Patents Issued in May 16, 2019
  • Publication number: 20190142776
    Abstract: Treatment of NAFLD and NASH by therapy with MBX-8025 or an MBX-8025 salt.
    Type: Application
    Filed: December 17, 2018
    Publication date: May 16, 2019
    Applicant: CymaBay Therapeutics, Inc.
    Inventors: Brian Roberts, Xueyan Wang, Yun-Jung Choi, David Karpf, Robert Martin, Charles McWherter
  • Publication number: 20190142777
    Abstract: The present disclosure relates to (a) an improved pharmaceutical composition comprising a levodopa active agent and a carbidopa active agent (b) methods of producing the pharmaceutical composition and (c) methods of treating Parkinson's disease and associated conditions comprising administering the pharmaceutical composition to a subject with Parkinson's disease.
    Type: Application
    Filed: October 16, 2018
    Publication date: May 16, 2019
    Inventors: Rajkumar Conjeevaram, Alexandru DEAC, Ye HUANG, Sean E. MACKEY, Randy A. MENGES, Jayne Zimmerman
  • Publication number: 20190142778
    Abstract: Provided herein are methods for treating or preventing myopia, or for inhibiting the development of myopia, comprising administering to a subject in need thereof an effective amount of an agent capable of increasing nitric oxide levels in one or more ocular It cells or an agent capable of promoting or increasing the expression and/or activity of nNOS in one or more ocular cells. Also provided are methods for inducing or promoting nNOS expression and/or activity in one or more ocular cells, comprising exposing said cells to an effective amount of L-arginine.
    Type: Application
    Filed: June 21, 2017
    Publication date: May 16, 2019
    Inventor: Sally Anne McFadden
  • Publication number: 20190142779
    Abstract: Methods for treating or preventing age-related cognitive impairment in an adult human are disclosed. One method comprises administering to an adult human having, or at risk of having, impaired cognitive function a dietetic food, medical food, or food supplement. The food or food supplement comprises a rumenic acid-rich conjugated linoleic acid (RAR-CLA), or a pharmaceutically acceptable salt, ester, mono-, di-, or triglyceride, metabolic precursor thereof, or mixture thereof, in an amount effective to enhance cognitive function in the human. The RAR-CLA comprises cis-9, trans-11 linoleic acid and trans-10, cis-12 linoleic acid isomers in a weight ratio of at least 2:1. Enrichment of a dietetic food, medical food, or food supplement with RAR-CLA can help to improve cognitive function. The impact is particularly evident in aging adult males, as indicated by their improved scores in the Rey Auditory Verbal Learning Test.
    Type: Application
    Filed: June 20, 2017
    Publication date: May 16, 2019
    Inventors: Hiskias Gerrit KEIZER, Jenifer HEYDINGER GALANTE
  • Publication number: 20190142780
    Abstract: Disclosed is the use of isothiocyanate compounds. In particular, disclosed is the use of a compound as shown by Formula (I) or a derivative as shown by Formula (II) in the manufacture of a composition or preparation for preventing and/or treating hyperlipidemia. The compound of the present invention can reduce the levels of triglycerides and low density lipoproteins in the serum of mammals (such as rats and humans), increase the level of high density lipoproteins in the serum, and reduce the level of total bilirubin in the serum of mammals (such as rats and humans).
    Type: Application
    Filed: April 20, 2017
    Publication date: May 16, 2019
    Inventors: Jingcai CHENG, Chunxia ZHANG, Zhiwei CHENG
  • Publication number: 20190142781
    Abstract: The present invention relates to the use of a pharmaceutically effective amount of an short-acting calcium channel blocking compound to treat ischemic heart conditions, cardiac arrhythmias, hypertensive crisis in an emergency room setting, hypertension before, during, or after surgery, no-reflow phenomenon following reperfusion, and diseases associated with decreased skeletal muscle blood flow. The invention also relates to pharmaceutical compositions formulated for use in such methods and to kits for such methods.
    Type: Application
    Filed: January 14, 2019
    Publication date: May 16, 2019
    Inventors: Martin P. MAGUIRE, Elise RIOUX, Harry J. LEIGHTON
  • Publication number: 20190142782
    Abstract: Inhibitors of glucosylceramide degradation, to pharmaceutical compositions containing same, and to the use of same in the treatment of diseases of the motor units, such as amyotrophic lateral sclerosis.
