Abstract: Provided is a pharmaceutical composition including as an active component a compound of formula (I): wherein X and (R1)n are as defined, and a physiological acceptable carrier. Also provided is a method for treating cancer including administering to an individual in need of such treatment an effective amount of the presently described pharmaceutical composition.
Type:
Grant
Filed:
August 10, 2008
Date of Patent:
July 9, 2013
Assignee:
Urifer Ltd.
Inventors:
Uri Nir, Sally Shpungin, Etai Yaffe, Moshe Cohen
Abstract: The present invention relates to methods of treating a patient infected by Actinomycetes sp. by administering 6-aza-17-substituted-androst-4-en-3-one compounds to that patient. Another aspect of the invention relates to the screening for drug candidates to treat patients infected by Actinomycetes sp.
Type:
Grant
Filed:
December 3, 2007
Date of Patent:
July 9, 2013
Assignee:
The Research Foundation of State University of New York
Abstract: A method of treating peripheral neuropathic pain in humans resulting from a peripheral nerve injury and for treating muscle spasm in humans resulting from a peripheral nerve injury comprises applying a therapeutically effective amount of a drug selected from the group consisting of a dopamine agonist, a skeletal muscle relaxant, and a combination thereof topically to the site of the injury.
Abstract: The present disclosure relates to methods of using fatty acid amide hydrolase (FAAH) inhibitors to treat aspects of Parkinson's disease (PD), restless legs syndrome (RLS) and periodic limb movement disorder (PLMD), the use of FAAH inhibitors for the manufacture of medicaments for use in the treatment of PD, RLS and PLMD, as well as pharmaceutically acceptable compositions comprising FAAH inhibitors for use in the treatment of PD, RLS and PLMD.
Type:
Application
Filed:
January 7, 2011
Publication date:
June 13, 2013
Applicants:
Ironwood Pharmaceutical, Inc.
Inventors:
James Philip Pearson, Todd G. Milne, Thomas Henry Johnston, Jonathan Michael Brotchie
Abstract: The present invention provides a method of promoting bone growth in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I. The present invention also provides methods for the treatment of renal disease and cancer.
Abstract: The present invention is directed to compositions and methods for the treatment of post-chemotherapeutic hypotrichosis. More specifically, the present invention is directed to the use of compositions comprising bimatoprost for the treatment of post-chemotherapeutic hypotrichosis which may be applied before, during and after receiving chemotherapeutic treatment.
Abstract: Embodiments of liquid-filled hard gel capsule pharmaceutical formulations comprise a non-emulsified mixture, wherein the non-emulsified mixture comprises about 0.1 to about 5% by weight of at least one active pharmaceutical ingredient, about 50 to about 95% by weight medium chain triglycerides, and about 5 to about 25% by weight medium chain mono/diglycerides, wherein the medium chain triglycerides and medium chain mono/diglycerides are present at a ratio by weight of from about 10:1 to about 5:1.
Type:
Application
Filed:
September 14, 2012
Publication date:
May 23, 2013
Applicant:
MYLAN INC.
Inventors:
Sarat C. Chattaraj, Glenn Allen Redelman
Abstract: The present invention provides a kit comprising, in separate compartments of a container, the following components (a) and (b): (a) a combination of apomorphine or a pharmaceutically acceptable acid addition salt thereof and a pharmaceutically acceptable excipient or carrier; and (b) a solution which comprises a diluent and a pH modifying agent; the components being presented such that they can be combined at the point of use into a formulation which is adjusted to a pH ranging from mildly acidic to alkaline and which is suitable for buccal administration. The formulation is useful in treating Parkinson's disease and in promoting sexual function.
Abstract: The invention features derivatives of R(?)-2-methoxy-11-hydroxyaporphines and methods of treating Parkinson's disease and sexual dysfunction therewith.
Abstract: An indenoquinolone compounds of Formula (A) is disclosed, wherein the definition of each group is described in the description. These compounds may specifically inhibit topoisomerase I, and they have good activities against many kinds of human tumor cells, such as lung cancer, colon cancer, breast cancer, liver cancer and the like. They can be used in the manufacture of antitumor drugs. The method for preparing the compound of formula (A), and pharmaceutical compositions containing such compounds and the use in the manufacture of antitumor drugs are also disclosed.
Type:
Application
Filed:
May 17, 2011
Publication date:
April 25, 2013
Applicant:
SECOND MILITARY MEDICAL UNIVERSITY, PLA
Abstract: Activated fatty acids, pharmaceutical composition compositions including activated fatty acids, methods for using activated fatty acids to treat nephropathy, and methods for preparing activated fatty acids are provided herein.
