138165-79-4Relevant articles and documents
Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C
Guay, Daniel,Beaulieu, Christian,Jagadeeswar Reddy,Zamboni, Robert,Methot, Nathalie,Rubin, Joel,Ethier, Diane,David Percival
scheme or table, p. 5392 - 5396 (2010/05/02)
A series of dipeptide nitriles with a thienyl alanine in P2 were identified as potent and selective cathepsin C inhibitors. Incorporation of a substituted cyclopropyl moiety in P1 effectively protects these derivatives against hydrolase activity in whole blood.
Endothelin receptor antagonists
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, (2008/06/13)
The present invention provides novel compounds represented by the general formula I: STR1 wherein R 1 is a straight or branched lower alkyl, a cycloalkyl-lower alkyl, an aryl-lower alkyl, a cycloalkyl, an aryl an aryl-cycloalkyl, lower alkoxy, an aryloxy, or a heteroaryl;R 2 is hydrogen, a straight or branched lower alkyl, a cycloalkyl, or a cycloalkyl-lower alkyl;R 3 and R 3 '' are each the same or different and each is hydrogen atom, a straight or branched lower alkyl, a cycloalkyl, an aryl-lower alkyl, an aryl, or a heteroaryl; orR 3 and R 3 '' together form a ring structure;R 3 "" is hydrogen, lower alkyl or an aryl; orR 2 and R 3 "" together form a lower alkylene group --(CH 2) n -- wherein n is an integer of 1, 2 or 3; orR 2 and R 3 "" together form a group represented by the formula: --(CH 2) p --Ar-- or --Ar--(CH 2) p --, respectively, wherein p is zero or an integer of 1 or 2, and Ar is an arylene or heteroarylene;C( X) is C( O), C( S), C( NH), C( N-lower alkyl); C NH--OH, or CH 2 ;Y is a direct bond, --NH--, a lower alkyl-N, an oxygen atom, or methylene; orC( X) is CHOH and Y is a direct bond or methylene;R 4 is --(CH 2) s --Ar'' wherein s is zero or an integer of 1, 2 or 3; and Ar'' is an aryl, or a heteroaryl; andR 5 is carboxy, substituted or unsubstituted carboxamide, PO(OH) 2, tetrazole, CH 2 OH, CN, or hydrogen;and salts thereof.
3,3,3-TRIFLUORO-2-MERCAPTOMETHYL-N-TETRAZOLYL SUBSTITUTED PROPANAMIDES AND METHOD OF USING SAME
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, (2008/06/13)
Compounds of the formula STR1 wherein Y can be tetrazolyl are disclosed. These compounds are useful as cardiovascular agents.