Patents Represented by Attorney Robert H. Brink
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Patent number: 5866591Abstract: Stable formulations of 3-?4-methoxycarbonyl-4-?(1 -oxopropyl)phenylamino!-1-piperidine!propanoic acid, methyl ester, generally referred to as remifentanil, are disclosed. In particular, stabilized lyophilized solid composition are disclosed comprising certain acids, most preferably comprising glycine.Type: GrantFiled: September 10, 1997Date of Patent: February 2, 1999Assignee: Glaxo Wellcome Inc.Inventors: Larry Alan Gatlin, Shirley Ann Heiman, Janet Sue Lewis
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Patent number: 5859007Abstract: Benzo?b!?1,4!diazepine compounds of formula (I), where R.sup.1 is selected from C.sub.1 C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, phenyl, or substituted phenyl; R.sup.2 is selected from C.sub.3 -C.sub.6 alkyl, C.sub.3 C.sub.6 cycloalkyl, C.sub.3 -C.sub.6 alkenyl, benzyl, phenylC.sub.1 -C.sub.3 alkyl of substituted phenyl; or NR.sup.1 R.sup.2 together form 1,2,3,4-tetrahydroquinoline or benzazepine, mono-, di-, or trisubstituted independently with C.sub.1-6 alkyl C.sub.1-6 alkoxy or halogen substituents; p is an integer 0 or 1; q is an integer 0 or 1; r is an integer 0 or 1; t is an integer 0 or 1, provided that when r is 0 then t is 0; R.sup.3, R.sup.5, and R.sup.6 are independently hydrogen or C.sub.1-6 alkyl; R.sup.4 is C.sub.1-6 alkyl or C.sub.1-6 alkenyl; R.sup.7 is selected from the group consisting of hydrogen, C.sub.1-6 alkyl, C.sub.1-6 cycloalkyl, C.sub.1-6 alkenyl, phenyl, substituted phenyl, napthyl, heteroaryl, substituted heteroaryl, bicycloheteroaryl or substituted bicycloheteroaryl; or NR.sup.Type: GrantFiled: November 14, 1996Date of Patent: January 12, 1999Assignee: Glaxo Wellcome Inc.Inventors: Christopher Joseph Aquino, Marcus Brackeen, Milana Dezube, Brad Richard Henke, Gavin Charles Hirst, Peter Walter Jeffs, Tanya Momtahen, Elizabeth Ellen Sugg, Edward Martin Suh, Timothy Mark Willson
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Patent number: 5846976Abstract: The present invention relates to the compound of formula (I), ##STR1## also known as 17.beta.-N-(2,5-bis(Trifluoromethyl))phenylcarbamoyl-4-aza-5.alpha.-andros t-1-en-3-one, solvates thereof, its preparation, intermediates used in its preparation, pharmaceutical formulations thereof and its use in the treatment of androgen responsive and mediated diseases.Type: GrantFiled: August 22, 1996Date of Patent: December 8, 1998Assignee: Glaxo Wellcome Inc.Inventors: Kenneth William Batchelor, Stephen Vernon Frye, George F. Dorsey, Jr., Robert A. Mook, Jr.
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Patent number: 5817818Abstract: The present invention relates to compounds of formula (I), wherein carbons 1 and 2 are joined by either a single or a double bond; R.sup.1 is hydrogen or methyl; R.sup.2 is hydrogen or methyl; R.sup.3 is (A) or (B) wherein X, W, Z, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are various groups, and pharmaceutically acceptable solvates thereof and their use in the treatment of androgen responsive and mediated diseases.Type: GrantFiled: March 14, 1996Date of Patent: October 6, 1998Assignee: Glaxo Wellcome Inc.Inventors: Kenneth William Batchelor, Stephen Vernon Frye
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Patent number: 5795887Abstract: A method of inducing a Cholescystokinin-A receptor agonist response in a mammal by administering a compound of formula (I), ##STR1## where R.sup.1 is C.sub.1 -C.sub.6 alkyl, C.sub.3-6 cycloalkyl, phenyl, or substituted phenyl; R.sup.2 is C.sub.3-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-6 alkenyl, benzyl, phenylC.sub.1-3 alkyl or substituted phenyl; or NR.sup.1 R.sup.2 together form 1,2,3,4-tetrahydroquinoline or benzazepine mono-, di-, or trisubstituted independently with C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen substituents; n is an integer selected from the grouping consisting of 0,1,2 or 3; p is the integer 0 or 1; q is the integer 0 or 1; r is the integer 0 or 1, provided that when q is 0 then r is 0; R.sup.3, R.sup.4, R.sup.5 and R.sup.8 are selected from a variety of substituents; X is nitrogen, nitroso or R.sup.Type: GrantFiled: October 11, 1996Date of Patent: August 18, 1998Assignee: Glaxo Wellcome Inc.Inventors: Christopher Joseph Aquino, Milana Dezube, Ronald George Sherrill, Elizabeth Ellen Sugg, Jerzy Ryszard Szewczyk, Timothy Mark Willson
