Abstract: The present disclosure is directed, in part, to compounds, or pharmaceutically acceptable salts thereof, for the treatment and/or prevention of neurodegenerative disease and/or mitchonodrial disease including Parkinson's disease and Leigh's disease.
Abstract: The present invention provides small molecules inhibitors of BMP signaling and compositions and methods for inhibiting BMP signaling. These compounds and compositions may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. These compounds and compositions may also be used to reduce circulating levels of ApoB-100 or LDL and treat or prevent acquired or congenital hypercholesterolemia or hyperlipoproteinemia; diseases, disorders, or syndromes associated with defects in lipid absorption or metabolism; or diseases, disorders, or syndromes caused by hyperlipidemia.
Type:
Application
Filed:
March 25, 2015
Publication date:
July 6, 2017
Inventors:
Paul B. Yu, Gregory D. Cuny, Agustin H. Mohedas
Abstract: The present invention is directed to a compound of formula (I): or a crystalline form thereof, or a solvate thereof; to a solid pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula (I), or a crystalline form thereof, or a solvate thereof, and at least one pharmaceutically acceptable carrier or diluent, and to the use of a compound of formula (I), or a crystalline form thereof, or a solvate thereof, for treating a patient suffering from, or subject to, a disease, disorder, or condition mediated by Aurora kinase, and methods related thereto.
Type:
Application
Filed:
October 13, 2016
Publication date:
July 6, 2017
Inventors:
Ian Armitage, Martin I. Cooper, Mark D. Eddleston, Neil C. Faiber, Quentin J. McCubbin, Stephen W. Watt
Abstract: Novel crystalline forms of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide free base and 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide mono hydrochloride, pharmaceutical compositions thereof and methods of their preparation and use are disclosed herein.
Type:
Application
Filed:
November 2, 2016
Publication date:
July 6, 2017
Inventors:
Christopher K. Murray, Leonard W. Rozamus, John J. Chaber, Pradeep Sharma
Abstract: The invention provides compounds of Formula I or Formula II: or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.
Type:
Application
Filed:
November 9, 2016
Publication date:
July 6, 2017
Inventors:
Kerim Babaoglu, Constantine G. Boojamra, Eugene J. Eisenberg, Hon Chung Hui, Richard L. Mackman, Jay P. Parrish, Michael Sangi, Oliver L. Saunders, Dustin Siegel, David Sperandio, Hai Yang
Abstract: The present invention provides compounds useful for treating or preventing a brain-related disease or disorder. The present invention further provides a method of treating or preventing a brain-related disease or disorder in a patient, comprising administering to the patient a pharmaceutical composition comprising at least one compound of the invention. The present invention further provides a method of modulating the activity of a monoamine transporter.
Type:
Application
Filed:
December 16, 2016
Publication date:
July 6, 2017
Inventors:
Sandhya KORTAGERE, Ole MORTENSEN, Andreia C. K. MORTENSEN, Joseph M. SALVINO
Abstract: A pharmaceutical composition is provided which includes perillyl alcohol conjugated with a therapeutic agent and further includes and a hydrolyzable acylated aliphatic tail. A method of using the pharmaceutical composition is also provided for treating a condition or disease of a patient, e.g., cancer.
Type:
Application
Filed:
March 17, 2017
Publication date:
July 6, 2017
Inventors:
Thomas Chen, Daniel Levin, Satish Puppali
Abstract: Provided are compounds represented by the formula: In which: Y is an unbranched, saturated or unsaturated hydrocarbon chain with 2-5 hydrocarbon atoms R1=aryl R2?NR3R4 wherein R3 and R4 together form a heterocycle or R2=4-substitutedcyclohexyl, 1-substitutedpiperidine-4-yl or imidazo(1,2-a)azine-2-yl when Y is as defined above and R1 is a heterocycle other than benzothiophene pharmaceutically acceptable salts thereof, deuterated forms thereof, isomers thereof, solvates thereof, and mixtures thereof. The compounds can be used for treating a patient suffering from a condition that is capable of treatment with a partial agonist or antagonist of the dopamine D2/D3 receptors.
Abstract: Provided herein are compounds of the formulas (I) and (II): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of Retinoic Acid Receptor-Related Orphan Receptor regulated diseases and disorders.
Type:
Application
Filed:
July 24, 2015
Publication date:
July 6, 2017
Inventors:
Anderson Gaweco, Jefferson Tilley, James Blinn
Abstract: Provided herein are substituted fused quadracyclic compounds useful as inhibitors of MK2. The invention further provides pharmaceutical compositions of the compounds of the invention. The invention also provides medical uses of substituted fused quadracyclic compounds.
