Patents Represented by Attorney, Agent or Law Firm Susan L. Hess
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Patent number: 8350043Abstract: Substituted pyridines, pyrimidines, pyrazines, pyridinones, pyrimidinones, pyrazinones and phenylacetamides useful in treating depression, stress and other disorders are disclosed. The compounds are of the formualae: Other embodiments are also disclosed.Type: GrantFiled: June 7, 2006Date of Patent: January 8, 2013Assignee: Pharmacopeia, Inc.Inventors: Jeffrey John Letourneau, Koc-Kan Ho, Michael J. Ohlmeyer, Patrick Jokiel, Christopher Mark Riviello
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Patent number: 8252803Abstract: Compounds of formula I: I selectively inhibit production of Ab(1-42) and hence find use in treatment of Alzheimer's disease and other conditions associated with deposition of A(b) in the brain.Type: GrantFiled: February 8, 2008Date of Patent: August 28, 2012Assignee: Merck Sharp & Dohme Corp.Inventor: Alexey A. Rivkin
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Patent number: 8242150Abstract: Compounds of formula I: Selectively attenuate production of A?(1-42) and hence find use in treatment or prevention of diseases associated with deposition of A? in the brain, in particular Alzheimer's disease.Type: GrantFiled: June 9, 2008Date of Patent: August 14, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Christian Fischer, Ben Munoz, Susan Zultanski, Joey Methot, Hua Zhou, W. Colby Brown
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Patent number: 8222418Abstract: Compounds of formula I: modulate the action of gamma secretase, and hence find use in treatment of Alzheimer's disease and related conditions.Type: GrantFiled: March 27, 2007Date of Patent: July 17, 2012Assignee: Merck Sharp + Dohme Corp.Inventors: Joanne Clare Hannam, Sascha Hartmann, Andrew Madin, Mark Peter Ridgill
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Patent number: 8203004Abstract: Tetrahydroindole derivatives of formula (I): are disclosed. These compounds modulate the activity of gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.Type: GrantFiled: November 3, 2006Date of Patent: June 19, 2012Assignee: Merck, Sharp & Dohme LimitedInventors: Frank Burkamp, Graham David Checksfield, Stephen Robert Fletcher, Stephen John Lewis, Edward Giles Mciver, Paul Joseph Oakley, Martin Richard Teall
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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: 8183276Abstract: The invention encompasses 2-[4-(imidazolyl)-phenyl]vinyl-heterocycle derivatives which selectively attenuate production of Abeta(1-42) and are useful in the treatment of Alzheimer's disease. Pharmaceutical compositions and methods of use are also encompassed.Type: GrantFiled: February 5, 2008Date of Patent: May 22, 2012Inventors: Christian Fischer, Benito Munoz, Alexey A. Rivkin
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Patent number: 8163956Abstract: A compound of the formula (I): wherein R1, R2, R3, R4, Ar, A, n and m are defined herein, is disclosed as a GlyT1 inhibitor; pharmaceutical compositions containing the compound of the formula (I) are also disclosed as are their use in medicine, for example in the treatment of schizophrenia.Type: GrantFiled: June 13, 2006Date of Patent: April 24, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Wesley Peter Blackaby, Ian Thomas Huscroft, Linda Elizabeth Keown, Richard Thomas Lewis, Piotr Antoni Raubo, Leslie Joseph Street, Christopher George Thomson, Joanne Thomson
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Patent number: 8129397Abstract: The present invention relates to a heterocyclic derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and learning and memory disorders such as Alzheimer's disease.Type: GrantFiled: November 12, 2008Date of Patent: March 6, 2012Assignee: MSD Oss B.V.Inventors: Michael Gerard Gallagher, Craig C. Jamieson, Amanda Jane Lyons, John Kinnaird Ferguson Maclean, Elizabeth Margaret Moir
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Patent number: 8058436Abstract: The invention provides a method for the preparation of enantiomerically pure mirtazapine, said method comprising a step of ring closure of a compound of formula (II) wherein X is a leaving group, said step comprising treatment with an acid, whereby mirlazapine with enantiomeric excess is formed by the ring closure of the compound of formula (II) with enantiomeric excess by treatment with a suitable acid in the absence of a solvent or a suitable combination of an acid and an organic solvent.Type: GrantFiled: July 5, 2004Date of Patent: November 15, 2011Assignee: N.V. OrganonInventors: Johannes Hubertus Wieringa, Adrianus Antonius Martinus Van De Ven, Gerardus Johannes Kemperman
