C07D263/22

OXAZOLIDINONE COMPOUNDS, LIPOSOME COMPOSITIONS COMPRISING OXAZOLIDINONE COMPOUNDS AND METHOD OF USE THEREOF

Compositions and methods for the treatment of tuberculosis, as well as other mycobacterial and gram positive bacterial infections are disclosed. These compositions contain a highly potent and selective oxazolidinone encapsulated with high efficiency to maximize dosing potential of low toxicity drugs, and are stable in the presence of plasma. The compositions are long circulating and retain their encapsulated drug while in the circulation following intravenous dosing to allow for efficient accumulation at the site of the bacterial or mycobacterial infection. The high doses that can be achieved when combined with the long circulating properties and highly stable retention of the drug allow for a reduced frequency of administration when compared to daily or twice daily administrations of other drugs typically utilized to treat these infections.

Process to prepare ethylene amines and ethylene amine derivatives

A process is provided for preparing ethyleneamines of the formula NH.sub.2—(C.sub.2H.sub.4—NH—).sub.pH wherein p is at least 3, or derivatives thereof wherein one or more units —NH—C.sub.2H.sub.4—NH— may be present as a cyclic ethylene urea unit or piperazine unit or between two units —NH—C.sub.2H.sub.4—NH— a carbonyl moiety is present. The process includes reacting an ethanolamine-functional compound OH—(C.sub.2H.sub.4—NH—).sub.qH wherein q is at least 2, an amine-functional compound NH.sub.2—(C.sub.2H.sub.4—NH—).sub.rH wherein r is at least 1, in the presence of a carbon oxide delivering agent, wherein the molar ratio of ethanolamine-functional compound to amine-functional compound is from about 0.05:1 to about 0.7:1 and the molar ratio of carbon oxide delivering agent to amine-functional compound is higher than the molar ratio of ethanolamine-functional compound to amine-functional compound, provided that the process does not comprise reacting 3 moles of ethylenediamine (EDA) and 1 mole of AEEA (aminoethylethanolamine) in the presence of 1.65 moles of urea at 280 deg C. for 2 hours.

Process to prepare ethylene amines and ethylene amine derivatives

A process is provided for preparing ethyleneamines of the formula NH.sub.2—(C.sub.2H.sub.4—NH—).sub.pH wherein p is at least 3, or derivatives thereof wherein one or more units —NH—C.sub.2H.sub.4—NH— may be present as a cyclic ethylene urea unit or piperazine unit or between two units —NH—C.sub.2H.sub.4—NH— a carbonyl moiety is present. The process includes reacting an ethanolamine-functional compound OH—(C.sub.2H.sub.4—NH—).sub.qH wherein q is at least 2, an amine-functional compound NH.sub.2—(C.sub.2H.sub.4—NH—).sub.rH wherein r is at least 1, in the presence of a carbon oxide delivering agent, wherein the molar ratio of ethanolamine-functional compound to amine-functional compound is from about 0.05:1 to about 0.7:1 and the molar ratio of carbon oxide delivering agent to amine-functional compound is higher than the molar ratio of ethanolamine-functional compound to amine-functional compound, provided that the process does not comprise reacting 3 moles of ethylenediamine (EDA) and 1 mole of AEEA (aminoethylethanolamine) in the presence of 1.65 moles of urea at 280 deg C. for 2 hours.

TRIAZOLE COMPOUNDS AND PREPARATION METHOD THEREFOR AND USE THEREOF

Certain triazole compounds have good LPAR1 antagonistic activity and selectivity, low toxicity, and good metabolic stability, and can be used for preventing or treating the LPAR1-related disease or disorder. The IC.sub.50 value of some triazole compounds can be below 300 nM, even 50 nM. The range of CC.sub.50 of the triazole compounds can be greater than 200 μM. They also show good metabolic stability in human, fancy rats, and house mice.

TRIAZOLE COMPOUNDS AND PREPARATION METHOD THEREFOR AND USE THEREOF

Certain triazole compounds have good LPAR1 antagonistic activity and selectivity, low toxicity, and good metabolic stability, and can be used for preventing or treating the LPAR1-related disease or disorder. The IC.sub.50 value of some triazole compounds can be below 300 nM, even 50 nM. The range of CC.sub.50 of the triazole compounds can be greater than 200 μM. They also show good metabolic stability in human, fancy rats, and house mice.

SIGMA RECEPTOR BINDERS
20210323913 · 2021-10-21 ·

Provided herein, inter alia, are compounds and methods of treating diseases including cancer, neurological disease, alcohol withdrawal, depression and anxiety, traumatic brain injury, and neuropathic pain.

HEPATITIS B ANTIVIRAL AGENTS

The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:


X-A-Y-L-R  (I)

which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Processes for removing carbon disulfide from symmetrical and asymmetrical sulfide product streams

Processes for removing carbon disulfide from product streams containing a sulfide compound are performed by contacting the product stream with an alkanolamine and converting the carbon disulfide to a higher boiling point product, thereby reducing or eliminating carbon disulfide from the product stream. Subsequent removal of the higher boiling point product via distillation can lead to a purified sulfide stream with high purity.

Hepatitis B antiviral agents

The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:
X-A-Y-L-R(I)
which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Method for the preparation of a monothiocarbonate compound

Process for the preparation of a compound with at least one monothiocarbonate group by reacting:a compound with at least one mercaptoalcohol group anda dialkylcarbonate, in the presence of a catalyst wherein the catalyst is a salt of a metal selected from group IIIb or IVb of the periodic system.