Nitrogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/352)
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Patent number: 8987307Abstract: This invention relates to novel 3-aminopyridines of the formula wherein B1, B2 and R1 to R6 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.Type: GrantFiled: February 28, 2012Date of Patent: March 24, 2015Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Henrietta Dehmlow, Shawn David Erickson, Prabha Saba Karnachi, Kyungjin Kim, Rainer E. Martin, Patrizio Mattei, Ulrike Obst Sander, Sherrie Lynn Pietranico-Cole, Hans Richter, Christoph Ullmer
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Publication number: 20150080436Abstract: A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at about 12 hours and the use of the composition to treat various neurological diseases, including multiple sclerosis. A method of selecting individuals based on responsiveness to a treatment, including, for example, identifying individuals who responded to treatment with a sustained release fampridine composition.Type: ApplicationFiled: November 3, 2014Publication date: March 19, 2015Inventors: Andrew R. Blight, Ron Cohen
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Publication number: 20150079116Abstract: NK cell licensing predisposes patients to chronic inflammatory disease. Methods and kits to diagnose and treat chronic inflammatory disease based on genetic haplotype and cytokine profile are described herein.Type: ApplicationFiled: April 11, 2013Publication date: March 19, 2015Inventors: Jonathan Braun, Lin Lin
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Publication number: 20150072006Abstract: The invention relates to drug preparations with controlled active ingredient released in the form of microtablets which contain, as active ingredient, flupirtin or one of its physiologically compatible salts, and to processes for their production.Type: ApplicationFiled: March 1, 2013Publication date: March 12, 2015Inventors: Katrin Moschner, Torsten Hoffmann, Mario Weingart, Annegret Hildebrand-Cyrener
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Publication number: 20150065517Abstract: The present invention provides organic compounds of the following structure; A-L1-B-C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.Type: ApplicationFiled: November 10, 2014Publication date: March 5, 2015Applicant: NOVARTIS AGInventors: Michael H. SERRANO-WU, Young-shin KWAK, Wenming LIU
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Publication number: 20150064234Abstract: It has been discovered that pharmacological inhibition of K+ channels (using the FDA-approved broad-spectrum K+ channel antagonist 4-AP) positively benefitted smn mutant phenotypes, a result that is consistent with the defective excitability of motor circuits by their interneuron or sensory neuron inputs being a critical consequence of SMN depletion. Based on these observations, certain embodiments of the invention are directed to methods of treatment of SMA by administering therapeutically effective amounts of one or more potassium channel antagonists, including 4-aminopyridine, 4-(dimethylamino)pyridine, 4-(methylamino)pyridine, and 4-(aminomethyl)pyridine. Other embodiments are directed to new pharmaceutical formulations comprising two or more potassium channel antagonists.Type: ApplicationFiled: March 26, 2013Publication date: March 5, 2015Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventor: Brian D. Mccabe
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Publication number: 20150065561Abstract: The present invention is based, in part, on our studies of molecular pathways that include the deubiquitinase CYLD. Accordingly, the present invention features, inter alia, nucleic acid constructs that express CYLD or a biologically active variant thereof (e.g., a variant including the catalytic domain), nucleic acids that inhibit the expression of a negative regulator of CYLD (e.g., PDE4B or LNK2), nucleic acids that modulate the expression of downstream CYLD targets (e.g., Akt, by inhibiting or promoting the expression of the downstream target), compositions including one or more of these types of constructs (e.g., pharmaceutical compositions), kits including one or more of the compositions described herein and instructions for use, screening methods to identify therapeutic agents {e.g., anti-inflammatory agents) that upregulate CYLD, downregulate a negative regulatory of CYLD, or modulate (e.g., inhibit) a downstream CYLD target (e.g.Type: ApplicationFiled: April 9, 2013Publication date: March 5, 2015Applicant: Georgia State University Research Foundation, Inc.Inventor: Jian-Dong Li
