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Serving leading biopharmaceutical companies globally:

Daiichi Sankyo
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Generated: December 11, 2017

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Details for Patent: 4,313,951

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Summary for Patent: 4,313,951

Title: 3-Substituted-6-(lower-alkyl)-5-(pyridinyl)-2(1H)-pyridinones, their cardiotonic use and intermediates therefor
Abstract:1-R.sub.1 -3-[amino, cyano, carbamyl, halo, lower-alkylamino, di-(lower-alkyl)amino or lower-acylamino]-6-(lower-alkyl)-5-(pyridinyl)-2(1H)-pyridinones or pharmaceutically-acceptable acid-addition or cationic salts thereof are useful as cardiotonic agents, where R.sub.1 is hydrogen, lower-alkyl or lower-hydroxyalkyl. 1-R.sub.1 -3-amino-6-(lower-alkyl)-5-(pyridinyl)-2(1H)-pyridinones are prepared by hydrolyzing the corresponding 3-cyano compounds to produce the corresponding 3-carbamyl compounds and reacting the latter with a reagent capable of converting carbamyl to amino. The 1-R.sub.1 -3-cyano-6-(lower-alkyl)-5-(pyridinyl)-2(1H)-pyridinones are prepared by reacting (pyridinylmethyl) lower-alkyl ketones with dimethylformamide di-(lower-alkyl) acetal to produce 1-(pyridinyl)-2-(dimethylamino)ethenyl lower-alkyl ketone and reacting said ketones with N-R.sub.1 -.alpha.-cyanoacetamide to produce the 1-R.sub.1 -3-cyano-6-(lower-alkyl)-5-(pyridinyl)-2(1H)-pyridinones. Also shown are the conversions: of the 3-cyano compounds to the 3-H compounds; of the 3-H compounds to the 3-halo compounds; of the 3-halo compounds to the 3-[mono-(lower-alkyl)- or di-(lower-alkyl)-amino]compounds; and, of the 3-amino compounds to the 3-lower-acylamino or 3-[mono-(lower-alkyl)- or di-(lower-alkyl)amino] compounds.
Inventor(s): Lesher; George Y. (Schodack, NY), Philion; Richard E. (Schodack, NY)
Assignee: Sterling Drug Inc. (New York, NY)
Application Number:06/198,461
Patent Claim Types:
see list of patent claims
Compound; Composition; Use; Dosage form;

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International Patent Family for Patent: 4,313,951

Country Document Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Argentina230029► Subscribe
Austria379386► Subscribe
Austria379387► Subscribe
AustriaA143781► Subscribe
AustriaA578080► Subscribe
AustriaA95983► Subscribe
Australia2475384► Subscribe
Australia536354► Subscribe
Australia545667► Subscribe
Australia551627► Subscribe
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The estimated expiration dates shown above are derived by simply adding 20 years to the priority date.
Due to the complexity of determining patent expirations even in a single country, compounded by the diversity of global patent laws, it is advisable to have patent counsel verify freedom to operate.

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Serving leading biopharmaceutical companies globally:

Argus Health
Farmers Insurance
Queensland Health
Boehringer Ingelheim
Fish and Richardson

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