Substituted N-arylmethyl and heterocyclylmethyl-1H-pyrazolo (3,4-b) quinolin-4-amines and compositions and methods of use thereof

A pharmaceutical composition which comprises a compound of the formula:

• ##STR10## wherein:
• R.sup.1 is lower-alkyl;
• R.sup.2 is hydrogen, or lower-alkyl;
• R.sup.3 is hydrogen, or lower-alkyl;
• R.sup.4 is hydrogen, or lower-alkyl;
• R.sup.5 is pyridazinyl, pyrazinyl, and pyrimidinyl;
• or R.sup.4 and R.sup.5 together with the CH group to which they are bonded form an indanyl ring;
• and
• R.sup.6 is from one to three, the same or different, substituents selected from the group consisting of hydrogen, lower-alkoxy, hydroxy, lower-alkyl, and halogen;
• or a pharmaceutically acceptable acid-addition salt and/or hydrate thereof, or an enantiomer or a racemic mixture thereof;
• together with a pharmaceutically acceptable carrier, adjuvant, diluent, or vehicle.

A method for effecting cGMP-phosphodiesterase inhibition in a mammalian organism in need thereof which comprises administering to said organism a cGMP-phosphodiesterase inhibiting amount of a compound of the formula:

• ##STR11## wherein:
• R.sup.1 is lower-alkyl;
• R.sup.2 is hydrogen, or lower-alkyl;
• R.sup.3 is hydrogen, or lower-alkyl;
• R.sup.4 is hydrogen, or lower-alkyl;
• R.sup.5 is phenyl (or phenyl substituted by from one to three, the same or different, substituents selected from the group consisting of lower-alkoxy, cyano, hydroxy, 4-morpholinyllower-alkoxy, lower-alkyl, and halogen), phenyl-lower-alkyl, pyridinyl, furanyl, isoxazolyl, thienyl, oxazolyl, thiazolyl, pyridazinyl, pyrazinyl, and pyrimidinyl;
• or R.sup.4 and R.sup.5 together with the CH group to which they are bonded form an indanyl ring;
• and
• R.sup.6 is from one to three, the same or different, substituents selected from the group consisting of hydrogen, lower-alkoxy, hydroxy, lower-alkyl, and halogen;
• or a pharmaceutically acceptable acid-addition salt and/or hydrate thereof, or an enantiomer or a racemic mixture thereof.

A method for treating heart failure and/or hypertension in a mammalian organism in need thereof which comprises administering to said organism a therapeutically effective amount of a compound of the formula;

• ##STR12## wherein:
• R.sup.1 is lower-alkyl;
• R.sup.2 is hydrogen, or lower-alkyl;
• R.sup.3 is hydrogen, or lower-alkyl;
• R.sup.4 is hydrogen, or lower-alkyl;
• R.sup.5 is phenyl (or phenyl substituted by from one to three, the same or different, substituents selected from the group consisting of lower-alkoxy, cyano, hydroxy, 4-morpholinyllower-alkoxy, lower-alkyl, and halogen), phenyl-lower-alkyl, pyridinyl, furanyl, isoxazolyl, thienyl, oxazolyl, thiazolyl, pyridazinyl, pyrazinyl, and pyrimidinyl;
• or R.sup.4 and R.sup.5 together with the CH group to which they are bonded form an indanyl ring;
• and
• R.sup.6 is from one to three, the same or different, substituents selected from the group consisting of hydrogen, lower-alkoxy, hydroxy, lower-alkyl, and halogen;
• or a pharmaceutically acceptable acid-addition salt and/or hydrate thereof, or an enantiomer or a racemic mixture thereof.

A method for treating angina pectoris, congestive heart disease or myocardial infarction in a mammalian organism in need thereof which comprises administering to said organism a therapeutically effective amount of a compound of the formula:

• ##STR13## wherein:
• R.sup.1 is lower-alkyl;
• R.sup.2 is hydrogen, or lower-alkyl;
• R.sup.3 is hydrogen, or lower-alkyl;
• R.sup.4 is hydrogen, or lower-alkyl;
• R.sup.5 is phenyl (or phenyl substituted by from one to three, the same or different, substituents selected from the group consisting of lower-alkoxy, cyano, hydroxy, 4-morpholinyllower-alkoxy, lower-alkyl, and halogen), phenyl-lower-alkyl, pyridinyl, furanyl, isoxazolyl, thienyl, oxazolyl, thiazolyl, pyridazinyl, pyrazinyl, and pyrimidinyl;
• or R.sup.4 and R.sup.5 together with the CH group to which they are bonded form an indanyl ring;
• and
• R.sup.6 is from one to three, the same or different, substituents selected from the group consisting of hydrogen, lower-alkoxy, hydroxy, lower-alkyl, and halogen;
• or a pharmaceutically acceptable acid-addition salt and/or hydrate thereof, or an enantiomer or a racemic mixture thereof, in combination with a nitrate.