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    Production method for isoquinoline derivatives and salts thereof
    3.
    发明授权
    Production method for isoquinoline derivatives and salts thereof 有权
    异喹啉衍生物及其盐的制备方法

    公开(公告)号：US09045460B2

    公开(公告)日：2015-06-02

    申请号：US13816534

    申请日：2011-08-25

    申请人： Noriaki Gomi ,  Tadaaki Ohgiya ,  Kimiyuki Shibuya

    发明人： Noriaki Gomi ,  Tadaaki Ohgiya ,  Kimiyuki Shibuya

    IPC分类号： C07D401/12 ,  C07D243/08

    CPC分类号： C07D401/12 ,  C07D243/08

    摘要： The present invention provides a method capable of industrially producing a target product, i.e., a compound represented by the aforementioned formula (I) or a salt thereof, which is useful for preventing and treating cerebrovascular disorders such as cerebral infarction, cerebral hemorrhage, subarachnoid hemorrhage, and cerebral edema, particularly for preventing and treating glaucoma, at high yield even on a large scale without imposing a negative impact on the environment. The present invention provides a method for producing a compound represented by formula (I) or a salt thereof, wherein the method comprises a step of reacting a compound represented by formula (III) or a salt thereof with a compound represented by formula (II) in the presence of at least one solvent selected from the group consisting of a nitrile solvent, an amide solvent, a sulfoxide solvent, and a urea solvent, and a base.

    摘要翻译： 本发明提供一种能够工业生产目标产物的方法，即由上述式（I）表示的化合物或其盐，其可用于预防和治疗脑梗塞，脑出血，蛛网膜下腔出血等脑血管疾病 ，脑水肿，特别是预防和治疗青光眼，即使大规模高产，也不会对环境造成负面影响。 本发明提供一种由式（I）表示的化合物或其盐的制备方法，其中所述方法包括使式（III）表示的化合物或其盐与式（II）表示的化合物反应的步骤， 在选自腈溶剂，酰胺溶剂，亚砜溶剂和尿素溶剂中的至少一种溶剂和碱存在下进行。

    NOVEL PRODUCTION METHOD FOR ISOQUINOLINE DERIVATIVES AND SALTS THEREOF
    4.
    发明申请
    NOVEL PRODUCTION METHOD FOR ISOQUINOLINE DERIVATIVES AND SALTS THEREOF 有权

    公开(公告)号：US20130144054A1

    公开(公告)日：2013-06-06

    申请号：US13816534

    申请日：2011-08-25

    申请人： Noriaki Gomi ,  Tadaaki Ohgiya ,  Kimiyuki Shibuya

    发明人： Noriaki Gomi ,  Tadaaki Ohgiya ,  Kimiyuki Shibuya

    IPC分类号： C07D401/12 ,  C07D243/08

    CPC分类号： C07D401/12 ,  C07D243/08

    摘要： The present invention provides a method capable of industrially producing a target product, i.e., a compound represented by the aforementioned formula (I) or a salt thereof, which is useful for preventing and treating cerebrovascular disorders such as cerebral infarction, cerebral hemorrhage, subarachnoid hemorrhage, and cerebral edema, particularly for preventing and treating glaucoma, at high yield even on a large scale without imposing a negative impact on the environment. The present invention provides a method for producing a compound represented by formula (I) or a salt thereof, wherein the method comprises a step of reacting a compound represented by formula (III) or a salt thereof with a compound represented by formula (II) in the presence of at least one solvent selected from the group consisting of a nitrile solvent, an amide solvent, a sulfoxide solvent, and a urea solvent, and a base.

    1,4-Dihydropyridine derivatives
    6.
    发明授权
    1,4-Dihydropyridine derivatives 失效
    1,4-二氢吡啶衍生物

    公开(公告)号：US06306853B1

    公开(公告)日：2001-10-23

    申请号：US09622086

    申请日：2000-08-10

    申请人： Shigeyuki Tasaka ,  Akira Kiue ,  Hiromasa Omori ,  Hirokazu Tanabe ,  Noriaki Gomi

    发明人： Shigeyuki Tasaka ,  Akira Kiue ,  Hiromasa Omori ,  Hirokazu Tanabe ,  Noriaki Gomi

