Abstract: Sustained release formulations for the anorectic agent, diethylpropion hydrochloride, are disclosed which are suitable for use in capsules.

Abstract: A process for preparing 16.alpha.-hydroxy-17.alpha.-aminopregnane derivatives through the opening of the corresponding 16.alpha., 17.alpha.-epoxides with amines.The use of the thus obtained compounds as intermediates in the synthesis of pharmacologically active pregnano-[17.alpha.,16.alpha.-d]oxazolines is also claimed.

Abstract: 3H-naphth[1,2-d]imidazole derivatives of formula ##STR1## wherein R stands for hydrogen, methyl or ethyl, R.sub.1 represents hydrogen, methyl or ethyl, R.sub.2 represents hydrogen, methyl, ethyl, phenyl or substituted phenyl, the symbol R.sub.3 stands for a phenyl radical optionally substituted and R.sub.4 and R.sub.5, each independently, may represent hydrogen, halogen, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)alkoxy or halo-(C.sub.1 -C.sub.4)alkoxy, are described. Also described is the process for preparing the novel compounds, their use as antiinflammatory agents and the pharmaceutical compositions containing them.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is H or NH.sub.2 ; R.sub.2 is C.sub.1-6 straight or branched chain alkyl; --CH.sub.2 OH; --(CH.sub.2).sub.n --O--(CH.sub.2).sub.m --CH.sub.3 ; phenyl; or --(CH.sub.2).sub.p NH.sub.2 ;n is 1-3;m is 0-3; andp is 1-5;and the pharmaceutically acceptable acid addition salts of those compounds of basic character,have antisecretory activity.

Abstract: Certain .alpha.-(fluoromethyl or difluoromethyl)-.alpha.-aminoacetonitriles are prepared by treating the appropriate .alpha.-(fluoromethyl or difluoromethyl) ketimine magnesium halide with hydrogen cyanide or with an alkali metal cyanide or ammonium cyanide and a proton source. The products are useful as intermediates for making .alpha.-(fluoromethyl or difluoromethyl)-.alpha.-amino acids having pharmacological activity.

Abstract: 1,7-Dihydro-pyrrolo[3,4-e][1,4]diazepin-2(1H)-ones of the formula ##STR1## wherein R is lower alkyl, R.sub.1 stands for hydrogen, methyl, ethyl or phenyl, R.sub.2 is hydrogen or lower alkyl and R.sub.3 is hydrogen, chloro, fluoro, bromo, trifluoromethyl or methoxy are described with anticonvulsant and anti-anxiety activity.Also described is the process for preparing the above compounds and pharmaceutical preparations containing them.

Abstract: Compounds of the formula ##STR1## wherein R is H, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, 3,4-methylenedioxy, CF.sub.3, NO.sub.2, NH.sub.2, N(C.sub.1-4 alkyl).sub.2, CN, OH, --S(C.sub.1-4 alkyl) or --SO.sub.2 (C.sub.1-4 alkyl); R.sub.1 and R.sub.2 are independently each H or C.sub.1-4 alkyl or taken together with the attached N atom are morpholino, piperidino, pyrrolidino, piperazino, or N-- C.sub.1-4 -alkyl piperazino; and, when R is halo, C.sub.1-4 alkyl or C.sub.1-4 alkoxy, x is 0-3 and, otherwise, is 0 or 1;or a pharmaceutically acceptable salt thereof with an acid or for the compounds wherein R.sub.1 and R.sub.2 are both not H, a quaternary ammonium salt thereof with a C.sub.1-4 alkyl halidehave valuable antiviral activity, e.g., for treatment of infections caused by a herpes virus.

Abstract: .alpha.-Substituted amines and .alpha.-substituted-.alpha.-amino acids are described which are useful in inhibiting the growth of protozoa in animals.

Abstract: A new class of pyrrolo-diazepines with anticonvulsant and anti-anxiety activity of the general formula ##STR1## wherein R is (C.sub.1 -C.sub.4)alkyl, R.sub.1 is chloro, bromo or nitro, R.sub.2 is hydrogen or (C.sub.1 -C.sub.4)alkyl and R.sub.3 is hydrogen, chloro, bromo, fluoro, trifluoromethyl or methoxy. The new compounds are prepared starting from the corresponding compounds wherein R.sub.1 is hydrogen through halogenation or nitration. Pharmaceutical preparations containing the new compounds of formula I are also described.

Abstract: Novel halomethyl derivatives of amino acids of the following general structure ##STR1## wherein Y is FCH.sub.2 --, F.sub.2 CH.sub.2 --, F.sub.3 C--, ClCH.sub.2 -- or Cl.sub.2 CH--; R.sub.1 is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.11 R.sub.12 wherein each of R.sub.11 and R.sub.12 is hydrogen or a straight or branched lower alkyl group of from 1 to 4 carbon atoms, ##STR2## wherein R.sub.5 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.2 is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched or ##STR3## wherein R.sub.6 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; each of R.sub.3 and R.sub.

