Quinazoline derivatives and pharmaceutical compositions thereof
    6.
    发明授权
    Quinazoline derivatives and pharmaceutical compositions thereof 有权
    喹唑啉衍生物及其药物组合物

    公开(公告)号:US08431586B2

    公开(公告)日:2013-04-30

    申请号:US12089087

    申请日:2006-10-03

    IPC分类号: A61K31/517

    摘要: The present invention relates to novel quinazoline derivatives with less skin irritation and an excellent action of strongly suppressing scratching behavior, and pharmaceutical compositions containing a quinazoline derivative as an active ingredient. The present invention is directed to the quinazoline derivatives represented by the general formula [1] or pharmaceutically acceptable salts thereof. In the general formula [1], R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 and R4 are the same or different and represent hydrogen, alkyl, alkoxy or halogen; R5 is combined with R6 to represent alkylene or represents hydrogen, hydroxy, alkyl, phenyl or alkoxy; R6 represents alkyl, cycloalkyl, phenyl, a 5- to 10-membered aromatic heterocyclic group containing one to three heteroatoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, or —N(R6-1)(R6-2).

    摘要翻译: 本发明涉及具有较少皮肤刺激性和强烈抑制划伤行为的优异作用的新型喹唑啉衍生物以及含有喹唑啉衍生物作为活性成分的药物组合物。 本发明涉及由通式[1]表示的喹唑啉衍生物或其药学上可接受的盐。 在通式[1]中,R 1表示氢等; R2表示氢等; R3和R4相同或不同,代表氢,烷基,烷氧基或卤素; R5与R6结合表示亚烷基或代表氢,羟基,烷基,苯基或烷氧基; R6表示烷基,环烷基,苯基,含有1至3个选自氮原子,氧原子和硫原子的杂原子的5至10元芳族杂环基或-N(R 6-1)( R6-2)。

    Quinazoline derivatives and medicaments
    7.
    发明授权
    Quinazoline derivatives and medicaments 失效
    喹唑啉衍生物和药物

    公开(公告)号:US07718663B2

    公开(公告)日:2010-05-18

    申请号:US10512954

    申请日:2003-04-28

    IPC分类号: A61K31/517 C07D239/94

    摘要: An object of the present invention is to provide an antipruritic agent having a novel action mechanism.The present invention provides an antipruritic agent comprising a compound represented by the following general formula (1): wherein R1 represents a hydrogen atom or alkyl; the ring Q represents a cyclohexylene group or a phenylene group; A1 and A2 represent a single bond or an alkylene group; E represents —NHCO—; A3 represents a single bond or a divalent saturated or unsaturated aliphatic hydrocarbon group; R3 represents a non-cyclic aliphatic hydrocarbon group; and R4 and R5 are the same or different and each represents a hydrogen atom or alkyl, or a pharmaceutically acceptable salt thereof as an active ingredient.

    摘要翻译: 本发明的目的是提供具有新颖作用机理的止痒剂。 本发明提供含有由以下通式(1)表示的化合物的止痒剂:其中R1表示氢原子或烷基; 环Q表示亚环己基或亚苯基; A1和A2表示单键或亚烷基; E表示-NHCO-; A3表示单键或二价饱和或不饱和脂族烃基; R3表示非环状脂族烃基; R 4和R 5相同或不同,各自表示氢原子或烷基,或其药学上可接受的盐作为活性成分。

    Quinazoline derivative and medicine
    8.
    发明申请
    Quinazoline derivative and medicine 失效
    喹唑啉衍生物和药物

    公开(公告)号:US20050176741A1

    公开(公告)日:2005-08-11

    申请号:US10512954

    申请日:2003-04-28

    摘要: An object of the present invention is to provide an antipruritic agent having a novel action mechanism. The present invention provides an antipruritic agent comprising a compound represented by the following general formula (1): wherein R1 represents a hydrogen atom or alkyl; the ring Q represents a cyclohexylene group or a phenylene group; A1 and A2 represent a single bond or an alkylene group; E represents —NHCO—; A3 represents a single bond or a divalent saturated or unsaturated aliphatic hydrocarbon group; R3 represents a non-cyclic aliphatic hydrocarbon group; and R4 and R5 are the same or different and each represents a hydrogen atom or alkyl, or a pharmaceutically acceptable salt thereof as an active ingredient.

