1,2,3-triazoles (including Hydrogenated) Patents (Class 548/255)
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Patent number: 8846913Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3—R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: GrantFiled: April 24, 2013Date of Patent: September 30, 2014Assignee: Theravance Biopharma R&D IP, LLCInventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Cameron Smith
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Publication number: 20140271527Abstract: The present disclosure provides polymer conjugates comprising a polymer and an agent, the agent linked to the polymer via a linking group containing a cleavable moiety.Type: ApplicationFiled: November 1, 2012Publication date: September 18, 2014Applicant: Serina Therapeutics, Inc.Inventors: Randall Moreadith, Kunsang Yoon, Zhihao Fang, Rebecca Weimer, Bekir Dizman, Tacey Viegas, Michael David Bentley
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Publication number: 20140274689Abstract: Provided herein are new N-,C-disubstituted azoles and derivatives thereof that exhibit nematicidal activity and are useful, for example, in methods for the control of unwanted nematodes.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Monsanto Technology LLCInventors: Urszula J. Slomczynska, William P. Haakenson, JR.
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Publication number: 20140275025Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid(benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ralf ANDERSKEWITZ, Florian BINDER, Matthias GRAUERT, Marc GRUNDL, Peter Wilhelm HAEBEL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS, Viktor VINTONYAK
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Publication number: 20140275555Abstract: Articles and methods comprising persistent carbenes are provided, as well as related compositions. In some embodiments, a persistent carbene may be associated with a portion of a substrate (e.g., at least a portion of a surface on the substrate). In certain embodiments, the association of persistent carbene with the substrate may be used to affect certain properties of substrate (e.g., surface chemistry, stability). In some cases, a persistent carbene may be functionalized after association with a portion of a substrate. In some embodiments, a persistent carbene and at least one secondary compound may be associated with a portion of a substrate. Articles and methods of the present invention may be useful for applications involving electronics, sensing, microfabrication, nanotechnology, biomimetic, and drug delivery, amongst others.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: Massachusetts Institute of TechnologyInventors: Jeremiah A. Johnson, Aleksandr V. Zhukhovitskiy
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Publication number: 20140256700Abstract: The present invention is directed to carbazole compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.Type: ApplicationFiled: February 26, 2014Publication date: September 11, 2014Inventors: Michael A. Poss, David R. Tortolani, Dharmpal S. Dodd, Christopher P. Mussari, John S. Tokarski, Ashvinikumar V. Gavai, Yufen Zhao, George V. Delucca, Daniel O'Malley, Derek J. Norris, Patrice Gill, Claude A. Quesnelle, Wen-Ching Han
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Publication number: 20140255696Abstract: Fluorescent silica nanoparticles with aggregation induced emission characteristics as well as methods for attaching biotin thereto for tumor cell targeting and long-term cell tracking. Additionally, dendrimers decorated with AIR fluorogens.Type: ApplicationFiled: March 20, 2014Publication date: September 11, 2014Applicant: THE HONG KONG UNIVERSITY OF SCIENCE AND TECHNOLOGYInventors: Benzhong TANG, Wing Yip LAM, Min LI, Mathieu ARSENEAULT
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Publication number: 20140243257Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B?, X, Y, R1, R1?, R2, R2?, R3, R3?, R5, R5?, R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: May 8, 2014Publication date: August 28, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: James A. Henderson, John Maxwell, Louis Vaillancourt, Mark Morris, Ronald Grey, JR., Simon Giroux, Laval Chan Chun Kong, Sanjoy Kumar Das, Bingcan Liu, Carl Poisson, Caroline Cadilhac, Monica Bubenik, T. Jagadeeswar Reddy, Guy Falardeau, Constantin Yannopoulos, Jian Wang, Oswy Z. Pereira, Youssef L. Bennani, Albert C. Pierce, Govinda Rao Bhisetti, Kevin M. Cottrell, Valerie Marone
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Patent number: 8809333Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.Type: GrantFiled: March 27, 2012Date of Patent: August 19, 2014Assignee: Pfizer Inc.Inventors: Matthew Frank Brown, Jinshan Michael Chen, Michael Joseph Melnick, Justin Ian Montgomery, Usa Reilly
