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公开(公告)号：EP1385870A2
公开(公告)日：2004-02-04
申请号：EP01954764.5
申请日：2001-07-19
发明人： SAKSENA, Anil, K. , GIRIJAVALLABHAN, Viyyoor, Moopil , LOVEY, Raymond, G. , JAO, Edwin, E. , BENNETT, Frank , MC CORMICK, Jinping, L. , WANG, Haiyan , PIKE, Russell, E. , BOGEN, Stephane, L. , CHAN, Tin-Yau , LIU, Yi-Tsung , ZHU, Zhaoning , NJOROGE, F., George , ARASAPPAN, Ashok , PAREKH, Tejal, N. , GANGULY, Ashit, K. , CHEN, Kevin, X. , VENKATRAMAN, Srikanth , VACCARO, Henry, A. , PINTO, Patrick A. , SANTHANAM, Bama , WU, Wanli , HENDRATA, Siska , HUANG, Yuhua , KEMP, Scott Jeffrey , LEVY, ODILE ESTHER , LIM-WILBY, Marguetita , TAMURA, Susan Y.
IPC分类号： C07K1/00
CPC分类号： C07K5/0202 , A61K38/00 , C07K5/0812 , C07K5/0827 , C07K7/02
摘要： The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
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2.发明公开
公开(公告)号：EP1301528A2
公开(公告)日：2003-04-16
申请号：EP01959046.2
申请日：2001-07-19
发明人： SAKSENA, Anil, K. , GIRIJAVALLABHAN, Viyyoor, Moopil , LOVEY, Raymond, G. , JAO, Edwin, E. , BENNETT, Frank , MCCORMICK, Jinping , WANG, Haiyan , PIKE, Russell, E. , BOGEN, Stephane, L. , LIU, Yi-Tsung , ARASAPPAN, Ashok , PAREKH, Tejal , PINTO, Patrick, A. , NJOROGE, F., George , GANGULY, Ashit, K. , BRUNCK, Terence, K. , KEMP, Scott, Jeffrey , LEVY, Odile, Esther , LIM-WILBY, Marguerita
摘要： The present invention discloses novel peptide compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such peptides as well as methods of using them to treat disorders associated with the HCV protease.
摘要翻译： 本发明公开了具有HCV蛋白酶抑制活性的新型肽化合物以及制备该化合物的方法。 在另一个实施方案中，本发明公开了包含此类肽的药物组合物以及使用它们治疗与HCV蛋白酶相关的病症的方法。
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3.发明公开NOVEL PEPTIDES AS NS3-SERINE PROTEASE INHIBITORS OF HEPATITIS C VIRUS 审中-公开NEW肽NS3蛋白酶抑制剂SERIN丙型肝炎病毒的
公开(公告)号：EP1303487A1
公开(公告)日：2003-04-23
申请号：EP01959041.3
申请日：2001-07-19
发明人： SAKESENA, Anil K. , GIRIJAVALLABHAN, Viyyoor, Moopil , BOGEN, Stephane, L. , LOVEY, Raymond, G. , JAO, Edwin, E. , BENNETT, Frank , MC CORMICK, Jinping, L. , WANG, Haiyan , PIKE, Russell, E. , LIU, Yi-Tsung , CHAN, Tin-Yau , ZHU, Zhaoning , ARASAPPAN, Ashok , CHEN, Kevin, X. , VENKATRAMAN, Srikanth , PAREKH, Tejal, N. , PINTO, Patrick, A. , SANTHANAM, Bama , NJOROGE, F., George , GANGULY, Ashit K. , VACCARO, Henry A. , KEMP, Scott Jeffrey , LEVY, Odile Esther , LIM-WILBY, Marguerita , TAMURA, Susan Y.