    摘要翻译: 本发明的目的是提供具有新颖作用机理的止痒剂。 本发明提供含有由以下通式(1)表示的化合物的止痒药:其中R 1表示氢原子或烷基; 环Q表示亚环己基或亚苯基; A 1和A 2代表单键或亚烷基; E表示-NHCO-; A 3表示单键或二价饱和或不饱和脂族烃基; R 3表示非环状脂族烃基; R 4和R 5相同或不同,各自表示氢原子或烷基或其药学上可接受的盐作为活性成分。

    QUINAZOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF
    9.
    发明申请
    QUINAZOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF 有权
    喹诺酮衍生物及其药物组合物

    公开(公告)号:US20100022566A1

    公开(公告)日:2010-01-28

    申请号:US12089087

    申请日:2006-10-03

    摘要: The present invention relates to novel quinazoline derivatives with less skin irritation and an excellent action of strongly suppressing scratching behavior, and pharmaceutical compositions containing a quinazoline derivative as an active ingredient. The present invention is directed to the quinazoline derivatives represented by the general formula [1] or pharmaceutically acceptable salts thereof. In the general formula [1], R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 and R4 are the same or different and represent hydrogen, alkyl, alkoxy or halogen; R5 is combined with R6 to represent alkylene or represents hydrogen, hydroxy, alkyl, phenyl or alkoxy; R6 represents alkyl, cycloalkyl, phenyl, a 5- to 10-membered aromatic heterocyclic group containing one to three heteroatoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, or —N(R6-1)(R6-2).

    摘要翻译: 本发明涉及具有较少皮肤刺激性和强烈抑制划伤行为的优异作用的新型喹唑啉衍生物以及含有喹唑啉衍生物作为活性成分的药物组合物。 本发明涉及由通式[1]表示的喹唑啉衍生物或其药学上可接受的盐。 在通式[1]中,R 1表示氢等; R2表示氢等; R3和R4相同或不同,代表氢,烷基,烷氧基或卤素; R5与R6结合表示亚烷基或代表氢,羟基,烷基,苯基或烷氧基; R6表示烷基,环烷基,苯基,含有1至3个选自氮原子,氧原子和硫原子的杂原子的5至10元芳族杂环基或-N(R 6-1)( R6-2)。

    Quinazoline derivatives and drugs
    10.
    发明授权
    Quinazoline derivatives and drugs 失效
    喹唑啉衍生物和药物

    公开(公告)号:US07220751B2

    公开(公告)日:2007-05-22

    申请号:US10399803

    申请日:2001-11-01

    CPC分类号: C07D401/06 C07D239/94

    摘要: The invention provides an excellent novel analgesic which acts on a nociceptin receptor to exhibit a wide range of the analgesic effect for example on a chronic pain as well as an allodynia accompanied with a herpes zoster.The invention relates to a nociceptin receptor agonist comprising as an active ingredient a compound represented by Formula (I) or a salt thereof: wherein R1 represents a hydrogen atom or alkyl; A1 and A2 are the same or different and each represents a single bond or a divalent aliphatic hydrocarbon group; Q represents a single bond, cycloalkylene group, phenylene group or a divalent heterocyclic group; R2A and R2B are the same or different and each represents a hydrogen atom or alkyl; R3 represents an optionally substituted phenyl group or heterocyclic group; R4 and R5 are the same or different and each represents a hydrogen atom, alkyl, alkoxy, aralkyloxy, halogen, nitro, hydroxy, alkoxycarbonyl, —NR6R7 and the like.

    摘要翻译: 本发明提供了一种优异的新颖止痛剂,其作用于伤害感受肽受体以表现出广泛的止痛效果,例如慢性疼痛以及伴随带状疱疹的异常性疼痛。 本发明涉及一种伤害感受肽受体激动剂,其包含作为活性成分的由式(I)表示的化合物或其盐:其中R 1表示氢原子或烷基; A 1和A 2相同或不同,各自表示单键或二价脂族烃基; Q表示单键,亚环烷基,亚苯基或二价杂环基; R 2A和R 2B相同或不同,各自表示氢原子或烷基; R 3表示任选取代的苯基或杂环基; R 4和R 5相同或不同,各自表示氢原子,烷基,烷氧基,芳烷氧基,卤素,硝基,羟基,烷氧基羰基,-NR 6< 7>等等。