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    Composition for prophylaxis or treatment of pulmonary circulatory diseases
    1.
    发明授权
    Composition for prophylaxis or treatment of pulmonary circulatory diseases 失效
    用于预防或治疗肺循环系统疾病的组合物

    公开(公告)号：US5753619A

    公开(公告)日：1998-05-19

    申请号：US564442

    申请日：1995-11-29

    申请人： Toshifumi Watanabe ,  Keiji Kusumoto ,  Mitsuhiro Wakimasu

    发明人： Toshifumi Watanabe ,  Keiji Kusumoto ,  Mitsuhiro Wakimasu

    IPC分类号： A61K38/00 ,  C07K7/64 ,  C07K14/575

    CPC分类号： C07K14/57536 ,  C07K7/64 ,  A61K38/00

    摘要： Cyclic hexapeptides having antagonistic activity on endothelin receptors of the formula �I!: ##STR1## wherein X and Y each is an .alpha.-amino acid residue having D-, L-form or DL-form, A is a D-acidic-.alpha.-amino acid residue, B is a neutral-.alpha.-amino acid residue having D- or L-form, C is an L-.alpha.-amino acid residue and E is a D-.alpha.-amino acid residue having an aromatic ring group can be effectively used for prophylaxis and/or treatment of pulmonary circulatory diseases.

    摘要翻译： 对式[I]的内皮素受体具有拮抗作用的环状六肽：其中X和Y各自为具有D-，L-型或DL-型的α-氨基酸残基，A为D- 酸性-α-氨基酸残基，B是具有D-或L-形式的中性-α-氨基酸残基，C是L-氨基酸残基，E是具有芳香族的D-氨基酸残基 环组可有效用于预防和/或治疗肺循环系统疾病。

    Cyclic hexapeptides, their production and use
    3.
    发明授权
    Cyclic hexapeptides, their production and use 失效
    循环六肽，其生产和使用

    公开(公告)号：US5948754A

    公开(公告)日：1999-09-07

    申请号：US739810

    申请日：1996-10-30

    申请人： Mitsuhiro Wakimasu ,  Takashi Kikuchi ,  Akira Kawada

    发明人： Mitsuhiro Wakimasu ,  Takashi Kikuchi ,  Akira Kawada

    IPC分类号： A61K38/00 ,  C07K14/575 ,  A61K38/12 ,  C07K7/64

    CPC分类号： C07K14/57536 ,  A61K38/00

    摘要： A cyclic hexapeptide represented by the formula:cyclo�A--Asp(R.sup.1)--Y--NH--CHR.sup.2 --CO--C--D--Trp(N.sup.in --R.sup.3)--! (I)wherein A is a D-acidic-.alpha.-amino acid residue; Y is an acidic-.alpha.-amino acid residue; C is an L-.alpha.-amino acid residue; R.sup.1 is a group represented by the formula: ##STR1## wherein X.sup.1 and X.sup.2 are independently H, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or nitro, and may bind together to form a ring in cooperation with the adjacent carbon atom; R.sup.2 is C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-C.sub.1-3 alkyl, C.sub.1-6 alkylthio-C.sub.1-3 alkyl, C.sub.3-7 cycloalkylthio-C.sub.1-3 alkyl, C.sub.1-5 alkoxy-C.sub.1-3 alkyl, C.sub.3-7 cycloalkoxy-C.sub.1-3 alkyl, C.sub.1-6 alkylthio, C.sub.3-7 cycloalkylthio, C.sub.1-5 alkoxy or C.sub.3-7 cycloalkoxy; R.sup.3 is H, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, --COR.sup.4, --COOR.sup.5 or --CONHR.sup.6 ; when X.sup.1, X.sup.2 and R.sup.3 are all hydrogen atoms, R.sup.2 is not an isobutyl group, or a salt thereof, which exhibits excellent antagonistic action against endothelin receptors, particularly endothelin B receptors.

