Search Patents
  • METHODS OF PREPARING HYDROXYLAMINE DERIVATIVES USEFUL IN THE PREPARATION OF ANTI-INFECTIVE AGENTS
    Publication number: 20190055216
    Abstract: The present invention relates to processes for the preparation of N-protected 4-((2S,5R)-5-((benzyloxy)amino)piperidine-2-carboxamido)piperidine-1-carboxylates. Such compounds have application in the preparation of beta-lactamase inhibitors such as 7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamides and esters, in particular, the beta lactamase inhibitor, (2S,5R)-7-oxo-N-piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide. The present invention also encompasses intermediates useful in the disclosed processes and methods for their preparation.
    Type: Application
    Filed: January 30, 2017
    Publication date: February 21, 2019
    Applicants: MERCK SHARP & DOHME CORP., MERCK SHARP & DOHME LIMITED
    Inventors: Aaron M. Dumas, Jeremy P. Scott, Michael Shevlin, Zhijian Liu, John Y. L. Chung, Feng Yu, Dongfang Meng
  • Methods of preparing hydroxylamine derivatives useful in the preparation of anti-infective agents
    Patent number: 10472345
    Abstract: The present invention relates to processes for the preparation of N-protected 4-((2S,5R)-5-((benzyloxy)amino)piperidine-2-carboxamido)piperidine-1-carboxylates. Such compounds have application in the preparation of beta-lactamase inhibitors such as 7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamides and esters, in particular, the beta lactamase inhibitor, (2S,5R)-7-oxo-N-piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide. The present invention also encompasses intermediates useful in the disclosed processes and methods for their preparation.
    Type: Grant
    Filed: January 30, 2017
    Date of Patent: November 12, 2019
    Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Limited
    Inventors: Aaron M. Dumas, Jeremy P. Scott, Michael Shevlin, Zhijian Liu, John Y. L. Chung, Feng Xu, Dongfang Meng
  • Process for {3-[2()-[(1)-1-[3,5-bis(trifluoromethyl) phenyl]ethoxy]-3()-(4-fluorophenyl)morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid
    Patent number: 7807829
    Abstract: The present invention is concerned with a process for the preparation of the compound {3-[2(R)-[(1R)-1-[3,5-bis(tri-fluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)-morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid, and pharmaceutically acceptable salts thereof. This compound is useful as a substance P (neurokinin-1) receptor antagonist. In particular, the compound is useful e.g., in the treatment of emesis and inflammatory diseases.
    Type: Grant
    Filed: November 3, 2005
    Date of Patent: October 5, 2010
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Corp.
    Inventors: James Michael McNamara, Louis Matty, Jonathan D. Rosen
  • Pyrazolyl derivatives as Syk inhibitors
    Patent number: 9242984
    Abstract: The present invention provides novel pyrazole derivatives 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, rheumatoid arthritis, and cancer.
    Type: Grant
    Filed: June 18, 2013
    Date of Patent: January 26, 2016
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Michelle R. Machacek, Michael D. Altman, Eric T. Romeo, Dilrukshi Vitharana, Brandon Cash, Tony Siu, Hua Zhou, Matthew Christopher, Solomon D. Kattar, Andrew M. Haidle, Kaleen Konrad Childers, Matthew L. Maddess, Michael H. Reutershan, Yves Ducharme, David J. Guerin, Kerrie Spencer, Christian Beaulieu, Vouy Linh Truong, Daniel Guay, Alan B. Northrup, Brandon M. Taoka, Jongwon Lim, Christian Fischer, John W. Butcher, Ryan D. Otte, Binyuan Sun, John Michael Ellis
  • POLYMORPHIC FORMS OF 1-[4-(5-CYANOINDOL-3-YL)BUTYL]-4-(2-CARBAMOYLBENZOFURAN-5-YL)PIPERAZINE HYDROCHLORIDE
    Publication number: 20130102616
    Abstract: The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation.
    Type: Application
    Filed: October 23, 2012
    Publication date: April 25, 2013
    Applicant: Merck Patentgesellschaft
    Inventor: Merck Patentgesellschaft
  • SPIROCYCLIC COMPOUNDS
    Publication number: 20130131041
    Abstract: The present invention relates to a novel class of substituted spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Application
    Filed: December 19, 2012
    Publication date: May 23, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventor: Merck Sharp & Dohme Corp.
