Plural Hetero Atoms In The Polycyclo Ring System Patents (Class 514/338)
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Patent number: 8975283Abstract: Disclosed herein is a method for the production of disulfide compounds of the formula I PAC-SA—SB—R*??(I) wherein PAC-SA is a residue of a pharmaceutically active drug a metabolite thereof or a pharmaceutically acceptable salt thereof that is covalently bonded via the sulfur atom, SA of a reduced sulfhydryl, sulfinyl, sulfonyl or sulfonamide group to the sulfur atom SB of an oxidized sulfhydryl group of a pharmacologically acceptable sulfhydryl compound in the absence of an acid. Preferably the pharmaceutically active drug is a proton pump inhibitor and the sulfhydryl compound is N-acetyl cysteine. The disulfide compounds according to the invention can be prepared either in vitro or in vivo and are stable in the acidic conditions of the stomach. Pharmaceutical compositions containing compounds of the formula I and a method for the treatment or prophylaxis of gastrointestinal disorders using compounds of the formula I are also described.Type: GrantFiled: January 4, 2013Date of Patent: March 10, 2015Assignee: JON Pty LimitedInventor: John Allen Hackett
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Patent number: 8975416Abstract: Disclosed are compounds of formula (I), which are of use in the treatment of bacterial diseases and infections, to compositions containing those compounds and to methods of treating bacterial diseases and infections using the compounds. In particular, the compounds are useful for the treatment of infection with, and diseases caused by, Clostridium difficile.Type: GrantFiled: December 1, 2009Date of Patent: March 10, 2015Assignee: Summit Corporation PLCInventors: Paul James Davis, Olivier De Moor, Colin Richard Dorgan, Peter David Johnson, Alan Geoffrey Roach, Richard Storer, Richard John Vickers, Francis Xavier Wilson, Graham Michael Wynne
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Patent number: 8975286Abstract: The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: GrantFiled: August 16, 2010Date of Patent: March 10, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Vadim Y. Dudkin, Mark E. Fraley, Cheng Wang, Robert M. Garbaccio, Douglas C. Beshore, Scott K. Kuduk, Jason W. Skudlarek
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Publication number: 20150065504Abstract: Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).Type: ApplicationFiled: August 19, 2014Publication date: March 5, 2015Inventors: Guangyi Wang, Leonid Beigelman, Anh Truong, Carmela Napolitano, Daniele Andreotti, Haiying He, Karin Ann Stein
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Publication number: 20150065445Abstract: The present invention relates to viral polymerase inhibitors of formula (I) or salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections.Type: ApplicationFiled: April 11, 2013Publication date: March 5, 2015Inventors: Tyrone Pieter Jeynes, Alistair George Draffan, Michael Harding, Silas Bond, Rosliana Halim
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Publication number: 20150065529Abstract: A fungicidal composition containing a fungicidally effective amount of a compound of Formula I-V and at least one fungicide selected from the group consisting of epoxiconazole, prothioconazole, azoxystrobin, pyraclostrobin, penthiopyrad, isopyrazam, bixafen, boscalid, prochloraz, and chlorothalonil provides synergistic control of selected fungi.Type: ApplicationFiled: November 11, 2014Publication date: March 5, 2015Inventors: W. John Owen, JR., Chenglin Yao
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Publication number: 20150065482Abstract: The invention relates to compounds of Formula (0): wherein Q, A1-A8, R4 and R5 and each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.Type: ApplicationFiled: August 22, 2014Publication date: March 5, 2015Applicant: GENENTECH, INC.Inventors: Nicole Blaquiere, Georgette Castanedo, Jianwen A. Feng, Baihua Hu, Steven Staben, Po-wai Yuen, Guosheng Wu, Jason Burch
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Publication number: 20150065497Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: August 5, 2014Publication date: March 5, 2015Inventors: Sara S. Hadida Ruah, Mark T. Miller, Brian Bear, Jason McCartney, Peter D.J. Grootenhuis
