Patents Issued in August 2, 2018
  • Development of Dietary Therapy in Cancer
    Publication number: 20180214410
    Abstract: The invention provides new compositions or combinations thereof for the treatment of cancer. More specifically, the invention provides compositions or combinations thereof for cancer treatment including a high-fat diet. Specifically, the high-fat diet is characterized by having approximately 120 g/day or more, or approximately 70% or more of the total daily energy, from fat, based on a real body weight of 50 kg. The diet is preferably a carbohydrate-restricted high-fat diet, and more preferably provided by a ketone formula and/or MCT oil. The dietary therapy by a high-fat diet of the present invention is provided along with surgical treatment, chemotherapy or radiation therapy, or combinations thereof.
    Type: Application
    Filed: September 2, 2016
    Publication date: August 2, 2018
    Inventors: Keisuke Hagihara, Kinya Ashida, Hidekazu Tonouchi, Kentaro Nakamura
  • COMPOSITION COMPRISING SATIETY-INDUCING PARTICLES
    Publication number: 20180214411
    Abstract: The invention provides a pharmaceutical or food composition comprising ingestible particles with a water-swellable or water-soluble polymeric material a lipid material; and optionally an amino acid, a vitamin, a micro-nutrient or any combination thereof. The polymeric material may be embedded in the lipid material. The particle may further comprise an inert core and/or an outer layer which rapidly disintegrates after oral ingestion. The composition comprises at least one further component, such as a source of protein, dietary fibre, dietary minerals or trace elements, or vitamins.
    Type: Application
    Filed: July 7, 2016
    Publication date: August 2, 2018
    Inventor: Dirk VETTER
  • IMMEDIATE RELEASE CANNABINOID FORMULATIONS
    Publication number: 20180214412
    Abstract: The present invention relates to immediate release pharmaceutical compositions comprising one or more natural or synthetic cannabinoids, and one or more pharmaceutically acceptable excipients. More specifically, the invention relates to immediate release pharmaceutical compositions comprising cannabinoids and a process for preparation thereof.
    Type: Application
    Filed: January 23, 2018
    Publication date: August 2, 2018
    Inventors: Jeff Renwick, Robert Scott Lefler
  • Small Molecule Agonists and Antagonists of NR2F6 Activity in Humans
    Publication number: 20180214413
    Abstract: The present technology is directed to modulators of nuclear receptor activity, specifically to the modulation of NR2F6 activity and NR2F6 utilizing compounds, and the immune modulation and modulation of cancer stem cell activity through administration of compounds described herein to humans.
    Type: Application
    Filed: November 21, 2017
    Publication date: August 2, 2018
    Inventors: Harry M. Lander, David R. Koos
  • COMPOSITIONS AND METHODS FOR TREATING ESTROGEN-RELATED MEDICAL DISORDERS
    Publication number: 20180214414
    Abstract: Disclosed herein are methods for treatment of estrogen-related medical disorders. The methods of treatment may comprise administering to a subject in need of such treatment a composition comprising a therapeutically effective amount of at least one compound of formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: January 31, 2018
    Publication date: August 2, 2018
    Inventors: Gregory R. Thatcher, Debra Tonetti, Mary Ellen Molloy, Bradley Michalsen, Zihui Qin
  • TREATMENT METHOD UTILIZING PYRROLIDINE-2, 5-DIONE DERIVATIVES AS IDO1 INHIBITORS
    Publication number: 20180214415
    Abstract: Uses of compound of Formula I: or pharmaceutically acceptable enantiomers, salts, solvates or prodrugs thereof are described. The compounds of Formula I are useful as IDO1 inhibitors. These are also useful for the treatment and/or prevention of cancer and endometriosis.
