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    Isoxazolopyridone derivatives and their use
    1.
    发明授权
    Isoxazolopyridone derivatives and their use 失效
    异恶唑吡啶酮衍生物及其用途

    公开(公告)号：US07053219B2

    公开(公告)日：2006-05-30

    申请号：US10732988

    申请日：2003-12-10

    申请人： Masayuki Nakamura ,  Hideki Kurihara ,  Mitsuru Ohkubo ,  Naohiro Tsukamoto

    发明人： Masayuki Nakamura ,  Hideki Kurihara ,  Mitsuru Ohkubo ,  Naohiro Tsukamoto

    IPC分类号： C07D471/22 ,  A61K31/44

    CPC分类号： C07D498/04

    摘要： The invention relates to isoxazolopyridone derivatives of a formula (I-a): wherein R1a represents an optionally-substituted heteroaryl or phenyl group, R2a represents an optionally-substituted phenyl or heteroaryl group, and R3a represents a methyl group, provided that, (1) when R1a is an unsubstituted phenyl group, then R2a must not be a para-substituted phenyl group of which the substituent is any of a methoxy group, a chloro group, a methyl group, a trifluoromethyl group, a fluoro group, a bromomethyl group or a dimethylaminomethyl group, and R2a must not be an unsubstituted heteroaryl group, and (2) when R1a is a 4-tolyl group or a 4-fluorophenyl group, then R2a must not be an unsubstituted phenyl group, a 4-methoxyphenyl group or a 4-fluorophenyl group, or their pharmaceutically-acceptable salts. The isoxazolopyridone derivatives or their pharmaceutically-acceptable salts of the invention have a metabotropic glutamic acid receptor-antagonistic effect, and are useful for remedy of, for example, anxiety disorders, psychosomatic disorders, obsessive-compulsive neurosis, bipolar disorders, melancholia, eating disorders, schizophrenia, multi-infarct dementia, Alzheimer disease, epilepsy, Parkinson disease, Huntington's chorea, pain or retrograde neurosis.

    摘要翻译： 本发明涉及式（Ia）的异恶唑吡啶酮衍生物：其中R 1a表示任选取代的杂芳基或苯基，R 2a表示任选取代的苯基或杂芳基 基团，且R 3a表示甲基，条件是（1）当R 1a为未取代的苯基时，R 2a必须 不是取代基是甲氧基，氯基，甲基，三氟甲基，氟基，溴甲基或二甲基氨基甲基中的任何一个的对位取代的苯基，R 2a， / SUP>不能是未取代的杂芳基，和（2）当R 1a是4-甲苯基或4-氟苯基时，R 2a不能 为未取代的苯基，4-甲氧基苯基或4-氟苯基，或其药学上可接受的盐。 本发明的异恶唑吡啶酮衍生物或其药学上可接受的盐具有代谢型谷氨酸受体拮抗作用，并且可用于治疗例如焦虑症，心理障碍，强迫性神经症，双相情感障碍，忧郁症，进食障碍 ，精神分裂症，多发性梗塞性痴呆，阿尔茨海默病，癫痫，帕金森病，亨廷顿舞蹈病，疼痛或逆行神经症。

    Spirochromanon derivatives
    2.
    发明授权
    Spirochromanon derivatives 有权
    螺二色素衍生物

    公开(公告)号：US08138197B2

    公开(公告)日：2012-03-20

    申请号：US12518466

    申请日：2008-01-08

    申请人： Tomoharu Iino ,  Hideki Jona ,  Hideki Kurihara ,  Masayuki Nakamura ,  Kenji Niiyama ,  Jun Shibata ,  Tadashi Shimamura ,  Hitomi Watanabe ,  Takeru Yamakawa ,  Lihu Yang

    发明人： Tomoharu Iino ,  Hideki Jona ,  Hideki Kurihara ,  Masayuki Nakamura ,  Kenji Niiyama ,  Jun Shibata ,  Tadashi Shimamura ,  Hitomi Watanabe ,  Takeru Yamakawa ,  Lihu Yang

    IPC分类号： A61K31/438 ,  C07D221/20

    CPC分类号： C07D491/107 ,  C07D491/20 ,  C07D519/00

    摘要： The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of benzene, pyrazole, isoxazole, pyridine, indole, 1H-indazole, 1H-furo[2,3-c]pyrazole, 1H-thieno[2,3-c]pyrazole, benzimidazole, 1,2-benzisoxazole, imidazo[1,2-a]pyridine, imidazo[1,5-a]pyridine and 1H-pyrazolo[3,4-a]pyridine, having Ar2, and optionally having one or two or more substituents selected from R3; R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; or a C1-C6 alkyl group optionally having a substituent; or an aryl or heterocyclic group optionally having a substituent; or a C1-C6 alkyl group or a C2-C6 alkenyl group having the aryl or heterocyclic group; T and U each independently represent a nitrogen atom or a methine group; and V represents an oxygen atom or a sulfur atom. The compound of the invention is useful as therapeutical agents for various ACC-related diseases.

