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106 results

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Page 1
Arylsulfonamide pyrimidines as VLA-4 antagonists.
Xu YZ, Konradi AW, Bard F, Dappen M, Dofiles L, Dreyer M, Gallager I, Garrido C, Krimm M, Liao Z, Messersmith E, Mutter L, Pleiss MA, Samant B, Semko CM, Smith J, Stappenbeck F, Stupi B, Vandervert C, Welch B, Wipke B, Yednock T. Xu YZ, et al. Among authors: bard f. Bioorg Med Chem Lett. 2013 May 15;23(10):3070-4. doi: 10.1016/j.bmcl.2013.03.010. Epub 2013 Mar 15. Bioorg Med Chem Lett. 2013. PMID: 23562062
Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor.
Bowers S, Truong AP, Neitz RJ, Neitzel M, Probst GD, Hom RK, Peterson B, Galemmo RA Jr, Konradi AW, Sham HL, Tóth G, Pan H, Yao N, Artis DR, Brigham EF, Quinn KP, Sauer JM, Powell K, Ruslim L, Ren Z, Bard F, Yednock TA, Griswold-Prenner I. Bowers S, et al. Among authors: bard f. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1838-43. doi: 10.1016/j.bmcl.2011.01.046. Epub 2011 Jan 20. Bioorg Med Chem Lett. 2011. PMID: 21316234
PEG conjugates of potent α4 integrin inhibitors, maintaining sustained levels and bioactivity in vivo, following subcutaneous administration.
Smith JL, Rossiter KI, Semko CM, Xu YZ, Quincy DA, Jagodzinski J, Dappen MS, Konradi AW, Vandevert C, Garrido C, Mao W, San Pablo FB, Wipke B, Dofiles L, Wadsworth A, Peterson E, Lorenzana C, Simmonds S, Messersmith EK, Bard F, Pleiss MA, Yednock TA. Smith JL, et al. Among authors: bard f. Bioorg Med Chem Lett. 2013 Jul 15;23(14):4117-9. doi: 10.1016/j.bmcl.2013.05.048. Epub 2013 May 24. Bioorg Med Chem Lett. 2013. PMID: 23743283
Orally available and efficacious α4β1/α4β7 integrin inhibitors.
Xu YZ, Smith JL, Semko CM, Rossiter KI, Fukuda JY, Dappen MS, Quincy DA, Konradi AW, Mao W, Welch B, Dreyer ML, Samant B, Zhang H, Lugar J, Liao Z, Henschel C, Petersen E, Vandevert C, Shoemaker M, Wehner N, Mutter L, Shopp G, Krimm M, Chen L, Wipke B, Dofiles L, Gallager I, Sauer JM, Messersmith EK, Pleiss MA, Bard F, Yednock TA. Xu YZ, et al. Among authors: bard f. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4370-3. doi: 10.1016/j.bmcl.2013.05.076. Epub 2013 May 31. Bioorg Med Chem Lett. 2013. PMID: 23777782
Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model.
Truong AP, Tóth G, Probst GD, Sealy JM, Bowers S, Wone DW, Dressen D, Hom RK, Konradi AW, Sham HL, Wu J, Peterson BT, Ruslim L, Bova MP, Kholodenko D, Motter RN, Bard F, Santiago P, Ni H, Chian D, Soriano F, Cole T, Brigham EF, Wong K, Zmolek W, Goldbach E, Samant B, Chen L, Zhang H, Nakamura DF, Quinn KP, Yednock TA, Sauer JM. Truong AP, et al. Among authors: bard f. Bioorg Med Chem Lett. 2010 Nov 1;20(21):6231-6. doi: 10.1016/j.bmcl.2010.08.102. Epub 2010 Aug 24. Bioorg Med Chem Lett. 2010. PMID: 20833041
Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK.
