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    METHOD FOR IN VIVO DETECTING TARGET PROTEIN GENE BY DRUG
    3.
    发明公开
    METHOD FOR IN VIVO DETECTING TARGET PROTEIN GENE BY DRUG 失效
    VERFAHREN ZUR BESTIMMUNG DES GENS EINES ZIELPROTEINS MIT HILEL EINES MEDIKAMENTES

    公开(公告)号：EP1072688A1

    公开(公告)日：2001-01-31

    申请号：EP98914021.5

    申请日：1998-04-15

    申请人： Hidaka, Hiroyoshi

    发明人： HIDAKA, Hiroyoshi ,  TANAKA, Hideki

    IPC分类号： C12Q1/68 ,  G01N33/53

    CPC分类号： C12N15/1048

    摘要： A method for detecting a gene of a drug-targeted protein in a living organism, which method includes causing an antigenic substance to be bound to a drug via a chemical cross-linker, the drug being administered to the living organism; using the obtained material as a probe; and directly screening the gene of the protein bound to the probe by use of a cDNA expression library containing genes of the living organism to which the drug is to be administered.
    The method of the present invention has eliminated the need for the protein purification step and amino acid sequence analysis, which are necessary when a conventional drug-fixed column method is performed. Also, the method of the present invention has enabled direct and simple isolation of the gene of the protein to which the drug is targeted.

    摘要翻译： 一种用于检测活体中药物靶向蛋白质的基因的方法，该方法包括使抗原物质通过化学交联剂与药物结合，所述药物被施用于所述活体; 使用获得的材料作为探针; 并通过使用含有待给药药物的生物体的基因的cDNA表达文库直接筛选与探针结合的蛋白质的基因。 本发明的方法消除了在进行常规药物固定柱方法时必需的蛋白质纯化步骤和氨基酸序列分析的需要。 此外，本发明的方法能够直接和简单地分离药物靶向的蛋白质的基因。

    APOVINCAMINIC ACID DERIVATIVE AND MEDICINE CONTAINING THE SAME
    4.
    发明公开
    APOVINCAMINIC ACID DERIVATIVE AND MEDICINE CONTAINING THE SAME 失效
    阿朴氨酸衍生物和含有它的药物

    公开(公告)号：EP0864571A1

    公开(公告)日：1998-09-16

    申请号：EP95938607.9

    申请日：1995-11-29

    申请人： Hidaka, Hiroyoshi

    发明人： HIDAKA, Hiroyoshi ,  ISHIKAWA, Tomohiko ,  MURAMATSU, Hiroshi ,  INOUE, Tsutomu

    IPC分类号： C07D461/00 ,  A61K31/435

    CPC分类号： C07D461/00

    摘要： This invention relates to an apovincaminic acid derivative represented by the following formula (1):
    wherein R 1 represents a lower alkyl group, and R 2 represents an aryl group, which may be substituted by 1 to 5 substituents selected from halogen atoms and lower alkyl, lower alkoxy, lower alkoxycarbonyl, acylamino and nitro groups, a benzyl group, a quinolyl group or a thienyl group, or an acid addition salt thereof; and also to a drug containing the same. This compound has excellent vasodilating activity and platelet aggregation inhibiting activity, and can be used for the treatment of cerebrovascular disorder, thromboembolism and chronic arterial occlusive diseases and also for the improvement of blood flow disturbances.

    摘要翻译： 本发明涉及由下式（1）表示的阿朴长春蔓宁酸衍生物：其中R 1表示低级烷基，并且R 2表示可以被1-5个选自卤素原子和低级烷基的取代基取代的芳基，低级 烷氧基，低级烷氧羰基，酰氨基和硝基，苄基，喹啉基或噻吩基，或其酸加成盐; 还涉及含有它的药物。 该化合物具有优异的血管舒张活性和血小板凝聚抑制活性，可用于治疗脑血管障碍，血栓栓塞症和慢性动脉闭塞性疾病，也可用于改善血流紊乱。

    ISOQUINOLINESULFONAMIDE DERIVATIVES AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT
    5.
    发明公开
    ISOQUINOLINESULFONAMIDE DERIVATIVES AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT 失效
    异喹啉磺酰胺衍生物和含有该衍生物的药物作为活性成分

