Abstract: A compound of formula (I), useful for the treatment of cancer, inflammation and inflammatory disorders, and a pharmaceutical composition containing the compound.
Type:
Grant
Filed:
December 21, 2012
Date of Patent:
August 1, 2017
Assignee:
Kancera AB
Inventors:
Jessica Martinsson, Katarina Faernegardh, Mattias Joensson, Rune Ringom
Abstract: Substituted 1,2,3-triazole compounds are disclosed which have utility in the treatment of a variety of neurological disorders. The compounds provided herein have the general structure: wherein R1, R2, R3 and n are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound provided herein in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for treating neurological disorders in a subject in need thereof.
Type:
Grant
Filed:
January 29, 2016
Date of Patent:
August 1, 2017
Assignee:
Neurocrine Biosciences, Inc.
Inventors:
Neil J. Ashweek, John P. Williams, Deborah Slee, Manisha Moorjani
Abstract: The invention relates to plasminogen activator-1 (PAI-1) inhibitor compounds and uses thereof in the treatment of any disease or disorder associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to prevent or reduce thrombosis and fibrosis, to promote thrombolysis, and to modulate lipid metabolism and treat diseases or disorders associated with elevated PAI-1, cholesterol, or lipid levels.
Type:
Grant
Filed:
October 31, 2013
Date of Patent:
August 1, 2017
Assignees:
THE REGENTS OF THE UNIVERSITY OF MICHIGAN, EASTERN MICHIGAN UNIVERSITY
Inventors:
Daniel A. Lawrence, Cory Emal, Ashley Reinke, Shih-Hon Li, Mark Warnock, Gregory Abernathy
Abstract: The invention concerns chromenone derivatives of Formula I or a pharmaceutically-acceptable salts thereof, wherein each of R1, R2, R3, R4, R5, R6, R7, R8, n and R9 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
Type:
Grant
Filed:
March 24, 2016
Date of Patent:
August 1, 2017
Assignee:
ASTRAZENECA AB
Inventors:
Bernard Christophe Barlaam, Sebastien Louis Degorce, Christine Marie Paul Lambert-Van Der Brempt, Remy Robert Morgentin, Patrick Ple
Abstract: The present invention relates to type II and type III crystals of 9-ethyl-6,6-dimethyl-8-(4-morpholin-4-yl-piperidin-1-yl)-11-oxo-6,11-dihydro-5H-benzo[b]carbazole-3-carbonitrile that is a pharmaceutically useful novel crystal.
Abstract: Compounds having a structure of formula (I), including stereoisomers and pharmaceutically acceptable salts and solvates thereof: wherein R1 is as defined herein. Such compounds are inhibitors of the vesicular monoamine transporter 2 (VMAT2) and have utility for treating, for example, hyperkinetic disorders. Also disclosed are compositions containing these compounds in combination with a pharmaceutically acceptable carrier or diluent, as well as methods relating to the use in a subject in need thereof.
Abstract: The present invention discloses substituted 2-aminopyridine derivatives as protein kinase inhibitors; specifically, the invention relates to 2-aminopyridine derivatives having protein kinase inhibitory properties, their manufacture, pharmaceutical compositions containing them, and use of the compounds and the pharmaceutical compositions thereof for the treatment of diseases associated with protein kinase.
Type:
Grant
Filed:
January 27, 2014
Date of Patent:
July 18, 2017
Assignees:
CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD., Centaurus Biopharma Co., Ltd., LIANYUNGANG RUNZHONG PHARMACEUTICAL CO., LTD.
Abstract: Symmetrical marinopyrrole derivatives are disclosed herein, as is a synthetic route for producing these compounds. Also disclosed are methods of using symmetrical marinopyrrole derivatives to treat bacterial pathogens, like MRSE, MSSA and MRSA.