Type:
Application
Filed:
January 3, 2017
Publication date:
July 6, 2017
Inventors:
Casey C. McComas, Michael H. Serrano-Wu, Joseph P. Vacca
Abstract: Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
Type:
Application
Filed:
March 23, 2017
Publication date:
July 6, 2017
Inventors:
Gabriella TRAQUANDI, Maria Gabriella BRASCA, Roberto D'ALESSIO, Paolo POLUCCI, Fulvia ROLETTO, Anna VULPETTI, Paolo PEVARELLO, Achille PANZERI, Francesca QUARTIERI, Ron FERGUSON, Paola VIANELLO, Daniele FANCELLI
Abstract: The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-{[4-(substituted pyridine)-2-yl]methyl}-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production.
Abstract: The present disclosure describes furo- and thieno-pyridine carboxamide compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
Type:
Application
Filed:
December 15, 2016
Publication date:
July 6, 2017
Inventors:
Yun-Long Li, David M. Burns, Hao Feng, Taisheng Huang, Song Mei, Jun Pan, Oleg Vechorkin, Hai-Fen Ye, Wenyu Zhu, Maria Rafalski, Anlai Wang, Chu-Biao Xue
Abstract: Compounds and compositions, and methods of use thereof, are provided and have utility in inhibiting hedgehog signaling and/or phosphodiesterase-4 activity.
Type:
Application
Filed:
March 7, 2017
Publication date:
July 6, 2017
Inventors:
Charles C. Hong, Charles H. Williams, Jonathan Hempel, TK Feaster, Don H. Rubin, Gary Sulikowski, Jijun Hao, Audrey Frist
Abstract: There is provided a 5,6-dihydro-4H-benzo[b]thieno-[2,3-d]azepine derivative which is useful in the treatment of respiratory syncytial virus (RSV) infection and for the prevention of disease associated with RSV infection. (Formula (1)).
Type:
Application
Filed:
October 8, 2015
Publication date:
July 6, 2017
Applicant:
Akliebolaget SKF
Inventors:
Simon Fraser HUNT, Stuart Thomas ONIONS, Vladimir SHERBUKHIN, Euan Alexander FORDYCE, Peter John MURRAY, Daniel William BROOKES, Kazuhiro ITO, Peter STRONG
Abstract: The present invention relates to a process for the preparation of a solid form of the gadobenate dimeglumine compound that comprises obtaining a solution of the said compound in a suitable solvent A wherein the amount by weight of the water optionally present in the solution is at most equal to or lower than the amount by weight of the gadobenate dimeglumine comprised in the solution and adding the obtained solution to an organic solvent B, acting as an appropriate antisolvent and favoring the formation of a solid form of the gadobenate dimeglumine that can be collected by filtration.
Type:
Application
Filed:
July 20, 2015
Publication date:
July 6, 2017
Applicant:
BRACCO IMAGING S.P.A.
Inventors:
Roberta MAZZON, Roberta FRETTA, Pier Lucio ANELLI
Abstract: Disclosed are Si-containing film forming compositions comprising alkylamino-substituted carbosilane precursors, methods of synthesizing the same, and their use for vapor deposition processes.
Type:
Application
Filed:
July 9, 2015
Publication date:
July 6, 2017
Inventors:
Claudia FAFARD, Glenn KUCHENBEISER, Venkateswara R. PALLEM, Jean-Marc GIRARD
Abstract: Provided is an alkoxysilyl-vinylene group-containing silicon compound represented by the following general formula (1): wherein each of R1 and R2 independently represents a monovalent hydrocarbon group having 1 to 20 carbon atoms; R represents a monovalent hydrocarbon group having an organic functional group(s) and 1 to 30 carbon atoms; and n represents an integer of 1 to 3. The alkoxy groups in the novel organic silicon compound of the invention have a dramatically improved hydrolyzability. Further, a high adhesion or adhesiveness; and a fast adhesiveness can be exhibited by adding the novel organic silicon compound to a room temperature curable organopolysiloxane.
Abstract: Disclosed herein are dialkyl cobalt complexes containing pyridine di-imine ligands and their use as catalysts for hydrosilylation, dehydrogenative silylation, and/or crosslinking processes.
