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    Compound and process
    3.
    发明授权
    Compound and process 有权

    公开(公告)号：US10710998B2

    公开(公告)日：2020-07-14

    申请号：US16309435

    申请日：2017-07-27

    申请人： VERONA PHARMA PLC

    发明人： Peter Lionel Spargo

    IPC分类号： C07D471/04

    摘要： The present invention relates to a novel nitrile derivative of a pyrimido[6,1-a]isoquinolin-4-one compound of formula (A). The invention further relates to a process for producing a compound of formula (A). The invention also relates to a process which comprises reducing a compound of formula (A). Compounds of the invention are useful in the production of compounds such as RPL554.

    CRYSTALLINE FORM OF PYRIMIDIO[6,1-A] ISOQUINOLIN-4-ONE COMPOUND
    4.
    发明申请
    CRYSTALLINE FORM OF PYRIMIDIO[6,1-A] ISOQUINOLIN-4-ONE COMPOUND 有权
    吡啶二酮[6,1-A]异喹啉-4-酮化合物的结晶形式

    公开(公告)号：US20130225616A1

    公开(公告)日：2013-08-29

    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： C07D471/04 ,  A61K45/06 ,  A61K31/519

    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。

    Derivatives of pyrimido[6, 1-A]isoquinolin-4-one
    5.
    发明申请
    Derivatives of pyrimido[6, 1-A]isoquinolin-4-one 有权

    公开(公告)号：US20080206163A1

    公开(公告)日：2008-08-28

    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： A61K9/12 ,  C07D471/04 ,  A61K31/519

    CPC分类号： C07D471/04

    摘要： Compounds of general formula (I) wherein each of R1 and R2 independently represents a C1-6 alkyl or C2-7 acyl group; R5 represents a hydrogen atom or a C1-3 alkyl, C2-3 alkenyl or C2-3 alkynyl group; R6 represents a hydrogen atom or a C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, amino, C1-6 alkylamino, di(C1-6) alkylamino or C2-7 acylamino group; each of R7 and R8 independently represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C2-7 acyl, C1-6 alkythio, C1-6 alkoxy, C3-6 cycloalkyl; and R9 represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C2-7 acyl, C1-6 alkythio, C1-6 alkoxy or C3-6 cycloalkyl group; X represents OCH2 or a group CR3R4, wherein each of R3 and R4 independently represents a hydrogen atom or a C1-3 alkyl group; each of R10 and R11 independently represents a hydrogen atom, a C1-3 alkyl, C3-6 cycloalkyl or phenyl group; y represents an oxygen atom or a group CHNO2, NCN, NH or NNO2, n is an integer from 2 to 4; or a salt thereof; are useful for treatment of respiratory disorders such as asthma. Compounds of the invention have a longer duration of action than the known compound trequinsin (9,10-dimethoxy-3-methyl-2-mesitylimino-2,3,6,7-tetrahydro-4H-pyrimido[6,1-a]isoquinolin-4-one) and do not have trequinsin's very bitter taste.

    DERIVATIVES OF PYRIMIDO [6,1-A] ISOQUINOLIN-4-ONE
    9.
    发明申请
    DERIVATIVES OF PYRIMIDO [6,1-A] ISOQUINOLIN-4-ONE 审中-公开
    吡咯烷[6,1-A]异喹啉-4-酮的衍生物

    公开(公告)号：US20120302533A1

    公开(公告)日：2012-11-29

    申请号：US13568754

    申请日：2012-08-07

    申请人： Alexander William Oxford ,  David Jack

    发明人： Alexander William Oxford ,  David Jack

    IPC分类号： A61K31/519 ,  A61P11/08 ,  A61P29/00 ,  A61K31/56

    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。

    PHARMACEUTICAL COMPOSITIONS COMPRISING RPL554 IN HFA-134A FOR ADMINISTRATION BY INHALATION
    10.
    发明申请
    PHARMACEUTICAL COMPOSITIONS COMPRISING RPL554 IN HFA-134A FOR ADMINISTRATION BY INHALATION 有权

    公开(公告)号：US20210379053A1

    公开(公告)日：2021-12-09

    申请号：US17280452

    申请日：2019-10-09

    申请人： VERONA PHARMA PLC

    发明人： Peter Lionel SPARGO ,  Phillip A. HAYWOOD

    IPC分类号： A61K31/4745 ,  A61K9/00 ,  A61K47/06

    摘要： The present invention relates to a liquid pharmaceutical composition suitable for administration by inhalation comprising: (i) a suspension of particles comprising 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 (RPL554); and (ii) a diluent which is 1,1,1,2-tetrafluoroethane (HFA-134a), wherein the liquid pharmaceutical composition is substantially free of surfactant. The invention also relates to a pressurised metered dose inhaler comprising the liquid pharmaceutical composition.