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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

WO2009105500A1 COMPOUNDS THAT ARE ERK INHIBITORS 审中-公开
标题翻译：化合物是ERK抑制剂
公开(公告)号：WO2009105500A1
公开(公告)日：2009-08-27
申请号：PCT/US2009/034447
申请日：2009-02-19
申请人： SCHERING CORPORATION , COOPER, Alan, B. , NAN, Yang , DENG, Yongqi , SHIPPS, Gerald W., Jr. , SHIH, Neng-Yang , ZHU, Hugh, Y. , KELLY, Joseph, M. , GUDIPATI, Subrahmanyam , DOLL, Ronald J. , PATEL, Mehul, F. , DESAI, Jagdish, A. , WANG, James, J-S , PALIWAL, Sunil , TSUI, Hon-Chung , BOGA, Sobhana, Babu , ALHASSAN, Abdul-Basit , GAO, Xiaolei , ZHU, Liang , YAO, Xin
发明人： COOPER, Alan, B. , NAN, Yang , DENG, Yongqi , SHIPPS, Gerald W., Jr. , SHIH, Neng-Yang , ZHU, Hugh, Y. , KELLY, Joseph, M. , GUDIPATI, Subrahmanyam , DOLL, Ronald J. , PATEL, Mehul, F. , DESAI, Jagdish, A. , WANG, James, J-S , PALIWAL, Sunil , TSUI, Hon-Chung , BOGA, Sobhana, Babu , ALHASSAN, Abdul-Basit , GAO, Xiaolei , ZHU, Liang , YAO, Xin
IPC分类号： C07D403/14 , A61K31/435
CPC分类号： C07D403/14
摘要： Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, and solvates thereof. Q is a tetrahydopyridinyl ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
摘要翻译：公开了式1.0的ERK抑制剂及其药学上可接受的盐和溶剂化物。 Q是四氢吡啶基环。所有其他取代基如本文所定义。还公开了使用式1.0化合物治疗癌症的方法。

3. 发明申请

WO2008153858A1 POLYCYCLIC INDAZOLE DERIVATIVES AND THEIR USE AS ERK INHIBITORS FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：多环吲哚衍生物及其用作治疗癌症的ERK抑制剂
公开(公告)号：WO2008153858A1
公开(公告)日：2008-12-18
申请号：PCT/US2008/006979
申请日：2008-06-04
申请人： SCHERING CORPORATION , COOPER, Alan , DENG, Yongqi , SHIPPS, Gerald, W., Jr. , SHIH, Neng-Yang , ZHU, Hugh , KELLY, Joseph , DOLL, Ronald , NAN, Yang , DESAI, Jagdish , WANG, James , PALIWAL, Sunil , TSUI, Hon-Chung , BOGA, Sobhana, Babu , ALHASSAN, Abdul-Basit , GAO, Xiaolei , ZHU, Liang , PATEL, Mehul
发明人： COOPER, Alan , DENG, Yongqi , SHIPPS, Gerald, W., Jr. , SHIH, Neng-Yang , ZHU, Hugh , KELLY, Joseph , DOLL, Ronald , NAN, Yang , DESAI, Jagdish , WANG, James , PALIWAL, Sunil , TSUI, Hon-Chung , BOGA, Sobhana, Babu , ALHASSAN, Abdul-Basit , GAO, Xiaolei , ZHU, Liang , PATEL, Mehul
IPC分类号： C07D401/14 , C07D403/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D491/056 , A61K31/4245 , A61K31/444 , A61K31/506 , A61P35/00
CPC分类号： C07D401/14 , C07D403/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D491/056
摘要： Disclosed are the ERK inhibitors of formula 1.0: (Chemical formula should be inserted here as it appears on abstract in paper form) and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
摘要翻译：公开了式1.0的ERK抑制剂：（化学式应该插入在此，其以纸质形式摘要出现）及其药学上可接受的盐，酯和溶剂化物。 Q是可以具有桥或稠合环的哌啶或哌嗪环。哌啶环可以在环中具有双键。所有其他取代基如本文所定义。还公开了使用式1.0化合物治疗癌症的方法。

