Abstract: The present invention relates to novel compounds of formula (II) that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating, or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.
Type:
Grant
Filed:
July 25, 2012
Date of Patent:
March 18, 2014
Assignee:
AC Immune SA
Inventors:
Wolfgang Froestl, Nampally Sreenivasachary, Sophie Lohmann, Maria Pilar Lopez Deber, Andreas Muhs, Maria Pihlgren Bosch
Abstract: A method of inhibiting blood platelet aggregation in a mammal is provided. The method comprises the administration of a platelet aggregation inhibiting amount of a modified amino acid or pharmaceutically acceptable salt thereof.
Abstract: This invention pertains generally to processes, uses, methods and materials utilizing particular xanthylium compounds, including compounds of formula (I) and (II), as further defined herein. These compounds are useful as drugs, for example, in the treatment of tauopathies, such as Alzheimer's disease.
Type:
Grant
Filed:
December 10, 2009
Date of Patent:
February 25, 2014
Assignee:
WisTa Laboratories Ltd.
Inventors:
Scott Clunas, John Mervyn David Storey, Janet Elizabeth Rickard, David Horsley, Charles Robert Harrington, Claude Michel Wischik
Abstract: The present invention relates to calcium salts of compounds of the general formula (I) wherein X is selected from the group consisting of CH2, S, or O; D is O or S; R8 is hydrogen or alkyl; E is an optionally substituted phenylene group; Y is a monocyclic or bicyclic substituted or unsubstituted 6-9 membered ring system which may contain one or more heteroatoms selected from N or S and which contains at least one aromatic ring; n is 0 or 1, and q is 0 or 1; with the proviso that compounds wherein X?CH2, q=0, Y=unsubstituted phenyl and E=unsubstituted phenylene are excluded; or a hydrate thereof.
Type:
Grant
Filed:
July 1, 2011
Date of Patent:
February 18, 2014
Assignee:
4SC MG
Inventors:
Aldo Ammendola, Julia Diederichs, Johann Leban, Daniel Vitt
Abstract: The present invention is directed to substituted six-membered heterocyclic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as obesity and diabetes, particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.
Type:
Grant
Filed:
August 18, 2008
Date of Patent:
February 18, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Tesfaye Biftu, Danqing Feng, Ann E. Weber, Jason M. Cox, Xiaoxia Qian, Jinyou Xu
Abstract: This invention relates to novel acetylcysteine compositions in solution, comprising acetylcysteine and which are substantially free of metal chelating agents, such as EDTA. Further, this invention relates to methods of making and using the acetylcysteine compositions. The present compositions and methods are designed to improve patient tolerance and compliance, while at the same time maintaining the stability of the pharmaceutical formulation. The compositions and methods of this invention are useful in the treatment of acetaminophen overdose, acute liver failure, various cancers, methacrylonitrile poisoning, reperfusion injury during cardio bypass surgery, and radiocontrast-induced nephropathy, and can also be used as a mucolytic agent.
Abstract: The use of polyunsaturated fatty acids of the ?-3 series such as eicosapentaenoic acid (EPA, C20:5 ?-3), docosahexaenoic acid (DHA, C22:6 ?-3), or their pharmaceutically acceptable derivatives is described for the primary prevention of major cardiovascular events in subjects who have not undergone previous infarct episodes.
Type:
Grant
Filed:
September 29, 2009
Date of Patent:
February 11, 2014
Assignee:
Pro Aparts Investimentos E. Consultoria LDA.
Abstract: Described herein is a method for increasing levels of S-adenosylmethionine within the human body without administering S-adenosylmethionine directly. The method of the invention may be achieved by administering one or more of L-methionine, methylcobalamin, 5-Methyl tetrahydrofolate, betaine, and malic acid, together with at least one compound selected from the group consisting of folic acid, vitamin B12, magnesium, calcium, and other cofactors.
Abstract: Pharmaceutical formulations and methods for the topical or transdermal delivery of 1isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine or 1-(2-methylpropyl)-1H-imidazo[4,5 c]quinolin-4-amine, i.e., imiquimod, to treat genital/perianal warts with shorter durations of therapy than currently prescribed for the commercially available for Aldara® 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating genital/perianal warts with an acceptable safety profile and dosing regimens that are shorter and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for Aldara® 5% imiquimod cream to treat genital/perianal warts are also disclosed and described.
Type:
Grant
Filed:
July 26, 2012
Date of Patent:
February 4, 2014
Assignee:
Medicis Pharmaceutical Corporation
Inventors:
Michael T. Nordsiek, Jefferson J. Gregory
Abstract: Herein are described compounds having a structure or a pharmaceutically acceptable salt thereof, wherein Y, A, and B are as described. Methods, compositions, and medicaments related thereto are also disclosed.
