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| Title : Optimization of Activity, Selectivity, and Liability Profiles in 5-Oxopyrrolopyridine DPP4 Inhibitors Leading to Clinical Candidate (Sa)-2-(3-(Aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b]py ridin-6(7H)-yl)-N,N-dimethylacetamide (BMS-767778) - Devasthale_2013_J.Med.Chem_56_7343 |
| Author(s) : Devasthale P , Wang Y , Wang W , Fevig J , Feng J , Wang A , Harrity T , Egan D , Morgan N , Cap M , Fura A , Klei HE , Kish K , Weigelt C , Sun L , Levesque P , Moulin F , Li YX , Zahler R , Kirby MS , Hamann LG |
| Ref : Journal of Medicinal Chemistry , 56 :7343 , 2013 |
| Abstract : Devasthale_2013_J.Med.Chem_56_7343 |
| ESTHER : Devasthale_2013_J.Med.Chem_56_7343 |
| PubMedSearch : Devasthale_2013_J.Med.Chem_56_7343 |
| PubMedID: 23964740 |
| Gene_locus related to this paper: human-DPP4 |
| Title : 7-Oxopyrrolopyridine-derived DPP4 inhibitors-mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site - Wang_2011_Bioorg.Med.Chem.Lett_21_6646 |
| Author(s) : Wang W , Devasthale P , Wang A , Harrity T , Egan D , Morgan N , Cap M , Fura A , Klei HE , Kish K , Weigelt C , Sun L , Levesque P , Li YX , Zahler R , Kirby MS , Hamann LG |
| Ref : Bioorganic & Medicinal Chemistry Lett , 21 :6646 , 2011 |
| Abstract : Wang_2011_Bioorg.Med.Chem.Lett_21_6646 |
| ESTHER : Wang_2011_Bioorg.Med.Chem.Lett_21_6646 |
| PubMedSearch : Wang_2011_Bioorg.Med.Chem.Lett_21_6646 |
| PubMedID: 21996520 |
| Gene_locus related to this paper: human-DPP4 |
| Title : Synthesis and SAR of azolopyrimidines as potent and selective dipeptidyl peptidase-4 (DPP4) inhibitors for type 2 diabetes - Brigance_2010_Bioorg.Med.Chem.Lett_20_4395 |
| Author(s) : Brigance RP , Meng W , Fura A , Harrity T , Wang A , Zahler R , Kirby MS , Hamann LG |
| Ref : Bioorganic & Medicinal Chemistry Lett , 20 :4395 , 2010 |
| Abstract : Brigance_2010_Bioorg.Med.Chem.Lett_20_4395 |
| ESTHER : Brigance_2010_Bioorg.Med.Chem.Lett_20_4395 |
| PubMedSearch : Brigance_2010_Bioorg.Med.Chem.Lett_20_4395 |
| PubMedID: 20598534 |
| Title : Discovery of 6-(Aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxa mides as Potent, Selective Dipeptidyl Peptidase-4 (DPP4) Inhibitors - Meng_2010_J.Med.Chem_53_5620 |
| Author(s) : Meng W , Brigance RP , Chao HJ , Fura A , Harrity T , Marcinkeviciene J , O'Connor SP , Tamura JK , Xie D , Zhang Y , Klei HE , Kish K , Weigelt CA , Turdi H , Wang A , Zahler R , Kirby MS , Hamann LG |
| Ref : Journal of Medicinal Chemistry , 53 :5620 , 2010 |
| Abstract : Meng_2010_J.Med.Chem_53_5620 |
| ESTHER : Meng_2010_J.Med.Chem_53_5620 |
| PubMedSearch : Meng_2010_J.Med.Chem_53_5620 |
| PubMedID: 20684603 |
| Gene_locus related to this paper: human-DPP4 |
| Title : Pharmacokinetics of the dipeptidyl peptidase 4 inhibitor saxagliptin in rats, dogs, and monkeys and clinical projections - Fura_2009_Drug.Metab.Dispos_37_1164 |
| Author(s) : Fura A , Khanna A , Vyas V , Koplowitz B , Chang SY , Caporuscio C , Boulton DW , Christopher LJ , Chadwick KD , Hamann LG , Humphreys WG , Kirby M |
| Ref : Drug Metabolism & Disposition: The Biological Fate of Chemicals , 37 :1164 , 2009 |
| Abstract : Fura_2009_Drug.Metab.Dispos_37_1164 |
| ESTHER : Fura_2009_Drug.Metab.Dispos_37_1164 |
| PubMedSearch : Fura_2009_Drug.Metab.Dispos_37_1164 |
| PubMedID: 19251818 |