Search Patents
  • New cyclic FR-900520 microbial biotransformation agent
    Patent number: 5290689
    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 MA6969) ATCC No. 55280. 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: March 1, 1994
    Assignee: Merck & Co., Inc.
    Inventors: George M. Garrity, Magda M. Gagliardi, Shieh-Shung T. Chen
  • Substituted phosphoramidate compounds and uses thereof
    Patent number: 10526363
    Abstract: The present invention is directed to Compounds of Formula (I) and salts thereof, wherein R1, R2, R3 and R4 are defined above herein. The present invention is also directed to uses of the compounds of Formula (I) to add phosphoramidate groups onto organic alcohols.
    Type: Grant
    Filed: August 14, 2015
    Date of Patent: January 7, 2020
    Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Ltd.
    Inventors: John Simon Edwards, Peter Richard Mullens, Edward Cleator, Bryon L. Simmons, Courtney K. Maguire, Jeremy Peter Scott, Nobuyoshi Yasuda, Yong-Li Zhong, Lisa F. Frey, Peter G. Dormer, Andrew Brunskill, Artis Klapars, Pu Qian, Yi Zhang, Baoqiang Wan, Eric Ashley
  • Process for making M1 receptor positive allosteric modulators
    Patent number: 10308633
    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: Grant
    Filed: September 26, 2016
    Date of Patent: June 4, 2019
    Assignees: 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
  • DIAGNOSIS AND PROGNOSIS OF BREAST CANCER PATIENTS
    Publication number: 20130116145
    Abstract: The present invention relates to genetic markers whose expression is correlated with breast cancer. Specifically, the invention provides sets of markers whose expression patterns can be used to differentiate clinical conditions associated with breast cancer, such as the presence or absence of the estrogen receptor ESR1, and BRCA1 and sporadic tumors, and to provide information on the likelihood of tumor distant metastases within five years of initial diagnosis. The invention relates to methods of using these markers to distinguish these conditions. The invention also relates to kits containing ready-to-use microarrays and computer software for data analysis using the statistical methods disclosed herein.
    Type: Application
    Filed: October 19, 2012
    Publication date: May 9, 2013
    Applicants: MERCK SHARP & DOHME CORP., THE NETHERLANDS CANCER INSTITUTE
    Inventors: The Netherlands Cancer Institute, Merck Sharp & Dohme Corp.
  • Heteroaryl piperidine glycine transporter inhibitors
    Patent number: 7825135
    Abstract: The present invention is directed to pyridyl, pyridazinyl, pyrimidinyl and pyrazinyl 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: Grant
    Filed: March 23, 2005
    Date of Patent: November 2, 2010
    Assignees: Merck Sharp & Dohme Limited, Merck Sharp & Dohme Corp.
    Inventors: Wesley Blackaby, Mark E. Duggan, David Hallett, George D. Hartman, Andrew S. Jennings, William H. Leister, Richard T. Lewis, Craig W. Lindsley, Elizabeth Naylor, Leslie J. Street, Yi Wang, David D. Wisnoski, Scott E. Wolkenberg, Zhijian Zhao
  • HIV PROTEASE INHIBITORS
    Publication number: 20160311786
    Abstract: The present invention is directed to 2,5,6-substituted morpholine derivatives and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: December 17, 2014
    Publication date: October 27, 2016
    Applicants: MERCK SHARP & DOHME CORP., MERCK CANADA INC.
    Inventors: John A. McCauley, Christian Beaulieu, David Jonathan Bennett, Christopher J. Bungard, Sheldon Crane, Thomas J. Greshock, Katharine M. Holloway, Daniel McKay, Carmela Molinaro, Oscar Miguel Moradei, Satyanarayana Tummanapalli, Vouy Linh Truong, Peter D. Williams
  • PROCESS FOR MAKING TETRACYCLIC HETEROCYCLE COMPOUNDS
    Publication number: 20180065985
    Abstract: The present invention is directed to a process for making Tetracyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2 and R3 are defined above herein. The present invention is also directed to compounds that may be useful as synthetic intermediates in the process of the invention.
    Type: Application
    Filed: November 9, 2017
    Publication date: March 8, 2018
    Applicants: Merck Sharpe & Dohme Corp., MSD R&D (China) Co., Ltd., Merck Sharp & Dohme Limited
    Inventors: Hongming Li, Jingjun Yin, Kevin M. Belyk, Kevin R. Campos, Qinghao Chen, Alan M. Hyde, Tetsuji Itoh, Artis Klapars, Matthew Thomas Tudge, Edward Cleator, Aaron M. Dumas, Louis-Charles Campeau, Yonggang Chen, Ji Qi, Wensong Xiao
  • LIQUID-CRYSTALLINE MEDIUM
    Publication number: 20130207038
    Abstract: The invention relates to a liquid-crystalline medium, characterised in that it contains one or more compounds of the formula IA, and at least one compound selected from the group of compounds of the formula IIA, IIB and IIC, in which RA, R2A, R2B, R2C, ring A, ring B, XA, Y1-6, L1-6, Z2, Z2?, o, p, q, v and (O)CvH2v+1 have the meanings indicated in Claim 1, and to the use thereof for electro-optical purposes, in particular for shutter glasses, 3D applications, in TN, PS-TN, STN, TN-TFT, OCB, IPS, PS-IPS, FFS, PS-FFS and PS-VA-IPS displays.