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Patent number: 8058441Abstract: The present invention relates to tetrahydroquinoline derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 is formyl, (1-6C)alkylcarbonyl or (1-6C)alkylsulfonyl; R2 and R3 are H or (1-4C)alkyl; R4 is phenyl; R5 is (1-4C)alkyl; Y—X is (CO)—O, (SO)2—O, NHC(O)—O, NHC(S)—O, OC(O)—O, bond-O, C(O)—NH, S(O)2—NH, NHC(O)—NH, NHC(S)—NH, OC(O)—NH, bond-NH, NH—C(O), O—C(O), NH—S(O)2, or O—S(O)2 or Y—X is a bond; R6 is H, trifluormethyl, (1-6C)alkyl, 1- or 2-adamantyl(1-4C)alkyl, (2-6C)alkenyl, (3-9C)heteroaryl, (3-6C)cycloalkyl, (2-6C)heterocycloalkyl, (1-4C)alkylthio(1-4C)alkyl, (6-10C)aryl(1-4C)alkyl, (3-9C)heteroaryl(1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl(1-4C)alkyl, R8,R9-aminocarbonyl(1-4C)alkyl, R8,R9-amino(1-4C)alkyl, R8-oxycarbonyl(1-4C)alkyl, R8-oxy(1-4C)alkyl, R8-carbonyl(1-4C)alkyl or (6-10C)aryl; R7 is H, (1-4C)alkyl, (1-4C)alkoxy, halogen, trifluoromethyl, cyano, nitro hydroxyl; and R8 and/or R9 is H, (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyType: GrantFiled: June 25, 2002Date of Patent: November 15, 2011Assignee: N.V. OrganonInventors: Nicole Corine Renée Van Straten, Rudolf Gijsbertus Van Someren, Jurgen Schulz
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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: 8026236Abstract: The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.Type: GrantFiled: January 13, 2010Date of Patent: September 27, 2011Assignee: N.V. OrganonInventors: John Stephen Robinson, Philip Stephen Jones, Jiaqiang Cai, David Jonathan Bennett
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Patent number: 7998958Abstract: Disclosed are novel gamma secretase inhibitors of the formula: Also disclosed are methods for inhibiting gamma secretase, for treating one or more neurodegenerative diseases, for inhibiting the deposition of beta amyloid protein, and for treating Alzheimer's disease using the compounds of formula (I).Type: GrantFiled: December 8, 2009Date of Patent: August 16, 2011Assignee: Schering CorporationInventors: Hubert B. Josien, John W. Clader, Thomas A. Bara, Ruo Xu, Hongmei Li, Dmitri A. Pissarnitski, Zhiqiang Zhao
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Patent number: 7994314Abstract: The invention relates to the preparation of mirtazapine precursors and mirtazapine preferably having a substantial enantiomeric excess.Type: GrantFiled: April 7, 2008Date of Patent: August 9, 2011Assignee: N.V. OrganonInventors: Gerardus Johannes Kemperman, Johannes Paulus Gerardus Seerden
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Patent number: 7985758Abstract: Compounds of formula (I) modulate the activity of gamma secretase and hence find use in treatment or prevention of Alzheimer's disease and related conditions.Type: GrantFiled: April 2, 2007Date of Patent: July 26, 2011Assignee: Merck, Sharp & Dohme LimitedInventors: Andrew Madin, Mark Peter Ridgill, Janusz Josef Kulagowski
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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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Patent number: 7960560Abstract: The invention relates to A 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivative having the general Formula I wherein R1 is H, (C1-6)alkyl (optionally substituted with oxo, OR4, COOR5, halogen or CN), (C2-6)alkenyl, (C2-6)alkynyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl; R2 and R2? are independently H or (C1-3)alkyl; or R2 and R2? form together with the carbon atom to which they are bound a (C3-5)cycloalkyl group; R3 represents H or 1 to 4 F substituents; Y represents or NR8R9; X represents CHR6, CF2, O, S, SO or SO2; R4 and R5 are (C1-6)alkyl; R6 is H, OR7 or CN; R7 is (C1-3)alkyl; R8 is (C5-7)cycloalkyl comprising a heteroatom selected from O, S, SO and SO2; R9 is H or (C1-4)alkyl; o and m represent the ortho or meta position of the substituent Y—CH2; or a pharmaceutically acceptable salt thereof; as well as to the use of said 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivatives in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, canceType: GrantFiled: December 1, 2009Date of Patent: June 14, 2011Assignee: N.V. OrganonInventors: Marcelis van der Stelt, Joseph Maria Gerardus Barbara Cals
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Patent number: 7947714Abstract: The present invention is directed to piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.Type: GrantFiled: October 27, 2006Date of Patent: May 24, 2011Assignee: Merck, Sharp & Dohme Corp.Inventors: David Hallett, Craig W. Lindsley, Elizabeth M. Naylor, Zhijian Zhao, Cory R. Theberge, Scott E. Wolkenberg, M. Brad Nolt
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Patent number: 7932251Abstract: The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.Type: GrantFiled: July 15, 2008Date of Patent: April 26, 2011Assignee: N.V. OrganonInventors: Jiaqiang Cai, Zoran Rankovic, Philip Stephen Jones, David Jonathan Bennett, Xavier Fradera