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    Quinone derivatives, their production and use
    41.
    发明授权
    Quinone derivatives, their production and use 失效
    喹诺酮衍生物，其生产和使用

    公开(公告)号：US5229385A

    公开(公告)日：1993-07-20

    申请号：US818856

    申请日：1992-01-10

    申请人： Shinji Terao ,  Kohei Nishikawa

    发明人： Shinji Terao ,  Kohei Nishikawa

    IPC分类号： C07D213/50 ,  C07D213/55 ,  C07D409/06 ,  C07D521/00

    CPC分类号： C07D231/12 ,  C07D213/50 ,  C07D213/55 ,  C07D233/56 ,  C07D249/08 ,  C07D409/06

    摘要： Quinone derivatives represented by the general formula ##STR1## (wherein, R.sup.1 and R.sup.2, the same or different, refer to hydrogen atom, methyl or methoxymethyl group, or R.sup.1 and R.sup.2 bind together to form --CH.dbd.CH--CH.dbd.CH--; R.sup.3 is hydrogen atom or methyl group; R.sup.4 is nitrogen-containing heterocyclic group which may be substituted; R.sup.5 is hydrogen atom, methyl group, hydroxymethyl group which may be substituted, or carboxyl group which may be esterified or amidated; Z is ##STR2## (wherein, R' is hydrogen atom or methyl group); n is an integer from 0 through 12, m is an integer from 0 through 3, and k is an integer from 0 through 7, providing that, when m is 2 or 3, Z and k are able to vary appropriately in the repeating unit shown in []), and the hydroquinone derivatives thereof, are novel compounds, possess improvement effects of metabolism of poly unsaturated fatty acids, particularly two or more of inhibition of production of fatty acid peroxides, inhibition of production of metabolites in 5-lipoxygenase pathway, inhibition of thromboxane A.sub.2 synthetase, thromboxane A.sub.2 receptor antagonism and scavenging action of active oxygen species, and of use as drugs, such as antithrombotics, anti-vascular constriction agents, anti-asthma agent, antiallergic agents, therpeutics for psoriasis, agents for improvement in heart, brain and cardiovascular systems, therapeutics for nephritis, active oxygen-eliminating agents, anticancer agents, agents for improvement of control of arachidonate cascade products, etc.

    摘要翻译： 由通式（I）表示的醌酮衍生物（其中，R1和R2相同或不同，指氢原子，甲基或甲氧基甲基，或R1和R2结合在一起形成-CH = CH-CH = CH-; R3是氢原子或甲基; R4是可以被取代的含氮杂环基; R5是氢原子，甲基，可被取代的羟甲基，或可被酯化或酰胺化的羧基; Z是 （其中，R'为氢原子或甲基）; n为0〜12的整数，m为0〜3的整数，k为0〜7的整数， 当m为2或3时，Z和k能够在[]）所示的重复单元中适当变化，并且其氢醌衍生物是新型化合物，具有改善多不饱和脂肪酸代谢的效果，特别是两种或更多种 抑制脂肪酸过氧化物的产生，抑制代谢物的产生 在5-脂氧合酶途径中，血栓烷A2合成酶的抑制，血栓素A2受体拮抗作用和活性氧的清除作用，以及用作药物，如抗血栓形成剂，抗血管收缩剂，抗哮喘药，抗过敏剂，治疗剂 牛皮癣，改善心脏，脑和心血管系统的药剂，肾炎治疗剂，活性氧消除剂，抗癌剂，改善花生四烯酸级联产物的控制剂等。

    Piperidine derivatives
    43.
    发明授权
    Piperidine derivatives 失效
    哌啶衍生物

    公开(公告)号：US4871842A

    公开(公告)日：1989-10-03

    申请号：US218951

    申请日：1988-07-14

    申请人： Hirosada Sugihara ,  Kohei Nishikawa ,  Katsumi Ito

    发明人： Hirosada Sugihara ,  Kohei Nishikawa ,  Katsumi Ito

    IPC分类号： A61K38/00 ,  C07K5/02

    CPC分类号： C07K5/0222 ,  A61K38/00

    摘要： Novel compounds of the formula: ##STR1## [wherein A is an .alpha.-amino acid residue; B is a group represented by the formula: ##STR2## (wherein R.sup.4 is hydrogen, lower alkyl, aralkyl or amino-lower alkyl), whereby the linkage between the symbols A and B designates a peptide bond and the group R.sup.4 in B may be linked with A; R.sup.1 is hydrogen, lower alkyl or aralkyl; R.sup.2 is hydrogen, lower alkyl, aralkyl or acyl; X is alkylene] and salts thereof possess, for example, inhibitory activity on angiotensin converting enzyme, and are useful as an agent for diagnosis, prevention or treatment of hypertension as well as circulatory diseases such as cardiopathy and cerebral apoplexy.

