Patents Issued in September 13, 2018
  • SUBSTITUTED 5-HYDROXYOXINDOLES AND THEIR USE AS ANALGESICS AND FEVER REDUCERS
    Publication number: 20180256543
    Abstract: The present invention provides compounds and compositions which are useful in methods for modulating pain and fevers in a subject. These compounds are of the structure of formula (I), wherein Rx-R4, X, Y, and Z are defined herein, or a pharmaceutically acceptable salt, solvate, or prodrug thereof to the subject. In one embodiment, the compound is 5-hydroxy-7-methyloxindole.
    Type: Application
    Filed: May 3, 2016
    Publication date: September 13, 2018
    Inventors: John R. CARON, Robert B. RAFFA, Kenneth G. CARSON
  • Mono- or Di-Substituted Indole Derivatives As Dengue Viral Replication Inhibitors
    Publication number: 20180256544
    Abstract: The present invention concerns mono- or di-substituted indole compounds, methods to prevent or treat dengue viral infections by using said compounds and also relates to said compounds for use as a medicine, more preferably for use as a medicine to treat or prevent dengue viral infections. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of dengue viral infections. The invention also relates to processes for preparation of the compounds.
    Type: Application
    Filed: September 15, 2016
    Publication date: September 13, 2018
    Applicants: Janssen Pharmaceuticals, Inc., Katholieke Universiteit Leuven
    Inventors: Bart Rudolf, Romanie KESTELEYN, Jean-François BONFANTI, Tim Hugo, Maria JONCKERS, Pierre Jean-Marie, Bernard RABOISSON, Dorothée Alice, Marie-Eve BARDIOT, Arnaud Didier, M MARCHAND
  • Mono- or Di-Substituted Indole Derivatives As Dengue Viral Replication Inhibitors
    Publication number: 20180256545
    Abstract: The present invention concerns mono- or di-substituted indole compounds, methods to prevent or treat dengue viral infections by using said compounds and also relates to said compounds for use as a medicine, more preferably for use as a medicine to treat or prevent dengue viral infections. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of dengue viral infections. The invention also relates to processes for preparation of the compounds.
    Type: Application
    Filed: September 15, 2016
    Publication date: September 13, 2018
    Applicants: Janssen Pharmaceuticals, Inc., Katholieke Universiteit Leuven
    Inventors: Bart Rudolf, Romanie KESTELEYN, Jean-François BONFANTI, Tim Hugo, Maria JONCKERS, Pierre Jean-Marie, Bernard RABOISSON, Dorothée Alice, Marie-Eve BARDIOT, Arnaud Didier, M MARCHAND
  • INDOLINONE COMPOUNDS AND USES THEREOF
    Publication number: 20180256546
    Abstract: Indolinone derivative compounds that act as EWS-FLI1 transcription factor inhibitors are provided. Also provided are pharmaceutical compositions of the indolinone derivatives, methods of synthesizing the same, methods of treating using same, and assays for identifying the inhibitors of EWS-FLI1 oncoprotein.
    Type: Application
    Filed: May 7, 2018
    Publication date: September 13, 2018
    Inventor: Jean-Michel Vernier
  • PYRAZOLE-AMIDE COMPOUNDS AND PHARMACEUTICAL USE THEREOF
    Publication number: 20180256547
    Abstract: A compound represented by the following formula: wherein n is 1 or 2, or a pharmaceutically acceptable salt thereof, and a pharmaceutical use thereof.
    Type: Application
    Filed: October 6, 2017
    Publication date: September 13, 2018
    Inventors: Takahisa Motomura, Gakujun Shomi
  • AQUEOUS COMPOSITION COMPRISING DANTROLENE
    Publication number: 20180256548
    Abstract: An aqueous composition includes either dantrolene or a pharmaceutically acceptable salt thereof and a cyclodextrin derivative, with the pH of the aqueous composition greater than 7. A powder can be obtained by drying the composition. The powder can be included in a kit.
