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    PYRAZOLOPYRIDINE DERIVATIVE OR PHARMACOLOGICALLY ACCEPTABLE SALT THEREOF
    104.
    发明申请
    PYRAZOLOPYRIDINE DERIVATIVE OR PHARMACOLOGICALLY ACCEPTABLE SALT THEREOF 审中-公开
    吡唑啉衍生物或其药理学上可接受的盐

    公开(公告)号：US20130331378A1

    公开(公告)日：2013-12-12

    申请号：US13981453

    申请日：2012-01-25

    申请人： Shigeki Seto ,  Kentaro Umei ,  Yosuke Nishigaya ,  Asao Tanioka ,  Tatsuhiro Kondo ,  Atsushi Kondo ,  Kazuya Tatani ,  Naohiro Kawamura

    发明人： Shigeki Seto ,  Kentaro Umei ,  Yosuke Nishigaya ,  Asao Tanioka ,  Tatsuhiro Kondo ,  Atsushi Kondo ,  Kazuya Tatani ,  Naohiro Kawamura

    IPC分类号： C07D471/04

    CPC分类号： C07D471/04

    摘要： A pyrazolopyridine derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof exhibits a strong EP1 receptor antagonistic effect. Thus, the derivative or the pharmacologically acceptable salt is useful as a therapeutic agent for lower urinary tract symptoms (LUTS), particularly, overactive bladder syndrome (OABs), or a prophylactic agent therefor and furthermore, is also useful in the treatment, prevention, or suppression of various pathological conditions in which the EP1 receptor is involved, such as inflammatory disease, pain disease, osteoporosis, and cancer. [A is a benzene ring or the like, Y1 is C1-6 alkylene, R1 is —C(═O)—OZ1 or the like, Z1 is H or the like, R2 is a branched C3-6 alkyl group or the like, R3 is H or the like, R4 is a hydrogen atom or the like, and R5 is a hydrogen atom or the like].

    摘要翻译： 由下式（I）表示的吡唑并吡啶衍生物或其药理学上可接受的盐表现出强烈的EP1受体拮抗作用。 因此，衍生物或药理学上可接受的盐可用作下尿路症状（LUTS），特别是膀胱过度活动症（OAB）或其预防剂的治疗剂，此外，还可用于治疗，预防， 或抑制涉及EP1受体的各种病理状况，例如炎性疾病，疼痛疾病，骨质疏松症和癌症。 [A是苯环等，Y 1是C 1-6亚烷基，R 1是-C（= O）-OZ 1等，Z 1是H等，R 2是支链C 3-6烷基等 ，R3为H等，R4为氢原子等，R5为氢原子等]。

    Process for production of bicyclo[2.2.2]octylamine derivative
    105.
    发明授权
    Process for production of bicyclo[2.2.2]octylamine derivative 失效
    二环[2.2.2]辛胺衍生物的制备方法

    公开(公告)号：US08476470B2

    公开(公告)日：2013-07-02

    申请号：US13057879

    申请日：2009-08-07

    申请人： Tomohiro Akeboshi ,  Yusuke Iriyama ,  Hirotaka Kawanami

    发明人： Tomohiro Akeboshi ,  Yusuke Iriyama ,  Hirotaka Kawanami

    IPC分类号： C07C62/20

    CPC分类号： C07C229/50 ,  C07C227/16 ,  C07C227/22 ,  C07C249/02 ,  C07C251/20 ,  C07C303/28 ,  C07C309/66 ,  C07C2602/44

    摘要： The present invention herein provides a process for production of a bicyclo[2.2.2]octylamine derivative which may be used as an intermediate for preparation of medical and pharmaceutical products. The process is quite efficient and can produce the derivative in a large-scale while using mild reaction conditions.The process for producing a bicyclo[2.2.2]octylamine derivative comprises the steps of subjecting, to ring-formation, a compound represented by the following general formula (1): [wherein R1 represents an alkyl group having 1 to 6 carbon atoms, which may have a substituent; an arylmethyl group which may have a substituent; or an arylethyl group which may have a substituent], and a compound represented by the following general formula (2): R2—NH2  (2) [wherein R2 represents an alkyl group having 1 to 6 carbon atoms, which may have a substituent; an aralkyl group which may have a substituent; a hydroxyl group; an alkyloxy group having 1 to 6 carbon atoms, which may have a substituent; or an aralkyloxy group which may have a substituent], and then reducing the resulting product.

