Abstract: Lower alkyl 2-oxo-4-phenyl-1-pyrrolidineacetic acid esters which are useful as pharmacological agents, especially cognition activators, are disclosed. They can be produced by reacting 4-phenyl-2-pyrrolidinone with a lower alkyl haloacetate in the presence of a strong base.

Abstract: N,N-dialkyl-3-[(phenylthio)methyl]-1H-indole-2-methanamines or 3-(1H-imidazol-1-ylmethyl)-N,N,-dimethyl-1H-indole-2-methanamines and acid addition salts thereof which are useful pharmacological agents, especially antifungals, are disclosed. The compounds can be produced by reacting a thiophenols or imidazoles with the appropriate 2-alkyl-1,2,3,4-tetrahydropyrrolo[3,4-b]indole.

Abstract: Pharmaceutical capsules with telescopically engaged body and cap portions, also known as hard shell capsules, having enteric properties. The capsule body and cap portions are formed by dip-molding using a homogeneous film-forming mixture comprising (1) hydroxypropyl methylcellulose and an ammonium salt of cellulose acetate phthalate polymer, or (2) gelatin and an ammonium salt of a copolymer of methacrylic acid and methacrylic acid alkyl ester; optionally with the inclusion of plasticizer and/or coloring agent. The capsules are soluble in or disintegrated by the alkaline intestinal secretions but are substantially insoluble or resistant to solution in the acid secretions of the stomach.

Abstract: Novel organic amide compounds which are N-[6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinyl]penicillin and cephalosporin type compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or cephalosporin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponding N-6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 6-aminopenicillanic acid, 7-aminocephalosporanic acid, 7-amino-3-methylceph-3-em-4-carboxylic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.

Abstract: Pyrrolo[1,2-a]indole compounds having in free base form the formulas ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are lower alkyl; R.sub.4 is lower alkyl, phenyl, lower alkoxy or ##STR2## in which R.sub.8 and R.sub.9 are hydrogen, lower alkyl, phenyl or benzyl; R.sub.5 is hydrogen or lower alkyl; A is O or NH; and R.sub.6 and R.sub.7 are lower alkyl, phenyl, or carbo(lower)alkoxy.

Abstract: Bis(2-[(disubstitutedamino)methyl]-1H-indole) compounds wherein said 2-[(disubstitutedamino)methyl]-1H-indol-3-ylmethylene moieties are linked together through a piperazine or 1,3-dihydro-2H-indol-2-one fragment and acid addition salts thereof which are useful pharmacological agents, especially antifungals, are disclosed. The compounds can be produced by reacting a piperazine or 1,3-dihydro-2H-indole-2-one compound with the appropriate quaternary salt of 2-alkyl-1,2,3,4-tetrahydropyrrolo-[3,4-b]indole.

Abstract: 3-Phenoxypyridine monosulfate, a pharmacological agent possessing mood elevating and cardiotonic properties. This compound is produced by reacting 3-phenoxypyridine with an equivalent amount of sulfuric acid.

Abstract: A new decapeptide having the formula, pGlu-His-Trp-Ser-Tyr-Gly-Leu-NO.sub.2 Arg-Pro-Gly(NH.sub.2); salts thereof; production thereof by reacting pGlu-His-Trp-Ser-Tyr(N.sub.3) with Gly-Leu-NO.sub.2 Arg-Pro-Gly(NH.sub.2), by reacting pGlu-His-Trp-Ser-Tyr-Gly(N.sub.3) with Leu-NO.sub.2 Arg-Pro-Gly(NH.sub.2), or by reacting pGlu-His-Trp-Ser-Tyr-Gly-Leu(N.sub.3) with NO.sub.2 Arg-Pro-Gly(NH.sub.2); certain peptide intermediates and their salts used in the production thereof; and the use thereof in the preparation of luteinizing hormone releasing factor.

Abstract: A process is provided for the production of 2,2-dimethyl-5-(2,5-xylyloxy)valeric acid which comprises subjecting 2,2-dimethyl-5-(2,5-xylyloxy)valeraldehyde to oxidation with elemental oxygen in a three-phase reaction mixture comprising a water immiscible organic solvent for said valeraldehyde, an aqueous alkaline solution, and a noble metal catalyst.

Abstract: New nonapeptides having the formula R-Trp-Ser(benzyl)-Tyr(benzyl)-D-Phe-Leu-Arg(X)-Pro-Gly-Y wherein X is a protective group, R is pGlu, protected His(benzyl), protected Ser(benzyl) or protected Cys(benzyl), and Y is lower alkoxy, amino, lower alkylamino or di(lower alkyl)amino.

Abstract: Process for the production of an ester product, 9-(.beta.-D-arabinofuranosyl)adenine, 5'-phosphate, in which the mixture resulting from reaction of 9-(.beta.-D-arabinofuranosyl)adenine with phosphorylating agent in trialkyl phosphate solvent is subjected to aqueous hydrolysis, the pH of the hydrolysis mixture is adjusted upward sufficiently to cause separation into aqueous and non-aqueous liquid phases, the trialkyl phosphate solvent is removed, and the product is precipitated from the residual aqueous mixture and isolated.

