Patents by Inventor Simon James Anthony Grove
Simon James Anthony Grove 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: 8952001Abstract: The invention relates to amino-heteroaryl derivatives having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.Type: GrantFiled: December 20, 2010Date of Patent: February 10, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Simon James Anthony Grove, Angus John Morrison, Craig Jamieson, Ronald Palin, John Kinnaird Ferguson Maclean
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Patent number: 8637551Abstract: The invention relates to 2-(1,2-benzisoxazol-3-yl)benzylamine derivatives having the general Formula (I) wherein R1 represents the group CONR2R3 which is present at one of the positions 5-, 6- or 7- on the 1,2-benzisoxazole ring; R2 and R3 are independently H or (C1-4)alkyl; and R4 is cyclopropyl, 2-pyridyl or phenyl, optionally substituted with one or more halogens; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.Type: GrantFiled: July 6, 2010Date of Patent: January 28, 2014Assignee: Merck Sharp & Dohme B.V.Inventor: Simon James Anthony Grove
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Publication number: 20130023566Abstract: The invention relates to 2-(1,2-benzisoxazol-3-yl)benzylamine derivatives having the general Formula (I) wherein R1 represents the group CONR2R3 which is present at one of the positions 5-, 6- or 7- on the 1,2-benzisoxazole ring; R2 and R3 are independently H or (C1-4)alkyl; and R4 is cyclopropyl, 2-pyridyl or phenyl, optionally substituted with one or more halogens; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.Type: ApplicationFiled: July 6, 2010Publication date: January 24, 2013Applicant: N.V. OrganonInventor: Simon James Anthony Grove
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Publication number: 20120264728Abstract: The invention relates to amino-heteroaryl derivatives having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.Type: ApplicationFiled: December 20, 2010Publication date: October 18, 2012Inventors: Simon James Anthony Grove, Angus John Morrison, Craig Jamieson, Ronald Palin, John Kinnaird Ferguson Maclean
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Patent number: 8188123Abstract: The invention relates to (pyrrolidin-2-yl)phenyl derivatives having the general Formula I wherein R1 is (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, or halo(C1-4)alkyloxy; R2 is H, (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, halo(C1-4)alkyloxy or halogen; R3 is H, (C1-4)alkyl or halo(C1-4)alkyl; R4 is H, (C1-4)alkyl or halo(C1-4)alkyl; R5 is H, (C1-4)alkyl or halo-(C1-4)-alkyl; or R4 and R5, when bonded to the same carbon atom, can together with the carbon atom form a spiro(C3-6)cycloalkyl group, optionally substituted with halogen; R6 is H, (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, halo(C1-4)alkyloxy or halogen; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these (pyrrolidin-2-yl)phenyl derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.Type: GrantFiled: November 3, 2009Date of Patent: May 29, 2012Inventors: Simon James Anthony Grove, Ronald Palin, Ashvinkumar Dhirubhai Mistry, John Kinnaird Ferguson MacLean
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Patent number: 8034804Abstract: The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R1, R2 and R3 are independently H or (C1-4)alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, CF3, halogen, nitro, cyano, NR4R5, NR4COR6, and CONR4R5; R4 and R5 are independently H or (C1-4)-alkyl; or R4 and R5 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR6; R6 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)-alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 20, 2009Date of Patent: October 11, 2011Assignee: N.V. OrganonInventors: Simon James Anthony Grove, Julia Adam-Worrall, Mingqiang Zhang, Robert Gilfillan
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Patent number: 7960365Abstract: The invention provides for compounds having the structure according to the formula I wherein: X is a carbon or nitrogen atom; Ar is phenyl or heteroaromatic ring; R1 is hydrogen, halogen, CN or (1C-4C)alkyl; R2 is hydrogen, halogen or optionally fluorinated (1C-3C)alkoxy; R3 and R5 are independently hydrogen, optionally halogenated (1C-4C)alkyl, optionally halogenated (1C-4C)alkoxy, optionally halogenated aryl(1C-4C)alkoxy, optionally halogenated (1C-4C)alkenyl or hydroxylmethyl; R4 is hydrogen, halogen, optionally halogenated (1C-4C)alkoxy or optionally halogenated aryl(1C-4C)alkoxy; R6 is hydrogen, benzyl, optionally substituted with one or more halogens or (1C-4C)alkyl, or R6 is optionally halogenated (1C-4C)alkyl; each R7 independently is hydrogen, halogen, optionally halogenated (1C-4C)alkyl or optionally halogenated (1C-4C)alkoxy and pharmaceutically suitable acid addition salts thereof for use as glucocorticoid receptor modulators, in particular for treatment of central nervous system disorders.Type: GrantFiled: December 19, 2006Date of Patent: June 14, 2011Assignee: N.V. OrganonInventors: Niall Morton Hamilton, Simon James Anthony Grove, Michael John Kiczun, John Richard Morphy, Brad Sherborne, Peter Thomas Albert Littlewood, Angus Richard Brown, Celia Kingsbury, Michael Ohhlmeyer, Koc-Kan Ho, Steven G. Kultgen