Type:
Application
Filed:
May 7, 2015
Publication date:
July 6, 2017
Inventors:
Tianning DIAO, Paul CHIRIK, Aroop ROY, Johannes DELIS, Kenrick LEWIS
Abstract: A novel method and system for using certain tin compounds as dopant sources for ion implantation are provided. A suitable tin-containing dopant source material is selected based on one or more certain attributes. Some of these attributes include stability at room temperature; sufficient vapor pressure to be delivered from its source supply to an ion chamber and, the ability to produce a suitable beam current for ion implantation to achieve the required implant Sn dosage. The dopant source is preferably delivered from a source supply that actuates under sub atmospheric conditions to enhance the safety and reliability during operation.
Type:
Application
Filed:
December 21, 2016
Publication date:
July 6, 2017
Inventors:
Aaron Reinicker, Ashwini K. Sinha, Qiong Guo
Abstract: The present invention is characterized in that racemic or optically active D- or L-?-glycerophosphoryl choline solids are prepared from liquid type racemic or optically active D- or L-?-glycerophosphoryl choline using an organic solvent. The present invention can produce solids at a high yield more easily through phase transformation rather than a method using a difference in solubility in a solvent, which is an existing method.
Type:
Application
Filed:
March 24, 2017
Publication date:
July 6, 2017
Inventors:
Soon Ook HWANG, Dae Myoung YUN, Chang-min KIM
Abstract: The present invention relates to a phosphazene compound and a prepreg and a composite metal laminate. The phosphazene compound has a structure as shown in Formula (I). The present invention obtains a phosphazene compound using an M group having specific components. The composite metal laminates prepared by the epoxy resin composition comprising the phosphazene compound have low dielectric properties, good heat resistance and mechanical properties and is a low dielectric material also having great economic properties and being environmental friendly.
Abstract: Pt(IV) prodrugs include one or more conjugated cyclooxygenase inhibitor. Reduction of Pt(IV) to Pt(II) can result cisplatin and a cyclooxygenase inhibitor. For proof of concept, a Pt(IV) prodrug that can produce cisplatin and aspirin, Platin-A, was synthesized. Platin-A exhibited excellent anticancer and anti-inflammatory properties, which were better than the combination of free formulation of cisplatin and aspirin.
Abstract: Methods of preparing highly purified steviol glycosides, particularly Rebaudioside D, are described. The methods include purification from the extraction stage of the Stevia rebaudiana Bertoni plant, purification of steviol glycoside mixtures, Rebaudioside D and Rebaudioside A from a commercial Stevia extract, and purification of Rebaudioside D from remaining solutions obtained after isolation and purification of Rebaudioside A and a high purity mixture of steviol glycosides. The methods are useful for producing high purity Rebaudioside D, Rebaudioside A, and steviol glycoside mixtures. The high purity steviol glycosides are useful as non-caloric sweeteners in edible and chewable compositions such as any beverages, confectioneries, bakery products, cookies, and chewing gums.
Abstract: The present invention is the following Amphotericin B derivative: wherein each symbol is defined in description. The compound of the present invention has 16th position (X) is urea structure, cyclic structure, hydroxyalkyl or substituted monoalkylcarbamoyl. The compound of the present invention has antifungal activity.
Abstract: This invention provides methods for attaching a nucleic acid to a solid surface and for sequencing nucleic acid by detecting the identity of each nucleotide analogue after the nucleotide analogue is incorporated into a growing strand of DNA in a polymerase reaction. The invention also provides nucleotide analogues which comprise unique labels attached to the nucleotide analogue through a cleavable linker, and a cleavable chemical group to cap the —OH group at the 3?-position of the deoxyribose.
Type:
Application
Filed:
May 27, 2016
Publication date:
July 6, 2017
Inventors:
Jingyue Ju, Zengmin Li, John Robert Edwards, Yasuhiro Itagaki
Abstract: The present invention relates to compounds having cholane scaffolds of formula (I), said compounds for use in the treatment and/or prevention of FXR and TGR5/GPBAR1 mediated diseases.
Abstract: The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.
Abstract: The present invention pertains to the field of pharmaceutical chemistry, and relates to compounds having cyclopentanoperhydrophenanthrene skeletons and preparation methods therefore. The compounds have some physiological activity, and are useful as synthons/intermediates for further synthesizing some compounds having specific structures. These compounds and salts thereof are useful as lead compounds for synthesizing pharmaceuticals, pesticides and new materials. From this, further screen and preparation by chemical, biological and medical means offer new compounds that are more valuable and have important applications, achieving the object of inventing and creating new drugs.
Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of virus infections, particularly hepatitis C infections.
