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1. 发明申请

WO2011101304A2 PIPERIDINE DERIVATIVES 审中-公开
标题翻译：哌啶衍生物
公开(公告)号：WO2011101304A2
公开(公告)日：2011-08-25
申请号：PCT/EP2011/052101
申请日：2011-02-14
申请人： F. HOFFMANN-LA ROCHE AG , BAUMANN, Karlheinz , FLOHR, Alexander , GOETSCHI, Erwin , GREEN, Luke , JOLIDON, Synese , KNUST, Henner , LIMBERG, Anja , LUEBBERS, Thomas , THOMAS, Andrew
发明人： BAUMANN, Karlheinz , FLOHR, Alexander , GOETSCHI, Erwin , GREEN, Luke , JOLIDON, Synese , KNUST, Henner , LIMBERG, Anja , LUEBBERS, Thomas , THOMAS, Andrew
IPC分类号： C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/04 , A61K31/4523 , A61P25/28
CPC分类号： C07D471/04 , C07D401/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D498/04
摘要： The invention relates to compounds of formula (I). Hetaryl I is a five or six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N; hetaryl II is a five or six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N, or is a two membered ring system containing 1 to 4 heteroatoms selected from S, O or N, wherein at least one ring is aromatic in nature; R 1 is lower alkyl, lower alkoxy, lower alkyl substituted by halogen, or halogen; R 2 is halogen, lower alkyl, lower alkoxy, hydroxy, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy or benzo[1,3]dioxolyl, or is -(CHR) p -phenyl, optionally substituted by halogen, lower alkyl, lower alkoxy, S(O) 2 -lower alkyl, cyano, nitro, lower alkoxy substituted by halogen, dimethylamino, -(CH 2 )P-NHC(O)O-Iower alkyl, or lower alkyl substituted by halogen, and R is hydrogen, halogen, hydroxy or lower alkoxy, or is cycloalkenyl or cycloalkyl, optionally substituted by hydroxy or lower alkyl substituted by halogen, or is a five or six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N, which is optionally substituted by halogen, lower alkyl, lower alkoxy or dimethylamino, or is O-phenyl, optionally substituted by halogen, or is heterocycloalkyl, optionally substituted by halogen, hydroxy, lower alkyl substituted by halogen or C(O)O-lower alkyl; R 3 is hydrogen, lower alkyl, cyano or phenyl; R 4 is lower alkoxy, lower alkyl or halogen; p is 0 or 1; n is 0, 1 or 2; if n is 2 then R 4 may be the same or different; m is 0, 1 or 2; if m is 2 then R 1 may be the same or different; o is 0, 1, 2 or 3, if o is 2 or 3 then R 2 may be the same or different; or to pharmaceutically active acid addition salts thereof. The compounds of formula (I) are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
摘要翻译：本发明涉及式（I）的化合物。 Hetary11是含有1至3个选自O，S或N的杂原子的五元或六元杂芳基; 杂芳基II是含有1至3个选自O，S或N的杂原子的五元或六元杂芳基，或者是含有1至4个选自S，O或N的杂原子的二元环体系，其中至少一个环本质上是芳香的; R 1为低级烷基，低级烷氧基，被卤素取代的低级烷基或卤素; R 2是卤素，低级烷基，低级烷氧基，羟基，被卤素取代的低级烷基，被羟基或苯并[1,3]二氧杂环戊烯基取代的低级烷基，或者是 - （CHR）p 低级烷基，低级烷氧基，S（O）2 - 低级烷基，氰基，硝基，被卤素取代的低级烷氧基，二甲基氨基， - （CH 2）（O）O-低级烷基或被卤素取代的低级烷基，且R为氢，卤素，羟基或低级烷氧基，或者为环烯基或环烷基，任选被羟基或低级被卤素取代的烷基，或者是含有1至3个选自O，S或N的杂原子的五元或六元杂芳基，其任选被卤素，低级烷基，低级烷氧基或二甲基氨基取代，或者是O-苯基，任选被卤素取代，或者为任选被卤素，羟基，被卤素取代的低级烷基或C（O）O-低级烷基取代的杂环烷基; R 3是氢，低级烷基，氰基或苯基; R 4是低级烷氧基，低级烷基或卤素; p是0或1; n是0,1或2; 如果n是2，则R 4可以相同或不同; m是0,1或2; 如果m是2，则R 1可以相同或不同; o是0,1,2或3，如果o是2或3，则R 2可以相同或不同; 或其药学活性酸加成盐。式（I）化合物是β-淀粉样蛋白的调节剂，因此它们可用于治疗或预防与β-淀粉状蛋白在脑中沉积相关的疾病，特别是阿尔茨海默氏病和其他疾病，如脑具有淀粉样变性的遗传性脑出血，荷兰型（HCHWA-D），多发性梗塞型痴呆，拳击员痴呆和唐氏综合症。