    摘要翻译： 本发明涉及通式（I）的化合物：其中Ar 1表示由选自苯，吡唑，异恶唑，吡啶，吲哚，1H-吲唑，1H-呋喃并[ 3-c]吡唑，1H-噻吩并[2,3-c]吡唑，苯并咪唑，1,2-苯并异恶唑，咪唑并[1,2-a]吡啶，咪唑并[1,5-a]吡啶和1H-吡唑并[ 3,4-a]吡啶，其具有Ar 2，并且任选具有一个或两个或更多个选自R 3的取代基; R 1和R 2各自独立地表示氢原子，卤素原子，氰基，C 2 -C 6烯基，C 1 -C 6烷氧基，C 2 -C 7烷酰基，C 2 -C 7烷氧基羰基，芳烷氧基羰基， 氨基甲酰基-C 1 -C 6烷氧基，羧基-C 2 -C 6烯基或-Q 1 -N（R a）-Q 2 -R b的基团; 或任选具有取代基的C1-C6烷基; 或任选具有取代基的芳基或杂环基; 或具有芳基或杂环基的C 1 -C 6烷基或C 2 -C 6烯基; T和U各自独立地表示氮原子或次甲基; V表示氧原子或硫原子。 本发明的化合物可用作各种ACC相关疾病的治疗剂。

    SPIROCHROMANON DERIVATIVES
    3.
    发明申请
    SPIROCHROMANON DERIVATIVES 有权
    螺吡喃衍生物

    公开(公告)号：US20090270436A1

    公开(公告)日：2009-10-29

    申请号：US12518466

    申请日：2008-01-08

    申请人： Tomoharu Iino ,  Hideki Jona ,  Hideki Kurihara ,  Masayuki Nakamura ,  Kenji Niiyama ,  Jun Shibata ,  Tadashi Shimamura ,  Hitomi Watanabe ,  Takeru Yamakawa ,  Lihu Yang

    发明人： Tomoharu Iino ,  Hideki Jona ,  Hideki Kurihara ,  Masayuki Nakamura ,  Kenji Niiyama ,  Jun Shibata ,  Tadashi Shimamura ,  Hitomi Watanabe ,  Takeru Yamakawa ,  Lihu Yang

    IPC分类号： A61K31/438 ,  C07D401/14 ,  A61P3/00 ,  A61P35/00 ,  A61P31/00

    CPC分类号： C07D491/107 ,  C07D491/20 ,  C07D519/00

    摘要： The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of benzene, pyrazole, isoxazole, pyridine, indole, 1H-indazole, 1H-furo[2,3-c]pyrazole, 1H-thieno[2,3-c]pyrazole, benzimidazole, 1,2-benzisoxazole, imidazo[1,2-a]pyridine, imidazo[1,5-a]pyridine and 1H-pyrazolo[3,4-b]pyridine, having Ar2, and optionally having one or two or more substituents selected from R3: R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; or a C1-C6 alkyl group optionally having a substituent; or an aryl or heterocyclic group optionally having a substituent; or a C1-C6 alkyl group or a C2-C6 alkenyl group having the aryl or heterocyclic group; T and U each independently represent a nitrogen atom or a machine group; and V represents an oxygen atom or a sulfur atom. The compound of the invention is useful as therapeutical agents for various ACC-related diseases.

    摘要翻译： 本发明涉及通式（I）的化合物：其中Ar 1表示由选自苯，吡唑，异恶唑，吡啶，吲哚，1H-吲唑，1H-呋喃并[ 3-c]吡唑，1H-噻吩并[2,3-c]吡唑，苯并咪唑，1,2-苯并异恶唑，咪唑并[1,2-a]吡啶，咪唑并[1,5-a]吡啶和1H-吡唑并[ 具有Ar 2且任选具有一个或两个以上选自R 3：R 1和R 2的取代基的3,4-b]吡啶各自独立地表示氢原子，卤素原子，氰基，C 2 -C 6烯基， C1-C6烷氧基，C2-C7烷酰基，C2-C7烷氧基羰基，芳烷氧基羰基，氨基甲酰基C1-C6烷氧基，羧基-C2-C6链烯基或-Q1-N （Ra）-Q2-Rb; 或任选具有取代基的C1-C6烷基; 或任选具有取代基的芳基或杂环基; 或具有芳基或杂环基的C 1 -C 6烷基或C 2 -C 6烯基; T和U各自独立地表示氮原子或机组; V表示氧原子或硫原子。 本发明的化合物可用作各种ACC相关疾病的治疗剂。