Patents Represented by Attorney, Agent or Law Firm Mary E. McCarthy
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Patent number: 6191304Abstract: This invention relates to certain tricyclic compounds that are integrin receptor antagonists.Type: GrantFiled: April 18, 2000Date of Patent: February 20, 2001Assignee: SmithKline Beecham CorporationInventors: William H. Miller, William E. Bondinell, Thomas Wen Fu Ku
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Patent number: 6172237Abstract: This invention relates to a process for preparing eprosartan by reacting 4-[(2-n-butyl-5-formyl-1H-imidazol-1-yl)methyl]benzoic acid or the bisulfite addition compound of 4-[(2-n-butyl-5-formyl-1H-imidazol-1-yl)methyl]benzoic acid with (2-thienylmethyl)propanedioic acid, mono-ethyl ester.Type: GrantFiled: July 27, 1999Date of Patent: January 9, 2001Assignee: SmithKline Beecham CorporationInventors: Clifford S. Labaw, Joseph Robert Flisak, Li Liu
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Patent number: 6159964Abstract: Compounds of formula (I) are disclosed, wherein: A is a fibrinogen antagonist template; W is a linking moiety of the form --(CHR.sup.g).sub.a --U--(CHR.sup.g).sub.b --V--; Q.sup.1, Q.sup.2, Q.sup.3 and Q.sup.4 are independently N or C--R.sup.y, provided that no more than one Q.sup.1, Q.sup.2, Q.sup.3 and Q.sup.4 is N; R' is H or C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-6 -alkyl or Ar--C.sub.0-6 alkyl; R.sup.g is H or C.sub.1-6 alkyl, Het-C.sub.0-6 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-6 alkyl or Ar--C.sub.0-6 alkyl; R.sup.k is R.sup.g, --C(O)R.sup.g or --C(O)OR.sup.g R.sup.i is H, C.sub.1-6 alkyl, Het-C.sub.0-6 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-6 alkyl, Ar--C.sub.0-6 alkyl, Het-C.sub.0-6 alkyl--U'--C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-6 alkyl--U'--C.sub.1-6 alkyl or Ar--C.sub.0-6 alkyl--U'--C.sub.1-6 alkyl; R.sup.y is H, halo, --OR.sup.g, --SR.sup.g, --CN, --NR.sup.g R.sup.k, --NO.sub.2, --CF.sub.3, CF.sub.3 S(O).sub.r, --CO.sub.2 R.sup.g, --COR.sup.g or --CONR.sup.g.sub.2, or C.sub.Type: GrantFiled: July 27, 1999Date of Patent: December 12, 2000Assignee: SmithKline Beecham CorporationInventors: Fadia E. Ali, William E. Bondinell, Richard M. Keenan, Thomas Wen-Fu Ku, William H. Miller, James Samanen
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Patent number: 6117910Abstract: This invention relates to compounds of the formula: ##STR1## which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, and a method for inhibiting platelet aggregation.Type: GrantFiled: June 13, 1997Date of Patent: September 12, 2000Assignee: SmithKline Beecham CorporationInventors: James Francis Callahan, Richard McCulloch Keenan, Chet Kwon, James Martin Samanen
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Patent number: 6096777Abstract: The present invention relates to a new method of treatment using compounds which are dual non-selective beta-adrenoceptor and alpha-1-adrenoceptor antagonists, in particularly the carbazolyl-(4)-oxypropanolainine compounds of Formula 1, as defined herein, for inhibiting the expression of Fas, a cell surface protein.Type: GrantFiled: February 22, 1999Date of Patent: August 1, 2000Assignees: Boehringer Mannheim Pharmaceuticals Corporation, SmithKline Bechman Corporation Limited Partnership No. 1Inventors: Giora Zeev Feuerstein, Tian-Li Yue
