Patent classifications
C07B59/00
Deuterated analogs of etifoxine, their derivatives and uses thereof
This invention relates to deuterated analogs of etifoxine of Formula 1, solvates, prodrugs, and pharmaceutically acceptable salts thereof, as well as to methods for their preparation and use, and to pharmaceutical compositions. Briefly, this invention is generally directed to deuterated analogs of etifoxine as well as to methods for their preparation and use, and to pharmaceutical compositions containing the same.
GRP-R agonistic 177-lutetium-labeled bombesin derivatives for diagnosis and treatment of prostate cancer
Provided is a novel compound capable of being usefully used to diagnose and treat prostate cancer by labeling a radioisotope on a bombesin derivatives capable of selectively targeting a target material over-expressed in tumor cells in order to develop an effective diagnose and treatment method of diseases associated with prostate cancer.
NOVEL COMPOUNDS FOR DIAGNOSIS
The present invention relates to novel compounds of formula (I), or a detectably labelled compound, stereoisomer, racemic mixture, pharmaceutically acceptable salt, hydrate, or solvate thereof, that can be employed in the imaging of alpha-synuclein aggregates and determining an amount thereof. Furthermore, the compounds can be used for diagnosing a disease, disorder or abnormality associated with an alpha-synuclein aggregates, including, but not limited to, Lewy bodies and/or Lewy neurites (such as Parkinson's disease), determining a predisposition to such a disease, disorder or abnormality, prognosing such a disease, disorder or abnormality, monitoring the evolution of the disease in a patient suffering from such a disease, disorder or abnormality, monitoring the progression of such a disease, disorder or abnormality and predicting responsiveness of a patient suffering from such a disease, disorder or abnormality to a treatment thereof.
2',2'-DIHALO NUCLEOSIDE ANALOGS FOR TREATMENT OF THE FLAVIVIRIDAE FAMILY OF VIRUSES AND CANCER
The present invention is directed to compounds, compositions and methods for treating or preventing Flaviviridae family of viruses (including HCV, Yellow fever, Dengue, Chikungunya Ebola and West Nile virus), RSV, HEV, and influenza infection and cancer in human subjects or other animal hosts.
F-18 LABELED TRACER AND METHODS OF MANUFACTURE
A method of producing a radiofluorinated compound comprising the steps of forming a reaction mixture comprising a reactant having a formula of R—Y and a radiofluorinating agent having a formula of R′—.sup.18F; and contacting the reaction mixture with microwave radiation to achieve a temperature of between 100° C. and 250° C. for a time sufficient to convert at least 10% of the reactant into the radiofluorinated compound having a formula of R—.sup.18F, wherein R is selected from the group consisting of an alkyl (C.sub.1-C.sub.20), a cycloalkyl (C.sub.3-C.sub.10), an aryl, a heteroaryl, an aralkyl and an alkenyl group (C.sub.2-C.sub.20); Y is selected from the group consisting of a sulfonate, a nitro, an acetate and a halogen; and R′ is selected from the group consisting of an alkali metal cation, an alkaline earth metal cation, a transition metal cation, an ammonium cation, and a tetraalkylammonium cation is provided.
Isoindolinone inhibitors of the MDM2-P53 interaction having anticancer activity
- Gianni Chessari ,
- Steven Howard ,
- Ildiko Maria Buck ,
- Benjamin David Cons ,
- Christopher Norbert Johnson ,
- Rhian Sara Holvey ,
- David Charles Rees ,
- Jeffrey David St. Denis ,
- Emiliano Tamanini ,
- Bernard Thomas Golding ,
- Ian Robert Hardcastle ,
- Celine Florence Cano ,
- Duncan Charles Miller ,
- Martin Edward Mäntylä Noble ,
- Roger John Griffin ,
- James Daniel Osborne ,
- Joanne Peach ,
- Arwel Lewis ,
- Kim Louise Hirst ,
- Benjamin Paul Whittaker ,
- David Wyn Watson ,
- Dale Robert Mitchell
The invention provides a compound of formula (I): ##STR00001##
or tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the various substituents are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds.
[18F]-labelled lactate derivative as PET radiotracer
A positron emission tomography (PET) radiotracer for imaging lactate uptake, wherein the tracer is [.sup.18F]-3-fluoro-2-hydroxypropionic acid, or a pharmaceutical acceptable salt and/or solvate thereof. Also, a process for the radiosynthesis of [.sup.18F]-3-fluoro-2-hydroxypropionic acid, or a pharmaceutical acceptable salt and/or solvate thereof. Further, the use of [.sup.18F]-3-fluoro-2-hydroxypropionic acid, or a pharmaceutical acceptable salt and/or solvate thereof, for imaging lactate uptake in living cells, especially in humans.
DEUTERATED HETEROARYL SULFONAMIDES AND THEIR USE
Compunds are provided that act as potent antagonists of the CCR2 receptor. These compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives that include deuterium modifications and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.
PET IMAGING WITH PD-L1 BINDING POLYPEPTIDES
Provided herein are novel .sup.10Fn3 domains which specifically bind to PD-L1, as well as imaging agents based on the same for diagnostics.
PET IMAGING WITH PD-L1 BINDING POLYPEPTIDES
Provided herein are novel .sup.10Fn3 domains which specifically bind to PD-L1, as well as imaging agents based on the same for diagnostics.