公开(公告)号：US20130245074A1

公开(公告)日：2013-09-19

申请号：US13991025

申请日：2011-12-01

申请人： Masaya Kokubo ,  Koji Yano

发明人： Masaya Kokubo ,  Koji Yano

IPC分类号： A61K31/198 ,  A61K45/06 ,  C07C229/36

CPC分类号： C07C229/26 ,  A61K31/12 ,  A61K31/122 ,  A61K31/165 ,  A61K31/198 ,  A61K31/216 ,  A61K31/235 ,  A61K31/24 ,  A61K31/277 ,  A61K31/4412 ,  A61K45/06 ,  C07B2200/13 ,  C07C229/36 ,  A61K2300/00

摘要： Provided is a levodopa prodrug that overcomes the problems attributed to the blood kinetics of levodopa such as large number of doses and the incidence of side effects due to frequent dosing. (2S)-2-Amino-3-(3,4-bis((2-(benzoyloxy)-2-methylpropanoyl)oxy)phenyl)propanoic acid, a salt thereof, or a solvate thereof is a levodopa prodrug, and provides a flat blood concentration-time profile of levodopa through oral administration, and therefore is useful as a preventive and/or therapeutic agent for Parkinson's disease and/or Parkinson's syndrome that overcomes the problems associated with pharmaceutical preparations of levodopa.

摘要翻译： 提供了左旋多巴前药，其克服了左旋多巴的血液动力学所引起的问题，例如大量的剂量以及由于频繁给药引起的副作用的发生率。 （2S）-2-氨基-3-（3,4-双（（2-（苯甲酰氧基）-2-甲基丙酰基）氧基）苯基）丙酸，其盐或其溶剂合物是左旋多巴前药，并提供 通过口服给药左旋多巴的平坦血液浓度 - 时间曲线，因此可用作克服与左旋多巴药物制剂相关的问题的帕金森病和/或帕金森综合征的预防和/或治疗剂。

公开(公告)号：US07968572B2

公开(公告)日：2011-06-28

申请号：US12089108

申请日：2006-10-02

申请人： Hisao Nakai ,  Shingo Yamamoto ,  Shingo Nakatani ,  Tomomi Hirosaki

发明人： Hisao Nakai ,  Shingo Yamamoto ,  Shingo Nakatani ,  Tomomi Hirosaki

IPC分类号： A61K31/4412 ,  A61K31/426 ,  A61K31/421 ,  C07D417/02

CPC分类号： A61K31/00 ,  A61K31/4439 ,  A61K45/06 ,  C07D401/04 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14

摘要： It is intended to provide a compound represented by the formula (I): wherein all the symbols are as defined in the description; which has a p38 MAP kinase inhibitory activity, a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. The compound of the invention is useful for preventing or treating a disease in which the abnormal production of a cytokine such as an inflammatory cytokine or a chemokine or overreaction to them is considered to be involved in the cause and aggravation of pathological conditions, in other words, an inflammatory disease, a respiratory disease, a cardiovascular disease, a central nervous system disease or the like, which is a cytokine-mediated disease.

摘要翻译： 旨在提供由式（I）表示的化合物：其中所有符号如说明书中所定义; 其具有p38 MAP激酶抑制活性，其盐，其N-氧化物，其溶剂化物或其前药。 本发明的化合物可用于预防或治疗其中细胞因子如炎性细胞因子或趋化因子的异常产生或对其过度反应被认为参与病理状况的原因和加重的疾病，换句话说 ，炎性疾病，呼吸系统疾病，心血管疾病，中枢神经系统疾病等，其是细胞因子介导的疾病。

公开(公告)号：US07291644B2

公开(公告)日：2007-11-06

申请号：US11412879

申请日：2006-04-28

申请人： Kazuhiko Torisu ,  Maki Iwahashi ,  Kaoru Kobayashi ,  Fumio Nambu

发明人： Kazuhiko Torisu ,  Maki Iwahashi ,  Kaoru Kobayashi ,  Fumio Nambu

IPC分类号： A61K31/335 ,  C07D265/36 ,  C07D405/00 ,  C07D209/02 ,  C07D209/04

CPC分类号： C07D405/12 ,  A61K31/405 ,  A61K31/422 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/538 ,  C07D209/22 ,  C07D401/12 ,  C07D413/12

