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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。

    Peptide compounds, their preparation and uses
    8.
    发明授权
    Peptide compounds, their preparation and uses 失效
    肽化合物，其制备和用途

    公开(公告)号：US5888972A

    公开(公告)日：1999-03-30

    申请号：US564271

    申请日：1997-06-24

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

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

    IPC分类号： A61K38/00 ,  A61P9/12 ,  C07K5/02 ,  C07K5/03 ,  C07K5/062 ,  C07K5/08 ,  C07K5/083 ,  A61K38/06 ,  A61K38/07

    CPC分类号： C07K5/0808 ,  C07K5/0207 ,  C07K5/0827 ,  A61K38/00 ,  Y02P20/55

    摘要： A compound of the formula: ##STR1## in which R.sup.4 is acyl,R.sup.5 is lower alkyl,R.sup.6 is optionally substituted ar(lower)alkyl or optionally substituted heterocyclic-(lower)alkyl,R.sup.7 is lower alkyl or lower alkylthio(lower)alkyl,R.sup.8 is carboxy or protected carboxy,A is lower alkylene,Z is a group of the formula: ##STR2## wherein R.sup.1 is hydrogen, lower alkyl, common amino-protective group or optionally substituted ar(lower)alkyl,R.sup.2 is hydrogen, lower alkyl, optionally substituted ar(lower)alkyl, optionally substituted heterocyclic-(lower)alkyl, optionally substituted cyclo(lower)alkyl(lower)alkyl, common amino-protective group, amino(or protected amino)(lower)alkyl, optionally substituted heterocyclic-carbonyl or cyclo(lower)alkyl, andR.sup.3 is optionally substituted heterocyclic(lower)alkyl, andm is an integer of 0 to 2,or pharmaceutically acceptable salts thereof, useful as endothelin antagonist.

    摘要翻译： PCT No.PCT / JP94 / 01042 Sec。 371日期1996年6月24日 102（e）1996年6月24日PCT 1994年6月28日PCT公布。 公开号WO95 / 00537 日期1995年1月5日具有下式的化合物：其中R 4为酰基，R 5为低级烷基，R 6为任选取代的芳（低级）烷基或任选取代的杂环 - （低级）烷基，R 7为低级烷基或低级 烷硫基（低级）烷基，R 8为羧基或被保护的羧基，A为低级亚烷基，Z为下式基团：其中R 1为氢，低级烷基，普通氨基保护基或任选取代的芳（低级）烷基 （低级）烷基，任选取代的杂环 - （低级）烷基，任选取代的环（低级）烷基（低级）烷基，常用氨基保护基，氨基（或被保护的氨基）（ 低级烷基，任选取代的杂环羰基或环（低级）烷基，R 3为任选取代的杂环（低级）烷基，m为0-2的整数，或其药学上可接受的盐，可用作内皮素拮抗剂。

    Piperazine compounds as inhibitors of MMP or TNF
    9.
    发明授权
    Piperazine compounds as inhibitors of MMP or TNF 失效
    哌嗪化合物作为MMP或TNF的抑制剂

    公开(公告)号：US06333324B1

    公开(公告)日：2001-12-25

    申请号：US09319928

    申请日：1999-07-26

    申请人： Masahiro Neya ,  Hitoshi Yamazaki ,  Natsuko Kayakiri ,  Kentaro Sato ,  Teruo Oku

    发明人： Masahiro Neya ,  Hitoshi Yamazaki ,  Natsuko Kayakiri ,  Kentaro Sato ,  Teruo Oku

    IPC分类号： C07D24104

    CPC分类号： C07D405/12 ,  C07D241/04 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

    摘要： A compound of formula (I) wherein A is a sulfonyl or a carbonyl; R1 is an optionally substituted aryl, an optionally substituted heterocyclic group, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; R2 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R3 is an optionally substituted lower alkyl, an optionally substituted lower alkoxy, an optionally substituted aryloxy, an optionally substitued lower alkenyl, an optionally substituted aryl, an optionally substituted heterocyclic group or an optionally substitued amino; R4 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R5 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; and R10 is a hydroxy or a protected hydroxy, and a pharmaceutically acceptable salt thereof. The compound of the present invention is useful as a medicament for prophylactic and therapeutic treatment of MMP- or TNF&agr;-mediated diseases.

    摘要翻译： 式（I）的化合物，其中A是磺酰基或羰基; R1是任选取代的芳基，任选取代的杂环基，任选取代的低级烷基或任选取代的低级烯基; R2是氢，任选取代的低级烷基，任选取代的芳基或任选取代的杂环基; R 3是任选取代的低级烷基，任选取代的低级烷氧基，任选取代的芳氧基，任选取代的低级烯基，任选取代的芳基，任选取代的杂环基或任选取代的氨基; R4是氢，任选取代的低级烷基，任选取代的芳基或任选取代的杂环基; R5是氢，任选取代的低级烷基，任选取代的芳基或任选取代的杂环基; R 10为羟基或被保护的羟基及其药学上可接受的盐。 本发明的化合物可用作用于预防和治疗MMP或TNFα介导的疾病的药物。

    Piperazine compounds as inhibitors of MMP or TNF
    10.
    发明授权
    Piperazine compounds as inhibitors of MMP or TNF 失效
    哌嗪化合物作为MMP或TNF的抑制剂

    公开(公告)号：US06489324B2

    公开(公告)日：2002-12-03

    申请号：US09982869

    申请日：2001-10-22

    申请人： Masahiro Neya ,  Hitoshi Yamazaki ,  Natsuko Kayakiri ,  Kentaro Sato ,  Teruo Oku

    发明人： Masahiro Neya ,  Hitoshi Yamazaki ,  Natsuko Kayakiri ,  Kentaro Sato ,  Teruo Oku

    IPC分类号： C07D24104

    CPC分类号： C07D405/12 ,  C07D241/04 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

    摘要： A compound of formula (I) wherein A is a sulfonyl or a carbonyl; R1 is an optionally substituted aryl, an optionally substituted heterocyclic group, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; R2 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R3 is an optionally substituted lower alkyl, an optionally substituted lower alkoxy, an optionally substituted aryloxy, an optionally substituted lower alkenyl, an optionally substituted aryl, an optionally substituted heterocyclic group or an optionally substituted amino; R4 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R5 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; and R10 is a hydroxy or a protected hydroxy, and a pharmaceutically acceptable salt thereof. The compound of the present invention is useful as a medicament for prophylactic and therapeutic treatment of MMP-or TNF&agr;-medicated diseases.

    摘要翻译： 式（I）的化合物，其中A是磺酰基或羰基; R1是任选取代的芳基，任选取代的杂环基，任选取代的低级烷基或任选取代的低级烯基; R2是氢，任选取代的低级烷基，任选取代的芳基或任选取代的杂环基; R3是任选取代的低级烷基，任选取代的低级烷氧基，任选取代的芳氧基，任选取代的低级烯基，任选取代的芳基，任选取代的杂环基或任选取代的氨基; R4是氢，任选取代的低级烷基，任选取代的芳基或任选取代的杂环基; R5是氢，任选取代的低级烷基，任选取代的芳基或任选取代的杂环基; R 10为羟基或被保护的羟基及其药学上可接受的盐。 本发明的化合物可用作用于预防和治疗MMP或TNFα药物疾病的药物。