- 4-Cyanothiazolidides as very potent, stable inhibitors of dipeptidyl peptidase IV
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A series of stable, very potent inhibitors of dipeptidyl peptidase IV has been developed. A number of dipeptide analogues, incorporating a 4-cyanothiazolidide, were found to have K(i) values of less than 1 nM versus human DP-IV and half-lives of between 5 and 27h in aqueous solution (pH 7.4).
- Ashworth, Doreen M.,Atrash, Butrus,Baker, Graham R.,Baxter, Andrew J.,Jenkins, Paul D.,Jones, D. Michael,Szelke, Michael
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- NOVEL DIPEPTIDYL PEPTIDASE INHIBITORS AND PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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The present invention relates to novel compounds representated by formula (I), where R, R1, R2, R3, X, Y, m, n are as defined.The present invention relates to compounds of the general formula I their derivatives, their analogs, their tautomeric forms, their stereoisomers, their diastereomers, their bioisosteres, their polymorphs, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them which are predominantly dipeptidyl peptidase IV inhibitors. The present invention also relates to the processes for the preparation of novel compounds of formula (I) and their use in treating type II diabetes and diabetic complications thereof and also for treating dislipidemia, hypercholesterolemia, obesity and hyperglycemia.
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Page/Page column 65
(2008/06/13)
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- NEW DIPEPTIDYL PEPTIDASE IN INHIBITORS; PROCESS FOR THEIR PREPARATION AND COMPOSITIONS CONTAINING THEM
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The present invention relates to new dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula (I), and their analogs, isomers, pharmaceutical compositions and therapeutic uses, methods of making the same.
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Page/Page column 41
(2010/02/12)
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- Inhibitors of dipeptidyl peptidase IV
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Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1-5 are new. The compo
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- Inhibitors of dipeptidyl peptidase IV
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Compounds according to general formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is O, S or CH2, X3 is NR5 or a carbonyl or thiocarbonyl group and R4
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- NEW COMPOUNDS
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The present invention relates to the novel compounds of the general formula (I) possessing DPP-IV inhibitory activity. These compounds contain tropane building blocks.
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