Abstract: Compounds of the formula (I), in which R1, R2, R3, R4 and R5 have the meanings indicated in Claim 1, are inhibitors of cell proliferation\cell vitality and can be employed for the treatment of tumors.
Type:
Grant
Filed:
June 19, 2012
Date of Patent:
October 15, 2013
Assignee:
Merck Patent GmbH
Inventors:
Dieter Dorsch, Christian Sirenberg, Thomas J. J. Mueller, Eugen Merkul
Abstract: The present invention relates to nonaqueous preparation for percutaneous absorption prepared by laminating an adhesive layer comprising a nonsteroidal anti-inflammatory analgesic in an alkali metal salt form, and an inorganic acid which is strongly acidic compared with the nonsteroidal anti-inflammatory analgesic in a free form, together with a nonaqueous base, on a support. According to the present invention, drug-releasing characteristics and skin penetration in a nonaqueous preparation for percutaneous absorption can be improved because the addition of an inorganic acid in a nonaqueous base containing a drug in an alkali metal salt form leads to an improvement in the solubility of the drug in the base, and a good partitioning of the drug to skin surface. In addition, as the inorganic acid has no alcoholic hydroxy group in the structure, the inorganic acid does not react with the drug, therefore it causes no lowering in the stability of the drug by esterification.
Abstract: The present invention provides compounds of Formula I along with compositions containing the same and methods of use thereof in treating oxidative stress.
Abstract: The invention provides a novel class of 2,7-naphthyridin derivatives; pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Syk, ZAP70, KDR, FMS, FLT3, c-Kit, RET, TrkA, TrkB, TrkC-GR-1R, Alk, c-FMS, or combinations thereof.
Type:
Grant
Filed:
January 27, 2009
Date of Patent:
October 1, 2013
Assignee:
IRM LLC
Inventors:
Barun Okram, Tetsuo Uno, Qiang Ding, Yahua Liu, Yunho Jin, Qihui Jin, Xu Wu, Jianwei Che, S. Frank Yan, Xueshi Hao
Abstract: This invention provides novel compounds, methods of using the compounds, and pharmaceutical compositions containing the compounds.
Type:
Grant
Filed:
November 16, 2012
Date of Patent:
October 1, 2013
Assignees:
Eli Lilly and Company, Anacor Pharmaceuticals, Inc.
Inventors:
Tsutomu Akama, Terry William Balko, Jean Marie Defauw, Jacob J. Plattner, William Hunter White, Joseph Raymond Winkle, Yong-Kang Zhang, Yasheen Zhou
Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
Type:
Grant
Filed:
March 24, 2009
Date of Patent:
October 1, 2013
Assignee:
Medivation Technologies, Inc.
Inventors:
David T. Hung, Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain
Abstract: The invention relates to the combination of an endothelin receptor antagonist of formula (I) with paclitaxel, and in particular to this combination for therapeutic use, simultaneously, separately or over a period of time, in the treatment of ovarian cancer.
Abstract: An object of the present invention is to provide a novel crystal form of a compound that has an inhibitory effect on activated blood coagulation factor X and is useful as a pharmaceutical compound for prevention and/or treatment of thrombotic and/or embolic diseases. The present invention provides a novel crystal form of N1-(5-chloropyridin-2-yl)-N2-((1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide p-toluenesulfonate monohydrate, and method for producing the same.
Abstract: Compositions are provided which contain immobilized flavorants for flavor delivery. In particular, smoking compositions are provided which contain flavorant ester salts of polycarboxylic acids.
Type:
Grant
Filed:
July 9, 2008
Date of Patent:
September 24, 2013
Assignee:
Philip Morris USA Inc.
Inventors:
Munmaya K. Mishra, Shengsheng Liu, Diane S. Kellogg
Abstract: The treatment of humans or other mammals for eczema and/or psoriasis using dosage forms or compositions that include cetyl myristate alone or (in admixture or serially) both cetyl myristate and cetyl palmitate.
Type:
Grant
Filed:
February 24, 2012
Date of Patent:
September 17, 2013
Assignee:
Lypanosys Pte Limited
Inventors:
Timothy David Meakin, Dianne Cadwallader, Craig Leonard Heatley
Abstract: The method includes the steps of cleansing of the scalp sufficiently to remove material which would otherwise block antiviral medication from reaching hair follicles, heating the scalp to increase the absorption of the antiviral medication and applying the antiviral medication to the scalp in effective amount to suppress viral replication or viral activation present in the nerves leading to the scalp.
Abstract: The present invention provides methods of inhibiting human myeloid leukemia cell growth and proliferation by administering a thrombopoietin receptor agonist (TpoRA), a derivative, or variant thereof, to an individual with AML.
