Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein ring A, B1, B2, B3, L, R1, R2, ring Z, m and n of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula (I), intermediates and processes useful for the preparation of compounds of Formula (I).
Type:
Grant
Filed:
January 14, 2011
Date of Patent:
May 27, 2014
Assignee:
Amgen Inc.
Inventors:
Nick A. Paras, James Brown, Yuan Cheng, Stephen A. Hitchcock, Ted Judd, Patricia Lopez, Ana Elena Minatti, Thomas Nixey, Timothy Powers, Christopher M. Tegley, Qiufen Xue, Bryant Yang, Wenge Zhong
Abstract: Nitrate esters and diazeniumdiolate derivatives of valsartanamide are described. They have valuable properties in the treatment of vascular and metabolic diseases.
Abstract: The invention relates to a compound of formula (I) wherein A and R1 to R7 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
Type:
Grant
Filed:
November 20, 2012
Date of Patent:
May 20, 2014
Assignee:
Hoffmann-La Roche Inc.
Inventors:
David Banner, Wolfgang Haap, Bernd Kuhn, Thomas Luebbers, Jens-Uwe Peters, Tanja Schulz-Gasch
Abstract: Embodiments of the present disclosure include methods for identifying a compound or compounds useful as therapeutic agents in the treatment of paramyxovirus infections, compounds for the treatment of measles, and high throughput screening methods for identifying compounds capable of inhibiting the proliferation of a paramyxovirus.
Type:
Grant
Filed:
February 11, 2008
Date of Patent:
May 20, 2014
Assignee:
Emory University
Inventors:
Richard K. Plemper, James P. Snyder, Aiming Sun
Abstract: The present invention includes new salts of Raltegravir and crystalline forms thereof, pharmaceutical compositions containing the salts or crystalline forms, methods of using the salts or crystalline forms or the compositions to treat HIV infection or to prepare medicament for treating HIV infection, and a process for preparing Raltegravir potassium.
Type:
Grant
Filed:
December 7, 2012
Date of Patent:
May 13, 2014
Assignee:
Teva Pharmaceutical Industries Ltd
Inventors:
Ana Kwokal, Lilach Hedvati, Revital Burstein, Adi Yeori, Rinat Moshkovits-Kaptsan
Abstract: The subject matter of the invention is quinazolinedione derivatives of formula (I), methods for obtaining same and therapeutic uses thereof, such as cancer, diabetes, muscle diseases, bone diseases, cardiovascular diseases, central nervous system diseases, peripheral nervous system diseases, inter alia.
Abstract: The present invention provides (1aR,12bS)-8-cyclohexyl-11-fluoro-N-((1 -methylcyclopropyl)sulfonyl)-1a-((3-methyl-3,8-diazabicyclo[3.2.1]oct-8-yl) carbonyl)-1,1a,2,12b-tetrahydrocyclopropa[d]indolo[2,1-a][2]benzazepine-5-carboxamide (formula I), including pharmaceutically acceptable salts, as well as compositions and methods of using the compound. The compound has activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
Type:
Grant
Filed:
October 15, 2012
Date of Patent:
May 6, 2014
Assignee:
Bristol-Myers Squibb Company
Inventors:
Zhizhen Barbara Zheng, Stanley D'Andrea
Abstract: The invention discloses a compound of formula (I) wherein, at least one of R1, R2, R3 and R4 is —C(?O)Rn and R1, R2R3 and R4 are H or CH3 and Rn is alkyl or alkenyl group. The alkenyl group have one or more number of double bonds either in cis form or trans form or both. In Rn, where n is 12 to 30 carbons; and pharmaceutically acceptable salt thereof. The said alkenyl groups are preferably selected from the group consisting of eicosapentaenoic acid (EPA) or DHA (docosahexaenoic acid). This invention further discloses processes for their preparation of compounds of formula I and pharmaceutical compositions that contain these compounds.
Abstract: The invention provides crystalline hydrochloride salts of (S)-3-[(S)-2-methanesulfonyl-1-(4-trifluoromethylphenoxy)ethyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salts, processes and intermediates for preparing the crystalline salts, and methods of using the crystalline salts to treat diseases.
Type:
Grant
Filed:
September 28, 2012
Date of Patent:
February 25, 2014
Assignee:
Theravance, Inc.