Type:
Grant
Filed:
January 22, 2014
Date of Patent:
July 11, 2017
Assignees:
H. Lee Moffitt Cancer Center and Research Institute, Inc., Chongqing Zein Pharmaceutical Co., Ltd.
Inventors:
Yong Qin, Chunwei Cheng, Hao Song, Rongshi Li, Yan Liu
Abstract: The disclosure provides novel chemical compounds represented by Formula I or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof. The compounds can be used as an inhibitor of Trk and are useful in the treatment of pain, cancer, inflammation, neurodegenerative disease and certain infectious diseases.
Type:
Grant
Filed:
December 14, 2015
Date of Patent:
July 11, 2017
Assignees:
CMG PHARMACEUTICAL CO., LTD., HANDOK INC.
Inventors:
Moonsoo Kim, Chaewoon Lee, Gilnam Lee, Cheol Hwan Yoon, Jeongbeob Seo, Je Hak Kim, MinWoo Lee, Hankyul Jeong, Hyang Choi, Myung Eun Jung, Kinam Lee, Hyun Jung Kim, Hye Kyoung Kim, Jae Il Lee, Misoon Kim, Soongyu Choi
Abstract: Provided are certain 1,2,3-triazole and 1,2,3-triazole dimer analogs of DM-PIT-1 which are second-generation selective non-phosphoinositide small molecule inhibitors of phosphatidylinositol-3,4,5-trisphosphate (PIP3), including 1,2,3-triazoles represented by formula (I) where: Ar represents aryl or heteroaryl; X represents O or S; each of Ra, Rb, Rc, and Rd independently represents hydrogen, halogen, C1-C10alkyl, —OH, —CF3, aryl, amino, or nitro; and Ar is optionally substituted with one or more substituents independently selected from the group consisting of halogen, C1-C10alkyl, —OH, —CF3, amino, and nitro. Also provided are pharmaceutical compositions comprising compounds of the invention and a pharmaceutical carrier. Also provided are methods of inhibiting PIP3-mediated signaling in a cell and treating cancer using compounds of the invention.
Type:
Grant
Filed:
March 18, 2014
Date of Patent:
July 11, 2017
Assignees:
TUFTS UNIVERSITY, COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH
Inventors:
Alexei Degterev, Chepuri V. Ramana, Jinbo Lee, Yadagiri Kommagalla
Abstract: The present invention relates to the compound (2R,2?R)-bis(((((tetrahydro-2H-pyran-4-yl)oxy)carbonyl)oxy)methyl) 1,1?-adipoylbis(pyrrolidine-2-carboxylate) of formula (I), pharmaceutical compositions comprising the same and the use of the same for treatment of diseases or disorders wherein depletion of serum amyloid P component (SAP) would be beneficial, including amyloidosis, Alzheimer's disease, type 2 diabetes mellitus and osteoarthritis.
Type:
Grant
Filed:
April 27, 2015
Date of Patent:
July 11, 2017
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Abstract: The present invention provides compounds of Formula (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.
Type:
Grant
Filed:
March 13, 2014
Date of Patent:
July 4, 2017
Assignee:
NOVARTIS AG
Inventors:
Robert John Aversa, Paul Andrew Barsanti, Matthew Burger, Michael Patrick Dillon, Alan Dipesa, Cheng Hu, Yan Lou, Gisele Nishiguchi, Yue Pan, Valery Polyakov, Savithri Ramurthy, Alice Rico, Lina Setti, Aaron Smith, Sharadha Subramanian, Benjamin Taft, Huw Tanner, Lifeng Wan, Naeem Yusuff
Abstract: 3,3?-Disubstituted indoline compounds, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
Type:
Grant
Filed:
October 6, 2014
Date of Patent:
June 27, 2017
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Jonathan E. Wilson, Petr Vachal, Ravi Kurukulasuriya
Abstract: The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK2 kinase is involved.
Type:
Grant
Filed:
February 27, 2014
Date of Patent:
June 27, 2017
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Michael Miller, Kallol Basu, Duane DeMong, Jack Scott, Hong Liu, Xing Dai, Andrew Stamford, Marc Poirier, Paul Tempest
Abstract: Disclosed herein are compounds of formula (I) wherein L1, L2, L3, L4, R1, R4, R5, R6, and s are as defined in the specification. Compounds of formula (I) are EP4 agonists useful in the treatment of glaucoma, osteoporosis, bone fracture, periodontal bone loss, orthopedic implant, alopecia, neuropathic pain, and related disorders. Pharmaceutical compositions and methods of treating conditions or disorders are also described.
