463349-87-3Relevant academic research and scientific papers
Dipeptidyl peptidase-IV inhibitors
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Page/Page column 25, (2010/02/14)
The invention provides compounds of Formula (I) or prodrugs thereof, or pharmaceutically acceptable salts of said compounds or prodrugs, or solvates of said compounds, prodrugs or salts, wherein A, N, X and R1 are as defined herein; pharmaceutical compositions thereof; and methods of using the pharmaceutical compositions for the treatment of diseases, including Type 2 diabetes, Type 1 diabetes, impaired glucose tolerance, hyperglycemia, metabolic syndrome (syndrome X and/or insulin resistance syndrome), glucosuria, metabolic acidosis, arthritis, cataracts, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, obesity, conditions exacerbated by obesity, hypertension, hyperlipidemia, atherosclerosis, osteoporosis, osteopenia, frailty, bone loss, bone fracture, acute coronary syndrome, short stature due to growth hormone deficiency, infertility due to polycystic ovary syndrome, anxiety, depression, insomnia, chronic fatigue, epilepsy, eating disorders, chronic pain, alcohol addiction, diseases associated with intestinal motility, ulcers, irritable bowel syndrome, inflammatory bowel syndrome; short bowel syndrome; and the prevention of disease progression in Type 2 diabetes.
4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors
Parmee, Emma R.,He, Jiafang,Mastracchio, Anthony,Edmondson, Scott D.,Colwell, Larry,Eiermann, George,Feeney, William P.,Habulihaz, Bahanu,He, Huaibing,Kilburn, Ruth,Leiting, Barbara,Lyons, Kathryn,Marsilio, Frank,Patel, Reshma A.,Petrov, Aleksandr,Di Salvo, Jerry,Wu, Joseph K.,Thornberry, Nancy A.,Weber, Ann E.
, p. 43 - 46 (2007/10/03)
Substituted 4-amino cyclohexylglycine analogues were evaluated for DP-IV inhibitory properties. Bis-sulfonamide 15e was an extremely potent 2.6 nM inhibitor of the enzyme with excellent selectivity over all counterscreens. 2,4-Difluorobenzenesulfonamide 1
Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors
Caldwell, Charles G.,Chen, Ping,He, Jiafang,Parmee, Emma R.,Leiting, Barbara,Marsilio, Frank,Patel, Reshma A.,Wu, Joseph K.,Eiermann, George J.,Petrov, Aleksandr,He, Huaibing,Lyons, Kathryn A.,Thornberry, Nancy A.,Weber, Ann E.
, p. 1265 - 1268 (2007/10/03)
Amides derived from fluorinated pyrrolidines and 4-substituted cyclohexylglycine analogues have been prepared and evaluated as inhibitors of dipeptidyl dipeptidase IV (DP-IV). Analogues which incorporated (S)-3-fluoropyrrolidine showed good selectivity for DP-IV over quiescent cell proline dipeptidase (QPP). Compound 48 had good pharmacokinetic properties and was orally active in an oral glucose tolerance test in lean mice.
