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1. 发明申请

WO2009076455A2 METHODS OF TREATING HEMATOLOGIC CANCERS 审中-公开
标题翻译：治疗肝癌的方法
公开(公告)号：WO2009076455A2
公开(公告)日：2009-06-18
申请号：PCT/US2008086256
申请日：2008-12-10
申请人： BIOCRYST PHARM INC , BANTIA SHANTA , BREITFELD PHILIP , BABU YARLAGADDA S
发明人： BANTIA SHANTA , BREITFELD PHILIP , BABU YARLAGADDA S
IPC分类号： A61K31/4184 , A61K31/4745 , A61K35/00 , A61K39/395 , A61K45/06 , A61P35/02
CPC分类号： A61K31/519 , A61K31/4184 , A61K31/7076 , A61K39/39541 , A61K39/3955 , A61K39/39558 , A61K45/06 , A61K2039/545 , C07K16/2887 , A61K2300/00
摘要： The present application relates to treatment of hematologic cancers, which treatments can include, e.g., administration of a purine nucleoside phosphorylase (PNP) inhibitor, an alkylating agent and/or an anti-CD20 agent, and related compositions and kits.
摘要翻译：本申请涉及血液癌的治疗，该治疗可以包括例如给予嘌呤核苷磷酸化酶（PNP）抑制剂，烷化剂和/或抗CD20剂，以及相关组合物和试剂盒。

2. 发明申请

WO2008141079A1 TETRAHYDROFURO [3 4-D] DIOXOLANE COMPOUNDS FOR USE IN THE TREATMENT OF VIRAL INFECTIONS AND CANCER 审中-公开
标题翻译：四氢呋喃[3 4-D]二恶唑化合物用于治疗病毒感染和癌症
公开(公告)号：WO2008141079A1
公开(公告)日：2008-11-20
申请号：PCT/US2008/063037
申请日：2008-05-08
申请人： BIOCRYST PHARMACEUTICALS, INC. , BABU, Yarlagadda, S. , CHAND, Pooran
发明人： BABU, Yarlagadda, S. , CHAND, Pooran
IPC分类号： C07D519/00 , A61K31/519 , A61P35/00 , A61P31/12
CPC分类号： C07D519/00
摘要： The invention provides compounds of formula (I), as described herein, or pharmaceutically acceptable salts thereof, 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）化合物或其药学上可接受的盐，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。

3. 发明申请

WO2006014913A3 INHIBITORS OF 5'-METHYLTHIOADENOSINE PHOSPHORYLASE AND 5'METHYLTHIOADENOSINE/S-ADENOSYLHOMOCYSTEINE NUCLEOSIDASE 审中-公开
标题翻译： 5'-甲基硫代腺苷磷酸化酶和5'-甲基硫代腺苷/ S-腺苷核糖核苷酸
公开(公告)号：WO2006014913A3
公开(公告)日：2006-12-14
申请号：PCT/US2005026419
申请日：2005-07-26
申请人： BIOCRYST PHARM INC , BABU YARLAGADDA S , KAMATH VIVEKANAND P , MORRIS JR PHILIP E
发明人： BABU YARLAGADDA S , KAMATH VIVEKANAND P , MORRIS JR PHILIP E
IPC分类号： C07D487/04 , A61K31/4015 , A61K31/4025 , A61K31/506 , A61K31/519 , C07D207/12 , C07D207/22 , C07D239/32 , C07D239/42 , C07D239/47 , C07D239/48 , C07D239/50
CPC分类号： C07D487/04
摘要： Described are compounds of the general formula (I), VI and (VII). Also described are pharmaceutical compositions comprising the compounds identified. The compounds and pharmaceutical compositions described are inhibitors of 5'-methylthioadenosine/S-adenosylhomocystein nucleosidase (MTAN) and/or 5'-methylthioadenosine phosphorylase (MTAP). Methods of treatment using the compounds and pharmaceutical compositions described are also provided for preventing and/or treating disease states and/or conditions by inhibiting MTAN and/or MTAP in patients.
摘要翻译：描述了通式（I），VI和（VII）的化合物。还描述了包含所鉴定的化合物的药物组合物。所述化合物和药物组合物是5'-甲硫腺苷/ S-腺苷高小核糖核苷酸酶（MTAN）和/或5'-甲硫腺苷磷酸化酶（MTAP）的抑制剂。还提供了使用所述化合物和药物组合物治疗的方法，用于通过抑制患者中的MTAN和/或MTAP来预防和/或治疗疾病状态和/或病症。

