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US 7,834,012 B2Granted
Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
AssigneeAbbott Laboratories
InventorsZhonghua Pei, Thomas von Geldern, David J. Madar, Xiaofeng Li, Fatima Basha, Hong Yong, Kenton L. Longenecker, Bradley J. Backes, Andrew S. Judd, Mathew M. Mulhern, Kent D. Stewart
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Abstract
The present invention relates to compounds, which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II, as well as hyperglycemia, metabolic syndrome, hyperinsulinemia, obesity, atherosclerosis, various immunomodulatory diseases, and other diseases.
Claims10
A compound of formula (I)
- or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof, wherein
- R1 is selected from the group consisting of hydrogen, alkyl, haloalkyl, aryl, heteroaryl, heterocycle, cycloalkyl and cycloalkenyl;
- and R2 is —C(O)G;
- G is R4;
- R4 at each occurrence is independently selected from the group consisting of aryl, heteroaryl, cycloalkyl, cycloalkenyl, and heterocycle;
- wherein
- the aryl, heteroaryl, heterocycle, cycloalkyl, cycloalkenyl, and the heterocycle moiety of heterocyclealkyl, represented by R1, and R4, are each independently unsubstituted or substituted with 1, 2, 3, 4 or 5 substituents independently selected from the group consisting of R7, alkyl, alkenyl, —CN, —NO2, halo, ethylenedioxy, methylenedioxy, oxo, —OR7A, —OC(O)R7A, —OC(O)OR7A, —OS(O)2R7A, —S(alkyl), —S(O)alkyl, —S(O)2R7A, —S(O)2OR7A, —S(O)2NR7ARb, —C(O)R7A, —C(O)OR7A, —C(O)NR7ARb, —NR7ARb, —NOR7A, —N(Rb)C(O)R7A, —N(Rb)C(O)OR7A, —N(Rb)S(O)2R7A, —N(Rb)C(O)NR7ARb, —N(Rb)S(O)2NR7ARb, haloalkyl, cyanoalkyl, nitroalkyl, -alkylenyl-OR7A, -alkylenyl-OC(O)R7A, -alkylenyl-OC(O)OR7A, -alkylenyl-OS(O)2R7A, -alkylenyl-S(alkyl), -alkylenyl-S(O)alkyl, -alkylenyl-S(O)2R7A, -alkylenyl-S(O)2OR7A, -alkylenyl-S(O)2NR7ARb, -alkylenyl-C(O)R7A, -alkylenyl-C(O)OR7A, -alkylenyl-C(O)NR7ARb, -alkylenyl-NR7ARb, -alkylenyl-NOR7A, -alkylenyl-N(Rb)C(O)R7A, -alkylenyl-N(Rb)C(O)OR7A, -alkylenyl-N(Rb)S(O)2R7A, -alkylenyl-N(Rb)C(O)NR7ARb, -alkylenyl-N(Rb)S(O)2NR7ARb and -alkylenyl-R7;
- R7A at each occurrence is independently selected from the group consisting of hydrogen, alkyl, alkenyl, haloalkyl, —R7 and -alkylenyl-R7;
- and
- R7 at each occurrence is independently selected from the group consisting of aryl, heteroaryl, cycloalkyl, cycloalkenyl and heterocycle;
- each R3 is independently selected from the group consisting of hydrogen, alkyl, and haloalkyl;
- is double bond;
- m is 4;
- Ar1 is a phenyl group;
- the phenyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, and heterocycle represented by Ar1 and R7, are independently unsubstituted or substituted with 1, 2, 3, 4 and 5 substituents independently selected from the group consisting of alkyl, alkenyl, —CN, —NO2, halo, ethylenedioxy, methylenedioxy, oxo, —ORa, —OC(O)alkyl, —OC(O)Oalkyl, —OS(O)2alkyl, —S(alkyl), —S(O)alkyl, —S(O)2alkyl, —S(O)2ORa, —S(O)2NRaRb, —C(O)Ra, —C(O)ORa, —C(O)NRaRb, —NRaRb, —NORa, —N(Rb)C(O)Ra, —N(Rb)C(O)ORa, —N(Rb)S(O)2Ra, —N(Rb)C(O)NRaRb, —N(Rb)S(O)2NRaRb, haloalkyl, cyanoalkyl, nitroalkyl, hydroxyalkyl, alkoxyalkyl, haloalkoxyalkyl, -alkylenyl-OC(O)alkyl, -alkylenyl-OC(O)Oalkyl, -alkylenyl-OS(O)2alkyl, -alkylenyl-S(alkyl), -alkylenyl-S(O)alkyl, -alkylenyl-S(O)2alkyl, -alkylenyl-S(O)2ORa, -alkylenyl-S(O)2NRaRb, -alkylenyl-C(O)Ra, -alkylenyl-C(O)ORa, -alkylenyl-C(O)NRaRb, -alkylenyl-NRaRb, -alkylenyl-NORa, -alkylenyl-N(Rb)C(O)Ra, -alkylenyl-N(Rb)C(O)ORa, -alkylenyl-N(Rb)S(O)2Ra, -alkylenyl-N(Rb)C(O)NRaRb, and -alkylenyl-N(Rb)S(O)2NRaRb;
- Ra at each occurrence is independently selected from the group consisting of hydrogen, alkyl, alkenyl and haloalkyl, and
- Rb at each occurrence is independently selected from the group consisting of hydrogen and alkyl.
14 more elements
Dependencies are inferred from the claim text.