Patents Assigned to Merck Sharp and Dohme
  • Patent number: 8551942
    Abstract: A lyophilized anti-fungal composition comprises (A) caspofungin, or a pharmaceutically acceptable salt thereof, in an effective amount; (B) one or more non-reducing sugars having a glass transition temperature Tg(s) of at least about 90° C.; and (C) an acetate buffer in an amount effective to provide a pH in a range of from about 5 to about 7; wherein the weight ratio of the one or more non-reducing sugars to caspofungin is in a range of from about 1.1:1 to about 10:1; the composition has a moisture content of about 0.8 wt. % or less; and the composition has a glass transition temperature Tg(c) of at least about 55° C. The lyophilized composition has good storage stability at temperatures up to and including room temperature. The composition can be reconstituted for use in preventing or treating fungal infections.
    Type: Grant
    Filed: September 27, 2012
    Date of Patent: October 8, 2013
    Assignee: Merck Sharp & Dohme, Corp.
    Inventors: Sachin Mittal, Hossain Jahansouz, Sutthilug Sottivirat
  • Patent number: 8552023
    Abstract: The present invention is directed to novel non-amidic linkers with branched termini derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. 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 CGRP is involved.
    Type: Grant
    Filed: August 11, 2009
    Date of Patent: October 8, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael R. Wood, June J. Kim, Harold G. Selnick, Shawn J. Stachel
  • Patent number: 8552193
    Abstract: The present invention is directed to alternative forms of the title phosphodiesterase 4 inhibitor which has the structural formula shown immediately below:
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: October 8, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Sophie-Dorothee Clas, Rafik Naccache, Hongshi Yu, Jerry Murry, Narayan Vanankaval
  • Patent number: 8552019
    Abstract: The instant invention provides for compounds of formula A that inhibit PDK1 activity: The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting PDK1 activity by administering the compound to a patient in need of treatment of cancer.
    Type: Grant
    Filed: November 24, 2009
    Date of Patent: October 8, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin A. Keenan, Alan B. Northrup
  • Patent number: 8551984
    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 15, 2010
    Date of Patent: October 8, 2013
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Michael H. Reutershan, Eric Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hua Zhou
  • Patent number: 8552022
    Abstract: Substituted cyclopropyl compounds of the formula I: are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
    Type: Grant
    Filed: August 3, 2010
    Date of Patent: October 8, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Harold B. Wood, Alan D. Adams, Jason W. Szewczyk, Yong Zhang, Meng Yang
  • Patent number: 8546404
    Abstract: Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
    Type: Grant
    Filed: June 5, 2007
    Date of Patent: October 1, 2013
    Assignee: Merck Sharp & Dohme
    Inventors: Alan B. Cooper, Yongqi Deng, Gerald W. Shipps, Jr., Neng-Yang Shih, Hugh Y. Zhu, Robert Sun, Joseph M. Kelly, Ronald J. Doll, Yang Nan, Tong Wang, Jagdish A. Desai, James J-S Wang, Youhao Dong, Vincent S. Madison, Li Xiao, Alan W. Hruza, M. Arshad Siddiqui, Ahmed A. Samatar, Sunil Paliwal, Hon-Chung Tsui, Azim Alan Celebi, Yiji Wu, Sobhana Babu Boga, Abdul-Basit Alhassan, Xiaolei Gao, Liang Zhu, Mehul Patel
  • Patent number: 8546420
    Abstract: The present invention relates to 4,5-ring annulated indole derivatives of formula (I), compositions comprising at least one 4,5-ring annulated indole derivatives, and methods of using the 4,5-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient, wherein ring Z of formula (I), is cyclohexyl, cyclohexenyl, 6-membered heterocycloalkyl, 6-membered heterocycloalkenyl, 6-membered aryl or 6-membered heteroaryl, wherein R1, R2, R3, R6, R7 and R10 are as described herein.
    Type: Grant
    Filed: December 17, 2007
    Date of Patent: October 1, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gopinadhan N. Anilkumar, Yueheng Jiang, Stuart B. Rosenblum, Srikanth Venkatraman, Francisco Velazquez, Neng-Yang Shih, F. George Njoroge, Joseph A. Kozlowski
  • Publication number: 20130251677
    Abstract: The present invention provides genetic markers on human chromosome 19 that are associated with a beneficial response to interferon alpha (IFN-?). These IFN-? response markers are useful, inter alia, to identify patients who are most likely to benefit from treatment with IFN-? pharmaceutical compositions and drug products, in methods of treating patients having a disease susceptible to treatment with an IFN-?, and in methods for selecting the most appropriate therapy for such patients.
    Type: Application
    Filed: May 30, 2013
    Publication date: September 26, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Arthur Bertelsen, Jacques Fellay, Dongliang Ge, David B. Goldstein, John G. McHutchison, Ping Qiu, Kevin Shianna, Jason S. Simon, Alexander J. Thompson, Thomas Urban
  • Patent number: 8541427
    Abstract: In its many embodiments, the present invention provides certain 2-imino-3-methyl pyrrolo pyrimidone compounds, including compounds Formula (II): and include tautomers, steroisomers, or pharmaceutically acceptable salts or solvates of said compounds, stereoisomers, or said tautomers, wherein R2, R3, R4, R5, R6, R7, R8, and R9 are each selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds, and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimer's Disease, are also disclosed.
