DISUBSTITUTED ALKYL-8-AZABICYCLO [3.2.1.]OCTANE COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS
    102.
    发明公开
    DISUBSTITUTED ALKYL-8-AZABICYCLO [3.2.1.]OCTANE COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS 有权
    二取代烷基-8-氮杂双环[3.2.1]辛烷化合物作为mu阿片类受体ANTAGONISTS-

    公开(公告)号:EP2195314A1

    公开(公告)日:2010-06-16

    申请号:EP08795603.3

    申请日:2008-08-26

    申请人: Theravance, Inc.

    CPC分类号: C07D451/02

    摘要: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I), where the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds. The compounds according to formula (I) are useful in treating opioid-induced bowel dysfunction or post-operative ileus.

    CRYSTALLINE FORMS OF A DIMETHYLPHENYL COMPOUND
    108.
    发明公开
    CRYSTALLINE FORMS OF A DIMETHYLPHENYL COMPOUND 有权
    二甲基苯基化合物的结晶形式

    公开(公告)号:EP2010490A2

    公开(公告)日:2009-01-07

    申请号:EP07794375.1

    申请日:2007-04-24

    申请人: Theravance, Inc.

    CPC分类号: C07D211/46 A61K31/445

    摘要: The invention relates to crystalline free base forms of biphenyl-2-ylcarbamic acid 1-[2-(4-{[(R)-2-(3-formylamino-4-hydroxyphenyl)-2-hydroxyethylamino]methyl}-2,5-dimethylphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof. This invention also relates to pharmaceutical compositions containing or prepared from such crystalline forms; processes and intermediates useful for preparing such crystalline forms; and methods of using such crystalline forms to, for example, treat a pulmonary disorder.

    摘要翻译: 本发明涉及联苯-2-基氨基甲酸1- [2-(4 - {[(R)-2-(3-甲酰氨基-4-羟苯基)-2-羟乙基氨基]甲基} 乙基]哌啶-4-基酯或其溶剂合物。 本发明还涉及含有或由此类晶体形式制备的药物组合物; 用于制备这种晶体形式的方法和中间体; 和使用这样的晶体形式来治疗例如肺部疾病的方法。