    Type: Application
    Filed: April 11, 2017
    Publication date: May 16, 2019
    Inventors: Michael SPEDDING, Alexandre HENRIQUES, Jean-Philippe LOEFFLER
  • Publication number: 20190142783
    Abstract: The use of dianhydrogalactitol provides a novel therapeutic modality for the treatment of glioblastoma multiforme and medulloblastoma. Dianhydrogalactitol acts as an alkylating agent on DNA that creates N7 methylation. Dianhydrogalactitol is effective in suppressing the growth of cancer stem cells and is active against tumors that are refractory to temozolomide; the drug acts independently of the MGMT repair mechanism.
    Type: Application
    Filed: January 8, 2019
    Publication date: May 16, 2019
    Applicant: Del Mar Pharmaceuticals (BC) Ltd.
    Inventors: Dennis M. Brown, Jeffrey Bacha, Sandra Dunn
  • Publication number: 20190142784
    Abstract: Provided herein are compounds, compositions containing the compounds, and methods for the treatment of cancer in a cancer patient. In particular, the compounds are made by a process comprising treating a first compound represented by either Formula G? or Formula M?: with a second compound of generalized formula R8R9C(OCH3)2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R1 and R2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R7 is an alkyl group, an olefinic group, or an aromatic group; P1 is a hydroxyl protecting group; P5 is H or an acid labile protecting group at the 7-O position; R8 is H, alkyl group, olefinic or aromatic group; and R9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.
    Type: Application
    Filed: January 14, 2019
    Publication date: May 16, 2019
    Inventors: Jan Zygmunt, James Ferrara, James D. McChesney
  • Publication number: 20190142785
    Abstract: The present invention provides a compound as shown in formula (I), formula (II), or formula (III), which can inhibit the binding of influenza virus PB2 protein to RNA cap and has an anti-influenza effect.
    Type: Application
    Filed: April 12, 2017
    Publication date: May 16, 2019
    Applicant: Sinoclone Ltd.
    Inventors: Bojian ZHENG, Shuofeng YUAN, Richard Yi Tsun KAO, Jie ZHOU
  • Publication number: 20190142786
    Abstract: The disclosed embodiments relate to, dosing regimens for the administration of topiramate, optionally in combination with one or more sympathomimetic agents such as phentermine. The dosing regimens can, for example, limit the exposure of subjects to topiramate, identify subjects who are unlikely to obtain a benefit from treatment with escalating dosages of topiramate (with or without the sympathomimetic agent, such as phentermine), or both, thereby reducing or eliminating harmful or intolerable side effects in subjects who are unlikely to respond to treatment and maximizing the therapeutic benefits from treatment in subjects who do respond.
    Type: Application
    Filed: June 13, 2018
    Publication date: May 16, 2019
    Inventors: Peter TAM, Roman DVORAK, Craig PETERSON
  • Publication number: 20190142787
    Abstract: The invention relates to novel liquid pharmaceutical compositions comprising at least one SGLT-2 inhibitor and one or more polar organic solvents, wherein the at least one SGLT-2 inhibitor comprises 1-cyano-2-(4-cyclopropyl-benzyl)-4-(?-D-glucopyranos-1-yl)-benzene according to formula (I): as well as corresponding processes of manufacturing such liquid pharmaceutical compositions and their medical uses.
    Type: Application
    Filed: January 2, 2019
    Publication date: May 16, 2019
    Inventors: Claudius Weiler, Thomas Duch, Marbod Haase, Timothy Shane Priddy, Heike Stettler
  • Publication number: 20190142788
    Abstract: Mutations in keratin genes or the genes that regulate keratin expression can result in epithelial cells lacking sufficient structural integrity. The resulting disruption of connective tissue gives rise to inherited disorders such epidermolysis bullosa. It has been found that various cannabinoids (including mixtures of cannabidiols and cannabinol) upregulate expression of various keratins such that loss of function in other keratin genes may be compensated for. By way of this upregulation, these cannabinoids can be used to treat epidermolysis bullosa and other connective tissue disorders arising from intermediate filament dysfunction.
