Abstract: Aerosol formulations substantially free of chlorofluorocarbons, for oral and/or nasal administration, are described. The formulations comprise 1,1,1,2-tetrafluoroethane, a medicament, optionally an excipient and optionally a surfactant. Methods of treatment using the formulations also are described.

Abstract: Aerosol formulations substantially free of chlorofluorocarbons, for oral and/or nasal administration are described. The formulations comprise 1,1,1,2 tetrafluoroethane, a medicament, optionally an excipient and optionally a surfactant. Methods of treatment utilizing the formulations also are described.

Abstract: A method of reducing cravings in a mammal to nicotine or tobacco is disclosed. The method comprises administering to the mammal an effective amount of a D1/D5 antagonist or a D1/D5 partial agonist alone or in combination with other specified CNS compounds.

Abstract: A dermatologically compatible substantive oil-in-water sunscreen composition is disclosed comprising a block polymer substantive agent and a sunscreening agent. The composition is adaptable for dispensing by a spray means.

Abstract: Process for preparing a key intermediate, 2-methyl-3-trifluoromethylaniline (MTA) of Flunixin, as well as novel intermediates thereof are described.

Abstract: There is disclosed a method for treating advanced cancer in patients in need of such treating. Temozolomide and cisplatin are administered in combination in amounts sufficient to achieve a clinical response.

Abstract: A novel process for the preparation of .alpha.-substituted arylacetamides wherein the substituent is an aromatic group or a 1-alkenyl or 1-cycloalkenyl group and wherein the nitrogen atom carries no hydrogen atoms comprises the reaction of an arylacetamide having one or two hydrogen atoms on the .alpha.-carbon atom, wherein the nitrogen atom carries no hydrogen atoms, with a strong base in an inert aprotic organic solvent, followed by reaction with a zerovalent transition metal catalyst and then with a compound of the formula R.sup.4 --X, wherein R.sup.4 is selected from aromatic groups, 1-alkenyl groups and 1-cycloalkenyl groups and X is a particular leaving group, especially a triflate group. The .alpha.-substituted arylacetamides are useful as intermediates in the preparation (by reduction) of .alpha.-substituted arylethylamines, e.g., 1-substituted-2,3,4,5-tetrahydro-1H-3-benzazepines, having pharmacological activity. Certain benzazepines wherein the 1-substituent R.sup.4 is 1-(1-cycloalkenyl) are novel.

Abstract: Novel steroids having a 9.alpha.-hydroxy or a 9.alpha.-carbonate substituent can be prepared from 9.alpha.-hydroxyandrostenedione and can be utilized in the synthesis of commercially valuable corticosteroids such as betamethasone. The 9.alpha.-carbonates are prepared by reaction of the corresponding 9.alpha.-hydroxy steroid with a sequence of excess base, trialkylsilyl chloride, alkyl haloformate and alkanol or by using excess base, alkyl haloformate and alkoxide. 9.alpha.-Carbonate-17-keto compounds can be treated with lithium acetylide and a lithium salt to afford the corresponding 17.alpha.-ethynyl-17.beta.-hydroxy-9.alpha.-carbonate. This compound is then esterified with a novel series of reagents to give the 17-ester which can be reduced the corresponding 17-allene. Oxidation of this allene to the bis-epoxide compound, followed by treatment with an alkali metal salt of a carboxylic acid under phase transfer conditions gives the 17.alpha.-hydroxy 21-ester 9.alpha.-carbonate. Elimination of the 9.alpha.

Abstract: A method for treating CNS disorders and/or improving cognitive ability in a mammal utilizing 2-phenyl-1,3-propanediol monocarbamate is disclosed. Also disclosed are formulations and methods for manufacturing this compound.

Abstract: Process for preparing a key intermediate, 2-methyl-3-trifluoromethylaniline (MTA) of Flunixin, as well as novel intermediates thereof are described.

Abstract: Aerosol formulations substantially free of chlorofluorocarbons for oral and/or nasal administration are described. The formulations comprise 1,1,1,2,3,3,3-heptafluoropropane, a medicament, optionally an excipient and optionally a surfactant. Methods of treatment utilizing the formulations are also described.

