Abstract: Disclosed is the use of an active ingredient in the manufacture of a medicament, wherein the active ingredient is selected from the group consisting of butylidenephthalide (BP), a pharmaceutically acceptable salt of butylidenephthalide, and combinations thereof, and wherein the medicament is used for the prevention and/or treatment of oral submucous fibrosis (OSF) and may be used in the form of an injection lozenge, oral solution, or smearing preparation.
Abstract: There is provided novel mono-acrylate functionalized siloxane monomer containing carbosiloxane linkage for improved hydrolysis resistance. This invention also provides copolymers produced using these monomers and their use in various applications.
Type:
Grant
Filed:
March 21, 2011
Date of Patent:
August 27, 2019
Assignee:
Momentive Performance Materials Inc.
Inventors:
Anubhav Saxena, Umpathy Senthilkumar, Kenrick M. Lewis
Abstract: Disclosed herein are formulations of dexamethasone or a prodrug thereof suitable for delivery by ocular iontophoresis and methods of use thereof.
Type:
Grant
Filed:
May 11, 2012
Date of Patent:
August 13, 2019
Assignee:
Eyegate Pharmaceuticals, Inc.
Inventors:
Mike Jaffe, Gary Cook, Perry Calias, Michael A. Patane
Abstract: The present disclosure relates to novel crystalline forms of JAK inhibitors and the preparation method thereof. The novel crystalline forms in the present disclosure can be used for the treatment of autoimmune diseases, particularly for the treatment of rheumatoid arthritis. The novel crystalline forms in the present disclosure have good stability and remarkable purification effect in process, moreover, its solubility and hygroscopicity meet the requirements for medical use. The preparation method of novel crystalline forms is simple, low cost, and has an important value for future optimization and development of the drug.
Abstract: A method to prepare a catheter locking formulation, comprising in a first step, dissolving trimethoprim in propylene glycol at a temperature greater than room temperature, and in a final step, adding absolute ethanol at about room temperature to a solution of trimethoprim, propylene glycol, EDTA Calcium Disodium Hydrate, phosphate buffered saline, and glycerin.
Abstract: The present invention discloses scalarane sesterterpenoids represented by formula (I) and meroditerpenoid represented by formula (II), which are extracted from Carteriospongia sp. sponge: where R1 is —CH3 or —C2H5. The compounds of formula (I) can be used to be an anticancer, act as an inhibitor targeting to topoisomerase II and hsp90 and a pharmaceutical composition for anticancer.
Type:
Grant
Filed:
August 14, 2017
Date of Patent:
June 11, 2019
Assignee:
National Dong Hwa University
Inventors:
Mei-Chin Lu, Ping-Jyun Sung, Jui-Hsin Su, Kuei-Hung Lai, Yi-Chang Liu, Ying-Chi Du, Yu-Ming Hsu, Ming-Kai Weng, Fu-Wen Kuo
Abstract: This invention provides novel polydentate selective high affinity ligands (SHALs) that can be used in a variety of applications in a manner analogous to the use of antibodies. SHALs typically comprise a multiplicity of ligands that each bind different region son the target molecule. The ligands are joined directly or through a linker thereby forming a polydentate moiety that typically binds the target molecule with high selectivity and avidity.
Type:
Grant
Filed:
September 13, 2017
Date of Patent:
May 21, 2019
Assignees:
Lawrence Livermore National Security, LLC, The Regents of the University of California
Inventors:
Sally J. DeNardo, Gerald L. DeNardo, Rodney L. Balhorn
Abstract: Described herein are nitroxyl progenitor compounds, and compositions including, and methods or generating, the compounds thereof, and methods of treating or preventing disease and disease symptoms using the compounds and compositions.
Type:
Grant
Filed:
September 22, 2014
Date of Patent:
April 30, 2019
Assignee:
The Johns Hopkins University
Inventors:
John P. Toscano, Christopher M. Pavlos, Preeya Kapur Boppana
Abstract: The disclosure relates to cyclopropyl derivatives and methods of use. In some embodiments, the disclosure relates to methods of managing medical disorders with pharmaceutical compositions disclosed herein administered to subject in need thereof. In certain embodiments, the disclosure relates to methods of managing mental disorders, mood disorders, pain, and fibromyalgia and related conditions with pharmaceutical compositions disclosed herein.
Type:
Grant
Filed:
May 3, 2016
Date of Patent:
February 19, 2019
Assignees:
Emory University, Wake Forest University Health Services
Inventors:
Huw M. L. Davies, Spandan Chennamadhavuni, Thomas J. Martin, Steven R. Childers
Abstract: The present invention relates to a class of benzimidazole-2-piperazine heterocyclic derivatives, a preparation method and medical use thereof. Specifically, the present invention relates to a new benzimidazole-2-piperazine heterocyclic derivative of general Formula (I), a preparation method, a pharmaceutical composition containing the same, and use thereof as a therapeutic agent and especially as a poly(ADP-ribose)polymerase (PARP) inhibitor.
