Abstract:
The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibitng kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.
Abstract:
Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
Abstract:
Compounds of formula A - Y - D - E - G - J - Z - L in which D is direct link, a substutited or unsubstituted phenyl or napththyl group or a heterocyclic ring system; and the other variables are as defined in the claims, their salts and compositions relating thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
Abstract:
The present invention describes a direct interaction between myosin and the cytoplasmic domain of membrane proteins, particularly the phosphorylated cytoplasmic domains of the beta -subunit of integrins. The invention provides methods of identifying agents which block integrin binding to myosin, methods of using agents which block integrin binding to myosin to modulate biological and pathological processes, and provides agents that block integrin mediated binding to myosin and thereby modulate related cellular or cellular component movement.
Abstract:
Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
Abstract:
A method for selectively inhibiting a kinase is disclosed, which comprises contacting a composition containing a kinase with a compound of formula (I), wherein: R1 is lower alkyl, lower hydrocarbyl, aryl lower alkyl, heteroaryl lower alkyl, 5- or 6-membered heterocyclic aromatic, polyaromatic, polyaromatic carbonyl, polyheteroaromatic or polyheteroaromatic carbonyl; R2 is lower alkyl, lower hydrocarbyl, aryl lower alkyl, heteroaryl lower alkyl, 5- or 6-membered heterocyclic aromatic, lower hydrocarboyl, 5- or 6-membered heterocyclic aromatic carbonyl, polyaromatic or polyheteroaromatic; R3 is H or lower alkyl; R5 is H, lower alkyl, lower hydrocarbyl, aryl lower alkyl, heteroaryl lower alkyl, 5- or 6-membered heterocyclic aromatic, halogen, or cyano; and R6 is H or lower hydrocarboyl.
Abstract translation:公开了选择性抑制激酶的方法,其包括将含有激酶的组合物与式(I)化合物接触,其中:R 1是低级烷基,低级烃基,芳基低级烷基,杂芳基低级烷基,5-或6- 多芳基,多芳基羰基,多杂芳基或多杂芳基羰基; R 2是低级烷基,低级烃基,芳基低级烷基,杂芳基低级烷基,5-或6-元杂环芳族,低级烃基,5-或6-元杂环芳族羰基,多芳族或多杂芳族; R3是H或低级烷基; R5是H,低级烷基,低级烃基,芳基低级烷基,杂芳基低级烷基,5-或6-元杂环芳族,卤素或氰基; R6为H或低级烃基。
Abstract:
A process, as shown in the figure, for producing a highly purified preparation of an inhibited form of an activated blood factor entails providing a partially purified preparation containing the blood factor of interest, treating the partially purified preparation to convert the blood factor to an inhibited activated form in a single step, and then purifiying the resulting inhibited activated blood factor.