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Patent number: 8969574Abstract: The present invention relates to a substantially a solid form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Compound 1, Solvate Form A and Compound 1, HCl Salt Form A), processes for making such forms, pharmaceutical compositions thereof, and methods of treatment therewith.Type: GrantFiled: April 10, 2014Date of Patent: March 3, 2015Assignee: Vertex Pharmaceuticals IncorporatedInventors: Ali Keshavarz-Shokri, Beili Zhang, Mariusz Krawiec
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Publication number: 20150056213Abstract: Disclosed are selective histone deactylase inhibitors (HDACi) that having Formula (I). Methods of making and using these inhibitors for the treatment of cancer, in particular melanoma are also disclosed.Type: ApplicationFiled: March 7, 2013Publication date: February 26, 2015Inventors: Eduardo M. Sotomayor, Joel Bergman, Alan Kozikowski, Karrune Veeraprasert Woan, Alejandro V. Villagra
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Publication number: 20150057279Abstract: This invention relates to certain heteroaryl compounds which may be used as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of parasitic infections such as helminth infections and the treatment of parasitosis caused by such infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.Type: ApplicationFiled: March 27, 2013Publication date: February 26, 2015Inventors: Michael Berger, Marko Eck, Christopher Kern
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Patent number: 8962847Abstract: The invention relates to novel multicomponent crystals, to the production thereof, and to the use thereof for treating pain conditions, in particular of unclear genesis, by means of a simultaneous effect on pains which are caused by muscle tension or degenerative joint diseases as well as on pains that are caused by inflammatory processes. The multicomponent crystals according to the invention contain ([2-amino-6-(4-fluoro-benzylamino)-pyridin-3-yl]-carbamic acid ethyl ester (flupirtine) and an arylpropionic acid as the sole active ingredient combination and can be produced by dissolving flupirtine and the arylpropionic acid in an inert organic solvent and subsequently crystallizing the multicomponent crystal.Type: GrantFiled: December 20, 2011Date of Patent: February 24, 2015Assignee: TEVA GmbHInventors: Christoph Martin Hoock, Asal Qadan, Bernd Terhaag
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Publication number: 20150051245Abstract: The invention relates to protein binding inhibitor compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating cell proliferative disorders, especially cancer.Type: ApplicationFiled: November 13, 2012Publication date: February 19, 2015Inventors: William G. Cance, Ravindra K. Pandey, Elena V. Kurenova, Manivannan Ethirajan
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Publication number: 20150051254Abstract: This invention relates to the treatment of varying degrees of cognitive impairment associated with, for example, aging, Alzheimer's disease, schizophrenia with low dose administration of a PDE4 inhibitor, specifically roflumilast.Type: ApplicationFiled: August 15, 2014Publication date: February 19, 2015Inventors: Jos Prickaerts, Marlies van Duinen, Anke Sambeth, Arjan Blokland
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Publication number: 20150051177Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.Type: ApplicationFiled: October 31, 2014Publication date: February 19, 2015Inventor: Darren Orton
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Publication number: 20150051199Abstract: The invention provides compounds that are useful in the treatment of hepatitis C virus (HCV) infections.Type: ApplicationFiled: October 31, 2012Publication date: February 19, 2015Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Andrew James Woodhead, Christopher Charles Frederick Hamlett, Gilbert Ebai Besong, Gianni Chessari, Maria Grazia Carr, Alessia Millemaggi, David Norton, Susanne Maria Saalau-Bethell, Hendrika Maria Gerarda Willems, Neil Thomas Thompson, Steven Douglas Hiscock
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Patent number: 8957063Abstract: Compounds which modulate the CB2 receptor are disclosed. The compounds are useful for treating CB2 receptor-mediated diseases such as pain.Type: GrantFiled: February 19, 2009Date of Patent: February 17, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, Monika Ermann, Innocent Mushi
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Publication number: 20150045364Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: October 23, 2014Publication date: February 12, 2015Applicant: NOVARTIS AGInventors: Urs BAETTIG, Kamlesh BALA, Emma BUDD, Lee EDWARDS, Catherine HOWSHAM, Glyn Alan HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
