Abstract: The disclosure herein generally relates to methods of treating an overweight or obese condition, and overweight- or obesity-related conditions. In one embodiment, the disclosure provides a method of treating an overweight or obese condition involving administering to the subject in need thereof, an amount of a pharmaceutical composition including a MetAP-2 inhibitory compound, or a salt, ester, or prodrug thereof, effective to result in weight loss in the subject.
Abstract: The present invention discloses novel difunctional monomers compound containing pendant clickable furyl group of formula (I), process for the preparation and polymers prepared there from. wherein, X is selected from —COOCH3, —COOH, —CON3, —NCO, —CONHNH2, —CH2OH n is selected from 2 to 12.
Type:
Application
Filed:
December 16, 2015
Publication date:
January 18, 2018
Applicant:
COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
Abstract: The invention relates to compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, a method of synthesis of said compounds, pharmaceutical compositions comprising them and their use in the treatment and/or prevention of conditions mediated by H1 histamine receptor, such as allergic disorders or diseases.
Type:
Application
Filed:
December 28, 2015
Publication date:
January 18, 2018
Inventors:
Rosa RODES SOLANES, Roberto OLIVERA TIZNE, Gonzalo HERNÁNDEZ HERRERO, Victor RUBIO ROYO, Francisco LEDO GÓMEZ
Abstract: Described herein are compounds that are somatostatin modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of somatostatin activity.
Type:
Application
Filed:
July 12, 2017
Publication date:
January 18, 2018
Inventors:
Jian ZHAO, Sangdon HAN, Sun Hee KIM, Shimiao WANG, Yunfei ZHU
Abstract: A medicament or pharmaceutical composition for the treatment of a respiratory tract disease, which is a compound having the following formula: or a pharmaceutically acceptable salt thereof. A method of treating a respiratory tract disease includes administering to a patient an effective amount of the compound or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
September 28, 2017
Publication date:
January 18, 2018
Inventors:
Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova
Abstract: A medicament or pharmaceutical composition for the treatment of exacerbations of asthma and chronic obstructive pulmonary disease, which is a compound having the following formula: or a pharmaceutically acceptable salt thereof. A method of treating exacerbations of asthma and chronic obstructive pulmonary disease includes administering to a patient an effective amount of the compound or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
September 28, 2017
Publication date:
January 18, 2018
Inventors:
Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova
Abstract: A medicament or pharmaceutical composition for the treatment of respiratory syncytial virus, which is a compound having the following formula: or a pharmaceutically acceptable salt thereof. A method of treating respiratory syncytial virus includes administering to a patient an effective amount of the compound or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
September 28, 2017
Publication date:
January 18, 2018
Inventors:
Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova
Abstract: A method for preparing a compound of formula I: or a pharmaceutically acceptable salt thereof, by heating of dicarboxylic acid monoamide of formula II with a dehydrating agent in an organic solvent.
Type:
Application
Filed:
September 28, 2017
Publication date:
January 18, 2018
Inventors:
Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova
Abstract: Disclosed are a 2-(2,4,5-substituted aniline) pyrimidine derivative, a pharmaceutical composition and a use thereof. The pharmaceutical composition comprises a therapeutically effective amount of the 2-(2,4,5-substituted aniline) pyrimidine derivative, a solvate, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient. Also disclosed is a use of the 2-(2,4,5-substituted aniline) pyrimidine derivative, a solvate, or a pharmaceutically acceptable salt thereof in the preparation of drugs for treating cancers. The compounds of the present invention have a relatively high solubility in water and a relatively high permeability, and/or a relatively low binding ability to plasma proteins, and at the same time have a relatively low toxicity characteristic and a relatively high anti-tumor activity.
Abstract: The invention relates to compounds of formula (I), or a pharmaceutically acceptable salt thereof: Formula (I) which possess inhibitory activity against activating mutant forms of EGFR, and are accordingly useful for their anti-cancer activity and in methods of treatment of the human or animal body. The invention also relates pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.
