Abstract: Disclosed is an in vitro screening method for identifying an antagonist-to-agonist allosteric modifier of a mu-opioid receptor and an in vivo method for confirming that a test compound is such a modifier of a mu-opioid receptor. Also disclosed is a method for treating an opioid receptor-associated condition using a compound of Formula (I) and a pharmaceutical composition containing the same.
Abstract: An object of the present invention is to provide a cancer cell inhibitory drug, particularly a cancer stem-cell inhibitory drug, or a cancer stem-cell detection probe.A cancer cell inhibitory drug containing at least a compound represented by general formula (1).
Abstract: Method of using dopamine reuptake inhibitors, e.g., sydnonimine derivatives, for the management of diabetic symptoms and associated complications or conditions, such as hyperglycemia and diabetic neuropathy.
Type:
Application
Filed:
November 14, 2016
Publication date:
March 2, 2017
Inventors:
Hao Chen, Ming Liu, Malathi Sathyamoorthy, Qi Su, Lisa Leary, Wayne Shaobin Zhong
Abstract: Methods and compounds for research and treatment of portal hypertension. The use of racemic or non-racemic mixtures of furopyridine isomers to stimulate eNOS function in sinusoidal endothelial cells and to increase NO production in both normal sinusoidal endothelial cells and injured endothelial cells.
Type:
Application
Filed:
November 10, 2016
Publication date:
March 2, 2017
Inventors:
Don C. Rockey, Songling Liu, Glenn Cornett
Abstract: The present invention relates to treatments and therapies for anemia conditions and diseases of the blood, and more particular is a therapy for the acute and chronic treatment of sickle cell diseases and thalassemia by administration of pyridoxamine, or a pharmaceutically acceptable salt thereof, optionally in combination with an additional bioactive agent.
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:
September 8, 2016
Publication date:
March 2, 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 the treatment of Herpes simplex virus lesion pain via application of a product containing a quick acting and long acting topical anesthetic.
Abstract: Described herein are dosing regimens and kits for the treatment and/or prevention of lysosomal storage disorders such as Gaucher disease. Also described are dosing regimens and kits for the treatment and/or prevention of degenerative disorders of the central nervous system, such as the synucleinopathies Parkinson's disease or Lewy Body Dementia.
Abstract: Disclosed herein are methods and compositions related to use of aminopyridines, such as 4-aminopyridine, to prove the neuro-cognitive impairments and related neuro-psychiatric impairments of patients with a demyelinating condition such as MS, traumatic brain injury, cerebral palsy, post-radiation encephalopathy.
Abstract: The present invention is directed to a nail lacquer consisting essentially of ciclopirox as an antimycotic agent, hydroxypropyl chitosan as film forming agent, water and a lower alkanol as solvent. The invention is also directed to such a nail lacquer for use in treating onychomycosis.
Abstract: This invention relates to 4-{[4-({([4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]-oxy}methyppiperidin-1-yl]methyl}tetrahydro-2H-pyran-4-carboxylic acid for use in therapeutic treatment of the human body. In particular, it relates to the compound having selective 5-HT4 receptor agonism, which is useful for treating gastroparesis, or preventing or delaying the onset or the progression of gastroparesis.
Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
Type:
Application
Filed:
September 6, 2016
Publication date:
March 2, 2017
Inventors:
Brian K. Albrecht, James Edmund Audia, Andrew Cook, Les A. Dakin, Martin Duplessis, Victor S. Gehling, Jean-Christophe Harmange, Christopher G. Nasveschuk, Rishi G. Vaswani
Abstract: The present disclosure is generally directed to compositions and methods for treating apicomplexan protozoan related disease, such as toxoplasmosis and cryptosporidiosis.
