Azepine compounds

A compound of the Formula ##STR158## or a tautomer thereof or a pharmaceutically acceptable salt thereof;

• wherein
• R.sub.1, R.sub.3, R.sub.4 and R.sub.6 are independently hydrogen, halo, C.sub.1 -C.sub.4 haloalkyl, C.sub.6 -C.sub.14 aryl, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, C.sub.6 -C.sub.14 aryl(C.sub.1 -C.sub.4)alkyl, C.sub.6 -C.sub.14 aryl(C.sub.1 -C.sub.4)alkenyl, C.sub.6 -C.sub.14 aryl(C.sub.1 -C.sub.4)alkynyl, C.sub.1 -C.sub.4 hydroxyalkyl, nitro, amino, cyano, C.sub.1 -C.sub.6 alkanoylamino, hydroxy, thiol, C.sub.1 -C.sub.6 alkanoyloxy, azido, C.sub.1 -C.sub.4 alkoxy, carboxy, carbonylamido, C.sub.1 -C.sub.4 alkylthiol, C.sub.3 -C.sub.18 trialkylsilyloxy, or C.sub.8 -C.sub.18 phenyldialkylsilyloxy;
• X' and Y' are independently hydrogen, halogen;
• hydroxy and hydrogen;
• nitro and hydrogen;
• C.sub.1 -C.sub.6 alkanoylamido and hydrogen;
• X' and Y' together form an oxirane ring;
• X' and Y' are vicinal C.sub.1 -C.sub.6 alkanoylamido C.sub.1 -C.sub.6 alkanoyloxy groups;
• or X' and Y' together form a double bond;
• Q is OR.sub.7 or NR.sub.12 R.sub.13, wherein R.sub.12 and R.sub.13 are independently selected from hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl(C.sub.3 -C.sub.6)alkyl, C.sub.6 -C.sub.14 aryl, C.sub.6 -C.sub.14 aryl(C.sub.1 -C.sub.6)alkyl, and CH.sub.2 Y wherein Y is selected from (CHOH).sub.n CH.sub.2 OH and (CH.sub.2).sub.m R.sup.c where m is 0 to 5, n is 1 to 5 and R.sup.c is selected from hydroxy, C.sub.1 -C.sub.6 alkoxycarbonyl, and NR.sup.d R.sup.e in which R.sup.d and R.sup.e are independently selected from hydrogen and C.sub.1 -C.sub.6 alkyl or R.sup.d and R.sup.e, together with the nitrogen atom to which they are attached, form a 5-, 6- or 7-membered heterocyclic ring which, in addition to said nitrogen atom, optionally contains one additional heteroatom selected from nitrogen, oxygen and sulfur;
• or R.sub.12 and R.sub.13, together with the nitrogen atom to which they are attached, form a 5-, 6- or 7-membered heterocyclic ring which is bonded to said compound through said nitrogen atom, said heterocyclic ring optionally containing, in addition to said nitrogen atom, one additional heteroatom selected from nitrogen, oxygen and sulfur;
• R.sub.7 is hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.6 alkanoyl;
• and
• T is selected from hydrogen, halo, hydroxy, C.sub.1 -C.sub.6 alkanoyloxy, C.sub.1 -C.sub.4 alkyl which may optionally bear a substituent selected from amino, C.sub.1 -C.sub.4 alkanoylamino, carboxy and carboxamido;
• and C.sub.6 -C.sub.14 aryl(C.sub.1 -C.sub.4)alkyl.

A compound of the Formula ##STR159## or a tautomer thereof or a pharmaceutically acceptable salt thereof;

