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    4-Tetrahydropyridylpyrimidine derivatives
    1.
    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。

    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。

    1,2-dihydro-2-oxoquinoline derivatives
    4.
    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

    2-carbonylthiazole derivatives and use of the same
    9.
    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。