    Type: Application
    Filed: March 23, 2018
    Publication date: August 2, 2018
    Inventors: Stefano CROSIGNANI, Sandra CAUWENBERGHS, Gregory DRIESSENS, Frederik DEROOSE
  • TREATMENT FOR WOLFRAM SYNDROME AND OTHER ENDOPLASMIC RETICULUM STRESS DISORDERS
    Publication number: 20180214416
    Abstract: The present invention generally relates to a method of treating or preventing an endoplasmic reticulum stress disorder in subjects, such as a method of treating or preventing Wolfram syndrome.
    Type: Application
    Filed: November 13, 2015
    Publication date: August 2, 2018
    Applicant: Washington University
    Inventors: Fumihiko URANO, Simin LU
  • METHOD FOR TREATING HEPATIC ENCEPHALOPATHY
    Publication number: 20180214417
    Abstract: A method of treating or preventing type C Hepatic Encephalopathy in a human patient diagnosed with cirrhosis by administering a composition containing at least 200 mg biotin to the human patient daily.
    Type: Application
    Filed: March 26, 2018
    Publication date: August 2, 2018
    Applicant: MEDDAY PHARMACEUTICALS
    Inventor: Frédéric SEDEL
  • MULTISUBSTITUTED AROMATIC COMPOUNDS AS INHIBITORS OF THROMBIN
    Publication number: 20180214418
    Abstract: There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing a disease or disorder, which disease or disorder is amenable to treatment or prevention by the inhibition of thrombin.
    Type: Application
    Filed: March 27, 2018
    Publication date: August 2, 2018
    Inventors: Kevin Michael Short, Son Minh Pham, David Charles Williams, Somalee Datta
  • COMPOUNDS, COMPOSITIONS, AND METHODS OF INCREASING CFTR ACTIVITY
    Publication number: 20180214419
    Abstract: The present disclosure features compounds such as those having the Formulae (I) and (II), which can increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells. The present disclosure also features methods of treating a condition associated with decreased CFTR activity or a condition associated with a dysfunction of proteostasis comprising administering to a subject an effective amount of a disclosed compound, such as a compound of Formula (I) or (II).
    Type: Application
    Filed: July 25, 2016
    Publication date: August 2, 2018
    Inventors: Benito Munoz, Cecilia M. Bastos, John Miller
  • Methods for treating hyperuricemia in patients with gout using halofenate or halofenic acid and a second urate-lowering agent
    Publication number: 20180214420
    Abstract: Disclosed herein are pharmaceutical compositions, methods and kits for lowering the serum uric acid level of a subject and for the treatment of a condition associated with elevated serum uric acid levels comprising administering a composition comprising a first urate-lowering agent and a second urate-lowering agent. In some aspects the first urate-lowering agent is (?)-halofenate, (?)-halofenic acid, or a pharmaceutically acceptable salts thereof. In some aspects the second urate-lowering agent is an inhibitor of uric acid production, a uricosuric agent, a uricase, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 2, 2017
    Publication date: August 2, 2018
    Applicants: CymaBay Therapeutics, Inc., DiaTex, Inc.
    Inventors: Brian K. Roberts, Gopal Chandra Saha, Brian Edward Lavan, Charles A. McWherter
  • COMPOSITIONS, METHODS AND KITS FOR REDUCING LIPID LEVELS
    Publication number: 20180214421
    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.
    Type: Application
    Filed: December 21, 2017
    Publication date: August 2, 2018
    Inventors: Michael Zemel, Antje Bruckbauer
  • SOLID DISPERSIONS COMPRISING TACROLIMUS
    Publication number: 20180214422
    Abstract: A pharmaceutical composition comprising tacrolimus (FK-506) dissolved and/or dispersed in a hydrophilic or water-miscible vehicle to form a solid dispersion or solid solution at ambient temperature have improved bioavailability.
