Search Patents
  • Benzimidazole and aza-benzimidazole carboxamides
    Patent number: 8470819
    Abstract: This invention provides compounds of Formula I which are PAFR antagonists: I and the pharmaceutically acceptable salts thereof. The compounds are useful for treating PAF-mediated disorders, and can be used in methods for treating atherosclerosis and preventing or reducing risk for atherosclerotic disease events. The compounds are also useful for treating or ameliorating pain, e.g. inflammatory pain and/or nociceptive pain, and for treating or ameliorating autoimmune and/or inflammatory diseases, among other conditions.
    Type: Grant
    Filed: October 26, 2009
    Date of Patent: June 25, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Lin Chu, Anthony Ogawa, Hyun O. Ok, Feroze Ujjainwalla
  • Hydroxymethyl pyrrolidines as beta 3 adrenergic receptor agonists
    Patent number: 8501786
    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: March 23, 2009
    Date of Patent: August 6, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Bart Harper, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Harvey Wendt, Cheng Zhu
  • SUBSTITUTED 6-MEMBERED ARYL OR HETEROARYL ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
    Publication number: 20210077511
    Abstract: present disclosure relates to compounds of formula (I) that are useful as modulators of ?7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation.
    Type: Application
    Filed: October 30, 2017
    Publication date: March 18, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: BRENDAN M. CROWLEY, IAN M. BELL, ANDREW JOHN HARVEY, BRIAN T. CAMPBELL, THOMAS J. GRESHOCK, VANESSA L. RADA
  • Conjugates useful in the treatment of prostate cancer
    Patent number: 6174858
    Abstract: Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA) and known cytotoxic agents are disclosed. The conjugates of the invention are characterized by attachment of the cleavable oligopeptide to the oxygen atom at the 4-position on a vinca drug that has be desacetylated. Such conjugates are useful in the treatment of prostatic cancer and benign prostatic hypertrophy (BPH).
    Type: Grant
    Filed: November 17, 1998
    Date of Patent: January 16, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Stephen F. Brady, Dong-Mei Feng, Victor M. Garsky
  • Mesogenic Compounds, Liquid Crystal Medium and Liquid Crystal Display
    Publication number: 20080116419
    Abstract: The instant invention relates to mesogenic media comprising one or more compounds which comprise two or more mesogenic groups two of which are linked to the ortho-positions of an aromatic ring, preferably of formula (I) wherein the parameters are as specified in the text, preferably the instant invention relates to mesogenic media showing a blue phase and their use in electro-optical light modulation elements and their respective use in displays, as well as to such devices. The instant invention further relates to compounds of formula (I).
    Type: Application
    Filed: December 22, 2005
    Publication date: May 22, 2008
    Applicant: MERCK PATENT GMBH
    Inventors: Peer Kirsch, Gerald Unger, Andreas Ruhl, Michael Heckmeier, Peter Best, John Patrick
  • INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
    Publication number: 20140031349
    Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
    Type: Application
    Filed: July 25, 2013
    Publication date: January 30, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Fa-Xiang Ding, Shuzhi Dong, Jessica Frie, Xin Gu, Jinlong Jiang, Alexander Pasternak, Haifeng Tang, Zhicai Wu, Yang Yu, Takao Suzuki
  • Electroluminescence Device
    Publication number: 20160181537
    Abstract: The present application relates to an electroluminescence device containing a) an anode, b) a cathode, c) at least one emitter layer containing at least one electroluminescent material and arranged between the anode and the cathode, and d) at least one electron transport layer containing at least one material having electron-conducting or predominantly electron-conducting properties and arranged between the at least one emitter layer and the cathode, said device being characterized in that the at least one emitter layer contains a polymer having hole-conducting or predominantly hole-conducting properties. The electroluminescence device according to the invention is distinguished by a high lifetime and a high radiation efficiency.
