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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。

    Indole derivatives
    10.
    发明授权
    Indole derivatives 失效
    吲哚衍生物

    公开(公告)号：US5312829A

    公开(公告)日：1994-05-17

    申请号：US956579

    申请日：1992-10-06

    申请人： Satoshi Okada ,  Kozo Sawada ,  Natsuko Kayakiri ,  Yuki Saitoh ,  Hirokazu Tanaka ,  Masashi Hashimoto

    发明人： Satoshi Okada ,  Kozo Sawada ,  Natsuko Kayakiri ,  Yuki Saitoh ,  Hirokazu Tanaka ,  Masashi Hashimoto

    IPC分类号： C07D209/12 ,  C07D209/14 ,  C07D209/18 ,  C07D403/10 ,  C07D413/10 ,  C07D417/10 ,  C07D209/10 ,  A61K31/405 ,  C07D405/04

    CPC分类号： C07D403/10 ,  C07D209/12 ,  C07D209/14 ,  C07D209/18 ,  C07D413/10 ,  C07D417/10

    摘要： A compound of the formula: ##STR1## wherein R.sup.1 is carboxy or pharmaceutically acceptable salts and esters thereof;R.sup.2 is hydrogen, lower alkyl or halogen;R.sup.3 is phenyl, naphthyl, phenyl or naphthyl each substituted by from one to three C.sub.1-6 alkyl groups, mono-, di- or triphenyl (C.sub.1-6)alkyl; or substituted mono-, di- or triphenyl (C.sub.1-6) alkyl;A is lower alkylene which may be substituted by oxo or lower alkenylene,Q is carbonyl or lower alkylene,X is ##STR2## in which R.sup.4 is hydrogen or C.sub.1-6 alkyl, andR.sup.5 is hydrogen, C.sub.1-6 alkyl or Y--Z--R.sup.3,Y is a bond or lower alkylene,Z is lower alkylene ##STR3## in which R.sup.6 is hydrogen, (C.sub.1 -C.sub.6) alkyl, mono-, di- or triphenyl(C.sub.1-10) alkyl, C.sub.1-6 alkyl or lower alkoxycarbonyl substituted mono-, di- or triphenyl(C.sub.1-6)alkyl or pharmaceutically acceptable carboxylic acid acyl, and pharmaceutically acceptable salts thereof. The compound is useful as a testosterone 5.alpha.-reductase inhibitor.

    摘要翻译： 下式的化合物：其中R 1是羧基或其药学上可接受的盐和酯; R2是氢，低级烷基或卤素; R 3为苯基，萘基，苯基或萘基，各自被一至三个C 1-6烷基，单 - ，二 - 或三苯基（C 1-6）烷基取代; 或取代的单 - ，二 - 或三苯基（C 1-6）烷基; A是可被氧代或低级亚烯基取代的低级亚烷基，Q是羰基或低级亚烷基，X是其中R 4是氢或C 1-6烷基，R 5是氢，C 1-6烷基或YZ-R 3 ，Y为键或低级亚烷基，Z为低级亚烷基，其中R6为氢，（C1-C6）烷基，单 - ，二 - 或三苯基（C1-10）烷基，C1-6烷基或低级烷氧基羰基 取代的单 - ，二 - 或三苯基（C 1-6）烷基或药学上可接受的羧酸酰基及其药学上可接受的盐。 该化合物可用作睾酮5α-还原酶抑制剂。