Patents by Inventor David LEESON
David LEESON 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: 6080745Abstract: A class of fused tricyclic heteroaromatic compounds of formula (I) as defined in claim 1 or a salt thereof or a prodrug thereof, containing a fused pyrazole, oxazole or pyrimidine ring are ligands for dopamine receptor subtypes within the body and are therefore of use in the treatment and/or prevention of disorders of the dopamine system, such as schizophrenia.Type: GrantFiled: March 12, 1996Date of Patent: June 27, 2000Assignee: Merck Sharp & Dohme LimitedInventors: William Barnaby Davey, Paul David Leeson, Michael Rowley
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Patent number: 5939436Abstract: A class of heteroaromatic compounds incorporating a substituted five-membered heteroaromatic nucleus which contains at least two nitrogen atoms 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 and depression.Type: GrantFiled: June 25, 1997Date of Patent: August 17, 1999Assignee: Merck Sharp & Dohme Ltd.Inventors: William Robert Carling, Paul David Leeson, Kevin William Moore
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Patent number: 5861407Abstract: A class of substituted 1,2,3,6-tetrahydropyridine derivatives are disclosed that are ligands for dopamine receptor subtypes within the body. These compounds are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia or depression.Type: GrantFiled: February 21, 1997Date of Patent: January 19, 1999Assignee: Merck Sharp & Dohme, Ltd.Inventors: Neil Roy Curtis, Janusz Jozef Kulagowski, Paul David Leeson, Ian Michael Mawer, Mark Peter Ridgill
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Patent number: 5849765Abstract: A class of 1,2,3,6-tetrahydropyridine derivatives, substituted in the 4-position by a fused bicyclic heteroaromatic moiety and in the 1-position by an optionally substituted benzyl moiety, are ligands for dopamine receptor subtypes within the body, in particular the D.sub.4 subtype, and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia or depression.Type: GrantFiled: March 7, 1997Date of Patent: December 15, 1998Assignee: Merck Sharp & Dohme, Ltd.Inventors: Neil Roy Curtis, Janusz Jozef Kulagowski, Paul David Leeson, Kevin William Moore, Andrew Pate Owens, Martin Richard Teall
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Patent number: 5830901Abstract: Disclosed is a class of pyrrolo?2,3-b!pyridine derivatives of formula (I) wherein Q represents a moiety of formula Qa or Qb, which are ligands for dopamine receptor subtypes within the body, in particular the dopamine D4 receptor subtype and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, including schizophrenia.Type: GrantFiled: January 27, 1997Date of Patent: November 3, 1998Assignee: Merch Sharp & Dohme LtdInventors: Neil Roy Curtis, Janusz Jozef Kulagowski, Paul David Leeson, Mark Peter Ridgill
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Patent number: 5814644Abstract: Compound of formula (I), or a pharmaceutically acceptable salt thereof or a prodrug thereof wherein E represents --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --; R represents hydrogen or C.sub.1-6 alkyl; Q represents a moiety of formula Qa, Qb, Qc or Qd which are antagonists of dopamine receptor subtypes within the brain, having a selective affinity for the dopamine D.sub.4 receptor subtype over other dopamine receptor subtypes, and are accordingly of benefit in the treatment and/or prevention of psychotic disorders such as schizophrenia whilst manifesting fewer side-effects than those associated with classical neuroleptic drugs.Type: GrantFiled: April 8, 1996Date of Patent: September 29, 1998Assignee: Merck Sharp & Dohme, Ltd.Inventors: Janusz Jozef Kulagowski, Paul David Leeson, Mark Peter Ridgill
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Patent number: 5792768Abstract: A class of benzimidazole derivatives, substituted at the 2-position by a substituted piperazinylmethyl or piperazinylethyl moiety, are antagonists of dopamine receptor subtypes within the brain, having a selective affinity for the dopamine D.sub.4 receptor subtype over other dopamine receptor subtypes, and are accordingly of benefit in the treatment and/or prevention of psychotic disorders such as schizophrenia whilst manifesting fewer side-effects than those associated with classical neuroleptic drugs.Type: GrantFiled: December 20, 1995Date of Patent: August 11, 1998Assignee: Merck, Sharp & Dohme LimitedInventors: Janusz Jozef Kulagowski, Paul David Leeson
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Patent number: 5780475Abstract: Disclosed is a class of 1H-indazole derivatives, substituted at the 3-position by a substituted piperazinylmethyl moiety, which are antagonists of dopamine receptor subtypes within the brain, having a selective affinity for the dopamine D4 receptor subtype over other dopamine receptor subtypes, and are accordingly, of benefit in the treatment and/or prevention of psychotic disorders, such as schizophrenia, while manifesting fewer side-effects than those associated with classical neuroleptic drugs.Type: GrantFiled: December 29, 1995Date of Patent: July 14, 1998Assignee: Merck, Sharp & Dohme LimitedInventors: Raymond Baker, Janusz Jozef Kulagowski, Paul David Leeson, Adrian Leonard Smith
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Patent number: 5763448Abstract: A class of substituted pyrimidine derivatives are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment of disorders of the dopamine system, in particular schizophrenia ##STR1##Type: GrantFiled: March 18, 1996Date of Patent: June 9, 1998Assignee: Merck, Sharp & Dohme LimitedInventors: William Robert Carling, Ian James Collins, Michael Rowley, Paul David Leeson
