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    PYRAZOLOPYRIDINE DERIVATIVE OR PHARMACOLOGICALLY ACCEPTABLE SALT THEREOF
    2.
    发明申请
    PYRAZOLOPYRIDINE DERIVATIVE OR PHARMACOLOGICALLY ACCEPTABLE SALT THEREOF 审中-公开
    吡唑啉衍生物或其药理学上可接受的盐

    公开(公告)号：US20130331378A1

    公开(公告)日：2013-12-12

    申请号：US13981453

    申请日：2012-01-25

    申请人： Shigeki Seto ,  Kentaro Umei ,  Yosuke Nishigaya ,  Asao Tanioka ,  Tatsuhiro Kondo ,  Atsushi Kondo ,  Kazuya Tatani ,  Naohiro Kawamura

    发明人： Shigeki Seto ,  Kentaro Umei ,  Yosuke Nishigaya ,  Asao Tanioka ,  Tatsuhiro Kondo ,  Atsushi Kondo ,  Kazuya Tatani ,  Naohiro Kawamura

    IPC分类号： C07D471/04

    CPC分类号： C07D471/04

    摘要： A pyrazolopyridine derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof exhibits a strong EP1 receptor antagonistic effect. Thus, the derivative or the pharmacologically acceptable salt is useful as a therapeutic agent for lower urinary tract symptoms (LUTS), particularly, overactive bladder syndrome (OABs), or a prophylactic agent therefor and furthermore, is also useful in the treatment, prevention, or suppression of various pathological conditions in which the EP1 receptor is involved, such as inflammatory disease, pain disease, osteoporosis, and cancer. [A is a benzene ring or the like, Y1 is C1-6 alkylene, R1 is —C(═O)—OZ1 or the like, Z1 is H or the like, R2 is a branched C3-6 alkyl group or the like, R3 is H or the like, R4 is a hydrogen atom or the like, and R5 is a hydrogen atom or the like].

    摘要翻译： 由下式（I）表示的吡唑并吡啶衍生物或其药理学上可接受的盐表现出强烈的EP1受体拮抗作用。 因此，衍生物或药理学上可接受的盐可用作下尿路症状（LUTS），特别是膀胱过度活动症（OAB）或其预防剂的治疗剂，此外，还可用于治疗，预防， 或抑制涉及EP1受体的各种病理状况，例如炎性疾病，疼痛疾病，骨质疏松症和癌症。 [A是苯环等，Y 1是C 1-6亚烷基，R 1是-C（= O）-OZ 1等，Z 1是H等，R 2是支链C 3-6烷基等 ，R3为H等，R4为氢原子等，R5为氢原子等]。

    Glucopyranosyloxybenzylbenzene derivatives and medicinal use thereof
    3.
    发明授权
    Glucopyranosyloxybenzylbenzene derivatives and medicinal use thereof 有权
    吡喃葡萄糖氧基苄基苯衍生物及其医药用途

    公开(公告)号：US07541341B2

    公开(公告)日：2009-06-02

    申请号：US10467823

    申请日：2002-02-13

    申请人： Nobuhiko Fushimi ,  Kazuya Tatani ,  Hideki Fujikura ,  Toshihiro Nishimura ,  Minoru Fujioka ,  Takeshi Nakabayashi ,  Masayuki Isaji

    发明人： Nobuhiko Fushimi ,  Kazuya Tatani ,  Hideki Fujikura ,  Toshihiro Nishimura ,  Minoru Fujioka ,  Takeshi Nakabayashi ,  Masayuki Isaji

    IPC分类号： A61K31/70 ,  C07H15/00 ,  C07H17/00

    CPC分类号： C07H15/203

    摘要： The present invention provides glucopyranosyloxybenzylbenzene derivatives represented by the general formula: wherein P represents a hydrogen atom or a group forming a prodrug; R1 represents a hydrogen atom, an optionally substituted amino group, a carbamoyl group, an optionally substituted lower alkyl group, an optionally substituted lower alkoxy group, etc.; R2 represents a hydrogen atom or a lower alkyl group; and R3 represents an optionally substituted lower alkyl group, an optionally substituted lower alkoxy group, an optionally substituted lower alkylthio group, etc., which have an improved oral absorption, and exert an inhibitory activity in human SGLT2, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, or pharmaceutically acceptable salts thereof, and pharmaceutical uses thereof.

