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1. 发明申请

WO2010022121A1 SUBSTITUTED PYRIDINE AND PYRIMIDINE DERIVATIVES AND THEIR USE IN TREATING VIRAL INFECTIONS 审中-公开
标题翻译：取代的吡啶和吡嗪衍生物及其在治疗病毒感染中的应用
公开(公告)号：WO2010022121A1
公开(公告)日：2010-02-25
申请号：PCT/US2009/054264
申请日：2009-08-19
申请人： SCHERING CORPORATION , SOUTHERN RESEARCH INSTITUTE , ARASAPPAN, Ashok , NJOROGE, F., George , BENNETT, Frank , GIRIJAVALLABHAN, Vinay, M. , HUANG, Yuhua , HUELGAS, Regina , PIWINSKI, John, J. , SHIH, Neng-Yang , VERMA, Vishal , VELAZQUEZ, Francisco , VENKATRAMAN, Srikanth , KWONG, Cecil, D. , ANANTHAN, Subramaniam , CLARK, Jeremy , GENG, Feng , KEZAR, Hollis, S., III. , MADDRY, Joseph, A. , REYNOLDS, Robert, C. , ROYCHOWDHURY, Abhijit , SECRIST, John, A., III. , FOWLER, Anita, T.
发明人： ARASAPPAN, Ashok , NJOROGE, F., George , BENNETT, Frank , GIRIJAVALLABHAN, Vinay, M. , HUANG, Yuhua , HUELGAS, Regina , PIWINSKI, John, J. , SHIH, Neng-Yang , VERMA, Vishal , VELAZQUEZ, Francisco , VENKATRAMAN, Srikanth , KWONG, Cecil, D. , ANANTHAN, Subramaniam , CLARK, Jeremy , GENG, Feng , KEZAR, Hollis, S., III. , MADDRY, Joseph, A. , REYNOLDS, Robert, C. , ROYCHOWDHURY, Abhijit , SECRIST, John, A., III. , FOWLER, Anita, T.
IPC分类号： C07D239/48 , C07D491/04 , C07D409/04 , C07D417/04 , C07D413/04 , C07D405/04 , C07D417/14 , C07D401/04 , C07D403/04 , C07D401/14 , C07D413/14 , A61K31/506 , A61P31/12
CPC分类号： C07D239/48 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D491/04
摘要： The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein wherein each of R, R 1 , X, Y, Z, R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 18 , R 19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.
摘要翻译：本发明提供式（I）的化合物：所述化合物的互变异构体，异构体和酯，以及所述化合物的药学上可接受的盐，溶剂合物和前药，其中R，R 1，X，Y，Z，R 2 ，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 18，R 19和n独立地如本文所定义。还提供了包含这些化合物的组合物。本发明的化合物作为HCV的抑制剂是有效的，并且单独和与其它治疗剂一起用于治疗或预防疾病或病症如病毒感染和病毒相关疾病。

2. 发明申请

WO1998011099A1 SUBSTITUTED BENZOCYCLOHEPTAPYRIDINE DERIVATIVES USEFUL FOR INHIBITION OF FARNESYL PROTEIN TRANSFERASE 审中-公开
标题翻译：用于抑制FARNESYY蛋白转移的替代苄基环己基吡啶衍生物
公开(公告)号：WO1998011099A1
公开(公告)日：1998-03-19
申请号：PCT/US1997015905
申请日：1997-09-11
申请人： SCHERING CORPORATION
发明人： SCHERING CORPORATION , TAVERAS, Arthur, G. , NJOROGE, F., George
IPC分类号： C07D401/14
CPC分类号： C07D401/14 , C07D405/14
摘要： Novel compounds of formula (1.0) are disclosed. Compounds of formula (1.0) are represented by the compounds of formulas (1.4) or (1.5) wherein R , R and R are each independently selected from halo. W represents a group selected from (a), (b), (c) or (d). Also disclosed are methods of inhibiting farnesyl protein transferase and the growth of abnormal cells, such as tumor cells.
摘要翻译：公开了新的式（1.0）化合物。式（1.0）的化合物由式（1.4）或（1.5）的化合物表示，其中R 1，R 3和R 4各自独立地选自卤素。 W表示选自（a），（b），（c）或（d）的基团。还公开了抑制法呢基蛋白转移酶和异常细胞如肿瘤细胞生长的方法。

