Abstract: The present invention is directed to [1,2,4]triazolo[4,3-a]pyridine and [1,2,4]triazolo[4,3-a]pyrazine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.
Type:
Grant
Filed:
July 9, 2015
Date of Patent:
September 12, 2017
Assignee:
Incyte Corporation
Inventors:
Liangxing Wu, Xiaozhao Wang, Wenqing Yao, Colin Zhang
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:
Grant
Filed:
July 28, 2014
Date of Patent:
September 5, 2017
Assignee:
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
Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.
Type:
Grant
Filed:
October 8, 2015
Date of Patent:
September 5, 2017
Assignee:
CHEMOCENTRYX, INC.
Inventors:
Xi Chen, Dean R. Dragoli, Pingchen Fan, Juan C. Jaen, Yandong Li, Jay P. Powers, Viengkham Malathong, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang
Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, wherein R1, R2 and R3, are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
Type:
Grant
Filed:
October 14, 2015
Date of Patent:
August 29, 2017
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Keith R. Hornberger, Kenneth Michael Meyers, Peter Allen Nemoto, Simon Surprenant, Hui Yu
Abstract: Described herein are nucleic acid prodrugs and nucleic acid prodrugs comprising chiral phosphorous moieties. Also described herein are methods of making and using nucleic acid prodrugs and nucleic acid prodrugs comprising chiral phosphorous moieties.
Type:
Grant
Filed:
July 6, 2010
Date of Patent:
August 29, 2017
Assignee:
WAVE LIFE SCIENCES LTD.
Inventors:
Gregory L. Verdine, Meena ., Naoki Iwamoto
Abstract: The present invention relates to a method of reducing cutaneous facial flushing caused by systemic use of phosphodiesterase type 5 (PDE5) inhibitors by topical facial dermatological application of an effective dose of a composition comprising at least one alpha adrenergic receptor agonist.
Type:
Grant
Filed:
October 12, 2012
Date of Patent:
August 29, 2017
Assignee:
GALDERMA LABORATORIES, INC.
Inventors:
Warren J. Scherer, Arthur Clapp, Philippe Andres
Abstract: The present invention provides neuroprotective polyphenol compounds, which can be synthetic analogs of fisetin, baicalein or chlorogenic acid, that maintain neuroprotective, anti-inflammatory, glutathione promoting, and/or antioxidant properties. The neuroprotective polyphenol compounds are useful for promoting, enhancing and/or increasing neuron protection, growth and/or regeneration. The polyphenol compounds further find use for increasing and or maintaining intracellular glutathione (GSH) levels. The polyphenol compounds are also useful for treating, preventing, mitigating and/or delaying neurodegenerative conditions, including diabetes, Parkinson's disease, Huntington's disease, Alzheimer's disease, non-Alzheimer's dementias, multiple sclerosis, traumatic brain injury, spinal cord injury or ALS.
Type:
Grant
Filed:
February 26, 2016
Date of Patent:
August 29, 2017
Assignee:
Salk Institute for Biological Studies
Inventors:
David R. Schubert, Pamela A. Maher, Chandramouli Chiruta
Abstract: The present invention encompasses compounds of the formula (I), wherein the variables are defined herein which are suitable for the modulation of RORC and the treatment of diseases related to the modulation of RORC. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.
Type:
Grant
Filed:
July 28, 2014
Date of Patent:
August 29, 2017
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Brian Nicholas Cook, John D. Huber, Robert Owen Hughes, Xiang Li, Shuang Liang, Ingo Andreas Mugge, Michael Robert Turner, Qiang Zhang
Abstract: A ligand having the structure or its enantiomer; (I) wherein: each one of Ra, Rb, Rc and Rd is selected from alkyl, cycloalkyl, and aryl; the bridge group is selected from CH2NH; *CH(CH3)NH(C*,R); and the organocatalyst is an organic molecule catalyst covalently bound to the bridge group. Also, a catalyst having the structure or its enantiomer: (II) wherein: each one of Ra, Rb, Rc and Rd is selected from alkyl, cycloalkyl, and aryl; the bridge group is selected from CH2NH; *CH(CH3)NH(C*,R); and *CH(CH3)NH(C*,S); the organocatalyst is an organic molecule catalyst covalently bound to the bridge group; and M is selected from the group consisting of Rh, Pd, Cu, Ru, Ir, Ag, Au, Zn, Ni, Co, and Fe.
