Patents by Inventor Barnett S. Pitzele

Barnett S. Pitzele has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 4933325
    Abstract: The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is hydrogen, lower alkyl, hydroxy, --OCO.sub.2 lower alkyl, lower alkoxy, --O(CH.sub.2).sub.n -phenyl with the phenyl optionally substituted by halogen, --NO.sub.2, --CN, --NH.sub.2 or lower alkyl wherein n is 1 to 4; R.sup.2 and R.sup.3 represent lower alkyl, halogen, or lower alkoxy, or either one of R.sup.2 or R.sup.3 is hydrogen and the other is lower alkyl, lower alkoxy or halogen; R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 may be the same or different and represent hydrogen or lower alkyl; R.sup.
    Type: Grant
    Filed: January 20, 1988
    Date of Patent: June 12, 1990
    Assignee: G. D. Searle & Co.
    Inventors: Donald W. Hansen, Jr., Barnett S. Pitzele, Michael Clare, Robert W. Hamilton
  • Patent number: 4880829
    Abstract: The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is hydrogen, lower alkyl, hydroxy, --OCO.sub.2 lower alkyl, lower alkoxy, --O(CH.sub.2).sub.n --phenyl with the phenyl optionally substituted by halogen, --NO.sub.2, --CN, --NH.sub.2 or lower alkyl wherein n is 1 to 4; R.sup.2 and R.sup.3 represent lower alkyl, halogen, or lower alkoxy, or either one of R.sup.2 or R.sup.3 is hydrogen and the other is lower alkyl, lower alkoxy or halogen; R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 may be the same or different and represent hydrogen or lower alkyl; R.sup.
    Type: Grant
    Filed: January 20, 1988
    Date of Patent: November 14, 1989
    Assignee: G. D. Searle and Company
    Inventors: Donald W. Hansen, Jr., Barnett S. Pitzele, Michael Clare, Robert W. Hamilton
  • Patent number: 4847241
    Abstract: The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is hydrogen, lower alkyl, hydroxy, --OCO.sub.2 lower alkyl, lower alkoxy, --O(CH.sub.2).sub.n --phenyl with the phenyl optionally substituted by halogen, --NO.sub.2, --CN, --NH.sub.2 or lower alkyl wherein n is 1 to 4; R.sup.2 and R.sup.3 represent lower alkyl, halogen, or lower alkoxy, or either one of R.sup.2 or R.sup.3 is hydrogen and the other is lower alkyl, lower alkoxy or halogen; R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 may be the same or different and represent hydrogen or lower alkyl; R.sup.
    Type: Grant
    Filed: January 20, 1988
    Date of Patent: July 11, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Donald W. Hansen, Jr., Robert W. Hamilton, Barnett S. Pitzele, Michael Clare
  • Patent number: 4822775
    Abstract: The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is hydrogen, lower alkyl, hydroxy, --OCO.sub.2 lower alkyl, lower alkoxy, --O(CH.sub.2).sub.n -phenyl with the phenyl optionally substituted by halogen, --NO.sub.2, --CN, --NH.sub.2 or lower alkyl wherein n is 1 to 4; R.sup.2 and R.sup.3 represent lower alkyl, halogen, or lower alkoxy, or either one of R.sup.2 or R.sup.3 is hydrogen and the other is lower alkyl, lower alkoxy or halogen; R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 may be the same or different and represent hydrogen or lower alkyl; R.sup.
    Type: Grant
    Filed: July 14, 1986
    Date of Patent: April 18, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Donald W. Hansen, Jr., Barnett S. Pitzele, Michael Clare, Robert W. Hamilton
  • Patent number: 4797470
    Abstract: This invention relates to compounds of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is ##STR2## where X is oxygen or sulfur, Y is oxygen or nitrogen, and R.sup.11 represents straight or branched chain lower alkenyl having 2-6 carbon atoms, or phenyl, benzyl, and their equivalents such as nitro, halogen, or lower alkyl or lower alkoxy substituted phenyl or benzyl; wherein R.sup.2 and R.sup.3 may be the same or different and represent straight or branched chain lower alkyl having 1-6 carbon atoms, wherein R.sup.4 -R.sup.9 may be the same or different and represent hydrogen, or straight or branched chain lower alkyl having 1-6 carbon atoms; wherein C.sub.w is an asymmetric carbon atom when R.sup.7 and R.sup.8 are not the same and may be racemic or have the D or L configuration; and wherein C.sup.v is an asymmetric carbon atom and may be racemic or may have the D or L configuration.