    Type: Application
    Filed: August 14, 2017
    Publication date: August 2, 2018
    Inventor: Per Holm
  • PHARMACEUTICAL COMPOSITION COMPRISING RAPAMYCIN OR DERIVATIVE THEREOF, AND METHOD FOR PRODUCING THE SAME
    Publication number: 20180214423
    Abstract: It is an object of the present invention to provide a pharmaceutical composition which can suppress a reduction in the content of an active ingredient caused by oxidation or decomposition of the rapamycin or a derivative thereof, can ensure long-term stability, and has high safety. The present invention provides a pharmaceutical composition comprising (A) rapamycin or a derivative thereof and (B) trehalose, and a method for producing a pharmaceutical composition comprising rapamycin or a derivative thereof, which comprises adding a solution containing rapamycin or a derivative thereof to sugars having a critical relative humidity at 25° C. of 95% or more.
    Type: Application
    Filed: July 27, 2016
    Publication date: August 2, 2018
    Applicant: NIPPON KAYAKU KABUSHIKI KAISHA
    Inventor: Dai KAWAMURA
  • PHARMACEUTICAL COMPOSITIONS COMPRISING 40-O-(2-HYDROXY)ETHYL-RAPAMYCIN
    Publication number: 20180214424
    Abstract: The invention relates to extended release pharmaceutical formulations in form of multiparticulates comprising 40-O-(2-hydroxy)ethyl-rapamycin, to dosage forms which comprise said pharmaceutical formulations, to methods of preparing said pharmaceutical formulations and said dosage forms, to uses of said pharmaceutical formulations and said dosage for the manufacture of a medicament for the treatment or prevention of diseases or conditions responsive to inhibition of mTOR signaling pathway, such as for instance proliferative diseases or immunosuppression.
    Type: Application
    Filed: January 24, 2018
    Publication date: August 2, 2018
    Inventors: Anke Diederich, Kurt LIECHTI, Peter KUEHL, Wing CHEUNG
  • METHODS OF TREATING BLADDER CANCER
    Publication number: 20180214425
    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.
    Type: Application
    Filed: March 28, 2018
    Publication date: August 2, 2018
    Inventor: Neil P. DESAI
  • PYRAZOLO[4,3-C]QUINOLINE DERIVATIVES FOR INHIBITION OF BETA-GLUCURONIDASE
    Publication number: 20180214426
    Abstract: The present invention provides novel pyrazolo[4,3-c]quinoline derivatives exhibiting specifically inhibition activity to microbiota ?-glucuronidase, whereby providing potent activities to prevent chemotherapy-induced diarrhea (CID) of cancers. Therefore, the compounds of the present invention can be used as (1) chemotherapy-adjuvant to prevent chemotherapy-induced diarrhea (CID) and enhance chemotherapeutic efficiency of cancers; (2) health-food supplement to prevent the carcinogens induced colon carcinoma.
    Type: Application
    Filed: May 26, 2016
    Publication date: August 2, 2018
    Inventors: Yeh-Long Chen, Tian-Lu Cheng, Cherng-Chyi Tzeng, Chih-Hua Tseng, Ta-Chun Cheng, Kai-Wen Cheng, Wei-Fen Luo
  • 3-(1H-PYRROLO[3,2-C]PYRIDIN-2-YL)-1H-PYRAZOLO[3,4-C]PYRIDINES AND THERAPEUTIC USES THEREOF
    Publication number: 20180214427
    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 2, 2018
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • 3-(1H-INDOL-2-YL)-1H-PYRAZOLO[3,4-B]PYRIDINES AND THERAPEUTIC USES THEREOF
    Publication number: 20180214428
    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 2, 2018
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • 3-(1H-PYRROLO[3,2-C]PYRIDIN-2-YL)-1H-PYRAZOLO[4,3-B]PYRIDINES AND THERAPEUTIC USES THEREOF
    Publication number: 20180214429
    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 2, 2018
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Selective Inhibitors Of i-NOS For Use Against Viral Infection
    Publication number: 20180214430
    Abstract: The present invention concerns compounds for use in the prevention of viral replication and/or the prevention or treatment of a viral infection, wherein the compounds are selective inhibitors of inducible nitric oxide synthase, and methods of preventing viral replication and/or preventing or treating viral infections in a subject comprising administering a prophylactically or therapeutically effective amount of the compounds.
