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Details for Patent: 8,188,275

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Details for Patent: 8,188,275

Title:Dipeptidyl peptidase inhibitors
Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: ##STR00001## wherein M is N or CR.sub.4; Q.sup.1 and Q.sup.2 are each independently selected from the group consisting of CO, SO, SO.sub.2, and C.dbd.NR.sub.9; and each L, X, R.sub.1, R.sub.2, and R.sub.3 are as defined herein.
Inventor(s): Feng; Jun (Carlsbad, CA), Gwaltney; Stephen L. (San Diego, CA), Stafford; Jeffrey A. (San Diego, CA), Zhang; Zhiyuan (San Diego, CA), Elder; Bruce J. (Wynantskill, NY), Isbester; Paul K. (Castleton, NY), Palmer; Grant J. (Clifton Park, NY), Salsbury; Jonathon S. (Albany, NY), Ulysse; Luckner G. (Albany, NY)
Assignee: Takeda Pharmaceutical Company Limited (Osaka, JP)
Filing Date:Oct 30, 2007
Application Number:11/928,944
Claims:1. A compound of the formula: 2-(6-Chloro-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl)-benzonitrile.

2. A compound of the formula: 2-(6-Chloro-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl)-benzo- nitrile.

3. A compound of the formula: 2-(6-Chloro-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl)-4-flu- oro-benzonitrile.

4. A compound selected from the group consisting of: 2-((6-chloro-3-ethyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)benzo- nitrile; 1-(2-bromobenzyl)-6-chloropyrimidine-2,4(1H,3H)-dione; 6-chloro-1-(2-iodobenzyl)pyrimidine-2,4(1H,3H)-dione; 1-(2-bromo-5-fluorobenzyl)-6-chloropyrimidine-2,4(1H,3H)-dione; 1-(2-bromo-5-fluorobenzyl)-6-chloro-3-methylpyrimidine-2,4(1H,3H)-dione; 6-chloro-1-(2-chloro-5-fluorobenzyl)pyrimidine-2,4(1H,3H)-dione; 6-chloro-1-(2-chloro-5-fluorobenzyl)-3-methylpyrimidine-2,4(1H,3H)-dione; 6-chloro-1-(2-chloro-4-fluorobenzyl)pyrimidine-2,4(1H,3H)-dione; 6-chloro-1-(2-chloro-4-fluorobenzyl)-3-methylpyrimidine-2,4(1H,3H)-dione; 1-(2-bromobenzyl)-6-chloro-3-methylpyrimidine-2,4(1H,3H)-dione; 2-((6-chloro-3-(3-cyanobenzyl)-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)me- thyl)benzonitrile; 2,2'-(6-chloro-2,4-dioxopyrimidine-1,3(2H,4H)-diyl)bis(methylene)dibenzon- itrile; 2-((6-chloro-3-(4-cyanobenzyl)-2,4-dioxo-3,4-dihydropyrimidin-1(2H- )-yl)methyl)benzonitrile; 2-((3-((1H-benzo[d]imidazol-2-yOmethyl)-6-chloro-2,4-dioxo-3,4-dihydropyr- imidin-1(2H)-yl)methyl)benzonitrile; 2-((3-(4-(1H-pyrazol-1-yl)benzyl)-6-chloro-2,4-dioxo-3,4-dihydropyrimidin- -1(2H)-yl)methyl)benzonitrile; 2-((3-(3-(1H-pyrrol-1-yl)benzyl)-6-chloro-2,4-dioxo-3,4-dihydropyrimidin-- 1(2H)-yl)methyl)benzonitrile; 2-((4-chloro-3-(2-cyanobenzyl)-2,6-dioxo-2,3-dihydropyrimidin-1(6H)-yl)me- thyl)thiophene-3-carbonitrile; methyl 3-((4-chloro-3-(2-cyanobenzyl)-2,6-dioxo-2,3-dihydropyrimidin-1(6H)-yl)me- thyl)benzoate; 1,3-bis(2-bromo-5-fluorobenzyl)-6-chloropyrimidine-2,4(1H,3H)-dione; 6-chloro-1-(2,5-dichlorobenzyl)pyrimidine-2,4(1H,3H)-dione; 6-chloro-1-(2,5-dichlorobenzyl)-3-methylpyrimidine-2,4(1H,3H)-dione; 6-chloro-1-(2-chloro-3,6-difluorobenzyl)pyrimidine-2,4(1H,3H)-dione; 6-chloro-1-(2-chloro-3,6-difluorobenzyl)-3-methylpyrimidine-2,4(1H,3H)-di- one; and 2-(6-Chloro-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy- l)-4-fluoro-benzonitrile.
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