Plural Nitrogens In The Hetero Ring Patents (Class 540/460)
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Patent number: 8754116Abstract: Inhibitors of HCV replication of formula (I) wherein W is a heterocycle of formula and the remaining variables are as defined in the specification.Type: GrantFiled: April 20, 2012Date of Patent: June 17, 2014Assignee: Janssen R&D IrelandInventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Dominique Louis Nestor Ghislain Surleraux, Wim Van De Vreken
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Patent number: 8754106Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy, or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrogType: GrantFiled: March 15, 2013Date of Patent: June 17, 2014Assignees: Janssen R&D Ireland, Medivir ABInventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Lili Hu, Abdellah Tahri, Dominique Louis Nestor Ghislain Surleraux, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Vladimir Ivanov, Mikael Pelcman, Anna Karin Gertrud Linea Belfrage, Per-Ola Mikael Johansson, Sandrine Marie Helene Vendeville
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Publication number: 20140163219Abstract: A compound of general formula (I); A is O, S, CH, NH or NR?, when O links with Z3, Z1 is N or CRZ1, Z2 is CRZ2, when Z1 links with O, Z2 is CH, Z3 is C—Ar; Ra, Rb, Rc and Rd independently is H, OH, halogen or —Y1—Rm; A1 is NH or CH2; R1? is alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl; A2 is N, O or linking bond; R1 is hydrogen, or, R1 linking covalently with R3 forms C5-C9 saturated or unsaturated hydrocarbon chain substituted by O or N; R3 is alkyl, cycloalkyl, heterocycloalkyl, alkyl substituted by cycloalkyl etc; R4 is alkoxy-CO, alkyl-NHCO, (alkyl)2NCO, or formyl substituted by aryl, cycloalkyl, heterocycloalkyl.Type: ApplicationFiled: July 23, 2012Publication date: June 12, 2014Applicant: Shanghai Tangrun Pharmaceuticals, Co., Ltd.Inventor: Suoming Zhang
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Publication number: 20140163002Abstract: The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: ApplicationFiled: August 6, 2012Publication date: June 12, 2014Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Patrick Y.S. Lam, Charles G. Clark, James R. Corte, William R. Ewing, Paul J. Gilligan, Yoon Jeon, Wu Yang, Leon M. Smith, II, Yufeng Wang
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Patent number: 8748388Abstract: Antitumoral compounds of Formula I, and pharmaceutically acceptable salts, derivatives, tautomers, prodrugs or stereoisomers thereof useful as antitumour agents.Type: GrantFiled: December 10, 2008Date of Patent: June 10, 2014Assignee: Pharma Mar, S.A.Inventors: Judit Tulla-Puche, Eleonora Marcucci, Núria Bayó-Puxan, Fernando Albericio, Maria del Carmen Cuevas Marchante
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Patent number: 8741926Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy, or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrogeType: GrantFiled: November 28, 2012Date of Patent: June 3, 2014Assignees: Janssen R&D Ireland, Medivir ABInventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Lili Hu, Abdellah Tahri, Dominique Louis Nestor Ghislain Surleraux, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Åsa Annica Kristina Rosenquist, Vladimir Ivanov, Mikael Pelcman, Anna Karin Gertrud Linnea Belfrage, Per-Ola Mikael Johansson, Sandrine Marie Helene Vendeville
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Patent number: 8729258Abstract: The present invention provides a novel class of macrocyclic compounds as well as complexes formed between a metal (e.g., lanthanide) ion and the compounds of the invention. Preferred complexes exhibit high stability as well as high quantum yields of lanthanide ion luminescence in aqueous media without the need for secondary activating agents. Preferred compounds incorporate hydroxy-isophthalamide moieties within their macrocyclic structure and are characterized by surprisingly low, non-specific binding to a variety of polypeptides such as antibodies and proteins as well as high kinetic stability. These characteristics distinguish them from known, open-structured ligands.Type: GrantFiled: April 30, 2012Date of Patent: May 20, 2014Assignee: The Regents of the University of CaliforniaInventors: Kenneth N. Raymond, Todd M. Corneillie, Jide Xu
