Patents by Inventor Norman W. Gilman

Norman W. Gilman 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: 5428004
    Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sub.1 is OR.sub.6 or NHR.sub.7, R.sub.6 and R.sub.7, which may be, the same or different, are hydrogen, lower alkyl, lower alkenyl, cycloalkyl having between 3 to 6 carbon atoms or phenyl, R.sub.2 is lower alkyl, lower alkoxy or trifluoromethyl, R.sub.3 and R.sub.4 independently, are hydrogen, chlorine, fluorine, lower alkyl or lower alkoxy, and R.sub.5 is lower alkyl or cycloalkyl having between 3 to 6 carbon atoms, and when at least one asymetric carbon is present, enantiomers, and racemates thereof, and pharmaceutically acceptable salts thereof.The compounds of formula I and pharmaceutically acceptable salts thereof are useful as bronchopulmonary agents for example in the relief of asthma and allergic reactions.In another aspect, the invention relates to pharmaceutical compositions, methods of using the compound of formula I and intermediates.
    Type: Grant
    Filed: December 8, 1993
    Date of Patent: June 27, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: James V. Earley, Norman W. Gilman, Perry Rosen
  • Patent number: 5302590
    Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sub.1 is OR.sub.6 or NHR.sub.7, R.sub.6 and R.sub.7, which may be, the same or different, are hydrogen, lower alkyl, lower alkenyl, cycloalkyl having between 3 to 6 carbon atoms or phenyl, R.sub.2 is lower alkyl, lower alkoxy or trifluoromethyl, R.sub.3 and R.sub.4, independently, are hydrogen, chlorine, fluorine, lower alkyl or lower alkoxy, and R.sub.5 is lower alkyl or cycloalkyl having between 3 to 6 carbon atoms, and when at least one asymetric carbon is present, enantiomers, and racemates thereof, and pharmaceutically acceptable salts thereof.The compounds of formula I and pharmaceutically acceptable salts thereof are useful as bronchopulmonary agents for example in the relief of asthma and allergic reactions.In another aspect, the invention relates to pharmaceutical compositions, methods of using the compound of formula I and intermediates.
    Type: Grant
    Filed: December 18, 1992
    Date of Patent: April 12, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: James V. Earley, Norman W. Gilman, Perry Rosen
  • Patent number: 4973599
    Abstract: Compounds of the formula ##STR1## wherein n is a integer of 0 to 2; R.sub.1 ' and R.sub.2 ' are, independently, hydrogen, halogen, trifluoromethyl, lower alkoxy or lower alkyl; and X is pyrimidinyl, thiazolyl or ##STR2## wherein R is hydrogen, lower alkyl, aryl or ar-lower alkyl; provided that at least one or R.sub.1 ' and R.sub.2 ' is other than hydrogen,and their pharmaceutically acceptable acid addition salts, and an anti-inflammatory method utilizing a compound of the formula ##STR3## wherein n is an integer of 0 to 2; R.sub.1 and R.sub.2 are, independently, hydrogen, halogen, trifluoromethyl, nitro, amino, lower alkylamino, di-lower-alkylamino, lower alkoxy or lower alkyl; and X is pyrimidinyl, thiazolyl or ##STR4## wherein R is hydrogen, lower alkyl, aryl or ar-lower alkyl; and their pharmaceutically acceptable acid addition salts, are described.
    Type: Grant
    Filed: March 14, 1989
    Date of Patent: November 27, 1990
    Assignee: Hoffman-La Roche Inc.
    Inventors: Norman W. Gilman, Wen Y. Chen
  • Patent number: 4777169
    Abstract: Benzodiazepine derivatives useful in immunoassays for benzodiazepines.
    Type: Grant
    Filed: November 6, 1987
    Date of Patent: October 11, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: James V. Earley, Norman W. Gilman
  • Patent number: 4547581
    Abstract: There is presented compounds of the formula ##STR1## wherein A is selected from the group consisting of ##STR2## R.sub.1 is selected from the group consisting of hydrogen, chlorine, bromine, lower alkyl, the group NR.sub.4 R.sub.5, the group --CH.sub.2 --CO--R.sub.7, the group --NH(CH.sub.2).sub.m NR.sub.8 R.sub.9, hydroxy, lower alkoxy, mercapto and lower alkyl mercapto; R.sub.2 is selected from the group consisting of hydrogen, amino and di-lower alkyl amino; R.sub.3 is selected from the group consisting of hydrogen, lower acyloxy and hydroxy; X is selected from the group consisting of hydrogen, halogen, trifluoromethyl, ethyl, .alpha.-hydroxy ethyl and acetyl; Y is hydrogen or halogen; R.sub.4 and R.sub.5 are hydrogen or lower alkyl or together with their co-bonded nitrogen atom form a five to seven membered heterocyclic group; R.sub.7 is selected from the group consisting of hydroxy lower alkoxy and NR.sub.8 R.sub.9 ; R.sub.8 and R.sub.