Abstract: The present invention refers to a new process for preparing N-2,3,4,5-substituted-1H-pyrrol-1-yl)-6-substituted amino-3-pyridazineamine, known as antihypertensive agents. The process is characterized in that a suitable 3,6-dihalogenopyridazine is reacted with hydrazine hydrate or other hydrazine derivatives of formula NH.sub.2 NHR, the obtained compound is reacted with a suitable dicarbonyl compound yielding first an alcandione-bis-[6-halogen-3-pyridazininyl]hydrazone, and then a 6-halogen-3-pyrrolylpyridazineamine derivative which is in turn reacted with an amine to yield the desired compounds.

Abstract: 1-[(2-Mercaptocycloalkyl)carbonyl]-L-proline derivatives of the formula ##STR1## wherein R, R.sup.1, and R.sup.2, each independently, represent hydrogen or a (C.sub.1 -C.sub.4)alkyl radical, n represents the integer 1, 2, 3, 4, or 5, and, in each of the n (CR'.sub.2) groups, R' represents hydrogen or (C.sub.1 -C.sub.4)alkyl, are described as well as the process for their manufacture, the intermediates for their synthesis and their use as antihypertensive agents.

Abstract: The use of lofexidine and its pharmaceutically acceptable salts in alleviating the adverse symptoms of drug withdrawal is disclosed.

Abstract: Beta-monofluoromethyl beta-alanine, beta-difluoromethyl beta-alanine and pharmaceutically acceptable esters and amides derived from the acid group, amides derived from the amine group, and salts thereof are novel compounds which inhibit .gamma.-aminobutyric acid transaminase (GABA-T).

Abstract: Novel compounds of the following general Formula I are useful pharmacological agents: ##STR1## wherein: Ado represents 5'-deoxyadenosin-5'-yl;R.sub.1 represents methyl, ethyl or, preferably hydrogen;R.sub.2 represents C.sub.1 -C.sub.8 alkylene;R.sub.4 represents C.sub.1 -C.sub.8 alkylene;R.sub.5 represents hydrogen, C.sub.1 -C.sub.6 alkyl or --R.sub.6 NHR.sub.7 ;R.sub.6 represents C.sub.1 -C.sub.4 alkylene; andR.sub.7 represents hydrogen or C.sub.1 -C.sub.6 alkyl;and pharmaceutically acceptable acid addition salts thereof.

Abstract: Fluorinated alkenylamines of the Formula V ##STR1## wherein n represents 0, 1, 2 or 3; R.sub.1 represents hydrogen or C.sub.1 -C.sub.10 alkyl and Y represents (a), when n represents O, CH.sub.2 F, (b), when n represents 1, CH.sub.2 F or CHF.sub.2, or (c) when n represents 2 or 3, CH.sub.2 F, CHF.sub.2 or CF.sub.3 are novel process intermediates. They are obtained by hydrolysis and subsequent reduction of the corresponding alkenyl fluorinated methyl ketimine magnesium halides, which are novel compounds resulting from reaction of the corresponding alkenyl magnesium halides with the corresponding fluorinated acetonitriles. The fluorinated alkenylamines of Formula V are oxidized while the amino group is protected to provide, after removal of the amine protecting group, the corresponding fluorinated methyl aminoalkanoic acids which are useful pharmacological or anti-bacterial agents.

Abstract: A method of reducing local hemorrhage and tissue necrosis resulting from the bite or sting of a venomous animal whereby an envenomated mammal is treated with a compound of the formula: ##STR1## or a corresponding disulfide wherein n is 1, 2 or 3; Z is O, S or NH; R is H, a straight or branched chain lower alkyl group of from 1 to 4 carbon atoms, hydroxy, a straight or branched chain lower alkoxy group of from 1 to 4 carbon atoms, fluoro, chloro, bromo, iodo or trifluoromethyl; or a pharmaceutically acceptable salt thereof.

Abstract: 2-Amino-2-fluoromethyl-3-(substituted)phenyl propionic acids and derivatives thereof are coadministered with dopamine for the treatment of schizophrenia, mania, tardive dyskinesia, anxiety, or depression.

Abstract: Novel analgesic and antipsychotic agents having the formula ##STR1## wherein Q is ##STR2## in which R.sub.1 is hydrogen, hydroxy or halogen and R.sub.4 is hydrogen or, R.sub.1 and R.sub.4 are both hydroxy; Z is hydrogen or straight chain lower alkyl having from 1 to 4 carbon atoms and X is methylene, carbonyl, hydroxymethylene, thio, sulfinyl or sulfonyl, or Z and X, taken together, are methylidenyl, with the proviso that when X is sulfonyl or sulfinyl, Z is other than hydrogen; R.sub.5 is hydrogen or halogen, and R.sub.2 is H, a straight or branched lower alkyl group having from 1 to 4 carbon atoms, the group ##STR3## or the group ##STR4## wherein R.sub.3 is hydroxy, amino, alkylamino or dialkylamino wherein the alkyl moiety is straight or branched and has from 1 to 4 carbon atoms, diastereomers, enantiomers and pharmaceutically acceptable salts thereof.

Abstract: .alpha.-Substituted amines and .alpha.-substituted-.alpha.-amino acids are described which are useful in controlling the growth of algae.