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1. 发明申请

WO2011031554A3 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：WO2011031554A3
公开(公告)日：2011-09-15
申请号：PCT/US2010046999
申请日：2010-08-27
申请人： BIOCRYST PHARM 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 , A61K31/4985 , A61P17/06 , A61P35/00 , A61P37/06
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，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）化合物。

2. 发明申请

WO2010011748A3 SYNTHETIC INTERMEDIATES AND PROCESSES 审中-公开
标题翻译：合成中间体和工艺
公开(公告)号：WO2010011748A3
公开(公告)日：2010-07-01
申请号：PCT/US2009051402
申请日：2009-07-22
申请人： BIOCRYST PHARM 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 R1 has any of the values described herein and R2 is a nucleoside sugar group.
摘要翻译：本发明提供了可用于制备式（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且R 2是核苷糖基。

3. 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。

4. 发明申请

WO2006050161A3 THERAPEUTIC FUROPYRIMIDINES AND THIENOPYRIMIDINES 审中-公开
标题翻译：治疗性F ID ID IN。。。。。。。
公开(公告)号：WO2006050161A3
公开(公告)日：2007-12-21
申请号：PCT/US2005039072
申请日：2005-10-28
申请人： BIOCRYST PHARM 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： C07H19/22 , A01N43/04 , A61K31/70
CPC分类号： C07D495/04 , A61K31/675 , A61K31/7076 , A61K38/212 , A61K38/2292 , C07D491/048 , C07D493/04 , C07F9/6561 , C07H7/06 , C07H19/22 , 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。

5. 发明申请

WO2006104945A3 HEPATITIS C THERAPIES 审中-公开
标题翻译：乙型肝炎治疗
公开(公告)号：WO2006104945A3
公开(公告)日：2007-02-08
申请号：PCT/US2006010948
申请日：2006-03-23
申请人： BIOCRYST PHARM 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
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。

6. 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。

7. 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。

8. 发明申请

WO2007002191A2 METHODS FOR THE PREPARATION OF 9-DEAZAPURINE DERIVATIVES 审中-公开
标题翻译：制备9-二氮杂萘衍生物的方法
公开(公告)号：WO2007002191A2
公开(公告)日：2007-01-04
申请号：PCT/US2006024134
申请日：2006-06-21
申请人： BIOCRYST PHARM 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： A61K31/675 , A61K31/7076 , A61K38/21
CPC分类号： C07H21/00 , Y02P20/55
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.
摘要翻译：提供了使用苄基保护基作为核糖中2和3个羟基的保护基制备9-脱氮嘌呤衍生物的异构体的方法。

