Patents Assigned to Merck Sharp & Dohme
  • Publication number: 20140088094
    Abstract: The invention provides tetrahydroquinoline and related compounds, pharmaceutical compositions, methods of inhibiting ROR? activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydroquinoline and related compounds are provided.
    Type: Application
    Filed: November 8, 2011
    Publication date: March 27, 2014
    Applicants: Merck Sharp & Dohme Corp., Lycera Corporation
    Inventors: Gary D. Glick, Peter L. Toogood, Arthur Glenn Romero, Chad A. Van Huis, Thomas Daniel Aicher, Carl Kaub, Matthew N. Mattson, William David Thomas, Karin Ann Sttein, Erik Krogh-Jespersen, Zhan Wang
  • Publication number: 20140088048
    Abstract: A compound having the structure or a pharmaceutically acceptable salt thereof, wherein R6 is hydrogen, —OH, —C1-6alkyl, —OC1-6alkyl, aryl, or halogen, or together with R7, forms an oxo group, or together with R7 and the atom to which they are attached, form a 5-7-membered carbocycle ring or a 5-7-membered heterocyclic ring having 1, 2, or 3 heteroatoms, wherein alkyl and aryl are unsubstituted or independently mono-, di-, or tri-substituted with R14; R7 is hydrogen, C1-6alkyl, —CF3, aryl, —O-aryl, —O—C1-6alkyl, —C(O)OC1-6alkyl, —C(R15R16)OH, a 5-7-membered heteroaryl having 1, 2, 3 or 4 nitrogen atoms, or halogen, or together with R6, forms an oxo group, or together with R6 and the atom to which they are attached, form a 5-7-membered carbocycle ring or a 5-7-membered heterocyclic ring having 1, 2, or 3 heteroatoms wherein alkyl, aryl and heteroaryl are unsubstituted or independently mono-, di- or tri-substituted with R14; R12 is hydrogen, C1-6alkyl, or —(CH2)1-2OH, or together with R13 and the nitr
    Type: Application
    Filed: April 27, 2012
    Publication date: March 27, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-Chu Lo, Lin Yan
  • Patent number: 8680271
    Abstract: A process for the preparation of the compound of Formula (I) is described.
    Type: Grant
    Filed: March 21, 2011
    Date of Patent: March 25, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Melodie D. Christensen, Jungchul Kim
  • Patent number: 8679472
    Abstract: This application covers a novel PEGylated interferon and a novel crystalline form of interferon which are useful, inter alia, for detailed structural analysis of interferon as well as treatment and prevention of viral infections and hyperproliferative diseases such as leukemia.
    Type: Grant
    Filed: October 5, 2007
    Date of Patent: March 25, 2014
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Paul Reichert, Marianna Marshall Long, Alan W. Hruza, Peter Orth, Tattanahalli L. Nagabhushan
  • Patent number: 8680116
    Abstract: The present invention is directed to quinolinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: July 19, 2010
    Date of Patent: March 25, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Pablo DeLeon, Melissa Egbertson, Ivory D. Hills, Adam Wayne Johnson, Michelle Machacek
  • Patent number: 8680294
    Abstract: Processes useful for the preparation of a Compound of Formula I: Formula (I). Intermediates useful for the preparation of the compound of Formula I, and processes useful for preparing said intermediates are disclosed.
    Type: Grant
    Filed: July 27, 2010
    Date of Patent: March 25, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John Traverse, William M. Leong, Steven P. Miller, Jennifer Albaneze-Walker, Thomas J. Hunter, Lijun Wang, Hongbiao Liao, Ashok Arasappan, Scott T. Trzaska, Randi M. Smith, Azzeddine Lekhal, Stephane L. Bogen, Jianshe Kong, Frank Bennett, F. George Njoroge, Marc Poirier, Shen-Chun Kuo, Yonggang Chen, Kenneth S. Matthews, Patrice Demonchaux, Amadeo Ferreira
  • 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
  • Patent number: 8673630
    Abstract: The present invention provides polynucleotides for enhanced expression of a target gene such as an immunoglobulin. Methods of expressing a target gene using the polynucleotides of the invention are also covered.
    Type: Grant
    Filed: November 12, 2009
    Date of Patent: March 18, 2014
    Assignee: Merck, Sharp & Dohme Corp.
    Inventor: Deba P. Saha
  • Patent number: 8673924
    Abstract: In its many embodiments, the present invention provides a method of inhibiting one or more cyclin dependent kinases in a patient comprising administering to said patient a therapeutically effective amount of at least one pyrazolo[1,5-a]pyrimidine compound or a pharmaceutical composition comprising such compound, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: April 20, 2007
    Date of Patent: March 18, 2014
    Assignees: Merck Sharp & Dohme Corp., Pharmacopeia, LLC
    Inventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Alan Mallams, Carmen S. Alvarez, Kartik M. Keertikar, Jocelyn Rivera, Tin-Yau Chan, Vincent S. Madison, Thierry O. Fischmann, Lawrence W. Dillard, Vinh D. Tran, Zhenmin He, Ray Anthony James, Haengsoon Park, Vidyadhar M. Paradkar, Douglas Walsh Hobbs, Paul Kirschmeier, Rajat Bannerji
  • Patent number: 8674093
    Abstract: The present invention is directed to processes for preparing a pyridyl piperidine 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.
