56358-46-4Relevant academic research and scientific papers
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties
Bruncko, Milan,McClellan, William J.,Wendt, Michael D.,Sauer, Daryl R.,Geyer, Andrew,Dalton, Christopher R.,Kaminski, Michele A.,Weitzberg, Moshe,Gong, Jane,Dellaria, Joseph F.,Mantei, Robert,Zhao, Xumiao,Nienaber, Vicki L.,Stewart, Kent,Klinghofer, Vered,Bouska, Jennifer,Rockway, Todd W.,Giranda, Vincent L.
, p. 93 - 98 (2007/10/03)
A series of non-amide-linked 6-substituted-2-naphthamidine urokinase plasminogen activator (uPA) inhibitors are described. These compounds possess excellent binding activities and selectivities with significantly improved pharmacokinetic profiles versus p
Naphthamidine urokinase inhibitors
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, (2008/06/13)
Compounds having the formula: are inhibitors of urokinase and are useful in the treatment of diseases in which urokinase plays a role. Also disclosed are urokinase-inhibiting compositions, methods for the preparation of urokinase-inhibitors, and a method of inhibiting urokinase in a mammal.
Naphthamidine urokinase inhibitors
-
, (2008/06/13)
Compounds having the formula are inhibitors of urokinase and are useful in the treatment of diseases in which urokinase plays a role. Also disclosed are urokinase-inhibiting compositions, methods for the preparation of urokinase-inhibitors, and a method of inhibiting urokinase in a mammal.
AROMATIC AMIDINE DERIVATIVES AND SALTS THEREOF
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, (2008/06/13)
An anticoagulant agent which comprises, as an active ingredient, an aromatic amidine derivative represented by the following general formula (1) or a salt thereof: STR1 wherein the group represented by STR2 is a group selected from indolyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, naphthyl, tetrahydronaphthyl and indanyl; X is a single bond, an oxygen atom, a sulfur atom or a carbonyl group; and Y is a saturated or unsaturated 5-or 6-membered heterocyclic moiety or cyclic hydrocarbon moiety optionally having a substituent group, an amino group optionally having a substituent group or an aminoalkyl group optionally having a substituent group.The inventive compound has a high anticoagulant capacity based on its excellent FXa inhibition activity.
Nonpeptidic Angiotensin II Antagonists: Synthesis and in Vitro Activity of a Series of Novel Naphthalene and Tetrahydronaphthalene Derivatives
Buehlmayer, Peter,Criscione, Leoluca,Fuhrer, Walter,Furet, Pascal,Gasparo, Marc de,et al.
, p. 3105 - 3114 (2007/10/02)
Starting from the structure of the novel nonpeptidic angiotensin II antagonist DuP 753, a series of more rigid analogues was prepared by replacing the biphenyl part of DuP 753 with a naphthalene ring.Five different regioisomers (compounds 6a-e) were synthesized, and receptor binding in rat smooth muscle cell preparations as well as inhibition of angiotensin II induced contraction of rabbit aortic rings was measured and the order of potency was compared with predictions made on the basis of a molecular modeling study.In good agreement with the predictions, the 2,6-substituted regioisomer 6d and its analogue 7 (isomeric at the imidazole substituent) were found to be most potent, but were still weaker than DuP 753.Tetrahydronaphthalene derivatives with and without an additional methyl group in the α-position to the acidic function and with this same 2,6-substitution pattern (compounds listed in Table III) were then prepared with the expectation of getting a further increase in potency.Whereas the carboxylic acid derivatives 13a,b showed activity in the expected potency range, surprisingly no further potency increase was observed after replacement of the carboxylic acid function by a tetrazole (compounds 18a,b).These results may indicate that the compounds do not bind to the AT1 receptor in the same way as DuP 753.
Pyridyl- and/or pyridoyl-(piperid-4-yl) ureas and analogues thereof
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, (2008/06/13)
The invention concerns the preparation of compounds of formula STR1 and acid addition and quaternary ammonium salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula STR2 in which Q is O, S, --CR7/s
Piperid-4-yl ureas and thio ureas used as antidepressant agents
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, (2008/06/13)
The invention concerns the preparation of compounds of formula STR1 and acid addition and quaternary ammoniun salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula STR2 in which Q is O, S, --CR7/s
