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    Oligocycloalkanoid compounds and methods of use
    9.
    发明授权
    Oligocycloalkanoid compounds and methods of use 失效
    寡核苷酸类化合物及其使用方法

    公开(公告)号：US06562782B1

    公开(公告)日：2003-05-13

    申请号：US09568403

    申请日：2000-05-10

    申请人： Benjamin L. Miller ,  Robert D. Hubbard

    发明人： Benjamin L. Miller ,  Robert D. Hubbard

    IPC分类号： A61K31015

    CPC分类号： A61K31/405 ,  A61K31/015 ,  A61K31/198 ,  Y02A50/411 ,  Y02A50/414 ,  Y02A50/423

    摘要： The present invention related to an oligocycloalkanoid compound comprising formula (I) wherein m, n, and o are independently an integer from 0 to 2; A1 through A10 are independently a direct link, alkylene, alkylene-O—, carbonyl, oxygen, or sulfur; X and Y are independently hydrogen, hydroxy, alkyl, or in combination an electrophilic group; and R1 through R10 are independently hydrogen, hydroxy, alkyl, alkenyl, alkynyl, substituted or unsubstituted aryl, N-, S-, or O-heterocycles, fused or multi-ring aryl with or without hetero ring members, arylalkyl, arylalkenyl, arylalkynyl, alkylphenyl, alkenylphenyl, alkynylphenyl, alkoxy, alkenyloxy, alkynyloxy, substituted or unsubstituted aryloxy, substituted or unsubstituted arylalkoxy, alkylacyl, alkenylacyl, alkynylacyl, arylacyl, aroyl, alkylaroyl, aminoaroyl, aminoalkylacyl, aminoalkyl, aminoalkenyl, aminoalkynyl, amino, alkylamino, alkenylamino, alkynylamino, arylamino, dialkylamino, dialkenylamino, dialkynylamino, arylalkylamino, arylalkenylamino, imino, alkylimino, alkenylimino, alkynylimino, arylimino, thiol, sulfoxide, alkyl sulfonamide, alkenyl sulfonamide, alkynyl sulfonamide, aryl sulfonamide, alkyl sulfonate ester, alkenyl sulfonate ester, alkynyl sulfonate ester, aryl sulfonate ester, amino acid, or polypeptide, with at least one of R1 through R4 and at least one of R7 through R10 being other than hydrogen. Also disclosed are a pharmaceutical composition including an oligocycloalkanoid compound of the present invention, and methods of using such compounds or compositions for treating a bacterial infection, inhibiting or treating septic shock, treating a disease caused by bacterial endotoxin, and inhibiting the activity of cathepsin K.

    摘要翻译： 本发明涉及包含式（I）的寡核苷酸化合物，其中m，n和o独立地为0至2的整数; A1至A10独立地为直链，亚烷基，亚烷基-O-，羰基，氧或硫; X和Y独立地是氢，羟基，烷基或者亲电基团的组合; R 1至R 10独立地为氢，羟基，烷基，烯基，炔基，取代或未取代的芳基，N-，S-或O-杂环，具有或不具有杂环成员的稠合或多环芳基，芳基烷基，芳基烯基，芳基炔基 烷基苯基，烯基苯基，炔基苯基，烷氧基，烯氧基，炔氧基，烷氧基，烯氧基，炔氧基，取代或未取代的芳氧基，取代或未取代的芳基烷氧基，烷基酰基，链烯基酰基，炔酰基，芳基酰基，芳酰基，烷酰基，氨基酰基，氨基烷基酰基，氨基烷基，氨基烯基，氨基炔基，氨基，烷基氨基， 炔基氨基，芳基氨基，二烷基氨基，二烷基氨基，二炔基氨基，芳基烷基氨基，芳基烯基氨基，亚氨基，烷基亚氨基，烯基亚氨基，炔基亚氨基，芳基亚氨基，硫醇，亚砜，烷基磺酰胺，烯基磺酰胺，炔基磺酰胺，芳基磺酰胺，烷基磺酸酯，链烯基磺酸酯，炔基 磺酸酯，芳基磺酸酯，氨基酸或多肽，与至少一个R1至R4和至少一个 R7至R10不是氢。 还公开了包含本发明的低聚核糖类化合物的药物组合物，以及使用这些化合物或组合物治疗细菌感染，抑制或治疗败血性休克，治疗细菌内毒素引起的疾病和抑制组织蛋白酶K的活性的方法 。