Inventors:
Pierre-Jean Colson, Timothy Fass, Venkat R. Thalladi
Abstract: The present invention provides a compound useful as an agent for the prophylaxis or treatment of neurodegenerative disease and the like, or a salt thereof. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
Type:
Grant
Filed:
October 3, 2012
Date of Patent:
February 11, 2014
Assignee:
Takeda Pharmaceutical Company Limited
Inventors:
Tatsuki Koike, Masato Yoshikawa, Haruhi Ando, William John Farnaby
Abstract: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt or a solvate thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
Type:
Grant
Filed:
December 3, 2009
Date of Patent:
February 4, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Hidemitsu Nishida, Fumihiko Saitoh, Tomokazu Hirabayashi, Samuel Chackalamannil, Tin-Yau Chan, Mariappan V. Chelliah, Martin C. Clasby, Michael Dwyer, William J. Greenlee, Yan Xia
Abstract: Azido-diarylpyrimidine (azido-DAPY) compounds, and compositions containing such compounds, are provided. In addition, methods of using azido-diarylpyrimidines to inactivate reverse transcriptases, prepare inactivated viruses, and treat or prevent viral infections are also provided.
Abstract: A 4?-demethylepipodophyllotoxin derivative of formula(III) having anti-tumor activity is provided. After the activation of hydroxyl in position C4 of 4?-demethylepipodophyllotoxin, tetramethylpyrazine is introduced by transamination to obtain the 4?-demethylepipodophyllotoxin derivative which is preferably used to inhibit gastric cancer line BGC-823.
Abstract: Compounds represented by general formula (I) (all of the symbols in the formula conform to the definitions in the Description) are compounds that, in addition to having a Btk-selective inhibitory activity, exhibit an excellent metabolic stability and can avoid hepatotoxicity or the like, and as a consequence can provide safe therapeutic agents for diseases in which B cells or mast cells participate.
Abstract: A composition for stimulating NKT cells to produce anti-cancer and anti-viral cytokines without causing anergy of NKT cells includes a glycolipid antigen and a nanoparticle conjugated with the glycolipid antigen. The glycolipid antigen and the nanoparticle are not antigenic in mouse and human being. The composition can further include covalent or non-covalent connection between the glycolipid antigen and the nanoparticle. The glycolipid antigen is alpha-galactosylceramide or an analog of that. The nanoparticle can be a polymer. A production method of the composition includes preparing a nanoparticle and a glycolipid antigen and loading the glycolipid antigen to the nanoparticle. The glycolipid antigen can be coated onto the surface of the nanoparticle or encapsulated within the nanoparticle. A method of stimulating NKT cells to produce anti-cancer and anti-viral cytokines without causing anergy of NKT cells is also provided.
Type:
Grant
Filed:
July 22, 2011
Date of Patent:
October 1, 2013
Assignee:
Board of Regents, The University of Texas System
Abstract: Provided herein is a method for chemically programmed vaccination. Methods include inducing a covalent-binding polyclonal antibody response in a subject and programming the polyclonal response with a targeting compound.
Abstract: Screening methods for identifying compounds and compounds and pharmaceutical compositions for treating and preventing cancer are disclosed. The compounds affect signal transduction downstream of the MET receptor.
Abstract: The present invention relates to purified 3-methanesulfonylpropionitrile or a pharmaceutically acceptable salt thereof, and a method for preparing such compound. The compound has at least 90% (w/w) purity. The present invention is also directed to a pharmaceutical composition comprises the purified compound and a pharmaceutically acceptable carrier. The present invention is further directed to a method for treating inflammation, inflammatory-related disorders, or pain, by administering 3-methanesulfonylpropionitrile or a pharmaceutically acceptable salt or solvate thereof to a subject in need thereof.
Abstract: The present invention relates to the use of masitinib or a pharmaceutically acceptable salt thereof, and in particular of masitinib mesylate, for the preparation of a medicament for the treatment of GIST, to the use of this therapy for the treatment of GIST, and a method of treating mammals, including humans, suffering from GIST by administering to said mammal in need of such treatment an effective dose of masitinib, and in particular masitinib mesylate.
Type:
Grant
Filed:
January 28, 2011
Date of Patent:
May 28, 2013
Assignee:
AB Science
Inventors:
Marco Ciufolini, Camille Wermuth, Bruno Giethlen, Alain Moussy, Jean-Pierre Kinet
Abstract: The present invention is directed to compounds which are conjugates of two non-toxic natural products, noscapine (and various noscapine analogs) and folic acid (and various folic acid analogs), where the folic acid is conjugated to noscapine or the noscapine analog at the 9-position on the isoquinoline ring on the noscapine framework. Pharmaceutical compositions including the compounds, and methods of treating various tumors using the compounds and compositions, are also disclosed. The conjugates are particularly useful for treating cancers which overexpress the Folate Receptor ? (FRa) receptor.
Type:
Grant
Filed:
January 8, 2010
Date of Patent:
April 23, 2013
Assignee:
Emory University
Inventors:
Harish C. Joshi, Surya N. Vangapandu, Ritu Aneja