摘要： Compounds represented by formula (I) wherein all symbols represent the same meanings as described in specification and salts thereof. Since the compound represented by the formula (I) binds and antagonizes to DP receptor, it is useful for the prevention or treatment against the disease such as allergic disorder, diseases accompanied with itching, secondary diseases generated by behaviors caused by itching, inflammation, chronic obstructive pulmonary disease, ischemic reperfusion disorder, pleuritis complicated by rheumatoid arthritis, cerebrovascular disease, and ulcerative colitis.

摘要翻译： 由式（I）表示的化合物，其中所有符号表示与说明书及其盐中所述相同的含义。 由于式（I）表示的化合物与DP受体结合并拮抗，因此可用于预防或治疗诸如过敏性疾病，伴有瘙痒的疾病，由瘙痒引起的行为引起的继发性疾病，炎症，慢性 阻塞性肺病，局部缺血再灌注障碍，类风湿关节炎并发的胸膜炎，脑血管疾病和溃疡性结肠炎。

公开(公告)号：US07629369B2

公开(公告)日：2009-12-08

申请号：US11239406

申请日：2005-09-30

申请人： Atsushi Naganawa ,  Tetsuji Saito ,  Kaoru Kobayashi ,  Takayuki Maruyama ,  Yoshihiko Nakai ,  Shinsuke Hashimoto

发明人： Atsushi Naganawa ,  Tetsuji Saito ,  Kaoru Kobayashi ,  Takayuki Maruyama ,  Yoshihiko Nakai ,  Shinsuke Hashimoto

IPC分类号： C07D285/08 ,  C07D271/06 ,  C07D257/04 ,  A61K31/41

CPC分类号： C07D213/70 ,  C07D277/36 ,  C07D307/64 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

摘要： An N-phenylarylsulfonylamide compound of formula (I) (R1 is COOH etc.; R2 is hydrogen, methyl, etc.; R3 and R4 are a combination of methyl and methyl, etc.; R5 is isopropyl etc.; Ar is thiazolyl, pyridyl, 5-methyl-2-furyl each optionally substituted with methyl; n is zero or 1), a synthetic intermediate for the compound and a process for its preparation. The compound of formula (I) binds to a prostaglandin E2 receptor, especially an EP1 subtype receptor, and antagonizes it. It is less affected by protein binding, so it has a satisfactory in vivo activity. Therefore, it is considered to be useful as an analgesic, an antipyretic agent, an agent for the treatment of pollakiuria (frequent urination) and/or lower urinary tract disease syndrome or an antineoplastic agent.

摘要翻译： 式（I）的N-苯基芳基磺酰胺化合物（R1是COOH等; R2是氢，甲基等; R3和R4是甲基和甲基的组合等; R5是异丙基等; Ar是噻唑基， 吡啶基，5-甲基-2-呋喃基，各自任选被甲基取代; n为0或1），化合物的合成中间体及其制备方法。 式（I）化合物结合前列腺素E2受体，特别是EP1亚型受体，并拮抗它。 蛋白质结合的影响较小，因此具有令人满意的体内活性。 因此，认为可用作止痛剂，解热剂，治疗尿频（尿频）和/或下尿路疾病综合征或抗肿瘤药物的药剂。

公开(公告)号：US08748485B2

公开(公告)日：2014-06-10

申请号：US13991025

申请日：2011-12-01

申请人： Masaya Kokubo ,  Koji Yano

发明人： Masaya Kokubo ,  Koji Yano

IPC分类号： A01N37/34 ,  A61K31/275 ,  A01N37/12 ,  A01N37/44 ,  A61K31/195 ,  C07C229/00 ,  A61K31/198 ,  C07C229/36

CPC分类号： C07C229/26 ,  A61K31/12 ,  A61K31/122 ,  A61K31/165 ,  A61K31/198 ,  A61K31/216 ,  A61K31/235 ,  A61K31/24 ,  A61K31/277 ,  A61K31/4412 ,  A61K45/06 ,  C07B2200/13 ,  C07C229/36 ,  A61K2300/00

