Abstract: The invention provides a process for preparing N,N?-di(3?,5?-dimethylphenyl)perylene bis(dicarboximide), and other pigments having modified properties, by reaction of perylene-3,4,9,10-tetracarboxylic dianhydride with 3,5-dimethylaniline, or a mixture of 3,5-dimethyl aniline and at least one other primary amine, in the presence of a secondary amine or tertiary amine as catalyst, wherein the reaction occurs in an aqueous reaction medium and in the presence of added seed crystals of N,N?-di(3?,5?-dimethylphenyl) perylenebis(dicarboximide), such that the aqueous medium is present at the beginning of the reaction.
Type:
Grant
Filed:
February 18, 2008
Date of Patent:
May 14, 2019
Assignee:
BASF SE
Inventors:
Heinrich Kowarsch, Josef Hetzenegger, Andreas Stohr, Hans-Joachim Uschmann
Abstract: In a first aspect, the present invention relates to new compounds as depicted in formula (I). In particular, compounds according to the present invention are bisindolylcyclobuten-dione-based structures having antiprotozoal activity. In a further aspect, pharmaceutical compositions containing the same are provided as well as the use of the compounds and pharmaceutical compositions for the prophylaxis and treatment of parasite based diseases including malaria. Finally, methods for the treatment of parasite diseases including malaria are provided.
Type:
Grant
Filed:
July 10, 2015
Date of Patent:
May 14, 2019
Assignees:
TECHNISCHE UNIVERSITAET BRAUNSCHWEIG, YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD.
Inventors:
Conrad Kunick, Hoang Lande, Johann Gruenefeld, Ron Dzikowski, Abed Nasereddin
Abstract: The present invention provides a compound having the structure: (structurally represented) wherein R1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl; R6 is H, OH, or halogen; B is a substituted or unsubstituted heterobicycle, pyridazine, pyrazole, pyrazine, thiadiazole, or triazole, wherein the heterobicycle is other than chloro substituted indole; and the pyrazole, when substituted, is substituted with other than trifluoromethyl, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
March 13, 2014
Date of Patent:
April 30, 2019
Assignee:
THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
Inventors:
Konstantin Petrukhin, Christopher Cioffi, Graham Johnson, Nicoleta Dobri, Emily Freeman, Ping Chen, Michael Conlon, Lei Zhu
Abstract: The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
Type:
Grant
Filed:
June 13, 2017
Date of Patent:
April 23, 2019
Assignee:
AUTIFONY THERAPEUCTICS LIMITED
Inventors:
Giuseppe Alvaro, Paolo Dambruoso, Simona Tommasi, Anne Decor, Charles Large, Agostino Marasco
Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
Type:
Grant
Filed:
May 9, 2017
Date of Patent:
April 9, 2019
Assignee:
Nimbus Lakshmi
Inventors:
Markus Dahlgren, Jeremy Robert Greenwood, Geraldine C. Harriman, Joshua Jahmil Kennedy-Smith, Craig E. Masse, Donna L. Romero, Mee Shelley, Ronald T. Wester
Abstract: The naphthyridinyl hydrazine derivatives as potent peripheral analgesic agents are (E)-2-(substituted benzylidene)-1-(2,7-dialkyl-1,8-naphthyridinyl) hydrazines that provide effective peripheral analgesic activity, as demonstrated using the mouse writhing test. The new target compounds include at least one compound that demonstrates higher potency in providing analgesic relief in mice (Protection (%)=81.44) compared to the reference drug acetyl salicylic acid (Protection (%)=78.47). These results demonstrated that the target compound exerts acute analgesic action, suggesting that it may represent an alternative in the development of new therapeutic strategies. Preferably, the (E)-2-(substituted benzylidene)-1-(2,7-dialkyl naphthyridinyl) hydrazine has the formula: wherein R1 and R2 are alkyl, R3 is hydrogen, and R4 is NO2.
Type:
Grant
Filed:
June 16, 2017
Date of Patent:
March 26, 2019
Assignee:
King Saud University
Inventors:
Nagy Mahmoud Hassan Khalifa, Mohamed A. Al-Omar
Abstract: Disclosed herein is a process of making a compound of formula I The compound of formula I is an inhibitor of MEK and thus can be used to treat cancer.
Type:
Grant
Filed:
August 25, 2017
Date of Patent:
March 26, 2019
Assignees:
EXELIXIS, INC., GENENTECH, INC.
Inventors:
Sriram Naganathan, Nathan Guz, Matthew Pfeiffer, C. Gregory Sowell, Tracy Bostick, Jason Yang, Amit Srivastava, Neel Kumar Anand
Abstract: Provided herein are processes for forming sufentanil citrate from sufentanil base. One process comprises forming sufentanil citrate in the presence of a polar non-aqueous solvent. Other processes comprise forming sufentanil citrate in the presence of water.
Type:
Grant
Filed:
May 25, 2016
Date of Patent:
March 12, 2019
Assignee:
SpecGX LLC
Inventors:
George Helmut Klemm, Brian Orr, Joel McClenaghan
Abstract: Described are novel salts of the compound (3R,4R,5S)-5-(difluoromethyl) piperidine-3,4-diol, as well as methods of using the same for preventing and/or treating lysosomal storage disorders and/or degenerative disorders of the central nervous system. In particular, the present invention provides methods for preventing and/or treating Gaucher's disease and/or Parkinson's disease.
