세포의 티올 수준을 측정하기 위한 실시간 이미징 센서
    2.
    发明申请
    세포의 티올 수준을 측정하기 위한 실시간 이미징 센서 审中-公开
    用于测量细胞THIOL水平的实时成像传感器

    公开(公告)号:WO2016080759A2

    公开(公告)日:2016-05-26

    申请号:PCT/KR2015/012415

    申请日:2015-11-18

    IPC分类号: G01N33/58 G01N33/52

    摘要: 본 발명은 세포의 티을 수준을 측정하기 위하여 실시간으로 이미징이 가능한 형광 센서에 관한 것이다. 본 발명은 본 발명의 FreSH-트레이서 (Fluorescent Real-time SH group-Tracer)가 생세포에서 티올의 양에 따라 형광 세기가 연속적이고, 비율계량적이며 가역적으로 증감한다는 것을 규명함으로써, 살아있는 세포에서 티올의 양을 실시간으로 정량 또는 정성적으로 검출하는데 현저한 민감성을 갖는바이오 센서로서 유용하게 이용될 수 있다.

    摘要翻译: 本发明涉及能够实时成像测量细胞硫醇水平的荧光传感器。 本发明揭示本发明的荧光实时SH组 - 示踪剂(FreSH-Tracer)的荧光强度根据活细胞中的硫醇水平而连续地,比例地或可逆地增加或减少,因此可以有用地使用 作为生物传感器,其对活细胞中细胞硫醇水平的定量或定性实时检测非常敏感。

    SUBSTITUTED PYRANO [2, 3 - B] PYRIDINE DERIVATIVES AS CANNABINOID -1 RECEPTOR MODULATORS
    6.
    发明申请
    SUBSTITUTED PYRANO [2, 3 - B] PYRIDINE DERIVATIVES AS CANNABINOID -1 RECEPTOR MODULATORS 审中-公开
    取代的吡咯并[2,3-B]吡啶衍生物作为CANNABINOID-1受体调节剂

    公开(公告)号:WO2008094476A1

    公开(公告)日:2008-08-07

    申请号:PCT/US2008/001042

    申请日:2008-01-25

    摘要: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, Huntington's disease movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and the promotion of wakefulness.

    摘要翻译: 结构式(I)的新型化合物是大麻素-1(CB1)受体的拮抗剂和/或反向激动剂,可用于治疗,预防和抑制由CB1受体介导的疾病。 本发明的化合物可用作治疗精神病,记忆缺陷,认知障碍,阿尔茨海默病,偏头痛,神经病,包括多发性硬化症和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症的中枢作用药物 脑血管意外,头部创伤,焦虑障碍,压力,癫痫,帕金森病,亨廷顿病运动障碍和精神分裂症。 该化合物还可用于治疗物质滥用障碍,治疗肥胖或进食障碍以及治疗哮喘,便秘,慢性肠假性梗阻,肝硬化,非酒精性脂肪性肝病(NAFLD) ,非酒精性脂肪性肝炎(NASH),以及促进觉醒。

    FLUORESCENT SUBSTRATES FOR MONOAMINE TRANSPORTERS AS OPTICAL FALSE NEUROTRANSMITTERS
    7.
    发明申请
    FLUORESCENT SUBSTRATES FOR MONOAMINE TRANSPORTERS AS OPTICAL FALSE NEUROTRANSMITTERS 审中-公开
    单色运输机荧光底物作为光学神经递质

    公开(公告)号:WO2008013997A2

    公开(公告)日:2008-01-31

    申请号:PCT/US2007/017014

    申请日:2007-07-27

    IPC分类号: C07D491/14

    摘要: The present invention relates to compounds of the general structure: wherein Y is O, X is O, bond α is absent and bond β is present, or Y is H, X is CH, bond α is present, and bond β is absent; atom Z is a carbon and bonds χ , δ and γ are present, or is a nitrogen and bonds χ , δ and γ are absent; R 1 is -H, -OH, -O-R 7 , -N(H) -R 8 , -N (H) - (CH 2 ) n -NH 2 , -N(R 9 ) (R 10 ), or a piperazine cation; R 2 is either covalently bound to R 9 , or is -H, or is covalently bound to R 3 so as to form a substituted or unsubstituted pyrrole or R 2 is covalently bound to R 9 or R 8 or R 7 ; or R 1 and R 2 are covalently joined to form an aromatic ring; R 3 is either covalently bound to R 2 so as to form a pyrrole, or is, inter alia, -H, -OH, alkyl, or when Z is nitrogen R 3 is =O; R 4 is, inter alia, -H, -OH, or -R 11 NH 2 ; R 5 is, inter alia, -H, -OH, or -R 12 NH 2 , and R 6 is either is covalently bound to R 10 or is -H, or R 6 is covalently bound to R 10 or R 8 or R 7 . This invention also provides processes for making the compounds as well as methods for monitoring activity of monoamine transporters or treating monoamine transporter-associated diseases by employing the compounds.