Type:
Application
Filed:
February 2, 2017
Publication date:
July 6, 2017
Inventors:
Caroline Aciro, Jean Yves Chiva, David Kenneth Dean, Adrian John Highton, Petr Jansa, Andrew John Keats, Linos Lazarides, Richard Mackman, Karine G. Poullennec, Adam James Schrier, Dustin Scott Siegel, Victoria Alexandra Steadman, Greg Watt
Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of virus infections, particularly hepatitis C infections.
Type:
Application
Filed:
March 21, 2017
Publication date:
July 6, 2017
Inventors:
Caroline Aciro, David Kenneth Dean, Neil Andrew Dunbar, Adrian John Highton, Petr Jansa, Kapil Kumar Karki, Andrew John Keats, Linos Lazarides, Richard L. Mackman, Simon N. Pettit, Karine G. Poullennec, Adam James Schrier, Dustin Siegel, Victoria Alexandra Steadman
Abstract: Cyclic tetrapeptide stereochemical isomers of CJ-15,208, pharmaceutical compositions from such cyclic tetrapeptides, and methods of using such pharmaceutical compositions. The cyclic tetrapeptide compounds and pharmaceutical compositions disclosed herein are potent analgesics active in several pain models with generally minimal tolerance and reduced likelihood to induce addiction relative to other known opiates.
Type:
Application
Filed:
July 13, 2015
Publication date:
July 6, 2017
Inventors:
Jane V. Aldrich, S P Sanjeewa Nilendra Senadheera
Abstract: A method for preparing AMG 416, or a pharmaceutically acceptable salt thereof, is provided. AMG 416 is a synthetic, eight amino-acid selective peptide agonist of the calcium sensing receptor. It is being developed as an intravenous treatment of secondary hyperparathyroidism (SHPT) in hemodialysis patients with chronic kidney disease—mineral and bone disorder (CKD-MBD).
Type:
Application
Filed:
April 3, 2015
Publication date:
July 6, 2017
Inventors:
Jeroen BEZEMER, Ying CHEN, Richard CROCKETT, Kevin CROSSLEY, Sheng CUI, Liang HUANG, Sian JONES, Asher LOWER, Krishnakumar RANGANATHAN
Abstract: There is described a material comprising tapes, ribbons, fibrils or fibres characterized in that each of the ribbons, fibrils or fibres have an antiparallel arrangement of peptides in a ?-sheet tape-like substructure.
Type:
Application
Filed:
March 16, 2017
Publication date:
July 6, 2017
Applicant:
University of Leeds
Inventors:
Neville Boden, Amalia Aggeli, Eileen Ingham, Jennifer Kirkham
Abstract: Compounds comprising peptides and peptidomimetics capable of binding the C3 protein and inhibiting complement activation are disclosed. These compounds display improved complement activation-inhibitory activity as compared with currently available compounds. Isolated nucleic acid molecules encoding the peptides are also disclosed.
Type:
Application
Filed:
October 22, 2014
Publication date:
July 6, 2017
Applicant:
THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
Abstract: Disclosed is a composition of a cyclic peptide compound having a water content of 3%-20%, represented by formula I is the structural formula of the cyclic peptide compound, and, also disclosed are a preparation method for same and uses thereof.
Type:
Application
Filed:
May 29, 2015
Publication date:
July 6, 2017
Inventors:
Shidong LIU, Xiusheng WANG, Xiaoming JI
Abstract: Disclosed herein are compounds having activity as cell penetrating peptides. In some examples, the compounds can comprise a cell penetrating peptide moiety and a cargo moiety. The cargo moiety can comprise one or more detectable moieties, one or more therapeutic moieties, one or more targeting moieties, or any combination thereof. In some examples, the cell penetrating peptide moiety is cyclic. In some examples, the cell penetrating peptide moiety and cargo moiety together are cyclic. In some examples, the cell penetrating peptide moiety is cyclic and the cargo moiety is appended to the cyclic cell penetrating peptide moiety structure. In some examples, the cargo moiety is cyclic and the cell penetrating peptide moiety is cyclic, and together they form a fused bicyclic system.
Abstract: The invention provides methods for drying dalbavancin. The method includes providing wet dalbavancin that includes dalbavancin, water, and a solvent. The wet dalbavancin is dried at at a temperature of about 30° C. or less, at a vacuum pressure of about 50 mbar or less, until the water level of the wet dalbavancin is less than about 20% (w/w). Water is then added to the dalbavancin and the resulting wet dalbavancin is dried at least once more at a temperature of about 30° C. or less, at a vacuum pressure of about 50 mbar or less, until the solvent level of the dalbavancin is less than about 3.0% (w/w).