    摘要翻译： 本发明提供由以下通式表示的吡喃葡萄糖氧基苄基苯衍生物：其中P表示氢原子或形成前药的基团; R1表示氢原子，任选取代的氨基，氨基甲酰基，任选取代的低级烷基，任选取代的低级烷氧基等; R2表示氢原子或低级烷基; R3代表任意取代的低级烷基，任意取代的低级烷氧基，任意取代的低级烷硫基等，它们具有改善的口服吸收，并且在人SGLT2中具有抑制活性，因此可用作 预防或治疗与糖尿病，糖尿病并发症或肥胖症等高血糖相关的疾病或其药学上可接受的盐及其药学用途。

    Nitrogenous heterocyclic derivatives, medicinal compositions containing the same, medicinal uses thereof, and intermediates therefor
    4.
    发明授权
    Nitrogenous heterocyclic derivatives, medicinal compositions containing the same, medicinal uses thereof, and intermediates therefor 失效
    含氮杂环衍生物，含有它们的药物组合物，其医药用途及其中间体

    公开(公告)号：US07271153B2

    公开(公告)日：2007-09-18

    申请号：US10481013

    申请日：2002-06-17

    申请人： Toshihiro Nishimura ,  Hideki Fujikura ,  Nobuhiko Fushimi ,  Kazuya Tatani ,  Kenji Katsuno ,  Masayuki Isaji

    发明人： Toshihiro Nishimura ,  Hideki Fujikura ,  Nobuhiko Fushimi ,  Kazuya Tatani ,  Kenji Katsuno ,  Masayuki Isaji

    IPC分类号： A01N43/04 ,  A61K31/70 ,  C07H15/24

    CPC分类号： C07H17/02 ,  Y02P20/55 ,  Y10S514/866 ,  Y10S514/909

    摘要： The present invention provides nitrogen-containing heterocyclic derivatives represented by the general formula: wherein X1 and X3 independently represent N or CH; X2 represents N or CR2; X4 represents N or CR3; and with the proviso that one or two of X1, X2, X3 and X4 represent N; R1 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a lower alkoxy-substituted (lower alkyl) group, a lower alkoxy-substituted (lower alkoxy) group, a lower alkoxy(lower alkoxy)-substituted (lower alkyl) group, a cyclic lower alkyl group, a halo(lower alkyl) group or a group represented by the general formula: HO-A- wherein A represents a lower alkylene group, a lower alkyleneoxy group or a lower alkylenethio group; R2 represents a hydrogen atom, a halogen atom, a lower alkyl group, a cyclic lower alkyl group, a lower alkoxy group, an amino group, a (lower acyl)amino group, a mono(lower alkyl)amino group or a di(lower alkyl)amino group; and R3 represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, or prodrugs thereof which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutical compositions comprising the same, and pharmaceutical uses and production intermediates thereof.

    摘要翻译： 本发明提供由以下通式表示的含氮杂环衍生物：其中X 1和X 3独立地表示N或CH; X 2表示N或CR 2; X 4表示N或CR 3; 并且条件是X 1，X 2，X 3和X 4中的一个或者两个表示N ; R 1表示氢原子，卤素原子，低级烷基，低级烷氧基，低级烷硫基，低级烷氧基取代的（低级烷基），低级烷氧基取代的（低级烷基） 低级烷氧基）基团，低级烷氧基（低级烷氧基） - 取代（低级烷基）基团，环状低级烷基基团，卤代（低级烷基）基团或由通式HO-A-表示的基团，其中A表示 低级亚烷基，低级亚烷基氧基或低级亚烷基硫基; R 2表示氢原子，卤素原子，低级烷基，环状低级烷基，低级烷氧基，氨基，（低级酰基）氨基，单（低级） 烷基）氨基或二（低级烷基）氨基; R 3表示氢原子或低级烷基，或其药学上可接受的盐或其前药，其可用作预防或治疗与高血糖相关的疾病如糖尿病，糖尿病 并发症或肥胖症，包含其的药物组合物及其药物用途和生产中间体。

