Patents Represented by Attorney Keith D. MacMillan
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Patent number: 7868000Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein j, k, U, W, R, R1, R2, R3, R4, R6, R7 and R7a are as described above in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: GrantFiled: June 12, 2006Date of Patent: January 11, 2011Assignee: Schering CorporationInventors: Zhaoning Zhu, Brian McKittrick, Andrew Stamford, William J. Greenlee, Xiaoxiang Liu, Mihirbaran Mandal, Johannes H. Voigt, Corey O. Strickland
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Patent number: 7847100Abstract: The present invention is directed to 1,3,5-phenyl substituted derivative compounds 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: April 15, 2005Date of Patent: December 7, 2010Assignee: Merck, Sharp & Dohme, Inc.Inventors: James C. Barrow, Georgia B. McGaughey, Philippe G. Nantermet, Hemaka A. Rajapakse, Harold G. Selnick, Shaun R. Stauffer, Craig A. Coburn
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Patent number: 7829597Abstract: The present invention is directed to compounds of formula (I) 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: September 29, 2004Date of Patent: November 9, 2010Assignee: Merck, Sharp & Dohme, Inc.Inventors: Philippe G. Nantermet, Hemaka Anthony Rajapakse, Harold G. Selnick
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Patent number: 7820674Abstract: The present invention is directed to aminomethyl compounds 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: January 13, 2006Date of Patent: October 26, 2010Assignee: Merck, Sharp & Dohme Corp.Inventors: Craig A. Coburn, Philippe G. Nantermet, Hemaka A. Rajapakse, Harold G. Selnick, Shaun R. Stauffer
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Patent number: 7816378Abstract: The present invention is directed to cyclic ketal compounds of formula (I) 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: July 28, 2006Date of Patent: October 19, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Philippe G. Nantermet, Joseph P. Vacca
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Patent number: 7812013Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt, solvate or ester thereof, wherein U, W, X, L, Y, M, Z, c, d, e, f, g, h, s, t, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and R18 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: GrantFiled: June 12, 2006Date of Patent: October 12, 2010Assignee: Schering CorporationInventors: Ulrich Iserloh, Zhaoning Zhu, Andrew Stamford, Johannes H. Voigt
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Patent number: 7803802Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of ?-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.Type: GrantFiled: July 20, 2005Date of Patent: September 28, 2010Assignee: Schering CorporationInventors: Ying Huang, Guoqing Li, Andrew W Stamford
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Patent number: 7763606Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Ar, R1, R2, R3, R4 and R5 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: GrantFiled: October 25, 2006Date of Patent: July 27, 2010Assignee: Schering CorporationInventors: Zhaoning Zhu, Andrew W. Stamford, Brian McKittrick
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Patent number: 7763609Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: GrantFiled: February 23, 2007Date of Patent: July 27, 2010Assignees: Schering Corporation, Pharmacopeia, LLCInventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey O. Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert D. Mazzola, John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Xiaoxiang Liu, Tao Guo, Thuy X. E. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse, Ying Huang, Guoqing Li, Jianping Pan, Jeffrey A. Misiaszek, Gaifa Lai, Jingqi Duo, Chuanxing Qu, Yuefei Shao
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Patent number: 7759353Abstract: Disclosed are certain substituted spiro iminopyrimidinones and other compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein U, W, A, R, R1, R2, R6a and R7, are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of using such compounds and compositions to inhibit aspartyl protease, and to treat a variety of disease and indications including (but not limited) to cardiovascular disease and cognitive and neurodegenerative disease. The compounds of the present invention are disclosed for use alone or in combination with one or more additional active ingredients such as cholinesterase inhibitors and a muscarinic m1 agonist and/or m2 antagonists.Type: GrantFiled: June 12, 2006Date of Patent: July 20, 2010Assignees: Schering Corporation, Pharmacopeia LLC.Inventors: Zhaoning Zhu, Brian McKittrick, Andrew Stamford, Tao Guo, Thuy X. H. Le
