US2011003860A1PendingUtilityA1
Hydroxyl compounds and compositions for cholesterol management and related uses
Est. expiryJan 23, 2023(expired)· nominal 20-yr term from priority
A61P 43/00A61P 9/00A61P 9/12A61P 3/10A61P 9/10A61P 5/50A61P 7/00A61P 3/08A61P 3/06A61P 7/02A61P 27/02A61P 29/00A61P 35/00A61P 25/16A61P 25/28A61P 3/04A61P 3/00A61P 31/04A61P 25/00A61P 19/02A61P 11/06A61P 13/12A61P 21/00A61P 1/18A61P 15/10A61P 17/00A61P 19/06A61P 1/04A61P 1/00C07D 309/10C07F 9/4423C07D 405/12A61K 31/20C07C 62/06C07C 59/48C07C 31/20C07D 307/33C07F 9/094C07C 31/27C07C 61/12C07F 9/2425C07C 59/01C07C 31/22C07C 69/017C07C 31/24C07D 261/08C07C 59/54C07C 59/29C07D 309/30C07C 65/17C07D 257/04C07C 69/757C07C 59/46A61K 31/23C07C 62/02C07C 59/105C07C 59/245A61K 31/194C07C 2601/04C07F 9/2416C07C 69/675C07C 59/11C07D 261/12C07C 309/25C07C 59/285C07D 495/04C07F 9/2408C07C 47/34C07C 2601/08C07C 2601/02C07D 309/12C07C 309/08C07D 213/80C07F 9/242C07F 9/093C07D 305/12A61K 31/191C07C 309/24C07F 9/12C07C 33/26C07F 9/11C07C 69/003C07F 9/117C07C 255/00C07C 47/19
63
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Claims
Abstract
The present invention relates to novel hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, pancreatitius, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
Claims
exact text as granted — not AI-modified1 - 34 . (canceled)
35 . A method according to claim 38 wherein said compound is selected from the group consisting of
or a pharmaceutically acceptable salt thereof.
36 - 37 . (canceled)
38 . A method for treating or preventing aging, Alzheimer's Disease, asthma, cancer, cardiomyopathy, cardiovascular disease, chronic obstructive airway disease, diabetes, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, metabolic syndrome disorder, obesity, oxysterol elimination in bile, pancreatitis, pancreatitius, Parkinson's disease, a peroxisome proliferator activated receptor associated disorder, phospholipid elimination in bile, renal disease, septicemia, thrombotic disorder, or enhancing bile production in a patient comprising administering to a patient in need of such treatment or prevention a therapeutically or prophylactically effective amount of a compound of the formula
or a pharmaceutically acceptable salt, hydrate, solvate or mixture thereof, wherein:
(a) a each occurrence of m is independently an integer ranging from 0 to 5;
(b) each occurrence of n is independently an integer ranging from 3 to 7;
(c) X is (CH 2 ) z or Ph, wherein z is an integer ranging from 0 to 4 and Ph is a 1,2-, 1,3-, or 1,4 substituted phenyl group;
(d) each occurrence of R 1 , R 2 , R 11 , and R 12 is independently H, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl, phenyl, or benzyl, wherein R 1 , R 2 , R 11 , and R 12 are not each simultaneously H; and
(e) each occurrence of Y 1 and Y 2 independently (C 1 -C 6 )alkyl, OH, COOH, COOR 3 , SO 3 H,
wherein:
(i) Y 1 and Y 2 are not each simultaneously (C 1 -C 6 )alkyl;
(ii) R 3 is (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl, phenyl, or benzyl and is unsubstituted or substituted with one or more halo, OH, (C 1 -C 6 )alkoxy, or phenyl groups,
(iii) each occurrence of R 4 is independently H, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, or (C 2 -C 6 )alkynyl and is unsubstituted or substituted with one or two halo, OH, C 1 -C 6 alkoxy, or phenyl groups; and
(iv) each occurrence of R 5 is independently H, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, or (C 2 -C 6 )alkynyl.
