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    Cyanine-based probe\tag-peptide pair fluorescence protein imaging and fluorescence protein imaging methods
    2.
    发明授权
    Cyanine-based probe\tag-peptide pair fluorescence protein imaging and fluorescence protein imaging methods 有权
    基于花青的探针\标签肽对荧光蛋白成像和荧光蛋白成像方法

    公开(公告)号：US08354499B2

    公开(公告)日：2013-01-15

    申请号：US12773707

    申请日：2010-05-04

    Applicant: M. Uljana Mayer-Cumblidge ,  Haishi Cao

    Inventor： M. Uljana Mayer-Cumblidge ,  Haishi Cao

    IPC: C07K7/06 ,  C07K5/04

    CPC classification number: C09B23/06 ,  C07K1/13 ,  C07K7/06 ,  C09B23/0075 ,  C09B23/083 ,  C09B23/086 ,  G01N33/582 ,  Y10T436/13

    Abstract: A molecular probe comprises two arsenic atoms and at least one cyanine based moiety. A method of producing a molecular probe includes providing a molecule having a first formula, treating the molecule with HgOAc, and subsequently transmetallizing with AsCl3. The As is liganded to ethanedithiol to produce a probe having a second formula. A method of labeling a peptide includes providing a peptide comprising a tag sequence and contacting the peptide with a biarsenical molecular probe. A complex is formed comprising the tag sequence and the molecular probe. A method of studying a peptide includes providing a mixture containing a peptide comprising a peptide tag sequence, adding a biarsenical probe to the mixture, and monitoring the fluorescence of the mixture.

    Abstract translation: 分子探针包含两个砷原子和至少一个基于花青的部分。 制备分子探针的方法包括提供具有第一式的分子，用HgOAc处理分子，随后用AsCl 3进行金属化。 As被配体化为乙二硫醇以产生具有第二式的探​​针。 标记肽的方法包括提供包含标签序列的肽并使肽与双链分子探针接触。 形成包含标签序列和分子探针的复合物。 一种研究肽的方法包括提供含有肽标签序列的肽的混合物，向该混合物中加入双缩醛探针，并监测该混合物的荧光。

    Inhibitors of cancer cell, T-cell and keratinocyte proliferation
    8.
    发明申请
    Inhibitors of cancer cell, T-cell and keratinocyte proliferation 失效
    癌细胞抑制剂，T细胞和角化细胞增殖

    公开(公告)号：US20070037753A1

    公开(公告)日：2007-02-15

    申请号：US11501722

    申请日：2006-08-10

    Applicant: Johann Leban ,  Martin Kralik

    Inventor： Johann Leban ,  Martin Kralik

    IPC: A61K38/05 ,  A61K38/04 ,  C07K5/04 ,  C07D403/02

    CPC classification number: C07D233/72 ,  A61K38/00 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/14 ,  C07K5/0205 ,  C07K5/06078 ,  C07K5/06191 ,  Y02A50/409

    Abstract: The invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein Y is —NRaRb, —NRcC═ONRaRb, —NRcC═SNRaRb, —NRcC═NRdNaRb, heterocycle, —C═ONRaRb, heterocycle, or aryl; n is 0 to 8; m is 0, or 1; r is 0 to 3; t is 0 to 3; X is O or N; Z is CH2, C═O, C═S or a single bond; Z1 is CO—R2, CS—R2, (CH2)t—R2 or the side-chain of a naturally occuring amino acid;, Z2 is CO—R2, CS—R2 or (CH2)t—R3 or the side-chain of a naturally occuring amino acid; Z3 is CO—R2, CS—R2 or (CH2)t—R4 or the side-chain of a naturally occuring amino acid; Z4 is H, alkyl, alkoxy, or cycloalkyl; R1, R2, R3, and R4 are independently from each other H, OH, SH, NH2, CN, NO2, alkyl, cycloalkyl, heterocycloalkyl, haloalkyl, alkylthio, haloalkyloxy, hydroxyalkyl, hydroxyalkylamino, alkylamino, alkylaryl, alkylsulfinyl, alkylsulfonyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, alkoxyalkyl, alkoxy, aryloxy, heteroaryl, aryl, or halogen.