Abstract: Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
Abstract: Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity.
Type:
Application
Filed:
September 27, 2017
Publication date:
January 18, 2018
Applicant:
TEMPLE UNIVERSITY OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
Inventors:
Daniel J. CANNEY, Benjamin E. BLASS, Rong GAO, Magid ABOU-GHARBIA
Abstract: Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity.
Type:
Application
Filed:
September 27, 2017
Publication date:
January 18, 2018
Applicant:
TEMPLE UNIVERSITY OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
Inventors:
Daniel J. CANNEY, Benjamin E. BLASS, Rong GAO, Magid ABOU-GHARBIA
Abstract: The present invention provides compounds of Formula (I); and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
Abstract: The present disclosure discusses salt forms of 4-cyano-N-[2-(4,4-dimethylcyclohex-1-en-1-yl)-6-(2,2,6,6-tetramethyltetrahydro-2H-pyran-4-yl)pyridin-3-yl]-1H-imidazole-2-carboxamide.
Abstract: Compounds of formula (I) are both phosphodiesterase 4 (PDE4) enzyme inhibitors and muscarinic M3 receptor antagonists and are useful for the prevention and/or treatment of diseases of the respiratory tract characterized by airway obstruction.
Type:
Application
Filed:
September 28, 2017
Publication date:
January 18, 2018
Applicant:
CHIESI FARMACEUTICI S.p.A.
Inventors:
Elisabetta ARMANI, Gabriele Amari, Wesley Blackaby, Herve Van De Poel, Charles Baker-Glenn, Naimisha Trivedi
Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, and R6 are as described herein. The compounds of Formula I are agonists of the kappa opioid receptor and relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology, organic chemistry and polymer chemistry.
Type:
Application
Filed:
September 28, 2017
Publication date:
January 18, 2018
Inventors:
Neel K. Anand, Franco J. Duarte, Wen Zhang, Zhongxu Ren
Abstract: Compounds of formula I defined herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.
Type:
Application
Filed:
July 12, 2017
Publication date:
January 18, 2018
Applicant:
CHIESI FARMACEUTICI S.P.A.
Inventors:
Fabio RANCATI, Andrea Rizzi, Laura Carzaniga, Ian Linney, Chris Knight, Wolfgang Schmidt
Abstract: The present invention discloses a novel EGFR inhibitor compound of formula (1), process for preparation thereof and methods of treating abnormal cell growth in mammals by administering the compounds of formula (1) wherein, R is selected from hydrogen, alkyl, nitro, halogens such as chlorine, bromine, fluorine and iodine; R1=hydrogen, alkyl, alkoxy, aryl, nitro, halogens such as chlorine, bromine, fluorine and iodine, trifluoromethyl, thioalkyl, trifluromethoxy, trialkylsilyl.
Abstract: The present disclosure relates to novel compounds, pharmaceutical compositions containing such compounds, and their use in prevention and treatment of estrogen-related diseases and conditions.
Abstract: Disclosed are a series of diaza-benzofluoranthrene compounds. The present invention particularly relates to a compound represented by formula (I), pharmaceutically acceptable salts or tautomers thereof.
Abstract: A novel class of fluorinated derivatives of Formula (I) have been prepared and found to be useful in the treatment of cancers and other disorders related mediated by Bromodomain-Containing Proteins.
Abstract: The invention relates to novel compounds of the formula (I) in which the R1, R2a, R2b, R3, A1, A2, A4 and n have the meanings given above, to their usee as acaricides and/or insecticides for controlling animal pests and to processes and intermediates for their preparation.
