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    Carbamoyl tetrahydropyridine derivatives
    4.
    发明授权
    Carbamoyl tetrahydropyridine derivatives 失效
    氨基甲酰四氢吡啶衍生物

    公开(公告)号：US06894168B2

    公开(公告)日：2005-05-17

    申请号：US10347288

    申请日：2003-01-21

    申请人： Atsuro Nakazato ,  Taketoshi Okubo ,  Toshihito Kumagai ,  Kazuyuki Tomisawa

    发明人： Atsuro Nakazato ,  Taketoshi Okubo ,  Toshihito Kumagai ,  Kazuyuki Tomisawa

    IPC分类号： A61K31/519 ,  A61P1/00 ,  A61P7/10 ,  A61P9/10 ,  A61P9/12 ,  A61P17/02 ,  A61P25/08 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P29/00 ,  A61P37/02 ,  A61P43/00 ,  C07D473/00 ,  C07D487/04 ,  C07D211/78

    CPC分类号： A61K31/519 ,  C07D473/00 ,  C07D487/04

    摘要： Carbamoyl tetrahydropyridine derivatives represented by the formula: [in the formula, R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-C5 alkyl group, or the like; Y1—Y2 represents (R4)C═C(R5), (R6)C═N, N═N, (R7) N—CO, or N═C(R8); X1, X2, and X3 are identical or different, and each represents a hydrogen atom, a halogen atom, or the like; R3, R4, R5, and R6 are identical or different, and each represents a hydrogen atom or an alkyl group; R7 represents a hydrogen atom, a C1-C5 alkyl group, or the like; and R8 represents a hydrogen atom or a carbamoyl group] or a pharmaceutically acceptable salt thereof, and intermediates for the preparation thereof are provided. The derivatives described above are effective for diseases which are believed to involve CRF.

    摘要翻译： 由下式表示的氨基甲酰基四氢吡啶衍生物：[式中，R 1，R 2和R 2'相同或不同，各自表示氢原子，C 1 C 5 -C 15烷基等; Y 1 - （CH 2）2（R 4 S）（R 5），（R 6） CN，NN，（R 7）N-CO或NC（R 8）; X 1，X 2和X 3相同或不同，各自表示氢原子，卤素原子等; R 3，R 4，R 5和R 6相同或不同，并且各自表示氢 原子或烷基; R 7表示氢原子，C 1 -C 5烷基等; 和R 8表示氢原子或氨基甲酰基]或其药学上可接受的盐，以及其制备中间体。 上述衍生物对于被认为涉及CRF的疾病是有效的。

    Dicarboxylic acid derivatives
    5.
    发明授权
    Dicarboxylic acid derivatives 失效
    二羧酸衍生物

    公开(公告)号：US06770676B2

    公开(公告)日：2004-08-03

    申请号：US10297479

    申请日：2002-12-06

    申请人： Atsuro Nakazato ,  Toshihito Kumagai ,  Kosuke Kanuma ,  Kazunari Sakagami

    发明人： Atsuro Nakazato ,  Toshihito Kumagai ,  Kosuke Kanuma ,  Kazunari Sakagami

    IPC分类号： C07C6113

    CPC分类号： C07C229/50 ,  C07C2602/18

    摘要： The present invention relates to 2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives represented by the formula: the pharmaceutically acceptable salts thereof, or the hydrates thereof. The compounds of the present invention are useful as a medicament, and in particular, are useful as modulators acting on group 2 metabotropic glutamate receptors, having effects for treating and/or preventing psychiatric disorders such as schizophrenia, anxiety and its associated diseases, depression, bipolar disorder, and epilepsy; and/or neurological diseases such as 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： 本发明涉及由下式表示的2-氨基-6-氟双环[3.1.0]己烷-2,6-二羧酸衍生物或其药学上可接受的盐或其水合物。 本发明的化合物可用作药物，特别是可用作作用于组2代谢型谷氨酸受体的调节剂，具有治疗和/或预防精神病学障碍如精神分裂症，焦虑及其相关疾病，抑郁症， 双相障碍和癫痫; 和/或神经系统疾病如药物依赖性，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，脊髓病和头部创伤。

    Carbamoyl tetrahydropyridine derivatives
    6.
    发明授权
    Carbamoyl tetrahydropyridine derivatives 失效
    氨基甲酰四氢吡啶衍生物

    公开(公告)号：US06600038B1

    公开(公告)日：2003-07-29

    申请号：US09914534

    申请日：2001-08-30

    申请人： Atsuro Nakazato ,  Taketoshi Okubo ,  Toshihito Kumagai ,  Kazuyuki Tomisawa

    发明人： Atsuro Nakazato ,  Taketoshi Okubo ,  Toshihito Kumagai ,  Kazuyuki Tomisawa

