Leo Pharmaceutical Products Ltd. A/s (lovens Kemiske Fabrik

Other

Leo Pharmaceutical Products, Ltd.

Leo Pharmaceutical Products Ltd. A/s Kemiske Fabrik Produkionsaktiese

Lise Binderup

Martin John Calverley

Kai Holst Hansen

Matthew S Miller

Ernst T Binderup

Fredrik Bj&ouml;rkling

Susan Carswell

Pawel Dobrzanski

The present invention is directed, inter alia, to methods of utilizing low calcemic vitamin D analogues. Particularly, the present invention is directed to using low calcemic vitamin D analogues to treat neurodegenerative diseases and disorders, to facilitate endogenous production of neurotrophic factors, to inhibit the degradation, dysfunction or loss of neural cells and/or to enhance the phenotype of neural cells or neuronal processes.

Vitamin D analogues and their neuronal effects

##STR1## The present invention relates to compounds of formula (I), in which formula R stands for an alkyl group containing from 7 to 12 carbon atoms optionally substituted with a hydroxy group; and derivatives of the compounds of formula (I) in which one or more hydroxy groups have been transformed into --O-acyl or --O-glycosyl or phosphate ester groups, such masked groups being hydrolyzable in vivo, in pure form or in mixtures. The present compounds find use in both the human and veterinary practice in the treatment and prophylaxis of autoimmune diseases, including diabetes mellitus, hypertension, inflammatory diseases such as rheumatoid arthritis and asthma as well as diseases characterized by abnormal cell differentiation and/or cell proliferation, and/or imbalance in the immune system.

Vitamin D analogues

Use of 20(R)-22-oxa-vitamin D analogues for the treatment of skin ageing

##STR1## The present invention relates to compounds of formula (I), in which formula, n is an integer from 1-7; and R.sup.1 and R.sup.2, which may be the same or different, stand for hydrogen, or lower alkyl (but with the proviso that when n=1, R.sup.1 and R.sup.2 cannot simultaneously be hydrogen, nor can R.sup.1 and R.sup.2 simultaneously be an alkyl group independently chosen from methyl, ethyl and normal-propyl, and when n=2, R.sup.1 and R.sup.2 cannot simultaneously be methyl), or lower cyclo-alkyl, or, taken together with the carbon (starred in formula I) bearing the hydroxyl group, R.sup.1 and R.sup.2 can form a saturated or unsaturated C.sub.3 -C.sub.9 carbocyclic ring; and R.sup.3 and R.sup.4 represent either simultaneously hydrogen, or when taken together constitute a bond, such that a double bond connects carbons 22 and 23; including diastereoisomeric forms (e.g. E or Z configuration of the 22,23-double bond; R or S configuration at the starred carbona atom) of the compounds of formula (I), in pure form or in mixtures. The present compounds find use in both the human and veterinary practice and show antiinflammatory and immuno-modulating effects as well as strong activity in inducing differentiation and inhibiting undesirable proliferation of certain cells, including cancer cells and skin cells.

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T.ang.strup, Denmark

Lise Binderup