首页> 外国专利> Derivatives of imidazo 1,2-a pyrimidine, Preparation procedure, intermediaries that process, Pharmaceutical compositions containing same and Use thereof as Protein Kinase Inhibitors, met, for the treatment of psoriasis, cancers, and other diseases of the central nervous system

Derivatives of imidazo 1,2-a pyrimidine, Preparation procedure, intermediaries that process, Pharmaceutical compositions containing same and Use thereof as Protein Kinase Inhibitors, met, for the treatment of psoriasis, cancers, and other diseases of the central nervous system

机译:咪唑并[1,2-a]嘧啶的衍生物,制备方法,所加工的中间体,含有该衍生物的药物组合物及其作为蛋白激酶抑制剂的用途,已用于治疗牛皮癣,癌症和其他中枢神经系统疾病

摘要

Claim 1: products of formula (1), in which n = 0, 1, or 2,; X represents a hydrogen Atom or a Halogen Atom, an alkyl radical; R represents a hydrogen Atom, a radical NH2, nhalk or N (alk) 2; ra represents a hydrogen Atom, a Halogen Atom, or a radical - or - - or alkyl, cycloalkyl, aryl or heteroaryl -, - O -, -, - NRD NRD (cycloalkyl) alkyl (aryl) - NRD)NRD - (heteroaryl), alkyl, cycloalkyl, aryl heterocicloalquilo, a radical, or a heteroaryl radical; in all these Radicals Radicals, aryl and heteroaryl alkyl, cycloalkyl, optionally substituted are as follows; RB represents a hydrogen Atom, a Radi Cal - coorc, RC, RC - CO - or a radical with co nrcrd; RC represents a radical alkyl, cycloalkyl,Heterocicloalquilo, aryl and heteroaryl, with all these radical optionally substituted as indicated below; RD represents a hydrogen Atom or a radical alkyl or cycloalkyl Radicals; while all the previously defined alkyl, cycloalkyl, heterocicloalquilo,Aryl and heteroaryl radical optionally substituted with one or more selected from Halogen Atoms and hydroxyl radicals, alkoxy, CN, CF3, nr1r2 -, - COOH, - - - cooalk, conr1r2, nr1cor2, COR1, Oxo, heterocicloalquilo, aryl and heteroaryl, Recent heterocicloalquilo,Aryl or heteroaryl being themselves radical optionally substituted with one or more selected from Halogen Atoms and Radicals hydroxyl, alkyl, alkoxy, - COOH, - nr3r4, cooalk, conr3r4, nr3cor4 - oxo -, and cor3 cycloalkyl Radicals; In addition, heterocicloalquilo, ar ILO or heteroaryl radical optionally substituted with an alkylThe same radical optionally substituted with one or more selected from Halogen Atoms and Radicals hydroxyl, alkyl, alkoxy, - COOH, - nr3r4, cooalk, conr3r4 nr3cor4, -, - cor3; being nr1r2 so that R1 and R2 being either identical or different, one of R1 and R2 represents a unto Volume of hydrogen or an alkyl radical, and the other of R1 and R2 represents a hydrogen Atom,A radical optionally substituted cycloalkyl or an alkyl radical with one or several identical or different radical selected from hydroxyl radicals, alkoxy, nr3r4, heterocicloalquilo, heteroaryl or themselves, phenyl optionally substituted with one or several radical selected from The Halogen Atoms and Radicals hydroxyl alkyl, alkoxy, NH2,Nhalk and N 2 (alk); R1 and R2 are with the nitrogen Atom to which are attached a cyclic radical comprising of 3 to 10 links and optionally one or more heteroatoms (S) or between different chosen, S, N, NH, and this included the NH radical containing substituted option optional Finally, nr3r4 such that being well R3 and R4 are identical or different.One of R3 and R4 represents a hydrogen Atom or an alkyl radical, and the other of R3 and R4 represents a hydrogen Atom, an alkyl or cycloalkyl radical radical