39 . A method according to claim 38 wherein the disease or condition is a cardiovascular disease.
40 . A method according to claim 38 wherein the disease or condition is a dyslipidemia.
41 . A method according to claim 38 wherein the disease or condition is a dyslipoproteinemia.
42 . A method according to claim 38 wherein the disease or condition is a disorder of glucose metabolism.
43 - 52 . (canceled)
53 . A method according to claim 38 wherein the disease or condition is inflammation.
54 - 57 . (canceled)
58 . A method according to claim 38 wherein the disease or condition is metabolic syndrome disorders.
59 . A method of increasing HDL levels, which comprises administering to a patient in need of such treatment a therapeutically effective amount of a compound of the formula
or a pharmaceutically acceptable salt, hydrate, solvate or mixture thereof, wherein:
(a) each occurrence of m is independently an integer ranging from 0 to 5;
(b) each occurrence of n is independently an integer ranging from 3 to 7;
(c) X is (CH 2 ) z or Ph, wherein z is an integer ranging from 0 to 4 and Ph is a 1,2-, 1,3-, or 1,4 substituted phenyl group;
(d) each occurrence of R 1 , R 2 , R 11 , and R 12 is independently H, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl, phenyl, or benzyl, wherein R 1 , R 2 , R 11 , and R 12 are not each simultaneously H; and
(e) each occurrence of Y 1 and Y 2 is independently (C 1 -C 6 )alkyl, OH, COOH, COOR 3 , SO 3 H,
wherein:
(i) Y 1 and Y 2 are not each simultaneously (C 1 -C 6 )alkyl;
(ii) R 3 is (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl, phenyl, or benzyl and is unsubstituted or substituted with one or more halo, OH, (C 1 -C 6 )alkoxy, or phenyl groups,
(iii) each occurrence of R 4 is independently H, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, or (C 2 -C 6 )alkynyl and is unsubstituted or substituted with one or two halo, OH, C 1 -C 6 alkoxy, or phenyl groups; and
(iv) each occurrence of R 5 is independently H, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, or (C 2 -C 6 )alkynyl.
60 . A method of lowering LDL levels, which comprises administering to a patient in need of such treatment a therapeutically effective amount of a compound of the formula
or a pharmaceutically acceptable salt, hydrate, solvate or mixture thereof, wherein:
(a) each occurrence of m is independently an integer ranging from 0 to 5;
(b) each occurrence of n is independently an integer ranging from 3 to 7;
(c) X is (CH 2 ) z or Ph, wherein z is an integer ranging from 0 to 4 and Ph is a 1,2-, 1,3-, or 1,4 substituted phenyl group;
(d) each occurrence of R 1 , R 2 , R 11 , and R 12 is independently H, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl, phenyl, or benzyl, wherein R 1 , R 2 , R 11 , and R 12 are not each simultaneously H; and
(e) each occurrence Y 1 and Y 2 independently (C 1 -C 6 )alkyl, OH, COOH, COOR 3 , SO 3 H,
wherein:
(i) Y 1 and Y 2 are not each simultaneously (C 1 -C 6 )alkyl;
(ii) R 3 is (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl, phenyl, or benzyl and is unsubstituted or substituted with one or more halo, OH, (C 1 -C 6 )alkoxy, or phenyl groups,
(iii) each occurrence of R 4 is independently H, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, or (C 2 -C 6 )alkynyl and is unsubstituted or substituted with one or two halo, OH, C 1 -C 6 alkoxy, or phenyl groups; and
(iv) each occurrence of R 5 is independently H, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, or (C 2 -C 6 )alkynyl.
