Search Patents
  • Microbial immunosoppressant agent
    Patent number: 5252612
    Abstract: Described is a new immunosuppressant, L-683,756, a bisdemethylated, ring rearranged derivative of L-683,590, produced under fermentation conditions utilizing the microorganism, Actinoplanacete sp. (Merck Culture Collection MA 6559) ATCC No. 53771. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.
    Type: Grant
    Filed: June 24, 1992
    Date of Patent: October 12, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Byron H. Arison, Edward S. Inamine, Shieh-Shung T. Chen, Linda S. Wicker
  • COMPOSITIONS AND METHODS FOR SHORT INTERFERING NUCLEIC ACID INHIBITION OF NAV1.8
    Publication number: 20130109739
    Abstract: The invention provides short interfering nucleic acids, either single-stranded or double-stranded, that cause RNAi-induced degradation of mRNA from the Nav1.8 sodium channel gene; to pharmaceutical compositions comprising such short interfering nucleic acids; recombinant vectors comprising such short interfering nucleic acids; a method for inhibiting translation of an mRNA; a method for inhibiting expression of a polypeptide; a method for blocking the membrane potential in a cell; a method for blocking the sodium current in a cell; and a method for inhibiting chronic pain.
    Type: Application
    Filed: October 16, 2012
    Publication date: May 2, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventor: Merck Sharp & Dohme Corp.
  • Tetrahydropyranyl cyclopentyl tetrahydroisoquinoline modulators of chemokine receptor activity
    Patent number: 7166614
    Abstract: The present invention is directed to compounds of the formula I: I(wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity.
    Type: Grant
    Filed: April 25, 2003
    Date of Patent: January 23, 2007
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Limited
    Inventors: Richard Jiao, Stephen D. Goble, Sander G. Mills, Gregori Morriello, Alexander Pasternak, Lihu Yang, Changyou Zhou, Gabor Butora, Shankaran Kothandaraman, Deodialsingh Guiadeen, Christopher Moyes
  • SUBSTITUTED PHENYL-SPLEEN TYROSINE KINASE (SYK) INHIBITORS
    Publication number: 20150232428
    Abstract: The invention provides certain substituted phenyl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
    Type: Application
    Filed: August 15, 2013
    Publication date: August 20, 2015
    Applicants: Merck Canada Inc., Merck Sharp & Dohme Corp.
    Inventors: Andrew M. Haidle, Jason Burch, Daniel Guay, Jacques Yves Gauthier, Joel Robichaud, Jean Francois Fournier, John Michael Ellis, Matthew Christopher, Solomon D. Kattar, Graham F. Smith, Alan B. Northrup
  • PROCESS FOR MAKING M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
    Publication number: 20180265493
    Abstract: This invention provides novel processes for the preparation of compounds such as 3-[(1S,2S)-2-hydroxycyclohexyl]-6-[(6-methylpyridin-3-yl)methyl]benzo[h]-quinazolin-4(3H)-one, salts and derivatives thereof. The compounds synthesized by the processes of the invention are useful for treating Alzheimer's disease and other diseases (e.g., cognitive impairment, schizophrenia, pain disorders, and sleep disorders) mediated by the muscarinic M1 receptor.
    Type: Application
    Filed: September 26, 2016
    Publication date: September 20, 2018
    Applicants: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Limited.
    Inventors: Qinghao Chen, Shane W. Krska, Lushi Tan, Peter E. Maligres, Jeremy Scott, Carl Baxter, Gavin William Stewart, Andrew Gibb
  • Cyclic FR-900520 microbial biotransformation agent
    Patent number: 5268281
    Abstract: Described is a process for producing a new immunosuppressant, a C-19/C-22 cyclic hemiketal (Compound I) biotransformation analog of FR-900520, under novel fermentation conditions utilizing the novel microorganism, Streptomyces sp. (Merck Culture Collection MA6968) ATCC No. 55279. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.
    Type: Grant
    Filed: September 28, 1992
    Date of Patent: December 7, 1993
    Assignee: Merck & Co., Inc.
