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1. 发明申请

WO2010132513A1 2'-FLUORO ARABINO NUCLEOSIDES AND USE THEREOF 审中-公开
标题翻译： 2-FLUORO ARABINO NUCLEOSIDES及其用途
公开(公告)号：WO2010132513A1
公开(公告)日：2010-11-18
申请号：PCT/US2010/034463
申请日：2010-05-12
申请人： SOUTHERN RESEARCH INSTITUTE , SECRIST, John A., III , FOWLER, Anita T. , TIWARI, Kamal N.
发明人： SECRIST, John A., III , FOWLER, Anita T. , TIWARI, Kamal N.
IPC分类号： C07H19/00
CPC分类号： C07H19/09 , C07H19/06 , C07H19/12 , C07H19/16 , C07H19/19
摘要： A method of treating cancer using certain 2'-fluoro arabino nucleosides is provided. Also provided are compounds represented by the formula: ( I & A) wherein R is alkyl; and pharmaceutically acceptable salts thereof; and pharmaceutical compositions containing these compounds.
摘要翻译：提供了使用某些2'-阿拉伯核苷治疗癌症的方法。还提供了由下式表示的化合物：（I＆A）其中R是烷基; 及其药学上可接受的盐; 和含有这些化合物的药物组合物。

2. 发明申请

WO0038668A3 USE OF A NITROSOUREA DERIVATIVE FOR PREVENTION OR TREATMENT OF ACUTE ALLOGRAFT REJECTION 审中-公开
标题翻译：使用NITROSOUREA衍生物预防或治疗急性乙型肝炎病毒
公开(公告)号：WO0038668A3
公开(公告)日：2000-12-07
申请号：PCT/US9930985
申请日：1999-12-28
申请人： SOUTHERN RES INST , BLATTER HERBERT M , KAHN DONALD R , PIPER JAMES R , SECRIST JOHN A III , STRUCK ROBERT F , TEMPLE CARROLL
发明人： BLATTER HERBERT M , KAHN DONALD R , PIPER JAMES R , SECRIST JOHN A III , STRUCK ROBERT F , TEMPLE CARROLL
IPC分类号： A61K31/175 , A61K31/45 , A61K31/17 , A61K31/445 , A61K31/4468 , A61P37/06
CPC分类号： A61K31/175 , A61K31/45 , Y10S514/885
摘要： A method for treating an organ donor prior to harvesting organ to reduce graft rejection in a recipient. An amount effective to reduce graft rejection of at least one compound selected from the group consisting of compounds having formulae (I), (II), (III), (IV), (V), (VI), and (VII) is administered to the organ donor, wherein Y is (a); X is F or Cl; R1 is a straight or branched alkyl group having from 1 to 7 carbon atoms; R2 is a straight or branched alkyl group having from 1 to 7 carbon atoms; R3 is H or a straight or branched alkyl group having from 1 to 7 carbon atoms; Z is H, OH, or a straight or branched alkyl group including from 1 to 7 carbon atoms; and in Formula (II), the OH groups may be substituted anywhere except where Y is present and are not on the same carbon atom; in Formula (III), the OH group may be substituted anywhere except where Y is present; in Formula (IV), the OH group may be substituted anywhere except where Y is present; in Formula (V), Z may be substituted anywhere except at C-1, C-6, and C-4 if Z is OH; in Formula (VI), Z may be substituted anywhere except at C-1, C-3, and C-5 if Z is OH; and in Formula (VII), Z may be at C-1, C-2, and C-3 except not on C-1 if Z is OH.
摘要翻译：在收获器官之前处理器官供体以减少受体中的移植物排斥的方法。降低至少一种选自具有式（I），（II），（III），（IV），（V），（VI）和（VII）的化合物的化合物的移植排斥反应的量）给予器官供体，其中Y为（a）; X是F或Cl; R1是具有1至7个碳原子的直链或支链烷基; R2是具有1至7个碳原子的直链或支链烷基; R3是H或具有1至7个碳原子的直链或支链烷基; Z是H，OH或包含1至7个碳原子的直链或支链烷基; 在式（II）中，除了存在Y并且不在相同碳原子上之外，OH基团可以被取代; 在式（III）中，除了存在Y之外，OH基团可以被取代; 在式（IV）中，除了存在Y之外，OH基团可以被取代; 在式（Ⅴ）中，如果Z是OH，则Z可以在C-1，C-6和C-4之外的任何地方被取代; 在式（VI）中，Z可以在C 1，C 3和C 5上的任何地方被取代，如果Z是OH; 并且在式（VII）中，Z可以是C-1，C-2和C-3，但如果Z是OH，则不在C-1上。

