Abstract: The present invention includes a method of inhibiting or reducing mTOR signaling or inhibition of indoleamine dioxygenase-1 (IDO1) in a subject with a proliferative disease, which comprises administering to the subject having or suspected to have the proliferative disease, a therapeutically or prophylactically effective amount of the compound of Formula I: or a pharmaceutically acceptable salt or solvate thereof.
Type:
Application
Filed:
May 9, 2017
Publication date:
November 9, 2017
Inventors:
Vadivel Ganapathy, Yangzom D. Bhutia, Babu Ellappan, Sabarish Ramachandran
Abstract: A method of treating chronic kidney disease in a mammalian subject by administering a composition that includes L-arginine, glycine, L-glutamine, L-histidine, L-aspartic acid L-glutamic acid, and L-carnosine.
Abstract: Methods of modulating healing response to vascular injury and/or vascular scarring in a subject are provided. As such, aspects of the disclosure relate to the use of pro-resolving lipid mediators to modulate inflammation and/or restenosis of a vascular wall. Another aspect of the disclosure relates to the use of pro-resolving lipid mediators to modulate a biological activity of vascular smooth muscle cells (VSMC) or vascular endothelial cells (VEC). Pro-resolving lipid mediators that find use in the subject methods include derivatives of omega-3 polyunsaturated fatty acids and omega-6 polyunsaturated fatty acids, such as resolvins, protectins, lipoxins and maresins and their therapeutically stable analogs. Also provided are vascular devices and compositions for use in the subject methods. Such methods, devices and compositions find use in a variety of applications, including applications related to treatment of vascular injuries and vascular scarring (e.g.
Abstract: A preparation containing a chlorogenic acid crystal form. The crystal form is an orthorhombic crystal system, a space group is P212121, cell parameters are as follows: a=7.7291(2)?, b=10.9808(2)?, c=36.5334(7)?, ?=?=?=90.00°, Z=8, and a cell volume is 3100.65(11)?3. The content of the chlorogenic acid crystal form in the preparation is 10-5000 mg/g. The preparation is advantageous to bioavailability, and can be used for preparing medicines for treating tumor, psoriasis and other immune system diseases, resisting oxidation, protecting liver and gallbladder, treating cardiovascular diseases, and resisting viruses.
Type:
Application
Filed:
November 18, 2015
Publication date:
November 9, 2017
Inventors:
Jie ZHANG, Lina ZHU, Wang HUANG, Liang ZHANG
Abstract: Provided herein are methods for treatment of a neurodegenerative disease, such as neuronal ceroid lipofuscinosis including administering to a subject in need of such treatment a composition comprising a therapeutically effective amount of an agent that mediates upregulation of TPP1.
Abstract: A method of treating and/or preventing blood-associated disorders is provided. Also provided is a method of treating and/or preventing hemophilic arthropathy and/or hemochromatosis arthropathy in a subject.
Type:
Application
Filed:
May 5, 2017
Publication date:
November 9, 2017
Inventors:
Chih-Kuang Chen, Jing-Yi Lee, Wei-Shu Lu, Carl Oscar Brown, III
Abstract: Methods and compositions containing a phorbol ester or a derivative of a phorbol ester are provided for the treatment of chronic and acute conditions. Such conditions may be caused by disease, be symptoms or sequelae of disease. Chronic and acute conditions may be due to viral infections such as HIV and AIDS, neoplastic diseases stroke, kidney disease, urinary incontinence, autoimmune disorders, Parkinson's disease, prostate hypertrophy, aging, or the treatment of such diseases. Additional compositions and methods are provided which employ a phorbol ester or derivative compound in combination with at least one additional agent to yield more effective treatment tools against acute and chronic conditions in mammalian subjects.
Abstract: A eutectic anesthetic composition used to deliver pharmaceutical products topically as well as a method for producing the eutectic anesthetic composition, which may contain up to 80% additive ingredients. Preferred embodiments of the invention may include eutectic emulsion compositions which provide high viscosity/no separation due to API, are not temperature-sensitive, have no shear stress from the ointment mill/EMP, have no gumming up/stickiness or hardening, have improved active penetration and skin adhesion, and can use larger amounts of lipophilic active substances without lessening storage stability.
Abstract: The invention relates to the field of prevention and treatment of cancer, in particular suppression of tumor manifestation. The invention also relates to compounds for use in this field. A novel tumour manifestation suppression (TMS) regulation in a mammalian brain is recognized. The invention relates to compounds, pharmaceutical preparations, in particular medicaments for use in the prevention and treatment of cancer, in particular suppression of tumor manifestation based on said TMS regulation as well as methods for the same.
