中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

194 records (took 0.028 seconds)

    SUBSTITUTED N-ARYLSULFONYLHETEROCYCLIC AMINES AS GAMMA-SECRETASE INHIBITORS
    5.
    发明申请
    SUBSTITUTED N-ARYLSULFONYLHETEROCYCLIC AMINES AS GAMMA-SECRETASE INHIBITORS 审中-公开
    作为GAMMA-分泌酶抑制剂的取代的N-芳基磺酰氧基化胺

    公开(公告)号：WO2006004880A3

    公开(公告)日：2007-03-08

    申请号：PCT/US2005023187

    申请日：2005-06-28

    Applicant: SCHERING CORP ,  JOSIEN HUBERT B ,  CLADER JOHN W ,  BARA THOMAS A ,  XU RUO ,  LI HONGMEI ,  PISSARNITSKI DMITRI ,  ZHAO ZHIQIANG

    Inventor： JOSIEN HUBERT B ,  CLADER JOHN W ,  BARA THOMAS A ,  XU RUO ,  LI HONGMEI ,  PISSARNITSKI DMITRI ,  ZHAO ZHIQIANG

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

    CPC classification number: C07D265/30 ,  C07D413/12 ,  C07D451/02 ,  C07D487/08

    Abstract: This invention discloses novel gamma secretase inhibitors of the formula I: wherein: L is -O- , -N(R 6 )-, -S-, -S(O)-, or -S(O 2 )-; R 1 is selected from the group consisting of aryl and heteroaryl; R 2 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; R 3 is selected from the group consisting of aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, and alkoxyalkyl; each R 4 and R 5 is independently selected from the group consisting of H and alkyl; and Y is selected from the group consisting of -NR 8 R 9 , -N(R 6 )-(CH 2 ) b -NR 8 R 9 , 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.

    Abstract translation: 本发明公开了式I的新型γ分泌酶抑制剂：其中：L是-O-，-N（R 6） - ， - S - ， - S（O） - 或-S（ 0 2 ） - ; R 1选自芳基和杂芳基; R 2选自烷基，-C（O）-Y，-XC（O）-Y， - 亚烷基-XC（O）-Y， - 亚烷基-C（O ）-Y-亚烷基 - 亚环烷基-OC（O）-Y-亚烷基 - 亚环烷基-C（O）-Y-亚烷基 - 亚烷基-OC（O）-Y-亚烷基 - 亚烷基-C（O） Y（ - ）亚环烷基-C（O）-Y-亚烷基-C（O）-Y-亚烷基 - 亚环烷基亚烷基-XC（O）-Y-亚烷基 - 亚环烷基 - 亚烷基-C（O）-Y， 芳基和杂芳基; R 3选自芳基，杂芳基，烷基，环烷基，芳基烷基，芳基环烷基，杂芳基烷基，杂芳基环烷基，芳基杂环烷基和烷氧基烷基; 每个R 4和R 5独立地选自H和烷基; 并且Y选自-NR 8 R 9，-N（R 6） - （CH 2） 芳基，杂芳基，烷基，环烷基，芳基烷基，芳基环烷基，杂芳基烷基，杂芳基环烷基和芳基杂环烷基 ; 或Y选自式II和式III的化合物：一种或多种式I化合物或包含该化合物的制剂可用于，例如， 治疗阿尔茨海默病。

    NOVEL GAMMA SECRETASE INHIBITORS
    6.
    发明申请
    NOVEL GAMMA SECRETASE INHIBITORS 审中-公开
    新的GAMMA SECRETASE抑制剂

    公开(公告)号：WO2005097768A3

    公开(公告)日：2005-12-15

    申请号：PCT/US2005011456

    申请日：2005-04-04

    Applicant: SCHERING CORP ,  ASBEROM THEODROS ,  CLADER JOHN W ,  JOSIEN HUBERT B ,  PISSARNITSKI DMITRI A ,  ZHAO ZHIQIANG ,  MCBRIAR MARK D

    Inventor： ASBEROM THEODROS ,  CLADER JOHN W ,  JOSIEN HUBERT B ,  PISSARNITSKI DMITRI A ,  ZHAO ZHIQIANG ,  MCBRIAR MARK D

    IPC: A61K31/44 ,  C07D211/96 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D451/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  A61P25/28

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

    Abstract: 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.

    Abstract translation: 化学式的γ-分泌酶抑制剂应插入此处，因为它以摘要形式出现在纸上。 可用于治疗各种神经变性疾病，其中例如：R 1包括未取代或取代的芳基或杂芳基; R2包括-C（O）-Y，亚烷基-C（O）-Y，亚烷基 - 亚环烷基-C（O）-Y，亚环烷基 - 亚烷基-C（O）-Y，亚烷基亚环烷基 - 亚烷基-C （O）-Y，亚烷基-S（O）-Y，亚烷基 - 亚环烷基-S（O）-Y，亚环烷基 - 亚烷基-S（O）-Y （O）-Y，亚环烷基-S（O）-Y，-S（O 2）-Y，亚烷基-S（O 2）-Y，亚烷基亚环烷基S（O 2）-Y，亚环烷基亚烷基 S（O 2）-Y，亚烷基亚环烷基 - 亚烷基-S（O 2）-Y和亚环烷基-S（O 2）-Y，其中Y如本文所定义，并且所述亚烷基或亚环烷基中的每一个可以未被取代或如所提供的被取代 本文; 每个R3独立地包括H，烷基，O烷基，OH，N（R9）2，酰基和芳酰基; 或部分（R 3）2与式I所示的环碳原子一起定义为羰基-C（O） - ; 每个R 3A和R 3B独立地包括H或烷基; R11包括芳基，杂芳基，烷基，环烷基，芳基烷基，芳基环烷基，杂芳基烷基，杂芳基环烷基，芳基杂环烷基或烷氧基烷基。 一种或多种式I化合物或其药学上可接受的盐，溶剂化物和/或酯或包含其的组合物可用于治疗例如阿尔茨海默氏病。

Patent Agency Ranking