公开(公告)号：US07211596B2

公开(公告)日：2007-05-01

申请号：US10477275

申请日：2002-05-09

申请人： Hiroshi Yoshida ,  Naoki Matsuo ,  Masatoshi Chiba

发明人： Hiroshi Yoshida ,  Naoki Matsuo ,  Masatoshi Chiba

IPC分类号： A61K31/4152

CPC分类号： C07D231/20 ,  A61K9/0019 ,  A61K31/4152 ,  A61K47/10 ,  A61K47/186

摘要： An injection which contains as the active ingredient a pyrazolone derivative which typically is Edaravone, a physiologically acceptable salt thereof, or a hydrate or solvate of either in an amount of 3 to 60 mg/mL. It is excellent in long-term stability, product storage, and suitability for use.

摘要翻译： 含有作为活性成分的吡唑啉酮衍生物，其通常为依达拉奉，其生理学上可接受的盐，或水合物或溶剂化物，其含量为3-60mg / mL。 它具有优异的长期稳定性，产品储存性和适用性。

公开(公告)号：US20070082910A1

公开(公告)日：2007-04-12

申请号：US10552340

申请日：2004-04-08

申请人： Toshihiro Yamamoto ,  Kumi Yamada

发明人： Toshihiro Yamamoto ,  Kumi Yamada

IPC分类号： A61K31/502

CPC分类号： A61K31/5025 ,  A61K31/502 ,  C07D237/32

摘要： The present invention provides an agent for inhibiting an excessive effect of NAD(P)H oxidase, which contains a compound that does not substantially inhibit the effect of leukocyte NADPH oxidase but inhibits the effect of NAD(P)H oxidase in tissues other than leukocytes, and a pharmaceutical composition containing said inhibitor.

摘要翻译： 本发明提供了抑制NAD（P）H氧化酶过度作用的药剂，其含有基本上不抑制白细胞NADPH氧化酶的作用但抑制NAD（P）H氧化酶在白细胞以外的组织中的作用的化合物 和含有所述抑制剂的药物组合物。

公开(公告)号：US07115635B2

公开(公告)日：2006-10-03

申请号：US10476149

申请日：2002-04-26

申请人： Masatoshi Kiuchi ,  Takanobu Kuroita ,  Hideo Tomozane ,  Shuuzou Takeda ,  Yoshihito Tanaka ,  Hidemitsu Higashi ,  Shigeki Kuwahara

发明人： Masatoshi Kiuchi ,  Takanobu Kuroita ,  Hideo Tomozane ,  Shuuzou Takeda ,  Yoshihito Tanaka ,  Hidemitsu Higashi ,  Shigeki Kuwahara

IPC分类号： A61K31/445 ,  C07D419/12

CPC分类号： C07D401/12 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/55 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D491/10

摘要： The object of the present invention is to provide a compound having a treatment effect based on a chemokine inhibitory activity, which is satisfactory as a pharmaceutical product for oral administration.The present inventors have found that the following benzylpiperidine derivative (the formula (1)) has a chemokine inhibitory activity. Further intensive studies have resulted in successful enhancement of the chemokine inhibitory activity and stability in blood of the present compound, as well as the completion of the present invention. wherein each symbol is as defined in the specification.

摘要翻译： 本发明的目的是提供一种具有基于趋化因子抑制活性的治疗效果的化合物，其作为用于口服给药的药物产品是令人满意的。 本发明人发现以下苄基哌啶衍生物（式（1））具有趋化因子抑制活性。 进一步的深入研究已经导致本发明化合物的趋化因子抑制活性和血液稳定性的成功增强以及本发明的完成。 其中每个符号如说明书中所定义。

公开(公告)号：US07112594B2

公开(公告)日：2006-09-26

申请号：US10344261

申请日：2001-08-09

申请人： Hiroyuki Ushio ,  Youichiro Naito ,  Naoki Sugiyama ,  Takafumi Kawaguchi ,  Makio Ohtsuki ,  Kenji Chiba

发明人： Hiroyuki Ushio ,  Youichiro Naito ,  Naoki Sugiyama ,  Takafumi Kawaguchi ,  Makio Ohtsuki ,  Kenji Chiba

IPC分类号： A61K31/445 ,  C07D409/10 ,  C07D211/06

CPC分类号： C07D405/12 ,  A61K31/015 ,  A61K31/343 ,  A61K31/381 ,  A61K31/404 ,  A61K31/4184 ,  A61K31/4365 ,  A61K31/4704 ,  A61K31/498 ,  C07D209/42 ,  C07D211/46 ,  C07D307/85 ,  C07D307/86 ,  C07D333/70 ,  C07D409/12 ,  C07D495/04

