利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

28 条记录 (耗时 0.025 秒)

    6-fluorobicyclo[3.1.0]hexane derivatives
    11.
    发明授权
    6-fluorobicyclo[3.1.0]hexane derivatives 有权
    6-氟二环[3.1.0]己烷衍生物

    公开(公告)号：US06333428B1

    公开(公告)日：2001-12-25

    申请号：US09763408

    申请日：2001-02-22

    申请人： Atsuro Nakazato ,  Toshihito Kumagai ,  Kazunari Sakagami ,  Kazuyuki Tomisawa

    发明人： Atsuro Nakazato ,  Toshihito Kumagai ,  Kazunari Sakagami ,  Kazuyuki Tomisawa

    IPC分类号： C07C6974

    CPC分类号： C07D317/72 ,  C07C229/50 ,  C07C2602/18 ,  C07D339/06

    摘要： The present invention provides fluorobicyclo[3.1.0]hexane derivatives represented by the formula [wherein R1 and R2 are the same or different and each represents a hydrogen atom, a C1-10 alkyl group, a C3-8 cycloalkyl group or a C3-8 cycloalkyl-C1-5 alkyl group: Y1 and Y2 are the same or different and each represents a hydrogen atom, a C1-10 alkylthio group, a C3-8 cycloalkylthio group, a C3-8 cycloalkyl-C1-5 alkylthio group, a C1-5 alkoxy group, a C3-8 cycloalkoxy group or a C3-8 cycloalkyl-C1-5 alkoxy group; or one represents a hydrogen atom and the other represents a hydroxyl group, a C1-5 alkoxy group, a C3-8 cycloalkoxy group or a C3-8 cycloalkyl-C1-5 alkoxy group; or Y1 and Y2 together represent an oxygen atom or —X(CH2)nX— (X represents an oxygen atom or a sulfur atom: N is 2 or 3)], pharmaceutically acceptable salts thereof, or hydrates thereof. The compounds of the present invention are useful as drugs, in particular group 2 metabotropic glutamate receptor agonists, and useful for treatment or prevention of psychiatric disorders such as, for example, schizophrenia, anxiety and associated diseases, depression, bipolar disorder, and epilepsy, as well as neurological diseases such as, for example, drug dependence, cognitive disorders, Alzheimer's disease, Huntington's chorea, Parkinson's disease, dyskinesia associated with muscular stiffness, cerebral ischemia, cerebral failure, myelopathy, and head trauma.

    摘要翻译： 本发明提供由式[其中R 1和R 2相同或不同，表示氢原子，C 1-10烷基，C 3-8环烷基或C 3-8环烷基]表示的氟双环[3.1.0] 8环烷基-C 1-5烷基：Y1和Y2相同或不同，各自表示氢原子，C1-10烷硫基，C3-8环硫基，C3-8环烷基-C1-5烷硫基， C 1-5烷氧基，C 3-8环烷氧基或C 3-8环烷基-C 1-5烷氧基; 或者一个表示氢原子，另一个表示羟基，C 1-5烷氧基，C 3-8环烷氧基或C 3-8环烷基-C 1-5烷氧基; 或Y1和Y2一起表示氧原子或-X（CH 2）n X-（X表示氧原子或硫原子：N为2或3）]，其药学上可接受的盐或其水合物。本发明化合物 本发明可用作药物，特别是组2代谢型谷氨酸受体激动剂，并且可用于治疗或预防精神病学障碍，例如精神分裂症，焦虑和相关疾病，抑郁症，双相性精神障碍和癫痫以及神经系统疾病 例如药物依赖，认知障碍，阿尔茨海默病，亨廷顿氏舞蹈病，帕金森病，与肌肉僵硬相关的运动障碍，脑缺血，脑衰竭，脊髓损伤和头部创伤。

    2-phenoxyaniline derivatives
    12.
    发明授权
    2-phenoxyaniline derivatives 失效
    2-苯氧基苯胺衍生物

