Patent classifications
C07D295/195
Compounds useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase
Compounds of formula (VII), which are useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase, are provided. Also provided are pharmaceutical compositions, kits comprising said compounds, and methods and uses pertaining to said compounds.
Urea/carbamates FAAH MAGL or dual FAAH/MAGL inhibitors and uses thereof
Disclosed are compounds of general formulas I-III that may be used to inhibit the action of fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL) or dual FAAH/MAGL. ##STR00001##
Urea/carbamates FAAH MAGL or dual FAAH/MAGL inhibitors and uses thereof
Disclosed are compounds of general formulas I-III that may be used to inhibit the action of fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL) or dual FAAH/MAGL. ##STR00001##
ANTIOXIDANT INFLAMMATION MODULATORS: OLEANOLIC ACID DERIVATIVES WITH AMINO AND OTHER MODIFICATIONS AT C-17
This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula:
##STR00001##
wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
CXCR6 SULFONAMIDE COMPOUNDS
Provided are sulfonamide compounds having formula (I):
##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and the subscripts n and m have the meanings provided in the specification. The compounds are useful for treating diseases and conditions associated with CXCR6 activity.
CXCR6 SULFONAMIDE COMPOUNDS
Provided are sulfonamide compounds having formula (I):
##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and the subscripts n and m have the meanings provided in the specification. The compounds are useful for treating diseases and conditions associated with CXCR6 activity.
Hydroxamic acid derivative, method for producing same and use thereof
The present disclosure is related to the field of enzyme inhibitors, and in particular to a hydroxamic acid derivative, a method for producing the same and use thereof. The hydroxamic acid group of the hydroxamic acid derivative can be chelated with zinc ions in the LpxC active area, and the derivative has a hydrophobic side chain which can bind to hydrophic channels in the enzyme LpxC. These guarantee that the hydroxamic acid derivative has good bactericidal activity against Gram-negative bacteria and low toxicity. The present disclosure also provides a method for producing the hydroxamic acid derivative, which requires a shorter reaction time and can provide the derivative with a high yield.
Hydroxamic acid derivative, method for producing same and use thereof
The present disclosure is related to the field of enzyme inhibitors, and in particular to a hydroxamic acid derivative, a method for producing the same and use thereof. The hydroxamic acid group of the hydroxamic acid derivative can be chelated with zinc ions in the LpxC active area, and the derivative has a hydrophobic side chain which can bind to hydrophic channels in the enzyme LpxC. These guarantee that the hydroxamic acid derivative has good bactericidal activity against Gram-negative bacteria and low toxicity. The present disclosure also provides a method for producing the hydroxamic acid derivative, which requires a shorter reaction time and can provide the derivative with a high yield.
Heterocyclylmethylidene derivatives and their use as modulators of mGluR5 receptors
This invention relates to compounds of formula (I) and their use as allosteric modulators of mGluR5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for the treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction, such as schizophrenia or cognitive decline, dementia or cognitive impairment, or other pathologies that can be related directly or indirectly to glutamate dysfunction. ##STR00001##
HIGH-THROUGHPUT METHOD TO RAPIDLY ADD CHEMICAL MOIETIES TO A SMALL MOLECULE LIBRARY
Organic compounds for target identification, drug discovery, chemical library production, high-throughput screening, fluorophore conjugation, chemiluminescent compound conjugation, creation of proximity induced modulators (e.g., protein degraders)/chimeric molecules, or a combination thereof are described. The compounds can contain small molecule moieties for identification of their potential targets; an isocyanate, photoactivatable groups; chemical moieties for enrichment and detection of target-small molecule moiety interactions; proximity induced modulator element; fluorophores; chemiluminescent groups; or combinations thereof.