C07C307/06

Bicyclic compounds

Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.

DOUBLE-HEADED PROTEASE INHIBITOR

The present invention provides a compound that is highly safe and useful in the prevention, alleviation, and/or treatment of various diseases involving enteropeptidase inhibition and/or trypsin inhibition, a pharmaceutical composition containing the compound, a method for producing the compound, and the like. Specifically, the present invention provides a compound represented by the following general formula (I):

##STR00001##

[wherein: A.sup.1 and A.sup.2 each independently represent an inhibitor residue having at least one activity selected from an enteropeptidase inhibitory activity and a trypsin inhibitory activity; and Z represents a spacer that links A.sup.1 to A.sup.2] or a pharmaceutically acceptable salt thereof.

DOUBLE-HEADED PROTEASE INHIBITOR

The present invention provides a compound that is highly safe and useful in the prevention, alleviation, and/or treatment of various diseases involving enteropeptidase inhibition and/or trypsin inhibition, a pharmaceutical composition containing the compound, a method for producing the compound, and the like. Specifically, the present invention provides a compound represented by the following general formula (I):

##STR00001##

[wherein: A.sup.1 and A.sup.2 each independently represent an inhibitor residue having at least one activity selected from an enteropeptidase inhibitory activity and a trypsin inhibitory activity; and Z represents a spacer that links A.sup.1 to A.sup.2] or a pharmaceutically acceptable salt thereof.

COMPOUNDS WITH ANTIMICROBIAL ACTIVITY
20200347010 · 2020-11-05 ·

This invention relates to compounds of formula 1, 2 or 3

##STR00001##

a pharmaceutically acceptable salt, or solvate thereof, wherein X.sub.1, Y, R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are as defined herein. The compounds are antimicrobial agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1, 2 or 3.

SULFONYLUREAS AND RELATED COMPOUNDS AND USE OF SAME

The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts, solvates and prodrugs thereof:

##STR00001##

wherein Q is selected from O, S and Se; J is S or Se; W.sup.1 and W.sup.2, when present, are independently selected from N and C; R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen, C.sub.1-C.sub.12 alkyl, C.sub.2-C.sub.12 alkenyl, C.sub.2-C.sub.12 alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, cycloalkenyl, amino, amido, alkylthio, acyl, arylalkyl and acylamido, all of which may be optionally substituted; and wherein at least one of W.sup.1 and W.sup.2 is present and is a nitrogen atom and when R.sup.1 or R.sup.2 are cyclic then the respective W.sup.1 or W.sup.2 may form part of the ring structure. The present invention also relates to pharmaceutical compositions including such compounds, to methods of treatment using such compounds, in particular in relation to NLRP3 inflammasome mediated disorders, and to associated diagnostic uses.

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured:

##STR00001## or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.

ISOCYANATE ELECTROLYTE SOLUTION ADDITIVE CONTAINING SULFAMIDE STRUCTURAL GROUP AND APPLICATION THEREOF

An isocyanate electrolyte solution additive containing a sulfamide structural group has a structure of formula I:

##STR00001##

where R.sub.1 and R.sub.2 are identical or different, R.sub.1 and R.sub.2 are each independently selected from methyl, ethyl, butyl, methoxy, methanesulfonyl, ethanesulfonyl, fluorosulfonyl, trifluoromethanesulfonyl, perfluoroethylsulfonyl, benzenesulfonyl, alkyl-containing benzenesulfonyl, cyano/fluorobenzenesulfonyl and alkoxy-containing benzenesulfonyl, and R.sub.1 and R.sub.2 can be linked to form one of five-membered ring or six-membered ring. In the electrolyte solution additive, sulfonyl and the isocyanate structural group are organically linked, so the electrolyte solution additive has good thermostability, can function as an electrolyte solution stabilizing agent and avoids high temperature discoloration and acid value increase of the electrolyte solution. The electrolyte solution containing the novel additive provided by the present disclosure patent is applied to a battery, which improves high-temperature cycle and high-temperature storage performances and exhibits low impedance.

ISOCYANATE ELECTROLYTE SOLUTION ADDITIVE CONTAINING SULFAMIDE STRUCTURAL GROUP AND APPLICATION THEREOF

An isocyanate electrolyte solution additive containing a sulfamide structural group has a structure of formula I:

##STR00001##

where R.sub.1 and R.sub.2 are identical or different, R.sub.1 and R.sub.2 are each independently selected from methyl, ethyl, butyl, methoxy, methanesulfonyl, ethanesulfonyl, fluorosulfonyl, trifluoromethanesulfonyl, perfluoroethylsulfonyl, benzenesulfonyl, alkyl-containing benzenesulfonyl, cyano/fluorobenzenesulfonyl and alkoxy-containing benzenesulfonyl, and R.sub.1 and R.sub.2 can be linked to form one of five-membered ring or six-membered ring. In the electrolyte solution additive, sulfonyl and the isocyanate structural group are organically linked, so the electrolyte solution additive has good thermostability, can function as an electrolyte solution stabilizing agent and avoids high temperature discoloration and acid value increase of the electrolyte solution. The electrolyte solution containing the novel additive provided by the present disclosure patent is applied to a battery, which improves high-temperature cycle and high-temperature storage performances and exhibits low impedance.

COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS

The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.

Method for making N-(fluorosulfonyl) dimethylamine
10407387 · 2019-09-10 · ·

Dimethylamine (Me.sub.2NH) is reacted with sulfuryl fluoride (SO.sub.2F.sub.2) to form at least a first phase comprising N-(fluorosulfonyl) dimethylamine (FSO.sub.2NMe.sub.2), tetramethylsulfamide (SO.sub.2(NMe.sub.2).sub.2), or a combination thereof. A second phase, which may include dimethylamine hydrofluoride (Me.sub.2NH.sub.2F), may be also formed and separated from the first phase. FSO.sub.2NMe.sub.2 or SO.sub.2(NMe.sub.2).sub.2 is then isolated from the first phase. For example, the first phase may be a liquid phase, and FSO.sub.2NMe.sub.2 and SO.sub.2(NMe.sub.2).sub.2 are separated by distillation, optionally under reduced pressure.