Substituted azabicyclic compounds

    公开(公告)号:US06800645B1

    公开(公告)日:2004-10-05

    申请号:US09612530

    申请日:2000-07-07

    IPC分类号: A61K3147

    摘要: This invention is directed to physiologically active compounds of formula (I) wherein represents a bicyclic ring system, of about 10 to about 13 ring members, in which the ring is an azaheterocycle, and the ring represents an azaheteroaryl ring, or an optionally halo substituted benzene ring; R1 represents hydrogen or a straight- or branched-chain alkyl group of 1 to about 4 carbon atoms, optionally substituted by hydroxy or one or more halogen atoms, or when Z1 represents a direct bond R1 may also represent a lower alkenyl or lower alkynyl group, or a formyl group; R2 represents hydrogen, alkenyl, alkoxy, alkyl, alkylsulphinyl, alkylsulphonyl, alkylthio, aryl, arylalkyloxy, arylalkylsulphinyl, arylalkylsulphonyl, arylalkylthio, aryloxy, arylsulphinyl, arylsulphonyl, arylthio, cyano, cycloalkenyl, cycloalkenyloxy, cycloalkyl, cycloalkyloxy, heteroaryl, heteroarylalkyloxy, heteroaryloxy, hydroxy, —SO2NR4R5, —NR4SO2R5, —NR4R5, —C(═O)R5, —C(═O)C(═O)R5, —C(═O)NR4R5, —C(═O)OR5, —O(C═O)NR4R5, or —NR4C(═O)R5; R3 represents —C(═Z)—N(R7)R6, —C(═Z)—CHR12R6, —C(═Z)—R6, —CR8═C(R9)(CH2)p—R6, —C(R10)═C(R11)R12, —C(R13)(R10)C(R11)(R14)R12, —C(R8)(R15)CH(R9)(CH2)p—R6, —R6, —V(═Z)—R6, —C(R17)═N—OC(═O)R18, —C(═O)—N(R19)OR20, —C≡C—R6, —CH2—C(═Z)—R6, —C(═Z)—C(═Z)R6, —CH2—NHR6, —CH2—ZR6, —CH2—SOR6, —CH2—SO2R6, —CF2—OR6, —NH—CH2R6, —Z—CH2R6, —SO—CH2R6, —SO2—CH2R6, —O—CF2R6, —O—C(═Z)R6, —N═N—R6, —NH—SO2R6, —SO2—NR21R22, —CZ—CZ—NHR6, —NH—CO—OR6, —O—CO—NHR6, —NH—CO—NHR6, —R23, —CX1═CX2R6, —C(═NOR24), —(CH2)qR6, —CH2—CO—NH(CH2)qR6, —CH2—NH—CO(CH2)qR6, —CH2—CO—CH2R6, —C(═NR25)—NH(CH2)qR6, —C(X3)═N—(CH2)qR6 or —CH(X4)—CH2R6; A1 represents a direct bond, or a straight or branched C1-6alkylene chain optionally substituted by hydroxyl, alkoxy, oxo, cycloalkyl, aryl or heteroaryl, or A1 represents a straight or branched C2-6alkenylene or C2-6alkynylene chain; Z1 represents a direct bond, an oxygen or sulphur atom or NH; n and m each represent zero or 1, provided that n is 1 when m is zero and n is zero when m is 1; and N-oxides thereof, and their prodrugs, and pharmaceutically acceptable salts and solvates of the compounds of formula (I) and N-oxides thereof, and their prodrugs. Such compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmaceutical compositions comprising compounds of formula (I), their pharmaceutical use and methods for their preparation.

    Rotary combine having a frusto-conical rotor housing
    5.
    发明授权
    Rotary combine having a frusto-conical rotor housing 有权
    具有截头圆锥形转子壳体的旋转组合体

    公开(公告)号:US06884161B2

    公开(公告)日:2005-04-26

    申请号:US10211279

    申请日:2002-08-02

    IPC分类号: A01F7/06 A01F12/18

    CPC分类号: A01F7/06

    摘要: A rotary crop processing unit for a combine is shown having a generally cylindrical rotor within a frusto-conical housing. The rotor is arranged in the housing with a generally constant gap between the rotor and the bottom of the housing along the housing length and with an increasing gap between the rotor and the top of the housing in the crop flow direction.

    摘要翻译: 示出了用于组合的旋转作物处理单元,其在截头圆锥形壳体内具有大致圆柱形的转子。 转子布置在壳体中,沿着壳体长度在转子和壳体的底部之间具有大致恒定的间隙,并且在转子和壳体的顶部之间沿着作物流动方向增加间隙。

    Rotary combine having a frusto-conical rotor housing
    8.
    发明授权
    Rotary combine having a frusto-conical rotor housing 失效
    具有截头圆锥形转子壳体的旋转组合体

    公开(公告)号:US06468152B2

    公开(公告)日:2002-10-22

    申请号:US09798082

    申请日:2001-03-02

    IPC分类号: A01F1218

    CPC分类号: A01F7/06

    摘要: A rotary crop processing unit for a combine is having a generally cylindrical rotor within a frusto-conical housing. The rotor is arranged in the housing with a generally constant gap between the rotor and the bottom of the housing along the housing length and with an increasing gap between the rotor and the top of the housing in the crop flow direction.

    摘要翻译: 用于组合体的旋转作物处理单元在截头圆锥形壳体内具有大致圆柱形的转子。 转子布置在壳体中,沿着壳体长度在转子和壳体的底部之间具有大致恒定的间隙,并且在转子和壳体的顶部之间沿着作物流动方向增加间隙。

    Rotary combine having a rotor axis divergent from a rotor housing axis
    10.
    发明授权
    Rotary combine having a rotor axis divergent from a rotor housing axis 有权
    旋转组合体具有从转子壳体轴线发散的转子轴线

    公开(公告)号:US06257977B1

    公开(公告)日:2001-07-10

    申请号:US09378773

    申请日:1999-08-20

    IPC分类号: A01F1210

    CPC分类号: A01F7/06

    摘要: A rotary crop-processing unit for an agricultural combine in which the rotor is mounted in a rotor housing with the rotor axis diverging from the housing axis in the crop flow direction through the crop-processing unit. The diverging rotor and housing axes enable the gap between the rotor and the top of the housing to increase in the crop flow direction without producing abrupt changes in the housing shape.

    摘要翻译: 一种用于农业联合体的旋转作物处理单元,其中转子安装在转子壳体中,其中转子轴在作物流动方向上从壳体轴线分叉通过作物处理单元。 发散的转子和壳体轴线使得转子和壳体的顶部之间的间隙能够在作物流动方向上增加,而不会引起壳体形状的突然变化。