Abstract: A one-step process for the preparation of 2,4-dihaloquinazolines is disclosed beginning with methoxycarbonyl- or phenoxycarbonyl-derivatives of substituted phenylureas which are cyclized and concomitantly halogenated with a cyclizing-halogenating reagent such as N,N-dimethylaniline in phosphorus oxychloride. The 2,4-dihaloquinazolines of the instant process are particularly valuable as intermediates in the preparation of 4-amino-2-(4-substituted-piperazin-1-yl) quinazolines useful in the treatment of cardiovascular disorders such as hypertension.

Abstract: 2-Halo-4-aminoquinazolines are produced by a two-step process involving cyclization of 1-phenyl-3-cyanoureas or 1-phenyl-3-cyanothioureas in the presence of phosphorus halides and phosphorus oxyhalides to provide a phosphoquinazoline intermediate which is hydrolyzed to the quinazoline. Exemplary of the process is the intramolecular cyclization of 1-(3,4-dimethoxyphenyl)-3-cyanourea in the presence of phosphorus pentachloride and phosphorus oxychloride to a phosphoquinazoline intermediate which is subsequently hydrolyzed with formic acid to 2-chloro-4-amino-6,7-dimethoxy-quinazoline. The 2-halo-4-aminoquinazolines of the instant process are particularly valuable as intermediates in the preparation of 4-amino-2-(4-substituted-piperazin-l-yl)quinazolines useful in the treatment of cardiovascular disease, e.g. hypertension.

Abstract: A series of 2-(substituted)phenyl-5-(5-1H-tetrazolyl)pyrimidin-4(3H)-ones is provided for use as inhibitors of allergic reactions. The compounds show antiallergy activity by both oral and parenteral routes of administration.

Abstract: Substituted 2-aminomethyl-4-phenyl-1,3-benzodioxans and derivatives thereof have been found to possess valuable anticonvulsant and antiarrhythmia activity in mammals. For example, cis-6-chloro-2-methylaminomethyl-4-phenyl-1,3-benzodioxan hydrochloride possesses potent anticonvulsant activity while cis-2-isopropylaminomethyl-4-phenyl-1,3-benzodioxan hydrochloride has potent antiarrhythmia activity.

Abstract: A series of 1,6-dihydro-6-oxo-2-(ortho-substituted phenyl)pyrimidine-5-carboxylic acid derivatives is provided for use as inhibitors of allergic reactions. The compounds show antiallergy activity by both oral and parenteral routes of administration.

Abstract: dl-N-Cyclopropylmethyl-3-hydroxy-9-azamorphinan is a compound known to possess analgesic activity that is about twice as potent as pentazocine. Resolution of the compound into its levorotatory and dextrorotatory isomers and subsequent animal testing revealed that l-N-cyclopropylmethyl-3-hydroxy-9-azamorphinan was much more potent than the dl-mixture.

Abstract: The 4-amino-6,7-dimethoxy-2-[4-(5-lower alkylthio-1,3,4-oxadiazole-2-carbonyl)-piperazin-1-yl]-quinazolines are potent antihypertensive drugs which have little or no .alpha.-adrenergic blocking activity.

Abstract: Compounds having the formula ##STR1## wherein Z is a substituted or unsubstituted oxazole, is isoxazole, thiazole or isothiazole group are potent antihypertensive drugs which have generally less .alpha.-adrenergic blocking activity than does 2-[4-(2-furoyl)-piperazin-1-yl]-4-amino-6,7-dimethoxy-quinazoline which is a known potent antihypertensive drug.

Abstract: Optionally substituted 6-alkoxymethyl-1,2,3,5-tetrahydroimidazo[2,1-b]-quinazolin-2-ones and 7-alkoxymethyl-6-[H]-1,2,3,4-tetrahydropyrimido[2,1-b]-quinazolin-2-ones or the pharmaceutically acceptable salts thereof are compounds useful as blood platelet anti-aggregative and/or antihypertensive and/or bronchodilator agents in mammals, including humans.

Abstract: A new process has been developed for the synthesis of optionally substituted 1,2,3,5-tetrahydroimidazo[2,1-b]quinazolin-2-ones. In particular, the process is particularly adaptable for the preparation of the 5,6-disubstituted compounds, e.g., 5,6-dimethyl-1,2,3,5-tetrahydroimidazo-[2,1-b]quinazolin-2-one. The compounds so prepared are useful as blood platelet anti-aggregative and/or antihypertensive agents in mammals, including humans.

Abstract: A new process has been developed for the synthesis of optionally substituted 1,2,3,5-tetrahydroimidazo[2,1-b]quinazolin-2-ones.

Abstract: Series of 5-endo-benzoyloxy-N-[amino(lower)-alkyl]bicyclo[2.2.2]octane-2,3-di-endo-c arboxylic acid imides, 5-endo-(3-indolecarbonyloxy)-N-[amino-(lower)alkyl]bicyclo[2.2.2]octane-2, 3-di-endo-carboxylic acid imides, 5-endo-n-substituted-carbamoyloxy-N-[amino(lower)alkyl]bicyclo[2.2.2]octan e-2,3-di-endo-carboxylic acid imides and 5-endo-(1-naphthoyloxy)-N-[amino(lower)alkyl]bicyclo[2.2.2]octane-2,3-di-e ndo-carboxylic acid imides have been found to possess unique prophylactic and therapeutic activity as anti-arrhythmia agents. An example of such a compound possessing activity is 5-endo-(3-indolecarbonyloxy)-N-(3-dimethylaminopropyl)bicyclo[2.2.

Abstract: Optionally substituted 1-H-2,3,3a,4-Tetrahydro-2-oxopyrrolo[2,3-b]quinolines or the pharmaceutically acceptable salts thereof are compounds useful as blood platelet anti-aggregative and/or antihypertensive agents in mammals, including humans.