Patents by Inventor Laramie Mary Gaster
Laramie Mary Gaster has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 5972935Abstract: The invention relates to novel heterocyclic compounds of formula (I) or a salt or N-oxide thereof, in which R is a group of formulae (i), (ii) or (iii), where R.sup.1 is hydrogen, halogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, COC.sub.1-6 akyl, C.sub.1-6 alkoxy, hydroxy, hydroxyC.sub.1-6 alkyl, hydroxyC.sub.1-6 alkoxy, C.sub.1-6 alkoxyC.sub.1-6 alkoxy, acyle, nitro, trifluoromethyl, cyano, SR.sup.9, SOR.sup.9, SO.sub.2 R.sup.9, NR.sup.9 CONR.sup.10 R.sup.11, NR.sup.10 SO.sub.2 R.sup.11, SO.sub.2 NR.sup.11 r.sup.11, SO.sub.2 NR.sup.10 R.sup.11, CO.sub.2 R.sup.10, CONR.sup.10 R.sup.11, CO.sub.2 NR.sup.10 R.sup.11, CONR.sup.10 (CH.sub.2).sub.a CO.sub.2 R.sup.11, (CH.sub.2).sub.a NR.sup.10 R.sup.11, ##STR1## (CH.sub.2).sub.a CONR.sup.10 R.sup.11, (CH.sub.2).sub.a COR.sup.11, (CH.sub.2).sub.a CO.sub.2 C.sub.1-6 alkyl, CO.sub.2 (CH.sub.2).sub.a OR.sup.10, NR.sup.10 R.sup.11, N.dbd.CNR.sup.9 NR.sup.10 R.sup.11, NR.sup.10 CO(CH.sub.2).sub.a NR.sup.10 R.sup.11, NR.sup.10 CO.sub.2 R.sup.11, CONHNR.sup.10 R.sup.11, CR.Type: GrantFiled: April 24, 1998Date of Patent: October 26, 1999Assignee: SmithKline Beecham p.l.c.Inventor: Laramie Mary Gaster
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Patent number: 5972979Abstract: Novel heterocyclic derivatives, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments are disclosed.Type: GrantFiled: March 10, 1999Date of Patent: October 26, 1999Assignee: SmithKline Beecham p.l.c.Inventor: Laramie Mary Gaster
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Patent number: 5972937Abstract: The invention relates to heterocyclic families of compounds having pharmacological activity, in particular possessing 5HT.sub.2C receptor antagonist activity processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders.Type: GrantFiled: September 16, 1997Date of Patent: October 26, 1999Assignee: SmithKline Beecham p.l.c.Inventors: Laramie Mary Gaster, Paul Adrian Wyman, Keith Raymond Mulholland, David Thomas Davies
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Patent number: 5972951Abstract: Novel piperidine derivatives of formula (I), processes for their preparation, pharmaceutical compositions containing them and their use as medicaments for the treatment of CNS disorders are disclosed.Type: GrantFiled: October 2, 1997Date of Patent: October 26, 1999Assignee: SmithKline Beecham plcInventors: Laramie Mary Gaster, Francis David King, Paul Adrian Wyman
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Patent number: 5952325Abstract: Novel amide derivatives of formula (I), processes for their preparation, pharmaceutical compositions containing them and their use as medicaments are disclosed.Type: GrantFiled: April 16, 1997Date of Patent: September 14, 1999Assignee: SmithKline Beecham plcInventors: Paul Adrian Wyman, Laramie Mary Gaster, Andrew John Jennings
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Patent number: 5919932Abstract: Biphenyl amide derivatives as 5HT.sub.1D antagonists, processes for their preparation, pharmaceutical compositions containing them and their use for the treatment of CNS disorders.Type: GrantFiled: October 7, 1997Date of Patent: July 6, 1999Assignee: SmithKline Beecham p.l.c.Inventors: Laramie Mary Gaster, Keith Raymond Mulholland
