Patents by Inventor Andrew G. Brewster
Andrew G. Brewster 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: 5612373Abstract: The invention concerns acid derivatives of formula IR.sup.1 --CON(R.sup.2)--N(R.sup.3)CO--X.sup.1 --Q--X.sup.2 --GIand pharmaceutically acceptable metabolically labile esters or amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.1, R.sup.2, R.sup.3, X.sup.1, Q, X.sup.2 and G have the meanings given in the specification. The invention also concerns processes for the preparation of the acid derivatives of formula I, pharmaceutical compositions containing them and their use as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa.Type: GrantFiled: June 27, 1994Date of Patent: March 18, 1997Assignee: Zeneca LimitedInventors: Andrew G. Brewster, Peter W. R. Caulkett, Alan W. Faull, Robert J. Pearce, Richard E. Shute
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Patent number: 5563141Abstract: A compound of the general formula(M.sup.1).sub.n --Q--(M.sup.2).sub.1-n --L--A Iwherein:n is 0 or 1;M.sup.1 is an amino group;Q is an aromatic heterocyclic group containing a basic nitrogen atom;M.sup.2 is an imino group;L is a template group; andA is an acidic group, or an ester or amide derivative thereof, or a sulphonamide group;and pharmaceutically acceptable salts and pro-drugs thereof, for use in the treatment of a disease in which platelet aggregation mediated by the binding of adhesion molecules to GPIIb-IIIa is involved. Novel compounds are also disclosed.Type: GrantFiled: March 28, 1994Date of Patent: October 8, 1996Assignee: Zeneca LimitedInventors: Michael G. Wayne, Michael J. Smithers, John W. Rayner, Alan W. Faull, Robert J. Pearce, Andrew G. Brewster, Richard E. Shute, Stuart D. Mills, Peter W. R. Caulkett
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Patent number: 5556977Abstract: Compounds of formula I ##STR1## and metabolically labile esters and amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.13, M.sup.2, X.sup.1, Z.sup.1, Z.sup.1a, X.sup.2 and A.sup.1 have the meanings given in the specification. The compounds are useful as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa. Intermediates are also disclosed.Type: GrantFiled: March 28, 1994Date of Patent: September 17, 1996Assignee: Zeneca LimitedInventors: Michael G. Wayne, Michael J. Smithers, John W. Rayner, Alan W. Faull, Robert J. Pearce, Andrew G. Brewster, Richard E. Shute, Sturat D. Mills, Peter W. R. Caulkett
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Patent number: 5401849Abstract: The invention concerns pharmaceutically useful 1,3-dioxane alkenoic acid derivatives of formula VII and formula XI containing a pyridyl moiety at position 4 of the dioxane ring and in which the groups at positions 2, 4 and 5 have cis-relative stereochemistry, wherein X is hydrogen, alkoxy or hydroxy, Y is vinylene, n is 1 or 2, A.sup.1 is alkylene, R.sup.1 is a variety of substituents defined hereinafter, Ra and Rb are independently methyl or ethyl, R.sup.2 is hydroxy, a physiologically acceptable alcohol residue or alkanesulphonamido, and the pharmaceutically acceptable salts thereof.Type: GrantFiled: June 21, 1993Date of Patent: March 28, 1995Assignee: Zeneca LimitedInventors: Andrew G. Brewster, George R. Brown, Alan W. Faull, Reginald Jessup, Michael J. Smithers
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Patent number: 5274118Abstract: A process for the preparation of (2R)-methyl-4,4,4-trifluorobutylamine, or an acid addition salt thereof which comprisesa) acylating an optically active amine with 2-methyl-4,4,4-trifluorobutanoic acid or a reactive derivative thereof to afford a butyramide;b) separating (R)-diastereomeric butyramide from (S)-diastereomeric butyramide; andc) converting the (R)-diastereomeric butyramide into the desired (2R)-methyl-4,4,4-trifluorobutylamine, or an acid addition salt thereof. The product may be acylated with a carboxylic acid of formula III ##STR1## wherein U is carboxy, or a reactive derivative thereof to afford (R)-4-[5-(N-[4,4,4-trifluoro-2-methylbutyl]carbamoyl)-1-methylindol-3-yl-m ethyl]-3-methoxy-N-o-tolylsulphonylbenzamide. The indole is useful as a leukotriene antagonist, for example in the treatment of asthma or allergic rhinitis.Type: GrantFiled: December 4, 1991Date of Patent: December 28, 1993Assignee: Imperial Chemical Industries PLCInventors: Robert T. Jacobs, Andrew G. Brewster, George J. Sependa
