Patents Assigned to Merck & Co., Inc.
  • Substituted pyrazolo[1,5-A]pyrimidines as tyrosine kinase inhibitors
    Patent number: 7550470
    Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, macular edema, retinal ischemia, inflammatory diseases, and the like in mammals.
    Type: Grant
    Filed: December 5, 2003
    Date of Patent: June 23, 2009
    Assignee: Merck & Co. Inc.
    Inventor: Mark E. Fraley
  • Substituted pyridyoxy amides
    Patent number: 7550489
    Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
    Type: Grant
    Filed: February 1, 2008
    Date of Patent: June 23, 2009
    Assignee: Merck & Co., Inc.
    Inventors: William K. Hagmann, Linus S. Lin, Shrenik K. Shah, Ravindra N. Guthikonda, Hongbo Qi, Linda L. Chang, Ping Liu, Helen M. Armstrong, James P. Jewell, Thomas J. Lanza, Jr.
  • Ophthalmic compositions for treating ocular hypertension
    Patent number: 7547720
    Abstract: This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.
    Type: Grant
    Filed: December 19, 2006
    Date of Patent: June 16, 2009
    Assignee: Merck & Co. Inc.
    Inventors: James B. Doherty, Meng-Hsin Chen, Luping Liu, Swaminathan R. Natarajan, Robert M. Tynebor
  • Tyrosine Kinase Inhibitors
    Publication number: 20090149467
    Abstract: The present invention relates to pyridinyloxy- and pyrimidinyloxyindole derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Application
    Filed: September 11, 2006
    Publication date: June 11, 2009
    Applicant: MERCK & CO., INC.
    Inventors: Christopher J. Dinsmore, David J. Guerin, Barbara Hanney, Yuntae Kim, Keith L. Spencer, Maricel Torrent
  • Inhibitors of Akt activity
    Patent number: 7544677
    Abstract: The present invention is directed to compounds which contain substituted 5-deazapteridine moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.
    Type: Grant
    Filed: August 19, 2005
    Date of Patent: June 9, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Mark T. Bilodeau, Nicholas D. P. Cosford, John C. Hartnett, Yiwei Li, Jun Liang, Peter J. Manley, Lou Anne Neilson, Tony Siu, Zhicai Wu
  • Spirocyclic compounds
    Patent number: 7544695
    Abstract: The present invention relates to a novel class of substituted spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Grant
    Filed: November 16, 2006
    Date of Patent: June 9, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Scott C. Berk, Joshua Close, Christopher Hamblett, Richard W. Heidebrecht, Solomon D. Kattar, Laura T. Kliman, Dawn M. Mampreian, Joey L. Methot, Thomas Miller, David L. Sloman, Matthew G. Stanton, Paul Tempest, Anna A. Zabierek
  • Process for making hydroisoindoline tachykinin receptor antagonists
    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
  • HIV integrase inhibitors
    Patent number: 7538112
    Abstract: Hydroxy-substituted pyrazinopyrrolopyridazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I) wherein R1, R2, R3, R4, R5, R6 and R7 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment 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 3, 2005
    Date of Patent: May 26, 2009
    Assignee: Merck & Co., Inc.
    Inventors: John S. Wai, Joseph P. Vacca, Linghang Zhuang, Boyoung Kim, Terry A. Lyle, Catherine M. Wiscount, Melissa S. Egbertson, Lou Anne Neilson, Mark Embrey, Thorsten E. Fisher, Donnette D. Staas
  • Tyrosine kinase inhibitors
    Patent number: 7538231
    Abstract: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises a substituted pyrrole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
    Type: Grant
    Filed: July 20, 2004
    Date of Patent: May 26, 2009
    Assignee: Merck & Co, Inc.
    Inventor: Annette S. Kim
  • Tyrosine Kinase Inhibitors
    Publication number: 20090131423
    Abstract: The present invention relates to imidazo[1,2-a]pyrimidine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Application
    Filed: October 18, 2006
    Publication date: May 21, 2009
    Applicant: MERCK & CO., INC.
    Inventors: Christopher J. Dinsmore, Ana Esther Gabarda Ortega, Jongwon Lim, Michelle R. Machacek, Alan B. Northrup, Jonathan R. Young
  • CGRP receptor antagonists
    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
  • C-purine nucleoside analogs as inhibitors of RNA-dependent RNA viral polymerase
    Patent number: 7534767
    Abstract: The present invention provides C-purine nucleoside analogs and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such C-nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the C-nucleoside compounds of the present invention.