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Publication number: 20140228358Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.Type: ApplicationFiled: September 21, 2012Publication date: August 14, 2014Inventors: Jason Brubaker, Joshua T. Close, Joon Jung, Michelle Martinez, Catherine White, Kevin Wilson, Jonathan R. Young, Hongjun Zhang
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Publication number: 20140228219Abstract: The present invention provides a compound having an excellent efficacy for controlling weeds. A cyclohexanone compound of the formula (I): wherein m is an integer of 1, 2 or 3; n is an integer of any one of 1 to 5; X represents CH2, O, S, S(O) or S(O)2; R1 represents a hydrogen atom or a methyl group; R2 and R3 represents a hydrogen atom, a C1-6 alkyl group and the like; R4 represents a C6-10 aryl group or a five- to six-membered heteroaryl group; G represents a hydrogen atom and the like; Z represents a halogen atom, a cyano group, a nitro group, a phenyl group, a C1-6 alkyl group and the like; is useful as an active ingredient for herbicides.Type: ApplicationFiled: May 29, 2012Publication date: August 14, 2014Inventors: Yosuke Nakashima, Yoshinobu Jin, Masato Konobe
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Publication number: 20140219925Abstract: Novel polymer nanovectors or particles and use thereof as medication and/or diagnostic agents.Type: ApplicationFiled: June 28, 2012Publication date: August 7, 2014Applicant: INSERM (Institut National de la Sante et de la Recherche Medicale)Inventors: Philippe Bertrand, Regis Delatouche, Valerie Heroguez, Floraine Collette, Marc Gregoire, Christophe Blanquart, Fabien Gueugnon
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Publication number: 20140221357Abstract: The present invention provides compounds of Formula (I) or Formula (III): [INSERT CHEMICAL STRUCTURE HERE] (I) [INSERT CHEMICAL STRUCTURE HERE] (III) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: September 25, 2012Publication date: August 7, 2014Applicant: Bristol-Myers Squibb CompanyInventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
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Publication number: 20140221421Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.Type: ApplicationFiled: January 9, 2014Publication date: August 7, 2014Applicant: GILEAD SCIENCES, INC.Inventors: Steven S. BONDY, Carina E. CANNIZZARO, Chien-Hung CHOU, John O. LINK, Qi LIU, Scott D. SCHROEDER, Winston C. TSE, Jennifer R. ZHANG
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Patent number: 8796465Abstract: The present invention relates to processes for the preparation of triazoles. These compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.Type: GrantFiled: March 18, 2013Date of Patent: August 5, 2014Assignee: Melinta Therapeutics, Inc.Inventors: Shili Chen, Rongliang Lou, Yusheng Wu, Jiacheng Zhou, Roger Hanselmann
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Patent number: 8790621Abstract: The invention provides multivalent surface-crosslinked micelle (SCM) particles, crosslinked reverse micelle (CRM) particles, and methods of making and using them. The SCM particles can be used, for example, to inhibit a virus or bacteria from binding to a host cell. The inhibition can be used in therapy for the flu, cancer, or AIDS. The CRM particles can be used, for example, to prepare metal nanoparticles or metal alloy nanoparticles, or they can be used in catalytic reactions.Type: GrantFiled: April 8, 2011Date of Patent: July 29, 2014Assignee: Iowa State University Research Foundation, Inc.Inventor: Yan Zhao
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Patent number: 8791102Abstract: This disclosure relates to sphingosine-1-phosphate (S1P) receptor antagonists, compositions comprising the S1P receptor antagonists and methods for using and processes for making the S1P receptor antagonists. In particular, this disclosure relates to sphingosine-1-phosphate 1 (S1P1) receptor antagonists, compositions comprising the S1P1 receptor antagonist and methods for using the S1P1 receptor antagonist, such as in the treatment of cancer, and processes for making the S1P1 receptor antagonists.Type: GrantFiled: October 16, 2009Date of Patent: July 29, 2014Assignee: Exelixis, Inc.Inventors: Mohamed Abdulkader Ibrahim, Joon Won Jeong, Henry William Beecroft Johnson, Patrick Kearney, James W. Leahy, Gary L. Lewis, Robin Tammie Noguchi, John M. Nuss
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Publication number: 20140206645Abstract: Disclosed herein are novel compounds of formula (I), and uses thereof. The compounds of Formula (I) are inhibitors of histone deacetylases (HDACs) and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase (HMGR). Also provided are methods of using the compounds of Formula (I) for inhibiting the activity of HDACs and HMGR, treating diseases associated with HDACs or HMGR (e.g.Type: ApplicationFiled: January 21, 2014Publication date: July 24, 2014Applicants: National Taiwan University, Academia SinicaInventors: Jung-Hsin LIN, Ching-Chow CHEN, Jim-Min FANG, Jhih-Bin CHEN, Ting-Rong CHERN, Tzu-Tang WEI
