Plural Nitrogens In The Hetero Ring Patents (Class 540/460)
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Publication number: 20120264794Abstract: 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: June 7, 2012Publication date: October 18, 2012Applicants: DANA-FARBER CANCER INSTITUTE, INC., COLORADO STATE UNIVERSITY RESEARCH FOUNDATIONInventors: Robert M. Williams, James E. Bradner, Albert Bowers, Tenaya Newkirk, Ann E. Youngman
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Publication number: 20120264802Abstract: The present invention relates to photosensitizer compounds based on functionalized fullerenes useful in targeted photodynamic therapy (PDT), and methods of use thereof.Type: ApplicationFiled: May 31, 2012Publication date: October 18, 2012Applicants: Lynntech, Inc., The General Hospital CorporationInventors: Tim Wharton, Hariprasad Gali, Michael R. Hamblin
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Publication number: 20120263675Abstract: The invention relates to diazo bicyclic Smac mimetics that are tethered through a covalent linker to give a bivalent species. Bivalent diazo bicyclic Smac mimetics function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs). The invention also relates to the use of bivalent diazo bicyclic Smac mimetics for inducing or sensitizing cells to the induction of apoptotic cell death. Thus, compounds of the invention are useful in the treatment, amelioration, or prevention of hyperproliferative diseases such as cancer.Type: ApplicationFiled: October 20, 2010Publication date: October 18, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Haiying Sun
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Patent number: 8278293Abstract: 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: April 14, 2008Date of Patent: October 2, 2012Assignee: 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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Patent number: 8278322Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.Type: GrantFiled: July 28, 2006Date of Patent: October 2, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: M. Katharine Holloway, Nigel J. Liverton, John A. McCauley, Michael T. Rudd, Joseph P. Vacca, Steven W. Ludmerer, David B. Olsen
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Patent number: 8273875Abstract: Embodiments relate to the field of chemistry and biochemistry, and, more specifically, to novel near-infrared dyes that are photostable and resistant to quenching. The dyes belong to a novel family of squaraine rotaxanes, and they are particularly well-suited for use in biological applications. Also disclosed are methods of synthesizing the dyes and methods of using the dyes.Type: GrantFiled: November 16, 2009Date of Patent: September 25, 2012Assignees: University of Notre Dame du Lac, Molecular Targeting Technologies, Inc.Inventors: Bradley Smith, Arunkumar Easwaran
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Publication number: 20120238746Abstract: The present invention relates to synthesis procedures and intermediates of a compound of formula: and the salts thereof.Type: ApplicationFiled: May 31, 2012Publication date: September 20, 2012Inventors: Andras Horvath, Dominique Paul Michel Depré, Dominic John Ormerod
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Publication number: 20120238745Abstract: 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: January 9, 2012Publication date: September 20, 2012Applicant: AnaSpec IncorporatedInventors: Zhenjun Diwu, Jianheng Zhang, Yi Tang, Xiang Guobing
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Publication number: 20120238595Abstract: The invention provides compounds of formula (I) wherein u, d, v, m, n, R1, W, X, Y, and Z have any values defined herein, as well as salts thereof. The compounds have activity as anti-proliferative agents.Type: ApplicationFiled: November 5, 2010Publication date: September 20, 2012Applicants: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEY, RUTGERS, THE STATE UNIVERSITY OF NEW JERSEYInventors: Edmond J. LaVoie, Joseph E. Rice, Suzanne G. Rzuczek, Daniel S. Pilch
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Publication number: 20120225892Abstract: The present invention relates to compounds of formula (I) compositions, in particular pharmaceutical compositions, and medicaments comprising at least one compound of formula (I). The invention also relates to the use of such a compound for manufacturing a medicament. In particular the medicament and the pharmaceutical composition are intended to treat diseases linked with insulin regulation problems, such as diabetes. This invention aims also to methods for treating or preventing such diseases.Type: ApplicationFiled: November 16, 2010Publication date: September 6, 2012Applicant: MELLITECHInventors: Didier Roche, Fabrice Chimienti, Martin Ohsten
