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    Antihistamine leukotriene combinations
    2.
    发明授权
    Antihistamine leukotriene combinations 有权

    公开(公告)号：US06436924B1

    公开(公告)日：2002-08-20

    申请号：US09784640

    申请日：2001-02-15

    申请人： Hildegard Poppe ,  Jürgen Engel ,  István Szelényi

    发明人： Hildegard Poppe ,  Jürgen Engel ,  István Szelényi

    IPC分类号： A61K3155

    摘要： The invention relates to a pharmaceutical composition for the treatment of allergic rhinitis, vasomotor rhinitis, and allergic conjunctivitis, which comprises (a) a nonsedating antihistamine or a pharmaceutically acceptable salt thereof, (b) a leukotriene D4 antagonist, or a 5-lipoxygenase inhibitor, or a FLAP antagonist, or a pharmaceutically acceptable salt thereof, and (c) one or more of a conventional pharmaceutical vehicle, extender, and excipient, and to its use for manufacturing a composition for the treatment of allergic rhinitis, vasomotor rhinitis, and allergic conjunctivitis.

    1,2,5-trisubstituted 1,2-dihydroindazol-3-ones having anti-asthmatic, anti-allergic, anti-inflammatory, immunomodulating and neuroprotective action, process for their preparation and their use as medicaments
    4.
    发明授权
    1,2,5-trisubstituted 1,2-dihydroindazol-3-ones having anti-asthmatic, anti-allergic, anti-inflammatory, immunomodulating and neuroprotective action, process for their preparation and their use as medicaments 失效

    公开(公告)号：US06180637B2

    公开(公告)日：2001-01-30

    申请号：US09305602

    申请日：1999-05-05

    申请人： Rudolf Schindler ,  Norbert Höfgen ,  Hildegard Poppe ,  Kay Brune

    发明人： Rudolf Schindler ,  Norbert Höfgen ,  Hildegard Poppe ,  Kay Brune

    IPC分类号： A61K31513

    CPC分类号： C07D231/56 ,  C07D403/06 ,  C07D417/06

    摘要： The invention relates to 1,2,5-trisubstituted 1,2-dihydroindazol-3-ones of formula (I) wherein X is —SO2—, —SO—, —(CH2)p—, —(CH2)p—O—, —(CH2)p—(C═O)—, —(CH2)p—(C═O)—NH—, —(CH2)p—CHOH—, —CHOH—(CH2)p—, —(CH2)p—CH═CH—, —CH═CH—(CH2)p—, Y is —(C═O)—, —(C═O)—NH—, —(C═O)—NH—(CH2)p—, —C═O)—(CH2)p—, —(CH2)p—, —(CH2)p—O—, —(CH2)p—(C═O)—, —(CH2)p—(C═O)—NH—, —(CH2)p—(C═O)—NH—(CH2)p—, —(CH2)p—CHOH—, —CHOH—(CH2)p—, —(CH2)p—CH═CH—, —CH═CH—(CH2)p—, Z is —O—, —O—(CH2)p—, —NH—, —NH—(C═O)—, —NH—(C═O)—NH—, —NH—(C═O)—O—, —NH—CH2—(C═O)— and —NH—(C═O)—CH2—, P is a cardinal number from 1 to 4, R1, R2 and R3 can be the same or different and are: mono-, bi- or tricyclic saturated or mono- or polyunsaturated carbocycles having from 5 to 14 ring members; or mono-, bi- or tricyclic saturated or mono- or polyunsaturated heterocycles having from 5 to 15 ring members and from 1 to 6 heteroatoms, in which the carbocycles and the heterocycles can be mono- or polysubstituted by: C1-6-alkyl, —O—C1-6-alkyl, —O—C3-7-cycloalkyl, mono-, bi- or tricyclic saturated or mono- or polyunsaturated carbocycles having from 3 to 14 ring members, mono-, bi- or tricyclic saturated or mono- or polyunsaturated heterocycles having from 5 to 15 ring members and from 1 to 6 heteroatoms, R1 is also H, provided that when X is CH2, then R1 is not H, R3—Z is also NO2, and their pharmaceutically acceptable salts, but excluding compounds of formula (I) in which if Z is —NH—(C═O)—, —NH—(C═O)—NH—, —NH—(C═O)—O—, —NH—(C═O)—CH2 and at the same time R1 is phenyl, monosubstituted or polysubstituted by —COOH, —COOC1-6-alkyl, —(CH2)p—COOH, —(CH2)p—COOC1-6-alkyl —CONHC1-6-alkyl, —CONHC6-14-aryl, —CONHSO2C1-6-alkyl, —CONHSO2C6-4-aryl, 1H-tetrazol-5-yl, then R2 is not phenyl, monosubstituted or polysubstituted by CN, halogen, C1-4-alkyl, C1-4-alkyloxy, CF3; and if R3—Z is NO2, then R1—X is not benzyl or 4-methoxybenzyl, and R2—Y is not benzyl or 2-picolyl at the same time; and to pharmaceutical treatment processes, and processes for making.