Search Patents
  • Crystalline forms of a dipeptidyl peptidase-IV inhibitors
    Patent number: 9181262
    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: Grant
    Filed: October 6, 2014
    Date of Patent: November 10, 2015
    Assignees: Merck Sharp & Dohme Corp, Merck Sharp & Dohme Ltd.
    Inventors: Itzia Z. Arroyo, Davida Krueger, Ping Chen, Aaron J. Moment, Tesfaye Biftu, Faye Sheen, Yanfeng Zhang
  • TRIAZOLYL DERIVATIVES AS SYK INHIBITORS
    Publication number: 20150239866
    Abstract: Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
    Type: Application
    Filed: September 24, 2013
    Publication date: August 27, 2015
    Applicants: MERCK CANADA INC., MERCK SHARP & DOHME CORP.
    Inventors: Michelle R. MACHACEK, Eric T. ROMEO, Solomon D. KATTAR, Matthew CHRISTOPHER, Michael D. ALTMAN, Alan B. NORTHRUP, John Michael ELLIS, Brendan O BOYLE, Anthony DONOFRIO, Jonathan GRIMM, Michael H. REUTERSHAN, Kaleen Konrad CHILDERS, Ryan D. OTTE, Brandon CASH, Yves DUCHARME, Andrew M. HAIDLE, Kerrie SPENCER, Dilrukshi VITHARANA, Lingyun WU, Li ZHANG, Peng ZHANG, Christian BEAULIEU, Daniel GUAY
  • Process for producing immunosuppressant agent L-683942 by fermentation
    Patent number: 5272068
    Abstract: Described is a new process for producing the immunosuppressant, L-683,742, a C-31 demethylated, derivative of L-683,590 (FK-520), produced under fermentation conditions utilizing the new mutant microorganism, Streptomyces hygroscopicus subsp. ascomyceticus (Merck Culture Collection MA 6646) ATCC No. 53855, being a blocked mutant of Streptomyces hygroscopicus subsp. ascomyceticus (MA 6475) ATCC No. 14891. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.
    Type: Grant
    Filed: July 23, 1991
    Date of Patent: December 21, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Carolyn L. Ruby, Susan J. Danis, Byron H. Arison
  • Leukotriene by amides and hydrazides
    Patent number: 4954638
    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: August 1, 1988
    Date of Patent: September 4, 1990
    Assignees: Merck Frosst Canada, Inc., Merck & Co., Inc.
    Inventors: Robert N. Young, Joshua Rokach, Edward C. Hayes
  • Tetrahydropyranyl cyclopentyl tetrahydropyridopyridine modulators of chemokine receptor activity
    Patent number: 6812234
    Abstract: The present invention is directed to compounds of the formula 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. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
    Type: Grant
    Filed: April 29, 2003
    Date of Patent: November 2, 2004
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Ltd.
    Inventors: Richard Jiao, Gregori Morriello, Lihu Yang, Stephen D. Goble, Sander G. Mills, Alexander Pasternak, Changyou Zhou, Gabor Butora, Shankaran Kothandaraman, Deodialsingh Guiadeen, Christopher Moyes, Cheng Tang
  • HIV protease inhibitors
    Patent number: 9737545
    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: Grant
    Filed: December 17, 2014
    Date of Patent: August 22, 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, Helen Juteau, Daniel McKay, Carmela Molinaro, Oscar Miguel Moradei, Christian Nadeau, Daniel Simard, Satyanarayana Tummanapalli, Vouy Linh Truong, Karine M. Villeneuve, Peter D. Williams
  • PROCESS FOR THE PREPARATION OF INTERMEDIATES USEFUL FOR MAKING (2S,5R)-7-OXO-N-PIPERIDIN-4-YL-6-(SULFOXY)-l,6-DIAZABICYCLO[3.2.1]OCTANE-2-CARBOXAMIDE
    Publication number: 20220194941
    Abstract: The invention is related to the preparation of protected piperidine carboxylates suitable for use as intermediates that lead, via a series of additional process steps, including a sulfation of a hydroxy urea compound, to the preparation of the beta lactamase inhibitor (2S,5R)-7-oxo-N-piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide.
