Abstract: Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Such compounds disrupt Nek2/Hec1 binding and may be useful as chemotherapeutic agents for neoplastic diseases.
Type:
Grant
Filed:
November 29, 2012
Date of Patent:
April 7, 2015
Assignees:
Taivex Therapeutics Corporation, Development Center of Biotechnology
Inventors:
Jiann-Jyh Huang, Shih-Hsien Chuang, Ying-Shuan Eda Lee, Yu-Ling Huang, Johnson Lau
Abstract: The present invention relates to diarylpyridazinone derivatives that block the potassium Kv channels (specifically the Kv1.5, Kv4.3, and Kv11.1 channels) and to the use thereof for the treatment of humans. Said compounds have the general formula (I), where R1 and R2 are simultaneously or independently one or more groupings such as: halogen, such as F, Br, Cl, a straight or branched C1-C4 alkyl, hydroxy, a straight or branched C1-C4 alkoxy, arylsulfonamido, in which the aryl is optionally replaced with a straight or branched C1-C4 alkyl, or nitrile, as well as the various enantiomers and the mixtures thereof in any proportion, and the pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
December 20, 2011
Date of Patent:
March 31, 2015
Assignee:
Pierre Fabre Medicament
Inventors:
Elisabeth Dupont-Passelaigue, Isabelle Le Roy, Samuel Mialhe, Christophe Pignier
Abstract: This invention relates to a convenient and improved process for preparation of glatiramer acetate (copolymer-1) of pharmaceutical grade. The process involves polymerizing N-carboxyanhydrides of tyrosine, alanine, y-benzyl glutamate and ?-N-trifluoroacetyllysine in dioxane with diethylamine as initiator to afford protected copolymer-1. Treatment with hydrogen bromide in acetic acid at 35° C. for 3-5 h cleaves benzyl group to produce trifluoroacetyl copolymer-1. The trifluoroacetyl copolymer-1 is washed with an organic solvent to remove reactive benzyl bromide generated during debenzylation. Deprotection with aqueous piperidine, followed by dialysis offers glatiramer acetate (copolymer-1) of Molecular weight 5000-9000 daltons.
Abstract: [Problem] To provide a diphenyl sulfide derivative which is useful as a pharmaceutical product that has excellent S1P3 antagonist activity. [Solution] The inventors have discovered that a diphenyl sulfide derivative represented by general formula (1) (wherein R1 represents an alkoxy group having 1-6 carbon atoms, R2 represents a propyl group or an allyl group, X represents methylene or an oxygen atom, and Z represents a halogen atom) has excellent S1P3 antagonist activity as a result of extensive researches for the production of a compound that has S1P3 antagonist activity.
Type:
Grant
Filed:
December 20, 2011
Date of Patent:
March 31, 2015
Assignee:
Kyorin Pharmaceutical Co., Ltd.
Inventors:
Kumi Ishikawa, Shigeru Koga, Yasushi Kohno, Kiyoshi Fujii, Ken Yoshikawa
Abstract: The present invention provides new antiviral compounds and pharmacological compositions comprising these new compounds and their use in the prophylaxis, prevention and treatment of viral infections, particularly adenovirus and herpes virus infections.
Type:
Grant
Filed:
June 13, 2011
Date of Patent:
March 31, 2015
Assignee:
Eirium AB
Inventors:
Göran Wadell, Karin Edlund, Marten Strand, Emma Andersson, Christopher Öberg, Mikael Elofsson, Ya-Fang Mei
Abstract: The present invention provides sustained-release oral pharmaceutical compositions and methods of use. The sustained-release oral pharmaceutical compositions include an opioid (including salts thereof) and a salt of a non-steroidal anti-inflammatory drug (NSAID).
Type:
Grant
Filed:
December 14, 2012
Date of Patent:
March 24, 2015
Assignee:
Upsher Smith Laboratories, Inc.
