Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
Type:
Application
Filed:
April 10, 2018
Publication date:
August 16, 2018
Inventors:
Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
Abstract: Disclosed are solid state forms of Eluxadoline, processes for their preparations, compositions comprising them and their medical use. The present invention also encompasses solid state forms of Eluxadoline for use in the preparation of other solid state forms of Eluxadoline, particularly form alpha.
Abstract: In one aspect, the invention relates to a compound of the structure: or a pharmaceutically acceptable salt thereof, and a crystalline form of this compound, having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising this compound; methods of using this compound; and processes for preparing this compound.
Type:
Application
Filed:
December 14, 2017
Publication date:
August 16, 2018
Applicant:
THERAVANCE BIOPHARMA R&D IP, LLC
Inventors:
Melissa Fleury, Adam D. Hughes, Anne-Marie Beausoleil, Erik Fenster, Venkat R. Thalladi, Miroslav Rapta
Abstract: The present invention provides a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof or a solvate of these. A compound having Nrf2 activation ability is provided by the present invention.
Abstract: Disclosed herein are methods of treating conditions, which may be associated with elevated levels of eosinophils and/or basophils, with a therapeutically effective amount of dexpramipexole or pharmaceutical acceptable salt thereof.
Type:
Application
Filed:
February 6, 2018
Publication date:
August 16, 2018
Inventors:
Michael E. BOZIK, Gregory HEBRANK, Thomas PETZINGER, JR., Steven DWORETZKY, Wildon FARWELL
Abstract: Compositions comprising S1P receptor modulators and at least one compound selected from one or more of the group consisting of steroids, opioids and non-steroidal anti-inflammatory drugs are provided. The compositions find use in the treatment of disease, particularly inflammation and immune mediated disorders.
Abstract: A modified release composition comprising tacrolimus releases less than 20% w/w of the active ingredient within 0.5 hours when subjected to an in vitro dissolution test using USP Paddle method and using 0.1 N HCl as dissolution medium and has increased bioavailability by effectively reducing or even avoiding the effects of CYP3A4 metabolism. The modified composition may be coated with an enteric coating; and/or may comprise a solid dispersion or a solid solution of tacrolimus in a hydrophilic or water-miscible vehicle and one or more modifying release agents; and/or may comprise a solid dispersion or a solid solution of tacrolimus in an amphiphilic or hydrophobic vehicle and optionally one or more modifying release agents.
Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
Type:
Application
Filed:
August 3, 2016
Publication date:
August 16, 2018
Inventors:
Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
Abstract: 6-Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a 6-azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
Type:
Application
Filed:
August 3, 2016
Publication date:
August 16, 2018
Inventors:
Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
Abstract: 6-Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a 6-azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
Type:
Application
Filed:
August 3, 2016
Publication date:
August 16, 2018
Inventors:
Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
Abstract: 7-Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a 7-azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
Type:
Application
Filed:
August 3, 2016
Publication date:
August 16, 2018
Inventors:
Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
Abstract: 4-Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a 4-azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
Type:
Application
Filed:
August 3, 2016
Publication date:
August 16, 2018
Inventors:
Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
Abstract: 4-Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a 4-azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
Type:
Application
Filed:
August 3, 2016
Publication date:
August 16, 2018
Inventors:
Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
Abstract: Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting HPK1 activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer.
Type:
Application
Filed:
February 14, 2018
Publication date:
August 16, 2018
Inventors:
Alexander Sokolsky, Oleg Vechorkin, Kai Liu, Jun Pan, Wenqing Yao, Qinda Ye
Abstract: Motor skill deficits and cognitive deficits associated with stroke and secondary neuronal cell death are ameliorated by treatment with pharmaceutically acceptable salts of 2-amino substituted nicotinamides.
Abstract: The invention provides treating cachexia and eating disorders in humans and veterinary animals by administering a composition including: (i) cyproheptadine (CYP); and (ii) a cannabis compound selected from the group of cannabidiol (CBD) and mixtures of CBD and up to 50% tetrahydrocannabinol (THC).
Abstract: This disclosure provides a dosage regimen for co-administration of 4-[7-[6-cyano-5-(trifluoromethyl)pyridin-3-yl]-8-oxo-6-sulfanylidene-5,7-diazaspiro[3.4]octan-5-yl]-2-fluoro-N-methylbenzamide and a strong CYP3A4 inducer.