3. 发明申请

WO1998011097A1 SUBSTITUTED BENZOCYCLOHEPTAPYRIDINE USEFUL AS INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE 审中-公开
标题翻译：取代的苄基胆碱吡啶可用作蛋白转移酶的抑制剂
公开(公告)号：WO1998011097A1
公开(公告)日：1998-03-19
申请号：PCT/US1997015902
申请日：1997-09-11
申请人： SCHERING CORPORATION
发明人： SCHERING CORPORATION , RANE, Dinanath, F. , COOPER, Alan, B. , MALLAMS, Alan, K. , DOLL, Ronald, J. , NJOROGE, F., George , TAVERAS, Arthur, G.
IPC分类号： C07D401/14
CPC分类号： C07D401/14
摘要： Novel tricyclic compounds of formula (1.0) or a pharmaceutically acceptable salt or solvate thereof, wherein: one of a, b, c and d represents N or NR wherein R is O , -CH3 or -(CH2)nCO2H wherein n is 1 to 3, and the remaining a, b, c and d groups represent CR or CR ; or each of a, b, c, and d are independently selected from CR or CR ; each R and each R is independently selected from H, halo, -CF3, -OR , -COR , -SR , -S(O)tR (wherein t is 0, 1 or 2), -SCN, -N(R )2, -NR R , -NO2, -OC(O)R , -CO2R , -OCO2R , -CN, -NHC(O)R , -NHSO2R , -CONHR , -CONHCH2CH2OH, -NR COOR , -SR C(O)OR , -SR N(R )2; y is 0 (zero) or 1; n is 0, 1, 2, 3, 4, 5 or 6; T is -CO-; -SO-; -SO2-; or -CR R ; Z represents alkyl, aryl, aralkyl, heteroalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl, heterocycloalkylalkyl, -OR , -SR , 1C-R R , (i), (ii), -NR R , (iii). Pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel tricyclic compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human.
摘要翻译：式（1.0）的新型三环化合物或其药学上可接受的盐或溶剂合物，其中：a，b，c和d中的一个表示N或NR 9，其中R 9是O - ， - CH 3或 - （CH 2）n CO 2 H，其中n为1至3，其余的a，b，c和d基团表示CR 1或CR 2; 或者a，b，c和d中的每一个独立地选自CR 1或CR 2; 每个R 1和每个R 2独立地选自H，卤素，-CF 3，-OR 10，-COR 10，-SR 10，-S（O）t R 11（其中t是0,1或2），-SCN，-N（R 10）2，-NR 10 R 11，-NO 2，-OC（O）R 10，-CO 2 R 10 ，-OCO 2 R 11，-CN，-NHC（O）R 10，-NHSO 2 R 10，-CONHR 10，-CONHCH 2 CH 2 OH，-NR 10 COOR 11，-SR 11 C（O）OR 11，-SR 11 N（R 75）2; y为0（零）或1; n为0，1，2，3，4，5或6; T是-CO-; -所以-; -SO2-; 或-CR 30 R 31; Z表示烷基，芳基，芳烷基，杂烷基，杂芳基，杂芳基烷基，杂环烷基，杂环烷基烷基，-OR 40，-SR 40，1C-R 40，（i），（ii） NR 40，R 42，（iii）。公开了作为酶的抑制剂的法呢基蛋白转移酶的药物组合物。还公开了抑制Ras功能并因此抑制细胞异常生长的方法。该方法包括将新型三环化合物施用于生物系统。特别地，该方法抑制哺乳动物（例如人）中细胞的异常生长。

