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11 条记录 (耗时 0.027 秒)

    ANTAGONIST FOR MUTATED ANDROGEN RECEPTOR
    2.
    发明公开
    ANTAGONIST FOR MUTATED ANDROGEN RECEPTOR 审中-公开
    ANTAGONISTFÜREINEN MUTIERTEN ANDROGENREZEPTOR

    公开(公告)号：EP2631233A1

    公开(公告)日：2013-08-28

    申请号：EP11834469.6

    申请日：2011-10-21

    申请人： Astellas Pharma Inc.

    发明人： IDEYAMA, Yukitaka ,  KUROMITSU, Sadao ,  FURUTANI, Takashi ,  TAKEDA, Masayoshi ,  KONAGAI, Satoshi ,  YAMADA, Tomohiro ,  TANIGUCHI, Nobuaki ,  KONDOH, Yutaka ,  HIRANO, Masaaki ,  WATANABE, Kazushi ,  SUGANE, Takashi ,  KAKEFUDA, Akio

    IPC分类号： C07D401/12 ,  A61K31/496 ,  A61K31/506 ,  A61P5/26 ,  A61P35/00 ,  C07D403/12

    CPC分类号： C07D401/02 ,  A61K31/496 ,  A61K31/506 ,  C07D401/12 ,  C07D401/14 ,  C07D403/02 ,  C07D403/12

    摘要： [Problem] An object of the present invention is to provide a novel anticancer drug which is useful for treating prostate cancer accompanying androgen receptor mutation [Means for Solution] The present inventors conducted thorough research on mutant androgen-related diseases for which the traditional anti-androgen drugs become ineffective. As a result, they found that the compound, which is an active ingredient of the pharmaceutical composition of the present invention, exhibits an inhibitory action against transcriptional activation in a human mutant androgen receptor (AR), and has an excellent antitumor action in a human prostate cancer-bearing mouse, thereby completing the present invention. Accordingly, the compound, which is an active ingredient of the pharmaceutical composition of the present invention, is useful for a series of androgen receptor-related diseases including prostate cancer.

    摘要翻译： 本发明的目的在于提供一种可用于治疗伴随雄激素受体突变的前列腺癌的新型抗癌药物。本发明人进行了关于突变型雄激素相关疾病的全面研究， 雄激素药物变得无效。 结果发现，作为本发明的药物组合物的活性成分的化合物在人类突变雄激素受体（AR）中表现出抗转录活化的抑制作用，并且在人体中具有优异的抗肿瘤作用 前列腺癌的小鼠，从而完成本发明。 因此，作为本发明的药物组合物的活性成分的化合物可用于一系列与前列腺癌有关的雄激素受体相关疾病。

    AZOLE COMPOUND
    3.
    发明公开
    AZOLE COMPOUND 有权
    AZOLVERBINDUNG

    公开(公告)号：EP2308869A1

    公开(公告)日：2011-04-13

    申请号：EP09797891.0

    申请日：2009-07-13

    申请人： Astellas Pharma Inc.

    发明人： AOKI, Satoshi ,  MUNAKATA, Ryosuke ,  KAWANO, Noriyuki ,  SAMIZU, Kiyohiro ,  OKA, Hiromasa ,  ISHII, Takahiro ,  SUGANE, Takashi

    IPC分类号： C07D401/14 ,  A61P25/04 ,  A61P43/00 ,  C07D413/14 ,  C07D417/14 ,  A61K31/4545

    CPC分类号： C07D401/14 ,  C07D413/14 ,  C07D417/14

    摘要： [Problems] A compound which is useful as an active ingredient of a pharmaceutical composition for treating neuropathic pain is provided.
    [Means for Solution] The present inventors have made extensive studies on compounds having an FAAH inhibitory activity, and as a result, have found that an azole compound substituted with an N-(pyridin-3-yl)oxycarbonyl-piperidin-4-yl group and a phenyl group or a pharmaceutically acceptable salt thereof has an excellent FAAH inhibitory activity, thereby completing the present invention.
    The compound of the present invention is confirmed to have an excellent FAAH inhibitory activity and an antiallodynic effect in rat models with neuropathic pain, and thus is useful as an agent for preventing and/or an agent for treating neuropathic pain.

    摘要翻译： [问题]提供了可用作治疗神经性疼痛的药物组合物的活性成分的化合物。 [解决方案]本发明人对具有FAAH抑制活性的化合物进行了广泛的研究，结果发现，用N-（吡啶-3-基）氧羰基 - 哌啶-4-基 基和苯基或其药学上可接受的盐具有优异的FAAH抑制活性，从而完成了本发明。 证实本发明的化合物在具有神经性疼痛的大鼠模型中具有优异的FAAH抑制活性和抗异常性疼痛作用，因此可用作预防和/或治疗神经性疼痛的药剂。

    CRYSTAL OF BENZOXADIAZOLE DERIVATIVE
    4.
    发明公开
    CRYSTAL OF BENZOXADIAZOLE DERIVATIVE 审中-公开
    苯并恶唑衍生物的晶体

    公开(公告)号：EP2042498A1

    公开(公告)日：2009-04-01

    申请号：EP07790741.8

    申请日：2007-07-13

    申请人： Astellas Pharma Inc.