4. 发明申请

WO2002072570A2 NOVEL NON-IMIDAZOLE COMPOUNDS 审中-公开
标题翻译：新型非咪唑化合物
公开(公告)号：WO2002072570A2
公开(公告)日：2002-09-19
申请号：PCT/US2002/007106
申请日：2002-03-11
申请人： SCHERING CORPORATION , PHARMACOPEIA, INC.
发明人： ROSENBLUM, Stuart, B. , ZENG, Qingbei , MUTAHI, Mwangi, Wa , ASLANIAN, Robert, G. , TING, Pauline, C. , SHIH, Neng-Yang , SOLOMON, Daniel, M. , CAO, Jianhua , VACCARO, Henry, A. , MC CORMICK, Kevin, D. , BALDWIN, John, J. , LI, Ge
IPC分类号： C07D401/00
CPC分类号： C07D401/14 , C07D211/26 , C07D211/38 , C07D211/62 , C07D211/96 , C07D243/08 , C07D401/06 , C07D407/12 , C07D407/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07D451/02 , C07D487/06
摘要： Disclosed are novel compounds of the formula (I). Also disclosed are pharmaceutical compositions comprising the compounds of Formula (I). Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula (I). Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula (I) in combination with a H1 receptor antagonist.
摘要翻译：公开了式（I）的新化合物。还公开了包含式（I）化合物的药物组合物。还公开了使用式（I）的化合物治疗各种疾病或病症的方法，例如过敏，过敏诱发的气道反应和充血（例如鼻塞）。还公开了使用式（I）化合物与H1受体拮抗剂组合治疗各种疾病或病症，例如变态反应，变态反应诱发的气道反应和充血（例如鼻塞）的方法。

5. 发明申请

WO1998020010A1 SUBSTITUTED OXIMES, HYDRAZONES AND OLEFINS AS NEUROKININ ANTAGONISTS 审中-公开
标题翻译：作为神经营养因子拮抗剂的替代物，水合物和油脂
公开(公告)号：WO1998020010A1
公开(公告)日：1998-05-14
申请号：PCT/US1997019164
申请日：1997-10-30
申请人： SCHERING CORPORATION
发明人： SCHERING CORPORATION , SHIH, Neng-Yang , REICHARD, Gregory, A. , ASLANIAN, Robert, G.
IPC分类号： C07D471/10
CPC分类号： C07D471/10
摘要： Compound represented by structural formula (I) or a pharmaceutically acceptable salt thereof, wherein: a is 0, 1, 2 or 3; b, d and e are independently 0, 1 or 2; R is H, C>1-6 2 6 -, -S(O)e-, -N(R )C(O)-, -C(O)N(R )-, -OC(O)NR -, -OC(=S)NR -, -N(R )C(=S)O-, -C(=NOR )-, -S(O)2N(R )-, -N(R )S(O)2-, -N(R )C(O)O- or -OC(O)-; T is H, phthalimidyl, aryl, heterocycloalkyl, heteroaryl, cycloalkyl or bridged cycloalkyl; Q is -SR , -N(R )(R ), -OR , phenyl, naphthyl or heteroaryl; R , R , R , R , R and R are H, C1-6 alkyl, C2-C6 hydroxyalkyl, C1-C6 alkoxy-C1-C6 alkyl, phenyl or benzyl; or R and R , together with the nitrogen to which they are attached, form a ring; R is R or -OR ; and Z is spiro-substituted piperidinyl or substituted piperazinyl wherein aryl, heterocycloalkyl, heteroaryl, cycloalkyl and bridged cycloalkyl groups are optionally substituted; methods of treating asthma, cough, bronchospasm, inflammatory diseases, and gastrointestinal disorders with said compounds, and pharmaceutical compositions comprising said compounds are disclosed.
摘要翻译：由结构式（I）表示的化合物或其药学上可接受的盐，其中：a为0,1,2或3; b，d和e独立地为0,1或2; R是H，C 1-6>烷基，-OH或C 2 -C 6羟烷基; A是任选取代的肟，腙或烯烃; X是键，-C（O） - ， - O - ， - NR 6 - ， - S（O）e - ， - N（R 6）C（O） N（R 6） - ， - OC（O）NR 6 - ， - OC（= S）NR 6 - ， - N（R 6）C（= S）（= NOR 1） - ， - S（O）2 N（R 6） - ， - N（R 6）S（O）2 - ， - N（R 6） O-或-OC（O） - ; T是H，苯二酰亚氨基，芳基，杂环烷基，杂芳基，环烷基或桥连环烷基; Q是-SR 6，-N（R 6）（R 7），-OR 6，苯基，萘基或杂芳基; R 6a，R 7a，R 8a，R 9a，R 6和R 7是H，C 1-6烷基，C 2 -C 6羟烷基，C 1 -C 6烷氧基-C 1 -C 6 烷基，苯基或苄基; 或R 6和R 7与它们所连接的氮一起形成环; R 9a是R 6或-OR 6; Z是螺取代的哌啶基或取代的哌嗪基，其中芳基，杂环烷基，杂芳基，环烷基和桥连的环烷基任选被取代; 公开了用所述化合物治疗哮喘，咳嗽，支气管痉挛，炎性疾病和胃肠道疾病的方法，以及包含所述化合物的药物组合物。

