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The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Patent No.:

US 9040490 B1

PDFFull Text
Date of Patent:
May. 26, 2015

Filed:

Mar. 17, 2011

Cytosine analogue, a method of preparation of a cytosine analogue, a dna methyltransferase 1 inhibitor, a method for dna methylation inhibition, the use of the analogue in the treatment of diseases associated with deviations from normal dna methylation

Applicants:

Jan Barciszewski, Poznan, PL;

Wojciech T. Markiewicz, Poznan, PL;

Ewelina Adamska, Kamien Pmorski, PL;

Beata Plitta, Poznan, PL;

Malgorzata Giel-pietraszuk, Poznan, PL;

Eliza Wyszko, Poznan, PL;

Maria Markiewicz, Poznan, PL;

Agnieszka Fedoruk-wyszomirska, Poznan, PL;

Tadeusz Kulinski, Poznan, PL;

Marcin Chmielewski, Poznan, PL;

Inventors:

Jan Barciszewski, Poznan, PL;

Wojciech T. Markiewicz, Poznan, PL;

Ewelina Adamska, Kamien Pmorski, PL;

Beata Plitta, Poznan, PL;

Malgorzata Giel-Pietraszuk, Poznan, PL;

Eliza Wyszko, Poznan, PL;

Maria Markiewicz, Poznan, PL;

Agnieszka Fedoruk-Wyszomirska, Poznan, PL;

Tadeusz Kulinski, Poznan, PL;

Marcin Chmielewski, Poznan, PL;

Assignee:

INSTYTUT CHEMII BIOORGANICZNEJ PAN, Posnan, PL;

Attorney:

Walker & Jocke

Primary Examiner:

Lawrence E Crane

Int. Cl.
CPC ...
A01N 43/04 (2006.01); A61K 31/70 (2006.01); A01N 43/54 (2006.01); A61K 31/505 (2006.01); C07H 19/00 (2006.01); C07D 239/00 (2006.01); C07D 239/02 (2006.01); C07H 19/073 (2006.01); C07D 239/47 (2006.01); C07D 401/12 (2006.01); C07D 405/12 (2006.01);
U.S. Cl.
CPC ...
C07H 19/073 (2013.01); C07D 239/47 (2013.01); C07D 401/12 (2013.01); C07D 405/12 (2013.01);
Abstract

A cytosine analog, a method of preparation of a cytosine analog, a DNA methyltransferase 1 inhibitor, and a method for DNA methylation inhibition, is provided for the treatment of diseases associated with deviations from normal DNA methylation. The analog of cytosine may be comprised of 1, N, 5 and 6-substituted derivatives of cytosine or 5,6-dihydrocytosine, wherein the analog can be described by the chemical formula where Ris H, R, R, 2'-deoxyribosyl, Ris alkyl or aryl, X is N or C, wherein if X in the analog of formula I is N, then Ris no substituent and if X in the analog of formula I and/or II is C or if X in the analog of formula II is N, then Rand Rare independently alkyl, aryl, hydroxyalkyl, aminoalkyl, hydroxyl, carboxyl, amino group, alkoxyl, aryloxyl, aminoalkyl, aminoaryl, thio group, sulfonyl, sulfinyl or halogen.

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