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Publication number: 20140200247Abstract: New polymorphs of 5-amino or substituted amino 1,2,3-triazole and substituted derivatives thereof, of orotates of the carboxyamidotriazoles, of formulations of the triazoles and orotic acid in the ratio of 1:1 to 1:4 (base:acid) and of safer processes of the preparation of the same are disclosed. The compounds are useful in the control and treatment of diseases including, but not limited to solid cancers, macular degeneration, retinopathy, chronic myeloid leukemia, AIDS and diseases which rely on aberrant signal transduction. The improved processes to prepare the orotate formulations use stable, efficient and safer starting azide intermediate materials in the synthesis of new polymorphs of carboxyamidotriazole.Type: ApplicationFiled: January 16, 2013Publication date: July 17, 2014Inventor: Rashida A. Karmali
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Publication number: 20140200333Abstract: Dendronic reporters are described which incorporate a high density of luminescent or non-luminescent dyes at periphery sites and a focal point group that is reactive, ionic or a conjugated substance. Such dendronic reporters are capable of sensing analytes, or are otherwise useful in luminescent assays. Additionally, methods of synthesis are described.Type: ApplicationFiled: August 14, 2012Publication date: July 17, 2014Applicant: SETA BIOMEDICALS, LLCInventors: Ewald Terpetschnig, Inna G. Yermolenko, Olena M. Obukhova, Anatoliy Tatarets, Leonid D. Patsenker
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Patent number: 8778626Abstract: A clickable cross-linker compound provides an easily scanned reporter ion for effective and efficient cross-linking and identification of intermolecular and intramolecular interactions of proteins and peptides.Type: GrantFiled: July 8, 2011Date of Patent: July 15, 2014Assignee: California Institute of TechnologyInventors: Chang Ho Sohn, Jesse L. Beauchamp
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Patent number: 8779155Abstract: A TAF compound that can have substitutions on either of the two benzene rings and/or the C-5 position of the triazole to alter the properties of the TAF compound can be wherein X can be H, an aromatic group, a hetero aromatic group, an alkyl or any substituted alkyl group, ketone, aldyhyde, carboxylic acid derivatives; Y1, Y2, Y3, Y4, and Y5 can be one or more of H, aromatic groups, hetero aromatic groups, alkyl or any substituted alkyl groups, ketone, aldyhyde, or carboxylic acid derivatives; and Z1, Z2, Z3, Z4, and Z5 can be one or more of H aromatic groups, hetero aromatic groups, alkyl or any substituted alkyl groups, ketone, aldyhyde, or carboxylic acid derivatives. Included is a preparation of the TAF compound and use as a photoactive and/or catalyst.Type: GrantFiled: May 12, 2011Date of Patent: July 15, 2014Assignee: West Virginia UniversityInventor: Xiaodong Shi
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Publication number: 20140194620Abstract: The present invention relates to a precursor of positron emission tomography (PET) radioactive medical supplies, a preparation method thereof, and an application thereof, and more specifically, to a precursor having a tetravalent organic salt leaving group, a preparation method, and a method for preparing desired PET radioactive medical supplies in a high radiochemical yield within a short preparation time by introducing 18F using the same through a single step. The precursor having a tetravalent organic salt leaving group of the present invention can simplify the known complex multistep preparation of radioactive medical supplies into a single step, can save production costs because an excessive amount of a phase transfer catalyst is not required, facilitates separation of a compound after reaction, and enables rapid reaction velocity. The features are appropriate for the mass production of PET radioactive medical supplies by an automated synthesis system.Type: ApplicationFiled: May 11, 2012Publication date: July 10, 2014Applicant: FUTURECHEM CO., LTD.Inventors: Dae-Yoon Chi, Byoung-Se Lee, Chansoo Park, Min-Hyung Lee, Hyojin Cha, Woojin Cho, Heewon Kang, Kyunghun Kim
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Publication number: 20140193363Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: January 15, 2014Publication date: July 10, 2014Applicant: ENANTA PHARMACEUTICALS, INC.Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
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Patent number: 8772510Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R5, W, X, X1, Y, Y1, Z and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used in the treatment of CNS disorders such as schizophrenia, Alzheimer's disease, and Parkinson's disease.Type: GrantFiled: August 30, 2012Date of Patent: July 8, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Stephan Bachmann, Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Markus Rudolph
