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    • 2. 发明公开
    • Ethanolamine derivates, processes for their preparation and pharmaceutical compositions containing them
    • 乙醇胺衍生物,它们的制备方法和含有它们的化合物的药物组合物。
    • EP0286242A2
    • 1988-10-12
    • EP88302151.1
    • 1988-03-11
    • GLAXO GROUP LIMITED
    • Skidmore, Ian FrederickFinch, HarryMitchell, William LeonardNaylor, AlanLunts, Lawrence HenryHartley, David
    • C07C93/08C07C149/32C07C143/75C07C127/17C07C103/76C07D213/65C07D215/52A61K31/10A61K31/135A61K31/165
    • C07D213/30C07D213/32C07D213/63
    • This invention relates to compounds of the general formula (I)
      and physiologically acceptable salts and solvates thereof where Ar represents
      where

      R 3 is a bond or a straight or branched C 1 2 alkylene group,
      R 4 is a hydroxy group or a group R 5 NH-where
      R 5 represents a group CH 3 SO 2 -, HCO-or NH 2 CO-,

      where R 6 is a chlorine atom or the group F 3 C-,

      k represents an integer from 1 to 8,
      m represents zero or an integer from 2 to 7 and
      n represents an integer from 2 to 7 with the proviso that the sum total of k. m and n is 4 to 12;
      R 1 and R 2 each represents a hydrogen atom or a methyl or ethyl group with the proviso that the sum total of carbon atoms in R 1 and R 2 is not more than 2;
      R 30 represents hydrogen or C 12 alkyl;
      X represents an oxygen or sulphur atom: and
      Y and Q may each represent a bond or an oxygen or sulphur atom with the provisos that at least one of Y and Q represents an oxygen or sulphur atom and when Y is a bond m is zero, or when Y represents an oxygen or sulphur atom m is an integer from 2 to 7:
      P represents a phenyl group otionally substituted by one or more substituents selected from halogen atoms, or the groups C 1 3 alkyl, C 1 3 alkoxy, hydroxy, -CH 2 OH-, -(CH 2 ) 2 OH, -CO 2 H. -CO 2 CH 3 , ·CO 2 (CH 2 )- 2 CH 3 , -R 7 , COR 7 , -NHCOR s and ·NR 9 SO 2 R 10 ; where
      R 7 represents an amino, aminoC 1 3 alkyl, aminoC, 3 dialkyl, pyrrolidino. piperidino. hexamethyleneimino, piperazino, N-methylpiperazino or morpholino group;
      R 8 represents a hydrogen atom or a C, 4 alkyl, C, 4 alkoxy, phenyl or amino group;
      R 9 represents a hydrogen atom or a methyl group;
      R 10 represents a methyl, phenyl, amino or dimethylamino group;