    Type: Application
    Filed: July 15, 2016
    Publication date: August 2, 2018
    Applicant: UCL Business PLC
    Inventors: Christopher O'Callaghan, Claire Smith, Angrew Easton
  • Methods of Maintaining, Treating or Improving Cognitive Function
    Publication number: 20180214431
    Abstract: A method of administering an effective amount of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide, or a pharmaceutically acceptable salt thereof, to a patient in need thereof.
    Type: Application
    Filed: September 1, 2017
    Publication date: August 2, 2018
    Inventors: Dana C. Hilt, Gerhard Koenig
  • PHARMACEUTICAL COMPOSITION COMPRISING BETAHISTINE
    Publication number: 20180214432
    Abstract: The present disclosure relates to a pharmaceutical composition comprising as active substance betahistine or a pharmaceutically acceptable salt thereof, for use in the treatment of otological or neurological disorders in a human subject by intranasal application.
    Type: Application
    Filed: February 2, 2018
    Publication date: August 2, 2018
    Inventors: Christopher John WRAIGHT, Thomas MEYER
  • COMPOSITIONS AND METHODS FOR REDUCING MUSCLE CONTRACTION
    Publication number: 20180214433
    Abstract: Disclosed herein are methods of reducing muscle contraction in a diaphragm or peripheral muscle(s) of a patient sufficient to permit a surgical procedure. The methods may comprise the step of administering an oxime or pharmaceutically acceptable salt thereof to a subject in need thereof in an amount sufficient to achieve said reduced muscle contraction/neuromuscular blockade. Kits and articles of manufacture comprising a container having a label and a composition are also disclosed.
    Type: Application
    Filed: February 1, 2018
    Publication date: August 2, 2018
    Inventors: Brian L. Burback, Jessica Catherine Bright, Jerry D. Johnson
  • SEMI-SOLID TOPICAL COMPOSITION CONTAINING PIRFENIDONE AND MODIFIED DIALLYL DISULFIDE OXIDE (M-DDO) FOR ELIMINATING OR PREVENTING ACNE
    Publication number: 20180214434
    Abstract: The instant invention relates to a semi-solid topical composition containing Pirfenidone and an antimicrobial/antiseptic agent such as Modified Diallyl Disulfide Oxide (M-DDO) and its preparation process, offering advantages compared to other pharmaceutical forms of topical administration known in the state of the art, useful as antifibrotic, anti-inflammatory and antiseptic agent in the prevention, treatment and reversion of acne and post acne lesions. Said compositions is also useful for reducing skin redness, detaining the formation of new acne outbreaks, reversing already existing outbreaks and regenerating skin damage caused by acne.
    Type: Application
    Filed: March 14, 2018
    Publication date: August 2, 2018
    Inventors: Juan Socorro ARMENDÁRIZ BORUNDA, José Agustín Rogelio MAGAÑA CASTRO, Pedro PEÑA SANTOYO, Laura VÁZQUEZ CERVANTES
  • ORAL PHARMACEUTICAL DOSAGE FORMS
    Publication number: 20180214435
    Abstract: Controlled release oral dosage forms suitable for administration of methylphenidate are provided. Abuse-resistant controlled release oral dosage forms suitable for administration of methylphenidate are also provided. Methods of treating ADD and ADHD using the oral dosage forms are also provided.
    Type: Application
    Filed: December 22, 2017
    Publication date: August 2, 2018
    Inventors: Jan J. Scicinski, William W. van Osdol, Huey-Ching Su, Michael H. Arenberg, Jaymin Shah
  • PHACETOPERANE FOR TREATING OF ATTENTION DEFICIT HYPERACTIVITY DISORDER
    Publication number: 20180214436
    Abstract: The invention relates to the treatment of an attention deficit hyperactivity disorder (ADHD) with alpha-phenyl(piperidin-2-yl)methanol, or the pharmaceutically acceptable salts and esters thereof, in particular the acetate derivative, more particularly dextrophacetoperane. The invention additionally provides a method of synthesis of the (S,S) enantiomer of alpha-phenyl(piperidin-2-yl)methanol as well as a method of synthesis of dextrophacetoperane.
