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    TETRAHYDROPYRANOCHROMENE GAMMA SECRETASE INHIBITORS
    4.
    发明公开
    TETRAHYDROPYRANOCHROMENE GAMMA SECRETASE INHIBITORS 有权
    四氢吡喃嗡烯γ-巯基化酶抑制剂

    公开(公告)号：EP2435416A2

    公开(公告)日：2012-04-04

    申请号：EP08768856.0

    申请日：2008-07-01

    申请人： Schering Corporation

    发明人： WU, Wen-lian ,  BARA, Thomas, A. ,  BURNETT, Duane, A. ,  CLADER, John, W. ,  DOMALSKI, Martin S. ,  JIN, Yan ,  JOSIEN, Hubert, B. ,  LI, Hongmei ,  LIANG, Xian ,  PISSARNITSKI, Dmitri, A. ,  SASIKUMAR, Thavalakulamgara, K. ,  WONG, Jesse, K. ,  XU, Ruo ,  ZHAO, Zhiqiang ,  MCNAMARA, Paul

    IPC分类号： C07D311/78 ,  C07D407/12 ,  C07D493/04 ,  A61K31/35 ,  A61K31/352 ,  A61P25/28

    CPC分类号： C07D493/04 ,  C07D311/78 ,  C07D407/12

    摘要： Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)-O-C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)-O-C(O)-heteroaryl and a basic tertiary amine.

    摘要翻译： 公开了下式的新型γ分泌酶抑制剂。 还公开了抑制γ-分泌酶的方法，治疗神经退行性疾病的方法以及治疗阿尔茨海默氏病的方法。 还公开了使用醛（或酮）和被两个吸电子基团取代的烷基的混合物在一个反应​​步骤中制备烯烃的方法，并使该混合物与以下物质反应：（a）磺酰卤（例如磺酰氯） （b）磺酰基酸酐和碱性胺，或（c）芳基-C（O） - 卤化物和碱性叔胺，或（d）芳基-C（O） - OC（O） - 芳基和碱性叔胺，或（e）杂芳基-C（O） - 卤化物和碱性叔胺，或（f）杂芳基-C（O）-OC（O） - 杂芳基和 一种碱性叔胺。

    SUBSTITUTED N-ARYLSULFONYLHETEROCYCLIC AMINES AS GAMMA-SECRETASE INHIBITORS
    5.
    发明授权
    SUBSTITUTED N-ARYLSULFONYLHETEROCYCLIC AMINES AS GAMMA-SECRETASE INHIBITORS 有权
    取代的N- ARYLSULFONYLHETEROCYCLISCHE胺作为γ分泌酶抑制剂

    公开(公告)号：EP1789404B1

    公开(公告)日：2010-03-24

    申请号：EP05790194.4

    申请日：2005-06-28

    申请人： Schering Corporation

    发明人： JOSIEN, Hubert B. ,  CLADER, John W. ,  BARA, Thomas A. ,  XU, Ruo ,  LI, Hongmei ,  PISSARNITSKI, Dmitri ,  ZHAO, Zhiqiang

    IPC分类号： C07D265/30 ,  C07D413/12 ,  C07D451/02 ,  C07D487/08 ,  A61K31/5377 ,  A61P25/28

    CPC分类号： C07D265/30 ,  C07D413/12 ,  C07D451/02 ,  C07D487/08

    摘要： This invention discloses novel gamma secretase inhibitors of the formula I: wherein: L is -O- , -N(R6)-, -S-, -S(O)-, or -S(O2)-; R1 is selected from the group consisting of aryl and heteroaryl; R2 is selected from the group consisting of alkyl, -C(O)-Y, -X-C(O)-Y, -alkylene-X-C(O)-Y, -alkylene-C(O)-Y, -alkylene-cycloalkylene-X-C(O)-Y, -alkylene-cycloalkylene-C(O)-Y, -cycloalkylene-alkylene-X-C(O)-Y, -cycloalkylene-alkylene-C(O)-Y, -cycloalkylene-X-C(O)-Y, -cycloalkylene-C(O)-Y, -alkylene-cycloalkylene-alkylene-X-C(O)-Y, -alkylene-cycloalkylene-alkylene-C(O)-Y, aryl, and heteroaryl; R3 is selected from the group consisting of aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, and alkoxyalkyl; each R4 and R5 is independently selected from the group consisting of H and alkyl; and Y is selected from the group consisting of -NR8R9, -N(R6)-(CH2)b-NR8R9, aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, and arylheterocycloalkyl; or Y is selected from the group consisting of Formula II and Formula III: One or more compounds of formula I, or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.

