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    Compositions and methods for stabilizing benzothiazole luciferin analogs
    2.
    发明授权
    Compositions and methods for stabilizing benzothiazole luciferin analogs 有权

    公开(公告)号：US11136615B2

    公开(公告)日：2021-10-05

    申请号：US16053413

    申请日：2018-08-02

    申请人： PROMEGA CORPORATION

    发明人： Ce Shi ,  Mary P. Hall ,  Thomas A. Kirkland ,  Lance P. Encell ,  Poncho Meisenheimer ,  Wenhui Zhou

    IPC分类号： C12Q1/66 ,  C07D253/06 ,  C07D417/04

    摘要： Disclosed herein are compositions and methods for stabilizing a benzothiazole luciferin analog such as D-luciferin and 6-amino-D-luciferin. The compositions may include the benzothiazole luciferin analog, a thionucleobase compound of formula (I), and a liquid medium, in which the thionucleobase is present in an amount effective to stabilize the luminogenic composition against decomposition. The methods provided herein may stabilize the benzothiazole luciferin analog against decomposition by contacting the benzothiazole luciferin analog with an effective amount of the thionucleobase compound in the presence of a liquid medium. Also provided herein is a kit containing the composition.

    Cyclic triazo and diazo sodium channel blockers
    9.
    发明授权
    Cyclic triazo and diazo sodium channel blockers 有权
    环状三唑和重氮钠通道阻滞剂

    公开(公告)号：US08691818B2

    公开(公告)日：2014-04-08

    申请号：US12811884

    申请日：2009-01-16

    申请人： Michael Leach ,  Laurence Harbige ,  Dieter Riddall ,  Karl Franzmann

    发明人： Michael Leach ,  Laurence Harbige ,  Dieter Riddall ,  Karl Franzmann

    IPC分类号： A61K31/53 ,  C07D253/06 ,  C07D253/08

    CPC分类号： C07D253/075 ,  C07D253/06 ,  C07D253/07 ,  C07D253/10 ,  C07D401/04 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12

    摘要： Compounds of general structure in which X and Y are each N or C with at least one of X and Y being N; Z is a single bond or an optionally substituted linking group R1 is hydrogen or a substituent group; R2 is amino or a substituent group; N* is amino when RI is hydrogen or ═NH when R1 is a substituent group; or N* is a group NRaRb where Ra and Rb are independently H or an alkyl group; or N* is an optionally substituted piperazinyl ring; and A is an optionally substituted heterocyclic or carbocyclic ring system which may be linked to the triazo/diazo ring through R2 to form a fused multicyclic ring; are indicated as suitable for treatment of disorders in mammals that are susceptible to sodium channel blockers and antifolates, and particularly disorders such epilepsy, multiple sclerosis, glaucoma and uevitis, cerebral traumas and cerebral ischaemias, stroke, head injury, spinal cord injury, surgical trauma, neurodegenerative disorders, motorneurone disease, Alzheimer's disease, Parkinson's disease, chronic inflammatory pain, neuropathic pain, migraine, bipolar disorder, mood, anxiety and cognitive disorders, schizophrenia and trigeminal autonomic cephalalgias; for treatment of mammalian cancers; and for treatment of malaria.

    摘要翻译： X和Y各自为N或C，X和Y中的至少一个为N的一般结构化合物; Z是单键或任选取代的连接基团R 1是氢或取代基; R2是氨基或取代基; 当R 1为氢时，N *为氨基，或当R 1为取代基时为= NH; 或N *为NRaRb基团，其中Ra和Rb独立地为H或烷基; 或N *是任选取代的哌嗪基环; 并且A是任选取代的杂环或碳环系，其可以通过R 2与三偶氮/重氮环连接以形成稠合多环; 适用于治疗对钠通道阻滞剂和抗叶酸剂敏感的哺乳动物的疾病，特别是诸如癫痫，多发性硬化，青光眼和uev病，脑创伤和脑缺血性脑卒中，脑损伤，脊髓损伤，手术创伤 神经退行性疾病，运动​​神经元疾病，阿尔茨海默病，帕金森病，慢性炎性疼痛，神经性疼痛，偏头痛，双相情感障碍，情绪，焦虑和认知障碍，精神分裂症和三叉神经性自主性头痛。 用于治疗哺乳动物癌症; 并用于治疗疟疾。