    Type: Grant
    Filed: February 13, 1987
    Date of Patent: January 10, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Barnett S. Pitzele, Donald W. Hansen, Jr., Robert W. Hamilton, Daniel R. Pilipauskas, Michael Clare
  • Patent number: 4760180
    Abstract: This invention encompasses compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is lower alkoxy or --O--(CH.sub.2).sub.n -phenyl where the phenyl may be optionally substituted with halogen, --NO.sub.2, --CN, --NH.sub.2 or lower alkyl wherein n is 1 to 4; R.sup.2 and R.sup.3 represent lower alkyl, halogen, lower alkoxy or one of R.sup.2 or R.sup.3 is hydrogen and the other is lower alkyl, lower alkoxy, or halogen; R.sup.4, R.sup.5, R.sup.7, R.sup.8, and R.sup.9 represent hydrogen or lower alkyl, R.sup.6 represents hydrogen, lower alkyl, lower alkenyl, or --(CH.sub.2).sub.m -cycloalkyl wherein m is 1 to 4 and the cycloalkyl has 3 to 8 carbon atoms; R.sup.10 is --(CH.sub.2).sub.p -phenyl wherein p is 1 to 4; and v represents an asymmetric carbon that may be racemic or have the D or L Configuration; w represents an asymmetric carbon when R.sup.7 and R.sup.8 are not the same that may be racemic or have the D or L configuration.
    Type: Grant
    Filed: July 14, 1986
    Date of Patent: July 26, 1988
    Assignee: G. D. Searle & Co.
    Inventors: Barnett S. Pitzele, Donald W. Hansen, Jr., Robert W. Hamilton, Daniel R. Pilipauskas, Michael Clare
  • Patent number: 4758675
    Abstract: This invention relates to novel 3-thiophene-substituted tryosyl dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable addition salts thereof, wherein R.sup.1 is --OH, benzyloxy, or --OCH.sub.3 ; wherein R.sub.2 and R.sub.3 may be the same or different and represent lower alkyl of 1-6 carbon atoms; wherein R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 may be the same or different and represent hydrogen or lower alkyl of 1-6 carbon atoms; wherein "v" represents an asymmetric carbon atom that may be racemic or that may have the D or L configuration; and wherein "w" represents an asymmetric carbon atom that has the D configuration. These compounds are useful as analgesic agents.
    Type: Grant
    Filed: February 13, 1987
    Date of Patent: July 19, 1988
    Assignee: G. D. Searle & Co.
    Inventors: Donald W. Hansen, Jr., Barnett S. Pitzele, Robert W. Hamilton, Michael Clare
  • Patent number: 4579951
    Abstract: This invention relates to novel substituted (azacycloalk-2-yl)iminophenols that are useful in the treatment of diarrhea.
    Type: Grant
    Filed: March 19, 1984
    Date of Patent: April 1, 1986
    Assignee: G. D. Searle & Co.
    Inventors: Barnett S. Pitzele, Stella S. T. Yu, Robert W. Hamilton
  • Patent number: 4533739
    Abstract: This invention relates to the novel use of certain aromatic substituted amidines as antidiarrheals.
    Type: Grant
    Filed: October 12, 1982
    Date of Patent: August 6, 1985
    Assignee: G. D. Searle & Co.
    Inventors: Barnett S. Pitzele, Stella S. T. Yu, Robert W. Hamilton, Alan E. Moormann
  • Patent number: 4523020
    Abstract: This invention relates to novel substituted 2-(3-aminophenoxymethyl)imidazolines which are useful for the treatment of diarrhea and useful as analgesics.
    Type: Grant
    Filed: November 10, 1983
    Date of Patent: June 11, 1985
    Assignee: G. D. Searle & Co.
    Inventors: Alan E. Moormann, Barnett S. Pitzele, Peter H. Jones
  • Patent number: 4431802
    Abstract: Compounds of formula I and salts thereof which are orally pharmacologically active as inhibitors of gastric secretion are disclosed.