    Type: Application
    Filed: October 19, 2016
    Publication date: September 13, 2018
    Inventors: HERVÉ JEAN SCHWEBEL, VINCENT ADAMO
  • COMBINATORIAL METHODS TO IMPROVE THE THERAPEUTIC BENEFIT OF BISANTRENE AND ANALOGS AND DERIVATIVES THEREOF
    Publication number: 20180256549
    Abstract: The present invention describes methods and compositions for improving the therapeutic efficacy of therapeutic agents previously limited by suboptimal therapeutic performance by either improving efficacy as monotherapy or reducing side effects. Such methods and compositions are particularly applicable to bisantrene or derivatives, analogs, or prodrugs thereof.
    Type: Application
    Filed: May 14, 2018
    Publication date: September 13, 2018
    Inventors: William J. GARNER, Amie FRANKLIN, John ROTHMAN
  • TARGET FOR TREATING HEPATITIS B VIRUS
    Publication number: 20180256550
    Abstract: A method of treating hepatitis B virus includes inhibiting the activities of AKT and/or mTOR, inhibiting the synthesis of 5-phosphate ribose, and inhibiting HBV DNA and HBV cccDNA.
    Type: Application
    Filed: June 15, 2015
    Publication date: September 13, 2018
    Inventor: Yong LIAO
  • METHODS OF TREATING HEMATOLOGICAL MALIGNANCY USING NANOPARTICLE MTOR INHIBITOR COMBINATION THERAPY
    Publication number: 20180256551
    Abstract: The present invention relates to methods and compositions for the treatment of hematological malignancy by administering compositions comprising nanoparticles that comprise an mTOR inhibitor (such as a limus drug, e.g., sirolimus or a derivative thereof) and an albumin in combination with compositions comprising a second therapeutic agent.
    Type: Application
    Filed: June 29, 2016
    Publication date: September 13, 2018
    Inventors: Neil P. DESAI, Mark ALLES
  • METHODS OF TREATING CANCER USING B-RAF INHIBITORS AND IMMUNE CHECKPOINT INHIBITORS
    Publication number: 20180256552
    Abstract: Provided herein are therapies including dosage regimens for the treatment of cancer using B-RAF and an immune checkpoint inhibitor in combination with and/or without a MEK inhibitor.
    Type: Application
    Filed: May 18, 2018
    Publication date: September 13, 2018
    Applicant: Genentech, Inc.
    Inventors: Dawn Colburn, Nicole Richie
  • CONTROLLED DELIVERY SYSTEM
    Publication number: 20180256553
    Abstract: The present invention relates to novel anesthetic compositions containing a non-polymeric carrier material and an anesthetic, where the compositions are suitable for providing a sustained local anesthesia without an initial burst and having a duration for about 24 hours or longer. Certain compositions are also provided that include a first anesthetic and a second anesthetic. In such compositions, the second anesthetic is a solvent for the first anesthetic and provides an initial anesthetic effect upon administration to a subject. The non-polymeric carrier may optionally be a high viscosity liquid carrier material such as a suitable sugar ester. The compositions can further include one or more additional ingredients including active and inactive materials. Methods of using the compositions of the invention to produce a sustained anesthetic effect at a site in a subject are also provided.
    Type: Application
    Filed: January 12, 2018
    Publication date: September 13, 2018
    Applicant: DURECT CORPORATION
    Inventor: Adrian Neil Verity
  • SUSTAINED-RELEASE TOPICALLY ADMINISTERED AGENT
    Publication number: 20180256554
    Abstract: A sustained-release topically administered agent includes a compound having a pharmacological action, a crosslinking polysaccharide derivative having at least one active ester group, introduced into a side chain of a polysaccharide, which is capable of reacting with an active hydrogen-containing group, and being capable of forming a crosslinked substance by a covalent bond between the active ester group and the active hydrogen-containing group; and a pH adjuster for adjusting a pH condition suitable for forming a biodegradable gel containing the compound when the sustained-release topically administered agent is mixed. The sustained-release topically administered agent forms the biodegradable gel containing the compound when the sustained-release topically administered agent is mixed. The pH of the biodegradable gel is not less than five.