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Patent number: 8951999Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.Type: GrantFiled: October 20, 2010Date of Patent: February 10, 2015Assignee: Orexo ABInventors: Henning Priepke, Henri Doods, Raimund Kuelzer, Roland Pfau, Dirk Stenkamp, Robert Roenn, Benjamin Pelcman
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Patent number: 8952001Abstract: The invention relates to amino-heteroaryl derivatives having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.Type: GrantFiled: December 20, 2010Date of Patent: February 10, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Simon James Anthony Grove, Angus John Morrison, Craig Jamieson, Ronald Palin, John Kinnaird Ferguson Maclean
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Publication number: 20150038531Abstract: An aminopyridine derivative of Formula 1 and a method of preventing or treating cancer using the same. Formula 1: In Formula 1: X1 and X2 are each independently selected from the group consisting of carbon and nitrogen; R1 to R5 are each independently selected from the group consisting of a hydrogen, a straight, a branched, or cyclo alkyl of C1-C4, a halogen, and a hydroxyl; and R6 is a hydrogen or an alkyl of C1-C6.Type: ApplicationFiled: October 20, 2014Publication date: February 5, 2015Inventors: Sunghoon Kim, Hee Sook Lee, Young Sun Oh, Dae Gyu Kim
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Patent number: 8946437Abstract: The present invention provides a novel compound having an excellent antitumor effect, stability and metabolic stability. The compound of the present invention is represented by the following general formula (1) wherein R1 represents a halogen atom, an aryl group, an aryloxy group or a lower alkyl group optionally substituted with one or more halogen atoms; R2 represents hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; and; m represents an integer of 1 to 3; provided that when m represents 2 or 3, R1s are the same or different.Type: GrantFiled: October 3, 2011Date of Patent: February 3, 2015Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Takashi Nakagawa, Makoto Sakamoto, Kazuya Yamaguchi, Yuki Terauchi, Masamichi Shirakura, Yasuo Harada, Yutaka Kojima, Takumi Sumida
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Patent number: 8946269Abstract: Provided herein are crystalline forms of a maleate salt of betrixaban, compositions and methods of preparation or use thereof.Type: GrantFiled: August 31, 2011Date of Patent: February 3, 2015Assignee: Portola Pharmaceuticals, Inc.Inventors: Vincent R. Capodanno, Liam Corcoran, Michael McNevin, Itzia Zoraida Arroyo, Robert M. Wenslow, Richard G. Ball, Eric L. Margelefsky, Timothy K. Maher, Anjali Pandey
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Publication number: 20150030549Abstract: Topical compositions are disclosed that are useful for delivering a therapeutic level of an NSAID to a target within a subject having a local inflammatory disorder. A composition of the present invention comprises a Drug and a solvent system, wherein the solvent system comprises at least two solvent alcohols and wherein the solvent system is present in an amount sufficient to solubilize the Drug, the solvent system is a low alkanol system, and the composition is a single phase composition. Exemplary solvent systems are those for which one of the at least two solvent alcohols is polyethylene glycol, glycerin, butylene glycol, dipropylene glycol, propylene glycol, ethanol, isopropanol, or a derivative thereof. Optionally the local inflammatory disorder is pseudofolliculitis barbae, dermatitis, psoriasis, wounds, or sunburn.Type: ApplicationFiled: August 11, 2014Publication date: January 29, 2015Inventors: Monique Renata Green, Kenton Fedde
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Publication number: 20150031663Abstract: The invention provides antimicrobial compounds and compositions, and methods of using them. The compounds and compositions include, for example, a compound of any one of Formulas I-X. The invention further provides methods of preparing the compounds, and useful intermediates for their preparation. The compounds can possess highly specific and selective activity, such as antibacterial activity and/or enzymatic inhibitory activity. Accordingly, the compounds and compositions can be used to treat bacterial infections, or to inhibit or kill bacteria, either in vitro or in vivo.Type: ApplicationFiled: October 13, 2014Publication date: January 29, 2015Applicant: UNIVERSITY OF NOTRE DAME DU LACInventors: Shahriar Mobashery, Dusan Hesek, Mayland Chang