Inventors:
Kenneth L. Evenstad, Christian F. Wertz, James S. Jensen, Victoria Ann O'Neill, Stephen M. Berge
Abstract: The present application relates to therapeutic organic compounds, compositions comprising an effective amount of a therapeutic organic compound; and methods for treating and preventing disease comprising administering and effective amount of a therapeutic organic compound to a subject in need thereof.
Type:
Grant
Filed:
February 18, 2011
Date of Patent:
March 24, 2015
Assignee:
Dana-Farber Cancer Institute, Inc.
Inventors:
Nathanael Gray, Wenjun Zhou, Xianming Deng
Abstract: Since each of the site I sodium channel blockers have a unique activity and cannot be used to extrapolate the same effective dosage for another site I sodium channel blocker, studies were conducted to identify dosages of neosaxitoxin (“NeoSTX”) and bupivacaine, alone or in combination with epinephrine, to provide two to three days of pain relief in humans. Bupivacaine-NeoSTX combinations produce more reliable blockade and longer duration blockade compared to NeoSTX alone. The three-way combination of NeoSTX-bupivacaine-epinephrine produces more prolonged local anesthesia than the two-way combination of NeoSTX-bupivacaine. Addition of epinephrine to this NeoSTX-bupivacaine combination dramatically prolongs the duration of complete blockade to a mechanical stimulus. These results led to development of specific combination dosage formulations.
Type:
Grant
Filed:
July 15, 2014
Date of Patent:
March 10, 2015
Assignee:
The Children's Medical Center Corporation
Abstract: Since each of the site I sodium channel blockers have a unique activity and cannot be used to extrapolate the same effective dosage for another site I sodium channel blocker, studies were conducted to identify dosages of neosaxitoxin (“NeoSTX”) and bupivacaine, alone or in combination with epinephrine, to provide two to three days of pain relief in humans. Bupivacaine-NeoSTX combinations produce more reliable blockade and longer duration blockade compared to NeoSTX alone. The three-way combination of NeoSTX-bupivacaine-epinephrine produces more prolonged local anesthesia than the two-way combination of NeoSTX-bupivacaine. Addition of epinephrine to this NeoSTX-bupivacaine combination dramatically prolongs the duration of complete blockade to a mechanical stimulus. These results led to development of specific combination dosage formulations.
Type:
Grant
Filed:
July 15, 2014
Date of Patent:
March 10, 2015
Assignee:
The Children's Medical Center Corporation
Abstract: Glucosylceramide synthase inhibitors and compositions containing the same are disclosed. Methods of using the glucosylceramide synthase inhibitors in the treatment of diseases and conditions wherein inhibition of glucosylceramide synthase provides a benefit, like Gaucher disease and Fabry disease, also are disclosed.
Type:
Grant
Filed:
October 15, 2012
Date of Patent:
February 24, 2015
Assignee:
The Regents of the University of Michigan
Inventors:
Scott Larsen, Akira Abe, Liming Shu, Michael William Wilson, Richard F. Keep, James A. Shayman
Abstract: The present invention relates to an acyclovir formulation having improved bioavailability resulting in better efficacy and/or requiring less frequent administration.
Type:
Grant
Filed:
March 15, 2013
Date of Patent:
February 10, 2015
Assignee:
Emisphere Technologies, Inc.
Inventors:
Amy C. Adams, Brahma N. Singh, Nikhil Dhoot, Shingai Majuru
Abstract: The invention is directed to a method of treating fibromyalgia syndrome in a subject, comprising administering a therapeutically effective amount of a carbamoyl compound, or pharmaceutically acceptable salt thereof.
