John Wyeth Brother, Limited

Robin Michael Black

Alan C White

John Leheup Archibald

The invention relates to pyrimido 1,2-b!isoquinolines of the formula ##STR1## and their pharmaceutically acceptable acid addition salts. In the formula, R.sup.1 and R.sup.2 each represent hydrogen, hydroxyl, lower alkyl, lower alkoxy, trifluoromethyl, halogen, amino or mono- or di-(lower)alkylamino and R.sup.3 and R.sup.4 each represent hydrogen or lower alkyl. The compounds have utility as anti-gastric ulcer agents.

Pyrimido 1,2-b!isoquinolines

The invention relates to imidazo[1,2-a]quinolines of formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts. In formula I R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, lower alkyl, lower alkoxy, trifluoromethyl or halogen, R.sup.3 and R.sup.4 which may be the same or different each represent lower alkyl and R.sup.5 represents hydrogen, lower alkyl, aryl or arylloweralkyl. The compounds possess hypotensive activity.

Imidazo[1,2-a]quinolines

The invention relates to dibenzopyrimidoazepines of the formula (I) ##STR1## and their acid addition and quaternary ammonium salts. In formula (I) R.sup.1 and R.sup.2 each represent hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl and X represents two hydrogen atoms, an oxo group, a protected oxo group or an oximino group. The compounds in which X represents two hydrogen atoms, an oxo group or an oximino group possess hypoglycaemic activity. The compound in which X represents a protected oxo group are intermediates for preparing the compounds in which X is an oxo group. The dibenzopyrimidoazepines may be prepared by cyclising or cyclodehydrating novel morphanthridine derivatives.

Dibenzopyrimidoazepines

The invention relates to quinoline derivatives of the formula (I) ##STR1## and the pharmaceutically acceptable acid addition salts of those compounds capable of forming acid addition salts. In formula (I), R.sup.1 and R.sup.2 which may be the same of different each represent hydrogen, lower alkyl, lower alkoxy, trifluoromethyl or halogen, R.sup.3 and R.sup.4 which may be the same or different each represent lower alkyl and X represents hydroxy, halogen, hydrazino, or a radical of formula -NR.sup.5 R.sup.6 where R.sup.5 and R.sup.6 which may be the same or different each represent hydrogen or lower alkyl or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are both attached represent a saturated heterocyclic ring containing 5 to 7 ring atoms. The compounds possess hypotensive activity.

Certain 2-substituted 4-phenylquinoline-4-ols

The disclosure relates to derivatives of tetrahydro-1H-1,3-diazepine and hexahydro-1,3-diazocine of the general formula ##STR1## or pharmaceutically acceptable acid addition salts thereof wherein n represents 2 or 3, R.sup.3 and R.sup.4 which may be the same or different each represent hydrogen or lower alkyl, Ph represents phenyl, halophenyl, lower alkyl phenyl, di(lower alkyl) phenyl or lower alkoxy phenyl, R is hydroxyl, lower alkoxy or halogen, R.sup.1 is phenyl, halophenyl, lower alkyl phenyl, di(lower-alkyl phenyl, lower alkoxyphenyl or naphthyl and R.sup.6 is hydrogen or lower alkyl. The compounds have hypoglycemic activity.

Derivatives of tetrahydro-1H-1,3-diazepine and hexahydro-1,3-diazocine

The invention relates to compounds of the formula (I) ##SPC1## and their pharmaceutically acceptable acid addition salts. In the formula R.sup.1 and R.sup.2 are each hydrogen, hydroxyl, lower alkyl, lower alkoxy, trifluoromethyl or halogen. The compounds have hypotensive activity. Some also have hypoglycaemic activity.

Fused ring benzimidazole derivatives

The invention relates to fluorene derivatives of the formula ##SPC1## And their pharmaceutically acceptable acid addition salts. In the formula R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each represent hydrogen, hydroxyl, lower alkyl, lower alkoxy or halogen, R.sup.5 and R.sup.6 each represent hydrogen or lower alkyl and n represents 1 or 2. The compounds have hypoglycaemic activity.

Fluorene derivatives

The invention relates to bases of the formula ##SPC1## And their acid addition salts with pharmaceutically acceptable acids. In the formula R.sup.1 represents phenyl or phenyl substituted by one or more hydroxyl, lower alkyl lower alkoxy, trifluoromethyl or halogen groups. The compounds have hypoglycemic activity.

Hexahydroimidazo[1,5-A]pyridines

The disclosure relates to derivatives of imidazoline of the general formula ##SPC1## Or pharmaceutically acceptable acid addition salts thereof wherein R.sup.3 and R.sup.4 which may be the same or different each represent hydrogen or lower alkyl, Ph represents phenyl, halophenyl, lower alkyl phenyl, di(lower alkyl) phenyl or lower alkoxy phenyl, R is hydroxyl, lower alkoxy or halogen, R.sup.1 is phenyl, halophenyl, lower alkyl phenyl, di(lower alkyl)phenyl, lower alkoxy phenyl or napthyl and R.sup.6 is hydrogen or lower alkyl. The compounds have hypoglycemic activity.

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Porton, United Kingdom

Robin Michael Black