Imidazoquinazoline derivatives
    11.
    发明授权
    Imidazoquinazoline derivatives 失效
    咪唑喹唑啉衍生物

    公开(公告)号:US6127541A

    公开(公告)日:2000-10-03

    申请号:US65061

    申请日:1998-04-27

    CPC classification number: C07D487/04

    Abstract: Imidazoquinoline derivatives of the formula ##STR1## (wherein X may be O or S) provide selective cyclic guanosine 3',5' monophosphate (cGMP)--specific phosphodiesterase (PDE) inhibitory activity. The compounds are useful for treating or ameliorating cardiovascular disease such as thrombosis, angina pectoris, hypertension, heart failure and arterial sclerosis, as well as asthma, impotence and the like.

    Abstract translation: PCT No.PCT / JP97 / 03023 Sec。 371日期:1998年4月27日 102(e)日期1998年4月27日PCT 1997年8月29日PCT公布。 出版物WO98 / 08848 日期:1998年3月5日式(其中X可以是O或S)的咪唑并喹啉衍生物提供选择性环状鸟苷3',5'单磷酸(cGMP)特异性磷酸二酯酶(PDE)抑制活性。 该化合物可用于治疗或改善心血管疾病如血栓形成,心绞痛,高血压,心力衰竭和动脉硬化,以及哮喘,阳ence等。

    Quinazoline derivatives as kinase inhibitors
    16.
    发明授权
    Quinazoline derivatives as kinase inhibitors 失效
    喹唑啉衍生物作为激酶抑制剂

    公开(公告)号:US08324205B2

    公开(公告)日:2012-12-04

    申请号:US12471280

    申请日:2009-05-22

    CPC classification number: C07D239/94 A61K31/517 C07D401/12 C07D403/12

    Abstract: The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.

    Abstract translation: 本发明涉及对抑制这种激酶活性的激酶磷酸化具有抑制活性的含氮杂环化合物及其药学上可接受的盐。 本发明还涉及通过抑制激酶的磷酸化来抑制哺乳动物的激酶和治疗疾病状态的方法。 在一个特定方面,本发明提供了抑制PDGF受体的磷酸化以阻止异常细胞生长和细胞游动的含氮杂环化合物及其药学上可接受的盐,以及预防或治疗细胞增殖性疾病如动脉硬化,血管 重建,癌症和肾小球硬化症。

    Quinazoline derivatives as kinase inhibitors
    18.
    发明授权
    Quinazoline derivatives as kinase inhibitors 失效
    喹唑啉衍生物作为激酶抑制剂

    公开(公告)号:US06982266B2

    公开(公告)日:2006-01-03

    申请号:US10344736

    申请日:2001-08-17

    CPC classification number: C07D239/94 A61K31/517 C07D401/12 C07D403/12

    Abstract: The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.

    Abstract translation: 本发明涉及对抑制这种激酶活性的激酶磷酸化具有抑制活性的含氮杂环化合物及其药学上可接受的盐。 本发明还涉及通过抑制激酶的磷酸化来抑制哺乳动物的激酶和治疗疾病状态的方法。 在一个特定方面,本发明提供了抑制PDGF受体的磷酸化以阻止异常细胞生长和细胞游动的含氮杂环化合物及其药学上可接受的盐,以及用于预防或治疗细胞增殖性疾病如动脉硬化的方法 ,血管重构,癌症和肾小球硬化症。

    Nitrogenous heterocylic compounds
    19.
    发明授权
    Nitrogenous heterocylic compounds 失效
    含氮杂环化合物

    公开(公告)号:US06956039B2

    公开(公告)日:2005-10-18

    申请号:US10344737

    申请日:2001-08-17

    CPC classification number: C07D401/12 C07D239/94 C07D403/12

    Abstract: The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.

    Abstract translation: 本发明涉及对抑制这种激酶活性的激酶磷酸化具有抑制活性的含氮杂环化合物及其药学上可接受的盐。 本发明还涉及通过抑制激酶的磷酸化来抑制哺乳动物的激酶和治疗疾病状态的方法。 在一个特定方面,本发明提供了抑制PDGF受体的磷酸化以阻止异常细胞生长和细胞游动的含氮杂环化合物及其药学上可接受的盐,以及预防或治疗细胞增殖性疾病如动脉硬化,血管 重建,癌症和肾小球硬化症。

    Derivatives of benzofuran or benzodioxole
    20.
    发明授权
    Derivatives of benzofuran or benzodioxole 失效
    苯并呋喃或苯并间二氧杂环戊烯的衍生物

    公开(公告)号:US06514996B2

    公开(公告)日:2003-02-04

    申请号:US08974739

    申请日:1997-11-19

    Abstract: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)—C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z represents CONH, CONHCH2, or a bond), or N], or (iii) a bond; and R5 represents aryl, an aromatic heterocyclic group, cycloalkyl, pyridine-N-oxide, cyano, or lower alkoxycarbonyl; or pharmaceutically acceptable salts thereof.

    Abstract translation: 由下式(I)表示的含氧杂环化合物:其中R1和R2独立地表示氢,低级烷基,氰基, - (CH2)n-E1-CO-G1(其中E1表示键,O或NH; 并且G 1表示氢,取代或未取代的低级烷基,OR 6或NR 7 R 8; n表示0〜4的整数)等。 R 1和R 2组合​​在一起,与邻近的碳原子一起代表饱和碳环; 或R 2,R 11或R 13组合形成单键; R3表示氢,苯基或卤素; R4代表羟基,低级烷氧基等; A表示-C(R 9)(R 10) - 或O; B表示O,NR 11,-C(R 12)(R 13) - 或-C(R 14)(R 15)-C(R 16)(R 17) - ; D表示(i)-C(R 18)(R 19)-X-(其中X表示-C(R 21)(R 22) - ,S或NR 23),(ⅱ)-C(R 19a)= Y- [Y -C(R 24)-Z-(其中Z表示CONH,CONHCH 2或键)或N]或(iii)键; R5表示芳基,芳香族杂环基,环烷基,吡啶-N-氧化物,氰基或低级烷氧基羰基; 或其药学上可接受的盐。

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