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1. (WO1981002164) SEVEN-MEMBERED RING COMPOUNDS AS INHIBITORS OF CYTIDINE DEAMINASE
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/1981/002164    International Application No.:    PCT/US1981/000127
Publication Date: 06.08.1981 International Filing Date: 28.01.1981
IPC:
C07D 243/04 (2006.01), C07D 491/10 (2006.01), C07D 495/10 (2006.01), C07H 19/04 (2006.01), C07H 19/052 (2006.01)
Applicants:
Inventors:
Priority Data:
115900 28.01.1980 US
Title (EN) SEVEN-MEMBERED RING COMPOUNDS AS INHIBITORS OF CYTIDINE DEAMINASE
(FR) COMPOSES CYCLIQUES A SEPT CHAINONS UTILISE EN TANT QU'INHIBITEURS DE CYTIDINE DEAMINASE
Abstract: front page image
(EN)Seven-membered heterocyclic nucleosides used to inhibit the deamination enzyme responsible for the inactivation of arabinosylcytosine (ara-C). Preferred nucleosides containing a seven-member aglycone are as follows: (FORMULA) R = H, benzoyl, para-nitrobenzoyl; X = H, OR A = R mono-, di- and tri-phosphates (PO3E2, P2O6E3, P3O9E4); E = H, Na. Preferred aglycones are as follows: (FORMULA) 1a:X=OCH2CH2O; 1b:X=SCH2CH2S; 1c:X=O; 1d:X=H, OH; 1e:X=2H; Active components utilized against pyrimidine deaminases from mammalian tissues (mouse kidney and human liver) showed optimum advantage when compared with tetrahydrouridine (THU).
(FR)Nucleosidea heterocycliques a sept chainons utilises pour inhiber l'enzyme de deamination responsable de la desactivation de l'arabinosylcytosine (ara-C). Les nucleosides preferes contenant un aglycone a sept chainons sont les suivants: (FORMULE) R = H, benzoyl, para-nitrobenzoyl X = H, OR A = R, mono-, di- et tri-phosphates (PO3E2, P2O6E3, P3O9E4) E = H, Na. Les aglycones preferes sont les suivants: (FORMULE) 1a: X = OCH2CH2O; 1b: X = SCH2CH2S; 1c: X= O; 1d: X = H, OH; 1e: X = 2H; Les composants actifs utilises contre les pyrimidines deaminases extraites de tissus de mammiferes (reins de rats et foies humains) ont presente des avantages optimaux en comparaison avec la tetrahydro uridine (THU).
Designated States:
Publication Language: English (EN)
Filing Language: English (EN)