Chalcogen Or Nitrogen Bonded Directly At 1-, 2- Or 3-position Of The Diazole Ring By Nonionic Bonding Patents (Class 514/395)
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Publication number: 20140127273Abstract: Disclosure is provided for imidazole derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions comprising these compounds, devices comprising these compounds, and methods of using the same.Type: ApplicationFiled: January 8, 2014Publication date: May 8, 2014Applicant: North Carolina State UniversityInventors: Christian Melander, John Cavanagh, Robert W. Huigens, III, T. Eric Ballard, Justin J. Richards
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Publication number: 20140121103Abstract: The present invention relates to synergistic mixtures comprising at least one compound I and at least one active compound II as defined herein and to the use of these mixtures for combating phytopathogenic fungi, and to seeds coated with at least one such mixture. The invention also relates methods for combating harmful fungi using such mixtures.Type: ApplicationFiled: June 15, 2012Publication date: May 1, 2014Applicant: BASF SEInventors: Nadege Boudet, Wassilios Grammenos, Jochen Dietz, Egon Haden, Richard Riggs, Bernd Müller, Jan Klaas Lohmann, Jurith Montag, Ian Robert Craig
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Patent number: 8710082Abstract: The various embodiments relate to a compound comprising: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are each independently hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocyclyl, alkoxy, aryloxy, heteroaryloxy, alkoxycarbonyl, aryloxycarbonyl, heteroaryloxycarbonyl, alkylsulfonyl, arylsulfonyl, aminosulfonyl, alkylcarbonyl, arylcarbonyl, heteroarylcarbonyl, acyl, acylamino, amino, alkylamino, dialkylamino, arylamino, carboxylate (—CO2H), cyano, nitro, —CONH2, heteroarylamino, oxime, alkyloxime, aryloxime, amino-oxime or halogen when A, B, C, D, E, F, G, H, I, J, K, L, M, N, O, P, and Q are carbon, and X is O, NR (where R is hydrogen, alkyl, aryl or acyl), S, SO (sulfoxide), SO2 (sulfone), or C(R)2 (where R=H, alkyl, aryl, alkenyl, alkynyl, or acyl); or wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are each independently hydrogen or hydroxyl when A, B, C, D, E, F, G, H, I, J, K, L, M, N, O, P, and Q are each independently nitrogen, and compositions, combinationType: GrantFiled: February 4, 2012Date of Patent: April 29, 2014Assignee: Board of Trustees of Michigan State UniversityInventors: Christopher Waters, Karthik Sambanthamoorthy, Matthew Neiditch, Martin Semmelhack
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Publication number: 20140113891Abstract: Methods for treating cancer using compounds that inhibit human DNA ligases. Methods for using compounds that inhibit human DNA ligases to provide insights into the reaction mechanisms of human DNA ligases, for example to identify the human DNA ligase involved in different DNA repair pathways. Screening methods for compounds that inhibit human DNA ligases.Type: ApplicationFiled: April 17, 2013Publication date: April 24, 2014Inventors: Alan E. Tomkinson, Xi Chen, Barbara Dziegielewska, Alexander D. Mackerell, Shijun Zhong, Gerald M. Wilson
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Publication number: 20140100242Abstract: Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production.Type: ApplicationFiled: September 17, 2013Publication date: April 10, 2014Applicant: THE TRUSTEES OF PRINCETON UNIVERSITYInventors: Bonnie Bassler, Lee Swem
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Patent number: 8685983Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: November 30, 2011Date of Patent: April 1, 2014Assignee: Amgen Inc.Inventors: Tae-Seong Kim, David Bauer, Steven Bellon, Alessadro Boezio, Shon Booker, Deborah Choquette, Derin C. D'Amico, Noel D'Angelo, Celia Dominguez, Ingrid M. Fellows, Julie Germain, Russell Graceffa, Jean-Christophe Harmange, Satoko Hirai, Daniel La, Matthew Lee, Longbin Liu, Mark H. Norman, Michele Potashman, Philip Roveto, Aaron C. Siegmund, Ning Xi, Kevin Yang
