Abstract: The invention provides methods and compositions for treating neuromuscular diseases including, but not limited to muscular dystrophies. It is demonstrated herein that statin drugs are therapeutic for neuromuscular disease, including, but not limited to muscular dystrophies.
Type:
Application
Filed:
July 14, 2015
Publication date:
January 14, 2016
Inventors:
Stanley C. Froehner, Nicholas P. Whitehead
Abstract: wherein, in formula (III), X1 represents a C1-6 alkyl group which is unsubstituted or has a substituent, or other groups; ml represents any integer of 0 to 5; A represents an oxygen atom or a sulfur atom; each of R1 and R2 independently represents a hydrogen atom, a C1-6 alkyl group which is unsubstituted or has a substituent, or other groups; R5 represents a hydrogen atom or a C1-6 alkyl group which is unsubstituted or has a substituent; B represents an oxygen atom or a sulfur atom; Q2 represents a C7-11 aralkyl group which is unsubstituted or has a substituent X2, or other groups; and each of R3a, R3b, R4a, and R4b independently represents a hydrogen atom, a C1-6 alkyl group which is unsubstituted or has a substituent, or other groups.
Abstract: Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment of arrhythmia and the production of analgesia and local anesthesia.
Type:
Application
Filed:
February 26, 2015
Publication date:
January 14, 2016
Inventors:
Gregory N. Beatch, Bertrand M.C. Plouvier, Tao Sheng, Michael J.A. Walker, Richard A. Wall, Sandro L. Yong, Jeff Jiqun Zhu, Alexander B. Zoloty
Abstract: The present invention relates to compounds that modulate nicotinic receptors as non-competitive antagonists, methods for their synthesis, methods for use, and their pharmaceutical compositions.
Type:
Application
Filed:
August 27, 2015
Publication date:
January 14, 2016
Inventors:
Srinivasa Rao Akireddy, Balwinder Singh Bhatti, Ronald Joseph Heemstra, Matt S. Melvin, Jason Speake, Yunde Xiao, Daniel Yohannes
Abstract: The invention provides polymorphic crystalline forms of acid addition salts of (+)-1-(3, 4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane designated as polymorph form A, polymorph form B and polymorph form C, where polymorph form A is more thermodynamically stable than the other forms, methods for preparing and using such polymorph forms and pharmaceutical compositions containing such polymorph forms.
Abstract: The invention provides for ischemia/reperfusion protection compositions having one or more ketone bodies and melatonin. The invention also provides for methods of using such compositions to reduce or prevent ischemia/reperfusion injury due to blood loss, stroke or cardiopulmonary arrest or surgery.
Type:
Application
Filed:
September 23, 2015
Publication date:
January 14, 2016
Inventors:
Matthew T. Andrews, Lester R. Drewes, Greg Beilman
Abstract: The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atom; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.
Abstract: Disclosed are methods for preventing metastasis of cancer cells. The disclosed compounds can be used to prevent the spread of tumor or other types of cancer cells.
Abstract: The present invention relates to pharmaceutical package comprising a pharmaceutical preparation comprising azilsartan medoxomil and salts thereof, and a desiccant. Also, relates to a pharmaceutical preparation comprising azilsartan medoxomil and salts thereof and a pH modifier, wherein pH modifier provides a pH range of about 5.5 to about 6.5 when dissolved or suspended in water at a concentration of 1% at 25° C. The invention also relates to processes for the preparation of such pharmaceutical preparation and use thereof for prophylaxis or treatment of circulatory diseases.
Abstract: Compositions, methods, and kits useful for treating hyperlipidemic conditions are provided herein. Such compositions can contain synergizing amounts of nicotinic acid, nicotinamide riboside and/or nicotinic acid metabolites in combination with leucine and/or a leucine metabolite, with or without resveratrol.
Abstract: The present invention provides methods and compositions for treating bladder cancer, including metastatic bladder cancer and non-muscle-invasive bladder cancer, by administering a composition comprising nanoparticles that comprise mTOR inhibitor and optionally an albumin.
