摘要:
A compound of formula I, or a stereoisomer, a tautomer, a pharmaceutically acceptable salt or solvate thereof, methods of using such compounds in the treatment of hyperproliferative, inflammatory, infectious, and immunoregulatory disorders and diseases; and to pharmaceutical compositions containing such compounds.
摘要:
In general, the instant invention comprises compounds of Formulas (I) and (II) including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase inhibitors and therefore are useful for treating cancer and other protein kinase mediated diseases.
摘要:
In general, the instant invention comprises compounds of Formulas I and II including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase inhibitors and therefore are useful for treating cancer and other protein kinase mediated diseases.
摘要:
Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g. a hydrate), or a pharmaceutically-acceptable salt, thereof, wherein: M is selected from alkyl, substituted alkyl, cycloalkyl, aryl, heterocyclo, and heteroaryl, provided that if M is alkyl then R 6 and R 7 taken together with the carbon atom to which they are both attached are selected from a group other than cycloalkyl; Q is selected from (i) hydrogen, C 1 -C 4 alkyl, and substituted C 1 -C 4 alkyl; or (ii) Q and R 6 are combined with the carbon atoms to which they are attached to form a 3- to 6-membered cycloalkyl; or (iii) Q and M a M are combined with the carbon atom(s) to which they are attached to form a 3- to 7-membered ring containing 1-2 heteroatoms which are independently selected from the group consisting of O, S, SO 2 , and N which ring may be optionally substituted with 0-2 R 5 groups or carbonyl; Z is selected from cycloalkyl, heterocyclo, aryl, or heteroaryl; and M a , Z a , R 1 , R 2 , R 3 , R 4 , R 6 , R 7 , and R 22 are as defined herein. Also provided are pharmaceutical compositions and methods of treating metabolic and inflammatory- or immune-associated diseases or disorders using said compounds.
摘要翻译:提供了新颖的非类固醇化合物,其用于治疗与糖皮质激素受体,AP-1和/或NF-κB活性的调节相关的疾病,包括具有式(I)结构的炎性和免疫疾病,肥胖症和糖尿病, 其中:M选自烷基,取代的烷基,环烷基,芳基,杂环基和杂芳基,条件是如果M是烷基,则M是烷基,取代的烷基,环烷基, R 6和R 7与它们都连接的碳原子一起选自除环烷基以外的基团; Q选自(i)氢,C 1 -C 4烷基和取代的C 1 -C 4 SUB SUB> 烷基; 或(ii)Q和R 6与它们所连接的碳原子结合形成3至6元环烷基; 或(iii)Q和MASS a M与它们所连接的碳原子结合形成含有1-2个独立选自以下的杂原子的3-至7-元环: 由O,S,SO 2,N和N组成的组,该环可以任选地被0-2个R 5基团或羰基取代; Z选自环烷基,杂环基,芳基或杂芳基; 和 a SUB>,Z a SUB>, 1 SUB>, 2 SUB>, 3 SUB> ,R 4,R 6,R 7,和R 22如本文所定义。 还提供了使用所述化合物治疗代谢和炎症或免疫相关疾病或病症的药物组合物和方法。
摘要:
In general, the instant invention comprises compounds of Formulas (I) and (II) including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase inhibitors and therefore are useful for treating cancer and other protein kinase mediated diseases.
摘要:
Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, and hydrates, thereof, (I) are useful as kinase modulators, including MK2 modulation, wherein one of E and F is a nitrogen atom and the other of E and F is a carbon atom, and Z is N or CR 3 , and R 1 , R 2 , R 3 , X and Y are as defined herein.
摘要:
Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, and hydrates, thereof, (I) are useful as kinase modulators, including MK2 modulation, wherein one of E and F is a nitrogen atom and the other of E and F is a carbon atom, and Z is N or CR 3 , and R 1 , R 2 , R 3 , X and Y are as defined herein.
摘要:
In general, the instant invention comprises compounds of Formulas I and II including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase inhibitors and therefore are useful for treating cancer and other protein kinase mediated diseases.
摘要:
Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g. a hydrate), or a pharmaceutically-acceptable salt, thereof, wherein: M is selected from alkyl, substituted alkyl, cycloalkyl, aryl, heterocyclo, and heteroaryl, provided that if M is alkyl then R 6 and R 7 taken together with the carbon atom to which they are both attached are selected from a group other than cycloalkyl; Q is selected from (i) hydrogen, C 1 -C 4 alkyl, and substituted C 1 -C 4 alkyl; or (ii) Q and R 6 are combined with the carbon atoms to which they are attached to form a 3- to 6-membered cycloalkyl; or (iii) Q and M a M are combined with the carbon atom(s) to which they are attached to form a 3- to 7-membered ring containing 1-2 heteroatoms which are independently selected from the group consisting of O, S, SO 2 , and N which ring may be optionally substituted with 0-2 R 5 groups or carbonyl; Z is selected from cycloalkyl, heterocyclo, aryl, or heteroaryl; and M a , Z a , R 1 , R 2 , R 3 , R 4 , R 6 , R 7 , and R 22 are as defined herein. Also provided are pharmaceutical compositions and methods of treating metabolic and inflammatory- or immune-associated diseases or disorders using said compounds.
摘要翻译:提供了新的非甾体化合物,其可用于治疗与调节糖皮质激素受体,AP-1和/或NF-κB活性相关的疾病,包括具有式(I)结构的炎性和免疫疾病,肥胖症和糖尿病, 对映体,非对映异构体,互变异构体,溶剂化物(例如水合物)或其药学上可接受的盐,其中:M选自烷基,取代的烷基,环烷基,芳基,杂环和杂芳基,条件是如果M是烷基,则 R 6和R 7与它们所连接的碳原子一起选自除环烷基之外的基团; Q选自(i)氢,C 1 -C 4烷基和取代的C 1 -C 4烷基 烷基; 或(ii)Q和R 6与它们所连接的碳原子结合形成3-至6-元环烷基; 或(iii)Q和M a a M与它们所连接的碳原子一起形成含有1-2个杂原子的3-至7-元环,其独立地选自 由O,S,SO 2和N组成的基团可以任选地被0-2个R 5基团或羰基取代; Z选自环烷基,杂环基,芳基或杂芳基; 和M a a,Z a,R 1,R 2,R 3, R 4,R 6,R 7和R 22如本文所定义。 还提供了使用所述化合物治疗代谢和炎症或免疫相关疾病或病症的药物组合物和方法。