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Patent number: 5780464Abstract: A pharmaceutical formulation in solid dosage form for oral administration which comprises a compound of the general Formula (I) ##STR1## or a physiologically acceptable salt or solvate thereof together with one or more pharmaceutically acceptable carriers wherein the formulation is encased in an enteric coating or capsule.Type: GrantFiled: April 14, 1997Date of Patent: July 14, 1998Assignee: Glaxo Wellcome Inc.Inventor: Elizabeth Ellen Sugg
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Patent number: 5739129Abstract: Compounds of general formula (I) and physiologically salts thereof, processes for their preparation and their use as modulators of the effects of gastrin and CCK.Type: GrantFiled: October 11, 1996Date of Patent: April 14, 1998Assignee: Glaxo Wellcome Inc.Inventors: Christopher Joseph Aquino, Elizabeth Ellen Sugg, Jerzy Ryszard Szewczyk
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Patent number: 5708001Abstract: The present invention relates to certain substituted 17.beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I), wherein R.sup.1 and R.sup.2 i) are independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, or ii) taken together are a --CH.sub.2 -- group forming a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond; R.sup.3 is preferably hydrogen, halogen or lower alkyl, R.sup.4 is preferably hydrogen or lower alkyl, X is preferably CH.sub.2, Y is preferably hydrogen and Z is preferably CONR.sup.14 R.sup.15 and R.sup.14 and R.sup.15 are a variety of organic groups, and pharmaceutically acceptable salts thereof, preparation, medical use and pharmaceutical formulations.Type: GrantFiled: June 7, 1995Date of Patent: January 13, 1998Assignee: Glaxo Wellcome Inc.Inventors: Robert Carl Andrews, Cynthia Markert Cribbs, Stephen Vernon Frye, Curt Dale Haffner, Patrick Reed Maloney
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Patent number: 5670643Abstract: The present invention relates to a process for the preparation of finasteride, the compound of formula (I), comprising the reaction of the compound of formula (II) with t-butylamine.Type: GrantFiled: March 16, 1995Date of Patent: September 23, 1997Assignee: Glaxo Wellcome Inc.Inventors: Roman Davis, Alan Millar
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Patent number: 5648347Abstract: A method for the treatment of depression in a human being, the method comprising administering to the human being an antidepressant effective amount of a compound of the following formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R and R.sup.1 are independently hydrogen or fluorine.Type: GrantFiled: May 19, 1995Date of Patent: July 15, 1997Assignee: Glaxo Wellcome Inc.Inventors: Nariman Bomanshaw Mehta, Grady Evan Boswell, James Leroy Kelley
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Patent number: 5635200Abstract: This invention relates to a composition which is substantially free of the bitter taste associated with ranitidine and comprises: a) a dispersion of lipid coated particles of ranitidine or a physiologically acceptable salt thereof in a non-aqueous vehicle; b) particles comprising ranitidine or a physiologically acceptable salt thereof incorporated into a core and coated with a lipid coating; c) lipid coated particles of a form of ranitidine which is poorly soluble in water; and processes for the preparation thereof and pharmaceutical compositions thereof.Type: GrantFiled: April 12, 1995Date of Patent: June 3, 1997Assignee: Glaxo Group LimitedInventors: Stephen J. Douglas, Jill Evans
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Patent number: 5565467Abstract: The present invention relates to the compound of formula (I), ##STR1## also known as 17.beta.-N-(2,5-bis(Trifluoromethyl))phenylcarbamoyl-4-aza-5.alpha.-andros t-1-en-3-one, solvates thereof, its preparation, intermediates used in its preparation, pharmaceutical formulations thereof and its use in the treatment of androgen responsive and mediated diseases.Type: GrantFiled: March 16, 1995Date of Patent: October 15, 1996Assignee: Glaxo Wellcome Inc.Inventors: Kenneth W. Batchelor, Stephen V. Frye, George F. Dorsey, Jr., Robert A. Mook, Jr.
