Abstract: The present invention relates to (S)-proline sulfonamide compounds of formula (I) wherein R1 and R2 are as described in the description, or pharmaceutically acceptable salts thereof, for use in the prevention or treatment of diseases or disorders related to the orexin system. The present invention also relates to the use of (S)-proline sulfonamide compounds of formula (II) as pharmaceuticals, to pharmaceutical compositions comprising compounds of formula (II), and especially their use in the prevention or treatment of diseases or disorders related to the orexin system.
Type:
Grant
Filed:
October 31, 2014
Date of Patent:
April 7, 2015
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Christoph Boss, Christine Brotschi, John Gatfield, Markus Gude, Bibia Heidmann, Thierry Sifferlen, Jodi T. Williams
Abstract: Compounds of the formula (I) in which R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed treatment of tumours.
Type:
Grant
Filed:
May 29, 2012
Date of Patent:
March 31, 2015
Assignee:
Merck Patent GmbH
Inventors:
Timo Heinrich, Margarita Wucherer-Plietker, Hans-Peter Buchstaller
Abstract: The invention relates generally to effective treatment leukemia. In particular, the present invention provides compositions and methods to inhibit the interaction of menin with MLL and MLL-fusion oncoproteins, and well as systems and methods to screen for such compositions.
Type:
Grant
Filed:
September 3, 2010
Date of Patent:
March 31, 2015
Assignees:
The Regents of The University of Michigan, University of Virginia Patent Foundation
Inventors:
Jolanta Grembecka, Tomasz Cierpicki, Jay Hess
Abstract: A pharmaceutical composition containing one or more antifungal agents selected from an arylamidine derivative represented by the general formula: (wherein R1 represents an amidino group that may be substituted with a hydroxyl group that may be protected with an acyl group, an amidino group that may be substituted with an alkoxy group that may be substituted, or an amidino group that may be substituted with an aralkyloxy group that may be substituted; R2 and R3 identically or differently represent a hydrogen atom or a halogen atom) or a salt thereof, an azole antifungal agent, a polyene antifungal agent, a candin antifungal agent and a fluoropyrimidine antifungal agent has a strong antifungal activity and is useful for the treatment of fungal infection. A method for using them in combination is useful as an excellent therapeutic method for fungal infection.
Abstract: The invention relates to the use of calixarenes for preventing or limiting the transfer of an actinide in the body from a site of skin contamination.
Type:
Grant
Filed:
December 17, 2009
Date of Patent:
March 24, 2015
Assignee:
Institut de Radioprotection et de Surete Nucleaire
Inventors:
Aurélie Spagnul, François Rebiere, Guillaume Phan, Céline Bouvier-Capely, Elias Fattal
Abstract: Disclosed are complexes of an antipneumocystic compound and an antimalarial compound, processes for their preparation, pharmaceutical compositions and methods of using said complexes or compositions for the treatment and/or prophylaxis of parasitic infections.
Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.
Type:
Grant
Filed:
April 19, 2013
Date of Patent:
March 24, 2015
Assignee:
Gilead Sciences, Inc.
Inventors:
Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
Abstract: Compounds of the general formula (I) wherein each of m and n is independently 0 or 1; R1 and R2, together with the carbon atom to which they are attached, form a heterocyclic ring comprising one or two heteroatoms selected from oxygen, sulfur, —S(O)— and —S(O)2—; R3 is —CHF2, —CF3, —OCHF2, —OCF3, —SCHF2 or —SCF3; X is a bond, —CH2—, or —NH—; A is aryl, cycloalkyl, cycloalkenyl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkenyl, optionally substituted with one or more, same or different substituents selected from R4; and R4 is hydrogen, amino, thioxo, alkyl, haloalkyl, hydroxyalkyl, alkoxy, haloalkoxy, halogen, oxo, thia, or hydroxy; or pharmaceutically acceptable salts, hydrates or solvates thereof, have been found to exhibit PDE4 inhibiting activity, and may therefore be useful in the treatment of inflammatory diseases and disorders.
Abstract: Disclosed are 2-arylimidazo[1,2-a]pyridine-3-acetamide derivatives represented by formula I, their tautomer, racemate or optical isomer, their pharmaceutically acceptable salt, or their solvates, wherein R1, R2, R3 and R4 are defined as in the specification.
