Abstract: Provided are novel heterocyclic compounds useful as anti-cancer drugs by suppressing protein kinase activities of growth factor receptors such as c-Met, pharmaceutical compositions containing the same, and methods for using the compound.
Type:
Grant
Filed:
August 28, 2009
Date of Patent:
February 17, 2015
Assignee:
Neopharm Co., Ltd.
Inventors:
Tae-Seong Kim, Eunkyung Lee, Doyoung Kim, Bu-mahn Park, Jiyeon Park, JungJe Joo
Abstract: Disclosed are formulations of gamma-hydroxybutyrate in an aqueous medium that are resistant to microbial growth. Also disclosed are formulations of gamma-hydroxybutyrate that are also resistant to the conversion into GBL. Disclosed are methods to treat sleep disorders, including narcolepsy, with these stable formulations of GHB. The present invention also provides methods to treat alcohol and opiate withdrawal, reduced levels of growth hormone, increased intracranial pressure, and physical pain in a patient.
Type:
Grant
Filed:
March 6, 2013
Date of Patent:
February 10, 2015
Assignee:
Jazz Pharmaceuticals, Inc.
Inventors:
Harry Cook, Martha Hamilton, Douglas Danielson, Colette Goderstad, Dayton T. Reardan
Abstract: Cancer can be treated by administration of a hypoxia-activated prodrug, such as TH-302, alone or in combination with other anticancer agents and/or radiation therapy. In combination therapy, the hypoxia-activated prodrug and another anti-cancer agent or radiation therapy may be administered within the same 24-hour period, and administration of the hypoxia-activated prodrug may be completed prior to beginning administration of the other anticancer agent or radiation therapy.
Type:
Grant
Filed:
October 21, 2009
Date of Patent:
February 3, 2015
Assignee:
Threshold Pharmaceuticals, Inc.
Inventors:
Stewart Kroll, Mark Matteucci, Charles P. Hart, Jian-Xin Duan, Karen Curd
Abstract: Compounds of Formula I: wherein X, Y, Z, R1, R2, R3, R4 are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other psychiatric, neurodegenerative and/or neurological disorders in mammals, including humans.
Type:
Grant
Filed:
October 31, 2013
Date of Patent:
January 13, 2015
Assignee:
Pfizer Inc.
Inventors:
Amy Beth Dounay, Laura Ann McAllister, Vinod Dipak Parikh, Suobao Rong, Patrick Robert Verhoest
Abstract: The present invention relates to substituted aromatic compounds of Formula I and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds in the prevention and/or treatment of various diseases and conditions in subjects, including the prevention or treatment of (i) blood disorders, (ii) renal disorders, a nephropathies, or renal disorder complications; (iii) inflammatory-related diseases; and/or (iv) oxidative stress related disorders.
Abstract: The invention provides a method of inhibiting the effects of platelet activating factor (PAF). For instance, a disease or condition mediated by PAF (particularly inflammation) can be treated or platelet aggregation can be inhibited. The invention also provides a method of inhibiting the production and/or release of interleukin 8 (IL-8) by cells. The effects of PAF and the production and/or release of IL-8 are inhibited according to the invention by a compound of the formula: wherein R1 and R2 are defined in the application, or a physiologically-acceptable salt thereof. The invention also provides pharmaceutical compositions comprising these compounds.
Type:
Grant
Filed:
August 28, 2013
Date of Patent:
December 23, 2014
Assignee:
Ampio Pharmaceuticals, Inc.
Inventors:
David Bar-Or, C. Gerald Curtis, Nagaraja K. R. Rao, Greg Thomas
Abstract: Improved methods and compositions for safe and effective treatment of telangiectasia or a symptom associated with telangiectasia in a subject are described. The methods involve topically applying to an affected skin area a topical composition comprising about 0.3% to about 10% by weight of brimonidine and a pharmaceutically acceptable carrier.
Type:
Grant
Filed:
March 25, 2011
Date of Patent:
December 23, 2014
Assignee:
Galderma Research & Development SNC
Inventors:
Michael Graeber, Christian Loesche, Philip Freidenreich, Yin Liu, Matthew James Leoni
Abstract: Compounds are provided that act as potent antagonists of the CCR(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR(9). The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR(9)-mediated diseases, and as controls in assays for the identification of CCR(9) antagonists.
Type:
Grant
Filed:
February 28, 2013
Date of Patent:
December 23, 2014
Assignee:
ChemoCentryx, Inc.
Inventors:
Xi Chen, Junfa Fan, Pingchen Fan, Antoni Krasinski, Lianfa Li, Rebecca M. Lui, Jeffrey P. McMahon, Jay P. Powers, Yibin Zeng, Penglie Zhang
Abstract: This invention is directed to a method of treating Excessive daytime Sleepiness (EDS) in a subject, comprising the step of administering a therapeutically effective amount of a compound of Formula (I): Formula (I) or a pharmaceutically acceptable salt or ester thereof wherein Rx is a member selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, Cl, Br and I, alkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, trifluoromethyl, and thioalkoxy containing 1 to 3 carbon atoms; x is an integer of 1 to 3, with the proviso that R may be the same or different when x is 2 or 3; R1 and R2 can be the same or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, arylalkyl, cycloalkyl of 3 to 7 carbon atoms; R1 and R2 can be joined to form a 5 to 7-membered heterocycle substituted with a member selected from the group consisting of hydrogen, alkyl, and aryl groups, wherein the cyclic
Type:
Grant
Filed:
January 23, 2013
Date of Patent:
November 4, 2014
Assignee:
SK Biopharmaceuticals Co., Ltd.
