US4235887A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Process for therapeutic treatment
Assignee: Pharmacia and Upjohn Co
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Filing: 1977-04-13
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Granted: 1980-11-25
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Expires: 1997-04-13
Abstract
Abstract This invention relates to a new method of therapy comprising the administration of a pro-drug to a human or animal, said pro-drug being a compound formed by a therapeutic compound chemically combined with another moiety by a photocleavable bond and irradiating the diseased area with ultraviolet radiation in an amount sufficient to cleave the bond and release the therapeutic compound in a therapeutically effective amount. Specifically disclosed are pro-drugs which are cleaved to therapeutically active medications which are anti-proliferative and anti-inflammatory compounds and the treatment of inflammatory and/or proliferative skin diseases therewith.
Inventors
- 👤 John J. Voorhees
- 👤 Wendell Wierenga
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-24 22:30
CPC Classifications
C; C07; C07C; C07C403/00; C07C403/20; A; A61; A61P; A61P17/00; C07C205/00; C07C205/39; C07C205/42; C07F; C07F9/00; C07F9/02; C07F9/547; C07F9/6564; C07F9/6571; C07F9/6574; C07F9/65744; C07J; C07J41/00; C07J41/0033; C07J41/005; C07C2601/00; C07C2601/12; C07C2601/16
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
77 words
A process for treating a dermatological disease which comprises: (a) administering to a human or animal afflicted with a dermatological disease a composition comprising a photocleavable pro-drug in combination with a pharmaceutical carrier, and (b) irradiating the diseased area with radiation having a wave length of from about 2500 to about 3600 angstroms in an amount sufficient to convert said administered pro-drug to a pharmacologically active form and in a concentration effective to alleviate the said disease.
Claim 2
Dependent Claim
77 words
A process for treating a dermatological disease which comprises: (a) administering to a human or animal afflicted with a dermatological disease a composition comprising a photocleavable pro-drug in combination with a pharmaceutical carrier, and (b) irradiating the diseased area with radiation having a wave length of from about 2500 to about 3600 angstroms in an amount sufficient to convert said administered pro-drug to a pharmacologically active form and in a concentration effective to alleviate the said disease.
Claim 3
Dependent Claim
148 words
A process for treating a dermatological disease which comprises: (a) administering to a human or animal afflicted with a dermatological disease a composition comprising a pro-drug in combination with a pharmaceutical carrier, and (b) irradiating the diseased area with radiation having a wave length of from about 2500 to about 3600 angstroms in an amount sufficient to convert said administered pro-drug to a pharmacologically active form and in a concentration effective to alleviate the said disease, wherein the pro-drug is a compound of the formula: ##STR142## wherein X is H, methoxy, bromine or chloro; R 1 is hydrogen, hydroxy, or acyloxy; R 2 is hydrogen, hydroxy, methyl, fluoro or chloro; and R 1 and R 2 taken together can be ##STR143## R 3 is hydrogen, methyl, chloro, or fluoro; R 4 is hydrogen, chloro or fluoro; R 5 is oxygen, hydroxy or when R 4 is chloro, chloro.
Claim 4
Dependent Claim
148 words
A process for treating a dermatological disease which comprises: (a) administering to a human or animal afflicted with a dermatological disease a composition comprising a pro-drug in combination with a pharmaceutical carrier, and (b) irradiating the diseased area with radiation having a wave length of from about 2500 to about 3600 angstroms in an amount sufficient to convert said administered pro-drug to a pharmacologically active form and in a concentration effective to alleviate the said disease, wherein the pro-drug is a compound of the formula: ##STR142## wherein X is H, methoxy, bromine or chloro; R 1 is hydrogen, hydroxy, or acyloxy; R 2 is hydrogen, hydroxy, methyl, fluoro or chloro; and R 1 and R 2 taken together can be ##STR143## R 3 is hydrogen, methyl, chloro, or fluoro; R 4 is hydrogen, chloro or fluoro; R 5 is oxygen, hydroxy or when R 4 is chloro, chloro.
