Abstract: An improved process for the preparation of substituted isoxazolo[4,5-c]pyridin-4(5H)-ones which are either useful as intermediates in the preparation of compounds having pharmaceutical activity or as hypolipidemic agents which comprises cyclizing a corresponding 5-(2-amino-2-phenyl- or substituted phenyl-ethenyl)-3-substituted-N-alkyl isoxazole-4-carboxamide under acidic conditions.
Abstract: Alpha-cyano-o-anisidino derivatives, e.g., alpha-cyano-o-acetanisidide, are useful as hypolipidemic agents. The compounds are obtainable by reacting an appropriate 2-amidophenol with a haloalkylnitrile.
Abstract: This disclosure describes compounds of the formula ##STR1## where R.sub.1 is straight chain alkyl, andR.sub.2 is hydrogen, halo having an atomic weight of about 19 to 36, lower alkoxy or trifluoromethyl,Which are useful as minor tranquilizers and sleep inducers.
Abstract: Substituted spiro[isoindoline-1,3'(4'H)-isoquinoline]-1',3-diones, e.g., 2,2'-dimethyl spiro[isoindoline-1,3'(4'H)-isoquinoline]-1',3-dione, are prepared by cyclizing .alpha.-(1-hydroxy-3-oxoisoindolin-1-yl)-o-toluamides and are useful as non-estrogenic anti-fertility agents.
Abstract: Substituted hydroxy pyridones, e.g., 3-(.alpha.-iminobenzyl)-4-hydroxy-6-phenyl-1-methyl-2(1H)-pyridone, are prepared by reducing corresponding isoxazolo[4,5-c]pyridin-4(5H)-ones and are useful as minor tranquilizers and sleep inducers.
Abstract: Disclosed are compounds of the class 1-phenyl-2,3-butadien-1-ol e.g. 2-(p-biphenyl)-3,4-pentadien-2-ol, which are useful by reason of their pharmacological activity in animals, e.g., as anti-inflammatory agents and tranquilizers. Said compounds can be prepared, e.g., by reduction of a corresponding 4-substituted-1-phenyl-2-butyne-1-ol with a complex hydride such as lithium aluminum hydride.
Abstract: Imidazo[2,1-a]isoquinolines useful as anorexics and anti-depressants, e.g. 5-(2-thienyl)-2,3,5,6-tetrahydroimidazo[2,1-a]isoquinolin-5-ol, are prepared from a dilithium derivative of a 2-(o-tolyl)-2-imidazoline.
Abstract: Phenoxyphenyl pyridyl carbinols and ketones, e.g., p-phenoxyphenyl-nicotinyl ketone, are useful as pharmaceutical agents. The ketones are obtainable by oxidation of corresponding phenoxyphenyl pyridyl carbinols.
Abstract: 2,4-Disubstituted-4b,5,6,7,8,8a,9,10-octahydro-9-oxo-phenanthrenes e.g., 2,4-dimethoxy-4b,5,6,7,8,8a,9,10-octahydro-9-oxo-phenanthrene are useful as hypolipidemic agents.
Abstract: Compounds of the formula ##STR1## WHEREIN R.sub.1 is hydrogen, alkyl of 1 to 6 carbon atoms or amino, R.sub.2 is hydrogen or alkyl of 1 to 6 carbon atoms, with the provisos that (1) at least one of R.sub.1 and R.sub.2 is not a tertiary alkyl group and (2) R.sub.2 is hydrogen when R.sub.1 is amino, orR.sub.1 and R.sub.2 taken together and with the nitrogen atom to which they are joined are pyrrolidino, piperidino or N'-2-hydroxyethylpiperazino,Each X' is independently alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or halo, or two X's on adjacent carbon atoms together are methylenedioxy, andn is 0, 1, 2 or 3,And the pharmaceutically acceptable acid addition salts thereof,Are useful as anti-obesity and anti-diabetic agents. The compounds wherein R.sub.1 is alkyl and R.sub.2 is hydrogen are synthesized by a two-step synthesis from 2-alkyl-5-arylisoxazolium salts and ethylenediamine. The compounds wherein R.sub.1 and R.sub.
Abstract: Pesticidal compositions useful in agriculture but subject to rapid degradation on exposure to sunlight are stabilized by including in the formulation an amount of a sulfonated copolymer of catechin and leucocyanidin having a molecular weight in the range of about 3000 to 6000, or of an agronomically acceptable metal or ammonium salt thereof, in an amount sufficient to provide a concentration of about 1/4 lb. to 5 lbs. per acre.
Abstract: Free flowing, rapid dissolving, effervescent granules in particular, potassium chloride granules, are prepared by granulating an alkali metal carbonate and/or bicarbonate and active ingredient with water containing a surfactant, such as polyethylene glycol 1540, and after drying mixing with a pharmaceutically acceptable organic acid plus additives.
Abstract: The compounds are 1-aryl-1-alknyl-1-(t-butyl)-substituted methanols, e.g. 3-(2'-naphthyl)-4,4-dimethyl-pent-1-yn-3-ol, are useful as hypolipidemic agents, and are prepared by reacting a 4-aryl-pivalophenone with a metallo-alkynyl reagent under Grignard reaction conditions.
Abstract: Controlled gastric residence time medicament formulations, e.g., tablets and/or capsules, containing polymeric film coatings are exposed to a volatile amine, e.g., anhydrous ammonia, methyl amine, or ethyl amine, to provide improved medicament formulations, which by virtue of mechanical or surface effects including expansion or swelling of the coating in gastric fluids are capable of prolonged, e.g., up to twelve hours, residence in the gastric area.
Abstract: Substituted or unsubstituted isoxazolyl benzamides, e.g., o-(3-phenylisoxazol-5-yl)-N-methylbenzamide, are prepared by cyclizing a corresponding 1-hydroxy-1-[substituted or unsubstituted -.beta.-(hydroxyimino)phenethyl]-2-alkyl phthalimidine with a strong acid and are useful as minor tranquilizers, muscle relaxants, and sleep inducers.
Abstract: This disclosure describes novel compounds of the formula ##STR1## where R.sub.1 is straight chain lower alkyl, andR.sub.2 and R.sub.3 independently represent hydrogen or lower alkyl or together with N represent ##STR2## where X is CH.sub.2, O or N--CH.sub.3, andR.sub.4 is hydrogen, halo having an atomic weight of about 19 to 36 or lower alkoxy which are useful as hypolipidemic agents.
Abstract: Hypolipidemic agents of the formula: ##STR1## wherein X is C.dbd.O or CHOH,R.degree. is branched lower alkyl,R is hydrogen, alkyl, or halo,n is 1 or 2, andR' and R" are hydrogen, halo, alkyl or alkoxy, e.g., 4-phenoxy-pivalophenone.
Abstract: Pivaloyl benzyl ureas, e.g., 1,1-bis(4-pivaloylbenzyl)-3-methyl urea, are prepared by reacting a corresponding 4",4'"-iminodimethylene-di-tert. alkylophenones with an alkyl isocyanate, and are useful as hypolipidemic agents.