312904-99-7Relevant articles and documents
Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase
Gomez, Robert,Jolly, Samson,Williams, Theresa,Tucker, Thomas,Tynebor, Robert,Vacca, Joe,McGaughey, Georgia,Lai, Ming-Tain,Felock, Peter,Munshi, Vandna,Destefano, Daniel,Touch, Sinoeun,Miller, Mike,Yan, Youwei,Sanchez, Rosa,Liang, Yuexia,Paton, Brenda,Wan, Bang-Lin,Anthony, Neville
, p. 7344 - 7350 (2011)
Next generation NNRTIs are sought which possess both broad spectrum antiviral activity against key mutant strains and a high genetic barrier to the selection of new mutant viral strains. Pyridones were evaluated as an acyclic conformational constraint to
THERAPEUTIC INHIBITORY COMPOUNDS
-
Page/Page column 177, (2015/07/16)
The invention provides compounds of Formula I and Formula II: A-B-C-D-E-F-G-J (I) C-D-E-F-G-J (II) wherein A, B, C, D, E, F, G, and J have any of the values defined in the specification, and salts thereof. The compounds are useful for inhibiting plasma kallikrein, and for treating a disease or condition in an animal where inhibition of plasma kallikrein is indicated.
NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
-
Page/Page column 98-99, (2009/06/27)
Heteroaromatic compounds of Formula (I), are HIV reverse transcriptase inhibitors, wherein ring A is: (ii-a), (ii-b), (ii-c), (ii-d), or (ii-e); and wherein n, L, M, U, X, Y, Z, RE, RF, R1, R2A, R2B,
Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines
Burgey, Christopher S.,Robinson, Kyle A.,Lyle, Terry A.,Sanderson, Philip E. J.,Lewis, S. Dale,Lucas, Bobby J.,Krueger, Julie A.,Singh, Rominder,Miller-Stein, Cynthia,White, Rebecca B.,Wong, Bradley,Lyle, Elizabeth A.,Williams, Peter D.,Coburn, Craig A.,Dorsey, Bruce D.,Barrow, James C.,Stranieri, Maria T.,Holahan, Marie A.,Sitko, Gary R.,Cook, Jacquelynn J.,McMasters, Daniel R.,McDonough, Colleen M.,Sanders, William M.,Wallace, Audrey A.,Clayton, Franklin C.,Bohn, Dennis,Leonard, Yvonne M.,Detwiler Jr., Theodore J.,Lynch Jr., Joseph J.,Yan, Youwei,Chen, Zhongguo,Kuo, Lawrence,Gardell, Stephen J.,Shafer, Jules A.,Vacca, Joseph P.
, p. 461 - 473 (2007/10/03)
Recent efforts in the field of thrombin inhibitor research have focused on the identification of compounds with good oral bioavailability and pharmacokinetics. In this manuscript we describe a metabolism-based approach to the optimization of the 3-(2-phen
THROMBIN INHIBITORS
-
Page column 16, (2010/01/30)
Compounds of the invention, useful as thrombin inhibitors and having therapeutic value in for example, preventing coronary artery disease, have the following structure: or a pharmaceutically acceptable salt thereof, whereinA is whereinY 1 and Y 2 are independentlyhydrogen,C 1-4 alkyl,C 1-4 alkoxy,F uH v C(CH 2) 0-1 O--, wherein u and v are either 1 or 2, provided that when u is 1, v is 2, and when u is 2, v is 1,C 3-7 cycloalkyl,thio C 1-4 alkyl,C 1-4 sulfinylalkyl,C 1-4 sulfonylalkyl, halogencyano, ortrifluoromethyl, andwherein b is 0 or 1.
Pyrazinone thrombin inhibitors
-
, (2008/06/13)
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: A is ?wherein Y1and Y2are independently hydrogen, C1-4alkyl, C1-4alkoxy, FuHvC(CH2)0-1O—, wherein u and v are either 1 or 2, provided that when u is 1, v is 2, and when u is 2, v is 1, C3-7cycloalkyl, thio C1-4alkyl, C1-4sulfinylalkyl, C1-4sulfonylalkyl, halogen cyano, or trifluoromethyl, and wherein b is 0 or 1.