    Type: Application
    Filed: July 1, 2014
    Publication date: June 23, 2016
    Applicant: Merck Patent GmbH
    Inventors: Junyou Pan, Frank Egon Meyer
  • IMIDAZO-PYRAZINYL DERIVATIVES USEFUL AS SOLUBLE GUANYLATE CYCLASE ACTIVATORS
    Publication number: 20180147208
    Abstract: A compound of Formula I or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or pharmaceutically acceptable salt thereofs, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of Formula I or pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: May 23, 2016
    Publication date: May 31, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Joie GARFUNKLE, Olga ORNOSKI, Dann L. PARKER, JR., Subharekha RAGHAVAN, Libo XU
  • Substituted pyrazolo[1,5-a]pyrido[3.2-e]pyrimidin-6-one inhibitors of mammalian target of rapamycin
    Patent number: 8703784
    Abstract: This invention relates to novel fused tricyclic compounds under Formula I that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example cancer and other proliferative disorders.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: April 22, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhaoyang Meng, Panduranga Adulla P. Reddy, M. Arshad Siddiqui, Amit K. Mandal, Duan Liu, Lianyun Zhao, Andrew McRiner
  • Interleukin-12p40 variants with improved stability
    Patent number: 7872107
    Abstract: Modified interleukin-12 (IL-12) p40 polypeptides are disclosed. The modified polypeptides have alterations in the IL-12p40 subunit to eliminate the protease site between positions Lys260 and Arg261. The modified IL-12p40 polypeptides according to the invention have improved stability compared to wild-type mature human IL-12p40 polypeptides.
    Type: Grant
    Filed: December 29, 2006
    Date of Patent: January 18, 2011
    Assignee: Merck Patent GmbH
    Inventors: Gordon D. Webster, Suzanne P. McKenzie, Kin-Ming Lo, Pascal André Stein
  • Inhibitors of the Renal Outer Medullary Potassium Channel
    Publication number: 20160207922
    Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
    Type: Application
    Filed: July 28, 2014
    Publication date: July 21, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Haifeng Tang, Barbara Pio, Jinlong Jiang, Alexander Pasternak, Shuzhi Dong, Ronald Dale Ferguson, II, Zack Zhiqiang Guo, Harry Chobanian, Jessica Frie, Yan Guo, Zhicai Wu, Yang Yu, Ming Wang
  • Process for the preparation of D-(+)-biotin
    Patent number: 4732987
    Abstract: D-(+)-Biotin can be prepared from optically active hydantoins of the formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, X and Y have the meaning given in patent claim 1, in a simple, stereospecific manner.Furthermore bicyclic nitriles of the formula XI ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, X and Y have the meaning given represent precious intermediate products and educts of a multitude of possibilities to synthesize optically active D-(+)-biotin.
    Type: Grant
    Filed: April 17, 1987
    Date of Patent: March 22, 1988
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Eike Poetsch, Michael Casutt
  • Oxadiazole and its salts, their use in treating dementia
    Patent number: 5106853
    Abstract: The compound (3R, 4R)-3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-1-azabicyclo[2.2.1]heptane and its salts behave as a functionally selective muscarinic agonist and are useful in the treatment of neurological and mental disorders, preferably in a pharmaceutical formulation comprising the active compound in association with a pharmaceutically acceptable carrier. The compound can be prepared by methods analogous to those known in the art via suitable chiral intermediates and cyclopropyl carboxamide oxime.
    Type: Grant
    Filed: May 9, 1990
    Date of Patent: April 21, 1992
    Assignee: Merck Sharp & Dohme, Ltd.
    Inventors: Graham A. Showell, Leslie J. Street
  • Cyclic amidines useful as NMDA NR2B antagonists
    Patent number: 6376530
    Abstract: The invention encompasses novel compounds of Formula I as well as a method of treating NMDA mediated diseases comprising administration to a patient in need of such treatment a non-toxic amount of a compound of Formula I effective to block the NMDA NR2B receptor sub-unit. The invention also encompasses certain pharmaceutical compositions for the treatment of NMDA mediated diseases comprising compounds of Formula I and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: April 17, 2000
    Date of Patent: April 23, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Christopher F. Claiborne, Nigel J. Liverton, David A. Claremon
  • 5-Methanesulfonamido-3H-isobenzofuran-1-ones as inhibitors of cyclooxygenase-2
    Patent number: 5968958
    Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: June 19, 1997
    Date of Patent: October 19, 1999
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Daniel Guay, Chun-Sing Li, Nathalie Ouimet
  • POLYMERISABLE LIQUID CRYSTAL MATERIAL AND POLYMERISED LIQUID CRYSTAL FILM
    Publication number: 20200291299
    Abstract: The invention relates to a polymerisable LC material comprising at least one monoreactive mesogenic compound, at least one di- or multireactive mesogenic compound and pentaerythritol tetrakis(3,5-di-tert-butyl-4-hydroxyhydrocinnamate). Furthermore, the present invention relates also to a method for its preparation, a polymer film with improved thermal durability obtainable from the corresponding polymerisable LC material, to a method of preparation of such polymer film, and to the use of such polymer film and said polymerisable LC material for optical, electro-optical, decorative or security devices.
