Patents Assigned to Merck & Co., Inc.
  • Acylated piperidine derivatives as melanocortin 4-receptor agonists
    Patent number: 7618987
    Abstract: Certain novel N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists 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 activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
    Type: Grant
    Filed: July 15, 2005
    Date of Patent: November 17, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Raman K. Bakshi, James P. Dellureficio, Ravi P. Nargund
  • Mitotic kinesin inhibitors
    Patent number: 7618971
    Abstract: The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: June 27, 2005
    Date of Patent: November 17, 2009
    Assignee: Merck & Co. Inc.
    Inventors: Paul J. Coleman, Christopher D. Cox, Mark E. Fraley, George D. Hartman, John Schreier
  • Amorphous form of a phosphoric acid salt of a dipeptidyl peptidase-IV inhibitor
    Patent number: 7612072
    Abstract: The present invention relates to a novel amorphous form of the dihydrogenphosphate salt of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-?]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine of structural formula I as well as a process for its preparation, pharmaceutical compositions containing this novel form, and methods of use of the novel form and pharmaceutical compositions for the treatment of diabetes, obesity, and high blood pressure.
    Type: Grant
    Filed: September 9, 2005
    Date of Patent: November 3, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Russell R. Ferlita, Robert M. Wenslow
  • sphingosine 1-phosphate receptor isoform 1
    Patent number: 7611851
    Abstract: A Canis sphingosine-1-phosphate (S1P) receptor isoform 1 (cS1P1), the nucleic acid encoding the cS1P1 receptor, and methods for using the cS1P1 receptor and the nucleic acid encoding the cS1P1 receptor in assays for identifying analytes which modulate activity of the cS1P1 receptor.
    Type: Grant
    Filed: July 22, 2005
    Date of Patent: November 3, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Suzanne M. Mandala, Cheryl Meyers, Gan-Ju Maria Shei
  • Piperdine Glycine Transporter Inhibitors
    Publication number: 20090270451
    Abstract: The present invention is directed to 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: Application
    Filed: October 27, 2006
    Publication date: October 29, 2009
    Applicants: MERCK & CO., INC., MERCK SHARP & DOHME LIMITED
    Inventors: David Hallett, Craig W. Lindsley, Elizabeth M. Naylor, Zhijian Zhao, Cory R. Theberge, Scott E. Wolkenberg, M. Brad Nolt
  • Aminocyclohexanes as Dipeptidyl Peptidase-IV Inhibitors for the Treatment or Prevention of Diabetes
    Publication number: 20090270467
    Abstract: The present invention is directed to novel substituted aminocyclohexanes of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme 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: January 19, 2007
    Publication date: October 29, 2009
    Applicant: MERCK & CO., INC.
    Inventors: Tesfaye Biftu, Jason Cox, Danqing Feng, Anthony Mastracchio, Xiaoxia Qian, Ann E. Weber
  • Mitotic kinesin inhibitors
    Patent number: 7608739
    Abstract: The present invention relates to N-substituted benzylic aniline derivatives that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: March 18, 2005
    Date of Patent: October 27, 2009
    Assignee: Merck & Co. Inc.
    Inventors: Robert M. Garbaccio, Christy M. Olson, Edward S. Tasber, Maricel Torrent
  • 17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators
    Patent number: 7605152
    Abstract: Compounds of structural formula I as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of activating the function of the androgen receptor in a patient, and in particular the method wherein the function of the androgen receptor is blocked in the prostate of a male patient or in the uterus of a female patient and activated in bone and/or muscle tissue.
    Type: Grant
    Filed: January 10, 2003
    Date of Patent: October 20, 2009
    Assignee: Merck & Co., Inc.
    Inventors: William P. Dankulich, Robert S. Meissner, Helen J. Mitchell, James J. Perkins
  • (3,4-disubstituted)propanoic carboxylates as S1P (Edg) receptor agonists
    Patent number: 7605171
    Abstract: The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by modulating leukocyte trafficking, sequestering lymphocytes in secondary lymphoid tissues, and enhancing vascular integrity. The invention is also directed to pharmaceutical compositions containing such compounds and methods of treatment or prevention.
    Type: Grant
    Filed: December 13, 2004
    Date of Patent: October 20, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Vincent J. Colandrea, George A. Doherty, Jeffrey J. Hale, Pei Huo, Irene E. Legiec, Leslie Toth, Petr Vachal, Lin Yan
  • Heterocyclic cyclopentyl tetrahydroisoquinoline and tetrahydropyridopyridine modulators of chemokine receptor activity
    Patent number: 7598243
    Abstract: The present invention is directed to compounds of the formula I: Wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X, n and the broken lines are as defined herein which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
    Type: Grant
    Filed: October 15, 2004
    Date of Patent: October 6, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Gabor Butora, Stephen D. Goble, Alexander Pasternak, Lihu Yang, Changyou Zhou, Christopher R. Moyes
  • HIV integrase inhibitors
    Patent number: 7598264
    Abstract: Hydroxy (tetra- or hexa-)hydronaphthyridine dione compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein a, R1?, R2?, R3?, R4? and R5? 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: March 9, 2005
    Date of Patent: October 6, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Wei Han, Melissa Egbertson, John S. Wai, Linghang Zhuang, Rowena D. Ruzek, Debra S. Perlow, Mark Cameron, Bruce S. Foster, Ulf H. Dolling, R. Scott Hoerrner, Philip J. Pye, Remy Angelaud, Danny E. Mancheno, David Askin
  • Acyl indoles, compositions containing such compounds and methods of use
    Patent number: 7598398
    Abstract: The present invention relates to substituted indoles, compositions containing such compounds and methods of treatment The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus and related conditions.