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Publication number: 20140080828Abstract: This disclosure relates to antiviral compounds disclosed herein and uses related thereto. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising 2-((benzo[d]imidazol-2-yl)thio)-N-phenylpropanamide derivatives, N-phenyl-2-((1-phenyl-benzo[d]imidazol-2-yl)thio)propanamide derivatives, or 2-((benzo[d]imidazol-2-yl)thio)-N-(2-chloro-4-methylphenyl)propanamide derivatives. The derivatives may be substituted with one or more substituents. Typically, the pharmaceutical composition comprises a compound of Formula (I), or salt, prodrug, or ester thereof wherein X, Y, and R1 to R7 are described herein.Type: ApplicationFiled: March 28, 2012Publication date: March 20, 2014Applicants: CHILDREN'S HEATLHCARE OF ATLANTA, INC., EMORY UNIVERSITYInventors: Richard K. Plemper, James P. Snyder, Aiming Sun, John M. Ndungu, Jeong-Joong Yoon
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Publication number: 20140066466Abstract: Described herein are compositions that inhibit the production of TNF? downstream of CD40 activation. As such, also described are various methods of using compositions exhibiting this activity for the treatment or prevention of inflammatory diseases associated with TNF? production or CD40 activation.Type: ApplicationFiled: March 12, 2012Publication date: March 6, 2014Applicant: President and Fellows of Harvard CollegeInventor: Junying Yuan
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Publication number: 20140066454Abstract: The present disclosure relates to benzimidazole-benzamide derivatives, and the use thereof, e.g., to treat infections.Type: ApplicationFiled: February 22, 2012Publication date: March 6, 2014Applicants: INSTITUT NATIONAL DE LA RECHERCHE SCIENTIFIQUE, THE GENERAL HOSPITAL CORPORATIONInventors: Laurence Rahme, Francois Lepine, Melissa Starkey, Biliana Lesic-Arsic
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Patent number: 8664252Abstract: The present invention relates to a phosphodiesterase type III (PDE III) inhibitor and/or Ca2+-sensitizing agent or a pharmaceutically acceptable derivative thereof for the treatment of a patient suffering from hypertrophic cardiomyopathy (HCM). According to another aspect the present invention relates to the use of a PDE III inhibitor and/or Ca2+-sensitizing agent for the preparation of a medicament for the treatment of a patient suffering from HCM.Type: GrantFiled: November 23, 2009Date of Patent: March 4, 2014Assignee: Boehringer Ingelheim Vetmedica GmbHInventors: Juergen Daemmgen, Olaf Joens
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Patent number: 8658677Abstract: Compounds are provided according to formula I: where R, R?, R3, R4, R5, and R6 are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, Alzheimer's Disease, Down's syndrome, Parkinson's Disease, and others.Type: GrantFiled: July 6, 2012Date of Patent: February 25, 2014Assignees: Aria Neurosciences Inc., New York UniversityInventors: Bijan Almassian, Martin J. Sadowski, Xu Kevin Lin
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Publication number: 20140051700Abstract: Methods and compositions for agonizing a type-2 orexin receptor (OX2R) in a cell determined to be in need thereof, including the general method of (a) administering to a subject a cyclic guanidinyl OX2R agonist and (b) detecting a resultant enhanced wakefulness or increased resistance to diet-induced accumulation of body fat, or abbreviated recovery from general anesthesia or jet lag.Type: ApplicationFiled: August 20, 2012Publication date: February 20, 2014Inventor: Masashi Yanagisawa
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Publication number: 20140045909Abstract: MN-029 di-hydrochloride (MN-029.2HCl, Formula 2) is a potent vascular targeting agent. The present invention focuses on the synthesis and characterization of the di-hydrochloride salt MN-029 and the preparation of pharmaceutically acceptable formulations thereof. Methods are disclosed of using the compound and formulations thereof in the treatment of diseases that rely on the generation of neovasculature by angiogenesis for disease progression.Type: ApplicationFiled: October 14, 2013Publication date: February 13, 2014Applicant: MediciNova, Inc.Inventor: Kale RUBY
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Patent number: 8642278Abstract: The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non-small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.Type: GrantFiled: November 22, 2006Date of Patent: February 4, 2014Assignee: University of South FloridaInventors: Said M. Sebti, Srikumar Chellappan, Nicholas James Lawrence