61 . (canceled)
62 . A method of lowering elevated levels of blood glucose comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound of the formula
or a pharmaceutically acceptable salt, hydrate, solvate or mixture thereof, wherein:
(a) each occurrence of in is independently an integer ranging from 0 to 5;
(b) each occurrence of is independently an integer ranging from 3 to 7;
(c) X is (CH 2 ) z or Ph, wherein z is an integer from 0 to 4 and Ph is a 1,2-, 3-, or 1,4 substituted phenyl group;
(d) each occurrence of R 1 , R 2 , R 11 , and R 12 is independently H, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl, phenyl, or benzyl, wherein R 1 , R 2 , R 11 , and R 12 are not each simultaneously H; and
(e) each occurrence of Y 1 and Y 2 is independently (C 1 -C 6 )alkyl, OH, COOH, COOR 3 , SO 3 H,
wherein:
(i) Y 1 and Y 2 are not each simultaneously (C 1 -C 6 )alkyl;
(ii) R 3 is (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl, phenyl, or benzyl and is unsubstituted or substituted with one or more halo, OH, (C 1 -C 6 )alkoxy, or phenyl groups,
(iii) each occurrence of R 4 is independently H, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, or (C 2 -C 6 )alkynyl and is unsubstituted or substituted with one or two halo, OH, C 1 -C 6 alkoxy, or phenyl groups; and
(iv) each occurrence of R 5 is independently H, (C 1 -C 6 )alkyl, C 2 -C 6 )alkenyl, or (C 2 -C 6 )alkynyl.
63 . A method according to claim 59 wherein said compound is selected from the group consisting of
7-Hydroxy-2,2,12,12-tetramethyl-pentadecanedioic acid;
or a pharmaceutically acceptable salt thereof.
64 . A method according to claim 60 wherein said compound is selected from the group consisting of
7-Hydroxy-2,2,12,12-tetramethyl-pentadecanedioic acid;
or a pharmaceutically acceptable salt thereof.
65 . A method according to claim 38 wherein said compound is selected from the group consisting of
or a pharmaceutically acceptable salt thereof.
66 . A method according to claim 59 wherein said compound is selected from the group consisting of
or a pharmaceutically acceptable salt thereof.
67 . A method according to claim 60 wherein said compound is selected from the group consisting of
or a pharmaceutically acceptable salt thereof.
68 . A method according to claim 38 wherein the compound is
8-Hydroxy-2,2,14,14-tetramethyl-pentadecanedioic acid;
or a pharmaceutically acceptable salt thereof.
69 . A method according to claim 59 wherein the compound is
8-Hydroxy-2,2,14,14-tetramethyl-pentadecanedioic acid;
or a pharmaceutically acceptable salt thereof.
70 . A method according to claim 60 wherein the compound is
8-Hydroxy-2,2,14,14-tetramethyl-pentadecanedioic acid;
or a pharmaceutically acceptable salt thereof.
71 . A method according to claim 39 wherein the compound is
8-Hydroxy-2,2,14,14-tetramethyl-pentadecanedioic acid;
or a pharmaceutically acceptable salt thereof.
72 . A method according to claim 40 wherein the compound is
8-Hydroxy-2,2,14,14-tetramethyl-pentadecanedioic acid;
or a pharmaceutically acceptable salt thereof.
73 . A method according to claim 41 wherein the compound is
8-Hydroxy-2,2,14,14-tetramethyl-pentadecanedioic acid;
or a pharmaceutically acceptable salt thereof.
74 . A method according to claim 42 wherein the compound is
8-Hydroxy-2,2,14,14-tetramethyl-pentadecanedioic acid;
or a pharmaceutically acceptable salt thereof.
75 . A method according to claim 53 wherein the compound is
8-Hydroxy-2,2,14,14-tetramethyl-pentadecanedioic acid;
or a pharmaceutically acceptable salt thereof.
76 . A method according to claim 58 wherein the compound is
8-Hydroxy-2,2,14,14-tetramethyl-pentadecanedioic acid;
or a pharmaceutically acceptable salt thereof.
77 . A method according to claim 62 wherein the compound is
8-Hydroxy-2,2,14,14-tetramethyl-pentadecanedioic acid;
or a pharmaceutically acceptable salt thereof.Join the waitlist — get patent alerts
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