197959-52-7Relevant academic research and scientific papers
AMIDINOHYDRAZONES AS PROTEASE INHIBITORS
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Page/Page column 19, (2010/11/23)
Amidino and benzamidino compounds, including compounds of the formula: I wherein R1-R4, R6-R9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I.
Oxyguanidines: Application to non-peptidic phenyl-based thrombin inhibitors
Tomczuk, Bruce,Lu, Tianbao,Soll, Richard M.,Fedde, Cynthia,Wang, Aihua,Murphy, Larry,Crysler, Carl,Dasgupta, Malini,Eisennagel, Stephen,Spurlino, John,Bone, Roger
, p. 1495 - 1498 (2007/10/03)
Although thrombin has been extensively researched with many examples of potent and selective inhibitors, the key characteristics of oral bioavailability and long half-life have been elusive. We report here a novel series non-peptidic phenyl-based, highly potent, highly selective and orally bioavailable thrombin inhibitors using oxyguanidines as guanidine-mimetics.
Aminoguanidines and alkoxyguanidines as protease inhibitors
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, (2008/06/13)
Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9and R114 R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and mare set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present 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, or are intermediates useful for forming compounds having antithrombotic activity. 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.
Amidinohydrazones as guanidine bioisosteres: Application to a new class of potent, selective and orally bioavailable, non-amide-based small-molecule thrombin inhibitors
Soll, Richard M.,Lu, Tianobao,Tomczuk, Bruce,Illig, Carl R.,Fedde, Cynthia,Eisennagel, Stephen,Bone, Roger,Murphy, Larry,Spurlino, John,Salemme, F. Raymond
, p. 1 - 4 (2007/10/03)
We describe a new class of potent, non-amide-based small molecule thrombin inhibitors in which an amidinohydrazone is used as a guanidine bioisostere on a non-peptide scaffold. Compound 4 exhibits nM inhibition of thrombin, is selective for thrombin, and
