Abstract: The present invention provides methods for reducing tumor burden, tumor growth, tumor progression, and/or metastasis in a subject suffering from a solid tumor cancer such as triple negative breast cancer. The methods include administering to a subject in need thereof a therapeutically effective amount of a PD-L1 inhibitor or a PD-1 inhibitor in combination with a small molecule chemokine receptor antagonist that blocks CCR1.
Type:
Application
Filed:
April 6, 2017
Publication date:
October 12, 2017
Inventors:
Israel CHARO, Heiyoun JUNG, Thomas J. SCHALL, Penglie ZHANG
Abstract: The present invention relates to compounds which are found to exhibit an antiviral effect. The compounds are modulators of the activity of the viral haemagglutinin and/or neuraminidase enzymes.
Type:
Application
Filed:
September 7, 2015
Publication date:
October 12, 2017
Applicant:
Griffith University
Inventors:
Mark Von Itzstein, Ibrahim El-Deeb, Larissa Dirr, Patrice Guillon, Moritz Winger
Abstract: Pharmaceutical compositions for treating, mitigating or preventing fungal nail diseases, disorders or pathologies are described, the compositions comprising at least one functionalized allylamine compound, at least one functionalized triazole compound, and at least one functionalized imidazole compound. Methods for fabricating the compositions and using them are also described.
Abstract: Orally administerable deferasirox formulations are disclosed having reduced release under gastric conditions and fast release at near neutral pH or at neutral pH.
Abstract: The present invention relates to the compound [2-[(5-nitro-1,3-thiazol-2-yl)carbamoyl]phenyl]ethanoate (Nitazoxanide) or 2-hydroxy-N-(5-nitro-2-thiazolyl)benzamide (Tizoxanide) for treating cholestatic and fibrotic diseases.
Type:
Application
Filed:
March 13, 2017
Publication date:
October 12, 2017
Inventors:
RAPHAEL DARTEIL, ROBERT WALCZAK, CAROLE BELANGER, EMILIE NEGRO, PIERRE DAUBERSIES, PHILIPPE DELATAILLE
Abstract: A compound, or a pharmaceutically acceptable salt thereof, having a structure of: wherein A is a ring; Y1 and Y2 are each independently N or C with the proper valency; X1 and X2 are each independently —NH—, —O—, —CH2—O—, —NH—CH2—, or —N(CH3)—CH2—, provided that when at least one of X1 and X2 is —CH2—O—, —NH—CH2—, or —N(CH3)—CH2— then the —CH2— is directly connected to A; a and b are each independently 0 or 1; c and d are each independently 0 or 1; Z1 and Z2 are each independently a heterocyclic; and R1 and R2 are each independently optionally substituted alkyl, optionally substituted aralkyl, optionally substituted cycloalkyl, amino, optionally substituted heteroaralkyl, optionally substituted alkylalkoxy, optionally substituted alkylaryloxy, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocycloalkyl; provided that if Y1 and Y2 are each C, then a is 1 and b is 1; provided that if Y1 and Y2 are each N, then a is 0 and b is 0; provided that if Y1 is N and Y
Type:
Application
Filed:
October 1, 2015
Publication date:
October 12, 2017
Applicants:
University of Pittsburgh - Of the Commonwealth System of Higher Education, Cornell University
Inventors:
Lee A. McDermott, Prema C. Iyer, Richard A. Cerione, William P. Katt
Abstract: In one aspect, the invention provides compounds of Formula (I) or (II): (I) or (II) and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2a, R2b, R3, R4, Z and G are defined as set forth in the disclosure. The invention also provides compounds of Formulae A and B and pharmaceutically acceptable salts and solvates thereof. Other aspects of the invention include the use of compounds of Formulae I, II, A, and B, and pharmaceutically acceptable salts and solvates thereof for the treatment of disorders responsive to modulation of one or more opioid receptors. In certain embodiments, the Compounds of the Invention are useful for treating pain.
Type:
Application
Filed:
September 17, 2015
Publication date:
October 12, 2017
Applicant:
Purdue Pharma L.P.
Inventors:
Xiaoming Zhou, Laykea Tafesse, John J. Engel
Abstract: A compound of formula (I): which is 4-(3-fluoro-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-yl)-3-(3-(2-methoxyethoxy)phenyl)butanoic acid, or a salt thereof.