2. 发明申请

WO2009087127A1 MODULATORS FOR AMYLOID BETA 审中-公开
标题翻译： AMYLOID BETA的调节剂
公开(公告)号：WO2009087127A1
公开(公告)日：2009-07-16
申请号：PCT/EP2009/050036
申请日：2009-01-05
申请人： F. HOFFMANN-LA ROCHE AG , BAUMANN, Karlheinz , FLOHR, Alexander , GOETSCHI, Erwin , JACOBSEN, Helmut , JOLIDON, Synese , LUEBBERS, Thomas
发明人： BAUMANN, Karlheinz , FLOHR, Alexander , GOETSCHI, Erwin , JACOBSEN, Helmut , JOLIDON, Synese , LUEBBERS, Thomas
IPC分类号： C07D277/60 , C07D401/14 , C07D403/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/052 , C07D513/04 , C07D491/113 , A61P25/28 , A61K31/428 , A61K31/517 , A61K31/519 , A61K31/527
CPC分类号： C07D417/12 , C07D277/82 , C07D401/14 , C07D403/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D491/052 , C07D491/113 , C07D513/04 , C07F7/1856
摘要： The invention relates to compounds of formula (I) R 1 is -C(O)O-lower alkyl, cyano or is hetaryl; hetaryl is a five-or six membered heteraryl group, optionally substituted by R'; R' is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy or lower alkoxy substituted by halogen; R 2 is hydrogen, lower alkoxy, lower alkyl, halogen or cyano; R 3 is -(CH 2 ) n -C(O)O-lower alkyl, lower alkyl, lower alkoxy, hydroxy, -O-Si(CH 3 ) 2 -lower alkyl, -C(O)-N(lower alkyl) 2 , -O-S(O) 2 -lower alkyl, C 3-7 -cycloalkyl, S(O) 2 -aryl, heterocyclyl, -C(O)-heterocyclyl, or is aryl or hetaryl, which aryl or hetaryl rings are optionally substituted by one or more R'; R 4 is hydrogen, lower alkyl, hydroxy or CH 2 CN; X is S or -N=C(R 5 )-; R 5 is hydrogen, lower alkyl or hydroxy, is a bond, -O-, -CH 2 -, -CH 2 -CH 2 -, formula (II) or or -N(R)-; R is hydrogen, lower alkyl, C(O)O-lower alkyl, C(O)-lower alkyl, S(O) 2 -lower alkyl, or benzyl; n is 0 or 1 or to pharmaceutically active acid addition salts. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.
摘要翻译：本发明涉及式（I）化合物，其中R 1为-C（O）O-低级烷基，氰基或杂芳基; 杂芳基是任选被R'取代的五元或六元杂芳基; R'是卤素，低级烷基，被卤素取代的低级烷基，低级烷氧基或被卤素取代的低级烷氧基; R2是氢，低级烷氧基，低级烷基，卤素或氰基; R3是 - （CH2）nC（O）O-低级烷基，低级烷基，低级烷氧基，羟基，-O-Si（CH3）2-低级烷基，-C（O）-N（低级烷基）（O）2-低级烷基，C 3-7 - 环烷基，S（O）2-芳基，杂环基，-C（O） - 杂环基，或芳基或杂芳基，该芳基或杂芳基环任选被一个或多个 R'; R4是氢，低级烷基，羟基或CH2CN; X是S或-N = C（R5） - ; R 5是氢，低级烷基或羟基，是键，-O-，-CH 2 - ， - CH 2 -CH 2 - ，式（II）或-N（R） - ; R是氢，低级烷基，C（O）O-低级烷基，C（O） - 低级烷基，S（O）2 - 低级烷基或苄基; n为0或1或与药学活性的酸加成盐。这些化合物可用于治疗阿尔茨海默病，脑淀粉样血管病，淀粉样变性遗传性脑出血，荷兰型（HCHWA-D），多发性梗死性痴呆，痴呆症或唐氏综合症。

