Patents Assigned to Merck Sharp & Dohme Ltd.
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Publication number: 20210309650Abstract: The present invention is directed to processes for preparing a diazepane compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is further directed to crystalline forms of this diazepane compound and pharmaceutical compositions thereof.Type: ApplicationFiled: July 16, 2015Publication date: October 7, 2021Applicants: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Ltd.Inventors: Carl A. Baxter, Edward Cleator, Faye Sheen, Shane W. Krska, Gavin Stewart, Neil Strotman, Debra J. Wallace, Timothy Wright
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Patent number: 10568968Abstract: Provided are methods of treatment for tumors. In particular, methods are provided for use of a chemically modified IL-10 to treat tumors.Type: GrantFiled: November 3, 2017Date of Patent: February 25, 2020Assignee: Merck Sharp & Dohme Ltd.Inventors: Martin Oft, Catherine Sheppard, John Brian Mumm, Lingling Wu
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Patent number: 10526363Abstract: 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: GrantFiled: August 14, 2015Date of Patent: January 7, 2020Assignees: 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
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Patent number: 10471126Abstract: Interleukin-10 (IL-10) conjugated via a linker to one or more polyethylene glycol (PEG) molecules at a single amino acid residue of the IL-10, and a method for preparing the same, are provided. The method produces a stable mono-pegylated IL-10, which retains IL-10 activity, where pegylation is selective for the N-terminus on one subunit of IL-10 with little or no formation of monomeric IL-10. The method also provides a substantially homogenous population of mono-PEG-IL-10.Type: GrantFiled: February 6, 2018Date of Patent: November 12, 2019Assignee: Merck Sharp & Dohme LtdInventors: Seoju Lee, David C. Wylie, Susan V. Cannon-Carlson
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Patent number: 9937153Abstract: The present invention is directed to stable, oral pharmaceutical formulations of dipeptidyl peptidase-4 inhibitors, such as omarigliptin. Such pharmaceutical formulations comprise omarigliptin; and neutral excipients, wherein the neutral excipient is present in the amount of at least 75% by weight of the pharmaceutical formulation and comprises at least one non-reducible sugar diluent or a mixture of non-reducible sugar diluents.Type: GrantFiled: August 25, 2014Date of Patent: April 10, 2018Assignees: Merck Sharp & Dohme LTD., Merck Sharp & Dohme Corp.Inventors: Vincent Brett Cooper, Kathryn Alanna Bradley, Samuel Robert Pygall, Rajan Gupta, Madison Paige Stanford, Lin Xie
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Patent number: 9527855Abstract: A process for the preparation of pyrazolopyrolidines of structural formula I: and W is or P, wherein in P is an amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.Type: GrantFiled: October 2, 2015Date of Patent: December 27, 2016Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Ltd.Inventors: Michael J. Zacuto, Robert F. Dunn, Aaron J. Moment, Jacob M. Janey, David Lieberman, Faye Sheen, Nadine Bremeyer, Jeremy Scott, Jeffrey T. Kuethe, Lushi Tan, Qinghao Chen
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Patent number: 9187488Abstract: A process for the preparation of pyrazolopyrolidines of structural formula I: and W is or P, wherein in P is an amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.Type: GrantFiled: June 25, 2012Date of Patent: November 17, 2015Assignees: Merck Sharp & Dohme Corp, Merck Sharp & Dohme Ltd.Inventors: Michael J. Zacuto, Robert F. Dunn, Aaron J. Moment, Jacob M. Janey, David Lieberman, Faye Sheen, Nadine Bremeyer, Jeremy Scott, Jeffrey T. Kuethe, Lushi Tan, Qinghao Chen
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Patent number: 9181262Abstract: 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: GrantFiled: October 6, 2014Date of Patent: November 10, 2015Assignees: 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
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Patent number: 8895603Abstract: 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: GrantFiled: June 25, 2012Date of Patent: November 25, 2014Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Ltd.Inventors: Itzia Arroyo, Davida Krueger, Ping Chen, Aaron Moment, Tesfaye Biftu, Faye Sheen, Yanfeng Zhang
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Publication number: 20140107346Abstract: A process for the preparation of pyrazolopyrolidines of structural formula I: and W is or P, wherein in P is an amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.Type: ApplicationFiled: June 25, 2012Publication date: April 17, 2014Applicants: Merck Sharp & Dohme Ltd., Merck Sharp & Dohme Corp.Inventors: Michael J. Zacuto, Robert F. Dunn, Aaron J. Moment, Jacob M. Janey, David Lieberman, Faye Sheen, Nadine Bremeyer, Jeremy Scott, Jeffrey T. Kuethe