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Patent number: 5905080Abstract: Novel amide and urea derivatives, processes for their preparation, pharmaceutical compositions containing hem and their use as medicaments are disclosed.Type: GrantFiled: February 15, 1996Date of Patent: May 18, 1999Assignee: SmithKline Beecham, p.l.c.Inventors: David Malcolm Duckworth, Laramie Mary Gaster, Sarah Maragaret Jenkins, Andrew John Jennings, Keith Raymond Mulholland
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Patent number: 5889022Abstract: Novel indole, indoline and quinoline derivatives of formula (I) processes for their preparation, pharmaceutical compositions containing them, and their use in medicine is disclosed. A structurally distinct class of compounds have now been discovered and have been found to exhibit 5HT.sub.1-D antagonist activity. In a first aspect, the present invention therefore provides a compound of formula (I) or a salt thereof, in which P is a 5-7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen or sulphur, A, B, m, R.sup.1 -R.sup.8 are defined in the application.Type: GrantFiled: June 20, 1996Date of Patent: March 30, 1999Assignee: SmithKline Beecham, p.l.c.Inventors: Laramie Mary Gaster, Paul Adrian Wyman
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Patent number: 5872134Abstract: The use of a compound of formula (I) or a pharmaceutically acceptable salt thereof for the treatment of artrial arrhythmia, stroke or CNS disordersX--CO--CH.sub.2 --Z (I)whereinX is a monocyclic or polycyclic aromatic group,Z is of sub-formula (h), (j) or (k): ##STR1## and wherein the remaining variables are as defined herein.Type: GrantFiled: January 26, 1998Date of Patent: February 16, 1999Assignee: SmithKline Beecham p.l.c.Inventors: Francis David King, Laramie Mary Gaster, Keith Raymond Mulholland
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Patent number: 5852014Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.Type: GrantFiled: June 2, 1995Date of Patent: December 22, 1998Assignee: SmithKline Beecham p.l.c.Inventors: Laramie Mary Gaster, Paul Adrian Wyman
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Patent number: 5827871Abstract: Use of a compound of general formula (I): ##STR1## wherein R.sup.1 represents hydrogen, halogen, trifluoromethyl, nitro, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, arylC.sub.1-6 alkoxy, --CO.sub.2 R.sup.4, --(CH.sub.2).sub.n CN, --(CH.sub.2).sub.n CONR.sup.5 R.sup.6, --(CH.sub.2).sub.n SO.sub.2 NR.sup.5 R.sup.6, C.sub.1-6 alkanoylamino(CH.sub.2).sub.n, or C.sub.1-6 alkylsulphonylamino(CH.sub.2).sub.n ;R.sup.4 represents hydrogen, C.sub.1-6 alkyl or arylC.sub.1-6 alkyl;R.sup.5 and R.sup.6 each independently represent hydrogen or C.sub.1-6 alkyl, or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached form a ring;n represents 0, 1 or 2; andR.sup.2 and R.sup.3 each independently represent hydrogen, C.sub.1-6 alkyl or benzyl or together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino or hexahydroazepino ring;or a physiologically acceptable salt thereof, in the manufacture of a medicament for the treatment of a condition where a 5-HT.sub.Type: GrantFiled: May 17, 1995Date of Patent: October 27, 1998Assignee: Smithkline Beecham plcInventors: Francis David King, Laramie Mary Gaster, Alberto Julio Kaumann, Rodney Christopher Young
