Patent classifications
C07D249/18
COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS
Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein, R.sup.1, R.sup.2a, R.sup.2b, R.sup.3 and A are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.
##STR00001##
COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS
Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein, R.sup.1, R.sup.2a, R.sup.2b, R.sup.3 and A are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.
##STR00001##
COMPOUND CONTAINING BENZENE RING AND APPLICATION THEREOF
A compound containing a benzene ring as shown in formula I, a pharmaceutically acceptable salt thereof, a stereoisomer thereof, a tautomer thereof, an isotopic compound thereof, a crystal form thereof, a nitrogen oxide thereof, and a solvate thereof or a solvate of the pharmaceutically acceptable salt thereof are provided. The compound has high P2X4 antagonistic activity, good selectivity, low toxicity and good metabolic stability.
##STR00001##
Synthesis of Vinyl Cyclobutyl Intermediates
Provided herein are processes for synthesizing intermediates useful in preparing Mcl-1 inhibitors. In particular, provided herein are processes for synthesizing compound F, or a salt thereof, wherein R.sup.1 and OPG.sup.2 are described herein. Compound F can be useful in synthesizing compound A1, or a salt of solvate thereof, and compound A2, or a salt of solvate thereof.
##STR00001##
Synthesis of Vinyl Cyclobutyl Intermediates
Provided herein are processes for synthesizing intermediates useful in preparing Mcl-1 inhibitors. In particular, provided herein are processes for synthesizing compound F, or a salt thereof, wherein R.sup.1 and OPG.sup.2 are described herein. Compound F can be useful in synthesizing compound A1, or a salt of solvate thereof, and compound A2, or a salt of solvate thereof.
##STR00001##
Neprilysin inhibitors
In one aspect, the invention relates to compounds having the formula: ##STR00001##
where R.sup.1-R.sup.6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
Neprilysin inhibitors
In one aspect, the invention relates to compounds having the formula: ##STR00001##
where R.sup.1-R.sup.6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
BROAD-SPECTRUM NON-COVALENT CORONAVIRUS PROTEASE INHIBITORS
This invention pertains to materials and methods for the treatment of patients with coronavirus infection and the control of zoonotic disease outbreaks using broad-spectrum non-covalent coronavirus protease inhibitors.
BROAD-SPECTRUM NON-COVALENT CORONAVIRUS PROTEASE INHIBITORS
This invention pertains to materials and methods for the treatment of patients with coronavirus infection and the control of zoonotic disease outbreaks using broad-spectrum non-covalent coronavirus protease inhibitors.
CRYSTALLINE AND SALT FORMS OF AN ORGANIC COMPOUND AND PHARMACEUTICAL COMPOSITIONS THEREOF
##STR00001##
Provided herein are various salts, including tris(hydroxymethyl)aminomethane salts and sodium salts, as well as various crystalline forms of the compound represented by the structural formula: Also provided are pharmaceutical compositions comprising these salts and crystalline forms, methods for their manufacture, and uses thereof for treating conditions, including but not limited to conditions that would benefit from inhibition of dihydroorotate dehydrogenase (DHODH).