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Publication number: 20150065500Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: September 11, 2014Publication date: March 5, 2015Applicant: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida-Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou, Frederick van Goor
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Publication number: 20150065483Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl 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.Type: ApplicationFiled: November 7, 2014Publication date: March 5, 2015Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan
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Publication number: 20150065477Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.Type: ApplicationFiled: March 14, 2013Publication date: March 5, 2015Inventors: Andreas Kling, Katja Jantos, Helmut Mack, Achim Möller, Wilfried Hornberger, Gisela Backfisch, Yanbin Lao, Marjoleen Nijsen
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Patent number: 8969341Abstract: The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.Type: GrantFiled: November 28, 2012Date of Patent: March 3, 2015Assignee: Novartis AGInventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
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Publication number: 20150057314Abstract: The present disclosure relates to pharmaceutical compositions comprising omeprazole, lansoprazole and sodium bicarbonate.Type: ApplicationFiled: September 18, 2014Publication date: February 26, 2015Inventor: Jeffrey O. Phillips
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Publication number: 20150057307Abstract: Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided.Type: ApplicationFiled: June 23, 2014Publication date: February 26, 2015Inventors: Edward Roberts, Hugh Rosen, Steven Brown, Miguel A. Guerrero, Xuemei Peng, Ramulu Poddutoori
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Publication number: 20150056257Abstract: The present invention relates to a method for preparing an emulsifiable granule comprising the steps of a) emulsifying water with a solution of a pesticide in a water-insoluble solvent, b) contacting the emulsion resulting from step a) and a solid dispersant containing a water-soluble polycarboxylate and a water-soluble anionic surfactant, and c) extruding the paste resulting from step b). The invention further relates to emulsifiable granules containing a water-insoluble solvent, a pesticide, which is dissolved in the water-insoluble solvent, a water-soluble polycarboxylate, and a water-soluble anionic surfactant.Type: ApplicationFiled: February 26, 2013Publication date: February 26, 2015Inventors: Claude Taranta, Thomas Bork, Jochen Schreieck, Helmut Mueller, Nadine Riediger, Clark D. Klein, Rebecca Willis, Tatjana Sikuljak, Simon Nord
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Publication number: 20150057272Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: August 1, 2014Publication date: February 26, 2015Inventors: Chi B. Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
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Patent number: 8962851Abstract: The present invention discloses one pot process for enantioselective synthesis of single enantiomers of substituted sulphoxides 2-(2-pyridinylmethylsulphinyl)-1H-benzimidazoles or said compounds in an enantiomerically enriched form.Type: GrantFiled: December 26, 2012Date of Patent: February 24, 2015Assignee: Cadila Healthcare LimitedInventors: Shriprakash Dhar Dwivedi, Ashok Prasad, Daya Ram Pal
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Patent number: 8962524Abstract: The present invention relates to a mixture comprising [(3S,4R,4aR,6S,12R,12aS,12bS)-3-(cyclopropanecarbonyloxy)-6,12-dihydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,2,3,4,4a,5,6,6a,12a,12b-decahydro-11H,12H-benzo[f]pyrano[4,3-b]chromen-4-yl]methyl cyclopropanecarboxylate and a fungicidal compound II in synergistic effective amounts, to the use of this mixture for controlling pests and for improving the plant health and to plant propagation material comprising this mixture.Type: GrantFiled: May 27, 2011Date of Patent: February 24, 2015Assignee: BASF SEInventors: Matthias Pohlman, Markus Gewehr, Egon Haden, Juergen Langewald
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Patent number: 8962688Abstract: The present invention relates to combined use of (a) a specific prostaglandin (PG) compound and (b) a H+,K+-ATPase inhibitor for the treatment of gastrointestinal disorders.Type: GrantFiled: April 11, 2006Date of Patent: February 24, 2015Assignee: Sucampo AGInventor: Ryuji Ueno