    公开(公告)号：US6156801A

    公开(公告)日：2000-12-05

    申请号：US381039

    申请日：1999-09-15

    申请人： Tomomi Ota ,  Misa Nakanishi ,  Minoru Taguchi ,  Kazuyuki Tomisawa

    发明人： Tomomi Ota ,  Misa Nakanishi ,  Minoru Taguchi ,  Kazuyuki Tomisawa

    IPC分类号： C07C217/90 ,  C07C225/22 ,  C07C233/43 ,  C07C235/34 ,  C07C255/59 ,  A61K31/136 ,  A61K31/167 ,  A61K31/277 ,  C07C237/40 ,  C07C255/58

    CPC分类号： C07C225/22 ,  C07C217/90 ,  C07C233/43 ,  C07C235/34 ,  C07C255/59 ,  C07C2101/02

    摘要： A 2-phenoxyaniline derivative represented by the formula: ##STR1## wherein R.sup.1 is a hydrogen atom, an amino group or an NHCOR.sup.3 group, R.sup.2 is a halogen atom, an amino group, a cyano group, a C.sub.1-6 alkyl group, a C.sub.1-3 perfluoroalkyl group, an NHCOR.sup.3 group, a CH.sub.2 OR.sup.4 group, an OCH.sub.2 R.sup.5 group or a COR.sup.6 group, R.sup.3 is a C.sub.1-6 alkyl group, R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl group, R.sup.5 is a hydrogen atom, a C.sub.1-6 alkyl group, a C.sub.1-5 aminoalkyl group, a C.sub.2-7 alkoxy-carbonyl group or a carbamoyl group, and R.sup.6 is a C.sub.1-6 alkyl group or a C.sub.3-8 cycloalkyl group which is unsubstituted or substituted by a halogen atom, an amino group, a cyano group or a straight or branched C.sub.1-6 alkyl group; or a pharmaceutically acceptable salt thereof.

    摘要翻译： PCT No.PCT / JP98 / 01367 Sec。 371日期1999年9月15日 102（e）1999年9月15日PCT 1998年3月26日PCT PCT。 第WO98 / 43943号公报 日期：1998年10月8日由下式表示的2-苯氧基苯胺衍生物：其中R1为氢原子，氨基或NHCOR3基，R2为卤素原子，氨基，氰基，C1-6烷基 ，C1-3全氟烷基，NHCOR3基，CH2OR4基，OCH2R5基或COR6基，R3是C1-6烷基，R4是氢原子或C1-6烷基，R5是氢 原子，C1-6烷基，C1-5氨基烷基，C2-7烷氧基 - 羰基或氨基甲酰基，R6是未取代或取代的C1-6烷基或C3-8环烷基 通过卤素原子，氨基，氰基或直链或支链C 1-6烷基; 或其药学上可接受的盐。

    Amino compounds and angiotensin IV receptor agonists
    13.
    发明授权
    Amino compounds and angiotensin IV receptor agonists 失效
    氨基化合物和血管紧张素IV受体激动剂

    公开(公告)号：US6066672A

    公开(公告)日：2000-05-23

    申请号：US101449

    申请日：1998-07-16

    申请人： Takeo Kobori ,  Kenichi Goda ,  Kikuo Sugimoto ,  Tomomi Ota ,  Kazuyuki Tomisawa

    发明人： Takeo Kobori ,  Kenichi Goda ,  Kikuo Sugimoto ,  Tomomi Ota ,  Kazuyuki Tomisawa

