By a News Reporter-Staff News Editor at World Disease Weekly -- From Washington, D.C., NewsRx journalists report that a patent application by the inventor Yokokawa, Fumiaki (Singapore, SG), filed on June 16, 2016, was made available online on October 13, 2016 (see also Pharmaceutical Companies).
The patent's assignee is Novartis AG.
News editors obtained the following quote from the background information supplied by the inventors: "Dengue fever is a febrile disease caused by one of the four dengue virus serotypes DEN-1, DEN-2, DEN-3 and DEN-4, which belong to the family Flaviviridae. The virus is transmitted to humans primarily by Aedes aegypti, a mosquito that feeds on humans.
"Infections produce a range of clinical manifestations, from milder flu-like symptoms to the more severe and sometimes fatal hemorrhagic disease. Typical symptoms include fever, severe headache, muscle and joint pains and rashes. The more severe forms of the disease are dengue hemorrhagic fever (DHF) and dengue shock syndrome (DSS). According to the WHO, there are four major clinical manifestations of DHF: (1) high fever (2) haemorrhagic phenomena (3) thrombocytopaenia and (4) leakage of plasma. DSS is defined as DHF plus weak rapid pulse, and narrow pulse pressure or hypotension with cold, clammy skin and restlessness. The severity of DHF can be reduced with early detection and intervention, but subjects in shock are at high risk of death.
"Dengue is endemic in tropical regions, particularly in Asia, Africa and Latin America, and an estimated 2.5 billion people live in areas where they are at risk of infection. There are around 40 million cases of dengue fever and several hundred thousand cases of DHF each year. In Singapore, an epidemic in 2005 resulted in more than 12000 cases of dengue fever.
"Despite regular outbreaks, previously infected people remain susceptible to infection because there are four different serotypes of the dengue virus and infection with one of these serotypes provides immunity to only that serotype. It is believed that DHF is more likely to occur in subjects who have secondary dengue infections. Efficient treatments for dengue fever, DHF and DSS are being sought.
"Yellow fever virus (YFV), West Nile virus (WNV), Japanese encephalitis virus (JEV), tick-borne encephalitis virus, Kunjin virus, Murray Valley encephalitis, St Louis encephalitis, Omsk hemorrhagic fever virus, bovine viral diarrhea virus, Zika virus and Hepatitis C virus (HCV) also belong to the family Flaviviridae.
"WNV can be asymptomatic, or it can cause flu-like symptoms in some individuals. In some cases it causes neurological disorders, encephalitis, and in severe cases can result in death. WNV is also transmitted by mosquitos. YFV is another mosquito-borne virus, which can cause severe symptoms in infected individuals. JEV is also transmitted by mosquitoes, and is either asymptomatic or causes flu-like symptoms, with some cases developing into encephalitis. The acute encephalitis stage of the disease is characterised by convulsions, neck stiffness and other symptoms.
"HCV is a blood-borne virus that is transmitted by blood-to-blood contact. In the initial (acute) stage of the disease, most subjects will not show any symptoms. Even during the chronic stage (i.e. where the disease persists for more than 6 months), severity of symptoms can vary from subject to subject. In the long term, some infected persons can progress to cirrhosis and liver cancer. The current treatment for HCV involves a combination of interferon alpha and ribavirin, an anti-viral drug.
"Efficient treatments for infections caused by these Flaviviridae viruses are being sought as well.
"It has now surprisingly been found that certain nucleoside analogs are useful for the treatment of viral infections such as those caused by a virus of the family Flaviviridae, especially dengue virus, yellow fever virus, West Nile virus, Japanese encephalitis virus, tick-borne encephalitis virus, Kunjin virus, Murray Valley encephalitis, St Louis encephalitis, Omsk hemorrhagic fever virus, bovine viral diarrhea virus, Zika virus and Hepatitis C virus, and other Flaviviridae viruses as described herein."
As a supplement to the background information on this patent application, NewsRx correspondents also obtained the inventor's summary information for this patent application: "The invention provides compounds and pharmaceutical compositions thereof, which are useful for the treatment of viral infections.
"In a first embodiment, the invention provides a compound of formula (I), or a pharmaceutically acceptable salt thereof:
"R.sup.2 is a C.sub.1-C.sub.6 alkyl optionally substituted with halogen, a C.sub.3-C.sub.7 cycloalkyl optionally substituted with halogen, a phenyl optionally substituted with halogen or C.sub.1-C.sub.4alkyl or a C.sub.1-C.sub.4alkyl-phenyl optionally substituted with halogen or C.sub.1-C.sub.4alkyl;
"R.sup.3 is H or C.sub.1-C.sub.4 alkyl
"R.sup.2 and R.sup.3 taken together and the carbon atom they are attached form a C.sub.3-C.sub.7 cycloalkyl;
"R.sup.4 is C.sub.1-C.sub.8 alkyl optionally substituted with halogen or C.sub.1-C.sub.4alkoxy, a C.sub.3-C.sub.7 cycloalkyl optionally substituted with halogen, a phenyl optionally substituted with halogen or C.sub.1-C.sub.4alkyl; a C.sub.1-C.sub.4alkyl-phenyl optionally substituted with halogen or C.sub.1-C.sub.4alkyl or a 4 to 7 membered heterocycle containing 1 to 3 heteroatom selected from N, S, and O, wherein said heterocycle is optionally substituted with one or more halogen, or C.sub.1-C.sub.4 alkyl."
For additional information on this patent application, see: Yokokawa, Fumiaki. 2'-Branched Nucleosides for Treatment of Viral Infections. Filed June 16, 2016 and posted October 13, 2016. Patent URL: http://appft.uspto.gov/netacgi/nph-Parser?Sect1=PTO2&Sect2=HITOFF&u=%2Fnetahtml%2FPTO%2Fsearch-adv.html&r=6531&p=131&f=G&l=50&d=PG01&S1=20161006.PD.&OS=PD/20161006&RS=PD/20161006
Keywords for this news article include: HCV, Asia, Pharmaceutical Companies, Virology, Singapore, Hepatology, Pestivirus, Zika Virus, Novartis AG, RNA Viruses, Dengue Fever, Dengue Virus, Epidemiology, Brain Diseases, Virus Diseases, West Nile Virus, Gastroenterology, Tropical Disease, Hepatitis C Virus, Vertebrate Viruses, Yellow Fever Virus, Risk and Prevention.
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