公开(公告)号：US06197806B1

公开(公告)日：2001-03-06

申请号：US08769008

申请日：1996-12-18

申请人： Hitoshi Endou ,  Kazuharu Ienaga

发明人： Hitoshi Endou ,  Kazuharu Ienaga

IPC分类号： A61K31445

CPC分类号： A61K31/4166

摘要： Hydantoin derivatives for eliminating free radicals and active oxygen which can be easily made into pharmaceutical preparations, show little, if any side effects, and are capable of being administered by the oral route. The pharmaceutical compositions for eliminating the active oxygen and the free radicals contain at least one hydantoin derivative represented by the following formula (I): wherein each of R1 and R2, which may be the same or different, represents hydrogen, an alkyl group or a cycloalkyl group; and each of X and Y, which may be the same or different, represents hydrogen, a hydroxyl group, an alkyl group or an alkoxy group, or X and Y together represent an oxo group. The hydantoin derivatives which have an action of eliminating the active oxygen and the free radicals are, accordingly, useful as pharmaceutical agents for treating a variety of diseases in which active oxygen and free radicals are involved or play a detrimental role. Exemplary of the diseases which may be treated are myocardial infarction, reperfusion disturbance, autoimmune diseases, fibrosis, pulmonary diseases, dermatological diseases, arthropathy, side effects of anticancer agents, radiation diseases, septic shock, inflammatory diseases and cataracts.

摘要翻译： 用于消除易于制成药物制剂的自由基和活性氧的乙内酰脲衍生物显示出很少的副作用，并且能够通过口服途径施用。 用于除去活性氧和自由基的药物组合物含有由下式（I）表示的至少一种乙内酰脲衍生物：其中R 1和R 2可以相同或不同，表示氢，烷基或 环烷基 X和Y各自可以相同或不同，表示氢，羟基，烷基或烷氧基，或X和Y一起表示氧代基。 因此，具有消除活性氧和自由基的作用的乙内酰脲衍生物可用作治疗涉及活性氧和自由基或起不利作用的各种疾病的药物。 可以治疗的疾病的示例是心肌梗死，再灌注障碍，自身免疫性疾病，纤维化，肺部疾病，皮肤病，关节病，抗癌剂的副作用，放射性疾病，脓毒性休克，炎性疾病和白内障。

公开(公告)号：US5686251A

公开(公告)日：1997-11-11

申请号：US510316

申请日：1995-08-02

申请人： Seikoh Horiuchi ,  Kazuharu Ienaga ,  Ko Nakamura

发明人： Seikoh Horiuchi ,  Kazuharu Ienaga ,  Ko Nakamura

IPC分类号： G01N33/531 ,  C07D471/04 ,  C07K14/76 ,  C07K16/00 ,  C07K16/44 ,  G01N33/53 ,  G01N33/532 ,  G01N33/68

CPC分类号： G01N33/6842 ,  C07D471/04 ,  C07K16/44 ,  G01N33/5308 ,  G01N33/68 ,  Y02P20/55

摘要： The present invention provides naphthyridinium derivatives which are effective, for example, in diagnosis of diabetes, diabetic complications, dialysis-related complications, aging, diseases accompanied by aging, etc. and also provides an antibody prepared from said derivative as a hapten. The naphthyridinium derivatives of the present invention are compounds represented by the general formula (I): ##STR1## wherein R and R' may be the same or different and are alkyl groups optionally substituted with at least one amino group, at least one protected amino group, at least one carboxyl group, or combinations thereof, and their pharmaceutically accepted salts. It is possible to conduct the diagnosis of diabetes, diabetic complications, dialysis-related complications, aging, diseases accompanied by aging, etc. using a compound of the present invention as an indicator. Moreover, it is possible to utilize a compound of the present invention for the evaluation of the pharmaceutical effect of pharmaceuticals effective for treating diabetes-related diseases, dialysis-related complications, aging and diseases accompanied by aging.

