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    Diarylpyridazinone derivatives, preparation thereof, and use thereof for the treatment of humans
    4.
    发明授权
    Diarylpyridazinone derivatives, preparation thereof, and use thereof for the treatment of humans 有权
    二芳基哒嗪酮衍生物，其制备方法及其用于治疗人的用途

    公开(公告)号：US08993569B2

    公开(公告)日：2015-03-31

    申请号：US13823671

    申请日：2011-12-20

    Applicant: Elisabeth Dupont-Passelaigue ,  Isabelle Le Roy ,  Samuel Mialhe ,  Christophe Pignier

    Inventor： Elisabeth Dupont-Passelaigue ,  Isabelle Le Roy ,  Samuel Mialhe ,  Christophe Pignier

    IPC: A01N43/58 ,  A61K31/50 ,  C07D237/00 ,  C07D237/02 ,  C07D237/14 ,  C07D231/20

    CPC classification number: C07D237/14 ,  C07D231/20

    Abstract: The present invention relates to diarylpyridazinone derivatives that block the potassium Kv channels (specifically the Kv1.5, Kv4.3, and Kv11.1 channels) and to the use thereof for the treatment of humans. Said compounds have the general formula (I), where R1 and R2 are simultaneously or independently one or more groupings such as: halogen, such as F, Br, Cl, a straight or branched C1-C4 alkyl, hydroxy, a straight or branched C1-C4 alkoxy, arylsulfonamido, in which the aryl is optionally replaced with a straight or branched C1-C4 alkyl, or nitrile, as well as the various enantiomers and the mixtures thereof in any proportion, and the pharmaceutically acceptable salts thereof.

    Abstract translation: 本发明涉及阻断Kv通道（特别是Kv1.5，Kv4.3和K​​v11.1通道）的二芳基哒嗪酮衍生物及其用于治疗人的用途。 所述化合物具有通式（I），其中R 1和R 2同时或独立地是一个或多个基团，例如：卤素如F，Br，Cl，直链或支链C 1 -C 4烷基，羟基，直链或支链 其中芳基任选被直链或支链C 1 -C 4烷基或腈取代的芳基磺酰氨基，以及各种对映异构体及其任何比例的混合物及其药学上可接受的盐。

    4-alkoxypyridazine derivatives as fast dissociating dopamine 2 receptor antagonists
    5.
    发明授权
    4-alkoxypyridazine derivatives as fast dissociating dopamine 2 receptor antagonists 有权
    4-烷氧基哒嗪衍生物作为快速解离的多巴胺2受体拮抗剂

    公开(公告)号：US08906921B2

    公开(公告)日：2014-12-09

    申请号：US12597166

    申请日：2008-04-18

    Applicant: Gregor James MacDonald ,  José Manuel Bartolomé-Nebreda

    Inventor： Gregor James MacDonald ,  José Manuel Bartolomé-Nebreda

    IPC: A61K31/50 ,  C07D237/02

    CPC classification number: C07D401/12

    Abstract: The present invention relates to (1-benzyl-piperidin-4-yl)-(4-alkoxy-pyridazin-3-y1)-amines that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.

    Abstract translation: 本发明涉及快速解离多巴胺2受体拮抗剂的（1-苄基 - 哌啶-4-基） - （4-烷氧基 - 哒嗪-3-基） - 胺，制备这些化合物的方法，包含这些化合物的药物组合物 作为活性成分。 该化合物可用作治疗或预防中枢神经系统疾病（例如精神分裂症）的药物，通过发挥抗精神病作用而没有运动副作用。

    5-phenyl-3-pyridazinone derivative
    7.
    发明授权
    5-phenyl-3-pyridazinone derivative 有权
    5-苯基-3-哒嗪酮衍生物