    摘要翻译： 由式：环[A-Asp（R1）-Y-NH-CHR2-CO-CD-Trp（Nin-R3） - ]（I）表示的环状六肽其中A是D-酸性α-氨基酸 残留物 Y是酸性α-氨基酸残基; C是L-α-氨基酸残基; R1是由下式表示的基团：其中X1和X2独立地是H，C1-6烷基，C1-6烷氧基，卤素或硝基，并且可以与相邻的碳原子一起结合形成环; R 2是C 1-6烷基，C 3-7环烷基，C 3-7环烷基-C 1-3烷基，C 1-6烷硫基-C 1-3烷基，C 3-7环烷硫基-C 1-3烷基，C 1-5烷氧基-C 1-3 烷基，C 3-7环烷氧基-C 1-3烷基，C 1-6烷硫基，C 3-7环烷硫基，C 1-5烷氧基或C 3-7环烷氧基; R3是H，C1-6烷基，C3-7环烷基，-COR4，-COOR5或-CONHR6; 当X1，X2和R3都是氢原子时，R2不是对内皮素受体，特别是内皮素B受体具有优异拮抗作用的异丁基或其盐。

    Phosphonic acid derivatives and use thereof
    4.
    再颁专利
    Phosphonic acid derivatives and use thereof 失效
    膦酸衍生物及其用途

    公开(公告)号：USRE35886E

    公开(公告)日：1998-09-01

    申请号：US680295

    申请日：1996-07-12

    申请人： Mitsuhiro Wakimasu ,  Masaaki Mori ,  Akira Kawada

    发明人： Mitsuhiro Wakimasu ,  Masaaki Mori ,  Akira Kawada

    IPC分类号： A61K38/00 ,  A61K38/55 ,  A61P9/00 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  C07K1/06 ,  C07K1/113 ,  C07K5/06 ,  C07F9/22 ,  A61K33/42

    CPC分类号： C07K5/06191 ,  A61K38/00 ,  Y02P20/55

    摘要： A phosphonic acid derivative compound represented by formula �I ! or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 each represent hydrocarbon groups which may be substituted, except cases in which (1) R.sub.2 is unsubstituted methyl, ( 2 ) R.sub.3 is an unsubstituted hydrocarbon group having 1 to 3 carbon atoms, and (3) R.sub.1 is benzyloxycarbonylaminomethyl, R.sub.2 is isobutyl and R.sub.3 is isobutyl or phenylmethyl, which has endothelin-converting enzyme inhibiting activity and is useful as pharmaceutical drugs such as therapeutic agents for hypertension, cardiac or cerebral circulatory diseases and renal diseases. This is a Reissue of a Patent which was the subject of a Reexamination Certificate No. B1 5,330,978, dated Jun. 18, 1996, Request No. 90/00400, Oct. 18, 1995.

    摘要翻译： 由式[I]表示的膦酸衍生物或其药学上可接受的盐：其中R 1，R 2和R 3各自表示可以被取代的烃基，除了（1）R 2是未取代的甲基 ，（2）R3为未取代的碳原子数1〜3的烷基，（3）R1为苄氧羰基氨基甲基，R2为异丁基，R3为异丁基或苯甲基，具有内皮素转化酶抑制活性，可用作药物 作为高血压，心脏或脑循环系统疾病和肾脏疾病的治疗剂。 + PR这是1996年10月18日，1996年10月18日申请号90/00400的1996年6月18日的复审证书B1 5,330,978的主题的重新发行。

    Cyclic peptides and use thereof
    5.
    发明授权
    Cyclic peptides and use thereof 失效
    循环肽及其用途

    公开(公告)号：US5616684A

    公开(公告)日：1997-04-01

    申请号：US231449

    申请日：1994-04-20

    申请人： Mitsuhiro Wakimasu ,  Takashi Kikuchi ,  Akira Kawada ,  Hideo Shirafuji

    发明人： Mitsuhiro Wakimasu ,  Takashi Kikuchi ,  Akira Kawada ,  Hideo Shirafuji

    IPC分类号： A61K38/00 ,  A61P3/06 ,  A61P9/00 ,  A61P9/12 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P29/00 ,  A61P35/00 ,  C07K7/64 ,  C07K14/575

