Patents Represented by Attorney, Agent or Law Firm John L. Lemanowicz
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Patent number: 7189712Abstract: Oxazole derivatives, which are useful as VEGFR2, CDK2, and CDK4 inhibitors are described herein. The described invention also includes methods of making such oxazole derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.Type: GrantFiled: October 10, 2003Date of Patent: March 13, 2007Assignee: SmithKline Beecham CorporationInventors: Matthew Lee Brown, Mui Cheung, Scott Howard Dickerson, Cassandra Gauthier, Philip Anthony Harris, Robert Neil Hunter, Gregory Pacofsky, Michael Robert Peel, Jeffrey Alan Stafford
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Patent number: 7166639Abstract: The present invention provides novel compounds and methods for using them to treat diseases with aminothiophene inhibitors of IKK-? phosphorylation of I?B. In so doing these aminothiophene inhibitors block pathological activation of transcription factor NF-?B in which diseases excessive activation of NF-?B is implicated.Type: GrantFiled: October 4, 2002Date of Patent: January 23, 2007Assignee: SmithKline Beecham CorporationInventors: Zehong Wan, Joelle L. Burgess, James F. Callahan
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Patent number: 7109333Abstract: A process for the preparation of a compound of formula (I) comprising the steps: (a) reacting a compound of formula (II) ?wherein L and L? are suitable leaving groups, with a compound of formula (III) UNH2??(III) to prepare a compound of formula (IV) and subsequently (b) substituting the group R1 by replacement of the leaving group L?.Type: GrantFiled: February 3, 2005Date of Patent: September 19, 2006Assignee: SmithKline Beecham CorporationInventors: Malcolm Clive Carter, George Stuart Cockerill, Stephen Barry Guntrip, Karen Elizabeth Lackey, Kathryn Jane Smith
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Patent number: 7084147Abstract: Heteroaromatic compounds are described, methods for their preparation, pharmaceutical compositions containing them, methods of use, and their use in medicines. In particular, the invention relates to quinazoline and pyridopyrimidine derivatives which exhibit protein tyrosine kinase inhibition.Type: GrantFiled: February 18, 2005Date of Patent: August 1, 2006Assignee: SmithKline Beecham CorporationInventors: George Stuart Cockerill, Karen Elizabeth Lackey
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Patent number: 7071217Abstract: The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis, In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.Type: GrantFiled: August 23, 2001Date of Patent: July 4, 2006Assignee: SmithKline Beecham CorporationInventors: Scott Howard Dickerson, Robert N Hunter, Lee Frederick Kuyper, Karen Elizabeth Lackey, Michael J. Luzzio, Edgar Raymond Wood, III
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Patent number: 7015231Abstract: The present invention is related to aza-oxindole derivatives, compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.Type: GrantFiled: September 24, 2002Date of Patent: March 21, 2006Assignee: SmithKline Beecham CorporationInventors: Karen Elizabeth Lackey, Edgar Raymond Wood, III
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Patent number: 6964977Abstract: The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.Type: GrantFiled: August 23, 2001Date of Patent: November 15, 2005Assignee: SmithKline Beecham CorporationInventors: Philip Anthony Harris, Robert N Hunter, Robert Walton McNutt, Jr., Lee Frederick Kuyper, Karen Elizabeth Lackey, Michael Robert Peel, Edgar Raymond Wood, III
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Patent number: 6943162Abstract: Triazine derivatives of formula (I), which exhibit pharmacological activity at estrogen receptors alpha (ER alpha) and beta (ER beta) are described herein. The described invention also includes compositions and medicaments containing the triazine derivatives as well as processes for the preparation and use of such compounds, compositions and medicaments.Type: GrantFiled: January 23, 2002Date of Patent: September 13, 2005Assignee: SmithKline Beecham CorporationInventors: Ronnie Lee Hale, Brad Richard Henke, Millard Hurst Lambert, III, Amy Tsai Lu, Paul Kenneth Spearing, Philip Stewart Turnbull
