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1. 发明申请

WO2008089105A2 ANTIVIRAL NUCLEOSIDE ANALOGS 审中-公开
标题翻译：杀虫剂核苷类似物
公开(公告)号：WO2008089105A2
公开(公告)日：2008-07-24
申请号：PCT/US2008/050929
申请日：2008-01-11
申请人： BIOCRYST PHARMACEUTICALS, INC. , BABU, Yarlagadda S. , CHAND, Pooran , KUMAR, V. Satish , KOTIAN, Pravin L. , WU, Minwan
发明人： BABU, Yarlagadda S. , CHAND, Pooran , KUMAR, V. Satish , KOTIAN, Pravin L. , WU, Minwan
IPC分类号： C07H19/23 , A61K31/706 , A61P31/12 , A61P35/00
CPC分类号： C07H19/23
摘要： The invention provides compounds of Formula (I), as described herein, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates that are useful for preparing the compounds. The compounds of Formula (I) are useful as anti-viral agents and/or as anti-cancer agents.
摘要翻译：本发明提供如本文所述的式（I）化合物以及包含该化合物的药物组合物，以及可用于制备化合物的合成方法和中间体。式（I）的化合物可用作抗病毒剂和/或作为抗癌剂。

2. 发明申请

WO2006104945A2 HEPATITIS C THERAPIES 审中-公开
标题翻译：乙型肝炎治疗
公开(公告)号：WO2006104945A2
公开(公告)日：2006-10-05
申请号：PCT/US2006/010948
申请日：2006-03-23
申请人： BIOCRYST PHARMACEUTICALS, INC. , BABU, Yarlagadda, S. , CHAND, Pooran , WU, Minwan , KOTIAN, Pravin, L. , KUMAR, V., Satish , LIN, Tsu-Hsing , EL-KATTAN, Yahya , GHOSH, Ajit, K.
发明人： BABU, Yarlagadda, S. , CHAND, Pooran , WU, Minwan , KOTIAN, Pravin, L. , KUMAR, V., Satish , LIN, Tsu-Hsing , EL-KATTAN, Yahya , GHOSH, Ajit, K.
IPC分类号： A61K31/7064 , A61P31/12
CPC分类号： A61K31/7064 , A61K31/7056 , A61K31/7068 , A61K38/212 , A61K38/2292 , A61K45/06 , C07H7/06 , C07H11/04 , C07H19/22 , Y02A50/393 , Y02A50/465
摘要： The invention provides methods for treating hepatitis C viral infections and related viral infections, as well as compounds and compositions that are useful for treating such infections.
摘要翻译：本发明提供了治疗丙型肝炎病毒感染和相关病毒感染的方法，以及可用于治疗这种感染的化合物和组合物。

3. 发明申请

WO2006050161A2 THERAPEUTIC FUROPYRIMIDINES AND THIENOPYRIMIDINES 审中-公开
标题翻译：治疗性F ID ID IN。。。。。。。
公开(公告)号：WO2006050161A2
公开(公告)日：2006-05-11
申请号：PCT/US2005/039072
申请日：2005-10-28
申请人： BIOCRYST PHARMACEUTICALS, INC. , BABU, Yarlagadda, S. , CHAND, Pooran , WU, Minwan , KOTIAN, Pravin, L. , KUMAR, V., Satish , LIN, Tsu-hsing , EL-KATTAN, Yahya , GHOSH, Ajit, K.
发明人： BABU, Yarlagadda, S. , CHAND, Pooran , WU, Minwan , KOTIAN, Pravin, L. , KUMAR, V., Satish , LIN, Tsu-hsing , EL-KATTAN, Yahya , GHOSH, Ajit, K.
IPC分类号： A61K31/7076
CPC分类号： C07D495/04 , A61K31/675 , A61K31/7076 , A61K38/212 , A61K38/2292 , C07D491/048 , C07D493/04 , C07F9/6561 , C07H7/06 , C07H19/22 , Y02A50/393 , Y02A50/465 , A61K2300/00
摘要： The invention provides compounds of formula I, II, and III as described herein, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates that are useful for preparing the compounds. The compounds of formula I, II, and III are useful as anti-viral agents and/or as anti-cancer agents.
摘要翻译：本发明提供了本文所述的式I，II和III的化合物，以及包含该化合物的药物组合物，以及可用于制备化合物的合成方法和中间体。式I，II和III的化合物可用作抗病毒剂和/或作为抗癌剂。