    IPC分类号： C07D47334

    CPC分类号： A61K31/519 ,  C07D473/00 ,  C07D487/04

    摘要： Carbamoyl tetrahydropyridine derivatives represented by the formula: [in the formula, R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-C5 alkyl group, or the like; Y1-Y2 represents (R4)C═C(R5), (R6)C═N, N═N, (R7)N—CO, or N═C(R8); X1, X2, and X3 are identical or different, and each represents a hydrogen atom, a halogen atom, or the like; R3, R4, R5, and R6 are identical or different, and each represents a hydrogen atom or an alkyl group; R7 represents a hydrogen atom, a C1-C5 alkyl group, or the like; and R8 represents a hydrogen atom or a carbamoyl group] or a pharmaceutically acceptable salt thereof, and intermediates for the preparation thereof are provided. The derivatives described above are effective for diseases which are believed to involve CRF.

    摘要翻译： 由下式表示的氨基甲酰基四氢吡啶衍生物：[式中，R 1和R 2相同或不同，各自表示氢原子，C 1 -C 5烷基等; Y1-Y2表示（R4）C = C（R5），（R6）C = N，N = N，（R7）N-CO或N = C（R8） X1，X2和X3相同或不同，各自表示氢原子，卤素原子等; R3，R4，R5和R6相同或不同，各自表示氢原子或烷基; R7表示氢原子，C1-C5烷基等; 并且R8表示氢原子或氨基甲酰基]或其药学上可接受的盐，并且提供其制备的中间体。上述衍生物对于被认为涉及CRF的疾病是有效的。

    1,2-dihydro-2-oxoquinoline derivatives
    7.
    发明授权
    1,2-dihydro-2-oxoquinoline derivatives 失效
    1,2-二氢-2-氧代喹啉衍生物

    公开(公告)号：US06380384B1

    公开(公告)日：2002-04-30

    申请号：US09829203

    申请日：2001-04-10

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

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

    IPC分类号： C07D40106

    CPC分类号： C07D401/06 ,  C07D215/54 ,  C07D241/44

    摘要： A 1,2-dihydro-2-oxoquinoline derivative represented by the formula: wherein Ar is a pyridyl group or a group represented by the formula: (wherein X3 and X4 are the same or different, and are each a hydrogen atom, a halogen atom, a C1-5 alkyl group, a C1-5 alkoxy group, a hydroxyl group or a trifluoromethyl group), Y is a nitrogen atom, CH or C(OH), R1 and R2 are the same or different, and are each a hydrogen atom, a C1-10 alkyl group, a C3-15 alkoxyalkyl group or a C3-15 alkylaminoalkyl group, or R1 and R2 taken together with the nitrogen atom to which they are attached form a cyclic amino group, X1 and X2 are the same or different, and are each a hydrogen atom, a C1-5 alkyl group, a C1-5 alkoxy group or a halogen atom; or X1 and X2 taken together form an alkylenedioxy group, and n is an integer of 1 to 3; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 由下式表示的1,2-二氢-2-氧代喹啉衍生物：其中Ar是吡啶基或由下式表示的基团：（其中X 3和X 4相同或不同，并且各自为氢原子，卤素 原子，C 1-5烷基，C 1-5烷氧基，羟基或三氟甲基），Y是氮原子，CH或C（OH），R 1和R 2相同或不同，各自相同或不同 氢原子，C 1-10烷基，C 3-15烷氧基烷基或C 3-15烷基氨基烷基，或者R 1和R 2与它们所连接的氮原子一起形成环状氨基，X 1和X 2是 相同或不同，并且各自为氢原子，C1-5烷基，C1-5烷氧基或卤素原子; 或者X1和X2一起形成亚烷基二氧基，n为1〜3的整数。 或其药学上可接受的盐。

    Heteroaromatic derivatives
    8.
    发明授权
    Heteroaromatic derivatives 失效
    杂芳族衍生物

    公开(公告)号：US06291467B1

    公开(公告)日：2001-09-18

    申请号：US09646309

    申请日：2000-09-15

    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： C07D41706

    CPC分类号： C07D231/12 ,  C07D401/06 ,  C07D417/06

    摘要： An aromaheterocyclic derivative represented by the formula: wherein Z is a group represented by the following formula: wherein Ar1 is a phenyl group or a phenyl group substituted with a halogen atom or an alkyl group of 1 to 5 carbon atoms, R2 is an alkyl group of 1 to 5 carbon atoms, Y is a hydrogen atom, a mercapto group, an alkylthio group of 1 to 5 carbon atoms, an amino group or an amino group substituted with one or two alkyl groups having 1 to 5 carbon atoms, Ar2 is a phenyl group of one or two substituents selected from the group consisting of a halogen atom, an alkyl group of 1 to 5 carbon atoms, an alkoxy group of 1 to 5 carbon atoms, a hydroxyl group and a trifluoromethyl group, or a phenyl group, B1-B2 is CH—CO or C═C(R1) (wherein R1 is a hydrogen atom or an alkyl group of 1 to 5 carbon atoms), and n is an integer of 1 to 4, or a pharmaceutically acceptable salt thereof, which is a dopamine D4 receptor antagonist compound having an antipsychotic action without causing extrapyramidal diseases.