    Type: Application
    Filed: May 11, 2018
    Publication date: September 13, 2018
    Applicant: TERUMO KABUSHIKI KAISHA
    Inventors: Hideka KIKUCHI, Chisato IWAKIRI
  • SUSTAINED RELEASE AMINOPYRIDINE COMPOSITION
    Publication number: 20180256555
    Abstract: A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at least 12 hours, preferably 24 hours or more and the use of the composition to treat various neurological diseases.
    Type: Application
    Filed: May 16, 2018
    Publication date: September 13, 2018
    Inventors: Sean Cunningham, Seamus Mulligan, Michael Myers
  • METHODS FOR TREATING AN IMPAIRMENT IN GAIT AND/OR BALANCE IN PATIENTS WITH MULTIPLE SCLEROSIS USING AN AMINOPYRIDINE
    Publication number: 20180256556
    Abstract: Disclosed herein is use of one or more aminopyridines in methods and compositions for treatment of impairments in gait or balance in patients with multiple sclerosis.
    Type: Application
    Filed: May 16, 2018
    Publication date: September 13, 2018
    Applicant: Acorda Therapeutics, Inc.
    Inventors: Gabriel Pardo, Gustavo Adolfo Suarez Zambrano, Cecilie Fjeldstad
  • PHARMACEUTICAL COMBINATION COMPRISING (A) THE ALPHA-ISOFORM SPECIFIC PI3K INHIBITOR ALPELISIB (BYL719) AND (B) AN AKT INHIBITOR, PREFERABLY MK-2206, AFURESERTIB OR UPROSERTIB, AND THE USE THEREOF IN THE TREATMENT/PREVENTION OF CANCER
    Publication number: 20180256557
    Abstract: The present disclosure pertains to a pharmaceutical combination comprising (a) alpha-isoform specific PI3K inhibitor and (b) an AKT inhibitor; combined preparations and pharmaceutical compositions thereof; the uses of such combination in the treatment or prevention of cancer; and methods of treating or preventing cancer in a subject in need thereof comprising administering a therapeutically effective amount of such combination.
    Type: Application
    Filed: August 24, 2016
    Publication date: September 13, 2018
    Inventors: Giordano Caponigro, Thomas Horn-Spirohn, Joseph Lehar, Samit Hirawat
  • METHODS AND COMPOSITIONS OF INHIBITING DCN1-UBC12 INTERACTION
    Publication number: 20180256558
    Abstract: In one aspect, the invention relates to substituted 1-phenyl-3-(piperidin-4-yl)urea analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the DCN1-UBC12 interaction inhibitors of DCN1-mediated cullin-RING ligase activity, methods of making same, pharmaceutical compositions comprising same, methods of treating disorders using the disclosed compounds and compositions, methods of treating disorders associated with a DCN1-UBC12 interaction dysfunction, methods of treating disorders associated with a DCN1-mediated cullin-RING ligase activity dysfunction, methods of male contraception comprising the disclosed compounds and compositions, and kits comprising the disclosed compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: September 19, 2016
    Publication date: September 13, 2018
    Applicants: Memorial Sloan Kettering Cancer Center, St. Jude Children's Research Hospital
    Inventors: Jaeki MIN, Daniel C. SCOTT, Deepak BHASIN, Brenda A. SCHULMAN, Bhuvanesh SINGH, Jared T. HAMMILL, R. Kiplin GUY
  • MUSCARINIC M2 RECEPTOR BLOCKADE TO DELAY OR PREVENT ONSET OF PROGRESSIVE MEMORY DECLINE
    Publication number: 20180256559
    Abstract: Provided are methods for delaying or preventing onset of progressive memory decline by administering a muscarinic M2 receptor blocking compound to patients identified as at risk of developing a condition characterized by progressive memory decline, prior to onset of the condition.