Type:
Application
Filed:
September 22, 2015
Publication date:
October 12, 2017
Inventors:
Niall Andrew Anderson, Matthew Howard James Campbell-Crawford, Ashley Paul Hancock, John Martin Pritchard, Joanna Mary Redmond
Abstract: A compound according to formula (I) wherein R1 is hydrogen, cyclopropyl, or pyrazolyl, wherein said pyrazolyl is optionally substituted by one or two methyl groups; or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
September 22, 2015
Publication date:
October 12, 2017
Inventors:
Niall Andrew ANDERSON, Matthew Howard James CAMPBELL-CRAWFORD, Ashley Paul HANCOCK, Seble LEMMA, Simon John Fawcett MACDONALD, John Martin PRITCHARD, Panayiotis Alexandrou PROCOPIOU, Stephen SWANSON
Abstract: The present disclosure relates to pirfenidone (5-methyl-1-phenyl-2-(1H)-pyridone) and its derivatives and pharmaceutically acceptable salts thereof, use of these compounds as a medicament, and for the manufacture of a medicament for treating or delaying the onset or development of pulmonary hypertension.
Abstract: The present invention provides an anti-influenza virus agent that targets biomolecules of host cells including human cells and a method of screening a candidate molecule for the anti-influenza virus agent. That is, the present invention is an anti-influenza virus agent that has an effect of suppressing expression or a function of a gene that encodes a protein having an effect of suppressing incorporation of an influenza virus vRNA or an NP protein into influenza virus-like particles in host cells and the gene is at least one selected from the group including JAK1 gene and the like.
Type:
Application
Filed:
September 18, 2015
Publication date:
October 12, 2017
Applicant:
Japan Science and Technology Agency
Inventors:
Yoshihiro KAWAOKA, Tokiko WATANABE, Eiryo KAWAKAMI, Shinji WATANABE
Abstract: This application provides for a method of treating a human patient afflicted with anti-TNF? refractory Crohn's disease, of treating a human patient afflicted with non-fibrostenotic Crohn's disease, and of treating a human patient whose Crohn's disease had not been surgically treated, the method comprising periodically administering to the patient an amount of laquinimod or pharmaceutically acceptable salt thereof effective to treat the patient. This application also provides for a method of inducing or maintaining clinical remission in a human patient afflicted with Crohn's disease comprising periodically administering to the patient an amount of laquinimod effective to induce or maintain clinical remission in the patient, which amount of laquinimod is less than 0.5 mg/day.
Type:
Application
Filed:
June 26, 2017
Publication date:
October 12, 2017
Applicant:
Teva Pharmaceutical Industries, Ltd.
Inventors:
Nora Tarcic, Asi Haviv, Eran Blaugrund, Joel Kaye
Abstract: Compositions and methods for treatment of Parkinson's disease to reduce the negative side effects of the disease by administering a therapeutically effective diarylmethylpiperazine compound which exhibits delta opioid receptor agonist activity, and optionally, mu receptor antagonist activity.
Type:
Application
Filed:
June 27, 2017
Publication date:
October 12, 2017
Inventors:
KWEN-JEN CHANG, WILLIAM PENDERGAST, JONATHON D.S. HOLT
Abstract: A compound which is useful as an active ingredient for a pharmaceutical composition for treating urine storage dysfunction, voiding dysfunction, lower urinary tract dysfunction, and the like. The present inventors have found that a 2-aminothiazole derivative has an excellent muscarinic M3 receptor-positive allosteric modulator activity and is expected as an agent for preventing or treating bladder/urinary tract diseases associated with bladder contractions via a muscarinic M3 receptor, thereby completing the present invention. 2-aminothiazole derivative or a salt thereof of the present invention is expected as an agent for preventing or treating bladder/urinary tract diseases associated with bladder contractions via a muscarinic M3 receptor, for example voiding dysfunction such as underactive bladder.
Abstract: Invented is a method of treating cancer or a pre-cancerous syndrome in a mammal, including a human, in need thereof which comprises the administration of an effective amount of a non-peptide thrombopoietin (TPO) receptor agonist to such mammal, suitably a human.
Abstract: Compounds of Formula I are disclosed As well as pharmaceutically acceptable salts thereof. Methods of using said compounds and pharmaceutical compositions containing said compounds are also disclosed.
