Composition containing a DPP-IV inhibitor for preventing or treating renal diseases

Inventors

CHA, Dae RyongKang, Young SunCHA, Jin JooLee, Ji EunKim, Hyun WookLEE, Mi HwaKim, Jung EunKim, Mi-KyungSon, Moon-HoKim, Soon Hoe

Assignees

Korea University Research and Business FoundationDong-A ST Co Ltd

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Publication Number

US-10159667-B2

Patent

Publication Date

2018-12-25

Expiration Date


Abstract

The present invention relates to a composition for preventing or treating renal diseases. The composition of the present invention improves lipid metabolism, prevents histological damage including renal fibrosis, alleviates microalbuminuria, and maintains nephrons of renal glomeruli. Therefore, the composition is useful for treating renal diseases.

Core Innovation

The invention relates to a pharmaceutical composition for preventing or treating renal diseases, wherein a subject is administered a therapeutically effective amount of a compound of Formula 1, or a pharmaceutically acceptable salt thereof. The compound of Formula 1 is characterized by X is OR and R1 is tert-butyl, and may be provided as pharmaceutically acceptable salts, hydrates, or solvates.

The problem addressed is renal disease in a subject, including renal disease in a subject who does not have diabetes, such as glomerulonephritis. The content describes renal pathology markers and renal function indicators including microalbuminuria, renal fibrosis markers (TGF-β1, type IV collagen, and PAI-1), mesangial expansion, urinary nephrin excretion, and nephrin expression.

The invention positions DPP-IV inhibition by DA1229 as a means to improve lipid metabolism and provide kidney protection. The content further states reduction of microalbuminuria, renal fibrosis markers, and mesangial expansion, together with preservation of nephrin expression and reduction of urinary nephrin excretion in diabetic and non-diabetic nephropathy contexts, including toxic nephropathy and glomerulonephritis.

Claims Coverage

The provided content includes one independent claim. It specifies treatment of a non-diabetic subject with a renal disease using a Formula 1 compound defined by X is OR and R1 is tert-butyl, including a specific (R) optical isomer and pharmaceutically acceptable salt.

Treating non-diabetic glomerulonephritis with Formula 1 compound

A method of treating a renal disease in a subject who does not have diabetes by administering a therapeutically effective amount of a pharmaceutical composition comprising a compound of Formula 1, or a pharmaceutically acceptable salt thereof, wherein X is OR and R1 is tert-butyl, and the renal disease is glomerulonephritis.

The claim coverage focuses on administering a Formula 1 composition to a non-diabetic subject with glomerulonephritis, with the core structure defined by X is OR and R1 is tert-butyl.

Stated Advantages

Reduces microalbuminuria as a renal pathology marker.

Reduces renal fibrosis markers including TGF-β1, type IV collagen, and PAI-1.

Reduces mesangial expansion.

Preserves nephrin expression.

Reduces urinary nephrin excretion.

Provides kidney protection in diabetic and non-diabetic nephropathy contexts.

Improves lipid metabolism.

Documented Applications

Treating a renal disease in a subject who does not have diabetes, where the renal disease is glomerulonephritis.

Treating renal diseases in both diabetic and non-diabetic nephropathy contexts, including toxic nephropathy described with an adriamycin-induced model.

Managing renal pathology features including microalbuminuria, renal fibrosis markers, mesangial expansion, and nephrin-related measures.

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