摘要： Provided is a levodopa prodrug that overcomes the problems attributed to the blood kinetics of levodopa such as large number of doses and the incidence of side effects due to frequent dosing. (2S)-2-Amino-3-(3,4-bis((2-(benzoyloxy)-2-methylpropanoyl)oxy)phenyl)propanoic acid, a salt thereof, or a solvate thereof is a levodopa prodrug, and provides a flat blood concentration-time profile of levodopa through oral administration, and therefore is useful as a preventive and/or therapeutic agent for Parkinson's disease and/or Parkinson's syndrome that overcomes the problems associated with pharmaceutical preparations of levodopa.

摘要翻译： 提供了左旋多巴前药，其克服了左旋多巴的血液动力学所引起的问题，例如大量的剂量以及由于频繁给药引起的副作用的发生率。 （2S）-2-氨基-3-（3,4-双（（2-（苯甲酰氧基）-2-甲基丙酰基）氧基）苯基）丙酸，其盐或其溶剂合物是左旋多巴前药，并提供 通过口服给药左旋多巴的平坦血液浓度 - 时间曲线，因此可用作克服与左旋多巴药物制剂相关的问题的帕金森病和/或帕金森综合征的预防和/或治疗剂。

公开(公告)号：US07273725B2

公开(公告)日：2007-09-25

申请号：US10493393

申请日：2002-10-22

申请人： Tasuku Honjo ,  Kei Tashiro ,  Jun Takahashi ,  Hiroki Toda

发明人： Tasuku Honjo ,  Kei Tashiro ,  Jun Takahashi ,  Hiroki Toda

IPC分类号： C12P21/06 ,  C07K14/00

CPC分类号： C07K16/18 ,  A61K38/00 ,  A61K48/00 ,  A61K2039/505 ,  C07K14/47 ,  G01N33/6896 ,  G01N2333/47 ,  G01N2500/00 ,  G01N2500/04

摘要： The present invention relates to human, rat and mouse stem cell-derived neuron survival factor polypeptides (SDNSF), a process for producing them, cDNA encoding SDNSF, a vector comprising the cDNA, host cells transformed by the vector, an antibody against SDNSF, pharmaceutical compositions containing SDNSF or the antibody, a method of assaying SDNSF, a reagent for assaying SDNSF, and a screening method using SDNSF. The polypeptides are effective in the survival of nerve cells and, therefore, efficacious in treating injury to the central nerve system caused by brain infarction, brain hemorrhage, spinal cord injury, etc.

摘要翻译： 本发明涉及人，大鼠和小鼠干细胞来源的神经元存活因子多肽（SDNSF），其制备方法，编码SDNSF的cDNA，包含cDNA的载体，载体转化的宿主细胞，针对SDNSF的抗体， 含有SDNSF或抗体的药物组合物，测定SDNSF的方法，用于测定SDNSF的试剂和使用SDNSF的筛选方法。 这些多肽在神经细胞的存活中是有效的，因此对于脑梗塞，脑出血，脊髓损伤等引起的中枢神经系统的损伤是有效的。

公开(公告)号：US09388157B2

公开(公告)日：2016-07-12

申请号：US14587829

申请日：2014-12-31

申请人： ONO PHARMACEUTICAL CO., LTD.

发明人： Tohru Kambe ,  Toru Maruyama ,  Shinsaku Yamane ,  Satoshi Nakayama ,  Kousuke Tani

IPC分类号： C07D313/00 ,  C07D313/06 ,  A61K31/4427 ,  A61K31/558 ,  C07D401/06 ,  C07D417/04 ,  C07D407/12 ,  C07D405/06

CPC分类号： A61K31/335 ,  A61K9/0048 ,  A61K31/4427 ,  A61K31/558 ,  C07D313/06 ,  C07D401/06 ,  C07D405/06 ,  C07D407/12 ,  C07D417/04

摘要： Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.