4. 发明申请

WO2011031554A2 HETEROCYCLIC COMPOUNDS AS JANUS KINASE INHIBITORS 审中-公开
标题翻译：作为JANUS激酶抑制剂的杂环化合物
公开(公告)号：WO2011031554A2
公开(公告)日：2011-03-17
申请号：PCT/US2010/046999
申请日：2010-08-27
申请人： BIOCRYST PHARMACEUTICALS, INC. , BABU, Yarlagadda S. , KOTIAN, Pravin L. , KUMAR, V. Satish , WU, Minwan , LIN, Tsu-Hsing
发明人： BABU, Yarlagadda S. , KOTIAN, Pravin L. , KUMAR, V. Satish , WU, Minwan , LIN, Tsu-Hsing
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The invention provides compounds of formula (I) or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for suppressing an immune response or treating cancer or a hematologic malignancy using compounds of formula (I).
摘要翻译：本发明提供如本文所述的式（I）的化合物或其盐。本发明还提供了包含式（I）化合物的药物组合物，制备式（I）化合物的方法，可用于制备式I化合物的中间体和使用化合物抑制免疫应答或治疗癌症或血液恶性肿瘤的治疗方法的式（I）。

5. 发明申请

WO2011014817A1 PYRROLO [1, 2-B] PYRIDAZINE DERIVATIVES AS JANUS KINASE INHIBITORS 审中-公开
标题翻译：吡咯烷[1,2-B]吡嗪类衍生物作为JANUS KINASE INHIBITORS
公开(公告)号：WO2011014817A1
公开(公告)日：2011-02-03
申请号：PCT/US2010/043987
申请日：2010-07-30
申请人： BIOCRYST PHARMACEUTICALS, INC. , BABU, Yarlagadda S. , KOTIAN, Pravin L. , KUMAR, V. Satish , WU, Minwan , LIN, Tsu-Hsing
发明人： BABU, Yarlagadda S. , KOTIAN, Pravin L. , KUMAR, V. Satish , WU, Minwan , LIN, Tsu-Hsing
IPC分类号： C07D487/04 , A61K31/5025 , A61P35/00
CPC分类号： C07D487/04
摘要： The invention provides compounds of formula l: ( I ) or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for suppressing an immune response or treating cancer or a hematologic malignancy using compounds of formula I.
摘要翻译：本发明提供了本文所述的式I化合物或其盐。本发明还提供包含式I化合物的药物组合物，制备式I化合物的方法，可用于制备式I化合物的中间体和使用式I化合物抑制免疫应答或治疗癌症或血液恶性肿瘤的治疗方法。

6. 发明申请

WO2009111653A3 ANTIVIRAL THERAPEUTIC AGENTS 审中-公开
公开(公告)号：WO2009111653A3
公开(公告)日：2009-09-11
申请号：PCT/US2009/036213
申请日：2009-03-05
申请人： BIOCRYST PHARMACEUTICALS, INC. , BABU, Yarlagadda S. , CHAND, Pooran , KOTIAN, Pravin , WU, Minwan , KUMAR, V. Satish
发明人： BABU, Yarlagadda S. , CHAND, Pooran , KOTIAN, Pravin , WU, Minwan , KUMAR, V. Satish
IPC分类号： C12N9/99 , A61K31/7052 , A61P35/00 , C07D498/06 , C07D491/06 , C07D487/06
摘要： The invention provides compounds of Formula I: [Formula I] as described herein, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates that are useful for preparing the compounds. The compounds of Formula (I) are useful as anti-viral agents and/or as anti-cancer agents.

