Plural Nitrogens In The Hetero Ring Patents (Class 540/460)
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Patent number: 7517882Abstract: Pyrimidine- and triazine-based chemical compounds that are useful, for example, as protein kinase inhibitors for treating cancer, neurological disorders, autoimmune disorders, and other diseases, and methods of using such compounds.Type: GrantFiled: September 17, 2007Date of Patent: April 14, 2009Assignee: Polaris GroupInventors: Shaosong Chu, Zhe Nie, Carin L. Perretta, Philip Eugene Erickson
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Publication number: 20090093533Abstract: Macrocyclic compounds having the structures described herein are useful for inhibiting replication of the hepatitis C virus (HCV). In preferred embodiments, the compounds are active against both the NS3 protease and the NS3 helicase of HCV.Type: ApplicationFiled: October 10, 2006Publication date: April 9, 2009Inventors: Leonid Beigelman, Scott D. Seiwert, Lawrence Blatt, Steven Andrews, Julia Haas
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Patent number: 7507726Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: August 12, 2004Date of Patent: March 24, 2009Assignee: SmithKlineBeecham CorporationInventors: Kelly M. Aubart, Andrew B. Benowitz, Siegfried B. Christensen, IV, Jinhwa Lee, Domingos J. Silva
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Publication number: 20090076115Abstract: The present invention relates to photosensitizer compounds based on functionalized fullerenes useful in targeted photodynamic therapy (PDT), and methods of use thereof.Type: ApplicationFiled: February 28, 2006Publication date: March 19, 2009Applicants: The General Hospital Corporation, Lynntech, Inc.Inventors: Tim Wharton, Hariprasad Gali, Michael R. Hamblin
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Publication number: 20090062311Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers thereof, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1a and R1b are hydrogen, C3-7cycloalkyl, aryl, Het, C1-6alkoxy, C1-6alkyl optionally substituted with halo, C1-6alkoxy, cyano, polyhaloC1-6alkoxy, C3-7cycloalkyl, aryl, or with Het; or R1a and R1b together with the nitrogen to which they are attached form a 4 to 6 membered heterocyclic ring which may be optionally substituted; L is a direct bond, —O—, —O—C1-4alkanediyl-, —O—CO—, —O—C(?O)—NR5a— or —O—C(?O)—NR5a—C1-4alkanediyl-; 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, amino, mono- or diC1-6alkylamino; R4 is aryl or a saturated, a partially unsaturated or completely unsaturated 5 or 6 membered monocyclic or 9 to 12 membered bicyclic heterocyclic ring system wherein said ring system contains one nitrogen, and optiType: ApplicationFiled: January 16, 2008Publication date: March 5, 2009Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Raboisson, Lili Hu, Dominique Louis Surleraux, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Lourdes Salvador Oden
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Publication number: 20090047244Abstract: Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, pharmaceutical compositions comprising such 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: ApplicationFiled: July 25, 2008Publication date: February 19, 2009Applicant: Idenix Pharmaceuticals, Inc.Inventors: Christophe Claude Parsy, Dominique Surleraux, Francois-Rene Alexandre, Michel Derock, Frederic Leroy
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Publication number: 20090047248Abstract: The present invention relates to compounds of Formula I or II, 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 to the subject a pharmaceutical composition comprising a compound of the present invention.Type: ApplicationFiled: August 8, 2007Publication date: February 19, 2009Inventors: Ying Sun, Deqiang Niu, Yat Sun Or, Zhe Wang
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Publication number: 20090048297Abstract: The invention provides 4-amino-4-oxobutanoyl peptide compounds of Formula I and the pharmaceutically salts and hydrates thereof. The variables R1-R9, R16, R18, R19, n, M, n, M, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. Certain 4-amino-4-oxobutanoyl peptide compounds disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptide compounds and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain 4-amino-4-oxobutanoyl peptide compound as the only active agent or may contain a combination of 4-amino-4-oxobutanoyl peptide containing peptides compound and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in mammals.Type: ApplicationFiled: July 13, 2007Publication date: February 19, 2009Applicant: ACHILLION PHARMACEUTICALSInventors: Avinash Phadke, Xiangzhu Wang, Suoming Zhang, Atul Agarwal
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Publication number: 20090047252Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: June 26, 2008Publication date: February 19, 2009Applicant: Gilead Sciences, Inc.Inventors: Zhenhong R. Cai, Aesop Cho, Choung U. Kim, Jie Xu
