Patents Represented by Attorney, Agent or Law Firm John L. Lemanowicz
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Patent number: 6620818Abstract: A composition and method for preventing/reducing the severity of epithelial cytoxicity side effects such as alopecia, plantar-palmar syndrome, mucositis) induced by chemoptherapy and/or radiation therapy in a patient receiving such therapy wherein a cyclin-dependent kinase II inhibitor is contemporaneously administered to the patient.Type: GrantFiled: August 28, 2001Date of Patent: September 16, 2003Assignee: SmithKline Beecham CorporationInventor: Stephen Thomas Davis
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Patent number: 6586440Abstract: This invention relates to pharmaceutical compositions of 5-alkynyluracil compounds in the form of tablets or capsules.Type: GrantFiled: April 23, 2001Date of Patent: July 1, 2003Assignee: SmithKline Beecham CorporationInventors: Thomas Spector, David J. T. Porter, Saad George Rahim
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Patent number: 6579877Abstract: 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: March 18, 2002Date of Patent: June 17, 2003Assignee: SmithKline Beecham CorporationInventors: Gary Keith Smith, David Stanley Duch, Robert Ferone, Arthur Koch
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Patent number: 6541503Abstract: Compounds of formula (I): wherein X is N, CH, CCF3, or C(C1-12 aliphatic); R4 is sulfonic acid, C1-12 aliphatic-sulfonyl, sulfonyl-C1-12 aliphatic, C1-12 aliphatic-sulfonyl-C1-6 aliphatic, C1-6 aliphatic-amino, R7-sulfonyl, R7 sulfonyl-C1-12 aliphatic, R7-aminosulfonyl, R7-aminosulfonyl-C1-12 aliphatic, R7-sulfonylamino, R7-sulfonylamino-C1-12 aliphatic, aminosulfonylamino, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl-C1-12 aliphatic, (R8)1-3-Arylamino, (R8)1-3-Arylsulfonyl, (R8)1-3-Aryl-aminosulfonyl, (R8)1-3-Aryl-sulfonylamino, Het-amino, Het-sulfonyl, Het-aminosulfonyl, aminoiminoamino, or aminoiminoaminosulfonyl, R5 is hydrogen; and further wherein R4 and R5 are optionally joined to form a fused ring, pharmaceutical formulations comprising them and their use in therapy, especially in the treatment of diseases mediated by CDK2 activity, such as alopecia induced by caType: GrantFiled: August 8, 2001Date of Patent: April 1, 2003Assignee: SmithKline Beecham CorporationInventors: Stephen Thomas Davis, Scott Howard Dickerson, Stephen Vernon Frye, Philip Anthony Harris, Robert Neil Hunter, III, Lee Frederick Kuyper, Karen Elizabeth Lackey, Michael Joseph Luzzio, James Marvin Veal, Duncan Herrick Walker
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Patent number: 6498176Abstract: 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: August 22, 2001Date of Patent: December 24, 2002Assignee: SmithKlineBeecham CorporationInventors: Karen Elizabeth Lackey, Robert Walton McNutt, Jr.
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Patent number: 6492398Abstract: Thiazole-indole compounds 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: December 10, 2002Assignee: SmithKline Beechman CorporationInventor: Ambrish Vyas
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Patent number: 6469022Abstract: A combination of 9,10-dihydro-5-methoxy-9-oxo-N-[4-[2-(1,2,3,4-tetrahydro-6,7,-dimethoxy-2-isoquinolinyl)ethyl]phenyl]-4-acridinecarboxamide or a salt thereof and paclitaxel and its analogs or derivatives.Type: GrantFiled: August 17, 2000Date of Patent: October 22, 2002Assignee: Smith Kline Beecham, CorporationInventor: Jan H. M. Schellens
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Patent number: 6391874Abstract: Substituted heteroaromatic compounds of formula (I) 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, or a salt or solvate thereof; wherein X is N or CH; Y is a group W(CH2), (CH2)W, or W, in which W is O, S(O)m wherein m is 0, 1 or 2, or NRa wherein Ra is hydrogen or a C1-8 alkyl group; R1 represents a phenyl group or a 5- or 6-membered heterocyclic ring containing 1 to 4 heteroatoms selected from N, O or S(O)m, wherein m is as defined above, with the provisos that the ring does not contain two adjacent O or S(O)m atoms and that where the ring contains only N as heteroatom(s) the ring is C-linked to the quinazoline or quinoline ring, R1 being optionally substituted by one or more R3;groups; P=0 to 3; U, R2, R3 are as defined in the application.Type: GrantFiled: December 31, 1998Date of Patent: May 21, 2002Assignee: SmithKline Beecham CorporationInventors: George Stuart Cockerill, Malcolm Clive Carter, Stephen Barry Guntrip, Kathryn Jane Smith