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Patent number: 5817833Abstract: Compounds of formula (I) or a salt thereof: ##STR1## R.sup.1 is hydrogen, halogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, COC.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, hydroxyC.sub.1-6 alkyl, hydroxyC.sub.1-6 alkoxy, C.sub.1-6 alkoxyC.sub.1-6 alkoxy, acyl, nitro, trifluoromethyl, cyano, CHO, SR.sup.9, SOR.sup.9, SO.sub.2 R.sup.9, SO.sub.2 NR.sup.10 R.sup.11, CO.sub.2 R.sup.10, NR.sup.10 SO.sub.2 R.sup.11, CONR.sup.10 R.sup.11, CO.sub.2 NR.sup.10 R.sup.11, CONR.sup.10 (CH.sub.2).sub.p CO.sub.2 R.sup.11, (CH.sub.2).sub.p NR.sup.10 R.sup.11, (CH.sub.2).sub.p CONR.sup.10 R.sup.11, (CH.sub.2).sub.p NR.sup.10 COR.sup.11, (CH.sub.2).sub.p CO.sub.2 C.sub.1-6 alkyl, CO.sub.2 (CH.sub.2).sub.p OR.sup.10, CONHNR.sup.10 R.sup.11, NR.sup.10 R.sup.11, NR.sup.10 CO.sub.2 R.sup.11, NR.sup.10 CONR.sup.10 R.sup.11, CR.sup.10 .dbd.NOR.sup.11, CNR.sup.10 .dbd.NOR.sup.11, where R.sup.10 and R.sup.11 are independently hydrogen or C.sub.1-6 alkyl and p is 1 to 4;R.sup.2 and R.sup.3 are independently hydrogen, halogen, C.sub.Type: GrantFiled: February 21, 1997Date of Patent: October 6, 1998Assignee: SmithKline Beecham p.l.c.Inventor: Laramie Mary Gaster
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Patent number: 5801170Abstract: A compound of formula (I) or a salt thereof: ##STR1## wherein P is a 5 to 7 membered heterocyclic ring selected from the group consisting of thienyl, furyl, pyrrolyl, triazolyl, diazolyl, tetrazolyl, imidazolyl, oxadiazolyl, isothiazolyl, isoxazolyl, thiadiazolyl, pyridyl, pyrimdyl and pyrazinyl;R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen, halogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkenyl, C.sub.1-6 alkoxy, hydroxyC.sub.1-6 alkyl, C.sub.1-6 alkylOC.sub.1-6 alkyl, alkanoyl, optionally substituted phenyl, alkanoyloxy, hydroxy, nitro, trifluoromethyl, cyano, CO.sub.2 R.sup.9,CONR.sup.10 R.sup.11 where R.sup.9, R.sup.10 and R.sup.11 are independently hydrogen or C.sub.1-6 alkyl;R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1-6 alkyl;R.sup.6 is hydrogen, halogen, hydroxy, C.sub.1-6 alkyl or C.sub.1-6 alkoxyR.sup.7 and R.sup.8 are independently hydrogen, C.sub.Type: GrantFiled: June 7, 1996Date of Patent: September 1, 1998Assignee: SmithKline Beecham plcInventors: Laramie Mary Gaster, Francis David King, Paul Adrian Wyman
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Patent number: 5786372Abstract: Compounds of formula (I), or pharmaceutically acceptable salts thereof are provided: ##STR1## in which X.sub.1 --(CH.sub.2).sub.x --X.sub.2 forms a 5-7 membered ring wherein:X.sub.1 is O or S;X.sub.2 is O, S or NR wherein R is hydrogen;x is 1, 2 or 3;R.sub.1 is hydrogen, amino, halo, C.sub.1-6 alkyl, hydroxy or C.sub.1-6 alkoxy;R.sub.2 is hydrogen, halo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, nitro, amino or C.sub.1-6 alkylthio;R.sub.3 is hydrogen, halo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or amino;R.sub.4 and R.sub.5 are independently hydrogen or C.sub.1-6 alkyl;Y is NH;Z is of sub-formula (a): ##STR2## wherein --(CH.sub.2).sub.n.sup.1 is attached at carbon; andn.sup.1 is 0, 1, 2, 3 or 4;q is 0, 1, 2 or 3;R.sub.a is (CH.sub.2).sub.n.sup.2 --R.sub.7 wherein n.sup.2 is 2 or 3 and R.sub.7 is selected from cyano, hydroxyl, C.sub.1-6 alkoxy, phenoxy, C(O)C.sub.1-6 alkyl, COC.sub.6 H.sub.5, --CONR.sub.8 R.sub.9, NR.sub.8 COR.sub.9, SO.sub.2 NR.sub.8 R.sub.9 or NR.sub.8 SO.sub.2 R.sub.9 whereinR.sub.8 and R.sub.Type: GrantFiled: December 20, 1996Date of Patent: July 28, 1998Assignee: SmithKline Beecham p.l.c.Inventors: Francis David King, Laramie Mary Gaster, Keith Raymond Mulholland