4. 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。

5. 发明申请

WO2013033093A1 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：WO2013033093A1
公开(公告)日：2013-03-07
申请号：PCT/US2012/052657
申请日：2012-08-28
申请人： BIOCRYST PHARMACEUTICALS, INC. , BABU, Yarlagadda, S. , KOTIAN, Pravin, L. , CHINTAREDDY, Venkat, R.
发明人： BABU, Yarlagadda, S. , KOTIAN, Pravin, L. , CHINTAREDDY, Venkat, R.
IPC分类号： C07D487/16
CPC分类号： C07D487/16 , C07D491/22 , C07D495/22
摘要： The invention provides compounds of formula I: (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, including 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化合物的中间体和用于抑制免疫应答或治疗癌症（包括血液恶性肿瘤）的治疗方法，使用式一世。

6. 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。

7. 发明申请

WO2011079230A3 HETEROCYCLIC COMPOUNDS AS JANUS KINASE INHIBITORS 审中-公开
公开(公告)号：WO2011079230A3
公开(公告)日：2011-06-30
申请号：PCT/US2010/061912
申请日：2010-12-22
申请人： BIOCRYST PHARMACEUTICALS, INC. , BABU, Yarlagadda, S. , KOTIAN, Pravin, L.
发明人： BABU, Yarlagadda, S. , KOTIAN, Pravin, L.
IPC分类号： C07D491/048 , A61K31/519 , A61P35/00
摘要： The invention provides compounds of formula (I): (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).

8. 发明申请

WO2004106350A1 NUCLEOSIDE ANALOGS AS VIRAL POLYMERASE INHIBITORS 审中-公开
标题翻译：核苷类似物作为病毒聚合酶抑制剂
公开(公告)号：WO2004106350A1
公开(公告)日：2004-12-09
申请号：PCT/US2003/015169
申请日：2003-05-14
申请人： BIOCRYST PHARMACEUTICAL, INC. , CHAND, Pooran , BABU, Yarlagadda, S. , EL-KATTAN, Yahya , WU, Minwan
发明人： CHAND, Pooran , BABU, Yarlagadda, S. , EL-KATTAN, Yahya , WU, Minwan
IPC分类号： C07F9/6561
CPC分类号： C07F9/65616 , C07F9/65121 , C07F9/6561
摘要： Compounds represented by the formula (I) HC(A)(B)(CH 2 ).-Y-CH2~P(=W)Z'Z Wherein A is -(CH 2 )~R, -CH =CH 2 , -CH 2 --CH =CH 2 , O-(CH 2 )~R,-CH(OH)CH 3 ,- CH(OH)-CH 2 0H,-CH 2 -CH(OH)CH 3 ,-CH 2 -CH(OH)-CH 2 0H,-CH(OH)-CH(OH)-CH 3 ; R is H, OH, F, N 3 , NH 2 , C0 2 H, SH, alkyl, S-alkyl, O-acyl, CONH 2 , CONH-alkyl; Z and Z' independently is OR 1 , OR 2 , O-(CH 2 )~O-alkyl or aniinoacids and esters thereof; R 1 and R 2 independently is H, alkyl, aryl, pivaloyloxymethyl, phthalyl or substituted phthalyl, C(R 3 ) 2 0C(O) X (R 4 )a, P(O)(OR 7 ) 2 , or -P(O)(OR 7 ) 2 or -O-P(O)(OR 7 ) 2 R 6 is H or C 1 -C 8 alkyl; R 7 is selected from H, alkyl, alkenyl, alkynyl, aryl, acyloxyalkyl, and pivaloyioxyalkyl; n is 1-3; Y is 0, S or NH; W is 0 or S; B is selected from the group consisting of adenine, guanine, cytosine, uracil, thymine, modified purines, pyrimidines and pyridines are provided.
摘要翻译：由式（I）表示的化合物（A）（B）（CH2）-Y-CH2-P（= W）Z'Z其中A是 - （CH2）-R，-CH = CH2，-CH2- -CH = CH 2，O-（CH 2）-R，-CH（OH）CH 3，-CH（OH）-CH 2 OH，-CH 2 -CH（OH）CH 3，-CH 2 -CH（OH）-CH 2 OH， OH）-CH（OH）-CH 3; R为H，OH，F，N 3，NH 2，CO 2 H，SH，烷基，S-烷基，O-酰基，CONH 2，CONH-烷基; Z和Z'独立地为OR 1，OR 2，O-（CH 2）O-烷基或二氨基酸及其酯; R 1和R 2独立地是H，烷基，芳基，新戊酰氧基甲基，邻苯二甲酰基或取代的邻苯二甲酰基，C（R 3）20 C（O）X（R 4）a，P（O）（OR 7）2或-P（O）（OR 7）2或-OP（O）（OR 7）2 R 6是H或C 1 -C 8烷基; R 7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1-3; Y为0，S或NH; W为0或S; B选自腺嘌呤，鸟嘌呤，胞嘧啶，尿嘧啶，胸腺嘧啶，修饰的嘌呤，嘧啶和吡啶。