    Type: Application
    Filed: February 11, 2013
    Publication date: August 15, 2013
    Applicant: MERCK PATENT GMBH
    Inventor: Merck Patent GmbH
  • RENIN INHIBITORS
    Publication number: 20120035214
    Abstract: The present invention relates to biaryl piperidine-based renin inhibitor compounds, and their use in treating cardiovascular events and renal insufficiency.
    Type: Application
    Filed: April 1, 2010
    Publication date: February 9, 2012
    Applicants: Merck Canada Inc., Merck Sharp & Dohme Corp.
    Inventors: Daniel J. McKay, Melissa Arbour, Renee Aspiotis, Austin Chen, Pierre-Andre Fournier, Michel Gallant, Yongxin Han, Helene Juteau, Patrick Lacombe, Sebastien Laliberte, Sophie Lauzon, Carmela Molinaro, Paul O'Shea, Yeeman Ramtohul, Daniel Simard, Dwight MacDonald, Bruce Mackay, Christophe Mellon, Krista Morley, Chit Tsui, Sarah Jennifer Dolman, Greg Hughes, Jacob Janey
  • Method of treating colonic adenomas
    Patent number: 6649649
    Abstract: This invention is directed to a method of retarding or preventing the transformation of a colonic adenoma to a colonic adenocarcinoma comprising the administration to a patient with FAP or a patient with one or more of said adenomas a non-toxic therapeutically effective amount of NSAID, said amount effective to inhibit the PGHS-2 in said adenoma. The preferred method comprises the administration of a specific PGHS-2 inhibiting agent as defined herein.
    Type: Grant
    Filed: March 2, 1999
    Date of Patent: November 18, 2003
    Assignees: Merck & Co., Inc., Merck Frosst Canada, & Co.
    Inventors: Stacia Kargman, Thomas J. Simon, Jilly Evans
  • HIV protease inhibitors
    Patent number: 9834526
    Abstract: The present invention is directed to 2,5,6-substituted morpholine derivatives and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. 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: December 17, 2014
    Date of Patent: December 5, 2017
    Assignees: MERCK SHARP & DOHME CORP., MERCK CANADA INC.
    Inventors: John A. McCauley, Christian Beaulieu, David Jonathan Bennett, Christopher J. Bungard, Sheldon Crane, Thomas J. Greshock, Katharine M. Holloway, Daniel McKay, Carmela Molinaro, Oscar Miguel Moradei, Satyanarayana Tummanapalli, Vouy Linh Truong, Peter D. Williams
  • 4'-SUBSTITUTED NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS AND PREPARATIONS THEREOF
    Publication number: 20210154221
    Abstract: The present invention is directed to 4?-substituted nucleoside derivatives of Formula I and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC. The present invention also provides processes for the preparation of 4?-substituted nucleoside derivatives of Formula I and derivatives thereof.
    Type: Application
    Filed: February 3, 2021
    Publication date: May 27, 2021
    Applicants: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Limited
    Inventors: Mark McLaughlin, Edward Cleator, Jongrock Kong, Andrew William Gibson, David R. Lieberman, Alejandro Diequez Vazquez, Stephen Philip Keen, Michael J. Williams, Jeffrey C. Moore, Erika M. Milczek, Feng Peng, Kevin M. Belyk, Zhiguo Jake Song
  • HIV PROTEASE INHIBITORS
    Publication number: 20160296527
    Abstract: The present invention is directed to 5-heteroarylmorpholine derivatives and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: December 17, 2014
    Publication date: October 13, 2016
    Applicants: MERCK SHARP & DOHME CORP., MERCK CANADA INC.
    Inventors: John A. McCauley, Christian Beaulieu, David Jonathan Bennett, Christopher J. Bungard, Sheldon Crane, Thomas J. Greshock, Katharine M. Holloway, Helen Juteau, Daniel McKay, Carmela Molinaro, Oscar Miguel Moradei, Christian Nadeau, Daniel Simard, Satyanarayana Tummanapalli, Vouy Linh Truong, Karine M. Villeneuve, Peter D. Williams
  • Conjugates of leukotrienes with proteins
    Patent number: 4767745
    Abstract: Leukotrienes may be conjugated with various proteins such as Bovine Serum Albumin (BSA) and Hemocyanin from Giant Keyhole Limpets (KLH) using 1,5-difluoro-2,4-dinitrobenzene or 6-N-maleimidohexanoic acid chloride as coupling agents.These conjugates are useful as reagents in a newly developed immunoassay for leukotrienes, as well as having potential utility as chemical immunotherapeutic agents in the treatment of various allergic and chronic inflammatory diseases of the skin, lung, and airways, including asthma, allergic rhinitis, rheumatoid arthritis, and skin diseases such as psoriasis and eczema.
