专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2007135380A3 ANTIPARASITIC COMPOUNDS AND COMPOSITIONS 审中-公开
标题翻译：抗微生物化合物和组合物
公开(公告)号：WO2007135380A3
公开(公告)日：2008-07-31
申请号：PCT/GB2007001820
申请日：2007-05-17
申请人： MEDICAL RES COUNCIL , LOAKES DAVID , TOO KATHLEEN
发明人： LOAKES DAVID , TOO KATHLEEN
IPC分类号： C07D473/16 , A61K31/404 , A61K31/416 , A61K31/52 , A61K31/7052 , A61K31/7076 , A61K31/708 , A61P33/02 , A61P33/06 , C07D209/04 , C07D231/56 , C07D473/30 , C07H19/02 , C07H19/052 , C07H19/16
CPC分类号： A61K31/404 , A61K31/416 , A61K31/52 , A61K31/7052 , A61K31/7076 , A61K31/708 , C07D209/40 , C07D209/42 , C07D473/16 , C07D473/18 , C07D473/24 , C07D473/30 , C07D473/34 , C07D487/04
摘要： Disclosed is use of a compound having a structure according to general formula (I) defined below, in the manufacture of a medicament to treat and/or prevent a parasitic infection or infestation in a mammalian subject wherein X 1 = N or CH or C=O (X 2 = NH) or C=S (X 2 = NH) or C-OR 1 or C-halogen or C-azide; X 2 = N or CR 1 or C-halogen or CS(O) n R 1 where n = 0-2 or a (C) m linker where m = 1-3 between X 2 and X 6 or C-X 5 X 6 (in which case X 5 X 6 at C6 (purine numbering) is replaced by H or NHR 1 or O or OR 1 or S or SR 1 ); X 3 = N or CH or C-NO 2 ; X 4 = N or CH or C-NO 2 or C-NR 1 R 2 or an amidine derivative or a guanidinium derivative; X 5 = O or NR 1 or CR 1 R 2 ; X 6 = OR 1 or O-acyl or 0-S(O) n R 1 or NR 1 R 2 or NH-acyl or N(Acyl) 2 or NH-OS(O) 2 R 1 or NH-S(O) n R 1 where n = 0-2 or a hydrazone derivative or an oxime derivative, but if X 5 = O, X 6 cannot = O or X 5 X 6 is an amidine or an N-substituted pyridine or substituted guanidine; Y = H or NH 2 or NR 1 R 2 or -O (X 3 = NH) or OR 1 or F or Cl or Br or I or CR 1 R 2 R 3 or S(O) n R 1 where n = 0-2 or azide or X 5 X 6 (in which case X 5 X 6 at C6 (purine numbering) is replaced by H or NHR 1 or O or OR 1 or S or SR 1 ); R 1 , R 2 , R 3 are independently selected from the group consisting of H or (optionally substituted), alkyl, alkenyl or alkynyl or aryl or aralkyl where the substituents may be selected from H, OH, NH 2 , halogen, N 3 , CN, CHO, COOR', C0NR' 2 , OR, NE' 2 , SR', NR'NR' 2 , NR'OR', NO 2 and R' is alkyl, alkenyl, alkynyl, aralkyl, acyl, sulfonyl; Z = H or substituted (alkyl or alkenyl or alkynyl or aralkyl) or a sugar derivative of general formula (II) in the ß-configuration where: B is the nucleobase from Formula (I); X 7 = CH 2 or O or NR 1 or S; R 4 = H or OH or OR 1 or halogen or azide or a phosphate derivative; R 5 = H or F or CH 3 ; R 6 = H or OH or OR 1 or halogen or azide or a phosphate derivative; and R 7 = H or halogen or R 1 or a derivative of an amino acid or PO 3 H 2 or P 2 O 6 H 3 or P 3 O 9 H 4 or a methylene derivative of P 2 O 6 H 3 or P 3 O 9 H 4 or a masked phosphate or a phosphonate derivative (5'-O replaced with CH 2 ).