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Publication number: 20090041721Abstract: The present invention discloses compounds of Formula I or II, 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 to the subject a pharmaceutical composition comprising a compound of the present invention.Type: ApplicationFiled: August 9, 2007Publication date: February 12, 2009Inventors: Deqiang Niu, Yonghua Gai, Yat Sun Or, Zhe Wang
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Publication number: 20090035271Abstract: 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: ApplicationFiled: August 1, 2007Publication date: February 5, 2009Inventors: Ying Sun, Dong Liu, Yat Sun Or, Zhe Wang
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Publication number: 20080306040Abstract: The invention relates to antibacterial amide macrocycles and methods for their preparation, their use for the treatment and/or prophylaxis of diseases as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially bacterial infections.Type: ApplicationFiled: January 11, 2008Publication date: December 11, 2008Inventors: Rainer Endermann, Kerstin Ehlert, Martin Michels, Stefan Weigand, Guido Schiffer
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Publication number: 20080300231Abstract: The invention relates to antibacterial amide macrocycles and methods for their preparation, their use for the treatment and/or prophylaxis of diseases, as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, in particular of bacterial infections.Type: ApplicationFiled: September 26, 2007Publication date: December 4, 2008Inventors: Rainer Endermann, Kerstin Ehlert, Siegfried Raddatz, Martin Michels, Yolanda Cancho-Grande, Stefan Weigand, Karin Fischer
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Publication number: 20080286233Abstract: The present invention relates to compounds of Formula I, 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: ApplicationFiled: April 24, 2008Publication date: November 20, 2008Inventors: Ying Sun, Yat Sun Or, Zhe Wang
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Publication number: 20080279821Abstract: The present invention relates to compounds of Formula I, 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: ApplicationFiled: April 24, 2008Publication date: November 13, 2008Inventors: Deqiang Niu, Yat Sun Or, Zhe Wang
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Publication number: 20080280945Abstract: Crystalline forms of a hexahydro-diazocinonaphthyridine trione compound are disclosed. The compound and its crystalline forms thereof are HIV integrase inhibitors useful for the prophylaxis or treatment of HIV infection or for the prophylaxis, treatment or delay in the onset or progression of AIDS.Type: ApplicationFiled: May 8, 2008Publication date: November 13, 2008Inventors: Sachin Lohani, Zhihui Peng, Arlene E. McKeown
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Publication number: 20080274080Abstract: The present invention relates to compounds of Formula I, 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: ApplicationFiled: April 24, 2008Publication date: November 6, 2008Inventors: Yat Sun Or, Deqiang Niu, Zhe Wang
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Patent number: 7446102Abstract: The invention relates to antibacterial amide macrocycles and processes for their preparation, their use for the treatment and/or prophylaxis of diseases and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially bacterial infections.Type: GrantFiled: March 23, 2007Date of Patent: November 4, 2008Assignee: AiCuris GmbH & Co. KGInventors: Rainer Endermann, Kerstin Ehlert, Christoph Freiberg, Siegfried Raddatz, Martin Michels, Yolanda Cancho-Grande, Joachim Schuhmacher, Stefan Weigand
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Patent number: 7442558Abstract: The present invention provides luminescent lanthanide metal chelates comprising a metal ion of the lanthanide series and a complexing agent comprising at least one phthalamidyl moiety. Also provided are probes incorporating the phthalamidyl ligands of the invention and methods utilizing the ligands of the invention and probes comprising the ligands of the invention.Type: GrantFiled: June 14, 2004Date of Patent: October 28, 2008Assignee: The Regents of the University of CaliforniaInventors: Kenneth N. Raymond, Stephane Petoud, Seth Cohen, Jide Xu
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Publication number: 20080260676Abstract: Provided are hydroxycucurbituril derivatives, their preparation methods and uses. The hydroxycucurbituril derivative is easy to further functionalize with enhanced solubility in common solvents, thereby providing wider applications.Type: ApplicationFiled: June 13, 2008Publication date: October 23, 2008Applicant: POSTECH FOUNDATIONInventors: Kimoon KIM, Sang Yong JON, Narayanan SELVAPALAM, Dong Hyun OH