      or P represents a pyridyl group optionally substituted by one or two substitutents selected from halogen atoms or hydroxy, C, 3 alkyl and C 1 3 alkoxy groups.
      The compounds have a stimulant action at β 2 -adrenoreceptors and are useful, in particular, in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.
    • 本发明涉及通式(I)生理学上可接受的盐的化合物和和它们的溶剂合物,其中Ar darstellt 其中R <3>是一个键或直链或支链的C 1-2亚烷基团,R <4> 为羟基或基团R <5> NH,其中R <5> darstellt的基团CH 3 SO 2,HCO或NH 2 CO--, 其中R <6>是氯原子或基团F3C ,ķdarstellt在整数从1到8,M darstellt为零或整数2至在整数7和n darstellt从2至7,条件的总和K,M没有和n是4到12; [R <1>和R <2>每一个darstellt氢原子或甲基或乙基,条件的总和中的R的碳原子的那样<1>和R <2>不大于2; [R <3> <0> darstellt氢或C1-2烷基; X darstellt到氧或硫原子; 和Y和Q可以各自代表一个键或氧或硫原子,条件没有氧或硫原子的Y和Q darstellt中的至少一个,并且当Y是键,m是零,或当氧或硫Y的darstellt 原子,m为2至7的整数; P表示被选自卤素原子中的一种或多种取代基,或基团C 1-3烷基,C 1-3烷氧基,羟基,-CH2OH-,otionally取代的苯基 - (CH 2)2 OH,-CO 2 H,-CO 2 CH 3,-CO 2(CH 2 )2 CH 3,-R <7>,COR <7>,-NHCOR <8>和-NR <9> SO 2 <1> <0>; 其中R <7> darstellt氨基的,aminoC1-3alkyl,aminoC1-3dialkyl,吡咯烷基,哌啶子基,六亚甲基亚,哌嗪子基,N-甲基哌嗪基或吗啉代基团; [R <8>表示一个氢原子或一个C 1-4烷基,C 1-4烷氧基,苯基或氨基; [R <9>代表氢原子或甲基; [R <1> <0>表示一个甲基,苯基,氨基或二甲基氨基; 或P被选自卤素原子或羟基,C 1-3烷基C 1-3烷氧基和基团的一个或两个取代基darstellt吡啶基,任选substituiertem。 所述化合物具有在β-2肾上腺素能受体兴奋剂作用和是有用的,特别是,在与可逆气道阻塞相关的疾病的治疗:如哮喘和慢性支气管炎。
    • 6. 发明公开
    • Ethanolamine compounds
    • 乙醇胺化合物乙醇胺化合物
    • EP0219350A3
    • 1988-06-08
    • EP86307976
    • 1986-10-15
    • GLAXO GROUP LIMITED
    • Finch, HarryLunts, Lawrence Henry CharlesNaylor, AlanSkidmore, Ian Frederick
    • C07C93/08C07C93/10A61K31/135C07D213/18C07C93/14C07C103/76C07C103/38C07C125/065C07C127/17C07C143/75C07D295/08
    • A61K31/135
    • The invention provides compounds of the general formula
      wherein
      Ar represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms, or the groups C 1-6 alkyl, nitro, -(CH 2 )qR, [where R is hydroxy, C 1-6 alkoxy. -NR 3 R 4 each represents a hydrogen atom, or a C 1-4 alkyl group. or -NR 3 R 4 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring one or more atoms selected from -O- or -S- or a group -NH- or -N(CH 3 )-), -NR 5 COR 6 (where R 5 represents a hydrogen atom or a C 1-4 alkyl group, and R 6 represents a hydrogen atom or a C I - 4 alkyl, C I - 4 alkoxy, phenyl or -NR 3 R 4 group), -NR 5 SO 2 R (where R 7 represents a C 1-4 alkyl, phenyl or -NR 3 R 4 group), -COR 8 (where R 8 represents hydroxy, C 1-4 alkoxy or -NR 3 R 4 , -SR9 (where R 9 is a hydrogen atom, or a C 1-4 alkyl or phenyl group), -SOR 9 , -S0 2 R 9 , or -CN, and q represents an integer from 0 to 3], or -O(CH 2 ) t R 11 [where R 11 represents a hydroxy or C 1-4 alkoxy group and t is 2 or 3], or Ar is a phenyl group substituted by an alkylenedioxy group of formula -O(CH 2 )pO-, where p represents 1 or 2; R 1 and R 2 each represent a hydrogen atom or a C I - 3 alkyl group, with the proviso that the sum total of carbon atoms in R 1 and R 2 is not more than 4; R 30 represents a hydrogen atom or a C 1-3 alkyl group; X represents a C 2 - 8 alkylene chain optionally substituted by one or two C 1-3 alkyl groups, or, when one carbon atom is substituted by two methyl groups, they may be linked to form an ethylene group, and Y represents a C 1-7 alkylene chain optionally substituted by one or two C 1-3 alkyl groups, or, when one carbon atom is substituted by two alkyl groups, they may be linked to form an alkylene group; with the proviso that the sum total of carbon atoms in X and Y is 4 to 12; and with the further proviso that at least one of X and Y is substituted by one or two C 1-3 alkyl groups or an alkylene group; Q represents (where R 12 is a straight or branched Ci.3 alkylene group).

      (where one or R 13 and R 14 is a hydroxy group and the other is a hydrogen or halogen atom or a hydroxy group).

      [where R' 5 is a group R 16 CO-, R 16 NHCO-, R 16 R 17 NS0 2 - or R 18 SO 2 - (where R 16 and R 17 is each a hydrogen atom or a C 1-3 alkyl group and R 18 is a C 1-3 alkyl group) and p is an integer 0 or 1],

      (where R 26 and R 27 is each a hydrogen atom or a C 1-3 alkyl group or, when R 26 is a hydrogen atom, R 27 may also be a C 1-4 alkoxycarbonyl group),

      (where R 19 is a C I - 3 alkyl group),
      and physiologically acceptable salts and solvates (e.g. hydrates) thereof. The compounds have a stimulant action at β2-adrenorecep- tors and may be used in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.