摘要:
The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.
摘要:
One embodiment of the present invention is a compound represented by the Structural Formula (I): Y is a covalent bond of a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C=Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 is an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, or a substituted non-aromatic heterocyclic group, R2-R4 are independently —H, an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, a substituted non-aromatic heterocyclic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is ═O or ═S. Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent.
摘要翻译:本发明的一个实施方案是由结构式(I)表示的化合物:Y是取代或未取代的直链烃基的共价键。 此外,Y与它所键合的两个> C = Z基团一起是取代或未取代的芳族基团。 优选地,Y是共价键或-C(R 7 R 8) - 。 R 1是脂族基团,取代的脂族基团,非芳族杂环基团或取代的非芳香族杂环基团,R 2 -R 4 独立地,-H,脂族基团,取代的脂族基团,非芳香族杂环基,取代的非芳族杂环基,芳基或取代的芳基,或R 1, SUB和R 3与它们所键合的碳原子和氮原子一起,和/或R 2和R 4结合在一起 与其键合的碳原子和氮原子形成任选地稠合到芳香环的非芳族杂环。 R 5 -R 6独立地是-H,脂族基团,取代的脂族基团,芳基或取代的芳基。 R 7和R 8各自独立地为-H,脂族或取代的脂族基团或R 7为-H, 8是取代或未取代的芳基,或者R 7和R 8一起是C2-C6取代或未取代的亚烷基。 Z是-O或-S。 还公开了包含本发明化合物和药学上可接受的载体或稀释剂的药物组合物。
摘要:
This invention relates to fused pyrrole compounds of Formula (I): and pharmaceutically acceptable salts and prodrugs thereof, wherein V1, V2, V3, V4, R1, R2, R3, W1 and W2 are as defined herein. The compounds of this invention may be used to prevent or treat cancer, inflammatory disorders, autoimmune diseasesand other conditions involving PDE4 or elevated levels of cytokines. The invention also provides methods of using the compounds to treat or prevent such disorders and pharmaceutical compositions containing the compounds.
摘要:
A silver halide photographic material comprising a support having thereon at least one silver halide emulsion layer, said emulsion layer or at least one of other hydrophilic colloid layers containing a compound represented by formula (I):PWR--Time--.sub.T LA (I)wherein PWR represents a group which undergoes reduction to release (Time).sub.t LA; Time represents a group which release LA upon reaction following release of (Time).sub.t LA from PWR; t represents an integer of 0 or 1; and LA represents a group having a maximum light absorption in a wavelength range of 310 nm or more. In a preferred embodiment, one of said other hydrophilic colloid layers substantially free of the compound represented by formula (I) is provided between said at least one silver halide emulsion layer in said silver halide photographic material and one of said other hydrophilic colloid layers containing the compound represented by formula (I), and at least one of these hydrophilic colloid layers or at least one other of said other hydrophilic colloid layers contains a hydrazine derivative. A process for the formation of an ultrahigh contrast image, which comprises exposing the above-described silver halide photographic material to light, and then developing the silver halide photographic material with a developing solution having a pH of 11.0 to 12.3 and containing 0.15 mol/l or more of sulfite ions.
摘要:
Disclosed are compounds of formulae (I), (III), (IV), (VII), (X), (XI), (XII), (XIII) and (XIV), wherein the variables are as defined in the claims, and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
摘要:
The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
摘要:
Disclosed herein are oral formulations of bis(thio-hydrazide amides) compounds of the following structural formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R7, R8, Z, and Y are defined herein.
摘要:
Disclosed are compounds of formulae (I), (III), (IV), (VII), (X), (XI), (XII), (XIII) and (XIV), wherein the variables are as defined in the claims, and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
摘要:
The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.
摘要:
The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.