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    Cyclic hexapeptides, their production and use
    2.
    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。

    Cyclic peptides and use thereof
    3.
    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。

    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。

    Phosphonic acid derivatives and use thereof
    5.
    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。

    1, 3-benzothiazinone derivatives and use thereof
    6.
    发明申请
    1, 3-benzothiazinone derivatives and use thereof 有权
    1,3-苯并噻嗪酮衍生物及其用途

    公开(公告)号：US20050032786A1

    公开(公告)日：2005-02-10

    申请号：US10488384

    申请日：2002-09-02

    申请人： Masahiro Kajino ,  Akira Kawada ,  Yutaka Nakayama ,  Haruhide Kimura

    发明人： Masahiro Kajino ,  Akira Kawada ,  Yutaka Nakayama ,  Haruhide Kimura

    IPC分类号： A61K31/5415 ,  A61P1/00 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P13/12 ,  A61P17/00 ,  A61P19/00 ,  A61P19/02 ,  A61P25/00 ,  A61P31/00 ,  A61P43/00 ,  C07D417/04 ,  C07D417/14 ,  C07D279/16

    CPC分类号： C07D417/04 ,  A61K31/5415 ,  C07D417/14

    摘要： This invention provides a compound represented by the formula (I): wherein R1 is a hydrogen atom, a halogen atom, hydroxy, nitro, optionally halogenated alkyl, alkoxy optionally having substituents, acyl or amino optionally having substituents; R2 is pyridyl, furyl, thienyl, pyrrolyl, quinolyl, pyrazinyl, pyrimidinyl, pyridazinyl, indolyl, tetrahydroquinolyl or thiazolyl, each of which may have substituents; n is 1 or 2; or a salt. And this invention provides a safe pharmaceutical comprising the compound of the formula (I), which has an excellent apoptosis inhibitory effect and MIF binding effect, for preventing and/or treating heart disease, nervous degenerative disease, cerebrovascular disease, central nervous infectious disease, traumatorathy, demyelinating disease, bone and articular disease, kidney disease, liver disease, osteomyelodysplasia, AIDS, cancer, and the like.

    摘要翻译： 本发明提供由式（I）表示的化合物：其中R 1为氢原子，卤素原子，羟基，硝基，任选卤代烷基，任选具有取代基的烷氧基，任选具有取代基的酰基或氨基; R 2是吡啶基，呋喃基，噻吩基，吡咯基，喹啉基，吡嗪基，嘧啶基，哒嗪基，吲哚基，四氢喹啉基或噻唑基，其各自可以具有取代基; n为1或2; 或盐。 本发明提供一种安全药物，其包含具有优异的细胞凋亡抑制作用和MIF结合作用的式（I）化合物，用于预防和/或治疗心脏病，神经退行性疾病，脑血管病，中枢神经感染性疾病， 外伤，脱髓鞘疾病，骨和关节疾病，肾脏疾病，肝病，骨发育不良，艾滋病，癌症等。

    1,3-BENZOTHIAZINONE DERIVATIVES AND USE THEREOF
    9.
    发明申请
    1,3-BENZOTHIAZINONE DERIVATIVES AND USE THEREOF 有权
    1,3-苯并噻嗪酮衍生物及其用途

    公开(公告)号：US20090082343A1

    公开(公告)日：2009-03-26

    申请号：US12099779

    申请日：2008-04-08

    申请人： Masahiro Kajino ,  Yutaka Nakayama ,  Akira Kawada ,  Haruhide Kimura ,  Taisuke Tawaraishi

    发明人： Masahiro Kajino ,  Yutaka Nakayama ,  Akira Kawada ,  Haruhide Kimura ,  Taisuke Tawaraishi

    IPC分类号： A61K31/5415 ,  C07D401/04 ,  A61P9/00 ,  A61P1/00

    CPC分类号： C07D417/04 ,  A61K31/5415 ,  C07D417/14

    摘要： This invention provides a compound represented by the formula (I): wherein R1 is a hydrogen atom, a halogen atom, hydroxy, nitro, optionally halogenated alkyl, alkoxy optionally having substituents, acyl or amino optionally having substituents; R2 is pyridyl, furyl, thienyl, pyrrolyl, quinolyl, pyrazinyl, pyrimidinyl, pyridazinyl, indolyl, tetrahydroquinolyl or thiazolyl, each of which may have substituents; n is 1 or 2; or a salt. And this invention provides a safe pharmaceutical comprising the compound of the formula (I), which has an excellent apoptosis inhibitory effect and MIF binding effect, for preventing and/or treating heart disease, nervous degenerative disease, cerebrovascular disease, central nervous infectious disease, traumatorathy, demyelinating disease, bone and articular disease, kidney disease, liver disease, osteomyelodysplasia, AIDS, cancer, and the like.

    摘要翻译： 本发明提供由式（I）表示的化合物：其中R1是氢原子，卤素原子，羟基，硝基，任选卤代烷基，任选具有取代基的烷氧基，任选具有取代基的酰基或氨基; R 2是可以具有取代基的吡啶基，呋喃基，噻吩基，吡咯基，喹啉基，吡嗪基，嘧啶基，哒嗪基，吲哚基，四氢喹啉基或噻唑基。 n为1或2; 或盐。 本发明提供了一种安全药物，其包含具有优异的细胞凋亡抑制作用和MIF结合作用的式（I）化合物，用于预防和/或治疗心脏病，神经退行性疾病，脑血管病，中枢神经感染性疾病， 外伤，脱髓鞘疾病，骨和关节疾病，肾脏疾病，肝病，骨发育不良，艾滋病，癌症等。