  • Substituted pyridine spleen tyrosine kinase (SYK) inhibitors
    Patent number: 9376418
    Abstract: The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
    Type: Grant
    Filed: June 17, 2013
    Date of Patent: June 28, 2016
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Andrew M. Haidle, Sandra Lee Knowles, Solomon D. Kattar, Denis Deschenes, Jason Burch, Joel Robichaud, Matthew Christopher, Michael D. Altman, James P. Jewell, Alan B. Northrup, Marc Blouin, John Michael Ellis, Hua Zhou, Christian Fischer, Adam J. Schell, Michael H. Reutershan, Brandon M. Taoka, Anthony Donofrio
  • THIAZOLE-SUBSTITUTED AMINOHETEROARYLS AS SPLEEN TYROSINE KINASE INHIBITORS
    Publication number: 20160060255
    Abstract: The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, and R4 are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
    Type: Application
    Filed: April 22, 2014
    Publication date: March 3, 2016
    Applicants: Merck Canada Inc., Merck Sharp & Dohme Corp.
    Inventors: Neville J. Anthony, Brian M. Andresen, Alan B. Northrup, Kaleen K. Childers, Anthony Donofrio, Thomas A. Miller, Yuan Liu, Michelle R. Machacek, Hyun Chong Woo, Kerrie B. Spencer, John Michael Ellis, Michael D. Altman, Eric T. Romeo, Daniel Guay, Jonathan Grimm, Marie-Eve Lebrun, Joel S. Robichaud, Liping Wang, Byron DuBois, Qiaolin Deng
  • Cyclohexyl derivatives and their use as therapeutic agents
    Patent number: 6953792
    Abstract: The present invention relates compounds of the formula (I): wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of: (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), (l) and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R?17, R18, R19, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.
    Type: Grant
    Filed: May 16, 2001
    Date of Patent: October 11, 2005
    Assignees: Merck Sharp & Dohme Limited, Merck & Co., Inc.
    Inventors: Jose Luis Castro Pineiro, Kevin Dinnell, Jason Matthew Elliot, Gregory John Hollingworth, Duncan Edward Shaw, Christopher John Swain, Lihu Yang
  • 5-(pyridin-3-yl)oxazole allosteric modulators of the M4 muscarinic acetylcholine receptor
    Patent number: 10981902
    Abstract: The present invention is directed to 5-(pyridine-3-yl)oxaxole compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
    Type: Grant
    Filed: June 22, 2018
    Date of Patent: April 20, 2021
    Assignees: Merck Sharp & Dohme Corp., Merck MSD (R&D) China Co., LTD.
    Inventors: Jianming Bao, Timothy J. Henderson, Chunsing Li, Michael Man-Chu Lo, Robert D. Mazzola, Jr., Meng Na, Michael T. Rudd, David M. Tellers, Ling Tong
  • Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
    Patent number: 9745295
    Abstract: The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, and R4 are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
    Type: Grant
    Filed: April 22, 2014
    Date of Patent: August 29, 2017
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Neville J. Anthony, Brian M. Andresen, Alan B. Northrup, Kaleen K. Childers, Anthony Donofrio, Thomas A. Miller, Yuan Liu, Michelle R. Machacek, Hyun Chong Woo, Kerrie B. Spencer, John Michael Ellis, Michael D. Altman, Eric T. Romeo, Daniel Guay, Jonathan Grimm, Marie-Eve Lebrun, Joel S. Robichaud, Liping Wang, Byron DuBois, Qiaolin Deng
  • BTK INHIBITORS
    Publication number: 20170008899
    Abstract: Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of 6-5 membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.
    Type: Application
    Filed: August 30, 2016
    Publication date: January 12, 2017
    Applicants: MERCK SHARP & DOHME CORP., MERCK SHARP & DOHME B.V.
    Inventors: ADRIANUS PETRUS ANTONIUS DE MAN, JAN-GERARD STERRENBURG, HANS C. A. RAAIJMAKERS, ALLARD KAPTEIN, ARTHUR A. OUBRIE, JOHANNES BERNARDUS MARI REWINKEL, CHRISTIAAN GERARDUS JOHANNES MARIA JANS, JACOBUS C.H.M. WIJKMANS, TJEERD A. BARF, ALAN B. COOPER, RONALD M. KIM, SOBHANA BABU BOGA, HUGH Y. ZHU, XIAOLEI GAO, XIN YAO, RAJAN ANAND, HAO WU, SHILAN LIU, CHUNDAO YANG, ABDUL-BASIT ALHASSAN, JAMES WANG, YOUNONG YU, JIAN LIU, HENRY M. VACCARO
  • HIV protease inhibitors
    Patent number: 9315475
    Abstract: The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset 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: September 9, 2013
    Date of Patent: April 19, 2016
    Assignees: MERCK SHARP & DOHME CORP., MERCK CANADA INC.
