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    GAMMA SECRETASE MODULATERS
    15.
    发明申请
    GAMMA SECRETASE MODULATERS 审中-公开
    GAMMA秘密调制解调器

    公开(公告)号：WO2011092272A1

    公开(公告)日：2011-08-04

    申请号：PCT/EP2011/051184

    申请日：2011-01-28

    Applicant: F. HOFFMANN-LA ROCHE AG ,  BAUMANN, Karlheinz ,  GOETSCHI, Erwin ,  GREEN, Luke ,  JOLIDON, Synese ,  KNUST, Henner ,  LIMBERG, Anja ,  LUEBBERS, Thomas ,  THOMAS, Andrew

    Inventor： BAUMANN, Karlheinz ,  GOETSCHI, Erwin ,  GREEN, Luke ,  JOLIDON, Synese ,  KNUST, Henner ,  LIMBERG, Anja ,  LUEBBERS, Thomas ,  THOMAS, Andrew

    IPC: C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  A61K31/4196 ,  A61P25/00

    CPC classification number: C07D471/04 ,  C07D487/04 ,  C07D498/04

    Abstract: The invention relates to compounds of formula ( I ) wherein R 1 /R 1' are independently from each other hydrogen, halogen, lower alkoxy or cyano; R 2 is lower alkyl, halogen, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, lower alkyl substituted by OR, =0, -C(O)O-lower alkyl, -C(O)NH-lower alkyl, cyano, CH 2 -O-lower alkyl, cycloalkyl, NRR'or is -O-(CH 2 ) o -phenyl optionally substituted by halogen, or is -(CH 2 ) o -phenyl optionally substituted by one, two or three substituents, selected from halogen, -(CH 2 ) o -cyano, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, C(O)H, -CH 2 -NH 2 -, -CH 2 -NH-C(O)O-lower alkyl, -CH 2 -NH-C(O)-lower alkyl, -CH 2 -NH-lower alkyl, -CH 2 -NH-S(O) 2 -lower alkyl, lower alkoxy or by lower alkoxy substituted by halogen, or is -(CH 2 ) o -cycloalkyl, or is -(CH 2 ) o -heterocycloalkyl which is optionally substituted by halogen, CF 3 , lower alkyl, -CH 2 CN, -C(O)-lower alkyl, -C(O)O-lower alkyl or S(O) 2 -lower alkyl, or is heteroaryl selected from the group consisting of furanyl, pyrazinyl, pyridinyl, benzooxazolyl or benzoimidazolyl which are optionally substituted by lower alkyl, or is 4-methyl-3,4-dihydro-2H-benzo[l,4]oxazine R and R' are independently from each other hydrogen or lower alkyl, and o is 0 or 1; R 3 may occur once or twice and is lower alkyl; A is Formula a), b), c), d), e), f), h), i), j) and Formula k); R 2' is hydrogen, lower alkyl, lower alkyl substituted by halogen, C(O)-lower alkyl, S(O) 2 -lower alkyl or phenyl optionally substituted by halogen; hetaryl is a 5 or 6 membered N, S or O-containing heteroaryl group; n is O, 1, 2 or 3; if n is 2 or 3, R 2 may be the same or not; or to pharmaceutically active acid addition salts thereof. The present 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.

    Abstract translation: 本发明涉及其中R 1 / R 1'彼此独立地为氢，卤素，低级烷氧基或氰基的式（I）化合物; R2是低级烷基，卤素，低级烷氧基，被卤素取代的低级烷基，被卤素取代的低级烷氧基，被OR取代的低级烷基，= 0，-C（O）O-低级烷基，-C（O） ，氰基，CH 2 -O-低级烷基，环烷基，NRR'或是任选被卤素取代的-O-（CH 2）o - 苯基，或是被选定的被一个，两个或三个取代基任选取代的 - （CH 2） 卤代低级烷基，被卤素取代的低级烷基，被羟基取代的低级烷基，C（O）H，-CH 2 -NH 2 - ， - CH 2 -NH-C（O）O-低级 烷基，-CH 2 -NH-C（O） - 低级烷基，-CH 2 -NH-低级烷基，-CH 2 -NH-S（O）2 - 低级烷基，低级烷氧基或被卤素取代的低级烷氧基， （CH 2）o - 环烷基，或者是 - （CH 2）o - 杂环烷基，其任选被卤素，CF 3，低级烷基，-CH 2 CN，-C（O） - 低级烷基，-C（O）O-低级烷基或 S（O）2-低级烷基，或者是选自呋喃基，吡嗪基，吡啶基，苯并恶唑基或苯并咪唑基的杂芳基。 或是4-甲基-3,4-二氢-2H-苯并[1,4]恶嗪R和R'彼此独立地为氢或低级烷基，o为0或1; R3可以发生一次或两次，并且是低级烷基; A是公式a），b），c），d），e），f），h），i），j）和公式k）; R 2'是氢，低级烷基，被卤素取代的低级烷基，C（O） - 低级烷基，任选被卤素取代的S（O）2 - 低级烷基或苯基） 杂芳基是5或6元N，S或O的杂芳基; n是0,1,2或3; 如果n为2或3，则R2可以相同或不相同; 或其药物活性的酸加成盐。 本发明的式（I）化合物是淀粉样蛋白β的调节剂，因此它们可用于治疗或预防与脑中β-淀粉样蛋白沉积相关的疾病，特别是阿尔茨海默病，以及其他疾病，例如 脑淀粉样血管病，遗传性脑出血伴淀粉样变性，荷兰型（HCHWA-D），多发梗死性痴呆，痴呆和唐氏综合征。

    ETHYNYL DERIVATIVES
    16.
    发明申请
    ETHYNYL DERIVATIVES 审中-公开
    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

    Applicant: F. HOFFMANN-LA ROCHE AG ,  GREEN, Luke ,  GUBA, Wolfgang ,  JAESCHKE, Georg ,  JOLIDON, Synese ,  LINDEMANN, Lothar ,  STADLER, Heinz ,  VIEIRA, Eric

    Inventor： GREEN, Luke ,  GUBA, Wolfgang ,  JAESCHKE, Georg ,  JOLIDON, Synese ,  LINDEMANN, Lothar ,  STADLER, Heinz ,  VIEIRA, Eric

    IPC: C07D471/04 ,  C07D487/04 ,  A61K31/4162 ,  A61P25/00

    CPC classification number: C07D487/04 ,  C07D471/04

    Abstract: 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.

    Abstract translation: 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。

    PIPERIDINE DERIVATIVES
    19.
    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

    Applicant: F. HOFFMANN-LA ROCHE AG ,  BAUMANN, Karlheinz ,  FLOHR, Alexander ,  GOETSCHI, Erwin ,  GREEN, Luke ,  JOLIDON, Synese ,  KNUST, Henner ,  LIMBERG, Anja ,  LUEBBERS, Thomas ,  THOMAS, Andrew

    Inventor： BAUMANN, Karlheinz ,  FLOHR, Alexander ,  GOETSCHI, Erwin ,  GREEN, Luke ,  JOLIDON, Synese ,  KNUST, Henner ,  LIMBERG, Anja ,  LUEBBERS, Thomas ,  THOMAS, Andrew

    IPC: C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  A61K31/4523 ,  A61P25/28

    CPC classification number: C07D471/04 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D498/04

    Abstract: 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.

    Abstract translation: 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。

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