Patents Assigned to Achillion Pharmaceuticals, Inc.
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Patent number: 8088806Abstract: The present invention provides compounds, salts and hydrates of Formula I, wherein the variables Ar1, R2, R3, R4, r, q, and t are defined herein. Certain compounds of Formula I described herein possess potent antiviral activity. The invention also provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. Certain compounds described herein inhibit assembly of the HCV replication complex. The invention also provides pharmaceutical compositions containing one or more compounds of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease. These infectious diseases include viral infections, particularly HCV infections.Type: GrantFiled: May 9, 2006Date of Patent: January 3, 2012Assignee: Achillion Pharmaceuticals, Inc.Inventors: Suoming Zhang, Avinash Phadke, Cuixian Liu, Xiangzhu Wang, Jesse Quinn, Dawei Chen, Venkat Gadhachanda, Shouming Li, Milind Deshpande
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Patent number: 8044204Abstract: The invention provides compound and salts of Formula I and II, disclosed herein, which includes compounds of Formula A and Formula B: Such compounds possess useful antimicrobial activity. The variables R2, R3, R5, R6, R7, and R9 shown in Formula A and B are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and/or selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.Type: GrantFiled: July 27, 2006Date of Patent: October 25, 2011Assignee: Achillion Pharmaceuticals, Inc.Inventors: Barton James Bradbury, Jason Allan Wiles, Qiuping Wang, Akhiro Hashimoto, Edlaine Lucien, Godwin Clarence Gilroy Pais, Milind Deshpande, Michael John Pucci, Ha Young Kim
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Publication number: 20110223132Abstract: The invention provides compounds and salts of Formula I and Formula which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A1, R2, R3, R5, R6, R7, A8 and R9 are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.Type: ApplicationFiled: March 14, 2011Publication date: September 15, 2011Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Barton James Bradbury, Milind Deshpande, Michael John Pucci, Qiuping Wang, Jason Allan Wiles, Monishing Song, Akihiro Hashimoto, Edlaine Lucien
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Publication number: 20110213152Abstract: The present invention provides process for synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones of the Formula A. The substituents R, R5, R6, R7, R8 and R9 are defined herein. The invention also provides novel synthetic intermediates useful in the synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones.Type: ApplicationFiled: March 4, 2011Publication date: September 1, 2011Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Barton James Bradbury, Jason Allan Wiles, Akihiro Hashimoto, Qiuping Wang, Edlaine Lucien, Godwin Pais, Ha Young Kim
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Patent number: 7985541Abstract: Methods for detecting populations of newly synthesized and newly initiated RNAs in a cell-free system are described. Suitable templates for the populations of newly synthesized and newly initiated RNAs are viral replicon RNAs, particularly HCV viral replicon RNA. The newly synthesized and newly initiated RNAs may be formed in the presence of a labeled nucleotide analog suitable for detection and/or quantitation of the RNAs. The assay may be employed to identify small molecule inhibitors of RNA synthesis of positive strand RNA viruses such as Hepatitis C Virus.Type: GrantFiled: March 23, 2005Date of Patent: July 26, 2011Assignee: Achillion Pharmaceuticals, Inc.Inventors: Mingjun Huang, Yongnian Sun, Wengang Yang
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Publication number: 20110150997Abstract: The invention provides novel pharmaceutical compositions of Elvucitabine. The invention also provides pharmaceutical compositions and oral dosage forms having unique physical-chemical properties.Type: ApplicationFiled: October 31, 2007Publication date: June 23, 2011Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Gautam Shah, Gary Bubb, Maryam Ahmadi
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Publication number: 20110070168Abstract: 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: November 29, 2010Publication date: March 24, 2011Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Avinash Phadke, Xiangzhu Wang, Suoming Zhang, Atul Agarwal
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Patent number: 7906619Abstract: 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: GrantFiled: July 13, 2007Date of Patent: March 15, 2011Assignee: Achillion Pharmaceuticals, Inc.Inventors: Avinash Phadke, Xiangzhu Wang, Suoming Zhang, Atul Agarwal