    Type: Grant
    Filed: April 21, 2009
    Date of Patent: September 24, 2013
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Andrew W. Stamford, Zhaoning Zhu, Mihirbaran Mandal, Yusheng Wu, Jared N. Cumming, Xiaoxiang Liu, Guoqing Li, Ulrich Iserloh
  • Patent number: 8541572
    Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF—or combinations thereof.
    Type: Grant
    Filed: November 9, 2009
    Date of Patent: September 24, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joseph A. Kozlowski, Wensheng Yu, Michael K. C. Wong, Seong Heon Kim, Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, De-Yi Yang, Robert Feltz, Aneta Maria Kosinski, Guowei Zhou, Razia K. Rizvi, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristin E. Rosner, M. Arshad Siddiqui, Liping Yang
  • Patent number: 8541434
    Abstract: The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and pro-drugs of said compounds, wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.
    Type: Grant
    Filed: August 19, 2009
    Date of Patent: September 24, 2013
    Assignees: Merck Sharp & Dohme Corp., Southern Research Institute
    Inventors: Cecil D. Kwong, F. George Njoroge, Subramaniam Ananthan, Ashok Arasappan, Frank Bennett, Jeremy Clark, Anita T. Fowler, Feng Geng, Hollis S. Kezar, III, Joseph A. Maddry, John J. Piwinski, Robert C. Reynolds, Abhijit Roychowdhury, John A. Secrist, III, Neng-Yang Shih
  • Publication number: 20130243692
    Abstract: This invention relates to methods for evaluating the efficacy of an IGF1R inhibitor, such as an anti-IGF1R antibody, for the treatment of an Ewing's sarcoma tumor by determining the level of tumoral glucose metabolism. Tumoral glucose metabolism is determining at an early point in the treatment regimen by any of several methods known in the art including FDG-PET/CT scan.
    Type: Application
    Filed: May 20, 2013
    Publication date: September 19, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Brian Der-Hua Lu, Siu-Long Yao, Cynthia Seidel-Dugan, Yan Wang
  • Patent number: 8536193
    Abstract: The instant invention provides for substituted [1,2,4]triazolo[4,3-a]-1,5-naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms, preferably Akt1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity, especially Akt1 by administering the compound to a patient in need of treatment of cancer.
    Type: Grant
    Filed: May 27, 2009
    Date of Patent: September 17, 2013
    Assignees: Merck Sharp & Dohme Corp., MSD K.K.
    Inventors: Hidetomo Furuyama, Yasuhiro Goto, Nobuhiko Kawanishi, Mark E. Layton, Takashi Mita, Yoshio Ogino, Yu Onozaki, Michael A. Rossi, Toshihiro Sakamoto, Philip E. Sanderson, Jiabing Wang
  • Patent number: 8535887
    Abstract: The present invention provides genetic markers on human chromosome 19 that are associated with a beneficial response to interferon alpha (IFN-?). These IFN-? response markers are useful, inter alia, to identify patients who are most likely to benefit from treatment with IFN-? pharmaceutical compositions and drug products, in methods of treating patients having a disease susceptible to treatment with an IFN-?, and in methods for selecting the most appropriate therapy for such patients.
    Type: Grant
    Filed: May 21, 2010
    Date of Patent: September 17, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Arthur Bertelsen, Jacques Fellay, Dongliang Ge, David B. Goldstein, John G. McHutchison, Ping Qiu, Kevin Shianna, Jason S. Simon, Alexander J. Thompson, Thomas Urban
  • Patent number: 8530483
    Abstract: The present invention relates to novel amyloid binding compounds of formula (I) and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET/) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted azabenzoxazole derivatives, compositions, and therapeutic uses and processes for making such compounds, or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof, wherein: X is O or S; A and Y independently are N, or CH.
    Type: Grant
    Filed: May 28, 2009
    Date of Patent: September 10, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James C. Barrow, Scott Harrison, James Mulhearn, Cyrille Sur, David L. Williams, Scott Wolkenberg, Eric Hostetler
  • Patent number: 8530521
    Abstract: A compound having the structure wherein Y is selected from the group consisting of —C(O)OR2, —C(O)NHR8, —C(CH2)1-2OR3, OH, and or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.
    Type: Grant
    Filed: July 27, 2009
    Date of Patent: September 10, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Robert K. Baker, Kathleen M. Rupprecht, Michael Man-Chu Lo, Brent Whitehead
  • Patent number: 8530234
    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: December 8, 2009
    Date of Patent: September 10, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: David C. Kaslow, Andrew J. Bett
  • Publication number: 20130230855
    Abstract: Nucleic acids encoding various monocyte-derived proteins and related compositions, including purified proteins and specific antibodies are described. Methods of using such composition are also provided.
    Type: Application
    Filed: April 19, 2013
    Publication date: September 5, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: ELIZABETH BATES, NATHALIE FOURNIER, LIONEL CHALUS, PIERRE GARRONE
  • Patent number: 8524230
    Abstract: Novel methods and drug products for treating autoimmune ocular inflammatory disease are disclosed, which involve administration of agents that antagonize one or both of IL-17 and IL-23 activity.
    Type: Grant
    Filed: December 21, 2009
    Date of Patent: September 3, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Daniel J. Cua, Robert A. Kastelein, Van T. Tsai, Rachel Caspi, Phyllis Silver