Nitrogenous heterocyclic compounds
    22.
    发明授权
    Nitrogenous heterocyclic compounds 有权
    含氮杂环化合物

    公开(公告)号:US06423716B1

    公开(公告)日:2002-07-23

    申请号:US09647490

    申请日:2000-09-29

    Abstract: The present invention relates to nitrogen-containing heterocyclic compounds represented by formula (I): wherein W represents 1,4-piperazinediyl, etc.; U represents NR1R2 (wherein R1 represents a hydrogen atom, a substituted or unsubstituted alkyl group, etc.; and R2 represents a hydrogen atom, etc. ), OR4, or SR5; V represents an oxygen atom, a sulfur atom, N—R6, or CR7R8, at least one of X, Y and Z represents a nitrogen atom, and the others are the same or different, and each represents a nitrogen atom or C—RA; and D1, D2, D3 and D4 each independently represent C—RB, a nitrogen atom, an oxygen atom, a sulfur atom, etc., optional adjoining two among D1 to D4 are combined to represent a nitrogen atom, N—R2A, an oxygen atom, a sulfur atom, etc., or optional adjoining two selected from D1 to D4 represent C—RB″ (wherein two RB″s are combined to represent substituted or unsubstituted alicyclic alkene, substituted or unsubstituted pyrrole, substituted or unsubstituted pyrazole, etc.; or pharmaceutically acceptable salts thereof.

    Abstract translation: 本发明涉及由式(I)表示的含氮杂环化合物:其中W表示1,4-哌嗪二基等; U表示NR1R2(其中R1表示氢原子,取代或未取代的烷基等; R2表示氢原子等),OR4或SR5; V表示氧原子,硫原子,N-R6或CR7R8,X,Y和Z中的至少一个表示氮原子,其它相同或不同,表示氮原子或C-RA ; D1,D2,D3和D4各自独立地表示C-RB,氮原子,氧原子,硫原子等,D1〜D4中任意相邻的2个相互组合,表示氮原子,N-R2A, 氧原子,硫原子等,或选自D1〜D4中任意相邻的2个表示C-RB“(其中两个RB'组合以代表取代或未取代的脂环族烯烃,取代或未取代的吡咯,取代或未取代的 吡唑等;或其药学上可接受的盐。

    Imidazoquinazoline derivatives
    23.
    发明授权
    Imidazoquinazoline derivatives 失效
    咪唑喹唑啉衍生物

    公开(公告)号:US5698560A

    公开(公告)日:1997-12-16

    申请号:US727598

    申请日:1996-10-23

    CPC classification number: C07D487/04

    Abstract: The present invention relates to imidazoquinazoline derivatives represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, cycloalkyl, lower alkenyl, substituted or unsubstituted aralkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroarylalkyl, or substituted or unsubstituted heteroaryl, R.sup.2 and R.sup.3 represent independently hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroarylalkyl, or substituted or unsubstituted heteroaryl, or R.sup.2 and R.sup.3 are combined to represent a heterocyclic group containing a nitrogen atom, R.sup.4 represents hydrogen or substituted or unsubstituted lower alkyl, X represents O or S, Y represents a single bond or O, n represents 0, 1, 2, or 3, and pharmaceutically acceptable salts thereof.

    Abstract translation: PCT No.PCT / JP96 / 00497 Sec。 371日期:1996年10月23日 102(e)日期1996年10月23日PCT 1996年3月1日PCT公布。 第WO96 / 26940号公报 日本1996年9月6日本发明涉及由式(I)表示的咪唑并喹唑啉衍生物:其中R1表示氢,取代或未取代的低级烷基,环烷基,低级烯基,取代或未取代的芳烷基,取代或未取代的芳基 取代或未取代的芳基,取代或未取代的杂芳基,或取代或未取代的杂芳基,或者取代或未取代的杂芳基,或者取代或未取代的杂芳基,或R 2和R 3 合并表示含有氮原子的杂环基,R4表示氢或取代或未取代的低级烷基,X表示O或S,Y表示单键或O,n表示0,1,2或3,以及药学上可接受的 的盐。

    [1,2,4] triazolo [1,5-C] pyrimidine derivatives
    26.
    发明授权
    [1,2,4] triazolo [1,5-C] pyrimidine derivatives 失效
    [1,2,4]三唑并[1,5-C]嘧啶衍生物