Type:
Application
Filed:
November 15, 2016
Publication date:
March 2, 2017
Inventors:
Erkang FAN, Wesley C. VAN VOORHIS, Zhongsheng ZHANG, Wenlin HUANG, Kayode K. OJO
Abstract: The present invention discloses a method of treating cancer and/or multidrug-resistant cancer, comprising administering an effective amount of hernandezine or thalidezine. A pharmaceutical composition comprising hernandezine or thalidezine admixed with a pharmaceutical carrier for treating cancers and/or multidrug-resistant cancer is also disclosed.
Abstract: The invention relates to a composition comprising buprenorphine and a ? opioid receptor antagonist, wherein the composition is characterized by an Agonist Antagonist Activity Index (AAnAI) of between about 0.7 and about 2.2; wherein; AAnAI = [ C max ? ( BUP ) / EC 50 ] [ C max ? ( ANTAGONIST ) / IC 50 ] .
Abstract: A method of effectively treating pain in humans is achieved by administering buprenorphine in accordance with first order kinetics over an initial three-day dosing interval, such that a maximum plasma concentration from about 20 pg/ml to about 1052 pg/ml is attained, and thereafter maintaining the administration of buprenorphine for at least an additional two-day dosing interval in accordance with substantially zero order kinetics, such that the patients experience analgesia throughout the at least two-day additional dosing interval.
Type:
Application
Filed:
November 15, 2016
Publication date:
March 2, 2017
Inventors:
Robert F. Reder, Paul D. Goldenheim, Robert F. Kaiko
Abstract: The disclosure is directed to a method of easing a patient's symptoms related to termination of opioid pain therapy, and compositions for achieving said method. The method and compositions comprise a series of self tapering dosages of a pharmaceutical composition that is configured to alleviate or prevent symptoms of the patient's termination of opioid pain therapy. The series of self tapering dosages may be supplied in a dosage package.
Abstract: The embodiments described herein include methods and formulations for treating lung and brain injury. The methods and formulations include, but are not limited to, methods and formulations for delivering effective concentrations of levocetirizine and montelukast to a patient in need. The methods and formulations can comprise conventional and/or modified-release elements, providing for drug delivery to the patient.
Abstract: Novel anticoagulant reversal compounds are disclosed, as well as methods of making the compounds, pharmaceutical compositions including the compounds, methods of using the compounds to reverse the anticoagulant effects of coagulation inhibitors, and diagnostic assays comprising the compounds.
Type:
Application
Filed:
November 10, 2016
Publication date:
March 2, 2017
Inventors:
Solomon S. Steiner, Bryan E. Laulicht, Sasha H. Bakhru, Edith Mathiowitz
Abstract: The invention relates to Histamine H4 receptor antagonists or inhibitors of Histamine H4 receptor gene expression for the treatment and/or the prevention of vestibular disorders.
Abstract: Methods of treating diseases associated with P2X3 and/or a P2X2/ with compounds formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, R1, R2, R3, R4, R5, R6 and R7 are as defined herein.
Type:
Application
Filed:
November 9, 2016
Publication date:
March 2, 2017
Applicant:
Roche Palo Alto LLC
Inventors:
Li Chen, Michael Patrick Dillon, Lichun Feng, Minmin Yang
Abstract: Biocompatible intraocular implants may include a brimonidine free base and a biodegradable polymer associated with the brimonidine free base to facilitate the release of the brimonidine free base into an eye with the polymer matrix lasts a period of time of not more than twice the drug release duration, but more than the drug release duration.
Abstract: The present disclosure relates to the use of a p75 receptor antagonist or its pharmaceutically acceptable salts for the preparation of a medicament for use in the treatment and/or prevention of overactive bladder.
Type:
Application
Filed:
August 10, 2016
Publication date:
March 2, 2017
Inventors:
Roberta AVALLONE, Marco BARONI, Tiziano CROCI
Abstract: A stable multi-particulate pharmaceutical composition comprising pellets, the pellets comprising a mixture of rosuvastatin or its pharmaceutically acceptable salts as a sole active ingredient, one or more osmotic release modifiers and one or more stabilizers.