Abstract: A method for treating onychomycosis without drilling a hole in a nail plate or without daily scraping of the nail, comprising topically administering to the afflicted nail of a mammali) a medicated device comprising salicylic acid or a salt, ester or mixture thereof in a plaster preparation, wherein said plaster preparation is attached to a carrier and the salicylic acid is present in the plaster preparation in an amount ranging from about 10 to about 80 percent (%) by weight of the plaster preparation; orii) a liquid preparation comprising salicylic acid or a salt, ester or mixture thereof in a film-forming liquid vehicle, and the salicylic acid is present in the liquid preparation in an amount ranging from about 6 to about 35% by weight of the liquid preparation.

Abstract: An improved process for converting gentamicin B to isepamicin comprising forming 3,6'-di-N-formylgentamicin B, acylating the 1-amino group with an N-protected (S)-isoserine compound and removing all the blocking groups under conditions which result in high yields of isepamicin. A novel formylating agent, 2-formylmercaptobenzothiazole, and intermediate compounds are also disclosed.

Abstract: A process for preparing an hydroxyketone of the formula (X): ##STR1## wherein Ar represents substituted phenyl, aromatic heterocyclic, or substituted aromatic heterocyclic; R.sup.1 and R.sup.2 independently represents hydrogen, C-1 to C-16 alkyl, aromatic, substituted aromatic, aromatic heterocyclic, substituted aromatic heterocyclic or C-1 to C-5 alkyl covalently bonded to Ar, with the provision that R.sup.1 and R.sup.2 are different. The process comprises contacting a compound of the formula (V): ##STR2## with a solvent, a base and a chiral hydroxylating agent at a temperature of about -85.degree. C. or less.Compounds of the formulae ##STR3## also are disclosed.

Abstract: Bis-benzo cyclohepta piperidine, piperidylidene and piperazine compounds of the general formula, ##STR1## and pharmaceutically acceptable salts thereof are disclosed, which possess anti-allergic and/or anti-inflammatory activity. Methods for preparing and using the compounds are also described.

Abstract: Novel benzazepines of the formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R represents H, alkyl, allyl or ##STR2## A represents --[CR.sup.1 R.sup.2].sub.n --; n represents 3 or 4; R.sup.1 and R.sup.2 may be the same or different and each independently represents H, OH, atkyl, alkoxy, phnenyl or substituted phenyl, with the proviso that R.sup.1 and R.sup.2 on the same carbon atom are not both OH, or R.sup.1 and R.sup.2 on the same carbon atom together represent=O;G represents H, R.sup.3 (CO)-- or ArNHCO--;R.sup.3 represents H, alkyl, alkoxy, phenyl or substituted phenyl;Ar represents phenyl or substituted phenyl; andY and Z may be the same or different and each is independently selected from H, halo, alkyl, alkoxy or halpalkyl;the pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, useful in the treatment of psychoses, drug dependence, D1 dependent neurological disorder or pain are disclosed.

Abstract: Disclosed are fused benzazepine compounds, pharmaceutical compositions including such compounds, methods of using such compounds, for example, in the treatment of psychoses and/or depression, and intermediates useful in the preparation of such compounds.

Abstract: A process for preparing an (S,S) or (R,R) diastereoisomer of the formula: ##STR1## or salts, esters or amides thereof, wherein R.sup.3 and R.sup.4 independently represent hydrogen, alkyl, aryl or aryl substituted with halogen, alkyl, nitro or alkoxy, and n and m independently represent integers from one to six, comprising combining a cyanide compound of the formula:M.sup.1 C.tbd.N (III)wherein M.sup.1 is hydrogen, trimethylsilyl or a metal, with an optional proton source, a solvent and a Lewis acid of the formula:M.sup.2 X.sub.4, AlCl.sub.3 or BF.sub.3 (IV)wherein M.sup.2 is Sn or Ti and X represents chloro, bromo, fluoro or iodo, with an .alpha.-amino acid compound or salts or esters thereof, followed by addition of an acyl or acetal compound to give the diastereoisomer of formula (X).

Abstract: A process for the decomposition of trichloroacetic acid (TCAA) to form chlorides, carbonates and formates is disclosed. The process comprises treating TCAA with 6 or more equivalents of a metal hydroxide at a temperature above 60.degree. C.

Abstract: The preparation of arylethanolamines, and in particular albuterol (salbutamol), together with their novel boron, acetal and hemi-acetal intermediates is described.