Patent classifications
C07D239/47
INHIBITORS OF LRRK2 KINASE
Compounds having activity as inhibitors of LRRK2 kinase are provided. The compounds have Structure (I):
##STR00001##
or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein A, B, R.sup.1a, R.sup.1b, R.sup.2 and L are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of LRRK2 kinase are also provided.
Cellular transport system for transferring a sulfonic acid construct carrying a cargo into the cytoplasm of a cell
The present invention relates to a cellular transport system for bringing a sulfonic acid construct which carries a cargo into a cell and releasing the cargo in the cell's cytoplasm, the cellular transport system comprising: (i) a sulfonate transporter located in the cytoplasm membrane of the cell wherein said sulfonate transporter is capable of transporting said sulfonic acid construct across the cytoplasm membrane into the cytoplasm; (ii) a γ-glutamyl transferase (GGT; EC 2.3.2.2) which is modified to be located in the cytoplasm of the cell, wherein said γ-glutamyl transferase is capable of hydrolyzing said sulfonic acid construct so as to release the cargo. Moreover, the present invention relates to the use of a cellular transport system for bringing a sulfonic acid construct which contains a cargo into a cell and releasing the cargo in the cell's cytoplasm. Further, the present invention relates to a γ-glutamyl transferase for hydrolyzing a sulfonic acid construct which contains a cargo.
Antimicrobial Compounds and Methods
The invention is directed to compounds that are active as antibacterial agents. The invention compounds are active against gram-positive and gram-negative bacteria and can be used to treat infections caused by gram-positive and gram-negative bacteria. Also disclosed are processes and intermediates for making the compounds.
SUBSTITUTED DIAMINOCARBOXAMIDE AND DIAMINOCARBONITRILE PYRIMIDINES, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
Provided herein are Diaminopyrimidine Compounds having the following structures:
##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidine Compound, and methods for treating or preventing liver fibrotic disorders or a condition treatable or preventable by inhibition of a JNK pathway.
SUBSTITUTED DIAMINOCARBOXAMIDE AND DIAMINOCARBONITRILE PYRIMIDINES, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
Provided herein are Diaminopyrimidine Compounds having the following structures:
##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidine Compound, and methods for treating or preventing liver fibrotic disorders or a condition treatable or preventable by inhibition of a JNK pathway.
Processes for preparing a diaminopyrimidine derivative or acid addition salt thereof
The present invention provides a novel process for preparing a diaminopyrimidine derivative or acid addition salt thereof having an activity as a 5-HT.sub.4 receptor agonist. And also, the present invention provides novel crystalline forms of a hydrochloride of the diaminopyrimidine derivative and processes for preparing the same.
Processes for preparing a diaminopyrimidine derivative or acid addition salt thereof
The present invention provides a novel process for preparing a diaminopyrimidine derivative or acid addition salt thereof having an activity as a 5-HT.sub.4 receptor agonist. And also, the present invention provides novel crystalline forms of a hydrochloride of the diaminopyrimidine derivative and processes for preparing the same.
Antimicrobial Compounds and Methods
The invention is directed to compounds that are active as antibacterial agents. The invention compounds are active against gram-positive and gram-negative bacteria and can be used to treat infections caused by gram-positive and gram-negative bacteria. Also disclosed are processes and intermediates for making the compounds.
Antimicrobial Compounds and Methods
The invention is directed to compounds that are active as antibacterial agents. The invention compounds are active against gram-positive and gram-negative bacteria and can be used to treat infections caused by gram-positive and gram-negative bacteria. Also disclosed are processes and intermediates for making the compounds.
JNK INHIBITOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF
A compound of formula (I), and racemates, stereoisomers, tautomers, isotopic markers, solvates, polymorphs and oxynitrides of the compound, or a pharmaceutically acceptable salt thereof can be used as JNK inhibitors. A method for preparing the compound of formula (I) and a pharmaceutical composition comprising the compound of formula (I) are provided. The compound of formula (I) can be used for preparing drugs. The resulting drugs are used for treating diseases that can be treated by inhibiting JNK activity.
##STR00001##