Patent classifications
C07C229/48
PROCESS FOR PREPARING SUBSTITUTED CYCLOHEXANE AMINO ACID ESTERS AND SPIROKETAL-SUBSTITUTED CYCLIC KETO-ENOLS
The present invention relates to a novel process for preparing substituted cyclohexane amino acid esters and spiroketal-substituted cyclic keto-enols, and to novel intermediates or starting compounds that are passed through or used in the process according to the invention.
THERAPEUTIC COMPOUNDS AND METHODS OF USE THEREOF
The invention provides compounds having the general formula I:
##STR00001##
and pharmaceutically acceptable salts thereof, wherein the variables R.sup.AA, n, ring A, X.sup.1, L, m, X.sup.2, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X, and R.sup.6 have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
THERAPEUTIC COMPOUNDS AND METHODS OF USE THEREOF
The invention provides compounds having the general formula I:
##STR00001##
and pharmaceutically acceptable salts thereof, wherein the variables R.sup.AA, n, ring A, X.sup.1, L, m, X.sup.2, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X, and R.sup.6 have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF
Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF
Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
Preparation of 18F-fluciclovine
The present invention provides a method for the production of [.sup.18F]-FACBC which has advantages over know such methods. Also provided by the present invention is a system to carry out the method of the invention and a cassette suitable for carrying out the method of the invention on an automated radiosynthesis apparatus.
Preparation of 18F-fluciclovine
The present invention provides a method for the production of [.sup.18F]-FACBC which has advantages over know such methods. Also provided by the present invention is a system to carry out the method of the invention and a cassette suitable for carrying out the method of the invention on an automated radiosynthesis apparatus.
ATX modulating agents
Disclosed are bicyclic aryl compounds of formula (I), that can modulate the activity of the autotaxin (ATX) enzyme. This invention further relates to compounds that are ATX inhibitors, and methods of making and using such compounds in the treatment of demyelination due to injury or disease, as well as for treating proliferative disorders such as cancer.
Radiolabelling Process
The present invention relates to a novel composition comprising 1-amino-3-[.sup.18F]-fluorocyclobutanecarboxylic acid ([.sup.18F]-FACBC) wherein said composition has certain superior properties in comparison with known compositions comprising [.sup.18F]-FACBC. Also provided by the invention is a method to obtain said composition.
Radiolabelling Process
The present invention relates to a novel composition comprising 1-amino-3-[.sup.18F]-fluorocyclobutanecarboxylic acid ([.sup.18F]-FACBC) wherein said composition has certain superior properties in comparison with known compositions comprising [.sup.18F]-FACBC. Also provided by the invention is a method to obtain said composition.