    Type: Application
    Filed: April 21, 2020
    Publication date: June 23, 2022
    Applicants: Merck Sharp & Dohme Corp., Merck Sharp & Dohme (UK) Limited
    Inventors: John Y.L. Chung, Tetsuji Itoh, Jungchul Kim, Jacob Henry Waldman, Debra J. Wallace, Andrew Wood, Feng Xu, Andrew Gibson, Jeremy Peter Scott
  • 4-Hydroxy-5-substituted-3-(2H)-isothiazolone-1,1-dioxide derivatives useful in treating urinary tract calcium oxalate lithiasis
    Patent number: 4428956
    Abstract: 4-Hydroxy-5-substituted-3(2H)-isothiazolone-1,1-dioxide derivatives of the formula: ##STR1## where X and Y are independently selected from the group consisting of hydrogen, halogen, and C.sub.1-6 alkyl; provided that positions 2 and 6 of the substituted phenyl moiety may not be substituted; and n is 0 or 1;or a pharmaceutically acceptable salt thereof; useful in treating urinary tract, especially renal calcium oxalate lithiasis.
    Type: Grant
    Filed: December 29, 1980
    Date of Patent: January 31, 1984
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme (I.A.) Corp.
    Inventors: Edward J. Cragoe, Jr., Clarence S. Rooney, Haydn W. R. Williams
  • Cyclcic FR-900520 microbial biotransformation agent
    Patent number: 5221625
    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 MA6963) ATCC No. 55230. 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: January 10, 1992
    Date of Patent: June 22, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Shieh-Shung T. Chen, Raymond F. White, Georgette Dezeny, Brian R. Petuch, George M. Garrity, Byron H. Arison, Amy M. Bernick
  • Process for making tetracyclic heterocycle compounds
    Patent number: 10202401
    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: Grant
    Filed: November 9, 2017
    Date of Patent: February 12, 2019
    Assignees: MSD R&D CN CO., LTD, MERCK SHARP & DOHME CORP., 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
  • Crystalline forms of a dipeptidyl peptidase-IV inhibitor
    Patent number: 8895603
    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: Grant
    Filed: June 25, 2012
    Date of Patent: November 25, 2014
    Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Ltd.
    Inventors: Itzia Arroyo, Davida Krueger, Ping Chen, Aaron Moment, Tesfaye Biftu, Faye Sheen, Yanfeng Zhang
  • Process for producing immunosuppressant agent
    Patent number: 5324644
    Abstract: Described is a new process for producing the immunosuppressant, L-682,993, a C-31 demethylated derivative of L-679,934 (FK-506), produced under fermentation conditions utilizing the new mutant microorganism Streptomyces sp. (Merck Culture Collection MA 7017) ATCC No. 55334, being a blocked second generation mutant of Streptomyces sp. (MA 6858) ATCC No. 55098. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.
    Type: Grant
    Filed: July 28, 1992
    Date of Patent: June 28, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Carolyn L. Ruby, Christine C. Chung, Byron H. Arison
  • L-683,590 microbial transformation product
    Patent number: 5138052
    Abstract: Described is a new L-679,934 (FK-506) antagonist, L-686,292, a C-15, C-31 bisdemethylated, derivative of L-683,590, produced under fermentation conditions utilizing the microorganism, Actinoplanacete sp. (Merck Culture Collection MA 6559) ATCC No. 53771. The macrolide reverses the immunosuppressant action of L-679,934 (FK-506), and can be used diagnostically as a tool to determine the presence of FK-506 macrolide type immunosuppressants in natural product broths, distinguishing such immunosuppressants from other chemical families such as the cycloporins.
    Type: Grant
    Filed: March 5, 1991
    Date of Patent: August 11, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Shieh-Shung T. Chen, Linda S. Wicker, Byron H. Arison
  • Microbial immunoregulant
    Patent number: 5431896
    Abstract: Described is a new immunosuppressant, L-687,819, a C-31 demethylated derivative of L-683,795 (FK-523), produced under fermentation conditions utilizing the new mutant microorganism, Streptomyces hygroscopicus subsp. ascomyceticus (Merck Culture Collection MA 6646) ATCC No. 53855, being a blocked mutant of Streptomyces hygroscopicus subsp. ascomyceticus (MA 6475) ATCC No. 14891. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.
