Patent USB522577I5 successfully refreshed from Google Patents.
US4069321A
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Blocked cholecalciferol and dihydrotachysterol 3 derivatives
Assignee: Merck and Co Inc
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Filing: 1976-09-13
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Granted: 1978-01-17
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Expires: 1996-09-13
Abstract
Abstract Novel cholecalciferol and dihydrotachysterol 3 derivatives produced against metabolic conversions at the 25-position, their preparation, pharmaceutical compositions, methods of treating steroid-induced osteoporosis, senile osteoporosis and secondary hyperparathyroidism, especially that induced by an insufficient amount of calcium in relationship to the amount of phosphate, novel intermediates and their preparation are disclosed.
Inventors
- 👤 Howard Jones
- 👤 Shu Shu Yang
- 👤 David P. Jacobus
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-25 22:45
CPC Classifications
C; C07; C07J; C07J9/00; A; A61; A61P; A61P3/00; A61P3/12; A61P3/14; C07J17/00; C07J41/00; C07J41/0033; C07J41/0055; C07J71/00; C07J71/0005; C07J71/001; C07J71/0036; C07J71/0042; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
69 words
A compound of the formulae: ##STR5## wherein R 1 is hydrogen, hydroxy, C 1-5 alkanoyloxy, substituted C 1-5 alkanoyloxy, branched C 3-5 alkanoyloxy, benzoyloxy or p-nitro-benzyloxy, R 3 , r 24 and R 25 are hydrogen, hydroxy, C 1-5 alkanoyloxy, substituted C 1-5 alkanoyloxy, branched C 3-5 alkanoyloxy, benzoyloxy, p-nitro-benzyloxy halo or O--C 1-5 alkyl carbamate with the proviso that R 25 is halo or O--C 1-5 akyl carbamate.
Claim 2
Dependent Claim
69 words
A compound of the formulae: ##STR5## wherein R 1 is hydrogen, hydroxy, C 1-5 alkanoyloxy, substituted C 1-5 alkanoyloxy, branched C 3-5 alkanoyloxy, benzoyloxy or p-nitro-benzyloxy, R 3 , r 24 and R 25 are hydrogen, hydroxy, C 1-5 alkanoyloxy, substituted C 1-5 alkanoyloxy, branched C 3-5 alkanoyloxy, benzoyloxy, p-nitro-benzyloxy halo or O--C 1-5 alkyl carbamate with the proviso that R 25 is halo or O--C 1-5 akyl carbamate.
Claim 3
Dependent Claim
18 words
The compounds of claim 1 wherein R 1 , R 3 and R 24 are hydrogen or hydroxy.
Claim 4
Dependent Claim
10 words
The compounds of claim 2 wherein R 25 is fluoro.
Claim 5
Dependent Claim
5 words
25-Fluoro-1α-hydroxycholecalciferol according to claim 3.
Claim 6
Dependent Claim
5 words
25-Fluorocholecalciferol according to claim 3.
Claim 7
Dependent Claim
6 words
O-Methyl cholecalciferol-25-carbamate according to claim 2.
Claim 8
Dependent Claim
6 words
25-Fluoro-1α-hydroxy-9,10-dihydrotachysterol 3 according to claim 3.
Claim 9
Dependent Claim
6 words
25-Fluoro-9,10-dihydrotachysterol 3 according to claim 3.
Claim 10
Dependent Claim
7 words
O-Methyl-9,10-dihydrotachysterol 3 -carbamate according to claim 2.
Claim 11
Dependent Claim
80 words
A pharmaceutical composition comprising a non-toxic pharmaceutically acceptable carrier and a compound of the formulae: ##STR6## wherein R 1 , is hydrogen, hydroxy, C 1-5 alkanoyloxy, substituted C 1-5 alkanoyloxy, branched C 3-5 alkanoyloxy, benzoyloxy or p-nitro-benzoyloxy, R 3 , r 24 and R 25 are hydrogen, hydroxy, C 1-5 alkanoyloxy, substituted C 1-5 alkanoyloxy, branched C 3-5 alkanoyloxy, benzoyloxy, p-nitro-benzoyloxy, halo or O--C 1-5 alkyl carbamate with the proviso that R 25 is halo or O--C 1-5 alkyl carbamate.
Claim 12
Dependent Claim
80 words
A pharmaceutical composition comprising a non-toxic pharmaceutically acceptable carrier and a compound of the formulae: ##STR6## wherein R 1 , is hydrogen, hydroxy, C 1-5 alkanoyloxy, substituted C 1-5 alkanoyloxy, branched C 3-5 alkanoyloxy, benzoyloxy or p-nitro-benzoyloxy, R 3 , r 24 and R 25 are hydrogen, hydroxy, C 1-5 alkanoyloxy, substituted C 1-5 alkanoyloxy, branched C 3-5 alkanoyloxy, benzoyloxy, p-nitro-benzoyloxy, halo or O--C 1-5 alkyl carbamate with the proviso that R 25 is halo or O--C 1-5 alkyl carbamate.
Claim 13
Independent Claim
91 words
A method of treating steroid-induced osteoporosis, senile osteoporosis and secondary hyderparathyroidism which comprises administering to a patient a therapeutically effective amount of a compound of the formulae: ##STR7## wherein R 1 is hydrogen, hydroxy, C 1-5 alkanoyloxy, substituted C 1-5 alkanoyloxy, branched C 3-5 alkanoyloxy, benzoyloxy or p-nitro-benzoyloxy, R 3 , r 24 and R 25 are hydrogen, hydroxy, C 1-5 alkanoyloxy, substituted C 1-5 alkanoyloxy, branched C 3-5 alkanoyloxy, benzoyloxy, p-nitro-benzoyloxy, halo or O--C 1-5 alkyl carbamate with the proviso that R 25 is halo or O--C 1-5 alkyl carbamate.
Claim 14
Independent Claim
91 words
A method of treating steroid-induced osteoporosis, senile osteoporosis and secondary hyderparathyroidism which comprises administering to a patient a therapeutically effective amount of a compound of the formulae: ##STR7## wherein R 1 is hydrogen, hydroxy, C 1-5 alkanoyloxy, substituted C 1-5 alkanoyloxy, branched C 3-5 alkanoyloxy, benzoyloxy or p-nitro-benzoyloxy, R 3 , r 24 and R 25 are hydrogen, hydroxy, C 1-5 alkanoyloxy, substituted C 1-5 alkanoyloxy, branched C 3-5 alkanoyloxy, benzoyloxy, p-nitro-benzoyloxy, halo or O--C 1-5 alkyl carbamate with the proviso that R 25 is halo or O--C 1-5 alkyl carbamate.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1981-01-16 | 1981-07-18 | 1982-01-17 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-01-16 | 1985-07-18 | 1986-01-17 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-01-16 | 1989-07-18 | 1990-01-17 | $7700.00 | Window Closed / Lapsed |