4. 发明申请

WO1996031111A1 TRICYCLIC COMPOUNDS USEFUL IN THE TREATMENT OF CELL PROLIFERATIVE DISORDERS 审中-公开
标题翻译：用于治疗细胞增殖性疾病的TRICYCLIC化合物
公开(公告)号：WO1996031111A1
公开(公告)日：1996-10-10
申请号：PCT/US1996004168
申请日：1996-04-03
申请人： SCHERING CORPORATION
发明人： SCHERING CORPORATION , DOLL, Ronald, J. , MALLAMS, Alan, K. , AFONSO, Adriano , RANE, Dinanath, F. , NJOROGE, F., George , ROSSMAN, Randall, R.
IPC分类号： A61K31/55 , A61P35/00 , C07D401/12 , C07D403/06 , C07D471/04
CPC分类号： C07D401/12 , C07D471/04
摘要： Novel compounds of Formula (1.0) are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the formula to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.
摘要翻译：公开了新的式（1.0）化合物。还公开了抑制Ras功能并因此抑制细胞异常生长的方法。该方法包括将下式的化合物施用于生物系统。特别地，该方法抑制哺乳动物例如人的细胞的异常生长。

5. 发明申请

WO1996030018A1 TRICYCLIC CARBAMATE COMPOUNDS USEFUL FOR INHIBITION OF G-PROTEIN FUNCTION AND FOR TREATMENT OF PROLIFERATIVE DISEASES 审中-公开
标题翻译：用于抑制G蛋白功能和治疗增殖性疾病的三元碳酸酯化合物
公开(公告)号：WO1996030018A1
公开(公告)日：1996-10-03
申请号：PCT/US1996003312
申请日：1996-03-21
申请人： SCHERING CORPORATION
发明人： SCHERING CORPORATION , BISHOP, W., Robert , DOLL, Ronald, J. , MALLAMS, Alan, K. , NJOROGE, F., George , PETRIN, Joanne, M. , PIWINSKI, John, J. , WOLIN, Ronald, L. , TAVERAS, Arthur, G. , REMISZEWSKI, Stacy, W.
IPC分类号： A61K31/495
CPC分类号： C07D401/12 , A61K31/4545 , A61K31/496 , C07D221/16 , C07D401/04 , C07D401/14
摘要： A method of inhibiting Ras function and therefore inhibiting cellular growth is disclosed. The method comprises the administration of a compound selected from (800.00), (801.00), (802.00), (803.00), (804.00), or (805.00). Compounds of structures (800.00) - (805.00) are novel compounds.
摘要翻译：公开了抑制Ras功能并因此抑制细胞生长的方法。该方法包括施用选自（800.00），（801.00），（802.00），（803.00），（804.00）或（805.00）的化合物。结构化合物（800.00） - （805.00）是新化合物。