    Type: Application
    Filed: May 4, 2017
    Publication date: May 16, 2019
    Inventor: Sazzad HOSSAIN
  • Publication number: 20190142789
    Abstract: Provided herein are pharmaceutically acceptable compositions containing a selective cyclooxygenase-2 (COX-2) inhibitor (coxib) and optionally buprenorphine. In particular, compositions containing a coxib formulated for oral, topical or subcutaneous administration to treat pain or inflammation are described.
    Type: Application
    Filed: August 9, 2018
    Publication date: May 16, 2019
    Inventors: Douglas I. Hepler, Gail L. Dempsey, Roland Johnson, Michael Kelly, Michael Daniel, Neil Paulsen, Bert Clayton
  • Publication number: 20190142790
    Abstract: Provided herein is a pharmaceutical composition comprising at least one isoflavonoid. Also provided herein are methods of treating cancer, sensitizing cancer cells, and inducing apoptosis in cancer cells by administering such compositions.
    Type: Application
    Filed: September 12, 2018
    Publication date: May 16, 2019
    Inventors: George JEOFFREYS, Alison JOHNSON, Andrew HEATON, Ofir MORENO
  • Publication number: 20190142791
    Abstract: Provided herein is a tocol rich fraction of rice bran oil deodorized distillate that is shown to be both radioprotective and able to protect against oxidative damage. This fraction may prove an inexpensive and readily available extract that can be used to prepare pharmaceutical compositions for use in protecting against radiation exposure and/or other forms of oxidative stress.
    Type: Application
    Filed: January 11, 2019
    Publication date: May 16, 2019
    Applicant: Tocol Pharmaceuticals, LLC
    Inventors: Cesar M. Compadre, Philip Breen, Nukhet Aykin-Burns, Martin Hauer-Jensen
  • Publication number: 20190142792
    Abstract: Epicatechins, Epicatechin Oligomers, or Thiolated Epicatechins are applied (A) directly to a genital wart in the form of a cream, ointment, paste or solution, (B) directly to the genital wart wherein such cream, ointment, paste or solution contains as an additional active ingredient a skin permeabilizing agent, (C) following electrosurgical resection or removal of the genital wart in such form of a cream, ointment, paste or solution, (D) following chemical resection or extirpation of the genital wart in such form, (E) following surgical resection or removal of the genital wart in such form, wherein said Epicatechins, Epicatechin Oligomers, or Thiolated Epicatechins both provide antiviral activity against multiple strains of human pappilomavirus (HPV) and promote healing following resection polymers contained in a vehicle. Disclosed are the compositions, therapeutical kits containing such composition, methods of treatment using such composition, and methods of enhancing the stability of such composition.
    Type: Application
    Filed: January 23, 2019
    Publication date: May 16, 2019
    Applicant: CACAO BIO-TECHNOLOGIES, LLC
    Inventors: Daniel PRESTON, Randall B. MURPHY
  • Publication number: 20190142793
    Abstract: The present invention relates to certain SGLT-2 inhibitors, such as ertugliflozin or a co-crystal or a pharmaceutically acceptable salt thereof, for treating and/or preventing metabolic disorders, such as type 1 or type 2 diabetes mellitus or pre-diabetes, in patients with renal impairment or chronic kidney disease (CKD).
    Type: Application
    Filed: January 10, 2019
    Publication date: May 16, 2019
    Applicants: Merck Sharp & Dohme Corp., Pfizer Inc.
    Inventors: Ramachandra G. Naik, Elizabeth S. Ommen, James Michael Rusnak, Steven G. Terra
  • Publication number: 20190142794
    Abstract: A pharmaceutical composition containing ginkgolide B and an ADP receptor antagonist, a preparation method thereof and use thereof in preparation of antiplatelet drugs, wherein the ADP receptor antagonist is clopidogrel, prasugrel, ticagrelor and/or ticlopidine.
    Type: Application
    Filed: January 10, 2019
    Publication date: May 16, 2019
    Applicant: CHENGDU BAIYU PHARMACEUTICAL CO., LTD
    Inventor: Yi SUN
  • Publication number: 20190142795
    Abstract: The present invention provides a dihydroisoxazole of formula: or a salt thereof, for use in the control of sea lice in fish.