Abstract: The present invention provides tetrahydropyrvinium (THP), derivatives thereof, benzoxazole compounds, and derivatives thereof. The present invention provides a method of using tetrahydropyrvinium (THP), derivatives thereof, benzoxazole compounds, and derivatives thereof.
Type:
Application
Filed:
December 6, 2012
Publication date:
April 18, 2013
Applicant:
The Regents of the University of California
Inventor:
The Regents of the University of California
Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
Type:
Grant
Filed:
August 5, 2010
Date of Patent:
April 9, 2013
Assignee:
Janssen Pharmaceutica, NV
Inventors:
José Maria Cid-Núñez, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez, Mohamed Koukni, Georges Joseph Cornelius Hoornaert, Frans Josef Cornelius Compernolle, Tomasz Kozlecki, Hua Mao, Sushil Chandra Jha, Francisco Javier Fernández-Gadea
Abstract: The invention features sublingual film formulations of dopamine agonists and methods of treating Parkinson's disease, tremors, restless leg syndrome, sexual dysfunction, and depressive disorders therewith.
Type:
Grant
Filed:
April 12, 2012
Date of Patent:
April 9, 2013
Assignees:
Cynapsus Therapeutics, Inc., ARx, LLC
Inventors:
Nathan John Bryson, Anthony John Giovinazzo, Scott David Barnhart, Michael Clinton Koons
Abstract: Indenoisoquinolinone derivatives (I), the manufacturing method and the medical use thereof, which belong to pharmaceutical chemistry and organic chemistry field, are disclosed. These compounds can be used for treating several medical symptoms related to postmenopausal syndrome, uterine fibers deterioration and aortic smooth muscle cells proliferation, especially ER-(+) depend breast cancer. Meanwhile, these compounds can also be used for treating glioma and lung cancer, and have inhibiting effect on tumor metastasis effect on tumor metastasis.
Type:
Application
Filed:
December 16, 2009
Publication date:
April 4, 2013
Applicant:
CHINA PHARMACEUTICAL UNIVERSITY
Inventors:
Hua Xiang, Tianlin Wang, Hong Xiao, Qidong You, Yao Yao, Xiaobo Li, Qingjiang Liao
Abstract: This invention relates to compositions and methods of combining berberine, artemisinin and loperamide or their derivatives in a therapeutic product for mammals suffering from malaria, diarrhea, travelers' diarrhea, dysentery, dengue fever, parasites, cholera and viruses by administration of a therapeutically effective amount of the composition.
Abstract: Disclosed is a method of treating a cancer on a mammal, comprising administering to the mammal in need thereof a therapeutically effective amount of a compound
Abstract: New uses of safinamide, safinamide derivatives and MAO-B inhibitors in novel types of treatment for Parkinson's Disease are described. More specifically, the invention relates to methods for treating Parkinson's Disease through the administration of safinamide, a safinamide derivative, or a MAO-B inhibitor, in combination with other Parkinson's Disease agents or treatments, such as levodopa/PDI or dopamine agonists.
Type:
Application
Filed:
August 24, 2012
Publication date:
February 28, 2013
Applicant:
Newron Pharmaceuticals S.P.A
Inventors:
Fariello Ruggero, Carlo CATTANEO, Patricia SALVATI, Luca BENATTI
Abstract: Tetrahydroberberine (THB), isolated from the Chinese herb “Corydalis ambigua”, exhibits a variety of pharmacological effects, although mechanisms of action are unclear or entirely unknown. Described herein are novel methods of using tetrahydroberberine (THB), THB analogs or derivatives, tetrahydroprotoberberines (THPB). Tetrahydroberberine (THB) and analogs such as l-stepholidine (l-SPD) potently block functional KATP channels natively expressed on midbrain dopamine neurons. Further, THB also blocks pancreatic ?-cell KATP channels, and can be developed to a novel drugs for treating disease and/or conditions such as diabetes and Parkinson's disease.
Abstract: The present invention is directed to a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.
Type:
Grant
Filed:
May 7, 2010
Date of Patent:
February 5, 2013
Assignee:
Tetraphase Pharmaceuticals, Inc.