    Type: Grant
    Filed: November 23, 1981
    Date of Patent: February 14, 1984
    Assignee: G. D. Searle & Co.
    Inventors: Alan E. Moormann, Barnett S. Pitzele, Gilbert W. Adelstein, Nancy J. Malek
  • Patent number: 4388308
    Abstract: N.sup.6 -2-hydroxypropylaryl-substituted adenosines and adenines represented by the formula ##STR1## wherein R.sub.1 is selected from the group consisting of naphthyl, phenyl, substituted phenyl or biphenyl; and R.sub.2 is hydrogen or 1-.beta.-ribosyl; and the pharmaceutically acceptable salts thereof. The compounds are anti-hypertensive agents.
    Type: Grant
    Filed: June 9, 1980
    Date of Patent: June 14, 1983
    Assignee: G.D. Searle & Co.
    Inventors: Robert W. Hamilton, Richard E. L. Henderson, Barnett S. Pitzele
  • Patent number: 4386211
    Abstract: The invention relates to certain urea derivatives of the formula R.sub.1 CH.sub.2 S(CH.sub.2).sub.2 NHCONHR.sub.2 where R.sub.1 are certain furanyls, imidazoles and thiazolyls and R.sub.2 are certain imidazoles and thiazolyls. These compounds are H-2 histamine receptor inhibitors and therefore useful in the treatment of ulcers.
    Type: Grant
    Filed: August 25, 1981
    Date of Patent: May 31, 1983
    Assignee: G. D. Searle & Co.
    Inventors: Richard E. L. Henderson, Barnett S. Pitzele
  • Patent number: 4374932
    Abstract: The present invention relates to novel compounds for the prophylaxis and treatment of Inflammatory Bowel disease (IBD) via the administration of an effective amount in a suitable pharmaceutical dosage of a polymeric agent for releasing 5,5'-azobis-salicylic acid which comprises a non-degradable anionic exchange resin and the dianionic form of 5,5'-azobis-salicylic acid. The 5,5'-azobis-salicylic acid undergoes bacterial cleavage in the mammalian lower bowel to release 5-aminosalicylic acid.
    Type: Grant
    Filed: June 8, 1981
    Date of Patent: February 22, 1983
    Assignee: G. D. Searle & Co.
    Inventors: Barnett S. Pitzele, Peter H. Jones
  • Patent number: 4340730
    Abstract: Novel N.sup.6 -adenosines according to formula I are disclosed. These novel compounds are useful as antihypertensive agents.
    Type: Grant
    Filed: January 30, 1981
    Date of Patent: July 20, 1982
    Assignee: G. D. Searle & Co.
    Inventors: Richard E. L. Henderson, Nancy J. Malek, Alan E. Moormann, Barnett S. Pitzele
  • Patent number: 4312806
    Abstract: The present invention relates to novel compounds and a method for the prophylaxis and treatment of Inflammatory Bowel Disease (IBD) via the administration of an effective amount in a suitable pharmaceutical dosage form of an azobenzene compound of formula I or a pharmacologically acceptable salt, which is reductively cleaved to 5-aminosalicylic acid (5-ASA) by bacteria in the large intestine.
    Type: Grant
    Filed: March 2, 1981
    Date of Patent: January 26, 1982
    Assignee: G. D. Searle & Co.
    Inventors: Howard J. Lambert, Barnett S. Pitzele
  • Patent number: 3971827
    Abstract: .gamma.-Alkylation of 2-butynoic acid utilizing lithium 2,2,6,6-tetramethylpiperidide and 1-bromo-3-methyl-2-butene, followed by esterification of the resulting 7-methyloct-6-en-2-ynoic acid and treatment of the ester with lithium dimethyl cuprate, yields methyl (Z)-3,7-dimethylocta-2,6-dienoate. The ester is reduced to (Z)-3,7-dimethylocta-2,6-dien-1-ol, commonly known as nerol, which is useful as perfume agent.
    Type: Grant
    Filed: September 9, 1974
    Date of Patent: July 27, 1976
    Assignee: G. D. Searle & Co.
    Inventors: John S. Baran, Barnett S. Pitzele