Patents by Inventor Graham A. Showell
Graham A. Showell 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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Publication number: 20070110708Abstract: A compound of formula (I) or formula (II) wherein the variables are as defined in the claims.Type: ApplicationFiled: June 18, 2004Publication date: May 17, 2007Inventors: David Miller, Parminder Ruprah, Graham Showell, Louise Walsh
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Patent number: 5618812Abstract: Compounds of Formula (I), and salts and prodrugs thereof, wherein R.sup.1 represents H, optionally substituted C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl; R.sup.2 is NHR.sup.12 or (CH.sub.2).sub.s R.sup.13 where 5 is 0, 1 or 2; R.sup.3 represents C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ; R.sup.4 and R.sup.5 are H, C.sub.1-12 alkyl optionally substituted by NR.sup.9 R.sup.9' or an azacyclic or azabicyclic group, optionally substituted C.sub.4-9 cycloalkyl, C.sub.4-9 cycloalkyl C.sub.1-4 alkyl, aryl, arylC.sub.1-6 alkyl or azacyclic or azabicyclic groups, or R.sup.4 and R.sup.5 together form the residue of an optionally substituted azacyclic or azabicyclic ring system; x is 0, 1, 2 or 3; R.sup.12 is optionally substituted phenyl or pyridyl; R.sup.13 represents a group (A) wherein R.sup.14 is H or C.sub.1-6 alkyl; R.sup.15 is H, C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ; and the dotted line is an optional covalent bond; are CCK and/or gastrin antagonists useful in therapy.Type: GrantFiled: January 26, 1995Date of Patent: April 8, 1997Assignee: Merck Sharp & Dohme, Ltd.Inventors: Jose L. Castro Pineiro, William R. Carling, Mark S. Chambers, Stephen R. Fletcher, Sarah C. Hobbs, Victor G. Matassa, Kevin W. Moore, Graham A. Showell, Michael G. Russell
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Patent number: 5614518Abstract: A class of substituted morpholine derivatives of formula ##STR1## wherein Y represents an optionally substituted bicyclic heteroaromatic ring system containing one or two nitrogen atoms, the ring system comprising a six-membered aromatic or heteroaromatic ring fused to a five- or six-membered heteroaromatic ring; and Z represents an optionally substituted arylalkyl, aryloxymethyl or arylalkoxymethyl group, are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia.Type: GrantFiled: May 20, 1996Date of Patent: March 25, 1997Assignee: Merck Sharp & Dohme Ltd.Inventors: Paul D. Leeson, Graham A. Showell
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Patent number: 5478933Abstract: Disclosed are new benzodiazepine compounds which are useful as cholecystokinin and gastrin receptor antagonists and are useful in the treatment of anxiety, panic and pain.Type: GrantFiled: April 8, 1994Date of Patent: December 26, 1995Assignee: Merck Sharpe & Dohme Ltd.Inventor: Graham A. Showell
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Patent number: 5384408Abstract: 3(R)-[2-(6-trifluoromethylpyrazin)yl]-1-azabicyclo[2.2.2]octane and its salts, and pharmaceutical formulations thereof are useful in medicine. In particular, they are useful for the treatment of neurological and mental illnesses whose clinical manifestations are due to cholinergic deficiency, and for lowering intraocular pressure. The compound may be prepared by dehydroxylating or decarboxylating the corresponding 3-hydroxy- or carboxy-quinuclidine analogue.Type: GrantFiled: March 10, 1993Date of Patent: January 24, 1995Assignee: Merck Sharpe & Dohme Ltd.Inventors: Raymond Baker, Victor J. Lotti, Graham A. Showell
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Patent number: 5324723Abstract: 1,3-Oxazole and 1,3-thiazole compounds of formula I, and their pharmaceutically acceptable salts and prodrugs: ##STR1## wherein X represents oxygen or sulphur;R.sup.1 represents a non-aromatic azacyclic or azabicyclic ring system.Type: GrantFiled: July 1, 1993Date of Patent: June 28, 1994Assignee: Merck Sharpe & Dohme Ltd.Inventors: Raymond Baker, John Saunders, Roger J. Snow, Graham A. Showell
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Patent number: 5242927Abstract: A class of novel oxadiazoles, substituted on one of the ring carbon atoms with a non-aromatic azacyclic or azabicyclic ring and on the other ring carbon atom with a substituent which is convertible in vivo to an amino group, are potent muscarinic agonists, and exhibit improved CNS penetrability and duration of action compared with the corresponding amino compounds. The compounds are therefore useful in the treatment of neurological and mental illnesses.Type: GrantFiled: July 18, 1988Date of Patent: September 7, 1993Assignee: Merck Sharp & Dohme LimitedInventors: Raymond Baker, John Saunders, Angus M. MaCleod, Graham A. Showell
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Patent number: 5219849Abstract: A class of pyrazine, pyrimidine and pyridazine derivatives, substituted by a non-aromatic azabicyclic ring system and optionally by up to two further substituents, is of use in the preparation of medicaments, especially formulations adapted for topical administration to the eye, suitable for the treatment of glaucoma and/or for reducing intraocular pressure.Type: GrantFiled: December 17, 1991Date of Patent: June 15, 1993Assignee: Merck Sharp & DohmeInventors: Victor Lotti, Graham A. Showell