Type:
Application
Filed:
April 14, 2017
Publication date:
October 12, 2017
Inventors:
Kyla Bjornson, Eda Canales, Jeromy J. Cottell, Kapil K. Karki, Ashley A. Katana, Darryl Kato, Tetsuya Kobayashi, John O. Link, Ruben Martinez, Barton W. Phillips, Hyung-Jung Pyun, Michael Sangi, Adam J. Schrier, Dustin Siegel, James G. Taylor, Chinh V. Tran, Teresa Alejandra Trejo Martin, Randall W. Vivian, Zheng-Yu Yang, Jeff Zablocki, Sheila M. Zipfel
Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Type:
Application
Filed:
November 29, 2016
Publication date:
October 12, 2017
Inventors:
Atwood Kim CHEUNG, Donovan Noel CHIN, Natalie DALES, Aleem FAZAL, Timothy HURLEY, John KERRIGAN, Gary O'BRIEN, Lei SHU, Robert SUN, Moo Je SUNG
Abstract: The invention relates to pimobendan for use in a method of reducing the heart size and/or delaying the onset of clinical symptoms in a patient suffering from asymptomatic (occult, preclinical) heart failure, preferably congestive heart failure, due to mitral valve disease (MVD), and/or delaying the onset of heart failure, preferably congestive heart failure, in a patient suffering from asymptomatic (occult, preclinical) heart failure, preferably congestive heart failure, due to mitral valve disease (MVD), wherein the patient is preferably a mammal, more preferably a human, a dog, a cat or a horse, and most preferably a dog.
Abstract: Small molecule regulators of steroid receptor coactivator (SRC) family proteins are provided, as well as methods for their use in treating or preventing SRC-related diseases. The SRC-related diseases can include cancer, metabolic disorders, human immunodeficiency virus, neurodegenerative disorders, and/or inflammatory diseases. Also provided are methods for regulating SRC family proteins in a cell.
Type:
Application
Filed:
April 6, 2017
Publication date:
October 12, 2017
Applicant:
BAYLOR COLLEGE OF MEDICINE
Inventors:
Bert W. O'Malley, David Michael Lonard, Jin Wang, Jianming Xu, Jianwei Chen
Abstract: A modified microbubble is provided. The modified microbubble includes an albumin microbubble and a plurality of chitosan oligosaccharide lactates. The albumin microbubble includes an albumin shell and a gas core inside the albumin shell. The plurality of chitosan oligosaccharide lactates is connected to an outer surface of the albumin shell.
Abstract: The present invention is directed to imidazolin-5-one derivatives, pharmaceutical compositions containing them, and their use as FASN inhibitors, in for example, the treatment of cancer, obesity related disorders, and liver related disorders.
Abstract: This application relates to various salts and solid state forms of Compound (I). This application also relates to pharmaceutical compositions and therapeutic uses of these materials and compositions.
Type:
Application
Filed:
June 23, 2017
Publication date:
October 12, 2017
Applicant:
IGNYTA, INC.
Inventors:
Stephen J. BIERLMAIER, Ralph C. HALTIWANGER, Martin J. JACOBS
Abstract: The present invention relates to a compound having the general formula (V), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
Type:
Application
Filed:
November 28, 2016
Publication date:
October 12, 2017
Inventors:
Andrea WOLKERSTORFER, Oliver SZOLAR, Norbert HANDLER, Helmut BUSCHMANN, Stephen CUSACK, Mark SMITH, Sung-Sau So, Ronald Charles Hawley, Achyutharao Sidduri
Abstract: A pharmaceutical composition is provided which includes a pharmaceutically acceptable excipient and a pharmaceutically and physically acceptable amount of a compound selected from the group consisting of Chemical Formulas I-IV as described herein, or a pharmaceutically acceptable salt thereof. Also provided are methods of increasing a level of a defined neurotrophic peptide in an organism or tissue comprising the administration of a pharmaceutically and physically acceptable amount of one or more of the compositions described above, and a method for treating a neurodegenerative disease in a subject in need thereof, the method comprising administering a therapeutically effective amount of the pharmaceutical composition of claim 1.
Abstract: The invention relates to novel compounds of the formula (I) which can be used for the inhibition of serine-threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation.
Type:
Application
Filed:
June 26, 2017
Publication date:
October 12, 2017
Inventors:
Thomas Fuchss, Ulrich Emde, Hans-Peter Buchstaller, Werner Mederski
Abstract: The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
Type:
Application
Filed:
November 22, 2016
Publication date:
October 12, 2017
Inventors:
Kevin Wayne Kuntz, John Emmerson Campbell, Masashi Seki
Abstract: The present application provides novel quinazolines and azaquinazolines and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in for co-regulating RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR pathways by administering a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, T and R4, and R6 to R8? are defined herein, to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR pathways. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.
Type:
Application
Filed:
April 28, 2017
Publication date:
October 12, 2017
Inventors:
Scott K. Thompson, Roger A. Smith, Sanjeeva Reddy, Tyler M. John, Vijay Kumar Nyavanandi, Hosahalli Subramanya, Vijay Potluri, Sunil Kumar Panigrahi, Prabhakara Rao Nadipalli, Saumitra Sengupta
Abstract: The present disclosure relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR3 and/or FGFR4 enzyme and are useful in the treatment of FGFR-associated diseases.
