Publication number: 20040087554
Abstract: The invention relates to a method of producing the 1-hydroxy-1,1-diphosphonic acid compounds of general formula (I), and/or the pharmacologically acceptable salts thereof, in which formula R1 represents hydrogen, OH, NO2, Cl, F, Br, C1-C6 alkyl that may be substituted with halogen, amine and/or aminoalkyl, C1-6 alkoxy, aryl, heteroaryl, a group NR3R4, wherein R3 and R4 may be the same or different and represent hydrogen, C1-C6 alkyl, halogen-substituted alkyl, hydroxy-C1-alkyl; R2 represents hydrogen, halogen, amine that may be substituted, C1-C6 alkyl that may be substituted with halogen, amine and/or aminoalkyl, C1-C6 alkoxy, aryl, heteroaryl; Y represents O, S or NH; Z represents C1-C5 alkylene that may be substituted with amine groups, and m and n are 0 or 1, with the proviso that if n=1, m=1.
Type:
Application
Filed:
September 15, 2003
Publication date:
May 6, 2004
Inventors:
Helmut Blum, Wolfgang Greb, Yurii Pustovit, Gerd-Volker Roschenthaler
Publication number: 20040087566
Abstract: The present invention provides a compound of the formula (I) or (II), wherein R1 is H, alkyl, alkenyl or aryl, R2 is H, alkyl or aryl, R3 is H, a alkyl, alkenyl or aryl, R4 and R4-R8 are independently R10, C(O)R10 or SO2R10, wherein R10 is H, alkyl, alkenyl or aryl, and R9 is R9a, C(O)R9a or SO2R9a, wherein R9a is H, alkyl, alkenyl or aryl. R9a can be unsubstituted or substituted with one or more oxo(═O), OR9b, OC(O)R9b, OSO2R9b, NHR9b, NHC(O)R9b and NHSO2R9b groups. R9a is H, alkyl, alkenyl, or aryl. R9b can be unsubstituted or substituted with one or more groups such as oxo(═O), OR9c, CO2R9c, CO2R9c and OC(O)R9c. R9c is H, or a unsubstituted or substituted alkyl, alkenyl or aryl. The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent.
Type:
Application
Filed:
June 11, 2003
Publication date:
May 6, 2004
Inventors:
Michael R Boyd, Kirk R Gustafson, Charles L Cantrell