Abstract: The present invention relates to the field of inflammatory bowel disease. In one aspect, the present invention provides methods for treating inflammatory bowel disease in a patient comprising administering to the patient a therapeutically effective amount of a stem cell mobilizer and an immunosuppressive agent. In particular embodiments, the present invention provides a method for treating inflammatory bowel disease in a patient comprising administering to the patient a therapeutically effective amount of an agent that mobilizes CD34+ and/or CD133+ stem cells and a low dose of an immunosuppressive agent.
Abstract: Embodiments described here are combinatorial compositions and methods using these compositions for treating melanomas having activated mutations. The compositions comprises combinations of inhibitors of a MAPK pathway, ERK inhibitors, EGFR inhibitors, oxidative phosphorylation (OXPHOS) inhibitors, inhibitors of B-Raf, mitochondrial inhibitors, c-KIT inhibitors, MEK inhibitors and tigecycline or a derivative thereof.
Type:
Application
Filed:
March 6, 2014
Publication date:
January 14, 2016
Applicants:
THE BRIGHAM AND WOMEN'S HOSPITAL, INC., THE GENERAL HOSPITAL CORPORATION
Inventors:
Rizwan HAQ, David E. FISHER, Hans Ragnar WIDLUND
Abstract: The present invention relates to a prophylactic or therapeutic agent for a posterior ocular disease containing the compound represented by a formula (1), its enantiomer or diastereomer, or their pharmaceutically acceptable salt thereof as an active ingredient.
Abstract: The present invention is directed to combinations of sedating antihistamines and at least one, and preferably two or more dietary supplements, which can be indole-based, such as tryptophan, 5-hydroxytryptophan, serotonin, N-acetyl-5-hydroxytryptamine and melatonin, and to their use for treating and thereby improving the health and quality of life of those suffering from sleep-related respiratory disorders, characterized by abnormal breathing during sleep. These include snoring, sleep disordered breathing, sleep apneas, upper airway resistance syndrome, obstructive sleep apnea, central sleep apnea and obesity hypoventilation syndrome and associated ailments.
Type:
Application
Filed:
March 5, 2014
Publication date:
January 14, 2016
Applicant:
REQUIS PHARMACEUTICALS INC.
Inventors:
Lars Jacob Stray Knutsen, James M. Hand
Abstract: A timed release pharmaceutical composition comprising donepezil is provided, wherein the composition exhibits the in vitro dissolution profile when tested in a Paddle dissolution apparatus at 50 rpm in 900 ml 6.8 buffer at 37° C., less than about 20% w/w of donepezil is released in 3 to 6 hrs, and more than 90% w/w of donepezil is released after 12 hrs.
Abstract: The present invention provides a method of treating a subject suffering from traumatic brain injury comprising administering to the subject an effective amount of an HDAC inhibitor, structurally represented, thereby treating the subject suffering from traumatic brain injury.
Abstract: The invention provides compositions and methods for the treatment of presbyopia. In a preferred embodiment correction of presbyopia occurs without reduction in distance vision acuity. The compositions of the invention preferably contain a muscarinic agonist and a cycloplegic agent.
Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and the treatment of certain conditions such as COPD.
Type:
Application
Filed:
September 24, 2015
Publication date:
January 14, 2016
Applicant:
Chiesi Farmaceutici S.p.A.
Inventors:
Elisabetta ARMANI, Gabriele Amari, Laura Carzaniga, Carmelida Capaldi, Oriana Esposito, Gino Villetti, Renato De Fanti
Abstract: The present invention relates to compound characterized by a general formula 1, wherein R1 is a aryl or a heteroaryl, and —R2 and R3 independently of each other are hydrogen or a C1-C5 alkyl, but at least one of R2 and R3 is not hydrogen, or together are a C3 or C4 alkyl forming a 5- or 6 membered ring, for use in a method for treating of heart failure, hypertension, cardiac hypertrophy or cancer.
Abstract: The purpose of the present invention is to identify a migratory factor that guides pluripotent stem cells (Muse cells) useful in new medical applications to damage, and to provide a pharmaceutical composition that includes the migratory factor for promoting tissue regeneration in regenerative medicine that makes use of Muse cells. In the present invention, a receptor that is specifically expressed in Muse cells rather than non-Muse cells was identified, and it was confirmed that a ligand for this receptor can function as a migratory factor. In the present invention, sphingosine-1-phosphate (S1P) was identified as a migratory factor, and thus, the present invention pertains to a pharmaceutical composition for guiding pluripotent stem cells to damage, the composition including S1P as an active ingredient.