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Publication number: 20140031403Abstract: The present invention provides forms of curcumin and the pharmaceutical compositions thereof. The forms of curcumin disclosed herein are curcumin polymorph Form III, curcumin-2-aminobenzimidazole co-crystal, and curcumin-L-lysine co-crystal. Further, the invention provides methods inhibiting cancer cells and HSV-1 using these curcumin novel solid forms.Type: ApplicationFiled: April 5, 2012Publication date: January 30, 2014Applicants: VAN ANDEL RESEARCH INSTITUTE, THE TRANSLATIONAL GENOMICS RESEARCH INSTITUTEInventors: Stephen T. Gately, Steven J. Triezenberg, Tong Wang
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Publication number: 20140005221Abstract: The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below.Type: ApplicationFiled: January 30, 2012Publication date: January 2, 2014Applicant: SATO PHARMACEUTICAL CO., LTD.Inventors: Keita Nagai, Koh Nagasawa, Hirobumi Takahashi, Motoaki Baba, Shinichi Fujioka, Eri Kondoh, Kenichi Tanaka, Yoshiki Itoh
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Publication number: 20140005193Abstract: The present invention is directed to benzoimidazole compounds of the formula: and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.Type: ApplicationFiled: September 3, 2013Publication date: January 2, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: Frances Meredith Hocutt, BARRY EASTMAN LEONARD, JR., HILLARY M. PELTIER, VICTOR K. PHUONG, MICHAEL H. RABINOWITZ, MARK D. ROSEN, KYLE T. TARANTINO, HARIHARAN VENKATESAN, LUCY XIUMIN ZHAO
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Patent number: 8618148Abstract: The present invention relates to a method for the prophylaxis of vascular headaches which do not originate from hypertension, especially migraine, the method comprising administration of telmisartan to a subject in need of such a treatment. The present invention relates also to a method for the prophylaxis of vascular headaches, comprising the co-administration of telmisartan in combination with other drugs suitable for migraine prophylaxis and/or acute treatment of migraine.Type: GrantFiled: June 16, 2006Date of Patent: December 31, 2013Assignee: Boehringer Ingelheim International GmbHInventor: Giora Davidai
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Publication number: 20130345261Abstract: The various embodiments relate to a compound comprising: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are each independently hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocyclyl, alkoxy, aryloxy, heteroaryloxy, alkoxycarbonyl, aryloxycarbonyl, heteroaryloxycarbonyl, alkylsulfonyl, arylsulfonyl, aminosulfonyl, alkylcarbonyl, arylcarbonyl, heteroarylcarbonyl, acyl, acylamino, amino, alkylamino, dialkylamino, arylamino, carboxylate (—CO2H), cyano, nitro, —CONH2, heteroarylamino, oxime, alkyloxime, aryloxime, amino-oxime or halogen when A, B, C, D, E, F, G, H, I, J, K, L, M, N, O, P, and Q are carbon, and X is O, NR (where R is hydrogen, alkyl, aryl or acyl), S, SO (sulfoxide), SO2 (sulfone), or C(R)2 (where R?H, alkyl, aryl, alkenyl, alkynyl, or acyl); or wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are each independently hydrogen or hydroxyl when A, B, C, D, E, F, G, H, I, J, K, L, M, N, O, P, and Q are each independently nitrogen, and compositions, combinationType: ApplicationFiled: February 4, 2012Publication date: December 26, 2013Inventors: Christopher Waters, Karthik Sambanthamoorthy, Matthew Neiditch, Martin Semmelhack
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Patent number: 8614229Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: GrantFiled: August 27, 2008Date of Patent: December 24, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Gopinadhan N. Anilkumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih
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Patent number: 8614213Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing (CRF1) receptor antagonists.Type: GrantFiled: August 5, 2009Date of Patent: December 24, 2013Assignee: Novartis AGInventors: David Beattie, Andrew James Culshaw, Lisa Rooney, Emily Stanley
