2-ethyl and 2-ethylidene-19-nor-vitamin D compounds

Details 2-ethyl and 2-ethylidene-19-nor-vitamin D compounds 2-ethyl and 2-ethylidene-19-nor-vitamin D compounds

2007-08-16

2008-12-23

Badio, Barbara P (Department: 1612)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

9,10-seco- cyclopentanohydrophenanthrene ring system doai

C514S861000

Reexamination Certificate

active

07468361

ABSTRACT:
Biologically active 19-nor vitamin D analogs substituted at C-2 in the A-ring with an ethylidene or an ethyl group. These compounds have preferential activity on mobilizing calcium from bone and either high or normal intestinal calcium transport activity which allows their in vivo administration for the treatment of metabolic bone diseases where bone loss is a major concern. These compounds are also characterized by high cell differentiation activity.

REFERENCES:
patent: 4666634 (1987-05-01), Miyamoto et al.
patent: 5086191 (1992-02-01), DeLuca et al.
patent: 5237110 (1993-08-01), DeLuca et al.
patent: 5246925 (1993-09-01), DeLuca et al.
patent: 5428029 (1995-06-01), Doran et al.
patent: 5484782 (1996-01-01), DeLuca et al.
patent: 5536713 (1996-07-01), DeLuca et al.
patent: 5587497 (1996-12-01), DeLuca et al.
patent: 5817648 (1998-10-01), Kutner et al.
patent: 5843927 (1998-12-01), DeLuca
patent: 5843928 (1998-12-01), DeLuca et al.
patent: 5846960 (1998-12-01), Labrie
patent: 5849726 (1998-12-01), Brenner
patent: 5877168 (1999-03-01), Miyamoto et al.
patent: 5936133 (1999-08-01), DeLuca et al.
patent: 5945410 (1999-08-01), DeLuca et al.
patent: 516410 (1982-12-01), None
patent: 184206 (1985-12-01), None
patent: 387077 (1990-09-01), None
patent: 474517 (1992-11-01), None
patent: WO96/01811 (1996-01-01), None
patent: WO98/41500 (1998-09-01), None
Baggiolini et al, “Stereocontrolled Total Synthesis of 1α,25-Dihydroxycholecalciferol and 1α,25-Dihydroxyerocalciferol,”, J. Org. Chem., 51, pp. 3098-3108, 1986.
Bouillon et al, “Biologic Activity of Dihydroxylated 19-Nor-(Pre) Vitamin D3,” Bioactivity of 19-Nor-Pre D, vol. 8, No. 8, pp. 1009-1015, 1993.
Chemical Abstracts, “2β-Substituted Vitamin D Derivatives,” vol. 121, No. 21, Nov. 21, 1994.
Chemical Abstracts, “Chemistry of Synthetic High Polymers,” vol. 110, No. 10, Mar. 6, 1989.
Kiegiel et al, “Chemical Conversion of Vitamin D3to its 1,25-Dihydroxy Metabolite,” Tetrahedron Letters, vol. 31, No. 43, pp. 6057-6060,1991.
Okano et al, “Regulatory Activities of 2β-(3-Hydroxypropoxy)-1α,25-Dihydroxy-Vitamin D3. A Novel Synthetic Vitamin D3Derivative, on Calcium Metabolism,” Biochemical and Biophysical Research Communications, vol. 163, No. 3, pp. 1444-1449, Sep. 29, 1989.
Perlman et al, “1α,25-Dihydroxy-19-Nor-Vitamin D3. A Novel Vitamin D-Related Compound with Potential Therapeutic Activity,” Tetrahedron Letters, vol. 31, No. 13, pp. 1823-1824, Feb. 1990.
Posner et al, “2-Fluoroalkyl A-Ring Analogs of 1,25-Dihdroxyvitamin D3. Stereocontrolled Total Synthesis via Intramolecular and Intermolecular Diels-Alder Cycloadditions. Preliminary Biological Testing,” J. Org. Chem., 1995, 60, pp. 4617-4628.
Posner et al, “Stereocontrolled Synthesis of a Trihydroxylated A Ring as an Immediate Precursor to 1α,2α25-Trihydroxyvitamin D3,” J. Org. Chem. 56, pp. 4339-4341, Apr. 15, 1991.
Sarandeses et al, “Synthesis of 1α,25-Dihydroxy-19-Norprevitamin D3,” Tetrahedron Letters, pp. 5445-5448, Apr. 1992.
Sicinski, Rafal R. et al, “New 1α,25-Dihydroxy-19-norvitamin D3Compounds of High Biological Activity: Synthesis and Biological Evaluation of 2-Hydroxymethyl, 2-Methyl, and 2-Methylene Analogues,” J. Med. Chem., 1998, 41, pp. 4662-4672.

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