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    ANTIPARASITIC COMPOUNDS AND COMPOSITIONS
    5.
    发明申请
    ANTIPARASITIC COMPOUNDS AND COMPOSITIONS 审中-公开
    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

    Applicant: MEDICAL RES COUNCIL ,  LOAKES DAVID ,  TOO KATHLEEN

    Inventor： LOAKES DAVID ,  TOO KATHLEEN

    IPC: 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 classification number: 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

    Abstract: 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 ).

    Abstract translation: 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）。

    USE OF CARBON MONOXIDE DEPENDENT GUANYLYL CYCLASE MODIFIERS TO STIMULATE NEURITOGENESIS
    9.
    发明申请
    USE OF CARBON MONOXIDE DEPENDENT GUANYLYL CYCLASE MODIFIERS TO STIMULATE NEURITOGENESIS 审中-公开
    使用一氧化碳依赖型肾上腺素调节剂刺激神经细胞增生

    公开(公告)号：WO0128545A3

    公开(公告)日：2002-05-10

    申请号：PCT/US0028836

    申请日：2000-10-19

    Applicant: NEOTHERAPEUTICS INC ,  GLASKY ALVIN ,  RATHBONE MICHAEL P

    Inventor： GLASKY ALVIN ,  RATHBONE MICHAEL P

    IPC: C12N5/06 ,  A61K31/52 ,  A61K31/522 ,  A61K31/708 ,  A61K45/00 ,  A61P25/00 ,  A61P25/28 ,  A61P43/00 ,  C07D473/30 ,  C07H19/167

    CPC classification number: A61K31/52 ,  A61K31/522 ,  A61K31/7076 ,  A61K31/708

    Abstract: Disclosed herein are methods directed generally to the control of neural activity and for selectively and controllably inducing the in vivo genetic expression of one or more naturally occurring genetically encoded molecules in mammals. More particularly, the present invention selectively activates or derepresses genes encoding for specific naturally occurring molecules such as neurotrophic factors through the administration of carbon monoxide dependent guanylyl cyclase modulating purine derivatives. The methods of the present invention may be used to affect a variety of cellular and neurological activities and to therapeutically or prophylactically treat a wide variety of neurodegenerative, neurological, and cellular disorders.

    Abstract translation: 本文公开的方法一般涉及神经活性的控制以及选择性和可控地诱导哺乳动物中一种或多种天然存在的遗传编码分子的体内基因表达的方法。 更具体地，本发明通过施用一氧化碳依赖性鸟苷酸环化酶调节嘌呤衍生物来选择性地激活或去抑制编码特定天然存在分子如神经营养因子的基因。 本发明的方法可用于影响多种细胞和神经活性，并且可用于治疗或预防性治疗各种各样的神经变性，神经系统和细胞疾病。

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