    Type: Grant
    Filed: July 30, 1992
    Date of Patent: July 11, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Louis Kaplan, Robert P. Borris, Kevin M. Byrne, Linda S. Wicker, Deborah L. Zink
  • Extracts from kibdelos porangium as antibacterial agents
    Patent number: 9126983
    Abstract: The present invention relates to novel compounds of formulae (I) and (II) and pharmaceutically acceptable salts thereof that are useful in the treatment and/or prevention of human and animal bacterial infections and associated diseases and conditions; compositions containing such compounds; derivation of such compounds by fermentation and isolation, partial synthesis and total synthesis; methods of inhibiting bacterial growth; methods of treating, preventing or controlling bacterial infection; biologically pure cultures of bacterial strains from which such compounds may be produced; and processes for preparing compositions containing such compounds.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: September 8, 2015
    Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme de Espana SA
    Inventors: Sheo Singh, Jon D. Polishook, Deborah L. Zink, Olga Genilloud, Michael Goetz, Francisca Vicente, David Brian Olsen, Scott Knoble Smith
  • Method for identifying inhibitors for apopain based upon the crystal structure of the apopain: Ac-DEVD-CHO complex
    Patent number: 5834228
    Abstract: The apopain:Ac-DEVD-CHO complex has been crystallized and its structure determined by x-ray crystallography. Based upon this crystal structure of the complex, a method for identifying inhibitors of apopain is presented which comprises designing putative inhibitors having specific contacts with apopain, making the putative inhibitors, and testing the putative inhibitors for their ability to inhibit apopain.
    Type: Grant
    Filed: February 13, 1997
    Date of Patent: November 10, 1998
    Assignees: Merck & Co., Inc., Merck Frosst Canada, Inc.
    Inventors: Joseph W. Becker, Donald W. Nicholson, Jennifer Rotonda, Nancy A. Thornberry, Kimberly M. Fazil, Michel Gallant, Yves Gareau, Marc Labelle, Erin P. Peterson, Dita M. Rasper, Rejean Ruel, John P. Vaillancourt
  • Triazolyl derivatives as Syk inhibitors
    Patent number: 9586931
    Abstract: Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
    Type: Grant
    Filed: September 24, 2013
    Date of Patent: March 7, 2017
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Michelle R. Machacek, Eric T. Romeo, Solomon D. Kattar, Matthew Christopher, Michael D. Altman, Alan B. Northrup, John Michael Ellis, Brendan O'Boyle, Anthony Donofrio, Jonathan Grimm, Michael H. Reutershan, Kaleen Konrad Childers, Ryan D. Otte, Brandon Cash, Yves Ducharme, Andrew M. Haidle, Kerrie Spencer, Dilrukshi Vitharana, Lingyun Wu, Li Zhang, Peng Zhang, Christian Beaulieu, Daniel Guay
  • 4-Hydroxy-5-substituted-3(2H)-isothiazolone-1,1-dioxide derivatives useful in treating urinary tract calcium oxalate lithiasis
    Patent number: 4431652
    Abstract: 4-Hydroxy-5-substituted-3(2H)-isothiazolone-1,1-dioxide derivatives of the formula: ##STR1## where X and Y are independently selected from the group consisting of hydrogen, halogen, and C.sub.1-6 alkyl; provided that positions 2 and 6 of the substituted phenyl moiety may not be substituted by C.sub.3-6 alkyl; or a pharmaceutically acceptable salt thereof;useful in treating urinary tract, especially renal calcium oxalate lithiasis.
    Type: Grant
    Filed: December 29, 1980
    Date of Patent: February 14, 1984
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme (I.A.) Corp.
    Inventors: Edward J. Cragoe, Jr., Clarence S. Rooney, Haydn W. R. Williams
  • C-21 hydroxylated FK-506 antagonist
    Patent number: 5225403
    Abstract: Described is a process for producing a new FK-506 antagonist agent, a C-21 hydroxylated analog of FR-900520 under novel fermentation conditions utilizing the novel microorganism, Streptomyces hygroscopicus (Merck Culture Collection MA 6832) ATCC No. 55166. The macrolide antagonist is useful in preventing and/or counteracting accidental or inadvertent FK-506 overdosage in an FK-506 therapeutic program designed to prevent autoimmune diseases or human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.
    Type: Grant
    Filed: June 25, 1991
    Date of Patent: July 6, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Laszlo R. Treiber, Georgette Dezeny, Lawrence F. Colwell, Jr., Byron H. Arison, Francis Dumont
  • ELECTRONIC DEVICE WITH BANK STRUCTURES
    Publication number: 20190181203
    Abstract: Electronic device and associated methods with multiple well areas located on a common substrate, where each well area is defined by at least three bank structures that form the side walls of the well area. Within each well area, there are at least two electrode segments where the electrode segments are separated laterally by at least one insulating bank where the insulating bank(s) are thicker than the electrode segments. There is at least one charge transporting layer completely filling the well area in direct contact and overlying both the electrode segments and the insulating bank(s). The well areas are filled using solution methods such as inkjet. Such devices have improved uniformity across the active areas.
    Type: Application
    Filed: August 14, 2017
    Publication date: June 13, 2019
    Applicants: Merck Patent GmbH, Merck Patent GmbH
    Inventors: Li Wei TAN, Peter LEVERMORE, Daniel WALKER
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