Patents Assigned to Merck Sharp and Dohme
  • 2,5-disubstituted piperidine orexin receptor antagonists
    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
  • Prolylcarboxypeptidase inhibitors
    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
  • Heterocyclic amide compounds as protein kinase inhibitors
    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
  • Substituted thieno[2,3-b]pyrazine compounds as modulators of B-Raf kinase activity
    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
  • Dihydrobenzoquinazolinone M1 receptor positive allosteric modulators
    Patent number: 8664234
    Abstract: The present invention is directed to dihydrobenzoquinazilinone 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: September 29, 2011
    Date of Patent: March 4, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Ronald K. Chang, Thomas J. Greshock
  • Imidazole derivatives useful as modulators of FAAH and as FAAH imaging agents
    Patent number: 8664253
    Abstract: The present invention is directed to certain Inidazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. 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, Alzeimer Disease, and Parkinson's Disease.
    Type: Grant
    Filed: February 22, 2010
    Date of Patent: March 4, 2014
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Ping Liu, Robert J. DeVita, Linus S. Lin, Marc D. Chioda, Terence G. Hamill, Wenping Li
  • Tetrahydropyranochromene gamma secretase inhibitors
    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
  • Pyridoquinazolinone M1 receptor positive allosteric modulators
    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
  • DRUG DELIVERY SYSTEM
    Publication number: 20140056962
    Abstract: The subject invention provides a drug delivery system comprising at least one compartment comprising (i) a drug-loaded thermoplastic polymer core layer, (ii) a drug-loaded thermoplastic polymer intermediate layer and (iii) a non-medicated thermoplastic polymer skin covering the intermediate layer, wherein said core layer is loaded with crystals of a first (pharmaceutically) active compound and said intermediate layer is loaded with crystals of the second (pharmaceutically) active compound.
    Type: Application
    Filed: October 31, 2013
    Publication date: February 27, 2014
    Applicant: Merck Sharp & Dohme B.V.
    Inventors: Wouter de Graaff, Raymond Zeeman
  • SUBSTITUTED CYCLOPROPLY COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
    Publication number: 20140057893
    Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119.
    Type: Application
    Filed: April 5, 2012
    Publication date: February 27, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Scott Edmondson, Zhiqiang Guo, Harold B. Wood, Andrew W. Stamford, Michael W. Miller, Duane E. DeMong, Gregori J. Morriello, Rajan Anand, Vincent J. Colandrea, Megan Macala, Milana Maletic, Cheng Zhu, Yuping Zhu, Wanying Sun, Kake Zhao, Yong Huang, Joel M. Harris, Lehua Chang, Nam Fung Kar, Zhiyong Hu, Liping Wang, Bowei Wang, Ping Liu, Jason W. Szewczyk, William B. Geiss
  • Compounds that are ERK inhibitors
    Patent number: 8658651
    Abstract: Disclosed are the ERK inhibitors of formula 1.0: (Formula (A1)), and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine ring that can have a bridge or a fused ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula A1.
    Type: Grant
    Filed: September 20, 2010
    Date of Patent: February 25, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Hugh Y. Zhu, Jagdish A. Desai, Alan B. Cooper, Ronald J. Doll
  • 8-methyl-1-phenyl-imidazol[1,5-a]pyrazine compounds as Lck inhibitors and uses thereof
    Patent number: 8658794
    Abstract: The present invention provides 8-methyl-1-phenyl-imidazo[1,5-a]pyrazine derivatives according to formula I or pharmaceutically acceptable salts thereof. The compounds of the current invention show inhibitory activity against Lck and can be used for the treatment of Lck-mediated diseases or Lck-mediated conditions such as inflammatory disorders.
    Type: Grant
    Filed: February 3, 2011
    Date of Patent: February 25, 2014
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Adrianus Petrus Antonius de Man, Johannes Bernardus Maria Rewinkel, Christiaan Gerardus Johannes Maria Jans, Hans Cornelis Andreas Raaijmakers, Jacobus Cornelis Henricus Maria Wijkmans
  • Injectable formulations containing asenapine and method of treatment using same
    Patent number: 8658687
    Abstract: The present invention provides a formulation comprising asenapine hemipamoate suspended particles, which formulation can be administered via a Depot provided by an IM injection of the formulation, and which depot does not display a particle-size dependent release rate. The present invention provides also methods of treatment using the same.
    Type: Grant
    Filed: June 24, 2010
    Date of Patent: February 25, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Werenfridus Adrianus Faassen, Gerardus Johannes Huissen Kemperman, Johannes Antonius Hendrikus van Laarhoven
  • AMINOTETRAHYDROPYRANS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
    Publication number: 20140051740
    Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.
    Type: Application
    Filed: October 22, 2013
    Publication date: February 20, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Tesfaye Biftu, Ann E. Weber
  • Pyrazolo [4,3-C] cinnolin-3-one M1 receptor positive allosteric modulators
    Patent number: 8653079
    Abstract: The present invention is directed to pyrazolo[4,3-c]cinnolin-3-one 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 11, 2012
    Date of Patent: February 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Douglas C. Beshore, Scott D. Kuduk
  • Hydroxymethyl pyrrolidines as beta 3 adrenergic receptor agonists
    Patent number: 8653260
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Grant
    Filed: June 20, 2012
    Date of Patent: February 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Ding-Ming Shen, Liping Wang, Cheng Zhu
  • Heterocyclic compounds as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
    Patent number: 8653059
    Abstract: The present invention is directed to substituted six-membered heterocyclic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as obesity and diabetes, particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: August 18, 2008
    Date of Patent: February 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tesfaye Biftu, Danqing Feng, Ann E. Weber, Jason M. Cox, Xiaoxia Qian, Jinyou Xu
  • ANTIDIABETIC TRICYCLIC COMPOUNDS
    Publication number: 20140045746
    Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
    Type: Application
    Filed: July 31, 2013
    Publication date: February 13, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: William K. Hagmann, Ravi P. Nargund, Timothy A. Blizzard, Hubert Josien, Purakkattle Biju, Christopher W. Plummer, Qun Dang, Bing Li, Linus S. Lin, Mingxiang Cui, Bin Hu, Jinglai Hao, Zhengxia Chen
  • Insulin-Like Growth Factor-1 Receptor Inhibitors
    Publication number: 20140045832
    Abstract: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating Insulin-Like-Growth Factor I Receptor and Insulin Receptor. The compounds of the instant invention possess a core structure that comprises a sulfonyl indole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
    Type: Application
    Filed: April 19, 2012
    Publication date: February 13, 2014
    Applicants: PIRAMAL ENTERPRISES LIMITED, MERCK SHARP & DOHME CORP.
    Inventors: Sarala Balachandran, Christopher J. Dinsmore, Abhijit Roychowdhury, Rajiv Sharma, Ram Asrey Vishwakarma
  • SUBSTITUTED 1,3-BENZOTHIAZOL-2(3H)-ONES AND [1,3]THIAZOLO[5,4-B]PYRIDIN-2(1H)-ONES AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2
    Publication number: 20140045829
    Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate 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 metabotropic glutamate receptors are involved.
    Type: Application
    Filed: October 8, 2013
    Publication date: February 13, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: MARK E. LAYTON, Michael J. Kelly