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Patent number: 7432371Abstract: 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: February 7, 2003Date of Patent: October 7, 2008Assignee: 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: 7432088Abstract: A process of the large-scale fermentation of a highly productive ansamitocin-producing strains. A method for isolating crude ansamitocins. A method for purifying ansamitocins.Type: GrantFiled: January 19, 2005Date of Patent: October 7, 2008Assignee: Immunogen Inc.Inventors: Cynthia Kuo, Graham S. Byng, Wayne C. Widdison
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Patent number: 7429565Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: April 26, 2004Date of Patent: September 30, 2008Assignee: Gilead Sciences, Inc.Inventors: Constantine G. Boojamra, Carina Cannizzaro, James M. Chen, Xiaowu Chen, Aesop Cho, Lee S. Chong, Maria Fardis, Haolun Jin, Ralph F. Hirschmann, Alan X. Huang, Choung U. Kim, Thorsten Kirschberg, Christopher P. Lee, William A. Lee, Richard L. Mackman, David Y. Markevitch, David A. Oare, Vidya K. Prasad, Hyung-Jung Pyun, Adrian S. Ray, Rosemarie Sherlock, Sundaramoorthi Swaminathan, William J. Watkins, Jennifer R. Zhang
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Publication number: 20080213917Abstract: 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: August 15, 2007Publication date: September 4, 2008Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Kenneth N. Raymond, Todd M. Corneillie, Jide Xu
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Publication number: 20080213780Abstract: 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: January 25, 2008Publication date: September 4, 2008Applicant: Lumiphore, Inc.Inventors: Nathaniel G. Butlin, Todd M. Corneillie, Jide Xu
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Publication number: 20080200503Abstract: Inhibitors of HCV of formula (I). and the N-oxides, salts, and stereoisomers thereof, wherein the dashed line represents an optional double bond between atoms C7 and C8; R1 is hydrogen or C1-6alkyl; R2 is hydrogen or C1-6alkyl; and n is 3, 4, 5, or 6; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I) are provided. Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.Type: ApplicationFiled: July 27, 2006Publication date: August 21, 2008Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Mats Stefan Lindstrom, Pia Cecilia Kahnberg, Dmitry Antonov, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist
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Publication number: 20080182834Abstract: The invention provides multi-nuclear metal complexes partially encapsulated by one or more cucurbit[7 to 12]urils or analogues thereof. The invention further relates to methods for treating cancer by administering a multi-nuclear metal complex having anti-tumour activity partially encapsulated by one or more cucurbit[7 to 12]urils or analogues thereof.Type: ApplicationFiled: January 14, 2005Publication date: July 31, 2008Applicant: NEWSOUTH INNOVATIONS PTY LIMITEDInventors: Nial Joseph Wheate, Anthony I. Day, Rodney J. Blanch, John G. Collins
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Patent number: 7404912Abstract: The present invention provides luminescent lanthanide metal chelates comprising a metal ion of the lanthanide series and a complexing agent comprising at least one salicylamidyl moiety. Also provided are probes incorporating the salicylamidyl ligands of the invention and methods utilizing the ligands of the invention and probes comprising the ligands of the invention.Type: GrantFiled: February 6, 2006Date of Patent: July 29, 2008Assignee: The Regents of the University of CaliforniaInventors: Kenneth N. Raymond, Stephane Petoud, Seth Cohen, Jide Xu
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Publication number: 20080167302Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: ApplicationFiled: August 12, 2004Publication date: July 10, 2008Inventors: Kelly M. Aubart, Andrew B. Benowitz, Siegfried B. Christensen IV, Jinhwa Lee, Domingos J. Silva
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Publication number: 20080161554Abstract: Disclosed are a macrocyclic carbodiimide (MC-CDI) and a process for synthesizing the same through condensation of a molecule with multiple-isocyanate terminal functional groups under high dilution in the presence of a phospholene catalyst such as phospholene or arsenic catalyst. Also disclosed are MC-CDI derivatives, such as MC-urea (MC-U), MC-acylurea (MC-ACU), acid functionalized MC-ACU, and anhydride functionalized MC-ACU, processes for synthesizing the same, and the applications of such derivatives as hydrolysis stabilizers in organic polymeric materials, such as polyurethane (PU) and polyesters, as well as the applications in the syntheses of the amide- and imide-modified polyurethane by ring-opening reaction of the MC-ACU.Type: ApplicationFiled: December 28, 2006Publication date: July 3, 2008Applicant: GREAT EASTERN RESINS INDUSTRIAL CO., LTD.Inventors: Shenghong A. Dai, Chih-Chia Cheng, Chien-Wen Chen, Chih-Hung Chen
