Photocleavable steroids
First Claim
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1. A compound of the formula:
- ##STR8## wherein R is ##STR9## X is H, methoxy, bromine, or chloro;
R1 is hydrogen or hydroxy, acyloxy wherein acyl is from 2-8 carbon atoms, inclusive;
R2 is hydrogen, hydroxy, methyl, fluoro, or chloro; and
R1 and R2 taken together can be ##STR10## R3 is hydrogen, methyl, chloro, or fluoro;
R4 is hydrogen, chloro or fluoro;
R5 is oxygen, β
-hydroxy or β
-chloro with the proviso that when R5 is β
-chloro R4 is chloro.
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Abstract
This invention relates to novel compounds of the formula: ##STR1## wherein X is H, methoxy, bromine or chloro; R1 is hydrogen or hydroxy, acyloxy wherein acyl is 2 to 8 carbon atoms, R2 is hydrogen, hydroxy, methyl, fluoro or chloro; and R1 and R2 taken together can be ##STR2## R3 is hydrogen, methyl, chloro, or fluoro; R4 is hydrogen, chloro or fluoro; R5 is oxygen, β-hydroxy or β-chloro, with the proviso that when R5 is β-chloro then R4 must be chloro.
The compounds have a photocleavable group (R) which is removable by irradiation. The compounds have reduced activity in the uncleaved state and provide a therapeutically active compound upon irradiation at the site of irradiation.
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Citations
7 Claims
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1. A compound of the formula:
- ##STR8## wherein R is ##STR9## X is H, methoxy, bromine, or chloro;
R1 is hydrogen or hydroxy, acyloxy wherein acyl is from 2-8 carbon atoms, inclusive;
R2 is hydrogen, hydroxy, methyl, fluoro, or chloro; and
R1 and R2 taken together can be ##STR10## R3 is hydrogen, methyl, chloro, or fluoro;
R4 is hydrogen, chloro or fluoro;
R5 is oxygen, β
-hydroxy or β
-chloro with the proviso that when R5 is β
-chloro R4 is chloro. - View Dependent Claims (2, 3, 4, 5, 6, 7)
- ##STR8## wherein R is ##STR9## X is H, methoxy, bromine, or chloro;
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Current AssigneeThe Upjohn Company (Pharmacia Corp.)
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Original AssigneeThe Upjohn Company (Pharmacia Corp.)
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InventorsWierenga, Wendell
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Primary Examiner(s)Roberts, Elbert L.
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Application NumberUS05/787,167Time in Patent Office377 DaysField of Search260/397.45US Class Current552/566CPC Class CodesA61P 17/16 Emollients or protectives, ...A61P 29/00 Non-central analgesic, anti...C07J 41/0033 not covered by C07J41/0005C07J 41/005 the 17-beta position being ...