    IPC分类号： C07D4012

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D471/04

    摘要： A 1,4-dihydropyridine derivative having the formula (I): wherein, R1 represents a substituted or unsubstituted phenyl or pyridyl group, R2 represents a C1 to C5 lower alkyl group, R3 represents a substituted or unsubstituted C1 to C8 alkyl, alkenyl, alkynyl or substituted or unsubstituted C3 to C7 cycloalkyl or cycloalkenyl group, R4 represents —A—R5, wherein A represents a C3 to C5 alkynylene group having one triple bond, and R5 represents a substituted or unsubstituted pyridyl, quinolyl, isoquinolyl or pyrimidyl group and a drug for overcoming resistance to an anti-cancer drug or a drug increasing the effect of an anti-cancer drug containing as an effective ingredient the derivative or its pharmacologically acceptable salt or hydrate.

    摘要翻译： 具有式（I）的1,4-二氢吡啶衍生物：其中，R1表示取代或未取代的苯基或吡啶基，R2表示C1至C5低级烷基，R3表示取代或未取代的C1至C8烷基，烯基， 炔基或取代或未取代的C3至C7环烷基或环烯基，R4表示-A-R5，其中A表示具有一个三键的C3至C5亚炔基，R5表示取代或未取代的吡啶基，喹啉基，异喹啉基或嘧啶基， 用于克服抗癌药物或药物的药物，其增加了含有作为有效成分的衍生物或其药理学上可接受的盐或水合物的抗癌药物的作用。

    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

    申请人： Noriaki Gomi ,  Shinji Ina ,  Kenjirou Yamana ,  Yoshio Kaneko

    发明人： Noriaki Gomi ,  Shinji Ina ,  Kenjirou Yamana ,  Yoshio Kaneko

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

    CPC分类号： C07D237/14 ,  C07D401/06 ,  C07D405/12 ,  C07D417/06

    摘要： 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.

    摘要翻译： 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。

    Pyrazolone Derivative
    8.
    发明申请
    Pyrazolone Derivative 审中-公开
    吡唑啉酮衍生物

    公开(公告)号：US20100324091A1

    公开(公告)日：2010-12-23

    申请号：US12666015

    申请日：2008-06-23

    申请人： Noriaki Gomi ,  Shinji Ina ,  Kenjirou Yamana ,  Yoshio Kaneko

    发明人： Noriaki Gomi ,  Shinji Ina ,  Kenjirou Yamana ,  Yoshio Kaneko

    IPC分类号： A61K31/454 ,  C07D231/20 ,  A61K31/4152 ,  C07D401/06 ,  A61P7/02

    CPC分类号： C07D231/20 ,  C07D231/22 ,  C07D401/06 ,  C07D405/12

    摘要： A pyrazolone derivative represented by formula (I) below: wherein R1 to R3 are the same as defined in claims; or an optical isomer, a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof is provided. The novel pyrazolone derivative according to the present invention has a PAI-1 production inhibitory activity, a tissue fibrosis inhibitory activity, and a fibrolytic activity, and is effective for preventing and/or treating tissue fibrotic diseases (lung fibrosis, kidney fibrosis, etc.) and diseases of which a pathological thrombus becomes the cause, such as ischemic cardiac diseases (cardiac infarction and angina pectoris), atrial thrombus, lung embolism, deep thrombophlebitis, disseminated intravascular clotting, ischemic brain diseases (brain infarction, brain hemorrhage), and arterial sclerosis. In addition, a pharmaceutical agent for preventing and/or treating the disease conditions or the symptoms mediated by plasminogen activator inhibitor-1, comprising the novel pyrazolone derivative according to the present invention is also provided.

    摘要翻译： 由下式（I）表示的吡唑啉酮衍生物：其中R1至R3与权利要求中所定义相同; 或光学异构体，其药学上可接受的盐，或其水合物或溶剂化物。 根据本发明的新型吡唑啉酮衍生物具有PAI-1产生抑制活性，组织纤维化抑制活性和纤维分解活性，对预防和/或治疗组织纤维化疾病（肺纤维化，肾纤维化等）有效 ）和病理性血栓成为原因的疾病，如缺血性心脏病（心肌梗死和心绞痛），心房血栓，肺栓塞，深部血栓性静脉炎，弥漫性血管内凝血，缺血性脑病（脑梗死，脑出血）等） 动脉硬化。 此外，还提供了包含根据本发明的新型吡唑啉酮衍生物的用于预防和/或治疗疾病状况或由纤溶酶原激活物抑制剂-1介导的症状的药剂。