Abstract: The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxyg
Type:
Grant
Filed:
October 12, 2007
Date of Patent:
December 23, 2014
Assignee:
Astex Therapeutics Limited
Inventors:
Neil James Gallagher, John Francis Lyons, Neil Thomas Thompson, Stephen Murray Yule, Christopher William Murray
Abstract: The 4-urea-phenyl substituted 6-morpholin-4-yl-pyrazolo[3,4-d]pyrimidine derivatives are potent and selective inhibitors of mTOR kinase and are useful in treating disorders related to abnormal mTOR activities such as cancer, immune disorders, cardiovascular disease, ocular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders.
Abstract: A method of treating polycystic kidney disease in a subject comprises administering to the subject an effective amount of a compound represented by Structural Formula (1): or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
October 3, 2008
Date of Patent:
December 16, 2014
Assignee:
Genzyme Corporation
Inventors:
Thomas A. Natoli, Oxana Ibraghimov-Beskrovnaya, John P. Leonard, Nelson S. Yew, Seng H. Cheng
Abstract: An aqueous formulation for topical application to the skin comprising water, a water-miscible organic solvent, and benzoyl peroxide, wherein the concentration of the organic solvent is sufficient to provide a stable suspension of benzoyl peroxide in the aqueous formulation without the inclusion of a surfactant in the formulation, wherein the ratio of concentrations of water and organic solvent in the formulation is sufficient to maintain the benzoyl peroxide in saturated solubility in the formulation following application to the skin, and wherein the concentration of benzoyl peroxide in the formulation is less than 5.0% and at least 1.0% w/w. The formulation may further contain a chemical compound in addition to benzoyl peroxide that is effective in the treatment of acne. The aqueous formulations of the invention are useful in the treatment of acne and acne rosacea.
Abstract: This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.
Abstract: The present invention relates to 2-thio-1,3,4-oxadiazoles 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 7, 2013
Date of Patent:
September 30, 2014
Assignee:
Allergan, Inc.
Inventors:
Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
Abstract: An individual alkamide and/or a mixture having two or more different alkamides, is disclosed for changing, masking or reducing the unpleasant flavor impression of an unpleasant-tasting substance or mixture of substances. The alkamide can be trans-pellitorine; cis-pellitorine; 2Z,4Z- or 2Z,4E-decadienoic acid-N-isobutylamide; 2E,4E-decadienoic acid-N-([2S]-2-methylbutyl)amide; 2E,4E-decadienoic acid-N-([2R]-2-methylbutylamide); 2E,4Z-decadienoic acid-N-(2-methylbutyl)amide; achilleamide; sarmentine; 2E- or 3E-decenoic acid-N-isobutylamide; 3E-nonenoic acid-N-isobutylamide; spilanthol; homospilanthol; 2E,6Z,8E-decatrienoic acid-N-([2R]-2-methylbutyl)amide; 2E- or 2Z-decen-4-oic acid-N-isobutylamide; ?-sanshool; ?-hydroxysanshool; ?-hydroxysanshool; ?-hydroxysanshool; ?-hydroxyisosanshool; ?-dehydrosanshool; ?-sanshool; bungeanool; isobungeanool; dihydrobungeanool; or tetrahydrobungeanool, or combinations thereof.
Type:
Grant
Filed:
November 6, 2008
Date of Patent:
September 9, 2014
Assignee:
Symrise AG
Inventors:
Kathrin Langer, Jakob Ley, Gerald Reinders, Günter Kindel, Gerhard Krammer
Abstract: The present invention relates to methods for treating optic disorders or for reducing or alleviating the signs, symptoms, or pathological conditions related to such optic disorders. In particular, methods are provided for treating optic disorders, or reducing the symptoms thereof, the methods involving the administration of one or more downstream folate compounds and/or methyl-B12. In one particular embodiment, the method comprises administration of L-methylfolate. In other embodiments, the method involves administering both L-methylfolate and methyl-B12. In still further embodiments, the method further involves reducing dietary intake of folic acid. In certain embodiments, the method further involves identifying a subject organism with a malfunction in one or more of the folate or B4 cycles. In certain embodiments, such a malfunction is one or more of the C677T and A1298C mutations.