    Piperidine derivatives
    44.
    发明授权
    Piperidine derivatives 失效
    哌啶衍生物

    公开(公告)号：US4816466A

    公开(公告)日：1989-03-28

    申请号：US180836

    申请日：1988-04-12

    申请人： Hirosada Sugihara ,  Kohei Nishikawa ,  Katsumi Ito

    发明人： Hirosada Sugihara ,  Kohei Nishikawa ,  Katsumi Ito

    IPC分类号： A61K38/00 ,  C07K5/02 ,  A61K31/445 ,  C07D211/32

    CPC分类号： C07K5/0222 ,  A61K38/00

    摘要： Novel Compounds of the formula: ##STR1## [wherein A is an .alpha.-amino acid residue; B is a group represented by the formula: ##STR2## (wherein R.sup.4 is hydrogen, lower alkyl, aralkyl or amino-lower alkyl), whereby the linkage between the symbols A and B designates a peptide bond and the group R.sup.4 is B may be linked with A; R.sup.1 is hydrogen, lower alkyl or aralkyl; R.sup.2 is hydrogen, lower alkyl, aralkyl or acyl; X is alkylene] and salts thereof posses, for example, inhibitory activity on angiotension converting enzyme, and are useful as an agent for diagnosis, prevention or treatment of hypertension as well as circulatory diseases such as cardiopathy and cerebral apoplexy.

    摘要翻译： 下式的化合物：其中A是α-氨基酸残基; B是由下式表示的基团：其中R4是氢，低级烷基，芳烷基或氨基 - 低级烷基），由此符号A和B之间的连接表示肽键，基团R4可以是B可以是 与A连接 R1是氢，低级烷基或芳烷基; R2是氢，低级烷基，芳烷基或酰基; X是亚烷基]，其盐具有例如对血管紧张素转换酶的抑制活性，可用作高血压以及循环系统疾病如心脏病和脑中风的诊断，预防或治疗剂。

    Thromboxane synthetase inhibiting 3-(1-alkenyl) pyridines
    45.
    发明授权
    Thromboxane synthetase inhibiting 3-(1-alkenyl) pyridines 失效
    抑制3-（1-烯基）吡啶的血栓烷合成酶

    公开(公告)号：US4563446A

    公开(公告)日：1986-01-07

    申请号：US632332

    申请日：1984-07-19

    申请人： Shinji Terao ,  Kohei Nishikawa

    发明人： Shinji Terao ,  Kohei Nishikawa

    IPC分类号： C07D213/02 ,  C07D213/06 ,  C07D213/16 ,  C07D213/26 ,  C07D213/30 ,  C07D213/48 ,  C07D213/55 ,  C07D213/56 ,  C07D213/57 ,  C07D213/80 ,  C07D213/89 ,  C07D401/06 ,  C07D405/02 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D521/00 ,  C07F7/18 ,  C07D213/59 ,  C07D213/24 ,  A61K31/44

    CPC分类号： C07D213/16 ,  C07D213/26 ,  C07D213/30 ,  C07D213/48 ,  C07D213/55 ,  C07D213/56 ,  C07D213/57 ,  C07D213/80 ,  C07D213/89 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D405/06 ,  C07D409/06 ,  C07F7/1856

