QUENCHER
    73.
    发明公开
    QUENCHER 审中-公开
    骤冷

    公开(公告)号:EP3235876A1

    公开(公告)日:2017-10-25

    申请号:EP15870088.0

    申请日:2015-12-18

    摘要: Conventional quenchers do not have quenching ability enough to suppress fluorescence emission of compounds having fluorescent property. Accordingly, it is an object of the present invention to provide a quencher capable of sufficiently quenching fluorescence of the compound having fluorescent property, including a xanthene-based dye.
    The present invention relates to a quencher, or the like, comprising a compound represented by the following general formula (1):

    [wherein R 5 each independently represent a halogen atom, an alkyl group, an alkoxy group, an alkylthio group, an amino group having a substituent or not having a substituent, a hydroxy group, an aryl group, an aryloxy group, or an arylalkyl group; R 6 represents a group having a polymerizable unsaturated group, a hydroxy group, or the like; Y 1 represents an oxygen atom, or the like; An - represents an anion; Ar 1 represents a specific ring structure; * and ** represent binding positions; Ar 2 represents a benzene ring, a naphthalene ring, or an anthracene ring; n 1 represents a specific integer;
    and the following structure (1-10) in the general formula (1) is an asymmetric structure;

    (wherein R 5 , Y 1 , Ar 1 , Ar 2 , n 1 , * and ** are the same as described above.).].

    摘要翻译: 常规猝灭剂不具有足以抑制具有荧光特性的化合物的荧光发射的猝灭能力。 因此,本发明的目的是提供能够充分猝灭包括x吨系染料在内的具有荧光性的化合物的荧光的猝灭剂。 本发明涉及包含由下述通式(1)表示的化合物的猝灭剂等:[其中R 5各自独立地表示卤素原子,烷基,烷氧基,烷硫基,氨基 具有或不具有取代基的取代基,羟基,芳基,芳氧基或芳基烷基; R6表示具有聚合性不饱和基团,羟基等的基团; Y1表示氧原子等; An-代表阴离子; Ar1表示特定的环结构; *和**代表结合位置; Ar 2表示苯环,萘环或蒽环; n1表示特定的整数; 以及通式(1)中的以下结构(1-10)为不对称结构; (其中R5,Y1,Ar1,Ar2,n1,*和**与上述相同。)。]。

    A USE OF ALKALOID IN PREPARING PHARMACEUTICAL COMPOSITIONS FOR PREVENTING OR TREATING PULMONARY FIBROSIS
    74.
    发明公开
    A USE OF ALKALOID IN PREPARING PHARMACEUTICAL COMPOSITIONS FOR PREVENTING OR TREATING PULMONARY FIBROSIS 审中-公开
    VERWENDUNG VON ALKALOID贝德赫斯通公司VAR PHARMAZEUTISCHEN ZUSAMMENSETZUNGEN ZUR VORBEUGUNG ODER BEHANDLUNG VON LUNGENFIBROSE

    公开(公告)号:EP3175854A4

    公开(公告)日:2017-09-13

    申请号:EP15827281

    申请日:2015-06-17

    摘要: Disclosed is a new use of a compound as indicated in structural formula I in preparing medications for preventing and/or treating pulmonary fibrosis. The compound having the structure as indicated in structural formula 1 substantially reduces the inflammation of diseased lung tissue, lowers the concentration of fibrosis factors TGF-²l in diseased lung tissue, decreases the excessive deposition of collagen in diseased lung tissue, and has substantial prevention and treatment effectiveness against fibrosis.

    摘要翻译: 公开了如结构式I所示的化合物在制备用于预防和/或治疗肺纤维化的药物中的新用途。 具有结构式1所示结构的化合物基本上减少患病肺组织的炎症,降低患病肺组织中纤维化因子TGF-β1的浓度,减少胶原在患病肺组织中的过度沉积,并且具有实质性的预防和 治疗纤维化的有效性。

    1,4,7,10-Tetrazacyclododecane based agents to target bacteria and its use
    77.
    发明公开
    1,4,7,10-Tetrazacyclododecane based agents to target bacteria and its use 审中-公开
    Mittel auf 1,4,7,10-Tetraazacyclododecanbasis zum Abzielen auf Bakterien und deren Verwendung

    公开(公告)号:EP2987792A1

    公开(公告)日:2016-02-24

    申请号:EP14181231.3

    申请日:2014-08-18

    摘要: The present invention relates to new compounds comprising a siderophore moiety as well as a core structure able to chelate a metal ion. Optionally, the compounds may have additionally a moiety with a functional element including a marker molecule, a bioactive agent, an activity based probe suitable to monitor the aberrant expression or activity of proteins involved in the initiation and progression of bacterial infection, or a compound useful for bacterial inhibition. In a further aspect, the present invention provides a pharmaceutical composition containing said compound, for example, said pharmaceutical composition is an antibiotic. Additionally, the present invention relates to the use of said compounds in diagnostic methods, in particular, imaging methods including SPEC, PET or MRI. In an embodiment of the present invention, the compound is part of a theranostic composition having both, therapeutic as well as diagnostic activities.

    摘要翻译: 本发明涉及包含铁载体部分的新化合物以及能够螯合金属离子的核心结构。 任选地,所述化合物可以另外具有包含标记分子,生物活性剂,适于监测参与细菌感染的起始和进展的蛋白质的异常表达或活性的基于活性的探针的功能元件的部分或有用的化合物 用于细菌抑制。 另一方面,本发明提供含有所述化合物的药物组合物,例如所述药物组合物是抗生素。 另外,本发明涉及所述化合物在诊断方法中的用途,特别是包括SPEC,PET或MRI的成像方法。 在本发明的一个实施方案中,化合物是具有治疗和诊断活性两者的组氨酸组合物的一部分。

    SUBSTITUTED PYRANO [2, 3 - B]PYRIDINE DERIVATIVES AS CANNABINOID-1 RECEPTOR MODULATORS
    80.
    发明授权
    SUBSTITUTED PYRANO [2, 3 - B]PYRIDINE DERIVATIVES AS CANNABINOID-1 RECEPTOR MODULATORS 有权
    取代的吡喃并[2,3 - B]吡啶衍生物ALS大麻素-1受体调节剂

    公开(公告)号:EP2109615B1

    公开(公告)日:2011-03-09

    申请号:EP08713287.4

    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.