首页> 外国专利> 8 pirido 2,3 pyrimidine 7 ones 2,4,8 - trisustituidas, Pharmaceutical compositions that include, use of these compounds in the manufacture of Drugs, Intermediates useful in the preparation of such Compounds, and processes for preparing Said compounds

8 pirido 2,3 pyrimidine 7 ones 2,4,8 - trisustituidas, Pharmaceutical compositions that include, use of these compounds in the manufacture of Drugs, Intermediates useful in the preparation of such Compounds, and processes for preparing Said compounds

机译:8 pirido [2,3]嘧啶7个2,4,8-trisustituidas,药物组合物,包括,这些化合物在药物生产中的用途,可用于制备此类化合物的中间体,以及制备所述化合物的方法

摘要

8 pirido [2.3D] pyrimidine 7 ones 2,4,8 - trisustituidas formula (1) or (2) or pharmaceutically acceptable salts thereof wherein R1 is an optionally substituted aryl or heteroaryl Ring optionally substituted alkyl; R2 is Hydrogen, C1 - C3 - 7 10, cycloalkyl alkyl, cycloalkyl C3 - 7, Ari The alkyl aryl, heteroaryl heteroaryl - 10 C1, C1 -, alkyl - 10A Functional group or a Heterocyclic alkyl Functional Group heterociclil C1 - 10, All Functional groups which are optionally substituted, or R2 is the functional Group cr10r20 x1) QC (A1), (A2), (A3)Or C (A1), (A2), (A3); A1 is a C1 - 10 alkyl optionally substituted alkyl; A2 is an optionally substituted C1 - 10; A3 is Hydrogen or alkyl of C1 - 10 is an optionally substituted alkyl; R3 is a C1 - C3 - 7 10, cycloalkyl alkyl, cycloalkyl C3 - 7 - c1-4 alkyl, aryl, aryl and heteroaryl, C1 - 10 Roaril C1 - 10 - alkyl Functional Group, a Heterocyclic alkyl or heterociclil C1 - 10Functional groups which are optionally substituted; R4 and R14 are each independently selected from Hydrogen, alkyl, optionally substituted cycloalkyl C1 - C3 - 4, 7 - 7 pp. ISBN cycloalkyl optionally substituted alkyl, optionally substituted aryl c1-4, c1-4 alkyl or aryl - option At present, replaced, or R9 and R14, along with the nitrogen Atom to which they are UnitedForm an optionally substituted Heterocyclic Ring of 4 to 7 Elements, optionally an additional Rings containing heteroatom selected from Oxygen, Sulfur or NR9 R6 is Hydrogen, alkyl, cycloalkyl C1 - C3 - 10, 7, heterociclilo, heterociclil C1 - aryl alkyl, aryl, alkyl - C1 10, or heteroaryl heteroaryl alkyl C1 - 10In each of these Functional groups can be optionally replaced; R9 is Hydrogen, C (Z) R6 C1 - 10 or alkyl aryl optionally substituted, optionally substituted aryl or alkyl, optionally substituted C1 - 4; R10 and R20 were selected independently between Hydrogen or alkyl C1 - 4; X is R2, OR2, S (MR2), (CH2) NN (R10) (MR2), S (CH2) NN (R10) C (o) - (CH2) nnr4r14,Or (CH2) NN (R2) 2; x1 is N (R10), or s (o) M or cr10r20; n is 0 or an integer number that has a value of 1 to 10; M is 0 or an integer number that has a value of 1 is 0 or 2, Q whole number that Has a value of 1 to 10; Z is Oxygen or Sulfur Compounds are useful in therapy, such as inhibidore S of the CSBP / p38 Kinase.Also disclosed is the use of said compounds in the manufacture of Medicines, Pharmaceutical compositions comprising such Compounds, processes for preparing such compounds and Intermediates useful in the preparation of such compounds.
机译:8,吡咯并[2.3D]嘧啶7、2、4、8-三古通式(1)或(2)或其药学上可接受的盐,其中R 1为任选取代的芳基或杂芳基。 R 2为氢,C 1 -C 3-10,环烷基烷基,环烷基C 3-7,Ari烷基芳基,杂芳基杂芳基-10 C 1,C 1-,烷基-10A官能团或杂环烷基官能团杂C 1-10,全部QC(A1),(A2),(A3)或C(A1),(A2),(A3)为任选取代的官能团,或R2为官能团cr10r20x1。 A1是C1-10烷基任选取代的烷基; A2为任选取代的C1-10; A3为氢或C1-10的烷基为任选取代的烷基; R3为C1至C3-10,环烷基烷基,环烷基C3至71-4烷基,芳基,芳基和杂芳基,C1至10 Roaril C1至10烷基官能团,杂环烷基或杂环基C1至10官能团任选取代的; R4和R14各自独立地选自氢,烷基,任选取代的环烷基C1-C3-4、7-7 pp。ISBN环烷基任选取代的烷基,任选取代的芳基c1-4,c1-4烷基或芳基-选项R9和R14与其取代的氮原子一起被取代,形成一个4至7个元素的可选取代的杂环,另一个可选的含杂原子的环选自氧,硫或NR9 R6为氢,烷基,环烷基C1- C3-10、7,杂环基,杂环基C1-芳基烷基,芳基,烷基-C1 10或杂芳基杂芳基烷基C1-10在这些官能团中的每一个可以任选地被取代; R9是氢,C(Z)R6C1-10或任选取代的烷基芳基,任选取代的芳基或烷基,任选取代的C1-4; R10和R20独立地选自氢或烷基C1-4; X是R2,OR2,S(MR2),(CH2)NN(R10)(MR2),S(CH2)NN(R10)C(o)-(CH2)nnr4r14,或(CH2)NN(R2)2; x1是N(R10)或s(o)M或cr10r20; n为0或1到10的整数; M为0或值为1的整数为0或2,Q为1到10的整数; Z是氧或硫的化合物,可用于治疗,例如CSBP / p38激酶的抑制剂S。还公开了所述化合物在药物生产中的用途,包含此类化合物的药物组合物,制备此类化合物的方法和中间体可用于制备此类化合物。

著录项

  • 公开/公告号AR035592A1

    专利类型

  • 公开/公告日2004-06-16

    原文格式PDF

  • 申请/专利权人 SMITHKLINE BEECHAM CORPORATION;

    申请/专利号AR2001P104924

  • 发明设计人

    申请日2001-10-19

  • 分类号C07D236/02;C07D239/46;C07D471/04;C07D471/02;A61K43/90;A61K31/505;A61P19/00;A61P31/00;

  • 国家 AR

  • 入库时间 2022-08-21 23:12:20

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