IPC分类号： C07D209/02 , C07D211/04 , C07D233/56 , C07D317/10 , C07D319/04 , C07D339/02 , C07D339/08 , C07C229/00 , C07C233/05 , C07C271/08 , C07C271/32 , A61K31/16 , A61K31/27 , A61K31/195 , A61K31/357 , A61K31/385 , A61K31/403 , A61K31/445 , A61K31/4164
CPC分类号： C07K7/06 , A61K31/16 , A61K31/195 , A61K31/27 , A61K31/357 , A61K31/385 , A61K31/403 , A61K31/4164 , A61K31/445 , A61K38/05 , C07C205/51 , C07K5/101 , C07K7/02 , A61K2300/00
摘要： The present invention discloses novel peptide compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
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4.发明公开ANTIVIRAL COMPOUNDS COMPOSED OF THREE LINKED ARYL MOIETIES TO TREAT DISEASES SUCH AS HEPATITIS C 有权THREE彼此相关芳基单元组合抗病毒化合物FOR疾病，如肝炎C的治疗
公开(公告)号：EP2435424A1
公开(公告)日：2012-04-04
申请号：EP10721906.5
申请日：2010-05-28
申请人： Schering Corporation
发明人： ZENG, Qingbei , CHEN, Kevin, X. , ANILKUMAR, Gopinadhan, N. , ROSENBLUM, Stuart, B. , KOZLOWSKI, Joseph, A. , NJOROGE, F., George
IPC分类号： C07D403/14 , A61P31/12 , A61K31/4184
CPC分类号： C07D403/14
摘要： The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient. in one aspect, the present invention provides Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein: Non-limiting examples of the Compounds of Formula (II) include compound 56
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5.发明授权ACYLSULFONAMIDE COMPOUNDS AS INHIBITORS OF HEPATITIS C VIRUS NS3 SERINE PROTEASE 有权丙型肝炎病毒的NS3丝氨酸蛋白酶的ACYLSULFONAMIDVERBINDUNGEN作为抑制剂
公开(公告)号：EP1797111B1
公开(公告)日：2011-06-22
申请号：EP05790914.5
申请日：2005-08-25
申请人： Schering Corporation
CPC分类号： C07K5/0808 , A61K38/00 , C07K5/0217
摘要： The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
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6.发明授权3,4-(CYCLOPENTYL)-FUSED PROLINE COMPOUNDS AS INHIBITORS OF HEPATITIS C VIRUS NS3 SERINE PROTEASE 有权3,4-（环戊基）FUSED脯氨酸化合物作为丙型肝炎病毒的NS3丝氨酸蛋白酶抑制剂的
公开(公告)号：EP1737821B1
公开(公告)日：2009-08-05
申请号：EP05723594.7
申请日：2005-02-24
申请人： Schering Corporation
发明人： NJOROGE, F., George , VENKATRAMAN, Srikanth , ARASAPPAN, Ashok , VELAZQUEZ, Francisco , GIRIJAVALLABHAN, Viyyoor, M.
IPC分类号： C07D209/52 , C07K5/08 , A61K31/401 , A61P31/00
CPC分类号： C07K5/0202
摘要： The present invention discloses novel compounds according to formula (I) which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease. Wherein: R1 is H, OR8, NR9R10, wherein R8, R9 and R10 can be the same or different, each being independently selected from the group consisting of H, alkyl-, alkenyl-, alkynyl-, aryl-, heteroalkyl-, heteroaryl-, cycloalkyl-, heterocyclyl-, arylalkyl-, and heteroarylalkyl, or alternately R9 and R10 in NR9R10 are connected to each other such that NR9R10 forms a four to eight-membered heterocyclyl, and likewise independently alternately R9 and R10 in CHR9R10 are connected to each other such that CHR9R10 forms a four to eight-membered cycloalkyl; Y represents a group G-R wherein G is NH or O.
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7.发明授权IMIDAZOLIDINONES AS NS3-SERINE PROTEASE INHIBITORS OF HEPATITIS C VIRUS 有权咪唑啉酮为NS3蛋白酶抑制剂SERIN丙型肝炎病毒的
公开(公告)号：EP1301486B1
公开(公告)日：2009-07-01
申请号：EP01961676.2
申请日：2001-07-19
申请人： Schering Corporation
发明人： ARASAPPAN, Ashok , PAREKH, Tejal , NJOROGE, F., George , GIRIJAVALLABHAN, Viyyoor, Moopil , GANGUILY, Ashit, K.
IPC分类号： C07D233/38
CPC分类号： C07K7/02 , A61K38/00 , C07D233/38 , C07K5/0202
摘要： The present invention discloses novel imidazolidinones which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazolidinones as well as methods of using them to treat disorders associated with the HCV protease.
