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    TRYCICLIC OR TETRACYCLIC COMPOUNDS, PROCESS FOR THEIR PREPARATION, AND MEDICINAL COMPOSITION CONTAINING THEM
    2.
    发明授权
    TRYCICLIC OR TETRACYCLIC COMPOUNDS, PROCESS FOR THEIR PREPARATION, AND MEDICINAL COMPOSITION CONTAINING THEM 失效
    TRYCICLIC或TETRACYCLIC化合物，其制备方法和含有它们的药物组合物

    公开(公告)号：EP0191867B1

    公开(公告)日：1991-10-16

    申请号：EP85904018.0

    申请日：1985-08-09

    申请人： Dainippon Pharmaceutical Co., Ltd.

    发明人： UNO, Hitoshi ,  KUROKAWA, Mikio ,  SATO, Fuminori ,  HATANO, Naonobu

    IPC分类号： C07D213/74 ,  C07D215/38 ,  C07D239/42 ,  C07D295/14 ,  C07D337/12 ,  C07D401/04 ,  C07D409/12 ,  A61K31/495 ,  A61K31/55 ,  A61K31/505

    CPC分类号： C07D215/38 ,  C07D213/74 ,  C07D239/42 ,  C07D277/38 ,  C07D295/15 ,  C07D337/12 ,  C07D409/12

    摘要： Compounds represented by general formula (I) (wherein A represents alkylene, Y-Z represents formula (II), -CH=CH-, -CH2CH2- or formula (III), R1 and R2 each represents a substituent, R3 represents hydrogen, alkyl or alkoxy, R4 represents phenyl, phenylalkyl, phenylalkenyl, diphenylmethyl, naphthyl, thiazolyl, optionally substituted pyridyl, optionally substituted pyrimidinyl, quinolyl, benzoylalkyl, benzoyl, furoyl, thenoyl, phenyloxycarbonyl, phenyloxysulfonyl or phenylsulfonyl, a represents 2 or 3, b and c each represents 1 or 2, and d represents an integer of 0 to 2, provided that the phenyl, phenyl moiety or naphthyl moiety may be substituted) and salts thereof, processess for their preparation, and medicinal compositions containing them. These compounds show a strong calcium-antagonistic effect, and are therefore useful for prophylaxis and treatment of hypertension and/or ischemic heart diseases.

    摘要翻译： PCT No.PCT / JP85 / 00445 Sec。 一九八六年四月十日 102（e）日期1986年4月10日PCT提交1985年8月9日PCT公布。 公开号WO86 / 01203 日期：1986年2月27日。下式的化合物：其中A表示亚烷基; Y-Z表示 -CH = CH-，-CH 2 CH 2 - 或R 1，R 2和R 2各自为取代基; R3是氢原子，烷基或烷氧基; R4是苯基，苯基烷基，苯基链烯基，二苯基甲基，萘基，噻唑基，任选取代的吡啶基，任选取代的嘧啶基，喹啉基，苯甲酰基烷基，苯甲酰基，糠酰基，噻吩甲酰基，苯氧基羰基，苯氧基磺酰基或苯基磺酰基; a为2或3，b和c各自为1或2，d为0至2的整数，条件是苯基，苯基部分和萘基可任选被取代，及其药学上可接受的盐，其制备方法 及含有该组合物的药物组合物。 化合物及其盐显示出有效的钙拮抗活性，可用于预防和治疗高血压和/或缺血性心脏病。

    HETEROCYCLIC COMPOUNDS HAVING ELASTASE−INHIBITING ACTIVITY AND INTERMEDIATES THEREOF
    3.
    发明公开
    HETEROCYCLIC COMPOUNDS HAVING ELASTASE−INHIBITING ACTIVITY AND INTERMEDIATES THEREOF 审中-公开
    兽医学家VERBINDUNGEN MIT ELASTASEHEMMENDER WIRKUNG UND ZWISCHENPRODUKTEDAFÜR

    公开(公告)号：EP1473302A1

    公开(公告)日：2004-11-03

    申请号：EP03737491.5

    申请日：2003-02-05

    申请人： Dainippon Pharmaceutical Co., Ltd.

    发明人： SATO, Fuminori ,  DEGUCHI, Takashi ,  SHIRATAKE, Ryotaro ,  OKAZAKI, Hiroshi ,  KUROMIYA, Akemi

    IPC分类号： C07K5/083 ,  C12N9/99 ,  A61K38/55 ,  A61P11/00 ,  A61P43/00

    CPC分类号： C07K5/06191 ,  A61K38/00

    摘要： Heterocyclic compounds represented by the general formula (I) and having elastase inhibiting activity; and intermediates for the synthesis thereof: (I) wherein R 1 is a heterocyclic group represented by the general formula (II): (II) [wherein A represents the presence or absence of a benzene ring; X is oxygen, sulfur or NH; and Y is nitrogen or CH], and the heterocyclic group may be substituted with one to three substituents which may be the same or different and are selected from the group consisting of lower alkyl, lower alkoxy, and phenyl which may be substituted with optionally halogenated lower alkyl, lower alkoxy or halogeno; and R 2 and R 3 are each hydrogen or hydroxyl, or R 2 and R 3 may be united to form an oxo group, with the proviso that both are not hydrogen.