公开(公告)号：US08703816B2

公开(公告)日：2014-04-22

申请号：US13991025

申请日：2011-12-01

申请人： Masaya Kokubo ,  Koji Yano

发明人： Masaya Kokubo ,  Koji Yano

IPC分类号： A01N37/34 ,  A61K31/275 ,  A01N37/12 ,  A01N37/44 ,  A61K31/195 ,  C07C229/00 ,  A61K31/198 ,  C07C229/36

摘要： Provided is a levodopa prodrug that overcomes the problems attributed to the blood kinetics of levodopa such as large number of doses and the incidence of side effects due to frequent dosing. (2S)-2-Amino-3-(3,4-bis((2-(benzoyloxy)-2-methylpropanoyl)oxy)phenyl)propanoic acid, a salt thereof, or a solvate thereof is a levodopa prodrug, and provides a flat blood concentration-time profile of levodopa through oral administration, and therefore is useful as a preventive and/or therapeutic agent for Parkinson's disease and/or Parkinson's syndrome that overcomes the problems associated with pharmaceutical preparations of levodopa.

公开(公告)号：US07300917B2

公开(公告)日：2007-11-27

申请号：US10519106

申请日：2003-05-28

申请人： Shinji Nakade ,  Hiromu Habashita ,  Takuya Seko

发明人： Shinji Nakade ,  Hiromu Habashita ,  Takuya Seko

IPC分类号： A61K38/00 ,  C12P13/06

CPC分类号： C07D213/40 ,  A61K31/4406 ,  C07C233/51 ,  C07C233/66 ,  C07C233/73 ,  C07C233/83 ,  C07C235/48 ,  C07C235/52 ,  C07D231/12 ,  C07D235/12 ,  C07D261/14

摘要： A remedy and/or a preventive for a chronic disease which contains an EDG-2 antagonist. Because of binding to a subtype EDG-2 of LPA receptor, an EDG-2 antagonist is useful in treating and/or preventing chronic diseases (for example, diseases caused by the progress of chronic asthma, glomerular nephritis, obesity, arteriosclerosis, rheumatoid and atopic diseases) induced and made chronic by tissue cells whose proliferation is accelerated by LPA mediated by EDG-2.

摘要翻译： 含有EDG-2拮抗剂的慢性疾病的补救措施和/或预防措施。 由于与EDA-2的LPA受体的结合，EDG-2拮抗剂可用于治疗和/或预防慢性疾病（例如由慢性哮喘，肾小球肾炎，肥胖症，动脉硬化，类风湿病， 特应性疾病）由EDG-2介导的LPA加速的组织细胞诱导和慢性。

公开(公告)号：US07285552B2

公开(公告)日：2007-10-23

申请号：US10472626

申请日：2002-03-18

申请人： Hiroaki Mitsuya ,  Kenji Maeda ,  Shiro Shibayama ,  Yoshikazu Takaoka

发明人： Hiroaki Mitsuya ,  Kenji Maeda ,  Shiro Shibayama ,  Yoshikazu Takaoka

IPC分类号： A61K31/497

CPC分类号： C07D471/10 ,  A61K31/49 ,  A61K31/5377 ,  A61K45/06 ,  A61K2300/00

摘要： A pharmaceutical composition for prevention and/or treatment for HIV infection or AIDS induced by the infection which comprises, as an active ingredient, a triazaspiro[5.5]undecane derivative, a quaternary ammonium salt thereof, an N-oxide thereof, or a non-toxic salt thereof, and if necessary, it may be combined with at least one member of other agents for prevention and/or treatment for HIV infection (wherein all symbols are as defined in the specification.) The triazaspiro[5.5]undecane derivatives, the quaternary ammonium salts thereof or the N-oxides thereof, or the non-toxic salts thereof are useful in preventing and/or treating HIV infection and AIDS induced by the infection.

摘要翻译： 一种用于预防和/或治疗由感染引起的HIV感染或AIDS的药物组合物，其包含作为活性成分的三氮烯[5.5]十一烷衍生物，其季铵盐，其N-氧化物或非 - 并且如果需要，可将其与至少一种其它用于HIV感染预防和/或治疗的试剂组合（其中所有符号如本说明书中所定义）。三氮杂螺[5.5]十一烷衍生物， 其季铵盐或其N-氧化物或其无毒盐可用于预防和/或治疗感染引起的HIV感染和AIDS。