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    Compounds for treatment of neurodegenerative diseases
    5.
    发明申请
    Compounds for treatment of neurodegenerative diseases 失效
    用于治疗神经变性疾病的化合物

    公开(公告)号：US20060004041A1

    公开(公告)日：2006-01-05

    申请号：US11120502

    申请日：2005-05-03

    申请人： Christopher Cummings ,  David Lowe ,  William Ripka

    发明人： Christopher Cummings ,  David Lowe ,  William Ripka

    IPC分类号： A61K31/4709 ,  C07D43/02 ,  C07D41/02

    CPC分类号： C07D217/02 ,  A61K31/47 ,  C07D217/06 ,  C07D217/08 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D409/12 ,  C07D417/12 ,  C07D471/04

    摘要： The present invention relates to a class of small molecule hydroxamic acid compounds capable of inhibiting histone deacetylases (HDACs). The present invention also relates to methods of preparation of hydroxamic acid HDAC inhibitor compounds of the invention, which are N-substituted-1,2,3,4-tetrahydroisoquinoline hydroxamic acid derivatives, and their incorporation into pharmaceutical compositions and methods of administration. The present invention also relates to N-substituted-1,2,3,4-tetrahydroisoquinoline hydroxamic acid derivatives, which may be prepared as a hydroxamic acid HDAC inhibitor compound library that can be utilized in screening methods known in the art.

    摘要翻译： 本发明涉及能抑制组蛋白脱乙酰酶（HDAC）的一类小分子异羟肟酸化合物。 本发明还涉及本发明的异羟肟酸HDAC抑制剂化合物的制备方法，它们是N-取代-1,2,3,4-四氢异喹啉异羟肟酸衍生物，以及它们掺入药物组合物和给药方法中。 本发明还涉及可以用于本领域已知的筛选方法中的异羟肟酸HDAC抑制剂化合物文库的N-取代-1,2,3,4-四氢异喹啉异羟肟酸衍生物。

    HETEROCYCLIC BORONIC ACID COMPOUNDS
    6.
    发明申请
    HETEROCYCLIC BORONIC ACID COMPOUNDS 审中-公开
    杂环硼酸化合物

    公开(公告)号：US20070185061A1

    公开(公告)日：2007-08-09

    申请号：US11556944

    申请日：2006-11-06

    申请人： David Campbell ,  David Winn ,  Juan Betancort ,  Kevin Shreder ,  Yi Hu ,  Bei Li ,  Melissa Wong ,  Lifu Ma ,  William Ripka ,  Min Wu

    发明人： David Campbell ,  David Winn ,  Juan Betancort ,  Kevin Shreder ,  Yi Hu ,  Bei Li ,  Melissa Wong ,  Lifu Ma ,  William Ripka ,  Min Wu

    IPC分类号： A61K31/69 ,  C07F5/02

    CPC分类号： C07F5/025

    摘要： Dipeptidyl peptidase IV (DPP-IV)-inhibiting compounds are provided that have formula I: wherein n is 1 to 3; X is CH2; S; O; CF2 or C(CH3)2; Z is H; halogen; hydroxyl; (C1-6)alkoxy; (C1-12)alkyl; (C3-12)cycloalkyl; phenyl; or heteroaryl; where the phenyl and heteroaryl groups are optionally mono- or independently plurisubstituted with R7; optionally, X together with an adjacent ring carbon and Z form a fused cyclopropyl; and optionally, one of the bonds in the ring containing X is a double bond; and CRiRii, R1, R2, R3, R4 and R5 are as described herein.

    摘要翻译： 提供二肽基肽酶IV（DPP-IV）抑制化合物，其具有式I：其中n为1至3; X是CH 2 2; S; O; CF 2或C（CH 3）2）2。 Z是H; 卤素; 羟; （C 1-6）烷氧基; （C 1-12）烷基; （C 3-12）环烷基; 苯基; 或杂芳基; 其中苯基和杂芳基任选被R 7独立或独立地取代; 任选地，X与相邻的环碳一起形成稠合的环丙基; 并且任选地，含有X的环中的一个键是双键; 和R 1，R 2，R 2，R 3，R 3， R 4和R 5如本文所述。