- THERAPEUTICALLY ACTIVE COMPOSITIONS AND THEIR METHODS OF USE
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Provided are compounds with the following structure, formula (I) pharmaceutically acceptable salts thereof, use of those compounds for treating cancer and pharmaceutical compositions comprising those compounds.
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- Novel Hepatitis C virus replicon inhibitors: Synthesis and structure-activity relationships of fused pyrimidine derivatives
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The synthesis of several pyrido[2,3-d]pyrimidine and pyrimido[4,5-d] pyrimidine analogs is described with one such analog possessing subnanomolar potency in both genotype 1a and 1b cell culture HCV replicon assays.
- Chris Krueger,Madigan, Darold L.,Beno, David W.,Betebenner, David A.,Carrick, Robert,Green, Brian E.,He, Wenping,Liu, Dachun,Maring, Clarence J.,McDaniel, Keith F.,Mo, Hongmei,Molla, Akhteruzzaman,Motter, Christopher E.,Pilot-Matias, Tami J.,Tufano, Michael D.,Kempf, Dale J.
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scheme or table
p. 2212 - 2215
(2012/04/18)
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- ANTI-VIRAL COMPOUNDS
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Compounds effective in inhibiting replication of Hepatitis C virus ( HCV ) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, coformulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.
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- ANTI-VIRAL COMPOUNDS
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Compounds effective in inhibiting replication of Hepatitis C virus ("HCV") or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-formulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.
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Page/Page column 75-76
(2010/11/27)
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- Synthesis and solid-state structures of alkyl-substituted 3-cyano-2-pyridones
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A series of 3-cyano-pyridones carrying a variety of alkyl substituents at C-5 and C-6 has been synthesized and their solid-state structures have been studied. Hydrogen bonding interactions between individual pyridone molecules lead either to the formation of symmetric dimers of the R2 2(8) type or to helical chains of the C(4) type. Based on known and calculated structures for the 2-pyridone parent system, the solid-state structures can be divided in two groups representing cases with little external influence on the hydrogen bonding array (group A) and those with a larger external influence (group B).
- Fischer, Christian B.,Polborn, Kurt,Steininger, Harald,Zipse, Hendrik
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p. 1121 - 1131
(2007/10/03)
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- Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors
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Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: wherein X is O or NR9and Het, R1, R7, R8, R12-R15, Ra, Rb, Rc, Z, and n are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.
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Page column 86
(2010/02/05)
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- Regioselective synthesis of 2(1H)-pyridinones from β-aminoenones and malononitrile. Reaction mechanism
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The identification of some intermediates of the reactions between β- aminoenones and malononitrile to give 2(1H)-pyridinones has allowed us to obtain valuable information concerning its mechanism. These reactions begin with a conjugated addition of the nitrile to the enone followed by elimination. The compounds thus obtained cyclize to nonisolable 2H-pyran-2- imine. This afforded 2(1H)-pyridinones by ring opening to unsaturated aminoamides followed by cyclization (Dimroth-type rearrangement).
- Alberola, Angel,Calvo, Luis A.,Ortega, Alfonso Gonzalez,Ruiz, M. Carmen Sanudo,Yustos, Pedro,Granda, Santiago Garcia,Garcia-Rodriguez, Esther
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p. 9493 - 9498
(2007/10/03)
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- Synthesis and cardiotonic activity of esters of 2-substituted 5-cyano-1,6-dihydro-6-oxo-3-pyridinecarboxylic acids. Crystal structure of 2-methyl, 2-t-butyl and 2-phenyl esters
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The synthesis of ethyl and methyl esters of 2-substituted 5-cyano-1,6-dihydro-6-oxo-3-pyridinecarboxylic acids by reaction of ethyl or methyl 2-dimethylaminomethylene-3-oxoalkanoates with sodium cyanoacetamide is described. These esters gave by alkaline hydrolysis the corresponding carboxylic acids, which were decarboxylated to 6-substituted 1,2-dihydro-2-oxo-3-pyridinecarbonitriles. As milrinone analogues, nearly all the above compounds were tested on contractile activity and frequency rate of spontaneously beating atria and electrically driven left atria from guinea pigs. Among the esters, ethyl 5-cyano-1,6-dihydro-2-methyl-6-oxo-3-pyridinecarboxylate induced positive inotropic and chronotropic effects superior to those caused by milrinone. By increasing or branching the 2-substituent, the activity decreased until faded or even reversed. Carboxylic acids and nitriles were less active than milrinone. Some aspects of the structure-activity relationship of these compounds are discussed on the basis of X-ray structural analyses of 2-methyl, 2-t-butyl and 2-phenyl esters.
- Mosti,Menozzi,Schenone,Dorigo,Gaion,Benetollo,Bombieri
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p. 517 - 529
(2007/10/02)
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