Type:
Application
Filed:
February 12, 2016
Publication date:
March 2, 2017
Applicant:
SUN PHARMA ADVANCED RESEARCH COMPANY LTD.
Abstract: Disclosed are methods whereby an effective amount of a HDAC6 inhibitor is used to activate a subjects T-cell response to tumor or tumor vaccine. Methods of using HDAC6 inhibitors to increase a subjects anti-tumor immune response, alone or in conjunction with other tumor treatments, are also disclosed.
Type:
Application
Filed:
April 6, 2015
Publication date:
March 2, 2017
Applicant:
H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.
Inventors:
Eduardo M. Sotomayor, Alejandro V. Villagra
Abstract: The present disclosure relates to the use of GnRH receptor antagonists used in the treatment of endometriosis or uterine fibroids. In particular, the present disclosure describes a method of treating endometriosis or uterine fibroids, where the method involves the administration of elagolix, and where the method may further involve the co-administration of rifampin or ketoconazole.
Type:
Application
Filed:
September 1, 2016
Publication date:
March 2, 2017
Inventors:
Sandra L. Goss, Cheri E. Klein, Juki Wing-Keung Ng, Ahmed Salem
Abstract: The present disclosure relates to a method of treating cancer using a composition comprising Nelfinavir, Metformin, Rosuvastatin, optionally along with a pharmaceutically acceptable excipient. The said composition is used for the treatment of cancer caused due to aberration in PTEN gene, optionally along with aberration in TP53 gene and related genes selected from group comprising PI3K, CDKN2A, MDM2 and MDM4.
Abstract: The present disclosure relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present disclosure provides compounds as therapeutic agents against bacterial infections (e.g., biofilms). The present disclosure also provides compounds as therapeutic agents in methods for treating pneumonia, methods for reducing bacterial virulence, methods for treating a bacterial wound infection, and methods for treating a urinary tract infection. The present disclosure also provides methods for treating a bacterial infection, wherein the bacterial infection has or is suspected of having an antibiotic-resistant bacteria. The present disclosure also provides surfaces coated with the chemical compounds disclosed herein.
Type:
Application
Filed:
October 26, 2016
Publication date:
March 2, 2017
Inventors:
Hongmin Sun, David W. Anderson, Lianhai Li
Abstract: A method for the treatment of cancer by administering a therapeutically effective amount of a cyclin-dependent kinase (CDK) inhibitor with a therapeutically effective amount of a B cell chronic lymphocytic leukemia/lymphoma 2 inhibitor (“B Cell CLL/Lymphoma 2”, or “BCL-2”). Administration of the CDK inhibitor and BCL-2 inhibitor can be simultaneous, successive or separate.
Abstract: A risperidone sustained release microsphere formulation is provided. The microsphere formulation includes risperidone or 9-hydroxy risperidone or salts thereof, and a polymer blend having a first uncapped lactide-glycolide copolymer and a second uncapped lactide-glycolide copolymer, in which the first uncapped lactide-glycolide copolymer is a copolymer with a high intrinsic viscosity and the second uncapped lactide-glycolide copolymer is a copolymer with a low intrinsic viscosity. The sustained release micro sphere formulation according to an embodiment of the present disclosure is suitable for large-scale industrialized production with improved stability, the in vivo release behavior of which will not change after long-term storage.
Abstract: The invention provides a method for treatment of the diseases in a human by identifying the human as one suffering from a herpes simplex virus (HSV), and then administering to the human the compound anti-HSV agent or a pharmaceutically acceptable salt thereof. The diseases include dermatosis and non-dermatosis, wherein the dermatosis include acnes, impetigo, pyoderma gangrenosum, chilblains and psoriasiform, asteatotic dermatitis, ichthyosis, lichen simplex chronicus (Neurodermatitis, Prurigo), seborrhoeic dermatitis, rosacea, perioral dermatitis, epidermal cyst, wound ulcer, discoid lupus erythematosus, vitiligo, Alopecia, diagnostic criteria of some autoimmune diseases such as systemic lupus erythematosus or diabetic skin complications, wherein the non-dermatosis include glomerulonephritis, arthritis, Crohn's disease, ulcerative colitis, myelodysplasia, multiple myeloma, demyelinating disease, Parkinson's disease, anemia, cytopenia those among the diagnostic criteria.
