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    THERAPEUTIC AGENT FOR FOOD COMPETENCE DISORDER IN STOMACH
    3.
    发明申请
    THERAPEUTIC AGENT FOR FOOD COMPETENCE DISORDER IN STOMACH 审中-公开

    公开(公告)号：US20200375954A1

    公开(公告)日：2020-12-03

    申请号：US16998637

    申请日：2020-08-20

    申请人： ZERIA PHARMACEUTICAL CO., LTD.

    发明人： Yugo MATSUNAGA ,  Shigeru UEKI ,  Hiroki KATO ,  Shiro KOBAYASHI

    IPC分类号： A61K31/426 ,  C07D277/56 ,  C07D307/68

    摘要： A therapeutic agent for impaired gastric accommodation which contains as an active ingredient a compound represented by the general formula (1): (wherein R1 represents a hydrogen atom, a hydroxyl group or a halogen atom; A represents a furyl group, a thienyl group, a thiazolyl group or an oxazolyl group; R2 and R3 each represents an alkyl group with 1 to 5 carbon atoms; and n represents an integer of 2 to 4), or an acid addition salt thereof.Use of a therapeutic agent of the present invention greatly alleviates symptoms caused by said disorders, such as early satiety and bloating, because it improves relaxation of gastric fundus and impaired gastric accommodation.

    ENTERIC COATED TABLET
    4.
    发明申请
    ENTERIC COATED TABLET 审中-公开
    ENTERIC涂层片

    公开(公告)号：US20150374632A1

    公开(公告)日：2015-12-31

    申请号：US14769660

    申请日：2014-02-21

    申请人： ZERIA PHARMACEUTICAL CO., LTD.

    发明人： Akio RYU ,  Miyako OSADA

    IPC分类号： A61K9/28 ,  A61K31/606

    CPC分类号： A61K9/2846 ,  A61K9/2866 ,  A61K9/2886 ,  A61K31/606

    摘要： To provide an enteric coated tablet containing a large amount of medicinal ingredient and having sufficient impact resistance, without forming a thick enteric coating layer.The enteric coated tablet contains (A) a core tablet containing a medicinal ingredient and having a weight of 1,000 mg or more; (B) a coating layer containing a water-soluble polymer applied onto the surface of the core tablet; and (C) an enteric coating layer dissolving at pH 7 or higher which is applied onto the surface of the coating layer containing a water-soluble polymer, wherein the sum of the polymer amount of the coating layer (B) and the polymer amount of the coating layer (C) is 10 to 18 mg/cm2, the polymer amount of the coating layer (B) is 6 to 12 mg/cm2, and the polymer amount of the coating layer (C) is 3 to 6 mg/cm2.

    摘要翻译： 提供含有大量药用成分并具有足够抗冲击性的肠溶衣片剂，而不形成厚的肠溶衣层。 肠溶片剂含有（A）含有药物成分并具有1,000mg以上重量的核心片剂; （B）涂布在芯片表面上的水溶性聚合物的涂层; 和（C）溶解在pH7以上的肠溶衣层，其被涂布在含有水溶性聚合物的被覆层的表面上，其中，涂布层（B）的聚合物量与聚合物的量 涂层（C）的涂布层（C）为10〜18mg / cm 2，涂层（B）的聚合物量为6〜12mg / cm 2，涂层（C）的聚合物量为3〜6mg / cm 2 。

    Carbazole derivative, solvate thereof, or pharmaceutically acceptable salt thereof
    5.
    发明申请
    Carbazole derivative, solvate thereof, or pharmaceutically acceptable salt thereof 有权
    咔唑衍生物，其溶剂化物或其药学上可接受的盐

    公开(公告)号：US20100286210A1

    公开(公告)日：2010-11-11

    申请号：US11666631

    申请日：2005-10-28

    申请人： Masakazu Murata ,  Yoshihiko Itokazu ,  Ryu Nakao

    发明人： Masakazu Murata ,  Yoshihiko Itokazu ,  Ryu Nakao

    IPC分类号： A61K31/4439 ,  A61K31/427 ,  A61K31/422 ,  C07D413/14 ,  C07D417/12 ,  C07D413/12 ,  A61P29/00 ,  A61P3/04 ,  A61P3/10 ,  A61P3/06 ,  A61P9/12 ,  A61P1/16 ,  A61P3/00