    SUBSTITUTED N-ARYLSULFONYLHETEROCYCLIC AMINES AS GAMMA-SECRETASE INHIBITORS
    7.
    发明公开
    SUBSTITUTED N-ARYLSULFONYLHETEROCYCLIC AMINES AS GAMMA-SECRETASE INHIBITORS 有权
    取代的N- ARYLSULFONYLHETEROCYCLISCHE胺作为γ分泌酶抑制剂

    公开(公告)号：EP1789404A2

    公开(公告)日：2007-05-30

    申请号：EP05790194.4

    申请日：2005-06-28

    申请人： SCHERING CORPORATION

    发明人： JOSIEN, Hubert B. ,  CLADER, John W. ,  BARA, Thomas A. ,  XU, Ruo ,  LI, Hongmei ,  PISSARNITSKI, Dmitri ,  ZHAO, Zhiqiang

    IPC分类号： C07D265/30 ,  C07D413/12 ,  C07D451/02 ,  C07D487/08 ,  A61K31/5377 ,  A61P25/28

    CPC分类号： C07D265/30 ,  C07D413/12 ,  C07D451/02 ,  C07D487/08

    摘要： This invention discloses novel gamma secretase inhibitors of the formula I: wherein: L is -O- , -N(R6)-, -S-, -S(O)-, or -S(O2)-; R1 is selected from the group consisting of aryl and heteroaryl; R2 is selected from the group consisting of alkyl, -C(O)-Y, -X-C(O)-Y, -alkylene-X-C(O)-Y, -alkylene-C(O)-Y, -alkylene-cycloalkylene-X-C(O)-Y, -alkylene-cycloalkylene-C(O)-Y, -cycloalkylene-alkylene-X-C(O)-Y, -cycloalkylene-alkylene-C(O)-Y, -cycloalkylene-X-C(O)-Y, -cycloalkylene-C(O)-Y, -alkylene-cycloalkylene-alkylene-X-C(O)-Y, -alkylene-cycloalkylene-alkylene-C(O)-Y, aryl, and heteroaryl; R3 is selected from the group consisting of aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, and alkoxyalkyl; each R4 and R5 is independently selected from the group consisting of H and alkyl; and Y is selected from the group consisting of -NR8R9, -N(R6)-(CH2)b-NR8R9, aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, and arylheterocycloalkyl; or Y is selected from the group consisting of Formula II and Formula III: One or more compounds of formula I, or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.

    NOVEL GAMMA SECRETASE INHIBITORS
    9.
    发明公开
    NOVEL GAMMA SECRETASE INHIBITORS 审中-公开
    新的抑制剂GAMMASEKRETASE

    公开(公告)号：EP1740570A2

    公开(公告)日：2007-01-10

    申请号：EP05733367.6

    申请日：2005-04-04

    申请人： SCHERING CORPORATION

    发明人： ASBEROM, Theodros ,  CLADER, John, W. ,  JOSIEN, Hubert, B. ,  PISSARNITSKI, Dmitri, A. ,  ZHAO, Zhiqiang ,  MCBRIAR, Mark, D.

    IPC分类号： C07D401/06 ,  C07D401/14 ,  C07D471/04 ,  A61K31/44 ,  A61P25/28

    CPC分类号： C07D451/04 ,  C07D211/96 ,  C07D401/06 ,  C07D401/12 ,  C07D413/06 ,  C07D413/14 ,  C07D451/06 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08

    摘要： Gamma-secretase inhibitors of the formula: Chemical formula should be inserted here as it appears on the abstract in paper form. are useful in treating various neurodegenerative diseases, wherein, for example: R1 includes unsubstituted or substituted aryl or heteroaryl groups; R2 includes -C(O)-Y, alkylene-C(O)-Y, alkylene-cycloalkylene-C(O)-Y, cycloalkylene-alkylene-C(O)-Y, alkylene cycloalkylene-alkylene-C(O)-Y, cycloalkylene-C(O)-Y, -S(O)-Y, alkylene-S(O)-Y, alkylene-cycloalkylene-S(O)-Y, cycloalkylene-alkylene-S(O)-Y, alkylene cycloalkylene-alkylene-S(O)-Y, cycloalkylene-S(O)-Y, -S(O2)-Y, alkylene-S(O2)-Y, alkylene cycloalkylene S(O2)-Y, cycloalkylene alkylene S(O2)-Y, alkylene cycloalkylene-alkylene-S(O2)-Y, and cycloalkylene-S(O2)-Y, wherein Y is as defined herein, and each of said alkylene or cycloalkylene may be unsubstituted or substituted as provided herein; each R3 is independently includes H, alkyl, O alkyl, OH, N(R9)2, acyl, and aroyl; or the moiety (R3)2, together with the ring carbon atom to which it is shown attached in formula I, defines a carbonyl group, -C(O)-; each R3A and R3B independently includes H, or alkyl; R11 includes aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. One or more of the compounds of formula I, or pharmaceutically acceptable salts, solvates, and/or esters, or compositions comprised thereof, may be used to treat, e.g., Alzheimer's Disease.