Type:
Grant
Filed:
June 9, 2011
Date of Patent:
March 17, 2015
Assignees:
Institute of Pharmacology, Toxicology Academy of Military Medical Sciences P.L.A., China
Abstract: Provided herein are methods of treating hemolysis by administering an active compound in an amount sufficient to treat said hemolysis. It has been found that nitroxyl donors or similar compounds preferentially react with cell-free OxyHb, as compared to OxyHb encapsulated in a red blood cell, and reacts with MetHb to form iron-nitrosyl Hb or nitrite bound MetHb. It has also been found that such compounds reduce cell-free Hb and hemolysis. Active compounds are also contemplated for use in combination therapies, for example, in combination with the administration of red blood cells and/or an agent that promotes hematopoiesis, or in combination with the administration of a nitric oxide donor.
Type:
Grant
Filed:
September 19, 2008
Date of Patent:
March 17, 2015
Assignees:
Wake Forest University Health Sciences, The United States of America, as represented by the Secretary, Department of Health and Human Services
Inventors:
Daniel B. Kim-Shapiro, S. Bruce King, Daniel A. Sweeney, Mark T. Gladwin
Abstract: Replication protein A (RPA) is a single-strand DNA-binding protein with essential roles in DNA replication, recombination and repair. Small molecule inhibitors (SMIs) with the ability to disrupt RPA binding activity to ssDNA have been identified and assessed using both lung and ovarian cancer cell lines. Lung cancer cell lines demonstrated increased apoptotic cell death following treatment with the SMI MCI13E, with IC50 values of ˜5 ?M. The A2780 ovarian cancer cell line and the p53-null lung cancer cell line HI 299 were particularly sensitive to MCI13E treatment with IC50 values below 3 ?M. Sequential treatment with MCI13E and cisplatin resulted in synergism, suggesting that decreasing RPA's DNA binding activity via a SMI may disrupt RPA's role in cell cycle regulation. Thus, RPA SMIs hold the potential to be used as single agent chemotherapeutics or in combination with current chemotherapeutic regimens to increase their efficacy.
Type:
Grant
Filed:
September 19, 2011
Date of Patent:
March 17, 2015
Assignee:
Indiana University Research and Technology
Abstract: The present invention relates to a method for controlling arthropods comprising the application of an aqueous gel which contains an insecticide, an attractant and a thickener, wherein the aqueous gel is applied in the form of spots on fruit trees. The invention further relates to an aqueous gel comprising an insecticide, an attractant, a thickener, a humectant and a feeding stimulant. The invention also relates to a concentrated gel for preparing the aqueous gel.
Type:
Grant
Filed:
January 21, 2011
Date of Patent:
March 10, 2015
Assignee:
BASF SE
Inventors:
Claude Taranta, Tatjana Levy, Ouidad Benlahmar, Marc Nolte, Thomas Kröhl, Christoph Randt, Thomas Bork, Wolfgang Meier, Clark D. Klein, Tiffany Hennessey
Abstract: Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control. The compounds of the invention are orally active.
Type:
Grant
Filed:
September 12, 2012
Date of Patent:
March 10, 2015
Assignee:
Cymabay Therapeutics, Inc.
Inventors:
Xin Chen, Peng Cheng, L. Edward Clemens, Jeffrey D. Johnson, Jingyuan Ma, Alison Murphy, Imad Nashashibi, Christopher J. Rabbat, Jiangao Song, Maria E. Wilson, Yan Zhu, Zuchun Zhao
Abstract: PAD4 inhibitory compositions and methods for their use in treatment of cancer and autoimmune disease are provided according to embodiments of the present invention.
