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11 条记录 (耗时 0.025 秒)

    BICYCLIC PYRIDINE COMPOUND
    1.
    发明公开
    BICYCLIC PYRIDINE COMPOUND 审中-公开
    双环吡啶化合物

    公开(公告)号：EP3269721A1

    公开(公告)日：2018-01-17

    申请号：EP15884684.0

    申请日：2015-11-27

    申请人： Astellas Pharma Inc. ,  Kotobuki Pharmaceutical Co., Ltd.

    发明人： KAWAGUCHI, Kenichi ,  ISHIHATA, Akihiro ,  KANAI, Akira ,  INAGAKI, Yusuke ,  HIRAMOTO, Masashi ,  ENJO, Kentaro ,  TAKAMATSU, Hajime

    IPC分类号： C07D491/048 ,  A61K31/4355 ,  A61K31/4365 ,  A61P13/02 ,  C07D495/04

    CPC分类号： C07D491/048 ,  A61K31/4355 ,  A61K31/4365 ,  C07D495/04

    摘要： The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia.
    The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-(bi-cyclic pyridylmethyl)-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.

    摘要翻译： 本发明要解决的问题是提供适用于药物组合物的化合物，特别是用于治疗夜尿症的药物组合物。 本发明人假定，胎盘亮氨酸氨肽酶（P-LAP），即氨肽酶的夜间活动的抑制裂解AVP，将维持和/或增加内源AVP水平，以提高抗利尿作用，这将有助于一个数的夜间减少 并且已经广泛研究了抑制P-LAP的化合物。 结果发现，（2R）-3-氨基-2-（双环吡啶基甲基）-2-羟基 - 丙酸衍生物具有优异的P-LAP抑制活性。 本发明人已经评估了水负荷大鼠的抗利尿作用，并且发现这些化合物通过抑制P-LAP而增加内源性AVP水平并因此减少尿量。 因此，本发明提供了预期用作基于P-LAP抑制剂治疗夜尿症的药剂的化合物。

    PYRIDINE DERIVATIVES
    4.
    发明公开
    PYRIDINE DERIVATIVES 有权
    吡啶衍生物

    公开(公告)号：EP3228616A1

    公开(公告)日：2017-10-11

    申请号：EP15865019.2

    申请日：2015-12-04

    申请人： Astellas Pharma Inc. ,  Kotobuki Pharmaceutical Co., Ltd.

    发明人： KAWAGUCHI, Kenichi ,  ISHIHATA, Akihiro ,  KANAI, Akira ,  TSUCHIYA, Kazuyuki ,  INAGAKI, Yusuke ,  KAZAMI, Junichi ,  MORIKAWA, Hiroshi ,  HIRAMOTO, Masashi ,  ENJO, Kentaro ,  TAKAMATSU, Hajime

    IPC分类号： C07D213/55 ,  A61K31/435 ,  A61K31/438 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/4433 ,  A61K31/444 ,  A61K31/472 ,  A61K31/4747 ,  A61P13/00 ,  A61P43/00 ,  C07D213/63 ,  C07D217/16 ,  C07D221/04 ,  C07D221/20 ,  C07D401/04 ,  C07D405/04

    摘要： The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically an agent for treating nocturia.
    The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-(pyridylmethyl)-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.

    摘要翻译： 本发明要解决的问题是提供适用于药物组合物的化合物，特别是用于治疗夜尿症的药剂。 本发明人假定，胎盘亮氨酸氨肽酶（P-LAP），即氨肽酶的夜间活动的抑制裂解AVP，将维持和/或增加内源AVP水平，以提高抗利尿作用，这将有助于一个数的夜间减少 并且已经广泛研究了抑制P-LAP的化合物。 结果，发明人发现（2R）-3-氨基-2-（吡啶基甲基）-2-羟基 - 丙酸衍生物具有优异的P-LAP抑制活性。 本发明人已经评估了水负荷大鼠的抗利尿作用，并且发现这些化合物通过抑制P-LAP而增加内源性AVP水平并因此减少尿量。 因此，本发明提供了预期用作基于P-LAP抑制剂治疗夜尿症的药剂的化合物。

    PYRIDINE DERIVATIVE
    5.
    发明公开
    PYRIDINE DERIVATIVE 审中-公开
    PYRIDINDERIVAT

    公开(公告)号：EP3150581A1

    公开(公告)日：2017-04-05

    申请号：EP15799163.9

    申请日：2015-05-28

    申请人： Astellas Pharma Inc. ,  Kotobuki Pharmaceutical Co., Ltd.

    发明人： KAWAGUCHI, Kenichi ,  ISHIHATA, Akihiro ,  INAGAKI, Yusuke ,  TSUCHIYA, Kazuyuki ,  HANADATE, Tadaatsu ,  KANAI, Akira ,  KAIZAWA, Hiroyuki ,  KAZAMI, Junichi ,  MORIKAWA, Hiroshi ,  HIRAMOTO, Masashi ,  ENJO, Kentaro ,  TAKAMATSU, Hajime

    IPC分类号： C07D213/68 ,  A61K31/4355 ,  A61K31/436 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61P13/00 ,  A61P43/00 ,  C07D213/70 ,  C07D213/74 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D407/06

    摘要： The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia.
    The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP.
    As a result, the inventors have found that (2R)-3-amino-2-{[4-(substituted pyridine)-2-yl]methyl}-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.