    Type: Application
    Filed: March 5, 2018
    Publication date: September 13, 2018
    Inventor: William Z. SUO
  • LIQUID NICOTINE FORMULATION
    Publication number: 20180256560
    Abstract: There is disclosed a liquid formulation for inhalation into the lungs, comprising an aqueous solution of nicotine or a nicotine analogous molecule, at least one organic and/or inorganic salt, an organic liquid having a viscosity higher than water, and optionally an organic alcohol, wherein the pH of the formulation is greater than pH 7 and the formulation does not include a propellant. There is further disclosed a corresponding method of aerosolising the liquid formulation, a method for delivering nicotine to the user, and an aerosol-generating device.
    Type: Application
    Filed: September 22, 2016
    Publication date: September 13, 2018
    Inventors: Hans-Jürgen Hoppe, Iain McDerment
  • Pharmaceutical Combination
    Publication number: 20180256561
    Abstract: This invention provides a pharmaceutical combination comprising biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]methyl}-5-methoxyphenylcarbamoyl)ethyl]piperidin-4-yl ester, or a pharmaceutically acceptable salt thereof, and fluticasone furoate, and use of the pharmaceutical combination in therapy, for example in the treatment or prophylaxis of respiratory disorders or diseases, for example pulmonary disorders such as chronic obstructive pulmonary disease (COPD) asthma and Asthma-COPD Overlap Syndrome (ACOS).
    Type: Application
    Filed: January 11, 2016
    Publication date: September 13, 2018
    Inventor: Colin John FISH
  • Transdermal Delivery System
    Publication number: 20180256562
    Abstract: Described is a transdermal device comprising a backing layer; a single layer adhesive matrix comprising buprenorphine or a salt thereof, a pressure sensitive adhesive including a silicone-type adhesive blended with an acrylate-type adhesive, a solubilizer, a permeation enhancer, and a crystallization inhibitor; and a release layer. Also described is a method of relieving pain and a method of preparing a transdermal delivery system.
    Type: Application
    Filed: September 9, 2016
    Publication date: September 13, 2018
    Inventors: Sameer Sachdeva, Tarun Goswami, Jay Audett
  • OLIGOMER-OPIOID AGONIST CONJUGATES
    Publication number: 20180256563
    Abstract: The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.
    Type: Application
    Filed: October 24, 2017
    Publication date: September 13, 2018
    Inventors: Jennifer Riggs-Sauthier, Bo-Liang Deng, Timothy A. Riley
  • PLATINUM COMPOUNDS THAT INHIBIT CONSTITUTIVE STAT3 SIGNALING AND INDUCE CELL CYCLE ARREST AND APOPTOSIS OF MALIGNANT CELLS
    Publication number: 20180256564
    Abstract: The subject invention concerns a compound and compositions having activity as an inhibitor of Stat3 protein and methods of using the compound and compositions. In one embodiment, a compound of the invention has the structure shown in formula I, formula II, or formula III. The subject invention also concerns methods of using the compounds and compositions of the invention.
    Type: Application
    Filed: May 14, 2018
    Publication date: September 13, 2018
    Inventors: SAID M. SEBTI, NICHOLAS J. LAWRENCE, JAMES TURKSON
  • OXABICYCLOHEPTANES AND OXABICYCLOHEPTENES FOR THE TREATMENT OF DEPRESSIVE AND STRESS DISORDERS
    Publication number: 20180256565
    Abstract: A method of treating a depressive or stress disorder in a subject afflicted therewith comprising administering to the subject an effective amount of a compound having the structure:
    Type: Application
    Filed: November 17, 2017
    Publication date: September 13, 2018
    Inventors: John S. Kovach, Salvatore Lecca, Manuel Mameli
  • DUAL MAGL AND FAAH INHIBITORS
    Publication number: 20180256566
    Abstract: Provided herein are compounds and pharmaceutical compositions comprising said compounds useful as modulators of MAGL and/or FAAH. The subject compounds and compositions are useful for the treatment of pain and neurological disorders.
