C07D291/02

Simplified Structural Mimetics of AIPS as Quorum Sensing Inhibitors
20210024476 · 2021-01-28 ·

Compounds that regulate quorum sensing in Staphylococcal bacteria and in particular in Staphylococcus aureus are provided. Compounds are described in formulas I, II, III, IV, V and VI herein. One or more compounds herein can be employed to inhibit QS and to thus inhibit virulence in Staphylococcus bacteria and in particular in Staphylococcus aureus. Compounds herein and pharmaceutical compositions containing one or more of these compounds are useful, for example, in treating infections of Staphylococcus bacteria and in particular of Staphylococcus aureus. Methods for treating such bacterial infections are provided.

Simplified Structural Mimetics of AIPS as Quorum Sensing Inhibitors
20210024476 · 2021-01-28 ·

Compounds that regulate quorum sensing in Staphylococcal bacteria and in particular in Staphylococcus aureus are provided. Compounds are described in formulas I, II, III, IV, V and VI herein. One or more compounds herein can be employed to inhibit QS and to thus inhibit virulence in Staphylococcus bacteria and in particular in Staphylococcus aureus. Compounds herein and pharmaceutical compositions containing one or more of these compounds are useful, for example, in treating infections of Staphylococcus bacteria and in particular of Staphylococcus aureus. Methods for treating such bacterial infections are provided.

METHODS, COMPOUNDS, COMPOSITIONS AND VEHICLES FOR DELIVERING 3-AMINO-1-PROPANESULFONIC ACID

The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compound that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to the prevention and treatment of Alzheimer's disease

METHODS, COMPOUNDS, COMPOSITIONS AND VEHICLES FOR DELIVERING 3-AMINO-1-PROPANESULFONIC ACID

The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compound that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to the prevention and treatment of Alzheimer's disease

Electronically activated strained alkynes

Compounds of Formula I: ##STR00001## wherein: R.sup.1 and R.sup.1 are independently selected from hydrogen, halogen, C.sub.1-to-C.sub.12 linear or branched hydroxyalkyl, C.sub.1-to-C.sub.12 linear or branched halo-alkyl, carboxy, carboxyalkyl, amido, N-alkylamido, N,N-dialkylamido, carbamoyloxy, N-alkylcarbamoyloxy, and N,N-dialkylcarbamoyloxy, provided that that R.sup.1 and R.sup.1 are not simultaneously hydrogen; R.sup.2 and R.sup.2 hydrogen, halogen, C.sub.1-to-C.sub.12 linear or branched hydroxyalkyl, C.sub.1-to-C.sub.12 linear or branched halo-alkyl, carboxy, carboxyalkyl, amido, N-alkylamido, N,N-dialkylamido, carbamoyloxy, N-alkylcarbamoyloxy, and N,N-dialkylcarbamoyloxy, provided that that R.sup.2 and R.sup.2 are not simultaneously hydrogen; R.sup.3 is selected from hydrogen, C.sub.1 to C.sub.12 linear or branched alkyl, and nitrogen protecting groups; X is oxygen or nitrogen; when X is oxygen, R.sup.4 is absent; and when X is nitrogen, R.sup.4 is selected from H, C.sub.1-to-C.sub.12 linear or branched alkyl, and nitrogen protecting groups.

Electronically activated strained alkynes

Compounds of Formula I: ##STR00001## wherein: R.sup.1 and R.sup.1 are independently selected from hydrogen, halogen, C.sub.1-to-C.sub.12 linear or branched hydroxyalkyl, C.sub.1-to-C.sub.12 linear or branched halo-alkyl, carboxy, carboxyalkyl, amido, N-alkylamido, N,N-dialkylamido, carbamoyloxy, N-alkylcarbamoyloxy, and N,N-dialkylcarbamoyloxy, provided that that R.sup.1 and R.sup.1 are not simultaneously hydrogen; R.sup.2 and R.sup.2 hydrogen, halogen, C.sub.1-to-C.sub.12 linear or branched hydroxyalkyl, C.sub.1-to-C.sub.12 linear or branched halo-alkyl, carboxy, carboxyalkyl, amido, N-alkylamido, N,N-dialkylamido, carbamoyloxy, N-alkylcarbamoyloxy, and N,N-dialkylcarbamoyloxy, provided that that R.sup.2 and R.sup.2 are not simultaneously hydrogen; R.sup.3 is selected from hydrogen, C.sub.1 to C.sub.12 linear or branched alkyl, and nitrogen protecting groups; X is oxygen or nitrogen; when X is oxygen, R.sup.4 is absent; and when X is nitrogen, R.sup.4 is selected from H, C.sub.1-to-C.sub.12 linear or branched alkyl, and nitrogen protecting groups.

RADIATION-SENSITIVE RESIN COMPOSITION, RESIST PATTERN-FORMING METHOD, AND COMPOUND

A radiation-sensitive resin composition includes a first polymer including a first structural unit that includes a first acid-labile group; a radiation-sensitive acid generator; and a compound represented by formula (1). n is 1 or 2. R.sup.1 represents a hydrogen atom or a monovalent organic group having 1 to 20 carbon atoms in a case in which n is 1. R.sup.1 represents a divalent organic group having 1 to 20 carbon atoms in a case in which n is 2. R.sup.2 represents a hydrogen atom or a monovalent organic group having 1 to 20 carbon atoms. E represents a group represented by formula (i). R.sup.2 and E may taken together represent a ring structure having 3 to 20 ring atoms together with the nitrogen atom. X represents a divalent organic group having 1 to 20 carbon atoms. R.sup.3 represents a second acid-labile group.

##STR00001##

METHODS, COMPOUNDS, COMPOSITIONS AND VEHICLES FOR DELIVERING 3-AMINO-1-PROPANESULFONIC ACID

The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compound that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to the prevention and treatment of Alzheimer's disease

METHODS, COMPOUNDS, COMPOSITIONS AND VEHICLES FOR DELIVERING 3-AMINO-1-PROPANESULFONIC ACID

The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compound that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to the prevention and treatment of Alzheimer's disease

METHODS, COMPOUNDS, COMPOSITIONS AND VEHICLES FOR DELIVERING 3-AMINO-1-PROPANESULFONIC ACID

The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compounds that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to, the prevention and treatment of Alzheimer's disease.