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Patent number: 6069143Abstract: This invention relates to compounds of the formula: ##STR1## which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, and a method for inhibiting platelet aggregation.Type: GrantFiled: January 11, 1996Date of Patent: May 30, 2000Assignee: SmithKline Beecham CorporationInventors: Fadia El-Fehail Ali, William Edward Bondinell, Raul Rolando Calvo, Thomas Wen-Fu Ku, William Henry Miller, James Samanen, Joseph Walter Venslavsky, Tobias Oregon Yellin
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Patent number: 6069158Abstract: This invention relates to certain tricyclic compounds that are integrin receptor antagonists.Type: GrantFiled: June 29, 1999Date of Patent: May 30, 2000Assignee: SmithKline Beecham CorporationInventors: William H. Miller, William E. Bondinell, Thomas Wen Fu Ku
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Patent number: 6034114Abstract: The present invention relates to the use of an angiotensin II receptor antagonist in the manufacture of a medicament for the treatment of left ventricular hypertrophy regression.Type: GrantFiled: August 10, 1999Date of Patent: March 7, 2000Assignee: SmithKline Beecham plcInventor: James Hill
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Patent number: 6031115Abstract: A process for preparing compounds of formula (B) wherein:one of A.sub.1 ' or A.sub.2 ' represents hydrogen and the other represents a group CF.sub.3 --Y-- wherein Y represents --CF.sub.2 --, >C.dbd.O, or --CH(OH)--, or A.sub.1 ' and A.sub.2 ' are groups convertible to A.sub.1 and A.sub.2 respectively.Y.sub.1 represents --O--, --CH.sub.2 -- or NR.sup.O wherein R.sup.O is hydrogen, alkyl or alkylcarbonyl; R.sub.1 and R.sub.2 independently represent hydrogen or alkyl; orR.sub.1 and R.sub.2 together represent a C.sub.2-7 polymethylene moiety;R.sub.3 represents hydrogen, hydroxy, alkoxy or acyloxy and R.sub.4 is hydrogen or R.sub.3 and R.sub.4 together represent a bond;which process comprises reacting a compound of formula (C): ##STR1## wherein the variable A.sub.1 ', A.sub.2 ', Y.sub.1, R.sub.1 and R.sub.2 are as defined above, in the presence of an oxygen source and a chiral catalyst as defined in WO/91/14694.Type: GrantFiled: July 2, 1998Date of Patent: February 29, 2000Assignee: SmithKline Beecham plcInventors: David Bell, Michael Fedouloff, Gillian Turner
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Patent number: 6028087Abstract: Compounds of the formula (I):W--Z--(CR'R.sup.10).sub.r --U--(CR'.sub.2).sub.s --V--A (I)wherein:A is ##STR1## W is .sup.N ; Z is (CH.sub.2).sub.1-2 ;U and V independently are present as CO, CR'.sub.2, C(.dbd.CR'.sub.2), S(O).sub.r, O, NR', CR'OR', CR'(OR")CR'.sub.2, CR'.sub.2 CR'(OR"), C(O)CR'.sub.2, CR'.sub.2 C(O), CONR', NR'CO, OC(O), C(O)O, C(S)O, OC(S), C(S)NR', NR'C(S), S(O).sub.r NR', NR'S(O).sub.r, N.dbd.N, NR'NR', NR'CR'.sub.2, NR'CR'.sub.2, CR'.sub.2 O, OCR'.sub.2, C.tbd.C, CR'.dbd.CR', or CR'(NR'R")C(O);each r independently is 0 to 3;s is 0 to 2;each R' independently is H, C.sub.1-4 alkyl, C.sub.3-7 cycloalky-C.sub.0-4 alkyl, or Ar-C.sub.0-4 alkyl;each R" independently is R', --C(O)R', or --C(O)OR.sup.15 ;R.sup.10 is H, C.sub.1-4 alkyl, or --NR'R';each R.sup.15 independently is C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-4 alkyl, or Ar-C.sub.0-4 alkyl;R.sup.2 is present once or twice as C.sub.1-4 alkyl, J--CO.sub.2 R', CONR', SR', NR'R", C .sub.1-4 alkoxy, hydroxy, CN, CF.sub.Type: GrantFiled: January 21, 1998Date of Patent: February 22, 2000Assignee: SmithKline Beecham CorporationInventors: William Edward Bondinell, James Francis Callahan, William Francis Huffman, Richard McCulloch Keenan, Brian Walter Metcalf, James Samanen, Tobias Oregon Yellin
