Patents by Inventor Graham Andrew Showell
Graham Andrew 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: 20110124626Abstract: A compound having the formula (1) wherein: R1 is a group selected from C3-8 cycloalkyl, C1-6 alkyl, C1-6 alkylene-C3-8 cycloalkyl, each of which groups may optionally be substituted with C1-6 alkyl, halogen, haloC1-6 alkyl or OR15, or R1 is heterocyclyl, optionally substituted with C1-6 alkyl, haloC1-6 alkyl or OR15; n is 0, 1, 2, 3 or 4, the alkylene group —(CH2)m— formed thereby being optionally substituted with a group selected from C1-4 alkyl, C3-8 cycloalkyl and arylsulfonyl; A is a group selected from —N(R2)CO—, —CON(R2)-, —OC(O)—, —C(O)O—, —CO—, —C(R2)(OR3)-, —C(?N—O—R3)-, —C(?CR2R3)-, —C3-8 cycloalkylene-, —C(R2)(haloC1-6alkyl)-, C1-4 alkylene and —C(OR3)(haloC1-6alkyl)-; R2 and R3 are each independently selected from H, C1-6 alkyl, and C3-8 cycloalkyl, or, when A is —N(R2)CO— and X is absent, R2 may form, together with the adjacent nitrogen atom and Z, an N-containing heterocyclyl group, which may optionally be substituted; X is absent or is C14 alkylene or C24 alkenylene, each of which may optionallType: ApplicationFiled: July 17, 2009Publication date: May 26, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Parminder Kaur Pooni, Kevin John Merchant, Catrina Morvern Kerr, Stuart Richard Crosby, Tomohiro Okawa, Mitsuru Sasaki, Mika Gotou, Graham Andrew Showell, Martin Richard Teall
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Publication number: 20090291915Abstract: A compound of any of formulae (I) to (III) wherein at least one of Y and Z includes a Si atom, is of utility in therapy.Type: ApplicationFiled: December 16, 2001Publication date: November 26, 2009Inventors: Graham Andrew Showell, David John Miller
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Publication number: 20090209522Abstract: A compound of formula (I): wherein either B is absent and A and Z are the same or different and are each hydrogen, halogen, alkyl, hydroxy, alkoxy, —CN, —C(Rc)2OH, —N(Rd)C(?X)Rc, —C(?X)N(Rc)(Rd), —S(O)m—Rc, —N(Rc)(Rd)S(O)2, —S(O)2N(Rc)(Rd), —N(Rc)2, aryl optionally substituted with Ra or —O-aryl optionally substituted with Ra; or B is present and is —(CH2)n—, —C(Rb)2— or —O—, or B taken together with A or Z can be —C?C(Rb)—, —C(Rb)?C—, —CH2—CH(Rb)— or —CH(Rb)—CH2—; D is —O— or —S(O)m?—; E is a bond or is —(CH2)n—, —N(Rd)—, —(CH2)nN(Rd)— or —N(Rd)(CH2)n—; F is —C(?X)—; G is —(CH2)n—, —N(Rd)—, —(CH2)nN(Rd)— or —N(Rd)(CH2)n; J is a bond, —O—, —N(RC)C(?X)—, —C(?X)N(Rc)—, —S(O)m?—, —N(Rc)S(O)m—, —S(O)nN(Rc)—, —N(Rc)— or —N(Rg)(Rh); K is a bond, alkylene, cycloalkylene, cycloalkenylene, arylene, heterocycloalkylene, heterocycloalkylene or heteroarylene; and L is hydrogen or a terminal group; has therapeutic utility.Type: ApplicationFiled: June 27, 2006Publication date: August 20, 2009Inventors: Graham Andrew Showell, David John Miller, Angela Glen, Maria Angeles Cubillo De Dios, Kevin Merchant, Ajay Kumar Mandal
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Publication number: 20080261918Abstract: A compound of any of formulas (I) to (V): wherein at least one of Y and Z includes a Si atom, is of utility in therapy.Type: ApplicationFiled: December 16, 2003Publication date: October 23, 2008Inventors: Graham Andrew Showell, Louise Marie Walsh, Ajay Kumar Mandal, David John Miller
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Patent number: 7407649Abstract: A compound of formula (I) or formula (II) wherein the variables are as defined in the claimsType: GrantFiled: June 18, 2004Date of Patent: August 5, 2008Assignee: Paradigm Therapeutics LtdInventors: David John Miller, Parminder Kaur Ruprah, Graham Andrew Showell, Louise Marie Walsh
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Patent number: 6852744Abstract: Novel pyrrolidine derivatives, being useful as chymase inhibitor or intermediate for synthesis of the active compounds, which has the formula (I): wherein R1 is cycloalkyl, substituted or unsubstituted phenyl or naphthyl, indanyl, thienyl, furyl, substituted or unsubstituted indolyl, benzofuryl, substituted or unsubstituted benzothienyl, etc.; R2 is H, alkyl, phenyl-lower alkyl, cycloalkyl or cycloalkyl-lower alkyl; R3 is (i) substituted or unsubstituted monocyclic heterocyclic group, (ii) substituted or unsubstituted benzene- or pyridine-fused heterocyclic group, or (iii) a group (a): R4 and R5 are independently H or OH, but R4 and R5 are not simultaneously H, or both form oxo; n is 0, 1, 2 or 3; or a salt thereof.Type: GrantFiled: August 21, 2001Date of Patent: February 8, 2005Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Takashi Deguchi, Ryotaro Shiratake, Fuminori Sato, Buichi Fujitani, Yayoi Honda, Akihiko Kiyoshi, Mitsue Notake, Graham Andrew Showell, Robert George Boyle, Sukhbinder Singh Klair
