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    • 1. 发明授权
    • Method for preparation of carborane anions
    • 碳硼烷阴离子的制备方法
    • US07161040B2
    • 2007-01-09
    • US10472329
    • 2002-04-01
    • Andreas FrankenBenjamin T. KingJosef Michl
    • Andreas FrankenBenjamin T. KingJosef Michl
    • C07C331/00C07C335/00C07C381/00
    • C07F5/027
    • This invention relates to an improved method for making unsubstituted carborane anions and monosubstituted carborane anions of formula: (R—CBn—Hm′)− where n is an integer ranging from 5 to about 11 and m′ is an integer ranging from 5 to 16 where the relative values of n and m′ depend upon the exact structure of the carborane and the presence of a non-hydrogen substituent. m as used herein is an integer ranging from 5 to 16. When R is hydrogen the anion is unsubstituted. When R is a halogen, a phenyl, a substituted phenyl group, such as fluorophenyl group, or any other substituent, the carborane is substituted. The method is particularly useful for preparation of twelve-vertex carborane anions R—CB11H11−, where R is a defined above, and is specifically useful for preparation of the unsubstituted carborane CB11H12-??, where R is H.
    • 本发明涉及一种制备未取代的碳硼烷阴离子和具有下式的单取代的碳硼烷阴离子的改进方法:(R-CB N-H) - H SUP >其中n是5至约11的整数,m'是5至16的整数,其中n和m'的相对值取决于碳硼烷的精确结构和非氢取代基的存在。 m为5〜16的整数。当R为氢时,阴离子为未取代的。 当R是卤素时,苯基,取代的苯基,例如氟苯基或任何其它取代基,碳硼烷被取代。 该方法对于制备十二个顶点碳硼烷阴离子R-CB 11,其中R为上述定义,特别有用,以及 特别适用于制备未取代的碳硼烷CB 11 H 12 -12,其中R为H.
    • 10. 发明授权
    • Peptides selectively lethal to malignant and transformed mammalian cells
    • 对恶性和转化的哺乳动物细胞选择性致死的肽
    • US07883888B2
    • 2011-02-08
    • US10549048
    • 2004-01-13
    • Josef MichlJesko KoehnkeMatthew R. Pincus
    • Josef MichlJesko KoehnkeMatthew R. Pincus
    • C12N15/00
    • C07K14/4746A61K38/00
    • The present invention provides peptides corresponding to all or a portion of amino acid residues 12-26 of human p53 protein, which peptides are lethal to malignant or transformed cells when fused to a membrane-penetrating leader sequence. The subject peptides are thus useful in treating neoplastic disease in an animal, preferably a human. Also provided are pharmaceutical compositions comprising the subject peptides admixed with a pharmaceutical acceptable carrier. Methods of treating neoplastic disease in a patient by administering a subject peptide fused at its carboxy terminal end to a membrane penetrating leader sequence are also provided. The present invention also provides replication incompetent Adenovirus (AdV) vectors comprising a promoter sequence operably linked to a nucleotide sequence encoding a subject peptide. Methods of selectively killing cancer cells in a subject by administering a therapeutically effective amount of a subject AdV vector are also provided by the present invention.
    • 本发明提供对应于人p53蛋白的全部或部分氨基酸残基12-26的肽,当与透膜前导序列融合时,该肽对恶性或转化细胞致死。 因此,本发明的肽可用于治疗动物,优选人类的肿瘤性疾病。 还提供了包含与药学上可接受的载体混合的受试肽的药物组合物。 还提供了通过将其羧基末端融合的受试肽施用于穿透前导序列的方法来治疗患者的肿瘤疾病。 本发明还提供了复制无能力的腺病毒(Adv)载体,其包含可操作地连接到编码目标肽的核苷酸序列的启动子序列。 通过施用治疗有效量的受试者AdV载体选择性地杀死受试者的癌细胞的方法也由本发明提供。