7. 发明申请

WO2011150356A1 HETEROCYCLIC COMPOUNDS AS JANUS KINASE INHIBITORS 审中-公开
标题翻译：杂环化合物作为JANUS KINASE INHIBITORS
公开(公告)号：WO2011150356A1
公开(公告)日：2011-12-01
申请号：PCT/US2011/038387
申请日：2011-05-27
申请人： BIOCRYST PHARMACEUTICALS, INC. , BABU, Yarlagadda, S. , KOTIAN, Pravin, L. , WU, Minwan
发明人： BABU, Yarlagadda, S. , KOTIAN, Pravin, L. , WU, Minwan
IPC分类号： C07D487/04 , A61P35/00 , A61K31/53 , A61K31/5025
CPC分类号： C07D487/04
摘要： The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for suppressing an immune response or treating cancer or a hematologic malignancy using compounds of formula I.
摘要翻译：本发明提供了本文所述的式I化合物或其盐。本发明还提供包含式I化合物的药物组合物，制备式I化合物的方法，可用于制备式I化合物的中间体和使用式I化合物抑制免疫应答或治疗癌症或血液恶性肿瘤的治疗方法。

8. 发明申请

WO2007002191A3 METHODS FOR THE PREPARATION OF 9-DEAZAPURINE DERIVATIVES 审中-公开
公开(公告)号：WO2007002191A3
公开(公告)日：2007-01-04
申请号：PCT/US2006/024134
申请日：2006-06-21
申请人： BIOCRYST PHARMACEUTICALS, INC. , CHAND, Pooran , WU, Minwan , KOTIAN, Pravin, L. , KUMAR, Satish, V. , LIN, Tsu-Hsing
发明人： CHAND, Pooran , WU, Minwan , KOTIAN, Pravin, L. , KUMAR, Satish, V. , LIN, Tsu-Hsing
IPC分类号： C07H21/00 , A01N43/04 , A61K31/70
摘要： Methods for the preparation of the isomer of a 9-deazapurine derivatives using benzyl protecting groups as the protecting groups for the 2 and 3 hydroxyl groups in ribose are provided.

