Abstract: Disclosed are preparations and formulations of high thermodynamic activity lipophilic associations (LA), in which there is pairing between an ionizable pharmaceutical agent and a lipophilic species having ionic characteristics opposite to that of the pharmaceutical agent. Such lipophilic associations manifest high thermodynamic activity, as evidenced by their being predominantly in a liquid phase at room temperature or solvated in a lower-than-water dielectric solvent. Further the pharmaceutical agent being solubilized means that dissolution is not rate limiting to transmucosal absorption. This LA or LA-solvate is formulated into a low dielectric dosage form, from whence, upon the dosage form's hydration, the pharmaceutical agent is driven through the mucosal tissue and into systemic circulation. The invention therefore provides an enhanced transmucosal drug delivery system for ionizable pharmaceutical agents at or near physiological pH.
Abstract: The present invention is directed to methods and compositions for inhibition of viral nucleic acid polymerases, such as RNA and DNA polymerases, and methods and compositions that are useful for treating viral infections in subjects. The methods comprise administering to the subject a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or hydrate thereof, or a composition comprising a compound of formula I, or a pharmaceutically acceptable salt or hydrate thereof, and a pharmaceutically acceptable carrier. The composition or method may optionally comprise one or more additional anti-viral agents.
Type:
Grant
Filed:
November 3, 2014
Date of Patent:
November 15, 2016
Assignee:
BioCryst Pharmaceuticals, Inc.
Inventors:
Shanta Bantia, Pravin L. Kotian, Yarlagadda S. Babu
Abstract: Anti-cancer compounds include N-arylmethylidene piperidones having structural formula I: where R is a hydrogen, halogen, methyl, methoxy, or nitro group, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
March 21, 2016
Date of Patent:
November 8, 2016
Assignee:
KING SAUD UNIVERSITY
Inventors:
Abdulrahman I. Almansour, Natarajan Arumugam, Raju Suresh Kumar, Periasamy Vaiyapuri Subbarayan, Ali Abdullah Alshatwi, Hazem A. Ghabbour
Abstract: A method of producing a liquid pharmaceutical suspension by mixing magnesium aluminum silicate, gellan gum, bismuth subsalicylate, and methyl cellulose.
Type:
Grant
Filed:
April 29, 2015
Date of Patent:
November 8, 2016
Assignee:
The Procter & Gamble Company
Inventors:
Steven Ray Gilbert, Edward Paul Fitch, V, Derrick Ho, Daniel Jerome White, Jr., Adam Michael Tunis
Abstract: A liquid pharmaceutical suspension for oral administration containing a bismuth-containing pharmaceutical agent, a suspension system, and water. The suspension system can contain from about 0.001% to about 0.2% gellan gum and from about 0.001% to about 0.75% magnesium aluminum silicate.
Type:
Grant
Filed:
April 29, 2015
Date of Patent:
November 8, 2016
Assignee:
The Procter & Gamble Company
Inventors:
Daniel Jerome White, Jr., Michael Selden Godlewski, Timothy Charles Gulbin, Graham John Myatt
Abstract: Platinum(II) complexes having thione-based heterocyclic ligands as anticancer agents. The central platinum atom is coordinated by four of the ligands, each having a five-, six- or seven-membered heterocyclic ring with two nitrogen atoms at positions 1 and 3 of the ring and a thiocarbonyl group at position 2. Pharmaceutical compositions incorporated the platinum(II) complexes, methods of synthesizing the complexes and methods of treating cancers with the complexes or pharmaceutical compositions thereof are also described.
Type:
Grant
Filed:
September 15, 2015
Date of Patent:
November 1, 2016
Assignee:
King Fahd University of Petroleum and Minerals
Inventors:
Muhammad Altaf, Anvarhusein Abdulkadir Isab
Abstract: Compounds of formula II are described: wherein D, n, Ra, Rb, and Rc are as herein defined, along with pharmaceutical compositions and methods of using compounds of formula II for treating or reducing the risk of peritoneal carcinomatosis in a patient.
Type:
Grant
Filed:
August 26, 2013
Date of Patent:
October 25, 2016
Assignees:
Cephalon, Inc., University of Utah Research Foundation, University of Hawaii
Inventors:
Bruce D. Dorsey, Scott K. Kuwada, Jay P. Theroff, Craig A. Zificsak
Abstract: The present invention relates to the treatment of an individual diagnosed with hearing loss comprising administering to the individual an effective amount of a 1-amino-alkylcyclohexane derivative.
Abstract: Methods for treating molluscum contagiosum warts include identifying a human with one or more molluscum contagiosum warts and applying an anti-infective composition to the one or more warts. The anti-infective composition comprises at least one anti-infective agent in a liquid carrier, such as an organohalide. The liquid carrier includes a tissue penetrating component for rapid penetration of the anti-infective agent into the one or more molluscum contagiosum warts. Application of the anti-infective composition to molluscum contagiosum warts causes the warts to turn black and/or fall off the skin in less than about 5 days.
Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
Type:
Grant
Filed:
October 2, 2014
Date of Patent:
October 11, 2016
Assignee:
ASTEX THERAPEUTICS LTD
Inventors:
Gordon Saxty, Christopher William Murray, Valerio Berdini, Gilbert Ebai Besong, Christopher Charles Frederick Hamlett, Christopher Norbert Johnson, Steven John Woodhead, Michael Reader, David Charles Rees, Laurence Anne Mevellec, Patrick René Angibaud, Eddy Jean Edgard Freyne, Tom Cornelis Hortense Govaerts, Johan Erwin Edmond Weerts, Timothy Pietro Suren Perera, Ronaldus Arnodus Hendrika Joseph Gilissen, Berthold Wroblowski, Jean Fernand Armand Lacrampe, Alexandra Papanikos, Olivier Alexis Georges Querolle, Elisabeth Thérèse Jeanne Pasquier, Isabelle Noëlle Constance Pilatte, Pascal Ghislain André Bonnet, Werner Constant Johan Embrechts, Rhalid Akkari, Lieven Meerpoel
Abstract: This disclosure relates to compounds, compositions and methods of epigenetically transforming cells. In certain embodiments, the disclosure relates to methods of generating epigenetically altered cells comprising mixing isolated cells with compositions disclosed herein under conditions such that epigenetically altered cells are formed. In certain embodiments, the disclosure contemplates inducing cells, such as adult somatic cells or cells that are not naturally pluripotent, into cells with chemically induce pluripotency. In certain embodiments, the disclosure contemplates certain compounds disclosed herein, compounds disclosed herein optionally substituted with one or more substituents, derivatives, or salts thereof, for these purposes.
Type:
Grant
Filed:
November 8, 2012
Date of Patent:
October 4, 2016
Assignee:
Emory University
Inventors:
Young-Sup Yoon, Xiaodong Cheng, Ji Woong Han, Antonello Mai
Abstract: Disclosed are certain pyridinyl and pyrimidinyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds and methods of treatment using such compounds.
Type:
Grant
Filed:
March 1, 2013
Date of Patent:
October 4, 2016
Inventors:
Kenneth W Bair, Timm R Baumeister, Peter Dragovich, Francis Gosselin, Po-Wai Yuen, Mark Zak, Xiaozhang Zheng
Abstract: The present disclosure describes a treatment for acid related gastrointestinal disorders. The compounds described herein are known gastric acid secretion inhibitors in combination with alpha lipoic acid (ALA) or related compounds. ALA is not known as a treatment for acid related gastrointestinal disorders, however, ALA, when combined as described in the present disclosure with certain compounds used in the treatment of acid related gastrointestinal disorders, significantly improves existing treatments.
Abstract: Tricyclic compounds are provided. These compounds are PBK inhibitors, and are useful for the treatment of PBK related diseases, including cancer.
Type:
Grant
Filed:
December 9, 2014
Date of Patent:
September 27, 2016
Assignee:
OncoTherapy Science, Inc.
Inventors:
Yusuke Nakamura, Yo Matsuo, Shoji Hisada, Feryan Ahmed, Raymond Huntley, Zohreh Sajjadi-Hashemi, David M. Jenkins, Robert B. Kargbo, Wenge Cui, Polivina Jolicia F. Gauuan, Joel R. Walker, Helene Decornez, Mahender Gurram
Abstract: The present invention involves novel crystal forms of Dabrafenib mesylate and preparation method thereof, wherein the novel crystal forms are more stable in water or an aqueous system, and have greater solubility and dissolution rate in water, thus having better stability and bioavailability compared with the existing crystal forms.
Abstract: Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for conditions associated with angiogenesis, for example, ocular conditions. Formulations for increased solubility are disclosed. Combination therapy with antibodies and PK/PD data are also disclosed.
Type:
Grant
Filed:
March 14, 2014
Date of Patent:
September 13, 2016
Assignee:
AERPIO THERAPEUTICS, INC.
Inventors:
Kevin Peters, Robert Shalwitz, John Janusz, Alexander Smith
Abstract: This invention provides a method of synthesizing new active compounds for pharmaceutical uses including cancer treatment, wherein the cancers comprise breast, leukocytic, liver, ovarian, bladder, prostatic, skin, bone, brain, leukemia, lung, colon, CNS, melanoma, renal, cervical, esophageal, testicular, spleenic, kidney, lymphatic, pancreatic, stomach and thyroid cancers. This invention is an anti-adhesion therapy which uses the compound as a mediator or inhibitor of adhesion proteins and angiopoietins. It inhibits excess adhesion and inhibits cell attachment. It modulates angiogenesis. The compounds also use as mediator of cell adhesion receptor, cell circulating, cell moving and inflammatory diseases.
Abstract: Methods for the safe administration of imidazole or imidazolium compounds, and conditions that may be treated by these methods, are described herein.
Abstract: A stable pharmaceutical mercury-free aqueous solution of cyanocobalamin comprised of cyanocobalamin and water wherein said solution of cyanocobalamin is suitable for intranasal administration, has a viscosity less than about 1000 cPs, and wherein said solution of cyanocobalamin has a bioavailability of cyanocobalamin when administered intranasally of at least about 7% relative to an intramuscular injection of cyanocobalamin with the proviso that the solution is essentially free of mercury and mercury-containing compounds. The present invention is also directed towards a method for elevating the vitamin B12 levels in the cerebral spinal fluid (CSF) comprising administering intranasally a sufficient amount of a mercury-free cyanocobalamin solution so as to increase the average ratio of vitamin B12 in the CSF to that in the blood serum (B12 CSF/B12 Serum×100) to at least about 1.
Type:
Grant
Filed:
September 12, 2014
Date of Patent:
August 16, 2016
Assignee:
PAR PHARMACEUTICAL, INC.
Inventors:
Steven C. Quay, Peter C. Aprile, Zenaida O. Go, Anthony P. Sileno
Abstract: The invention provides methods for treating fibrosis, as well as methods for modulating mitochondrial peroxide production in a cell, and methods for modulating the import of Rac1 into the mitochondria of a cell.