    摘要翻译： 具有通式（I）表示的并具有弹性蛋白酶抑制活性的杂环化合物 及其合成中间体：（I）其中R 1为通式（II）表示的杂环基：（Ⅱ）Ä其中A表示苯环的存在或不存在; X是氧，硫或NH; 并且Y是氮或CH，并且杂环基可以被一至三个可以相同或不同并且选自低级烷基，低级烷氧基和可被任选卤代低级取代的苯基的取代基取代 烷基，低级烷氧基或卤代; R 2和R 3各自为氢或羟基，或者R 2和R 3可以一起形成氧代基，条件是两者都不是氢。

    PROCESSES FOR PRODUCING (AMINOMETHYL)TRIFLUOROCARBINOL DERIVATIVES
    4.
    发明公开
    PROCESSES FOR PRODUCING (AMINOMETHYL)TRIFLUOROCARBINOL DERIVATIVES 有权
    VERFAHREN ZUR HERSTELLUNG VON（AMINOMETHYL）三氟甲磺酸衍生物

    公开(公告)号：EP1243576A1

    公开(公告)日：2002-09-25

    申请号：EP00905281.2

    申请日：2000-02-23

    申请人： Dainippon Pharmaceutical Co., Ltd.

    发明人： SATO, Fuminori ,  OMODANI, Tomoki ,  SHIRATAKE, Ryotaro ,  INOUE, Yasunao ,  DEGUCHI, Takashi

    IPC分类号： C07C213/02 ,  C07C215/08 ,  C07C269/06 ,  C07C271/16

    CPC分类号： C07C213/02 ,  C07C269/06 ,  Y02P20/55 ,  C07C215/08 ,  C07C271/16

    摘要： The present invention provides a process for industrially producing (aminomethyl)trifluoromethylcarbinol derivatives (I), in particularly, optically active compounds thereof, which are useful as starting compounds for drugs such as protease inhibitors, etc. The present invention relates to a process for producing the compound (I) from 1,3-oxazolidin-5-one derivative (II) being easily derived from an α-amino acid, which is carried out stepwise or by one-spot reaction, and further relates to a process for producing the compound (I) comprising the reduction of the 5-hydroxy compound (II).
    wherein R 1 is a group corresponding to the side chain of a natural or non-natural α-amino acid, R 2 is a hydrogen atom or R 21 (in which R 21 is a protecting group for amino group having a carbonyl group at the binding site to the nitrogen atom).

    摘要翻译： 本发明提供工业上制备（氨基甲基）三甲基甲醇衍生物（I）的方法，特别是其光学活性化合物，其可用作诸如蛋白酶抑制剂等药物的起始化合物。本发明涉及一种生产 来自1,3-恶唑烷-5-酮衍生物（II）的化合物（I）容易从α-氨基酸衍生，其逐步进行或通过一点反应进行，并且还涉及制备 包括还原5-羟基化合物（II）的化合物（I）。 其中R 1为对应于天然或非天然α-氨基酸的侧链的基团，R 2为氢原子或R 21（其中R 21为 在与氮原子的结合位置具有羰基的氨基的保护基）。

    HETEROCYCLIC COMPOUNDS, INTERMEDIATES THEREOF AND ELASTASE INHIBITORS
    5.
    发明公开
    HETEROCYCLIC COMPOUNDS, INTERMEDIATES THEREOF AND ELASTASE INHIBITORS 有权
    HETEROZYKLISCHE VERBINDUNGEN，IHRE ZWISCHENPRODUKTE UND ELASTASE-INHIBITOREN

    公开(公告)号：EP1157998A1

    公开(公告)日：2001-11-28

    申请号：EP00905282.0

    申请日：2000-02-23

    申请人： Dainippon Pharmaceutical Co., Ltd.

    发明人： SATO, Fuminori ,  INOUE, Yasunao ,  OMODANI, Tomoki ,  SHIRATAKE, Ryotaro ,  HONDA, Seiji ,  KOMIYA, Masanobu ,  TAKEMURA, Tadashi

    IPC分类号： C07K5/103 ,  C07K5/083 ,  C07D239/54 ,  C07D233/34 ,  A61K38/55 ,  A61P43/00 ,  A61P11/00

    CPC分类号： C07D403/12 ,  A61K38/00 ,  C07K5/0202 ,  C07K5/0222 ,  C07K5/0806 ,  C07K5/0821 ,  C07K5/1008

    摘要： The present invention relates to a heterocyclic compound of the following formula (I-a), its ester, or a salt thereof, and a human neutrophilic elastase inhibitor containing the same as the active ingredient, etc.
    wherein A and B are the same or different and each is a lower alkylene group being optionally substituted by an oxo group, D is a heteromonocyclic or heterobicyclic group being optionally substituted by an oxo group, R 1 and R 2 are the same or different and each is a lower alkyl group, R 3 and R 4 are different from each other, and each is a hydrogen atom or a hydroxy group, or both combine together to form an oxo group, and R 5 is 2-benzoxazolyl, trifluoromethyl, benzylaminocarbonyl, etc.

    摘要翻译： 本发明涉及下式（Ia）的杂环化合物，其酯或其盐，以及含有该活性成分的人嗜中性粒细胞弹性蛋白酶抑制剂等。＆lt; CHEM＆gt;其中A和B相同 或不同的，并且各自为任选被氧代基取代的低级亚烷基，D是任选被氧代基取代的杂单环或杂双环基团，R 1和R 2相同或不同，并且各自为 低级烷基，R 3和R 4彼此不同，各自为氢原子或羟基，或两者结合在一起形成氧代基，R 5为2-苯并恶唑基， 三氟甲基，苄基氨基羰基等