Abstract: Disclosed are a protein and a gene each of which is a factor involved in latent infection with a herpesvirus. An antibody against the factor was detected in approximately 50% of patients suffering from mental disorders, whereas the antibody was hardly detected in healthy persons. Further, a mouse having SITH-1 introduced therein developed a mental disorder such as a manic-depressive illness or depression-like disorder. Based on these findings, it is possible to provide a method for objectively determining a mental disorder and an animal model of a mental disorder.
Type:
Application
Filed:
March 17, 2017
Publication date:
July 6, 2017
Applicants:
Virus Ikagaku Kenkyusho Inc., Japan Tobacco Inc.
Abstract: Provided are a recombinant polypeptide in which a small leucine-rich proteoglycan mimetic sequence is attached to a terminal of a mussel adhesive protein, a composition for wound healing including the same, a bioadhesive material, and a preparation method thereof. According to the present disclosure, the recombinant polypeptide in which the small leucine-rich proteoglycan mimetic sequence is attached to the terminal of the mussel adhesive protein has an excellent epidermal regeneration effect in which the wound site is uniformly restored by promoting rapid wound healing at the wound site when being applied to the wound site and inducing formation of collagens which are arranged and concentrated at the wound site, and thus can be usefully used as various drugs, cosmetics, and quasi-drugs.
Type:
Application
Filed:
December 29, 2016
Publication date:
July 6, 2017
Inventors:
Hyung Joon CHA, Bong Hyuk CHOI, Eun Young JEON
Abstract: A spider venom (SV) 82 polypeptide has an amino acid sequence of SEQ ID NO: 2. An SV82 polypeptide-encoding gene having a nucleotide sequence of SEQ ID NO: 1 which is optimized for E. coli codon. A recombinant vector includes the SV82 polypeptide-encoding gene, An E. coli is transformed with the recombinant vector. A method of producing SV82 polypeptide includes transforming a host cell with the recombinant vector. A cosmetic composition for reducing skin wrinkles and maintaining skin elasticity includes SV82 polypeptide as an active ingredient.
Type:
Application
Filed:
August 26, 2016
Publication date:
July 6, 2017
Inventors:
Sun Kyo LEE, Je Geun YOO, Seong Ran LEE, Han Bong RYU, Tae Won CHOI, Jong Nam CHOI, Tae Hyun KIM
Abstract: The present disclose relates to anti-inflammatory proteins/peptides, their uses, methods of preparation and methods of their detection. In particular, the invention relates to major royal jelly proteins modified by methyglyoxal and fragments thereof from a Leptospermum derived honey and royal jelly.
Abstract: Genetically encoded, photocleavable proteins are derived from a fluorescent protein. Upon illumination, the proteins photocleave and spontaneously dissociate into two or more fragments or release one end of an internal loop.
Type:
Application
Filed:
February 10, 2015
Publication date:
July 6, 2017
Applicant:
THE GOVERNORS OF THE UNIVERSITY OF ALBERTA
Abstract: A peptide (Peptide-1) based on the C-terminal of Equine CC10 has been discovered that can be used as a vaccine to protect horses from respiratory airway obstruction (RAO), Antibodies to Peptide-1 may also be administered for short-term passive immunotherapy to RAO-affected horses, and can be used to measure the level of CC10 protein in serum to identify potential RAO horses (horses with reduced CC10). Due to similarities between equine RAO and human asthma, this peptide or its antibodies may also be useful in treatment or prevention of human asthma.
Type:
Application
Filed:
January 13, 2017
Publication date:
July 6, 2017
Applicant:
Board of Supervisors of Louisiana State University and Agricultural and Mechanical College
Inventors:
Changaram S. Venugopal, Sudhirdas K. Prayaga
Abstract: In one aspect the present invention is directed to mutant NGAL proteins that have the ability to bind to siderophores, such as enterochelin, and to chelate and transport iron, and that are excreted in the urine. Such NGAL mutants, and complexes thereof with siderophores, can be used to clear excess iron from the body, for example in the treatment of iron overload. The NGAL mutants of the invention also have antibacterial activity and can be used in the treatment of bacterial infections, such as those of the urinary tract.
Abstract: The present invention is related to a virus, preferably an adenovirus, characterised in that the virus comprises: a lacking functional wildtype E1 region, and a transporter for the transport of YB-1 into the nucleus of a cell which is infected with the virus.