    Type: Application
    Filed: May 3, 2017
    Publication date: May 16, 2019
    Inventor: Chouaib Tahtaoui
  • Publication number: 20190142796
    Abstract: The present invention relates to a pharmaceutical combination comprising LSZ102 and ribociclib; pharmaceutical compositions comprising the same; and methods of using such combinations and compositions in the treatment or prevention of conditions in which degradation of estrogen receptors combined with CDK4/6 inhibition is beneficial in, for example, the treatment of cancers.
    Type: Application
    Filed: November 14, 2018
    Publication date: May 16, 2019
    Inventors: Tinya ABRAMS, Larry Alexander GAITHER
  • Publication number: 20190142797
    Abstract: Provided herein are stable enalapril oral liquid formulations. Also provided herein are methods of using enalapril oral liquid formulations for the treatment of certain diseases including hypertension, heart failure and asymptomatic left ventricular dysfunction.
    Type: Application
    Filed: January 8, 2019
    Publication date: May 16, 2019
    Inventors: Gerold L. MOSHER, David W. MILES
  • Publication number: 20190142798
    Abstract: The invention relates to (among other things) polymer-des-ethyl sunitinib conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over des-ethyl sunitinib in unconjugated form.
    Type: Application
    Filed: January 9, 2019
    Publication date: May 16, 2019
    Inventors: Antoni Kozlowski, Sean M. Culbertson, Xiaoming Shen, Samuel P. McManus, Mark A. Wilson
  • Publication number: 20190142799
    Abstract: Provided herein are small molecule inhibitors of ASH1L activity and small molecules that facilitate ASH1L degradation and methods of use thereof for the treatment of disease, including acute leukemia, solid cancers and other diseases dependent on activity of ASH1L.
    Type: Application
    Filed: May 12, 2017
    Publication date: May 16, 2019
    Inventors: Jolanta Grembecka, Tomasz Cierpicki, David Rogawski, Dmitry Borkin, Szymon Klossowski, Jin Zhuang, Deanna Montgomery
  • Publication number: 20190142800
    Abstract: The present invention relates to the field of antimicrobials and pharmaceutical sciences. The invention provides anti-fungal compositions for the management of fungal growth and treatment of fungal infections, including treatment of resistant fungal infections. The present compositions comprise at least one antifungal agent and at least one medium-chain saturated or unsaturated fatty acid having carbon chain length of C-1 to C-14 or ester thereof, optionally along with excipient(s), giving rise to a synergistic antifungal activity.
    Type: Application
    Filed: June 13, 2017
    Publication date: May 16, 2019
    Applicant: VYOME THERAPEUTICS LIMITED
    Inventors: Shamik GHOSH, Sumana GHOSH, Mau SINHA, Suresh SADHASIVAM, Anubhuti JAIN, Anamika BHATTACHARYYA
  • Publication number: 20190142801
    Abstract: Disclosed are methods and compositions for reducing toxicity associated with infection by Clostridium difficile by inhibiting Clostridium difficile toxin B (TcdB) and/or toxin A (TcdA). Such compounds include ebselen compounds, namely ebselen and its salts, ebselen functional analogues and ebselen structural analogues, as well as certain amide derivatives. This includes Formula I, e.g. 1-methyl-3-phenylpropylamine, Formula II, e.g., 2,2?-diselane-1,2-diylbis[N-(2,4-difluorophenyl)benzamide]; and Formula III, e.g. 2-(2-methoxy-5-methylphenyl)-1, 2-benzoselenazol-3-one. The present compositions may be comprised in a colon-retentive formulation that increases residence of and/or release of the compound in the area where the infection is active.
    Type: Application
    Filed: January 7, 2019
    Publication date: May 16, 2019
    Inventors: Kristina Oresic Bender, Aaron Puri, Aimee Shen, Matthew S. Bogyo
  • Publication number: 20190142802
    Abstract: Disclosed are compounds of formula I, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising a compound of formula I, and methods involving use of the compounds and compositions in the treatment and prevention of diseases and conditions characterized by aberrant complement system activity.
    Type: Application
    Filed: February 1, 2017
    Publication date: May 16, 2019
    Applicant: BioCryst Pharmaceuticals, Inc.
