PHOSPHATE TRANSPORT INHIBITORS

WIPO Patent Application WO2003080630

A3

Disclosed is a phosphate transport inhibiting compound represented by Structural Formula (I). R1 and R2 are independently -H, an electron withdrawing group or a C1-C10 alkyl group. Y is a covalent bond, a substituted methylene group, an unsubstituted methylene group or -CR1R2P(O)(OH)-. R3 is a hydrocarbyl group optionally comprising one or more amine, ammonium, ether, thioether or phenylene linking groups, a substituted hydrocarbyl group optionally comprising one or more amine, ammonium, ether, thioether or phenylene linking groups, a heteroaryl group, a substituted heteroaryl group or a phenyl group substituted with one or more groups selected from -C1, -Br, -F, -CN, -NO2, -OR, -N(R)2, -COOR, -CON(R)2, -COR, -S(O)R, -S(O)2R, -S(O)2N(R)2, -NRS(O)2R, -NRCOR, a halogenated lower alkyl group, an aryl group, a substituted aryl group, or a halogenated alkoxy group. Each R is independently -H, lower alkyl, substituted lower alkyl, aryl or substituted aryl. Each Rb is independently -H, a lower alkyl group, or a phosphate protecting group.

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GENZYME CORP (US)
JOZEFIAK THOMAS (US)
BASTOS CECILIA M (US)
HUVAL CHAD C (US)

A61K31/663; A61K31/785; A61P5/18; A61P7/00; A61P13/12; A61P19/00; A61P19/10; A61K45/00; A61P43/00; C07F9/30; C07F9/32; C07F9/38; C07F9/40; C07F9/553; C07F9/655; C08F8/40; C08F30/02; (IPC1-7): C07F9/38; C07F9/40; C07F9/553; C07F9/655; A61K31/663; A61P13/12; C08F30/02

EP0570706A1	1993-11-24
US3845169A	1974-10-29
US6083495A	2000-07-04

MCKENNA C. E. ET AL.: "Alpha-halo ((phenylphosphinyl)methyl)phosphonates as specific inhibitors of Na+-gradient- dependent Na+-phosphate cotransport across renal brush border membrane", JOURNAL OF MEDICINAL CHEMISTRY., vol. 35, no. 26, 1992, AMERICAN CHEMICAL SOCIETY. WASHINGTON., US, pages 4885 - 4892, XP002247463, ISSN: 0022-2623
KELLEY J.L. ET AL.: "(((Guaninylalkyl) phosphinico)methyl)phosphonic acids. Multisubstrate analogue inhibitors of human erythrocyte purine nucleoside phosphorylase", JOURNAL OF MEDICINAL CHEMISTRY., vol. 38, no. 6, 1995, AMERICAN CHEMICAL SOCIETY. WASHINGTON., US, pages 1005 - 1014, XP001148279, ISSN: 0022-2623
STOWELL M. H. B. ET AL.: "The phosphonyl- phosphinyl dianion: a convenient synthon for the preparation of biologically interesting phosphonylphosphinyl (P-C-P-C-) compounds", TETRAHEDRON LETTERS., vol. 30, no. 4, 1989, ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM., NL, pages 411 - 414, XP002247464, ISSN: 0040-4039
MAGNIN D. R. ET AL.: "1,1-Bisphosphonate squalene synthase inhibitors: interplay between the isoprenoid subunit and the diphosphate surrogate", JOURNAL OF MEDICINAL CHEMISTRY., vol. 38, no. 14, 1995, AMERICAN CHEMICAL SOCIETY. WASHINGTON., US, pages 2596 - 2605, XP002247465, ISSN: 0022-2623
EBETINO F. H. ET AL.: "Recent works on the synthesis of phosphonate containing bone-active heterocycles", HETEROCYCLES., vol. 30, no. 2, 1990, ELSEVIER SCIENCE PUBLISHERS B.V. AMSTERDAM., NL, pages 855 - 862, XP008019463, ISSN: 0385-5414

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