Inventors:
Roger B. Clark, Minsheng He, Louis Plamondon, Xiao-Yi Xiao, Magnus P. Rönn
Abstract: The present invention is a method for identifying agents which modulate microRNA activity. The invention involves contacting a cell harboring a microRNA and a microRNA binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent and determining whether the test agent increases or decreases the expression of the reporter protein thereby identifying a microRNA modulator. Antagonists identified by this screening assay are provided, as are methods for using the same to inhibit microRNA activity and prevent or treat disease.
Type:
Application
Filed:
June 20, 2012
Publication date:
January 24, 2013
Inventors:
Qihong Huang, Alexander Deiters, Kiranmai Gumireddy
Abstract: A therapeutic drug for psychoneurotic disorders, which is useful for therapies of psychoneurotic disorders, especially restless legs syndrome is disclosed. The therapeutic drug for psychoneurotic disorders according to the present invention comprises as an effective ingredient an opioid ? receptor agonist compound (excluding pentazocine) such as (?)-17-(cyclopropylmethyl)-3,14?-dihydroxy-4,5?-epoxy-6?[N-methyl-trans-3-(3-furyl)acrylamide]morphinan hydrochloric acid salt.
Abstract: The present invention relates to enhancing the dosing efficiency of pharmaceutical dry powder formulations administered by pulmonary inhalation. In particular, the present invention relates to the provision of dry powder inhalers and dry powder compositions which reproducibly achieve a much higher delivered dose of the pharmaceutically active agent than currently achieved.
Type:
Application
Filed:
May 4, 2012
Publication date:
December 20, 2012
Applicant:
VECTURA LTD.
Inventors:
John Nicholas Staniforth, David Morton, Michael Tobyn, Stephen Eason, Quentin Harmer, David Granderton
Abstract: The present disclosure relates to a method to stimulate endogenous BMP-2 up-regulation in a subject which method comprises administering to a subject an effective amount of one or more of the following compounds prazosin, quinacrine, emetine, apomorphine, and debrisoquine, whereby endogenous BMP-2 up-regulation is stimulated in said subject. The endogenous BMP-2 up-regulation may enhance bone formation and/or cartilage formation.
Abstract: The present invention provides a method of promoting bone growth in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I. The present invention also provides methods for the treatment of renal disease and cancer.
Abstract: The present invention concern the use of isoquinoline alkaloid compounds of formula I in the preparation of pharmaceutical compositions useful in the treatment of neurodegenerative diseases, particularly Alzheimer's disease, as well as pharmaceutical composition comprising said compounds and method of treatment of neurodegenerative diseases wherein R1 is —OH or —OCH3, and X is non-existent, HCl or HBr, including their isomers,
Type:
Application
Filed:
January 19, 2011
Publication date:
November 29, 2012
Inventors:
Luiz Francisco Pianowski, Joäo Batista Calixto, Jan A. Glinski
Abstract: Pharmaceutical compositions that bind to a predicted FK506 Binding Protein 52 (FKBP52) interaction surface on the androgen receptor hormone binding domain, otherwise known as FKBP52 Targeting Agents (FTAs) are provided. These compositions of the present invention are found to specifically recognize the FKBP52 regulatory surface on the androgen receptor and inhibit FKBP52 from functionally interacting with the androgen receptor. Compositions comprising the pharmaceutical composition, as well as methods of use, treatment and screening are also provided.
Type:
Application
Filed:
September 14, 2010
Publication date:
November 8, 2012
Applicants:
The Regents of the University of California, a California Corporation, University of Texas at El Paso, Health and Human Services
Inventors:
Leonard M. Neckers, Marc B. Cox, Jane B. Neckers, Yeong Sang Kim, Aki Iwai, Yangmin Ning, Johanny Tonos de Leon, Heather Balsiger, Robert Fletterick
Abstract: The present invention relates to methods and compositions for modulating calcium channels. In particular, the present invention provides methods and compositions for modulating (e.g., disrupting) Cav1.3a calcium channels for research and therapeutic methods (e.g., treating dopaminergic diseases and conditions).
Type:
Application
Filed:
June 7, 2012
Publication date:
October 18, 2012
Inventors:
D. James Surmeier, Michelle Day, Jun Ding, Savio Chan, Jamie Guzman, Jeff Mercer, Tatiana Tkatch, Zhongfeng Wang, Ema Ilijic
Abstract: Pseudobase benzo[c]phenanthridines and the pharmaceutically acceptable salts thereof of Formula I are provided herein. The variables R, R1, R2, R3, and R4 are defined herein. Certain pseudobase benzo[c]phenanthridines provided herein act as prodrugs, targeting the parent benzo[c]phenanthridinium alkaloid to hydrophilic or hydrophobic regions in the body. Pharmaceutical compositions comprising a pseudobase benzo[c]phenanthridine and a carrier, excipient, or diluent are provided herein. Methods of treating or preventing microbial, fungal and or viral infections and methods of treating diseases and disorders responsive to protein kinase C modulation, topoisomerase I, and/or topoisomerase II modulation are also provided.