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Patent number: 5248780Abstract: The invention concerns novel, pharmaceutically useful 1,3-dioxane alkenoic acid derivatives of the formula I containing a pyridyl moiety at position 4 of the dioxane ring and in which the groups at positions 2, 4 and 5 have cis-relative stereochemistry, X is hydrogen, alkoxy or hydroxy, Y is vinylene, n is 1 or 2, A.sup.1 is alkylene, R.sup.1 is a variety of substituents defined hereinafter, and R.sup.2 is hydroxy, a physiologically acceptable alcohol residue or alkanesulphonamido, and the pharmaceutically acceptable salts thereof. The invention also includes processes for the manufacture and use of the acid derivatives as well as pharmaceutical compositions for therapeutic use in one or more of a variety of diseases such as ischaemic heart disease, cerebrovascular disease, asthmatic disease and/or inflammatory disease.Type: GrantFiled: September 25, 1992Date of Patent: September 28, 1993Assignee: Imperial Chemical Industries, PlcInventors: Andrew G. Brewster, George R. Brown, Alan W. Faull, Reginald Jessup, Michael J. Smithers
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Patent number: 5166377Abstract: The invention concerns novel 4-phenyl-1,3-dioxan-5-ylalkenoic acid derivatives of the formula I having cis relative stereochemistry at positions 4 and 5 of the dioxane ring and wherein Ra and Rb are variously hydrogen, alkyl, halogenoalkyl, alkenyl, and optionally substituted aryl or arylalkyl, Rc is hydroxy, alkoxy or alkanesulphonamido, n is 1 or 2, A is ethylene or vinylene, Y is (2-5C)polymethylene optionally substituted by alkyl, and benzene ring B is optionally substituted phenyl, or, when Rc is hydroxy, a salt thereof. The acid derivatives antagonize one or more of the actions of thromboxane A.sub.2 (TXA.sub.2) and are expected to be of value in those disease conditions in which TXA.sub.2 is involved. The invention also provides pharmaceutical compositions containing an acid derivative of formula I, and processes for their chemical production.Type: GrantFiled: February 9, 1988Date of Patent: November 24, 1992Assignee: Imperial Chemical Industries PLCInventors: Andrew G. Brewster, Peter W. R. Caulkett
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Patent number: 5166213Abstract: The invention concerns novel, pharmaceutically useful 1,3-dioxane alkenoic acid derivatives of the formula I containing a pyridyl moiety at position 4 of the dioxane ring and in which the groups at positions 2, 4 and 5 have cis-relative stereochemistry, X is hydrogen, alkoxy or hydroxy, Y is vinylene, n is 1 or 2, A.sup.1 is alkylene, R.sup.1 is a variety of substituents defined hereinafter, and R.sup.2 is hydroxy, a physiologically acceptable alcohol residue or alkanesulphonamido, and the pharmaceutically acceptable salts thereof. The invention also includes processes for the manufacture and use of the acid derivatives as well as pharmaceutical compositions for therapeutic use in one or more of a variety of diseases such as ischaemic heart disease, cerebrovascular disease, asthmatic disease and/or inflammatory disease.Type: GrantFiled: February 14, 1989Date of Patent: November 24, 1992Assignee: Imperial Chemical Industries PLCInventors: Andrew G. Brewster, George R. Brown, Alan W. Faull, Reginald Jessup, Michael J. Smithers
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Patent number: 5053415Abstract: The invention concerns novel, pharmaceutically useful 1,3-dioxane alkenoic acid derivatives of the formula I containing a pyridyl moiety at position 4 of the dioxane ring and in which the groups at positions 2, 4 and 5 have cis-relative stereochemistry, X is hydrogen, alkoxy or hydroxy, Y is vinylene, n is 1 or 2, A.sup.1 is alkylene, the substituents R.sup.1 and R.sup.2 at position 2 of the dioxane ring have a variety of values defined hereinafter, and R.sup.4 is hydroxy, a physiologically acceptable alcohol residue or alkanesulphonamido, and the pharmaceutically acceptable salts thereof. The invention also includes processes for the manufacture and use of the acid derivatives as well as pharmaceutical compositions for therapeutic use in one or more of a variety of diseases such as ischaemic heart disease, cerebrovascular disease, asthmatic disease and/or inflammatory disease.Type: GrantFiled: October 20, 1989Date of Patent: October 1, 1991Assignee: Imperial Chemical Industries PLCInventors: Andrew G. Brewster, George R. Brown, Alan W. Faull, Reginald Jessup, Michael J. Smithers