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Publication number: 20130338092Abstract: This invention relates to high-throughput, semi-automated methods for identifying compounds that are effective in targeting leukemia stem cells, as well as compounds identified by those methods and uses thereof for treating leukemia.Type: ApplicationFiled: August 16, 2013Publication date: December 19, 2013Inventors: Kimberly Hartwell, Malcolm A.S. Moore, David T. Scadden, Stuart L. Schreiber, Todd R. Golub, Benito Munoz, Benjamin L. Ebert, Andrew M. Stern, Peter G. Miller, D. Gary Gilliland, Anne Van Dyk Carpenter, David J. Logan, Joseph Negri, Nicola Tolliday, Alykhan Shamji, Siddhartha Mukherjee, Alison Stewart
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Patent number: 8598078Abstract: Compounds of Formula I wherein the substituents are as defined in Claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: GrantFiled: August 21, 2008Date of Patent: December 3, 2013Assignee: Syngenta Crop Protection, LLCInventors: Olivier Loiseleur, Roger Graham Hall, André Denis Stoller, Gerald Wayne Craig, André Jeanguenat, Andrew Edmunds
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Publication number: 20130303571Abstract: The present invention relates to compounds of general formula I in which A, L, M, Q2, Q3, Q4, R1, R5, Ra, Rb, Rc, W, X, Y, Z1, Z2, Z3 are defined in the description, the salts thereof, particularly the physiologically acceptable salts thereof. The compounds are of potential utility in the treatment and/or prevention of inflammatory diseases and associated conditions, in particular, in the treatment and/or prevention of pain. The invention also relates to the use of such compounds as medicaments, to pharmaceutical compositions containing them, and to their preparation.Type: ApplicationFiled: July 15, 2013Publication date: November 14, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Roland PFAU, Kirsten ARNDT, Henri DOODS, Klaus KLINDER, Raimund KUELZER, Dimitrijs LUBRIKS, Juergen MACK, Benjamin PELCMAN, Henning PRIEPKE, Robert ROENN, Dirk STENKAMP, Edgars SUNA
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Publication number: 20130295143Abstract: Electrospinning of crystalline particles comprising active pharmaceutical ingredients (API) from suspensions yields fibrous compositions comprising the API. The morphology and size of the crystalline particles may be preserved. The particles may be predominantly retained by fibers and distributed throughout the fibrous mesh. Tablet forms of the APIs prepared from the fibrous compositions demonstrate higher dissolution rates than tablets prepared from compacted powders of the APIs.Type: ApplicationFiled: March 15, 2013Publication date: November 7, 2013Inventors: Bernhardt Levy Trout, Blair Kathryn Brettmann, Allan Stuart Myerson
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Publication number: 20130289057Abstract: The invention relates to N-arylaminomethylenebenzothiophenones of General Formula (I) for use as a drug for the treatment of cardiovascular diseases: wherein E is S, O, or CH2, D is CH or NH, and Ar is a phenyl or naphtyl moiety substituted by an electron-withdrawing group, an unsubstituted heteroaryl residue, or a heteroaryl residue substituted by alkyl or an electron-withdrawing group.Type: ApplicationFiled: January 12, 2012Publication date: October 31, 2013Applicants: FORSCHUNGSVERBUND BERLIN E.V., MAX-DELBRUCK-CENTRUM FUR MOLEKULARE MEDIZINInventors: Enno Klussmann, Walter Rosenthal, Jelena Milic, Martin W. Bergmann
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Publication number: 20130281392Abstract: The invention relates to oral, topical or injectable compositions for combating liver fluke parasites in mammals, comprising at least one benzimidazole derivative active agent. The invention also provides for an improved method for eradicating and controlling liver fluke parasite infections and infestations in a mammal comprising administering the compositions of the invention to the mammal in need thereof.Type: ApplicationFiled: April 18, 2013Publication date: October 24, 2013Applicant: MERIAL LIMITEDInventor: Charles Q. Meng
