Abstract: Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure 1

Abstract: The present invention provides a genus of bis-benzimidazole compounds, methods and pharmaceutical compositions that are useful as modulators of potassium ion channels. The compounds of the invention are of use in both therapeutic and diagnostic methods.

Abstract: Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure where A, B, D, Q, X1, R, R1, X2 and R2 are as defined herein. These compounds are useful as antiarrhythmic agents. In addition, a method is provided for preventing cardiac arrhythmia employing the above compounds.

Abstract: A method for screening compounds for biological activity is disclosed. The method may include selecting a test set of compounds and selecting a training set of compounds. An assay is performed on the training set of compounds and training set data are formed. This data are entered into a digital computer, and an analytical model is formed. A subset of compounds is identified using the analytical model.

Abstract: Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure ##STR1## where A, B, D, Q, X.sup.1, R, R.sup.1, X.sup.2 and R.sup.2 are as defined herein. These compounds are useful as antiarrhythmic agents. In addition, a method is provided for preventing cardiac arrhythmia employing the above compounds.

Abstract: Compounds of the invention inhibit urokinase plasminogen activator or uPAR: ##STR1## where R.sub.10 is --CH(R.sub.9)XCH(R.sub.1)(R.sub.11) or a capping group, where X is NR.sub.12, CR.sub.12 R.sub.15, O, S, SR.sub.12, or SR.sub.12 R.sub.15 ; R.sub.1, R.sub.9, R.sub.11, R.sub.12 R.sub.15 are each H, lower alkyl, lower alkenyl, lower alkynyl, aryl, aralkyl, aryl-alkenyl, aryl-alkynyl, aryl-cycloalkyl, substituted with 0-3 halo, OH, NH.sub.2, lower alkyl, halo-lower alkyl, lower alkoxy, lower alkylamino, lower alkylthio, CN or NO.sub.2 ; R.sub.16 is --CH(R.sub.5)C(.dbd.O)NH.sub.2, H, lower alkyl, cycloalkyl, or lower alkenyl; R.sub.2 is aryl or aralkyl, unsubstituted or substituted with 1-3 halo, OH, NH.sub.2, CN, NO.sub.2, lower alkyl, halo-lower alkyl, lower alkoxy, lower alkylamino, lower alkylthio, or cycloalkyl; R.sub.3 and R.sub.5 are each independently H or lower alkyl; R.sub.4 is --CH.sub.2 C(.dbd.O)NR.sub.13 R.sub.14, where R.sub.13 is H, lower alkyl, phenyl or benzyl, and R.sub.

Abstract: Effective urokinase-type plasminogen activator receptor antagonists have sequences selected from the group LNFGQYLWYT, LCFGCYLWYT, LNFGCYLWCT, LNFGQYLnAYT, LNFdSQYLWYT, LCFGCYLWY, LNFdSQYLnAYT, LNFGdCYLWCT, LCFdSCYLWYT, LCFdSCYLnAYT, LNFdSCYLWCT, or active analogs or active portions thereof.

Abstract: The invention relates to libraries of cyclic organic compounds and method of producing and assaying such libraries. According to the invention, each cyclic organic compound is constructed from a starting material in the form of a solid surface derivatized with a starting resin. Compounds are reacted with the resin to add or to form a cyclic group. The reactions are preferable carried out using a split resin procedure so that different compounds can be reacted with a plurality of subamounts so as to increase the size of the library. For example, compounds are reacted with a solid support bound starting resin to obtain a compound which includes an aldehyde functional group wherein the aldehyde compound or compounds reacted with it have substituents which are varied such that a mixture of products is obtained.

Abstract: Compounds of the invention inhibit urokinase plasminogen activator: ##STR1## where R.sub.1 is lower alkyl, lower alkenyl, lower alkynyl, aryl, aralkyl, aryl-alkenyl, aryl-alkynyl, aryl-cycloalkyl, unsubstituted or substituted with 1-3 halo, OH, NH.sub.2, lower alkyl, halo-lower alkyl, lower alkoxy, lower alkylamino, lower alkylthio, CN or NO.sub.2 ;R.sub.2 is aryl or aralkyl, unsubstituted or substituted with 1-3 halo, OH, NH.sub.2, CN, NO.sub.2, lower alkyl, halo-lower alkyl, lower alkoxy, lower alkylamino, lower alkylthio, or cycloalkyl;R.sub.3, R.sub.5 and R.sub.9 are each independently H or lower alkyl;R.sub.4 is ##STR2## where R.sub.6 and R.sub.7 are each independently H, OH, NH.sub.2, CN, NO.sub.2, lower alkyl, halo-lower alkyl, lower alkoxy, lower alkylamino, lower alkylthio, or cycloalkyl, and n and m are each independently an integer from 1 to 3 inclusive; and pharmaceutically acceptable acid addition salts thereof.

Abstract: Disclosed herein are compounds of the general formula ##STR1## which are useful as herbicides.