摘要翻译： 本发明提供了例如糖尿病诊断，糖尿病并发症，透析相关并发症，衰老，老化等疾病等有效的萘啶鎓衍生物，并且还提供由所述衍生物制备的抗体作为半抗原。 本发明的萘啶鎓衍生物是由通式（I）表示的化合物：其中R和R'可以相同或不同，并且是任选被至少一个氨基取代的烷基，至少 一个保护的氨基，至少一个羧基或其组合，以及它们的药学上可接受的盐。 使用本发明化合物作为指标，可以进行糖尿病，糖尿病并发症，透析相关并发症，老化，老化等疾病的诊断。 此外，可以利用本发明的化合物来评价有效治疗糖尿病相关疾病，透析相关并发症，老化和伴随衰老的疾病的药物的药效。

公开(公告)号：US5084473A

公开(公告)日：1992-01-28

申请号：US564520

申请日：1990-08-09

申请人： Hiroki Mikami ,  Kazuharu Ienaga

发明人： Hiroki Mikami ,  Kazuharu Ienaga

IPC分类号： C07D233/72 ,  A61K31/415 ,  A61K31/4166 ,  A61P13/02 ,  A61P15/00

CPC分类号： A61K31/415

摘要： The present invention relates to a method for preventing or treating renal failure in a mannal which comprises administering the mammal an effective amount for renal failure of at least one hydantoin derivative of the following formula (I) or a pharmaeutically acceptable salt thereof. ##STR1##

公开(公告)号：US5446021A

公开(公告)日：1995-08-29

申请号：US240534

申请日：1994-05-10

申请人： Masaharu Kurohashi ,  Ko Nakamura ,  Kazuharu Ienaga

发明人： Masaharu Kurohashi ,  Ko Nakamura ,  Kazuharu Ienaga

IPC分类号： A01N43/90 ,  C07K5/12 ,  A61K38/12

CPC分类号： A01N43/90 ,  C07K5/12

摘要： The present invention relates to an agricultural and horticultural composition inducing resistance in plants against salt- and water-stresses which comprises as an active ingredient an effective amount of at least one cyclic dipeptide of the following formula (I) or an agriculturally or horticulturally acceptable salt thereof; ##STR1## wherein each of R.sub.1 and R.sub.2, which may be the same or different, is a hydrogen atom or lower alkyl group, or R.sub.1 and R.sub.2 are joined to form pyrrolidine ring which may optionally have hydroxy group, and R.sub.3 is a hydrogen atom or hydroxy group.

摘要翻译： 本发明涉及一种诱导植物对抗盐胁迫和水分胁迫的抗性的农业和园艺组合物，其包含作为活性成分的有效量的至少一种下式（I）的环状二肽或农业上或园艺上可接受的盐 的; （I）其中R 1和R 2可以相同或不同，其中R 1和R 2各自为氢原子或低级烷基，或R 1和R 2连接形成可任选具有羟基的吡咯烷环，R 3为 氢原子或羟基。

公开(公告)号：US4683240A

公开(公告)日：1987-07-28

申请号：US826607

申请日：1986-02-06

申请人： Kazuharu Ienaga ,  Ko Nakamura ,  Akira Ishii

发明人： Kazuharu Ienaga ,  Ko Nakamura ,  Akira Ishii

IPC分类号： A61K31/415 ,  C07D233/96

CPC分类号： C07D233/96 ,  A61K31/415 ,  Y10S514/824 ,  Y10S514/866

摘要： Pharmaceutical compositions containing imidazolidinetrione derivatives or pharmaceutically acceptable salts thereof having hypoglycemic and hypolipidemic effects. The compositions comprise as an active ingredient at least one imidazolidinetrione derivative of the formula: ##STR1## wherein each of R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, an alkyl group, a cycloalkyl group or ##STR2## and each of R.sub.3 and R.sub.4, which may be the same or different, is hydrogen, halogen, a nitro group, a lower alkyl group or a lower alkoxy group.