    摘要翻译: 本发明涉及通式结构的化合物:其中Y为O,X为O,不存在键a,键ß存在,或Y为H,X为CH,存在键a,键ß不存在; 原子Z是碳并键合α,d和? 是否存在,或是氮并键合?,d和? 不存在 R 1是-H,-OH,-OR 7,-N(H)-R 8,-N(H) - ( CH 2 N 2,-N(R 9)(R 10) SUB>)或哌嗪阳离子; R 2与R 9共价结合,或者是-H,或者共价键合到R 3,以便形成取代或未取代的 未取代的吡咯或R 2 2共价键合到R 9或R 8或R 7上。 或R 1和R 2 2共价连接形成芳香环; R 3共价结合到R 2上,以便形成吡咯,或者尤其是-H,-OH,烷基或当Z是氮时R 3 = O; 其中R 4尤其是-H,-OH或-R 11 NH 2; 特别地,R 5是-H,-OH或-R 12 NH 2,和R 6 N 2 >与R 10共价结合或为-H,或R 6共价结合R 10或R 8 或者R 7 。 本发明还提供了制备该化合物的方法以及通过使用该化合物来监测单胺转运蛋白的活性或治疗单胺转运蛋白相关疾病的方法。

    HETEROCYCLIC COMPOUNDS HAVING AFFINITIES FOR SEROTONIN RECEPTORS
    8.
    发明申请
    HETEROCYCLIC COMPOUNDS HAVING AFFINITIES FOR SEROTONIN RECEPTORS 审中-公开
    具有丝氨酸蛋白酶受体活性的杂环化合物

    公开(公告)号:WO00059909A1

    公开(公告)日:2000-10-12

    申请号:PCT/JP2000/001224

    申请日:2000-03-02

    CPC分类号: C07D491/16

    摘要: Compounds represented the general formula (I) exhibit affinities for various serotonin receptors (such as 5HT-1A, 2, 6, 7, and so on) and are therefore useful as remedies for central nervous system diseases or the like wherein R and R are each independently hydrogen, lower alkyl, or the like; R and R are each independently hydrogen, lower alkyl, or the like; or alternatively R and R may be united to form a single bond; n is 0 or 1; R is hydrogen; R is hydrogen, hydroxyl, or the like; R is hydrogen; R and R are each independently hydrogen, lower alkylthio, or the like; or alternatively R and R may be united to form a single bond; R is hydrogen, lower alkyl, or the like; R is hydrogen, lower alkyl, or the like; and R is hydrogen or lower alkyl

    摘要翻译: 表示通式(I)的化合物对各种5-羟色胺受体(例如5HT-1A,2,6,7等)表现出亲和力,因此可用作中枢神经系统疾病等的治疗方法,其中R 1, 和R 2各自独立地为氢,低级烷基等; R 3和R 4各自独立地为氢,低级烷基等; 或者R 1和R 3可以一起形成单键; n为0或1; R 5是氢; R 6是氢,羟基等; R 7是氢; R 8和R 9各自独立地为氢,低级烷硫基等; 或者R 7和R 9可以结合形成单键; R 10是氢,低级烷基等; R 11是氢,低级烷基等; 和R 12是氢或低级烷基

    NEW DERIVATIVES OF TETRAHYDRO-2,3,6,7,1H,5H,11H-(1)BENZOPYRANO(6,7,8,ij)QUINOLIZONONE-11 USABLE AS MARKERS FOR ORGANIC COMPOUNDS FOR THE PURPOSE OF DETECTING SAID COMPOUNDS BY CHEMILUMINESCENCE OR FLUORESCENCE
    9.
    发明申请
    NEW DERIVATIVES OF TETRAHYDRO-2,3,6,7,1H,5H,11H-(1)BENZOPYRANO(6,7,8,ij)QUINOLIZONONE-11 USABLE AS MARKERS FOR ORGANIC COMPOUNDS FOR THE PURPOSE OF DETECTING SAID COMPOUNDS BY CHEMILUMINESCENCE OR FLUORESCENCE 审中-公开
    四氰基-2,3,6,7,1H,5H,11H-(1)苯并噻吩(6,7,8,ij)喹诺酮酮的新衍生物可用作有机化合物标记,用于通过显微镜检测化合物的目的 或荧光

    公开(公告)号:WO1989012052A1

    公开(公告)日:1989-12-14

    申请号:PCT/FR1989000277

    申请日:1989-06-02

    IPC分类号: C07D491/16

    CPC分类号: C07D491/16

    摘要: The invention concerns new derivatives of tetrahydro-2,3,6,7,1H,5H,11H-(1)benzopyrano (6,7,8,ij)quinolizinone in accordance with formula (I), in which R represents a radical having formula (II), wherein m is equal to 0 or 1, and n is equal to 0 or is a whole number between 1 and 12, provided that n is equal to 0 when m is 0, or the radical having the formula: -NH-(CH2)n-NH2, in which n has the above meaning. Said derivatives can be used as markers for organic compounds, in order to detect them by chemiluminescence or fluorescence.

    摘要翻译: 本发明涉及根据式(I)的四氢-2,3,6,7,1H,5H,11H-(1)苯并吡喃酮(6,7,8,ij)喹嗪酮的新衍生物,其中R 1, 表示具有式(II)的基团,其中m等于0或1,并且n等于0或者为1至12之间的整数,条件是当m为0时n等于0,或者具有 式:-NH-(CH 2)n -NH 2,其中n具有上述含义。 所述衍生物可用作有机化合物的标记物,以便通过化学发光或荧光检测它们。