    Type: Application
    Filed: March 6, 2018
    Publication date: August 2, 2018
    Inventors: Eric KONOFAL, Bruno FIGADERE
  • NEW ALFENTANIL COMPOSITION FOR THE TREATMENT OF ACUTE PAIN
    Publication number: 20180214437
    Abstract: There is provided pharmaceutical compositions for the treatment of pain e.g. short-term pain, which compositions comprise a mixture comprising: (a) microparticles of alfentanil, or a pharmaceutically acceptable salt thereof, which microparticles are presented on the surfaces of larger carrier particles; (b) a water-soluble weak base; and (c) a compound which is a weak acid, which acid is presented in intimate mixture with the microparticles of alfentanil or salt thereof. The composition may further comprise a disintegrant. The acid is preferably citric acid.
    Type: Application
    Filed: September 11, 2017
    Publication date: August 2, 2018
    Inventors: Anders Pettersson, Barbro Johansson, Emil Schwan
  • SELECTIVE PFKFB4 INHIBITORS FOR THE TREATMENT OF CANCER
    Publication number: 20180214438
    Abstract: Methods and pharmaceutical compositions for inhibiting 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 4 (PFKFB4) and the treatment of cancer are described.
    Type: Application
    Filed: April 22, 2016
    Publication date: August 2, 2018
    Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.
    Inventors: Sucheta TELANG, Jason CHESNEY, John O. TRENT
  • AZA-CYANOQUINOLINONE PDE9 INHIBITORS
    Publication number: 20180214439
    Abstract: The present invention is directed to azacyanoquinolinone compounds which may be useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: July 27, 2016
    Publication date: August 2, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: ANTONELLA CONVERSO, KEVIN RODZINAK
  • ORAL COMPOSITION
    Publication number: 20180214440
    Abstract: The invention provides an oral composition comprising 4-methyl-8-phenoxy-1-(2-phenylethyl)-2,3-dihydro-1H-pyrrolo[3,2-c]quinoline or a pharmaceutically acceptable salt and/or solvate thereof and chlorhexidine or a pharmaceutically acceptable salt and/or solvate thereof, wherein the composition is in the form of a mouthwash and comprises about 0.001% w/v to about 0.06% w/v of chlorhexidine or a pharmaceutically acceptable salt and/or solvate thereof. Also provided is an oral composition comprising 4-methyl-8-phenoxy-1-(2-phenylethyl)-2,3-dihydro-1H-pyrrolo[3,2-c]quinoline or a pharmaceutically acceptable salt and/or solvate thereof, chlorhexidine or a pharmaceutically acceptable salt and/or solvate thereof, and a zinc compound.
    Type: Application
    Filed: April 11, 2016
    Publication date: August 2, 2018
    Applicant: HELPERBY THERAPEUTICS LIMITED
    Inventors: Anthony COATES, Yanmin HU, Sanju DHAWAN, Kartik SHAH
  • Method for producing benzazoloquinolium (BQs) salts and using the biological activity of the composition
    Publication number: 20180214441
    Abstract: Disclosed is the synthesis procedure for benzazolo[3,2-a]quinolinium chloride salts and the inclusion of chloro-substituent, amino-substituent, and nitro-substituent resulting in several compounds. The compounds are further used as markers due to their fluorescent properties including in hypoxic environments. This disclosure further describes anti-cancer screening of two BQS, namely, 7-benzyl-3-aminobenzimidazo[3,2-a]quinolinium chloride (ABQ-48: NSC D-763307) and the corresponding 7-benzyl-3-nitrobenzimidazo[3,2-a]quinolinium chloride (NBQ 48: NSC D-763303).