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Publication number: 20080159982Abstract: Macrocyclic peptides having the general formula: are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.Type: ApplicationFiled: November 14, 2007Publication date: July 3, 2008Inventors: Alan Xiangdong Wang, Barbara Zhizhen Zheng, Stanley D'Andrea, Nicholas A. Meanwell, Paul Michael Scola
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Publication number: 20080145334Abstract: Macrocyclic peptides having the general formula: are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.Type: ApplicationFiled: November 14, 2007Publication date: June 19, 2008Inventors: Alan Xiangdong Wang, Barbara Zhizhen Zheng, Stanley D'Andrea, Nicholas A. Meanwell, Paul Michael Scola
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Publication number: 20080132469Abstract: Disclosed are compounds represented by the formula: or a pharmaceutically acceptable salt or isomer thereof, wherein R1-R6 are as defined in the specification. These compounds are targeted for use as inhibitors of SH2 domain binding with a phosphoprotein, and are contemplated for use in a number of diseases including cancer. Also disclosed are pharmaceutical compositions comprising a compound of the invention and a pharmaceutically acceptable carrier.Type: ApplicationFiled: October 31, 2007Publication date: June 5, 2008Applicant: GOVERNMENT OF THE UNITED STATES, REPRESENTED BY THE SECRETARY, DEPARTMENTInventors: Terrence R. BURKE, Zhen-Dan SHI, Sang-Uk KANG
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Publication number: 20080132477Abstract: The invention relates to novel macrocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16 or 17, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.Type: ApplicationFiled: January 13, 2006Publication date: June 5, 2008Inventors: Claudia Betschart, Andreas Lerchner, Rainer Machauer, Heinrich Rueger, Marina Tintelnot-Blomley, Siem Jacob Veenstra
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Patent number: 7378411Abstract: The present invention relates to thienopyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: December 2, 2002Date of Patent: May 27, 2008Assignee: Merck & Co., Inc.Inventors: Mark E. Fraley, George D. Hartman, William F. Hoffman
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Patent number: 7358239Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q isType: GrantFiled: March 14, 2005Date of Patent: April 15, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
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Patent number: 7354922Abstract: A compound having the general structure shown in Formula (I): or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.Type: GrantFiled: December 1, 2005Date of Patent: April 8, 2008Assignee: Schering CorporationInventors: Dong Xiao, Anandan Palani, Cheng Wang, Hon-Chung Tsui, Xianhai Huang, Sapna S. Shah, Ashwin U. Rao, Xiao Chen, Sunil Paliwal, Neng-Yang Shih
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Publication number: 20080039470Abstract: The present invention discloses compounds of formulae I and II, 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: ApplicationFiled: August 11, 2006Publication date: February 14, 2008Inventors: Deqiang Niu, Joel D. Moore, Dong Liu, Yonghua Gai, Zhigang Chen, Yat Sun Or, Zhe Wang
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Patent number: 7312225Abstract: Macrocyclic pyrimidine derivatives of general formula I in which R1 to R5, X, Y, A, B, m and n have the meanings that are contained in the description, as inhibitors of the cyclin-dependent kinase, their processes for production as well as their use as medications for treating various diseases are described.Type: GrantFiled: August 20, 2003Date of Patent: December 25, 2007Assignee: Bayer Schering Pharma AGInventors: Ulrich Luecking, Gerhard Siemeister, Martina Schaefer, Hans Briem
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Publication number: 20070281884Abstract: 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: ApplicationFiled: August 11, 2006Publication date: December 6, 2007Inventors: Ying Sun, Deqiang Niu, Guoyou Xu, Yat Sun Or, Zhe Wang
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Patent number: 7279582Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: GrantFiled: October 25, 2002Date of Patent: October 9, 2007Assignee: Abbott LaboratoriesInventors: Eric J. Stoner, Arthur J. Cooper, Lawrence Kolaczkowski, Ketan M. Patel, Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Daniel A. Dickman, Patricia A. Oliver, Jien-Heh J. Tien
