Claims for Patent: 10,941,095

Summary for Patent: 10,941,095

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:	16/142,547
Patent Claims:	1. A method of lowering LDL cholesterol in a human in need thereof, comprising administering to the human a therapeutically effective amount of a compound of formula I, wherein formula I is represented by: ##STR00106## 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, ##STR00107## 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, and R.sup.11 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: ##STR00108## or a pharmaceutically acceptable salt thereof. 9. The method of claim 1, wherein the compound of formula I is the following: ##STR00109## 10. The method of claim 1, wherein the compound is administered orally to the human. 11. A method of lowering LDL cholesterol in a human in need thereof, comprising administering to the human a therapeutically effective amount of a compound of formula I, wherein formula I is represented by: ##STR00110## or a pharmaceutically acceptable salt thereof. 12. The method of claim 11, wherein the compound of formula I is: ##STR00111## 13. The method of claim 1, wherein the compound of formula I is orally administered to the human in the form of a pharmaceutical composition comprising the compound of formula I, and a pharmaceutically acceptable vehicle. 14. The method of claim 11, wherein the compound of formula I is orally administered to the human in the form of a pharmaceutical composition comprising the compound of formula I, and a pharmaceutically acceptable vehicle. 15. The method of claim 12, wherein the compound of formula I is orally administered to the human in the form of a pharmaceutical composition comprising the compound of formula I, and a pharmaceutically acceptable vehicle. 16. The method of claim 1, wherein the human has familial hypercholesterolemia. 17. The method of claim 1, wherein the human has cardiovascular disease. 18. The method of claim 17, wherein the cardiovascular disease is atherosclerotic cardiovascular disease. 19. The method of claim 11, wherein the human has familial hypercholesterolemia. 20. The method of claim 11, wherein the human has cardiovascular disease. 21. The method of claim 20, wherein the cardiovascular disease is atherosclerotic cardiovascular disease. 22. The method of claim 12, wherein the human has familial hypercholesterolemia. 23. The method of claim 12, wherein the human has cardiovascular disease. 24. The method of claim 23, wherein the cardiovascular disease is atherosclerotic cardiovascular disease.