    Inventors: Pravin L. Kotian, Yarlagadda S. Babu, Weihe Zhang, Lakshminarayana Vogeti, Minwan Wu, Venkat R. Chintareddy, Krishhan Raman
  • Publication number: 20190142803
    Abstract: The present invention relates to methods of treatment using [3-(4-{2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-propyl]-diethyl amine (“COMPOUND I”) or a pharmaceutically acceptable salt thereof. In various embodiments, the methods of treatment include treatment of mild-to-moderate dementia of Alzheimer's type, diabetes, insomnia, and other indications. The present invention also relates to pharmaceutical compositions comprising COMPOUND I or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: January 8, 2019
    Publication date: May 16, 2019
    Inventors: Cesare Orlandi, David J. Clark, Imogene M. Dunn, Maria Carmen Valcarce Lopez, Matthew J. Kostura
  • Publication number: 20190142804
    Abstract: The present invention relates to novel 5-(fluoroalkyl)-1-aryl-1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.
    Type: Application
    Filed: May 2, 2017
    Publication date: May 16, 2019
    Inventors: Thomas NEUBAUER, Marie-Pierre COLLIN-KRÖPELIN, Peter KOLKHOF, Elisabeth POOK, Matthias Beat WITTWER, Klemens LUSTIG, Carsten SCHMECK, Pierre WASNAIRE, Heiko SCHIRMER
  • Publication number: 20190142805
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: January 14, 2019
    Publication date: May 16, 2019
    Inventors: Barry D. Quart, Jean-Luc Giradet, Esmir Gunic, Li-Tain Yeh
  • Publication number: 20190142806
    Abstract: Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.
    Type: Application
    Filed: May 5, 2017
    Publication date: May 16, 2019
    Inventors: Carmela Sidrauski, Marina Pliushchev, Jennifer M. Frost, Lawrence A. Black, Xiangdong Xu, Ramzi Farah Sweis, Lei Shi, Qingwei I. Zhang, Yunsong Tong, Charles W. Hutchins, Seungwon Chung, Michael J. Dart
  • Publication number: 20190142807
    Abstract: The present invention is directed to methods of treating and/or ameliorating muscular dystrophy and/or treating cardiomyopathy in muscular dystrophy patients by administration of a therapeutically effective amount of a thromboxane A2 receptor antagonist.
    Type: Application
    Filed: January 4, 2019
    Publication date: May 16, 2019
    Inventors: Leo PAVLIV, James WEST, Ines Macias-Perez, Erica Carrier
  • Publication number: 20190142808
    Abstract: The present invention relates to a sustained-release pharmaceutical composition intended for animal use, which comprises a drug, a sugar, a wax, and a water-soluble polymer.
    Type: Application
    Filed: June 8, 2017
    Publication date: May 16, 2019
    Applicant: DS Pharma Animal Health Co., Ltd.
    Inventor: Teruaki KURIYAMA
  • Publication number: 20190142809
    Abstract: The present invention provides a benzo[d]thiazole derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The benzo[d]thiazole derivative or its pharmaceutically acceptable salt can selectively inhibit the protein-protein interaction between KRS and a laminin receptor (LR), thereby inhibiting migration of cancer cells. Therefore, the benzo[d]thiazole derivative or its pharmaceutically acceptable salt may be usefully applied for preventing or treating the diseases associated with cancer cell metastasis.
    Type: Application
    Filed: July 6, 2017
    Publication date: May 16, 2019
    Applicant: Yuhan Corporation
    Inventors: Se-Woong Oh, Youn Hur, Jin-Hwi Park, Jae-Eun Joo, Ho-Woong Kang, Hyok-Jun Cho, Eui-Chul Lee, Chan-Sun Park, Dong-Hyun Kim, Jong-Gyun Kim, Su-Youn Nam
  • Publication number: 20190142810
    Abstract: The invention provides compounds of formula I or pharmaceutically acceptable salt, solvate or hydrate thereof (I) wherein ring A represents group A-I or A-II (A-I, A-II) A1, A2, A3, A4 represent independently C(R4aa) or N, wherein no more than one of A1, A2, A3, and A4 represents N; A5 represents C(R4b) or N; B1, B2, B3 and B4 represent independently C(R3) or N, wherein no more than two of B1, B2, B3 and B4 represent N; n is 1 or 2; and R1, R2, R3, R4a and R4aa and R4b are as defined in the claims, as well as methods of using the compounds to treat proliferation diseases, in particular cancer.
