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    IMPROVED FORMULATIONS AND METHODS FOR LYOPHILIZATION AND LYOPHILATES PROVIDED THEREBY
    5.
    发明公开
    IMPROVED FORMULATIONS AND METHODS FOR LYOPHILIZATION AND LYOPHILATES PROVIDED THEREBY 有权
    改进润滑油的配方和方法冻干及由此提供的冻干

    公开(公告)号：EP2868315A1

    公开(公告)日：2015-05-06

    申请号：EP14188334.8

    申请日：2008-12-03

    申请人： Remedy Pharmaceuticals, Inc.

    发明人： Jacobson, Martin, Sven

    IPC分类号： A61K9/16 ,  A61K9/20 ,  A61K31/175

    CPC分类号： A61K9/1682 ,  A61K9/0019 ,  A61K9/1611 ,  A61K9/1623 ,  A61K9/19 ,  A61K31/175 ,  A61K31/451 ,  A61K31/64 ,  Y10S514/96

    摘要： The present invention provides compositions, methods for lyophilizing compounds and making pharmaceutical compositions, and kits providing solutions and lyophilized formulations of compounds. The compositions, methods, and kits are particularly useful in pharmaceutical applications involving therapeutic agents that have low solubility at low pH and medium pll values. Certain embodiments provide methods for lyophilizing compounds in liquid solutions, which include the steps of: a) preparing aqueous solutions of a compound of interest in the absence of buffer; b) adjusting the pH to high values of pH in order to increase the solubility of the compound of interest; and c) frecze-drying the solution to provide a lyophilized solid composition. Aqueous solutions including buffer are also disclosed. Lyophilized formulations, including micronized and non-micronized powders, are provided.

    ANDROGEN RECEPTOR LIGANDS
    6.
    发明公开
    ANDROGEN RECEPTOR LIGANDS 审中-公开
    雄激素受体配体

    公开(公告)号：EP2782643A1

    公开(公告)日：2014-10-01

    申请号：EP12794928.7

    申请日：2012-11-23

    申请人： The Provost, Fellows, Foundation Scholars, & the other members of Board, of the College of the Holy & Undiv. Trinity of Queen Elizabeth near Dublin

    发明人： LLOYD, David George ,  FAYNE, Darren ,  MEEGAN, Mary Jane ,  CARR, Miriam ,  KINSELLA, Gemma Karena ,  CABONI, Laura ,  JAGOE, William Nicholas ,  EGAN, Billy ,  BLANCO, Fernando

    IPC分类号： A61P35/00 ,  A61K31/175 ,  A61K31/343 ,  A61K31/16 ,  A61P17/10 ,  A61P15/00 ,  A61K31/166

    CPC分类号： C07D307/92 ,  A61K31/166 ,  A61K31/175 ,  A61K31/343 ,  C07C251/86 ,  C07D213/56 ,  C07D307/54

    摘要： Non ligand binding pocket antagonists for the human androgen receptor. The androgen receptor (AR) is a member of the Nuclear Receptor (NR) family and its role is to modulate the biological effects of the endogenous androgens, testosterone (tes) and dihydrotestosterone (DHT). Synthetic androgens and anti-androgens have therapeutic value in the treatment of various androgen dependent conditions, from regulation of male fertility to prostate cancer. Current treatment of prostate cancer (PCa) typically involves administration of 'classical' antiandrogens, competitive inhibitors of natural AR ligands, DHT and tes, for the ligand binding pocket (LBP) in the C-terminal ligand binding domain (LBD) of the AR. However, prolonged LBP-targeting can often lead to androgen resistance and alternative therapies and therapeutic strategies are urgently required. Disclosed herein are a class of non-steroidal, small molecule AR antagonists which inhibit the transcriptional activity of the AR by non LBP-mediated modulation. The novel class reported demonstrates full ('true') antagonism in AR with low micromolar potency, high selectivity over both the Estrogen Receptors alpha and beta (ERα and ERβ) and the Glucocorticoid Receptor (GR) and only micromolar partial antagonism in the Progesterone Receptor (PR). Data provide compelling evidence for such non-LBP intervention as an alternative approach to classical PCa therapy. (Formula I).

