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1. 发明申请

WO2011103441A1 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：WO2011103441A1
公开(公告)日：2011-08-25
申请号：PCT/US2011/025453
申请日：2011-02-18
申请人： SCHERING CORPORATION , SOUTHERN RESEARCH INSTITUTE , ARASAPPAN, Ashok , NJOROGE, George, F. , KWONG, Cecil, D. , ANANTHAN, Subramaniam , BENNETT, Frank , CLARK, Jeremy , GENG, Feng , GIRIJAVALLABHAN, Vinay, M. , HUANG, Yuhua , KEZAR, Hollis, S., III , MADDRY, Joseph, A. , REYNOLDS, Robert, C. , ROYCHOWDHURY, Abhijit , FOWLER, Anita, T. , SECRIST, John, A., III , KOZLOWSKI, Joseph, A. , SHANKAR, Bandarpalle, B. , TONG, Ling , KIM, Seong Heon , MACCOSS, Malcolm
发明人： ARASAPPAN, Ashok , NJOROGE, George, F. , KWONG, Cecil, D. , ANANTHAN, Subramaniam , BENNETT, Frank , CLARK, Jeremy , GENG, Feng , GIRIJAVALLABHAN, Vinay, M. , HUANG, Yuhua , KEZAR, Hollis, S., III , MADDRY, Joseph, A. , REYNOLDS, Robert, C. , ROYCHOWDHURY, Abhijit , FOWLER, Anita, T. , SECRIST, John, A., III , KOZLOWSKI, Joseph, A. , SHANKAR, Bandarpalle, B. , TONG, Ling , KIM, Seong Heon , MACCOSS, Malcolm
IPC分类号： A61K31/535
CPC分类号： A61K31/506 , A61K45/06 , C07D403/04 , C07D413/04 , C07D417/04 , C07D417/14 , C07D491/048 , C07D513/04
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 dieases 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。

2. 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).

3. 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。

4. 发明申请

WO2011046771A1 SUBSTITUTED PIPERIDINES THAT INCREASE p53 ACTIVITY AND THE USES THEREOF 审中-公开
标题翻译：增加p53活性的替代药物及其用途
公开(公告)号：WO2011046771A1
公开(公告)日：2011-04-21
申请号：PCT/US2010/051403
申请日：2010-10-05
申请人： SCHERING CORPORATION , BOGEN, Stephane, L. , MA, Yao , WANG, Yaolin , LAHUE, Brian Robert , NAIR, Latha, G. , SHIZUKA, Manami , VOSS, Matthew Ernst , KIROVA-SNOVER, Margarita , PAN, Weidong , TIAN, Yuan , KULKARNI, Bheemashankar, A. , GIBEAU, Craig, R. , LIU, Yuan , SCAPIN, Giovanna , RINDGEN, Diane , DOLL, Ronald, J. , GUZI, Timothy, J. , HICKLIN, Danny, J. , NOMEIR, Amin , SEIDEL-DUGAN, Cynthia , SHIPPS, Gerald, W., Jr. , MACCOSS, Malcolm
发明人： BOGEN, Stephane, L. , MA, Yao , WANG, Yaolin , LAHUE, Brian Robert , NAIR, Latha, G. , SHIZUKA, Manami , VOSS, Matthew Ernst , KIROVA-SNOVER, Margarita , PAN, Weidong , TIAN, Yuan , KULKARNI, Bheemashankar, A. , GIBEAU, Craig, R. , LIU, Yuan , SCAPIN, Giovanna , RINDGEN, Diane , DOLL, Ronald, J. , GUZI, Timothy, J. , HICKLIN, Danny, J. , NOMEIR, Amin , SEIDEL-DUGAN, Cynthia , SHIPPS, Gerald, W., Jr. , MACCOSS, Malcolm
IPC分类号： A01N43/40 , A61K31/445
CPC分类号： C07D401/14 , C07D409/14
摘要： The present invention provides a compound of Formula (1) as described herein or a pharmaceutically acceptable salt, solvate or ester thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.
摘要翻译：本发明提供本文所述的式（1）化合物或其药学上可接受的盐，溶剂合物或酯。该化合物可用作HDM2蛋白的抑制剂。还公开了包含上述化合物的药物组合物和使用其治疗癌症的方法。

