C07C237/20

Compound and Use Thereof

Provided is a compound that achieves a good balance between the LO. scavenging ability and the LOO. scavenging ability. The compound of the present invention or a salt thereof is represented by the following formula (1). In the formula (1), R.sup.1 and R.sup.2 may be the same or different and are each independently a hydrogen atom or an alkyl group, R.sup.3 is —OR.sup.4 or —NHR.sup.5, R.sup.4 is a sec-butyl group, a tert-butyl group, or an iso-butyl group, and R.sup.5 is a sec-butyl group, a tert-butyl group, or an iso-butyl group.

Compound and Use Thereof

Provided is a compound that achieves a good balance between the LO. scavenging ability and the LOO. scavenging ability. The compound of the present invention or a salt thereof is represented by the following formula (1). In the formula (1), R.sup.1 and R.sup.2 may be the same or different and are each independently a hydrogen atom or an alkyl group, R.sup.3 is —OR.sup.4 or —NHR.sup.5, R.sup.4 is a sec-butyl group, a tert-butyl group, or an iso-butyl group, and R.sup.5 is a sec-butyl group, a tert-butyl group, or an iso-butyl group.

Dual mechanism inhibitors for the treatment of disease

Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.

Dual mechanism inhibitors for the treatment of disease

Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.

METHOD FOR RACEMIC PREPARATION OF CHIRAL B-AMINO ACIDS AND DERIVATIVES THEREOF
20230142248 · 2023-05-11 ·

The present disclosure relates to the field of medicine synthesis, and relates to a method for a racemic preparation of chiral h β-amino acids and derivatives thereof, and in particular to a method for racemizing sitagliptin intermediates.

##STR00001##

where R.sub.1 is hydrogen, alkyl or aryl; R.sub.2 is hydrogen, alkyl or aryl; R.sub.3 is hydrogen, alkyl, aryl or acyl; R.sub.4 is alkyl, aryl, OR′, SR′, NHR′ or NR′R″, wherein R′, R″ are hydrogen, alkyl or aryl.

METHOD FOR RACEMIC PREPARATION OF CHIRAL B-AMINO ACIDS AND DERIVATIVES THEREOF
20230142248 · 2023-05-11 ·

The present disclosure relates to the field of medicine synthesis, and relates to a method for a racemic preparation of chiral h β-amino acids and derivatives thereof, and in particular to a method for racemizing sitagliptin intermediates.

##STR00001##

where R.sub.1 is hydrogen, alkyl or aryl; R.sub.2 is hydrogen, alkyl or aryl; R.sub.3 is hydrogen, alkyl, aryl or acyl; R.sub.4 is alkyl, aryl, OR′, SR′, NHR′ or NR′R″, wherein R′, R″ are hydrogen, alkyl or aryl.

CRYSTALLINE DIPEPTIDES USEFUL IN THE SYNTHESIS OF ELAMIPRETIDE
20230203093 · 2023-06-29 ·

Disclosed are crystalline forms of L-Lys(Boc)-Phe-NH.sub.2 and Boc-D-Arg-DMT. The crystalline forms may be used in the synthesis of elamipretide.

CRYSTALLINE DIPEPTIDES USEFUL IN THE SYNTHESIS OF ELAMIPRETIDE
20230203093 · 2023-06-29 ·

Disclosed are crystalline forms of L-Lys(Boc)-Phe-NH.sub.2 and Boc-D-Arg-DMT. The crystalline forms may be used in the synthesis of elamipretide.

N-(2-Aminophenyl)-Prop-2-Enamide Derivatives, and Uses Thereof in the Treatment of Cancer

Provided herein are N-(2-aminophenyl)-prop-2-enamide derivatives, such as those of Formula (I), methods for the synthesis thereof, and uses thereof in the treatment of cancer, such as SALL4-expressing cancer, in a cell or subject in need thereof.

High penetration drugs and their compositions thereof for treatment of Parkinson diseases
11685739 · 2023-06-27 · ·

One aspect of the invention provides a composition of novel high penetration compositions (HPC) or a high penetration prodrug (HPP) for treatment of Parkinson's disease. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.