    摘要翻译： 用于人类雄激素受体的非配体结合口袋拮抗剂。 雄激素受体（AR）是核受体（NR）家族的成员，其作用是调节内源性雄激素，睾酮（睾酮）和二氢睾酮（DHT）的生物学作用。 合成雄激素和抗雄激素在治疗各种雄激素依赖性病症（从调节男性生育力到前列腺癌）中具有治疗价值。 目前对前列腺癌（PCa）的治疗通常包括给予AR的C-末端配体结合结构域（LBD）中的配体结合口袋（LBP）的“经典”抗雄激素物质，天然AR配体的竞争性抑制剂DHT和tes 。 然而，长时间的LBP靶向通常会导致雄激素耐药性，并迫切需要替代治疗和治疗策略。 本文公开了一类非甾族小分子AR拮抗剂，其通过非LBP介导的调节来抑制AR的转录活性。 所报道的这类新型类药物在AR中具有低微摩尔效力，对雌激素受体α和β（ERα和ERβ）以及糖皮质激素受体（GR）具有高选择性，并且在孕酮受体中仅具有微摩尔比部分拮抗作用，表现出完全（'真正' （PR）。 数据为这种非LBP干预提供了令人信服的证据，作为经典PCa治疗的替代方法。 （式I）。

    Formulations for a tight junction effector
    7.
    发明公开
    Formulations for a tight junction effector 有权
    Formulierungenfürtight-junction-Effektor

    公开(公告)号：EP2777695A1

    公开(公告)日：2014-09-17

    申请号：EP14150323.5

    申请日：2007-02-09

    申请人： Alba Therapeutics Corporation

    发明人： Paterson, Blake ,  Ginski, Mark, J.

    IPC分类号： A61K9/16 ,  A61K9/50 ,  A61K38/08

    CPC分类号： A61K38/08 ,  A61K9/009 ,  A61K9/14 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/1676 ,  A61K9/20 ,  A61K9/4808 ,  A61K9/5026 ,  A61K9/5036 ,  A61K9/5042 ,  A61K9/5047 ,  A61K9/5078 ,  A61K31/175 ,  A61K31/426 ,  A61K38/00

    摘要： Enteric compositions comprising one or more tight junction agonists and/or one or more tight junction antagonists are provided. Compositions of the invention may comprise a delayed-release coating disposed over a tight junction agonist and/or tight junction antagonist layer which may be disposed over an inert core. Delayed-release coatings may be substantially stable in gastric fluid and substantially unstable in intestinal fluid, thus providing for substantial release of the tight junction agonist and/or antagonist from the composition in the duodenum or jejunum of the small intestine.

    摘要翻译： 提供包含一种或多种紧密结合激动剂和/或一种或多种紧密连接拮抗剂的肠溶组合物。 本发明的组合物可以包含设置在可以设置在惰性核心上的紧密连接激动剂和/或紧密连接拮抗剂层上的延迟释放涂层。 延迟释放的涂层可能在胃液中基本上是稳定的，并且在肠液中基本不稳定，从而提供紧密联结激动剂和/或拮抗剂从小肠十二指肠或空肠中的组合物的显着释放。

    METHODS AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF DISORDERS OF GLUCOSE HOMEOSTASIS
    9.
    发明公开
    METHODS AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF DISORDERS OF GLUCOSE HOMEOSTASIS 审中-公开
    方法和药物组合物治疗葡萄糖稳态

    公开(公告)号：EP2490696A1

    公开(公告)日：2012-08-29

    申请号：EP10771701.9

    申请日：2010-10-19

    申请人： INSERM (Institut National de la Santé et de la Recherche Médicale)

    发明人： SCHARFMANN, Raphael ,  POLAK, Michel ,  ZERTAL, Samia

    IPC分类号： A61K31/64 ,  A61K31/175 ,  A61P3/08

    CPC分类号： A61K31/175 ,  A61K31/27 ,  A61K31/64

    摘要： The invention is in the field of disorders of glucose homeostasis therapy. In particular the invention relates to a CFTR inhibitor or an inhibitor of CFTR gene expression for use in the treatment of disorders of glucose homeostasis. The present invention also relates to an in vitro methods for increasing the pool of Ngn3+ endocrine progenitor cells, pancreatic endocrine cells, or β cell mass obtained from stem cells, wherein said methods comprises the step of contacting stem cells with a CFTR inhibitor or an inhibitor of CFTR gene expression. The present invention also relates to a method of testing a subject thought to have or be predisposed to having disorders of glucose homeostasis, which comprises the step of analyzing a sample of interest from said subject for: (i) detecting the presence of a mutation in the CFTR gene and/or its associated promoter, and/or (ii) analyzing the expression of the CFTR gene.