Type:
Application
Filed:
February 2, 2016
Publication date:
January 18, 2018
Inventors:
RUEDIGER FISCHER, DAVID WILCKE, KERSTIN ILG, DANIELA PORTZ, ULRICH GOERGENS, SASCHA EILMUS, OLGA MALSAM, ANDREAS TURBERG
Abstract: The present invention relates to compounds of formula I, wherein A1, A2, A3, R1, R2, R3, R4, R5, R6, L, Ar and Q are each as defined herein. The compounds of the present invention are inhibitors of autotaxin (ATX) enzyme activity. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions (e.g. fibrosis) in which ATX activity is implicated.
Type:
Application
Filed:
February 4, 2016
Publication date:
January 18, 2018
Applicant:
CANCER RESEARCH TECHNOLOGY LIMITED
Inventors:
Martin Lee STOCKLEY, Ellen Catherine MACDONALD, Pritom SHAH, Allan JORDAN, James HITCHIN, Niall HAMILTON
Abstract: A compound according to Formula Ia: wherein Cy, L1, G, and R1 are as described herein. The present invention relates to novel compounds according to Formula I that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (IBD), rheumatoid arthritis, vasculitis), lung diseases (e.g. chronic obstructive pulmonary disease (COPD) and lung interstitial diseases (e.g. idiopathic pulmonary fibrosis (IPF))), neuroinflammatory conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.
Type:
Application
Filed:
May 30, 2017
Publication date:
January 18, 2018
Applicant:
GALAPAGOS NV
Inventors:
Frédéric Gilbert LABÉGUÈRE, Gregory John Robert NEWSOME, Luke Jonathan ALVEY, Laurent Raymond Maurice SANIÈRE, Stephen Robert FLETCHER
Abstract: The invention relates to fluorinated compounds and their use as integrin receptor antagonists. Novel fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives and pharmaceutically acceptable salts or solvates thereof and their use are described.
Type:
Application
Filed:
September 26, 2017
Publication date:
January 18, 2018
Inventors:
Ben C. ASKEW, Richard W. HEIDEBRECHT, Takeru FURUYA, Mark E. DUGGAN
Abstract: This invention relates to novel imidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(1H)-one compounds, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions alone or in combination with other therapeutics in the treatment of diseases and conditions that are beneficially treated by administering an inducer of the gene encoding tumor necrosis factor (TNF) related apoptosis-inducing ligand (TRAIL) superfamily member 10.
Abstract: The invention relates to imidazo[1,2-a]quinoxaline compounds of formula (I) for the treatment of cancer, the pharmaceutical compositions comprising said chemical compounds, and the therapeutic uses thereof.
Type:
Application
Filed:
December 30, 2015
Publication date:
January 18, 2018
Inventors:
Carine Deleuze-Masquefa, Pierre-Antoine Bonnet, Pierre Cuq, Cindy Patinote
Abstract: Provided is a compound capable of effectively control worst weeds of higher leaf stages that present practical problems. A specific pyrazolylpyrazole derivative of formula (I) is disclosed that is able to solve the above-mentioned problems.
Abstract: Provided herein are formulations, methods and substituted tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds.
Type:
Application
Filed:
May 31, 2017
Publication date:
January 18, 2018
Inventors:
Michael O' Neil Hanrahan Clarke, Edward Doerffler, Richard L. Mackman, Dustin Siegel
Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
Type:
Application
Filed:
August 11, 2016
Publication date:
January 18, 2018
Inventors:
Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Li-Huei Tsai, Stephen J. Haggarty, Yan-Ling Zhang
Abstract: The present invention provides solid state forms of certain spiro-oxindole compounds, such as funapide and the racemic mixture of funapide and its corresponding (R) enantiomer, pharmaceutical compositions comprising the solid state forms and processes for preparing the solid state forms and the pharmaceutical compositions.
Type:
Application
Filed:
June 16, 2017
Publication date:
January 18, 2018
Inventors:
Ronen Ben-David, Stephen Bierlmaier, Ralph Curtis Haltiwanger, Alexandr Jegorov, Raeann Ruiyun Wu, Mehran Yazdanian
Abstract: The invention relates to a polymorphic forms of (S)-3-(3-(1-methyl-2-oxo-5-(pyrazolo[1,5-a]pyridine-3-yl)-1H-imidazo[4,5-b]pyridine-3(2H)-yl)piperidin-1-yl)-3-oxopropanenitrile and their use as a therapeutic agent for the treatment of respiratory diseases.