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Patent number: 7902365Abstract: The present invention provides process for synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones of the Formula A. The substituents R, R5, R6, R7, R8 and R9 are defined herein. The invention also provides novel synthetic intermediates useful in the synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones.Type: GrantFiled: August 16, 2007Date of Patent: March 8, 2011Assignee: Achillion Pharmaceuticals, Inc.Inventors: Barton James Bradbury, Jason Allan Wiles, Akihiro Hashimoto, Qiuping Wang, Edlaine Lucien, Godwin Pais, Ha Young Kim
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Publication number: 20100292219Abstract: The present invention provides tertiary amine substituted peptides of Formula (I) useful as inhibitors of HCV replication. The variables R and R1-R12 in Formula I are described herein. The invention also includes methods for preparing such compounds. The present invention further includes pharmaceutical compositions containing tertiary amine substituted peptides and methods for using such compounds, including methods for using the compounds to treat hepatitis C infection.Type: ApplicationFiled: February 26, 2008Publication date: November 18, 2010Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Atul Agarwal, Xiangzhu Wang, Dawei Chen, Suoming Zhang, Avinash Phadke
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Publication number: 20100256112Abstract: Disclosed herein are hydroxylthienoquinolones and related compounds and their pharmaceutically acceptable salts useful as antiviral agents and having the general formula in which the variables R2, R6, and R7 are defined herein. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity and are particularly efficacious for the treatment of MRSA infections. The invention also provides pharmaceutical compositions, pharmaceutical compositions containing a hydroxylthienoquinolone in combination with one or more other active agent, and methods of treating microbial infections in animals by administering an effective amount of a hydroxylthienoquinolone or related compound to an animal suffering from a microbial infection.Type: ApplicationFiled: April 5, 2010Publication date: October 7, 2010Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Barton James BRADBURY, Milind DESHPANDE, Akihiro HASHIMOTO, Ha Young KIM, Edlaine LUCIEN, Godwin PAIS, Michael PUCCI, Qiuping WANG, Jason Allan WILES, Avinash PHADKE
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Publication number: 20100256088Abstract: A method of treating viral infections, particularly Hepatitis B (HBV) and Human Immunodeficiency Virus (HIV), by administering a low dose of Elvucitabine to a patient suffering viral infection, is provided herein. The Elvucitabine dosages provided herein for effective anti-viral therapy are approximately 10-fold less than the effective dosages of currently marketed reverse transcriptase inhibitors. The Elvucitabine dosage may be given BID, daily, once ever 48 hours, or once weekly. Also provided herein are packaged pharmaceutical formulations comprising Elvucitabine and instructions for treating a viral infection by administering a low BID, daily, once/48 hour period, or weekly dosage of Elvucitabine. The low dose Elvucitabine formulations provided herein have the additional benefit of improving patient compliance with anti-viral therapy.Type: ApplicationFiled: June 21, 2010Publication date: October 7, 2010Applicant: ACHILLION PHARMACEUTICALS, INC.Inventor: John POTTAGE
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Publication number: 20100216725Abstract: The invention provides 4-amino-4-oxobutanoyl peptides of Formula I and the pharmaceutically salts and hydrates thereof. The variables R, R1, R6-R8, R16, R18, R19, M, n, T, Y, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. The 4-amino-4-oxobutanoyl peptides 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 peptides and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptides as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptides and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections.Type: ApplicationFiled: December 10, 2009Publication date: August 26, 2010Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Avinash Phadke, Dawei Chen, Venkat Gadhachanda, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Atul Agarwal, Ha Young Kim, Shuoming Li, Cuixian Liu, Suoming Zhang, Milind Deshpande
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Patent number: 7767706Abstract: The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections.Type: GrantFiled: February 25, 2008Date of Patent: August 3, 2010Assignee: Achillion Pharmaceuticals, Inc.Inventors: Avinash Phadke, Dawei Chen, Milind Deshpande, Andrew Thurkauf, Xiangzhu Wang, Yiping Shen, Cuixian Liu, Jesse Quinn, Junko Ohkanda, Shouming Li