    Purinenucleoside derivative modified in 8-position and medical use thereof
    5.
    发明申请
    Purinenucleoside derivative modified in 8-position and medical use thereof 失效
    8位修饰的嘌呤核苷衍生物及其用途

    公开(公告)号：US20070179115A1

    公开(公告)日：2007-08-02

    申请号：US11717741

    申请日：2007-03-13

    申请人： Kazuya Tatani ,  Yoshinori Nonaka ,  Norihiko Kikuchi

    发明人： Kazuya Tatani ,  Yoshinori Nonaka ,  Norihiko Kikuchi

    IPC分类号： A61K31/7076 ,  C07H19/16

    CPC分类号： A61K45/06 ,  A61K31/7076 ,  C07H19/167 ,  C07H19/173

    摘要： The present invention provides an 8-modified purinenucleoside derivative which is useful for diseases associated with an abnormality of plasma uric acid level. An 8-modified purinenucleoside derivative represented by the following formula (I), a prodrug thereof or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, is useful for the prevention or treatment of gout, hyperuricemia, urinary lithiasis, hyperuricemic nephropathy or the like. In the formula, n is 1 or 2; RA is a hydrogen atom or a hydroxyl group; R1 is a hydrogen atom, a hydroxyl group, a thiol group, an amino group or a chlorine atom; ring J represents an optionally substituted 2-naphthyl group, or a group represented by the following general formula (II) wherein Y represents a single bond or a connecting group; ring Z represents an optionally substituted aryl group or heteroaryl group or the like; and R2 to R4, P1 and Q represents a halogen atom, a cyano group or the like.

    摘要翻译： 本发明提供了可用于与血浆尿酸水平异常相关的疾病的8-修饰的嘌呤核苷衍生物。 由下式（I）表示的8-修饰的嘌呤核苷衍生物，其前体药物或其药学上可接受的盐或其水合物或溶剂合物可用于预防或治疗痛风，高尿酸血症，尿结石病，高尿酸性肾病或 类似。 在该式中，n为1或2; R A是氢原子或羟基; R 1是氢原子，羟基，硫醇基，氨基或氯原子; 环J表示任选取代的2-萘基，或由以下通式（II）表示的基团，其中Y表示单键或连接基团; 环Z表示任选取代的芳基或杂芳基等; R 2〜R 4，P 1和Q表示卤素原子，氰基等。

    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof
    6.
    发明授权
    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof 失效
    吡喃葡萄糖氧基苄基苯衍生物，含有它们的药物组合物及其制备中间体

    公开(公告)号：US07129381B2

    公开(公告)日：2006-10-31

    申请号：US10978413

    申请日：2004-11-02

    申请人： Hideki Fujikura ,  Toshihiro Nishimura ,  Nobuhiko Fushimi ,  Kazuya Tatani ,  Norihiko Kikuchi ,  Kenji Katsuno ,  Masayuki Isaji

    发明人： Hideki Fujikura ,  Toshihiro Nishimura ,  Nobuhiko Fushimi ,  Kazuya Tatani ,  Norihiko Kikuchi ,  Kenji Katsuno ,  Masayuki Isaji

    IPC分类号： C07C15/00 ,  C07C27/10 ,  C07C33/18 ,  C07C39/00

    CPC分类号： C07H15/203

    摘要： The present invention relates to glucopyranosyl-oxybenzylbenzene derivatives represented by the general formula: wherein R1 represents a hydrogen atom, a hydroxy group, a substituted or unsubstituted amino group, a carbamoyl group, a substituted or unsubstituted(lower alkyl) group, a substituted or unsubstituted(lower alkoxy) group etc.; R2 represents a hydrogen atom or a lower alkyl group; and R3 represents a substituted or unsubstituted(lower alkyl) group, a substituted or unsubstituted(lower alkoxy) group, a substituted or unsubstituted(lower alkylthio) group etc., or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complication or obesity, pharmaceutical compositions comprising the same and intermediates thereof.