    Type: Grant
    Filed: May 5, 1986
    Date of Patent: August 30, 1988
    Assignees: Merck Frosst Canada, Inc., Merck & Co., Inc.
    Inventors: Robert N. Young, Joshua Rokach, Edward C. Hayes
  • NOVEL CRYSTALLINE FORMS OF A DIPEPTIDYL PEPTIDASE-IV INHIBITOR
    Publication number: 20140080884
    Abstract: Novel crystalline forms of (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel forms, processes to prepare these forms and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.
    Type: Application
    Filed: June 25, 2012
    Publication date: March 20, 2014
    Applicants: Merck Sharp & Dohme Ltd., Merck Sharp & Dohme Corp.
    Inventors: Itzia Arroyo, Davida Krueger, Ping Chen, Aaron Moment, Tesfaye Biftu, Faye Sheen, Yanfeng Zhang
  • 4'-SUBSTITUTED NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS AND PREPARATIONS THEREOF
    Publication number: 20190022115
    Abstract: The present invention is directed to 4?-substituted nucleoside derivatives of Formula (I) and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC. The present invention also provides processes for the preparation of 4?-substituted nucleoside derivatives of Formula (I) and derivatives thereof.
    Type: Application
    Filed: September 16, 2016
    Publication date: January 24, 2019
    Applicants: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Limited
    Inventors: Vinay M. Girijavallabhan, Mark McLaughlin, Edward Cleator, Jongrock Kong, Andrew William Gibson, David R. Lieberman, Alejandro Dieguez Vazquez, Stephen Philip Keen, Michael J. Williams, Jeffrey C. Moore, Erika M. Milczek, Feng Peng, Kevin M. Belyk, Zhiguo Jake Song
  • Immunosuppressant-producing culture
    Patent number: 5202258
    Abstract: Described is a new microorganism, Actinoplanacete sp., (Merck Culture Collection MA 6559) ATCC No. 53771. The microorganism acts as a demethylating agent and can produce the new immunosuppressants, "demethomycin" (L-682,993) a C-31 demethylated analog of L-679,934, and "demethimmunomycin" (L-683,742) a C-31 demethylated analog of L-683,590, under novel fermentation conditions. These macrolide immunosuppressants are useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.
    Type: Grant
    Filed: March 9, 1992
    Date of Patent: April 13, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Shieh-Shung T. Chen, Byron H. Arison, George M. Garrity, Edward S. Inamine, Sagrario Mochales, Linda S. Wicker
  • Method for Production and Use of Mite Group 1 Proteins
    Publication number: 20130157310
    Abstract: The present invention includes a method to produce a recombinant mite Group 1 protein in a methyltrophic yeast or an Escherichia coli microorganism. The present invention also relates to a recombinant mite Group 1 protein obtained by such a method, such a recombinant protein being able to selectively bind IgE or cause proliferation of a T cell that proliferates in response to a native mite Group 1 protein. Also included in the present invention is the use of such a recombinant mite Group 1 protein to detect mite allergy or to reduce an allergic response to a mite Group 1 protein. The present invention also includes novel mite Group 1 nucleic acid molecules, proteins, recombinant molecules, and recombinant cells, as well as uses thereof.
    Type: Application
    Filed: February 21, 2013
    Publication date: June 20, 2013
    Applicant: MERCK PATENT GMBH
    Inventor: Merck Patent GmbH
  • Bipyridylaminopyridines as Syk inhibitors
    Patent number: 9145391
    Abstract: The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, or are prodrugs thereof, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis and cancer.
    Type: Grant
    Filed: May 4, 2012
    Date of Patent: September 29, 2015
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Denis Deschenes, Michael D. Altman, John Michael Ellis, Christian Fischer, Andrew M. Haidle, Solomon D. Kattar, Alan B. Northrup, Adam J. Schell, Graham F. Smith, Brandon M. Taoka, Corey Bienstock, Maria Emilia Di Francesco, Anthony Donofrio, Scott Peterson, Kerrie B. Spencer, James Patrick Jewell, Amjad Ali, David Jonathan Bennett, Qun Dang, John Wai
  • BIARYL SPIROAMINOOXAZOLINE ANALOGUES AS ALPHA2C ADRENERGIC RECEPTOR MODULATORS
    Publication number: 20130045914
    Abstract: In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: October 18, 2012
    Publication date: February 21, 2013
    Applicant: Merck Sharp & Dohme Corp
    Inventor: Merck Sharp & Dohme Corp.
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