Patent classifications
C07C259/06
Methods for low temperature fluorine-18 radiolabeling of biomolecules
New chelators such as H.sub.3L1, H.sub.3L2, H.sub.3L3, H.sub.3L26 and derivatives were synthesized for the complexation of {Al.sup.18F}.sup.2+. These new chelators are able to complex {AI.sup.18F}.sup.2+ with good radiochemical yields using a labeling temperature of 37° C. The stability of the new Al.sup.18F-complexes was tested in phosphate buffered saline (PBS) at pH 7 and in rat serum. AI.sup.18F-L3 and AI.sup.18F-L26 showed a stability comparable to that of the previously reported Al.sup.18F-NODA. Moreover, the biodistribution of Al.sup.18F-L3 and AI.sup.18F-L26 showed absence of in vivo demetallation since only very limited bone uptake was observed, whereas the major fraction of activity 60 min p.i. was observed in liver and intestine due to hepatobiliary clearance of the radiolabeled ligand. The chelators H.sub.3L3 and Al.sup.18F-L26 demonstrated to be a good lead candidates for the labeling of heat sensitive biomolecules with .sup.18F-fluorine and derivatives have been synthesized. We have explored the complexation of {AI.sup.18F}.sup.2+ with new chelators and obtained very favourable radiochemical yields (>85%) using a labeling temperature of 37° C. The stability of the new Al.sup.18F-complexes was tested in phosphate buffered saline (PBS) at pH 7 and in rat serum at 37° C., where AI.sup.18F-L3 and AI.sup.18F-L26 showed a stability comparable to that of the previously reported Al.sup.18F-NODA. Moreover, the biodistribution of Al.sup.18F-L3 and Al.sup.18F-L26 showed high stability, since only very limited bone uptake—which would be an indication of release of fluorine-18 in the form of fluoride—was observed, whereas the major fraction of activity 60 min p.i. was observed in liver and intestines due to hepatobiliary clearance of the radiolabeled ligand. The chelators H.sub.3L3 and H.sub.3L26 demonstrated to be good lead candidates for the labeling of heat sensitive biomolecules with .sup.18F-fluorine and several derivatives have been synthesized.
PPAR agonists
Provided herein are compounds and compositions useful in increasing PPARδ activity. The compounds and compositions provided herein are useful for the treatment of PPARδ related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).
PPAR agonists
Provided herein are compounds and compositions useful in increasing PPARδ activity. The compounds and compositions provided herein are useful for the treatment of PPARδ related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).
CYCLOPROPYL-AMIDE COMPOUNDS AS DUAL LSD1/HDAC INHIBITORS
The present disclosure describes novel compounds of the general Formula (I), their analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites, and prodrugs thereof. These compounds can inhibit both LSD and HDAC and are useful as therapeutic or ameliorating agent for diseases that are involved in cellular growth such as malignant tumors, schizophrenia, Alzheimer's disease, parkinson's disease and the like.
##STR00001##
PHENOL DERIVATIVES FOR USE AS ANTIMICROBIAL, ANTIBACTERIAL, BACTERICIDE
Phenol derivatives of general formula (I) and (II), wherein meanings of the substituents are indicated in the description, their pharmaceutically acceptable salts, together with the processes for their preparation, their use as antimicrobial, antibacterial, bactericide agents and the corresponding pharmaceutical compositions are disclosed.
N-FORMYLHYDROXYLAMINES AS NEPRILYSIN (NEP) INHIBITORS, IN PARTICULAR AS MIXED AMINOPEPTIDASE N (APN) AND NEPRILYSIN (NEP) INHIBITORS
The present invention relates to a compound of following formula (I):
H—CO—N(OH)—CH.sub.2—CH(R.sub.1)—CO—NH—(CH.sub.2).sub.n—CH(R.sub.2)—(CH.sub.2).sub.m—CO—R.sub.3 (I) as well as a pharmaceutically acceptable salt and/or solvate thereof.
The present invention also pertains to a pharmaceutical composition comprising at least one compound of formula (I) and at least one pharmaceutically acceptable excipient.
The present invention also relates to the use of a compound of formula (I), or a pharmaceutically acceptable salt and/or solvate thereof, or a composition comprising it, as analgesic, anxiolytic, antidepressant or anti-inflammatory.
N-FORMYLHYDROXYLAMINES AS NEPRILYSIN (NEP) INHIBITORS, IN PARTICULAR AS MIXED AMINOPEPTIDASE N (APN) AND NEPRILYSIN (NEP) INHIBITORS
The present invention relates to a compound of following formula (I):
H—CO—N(OH)—CH.sub.2—CH(R.sub.1)—CO—NH—(CH.sub.2).sub.n—CH(R.sub.2)—(CH.sub.2).sub.m—CO—R.sub.3 (I) as well as a pharmaceutically acceptable salt and/or solvate thereof.
The present invention also pertains to a pharmaceutical composition comprising at least one compound of formula (I) and at least one pharmaceutically acceptable excipient.
The present invention also relates to the use of a compound of formula (I), or a pharmaceutically acceptable salt and/or solvate thereof, or a composition comprising it, as analgesic, anxiolytic, antidepressant or anti-inflammatory.
Selective histone deacetylase inhibitors for the treatment of human disease
Selective HDAC inhibitors, and pharmaceutical compositions that include the same, are described herein for the treatment of cancer, immunological diseases, inflammatory diseases, and neurological diseases.
Retinoid derivatives with antitumor activity
The present invention relates to compounds of formula (I) and to pharmaceutical compositions containing them: ##STR00001##
wherein meanings of the substituents are indicated in the description. Such compounds for use in the treatment of cancer and other diseases related to altered angiogenesis, such as arthritic pathology, diabetic retinopathy, psoriasis and chronic inflammatory disease, are also within the scope of the present invention.
Compounds and methods for delivery of prostacyclin analogs
This invention pertains generally to prostacyclin formulations and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis.