Method and compositions for treating hematological malignancies

a hematological malignancy and composition technology, applied in the direction of drug compositions, biocide, group 5/15 element organic compounds, etc., can solve the problems of substantial unmet medical needs, unmet medical needs for novel, efficacious therapeutics, and lack of promising drugs, and achieve the effect of high preference distribution of cpr-pmedap and enhanced stability of these salts (particularly in parenteral formulations)
US20080039427A1Inactive Publication Date: 2008-02-14GILEAD SCI INC
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Patent Information

Authority / Receiving Office
US Ā· United States
Patent Type
Applications(United States)
Current Assignee / Owner
GILEAD SCI INC
Publication Date
2008-02-14
Estimated Expiration
Not applicable Ā· inactive patent

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Abstract

A compound of formula 1 and / or its salts, tautomers or solvates is used to treat hematological malignancies. In an embodiment, an organic acid salt of compound 1 is provided for general use in treatment of neoplasms, and in a further embodiment the salt is stabilized with carbohydrate.
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Description

BACKGROUND OF THE INVENTION

[0001] N-6 cyclopropylPMEDAP (ā€œcpr-PMEDAPā€) has been shown to be effective producing an antiproliferative and differentiation-inducing effect in in vitro cell culture against a variety of tumor cell lines (Naessens et al., ā€œBiochem. Pharmacol.ā€ 1999 Jul. 15; 58(2):311-23). However, when cpr-PMEDAP and other N6-substituted PMEDAP compounds were employed in an in vivo model of haematological malignancy of inbred Sprague-Dawley rats (Valerianova et al. ā€œAnticancer Res.ā€ 2001 May-June; 21(3B):2057-64), the authors concluded that the ā€œacyclic nucleoside phosphonates substituted at the 6-position of 2,6-diaminepurine ring do not seem to be promising drugs for the treatment of haematological malignanciesā€ due to ā€œhigh toxicityā€.

[0002] Various bis- and mono-amino acid amidate esters of cpr-PMEDAP (and their use as antiproliferative agents) have been disclosed. See WO 05 / 066189. WO 02 / 08241 discloses a method for screening methoxyphosphonate nucleotide analogue p...

Claims

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