    Type: Application
    Filed: February 7, 2017
    Publication date: September 17, 2020
    Applicant: MERCK PATENT GMBH
    Inventors: Stephen MULCAHY, lain GARDINER, Jack BRADFORD
  • Yellow nacreous pigments having calcined CR oxide and phosphate layer for improved light-fastness, process and use
    Patent number: 4456486
    Abstract: Nacreous pigments having a yellow powder color and an improved light-fastness comprise a mica platelet coated with titanium dioxide and on the titanium dioxide layer, a thin layer of calcined chromium oxide and/or chromium phosphate as a protective layer. The pigments are produced by coating mica platelets coated with metal oxides and/or hydroxides, with a thin layer of a sparingly soluble chromium(III) compound and calcining at about 500.degree.-1000.degree. C.
    Type: Grant
    Filed: September 22, 1982
    Date of Patent: June 26, 1984
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventor: Horst Bernhard
  • BCMA polypeptides and uses thereof
    Patent number: 7947805
    Abstract: The present invention relates to BCMA polypeptide variants and their uses, particularly for therapeutic or prophylactic treatment in human subjects. The invention also relates to nucleic acids encoding said polypeptides, vectors comprising such nucleic acids and recombinant cells containing the same. The invention further discloses methods of producing such polypeptides, as well as methods and tools for detecting or dosing these polypeptides in any sample.
    Type: Grant
    Filed: December 22, 2005
    Date of Patent: May 24, 2011
    Assignee: Merck Serono S.A.
    Inventors: Benedicte Belloir, Anne-Francoise Cledat, Gwenael Primas
  • MODIFIED IMIDAZOPYRIDINES AS GLUCOSYLCERAMIDE SYNTHASE INHIBITORS
    Publication number: 20240018140
    Abstract: The present invention relates to Compounds of Formula I: I and pharmaceutically acceptable salts or prodrug thereof. The present invention also relates to compositions comprising at least one compound of Formula I, and methods of using the compounds of Formula I for treatment or prophylaxis of lysosomal storage diseases, neurodegenerative disease, cystic disease, cancer, or a diseases or disorders associated with elevated levels of glucosylceramide (GlcCer), glucosylsphingosine (GlcSph) and/or other glucosylceramide-based glycosphingolipids (GSLs).
    Type: Application
    Filed: September 15, 2021
    Publication date: January 18, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Melissa C. Ford, Mark E. Fraley, Kristen L.G. Jones, H. Marie Loughran, James J. Mulhearn, Anthony J. Roecker, Kathy M. Schirripa, Ling Tong
  • Paraherquamide and dihydroparaherquamide as antihelminthic agents
    Patent number: 5075307
    Abstract: Paraherquamide and dihydroparaherquamide, known compounds, are disclosed as having antiparasitic activity. The compounds are fungal metabolites isolated from the known fungus Penicillium paraherquei, and from a newly isolated strain of Penicillium charlesii. Compositions including paraherquamide and dihydroparaherquamide as the active ingredient thereof for antiparasitic uses against endo and ecto parasites are also disclosed, as well as processes for the preparation of paraherquamide from the newly isolated fungus.
    Type: Grant
    Filed: July 28, 1987
    Date of Patent: December 24, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Maria T. D. Matas, Dan A. Ostlind, Luis Punsola, Sagrario Moohales del Val
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