    Type: Application
    Filed: February 13, 2018
    Publication date: August 2, 2018
    Applicant: Sistema Universitario Ana G. Mendez, Inc.
    Inventors: Osvaldo Cox, Beatriz Zayas
  • METHODS FOR ATTENUATING OR PREVENTING MU(?)-OPIOID RECEPTOR MEDIATED TOLERANCE AND OPIOID-INDUCED HYPERALGESIA
    Publication number: 20180214442
    Abstract: Methods are provided for attenuating or preventing ?-opioid receptor mediated tolerance and opioid-induced hyperalgesia in a subject in need of acute or chronic opioid treatment for pain or in need of opioid anesthesia.
    Type: Application
    Filed: January 17, 2018
    Publication date: August 2, 2018
    Inventors: Gregory Scherrer, Vivianne L Tawfik, Gregory Corder
  • PHARMACEUTICAL PREPARATION CONTAINING OXYCODONE AND NALOXONE
    Publication number: 20180214443
    Abstract: The invention concerns a storage stable pharmaceutical preparation comprising oxycodone and naloxone for use in pain therapy, with the active compounds being released from the preparation in a sustained, invariant and independent manner.
    Type: Application
    Filed: January 26, 2018
    Publication date: August 2, 2018
    Inventors: Bianca BRÖGMANN, Silke MÜHLAU, Christof SPITZLEY
  • Piperazine-Substituted Benzothiophenes For Treatment of Mental Disorders
    Publication number: 20180214444
    Abstract: The present invention provides a heterocyclic compound represented by the general formula (1): The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
    Type: Application
    Filed: October 31, 2017
    Publication date: August 2, 2018
    Applicant: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Hiroshi YAMASHITA, Nobuaki ITO, Shin MIYAMURA, Kunio OSHIMA, Jun MATSUBARA, Hideaki KURODA, Haruka TAKAHASHI, Satoshi SHIMIZU, Tatsuyoshi TANAKA
  • ARYL SUBSTITUTED BICYCLIC HETEROARYL COMPOUNDS
    Publication number: 20180214445
    Abstract: Disclosed is a compound of Formula (I) or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate or prodrug thereof, wherein one R3 is H and the other R3 is an aryl group substituted with zero to 3 R3a; and R1, R2, and R3a are defined herein. Also disclosed are methods of using such compounds as PAR4 inhibitors for the inhibition or prevention of platelet aggregation, and the treatment of a thromboembolic disorder or the primary prophylaxis of a thromboembolic disorder. Also disclosed are methods of using such compounds for the treatment of human papillomavirus. Additionally, pharmaceutical compositions comprising at least one compound of Formula (I) are disclosed.
    Type: Application
    Filed: July 28, 2016
    Publication date: August 2, 2018
    Inventors: Xiaojun Zhang, Xiaofan Zheng, Louis S. Chupak
  • SOLID STATE FORMS OF SELEXIPAG
    Publication number: 20180214446
    Abstract: The present disclosure relates to solid state forms of Selexipag, in particular selexipag forms IV and V, and processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: September 2, 2016
    Publication date: August 2, 2018
    Inventors: Nidia VILLALVA, Ivon CANTE, Martin AYBAR, Angel RODRIGUEZ, Alejandro Guillen TORRES, Hana KANTOR, Ales GAVENDA, Hugo HERRERA, Alexander JEGOROV, Nydia LOPEZ
  • PYRAZOLE PYRIMIDINE DERIVATIVE AND USES THEREOF
    Publication number: 20180214447
    Abstract: The present invention provides pyrazole pyrimidine derivatives which inhibit Casein kinase I (CKI) and/or Interleukin-1 receptor-associated kinase 1 (IRAKI) and methods of their manufacture, compositions comprising them and uses thereof in methods of treating malignant disease and disorders and methods for treating inflammatory diseases and disorders.
