Patents Represented by Attorney William Krovatin
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Patent number: 7759492Abstract: An enantioselective route to compounds of formula I is disclosed: The compounds of formula I are key intermediates in the synthesis of compounds useful in treatment of Alzheimer's disease.Type: GrantFiled: August 17, 2005Date of Patent: July 20, 2010Assignee: Merck Sharp & Dohme LimitedInventors: Stephen Philip Keen, Steven Fraser Oliver, Gavin William Stewart
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Patent number: 7696192Abstract: The present invention is directed to compounds of Formula I: I (where A1, A2, B1, B2, B3, B4, D1, D2, J, K, T, U, V, W, X, Y, Z, R4, R5a, R5b, R5c, m and n are defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: September 6, 2005Date of Patent: April 13, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Steven N. Gallicchio, Craig A. Stump, Cory R. Theberge, Joseph P. Vacca, C. Blair Zartman, Xufang Zhang
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Patent number: 7659300Abstract: The present invention is directed to compounds of Formula I: I (where A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: September 6, 2005Date of Patent: February 9, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Craig A. Stump
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Patent number: 7659264Abstract: The present invention is directed to compounds of Formula I: Formula I: I and Formula II: (where variables R1, R2, R3, R4, A, B, J, Q, T, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: October 5, 2005Date of Patent: February 9, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher S. Burgey, James Z. Deng, Craig Potteiger, Theresa M. Williams
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Patent number: 7655675Abstract: Compounds of formula I: inhibit the processing of APP by gamma-secretase and hence find use in treatment of Alzheimer's disease.Type: GrantFiled: October 1, 2004Date of Patent: February 2, 2010Assignee: Merck Sharp & Dohme LimitedInventors: Alan John Nadin, Andrew Pate Owens, Martin Richard Teall
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Patent number: 7655644Abstract: The present invention provides compounds of formula (I), wherein both p's are one or two, R1 is generally heteroaryl or cycloalkyl, R2 is C3-6cycloalkyl or phenyl and R3 is heteroaryl, and pharmaceutically acceptable salts thereof, as GlyT1 inhibitors for treating schizophrenia, pharmaceutical compositions comprising the same and methods for their preparation.Type: GrantFiled: December 21, 2005Date of Patent: February 2, 2010Assignee: Merck Sharp & Dohme LimitedInventors: Wesley Peter Blackaby, Stephen Robert Fletcher, Andrew Jennings, Richard Thomas Lewis, Elizabeth Mary Naylor, Leslie Joseph Street, Joanne Thomson
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Patent number: 7645790Abstract: The present invention is directed to certain hydroisoindoline compounds of formula I which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.Type: GrantFiled: January 26, 2005Date of Patent: January 12, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Jaime Lynn Bunda, Robert J. DeVita, Jinlong Jiang, Sander G. Mills
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Patent number: 7625901Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, m, n, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: June 19, 2008Date of Patent: December 1, 2009Assignee: Merck & Co., Inc.Inventors: Michael R. Wood, Steven N. Gallicchio, Harold G. Selnick, C. Blair Zartman, Ian M. Bell, Craig A. Stump
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Patent number: 7626056Abstract: The present invention provides compounds of formula I: wherein R1 is an alkyl, phenyl, heterocyclyl, cycloalkyl, alkoxy, ester, amino or amide group; R2 is a phenyl, heterocyclyl, alkyl, cycloalkyl or cycloalkylalkyl group; R3 is an alkyl, cycloalkyl, cycloalkylalkyl, amino or heterocyclyl group; R4 and R5 are hydrogen or alkyl or form a cycloalkyl ring; A is O or N; and m is zero or one; as inhibitors of GlyT1 and thus as useful for treating or preventing diseases such as schizophrenia; with the provision of pharmaceutical compositions, first and second medical uses and methods of treatment.Type: GrantFiled: June 5, 2006Date of Patent: December 1, 2009Assignee: Merck Sharp & Dohme LimitedInventors: Wesley Peter Blackaby, Jose Luis Castro Pineiro, Richard Thomas Lewis, Elizabeth Mary Naylor, Leslie Joseph Street
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Patent number: 7595344Abstract: Disclosed are sulphones which modulate the action of gamma-secretase. The compounds are useful in the treatment or prevention of Alzheimer's disease.Type: GrantFiled: May 6, 2008Date of Patent: September 29, 2009Assignee: Merck Sharp & Dohme LimitedInventors: Jose Luis Castro Pineiro, Ian Churcher, Kevin Dinnell, Timothy Harrison, Sonia Kerrad, Alan John Nadin, Paul Joseph Oakley, Andrew Pate Owens, Duncan Edward Shaw, Martin Richard Teall, Susannah William, Brian John Williams