Abstract: This invention provides, among other things, novel compounds useful for treating bacterial infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
Type:
Application
Filed:
September 28, 2017
Publication date:
January 18, 2018
Inventors:
Stephen J. Baker, Vincent S. Hernandez, Rashmi Sharma, James A. Nieman, Tsutomu Akama, Yong-Kang Zhang, Jacob J. Plattner, Michael Richard Kevin Alley, Rajeshwar Singh, Fernando Rock
Abstract: Siloxanes which are liquid at 25° C. and 1 bar, have 2% to 12% by weight of silanol groups and are of the formula (1): MaDbTcQdM?eD?fT?g ??(1), are prepared by reacting metal salts of silanols of the formula (2): R1Si(OH)4?l?m(O?Zr+/r)m ??(2) or condensation products thereof with silanes of the formula (3): R?nSiX4?n ??(3) in a ratio which is calculated by: mol of organosiliconate of the general formula (2): mol of silane of the general formula (3)= x*(4?n)/m, where x=0.8 to 1.2.
Abstract: A method of stabilizing imino-functional silane involving adding thereto at least one Brønsted-Lowry base to inhibit, suppress or prevent the addition reactions of the imino-functional silane with itself to form a imino- and amino-functional silane and the subsequent deamination reactions to form conjugated carbon-carbon double bond-containing imino-functional silanes and stabilized imino-functional silanes containing the at least one Brønsted-Lowry base.
Abstract: Compounds of formula (I) wherein: Ak1 represents an alkyl chain, X represents —(CH2)m—, —CH(R)—, —N(R)—, —CH2—N(R)—, —N(R)—CH2— or —CH2—N(R)—CH2—, m and R are as defined in the description, R1 and R2 each represent H when X represents —(CH2)m—, —CH(R)—, —N(R)—, —CH2—N(R)— or —N(R)—CH2—, or together form a bond when X represents —CH2—N(R)—CH2—, R3 represents NH2, Cy-NH2, Cy-Ak3-NH2 or piperidin-4-yl, Cy and Ak3 are as defined in the description, R4 and R5, which may be identical or different, each represent H or F, their optical isomers, and addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in treating conditions requiring a TAFIa inhibitor.
Type:
Application
Filed:
January 13, 2017
Publication date:
January 18, 2018
Inventors:
Philippe GLOANEC, Arnaud-Pierre SCHAFFNER, Patricia SANSILVESTRI-MOREL, Alain RUPIN, Philippe MENNECIER, Marie-Odile VALLEZ
Abstract: There is provided a redox-sensitive compound comprising a redox-sensitive organometallic moiety and a phospholipid or modified-phospholipid moiety. The compound is embodied in a redox-sensitive drug delivery system. In preferred embodiments, the system comprises redox active giant unilamellar vesicles (GUVs), which are used as drug delivery vessels.
Type:
Application
Filed:
January 19, 2016
Publication date:
January 18, 2018
Inventors:
JANINE MAUZEROLL, TOMER AHARON MOYHOUZER, MICHAEL EDWARD SNOWDEN, PHILIPPE DAUPHIN DUCHARME, STEPHANI MAZURKIEWICZ, CHLOÉ L'HOMME, SAMUEL DESJARDINS, SYLVAIN CANESI
Abstract: The present disclosure provides novel compounds that are steviol derivatives. The compounds generally can be characterized by a structure according to Formula I: wherein A1, L1, and G1 are described herein. Also provided are sweetener compositions comprising the compound described herein either as a sweetener or a sweetener enhancer. Additionally, the compound or the sweetener composition can be included in a product such as a beverage product or a food product, which can reduce the amount of sweetener in the product required to achieve the same sweetness level in an otherwise identical product not including the compound or the sweetener composition.