Abstract: This invention relates to the use of pterosin compounds of formula I for treating diabetes including type I and type II. Also disclosed is the use of the pterosin compounds for treating obesity.
Type:
Grant
Filed:
January 26, 2010
Date of Patent:
January 21, 2014
Assignees:
Taipei Medical University, National Taiwan University, National Tsing Hua University, DCB-USA LLC
Inventors:
Feng-Lin Hsu, Shing-Hwa Liu, Biing-Jiun Uang
Abstract: The present disclosure relates to a combination of therapeutic agents for use in treating a patient a subject suffering from cancer. In addition, the present disclosure also relates to diagnostic assays useful in classification of patients for treatment with one or more therapeutic agents.
Type:
Grant
Filed:
December 4, 2009
Date of Patent:
January 7, 2014
Assignee:
AbbVie Inc.
Inventors:
Omar Jameel Shah, Yu Shen, Xiaoyu Lin, Mark Anderson, Xiaoli Huang, Junling Li, Leiming Li
Abstract: A compound of formula (I), wherein A1, A2, A3, A4, G1, L, R1, R2, R3, R4, Y1, Y2 and Y3 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.
Type:
Grant
Filed:
December 16, 2008
Date of Patent:
January 7, 2014
Assignee:
Syngenta Crop Protection, LLC
Inventors:
Peter Renold, Werner Zambach, Peter Maienfisch, Michel Muehlebach
Abstract: A pharmaceutical composition and methods of producing and application of the composition for treating myocardial infarction of a subject are disclosed. The pharmaceutical composition comprises a therapeutically effective amount of at least one synthesized compound selected from the group consisting of SEC, SPC, SBC, SPEC, SAC, SAMC, and SPRC, and a pharmaceutically acceptable carrier.
Type:
Grant
Filed:
August 1, 2008
Date of Patent:
January 7, 2014
Assignee:
Fudan University
Inventors:
Yizhun Zhu, Qian Wang, Yichun Zhu, Qing Mu
Abstract: The present invention is related to novel compounds of formula (I) having antibacterial activity against Clostridium bacteria, in particular Clostridium perfringens, pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
Type:
Grant
Filed:
August 4, 2011
Date of Patent:
December 31, 2013
Assignee:
Elanco Animal Health Ireland Limited
Inventors:
Jerome Emile Georges Guillemont, Pierre Jean-Marie Bernard Raboisson, Nacer Lounis
Abstract: In certain embodiments, the invention is directed to composition comprising stable particles comprising ganaxolone, wherein the volume weighted median diameter (D50) of the particles is from about 50 nm to about 500 nm.
Abstract: The present invention discloses methods of modulating the activity of Group I mGluRs using a defined class of benzamide compounds. In one embodiment, methods of modulating the activity of mGluR1 are provided. In another embodiment, methods of modulating the activity of mGluR5 are provided. In still another embodiment, methods of simultaneously modulating the activities of both mGluR1 and mGluR5 are provided. The present invention also provides methods of treating diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of benzamide compounds. The present invention further provides methods of preventing diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of compounds.
Abstract: The present invention relates to compounds of Formula (Ia) or (Ib), the N-oxide forms, pharmaceutically acceptable addition salts, quaternary amines, stereoisomers, tautomers, racemics, metabolites, prodrugs, hydrates, or solvates thereof, wherein Y1, m, n, R1; X1; X2; R2; X3; X4; R3; and R4 have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to compounds that are kinase inhibitors useful for the treatment of disease states mediated by kinase, especially PLK4, in particular such compounds that are useful in the treatment of pathological processes which involve an aberrant cellular proliferation, such as tumor growth, rheumatoid arthritis, restenosis and atherosclerosis.
Type:
Grant
Filed:
October 16, 2012
Date of Patent:
December 17, 2013
Assignee:
Janssen Pharmaceutica NV
Inventors:
Peter Jacobus Johannes Buijnsters, Marc Gustaaf Celine Verdonck, Pascal Ghislain André Bonnet, Kristof Van Emelen
Abstract: Combinations of PI3K inhibitor compounds having Formulas I and II and chemotherapeutic agents, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for treating hyperproliferative disorders such as cancer. Methods of using such combinations for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
Type:
Grant
Filed:
May 17, 2011
Date of Patent:
December 10, 2013
Assignees:
Genentech, Inc., F. Hoffmann-La Roche AG
Inventors:
Marcia Belvin, Lori Friedman, Klaus Hoeflich, Deepak Sampath, Ulka Vijapurkar, Jeffrey Wallin, Leisa Johnson, Mallika Singh, Sonal Patel