Patent Publications - 09/04/2008

US20080214567
Benzimidazole Thiophene Compounds

US20080214563
Benzimidazole Thiophene Compounds As Plk Modulators

PKA/Akt - Abbott

Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase B/Akt inhibitors with reduced hypotension.
LinksZhu GD, Gandhi VB, Gong J, Thomas S, Woods KW, Song X, Li T, Diebold RB, Luo Y, Liu X, Guan R, Klinghofer V, Johnson EF, Bouska J, Olson A, Marsh KC, Stoll VS, Mamo M, Polakowski J, Campbell TJ, Martin RL, Gintant GA, Penning TD, Li Q, Rosenberg SH, Giranda VL.

p38 - BMS

Structural basis for the high-affinity binding of pyrrolotriazine inhibitors of p38 MAP kinase.
LinksSack JS, Kish KF, Pokross M, Xie D, Duke GJ, Tredup JA, Kiefer SE, Newitt JA.

IRAK4 - UCB

IRAK-4 inhibitors. Part III: a series of imidazo[1,2-a]pyridines. Buckley GM, Fosbeary R, Fraser JL, Gowers L, Higueruelo AP, James LA, Jenkins K, Mack SR, Morgan T, Parry DM, Pitt WR, Rausch O, Richard MD, Sabin V.

TrkA - Cephalon

TrkA kinase inhibitors from a library of modified and isosteric Staurosporine aglycone. Tripathy R, Angeles TS, Yang SX, Mallamo JP.

Src - University of Rhode Island

Development of Src tyrosine kinase substrate binding site inhibitors. Ye G, Tiwari R, Parang K.

p38 - Eberhard-Karls-University Tuebingen

Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. Laufer SA, Hauser DR, Domeyer DM, Kinkel K, Liedtke AJ.

JAK2 - University of Florida

Z3, a novel Jak2 tyrosine kinase small-molecule inhibitor that suppresses Jak2-mediated pathologic cell growth. Sayyah J, Magis A, Ostrov DA, Allan RW, Braylan RC, Sayeski PP.

JNK - Pfizer

Pharmacological characterization of a small-molecule inhibitor of c-Jun kinase. Cho HK, Black SC, Looper D, Shi M, Kelly-Sullivan D, Timofeevski S, Siegel K, McDonnell SR, Yu XH, Chen P, Yie J, Ogilvie KM, Fraser JD, Briscoe CP.

PI3K - Piramed/Genentech

The Identification of 2-(1H-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a Potent, Selective, Orally Bioavailable Inhibitor of Class I PI3 Kinase for the Treatment of Cancer. Folkes AJ, Ahmadi K, Alderton WK, Alix S, Baker SJ, Box G, Chuckowree IS, Clarke PA, Depledge P, Eccles SA, Friedman LS, Hayes A, Hancox TC, Kugendradas A, Lensun L, Moore P, Olivero AG, Pang J, Patel S, Pergl-Wilson GH, Raynaud FI, Robson A, Saghir N, Salphati L, Sohal S, Ultsch MH, Valenti M, Wallweber HJ, Wan NC, Wiesmann C, Workman P, Zhyvoloup A, Zvelebil MJ, Shuttleworth SJ.