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Patent number: 7268211Abstract: A process for removing ruthenium or ruthenium-containing compounds from a reaction mixture comprising a compound of the following formula I in an organic solvent using supercritical fluid processing techniques: wherein RA, R3, R4, D and A are as defined herein. This invention has particular application for removing ruthenium-containing catalyst and ruthenium-containing catalyst by products from reaction mixtures that result from ring-closing olefin metathesis (RCM) reactions.Type: GrantFiled: December 7, 2004Date of Patent: September 11, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Fabrice Gallou, Said Saim, Nathan K. Yee
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Patent number: 7262186Abstract: The present invention relates to azolopyriniidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: December 2, 2002Date of Patent: August 28, 2007Assignee: Merck & Co., Inc.Inventors: Mark E. Fraley, George D. Hartman, William F. Hoffman
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Patent number: 7262187Abstract: The present invention relates to azolopyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: December 2, 2002Date of Patent: August 28, 2007Assignee: Merck & Co., Inc.Inventors: Mark E. Fraley, George D. Hartman, William F. Hoffman
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Patent number: 7253160Abstract: The present invention discloses novel depeptidized compounds which have HCV protease inhibitory activity as well as pharmaceutical compositions comprising such compounds and methods of using them to treat disorders associated with the HCV protease.Type: GrantFiled: November 19, 2004Date of Patent: August 7, 2007Assignee: Schering CorporationInventors: F. George Njoroge, Srikanth Venkatraman, Viyyoor M. Girijavallabhan
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Patent number: 7244723Abstract: The present invention relates to furanopyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: December 2, 2002Date of Patent: July 17, 2007Assignee: Merck & Co., Inc.Inventors: Mark E. Fraley, George D. Hartman
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Patent number: 7230021Abstract: The present invention provides a compound of Formula I, all of its related stereoisomers, and their pharmaceutically acceptable salts, wherein A—B, K, Q, X, Y, Z, R and R1 are as defined in Claim 1.Type: GrantFiled: March 13, 2003Date of Patent: June 12, 2007Assignee: The Texas A&M University SystemInventors: Daniel Romo, Jun Liu, Nam Song Choi, Zonggao Shi
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Patent number: 7211572Abstract: The present invention relates to a nitrogen-containing fused ring compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, and an anti-HIV agent containing such compound. The compound of the present invention has an HIV integrase inhibitory activity, and is useful as an agent for the prophylaxis or treatment of AIDS, or as an anti-HIV agent. In addition, by the combined use with other anti-HIV agents such as a protease inhibitor, a reverse transcriptase inhibitor and the like, it can be a more effective anti-HIV agent. Because it shows integrase-specific high inhibitory activity, the compound can be a pharmaceutical agent safe on human body, which causes only a fewer side effects.Type: GrantFiled: October 13, 2005Date of Patent: May 1, 2007Assignee: Japan Tobacco Inc.Inventors: Susumu Miyazaki, Susumu Katoh, Kaoru Adachi, Hirotaka Isoshima, Satoru Kobayashi, Yuji Matsuzaki, Wataru Watanabe, Kazunobu Yamataka, Shinichi Kiyonari, Shuichi Wamaki
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Patent number: 7208595Abstract: A macrocyclic peptide deformylase (PDF) inhibitor comprising a peptide or peptide mimetic having three residues, P1?, P2?, and P3?, wherein P2? connects P1? and P3?, wherein P1? and P3? each have a side chain, and wherein the side chains on P1? and P3? are crosslinked to form the macrocyclic PDF inhibitor. The side chains of P1? and P3? interact with the PDF active site, and preferably, P2? has a side chain that interacts with a solvent. Also provided are methods of inhibiting the growth of a bacterium, the methods comprising contacting the bacterium with an anti-bacterial effective amount of the inventive macrocyclic PDF inhibitor. Additionally, a method of treating a bacterial infection in a subject comprising administering an effective amount of a macrocyclic PDF inhibitor to a subject in need of treatment.Type: GrantFiled: July 26, 2004Date of Patent: April 24, 2007Assignee: The Ohio State University Research FoundationInventor: Dehua Pei
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Patent number: 7192750Abstract: A microorganism that is a mutant bacterial strain of the species Actinosynnema pretiosum, designated PF4-4, (ATCC PTA-3921), being capable of producing maytansinoid ansamitocins such as ansamitocin P-3 in improved yield compared to previous known strains, and capable of growth under varied culture conditions, and methods of producing maytansinoid ansamitocins by culturing PF4-4 in a suitable growth medium.Type: GrantFiled: July 26, 2004Date of Patent: March 20, 2007Assignees: Immunogen Inc., Genentech, Inc.Inventors: Johnson Chung, Graham S. Byng