5. 发明申请

WO2010117932A1 INDOLE DERIVATIVES AND METHODS FOR ANTIVIRAL TREATMENT 审中-公开
标题翻译：吲哚衍生物和抗病毒治疗方法
公开(公告)号：WO2010117932A1
公开(公告)日：2010-10-14
申请号：PCT/US2010/029923
申请日：2010-04-05
申请人： SCHERING CORPORATION , PTC THERAPEUTICS, INC , MACCOSS, Malcolm , NJOROGE, F., George , NOMEIR, Amin , CHEN, Guangming , HUANG, Song, Xiao , KAKARLA, Ramesh , KARP, Gary, Mitchell , LENNOX, William, Joseph , LI, Chunshi , LIU, Ronggang , LIU, Yalei , MORRILL, Christie , PAGET, Steven, D. , SMITH, Sean, W. , TAKASUGI, James , TURPOFF, Anthony, A. , REN, Hongyu , ZHANG, Nanjing , ZHANG, Xiaoyan , ZHU, Jin
发明人： MACCOSS, Malcolm , NJOROGE, F., George , NOMEIR, Amin , CHEN, Guangming , HUANG, Song, Xiao , KAKARLA, Ramesh , KARP, Gary, Mitchell , LENNOX, William, Joseph , LI, Chunshi , LIU, Ronggang , LIU, Yalei , MORRILL, Christie , PAGET, Steven, D. , SMITH, Sean, W. , TAKASUGI, James , TURPOFF, Anthony, A. , REN, Hongyu , ZHANG, Nanjing , ZHANG, Xiaoyan , ZHU, Jin
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , A61P31/12 , A61K31/4439 , A61K31/444 , A61K31/4436 , A61K31/443 , A61K31/4433 , A61K31/506
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention is directed to compounds 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化合物及其形式和药物组合物。

6. 发明申请

WO2010056722A1 GAMMA SECRETASE MODULATORS 审中-公开
标题翻译： GAMMA秘密调节器
公开(公告)号：WO2010056722A1
公开(公告)日：2010-05-20
申请号：PCT/US2009/063993
申请日：2009-11-11
申请人： SCHERING CORPORATION , ZHU, Zhaoning , GREENLEE, William, J. , LI, Hongmei , VICAREL, Monica, L. , QIN, Jun , DHONDI, Pawan, Kumar , HUANG, Xianhai , PALANI, Anandan , LIU, Xiaoxiang , SUN, Zhong-Yue , JOSIEN, Hubert B. , XU, Ruo , COLE, David, James , BURNETT, Duane, A. , BENNETT, Chad, E. , MCCRACKEN, Troy, M. , MACCOSS, Malcolm
发明人： ZHU, Zhaoning , GREENLEE, William, J. , LI, Hongmei , VICAREL, Monica, L. , QIN, Jun , DHONDI, Pawan, Kumar , HUANG, Xianhai , PALANI, Anandan , LIU, Xiaoxiang , SUN, Zhong-Yue , JOSIEN, Hubert B. , XU, Ruo , COLE, David, James , BURNETT, Duane, A. , BENNETT, Chad, E. , MCCRACKEN, Troy, M. , MACCOSS, Malcolm
IPC分类号： C07D409/14 , C07D413/10 , C07D498/04 , C07D498/14 , C07D498/20 , A61K31/5395 , A61K31/553 , A61P25/28
CPC分类号： C07D498/04 , C07D409/14 , C07D413/10 , C07D498/14 , C07D498/20
摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system 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下式杂环化合物：作为γ-分泌酶的调节剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备包含一种或多种这样的化合物的药物制剂的方法化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与中枢神经系统相关的一种或多种疾病的方法。

