Purified pyrroloquinolinyl-pyrrolidine-2,5-dione compositions and methods for preparing and using same
    1.
    发明授权
    Purified pyrroloquinolinyl-pyrrolidine-2,5-dione compositions and methods for preparing and using same 有权
    纯化的吡咯并喹啉基 - 吡咯烷-2,5-二酮组合物及其制备和使用方法

    公开(公告)号:US08552192B2

    公开(公告)日:2013-10-08

    申请号:US12975644

    申请日:2010-12-22

    IPC分类号: C07D471/06

    CPC分类号: C07D471/04 C07D471/06

    摘要: The present invention relates to a form 1 and form 2 polymorph of (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione. The present invention also relates to (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl) pyrrolidine-2,5-dione compounds having a chiral purity greater than 99%, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising these (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a composition comprising (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione having a chiral purity greater than 99% or a form 1 and form 2 polymorph of (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione.

    摘要翻译: 本发明涉及( - ) - 反式-3-(5,6-二氢-4H-吡咯并[3,2,1-ij]喹啉-1-基)-4-( -1H-吲哚-3-基)吡咯烷-2,5-二酮。 本发明还涉及( - ) - 反式-3-(5,6-二氢-4H-吡咯并[3,2,1-ij]喹啉-1-基)-4-(1H-吲哚-3-基 )吡咯烷-2,5-二酮化合物及其制备方法。 本发明还涉及包含这些( - ) - 反式-3-(5,6-二氢-4H-吡咯并[3,2,1-ij]喹啉-1-基)-4-(1H-吲哚 -3-基)吡咯烷-2,5-二酮化合物。 本发明提供了通过向有需要的受试者施用治疗有效量的包含( - ) - 反式-3-(5,6-二氢-4H-吡喃并[ 吡咯并[3,2,1-ij]喹啉-1-基)-4-(1H-吲哚-3-基)吡咯烷-2,5-二酮,手性纯度大于99%,形式1和形式2 ( - ) - 反式-3-(5,6-二氢-4H-吡咯并[3,2,1-ij]喹啉-1-基)-4-(1H-吲哚-3-基)吡咯烷-2 ,5-二酮。

    Purified Pyrroloquinolinyl-Pyrrolidine-2,5-Dione Compositions And Methods For Preparing And Using Same
    3.
    发明申请
    Purified Pyrroloquinolinyl-Pyrrolidine-2,5-Dione Compositions And Methods For Preparing And Using Same 有权
    纯化的吡咯并喹啉基 - 吡咯烷-2,5-二酮组合物及其制备和使用方法

    公开(公告)号:US20110160242A1

    公开(公告)日:2011-06-30

    申请号:US12975644

    申请日:2010-12-22

    CPC分类号: C07D471/04 C07D471/06

    摘要: The present invention relates to a form 1 and form 2 polymorph of (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione. The present invention also relates to (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds having a chiral purity greater than 99%, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising these (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a composition comprising (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione having a chiral purity greater than 99% or a form 1 and form 2 polymorph of (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione.

    摘要翻译: 本发明涉及( - ) - 反式-3-(5,6-二氢-4H-吡咯并〔3,2,1-ij〕喹啉-1-基)-4-( -1H-吲哚-3-基)吡咯烷-2,5-二酮。 本发明还涉及( - ) - 反式-3-(5,6-二氢-4H-吡咯并[3,2,1-ij]喹啉-1-基)-4-(1H-吲哚-3-基 )吡咯烷-2,5-二酮化合物及其制备方法。 本发明还涉及包含这些( - ) - 反式-3-(5,6-二氢-4H-吡咯并[3,2,1-ij]喹啉-1-基)-4-(1H-吲哚 -3-基)吡咯烷-2,5-二酮化合物。 本发明提供了通过向有需要的受试者施用治疗有效量的包含( - ) - 反式-3-(5,6-二氢-4H-吡喃并[ 吡咯并[3,2,1-ij]喹啉-1-基)-4-(1H-吲哚-3-基)吡咯烷-2,5-二酮,手性纯度大于99%,形式1和形式2 ( - ) - 反式-3-(5,6-二氢-4H-吡咯并[3,2,1-ij]喹啉-1-基)-4-(1H-吲哚-3-基)吡咯烷-2 ,5-二酮。

    Dosage form for aerosol administration
    6.
    发明授权
    Dosage form for aerosol administration 失效
    用于气雾剂给药的剂型

    公开(公告)号:US6161536A

    公开(公告)日:2000-12-19

    申请号:US168216

    申请日:1998-10-07

    摘要: A method for preparing aerosols of water-sensitive medicaments and a pharmaceutical kit for aerosol administration are disclosed. The kit includes (a) a solid state open matrix network of a medicament in a first container; and (b) an aqueous vehicle in a second container. The first and second containers may be separate or they may be chambers within a single housing. The solid state network may be a unit dose of medicament, and the quantity of aqueous vehicle will then be that quantity needed to deliver one unit dose by aerosol; alternatively, the solid state network may contain a plurality of unit doses of medicament, in which case the quantity of aqueous vehicle will be that quantity needed to deliver the number of unit doses in the network. The kit may also include a metered dose nebulizer. A preferred medicament for use in the method is formoterol.

    摘要翻译: 公开了一种制备水敏性药物的气溶胶的方法和用于气雾剂给药的药物试剂盒。 试剂盒包括(a)在第一容器中的药物的固态开式基质网络; 和(b)在第二容器中的水性载体。 第一和第二容器可以是分离的,或者它们可以是单个壳体内的室。 固态网络可以是单位剂量的药物,然后水性载体的量将是通过气溶胶递送一个单位剂量所需的量; 或者,固态网络可以包含多个单位剂量的药物,在这种情况下,水性载体的量将是递送网络中单位剂量数量所需的量。 试剂盒还可以包括计量剂量雾化器。 用于该方法的优选药物是福莫特罗。