Type:
Grant
Filed:
October 8, 2008
Date of Patent:
September 10, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Alan Gewirtz, Anna Kalota, Connie L. Erickson-Miller
Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl sulfonamides and related compounds (collectively referred to herein as ‘BPSAAA compounds’), as described herein, and including, for example, biphenyl-4-sulfonic acid (hydroxyalkyl-phenyl)-amides and related compounds.
Type:
Grant
Filed:
March 20, 2008
Date of Patent:
September 3, 2013
Assignee:
PIMCO 2664 Limited
Inventors:
Iain Robert Greig, Robert Jurgen Van't Hof, Stuart Hamilton Ralston
Abstract: The present invention provides a scalable process for the preparation of stilbenes by (i) condensing 3,5-dialkylbenzyl phosphonates with 4?-O-tetrahydropyranyl benzaldehyde to get 3,5-alkyl-4?-O-tetrahydropyranyl Stilbene and (ii) deprotecting the obtained 3,5-Dialkyl-4?-O-tetrahydropyranylstilbene to yield stilbenes. The present invention also provides a novel intermediate 3,5-Dialkyl-4?-O-tetrahydropyranyl stilbene, which is a key intermediate for the synthesis of stilbenes such as Pterostilbene and Resveratrol. The present invention also provides characteristics of various solid forms of Pterostilbene, methods for their preparation, as well as dosage forms containing the same for administration to or consumption by humans.
Type:
Grant
Filed:
January 21, 2011
Date of Patent:
September 3, 2013
Assignee:
Laurus Labs Private Limited
Inventors:
Gottumukkala V. Subbaraju, Masna Mahesh, Hindupur R. Mohan, Thatipally Suresh, Igor Ivanisevic, Mark Andres, Kyle Stephens
Abstract: Water-soluble compositions comprising a lipophilic compound and a solubilizing agent of the general formula: {X—OOC—[(CH2)n—COO]m}p—Y??(I) wherein: X is a residue of a hydrophobic moiety, Y is a residue of a hydrophilic moiety, p is 1 or 2, m is 0 or 1, and n is an integer greater than or equal to 0 are disclosed. The lipophilic compound is preferably selected from the group consisting of water-insoluble ubiquinones, ubiquinols, vitamins, provitamins, polyene macrolide antibiotics, and mixtures thereof. The hydrophobic moiety is preferably a sterol or a tocopherol and the hydrophilic moiety is preferably a polyalkylene glycol. In some embodiments, the sterol is cholesterol or sitosterol, the tocopherol is ?-(+)-tocopherol, the polyalkylene glycol is a polyethylene glycol or its methyl monoether having an average molecular weight between 400 and 1000, p is equal to 1 or 2, m is equal to 0 or 1 and n is an integer between 2 and 18.
Type:
Grant
Filed:
April 28, 2009
Date of Patent:
September 3, 2013
Assignee:
National Research Council of Canada
Inventors:
Henryk Borowy-Borowski, Marianna Sikorska-Walker, P. Roy Walker
Abstract: The present invention is about the use of at least one epothilone or derivative thereof as an active ingredient for manufacturing a medicament for use in the treatment of disease(s) involving a neuronal connectivity defect.
Type:
Grant
Filed:
September 9, 2010
Date of Patent:
August 20, 2013
Assignees:
Institut National de la Sante et de la Recherche Medicale, Commissariat a l'Energie Atomique, Gesellschaft fur Biotechnologische Forschung mbH (GBF)
Inventors:
Annie Andrieux, Didier Job, Annie Schweitzer, Gerhard Höfle
Abstract: Indazole compounds, processes for their preparation, intermediates usable in these processes, pharmaceutical compositions containing such compounds and their use in therapy.
Type:
Grant
Filed:
October 2, 2012
Date of Patent:
August 13, 2013
Assignee:
Glaxo Group Limited
Inventors:
Simon Teanby Hodgson, Yannick Maurice Lacroix, Panayiotis Alexandrou Procopiou
Abstract: The present invention concerns compounds derived from the anaethetic propofol. The compounds may be useful in the treatment of pain, particularly, but not exclusively, chronic pain and central pain sensitisation.
Type:
Grant
Filed:
December 9, 2009
Date of Patent:
August 13, 2013
Assignee:
The University of Dundee
Inventors:
Martin Leuwer, Paul O'Neill, Neil Berry, Gertrud Haeseler
Abstract: There is provided a salt of 1-cyclopropyl-8-methyl-7-[5-methyl-6-(methylamino)-3-pyridinyl]-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid selected from the group consisting of citrate, hemi-fumarate, maleate, L-tartrate, mesylate, hydrochloride, potassium, and sodium salts.