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    Carbamoyl tetrahydropyridine derivatives
    1.
    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。

    1,2-Dihydro-2-oxoquinoline derivatives
    2.
    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：US06329525B1

    公开(公告)日：2001-12-11

    申请号：US09555568

    申请日：2000-06-01

    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： C07D215227

    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，各自为氢原子，C1-5烷基，C1-5烷氧基或卤素原子，或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。

    Nitrogen-containing tetracyclic compounds
    3.
    发明授权
    Nitrogen-containing tetracyclic compounds 失效
    含氮四环化合物

    公开(公告)号：US06281355B1

    公开(公告)日：2001-08-28

    申请号：US09555570

    申请日：2000-06-01

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

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

    IPC分类号： A61K31403

    CPC分类号： C07D471/04 ,  C07D495/04

    摘要： A nitrogen-containing tetracyclic compound represented by the formula: wherein Y1—Y2—Y3 is N—C═N or a group represented by the formula: C═C—NR3 (wherein R3 is a hydrogen atom, a C1-5 alkyl group or a nitrogen-containing C2-10 alkyl group), Y4 is S, SO, SO2, CH2 or a group represented by the formula: NR4 (wherein R4 is a C1-5 alkanoyl group or a C1-5 alkyl group), 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, and n is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 一种由下式表示的含氮四环化合物：其中Y1-Y2-Y3为NC = N或由下式表示的基团：C = C-NR3（其中R3为氢原子，C1-5烷基或 含氮的C2-10烷基），Y4是S，SO，SO2，CH2或由下式表示的基团：NR4（其中R4是C1-5烷酰基或C1-5烷基），R1和R2 各自为氢原子，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，X1和X2相同或不同，分别为氢原子，C1-5烷基，C1-5烷氧基或卤素原子，n为0,1或2; 或其药学上可接受的盐。

    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：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
    5.
    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。

    4-Tetrahydropyridylpyrimidine derivatives
    6.
    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。

    Carboxylic acid derivatives and process for producing the same
    9.
    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]。

    Carboxylic acid derivatives and process for producing same
    10.
    发明授权
    Carboxylic acid derivatives and process for producing same 失效
    羧酸衍生物及其制备方法

    公开(公告)号：US06479674B1

    公开(公告)日：2002-11-12

    申请号：US09937212

    申请日：2001-09-24

    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： C07D31500

    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]。