Claim 5
Dependent Claim
10 words
The process of claim 2 wherein the pro-drug is 11β,17-dihydroxy-6α-methyl-21-[(o-nitrobenzyl)oxy]pregna-1,4-diene-3,20-dione.
Claim 6
Dependent Claim
10 words
The process of claim 2 wherein the pro-drug is 11β,17-dihydroxy-9α-fluoro-16α-methyl-21-[(o-nitrobenzyl)oxy]-pregna-1,4-diene-3,20-dione.
Claim 7
Dependent Claim
10 words
The process of claim 2 wherein the pro-drug is 11β,17-dihydroxy-6α-methyl-21-[(3,4-dimethoxy-6-nitrobenzyl)oxy]-pregna-1,4-diene-3,20-dione.
Claim 8
Dependent Claim
10 words
The process of claim 2 wherein the pro-drug is 11β,17α-dihydroxy-6α-methyl-21-[(o-nitrobenzyl)oxycarbonyl]oxy-pregna-1,4-diene-3,20-dione.
Claim 9
Dependent Claim
10 words
The process of claim 2 wherein the pro-drug is 11β,17-dihydroxy-9α-fluoro-16α-methyl-21-[(o-nitrobenzyl)oxycarbonyl]oxy-pregna-1,4-diene-3,20-dione.
Claim 10
Dependent Claim
10 words
The process of claim 2 wherein the pro-drug is 9α-fluoro-21-[(o-nitrobenzyl)oxycarbonyl]oxy-11β,16,17-trihydroxypregna-1,4-diene-3,20-dione.
Claim 11
Dependent Claim
27 words
The process of claim 2 wherein R 1 is α-hydroxy; R 2 is hydrogen; R 3 is hydrogen; R 4 is hydrogen; and R 5 is β-hydroxy.
Claim 12
Dependent Claim
32 words
The process of claim 2 wherein R 1 is α-hydroxy; R 2 is hydrogen; R 3 is hydrogen; R 4 is hydrogen; R 5 is β-hydroxy, and the 1-2 bond is unsaturated.
Claim 13
Dependent Claim
32 words
The process of claim 2 wherein R 1 is α-hydroxy; R 2 is hydrogen; R 3 is hydrogen; R 4 is α-fluoro; R 5 is β-hydroxy; and the 1-2 bond is unsaturated.
Claim 14
Dependent Claim
32 words
The process of claim 2 wherein R 1 is α-hydroxy; R 2 is hydrogen; R 3 is 6α-methyl; R 4 is hydrogen, R 5 is β-hydroxy and the 1-2 bond is unsaturated.
Claim 15
Dependent Claim
32 words
The process of claim 2 wherein R 1 is α-hydroxy; R 2 is α-methyl; R 3 is hydrogen; R 4 is α-fluoro; R 5 is β-hydroxy; and the 1-2 bond is unsaturated.
Claim 16
Dependent Claim
32 words
The process of claim 2 wherein R 1 is α-hydroxy; R 2 is β-methyl; R 3 is hydrogen; R 4 is α-fluoro; R 5 is β-hydroxy; and the 1-2 bond is unsaturated.
Claim 17
Dependent Claim
30 words
The process of claim 2 wherein R 1 and R 2 are ##STR144## R 3 is hydrogen; R 4 is α-fluoro; R 5 β-hydroxy; and the 1-2 bond is unsaturated.
Claim 18
Dependent Claim
31 words
The process of claim 2 wherein R 1 and R 2 are ##STR145## R 3 is α-fluoro; R 4 is α-fluoro; R 5 is β-hydroxy; and the 1-2 bond is unsaturated.
References Cited (Backward Citations)
US4069322A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1983-11-25 | 1984-05-26 | 1984-11-25 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-11-25 | 1988-05-26 | 1988-11-25 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-11-25 | 1992-05-26 | 1992-11-25 | $7700.00 | Window Closed / Lapsed |