摘要翻译：本发明公开了具有下述通式（I）结构的化合物在制备用于治疗和/或预防哺乳动物受试者的寄生虫感染或侵染的药物中的用途，其中X < = N或CH或C = O（X 2 N = NH）或C = S（X 2 N = NH）或C-OR 1 或C-卤素或C-叠氮化物; X 2 = N或CR 1或C - 卤素或CS（O）n R 1 R 1其中n = 0-2或其中在X 2和X 6或CX 5之间的m = 1-3的（C）m < （在这种情况下）C6（嘌呤编号）的X 5 X 6取代为H或NHR 1 或O或OR 1或S或SR 1）; X 3 = N或CH或C-NO 2; X 4 = N或CH或C-NO 2或C-NR 1 R 2或脒衍生物或胍衍生物; X 5 = O或NR 1或CR 1 R 2 2; 或者O - 酰基或0-S（O）n R 1或NR 1，或者NH-酰基或N（酰基）2或NH-OS（O）2 R 2，其中n = 0-2或腙衍生物或肟衍生物，但如果X C6（嘌呤编号）的5个X 6位被H或NHR 1或O或OR 1取代，或S或 SR _{1 ）; R 1，R 2，R 3，R 3独立地选自H或（任选取代的），烷基，烯基或炔基或芳基或芳烷基，其中取代基可以选自H，OH，NH 2，卤素，N 3，CN，CHO，COOR'，C0NR' / SUB，OR，NE'2，SR'，NR'NR'2，NR'OR'，NO 2和R' 烷基，烯基，炔基，芳烷基，酰基，磺酰基; Z = H或通式（II）的取代的（烷基或烯基或炔基或芳烷基）或糖衍生物，其中：B是式（I）的核碱基; X 7或CH 2或O或NR 1或S; R 4 = H或OH或OR 1或卤素或叠氮化物或磷酸酯衍生物; R 5 = H或F或CH 3; R 6 = H或OH或OR 1或卤素或叠氮化物或磷酸酯衍生物; 和R 7 = H或卤素或R 1或氨基酸或PO 3 H 2的衍生物，或者P 2 3 3或3 3 > 4 或者P 2 O 3 H 3或S 3 O 3的亚甲基衍生物，或者掩蔽的磷酸盐或膦酸盐衍生物（5'-O被CH 2取代）。}

2. 发明申请

WO2007135380A2 ANTIPARASITIC COMPOUNDS AND COMPOSITIONS 审中-公开
标题翻译：抗微生物化合物和组合物
公开(公告)号：WO2007135380A2
公开(公告)日：2007-11-29
申请号：PCT/GB2007/001820
申请日：2007-05-17
申请人： MEDICAL RESEARCH COUNCIL , LOAKES, David , TOO, Kathleen
发明人： LOAKES, David , TOO, Kathleen
IPC分类号： A61K31/404 , A61K31/416 , A61K31/52 , A61K31/7052 , A61K31/7076 , A61K31/708
CPC分类号： A61K31/404 , A61K31/416 , A61K31/52 , A61K31/7052 , A61K31/7076 , A61K31/708 , C07D209/40 , C07D209/42 , C07D473/16 , C07D473/18 , C07D473/24 , C07D473/30 , C07D473/34 , C07D487/04 , Y02A50/409 , Y02A50/411
摘要： Disclosed is use of a compound having a structure according to general formula (I) defined below, in the manufacture of a medicament to treat and/or prevent a parasitic infection or infestation in a mammalian subject wherein X 1 = N or CH or C=O (X 2 = NH) or C=S (X 2 = NH) or C-OR 1 or C-halogen or C-azide; X 2 = N or CR 1 or C-halogen or CS(O) n R 1 where n = 0-2 or a (C) m linker where m = 1-3 between X 2 and X 6 or C-X 5 X 6 (in which case X 5 X 6 at C6 (purine numbering) is replaced by H or NHR 1 or O or OR 1 or S or SR 1 ); X 3 = N or CH or C-NO 2 ; X 4 = N or CH or C-NO 2 or C-NR 1 R 2 or an amidine derivative or a guanidinium derivative; X 5 = O or NR 1 or CR 1 R 2 ; X 6 = OR 1 or O-acyl or 0-S(O) n R 1 or NR 1 R 2 or NH-acyl or N(Acyl) 2 or NH-OS(O) 2 R 1 or NH-S(O) n R 1 where n = 0-2 or a hydrazone