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Patent number: 6028091Abstract: The present invention relates to the use of an angiotensin II receptor antagonist in the manufacture of a medicament for the treatment of diabetic nephropathy.Type: GrantFiled: August 10, 1999Date of Patent: February 22, 2000Assignee: SmithKline Beecham plcInventor: James Hill
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Patent number: 6025380Abstract: The present invention relates to the use of an angiotensin II receptor antagonist in the manufacture of a medicament for the treatment of macular degeneration.Type: GrantFiled: June 2, 1999Date of Patent: February 15, 2000Assignee: SmithKline Beecham plcInventor: James Hill
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Patent number: 6008213Abstract: Compounds of formula (I) ##STR1## wherein A.sub.1 is C or N; E is a five- or six-membered heteroaromatic or six-membered aromatic ring optionally substituted by R.sup.3 or R.sup.4 ; X.sup.1 --X.sup.2 is CHR.sup.1 --CH, CR.sup.1 .dbd.CH, NR.sup.1 --CH, S(O).sub.u --CH or O--CH; X.sup.3 is CR.sup.5 R.sup.5 ', NR.sup.5, S(O).sub.u or O; R.sup.2 is --OR', --NR'R", --NR'SO.sub.2 R'", --NR'OR', --OCR'.sub.2 C(O)OR', --OCR'.sub.2 OC(O)--R', --OCR'.sub.2 C(O)NR'.sub.2, CF.sub.3 or --COCR'.sub.2 R.sup.2 '; R.sup.3, R.sup.4 and R.sup.7 are independently H, halo, --OR.sup.12, --SR.sup.12, --CN, --NR'R.sup.12, --NO.sub.2, --CF.sub.3, CF.sub.3 S(O).sub.r --, --CO.sub.2 R', --CONR'.sub.2, R.sup.14 --C.sub.0-6 alky-, R.sup.14 --C.sub.1-6 oxoalkyl-, R.sup.14 --C.sub.2-6 alkenyl-, R.sup.14 --C.sub.2-6 alkynyl-, R.sup.14 --C.sub.0-6 alkyloxy-, R.sup.14 --C.sub.0-6 alkylamino- or R.sup.14 --C.sub.0-6 alkyl--S(O).sub.r --; R.sup.6 is W--(CR'.sub.2).sub.q --Z--(CR'R.sup.10)--U--(CR'.sub.2).sub.s --V-- or W'--(CR'.sub.2).sub.Type: GrantFiled: December 19, 1997Date of Patent: December 28, 1999Assignee: SmithKline Beecham CorporationInventors: William E. Bondinell, William H. Miller
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Patent number: 6008214Abstract: This invention relates to compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, which are effective for inhibiting platelet aggregation and bone resorption, pharmaceutical compositions for effecting such activity, and a method for using these compounds.Type: GrantFiled: February 18, 1997Date of Patent: December 28, 1999Assignee: SmithKline Beecham CorporationInventors: Chet Kwon, William Henry Miller
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Patent number: 5977101Abstract: Vitronectin receptor antagonists having the formula: ##STR1## which are useful for the treatment of inflammation, cancer and cardiovascular disorders, such as atherosclerosis and restenosis, and diseases wherein bone resorption is a factor, such as osteoporsis.Type: GrantFiled: December 20, 1996Date of Patent: November 2, 1999Assignee: SmithKline Beecham CorporationInventors: Fadia El-Fehail Ali, William Bondinell, William Francis Huffman, M. Amparo Lago, Richard McCulloch Keenan, Chet Kwon, William Henry Miller, Thomas Nguyen, Dennis T. Takata
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Patent number: 5977179Abstract: 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 C.sub.1-4 n-alkylene group wherein each carbon is optionally substituted by 1 or 2 C.sub.1-6 -alkyl groups; R.sub.1 represents hydrogen, alkyl, alkenyl or cycloalkyl; one or two of the group of R.sub.2, R.sub.3 and R.sub.4 represents nitro the remaining members of the group of R.sub.2, R.sub.3 and R.sub.4 represent hydrogen; X represents a --CO--NH-- moiety; and Z represents C.sub.2-4 n-alkylene group wherein each carbon is optionally substituted 1 or 2 C.sub.Type: GrantFiled: July 2, 1997Date of Patent: November 2, 1999Assignee: SmithKline Beecham p.l.c.Inventors: Guy Marguerite Marie Gerard Nadler, Michel Jean Roger Martin
