Search Patents
  • 9-(piperazinylalkyl) carbazoles as bax-modulators
    Patent number: 8053436
    Abstract: The present invention is related to piperazine derivatives of carbazole of formula (I) notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such piperazine derivatives of carbazole. Said piperazine derivatives of carbazole are efficient modulators, in particular efficient inhibitors, of the Bax function and/or activation. The present invention is furthermore related to novel piperazine derivatives of carbazole as well as methods of their preparation.
    Type: Grant
    Filed: October 18, 2000
    Date of Patent: November 8, 2011
    Assignee: Merck Serono SA
    Inventors: Serge Halazy, Dennis Church, Bruno Antonsson, Agnes Bombrun, Patrick Gerber, Jean-Claude Martinou
  • PNEUMOCOCCAL POLYSACCHARIDES AND THEIR USE IN IMMUNOGENIC POLYSACCHARIDE-CARRIER PROTEIN CONJUGATES
    Publication number: 20230075760
    Abstract: The present invention provides capsular polysaccharides from Streptococcus pneumoniae serotypes identified using NMR. The present invention further provides polysaccharide-protein conjugates in which capsular polysaccharides from one or more of these serotypes are conjugated to a carrier protein such as CRM197. Polysaccharide-protein conjugates from one or more of these serotypes may be included in multivalent pneumococcal conjugate vaccines having polysaccharides from multiple additional Streptococcus pneumoniae serotypes.
    Type: Application
    Filed: September 22, 2022
    Publication date: March 9, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Richard J. Porambo, Chitrananda Abeygunawardana, Luwy Kavuka Musey, Michael J. Kosinski, Yadong Adam Cui, Julie Marie Skinner
  • Functionally selective alpha2C adrenoreceptor agonists
    Patent number: 8383818
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic derivatives as a2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the a2C adrenergic receptors using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: February 19, 2009
    Date of Patent: February 26, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Junying Zheng, Jianhua Chao, Kevin D. McCormick, Robert G. Aslanian, Mwangi W. Mutahi, Christopher W. Boyce, Walter S. Won
  • Tamperproof container
    Patent number: 4211333
    Abstract: An improved tamperproof container for lyophilized material wherein the container comprises a vial having flange about its opening. Below the flange, but spaced apart therefrom is a shoulder to define an indented neck therebetween. The opening is sealed with a pierceable stopper. An overcap extends over the flange and about the neck to form a skirt about the neck. The skirt has at least a portion thereof extending inwardly in gripping relation with the neck and limited in removal by contact with the underside of the flange whereby the cap cannot be removed without destroying its structural integrity.
    Type: Grant
    Filed: June 5, 1978
    Date of Patent: July 8, 1980
    Assignee: Merck & Co., Inc.
    Inventor: Miguel Villarejos
  • P38 kinase inhibiting agents
    Patent number: 8513289
    Abstract: Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: Formula (I); are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, COPD, ARDS, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.
    Type: Grant
    Filed: April 26, 2010
    Date of Patent: August 20, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Hiroo Koyama, Soumya P. Sahoo, Ginger Xu-Qiang Yang, Daniel J. Miller
  • CHROMANE AMIDINE MONOBACTAM COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS
    Publication number: 20230159517
    Abstract: The present invention relates to monobactam compounds of Formula I: and pharmaceutically acceptable salts thereof. The present invention also relates to compositions which comprise a monobactam compound of structural formula I or a pharmaceutically acceptable salt therof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of structural formula I, either alone or in combination with a therapeutically effective amount of a second beta-lactam antibiotic.
    Type: Application
    Filed: November 16, 2022
    Publication date: May 25, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Helen Y. Chen, Shuzhi Dong, Zhiyong Hu, Jing Su, Tao Yu, Yong Zhang
  • Substituted pyrido[3,4-d]pyrimidines and pyrido[4,3-d]pyrimidines as p70S6K inhibitors
    Patent number: 10233160
    Abstract: Novel azaquinazoline carboxamide derivatives of formula (I) wherein W1, W2, W3, W4, R1, R2, R3 and m which are defined above, are p70S6K inhibitor, and can be employed, inter alia, for the treatment of hyperproliferative disorders.