9. 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。

10. 发明申请

WO2002076971A1 COMPOUNDS USEFUL FOR INHIBITING PARAMYXOVIRUS NEURAMINIDASE 审中-公开
标题翻译：有用的抑制氨甲蝶呤神经酰胺酶的化合物
公开(公告)号：WO2002076971A1
公开(公告)日：2002-10-03
申请号：PCT/US2002/007052
申请日：2002-03-08
申请人： BIOCRYST PHARMACEUTICALS, INC. , CHAND, Pooran , BABU, Yarlagadda, S. , ROWLAND, Scott, R. , LIN, Tsu-Hsing
发明人： CHAND, Pooran , BABU, Yarlagadda, S. , ROWLAND, Scott, R. , LIN, Tsu-Hsing
IPC分类号： C07D315/00
CPC分类号： A61K31/4178 , A61K31/351 , A61K31/381 , A61K31/4025 , A61K31/4192 , A61K31/422 , A61K31/427 , A61K31/453 , C07D309/08 , C07D309/14 , C07D309/28
摘要： Compounds represented by the formulae (A, B, C) wherein X is selected from the group consisting of: CHR, O, NR, N-OR, NR(O), S, S(O) and S(O)O X 1 is selected from the group consisting of CR, N, and N(O); R is selected from the group consisting of: H, alkyl, alkene, alkyne, CN, NO 2 , N 3 , halo and NHR 10 ; R 1 is selected from the group consisting of: H, (CH 2 )nCO 2 R 10 , (CH 2 )n-tetrazol, (CH 2 )nSO 3 H, (CH 2 )nSO 2 H, (CH 2 )nPO 3 H 2 , (CH 2 )nCONR 10 , (CH 2 )nNO 2 , and (CH 2 )nCHO; R 1a is selected from the group consisting of: H, (CH 2 )nOR 10 , (CH 2 )nCN, (CH 2 )nNR 10 R 10a , (CH 2 )nNHC(O)R 10 , (CH 2 )nC(O)NR 10 R 10a , and (CH 2 )nOC(O)R 10 ; R 1 and R 1a both cannot be H each of R 2 and R 2a is independently selected from the group consisting of H, halo, CN, (CH 2 )nCO 2 R 10 , (CH 2 )nNR 10 R 10a and (CH 2 ) n -OR 10 ; each of R 3 and R 3a is independently selected from the group consisting of: H, NHSO 2 R 10 , N(O)-SO 2 R 10 , NR 10 SO 2 R 10a , (CH 2 )mYR 10 , and (CH 2 )mR 6 ; at least oneof R 3 and R 3a should be other than H Y is selected from the group consisting of: O, NH, NHC(O), C(O)NH, S, S(O), S(O)O, NHS(O)O, S(O)ONH, NHC(O)NH and heterocycle; R 3 and R 3a together may be =O, =CHR 6 , =CHR 10 , NR 10 and =N-OR 10 R 4 and R 4a is independently selected from the group consisting of: H, (CH 2 )mYR 10 and (CH 2 )mYR 10 and (CH 2 )mR 6 R 4 and R 4a together may be: =O, =CHR 6 , =CHR 10 , =NR 10 and =N-OR 10 each of R 5 and R 5a is independently selected from the group consisting of C(R 7 )(R 7a ), C(R 7 )(R 7a )C(R 8 )(R 8a ), C(R 7 )(R 7a )C(R 8 )(R 8a )C(R 9 )(R 9a ), OC(R 7 )(R 7a ), OC(R 7 )(R 7a )C(R 8 )(R 8a ), C(R 7)(R¿7a )OC(R 8 )(R 8a ), N(R 10 )C(R 7 )(R 7a ), N(R 10 )C(R 7 )(R 7a )C(R 8 )(R 8a ), C(R 7 )(R 7a )N(R 10 )C(R 8a ), and C(O)NR 10 R 10a ; R 6 is selected from the group consisting of H, halo, CN, NO 2 , N 3 , CO 2 R¿10, R 10 and NR 10 R 10a ; R 7 , R 7a , R 8 , R 8a , R 9 and R 9a is selected from the group from the group consisting of: H, (CH 2 )mYR 10 and (CH 2 )mR 6 each of the R 10 and R 10a is individually selected from the groups consisting of: H, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heterocycle, substituted heterocycle, alkenyl, substituted alkenyl, alkynyl, and substituted alkynyl; each of m and n is individually O, 1, 2, 3, or 4; and pharmaceutically acceptable salt thereof; and prodrugs thereof, and uses thereof.
摘要翻译：由式（A，B，C）表示的化合物，其中X选自：CHR，O，NR，N-OR，NR（O），S，S（O）和S（O）选自CR，N和N（O）; R选自：H，烷基，烯烃，炔烃，CN，NO 2，N 3，卤素和NHR 10; R 1选自：H，（CH 2）n CO 2 R 10，（CH 2）n - 四唑，（CH 2）n SO 3 H，（CH 2）n SO 2 H，（CH 2）n PO 3 H 2，（CH 2）n CONR 10，（CH 2）n NO 2， CH2）NCHO; R1a选自H，（CH2）nOR10，（CH2）nCN，（CH2）nNR10R10a，（CH2）nNHC（O）R10，（CH2）nC（O）NR10R10a和（CH2）nOC O）R10; R 1和R 1a均不能为H，R2和R2a独立地选自H，卤素，CN，（CH2）nCO2R10，（CH2）nNR10R10a和（CH2）n-OR10; R 3和R 3a各自独立地选自：H，NHSO 2 R 10，N（O）-SO 2 R 10，NR 10 SO 2 R 10a，（CH 2）m YR 10和（CH 2）m R 6; R 3和R 3a中的至少一个应该不是HY选自：O，NH，NHC（O），C（O）NH，S，S（O），S（O）O，NHS O）O，S（O）ONH，NHC（O）NH和杂环; R 3和R 3a一起可以是= O，= CHR 6，= CHR 10，NR 10和= N-OR 10 R 4和R 4a独立地选自：H，（CH 2）m YR 10和（CH 2）m YR 10和（CH 2）m R 6 R 4 和R 4a一起可以是：= O，= CHR 6，= CHR 10，= NR 10和= N-OR 10，R 5和R 5a各自独立地选自C（R7）（R7a），C（R7）（R7a） C（R8）（R8a），C（R7）（R7a）C（R8）（R8a）C（R9）（R9a），OC（R7）（R7a） R8a），C（R7）（R7a）OC（R8）（R8a），N（R10）C（R7）（R7a），N（R10）C（R7）（R7a）C（R8）（R8a）（R7）（R7a）N（R10）C（R8a）和C（O）NR10R10a; R6选自H，卤素，CN，NO2，N3，CO2R10，R10和NR10R10a; R7，R7a，R8，R8a，R9和R9a选自H，（CH2）mYR10和（CH2）mR6，R10和R10a各自独立地选自：H，烷基，取代的烷基，芳基，取代的芳基，芳基烷基，取代的芳基烷基，杂环，取代的杂环，烯基，取代的烯基，炔基和取代的炔基; m和n各自独立地为O，1,2,3或4; 及其药学上可接受的盐; 及其前药，及其用途。

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