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Publication number: 20130281496Abstract: The novel active compound combinations of a carboxamide of the general formula (I) (group 1) in which R, G, R1 and A have the meanings given in the description and the active compound groups (2) to (23) listed in the description have very good fungicidal properties.Type: ApplicationFiled: June 12, 2013Publication date: October 24, 2013Inventors: Ulrike WACHENDORFF-NEUMANN, Peter DAHMEN, Ralf DUNKEL
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Publication number: 20130245079Abstract: The use of polyhexamethylene guanidine hydrochloride as preservative for preventing and controlling citrus sour rot and its application are disclosed by the present invention. The citrus preservative calculated by 100% total mass fraction comprises 0.05%-0.5% polyhexamethylene guanidine hydrochloride, 0.05%-0.2% of one or more selected from the group consisting of a mixture of several of the following: 0.05%-0.2% imidazole fungicidebactericide, benzimidazole fungicidebactericide, pyrimethanil, fludioxonil and [or] azoxystrobin, and 0.02%-0.15% polyethenoxy ether emulsion or quaternary ammonium salt emulsion, and the rest is water. The citrus preservative can significantly inhibit the decay of citrus fruit such as Citrus microcarpa during storage, especially the incidence of sour rot. So the commercial value of citrus is obviously increased.Type: ApplicationFiled: November 15, 2010Publication date: September 19, 2013Inventors: Xuewu Duan, Yueming Jiang, Linyan Feng, Fuwang Wu
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Publication number: 20130245019Abstract: Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R?, R?, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.Type: ApplicationFiled: April 30, 2013Publication date: September 19, 2013Applicant: CONGENIA SRLInventors: Daniele Fancelli, Mario Varasi, Simon Plyte, Marco Ballarini, Anna Cappa, Giacomo Carenzi, Saverio Minucci, Gilles Pain, Manuela Villa
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Publication number: 20130245070Abstract: The present invention relates to a method for enhancing arginase activity in a damaged or injured cell. In other aspects, the invention provides a method for treating a disorder that can be treated by enhancing arginase activity in a human in need thereof, the method comprising administering to the human an effective amount of a compound that enhances arginase activity. Such disorders include ischemia, hypoxia, neurodegenerative disease or condition, stroke or trauma of the nervous system. In yet another aspect, the invention provides methods for promoting regeneration of a neural cell in a human in need thereof.Type: ApplicationFiled: March 9, 2012Publication date: September 19, 2013Applicant: THE RESEARCH FOUNDATION OF THE CITY UNIVERSITY OF NEW YORKInventors: Rajiv R. Ratan, Marie T. Filbin
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Patent number: 8518940Abstract: The present invention embraces compounds selected for interacting with the Fingers-Palm pocket of telomerase and use thereof for modulating the activity of telomerase and preventing or treating diseases or conditions associated with telomerase.Type: GrantFiled: February 8, 2010Date of Patent: August 27, 2013Assignee: The Wistar InstituteInventor: Emmanuel Skordalakes
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Publication number: 20130203599Abstract: The present invention provides the agricultural chemical-spreading agent composition, containing: (A) a polysaccharide in an amount of 5 to 30% by weight; (B) a polyoxyalkylene sorbitan fatty acid ester in an amount of 5 to 40% by weight; and (C) at least one nonionic surfactant selected from polyoxyalkylene alkyl ethers, sorbitan fatty acid esters, and silicone surfactants in an amount of 5 to 40% by weight, wherein the component (A) has a viscosity of not less than 5000 mPa·s in the form of a 5% by weight aqueous solution at 25° C., and a weight ratio of contents of the component (A) to the sum of components (B) and (C), (A)/[(B)+(C)], is 10/90 to 40/60.Type: ApplicationFiled: September 1, 2011Publication date: August 8, 2013Applicant: KAO CORPORATIONInventors: Masaki Inoue, Masatoshi Kamei
