Abstract: This invention relates to a process for converting isovanillin to substituted 4-cyano-4-(3,4-disubstitutedphenyl)cyclhexanones. These ketones are useful in preparing certain PDE4 ingibitors wherein the 1-postion keto group is converted to a carboxylic acid group.
Abstract: This invention relates to treating pulmonary diseases such as chronic obstructive pulmonary disease or asthma by administering a phosphodiesterase-4 inhibitor with a beta-adrenergic bronchodilator.
Type:
Grant
Filed:
February 23, 2001
Date of Patent:
September 11, 2001
Assignee:
SmithKline Beecham Corporation
Inventors:
Richard Nieman, Anthony S Rebuck, Theodore J Torphy
Abstract: A method of treatment of bacterial infections in humans or animals which comprises administering, in combination with a &bgr;-lactam antibiotic, a therapeutically effective amount of an amino acid derivative or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof.
Type:
Grant
Filed:
August 17, 1999
Date of Patent:
April 3, 2001
Assignee:
SmithKline Beecham p.l.c.
Inventors:
John Hargreaves Bateson, Desmond John Best
Abstract: This invention relates to ketones, alcohols and amines represented by the likes of of 3-(3-cyclopentyloxy-4-methoxyphenyl)-3-phenylethynylcyclobutan-1-one. They are useful as PDE 4 antagonists.
Type:
Grant
Filed:
April 8, 1999
Date of Patent:
January 9, 2001
Assignee:
SmithKline Beecham Corporation
Inventors:
Siegfried B. Christensen, IV, Cornelia J. Forster
Abstract: Novel spiro piperdine derivatives of formula (I), in which P.sup.1, P.sup.2, R.sup.1, R.sup.2, R.sup.2 ', R.sup.3, m, A, E, G, X, Y, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 have the meanings defined in claim 1 are described, as well as their use for preparing medicaments which have 5HT1D receptor antagonist activity.
Abstract: Mercapto amino acid derivatives of formula (I), wherein R is hydrogen, a salt-forming cation of a in vivo hydrolysable ester-forming group; R.sub.1 is selected from (a) and (b) in which A is a monocyclic aryl or heteroaryl ring and B is a monocyclic aryl, alicyclic or heterocyclic ring, C and D are independently --Z.sub.p --(CR.sub.8 CR.sub.9).sub.q -- or --(CR.sub.8 CR.sub.9).sub.q --Z.sub.p -- where p is 0 or 1, q is 0 to 3 provided that p+q in C is not 0, R.sub.8 and R.sub.9 are independently hydrogen or (C.sub.1-6)alkyl or together represent oxo and Z is O, NR.sub.10 or S(O).sub.x where R.sub.10 is hydrogen, (C.sub.1-6)alkyl or aryl(C.sub.1-6)alkyl and x is 0-2, and wherein C and D are linked ortho to one another on each of the rings A and B in formula (b); R.sub.2 is hydrogen, (C.sub.1-6)alkyl or aryl(C.sub.1-6)alkyl; R.sub.3 is hydrogen, (C.sub.1-6)alkyl optionally substituted by up to three halogen atoms, (C.sub.3-7)cycloalkyl, fused aryl(C.sub.3-7)cycloalkyl, (C.sub.3-7)cycloalkyl(C.sub.2-6)alkyl, (C.
Type:
Grant
Filed:
April 7, 1999
Date of Patent:
December 5, 2000
Assignee:
SmithKline Beecham P.L.C.
Inventors:
John Hargreaves Bateson, Desmond John Best, Brian Peter Clarke, Martin Leonard Gilpin, David Witty
Abstract: Novel azabicyclic derivatives, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments are disclosed.
Abstract: This invention relates to a method for selecting PDE IV inhibitors which have a salutory therapeutic index, and to compounds having these properties.
Type:
Grant
Filed:
May 31, 1995
Date of Patent:
November 7, 2000
Assignee:
SmithKline Beecham Corporation
Inventors:
Mary S. Barnette, Theodore J. Torphy, Siegfried Benjamin Christensen, IV
Abstract: This invention relates to ketones, alcohols and amines and acids represented by the likes of 3-(3-cyclopentyloxy-4-methoxyphenyl)-3-phenylcyanoclobutan-1-one. They are useful as PDE 4 antngionists.
Type:
Grant
Filed:
April 8, 1999
Date of Patent:
September 12, 2000
Assignee:
SmithKline Beecham Corporation
Inventors:
Siegfried B. Christensen, IV, Cornelia J. Forster
Abstract: Invented are substituted thieno (2,3-b)pyrazolo(3,4-d)pyridin-3-ones, pharmaceutical compositions containing these compounds, and methods of using these compounds to enhance erythropoiesis. Also invented are intermediates and processess used in preparing these compounds.
Abstract: The present application is directed to the use of 5HT.sub.1B or 5HT.sub.1D receptor antagonists in the treatment of vascular diseases, in particular angina, Raynaud's syndrome, peripheral vascular syndrome or portal hypertension.