Inventors:
Abdallah Ahnaou, Wilhelmus H. I. M. Drinkenburg, Joseph Palumbo, Jonathan Sporn
Abstract: Melanocortin receptor modulators, processes for preparing them and use thereof in human medicine and cosmetics are described. Melanocortin receptor modulators corresponding to formula (I): compositions containing them, processes for their preparation and their use in pharmaceutical or cosmetic compositions are also described.
Abstract: Disclosed are formulations of gamma-hydroxybutyrate in an aqueous medium that are resistant to microbial growth. Also disclosed are formulations of gamma-hydroxybutyrate that are also resistant to the conversion into GBL. Disclosed are methods to treat sleep disorders, including narcolepsy, with these stable formulations of GHB. The present invention also provides methods to treat alcohol and opiate withdrawal, reduced levels of growth hormone, increased intracranial pressure, and physical pain in a patient.
Type:
Grant
Filed:
November 26, 2012
Date of Patent:
October 14, 2014
Assignee:
Jazz Pharmaceuticals, Inc.
Inventors:
Harry Cook, Martha Hamilton, Douglas Danielson, Colette Goderstad, Dayton T. Reardan
Abstract: The invention provides a method of inhibiting the effects of platelet activating factor (PAF). For instance, a disease or condition mediated by PAF (particularly inflammation) can be treated or platelet aggregation can be inhibited. The invention also provides a method of inhibiting the production and/or release of interleukin 8 (IL-8) by cells. The effects of PAF and the production and/or release of IL-8 are inhibited according to the invention by a compound of the formula: wherein R1 and R2 are defined in the application, or a physiologically-acceptable salt thereof. The invention also provides pharmaceutical compositions comprising these compounds.
Type:
Grant
Filed:
October 4, 2011
Date of Patent:
September 23, 2014
Assignee:
Ampio Pharmaceuticals, Inc.
Inventors:
David Bar-Or, C. Gerald Curtis, Nagaraja K. R. Rao, Greg Thomas
Abstract: The invention relates to a solid oral dosage form comprising a pharmaceutically active ingredient in combination with an enhancer which enhances the bioavailability and/or the absorption of the active ingredient. Accordingly, a solid oral dosage form comprises a drug and an enhancer wherein the enhancer is a medium chain fatty acid ester, ether or salt or a derivative of a medium chain fatty acid, which is, preferably, solid at room temperature and which has a carbon chain length of from 6 to 20 carbon atoms. Preferably, the solid oral dosage form is controlled release dosage form such as a delayed release dosage form.
Abstract: Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula I or a pharmaceutically acceptable salt thereof. In Formula I m is 0, 1, 2, 3 or 4; n is 0 or 1; t is 0 or 1; q is 0 or 1; and r is 0, 1 or 2. R6 is hydrogen, O or hydroxyl. R7 is hydrogen or alkyl having from 1 to 3 carbon atoms. One of R8 and R9 is alkyl having from 1 to 3 carbon atoms, and the other is hydrogen or alkyl having from 1 to 3 carbon atoms. R10 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms or alkoxy having from 1 to 3 carbon atoms. X is C(O) and r is 0 and t is 0; or X is NH(R11) wherein R11 is hydrogen or alkyl having from 1 to 3 carbon atoms.
Type:
Grant
Filed:
March 13, 2009
Date of Patent:
September 9, 2014
Assignee:
Wellstat Therapeutics Corporation
Inventors:
James Dennen O'Neil, Michael K. Bamat, Reid W. von Borstel, Shalini Sharma, Ramachandran Arudchandran
Abstract: The present invention includes novel compound and methods of treating a disease or disorder by antagonizing Bcl-2 family proteins, particularly compounds of formula (I): or pharmaceutically acceptable salt thereof, as well as methods of treating a disease, disorder, or syndrome associated with Bcl-2 inhibition, particularly hyperproliferative diseases. The present invention also includes pharmaceutical compositions including compounds of formula I and pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
September 8, 2010
Date of Patent:
August 19, 2014
Assignee:
Novartis AG
Inventors:
Karen Miller-Moslin, Bakary-Barry Toure, Michael Scott Visser, Naeem Yusuff
Abstract: The invention relates to a microbicidal use solution which comprises a) one or more isothiazolin-3-ones and b) one or two organic amines selected from N-dodecylpropane-1,3-diamine and bis(aminopropyl)-dodecylamine and optionally c) one or more oxidizing agents. The use solution is preferably in the form of technical and domestic products.
Type:
Grant
Filed:
September 22, 2010
Date of Patent:
July 1, 2014
Assignee:
L'Air Liquide, Societe Anonyme pour l'Etude et l'Exploitation des Procedes Georges Claude
Inventors:
Wolfgang Beilfuss, Ralf Gradtke, Ingo Krull, Jennifer Knopf
Abstract: The present invention relates to injectable compositions comprising biocompatible, swellable, substantially hydrophilic, non-toxic and substantially spherical polymeric material carriers which are capable of efficiently delivering bioactive therapeutic factor(s) for use in embolization drug therapy. The present invention further relates to methods of embolization gene therapy, particularly for the treatment of angiogenic and non-angiogenic-dependent diseases, using the injectable compositions.
Abstract: An object of the present invention is to provide a medicinal composition useful for external application in the treatment of a fungal infection reaching the lower part of a thick keratin layer. Provided is an antifungal medicinal composition, comprising: (1) a film-forming agent; (2) a water-soluble plasticizer in a form of a solid or a paste at 20° C. at 1 atm; and (3) an antifungal compound represented by a general formula (1) and/or a physiologically acceptable salt thereof.