Patent classifications
C07C223/02
Substituted amines as disrupters of ABETA42 oligomer formation
The present disclosure provides small molecule drugs and pharmaceutical compositions for the treatment and prevention of diseases related to the formation of Aβ42 oligomers in a subject. It further provides a method of reducing formation of or disrupting Aβ42 oligomers in a subject, the method comprising the step of administering to the subject in need thereof a therapeutically effective amount of a pharmaceutical composition. One such compound is a compound of formula 120: ##STR00001##
3-(5-CHLORO-2-OXOBENZO[D]OXAZOL-3(2H)-YL) PROPANOIC ACID DERIVATIVES AS KMO INHIBITORS
A compound of formula (I) or a salt thereof are provided:
##STR00001##
wherein R.sup.1, X and R.sup.3 are defined in the specification, useful in the treatment of disorders mediated by KMO such as acute pancreatitis, chronic kidney disease, other conditions associated with systemic inflammatory response syndrome (SIRS), Huntington's disease, Alzheimer's disease, spinocerebellar ataxias, Parkinson's disease, AIDS-dementia complex, amylotrophic lateral sclerosis (ALS), depression, schizophrenia, sepsis, cardiovascular shock, severe trauma, acute lung injury, acute respiratory distress syndrome, acute cholecystitis, severe burns, pneumonia, extensive surgical procedures, ischemic bowel, severe acute hepatic disease, severe acute hepatic encephalopathy or acute renal failure.
3-(5-CHLORO-2-OXOBENZO[D]OXAZOL-3(2H)-YL) PROPANOIC ACID DERIVATIVES AS KMO INHIBITORS
A compound of formula (I) or a salt thereof are provided:
##STR00001##
wherein R.sup.1, X and R.sup.3 are defined in the specification, useful in the treatment of disorders mediated by KMO such as acute pancreatitis, chronic kidney disease, other conditions associated with systemic inflammatory response syndrome (SIRS), Huntington's disease, Alzheimer's disease, spinocerebellar ataxias, Parkinson's disease, AIDS-dementia complex, amylotrophic lateral sclerosis (ALS), depression, schizophrenia, sepsis, cardiovascular shock, severe trauma, acute lung injury, acute respiratory distress syndrome, acute cholecystitis, severe burns, pneumonia, extensive surgical procedures, ischemic bowel, severe acute hepatic disease, severe acute hepatic encephalopathy or acute renal failure.
Process for the preparation of enantiomerically pure norepinephrine
The invention concerns a new, efficient process for the preparation of enantiomerically pure norepinephrine (also known as noradrenaline), or an addition salt thereof, using a catalytic hydrogenation system under hydrogen donor transfer. The invention also discloses a novel intermediate and the process for the preparation thereof.
Process for the preparation of enantiomerically pure norepinephrine
The invention concerns a new, efficient process for the preparation of enantiomerically pure norepinephrine (also known as noradrenaline), or an addition salt thereof, using a catalytic hydrogenation system under hydrogen donor transfer. The invention also discloses a novel intermediate and the process for the preparation thereof.
A PROCESS FOR THE PREPARATION OF ENANTIOMERICALLY PURE NOREPINEPHRINE
The invention concerns a new, efficient process for the preparation of enantiomerically pure norepinephrine (also known as noradrenaline), or an addition salt thereof, using a catalytic hydrogenation system under hydrogen donor transfer. The invention also discloses a novel intermediate and the process for the preparation thereof.
A PROCESS FOR THE PREPARATION OF ENANTIOMERICALLY PURE NOREPINEPHRINE
The invention concerns a new, efficient process for the preparation of enantiomerically pure norepinephrine (also known as noradrenaline), or an addition salt thereof, using a catalytic hydrogenation system under hydrogen donor transfer. The invention also discloses a novel intermediate and the process for the preparation thereof.
COMPOUND HAVING PD-L1 INHIBITORY ACTIVITY, PREPARATION METHOD THEREFOR AND USE THEREOF
Provided are a compound for the prevention and treatment of diseases associated with PD-L1, a preparation method therefor and use thereof. Specifically, provided are the compound of formula I, the stereoisomer and the racemate thereof, or pharmaceutically acceptable salts thereof, and also provided is an application thereof in the preparation of a drug for the prevention and treatment of diseases associated with PD-Ll.
##STR00001##
COMPOUND HAVING PD-L1 INHIBITORY ACTIVITY, PREPARATION METHOD THEREFOR AND USE THEREOF
Provided are a compound for the prevention and treatment of diseases associated with PD-L1, a preparation method therefor and use thereof. Specifically, provided are the compound of formula I, the stereoisomer and the racemate thereof, or pharmaceutically acceptable salts thereof, and also provided is an application thereof in the preparation of a drug for the prevention and treatment of diseases associated with PD-Ll.
##STR00001##
METHODS OF MANUFACTURING BENZOQUINOLINE COMPOUNDS
The present invention relates to new methods of manufacturing benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), and intermediates thereof.
##STR00001##