Abstract: 2-Amino-1-(5-amino-1H-imidazol-4-yl)ethanone, 6,7-dihydroimidazo[4,5-d][1,3]diazepin-8(3H)-one and acid-addition salts thereof are disclosed. 2-Amino-1-(5-amino-1H-imidazol-4-yl)ethanone and its acid-addition salts are prepared by catalytically reducing an acid-addition salt of 2-amino-1-[5-amino-1-(protected)-1H-imidazol-4-yl]ethanone. 6,7-Dihydroimidazo[4,5-d][1,3]-diazepin-8(3H)-one and its acid-addition salts are prepared by reacting an acid-addition salt of 2-amino-1-(5-amino-1H-imidazol-4-yl)ethanone with a compound able to contribute a formyl group. The later product may subsequently be converted into (R)-3-(2-deoxy-.beta.-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo[ 4,5-d][1,3]diazepin-8-ol. Furanose derivatives of 6,7-dihydroimidazo[4,5-d][1,3]diazepine are also disclosed and their methods of preparation. Lastly, a method for resolving an isomer mixture of 3-(2-deoxy-.beta.-D-erythro-pentafuranosyl)-3,6,7,8-tetrahydroimidazo[4 ,5-d][1,3]diazepin-8-ol compounds is related.

Abstract: New octapeptides having the formula Prot Grp-R-Trp-Ser-Tyr-R.sub.2 -Leu-Arg-Pro-R.sub.3 ; salts thereof; wherein R is Gln, Gln (bzl), His (bzl), Ser (bzl), Pro, Leu, Tyr (bzl), Ile, Cys (bzl) or Phe, R.sub.2 is D-Phe, D-Ala, D-Leu, D-Trp, D-Tyr, D-Tyr (Me), D-Ser, D-Met, D-Arg, D-Val, D-His, D-Gln, D-Phs, D-Thr, D-Pro, D-Me.sub.5 Phe or D-Asn and R.sub.3 is NH.sub.2, NH(lower alkyl), N-(lower alkyl).sub.2, NH-benzyl, NHCH.sub.2 CH.sub.2 N-(lower alkyl).sub.2 or NH-CH.sub.2 CH.sub.2 SO.sub.2 NH-benzyl; methods for their production; certain peptide intermediates and their salts used in the production thereof; and the use of said octapeptides as luteinizing hormone releasing factor antagonists.

Abstract: 3-(Thienyloxy)pyridines and acid-addition salts thereof, which are useful as pharmacological agents, especially in the area of psychostimulants, are disclosed. These compounds can be produced by reacting a halothiophene with a metallic salt of 3-hydroxypyridine.

Abstract: (+,-)-cis-.alpha.[3-(2,6-Dimethyl-1-piperidinyl)propyl]-.alpha.-phenyl-2-py ridinemethanol and acid-addition salts. The compounds are pharmacological agents, especially antiarrhythmic agents. The compounds can be produced by reacting pyridyllithium with cis-.gamma.-(2,6-dimethylpiperidino)butyrophenone, or by reacting cis-1-(3-lithiopropyl)-2,6-dimethylpiperidine with 2-benzoylpyridine. Pharmaceutical compositions comprising (+,-)-cis-.alpha.-[3-(2,6-dimethyl-1-piperidinyl)propyl]-.alpha.-phenyl-2- pyridinemethanol and acid-addition salts thereof and methods for treating cardiac arrhythmia using said pharmaceutical compositions are also disclosed.

Abstract: 4-Aryl-1,6-dihydro-1,3,8-trimethylimidazo[1,2-a]-pyrazolo[4,3-f][1,4]diazep ines; and acid-addition salts. The aryl group is o-fluorophenyl or o-chlorophenyl. The compounds are pharmacological agents, especially anticonvulsant and antianxiety agents. They can be produced by reacting an aryl-(2-hydroxymethyl)-imidazol-1-yl-1,3-dimethylpyrazol-4-ylmethanone hydrocarbon sulfonate ester with ammonia in the presence of iodide.

Abstract: Novel organic amide compounds which are N-[6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinyl]penicillin and cephalosporin type compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or cephalosporin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponing N-6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 6-aminopenicillanic acid, 7-aminocephalosporanic acid, 7-amino-3-methylceph-3-em-4-carboxylic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.

Abstract: New octapeptides having the formula X-R.sup.1 -Trp-Ser(benzyl)-Tyr(benzyl)-R.sup.2 -Leu-Arg(R)-Pro-R.sup.3 -Y wherein X is a protective group, R is hydrogen or a protective group, R.sup.1 is a single bond, Gln, D-Leu or D-Val, R.sup.2 is D-Phe or D-Ala, R.sup.3 is a single bond or Gly and Y is lower alkoxy, amino, lower alkylamino or di(lower alkyl)amino.

Abstract: New nonapeptides having the formula R-Gln-Trp-Ser-Tyr-Trp-Pro-Pro-Tyr(benzyl)-Ser(benzyl)-Y wherein R is a protective group and Y is amino, lower alkylamino or di(lower alkyl)amino.

Abstract: New octapeptides having the formula X-R-Pro-His(benzyl)-His(benzyl)-R.sup.1 -Trp-D-Ala-Y wherein X is a protective group, R is Pro or Gln; R.sup.1 is Tyr(benzyl)-Ser(benzyl) or Ser(benzyl)-Pro and Y is lower alkoxy, amino, lower alkylamino or di(lower alkyl)amino.