Patent Application

App. No. 15/675,862

Abstract

Claims (47)

1 . A method for treating renal/kidney disease (RKD), insulin resistance, diabetes, endothelial dysfunction, fatty liver disease, or cardiovascular disease (CVD) in a patient comprising, administering to the patient a pharmaceutically effective amount of a compound having the structure:

wherein R 1 is:

—CN, or

C 1 -C 15 -acyl or C 1 -C 15 -alkyl, wherein either of these groups is heteroatom-substituted or heteroatom-unsubstituted; or

a pharmaceutically acceptable salt, hydrate or solvate thereof, wherein the patient is human.

2 . The method of claim 1 , wherein the patient has RKD.

3 . The method of claim 2 , wherein the RKD is diabetic nephropathy (DN).

4 - 16 . (canceled)

17 . The method of claim 1 , wherein the patient has insulin resistance.

18 . The method of claim 1 , wherein the patient has diabetes.

19 - 24 . (canceled)

25 . The method of claim 1 , wherein the patient has CVD.

26 . (canceled)

27 . The method of claim 1 , wherein the patient has endothelial dysfunction.

28 - 40 . (canceled)

41 . The method of claim 1 , wherein the compound is administered orally.

42 . (canceled)

43 . The method of claim 1 , wherein the compound is formulated as a solid dispersion.

44 - 50 . (canceled)

51 . The method of claim 1 , wherein the daily dose is from about 10 mg to about 200 mg of the compound.

52 . The method of claim 51 , wherein the daily dose is about 25 mg of the compound.

53 . (canceled)

54 . (canceled)

55 . The method of claim 1 , wherein the daily dose is from about 0.1 mg to about 30 mg of the compound.

56 - 58 . (canceled)

59 . The method of claim 55 , wherein the daily dose is from about 5 mg to about 30 mg of the compound.

60 - 66 . (canceled)

67 . The method of claim 1 , further comprising a second therapy, wherein the second therapy comprises administering to the patient a pharmaceutically effective amount of a second drug.

68 . (canceled)

69 . The method of claim 67 , wherein the second drug is a cholesterol lowering drug, an anti-hyperlipidemic, a calcium channel blocker, an anti-hypertensive, or an HMG-CoA reductase inhibitor.

70 . (canceled)

71 . (canceled)

72 . The method of claim 67 , wherein the second drug is a statin.

73 . The method of claim 72 , wherein the statin is atorvastatin, cerivastatin, fluvastatin, lovastatin, mevastatin, pitavastatin, pravastatin, rosuvastatin or simvastatin.

74 - 117 . (canceled)

118 . The method of claim 1 , wherein the compound is further defined as:

119 . The method of claim 118 , wherein at least a portion of the compound of claim 118 is present as a polymorphic form, wherein the polymorphic form is a crystalline form having an X-ray diffraction pattern (CuKα) comprising significant diffraction peaks at about 8.8, 12.9, 13.4, 14.2 and 17.4 °2θ.

120 . (canceled)

121 . The method of claim 118 , wherein at least a portion of the compound of claim 118 is present as a polymorphic form, wherein the polymorphic form is an amorphous form having an X-ray diffraction pattern (CuKα) with a halo peak at approximately 13.5 °2θ, substantially as shown in FIG. 12C , and a T g in the range of about 120° C. to about 135° C.

122 - 131 . (canceled)

132 . The method of claim 118 , wherein the compound is formulated as a pharmaceutical composition comprising (i) a therapeutically effective amount of the compound and (ii) an excipient is (A) a carbohydrate, carbohydrate derivative, or carbohydrate polymer, (B) a synthetic organic polymer, (C) an organic acid salt, (D) a protein, polypeptide, or peptide, or (E) a high molecular weight polysaccharide.

133 - 136 . (canceled)

137 . The method of claim 132 , wherein the excipient is a methacrylic acid-ethyl acrylate copolymer.

138 - 157 . (canceled)

158 . The method of claim 67 , wherein the second drug is an anti-hypertensive.

159 . The method of claim 158 , wherein the anti-hypertensive is an angiotensin II receptor blocker.

160 . The method of claim 158 , wherein the anti-hypertensive is an angiotensin-converting enzyme inhibitor.

Assignments (9)