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    Peptide compound and its preparation
    5.
    发明授权
    Peptide compound and its preparation 失效
    肽化合物及其制备

    公开(公告)号：US5656604A

    公开(公告)日：1997-08-12

    申请号：US422944

    申请日：1995-04-17

    申请人： Keiji Hemmi ,  Masahiro Neya ,  Naoki Fukami ,  Masashi Hashimoto ,  Hirokazu Tanaka ,  Natsuko Kayakiri

    发明人： Keiji Hemmi ,  Masahiro Neya ,  Naoki Fukami ,  Masashi Hashimoto ,  Hirokazu Tanaka ,  Natsuko Kayakiri

    IPC分类号： A61K38/00 ,  C07K5/02 ,  C07K5/078 ,  C07K5/083 ,  C07K5/103 ,  A61K38/06 ,  C07K5/087 ,  C07K5/097

    CPC分类号： C07K5/06156 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/0207 ,  C07K5/021 ,  C07K5/0217 ,  C07K5/0808 ,  C07K5/101 ,  A61K38/00

    摘要： Peptide compounds of the formula (I') ##STR1## in which R.sup.1 is acyl,R.sup.2 is lower alkyl, cyclo(lower)alkyl(lower)alkyl or optionally substituted heterocyclic(lower)alkyl,R.sup.3 is optionally substituted heterocyclic(lower)alkyl or optionally substituted ar(lower)alkyl,R.sup.4 is lower alkyl, amino(lower)alkyl, protected amino(lower)alkyl, carboxy(lower)alkyl, protected carboxy(lower)alkyl or optionally substituted heterocyclic(lower)alkyl,R.sup.5 is carboxy, protected carboxy, carboxy(lower)alkyl or protected carboxy(lower)alkyl,R.sup.6 is hydrogen, lower alkyl, C.sub.6-10 ar(lower)alkyl amino(lower)alkyl, protected amino(lower)alkyl, carboxy(lower)alkyl, protected carboxy(lower)alkyl, or heterocyclic(lower)alkyl,R.sup.7 is hydrogen or lower alkyl, andA is --O--, --NH--, lower alkylimino or lower alkylene, or a pharmaceutically acceptable salt thereof are disclosed. The compounds can be used to treat and prevent endothelin mediated diseases such as hypertension. The preparation of such peptides is also disclosed.

    摘要翻译： 式（I'）的肽化合物其中R 1是酰基，R 2是低级烷基，环（低级）烷基（低级）烷基或任选取代的杂环（低级）烷基），其中R 1是任选取代的杂环 （低级）烷基或任选取代的芳（低级）烷基，R 4是低级烷基，氨基（低级）烷基，保护的氨基（低级）烷基，羧基 烷基，R 5为羧基，保护的羧基，羧基（低级）烷基或保护的羧基（低级）烷基，R6为氢，低级烷基，C6-10ar（低级）烷基氨基（低级）烷基，被保护的氨基 （低级）烷基，受保护的羧基（低级）烷基或杂环（低级）烷基，R7是氢或低级烷基，A是-O - ， - NH-，低级烷基亚氨基或低级亚烷基或其药学上可接受的盐是 披露 该化合物可用于治疗和预防内皮素介导的疾病如高血压。 还公开了这种肽的制备。

    Peptide compound and its preparation
    7.
    发明授权
    Peptide compound and its preparation 失效
    肽化合物及其制备

    公开(公告)号：US5430022A

    公开(公告)日：1995-07-04

    申请号：US86094

    申请日：1993-07-06

    申请人： Keiji Hemmi ,  Masahiro Neya ,  Naoki Fukami ,  Masashi Hashimoto ,  Hirokazu Tanaka ,  Natsuko Kayakiri

    发明人： Keiji Hemmi ,  Masahiro Neya ,  Naoki Fukami ,  Masashi Hashimoto ,  Hirokazu Tanaka ,  Natsuko Kayakiri

    IPC分类号： A61K38/00 ,  C07K5/02 ,  C07K5/078 ,  C07K5/083 ,  C07K5/103 ,  A61K38/06 ,  C07K1/02 ,  C07K1/06 ,  C07K5/08

    CPC分类号： C07K5/06156 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/0207 ,  C07K5/021 ,  C07K5/0217 ,  C07K5/0808 ,  C07K5/101 ,  A61K38/00

