TGF-β superfamily production/secretion promoter
    11.
    发明授权
    TGF-β superfamily production/secretion promoter 失效
    TGF-β超家族生产/分泌启动子

    公开(公告)号:US07498352B2

    公开(公告)日:2009-03-03

    申请号:US10480849

    申请日:2002-06-25

    IPC分类号: A61K31/42 C07D263/30

    CPC分类号: A61K31/422

    摘要: The present invention provides a TGF-β superfamily production/secretion promoter comprising a compound represented by the formula wherein R1 is a halogen atom, an optionally substituted heterocyclic group, an optionally substituted hydroxy group, an optionally substituted thiol group or an optionally substituted amino group; A is an optionally substituted acyl group, an optionally substituted heterocyclic group, an optionally substituted hydroxy group or an optionally esterified or amidated carboxyl group; B is an optionally substituted aromatic group; X is an oxygen atom, a sulfur atom or an optionally substituted nitrogen atom; and Y is a divalent hydrocarbon group or heterocyclic group, or a salt thereof or a prodrug thereof, which is useful as an agent for the prophylaxis or treatment of dysautonomia, bladder dysfunction, hearing impairment, bone disease and the like.

    摘要翻译: 本发明提供了包含下式表示的化合物的TGF-β超家族产生/分泌促进剂,其中R1是卤素原子,任选取代的杂环基,任选取代的羟基,任选取代的硫醇基或任选取代的氨基 ; A是任选取代的酰基,任选取代的杂环基,任选取代的羟基或任选酯化或酰胺化的羧基; B是任选取代的芳基; X是氧原子,硫原子或任选取代的氮原子; Y是二价烃基或杂环基,或其盐或其前药,其可用作预防或治疗自主神经功能障碍,膀胱功能障碍,听力障碍,骨病等。

    Thiazole and oxazole VDAC regulator
    12.
    发明授权
    Thiazole and oxazole VDAC regulator 失效
    噻唑和恶唑VDAC调节剂

    公开(公告)号:US07462635B2

    公开(公告)日:2008-12-09

    申请号:US10507731

    申请日:2003-03-13

    摘要: The present invention provides a VDAC regulator comprising a compound represented by the formula (I): wherein R1 is a halogen atom, an optionally substituted heterocyclic group, an optionally substituted hydroxyl group, an optionally substituted thiol group or an optionally substituted amino group; A is an optionally substituted acyl group, an optionally substituted heterocyclic group, an optionally substituted hydroxyl group or an optionally esterified or amidated carboxyl group; B is an optionally substituted aromatic group; X is an oxygen atom, a sulfur atom or an optionally substituted nitrogen atom; and Y is a divalent hydrocarbon group or heterocyclic group; a salt thereof or a prodrug thereof, which is useful as an agent for the prophylaxis or treatment of Down's syndrome and the like.

    摘要翻译: 本发明提供一种VDAC调节剂,其包含由式(I)表示的化合物:其中R1是卤素原子,任选取代的杂环基,任选取代的羟基,任选取代的硫醇基或任选取代的氨基; A是任选取代的酰基,任选取代的杂环基,任选取代的羟基或任选酯化或酰胺化的羧基; B是任选取代的芳基; X是氧原子,硫原子或任选取代的氮原子; Y为二价烃基或杂环基; 其盐或其前药,其可用作预防或治疗唐氏综合征等的药剂。

    Agent for preventing or treating organ functional disorders and organ dysfunction
    13.
    发明申请
    Agent for preventing or treating organ functional disorders and organ dysfunction 审中-公开
    用于预防或治疗器官功能障碍和器官功能障碍的药剂

    公开(公告)号:US20060241096A1

    公开(公告)日:2006-10-26

    申请号:US11473560

    申请日:2006-06-23

    IPC分类号: A61K31/553

    摘要: The present invention provides an agent for preventing or treating organ functional disorders, an agent for preventing or treating organ dysfunction and an agent for preventing or treating obesity and deuteropathy thereof, each of which comprises a compound having an effect of increasing ubiquinone or a salt thereof or a prodrug thereof; as well as a ubiquinone increasing agent comprising a compound having a squalene synthase inhibitory effect or a salt thereof or a prodrug thereof.

    摘要翻译: 本发明提供了用于预防或治疗器官功能障碍的药剂,用于预防或治疗器官功能障碍的药剂和用于预防或治疗肥胖症及其脱发病的药剂,其各自包括具有增加泛醌或其盐的作用的化合物 或其前药; 以及含有具有角鲨烯合酶抑制作用的化合物或其前体药物的泛醌增加剂。

    Fused imidazopyridine derivatives as antihyperlipidemic agents
    14.
    发明授权
    Fused imidazopyridine derivatives as antihyperlipidemic agents 失效
    融合的咪唑并吡啶衍生物作为抗高血脂药物