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Patent number: 8765812Abstract: Substituted cinnamoyl anthranilate compounds exhibiting anti-fibrotic activity; or derivatives thereof, analogues thereof, pharmaceutically acceptable salts thereof, and metabolites thereof; with the proviso that the compound is not Tranilast.Type: GrantFiled: July 5, 2007Date of Patent: July 1, 2014Assignee: Fibrotech Therapeutics Pty LtdInventors: Spencer John Willams, David Stapleton, Steven Zammit, Darren James Kelly, Richard Ernest Gilbert, Henry Krum
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Publication number: 20140179733Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.Type: ApplicationFiled: December 20, 2013Publication date: June 26, 2014Applicant: ChemoCentryx, Inc.Inventors: Xi Chen, Dean R. Dragoli, Pingchen Fan, Juan C. Jaen, Yandong Li, Jay P. Powers, Viengkham Malathong, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang
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Publication number: 20140179626Abstract: Acadesine derivatives as a drug, as well as the derivatives for the treatment of cancer and in particular for the treatment of chronic myeloid leukemia are described. Also, product containing the derivatives and at least one second active ingredient as a combination product for simultaneous, separate or sequential administration, in the treatment of cancer, as well as a pharmaceutical composition containing the derivatives and a pharmaceutically acceptable carrier are described. Finally, a method for inhibiting the in vitro cell proliferation including the placement of an in vitro cell in contact with the derivatives and methods for synthesis of said derivatives and methods for synthesis of the derivatives are described.Type: ApplicationFiled: April 17, 2012Publication date: June 26, 2014Inventors: Rachid Benhida, Patrick Auberger, Vincent Malnuit, Mohsine Driowya, Alexandre Puissant, Guillaume Robert
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Publication number: 20140179699Abstract: The present invention relates to compounds useful as inhibitors of indoleamine 2,3-dioxygenase (IDO). The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications. The compounds of this invention have formula I-A: wherein the variables are as defined herein.Type: ApplicationFiled: November 19, 2013Publication date: June 26, 2014Inventors: Dean Boyall, Christopher Davis, James Dodd, Simon Everitt, Andrew Miller, Peter Weber, James Westcott, Stephen Young
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Publication number: 20140171403Abstract: The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in diseases and disorders mediated by autotaxin.Type: ApplicationFiled: March 15, 2013Publication date: June 19, 2014Applicant: Novartis AGInventors: Darren Mark Legrand, Vikki Furminger, Christopher Thomson, Owen Rhys Hughes, Emily Stanley
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Patent number: 8754237Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel bifunctional, trifunctional, or multifunctional compounds for inhibiting histone deacetylases, and pharmaceutically acceptable salts and derivatives thereof. The present invention further provides methods for treating disorders regulated by histone deacetylase activity (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, hair loss, etc.) comprising administering a therapeutically effective amount of an inventive compound to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.Type: GrantFiled: July 16, 2012Date of Patent: June 17, 2014Assignees: President and Fellows of Harvard College, Dana-Farber Cancer Institute, Inc.Inventors: James Elliot Bradner, Ralph Mazitschek, Weiping Tang, Stuart L. Schreiber
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Publication number: 20140155618Abstract: A charge transport material includes a combined structure obtained by condensing a compound represented by (1) and a compound represented by (2), and combining the compound represented by (2) and a compound represented by (3) with an Ar included in the compound represented by (2) therebetween, in following Formula 1,Type: ApplicationFiled: November 26, 2013Publication date: June 5, 2014Applicant: SAMSUNG DISPLAY CO., LTD.Inventor: Junta FUCHIWAKI
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Publication number: 20140155619Abstract: The invention relates to the preparation of 1,2,3-triazole-4-carboxamide of general Formula I: wherein R1 and R2 may be the same or different and are selected from H, F, Cl, Br, I, OR, C(O)R, NH2, NHR or NR2. R can be a linear or branched alkyl group, for example a C1-C4 alkyl group. In exemplary embodiments, R1 and R2 are independently selected from H, F, Cl, Br, and I. The compound of Formula I can be Rufinamide.Type: ApplicationFiled: December 3, 2013Publication date: June 5, 2014Applicant: TARO PHARMACEUTICAL INDUSTRIES LIMITEDInventors: Shimon Cherynyak, Rosa Cyjon, Ilana Ozer
