Antidepressant
    2.
    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
    3.
    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

    Tricyclic compounds, their production and use
    6.
    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:US06248766B1

    公开(公告)日:2001-06-19

    申请号:US09254446

    申请日:1999-03-09

    IPC分类号: A61K31428

    摘要: A compound of the formula: wherein R1 is H or a substituent; m is 1-3; Ar is an aromatic group which may be substituted; X is a bond or a divalent straight-chain group having 1-6 atoms which may be substituted; Y is —S—, —O—, or —N(R2— (R2 is H or a substituent group), Z is —N═ or —C(R3)═ (R3 is H or a hydrocarbon group), ring A is a benzene ring; ring B is a 5- to 7-membered ring which may be substituted, or a salt thereof is useful for eliciting a prostaglandin I2 receptor agonistic effect.

    摘要翻译: 下式的化合物:其中R 1是H或取代基; m为1-3; Ar是可以被取代的芳基; X是可以被取代的具有1-6个原子的键或二价直链基团; Y是-S-,-O-或-N(R2-(R2是H或取代基),Z是-N =或-C(R3)=(R3是H或烃基),环A 是苯环;环B是可被取代的5-至7-元环,或其盐可用于引发前列腺素I2受体激动作用。

    Nitrosothiol derivatives and their use
    7.
    发明授权
    Nitrosothiol derivatives and their use 失效
    硝基苯酚衍生物及其用途

    公开(公告)号:US5116861A

    公开(公告)日:1992-05-26

    申请号:US562626

    申请日:1990-08-03

    摘要: Novel nitrosothiol derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.3 is a hydrogen atom, an acyl group or a hydrocarbon residue which may be substituted; X.sup.1 is a hydrogen atom, an acyl group, a lower alkoxy group or a hydrocarbon residue which may be substituted; X.sup.2 is an acyl group or a carboxyl group which may be esterified or which may form an amide; with proviso that when X.sup.2 is a carboxyl group X.sup.1 is not a hydrogen atom or acetyl group and that when both R.sup.1 and R.sup.2 are hydrogen atoms X.sup.1 is not acetyl group or .gamma.-glutamyl group, and salts thereof, show excellent hypotensive action, antiarrhythmic action, anti-anginal action, cardiotonic action or coronary vasodilation, thus being useful as therapeutic or prophylactic agents for the cardiovascular diseases such as hypertension and angina pectoris.

    5-pyridyl-1, 3-azole compounds, process for producing the same and use there of
    9.
    发明申请
    5-pyridyl-1, 3-azole compounds, process for producing the same and use there of 审中-公开
    5-吡啶基-1,3-唑化合物,其制备方法和用途

    公开(公告)号:US20090048307A1

    公开(公告)日:2009-02-19

    申请号:US11896072

    申请日:2007-08-29

    CPC分类号: C07D417/14 C07D417/04

    摘要: An optionally N-oxidized compound represented by the formula: wherein R1 represents hydrogen, hydrocarbon, heterocycle, amino, acyl, R2 represents an aromatic group, R3 represents hydrogen, pyridyl, aromatic hydrocarbon, X represents oxygen, optionally oxidized sulfur, Y represents a bond, an oxygen, optionally oxidized sulfur, a group represented by the formula NR4 (R4 represents hydrogen, hydrocarbon or acyl) and Z represents a bond or a divalent acyclic hydrocarbon, or a salt thereof has an excellent adenosine A3 receptor antagonistic activity and is used as an agent for preventing or treating diseases related to an adenosine A3 receptor. Furthermore, the compound (I) or a salt thereof has p38 MAP kinase inhibitory activity and TNF-α inhibitory activity and is used as an agent for preventing or treating diseases related to p38 MAP kinase and diseases related to TNF-α.

    摘要翻译: 由下式表示的任选的N-氧化化合物:其中R1表示氢,烃,杂环,氨基,酰基,R2表示芳族基团,R3表示氢,吡啶基,芳香烃,X表示氧,任选氧化的硫,Y表示 键,氧,任选氧化的硫,由式NR4表示的基团(R4表示氢,烃或酰基),Z表示键或二价无环烃或其盐具有优异的腺苷A3受体拮抗活性,并且为 用作预防或治疗与腺苷A3受体有关的疾病的药剂。 此外,化合物(I)或其盐具有p38 MAP激酶抑制活性和TNF-α抑制活性,并且用作预防或治疗与p38 MAP激酶相关的疾病和与TNF-α相关的疾病的药剂。