    Type: Application
    Filed: March 12, 2018
    Publication date: September 13, 2018
    Inventors: Cheryl A. GRICE, Justin S. CISAR, Katharine K. DUNCAN, Yu FENG, John J.M. WIENER, Olivia D. WEBER
  • COMPOSITIONS AND METHODS FOR TREATING CENTRALLY MEDIATED NAUSEA AND VOMITING
    Publication number: 20180256567
    Abstract: Provided are compositions and methods for treating or preventing nausea and vomiting in patients undergoing chemotherapy, radiotherapy, or surgery.
    Type: Application
    Filed: March 16, 2018
    Publication date: September 13, 2018
    Inventors: Fabio TRENTO, Sergio CANTOREGGI, Giorgia ROSSI, Roberta CANNELLA, Daniele BONADEO
  • Methods and Compositions for Killing Senescent Cells and for Treating Senescence-Associated Diseases and Disorders
    Publication number: 20180256568
    Abstract: Methods are provided herein for selectively killing senescent cells and for treating senescence-associated diseases and disorders by administering a senolytic agent. Senescence-associated diseases and disorders treatable by the methods using the senolytic agents described herein include cardiovascular diseases and disorders associated with or caused by arteriosclerosis, such as atherosclerosis; idiopathic pulmonary fibrosis; chronic obstructive pulmonary disease; osteoarthritis; senescence-associated ophthalmic diseases and disorders; and senescence-associated dermatological diseases and disorders.
    Type: Application
    Filed: April 11, 2018
    Publication date: September 13, 2018
    Inventors: Remi-Martin Laberge, Judith Campisi, Albert Davalos, Marco Demaria, Nathaniel David, Alain Philippe Vasserot, Darren J. Baker, Bennett G. Childs, James L. Kirkland, Tamar Tchkonia, Jan M.A. van Deursen, Jennifer Elisseeff, Chaekyu Kim, Okhee Jeon, Allyson K. Palmer, Yi Zhu
  • SUBSTITUTED 6,7-DIHYDROPYRAZOLO[1,5-a]PYRAZINES AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
    Publication number: 20180256569
    Abstract: The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.
    Type: Application
    Filed: May 10, 2018
    Publication date: September 13, 2018
    Inventors: Sergio-Alvar Alonso-de Diego, Michiel Luc, Maria Van Gool, Óscar Delgado-González, José Ignacio Andrés-Gil, Andrés Avelino Trabanco-Suárez
  • TOPICAL FORMULATIONS
    Publication number: 20180256570
    Abstract: Described herein are pharmaceutical formulations comprising 4-fluoro-N-methyl-N-(1-(4-(1-methyl-1H-pyrazol-5-yl)phthalazin-1-yl)piperidin-4-yl)-2-(trifluoromethyl)benzamide, or a pharmaceutically acceptable salt thereof, wherein the pharmaceutical formulations are suitable for topical use, and methods of using such formulations in the treatment of subjects having cancer.
    Type: Application
    Filed: November 28, 2016
    Publication date: September 13, 2018
    Applicant: IGNYTA, INC.
    Inventors: Jeffrey Alan PETERSON, Stephanie Ann SWEETANA
  • METHODS RELATING TO THE DIAGNOSIS AND TREATMENT OF THROMBOTIC MICROANGIOPATHY
    Publication number: 20180256571
    Abstract: Described herein are methods, assays, and compositions relating to the treatment of thrombosis, preeclampsia, cancer, and intestinal inflammation, e.g., by administering ADAMTS13 to a subject in need of treatment.
    Type: Application
    Filed: May 13, 2016
    Publication date: September 13, 2018
    Applicant: CHILDREN'S MEDICAL CENTER CORPORATION
    Inventors: Denisa D. WAGNER, Luise ERPENBECK
  • METALLOENZYME INHIBITOR COMPOUNDS
    Publication number: 20180256572
    Abstract: Provided are compounds having HDAC6 modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by HDAC6.