    CPC分类号： C07D413/12 ,  C07D413/14 ,  C07D417/12

    摘要： An object of the present invention is to provide novel carbazole derivatives, solvates thereof, or pharmaceutically acceptable salts thereof having an excellent adipose tissue weight reducing effect, hypoglycemic effect, and hypolipidemic effect, which are useful as a preventive and/or therapeutic agent for fatty liver, obesity, lipid metabolism abnormality, visceral adiposity, diabetes, hyperlipemia, impaired glucose tolerance, hypertension, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, and the like.The above-mentioned object can be achieved by carbazole derivatives, solvates thereof, or pharmaceutically acceptable salts thereof, wherein the carbazole derivatives are represented by the following general formula (I): (In the formula (I), the ring A represents phenyl group or the like; X represents —O— or the like; Y represents ═N— or the like; a and b represent methylene group or the like; both V and Z represent —O— or the like; W represents a C1-C10 alkylene group whose 1 or 2 hydrogen atoms may be substituted by a phenyl group or a C1-C6 alkyl group; 1,2-phenylene group; 1,3-cyclohexyl group; or the like; R1 represents methyl group or the like; R2 represents methoxy group or the like; and R3 represents carboxy group or the like.)

    摘要翻译： 本发明的目的是提供具有优异的脂肪组织减重作用，降血糖作用和降血脂作用的新型咔唑衍生物，溶剂合物或其药学上可接受的盐，其可用作脂肪的预防和/或治疗剂 肝脏，肥胖症，脂质代谢异常，内脏肥胖，糖尿病，高脂血症，葡萄糖耐量降低，高血压，非酒精性脂肪性肝病，非酒精性脂肪性肝炎等。 上述目的可以通过其咔唑衍生物，溶剂化物或其药学上可接受的盐来实现，其中咔唑衍生物由以下通式（I）表示：（式（I）中，环A表示苯基 X表示-O-等; Y表示= N-等; a和b表示亚甲基等; V和Z均表示-O-等; W表示C1-C10 其1或2个氢原子可被苯基或C1-C6烷基取代的亚烷基; 1,2-亚苯基; 1,3-环己基;等; R1代表甲基等; R2 表示甲氧基等; R3表示羧基等。）

    THERAPEUTIC AGENT FOR FOOD COMPETENCE DISORDER IN STOMACH
    6.
    发明申请
    THERAPEUTIC AGENT FOR FOOD COMPETENCE DISORDER IN STOMACH 审中-公开
    食品中的食物不良症状的治疗药物

    公开(公告)号：US20090156652A1

    公开(公告)日：2009-06-18

    申请号：US12372234

    申请日：2009-02-17

    申请人： Yugo Matsunaga ,  Shigeru Ueki ,  Hiroki Kato ,  Shiro Kobayashi

    发明人： Yugo Matsunaga ,  Shigeru Ueki ,  Hiroki Kato ,  Shiro Kobayashi

    IPC分类号： A61K31/426 ,  A61K31/341 ,  A61P1/04

    CPC分类号： A61K31/426 ,  C07D277/56 ,  C07D307/68

    摘要： A therapeutic agent for impaired gastric accommodation which contains as an active ingredient a compound represented by the general formula (1): (wherein R1 represents a hydrogen atom, a hydroxyl group or a halogen atom; A represents a furyl group, a thienyl group, a thiazolyl group or an oxazolyl group; R2 and R3 each represents an alkyl group with 1 to 5 carbon atoms; and n represents an integer of 2 to 4), or an acid addition salt thereof.Use of a therapeutic agent of the present invention greatly alleviates symptoms caused by said disorders, such as early satiety and bloating, because it improves relaxation of gastric fundus and impaired gastric accommodation.

    摘要翻译： 含有作为活性成分的通式（1）表示的化合物作为活性成分的治疗剂：其中，R1表示氢原子，羟基或卤素原子，A表示呋喃基，噻吩基， 噻唑基或恶唑基; R2和R3各自表示碳原子数1〜5的烷基，n表示2〜4的整数）或其酸加成盐。 使用本发明的治疗剂可以大大减轻所述疾病引起的症状，如早期饱腹感和腹胀，因为这改善了胃底松弛和胃容易受损。

    Substituted benzoylaminothiazole derivatives and drugs containing the same
    7.
    发明授权
    Substituted benzoylaminothiazole derivatives and drugs containing the same 有权
    取代苯甲酰氨基噻唑衍生物和含有它们的药物