摘要翻译： 含有具有低血糖和降血脂作用的咪唑烷四酮衍生物或其药学上可接受的盐的药物组合物。 所述组合物包含至少一种下式的咪唑烷四酮衍生物作为活性成分：其中R 1和R 2可以相同或不同，分别为氢，烷基，环烷基或者每个 可以相同或不同的R 3和R 4是氢，卤素，硝基，低级烷基或低级烷氧基。

公开(公告)号：US06451831B1

公开(公告)日：2002-09-17

申请号：US10074772

申请日：2002-02-12

申请人： Kazuharu Ienaga ,  Hiroki Mikami ,  Ryoji Nishibata

发明人： Kazuharu Ienaga ,  Hiroki Mikami ,  Ryoji Nishibata

IPC分类号： A61K31415

CPC分类号： A61K31/4166

摘要： A highly safe and useful therapeutic agent for hypoalbuminaemia contains a hydantoin derivative represented by the formula (I) or a pharmaceutically acceptable salt thereof as an effective ingredient: wherein each of R1 and R2, which may be the same or different, represents hydrogen, an alkyl group or a cycloalkyl group; and each of X and Y, which may be the same or different, represents hydrogen, a hydroxyl group, an alkyl group or an alkoxy group, or X and Y together represent an oxo group. Administration of the compounds substantially increases the serum albumin value of patients suffering from hypoalbuminaemia from abnormal values, and significantly improves the condition of hypoalbuminaemia.

摘要翻译： 用于低白蛋白血症的高度安全和有用的治疗剂含有由式（I）表示的乙内酰脲衍生物或其药学上可接受的盐作为有效成分：其中R 1和R 2可以相同或不同，表示氢， 烷基或环烷基; X和Y各自可以相同或不同，表示氢，羟基，烷基或烷氧基，或X和Y一起表示氧代基。 化合物的施用显着提高了患有低蛋白血症的患者的血清白蛋白值异常值，并显着改善了低白蛋白血症的状况。

公开(公告)号：US5013750A

公开(公告)日：1991-05-07

申请号：US551375

申请日：1990-07-11

申请人： Ko Nakamura ,  Kazuharu Ienaga

发明人： Ko Nakamura ,  Kazuharu Ienaga

IPC分类号： C07D233/88

CPC分类号： C07D233/88

摘要： The glycocyamidine derivatives of the present invention are represented by the following formula (I): ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3, which may be the same or different, is hydrogen or a lower alkyl group, preferably a straight or branched alkyl group having 1 to 3 carbon atoms, such as methyl, ethyl, propyl or isopropyl, and R represents hydrogen or an acetyl group,which are useful as test reagents for diagnosis of renal failure.

摘要翻译： 本发明的甘氨酰胺衍生物由下式（I）表示：其中R 1，R 2和R 3可以相同或不同，为氢或低级烷基，优选直链或 甲基，乙基，丙基，异丙基等碳原子数1〜3的支链烷基，R表示氢或乙酰基，可用作肾功能衰竭的诊断试剂。

公开(公告)号：US4708961A

公开(公告)日：1987-11-24

申请号：US919746

申请日：1986-10-16

申请人： Kazuharu Ienaga ,  Ko Nakamura

发明人： Kazuharu Ienaga ,  Ko Nakamura

IPC分类号： C07D209/12 ,  A61K31/40

CPC分类号： C07D209/12

摘要： The present invention is concerned with novel acylindole derivatives of the formula (I) and platelet-aggregation inhibiting agents containing them as an active ingredient. ##STR1## In the formula (I), either R.sub.1 and R.sub.2 is hydrogen, an alkyl group having 1 to 5 carbon atoms, an alkyl group substituted by at least one hydroxy group and having 1 to 5 carbon atoms, or a group of the formula ##STR2## in which R.sub.3 is an alkyl group having 1 to 5 carbon atoms, and --OR.sub.2 is a substituent at the ortho or para position.The compounds of the invention are useful as preventive medicine or remedy for various diseases or symptoms caused by platelet-aggregation, as well as inhibitors of platelet-aggregation on vascular walls during or after an operation.

