Derivatives of pyrimido[6.1-a]isoquinolin-4-one

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 bronchodilat...

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Hauptverfasser: Oxford, Alexander William, Jack, David
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Jack, David
description 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. The invention provides compounds or salts thereof of the general formula (I): wherein each of Rand Rindependently represents a Calkyl or Cacyl group; X represents OCHor a group CRR; wherein each of Ror Rindependently represents a hydrogen atom or a Calkyl group; Rrepresents a hydrogen atom or a Calkyl, Calkenyl or Calkynyl group; Rrepresents a hydrogen atom or a Calkyl, Calkenyl, Calkynyl, amino, Calkylamino, di(C) alkylamino or Cacylamino group; each of Rand Rindependently represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, Calkyl, Calkenyl, Calkynyl, Cacyl, Calkylthio, Calkoxy, Ccycloalkyl; and Rrepresents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, Calkyl, Calkenyl, Calkynyl, Cacyl, Calkylthio, Calkoxy or Ccycloalkyl group. The compounds or salts 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--H-pyrimido[6,1-a]isoquinolin-4-one).
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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. The invention provides compounds or salts thereof of the general formula (I): wherein each of Rand Rindependently represents a Calkyl or Cacyl group; X represents OCHor a group CRR; wherein each of Ror Rindependently represents a hydrogen atom or a Calkyl group; Rrepresents a hydrogen atom or a Calkyl, Calkenyl or Calkynyl group; Rrepresents a hydrogen atom or a Calkyl, Calkenyl, Calkynyl, amino, Calkylamino, di(C) alkylamino or Cacylamino group; each of Rand Rindependently represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, Calkyl, Calkenyl, Calkynyl, Cacyl, Calkylthio, Calkoxy, Ccycloalkyl; and Rrepresents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, Calkyl, Calkenyl, Calkynyl, Cacyl, Calkylthio, Calkoxy or Ccycloalkyl group. The compounds or salts 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--H-pyrimido[6,1-a]isoquinolin-4-one).</description><language>eng</language><creationdate>2004</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://image-ppubs.uspto.gov/dirsearch-public/print/downloadPdf/6794391$$EPDF$$P50$$Guspatents$$Hfree_for_read</linktopdf><link.rule.ids>230,308,776,798,881,64012</link.rule.ids><linktorsrc>$$Uhttps://image-ppubs.uspto.gov/dirsearch-public/print/downloadPdf/6794391$$EView_record_in_USPTO$$FView_record_in_$$GUSPTO$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>Oxford, Alexander William</creatorcontrib><creatorcontrib>Jack, David</creatorcontrib><creatorcontrib>Vernalis Limited</creatorcontrib><title>Derivatives of pyrimido[6.1-a]isoquinolin-4-one</title><description>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. The invention provides compounds or salts thereof of the general formula (I): wherein each of Rand Rindependently represents a Calkyl or Cacyl group; X represents OCHor a group CRR; wherein each of Ror Rindependently represents a hydrogen atom or a Calkyl group; Rrepresents a hydrogen atom or a Calkyl, Calkenyl or Calkynyl group; Rrepresents a hydrogen atom or a Calkyl, Calkenyl, Calkynyl, amino, Calkylamino, di(C) alkylamino or Cacylamino group; each of Rand Rindependently represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, Calkyl, Calkenyl, Calkynyl, Cacyl, Calkylthio, Calkoxy, Ccycloalkyl; and Rrepresents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, Calkyl, Calkenyl, Calkynyl, Cacyl, Calkylthio, Calkoxy or Ccycloalkyl group. The compounds or salts thereof are useful for treatment of respiratory disorders such as asthma. 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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. The invention provides compounds or salts thereof of the general formula (I): wherein each of Rand Rindependently represents a Calkyl or Cacyl group; X represents OCHor a group CRR; wherein each of Ror Rindependently represents a hydrogen atom or a Calkyl group; Rrepresents a hydrogen atom or a Calkyl, Calkenyl or Calkynyl group; Rrepresents a hydrogen atom or a Calkyl, Calkenyl, Calkynyl, amino, Calkylamino, di(C) alkylamino or Cacylamino group; each of Rand Rindependently represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, Calkyl, Calkenyl, Calkynyl, Cacyl, Calkylthio, Calkoxy, Ccycloalkyl; and Rrepresents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, Calkyl, Calkenyl, Calkynyl, Cacyl, Calkylthio, Calkoxy or Ccycloalkyl group. The compounds or salts 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--H-pyrimido[6,1-a]isoquinolin-4-one).</abstract><oa>free_for_read</oa></addata></record>
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title Derivatives of pyrimido[6.1-a]isoquinolin-4-one
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