Patents by Inventor Colin A. Leach
Colin A. Leach 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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Publication number: 20100179109Abstract: Disclosed are compounds of Formula (I) wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.Type: ApplicationFiled: April 4, 2008Publication date: July 15, 2010Inventors: Jonh J. Baldwin, Salvacion Cacatian, David Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Bahman Ghavimi-Alagha, Damiano Ghirlanda, Alexey V. Ishchenko, Lara S. Kallander, Brian Lawhorn, Colin A. Leach, Qing Lu, Gerard McGeehan, Jaclyn R. Patterson, Robert D. Simpson, Suresh B. Singh, Patrick Stoy, Lamont R. Terrell, Colin Tice, Zhenrong Xu, Jing Yuan, Catherine C. K. Yuan, Jing Zhang, Wei Zhao
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Publication number: 20090275581Abstract: Disclosed are compounds according to Formula I: wherein the variables are defined herein. Such compounds are can bind aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described herein are methods of antagonizing aspartic protease inhibitors in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a compound according to Formula I.Type: ApplicationFiled: April 5, 2007Publication date: November 5, 2009Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty, Lara S. Kallander, Colin A. Leach, Brian Lawhorn, Qing Lu, Lamont R. Terrell, Bahman Ghavini-Alagha, Jing Zhang, Damiano Ghirlanda, Xiaoping Hou, Simon Semus
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Patent number: 5432182Abstract: Substituted 4-aminoquinazoline derivatives which are inhibitors of gastric acid secretion. A compound of the invention are the salts of strong acids of 3-butyryl-4-(2-methylphenylamino)-8-(hydroxymethyl)quinoline.Type: GrantFiled: January 29, 1992Date of Patent: July 11, 1995Assignee: SmithKline Beecham Intercredit B.V.Inventors: Robert J. Ife, Colin A. Leach
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Patent number: 5420135Abstract: Substituted quinoline derivatives are described as inhibitors bone resorption with in particular, the compound 1-(2-methylphenyl)imidazo[4,5-c]quinoline hydrochloride.Type: GrantFiled: December 10, 1990Date of Patent: May 30, 1995Assignee: Smith Kline & French Laboratories LimitedInventors: Thomas H. Brown, Robert J. Ife, Colin A. Leach, David J. Keeling
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Patent number: 5409943Abstract: The present invention relates to N-pyridylamidine and N-pyridylguanidine derivatives of general formula (I) in which: Ar.sup.1 is an optionally substituted phenyl ring; Ar.sup.2 is an optionally substituted phenyl ring; R.sup.1 is hydrogen or C.sub.1-4 alkyl; R.sup.2 is hydrogen or C.sub.1-4 alkyl; R.sup.3 is hydrogen or C.sub.1-4 alkyl; R.sup.4 is hydrogen, halogen, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; X is CH.sub.2 or NR.sup.5, and R.sup.5 is hydrogen or C.sub.1-4 alkyl, and the salts thereof, and their use in therapy as gastric acid secretion inhibitors.Type: GrantFiled: July 20, 1994Date of Patent: April 25, 1995Assignee: SmithKline Beecham Intercredit B.V.Inventors: Robert J. Ife, Colin A. Leach, Dashyant Dhanak
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Patent number: 5280026Abstract: Thienopyrimidine compounds are disclosed as inhibitors of the H.sup.+ K.sup.+ ATPase enzyme useful in the treatment of gastric acid secretion. A compound of the invention is 2-(2-methylphenylamino)-4-(N-methylphenylamino)thieno[3,2-d]pyrimidine.Type: GrantFiled: November 24, 1992Date of Patent: January 18, 1994Assignee: SmithKline Beecham Intercredit B.V.Inventors: Thomas H. Brown, Robert J. Ife, Colin A. Leach
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Patent number: 5200417Abstract: Isoquinoline compounds, compositions containing them and their use in the inhibition of gastric acid secretion in mammals. A compound of the invention is 1-[(2-Methoxyphenylmethyl)amino]isoquinoline hydrochloride.Type: GrantFiled: April 4, 1990Date of Patent: April 6, 1993Assignee: Smithkline Beecham Intercredit B.V.Inventors: Thomas H. Brown, Robert J. Ife, Colin A. Leach