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Publication number: 20140155436Abstract: The present invention relates to a compound of one of the formulas I to XXI; a pharmaceutical composition comprising at least one such compound; and the use of at least one such compound in preparing a drug to treat, in a subject, a genetic disease resulting from at least one splicing anomaly.Type: ApplicationFiled: November 4, 2013Publication date: June 5, 2014Applicants: CENTRE NATIONAL DE RECHERCHE SCIENTIFIQUE, UNIVERSITE MONTPELLIER 2 SCIENCES ET TECHNIQUES, INSTITUT CURIEInventors: Jamal TAZI, David GRIERSON, Florence MAHUTEAU-BETZER, Pierre ROUX
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Patent number: 8729114Abstract: Disclosed are Cathepsin-S reversible inhibitor compounds of the formula (I) which are useful in the treatment of autoimmune and other diseases. Also disclosed are pharmaceutical compositions containing the same, and methods of making and using the same.Type: GrantFiled: March 2, 2011Date of Patent: May 20, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Michael J. Burke, Derek Cogan, Donghong Amy Gao, Alexander Heim-Riether, Eugene Richard Hickey, Matthew Russell Netherton, Philip Dean Ramsden, David Charles Thompson, Zhaoming Xiong
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Patent number: 8729270Abstract: Embodiments relate to the field of chemistry and biochemistry, and, more specifically, to anti-cancer compounds, synthesis thereof, and methods of using same. Disclosed herein are various heterocyclic compounds and methods of using the novel anti-cancer compounds to inhibit the growth of a cancer cell, for instance a leukemia, non-small cell lung, central nervous system (CNS), skin, ovarian, renal, prostate, breast, or colon cancer cell. Other embodiments include methods of treating cancer in a subject, such as using the disclosed heterocyclic anti-cancer agents.Type: GrantFiled: July 17, 2012Date of Patent: May 20, 2014Assignee: University of Notre Dame du LacInventors: Marvin J. Miller, Garrett C. Moraski, Jonathan Stefely
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Patent number: 8728978Abstract: Suggested are biocide compositions, comprising (a) esters based on ketocarboxylic acids, (b) biocides, and optionally (c) oil components or co-solvents and/or (d) emulsifiers. The compositions exhibit an improved stability even if stored at temperatures between 5° and 40° C. over a longer period.Type: GrantFiled: August 24, 2010Date of Patent: May 20, 2014Assignee: Cognis IP Management GmbHInventors: Joaquin Bigorra Llosas, Stéphanie Merlet, Ramon Valls, Stefan Busch
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Patent number: 8722686Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II); and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B. L1-L4 A, B, R1-R4 and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.Type: GrantFiled: September 1, 2009Date of Patent: May 13, 2014Assignee: Pfizer Inc.Inventors: Matthew F. Brown, Charles F. Donovan, Edmund L. Ellsworth, Denton W. Hoyer, Timothy A. Johnson, Manjinder S. Lall, Chris Lim-Berakis, Sean T. Murphy, Debra A. Sherry, Clarke B. Taylor, Joseph S. Warmus
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Publication number: 20140113944Abstract: The present invention provides novel mGlu2 agonists useful in the treatment of bipolar disorder, schizophrenia, and generalized anxiety disorder.Type: ApplicationFiled: June 7, 2012Publication date: April 24, 2014Applicant: ELI LILLY AND COMPANYInventors: Teresa Tse Ki Man, James Allen Monn, Carlos Montero Salgado, Lourdes Prieto, David Edward Tupper, Lesley Walton
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Publication number: 20140113941Abstract: This invention provides a compound having the structure wherein R1 is H, wherein n and q are independently an integer from 0 to 8; A is absent or present and when present is wherein m is an integer from 0 to 8; R3 is an amino, alkyl, aryl, heteroaryl, diol, piperazine, morpholine, piperidine, triazole, azide or biphenyl, each with or without substitution, branched or unbranched, or and R4 is alkyl, aryl, or heteroaryl, each with or without substitution, branched or unbranched, R2 is H, CH3, or alkyl, aryl, heteroaryl, pyrrole, diazole, or triazole, each with or without substitution, branched or unbranched, or wherein n and q are independently an integer from 0 to 8; A is absent or present and when present is and R6 is azide, methoxy, trifluoromethyl, biphenyl, substituted phenyl, substituted triazole, or alkyl, aryl or heteroaryl, with or without substitution, branched or unbranched, when R1 is H then R2 is other than H or CH3, andType: ApplicationFiled: March 23, 2012Publication date: April 24, 2014Applicant: The Research Foundation for The State University of New YorkInventors: Peter Tonge, Carl Machutta, Gopal Reddy Bommineni, Kanishk Kapilashrami