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Patent number: 8258292Abstract: 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: GrantFiled: October 6, 2008Date of Patent: September 4, 2012Assignee: AnaSpec IncorporatedInventors: Zhenjun Diwu, Jianheng Zhang, Yi Tang, Xiang Guobing
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Publication number: 20120214253Abstract: 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 comprise hydroxypyridinonyl 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.Type: ApplicationFiled: August 24, 2010Publication date: August 23, 2012Applicant: LUMIPHORE, INC.Inventors: Nathaniel G. Butlin, Kenneth N. Raymond, Jide Xu, Anthony D'Aleo
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Publication number: 20120207703Abstract: Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, and pharmaceutical compositions and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.Type: ApplicationFiled: February 9, 2012Publication date: August 16, 2012Applicant: IDENIX PHARMACEUTICALS, INC.Inventors: Christophe Claude PARSY, Francois-Rene ALEXANDRE, Thierry CONVARD, Dominique SURLERAUX
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Publication number: 20120202859Abstract: 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: ApplicationFiled: April 20, 2012Publication date: August 9, 2012Inventors: 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: 8236807Abstract: The present invention relates to compounds of Formula I or II, or a pharmaceutically acceptable salt, ester, or prodrug, 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 the compounds of the present invention.Type: GrantFiled: July 20, 2009Date of Patent: August 7, 2012Assignee: Enanta Pharmaceuticals, Inc.Inventors: Suanne Nakajima, Zhenwei Miao, Ying Sun, Datong Tang, Guoyou Xu, Brian Porter, Yat Sun Or, Zhe Wang
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Patent number: 8222257Abstract: Compounds and compositions are provided for treatment, prevention, or amelioration of a variety of medical disorders associated with viral infections and/or cell proliferation. The compounds provided herein are 5-phosphono-pent-2-en-1-yl nucleosides and esters thereof.Type: GrantFiled: March 30, 2006Date of Patent: July 17, 2012Assignee: The Regents of the University of CaliforniaInventors: Karl Y. Hostetler, James R. Beadle, Hyunah Choo
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Publication number: 20120171157Abstract: 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: ApplicationFiled: March 6, 2012Publication date: July 5, 2012Inventors: 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 Bertril Samuelsson, Asa Annica Kristina Rosenquist, Vladimir Ivanov, Michael Pelcman, Anna Karin Gertrud Linnea Belfrage, Per-Ola Mikael Johansson, Sandrine Marie Helene Vendeville
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Publication number: 20120172367Abstract: 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: ApplicationFiled: October 13, 2010Publication date: July 5, 2012Applicant: ELANCO ANIMAL HEALTH IRELAND LIMITEDInventors: Johannes Wilhelmus J Thuring, Jean-Francois Bonfanti, Jerome Michel Claude Fortin
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Patent number: 8211891Abstract: The present invention discloses compounds of formula I 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 the compounds of the present invention.Type: GrantFiled: April 30, 2009Date of Patent: July 3, 2012Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yonghua Gai, Dong Liu, Joel D. Moore, Yat Sun Or, Zhe Wang
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Publication number: 20120149895Abstract: The present invention discloses a process for dimethylation of active methylene groups. Specifically, the invention discloses a process for preparing 3-amino-2,2-dimethylpropanamide. Compounds produced by the present dimethylation process such as 3-amino-2,2-dimethylpropanamide can be used as intermediates in the route of synthesis of therapeutic, prophylactic or diagnostic agent, for example aliskiren or cryptophycin. Particularly, the invention relates to embodiments further extending to processes for preparing pharmaceutical dosage form comprising said therapeutic, prophylactic or diagnostic agents. More specifically, the invention relates to the use of compounds produced by the present dimethylation process for the manufacture of therapeutic, prophylactic or diagnostic agents or for the manufacture of pharmaceutical dosage forms comprising said therapeutic, prophylactic or diagnostic agents.Type: ApplicationFiled: March 30, 2010Publication date: June 14, 2012Applicant: LEK PHARMACEUTICALS D.D.Inventors: Branko Jenko, Anton Copar
