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304 条记录 (耗时 0.041 秒)

    Peptides, process for preparation thereof and use thereof
    24.
    发明授权
    Peptides, process for preparation thereof and use thereof 失效
    肽，其制备方法和用途

    公开(公告)号：US4354966A

    公开(公告)日：1982-10-19

    申请号：US193453

    申请日：1980-10-03

    申请人： Yoshihiko Kitaura ,  Osamu Nakaguchi ,  Keiji Hemmi ,  Matsuhiko Aratani ,  Hidekazu Takeno ,  Satoshi Okada ,  Hirokazu Tanaka ,  Masashi Hashimoto

    发明人： Yoshihiko Kitaura ,  Osamu Nakaguchi ,  Keiji Hemmi ,  Matsuhiko Aratani ,  Hidekazu Takeno ,  Satoshi Okada ,  Hirokazu Tanaka ,  Masashi Hashimoto

    IPC分类号： A61K38/00 ,  C07K5/02 ,  C07K9/00 ,  C07C103/52

    CPC分类号： C07C243/00 ,  C07K5/0215 ,  C07K9/005 ,  C12R1/465 ,  A61K38/00

    摘要： The invention relates to novel peptides and their pharmaceutically acceptable salts, particularly useful for pharmaceutical purposes such as in the therapeutic treatment of infectious diseases caused by pathogenic microorganisms. The compounds have the structure ##STR1## wherein R.sup.1 is hydrogen or acyl;R.sup.2 is carboxy or protected carboxy or a group of the formula: --COHN--R.sub.a.sup.2 wherein R.sub.a.sup.2 is carboxy (lower) alkyl or protected carboxy (lower) alkyl;R.sup.3 is carboxy, protected carboxy, lower alkyl, hydroxyphenyl, carbamoyl or a group of the formula: ##STR2## wherein R.sub.a.sup.3 is hydrogen, amino, protected amino or acylamino, R.sub.b.sup.3 is carboxy or protected carboxy;R.sup.p is carboxy, protected carboxy, carbamoyl, carboxy (lower) alkyl or protected carboxy (lower) alkyl;l is an integer 2,m is an integer 0 to 2 andn is an integer 1,provided that,whenR.sup.1 is hydrogen or acyl,R.sup.2 is carboxy, protected carboxy or a group of the formula: --CONHR.sub.a.sup.2 wherein R.sub.a.sup.2 is carboxy (lower) alkyl or protected carboxy (lower) alkyl,R.sup.p is carboxy, or protected carboxy, m is an integer 2, thenR.sup.3 is carbamoyl, lower alkyl or hydroxyphenyl or a group of the formula: ##STR3## wherein R.sub.a.sup.3 is hydrogen or acylamino and R.sub.b.sup.3 is carboxy or protected caboxy, andwhenR.sup.p is carbamoyl, thenR.sup.1 is acyl.

    摘要翻译： 本发明涉及新型肽及其药学上可接受的盐，特别可用于药物目的，例如由病原微生物引起的感染性疾病的治疗性治疗。 这些化合物具有结构，其中R 1是氢或酰基; R2是羧基或保护的羧基或下式基团-COHN-Ra2，其中Ra2是羧基（低级）烷基或被保护的羧基（低级）烷基; R 3是羧基，保护的羧基，低级烷基，羟基苯基，氨基甲酰基或下式的基团：其中R 3a是氢，氨基，被保护的氨基或酰氨基，R 3b是羧基或被保护的羧基; Rp是羧基，保护的羧基，氨基甲酰基，羧基（低级）烷基或被保护的羧基（低级）烷基; l为整数2，m为整数0〜2，n为整数1，条件是当R 1为氢或酰基时，R 2为羧基，被保护的羧基或式-CONHRa 2基团，其中Ra 2为羧基（ 低级）烷基或受保护的羧基（低级）烷基，Rp是羧基或受保护的羧基，m是整数2，则R3是氨基甲酰基，低级烷基或羟基苯基或下式的基团：其中R 3a是氢或酰基氨基 并且R 3b是羧基或被保护的环氧基，当Rp是氨基甲酰基时，则R1是酰基。

    Peptide compound and its preparation
    26.
    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。

    Trifluoromethylketone derivatives, processes for preparation thereof and use thereof
    27.
    发明授权
    Trifluoromethylketone derivatives, processes for preparation thereof and use thereof 失效
    三氟甲基酮衍生物，其制备方法及其用途

    公开(公告)号：US5296591A

    公开(公告)日：1994-03-22

    申请号：US805610

    申请日：1991-12-12

    申请人： Keiji Hemmi ,  Ichiro Shima ,  Keisuke Imai ,  Hirokazu Tanaka

    发明人： Keiji Hemmi ,  Ichiro Shima ,  Keisuke Imai ,  Hirokazu Tanaka

    IPC分类号： A61K31/16 ,  A61K31/24 ,  A61K31/40 ,  A61K31/535 ,  A61K31/5375 ,  A61K38/00 ,  A61K38/05 ,  A61P11/00 ,  A61P43/00 ,  C07C231/02 ,  C07C233/68 ,  C07C237/22 ,  C07C275/42 ,  C07D295/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/00

    CPC分类号： C07K5/06191 ,  A61K38/00

    摘要： The trifluoromethylketone derivatives (I) and pharmaceutically acceptable salts thereof have a human leukocyte elastase inhibiting activity and are useful as human leukocyte elastase inhibitors for treating or preventing degenerative diseases. The trifluoromethylketone derivatives (I) have the following formula: ##STR1## wherein R.sup.1 is C.sub.1-6 alkyl which has one or two substituents selected from carboxy, esterified carboxy and di-C.sub.1-6 alkylcarbamoyl; phenyl(C.sub.1-6) alkyl, the phenyl moiety of which may have halogen or nitro or amino substituents and the alkyl moiety of which may have carboxy or esterified carboxy substituents; halo-phenyl; morpholino; or morpholino(C.sub.1-6) alkyl,R.sup.2 and R.sup.3 are each C.sub.1-6 alkyl,X is -- or --NH--, andY is ##STR2## and pharmaceutically acceptable salts thereof.

    摘要翻译： 三氟甲基酮衍生物（I）及其药学上可接受的盐具有人白细胞弹性蛋白酶抑制活性，可用作治疗或预防退行性疾病的人白细胞弹性蛋白酶抑制剂。 三氟甲基酮衍生物（I）具有下式：（*化学结构*）（I）其中R1是具有一个或两个选自羧基，酯化羧基和二-C 1-6烷基氨基甲酰基的取代基的C 1-6烷基; 苯基（C 1-6）烷基，其苯基部分可以具有卤素或硝基或氨基取代基，其烷基部分可以具有羧基或酯化的羧基取代基; 卤代苯基; 吗啉代 或吗啉代（C 1-6）烷基，R 2和R 3各自为C 1-6烷基，X为 - 或-NH-，Y为（*化学结构*）及其药学上可接受的盐。