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Patent number: 5756496Abstract: Compound of formula (1), processes for their preparation and their use as CNS agents are disclosed, in which A is CONR where R is hydrogen or C.sub.1-6 alkyl; Q is an optionally substituted 5 to 7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen or sulphur, R.sup.1 is hydrogen, halogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, COC.sub.1-6 -alkyl, C.sub.1-6 alkoxy, hydroxy, hydroxyC.sub.1-6 alkyl, hydroxyC.sub.1-6 alkoxy, C.sub.1-6 alkoxyC.sub.1-6 alkoxy, acyl, nitro, trifluoromethyl, cyano, SR.sup.9, SOR.sup.9, SO.sub.2 R.sup.9, SO.sub.2 NR.sup.10 R.sup.11, CO.sub.2 R.sup.10, CONR.sup.10 R.sup.11, CO.sub.2 NR.sup.10 R.sup.11, CONR.sup.10 (CH.sub.2).sub.a CO.sub.2 R.sup.11, (CH.sub.2).sub.a NR.sup.10 R.sup.11, (CH.sub.2).sub.a CONR.sup.10 R.sup.11, (CH.sub.2).sub.a NR.sup.10 COR.sup.11, (CH.sub.2).sub.a CO.sub.2 C.sub.1-6 alkyl, CO.sub.2 (CH.sub.2).sub.a OR.sup.10, NR.sup.10 R.sup.11, NR.sup.10 CO.sub.2l R.sup.11, NR.sup.10 CONR.sup.10 R.sup.11, CR.sup.10 =NOR.sup.11, CNR.Type: GrantFiled: November 21, 1996Date of Patent: May 26, 1998Assignee: SmithKline Beecham p.l.c.Inventors: Peter Ham, Laramie Mary Gaster, David Francis King, David Malcolm Duckworth
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Patent number: 5741801Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof, and the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof:X--CO--CH.sub.2 --Z (I)whereinX is a monocyclic or polycyclic aromatic group,Z is of sub-formula (h), (j) or (k): ##STR1## wherein n.sup.1 is 1, 2, 3 or 4; n.sup.2 is 0, 1, 2, 3 or 4; n.sup.3 is 2, 3, 4 or 5;q is 0, 1, 2 or 3; p is 0, 1 or 2; m is 0, 1 or 2;R.sub.5 is hydrogen, C.sub.1-12 alkyl, aralkyl or R.sub.5 is (CH.sub.2).sub.z --R.sub.10 wherein z is 2 or 3 and R.sub.10 is selected from cyano, hydroxyl, C.sub.1-6 alkoxy, phenoxy, C(O)C.sub.1-6 alkyl, COC.sub.6 H.sub.5, --CONR.sub.11 R.sub.12, NR.sub.11 COR.sub.12, SO.sub.2 NR.sub.11 R.sub.12 or NR.sub.11 SO.sub.2 R.sub.12 wherein R.sub.11 and R.sub.12 are hydrogen or C.sub.1-6 alkyl; or R.sub.Type: GrantFiled: November 22, 1995Date of Patent: April 21, 1998Assignee: SmithKline Beecham plcInventors: Francis David King, Laramie Mary Gaster, Keith Raymond Mulholland
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Patent number: 5726187Abstract: Fused-ring system N-alkylpiperidinyl-4-methyl carboxylic acid ester or amide derivs. and analogues (D, having formula (I-1)-(I-5), and their salts. The variables are defined herein. The compounds (I) are 5-HT4 receptor antagonists, and are useful for treatment or prophylaxis of gastrointestinal, cardiovascular or CNS disorders. Typically (I) are used for treatment of irritable bowel syndrome (including associated diarrhea and urinary incontinence); for treatment of the nausea and gastric symptoms of gastro-oesophageal reflux disease and dyspepsia; as antiemetics (e.g. against cytotoxin agent or radiation-induced emesis); for preventing atrial fibrillation and other atrial arrhythmias and reducing occurrence of stroke; as anxiolytics; and for treatment of migraine, schizophrenia, Parkinson's disease and Huntington's chorea.Type: GrantFiled: April 14, 1995Date of Patent: March 10, 1998Assignee: SmithKline Beecham plcInventors: Laramie Mary Gaster, Graham Francis Joiner, Keith Raymond Mulholland, Paul Adrian Wyman