    IPC分类号： C07C237/20 ,  C07D213/40 ,  C07D215/12 ,  A61K31/165 ,  C07C233/05

    CPC分类号： C07D213/40 ,  C07C237/20 ,  C07D215/12

    摘要： The present invention provides an amino compound represented by Formula: ##STR1## wherein X is CH.sub.2 NH or CONH, Y is CH.sub.2 NH or CONH with the proviso that X and Y are not CONH at the same time; Z is CH.dbd.C(R.sup.4)R.sup.5, CH.sub.2 CH(R.sup.4)R.sup.5 or an alkoxycarbonyl group, R.sup.1 is a hydrogen atom; a lower alkyl group, a cycloalkyl group, a cycloalkyl-substituted alkyl group, an aralkyl group or an aryl group, each group of which is substituted or unsubstituted, R.sup.2 and R.sup.3 are each independently a lower alkyl group or an aralkyl group, each group of which is substituted or unsubstituted, and R.sup.4 and R.sup.5 are each independently a hydrogen atom; an alkyl group, an aralkyl group, an aryl group or a heteroaryl group, each group of which is substituted or unsubstituted, or a pharmaceutically acceptable salt thereof; a medicine comprising the amino compound of Formula (1) or a pharmaceutically acceptable salt; and an angiotensin IV receptor agonist containing the same as an effective component, which are useful, in particular, as a therapeutical drug (antagonist or agonist) for various diseases in which angiotensin IV participates, for example, acceleration of renal blood flow, cerebral vasodilation, inhibition of cell proliferation and hypermnesia.

    摘要翻译： PCT No.PCT / JP97 / 02716 Sec。 371日期：1998年7月16日 102（e）日期1998年7月16日PCT提交1997年8月5日PCT公布。 第WO98 / 05624号公报 日期：1998年2月12日本发明提供由下式表示的氨基化合物：其中X为CH 2 NH或CONH，Y为CH 2 NH或CONH，条件是X和Y不同时为CONH; Z是CH = C（R4）R5，CH2CH（R4）R5或烷氧基羰基，R1是氢原子; 低级烷基，环烷基，环烷基取代的烷基，芳烷基或芳基，其各自为取代或未取代的，R2和R3各自独立地为低级烷基或芳烷基，各基团 其中R 4和R 5各自独立地为氢原子; 其各自为取代或未取代的烷基，芳烷基，芳基或杂芳基，或其药学上可接受的盐; 包含式（1）的氨基化合物或其药学上可接受的盐的药物; 和含有与有效组分相同的血管紧张素IV受体激动剂，其特别可用作血管紧张素IV参与的各种疾病的治疗药物（拮抗剂或激动剂），例如加速肾血流量，脑血管舒张 ，抑制细胞增殖和高血症。

    Intermediates and process for producing fluorine-containing amino acid compound by using the same
    15.
    发明授权
    Intermediates and process for producing fluorine-containing amino acid compound by using the same 有权
    中间体及使用它们的含氟氨基酸化合物的制造方法

    公开(公告)号：US06392086B1

    公开(公告)日：2002-05-21

    申请号：US09857631

    申请日：2001-06-07

    申请人： Atsuro Nakazato ,  Toshihito Kumagai ,  Kazunari Sakagami ,  Kazuyuki Tomisawa ,  Hisanako Ito ,  Takeo Taguchi

    发明人： Atsuro Nakazato ,  Toshihito Kumagai ,  Kazunari Sakagami ,  Kazuyuki Tomisawa ,  Hisanako Ito ,  Takeo Taguchi

    IPC分类号： C07C6974

    CPC分类号： C07D235/02 ,  C07B2200/07 ,  C07C51/363 ,  C07C62/38 ,  C07C69/757 ,  C07C227/18 ,  C07C229/50 ,  C07C235/82 ,  C07C255/47 ,  C07C2602/18 ,  C07C2602/40 ,  C07D303/42 ,  C07D303/46

    摘要： The present inventions relate to a (1S,5R,6S)- or (1SR, 5RS, 6SR)-3-fluoro-2-oxobicyclo[3.1.0]hex-3-ene-6-carboxylic acid derivative represented by Formula (1): [in the formula, R represents OR1 or NR1R2, wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a (C3-C6 cycloalkyl) (C1-C6 alkyl) group, an aryl group, an aryl (C1-C6 alkyl) group, a (C1-C6 alkoxy) (C1-C6 alkyl) group, a C1-C6 hydroxyalkyl group, a (C1-C6 alkylthio) (C1-C6 alkyl) group, or a C1-C6 mercaptoalkyl group], and a process for producing the same, and a process for efficiently producing a fluorine-containing amino acid compound acting on group 2 metabotropic glutamate receptors, which has treatment effects or prevention effects on psychiatric diseases or neurological diseases, characterized by hydrogenating the derivative, and subsequently, subjecting it to hydantoination or aminocyanidation, followed by hydrolysis.