Type:
Grant
Filed:
March 14, 2014
Date of Patent:
June 27, 2017
Assignee:
CAYMAN CHEMICAL COMPANY, INC.
Inventors:
Stephen Douglas Barrett, Joseph Michael Colombo, Bradlee David Germain, Gregory William Endres, Andriy Komilov, James Bernard Kramer, Adam Uzieblo, Fred Lawrence Ciske, Kirk M. Maxey, James Paul O'Malley, Thomas Allen Owen
Abstract: The present invention provides bumetanide analogs and compositions comprising such analogs. The present invention also provides pharmaceutical compositions containing these bumetanide analogs and methods for their use. These analogs are particularly useful for the treatment and/or prophylaxis of conditions that involve the Na+K+Cl? co-transporter or GABAA receptor including but not limited to addictive disorders, Alzheimer's Disease, anxiety disorders, ascites, autism, bipolar disorder, cancer, depression, endothelial corneal dystrophy, edema, epilepsy, glaucoma. Huntington's Disease, insomnia, ischemia, migraine, migraine with aura, neuropathic pain, nociceptive neuralgia, nociceptive pain, ocular diseases, pain, Parkinson's disease, personality disorders, postherpetic neuralgia, psychosis, schizophrenia, seizure disorders, tinnitus, and withdrawal syndromes.
Abstract: A new molecular sieve material is designated as EMM-23 and has, in its as-calcined form, an X-ray diffraction pattern including the following peaks in Table 1: TABLE 1 d-spacing (?) Relative Intensity [100 × I/I(o)] 17.5-16.3 60-100 10.6-10.1 5-50 9.99-9.56 20-70? 6.23-6.06 1-10 5.84-5.69 1-10 5.54-5.40 1-10 4.29-4.21 1-10 3.932-3.864 1-10 3.766-3.704 5-40 3.735-3.674 1-10 3.657-3.598 1-10 3.595-3.
Type:
Grant
Filed:
October 21, 2015
Date of Patent:
June 20, 2017
Assignee:
ExxonMobil Chemical Patents Inc.
Inventors:
Allen W. Burton, Karl G. Strohmaier, Hilda B. Vroman
Abstract: A molecule with neural activities, especially 4-substituent-2-hydroxymorpholin-3-one, as a new intermediate of neurokinin-1 receptor antagonist aprepitant, and preparation method thereof.
Abstract: A method for obtaining solutions that contain 1,2,4-triazole-5-one (OTA) in concentrated sulphuric acid, includes using 3-amino-1,2,4-triazole (ATA) as a precursor of OTA. There is also provided a method for preparing 3-nitro-1,2,4-triazole-5-one (4) (ONTA) from the solutions.
Type:
Grant
Filed:
April 4, 2014
Date of Patent:
June 13, 2017
Assignees:
HERAKLES, EURENCO
Inventors:
Grégoire Herve, Guy Jacob, Guy Cagnon, Jean-Marc Bouchez
Abstract: The invention disclosed herein is directed to compounds of Formula I and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention disclosed herein is also directed to methods of treating prostate, breast, ovarian, liver, kidney, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention disclosed herein is further directed to methods of treating prostate, breast, colon, pancreatic, chronic lymphocytic leukemia, melanoma and other cancers comprising administration of a therapeutically effective amount of a selective PPAR? antagonist.
Type:
Grant
Filed:
December 10, 2013
Date of Patent:
June 13, 2017
Assignee:
Inception 2, Inc.
Inventors:
Nicholas Simon Stock, Austin Chih-Yu Chen, Yalda Mostofi Bravo, Jason Duarte Jacintho, Jill Melissa Baccei, Brian Andrew Stearns, Ryan Christopher Clark