    摘要： Peptide compounds of the formula (I') ##STR1## in which R.sup.1 is acyl,R.sup.2 is lower alkyl, cyclo(lower)alkyl(lower)alkyl or optionally substituted heterocyclic(lower)alkyl,R.sup.3 is optionally substituted heterocyclic(lower)alkyl or optionally substituted ar(lower)alkyl,R.sup.4 is lower alkyl, amino(lower)alkyl, protected amino(lower)alkyl, carboxy(lower)alkyl, protected carboxy(lower)alkyl or optionally substituted heterocyclic(lower)alkyl,R.sup.5 is carboxy, protected carboxy, carboxy(lower)alkyl or protected carboxy(lower)alkyl,R.sup.6 is hydrogen, lower alkyl, C.sub.6-10 ar(lower)alkyl amino(lower)alkyl, protected amino(lower)alkyl, carboxy(lower)alkyl, protected carboxy(lower)alkyl, or heterocyclic(lower)alkyl,R.sup.7 is hydrogen or lower alkyl, andA is --O--, --NH--, lower alkylimino or lower alkylene, or a pharmaceutically acceptable salt thereof are disclosed. The compounds can be used to treat and prevent endothelin mediated diseases such as hypertension. The preparation of such peptides is also disclosed.

    摘要翻译： 式（I'）的肽化合物其中R 1是酰基，R 2是低级烷基，环（低级）烷基（低级）烷基或任选取代的杂环（低级）烷基），其中R 1是任选取代的杂环 （低级）烷基或任选取代的芳（低级）烷基，R 4是低级烷基，氨基（低级）烷基，保护的氨基（低级）烷基，羧基 烷基，R 5为羧基，保护的羧基，羧基（低级）烷基或保护的羧基（低级）烷基，R6为氢，低级烷基，C6-10ar（低级）烷基氨基（低级）烷基，被保护的氨基 （低级）烷基，受保护的羧基（低级）烷基或杂环（低级）烷基，R7是氢或低级烷基，A是-O - ， - NH-，低级烷基亚氨基或低级亚烷基或其药学上可接受的盐是 披露 该化合物可用于治疗和预防内皮素介导的疾病如高血压。 还公开了这种肽的制备。

    Endothelin antagonists
    10.
    发明授权
    Endothelin antagonists 失效
    内皮素拮抗剂

    公开(公告)号：US06207686B1

    公开(公告)日：2001-03-27

    申请号：US08836198

    申请日：1997-06-20

    申请人： Masahiro Neya ,  Tatsuya Zenkoh ,  Hitoshi Sawada ,  Chiyoshi Kasahara ,  Masayoshi Murata ,  Keiji Hemmi

    发明人： Masahiro Neya ,  Tatsuya Zenkoh ,  Hitoshi Sawada ,  Chiyoshi Kasahara ,  Masayoshi Murata ,  Keiji Hemmi

    IPC分类号： A61K3138

    CPC分类号： C07D405/12 ,  C07D209/20 ,  C07D317/60 ,  C07D409/12

    摘要： A compound of formula (I), in which: R1 is lower alkyl, cyclo(lower)alkyl, optionally substituted aryl, optionally substituted heterocyclic group, cyclo(lower)alkyl(lower)alkyl, or ar(lower)alkyl; R2 is hydrogen, hydroxy or protected hydroxy; R3 is lower alkyl, aryl, ar(lower)alkyl or optionally substituted heterocyclic(lower)alkyl; R4 is carboxy, protected carboxy or lower alkylsufonylcarbamoyl; R5 is hydrogen or lower alkyl; R6 is hydrogen or heterocyclic group; A is a single bond or lower alkylene, and Ar is optionally substituted aryl, or pharmaceutically acceptable salts thereof, having endothelin antagonistic activity.

    摘要翻译： 式（I）化合物，其中：R 1为低级烷基，环（低级）烷基，任选取代的芳基，任选取代的杂环基，环（低级）烷基（低级）烷基或芳（低级）烷基; R2是氢，羟基或被保护的羟基; R3是低级烷基，芳基，芳（低级）烷基或任选取代的杂环（低级）烷基; R4是羧基，被保护的羧基或低级烷基磺酰基氨基甲酰基; R5是氢或低级烷基; R6是氢或杂环基; A是单键或低级亚烷基，Ar是具有内皮素拮抗活性的任选取代的芳基或其药学上可接受的盐。