    摘要翻译： 本发明涉及式（1S，5R，6S） - 或（1SR，5RS，6SR）-3-氟-2-氧代双环[3.1.0]己-3-烯-6-羧酸衍生物 1）：[式中，R表示OR 1或NR 1 R 2，其中R 1和R 2相同或不同，表示氢原子，C1-C6烷基，C3-C6环烷基，（C3-C6环烷基） ）（C1-C6烷基），芳基（C1-C6烷基），（C1-C6烷氧基）（C1-C6烷基），C1-C6羟基烷基，（C1-C6烷基） 烷基硫基）（C1-C6烷基）或C1-C6巯基烷基]及其制备方法，以及有效地制备作用于第2族代谢型谷氨酸受体的含氟氨基酸化合物的方法，其具有 治疗效果或预防对精神疾病或神经系统疾病的影响，其特征在于使该衍生物氢化，然后使其进行乙烯基化或氨基化，然后进行水解。

    Fluorine-containing amino acid derivatives
    16.
    发明授权
    Fluorine-containing amino acid derivatives 有权
    含氟氨基酸衍生物

    公开(公告)号：US06316498B1

    公开(公告)日：2001-11-13

    申请号：US09601131

    申请日：2000-07-27

    申请人： Atsuro Nakazato ,  Toshihito Kumagai ,  Kazunari Sakagami ,  Kazuyuki Tomisawa

    发明人： Atsuro Nakazato ,  Toshihito Kumagai ,  Kazunari Sakagami ,  Kazuyuki Tomisawa

    IPC分类号： C07C6974

    CPC分类号： C07C229/50 ,  C07C2602/18

    摘要： Fluorine-containing amino acid derivatives represented general formula (I), pharmaceutically acceptable salts thereof or hydrates of the same, wherein X1 represents hydrogen or fluorine; and R1 and R2 are the same or different and each represents hydrogen or lower C1-10 alkyl. These compounds are useful as drugs, in particular, group 2 metabotropic glutamate receptor agonists for treating and preventing psychiatric disorders such as schizophrenia, anxiety and associated diseases, depression, bipolar disturbance and epilepsy, and neurological diseases such as drug addiction, cognition disorder, Alzheimer's disease, Huntington's chorea, Parkinson's disease, motility disturbance associating muscular stiffness, cerebral ischemia, cerebral insufficiency, spinal cord lesion and head disturbance.

    摘要翻译： 含氟氨基酸衍生物表示通式（I），其药学上可接受的盐或其水合物，其中X1表示氢或氟; 并且R 1和R 2相同或不同，各自表示氢或低级C 1-10烷基。 这些化合物可用作药物，特别是用于治疗和预防精神疾病如精神分裂症，焦虑和相关疾病，抑郁症，双相障碍和癫痫以及神经系统疾病如药物成瘾，认知障碍，阿尔茨海默氏症的药物，特别是第2代代谢型谷氨酸受体激动剂 疾病，亨廷顿氏舞蹈病，帕金森病，运动障碍，肌肉僵硬，脑缺血，脑功能不全，脊髓损伤和头部干扰。

    4-Tetrahydropyridylpyrimidine derivatives
    17.
    发明授权
    4-Tetrahydropyridylpyrimidine derivatives 失效
    4-四氢吡啶基嘧啶衍生物

    公开(公告)号：US06187781B1

    公开(公告)日：2001-02-13

    申请号：US09381462

    申请日：1999-09-21

    申请人： Atsuro Nakazato ,  Toshihito Kumagai ,  Taketoshi Okubo ,  Izumi Aibe ,  Hideo Tanaka ,  Shigeyuki Chaki ,  Shigeru Okuyama ,  Kazuyuki Tomisawa