    Inventors: George M. Garrity, Magda M. Gagliardi, Shieh-Shung T. Chen
  • Cyclic FR-900520 microbial biotransformation agent
    Patent number: 5268282
    Abstract: Described is a process for producing a new immunosuppressant, a C-19/C-22 cyclic hemiketal (Compound I) biotransformation analog of FR-900520, under novel fermentation conditions utilizing the novel microorganism, Streptomyces sp. (Merck Culture Collection MA6970) ATCC No. 55281. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.
    Type: Grant
    Filed: September 28, 1992
    Date of Patent: December 7, 1993
    Assignee: Merck & Co., Inc.
    Inventors: George M. Garrity, Shieh-Shung T. Chen
  • Immunosuppressant agent
    Patent number: 5290772
    Abstract: Described is a process for producing an immunosuppressant, "demethimmunomycin" (L-683,7411) a C-31 demethylated analog of L-683,590 under fermentation conditions utilizing the microorganism, Actinoplanacete sp, (Merck Culture Collection MA 6559) ATCC No. 53771. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.
    Type: Grant
    Filed: June 16, 1992
    Date of Patent: March 1, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Edward S. Inamine, Shieh-Shung T. Chen, Byron H. Arison, Linda S. Wicker
  • ANTAGONISTS OF PCSK9
    Publication number: 20130189278
    Abstract: Antagonists of human proprotein convertase subtilisin-kexin type 9 (“PCSK9”) are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for the use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.
    Type: Application
    Filed: January 15, 2013
    Publication date: July 25, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventor: Merck Sharp & Dohme Corp.
  • PHARMACEUTICAL COMPOSITIONS OF COMBINATIONS OF DIPEPTIDYL PEPTIDASE-4 INHIBITORS WITH SIMVASTATIN
    Publication number: 20140093564
    Abstract: The present invention is directed to novel pharmaceutical compositions comprising fixed dose combinations of a dipeptidyl peptidase-4 inhibitor (DPP-4 inhibitor), or a pharmaceutically acceptable salt thereof, and simvastatin, or pharmaceutically acceptable salt thereof, methods of preparing such pharmaceutical compositions, and methods of treating Type 2 diabetes and hypercholesterolemia with such pharmaceutical compositions. In particular, the invention is directed to pharmaceutical compositions comprising fixed-dose combinations of sitagliptin phosphate and simvastatin.
    Type: Application
    Filed: June 8, 2012
    Publication date: April 3, 2014
    Applicants: MERCK SHARP & DOHME LTD., Merck Sharp & Dohme Corp
    Inventors: Kathryn Bradley, Richard Elkes, Shaun Fitzpatrick, Robert Saklatvala, Mustafa Mohamed, Richard Kendall
  • Substituted phenyl-Spleen Tyrosine Kinase (Syk) inhibitors
    Patent number: 9353066
    Abstract: The invention provides certain substituted phenyl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
    Type: Grant
    Filed: August 15, 2013
    Date of Patent: May 31, 2016
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Andrew M. Haidle, Jason Burch, Daniel Guay, Jacques Yves Gauthier, Joel Robichaud, Jean Francois Fournier, John Michael Ellis, Matthew Christopher, Solomon D. Kattar, Graham F. Smith, Alan B. Northrup
  • Cyclic FR-900520 microbial biotransformation agent
    Patent number: 5283183
    Abstract: Described is a process for producing a new immunosuppressant, a C-19/C-22 cyclic hemiketal (Compound I) biotransformation analog of FR-900520, under novel fermentation conditions utilizing the novel microorganism, Streptomyces sp. (Merck Culture Collection MA6971) ATCC No. 55282. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.
    Type: Grant
    Filed: September 28, 1992
    Date of Patent: February 1, 1994
    Assignee: Merck & Co., Inc.
    Inventors: George M. Garrity, Shieh-Shung T. Chen
  • Imidazolyl analogs as syk inhibitors
    Patent number: 9487504
    Abstract: The present invention provides novel imidazole analogs of Formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
    Type: Grant
    Filed: June 18, 2013
    Date of Patent: November 8, 2016
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Jongwon Lim, Michael H. Reutershan, John Michael Ellis, Kaleen Konrad Childers, Anthony Donofrio, Michael D. Altman, Andrew M. Haidle, Anna Zabierek, Matthew Christopher, Jonathan Grimm, Jason Burch, Maria Emilia Di Francesco, Alessia Petrocchi, Christian Beaulieu, Vouy Linh Truong, Alan B. Northrup, Marc Blouin
  • ANTAGONISTS OF PCSK9
    Publication number: 20130115223
    Abstract: Antagonists of human proprotein convertase subtilisin-kexin type 9 (“PCSK9”) are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for the use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.