Abstract: Provided herein are compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, R1, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is a 6-membered monocyclic heteroaryl ring system of formula: wherein L2, R13, G8, G10, G11, and G12 are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described.
Type:
Application
Filed:
April 7, 2016
Publication date:
March 2, 2017
Applicant:
Epizyme, Inc.
Inventors:
Richard Chesworth, Oscar Miguel Moradei, Gideon Shapiro, Lei Jin, Robert E. Babine
Abstract: The present invention relates generally to compositions and methods for treating diseases and disorders caused by herpes simplex virus type 1, including herpes simplex keratitis, in a subject. In certain embodiments, the compositions of the present invention comprise an ATM inhibitor and an anti-herpetic agent. In other embodiments, the compositions comprise a Chk2 inhibitor and an anti-herpetic agent. In yet other embodiments, the compositions comprise a Chk2 inhibitor and an ATM inhibitor, and optionally an anti-herpetic agent.
Type:
Application
Filed:
November 9, 2016
Publication date:
March 2, 2017
Inventors:
Jane E. CLIFFORD, Oleg ALEKSEEV, Stephen R. JENNINGS
Abstract: Controlled-release preparations of oxcarbazepine and derivatives thereof for once-a-day administration are disclosed. The inventive compositions comprise solubility- and/or release enhancing agents to provide tailored drug release profiles, preferably sigmoidal release profiles. Methods of treatment comprising the inventive compositions are also disclosed.
Type:
Application
Filed:
May 27, 2016
Publication date:
March 2, 2017
Applicant:
Supernus Pharmaceuticals, Inc.
Inventors:
Padmanabh P. BHATT, Argaw KIDANE, Kevin EDWARDS
Abstract: Prostamide-containing intraocular implants that biodegrade in the eye and that are effective for reducing intraocular pressure in an eye for a sustained period. The implants generally contain a prostamide, such as bimatoprost, and at least three distinct biodegradable polymers selected from polylactide and poly(lactide-co-glycolide) polymers and are optimized for placement in and compatibility with the anterior chamber of the eye, particularly the anterior chamber angle. Methods for making and using the implants to reduce ocular hypertension and intraocular pressure in a patient are described.
Type:
Application
Filed:
November 14, 2016
Publication date:
March 2, 2017
Inventors:
Alazar N. Ghebremeskel, Michael R. Robinson
Abstract: The present invention provides methods of identifying compounds that selectively induce an oxidative stress response in a biological sample. The present invention further provides methods of treating a subject having a disease associated with oxidative stress using compounds that selectively induce an oxidative stress response in the subject. The invention further provides methods of selectively inducing an oxidative stress response in a cell.
Type:
Application
Filed:
August 25, 2016
Publication date:
March 2, 2017
Inventors:
Jareer Nabeel Kassis, Otis Clinton Attucks, Matthew J. Kostura
Abstract: Certain embodiments are directed to methods and compositions for treating obesity, diabetes, and/or cancer with a combination of ursolic acid and resveratrol.
Type:
Application
Filed:
May 5, 2015
Publication date:
March 2, 2017
Inventors:
Thomas J. SLAGA, Jacob JUNCO, Huiyun LIANG, Sara REYNA
Abstract: Disclosed are bioavailable solid state (17-?)-Hydroxy-4-Androsten-3-one esters suitable for pharmaceutical uses and administration to mammals in need of (17-?)-Hydroxy-4-Androsten-3-one.