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Publication number: 20100210680Abstract: The present invention relates to a tricyclic heterocyclic derivative of Formula (I) wherein the variables are as defined in the specification. The present invention further relates to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular for the treatment of serotonin-mediated disorders such as obesity, schizophrenia and cognitive dysfunction.Type: ApplicationFiled: September 15, 2008Publication date: August 19, 2010Inventors: Simon James Anthony Grove, Takao Kiyoi, Ashvinkumar Dhirubhai Mistry, Peter Christopher Ray, Grant Wishart
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Publication number: 20100113493Abstract: The invention relates to (pyrrolidin-2-yl)phenyl derivatives having the general Formula I wherein R1 is (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, or halo(C1-4)alkyloxy; R2 is H, (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, halo(C1-4)alkyloxy or halogen; R3 is H, (C1-4)alkyl or halo(C1-4)alkyl; R4 is H, (C1-4)alkyl or halo(C1-4)alkyl; R5 is H, (C1-4)alkyl or halo-(C1-4)-alkyl; or R4 and R5, when bonded to the same carbon atom, can together with the carbon atom form a spiro(C3-6)cycloalkyl group, optionally substituted with halogen; R6 is H, (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, halo(C1-4)alkyloxy or halogen; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these (pyrrolidin-2-yl)phenyl derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.Type: ApplicationFiled: November 3, 2009Publication date: May 6, 2010Inventors: Simon James Anthony Grove, Ronald Palin, Ashvinkumar Dhirubhai Mistry, John Kinnaird Ferguson MacLean
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Patent number: 7566778Abstract: The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R1, R2 and R3 are independently H or (C1-4)alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, CF3, halogen, nitro, cyano, NR4R5, NR4COR6, and CONR4R5; R4 and R5 are independently H or (C1-4-)alkyl; or R4 and R5 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR6; R6 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 1, 2008Date of Patent: July 28, 2009Assignee: N.V. OrganonInventors: Simon James Anthony Grove, Julia Adam-Worrall, Mingqiang Zhang, Robert Gilfillan
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Publication number: 20090163473Abstract: The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R1, R2 and R3 are independently H or (C1-4)alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, CF3, halogen, nitro, cyano, NR4R5, NR4COR6, and CONR4R5; R4 and R5 are independently H or (C1-4)-alkyl; or R4 and R5 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR6; R6 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)-alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: February 20, 2009Publication date: June 25, 2009Inventors: Simon James Anthony Grove, Julia Adam-Worrall, Mingqiang Zhang, Robert Gilfillan
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Patent number: 7504390Abstract: The present invention relates to benzoxazepine derivative having the general formula I, wherein X represents CO or SO2; R1, R2, R3 and R4 are independently selected from H, (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, halogen, nitro, cyano, NR8R9, NR8COR10, and CONR8R9, R5, R6 and R7 are independently H or (C1-4)alkyl; R8 and R9 are independently H or (C1-4)alkyl; or R8 and R9 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR11; R10 is (C1-4)alkyl; R11 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 25, 2007Date of Patent: March 17, 2009Assignee: N.V. OrganonInventors: Simon James Anthony Grove, Mingqiang Zhang, Mohammad Shahid
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Publication number: 20080262221Abstract: The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R1, R2 and R3 are independently H or (C1-4)alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, CF3, halogen, nitro, cyano, NR4R5, NR4COR6, and CONR4R5; R4 and R5 are independently H or (C1-4-)alkyl; or R4 and R5 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR6; R6 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: February 1, 2008Publication date: October 23, 2008Applicant: N.V. OrganonInventors: Simon James Anthony Grove, Julia Adam-Worall, Mingqiang Zhang, Robert Gilfillan