Type:
Application
Filed:
August 11, 2016
Publication date:
August 16, 2018
Inventors:
Jacqueline GIBBONS, Joyce MORDENTI, Michiel DE VRIES, Walter KRAUWINKEL
Abstract: This invention relates to compounds that are agonists of the muscarinic M4 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1a or a salt thereof, wherein n, p, Q, R1, R2, R3, R9 and R4 are as defined herein.
Type:
Application
Filed:
August 3, 2016
Publication date:
August 16, 2018
Inventors:
Giles Albert Brown, Miles Stuart Congreve, Mark Pickworth, Mark Rackham, Benjamin Gerald Tehan
Abstract: The invention pertains to methods that include administering to a subject a transoral dosage form comprising a pharmaceutical carrier and sufentanil, and maintaining a mean pH ranging from about 3.5 to about 5.5 during a dosing period after administration of the transoral dosage form as determined using an in vitro donor media test. Related dosage forms are also disclosed. Also disclosed are transoral dosage forms and related methods, wherein a transoral dosage form may comprise: (1) about 5 to about 1000 micrograms of sufentanil; (2) about 50 micrograms to about 100 milligrams of naloxone; and (3) acidifying material in an amount sufficient to provide a mean pH ranging from about 3.5 to about 5.
Type:
Application
Filed:
January 12, 2018
Publication date:
August 16, 2018
Applicant:
Durect Corporation
Inventors:
Su Il Yum, Jaymin Shah, Sung Yun Kwon, Xiaoping Song
Abstract: A nicotine lozenge provided herein includes a body that is partially or wholly receivable in an oral cavity. The body includes a soluble-fiber matrix and nicotine or a derivative thereof dispersed in the soluble-fiber matrix. In some cases, a nicotine lozenge provided herein includes at least 40 weight percent of soluble fiber. In some cases, soluble fiber in a nicotine lozenge provided herein can include maltodextrin. The nicotine lozenge is adapted to release the nicotine or a derivative thereof from the body when the body is received within the oral cavity of an adult consumer and exposed to saliva. A method of making nicotine lozenges provided herein includes forming a molten mixture of at least 40 weight percent soluble fiber, nicotine, and less than 15 weight percent water while maintaining a mixture temperature of less than 150° C. and portioning the molten mixture into a plurality of nicotine lozenges. In some cases, the ingredients can be mixed to form the molten mixture in an extruder.
Type:
Application
Filed:
April 16, 2018
Publication date:
August 16, 2018
Inventors:
Feng Gao, Diane L. Gee, Phillip M. Hulan, Shuzhong Zhuang, William J. Burke
Abstract: The present invention provides a method of treating squamous histology cancers, breast cancer, prostate cancer, bladder cancer, cervical cancer, endometrial cancer, ovarian cancer, and colorectal cancer in a patient comprising administering to a patient in need of such treatment an effective amount of a compound of the formula: or a pharmaceutically acceptable salt thereof; in combination with an effective amount of a compound of the formula: or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
December 8, 2016
Publication date:
August 16, 2018
Inventors:
Richard Paul Beckmann, Gregory Paul Donoho, Aimee Karis Lin, Volker Wacheck
Abstract: Provided herein are methods and compositions for effective treatment or prevention of pain, which also reduce or eliminate adverse effects associated with an opioid analgesic. In addition, provided herein are methods and compositions for treatment or prevention of pain, and for reducing or preventing retching in a subject. Also provided herein are methods and compositions for treatment or prevention of pain, and for reducing or preventing sleep disturbances. Also provided herein are methods and compositions for treatment or prevention of pain, and for reducing or preventing a sensory or affective quality associated with the pain, such as agonizing pain, in a subject. Compositions described herein may include an opioid analgesic and an antiemetic. Compositions described herein may further include a non-opioid analgesic.
Type:
Application
Filed:
April 11, 2018
Publication date:
August 16, 2018
Inventors:
Paul BOSSE, John AMELING, Bernard SCHACHTEL, William KOZAREK
Abstract: The present invention relates to a gastro-resistant pharmaceutical composition comprising a solid solution prepared by hot-melt extrusion, whereby the solid solution contains posaconazole, an enteric polymer and a non-enteric polymer. The composition is preferably a granulate material that can be filled into a capsule or compressed into a tablet.
Abstract: Methods for treating neurological or mental disorders in humans and the symptoms associated therewith are provided by administering eltoprazine and/or related compounds. In some embodiments, specific symptoms are treated by administering eltoprazine and/or a related compound in an effective amount to ameliorate the symptoms. Of particular significance are symptoms that are associated with cognitive dysfunction where eltoprazine will improve the symptoms and the disorder associated with that symptom. Of particular interest are non-ADHD-associated inattention, hyperactivity and impulsiveness. The methods provided herein are especially useful for improving functional recovery after CNS injury such as stroke where improved cognitive function will facilitate the acquisition of learning and memory of rehabilitative tasks.
