Abstract: The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof The Formula (I) compounds inhibit tyrosine kinase activity of Jak2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.
Type:
Grant
Filed:
December 17, 2009
Date of Patent:
August 26, 2014
Assignee:
Bristol-Myers Squibb Company
Inventors:
Ashok Vinayak Purandare, Douglas G. Batt, Qingjie Liu, Harold Mastalerz, Kurt Zimmermann
Abstract: The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydromorphone (4,5-?-epoxy-3-hydroxy-17-methyl morphinan-6-one) to form novel prodrugs/compositions of hydromorphone. The hydromorphone prodrugs of the present technology have decreased side effects and decreased potential for abuse compared to unconjugated hydromorphone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.
Type:
Grant
Filed:
October 25, 2012
Date of Patent:
August 26, 2014
Assignee:
KemPharm, Inc.
Inventors:
Travis Mickle, Sven Guenther, Guochen Chi, Jaroslaw Kanski, Andrea K. Martin, Bindu Bera
Abstract: This invention is a method of killing the stealthy intra-cellular bacteria which are key to the pathogenesis Cancers. These very tiny L-form Cell-Wall-Deficient (CWD) antibiotic-resistant bacteria live within the cytoplasm of cells, including the phagocytic cells (e.g. monocytes, macrophages, lymphocytes, neutrophils and polymorphonuclear cells) of the immune system itself. The cellular proliferation in Cancer is catalysed the action of the same tiny L-form bacteria. They cause the cell nucleus to release mRNA signaling the Th1 cytokine cascade without the need for conventional signaling via, for example, CD4+T -Lymphocytes. Some of these Cytokines and Chemokines, including, without limitation, Cellular Adhesion Molecule (CAM), create the environment which allows the cellular proliferation to start, and then allows the cancerous growth to gain a foothold in the body. Killing these stealthy pathogens removes the environment needed to initiate and feed the cellular proliferation commonly called ‘Cancer’.
Abstract: The present invention provides a novel class of pro-fluorescent probes for reactive oxygen species (ROS). One exemplary probe is mitochondria peroxy yellow 1 (MitoPY1), a new type of flurophore for imaging mitochondrial H2O2 in living cells with ROS and spatial specificity. The invention also provides methods of using pro-fluorescent probes to detect analytes. One exemplary method comprises using a pro-fluorescent probe of the invention to detect an explosive.
Type:
Grant
Filed:
June 8, 2009
Date of Patent:
July 29, 2014
Assignee:
The Regents of the University of California
Abstract: The present invention is directed to a series of citrate ester emulsifiers that are effective in making water in oil (regular emulsions) and oil in water (invert emulsions). In addition to being outstanding emulsifiers, these emulsifiers provide unique solubility, liquidity and outstanding feel when applied to the skin, making them highly desirable in cosmetic emulsions.
Abstract: Nitrone, nitroso, and nitroxide spintraps and spin labels and their reduction products are claimed for the prevention and treatment of fibrocystic disease of breast, premenstrual dysphoric syndrome and associated symptomology, prevention and treatment of migraine headache, cyclic vomiting syndrome, rectal hemorrhoids, trigeminal neuralgia, peripheral vascular disease, influenza, peridontitis and gingivitis, herpes zoster, herpes simplex, and post-herpetic neuralgia.
Abstract: The present invention is directed to a wound composition comprising an effective amount of phenytoin and an effective amount of vitamin C. The present invention is further directed to a method of treating a wound in a patient comprising administering an effective amount of phenytoin and an effective amount of vitamin C to the wound.
Abstract: The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
Type:
Grant
Filed:
April 3, 2009
Date of Patent:
July 8, 2014
Assignee:
Almirall, S.A.
Inventors:
Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Bernet Vidal Juan, Nuria Aguilar Izquierdo
Abstract: A process for the preparation of (R)-2-(3-diisopropylamino-1-phenylpropyl)-4-(hydroxymethyl)-phenol isobutyrate (Fesoterodine) or a pharmaceutically acceptable salt thereof having low content in impurities.
Type:
Grant
Filed:
November 14, 2011
Date of Patent:
July 8, 2014
Assignee:
Dipharma Francis S.r.l.