Hom RK, Bowers S, Sealy JM, Truong AP, Probst GD, Neitzel ML, Neitz RJ, Fang L, Brogley L, Wu J, Konradi AW, Sham HL, Tóth G, Pan H, Yao N, Artis DR, Quinn K, Sauer JM, Powell K, Ren Z, Bard F, Yednock TA, Griswold-Prenner I. Hom RK, et al. Among authors: bard f. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7303-7. doi: 10.1016/j.bmcl.2010.10.066. Epub 2010 Oct 21. Bioorg Med Chem Lett. 2010. PMID: 21071223
Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration.
Probst GD, Bowers S, Sealy JM, Truong AP, Hom RK, Galemmo RA Jr, Konradi AW, Sham HL, Quincy DA, Pan H, Yao N, Lin M, Tóth G, Artis DR, Zmolek W, Wong K, Qin A, Lorentzen C, Nakamura DF, Quinn KP, Sauer JM, Powell K, Ruslim L, Wright S, Chereau D, Ren Z, Anderson JP, Bard F, Yednock TA, Griswold-Prenner I. Probst GD, et al. Among authors: bard f. Bioorg Med Chem Lett. 2011 Jan 1;21(1):315-9. doi: 10.1016/j.bmcl.2010.11.010. Epub 2010 Nov 5. Bioorg Med Chem Lett. 2011. PMID: 21112785
Highly selective c-Jun N-terminal kinase (JNK) 3 inhibitors with in vitro CNS-like pharmacokinetic properties II. Central core replacement.
Neitz RJ, Konradi AW, Sham HL, Zmolek W, Wong K, Qin A, Lorentzen C, Nakamura D, Quinn KP, Sauer JM, Powell K, Ruslim L, Chereau D, Ren Z, Anderson J, Bard F, Yednock TA, Griswold-Prenner I. Neitz RJ, et al. Among authors: bard f. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3726-9. doi: 10.1016/j.bmcl.2011.04.074. Epub 2011 Apr 27. Bioorg Med Chem Lett. 2011. PMID: 21570836
Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration.
Bowers S, Truong AP, Jeffrey Neitz R, Hom RK, Sealy JM, Probst GD, Quincy D, Peterson B, Chan W, Galemmo RA Jr, Konradi AW, Sham HL, Tóth G, Pan H, Lin M, Yao N, Artis DR, Zhang H, Chen L, Dryer M, Samant B, Zmolek W, Wong K, Lorentzen C, Goldbach E, Tonn G, Quinn KP, Sauer JM, Wright S, Powell K, Ruslim L, Ren Z, Bard F, Yednock TA, Griswold-Prenner I. Bowers S, et al. Among authors: bard f. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5521-7. doi: 10.1016/j.bmcl.2011.06.100. Epub 2011 Jul 7. Bioorg Med Chem Lett. 2011. PMID: 21813278
Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007): metabolically stable γ-secretase Inhibitors that selectively inhibit the production of amyloid-β over Notch.
Probst G, Aubele DL, Bowers S, Dressen D, Garofalo AW, Hom RK, Konradi AW, Marugg JL, Mattson MN, Neitzel ML, Semko CM, Sham HL, Smith J, Sun M, Truong AP, Ye XM, Xu YZ, Dappen MS, Jagodzinski JJ, Keim PS, Peterson B, Latimer LH, Quincy D, Wu J, Goldbach E, Ness DK, Quinn KP, Sauer JM, Wong K, Zhang H, Zmolek W, Brigham EF, Kholodenko D, Hu K, Kwong GT, Lee M, Liao A, Motter RN, Sacayon P, Santiago P, Willits C, Bard F, Bova MP, Hemphill SS, Nguyen L, Ruslim L, Tanaka K, Tanaka P, Wallace W, Yednock TA, Basi GS. Probst G, et al. Among authors: bard f. J Med Chem. 2013 Jul 11;56(13):5261-74. doi: 10.1021/jm301741t. Epub 2013 Jun 20. J Med Chem. 2013. PMID: 23713656
106 results