Abstract: The present invention concerns combinations of a pyrimidine containing NNRTI with nucleoside reverse transcriptase inhibitors and nucleotide reverse transcriptase inhibitors useful for the treatment of HIV infected patients or for the prevention of HIV transmission or infection.
Abstract: A method for enhancing learning ability and memory of patients with Alzheimer's disease using mocetinostat is provided. The method includes administering an effective dose of mocetinostat into a subject in need. Based on the administration of mocetinostat, A? accumulation, Tau protein phosphorylation, and neuroinflammation can be reduced, and the level of synaptophysin and numbers of serotonergic neuron can be increased. Hence, the damage caused by the injection of oligomeric A?25-35 within hippocampal CA1 is relieved. The method may be a potential solution for relieving the symptoms of anxiety and cognitive impairment.
Abstract: The present invention relates to 5-bromo-2,6-di-(1H-pyrazol-1-yl)pyrimidin-4-amine, its pharmaceutically acceptable salts and co-crystals thereof and to pharmaceutical compositions comprising said compounds for use in the treatment of cancer.
Type:
Application
Filed:
August 10, 2016
Publication date:
August 16, 2018
Applicants:
NOVARTIS AG, PALOBIOFARMA, S.L.
Inventors:
Sanela BILIC, Juan Alberto CAMACHO GOMEZ, John Scott CAMERON, Julio Cesar CASTRO-PALOMINO LARIA, Danny Roland HOWARD, Jr.
Abstract: The present invention relates to compounds according to Formula (I): or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof wherein X1, X2, R1, R2, R3 and n are as defined herein. Also described are pharmaceutically acceptable compositions of Formula (I) compounds as well as methods for utilizing the compounds of Formula (I) and the pharmaceutically acceptable compositions of Formula (I) compounds as inhibitors of Mnk as well as therapeutics for the treatment of diseases such as cancer.
Type:
Application
Filed:
February 13, 2018
Publication date:
August 16, 2018
Inventors:
Justin T. ERNST, Paul A. SPRENGELER, Siegfried H. REICH, Samuel SPERRY
Abstract: The invention provides a composition comprising an inhibitor of Na+-taurocholate cotransporting polypeptide (NTCP) and a active ingredient selected from the group consisting of a nucleoside analogue such as lamivudine, telbivudine, or entecavir, a nucleotide analogue such as tenofovir, adefovir and an immunomodulator such as interferon alpha. The NTCP inhibitor inhibits HBV/HDV entry into a cell and is preferably derived from an HBV pre-S1 peptide. Also provided are methods of treating HBV and HDV infection, hepatitis B and D, or chronic hepatitis B and D.
Abstract: The invention relates to fungicides and can be used for treating diseases caused by fungi, and also for preventing fungal damage to various materials and agricultural products. Claimed is an agent against fungal infections which is in the form of salts of 2,4-dioxo-5-arylideneamino-6-methyl-1,3-pyrimidine, where R is 4-NO2, 2-OH-5-NO2, 2-OH-3,5-Cl2, 5-Br-4-OH-3-OCH3, 2-OH-5-Cl, 2,4-Cl2, 3,5-Br2-2-OH. The result is an agent against fungal infections which has a broad spectrum of activity and is highly soluble, rendering it more effective for use in the form of solutions.
Type:
Application
Filed:
August 1, 2016
Publication date:
August 16, 2018
Inventors:
Viktor Veniaminovich Tets, Georgy Viktorovich Tets
Abstract: The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TR? mutation.
Abstract: Use of H3K9me3 modulation for enhancing cognitive function and treating anxiety related disorders is presented. A composition is administered to the subject comprising a therapeutically effective amount of a SUV39H1 inhibitor comprising analogs of ETP69. The therapeutically effective amount is effective in treating cognitive dysfunction in aging and age-related disorders.
Type:
Application
Filed:
June 3, 2016
Publication date:
August 16, 2018
Inventors:
Carl W. COTMAN, Larry E. OVERMAN, Shikha SNIGDHA
Abstract: The present invention is directed to nanoparticulate compositions comprising meloxicam particles having an effective average particle size of less than about 2000 nm.
