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1. 发明申请

WO0004866A9 PREPARATION OF THIOARABINOFURANOSYL COMPOUNDS AND USE THEREOF 审中-公开
公开(公告)号：WO0004866A9
公开(公告)日：2000-08-10
申请号：PCT/US9916630
申请日：1999-07-23
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 , A61K31/7042 , A61K31/7052 , A61K31/706 , A61K31/7064 , A61K31/7068 , A61P35/00 , C07D409/04 , C07H19/04 , C07H19/12 , A61K31/70
CPC分类号： C07D409/04 , A61K31/513 , A61K31/53 , C07H19/04
摘要： Patients suffering from cancer are treated by being administered a compound represented by formula: (1), wherein each R individually is H or an aliphatic or aromatic acyl group; A is selected from the group consisting of formulae (IIa, IIb, IIc, IId), wherein X is selected from the group consisting of hydrogen, fluorine, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, cyano and nitro. The above compounds also inhibit DNA replication in mammalian cells.

2. 发明申请

WO0004866A2 PREPARATION OF THIOARABINOFURANOSYL COMPOUNDS AND USE THEREOF 审中-公开
标题翻译：硫代氨基亚磺酰基甲基化合物的制备及其用途
公开(公告)号：WO0004866A2
公开(公告)日：2000-02-03
申请号：PCT/US9916630
申请日：1999-07-23
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 , A61K31/7042 , A61K31/7052 , A61K31/706 , A61K31/7064 , A61K31/7068 , A61P35/00 , C07D409/04 , C07H19/04 , C07H19/12 , A61K
CPC分类号： C07D409/04 , A61K31/513 , A61K31/53 , C07H19/04
摘要： Patients suffering from cancer are treated by being administered a compound represented by formula: (1), wherein each R individually is H or an aliphatic or aromatic acyl group; A is selected from the group consisting of formulae (IIa, IIb, IIc, IId), wherein X is selected from the group consisting of hydrogen, fluorine, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, cyano and nitro. The above compounds also inhibit DNA replication in mammalian cells.
摘要翻译：通过给药由式（1）表示的化合物治疗患有癌症的患者，其中每个R各自为H或脂肪族或芳香族酰基; A选自式（IIa，IIb，IIc，IId），其中X选自氢，氟，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，氰基和硝基。上述化合物还抑制哺乳动物细胞中的DNA复制。

3. 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。

4. 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。

5. 发明申请

WO02069903A3 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：WO02069903A3
公开(公告)日：2003-02-27
申请号：PCT/US0206551
申请日：2002-03-06
申请人： BIOCRYST PHARM 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： A61K31/7084 , A61K45/06 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C12N15/40 , A01N43/04 , A61K31/70 , C07G3/00 , C07G11/00 , C07H1/00 , C07H15/00 , C07H17/00 , C07H19/00 , C07H21/00 , C07H23/00
CPC分类号： A61K31/7084 , A61K45/06 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20
摘要： The compounds represented by the formulae (I) wherein X is selected from the group consisting of: O, S, N-R , and CHR ; Y and Y' is individually selected from H, OR , NR R , and N3 Z and Z' is individually selected from H, OR , and NR R R = H, formula (II), formula (III), or formula (III), R and R is selected from H, alkyl, acyl, aryl which may be substituted or unsubstituted, R 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 R . 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。

6. 发明申请

WO1997047194A1 SUBSTITUTED CYCLOPENTANE COMPOUNDS USEFUL AS NEURAMINIDASE INHIBITORS 审中-公开
标题翻译：作为神经酰胺酶抑制剂的替代环孢素化合物
公开(公告)号：WO1997047194A1
公开(公告)日：1997-12-18
申请号：PCT/US1997009309
申请日：1997-06-13
申请人： BIOCRYST PHARMACEUTICALS, INC. , BABU, Yarlagadda, S. , CHAND, Pooran , MONTGOMERY, John, A.
发明人： BIOCRYST PHARMACEUTICALS, INC.
IPC分类号： A01N37/12
CPC分类号： C07D295/185 , C07C61/06 , C07C62/02 , C07C69/757 , C07C233/47 , C07C279/14 , C07C279/16 , C07C2601/08 , C07D205/04
摘要： Compounds represented by formula (I), and pharmaceutically acceptacle salts thereof; and their method of preparation are provided. Compounds of the above formula are influenza virus neuraminidase inhibitors and can be used in treating patients infected with influenza virus.
摘要翻译：由式（I）表示的化合物及其药学上可接受的盐; 并提供了它们的制备方法。上述化合物是流感病毒神经氨酸酶抑制剂，可用于治疗感染流感病毒的患者。

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