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Patent number: 4921866Abstract: The invention concerns novel, pharmaceutically useful 1,3-dioxane alkanoic and alkenoic acid derivatives of the formula I in which the groups at positions 2, 4 and 5 of the 1,3-dioxane ring have cis-relative stereochemistry, Y is ethylene or vinylene, n is 1-4, Z is hydrogen or hydroxy, and X is a pyridine containing group (as defined hereinafter); and the pharmaceutically acceptable salts thereof. The invention also includes processes for the manufacture and use of the acid derivatives as well as pharmaceutical compositions for therapeutic use in one or more of a variety of diseases such as ischaemic heart disease, cerebrovascular disease, asthmatic disease and/or inflammatory disease.Type: GrantFiled: April 25, 1988Date of Patent: May 1, 1990Assignee: Imperial Chemical Industries plcInventors: Andrew G. Brewster, George R. Brown, Reginald Jessup, Michael J. Smithers
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Patent number: 4908380Abstract: The invention concerns novel pharmaceutical compositions containing a 4(Z)-6-(2,4-diphenyl-1,3-dioxan-5-yl)-alkenoic acid which antagonizes one or more of the actions of thromboxane A.sub.2, together with a compound which inhibits the synthesis of thromboxane A.sub.2. The compositios are useful as medicines in treating a variety of diseases or medical conditions in which thromboxane A.sub.2 and/or other prostanoid contractile substances are involved.Type: GrantFiled: November 3, 1987Date of Patent: March 13, 1990Assignee: Imperial Chemical Industries plcInventors: Andrew G. Brewster, George R. Brown, Michael J. Smithers
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Patent number: 4895963Abstract: The invention provides a novel group of 4(Z)-6-([2,4,5-cis]-2-alkyl-4-o-hydroxyphenyl-1,3-dioxan-5-yl)hexenoic acids of formula I wherein R is branched alkyl or 3-5 carbon atoms and one of X and Y is hydrogen or fluoro and the other is hydrogen, and their pharmaceutically acceptable salts; together with their pharmaceutical compositions for use in treating a variety of disease conditions. Also provided are methods for the manufacture of the novel compounds. A representative compound is that in which R is t-butyl and X and Y are both hydrogen.Type: GrantFiled: July 12, 1988Date of Patent: January 23, 1990Assignee: Imperial Chemical Industries plcInventors: Andrew G. Brewster, Michael J. Smithers
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Patent number: 4895962Abstract: The invention provides a novel group of 4(Z)-([2,4,5-cis]-2,4-diphenyl-1,3-dioxan-5-yl)hexenoic acids of formula I, wherein X is F, Cl, Br, CF.sub.3, CN, CH.sub.3 O or NO.sub.2 and one of Y and Z is hydrogen or fluoro and the other is hydrogen, and their pharmaceutically acceptable salts; together with their pharmaceutical compositions for use in treating a variety of disease conditions. Also provided are methods for the manufacture of novel compounds. Representative compounds are those in which X is 2-cyano or 2-chloro and Y and Z are both hydrogen.Type: GrantFiled: July 13, 1988Date of Patent: January 23, 1990Assignee: Imperial Chemical Industries plcInventors: Andrew G. Brewster, George R. Brown, Michael J. Smithers
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Patent number: 4803220Abstract: The invention concerns the novel racemic and laevorotatory optically active forms of the thromboxane A.sub.2 antagonist 5(Z)-7-([ 2,4,5-cis]-4-o-hydroxyphenyl-2-trifluoromethyl-1,3-dioxan-5-yl)heptenoic acid of formula I, their salts, pharmaceutical compositions, and processes for their manufacture and intermediates therefor. The pharmaceutical agents and their compositions are of value in certain pulmonary and/or vascular disorders.Type: GrantFiled: June 28, 1985Date of Patent: February 7, 1989Assignee: Imperial Chemical Industries PLCInventors: Andrew G. Brewster, George R. Brown, Michael J. Smithers