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Publication number: 20150025077Abstract: This invention relates to geranylgeranyl acetone (GGA) derivatives and the use of GGA, its isomers, and GGA derivatives in methods for inhibiting neural death, increasing neural activity, increasing axon growth and cell viability, and increasing the survival rate of subjects administered the GGA or GGA derivatives.Type: ApplicationFiled: February 27, 2013Publication date: January 22, 2015Applicant: COYOTE PHARMACEUTICALS, INC.Inventors: Hiroaki Serizawa, Ankush B. Argade, Akash Datwani, Natalie Spencer, Yonghua Pan, Florian Ermini
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Patent number: 8937090Abstract: The invention provides a parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent that has a function such as parakeratosis inhibition, pore shrinkage, or rough skin-inhibition/abatement, poses no safety problems such as sensory irritation, and is very safe, and further provides an external composition for skin to which a compound having the above-mentioned function has been added. The parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent comprises one or more compounds selected from the group consisting of ?-alanine derivatives and salts thereof. The external composition for skin comprises the one or more compounds selected from the group consisting of ?-alanine derivatives and salts thereof as the above-mentioned parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent.Type: GrantFiled: April 28, 2006Date of Patent: January 20, 2015Assignee: Shiseido Company, Ltd.Inventors: Mikiko Kaminuma, Masaru Suetsugu, Toshii Iida, Shinji Inomata
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Publication number: 20150018293Abstract: Compositions and methods for the treatment and control of various conditions in an animal which comprises administering to said animal an effective amount of a immediate release composition of about 0.5% to 50% wt/wt of active ingredient together with excipients to a total of about 100%, wherein said composition dissolves in a relatively short period of time, e.g., 75 seconds or less, 5 seconds or less, or 3 seconds or less, upon administration to said animal.Type: ApplicationFiled: May 12, 2014Publication date: January 15, 2015Applicant: NEWMARKET PHARMACEUTICALS LLCInventors: David ROCK, Mark RIDALL
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Patent number: 8933106Abstract: The invention relates to 2-(4-Substituted phenylamino) polysubstituted pyridine compounds as inhibitors of non-nucleoside HIV reverse transcriptase, preparation methods and uses thereof. Specifically, the invention relates to compounds of formula I or the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the description. The compounds of formula I of the invention are a type of anti-HIV active compounds having new backbone structure.Type: GrantFiled: September 28, 2009Date of Patent: January 13, 2015Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. ChinaInventors: Lan Xie, Xingtao Tian, Kuo-Hsiung Lee, Shibo Jiang, Hong Lu
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Publication number: 20150011574Abstract: The present invention provides a compound which enhances the production of erythropoietin. The present invention provides a compound represented by the formula (1) wherein R1: an aromatic hydrocarbon ring group or an aromatic heterocyclic group; R2: a hydrogen atom, an alkyl group, or a heterocycloalkyl group; R3: a hydrogen atom or an alkyl group; A: a hydrogen atom or a hydroxy group; L: —NHCO— or —OCH2—; and X: a nitrogen atom or ?CH—.Type: ApplicationFiled: September 24, 2014Publication date: January 8, 2015Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Tatsuya NISHI, Naoki TANAKA, Ryoko KITAZAWA, Riki GOTO, Takashi ISHIYAMA
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Publication number: 20150010484Abstract: A method for anti-skin aging, especially for anti-skin photo-aging in a subject is provided. The method comprising administering to the subject an effective amount of an active component selected from the group consisting of a caffeamide derivative of formula (I), a pharmaceutically acceptable salt of the caffeamide derivative, and a combination thereof: wherein A is H or an alkyl; B is —[CH2]m—; m is an integer ranging from 0 to 10; R1 is H, an optionally substituted phenyl, an optionally substituted pyridyl, —OH, or —OCH3; or, N, A, B, and R1 together form an optionally substituted pyrrolyl or piperidyl.Type: ApplicationFiled: October 8, 2013Publication date: January 8, 2015Applicant: CHINA MEDICAL UNIVERSITYInventors: Hsiu-Mei CHIANG, Yueh-Hsiung KUO, Kuo-Ching WEN