    Inventors: Christian Beaulieu, David J. Bennett, Christopher J. Bungard, Ronald K. Chang, Sheldon Crane, Thomas J. Greshock, Li Hao, Kate Holloway, Jesse J. Manikowski, John A. McCauley, Daniel McKay, Carmela Molinaro, Oscar Miguel Moradei, Philippe G. Nantermet, Christian Nadeau, Satyanarayana Tummanapalli, William Shipe, Sanjay Kumar Singh, Vouy Linh Truong, Sivalenka Vijayasaradhi, Peter D. Williams, Catherine M. Wiscount
  • HIV protease inhibitors
    Patent number: 9994587
    Abstract: The present invention is directed to 2,6-morpholine derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein Z1, Z2, V1, V2, V3, R6, R6A, and X are defined herein. The invention also relates to methods of using the 2,6-morpholine derivatives of the invention for the inhibition of HV protease, the inhibition of HV 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: March 2, 2015
    Date of Patent: June 12, 2018
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: John A. McCauley, David Jonathan Bennett, Christopher J. Bungard, Thomas J. Greshock, M. Katharine Holloway, Peter D. Williams, Christian Beaulieu, Sheldon Crane, Stephanie Lessard, Daniel Mckay, Carmela Molinaro, Oscar Miguel Moradei, Vijayasaradhi Sivalenka, Vouy Linh Truong, Satyanarayana Tummanapalli
  • HIV PROTEASE INHIBITORS
    Publication number: 20170217986
    Abstract: The present invention is directed to 2,6-morpholine derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein Z1, Z2, V1, V2, V3, R6, R6A, and X are defined herein. The invention also relates to methods of using the 2,6-morpholine derivatives of the invention for the inhibition of HV protease, the inhibition of HV 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: Application
    Filed: March 2, 2015
    Publication date: August 3, 2017
    Applicants: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: John A. McCauley, David Jonathan Bennett, Christopher J. Bungard, Thomas J. Greshock, M. Katharine Holloway, Peter D. Williams, Christian Beaulieu, Sheldon Crane, Stephanie Lessard, Daniel Mckay, Carmela Molinaro, Oscar Miguel Moradei, Vijayasaradhi Sivalenka, Vouy Linh Truong, Satyanarayana Tummanapalli
  • TETRAHYDRONAPHTHYRIDINE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE
    Publication number: 20170305902
    Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, L, X1, X2, and X3, are as defined herein. The compounds of the invention, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising them, are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a person in need thereof for diseases or disorders in which the mGluR2-NAM receptor plays a causative role, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders.
    Type: Application
    Filed: August 24, 2015
    Publication date: October 26, 2017
    Applicants: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Ashok Arasappan, Christopher James Bungard, Jessica L. Frie, Yongxin Han, Scott B. Hoyt, Peter J. Manley, Robert S. Meissner, James J. Perkins, Iyassu K. Sebhat, Robert R. Wilkening, Kenneth J. Leavitt
  • Aminopyrimidines as SYK inhibitors
    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
  • BTK Inhibitors
    Patent number: 9718828
    Abstract: Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of 6-5 membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.
    Type: Grant
    Filed: August 30, 2016
    Date of Patent: August 1, 2017
    Assignees: MERCK SHARP & DOHME CORP., MERCK SHARP & DOHME B.V.
    Inventors: Adrianus Petrus Antonius De Man, Jan-Gerard Sterrenburg, Hans C. A. Raaijmakers, Allard Kaptein, Arthur A. Oubrie, Johannes Bernardus Maria Rewinkel, Christiaan Gerardus Johannes Maria Jans, Jacobus C. H. M. Wijkmans, Tjeerd A. Barf, Alan B. Cooper, Ronald M. Kim, Sobhana Babu Boga, Hugh Y. Zhu, Xiaolei Gao, Xin Yao, Rajan Anand, Hao Wu, Shilan Liu, Chundao Yang, Abdul-Basit Alhassan, James Wang, Younong Yu, Jian Liu, Henry M. Vaccaro
  • Sulphonamido-substituted bridged bicycloalkyl derivatives
    Patent number: 7365196
    Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.
    Type: Grant
    Filed: March 15, 2001
    Date of Patent: April 29, 2008
    Assignees: Merck Sharp & Dohme Ltd., Merck Frosst Canada & Co.
    Inventors: Patrice Charles Belanger, Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Edward Giles McIver, Alan John Nadin, Joseph George Neduvelil, Mark Steven Shearman, Adrian Leonard Smith, Timothy Jason Sparey, Graeme Irvine Stevenson, Martin Richard Teall
  • SUBSTITUTED ARYL SULFONE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS
    Publication number: 20130040932
    Abstract: A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
    Type: Application
    Filed: September 24, 2012
    Publication date: February 14, 2013
    Applicants: Neuromed Pharmaceuticals Ltd., Merck Sharp & Dohme Corp.
    Inventors: Merck Sharp & Dohme Corp., Neuromed Pharmaceuticals Ltd.
Narrow Results

Filter by US Classification