    摘要： Novel compounds of the formula: ##STR1## wherein R.sup.2 is an aromatic or heterocyclic group, which may optionally be substituted, R.sup.2 is a methyl group, a hydroxymethyl group, a nitroxymethyl group, a formyl group, a nitrogen-containing five-membered ring-methyl group, an acetal-methyl group, a trialkylsilyloxymethyl group, an alkyl- or aryl-sulfonyloxymethyl group, an alkyl- or aryl-sulfonylaminocarbonyloxymethyl group, an acyloxymethyl group, an alkoxycarbonyloxymethyl group, a halogenomethyl group, an alkoxymethyl group, an aryloxymethyl group, a cyano group, a carbamoyl group which may optionally be substituted, a carbamoyloxymethyl group which may optionally be substituted, a thiocarbamoyloxymethyl group which may optionally be substituted, and an alkoxycarbonyl group, n is an integer of 1 to 20, and ##STR2## provided that n is an integer of 9 to 20 when ##STR3## and, at the same time, R.sup.2 is a carboxyl group or an alkoxycarbonyl group, or a pharmacologically acceptable salt thereof, have a selective inhibitory action on biosynthesis of thromboxane A.sub.2 (TXA.sub.2) and an effect of enhancing the production of prostaglandin I.sub.2 (PGI.sub.2), and can be used for mammals to prevent and treat arterial thrombosis caused by platelet aggregation or ischemic diseases caused by vasospasms in cardiac, cerebral and peripheral circulatory system (e.g. cardiac infarction, stroke, occlusion of blood vessels in kidney, lung and other organs, pectic ulcer, etc.).

    摘要翻译： 下式的新型化合物：其中R 2为可任意取代的芳族或杂环基，R 2为甲基，羟甲基，硝酰甲基，甲酰基，含氮五元环 甲基，缩醛 - 甲基，三烷基甲硅烷氧基甲基，烷基 - 或芳基 - 磺酰氧基甲基，烷基 - 或芳基 - 磺酰基氨基羰基氧基甲基，酰氧基甲基，烷氧基羰氧基甲基，卤代甲基，烷氧基甲基， 基团，氰基，可以任意取代的氨基甲酰基，可任意取代的氨基甲酰氧基甲基，可任意取代的硫代氨基甲酰氧基甲基，烷氧基羰基，n为1〜20的整数，＆lt; IMAGE >条件是当中n为9〜20的整数，并且同时R2为羧基或烷氧基羰基时，或其药理学上可接受的盐具有 对血栓素A2（TXA2）的生物合成的选择性抑制作用和增强前列腺素I2（PGI2）的产生的作用，可用于哺乳动物预防和治疗血小板聚集或心脏血管痉挛引起的缺血性疾病引起的动脉血栓形成 ，脑和周围循环系统（例如， 心脏梗死，中风，肾脏，肺部和其他器官中血管闭塞，果胶性溃疡等）。

    Hypotensive imidazole-5-acetic acid derivatives
    46.
    发明授权
    Hypotensive imidazole-5-acetic acid derivatives 失效
    低血糖咪唑-5-乙酸衍生物

    公开(公告)号：US4355040A

    公开(公告)日：1982-10-19

    申请号：US204357

    申请日：1980-11-05

    申请人： Yoshiyasu Furukawa ,  Shoji Kishimoto ,  Kohei Nishikawa

    发明人： Yoshiyasu Furukawa ,  Shoji Kishimoto ,  Kohei Nishikawa

    IPC分类号： A61K31/415 ,  A61K31/4164 ,  A61P9/12 ,  C07D233/64 ,  C07D233/68

    CPC分类号： C07D233/68

    摘要： Novel imidazole-5-acetic acid derivatives of the formula: ##STR1## wherein R.sup.1 is lower alkyl, cycloalkyl or, phenyl which may be substituted with one to three of halogen, nitro, amino, mono(lower alkyl)amino, di(lower alkyl)amino, lower alkyl, lower alkoxyl, benzyloxyl or/and hydroxyl; X.sup.1, X.sup.2 and X.sup.3 are each hydrogen, halogen, nitro, amino, lower alkyl, lower alkoxyl, benzyloxyl or hydroxyl; Y is halogen and R.sup.2 is hydrogen or lower alkyl; provided that X.sup.1 is halogen, lower alkyl, lower alkoxyl, benzyloxyl or hydroxyl when R.sup.1 is unsubstituted or substituted phenyl only with one halogen, di(lower alkyl)amino, lower alkyl or lower alkoxyl, and its salts have hypotensive activity.

    摘要翻译： 下式的新型咪唑-5-乙酸衍生物：其中R 1为低级烷基，环烷基或可被一至三个卤素，硝基，氨基，单（低级烷基）氨基，二（低级 烷基）氨基，低级烷基，低级烷氧基，苄氧基或/和羟基; X 1，X 2和X 3各自为氢，卤素，硝基，氨基，低级烷基，低级烷氧基，苄氧基或羟基; Y是卤素，R 2是氢或低级烷基; 当R1为未取代的或低级烷氧基，苄氧基或羟基时，X1为卤素，二（低级烷基）氨基，低级烷基或低级烷氧基，其盐为低血压活性。