6. 发明申请

WO1995010516A1 TRICYCLIC AMIDE AND UREA COMPOUNDS USEFUL FOR INHIBITION OF G-PROTEIN FUNCTION AND FOR TREATMENT OF PROLIFERATIVE DISEASES 审中-公开
标题翻译：用于抑制G蛋白功能和治疗增殖性疾病的三酰胺和尿素化合物
公开(公告)号：WO1995010516A1
公开(公告)日：1995-04-20
申请号：PCT/US1994011392
申请日：1994-10-12
申请人： SCHERING CORPORATION
发明人： SCHERING CORPORATION , BISHOP, W., Robert , DOLL, Ronald, J. , MALLAMS, Alan, K. , NJOROGE, F., George , PETRIN, Joanne, M. , PIWINSKI, John, J. , REMISZEWSKI, Stacy, W. , TAVERAS, Arthur, G. , WOLIN, Ronald, L.
IPC分类号： C07D401/04
CPC分类号： C07D231/12 , A61K31/444 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/505 , C07D221/16 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： A method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells is disclosed. The method comprises the administration of a compound of formula (1.0) to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being. Novel compounds of formulae (5.0, 5.1, 5.2, 5.3, 5.3A and 5.3B) are disclosed. Also disclosed are processes for making 3-substituted compounds of formulae (5.0, 5.1, 5.2 and 5.3). Further disclosed are novel compounds which are intermediates in the process for making 3-substituted compounds of formulae (5.0, 5.1, 5.2 and 5.3).
摘要翻译：公开了抑制Ras功能并因此抑制细胞异常生长的方法。该方法包括向生物系统施用式（1.0）化合物。特别地，该方法抑制哺乳动物例如人的细胞的异常生长。公开了新的式（5.0,5.1,5.2,5.3,5.3A和5.3B）的化合物。还公开了制备式（5.0,5.1,5.2和5.3）的3-取代的化合物的方法。进一步公开的是在制备3-取代的式（5.0,5.1,5.2和5.3）化合物的方法中的中间体的新化合物。

7. 发明申请

WO2010138790A1 ANTIVIRAL COMPOUNDS COMPOSED OF THREE ALIGNED ARYL MOIETIES TO TREAT DISEASES SUCH AS HEPATITIS C 审中-公开
标题翻译：由三种对齐的ARYL MOIETIES组成的抗病毒化合物治疗疾病如HEPATITIS C
公开(公告)号：WO2010138790A1
公开(公告)日：2010-12-02
申请号：PCT/US2010/036520
申请日：2010-05-28
申请人： SCHERING CORPORATION , CHEN, Kevin, X. , ANILKUMAR, Gopinadhan, N. , ZENG, Qingbei , ROSENBLUM, Stuart, B. , KOZLOWSKI, Joseph, A. , NJOROGE, F., George
发明人： CHEN, Kevin, X. , ANILKUMAR, Gopinadhan, N. , ZENG, Qingbei , ROSENBLUM, Stuart, B. , KOZLOWSKI, Joseph, A. , NJOROGE, F., George
IPC分类号： C07D401/14 , C07D403/14 , C07D409/14 , C07D417/14 , A61K31/4184 , A61K31/12
CPC分类号： C07D401/14 , C07D403/14 , C07D409/14 , C07D417/14
摘要： The present invention relates to novel Tricyclic Compounds, compositions comprising at least one Tricyclic Compound, and methods of using Tricyclic Compounds for treating or preventing a viral infection or a virus-related disorder in a patient. The present invention provides Tricyclic Compounds of Formula (I): Non-limiting examples of the Compounds of Formula (I) include compound 44 The Compounds of Formula (II) can be useful for inhibiting HCV viral replication or replicon activity, and for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及新型三环化合物，包含至少一种三环化合物的组合物，以及使用三环化合物治疗或预防患者病毒感染或病毒相关疾病的方法。本发明提供式（I）的三环化合物：式（I）化合物的非限制性实例包括化合物44式（II）化合物可用于抑制HCV病毒复制或复制子活性，并且可用于治疗或预防患者的HCV感染。

