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    Immunosuppressive drug
    1.
    发明授权
    Immunosuppressive drug 失效
    免疫抑制药

    公开(公告)号：US5686479A

    公开(公告)日：1997-11-11

    申请号：US244811

    申请日：1994-06-10

    申请人： Takeki Okumoto ,  Kenji Chiba ,  Yukio Hoshino ,  Hirotsugu Komatsu ,  Mariko Nagasawa ,  Hidekazu Aratani ,  Michio Terasawa ,  Minoru Moriwaki

    发明人： Takeki Okumoto ,  Kenji Chiba ,  Yukio Hoshino ,  Hirotsugu Komatsu ,  Mariko Nagasawa ,  Hidekazu Aratani ,  Michio Terasawa ,  Minoru Moriwaki

    IPC分类号： A61K31/55 ,  C07D495/14 ,  C07D495/22 ,  A61K31/41

    CPC分类号： C07D495/14 ,  A61K31/55

    摘要： An immunosuppressive drug, an autoimmune disease treating drug, an immunosuppression enhancing drug and a cell adhesion inhibitor, each containing a thienotriazolodiazepine compound wherein the 2-position of its diazepine ring is alkylated as an active ingredient, an immunosuppression method, an autoimmune disease treating method, an immunosuppression enhancing method and a cell adhesion inhibiting method, each of which comprising administering the compound, and uses of the compound for the production of an immunosuppressive drug, an autoimmune disease treating drug, an immunosuppression enhancing drug and a cell adhesion inhibitor.

    摘要翻译： PCT No.PCT / JP92 / 01619 Sec。 371日期：1994年6月10日 102（e）日期1994年6月10日PCT提交1992年12月10日PCT公布。 公开号WO93 / 12117 日期：1993年6月24日免疫抑制药物，自身免疫疾病治疗药物，免疫抑制增强药物和细胞粘附抑制剂，其各自含有噻吩并三氮杂环庚烯化合物，其中二氮杂环的2位被烷基化为活性成分，免疫抑制法， 一种自身免疫疾病治疗方法，免疫抑制增强方法和细胞粘附抑制方法，其包括施用该化合物，以及该化合物用于制备免疫抑制药物，自身免疫疾病治疗药物，免疫抑制增强药物和 细胞粘附抑制剂。

    Thienotriazolodiazepine compound and pharmaceutical use thereof
    4.
    发明授权
    Thienotriazolodiazepine compound and pharmaceutical use thereof 失效
    噻吩并三唑并噻嗪类化合物及其药物用途

    公开(公告)号：US5721231A

    公开(公告)日：1998-02-24

    申请号：US535913

    申请日：1995-09-28

    申请人： Minoru Moriwaki ,  Hiroyuki Kitani ,  Syuji Ehara ,  Hirotsugu Komatsu ,  Mariko Amano

    发明人： Minoru Moriwaki ,  Hiroyuki Kitani ,  Syuji Ehara ,  Hirotsugu Komatsu ,  Mariko Amano

    IPC分类号： C07D495/14 ,  A61K31/55

    CPC分类号： C07D495/14

    摘要： N-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno �3,2-f!�1,2,4!triazolo�4,3-a!�1,4!diazepin-6-yl )-N'- (2-methoxyphenyl)urea, optical isomers thereof and pharmaceutically acceptable salts thereof. The compounds of the present invention strongly and selectively inhibit the expression of VCAM-1 and have an inhibitory effect on leukocyte adhesion to vascular endothelial cells. Accordingly, the compounds of the present invention can be used as cell adhesion inhibitors for prophylaxis or treatment of various diseases in which cell adhesion is involved in the onset and progress thereof.

    摘要翻译： N-（4-（4-氯苯基）-2,3,9-三甲基-6H-噻吩并〔3,2-f〕〔1,2,4〕三唑并〔4,3-a〕〔1,4〕二氮杂 -6-基）-N'-（2-甲氧基苯基）脲，其旋光异构体和其药学上可接受的盐。 本发明化合物强烈和选择性地抑制VCAM-1的表达，并且对白细胞对血管内皮细胞的粘附具有抑制作用。 因此，本发明的化合物可以用作细胞粘附抑制剂，用于预防或治疗其起因和进展中涉及细胞粘附的各种疾病。

    Immunosuppressive factor
    6.
    发明授权
    Immunosuppressive factor 失效
    免疫抑制因子

    公开(公告)号：US5037958A

    公开(公告)日：1991-08-06

    申请号：US146167

    申请日：1987-12-12

    申请人： Yoshiyuki Hashimoto ,  Kenji Chiba ,  Hirotsugu Komatsu ,  Takeki Okumoto

    发明人： Yoshiyuki Hashimoto ,  Kenji Chiba ,  Hirotsugu Komatsu ,  Takeki Okumoto

    IPC分类号： C12P21/00 ,  A61K35/12 ,  A61K38/00 ,  A61P37/06 ,  C07K14/005 ,  C07K14/195 ,  C07K14/52 ,  C12R1/91

    CPC分类号： A61K38/1709 ,  A61K35/17 ,  Y10S530/827 ,  Y10S530/829

    摘要： A new immunosuppressive factor derived from human T cell leukemia cells characterized by the following properties:(1) molecular weight: 45,000 to 65,000 daltons and 150,000 to 200,000 daltons by gel filtration, and approximately 31,000 daltons by SDS-polyacrylamide gel electrophoresis;(2) isoelectric point: 4.6 to 4.8;(3) being elutable at a concentration of 0.31 to 0.32 M sodium chloride by FPLC-Mono Q anion exchange chromatography;(4) not adsorbable to immobilized concanavalin A Sepharose or blue Sepharose;(5) resistant to deoxyribonuclease, ribonuclease, papin and periodic acid but sensititive to trypsin, .alpha.-chymotrypsin or pronase;(6) stable at pH 2 to 10;(7) stable for a long time at 4.degree. C. but partially inactivated by heat treatment at 56.degree. C. or 90.degree. C. for 30 minutes;(8) not inhibitable by 2-mercaptoethanol, levamisole, N-acetyl-D-glucosamine, N-acetyl-D-galactosamine, .alpha.-methyl-D-mannoside, L-arginine or L-ornithine;(9) suppressing production of antibody;(10) suppressing blastogeneis of lymphocytes;(11) suppressing cell proliferation; and(12) having structural amino acid and specific contents thereof.This immunosuppressive factor has an excellent immunosuppressing effect and is useful as medicine or reagent.