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Patent number: 5143920Abstract: Substituted 4-aminoquinazoline derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkoxy C.sub.1-6 alkyl,C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkyl C.sub.1-6 alkyl, phenyl C.sub.1-6 alkyl, the phenyl group being optionally substituted;R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, amino, C.sub.1-6 alkylthio, halogen, cyano, hydroxy, C.sub.1-6 alkanoyl or trifuromethyl;m is 1 to 3;R.sup.3 is hydrogen, C.sub.1-6 alkyl, phenyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-6 alkanoyl, amino, C.sub.1-6 alkylamino, ci-C.sub.1-6 alkylamino, halogen, trifluoromethyl or cyano;n is 1 or 2; andR.sup.4 is hydrogen; or a salt thereof are useful as inhibitors of gastric acid secretion.Type: GrantFiled: February 23, 1989Date of Patent: September 1, 1992Assignee: SmithKline Beckman Intercredit B.V.Inventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach
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Patent number: 5089498Abstract: Substituted 4-aminiquinazoline derivatives of the formula: ##STR1## in which R.sup.1 hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkoxyC.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkylC.sub.1-6 alkyl, phenylC.sub.1-6 alkyl, the phenyl group being optionally substituted;R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, amino, C.sub.1-6 alkylthio, halogen, cyano, hydroxy, carbamoyl, carboxy, C.sub.1-6 alkanoyl or trifluromethyl;m is 1 to 3;p is 0 to 4;R.sup.3 is COR.sup.4 ;R.sup.4 is hydroxy, C.sub.1-6 alkoxy, or NR.sup.5 R.sup.6 ;R.sup.5 and R.sup.6 are each hydrogen or C.sub.1-6 alkyl or together with the nitrogen atom to which they are attached form a heterocyclic ring; andR.sup.7 is hydrogen, C.sub.1-6 alkoxy or C.sub.1-6 alkyl;or a salt thereof.Type: GrantFiled: February 23, 1989Date of Patent: February 18, 1992Assignee: SmithKline Beckman Intercredit B.V.Inventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach
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Patent number: 5089504Abstract: Substituted 4-aminoquinazoline derivatives of the formula: ##STR1## in which R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkoxyC.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkylC.sub.1-6 alkyl, phenylC.sub.1-6 alkyl, the phenyl group being optionally substituted;R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, amino, C.sub.1-6 alkylthio, halogen, cyano, hydroxy, carbamoyl, carboxy, C.sub.1-6 alkanoyl or trifluoromethyl;m is 1 to 3;p is 0 to 4;R.sup.3 is COR.sup.4 ;R.sup.4 is hydroxy, C.sub.1-6 alkoxy, or NR.sup.5 R.sup.6 ;R.sup.5 and R.sup.6 are each hydrogen or C.sub.1-6 alkyl or together with the nitrogen atom to which they are attached form a heterocyclic ring; andR.sup.7 is hydrogen, C.sub.1-6 alkoxy or C.sub.1-6 alkyl;or a salt thereof.Type: GrantFiled: February 23, 1989Date of Patent: February 18, 1992Assignee: SmithKline Beckman Intercredit B.V.Inventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach
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Patent number: 5082841Abstract: Aminoquinoline derivatives are described as inhibitors of the H.sup.+ K.sup.+ ATPase enzyme useful in the treatment of gastric acidity. A compound of the invention is 3-butyryl-4-(2-methylphenylamino)-8-(3-dimethylaminopropoxy)quinoline.Type: GrantFiled: August 7, 1990Date of Patent: January 21, 1992Assignee: SmithKline Beecham Intercredit B.V.Inventors: Thomas H. Brown, Robert J. Ife, Colin A. Leach