    Prophylactic or therapeutic drug for renal diseases
    47.
    发明授权
    Prophylactic or therapeutic drug for renal diseases 失效
    肾病预防或治疗药物

    公开(公告)号：US06319938B1

    公开(公告)日：2001-11-20

    申请号：US09467488

    申请日：1999-12-20

    申请人： Kohei Nishikawa ,  Yumiko Shibouta ,  Keiji Kubo

    发明人： Kohei Nishikawa ,  Yumiko Shibouta ,  Keiji Kubo

    IPC分类号： A61K3141

    CPC分类号： A61K31/4184 ,  A61K31/415 ,  A61K31/4245 ,  Y02A50/395

    摘要： Prophylactic or therapeutic drugs for diabetic nephropathy or glomerulonephritis, comprising, as an active ingredient, a compound or salt thereof represented by formula (I) wherein R1 stands for H or an optionally substituted hydrocarbon residue; R2 stands for an optionally esterified carboxyl group; R3 stands for a group actually or potentially capable of forming an anion; X shows that the phenylene and phenyl groups bind to each other directly or through a spacer having an atomic chain length of two or less; n stands for 1 or 2; ring A stands for a benzene ring having an optional substituent in addition to R2; Y stands for a bond, —O—, —S(O)m—, wherein m stands for 0, 1 or 2, or —N(R4)— wherein R4 stands for H or an optionally substituted alkyl group are disclosed.

    摘要翻译： 糖尿病性肾病或肾小球性肾炎的预防或治疗药物，其包含作为活性成分的由式（I）表示的化合物或其盐，其中R1代表H或任选取代的烃残基; R2代表任选酯化的羧基; R3代表实际上或潜在能够形成阴离子的组; X表示亚苯基和苯基直接或通过原子链长度为2或更小的间隔物彼此结合; n代表1或2; 环A代表除R2之外具有任选取代基的苯环; Y代表键，-O - ， - S（O）m - ，其中m代表0,1或2或-N（R 4） - ，其中R 4代表H或任意取代的烷基。

    Atrial natriuretic peptide derivative
    49.
    发明授权
    Atrial natriuretic peptide derivative 失效
    ATRIAL NATRIURETIC DEPORATIVE

    公开(公告)号：US5159061A

    公开(公告)日：1992-10-27

    申请号：US101199

    申请日：1987-09-25

    申请人： Masahiko Fujino ,  Mitsuhiro Wakimasu ,  Kohei Nishikawa

    发明人： Masahiko Fujino ,  Mitsuhiro Wakimasu ,  Kohei Nishikawa

    IPC分类号： C07K7/08 ,  A61K38/00 ,  A61P7/10 ,  A61P9/00 ,  A61P9/12 ,  A61P21/02 ,  C07K1/00 ,  C07K1/02 ,  C07K1/113 ,  C07K14/00 ,  C07K14/575 ,  C07K14/58 ,  C07K14/60 ,  D02G3/02 ,  D02G3/06 ,  D02G3/44

    CPC分类号： C07K14/58 ,  C07K14/582 ,  C07K14/60 ,  A61K38/00

    摘要： A peptide derivative of the formula ##STR1## wherein A is hydrogen or a hydrocarbon acyl having 2 to 18 carbon atoms which is substituted by an amino group at the .alpha.-position; B is F-Gly wherein F is a neutral .alpha.-amino acid residue, or NH-(CH.sub.2)nCO wherein n is an integer of 1 to 4; C is a neutral .alpha.-amino acid residue; and E is L-Arg or D-Arg; when A, B and C are hydrogen, Gly-Gly, and Met or Ile, respectively, E is D-Arg, or its pharmacologically acceptable salt has strong hypotensive and natriuretic activity; therefore it is useful as a therapeutic drug for hypertension, a diuretic, and a therapeutic drug for cardiac and cerebral circulatory diseases.

    摘要翻译： 其中A是氢或具有2至18个碳原子的烃基，其被α-位上的氨基取代， ; B是F-Gly，其中F是中性α-氨基酸残基或NH-（CH 2）n CO，其中n是1至4的整数; C是中性α-氨基酸残基; 且E为L-Arg或D-Arg; 当A，B和C分别为氢，Gly-Gly和Met或Ile时，E为D-Arg，或其药理学上可接受的盐具有强烈的降血压和利尿钠活性; 因此作为心血管和脑循环系统疾病的高血压，利尿剂，治疗药物的治疗药物是有用的。