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.
Type:
Grant
Filed:
July 21, 1980
Date of Patent:
October 12, 1982
Assignee:
Merrell Toraude et Compagnie
Inventors:
Philippe Bey, Fritz Gerhart, Viviane Van Dorsselaer
Abstract: 2-Amino-3-(3'-hydroxyphenyl)-3-butenoic acid or 2-amino-3-(3',4'-dihydroxyphenyl)-3-butenoic acid can be used to treat depression either alone or in combination with an extracerebrally acting AADC inhibitor.
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: There is described a method for treating benign prostatic hypertrophy comprising the administration of 2,5-di-amino-2-(mono-,di-, or trifluoromethyl)pentanoic acid or derivative thereof.
Abstract: A method for preventing gestation in mammals comprising the administration of a 2,5-diamino-2-halomethylpentanoic acid or derivative thereof.
Abstract: N-chlorophthalimide, N-chlorosuccinimide, and N-chloroglutarimide are prepared by contacting the corresponding imide with molecular chlorine under substantially non-aqueous conditions in an inert organic solvent in the presence of a poly(4-vinylpyridine)-divinylbenzene copolymer.
Abstract: Antibiotics of the formula ##STR1## wherein R is .alpha.-3,4-di-O-methylrhamnosyl, are produced by the cultivation of Streptomyces capreolus NRRL 11429 under submerged aerobic fermentation conditions. A crude antibiotic mixture is obtained from the fermentation medium by extraction. The compounds of Formula II, III, and IV are separated from coproduced Antibiotic A201A (See U.S. Pat. No. 3,843,784) and from each other by repetitive chromatography on silica gel.
Abstract: The tetradecapeptides of the formula ##STR1## wherein X is H--Ala--D--Ala, H--D--Ala--Gly, or H--D--Val--Gly; and X is Ala--Leu, Ala--Phe, Ala--D--Phe, D--Ala--Phe, or D--Ala--Cha; or the non-toxic, pharmaceutically acceptable acid addition salts thereof; inhibit secretion of growth hormone, while not materially inhibiting the secretion of insulin or glucagon. Intermediates used in the synthesis of the tetradecapeptides are also described.
Abstract: The tetradecapaptides of the formula ##STR1## wherein X is H-Ala-D-Ala, H-D-Ala-Gly, or H-D-Val-Gly, or the non-toxic, pharmaceutically acceptable acid addition salts thereof; inhibit the secretion of growth hormone, while not materially inhibiting the secretion of insulin or glucagon. Intermediates used in the synthesis of the tetradecapeptides are also described.
Abstract: Tetradecapeptides of the formula ##STR1## wherein X is H-Ala-D-Ala, H-D-Ala-Gly, or H-D-Val-Gly, and X.sup.1 is Phe or Cha, or a non-toxic pharmaceutically acceptable acid addition salt thereof, inhibit the secretion of growth hormone without materially inhibiting the secretion of glucagon or insulin. Intermediates and processes for making the tetradecapeptides are also described.
Abstract: Polypeptides of the formula ##STR1## wherein: R is hydrogen, lower alkanoyl, Ala-Gly-, Gly-Gly-Gly-, Ala-D-Ala- or p-Glu;AndX.sub.8 is L-Trp or D-Trp;Or the linear reduced form thereof; or a nontoxic acid addition salt thereof; are described. (D-Trp.sup.5)-Somatostatin and its analogues inhibit the release of growth hormone and insulin without materially affecting the secretion of glucagon, and are useful in the treatment of hyperinsulinemia and acromegaly.
Abstract: Prostaglandin compounds substituted at the 11-position, and possessing bronchodilating and hypotensive activity are prepared from PGA.sub.2 and its esters and 15-epimers.
Abstract: Compounds of the formula ##STR1## WHEREIN R is hydrogen (lower)alkyl, phen(lower)-alkyl, benzoyl(lower)alkyl, or p-halobenzoyl-(lower)alkyl; R.sup.1 is hydrogen or (lower)alkyl; R.sup.2 is hydrogen, (lower)alkyl, (lower)alkoxy, chlorine, fluorine, trifluoromethyl, or amino in the 7-, 8-, or 9-position; R.sup.3 is hydrogen, or (lower)alkyl; and R.sup.4 is hydrogen, (lower)-alkyl, (lower)alkoxy, chlorine, fluorine, or trifluoromethyl in the 7-, 8-, or 9-position; or the non-toxic acid addition salts thereof; exert a hyptotensive effect in hypertensive animals.
Abstract: Prostaglandin compounds substituted at the 11-position, and possessing broncho-dilating and hypotensive activity are prepared from PGA.sub.2 and its esters and 15-epimers.
Abstract: Prostaglandin compounds substituted at the 11-position, and possessing bronchodilating and hypotensive activity are prepared from PGA.sub.2 and its esters and 15-epimers.
Abstract: 9-Oxo-15-Substituted prostanoic acids, and intermediates for their preparation and for the preparation of other known prostaglandins are disclosed. The final products have bronchodilatory activity.
Abstract: Prolactin release is stimulated by parenteral administration of a pentapeptide of the formula:H-Tyr-Gly-Gly-Phe-Met-OH IorH-Tyr-Gly-Gly-Phe-Leu-OH IIor a non-toxic pharmacologically acceptable acid addition salt thereof.
Type:
Grant
Filed:
December 27, 1976
Date of Patent:
December 6, 1977
Assignee:
American Home Products Corporation
Inventors:
Harvey E. Alburn, Eric L. Lien, Norman H. Grant
Abstract: There is disclosed herein a process for relieving bronchial spasm and facilitating breathing in warm-blooded animals which comprises administering to a warm-blooded animal in need thereof an amount sufficient to relieve bronchial spasm and facilitate breathing in said warm-blooded animal of a prostanoic acid of the formula: ##STR1## wherein R is ethynyl, A is --CH.sub.2 --CH.sub.2 -- and B is --CH.sub.2 --CH.sub.2 --; R is ethynyl, A is --CH.sub.2 --CH.sub.2 --, and B is trans --CH=CH--; or R is ethynyl, A is cis --CH=CH--; and B is trans --CH=CH--; and R.sup.1 is hydrogen, alkyl of from 1 to about 6 carbon atoms, alkali metal, or a pharmacologically acceptable cation derived from ammonia or a basic amine.
Abstract: An aqueous vehicle containing about 80% polyethylene glycol 400 or polyethylene glycol 300 imparts long-acting growth hormone release inhibiting activity to somatostatin or linear somatostatin.
Abstract: The reaction of the periodate oxidation product from inosine, adenosine, or cytidine with methanol or ethanol affords a product having activity against lymphocytic leukemia P388 in mice.