Patent classifications
C07D215/00
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.
Substituted spirocycles
This invention relates to a compound of formula I ##STR00001##
wherein A and Cy have one of the meanings as indicated in the specification and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
Quinolinone-carboxamide compounds as 5-HT4 receptor agonists
The invention provides novel quinolinone-carboxamide 5-HT.sub.4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT.sub.4 receptor activity, and processes and intermediates useful for preparing such compounds.
Production method for T cells or NK cells, medium for culturing T cells or NK cells, method for culturing T cells or NK cells, method for maintaining undifferentiated state of undifferentiated T cells, and growth-accelerating agent for T cells or NK cells
The present invention relates to a method for producing T cells or NK cells including culturing T cells or NK cells in a culture medium containing a CaMKII inhibitor such as a bisbenzylisoquinoline alkaloid compound. The disclosed compounds and methods can be used for maintaining the undifferentiated state of undifferentiated T cells, or for efficiently proliferating T cells or NK cells.
Production method for T cells or NK cells, medium for culturing T cells or NK cells, method for culturing T cells or NK cells, method for maintaining undifferentiated state of undifferentiated T cells, and growth-accelerating agent for T cells or NK cells
The present invention relates to a method for producing T cells or NK cells including culturing T cells or NK cells in a culture medium containing a CaMKII inhibitor such as a bisbenzylisoquinoline alkaloid compound. The disclosed compounds and methods can be used for maintaining the undifferentiated state of undifferentiated T cells, or for efficiently proliferating T cells or NK cells.
Substituted quinoline compounds as S-nitrosoglutathione reductase inhibitors
The present invention is directed to novel quinoline compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
Substituted quinoline compounds as S-nitrosoglutathione reductase inhibitors
The present invention is directed to novel quinoline compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
Quinoline compounds
The present invention relates to quinoline compounds as defined by Formula I below. Such quinoline compounds have been shown to inhibit the formation of amyloid deposits (e.g., amyloid oligomers, fibrils or plaques). Consequently, these compounds are suitable for treating a range of diseases and disorders in which amyloid deposits are implicated, such as type-2 diabetes and Alzheimer's disease. ##STR00001##
Process for the preparation of optically active isoxazoline compounds
The present invention relates to a process for the preparation of a compound of formula (I) wherein A.sub.1 and A.sub.2 are CH, or one of A.sub.1 and A.sub.2 is CH and the other is N; R.sub.1 is C.sub.1-C.sub.4alkyl, C.sub.1-C.sub.4haloalkyl or C.sub.3-C.sub.6cycloalkyl; each R.sub.2 is independently bromo, chloro, fluoro or trifluoromethyl; R.sub.3 is hydrogen; R.sub.4 is hydrogen, halogen, methyl, halomethyl or cyano; or R.sub.3 and R.sub.4 together form a bridging 1,3-butadiene group; R.sub.5 is chlorodifluoromethyl or trifluoromethyl; n is 2 or 3; by reacting a compound of formula (II) wherein A.sub.1, A.sub.2, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and n is as defined under formula (I) above, with hydroxylamine, a base and a chiral catalyst, characterized in that the chiral catalyst is a dimeric chiral catalyst of formula (III) wherein R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and X are as defined in claim 1. ##STR00001##
CGRP receptor antagonists
The disclosures herein relate to novel compounds of formula ##STR00001##
wherein R.sup.1, R.sup.2 and R.sup.3 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.