3. 发明申请

WO2004026826A1 4-PYRROLIDINO-PHENYL-BENZYL ETHER DERIVATIVES 审中-公开
标题翻译： 4-吡咯烷基 - 苯基 - 苯甲醚衍生物
公开(公告)号：WO2004026826A1
公开(公告)日：2004-04-01
申请号：PCT/EP2003/010383
申请日：2003-09-18
申请人： F. HOFFMANN-LA ROCHE AG
发明人： JOLIDON, Synese , RODRIGUEZ-SARMIENTO, Rosa, Maria , THOMAS, Andrew, William , WOSTL, Wolfgang , WYLER, Rene
IPC分类号： C07D207/26
CPC分类号： C07D207/273 , C07D207/277
摘要： Racemic or enantiomerically pure 4-pyrrolidino derivatives of formula (I), processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of illness, e.g. which are mediated by monoamine oxidase B inhibitors, in particular Alzheimer's disease or senile dementia.
摘要翻译：式（I）的外消旋或对映异构体纯的4-吡咯烷子基衍生物，其制备方法，包含所述衍生物的药物组合物及其在预防和治疗疾病中的用途。其由单胺氧化酶B抑制剂介导，特别是阿尔茨海默病或老年痴呆。

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

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

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。

7. 发明申请

WO2010052199A1 HETEROCYCLIC GAMMA SECRETASE MODULATORS 审中-公开
标题翻译：杂环游戏分泌物调节剂
公开(公告)号：WO2010052199A1
公开(公告)日：2010-05-14
申请号：PCT/EP2009/064497
申请日：2009-11-03
申请人： F. HOFFMANN-LA ROCHE AG , BAUMANN, Karlheinz , GOETSCHI, Erwin , JOLIDON, Synese , LIMBERG, Anja , LUEBBERS, Thomas
发明人： BAUMANN, Karlheinz , GOETSCHI, Erwin , JOLIDON, Synese , LIMBERG, Anja , LUEBBERS, Thomas
IPC分类号： A61K31/4178 , C07D401/12 , C07D413/12 , C07D417/12
CPC分类号： C07D417/12 , C07D401/12 , C07D403/12 , C07D413/12
摘要： The invention relates to the use of compounds of formula wherein R 1 is a five or six membered heteroaryl group, optionally substituted by one or two R'; R' is lower alkyl; R 2 is hydrogen, lower alkyl, lower alkoxy, hydroxy, halogen or cyano; Z is N, C, O or S; V is N, C(R''), O or S; W is N, C(R''), O, or S; Y is N or C; with the proviso that only one of Z, V or W may be O or S; R'' is hydrogen, lower alkyl, lower alkyl substituted by halogen or hydroxy, or is C(O)O-R 4 ; L is a bond, -(CR 4 2 ) n -, -C(O)NR 4 -, -C(O)NR 4 CH 2 -, or -C(O)-; R 4 may be the same or different and is hydrogen or lower alkyl; R 3 is lower alkyl, phenyl, optionally substituted by one or more R''' or is cycloalkyl; R''' is halogen, cyano, lower alkyl, lower alkyl substituted by halogen or hydroxy, or is lower alkoxy or is C(O)O-R 4 ; n is 1, 2 or 3; or to pharmaceutically active acid addition salts for the manufacture of medicaments for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.
摘要翻译：本发明涉及下式化合物的用途，其中R 1是任选被一个或两个R'取代的五或六元杂芳基; R'是低级烷基; R2是氢，低级烷基，低级烷氧基，羟基，卤素或氰基; Z是N，C，O或S; V是N，C（R“），O或S; W是N，C（R“），O或S; Y为N或C; 条件是Z，V或W中只有一个可以是O或S; R“是氢，低级烷基，被卤素或羟基取代的低级烷基，或是C（O）O-R 4; L是键， - （CR 4 2）n - ， - C（O）NR 4 - ， - C（O）NR 4 CH 2 - 或-C（O） - ; R 4可以相同或不同，为氢或低级烷基; R3是低级烷基，任选被一个或多个R“取代的苯基，或是环烷基; R“是卤素，氰基，低级烷基，被卤素或羟基取代的低级烷基，或是低级烷氧基，或是C（O）O-R4; n为1,2或3; 或用于制备用于治疗阿尔茨海默氏病，脑淀粉样血管病，淀粉样变性遗传性脑出血，荷兰型（HCHWA-D），多发性梗死性痴呆，痴呆症或唐氏综合征的药物的药学活性的酸加成盐。

