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Page 1
Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases.
Gavai AV, Fink BE, Fairfax DJ, Martin GS, Rossiter LM, Holst CL, Kim SH, Leavitt KJ, Mastalerz H, Han WC, Norris D, Goyal B, Swaminathan S, Patel B, Mathur A, Vyas DM, Tokarski JS, Yu C, Oppenheimer S, Zhang H, Marathe P, Fargnoli J, Lee FY, Wong TW, Vite GD. Gavai AV, et al. Among authors: zhang h. J Med Chem. 2009 Nov 12;52(21):6527-30. doi: 10.1021/jm9010065. J Med Chem. 2009. PMID: 19821562
Design, synthesis, and anti-inflammatory properties of orally active 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38alpha mitogen-activated protein kinase inhibitors.
Hynes J Jr, Dyckman AJ, Lin S, Wrobleski ST, Wu H, Gillooly KM, Kanner SB, Lonial H, Loo D, McIntyre KW, Pitt S, Shen DR, Shuster DJ, Yang X, Zhang R, Behnia K, Zhang H, Marathe PH, Doweyko AM, Tokarski JS, Sack JS, Pokross M, Kiefer SE, Newitt JA, Barrish JC, Dodd J, Schieven GL, Leftheris K. Hynes J Jr, et al. Among authors: zhang r, zhang h. J Med Chem. 2008 Jan 10;51(1):4-16. doi: 10.1021/jm7009414. Epub 2007 Dec 12. J Med Chem. 2008. PMID: 18072718
New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.
Mastalerz H, Chang M, Chen P, Dextraze P, Fink BE, Gavai A, Goyal B, Han WC, Johnson W, Langley D, Lee FY, Marathe P, Mathur A, Oppenheimer S, Ruediger E, Tarrant J, Tokarski JS, Vite GD, Vyas DM, Wong H, Wong TW, Zhang H, Zhang G. Mastalerz H, et al. Among authors: zhang g, zhang h. Bioorg Med Chem Lett. 2007 Apr 1;17(7):2036-42. doi: 10.1016/j.bmcl.2007.01.002. Epub 2007 Jan 12. Bioorg Med Chem Lett. 2007. PMID: 17270437
Novel C-5 aminomethyl pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.
Mastalerz H, Chang M, Gavai A, Johnson W, Langley D, Lee FY, Marathe P, Mathur A, Oppenheimer S, Tarrant J, Tokarski JS, Vite GD, Vyas DM, Wong H, Wong TW, Zhang H, Zhang G. Mastalerz H, et al. Among authors: zhang g, zhang h. Bioorg Med Chem Lett. 2007 May 15;17(10):2828-33. doi: 10.1016/j.bmcl.2007.02.050. Epub 2007 Feb 27. Bioorg Med Chem Lett. 2007. PMID: 17368025
5-((4-Aminopiperidin-1-yl)methyl)pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.
Mastalerz H, Chang M, Chen P, Fink BE, Gavai A, Han WC, Johnson W, Langley D, Lee FY, Leavitt K, Marathe P, Norris D, Oppenheimer S, Sleczka B, Tarrant J, Tokarski JS, Vite GD, Vyas DM, Wong H, Wong TW, Zhang H, Zhang G. Mastalerz H, et al. Among authors: zhang g, zhang h. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4947-54. doi: 10.1016/j.bmcl.2007.06.019. Epub 2007 Jun 10. Bioorg Med Chem Lett. 2007. PMID: 17606372
Discovery of a tetrazole-based growth hormone secretagogue: 4-(hydroxybutyl)carbamic acid 2-{5-[1-(2-amino-2-methylpropionylamino)-2- benzyloxyethyl]tetrazol-1-yl}ethyl ester (BMS-317180).
Li J, Chen SY, Li JJ, Wang H, Hernandez AS, Tao S, Musial CM, Qu F, Swartz S, Chao ST, Flynn N, Murphy BJ, Slusarchyk DA, Seethala R, Yan M, Sleph P, Grover G, Smith MA, Beehler B, Giupponi L, Dickinson KE, Zhang H, Humphreys WG, Patel BP, Schwinden M, Stouch T, Cheng PT, Biller SA, Ewing WR, Gordon D, Robl JA, Tino JA. Li J, et al. Among authors: zhang h. J Med Chem. 2007 Nov 29;50(24):5890-3. doi: 10.1021/jm7010595. Epub 2007 Oct 31. J Med Chem. 2007. PMID: 17973363
The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor.
Hynes J Jr, Wu H, Pitt S, Shen DR, Zhang R, Schieven GL, Gillooly KM, Shuster DJ, Taylor TL, Yang X, McIntyre KW, McKinnon M, Zhang H, Marathe PH, Doweyko AM, Kish K, Kiefer SE, Sack JS, Newitt JA, Barrish JC, Dodd J, Leftheris K. Hynes J Jr, et al. Among authors: zhang r, zhang h. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1762-7. doi: 10.1016/j.bmcl.2008.02.031. Epub 2008 Feb 16. Bioorg Med Chem Lett. 2008. PMID: 18313298
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