6. 发明申请

WO2010022128A1 ETHENYL-SUBSTITUTED PYRIDINE AND PYRIMIDINE DERIVATIVES AND THEIR USE IN TREATING VIRAL INFECTIONS 审中-公开
标题翻译：乙基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：WO2010022128A1
公开(公告)日：2010-02-25
申请号：PCT/US2009/054271
申请日：2009-08-19
申请人： SCHERING CORPORATION , SOUTHERN RESEARCH INSTITUTE , NJOROGE, F. George , PIWINSKI, John J. , SHIH, Neng-Yang , KWONG, Cecil D. , ANANTHAN, Subramaniam , CLARK, Jeremy , GENG, Feng , KEZAR, III, Hollis S. , MADDRY, Joseph A. , REYNOLDS, Robert C. , ROYCHOWDHURY, Abhijit , SECRIST, III, John A.
发明人： NJOROGE, F. George , PIWINSKI, John J. , SHIH, Neng-Yang , KWONG, Cecil D. , ANANTHAN, Subramaniam , CLARK, Jeremy , GENG, Feng , KEZAR, III, Hollis S. , MADDRY, Joseph A. , REYNOLDS, Robert C. , ROYCHOWDHURY, Abhijit , SECRIST, III, John A.
IPC分类号： C07D239/48 , A61K31/505 , A61P31/14
CPC分类号： C07D239/48
摘要： The present invention provides compounds of Formula (A): (Chemical formula should be inserted here as it appears on abstract in paper form) (A) 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 , R 22 , R 23 , 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 dieases or disorders such as viral infections and virus-related disorders.
摘要翻译：本发明提供了式（A）化合物：（化学式应该插在这里，它以纸质形式的摘要出现）（A）和所述化合物的互变异构体，异构体和酯以及药学上可接受的盐，溶剂合物和前药的所述化合物，其中R，R1，X，Y，Z，R2，R3，R4，R5，R6，R7，R8，R9，R18，R19，R22，R23和n各自独立地和定义于此。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，并且可单独使用和与其它治疗剂一起用于治疗或预防死亡或病症如病毒感染和病毒相关疾病。