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Patent number: 5714498Abstract: The invention is directed to substituted benzimidazole compounds which are ligands for dopamine receptor subtypes used in the treatment of the dopamine system.Type: GrantFiled: September 12, 1995Date of Patent: February 3, 1998Assignee: Merck, Sharp, & Dohme, Ltd.Inventors: Janusz Jozef Kulagowski, Paul David Leeson
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Patent number: 5712285Abstract: A class of pyrrolo?2,3 -b!pyridine derivatives, linked via the 3-position thereof by a methylene group to a tetrahydropyridinyl moiety, the latter moiety being substituted in turn by an aryl- or heteroaryl-substituted divalent monocyclic radical, are ligands for dopamine receptorsubtypes within the body, in particular the D.sub.4 subtype, and are accordingly of use in the treatment and/or prevention of disorders of the dopamine system, including schizophrenia and depression.Type: GrantFiled: April 3, 1996Date of Patent: January 27, 1998Assignee: Merck, Sharp & Dohme, Ltd.Inventors: Neil Roy Curtis, Janusz Jozef Kulagowski, Paul David Leeson, Mark Peter Ridgill
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Patent number: 5700809Abstract: Compounds of formula I 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: August 29, 1995Date of Patent: December 23, 1997Assignee: Merck Sharp & Dohme, Ltd.Inventors: Paul David Leeson, Adrian Leonard Smith, Mark Peter Ridgill, Raymond Baker, Neil Roy Curtis, Janusz Jozef Kulagowski
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Patent number: 5700802Abstract: A class of substituted furo?2,3-b!pyridine derivatives are ligands for dopamine receptor subtypes within the body, in particular the D.sub.4 subtype, and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia or depression.Type: GrantFiled: October 9, 1996Date of Patent: December 23, 1997Assignee: Merck Sharp & Dohme, Ltd.Inventors: Neil Roy Curtis, Janusz Jozef Kulagowski, Paul David Leeson
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Patent number: 5686480Abstract: A class of fused tricyclic heteroaromatic compounds of formula (I), or a salt thereof or a prodrug thereof containing a fused pyrazole ring are ligands for dopamine receptor subtypes within the body and are therefore of use in the treatment and/or prevention of disorders of the dopamine system, such as schizophrenia.Type: GrantFiled: March 1, 1996Date of Patent: November 11, 1997Assignee: Merck, Sharp & Dohme, Ltd.Inventors: Ian James Collins, Paul David Leeson, Michael Rowley
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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
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Patent number: 5681836Abstract: The methanesulfonate salt of a class of antipsychotic compounds comprising a benzo?b!furan moiety and a substituted heterocyclic moiety, linked via the 3-position of the benzo?b!furan moiety by a methylene group, which are antagonists of dopamine receptor subtypes within the brain, being extremely potent antagonists of the human dopamine D.sub.4 receptor subtype and having a selective affinity for the D.sub.4 subtype over other dopamine receptor subtypes, possess advantageous qualities in terms of their improved aqueous solubility relative to the corresponding free base and, as such, provide for greater ease of formulation and display enhanced pharmacokinetic properties, including oral absorption.Type: GrantFiled: October 9, 1996Date of Patent: October 28, 1997Assignee: Merck, Sharp & Dohme, Ltd.Inventors: Neil Roy Curtis, Janusz Jozef Kulagowski, Paul David Leeson
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Patent number: 5665722Abstract: A class of chemical compounds comprising a benzo [b] furan moiety and a substituted heterocyclic moiety, linked via the 3-position of the benzo [b] furan moiety by a methylene group, are antagonists of dopamine receptor subtypes within the brain, being extremely potent antagonists of the human dopamine D.sub.4 subtype over other dopamine receptor subtypes, and are accordingly of benefit in the treatment and/or prevention of psychotic disorders such as schizophrenia while manifesting fewer side-effects than those associated with classical neuroleptic drugs.Type: GrantFiled: October 18, 1996Date of Patent: September 9, 1997Assignee: Merck, Sharp & Dohme, Ltd.Inventors: Janusz Jozef Kulagowski, Paul David Leeson, Ian Michael Mawer
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Patent number: 5665732Abstract: A class of chemical compounds comprising a 1-H-indazole moiety and a substituted heterocyclic moiety, linked via the 3-position of the indazole moiety by a methylene 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. In formula (I) R represents hydrogen or C.sub.1-6 alkyl, Q represents a moiety of formula Qa, Qb, or Qc.Type: GrantFiled: September 8, 1995Date of Patent: September 9, 1997Assignee: Merck, Sharp & Dohme Ltd.Inventors: Raymond Baker, Janusz Jozef Kulagowski, Paul David Leeson, Adrian Leonard Smith
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Patent number: 5641787Abstract: The present invention accordingly provides the use of a compound of formula I, or a pharmaceutically acceptable salt thereof or a prodrug thereof: ##STR1## wherein R.sup.1 represents hydrogen or C.sub.1-6 alkyl;Z represents --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --;R.sup.2 represents hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, aryl(C.sub.1-6)alkyl or halogen;R.sup.3, R.sup.4 and R.sup.5 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.sub.a R.sup.b, --NR.sup.a COR.sup.b, --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 ; andR.sup.a and R.sup.b independently represent hydrogen, hydrocarbon or a heterocyclic group;for the manufacture of a medicament for the treatment and/or prevention of psychotic disorders such as schizophrenia.Type: GrantFiled: September 12, 1995Date of Patent: June 24, 1997Assignee: Merck, Sharp & Dohme Ltd.Inventors: Ian Michael Mawer, Howard Barff Broughton, Janusz Jozef Kulagowski, Paul David Leeson