    公开(公告)号:US06235731B1

    公开(公告)日:2001-05-22

    申请号:US09155889

    申请日:1998-10-08

    IPC分类号: A61K31549

    CPC分类号: C07D513/16

    摘要: A novel compound of the formula: wherein ring Q is an optionally substituted pyridine ring; One of R0, R1 and R2 is —Y0—Z0, and the other tow groups are a hydrogen, a halogen, an optionally substituted hydroxy group, a hydrocarbon group that may be an optionally substituted hydrocarbon group or an acyl group; Y0 is a bond or an optionally substituted bivalent hydrocarbon group; Z0 is a basic group which may be bonded via oxygen, nitrogen, —CO—, —CS—, —SO2N(R3)— (where R3 is hydrogen or an optionally substituted hydrocarbon group), or S(O)n (wherein n is to 0, 1 or 2); ......... is a single bond or a double bond, or a salt thereof, which has an excellent LDL receptor up-regulating, blood-lipids lowering, blood-sugar lowering and diabetic complication-ameliorating activity.

    摘要翻译: 一种下式的新化合物:其中环Q是任选取代的吡啶环; R 0,R 1和R 2之一是-YO-Z 0,其它的三个基团是氢,卤素,任选取代的羟基,烃 可以是任意取代的烃基或酰基的基团; Y 0是一个键或任意取代的二价烃基; Z 0是可以通过氧,氮,-CO-,-CS-,-SO 2 N键合的碱性基团 (R 3) - (其中R 3是氢或任选取代的烃基)或S(O)n(其中n是0,1或2); .........是单键或 双键或其盐,其具有优异的LDL受体上调,血脂降低,血糖降低和糖尿病并发症改善活性。

    Benzoxazepine compounds, their production and use
    18.
    发明授权
    Benzoxazepine compounds, their production and use 失效
    苯并西泮化合物,其生产和使用

    公开(公告)号:US06613761B1

    公开(公告)日:2003-09-02

    申请号:US09587947

    申请日:2000-06-06

    IPC分类号: A61K3155

    摘要: This invention provides new benzoxazepine compounds represented by the formula: [wherein R stands for a lower alkyl group optionally substituted with a hydroxyl group, X stands for an optionally substituted carbamoyl group or an optionally substituted heterocyclic group having a deprotonatable hydrogen atom, R1 stands for a lower alkyl group and W stands for a halogen atom] having activities of lowering cholesterol-level and lowering trigluceride-level, and being useful for prophylaxis and therapy of hyperlipidemia.

    摘要翻译: 本发明提供由下式表示的新的苯并氧氮杂化合物:其中R代表任选被羟基取代的低级烷基,X代表任选取代的氨基甲酰基或具有可去质子化的氢原子的任意取代的杂环基,R1代表 低级烷基,W代表卤素原子]具有降低胆固醇水平和降低三倍体水平的活性,并且可用于预防和治疗高脂血症。

    Condensed cyclic compounds and their use
    20.
    发明授权
    Condensed cyclic compounds and their use 失效
    缩合的环状化合物及其用途

    公开(公告)号:US5698691A

    公开(公告)日:1997-12-16

    申请号:US311932

    申请日:1994-09-26

    摘要: Disclosed is a squalene synthetase inhibitor which comprises the compound represented by the formula ##STR1## wherein R.sub.1 is hydrogen or an optionally substituted hydrocarbon group; R.sub.2 is hydrogen, an optionally substituted alkyl group, an optionally substituted phenyl group or an optionally substituted aromatic heterocyclic ring group; X' is a substituent comprising an optionally esterified carboxyl group, an optionally substituted carbamoyl group, an optionally substituted hydroxyl group, an optionally substituted amino group or an optionally substituted heterocyclic radical having a protonizable hydrogen; Ring A is an optionally substituted benzene ring or an optionally substituted aromatic heterocyclic ring; Ring J' is a 7- to 8-membered heterocyclic ring containing at most three ring constituting hetero atoms; D is C or N; the Ring J' optionally having, besides R.sub.1, R.sub.2 and X', a further substituent; provided that the condensed ring composed of Ring A and ring J' is not a 2-oxo-1,2,3,5-tetrahydro-4,1-benzoxazepine ring, or a pharmaceutically acceptable salt thereof, and which is useful for the prophylaxis or therapy of hypercholesteremia or coronary sclerosis of mammals.

    摘要翻译: 公开了一种角鲨烯合成酶抑制剂,其包含由通式取代的烃基表示的化合物; R2是氢,任选取代的烷基,任选取代的苯基或任选取代的芳族杂环基; X'是包含任选酯化的羧基,任选取代的氨基甲酰基,任选取代的羟基,任选取代的氨基或具有可质子化氢的任选取代的杂环基的取代基; 环A是任选取代的苯环或任选取代的芳族杂环; 环J'是含有至多三个环构成杂原子的7-至8-元杂环; D为C或N; 除了R1,R2和X'之外,环J'还可以具有另外的取代基; 条件是由环A和环J'组成的稠环不是2-氧代-1,2,3,5-四氢-4,1-苯并氧氮杂环,或其药学上可接受的盐,并且其可用于 预防或治疗哺乳动物的高胆固醇血症或冠状动脉硬化。