Type:
Grant
Filed:
August 31, 2017
Date of Patent:
March 5, 2019
Assignee:
Amicus Therapeutics, Inc.
Inventors:
Robert Boyd, Philip J. Rybczynski, Kamlesh Sheth
Abstract: The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors.
Abstract: Disclosed herein are aza-pyridone compounds, pharmaceutical compositions that include one or more aza-pyridone compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an orthomyxovirus infection, with an aza-pyridone compound. Examples of an orthomyxovirus viral infection include an influenza infection.
Type:
Grant
Filed:
March 9, 2016
Date of Patent:
February 19, 2019
Assignee:
Alios BioPharma, Inc.
Inventors:
Robert Than Hendricks, Leonid Beigelman, David Bernard Smith, Antitsa Dimitrova Stoycheva
Abstract: [1,2,4]triazolo[1,5-a]pyridine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diseases involving cartilage degradation, bone and/or joint degradation, for example osteoarthritis; and/or conditions involving inflammation or immune responses, such as Crohn's disease, rheumatoid arthritis, psoriasis, allergic airways disease (e.g. asthma, rhinitis), juvenile idiopathic arthritis, colitis, inflammatory bowel diseases, endotoxin-driven disease states (e.g. complications after bypass surgery or chronic endotoxin states contributing to e.g. chronic cardiac failure), diseases involving impairment of cartilage turnover (e.g.
Type:
Grant
Filed:
August 15, 2016
Date of Patent:
February 19, 2019
Assignee:
GALAPAGOS NV
Inventors:
Christel Jeanne Marie Menet, Luc Juliaan Corina Van Rompaey, Stephen Robert Fletcher, Javier Blanc, Nolwenn Jouannigot, Alastair James Hodges, Koen Kurt Smits
Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof in which m, n, W, X, Y, Z, R1, R2, R3, R4 and R5 are as defined in the specification, compositions containing them and their use in therapy.
Abstract: The present invention relates to novel cluster boron compounds and their use as sodium channel blockers. The invention also provides methods for making and using the compounds.
Type:
Grant
Filed:
August 18, 2015
Date of Patent:
February 12, 2019
Assignee:
THE CURATORS OF THE UNIVERSITY OF MISSOURI
Inventors:
George R. Kracke, Yulia Sevryugina, Marion Frederick Hawthorne
Abstract: The present invention provides a compound of Formula I, and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing unstable angina, refractory angina, myocardial infarction, transient ischemic attacks, atrial fibrillation, thrombotic stroke, embolic stroke, deep vein thrombosis, disseminated intravascular coagulation, ocular build up of fibrin, and reocclusion or restenosis of recanalized vessels. The compounds are selective Factor IXa inhibitors.
Inventors:
Ting Zhang, Yi-Heng Chen, Liangqin Guo, Alan Hruza, Tianying Jian, Bing Li, Dongfang Meng, Dann L. Parker, Edward C. Sherer, Harold B. Wood, Isao Sakurada
Abstract: The present invention relates to novel crystal forms of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid. More particularly, the invention relates to polymorph forms of Polymorph Form I, Polymorph Form II, Polymorph Form III, Polymorph Form IV, Polymorph Form V, and Polymorph Form VI, and to processes for the preparation of, compositions containing and to uses of, such polymorph forms.
Abstract: The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.
Type:
Grant
Filed:
April 26, 2017
Date of Patent:
January 8, 2019
Assignee:
Incyte Corporation
Inventors:
Liangxing Wu, Chunhong He, Xiaozhao Wang, Joel R. Courter, Fenglei Zhang, Wenqing Yao
Abstract: Provided herein is a compound, 1-(4-(3-amino-[1,2,3]triazolo[1,5-a]pyridin-4-yl)phenyl)-3-(3-chlorophenyl)urea, pharmaceutical compositions thereof, and crystal forms thereof. Also provided are particles (e.g., nanoparticles) comprising the compound, and pharmaceutical compositions thereof, that are mucus penetrating. Also provided herein are methods and kits for using the compound, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.
Type:
Grant
Filed:
December 10, 2015
Date of Patent:
January 8, 2019
Assignee:
Kala Pharmaceuticals, Inc.
Inventors:
Pawel Wojciech Nowak, Minh Ngoc Nguyen, Elizabeth Enlow, Winston Zapanta Ong
Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof in which q, R11, R12, R13 and R14 are as defined in the specification, for use in therapy.
Type:
Grant
Filed:
September 12, 2016
Date of Patent:
January 1, 2019
Assignee:
Takeda Pharmaceutical Company Limited
Inventors:
Colm Carroll, Anne Goldby, Martin Teall
Abstract: Disclosed is a compound of formula (I). or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions including the compound of formula (I) and methods of using the compound of formula (I).
Type:
Grant
Filed:
December 16, 2016
Date of Patent:
December 25, 2018
Assignee:
THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
Inventors:
Gregory R. Thatcher, Marton Siklos, Rui Xiong