    Type: Application
    Filed: August 4, 2016
    Publication date: August 2, 2018
    Inventors: Yinon Ben Neriah, Guy Brachya, Ido Burstain, Waleed Minzel, Irit Snir-Alkalay, Joseph Vacca, Dansu Li
  • METHOD OF DIAGNOSING AND TREATING SKIN NECROPTOSIS DISEASE COMPRISING RIP3-MLKL PATHWAY BLOCKER
    Publication number: 20180214448
    Abstract: The present invention relates to methods of preventing or treating skin necroptosis diseases, including administering to subjects receptor-interacting protein kinase-3 (RIP3)-mixed lineage kinase domain-like protein (MLKL) pathway blockers or dabrafenib, and method of diagnosing of skin necroptosis diseases, including detecting phosphorylated MLKL. The RIP3-MLKL pathway blockers according to the present invention directly suppress RIP3 overexpressing in skin necroptosis diseases, or inhibit phosphorylation and translocation to plasma membranes of MLKL, subsequently induced therefrom, thereby effectively preventing skin cell death via necroptosis. Thus, the present invention can prevent or treat a variety of skin diseases caused by necroptosis.
    Type: Application
    Filed: March 26, 2018
    Publication date: August 2, 2018
    Applicant: Ajou University Industry-Academic Cooperation Foun dation
    Inventor: You Sun KIM
  • CANCER THERAPY USING JAK INHIBITOR IN COMBINATION WITH MAPK INHIBITORS
    Publication number: 20180214449
    Abstract: Provided herein are new therapeutic regimens for treatment of cancer with a combination of a JAK inhibitor and an inhibitor targeting the MAPK pathway, combinations and methods of use thereof. In some embodiments, described herein are methods for treating cancer in an individual in need thereof, comprising administration of a JAK inhibitor and an inhibitor targeting the MAPK pathway to the individual. In some embodiments, the JAK inhibitor is a JAKI inhibitor.
    Type: Application
    Filed: January 28, 2016
    Publication date: August 2, 2018
    Inventors: Hyungsoo KIM, Ze'ev RONAI, Keith T. FLAHERTY
  • TREATMENT OF KIDNEY DISEASES ASSOCIATED WITH ELEVATED AVP
    Publication number: 20180214450
    Abstract: Disclosed are methods for treating kidney disease including autosomal dominant polycystic kidney disease (ADPKD) in a subject, comprising the step of administering to the subject a composition comprising a therapeutically effective amount of ticagrelor or a derivative thereof, thereby treating ADPKD. Disclosed are methods of decreasing arginine vasopressin (AVP) production in a subject comprising the step of administering to the subject a composition comprising an effective amount of ticagrelor, thereby decreasing AVP production. Disclosed are methods for treating dilutional hyponatremia in a subject comprising the step of administering to the subject a composition comprising an effective amount of ticagrelor, thereby decreasing AVP production.
    Type: Application
    Filed: January 31, 2018
    Publication date: August 2, 2018
    Inventors: Bellamkonda K. Kishore, Yue Zhang, Noel G. Carlson
  • Combination
    Publication number: 20180214451
    Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering 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, and N-[(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl]-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof.
    Type: Application
    Filed: March 27, 2018
    Publication date: August 2, 2018
    Inventors: Melissa Dumble, Tona Gilmer, Rakesh Kumar, Sylvie Laquerre, Peter F. Lebowitz, Shannon Renae Morris
  • COMPOSITION FOR PREVENTION OR TREATMENT OF INTRACTABLE EPILEPSY COMPRISING mTOR INHIBITOR
    Publication number: 20180214452
    Abstract: Provided is a use of the prophylaxis, amelioration or therapy of intractable epilepsy, for example, Focal Cortical Dysplasia (FCD).
    Type: Application
    Filed: March 7, 2016
    Publication date: August 2, 2018
    Inventors: Jeong Ho LEE, Jae Seok LIM, Woo-II KIM, Dong Seok KIM, Hoon Chul KANG, Se Hoon KIM
  • RIVAROXABAN PHARMACEUTICAL COMPOSITIONS
    Publication number: 20180214453
    Abstract: A rivaroxaban immediate release tablet comprising a non-ionic surfactant obtainable by using a dry process (i.e. no solvent is used during the manufacturing of the core tablet) which rapidly releases the drug as well as shows high stability and its fast and fed bioavailability is only attributable to the rivaroxaban behaviour.
