Homologated vitamin D2 compounds and the corresponding 1.alpha.-

Organic compounds -- part of the class 532-570 series – Organic compounds – 9,10-seco-cyclopentanohydrophenanthrene ring system or...

Patent

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

C07C40100

Patent

active

057507465

ABSTRACT:
The invention provides new 24, 26, and/or 27 homologated vitamin D.sub.2 compounds, such as 26,27-dihomo-1.alpha.-hydroxyvitamin D.sub.2, 26,27-dihomo-1.alpha.-hydroxy-24-epivitamin D.sub.2, 26,27-dihomo-1.alpha.,25-dihydroxy-24-epi-vitamin D.sub.2 and certain hydroxy-protected derivatives thereof. The new epi compounds in particular exhibit a distinctive activity pattern comprising high potency in stimulating intestinal calcium transport and little or no activity in inducing bone calcium mobilization or the differentiation of undifferentiated cells in culture, thereby evincing utility in the treatment of diseases characterized by loss of bone mass. In contrast, the natural form exhibits no activity in either mobilizing calcium from bone or stimulating intestinal calcium transport. A process for preparing such compounds is also disclosed.

REFERENCES:
patent: 3585221 (1971-06-01), DeLuca et al.
patent: 3880894 (1975-04-01), DeLuca et al.
patent: 3907843 (1975-09-01), DeLuca et al.
patent: 4004003 (1977-01-01), Babcock et al.
patent: 4230701 (1980-10-01), Holick et al.
patent: 4338250 (1982-07-01), DeLuca et al.
patent: 4448721 (1984-05-01), DeLuca et al.
patent: 4508651 (1985-04-01), Baggiolini et al.
patent: 4758383 (1988-07-01), Tachibana
patent: 4769181 (1988-09-01), DeLuca et al.
patent: 4847012 (1989-07-01), DeLuca et al.
patent: 4866048 (1989-09-01), Calverley et al.
patent: 4929609 (1990-05-01), Batcho et al.
patent: 4973584 (1990-11-01), DeLuca et al.
patent: 5063221 (1991-11-01), Nishii et al.
patent: 5190935 (1993-03-01), Binderup et al.
patent: 5206229 (1993-04-01), Calverley et al.
patent: 5250523 (1993-10-01), DeLuca et al.
patent: 5260290 (1993-11-01), DeLuca
patent: 5276061 (1994-01-01), DeLuca et al.
patent: 5281731 (1994-01-01), DeLuca et al.
patent: 5354744 (1994-10-01), DeLuca et al.
patent: 5414098 (1995-05-01), DeLuca et al.
patent: 5449668 (1995-09-01), Sestelo et al.
Chemical and Pharmaceutical Bulletin, vol. 34, No. 11, Nov. 1986, The Pharmaceutical Society of Japan, H. Sai et al: "Synthesis of Some Side-Chain Homologues of 1 Alpha, 25-dihydroxyvitamin D.sub.3 and Investigation of Their Biological Activities", pp. 4508-4515.
Chemical Abstracts, vol. 101, No. 15, Oct. 8, 1994, (Columbus, Ohio, US), I.A. Alekseeva et al: "Activity of 5,6-trans-and 22-dehydro analogs of 1,25-dihydroxyvitamin D.sub.3 ", see p. 601, Abstract 129315q, and Khim.-Fram, Zh, 1984, 18(6), 659-65.
Perlman et al, "24-Homologated 1,25-Dihydroxyvitamin D.sub.3 Compounds: Separation of Calcium and Cell Differentiation Activities," Biochemistry, 1990, vol. 29, 190-196.

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Homologated vitamin D2 compounds and the corresponding 1.alpha.- does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Homologated vitamin D2 compounds and the corresponding 1.alpha.-, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Homologated vitamin D2 compounds and the corresponding 1.alpha.- will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-980799

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.