    公开(公告)号:US06222035B1

    公开(公告)日:2001-04-24

    申请号:US09401984

    申请日:1999-09-23

    CPC classification number: C07D487/04

    Abstract: [1,2,4]Triazolo[1,5-c]pyrimidine derivatives represented by formula (I) or pharmaceutically acceptable salts thereof are provided, which have adenosine A2A receptor antagonism and are useful for the treatment or prevention of various diseases induced by hyperactivity of adenosine A2A receptors (for example, Parkinson's disease or senile dementia): wherein R1 represents substituted or unsubstituted aryl, or the like; R2 represents hydrogen, halogen, lower alkyl, substituted or unsubstituted aryl, or the like; R3 represents hydrogen, halogen, XR10 (wherein X represents O or S; and R10 represents substituted or unsubstituted aryl, a substituted or unsubstituted aromatic heterocyclic ring, substituted or unsubstituted aralkyl, lower alkyl, or hydroxy lower alkyl), or the like; and Q represents hydrogen or 3,4-dimethoxybenzyl.

    Abstract translation: [1,2,4]具有式(I)表示的三唑并[1,5-c]嘧啶衍生物或其药学上可接受的盐,其具有腺苷A2A受体拮抗作用,可用于治疗或预防由 腺苷A2A受体(例如帕金森病或老年性痴呆)的多动症:其中R1表示取代或未取代的芳基等; R 2表示氢,卤素,低级烷基,取代或未取代的芳基等; R3表示氢,卤素,XR10(其中X表示O或S; R10表示取代或未取代的芳基,取代或未取代的芳族杂环,取代或未取代的芳烷基,低级烷基或羟基低级烷基)等; Q表示氢或3,4-二甲氧基苄基。

    Derivatives of benzofuran or benzodioxazole compounds
    28.
    发明授权
    Derivatives of benzofuran or benzodioxazole compounds 失效
    苯并呋喃或苯并恶唑化合物的衍生物

    公开(公告)号:US06716987B1

    公开(公告)日:2004-04-06

    申请号:US10023091

    申请日:2001-12-20

    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R 1和R 2独立地表示氢,低级烷基,氰基, - (CH 2)nE 1 -CO-G 1(其中 E 1表示键,O或NH;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)等; R 1和R 2相互结合形成饱和碳环和与其相邻的碳原子。 或R 2,以及下述R 11或R 13组合形成单键; R 3表示氢,苯基或卤素; R 4表示羟基,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 16) <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 19)= Y- [Y表示-C(R 24) - Z-(其中Z表示CONH,CONHCH 2或键)或N]或(iii) 一个债券 R 5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。

    Condensed purine derivatives
    29.
    发明授权
    Condensed purine derivatives 失效
    凝血嘌呤衍生物

    公开(公告)号:US06306847B1

    公开(公告)日:2001-10-23

    申请号:US09090936

    申请日:1998-06-05

    CPC classification number: C07D487/14

    Abstract: The present invention provides condensed purine derivatives or pharmacologically acceptable salts thereof exhibiting adenosine A3 acceptor antagonising activity, and having an antiasthmatic action, a bronchodilator action, an antiantiitching action, etc., and represented by the following formula (I): (wherein R1 represents substituted or unsubstituted aryl or a substituted or unsubstituted aromatic heterocyclic group; R2 represents hydrogen, lower alkyl, alicyclic alkyl, substituted or unsubstituted aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted aromatic heterocyclic group; R3 represents hydrogen, lower alkyl, or substituted or unsubstituted aralkyl; X1 and X2 are the same or different and each represents hydrogen, lower alkyl, substituted or unsubstituted aralkyl, or substituted or unsubstituted aryl; and n represents an integer of 0 to 3).

    Abstract translation: 本发明提供具有腺苷A3受体拮抗活性的缩合嘌呤衍生物或其药理学上可接受的盐,并具有抗哮喘作用,支气管扩张剂作用,抗脱除作用等,并由下式(I)表示:(其中R1表示 取代或未取代的芳基或取代或未取代的芳族杂环基; R 2表示氢,低级烷基,脂环族烷基,取代或未取代的芳烷基,取代或未取代的芳基或取代或未取代的芳族杂环基; R 3表示氢,低级烷基或 取代或未取代的芳烷基; X 1和X 2相同或不同,各自表示氢,低级烷基,取代或未取代的芳烷基或取代或未取代的芳基; n表示0〜3的整数。

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