Carbamoyl tetrahydropyridine derivatives
    2.
    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

    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。

    2-Phenoxyaniline derivatives
    3.
    发明授权
    2-Phenoxyaniline derivatives 有权
    2-苯氧基苯胺衍生物

    公开(公告)号:US6162832A

    公开(公告)日:2000-12-19

    申请号:US529218

    申请日:2000-04-10

    IPC分类号: C07C217/90 A61K31/135

    CPC分类号: C07C217/90

    摘要: A 2-phenoxyaniline derivative represented by the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or a lower alkoxy group, R.sup.2 is a halogen atom or a nitro group, and R.sup.3 is a hydrogen atom or a halogen atom, or a pharmaceutically acceptable salt thereof.

    摘要翻译: PCT No.PCT / JP98 / 04729 Sec。 371日期2000年04月10日 102(e)日期2000年4月10日PCT提交1998年10月20日PCT公布。 公开号WO99 /​​ 20598 日期1999年4月29日由下式表示的2-苯氧基苯胺衍生物:其中R1是氢原子或低级烷氧基,R2是卤素原子或硝基,R3是氢原子或卤原子,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

    IPC分类号: C07D47334

    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

    IPC分类号: C07D40106

    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
    7.
    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

    IPC分类号: C07D41706

    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

    Method for production of cis-4-fluoro-L-proline derivatives
    8.
    发明授权
    Method for production of cis-4-fluoro-L-proline derivatives 失效
    顺式-4-氟-L-脯氨酸衍生物的制备方法

    公开(公告)号:US07279584B2

    公开(公告)日:2007-10-09

    申请号:US10568708

    申请日:2004-08-18

    IPC分类号: C07D207/16

    CPC分类号: C07D207/16 Y02P20/55

    摘要: The present invention provides a safer method for production of a cis-4-fluoro-L-proline derivative under milder conditions and in good yield to give a product of high purity on an industrial scale at low cost. Namely, the present invention provides a method for producing a cis-4-fluoro-L-proline derivative, which comprises reacting a trans-4-hydroxy-L-proline derivative of the following Formula [I]: (wherein R1 represents a protecting group for an α-amino group, and R2 represents a protecting group for a carboxyl group) with N,N-diethyl-N-(1,1,2,3,3,3-hexafluoropropyl)amine in the presence of a hydrogen fluoride-scavenger.

    摘要翻译: 本发明提供了一种在更温和的条件下生产顺式-4-氟-L-脯氨酸衍生物的更安全的方法,并以良好的产率,以低成本在工业规模上得到高纯度的产物。 即,本发明提供顺式-4-氟-L-脯氨酸衍生物的制造方法,该方法包括使下式[I]的反式-4-羟基-L-脯氨酸衍生物:其中R < 1代表α-氨基的保护基,R 2代表羧基的保护基)与N,N-二乙基-N-(1,1,2 ,3,3,3-六氟丙基)胺在氟化氢 - 清除剂的存在下反应。

    Process for production of cis-4-fluoro-l-proline derivatives
    9.
    发明申请
    Process for production of cis-4-fluoro-l-proline derivatives 失效
    顺式-4-氟-1-脯氨酸衍生物的制备方法

    公开(公告)号:US20060281927A1

    公开(公告)日:2006-12-14

    申请号:US10568708

    申请日:2004-08-18

    IPC分类号: C07D207/02

    CPC分类号: C07D207/16 Y02P20/55

    摘要: The present invention provides a safer method for production of a cis-4-fluoro-L-proline derivative under milder conditions and in good yield to give a product of high purity on an industrial scale at low cost. Namely, the present invention provides a method for producing a cis-4-fluoro-L-proline derivative, which comprises reacting a trans-4-hydroxy-L-proline derivative of the following Formula [I]: (wherein R1 represents a protecting group for an α-amino group, and R2 represents a protecting group for a carboxyl group) with N,N-diethyl-N-(1,1,2,3,3,3-hexafluoropropyl)amine in the presence of a hydrogen fluoride-scavenger.

    摘要翻译: 本发明提供了一种在更温和的条件下生产顺式-4-氟-L-脯氨酸衍生物的更安全的方法,并以良好的产率,以低成本在工业规模上得到高纯度的产物。 即,本发明提供顺式-4-氟-L-脯氨酸衍生物的制造方法,该方法包括使下式[I]的反式-4-羟基-L-脯氨酸衍生物:其中R < 1代表α-氨基的保护基,R 2代表羧基的保护基)与N,N-二乙基-N-(1,1,2 ,3,3,3-六氟丙基)胺在氟化氢 - 清除剂的存在下反应。