Abstract: The present invention provides compositions, methods, and kits for treatment of Parkinson's disease and other conditions for which treatment with a dopamine agonist is therapeutically beneficial. The invention provides a biocompatible nonerodible polymeric device which releases dopamine agonist continuously with generally linear release kinetics for extended periods of time. Dopamine agonist is released through pores that open to the surface of the polymeric matrix in which it is encapsulated. The device may be administered subcutaneously to an individual in need of continuous treatment with dopamine agonist.
Type:
Application
Filed:
June 15, 2012
Publication date:
October 11, 2012
Inventors:
Rajesh A. PATEL, Louis R. Bucalo, Lauren Costantini, Sofie Kleppner
Abstract: The invention relates to insect attractants containing compounds with pentagonal heterocyclic structures that are effective in attracting fruitflies.
Abstract: This invention relates to a topical cosmetic skin care method and composition. The method and composition is for treating facial skin to cause contraction and tightening of the facial skin, by effecting contraction of the collagen of the skin using an active agent/s that induces fibroblast contraction of the extra cellular matrix of the skin. A preferred active agent is a beta-2-adrenergic receptor (beta2AR) inhibitor.
Abstract: A reversely thermo-reversible hydrogel composition comprising a water soluble block copolymer comprising at least two blocks of polyethylene oxide and at least one block of polypropylene oxide, and at least one associative gelling adjuvant having water solubility less than 0.5 g/100 ml, preferably less than 0.3 g/100 ml at 20° C., and being capable of forming water soluble inter-molecular complexes with the water soluble block copolymer in water. The hydrogel composition exhibits improved gelling efficiency, enhanced solubility and/or stability for water sparely soluble and insoluble pharmaceutical agents. The hydrogel compositions are useful in a variety of pharmaceutical and cosmetic products and applications, such as esophageal, otic, vaginal, rectal, ophthalmic, treatments of disorders and imperfections of the skin, and treating and/or preventing alopecia and restoring and/or promoting hair growth.
Abstract: Classes of compounds that exhibit effective inhibition of autotaxin enzymes are provided. Such classes include thioureas, diphenyldiazerenes, xanthenes, and isoindoles and exhibit reactivity with autotaxin to ultimately reduce the size of the reactive sites thereon to prevent conversion of lysophosphatidyl choline to lysophophatidic acid. Furthermore, such compounds can be incorporated within delivery forms for human ingestion. As such, these compounds accord an excellent manner of potentially reducing generation of certain cancers attributable to the presence of naturally occurring autotaxin within the human body. Methods of inactivating autotaxin to certain degrees therewith such compounds are encompassed within invention as well.
Type:
Grant
Filed:
November 13, 2008
Date of Patent:
September 18, 2012
Assignee:
University of Memphis Research Foundation
Inventors:
Abby Louise Parrill-Baker, Daniel Lee Baker
Abstract: Compositions and methods of making the same for improving the bioavailability of a substantially water-insoluble pharmacologically active agent are described. The composition includes a substantially water-insoluble pharmacologically active agent, and a substantially water-insoluble matrix forming material comprising enzyme digestible or bile soluble nutrients, wherein the substantially water-insoluble pharmacologically active agent is dispersed in a solid matrix and wherein said pharmacologically active agent in said matrix is substantially free of the original crystalline form.
Abstract: The present invention relates to a method of reducing the production of glutamate from glutamine by glutaminase C in a cell or tissue. The method involves inhibiting glutaminase C activity in the cell or tissue under conditions effective to reduce production of glutamate from glutamine. Compounds for carrying out this method are also disclosed.
Type:
Application
Filed:
March 25, 2010
Publication date:
August 30, 2012
Applicant:
CORNELL UNIVERSITY
Inventors:
Richard A. Cerione, Jon W. Erickson, Kristin Wilson Cerione, Jianbin Wang
Abstract: The invention features sublingual film formulations of dopamine agonists and methods of treating Parkinson's disease, tremors, restless leg syndrome, sexual dysfunction, and depressive disorders therewith.
Type:
Application
Filed:
April 12, 2012
Publication date:
August 2, 2012
Applicants:
ARx, LLC, Cynapsus Therapeutics, Inc.