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Patent number: 8722881Abstract: A tetradendate amide based macrocyclic ligand and its Fe(III) complex which act as activators of hydrogen peroxide. The synthetic methodology to develop the ligands is new, simple and provides better yield for each step of the ligand synthesis. The Fe(III)-complexes and hydrogen peroxide together are can perform several environmentally benign oxidation reactions. Organic dye bleaching, bleaching of pulp and paper effluent and N-oxide synthesis may be performed using the newly developed catalyst and hydrogen peroxide. Alcohol oxidation and alkene epoxidation may also be performed using the catalysts and hydrogen peroxide.Type: GrantFiled: October 13, 2010Date of Patent: May 13, 2014Assignee: Board of Trustees of the University of ArkansasInventors: Anindya Ghosh, Shane Z. Sullivan, Samuel L. Collom, Sharon Pulla
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Patent number: 8710046Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.Type: GrantFiled: June 30, 2010Date of Patent: April 29, 2014Assignee: Albany Molecular Research, Inc.Inventors: Peter R. Guzzo, David D. Manning, William Earley
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Publication number: 20140113929Abstract: Inhibitors of HCV replication of formula (I) and the salts and stereoisomers thereof, wherein each dashed line (represented by - - - - -) represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 is C1-6alkyl or C3-7cycloalkyl; R5 is hydrogen, halo, C1-6alkyl, hydroxy, C1-6alkoxy, polyhaloC1-6alkyl; R6 is hydrogen, C1-6alkoxy, mono- or diC1-6alkylamino; or R5 and R6 may form a 5- or 6-membered unsaturated or partially unsaturated ring, optionally comprising one or two selected from O, N and S; R7 is hydrogen; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl; R8 is C3-7cycloalkyl optionally substituted with C1-6alkyl; C1-6alkyl optionally substituted with C3-7cycloalkyl; or —NR8aR8b; R8a and R8b are C1-6alkyl, or both may form a 5- or 6-memberType: ApplicationFiled: December 20, 2013Publication date: April 24, 2014Applicant: Janssen R&D Ireland (formerly Tibotec Pharmaceuticals)Inventors: Pierre Jean-Marie Raboisson, Herman Augustinus De Kock, David Craig Mc Gowan, Lili Hu, Abdellah Tahri, Sandrine Marie Helene Vendeville, Wim Van De Vreken
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Publication number: 20140100364Abstract: Compounds useful for making HCV protease inhibitors are described. Methods of using these compounds to make HCV protease inhibitors are also provided.Type: ApplicationFiled: October 7, 2013Publication date: April 10, 2014Inventors: Kenneth M. Engstrom, Yanqun Zhao
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Publication number: 20140093449Abstract: Analogs of largazole are described herein. Methods of treating cancer and blood disorders using largazole and largazole analogs and pharmaceutical compositions comprising the same are additionally described herein. Methods for preparing largazole analogs are likewise described.Type: ApplicationFiled: July 17, 2013Publication date: April 3, 2014Applicants: COLORADO STATE UNIVERSITY RESEARCH FOUNDATION, UNIVERSITY OF NOTRE DAME DU LAC, DANA-FARBER CANCER INSTITUTE, INC.Inventors: Robert M. Williams, James E. Bradner, Albert Bowers, Tenaya Newkirk, Olaf G. Wiest
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Patent number: 8685953Abstract: The present invention relates to linear and cyclic guanidine derivatives, method of preparation and uses thereof, pharmaceutical compositions to be used as antifungal agents, in particular against Candida species.Type: GrantFiled: March 12, 2009Date of Patent: April 1, 2014Assignee: Universita Degli Studi Di SienaInventors: Maurizio Botta, Francesco Raffi, Paolo Visca
