- DENGUE AND WEST NILE VIRUS PROTEASE INHIBITORS
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Compounds and methods of treating or preventing a Flavivirus infection in a subject are provided. The methods comprise administering to the subject a therapeutically effective amount of a compound as described herein. The methods are useful in treating and/or preventing Flavivirus infections such as, for example, West Nile Virus, Dengue Virus, and Japanese Encephalitis Virus. Methods of inhibiting a Flavivirus protease in a cell are also provided.
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Page/Page column 29-30
(2014/10/18)
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- AN IMPROVED PROCESS FOR PREPARATION OF (2E)-2-CYANO-3-(3,4- DIHYDROXY-5-NITROPHENYL)N,N-DIETHYL-2-PROPENAMIDE POLYMORPHIC FORM A
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The present invention relates to an improved, cost effective, eco-friendly and easy t handle process to manufacture substantially pure form of (2E)-2-Cyano-3-(3,4-dihydroxy-5 nitrophenyl)-N,N-diethyl-2-propenamide or (E)- N,N-diethyl-2-cyano-3-(3,4-dihyroxy-5 nitroρhenyl)-acrylamide polymorphic form A commonly known as (E)-Entacapone represente by Formula I, using ammonium acetate as a base.
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Page/Page column 7-8
(2009/08/14)
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- PROCESS AND PRODUCT
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The present invention relates to an improved process for isolation and purification of Entacapone, pharmaceutical compositions and therapeutic uses thereof. The process provides an improved yield and improved isomeric purity of produced Entacapone.
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Page/Page column 9
(2008/06/13)
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- AN IMPROVED PROCESS FOR THE PREPARATION OF ENTACAPONE
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The invention relates to Novel Z form of ENTACAPONE-( Z N1N- Diethyl-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-acrylamide . This invention also relates to a process for the preparation of Novel Z form of ENTACAPONE- by treating pure 3- O- alkylated Entacapone with aluminium chloride and pyridine with dichloromethane as solvent to get crude Entacapone with no impurity and dissolving the crude entacapone in one or more solvents selected from soluble or partially soluble solvents or their mixtures filtering . and concentrating by distillation
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Page/Page column 15
(2008/06/13)
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- PROCESS FOR MANUFACTURING ENTACAPONE
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A new process for manufacturing entacapone comprising reacting 3,4-dihydroxy-5-nitrobenzaldehyde with N,N-diethyl-2-cyanoacetamide in the presence of a catalyst in a C 4 to 8 alcohol at reduced pressure and at a temperature of at least 70 °C, cooling the mixture to a temperature of 30 °C or below, seeding the mixture with N,N-diethyl-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)acrylamide comprising at least 10 % of the Z-isomer by weight in the seeding crystals, cooling the mixture to a temperature of 5 °C or below, isolating the crystallized product and converting the obtained mixture of the E- and Z-isomers of N,N-diethyl-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)acrylamide to the E-isomer (entacapone).
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Page/Page column 9-11
(2008/06/13)
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- STABLE POLYMORPHS OF (E)-N,N-DIETHYL-2-CYANO-3-(3,4-DIHYDROXY-5-NITROPHENYL)ACRYLAMIDE
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The present invention relates to stable crystalline polymorphic forms C and D of (E)-N,N-diethyl-2-cyan-3-(3,4-dihydroxy-5-nitrophenyl)acrylamide (Entacapone) and their preparation processes. (E)-Entacapone Form C is obtained by condensing 3,4-Dihydroxy-5-nitrobenzaldehyde and N,N-Diethylcyanoacetamide in presence of a base followed by addition of acetic acid after the reaction is over and crystallization step. (E)-Entacapone Form D is prepared from Entacapone Form C, Crystallographically pure (E)-Entacapone Form A or Crystallographically essentially pure From A. Polymorphic forms C and D of (E)-Entacapone are characterized by specific Infra Red (IR) and X-ray powder diffraction peak values.
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Page/Page column 11
(2008/06/13)
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