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Publication number: 20120142912Abstract: Disclosed is a novel family of macrocyclic compounds, coined calixurenes, which comprises linear and cyclic oligomers composed of alternating moieties of an aromatic unit and a ureatic unit, linked to one another via a bridging moiety. The disclosed calixurenes feature multiple heteroatom-containing groups, and can be designed so as to feature other functionalities, and can thus be used in a variety of applications. Further disclosed are processes of preparing the calixurenes, articles containing same and uses thereof.Type: ApplicationFiled: August 12, 2010Publication date: June 7, 2012Applicant: Technion Research & Development Foundation Ltd.Inventors: Ehud Keinan, Galit Parvari, Doron Pappo
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Patent number: 8193346Abstract: The present invention relates to a process for the preparation of macrocyclic compounds that are useful as hepatitis C virus (HCV) protease inhibitor compounds.Type: GrantFiled: December 4, 2008Date of Patent: June 5, 2012Assignee: Enanta Pharmaceuticals, Inc.Inventors: Seble Wagaw, Matthew Ravn, Kenneth Engstrom, Guoyou Xu, Zhe Wang, Ying Sun, Deqiang Niu, Yat Sun Or
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Patent number: 8178520Abstract: The present invention relates to macrocyclic compounds of formula (I): wherein W, n, R1, Ra, Rb, R3, R4, M, Z, ring A and ring B are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.Type: GrantFiled: May 11, 2007Date of Patent: May 15, 2012Assignee: Istituto di Ricerche di Biologia Molecolare P. Angeletti SpAInventors: Maria Emilia Di Francesco, Emanuela Nizi, Paola Pace, Vincenzo Summa
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Patent number: 8173800Abstract: 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: August 15, 2007Date of Patent: May 8, 2012Assignee: The Regents of the University of CaliforniaInventors: Kenneth N. Raymond, Todd M. Corneillie, Jide Xu
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Publication number: 20120108562Abstract: PAD4 inhibitory compositions and methods for their use in treatment of cancer and autoimmune disease are provided according to embodiments of the present invention.Type: ApplicationFiled: November 1, 2011Publication date: May 3, 2012Applicant: The Penn State Research FoundationInventors: Gong Chen, Yanming Wang, Pingxin Li, Jing Hu, Shu Wang, Yuji Wang
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Patent number: 8163752Abstract: Compounds of formula I: wherein variables A1, A2, B, m, n, J, R4, G1, G2, G3 and Y are as described herein, which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: June 3, 2008Date of Patent: April 24, 2012Assignee: Merck, Sharp & Dohme Corp.Inventors: Ian Bell, Craig A. Stump
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Publication number: 20120093766Abstract: 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 13, 2011Publication date: April 19, 2012Inventors: Tao Wang, Annapurna Pendri, Zhongxing Zhang, Weixu Zhai, Guo Li, Samuel Gerritz, Paul Michael Scola, Li-Qiang Sun, Qian Zhao, Eric Mull
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Publication number: 20120093767Abstract: 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 14, 2011Publication date: April 19, 2012Inventors: Tao Wang, Zhiwei Yin, Zhongxing Zhang, Annapurna Pendri, Guo Li, Samuel Gerritz, Weixu Zhai, Paul Michael Scola, Li-Qiang Sun, Eric Mull
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Publication number: 20120095211Abstract: The embodiments provide compounds of the general Formulae I, Ia, II, IIa, III, IIIa, IIIb, IV, IVa, IVb, V, Va, Vb, VI, VIa, VIb, and VIc, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition. The embodiments also provide methods for the synthesis of subject compounds and intermediates in the synthetic methods.Type: ApplicationFiled: September 20, 2011Publication date: April 19, 2012Applicant: InterMune, Inc.Inventors: Brad Buckman, John B. Nicholas, Vladimir Serebryany, Scott D. Seiwert
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Patent number: 8148399Abstract: 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, 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 nitrogen, oxygen and sulfurType: GrantFiled: July 28, 2006Date of Patent: April 3, 2012Assignees: Tibotec Pharmaceuticals Ltd., Medivar ABInventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Åsa Annica Kristina Rosenquist
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Publication number: 20120071527Abstract: 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: ApplicationFiled: November 30, 2011Publication date: March 22, 2012Applicants: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEY, RUTGERS, THE STATE UNIVERSITY OF NEW JERSEYInventors: Edmond J. Lavoie, Joseph E. Rice, Leroy F. Liu
