摘要:
Vasodilating activity is exhibited by compounds having the formula ##STR1## wherein X can be --S--or --CH.sub.2 --; andR.sub.2 is ##STR2##depending upon the definition of X.
摘要:
Vasodilating activity is exhibited by compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein X is --CH.sub.2 -- or --S--;R.sub.1 is ##STR2## or --O--Y.sub.3 ; R.sub.2 is heterocyclo or heteroaryl;R.sub.3 and R.sub.4 are each independently hydrogen, halogen, alkyl, alkoxy, aryloxy, arylalkoxy, arylalkyl, cyano, hydroxy, alkanoyloxy, ##STR3## fluoro-substituted alkoxy, fluoro-substituted alkyl, (cycloalkyl)alkoxy, --NO.sub.2, --NY.sub.10 Y.sub.11, --S(O).sub.k alkyl, --S(O).sub.k aryl ##STR4## n is 0, 1, 2 or 3; m is 0, 1, 2 or 3;k is 0, 1 or 2;Y.sub.1 and Y.sub.2 are each independently hydrogen or alkyl; or Y.sub.1 is hydrogen and Y.sub.2 is alkenyl, alkynyl, aryl, heteroaryl, or cycloalkyl; or Y.sub.1 and Y.sub.2, together with the carbon atom to which they are attached, are cycloalkyl;Y.sub.3 is hydrogen, alkyl, alkanoyl, alkenyl, arylcarbonyl, heteroarylcarbonyl, or ##STR5## Y.sub.8 and Y.sub.9 are each independently hydrogen, alkyl, aryl, or heteroaryl; or Y.sub.8 and Y.sub.9, together with the nitrogen atom to which they are attached, are pyrrolidinyl, piperidinyl or morpholinyl;Y.sub.10 and Y.sub.11 are each independently hydrogen, alkyl, alkanoyl, arylcarbonyl, heteroarylcarbonyl, or ##STR6## Y.sub.12 is hydroxy, alkoxy, aryloxy, amino, alkylamino, or dialkylamino; andY.sub.13 is alkyl, alkoxy or aryloxy.
摘要:
Thrombin inhibitors are provided which have the formula ##STR1## wherein Z is a thrombin inhibitor substructure containing distal and proximal binding site residues; andR.sup.1 is cyano, hydroxyl, alkoxy, amino, aminoalkyl or nitro.
摘要:
Hypotensive activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1 is hydrogen or alkyl;R.sub.2 and R.sub.3 are each independently phenyl, substituted phenyl, cycloalkyl, or R.sub.2 is hydrogen and R.sub.3 is heteroaryl;R.sub.4 and R.sub.5 are the same or different and each is hydrogen, hydroxy, alkoxy, alkanoyl or alkyl;R.sub.6 is hydrogen or alkyl; andn is 1, 2, 3 or 4; with the proviso that if R.sub.2 and R.sub.3 are each phenyl, at least one of R.sub.1, R.sub.4, R.sub.5 and R.sub.6 is other than hydrogen.
摘要:
A compound of the formula ##STR1## (symbols defined in the specification), its 3,4-dihydropyrimidine tautomer form and pharmaceutically acceptable salts thereof have calcium entry blocking activity. A process of preparation, pharmaceutical composition and method of using the compound to reduce blood pressure are also provided.
摘要:
Disubstituted heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein G is ##STR2## wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; p is 0, 1 or 2, Q is a single bond or ##STR3## and Z, A, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.6 are as defined herein.
摘要:
Pyrimidine compounds of the formula ##STR1## wherein X is sulfur or oxygen, Y is R.sub.11 or --O--R.sub.1, and R.sub.4 is aryl or heterocyclo are disclosed. These compounds are useful as cardiovascular agents, particularly anti-hypertensive agents, due to their calcium entry blocking vasodilator activity.
摘要:
Antibacterial activity is exhibited by 3-acylamino-2-azetidinones having in the 1-position a group of the formula ##STR1## or an ester of salt thereto, wherein R.sub.5 and R.sub.6 are the same or different and each is hydrogen, alkyl, phenyl or substituted phenyl.
摘要:
This disclosure describes a novel compounds and pharmaceutical compositions for inhibiting the TRPA1 ion channel and/or medical conditions related to TRPA1, such as pain.