Type:
Application
Filed:
June 20, 2017
Publication date:
October 12, 2017
Inventors:
Liang Lu, Bo Shen, Alexander Sokolsky, Xiaozhao Wang, Liangxing Wu, Wenqing Yao, Yingda Ye
Abstract: The present invention provides a novel corneal thickness modulating agent. The present invention pertains to a corneal thickness modulating agent containing 1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine or a salt thereof or a solvate thereof.
Abstract: An aqueous composition having an excellent antiseptic effect is provided. An aqueous composition comprising a compound represented by Formula (1), wherein X represents a halogen atom, or a salt thereof, or a solvate of the compound or the salt thereof, and a quaternary ammonium surfactant.
Abstract: Provided are novel compounds which are capable of inhibiting an activity of RNA polymerase I, and uses thereof in treating diseases or disorders modulated by RNA polymerase I, preferably autoimmune diseases such as multiple sclerosis and proliferative diseases.
Type:
Application
Filed:
June 19, 2017
Publication date:
October 12, 2017
Applicant:
Tel HaShomer Medical Research Infrastructure and Services, Ltd.
Inventors:
Anat ACHIRON, Roi MASHIACH, Michael GUREVICH
Abstract: A method of increasing abundance of hematopoietic stem cells and progenitor cells and an adjuvant method of radiotherapy based treatment for radioprotection of the subject against ?-radiation toxicity and/or IR-induced death of cancer cells involving pharmaceutically effective dosages of chlorophyllin or a pharmaceutically acceptable salt thereof. The advancement is directed to selectively protect normal hematopoietic stem cells and/or sensitizes radio-resistant cancer cells to gamma radiation thereby lowering the risk of normal tissue radiation toxicity. The effective dose of the CHL formulation synergistically improves the outcome of radiotherapy for cancer when administered to the subject prior the radiotherapy for treating cancer. Also disclosed is kit having chlorophyllin containing therapeutic preparation for treating indications selected from reduction in hematopoietic stem cells and progenitor cells (HSPCs) and/or protection against whole body irradiation induced mortality.
Abstract: The present invention relates to methods of treating or preventing respiratory infections, in particular respiratory infections in patients with an underlying respiratory disorder such as chronic obstructive pulmonary disease (COPD). The present invention also relates to methods of treating or preventing COPD or COPD exacerbations. The invention particularly describes the role of Notch 3 and/or Notch 4 signalling in such methods and the use of Notch 3 and/or Notch 4 as therapeutic and screening targets.
Type:
Application
Filed:
September 22, 2015
Publication date:
October 12, 2017
Inventors:
Soren BEINKE, Nikolai Nikolaevich BELYAEV, Edith HESSEL
Abstract: Provided are methods for slowing, halting, and reversing gray matter atrophy and progression of disability in certain neurodegenerative diseases, including multiple sclerosis, using estrogen, alone or in combination with another agent.
Type:
Application
Filed:
September 1, 2015
Publication date:
October 12, 2017
Applicant:
The Regents of the University of California
Abstract: The present invention relates to an injectable polymer matrix drug delivery system comprising a biodegradable polymer, a solvent or a combination of solvents, and an active pharmaceutical ingredient.
Abstract: Novel methods for prevention, reduction or elimination of the incidence of male androgen deficiency symptoms or diseases including male hypogonadism-associated symptoms and diseases associated with low serum testosterone and/or low DHEA or low total androgens in susceptible warm-blooded animals including humans involving administration of an amount of a sex steroid precursor, particularly dehydroepiandrosterone (DHEA) and a selective estrogen receptor modulator (SERM) (particularly acolbifene), an antiestrogen or a prodrug of the two.
Abstract: This disclosure relates to compositions, kits and methods for non-surgical reduction of localized subcutaneous fat such as that associated with a cosmetic fat accumulation. The methods employ compositions having specific concentrations of a salt of deoxycholic acid which provides a superior fat cell necrosis with modest adverse effects. Examples of localized subcutaneous fat are found in the submental area, in particular under the chin.
Abstract: A mechanism whereby aberrant Shh signaling converges on the Akt1-mTOR pathway, conferring selective growth advantage and enhanced survival of tumor cells has been identified. Utilizing a mouse model of BCNS, a pivotal role has been discovered for Akt1 signaling in BCC tumorigenesis. Based on the results described here certain embodiments are directed to methods and pharmaceutical formulations for treating BCC/BCNS, other cancers that are Shh+ and Akt+, cancers that are Shh+ and mTOR plus and cancers that are Shh+ by administering therapeutically effective amounts of various combinations of Akt inhibitors, Shh pathway inhibitors such as SMO inhibitors, and mTOR inhibitors.