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Publication number: 20080139529Abstract: The present invention relates to benzoxazepine derivative having the general formula I, wherein X represents CO or S02; R1, R2, R3 and R4 are independently selected from H, (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, halogen, nitro, cyano, NR8R9, NR8COR10, and CONR8R9, R5, R6 and R7 are independently H or (C1-4)alkyl; R8 and R9 are independently H or (C1-4)alkyl; or R8 and R9 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR11; R10 is (C1-4)alkyl; R11 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 25, 2007Publication date: June 12, 2008Applicant: N.V. OrganonInventors: Simon James Anthony Grove, Mingqiang Zhang, Mohammad Shahid
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Patent number: 7345036Abstract: The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula (I) or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these (pyrido/thieno)-[f]-oxazepine-5-one derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.Type: GrantFiled: June 10, 2002Date of Patent: March 18, 2008Assignee: N.V. OrganonInventors: Simon James Anthony Grove, Julia Adam-Worall, Minggiang Zhang, Robert Gilfillan
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Patent number: 7307073Abstract: The present invention relates to benzoxazepine derivative having the general formula I, wherein X represents CO or SO2; R1, R2, R3 and R4 are independently selected from H, (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, halogen, nitro, cyano, NR8R9, NR8COR10, and CONR8R9, R5, R6 and R7 are independently H or (C1-4)alkyl; R8 and R9 are independently H or (C1-4)alkyl; or R8 and R9 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR11; R10 is (C1-4)alkyl; R11 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 5, 2002Date of Patent: December 11, 2007Assignee: N.V. OrganonInventors: Simon James Anthony Grove, Mingqiang Zhang, Mohammad Shahid
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Publication number: 20040229910Abstract: The present invention relates to certain novel benzylamine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of depression.Type: ApplicationFiled: November 19, 2003Publication date: November 18, 2004Inventors: Fredericus Antonius Dijcks, Dirk Leysen, Joannes Theodorus Maria Linders, Gerardus Stephanus Franciscus Ruigt, Ian Craig Carlyle, Simon James Anthony Grove, Duncan Robertson Rae, Simon N. Thorn
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Publication number: 20040220175Abstract: The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R1, R2 and R3 are independently H or (C1-4)alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, CF3, halogen, nitro, cyano, NR4R5, NR4COR6, and CONR4R5; R4 and R5 are independently H or (C1-4)-alkyl; or R4 and R5 form together with the nitrogen atom to which they are bound a 5-or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR6; R6 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)-alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: June 14, 2004Publication date: November 4, 2004Inventors: Simon James Anthony Grove, Julia Adam-Worall, Minggiang Zhang, Robert Gilfillan
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Publication number: 20040171605Abstract: The present invention relates to benzoxazepine derivative having the general formula I, wherein X represents CO or SO2; R1, R2, R3 and R4 are independently selected from H, (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, halogen, nitro, cyano, NR8R9, NR8COR10, and CONR8R9, R5, R6 and R7 are independently H or (C1-4)alkyl; R8 and R9 are independently H or (C1-4)alkyl; or R8 and R9 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR11; R10 is (C1-4)alkyl; R11 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 11, 2003Publication date: September 2, 2004Inventors: Simon James Anthony Grove, Mingqiang Zhang
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Publication number: 20020037885Abstract: The present invention relates to certain novel benzylamine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of depression.Type: ApplicationFiled: August 20, 2001Publication date: March 28, 2002Inventors: Fredericus Antonius Dijcks, Diark Leysen, Joannes Theodorus Maria Linders, Gerardus Stephanus Franciscus Ruigt, Ian Craig Carlyle, Simon James Anthony Grove, Duncan Robertson Rae, Simon N. Thorn