Patents Represented by Attorney William Krovatin
  • Patent number: 7759492
    Abstract: 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: Grant
    Filed: August 17, 2005
    Date of Patent: July 20, 2010
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Stephen Philip Keen, Steven Fraser Oliver, Gavin William Stewart
  • Patent number: 7696192
    Abstract: 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: Grant
    Filed: September 6, 2005
    Date of Patent: April 13, 2010
    Assignee: 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
  • Patent number: 7659300
    Abstract: 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: Grant
    Filed: September 6, 2005
    Date of Patent: February 9, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Craig A. Stump
  • Patent number: 7659264
    Abstract: 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: Grant
    Filed: October 5, 2005
    Date of Patent: February 9, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, James Z. Deng, Craig Potteiger, Theresa M. Williams
  • Patent number: 7655675
    Abstract: Compounds of formula I: inhibit the processing of APP by gamma-secretase and hence find use in treatment of Alzheimer's disease.
    Type: Grant
    Filed: October 1, 2004
    Date of Patent: February 2, 2010
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Alan John Nadin, Andrew Pate Owens, Martin Richard Teall
  • Patent number: 7655644
    Abstract: 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: Grant
    Filed: December 21, 2005
    Date of Patent: February 2, 2010
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Wesley Peter Blackaby, Stephen Robert Fletcher, Andrew Jennings, Richard Thomas Lewis, Elizabeth Mary Naylor, Leslie Joseph Street, Joanne Thomson
  • Patent number: 7645790
    Abstract: 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: Grant
    Filed: January 26, 2005
    Date of Patent: January 12, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jaime Lynn Bunda, Robert J. DeVita, Jinlong Jiang, Sander G. Mills
  • Patent number: 7625901
    Abstract: 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: Grant
    Filed: June 19, 2008
    Date of Patent: December 1, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Michael R. Wood, Steven N. Gallicchio, Harold G. Selnick, C. Blair Zartman, Ian M. Bell, Craig A. Stump
  • Patent number: 7626056
    Abstract: 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: Grant
    Filed: June 5, 2006
    Date of Patent: December 1, 2009
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Wesley Peter Blackaby, Jose Luis Castro Pineiro, Richard Thomas Lewis, Elizabeth Mary Naylor, Leslie Joseph Street
  • Patent number: 7595344
    Abstract: Disclosed are sulphones which modulate the action of gamma-secretase. The compounds are useful in the treatment or prevention of Alzheimer's disease.
    Type: Grant
    Filed: May 6, 2008
    Date of Patent: September 29, 2009
    Assignee: Merck Sharp & Dohme Limited
    Inventors: 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
  • Patent number: 7592360
    Abstract: 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: Grant
    Filed: May 28, 2004
    Date of Patent: September 22, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Nigel J. Liverton, Christopher F. Claiborne, David A. Claremon, John A. McCauley
  • Patent number: 7576083
    Abstract: 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: Grant
    Filed: April 29, 2005
    Date of Patent: August 18, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Craig W. Lindsley, Scott E. Wolkenberg, Zhijian Zhao
  • Patent number: 7572792
    Abstract: 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: Grant
    Filed: April 25, 2005
    Date of Patent: August 11, 2009
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Limited
    Inventors: Craig W Lindsley, David Hallett, Scott E. Wolkenberg
  • Patent number: 7550481
    Abstract: 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: Grant
    Filed: December 15, 2004
    Date of Patent: June 23, 2009
    Assignee: 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
  • Patent number: 7544815
    Abstract: 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: Grant
    Filed: July 11, 2006
    Date of Patent: June 9, 2009
    Assignee: Merck & Co, Inc.
    Inventors: Jeffrey T. Kuethe, Jingjun Yin, Mark A. Huffman, Michel Journet
  • Patent number: 7534784
    Abstract: 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: Grant
    Filed: April 9, 2008
    Date of Patent: May 19, 2009
    Assignee: Merck + Co., Inc.
    Inventors: Christopher S. Burgey, Zhengwu J. Deng, Diem N. Nguyen, Daniel V. Paone, Anthony W. Shaw, Theresa M. Williams
  • Patent number: 7521455
    Abstract: 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: Grant
    Filed: February 14, 2005
    Date of Patent: April 21, 2009
    Assignee: Banyu Pharmaceutical Co. Ltd.
    Inventors: Tsuyoshi Nagase, Nagaaki Sato, Akio Kanatani, Shigeru Tokita
  • Patent number: 7514459
    Abstract: 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: Grant
    Filed: September 16, 2004
    Date of Patent: April 7, 2009
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Ian James Collins, Joanne Clare Hannam, Andrew Madin, Mark Peter Ridgill
  • Patent number: 7495029
    Abstract: 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: Grant
    Filed: November 10, 2005
    Date of Patent: February 24, 2009
    Assignee: Merck & Co., Inc
    Inventors: Benito Munoz, Joseph E. Payne, Petpiboon Prasit, Thomas S. Reger, Nicholas D. Smith
  • Patent number: 7491713
    Abstract: 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: Grant
    Filed: January 25, 2005
    Date of Patent: February 17, 2009
    Assignee: Merck + Co., Inc.
    Inventors: Christopher S. Burgey, Daniel V. Paone, Anthony W Shaw, Craig A. Stump, Theresa M. Williams