    Type: Grant
    Filed: June 10, 2005
    Date of Patent: May 19, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Gabor Butora, Malcolm MacCoss, Balkrishen Bhat, Anne B. Eldrup
  • Histone deacetylase inhibitors
    Patent number: 7534918
    Abstract: This invention relates to hydroxamic acid derivatives having a sulfonamide linkage, that are inhibitors of histone deacetylase (HDAC), and are useful in the prevention and/or treatment of cellular proliferative diseases, for example cancer, autoimmune, allergic and inflammatory diseases, diseases of the central nervous system (CNS) such as neurodegenerative diseases, and in the prevention and/or treatment of restenosis.
    Type: Grant
    Filed: July 8, 2005
    Date of Patent: May 19, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Sandro Belvedere, Joey Lee Methot, Thomas A. Miller, David J. Witter, Jiaming Yan
  • HCV NS3 PROTEASE INHIBITORS
    Publication number: 20090124661
    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: Application
    Filed: December 1, 2008
    Publication date: May 14, 2009
    Applicant: MERCK & CO., INC.
    Inventors: M. Katharine HOLLOWAY, Nigel J. LIVERTON, Steven W. LUDMERER, John A. MCCAULEY, David B. OLSEN, Michael T. RUDD, Joseph P. VACCA, Charles J. MCINTYRE
  • Ophthalmic compositions for treating ocular hypertension
    Patent number: 7528163
    Abstract: This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.
    Type: Grant
    Filed: November 4, 2003
    Date of Patent: May 5, 2009
    Assignee: Merck & Co. Inc.
    Inventors: James B. Doherty, Meng-Hsin Chen, Luping Liu, Swaminathan R. Natarajan, Dong-Ming Shen, Robert M. Tynebor
  • Substituted pyrazine inhibitors of AKT
    Patent number: 7524850
    Abstract: The compounds of Formula E are useful as anti-cancer agents:
    Type: Grant
    Filed: February 8, 2007
    Date of Patent: April 28, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, Craig W. Lindsley, Zhijian Zhao
  • PPAR alpha selective compounds for the treatment of dyslipidemia and other lipid disorders
    Patent number: 7524882
    Abstract: A class of benzodihydrofuran compounds having the structure of formula (I) below and pharmaceutically acceptable salts thereof are useful as therapeutic compounds, particularly in the treatment of hyperlipidemia, hypercholesterolemia, dyslipidemia, and other lipid disorders, and in delaying the onset of or reducing the risk of conditions and sequelae that are associated with these diseases, such as atherosclerosis.
    Type: Grant
    Filed: July 25, 2003
    Date of Patent: April 28, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Guo Q. Shi, Yong Zhang
  • 4-Oxo-1-3-Substituted Phenyl-1,4-Dihydro-1,8-Napthyridene-3-Carboxamide Phosphodiesterase-4 Inhibitor and a Method of Preparing Same
    Publication number: 20090105479
    Abstract: The invention is directed to a compound of the structural formula (22) (22) crystal form of structural formulae (21) and its free acid, pharmaceutical compositions comprising these compounds and methods of preparing and using these compounds.
    Type: Application
    Filed: October 24, 2006
    Publication date: April 23, 2009
    Applicant: MERCK & CO., INC.
    Inventors: Mark Cameron, Frederick W. Hartner, Lushi Tan, Nobuyoshi Yasuda, Naoki Yoshikawa
  • Aminocyclohexanes as Dipeptidyl Peptidase-IV for the Treatment or Prevention of Diabetes
    Publication number: 20090105284
    Abstract: The present invention is directed to novel substituted aminocyclohexanes which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.
    Type: Application
    Filed: May 19, 2006
    Publication date: April 23, 2009
    Applicant: MERCK & CO., INC.
    Inventors: Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Ann E. Weber, Jason Cox
  • Crystalline forms of carbapenem antibiotics and methods of preparation
    Patent number: RE40794
    Abstract: A process for preparing a crystalline, carbapenem monosodium salt of formula IIa: characterized by the steps a) adding about 10 to 30% of an organic solvent to an aqueous solution of the carbapenem, b) cooling the resulting solution to less than ?5° C., c) adjusting the pH using a solution containing an acid in an organic solvent to give the appropriate pH for crystallization, and d) crystallizing the compound by adding methanol, and a C2-5 alcohol at between ?5 and ?25° C.
    Type: Grant
    Filed: September 20, 2002
    Date of Patent: June 23, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Karel M. J. Brands, Raymond Cvetovich, Louis S. Crocker, Michael D. Ward, Amar J. Mahajan, Robert M. Wenslow, John M. Williams, Daniel R. Sidler, Charles Orella, Elizabeth S. Fisher, Ronald Jobson