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    PIPERIDINE DERIVATIVES
    1.
    发明申请
    PIPERIDINE DERIVATIVES 审中-公开
    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。

    MODULATORS FOR AMYLOID BETA
    2.
    发明申请
    MODULATORS FOR AMYLOID BETA 审中-公开
    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。

    4-PYRROLIDINO-PHENYL-BENZYL ETHER DERIVATIVES
    3.
    发明申请
    4-PYRROLIDINO-PHENYL-BENZYL ETHER DERIVATIVES 审中-公开
    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。

    PYRAZOLIDIN-3-ONE DERIVATIVES
    4.
    发明申请
    PYRAZOLIDIN-3-ONE DERIVATIVES 审中-公开
    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）。

    ETHYNYL DERIVATIVES AS POSITIVE ALLOSTERIC MODULATORS OF THE MGLUR5
    5.
    发明申请
    ETHYNYL DERIVATIVES AS POSITIVE ALLOSTERIC MODULATORS OF THE MGLUR5 审中-公开
    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。

    HETEROCYCLIC GAMMA SECRETASE MODULATORS
    7.
    发明申请
    HETEROCYCLIC GAMMA SECRETASE MODULATORS 审中-公开
    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。