Patents Assigned to Merck Sharp and Dohme
  • Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
    Patent number: 8293900
    Abstract: Certain novel N-acylated spiropiperidine derivatives are ligands of the human melanocortin receptor(s) and, in particular, are selective ligands of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of MC-4R, such as obesity, diabetes, nicotine addiction, alcoholism, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
    Type: Grant
    Filed: September 25, 2006
    Date of Patent: October 23, 2012
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Tianying Jian, Jian Liu, Ravi P. Nargund
  • HIV integrase inhibitors
    Patent number: 8293731
    Abstract: Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: May 13, 2011
    Date of Patent: October 23, 2012
    Assignee: Merck Sharp + Dohme Corp.
    Inventors: Joseph P. Vacca, John S. Wai, Linda S. Payne
  • Heterocyclic amide compounds as protein kinase inhibitors
    Patent number: 8293747
    Abstract: The present invention relates to novel heterocyclic amide compounds of Formula I: as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are compositions comprising said compounds, and methods for using said compounds for treating or preventing a proliferative disease, an anti-proliferative disorder, inflammation, arthritis, a neurological or neurodegenerative disease, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease or a fungal disease.
    Type: Grant
    Filed: July 17, 2008
    Date of Patent: October 23, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Panduranga Adulla P. Reddy, Lianyun Zhao, Praveen K. Tadikonda, Tzu Tshin Wong, Shuyi Tang, Luis E. Torres, David F. Cauble, Jr., Timothy J. Guzi, M. Arshad Siddiqui
  • Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease
    Patent number: 8293759
    Abstract: The present invention is directed to spiropiperidine 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: Grant
    Filed: October 29, 2007
    Date of Patent: October 23, 2012
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Shaun R. Stauffer, Ivory D. Hills, Ashley Nomland
  • Heterocyclic fused cinnoline M1 receptor positive allosteric modulators
    Patent number: 8293744
    Abstract: The present invention is directed to heterocyclic fused cinnoline compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: April 13, 2010
    Date of Patent: October 23, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Douglas C. Beshore
  • Angiotensin II receptor antagonists
    Patent number: 8293777
    Abstract: A compound having the structure wherein R is an angiotensin receptor antagonist active group, and Y is Y is selected from the group consisting of R1 is selected from the group consisting of —O—C1-6 alkyl, —O-aryl, —O-heteroaryl, —O—C3-8 cycloalkyl, —C1-6 alkyl, -aryl, -heteroaryl, and —C3-8 cycloalkyl; R2 and R3 are independently selected from the group consisting of hydrogen and C1-4 alkyl, or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.
    Type: Grant
    Filed: December 2, 2009
    Date of Patent: October 23, 2012
    Assignee: Merck Sharp & Dohme, Corp.
    Inventors: Michael Man-Chu Lo, Amjad Ali, Ravi P. Nargund
  • 4-OXO,1-4-dihydroquinoline M1 receptor positive allosteric modulators
    Patent number: 8293914
    Abstract: The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: April 23, 2009
    Date of Patent: October 23, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Christina Ng Di Marco, William D. Shipe
  • OXADIAZOLE BETA CARBOLINE DERIVATIVES AS ANTIDIABETIC COMPOUNDS
    Publication number: 20120264777
    Abstract: Beta-carboline derivatives of structural formula I are selective antagonists of the somatostatin sub-type receptor 3 (SSTR3) and are useful for the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including hyperglycemia, insulin resistance, obesity, lipid disorders, and hypertension. The compounds are also useful for the treatment of depression and anxiety.
    Type: Application
    Filed: January 11, 2011
    Publication date: October 18, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Liangqin Guo, William K. Hagmann, Shuwen He, Zhong Lai, Jian Liu, Ravi P. Nargund, Shrenik K. Shah, Quang T. Truong
  • Formulations of suberoylanilide hydroxamic acid and methods for producing same
    Patent number: 8288440
    Abstract: The present invention provides a pharmaceutical composition or crystalline composition with a specific dissolution profile, which comprises suberoylanilide hydroxamic acid or a pharmaceutically acceptable salt or hydrate thereof as an active ingredient. The present invention provides a process of producing said crystalline composition or pharmaceutical composition. The present invention also provides compositions with a specific particle size distribution.