    公开(公告)号：US08106053B2

    公开(公告)日：2012-01-31

    申请号：US12665492

    申请日：2008-06-19

    Applicant: Noriaki Gomi ,  Shinji Ina ,  Kenjirou Yamana ,  Yoshio Kaneko

    Inventor： Noriaki Gomi ,  Shinji Ina ,  Kenjirou Yamana ,  Yoshio Kaneko

    IPC: A61K31/50 ,  A61K31/501 ,  C07D237/02

    CPC classification number: C07D237/14 ,  C07D401/06 ,  C07D405/12 ,  C07D417/06

    Abstract: To find a compound having a tissue fibrinosis-inhibitory activity and a fibrinolytic activity, and to provide a novel compound that is useful for preventing and/or treating tissue fibrinosis diseases (pulmonary fibrosis, renal fibrosis etc.), diseases caused by pathological blood clots such as ischemic heart diseases (myocardial infarction, angina), intraatrial thrombus, pulmonary embolism, deep venous thrombosis, disseminated intravascular coagulation, ischemic cerebral diseases (cerebral infarction, cerebral bleeding) and arteriosclerosis and the like. To provide a pharmaceutical drug comprising a 5-phenyl-3-pyridazinone derivative represented by the following general formula (I): and an optical isomer thereof, or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, useful for preventing and/or treating disease conditions or symptoms mediated by plasminogen activator inhibitor-1.

    Abstract translation: 为了找到具有组织纤维蛋白沉积抑制活性和纤维蛋白溶解活性的化合物，并提供可用于预防和/或治疗组织纤维蛋白病（肺纤维化，肾纤维化等）的新型化合物，由病理性血块引起的疾病 心肌梗塞，心绞痛，心内膜血栓，肺栓塞，深静脉血栓形成，弥散性血管内凝血，缺血性脑疾病（脑梗死，脑出血），动脉硬化等。 提供一种药物，其含有下述通式（I）表示的5-苯基-3-哒嗪酮衍生物及其旋光异构体或其药学上可接受的盐或其水合物或溶剂合物，其用于预防和/ 或治疗由纤溶酶原激活物抑制剂-1介导的疾病状况或症状。

    Brain/neuronal cell-protecting agent and therapeutic agent for sleep disorder
    10.
    发明授权
    Brain/neuronal cell-protecting agent and therapeutic agent for sleep disorder 失效
    脑/神经元细胞保护剂和睡眠障碍治疗剂

    公开(公告)号：US07812025B2

    公开(公告)日：2010-10-12

    申请号：US11990385

    申请日：2006-08-11

    Applicant: Takahiro Matsumoto ,  Masakuni Kori ,  Mitsunori Kouno

    Inventor： Takahiro Matsumoto ,  Masakuni Kori ,  Mitsunori Kouno

    IPC: A61K31/501 ,  A61K31/497 ,  A61K31/44 ,  C07D237/02 ,  C07D401/06 ,  C07D403/06 ,  C07D413/06 ,  C07D241/06 ,  C07D401/02 ,  C07D213/02

    CPC classification number: C07D213/75 ,  C07D237/20 ,  C07D261/14 ,  C07D333/20 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

    Abstract: A compound represented by the formula (I) or a salt thereof; and an agent for protecting a brain/neuronal cell or a therapeutic agent for sleep disorder comprising the compound or salt: wherein Z represents an oxygen or sulfur; R1 represents an aryl or heterocyclic group which may be substituted, provided that R1 is not a 3-ethyl-6-methoxy-2-methyl-5-naphthalen-1-yl group; R1a represents a hydrogen atom, a hydrocarbon group which may be substituted, a hydroxyl group or the like; R2 represents a piperidin-1,4-diyl or piperazin-1,4-diyl which may be substituted; R3 represents a bivalent group which is formed by removing two hydrogen atoms from a benzene ring or 6-membered aromatic heterocyclic ring which may have a substituent, provided that R3 is not a pyridazin-3,6-diyl; and R4 represents a group which is formed by removing one hydrogen atom from a benzene ring or 5- to 6-membered heterocyclic ring which may be substituted, provided that the substituent on the heterocyclic ring is not a phenylethyl group which may be substituted when Z is sulfur.

    Abstract translation: 由式（I）表示的化合物或其盐; 以及用于保护脑/神经元细胞或用于睡眠障碍的治疗剂的药剂，其包含所述化合物或盐：其中Z表示氧或硫; R1表示可被取代的芳基或杂环基，条件是R 1不是3-乙基-6-甲氧基-2-甲基-5-萘-1-基; R 1a表示氢原子，可被取代的烃基，羟基等; R2代表可被取代的哌啶-1,4-二基或哌嗪-1,4-二基; R3表示通过从可以具有取代基的苯环或6元芳族杂环除去2个氢原子而形成的二价基团，条件是R 3不是哒嗪-3,6-二基; 并且R 4表示通过从可以被取代的苯环或5-至6-元杂环除去一个氢原子而形成的基团，条件是杂环上的取代基不是Z时可以被取代的苯基乙基 是硫。

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