Type:
Application
Filed:
February 28, 2014
Publication date:
January 14, 2016
Inventors:
Mari Dezawa, Yoshinori Fujiyoshi, Masanori Yoshida
Abstract: The present invention relates to the crystalline mono mesylate monohydrate salt of N-[5-(amino sulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide in a definite particle size range, particle size distribution and a specific surface area range, which has demonstrated increased long term stability and release kinetics from pharmaceutical compositions, as well as to pharmaceutical compositions containing said crystalline N-[5-(amino sulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mono mesylate monohydrate having the afore-mentioned particle size range, particle size distribution and specific surface area range.
Type:
Application
Filed:
August 31, 2015
Publication date:
January 14, 2016
Applicant:
AICURIS GMBH & CO. KG
Inventors:
Wilfried SCHWAB, Alexander BIRKMANN, Kerstin PAULUS, Kurt VOGTLI, Dieter HAAG, Stephan MAAS, Kristian RUEPP
Abstract: Provided are methods for improving cell-based therapies by co-administration with an agent that increases the production and or levels of epoxygenated fatty acids, as well as kits, stents and patches for co-administering stem cells with an agent that increases the production and/or levels of epoxygenated fatty acids.
Type:
Application
Filed:
June 11, 2015
Publication date:
January 14, 2016
Applicant:
THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Inventors:
Nipavan CHIAMVIMONVAT, Bruce D. HAMMOCK
Abstract: It is an object of the present invention that the novel nicotinic receptor antagonists disclosed herein may be used in a broad array of clinical or medicinal facets. For example, it is a contemplated use of the present invention that the novel nicotinic receptor antagonists be used to inhibit the growth cycle of non-small cell lung cancer cells. Without being bound by theory, it is an object of the present invention that the nicotinic receptor antagonists disclosed herein are believed to possess reversible binding properties. Moreover, the compounds of the present invention are selective for 0.7 nAChR. For example, the compounds of the present invention are not believed to bind to 0.4 (32 nAChR neuromuscular receptors. It is also contemplated that the nicotinic receptor antagonists of the present invention will be used as a counter measure to treat exposure, or potential exposure, to a wide array of potential neurotoxins.
Type:
Application
Filed:
June 17, 2015
Publication date:
January 14, 2016
Inventors:
Youyi PENG, Lawrence P. WENNOGLE, Qiang ZHANG, John TOMESCH
Abstract: Methods of treating or managing specific cancers, including non-Hodgkin's lymphoma, by the administration of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Methods of using gene and protein biomarkers as a predictor of non-Hodgkin's lymphoma response to treatment with 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione are also disclosed.
Type:
Application
Filed:
September 18, 2015
Publication date:
January 14, 2016
Inventors:
Peter H. SCHAFER, J. Blake BARTLETT, Ling-Hua ZHANG, Carla HEISE
Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
Abstract: Abuse-resistant, controlled release opioid tablets are a combination containing an opioid antagonist such as naloxone at a level above that needed to suppress the euphoric effect of the opioid, if the combination were crushed to break the controlled release properties causing the opioid and opioid antagonist to be released as a immediate release product as a single dose. The controlled release nature of the table prevents the accumulation of orally effective amounts of opioid antagonist when taken normally. The opioid antagonist is contained in a controlled-release matrix and released, over time, with the opioid.
Abstract: The use of nicotine for treating inflammatory pain and hyphema is described. It is believed that inflammatory pain, such as renal pain, and hyphema can be improved by The various diseases, disorders or conditions can be improved by increasing the activity of ?-melanocyte stimulating hormone (?-MSH), whose release is affected by nicotine.
Abstract: Provided is a prophylactic and/or therapeutic drug for mild cognitive impairment, which can improve interstitial flow in cerebral blood vessel and the like to achieve sufficient clearance of harmful proteins accumulated in the brain. The prophylactic and/or therapeutic drug includes 6-[4-(1-cyclohexyl-1H-tetrazole-5-yl)butoxy]3,4-dihydrocarbostyril or a salt thereof as an active ingredient. The prophylactic and/or therapeutic drug can improve a flow of interstitial fluid around blood vessels in a drainage pathway to excrete harmful proteins. The prophylactic and/or therapeutic drug for mild cognitive impairment may take the form of a pharmaceutical product for oral administration, a liquid pharmaceutical product for oral administration, or an injectable preparation.
