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21 条记录 (耗时 0.018 秒)

    NEW TREATMENT
    11.
    发明申请
    NEW TREATMENT 有权

    公开(公告)号：US20210106585A1

    公开(公告)日：2021-04-15

    申请号：US17099598

    申请日：2020-11-16

    申请人： VERONA PHARMA PLC

    发明人： Katharine ABBOTT-BANNER ,  John HANRAHAN ,  David THOMAS

    IPC分类号： A61K31/519 ,  A61K45/06 ,  A61K31/47 ,  A61K31/404 ,  A61K31/443

    摘要： The invention provides a compound for use in treating or preventing a disease or condition selected from cystic fibrosis, chronic obstructive pulmonary disease (COPD), asthma, mild pulmonary disease, bronchitis, bronchiectasis, idiopathic bronchiectasis, allergic bronchopulmonary aspergillosis, sinusitis, rhinosinusitis, CFTR-related metabolic syndrome (CRMS), pancreatitis, idiopathic chronic pancreatitis and Sjörgren's syndrome, or for use in preventing male infertility caused by congenital absence of the vas deferens, in a patient by modulating CFTR activity, which compound is 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof. The invention also provides a composition comprising (i) 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof and (ii) a leukotriene receptor antagonist. The invention also provides a composition comprising (i) 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof and (ii) a CFTR potentiator or a CFTR corrector.

    Derivatives of pyrimido[6,1-A]isoquinolin-4-one
    15.
    发明授权
    Derivatives of pyrimido[6,1-A]isoquinolin-4-one 有权
    嘧啶并[6,1-A]异喹啉-4-酮的衍生物

    公开(公告)号：US08242127B2

    公开(公告)日：2012-08-14

    申请号：US12150232

    申请日：2008-04-24

    申请人： Alexander William Oxford ,  David Jack

    发明人： Alexander William Oxford ,  David Jack

    IPC分类号： A01N43/54 ,  A61K31/505

    CPC分类号： C07D471/04

    摘要： The present invention relates to derivatives of pyrimido[6,1-a]isoquinolin-4-one and their application as inhibitors of phosphodiesterase (PDE) isoenzymes. More particularly the invention relates to derivatives of pyrimido[6,1-a]isoquinolin-4-one and their use in medicine for example as bronchodilators with anti-inflammatory properties.

    摘要翻译： 本发明涉及嘧啶并[6,1-a]异喹啉-4-酮的衍生物及其作为磷酸二酯酶（PDE）同功酶抑制剂的应用。 更具体地，本发明涉及嘧啶并[6,1-a]异喹啉-4-酮的衍生物及其在医学中的用途，例如具有抗炎性质的支气管扩张剂。

    Crystalline form of pyrimido[6,1-A] isoquinolin-4-one compound
    17.
    发明授权
    Crystalline form of pyrimido[6,1-A] isoquinolin-4-one compound 有权
    嘧啶基[6,1-A]异喹啉-4-酮化合物的结晶形式

    公开(公告)号：US09062047B2

    公开(公告)日：2015-06-23

    申请号：US13814877

    申请日：2011-08-09

    申请人： Michael J. A. Walker ,  Bertrand M. C. Plouvier ,  Julian S. Northen ,  Philippe Fernandes

    发明人： Michael J. A. Walker ,  Bertrand M. C. Plouvier ,  Julian S. Northen ,  Philippe Fernandes

    IPC分类号： A61K31/519 ,  C07D471/04 ,  A61K45/06

    CPC分类号： C07D471/04 ,  A61K31/519 ,  A61K45/06

    摘要： The current invention is directed towards a polymorph of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, in the form of a crystalline solid consisting of greater than 99% by weight of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, at least 95% in the polymorphic form of a thermodynamically stable polymorph (I) of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, wherein said polymorph is determined by single crystal X-ray structural analysis and X-ray powder diffraction pattern.

    摘要翻译： 本发明涉及N- {2 - [（2E）-2-（甲基咪唑基）-9,10-二甲氧基-4-氧代-6,7-二氢-2H-嘧啶并[6,1-a ] - 异喹啉-3（4H） - 基]乙基}脲，其结晶固体形式由大于99重量％的N- {2 - [（2E）-2-（甲基咪唑基）-9,10 - 二甲氧基-4-氧代-6,7-二氢-2H-嘧啶并[6,1-a]异喹啉-3（4H） - 基]乙基}脲，多晶型物的热力学稳定多晶型物的至少95％ （I）N- {2 - [（2E）-2-（甲基咪唑基）-9,10-二甲氧基-4-氧代-6,7-二氢-2H-嘧啶并[6,1-a] - 异喹啉-3 （4H） - 基]乙基}脲，其中所述多晶型物通过单晶X射线结构分析和X射线粉末衍射图确定。

    TREATING COUGH AND TUSSIVE ATTACKS
    18.
    发明申请
    TREATING COUGH AND TUSSIVE ATTACKS 审中-公开
    治疗酷刑和武装攻击

    公开(公告)号：US20140242174A1

    公开(公告)日：2014-08-28

    申请号：US14342490

    申请日：2012-09-06

    申请人： Michael J.A. Walker

    发明人： Michael J.A. Walker

    IPC分类号： A61K31/167 ,  A61K9/00 ,  A61K9/14

    CPC分类号： A61K9/14 ,  A61K9/0073 ,  A61K9/0075 ,  A61K9/0078 ,  A61K31/167

    摘要： The invention is directed towards carcainium in the form of a salt having an anion An−, wherein An− is an anion of pharmaceutically acceptable acid for use in the treatment and/or suppression of cough, tussive attacks or tussive episodes in a patient.

    摘要翻译： 本发明涉及具有阴离子An-的盐形式的樟脑，其中An-是用于治疗和/或抑制患者咳嗽，咳嗽发作或咳嗽发作的药学上可接受的酸的阴离子。

    PHARMACEUTICAL COMPOSITION COMPRISING ENSIFENTRINE
    19.
    发明申请
    PHARMACEUTICAL COMPOSITION COMPRISING ENSIFENTRINE 有权

    公开(公告)号：US20220265549A1

    公开(公告)日：2022-08-25

    申请号：US17632891

    申请日：2020-08-12

    申请人： VERONA PHARMA PLC

    发明人： Peter Lionel SPARGO ,  Edward James FRENCH

    IPC分类号： A61K9/00 ,  A61P11/00 ,  A61K9/14 ,  A61K31/519

    摘要： The present invention relates to a dry powder pharmaceutical composition suitable for administration by inhalation comprising: (i) ensifentrine particles; (ii) coarse lactose particles having a Dv50 of from 40 μm to 80 μm; and (iii) fine lactose particles having a Dv50 of from 5 μm to 10 μm, wherein: the fine lactose particles are present in an amount of from 0.1 wt % to 6.0 wt % relative to the total weight to the dry powder pharmaceutical composition. Also provided is a dry powder inhaler comprising the dry powder pharmaceutical composition and medical use of the dry powder pharmaceutical composition.