Inventors:
Marco Artico, Emanuele Attolino, Pietro Allegrini, Gabriele Razzetti
Abstract: The invention provides an oil-in-water type cosmetic emulsion which can be applied to the skin without stickiness, and impart resilient and supple feel to the skin, while having good stability without causing viscosity decrease or separation even during a long-term storage. The oil-in-water type cosmetic emulsion comprises (a) a higher alcohol having 14 to 22 carbon atoms, (b) a hydrophilic polyoxyethylene alkyl ether, and (c) a glycerin monoalkyl ether, wherein alkyl moieties in (b) and (c) are linear saturated alkyl chains, and molar concentrations of (a) to (c) satisfy a relation [(b)+(c)]/(a)=0.1 to 1.0, and preferably satisfy a relation [(a)+(c)]/(b)=3 to 20.
Abstract: The invention relates to compositions and co-crystals each comprising VX-950 and a co-crystal former selected from the group consisting of 4-hydroxybenzoic acid, 4-amino salicylic acid, phenylalanine, threonline, tartaric acid, adipic acid, succinic acetate, proline, methyl 4-hydroxybenzoate, anthranilic acid, and d-Biotin. Also within the scope of this invention are methods of making and using the same.
Type:
Grant
Filed:
February 27, 2008
Date of Patent:
June 24, 2014
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Patrick R. Connelly, Irina Kadiyala, Kathy Stavropoulos, Yuegang Zhang, Steven C. Johnston, Govinda Rao Bhisetti, Valdas Jurkauskas, Peter Rose
Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.
Type:
Grant
Filed:
November 10, 2011
Date of Patent:
June 17, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Heather E. Stevenson, Cheng Wang, C. Blair Zartman
Abstract: The present invention relates to novel benzyl azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
Type:
Grant
Filed:
November 11, 2011
Date of Patent:
May 20, 2014
Assignee:
Allergan, Inc.
Inventors:
Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha Bin Im
Abstract: The present invention is directed to pyridazine carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. 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 orexin receptors are involved.
Type:
Grant
Filed:
October 26, 2009
Date of Patent:
April 22, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Paul J. Coleman, Christopher D. Cox, Swati P. Mercer, Anthony J. Roecker, John D. Schreier
Abstract: This invention relates to, among other items, benzoxaborole compounds and their use for treating bacterial infections.
Type:
Grant
Filed:
September 7, 2011
Date of Patent:
April 22, 2014
Assignee:
Anacor Pharmaceuticals, Inc.
Inventors:
Vincent S. Hernandez, Charles Ding, Jacob J. Plattner, Michael Richard Kevin Alley, Fernando Rock, Suoming Zhang, Eric Easom, Xianfeng Li, Ding Zhou
Abstract: The invention relates to compounds of formula (I) wherein R, R0, R1, m, n and X1 to X4 have the meaning as cited in the description and the claims. These compounds are useful as Histamine H3 receptor antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
Type:
Grant
Filed:
May 5, 2009
Date of Patent:
April 8, 2014
Assignee:
Evotec AG
Inventors:
Adam James Davenport, David James Hallett, Massimo Corsi
Abstract: An agrochemical composition comprises an azole active ingredient and an N,N-dialkyl long chain alkylamide. The N,N-dialkyl long chain alkylamide is present in sufficient amount to prevent or inhibit the crystallization of the azole derivative during the application of the composition to a locus. Preferred N,N-Dialkyl long chain alkylamide(s) comprised in the composition is/are selected from the group consisting of compounds of the formula (I): in which (a) R1 and R2 are independently normal alkyl radicals having 2 carbon atoms, and R represents an alkyl group having from 10 to 30 carbon atoms; or (b) R1 and R2 are independently normal alkyl radicals having 3 carbon atoms, and R represents an alkyl group having from 9 to 30 carbon atoms; or 20 (c) R1 and R2 are independently normal alkyl radicals having from 4 to 20 carbon atoms and R represents an alkyl group having from 6 to 30 carbon atoms.
Abstract: The invention relates to a medicament for preventing and/or treating fatty liver which comprises as an active ingredient cilostazol or a pharmaceutically acceptable salt thereof.