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    ENANTIOMERS OF THE 1',6'-ISOMER OF NEPLANOCIN A
    3.
    发明申请
    ENANTIOMERS OF THE 1',6'-ISOMER OF NEPLANOCIN A 审中-公开
    NEPLANOCIN的1'，6'异构体的成员A

    公开(公告)号：WO2016022563A1

    公开(公告)日：2016-02-11

    申请号：PCT/US2015/043617

    申请日：2015-08-04

    Applicant: AUBURN UNIVERSITY

    Inventor： SCHNELLER, Stewart W. ,  LIU, Chong ,  CHEN, Qi ,  YE, Wei

    IPC: A61K31/52 ,  A61K31/437 ,  C07D471/04

    CPC classification number: C07H19/16 ,  C07D471/04 ,  C07D473/30 ,  C07D473/34

    Abstract: Enantiomers of 1',6'-isoneplanocin, including derivatives of the enantiomers of 1',6'-isoneplanocin, are disclosed along with novel synthetic methods. In particular, a substituted cyclopentane epoxide is synthesized into the enantiomers of 1',6'-isoneplanocin. Enantiomers of carbocyclic nucleoside analogs of 3-deazaneplanocin to provide D- and L-like 1',6'-iso-3-deazaneplanocin are also disclosed. The small molecule chemotherapeutic compounds beneficially provide DNA and RNA antiviral activity, demonstrating activity towards, for example, human cytomegalovirus, measles, Ebola, norovirus, dengue, vaccinia and HBV. Compounds exhibiting reduced S-adenosylhomocysteine hydrolase inhibitory effects are disclosed and provide improved toxicity profiles in comparison to neplanocin. The invention provides improved prophylactic and/or therapeutic antiviral efficacy.

    Abstract translation: 包括1'，6'-异丙肾上腺素的对映异构体，包括1'，6'-异丙肾上腺素的对映异构体的衍生物，以及新的合成方法。 特别地，将取代的环戊烷环氧化合物合成为1'，6'-异丙肾上腺素的对映异构体。 还公开了3-去氮吗兰普兰的碳环核苷类似物的对映异构体以提供D-和L-样的1'，6'-异-3-去氮吗啡酮。 小分子化学化合物有利地提供了DNA和RNA抗病毒活性，证明了对例如人巨细胞病毒，麻疹，埃博拉病毒，诺如病毒，登革热，牛痘和HBV的活性。 公开了表现出降低的S-腺苷高半胱氨酸水解酶抑制作用的化合物，并且与尼泊洛环相比提供改进的毒性特征。 本发明提供改进的预防和/或治疗性抗病毒功效。

    ANTIPARASITIC COMPOUNDS AND COMPOSITIONS
    9.
    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）。

    CIS-CYCLOHEXYL SUBSTITUTED PYRIMIDINONE DERIVATIVES
    10.
    发明申请
    CIS-CYCLOHEXYL SUBSTITUTED PYRIMIDINONE DERIVATIVES 审中-公开
    CIS-CYCLOHEXYL取代的嘧啶酮衍生物

    公开(公告)号：WO2008066664A2

    公开(公告)日：2008-06-05

    申请号：PCT/US2007/023318

    申请日：2007-11-05

    Applicant: NEUROGEN CORPORATION ,  BLUM, Charles, A. ,  GHOSH, Manuka ,  MARTINEZ, Isamir ,  ZHANG, Xuechun ,  ZHENG, Xiaozhang

    Inventor： BLUM, Charles, A. ,  GHOSH, Manuka ,  MARTINEZ, Isamir ,  ZHANG, Xuechun ,  ZHENG, Xiaozhang

    IPC: A61K31/522

    CPC classification number: C07D473/30 ,  C07D471/04 ,  C07D495/04 ,  C07D513/04

    Abstract: Cis-cyclohexyl substituted pyrimidinone derivatives are provided, of Formula (I) wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro , and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

    Abstract translation: 提供顺式 - 环己基取代的嘧啶酮衍生物，式（I）其中变量如本文所述。 这些化合物是可用于在体内或体外调节特异性受体活性的配体，并且特别可用于治疗与人类，驯养伴侣动物和家畜中的病理受体激活相关的病症。 还提供了使用这些化合物治疗这种病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法。

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