摘要:
The present invention provides novel compounds and methods for using them to treat diseases with aminothiophene inhibitors of IKK-β phosphorylation of IκB. In so doing these aminothiophene inhibitors block pathological activation of transcription factor NF-κB in which diseases excessive activation of NF-κB is implicated.
摘要:
3-carboxy quinoline derivatives, which are useful as YAK3 inhibitors are described herein. The described invention also includes methods of making such 3-carboxy quinoline derivatives as well as methods of using the same in the treatment of diseases mediated by inappropriate YAK3 activity.
摘要:
Compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1, R2 and R3 are various substituent groups; and one of X1 and X2 is N or CR′, and the other is NR′ or CHR′ wherein R′ is hydrogen, OH, C1-6alkyl, or C3-7cycloalkyl; or when one of X1 and X2 is N or CR′ then the other may be S or O; and their use as pharmaceuticals.
摘要:
This invention relates to novel quinoline inhibitors of hYAK1 and hYAK3 kinases and pharmaceutically acceptable salts, hydrates or solvates thereof, pharmaceutical compositions thereof, and methods of treatment of diseases in which an excessive amount of either such kinase is a factor.
摘要:
Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.
摘要:
Novel substituted 1,5,7-trisubstituted-3,4-dihydro-pyrimido[4,5-d]pyrimidin-2-(1H)-one compounds and compositions, and their use in therapy as CSBP/RK/p38 kinase inhibitors.
摘要:
Novel substituted 2,4,8-trisubstituted 8H-pyrido[2,3-d]pyrimidin-7-one containing compounds and compositions, and their use in therapy as CSBP/RK/p38 kinase inhibitors.
摘要:
Novel substituted 2,4,8-trisubstituted 8H-pyrido[2,3-d]pyrimidin-7-one containing compounds and compositions, and their use in therapy as CSBP/RK/p38 kinase inhibitors.
摘要:
The present invention is directed to a novel method of preparing of 2,4,8-trisubstituted pyrido[2,3-d]pyrimidin-7-one pharmacophores of Formula (II) or (IIa) wherein G1 is CH2; G2 is CH; Rx is chloro, bromo, iodo, or O—S(O)2CF3; Rg is a C1-10 alkyl; m is 0, or an integer having a value of 1, or 2; R3 is a C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties may be optionally substituted. which comprises reacting a compound of the formula: wherein Ry is chloro, bromo, iodo, O—S(O)2CF3; and Rg is a C1-10 alkyl; with a olefin forming reagent in a suitable base to yield a compound of Formula (II), or (IIa) wherein m=0 and oxidizing the sulphur as necessary or desired.
摘要翻译:本发明涉及制备式(II)或(IIa)的2,4,8-三取代吡啶并[2,3-d]嘧啶-7-酮药代动力学的新方法,其中G1是CH2; G2是CH; R x是氯,溴,碘或O-S(O)2 C 3 F 3; Rg为C1-10烷基; m为0,或值为1或2的整数; R 3是C 1-10烷基,C 3-7环烷基,C 3-7环烷基C 1-10烷基,芳基,芳基C 1-10烷基,杂芳基,杂芳基C 1-10烷基,杂环基或杂环基C 1-10烷基部分,并且其中 部分可以任选被取代。 其包括使下式化合物:其中R y是氯,溴,碘,O-S(O)2 C 3 F 3; 且R g为C 1-10烷基; 在合适的碱中加入烯烃形成试剂,得到式(II)化合物或其中m = 0的(IIa),并根据需要氧化硫。
摘要:
The present invention is directed to a novel method of preparing of 2,4,8-trisubstituted pyrido[2,3-d]pyrimidin-7-one pharmacophores of Formula (II) or (IIa) wherein G1 is CH2 or NH: G2 is CH or nitrogen; Rx is chloro, bromo, iodo, or O—S(O)2CF3; Rg is a C1-10alkyl; m is 0, or an integer having a value of 1, or 2; R3 is a C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties may be optionally substituted. which comprises reacting a compound of the formula: wherein Ry is chloro, bromo, iodo, O—S(O)2CF3; and Rg is a C1-10 alkyl; with a olefin forming reagent in a suitable base to yield a compound of Formula (II), or (IIa) wherein m=0 and oxidizing the sulphur as necessary or desired.
摘要翻译:本发明涉及一种制备式(II)或(IIa)的2,4,8-三取代吡啶并[2,3-d]嘧啶-7-酮药效团的新方法,其中G1是CH2或NH:G2 是CH或氮; R x是氯,溴,碘或O-S(O)2 C 3 F 3; Rg为C1-10烷基; m为0,或值为1或2的整数; R 3是C 1-10烷基,C 3-7环烷基,C 3-7环烷基C 1-10烷基,芳基,芳基C 1-10烷基,杂芳基,杂芳基C 1-10烷基,杂环基或杂环基C 1-10烷基部分,并且其中 部分可以任选被取代。 其包括使下式化合物:其中R y是氯,溴,碘,O-S(O)2 C 3 F 3; 且R g为C 1-10烷基; 在合适的碱中加入烯烃形成试剂,得到式(II)化合物或其中m = 0的(IIa),并根据需要氧化硫。