US2017312246A1PendingUtilityA1
Lipidic furan, pyrrole, and thiophene compounds for use in the treatment of atrophic vaginitis
Est. expiryApr 27, 2036(~9.8 yrs left)· nominal 20-yr term from priority
Inventors:Richard Huber
A61K 47/44A61P 15/02A61K 9/0014A61K 9/0034C07D 307/36A61K 31/40A61K 31/341A61K 9/4875A61K 31/381A61K 9/02A61K 45/06
60
PatentIndex Score
0
Cited by
0
References
0
Claims
Abstract
Provided herein are lipidic furan, pyrrole, and thiophene compounds, compositions, and methods using such compounds and compositions for the treatment of atrophic vaginitis. Specifically, the invention includes administering an effective amount of a compound of Formula I, I′, or I″, or a pharmaceutically acceptable composition, salt, isotopic analog, prodrug, or combination thereof, to a subject suffering from atrophic vaginitis.
Claims
exact text as granted — not AI-modified1 . A compound of Formula I(ap)
2 . A compound of Formula I(aq)
3 . A method for the treatment of atrophic vaginitis in a host, comprising administering an effective amount of a compound of Formula I, I′, or I″ to a host in need thereof:
wherein;
each Z is independently O, S or NR 5 ;
wherein R 1 , R 2 , R 3 and R 4 , are the same or different, separately represent a hydrogen atom, a C 1 -C 35 alkyl radical; a C 1 -C 35 alkenyl radical; or a C 1 -C 35 alkynyl radical; said alkyl, alkenyl and alkynyl radicals optionally substituted by one or more halogens and/or by one or more functions chosen from the group consisting of epoxy, hydroxyl (—OH), thiol (—SH), ether (OR 5 ), primary amine (—NH 2 ), secondary amine (—NHR 5 ), tertiary amine (—NR 5 R 6 ), aldehyde (—CHO), ketone (—COR 5 ), acetyl (—O—CO—R 5 ) functions wherein R 5 and R 6 separately represent a hydrogen atom, a C 1 -C 35 alkyl radical, a C 1 -C 35 alkenyl radical, or a C 1 -C 35 alkynyl radical.
4 . The method of claim 3 , wherein R 1 , R 2 , R 3 , or R 4 is an alkyl radical, an alkenyl radical, or an alkynyl radical having a carbon chain comprising C 2 -C 35 .
5 . The method of claim 3 , wherein R 1 , R 2 , R 3 or R 4 is an alkyl radical, an alkenyl radical, or an alkynyl radical having a carbon chain comprising C 10 -C 22 .
6 . The method of claim 3 , wherein R 1 , R 2 , R 3 or R 4 is an alkyl radical, an alkenyl radical, or an alkynyl radical having a carbon chain comprising C 13 -C 17 .
7 . The method of claim 3 , wherein R 5 or R 6 , is an alkyl radical, an alkenyl radical, or an alkynyl radical having a carbon chain comprising C 10 -C 22 .
8 . The method of claim 3 , wherein R 5 or R 6 , is an alkyl radical, an alkenyl radical, or an alkynyl radical having a carbon chain comprising C 13 -C 17 .
9 . The method of claim 3 , wherein the compound is:
wherein;
Z is independently O, S, NR 5 ;
R 1 ═R 2 ═R 3 ═H;
R 4 is a C 9 -C 20 alkyl chain comprising two or more double bonds optionally substituted as defined above.
10 . The method of claim 3 , wherein the compound is:
wherein;
R 1 is a C 9 -C 20 alkyl chain comprising two or more double bonds optionally substituted as defined above.
11 . The method of claim 3 , wherein the compound is selected from:
Formula I(n)
Formula I(o)
Formula I(p)
Formula I(q)
Formula I(r)
Formula I(s)
Formula I(t)
Formula I(u)
Formula I(v)
Formula I(w)
Formula I(x)
Formula I(y)
Formula I(z)
Formula I(aa)
Formula I(ab)
Formula I(ac)
Formula I(ad)
Formula I(ae)
Formula I(af)
Formula I(ag)
Formula I(ah)
Formula I(ai)
Formula I(aj)
Formula I(ak)
Formula I(al)
Formula I(am)
Formula I(an)
Formula I(ao)
Formula I(ap)
Formula I(aq)
12 . The method of claim 3 , wherein the compound is Formula I(n):
13 . The method of claim 3 , wherein the compound is Formula I(ap):
14 . The method of claim 3 , wherein the compound is Formula I(aq):
15 . The method of claim 3 , further comprising administering an estrogenic agent.
16 . The method of claim 15 , wherein the estrogenic agent is Estradiol Vaginal Cream, Estradiol Vaginal (local), Conjugated Estrogens, Estradiol Transdermal, Estradiol, Estradiol Patch, Estradiol topical (for use on skin), Estradiol and Norethindrone, Estradiol Valerate, Estradiol Cypionate, Conjugated Estrogens (synthetic a), Conjugated Estrogens (oral), Esterified Estrogens, Conjugated Estrogens and Medroxyprogesterone, or Estropipate.
17 . The method of claim 3 , wherein the host is a human.
18 . The method of claim 3 , wherein the compound is administered topically.
19 . The method of claim 3 , wherein the compound is administered as a vaginal suppository.
20 . The method of claim 12 , wherein the compound is administered topically.
21 . The method of claim 12 , wherein the compound is administered as a vaginal suppository.Cited by (0)
No later patents cite this yet.
References (0)
No backward citations on record.