Type:
Application
Filed:
December 7, 2015
Publication date:
November 9, 2017
Inventors:
József KNOLL, Ildikó MIKLYA, Péter FERDINANDY, Dezso SCHULER, Zsuzsanna SCHAFF, Sándor ECKHARDT
Abstract: Disclosed are small molecule therapeutic compounds that are potent inhibitors of arginase 1 and arginase 2 activity. Also disclosed are pharmaceutical compositions comprising the compounds, and methods for using the compounds for treating or preventing a disease or condition associated with arginase activity.
Type:
Application
Filed:
May 2, 2017
Publication date:
November 9, 2017
Inventors:
Roman Blaszczyk, Joanna Brzezinska, Anna Gzik, Adam Golebiowski, Julita Nowicka, Bartlomiej Borek, Marek Dziegielewski, Karol Jedrzejczak, Krzysztof Matyszewski, Jacek Olczak
Abstract: The invention provides naphthofuran compounds, polymorphs of naphthofuran compounds, naphthofuran compounds in particle form, purified compositions that contain one or more naphthofuran compounds, purified compositions that contain one or more naphthofuran compounds in particle form, methods of producing these naphthofuran compounds, polymorphs, purified compositions and/or particle forms, and methods of using these naphthofuran compounds, polymorphs, purified compositions and/or particle forms to treat subjects in need thereof.
Type:
Application
Filed:
July 5, 2017
Publication date:
November 9, 2017
Applicant:
BOSTON BIOMEDICAL, INC.
Inventors:
Chiang Jia Li, David Leggett, Youzhi Li, Wei Li
Abstract: The present invention relates to a solid pharmaceutical composition for oral administration characterized in that it comprises a benzofuran derivative with antiarrhythmic activity, or one of the pharmaceutically acceptable salts thereof, as an active principle, and a pharmaceutically acceptable nonionic hydrophilic surfactant optionally in combination with one or more pharmaceutical excipients.
Type:
Application
Filed:
July 26, 2017
Publication date:
November 9, 2017
Inventors:
Bernard ABRAMOVICI, Jean-Claude GAUTIER, Jean-Claude GROMENIL, Jean-Marie MARRIER
Abstract: The present disclosure relates to methods of preventing, treating, delaying the onset of, and delaying the progression of liver disease by administering topiramate in combination with phentermine to a patient in need thereof.
Abstract: The present invention provides methods of slowing or reversing the loss of memory and learning comprising the steps of contacting an effective amount of a PKC activator with a protein kinase C (PKC) in a subject identified with memory loss slowing or reversing memory loss. The present invention provides methods of stimulating cellular growth, neuronal growth, dendritic growth, dendritic spine formation, dendritic spine density, and the translocation of ELAV to proximal dendrites, and synaptic remodeling. The present invention also provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to stimulate the synthesis of proteins sufficient to consolidate long-term memory. The present invention also provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to downregulate PKC.
Type:
Application
Filed:
March 24, 2014
Publication date:
November 9, 2017
Applicant:
Blanchette Rockefeller Neuroscience Institute
Abstract: A pharmaceutical composition containing ginkgolide B and an Xa factor inhibitor xaban, a preparation method and use of the pharmaceutical composition, wherein the xaban is selected from Rivaroxaban, Apixaban, Edoxaban, Razaxaban and Otamixaban.
Abstract: The present invention relates to the recognition that inhibition of the base excision repair pathway is selectively lethal in cells which are deficient in HR dependent DNA DSB repair. Methods and means relating to the treatment of cancers which are deficient in HR dependent DNA DSB repair using inhibitors which target base excision repair components, such as PARP, is provided herein.
Type:
Application
Filed:
May 12, 2017
Publication date:
November 9, 2017
Inventors:
Alan Ashworth, Stephen Jackson, Niall Martin, Graeme Cameron Murray Smith
Abstract: An object is to provide a solid composition of stabilized pyrrole carboxamide. A means for achieving the object is a solid composition for medical use containing (S)-1-(2-hydroxyethyl)-4-methyl-N-[4-(methylsulfonyl)phenyl]-5-[2-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide and an appropriate additive.
Abstract: An object of the present invention is to provide a method for controlling skin permeability of an anionic compound and having superior safety. An ionic liquid formed by an anionic compound and an amino acid ester is used.
Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.
