摘要:
The present invention relates to a polymer composed by two to ten monomers of formula (I) as well as to a process for its preparation and its use as fluorophore wherein: X is a radical of formula (II) wherein —R5 is an electron pair or a (C1-C3)-alkyl radical; —Ra and —Rb are radicals independently selected from the group consisting of H, (C1-C4)-alKyI, (C1-C4)-alkoxy, (C1-C4)-alkylamino, phenyl, F, Cl, Br, amino, hydroxy, and nitro or —Ra and —Rb are fused forming with the carbon atoms to which they are attached a ring of formula (III) with the condition that (I) when —R5 is an electron pair, a is a N═C double bond, and Ra and Rb are fused forming the ring (III), said ring being a biradical selected from (IIIa) and (IIIb), thus, radical (II) is (IIa) or (IIb) respectively (II) when —R5 is a (C1-C3)-alkyl radical, a is a N—C single bond and Ra and Rb are fused forming the ring (III), said ring being a biradical (a), thus, the radical (II) is (IIc) R1-R4 and R7-R18 represent radicals, same or different, selected for the group consisting of H1 (C1-C4)-alkyl, (C1-C4)-alky-lamiπo, phenyl, F, Cl, Br, amino, hydroxy, and nitro; p is an integer from 0 to 1; R6 is a biradical selected from the group consisting of —CO—; —CONH(CH2)mCO—; and —CO[NHCHR″CO]m—, wherein —R″ are side chains radicals, same or different, corresponding to natural aminoacids; and m is an integer from 1 to 3; Z is a triradical of formula (IV) wherein r is an integer from 0 to 1; v is an integer from O to 1; Z′ is a triradical selected from —CH2— and nitrogen; Z″ is H, with the proviso that: (a) when Z′ is nitrogen, forming an amide bound with R6, then is hydrogen and v is an integer from O to 1, and (b) when Z″ is —NH—, forming an amide group with R6, then Z1 is —CH2 and v=O or of formula (V) wherein Z″ is selected from —CH3 and —CH2NH—, Z1v is selected from H and NH, Zv is selected from S and O atom, W is an integer from 0 to 1, with the proviso that (c) when R6 is bound to Z′″ then Z′″ is —CH2NH—, Z1v is hydrogen and w is 0; and (d) when Z1v is —NH— forming an amide bound with R6, Z′″ is —CH3 and w is 1; and and wherein the monomers of formula (I) are linked through the triradical Z, forming an amide or phosphate bound.
摘要:
The invention provides compounds of Formula (I): and Formula (II) or a pharmaceutically-acceptable salt, solvate, or hydrate thereof. Compounds of this invention, or pharmaceutical compositions thereof, are useful for treating diabetes, elevated plasma glucose levels, and/or ketoacidosis in mammals.
摘要:
This invention provides compounds and pharmaceutical compositions thereof for treating human type 1 and type 2 diabetes, particularly insulin-resistant diabetes.
摘要:
This invention is directed to inhibitors of copper-containing amine oxidases (E.C.1.4.3.6) including semicarbazide-sensitive amine oxidase (SSAO; also known as vascular adhesion protein-1, VAP-I), and their therapeutic use in inflammatory diseases, diabetes and its associated complications, atherosclerosis, neurodegenerative diseases, obesity, hypertension and cancer.
摘要:
This invention is directed to inhibitors of copper-containing amine oxidases (E.C. 1.4.3.6) including semicarbazide-sensitive amine oxidase (SSAO; also known as vascular adhesion protein-1, VAP-1), and their therapeutic use in inflammatory diseases, diabetes and its associated complications, atherosclerosis, neurodegenerative diseases, obesity, hypertension and cancer.