Abstract: Compounds of the formula ##SPC1##Where A is selected from the group consisting of hydrogen, halogen, lower alkoxy, lower alkylthio, hydroxyl, thio, trifluoromethyl, lower diakylaminoalkyl, amino, lower alkylamino and lower dialkylamino,Where B is selected from the group consisting of hydrogen, lower alkyl, lower alkoxyl, lower alkylthio, hydroxyl, thio, trifluoromethyl, lower dialkylaminoalkoxyl, amino, lower alkylamino, and lower dialkylamino,Where C is selected from the group consisting of hydrogen, halogen, lower alkyl, lower alkoxyl, lower alkylthio, hydroxyl, thio, trifluoromethyl, lower dialkylaminoalkoxy, amino, lower alkylamino and lower dialkylamino,Where D is selected from the group consisting of hydrogen, halogen, lower alkyl, lower alkoxy, lower alkylthio, hydroxyl, thio, trifluoromethyl, lower dialkylaminoalkoxyl, amino, lower alkylamino and lower diaklamino,Where n is an integer from 2 to 12 inclusive,And Y is selected from the group consisting of amino, lower alkylamino, lower dialkylamino, and

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: 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: 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: N-substituted-14-hydroxy-3-substituted-morphinan derivatives have been found to possess potent narcotic agonist or antagonist activity. In particular, the compound 3,14-dihydroxy-N-cyclopropylmethylmorphinan has been found to possess potent agonist-antagonist activity.

Abstract: A series of 5-endo-(3-indolecarbonyloxy)-N-[amino-(lower)alkyl]bicyclo[2.2.1]heptane-2 ,3-di-endo-carboxylic acid imides having the formula ##SPC1##Wherein R.sup.1 is H, Cl, Br, F or (lower)alkyl, R.sup.7 is H or methyl, R.sup.2 and R.sup.3 are alike or different and each is H, Cl, Br, F, (lower)alkyl, nitro, CF.sub.3, OH or (lower)alkoxy, n is an integer of 2 to 4 inclusive and R.sup.4 and R.sup.5 are alike or different and each is H, (lower)alkyl or when taken together with the nitrogen a radical of the formula ##SPC2##In which R.sup.6 is (lower)alkyl; or a pharmaceutically acceptable acid addition salt thereof have been found to possess unique prophylactic and therapeutic activity as anti-arrhythmia agents. An example of such a compound possessing excellent activity is 5-endo-(3-indolecarbonyloxy)-N-(3-dimethylaminopropyl)bicyclo-[2.2.1]hepta ne-2,3-di-endo-carboxylic acid imide hydrochloride.

Abstract: 1-[L-(-)-.gamma.-amino-.alpha.-hydroxybutyryl]-kanamycin A is a compound useful as an antibacterial agent. A new process for its preparation has been developed which comprises using aldehyde blocking agents on the amine functions prior to acylation with L-(-)-.gamma.-amino-.alpha.-hydroxybutyric acid.

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.

Abstract: N-substituted-9-hydroxy-6,7-benzomorphans have been found to possess potent narcotic agonist and/or antagonist activity. In particular, the compound 2'-hydroxy-2-cyclobutylmethyl-5-allyl-9.beta.-hydroxy-9.alpha.-methyl-6,7- benzomorphan has been found to possess potent narcotic agonist and antagonist activity. These compounds are prepared by total synthesis and are not derived from opium alkaloids.

Abstract: Orally effective, analgetic compositions have been developed which are useful in the prevention of drug abuse because upon parenteral administration, they do not produce analgesia, euphoria, or physical dependence. Such compositions comprise an orally active, strong analgetic in oral dosage form and containing, for each analgetic dose of the analgetic agent, an amount of naloxone sufficient, upon parenteral administration of said oral dosage form, to negate the analgetic, euphoretic and dependence producing action of the composition, but insufficient to block the therapeutic effect of the analgetic when the admixture is taken orally.

Abstract: 3'-Deoxybutirosin A (3'-deoxyambutyrosin A), which is prepared from butirosin A, possesses an improved antibacterial spectra, especially against butirosin A resistant organisms.

Abstract: N-Substituted-3-hydroxy-8-oxamorphinans have been found to possess potent narcotic agonist and/or antagonist activity. In particular, the compound l-N-cyclopropylmethyl-3-hydroxy-14.beta.-methyl-8-oxamorphinan has been found to possess potent narcotic antagonist and agonist activity. These compounds are prepared by total synthesis and are not derived from opium alkaloids.

Abstract: N-Substituted-9-alkoxy-5-methyl-6,7-benzomorphans have been found to possess potent narcotic agonist and/or antagonist activity. In particular, the compound 2-cyclopropylmethyl-2'-hydroxy-9.alpha.-methoxy-5-methyl-6,7-benzomorphan has been found to possess potent narcotic agonist and antagonist activity. These compounds are prepared by total synthesis and are not derived from opium alkaloids.

Abstract: A series of 5-endo-carbamoyloxy-N-[amino(lower)-alkyl]bicyclo[2.2.1]heptane-2,3-di-end o-carboxylic acid imides have been found to possess unique prophylactic and therapeutic activity as anti-arrhythmia agents. An example of such a compound possessing excellent activity is 5-endo-phenylcarbamoyloxy-N-(3-dimethylaminopropyl)bicyclo[2.2.1]heptane-2 ,3-diendo-carboxylic acid imide hydrochloride.

Abstract: 7-Aminocephalosporanic acid (7-ACA) and 7-amino-3-methyl-3-cephem-4-carboxylic acid (7-ADCA) are valuable intermediates in the preparation of semi-synthetic cephalosporins. These compounds are commonly prepared by cleaving the amide bond of compounds having the formula ##SPC1##In which R.sup.6 is H or ##EQU1## R is the side chain of a known penicillin, especially phenoxymethyl or benzyl, and the amino and carboxyl functions are blocked; byA. halogenating the blocked compounds Ia or IIa to produce an imino-halide;B. forming an imino-ether from the imino-halide by treatment with an alcohol; andC. mixing said imino-ether with water or an alcohol to produce 7-aminocephalosporanic acid or 7-amino-3-methyl-3-cephem-4-carboxylic acid.The invention claimed is the use of dicyclohexylamine or diisopropylamine instead of a tertiary amine acid scavenger in step A.

Abstract: Optionally substituted 1,2,3,5-tetrahydroimidazo[2,1-b]-quinazolin-2-ones and 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: Compounds having the formula ##SPC1##In which R is cyclopropyl or cyclobutyl have been designated 3-hydroxy-17-substituted-5,6-benzomorphinans. The compounds possess potent narcotic agonist and/or antagonist activity. In particular, the compounds 3-hydroxy-17-cyclopropylmethyl-5,6-benzomorphinan and 3-hydroxy-17-cyclobutylmethyl-5,6-benzomorphinan have been found to possess both activities. These compounds are prepared by total synthesis and are not derived from opium alkaloids.