Type:
Application
Filed:
September 26, 2016
Publication date:
March 2, 2017
Inventors:
Mahesh V. Patel, Nachiappan Chidambaram, Satish Kumar Nachaegari, Srinivasan Venkateshwaran, Joel Frank
Abstract: The present invention provides the steroidal compound 3?-ethynyl-3?-hydroxyandrostan-17-one oxime, or a pharmaceutically acceptable salt thereof, for use in treatment of hepatic encephalopathy.
Type:
Application
Filed:
November 15, 2016
Publication date:
March 2, 2017
Inventors:
Magnus Doverskog, Hanns Möhler, Vicente Felipo, Torbjörn Bäckström
Abstract: The invention relates to a method for scheduling ovulation in a female subject, which method comprises administering ulipristal acetate (UPA) to the female subject during the follicular phase.
Abstract: Certain bile acids, including novel bile acids, and derivatives thereof can be used to inhibit the germination of C. difficile spores and/or the growth of C. difficile cells. The methods and compositions of the invention are useful for preventing and treating C. difficile-associated diseases, including but not limited to C. difficile colitis.
Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: with X selected from C4-8 cycloalkyl, C4-8 cycloalkenyl, C4-9 spirocycloalkyl, C4-9 spirocycloalkenyl, C4-8 oxacycloalkyl, C4-8 dioxacycloalkyl, C6-8 oxacycloalkenyl, C6-8 dioxacycloalkenyl, C6 cyclodialkenyl, C6 oxacyclodialkenyl, C6-9 oxaspirocycloalkyl and C6-9 oxaspirocycloalkenyl ring, such that X is substituted with A, wherein A is —C1-6 alkyl-halo. These compounds are useful for the treatment of HIV and AIDS.
Type:
Application
Filed:
November 7, 2016
Publication date:
March 2, 2017
Inventors:
Sing-Yuen SIT, Yan CHEN, Jie CHEN, Jacob SWIDORSKI, Brian Lee VENABLES, Ny SIN, Nicholas A. MEANWELL, Alicia REGUEIRO-REN, Richard A. HARTZ, Li XU, Zheng LIU
Abstract: The present disclosure provides compositions and methods for selectively killing senescent cells, wherein the selective killing of senescent cells delays aging and treats age-related disorders.
Abstract: The present disclosure provides for methods of addressing the devastating effects of malaria infection by mosquito-borne Plasmodium parasites. The methods include the administration of an effective amount of at least one pro-apoptotic agent and the administration of an effective amount of at least one p53 activator. The at least one pro-apoptotic agent can be administered concurrently with, prior to, or subsequent to the at least one p53 activator. The at least one pro-apoptotic agent and/or at least one p53 activator can be administered concurrently with, prior to, or subsequent to exposure of a hepatocyte (in vivo or in vitro) by a Plasmodium parasite. In some embodiments, the administration of the at least one pro-apoptotic agent combined with the administration of the at least one p53 activator results in clearance of hypnozoite stage of P. vivax or P. ovale, and thus prevents relapse of symptoms and disease from the infection of these parasites.
Type:
Application
Filed:
May 7, 2015
Publication date:
March 2, 2017
Applicant:
Seattle Biomedical Research Institute
Inventors:
Alexis Kaushansky, Stefan H.I. Kappe, Alyse N. Douglass, Heather S. Kain
Abstract: The use of the hemifumarate form of {9-[(R)-2-[[(S)-[[(S)-1-(isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine} (tenofovir alafenamide hemifumarate) in combination with cobicistat is disclosed. In addition, the combination of tenofovir alafenamide hemifumarate, cobicistat, emtricitabine, and elvitegravir, and the combination of tenofovir alafenamide hemifumarate, cobicistat, emtricitabine, and darunavir, are disclosed.
Abstract: Therapeutic compositions comprising substituted imidazole or imidazolium compounds may be used for a number of medical purposes, such as treatment of undesirable conditions or diseases, including disease or conditions related to bone, cancer, and/or pain such as complex regional pain syndrome.
Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions such as complex regional pain syndrome.