Type:
Application
Filed:
July 15, 2016
Publication date:
January 18, 2018
Inventors:
William BONORDEN, Shawn ERICKSON, Christophe GALOPIN, Laura NATTRESS
Abstract: The present invention relates to a process for the preparation of diosmin from hesperidin. The process involves the oxidation of acylated hesperidin with iodine or bromine in a C2-C4 carboxylic acid medium and subsequent treatment with an inorganic base to partially neutralize the acidic media. The process allows obtaining diosmin with low iodine or bromine content, avoiding the use of organic solvents.
Abstract: The present disclosure provides a solid phase method of making oligonucleotides via sequential coupling cycles including at least one coupling of a dinucleotide dimer subunit to a free 3?-terminal group of a growing chain. The oligonucleotides include at least two nucleoside subunits joined by a N3??P5? phosphoramidate linkage. The method may include the steps of (a) deprotecting the protected 3? amino group of a terminal nucleoside attached to a solid phase support, said deprotecting forming a free 3? amino group; (b) contacting the free 3? amino group with a 3?-protected amino-dinucleotide-5?-phosphoramidite dimer in the presence of a nucleophilic catalyst to form an internucleoside N3??P5? phosphoramidite linkage; and (c) oxidizing (e.g., sulfurizing) the linkage. The compositions produced by the subject methods may include a reduced amount of one or more (N?x) oligonucleotide products. Also provided are pharmaceutical compositions including the subject oligonucleotide compositions.
Abstract: The present disclosure provides a solid phase method of making oligonucleotides via sequential coupling cycles including at least one coupling of a dinucleotide dimer subunit to a free 3?-terminal group of a growing chain. The oligonucleotides include at least two nucleoside subunits joined by a N3??P5? phosphoramidate linkage. The method may include the steps of (a) deprotecting the protected 3? amino group of a terminal nucleoside attached to a solid phase support, said deprotecting forming a free 3? amino group; (b) contacting the free 3? amino group with a 3?-protected amino-dinucleotide-5?-phosphoramidite dimer in the presence of a nucleophilic catalyst to form an internucleoside N3??P5? phosphoramidite linkage; and (c) oxidizing (e.g., sulfurizing) the linkage. The compositions produced by the subject methods may include a reduced amount of one or more (N?x) oligonucleotide products. Also provided are pharmaceutical compositions including the subject oligonucleotide compositions.
Abstract: The invention relates to compounds of Formula A: or a salt, solvate, hydrate, or prodrug thereof. The compounds of Formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, liver disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.
Abstract: The automated synthesis of clinically relevant amounts of 16?-18F-fluoro-5?-dihydrotestosterone (18F-FDHT) using a commercially available radiosynthesizer. Synthesis was performed in 90 minutes with a decay-corrected radiochemical yield of 29±5%. The specific activity was 4.6 Ci/?mol (170 GBq/?mol) at end of formulation with a starting activity of 1.0 Ci (37 GBq). The formulated 18F-FDHT yielded sufficient activity for multiple patient doses and passed all quality control tests required for routine clinical use.
Type:
Application
Filed:
February 3, 2016
Publication date:
January 18, 2018
Applicant:
THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Inventors:
Jennifer Marie Murphy, Mark Saul Lazari
Abstract: The present invention relates to crystalline forms of S-[4-(3-fluoro-3-methylbutyryloxy)but-2-ynyl] 6?,9?-difluoro-17?-(furan-2-yl)carbonyloxy-11?-hydroxy-16?-methyl-3-oxoandrosta-1,4-diene-17?-carbothioate, an anti-inflammatory and anti-allergic glucocorticoid compound.
Abstract: It is intended to provide a novel terpenoid derivative that exhibits anti-inflammatory action and a cytoprotective action by activating the Keap1/Nrf2/ARE signaling pathway.