US2014011785A1PendingUtilityA1
Locally active "soft" antiandrogens
Est. expiryMay 3, 2027(~0.8 yrs left)· nominal 20-yr term from priority
Inventors:Richard Hochberg
A61P 5/28A61P 5/00A61P 17/14A61P 17/10A61P 17/08A61P 17/00A61P 17/02C07J 21/003C07C 235/74C07J 1/007C07J 41/0038C07J 1/0051
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Claims
Abstract
The present invention relates to antiandrogenic compounds which may be administered for the treatment of androgen excess in the skin and by way of consequence, the treatment of acne, baldness or hirsuitism in subject or patient. These compounds have the general chemical structure I, II, III or IV:
Claims
exact text as granted — not AI-modified1 . A compound according to the chemical structure:
Where n is 1, 2 or 3; and
R is an optionally substituted C 4 -C 10 group, wherein R is a C 5 -C 10 alkyl group when n=1 and R is an optionally substituted C 4 -C 10 alkyl group when n=2; or
A compound according to the chemical structure:
Wherein n is 1, 2 or 3 and R′ is an optionally substituted C 1 -C 5 alkyl group; or
A compound according to the chemical structure:
Where n is 1, 2 or 3;
R N is a
group or a
group;
j is 2, 3 or 4;
is a 5 or 6 membered heterocyclic group containing at least one nitrogen atom bonded to the carbonyl group, optionally substituted with from 1-3 methyl groups or halogen groups (F, Cl, Br, I, preferably F); and
R 1 and R 2 are each independently H, or an optionally substituted C 1 -C 4 alkyl group; or
A compound according to the chemical structure:
Where R b is an optionally substituted C 1 -C 6 optionally substituted alkyl group.
2 . The compound according to chemical structure IV which is
Where R b is an ethyl group.
3 . The compound according to claim 1 , wherein n is 1 or 2.
4 . The compound according to claim 1 having the chemical structure I, wherein R is a C 4 -C 7 alkyl group.
5 . The compound according to claim 1 having the chemical structure II, wherein R′ is a C 1 -C 3 alkyl group.
6 . The compound according to claim 1 having the chemical structure III, wherein j is 2 or 3.
7 . The compound according to claim 1 having the chemical structure IV, wherein R b is an optionally substituted C 2 or C 3 alkyl group.
8 . The compound according to claim 1 having the chemical structure II, wherein R′ is an ethyl group.
9 . The compound according to claim 1 having the chemical structure III, wherein n is 1 or 2 and j is 2 or 3.
10 . The compound according to claim 1 having the chemical structure III, wherein n is 1 or 2, j is 2 or 3 and R N is a
group.
11 . The compound according to claim 9 wherein
is an optionally substituted piperidine group, a pyrazine group or a morpholine group.
12 . The compound according to claim 1 wherein n is 2, j is 3 and
is an unsubstituted piperidine group.
13 . The compound according to claim 1 wherein
is an optionally substituted piperidine group.
14 . The compound according to claim 1 wherein
is an optionally substituted pyrazine group.
15 . The compound according to claim 1 wherein
is an optionally substituted morpholine group.
16 . The compound according to claim 1 having the chemical structure III, wherein R N is a
group.
17 . The compound according to claim 1 wherein R 1 and R 2 are independently H or a C 1 -C 3 alkyl group.
18 . The compound according to claim 17 wherein R 1 and R 2 are each independently H or CH 3 .
19 . A pharmaceutical composition comprising an effective amount of a compound according to claim 1 in combination with a pharmaceutically acceptable carrier, additive or excipient.
20 . The composition according to claim 19 in topical dosage form.
21 . A method of treating acne in a patient in need thereof comprising administering an effective amount of a composition according to claim 19 to said patient.
22 . A method of treating baldness in a patient in need thereof comprising administering an effective amount of a composition according to claim 19 to said patient.
23 . The method according to claim 22 wherein said baldness is female pattern baldness.
24 . The method according to claim 22 wherein said baldness is male pattern baldness.
25 . A method of treating hirsutism in a patient in need thereof comprising administering an effective amount of a composition according to claim 19 to said patient.
26 . The method according to claim 25 wherein said patient is a female.
27 . A method of treating seborrhea in a patient in need thereof comprising administering an effective amount of a composition according to claim 19 to said patient.
28 . A method of treating androgen excess on the skin of a patient comprising administering to said patient an effective amount of a composition according to claim 19 to said patient.
29 . The method according to claim 28 wherein said androgen excess results in the condition of acne, baldness, hirsutism or seborrhea on the skin of said patient.
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