Type:
Grant
Filed:
April 25, 2014
Date of Patent:
March 3, 2015
Assignee:
The Penn State Research Foundation
Inventors:
Gong Chen, Yanming Wang, Pingxin Li, Jing Hu, Shu Wang, Yuji Wang
Abstract: The present invention relates to substituted benzosulphonamide compounds of general formula (I): in which R1, R2, R3, R4, R5 and A are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
Type:
Grant
Filed:
October 7, 2010
Date of Patent:
February 24, 2015
Assignee:
Bayer Intellectual Property GmbH
Inventors:
Marion Hitchcock, Ingo Hartung, Florian Pühler
Abstract: An effective dose of a pharmaceutically acceptable phenylbutyrate salt such as sodium phenylbutyrate applied to human ocular tissues or through injection or other means prevents ocular hypertension and treats glaucoma in humans, leading to a new medical therapy for lowering the intraocular pressure via a mechanism different from the existing glaucoma medications. This compound can be formulated in combination with topical or other forms of steroids in prevention and treatment of steroid induced ocular hypertension and glaucoma.
Type:
Grant
Filed:
April 21, 2011
Date of Patent:
February 24, 2015
Assignee:
The Chinese University of Hong Kong
Inventors:
Dennis Shun Chiu Lam, Johnson Yiu Nam Lau, Gary Hin Fai Yam, Chi Pui Pang, Christopher Kai Shun Leung, Haoyu Chen, Srinivas Kamalakara Rao, Dorothy Shu Ping Fan
Abstract: A class of anionic oligomers and polymers that function for inhibition of nucleases, particularly RNase. Specific inhibitors include mixtures of oligomers of vinyl sulfate. Methods for inhibition or inactivation of one or more nucleases in vitro which comprises the step of contacting the one or more nucleases in a biological medium with one or more of the anionic oligomeric or polymeric inhibitors of this invention. Kits for carrying out a biological procedure, biological reaction and/or a biological assay containing one or more inhibitors of this invention. The use of oligomers and/or polymers of this invention as additives in buffers or reagents. The inhibitors of the invention can also be attached to surfaces to provide for removal of nucleases from media, solutions or other liquids in contact with the solid.
Type:
Grant
Filed:
June 10, 2013
Date of Patent:
February 24, 2015
Assignee:
Wisconsin Alumni Research Foundation
Inventors:
Ronald T. Raines, Bryan D. Smith, Matthew B. Soellner, David M. Lynn
Abstract: Compounds of formula (I), and salts, N-oxides, hydrates and solvates thereof are histone deacetylase inhibitors and are useful in the treatment of cell proliferative diseases, including cancers: wherein Q, V and W independently represent —N? or —C?; B is a divalent radical selected from (B1), (B2), (B3), (B4), (B5) and (B6). wherein the bond marked * is linked to the ring containing Q, V and W through -[Linker1]- and the bond marked ** is linked to A through -[Linker2]-; A is an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system; -[Linker1]- and -[Linker2]- independently represent a bond, or a divalent linker radical; and R is (a) a radical of formula R1R2CHNH—Y-L1-X1—(CH2)z— or (b) a radical of formula R-L1-Y1—(CH2)z—.
Type:
Grant
Filed:
October 30, 2006
Date of Patent:
February 24, 2015
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Inventors:
David Charles Festus Moffat, Sanjay Ratilal Patel, Francesca Ann Day, Andrew James Belfield, Alistair David Graham Donald, Alan Hornsby Davidson, Alan Hastings Drummond
Abstract: The invention relates to the use of a chemical substance selected from the group consisting of N-?2-hydroxy-3-(1-piperidinyl)-propoxyl 1-pyridine-1-oxide-3-carboximidoyl chloride, the optically active enantiomers and the mixtures of enantiomers thereof and pharmaceutically acceptable salts of the racemic and optically active compounds in the preparation of a pharmaceutical composition for the treatment or prevention of neurodegenerative diseases.
Type:
Grant
Filed:
September 12, 2011
Date of Patent:
February 24, 2015
Assignee:
Orphazyme ApS
Inventors:
Linda Greensmith, Geoffrey Burnstock, Rudolf Urbanics
Abstract: The present invention provides substituted imidazopyridines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
Type:
Grant
Filed:
August 21, 2014
Date of Patent:
February 24, 2015
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Matthew P. Christopher, Francesc Xavier Fradera Llinas, Michelle Machacek, Michelle Martinez, Michael Hale Reutershan, Manami Shizuka, Binyuan Sun, Christopher Francis Thompson, B. Wesley Trotter, Matthew E. Voss, Michael D. Altman, Stephane L. Bogen, Ronald J. Doll