Patents by Inventor Kevin John Merchant
Kevin John Merchant 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: 20110172204Abstract: A compound of the formula: wherein: R1 represents C1-6 alkyl or H; Y represents —NR2R3 as depicted in formula (B), or a ring of formula (A) wherein a represents the point of attachment to the pyrimidinyl ring; R2 represents C1-4alkyl substituted by C1-3 alkoxy; R3 represents C1-4 alkyl; W represents —(CH2)n—; W1 represents —(CH2)p—; n represents 1 or 2 or 3; p represents 1 or 2; R4 represents C1-4 alkoxy, C1-6 alkyl or halogen; and R5 represents halogen or H, provided that, when R4 represents halogen, R5 is not H, or a pharmaceutically acceptable salt thereof. The compounds of the invention have been found to modulate the histamine H3 receptor.Type: ApplicationFiled: January 7, 2011Publication date: July 14, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Parminder Kaur Pooni, Kevin John Merchant, William John Buffham
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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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Patent number: 7592456Abstract: Compounds of formula (I) are potent and selective 5-HT2A antagonists, useful in treatment of a variety of adverse conditions of the CNS.Type: GrantFiled: November 28, 2005Date of Patent: September 22, 2009Assignee: Merck Sharp & Dohme LimitedInventors: Mark Stuart Chambers, Neil Roy Curtis, Emanuela Gancia, Myra Gilligan, Alexander Charles Humphries, Tamara Ladduwahetty, Robert James Maxey, Kevin John Merchant
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Publication number: 20090170824Abstract: Compounds of formula I: are potent and selective antagonists of the human 5-HT2A receptor, and hence useful in treatment of a variety of adverse conditions of the CNS.Type: ApplicationFiled: December 12, 2008Publication date: July 2, 2009Inventors: Jose Luis Castro Pineiro, Laura Catherine Cooper, Myra Gilligan, Alexander Charles Humphries, Peter Alen Hunt, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Monique Bodil Van Niel, Kevin Wilson
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Patent number: 7468393Abstract: Compounds of formula I: are potent and selective antagonists of the human 5-HT2A receptor, and hence useful in treatment of a variety of adverse conditions of the CNS.Type: GrantFiled: April 27, 2007Date of Patent: December 23, 2008Assignee: Merck Sharp & Dohme Ltd.Inventors: Jose Luis Castro Pineiro, Laura Catherine Cooper, Myra Gilligan, Alexander Charles Humphries, Peter Alan Hunt, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Monique Bodil Van Niel, Kevin Wilson
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Patent number: 7452899Abstract: Compounds of Formula (I): inhibit the processing of APP by gamma-secretase, and hence are useful for treatment or prevention of Alzheimer's disease.Type: GrantFiled: July 29, 2004Date of Patent: November 18, 2008Assignee: Merck Sharp & Dohme LimitedInventors: Michela Bettati, Amanda Louise Boase, Ian Churcher, Tamara Ladduwahetty, Kevin John Merchant, Abdul Quddus
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Publication number: 20080280956Abstract: Compounds of formula I: are potent and selective antagonists of the 5-HT2A receptor, and hence are useful in treatment of various 10 CNS disorders.Type: ApplicationFiled: March 2, 2006Publication date: November 13, 2008Inventors: Myra Gilligan, Alexander Charles Humphries, Tamara Ladduwahetty, Kevin John Merchant
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Patent number: 7279580Abstract: A class of 8-fluoro-3-phenylimidazo[1,2-?]pyridine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group, or by a pyrrolidinonyl group, which is directly attached or bridged by an oxygen atom or by a —NH— or —OCH2— linkage, being selective ligands for GABAA receptors, in particular having high affinity for the ?2 and/or ?3 and/or ?5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.Type: GrantFiled: May 23, 2003Date of Patent: October 9, 2007Assignee: Merck Sharp & Dohme LimitedInventors: Simon Charles Goodacre, David James Hallett, Alexander Charles Humphries, Philip Jones, Sarah Margaret Kelly, Kevin John Merchant, Kevin William Moore, Michael Reader