摘要： Compounds represented by the following general formula (I) wherein ring A is benzene, cyclohexane, pyridine, piperidine, a derivative thereof, imidazole, a derivative thereof, etc.; the ring B represents benzene, cyclohexane, pyrrole or a derivative thereof, furan, thiophene, etc.; R1, R2 and R3 represent each hydrogen, alkyl, halogen, hydroxyl, alkoxy, etc.; W represents hydrogen, alkyl or hydroxycarbonylalkyl; X represents halogen, cyano, nitro, etc.; X′ represents hydrogen, halogen, etc.; and Y represents alkyl, hydroxyalkyl, hydroxycarbonylalkyl, aminoalkyl, etc.; salt thereof, and drugs comprising these compounds. Because of having an exellent effect of inhibiting activated lymphocyte proliferation, these compounds are usefull as preventives or remedies for various autoimmune diseases.

摘要翻译： 由下列通式（I）表示的化合物，其中环A为苯，环己烷，吡啶，哌啶，其衍生物，咪唑，其衍生物等; 环B表示苯，环己烷，吡咯或其衍生物，呋喃，噻吩等; R 1，R 2和R 3表示每个氢，烷基，卤素，羟基，烷氧基等; W表示氢，烷基或羟基羰基烷基; X表示卤素，氰基，硝基等; X'表示氢，卤素等; Y表示烷基，羟烷基，羟基羰基烷基，氨基烷基等; 其盐，以及包含这些化合物的药物。 由于具有抑制活化淋巴细胞增殖的效果，这些化合物可用作各种自身免疫性疾病的预防剂或治疗剂。

公开(公告)号：US07109208B2

公开(公告)日：2006-09-19

申请号：US10474369

申请日：2002-04-11

申请人： Yoshiko Takayama ,  Yukuo Yoshida ,  Masayoshi Uehata

发明人： Yoshiko Takayama ,  Yukuo Yoshida ,  Masayoshi Uehata

IPC分类号： A61K31/437 ,  A61K31/44

CPC分类号： C07D471/04 ,  A61K9/0048 ,  A61K31/00 ,  A61K31/437 ,  C07D211/00

摘要： The present invention provides a visual function disorder improving agent containing a compound having Rho kinase inhibitory activity, particularly (R)-(+)-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)-4-(1-aminoethyl)benzamide, as an effective component. This agent has axon of the retinal ganglion cellal extension promoting action and optic nerve cell regeneration promoting action, and is useful for the treatment of a visual function disorder associated with various eye diseases caused by damage, defects, degeneration and the like in the retinal or optic nerve.

摘要翻译： 本发明提供含有具有Rho激酶抑制活性的化合物的视觉功能障碍改善剂，特别是（R） - （+） - N-（1H-吡咯并[2,3-b]吡啶-4-基）-4- （1-氨基乙基）苯甲酰胺作为有效成分。 该药剂具有视网膜神经节细胞延伸促进作用和视神经细胞再生促进作用的轴突，并且可用于治疗由视网膜中的损伤，缺陷，变性等引起的各种眼病的视觉功能障碍， 视神经

公开(公告)号：US20060111418A1

公开(公告)日：2006-05-25

申请号：US10541702

申请日：2004-01-09

申请人： Junichi Kawakami

发明人： Junichi Kawakami

IPC分类号： A61K31/4152

CPC分类号： C07D231/26 ,  A61K31/4152

摘要： An object of the present invention is to provide a blood-brain barrier disruption inhibitor. The present invention provides a blood-brain barrier disruption inhibitor which comprises as an active ingredient a pyrazolone derivative represented by the following formula (I) or a physiologically acceptable salt thereof, or a hydrate thereof or a solvate thereof: wherein R1 represents a hydrogen atom, an aryl group, an alkyl group, or an alkoxycarbonylalkyl group; R2 represents a hydrogen atom, an aryloxy group, an arylmercapto group, an alkyl group or a hydroxyalkyl group; or R1 and R2 are combined with each other to represent an alkylene group; and R3 represents a hydrogen atom, an alkyl group, a cycloalkyl group, a hydroxyalkyl group, a benzyl group, a naphthyl group, a phenyl group, or a phenyl group substituted with 1 to 3 substituents selected from the group consisting of an alkyl group, an alkoxy group, a hydroxyalkyl group, an alkoxycarbonyl group, an alkylmercapto group, an alkylamino group, a dialkylamino group, a halogen atom, a trifluoromethyl group, a carboxyl group, a cyano group, a hydroxyl group, a nitro group, an amino group and an acetamide group.