    Type: Grant
    Filed: April 24, 2018
    Date of Patent: March 19, 2019
    Assignee: Merck Patent GmbH
    Inventors: Bayard R. Huck, Ruoxi Lan, Justin Potnick, Lizbeth Celeste DeSelm, Mark W. Cronin, Jr., Constantin Neagu, Xiaoling Chen, Roch Boivin, Theresa L. Johnson, Andreas Goutopoulos
  • PIGMENT MIXTURE
    Publication number: 20170290750
    Abstract: The present invention relates to a pigment mixture based on at least two components A and B, where component A is a mixture of flake-form and spherical substrates which is covered with one or more inorganic layers and/or organic layers, and component B comprises crystalline or amorphous particles selected from the group of the metal oxides, metal hydroxides, metal oxyhalides, Prussian Blue or mixtures thereof, and to the use thereof in paints, coatings, printing inks, security printing inks, plastics, ceramic materials, glasses, in cosmetic formulations, as tracer, as filler and for the preparation of pigment preparations and dry preparations.
    Type: Application
    Filed: April 11, 2017
    Publication date: October 12, 2017
    Applicant: MERCK PATENT GMBH
    Inventors: Lukas HAMM, Nicole HAFERKORN, Marita JEKEL
  • Pharmaceutical formulations of cyclic urea type compounds
    Patent number: 5559110
    Abstract: Compositions comprising a cyclic urea type compound in a liquid or solid vehicle comprising a fatty acid ester of glycerol, or a fatty acid ester of polyethylene glycol, or a mixture thereof, wherein said vehicle has an hydrophil-lipophil balance of at least about 10, and, optionally, other excipients are described. The compositions are useful for providing good systemic absorption of the cyclic urea compounds when administered enterally, especially orally. The subject compounds and compositions are useful for treating viral infections, particularly HIV infection, in a mammal.
    Type: Grant
    Filed: March 9, 1994
    Date of Patent: September 24, 1996
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventor: Bruce J. Aungst
  • 9-Thia-, 9-oxothia-, and 9-dioxothia-11,12-seco-prostaglandins and processes
    Patent number: 4085125
    Abstract: This invention relates to 9-thia-, 9-oxothia-, and 9-dioxothia-11,12-seco-prostaglandins and processes for their manufacture. These compounds have prostaglandin-like biological activity and are particularly useful for the treatment of skin diseases such as psoriasis, for the prevention of thrombus formation, in stimulating the production of growth hormone in intact animals, and as regulators of the immune response.
    Type: Grant
    Filed: November 22, 1976
    Date of Patent: April 18, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., John B. Bicking, Robert L. Smith
  • Cathepsin cysteine protease inhibitors
    Patent number: 7375134
    Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
    Type: Grant
    Filed: February 28, 2003
    Date of Patent: May 20, 2008
    Assignees: Axys Pharmaceuticals, Inc., Merck Frosst Canada & Co.
    Inventors: Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Christophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien
  • HYDROXYALKYLAMINE- and HYDROXYCYCLOALKYLAMINE-SUBSTITUTED DIAMINE-ARYLSULFONAMIDE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATED SODIUM CHANNELS
    Publication number: 20170174674
    Abstract: Disclosed are compounds of Formula A, or a salt thereof: wherein R1, R2, and E are defined herein, which compounds have properties for inhibiting Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain disorders, cough, and itch using the same.
    Type: Application
    Filed: December 14, 2016
    Publication date: June 22, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Thomas J. Greshock, James Mulhearn, Junying Zheng, Ronald M. Kim, Ting Zhang, Anthony J. Roecker, Walter Won, Philippe Nantermet, Rajan Anand, Gang Zhou, Deping Wang, Liangqin Guo
  • FILTER HOUSING ASSEMBLY
    Publication number: 20200139284
    Abstract: A filter housing assembly includes a base plate, an adapter block, and a shroud. The base plate may be permanently installed in a fluid-conveying system of conduits. A filter member is secured to a filter-receiving formation such as a pipe nipple extending from the adapter block and the shroud is secured to the adapter block to cover and seal the filter member. The adapter block is releasably secured to the base plate. The arrangement facilitates insertion and removal of the filter housing assembly into and out of the fluid-conveying system of conduits by converting multiple junction points into a single junction point, at which a subassembly consisting of just the shroud and the adapter block are connected into the system.
    Type: Application
    Filed: November 5, 2018
    Publication date: May 7, 2020
    Applicant: Laboratories Merck Sharp & Dohme-Chibret
    Inventors: Bertrand Pessaud, Michael Meyer
  • Indazole derivatives useful as inhibitors of diacylglyceride O-acyltransferase 2
    Patent number: 11104690
    Abstract: The present invention relates to a compound represented by formula I?: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.