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Publication number: 20150011551Abstract: Described herein are compounds that modulate the activity of TNAP. In some embodiments, the compounds described herein inhibit TNAP. In certain embodiments, the compounds described herein are useful in the treatment of conditions associated with hyper-mineralization.Type: ApplicationFiled: February 21, 2013Publication date: January 8, 2015Applicant: Sanford- Burnham Medical Reseach InstituteInventors: Anthony B. Pinkerton, Russell Dahl, Nicholas D.P. Cosford, Jose Luis Millan
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Publication number: 20150005349Abstract: The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula I or II or a stereoisomer, tautomer, racemic, metabolite, pro- or pre-drug, salt, hydrate, or solvate thereof, wherein Ar, Cy, R1, R3, p and n have the meaning defined in the claims. In particular, the present invention relates to more specifically AGC kinases inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease.Type: ApplicationFiled: July 1, 2014Publication date: January 1, 2015Inventors: Robert Owen Messing, Michael A. Pleiss, Jon D. Levine
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Publication number: 20140378513Abstract: The present disclosure provides methods to detect pests in liquid culture systems for the growth of microalgae. The disclosure further provides methods to treat and control pests in a liquid system and for methods to increase yields of microalgae grown in a liquid culture systems. Methods are provided for the growth, monitoring, treatment and harvesting of microalgae from liquid culture systems.Type: ApplicationFiled: October 12, 2012Publication date: December 25, 2014Inventors: Robert C McBride, Craig A Behnke, Kyle M Botsch, Nicole A Heaps, Christopher Del Meenach
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Patent number: 8916593Abstract: The invention relates to compounds of Formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.Type: GrantFiled: May 4, 2011Date of Patent: December 23, 2014Assignee: Pfizer Inc.Inventors: Mark Edward Bunnage, Andrew Simon Cook, Jingrong Jean Cui, Kevin Nell Dack, Judith Gail Deal, Danlin Gu, Mingying He, Patrick Stephen Johnson, Ted William Johnson, Phuong Thi Quy Le, Cynthia Louise Palmer, Hong Shen
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Publication number: 20140369932Abstract: The present disclosure provides novel compounds, including compounds that bind to potassium channels, methods for their manufacture, and methods for their use, including their use to diagnose and/or assess traumatic brain injury and use to treat dymeylinating diseases, and/or in vivo imaging of the central nervous system, and to diagnose and/or assess the progression of MS or other diseases.Type: ApplicationFiled: July 11, 2014Publication date: December 18, 2014Inventors: Pedro Brugarolas, Brian POPKO, Daniel APPELBAUM, Chin-Tu CHEN
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Publication number: 20140371268Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases, gastrointestinal diseases and respiratory diseases.Type: ApplicationFiled: August 31, 2012Publication date: December 18, 2014Applicant: AMAKEM NVInventors: Jo Alen, Sandro Boland, Arnaud Pierre Jean Bourin, Olivier Defert, Dirk Leysen
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Publication number: 20140350034Abstract: The invention relates to compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.Type: ApplicationFiled: January 25, 2013Publication date: November 27, 2014Applicant: NOVARTIS AGInventors: Trixi Brandl, Stefanie Flohr, Christian Markert, Kenji Namoto, Bernard Pirard, Martin Renatus
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Publication number: 20140350055Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.Type: ApplicationFiled: August 31, 2012Publication date: November 27, 2014Applicant: Amakem NVInventors: Jo Alen, Sandro Boland, Arnaud Pierre Jean Bourin, Olivier Defert, Dirk Leysen
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Publication number: 20140349969Abstract: The present invention relates to new therapies to treat pain and related diseases, as well as pharmaceutical compounds for use in said therapies.Type: ApplicationFiled: May 8, 2014Publication date: November 27, 2014Inventors: Josef PENNINGER, Graham Gregory NEELY, Shane MCMANUS, Henrik NILSSON
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Publication number: 20140343000Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 and C-3 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: These compounds are useful for the treatment of HIV and AIDS.Type: ApplicationFiled: July 24, 2014Publication date: November 20, 2014Inventors: Alicia Regueiro-Ren, Zheng Liu, Jacob Swidorski, Ny Sin, Brian Lee Venables, Sing-Yuen Sit, Yan Chen, Jie Chen, Nicholas A. Meanwell