    摘要翻译： 本发明涉及由以下通式表示的吡喃葡萄糖基 - 氧苄基苯衍生物：其中R 1表示氢原子，羟基，取代或未取代的氨基，氨基甲酰基，取代或未取代的（ 低级烷基）基团，取代或未取代的（低级烷氧基）基团等; R 2表示氢原子或低级烷基; 和R 3表示取代或未取代的（低级烷基）基团，取代或未取代的（低级烷氧基）基团，取代或未取代的（低级烷硫基）等，或其药学上可接受的盐，其中 在人SGLT2中具有抑制活性，并且可用作预防或治疗与高血糖相关的疾病如糖尿病，糖尿病并发症或肥胖症的药剂，包含其的药物组合物及其中间体。

    Glucopyranosyloxybenzylbenzene derivatives and medicinal compositions containing the same
    7.
    发明申请
    Glucopyranosyloxybenzylbenzene derivatives and medicinal compositions containing the same 审中-公开
    吡喃葡萄糖氧基苄基苯衍生物和含有它们的药物组合物

    公开(公告)号：US20050065098A1

    公开(公告)日：2005-03-24

    申请号：US10916548

    申请日：2004-08-12

    申请人： Hideki Fujikura ,  Nobuhiko Fushimi ,  Toshihiro Nishimura ,  Kazuya Tatani ,  Masayuki Isaji

    发明人： Hideki Fujikura ,  Nobuhiko Fushimi ,  Toshihiro Nishimura ,  Kazuya Tatani ,  Masayuki Isaji

    IPC分类号： A61K31/7034 ,  A61P3/04 ,  A61P3/10 ,  A61P43/00 ,  C07H15/203 ,  A61K31/70 ,  C07H13/02

    CPC分类号： C07H15/203 ,  A61K31/7034

    摘要： The present invention relates to glucopyranosyloxy-benzylbenzene derivatives represented by the general formula: wherein P represents a group forming a prodrug; and R represents a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a lower alkoxy-substituted (lower alkyl) group, a lower alkoxy-substituted (lower alkoxy) group or a lower alkoxy-substituted (lower alkylthio) group, which have an improved oral absorption and can exert an excellent inhibitory activity in human SGLT2 in vivo and which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutical compositions comprising the same.

    摘要翻译： 本发明涉及由以下通式表示的吡喃葡萄糖氧基 - 苄基苯衍生物：其中P表示形成前药的基团; R代表低级烷基，低级烷氧基，低级烷硫基，低级烷氧基取代的（低级烷基），低级烷氧基取代的（低级烷氧基）或低级烷氧基取代的（低级烷硫基） 其具有改善的口服吸收并且可以在体内在人SGLT2中发挥优异的抑制活性，并且其可用作预防或治疗与高血糖相关的疾病如糖尿病，糖尿病并发症或肥胖症的药剂，以及包含 相同。

    Benzimidazole derivatives and medical uses thereof
    9.
    发明授权
    Benzimidazole derivatives and medical uses thereof 失效
    苯并咪唑衍生物及其医疗用途

    公开(公告)号：US07547680B2

    公开(公告)日：2009-06-16

    申请号：US11473957

    申请日：2006-06-23

    申请人： Norihiko Kikuchi ,  Yoshinori Nonaka ,  Kazuya Tatani ,  Masahiro Hiratochi ,  Yu Kuramochi ,  Masayuki Isaji ,  Kazuo Shimizu ,  Takashi Miyagi

    发明人： Norihiko Kikuchi ,  Yoshinori Nonaka ,  Kazuya Tatani ,  Masahiro Hiratochi ,  Yu Kuramochi ,  Masayuki Isaji ,  Kazuo Shimizu ,  Takashi Miyagi