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Patent number: 6933299Abstract: Heteroaromatic compounds are described, methods for their preparation, pharmaceutical compositions containing them, methods of use, and their use in medicines. In particular, the invention relates to quinazoline and pyridopyrimidine derivatives which exhibit protein tyrosine kinase inhibition.Type: GrantFiled: June 30, 2000Date of Patent: August 23, 2005Assignee: SmithKline Beecham CorporationInventors: George Stuart Cockerill, Karen Elizabeth Lackey
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Patent number: 6855712Abstract: The use of a protecting agent, for example a folate derivative such as folic acid or leucovorin, in combination with a non-competitive folic acid analogue, for example benzoquinazoline derivatives, for use in reducing the side effects associated with the administration of such non-competitive folic acid analogues, and pharmaceutical formulations comprising such combinations are disclosed.Type: GrantFiled: May 7, 2003Date of Patent: February 15, 2005Assignee: SmithKline Beecham CorporationInventors: Gary Keith Smith, David Stanley Duch, Robert Ferone, Arthur Koch
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Patent number: 6828320Abstract: Substituted heteroaromatic compounds, and in particular substituted quinolines and quinazolines, are protein tyrosine kinase inhibitors. The compounds are described as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of cancer and psoriasis.Type: GrantFiled: January 31, 2002Date of Patent: December 7, 2004Assignee: SmithKline Beecham CorporationInventors: George Stuart Cockerill, Malcolm Clive Carter, Stephen Barry Guntrip, Kathryn Jane Smith
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Patent number: 6818632Abstract: Compounds of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, A, D, X, Y and Z have the meaning as defined in the claims, exhibit protein tyrosine kinase and protein serin/threonine kinase inhibitory activity.Type: GrantFiled: September 27, 2001Date of Patent: November 16, 2004Assignee: SmithKline Beecham CorporationInventors: Kimberley Caroline Glennon, Karen Elizabeth Lackey
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Patent number: 6815439Abstract: Substituted aza-oxindole derivatives useful as cyclin dependent kinase II inhibitors, for preventing/reducing the severity of epithelial cytotoxicity side-effects (e.g., alopecia, plantar-palmar syndrome, mucositis) induced by chemoptherapy and/or radiation therapy in a patient receiving such therapy.Type: GrantFiled: September 23, 2003Date of Patent: November 9, 2004Assignee: SmithKline Beecham CorporationInventors: Philip Anthony Harris, Lee Frederick Kuyper, Karen Elizabeth Lackey, James Marvin Veal
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Patent number: 6803373Abstract: A combination of 9,10-dihydro-5-methoxy-9-oxo-N-[4-[2-(1,2,3,4-tetrahydro-6,7,-dimethoxy-2-isoquinolinyl)ethyl]pheny]-4-acridinecarboxamide or a salt thereof and paclitaxel and its analogs or derivatives.Type: GrantFiled: September 3, 2002Date of Patent: October 12, 2004Assignee: SmithKline Beecham CorporationInventor: Jan H. M. Schellens
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Patent number: 6762188Abstract: Compounds of formula (I) or salts thereof, wherein the dotted Line represents a single or double bond, R1 is alkyl or amino optionally substituted by alkyl, alkanoyl or benzyl group; R2, R3, R4 and R5 are the same or different and each is selected from hydrogen, phenyl, halo, nitro, a group S(O)nR8 wherein n is the integer 0, 1 or 2 and R8 is halo or alkyl or a group NR9R10 wherein R9 and R10 are both hydrogen, a group NR11R12 wherein R11 and R12 are the same or different and each is hydrogen or alkyl, a group OR13 wherein R13 is hydrogen or C1-4 of alkyl optionally substituted by halo; a C1-4 aliphatic group optionally substituted by a group OR14 or NR14R15 wherein R14 and R15 are the same or different and each is hydrogen or alkyl; or two of R2 to R5 are linked together to form a benzo group, or one of R2 to R5 is a group X—Y—R16 wherein X is CH2, NR17, CO or S(O)m and Y is CH2, NR17, O or S(O)m, or X—Y is O, NR17, —CH═CH— or N═N—, are disclosed as pharmacologicType: GrantFiled: September 12, 2001Date of Patent: July 13, 2004Assignee: SmithKline Beecham CorporationInventors: William Pendergast, Scott Howard Dickerson, Julius Vass Johnson, Robert Ferone
