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Last Updated: November 22, 2024

Claims for Patent: 7,335,799


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Summary for Patent: 7,335,799
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 Henri (Brighton, MI), Oniciu; Carmen Daniela (Ann Arbor, MI)
Assignee: Esperion Therapeutics, Inc. (Ann Arbor, MI)
Application Number:10/743,470
Patent Claims: 1. A compound of the formula I: ##STR00109## 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.sub.2).sub.z or Ph, wherein z is an integer from 0 to 4 and Ph is a 1,2-, 1,3-, or 1,4 substituted phenyl group; (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, (C.sub.2-C.sub.6)alkenyl, (C.sub.2-C.sub.6)alkynyl, phenyl, or benzyl, 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 (C.sub.1-C.sub.6)alkyl, OH, COOH, COOR.sup.3, SO.sub.3H, ##STR00110## wherein: (i) Y.sup.1 and Y.sup.2 are not each simultaneously (C.sub.1-C.sub.6)alkyl; (ii) R.sup.3 is (C.sub.1-C.sub.6)alkyl, (C.sub.2-C.sub.6)alkenyl, (C.sub.2-C.sub.6)alkynyl, phenyl, or benzyl and is unsubstituted or substituted with one or more halo, OH, (C.sub.1-C.sub.6)alkoxy, or phenyl groups, (iii) each occurrence of R.sup.4 is independently H, (C.sub.1-C.sub.6)alkyl, (C.sub.2-C.sub.6)alkenyl, or (C.sub.2-C.sub.6)alkynyl and is unsubstituted or substituted with one or two halo, OH, C.sub.1-C.sub.6 alkoxy, or phenyl groups; and (iv) each occurrence of R.sup.5 is independently H, (C.sub.1-C.sub.6)alkyl, (C.sub.2-C.sub.6)alkenyl, or (C.sub.2-C.sub.6)alkynyl.

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

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

4. The compound of claim 1, wherein m is 1.

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

6. The compound of claim 1, wherein n is 5.

7. The compound of claim 1, wherein z is 0.

8. The compound of claim 1, wherein z is 1.

9. The compound of claim 1, wherein Y.sup.1 is (C.sub.1-C.sub.6)alkyl and Y.sup.2 is OH.

10. The compound of claim 1, wherein Y.sup.1 is methyl and Y.sup.2 is OH.

11. A compound according to claim 1 wherein said compound has the structure: ##STR00111## or a pharmaceutically acceptable salt, hydrate, or solvate thereof.

12. A compound according to claim 1 wherein said compound has the structure: ##STR00112## or a pharmaceutically acceptable salt, hydrate, or solvate thereof.

13. A compound according to claim 1 wherein said compound has the structure: ##STR00113## or a pharmaceutically acceptable salt, hydrate, or solvate thereof.

14. A compound according to claim 1 wherein said compound has the structure: ##STR00114## or a pharmaceutically acceptable salt, hydrate, or solvate thereof.

15. A compound of structure: ##STR00115## or a pharmaceutically acceptable salt, hydrate, or solvate thereof.

16. A pharmaceutical composition comprising a compound of claim 1, 15, 11, 12, 13, or 14 and a pharmaceutically acceptable vehicle, excipient, or diluent.

17. A pharmaceutical composition comprising a compound of claim 1, 15, 11, 12, 13, or 14 and further comprising a second therapeutic agent.

18. A pharmaceutical composition comprising a compound of claim 1, 11, 12, 13, or 14 and a pharmaceutically acceptable vehicle, excipient, or diluent which is administered in combination with a statin.

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