3. 发明申请

WO0166118A8 4'-THIO-L-XYLO FURANOSYL NUCLEOSIDES, PRECURSORS THEREOF, PREPARATION AND USE THEREOF 审中-公开
标题翻译： 4'-THIO-L-XYLO FURANOSYL NUCLEOSIDES，其前身，其制备和使用
公开(公告)号：WO0166118A8
公开(公告)日：2001-12-06
申请号：PCT/US0107323
申请日：2001-03-08
申请人： SOUTHERN RES INST , SECRIST JOHN A III , TIWARI KAMAL N , MONTGOMERY JOHN A
发明人： SECRIST JOHN A III , TIWARI KAMAL N , MONTGOMERY JOHN A
IPC分类号： C07H19/06 , C07H19/16 , A61K31/70 , C07H19/173
CPC分类号： C07H19/06 , A61K31/4436 , A61K31/519 , A61K31/522 , A61K31/53 , C07H19/16
摘要： 4'-Thio-L-Xylo furanosyl nucleosides can be used as anti-cancer agents, or antiviral agents or to inhibit DNA replication.
摘要翻译： 4'-硫代-L-木糖呋喃糖基核苷可用作抗癌剂或抗病毒剂或抑制DNA复制。

4. 发明申请

WO2009018541A8 5'-SUBSTITUTED ADENOSYNES, PREPARATION THEREOF AND USE AS INHIBITORS OF S-ADENOSYLMETHIONINE DECARBOXYLASE 审中-公开
标题翻译： 5'-取代腺苷，其制备方法和用作S-腺嘧啶脱乙酰酶的抑制剂
公开(公告)号：WO2009018541A8
公开(公告)日：2010-03-04
申请号：PCT/US2008071999
申请日：2008-08-01
申请人： SOUTHERN RES INST , UNIV CORNELL , PENN STATE RES FOUND , H LEE MOFFITT CANCER CT AND RE , SECRIST JOHN A III , EALICK STEVE , BALE SHRIDHAR , PEGG ANTHONY E , MCCLOSKEY DIANE E , GUIDA WAYNE C
发明人： SECRIST JOHN A III , EALICK STEVE , BALE SHRIDHAR , PEGG ANTHONY E , MCCLOSKEY DIANE E , GUIDA WAYNE C
IPC分类号： A01N43/04
CPC分类号： C07H19/167 , A61K9/20
摘要： The crystal structure of the complex of S-adenosylmethionine methyl ester with h?doMetDC F223A, a mutant where the stacking of the aromatic rings of F7, adenine and F223 would be eliminated. The structure of this mutant with the ester shows that the ligand still maintains a syn conformation aided by pi-pi interactions to F7, hydrogen bonds to the backbone of Glu67, and electrostatic interactions. Several series of AdoMet substrate analogues with a variety of substituents at the 8 position of adenine were synthesized and analyzed for their ability to inhibit hAdoMetDC. To understand these results, virtual modeling of the enzyme inhibitor complexes and the crystal structures of human AdoMetDC with 5'-deoxy-5'-[N-methyl-N-[2- (aminooxy)ethyl]amino-8-rnethyl]adenosine (MAOEMA) and 5'-deoxy-5'-[N-methyl-N-[4- (aminooxy)butyl]amino-8-ethyl]adenosine (MAOBEA) at the active site have been determined experimentally.
摘要翻译： S-腺苷甲硫氨酸甲酯与h？doMetDC F223A的复合物的晶体结构，其中F7，腺嘌呤和F223的芳环的堆叠将被消除。该突变体与酯的结构显示配体仍然保持通过与F7的π-π相互作用，与Glu67的主链的氢键和静电相互作用的顺序构象。合成了多个在腺嘌呤8位具有多种取代基的AdoMet底物类似物，并分析其抑制hAdoMetDC的能力。为了理解这些结果，使用5'-脱氧-5' - [N-甲基-N- [2-（氨基氧基）乙基]氨基-8-甲基]腺苷的酶抑制剂复合物和人AdoMetDC的晶体结构的虚拟建模（MAOEMA）和5'-脱氧-5' - [N-甲基-N- [4-（氨基氧基）丁基]氨基-8-乙基]腺苷（MAOBEA）在活性位点已经通过实验测定。