    公开(公告)号：EP1074545A1

    公开(公告)日：2001-02-07

    申请号：EP98917644.1

    申请日：1998-04-23

    申请人： Hidaka, Hiroyoshi

    发明人： HIDAKA, Hiroyoshi ,  MURAMATSU, Hiroshi

    IPC分类号： C07D217/02 ,  C07D217/24 ,  C07D401/12 ,  A61K31/495 ,  A61K31/55

    CPC分类号： C07D401/12 ,  C07D217/02 ,  C07D217/04 ,  C07D217/24

    摘要： This invention relates to isoquinolinesulfonamide derivatives represented by the following formula (1):
    wherein A represents a linear or branched alkylene group, R 1 represents a hydrogen atom, an hydroxyl, alkoxy or alkyl group or the like, R 2 represents a hydrogen atom, an alkyl group or the like, R 3 represents a hydrogen atom, an alkyl group or the like, and R 4 and R 5 may be the same or different and individually represent hydrogen atoms or lower alkyl groups; N-oxides and salts thereof; and solvates thereof. This invention is also concerned with pharmaceutical compositions, which contain the derivatives, N-oxides, salts, or solvates. These derivatives, N-oxides, salts, and solvates have viral proliferation inhibiting activities and are useful as AIDS therapeutics.

    摘要翻译： 本发明涉及由下式（1）表示的异喹啉磺酰胺衍生物：其中A表示直链或支链亚烷基，R 1表示氢原子，羟基，烷氧基或烷基等，R 2表示氢原子，烷基 基团等，R 3表示氢原子，烷基等，并且R 4和R 5可以相同或不同并且各自表示氢原子或低级烷基; 其N-氧化物和盐; 和它们的溶剂化物。 本发明还涉及含有衍生物，N-氧化物，盐或溶剂合物的药物组合物。 这些衍生物，N-氧化物，盐和溶剂化物具有病毒增殖抑制活性并可用作AIDS治疗剂。

    METHOD FOR IN VIVO DETECTING A TARGET PROTEIN GENE BY A DRUG
    6.
    发明授权
    METHOD FOR IN VIVO DETECTING A TARGET PROTEIN GENE BY A DRUG 失效
    PROCEDURE用于确定所述基因中的靶蛋白的使用的药物

    公开(公告)号：EP1072688B1

    公开(公告)日：2004-06-30

    申请号：EP98914021.5

    申请日：1998-04-15

    申请人： Hidaka, Hiroyoshi

    发明人： HIDAKA, Hiroyoshi ,  TANAKA, Hideki

    IPC分类号： C12N15/10

    CPC分类号： C12N15/1048

    摘要： A method for in vivo detecting a target protein gene by a drug, which comprises binding an antigenic substance to a drug to be administered to a living organism via a chemical crosslinker, using the obtained material as a probe, and directly screening the gene of the protein bonded to the above probe by using a cDNA expression library containing genes of the living organism to which the drug is to be administered. Compared with the conventional drug-fixed column methods, the above method makes it possible to directly and conveniently isolate the gene of the target molecule without resort to the purification of the protein and the analysis of the amino acid sequence thereof.

    ISOQUINOLINE DERIVATIVES AND DRUGS
    8.
    发明公开
    ISOQUINOLINE DERIVATIVES AND DRUGS 失效
    ARZNEIMITTEL公司的ISOCHINOLINDERIVATE

    公开(公告)号：EP0885888A1

    公开(公告)日：1998-12-23

    申请号：EP97901806.6

    申请日：1997-01-31

    申请人： NIPPON SHINYAKU COMPANY, LIMITED

    发明人： HIDAKA, Hiroyoshi ,  MATSUURA, Akira ,  MATSUZAKI, Takushi

    IPC分类号： C07D217/02 ,  C07D217/22 ,  C07D401/12 ,  C07D471/08 ,  C07D487/18 ,  A61K31/495 ,  A61K31/55

    CPC分类号： C07D401/12 ,  A61K31/495 ,  C07D217/02 ,  C07D217/04 ,  C07D217/22 ,  C07D471/08

    摘要： The invention relates to a compound of the following general formula [I] or a medicinally acceptable salt thereof, or a solvate thereof,
    wherein R 1 represents alkyl, alkenyl, alkynyl, alkoxy, hydroxy, cyano, or halogen; R 2 represents hydrogen, hydroxy, or halogen; R 3 represents hydrogen, alkyl, or amidino; Ring A represents a 5 to 11-membered cyclic amino group which may be substituted, which cyclic amino group may be bridged between two carbon atoms in optional positions.
    The compound of this invention is useful for the prevention or treatment of cerebral tissue impairment due to the vasospasm following cerebral hemorrhage.

    摘要翻译： 本发明涉及以下通式的化合物或其药学上可接受的盐或其溶剂化物，其中R 1表示烷基，烯基，炔基，烷氧基，羟基，氰基或卤素; R 2表示氢，羟基或卤素; R 3表示氢，烷基或脒基; 环A表示可被取代的5至11元环状氨基，该环状氨基可以在任选位置的两个碳原子之间桥连。 本发明的化合物可用于预防或治疗脑出血后血管痉挛引起的脑组织损伤。