    摘要翻译： 本发明提供了可用作制备医药产品的中间体的双环[2.2.2]辛胺衍生物的制备方法。 该方法是非常有效的，并且可以在使用温和的反应条件的情况下大量产生衍生物。 制备双环[2.2.2]辛胺衍生物的方法包括以下步骤：使由下列通式（1）表示的化合物进行成环：其中R 1表示具有1至6个碳原子的烷基， 其可以具有取代基; 可以具有取代基的芳基甲基; 或可以具有取代基的芳基乙基）和由以下通式（2）表示的化合物：R2-NH2（2）[其中R2表示可以具有取代基的碳原子数1〜6的烷基] 可以具有取代基的芳烷基; 羟基; 可以具有取代基的碳原子数1〜6的烷氧基; 或可具有取代基的芳烷氧基），然后还原所得产物。

    Phosphodiesterase 10A inhibitor
    106.
    发明授权
    Phosphodiesterase 10A inhibitor 有权
    磷酸二酯酶10A抑制剂

    公开(公告)号：US08404710B2

    公开(公告)日：2013-03-26

    申请号：US12913094

    申请日：2010-10-27

    申请人： Michiaki Nagasawa ,  Simon John Mackenzie

    发明人： Michiaki Nagasawa ,  Simon John Mackenzie

    IPC分类号： A61K31/437 ,  A61P25/16

    CPC分类号： A61K31/437

    摘要： A phosphodiesterase 10A inhibitor serving as an effective prophylactic or therapeutic agent for Parkinson's disease, Huntington's disease, Alzheimer's disease, and schizophrenia.The PDE10A inhibitor contains as an active ingredient a pyrazolo[1,5-a]pyridine derivative represented by the following general formula: wherein R1 and R2 are each independently a hydrogen atom or a lower alkyl group having 1 to 4 carbons; and R3 is a hydrogen atom, a lower alkyl group having 1 to 4 carbons, or a lower alkoxyl group having 1 to 3 carbons.

    摘要翻译： 用作帕金森病，亨廷顿病，阿尔茨海默氏病和精神分裂症的有效预防或治疗剂的磷酸二酯酶10A抑制剂。 PDE10A抑制剂含有作为活性成分的由以下通式表示的吡唑并[1,5-a]吡啶衍生物：其中R 1和R 2各自独立地为氢原子或具有1至4个碳的低级烷基; R3为氢原子，碳原子数1〜4的低级烷基或碳原子数1〜3的低级烷氧基。

    Oral sustained-release tablet
    107.
    发明授权
    Oral sustained-release tablet 失效
    口服缓释片

    公开(公告)号：US08343544B2

    公开(公告)日：2013-01-01

    申请号：US12855226

    申请日：2010-08-12

    申请人： Ryouichi Hoshino ,  Katashi Nakashima ,  Kazuo Kazama

    发明人： Ryouichi Hoshino ,  Katashi Nakashima ,  Kazuo Kazama

    IPC分类号： A61K9/22

    CPC分类号： A61K9/2054 ,  A61K31/4174

    摘要： (Object) An oral sustained-release tablet is provided, which does not cause initial rapid increases in the bloodlevels of 4-(2-methyl-1-imidazolyl)-2,2-diphenylbutylamide (KRP-197) and can maintain constant the blood levels.(Solving means) An oral sustained-release tablet comprises a pharmaceutical composition and a gel-forming material, the pharmaceutical composition containing KRP-197 as an active ingredient.