8. 发明申请

WO2005039591A1 BENZAZEPINE DERIVATIVES AS MAO-B INHIBITORS 审中-公开
标题翻译：苯并噻吩衍生物作为MAO-B抑制剂
公开(公告)号：WO2005039591A1
公开(公告)日：2005-05-06
申请号：PCT/EP2004/011541
申请日：2004-10-14
申请人： F. HOFFMANN-LA ROCHE AG , JOLIDON, Synese , RODRIGUEZ SARMIENTO, Rosa Maria , THOMAS, Andrew, William , WOSTL, Wolfgang , WYLER, Rene
发明人： JOLIDON, Synese , RODRIGUEZ SARMIENTO, Rosa Maria , THOMAS, Andrew, William , WOSTL, Wolfgang , WYLER, Rene
IPC分类号： A61K31/55
CPC分类号： C07D223/16
摘要： The present invention relates to novel benzazepine derivatives of the following formula: (I) wherein R 1 , R 2 , R 3 , R 4 and R 5 , X, X’, Y and Y’ are as defined in the description and claims, processes for their preparation, pharmaceutical compositions containing said derivatives and their use for the preparation of medicaments useful for the prevention and treatment of diseases in which selective inhibition of monoamine oxidase B activity plays a role or is implicated.
摘要翻译：本发明涉及下式的新的苯并氮杂衍生物：其中R 1，R 2，R 3，R 4和R 5，X，X'，Y和Y '如在说明书和权利要求书中所定义，其制备方法，含有所述衍生物的药物组合物及其用于制备可用于预防和治疗单胺氧化酶B活性的选择性抑制发挥作用的疾病的药物的用途牵连。

9. 发明申请

WO2005014563A1 PIPERAZINE WITH OR-SUBSTITUTED PHENYL GROUP AND THEIR USE AS GLYT1 INHIBITORS 审中-公开
标题翻译：具有或取代的苯基的哌嗪及其作为GLYT1抑制剂的用途
公开(公告)号：WO2005014563A1
公开(公告)日：2005-02-17
申请号：PCT/EP2004/008633
申请日：2004-08-02
申请人： F. HOFFMANN-LA ROCHE AG , JOLIDON, Synese , NARQUIZIAN, Robert , NETTEKOVEN, Matthias, Heinrich , NORCROSS, Roger, David , PINARD, Emmanuel , STALDER, Henri
发明人： JOLIDON, Synese , NARQUIZIAN, Robert , NETTEKOVEN, Matthias, Heinrich , NORCROSS, Roger, David , PINARD, Emmanuel , STALDER, Henri
IPC分类号： C07D295/192
CPC分类号： C07D239/42 , C07D213/85 , C07D241/20 , C07D251/42 , C07D257/04 , C07D263/32 , C07D271/06 , C07D295/192 , C07D309/12
摘要： The invention relates to compounds of formula (I) wherein the substituents are described in claim 1. The compounds may be used in the treatment of illnesses based on the glycine uptake inhibitor, such as psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
摘要翻译：本发明涉及式（I）化合物，其中取代基描述于权利要求1中。该化合物可用于治疗基于甘氨酸摄取抑制剂的疾病，例如精神病，疼痛，记忆和学习中的神经变性功能障碍，精神分裂症，痴呆症和认知过程受损的其他疾病，如注意力缺陷障碍或阿尔茨海默病。

10. 发明申请

WO2004014856A1 2,3-DIHYDRO-ISOINDOL-1-ONES WITH MAO-B INHIBITING ACTIVITY 审中-公开
标题翻译： 2,3-DIHYDRO-ISOINDOL-1-ONES与MAO-B抑制活性
公开(公告)号：WO2004014856A1
公开(公告)日：2004-02-19
申请号：PCT/EP2003/008456
申请日：2003-07-31
申请人： F. HOFFMANN-LA ROCHE AG
发明人： JOLIDON, Synese , RODRIGUEZ-SARMIENTO, Rosa, Maria , THOMAS, Andrew, William , WYLER, Rene
IPC分类号： C07D209/46
CPC分类号： C07D471/04 , C07D209/46
摘要： 2,3 Dihydro-isoindol-1-one derivatives, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them, for the prevention and treatment of diseases which are mediated by monoamine oxidase B inhibitors.
摘要翻译： 2,3二氢 - 异吲哚-1-酮衍生物，其制备方法，它们作为药物的用途和包含它们的药物组合物，用于预防和治疗由单胺氧化酶B抑制剂介导的疾病。

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