首页> 外国专利> DERIVATIVES OF XANTHINE AS ANTAGONISTS OF ADENOSINE A2B RECEPTORS

DERIVATIVES OF XANTHINE AS ANTAGONISTS OF ADENOSINE A2B RECEPTORS

机译:黄嘌呤衍生物作为腺苷A 2B 受体的拮抗剂

摘要

FIELD: organic chemistry, medicine, pharmacology.;SUBSTANCE: invention relates to compound of the formula (I): or (II): wherein R1 and R2 are chosen independently from hydrogen, optionally substituted alkyl or the group: -D-E wherein R represents a covalent bond or alkylene; E represents optionally substituted alkoxy-group, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted alkenyl or optionally substituted alkynyl under condition that if D represents a covalent bond then E can't represents alkoxy-group; R3 represents hydrogen atom, optionally substituted alkyl or optionally substituted cycloalkyl; X represents optionally substituted arylene or heteroarylene; Y represents a covalent bond or alkylene wherein one carbon atom can be substituted optionally for -O-, -S- or -NH-, and optionally substituted hydroxy-, alkoxy-, optionally substituted amino-group or -COR wherein R represents hydroxy-, alkoxy- or amino-group under condition that if an optional substitute represents hydroxy- or amino-group then it can't be adjacent with a heteroatom; Z represents hydrogen atom, optionally substituted monocyclic aryl or optionally substituted monocyclic heteroaryl under condition that Z represents hydrogen atom only under condition that Y represents a covalent bond, and X represents optionally substituted 1,4-pyrazolene, and under condition that if X represents optionally substituted arylene then Z represents optionally substituted monocyclic heteroaryl. Also, invention describes a method for treatment of the morbid state by inhibition of adenosine receptors describes as A2B based on compounds of the formula (I) or the formula (II). Invention provides synthesis of novel compounds possessing useful biological properties.;EFFECT: valuable medicinal properties of compounds.;32 cl, 35 ex
机译:技术领域:有机化学,医学,药理学;发明领域:本发明涉及式(I)的化合物:<图像文件=“ 00000002.GIF” he =“ 45” id =“ imag00000002” imgContent =“ undefined” imgFormat =“ GIF“ wi =” 51“ />或(II):其中R 1 和R 2 独立地选自氢,任选取代的烷基或基团:-DE,其中R代表共价键或亚烷基; E代表任选取代的烷氧基,任选取代的环烷基,任选取代的芳基,任选取代的杂芳基,任选取代的杂环基,任选取代的烯基或任选取代的炔基,条件是如果D代表共价键,则E不能代表烷氧基; R 3 代表氢原子,任选取代的烷基或任选取代的环烷基; X代表任选取代的亚芳基或杂亚芳基; Y代表共价键或亚烷基,其中一个碳原子可任选被-O-,-S-或-NH-取代,以及任选被取代的羟基-,烷氧基-,任选被取代的氨基或-COR,其中R代表羟基- ,烷氧基或氨基,条件是如果一个可选的取代基代表羟基或氨基,那么它不能与杂原子相邻; Z代表氢原子,任选取代的单环芳基或任选取代的单环杂芳基,其条件是Z仅在Y代表共价键的条件下代表氢原子,并且X代表任选取代的1,4-吡唑基,并且如果X代表任选地,取代的亚芳基,则Z代表任选取代的单环杂芳基。另外,本发明还描述了一种通过抑制基于式(I)或式(II)化合物描述为A 2B 的腺苷受体来治疗病态的方法。本发明提供了具有有用生物学特性的新型化合物的合成。效果:这些化合物的有价值的医学特性。32 cl,35 ex

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