    Type: Application
    Filed: December 21, 2012
    Publication date: May 9, 2013
    Applicant: MERCK SHARP & DOHME CORP.
    Inventor: Merck Sharp & Dohme Corp.
  • Aminopyrimidines as Syk inhibitors
    Patent number: 8735417
    Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: May 27, 2014
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Michael D. Altman, Kenneth L. Arrington, Jason Burch, Bernard Cote, Jean-Francois Fournier, Jacques Yves Gauthier, Solomon Kattar, Sandra Lee Knowles, Jongwon Lim, Michelle R. Machacek, Alan B. Northrup, Michael H. Reutershan, Joel S. Robichaud, Adam J. Schell, Kerrie B. Spencer
  • Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
    Patent number: 9822107
    Abstract: The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein ring R1, R2, R3, R4, ring B, and the subscript r are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
    Type: Grant
    Filed: December 18, 2014
    Date of Patent: November 21, 2017
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Brian M. Andresen, Kenneth L. Arrington, Ryan D. Otte, John Michael Ellis, John W. Butcher, Alan B. Northrup, Joel S. Robichaud, Jacques Yves Gauthier, Jean-Francois Fournier
  • Microbial transformation product of L-679,934
    Patent number: 5268370
    Abstract: Described is a new immunosuppressant, L-683,519, a monodemethylated rearranged derivative of L-679,934, (FK-506) produced under fermentation conditions utilizing the microorganism, unidentified Actinomycete (Merck Culture Collection MA 6474) ATCC No. 53828. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.
    Type: Grant
    Filed: April 22, 1992
    Date of Patent: December 7, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Byron H. Arison, Edward S. Inamine, Shieh-Shung T. Chen, Linda S. Wicker
  • Microbial transformation product
    Patent number: 5270187
    Abstract: Described is a process for producing a new immunosuppressant, L-682,992, a C-13, C-31 demethylated ring-rearranged analog of L-679,934, under novel fermentation conditions utilizing the microorganism, Actinoplanacete Sp., (Merck Culture Collection MA 6559) ATCC No. 53771. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.
    Type: Grant
    Filed: January 21, 1992
    Date of Patent: December 14, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Shieh-Shung T. Chen, Byron H. Arison, Linda S. Wicker
  • Immunosuppressant compound
    Patent number: 4981792
    Abstract: Described is a process for producing a new immunosuppressant, "demethomycin" (L-682,993) a C-31 demethylated analog of L-679,934 under novel fermentation conditions utilizing the microorganism, Actinoplanacete sp., (Merck Culture Collection MA 6559) ATCC No. 53771. The macrolide immunosuppressant is useful in prevent human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.
    Type: Grant
    Filed: June 29, 1988
    Date of Patent: January 1, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Edward S. Inamine, Byron H. Arison, Shieh-Shung T. Chen, Linda S. Wicker
  • HCV NS3 protease inhibitors
    Patent number: 8987195
    Abstract: The present invention relates to hepatitis C virus (HCV) NS3 protease inhibitors containing a spirocyclic moeity, uses of such compounds, and synthesis of such compounds.
    Type: Grant
    Filed: August 6, 2013
    Date of Patent: March 24, 2015
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Thomas Bara, Sathesh Bhat, Dipshikha Biswas, Linda Brockunier, Duane A. Burnett, Samuel Chackalamannil, Mariappan V. Chelliah, Austin Chen, Martin Clasby, Vince J. Colandrea, Zhuyan Guo, Yongxin Han, Charles Jayne, Hubert Josien, Karen Marcantonio, Shouwu Miao, Santhosh Neelamkavil, Patrick Pinto, Murali Rajagopalan, Unmesh Shah, Francisco Velazquez, Srikanth Venkatraman, Yan Xia
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