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Publication number: 20120065366Abstract: Macrocyclization of amino acids or linear peptides upon reaction with amphoteric amino aldehydes and isocyanides is provided.Type: ApplicationFiled: March 16, 2010Publication date: March 15, 2012Applicant: THE GOVERNING COUNCIL OF THE UNIVERSITY OF TORONTOInventors: Andrei Yudin, Ryan Hili
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Publication number: 20120041191Abstract: 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 2, 2010Publication date: February 16, 2012Applicant: Idenix Pharmaceuticals, Inc.Inventors: Christophe Claude Parsy, Francois-Rene Alexandre, Florence Marie-Emilie Bonnaterre, Dominique Surleraux
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Publication number: 20120041192Abstract: The present invention relates to novel macrocyclic derivatives of glycolurils of general formula I, and methods of their preparation. These novel derivatives can be used for the selective removing of various compounds from solutions in polar and nonpolar solvents, and from water, e.g. for water purification and desalination, also for separation of liquid mixtures and mixtures of gases and organic solvent vapors, preparation of ion-exchange materials and materials which are used as stationary phase in chromatography, construction of sensors, transport and targeting of drugs in organisms, and also preparation of materials bearing aromatic or curative compounds.Type: ApplicationFiled: October 26, 2010Publication date: February 16, 2012Inventors: Vladimir Sindelar, Jan Svec, Vaclav Havel
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Publication number: 20120041190Abstract: 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: February 16, 2012Inventors: James R. Corte, Tianan Fang, Carl P. Decicco, Donald J.P. Pinto, Karen A. Rossi, Zilun Hu, Yoon Jeon, Mimi L. Quan, Joanne M. Smallheer, Yufeng Wang, Wu Yang
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Patent number: 8110679Abstract: Nanofilms useful for filtration are prepared from oriented amphiphilic molecules and oriented macrocyclic modules. The amphiphilic species may be oriented on an interface or surface. The nanofilm may be prepared by depositing or attaching an oriented layer to a substrate. A nanofilm may also be prepared by coupling the oriented macrocyclic modules to provide a membrane.Type: GrantFiled: July 31, 2008Date of Patent: February 7, 2012Assignee: Covalent Partners LLCInventors: Joshua W. Kriesel, Timothy B. Karpishin, Donald B. Bivin, Grant Merrill, Martin S. Edelstein, Thomas H. Smith, Jeffery A. Whiteford, Robert T. Jonas, Mark Micklatcher, Serena Joshi
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Patent number: 8105829Abstract: 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: GrantFiled: October 21, 2010Date of Patent: January 31, 2012Assignee: AnaSpec IncorporatedInventors: Zhenjun Diwu, Jianheng Zhang, Yi Tang, Xiang Guobing
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Patent number: 8106187Abstract: The present invention relates to a new process for the preparation of macrocyclic HCV protease inhibitor compounds of the formula wherein R1 is an amino protecting group and X is halogen by way of a ring closing metathesis approach.Type: GrantFiled: August 7, 2009Date of Patent: January 31, 2012Assignee: Roche Palo Alto LLCInventors: Michelangelo Scalone, Helmut Stahr
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Patent number: 8093235Abstract: 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: October 24, 2008Date of Patent: January 10, 2012Assignees: Rutgers, The State University of New Jersey, University of Medicine and Dentistry of New JerseyInventors: Edmond J. Lavoie, Joseph E. Rice, Leroy F. Liu
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Patent number: 8093379Abstract: Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.Type: GrantFiled: September 18, 2009Date of Patent: January 10, 2012Assignee: Idenix Pharmaceuticals, Inc.Inventors: Adel Moussa, Benjamin Alexander Mayes, Elodie Rosinovsky, Alistair Stewart
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Publication number: 20110294801Abstract: Macrocyclic derivative compounds that inhibit protein kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed kinase activity such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases.Type: ApplicationFiled: September 3, 2009Publication date: December 1, 2011Applicant: MERCK PATENT GMBHInventors: Henry Yu, Lizbeth Celeste De Selm, Xuliang Jiang, Benny C. Askew, Jr., Srinivasa R. Karra, Andreas Goutopoulos
