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US5206230A
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Fluorine-containing vitamin D3 analogues and pharmaceutical composition containing the same
Assignee: Daikin Industries Ltd
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Filing: 1991-06-05
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Granted: 1993-04-27
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Expires: 2011-06-05
Abstract
Abstract Fluorine-containing vitamin D3 analogues of the formula[I]: <IMAGE> [I] wherein R1, R2 and R3 are independently hydrogen atom, a chemically inactive hydroxy-protecting group, an acyl having 2 to 8 carbon atoms, or an alkyl having 1 to 8 carbon atoms, X is a straight carbon chain having 4 to 6 carbon atoms which contains at least one double or triple bond, which have excellent vitamin D3-like activities, particularly anti-tumor activity owing to differentiation-inducing activity and are useful for the prophylaxis and treatment of various tumors, and intermediates therefor.
Inventors
- 👤 Nobuo Ikekawa
- 👤 Yoshiro Kobayashi
- 👤 Takeo Taguchi
- 👤 Yoko Tanaka
- 👤 Yutaka Ohira
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-24 01:05
CPC Classifications
C; C07; C07C; C07C401/00; A; A61; A61P; A61P35/00; C07F; C07F7/00; C07F7/02; C07F7/08; C07F7/18; C07F7/1804; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 6
Claim 1
Independent Claim
70 words
A fluorine-containing vitamin D 3 analogue of the formula [I]: ##STR9## wherein R 1 , R 2 and R 3 are independently hydrogen atom, a chemically inactive hydroxy-protecting group, an acyl having 2 to 8 carbon atoms, or an alkyl having 1 to 8 carbon atoms, X is a straight carbon chain having 4 to 6 carbon atoms which contains at least one double or triple bond at the 24-position.
Claim 2
Dependent Claim
70 words
A fluorine-containing vitamin D 3 analogue of the formula [I]: ##STR9## wherein R 1 , R 2 and R 3 are independently hydrogen atom, a chemically inactive hydroxy-protecting group, an acyl having 2 to 8 carbon atoms, or an alkyl having 1 to 8 carbon atoms, X is a straight carbon chain having 4 to 6 carbon atoms which contains at least one double or triple bond at the 24-position.
Claim 3
Dependent Claim
43 words
The compound according to claim 1, wherein R 1 , R 2 and R 3 are all hydrogen atom and X is a straight carbon chain having 4 carbon atoms which contain at least one double or triple bond at the 24 position.
Claim 4
Dependent Claim
27 words
The compound according to claim 1 which is a member selected from the following groups: dihydroxyvitamin D 3 , and 1α-t-butyldimethylsilyloxy-26,26,26,27,27,27-hexafluoro-24-homo-25-hydroxy-Δ 24 -vitamin D 3 -t-butyldimethylsilyl ether.
Claim 5
Dependent Claim
31 words
A pharmaceutical composition which comprises as an active ingredient an effective amount of the compound as set forth in claim 1 in admixture with a conventional pharmaceutically acceptable carrier or diluent.
Claim 6
Dependent Claim
31 words
A pharmaceutical composition which comprises as an active ingredient an effective amount of the compound as set forth in claim 2, in admixture with a conventional pharmaceutically acceptable carrier or diluent.
References Cited (Backward Citations)
US4613594A
Cited
US4717721A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1996-04-26 | 1996-10-26 | 1997-04-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2000-04-26 | 2000-10-26 | 2001-04-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2004-04-26 | 2004-10-26 | 2005-04-27 | $7700.00 | Window Closed / Lapsed |