摘要翻译： 本发明涉及式（I）的新型丙烯酰基吲哚衍生物和含有它们作为活性成分的血小板聚集抑制剂。 （I）在式（I）中，R 1和R 2是氢，具有1至5个碳原子的烷基，被至少一个羟基取代且具有1至5个碳原子的烷基，或 其中R 3是具有1至5个碳原子的烷基的式“IMAGE”的基团，-OR 2是邻位或对位的取代基。 本发明的化合物可用作预防药物或由血小板聚集引起的各种疾病或症状的补救剂，以及在手术期间或手术后在血管壁上血小板聚集的抑制剂。

公开(公告)号：US06251929B1

公开(公告)日：2001-06-26

申请号：US09434494

申请日：1999-11-05

申请人： Mitsuru Naiki ,  Takumi Numazawa ,  Tomoyuki Okada ,  Kazuharu Ienaga ,  Kazuyoshi Sawada

发明人： Mitsuru Naiki ,  Takumi Numazawa ,  Tomoyuki Okada ,  Kazuharu Ienaga ,  Kazuyoshi Sawada

IPC分类号： A64K31415

CPC分类号： A61K31/4166

摘要： A highly safe therapeutic agent for intractable vasculitis such as malignant rheumatoid arthritis contains a hydantoin derivative represented by the formula (I) or a pharmaceutically acceptable salt thereof as an effective ingredient: wherein each of R1, and R2, which may be the same or different, represents hydrogen, an alkyl group or a cycloalkyl group; and each of X and Y, which may be the same or different, represents hydrogen, a hydroxyl group, an alkyl group or an alkoxy group, or X and Y together represent an oxo group. The hydantoin derivatives significantly suppress the generation of arthritis and arteritis (cutaneous ulcer and auricular infarcted necrosis) which are naturally developed in model animals (MRL/lpr), and further significantly elongate the survival rate of MRL/lpr mice. Consequently, the hydantoin derivatives, having low toxicity and little side effects are very useful as highly safe therapeutic agents for intractable vasculitis such as malignant rheumatoid arthritis.

摘要翻译： 用于顽固性血管炎的恶性类风湿性关节炎的高度安全的治疗剂含有式（I）表示的乙内酰脲衍生物或其药学上可接受的盐作为有效成分：其中R1和R2可以相同或不同 表示氢，烷基或环烷基; X和Y各自可以相同或不同，表示氢，羟基，烷基或烷氧基，或X和Y一起表示氧代基。 乙内酰脲衍生物显着抑制模型动物（MRL / lpr）中天然发育的关节炎和动脉炎（皮肤溃疡和耳廓梗塞坏死）的产生，并进一步显着延长MRL / lpr小鼠的存活率。 因此，具有低毒性和少量副作用的乙内酰脲衍生物作为难治性血管炎如恶性类风湿性关节炎的高度安全的治疗剂是非常有用的。

公开(公告)号：US4957936A

公开(公告)日：1990-09-18

申请号：US472494

申请日：1990-01-30

申请人： Ko Nakamura ,  Kazuharu Ienaga

发明人： Ko Nakamura ,  Kazuharu Ienaga

IPC分类号： G01N33/50 ,  A61K31/415 ,  A61K49/00 ,  A61P9/08 ,  A61P9/10 ,  C07D233/88

CPC分类号： C07D233/88 ,  Y02P20/55

摘要： The glycocyamidine derivatives of the present invention are represented by the following formula (I): ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3, which may be the same or different, is hydrogen or a lower alkyl group, preferably a straight or branched alkyl group having 1 to 3 carbon atoms, such as methyl, ethyl, propyl or isopropyl, and R represents hydrogen or an acetyl group.which are useful as test reagents for diagnosis of renal failure.

摘要翻译： 本发明的糖胞苷衍生物由下式（I）表示：其中R 1，R 2和R 3可以相同或不同，为氢或低级烷基，优选直链或支链 具有1至3个碳原子的烷基，例如甲基，乙基，丙基或异丙​​基，R代表氢或乙酰基。 其用作诊断肾衰竭的测试试剂。