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Publication number: 20040102384Abstract: Novel pyrrolidine derivatives, being useful as chymase inhibitor or intermediate for synthesis of the active compounds, which has the formula (I): wherein R1 is cycloalkyl, substituted or unsubstituted phenyl or naphthyl, indanyl, thienyl, furyl, substituted or unsubstituted indolyl, benzofuryl, substituted or unsubstituted benzothienyl, etc.; R2 is H, alkyl, phenyl-lower alkyl, cycloalkyl or cycloalkyl-lower alkyl; R3 is (i) substituted or unsubstituted monocyclic heterocyclic group, (ii) substituted or unsubstituted, benzene- or pyridine-fused heterocyclic group, or (iii) a group (a): R4 and R5 are independently H or OH, but R4 and R5 are not simultaneously H, or both form oxo; n is 0, 1, 2 or 3; or a salt thereof.Type: ApplicationFiled: February 28, 2003Publication date: May 27, 2004Inventors: Takashi Deguchi, Ryotaro Shiratake, Fuminori Sato, Buichi Fujitani, Yayoi Honda, Akihiko Kiyoshi, Mitsue Notake, Graham Andrew Showell, Robert George Boyle, Sukhbinder Singh Klair
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Patent number: 6211219Abstract: A class of substituted aminocyclohexane derivatives are selective agonists of 5-HT1-like receptors, being potent agonists of the human 5-HT1D&agr; receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT1D&agr; receptor subtype relative to the 5-HT1D&bgr; subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.Type: GrantFiled: January 4, 1999Date of Patent: April 3, 2001Assignee: Merck Sharp & Dohme Ltd.Inventors: Angus Murray MacLeod, Graham Andrew Showell, Leslie Joseph Street
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Patent number: 6140347Abstract: A class of compounds of formula (I) wherein Z, E, Q, T, U, V, W, M, R.sup.1, R.sup.7 and R.sup.8 are as defined herein; are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.Type: GrantFiled: October 14, 1998Date of Patent: October 31, 2000Assignee: Merck Sharp & Dohme Ltd.Inventors: Jose Luis Castro Pineiro, Andrew Madin, Joseph George Neduvelil, Graham Andrew Showell, Leslie Joseph Street, Monique Bodil Van Niel
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Patent number: 6127388Abstract: A class of substituted azetidine, pyrrolidine and piperidine derivatives of Formula I are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.Type: GrantFiled: October 26, 1998Date of Patent: October 3, 2000Assignee: Merck Sharp & Dohme Ltd.Inventors: Sylvie Bourrain, Angus Murray MacLeod, Graham Andrew Showell, Leslie Joseph Street
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Patent number: 6054469Abstract: Compounds having formula I, or salts or prodrugs thereof: ##STR1## are selective agonists of the 5-HT.sub.1D.alpha. receptor and are useful in the treatment of migraine and associated conditions.Type: GrantFiled: April 29, 1998Date of Patent: April 25, 2000Assignee: Merck Sharp & Dohme Ltd.Inventors: Sylvie Bourrain, Angus Murray MacLeod, Graham Andrew Showell
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Patent number: 6048878Abstract: A compound of formula (I), or a salt or prodrug thereof, is described, wherein G is attached at position 3 or 4 of the piperidine ring and represents halogen or C.sub.1-6 alkoxy; R1 represents C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, aryl(C.sub.1-6)alkyl or heteroaryl (C.sub.1-6)alkyl, any of which groups may be optionally substituted; processes for its preparation and its use in therapy, particularly in the treatment of migraine.Type: GrantFiled: May 13, 1998Date of Patent: April 11, 2000Assignee: Merck Sharp & Dohme Ltd.Inventors: Jose Luis Castro Pineiro, Ian James Collins, Angus Murray MacLeod, Christopher Richard Moyes, Michael Rowley, Graham Andrew Showell