    Type: Grant
    Filed: August 23, 1984
    Date of Patent: October 15, 1985
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rodney I. Fryer, Norman W. Gilman, Eugene J. Trybulski, Armin Walser
  • Patent number: 4546183
    Abstract: There is presented compounds of the formula ##STR1## wherein A is selected from the group consisting of ##STR2## R.sub.1 is selected from the group consisting of hydrogen, chlorine, bromine, lower alkyl, the group NR.sub.4 R.sub.5, the group --CH.sub.2 --CO--R.sub.7, the group --NH(CH.sub.2).sub.m NR.sub.8 R.sub.9, hydroxy, lower alkoxy, mercapto and lower alkyl mercapto; R.sub.2 is selected from the group consisting of hydrogen, amino and di-lower alkyl amino; R.sub.3 is selected from the group consisting of hydrogen, lower acyloxy and hydroxy; X is selected from the group consisting of hydrogen, halogen, trifluoromethyl, ethyl, .alpha.-hydroxy ethyl and acetyl; Y is hydrogen or halogen; R.sub.4 and R.sub.5 are hydrogen or lower alkyl or together with their co-bonded nitrogen atom form a five to seven membered heterocyclic group; R.sub.7 is selected from the group consisting of hydroxy lower alkoxy and NR.sub.8 R.sub.9 ; R.sub.8 and R.sub.
    Type: Grant
    Filed: August 23, 1984
    Date of Patent: October 8, 1985
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rodney I. Fryer, Norman W. Gilman, Eugene J. Trybulski, Armin Walser
  • Patent number: 4481142
    Abstract: There is presented compounds of the formula ##STR1## wherein A is selected from the group consisting of ##STR2## R.sub.1 is selected from the group consisting of hydrogen, chlorine, bromine, lower alkyl, the group NR.sub.4 R.sub.5, the group --CH.sub.2 --CO--R.sub.7, the group--NH(CH.sub.2).sub.m NR.sub.8 R.sub.9, hydroxy, lower alkoxy, mercapto and lower alkyl mercapto; R.sub.2 is selected from the group consisting of hydrogen, amino and dilower alkyl amino; R.sub.3 is selected from the group consisting of hydrogen, lower acyloxy and hydroxy; X is selected from the group consisting of hydrogen, halogen, trifluoromethyl, ethyl, .alpha.-hydroxy ethyl and acetyl; Y is hydrogen or halogen; R.sub.4 and R.sub.5 are hydrogen or lower alkyl or together with their co-bonded nitrogen atom form a five to seven membered heterocyclic group; R.sub.7 is selected from the group consisting of hydroxy lower alkoxy and NR.sub.8 R.sub.9 ; R.sub.8 and R.sub.
    Type: Grant
    Filed: October 27, 1982
    Date of Patent: November 6, 1984
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rodney I. Fryer, Norman W. Gilman, Eugene J. Trybulski, Armin Walser
  • Patent number: 4336388
    Abstract: There is presented compounds of formula ##STR1## wherein X and Y are hydrogen or halogen and R.sub.1 is lower alkyl or NR.sub.2 R.sub.3wherein R.sub.2 and R.sub.3 are hydrogen or lower alkyland the pharmaceutically acceptable salts thereof.Also presented are novel intermediates and a process to produce the novel end products.The compounds of formula I are useful as anxiolytic and sedative agents.
    Type: Grant
    Filed: December 15, 1980
    Date of Patent: June 22, 1982
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rodney I. Fryer, Norman W. Gilman
  • Patent number: 4321199
    Abstract: There is presented compounds of formula ##STR1## wherein X and Y are hydrogen or halogen and R.sub.1 is lower alkyl or NR.sub.2 R.sub.3wherein R.sub.2 and R.sub.3 are hydrogen or lower alkyland the pharmaceutically acceptable salts thereof.Also presented are novel intermediates and a process to produce the novel end products.The compounds of formula I are useful as anxiolytic and sedative agents.
    Type: Grant
    Filed: December 15, 1980
    Date of Patent: March 23, 1982
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rodney I. Fryer, Norman W. Gilman
  • Patent number: 4269774
    Abstract: There is presented compounds of formula ##STR1## wherein X and Y are hydrogen or halogen and R.sub.1 is lower alkyl or NR.sub.2 R.sub.3wherein R.sub.2 and R.sub.3 are hydrogen or lower alkyland the pharmaceutically acceptable salts thereof.Also presented are novel intermediates and a process to produce the novel end products.The compounds of formula I are useful as anxiolytic and sedative agents.
    Type: Grant
    Filed: June 23, 1980
    Date of Patent: May 26, 1981
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rodney I. Fryer, Norman W. Gilman