Abstract: Compounds of formula(I) where B is oxygen or sulphur, D is nitrogen, R.sup.6 and R.sup.7 forms a ring, m is 2, R is a substituted latam ring of formula (i) ##STR1## where p is 1, P is a substituted or unsubstituted bicyclic ring containing one or two heteroatoms or P is an unsbustituted or substituted 5- to 7-memebered saturated ring containing one or two heteroatoms; X, Y, Z, E, G, R.sup.3, R.sup.4, R.sup.5, R.sup.8, R.sup.9, and R.sup.10 are as defined in the specification.
Type:
Grant
Filed:
September 18, 1998
Date of Patent:
August 8, 2000
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Laramie Mary Gaster, Peter Ham, Francis David King, Paul Adrian Wyman
Abstract: A novel physical form of (E)-3-[6-[[(2,6-dichlorophenyl)-thio]methyl]-3-(2-phenylethoxy)-2-pyridiny l]-2-propenoic acid and its use in therapy is disclosed.
Type:
Grant
Filed:
December 16, 1997
Date of Patent:
July 25, 2000
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Victor Witold Jacewicz, Michael Anthony Harris, Richard Keith Anderson
Abstract: Azetidinone derivatives of formula (I) in which R.sup.1 and R.sup.2, which may be the same or different, is each selected from hydrogen or C.sub.(1-8) alkyl; R.sup.3 is C.sub.(1-8) alkyl or C.sub.(3-8) cycloalkyl each of which may be optionally substituted; X is a linker group; Y is an aryl group; and n is 0, 1 or 2; and excluding benzyl (4-methylthio-2-oxo-azetidin-1-yl)acetate are inhibitors of the enzyme Lp PLA2 and are of use in therapy, in particular treating atherosclerosis.
Type:
Grant
Filed:
September 30, 1997
Date of Patent:
June 6, 2000
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Deirdre Mary Bernadette Hickey, Dashyant Dhanak, Colin Andrew Leach, Robert John Ife, David Graham Tew
Abstract: Compounds of formula (I) in which B is oxygen, CR.sup.17 R.sup.18 or NR.sup.19 where R.sup.17, R.sup.18 and R.sup.19 are independently hydrogen or C.sub.1-6 alkyl or B is a group S(O).sub.b where b is 1, 2, or 3; and R.sup.6 is a group --(CH.sub.2).sub.p --R.sup.15 where R.sup.15 is OR.sup.16 or SR.sup.16 is hydrogen or C.sub.1-6 alkyl or R.sup.15 is NR.sup.10 R.sup.11 where R.sup.10 and R.sup.11 are as defined for R.sup.1 ; have been found to exhibit 5TH.sub.1B antagonist activity.
Abstract: A compound of formula (Ia) of (Ib), wherein A and B each independently represents hydrogen or one, two or three naphthylidene substituents, which substituents are selected from C.sub.1-6 alkyl, C.sub.1-6 alkoxy, aryl, aryloxy, silyl and silyloxy; R.sup.1 represents phenyl, C.sub.1-6 alkyl, phenyl C.sub.1-6 alkyl or a moiety of formula (a): wherein R.sup.2 represents C.sub.1-6 alkyl, phenyl or benzyl, R.sup.3 represents H or OR.sup.4 wherein R.sup.4 is C.sub.1-6 alkyl or C.sub.1-6 alkylsilyl and n is zero or an integer 1 or 2; and X.sup.- is a counter ion; a process for the preparation of such compounds and the use of such compounds for enantioselectively epoxidising a prochiral olefin.
Abstract: A method of treatment of bacterial infections in humans or animals which comprises administering, in combination with a .beta.-lactam antibiotic, a therapeutically effective amount of an amino acid derivative of Formula (I) or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof, ##STR1## wherein: R is hydrogen, a salt forming cation or an in vivo hydrolysable ester-forming group; R.sub.1 is hydrogen, (C.sub.1-6)alkyl optionally substituted by up to three halogen atoms or by a mercapto, (C.sub.1-6)alkoxy, hydroxy, amino, nitro, carboxy, (C.sub.1-6)alkylcarbonyloxy, (C.sub.1-6)alkoxycarbonyl, formyl or (C.sub.1-6)alkylcarbonyl group, (C.sub.3-7)cycloalkyl, (C.sub.3-7)cycloalkyl(C.sub.2-6)alkyl, (C.sub.2-6)alkenyl, (C.sub.2-6)alkynyl, aryl, aryl(C.sub.1-6)alkyl, heterocyclyl or heterocyclyl(C.sub.1-6)alkyl; R.sub.2 is hydrogen, (C.sub.1-6)alkyl or aryl(C.sub.1-6)alkyl; R.sub.3 is hydrogen, (C.sub.1-6)alkyl optionally substituted by up to three halogen atoms, (C.sub.
Type:
Grant
Filed:
January 13, 1999
Date of Patent:
April 11, 2000
Assignee:
SmithKline Beecham p.l.c.
Inventors:
John Hargreaves Bateson, David R Witty, Brian Charles Gasson, Desmond John Best, David John Payne