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Patent number: 7741334Abstract: A method of treating viral infections, particularly Hepatitis B (HBV) and Human Immunodeficiency Virus (HIV), by administering a low dose of Elvucitabine to a patient suffering viral infection is provided herein. The Elvucitabine dosages provided herein for effective anti-viral therapy are approximately 10-fold less than the effective dosages of currently marketed reverse transcriptase inhibitors. The Elvucitabine dosage may be given BID, daily, once every 48 hours, or once weekly. Also provided herein are packaged pharmaceutical formulations comprising Elvucitabine and instructions for treating a viral infection by administering a low BID, daily, once/48 hour, or weekly dosage of Elvucitabine. The low dose Elvucitabine formulations provided herein have the additional benefit of improving patient compliance with anti-viral therapy.Type: GrantFiled: April 1, 2005Date of Patent: June 22, 2010Assignee: Achillion Pharmaceuticals, Inc.Inventor: John Pottage
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Publication number: 20100152103Abstract: The invention provides 4-amino-4-oxobutanoyl peptides and cyclic analogues thereof of Formula I and the pharmaceutically salts thereof. The variables are defined herein. Certain compounds of Formula I are useful as antiviral agents. 4-amino-4-oxobutanoyl peptide cyclic analogues as 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 cyclic analogues and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptide cyclic analogue as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptide cyclic analogue and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in patients.Type: ApplicationFiled: December 10, 2009Publication date: June 17, 2010Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Avinash Phadke, Xiangzhu Wang, Godwin Pais, Akihiro Hashimoto, Venkat Gadhachanda, Dawei Chen, Atul Agarwal, Suoming Zhang, Cuixian Liu, Shouming Li, Milind Deshpande
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Publication number: 20100124545Abstract: The invention provides cyclic carboxamide compounds and analogues thereof of Formula I and the pharmaceutically salts and hydrates thereof. The variables R, R1, R6-R8, R16, R18, R19, M, n, T, Y, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. Certain cyclic carboxamide compounds and cyclic carboxamide analogues 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 cyclic carboxamide compounds or cyclic carboxamide analogues and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a cyclic carboxamide compound or cyclic carboxamide analogue as the only active agent or may contain a combination of a cyclic carboxamide compound or cyclic carboxamide analogue and one or more other pharmaceutically active agents.Type: ApplicationFiled: November 20, 2009Publication date: May 20, 2010Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Suoming Zhang, Avinash Phadke, Milind Deshpande, Venkat Gadhachanda
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Patent number: 7718671Abstract: Substituted arylthiourea compounds of Formula I, and the pharmaceutically acceptable salts of such compounds, useful as antiviral agents, are provided herein. Certain substituted arylthioureas disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions containing one or more substituted arylthiourea compounds and one or more pharmaceutically acceptable carriers, excipients, or diluents are provided herein. Such pharmaceutical compositions may contain a substituted arylthiourea as the only active agent or may contain a combination of a substituted arylthiourea derivative and one or more other pharmaceutically active agents. Methods of treating Hepatitis C viral infections in mammals are also provided herein.Type: GrantFiled: July 8, 2004Date of Patent: May 18, 2010Assignee: Achillion Pharmaceuticals, Inc.Inventors: Avinash Phadke, Jesse Quinn, Junko Ohkanda, Andrew Thurkauf, Yiping Shen, Cuixian Liu, Dawei Chen, Shouming Li, Xiangzhu Wang
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Publication number: 20100093018Abstract: Cells expressing chimeric hepatitis C virus NS4A protein are disclosed, as are vectors and methods for preparing such cells and methods of using the cells and the chimeric proteins therein in screening assays for detecting compounds that alter the associative characteristics of NS4A proteins. Disclosed screening assays are suitable for use in high throughput screening of compound libraries to identify compounds with a exhibiting specific anti-viral activity against hepatitis C virus.Type: ApplicationFiled: April 28, 2008Publication date: April 15, 2010Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Xiaohong Hou, Mingjun Huang, Wengang Yang
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Patent number: 7659399Abstract: The invention provides compounds and salts of Formula I and Formula II: which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A1, A8, R2, R3, R5, R6, R7, and R9 are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.Type: GrantFiled: January 5, 2006Date of Patent: February 9, 2010Assignee: Achillion Pharmaceuticals, Inc.Inventors: Barton James Bradbury, Jason Allan Wiles