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Patent number: 5082848Abstract: Substituted 4-aminoquinoline derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxyC.sub.1-6 alkyl; C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkyl-C.sub.1-6 alkyl, phenyl C.sub.1-6 alkyl, the phenyl groups being optionally substituted;R.sup.2 is hydroxy C.sub.1-6 alkyl, C.sub.1-6 alkoxyC.sub.1-6 alkyl or two adjacent groups R.sup.2 together form a C.sub.1-4 alkylenedioxy group;R.sup.3 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, amino, C.sub.1-6 alkylthio, halogen, cyano, hydroxy, C1-6alkanoyl, or trifluromethyl;R.sup.4 is hydrogen, C.sub.1-6 alkyl, phenyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-6 alkanoyl, amino, C.sub.1-6 alkylamino, di- C.sub.1-6 alkyl amino, halogen, or trifluromethyl;n is 1 or 2;q is 0 to 4;m is 1, 2, or 3; andp is 1, 2, 3, or 4 provided that m+p is not greater than 5;or a salt thereof are useful as inhibitors of gastric acid secretion.Type: GrantFiled: February 23, 1989Date of Patent: January 21, 1992Assignee: Smith Kline & French Laboratories, Ltd.Inventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach
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Patent number: 5064833Abstract: 2,4-diaminoquinazoline compounds are inhibitors of the H.sup.+ K.sup.+ ATPase enzyme and useful for the treatment of diseases of the stomach based on excessive gastric acid secretion. A compound of the invention is 2-[2-methyl-4-fluorophenyl)amino]-4-(N-methylphenylamino)quinazoline.Type: GrantFiled: May 8, 1990Date of Patent: November 12, 1991Assignee: Smithkline Beecham Intercredit B.V.Inventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach, David J. Keeling
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Patent number: 5051508Abstract: 1,4-Substituted 2,3-dihydropyrrolo[3,2-c]quinolines which are inhibitors of H.sup.+ K.sup.+ ATPase activity and useful as inhibitors of gastric acid secretion. A compound of the invention is 1-(2-methylphenyl)-4-amino-6-methyl-2,3-dihydropyrrolo[3,2-c]quinoline.Type: GrantFiled: June 19, 1990Date of Patent: September 24, 1991Assignee: SmithKline Beckman Intercredit B.V.Inventors: Thomas H. Brown, Robert J. Ife, Colin A. Leach
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Patent number: 5049567Abstract: Substituted 4-aminoquinazoline derivatives which are inhibitors of gastric acid secretion. A compound of the invention is ethyl 8-methoxy-4-(4-methyl-3-thinenylamino)quinoline-3-carboxylate.Type: GrantFiled: January 9, 1991Date of Patent: September 17, 1991Assignee: SmithKline Beckman Intercredit B.V.Inventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach
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Patent number: 5006535Abstract: Substituted 4-aminoquinazoline derivatives which are inhibitors of gastric acid secretion. A compound of the invention is ethyl 8-methoxy-4-(4-methyl-3-thienyl-amino)quinoline-3-carboxylate.Type: GrantFiled: February 23, 1989Date of Patent: April 9, 1991Assignee: Smith Kline & French Laboratories Ltd.Inventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach
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Patent number: 4935431Abstract: Substituted 4-aminothienopyridine derivatives which are inhibitors of gastric acid secretion. A compound of the invention is 6-butyryl-7-(2-isopropylphenylamino)-thieno[3,2-b]pyridine.Type: GrantFiled: February 23, 1989Date of Patent: June 19, 1990Assignee: SmithKline Beckman Intercredit B.V.Inventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach
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Patent number: 4806550Abstract: This invention relates to novel substituted 4-aminoquinoline derivatives which are inhibitors of gastric acid secretion in mammals. A compound of the invention is 3-butyryl-4-(2-methylphenylamino)-8-methoxyquinoline.Type: GrantFiled: May 12, 1988Date of Patent: February 21, 1989Assignee: SmithKline & French Laboratories LimitedInventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach
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Patent number: 4806549Abstract: This invention relates to novel substituted 4-aminoquinoline derivatives which are inhibitors of gastric acid secretion in mammals. A compound of the invention is 3-butyryl-4-(2-methylphenylamino)-8-methoxyquinoline.Type: GrantFiled: September 3, 1987Date of Patent: February 21, 1989Assignee: Smith Kline & French Laboratories LimitedInventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach