Vitamin D derivatives, process for producing the same and their

Details Vitamin D derivatives, process for producing the same and their Vitamin D derivatives, process for producing the same and their

1988-06-13

1990-01-02

Robinson, Douglas W.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

9,10-seco- cyclopentanohydrophenanthrene ring system doai

2603972, A61K 3159, C07J 900

Patent

active

048913642

ABSTRACT:
Vitamin D derivatives of the formula ##STR1## where R.sub.1, R.sub.2 and R.sub.3 which may be the same or different each represents a hydrogen atom or a hydroxyl group; X is an oxygen atom, the group of the formula OR.sub.4 (where R.sub.4 is either a hydrogen atom or a lower alkyl having 4 to 6 carbon atoms that may or may not be substituted by a hydroxyl group), or the group of the formula=N-OR.sub.5 (where R.sub.5 is either a hydrogen atom or a lower alkyl group having 1 to 5 carbon atoms that may or may not be substituted by a hydroxyl group, an amino group or a lower alkylamino group having 1 to 3 carbon atoms), provided that the carbon atom at 20-position is linked to X by a single bond when X is the group of the formula OR.sub.4, and by a double bond in other cases, and a process for preparing the derivatives are disclosed.
The derivatives have both the immunoregulating action and the ability to induce differentiation in tumor cells and hence are useful as medicines such as antiallergic agents, antirheumatic agents and antitumor agents.

REFERENCES:
patent: 4338250 (1982-07-01), DeLuca et al.
patent: 4470981 (1984-03-01), Hesse
patent: 4772433 (1988-09-01), Hesse
Pass Murari et al, "Synthesis and Biological Activity of 3.beta.-hydroxy-9-10-secopregna-5,7,10(19)-triene-2-one; A Side Chain Analog of Vitamin D.sub.3 ", Chem. Abstr., vol. 99, No. 5, (1983), p. 439, 37381v.
Holik et al, "Relation of 25-Hydroxyvitamin D.sub.3 Side Chain Structure to Biological Activity", Chem. Abstr., vol. 82, No. 17 (1975), p. 400, 110660r.
Hing-Yat Lam et al, "Structural Analogs of 1.alpha.,25-Dihydroxycholecalciferol: Preparation and Biological Assay of 1.alpha.-Hydroxypregnacalciferol", Steroids, vol. 26, No. 4 (1975), pp. 422-436.

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