Patent classifications
C07B59/00
CXCR4 Receptor Antagonists
The compounds of formula (I) are antagonists of the CXCR4 receptor Wherein R.sup.1, X, Y and R.sup.2 are as defined in the claims.
##STR00001##
ISOTOPES OF ALPHA KETOGLUTARATE AND RELATED COMPOUNDS AND THEIR USE IN HYPERPOLARIZED IMAGING
A compound of the Formula I or a pharmaceutically acceptable salt thereof, wherein R.sub.1, Ca, Cb, Cd, and n are the same as described in the specification. Disclosed is a method of diagnosing or monitoring a patient suffering from cancer, the method comprising: administering a pharmaceutical composition comprising an effective amount of an active agent, wherein the active agent is the compound of Formula I, a pharmaceutically acceptable salt of any of the foregoing thereof, or a combination thereof, together with a pharmaceutically acceptable carrier to the patient and diagnosing or monitoring the patient by hyperpolarized .sup.13C-MRI. Also disclosed is a method of synthesizing 1-.sup.13C-5-.sup.12C-diacid.
##STR00001##
MESCALINE DERIVATIVES WITH MODIFIED ACTION
A composition for use in substance-assisted therapy, wherein: R is hydrogen, methyl, or ethyl, and R′ is C.sub.1-C.sub.5 branched or unbranched alkyl with the alkyl optionally substituted with F.sub.1-F.sub.5 fluorine substituents up to a fully fluorinated alkyl, C.sub.3-C.sub.6 cycloalkyl optionally and independently substituted with one or more substituents such as F.sub.1-F.sub.5 fluorine and/or C.sub.1-C.sub.2 alkyl, (C.sub.3-C.sub.6 cycloalkyl)-C.sub.1-C.sub.2 branched or unbranched alkyl optionally substituted with one or more substituents such as F.sub.1-F.sub.5 fluorine and/or C.sub.1-C.sub.2 alkyl, or C.sub.2-C.sub.5 branched or unbranched alkenyl with E or Z vinylic, cis or trans allylic, E or Z allylic or other double bond position in relation to the attached ether function, where any of the carbons of the branched or unbranched alkenyl substituent is optionally substituted independently with one or more C.sub.1-C.sub.2 alkyl, with F.sub.1-F.sub.5 fluorine or with D.sub.1-D.sub.5 deuteron substituents.
METHODS AND KITS FOR PREPARING RADIONUCLIDE COMPLEXES
A method for preparing a complex comprising a radioisotope of gallium for use in radiotherapy or in a medical imaging procedure, said method comprising adding a gallium radioisotope solution obtained directly from a gallium radionuclide generator to a composition comprising a pharmaceutically acceptable buffer and optionally also a pharmaceutically acceptable basic reagent, in amounts sufficient to increase the pH to a level in the range of 3 to 8, wherein the composition further comprises a chelator that is able to chelate radioactive gallium within said pH range and at moderate temperature, said chelator being optionally linked to a biological targeting agent. Kits and compositions for use in the method are also described and claimed.
METHODS AND KITS FOR PREPARING RADIONUCLIDE COMPLEXES
A method for preparing a complex comprising a radioisotope of gallium for use in radiotherapy or in a medical imaging procedure, said method comprising adding a gallium radioisotope solution obtained directly from a gallium radionuclide generator to a composition comprising a pharmaceutically acceptable buffer and optionally also a pharmaceutically acceptable basic reagent, in amounts sufficient to increase the pH to a level in the range of 3 to 8, wherein the composition further comprises a chelator that is able to chelate radioactive gallium within said pH range and at moderate temperature, said chelator being optionally linked to a biological targeting agent. Kits and compositions for use in the method are also described and claimed.
Prostate-specific membrane antigen targeted high-affinity agents for endoradiotherapy of prostate cancer
Prostate-specific membrane antigen targeted high-affinity agents for endoradiotherapy of prostate cancer are disclosed.
Neuro-attenuating ketamine and norketamine compounds, derivatives thereof, and methods
The present invention is directed to novel neuro-attenuating norketamine (NANKET) compounds according to any one of formulas (I—shown below), (I-A) and (I-B), or any of the compounds described in Tables A-D, or in any of the Examples provided herein, and pharmaceutically acceptable salts thereof, novel pharmaceutical formulations and novel methods of uses thereof. The present invention also features novel oral neuro-attenuating ketamine (NAKET) and neuro-attenuating norketamine (NANKET) modified-release pharmaceutical formulations, and novel methods of administration thereof, which ensure the steady release of a therapeutically effective amount of ketamine, norketamine, or derivatives thereof from the oral modified-release pharmaceutical formulations without neurologically toxic spikes in plasma concentration of the ketamine, norketamine, or derivatives during the release periods. ##STR00001##
CRYSTALLINE FORMS OF DEUTERIUM-ENRICHED PIOGLITAZONE
Provided herein are crystalline forms of deuterium-enriched (R)-pioglitazone and compositions thereof. Also provided herein are methods of using the crystalline forms of deuterium-enriched (R)-pioglitazone and compositions thereof.
Morphinan compounds
This disclosure relates to novel morphinan compounds and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a σ.sub.1 receptor agonist that also has NMDA antagonist activity.
Microfluidic cassette for synthesizing a radio-tracer and method of synthesizing a radio-tracer with such a cassette
The present application concerns a microfluidic cassette for synthesizing a radiotracer including a microfluidic circuit in a support card that includes at least one intake for supply by a vial, at least one isotope port, at least one reaction chamber, at least one mixing chamber, at least one formulation chamber, and at least one connection for a syringe, linked together by capillaries. Also disclosed is a method for synthesizing a radiotracer in such a cassette.