Patents Represented by Attorney David E. Frankhouser
  • Patent number: 4353828
    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
  • Patent number: 4346110
    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.
    Type: Grant
    Filed: June 1, 1981
    Date of Patent: August 24, 1982
    Assignee: Merrell Toraude et Compagnie
    Inventors: Michael G. Palfreyman, Ian A. McDonald
  • Patent number: 4342780
    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.
    Type: Grant
    Filed: February 17, 1981
    Date of Patent: August 3, 1982
    Assignee: Merrell-Toraude et Cie
    Inventors: Philippe Bey, Michel Jung
  • Patent number: 4330559
    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.
    Type: Grant
    Filed: February 3, 1981
    Date of Patent: May 18, 1982
    Assignee: Merrell-Toraude et Cie
    Inventors: Philippe Bey, Michel Jung
  • Patent number: 4309442
    Abstract: A method for preventing gestation in mammals comprising the administration of a 2,5-diamino-2-halomethylpentanoic acid or derivative thereof.
    Type: Grant
    Filed: December 3, 1980
    Date of Patent: January 5, 1982
    Assignee: Merrell Toraude et Compagnie
    Inventors: Philippe Bey, Michel Jung
  • Patent number: 4212977
    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.
    Type: Grant
    Filed: December 20, 1978
    Date of Patent: July 15, 1980
    Assignee: Eli Lilly and Company
    Inventor: Ta-Sen Chou
  • Patent number: 4205164
    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.
    Type: Grant
    Filed: March 2, 1979
    Date of Patent: May 27, 1980
    Assignee: Eli Lilly and Company
    Inventor: Herbert A. Kirst
  • Patent number: 4202802
    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.
    Type: Grant
    Filed: October 2, 1978
    Date of Patent: May 13, 1980
    Assignee: Eli Lilly and Company
    Inventor: James E. Shields
  • Patent number: 4199500
    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.
    Type: Grant
    Filed: November 20, 1978
    Date of Patent: April 22, 1980
    Assignee: Eli Lilly and Company
    Inventor: James E. Shields
  • Patent number: 4199501
    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.
    Type: Grant
    Filed: November 20, 1978
    Date of Patent: April 22, 1980
    Assignee: Eli Lilly and Company
    Inventor: James E. Shields
  • Patent number: 4100153
    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.
    Type: Grant
    Filed: May 11, 1977
    Date of Patent: July 11, 1978
    Assignee: American Home Products Corporation
    Inventor: Victor M. Garsky
  • Patent number: 4097514
    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.
    Type: Grant
    Filed: August 2, 1974
    Date of Patent: June 27, 1978
    Assignee: American Home Products Corporation
    Inventors: Donald P. Strike, Wen-Ling Kao
  • Patent number: 4089958
    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.
    Type: Grant
    Filed: December 20, 1976
    Date of Patent: May 16, 1978
    Assignee: American Home Products Corporation
    Inventors: Meier E. Freed, John R. Potoski
  • Patent number: 4076730
    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.
    Type: Grant
    Filed: August 2, 1974
    Date of Patent: February 28, 1978
    Assignee: American Home Products Corporation
    Inventor: Donald P. Strike
  • Patent number: 4067898
    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.
    Type: Grant
    Filed: June 11, 1976
    Date of Patent: January 10, 1978
    Assignee: American Home Products Corporation
    Inventors: Donald P. Strike, Wen-Ling Kao
  • Patent number: 4065494
    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.
    Type: Grant
    Filed: April 19, 1976
    Date of Patent: December 27, 1977
    Assignee: American Home Products Corporation
    Inventor: Donald Peter Strike
  • Patent number: 4061737
    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
  • Patent number: 4059701
    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.
    Type: Grant
    Filed: April 19, 1976
    Date of Patent: November 22, 1977
    Assignee: American Home Products Corporation
    Inventor: Donald Peter Strike
  • Patent number: 4041155
    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.
    Type: Grant
    Filed: October 29, 1974
    Date of Patent: August 9, 1977
    Assignee: American Home Products Corporation
    Inventors: Richard L. Fenichel, Howard J. Levin
  • Patent number: 4041037
    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.
    Type: Grant
    Filed: June 21, 1976
    Date of Patent: August 9, 1977
    Assignee: American Home Products Corporation
    Inventors: William Dvonch, Harvey E. Alburn