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    • 1. 发明授权
      US06180637B2 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
    • 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
    • US06180637B2
    • 2001-01-30
    • US09305602
    • 1999-05-05
    • Rudolf Schindler , Norbert Höfgen , Hildegard Poppe , Kay Brune
    • Rudolf Schindler , Norbert Höfgen , Hildegard Poppe , Kay Brune
    • A61K31513
    • C07D231/56 , C07D403/06 , C07D417/06
    • 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 6. 发明授权
      US4732986A Benzothiazole derivatives, processes for their preparation and pharmaceutical compositions containing these compounds 失效
    • Benzothiazole derivatives, processes for their preparation and pharmaceutical compositions containing these compounds
    • 苯并噻唑衍生物，其制备方法和含有这些化合物的药物组合物
    • US4732986A
    • 1988-03-22
    • US51214
    • 1987-05-12
    • Kay Brune , Heidrun Engler , Istvan Szelenyi , Peter Morsdorf , Helmut Schickaneder , Kurt H. Ahrens
    • Kay Brune , Heidrun Engler , Istvan Szelenyi , Peter Morsdorf , Helmut Schickaneder , Kurt H. Ahrens
    • A61K31/425 , A61K31/428 , A61P11/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07D277/82 , C12N9/99
    • C07D277/82
    • Benzothiazole derivatives corresponding to the general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent, independently of one another, a hydrogen atom, a halogen atom, a linear C.sub.1 -C.sub.3 -alkyl group or a linear C.sub.1 -C.sub.3 -alkoxy group, R.sup.5 represents a hydrogen atom or a linear C.sub.1 -C.sub.3 -alkyl group, R.sup.6 represents a hydrogen atom, and R.sup.7 represents a formyl group, a carbalkoxy group of the formula ##STR2## wherein R.sup.8 denotes a linear or branch chained C.sub.1 -C.sub.4 -alkyl group, or it represents an acyl group of the formula ##STR3## wherein R.sup.9 denotes a linear C.sub.1 -C.sub.3 -alkyl group, or R.sup.6 and R.sup.7 together represent the group ##STR4## wherein R.sup.10 and R.sup.11 represent, independently of one another, a hydrogen atom or a linear C.sub.1 -C.sub.6 -alkyl group or R.sup.6 and R.sup.7 represent the group ##STR5## wherein R.sup.12 and R.sup.13 represent, independently of one another, a linear C.sub.1 -C.sub.3 -alkyl group or a linear C.sub.1 -C.sub.3 -alkoxy group or R.sup.6 and R.sup.7 represent the group ##STR6## wherein R.sup.14 denotes a linear C.sub.1 -C.sub.3 -alkyl group, as well as the physiologically acceptable salts thereof, a process for the preparation of these compounds, and a pharmaceutical preparation containing them, are described.
    • 对应于通式I（I）的苯并噻唑衍生物，其中R 1，R 2，R 3和R 4彼此独立地表示氢原子，卤素原子，直链C 1 -C 3 - 烷基或直链C 1 -C 3 - C 3 - 烷氧基，R 5表示氢原子或直链C 1 -C 3 - 烷基，R 6表示氢原子，R 7表示甲酰基，式◎的烷氧基，其中，R 8表示直链或支链 或者它表示下式的酰基，其中R 9表示直链C 1 -C 3 - 烷基，或者R 6和R 7一起表示基团，其中R 10和R 11独立地表示 另一方面，氢原子或直链C 1 -C 6 - 烷基或R 6和R 7表示基团，其中R 12和R 13彼此独立地表示直链C 1 -C 3 - 烷基或直链C 1 -C 3 - 烷氧基或R6和R7表示基团，其中R14表示直链C1-C3-烷基，以及生理记录 描述了其可接受的盐，制备这些化合物的方法和含有它们的药物制剂。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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