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Patent number: 6387919Abstract: Compounds of formula (I): wherein X is N, CH, CCF3, or C(C1-12 aliphatic); R4 is sulfonic acid, C1-12 aliphatic-sulfonyl, sulfonyl-C1-12 aliphatic, C1-12 aliphatic-sulfonyl-C1-6 aliphatic, C1-6 aliphatic-amino, R7-sulfonyl, R7 sulfonyl-C1-12 aliphatic, R7-aminosulfonyl, R7-aminosulfonyl-C1-12 aliphatic, R7-sulfonylamino, R7-sulfonylamino-C1-12 aliphatic, aminosulfonylamino, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl-C1-12 aliphatic, (R8)1-3-Arylamino, (R8)1-3-Arylsulfonyl, (R8)1-3-Aryl-aminosulfonyl, (R8)1-3-Aryl-sulfonylamino, Het-amino, Het-sulfonyl, Het-aminosulfonyl, aminoiminoamino, or aminoiminoaminosulfonyl, R5 is hydrogen; and further wherein R4 and R5 are optionally joined to form a fused ring, pharmaceutical formulations comprising them and their use in therapy, especially in the treatment of diseases mediated by CDK2 activity, such as alopecia induced by caType: GrantFiled: June 6, 2000Date of Patent: May 14, 2002Assignee: Glaxo Wellcome Inc.Inventors: Stephen Thomas Davis, Scott Howard Dickerson, Philip Anthony Harris, Robert Neil Hunter, III, Lee Frederick Kuyper, Michael Joseph Luzzio, James Marvin Veal, Duncan Herrick Walker
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Patent number: 6369086Abstract: The present invention relates generally to novel substituted oxindole compounds and compositions. Such compounds and compositions have utility as pharmacological agents in treating diseases or conditions alleviated by the inhibition or antagonism of protein kinase activated signalling pathways. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit protein tyrosine kinase and protein serine/threonine kinase inhibition, and which are useful in inhibiting tumor growth via inhibition of such kinases as well as protecting a patient undergoing chemotherapy from chemotherapy induced alopecia.Type: GrantFiled: March 4, 1999Date of Patent: April 9, 2002Assignee: SmithKline Beecham CorporationInventors: Stephen Thomas Davis, Scott Howard Dickerson, Philip Anthony Harris, Robert Neil Hunter, III, Lee Frederick Kuyper, Karen Elizabeth Lackey, Michael Joseph Luzzio, James Marvin Veal, Duncan Herrick Walker
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Patent number: 6358952Abstract: 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 pharmeceutical formulations comprising such combinations are disclosed.Type: GrantFiled: June 6, 1995Date of Patent: March 19, 2002Assignee: SmithKline Beecham CorporationInventors: Gary Keith Smith, David Stanley Duch, Robert Ferone, Arthur Koch
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Patent number: 6350747Abstract: The present invention relates generally to novel amine substituted oxindole compounds and compositions. Such compounds and compositions have utility as pharmacological agents in treating diseases or conditions alleviated by the inhibition or antagonism of protein kinase activated signalling pathways in general, and in particular in the pathological processes which involve aberrant cellular proliferation, such as tumor growth. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit protein tyrosine kinase and protein serine/threonine kinase inhibition, and which are useful in inhibiting tumor growth via inhibition of tumor-related angiogenesis.Type: GrantFiled: February 28, 2000Date of Patent: February 26, 2002Assignee: Glaxo Wellcome Inc.Inventors: Kimberley Caroline Glennon, Lee Frederick Kuyper, Karen Elizabeth Lackey, Robert Walton Mcnutt, Jr.