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8.发明授权MACROCYCLIC NS3-SERINE PROTEASE INHIBITORS OF HEPATITIS C VIRUS COMPRISING N-CYCLIC P2 MOIETIES 有权与含氮CYCLIC P2 GROUPS丙型肝炎病毒的大环NS3丝氨酸蛋白酶抑制剂
公开(公告)号：EP1268525B1
公开(公告)日：2008-12-31
申请号：EP01926601.4
申请日：2001-04-03
申请人： Schering Corporation
发明人： CHEN, Kevin, X. , ARASAPPAN, Ashok , VENKATRAMAN, Srikanth , PAREKH, Tejal, N. , GU, Haining , NJOROGE, F., George , GIRIJAVALLABHAN, Viyyoor, M. , GANGULY, Ashit , SAKSENA, Anil , JAO, Edwin , YAO, Nanhua, H. , PRONGAY, Andrew, J. , MADISON, Vincent, S. , VIBULBHAN, Bancha
IPC分类号： C07K7/06 , C07K14/18 , C07K5/062 , C07K5/065 , C07K5/087 , C07K5/107 , A61K38/05 , A61K38/06 , A61K38/07 , A61K38/08 , A61P31/14
CPC分类号： C07K5/12 , A61K38/00 , C07K1/02 , C07K5/08 , C07K5/0802 , C07K5/0806 , C07K7/02
摘要： The present invention discloses novel macrocyclic compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such macrocycles as well as methods of using them to treat disorders associated with the HCV protease.
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9.发明授权
公开(公告)号：EP1313725B1
公开(公告)日：2007-04-11
申请号：EP01968188.1
申请日：2001-08-28
发明人： NJOROGE, F., George , VIBULBHAN, Bancha , COOPER, Alan, B. , GUZI, Timothy , RANE, Dinanath, F. , MINOR, Keith, P. , DOLL, Ronald, J. , GIRIJAVALLABHAN, Viyyoor, Moopil , SANTHANAM, Bama , PINTO, Patrick, A. , ZHU, Hugh, Y. , KEERTIKAR, Kartik, M. , ALVAREZ, Carmen, S. , BALDWIN, John, J. , LI, Ge , HUANG, Chia-Yu , JAMES, Ray, A. , BISHOP, Robert, W. , WANG, James , DESAI, Jagdish, A.
IPC分类号： C07D401/06 , C07D401/04 , C07D401/14 , C07D221/16 , A61K31/435 , A61P35/00
CPC分类号： C07D231/12 , C07D221/16 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/14
摘要： The present invention discloses novel tricyclic compounds represented by the formula (1.0), a prodrug thereof, or a pharmaceutically acceptable salt or solvate of the compound or of said prodrug useful for inhibiting farnesyl protein transferase. Also disclosed are pharmaceutical compositions comprising such compounds their preparation as well as methods of using them to treat proliferative diseases such as cancer.
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10.发明公开3,4-(CYCLOPENTYL)-FUSED PROLINE COMPOUNDS AS INHIBITORS OF HEPATITIS C VIRUS NS3 SERINE PROTEASE 有权3,4-（环戊基）FUSED脯氨酸化合物作为丙型肝炎病毒的NS3丝氨酸蛋白酶抑制剂的
公开(公告)号：EP1737821A1
公开(公告)日：2007-01-03
申请号：EP05723594.7
申请日：2005-02-24
申请人： SCHERING CORPORATION
发明人： NJOROGE, F., George , VENKATRAMAN, Srikanth , ARASAPPAN, Ashok , VELAZQUEZ, Francisco , GIRIJAVALLABHAN, Viyyoor, M.
IPC分类号： C07D209/52 , C07K5/08 , A61K31/401 , A61P31/00
CPC分类号： C07K5/0202
摘要： The present invention discloses novel compounds according to formula (I) which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease. Wherein: R1 is H, OR8, NR9R10, wherein R8, R9 and R10 can be the same or different, each being independently selected from the group consisting of H, alkyl-, alkenyl-, alkynyl-, aryl-, heteroalkyl-, heteroaryl-, cycloalkyl-, heterocyclyl-, arylalkyl-, and heteroarylalkyl, or alternately R9 and R10 in NR9R10 are connected to each other such that NR9R10 forms a four to eight-membered heterocyclyl, and likewise independently alternately R9 and R10 in CHR9R10 are connected to each other such that CHR9R10 forms a four to eight-membered cycloalkyl; Y represents a group G-R wherein G is NH or O.
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