011/063498
申请日：2011-08-05
申请人： F. HOFFMANN-LA ROCHE AG , SIENA BIOTECH S.P.A , BANNER, David , GABELLIERI, Emanuele , GUBA, Wolfgang , HILPERT, Hans , HORNSPERGER, Benoit , HUMM, Roland , MAUSER, Harald , MAYWEG, Alexander, V. , NARQUIZIAN, Robert , PINARD, Emmanuel , ROGERS-EVANS, Mark , WOLTERING, Thomas , WOSTL, Wolfgang
发明人： BANNER, David , GABELLIERI, Emanuele , GUBA, Wolfgang , HILPERT, Hans , HORNSPERGER, Benoit , HUMM, Roland , MAUSER, Harald , MAYWEG, Alexander, V. , NARQUIZIAN, Robert , PINARD, Emmanuel , ROGERS-EVANS, Mark , WOLTERING, Thomas , WOSTL, Wolfgang
IPC分类号： C07D239/22 , C07D239/70 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , A61K31/513 , A61P3/10
CPC分类号： C07D417/12 , A61K31/513 , C07D239/22 , C07D239/70 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： This invention relates to compounds of the formula wherein R 1 to R 9 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as diabetes, particularly type 2 diabetes, and other metabolic disorders.
摘要翻译：本发明涉及下式化合物或其药学上可接受的盐：其中R 1至R 9如下所述。这些化合物是BACE2抑制剂，可用作治疗和/或预防性治疗诸如糖尿病，特别是2型糖尿病和其它代谢疾病的药物。

10. 发明申请

WO2011069934A1 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：作为BACE 1和/或BACE 2抑制剂的2-氨基-5,5-二氟-5,6-二氢-4H-氧化物
公开(公告)号：WO2011069934A1
公开(公告)日：2011-06-16
申请号：PCT/EP2010/068912
申请日：2010-12-06
申请人： F. HOFFMANN-LA ROCHE AG , SIENA BIOTECH S.P.A. , BANNER, David , GUBA, Wolfgang , HILPERT, Hans , MAUSER, Harald , MAYWEG, Alexander, V. , NARQUIZIAN, Robert , PINARD, Emmanuel , POWER, Eoin , ROGERS-EVANS, Mark , WOLTERING, Thomas , WOSTL, Wolfgang
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.
摘要翻译：本发明涉及具有BACE1和/或其衍生物的式（I）的2-氨基-5,5-二氟-5,6-二氢-4H- [1,3]恶嗪-4-基） - 苯基] BACE2抑制活性，其制备，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。阿尔茨海默病和2型糖尿病。

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