7. 发明申请

WO2006065335A2 FLUORINATED PYRROLO[2,3-D]PYRIMIDINE NUCLEOSIDES FOR THE TREATMENT OF RNA-DEPENDENT RNA VIRAL INFECTION 审中-公开
标题翻译：氟化吡咯并[2,3-D]嘧啶核苷用于治疗RNA依赖性RNA病毒感染
公开(公告)号：WO2006065335A2
公开(公告)日：2006-06-22
申请号：PCT/US2005/037224
申请日：2005-10-17
申请人： MERCK & CO., INC. , MACCOSS, Malcolm , OLSEN, David, B. , LEONE, Joseph , DURETTE, Philippe, L.
发明人： MACCOSS, Malcolm , OLSEN, David, B. , LEONE, Joseph , DURETTE, Philippe, L.
IPC分类号： A61K31/7072 , A61K31/519
CPC分类号： C07H19/14
摘要： The present invention provides fluorinated pyrrolo[2,3, d ]pyrimidine nucleoside compounds which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaeutical compositions containing such fluorinated pyrrolo[2,3- d ]pyrimidine nucleoside alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the fluorinated pyrrolo[2,3- d ]pyrimidine nucleoside of the present invention.
摘要翻译：本发明提供氟化吡咯并[2,3，d]嘧啶核苷化合物，其是RNA依赖性RNA病毒聚合酶的抑制剂。这些化合物是RNA依赖性RNA病毒复制的抑制剂，并且可用于治疗RNA依赖性RNA病毒感染。它们作为丙型肝炎病毒（HCV）NS5B聚合酶抑制剂的前体特别有用，作为HCV复制抑制剂的前体和/或用于治疗丙型肝炎感染。本发明还描述了含有这种氟化吡咯并[2,3-d]嘧啶核苷的药物组合物，所述组合物单独或与其他活性物质联合用于抗RNA依赖性RNA病毒感染，特别是HCV感染。还公开了用氟化吡咯并[2,3-d]嘧啶核苷抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。本发明。

8. 发明申请

WO2006049933A3 COMPOSITIONS AND METHODS FOR THE TREATMENT OF OBESITY AND SEXUAL DYSFUNCTION 审中-公开
公开(公告)号：WO2006049933A3
公开(公告)日：2006-05-11
申请号：PCT/US2005/038194
申请日：2005-10-25
申请人： MERCK & CO., INC. , MACCOSS, Malcolm , MACINTYRE, Duncan, E. , STRACK, Alison, M.
发明人： MACCOSS, Malcolm , MACINTYRE, Duncan, E. , STRACK, Alison, M.
IPC分类号： A61K38/00 , A61K31/675 , A61K31/535 , A61K31/445 , A61K31/235 , A61K31/24 , A61K31/135
摘要： The present invention relates to methods of treating and preventing obesity and obesity-related disorders in a subject comprising administering a neurokinin-1 antagonist and an anti-obesity agent, such as a melanocortin 4 receptor agonist, to said subject. The present invention further relates to methods of treating or preventing sexual dysfunction, including male erectile dysfunction, in a subject comprising administering a neurokinin-1 antagonist and a sexual dysfunction therapeutic agent, such as a melanocortin 4 receptor agonist, to said subject. The present invention further provides for pharmaceutical compositions and medicaments useful in carrying out these methods.

9. 发明申请

WO2003105770A3 CARBOCYCLIC NUCLEOSIDE ANALOGS AS RNA-ANTIVIRALS 审中-公开
公开(公告)号：WO2003105770A3
公开(公告)日：2003-12-24
申请号：PCT/US2003/018841
申请日：2003-06-14
申请人： MERCK & CO., INC. , ISIS PHARMACEUTICALS, INC. , BHAT, Balkrishen , BHAT, Neelima , DANDE, Prasad , ELDRUP, Anne, B. , OLSEN, David, B. , MACCOSS, Malcolm
发明人： BHAT, Balkrishen , BHAT, Neelima , DANDE, Prasad , ELDRUP, Anne, B. , OLSEN, David, B. , MACCOSS, Malcolm
IPC分类号： C07D473/00
摘要： The present invention provides carbocyclic nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such carbocyclic nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the carbocyclic nucleoside compounds of the present invention

10. 发明申请

WO2002057287A3 NUCLEOSIDE DERIVATIVES AS INHIBITORS OF RNA-DEPENDENT RNA VIRAL POLYMERASE 审中-公开
公开(公告)号：WO2002057287A3
公开(公告)日：2002-07-25
申请号：PCT/US2002/003086
申请日：2002-01-18
申请人： MERCK & CO., INC. , ISIS PHARMACEUTICALS, INC. , CARROLL, Steven, S. , MACCOSS, Malcolm , OLSEN, David, B. , BHAT, Balkrishen , BHAT, Neelima , COOK, Phillip Dan , ELDRUP, Anne, B. , PRAKASH, Thazha, P. , PRHAVC, Marija , SONG, Quanlai
发明人： CARROLL, Steven, S. , MACCOSS, Malcolm , OLSEN, David, B. , BHAT, Balkrishen , BHAT, Neelima , COOK, Phillip Dan , ELDRUP, Anne, B. , PRAKASH, Thazha, P. , PRHAVC, Marija , SONG, Quanlai
IPC分类号： C07H19/14
摘要： The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.

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