    Type: Grant
    Filed: November 13, 2017
    Date of Patent: August 31, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dong-Ming Shen, Thomas H. Graham, Wensheng Liu, Clare Tudge, Andreas Verras, Jinlong Jiang
  • Method for enhancing the lowering of plasma-cholesterol levels
    Patent number: 5376383
    Abstract: The instant invention is directed to a method for enhancing the lowering of plasma cholesterol level in a subject in need thereof which comprises the time-controlled administration of a nontoxic therapeutically effective amount of an HMG-CoA reductase inhibitor to said subject which surprisingly affords an equivalent or improved reduction of plasma cholesterol levels while significantly reducing the amount of HMG-CoA reductase inhibitor circulating in the bloodstream of the subject as compared to the same parameters when the oral administration of a conventional rapid release dosage form is utilized.
    Type: Grant
    Filed: February 1, 1993
    Date of Patent: December 27, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Alfred W. Alberts, Edward M. Scolnick, Arnold J. Repta
  • DNA sequence, and recombinant preparation of the grass pollen allergen Lol p4
    Patent number: 8945530
    Abstract: The present invention relates to the provision of a DNA sequence of the major grass pollen allergen Lol p 4. The invention also encompasses fragments, new combinations of partial sequences and point mutants having a hypoallergenic action. The recombinant DNA molecules and the derived polypeptides, fragments, new combinations of partial sequences and variants can be utilised for the therapy of pollen-allergic diseases. The proteins prepared by recombinant methods can be employed for in vitro and in vivo diagnosis of pollen allergies.
    Type: Grant
    Filed: December 6, 2010
    Date of Patent: February 3, 2015
    Assignee: Merck Patent GmbH
    Inventors: Andreas Nandy, Helmut Fiebig, Oliver Cromwell
  • EP4 Receptor Agonist, Compositions and Methods Thereof
    Publication number: 20110237511
    Abstract: This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.
    Type: Application
    Filed: June 3, 2011
    Publication date: September 29, 2011
    Applicant: Merck Frosst Canada
    Inventors: Xavier Billot, John Colucci, Yongxin Han, Marie-Claire Wilson, Robert N. Young
  • Isoquinoline derivatives useful as inhibitors of diacylglyceride O-acyltransferase 2
    Patent number: 9828369
    Abstract: The present invention relates to a compound represented by formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cardio-renal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.
    Type: Grant
    Filed: August 31, 2015
    Date of Patent: November 28, 2017
    Assignee: Merck Sharpe & Dohme Corp.
    Inventors: Jason Imbriglio, Clare London, Zhijian Lu, James Tata, Yusheng Xiong, Ming You, Hyewon Youm
  • Contamination-resistant dispensing and metering device
    Patent number: 5265770
    Abstract: A cap for dispensing liquids from a container comprising a base portion; structure to attach the base portion to a container; and an off-center dispenser tip projecting from the base portion and having a passageway extending between an orifice at the distal end of the dispenser tip and the interior underside of the cap, the axis of said passageway forming an angle of no greater than 90 with the longitudinal axis of the base. Included is a composite membrane having liquophilic and liquophobic components for preventing fluid contamination and metering dispersing.
    Type: Grant
    Filed: May 11, 1992
    Date of Patent: November 30, 1993
    Assignees: Pall Corporation, Merck and Company
    Inventors: Vlado I. Matkovich, Thomas J. Bormann
  • Rotor device for peristaltic pump
    Patent number: 11022108
    Abstract: A rotor device for a peristaltic pump containing a housing, a supporting shaft extending in an axial direction and being mounted in the housing, a rotor which contains a rotor-body mounted on the supporting shaft and extending in a radial direction from the supporting shaft and a plurality of rollers, mounted on the radially outer portion of the rotor-body and a driving device connected to the supporting shaft for driving the rotor, in which the peristaltic pump further contains a number of roller-markers corresponding to the number of rollers, in which the roller-markers indicate a dead zone, the roller-markers are provided directly or indirectly on the supporting shaft.
    Type: Grant
    Filed: June 25, 2015
    Date of Patent: June 1, 2021
    Assignee: Merck Patent GmbH
    Inventors: Raoul Weil, Emmanuelle Simon, Christophe Di-Palo, Vincent Schaal
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