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Last Updated: March 29, 2024

Claims for Patent: 10,118,881


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Summary for Patent: 10,118,881
Title:Hydroxyl compounds and compositions for cholesterol management and related uses
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.
Inventor(s): Dasseux; Jean-Louis H. (Toulouse, FR), Oniciu; Carmen D. (Toulouse, FR)
Assignee: Esperion Therapeutics, Inc. (Ann Arbor, MI)
Application Number:15/487,623
Patent Claims: 1. A method for treating dyslipidemia in a human patient, comprising orally administering to a human patient in need of such treatment a therapeutically effective amount of a compound of formula I to treat the dyslipidemia, wherein formula I is represented by: ##STR00099## or a pharmaceutically acceptable salt 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.sub.2).sub.z, wherein z is an integer from 0 to 4; (d) each occurrence of R.sup.1, R.sup.2, R.sup.11, and R.sup.12 is independently H, (C.sub.1-C.sub.6)alkyl, or phenyl, wherein R.sup.1, R.sup.2, R.sup.11, and R.sup.12 are not each simultaneously H; and (e) each occurrence of Y.sup.1 and Y.sup.2 is independently OH, COOH, COOR.sup.3, ##STR00100## wherein R.sup.3 is (C.sub.1-C.sub.6)alkyl, phenyl, or benzyl and is unsubstituted or substituted with one or more halo, OH, or (C.sub.1-C.sub.6)alkoxy.

2. The method of claim 1, wherein each occurrence of Y.sup.1 and Y.sup.2 is independently OH, COOR.sup.3, or COOH.

3. The method of claim 1, wherein m is 0.

4. The method of claim 1, wherein n is 5.

5. The method of claim 1, wherein z is 0.

6. The method of claim 5, wherein R.sup.1, R.sup.2, R.sup.11, and R.sup.12 are (C.sub.1-C.sub.6)alkyl.

7. The method of claim 6, wherein Y.sup.1 and Y.sup.2 is COOH.

8. The method of claim 1, wherein the compound of formula I is the following: ##STR00101## or a pharmaceutically acceptable salt thereof.

9. The method of claim 1, wherein the compound of formula I is the following: ##STR00102##

10. A method for treating hypercholesterolemia in a human patient, comprising orally administering to a human patient in need of such treatment a therapeutically effective amount of a compound of formula I to treat the hypercholesterolemia, wherein formula I is represented by: ##STR00103## or a pharmaceutically acceptable salt 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.sub.2).sub.z, wherein z is an integer from 0 to 4; (d) each occurrence of R.sup.1, R.sup.2, R.sup.11, and R.sup.12 is independently H, (C.sub.1-C.sub.6)alkyl, or phenyl, wherein R.sup.1, R.sup.2, R.sup.11, and R.sup.12 are not each simultaneously H; and (e) each occurrence of Y.sup.1 and Y.sup.2 is independently OH, COOH, COOR.sup.3, ##STR00104## wherein R.sup.3 is (C.sub.1-C.sub.6)alkyl, phenyl, or benzyl and is unsubstituted or substituted with one or more halo, OH, or (C.sub.1-C.sub.6)alkoxy.

11. The method of claim 10, wherein each occurrence of Y.sup.1 and Y.sup.2 is independently OH, COOR.sup.3, or COOH.

12. The method of claim 10, wherein m is 0.

13. The method of claim 10, wherein n is 5.

14. The method of claim 10, wherein z is 0.

15. The method of claim 14, wherein R.sup.1, R.sup.2, R.sup.11, and R.sup.12 are (C.sub.1-C.sub.6)alkyl.

16. The method of claim 15, wherein Y.sup.1 and Y.sup.2 is COOH.

17. A method for treating hypercholesterolemia in a human patient, comprising orally administering to a human patient in need of such treatment a therapeutically effective amount of a compound of formula I to treat the hypercholesterolemia, wherein formula I is represented by: ##STR00105## or a pharmaceutically acceptable salt thereof.

18. The method of claim 17, wherein the compound of formula I is the following: ##STR00106##

19. The method of claim 10, wherein the compound of formula I is orally administered to the human patient in the form of a pharmaceutical composition that comprises said compound of formula I.

20. The method of claim 17, wherein the compound of formula I is orally administered to the human patient in the form of a pharmaceutical composition that comprises said compound of formula I.

21. The method of claim 18, wherein the compound of formula I is orally administered to the human patient in the form of a pharmaceutical composition that comprises said compound of formula I.

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