Type:
Grant
Filed:
March 11, 2014
Date of Patent:
August 29, 2017
Assignee:
RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
Abstract: A composition containing a malodor counteracting compound and a method for using the compound for counteracting a malodor in air space or a substrate is provided.
Type:
Grant
Filed:
September 25, 2014
Date of Patent:
August 22, 2017
Assignee:
INTERNATIONAL FLAVORS & FRAGRANCES INC.
Inventors:
Sean M. Wetterer, Drew T. Parkhurst, Richard Anthony Weiss, Anthony T. Levorse, Jr., Michael G. Monteleone, Richard M. Boden
Abstract: Trientine prodrugs, pharmaceutical compositions comprising the trientine prodrugs, and methods of using trientine prodrugs and pharmaceutical compositions thereof for treating Wilson's disease.
Abstract: The present invention relates to “a method for synthesizing 2,6-bis[3?-(N-carbazolyl)phenyl]pyridine compound”, and belongs to the field of chemical synthesis. In the present invention, a pyridine ring is formed by cyclization, the intermediate product can be directly used in the next reaction without purification and thus the process is very easy; the final product I will precipitate from the mixed reaction solution after the completion of the reaction, and the product can be very conveniently extracted.
Abstract: Disclosed is a process for purifying one or more chemical constituents from plant matter using extraction with a fluid that is not a solvent, for example, with a vegetable oil. The extracted chemical constituents may then optionally be further processed by heating in order to induce desired chemical transformations. The extracted chemical constituents are also processed by concentrating at reduced pressure, for example, by distillation.
Abstract: Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.
Type:
Grant
Filed:
March 14, 2012
Date of Patent:
August 15, 2017
Assignees:
MERCK SHARP & DOHME CORP., LAWRENCE LIVERMORE NATIONAL SECURITY, LLC
Inventors:
Daniel Bensen, Zhiyong Chen, John Finn, Thanh To Lam, Suk Joong Lee, Xiaoming Li, Douglas W. Phillipson, Leslie William Tari, Michael Trzoss, Junhu Zhang, Felice C. Lightstone, Toan B. Nguyen, Sergio E. Wong, Paul Aristoff, Michael Jung
Abstract: Provided is a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity, and useful as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, sleep disorder and the like. The present invention relates to a compound represented by the formula wherein ring A is a 4- to 7-membered ring optionally having substituent(s); L is —O—, —S—, —SO— or —SO2—; R1 is a C1-6 alkyl group optionally having substituent(s) (provided that when L is —O—, R1 is not a C1-6 alkyl group optionally substituted by halogen atom(s)), or a cyclic group optionally having substituent(s); X1 is —CRa? or —N?; X2 is —CRb? or —N?; X3 is —CRc= or —N?; Ra, Rb and Rc are each a C1-6 alkyl group, C2-6 alkenyl group, C1-6 alkoxy group, C3-6 cycloalkyl group, C3-6 cycloalkoxy group or C6-14 aryl group, each of which optionally having substituent(s), H or halogen, or a salt thereof.
Abstract: Compounds of the formula (I) in which R, R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumors.
Type:
Grant
Filed:
January 5, 2016
Date of Patent:
August 8, 2017
Assignee:
Merck Patent GmbH
Inventors:
Dieter Dorsch, Christian Sirrenberg, Thomas J. J. Mueller, Eugen Merkul, Gnuni Amatunu Karapetyan
Abstract: A method of identifying or evaluating synergistic combinations of actives such as skin-care actives that improve the metabolism of a cell and provides an advantage over using the actives alone. The method includes contacting cells with test agents, alone and in combination, and determining a response of the cells to the test agent(s), wherein the response corresponds to a change in a metabolic indicator associated with glycolysis and a change in a metabolic indicator associated with oxidative phosphylation.
Abstract: The present invention is directed to hydroxy compounds which are antagonists of orexin receptors. 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 orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
Type:
Grant
Filed:
April 21, 2014
Date of Patent:
August 8, 2017
Assignee:
MERCK SHARP & DOHME CORP.
Inventors:
Scott D. Kuduk, Nigel L. Liverton, Jason W. Skudlarek