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Patent number: 5543406Abstract: The present invention relates to certain substituted 17.beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I), especially those of formula (IG) ##STR1## wherein R.sup.1 and R.sup.2 arei) independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, orii) taken together are a --CH.sub.2 -- group to form a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond;R.sup.3c is hydrogen;R.sup.4c is hydrogen, lower alkyl, lower cycloalkyl, lower alkenyl, alkanoyl of 2-6 carbons, --(CH.sub.2).sub.m CO.sub.2 R.sup.16, --(CH.sub.2).sub.m Ar.sup.a, --(CH.sub.2).sub.n 'CONR.sup.17 R.sup.18, --(CH.sub.2).sub.n 'NR.sup.17 R.sup.18 or --(CH.sub.2).sub.n 'OR.sup.16, wherein R.sup.16 is hydrogen, lower alkyl or lower alkenyl; R.sup.17 and R.sup.18 are independently hydrogen, lower alkyl lower cycloalkyl or lower alkenyl; Ar.sup.Type: GrantFiled: August 15, 1994Date of Patent: August 6, 1996Assignee: Glaxo Wellcome, Inc.Inventors: Robert C. Andrews, Cynthia M. Cribbs, Stephen V. Frye, Curt D. Haffner, Patrick R. Maloney
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Patent number: 5541322Abstract: A process of providing novel compounds of Formula (I), that are useful as 6-azaandrostenone testosterone 5-alpha-reductase inhibitors, from commercially available compounds of Formula (II) ##STR1## wherein the substituents are as defined in the specification, and the pharmaceutically acceptable salts and solvates thereof.Type: GrantFiled: October 14, 1994Date of Patent: July 30, 1996Assignee: Glaxo Wellcome Inc.Inventors: Francis G. Fang, Matthew J. Sharp
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Patent number: 5498745Abstract: Novel compounds which are 2,6-di-t-butylphenols substituted on the 4 position by an anilino group, which anilino group is substituted by a carboxyl substituent, a tetrazolyl substituent or an N-methyltetrazolyl substituent, are useful antiallergic agents. Pharmaceutical compositions containing and pharmacological methods of using such compounds are also disclosed, as are synthetic intermediates for preparing such compounds. Certain of the synthetic intermediates also exhibit useful antiallergic activity.Type: GrantFiled: May 5, 1995Date of Patent: March 12, 1996Assignee: Riker Laboratories, Inc.Inventor: Robert A. Scherrer
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Patent number: 5495043Abstract: Novel compounds which are 2,6-di-t-butylphenols substituted on the 4 position by an anilino group, which anilino group is substituted by a carboxyl substituent, a tetrazolyl substituent or an N-methyltetrazolyl substituent, are useful antiallergic agents. Pharmaceutical compositions containing and pharmacological methods of using such compounds are also disclosed, as are synthetic intermediates for preparing such compounds. Certain of the synthetic intermediates also exhibit useful antiallergic activity.Type: GrantFiled: May 5, 1995Date of Patent: February 27, 1996Assignee: Riker Laboratories, Inc.Inventor: Robert A. Scherrer
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Patent number: 5494680Abstract: A transdermal drug delivery device involving a backing bearing at least one adhesive layer of an acrylate copolymer and a therapeutically effective amount of (S)-3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole. The device optionally further involves (i) a second adhesive layer of an acrylate copolymer and optionally a therapeutically effective amount of (S)-3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole, and (ii) a membrane intermediate the first and second adhesive layers.Type: GrantFiled: December 8, 1993Date of Patent: February 27, 1996Assignee: Minnesota Mining and Manufacturing CompanyInventor: Timothy A. Peterson
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Patent number: 5494916Abstract: Imidazo[4,5-c]pyridin-4-amines that induce interferon (.alpha.) biosynthesis in human cells. Also disclosed are pharmaceutical compositions containing such compounds and methods of inducing interferon (.alpha.) biosynthesis involving the use of such compounds.Type: GrantFiled: November 4, 1994Date of Patent: February 27, 1996Assignee: Minnesota Mining and Manufacturing CompanyInventors: Kyle J. Lindstrom, Nick Nikolaides
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Patent number: 5482936Abstract: Compounds and pharmaceutically acceptable salts thereof formally derived by bridging the 1- and 2-positions of 1H-imidazo[4,5-c]quinolin-4-amines. Also, methods of using such compounds and pharmaceutical formulations containing such compounds. Said compounds are useful to induce interferon biosynthesis in an animal.Type: GrantFiled: January 12, 1995Date of Patent: January 9, 1996Assignee: Minnesota Mining and Manufacturing CompanyInventor: Kyle J. Lindstrom
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Patent number: RE35466Abstract: Group IV organometallic compounds, e.g. alkylsilane, or alkylsiloxane compounds, are used as chain tranfer agent in the radical initiated polymerization of ethylenically unsaturated monomers, to give polymers comprising non-ionic end groups.Type: GrantFiled: June 30, 1994Date of Patent: February 25, 1997Assignee: Minnesota Mining and Manufacturing CompanyInventor: Werner M. Grootaert