    发明人： Atsuro Nakazato ,  Toshihito Kumagai ,  Taketoshi Okubo ,  Izumi Aibe ,  Hideo Tanaka ,  Shigeyuki Chaki ,  Shigeru Okuyama ,  Kazuyuki Tomisawa

    IPC分类号： C07D40144

    CPC分类号： C07D401/04 ,  C07D405/14 ,  C07D409/14

    摘要： A 4-tetrahydropyridylpyrimidine compound represented by formula (I): wherein Ar represents a phenyl group substituted with 1 to 3 substituents selected from a halogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, and a trifluoromethyl group, a phenyl group, a thienyl group or a furanyl group; R1 represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an amino group or an amino group substituted with 1 or 2 alkyl groups having 1 to 5 carbon atoms; R2 represents an alkyl group having 1 to 5 carbon atoms, a cycloalkylalkyl group having 4 to 7 carbon atoms, an alkenyl group having 2 to 5 carbon atoms or an alkynyl group having 2 to 5 carbon atoms; and X1, X2, and X3, which may be the same or different, each represent a hydrogen atom, a halogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, an alkylthio group having 1 to 5 carbon atoms, an amino group or an amino group substituted with 1 or 2 alkyl groups having 1 to 5 carbon atoms, or a pharmaceutically acceptable salt thereof. The 4-Tetrahydropyridylpyrimidine compound finds utility in the treatment of diseases in which CRF is implicated.

    摘要翻译： 由式（I）表示的4-四氢吡啶基嘧啶化合物：其中Ar表示被1至3个选自卤素原子，具有1至5个碳原子的烷基，具有1至5个碳原子的烷氧基的取代基取代的苯基， 和三氟甲基，苯基，噻吩基或呋喃基; R1表示氢原子，碳原子数1〜5的烷基，氨基或被1〜2个碳原子数1〜2的烷基取代的氨基。 R2表示碳原子数1〜5的烷基，碳原子数4〜7的环烷基烷基，碳原子数2〜5的烯基或碳原子数2〜5的炔基。 X 1，X 2和X 3可以相同或不同，分别表示氢原子，卤素原子，碳原子数1〜5的烷基，碳原子数1〜5的烷氧基，烷硫基， 1至5个碳原子的氨基或被1或2个具有1至5个碳原子的烷基取代的氨基，或其药学上可接受的盐。 4-四氢吡啶基嘧啶化合物可用于治疗涉及CRF的疾病。

    2-carbonylthiazole derivatives and use of the same
    18.
    发明授权
    2-carbonylthiazole derivatives and use of the same 失效
    2-羰基噻唑衍生物及其用途

    公开(公告)号：US6166033A

    公开(公告)日：2000-12-26

    申请号：US269021

    申请日：1999-11-05

    申请人： Atsuro Nakazato ,  Toshihito Kumagai ,  Shigeyuki Chaki ,  Kazuyuki Tomisawa ,  Masashi Nagamine ,  Makoto Gotoh ,  Masanori Yoshida

    发明人： Atsuro Nakazato ,  Toshihito Kumagai ,  Shigeyuki Chaki ,  Kazuyuki Tomisawa ,  Masashi Nagamine ,  Makoto Gotoh ,  Masanori Yoshida

    IPC分类号： A61K31/425 ,  C07D417/06 ,  A61K31/4535 ,  A61K31/496 ,  C07D211/70 ,  C07D401/14 ,  C07D413/06

    CPC分类号： C07D417/06

    摘要： This invention provides a 2-carbonylthiazole derivative represented by formula (I): ##STR1## wherein each of Ar.sup.1 and Ar.sup.2 represents a phenyl group or a substituted phenyl group; R.sup.1 represents an alkoxy group having 1 to 5 carbon atoms, a hydroxyl group or an amino group; Y.sup.1 --Y.sup.2 represents CH--CO or C.dbd.CR.sup.2, wherein R.sup.2 represents a hydrogen atom or an alkyl group having 1 to 5 carbon atoms; and n is an integer of from 1 to 4, or a pharmaceutically acceptable salt thereof. The disclosed compounds are useful as drugs for preventing and treating dopamine D receptor-related morbid states such as schizophrenia and problematic behavior caused by cerebrovascular accidents and senile dementia and do not induce extrapyramidal disorders as side effects.