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Patent number: 7226926Abstract: A class of 8-fluoroimidazo[1,2-?]pyridine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, being selective ligands for GABAA receptors, in particular having high affinity for the ?2 and/or ?3 and/or ?5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.Type: GrantFiled: May 23, 2003Date of Patent: June 5, 2007Assignee: Merck Sharp & Dohme Ltd.Inventors: Wesley Peter Blackaby, Jose Luis Castro Pineiro, Simon Charles Goodacre, David James Hallett, Alexander Charles Humphries, Philip Jones, Kevin John Merchant, Michael Reader
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Patent number: 7217740Abstract: Compounds of formula I: are potent and selective antagonists of the human 5-HT2A receptor, and hence useful in treatment of a variety of adverse conditions of the CNS.Type: GrantFiled: August 26, 2005Date of Patent: May 15, 2007Assignee: Merck Sharp and DohmeInventors: Jose Luis Castro Pineiro, Laura Catherine Cooper, Myra Gilligan, Alexander Charles Humphries, Peter Alan Hunt, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Monique Bodil Van Niel, Kevin Wilson
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Patent number: 7060710Abstract: The present invention provides compounds of formula I: in which: one of X and Y is a nitrogen atom substituted by a group R6? and the other is a carbon atom substituted by an isoxazole group substituted on its carbon atoms by groups R3 and R4; one of R6 and R6? is hydrogen; either all of W1, W2, W3 and W4 are carbon or one of W1, W2, W3 and W4 is nitrogen and the rest are carbon; and R1 and R2 are, independently, a small group, heteroaromatic ring or a 4–7 membered cyclic amine ring; processes for making them; pharmaceutical composition containing them; their use in therapy, particularly for enhancing cognition in conditions such as Alzheimer's Disease; and methods of treatment using them.Type: GrantFiled: November 22, 2002Date of Patent: June 13, 2006Assignee: Merck Sharp & Dohme Ltd.Inventors: Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Francine Sternfeld
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Patent number: 7022724Abstract: The present invention relates to compounds of formula I: in which R1 is a linear group or a five membered heterocycle optionally fused to a phenyl ring, R2 is a 5-membered heterocycle, R3 is chosen from a range of substituents, m is 0–3 and n is 0 or 1; the compounds are generally inverse agonists at GABA-A receptors containing the alpha 5 subunit and so are useful in methods of enhancing cognition in subjects with diminished cognition in diseases such as Alzheimer's Disease.Type: GrantFiled: October 22, 2002Date of Patent: April 4, 2006Assignee: Merck Sharp & Dohme Ltd.Inventors: Amanda Louise Boase, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant
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Publication number: 20040058970Abstract: The present invention relates to compounds of formula I: 1Type: ApplicationFiled: October 22, 2002Publication date: March 25, 2004Inventors: Amanda Louise Boase, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant
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Publication number: 20040006226Abstract: The present invention provides compounds of formula I: 1Type: ApplicationFiled: November 22, 2002Publication date: January 8, 2004Inventors: Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Francine Sternfeld
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Patent number: 6448249Abstract: A substituted triazolopyridazine derivative, its use in cognition enhancement therapy, compositions containing it and processes for its manufacture.Type: GrantFiled: July 24, 2000Date of Patent: September 10, 2002Assignee: Merck Sharp & Dohme Ltd.Inventors: William Robert Carling, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Kevin William Moore, Francine Sternfeld, Leslie Joseph Street