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Patent number: 6329400Abstract: A family of compounds having the general structural formula where W is a reverse hydroxamic acid group, and R1, R2, R3, R4, R5 and R6 are as described in the specification, or a pharmaceutically acceptable salt, solvate, biohydrolyzable ester, biohydrolyzable amide, affinity reagent, or prodrug thereof.Type: GrantFiled: August 25, 1999Date of Patent: December 11, 2001Assignee: Glaxo Wellcome Inc.Inventors: Robert Carl Andrews, Marc Werner Andersen, Dulce Garrido Bubacz, Joseph Howing Chan, David John Cowan, Michael David Gaul, Daryl Lynn McDougald, David Lee Musso, Michael Howard Rabinowitz, Jennifer Badiang Stanford, Robert William Wiethe
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Patent number: 6322860Abstract: Disclosed is the use of certain polyglutarimides as plastic substrates for use in electronic display applications. These substrates have relatively high Tgs for plastics, and good optical clarity and flatness, with low shrinkage and low birefringence. Also disclosed are electronic display cells made using such polyglutarimide substrates.Type: GrantFiled: November 2, 1998Date of Patent: November 27, 2001Assignee: Rohm and Haas CompanyInventors: Alan Daniel Stein, Michael Paul Hallden-Abberton, Audrey Brenda Liss, Steven David Fields
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Patent number: 6306865Abstract: 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: June 6, 2000Date of Patent: October 23, 2001Assignee: Glaxo Wellcome Inc.Inventors: William Pendergast, Scott Howard Dickerson, Julius Vass Johnson, Robert Ferone
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Patent number: 6297223Abstract: Uracil reductase inactivators, notably a 5-substituted uracil or 5,6-dihydro-5-substituted uracil, potentiate 5-fluorouracil and find use particularly in the treatment of cancer. The 5-substituent is selected from bromo, iodo, cyano, halo-substituted C1-4 alkyl, C2-6 alkenyl, 1-halo-C2-6 alkenyl and halo-substituted C2-6 aklynyl.Type: GrantFiled: June 30, 2000Date of Patent: October 2, 2001Assignee: Glaxo Wellcome Inc.Inventors: Thomas Spector, David J. T. Porter, Saad G. Rahim
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Patent number: 6270863Abstract: Disclosed is a process and apparatus for formation of high quality plastic sheet in a continuous fashion, wherein the plastic sheet produced is capable of use in a variety of optical and electronic display applications.Type: GrantFiled: November 2, 1998Date of Patent: August 7, 2001Assignee: Rohm and Haas CompanyInventors: Jeffrey Lawrence Daecher, Steven David Fields, Toshiaki Yatabe, Kazuo Yahata
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Patent number: 6271898Abstract: Disclosed are uniformly sized domains of liquid crystals, a method for forming the domains, and their performance in polymer dispersed liquid crystal displays. The method provides the ability to form discrete domains of liquid crystal surrounded by a polymer shell, also known as polymer encased liquid crystals, or PELCs. Further, the method provides for the ability to make PELCs that have uniformly sized particles. Displays made comprising uniformly sized PELCs demonstrate markedly improved electro-optical performance over displays made by conventional polymer dispersed liquid crystal processes.Type: GrantFiled: December 23, 1997Date of Patent: August 7, 2001Assignee: Rohm and Haas CompanyInventors: Richard Roy Clikeman, Morris Christopher Wills, Peter Reeves Sperry, Martin Vogel, Jiun-Chen Wu, Willie Lau
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Patent number: 6268374Abstract: The present invention relates to a group of 5-substituted uracil derivatives which are inactivators of uracil reductase and which are particularly useful in cancer chemotherapy, especially in combination with antimetabolite antineoplastic agents such as 5-fluorouracil.Type: GrantFiled: July 23, 1993Date of Patent: July 31, 2001Assignee: Glaxo Wellcome Inc.Inventors: Thomas Spector, David J. T. Porter, Saad G. Rahim
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Patent number: 6268391Abstract: Compounds of general formula (I) wherein: R1 is H or optionally joined with R2 to form a fused ring selected from the group consisting of five to ten membered aryl, heteroaryl or heterocyclyl rings, R2 and R3 are independently H, HET, aryl, C1-12 aliphatic, CN, NO2, halogen, R10, —OR10, —SR10, —S(O)R10, —SO2R10, —NR10R11, —NR11R12, —NR12COR11, —NR12CO2R11, —NR12CONR11R12, —NO12SO2R11, —NR12C(NR 12)NHR11, —COR11, —CO2R11, —CONR12R11, —SO2NR12R11, —OCONR12R11, C(NR12)NR12R11, R6 and R7 are independently halogen, CN, NO2, —CONR10R11, —SO2NR10R11, —NR10R11, or —OR11, where R10 and R11 are as defined below; R8 is OH, NHSO2R12 or NHCOCF3; and their use in therapy, especially in the treatment of disorders mediated by cRaf1 kinase.Type: GrantFiled: April 7, 2000Date of Patent: July 31, 2001Assignee: Glaxo Wellcome Inc.Inventors: Scott Howard Dickerson, Philip Anthony Harris, Robert Neil Hunter, III, David Kendall Jung, Karen Elizabeth Lackey, Robert Walton McNutt, Jr., Michael Robert Peel, James Marvin Veal