    Abstract translation: 本发明涉及通式（I）的化合物及其盐和生理功能衍生物，其中Y是-NR a，R b， C-ON＆lt; b＆gt; b＆lt;＆lt;＆lt; C＆gt; C-SNR＆lt; b＆gt; b C 1 -C 6卤代烷基，杂环基，C 1 -C 6 - 杂环或芳基;杂环或芳基; n为0〜8; m为0或1; r为0〜3; t为0〜3; X是O或N; Z是CH 2，C-O，C-S或单键; Z 1是CO-R 2，CS-R 2，（CH 2）2， / SUB> -R 2或天然存在的氨基酸的侧链; Z 2是CO-R 2，CS- R 2或（CH 2）2 -TH 3或天然存在的氨基酸的侧链 ; Z 3是CO-R 2，CS-R 2或（CH 2 CH 2） / SUB→4或天然存在的氨基酸的侧链; Z 4是H，烷基，烷氧基或环烷基; R 1，R 2，R 3和R 4彼此独立地为H，OH，SH ，NH 2，CN，NO 2，烷基，环烷基，杂环烷基，卤代烷基，烷硫基，卤代烷氧基，羟烷基，羟烷基氨基，烷基氨基，烷基芳基，烷基亚磺酰基，烷基磺酰基，烷硫基烷基，烷基亚磺酰基烷基 烷基磺酰基烷基，烷氧基烷基，烷氧基，芳氧基，杂芳基，芳基或卤素。

    Oxadiazole derivatives and drugs containing these derivatives as the active ingredient
    10.
    发明申请
    Oxadiazole derivatives and drugs containing these derivatives as the active ingredient 审中-公开
    恶二唑衍生物和含有这些衍生物的药物作为活性成分

    公开(公告)号：US20070004642A1

    公开(公告)日：2007-01-04

    申请号：US11488782

    申请日：2006-07-19

    Applicant: Kazuyuki Ohmoto ,  Iori Itagaki

    Inventor： Kazuyuki Ohmoto ,  Iori Itagaki

    IPC: A61K38/05 ,  A61K38/04 ,  C07K5/06 ,  C07K5/04 ,  C07D413/02

    CPC classification number: C07D271/07 ,  A61K38/00 ,  C07D271/113 ,  C07D413/06 ,  C07D413/12 ,  C07K5/06043 ,  C07K5/06139

    Abstract: An oxadiazole derivative of formula (I) and a non-toxic salt thereof, wherein R is hydrogen, alkyl, CycA, etc.; AA1 is a single bond, amino acid residue, etc.; AA2 is a single bond, amino acid residue, etc.; R7 and R8 are hydrogen, alkyl, etc.; R9 is hydrogen, alkyl, etc.; R10 is hydrogen, alkyl, etc.). The compound of formula (I) has an inhibitory activity against cysteine protease and therefore it is useful as an agent for the prophylaxis and/or treatment of inflammatory diseases, diseases induced by apoptosis, diseases induced by disorders of immune responses, autoimmune diseases, diseases induced by decomposition of proteins which compose organism, shock, circulatory system disorders, blood coagulation system disorders, malignant tumors, acquired immune deficiency syndrome (AIDS) and AIDS-related complex (ARC), parasitic diseases, nerve degeneration diseases, pulmonary disorders, bone resorption diseases, endocrinesthenia, etc.

    Abstract translation: 式（I）的恶二唑衍生物及其无毒盐，其中R为氢，烷基，CycA等; AA 1是单键，氨基酸残基等; AA 2是单键，氨基酸残基等; R 7和R 8是氢，烷基等; R 9为氢，烷基等; R 10是氢，烷基等）。 式（I）化合物对半胱氨酸蛋白酶具有抑制活性，因此可用作预防和/或治疗炎性疾病，由凋亡诱导的疾病，由免疫应答障碍引起的疾病，自身免疫性疾病，疾病 由构成有机体的蛋白质，休克，循环系统疾病，凝血系统疾病，恶性肿瘤，获得性免疫缺陷综合征（AIDS）和AIDS相关复合物（ARC），寄生虫病，神经变性疾病，肺功能障碍，骨骼 吸收疾病，内分泌等

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