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Publication number: 20130172335Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: February 22, 2013Publication date: July 4, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130156816Abstract: The invention features compositions, methods, and kits for the administration of an oxidatively transformed carotenoid, or a fractionated component thereof, for use in aquaculture.Type: ApplicationFiled: February 18, 2011Publication date: June 20, 2013Applicant: Chemaphor Inc.Inventors: Larry Arthur Stobbs, James Gary Nickerson, Clayton Paul Dick
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Patent number: 8466186Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), to pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, M, W, R1, R2, R3, R4, R6, R2, R7, R8, R9, Ra, Rb have meanings given in the description.Type: GrantFiled: December 8, 2011Date of Patent: June 18, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Henning Priepke, Raimund Kuelzer, Juergen Mack, Roland Pfau, Dirk Stenkamp, Benjamin Pelcman, Robert Roenn, Dimitrijs Lubriks, Edgars Suna
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Publication number: 20130136782Abstract: Compounds described herein inhibit biofilm formation or disperse pre-formed biofilms of Gram-negative bacteria. Biofilm-inhibitory compounds can be encapsulated or contained in a polymer matrix for controlled release. Coatings, films, multilayer films, hydrogels, microspheres and nanospheres as well as pharmaceutical compositions and disinfecting compositions containing biofilm-inhibitory compounds are also provided. Methods for inhibiting formation of biofilms or dispersing already formed biofilms are provided. Methods for treating infections of gram-negative bacteria which form biofilms, particularly those of Pseudomonas and more particularly P. aeruginosa.Type: ApplicationFiled: November 5, 2012Publication date: May 30, 2013Inventors: Helen BLACKWELL, Reto Frei, Anthony Breitbach, David M. Lynn, Adam H. Broderick
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Patent number: 8445473Abstract: The invention relates to heteroaryl-substituted bicyclic mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.Type: GrantFiled: April 13, 2009Date of Patent: May 21, 2013Assignee: The Regents of the University of MichiganInventors: Shaomeng Wang, Haiying Sun, Zaneta Nikolovska-Coleska
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Publication number: 20130096129Abstract: The present invention provides compounds of Formulae (A), (B), (C), and (D), pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof, pharmaceutical compositions thereof, and kits thereof. The present invention further provides methods of using the compounds to treat or prevent neurological disorders. In one aspect, the methods include administering to a subject in need of treatment for a neurological disorder a therapeutically effective amount of DAC-001, DAC-002, DAC-003, DAC-009, or DAC-012, or a compound of Formula (A), (B), (C), or (D).Type: ApplicationFiled: July 20, 2012Publication date: April 18, 2013Inventors: Li-Huei Tsai, Ling Pan, Stephen J. Haggarty, Debasis Patnaik
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Publication number: 20130079376Abstract: Compounds are provided according to formula I: where R, R?, R3, R4, R5, and R6 are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, Alzheimer' s Disease, Down's syndrome, Parkinson's Disease, and others.Type: ApplicationFiled: July 6, 2012Publication date: March 28, 2013Inventors: Bijan Almassian, Martin J. Sadowski, Xu Kevin Lin
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Publication number: 20130064895Abstract: The inventions provided herein relate to amphiphilic peptides and particles comprising the amphiphilic peptides. Such amphiphilic peptides and particles described herein can be used as a delivery system, e.g., for therapeutic or diagnostic purposes, or as cell penetration vehicles or cell transfection agents.Type: ApplicationFiled: August 23, 2012Publication date: March 14, 2013Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGEInventor: Christian Dittrich
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Patent number: 8394803Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, that inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.Type: GrantFiled: November 6, 2006Date of Patent: March 12, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Paul Charifson, David Deininger, Joseph Drumm, Anne-Laure Grillot, Arnaud LeTiran, Yusheng Liao, Emanuele Perola, Steven Ronkin, Dean Stamos, Tiansheng Wang
