US2021085626A1PendingUtilityA1
Substituted aromatic compounds and pharmaceutical compositions for tissue self-repair and regeneration
Est. expiryNov 12, 2034(~8.3 yrs left)· nominal 20-yr term from priority
A61K 31/192A61P 17/00A61K 8/19A61K 8/37A61K 33/00A61K 31/216A61Q 19/08A61K 8/36C07C 59/52C07C 57/58C07C 57/32C07C 57/30A61P 17/02A61K 8/365A61P 43/00C07C 59/84A61P 19/08
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Claims
Abstract
Described herein are compounds of Formula I, or pharmaceutically acceptable salts thereof, or combinations thereof, as well as uses thereof. Such uses include promoting tissue self-repair or tissue regeneration of an organ, stimulating the generation of tissue growth, modulating (e.g., increasing) the level of a tissue-repair marker, treating physical injury in an organ, tissue or cell, promoting wound healing, as well as anti-aging applications. Corresponding compositions, methods, kits, and uses are also described. Formula I wherein A is C5 alkyl, C6 alkyl, C5 alkenyl, C6 alkenyl, C(O)—(CH2)n—CH3 or CH(OH)—(CH2)n—CH3 wherein n is 3 or 4; R1 is H, F of OH; R2 is H, F, OH, C5 alkyl, C6 alkyl, C5 alkenyl, C6 alkenyl, C(O)—(CH2)n—CH3 or CH(OH)—(CH2)n—CH3 wherein n is 3 or 4; R3 is H, F, OH, or CH2Ph; R4 is H, F or OH; Q is 1) (CH2), C(O)OH wherein m is 1 or 2 2) CH(CH3)C(O)OH, 3) C(CH3)2C(O)OH, 4) CH(F)—C(O)OH, 5) CF2—C(O)OH or 6) C(O)—C(O)OH.
Claims
exact text as granted — not AI-modified1 . (canceled)
2 . A method for stimulating tissue growth or regeneration in an organ or tissue of a subject in need thereof, wherein the organ or tissue is bladder, ovary, prostate, spleen, breast, blood vessel or a neural tissue, the method comprising administering to the subject an effective amount of a compound represented by Formula I or a pharmaceutically acceptable salt thereof:
wherein
A is C 5 alkyl, C 6 alkyl, C 5 alkenyl, C 6 alkenyl, C(O)—(CH 2 ) n —CH 3 or CH(OH)—(CH 2 ) n —CH 3 wherein n is 3 or 4;
R 1 is H, F or OH;
R 2 is H, F, OH, C 5 alkyl, C 6 alkyl, C 5 alkenyl, C 6 alkenyl, C(O)—(CH 2 ) n —CH 3 or CH(OH)—(CH 2 ) n —CH 3 wherein n is 3 or 4;
R 3 is H, F, OH or CH 2 Ph;
R 4 is H, F or OH;
Q is
1) (CH 2 ) m C(O)OH wherein m is 1 or 2,
2) CH(CH 3 )C(O)OH,
3) C(CH 3 ) 2 C(O)OH,
4) CH(F)—C(O)OH,
5) CF 2 —C(O)OH, or
6) C(O)—C(O)OH.
3 . The method according to claim 2 , wherein A is C 5 alkyl or C 6 alkyl.
4 . The method according to claim 2 , wherein R 2 is H, F, OH, C 5 alkyl or C 6 alkyl.
5 . The method according to claim 2 , wherein R 3 is H, OH or CH 2 Ph.
6 . The method according to claim 2 , wherein Q is (CH 2 ) m C(O)OH where m is 1 or 2.
7 . The method according to claim 2 , wherein A is C 5 alkyl or C 6 alkyl; R 1 is H, F or OH; R 2 is H, F, OH, C 5 alkyl or C 6 alkyl; R 3 is H, OH or CH 2 Ph; R 4 is H, F or OH; and Q is (CH 2 ) m C(O)OH where m is 1 or 2.
8 . The method according to claim 2 , wherein A is C 5 alkyl; R 1 is H; R 2 is H or C 5 alkyl; R 3 is H; R 4 is H; and Q is (CH 2 ) m C(O)OH where m is 1.
9 . The method according to claim 2 , wherein said compound or pharmaceutically acceptable salt thereof is:
or a pharmaceutically acceptable salt thereof.
10 . The method according to claim 9 , wherein said compound or pharmaceutically acceptable salt thereof is:
or pharmaceutically acceptable salt thereof.
11 . The method according to claim 9 , wherein said compound or pharmaceutically acceptable salt thereof is:
or pharmaceutically acceptable salt thereof.
12 . The method according to claim 2 , wherein the pharmaceutically acceptable salt is a base addition salt comprising a metal counterion selected from the group consisting of sodium, potassium, calcium, magnesium, lithium, ammonium, manganese, zinc, iron, or copper.
13 . The method according to claim 12 , wherein the pharmaceutically acceptable salt is sodium.
14 . The method according to claim 2 , wherein the organ or tissue is an injured organ or tissue.
15 . A method for increasing the expression of a tissue self-repair marker or a tissue regeneration marker in an organ or tissue of a subject, wherein the organ or tissue is bladder, ovary, prostate, spleen, breast, blood vessel or a neural tissue, the method comprising the step of administering to a subject in need of tissue regeneration a compound represented by Formula I or a pharmaceutically acceptable salt thereof:
wherein
A is C 5 alkyl, C 6 alkyl, C 5 alkenyl, C 6 alkenyl, C(O)—(CH 2 ) n —CH 3 or CH(OH)—(CH 2 ) n —CH 3 wherein n is 3 or 4;
R 1 is H, F or OH;
R 2 is H, F, OH, C 5 alkyl, C 6 alkyl, C 5 alkenyl, C 6 alkenyl, C(O)—(CH 2 ) n —CH 3 or CH(OH)—(CH 2 ) n —CH 3 wherein n is 3 or 4;
R 3 is H, F, OH or CH 2 Ph;
R 4 is H, F or OH;
Q is 1) (CH 2 ) m C(O)OH wherein m is 1 or 2,
2) CH(CH 3 )C(O)OH,
3) C(CH 3 ) 2 C(O)OH,
4) CH(F)—C(O)OH,
5) CF 2 —C(O)OH, or
6) C(O)—C(O)OH.
16 . The method according to claim 15 , wherein said compound or a pharmaceutically acceptable salt thereof is:
and pharmaceutically acceptable salts thereof.
17 . The method according to claim 16 , wherein said compound or pharmaceutically acceptable salt thereof is:
or pharmaceutically acceptable salt thereof.
18 . The method according to claim 16 , wherein said compound or pharmaceutically acceptable salt thereof:
or pharmaceutically acceptable salt thereof.
19 . The method according to claim 15 , wherein the marker is a metalloproteinase or a growth factor.
20 . The method according to claim 15 , wherein the marker is hepatocyte growth factor (HGF) or Serpin A1 (AAT).
21 . The method according to claim 15 , wherein the marker is Serpin A1 (AAT) and wherein the tissue or a neural tissue.Join the waitlist — get patent alerts
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