发明名称 Vitamin D3 derivatives and intermediates containing a tert-butyl-dimethyl-silyloxy group
摘要 The vitamin D3 derivative or a diastereoisomer or mixture thereof has the formula I wherein: Q is methylene, ethylene or tri- tetra- or pentamethylene, -CH=CH-, -CH=CH-CH=CH-, -CH=CH-CH2-, -CºC-, -CºC-CH2-, -CH(R)-(CH2)2-, -CH(R)-CH=CH- or -CH(R)-CºC-; R is alkyl; Y is a single bond, a carbonyl group, methylene, ethylene, -CH(OH)-, -O-(C6H4)- or -S-(C6H4)- radical; R1 and R2 are independently hydrogen or a hydrocarbyl radical or R1 and R2 with the carbon atom to which they are attached (starred in formula I) can form a carbocyclic ring and Z is hydrogen or hydroxy; with the proviso that when Q is ethylene, Y is methylene, carbonyl or -CH(OH)-, R1 and R2 are methyl and Z is hydroxy, then the configuration at C-20 cannot be (R). Also disclosed as certain intermediate compounds having a 3(R)-bis-(tert-butyldimethylsilyoxy) radical. A pharmaceutical composition thereof is useful for treating or prophylaxis of psoriasis, cancer, myelofibrosis, rheumatoid arthritis, asthma, secondary hyperparathyroidism associated with renal failure or Alzheimer's disease.
申请公布号 NZ335862(A) 申请公布日期 2000.11.24
申请号 NZ19970335862 申请日期 1997.11.28
申请人 LEO PHARMACEUTICAL PRODUCTS LTD 发明人 VON DAEHNE, WELF
分类号 A61K31/59;A61K31/593;A61P3/10;A61P9/12;A61P11/06;A61P13/12;A61P17/00;A61P17/06;A61P19/00;A61P19/02;A61P19/10;A61P25/00;A61P25/28;A61P29/00;A61P35/00;A61P35/02;A61P37/02;A61P37/04;A61P37/06;C07C401/00;(IPC1-7):C07F7/18 主分类号 A61K31/59
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