Substituted heterocyclylisoquinolinium salts and compositions and method of use thereof

A compound of the formula:

• ##STR348## wherein:
• R.sup.1 is hydrogen, or lower-alkyl;
• R.sup.2 and R.sup.3 are independently hydrogen, or lower-alkyl;
• or R.sup.2 and R.sup.3 together form a cycloalkyl ring, or a lower-alkylidene group;
• R.sup.4 and R.sup.5 are independently lower-alkynyl, lower-alkoxy, phenyl (or phenyl substituted by lower-alkoxy, halogen, lower-alkyl, polyfluorolower-alkyl, polychlorolower-alkyl, or hydroxy), a 5- or 6-membered monocyclic aromatic heterocyclic ring system containing from one to three, the same or different, heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur (or said 5- or 6-membered monocyclic aromatic heterocyclic ring system substituted on any available carbon atom thereof by hydroxy, lower-alkyl, oxo, nitro, halogen, or lower-alkoxy;
• or on any available nitrogen atom thereof by lower-alkyl, tri-lower-alkylsilyl, trilower-alkylsilyl-lower-alkoxy-lower-alkyl, or phenyl-lower-alkyl (or said phenyl-lower-alkyl group substituted on the phenyl group by lower-alkoxy, lower-alkyl or halogen));
• a 9- or 10-membered bicyclic aromatic heterocyclic ring system containing from one to two, the same or different, heteroatoms selected from the group consisting of oxygen, nitrogen and sulfur (or said 9- or 10-membered bicyclic aromatic heterocyclic ring system substituted at any available carbon atom thereof by hydroxy, lower-alkyl, oxo, nitro, halogen, or lower-alkoxy;
• or on any available nitrogen atom thereof by lower-alkyl, trilower-alkylsilyl, trilower-alkylsilyl-lower-alkoxy-lower-alkyl, or phenyl-lower-alkyl (or said phenyl-lower-alkyl group substituted on the phenyl group by lower-alkoxy, lower-alkyl, or halogen));
• or a 5- or 6-membered monocyclic nonaromatic heterocyclic ring system containing from one to two, the same or different, heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur (or said 5- or 6-membered nonaromatic heterocyclic ring system substituted on any available carbon atom thereof by hydroxy, lower-alkyl, oxo, nitro, halogen, or lower-alkoxy, or on any available nitrogen atom thereof by lower-alkyl, trilower-alkylsilyl, trilower-alkylsilyl-lower-alkoxy-lower-alkyl, or phenyl-lower-alkyl (or said pheny-lower-alkyl group substituted on the phenyl group by lower-alkoxy, lower-alkyl or halogen));
• or R.sup.2 and R.sup.4 and/or R.sup.3 and R.sup.5 taken together with the carbon atoms to which they are attached form a bicyclic ring system of the formula ##STR349## wherein B is:
• phenyl, or a 5- or 6-membered monocyclic aromatic heterocyclic ring system containing from one to three, the same or different, heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, (or said B ring substituted on any available carbon atom thereof by lower-alkoxy, or lower-alkyl), and n is an integer from one to three;
• R.sup.6 is hydrogen, or from one to four, the same or different, substituents in any of the 7-, 8-, 9-, or 10-positions (if A is a six-membered ring), or in any of the 6-, 7-, 8-, or 9- position (if A is a five-membered ring) selected from the group consisting of lower-alkyl, lower-alkanoyloxy, halogen, nitro, hydroxy, lower-alkoxy, methylenedioxy, polychlorolower-alkyl, OCO(CH.sub.2)m, C(O)O alkyl, OC(O)alkyl, C(O)Oalkyl, CO.sub.2.sup.-, carboxy, sulfo, SO.sub.3.sup.-, PO.sub.3 H, PO.sub.3.sup.-, cyano, polyfluorolower-alkyl, OC(O) alkyl-CH.dbd.CH-alkyl, OC(O)-lower-alkenyl-C(O)alkyl, alkoxy, OC(O)alkylC(O)Oalkyl, amino, and lower-alkylsulfonylamino, wherein m is an integer from one to four;
• A together with the carbon and nitrogen atoms to which it is attached forms a 5- or 6-membered monocyclic aromatic heterocycle containing from two to three, the same or different, heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur (or said 5- or 6-membered monocyclic aromatic heterocycle substituted on any available carbon atom thereof by hydroxy, OC(O)alkyl-CH.dbd.CH-alkyl, OC(O)alkyl, OC(O)lower-alkenyl-C(O)Oalkyl, alkoxy, OC(O)alkylC(O)Oalkyl, nitro, amino, lower-alkylsulfonylamino, lower-alkyl, lower-alkoxy, or halogen;
• or on any available nitrogen atom thereof by phenyl (or said phenyl group substituted by lower-alkoxy, lower-alkyl or halogen), diphenylmethyl, naphthyl-lower-alkyl (or said naphthyl-lower-alkyl group substituted on the naphthyl group by lower-alkoxy, lower-alkyl or halogen), lower-alkyl, or phenyl-lower-alkyl (or said phenyl-lower-alkyl group substituted on the phenyl group by lower-alkoxy, lower-alkyl or halogen));
• X.sup.- is an anion;
• and p is zero when R.sup.6 is a negatively charged radical, and p is one when R.sup.6 is other than a negatively charged radical;
• or a pharmaceutically acceptable acid-addition salt of basic members thereof;
• or a hydrate thereof;
• or a stereoisomer thereof.