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Patent number: 8962574Abstract: A method for preventing stroke in a patient suffering from atrial fibrillation, wherein the patient has at least one risk factor for major bleeding events, the method comprising administering to the patient 110 mg b.i.d. of dabigatran etexilate, optionally in the form of a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 10, 2009Date of Patent: February 24, 2015Assignee: Boehringer Ingelheim International GmbHInventor: Paul Anthony Reilly
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Patent number: 8962016Abstract: The present invention relates to extended release dosage forms of metoprolol or salts thereof comprising a water insoluble and non-swellable inert core and one or more pharmaceutically acceptable excipients. The invention also relates to processes for the preparation of an inert core and extended release dosage forms.Type: GrantFiled: November 25, 2010Date of Patent: February 24, 2015Assignee: Wockhardt Ltd.Inventors: Prashant Manohar Mandaogade, Venkatesh Madhavacharya Joshi, Saurabh Srivastava, Vinayak Dinkar Kadam, Girish Kumar Jain
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Patent number: 8962595Abstract: Compositions containing a small molecule therapeutic and an alkyl N,N-disubstituted amino acetate are disclosed. Inclusion of the alkyl N,N-disubstituted amino acetate enhances the pharmacokinetic properties of the small molecule therapeutic.Type: GrantFiled: May 4, 2011Date of Patent: February 24, 2015Assignee: Nexmed Holdings, Inc.Inventors: Bassam B. Damaj, Richard Martin
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Publication number: 20150051183Abstract: The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain.Type: ApplicationFiled: March 15, 2013Publication date: February 19, 2015Inventors: Daniel Obrecht, Philipp Ermert, Said Oumouch, Arnaud Piettre, Jean-François Gosalbes, Marc Thommen
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Publication number: 20150050239Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: ApplicationFiled: July 19, 2013Publication date: February 19, 2015Applicants: Calitor Sciences, LLC, Sunshine Lake Pharma Co., Ltd.Inventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
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Publication number: 20150051203Abstract: A compound of structural formula (I) or (II): as HSP90 inhibitors that possess significantly improved bioavailability over comparative compounds, which are suitable for the treatment of hyperproliferative diseases such as cancer, infections, immune disorders, inflammation, and CNS related disorders.Type: ApplicationFiled: March 27, 2013Publication date: February 19, 2015Inventors: Dinesh Chimmanamada, Zachary Demko, Weiwen Ying
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Publication number: 20150051208Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R3 and X1 through X6 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.Type: ApplicationFiled: August 11, 2014Publication date: February 19, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Harald ENGELHARDT, Laetitia MARTIN, Christian SMETHURST
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Patent number: 8957215Abstract: The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted benzothiazole derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents.Type: GrantFiled: April 23, 2012Date of Patent: February 17, 2015Assignee: Navidea Biopharmaceuticals, Inc.Inventors: Ylva Gravenfors, Catrin Jonasson, Jonas Malmstrom, Gunnar Nordvall, David Pyring, Can Slivo, Daniel Sohn, Peter Strom, David Wensbo
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Publication number: 20150045394Abstract: The present invention relates to novel carboxamide compounds and their use as a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity and to a method for the therapeutic and/or prophylactic treatment by administering an effective amount of at least one of these carboxamide compounds. The carboxamide compounds are compounds of the general formula I in which W—R2 is selected from and R1, R2, R3a, R3b, Y1, Y2, Y3, Y4, X, Q, m, k, Rw and Rw* have the meanings mentioned in the claims, the tautomers thereof and the pharmaceutically suitable salts thereof.Type: ApplicationFiled: October 23, 2014Publication date: February 12, 2015Inventors: Andreas Kling, Helmut Mack, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
