发明名称 Vitamin D analogues
摘要 Described are compounds of formula (I) wherein Q stands for a C1 -C8 hydrocarbylene diradical, and R stands for hydrogen or C1 -C6 hydrocarbyl, or two R groups, taken together with the carbon atom bearing the hydroxy group can form a C3 -C8 carbocyclic ring. Preferred compounds of formula I are 1(S),3(R)-Dihydroxy-20-methyl-18-(5-methyl-5-hydroxy-hexyloxy)-9,10-seco-p regna-5(Z),7(E),10(19)-triene, 1(S),3(R)-Dihydroxy-20-methyl-18-(4-ethyl-4-hydroxy-hexyloxy)-9,10-seco-pr egna-5(Z),7(E),10(19)-triene, 1(S),3(R)-Dihydroxy-20-methyl-18-(4-ethyl-4-hydroxy-hex-2-ynyloxy)-9,10-se co-pregna-5(Z),7(E),10(19)-triene, 1(S),3(R)-Dihydroxy-20-methyl-18-(4-hydroxy-4-methylpentyloxy)-9,10-seco-p regna-5(Z),7(E),10(19)-triene, 1(S),3(R)-Dihydroxy-20-methyl-18-(4-hydroxy-4-methylpent-2-yn-1-yloxy)-9,1 0-seco-pregna-5(Z),7(E),-10(19)-triene, or f1(S),3(R)-Dihydroxy-20-methyl-18-(3-(1-hydroxy-1-methylethyl)phenylmethylo xy)-9,10-seco-pregna-5(Z),-7(E),10(19)-triene. The compounds are reported to show antiinflammatory and immunomodulating effects as well as strong activity in inducing differentiation and inhibiting undesirable proliferation of certain cells, including cancer cells and skin cells. Also reported is their use in the treatment and prophylaxis of hyperparathyroidism, particularly secondary hyperparathyroidism associated with renal failure, for promoting osteogenesis and treating osteoporosis, for treating neurological dysfunctions such as Alzheimer's disease and a number of disease states including diabetes mellitus, hypertension, acne, alopecia, skin ageing, imbalance in the immune system, inflammatory diseases such as rheumatoid arthritis and asthma as well as diseases characterized by abnormal cell differentiation and/or cell proliferation, such as psoriasis and cancer.
申请公布号 NZ329531(A) 申请公布日期 2001.03.30
申请号 NZ19970329531 申请日期 1997.03.21
申请人 LEO PHARMACEUTICAL PRODUCTS LTD 发明人 GRUE-SORENSEN, GUNNAR
分类号 C07D309/12;A61K31/00;A61K31/59;A61P3/00;A61P3/02;A61P3/10;A61P9/00;A61P9/12;A61P17/00;A61P17/06;A61P17/10;A61P17/14;A61P19/00;A61P19/10;A61P25/28;A61P29/00;A61P35/00;A61P37/00;A61P37/02;C07C41/26;C07C43/13;C07C401/00;C07F7/18;(IPC1-7):A61K31/59 主分类号 C07D309/12
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