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Publication number: 20140114068Abstract: Disclosed are novel indanone derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The indanone derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, flu, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media.Type: ApplicationFiled: June 18, 2012Publication date: April 24, 2014Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN K.U. LEUVEN R & D, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Young Sik Jung, Chong Kgo Lee, Hae Soo Kim, Hee Chun Jeong, Pil Ho Kim, Soo Bong Han, Jin Soo Shin, Johan Neyts, Hendrik Jan Thibaut
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Publication number: 20140107327Abstract: This disclosure relates to a method that involves reacting an azide with an alkyne in the presence of deuterated water and a copper-containing catalyst, thereby forming a deuterated 1,2,3-triazole.Type: ApplicationFiled: March 26, 2012Publication date: April 17, 2014Applicant: RESEARCH FOUDATION OF THE CITY UNIVERSITY OF NEW YORKInventors: Mahesh K. Lakshman, Hari Kiran Akula
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Publication number: 20140107168Abstract: A compound of formula I wherein Ar1 is a bicyclic aryl or heteroaryl, which may be optionally substituted; X and Y are each independently a group of formula II: -L1-Ar2-L2-Ar3-Q-(CH2)n-NR1R2 L1 and L2 are each independently selected from NR3, C2H2, CH2, —O—, —S— and a bond; Ar2 and Ar3 are independently optionally substituted C5 or C6 aryl or heteroaryl; Q is selected from NH(C?O), NR3, S, O; n is an integer from 1 to 5; R1 and R2 are optionally substituted and are independently hydrogen, C1-7 alkyl, C3-20 heterocyclyl, or C5-20 aryl, or R1 and R2, taken together with the nitrogen atom to which they are attached, form a heterocyclic ring having from 3 to 8 ring atoms; R3 is H or C1-7 alkyl.Type: ApplicationFiled: April 4, 2012Publication date: April 17, 2014Applicant: UNIVERSITY COLLEGE LONDONInventors: Stephen Neidle, Caterina Lombardo, Sarah Walsh
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Patent number: 8697696Abstract: The present invention is concerned with novel triazole compounds of formula (I) wherein A, X, Y, u, v, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts thereof. The compounds of present invention have affinity and selectivity for the GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.Type: GrantFiled: November 2, 2011Date of Patent: April 15, 2014Assignee: Roche Palo Alto LLCInventors: Stephen Deems Gabriel, Andrew Thomas
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Patent number: 8697911Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: June 29, 2011Date of Patent: April 15, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Brian Nicholas Cook, Jennifer A. Kowalski, Xiang Li, Daniel Richard Marshall, Sabine Schlyer, Robert Sibley, Lana Louise Smith-Keenan, Fariba Soleymanzadeh, Ronald John Sorcek, Erick Richard Roush Young, Yunlong Zhang
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Publication number: 20140093518Abstract: Provided herein is a method for chemically programmed vaccination. Methods include inducing a covalent-binding polyclonal antibody response in a subject and programming the polyclonal response with a targeting compound.Type: ApplicationFiled: August 26, 2013Publication date: April 3, 2014Applicant: The Scripps Research InstituteInventor: Carlos F. Barbas, III
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Publication number: 20140094480Abstract: This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protection from neuron cell death.Type: ApplicationFiled: December 9, 2013Publication date: April 3, 2014Applicant: Board of Regents of The University of Texas SystemInventors: Steven L. McKnight, Joseph M. Ready, Andrew A. Pieper, Jef K. De Brabander
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Patent number: 8685975Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.Type: GrantFiled: November 16, 2012Date of Patent: April 1, 2014Assignee: Omeros CorporationInventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
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Patent number: 8680125Abstract: Described herein are methods for treating inflammatory disorders. The methods comprise administering to a subject in need thereof a therapeutically effective amount of a synthetically modified fullerene.Type: GrantFiled: March 3, 2009Date of Patent: March 25, 2014Assignee: Luna Innovations IncorporatedInventors: Christopher L. Kepley, Robert P. Lenk, Stephen R. Wilson, Zhiguo Zhou, Darren K. MacFarland
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Patent number: 8669274Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: GrantFiled: December 13, 2011Date of Patent: March 11, 2014Assignee: Viamet Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Robert J. Schotzinger, Stephen W. Rafferty