    Type: Grant
    Filed: January 13, 2010
    Date of Patent: October 16, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jeannie Chow Wong, Aaron S. Cote, Erik A. Dienemann, Kimberly Gallagher, Craig Ikeda, Justin Moser, Pavol Rajniak, Robert A. Reed, Cindy Starbuck, Hsien-Hsin Tung, Qingxi Wang, Benjamin Max Cohen, Vincent R. Capodanno, Brian Sell
  • Substituted naphthyridine compounds as inhibitors of Akt activity
    Patent number: 8288407
    Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
    Type: Grant
    Filed: March 11, 2011
    Date of Patent: October 16, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael J. Kelly, III, Mark E. Layton, Philip E. Sanderson
  • Quinolizidinone M1 receptor positive allosteric modulators
    Patent number: 8288409
    Abstract: The present invention is directed to compounds of formula (I) (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: February 3, 2009
    Date of Patent: October 16, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Ronald K. Chang, Christina Ng Di Marco
  • Method for treating atherosclerosis by administering human MCP1 fusions
    Patent number: 8282914
    Abstract: The present invention provides polypeptides including MCP1 fused, optionally, by a linker, to an immunoglobulin. Methods for using the polypeptides to treat medical disorders are also covered.
    Type: Grant
    Filed: May 2, 2011
    Date of Patent: October 9, 2012
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Chuan-Chu Chou, Loretta A. Bober, Lee Sullivan
  • Bicyclic heterocyclic derivatives and methods of use thereof
    Patent number: 8283360
    Abstract: The present invention relates to novel Bicyclic Heterocyclic Derivatives, pharmaceutical compositions comprising the Bicyclic Heterocyclic Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a cognitive disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: October 9, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Anandan Palani, Ashwin U. Rao, Xiao Chen, Ning Shao, Ying R. Huang, Robert G. Aslanian
  • Substituted pyridines that are JNK inhibitors
    Patent number: 8278337
    Abstract: Disclosed are compounds of the formula (I) wherein X is N or CH, and Y is N or CR5. Also disclosed are methods of treating JNK and ERK mediated diseases using the compounds of formula 1.0.
    Type: Grant
    Filed: December 17, 2007
    Date of Patent: October 2, 2012
    Assignee: Merck Sharp & Dohme
    Inventors: David B. Belanger, M. Arshad Siddiqui, Patrick J. Curran, Blake Hamann, Lianyun Zhao, Panduranga Adulla P. Reddy, Praveen K. Tadikonda, Gerald W. Shipps, Jr., Umar Faruk Mansoor
  • Cyclic amine BACE-1 inhibitors having a benzamide substituent
    Patent number: 8278334
    Abstract: 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: Grant
    Filed: December 18, 2009
    Date of Patent: October 2, 2012
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: 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
  • HCV NS3 protease inhibitors
    Patent number: 8278322
    Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
    Type: Grant
    Filed: July 28, 2006
    Date of Patent: October 2, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: M. Katharine Holloway, Nigel J. Liverton, John A. McCauley, Michael T. Rudd, Joseph P. Vacca, Steven W. Ludmerer, David B. Olsen
  • Substituted 4-hydroxypyrimidine-5-carboxamides
    Patent number: 8278304
    Abstract: The present invention relates to substituted 4-hydroxypyrimidine-5-carboxamides useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
    Type: Grant
    Filed: March 12, 2009
    Date of Patent: October 2, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Matthew J. Clements, John S. Debenham, Jeffrey J. Hale, Christina B. Madsen-Duggan, Thomas F. Walsh
  • Potassium channel inhibitors
    Patent number: 8278317
    Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
    Type: Grant
    Filed: July 18, 2006
    Date of Patent: October 2, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: B. Wesley Trotter, Kausik K. Nanda, Scott E. Wolkenberg, M. Brad Nolt, David Wisnoski
  • Inhibitors of Janus kinases
    Patent number: 8278335
    Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
    Type: Grant
    Filed: April 9, 2009
    Date of Patent: October 2, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michelle R. Machacek, Andrew Haidle, Anna A. Zabierek, Kaleen M. Konrad, Michael D. Altman
  • Quinolizidinone M1 receptor positive allosteric modulators
    Patent number: 8278453
    Abstract: The present invention is directed to quinolizidinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: September 29, 2009
    Date of Patent: October 2, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Christina Ng Di Marco