Patent classifications
C07D211/18
DOPAMINE D2 RECEPTOR LIGANDS
The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity.
Halogen-containing metathesis catalysts and methods thereof
The present disclosure provides compounds, compositions, and methods for preparing alkenyl halides and/or haloalkyl-substituted olefins with Z-selectivity. The methods are particularly useful for preparing alkenyl fluorides such as CF.sub.3-substituted olefins by means of cross-metathesis reactions using halogen-containing molybdenum and tungsten complexes.
Halogen-containing metathesis catalysts and methods thereof
The present disclosure provides compounds, compositions, and methods for preparing alkenyl halides and/or haloalkyl-substituted olefins with Z-selectivity. The methods are particularly useful for preparing alkenyl fluorides such as CF.sub.3-substituted olefins by means of cross-metathesis reactions using halogen-containing molybdenum and tungsten complexes.
Chemical Compounds as ATF-4 Pathway Inhibitors
The invention is directed to substituted bridged cycloalkane derivatives. Specifically, the invention is directed to compounds according to Formula IIIQ:
##STR00001##
wherein X.sup.6′, a, b, C.sup.8′, D.sup.8′, L.sup.82′, L.sup.83′, R.sup.81′, R.sup.82′, R.sup.83′, R.sup.84′, R.sup.85′, R.sup.86′, z.sup.82′, z.sup.84′, z.sup.85′, and z.sup.86′ are as defined herein; or salts thereof.
The compounds of the invention are inhibitors of the ATF4 pathway. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting the ATF4 pathway and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
Chemical Compounds as ATF-4 Pathway Inhibitors
The invention is directed to substituted bridged cycloalkane derivatives. Specifically, the invention is directed to compounds according to Formula IIIQ:
##STR00001##
wherein X.sup.6′, a, b, C.sup.8′, D.sup.8′, L.sup.82′, L.sup.83′, R.sup.81′, R.sup.82′, R.sup.83′, R.sup.84′, R.sup.85′, R.sup.86′, z.sup.82′, z.sup.84′, z.sup.85′, and z.sup.86′ are as defined herein; or salts thereof.
The compounds of the invention are inhibitors of the ATF4 pathway. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting the ATF4 pathway and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
AGENTS FOR DIFFERENTIATING STEM CELLS AND TREATING CANCER
The present application discloses a method for identifying an agent for the treatment or prevention of cancer or metastatic cancer comprising the steps of contacting stem cell with a potential agent, and identifying an agent that induces differentiation, or inhibits stem cell pluripotency or growth of the stem cell, wherein such agent is determined to be an anti-cancer agent.
HETEROCYCLIC P2Y14 RECEPTOR ANTAGONISTS
Disclosed are compounds of formulas (I)-(IX) for treating or preventing a disease or disorder responsive to antagonism of a P2Y.sub.14R receptor agonist in a mammal in need thereof, wherein R.sup.1-R.sup.8, X, Y, Z, X, Y, Z, and A are as defined herein, that are useful in treating an inflammatory such as asthma, cystic fibrosis, and sterile inflammation of the kidney.
##STR00001##
Processes for the preparation of Niraparib and intermediates thereof
The present invention relates to novel procedures and novel intermediates useful in the synthesis of Niraparib or any salt thereof.
COMPOUNDS FOR BINDING PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9
The present disclosure relates to novel compounds, methods, and compositions capable of binding to PCSK9, thereby modulating PCSK9 proprotein convertase enzyme activity. The compounds of the disclosure include compounds Formula (I).
COMPOUNDS FOR BINDING PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9
The present disclosure relates to novel compounds, methods, and compositions capable of binding to PCSK9, thereby modulating PCSK9 proprotein convertase enzyme activity. The compounds of the disclosure include compounds Formula (I).