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Patent number: 7592360Abstract: Compounds represented by Formula (I) or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for treating conditions such as, for example, Parkinson's disease, Alzheimer's disease, migraine, epilepsy and pain.Type: GrantFiled: May 28, 2004Date of Patent: September 22, 2009Assignee: Merck & Co., Inc.Inventors: Nigel J. Liverton, Christopher F. Claiborne, David A. Claremon, John A. McCauley
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Patent number: 7576083Abstract: The present invention is directed to morpholinyl 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: April 29, 2005Date of Patent: August 18, 2009Assignee: Merck & Co., Inc.Inventors: Craig W. Lindsley, Scott E. Wolkenberg, Zhijian Zhao
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Patent number: 7572792Abstract: The present invention is directed to azetidine 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: April 25, 2005Date of Patent: August 11, 2009Assignees: Merck & Co., Inc., Merck Sharp & Dohme LimitedInventors: Craig W Lindsley, David Hallett, Scott E. Wolkenberg
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Patent number: 7550481Abstract: The present invention is directed to phenylamide and pyridylamide derivative compounds of which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: GrantFiled: December 15, 2004Date of Patent: June 23, 2009Assignee: Merck & Co., Inc.Inventors: James C. Barrow, Craig A. Coburn, Philippe G. Nantermet, Harold G. Selnick, Shawn J. Stachel, Matthew G. Stanton, Shaun R. Stauffer, Linghang Zhuang, Jennifer R. Davis
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Patent number: 7544815Abstract: The present invention is directed to a process for preparing certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The compounds are useful in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.Type: GrantFiled: July 11, 2006Date of Patent: June 9, 2009Assignee: Merck & Co, Inc.Inventors: Jeffrey T. Kuethe, Jingjun Yin, Mark A. Huffman, Michel Journet
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Patent number: 7534784Abstract: The present invention is directed to compounds of Formula I: (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: April 9, 2008Date of Patent: May 19, 2009Assignee: Merck + Co., Inc.Inventors: Christopher S. Burgey, Zhengwu J. Deng, Diem N. Nguyen, Daniel V. Paone, Anthony W. Shaw, Theresa M. Williams
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Patent number: 7521455Abstract: The present invention provides a compound represented by formula (I) below, or a pharmaceutically acceptable salt thereof, which, having histamine H3 receptor antagonist or inverse agonist activity, is useful in the prophylaxis or therapy of metabolic diseases, circulatory diseases, or nervous system diseases. [where, for example, Ar is a divalent group formed by eliminating two hydrogen atoms from benzene, X1 is a nitrogen atom, sulfur atom or oxygen atom, R1 is a 5- to 6-membered heteroaryl group, Ring A is a 5- to 6-membered heteroaryl ring, R2 and R3 are amino groups or alkylamino groups, and X2 is represented by formula (II): (where R4 and R5 are lower alkyl groups, and n is an integer from 2 to 4).Type: GrantFiled: February 14, 2005Date of Patent: April 21, 2009Assignee: Banyu Pharmaceutical Co. Ltd.Inventors: Tsuyoshi Nagase, Nagaaki Sato, Akio Kanatani, Shigeru Tokita
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Patent number: 7514459Abstract: Compounds of formula I: are potent inhibitors of gamma-secretase and hence find use in treatment or prevention of diseases associated with deposition of ?-amyloid.Type: GrantFiled: September 16, 2004Date of Patent: April 7, 2009Assignee: Merck Sharp & Dohme Ltd.Inventors: Ian James Collins, Joanne Clare Hannam, Andrew Madin, Mark Peter Ridgill
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Patent number: 7495029Abstract: Disclosed are prodrugs of (2R)-2-propyloctanoic acid, and pharmaceutical compositions comprising them, which may be effective in modulating multiple events in the biochemical cascade of stroke. Also disclosed are methods of treating patients who have had a stroke, or are at risk of stroke, by administering the compounds or compositions of the invention.Type: GrantFiled: November 10, 2005Date of Patent: February 24, 2009Assignee: Merck & Co., IncInventors: Benito Munoz, Joseph E. Payne, Petpiboon Prasit, Thomas S. Reger, Nicholas D. Smith
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Patent number: 7491713Abstract: Compounds of Formula I: and Formula II: (where variables R1, R2, R3, R4, A, B, D, G, J, Q, T, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, pharmaceutical compositions comprising these compounds, use of these compounds and compositions to prevent or treat diseases involving CGRP.Type: GrantFiled: January 25, 2005Date of Patent: February 17, 2009Assignee: Merck + Co., Inc.Inventors: Christopher S. Burgey, Daniel V. Paone, Anthony W Shaw, Craig A. Stump, Theresa M. Williams