    Type: Application
    Filed: March 9, 2018
    Publication date: September 13, 2018
    Applicant: VPS-3, Inc.
    Inventor: Christopher M. Yates
  • Trk-INHIBITING COMPOUND
    Publication number: 20180256573
    Abstract: The present invention provides a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy for Trk-related diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I), wherein all symbols represent the same meanings as described in the specification, a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.
    Type: Application
    Filed: May 9, 2018
    Publication date: September 13, 2018
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Jun TAKEUCHI, Satoshi ITADANI, Kazuya HASHIMURA, Masahiro IKURA, Masato HIGASHINO, Tetsuya YASUHIRO, Takeshi NAGAURA
  • SPIROCYCLIC COMPOUNDS AS TRYPTOPHAN HYDROXYLASE INHIBITORS
    Publication number: 20180256574
    Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.
    Type: Application
    Filed: May 14, 2018
    Publication date: September 13, 2018
    Inventors: Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren, Andrew Scribner
  • PYRIMIDINONE AMIDE COMPOUNDS AS PDE2 INHIBITORS
    Publication number: 20180256575
    Abstract: The present invention is directed to pyrimidinone amide compounds which may be useful as therapeutic agents for the treatment of central nervous system and/or peripheral disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Alzheimer's, cognitive impairment, anxiety, depression, migraines, or Huntington's disease, Parkinson's disease, Parkinson's disease dementia (PDD), and other diseases associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: May 10, 2016
    Publication date: September 13, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Dong-Ming Shen, Deping Wang, XiaoXia Qian, Bart Harper, Meng Yang, Yingjian Bo
  • BICYCLICALLY SUBSTITUTED URACILS AND THE USE THEREOF
    Publication number: 20180256576
    Abstract: The present application relates to novel bicyclically substituted uracil derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases.
    Type: Application
    Filed: March 5, 2018
    Publication date: September 13, 2018
    Applicant: Bayer Pharma Aktiengesellschaft
    Inventors: Chantal FÜRSTNER, Jens ACKERSTAFF, Alexander STRAUB, Heinrich MEIER, Hanna TINEL, Katja ZIMMERMANN, Adrian TERSTEEGEN, Dmitry ZUBOV, Raimund KAST, Jens SCHAMBERGER, Martina SCHÄFER, Kirsten BÖRNGEN
  • KSR Antagonists
    Publication number: 20180256577
    Abstract: This invention relates to antagonists of Kinase Suppressor of Ras (KSR). Pharmaceutical compositions comprising KSR inhibitors and methods of treating cancer are also provided.
    Type: Application
    Filed: April 15, 2016
    Publication date: September 13, 2018
    Inventors: Arvin Dar, Neil Dhawan, Alex P. Scopton
  • A Combination Therapy Comprising Varlitinib and an Anticancer Agent
    Publication number: 20180256578
    Abstract: In one aspect the present disclosure provides a method of sensitizing a cancer patient to chemotherapy by administering a combination therapy comprising; a) a therapeutically effective amount of a compound of formula (I) an enantiomer thereof or a pharmaceutically acceptable salts of any one of the same, and b) a chemotherapeutic agent or a combination of chemotherapeutic agents.
    Type: Application
    Filed: September 5, 2016
    Publication date: September 13, 2018
    Inventors: Bertil Lindmark, Lisa Ooi
  • METHODS AND COMPOSITIONS FOR TREATING DRUG RESISTANCE IN CANCER
    Publication number: 20180256579
    Abstract: Disclosed herein are compositions and methods for treating cancer. Further provided herein are compositions and methods for reducing, inhibiting, or preventing resistance of cancer to tyrosine kinase inhibitors. The methods may include administering an anti-resistance agent such as a CYP51A1 inhibitor or an agonist of miRNA-764 (SEQ ID NO: 4) to a subject. A tyrosine kinase inhibitor may also be administered to the subject in addition to the anti-resistance agent.