5. 发明申请

WO2009018541A1 5'-SUBSTITUTED ADENOSYNES, PREPARATION THEREOF AND USE AS INHIBITORS OF S-ADENOSYLMETHIONINE DECARBOXYLASE 审中-公开
标题翻译： 5'-取代腺苷，其制备方法和用作S-腺嘧啶脱乙酰酶的抑制剂
公开(公告)号：WO2009018541A1
公开(公告)日：2009-02-05
申请号：PCT/US2008/071999
申请日：2008-08-01
申请人： SOUTHERN RESEARCH INSTITUTE , CORNELL UNIVERSITY , PENNSYLVANIA STATE UNIVERSITY , R. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC. , SECRIST, John, A., III , EALICK, Steve , BALE, Shridhar , PEGG, Anthony, E. , MCCLOSKEY, Diane, E. , GUIDA, Wayne, C
发明人： SECRIST, John, A., III , EALICK, Steve , BALE, Shridhar , PEGG, Anthony, E. , MCCLOSKEY, Diane, E. , GUIDA, Wayne, C
IPC分类号： A01N43/04
CPC分类号： C07H19/167 , A61K9/20 , Y02A50/411
摘要： The crystal structure of the complex of S-adenosylmethionine methyl ester with hΛdoMetDC F223A, a mutant where the stacking of the aromatic rings of F7, adenine and F223 would be eliminated. The structure of this mutant with the ester shows that the ligand still maintains a syn conformation aided by pi-pi interactions to F7, hydrogen bonds to the backbone of Glu67, and electrostatic interactions. Several series of AdoMet substrate analogues with a variety of substituents at the 8 position of adenine were synthesized and analyzed for their ability to inhibit hAdoMetDC. To understand these results, virtual modeling of the enzyme inhibitor complexes and the crystal structures of human AdoMetDC with 5'-deoxy-5'-[N-methyl-N-[2- (aminooxy)ethyl]amino-8-rnethyl]adenosine (MAOEMA) and 5'-deoxy-5'-[N-methyl-N-[4- (aminooxy)butyl]amino-8-ethyl]adenosine (MAOBEA) at the active site have been determined experimentally.
摘要翻译： S-腺苷甲硫氨酸甲酯与h？doMetDC F223A的复合物的晶体结构，其中F7，腺嘌呤和F223的芳环的堆叠将被消除。该突变体与酯的结构显示配体仍然保持通过与F7的π-π相互作用，与Glu67的主链的氢键和静电相互作用的顺序构象。合成了多个在腺嘌呤8位具有多种取代基的AdoMet底物类似物，并分析其抑制hAdoMetDC的能力。为了理解这些结果，使用5'-脱氧-5' - [N-甲基-N- [2-（氨基氧基）乙基]氨基-8-甲基]腺苷的酶抑制剂复合物和人AdoMetDC的晶体结构的虚拟建模（MAOEMA）和5'-脱氧-5' - [N-甲基-N- [4-（氨基氧基）丁基]氨基-8-乙基]腺苷（MAOBEA）在活性位点已经通过实验测定。