Type:
Application
Filed:
July 20, 2017
Publication date:
November 9, 2017
Inventors:
William Fenical, Paul Jensen, Tracy Mincer, Robert H.R. Feling
Abstract: The present invention relates to tetracaine based anesthetic formulations and methods of use thereof The invention further relates to topical formulations of tetracaine and methods of topically anesthetizing body tissues. The present invention also relates to tetracaine based dental anesthetic formulations and methods for anesthetizing the maxillary dental arch using these formulations.
Abstract: Cenicriviroc (CVC) is an orally active antagonist of ligand binding to C-C chemokine receptor type 5 (CCR5) and C-C chemokine receptor type 2 (CCR2). CVC blocks the binding of RANTES, MIP-1?, and MIP-1? to CCR5, and of MCP-1/CCL2 to CCR2. Methods of treating fibrosis and related conditions comprising co-administration of CVC with FXR agonists, high dose vitamin E (>400 iU/d), a peroxisome proliferator-activated receptor alpha (PPAR-?) agonist, PPAR-? agonist, PPAR-? agonist and/or chemokine antagonists are provided herein.
Abstract: The present invention relates to benzimidazol-2-amines of general formula (I) in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.
Type:
Application
Filed:
October 21, 2015
Publication date:
November 9, 2017
Applicant:
Bayer Pharma Aktiengesellschaft
Inventors:
Hartmut REHWINKEL, Sonja ANLAUF, Duy NGUYEN, Olaf PANKNIN, Marcus BAUSER, Katja ZIMMERMANN, Stefan KAULFUSS, Roland NEUHAUS, Paul Matthew BLANEY, Gianna TOSCHI
Abstract: This invention relates to the treatment of uveitis, in particular posterior infectious uveitis. In specific embodiments, the invention provides for methods of treating uveitis and/or infectious uveitis comprising administration of a sustained-release system containing 5-amino-[4-(4-chlorobenzoyl)-3,5-dichlorobenzyl]-1,2,3-triazole-4-carboxamide) and optionally a glucocorticoid. In one embodiment, the glucocorticoid is dexamethasone. In another embodiment, the sustained-release system comprises a polmyer such as e.g. polylactic-coglycolic acid.
Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula I, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.
Type:
Application
Filed:
January 24, 2017
Publication date:
November 9, 2017
Inventors:
Vincent P. Sandanayaka, Sharon Shechter, Sharon Shacham, Dilara McCauley, Erkan Baloglu
Abstract: Atropisomers of 2-(5-bromo-4-(4-cyclopropyl naphthalen-1-yl)-4H- 1,2,4-triazol-3-ylthio)acetic acid are described. Pharmaceutical compositions and the uses of such compounds, compound forms, and compositions for the treatment of a variety of diseases and conditions are also presented.
Abstract: The present invention is directed to methods of treating hepatorenal syndrome by administration of a therapeutically effective amount of a thromboxane A2 receptor antagonist to a patient in need thereof. The present invention is also directed to methods of treating hepatic encephalopathy and cerebral edema by administration of a therapeutically effective amount of a thromboxane A2 receptor antagonist to a patient in need thereof.
Abstract: The present invention relates to a dosing regimen for (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylimino)-3-o-tolyl-thiazolidin-4-one.
Type:
Application
Filed:
December 10, 2015
Publication date:
November 9, 2017
Applicant:
ACTELION PHARMACEUTICALS LTD
Inventors:
Jasper DINGEMANSE, Matthias HOCH, Andreas KRAUSE
Abstract: Methods of treating a developmental disorder such as Dravet syndrome by administering a pharmaceutical composition of gaboxadol or a pharmaceutically acceptable salt thereof are provided.
Abstract: Provided is a powder inhaler comprising a powder inhalant comprising 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.
Type:
Application
Filed:
May 19, 2017
Publication date:
November 9, 2017
Inventors:
Maria Dolors FERNANDEZ FORNER, Maria PRAT QUINONES, Maria Antonia BUIL ALBERO
Abstract: This present invention relates to a method of treating a autoimmune, respiratory and/or inflammatory disease or condition (e.g., psoriasis, rheumatoid arthritis, asthma, COPD). The method comprises administering a PI3K Delta inhibitor or a dual PI3K Delta-Gamma inhibitor and a PDE4 inhibitor. The present invention also relates to pharmaceutical compositions containing a PI3K Delta or dual PI3K Delta-Gamma inhibitor and a PDE4 inhibitor.
