公开(公告)号：EP0955313A4

公开(公告)日：2001-11-07

申请号：EP96910198

申请日：1996-04-19

申请人： HOECHST MARION ROUSSEL LTD

发明人： MAKISHIMA FUSAO ,  TAKAMATSU HIROYUKI ,  MIKI HIDEO ,  KAWAI SHINJI ,  KIMURA MICHIO ,  MATSUMOTO TOMOAKI ,  KATSUURA MIEKO ,  ENOMOTO KOICHI ,  SATOH YUSUKE

IPC分类号： A61K38/00 ,  C07K14/51 ,  C12N1/21 ,  C12N15/12 ,  A61K38/17 ,  C12P21/02

CPC分类号： C07K14/51 ,  A61K38/00 ,  Y10S514/801

摘要： A protein comprising an amino acid sequence represented by SEQ ID NO: 1 in the Sequence Listing and originating in human MP52 and the dimer of this protein. This dimer protein can be obtained by constructing a plasmid containing a DNA wherein a codon encoding methionine is added to the 5' end of a DNA sequence encoding the above-mentioned aminoacid sequence, transforming Escherichia coli by this plasmid, incubating the E. coli transformant, solubilizing and purifying the obtained inclusion body to thereby give a monomer protein, and then renaturing the obtained monomer protein into the dimer followed by purification. This dimer protein is useful in the treatment of cartilage and bone diseases.

摘要翻译： 一种蛋白质，其包含序列表中SEQ ID NO：1所示的氨基酸序列，并且源自人MP52和该蛋白质的二聚体。 该二聚体蛋白质可通过构建含有DNA的质粒来获得，其中在编码上述氨基酸序列的DNA序列的5'末端添加编码甲硫氨酸的密码子，用该质粒转化大肠杆菌，将大肠杆菌转化体 ，将得到的包涵体溶解并纯化，由此得到单体蛋白质，然后将获得的单体蛋白质复性成二聚体，然后纯化。 该二聚体蛋白质可用于治疗软骨和骨骼疾病。

公开(公告)号：EP0994093A4

公开(公告)日：2000-05-17

申请号：EP97922050

申请日：1997-05-14

申请人： HOECHST MARION ROUSSEL LTD

发明人： SAKAI KUNIKAZU ,  SATOH YUSUKE ,  DOI KAZUYUKI ,  KITAMURA KAZUYUKI

IPC分类号： A61K31/12 ,  A61P3/00 ,  A61P19/10 ,  A61P43/00 ,  C07C45/00 ,  C07C45/46 ,  C07C45/51 ,  C07C45/62 ,  C07C45/68 ,  C07C45/71 ,  C07C49/713 ,  C07C49/743 ,  C07C49/747 ,  C07C49/825 ,  C07C49/83 ,  C07C49/835 ,  C07C49/84

CPC分类号： C07C49/84 ,  C07C45/00 ,  C07C45/46 ,  C07C45/512 ,  C07C45/62 ,  C07C45/68 ,  C07C45/71 ,  C07C49/713 ,  C07C49/743 ,  C07C49/747 ,  C07C49/825 ,  C07C49/83 ,  C07C49/835

摘要： Compounds useful as preventive and therapeutic agents for bone and cartilage diseases; and drug compositions containing the same. The compounds are polyhydroxyphenol derivatives of general formula (I) and quinone analogues derived therefrom (wherein R1 is alkyl, optionally substituted benzyl or optionally substituted aryl; R2 is hydrogen, alkyl, alkenyl or optionally substituted benzyl; R3 is hydrogen, alkyl, alkenyl, optionally substituted benzyl, hydroxyl, alkoxy, alkenyloxy or optionally substituted benzyloxy; R4 is hydrogen, alkyl, alkenyl, optionally substituted benzyl or hydroxyl; and R5 and R6 are each independently hydrogen, alkyl, alkenyl or optionally substituted benzyl). The polyhydroxyphenol derivatives and the quinone analogues exhibit a potent inhibitory activity against bone resorption and are useful as preventive and therapeutic agents for bone and cartilage diseases.

摘要翻译： 用作骨和软骨疾病预防和治疗剂的化合物; 和含有它们的药物组合物。 所述化合物是通式（I）的多羟基酚衍生物和由其衍生的醌类似物（其中R1是烷基，任选取代的苄基或任选取代的芳基; R2是氢，烷基，烯基或任选取代的苄基; R3是氢，烷基， 任选取代的苄基，羟基，烷氧基，烯氧基或任选取代的苄氧基; R 4为氢，烷基，烯基，任选取代的苄基或羟基;并且R 5和R 6各自独立地为氢，烷基，烯基或任选取代的苄基。 多羟基酚衍生物和醌类似物表现出对骨吸收的有效抑制活性，并且可用作骨和软骨疾病的预防和治疗剂。