Abstract: The present invention provides a novel hydrate of 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione, maleic acid.
Type:
Grant
Filed:
February 7, 2002
Date of Patent:
December 16, 2003
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Michael John Sasse, Paul David James Blackler, David C. Lee
Abstract: The invention relates to novel sulfonamide compounds having 5-HT7 receptor antagonist activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders.
Abstract: This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
Type:
Grant
Filed:
October 7, 2002
Date of Patent:
November 25, 2003
Assignee:
SmithKline Beecham Corporation
Inventors:
Michael R. Palovich, Katherine L. Widdowson, Hong Nie
Abstract: This invention relates to the novel use of diphenyl sulfamido in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
Type:
Grant
Filed:
August 30, 2002
Date of Patent:
November 25, 2003
Assignee:
SmithKline Beecham Corporation
Inventors:
Michael R. Palovich, Joseph Weinstock, Katherine L. Widdowson
Abstract: A compound of general formula (I) and physiologically acceptable salts wherein R represents phthalidyl, (2-oxo-5-methyl-1,3-diox-olen-4-yl)methyl or the group CHR4 OCO(O)pR5 wherein R4 is hydrogen or C1-4 alcyl, p is zero or I, R5 is C1-6 alkly, C5-8 cycloalyl (optionally substituted by C1-3 alkyl or carboxyl), C1-4 alkyl substituted by C1-3 alkoxy or carboxy), C1-4 alkyl substituted by one or more groups selected from amino, (C1-4 alkylamino di(C1-4 alkyl)amino or carboxyl, phenyl (optionally substituted by carboxyl or aminoalkyl, C1-4 alkylaminoalkyl or di(C1-4 alkyl)aminoalcyl, or R5 is a 5-8 membered heterocyclic group containing 1 or 2 heteroatoms selected from oxygen or nitrogen, processes for their preparation, pharmaceutical compositions containing them and their use in medicine.
Abstract: A process for preparing a compound of formula (I, I) or a tautomeric form thereof or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof, wherein: J represents O or S; T represents a substituted or unsubstituted aryl group and T1 is O or S; which process comprises reducing a compound of formula (II, II) or a tautomeric form thereof or a salt thereof or a solvate thereof, wherein T and T1 are as defined in relation to formula (I), with a complex hydride reducing agent or a source of a complex hydride reducing agent; and thereafter, as required, preparing a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate of the compound of formula (I) or a tautomeric form thereof.
Type:
Grant
Filed:
November 8, 2001
Date of Patent:
October 14, 2003
Assignee:
SmithKline Beecham plc
Inventors:
Robert Gordon Giles, Norman John Lewis, Stephen Moore, Colin Ripley Pool, John Kirby Quick, Michael Urquhart
Abstract: This invention relates to (E)-&agr;-[2-n-butyl-1-[(4-carboxyphenyl)methyl]-1H-imidazol-5-yl]methylene-2-thiophenepropionic acid arginyl charge-neutralization-complex, a process for its production, compositions containing the compound and methods of using the compound to block angiotensin II receptors and to treat hypertension, congestive heart failure and renal failure.
Type:
Grant
Filed:
December 12, 2001
Date of Patent:
October 7, 2003
Assignee:
SmithKline Beecham Corporation
Inventors:
Manga R Gudipati, John M Jushchyshyn, Nageswara R Palepu, Gopadi M Venkatesh
Abstract: This invention relates to novel compounds of Formula (I) to (VII), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
Abstract: Piperidine derivatives and pharmaceutical derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.
Type:
Grant
Filed:
May 24, 2001
Date of Patent:
August 5, 2003
Assignee:
SmithKline Beecham p.l.c.
Inventors:
David Thomas Davies, Roger Edward Markwell, Neil David Pearson, Andrew Kenneth Takle
Abstract: A process for the preparation of methyl 2-(3-chloropropoxy)-indole-3-carboxylate, which comprises reacting a 3-chloro-3-carboxylate indole compound with 3-chloropropanol in the presence of an acid having a pKa of from 0 to 2.
Abstract: Compounds of the formula (I) are disclosed which are vitronectin receptor antagonists and are useful in the treatment of osteoporosis:
or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
December 17, 2001
Date of Patent:
June 10, 2003
Assignee:
SmithKline Beecham Corporation
Inventors:
William E. Bondinell, William H. Miller, Dirk Heerding, James M. Samanen
Abstract: A compound of formula (I): or a salt thereof, or a solvate thereof, wherein Ar represents substituted or unsubstituted aryl, wherein the optional substituents are selected from alkyl, hydroxy or alkoxy or, if attached to adjacent carbon atoms any two substituents together with the carbon atoms to which they are attached may form a fused heterocyclic ring of five to six atoms wherein one, two or three of the said atoms are oxygen or nitrogen; A represents a C1-4 n-alkylene group wherein each carbon is optionally substituted by 1 or 2 C1-6 alkyl groups; R1 represents hydrogen, alkyl, alkenyl or cycloalkyl; one or two of of the group of R2, R3 and R4 represents nitro the remaining members of the group of R2, R3 and R4 represent hydrogen; X represents a —CO—NH— moiety; and Z represents C2-4 n-alkylene group wherein each carbon is optionally substituted 1 or 2 C1-6 alkyl groups; a process for preparing such compounds, pharmaceutical compositions comprising such compounds and the use of such compo
Abstract: The invention relates to 3-hydroxy-and 3-keto-cyclohetero-substituted leucine compounds that are inhibitors of cysteine proteases, particularly cathepsin K, and are useful in the treatment of diseases in which inhibition of bone loss is a factor. The 3-hydroxy-or 3-keto-moiety is bonded to a tetrahydrothiophene, tetrahydrothiopyran, tetrahydrofuran or tetrahydropyran ring.
Abstract: This invention relates to high drug load granulation of (E)-&agr;-[2-n-butyl-1-[(4-carboxyphenyl)methyl]-1H-imidazol-5-yl]methylene-2-thiophenepropionic acid in the anhydrous form, a process for its production, compositions containing the compound and methods of using the compound to block angiotensin II receptors and to treat hypertension, congestive heart failure and renal failure.