    CPC分类号： C07K14/57536 ,  C07K7/64 ,  A61K38/00 ,  Y02P20/55

    摘要： Cyclic peptides and their salts have antagonistic activity on endothelin receptors and antagonistic activity on NK2 receptors. The peptides have the formula ##STR1## wherein X and Y each represent .alpha.-amino acid residues, A represents a D-acidic-.alpha.-amino acid residue, B represents a neutral .alpha.-amino acid residue, C represents an L-.alpha.-amino acid residue and D represents a D-.alpha.-amino acid residue having an aromatic ring group; wherein hydroxy, thiol, amino, imino and carboxyl groups can be substituted or unsubstituted. Pharmaceutical compositions containing such peptides are also described.

    摘要翻译： 环肽及其盐对内皮素受体具有拮抗作用，对NK2受体具有拮抗作用。 肽具有下式：其中X和Y各自表示α-氨基酸残基，A表示D-酸性-α-氨基酸残基，B表示中性α-氨基酸残基，C表示L - α-氨基酸残基，D表示具有芳环基团的D-α-氨基酸残基; 其中羟基，硫醇，氨基，亚氨基和羧基可以是取代或未取代的。 还描述了含有这些肽的药物组合物。

    Method for controlling conformation of cyclopentapeptide
    6.
    发明授权
    Method for controlling conformation of cyclopentapeptide 失效
    控制环戊肽构象的方法

    公开(公告)号：US06346604B1

    公开(公告)日：2002-02-12

    申请号：US08969007

    申请日：1997-11-12

    申请人： Mitsuhiro Wakimasu ,  Hiroshi Inooka ,  Satoshi Endo ,  Takashi Kikuchi

    发明人： Mitsuhiro Wakimasu ,  Hiroshi Inooka ,  Satoshi Endo ,  Takashi Kikuchi

    IPC分类号： C07K102

    CPC分类号： C07K7/64 ,  A61K38/00

    摘要： Cyclic pentapeptides having a &ggr;-turn and a &bgr;-turn wherein the cyclic pentapeptide has the following formula (I): Cyclo(—A1—A2—A3—A4—A5—)  (I) wherein A1, A2, A3, A4 and A5 are amino acid residues; said pentapeptide having amino acid residues in positions 1-2-3 to form a &ggr;-turn, and amino acid residues in positions 3-4-5-1 to form a &bgr;-turn in combination with the &ggr;-turn; in which D-&agr;-amino acid residues are selected for A1, A3 and A5 and L-&agr;-amino acid residues are selected for A2 and A4 or wherein L-&agr;-amino acid residues are selected for A1, A3 and A5 and D-&agr;-amino acid residues are selected for A2 and A4; are provided. Compounds having &ggr;-turns and &bgr;-turns can be systhesized, regardless of the kinds of amino acid residues, and it is possible to synthesize compounds in which desired amino acid residues are introduced into sites of &bgr;-turn and &ggr;-turn based on their importance from the viewpoint of biological activity. The present invention is therefore available for design of compounds having biological activity.

    摘要翻译： 具有γ-匝和β-匝的环状五肽，其中环状五肽具有下式（I）：其中A1，A2，A3，A4和A5是氨基酸残基;所述五肽在1-2位具有氨基酸残基 -3以形成γ-匝数，以及位置3-4-5-1处的氨基酸残基与γ匝组合形成β-匝数;其中选择D-α-氨基酸残基用于A1， A2和A4选择A3和A5和L-α-氨基酸残基，或选择A1，A3和A5的L-α-氨基酸残基，A2和A4选择D-α-氨基酸残基; 具有γ-匝数和β-匝数的化合物可以被控制，而不管氨基酸残基的种类如何，并且可以合成将期望的氨基酸残基引入β-匝和γ-匝的位点的化合物 基于它们从生物活性的角度的重要性。 因此，本发明可用于设计具有生物活性的化合物。