    NOVEL SULFONAMIDE DERIVATIVE AND PHARMACEUTICAL PRODUCT CONTAINING SAME
    9.
    发明申请
    NOVEL SULFONAMIDE DERIVATIVE AND PHARMACEUTICAL PRODUCT CONTAINING SAME 审中-公开
    新型磺酰胺衍生物和含有其的药物产品

    公开(公告)号：US20120122906A1

    公开(公告)日：2012-05-17

    申请号：US13384519

    申请日：2010-08-27

    申请人： Toru Miura ,  Kazuhiro Onogi ,  Noriaki Gomi ,  Takaaki Araki ,  Junya Tagashira ,  Ryohei Sekimoto ,  Rio Ishida ,  Hitomi Aoki ,  Tadaaki Ohgiya

    发明人： Toru Miura ,  Kazuhiro Onogi ,  Noriaki Gomi ,  Takaaki Araki ,  Junya Tagashira ,  Ryohei Sekimoto ,  Rio Ishida ,  Hitomi Aoki ,  Tadaaki Ohgiya

    IPC分类号： A61K31/513 ,  A61P9/00 ,  A61P3/10 ,  A61P9/10 ,  A61P13/12 ,  A61P3/00 ,  C07D403/04 ,  A61P9/12

    CPC分类号： C07D403/04

    摘要： Disclosed is a novel compound which has both angiotensin II receptor antagonist activity and PPARγ activating activity, and is useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, angina pectoris, cerebrovascular disorders, cerebral circulatory disorders, ischemic peripheral circulatory disorders, kidney diseases, arteriosclerosis, inflammatory diseases, type 2 diabetes, diabetic complication, insulin resistant syndrome, syndrome X, metabolic syndrome and hyperinsulinemia. Also disclosed is a pharmaceutical composition which contains the novel compound. Specifically disclosed are: a sulfonamide derivative represented by general formula (I), a salt thereof, or a solvate of the derivative or salt; and a pharmaceutical composition which contains the sulfonamide derivative, a salt thereof, or a solvate of the derivative or salt. (In the formula, R1 represents a C1-6 alkyl group; R2 and R3 each represents a C1-6 alkyl group or the like; and R4 represents a hydrogen atom, a C1-6 alkyl group, a C1-6 alkanoyl group or a C3-8 cycloalkylcarbonyl group.)

    摘要翻译： 公开了具有血管紧张素II受体拮抗剂活性和PPARγ活化活性两者的新型化合物，可用作高血压，心脏病，心绞痛，脑血管障碍，脑循环障碍，缺血性外周循环障碍等的预防和/ 肾脏疾病，动脉硬化，炎性疾病，2型糖尿病，糖尿病并发症，胰岛素抵抗综合征，X综合征，代谢综合征和高胰岛素血症。 还公开了含有新化合物的药物组合物。 具体公开的是：由通式（I）表示的磺酰胺衍生物，其盐或衍生物或盐的溶剂合物; 以及含有磺酰胺衍生物，其盐或衍生物或盐的溶剂合物的药物组合物。 （式中，R1表示碳原子数1〜6的烷基，R2，R3各自表示C1-6烷基等，R4表示氢原子，C1-6烷基，C1-6烷酰基或 C3-8环烷基羰基）

    5-PHENYL-3-PYRIDAZINONE DERIVATIVE
    10.
    发明申请
    5-PHENYL-3-PYRIDAZINONE DERIVATIVE 有权
    5-苯基-3-吡啶酮衍生物

    公开(公告)号：US20100197698A1

    公开(公告)日：2010-08-05

    申请号：US12665492

    申请日：2008-06-19

    申请人： Noriaki Gomi ,  Shinji Ina ,  Kenjirou Yamana ,  Yoshio Kaneko

    发明人： Noriaki Gomi ,  Shinji Ina ,  Kenjirou Yamana ,  Yoshio Kaneko

    IPC分类号： A61K31/501 ,  C07D237/14 ,  A61K31/50 ,  C07D405/12 ,  A61P7/02

    CPC分类号： C07D237/14 ,  C07D401/06 ,  C07D405/12 ,  C07D417/06

    摘要： 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.

    摘要翻译： 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。