Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
Type:
Grant
Filed:
February 3, 2017
Date of Patent:
April 17, 2018
Assignee:
Gilead Sciences, Inc.
Inventors:
Steven S. Bondy, Carina E. Cannizzaro, Chien-Hung Chou, Randall L. Halcomb, Yunfeng Eric Hu, John O. Link, Qi Liu, Scott D. Schroeder, Winston C. Tse, Jennifer R. Zhang
Abstract: The present invention relates to the treatment or prevention of skeletal disorders, in particular skeletal diseases, developed by patients that display abnormal increased activation of the fibroblast growth factor receptor 3 (FGFR3), in particular by expression of a constitutively activated mutant of FGFR3.
Type:
Grant
Filed:
September 3, 2015
Date of Patent:
April 3, 2018
Assignees:
INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM), UNIVERSITE PARIS DESCARTES, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), ASSITANCE PUBLIQUE HOPITAUX DE PARIS, UNIVERSITE PARIS DIDEROT-PARIS 7, IMAGINE
Inventors:
Laurence Legeai-Mallet, Arnold Munnich, Patricia Busca, Florent Barbault
Abstract: The present invention relates to a ready-to-administer parenteral dosage form of norepinephrine which comprises an aqueous solution of norepinephrine, having an anti-oxidant which is not a sulfite anti-oxidant, wherein the dosage form is stable at room temperature for prolonged period of time.
Type:
Grant
Filed:
August 27, 2015
Date of Patent:
January 30, 2018
Assignee:
SUN PHARMACEUTICAL INDUSTRIES LIMITED
Inventors:
Thummar Rakesh, Pawar Shantaram, Kane Prashant, Bhowmick Subhas Balaram, Kumar Samarth, Thakkar Milan Natvarbhai, Dave Kandarp Maheshkumar
Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.
Type:
Grant
Filed:
December 7, 2015
Date of Patent:
December 19, 2017
Assignee:
ABBVIE INC.
Inventors:
Le Wang, George Doherty, Xilu Wang, Zhi-Fu Tao, Milan Bruncko, Aaron R. Kunzer, Michael D. Wendt, Xiaohong Song, Robin Frey, Todd M. Hansen, Gerard M. Sullivan, Andrew Judd, Andrew Souers
Abstract: A disinfecting shower cleaner composition including a medium-chain fatty acid coupled with a nonionic surfactant providing temperature stable antimicrobial compositions. The invention specifically relates to antimicrobial compositions including fatty acid antimicrobial agents coupled with an ethoxylated amine and methods of using the antimicrobial compositions.
Type:
Grant
Filed:
May 22, 2017
Date of Patent:
October 24, 2017
Assignee:
Ecolab USA Inc.
Inventors:
Elizabeth Kiesel, Michael Edward Besse, Lisa A. Hellickson, Mark Levitt, Daniel E. Pedersen
Abstract: This invention provides methods and compositions for modulating movement of eukaryotic cells with migratory capacity. More specifically, the invention provides anti-fugetactic agents and methods for the use thereof in enhancing an immune response.
Type:
Grant
Filed:
November 4, 2005
Date of Patent:
October 17, 2017
Assignee:
THE GENERAL HOSPITAL CORPORATION
Inventors:
Mark C. Poznansky, John T. Potts, Jr., Fabrizio Vianello, Natalia Papeta
Abstract: A compound suitable for treating cancer, in particular NSCLC, inhibits activity of oncogenic ROS1 kinase and ALK kinase. The compound has certain structural components such as a quinoline moiety in the backbone and at least one phenyl-containing moiety in a side chain with a hydrophobic substituent attached to the backbone via an up to 6-membered linking group as well as a further hydrophobic moiety. The presence of the structural components allows for an advantageous interaction with the ROS1 kinase domain and, further, with the ALK kinase domain. Hence, said compound represents a highly promising opportunity for patients bearing ROS1- or ALK-dependent cancer. A composition, in particular a pharmaceutical composition, includes the compound. A method for targeting cancer cells harboring an abnormality in ROS1 gene or ALK gene includes contacting a cell with the compound.
Type:
Grant
Filed:
December 2, 2015
Date of Patent:
October 10, 2017
Assignee:
Macau University of Science and Technology
Inventors:
Xiao Jun Yao, Lai Han Leung, Lian Xiang Luo, Liang Liu
Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, wherein the variables R1, R2, R3, R4 and X are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
Type:
Grant
Filed:
September 22, 2016
Date of Patent:
September 26, 2017
Assignee:
PFIZER INC.
Inventors:
Michael Aaron Brodney, Christopher Ryan Butler, Lei Zhang, Brian Thomas O'Neill
Abstract: The invention proposes a container further extending the shelf life of foods, particularly berries, by including an active agent having antifungal capability into the container surface so that when the fruit is packaged inside the container it is permanently exerted an antifungal effect over the surface, which is the place on the longer determinants occurs, but also contributing to preserve the general environment. Also it proposes a preparation process and its use.