    IPC分类号： A01N43/04 ,  A61K31/70

    CPC分类号： C07H19/052

    摘要： The present invention provides benzimidazole derivatives represented by the following formula (I) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exert an inhibitory activity on sodium-dependent nucleoside transporter 2 and are useful for a disease associated with an abnormality of plasma uric acid level. The compounds of the present invention are useful for the prevention or treatment of gout, hyperuricemia, urinary lithiasis, hyperuricemic nephropathy or the like.In the formula, n is 1 or 2; R1 and R2 are H, a halogen atom, cyano group, optionally substituted alkyl group, optionally substituted aryl group or the like; R3 is H, a halogen atom, optionally substituted alkyl group or the like; R4 and R5 are H, a halogen atom, OH or the like; and R6 and RX are H or OH: RY is F or OH.

    摘要翻译： 本发明提供由下式（I）表示的苯并咪唑衍生物或其药学上可接受的盐或其前药，其对钠依赖性核苷转运蛋白2具有抑制活性，并且可用于与血浆尿酸异常有关的疾病 水平。 本发明的化合物可用于预防或治疗痛风，高尿酸血症，尿结石病，高尿酸性肾病等。 在该式中，n为1或2; R 1和R 2是H，卤素原子，氰基，任选取代的烷基，任选取代的芳基等; R3是H，卤素原子，任选取代的烷基等; R 4和R 5是H，卤素原子，OH等; R6和RX是H或OH：RY是F或OH。

    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates for the preparation of the derivatives
    10.
    发明授权
    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates for the preparation of the derivatives 有权
    吡喃葡萄糖氧基苄基苯衍生物，含有该衍生物的药物组合物和用于制备衍生物的中间体

    公开(公告)号：US07045665B2

    公开(公告)日：2006-05-16

    申请号：US10959505

    申请日：2004-10-07

    申请人： Hideki Fujikura ,  Nobuhiko Fushimi ,  Toshihiro Nishimura ,  Kazuya Tatani ,  Kenji Katsuno ,  Masahiro Hiratochi ,  Yoshiki Tokutake ,  Masayuki Isaji

    发明人： Hideki Fujikura ,  Nobuhiko Fushimi ,  Toshihiro Nishimura ,  Kazuya Tatani ,  Kenji Katsuno ,  Masahiro Hiratochi ,  Yoshiki Tokutake ,  Masayuki Isaji

    IPC分类号： C07C39/12 ,  C07C27/10 ,  C07C33/18

    CPC分类号： C07H15/203

    摘要： The present invention relates to benzylphenol derivatives represented by the general formula: wherein R11 represents a hydrogen atom or a protected hydroxy(lower alkyl) group; and R12 represents a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a protected hydroxy(lower alkyl) group, a protected hydroxy(lower alkoxy) group, a protected hydroxy(lower alkylthio) group, a lower alkoxy-substituted (lower alkyl) group, a lower alkoxy-substituted (lower alkoxy) group or a lower alkoxy-substituted (lower alkylthio) group; with the proviso that R12 is not a methyl group, an ethyl group, an isopropyl group, a tert-butyl group or a methoxy group when R11 is a hydrogen atom, or a salt thereof, which are used as intermediates for making glucopyranosyloxybenzylbenzene compounds having inhibitory activity in human SGLT2 and are useful in treating diseases associated with hyperglycemia, such as diabetes.

    摘要翻译： 本发明涉及由以下通式表示的苄基酚衍生物：其中R 11表示氢原子或被保护的羟基（低级烷基）基团; R 12表示低级烷基，低级烷氧基，低级烷硫基，被保护的羟基（低级烷基），被保护的羟基（低级烷氧基），被保护的羟基（低级烷硫基 ）基团，低级烷氧基取代的（低级烷基）基团，低级烷氧基取代的（低级烷氧基基团）或低级烷氧基取代的（低级烷硫基）基团; 条件是当R 11是氢原子时，R 12不是甲基，乙基，异丙基，叔丁基或甲氧基 或其盐，其用作制备在人SGLT2中具有抑制活性的吡喃葡萄糖氧基苄基苯化合物的中间体，并且可用于治疗与高血糖相关的疾病如糖尿病。