Tricyclic lactams, method for making them, pharmaceutical compositions containing them

Claim 2

A compound of the formula wherein R is hydrogen or lower alkyl; R 1 is hydrogen, hydroxy, lower alkoxy, cyano, lower alkyl, halogen, -NR 2 R 3 , - CONR 2 R 3 , (wherein R 2 and R 3 are independently hydrogen, lower alkyl, or hydroxy lower alkyl), - NH CO R 2 , -COOR 2 (wherein R 2 is as defined above), or wherein M is sulfur or NH; with the proviso that R and R 1 are not both hydrogen; Z is selected from -CH=CH - , wherein n is 1,2,3 or 4, -(CH 2 ) p -S(O) m -(CH 2 ) r , or -(CH 2 ) p -O-(CH 2 ) r wherein m is 0,1 or 2, and p and r are independently 0,1,2 or 3 subject to the proviso that r + p is 0,1,2 or 3; A is a substituted or unsubstituted benzo or pyrido ring which when substituted have 1 to 3 substitutents independently selected from halogen, hydroxy, lower alkyl and lower alkoxy; and pharmaceutically acceptable salts thereof.

Claim 3

A compound as defined in claim 1 characterized in that R 1 is hydroxy, lower alkoxy, cyano, -NR2 R 3, -CONR 2 R 3o r - NHCOR 2 wherein R 2 and R3 are as defined in claim 1.

Claim 4

A compound as defined in claim 2, characterized.in that Rl is cyano, amino or

Claim 5

A compound as defined in anyone of the preceding claims, characterized in that R is hydrogen or methyl.

Claim 6

A compound as defined in any one of the preceding claims, characterized in that R is hydrogen and R l is cyano.

Claim 7

A compound as defined in any one of the preceding claims, characterized in that Z is

Claim 9

A compound as defined in any one of the preceding claims, characterized in that A is a benzo or a 3-pyrido ring.

Claim 10

2-cyano-5,6-dihydro-benzo[f] quinolin-3[4H]-one; 2-cyano-benzo[f] quinolin-3[4H]-one; 9-cyano-5,6-dihydro-3,7-phenanthrolin-8[7H]-one; 9-cyano -3,7-phenanthrolin-8[7H]-one; or 2-cyano-4,6-dihydro-3H-[2]benzopyrano-[3,4-b] pyridin-3-one.

Claim 11

A pharmaceutical composition comprising a compound as defined in any one of the preceding claims in admixture with a pharmaceutically acceptable carrier or excipient.

Claim 12

A process for making a compound of formula I as defined in claim 1, characterized by reacting a compound of formula II in which R and A are as defined in claim 1, and X is (̵CH 2 )̵ n , or (̵CH 2 )̵ p -O(̵CH 2 )̵ r or (̵CH 2 )̵ p S(̵CH 2 )̵ r wherein n,p and r are as defined in claim 1, with a compound of formula III in which R 8 is hydrogen, cyano, lower alkoxy or lower alkyl under basic conditions to form a compound of formula I a (and when R and R 8 are both hydrogen, halogenating the so obtained compound of formula Ia to produce a compound of formula I in which R 1 is halogen), whereby a compound of formula I is obtained in which A,R, and X are as defined above and R 1 is halogen, hydrogen, cyano, loweralkoxy or loweralkyl, and thereafter if desired, converting such compound of formula:I into another compound of formula I by a known method, and isolating the compound of formula I as such or as a pharmaceutically acceptable salt.