Type:
Application
Filed:
July 19, 2017
Publication date:
November 9, 2017
Inventors:
Swaroop K. Vakkalanka, Srikant Viswanadha
Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
Type:
Application
Filed:
July 21, 2017
Publication date:
November 9, 2017
Inventors:
Guoxian Wu, Jiazhong Zhang, Yong-Liang Zhu, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, Dean R. Artis, James Tsai
Abstract: The present invention is directed to pyrazole, triazole and tetrazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the pyrazole, triazole, and tetrazole compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
Type:
Application
Filed:
October 27, 2015
Publication date:
November 9, 2017
Applicant:
MERCK SHARP & DOHME CORP.
Inventors:
NIGEL LIVERTON, SCOTT D. KUDUK, DOUGLAS BESHORE, YUNFU LUO, NA MENG
Abstract: The present invention relates to a donepezil derivative of general formula (I) or a pharmaceutically acceptable salt thereof, wherein R in the formula is as disclosed herein; and a method for preparation thereof; and a composition comprising an effective amount of a compound of the general formula (I) or a pharmaceutically acceptable salt thereof. The present invention also relates to use of a compound of the general formula (I) or a pharmaceutically acceptable salt thereof in preparing a medicament for treating a disease resulted from an abnormality in acetylcholinesterase activity.
Type:
Application
Filed:
November 26, 2015
Publication date:
November 9, 2017
Applicant:
NORATECH PHARMACEUTICALS, INC.
Inventors:
Fei LIU, Cuixia ZHANG, Chenggang LIN, Chunyan ZHOU, Pan CHEN, Wei WANG, Lulu WANG
Abstract: Disclosed herein are methods and compositions related to use of aminopyridines, such as 4-aminopyridine, for use in a therapeutically effective manner for patients with a demyelinating condition, such as multiple sclerosis.
Abstract: The present invention relates to the use of the compound 1-(2-(4-fluorophenyl)thiazol-5-yl)-1-(pyridin-4-yl)ethanol (“ASNOO1”) in treatments without concomitant use of a steroid and/or in the form of a racemic mixture, e.g. in prostate cancer treatment. It also relates to its use in methods that are food indifferent.
Type:
Application
Filed:
July 31, 2014
Publication date:
November 9, 2017
Inventors:
Roger Astbury Smith, Nicholas James Laping, Sandeep Gupta
Abstract: The present invention is directed to compounds of formula (I) which are inhibitors of the BACE1 enzyme. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat disorders for which the reduction of A? deposits is beneficial such as Alzheimer's disease.
Type:
Application
Filed:
November 9, 2015
Publication date:
November 9, 2017
Applicant:
H. Lundbeck A/S
Inventors:
Karsten Juhl, Lena Tagmose, Mauro Marigo
Abstract: Provided herein are drug products with low dose pioglitazone for use in the treatment (e.g., delay of onset) of cognitive impairment of the Alzheimer's type. Methods of manufacture thereof are also provided. Further provided are methods of treatment for Alzheimer's disease including administering a drug product with low dose pioglitazone. The methods may include determining whether the subject is at risk of developing Alzheimer's disease based upon the subject's age and TOMM40 523 genotype.
Type:
Application
Filed:
May 22, 2017
Publication date:
November 9, 2017
Applicants:
Takeda Pharmaceutical Company Limited, Zinfandel Pharmaceuticals, Inc.
Abstract: An oral methylphenidate extended release tablet is described, which can be scored and still retain its extended release profile. The tablet contains a combination of an uncoated methylphenidate—ion exchange resin complex, a barrier coated methylphenidate—ion exchange resin complex—matrix, and an uncomplexed methylphenidate active component. Following administration of a single dose of the extended release methylphenidate chewable tablet, a therapeutically effective amount of methylphenidate is reached in less than about 20 minutes and the composition provides a twelve-hour extended release profile.
Abstract: The present invention relates to CCR3 inhibitors of formula 1, wherein R1 is H, C1-6-alkyl, C0-4-alkyl-C3-6-cycloalkyl, C1-6-haloalkyl; R2 is H, C1-6-alkyl; X is an anion selected from the group consisting of chloride or ½ dibenzoyltartrate j is 1 or 2. for use as a medicament for the treatment of diseases selected from dry age-related macular degeneration (dAMD), wet age-related macular degeneration (wAMD), retinopathy of prematurity (ROP), central retinal vein occlusion (CRVO), nasal polyposis, eosinophilic esophagitis, eosinophillic gastroenteritis (e.g. eosinophilic gastritis and eosinophilic ententeritis), hypereosinophilic syndrome and Churg Strauss syndrome.