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Patent number: 6444666Abstract: A compound of formula I, or a salt or prodrug thereof: wherein: Z represents C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkenyl, aryl, C3-7 heterocycloalkyl, heteroaryl or di(C1-6)alkylamino, any of which groups may be optionally substituted; R1 represents an optionally substituted five-membered heteroaromatic ring selected from oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole; or R1 represents an optionally substituted six-membered heteroaromatic ring selected from pyrazine, pyrimidine and pyridazine; and R2 represents cyano(C1-6)alkyl, hydroxy(C1-6)alkyl, C3-7 cycloalkyl(C1-6)alkyl, propargyl, C3-7 heterocycloalkylcarbonyl(C1-6)alkyl, aryl(C1-6)alkyl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted; its use in treating anxiety and pharmaceutical compositions comprising it; a subclass of compounds which are useful in enhancing cognition, such as Alzheimer's Disease, is also disclosed.Type: GrantFiled: August 27, 1998Date of Patent: September 3, 2002Assignee: Merck Sharp & Dohme Ltd.Inventors: Tamara Ladduwahetty, Kevin John Merchant, Francine Sternfeld, Leslie Joseph Street
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Precursor compounds to substituted 1,2,4-triazolo[3,4,-a]phathalazine GABA alpha 5 ligands
Patent number: 6310203Abstract: Substituted 1,2,4-Triazolo[3,4-A]phthalazine derivatives that are GABA Alpha 5 ligands are prepared from compounds represented by the formula: in which R1 is hydrogen, halogen, CF3, OCF3, CN or an optionally substituted C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, C2-4alkenyloxy or C2-4alkynyloxy group; R2 is hydrogen, halogen, CF3, OCF3, CN or an optionally substituted C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, C2-4alkenyloxy or C2-4alkynyloxy group; Z is an optionally substituted 5-membered or 6-membered heteroaromatic ring; and G is a leaving group.Type: GrantFiled: April 11, 2000Date of Patent: October 30, 2001Assignee: Merck Sharpe & Dohme LimitedInventors: William Robert Carling, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Kevin William Moore, Francine Sternfeld, Leslie Joseph Street -
Patent number: 6297235Abstract: A compound of formula I, or a salt or prodrug thereof: wherein: Z represents C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkenyl, aryl, C3-7 heterocycloalkyl, heteroaryl or di(C1-6)alkylamino, any of which groups may be optionally substituted; R1 represents an optionally substituted five-membered heteroaromatic ring selected from oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole; or R1 represents an optionally substituted six-membered heteroaromatic ring selected from pyrazine, pyrimidine and pyridazine; and R2 represents cyano(C1-6)alkyl, hydroxy(C1-6)alkyl, C3-7 cycloalkyl(C1-6)alky, propargyl, C3-7 heterocycloalkylcarbonyl(C1-6)alkyl, aryl(C1-6)alkyl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted; its use in treating anxiety and pharmaceutical compositions comprising it; a subclass of compounds which are useful in enhancing cognition, such as Alzheimer's Disease, is also disclosed.Type: GrantFiled: November 12, 1998Date of Patent: October 2, 2001Assignee: Merck Sharp & Dohme Ltd.Inventors: Tamara Ladduwahetty, Kevin John Merchant, Francine Sternfeld, Leslie Joseph Street
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Patent number: 6200975Abstract: Substituted 1,2,4-Triazolo[3,4-A]phthalazine derivatives are GABA Alpha 5 ligands and are represented by the formulaType: GrantFiled: November 12, 1998Date of Patent: March 13, 2001Assignee: Merck Sharp & Dohme LimitedInventors: William Robert Carling, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Kevin William Moore, Francine Sternfeld, Leslie Joseph Street
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Patent number: 5973156Abstract: A class of substituted piperidine and tetrahydropyridine derivatives, linked through the 4-position thereof via an alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, and further substituted at the 1-position by an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl-alkyl, 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.spsb..alpha. receptor subtype whilst processing at least a 10-fold selective affinity for the 5-HT.sub.1D.spsb..alpha. receptor subtype relative to the 5-HT.sub.1D.spsb..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: May 13, 1998Date of Patent: October 26, 1999Assignee: Merck Sharp & Dome Ltd.Inventors: Mark Stuart Chambers, Sarah Christine Hobbs, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant