Tricyclic compounds, their production and use
    1.
    发明授权
    Tricyclic compounds, their production and use 有权
    三环化合物,其生产和使用

    公开(公告)号:US06218429B1

    公开(公告)日:2001-04-17

    申请号:US09309519

    申请日:1999-05-10

    IPC分类号: A01N34308

    摘要: A compound of the formula: wherein R1 is an optionally substituted hydrocarbon, amino or heterocyclic group; R2 is H or an optionally substituted hydrocarbon group; R3 is H or an optionally substituted hydrocarbon or heterocyclic group; X is CHR4, NR4, O or S in which R4 is H or an optionally substituted hydrocarbon group; Y is C, CH or N; ring A is optionally substituted 5- to 7-membered ring; ring B is an optionally substituted benzene ring; and m is 1 to 4, or a salt thereof, a process for producing it, an intermediate for the production and a pharmaceutical composition comprising it are provided.

    摘要翻译: 下式的化合物:其中R 1是任选取代的烃,氨基或杂环基; R2是H或任选取代的烃基; R3是H或任选取代的烃或杂环基; X是CHR 4,NR 4,O或S,其中R 4是H或任选取代的烃基; Y为C,CH或N; 环A为任选取代的5-至7-元环; 环B是任选取代的苯环; 和m为1至4,或其盐,其制备方法,制备中间体和包含其的药物组合物。

    Tricyclic compounds, their production and use
    2.
    发明授权
    Tricyclic compounds, their production and use 失效
    三环化合物,其生产和使用

    公开(公告)号:US6034239A

    公开(公告)日:2000-03-07

    申请号:US812168

    申请日:1997-03-06

    摘要: A compound of the formula: ##STR1## wherein R.sup.1 is an optionally substituted hydrocarbon, amino or heterocyclic group; R.sup.2 is H or an optionally substituted hydrocarbon group; R.sup.3 is H or an optionally substituted hydrocarbon or heterocyclic group; X is CHR.sup.4, NR.sup.4, O or S in which R.sup.4 is H or an optionally substituted hydrocarbon group; Y is C, CH or N; ring A is optionally substituted 5- to 7-membered ring; ring B is an optionally substituted benzene ring; and m is 1 to 4, or a salt thereof, a process for producing it, an intermediate for the production and a pharmaceutical composition comprising it are provided.

    摘要翻译: 下式的化合物:其中R 1是任选取代的烃,氨基或杂环基; R2是H或任选取代的烃基; R3是H或任选取代的烃或杂环基; X是CHR 4,NR 4,O或S,其中R 4是H或任选取代的烃基; Y为C,CH或N; 环A为任选取代的5-至7-元环; 环B是任选取代的苯环; 和m为1至4,或其盐,其制备方法,制备中间体和包含其的药物组合物。

    Quinolines, their production and use
    5.
    发明授权
    Quinolines, their production and use 失效
    喹啉,其生产和使用

    公开(公告)号:US5708005A

    公开(公告)日:1998-01-13

    申请号:US718430

    申请日:1996-12-10

    摘要: A compound of the formula: ##STR1## wherein R.sup.1 represents hydrogen or an optionally substituted hydrocarbon group; R.sup.2 represents an optionally substituted hydrocarbon group, an optionally substituted amino group or a substituted hydroxyl group; X represents an optionally halogenated lower alkylene group; Y represents a substituent; n represents an integer of 0 to 6; and m represents 0 or 1; or a salt thereof, a process for producing it, an intermediate for the production, and a pharmaceutical composition containing it are provided.

    摘要翻译: PCT No.PCT / JP96 / 01759 Sec。 371日期1996年12月10日第 102(e)日期1996年12月10日PCT提交1996年6月26日PCT公布。 公开号WO97 / 01539 日期1997年1月16日具有下式的化合物:其中R 1表示氢或任选取代的烃基; R2表示任选取代的烃基,任选取代的氨基或取代的羟基; X表示任选卤代的低级亚烷基; Y表示取代基; n表示0〜6的整数, m表示0或1; 或其盐,其制备方法,制备中间体和含有它的药物组合物。

    Cyclic ether compounds as sodium channel modulators
    6.
    发明授权
    Cyclic ether compounds as sodium channel modulators 失效
    环状醚化合物作为钠通道调节剂

