摘要:
The present invention provides, inter alia, crystals of the MEK1 polypeptide which are particularly useful for structure based drug design as well as methods of use thereof.
摘要:
The present invention relates to crystals of the ERK2 polypeptide and complexes thereof which are useful, inter alia, for structure assisted drug design.
摘要:
The present invention relates to crystals of the ERK2 polypeptide and complexes thereof which are useful, inter alia, for structure assisted drug design.
摘要:
The present invention relates to crystals of the ERK2 polypeptide and complexes thereof which are useful, inter alia, for structure assisted drug design.
摘要:
The present invention relates to crystals of the ERK2 polypeptide and complexes thereof which are useful, inter alia, for structure assisted drug design.
摘要:
The present invention relates to crystals of the ERK2 polypeptide and complexes thereof which are useful, inter alia, for structure assisted drug design.
摘要:
The present invention provides a method of diagnosing the presence or severity of tissue fibrosis in an individual by detecting α2-macroglobulin (α2-MG) in a sample from the individual; detecting hyaluronic acid (HA) in a sample from the individual; detecting tissue inhibitor of metalloproteinases-1 (TIMP-1) in a sample from the individual; and diagnosing the presence or severity of tissue fibrosis in the individual based on the presence or level of α2-MG, HA and TIMP-1.
摘要:
The present invention relates to trans-capsularly administering into a diseased joint a high specificity antagonist selected from the group consisting of: i) an inhibitor of a pro-inflammatory interleukin; ii) an inhibitor of TNF-α synthesis; iii) an inhibitor of membrane-bound TNF-α; iv) an inhibitor of a natural receptor of TNF-α; v) an inhibitor of NO synthase, vi) an inhibitor of PLA2 enzyme; vii) an anti-proliferative agent; viii) an anti-oxidant; ix) an apoptosis inhibitor selected from the group consisting of EPO mimetic peptides, EPO mimetibodies, IGF-I, IGF-II, and caspase inhibitors, and x) an inhibitor of MMPs; and xi) an inhibitor of p38 kinase.
摘要:
A method of synthesizing a compound of formula I: comprising the step of reacting a moiety of formula II: with a moiety of formula III: in compressed carbon dioxide in the presence of a transition metal catalyst and a base, wherein L is a labile leaving group; RN1 is optionally substituted C5-20 aryl; RN2 is selected from optionally substituted C5-20aryl, optionally substituted C3-20 heterocyclyl, optionally substituted C3-7 alkyl, and optionally substituted sulfonyl; RN3 is selected from H and optionally substituted C1-7 alkyl, C3-20 heterocyclyl and C5-20 aryl; or RN2 and RN3 together with the nitrogen atom to which they are attached form optionally substituted nitrogen-containing C3-20 heterocylyl or C5-20 heteroaryl; and R1 R2 and R3 are independently selected from optionally substituted C1-7 alkyl, C5-20 aryl, C3-20 heterocyclyl, hydroxy, halo, amino and C1-7 alkoxy, or two of R1, R2 and R3, together with the silicon atom to which they are attached, may form a silicon containing C5-7 heterocyclyl group.
摘要翻译:合成式I化合物的方法:包括使式II部分与式III部分反应的步骤:在过渡金属催化剂和碱的存在下,在压缩二氧化碳中,其中L是不稳定的离去 组; R 01是任选取代的C 5-20芳基; R N2选自任选取代的C 5-20芳基,任选取代的C 3-20杂环基,任选取代的C 3-8芳基, 7烷基和任选取代的磺酰基; R N 3选自H和任选取代的C 1-7 - 烷基,C 3-20 - 杂环基和C 5-20杂环基, / SUB>芳基; 或R N2和R N3与它们所连接的氮原子一起形成任选取代的含氮C 3-20异氰酸酯或C 5-20杂芳基; R 1和R 3独立地选自任选取代的C 1-7烷基,C 1 -C 6烷基, 羟基,卤素,氨基和C 1-7 - 烷氧基,或者R 1,R 2,R 2, 1,R 2和R 3与它们所连接的硅原子一起可以形成含有C 5-7的硅, / SO 2杂环基。