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Publication number: 20140093564Abstract: 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: ApplicationFiled: June 8, 2012Publication date: April 3, 2014Applicants: MERCK SHARP & DOHME LTD., Merck Sharp & Dohme CorpInventors: Kathryn Bradley, Richard Elkes, Shaun Fitzpatrick, Robert Saklatvala, Mustafa Mohamed, Richard Kendall
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Publication number: 20140080884Abstract: 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: ApplicationFiled: June 25, 2012Publication date: March 20, 2014Applicants: Merck Sharp & Dohme Ltd., Merck Sharp & Dohme Corp.Inventors: Itzia Arroyo, Davida Krueger, Ping Chen, Aaron Moment, Tesfaye Biftu, Faye Sheen, Yanfeng Zhang
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Patent number: 7834222Abstract: A process for the preparation of a the formula (I): which process comprises the intramolecular cyclopropanation of an epoxide of me formula (II); in the presence of 0.05 to 0.75 equivalents of a secondary amine base and at least one equivalent of an alkyl lithium base, wherein R R1, R2 and R3 are each hydrogen or C1-4 alkyl or R1 and R2 are linked to form- a C3-7 cycloaUcyl or C3-7 cycloalkenyl ring.Type: GrantFiled: August 1, 2006Date of Patent: November 16, 2010Assignee: Merck Sharp & Dohme Ltd.Inventors: Matthew Bio, Karel Marie Joseph Brands, Edward Cleator
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Patent number: 7728022Abstract: Compounds of formula I: are disclosed. The compounds are useful in treating or preventing diseases associated with deposition of A? in the brain.Type: GrantFiled: May 6, 2005Date of Patent: June 1, 2010Assignee: Merck Sharp & Dohme Ltd.Inventors: Michela Bettati, Ian Churcher, Victoria Alexandra Doughty, Timothy Harrison, Emmanuela Nizi, Adam Smith
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Patent number: 7638629Abstract: Compounds of formula I: selectively inhibit production of A?(1-42) and hence are useful in treatment or prevention of disease associated with deposition of ?-amyloid in the brain.Type: GrantFiled: October 20, 2005Date of Patent: December 29, 2009Assignee: Merck Sharp & Dohme Ltd,Inventors: Joanne Clare Hannam, Janusz Jozef Kulagowski, Andrew Madin, Mark Peter Ridgill, Eileen Mary Seward
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Patent number: 7514459Abstract: Compounds of formula I: are potent inhibitors of gamma-secretase and hence find use in treatment or prevention of diseases associated with deposition of ?-amyloid.Type: GrantFiled: September 16, 2004Date of Patent: April 7, 2009Assignee: Merck Sharp & Dohme Ltd.Inventors: Ian James Collins, Joanne Clare Hannam, Andrew Madin, Mark Peter Ridgill
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Patent number: 7468393Abstract: Compounds of formula I: are potent and selective antagonists of the human 5-HT2A receptor, and hence useful in treatment of a variety of adverse conditions of the CNS.Type: GrantFiled: April 27, 2007Date of Patent: December 23, 2008Assignee: Merck Sharp & Dohme Ltd.Inventors: Jose Luis Castro Pineiro, Laura Catherine Cooper, Myra Gilligan, Alexander Charles Humphries, Peter Alan Hunt, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Monique Bodil Van Niel, Kevin Wilson
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Patent number: 7449585Abstract: Compounds of formula (I), which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1).Type: GrantFiled: November 12, 2004Date of Patent: November 11, 2008Assignee: Merck Sharp & Dohme Ltd.Inventors: Frank Burkamp, Stephen Robert Fletcher
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Patent number: 7442701Abstract: The present invention provides a compound of formula (I): wherein V represents NR5, O, S, SO or S(O)2; W and X each independently represent CH or N; Y represents N, CH or C—Ar2, with the proviso that at least one, but no more than two, of W, X and Y are N; Z represents CH or C—Ar2, with the proviso that when Y is N or CH then Z is C—Ar2, and with the further proviso that when Y is C—Ar2 then Z is CH; Ar1 represents a fused 9 or 10 membered heterobicyclic ring system containing one, two, three or four heteroatoms selected from nitrogen, oxygen and sulfur, wherein at least one of the rings in said ring system is aromatic; Ar2 represents an aromatic ring selected from phenyl, pyridyl, pyrimidinyl and pyridazinyl which is optionally fused and substituted; R1 represents halogen, hydroxy, oxo, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6alkyl, hydroxyC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, hydroxyC1-6alkoxy, C3-7cycloalkyl, C3-7cycloalkoxy, C3-5cycloalkylC1-4alkyl, cyano, nitro, SR6, SOR6, SO2R6, COR6, NR3COR6, CONType: GrantFiled: November 14, 2003Date of Patent: October 28, 2008Assignee: Merck Sharp & Dohme Ltd.Inventors: Peter Blurton, Frank Burkamp, Stephen Robert Fletcher, Gregory John Hollingworth, A. Brian Jones, Edward Giles McIver, Christopher Richard Moyes, Lauren Rogers
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Patent number: 7435748Abstract: Compounds of formula I: inhibit gamma-secretase and hence find use in treatment of Alzheimer's disease.Type: GrantFiled: December 14, 2006Date of Patent: October 14, 2008Assignee: Merck Sharp & Dohme Ltd.Inventors: Jose Luis Castro Pineiro, Ian James Collins, Timothy Harrison