Type:
Application
Filed:
September 8, 2015
Publication date:
October 12, 2017
Applicant:
The Trustees of Columbia University in the City of New York
Inventors:
Arianna L. Kim, David Bickers, Mohammad Athar
Abstract: The invention relates to compositions of nicotinamide mononucleotide derivatives and their methods of use. The invention also relates to methods of preparing nicotinamide mononucleotide derivatives. The invention relates to pharmaceutical compositions and nutritional supplements containing a nicotinamide mononucleotide derivative. The invention relates to methods of using nicotinamide mononucleotide derivatives that promote the increase of intracellular levels of nicotinamide adenine dinucleotide (NAD+) in cells and tissues for treating diseases and improving cell and tissue survival.
Type:
Application
Filed:
August 5, 2016
Publication date:
October 12, 2017
Inventors:
Karl D. Normington, David A. Sinclair, David J. Livingston, James M. McKearin, Bruce Szczpankiewicz, Jonathan N. Kremsky
Abstract: The present invention provides a method of treating or preventing type 2 diabetes and hyperlipidemia in a subject in need thereof, comprising administrating to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a pharmaceutical composition for treatment or prevention of type 2 diabetes and hyperlipidemia, comprising a compound of formula I and a pharmaceutically acceptable carrier. Through down-regulation of PEPCK, G6Pase, 11?-HSD1, DGAT2, and GPAT, up-regulation of PPAR? and adiponectin, and promotion of membrane GLUT4 expression and phosphorylation of AMPK and Akt, the compound of formula I of the present invention exerts antidiabetic and antihyperlipidemic effects, including reduced weight of visceral fat, decreased blood levels of triglycerides, free fatty acids, glucose, insulin, and leptin as well as decreased hepatic levels of total lipid and triacylglycerol. The compound of formula I also inhibits adipocyte hypertrophy and hepatic ballooning.
Abstract: The present technology relates generally to micelle formulations of amphotericin B that optionally include 5-fluorocytosine and methods of preparing such formulations. Methods of treating fungal infections with the present compositions are also provided.
Abstract: The present application relates to methods to facilitate the solubilization of beta-1,3-glucan in solution, for instance an aqueous or organic solvent and uses thereof to enhance immune function in an individual. Others aspects of the present invention relate to administering compositions or mixtures comprising solubilized beta-1,3-glucan to enhance immune function in humans or animals.
Type:
Application
Filed:
April 12, 2017
Publication date:
October 12, 2017
Inventors:
Geoffrey Paul HORST, Robert Bernard LEVINE
Abstract: In various embodiments, the present application teaches numerous compositions that include water clusters and methods of use thereof. In some embodiments, the present application teaches compositions and methods for treating, preventing and promoting the prophylaxis of bacterial infections in plants and animals. The present application further teaches compositions and methods for treating the surfaces of non-living substrates upon which bacteria are known or thought to reside. The present invention also teaches methods for adding compositions that include water clusters to foods and feed.
Abstract: A silicate-doped hydroxyapatite material has an ordered and directional growth structure. The silicon content in the silicate-doped hydroxyapatite material ranges from 0.1 wt % to 1.6 wt %, and silicon is doped in hydroxyapatite lattices in a form of silicate. A template-induced method for manufacturing the synthetic silicate-doped hydroxyapatite material above.
Abstract: Activated carbon (for example medicinal carbon), which has long been used for adsorbing and removing harmful substances from the digestive system, has the drawback of causing constipation, and the production of a spherical adsorbent carbon that is believed to overcome this drawback from a petroleum-based hydrocarbon requires a complicated production process. These issues can be addressed by an oral adsorbent, a therapeutic or prophylactic agent for kidney disease, and a therapeutic or prophylactic agent for liver disease, containing a fibrous carbonaceous substance obtained by carbonizing cotton fiber. The issues can also be addressed by an oral adsorbent, a therapeutic or prophylactic agent for kidney disease, and a therapeutic or prophylactic agent for liver disease, containing a fibrous carbonaceous substance having a twisted hollow ribbon-like structure.
Abstract: The present invention includes vaccine compositions and methods for using these vaccine compositions in active immunotherapy. The vaccine compositions include allogeneic activated Th1 memory cells. The compositions can also include one or more disease-related antigens. The methods include administering the vaccine compositions to provide a Th1 footprint in normal individuals or patients susceptible to disease or having minimal residual disease.