8. 发明申请

WO2010117935A1 COMPOUNDS AND METHODS FOR ANTIVIRAL TREATMENT 审中-公开
标题翻译：化合物和方法进行抗病毒治疗
公开(公告)号：WO2010117935A1
公开(公告)日：2010-10-14
申请号：PCT/US2010/029928
申请日：2010-04-05
申请人： SCHERING CORPORATION , PTC THERAPEUTICS, INC , MACCOSS, Malcolm , NJOROGE, F., George , NOMEIR, Amin , CHEN, Guangming , KARP, Gary, Mitchell , LENNOX, William, Joseph , LI, Chunshi , MORRILL, Christie , PAGET, Steven, D. , REN, Hongyu , ZHANG, Nanjing , ZHANG, Xiaoyan
发明人： MACCOSS, Malcolm , NJOROGE, F., George , NOMEIR, Amin , CHEN, Guangming , KARP, Gary, Mitchell , LENNOX, William, Joseph , LI, Chunshi , MORRILL, Christie , PAGET, Steven, D. , REN, Hongyu , ZHANG, Nanjing , ZHANG, Xiaoyan
IPC分类号： C07D471/04 , C07D487/04 , A61K31/519 , A61P31/12
CPC分类号： C07D471/04 , A61K31/437 , A61K31/506 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D487/04
摘要： The present invention is directed to compounds of formula (I) and forms and pharmaceutical compositions thereof useful for treating a viral infection, or for affecting viral activity by modulating viral replication.
摘要翻译：本发明涉及用于治疗病毒感染或通过调节病毒复制影响病毒活性的式（I）化合物及其形式和药物组合物。

9. 发明申请

WO2010068714A3 DEUTERATED COMPOUNDS AS HEPATITIS C VIRUS (HCV) INHIBITORS 审中-公开
公开(公告)号：WO2010068714A3
公开(公告)日：2010-06-17
申请号：PCT/US2009/067415
申请日：2009-12-10
申请人： SCHERING CORPORATION , MACCOSS, Malcolm , NJOROGE, F., George , BENNETT, Frank , VENKATRAMAN, Srikanth , KOZLOWSKI, Joseph, A. , YU, Wensheng , McNAMARA, Paul, E. , ROYSTER, Pernilla, R.
发明人： MACCOSS, Malcolm , NJOROGE, F., George , BENNETT, Frank , VENKATRAMAN, Srikanth , KOZLOWSKI, Joseph, A. , YU, Wensheng , McNAMARA, Paul, E. , ROYSTER, Pernilla, R.
IPC分类号： A61K31/403 , A61K31/7056 , A61K38/21 , A61P31/14 , A61K45/06 , A61K38/05 , C07K5/06
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 wet! as methods of using them to treat disorders associated with the HCV protease An illustrative inventsve compound is shown below: Formula (I).

10. 发明申请

WO2009032124A1 SUBSTITUTED INDOLE DERIVATIVES AND METHODS OF USE THEREOF 审中-公开
标题翻译：取代的吲哚衍生物及其使用方法
公开(公告)号：WO2009032124A1
公开(公告)日：2009-03-12
申请号：PCT/US2008/010148
申请日：2008-08-27
申请人： SCHERING CORPORATION , ANILKUMAR, Gopinadhan, N. , BENNETT, Frank , CHAN, Tin-Yau , CHEN, Kevin, X. , SANNIGRAHI, Mousumi , VELAZQUEZ, Francisco , VENKATRAMAN, Srikanth , ZENG, Qingbei , DUCA, Jose, S. , LESBURG, Charles, A. , KOZLOWSKI, Joseph, A. , NJOROGE, F., George , ROSENBLUM, Stuart, B. , SHIH, Neng-Yang
发明人： ANILKUMAR, Gopinadhan, N. , BENNETT, Frank , CHAN, Tin-Yau , CHEN, Kevin, X. , SANNIGRAHI, Mousumi , VELAZQUEZ, Francisco , VENKATRAMAN, Srikanth , ZENG, Qingbei , DUCA, Jose, S. , LESBURG, Charles, A. , KOZLOWSKI, Joseph, A. , NJOROGE, F., George , ROSENBLUM, Stuart, B. , SHIH, Neng-Yang
IPC分类号： C07D401/04 , C07D403/04 , A61K31/513 , A61P31/12
CPC分类号： C07D403/04 , C07D401/04
摘要： The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
摘要翻译：本发明涉及取代的吲哚衍生物，包含至少一种取代的吲哚衍生物的组合物，以及使用这些取代的吲哚衍生物来治疗或预防患者的病毒感染或病毒相关病症的方法。

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