Type:
Application
Filed:
September 21, 2015
Publication date:
January 14, 2016
Applicant:
FOUNDATION FOR BIOMEDICAL RESEARCH AND INNOVATION
Abstract: The invention provides storage stable sublingual formulations containing naloxone, a pharmaceutically acceptable salt or a derivative thereof. The invention further provides methods for treating opioid dependence, opioid overdose, and congenital insensitivity to pain with anhidrosis by administering the sublingual formulations of the present invention to a patient in need thereof.
Abstract: Disclosed in certain embodiments is an oral dosage form comprising a therapeutically effective amount of an opioid analgesic, an opioid antagonist and one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid.
Type:
Application
Filed:
July 7, 2015
Publication date:
January 14, 2016
Inventors:
Benjamin Oshlack, Curtis Wright, Christopher Breder
Abstract: Abuse-resistant, controlled release opioid tablets are a combination containing an opioid antagonist such as naloxone at a level above that needed to suppress the euphoric effect of the opioid, if the combination were crushed to break the controlled release properties causing the opioid and opioid antagonist to be released as a immediate release product as a single dose. The controlled release nature of the table prevents the accumulation of orally effective amounts of opioid antagonist when taken normally. The opioid antagonist is contained in a controlled-release matrix and released, over time, with the opioid.
Abstract: Pharmaceutical compositions and methods for treating depression, anxiety, and neurodegenerative diseases and cognitive disorders, such as dementia and Alzheimer's disease, by administering same are provided. The compositions comprise dextromethorphan in combination with quinidine.
Abstract: Biocompatible intraocular implants include an alpha-2 adrenergic receptor agonist and a polymer associated with the alpha-2 adrenergic receptor agonist to facilitate release of the alpha-2 adrenergic receptor agonist into an eye for an extended period of time. The alpha-2 adrenergic receptor agonist may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. The implants may be placed in an eye to prevent the occurrence of one or more ocular conditions, or to reduce one or more symptoms of an ocular condition, such as an ocular neurosensory disorder and the like.
Type:
Application
Filed:
September 22, 2015
Publication date:
January 14, 2016
Inventors:
Glenn T. Huang, James A. Burke, Patrick M. Hughes, Kai-Ming Zhang, Ton Lin, Larry A. Wheeler, Rosy Sheng Donn
Abstract: Methods and products for treating or preventing erythema or a symptom associated with erythema in a subject are described. The methods involve topically applying to an affected skin area a topical aqueous gel composition comprising about 0.01% to about 10% by weight of at least one ?-adrenergic receptor agonist and a pharmaceutically acceptable carrier.
Type:
Application
Filed:
September 23, 2015
Publication date:
January 14, 2016
Inventors:
Michael GRAEBER, Christian LOESCHE, Philip FREIDENREICH, Jack A. DEJOVIN, Isabelle Jean DEJOVIN, Yin-sang LIU, Matthew James LEONI
Abstract: Provided herein are methods for treating or preventing a neuroendocrine tumor of non-gut origin in a patient, comprising administering an effective amount of a TOR kinase inhibitor to a patient having a neuroendocrine tumor of non-gut origin.
Abstract: This invention relates to pyridazine derivatives, compositions comprising therapeutically effective amounts of those pyridazine derivatives and methods of using those derivatives or compositions in treating central nervous system (CNS) disorders with cognitive impairment that are responsive to agonists of ?5 subunit containing GABAA receptor, e.g., age-related cognitive impairment, Mild Cognitive Impairment (MCI), dementia, Alzheimer's Disease (AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia and cancer-therapy-related cognitive impairment.
Abstract: The present invention relates to stable aqueous pharmaceutical compositions of voriconazole or a pharmaceutically acceptable salt thereof suitable for parenteral administration. In particular, the invention relates to ready-to-use stable injectable compositions of voriconazole or a pharmaceutically acceptable salt thereof. The invention also relates to processes for the preparation of such compositions and use thereof for the treatment of fungal infections.
Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. 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:
Application
Filed:
July 29, 2015
Publication date:
January 14, 2016
Inventors:
Luc Farmer, Gabriel Martinez-Botella, Albert Pierce, Francesco Salituro, Jian Wang, Marion W. Wannamaker, Tiansheng Wang
Abstract: Alkyl-piperazine-phenyl 4 (3H)-quinazolinones compounds of general formula (I) below are provided that are pharmacologically active and able to act on the 5-HT1A and 5-HT2A serotonin receptors in a manner that promotes the control, relief or cure of disorders associated with these receptors, and pharmaceutical compositions containing the compounds for the treatment of disorders associated with these receptors. These compounds and their pharmaceutical compositions are useful in the treatment of conditions such as depression, anxiety, phobias, addictions, aggressiveness, impulsiveness, panic, psychotic, eating and sleep disorders, obsessive-compulsive disorder and female sexual dysfunctions, including loss of sexual desire, inhibition of sexual desire and absence of sexual desire, among other disorders associated with these receptors.
Type:
Application
Filed:
September 23, 2015
Publication date:
January 14, 2016
Inventors:
Valter FREIRE TORRES RUSSO, Elisa Mannochio De Souza Russo
Abstract: The instant invention relates to methods for the treatment of WEE1 kinase associated cancer by administering a WEE1 inhibitor, wherein the WEE1 inhibitor is WEE1-1 or a pharmaceutically acceptable salt thereof, or WEE1-2 or a pharmaceutically acceptable salt thereof. In another embodiment, the invention relates to a method for treating a WEE1 kinase associated cancer patient, comprising administering a WEE1 inhibitor, wherein the cancer cells of said patient to be treated are characterized by low expression levels of PKMYT1.
Abstract: The invention provides a method for prophylaxis and/or treatment of an ocular inflammatory disease comprising administering an effective amount of a pyrazolopyrimidine compound represented by formula (I), wherein R1 represents —NR1aR1b (wherein R1a and R1b are the same or different and each represents a hydrogen atom and the like), and the like, R2 represents the formula (R2?1) [wherein k and m represent each an integer of 0-2, n represents an integer of 0-2, L represents a single bond and the like, R5 represents a halogen and the like, R6 represents aryl and the like, X represents —CR8 (wherein R8 represents a hydrogen atom and the like), and the like, R7 represents a hydrogen atom, and the like, and the like, R3 represents —SO2R13 (wherein R13 represents lower alkoxy and the like), and the like, and R4 represents a hydrogen atom and the like, or a pharmaceutically acceptable salt thereof.
Abstract: The invention provides a composition which comprises (a) a PDE3/PDE4 inhibitor which is 9,10-Dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof and (b) a ?2-adrenergic receptor agonist.
Type:
Application
Filed:
March 17, 2014
Publication date:
January 14, 2016
Applicant:
VERONA PHARMA PLC
Inventors:
Michael J.A. Walker, Mario Cazzola, Luigino Calzetta
Abstract: Provided herein are methods for treating or preventing a cancer, in particular solid tumors and hematological cancers, comprising administering to a subject in need thereof an effective amount of a compound of formula (I):
Type:
Application
Filed:
July 13, 2015
Publication date:
January 14, 2016
Inventors:
Dan ZHU, John BOYLAN, Shuichan XU, Jennifer RIGGS, Tao SHI, Andrew WURMSER, David MIKOLON, Gordafaried DEYANAT-YAZDI
Abstract: Described herein are irreversible Btk inhibitor compounds, and methods for using such irreversible inhibitors in the treatment of CNS malignancies.
Abstract: A novel combination comprising the MEK inhibitor N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethyl; -2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, with a mTOR inhibitor, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of MEK and/or mTOR is beneficial, e.g. cancer.
Abstract: Dry powder formulations for inhalation and their use in the treatment diseases and conditions. The formulation contains a uniform blend of a first spray-dried powder and a second spray-dried powder. The first spray-dried powder contains spray-dried particles of a therapeutically active ingredient dispersed in a pharmaceutically acceptable hydrophobic excipient. The second spray-dried powder contains spray-dried particles formed from a pharmaceutically acceptable hydrophobic excipient but are substantially free of any therapeutically active ingredient. The active ingredient in the first spray-dried powder is loaded sufficiently high to compensate for the second spray-dried powder being substantially free of any active ingredient. A process for preparing such formulations is also described.