Type:
Grant
Filed:
June 13, 2014
Date of Patent:
February 5, 2019
Assignee:
SHANGHAI HUILUN LIFE SCIENCE &TECHNOLOGY CO., LTD
Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
Type:
Grant
Filed:
May 23, 2017
Date of Patent:
January 22, 2019
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Alex Aronov, Jon H. Come, Robert J. Davies, Albert Charles Pierce, Philip N. Collier, Ronald Lee Grey, Hardwin O'Dowd, James A. Henderson, Elaine B. Krueger, Anne-Laure Grillot, Arnaud Le Tiran, Yusheng Liao, David Messersmith, Jian Wang, Jingrong Cao, Upul Keerthi Bandarage, Suganthini S. Nanthakumar
Abstract: The present invention relates to a tablet having a weight of 30-200 mg and consisting of: 60-100 wt. % of granules consisting of: 50-90% by weight of the granules of dehydroepiandrosterone (DHEA); 6-35% by weight of the granules of microcrystalline cellulose; 0-20% by weight of the granules of one or more other pharmaceutically acceptable granule ingredients; and 0-40 wt. % of one or more other pharmaceutically acceptable tablet components. These tablets can suitably be used to orally administer DHEA in dosages of around 50 mg and are sufficiently small to be incorporated in, for instance, ordinary oral contraceptive blister packs.
Type:
Grant
Filed:
July 17, 2012
Date of Patent:
January 15, 2019
Assignee:
PANTARHEI BIOSCIENCE B.V.
Inventors:
Herman Jan Tijmen Coelingh Bennink, Johannes Jan Platteeuw
Abstract: Provided are an agent for imparting ceramide-like function, an agent for reinforcing skin barrier function, a moisturizing agent and a skin drug for external use. The agent for imparting ceramide-like function comprises as an effective ingredient a derivative of succinic acid diamide represented by the following formula (1): [wherein R1 and R2 each independently represents a hydroxyalkyl group of from 1 to 6 carbon atoms, R3 represents a group: —CH2CH2CH2CH2—R4 or a group: —CH2CH?CHCH2—R4 (wherein R4 represents an alkyl group of from 8 to 26 carbon atoms)].
Abstract: There is provided inter alia a compound of formula (I): wherein R1, J, Ar, L, X, R3 and R4 are as defined in the specification, for use in the treatment of inflammatory disorders.
Type:
Grant
Filed:
January 6, 2016
Date of Patent:
December 4, 2018
Assignee:
Respivert Ltd.
Inventors:
John King-Underwood, Ito Kazuhiro, Peter Strong, William Garth Rapeport, Catherine Elisabeth Charron, Peter John Murray, Jonathan Gareth Williams, Stuart Thomas Onions
Abstract: A method for reducing parasites in aquatic animals is provided. The method includes administering to the aquatic animal a compound comprising propyl propane thiosulfonate (PTSO) having the formula R—SOa-S—R, where R represents n-propyl group (—CH2—CH2—CH3) and a is 2 and also propyl propane thiosulfinate (PTS) having the formula R—SOa-S—R, where R represents n-propyl group (—CH2—CH2—CH3) and a is 1, so that a combination of PTS and PTSO is administered to the aquatic animal resulting in the reduction of a plurality of crustaceans infecting the aquatic animal in response to administering the combination of PTS and PTSO to the aquatic animal.
Type:
Grant
Filed:
September 25, 2017
Date of Patent:
December 4, 2018
Assignee:
INVESTFOOD, LLC
Inventors:
Cristina Núñez Lechado, Alberto Baños Arjona, Enrique Guillamón Ayala, Adela Valero López, Ma Concepción Navarro Moll, Ana Sanz Rus
Abstract: This application relates to a novel benzo-heterocycle derivative and more particularly, it relates a composition for preventing and treating cancer or for inhibiting metastasis comprising benzo-heterocycle derivative or pharmaceutically acceptable salts thereof as an active ingredient. The present inventors confirmed that KRS has an effect on cancer metastasis by facilitating cancer (or tumor) cell migration through interaction with 67LR, and also found that a substance inhibiting the interaction between KRS and 67LR can prevent and treat cancer by inhibiting cancer cell metastasis. Accordingly, the composition of the present invention can inhibit cancer metastasis, and thus provide a novel means for prevention and treatment of cancer.
Type:
Grant
Filed:
May 7, 2012
Date of Patent:
November 20, 2018
Assignee:
MEDICINAL BIOCONVERGENCE RESEARCH CENTER
Inventors:
Sunghoon Kim, Jin Woo Choi, Jin Young Lee, Dae Gyu Kim, Gyoon Hee Han, Jee Sun Yang, Chul Ho Lee
Abstract: Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR?R?, Q is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R? is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR?R? or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.
Type:
Grant
Filed:
October 26, 2017
Date of Patent:
November 20, 2018
Assignee:
Molecular Insight Pharmaceuticals, Inc.
Inventors:
John W. Babich, Craig N. Zimmerman, Kevin P. Maresca
Abstract: The present invention provides a compound having a PDE2A selective inhibitory action, which is useful as an agent for the prophylaxis or treatment of schizophrenia, Alzheimer's disease and the like. The present invention is a compound represented by the formula (1): wherein each symbol is as described in the specification, or a salt thereof.
Abstract: An aqueous solution formulation containing Compound (I) can be manufactured by performing a first step of preparing a dissolution liquid obtained by dissolving a compound represented by Formula (I) below or a pharmacologically acceptable salt thereof and a compound represented by any of General Formulas (II) to (IV) below in an organic solvent, a second step of removing the organic solvent from the dissolution liquid, and a third step of adding a solution to residual substances obtained through the second step to dissolve the residual substances.