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Patent number: 6727256Abstract: Substituted heteroaromatic compounds of formula (I), wherein X is N or CH; Y is CR1 and V is N; or Y is N and V is CR1; or Y is CR1 and V is CR2; or Y is CR2 and V is CR1; R1 represents a group CH3SO2CH2CH2NHCH2—Ar—, wherein Ar is selected from phenyl, furan, thiophene, pyrrole and thiazole, each of which may optionally be substituted by one or two halo, C1-4alkyl or C1-4alkoxy groups; R2 is selected from the group comprising hydrogen, halo, hydroxy, C1-4alkyl, C1-4alkoxy, C1-4alkylamino and di[C1-4alkyl]amino; U represents a phenyl, pyridyl, 3H-imidazolyl, indolyl, isoindolyl, indolinyl, isoindolinyl, 1H-indazolyl, 2,3-dihydro-1H-indazolyl, 1H-benzimidazolyl, 2,3-dihydro-1H-benzimidazolyl or 1H-benzotriazolyl group, substituted by an R3 group and optionally substituted by at least one independently selected R4 group; R3 is selected from a group comprising benzyl, halo-, dihalo- and trihalobenzyl, benzoyl, pyridylmethyl, pyridylmethoxy, phenoxy, benzyloxy, halo-, dihalo- and trihalobenzyType: GrantFiled: June 30, 2000Date of Patent: April 27, 2004Assignee: SmithKline Beecham CorporationInventors: Malcolm Clive Carter, George Stuart Cockerill, Stephen Barry Guntrip, Karen Elizabeth Lackey, Kathryn Jane Smith
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Patent number: 6723726Abstract: Substituted heteroaromatic compounds, and in particular substituted bicyclic heteroaromatic compounds of formula (I), wherein X is N or CH; A represents a fused 5, 6 or 7-membered heterocyclic ring containing 1 to 5 heteroatoms which may be the same or different and which are selected from N, O or S(O)m, wherein m is as defined above, the heterocyclic ring containing a total of 1, 2 or 3 double bonds inclusive of the bond in the pyridine or pyrimidine ring to which it is fused, with the provisos that the heterocyclic ring does not form part of a purine and that the fused heterocyclic ring does not contain two adjacent O or S(O)m atoms.Type: GrantFiled: June 30, 2000Date of Patent: April 20, 2004Assignee: SmithKline Beecham CorporationInventors: George Stuart Cockerill, Malcolm Clive Carter, Stephen Barry Guntrip, Kathryn Jane Smith
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Patent number: 6720332Abstract: Oxindole derivatives, specifically pyrrolo[3,2-f]quinoline-2-ones, which are useful as CDK4 inhibitors are described herein. The described invention also includes methods of making such oxindole derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.Type: GrantFiled: February 27, 2003Date of Patent: April 13, 2004Assignee: SmithKline Beecham CorporationInventors: Scott Howard Dickerson, David Harold Drewry, James Andrew Linn
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Patent number: 6713485Abstract: The present invention relates to substituted heteroaromatic compounds, methods for their preparation, pharmaceutical compositions containing them and their use in medicine. Specifically, the invention relates to quinazoline derivatives useful in treating disorders mediated by protein tyrosine kinase activity, in particular erbB-2 and/or EGFR activity.Type: GrantFiled: February 8, 2002Date of Patent: March 30, 2004Assignee: SmithKline Beecham CorporationInventors: Malcolm Clive Carter, George Stuart Cockerill, Stephen Barry Guntrip, Karen Elizabeth Lackey, Kathryn Jane Smith
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Patent number: 6624171Abstract: Substituted aza-oxindole derivatives useful as cyclin dependent kinase 11 inhibitors, for preventing/reducing the severity of epithelial cytotoxicity side-effects (e.g., alopecia, plantar-palmar syndrome, mucositis) induced by chemoptherapy and/or radiation therapy in a patient receiving such therapy.Type: GrantFiled: August 28, 2001Date of Patent: September 23, 2003Assignee: SmithKline Beecham CorporationInventors: Philip Anthony Harris, Lee Frederick Kuyper, Karen Elizabeth Lackey, James Marvin Veal