Type:
Grant
Filed:
August 22, 2016
Date of Patent:
September 19, 2017
Assignee:
Universidad de Santiago de Chile
Inventors:
Maria Paula Junqueira Conceicao Gonsalves, Andrea Marcarena Tapia Ulloa
Abstract: An injectable preparation of estrogenic and progestrogenic hormonal compounds in an anhydrous excipient injected to synchronize estrus in non-menstruating placental female animals, and a five to nine day protocol to apply the unique preparation to achieve estrus synchronization.
Abstract: Optionally substituted (1- or 3-oxy)-4,5,7,8-tetrahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-imidazo[1,2-a]pyrrolo[3,4-e]pyrimidine or (1- or 3-oxy)-4,5,7,8,9-pentahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-pyrimido[1,2-a]pyrrolo[3,4-e]pyrimidine compounds, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising the same.
Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
Type:
Grant
Filed:
July 11, 2016
Date of Patent:
September 12, 2017
Assignee:
CHEMOCENTRYX, INC.
Inventors:
Trevor T. Charvat, Junfa Fan, Christopher W. Lange, Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jeffrey P. McMahon, Jay Powers, Sreenivas Punna, Ju Yang
Abstract: Combinations of a muscarinic acetylcholine receptor antagonist and a beta 2 agonist for inhaled administration via the nose or mouth, and methods of using them are provided.
Type:
Grant
Filed:
December 16, 2015
Date of Patent:
September 5, 2017
Assignee:
Glaxo Group Limited
Inventors:
Darrell Baker, Mark Bruce, Glenn Crater, Brian Noga, Marian Thomas, Patrick Wire
Abstract: The invention relates to tetrahydroquinoline derivatives and their use in the treatment and/or the prevention of a disease wherein the Epac protein is involved, such as inflammation, cancer, vascular diseases, kidney diseases, cognitive disorders and cardiac diseases.
Type:
Grant
Filed:
September 17, 2013
Date of Patent:
September 5, 2017
Assignees:
Institut National de la Sante et de la Recherche Medicale (INSERM), Universite Paul Sabatier Toulouse III, Universite Paris-Sud, Universite d'Orleans
Inventors:
Frank Lezoualc'h, Rodolphe Fischmeister, Malik Bisserier, Pascal Bouyssou, Jean-Paul Blondeau, Delphine Courilleau
Abstract: The present disclosure refers to heptyl glucoside included, as a natural solubilizer and as a skin penetration enhancer, in transdermal pharmaceutical compositions. Heptyl glucoside is a natural alkyl glycoside and a hydrotrope that improves solubility of active pharmaceutical ingredients (APIs), thereby enhancing skin permeability to APIs. Transdermal pharmaceutical compositions including heptyl glucoside allow lower APIs dosage requirements. Heptyl glucoside can be combined with at least one API and suitable ingredients to formulate transdermal pharmaceutical compositions with improved skin permeability, thereby promoting percutaneous absorption of APIs. Transdermal pharmaceutical compositions including heptyl glucoside can be formulated in a plurality of dosage forms, such as, a liquid, cream, paste, gel, lotion, patch (e.g., matrix and reservoir), tape, film former (e.g., plaster), and the like.
Type:
Grant
Filed:
April 9, 2015
Date of Patent:
September 5, 2017
Assignee:
Professional Compounding Centers of America (PCCA)
Abstract: Disclosed herein are methods of diagnosing and treating infectious disease characterized by a pathology that involves hemorrhaging or pathological vascular leakage.
Abstract: Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein R1, R2, RE, L, M and Z are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
Type:
Grant
Filed:
February 1, 2016
Date of Patent:
August 1, 2017
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Kenneth L. Arrington, Christopher Burgey, Robert Gilfillan, Yongxin Han, Mehul Patel, Chun Sing Li, Yunfu Luo, Zhiyu Lei
Abstract: The present invention relates to a selective dual delta (?) and gamma (?) PI3K protein kinase modulator (S)—N-(5-(4-amino-1-(1-(5-fluoro-3-(3-fluorophenyl)-4-oxo-4H-chromen-2-yl)ethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-methoxyphenyl) methane sulfonamide, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of PI3K kinase mediated diseases or disorders with them.
Type:
Grant
Filed:
June 26, 2015
Date of Patent:
July 18, 2017
Assignee:
RHIZEN PHARMACEUTICALS SA
Inventors:
Prashant K. Bhavar, Swaroop K. Vakkalanka
Abstract: Disclosed are compounds of Formula G1 (structurally represented): where “RG3” “Rd1” to “Rd4”, “n”, “m”, “p”, “W”, “X”, “Y”, and “Z” are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.
Type:
Grant
Filed:
December 20, 2013
Date of Patent:
July 18, 2017
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Amjad Ali, Michael Man-Chu Lo, Yeon-Hee Lim
Abstract: To provide pharmaceutical preparation exhibiting satisfactory dissolution property in a wide pH range. The pharmaceutical composition is characterized by containing (A) 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, represented by the following formula (1), a pharmacologically acceptable salt thereof, or a hydrate of any of these, and (B) one or more species selected from the group consisting of a sugar alcohol and a water-swelling additive.