Invention Grant
US09040490B2 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
有权
胞嘧啶类似物,胞嘧啶类似物的制备方法,DNA甲基转移酶1抑制剂,DNA甲基化抑制方法,类似物在治疗与正常DNA甲基化偏差相关的疾病中的应用
- Patent Title: 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
- Patent Title (中): 胞嘧啶类似物,胞嘧啶类似物的制备方法,DNA甲基转移酶1抑制剂,DNA甲基化抑制方法,类似物在治疗与正常DNA甲基化偏差相关的疾病中的应用
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Application No.: US13576709Application Date: 2011-03-17
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Publication No.: US09040490B2Publication Date: 2015-05-26
- Inventor: Jan Barciszewski , Wojciech T. Markiewicz , Ewelina Adamska , Beata Plitta , Malgorzata Giel-Pietraszuk , Eliza Wyszko , Maria Markiewicz , Agnieszka Fedoruk-Wyszomirska , Tadeusz Kulinski , Marcin Chmielewski
- Applicant: Jan Barciszewski , Wojciech T. Markiewicz , Ewelina Adamska , Beata Plitta , Malgorzata Giel-Pietraszuk , Eliza Wyszko , Maria Markiewicz , Agnieszka Fedoruk-Wyszomirska , Tadeusz Kulinski , Marcin Chmielewski
- Applicant Address: PL Posnan
- Assignee: INSTYTUT CHEMII BIOORGANICZNEJ PAN
- Current Assignee: INSTYTUT CHEMII BIOORGANICZNEJ PAN
- Current Assignee Address: PL Posnan
- Agency: Walker & Jocke
- Priority: PL390769 20100319
- International Application: PCT/PL2011/000032 WO 20110317
- International Announcement: WO2011/115513 WO 20110922
- Main IPC: A01N43/04
- IPC: A01N43/04 ; A61K31/70 ; A01N43/54 ; A61K31/505 ; C07H19/00 ; C07D239/00 ; C07D239/02 ; C07H19/073 ; C07D239/47 ; C07D401/12 ; C07D405/12

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, N4, 5 and 6-substituted derivatives of cytosine or 5,6-dihydrocytosine, wherein the analog can be described by the chemical formula where R1 is H, R3, R4, 2′-deoxyribosyl, R4 is alkyl or aryl, X is N or C, wherein if X in the analog of formula I is N, then R5 is 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 R5 and R6 are independently alkyl, aryl, hydroxyalkyl, aminoalkyl, hydroxyl, carboxyl, amino group, alkoxyl, aryloxyl, aminoalkyl, aminoaryl, thio group, sulfonyl, sulfinyl or halogen.
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