optionally substituted with one or several identical or different radical selected from hydroxyl radicals, alkoxy, and Rocicloalquilo themselves, or heteroaryl phenyl optionally substituted,With one or several radical selected from Halogen Atoms and Radicals hydroxyl, alkyl, alkoxy, NH2, and nhalk N (alk) 2; R3 and R4 form with the nitrogen Atom to which are attached a cyclic radical comprising of 3 to 10 links and optionally one or more heteroatoms di Various elected (S) between o, S, N and NHThis included the Optional containing NH radical optionally substituted; cyclic Radicals that can form R1 and R2 or R3 and R4 respectively with the nitrogen Atom to which they are United, being optionally substituted with one or several identical or different chose radical Between the two Halogen ATOMS, hydroxyl radicals, Oxo, alkoxy, NH2, nhalk,(alk) 2 radical and alkyl, cycloalkyl, heterocicloalquilo, co - co2alk alkyl, phenyl, phenyl heteroaryl - CH2, such that in these last heterocicloalquilo alkyl Radicals, radical, phenyl optionally substituted heteroaryl are themselves with one or several radical the Egidos between Halogen Atoms and hydroxyl radicals.Alkyl and alkoxy containing 1 to 4 carbon ATOMS, N and NH2; nhaik (alk) 2; R1, R2, R3 and R4 in the radical nr1cor2 nr3cor4 COR1, -, -, and - cor3 being selected among the meanings indicated above for R1, R2,R3 and R4 in nr1r2 and nr3r4 part when R1 and R2 and R3 and R4 form a cyclic radical with the nitrogen Atom to which they are United; comprising all alkyl and alkoxy Radicals (alk) above of 1 to 6 carbon Atoms; and such products of formula (1) in All Forms Isomeras possible enantiomers and Racemic, diastereoisomeras,As well as the addition salts with Mineral and organic acids or bases with Organic and Mineral Products of formula (1).
机译:权利要求1:式(1)的产物,其中n = 0、1或2;和X代表氢原子或卤素原子,烷基; R代表氢原子,NH 2基,nhalk或N(烷)2; ra代表氢原子,卤素原子或基团-或--或烷基,环烷基,芳基或杂芳基-,-O-,-,-NRD NRD(环烷基)烷基(芳基)-NRD)NRD-(杂芳基),烷基,环烷基,芳基杂环烷基,基团或杂芳基基团;在所有这些自由基中,任选被取代的芳基和杂芳基烷基,环烷基如下: RB表示氢原子,Radi Cal-coorc,RC,RC-CO-或具有concrd的基团; RC表示烷基,环烷基,杂环基,杂芳基和杂芳基,所有这些基团如下所述任选地被取代; RD代表氢原子或烷基或环烷基基团;而所有先前定义的烷基,环烷基,杂环烷基,芳基和杂芳基基团可选地被一个或多个选自卤素原子和羟基基团,烷氧基,CN,CF3,nr1r2-,-COOH,---cooalk,conr1r2,nr1cor2取代的芳基和杂芳基, COR1,氧代,杂环烷基,芳基和杂芳基,新杂环基,芳基或杂芳基本身是可任选被一个或多个选自卤素原子和自由基的羟基,烷基,烷氧基,-COOH,-nr3r4,cooalk,conr3r4,nr3cor4-氧代取代的基团-和cor3环烷基基团;另外,杂环氯基,ar ILO或任选被烷基取代的杂芳基基团任选被一个或多个选自卤素原子和自由基的相同基团羟基,烷基,烷氧基,-COOH,-nr3r4,cooalk,conr3r4 nr3cor4,-,-cor3 ;为nr1r2,因此R1和R2相同或不同,R1和R2之一代表氢或烷基的体积,R1和R2另一个代表氢原子,原子团为可取代的环烷基或烷基具有一个或几个选自羟基,烷氧基,nr3r4,杂环烷基,杂芳基或它们本身的相同或不同基团,苯基任选被一个或多个选自卤素原子和自由基的羟烷基,烷氧基,NH2,Nhalk和N 2( alk); R1和R2与氮原子相连,该环上含有3至10个键和一个或多个杂原子(S)或在不同选择的S,N,NH之间构成的环状基团,其中包括含有取代基的NH基团最后,nr3r4使得R3和R4孔相同或不同。R3和R4中的一个代表氢原子或烷基,R3和R4的另一个代表氢原子,烷基或环烷基具有选自羟基,烷氧基和Rocicloalquilo本身的一个或几个相同或不同的基团,或任选取代的杂芳基苯基,具有选自卤素原子和自由基的一个或多个基团的羟基,烷基,烷氧基,NH2和nhalk N(alk) 2; R3和R4与氮原子一起形成环原子团,该环原子团包含3至10个键和任选地一个或多个杂原子。在o,S,N和NH之间的各种选择的(S)。可以与它们所连接的氮原子分别形成R1和R2或R3和R4的环状自由基,在两个卤素原子ATOMS之间可任选被一个或多个相同或不同选择的基团取代,羟基,氧代,烷氧基,NH2, nhalk,(alk)2自由基和烷基,环烷基,杂环烷基,co-co2烷基,苯基,苯基杂芳基-CH2,这样在这些最后的杂环烷基烷基中,自由基,可被取代的苯基杂芳基本身带有一个或多个自由基Egidos含1-4个碳原子的ATOMS,N和NH2的烷基和烷氧基。 nhaik(alk)2; nr1cor2 nr3cor4基团中的R1,R2,R3和R4 COR1,-,-和-cor3选自上面对nr1r2和nr3r4部分中的R1,R2,R3和R4表示的含义,当形成R1和R2以及R3和R4时与氮原子相连的环状自由基;包含以上所有1至6个碳原子的烷基和烷氧基自由基(alk);以及所有形式的Isomeras可能的对映异构体和外消旋,非对映异构体以及与矿物和有机酸形成的加成盐或与式(1)的有机和矿物形成的碱的此类式(1)产物。

著录项

相似文献

  • 专利
  • 外文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号