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Patent number: 8664212Abstract: The invention relates to diazo 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: July 25, 2012Date of Patent: March 4, 2014Assignee: The Regents of the University of MichiganInventors: Shaomeng Wang, Yuefeng Peng, Haiying Sun, Qian Cai, Zaneta Nikolovska-Coleska, Jianfeng Lu, Su Qiu
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Publication number: 20140057924Abstract: Inhibitors of IAP proteins and compositions containing the same are disclosed. Methods of using the IAP protein inhibitors in the treatment of diseases and conditions wherein inhibition of IAP proteins provides a benefit, like cancers, also are disclosed.Type: ApplicationFiled: August 16, 2013Publication date: February 27, 2014Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Rong Sheng, Haiying Sun, Liu Liu, Jianfeng Lu, Donna McEachern
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Publication number: 20140058082Abstract: The present invention relates to an intermediate, as represented by formula (I), for synthesizing caspofungin, and a preparation method thereof. The intermediate enables efficient preparation of caspofungin.Type: ApplicationFiled: March 21, 2012Publication date: February 27, 2014Applicant: UNITRIS BIOPHARMA CO., LTD.Inventors: Fuyao Zhang, Xiaoming Shen, Gaoqiang Hu, Piaoyang Sun
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Publication number: 20140038969Abstract: The present invention provides compounds of Formula (VIII): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: ApplicationFiled: August 2, 2013Publication date: February 6, 2014Inventors: Wu Yang, James R. Corte, Paul J. Gilligan, Donald J.P. Pinto, William R. Ewing, Yufeng Wang
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Patent number: 8642014Abstract: Luminescent reporter compounds that are rotaxanes having the structure where B—Z—C is a reporter molecule based on a cyanine, squaric acid, or other reporter, and K is a macrocycle that encircles and interlocks with the reporter molecule. Applications of the reporter compounds are provided, as well as reactive intermediates used to synthesize the reporter compounds, and methods of synthesizing the reporter compounds.Type: GrantFiled: July 30, 2009Date of Patent: February 4, 2014Assignee: SETA BioMedicals, LLCInventors: Ewald A. Terpetschnig, Leonid D. Patsenker, Oleksii Klochko, Yuliia Kudriavtseva, Anatoliy L. Tatarets, Inna G. Yermolenko, Yevgen A. Povrozin
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Publication number: 20140030221Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of virus infections, particularly hepatitis C infections.Type: ApplicationFiled: June 7, 2013Publication date: January 30, 2014Inventors: Caroline Aciro, Victoria Alexandra Steadman, Simon Neil Pettit, Karine G. Poullennec, Linos Lazarides, David Kenneth Dean, Neil Andrew Dunbar, Adrian John Highton, Andrew John Keats, Dustin Scott Siegel, Kapil Kumar karki, Adam James Schrier, Petr Jansa, Richard Mackman
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Publication number: 20140031351Abstract: The present invention provides compounds of Formula I or a pharmaceutically acceptable salt forms thereof, wherein R1, R2, R3, R4, R5, A and X are as defined herein, methods of treatment and uses thereof.Type: ApplicationFiled: September 13, 2013Publication date: January 30, 2014Applicant: Cephalon, Inc.Inventors: Henry J. Breslin, Bruce D. Dorsey, Gregory R. Ott
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Patent number: 8557798Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt, solvate or ester thereof, wherein U, W, X, L, Y, M, Z, c, d, e, f, g, h, s, t, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and R18 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: GrantFiled: November 17, 2009Date of Patent: October 15, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Ulrich Iserloh, Zhaoning Zhu, Andrew Stamford, Johannes H. Voigt
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Publication number: 20130267698Abstract: Provided herein are ruthenium complexes of Formula I, and processes of preparation thereof. Also provided are methods of their use as a metathesis catalyst.Type: ApplicationFiled: June 5, 2013Publication date: October 10, 2013Inventors: Christophe Claude Parsy, Francois-Rene Alexandre, Florence Marie-Emilie Bonnaterre, Dominique Surleraux