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Patent number: 7759354Abstract: The present application provides compounds of the Formula: and stereoisomers, tautomers, or pharmaceutically acceptable salts and solvates thereof, wherein U, W, R, R1, R2, R3 and R4 in each formula (when present) are as defined in the specification, and pharmaceutical compositions comprising such compounds. Also disclosed are methods of using such compounds and compositions to inhibit aspartyl protease, and to treat a variety of disease and indications including (but not limited) to cardiovascular disease and cognitive and neurodegenerative disease. The compounds of the present invention are disclosed for use alone or in combination with one or more additional active ingredients such as cholinesterase inhibitors and a muscarinic m1 agonist and/or m2 antagonists.Type: GrantFiled: June 12, 2006Date of Patent: July 20, 2010Assignee: Schering CorporationInventors: Zhaoning Zhu, Brian McKittrick, Andrew Stamford, Ying Huang, Elizabeth M. Smith
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Patent number: 7750158Abstract: Compounds of Formula I: and/or pharmaceutically acceptable salts, solvates or prodrugs thereof, or pharmaceutical compositions containing such compounds exhibit anti-inflammatory and immunomodulatory activity, and can be effective in treating cancer and inflammatory, immunomodulatory or respiratory diseases or conditions.Type: GrantFiled: June 21, 2005Date of Patent: July 6, 2010Assignee: Schering CorporationInventors: Bandarpalle B. Shankar, Eric Gilbert, Razia K. Rizvi, Chunli Huang, Joseph A. Kozlowski, Stuart McCombie, Neng-Yang Shih
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Patent number: 7718702Abstract: There are disclosed compounds of the formula a prodrug thereof, or a pharmaceutically acceptable salt, solvate or stereoisomer of the compound or of said prodrug; which exhibit anti-inflammatory and immunodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds and methods of using the compounds for the treatment of various diseases and conditions.Type: GrantFiled: August 15, 2005Date of Patent: May 18, 2010Assignee: Schering CorporationInventors: Joseph A. Kozlowski, Neng-Yang Shih, Brian J. Lavey, Razia K. Rizvi, Bandarpalle B. Shankar, James M. Spitler, Ling Tong, Ronald L. Wolin, Michael K. Wong
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Patent number: 7714021Abstract: The present invention is directed to pyrrolidin-3-yl derivative compounds 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: June 10, 2005Date of Patent: May 11, 2010Assignee: Merck & Co., Inc.Inventor: Craig A. Coburn
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Patent number: 7700597Abstract: Compounds of Formula (I): or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.Type: GrantFiled: December 1, 2005Date of Patent: April 20, 2010Assignee: Schering CorporationInventors: Eric J. Gilbert, Michael W. Miller, Jack D. Scott, Andrew W. Stamford, William J. Greenlee, Jay Weinstein
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Patent number: 7700603Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: GrantFiled: June 9, 2005Date of Patent: April 20, 2010Assignee: Schering CorporationInventors: Zhaoning Zhu, Brian A McKittrick, Zhong-Yue Sun, Yuanzan C Ye, Johannes H Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X. H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Gang Qian, Dawit Tadesse
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Patent number: 7662816Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.Type: GrantFiled: August 4, 2004Date of Patent: February 16, 2010Assignee: Schering CorporationInventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voigt, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X. H. Le, Jeffrey F. Lowrie, Kurt W. Saionz, Suresh D. Babu
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Patent number: 7652003Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, n and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of ?-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.Type: GrantFiled: July 26, 2005Date of Patent: January 26, 2010Assignee: Schering-Plough CorporationInventors: Andrew W Stamford, Ying Huang, Guoqing Li, Corey O Strickand, Johannes H. Voigt
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Patent number: 7645774Abstract: There are disclosed compounds of the formula I: or a pharmaceutically acceptable salt of the compound, which exhibit anti-inflammatory and immunomodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds.Type: GrantFiled: August 5, 2005Date of Patent: January 12, 2010Assignee: Schering CorporationInventors: Richard J. Friary, Joseph A. Kozlowski, Bandarpalle B. Shankar, Michael K. C. Wong, Guowei Zhou, Brian J. Lavey, Neng-Yang Shih, Ling Tong, Lei Chen, Youheng Shu
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Patent number: 7642272Abstract: There are disclosed compounds of the formula I a pharmaceutically acceptable salt or solvate of the compound, which exhibit anti-inflammatory and immunomodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds.Type: GrantFiled: March 18, 2004Date of Patent: January 5, 2010Assignee: Schering CorporationInventors: Bandarpalle B. Shankar, Razia K. Rizvi, Joseph A. Kozlowski, Neng-Yang Shih