derivative or an oxime derivative, but if X 5 = O, X 6 cannot = O or X 5 X 6 is an amidine or an N -substituted pyridine or substituted guanidine; Y = H or NH 2 or NR 1 R 2 or -O (X 3 = NH) or OR 1 or F or Cl or Br or I or CR 1 R 2 R 3 or S(O) n R 1 where n = 0-2 or azide or X 5 X 6 (in which case X 5 X 6 at C6 (purine numbering) is replaced by H or NHR 1 or O or OR 1 or S or SR 1 ); R 1 , R 2 , R 3 are independently selected from the group consisting of H or (optionally substituted), alkyl, alkenyl or alkynyl or aryl or aralkyl where the substituents may be selected from H, OH, NH 2 , halogen, N 3 , CN, CHO, COOR', C0NR' 2 , OR, NE' 2 , SR', NR'NR' 2 , NR'OR', NO 2 and R' is alkyl, alkenyl, alkynyl, aralkyl, acyl, sulfonyl; Z = H or substituted (alkyl or alkenyl or alkynyl or aralkyl) or a sugar derivative of general formula (II) in the β-configuration where: B is the nucleobase from Formula (I); X 7 = CH 2 or O or NR 1 or S; R 4 = H or OH or OR 1 or halogen or azide or a phosphate derivative; R 5 = H or F or CH 3 ; R 6 = H or OH or OR 1 or halogen or azide or a phosphate derivative; and R 7 = H or halogen or R 1 or a derivative of an amino acid or PO 3 H 2 or P 2 O 6 H 3 or P 3 O 9 H 4 or a methylene derivative of P 2 O 6 H 3 or P 3 O 9 H 4 or a masked phosphate or a phosphonate derivative (5'-O replaced with CH 2 ).
摘要翻译：本发明公开了具有下述通式（I）结构的化合物在制备用于治疗和/或预防哺乳动物受试者的寄生虫感染或侵染的药物中的用途，其中X < = N或CH或C = O（X 2 N = NH）或C = S（X 2 N = NH）或C-OR 1 或C-卤素或C-叠氮化物; X 2 = N或CR 1或C - 卤素或CS（O）n R 1 R 1其中n = 0-2或其中在X 2和X 6或CX 5之间的m = 1-3的（C）m < （在这种情况下）C6（嘌呤编号）的X 5 X 6取代为H或NHR 1 或O或OR 1或S或SR 1）; X 3 = N或CH或C-NO 2; X 4 = N或CH或C-NO 2或C-NR 1 R 2或脒衍生物或胍衍生物; X 5 = O或NR 1或CR 1 R 2 2; 或者O - 酰基或0-S（O）n R 1或NR 1，或者NH-酰基或N（酰基）2或NH-OS（O）2 R 2，其中n = 0-2或腙衍生物或肟衍生物，但如果X C6（嘌呤编号）的5个X 6位被H或NHR 1或O或OR 1取代，或S或 SR _{1 ）; R 1，R 2，R 3，R 3独立地选自H或（任选取代的），烷基，烯基或炔基或芳基或芳烷基，其中取代基可以选自H，OH，NH 2，卤素，N 3，CN，CHO，COOR'，C0NR' / SUB，OR，NE'2，SR'，NR'NR'2，NR'OR'，NO 2和R' 烷基，烯基，炔基，芳烷基，酰基，磺酰基; Z = H或通式（II）的取代的（烷基或烯基或炔基或芳烷基）或糖衍生物，其中：B是式（I）的核碱基; X 7或CH 2或O或NR 1或S; R 4 = H或OH或OR 1或卤素或叠氮化物或磷酸酯衍生物; R 5 = H或F或CH 3; R 6 = H或OH或OR 1或卤素或叠氮化物或磷酸酯衍生物; 和R 7 = H或卤素或R 1或氨基酸或PO 3 H 2的衍生物，或者P 2 3 3或3 3 > 4 或者P 2 O 3 H 3或S 3 O 3的亚甲基衍生物，或者掩蔽的磷酸盐或膦酸盐衍生物（5'-O被CH 2取代）。}

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式