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Publication number: 20130267467Abstract: The invention provides methods of making and using compounds of the formula shown, which are inhibitors of human plasmin and plasma kallikrein. (Formula I) The compounds are useful for the prevention of blood loss, and as components of fibrin adhesives.Type: ApplicationFiled: July 5, 2011Publication date: October 10, 2013Inventors: Torsten Steinmetzer, Sebastian Martin Saupe
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Publication number: 20130267511Abstract: The present invention relates to inhibitors of HCV replication of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein R1; R3; and R4 have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.Type: ApplicationFiled: June 3, 2013Publication date: October 10, 2013Inventors: Pierre Jean-Marie Bernard Raboisson, Lili Hu, Sandrine Vendeville, Origene Nyanguile
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Publication number: 20130266512Abstract: A Diels-Alder adduct of a trans-cyclooctene with a tetrazine is provided, wherein the adduct bears a substituent labeled with a radionuclide. A method of producing a PET or other image of an organ in an animal or human includes forming the Diels-Alder adduct in the animal or human. Trans-cyclooctenes and tetrazines suitable for preparing the adducts are provided.Type: ApplicationFiled: July 21, 2011Publication date: October 10, 2013Applicants: University of Southern California, University of DelawareInventors: Joseph M. Fox, Matthew Hassink, Melissa Blackman, Zibo Li, Peter S. Conti, Ramajeyam Selvaraj
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Patent number: 8518928Abstract: The invention provides compounds of formula I: wherein A, B, D, E, R1, R2, R3, R4, R5, X, and - - - have any values defined herein, as well as salts thereof. The compounds have activity as G-quadruplex DNA stabilizers and as anti-proliferative agents.Type: GrantFiled: November 30, 2011Date of Patent: August 27, 2013Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. Lavoie, Joseph E. Rice, Leroy F. Liu
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Publication number: 20130210113Abstract: Chemically reactive carbocyanine dyes that are intramolecularly crosslinked between the 1-position and 3?-position, their bioconjugates and their uses are described. 1,3?-crosslinked carbocyanines are superior to those of conjugates of spectrally similar 1,1?-crosslinked or non-crosslinked dyes. The invention includes derivative compounds having one or more benzo nitrogens.Type: ApplicationFiled: December 18, 2012Publication date: August 15, 2013Applicant: AnaSpec IncorporatedInventor: AnaSpec Incorporated
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Publication number: 20130203776Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.Type: ApplicationFiled: May 13, 2011Publication date: August 8, 2013Inventors: Steven Wade Andrews, Kevin Ronald Condroski, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Jeongbeob Seo, HongWoon Yang, Qian Zhao
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Patent number: 8497270Abstract: Compound having formula (I), wherein —W is NH—, —N(CH3)— or piperazine, —X is a bond, —C(?O)— or S(?O)2—, —Y is C3-7alkylene, and —Z is NH—C(?O)— or —O—, and pharmaceutically acceptable salts thereof, their pharmaceutical formulations and use as HIV inhibitors.Type: GrantFiled: October 13, 2010Date of Patent: July 30, 2013Assignee: Elanco Animal Health Ireland LimitedInventors: Johannes Wilhelmus J Thuring, Jean-Francois Bonfanti, Jerome Michel Claude Fortin
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Publication number: 20130150572Abstract: Provided herein are ruthenium complexes of Formula I, and processes of preparation thereof. Also provided are methods of their use as a metathesis catalyst.Type: ApplicationFiled: February 12, 2013Publication date: June 13, 2013Applicant: IDENIX PHARMACEUTICALS, INC.Inventor: Idenix Pharmaceuticals, Inc.
