Abstract: Compounds are provided which are crossreactive with peptides such as those which bind G-protein-linked receptors, together with preparative and therapeutic methods therefor. The compounds have the general structure: ##STR1## wherein at least one of R.sub.1, R.sub.2, R.sub.3, R.sub.4, or R.sub.5 comprises a functional group which is chemically similar to that found in the peptide of interest.

Abstract: Methods are provided for using 2-hydroxy-3-aminopropylsulfonamides to mimic peptides and to modulate the chemical and/or biological activity of enzymes, particularly proteolytic enzymes. Also provided are compositions comprising the sulfonamides in admixture with a pharmaceutically acceptable carrier, adjuvant, or vehicle.

Abstract: This invention relates to monomeric and polymeric pyrrolinone-based compounds, to the use of pyrrolinone-based compounds in place of amino acids in naturally-occurring or synthetic peptides, and to methods for preparing such compounds.

Abstract: The uricosuric and diuretic properties of indacrinone, [6,7-dichloro-2,3-dihydro-2-methyl-1-oxo-2-phenyl-1H-inden-5-yl)oxy]acetic acid, are carefully balanced for maximum therapeutic benefit by manipulation of the proportion of (+) and (-) enantiomers in the final product within critical limits.

Abstract: Fluorinated somatostatin analogs are prepared wherein a cyclic hexapeptide contains a secondary amino acid which replaces seven of the ring amino acids of somatostatin and the Lys side chain is monofluorinated in the .gamma. or .delta. positions. The cyclic hexapeptides are easier to synthesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting the release of gastric acid secretions. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These cyclic hexapeptides are prepared by the solid phase method.

Abstract: Improved process for preparing esters of .alpha.-methyl-3,4-dihydroxyphenylalanine having pharmaceutical activity via novel N-(tert-butoxycarbonyl) intermediates.

Abstract: 7-[3-(4-Acetyl-3-hydroxy-6-iodo-2-propylphenoxy)-2-hydroxypropoxy]-4-oxo-8- propyl-4H-1-benzopyran-2-carboxylic acid and its pharmaceutically acceptable salts are employed as antagonists of SRS-A (the slow reacting substance of anaphylaxis) in the treatment of asthma and allergic diseases.

Abstract: Somatostatin analogs having the structural formula: ##STR1## are prepared by controlled stepwise procedures starting with individual amino acid components. These peptides have the property of lowering blood glucose, inhibiting gastric secretion, inhibiting growth hormone release and inhibiting glucagon release in humans and animals.

Abstract: The isomer (R)-(-)-3-{[2-(p-hydroxyphenyl)-1-methylethyl]-aminomethyl}-3,4-dihydro-2H -1,5-benzodioxepin-3-ol and its non-toxic acid addition salts is unexpectedly more potent in the reduction of elevated interocular pressure in mammals than its enantiomorph or the racemate thereof.

Abstract: A novel tetrapeptide L-2-ketopiperidine-6-carbonyl-L-histidyl-L-thiazolidine-4-carbonyl-.beta.- alanin-amide, (L-Kpc-L-His-L-Tca-.beta.-ala-NH.sub.2), is a stimulant of the central nervous system. It is preparable by standard peptide synthetic procedures.

Abstract: The disclosed invention relates to .epsilon.-N-pyridyl-4-methyloxycarbonyllysine valuable in the synthesis of lysine containing peptides to the process of preparing this compound starting with 4-pyridyl-carbinol and succinimido-chloroformate and to the pyridyl-4-methyl-succinimidocarbonate intermediate in this process.

Abstract: Novel protecting groups for peptides containing a cysteine residue. Process for the synthesis of peptides containing a cysteine residue wherein the mercapto function of the cysteine residue is protected by an acetamidomethyl radical or other labile blocking group. Novel intermediates useful in peptide synthesis.

Abstract: The disclosed invention relates to .epsilon.-N-pyridyl-4-methyloxycarbonyllysine valuable in the synthesis of lysine containing peptides to the process of preparing this compound starting with 4-pyridylcarbinol and succinimido-chloroformate and to the pyridyl-4-methyl-succinimidocarbonate intermediate in this process.

Abstract: Hexa- and heptapeptides of formula W-[X-Pro-Phe-Phe-Y-Z].sub.n H prepared by standard synthetic peptide techniques are anti-inflammatory, anti-rheumatoid arthritic and anti-ulcer agents.

Abstract: A process for preparing peptides containing lysine wherein the terminal amino group of lysine is protected by a pyridyl-4-methyloxycarbonyl group during formation of the peptide and removing this group with zinc in acid.

Abstract: The invention disclosed herein relates to processes and intermediates useful in the preparation of certain 16-lower alkyl-1,4-pregnadiene compounds. It is particularly concerned with novel methods of preparing 16-lower alkyl-9.alpha.-fluoro-11.beta.,17.alpha.,21-trihydroxy-1,4-pregndiene-3,20 -dione and esters thereof, and with novel intermediates useful in these novel methods. It is further concerned with 16-lower alkyl-1,4,9(11)-pregnatriene-17.alpha.,21-diol-3,20-diones and their 21-lower alkanoates which, in addition to being valuable as intermediates, are valuable diuretic agents useful in the treatment of edema.