    摘要翻译： 本发明要解决的问题是提供一种适用于药物组合物的化合物，特别是用于治疗夜尿症的药物组合物。 本发明人已经假设抑制胎盘亮氨酸氨基肽酶（P-LAP）的夜间活性，即切割AVP的氨基肽酶将维持和/或增加内源性AVP水平以增强抗利尿作用，这将有助于减少数量的夜间 空洞，并广泛研究抑制P-LAP的化合物。 结果发现，（2R）-3-氨基-2 - {[4-（取代的吡啶）-2-基]甲基} -2-羟基 - 丙酸衍生物具有优异的P-LAP抑制活性。 本发明人评估了耐水大鼠的抗利尿作用，发现该化合物通过抑制P-LAP而增加内源性AVP水平，从而减少尿液产生。 因此，本发明提供预期用作基于P-LAP抑制治疗夜尿症的药剂的化合物。

    2-ACYLAMINOTHIAZOLE DERIVATIVE OR SALT THEREOF
    7.
    发明公开
    2-ACYLAMINOTHIAZOLE DERIVATIVE OR SALT THEREOF 审中-公开
    2-乙酰胺基噻唑衍生物或其盐

    公开(公告)号：EP3153511A1

    公开(公告)日：2017-04-12

    申请号：EP15803484.3

    申请日：2015-06-05

    申请人： Astellas Pharma Inc.

    发明人： TAKAHASHI, Taisuke ,  KOIKE, Takanori ,  NEGORO, Kenji ,  TANAKA, Hiroaki ,  MAEDA, Jun ,  YOKOYAMA, Kazuhiro ,  TAKAMATSU, Hajime

    IPC分类号： C07D417/14 ,  A61K31/497 ,  A61P13/02 ,  A61P13/10 ,  A61P43/00

    CPC分类号： C07D417/14 ,  A61K31/497

    摘要： To provide a compound useful as an active ingredient of a pharmacological composition for the treatment of urinary storage symptoms, dysuria, lower urinary tract diseases, and the like. [Solution] The inventors perfected the present invention after discovering that thiazole derivatives substituted at position 2 by pyrazinylcarbonylamino are exceptional muscarinic M 3 receptor positive allosteric modulators and can be expected to serve as agents for the prevention or treatment of urinary bladder and urinary tract diseases involving bladder contraction mediated by muscarinic M 3 receptors. The 2-acylaminothiazole derivatives or salts thereof of the present invention can be expected to serve as agents for the prevention or treatment of urinary bladder and urinary tract diseases involving bladder contraction mediated by muscarinic M 3 receptors, e.g., underactive bladder and the like.

    摘要翻译： 提供用作治疗尿液贮存症状，排尿困难，下尿路疾病等的药物组合物的有效成分的化合物。 [发明]在发现吡嗪酰基羰基氨基在2位取代的噻唑衍生物为例外的毒蕈碱M3受体正变构调节剂之后，本发明人完善了本发明，并且可以预期作为用于预防或治疗涉及膀胱的膀胱和尿道疾病的药剂 由毒蕈碱M3受体介导的收缩。 预期本发明的2-酰氨基噻唑衍生物或其盐可用作预防或治疗涉及由毒蕈碱M3受体介导的膀胱收缩的膀胱和尿道疾病的药剂，例如膀胱过度活动等。

    2-AMINOTHIAZOLE DERIVATIVE OR SALT THEREOF
    10.
    发明公开
    2-AMINOTHIAZOLE DERIVATIVE OR SALT THEREOF 审中-公开
    2-氨基噻唑衍生物或其盐

    公开(公告)号：EP3196200A1

    公开(公告)日：2017-07-26

    申请号：EP15836701.1

    申请日：2015-08-25

    申请人： Astellas Pharma Inc.

    发明人： TAKAHASHI, Taisuke ,  TANAKA, Hiroaki ,  AKAIWA, Michinori ,  NEGORO, Kenji ,  MIHARA, Hisashi ,  FUJI, Hideyoshi ,  TAKAMATSU, Hajime

    IPC分类号： C07D417/14 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/506 ,  A61P13/02 ,  A61P13/10 ,  A61P43/00 ,  C07D417/12

    CPC分类号： A61K31/496 ,  A61K31/4439 ,  A61K31/506 ,  C07D417/12 ,  C07D417/14

    摘要： [Problem] To provide a compound useful as an active ingredient in a pharmaceutical composition for treating bladder storage disorders, dysuria, lower urinary tract diseases, and the like. [Solution] The inventors of the present invention have discovered that a 2-aminothiazole derivative exhibits an excellent muscarinic M 3 receptor positive allosteric modulator activity, and has potential as a preventative or therapeutic agent against bladder and urinary tract diseases to which bladder contraction mediated by muscarinic M 3 receptors contributes. The 2-aminothiazole derivative or salt thereof has potential as a preventative or therapeutic agent against bladder and urinary tract diseases such as, for example, dysuria including underactive bladder, and to which bladder contraction mediated by muscarinic M 3 receptors contributes.

    摘要翻译： 本发明提供可用作治疗膀胱储存障碍，排尿困难，下尿路疾病等的药物组合物中有效成分的化合物。 本发明的发明人发现2-氨基噻唑衍生物表现出优异的毒蕈碱M3受体正变构调节剂活性，并且具有作为预防或治疗药物的潜力，所述药物用于预防由毒蕈碱介导的膀胱收缩的膀胱和尿道疾病 M3受体有助于。 该2-氨基噻唑衍生物或其盐具有作为预防或治疗膀胱和尿道疾病的潜力，例如排尿困难包括膀胱过度活动，并且由毒蕈碱M3受体介导的膀胱收缩有助于该膀胱和尿道疾病。