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Publication number: 20150045347Abstract: Compounds having the following formula: (I) wherein: A is an optionally substituted triazole, or a stereoisomer or a pharmaceutically-acceptable salt thereof, are useful as kinase modulators, including IRAK-4 modulation.Type: ApplicationFiled: January 11, 2013Publication date: February 12, 2015Inventors: Dharmpal S. Dodd, Christopher P. Mussari, Rajeev S. Bhide, Satheesh Kesavan Nair, Venkatram Reddy Paidi, Sreekantha Ratna Kumar, Abhisek Banerjee, Ramesh Sistla, William J. Pitts, John Hynes
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Publication number: 20150045327Abstract: The present invention discloses compounds according to Formula I: wherein R1 is as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment cystic fibrosis by administering a compound of the invention.Type: ApplicationFiled: August 5, 2014Publication date: February 12, 2015Inventors: Steven Emiel VAN DER PLAS, Hans KELGTERMANS, Sébastien Jean Jacques Cédric DROPSIT MONTOVER, Sébastien Laurent Xavier MARTINA, Martin James Inglis ANDREWS
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Publication number: 20150045355Abstract: Provided are certain fused tricyclic compounds and salts thereof, compositions thereof, and methods of use therefor.Type: ApplicationFiled: December 31, 2011Publication date: February 12, 2015Inventors: Changyou Zhou, Shaohui Wang, Guoliang Zhang
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Patent number: 8952037Abstract: Heteroaryloxycarbocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.Type: GrantFiled: May 11, 2011Date of Patent: February 10, 2015Assignee: Amgen Inc.Inventors: Jennifer R. Allen, Michael J. Frohn, Paul E. Harrington, Essa Hu, Alexander J. Pickrell, Robert M. Rzasa, Kelvin K. C. Sham
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Patent number: 8952005Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: GrantFiled: October 8, 2013Date of Patent: February 10, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Mark E. Layton, Michael J. Kelly, III
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Publication number: 20150038536Abstract: The present disclosure relates to the field of tyrosine kinase enzyme inhibition, in particular anaplastic lymphoma kinase (ALK) inhibition using novel small molecules. Provided are compounds capable to modulate ALK activity, compositions that comprise the compounds, and methods of using the compounds for the treatment or prevention of diseases or conditions that are characterized by ALK activity or expression.Type: ApplicationFiled: June 18, 2014Publication date: February 5, 2015Inventor: Vlad Edward Gregor
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Publication number: 20150038488Abstract: The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I wherein X1, X2, X3, R2, R3, R4, R5, and Y are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.Type: ApplicationFiled: July 31, 2014Publication date: February 5, 2015Inventors: Kevin S. Currie, Zhimin Du, Julie Farand, Juan A. Guerrero, Ashley A. Katana, Darryl Kato, Scott E. Lazerwith, Jiayao Li, John O. Link, Nicholas Mai, Gregory Notte, Hyung-Jung Pyun, Michael Sangi, Aaron C. Schmitt, Adam J. Schrier, Kirk L. Stevens, Chandrasekar Venkataramani, William J. Watkins, Zheng-Yu Yang, Jeff Zablocki, Sheila Zipfel
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Publication number: 20150038437Abstract: The present description relates to compounds and forms and pharmaceutical compositions thereof and methods for use thereof to treat or ameliorate bacterial infections caused by wild-type and multi-drug resistant Gram-negative and Gram-positive pathogens.Type: ApplicationFiled: August 29, 2012Publication date: February 5, 2015Applicant: PTC THERAPEUTICS, INC.Inventors: Arthur Branstrom, Vara Prasad Venkata Nagendra Josyula, Michael Andrew Arnold, Aleksey I. Gerasyuto, Gary Karp, Jiashi Wang, John David Baird, Guangming Chen, Olya Ginzburg, Jana Narasimhan, Srinivasa Peddi, Hongyan Qi, Sean Wesley Smith, Matthew G. Woll, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang
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Publication number: 20150037423Abstract: The present invention provides an orally-disintegrating solid preparation such as a tablet produced by tabletting fine granules showing controlled release of a pharmaceutically active ingredient and an additive, and the like, and the orally-disintegrating solid preparation containing fine granules coated with a coating layer containing a polymer affording a casting film having an elongation at break of about 100-about 700%. With the preparation, breakage of fine granules during tabletting can be suppressed in the production of an orally-disintegrating solid preparation containing fine granules showing controlled release of a pharmaceutically active ingredient.Type: ApplicationFiled: October 21, 2014Publication date: February 5, 2015Inventors: Takashi KURASAWA, Yasuko WATANABE, Yoshihiro OMACHI
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Patent number: 8946264Abstract: The present invention relates to a novel pyridine derivative or a pharmacologically acceptable ester thereof, or a pharmacologically acceptable salt of the derivative or ester, which has an excellent hypoglycemic effect or treats and/or prevents the onset of a disorder of carbohydrate or lipid metabolism or a disease mediated by peroxisome proliferator-activated receptor (PPAR) ?. A compound represented by the general formula (I): [wherein R represents a pyridyl group substituted with 1 to 3 group(s) independently selected from Substituent Group A, and Substituent Group A represents a halogen atom, a C1-C6 alkyl group and a C1-C6 alkoxy group] or a pharmacologically acceptable ester thereof, or a pharmacologically acceptable salt of the compound or ester.Type: GrantFiled: October 20, 2012Date of Patent: February 3, 2015Assignee: Daiichi Sankyo Company, LimitedInventors: Tsuyoshi Shinozuka, Tomoharu Tsukada, Kunihiko Fujii, Makoto Mori
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Patent number: 8945626Abstract: A process for the production of a composition comprising a water-insoluble paracetamol or NSAID which comprises the steps of: a) providing a mixture comprising: i) a water-insoluble paracetamol or NSAID, ii) a water soluble carrier, and iii) a solvent for each of the paracetamol or NSAID and the carrier, and b) spray-drying the mixture to remove the or each solvent and obtain a substantially solvent-free nano-dispersion of the paracetamol or NSAID in the carrier.Type: GrantFiled: July 13, 2007Date of Patent: February 3, 2015Inventors: Andrew James Elphick, John Staniforth, Dong Wang, David John Duncalf, Steven Paul Rannard, James Long, Alison Jayne Foster
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Publication number: 20150031703Abstract: [Problem] The present invention aims to elucidate a polynucleotide as a novel responsible gene for cancer and aims to thus provide a method for detecting the polynucleotide and a polypeptide encoded by the polynucleotide and a detection kit, a probe set, and a primer set for the detection. The present invention also aims to provide a pharmaceutical composition for treating cancer. [Means for Solution] The method detects a fusion gene composed of a portion of an FGFR3 gene and a portion of a TACC3 gene or a fusion protein encoded by the fusion gene. The primer set, the probe set, or the detection kit comprises a sense primer and a probe set designed from the portion encoding FGFR3 and an antisense primer and a probe set designed from the portion encoding TACC3. Since an inhibitor of the polypeptide exhibits antitumor effect, a pharmaceutical composition for treating cancer which is positive for either the fusion gene or the polypeptide is provided.Type: ApplicationFiled: March 7, 2013Publication date: January 29, 2015Applicant: Astellas Pharma Inc.Inventors: Atsushi Suzuki, Makoto Asaumi, Kazuhisa Tsunoyama, Kouichi Nishimura, Akifumi Morinaka, Tomohiro Yamauchi, Masayasu Yoshino, Hiroaki Yoshizaki
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Publication number: 20150031725Abstract: Provided herein, inter alia, are compositions and methods useful for treating hyperproliferative diseases, including cancer and non-malignant hyperproliferative diseases.Type: ApplicationFiled: October 2, 2014Publication date: January 29, 2015Inventors: Richard J. Pietras, Michael E. Jung, Diana C. Marquez-Garban, Gang Deng
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Publication number: 20150031535Abstract: The present invention relates to a liquid concentrate formulation comprising a pyripyropene pesticide of the formula I as defined below and an alkoxylated aliphatic alcohol as an adjuvant. Moreover, the invention relates to the use of the formulations for the treatment of plants and seed and to corresponding methods.Type: ApplicationFiled: March 11, 2013Publication date: January 29, 2015Applicant: BASF SEInventors: Wen Xu, Matthias Pohlman
