Abstract:
Provided herein are novel substituted thiazoles and oxazoles of the Formula (I):[Insert Formula (I)]as well as compositions, including pharmaceutical compositions, containing the same, and the use thereof in the treatment of various neurological and psychological disorders, e.g., affective disorder, anxiety and depression, treatable by antagonizing CRF receptors.
Abstract:
Compounds of formula (I) and pharmaceutically acceptable salts, solvates and hydrolysable esters thereof wherein X is O or S; X is O or S; X is S or O; R and R are independently H, methyl, or halogen; R and R are independently H or C1-3 alkyl or R and R may, together with the carbon atom to which they are bonded, form a 3-5 membered cycloalkyl ring; R and R are independently H, C1-3 alkyl, or allyl; each R is independently halogen, C1-6 straight or branched alkyl, or CF3; and y is 0, 1, 2, 3, 4 or 5 act as hPPAR alpha agonists.
Abstract translation:式(I)化合物及其药学上可接受的盐,溶剂合物和可水解的酯,其中X是O或S; X 1是O或S; X是S或O; R 1和R 2独立地是H,甲基或卤素; R 4和R 5独立地为H或C 1-3烷基或R 4和R 5可以与它们所键合的碳原子一起形成3-5元环烷基环; R 6和R 7独立地为H,C 1-3烷基或烯丙基; 每个R 3独立地是卤素,C 1-6直链或支链烷基或CF 3; y为0,1,2,3,4或5作为hPPARα激动剂。
Abstract:
This invention generally relates to nanocrystal compounds, and linker arm for nanocrystal compounds that attach the nanocrystals to the organic compounds. The nanocrystal compound comprises a nanocrystal, linker arm, and organic compound. Preferably, the organic compound is a biologically active compound that can provide a fluorescent sensor. Preferably, the linker arm is a polyether chain with an attachment point for the nanocrystal and an attachment point for the organic compound. Specifically, the nanocrystal is attached to the linker arm through a R group and the organic compound is attached to the linker arm through a R2 group.R is a bond or is selected from the group consisting of: SH, O(CH2(n)O)nSH, NH(CH2(n)O)nSH, NH(CH2(n)NH)SH, S(CH2(n)O)nSH, and S(CH2(n)S)SH. n is 1-10, with S being attached to the nanocrystal. R2 is a bond or selected from the group consisting of carbonyl, NH, S, CONH, COO, S, C1-10 alkyl, carbamate, and thiocarbamate.
Abstract:
The invention concerns compounds of general formula (I) wherein: R1 represents either a hydrogen atom, or an amino group, or a C1-C4 alkyl group, or a C1-C6 alkoxycarbonyl group, or a -OH group; R2 represents either a C1-C6 alkyl group, or a phenyl or benzyl group, or a -CH2Q group, wherein Q is a heterocyclic group; R3 and R5 represent independently of each other for example either a hydrogen atom, or a C1-C4 alkyl group, or a -COOH group; R4 represents either a hydrogen atom, or a C1-C4 alkyl group, or a -(CH2)p-COOR8 group; Z represents either a -CH- group, or a nitrogen atom. The invention also concerns the methods of preparation and therapeutic use of said compounds.
Abstract:
The invention encompasses the novel compound of Formula (I) useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula (I).
Abstract:
Thionaphthalene derivatives represented by formula (I) and nontoxic salts thereof, wherein R represents hydrogen, (un)substituted C1 to C5 alkyl, (un)substituted aryl, heterocyclic group, R4CO- (wherein R4 represents (un)substituted C¿1? to C5 alkyl, (un)substituted aryl, or heterocyclic group), R?5¿OCO- (wherein R5 represents hydrogen, (un)substituted C¿1? to C10 alkyl, (un)substituted C3 to C10 alkenyl, or (un)substituted C5 to C7 cycloalkyl), R?6¿NHCO- (wherein R6 represents (un)substituted C¿1? to C5 alkyl, (un)substituted aryl, or heterocyclic group), or cyano; R?1 and R2¿ represent each independently hydrogen, C¿1? to C5 alkyl, or phenyl; R?3¿ represents hydrogen, C¿1? to C5 alkyl, or R?7¿CO- (wherein R7 represents -OR?81, -R82¿, or -NR¿2??83, and R81, R82 and R83¿ represent each C¿1? to C4 alkyl); and n represents an integer of 0 to 2.
Abstract:
The disclosure provides compounds, compositions, and methods for modulating PPARd receptor. In one embodiment, the compounds of the disclosure comprise a tri-substituted thiazole group. The substituent at the 2-position of the thiazole group provides steric bulk to the compounds. The compounds, compositions, and methods may be useful, for example, in the treatment of cancer.