    公开(公告)号：US6121301A

    公开(公告)日：2000-09-19

    申请号：US284477

    申请日：1999-04-21

    申请人： Masaaki Nagasawa ,  Kenji Sato ,  Tadashi Kurimoto ,  Shigeru Ueki

    发明人： Masaaki Nagasawa ,  Kenji Sato ,  Tadashi Kurimoto ,  Shigeru Ueki

    IPC分类号： C07D277/46 ,  C07D277/56 ,  C07D417/12 ,  A61K31/425

    CPC分类号： C07D417/12 ,  C07D277/46 ,  C07D277/56

    摘要： The present invention relates to a substituted benzoylaminothiazole derivative represented by the following formula (I): ##STR1## wherein X represents an imino group which may be substituted by a lower alkyl group, or an oxygen atom, R.sup.1 represents a cyano group, a lower alkoxycarbonyl group, a lower alkoxycarbonylamino group, a lower alkylsulfonylamino group, a lower alkanoyl or lower alkylsulfonyl group which may be substituted by a halogen atom, a 1-ureido group, a halo-substituted lower alkyl group or a 2-pyrrolylimino group, R.sup.2 and R.sup.3 are the same or different and each independently represents a hydrogen atom or a lower alkyl group and m stands for an integer of 2 to 4, or a salt thereof; and a medicament comprising the compound as an effective ingredient. The compound of the invention is useful as a preventive and therapeutic agent for epigastric dyscomfort, nausea, vomiting, heartburn, anorexia, bellyache, abdominal flatulence, chronic gastritis or the like.

    摘要翻译： PCT No.PCT / JP97 / 03774 Sec。 371 1999年4月21日第 102（e）1999年4月21日PCT PCT 1997年10月20日PCT公布。 公开号WO98 / 17654 日期：1998年04月30日本发明涉及由下式（I）表示的取代苯甲酰氨基噻唑衍生物：其中X表示可被低级烷基或氧原子取代的亚氨基，R 1表示氰基， 低级烷氧基羰基，低级烷氧基羰基氨基，低级烷基磺酰基氨基，可被卤素原子取代的低级烷酰基或低级烷基磺酰基，1-脲基，卤代低级烷基或2-吡咯基咪唑基 ，R2和R3相同或不同，各自独立地表示氢原子或低级烷基，m表示2〜4的整数，或其盐; 以及包含该化合物作为有效成分的药物。 本发明的化合物可用作上腹部不适，恶心，呕吐，胃灼热，厌食，腹痛，腹胀气，慢性胃炎等的预防和治疗剂。

    Indole derivative for treating overproduction of dihydrotestosterone
    8.
    发明授权
    Indole derivative for treating overproduction of dihydrotestosterone 失效
    用于治疗二氢睾酮过量产生的吲哚衍生物

    公开(公告)号：US5760040A

    公开(公告)日：1998-06-02

    申请号：US714079

    申请日：1997-05-05

    申请人： Kiyoshi Yoshida ,  Tadashi Kurimoto ,  Mineo Takei ,  Hiroki Sato

    发明人： Kiyoshi Yoshida ,  Tadashi Kurimoto ,  Mineo Takei ,  Hiroki Sato

    IPC分类号： C07D209/12 ,  A61K31/405 ,  A61K31/495 ,  C07D403/10

    CPC分类号： C07D209/12

    摘要： The present invention relates to an indole derivative represented by formula (1) or a salt thereof, and a pharmaceutical containing the derivative or the salt: ##STR1## wherein R.sup.1 represents lower alkyl; R.sup.2 represents hydrogen or phenyl which may be substituted by at least one lower alkyl, lower alkoxy or a halogen atom; R.sup.3 represents hydrogen, lower alkyl, lower alkoxy, or phenylalkyloxy which may be substituted by halogen or lower alkyl; R.sup.4 represents hydrogen, lower alkyl or lower alkoxy; R.sup.5 represents hydrogen or lower alkyl; and n represents an integer of 1 to 5. This compound has the effects of both blocking .alpha..sub.1 -adrenergic receptors and inhibiting testosterone 5.alpha.-reductases, and is useful as a remedy and/or a preventive for diseases caused by dihydrotestosterone overproduction, such as prostatic hypertrophy, and diseases accompanying the same, such as urination disorder, male pattern alopecia, acne, and so forth.

    摘要翻译： PCT No.PCT / JP95 / 00599 Sec。 371日期：1997年5月5日 102（e）日期1997年5月5日PCT提交1995年3月29日PCT公布。 第WO95 / 26955号公报 日期：1995年10月12日本发明涉及式（1）表示的吲哚衍生物或其盐，以及含有该衍生物或其盐的药物：其中R1表示低级烷基; R2代表氢或可被至少一个低级烷基，低级烷氧基或卤原子取代的苯基; R 3表示可被卤素或低级烷基取代的氢，低级烷基，低级烷氧基或苯基烷氧基; R4代表氢，低级烷基或低级烷氧基; R5代表氢或低级烷基; 并且n表示1至5的整数。该化合物具有阻断α1-肾上腺素能受体和抑制睾酮5α-还原酶的作用，并且可用作二氢睾酮过量产生引起的疾病的补救和/或预防，例如 作为前列腺肥大，以及伴随的疾病，例如排尿障碍，男性脱发，痤疮等。