    Type: Grant
    Filed: October 13, 2006
    Date of Patent: October 6, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Ronald M. Kim, Amy R. Bittner, Christopher Joseph Sinz, Emma R. Parmee
  • Hepatitis C virus vaccine
    Patent number: 7598362
    Abstract: The present invention features Ad6 vectors and a nucleic acid encoding a Met-NS3-NS4A-NS4B-NS5A-NS5B polypeptide containing an inactive NS5B RNA-dependent RNA polymerase region. The nucleic acid is particularly useful as a component of an adenovector or DNA plasmid vaccine providing a broad range of antigens for generating an HCV specific cell mediated immune (CMI) response against HCV.
    Type: Grant
    Filed: October 10, 2002
    Date of Patent: October 6, 2009
    Assignees: Merck & Co., Inc., Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.p.A.
    Inventors: Emilio A. Emini, David C. Kaslow, Andrew J. Bett, John W. Shiver, Alfredo Nicosia, Armin Lahm, Alessandra Luzzago, Riccardo Cortese, Stefano Colloca
  • Pyrazole derivatives, compositions containing such compounds and methods of use
    Patent number: 7598285
    Abstract: Pyrazoles having a naphthyl group attached are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: June 3, 2005
    Date of Patent: October 6, 2009
    Assignee: Merck & Co., Inc
    Inventors: Emma R. Parmee, Yusheng Xiong, Jian Guo, Rui Liang, Linda Brockunier
  • Compressed tablet formulation
    Patent number: 7595063
    Abstract: This invention relates to a 50% drug loaded compressed tablet formulation for efavirenz. Efavirenz is a non-nucleoside reverse trancriptase inhibitor being studied clinically for use in the treatment of HIV infections and AIDS.
    Type: Grant
    Filed: April 14, 2006
    Date of Patent: September 29, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Udit Batra, Raymond J. Higgins, Karen C. Thompson, Ashok V. Katdare
  • Mitotic kinesin inhibitors
    Patent number: 7595337
    Abstract: The present invention relates to tricyclic pyrazoles that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: February 6, 2006
    Date of Patent: September 29, 2009
    Assignee: Merck & Co. Inc.
    Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, Lou Anne Neilson, David B. Whitman
  • Cyanation of aromatic halides
    Patent number: 7595417
    Abstract: A practical, ligand-free cyanation of aryl bromides employs Pd catalyst in combination with a non-toxic cyanide source, Mn[Fe(CN)6] (M=K or Na; n is 3 or 4), or a hydrate thereof, and a base. The reactions are performed in a polar aprotic solvents and provide the corresponding aryl nitrile in 83-96% yield, typically in less than 5 h.
    Type: Grant
    Filed: November 14, 2005
    Date of Patent: September 29, 2009
    Assignee: Merck & Co., Inc.
    Inventor: Steven A. Weissman
  • Modified polynucleotides for reducing off-target effects in RNA interference
    Patent number: 7595387
    Abstract: Methods and compositions for performing RNA interference with decreased off-target effects are provided The methods and compositions permit effective and efficient applications of RNA interference to applications such as diagnostics and therapeutics through the use of modifications to the siRNA. Uniquely modified siRNAs have been developed that reduce off-target effects incurred in gene-silencing. The modifications comprise 2?-O-alkyl or mismatch modification(s) at specific positions on the sense and/or antisense strands.
    Type: Grant
    Filed: December 22, 2004
    Date of Patent: September 29, 2009
    Assignees: Dharmacon, Inc., Merck & Co., Inc.
    Inventors: Devin Leake, Angela Reynolds, Anastasia Khvorova, William Marshall, Peter S. Linsley
  • Synthesis of functional polymers for use in organic synthesis and combinatorial chemistry
    Patent number: 7592392
    Abstract: The present invention relates to a novel process for the preparation of solid-supported scavenging reagents and solid-supported functional polymers. The invention further relates to novel solid-supported functional polymers and to their use in organic synthesis and combinatorial chemistry.
    Type: Grant
    Filed: March 31, 2004
    Date of Patent: September 22, 2009
    Assignee: Merck & Co. Inc.
    Inventors: Craig W. Lindsley, David D. Wisnoski
  • Di-aryl substituted tetrazole modulators of metabotropic glutamate receptor-5
    Patent number: 7592337
    Abstract: Tetrazole compounds substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl and ii) another heteroaryl or aryl ring, with at least one of the rings being further substituted with another ring, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, panic, and bipolar disorder, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal, obesity and other diseases.
    Type: Grant
    Filed: March 7, 2003
    Date of Patent: September 22, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Chixu Chen, Nicholas D. P. Cosford, Brian W. Eastman, Dehua Huang, Steve F. Poon, Thomas S. Reger, Jeffrey R. Roppe, Nicholas D. Smith