    Type: Grant
    Filed: May 18, 2009
    Date of Patent: March 18, 2014
    Assignees: Merck Canada Inc., Merck Sharp & Dohme Corp.
    Inventors: Louis-Charles Campeau, John Y. Chung, Danny Gauvreau, Melina Girardin-Rondeau, Gregory Hughes, Kevin M. Maloney, Christophe Mellon, Jeffrey C. Moore, Paul O'Shea, Stephane Ouellet
  • Patent number: 8673920
    Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
    Type: Grant
    Filed: April 27, 2010
    Date of Patent: March 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Alexander Pasternak, Aurash Shahripour, Haifeng Tang, Nardos H. Teumelsan, Lihu Yang, Yuping Zhu, Shawn P. Walsh
  • Patent number: 8673900
    Abstract: In many embodiments, the present invention provides novel heterocyclic compounds which are modulators of gamma secretase, 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 disease associated with the central nervous system using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: November 12, 2009
    Date of Patent: March 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhaoning Zhu, William J. Greenlee, Xianhai Huang, Jun Qin, Xiaoxiang Liu, Hongmei Li, Wei Zhou, Anandan Palani, Xiaohong Zhu, Monica L. Vicarel, Mihirbaran Mandal, Zhong-Yue Sun, Chad E. Bennett, Troy Michael McCracken, Gioconda V. Gallo
  • Patent number: 8673941
    Abstract: The present invention is directed to certain oxazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.
    Type: Grant
    Filed: July 30, 2009
    Date of Patent: March 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Harry Chobanian, Linus S. Lin, Ping Liu, Marc D. Chioda, Robert J. DeVita, Ravi P. Nargund, Yan Guo
  • Patent number: 8674105
    Abstract: The instant invention relates to crystalline forms of Compound A, an inhibitor of c-MET kinase. Specifically, the instant invention relates to hydrochloride salts of Compound A.
    Type: Grant
    Filed: September 21, 2010
    Date of Patent: March 18, 2014
    Assignees: Merck Sharp & Dohme Limited, Merck Sharp & Dohme Corp.
    Inventors: Paolo Avalle, Minhua Chen
  • Patent number: 8669259
    Abstract: The present invention relates to heterocyclic amide derivatives of Formula (I): Formula (I) wherein the variables are as defined in the specification. The present invention further relates to compositions comprising said heterocyclic amide derivatives of formula (I) and methods for using said heterocyclic amide derivatives of formula (I) for treating or preventing a disease or disorder related to the activity of a protein kinase, in particular, a proliferative disease, an anti-proliferative disorder, inflammation, arthritis, a neurological or neurodegenerative disease, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease or a fungal infection.
    Type: Grant
    Filed: August 19, 2010
    Date of Patent: March 11, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Panduranga P. Adulla Reddy, M. Arshad Siddiqui, Tzu Tshin Wong
  • Patent number: 8669272
    Abstract: The present invention is directed to 2,5-disubstituted piperidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. 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 orexin receptors are involved.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: March 11, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, John D. Schreier, David B. Whitman
  • Patent number: 8669256
    Abstract: The invention relates to compounds according to general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of cancer.
    Type: Grant
    Filed: May 23, 2011
    Date of Patent: March 11, 2014
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Brigitte Johanna Bernita Folmer, de Adrianus Petrus Antonius Man, Elisabeth Sophia Gernette, Rita Corte Real Goncalves Azevedo, Hemen Ibrahim
  • Patent number: 8669252
    Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
    Type: Grant
    Filed: May 12, 2011
    Date of Patent: March 11, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dong-Ming Shen, John S. Debenham, Thomas H. Graham, Matthew J. Clements, Yong Zhang
  • Patent number: 8664387
    Abstract: The present invention is directed to quinolinone-pyrazolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: December 9, 2010
    Date of Patent: March 4, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Ronald K. Chang, Thomas J. Greshock
  • Patent number: 8664411
    Abstract: Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)—O—C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)—O—C(O)-heteroaryl and a basic tertiary amine.
    Type: Grant
    Filed: July 1, 2008
    Date of Patent: March 4, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Wen-Lian Wu, Thomas A. Bara, Duane A. Burnett, John W. Clader, Martin S. Domalski, Yan Jin, Hubert B. Josien, Hongmei Li, Xian Liang, Dmitri A. Pissarnitski, Thavalakulamgara K. Sasikumar, Jesse K. Wong, Ruo Xu, Zhiqiang Zhao, Paul McNamara