C07C233/29

ANESTHETIC COMPOUNDS AND METHODS OF MAKING AND USING SAME TO TREAT OR PREVENT PAIN SYMPTOMS

The present disclosure provides compositions comprising one or more compounds of general formula (I):

##STR00001##

wherein: R.sub.1 is H, —OMe, Me, or one or more electron withdrawing groups; R.sub.2 and R.sub.3 are each independently H or alkyl or, taken together, form a 4- to 8-membered heterocyclic ring with the adjacent nitrogen atom; R.sub.4 is H or alkyl; R.sub.5 is H or one or more electron donating groups; and n is 1 to 4.

ANESTHETIC COMPOUNDS AND METHODS OF MAKING AND USING SAME TO TREAT OR PREVENT PAIN SYMPTOMS

The present disclosure provides compounds useful as anesthetics, such as topical anesthetics, of general formula (XIII):

##STR00001##

wherein: R.sub.8=NH.sub.2, NH(Me), N(Me).sub.2,

##STR00002##

The present disclosure further provides methods of making compounds of general formula (XIII), compositions comprising a therapeutically effective amount of a compound of general formula (XIII), and methods of treating or preventing pain in a subject by administering (e.g., topically applying) compositions comprising an effective amount of a compound of general formula (XIII) to the subject.

ANESTHETIC COMPOUNDS AND METHODS OF MAKING AND USING SAME TO TREAT OR PREVENT PAIN SYMPTOMS

The present disclosure provides compounds useful as anesthetics, such as topical anesthetics, of general formula (XIII):

##STR00001##

wherein: R.sub.8=NH.sub.2, NH(Me), N(Me).sub.2,

##STR00002##

The present disclosure further provides methods of making compounds of general formula (XIII), compositions comprising a therapeutically effective amount of a compound of general formula (XIII), and methods of treating or preventing pain in a subject by administering (e.g., topically applying) compositions comprising an effective amount of a compound of general formula (XIII) to the subject.

Anesthetic compounds and methods of making and using same to treat or prevent pain symptoms

The present disclosure provides compounds useful as anesthetics, such as topical anesthetics, of general formula (VIIIg): ##STR00001##
wherein: R.sub.2=H or Me; R.sub.3=H or Me; R.sub.4=Alkyl; R.sub.5=O-Alkyl; and Alkyl=aliphatic C.sub.1-C.sub.4 alkyl. The present disclosure further provides methods of making compounds of general formula (VIIIg), compositions comprising a therapeutically effective amount of a compound of general formula (VIIIg), and methods of treating or preventing pain in a subject by administering (e.g., topically applying) compositions comprising an effective amount of a compound of general formula (VIIIg) to the subject.

Anesthetic compounds and methods of making and using same to treat or prevent pain symptoms

The present disclosure provides compounds useful as anesthetics, such as topical anesthetics, of general formula (VIIIg): ##STR00001##
wherein: R.sub.2=H or Me; R.sub.3=H or Me; R.sub.4=Alkyl; R.sub.5=O-Alkyl; and Alkyl=aliphatic C.sub.1-C.sub.4 alkyl. The present disclosure further provides methods of making compounds of general formula (VIIIg), compositions comprising a therapeutically effective amount of a compound of general formula (VIIIg), and methods of treating or preventing pain in a subject by administering (e.g., topically applying) compositions comprising an effective amount of a compound of general formula (VIIIg) to the subject.

Catalyst, method for forming amide bond, and method for producing amide compound

A catalyst represented by General Formula (1) below: ##STR00001## where in the General Formula (1), R.sup.1 to R.sup.14 each independently represent a hydrogen atom or a substituent.

Catalyst, method for forming amide bond, and method for producing amide compound

A catalyst represented by General Formula (1) below: ##STR00001## where in the General Formula (1), R.sup.1 to R.sup.14 each independently represent a hydrogen atom or a substituent.

INHIBITORS OF HISTONE LYSINE SPECIFIC DEMETHYLASE (LSD1) AND HISTONE DEACETYLASES (HDACS)
20210009511 · 2021-01-14 ·

A series of phenelzine analogs comprising a phenelzine scaffold linked to an aromatic moiety and their use as inhibitors of lysine-specific demethylase 1 (LSD1) and/or one or more histone deacetylases (HDACs) is provided. The presently disclosed phenelzine analogs exhibit potency and selectivity for LSD1 versus MAO and LSD2 enzymes and exhibit bulk, as well as, gene specific histone methylation changes, anti-proliferative activity in several cancer cell lines, and neuroprotection in response to oxidative stress. Accordingly, the presently disclosed phenelzine analogs can be used to treat diseases, conditions, or disorders related to LSD1 and/or HDACs, including, but not limited to, cancers and neurodegenerative diseases.

INHIBITORS OF HISTONE LYSINE SPECIFIC DEMETHYLASE (LSD1) AND HISTONE DEACETYLASES (HDACS)
20210009511 · 2021-01-14 ·

A series of phenelzine analogs comprising a phenelzine scaffold linked to an aromatic moiety and their use as inhibitors of lysine-specific demethylase 1 (LSD1) and/or one or more histone deacetylases (HDACs) is provided. The presently disclosed phenelzine analogs exhibit potency and selectivity for LSD1 versus MAO and LSD2 enzymes and exhibit bulk, as well as, gene specific histone methylation changes, anti-proliferative activity in several cancer cell lines, and neuroprotection in response to oxidative stress. Accordingly, the presently disclosed phenelzine analogs can be used to treat diseases, conditions, or disorders related to LSD1 and/or HDACs, including, but not limited to, cancers and neurodegenerative diseases.

Chemosensitization of resistant <i>Pseudomonas aeruginosa </i>by synthetically related compounds

Compounds for the chemosensitization of antibiotic resistant bacteria such as multidrug resistant (MDR) Pseudomonas aeruginosa (Pa) are provided. The compounds inhibit the MDR efflux proteins and re-sensitize the bacteria towards killing by antibiotics. Thus, the compounds are used in combination with antibiotics to treat or prevent infections caused by MDR bacteria.