    Type: Application
    Filed: June 29, 2017
    Publication date: May 16, 2019
    Inventors: Heidi LANE, Florian RICHALET, Mahmoud EL SHEMERLY
  • Publication number: 20190142811
    Abstract: Compounds of Formula (I) are estrogen receptor alpha modulators, where the variables in Formula (I) are described in the disclosure. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions that are estrogen receptor alpha dependent and/or estrogen receptor alpha mediated, including conditions characterized by excessive cellular proliferation, such as breast cancer.
    Type: Application
    Filed: March 29, 2017
    Publication date: May 16, 2019
    Inventors: Peter Qinhua Huang, Deborah Helen Slee, Sayee Gajanan Hegde, Chad Daniel Hopkins, Kevin Duane Bunker, Joseph Robert Pinchman, Rakesh Kumar Sit
  • Publication number: 20190142812
    Abstract: The present invention relates to 5-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: January 6, 2017
    Publication date: May 16, 2019
    Inventors: Ulrich LÜCKING, Marcus KOPPITZ, Julien LEFRANC, Lars WORTMANN, Antje Margret WENGNER, Gerhard SIEMEISTER, Ulf BÖMER, Benjamin BADER, Philip LIENAU, Hans SCHICK
  • Publication number: 20190142813
    Abstract: There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of kallikrein, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing certain diseases or disorders, which disease or disorder is amenable to treatment or prevention by the inhibition of kallikrein.
    Type: Application
    Filed: January 10, 2019
    Publication date: May 16, 2019
    Inventors: Kevin Michael Short, Son Minh Pham, David Charles Williams, David Ben Kita
  • Publication number: 20190142814
    Abstract: The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
    Type: Application
    Filed: January 15, 2019
    Publication date: May 16, 2019
    Inventors: Olaf Kinzel, Christoph Steeneck, Claus Kremoser
  • Publication number: 20190142815
    Abstract: The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.
    Type: Application
    Filed: January 10, 2019
    Publication date: May 16, 2019
    Inventors: Sven Guenther, Guochen Chi, Bindu Bera, Travis Mickle, Sanjib Bera
  • Publication number: 20190142816
    Abstract: The invention provides a crystalline hydrochloride salt of 4-[2-(2,4,6-trifluorophenoxymethyl)phenyl]piperidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.
    Type: Application
    Filed: January 10, 2019
    Publication date: May 16, 2019
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Lori Jean Patterson, Robert S. Chao, Miroslav Rapta
  • Publication number: 20190142817
    Abstract: Compositions and methods for inhibiting and/or sensitizing or re-sensitizing a parasite to an antiparasitic drug are provided. The compositions can comprise a rifamycin derivative or a pharmaceutically acceptable salt, hydrate, or prodrug thereof in an amount and formulation sufficient to inhibit or induce drug-sensitization in a parasite. The methods can comprise administering a rifamycin derivative or a pharmaceutically acceptable salt, hydrate, or prodrug thereof to a parasite in an amount and formulation sufficient to inhibit or induce drug-sensitization in the parasite.
    Type: Application
    Filed: January 16, 2019
    Publication date: May 16, 2019
    Inventors: James C. Sacchettini, Matthew W. Miller, Deeann Wallis, Nian E. Zhou, Theresa W. Fossum
  • Publication number: 20190142818
    Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) for treatment of pulmonary conditions (e.g. asthma). The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
    Type: Application
    Filed: January 16, 2019
    Publication date: May 16, 2019
    Inventors: Chongxi YU, Lina XU
  • Publication number: 20190142819
    Abstract: Methods and compositions for treating a renal cell carcinoma with the combination of lenvatinib or a pharmaceutically acceptable salt thereof and everolimus are provided. Particularly useful dosages and dose modifications upon the occurrence of adverse events are also provided.
    Type: Application
    Filed: April 17, 2017
    Publication date: May 16, 2019
    Inventor: Alton Kremer
  • Publication number: 20190142820
    Abstract: Provided is a drug superior for preventing and/or treating dementia. It contains a carbostyril derivative of the following formula (1) (wherein R is a cycloalkyl group, A is a lower alkyl group, and a single bond or a double bond is present between the 3-position and the 4-position of the carbostyril nucleus) and dihydroquercetin.