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Patent number: 8377983Abstract: The present invention relates to compounds and methods from the treatment of cancer. The invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising compounds that inhibit Aurora kinase, and methods for the treatment of cancer using the compounds of the presentation invention or pharmaceutical compositions comprising compounds of the present invention.Type: GrantFiled: February 10, 2010Date of Patent: February 19, 2013Assignee: TransTech Pharma, Inc.Inventors: Adnan M. M. Mjalli, Brian S. Grella, Govindan Subramanian, Murty N. Arimilli, Ramesh Gopalaswamy, Robert C. Andrews, Stephen Davis, Xiaochuan Guo, Jeff Zhu
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Patent number: 8362051Abstract: Wallboard and facing paper that provides increased mold resistance at lower biocide loadings. The biocide is: (a) an n-alkyl isothiazolinone such as octylisothiazolinone (OIT), a monohalo and dihalo substituted n-alkylisothiazolinone such as chloromethylisothiazolinone (CMIT) or dichlorooctylisothiazolinone (DCOIT), 3-iodo-2-propynyl-butylcarbamate (IPBC), chlorothalonil, methylene-bis-thiocyanate, or mixtures of two or more thereof; or (b) carbendazim and a second biocide selected from 3-iodo-2-propynyl-butylcarbamate (IPBC), diiodomethyltolylsulfone (DIMTS), sodium pyrithione, octylisothiazolinone (OIT), dichlorooctylisothiazolinone (DCOIT), and chlorothalonil.Type: GrantFiled: January 18, 2008Date of Patent: January 29, 2013Assignee: Rohm and Haas CompanyInventors: Sheila M. Tinetti, Paul Foley, Li Wang, Michael V. Enzien, Sanjay B. Bishnoi
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Publication number: 20130023525Abstract: The present invention relates to compounds which inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.Type: ApplicationFiled: April 24, 2012Publication date: January 24, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Paul S. Charifson, David D. Deininger, Anne-Laure Grillot, Yusheng Liao, Steven Ronkin, Dean Stamos, Emanuele Perola, Tiansheng Wang, Arnaud Le Tiran, Joseph Drumm
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Publication number: 20120322820Abstract: Methods of treating one or more growth deregulated cells are disclosed. An effective amount of a pharmaceutical composition including a proton pump inhibitor is administered thereby treating a growth deregulated cell outside of the gastric lumen of a subject.Type: ApplicationFiled: August 28, 2012Publication date: December 20, 2012Applicant: NEXMED HOLDINGS, INC.Inventor: Bassam DAMAJ
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Patent number: 8329914Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.Type: GrantFiled: October 22, 2009Date of Patent: December 11, 2012Assignees: Merck Sharp & Dohme Corp, Metabasas Therapeutics, Inc.Inventors: Jianming Bao, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, Dariusz Wodka, Qun Dang, De Michael Chung, Tony S. Gibson, Hongjian Jiang, Daniel K. Cashion
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Publication number: 20120309736Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.Type: ApplicationFiled: February 21, 2011Publication date: December 6, 2012Inventors: Jinlong Jiang, Andrew J. Kassick, Ahmet Kekec, Iyassu K. Sebhat
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Publication number: 20120309738Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), to pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, M, W, R1, R2, R3, R4, R6, R2, R7, R8, R9, Ra, Rb have meanings given in the description.Type: ApplicationFiled: December 8, 2011Publication date: December 6, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning Priepke, Raimund Kuelzer, Juergen Mack, Roland Pfau, Dirk Stenkamp, Benjamin Pelcman, Robert Roenn, Dimitrijs Lubriks, Edgars Suna
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Publication number: 20120283260Abstract: The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists.Type: ApplicationFiled: July 24, 2012Publication date: November 8, 2012Applicants: ASTELLAS PHARMA INC., ALCON RESEARCH, LTD.Inventors: Keith D. Combrink, Suchismita Mohapatra, Mark R. Hellberg, Najam A. Sharif, Ganesh Prasanna, Iok-Hou Pang, Bryon Severns, Hwang-Hsing Chen, Abdelmoula Namil