6. 发明申请

WO2009114651A3 USE OF '-THIO-2'-DEOXYNUCLEOSIDES AS ANRI ORTHOPOXVIRUS AGENTS 审中-公开
标题翻译： '二硫代脱氧核糖核苷酸作为角叉菜病毒剂使用
公开(公告)号：WO2009114651A3
公开(公告)日：2010-03-18
申请号：PCT/US2009036869
申请日：2009-03-12
申请人： SOUTHERN RES INST , SECRIST JOHN A III , TIWARI KAMAL N , MADDRY JOSEPH A
发明人： SECRIST JOHN A III , TIWARI KAMAL N , MADDRY JOSEPH A
IPC分类号： A01N43/04
CPC分类号： A61K31/513 , A61K9/2054 , A61K9/4858 , A61K9/4866 , A61K2300/00
摘要： Compound represented by the formulae: wherein each R individually is H or aliphatic acyl or aromatic acyl group; X is selected from the group consisting of hydrogen, fiuoro, chloro, bromo, iodo, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, cyano, aryl and nitro; pharmaceutically acceptable salts thereof, prodrugs thereof and mixtures thereof are used as inhibitors of orthopoxviruses and for treating patients suffering from an orthopoxvirus infection such as, but not limited to, smallpox, cowpox, monkeypox and camelpox.
摘要翻译：由下式表示的化合物：其中每个R各自为H或脂族酰基或芳族酰基; X选自氢，氟，氯，溴，碘，烷氧基，烷基，卤代烷基，烯基，卤代烯基，炔基，氨基，单烷基氨基，二烷基氨基，氰基，芳基和硝基。其药学上可接受的盐，其前药及其混合物用作正痘病毒的抑制剂并用于治疗患有正痘病毒感染的患者，例如但不限于天花，牛痘，猴痘和骆驼痘。

7. 发明申请

WO2009114651A8 USE OF '-THIO-2'-DEOXYNUCLEOSIDES AS ANRI ORTHOPOXVIRUS AGENTS 审中-公开
标题翻译： '二硫代脱氧核糖核苷酸作为角叉菜病毒剂使用
公开(公告)号：WO2009114651A8
公开(公告)日：2009-12-03
申请号：PCT/US2009036869
申请日：2009-03-12
申请人： SOUTHERN RES INST , SECRIST JOHN A III , TIWARI KAMAL N , MADDRY JOSEPH A
发明人： SECRIST JOHN A III , TIWARI KAMAL N , MADDRY JOSEPH A
IPC分类号： A61K31/513
CPC分类号： A61K31/513 , A61K9/2054 , A61K9/4858 , A61K9/4866 , A61K2300/00
摘要： Compound represented by the formulae: wherein each R individually is H or aliphatic acyl or aromatic acyl group; X is selected from the group consisting of hydrogen, fiuoro, chloro, bromo, iodo, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, cyano, aryl and nitro; pharmaceutically acceptable salts thereof, prodrugs thereof and mixtures thereof are used as inhibitors of orthopoxviruses and for treating patients suffering from an orthopoxvirus infection such as, but not limited to, smallpox, cowpox, monkeypox and camelpox.
摘要翻译：由下式表示的化合物：其中每个R各自为H或脂族酰基或芳族酰基; X选自氢，氟，氯，溴，碘，烷氧基，烷基，卤代烷基，烯基，卤代烯基，炔基，氨基，单烷基氨基，二烷基氨基，氰基，芳基和硝基。其药学上可接受的盐，其前药及其混合物用作正痘病毒的抑制剂并用于治疗患有正痘病毒感染的患者，例如但不限于天花，牛痘，猴痘和骆驼痘。

8. 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。

9. 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。

10. 发明申请

WO2003035012A3 MUTANT PURINE NUCLEOSIDE PHOSPHORYLASE PROTEINS AND CELLULAR DELIVERY THEREOF 审中-公开
公开(公告)号：WO2003035012A3
公开(公告)日：2003-05-01
申请号：PCT/US2002/034626
申请日：2002-10-28
申请人： UAB RESEARCH FOUNDATION , SOUTHERN RESEARCH INSTITUTE , CORNELL RESEARCH FOUNDATION, INC. , EALICK, Steven, E. , PARKER, William, B. , SECRIST, John, A., III , SORSCHER, Eric, J.
发明人： EALICK, Steven, E. , PARKER, William, B. , SECRIST, John, A., III , SORSCHER, Eric, J.
IPC分类号： C12N9/12
摘要： A host cell stably transformed or transfected by a vector including a DNA sequence encoding for mutant purine nucleoside cleavage enzymes is provided. The transformed or transfected host cell can be used in combination with a purine substrate to treat tumour cells and/or virally infected cells. A nucleotide sequence encoding mutant E. coli derived purine nucleoside phosphorylase proteins which can be used in conjunction with an appropriate substrate to produce toxins which impair abnormal cell growth is also provided. A method is detailed for the delivery of toxin by generation withing target cells or by administration and delivery to the cells from without. Novel purine nucleosides are detailed that yield a cytotoxic purine upn enzymatic cleavage. A synthetic process for nucleosides is also detailed.

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