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Patent number: 8940900Abstract: Compounds of the present disclosure are 2,2,2-tri-substituted acetamide derivatives of formula (I), its polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts and formulations thereof, useful as Glucokinase activator. Processes of their preparation are also described in the disclosure. The disclosure also describes method to characterize partial glucokinase activators.Type: GrantFiled: February 25, 2008Date of Patent: January 27, 2015Assignee: Advinus Therapeutics Private LimitedInventors: Kasim A. Mookhtiar, Debnath Bhuniya, Bhavesh Dave, Gobind S. Kapkoti, Sujay Basu, Anita Chugh, Siddhartha De, Venkata P. Palle
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Patent number: 8940730Abstract: Briefly described, embodiments of this disclosure include compounds, pharmaceutical compositions, methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of inhibiting HCV replication in a host, methods of inhibiting the binding of NS4B polypeptide to the 3?UTR of HCV negative strand RNA in a host, methods of treating liver fibrosis in a host, and the like.Type: GrantFiled: March 16, 2010Date of Patent: January 27, 2015Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Jeffrey S. Glenn, Wenjin Yang, Ingrid C. Choong
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Patent number: 8940769Abstract: Disclosed are biaryl benzoimidazole derivatives. They have an inhibitory effect on calcium influx in HEK cells, thereby showing a powerful antagonistic effect on a vanilloid receptor, and further have an analgesic effect, thereby being useful for preventing or treating pain, acute pain, chronic pain, neuropathic pain, postoperative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurological illness, neurodermatitis, stroke, bladder hypersensitivity, irritable bowel syndrome, a respiratory disorder such as cough, asthma, and chronic obstructive pulmonary disease, burning, psoriasis, itching, vomiting, irritation of the skin, eyes, and mucous membranes, gastric-duodenal ulcers, inflammatory intestinal diseases, and inflammatory diseases.Type: GrantFiled: April 5, 2013Date of Patent: January 27, 2015Assignee: Daewoong Pharmaceutical Co., Ltd.Inventors: Ji Duck Kim, Hong-Chul Yoon, In Woo Kim, Hyae Jung Hyun
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Patent number: 8940773Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.Type: GrantFiled: October 24, 2013Date of Patent: January 27, 2015Assignee: Akebia Therapeutics, Inc.Inventors: Richard Masaru Kawamoto, Shengde Wu, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Namal C. Warshakoon
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Publication number: 20150025115Abstract: A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent.Type: ApplicationFiled: October 7, 2014Publication date: January 22, 2015Inventors: Akira FUJISHIMA, Isao AOKI
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Publication number: 20150025114Abstract: In one aspect, the invention relates to substituted 1H-benzo[d][1,2,3]triazol-1-ol analgoues, derivatives thereof, and related compound; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders, e.g. various tumors and cancers, associated with ?-catenin/Tcf protein-protein interaction dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: February 10, 2013Publication date: January 22, 2015Applicant: UNIVERSITY OF UTAH RESEARCH FOUNDATIONInventors: Haitao Ji, Binxun Yu, Min Zhang, Wenxing Guo
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Publication number: 20150025046Abstract: The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: X is —O—, —N(R), —C(R8)(R9) or —C(O)—; and Y is —O—, —N(R), —C(R8)(R9) or —C(O)— and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ACS, secondary prevention of myocardial infarction or stroke, or PAD.Type: ApplicationFiled: February 27, 2013Publication date: January 22, 2015Inventors: Mihir Mandal, Timothy A. Blizzard, Helen Chen, Harry Chobanian, Yan Guo, Barbara Pio, Zhicai Wu, Tesfaye Biftu, William J. Greenlee, Johnny Zhaoning Zhu
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Publication number: 20150023916Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.Type: ApplicationFiled: February 14, 2013Publication date: January 22, 2015Applicant: SIGA TECHNOLOGIES INC.Inventors: Dongcheng Dai, James R. Burgeson, Sean M. Amberg, Dennis E. Hruby