9. 发明申请

WO2003087298A2 NUCLEOSIDES PREPARATION THEREOF AND USE AS INHIBITORS OF RNA VIRAL POLYMERASES 审中-公开
标题翻译：核苷酸的制备和用作RNA病毒聚合酶的抑制剂
公开(公告)号：WO2003087298A2
公开(公告)日：2003-10-23
申请号：PCT/US2002/036621
申请日：2002-11-14
申请人： BIOCRYST PHARMACEUTICALS, INC. , BABU, Yarlagadda, S. , CHAND, Pooran , EL-KATTAN, Yahya , WU, Minwan
发明人： BABU, Yarlagadda, S. , CHAND, Pooran , EL-KATTAN, Yahya , WU, Minwan
IPC分类号： C12N
CPC分类号： C07F9/65616 , A61K31/13 , A61K31/66 , A61K36/28 , A61K38/20 , A61K38/208 , A61K38/21 , A61K38/212 , C07F9/10 , C07F9/65121 , C07F9/65122 , Y02A50/393 , Y02A50/465 , A61K2300/00
摘要： Compounds represented by the formula ( I ) R is H, OH, alkyl, O-alkyl, CH 2 -O-alkyl, (CH 2 )nOH, (CH 2 )nNH 2 , (CH 2 )nCONH 2 , (CH 2 )nOOOH; R 1 is H, OH, alkyl, O-alkyl, CH 2 -O-alkyl, C 6 H 11 , CH 2 OH; R 2 is H, alkyl, OH, CH 2 OH, CH 2 -O-alkyl, CH(OH)-alkyl, CH(OH)CH 2 OH, CH 2 -halogen; R 3 and R 4 independently is H, OH, alkyl; Z is OR 5 , OR 6 , or aminoacids and esters thereof R 5 and R 6 independently is H, alkyl, aryl, pivaloyloxymethyl, C(R 7 ) 2 OC(O) X (R 8 )a formula ( I I ), R 7 independently is -H, C 1 -C 12 alkyl, C 5 C 12 aryl, C 2 -C 12 alkenyl, C 2 -C 12 alkynyl, C 7 -C 12 alkenylaryl, C 7 -C 12 alkynylaryl, or C 6 -C 12 alkaryl, any of which is unsubstituted or is substituted with 1 or 2 halo, cyano, azido, nitro, or -OR 9 ; R 9 is C 1 -C 12 alkyl, C 2 -C 12 alkenyl, C 2 -C 12 alkynyl or C 5 -C 12 aryl; provided that at least one R 8 is not H; and a is 1 when X is CH 2 , or direct bond, or 1 or 2 when X is N with the proviso that when a is 2 and X is N, (a) two N-linked R groups can be taken together to form a carbocyclic or oxygen containing heterocycle, (b) one N-linked R 8 additionally can be -OR 9 or (c) both N-linded R 8 groups can be -H; R 10 is H or C 1 -C 8 alkyl; R 11 is selected from H, alkyl, alkenyl, alkynyl, aryl, acyloxyalkyl, and pivaloyloxyalkyl n is 1-5 m is 0 to 5 X is S, N(R 8 ) or direct bond Y is O, S, N (R 8 ), and CHR 1 B is selected from the group consisting of adenine, guanine, cytosine, uracil, thymine, modified purines and pyrimidines such as inosin-9-yl, 2-amino-purin-9-yl, 2amino-6-chloro-purin-9-yl, 2-6-diamino-purin-9-yl, 3-carboxamido-1, 2, 4-triazol-1-yl, 3-deaza-adenin-9-yl, 3-deaza-guanin-9-yl, 3-deaza-inosin-9-yl, 3-deaza-2-amino-purin-9-yl, 3-deaza-2-amino-6-chloro-purin-9-yl, 3-deaza-2, 6-diamino-purin-9-yl, 7-deaza-adenin-9-yl, 7-deaza-guanin-9-yl, 7-deaza-inosin-9-yl, 7-deaza-2-amino-purin-9-yl, 7-deaza-2-amino-6-chloro-purin-9-yl, 7-deaza-2-6-diamino-purin-9-yl, 7-deaza-8-aza-adenin-9-yl, 7-deaza-8-aza-guanin-9-yl, 7-deaza-8-aza-inosnin-9-yl, 7-deaza-8-aza-2-amino-purin-9-yl, 7-deaza-8-aza-2-amino-6-chloro-purin-9-yl, 7-deaza-8-aza-2-6-diamino-purin-9-yl, -8-aza-adenin-9-yl,-8-aza-guanin-9-yl, -8-aza-inosnin-9-yl, -8-aza-2-amino-purin-9-yl, -8-aza-2-amino-6-chloro-purin-9-yl, -8-aza-2-6- diamino-purin-9-yl, 