US2017173004A1PendingUtilityA1
Methods For Treating Inflammatory Conditions
Est. expiryNov 10, 2026(~0.3 yrs left)· nominal 20-yr term from priority
A61K 31/497A61K 8/494A61K 2800/10A61K 2800/92A61K 9/0019A61Q 19/00A61K 9/0053A61K 31/496
53
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Claims
Abstract
The present invention relates to compounds and pharmaceutically acceptable salts thereof and formulations comprising tenilsetam or pharmaceutically acceptable salts thereof that are useful in modulating inflammation. In particular, the compounds or pharmaceutically acceptable salts thereof are useful for treating or preventing a disease or disorder involving inflammation, including, but not limited to, delayed type hypersensitivity and contact hypersensitivity.
Claims
exact text as granted — not AI-modified1 - 25 . (canceled)
26 . A method of enhancing the appearance of the skin of a human comprising administering to the human in need thereof a pharmaceutical composition comprising a therapeutically effective amount of a compound of formula I
and pharmaceutically acceptable carrier, wherein:
X is 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, or phenyl, each unsubstituted, mono-substituted, di-substituted, or tri-substituted with, independently, OH, halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, or (C 1 -C 4 )alkoxy-(C 1 -C 4 ) alkyl;
R 1 and R 4 are, independently, H or C 1 -C 4 alkyl;
R 2a and R 2b are, independently, H, OH, or C 1 -C 4 alkyl, or, together, R 2a and R 2b are C═O;
R 3a and R 3b are, independently, H, OH, or C 1 -C 4 alkyl, or, together, R 3a and R 3b are C═O; and
R X is H, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, or (C 1 -C 4 ) alkoxy-(C 1 -C 4 ) alkyl;
or a pharmaceutically acceptable salt thereof, wherein the compound of formula I is administered in the absence of another therapeutic agent; and
wherein the enhancement of the appearance of the skin is one or more of increased softness of the skin, increased turgor of the skin, decreased redness, and decreased swelling.
27 . The method of claim 26 wherein X is 2-thienyl, 3-thienyl, 2-furyl, or 3-furyl, each unsubstituted, mono-substituted, or di-substituted with, independently, OH, halogen, C 1 -C 4 alkyl, or C 1 -C 4 alkoxy.
28 . The method of claim 26 wherein X is unsubstituted 2-thienyl or 2-thienyl mono-substituted with OH, halogen, or C 1 -C 4 alkyl.
29 . The method of claim 26 wherein X is unsubstituted 2-thienyl.
30 . The method of claim 26 wherein R 1 and R 4 are H or C 1 -C 4 alkyl.
31 . The method of claim 26 wherein R 2a and R 2b are, independently, H or C 1 -C 4 alkyl, or, together, R 2a and R 2b are C═O.
32 . The method of claim 26 wherein R 2a and R 2b are both H.
33 . The method of claim 26 wherein R 3a and R 3b are, independently, H or C 1 -C 4 alkyl, or, together, R 3a and R 3b are C═O.
34 . The method of claim 26 wherein R 3a and R 3b are both H.
35 . The method of claim 26 wherein R X is H, C 1 -C 4 alkyl, or C 1 -C 4 alkoxy.
36 . The method of claim 26 wherein R X is H.
37 . The method of claim 26 wherein:
X is unsubstituted 2-thienyl or 2-thienyl mono-substituted with OH, halogen, or C 1 -C 4 alkyl;
R 1 and R 4 are, independently, H or C 1 -C 4 alkyl;
R 2a and R 2b are, independently, H or OH;
R 3a and R 3b are, independently, H or OH; and
R X is H.
38 . The method of claim 26 wherein:
X is unsubstituted 2-thienyl or 2-thienyl mono-substituted with OH, halogen, or C 1 -C 4 alkyl; and
R 1 , R 4 , R 2a , R 2b , R 3a , R 3b , and R X are H.
39 . The method of claim 26 wherein:
X is unsubstituted 2-thienyl; and
R 1 , R 4 , R 2a , R 2b , R 3a , R 3b , and R X are H.
40 . The method of claim 26 wherein the pharmaceutical composition is administered to the human topically.
41 . The method of claim 40 wherein the pharmaceutical composition is applied to the skin as a topical cream, liquid solution, or dispersion.
42 . The method of claim 40 wherein the pharmaceutical composition is formulated as a bar, liquid, paste, mousse, cream, gel, aerosol, lotion, hair shampoo, hair lotion, beach oil, foam bath, shower bath, alcoholic and aqueous/alcoholic solution, emulsion, wax/fat compound, stick preparation, spray, powder, or ointment.
43 . The method of claim 40 wherein the pharmaceutical composition further comprises collagen, hyaluronic acid, elastin, hydrolysate, primrose oil, jojoba oil, epidermal growth factor, soybean saponin, or mucopolysaccharide, or any mixture thereof; or wherein the pharmaceutical composition further comprises a superfatting agent, pearlizing wax, consistency factor, thickener, polymer additive, silicone compound, fat, oil, wax, stabilizer, biogenic agent, deodorizer, anti-dandruff agent, film former, foam stabilizer, electrolyte, swelling agent, UV protection factor, hydrotrope, preservative, bactericide, perfume, dye, pigment, moisturizer and/or humectant, insect repellent, self-tanning agent, solubilizer, germ inhibitor, benofuran derivative, retinoid, or chelating agent.
44 . The method of claim 26 wherein the pharmaceutical composition is administered to the human orally.
45 . The method of claim 44 wherein the pharmaceutical composition is formulated as a tablet, lozenge, aqueous or oily suspension, granule, powder, emulsion, capsule, syrup, or elixir.Cited by (0)
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