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Patent number: 5973205Abstract: A process for preparing a compound of formula (I) or an addition salt thereof and/or a solvate thereof: ##STR1## wherein R.sup.1, R.sup.2, R.sup.4 and R.sup.5 are each independently C.sub.1-4 alkoxy and R.sup.3 is C.sub.1-6 alkyl, which process comprises reacting an arylamine of formula (II): ##STR2## wherein R.sup.4 and R.sup.5 are as defined in relation to formula (I) with a .beta.-aminoaldehyde of formula (III): ##STR3## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined in relation to formula (I); and thereafter reducing the intermediate so formed and, optionally, forming an addition salt of the compound of formula (I) and/or a solvate thereof.Type: GrantFiled: April 23, 1998Date of Patent: October 26, 1999Assignee: SmithKline Beecham plcInventors: Thomas Weir Ramsay, Robin Patrick Attrill
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Patent number: 5948811Abstract: A compound of formula (I) or pharmaceutically acceptable salt thereof: ##STR1## wherein either Y is N and R.sub.2 is hydrogen, or Y is C--R.sub.1 ; where either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from the class of hydrogen, C.sub.3-8 cycloalkyl, C.sub.1-6 alkyl optionally interrupted by oxygen or substituted by hydroxy, C.sub.1-6 alkoxy or substituted arminocarbonyl, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkoxy, nitro, cyano, halo, trifluoromethyl, CF.sub.3 S, or a group CF.sub.3 --A--, or a group CF.sub.2 H--A'--, trifluoromethoxy, C.sub.1-6 alkylsulphinyl, perfluoro C.sub.2-6 alkylsulphonyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl, C.sub.1-6 alkoxysulphonyl, aryl, heteroaryl, arylcarbonyl, heteroarylcarbonyl, phosphono, arylcarbonyloxy, heteroarylcarbonyloxy, arylsulphinyl, heteroarylsulphinyl, arylsulphonyl, heteroarylsulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.Type: GrantFiled: May 8, 1997Date of Patent: September 7, 1999Assignee: SmithKline Beegham p.l.c.Inventors: Wai Ngor Chan, John Morris Evans, Geoffrey Stemp, Neil Upton, Robert Nicholas Willette
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Patent number: 5929249Abstract: Angiotensin II receptor antagonists having the formula: ##STR1## which are useful in regulating hypertension and in the treatment of congestive heart failure, renal failure, and glaucoma, pharmaceutical compositions including these antagonists, and methods of using these compounds to produce angiotensin II receptor antagonism in mammals.Type: GrantFiled: January 21, 1998Date of Patent: July 27, 1999Assignee: SmithKline Beecham CorporationInventors: David Taylor Hill, Joseph Weinstock, John Gerald Gleason
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Patent number: 5919953Abstract: There is provided a 2-stage process for making 2H-1-benzopyrans wherein an alpha,beta-unsaturated aldehyde is reacted with an alkanol or an alkane-diol in the presence of a dehydrating compound which is an orthoformate and an aluminum oxide/silicon oxide catalyst to form an aliphatic acetal, which is then condensed in a second stage with a phenol in the presence of base in an organic solvent.Type: GrantFiled: August 11, 1998Date of Patent: July 6, 1999Assignee: SmithKline Beecham p.l.c.Inventors: Pierre Bossard, Michael Gottsponer, Frances Finney