Vitamin D derivative with substituent at the 2.beta.-position

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – 9,10-seco- cyclopentanohydrophenanthrene ring system doai

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552653, A61K 3159, C07C40100

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active

061242764

ABSTRACT:
1.alpha.-hydroxy-vitamin D derivatives represented by formula ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxyl group; and R.sub.2 represents a straight-chain or branched C.sub.2 -C.sub.7 alkyl, C.sub.2 -C.sub.7 alkenyl, or C.sub.2 -C.sub.7 alkynyl group. The compounds exhibit calcium metabolism regulating activity and differentiation stimulating activity on tumor cells, and are useful as treating agents for diseases caused by abnormal calcium metabolism, such as osteoporosis and osteomalacia, or as antitumor agents.

REFERENCES:
patent: 4011250 (1977-03-01), Ishiwaka et al.
patent: 5389622 (1995-02-01), Posner et al.
patent: 5661140 (1997-08-01), DeLuca et al.
Cho, Cheon-Gyu, Asymmetric intramolecular diels-alder cycloadditions of 2-pyrone carboxylates and application toward an enantiospecific total synthesis of 1.beta.,25-(OH)2,2.beta.-butylvitamin D3. Development of novel inducers of anticarcinogenic detox, 1994.
Posner et al, "Stereocontrolled Total Synthesis of Calcitriol Derivatives: 1,25-Dihydroxy-2-(4'-hydroxbutyl) Vitamin D.sub.3 Analogs for an Osteoporosis Drug", J. Org. Chem. 59:7855-7861 (1994).

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