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Patent number: 5708174Abstract: Compounds of formula (I), wherein formula I consists of formulae (I-1) to (I-4), which are defined in the specification, and pharmaceutically acceptable salts thereof, and the use of a compound of formula I or a pharmaceutically acceptable salt thereof, and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorder.Type: GrantFiled: April 11, 1995Date of Patent: January 13, 1998Assignee: SmithKline Beecham p.l.c.Inventors: Francis David King, Laramie Mary Gaster, Graham Francis Joiner, Keith Raymond Mulholland, Shirley Katherine Rahman
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Patent number: 5705498Abstract: Compounds of formula (I): ##STR1## wherein X.sup.g is O, S, SO, SO.sub.2, CH.sub.2, CH, N or NR wherein R is hydrogen or C.sub.1-6 alkyl;A is a saturated or unsaturated polymethylene chain of 2-4 carbon atoms;R.sub.1.sup.g and R.sub.2.sup.g are hydrogen or C.sub.1-6 alkyl;R.sub.3.sup.g is hydrogen, halo, C.sub.1-6 alkyl, amino, nitro or C.sub.1-6 alkoxy;R.sub.4.sup.g is hydrogen, halo, C.sub.1-6 alkyl or C.sub.1-6 alkoxy,Y is O or NH, or CO--Y together are a heterocyclic bioisostere;Z is of sub-formula: ##STR2## wherein --(CH.sub.2).sub.n.sup.1 is attached at carbon; and n.sup.1 is 0, 1, 2, 3 or 4;q is 0, 1, 2 or 3;R.sub.a is a straight or branched chain alkylene of chain length 1-6 carbon atoms terminally substituted by R.sub.7 wherein R.sub.7 is 3 to 8 membered heterocyclyl, 5 or 6 membered monocyclic heteroaryl or 9 or 10 membered fused bicyclic heteroaryl linked through carbon, or R.sub.7 is C.sub.2-7 alkoxycarbonyl or secondary or tertiary hydroxy substituted C.sub.1-6 alkyl; andR.sub.6 is hydrogen or C.Type: GrantFiled: May 4, 1995Date of Patent: January 6, 1998Assignee: SmithKline Beecham plc.Inventors: Laramie Mary Gaster, Paul Adrian Wyman
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Patent number: 5705509Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X.sub.1 --(CH.sub.2).sub.x --X.sub.2 and the aromatic carbon atoms to which they are attached form 5-7 membered ring wherein X.sub.1 is O or S; X.sub.2 is O, S, NR.sub.5 or NR.sub.6 CO wherein R.sub.5 is hydrogen or C.sub.1-6 alkyl; or one of X.sub.1 and X.sub.2 is O, S or CH.sub.2 and the other is CH.sub.2 ; x is 1, 2 or 3; R.sub.1 and R.sub.2 together are Q--CH.sub.2 --CH.sub.2, Q--CH.dbd.CH, or Q--CH.dbd.N where Q is linked either to the R.sub.1 or the R.sub.2 substitution position and Q is O, S or NR.sub.t wherein R.sub.t is hydrogen or C.sub.1-6 alkyl; R.sub.3 is hydrogen halo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or amino; R.sub.4.sup.1 and R.sub.4.sup.2 are independently hydrogen or C.sub.1-6 alkyl; Y is O or NH; Z is of sub-formula (a), (b) or (c) and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.Type: GrantFiled: July 28, 1995Date of Patent: January 6, 1998Assignee: SmithKline Beecham plcInventors: Laramie Mary Gaster, Paul Adrian Wyman