UNIVERSITY OF IOWA RESEARCH FOUNDATION;WIEMER, DAVID F.;HOHL, RAYMOND J.
发明人:
WIEMER, DAVID F.,HOHL, RAYMOND J.
申请号：
ES05791545
公开号：
ES2517840T3
申请日:
2005.08.25
申请国别(地区):
ES
年份:
2014
代理人:
摘要：
A bisphosphonate compound of formula I: ** Formula ** in which: R1 is an (C5-C20) unsaturated alkyl of formula, in which n is 0 or 1； each bond designated by ----- is present, which is optionally substituted with one or more halo, trifluoromethyl, -ORa, - P (>； = O) (ORa) 2 or -NRbRc； R2 is a (C5-C20) unsaturated alkyl chain of the formula, wherein n is 0, 1, 2 or 3； and each bond designated by ----- is present, which is optionally substituted with one or more halo, trifluoromethyl, -ORa, - P (>； = O) (ORa) 2 or -NRbRc； each R3, R4, R5 and R6 is independently OH or (C1-C6) alkoxy； each Ra is independently H, (C1-C6) alkyl or aryl； and each Rb and Rc is independently H, (C1-C6) alkyl or aryl； or Rb and Rc together with the nitrogen to which they are attached form a pyrrolidino, piperidino, morpholino or thiomorpholino ring； wherein any aryl is optionally substituted with one or more (C1-C6) alkyl, (C1-C6) alkoxy, (C1-C6) alkanoyl, (C1-C6) alkanoyloxy, (C1-C6) alkoxycarbonyl, halo, cyano, nitro, carboxy, trifluoromethyl, trifluoromethoxy, NRdRe or S (O) 2NRdRe, where each Rd and Re is independently H or (C1-C6) alkyl； where asymmetric means that R1 is not equal to R2 and aryl indicates a phenyl radical or a bicyclic carbocyclic radical fused in the ortho position, which has nine to ten atoms in the ring, where at least one ring is aromatic； or one of its pharmaceutically acceptable salts； or one of its prodrugs in which one or more of R3, R4, R5 and R6 is pivaloyloxymethyloxy, s-acyl-2-thioethyloxy or an amino acid.Un compuesto bisfosfonato de fórmula I: **Fórmula** en la que: R1 es un (C5-C20)alquilo insaturado de fórmula, en la que n es 0 o 1； cada enlace designado por ----- está presente, el cual está opcionalmente sustituido con uno o más halo, trifluorometilo, -ORa, - P(>；=O)(ORa)2 o -NRbRc； R2 es una cadena (C5-C20)alquilo insaturada de fórmula, en la que n es 0, 1, 2 o 3； y cada enlace designado por ----- está presente, el cual está opcionalmente sustitui