    摘要翻译： 由下式表示的芳族杂环衍生物：其中Z为下式表示的基团：其中Ar1为苯基或被卤素原子或1〜5个碳原子的烷基取代的苯基，R2为烷基 1〜5个碳原子，Y为氢原子，巯基，1〜5个碳原子的烷硫基，氨基或被一个或两个碳原子数为1〜5的烷基取代的氨基，Ar2为 选自卤素原子，1〜5个碳原子的烷基，1〜5个碳原子的烷氧基，羟基和三氟甲基，或苯基中的一个或两个取代基的苯基 ，B1-B2为CH-CO或C = C（R1）（其中R1为氢原子或1〜5个碳原子的烷基），n为1〜4的整数，或其药学上可接受的盐 ，其是具有抗精神病作用而不引起外敷的多巴胺D4受体拮抗剂化合物 痉挛性疾病

    Optically active substituted phenylalkylamine derivatives
    9.
    发明授权
    Optically active substituted phenylalkylamine derivatives 失效
    光学活性取代苯基烷基胺衍生物

    公开(公告)号：US5990151A

    公开(公告)日：1999-11-23

    申请号：US981539

    申请日：1998-05-15

    申请人： Atsuro Nakazato ,  Toshihito Kumagai ,  Tomoki Miyazawa ,  Koumei Ohta ,  Yutaka Kawashima ,  Katsuo Hatayama, deceased

    发明人： Atsuro Nakazato ,  Toshihito Kumagai ,  Tomoki Miyazawa ,  Koumei Ohta ,  Yutaka Kawashima ,  Katsuo Hatayama, deceased

    IPC分类号： C07C217/60 ,  C07C217/62 ,  C07C271/16 ,  C07D333/16 ,  A61K31/135 ,  A61K31/38 ,  C07D333/06

    CPC分类号： C07C271/16 ,  C07C217/60 ,  C07C217/62 ,  C07D333/16

    摘要： The present invention relates to an optically active, substituted phenylalkylamine derivative represented by Formula [1]: ##STR1## wherein A is a substituted or non-substituted phenyl or thienyl; X.sup.1 is hydrogen, halogen, hydroxyl or a substituted or non-substituted C.sub.1-5 alkoxy; R.sup.1 and R.sup.2 are equally or differently hydrogen, C.sub.1-7 alkyl, C.sub.3-7 alkenyl or C.sub.3-7 alkynyl; R.sup.3 is C.sub.1-10 alkyl, C.sub.2-10 alkenyl or C.sub.2-10 alkynyl; n is an integer from 2 to 5; and m is an integer from 1 to 4,or a pharmaceutically acceptable salt thereof, and pharmaceutical use of such compound or salt. The compound of the invention is excellent in sigma 1 receptor antagonism and useful for treating schizophrenia, depression, anxiety, cerebrovascular diseases/senile troublesome behaviors, and cognitive dysfunctions and motor dysfunctions such as Alzheimer's disease, Parkinson's disease and Huntington's disease which are neurodegenerative diseases. Further, the compound of the invention is also useful for treating dependence resulted from drug abuse.

    摘要翻译： PCT No.PCT / JP96 / 01613 Sec。 371日期：1998年5月15日 102（e）日期1998年5月15日PCT提交1996年6月13日PCT公布。 出版物WO97 / 00238 日本1997年1月3日本发明涉及由式[1]表示的光学活性的取代的苯基烷基胺衍生物：其中A是取代或未取代的苯基或噻吩基; X 1为氢，卤素，羟基或取代或未取代的C 1-5烷氧基; R1和R2同等或不同，氢，C1-7烷基，C3-7烯基或C3-7炔基; R3是C1-10烷基，C2-10烯基或C2-10炔基; n是2至5的整数; m为1〜4的整数，或其药学上可接受的盐，以及该化合物或其盐的药物用途。 本发明化合物在σ1受体拮抗作用方面优异，可用于治疗精神分裂症，抑郁症，焦虑症，脑血管疾病/老年麻醉行为，以及认知功能障碍和运动功能障碍如阿尔茨海默氏病，帕金森病和亨廷顿舞蹈病，这些疾病均为神经变性疾病。 此外，本发明的化合物还可用于治疗药物滥用引起的依赖性。

    Carboxylic acid derivatives and process for producing the same
    10.
    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]。