    摘要翻译： PCT No.PCT / JP97 / 03342 Sec。 371日期1999年11月5日 102（e）1999年11月5日PCT PCT 1997年9月19日PCT公布。 公开号WO98 / 12195 日期：1998年3月26日本发明提供由式（I）表示的2-羰基噻唑衍生物：其中Ar1和Ar2各自表示苯基或取代的苯基; R1表示碳原子数1〜5的烷氧基，羟基或氨基。 Y1-Y2表示CH-CO或C = CR2，其中R2表示氢原子或具有1至5个碳原子的烷基; 和n为1〜4的整数，或其药学上可接受的盐。 所公开的化合物可用作预防和治疗多巴胺D受体相关的病态，如精神分裂症和由脑血管意外和老年痴呆引起的问题行为的药物，并且不诱导锥体外系疾病作为副作用。

    Carboxylic acid derivatives and process for producing the same
    20.
    发明授权
    Carboxylic acid derivatives and process for producing the same 失效
    羧酸衍生物及其制备方法

    公开(公告)号：US06500958B2

    公开(公告)日：2002-12-31

    申请号：US10176528

    申请日：2002-06-24

    申请人： Atsuro Nakazato ,  Toshihito Kumagai ,  Kazunari Sakagami ,  Kazuyuki Tomisawa

    发明人： Atsuro Nakazato ,  Toshihito Kumagai ,  Kazunari Sakagami ,  Kazuyuki Tomisawa

    IPC分类号： C07D23500

    CPC分类号： C07D235/02 ,  C07C62/26 ,  C07C65/40 ,  C07C69/757 ,  C07C2602/18 ,  C07D339/06 ,  C07D495/10

    摘要： The present invention relates to compounds which are useful for efficient synthesis of 2-amino-4-oxobicyclo[3.1.0]hexane-2,6-dicarboxylic acids. The compounds according to the present invention comprise 2-oxobicyclo[3.1.0]hexane-6-carboxylic acid derivatives represented by the formula as follows: [wherein, R1 represents a hydrogen atom, a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a C3-C6 cycloalkyl C1-C6 alkyl group, an aryl group, an aryl C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C1-C6 hydroxyalkyl group, a C1-C6 alkylthio C1-C6 alkyl group, a C1-C6 mercaptoalkyl group, a tetrahydrofuranyl group, or a tetrahydropyranyl group; R2 and R3 are identical or different, and each represents a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a C3-C6 cycloalkyl C1-C6 alkyl group, an aryl group, or an aryl C1-C6 alkyl group, or alternatively, R2 and R3 together represent —(CH2)n— (wherein n represents 2 or 3); and Y1 and Y2 are identical or different, and each represents a sulfur atom, an oxygen atom, or a nitrogen atom].

    摘要翻译： 本发明涉及可用于高效合成2-氨基-4-氧代双环[3.1.0]己烷-2,6-二羧酸的化合物。根据本发明的化合物包含2-氧代双环[3.1.0] 由下式表示的己烷-6-羧酸衍生物：[其中，R1表示氢原子，C1-C6烷基，C3-C6环烷基，C3-C6环烷基C1-C6烷基，芳基 基团，芳基C1-C6烷基，C1-C6烷氧基C1-C6烷基，C1-C6羟基烷基，C1-C6烷硫基C1-C6烷基，C1-C6巯基烷基，四氢呋喃基， 或四氢吡喃基; R2和R3相同或不同，各自表示C1-C6烷基，C3-C6环烷基，C3-C6环烷基C1-C6烷基，芳基或芳基C1-C6烷基，或 或者，R2和R3一起表示 - （CH 2）n - （其中n表示2或3）; Y 1和Y 2相同或不同，各自表示硫原子，氧原子或氮原子]。