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Publication number: 20110294827Abstract: IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPs (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a Kd of less that 0.1 micromolar. Methods of using these IAP binding molecules for therapeutic, diagnostic, and assay purposes are also disclosed.Type: ApplicationFiled: June 3, 2011Publication date: December 1, 2011Applicant: TETRALOGIC PHARMACEUTICALS CORPORATIONInventors: Stephen M. Condon, Matthew G. LaPorte, Yijun Deng, Susan R. Rippin
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Publication number: 20110294778Abstract: Compounds of Formula (I) wherein R1, R2, R3, R4 and R5 are defined herein, maintain good activity against NS3 proteases containing clinically relevant genotype 1a R155K and genotype 1b D168V resistance mutations. The compounds are useful as inhibitors of HCV NS3 protease for the treatment of hepatitis C viral infection.Type: ApplicationFiled: November 23, 2010Publication date: December 1, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Montse LLINAS-BRUNET, Josée BORDELEAU, Cédrickx GODBOUT, Mélissa LEBLANC, Benoît MOREAU, Jeffrey O'MEARA
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Publication number: 20110275621Abstract: Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: May 13, 2011Publication date: November 10, 2011Inventors: Joseph P. Vacca, John S. Wai, Linda S. Payne
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Patent number: 8048862Abstract: The embodiments provide compounds of the general Formulae I, II, III, IV, V, VI, VII, and X, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: GrantFiled: April 14, 2009Date of Patent: November 1, 2011Assignee: InterMune, Inc.Inventors: Scott D. Seiwert, Leonid Beigelman, Brad Buckman, Antitsa Dimitrova Stoycheva, Steven B. Porter, Williamson Ziegler Bradford, Vladimir Serebryany
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Publication number: 20110263844Abstract: The present invention is directed to a method for the preparation of macrocyclic compounds of formula (I), comprising the step of cyclizing a diene of formula (II), in the presence of a catalyst, wherein R1-R6, A, W and V are as defined herein. The present invention is also directed to intermediate compounds of formula II.Type: ApplicationFiled: May 5, 2009Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Chutian Shu, Chris Hugh Senanayake, Zhulin Tan, Nathan Yee, Xingzhong Zeng
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Publication number: 20110257145Abstract: A method of treating neurological diseases, like Alzheimer's Disease by administering a compound that activates protein kinase C and inhibits histone deacetylases to an individual suffering from the neurological disease. The method utilizes benzolactam compounds that reduce A? production and blocks oxidative stress in the treatment of Alzheimer's disease. The benzolactam compounds and compositions containing the benzolactam compounds also are disclosed.Type: ApplicationFiled: August 5, 2009Publication date: October 20, 2011Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISInventors: Alan Kozikowski, Yihua Chen
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Patent number: 8039455Abstract: The invention relates to novel macrocyclic compounds of the formula in which all of the variables are as defined in the specification, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.Type: GrantFiled: December 28, 2006Date of Patent: October 18, 2011Assignee: Novartis AGInventors: Claudia Betschart, Manuel Koller, Kurt Laumen, Andreas Lerchner, Rainer Machauer, Clive McCarthy, Marina Tintelnot-Blomley, Siem Jacob Veenstra
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Patent number: 8034927Abstract: 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: GrantFiled: August 20, 2009Date of Patent: October 11, 2011Assignee: AnaSpec IncorporatedInventors: Zhenjun Diwu, Jianheng Zhang, Yi Tang, Xiang Guobing
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Patent number: 8012939Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers thereof, wherein each variable has specific definitions. Pharmaceutical compositions containing compounds (I) and process for preparing compounds (I) are also provided. Bioavailable combinations of the inhibitors of HCV of Formula (I) with ritonavir are also provided.Type: GrantFiled: July 28, 2006Date of Patent: September 6, 2011Assignees: Tibotec Pharmaceuticals Ltd. Co, Medivir ABInventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Sandrine Marie Helene Vendeville, Lili Hu, Abdellah Tahri, Dominique Louis Nestor Ghislain Surleraux, Wim Van De Vreken, Ismet Dorange, Yvan Simonnet, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Hans Kristian Wallberg