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Publication number: 20140343107Abstract: The invention provides retinoic acid receptor (RAR) selective agonists and formulations thereof for the treatment of disease or for inducing a medically beneficial effect.Type: ApplicationFiled: May 23, 2014Publication date: November 20, 2014Applicant: QuRetino Therapeutics, Inc.Inventor: Ferenc Makra
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Patent number: 8889694Abstract: N-Alkoxyamides of 4-aminopicolinic acids and 6-amino-4-pyrimidinecarboxylates are selective herbicides for corn, canola and sugar beet.Type: GrantFiled: August 8, 2013Date of Patent: November 18, 2014Assignee: Dow AgroSciences, LLC.Inventors: Joseph D. Eckelbarger, Paul R. Schmitzer, Carla N. Yerkes, Timothy A. Boebel, Norbert M. Satchivi, Gregory T. Whiteker
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Patent number: 8889719Abstract: The invention provides novel compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation.Type: GrantFiled: March 5, 2013Date of Patent: November 18, 2014Assignee: Merck Patent GmbHInventors: Andreas Goutopoulos, Henry Yu, Benny C. Askew, Jr., Lesley Liu-Bujalski
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Patent number: 8889876Abstract: The present invention discloses a group of histone deacetylase inhibitors and use thereof. The histone deacetylase inhibitors are useful in the treatment of malignant tumors and the diseases associated with differentiation and proliferation.Type: GrantFiled: June 9, 2009Date of Patent: November 18, 2014Assignee: Jiangsu Hengyi Pharmaceutical Co., Ltd.Inventors: Jianqi Li, Juan Feng, Wangping Cai
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Publication number: 20140336194Abstract: The present invention provides the use of a neutral endopeptidase inhibitor, in the manufacture of a medicament for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The invention also relates to the use of a compound of Formula I: wherein R1, R2, R3, R5, X, A3, B1, s and n are defined herein, for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of contrast-induced nephropathy.Type: ApplicationFiled: July 28, 2014Publication date: November 13, 2014Applicant: NOVARTIS AGInventor: Shi Yin FOO
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Publication number: 20140336440Abstract: Compounds and compositions having activity as inhibitors of Rho-associated proteinkinases (ROCKs), and methods of making and using the subject compounds are disclosed.Type: ApplicationFiled: January 24, 2013Publication date: November 13, 2014Inventors: Ernst Schonbrunn, Rongshi Li, Said M. Sebti
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Publication number: 20140329674Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.Type: ApplicationFiled: May 3, 2014Publication date: November 6, 2014Applicant: INSCENT, INC.Inventors: Daniel F. Woods, Spiros Dimitratos, Robin W. Justice
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Publication number: 20140329854Abstract: Provided are novel heterocyclic sirtuin binding agents, e.g., N-aryl substituted pyridine dicarboxamides, which are useful as sirtuin modulators. Also provided are methods of using the pyridine dicarboxamide compounds for treating sirtuin mediated disorders and conditions, such as diabetes, cancers, and obesity and diseases related to aging.Type: ApplicationFiled: December 12, 2012Publication date: November 6, 2014Applicant: SMB InnovationInventors: Bjarne Due Larsen, Soren Andersen, Marianne Spanget Larsen
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Patent number: 8877935Abstract: A process for the preparation of Dalfampridine (1), 4-aminopyridine, starting from 4-pyridinecarbonitrile using a one-pot procedure. Said process is carried out with no need for isolating intermediates and is particularly advantageous as far as environment, yields, productivity and purity of the resulting product are concerned, both in the reaction mixture and in the isolated crystal.Type: GrantFiled: June 7, 2011Date of Patent: November 4, 2014Assignee: Procos S.p.A.Inventors: Fabio Garavaglia, Alessandro Barozza, Jacopo Roletto, Paolo Paissoni
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Patent number: 8877741Abstract: The invention relates to new pyrrolidine derivatives of the formula to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: GrantFiled: January 22, 2014Date of Patent: November 4, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Martin Fleck, Niklas Heine, Bernd Nosse, Gerald Juergen Roth