5-aza-thymin-1-yl, 5-aza-cytosin-1-yl, 5-aza-uracil-1-yl, 6-aza-thymin-1-yl, 6-aza-cytosin-1-yl, 6-aza-uracil-1-yl, 2-thiouracil-1-yl, 4-thiouracil-1-yl, 2 thiocytosine-1-yl, uracil-5-yl, 2-thiouracil-5-yl, 4-thiouracil-5-yl, substituted pyridine derivatives such as 6-azauracil, and azacyzosine. In general, attachment may be at different positions in the ring at nitrogen or carbon. These B ring systems may be substituted with halo, alkyl, substituted alkyl (F, C1, Br, I, OH), NH 2 , N 3 , aryl, substituted aryl (F, C1, Br, I, OH, NH 2 ), aralkyl; and pharmaceutically acceptable salts thereof and prodrugs thereof are provided.
摘要翻译：由式（I）R表示的化合物是H，OH，烷基，O-烷基，CH 2 -O-烷基，（CH 2）n OH，（CH 2）n NH 2，（CH 2）n CONH 2，（CH 2） R 1是H，OH，烷基，O-烷基，CH 2 -O-烷基，C 6 H 11，CH 2 OH; R 2是H，烷基，OH，CH 2 OH，CH 2 -O-烷基，CH（OH） - 烷基，CH（OH）CH 2 OH， R 3和R 4独立地是H，OH，烷基; Z为OR 5，OR 6或其氨基酸及其酯R 5和R 6独立地为H，烷基，芳基，新戊酰氧基甲基，C（R 7）2 OC（O）X（R 式（II）中，R 7独立地是-H，C 1 -C 12烷基，C 5 -C 12芳基，C 2 -C 12烯基，C 2 -C 12炔基，C 7 -C 12链烯基芳基，C 7 -C 12炔基芳基或C 6 -C 12炔基芳基， C 12烷芳基，其中任何一个是未取代的或被1或2个卤素，氰基，叠氮基，硝基或-OR 9取代; R 9是C 1 -C 12烷基，C 2 -C 12烯基，C 2 -C 12炔基或C 5 -C 12芳基; 条件是至少一个R 8不是H; 当X为CH 2或直接键合时，a为1，X为N时为1或2，条件是当a为2且X为N时，（a）两个N-连接的R基团可以一起形成碳环或含氧杂环，（b）一个N-连接的R 8另外可以是-OR 9或（c）两个N-烯键式R 8基团可以是-H; R 10是H或C 1 -C 8烷基; R 11选自H，烷基，烯基，炔基，芳基，酰氧基烷基和新戊酰氧基烷基n为1-5m为0至5 X为S，N（R 8）或直接键Y为O，S ，N（R 8）和CHR 1 B选自腺嘌呤，鸟嘌呤，胞嘧啶，尿嘧啶，胸腺嘧啶，修饰的嘌呤和嘧啶，例如肌内注射-9-基，2-氨基 - 嘌呤 - 2-氨基-6-氯 - 嘌呤-9-基，2-6-二氨基 - 嘌呤-9-基，3-甲酰胺基-1,2,4-三唑-1-基，3-脱氮腺嘌呤-9-基， 9-去氮杂 - 胍苷-9-基，3-脱氮-2-胍-9-基，3-脱氮-2-氨基 - 嘌呤-9-基，3-脱氮-2-氨基-6-嘌呤-9-基，嘌呤-9-基，3-脱氮-2,6-二氨基 - 嘌呤-9-基-7-去氮腺嘌呤-9-基-7-去氮 - 胍胍-9-基-7-氮杂 - 7-脱氮-2-氨基嘌呤-9-基，7-脱氮-2-氨基-6-氯 - 嘌呤-9-基-7-去氮杂-2-二氨基 - 嘌呤-9-基， 7-脱氮-8-氮杂腺嘌呤-9-基，7-脱氮-8-氮杂 - 鸟嘌呤-9-基，7-脱氮-8-氮杂 - 肌苷-9-基-7-去氮-8-氮杂 - 2-氨基 - 嘌呤-9-基，7-脱氮-8-氮杂-2-氨基-6-氯 - 嘌呤-9-基-7-去氮-8-氮杂-2-二氨基 - 嘌呤-9- 8-氮杂 - 腺嘌呤-9-基，-8-氮杂 - 鸟嘌呤-9-基，8-氮杂 - 肌苷三磷酸-9-基， -8-氮杂-2-氨基 - 嘌呤-9-基，-8-氮杂-2-氨基-6-氯 - 嘌呤-9-基，-8-氮杂-2-二氨基 - 嘌呤-9 5-氮杂 - 丝氨酸-1-基，5-氮杂 - 尿嘧啶-1-基，6-氮杂 - 甲氨基-1-基，6-氮杂 - 胞嘧啶-1-基，5-氮杂 - 2-氮杂尿嘧啶-1-基，2-硫尿嘧啶-1-基，4-硫尿嘧啶-1-基，2-硫代胞嘧啶-1-基，尿嘧啶-5-基，2-硫尿嘧啶-5-基， 4-硫尿嘧啶-5-基，取代的吡啶衍生物，例如6-氮尿嘧啶和氮杂胞苷。通常，连接可以在氮环境中的环或碳上的不同位置。这些B环体系可以被卤素，烷基，取代的烷基（F

10. 发明申请

WO2010011748A2 SYNTHETIC INTERMEDIATES AND PROCESSES 审中-公开
标题翻译：合成中间体和方法
公开(公告)号：WO2010011748A2
公开(公告)日：2010-01-28
申请号：PCT/US2009/051402
申请日：2009-07-22
申请人： BIOCRYST PHARMACEUTICALS, INC. , CHAND, Pooran , WU, Minwan , KOTIAN, Pravin, L. , KUMAR, V., Satish , LIN, Tsu-hsing
发明人： CHAND, Pooran , WU, Minwan , KOTIAN, Pravin, L. , KUMAR, V., Satish , LIN, Tsu-hsing
IPC分类号： C07D491/04
CPC分类号： C07D491/04
摘要： The invention provides novel synthetic intermediates and processes that can be used to prepare compounds of formula (I), wherein R 1 has any of the values described herein and R 2 is a nucleoside sugar group.
摘要翻译：本发明提供可用于制备式（I）化合物的新型合成中间体和方法，其中R 1具有本文所述的任何值，R 2为核苷糖基团。

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