    公开(公告)号:US06172085B2

    公开(公告)日:2001-01-09

    申请号:US09242067

    申请日:1999-02-08

    IPC分类号: C07D40506

    摘要: A compound of the formula: wherein R1 and R2 each represents hydrogen, lower alkyl which may be substituted or acyl; R3, R4 and R5 each represents lower alkyl which may be substituted or lower alkoxy which may be substituted or R4 and R5 taken together represent a 5- or 6-membered carbocyclic group; R6 represents lower alkyl; Ar represents an aromatic group which may be substituted; ring A represents a 5- to 8-membered nitrogen-containing heterocyclic ring which may be substituted; X represents lower alkylene which may be substituted; Y represents carbon or nitrogen; Za represents CH2, COCH2, OCH2, SCH2, NHCH2, etc.; Zb represents a bond or a divalent aliphatic hydrocarbon group which may be substituted and may contain O, N or S; and m represents an integer of 1 to 3, or a salt thereof is useful for a pharmaceutical composition for modulating sodium channel.

    摘要翻译: 下式的化合物:其中R1和R2各自表示氢,可被取代的或低级烷基的酰基; R 3,R 4和R 5各自表示可以被取代的低级烷基或可被取代的低级烷氧基,或者R 4和R 5一起代表5-或6-元碳环基; R6代表低级烷基; Ar表示可以被取代的芳基; 环A表示可以被取代的5至8元含氮杂环; X表示可以被取代的低级亚烷基; Y表示碳或氮; Za表示CH2,COCH2,OCH2,SCH2,NHCH2等; Zb表示可以被取代并可以含有O,N或S的键或二价脂族烃基; m表示1〜3的整数,或其盐可用于调制钠通道的药物组合物。

    Antidepressant
    7.
    发明授权
    Antidepressant 失效
    抗抑郁药

    公开(公告)号:US07750037B2

    公开(公告)日:2010-07-06

    申请号:US11475539

    申请日:2006-06-27

    IPC分类号: A61K31/4035 C07D405/02

    摘要: A PKB (Akt) activating agent comprising a compound represented by the formula (I): wherein R1 and R2: H, a hydrocarbon group or a heterocyclic group or R1 and R2 form a ring in cooperation with the adjacent carbon atom; R3: H, a hydrocarbon group or a heterocyclic group; W: represents a group represented by the formulas: wherein ring A: an optionally substituted benzene ring; ring B: an optionally substituted 5- to 7-membered nitrogen-containing heterocycle; R4: an aliphatic hydrocarbon group substituted with an aromatic group and further optionally substituted, or an acyl group containing an aromatic group; R5: H, C1-6 alkyl or acyl; R4c: an aromatic group, an aliphatic hydrocarbon group or acyl; and X: O or S; Y: O, S or NH; and ring C: an optionally substituted benzene ring, or a salt or a prodrug thereof, and use of the activating agent in prevention or treatment of depression, anxiety, manic-depressive psychosis or PTSD are provided.

    摘要翻译: 一种PKB(Akt)活化剂,其包含由式(I)表示的化合物:其中R1和R2:H,烃基或杂环基或R1和R2与相邻碳原子一起形成环; R3:H,烃基或杂环基; W:表示由下式表示的基团:其中环A:任选取代的苯环; 环B:任选取代的5-至7-元含氮杂环; R4:被芳基取代并进一步任选取代的脂族烃基或含芳基的酰基; R5:H,C1-6烷基或酰基; R4c:芳基,脂族烃基或酰基; 和X:O或S; Y:O,S或NH; 和环C:任选取代的苯环,或其盐或前药,并且提供了用于预防或治疗抑郁,焦虑,躁狂抑郁性精神病或PTSD的活化剂。

    Antidepressant
    8.
    发明申请
    Antidepressant 审中-公开
    抗抑郁药

    公开(公告)号:US20050148650A1

    公开(公告)日:2005-07-07

    申请号:US10506269

    申请日:2003-02-28

    摘要: A PKB (Akt) activating agent comprising a compound represented by the formula (I): wherein R1 and R2: H, a hydrocarbon group or a heterocyclic group or R1 and R2 form a ring in cooperation with the adjacent carbon atom; R3: H, a hydrocarbon group or a heterocyclic group; W: represents a group represented by the formulas: wherein ring A: an optionally substituted benzene ring; ring B: an optionally substituted 5- to 7-membered nitrogen-containing heterocycle; R4: an aliphatic hydrocarbon group substituted with an aromatic group and further optionally substituted, or an acyl group containing an aromatic group; R5: H, C1-6 alkyl or acyl; R4c: an aromatic group, an aliphatic hydrocarbon group or acyl; and X:O or S; Y:O, S or NH; and ring C: an optionally substituted benzene ring, or a salt or a prodrug thereof, and use of the activating agent in prevention or treatment of depression, anxiety, manic-depressive psychosis or PTSD are provided.

    摘要翻译: 一种PKB(Akt)活化剂,其包含由式(I)表示的化合物:其中R 1和R 2:H,烃基或杂环基或R 与相邻的碳原子一起形成环;和<! - SIPO

    Benzo-fused 5-membered hetrocycle compounds, process for preparation of the same, and use thereof
    9.
    发明授权
    Benzo-fused 5-membered hetrocycle compounds, process for preparation of the same, and use thereof 失效
    苯并稠合的5元杂环化合物,其制备方法及其用途

    公开(公告)号:US07208495B2

    公开(公告)日:2007-04-24

    申请号:US10481367

    申请日:2002-07-04

    摘要: A compound represented by the formula: (wherein, R1 and R2 are the same or different and each represents a hydrogen atom, hydrocarbon group or heterocyclic group, or R1 and R2 may form, together with the adjacent carbon atom, a 3–8 membered iso- or heterocyclic group, R3 represents a cyclic group, a hydroxy group, a mercapto group that may have oxo, or an amino group, R4 represents a hydrogen atom, a hydrocarbon group, a hydroxy group, a mercapto group which may have oxo, or an amino group, or R2 and R4 may link together to form a double bond, X represents a bond or a linear hydrocarbon group, W represents an oxygen atom or a sulfur atom, ring B represents a 5–8 membered nitrogen-containing heterocyclic group, ring C represents a benzene ring, and— represents a single bond or a double bond), or a salt or a prodrug thereof that has excellent neurodegenerative inhibitory activity and brain penetrability, and is useful as an agent for preventing/treating neurodegenerative diseases.

    摘要翻译: 由下式表示的化合物(其中,R 1和R 2相同或不同,各自表示氢原子,烃基或杂环基, 可以与相邻的碳原子一起形成3-8元的异或杂环基,R 3表示环状 基团,羟基,可具有氧代基的巯基或氨基,R 4表示氢原子,烃基,羟基,可具有氧代基的巯基,或 氨基或R 2和R 4可以连接在一起形成双键,X表示键或直链烃基,W表示氧原子或 硫原子,环B表示5-8元含氮杂环基,环C表示苯环,代表单键或双键)或其盐或前药具有优异的神经变性抑制活性, 脑穿透性 并且可用作预防/治疗神经变性疾病的药剂。

    Benzo-fused 5-membered heterocyclic compounds, their production and use
    10.
    发明申请
    Benzo-fused 5-membered heterocyclic compounds, their production and use 审中-公开
    苯并稠合的5元杂环化合物,其生产和使用

    公开(公告)号:US20070149558A1

    公开(公告)日:2007-06-28

    申请号:US11679257

    申请日:2007-02-27

    IPC分类号: A61K31/4747 A61K31/407

    摘要: A compound represented by the formula: (wherein, R1 and R2 are the same or different and each represents a hydrogen atom, hydrocarbon group or heterocyclic group, or R1 and R2 may form, together with the adjacent carbon atom, a 3-8 membered iso- or heterocyclic group, R3 represents a cyclic group, a hydroxy group, a mercapto group that may have oxo, or an amino group, R4 represents a hydrogen atom, a hydrocarbon group, a hydroxy group, a mercapto group which may have oxo, or an amino group, or R2 and R4 may link together to form a double bond, X represents a bond or a linear hydrocarbon group, W represents an oxygen atom or a sulfur atom, ring B represents a 5-8 membered nitrogen-containing heterocyclic group, ring C represents a benzene ring, and represents a single bond or a double bond), or a salt or a prodrug thereof that has excellent neurodegenerative inhibitory activity and brain penetrability, and is useful as an agent for preventing/treating neurodegenerative diseases.

    摘要翻译: 由下式表示的化合物(其中,R 1和R 2相同或不同,各自表示氢原子,烃基或杂环基, 可以与相邻的碳原子一起形成3-8元的异或杂环基,R 3表示环状 基团,羟基,可具有氧代基的巯基或氨基,R 4表示氢原子,烃基,羟基,可具有氧代基的巯基,或 氨基或R 2和R 4可以连接在一起形成双键,X表示键或直链烃基,W表示氧原子或 硫原子,环B表示5-8元含氮杂环基,环C表示苯环,并且表示单键或双键)或其具有优异的神经变性抑制活性和脑渗透性的盐或其前药,并且可用作预防/治疗神经变性疾病的药剂。