摘要翻译： 本发明的目的是提供一种血脑屏障破坏抑制剂。 本发明提供一种血脑屏障破坏抑制剂，其包含作为活性成分的由下式（I）表示的吡唑啉酮衍生物或其生理学上可接受的盐，或其水合物或其溶剂合物：其中R 1 代表氢原子，芳基，烷基或烷氧基羰基烷基; R 2表示氢原子，芳氧基，芳基巯基，烷基或羟烷基; 或R 1和R 2彼此结合以表示亚烷基; R 3表示氢原子，烷基，环烷基，羟基烷基，苄基，萘基，苯基或被1〜3个取代基取代的苯基 由烷基，烷氧基，羟基烷基，烷氧基羰基，烷基巯基，烷基氨基，二烷基氨基，卤素原子，三氟甲基，羧基，氰基， 羟基，硝基，氨基和乙酰胺基。

公开(公告)号：US20060088538A1

公开(公告)日：2006-04-27

申请号：US10546594

申请日：2004-02-27

申请人： Saiko Hosokawa ,  Masahiko Aoki ,  Yoko Hirakawa ,  Seima Itami ,  Hiroe Umeki ,  Yoshiro Saikawa ,  Koichiro Kumai ,  Kazumasa Fukuda

发明人： Saiko Hosokawa ,  Masahiko Aoki ,  Yoko Hirakawa ,  Seima Itami ,  Hiroe Umeki ,  Yoshiro Saikawa ,  Koichiro Kumai ,  Kazumasa Fukuda

IPC分类号： A61K39/395 ,  C07H21/04 ,  C12P21/06 ,  C07K16/30

CPC分类号： G01N33/57442 ,  A61K47/6857 ,  A61K47/6913 ,  C07K16/30 ,  C07K2317/73 ,  G01N33/57423

摘要： A novel human monoclonal antibody specifically recognizing cancer cells such as non-small cell lung cancer, pancreatic cancer and gastric cancer cells is produced by hybridomas which are obtained by fusing lymphocytes derived from a cancer tissue of a cancer patient with mouse myeloma cells. An anti-cancer drug is obtained by using the antibody alone or anchoring the antibody on the surface of a liposome containing a toxin or an anti-cancer drug encapsulated therein. More specifically, an anti-cancer drug is obtained by using an antibody, in which variable region of its heavy chain comprises the amino acid sequence of SEQ ID NO: 115 and variable region of the light chain comprises the amino acid sequence of SEQ ID NO: 117, alone or anchoring the antibody on the surface of a liposome containing a toxin or an anti-cancer drug encapsulated therein.

摘要翻译： 通过将衍生自癌症患者的癌症组织的淋巴细胞与小鼠骨髓瘤细胞融合获得的杂交瘤产生特异性识别癌细胞例如非小细胞肺癌，胰腺癌和胃癌细胞的新型人单克隆抗体。 通过单独使用抗体或将抗体锚定在包含毒素或其中的抗癌药物的脂质体的表面上来获得抗癌药物。 更具体地，通过使用抗体，其重链的可变区包含SEQ ID NO：115的氨基酸序列并且轻链的可变区包含SEQ ID NO的氨基酸序列 ：117单独或将抗体锚定在包含其中的毒素或抗癌药物的脂质体的表面上。

公开(公告)号：US06974819B2

公开(公告)日：2005-12-13

申请号：US10362850

申请日：2001-08-31

申请人： Antonio Almario Garcia ,  Thierry Gallet ,  Adrien Tak Li ,  Alistair Lochead ,  Séverine Marguerie ,  Alain Nedelec ,  Mourad Saady ,  Philippe Yaiche

发明人： Antonio Almario Garcia ,  Thierry Gallet ,  Adrien Tak Li ,  Alistair Lochead ,  Séverine Marguerie ,  Alain Nedelec ,  Mourad Saady ,  Philippe Yaiche

IPC分类号： A61K31/519 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P17/14 ,  A61P23/02 ,  A61P25/00 ,  A61P25/02 ,  A61P25/16 ,  A61P25/24 ,  A61P25/28 ,  A61P27/06 ,  A61P35/00 ,  A61P35/02 ,  C07D487/04

CPC分类号： C07D487/04 ,  A61K31/519

摘要： Imidazo[1,2-α]pyrimidinones and pyrimido[1,2-α]pyrimidinones useful for preventive and/or therapeutic treatment of neurodegenerative diseases, such as Alzheimer's disease, caused by abnormal GSK3β activity.