    Type: Application
    Filed: August 4, 2016
    Publication date: August 2, 2018
    Applicant: INTERQUIM, S.A.
    Inventor: Berta FERNÁNDEZ MOLLAR
  • ANTIBIOTIC SOLUTION AND METHOD OF INJECTION TO PREVENT OPHTHALMIC INFECTIONS
    Publication number: 20180214454
    Abstract: A method of preventing post-operative endophthalmitis involves injecting an antibiotic solution into the anterior segment of the eye during surgery, the antibiotic solution having moxifloxacin, cefuroxime, vancomycin, or some combination thereof.
    Type: Application
    Filed: February 1, 2018
    Publication date: August 2, 2018
    Inventor: Jason Ahee
  • 5-HT2C RECEPTOR AGONISTS AND COMPOSITIONS AND METHODS OF USE
    Publication number: 20180214455
    Abstract: Provided in some embodiments are compounds of Formula A, as defined herein, that modulate the activity of 5-HT2C receptor.
    Type: Application
    Filed: July 28, 2016
    Publication date: August 2, 2018
    Inventors: Juerg Lehmann, Konrad Feichtinger, Albert S. Ren, Graeme Semple
  • ORBIT AZINE-FUMARATE, HYDRATE, CRYSTAL FORM AND PREPARATION METHOD THEREFOR
    Publication number: 20180214456
    Abstract: The invention relates to the field of pharmaceutical chemistry, particularly relates to an orbit azine-fumarate, a hydrate, a crystal form, and a preparation method therefor. Specifically, in the invention, different crystal forms of orbit azine-fumarate, an orbit azine-fumarate hydrate and a crystal form thereof, and an amorphous form of orbit azine-fumarate are prepared by adjusting the ratio of orbit azine and fumaric acid and using different crystallization methods. The invention makes it possible to provide an orbit azine-fumarate which has a higher pharmaceutical effect, is easier to be prepared, and has a better storage stability.
    Type: Application
    Filed: July 24, 2015
    Publication date: August 2, 2018
    Inventor: Liren Cheng
  • USE OF CYMANQUINE COMPOUNDS AS ANTIMALARIAL AGENTS
    Publication number: 20180214457
    Abstract: Organometallic compounds comprising a chloroquinoline moiety for use in the prophylaxis and treatment of malaria. The compounds can be manganese or rhenium complexes of a ligand comprising a chloroquinoline moiety.
    Type: Application
    Filed: July 20, 2016
    Publication date: August 2, 2018
    Inventors: William E. GEIGER, Kevin Lam, Lawrence W. BERGMAN
  • 1,5-DIHYDRO-2H-PYRROL-2-ONE COMPOUNDS AND METHODS OF USING SAME
    Publication number: 20180214458
    Abstract: The present invention relates to 1,5-dihydro-2H-pyrrol-2-one compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into tissue cells.
    Type: Application
    Filed: December 22, 2017
    Publication date: August 2, 2018
    Inventors: Christopher LOOSE, Bradley TAIT, Rajesh MANCHANDA, Will MCLEAN
  • LIQUID POLYMER DELIVERY SYSTEM FOR EXTENDED ADMINISTRATION OF DRUGS
    Publication number: 20180214459
    Abstract: Liquid polymer pharmaceutical compositions with a biodegradable liquid polyester that has a carboxylic acid end group, a biocompatible solvent, and an active pharmaceutical agent are useful for administration into the body to provide extended long term release of the drug.
    Type: Application
    Filed: August 3, 2016
    Publication date: August 2, 2018
    Inventors: John Milton DOWNING, Vipin SAXENA, John MIDDLETON