Type:
Application
Filed:
April 11, 2018
Publication date:
August 16, 2018
Inventors:
Eugene R. Cooper, Tuula Ryde, John Pruitt, Laura Kline
Abstract: The present invention is directed to nanoparticulate compositions comprising meloxicam particles having an effective average particle size of less than about 2000 nm.
Type:
Application
Filed:
April 11, 2018
Publication date:
August 16, 2018
Inventors:
Eugene R. Cooper, Tuula Ryde, John Pruitt, Laura Kline
Abstract: Methods and compositions for glial cell-derived neurotrophic factor (GDNF) induction in the eye, and for treatment and/or prevention of retinal disorders are described.
Type:
Application
Filed:
December 11, 2015
Publication date:
August 16, 2018
Inventors:
Dwight M. Morrow, Kathryn L. McCabe, Hong Lin, Petr Y. Baranov, Michael J. Young
Abstract: The present disclosure provides oral dosage forms comprising a cephalotaxine and a pharmaceutically acceptable carrier selected from protein, carbohydrate and lipid, an oral dosage form comprising cephalotaxine and a second active agent, as well as methods of treating subjects with such oral formulations.
Abstract: Disclosed herein are compositions for lowering intraocular pressure (IOP) of an eye comprising a combination IOP-lowering agents bimatoprost, brimonidine, and timolol. Further disclosed are methods for reducing IOP in the eye of a subject.
Abstract: The present invention resides in the surprising discovery of the previously unrecognized synergistic effects resulted from combined use of narigenin and asiatic acid. New methods and compositions are therefore provided for the treatment or prevention of various types of cancer.
Abstract: The present disclosure is drawn to pharmaceutical compositions and oral dosage capsules containing testosterone undecanoate, as well as related methods. The capsule includes a capsule shell and a capsule fill. The capsule fill can include a solubilizer and about 14 wt % to about 35 wt % testosterone undecanoate based on the total capsule fill. The oral dosage capsule is such that when a single oral administration to a male subject of one or more capsules with a total testosterone undecanoate daily dose of about 350 mg to about 650 mg it provides a ratio of serum testosterone Cmax to serum testosterone Cave of about 2.7 or less. In yet another embodiment, a method for providing a serum concentration of testosterone within a target serum testosterone concentration Cave range for a male subject is provided.
Abstract: The present disclosure is drawn to pharmaceutical compositions and oral dosage capsules containing testosterone undecanoate, as well as related methods. The capsule includes a capsule shell and a capsule fill. The capsule fill can include a solubilizer and about 14 wt % to about 35 wt % testosterone undecanoate based on the total capsule fill. The oral dosage capsule is such that when a single oral administration to a male subject of one or more capsules with a total testosterone undecanoate daily dose of about 350 mg to about 650 mg it provides a ratio of serum testosterone Cmax to serum testosterone Cave of about 2.7 or less. In yet another embodiment, a method for providing a serum concentration of testosterone within a target serum testosterone concentration Cave range for a male subject is provided.
Abstract: The present invention is based on the unexpected discovery that a combination of certain known drugs exhibits synergistic effects in treating metabolic syndrome and various other diseases. In particular, the invention comprises a pharmaceutical composition comprising: (1) a therapeutically effective quantity of a first agent that is Metformin or a salt thereof; (2) a therapeutically effective quantity of a second agent that is Aspirin; (3) a therapeutically effective quantity of a third agent that serotonin creatinine sulfate complex; (4) a non-ionic surfactant; and (5) a solvent that is a lower alkanol. A preferred composition comprises metformin hydrochloride, aspirin, and serotonin creatinine sulfate complex for the first, second, and third agents. The invention further comprises methods for the use of these compositions for the treatment of metabolic syndrome, hyperproliferative diseases including cancer, and other diseases and conditions.
Abstract: The invention provides compositions comprising choline and water soluble derivatives thereof, processes for their preparation and uses thereof.
Type:
Application
Filed:
April 21, 2015
Publication date:
August 16, 2018
Applicant:
ENZYMOTEC LTD.
Inventors:
Asher WIDBERG, Ran NUMA, Gai BEN-DROR, Fabiana BAR-YOSEPH, Itay SHAFAT
Abstract: Oral dosage forms of osteoclast inhibitors, such as zoledronic acid, in an acid or a salt form can be used to treat or alleviate pain or related conditions, such as arthritis.
Abstract: Oral dosage forms of osteoclast inhibitors, such as zoledronic acid, in an acid or a salt form can be used to treat or alleviate pain or related conditions, such as osteoarthritis.