公开(公告)号：EP1328277A1

公开(公告)日：2003-07-23

申请号：EP01980564.7

申请日：2001-10-26

申请人： Schering Oy

发明人： ÖSTERMAN, Thua ,  HANNUNIEMI, Ritva ,  HENTUNEN, Teuvo ,  LIUKKO-SIPI, Sirpa ,  NIKANDER, Hannu ,  SELANDER, Katri,UAB Cancer Center, WTI Room T558 ,  SELLMAN, Raija ,  VÄÄNÄNEN, Kalervo

IPC分类号： A61K31/662 ,  C07F9/58 ,  C07F9/40

CPC分类号： A61K45/06 ,  A61K31/662

摘要： The present invention is directed to a method for the preparation of a pharmaceutical composition having osteoclast formation inhibiting or suppressing activity, characterized in that, as the active agent, a compound of the formula (I) is used, in which formula Q1 is hydrogen, hydroxyl, halogen, amino -NH2, or -OR', wherein R' is C1-C4-alkyl or acyl, Q2 is straight or branched alkyl, hydroxyalkyl or aminoalkyl, or a corresponding unsaturated group optionally substituted at the hydroxy or amino group, or a unsubstituted or substituted, saturated or unsaturated cycloalkyl, which can be bound to the methylene carbon over a straight or branched alkylene group, or is the group (a) wherein Y is a saturated or unsaturated heterocyclic group, or a carbocyclic aromatic group, X is a bond, O, S or NR3, wherein R3 is hydrogen or a protecting group, especially lower alkyl, acyl, aryl or arylalkyl, and n is an integer 0 to 6, R?1 and R2¿ are independently hydrogen or C1-C4-alkyl, or it is halogen, and the groups R1 to R4 are the same or different, and mean an alkyl group with 1 - 5 carbon atoms, whereby one or two of the groups R1 to R4 can also mean hydrogen, or a pharmacologically acceptable salt thereof.