    摘要翻译： （对象）提供口服持续释放片剂，其不会引起4-（2-甲基-1-咪唑基）-2,2-二苯基丁基酰胺（KRP-197）的血液水平的初始快速增加，并且可以保持恒定 血液水平。 （解决方案）口服缓释片剂包含药物组合物和凝胶形成材料，所述药物组合物含有KRP-197作为活性成分。

    Method for treating an inflammatory bowel disease using 2-amino-2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl-1,3-propanediol or a salt thereof
    108.
    发明授权
    Method for treating an inflammatory bowel disease using 2-amino-2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl-1,3-propanediol or a salt thereof 有权
    使用2-氨基-2- [4-（3-苄氧基苯硫基）-2-氯苯基]乙基-1,3-丙二醇或其盐治疗炎症性肠病的方法

    公开(公告)号：US08318811B2

    公开(公告)日：2012-11-27

    申请号：US12223584

    申请日：2007-02-05

    申请人： Ryotaro Kojima ,  Koichi Nakamaru ,  Tokutarou Yasue

    发明人： Ryotaro Kojima ,  Koichi Nakamaru ,  Tokutarou Yasue

    IPC分类号： A61K31/137

    CPC分类号： A61K31/137 ,  A61K45/06

    摘要： A novel therapeutic and prophylactic agent for inflammatory bowel diseases and a method for treating inflammatory bowel diseases is provided. The agent comprises a 2-amino-1,3-propanediol derivative (e.g., 2-amino-2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl-1,3-propanediol hydrochloride) represented by the chemical formula (1) or a pharmaceutically acceptable salt or hydrate thereof: The agent is useful in the treatment or prevention of Crohn's disease, Crohn's disease in large intestine, intestinal Behcet's disease, ulcerative colitis, bleeding rectal ulcer and pouchitis.

    摘要翻译： 提供了一种新型的炎症性肠病治疗和预防剂及其治疗炎症性肠病的方法。 该试剂包括由化学式表示的2-氨基-1,3-丙二醇衍生物（例如2-氨基-2- [4-（3-苄氧基苯硫基）-2-氯苯基]乙基-1,3-丙二醇盐酸盐） （1）或其药学上可接受的盐或水合物：该试剂可用于治疗或预防克罗恩病，大肠克罗恩病，肠内切塞特氏病，溃疡性结肠炎，直肠溃疡出血和肠炎。

    Amino phosphate derivative and S1P receptor modulator having same as an active ingredient
    110.
    发明授权
    Amino phosphate derivative and S1P receptor modulator having same as an active ingredient 有权
    具有与活性成分相同的氨基磷酸酯衍生物和S1P受体调节剂

    公开(公告)号：US08232319B2

    公开(公告)日：2012-07-31

    申请号：US12310007

    申请日：2007-08-07

    申请人： Yasushi Kohno ,  Kiyoshi Fujii ,  Tatsuhiro Saito

    发明人： Yasushi Kohno ,  Kiyoshi Fujii ,  Tatsuhiro Saito

    IPC分类号： A61K31/185 ,  C07F9/28

    CPC分类号： C07F9/091

    摘要： To provide an amino phosphate derivative having an excellent sphingosine-1-phosphate (S1P) receptor modulatory action.As a result of continued intensive research to create a highly safe compound which has an S1P receptor modulatory action, is has been discovered that an amino phosphate derivative represented by the following general formula (1), has a strong S1P receptor modulatory action.

    摘要翻译： 提供具有优异的鞘氨醇-1-磷酸（S1P）受体调节作用的氨基磷酸酯衍生物。 作为继续深入研究以产生具有S1P受体调节作用的高度安全的化合物的结果，已经发现由以下通式（1）表示的氨基磷酸酯衍生物具有强的S1P受体调节作用。