    Type: Application
    Filed: February 23, 2018
    Publication date: September 13, 2018
    Inventors: Subhra Mohapatra, Shyam S. Mohapatra, Mark Howell, Rajesh Nair
  • COMBINATION THERAPIES FOR TREATMENT OF CANCER
    Publication number: 20180256580
    Abstract: Combination therapies for treatment of cancer are provided. The disclosed methods comprise administration of a cyclin-dependent kinase inhibitor and a DNA methyltransferase inhibitor to a mammal in need thereof.
    Type: Application
    Filed: August 3, 2016
    Publication date: September 13, 2018
    Inventors: David J. Bearss, Steven L. Warner, Adam Siddiqui-Jain, Clifford J. Whatcott, Wontak Kim
  • USE OF INHIBITORS OF BRUTON'S TYROSINE KINASE (BTK)
    Publication number: 20180256581
    Abstract: Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.
    Type: Application
    Filed: April 27, 2018
    Publication date: September 13, 2018
    Inventors: Joseph J. Buggy, Laurence Elias, Gwen Fyfe, Eric Hedrick, David J. Loury, Tarak D. Mody
  • METHODS AND COMPOSITIONS FOR THE TREATMENT OF METABOLIC DISORDERS
    Publication number: 20180256582
    Abstract: The present invention is directed to a novel methods and compositions for the therapeutic intervention in hyperphenylalaninemia. More specifically, the specification describes methods and compositions for treating various types of phenylketonurias using compositions comprising BH4. Combination therapies of BH4 and other therapeutic regimens are contemplated.
    Type: Application
    Filed: May 8, 2018
    Publication date: September 13, 2018
    Inventors: Daniel I. Oppenheimer, Emil D. Kakkis, Fredric D. Price, Alejandro Dorenbaum, Rudolf Moser, Viola Groehn, Thomas Egger, Fritz Blatter
  • TREATMENTS FOR AUTOIMMUNE DISEASE
    Publication number: 20180256583
    Abstract: The invention relates to a novel approach to the treatment of autoimmune diseases, particularly multiple sclerosis. In a further embodiment of the invention there is provided a molecule capable of acting as substrate for the queuine-insertase enzyme complex and where said molecule is not a substrate for Hypoxanthine-guanine phosphoribosyltransferase and said molecule has the effect of lowering interferon gamma, for use in the treatment of auto-immune diseases. Preferably the autoimmune disease is multiple sclerosis.
    Type: Application
    Filed: May 10, 2018
    Publication date: September 13, 2018
    Inventor: Vincent Kelly
  • Pemetrexed Polymeric Nanoparticles And Methods Of Making And Using Same
    Publication number: 20180256584
    Abstract: The present disclosure generally relates to nanoparticles having about 0.2 to about 35 weight percent of pemetrexed; and about 10 to about 99 weight percent of biocompatible polymer such as a diblock poly(lactic) acid-poly(ethylene)glycol. Other aspects of the invention include methods of making such nanoparticles.
    Type: Application
    Filed: May 15, 2018
    Publication date: September 13, 2018
    Applicant: Pfizer Inc.
    Inventor: Stephen E. Zale
  • METHOD FOR ENHANCING WOUND HEALING BY ADMINISTRATING ADENINE
    Publication number: 20180256585
    Abstract: Provided is a composition for wound healing, which includes adenine and a pharmaceutically acceptable salt thereof. Also provided is a method for enhancing wound healing in a subject in need thereof including administering to the subject the composition.