    发明人： HAMADA, Noritaka ,  MIZOGUCHI, Ryo ,  SANO, Kuniyuki ,  SAKAIDA, Takaaki ,  AWAMURA, Yuji ,  IWAKAWA, Yu ,  TOBE, Takahiko ,  SUGANE, Takashi

    IPC分类号： C07D401/14 ,  A61K31/4439 ,  A61P25/18 ,  A61P25/28 ,  A61P43/00

    CPC分类号： C07D413/14

    摘要： Object
    Provided are β-form crystal, γ-form crystal, and α-form crystal of a benzoxadiazole derivative, wherein a uniform crystal having sufficient qualities can be obtained with high reproducibility, and they can be anytime supplied as crystals of drug substance for use in producing pharmaceuticals, are particularly suitable for mass synthesis in industrial production, hardly exhibit hygroscopicity and have particularly excellent photo-resistance.
    Means for Resolution
    A solving means includes β-form crystal of 4-[3-isopropyl-5-(6-phenyl-3-pyridyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole, which shows an endothermic peak at 145 to 150°C according to a differential scanning calorimeter analysis (DSC analysis) and shows X-ray powder diffraction peaks at 9.8, 11.1, 12.8, 13.3, 17.1, 20.2, 21.2 and 22.3 in 2θ(°), and the like. Selected Figure

    摘要翻译： 提供的对象为苯并恶二唑衍生物的β型晶体，γ型晶体和α型晶体，其中可以以高重复性获得具有足够品质的均匀晶体，并且它们可以随时作为药物晶体供应使用 在制造医药品时，特别适用于工业生产中的大量合成，几乎不显示吸湿性并且具有特别优异的耐光性。 解决方案的手段解决手段包括4- [3-异丙基-5-（6-苯基-3-吡啶基）-4H-1,2,4-三唑-4-基] -2,1-二甲基 - 3-苯并恶二唑根据差示扫描量热计分析（DSC分析）在145至150℃显示吸热峰，并显示在9.8,11.1,12.8,13.3,17.1,20.2,21.2和22.3处的X射线粉末衍射峰 2θ（°）等。 选定图

    CARBAMATE COMPOUND OR SALT THEREOF
    6.
    发明公开
    CARBAMATE COMPOUND OR SALT THEREOF 审中-公开
    CARBAMATVERBINDUNG ODER SALZ DAVON

    公开(公告)号：EP2351749A1

    公开(公告)日：2011-08-03

    申请号：EP09824819.8

    申请日：2009-11-05

    申请人： Astellas Pharma Inc.

    发明人： ISHII, Takahiro ,  SUGANE, Takashi ,  MUNAKATA, Ryosuke ,  AOKI, Satoshi ,  HIGAKI, Masahide ,  SOMEYA, Akiyoshi

    IPC分类号： C07D401/12 ,  A61K31/496 ,  A61P7/12 ,  A61P13/00 ,  A61P13/08 ,  A61P13/10 ,  A61P25/20 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

    CPC分类号： A61K31/496 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/04 ,  C07D417/12

    摘要： [Problems] A compound useful as an active ingredient for a pharmaceutical composition for treating FAAH-related diseases is provided.
    [Means for Solution] The present inventors have made extensive studies on compounds having an FAAH inhibitory activity, and as a result, have found that a piperazine-1-carboxylate compound, in which benzimidazol-2-ylcarbonyl, benzofuran-2-ylcarbonyl or the like binds to the 4-position of the piperazine, has an excellent FAAH inhibitory activity and further has an action to increase the effective bladder capacity, an action to ameliorate sleep disorders, an anti-diuretic action, and an analgesic activity on lower urinary tract pain including bladder pain and the like, thereby completed the present invention. The carbamate compound of the present invention has an excellent FAAH inhibitory activity and can be used as an agent for preventing and/or treating FAAH-related diseases, particularly nocturia, interstitial cystitis, painful bladder syndrome, or chronic non-bacterial prostatitis/chronic pelvic pain syndrome.

    摘要翻译： [问题]提供了用作治疗FAAH相关疾病的药物组合物的活性成分的化合物。 [解决方案]本发明人对具有FAAH抑制活性的化合物进行了广泛的研究，结果发现了哌嗪-1-羧酸酯化合物，其中苯并咪唑-2-基羰基，苯并呋喃-2-基羰基或 类似物与哌嗪的4-位结合，具有优异的FAAH抑制活性，并且还具有增加膀胱有效能力的作用，改善睡眠障碍的作用，抗利尿作用和对下尿路的止痛活性 包括膀胱疼痛等的道痛，从而完成了本发明。 本发明的氨基甲酸酯化合物具有优异的FAAH抑制活性，可用作预防和/或治疗FAAH相关疾病，特别是夜尿症，间质性膀胱炎，疼痛膀胱综合征或慢性非细菌性前列腺炎/慢性骨盆 疼痛综合征。

    PIPERAZINE DERIVATIVE
    9.
    发明公开
    PIPERAZINE DERIVATIVE 审中-公开

    公开(公告)号：EP3489231A1

    公开(公告)日：2019-05-29

    申请号：EP17830975.3

    申请日：2017-07-18

    申请人： Astellas Pharma Inc.

    发明人： SUGANE, Takashi ,  ASAI, Norio ,  MORITOMO, Hiroyuki ,  YAMASHITA, Daisuke ,  HOSOGAI, Naomi

    IPC分类号： C07D401/14 ,  A61K31/496 ,  A61P13/02 ,  A61P13/10 ,  A61P43/00 ,  C07D403/06 ,  C07D405/14

    摘要： [Problem] To provide a compound useful as an MC 4 receptor agonist. [Solution] The present inventors have made studies on MC 4 receptor agonists. As a result, it is confirmed that a piperazine derivative has an MC 4 receptor agonist activity, which leads to the accomplishment of the present invention. The piperazine derivative according to the present invention has an MC 4 receptor agonist activity, and therefore can be used as a prophylactic or therapeutic agent for disturbance of urination in bladder and urinary tract diseases, particularly underactive bladder, hypotonic bladder, acontractile bladder, detrusor underactivity, neurogenic bladder, urethral relaxation failure, detrusor-sphincter dyssynergia and prostatic hyperplasia.