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Patent number: 5998416Abstract: A class of N-substituted piperazine, piperidine, and tetrahydropyridine derivatives, further subltitutedat the 4-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.Type: GrantFiled: October 26, 1998Date of Patent: December 7, 1999Assignee: Merck Sharp & Dohme Ltd.Inventors: Sylvie Bourrain, Angus Murray MacLeod, Graham Andrew Showell, Leslie Joseph Street
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Patent number: 5994374Abstract: A class of 1-[3-(1H-indol-3-yl)propyl]-4-benzyl-1,2,5,6-tetrahydropyridine derivatives, substituted at the 5-position of the indole nucleus by a 1,2,4-triazol-4-yl moiety, and on the methylene linkage of the benzyl moiety by an alkyl, alkoxy, or alkoxy-alkoxy substituent, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype while possessing at least a 10-fold selective affinity for the 5HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype. They are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D.alpha. receptors is indicated, and are expected to have fewer undesirable cardiovascular and other side effects.Type: GrantFiled: May 8, 1998Date of Patent: November 30, 1999Assignee: Merck Sharp & Dohme Ltd.Inventors: Sylvie Bourrain, Angus Murray MacLeod, Joseph George Neduvelil, Graham Andrew Showell
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Patent number: 5854268Abstract: A class of substituted azetidine, pyrrolidine and piperidine derivatives are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.Type: GrantFiled: January 22, 1997Date of Patent: December 29, 1998Assignee: Merck Sharp & Dohme, Ltd.Inventors: Raymond Baker, Sylvie Bourrain, Jose Luis Castro Pineiro, Mark Stuart Chambers, Alexander Richard Guiblin, Sarah Christine Hobbs, Richard Alexander Jelley, Andrew Madin, Victor Giulio Matassa, Austin John Reeve, Michael Geoffrey Russell, Graham Andrew Showell, Francine Sternfeld, Leslie Joseph Street, Monique Bodil Van Niel
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Patent number: 5807857Abstract: Compounds of formula (I), or a salt or prodrug thereof, wherein Z represents an optionally substituted five-membered heteroaromatic ring selected from furan, thiophene, pyrrole, oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole; E represents a chemical bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms; Q represents a straight or branched alkylene chain containing from 1 to 6 carbon atoms, optionally substituted in any position by a hydroxy group; T represents nitrogen or CH; U represents nitrogen or C--R.sup.2 ; V represents oxygen, sulphur or N--R.sup.3 ; --F--G-- represents --CH2--N--, --CH2--CH-- or --CH.dbd.C--; R.sup.1 represents C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, aryl(C.sub.1-6)alkyl or heteroaryl(C.sub.1-6)alkyl, any of which groups may be optionally substituted; and R.sup.2 and R.sup.3 independently represent hydrogen or C.sub.Type: GrantFiled: November 15, 1996Date of Patent: September 15, 1998Assignee: Merck Sharp & Dohme Ltd.Inventors: Jose Luis Castro Pineiro, Mark Stuart Chambers, Sarah Christine Hobbs, Austin John Reeve, Graham Andrew Showell, Leslie Joseph Street, Victor Giulio Matassa
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Patent number: 5696110Type: GrantFiled: September 5, 1995Date of Patent: December 9, 1997Assignee: Merck, Sharp & Dohme, Ltd.Inventors: Sylvie Bourrain, Stephen Robert Fletcher, Victor Giulio Matassa, Graham Andrew Showell
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Patent number: 5684006Abstract: A class of substituted isoxazole and pyrazole derivatives of formula (I), or a salt thereof of or a prodrug thereof, wherein the broken circle represents two non-adjacent double bonds whereby the five-membered ring containing X and Y is aromatic; one of X and Y represents nitrogen, and the other of X and Y represents oxygen or N--R.sup.5 ; R.sup.1 represents hydrogen, C.sub.1-6 alkyl or trifluoromethyl; R.sup.2 and R.sup.3 independently represent hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano, trifluoromethyl, nitro, --OR.sup.a, --SR.sup.a, --SOR.sup.a, --SO.sub.2 R.sup.a, --SO.sub.2 NR.sup.a R.sup.b, --NR.sup.a R.sup.a, --NR.sup.a CO.sub.2 R.sup.b, --COR.sup.a, --CO.sub.2 R.sup.a or --CONR.sup.a R.sup.b, R.sup.4 represents hydrocarbon or a heterocyclic group; R.sup.5 represents hydrogen or C.sub.1-6 alkyl; and R.sup.a and R.sup.Type: GrantFiled: May 14, 1996Date of Patent: November 4, 1997Assignee: Merck, Sharp & Dohme, Ltd.Inventors: Sylvie Bourrain, Joseph George Neduvelil, Paul David Leeson, Graham Andrew Showell