    Type: Application
    Filed: March 13, 2017
    Publication date: September 13, 2018
    Inventors: Han-Min Chen, Cheng-Yi Kuo, Chun-Fang Huang, Jiun-Tsai Lin
  • COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF FETAL LIVER KINASE POLYPEPTIDES
    Publication number: 20180256586
    Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of FLT3 (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hppel-Lindau, cereblon, ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds the target protein FLT3, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of the target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
    Type: Application
    Filed: December 13, 2017
    Publication date: September 13, 2018
    Inventors: Andrew P. Crew, Keith R. Hornberger, Craig M. Crews, George Burslem
  • A Synthetic Lethal Drug Combination for Treating Renal Cell Carcinoma
    Publication number: 20180256587
    Abstract: The present invention pertains to a novel treatment of renal cell carcinoma and other a solid tumors which harbor a VHL inactivation, based on the combination of a first agent inhibiting a protein kinase CK2 (CK2) and a second agent inhibiting an Ataxia Telangiectasia Mutated (ATM) kinase.
    Type: Application
    Filed: September 21, 2016
    Publication date: September 13, 2018
    Applicants: Commissariat a l'Energie Atomique et aux Energies Alternatives, Institut National de la Sante et de la Recherche Medicale (INSERM)
    Inventors: Sofia Giacosa, Catherine Pillet, Claude Cochet, Odile Filhol, Caroline Barette, Emmanuelle Soleilhac
  • 1H-PYRAZOLO[3,4-B]PYRIDINES AND THERAPEUTIC USES THEREOF
    Publication number: 20180256588
    Abstract: Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof , and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:
    Type: Application
    Filed: November 14, 2017
    Publication date: September 13, 2018
    Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
  • METHODS OF TREATING AND/OR PREVENTING ACTINIC KERATOSIS
    Publication number: 20180256589
    Abstract: The application pertains to methods of treating and/or preventing actinic keratosis, comprising administering a therapeutically effective amount of KX-01, to a subject in need thereof.
    Type: Application
    Filed: March 12, 2018
    Publication date: September 13, 2018
    Inventors: Min-Fun Rudolf KWAN, Johnson Yiu-Nam LAU, E. Douglas KRAMER, David Lawrence CUTLER, Jane FANG
  • METHODS FOR CONTROLLED PROLIFERATION OF STEM CELLS / GENERATING INNER EAR HAIR CELLS USING 3-(PYRIDIN-2-YL)-1H-INDOL-2-OL BASED COMPOUNDS
    Publication number: 20180256590
    Abstract: The present invention relates to methods of inducing the 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 hair cells. Specifically, the invention relates to methods of using compounds comprising a 3-(pyridin-2-yl)-1H-indol-2-ol containing moiety having a Formula I: and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: April 10, 2018
    Publication date: September 13, 2018
    Inventors: Christopher LOOSE, Will MCLEAN, Melissa HILL-DRZEWI
  • 2-(MORPHOLIN-4-YL)-1,7-NAPHTHYRIDINES
    Publication number: 20180256591
    Abstract: The present invention relates to substituted 2-(morpholin-4-yl)-1,7-naphthyridine compounds of general formula (I) or (Ib), to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative disease as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 8, 2018
    Publication date: September 13, 2018
    Inventors: Lars WORTMANN, Ulrich LÜCKING, Julien LEFRANC, Hans BRIEM, Marcus KOPPITZ, Knut EIS, Franz VON NUSSBAUM, Benjamin BADER, Antje Margret WENGNER, Gerhard SIEMEISTER, Wilhelm BONE, Philip LIENAU, Joanna GRUDZINSKA-GOEBEL, Dieter MOOSMAYER, Uwe EBERSPÄCHER, Hans SCHICK
  • ANTIBACTERIAL COMPOSITIONS
    Publication number: 20180256592
    Abstract: Pharmaceutical compositions comprising ceftibuten or a pharmaceutically acceptable salt thereof, and clavulanic acid or a pharmaceutically acceptable salt thereof are disclosed.
    Type: Application
    Filed: May 11, 2018
    Publication date: September 13, 2018
    Applicant: WOCKHARDT LIMITED
    Inventors: Mahesh Vithalbhai PATEL, Sachin BHAGWAT, Swapna Shripad TAKALKAR, Amol KULKARNI, Jaykumar Satwaji SATAV, Snehal Rameshwar PALWE, Hemant Narendra KHANDE