Type:
Application
Filed:
July 25, 2017
Publication date:
November 9, 2017
Inventors:
Michael Chadham Nivens, Thierry Bouyssou, Peter Seither, Rolf Goeggel
Abstract: This invention provides a method of treating a patient afflicted with a neurodegenerative disorder, e.g., Huntington's disease (HD), comprising administering to the patient laquinimod as an add-on therapy to or in combination with pridopidine. This invention also provides a package and a pharmaceutical composition comprising laquinimod and pridopidine for treating a patient afflicted with a neurodegenerative disorder, e.g., HD. This invention also provides laquinimod for use as an add-on therapy or in combination with pridopidine in treating a patient afflicted with a neurodegenerative disorder, e.g., HD. This invention further provides use of laquinimod and pridopidine in the preparation of a combination for treating a patient afflicted with a neurodegenerative disorder, e.g., HD.
Abstract: This invention provides a method of treating a subject afflicted with multiple sclerosis or presenting a clinically isolated syndrome comprising administering to the subject laquinimod as an add-on therapy to or in combination with DMF. This invention also provides a package comprising laquinimod and DMF for treating a subject afflicted with multiple sclerosis or presenting a clinically isolated syndrome. This invention also provides laquinimod for use as an add-on therapy or in combination with DMF in treating a subject afflicted with multiple sclerosis or presenting a clinically isolated syndrome. This invention also provides a pharmaceutical composition comprising laquinimod and DMF for use in treating a subject afflicted with multiple sclerosis or presenting a clinically isolated syndrome. This invention further provides use of laquinimod and DMF in the preparation of a combination for treating a subject afflicted with multiple sclerosis or presenting a clinically isolated syndrome.
Abstract: [Problem] To provide a novel pharmaceutical composition which can suppress delayed, release of the compound represented in general formula (1) or a salt thereof. [Solution] This solid pharmaceutical composition contains the compound represented in general formula (1), or a salt thereof, and a salting-out agent.
Abstract: A composition, including a fixed dose composition, comprising Compound (I), Compound (II), and Compound (III) for the treatment of hepatitis C, and methods of manufacture thereof.
Type:
Application
Filed:
July 25, 2017
Publication date:
November 9, 2017
Applicants:
JANSSEN PHARMACEUTICALS, INC., ACHILLION PHARMACEUTICALS, INC.
Inventors:
Maria Gloria Beumont, Lieve Bijnens, Lawrence M. Blatt, Sushmita Mukherjee Chanda, John Fry, Eugene Jans, Thomas Naoki Kakuda, Sivi Mahadevan, Roel Mertens, Gaston Rafael Picchio, Alex Van Dijck, Peter Van Remoortere, David Apelian, Dawei Chen, Milind Deshphande, James Hui, Avinash Phadke
Abstract: Irinotecan phospholipid liposomes with improved storage stability are provided, with related methods of treatment and manufacture. The irinotecan liposomes can have reduced formation of lyso-phosphatidylcholine (lyso-PC) during storage, and prior to administration to a patient.
Type:
Application
Filed:
July 27, 2017
Publication date:
November 9, 2017
Inventors:
Daryl C. Drummond, Dmitri B. Kirpotin, Mark Eamon Hayes, Charles Noble, Kevin Kesper, Antoine M. Awad, Douglas J. Moore, Andrew J. O'Brien
Abstract: The invention relates to an improved method of preparing buprenorphine, a salt thereof, analogues of buprenorphine and their salts. In particular, the invention relates to a method of preparing buprenorphine and related products and salts in economic and ecologic ways having increased yields.
Abstract: Tamper-resistant pharmaceutical compositions have been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opioids. The tamper-resistant compositions retard the release of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is passes through the GI tract.
Type:
Application
Filed:
May 26, 2017
Publication date:
November 9, 2017
Inventors:
Roman V. Rariy, Alison FLEMING, Jane C. HIRSH, Said SAIM, Ravi K. VARANASI
Abstract: The present invention relates to a composition comprising pharmaceutical active ingredients which are susceptible to, or have potential for, abuse. The invention provides an oral pharmaceutical composition comprising a first population of beads and a second population of beads. The first bead population comprises a pharmaceutically active ingredient susceptible to, or having the potential for, abuse. The second bead population comprises a gelling agent and a coating substantially surrounding the gelling agent, but containing no pharmaceutically active ingredient. The first bead population and the second bead population are physically separable, but visually indistinguishable to the naked eye. Upon ingress of water into the second population of beads, the gelling agent is caused to swell forming a viscous mass inhibiting or preventing the extraction of the active ingredient.