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).
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Patent number: 5428004Abstract: 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: GrantFiled: December 8, 1993Date of Patent: June 27, 1995Assignee: Hoffmann-La Roche Inc.Inventors: James V. Earley, Norman W. Gilman, Perry Rosen
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Patent number: 5302590Abstract: 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: GrantFiled: December 18, 1992Date of Patent: April 12, 1994Assignee: Hoffmann-La Roche Inc.Inventors: James V. Earley, Norman W. Gilman, Perry Rosen
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Patent number: 4973599Abstract: 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: GrantFiled: March 14, 1989Date of Patent: November 27, 1990Assignee: Hoffman-La Roche Inc.Inventors: Norman W. Gilman, Wen Y. Chen
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Patent number: 4777169Abstract: Benzodiazepine derivatives useful in immunoassays for benzodiazepines.Type: GrantFiled: November 6, 1987Date of Patent: October 11, 1988Assignee: Hoffmann-La Roche Inc.Inventors: James V. Earley, Norman W. Gilman
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Patent number: 4547581Abstract: 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: GrantFiled: August 23, 1984Date of Patent: October 15, 1985Assignee: Hoffmann-La Roche Inc.Inventors: Rodney I. Fryer, Norman W. Gilman, Eugene J. Trybulski, Armin Walser
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Patent number: 4546183Abstract: 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: GrantFiled: August 23, 1984Date of Patent: October 8, 1985Assignee: Hoffmann-La Roche Inc.Inventors: Rodney I. Fryer, Norman W. Gilman, Eugene J. Trybulski, Armin Walser
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Patent number: 4481142Abstract: 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: GrantFiled: October 27, 1982Date of Patent: November 6, 1984Assignee: Hoffmann-La Roche Inc.Inventors: Rodney I. Fryer, Norman W. Gilman, Eugene J. Trybulski, Armin Walser
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Patent number: 4336388Abstract: 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: GrantFiled: December 15, 1980Date of Patent: June 22, 1982Assignee: Hoffmann-La Roche Inc.Inventors: Rodney I. Fryer, Norman W. Gilman
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Patent number: 4321199Abstract: 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: GrantFiled: December 15, 1980Date of Patent: March 23, 1982Assignee: Hoffmann-La Roche Inc.Inventors: Rodney I. Fryer, Norman W. Gilman
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Patent number: 4269774Abstract: 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: GrantFiled: June 23, 1980Date of Patent: May 26, 1981Assignee: Hoffmann-La Roche Inc.Inventors: Rodney I. Fryer, Norman W. Gilman