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Patent number: 4775685Abstract: The invention provides a novel group of 4(Z)-([2,4,5-cis]-2,4-diphenyl-1,3-dioxan-5-yl)hexenoic acids of formula I, wherein X is F, Cl, Br, CF.sub.3, CN, CH.sub.3 O or NO.sub.2 and one of Y and Z is hydrogen or fluoro and the other is hydrogen, and their pharmaceutically acceptable salts; together with their pharmaceutical compositions for use in treating a variety of disease conditions. Also provided are methods for the manufacture of novel compounds. Representative compounds are those in which X is 2-cyano or 2-chloro and Y and Z are both hydrogen.Type: GrantFiled: May 9, 1986Date of Patent: October 4, 1988Assignee: Imperial Chemical Industries PLCInventors: Andrew G. Brewster, George R. Brown, Michael J. Smithers
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Patent number: 4772625Abstract: The invention provides a novel group of 4(Z)-6-([2,4,5-cis]-2-alkyl-4-o-hydroxyphenyl-1,3-dioxan-5-yl)hexenoic acids of formula I wherein R is branched alkyl of 3-5 carbon atoms and one of X and Y is hydrogen or fluoro and the other is hydrogen, and their pharmaceutically acceptable salts; together with their pharmaceutical compositions for use in treating a variety of disease conditions. Also provided are methods for the manufacture of the novel compounds. A representative compound is that in which R is t-butyl ans X and Y are both hydrogen.Type: GrantFiled: May 9, 1986Date of Patent: September 20, 1988Assignee: Imperial Chemical Industries PLCInventors: Andrew G. Brewster, Michael J. Smithers
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Patent number: 4745198Abstract: The invention concerns novel 4-phenyl-1,3-dioxan-5-ylalkenoic acid derivatives of the formula I having cis relative stereochemistry at positions 4 and 5 of the dioxane ring and wherein Ra and Rb are variously hydrogen, alkyl, halogenoalkyl, alkenyl, and optionally substituted aryl or arylalkyl, Rc is hydroxy, alkoxy or alkanesulphonamido, n is 1 or 2, A is ethylene or vinylene, Y is (2-5C)polymethylene optionally substituted by alkyl, and benzene ring B is optionally substituted phenyl, or, when Rc is hydroxy, a salt thereof. The acid derivatives antagonize one or more of the actions of thromboxane A.sub.2 (TXA.sub.2) and are expected to be of value in those disease conditions in which TXA.sub.2 is involved. The invention also provides pharmaceutical compositions containing an acid derivative of formula I, and processes for their chemical production.Type: GrantFiled: November 12, 1985Date of Patent: May 17, 1988Assignee: Imperial Chemical Industries PLCInventors: Andrew G. Brewster, Peter W. R. Caulkett
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Patent number: 4668698Abstract: The invention concerns novel [(4-phenyl-1,3-dioxan-cis-5-yl)alkyl]phenylalkanoic acids of the formula I wherein Ra and Rb are a variety of substituents including alkyl, alkenyl, halogenoalkyl, phenyl and benzyl, or together form polymethylene; Rc is hydroxy, alkoxy or alkanesulphonamido; A.sup.1 and A.sup.2 are polymethylene; X is oxygen, sulphur or a direct bond; and benzene ring A bears a variety of substituents; and, when Rc is hydroxy, the physiologically acceptable salts thereof. The compounds of formula I are thromboxane antagonists of value in treating a variety of disease conditions. The invention also provides processes for the manufacture of, and pharmaceutical compositions of, the compounds of formula I.Type: GrantFiled: November 9, 1984Date of Patent: May 26, 1987Assignee: Imperial Chemical Industries PLCInventor: Andrew G. Brewster
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Patent number: 4567197Abstract: The invention concerns novel 4-phenyl-1,3-dioxan-5-ylalkenoic acid derivatives of the formula I having cis relative stereochemistry at positions 4 and 5 of the dioxane ring and wherein Ra and Rb are variously hydrogen, alkyl, halogenoalkyl, alkenyl, and optionally substituted aryl or arylalkyl, Rc is hydroxy, alkoxy or alkanesulphonamido, n is 1 or 2, A is ethylene or vinylene, Y is (2-5C)polymethylene optionally substituted by alkyl, and benzene ring B is optionally substituted phenyl, or, when Rc is hydroxy, a salt thereof. The acid derivatives antagonize one or more of the actions of thromboxane A.sub.2 (TXA.sub.2) and are expected to be of value in those disease conditions in which TXA.sub.2 is involved. The invention also provides pharmaceutical compositions containing an acid derivative of formula I, and processes for their chemical production.Type: GrantFiled: May 6, 1983Date of Patent: January 28, 1986Assignee: Imperial Chemical Industries PLCInventors: Andrew G. Brewster, Peter W. R. Caulkett