    Phosphonic acid derivatives and use thereof
    7.
    发明授权
    Phosphonic acid derivatives and use thereof 失效
    膦酸衍生物及其用途

    公开(公告)号：US5330978A

    公开(公告)日：1994-07-19

    申请号：US892768

    申请日：1992-06-03

    申请人： Mitsuhiro Wakimasu ,  Masaaki Mori ,  Akira Kawada

    发明人： Mitsuhiro Wakimasu ,  Masaaki Mori ,  Akira Kawada

    IPC分类号： A61K38/00 ,  A61K38/55 ,  A61P9/00 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  C07K1/06 ,  C07K1/113 ,  C07K5/06 ,  C07F9/22 ,  A61K33/42

    CPC分类号： C07K5/06191 ,  A61K38/00 ,  Y02P20/55

    摘要： A phosphonic acid derivative compound represented by formula [I ] or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 each represent hydrocarbon groups which may be substituted, except cases in which (1) R.sub.2 is unsubstituted methyl, ( 2 ) R.sub.3 is an unsubstituted hydrocarbon group having 1 to 3 carbon atoms, and (3) R.sub.1 is benzyloxycarbonylaminomethyl, R.sub.2 is isobutyl and R.sub.3 is isobutyl or phenylmethyl, which has endothelin-converting enzyme inhibiting activity and is useful as pharmaceutical drugs such as therapeutic agents for hypertension, cardiac or cerebral circulatory diseases and renal diseases.

    摘要翻译： 由式[I]表示的膦酸衍生物或其药学上可接受的盐：其中R 1，R 2和R 3各自表示可以被取代的烃基，除了（1）R 2是未取代的甲基 ，（2）R3为未取代的碳原子数1〜3的烷基，（3）R1为苄氧羰基氨基甲基，R2为异丁基，R3为异丁基或苯甲基，具有内皮素转化酶抑制活性，可用作药物 作为高血压，心脏或脑循环系统疾病和肾脏疾病的治疗剂。

    TAN-1511, its derivatives, production and use thereof
    10.
    发明授权
    TAN-1511, its derivatives, production and use thereof 失效
    TAN-1511，其衍生物，生产和使用

    公开(公告)号：US5478809A

    公开(公告)日：1995-12-26

    申请号：US174365

    申请日：1993-12-28

    申请人： Seiichi Tanida ,  Tsuneaki Hida ,  Mitsuhiro Wakimasu

    发明人： Seiichi Tanida ,  Tsuneaki Hida ,  Mitsuhiro Wakimasu

    IPC分类号： A61K38/00 ,  C07K5/06 ,  C07K5/083 ,  C07K5/103 ,  C07K7/06 ,  C07K5/00 ,  C07K7/00 ,  C07K17/00

    CPC分类号： C07K7/06 ,  C07K5/0606 ,  C07K5/081 ,  C07K5/1013 ,  A61K38/00

    摘要： A compound of the formula: ##STR1## wherein each R.sup.1, R.sup.2 and R.sup.3 is an aliphatic acyl group, X is an amino acid sequence consisting of 1 to 5 amino acid residues which contain at least one acidic amino acid residue, n is an integer of 0 to 4, provided that when n is 0, X has glutamyl-glycyl at its N-terminal and when n is 1 or 2, the acidic amino acid residue is an acidic amino acid residue other than D-glutamyl, or a salt thereof has an activity of remarkably improving anhematopoiesis and is useful as an immuno-stimulating agent having a leukocyte-increasing activity.

    摘要翻译： 下式的化合物：其中每个R 1，R 2和R 3是脂族酰基，X是由1至5个氨基酸残基组成的氨基酸序列，其含有至少一个酸性氨基酸残基，n是整数 为0〜4，条件是当n为0时，X在其N-末端具有谷氨酰 - 甘氨酰，当n为1或2时，酸性氨基酸残基为除D-谷氨酰以外的酸性氨基酸残基或盐 其具有显着改善造血作用的活性，并且可用作具有白细胞增加活性的免疫刺激剂。