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Publication number: 20130150309Abstract: Cyclic peptidomimetics that inhibit the interaction between MLL1 and WDR5 are disclosed. Methods of inhibiting MLL1 activity and methods of treating cancers also are disclosed.Type: ApplicationFiled: November 27, 2012Publication date: June 13, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventor: The Regents of the University of Michigan
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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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Patent number: 8431716Abstract: The invention relates to special (methyl)acrylaic monomers and concerns more particularly an enhanced process for preparing solutions of alkylimiozolidone (meth)acrylates in water solutions of alkylimidazolidone (meth)acrylates in a light (meth)acrylate.Type: GrantFiled: April 8, 2009Date of Patent: April 30, 2013Assignee: Arkema FranceInventors: Alain Riondel, Jean-Michel Paul
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Publication number: 20130102774Abstract: A process for transforming a group >C?O (I) in a compound into a group >C?S (II) or into a tautomeric form of group (II) in a reaction giving a thionated reaction product, by use of crystalline P2S5.2 C5H5N as a thionating agent. A thionating agent which is crystalline P2S5.2 C5H5N.Type: ApplicationFiled: February 3, 2012Publication date: April 25, 2013Applicant: VIRONOVA ABInventors: Birgitta Pettersson, Vedran Hasimbegovic, Per H Svensson, Jan Bergman
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Publication number: 20130095066Abstract: The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: ApplicationFiled: April 5, 2012Publication date: April 18, 2013Inventors: Tao Wang, Li-Qiang Sun, Paul Michael Scola
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Publication number: 20130089520Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy, or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrogeType: ApplicationFiled: November 28, 2012Publication date: April 11, 2013Applicants: MEDIVIR AB, TIBOTEC PHARMACEUTICALS LTD.Inventors: TIBOTEC PHARMACEUTICALS LTD., MEDIVIR AB
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Publication number: 20130065872Abstract: The disclosure relates generally to methods for the preparation of a family of natural compounds, the syrbactins and their analogs.Type: ApplicationFiled: December 3, 2010Publication date: March 14, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventor: Michael C. Pirrung
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Patent number: 8367065Abstract: The present invention provides single chain antibody-directed polymeric prodrugs containing multifunctional linkers. Methods of making the polymeric delivery systems and methods of treating mammals using the same are also disclosed.Type: GrantFiled: March 12, 2009Date of Patent: February 5, 2013Assignee: Enzon Pharmaceuticals, Inc.Inventors: Hong Zhao, Prasanna Reddy, Maria Belen Rubio
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Patent number: 8349869Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy, or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrogType: GrantFiled: March 6, 2012Date of Patent: January 8, 2013Assignees: Tibotec Pharmaceuticals Ltd., Medivir ABInventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Lili Hu, Abdellah Tahri, Dominique Louis Nestor Ghislain Surleraux, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Åsa Annica Kristina Rosenquist, Vladimir Ivanov, Mikael Pelcman, Anna Karin Gertrud Linea Belfrage, Per-Ola Mikael Johansson, Sandrine Marie Helene Vendeville
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Publication number: 20120329174Abstract: The present invention provides a novel class of macrocyclic compounds as well as complexes formed between a metal (e.g., lanthanide) ion and the compounds of the invention. Preferred complexes exhibit high stability as well as high quantum yields of lanthanide ion luminescence in aqueous media without the need for secondary activating agents. Preferred compounds incorporate hydroxy-isophthalamide moieties within their macrocyclic structure and are characterized by surprisingly low, non-specific binding to a variety of polypeptides such as antibodies and proteins as well as high kinetic stability. These characteristics distinguish them from known, open-structured ligands.Type: ApplicationFiled: April 30, 2012Publication date: December 27, 2012Applicant: The Regents of the University of CaliforniaInventors: Kenneth N. RAYMOND, Tood M. CORNEILLIE, Jide XU
