Abstract: The invention relates to compounds of formula (I): wherein X, W, Q, R, R1 and R2 have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.
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.
Abstract: The instant invention provides for tetracyclic compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
Abstract: In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, 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 conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.
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 16, 2010
Date of Patent:
May 27, 2014
Assignees:
Merck Sharp & Dohme Corp., Merck Canada Inc.
Inventors:
Michael D. Altman, Kenneth L. Arrington, Jason Burch, Bernard Cote, Jean-Francois Fournier, Jacques Yves Gauthier, Solomon Kattar, Sandra Lee Knowles, Jongwon Lim, Michelle R. Machacek, Alan B. Northrup, Michael H. Reutershan, Joel S. Robichaud, Adam J. Schell, Kerrie B. Spencer
Abstract: In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, 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 conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.
Abstract: The present invention relates to five-layered pigments based on multicoated platelet-shaped substrates which comprise a layer sequence comprising (A) a layer of SnO2 having a layer thickness of 0.1-50 nm, (B) a high-refractive-index coating consisting of TiO2 in the rutile modification having a layer thickness of 10-800 nm, (C) a colorless coating having a refractive index n?1.8 having a layer thickness of 20-800 nm, (D) a high-refractive-index coating consisting of SnO2 having a layer thickness of 0.1-50 nm, (E) a layer of TiO2 in the rutile modification having a layer thickness of 10-800 nm, and optionally (F) an outer protective layer, and to the use thereof in paints, coatings, powder coatings, printing inks, security printing inks, plastics, ceramic materials, glasses, as dopants for the laser marking of papers and plastics, in cosmetic formulations and for the preparation of pigment preparations and dry preparations.
Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
Type:
Application
Filed:
June 11, 2012
Publication date:
August 7, 2014
Applicant:
MERCK PATENT GMBH
Inventors:
Timo Heinrich, Nadia Brugger, Kristopher Josephson
Abstract: There are disclosed compounds of formula (I)
and pharmaceutically acceptable salts thereof which may be useful for the treatment of cytokine mediated diseases such as arthritis.
Type:
Grant
Filed:
December 20, 2000
Date of Patent:
July 27, 2004
Assignee:
Merck & Co., Inc
Inventors:
Christopher F. Claiborne, Nigel J. Liverton, David A. Claremon
Abstract: Disclosed are the use of compatible solutes for inhibiting the release of ceramides or for the prophylaxis and protection of human skin against premature skin aging and for the prophylaxis and protection of human skin against wrinkling.
Abstract: Thiophene-2-sulfonamides with an alkyl or substituted-alkyl and an alkyl-S(O).sub.n -substituent are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
Type:
Grant
Filed:
December 14, 1988
Date of Patent:
May 29, 1990
Assignee:
Merck & Co., Inc.
Inventors:
John J. Baldwin, Gerald S. Ponticello, Charles N. Habecker
Abstract: The present invention provides methods of treating MS using pyrimidine and pyridine compounds which are inhibitors of Bruton's tyrosine kinase (BTK).
Abstract: The invention provides novel cyclic amine azaheterocyclic carboxamide according to Formula (I), Formula (II) and Formula (III) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
Type:
Application
Filed:
July 28, 2011
Publication date:
August 22, 2013
Applicant:
MERCK PATENT GMBH
Inventors:
Bayard R. Huck, Xiaoling Chen, Constantin Neagu, Reinaldo Jones, Yufang Xiao, Igor Mochalkin
Abstract: N-Biarylmethylaminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
Type:
Grant
Filed:
August 25, 2003
Date of Patent:
January 16, 2007
Assignee:
Merck & Co., Inc.
Inventors:
Scott D. Kuduk, Michael R. Wood, Mark G. Bock
Abstract: The invention relates to a compound of a formula (I): or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders.
Type:
Grant
Filed:
July 14, 2006
Date of Patent:
August 12, 2008
Assignee:
Merck & Co., Inc.
Inventors:
Takeru Yamakawa, Hideki Jona, Kenji Niiyama, Koji Yamada, Tomoharu Iino, Mitsuru Ohkubo, Hideaki Imamura, Jun Shibata, Jun Kusunoki, Lihu Yang
Abstract: There are disclosed compounds of formula (I)
and pharmaceutically acceptable salts thereof which exhibit utility for the treatment of cytokine mediated diseases such as arthritis.
Type:
Grant
Filed:
June 12, 2000
Date of Patent:
June 11, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Nigel J. Liverton, David A. Claremon, John W. Butcher, Cory R. Theberge