- Practical synthesis of functionalized 1,5-disubstituted 1,2,4-triazole derivatives
-
A general approach for the synthesis of 1,5-disubstituted-1,2,4-triazole compounds is described. A series of new oxamide-derived amidine reagents can be accessed in excellent yield with minimal purification necessary. Typically, these amidine reagents are stable crystalline solids and in certain cases were found to exist in a cyclic form as determined by NMR spectroscopy. Under optimized conditions, the direct reaction of these prepared reagents with various hydrazine hydrochloride salts efficiently generates the target triazoles. Both aromatic and aliphatic hydrazines react readily with the amidine reagents under very mild reaction conditions, delivering desired 1,5-disubstituted-1,2,4-triazole derivatives in good yields.
- Xu, Yingju,McLaughlin, Mark,Bolton, Emily N.,Reamer, Robert A.
-
supporting information; experimental part
p. 8666 - 8669
(2011/02/28)
-
- Hydantoins and related heterocycles as inhibitors of matrix metalloproteinases and/or TNF-alpha converting enzyme (TACE)
-
The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-α converting enzyme (TACE), aggrecanase, or a combination thereof.
- -
-
-
- Modulators of Protein Tyrosine Phosphatases (PTPases)
-
The present invention provides novel thienopyridines, novel compositions, methods of their use, and methods of their manufacture, where such compounds of Formula 1 are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) includi
- -
-
-
- Modulators of protein tyrosine phosphatases (PTPases)
-
The present invention provides novel thienopyridines, novel compositions, methods of their use, and methods of their manufacture, where such compounds of Formula 1 are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) including PTP1B, T cell PTP (TC-PTP), wherein X, R1, R2, R3, and R4 are defined more fully in the description. The compounds are useful in the treatment of type 1 diabetes, type 2 diabetes, impaired glucose tolerance, insulin resistance, obesity, and other diseases.
- -
-
-