Benzazepine and benzothiazepine derivatives

A method of treating a host having a disease susceptible to treatment with a vasodilator which comprises administering to said host an effective amount of a compound having the formula ##STR48## and the pharmaceutically acceptable salts thereof, wherein X is --CH.sub.2 --or --S--;

• R.sub.1 is ##STR49## when X is --C.sub.2 2--, R.sub.2 is ##STR50## when X is --S--, R.sub.2 is ##STR51## R.sub.3 and R.sub.4 are each independently hydrogen halogen, alkyl, alkoxy, aryloxy, arylalkoxy, arylalkyl,-cyano, hydroxy, alkanoyloxy, ##STR52## fluoro substituted alkoxy, fluoro substituted alkyl, (cycloalkyl)alkoxy, --NO.sub.2, --NY.sub.10 Y.sub.11, --S(O).sub.m aryl, ##STR53## n or n' are independently 0, 1, 2 or 3;
• m is 0, 1 or 2;
• Y.sub.1 and Y.sub.2 are independently hydrogen or alkyl, Y.sub.1 is hydrogen and Y.sub.2 is alkenyl, alkynyl, aryl, heteroaryl, or cycloalkyl, or Yl and Y2 together with the carbon atom to which they are attached are cycloalkyl;
• Y.sub.3 is hydrogen, alkyl, alkanoyl, alkenyl, arylcarbonyl, heteroarylcarbonyl, or ##STR54## Y.sub.4 and Y.sub.5 are each independently hydrogen, alkyl, aryl or arylalkyl, provided that when both are present they are not both hydrogen, and provided further that when both are attached to the same carbon atom neither of them is hydrogen;
• Y.sub.6 and Y.sub.7 are each independently hydrogen, alkyl, cycloalkyl or arylalkyl or Y.sub.6 and Y.sub.7 together with the nitrogen atom to which they are attached are azetidinyl, pyrrolidinyl, piperidinyl, or morpholinyl;
• 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 ##STR55## Y.sub.12 is hydroxy, alkoxy, aryloxy, amino, alkylamino or dialkylamino;
• Y.sub.13 is alkyl, alkoxy or aryloxy;
• and,
• Y.sub.14 is hydrogen, hydroxy, alkoxy, aryloxy or arylalkoxy. wherein
• the terms "alkyl" and "alkoxy" refer to both straight and branched chain groups having 1 to 10 carbon atoms;
• the term "alkenyl" refers to both straight and branched chain groups having 2 to 10 carbon atoms;
• the term "aryl" refers to phenyl and substituted phenyl wherein said substituents may be 1, 2 or 3 groups independently selected from amino, alkylamino, dialkylamino, nitro, halogen, hydroxyl, trifluoromethyl, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, alkylthio of 1 to 4 Carbon atoms, alkanoyloxy, carbonyl, or carboxyl;
• the term "alkanoyl" refers to groups having the formula ##STR56## having 2 to 11 carbon atoms;
• the term "heteroaryl" refers to an aromatic heterocyclic group selected from pyridinyl, pyrrolyl, imidazolyl, furyl, thienyl, oxazolyl and thiazolyl;
• the term "cycloaalkyl" refers to groups having 3, 4, 5, 6 or 7 carbon atoms;
• the term "halogen" refers to fluorine, chlorine, bromine and iodine;
• and,
• the term "fluoro substituted alkyl" and "fluoro substituted alkoxy" refer to alkyl and alkoxy groups in which one or more hydrogens have been replaced by fluorine atoms.

A compound having the formula ##STR57## or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is ##STR58## R.sub.2 is ##STR59## R.sub.3 and R.sub.4 are each independently hydrogen, halogen, alkyl, alkoxy, aryloxy, arylalkoxy, diarylalkoxy, arylalkyl, cyano, hydroxy, alkanoyloxy, ##STR60## fluoro substituted alkoxy, fluoro substituted alkyl, (cycloalkyl)alkoxy, --NO.sub.2, --NY.sub.10 Y.sub.11,--S(O).sub.m alkyl, --S(O).sub.m aryl, ##STR61## n is 0, 1, 2 or 3;

• m is 0, 1 or 2;
• Y.sub.1 and Y.sub.2 are each hydrogen or alkyl, 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 ##STR62## Y.sub.4 and Y.sub.5 are each independently hydrogen, alkyl, aryl or arylalkyl, provided that when both are present they are not both hydrogen, and provided further that when both are attached to the same carbon atom neither of them is hydrogen;
• Y.sub.6 and Y.sub.7 are each independently hydrogen, alkyl, cycloalkyl or arylalkyl or Y.sub.6 and Y.sub.7 together with the nitrogen atom to which they are attached are azetidinyl, pyrrolidinyl, piperidinyl, or morpholinyl;
• 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 eacn independently hydrogen, alkyl, alkanoyl, arylcarbonyl, heteroarylcarbonyl, or ##STR63## Y.sub.12 is hydroxy, alkoxy, aryloxy, amino, alkylamino or dialkylamino;
• and
• Y.sub.13 is alkyl, alkoxy or aryloxy. wherein
• the terms "alkyll" and "alkoxy" refer to both straight and branched chain groups having 1 to 10 carbon atoms;
• the term "alkenyl" refers to both straight and branched chain groups having 2 to 10 carbon atoms;
• the term "aryl" refers to phenyl and substituted phenyl wherein said substituents may be 1, 2 or 3 groups independently selected from amino, alkylamino, dialkylamino, nitro, halogen, hydroxyl, trifluoromethyl, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, alkylthio of 1 to 4 carbon atoms, alkanoyloxy. carbonyl, or carboxyl;
• the term "alkanoyl" refers to groups having the formula ##STR64## having 2 to 11 carbon atoms;
• the term "heteroaryl" refers to an aromatic heterocyclic group selected from pyridinyl, pyrrolyl, imidazolyl, furyl, thienyl, oxazolyl and thiazolyl;
• the term "cycloalkyl" refers to groups having 3,4, 5, 6 or 7 carbon atoms;
• the term "halogen" refers to fluorine, chlorine, bromine and iodine;
• and,
• the term "fluoro substituted alkyl" and "fluoro substituted alkoxy" refer to alkyl and alkoxy groups in which one or more hydrogens have been replaced by fluorine atoms.