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Publication number: 20120323000Abstract: The present invention relates generally to olefin metathesis. In some embodiments, the present invention provides methods for Z-selective ring-closing metathesis.Type: ApplicationFiled: June 1, 2012Publication date: December 20, 2012Applicants: TRUSTEES OF BOSTON COLLEGE, MASSACHUSETTS INSTITUTE OF TECHNOLOGYInventors: Amir H. Hoveyda, Miao Yu, Chenbo Wang, Richard R. Schrock
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Publication number: 20120309960Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: ApplicationFiled: February 10, 2011Publication date: December 6, 2012Inventors: Mimi L. Quan, Carl P. Decicco, James R. Corte, Cailan Wang
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Publication number: 20120309961Abstract: The invention relates to diazo 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: ApplicationFiled: July 25, 2012Publication date: December 6, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Yuefeng Peng, Haiying Sun, Qian Cai, Zaneta Nikolovska-Coleska, Jianfeng Lu, Su Qiu
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Publication number: 20120302613Abstract: The invention relates generally to novel antibiotics and their analogs, to processes for the preparation of these novel antibiotics, to pharmaceutical compositions comprising the novel antibiotics; and to methods of using the novel antibiotics to treat or inhibit various disorders.Type: ApplicationFiled: May 24, 2012Publication date: November 29, 2012Applicant: NOVOBIOTIC PHARMACEUTICALS LLCInventors: Aaron PEOPLES, Losee Lucy LING, Kim LEWIS, Slava S. EPSTEIN
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Patent number: 8318764Abstract: The present invention relates to the use of novel macrocyclic compounds of Formula I, wherein the variables Q, Q1, Q2, Q3, and Q4 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.Type: GrantFiled: September 17, 2010Date of Patent: November 27, 2012Assignee: Roche Palo Alto LLCInventors: Alam Jahangir, Stephen M Lynch, Michael Soth, Hanbiao Yang
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Patent number: 8318720Abstract: In part, the present invention is directed to antibacterial compounds.Type: GrantFiled: July 19, 2007Date of Patent: November 27, 2012Assignee: Affinium Pharmaceuticals, Inc.Inventors: Heinz W. Pauls, Jailall Ramnauth, Peter Sampson, Andras Toro
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Publication number: 20120295941Abstract: The present invention relates to an improved method for the synthesis of particular macrocycles that are inhibitors of the proteasomic degradation of p27, in particular argyrin and derivatives thereof.Type: ApplicationFiled: December 14, 2010Publication date: November 22, 2012Inventors: Markus Kalesse, Ulrike Eggert
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Publication number: 20120296085Abstract: Chemiluminescent compounds that can be activated by reaction with chemical or photochemical sources of singlet oxygen are provided. At certain temperatures, such as from approximately 15 to 60° C., the compounds slowly return to their deactivated state by emitting visible and/or infrared light that is observable with various types of light detectors. Suitable conjugates of these compounds, or small particles containing these compounds, may be used for chemiluminescence imaging and sensing technologies. In particular, embodiments provide optical molecular imaging using novel squaraine rotaxane endoperoxides (SREPs) and squaraine catenane endoperoxides (SCEPs), interlocked fluorescent and chemiluminescent dye molecules that have a squaraine chromophore encapsulated inside a macrocycle endoperoxide. The dyes may be stored at low temperature, such as below 0° C., but, upon warming above 15° C.Type: ApplicationFiled: June 1, 2010Publication date: November 22, 2012Applicant: University of Notre Dame du LacInventor: Bradley Smith
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Patent number: 8304385Abstract: The present invention relates to compounds of Formula I, II, III or IV, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. 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 a compound of the present invention.Type: GrantFiled: November 14, 2008Date of Patent: November 6, 2012Assignee: Enanta Pharmaceuticals, Inc.Inventors: Ying Sun, Dong Liu, Yat Sun Or, Zhe Wang
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Publication number: 20120270857Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: June 30, 2010Publication date: October 25, 2012Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter R. Guzzo, David D. Manning, William Earley