Inventors:
Nathan John Bryson, Anthony John Giovinazzo, Scott David Barnhart, Michael Clinton Koons
Abstract: Manzamine compounds have been discovered to decrease cell dissociation and cell migration associated with the metastatic potential of cancer cells and a restoration of cancer cell susceptibility to agents, such as TRAIL, which can induce apoptosis. Specifically, Manzamine A has a formerly unrecognized utility in both blocking tumor cell invasion and tumor metastasis as well in restoring cancer cell susceptibility to standard chemotherapeutic agents which induce apoptosis and, therefore, has utility in treating cancer.
Type:
Grant
Filed:
February 20, 2007
Date of Patent:
July 31, 2012
Assignee:
Florida Atlantic University Board of Trustees
Inventors:
Esther A. Guzman, Jacob D. Johnson, Amy E. Wright
Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.
Type:
Grant
Filed:
June 23, 2011
Date of Patent:
July 10, 2012
Assignee:
Eli Lilly and Company
Inventors:
Robert Dean Dally, Jeffrey Alan Dodge, Scott Alan Frank, Ronald Jay Hinklin, Timothy Alan Shepherd, Owen Brendan Wallace
Abstract: The invention pertains to topical pharmaceutical formulations of berberine and its biologically equivalent analogues, such as palmatine and coptisine, for the treatment of rosacea and other red face-related skin disorders. The topical pharmaceutical formulations of this invention contain purified berberine as the primary active drug ingredient at concentrations higher than 0.1%. The invention also pertains to methods of treating rosacea and other red face related skin disorders, such as steroid-induced rosacea-like dermatitis, comprising the administration of topical pharmaceutical formulations that contain berberine or its biologically equivalent analogues, such as palmatine.
Abstract: Compositions and methods for treating chronic infectious diseases using substantially pure oxymatrine or pharmaceutically acceptable salts or esters thereof are disclosed. In one embodiment described herein, the chronic infectious disease is chronic fatigue syndrome. Further described are compositions having an anti-infective amount of substantially pure oxymatrine or pharmaceutically acceptable salts or esters thereof.
Abstract: The present invention relates to particles and to methods of making particles. In particular, the invention relates to methods of making composite active particles comprising a pharmaceutically active material for pulmonary inhalation, the method comprising a jet milling process.
Abstract: 13-substituted 5,6-dihydrodibenzo[a,g]quinolizinium salt compounds of the general formula (I): processes for the preparation of said compounds, pharmaceutical compositions containing said compounds and the use of said compounds for the manufacture of medicaments suitable for the treatment of cancerous diseases.
Type:
Grant
Filed:
July 20, 2009
Date of Patent:
May 29, 2012
Assignee:
Naxospharma S.r.l.
Inventors:
Paolo Lombardi, Franco Buzzetti, Andrea Guido Arcamone
Abstract: The present invention provides a method of promoting bone growth in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I. The present invention also provides methods for the treatment of renal disease and cancer.
Abstract: Cadherin-11 inhibitors and methods for the prevention and treatment of cadherin-11 related diseases are described herein. Cadherin-11 related diseases include cancer and rheumatoid arthritis.
Type:
Application
Filed:
February 9, 2010
Publication date:
May 24, 2012
Applicant:
GEORGETOWN UNIVERSITY
Inventors:
Stephen W. Byers, Sivanesan Dakshanamurthy, Jaime M. Guidry Auvil, Milton L. Brown
Abstract: A synthesis procedure for benzazolo[3,2-a]quinolinium chloride salts and the inclusion of chloro-substituent, amino-substituent, and nitro-substituent resulting in several compounds wherein said procedures provides an increment in the compounds biological activity. The compounds are further used for intra cellular binding, cytotoxicity on malignant cells through apoptosis activation mediated by mitochondrial damage, cellular organelles binding and damage, DNA fragmentation, marker of bacterial growth, antibacterial activity, cell cycle disruption, and a marker due to the auto-fluorescent properties.
Abstract: The invention concerns the combinations of an mGluR modulator, e.g. an mGluR5 modulator and at least one of L-dopa, a dopamine modulator, e.g. a dopamine agonist, a dopa decarboxylase inhibitor or a catechol-O-methyl transferase inhibitor.
Abstract: The present invention provides methods of treating baldness in a subject and generating new hair follicles, comprising epidermal disruption and administration of a compound that promotes a differentiation of an uncommitted epidermal cell into a hair follicle cell. The present invention also provides methods for hair removal and inducing hair pigmentation.