IPC분류정보
국가/구분 |
United States(US) Patent
등록
|
국제특허분류(IPC7판) |
|
출원번호 |
US-0352473
(2009-01-12)
|
등록번호 |
US-8129429
(2012-03-06)
|
발명자
/ 주소 |
- Sporn, Michael B.
- Liby, Karen T.
- Gribble, Gordon W.
- Honda, Tadashi
- Kral, Robert M.
- Meyer, Colin J.
|
출원인 / 주소 |
- Reata Pharmaceuticals, Inc.
|
대리인 / 주소 |
Fulbright & Jaworski L.L.P.
|
인용정보 |
피인용 횟수 :
43 인용 특허 :
23 |
초록
The present invention concerns methods for treating and preventing renal/kidney disease, insulin resistance/diabetes, fatty liver disease, and/or endothelial dysfunction/cardiovascular disease using synthetic triterpenoids, optionally in combination with a second treatment or prophylaxis.
대표청구항
▼
1. A method of improving kidney function in a subject in need thereof comprising administering to the subject a compound of the formula, in an amount sufficient to improve kidney function. 2. The method of claim 1, where the subject has chronic kidney disease (CKD) or exhibits one or more symptoms
1. A method of improving kidney function in a subject in need thereof comprising administering to the subject a compound of the formula, in an amount sufficient to improve kidney function. 2. The method of claim 1, where the subject has chronic kidney disease (CKD) or exhibits one or more symptoms of CKD. 3. The method of claim 2, where the subject has been identified as having CKD. 4. The method of claim 2, where the CKD is characterized by a serum creatinine level of 1.3-3.0 mg/DL where the subject is a human female or a serum creatinine level of 1.5-3.0 mg/DL where the subject is a human male. 5. The method of claim 2, where the CKD is stage 4. 6. The method of claim 1, where the subject has diabetic nephropathy (DN) or exhibits one or more symptoms of DN. 7. The method of claim 6, where the subject has been identified as having DN. 8. The method of claim 1, where the administering results in an improvement in estimated glomerular filtration rate (eGFR) of the subject. 9. The method of claim 8, where the administering reduces the level of serum creatinine in the subject. 10. The method of claim 9, where the level of serum creatinine in the blood of the subject has been measured. 11. The method of claim 1, where the level of blood urea nitrogen (BUN) in the subject has been measured. 12. The method of claim 1, where the level of Adiponectin in the blood of the subject has been measured. 13. The method of claim 1, where the level of Angiotensin II in the subject has been measured. 14. The method of claim 1, where the subject has insulin resistance or exhibits one or more symptoms of insulin resistance. 15. The method of claim 14, where the subject has been identified as having insulin resistance. 16. The method of claim 14, where the level of hemoglobin Alc in the subject has been measured. 17. The method of claim 14, where a blood sugar level of the subject has been measured. 18. The method of claim 14, where the administering reduces the level of hemoglobin Alc or fasting blood glucose in the subject. 19. The method of claim 17, where a fasting glucose level of the subject has been measured. 20. The method of claim 14, where the insulin sensitivity of the subject has been measured by a hyperinsulinemic euglycemic clamp test. 21. The method of claim 14, where a glucose disposal rate (GDR) in the subject has been measured. 22. The method of claim 1, where the subject has cardiovascular disease (CVD) or exhibits one or more symptoms of CVD. 23. The method of claim 22, where the subject has been identified as having CVD. 24. The method of claim 22, where the level of a marker of CVD in the subject has been measured. 25. The method of claim 22, where the number of circulating endothelial cells (CFCs) in the blood of the subject has been measured. 26. The method of claim 25, where the CECs are iNOS-positive circulating endothelial cells. 27. The method of claim 22, where the administering reduces the level of circulating endothelial cells in the subject. 28. The method of claim 27, where the administering reduces the level of hemoglobin Alc or fasting blood glucose in the subject. 29. The method of claim 1, wherein the subject is a human. 30. The method of claim 1, wherein at least a portion of the compound is present as 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. 31. The method of claim 30, wherein the X-ray diffraction pattern (CuKα) is substantially as shown in FIG. 12A or FIG. 12B. 32. The method of claim 30, wherein the pharmaceutically effective amount is a daily dose of about 10 mg to about 200 mg of the compound. 33. The method of claim 1, wherein at least a portion of the compound is present as 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 Tg from about 120 ° C. to about 135 °C. 34. The method of claim 33, wherein the Tg is from about 125 ° C. to about 130 ° C. 35. The method of claim 33, wherein the pharmaceutically effective amount is a daily dose from about 0.1 mg to about 30 mg of the compound. 36. The method of claim 1, where the compound is administered orally, intraarterially or intravenously. 37. The method of claim 1, where the compound is formulated as a hard or soft capsule or a tablet. 38. The method of claim 1, wherein the compound is formulated as a solid dispersion comprising (i) the compound and (ii) an excipient. 39. The method of claim 38, wherein the excipient is a methacrylic acid-ethyl acrylate copolymer (1:1). 40. A method of improving kidney function in a subject comprising administering to the subject a compound of the formula, in an amount sufficient to improve kidney function, wherein: (a) at least a portion of the compound is present as 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 Tg from about 120 ° C. to about 135 ° C.; and(b) where the subject has been identified as having chronic kidney disease (CKD).
※ AI-Helper는 부적절한 답변을 할 수 있습니다.