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Patent number: 5177084Abstract: Benzenes, substituted by a non-aromatic, non-fused 1-azabicycle and a substituent of low lipophilicity or a hydrocarbon substituent, their salts and prodrugs are useful in medicine, for example, in treating dementia. Some formulations of such benzenes are novel as are some of the compounds per se. They can be synthesized by methods analogous to those known in the art.Type: GrantFiled: November 19, 1991Date of Patent: January 5, 1993Assignee: Merck Sharp & Dohme Ltd.Inventors: Raymond Baker, Graham A. Showell
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Patent number: 5134146Abstract: The use of compounds for formula (I): ##STR1## or a salt or prodrug thereof; wherein one of X, Y, or Z is an oxygen or sulphur atom and the other two are nitrogen atoms, and the dotted circle represents two double bonds thus forming a 1,3,4-oxadiazole, 1,2,4-oxadiazole, 1,3,4-thiadiazole or 1,2,4-thiadiazole nucleus;R.sup.1 represents a non-aromatic azacyclic or azabicyclic ring system selected from ##STR2## wherein the broken line represents an optional chemical bond; the substituents R.sup.3 and R.sup.4 may be present at any position, including the point of attachment to the oxa- or thia-diazole ring, and independently represent hydrogen, C.sub.1-4 alkyl, halo, C.sub.1-4 alkoxy, hydroxy or carboxy, or R.sup.3 and R.sup.4 together represent carbonyl;the group R.sup.5 represents hydrogen or C.sub.1-4 alkyl; andR.sup.2 represents hydrogen, C.sub.1-8 hydrogen, C.sub.1-8 alkyl optionally substituted by hydroxy or fluoro, C.sub.2-8 alkenyl, OR.sup.7, SR.sup.7, NR.sup.7 R.sup.8, CN, CO.sub.2 R.sup.7, CONR.sup.7 R.Type: GrantFiled: May 29, 1991Date of Patent: July 28, 1992Assignee: Merck Sharp and Dohme Ltd.Inventors: Graham Showell, Victor Lotti
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Patent number: 5106853Abstract: The compound (3R, 4R)-3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-1-azabicyclo[2.2.1]heptane and its salts behave as a functionally selective muscarinic agonist and are useful in the treatment of neurological and mental disorders, preferably in a pharmaceutical formulation comprising the active compound in association with a pharmaceutically acceptable carrier. The compound can be prepared by methods analogous to those known in the art via suitable chiral intermediates and cyclopropyl carboxamide oxime.Type: GrantFiled: May 9, 1990Date of Patent: April 21, 1992Assignee: Merck Sharp & Dohme, Ltd.Inventors: Graham A. Showell, Leslie J. Street
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Patent number: 4366163Abstract: Compounds of the formula (I) ##STR1## and salts and pro-drugs thereof, wherein: R.sub.1 is a hydrogen atom or a lower alkyl group;R.sub.2 is a hydrogen atom or a lower alkyl group;R.sub.3 is a hydrogen atom or a lower alkyl group;R.sub.4 is a hydrogen atom or an alkyl group;R.sub.5 is a lower alkyl or a substituted alkyl group;or R.sub.4 and R.sub.5 are joined so that together with the nitrogen atom to which they are attached they form a 5-, 6- or 7-membered ring optionally containing an oxygen or sulphur atom;R.sub.6 is an electron donating group;R.sub.7 is an electron withdrawing group; andthe NR.sub.4 R.sub.5 and OR.sub.3 moieties are trans having compositions containing them and processes for their preparation.Type: GrantFiled: September 12, 1980Date of Patent: December 28, 1982Assignee: Beecham Group LimitedInventors: John M. Evans, Graham A. Showell, Charles S. Fake
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Patent number: 4363811Abstract: Compounds of the formula (I): ##STR1## and salts and pro-drugs thereof, wherein: R.sub.1 is a hydrogen atom or a lower alkyl group;R.sub.2 is a hydrogen atom or a lower alkyl group;R.sub.3 is a hydrogen atom or a lower alkyl group;R.sub.4 is a hydrogen atom or an alkyl group;R.sub.5 is a lower alkyl or a substituted alkyl group;or R.sub.4 and R.sub.5 are joined so that together with the nitrogen atom to which they are attached they form a 5-, 6- or 7-membered ring optionally containing an oxygen or sulphur atom;R.sub.6 is an electron donating group;R.sub.7 is an electron withdrawing group; andthe NR.sub.4 R.sub.5 and OR.sub.3 moieties are trans having antihypertensive activity, pharmaceutical compositions containing them and processes for their preparation.Type: GrantFiled: September 12, 1980Date of Patent: December 14, 1982Assignee: Beecham Group LimitedInventors: John M. Evans, Graham A. Showell, Charles S. Fake
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Patent number: 4353906Abstract: Compounds of the formula (I): ##STR1## wherein: R.sub.1 and R.sub.2 are independently selected from a hydrogen atom and a C.sub.1-3 alkyl group;R.sub.3 is a hydrogen atom, a C.sub.1-3 alkyl or C.sub.2-4 acyl group;R.sub.4 is a hydrogen atom or C.sub.1-5 alkyl group;R.sub.5 is a C.sub.1-5 alkyl group, a straight chain C.sub.1-3 alkyl group terminally substituted by a chlorine atom; orR.sub.4 and R.sub.5 are joined so that together with the nitrogen atom to which they are attached they form a 5-, 6- or 7-membered ring optionally containing an oxygen or sulphur atom;R.sub.6 is a C.sub.1-5 alkyl group;the NR.sub.4 R.sub.5 and OR.sub.3 moieties are trans; and pharmaceutically acceptable salts thereof having antihypertensive activity, processes for their preparation and their use in compositions.Type: GrantFiled: February 2, 1981Date of Patent: October 12, 1982Assignee: Beecham Group LimitedInventor: Graham A. Showell