Pyrimidine acyclonucleoside derivatives, preparation method...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C544S311000, C544S312000

Reexamination Certificate

active

06911450

ABSTRACT:
The invention relates to a compound having general formula (I): wherein n is equal to 3; R1is an ethyl or isopropyl group; each of the R2groups is independently of each other a hydrogen atom, a C1-C3alkyl group or a halogen atom; one of the R3and R4groups represents a hydrogen atom while the other of the R3and R4groups represents an OH or OR5group, where R5can be a C2-C7acyl group, an alkyl(C1-C6)animo-carbonyl group, an aralkyl(C1-C6)aminocarbonyl optionally substituted on the aryl, an arylcarbonyl group optionally substituted or a heteroarylaminocarbonyl group. Said compound is particularly suitable as an antiviral agent and especially as an anti-HIV-1 agent.

REFERENCES:
patent: 0 420 763 (1991-04-01), None
patent: 0 631 783 (1995-01-01), None
Tronchet et al., Antiviral Nucleoside-N-Hydroxyureas and Carbamates, Carbohydrate Letters, vol. 2, pp. 313-320, 1997.
HIV Infection and AIDS: An Overview, National Institute of Allergy and Infectious Diseases, Oct. 2003.
Douglas, Jr., Introduction to Viral Diseases, Cecil Textbook of Medicine, 20thEdition, vol. 2, pp. 1739-1747, 1996.
Beers et al., Viral Diseases [General], The Merck Manual of Diagnosis and Therapy, 1999. http://www.merck.com/mrkshared/mmanual/section13/chapter162/162a.jsp.
Database Chemabs 'Online! Chemical Abstracts Service, Columbus, Ohio, US; Tronchet, Jean M. J. et al.: “Antiviral nucleoside N-hydroxyureas and carbamates” retrieved from STN Database accession no. 127:346601; XP002172470 * abrege; compose RN:198208-92-3 * & Carbohydr. Lett. (1997), 2(5), 313-320.
Pontikis, Renee et al: “Synthesis and Anti-HIV Activity of Novel N-1 Side Chain-Modified Analogs of 1-′(2-Hydroxyethoxy) methyl!-6-(phenylthio) thymine (HEPT)” J. Med. Chem. (1997), 40(12), 1845-1854, XP002172467.
Tronchet JMJ Grigorov M Dolatshahi N Moriaud F Weber J: “A QSAR study confirming the heterogeneity of the HEPT derivative series regarding their interaction with HIV reverse transcriptase” European Journal of Medicinal Chemistry. Chimica Therapeutica, FR, Editions Scientifique Elsevir, Paris, vol. 32, No. 4, 1997, pp. 279-299, XP004086652 ISSN: 0223-5234.
Luco Juan M. et al.: “QSAR Based on Multiple Linear Regression and PLS Methods for the Anti-HIV Activity of a Large Group of HEPT Derivatives”, J. Chem. Inf. Comput. Sci. (1997), 37(2), 392-401, XP002172468.
Jalali-Heravi, M. et al: “Use of Artificial Neural Networks in a QSAR Study of Anti-HIV Activity for a Large Group of HEPT Derivatives” J. Chem. Inf. Comput. Sci. (2000), 40(1), 147-154, XP002172469.

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