摘要翻译： 咪唑并[1,2-α]嘧啶酮和嘧啶并[1,2-α]嘧啶酮，用于预防和/或治疗由异常GSK3β活性引起的神经变性疾病，如阿尔茨海默病。

公开(公告)号：US06967207B2

公开(公告)日：2005-11-22

申请号：US10203278

申请日：2001-02-07

申请人： Satoshi Yamazaki

发明人： Satoshi Yamazaki

IPC分类号： A61K31/439 ,  A61P1/04 ,  C07D495/04 ,  C07D519/00 ,  A61K31/44

CPC分类号： C07D495/04 ,  A61K31/439 ,  A61K31/4743

摘要： The compound of the following formula: wherein R1 and R2 independently represent a hydrogen atom or a lower alkyl group; A represents a group selected from the group consisting of 1-azabicyclo[3.2.2]nonyl group, 1-azabicyclo[2.2.2]octyl group, or an N-oxide thereof, or a pharmaceutically acceptable salt thereof or a hydrate thereof has both improving effect on enterokinetic functions and suppressing effect on acid secretion, and also is highly safe. Accordingly, the substance is useful as preventive or therapeutic medicament for a gastroesophageal reflux disease.

摘要翻译： 下式的化合物：其中R 1和R 2独立地表示氢原子或低级烷基; A表示选自1-氮杂双环[3.2.2]壬基，1-氮杂双环[2.2.2]辛基或其N-氧化物或其药学上可接受的盐或其水合物的基团具有 对肠动力学功能的改善作用和对酸分泌的抑制作用，也是高度安全的。 因此，该物质可用作胃食管反流病的预防或治疗药物。

公开(公告)号：US06926884B2

公开(公告)日：2005-08-09

申请号：US10220610

申请日：2001-03-02

申请人： Yasuo Ikeda ,  Hiroshi Saito ,  Hiromichi Mukai ,  Yoshiyuki Mori ,  Mitsuru Murata

发明人： Yasuo Ikeda ,  Hiroshi Saito ,  Hiromichi Mukai ,  Yoshiyuki Mori ,  Mitsuru Murata

IPC分类号： A61K38/00 ,  A61K47/48 ,  A61K49/00 ,  A61K49/14 ,  A61K51/08 ,  A61P7/02 ,  A61P7/04 ,  A61P9/00 ,  A61P29/00 ,  C07K14/705 ,  A61K38/14 ,  A61K47/34 ,  C07K14/475

CPC分类号： C07K14/705 ,  A61K38/00 ,  A61K47/544 ,  A61K47/60 ,  A61K47/64 ,  A61K47/6911 ,  A61K49/0002 ,  A61K49/085 ,  A61K49/14

摘要： The present invention provides a conjugate wherein GP (glycoprotein) Ib and a lipid are bonded via polyalkylene oxide. The present invention also provides a complex (GPIb lipid complex) containing this conjugate and a free lipid. The GPIb lipid complex is expected to have a potential for practical application in a wide range, as a platelet substitute, a pharmaceutical agent for the prophylaxis or treatment of angiopathy, vascular damage and thrombosis, a diagnostic for vWF deficiency and the like, a biological or medical reagent, a reagent for screening platelet aggregation suppressant or antithrombosis, and the like. The GPIb lipid complex of the present invention is also useful as a diagnostic for finding the location of vascular lesion or thrombus formation, or a therapeutic agent thereof. Moreover, the GPIb lipid complex of the present invention is also superior in retention property in blood, which enables continuous expression of a pharmacological action. The conjugate of the present invention is highly utilizable as an active ingredient of the GPIb lipid complex of the present invention.

摘要翻译： 本发明提供了通过聚环氧烷键合GP（糖蛋白）1b和脂质的结合物。 本发明还提供了含有该缀合物和游离脂质的复合物（GPIb脂质复合物）。 预期GPIb脂质复合物在广泛范围内具有实际应用的潜力，作为血小板替代物，用于预防或治疗血管病，血管损伤和血栓形成的药剂，对vWF缺乏症的诊断等，生物 或医用试剂，用于筛选血小板聚集抑制剂或抗血栓形成的试剂等。 本发明的GPIb脂质复合物也可用作诊断血管损伤或血栓形成的位置，或其治疗剂。 此外，本发明的GPIb脂质复合物在血液中的保留性也优异，能够连续表达药理作用。 本发明的缀合物作为本发明的GPIb脂质复合物的活性成分是高度可利用的。