    Type: Application
    Filed: May 1, 2017
    Publication date: May 16, 2019
    Applicants: NATIONAL CEREBRAL AND CARDIOVASCULAR CENTER, FOUNDATION FOR BIOMEDICAL RESEARCH AND INNOVATION AT KOBE
    Inventors: Tadamasa MATSUMOTO, Masafumi IHARA, Satoshi SAITO, Masanori FUKUSHIMA
  • Publication number: 20190142821
    Abstract: The present disclosure is directed to compositions and methods for treating or preventing vasomotor symptoms such as hot flashes, comprising a Transient Receptor Potential Melastatin 8 (TRPM8) antagonist and administering a TRPM8 antagonist, respectively.
    Type: Application
    Filed: June 12, 2017
    Publication date: May 16, 2019
    Inventor: Joseph M. Palumbo
  • Publication number: 20190142822
    Abstract: Provided are methods for treating breast cancer in a patient by administering effective amounts of liposomal irinotecan sucrosofate (MM-398). The breast cancer may be triple negative breast cancer (TNBC), estrogen receptor/progesterone receptor (ER/PR) positive breast cancer, ER-positive breast cancer, or PR-positive breast cancer, or metastatic breast cancer.
    Type: Application
    Filed: July 16, 2018
    Publication date: May 16, 2019
    Inventors: Eliel Bayever, Jonathan Basil Fitzgerald, Jaeyeon Kim, Stephan Klinz
  • Publication number: 20190142823
    Abstract: An injectable pharmaceutical composition includes a solution of 3-acyl-buprenorphine, or a pharmaceutically acceptable salt thereof, in a biocompatible organic solvent, wherein the injectable pharmaceutical composition exhibits a steady release profile lasting over one week when injected into a patient. The acyl group is an alkylcarbonyl group, and an alkyl portion of the alkylcarbonyl group is a straight-chain, branched-chain, having 1-20 carbon atoms. The biocompatible organic solvent is N-methyl-2-pyrrolidone, ethyl acetate, ethanol, butanol, 2-butanol, isobutanol, ispropanol, glycerin, benzyl benzoate, dimethyl sulfoxide, N,N-dimethylacetamide, propylene glycol, dimethyl glycol, benzyl alcohol, or a combination of two or more thereof.
    Type: Application
    Filed: September 12, 2017
    Publication date: May 16, 2019
    Applicant: Alar Pharmaceuticals, Inc.
    Inventors: Tong-Ho Lin, Yung-Shun Wen, Jui-Wei Liang
  • Publication number: 20190142824
    Abstract: An anti-neoplastic stable pharmaceutical composition comprising Temozolomide, high substituted polysaccharide phosphate in salt form, and high substituted polysaccharide phosphate in acidic form, in particular in a weight ratio of from 5 to 20% Temozolomide to 30 to 80% of polysaccharide in salt form, the reminder up to 100% being polysaccharide in acidic form. The level of 5-aminomidazole-4-carboxamide is below 0.5% by weight of Temozolomide in both the composition and the formulation disclosed. Also disclosed is a hydrogel for intrathecal administration obtainable by contacting the composition with sterile water, a method of manufacture of the composition and uses of the composition and the gel.
    Type: Application
    Filed: April 28, 2017
    Publication date: May 16, 2019
    Inventors: Yurkshtovich MIKALAI, Veyeunik DZMITRY, Alinouskaya VALIANTSINA, Natalia ATRAKHIMOVICH, Lryna HALOUCHYK, Sergey BELIAEV, Tatjana YURKSHTOVICH, Pavel BYCHKOUSKI, Aliaksandr FEDULAU, Tatsiana TRUKHACHOVA
  • Publication number: 20190142825
    Abstract: Compositions and therapeutic uses of HEPES and derivatives in the treatment of pain associated with cancers and side-effects including post-chemotherapy cognitive impairment are disclosed herein. HEPES is also used to treat neurodegenerative and neurological diseases, demyelinization injuries, and side-effects and withdrawal symptoms associated with benzodiazepines, anti-depressants, and other neurological agents.
    Type: Application
    Filed: January 14, 2019
    Publication date: May 16, 2019
    Inventor: Ivan E. Danhof