Methods of Treating Bladder Dysfunction Using Netupitant
    2.
    发明申请
    Methods of Treating Bladder Dysfunction Using Netupitant 审中-公开
    治疗膀胱功能障碍的方法

    公开(公告)号:US20100261734A1

    公开(公告)日:2010-10-14

    申请号:US12758479

    申请日:2010-04-12

    IPC分类号: A61K31/497 A61P13/10

    CPC分类号: A61K31/4523

    摘要: The present invention relates to methods for reducing the frequency of bladder contractions without significantly affecting micturition pressure, comprising administering a pharmaceutical composition comprising a therapeutically effective amount of netupitant, or a pharmaceutically acceptable salt or prodrug thereof. The method can be used to treat bladder dysfunction without significantly increasing residual volume, including urgency, frequency, pollakiuria, nocturia, low deferment time, suboptimal volume threshold, neurogenic bladder, or combinations thereof.

    摘要翻译: 本发明涉及用于降低膀胱收缩频率而不显着影响排尿压力的方法,其包括施用包含治疗有效量的中间体或其药学上可接受的盐或前药的药物组合物。 该方法可用于治疗膀胱功能障碍,而不显着增加残留量,包括尿频,频率,尿频,夜尿,低延迟时间,次最佳体积阈值,神经源性膀胱或其组合。

    Process for the preparation of 13-cis-retinoic acid
    6.
    发明授权
    Process for the preparation of 13-cis-retinoic acid 有权
    13-顺式视黄酸的制备方法

    公开(公告)号:US07057058B2

    公开(公告)日:2006-06-06

    申请号:US11058290

    申请日:2005-02-16

    IPC分类号: C07C51/00 C07C51/353

    摘要: A process for the preparation of 13-cis-retinoic acid (I) from 3-methyl-5-(2,6,6-trimethyl-1-cyclohexen-1-yl)-2,4-pentadienyl)-triphenylphosphonium chloride (IIa) and 5-hydroxy-4-methyl-2(5H)-furanone (III) is herein disclosed. Compounds (IIa) and (III) are reacted in ethanol as the solvent and KOH as the base at a temperature ranging from −5 to 0° C. to give a mixture of retinoic acids which is isomerized to (I) by treatment with a palladium complex.

    摘要翻译: 从3-甲基-5-(2,6,6-三甲基-1-环己烯-1-基)-2,4-戊二烯基) - 三苯基氯化鏻制备13-顺 - 视黄酸(I)的方法 IIa)和5-羟基-4-甲基-2(5H) - 呋喃酮(III)。 化合物(IIa)和(III)在乙醇中作溶剂和KOH作为碱,在-5至0℃的温度下反应,得到视黄酸的混合物,其通过用 钯络合物。

    Ipamorelin Diacetate Injection and Infusion Solutions
    9.
    发明申请
    Ipamorelin Diacetate Injection and Infusion Solutions 审中-公开
    Ipamorelin二醋酸盐注射液和输注溶液

    公开(公告)号:US20100317581A1

    公开(公告)日:2010-12-16

    申请号:US12796001

    申请日:2010-06-08

    IPC分类号: A61K38/27 A61P5/00 A61P43/00

    摘要: Injection and infusion solutions of ipamorelin, having the following composition: a) ipamorelin solubilized by approximately two molar equivalents of acetic acid (ipamorelin diacetate), in an amount of from 0.001 to 20%, based on the weight of the free base of ipamorelin; b) a molar excess of acid, preferably acetic acid, in an amount sufficient to give a pH of at least 3 and less than 7; c) optionally from 0.1 to 30% of one or more formulation aids; and d) water q.s. to 100%; all percentages based on the total weight of the solution.

    摘要翻译: 具有以下组成的ipamorelin的注射和输注溶液:a)以约2%摩尔当量的乙酸(ipamorelin diacetate)溶解的伊帕林林,其量为伊马克林游离碱重量的0.001-20%; b)摩尔过量的酸,优选乙酸,其量足以产生至少3和小于7的pH; c)任选地0.1至30%的一种或多种制剂助剂; 和d)水适量 至100%; 所有百分比基于溶液的总重量。

    CRYSTALLINE AND AMORPHOUS FORMS OF PALONOSETRON HYDROCHLORIDE
    10.
    发明申请
    CRYSTALLINE AND AMORPHOUS FORMS OF PALONOSETRON HYDROCHLORIDE 审中-公开
    PALONOSETRON HYDROCHLORIDE的晶体和非晶形式

    公开(公告)号:US20100105724A1

    公开(公告)日:2010-04-29

    申请号:US12513589

    申请日:2007-12-04

    IPC分类号: A61K31/439 C07D453/02

    CPC分类号: C07D453/02 A61K31/415

    摘要: Amorphous and polymorphic of palonosetron hydrochloride are disclosed that can be characterized by X-ray powder diffraction patterns, thermal properties, purity and methods of manufacture. These forms of palonosetron hydrochloride can be produced from solution or by solid state interconversions. The forms can be used in pharmaceutical formulations: particularly preferred uses of these formulations are in prevention and treatment of nausea and emesis arising from chemotherapy or postoperative side effects. The forms can optionally be used as mixtures of the crystalline and/or amorphous forms.

    摘要翻译: 公开了盐酸帕洛诺司琼的无定形和多晶型物,其可以通过X射线粉末衍射图,热性质,纯度和制造方法来表征。 这些形式的盐酸帕洛诺司琼可以通过溶液或通过固相互变而产生。 这些形式可以用于药物制剂中:这些制剂的特别优选用途是预防和治疗由化疗或术后副作用引起的恶心和呕吐。 这些形式可以任选地用作结晶和/或无定形形式的混合物。