• wherein
• R.sub.1, R.sub.3, R.sub.4 and R.sub.6 are independently hydrogen, halo, C.sub.1 -C.sub.4 haloalkyl, C.sub.6 -C.sub.4 aryl, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, C.sub.6 -C.sub.14 aryl(C.sub.1 -C.sub.4)alkyl, C.sub.6 -C.sub.14 aryl(C.sub.1 -C.sub.4)alkenyl, C.sub.6 -C.sub.4 aryl(C.sub.1 -C.sub.4)alkynyl, C.sub.1 -C.sub.4 hydroxyalkyl, nitro, amino, cyano, C.sub.1 -C.sub.6 alkanoylamino, hydroxy, thiol, C.sub.1 -C.sub.6 alkanoyloxy, azido, C.sub.1 -C.sub.4 alkoxy, carboxy, carbonylamido, C.sub.1 -C.sub.4 alkylthiol, C.sub.3 -C.sub.18 trialkylsilyloxy, or C.sub.8 -C.sub.18 phenyldialkylsilyloxy;
• X' and Y' are independently hydrogen, halogen;
• hydroxy and hydrogen;
• nitro and hydrogen;
• C.sub.1 -C.sub.6 alkanoylamido and hydrogen;
• X' and Y' together form an oxirane ring;
• X' and Y' are vicinal C.sub.1 -C.sub.6 alkanoylamido C.sub.1 -C.sub.6 alkanoyloxy groups;
• or X' and Y' together form a double bond;
• one of A' and B' is hydrogen and the other of A' and B' is C.sub.1 -C.sub.4 alkyl or C.sub.6 -C.sub.14 ar(C.sub.1 -C.sub.4)alkyl;
• Q is OR.sub.7 or NR.sub.12 R.sub.13, wherein R.sub.12 and R.sub.13 are independently selected from hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.6)alkyl, C.sub.6 -C.sub.14 aryl, C.sub.6 -C.sub.14 aryl(C.sub.1 -C.sub.6)alkyl, and CH.sub.2 Y wherein Y is selected from (CHOH).sub.n CH.sub.2 OH and (CH.sub.2).sub.m R.sup.c where m is 0 to 5, n is 1 to 5 and R.sup.c is selected from hydroxy, C.sub.1 -C.sub.6 alkoxycarbonyl, and NR.sup.d R.sup.e in which R.sup.d and R.sup.e are independently selected from hydrogen and C.sub.1 -C.sub.6 alkyl or R.sup.d and R.sup.e, together with the nitrogen atom to which they are attached, form a 5-, 6- or 7-membered heterocyclic ring which, in addition to said nitrogen atom, optionally contains one additional heteroatom selected from nitrogen, oxygen and sulfur;
• or R.sub.12 and R.sub.13, together with the nitrogen atom to which they are attached, form a 5-, 6- or 7-membered heterocyclic ring which is bonded to said compound through said nitrogen atom, said heterocyclic ring optionally containing, in addition to said nitrogen atom, one additional heteroatom selected from nitrogen, oxygen and sulfur;
• R.sub.7 is hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.6 alkanoyl;
• and
• T is selected from hydrogen, halo, hydroxy, C.sub.1 -C.sub.6 alkanoyloxy, C.sub.1 -C.sub.4 alkyl which may optionally bear a substituent selected from amino, C.sub.1 -C.sub.4 alkanoylamino, carboxy and carboxamido;
• and C.sub.6 -C.sub.14 aryl(C.sub.1 -C.sub.4)alkyl.

A compound of the Formula ##STR160## or a tautomer thereof or a pharmaceutically acceptable salt thereof;

• wherein
• R.sub.1, R.sub.3, R.sub.4 and R.sub.6 are independently hydrogen, halo, C.sub.1 -C.sub.4 haloalkyl, C.sub.6 -C.sub.4 aryl, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, C.sub.6 -C.sub.14 aryl(C.sub.1 -C.sub.4)alkyl, C.sub.6 -C.sub.14 aryl(C.sub.1 -C.sub.4)alkenyl, C.sub.6 -C.sub.4 aryl(C.sub.1 -C.sub.4)alkynyl, C.sub.1 -C.sub.4 hydroxyalkyl, nitro, amino, cyano, C.sub.1 -C.sub.6 alkanoylamino, hydroxy, thiol, C.sub.1 -C.sub.6 alkanoyloxy, azido, C.sub.1 -C.sub.4 alkoxy, carboxy, carbonylamido, C.sub.1 -C.sub.4 alkylthiol, C.sub.3 -C.sub.18 trialkylsilyloxy, or C.sub.8 -C.sub.18 phenyldialkylsilyloxy;
• A is (CH.sub.2).sub.n, wherein n is 1 to 4;
• X' and Y' are independently hydrogen, halogen;
• hydroxy and hydrogen;
• nitro and hydrogen;
• C.sub.1 -C.sub.6 alkanoylamido and hydrogen;
• X' and Y' together form an oxirane ring;
• X' and Y' are vicinal C.sub.1 -C.sub.6 alkanoylamido C.sub.1 -C.sub.6 alkanoyloxy groups;
• or X' and Y' together form a double bond;
• Q is OR.sub.7 or NR.sub.12 R.sub.13, wherein R.sub.12 and R.sub.13 are independently selected from hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.6)alkyl, C.sub.6 -C.sub.14 aryl, C.sub.6 -C.sub.14 aryl(C.sub.1 -C.sub.6)alkyl, and CH.sub.2 Y wherein Y is selected from (CHOH).sub.n CH.sub.2 OH and (CH.sub.2).sub.m R.sup.c where m is 0 to 5, n is 1 to 5 and R.sup.c is selected from hydroxy, C.sub.1 -C.sub.6 alkoxycarbonyl, and NR.sup.d R.sup.e in which R.sup.d and R.sup.e are independently selected from hydrogen and C.sub.1 -C.sub.6 alkyl or R.sup.d and R.sup.e, together with the nitrogen atom to which they are attached, form a 5-, 6- or 7-membered heterocyclic ring which, in addition to said nitrogen atom, optionally contains one additional heteroatom selected from nitrogen, oxygen and sulfur;
• or R.sub.12 and R.sub.13, together with the nitrogen atom to which they are attached, form a 5-, 6- or 7-membered heterocyclic ring which is bonded to said compound through said nitrogen atom, said heterocyclic ring optionally containing, in addition to said nitrogen atom, one additional heteroatom selected from nitrogen, oxygen and sulfur;
• R.sub.7 is hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.6 alkanoyl;
• and
• T is selected from hydrogen, halo, hydroxy, C.sub.1 -C.sub.6 alkanoyloxy, C.sub.1 -C.sub.4 alkyl which may optionally bear a substituent selected from amino, C.sub.1 -C.sub.4 alkanoylamino, carboxy and carboxamido;
• and C.sub.6 -C.sub.14 aryl(C.sub.1 -C.sub.4)alkyl.