7. 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。

8. 发明申请

WO2009008913A2 P1-NONEPIMERIZABLE KETOAMIDE INHIBITORS OF HCV NS3 PROTEASE 审中-公开
标题翻译：丙型肝炎病毒NS3蛋白酶的P1非可庚酮酰胺抑制剂
公开(公告)号：WO2009008913A2
公开(公告)日：2009-01-15
申请号：PCT/US2008/003652
申请日：2008-03-20
申请人： SCHERING CORPORATION , VENKATRAMAN, Srikanth , NJOROGE, F., George , VELAZQUEZ, Francisco , WU, Wanli , MADISON, Vincent, S. , SHIH, Neng-Yang
发明人： VENKATRAMAN, Srikanth , NJOROGE, F., George , VELAZQUEZ, Francisco , WU, Wanli , MADISON, Vincent, S. , SHIH, Neng-Yang
IPC分类号： C07D207/16 , C07D401/12 , A61K31/401 , A61P31/12
CPC分类号： C07D207/16 , C07D401/12
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.
摘要翻译：本发明公开了具有HCV蛋白酶抑制活性的新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化合物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。

9. 发明申请

WO2007145921A1 IMIDAZOPYRAZINES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的咪唑吡嗪
公开(公告)号：WO2007145921A1
公开(公告)日：2007-12-21
申请号：PCT/US2007/013201
申请日：2007-06-05
申请人： SCHERING CORPORATION , ZHAO, Lianyun , REDDY, Panduranga, Adulla, P. , SHIH, Neng-Yang , PARUCH,, Kamil , GUZI, Timothy, J. , SIDDIQUI, M., Arshad
发明人： ZHAO, Lianyun , REDDY, Panduranga, Adulla, P. , SHIH, Neng-Yang , PARUCH,, Kamil , GUZI, Timothy, J. , SIDDIQUI, M., Arshad
IPC分类号： C07D487/04 , A61K31/4985 , A61P35/00
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds of formula (I) as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions.
摘要翻译：在其许多实施方案中，本发明提供了一类新颖的式（I）的咪唑并吡嗪化合物作为蛋白质和/或检查点激酶的抑制剂，制备这些化合物的方法，包含一种或多种这类化合物的药物组合物，制备药物制剂的方法包括一种或多种这样的化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与蛋白质或检查点激酶相关的一种或多种疾病的方法。

10. 发明申请

WO2007084451A1 HYDANTOIN DERIVATIVES FOR THE TREATMENT OF INFLAMMATORY DISORDERS 审中-公开
标题翻译：用于治疗炎症性疾病的HYDANTOIN衍生物
公开(公告)号：WO2007084451A1
公开(公告)日：2007-07-26
申请号：PCT/US2007/001025
申请日：2007-01-16
申请人： SCHERING CORPORATION , LAVEY, Brian, J. , KOZLOWSKI, Joseph, A. , ZHOU, Guowei , TONG, Ling , YU, Wensheng , WONG, Michael, K.C. , SHANKAR, Bandarpalle, B. , SHIH, Neng-Yang , SIDDIQUI, M., Arshad , ROSNER, Kristin, E. , DAI, Chaoyang , POPOVICI-MULLER, Janeta , GIRIJAVALLABHAN, Vinay, M. , LI, Dansu , RIZVI, Razia , CHEN, Lei , YANG, De-yi , FELTZ, Robert , KIM, Seong-heon
发明人： LAVEY, Brian, J. , KOZLOWSKI, Joseph, A. , ZHOU, Guowei , TONG, Ling , YU, Wensheng , WONG, Michael, K.C. , SHANKAR, Bandarpalle, B. , SHIH, Neng-Yang , SIDDIQUI, M., Arshad , ROSNER, Kristin, E. , DAI, Chaoyang , POPOVICI-MULLER, Janeta , GIRIJAVALLABHAN, Vinay, M. , LI, Dansu , RIZVI, Razia , CHEN, Lei , YANG, De-yi , FELTZ, Robert , KIM, Seong-heon
IPC分类号： C07D403/14 , A61K31/4178 , A61P29/00
CPC分类号： C07D403/14 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00
摘要： This invention relates to compounds of the Formula: (I); or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-α or combinations thereof.
摘要翻译：本发明涉及式（I）化合物：或其药学上可接受的盐，溶剂化物或异构体，其可用于治疗由MMP，ADAM，TACE，聚集蛋白聚糖蛋白酶，TNF-α或其组合介导的疾病或病症。

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