9. 发明申请

WO2003100009A3 ENHANCING THE EFFICACY OF REVERSE TRANSCRIPTASE AND DNA POLYMERASE INHIBITORS (NUCLEOSIDE ANALOGS) USING PNP INHIBITORS AND/OR 2'-DEOXYGUANOSINE AND/OR PRODRUG THEREOF 审中-公开
公开(公告)号：WO2003100009A3
公开(公告)日：2003-12-04
申请号：PCT/US2003/016364
申请日：2003-05-23
申请人： BIOCRYST PHARMACEUTICALS, INC. , BANTIA, Shanta , BABU, Yarlagadda, S.
发明人： BANTIA, Shanta , BABU, Yarlagadda, S.
IPC分类号： C07D487/02
摘要： The efficacy of reverse transcriptase and DNA polymerase inhibitors (nucleoside analogs) in a mammalian host is enhanced by administering an effective amount of PNP inhibitor of prodrug of PNP inhibitor and/or an effective amounts of 2'-deoxyguanosine and/or prodrugs thereof.

10. 发明申请

WO2002069903A2 NUCLEOSIDES, PREPARATION THEREOF AND USE AS INHIBITORS OF RNA VIRAL POLYMERASES 审中-公开
标题翻译：核苷酸，其制备方法和用作RNA病毒聚合酶的抑制剂
公开(公告)号：WO2002069903A2
公开(公告)日：2002-09-12
申请号：PCT/US2002/006551
申请日：2002-03-06
申请人： BIOCRYST PHARMACEUTICALS, INC. , MONTGOMERY, John, A. , BABU, Yarlagadda, S. , ROWLAND, R., Scott , CHAND, Pooran
发明人： MONTGOMERY, John, A. , BABU, Yarlagadda, S. , ROWLAND, R., Scott , CHAND, Pooran
IPC分类号： A61K
CPC分类号： A61K31/7084 , A61K45/06 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , Y02A50/393 , Y02A50/465
摘要： The compounds represented by the formulae (I) wherein X is selected from the group consisting of: O, S, N-R 1 , and CHR 1 ; Y and Y' is individually selected from H, OR 1 , NR 1 R 2 , and N 3 Z and Z' is individually selected from H, OR 1 , and NR 1 R 2 R = H, formula (II), formula (III), or formula (III), R 1 and R 2 is selected from H, alkyl, acyl, aryl which may be substituted or unsubstituted, R 3 is selected from H, alkyl, alkenyl, alkynyl, aryl, acyloxyalkyl, and pivaloyloxyalkyl, B is selected from 5 or 6-substituted uracil or cytosine, pseudouracil, N-substituted pseudouracil, 2-thiouracil, 2-thiocytosine, 5- or 6-substituted 2-thiouracil and 2-thiocytosine, 6-azauracil, 5-azacytosine, 8-azapurines, and 7-aza-8-deazapurines. Substitutions may be halosubstituted alkyl, halosubstituted alkenyl, halosubstituted alkynyl, halosubstituted aryl, alkylthio, or NR 1 R 2 . When Z and Z' are H and Y or Y' is OH then B is not 5-methyl uracil or cytosine; and pharmaceutically acceptable salts thereof, mono, di or triphosphate and prodrugs thereof.
摘要翻译：由式（I）表示的化合物，其中X选自：O，S，N-R 1和CHR 1; Y和Y'分别选自H，OR 1，NR 1 R 2，N 3 Z和Z'分别选自H，OR 1和NR 1 R 2， R = H，式（II），式（III）或式（III），R 1和R 2选自H，烷基，酰基，可被取代或未取代的芳基，R 3，选自H，烷基，烯基，炔基，芳基，酰氧基烷基和新戊酰氧基烷基，B选自5或6位取代的尿嘧啶或胞嘧啶，假尿嘧啶，N-取代的假尿嘧啶，2-硫尿嘧啶，2-硫代胞嘧啶，5-或6 2-取代的2-硫尿嘧啶和2-硫代胞嘧啶，6-氮尿嘧啶，5-氮杂胞嘧啶，8-氮杂嘌呤和7-氮杂-8-脱氮嘌呤。取代的可以是卤代烷基，卤代烯基，卤代炔基，卤代芳基，烷硫基或NR 1 R 2。当Z和Z'为H且Y或Y'为OH时，B不为5-甲基尿嘧啶或胞嘧啶; 其药学上可接受的盐，单，二或三磷酸及其前药。

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