C07C311/05

COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS
20190016669 · 2019-01-17 ·

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.

PREPARATION OF SULFONAMIDE-CONTAINING ANTIMICROBIALS AND SUBSTRATE TREATING COMPOSITIONS OF SULFONAMIDE-CONTAINING ANTIMICROBIALS

A quaternary ammonium sulfonamide compound of formula (I): wherein R=(II), C.sub.1-C.sub.3 linear or branched alkyl, R.sub.1 and R.sub.2 are the same or different and selected from C.sub.1 to C.sub.18 linear or branched alkyl, R.sub.3 and R.sub.4 are the same or different and selected from C.sub.1 to C.sub.4 linear or branched alkyl, CF.sub.3, OR.sub.5 where R.sub.5 is C.sub.1 to C.sub.8 linear or branched alkyl or polyethylene oxide, l is 1, 2, 3, 4, 5, 6, 7 or 8, m is 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16 or 17, n is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17 or 18, wherein the aryl groups of R may be substituted or unsubstituted, X=halogen, and Y=(III) wherein R.sub.6, R.sub.7, R.sub.8, R.sub.9 and R.sub.10 are the same or different and selected from C.sub.1 to C.sub.6 linear or branched alkyl and the benzophenone is selected from the group consisting of substituted benzophenone and unsubstituted benzophenone, process for preparing the compound and antimicrobial surface coating compositions of the compound.

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PREPARATION OF SULFONAMIDE-CONTAINING ANTIMICROBIALS AND SUBSTRATE TREATING COMPOSITIONS OF SULFONAMIDE-CONTAINING ANTIMICROBIALS

A quaternary ammonium sulfonamide compound of formula (I): wherein R=(II), C.sub.1-C.sub.3 linear or branched alkyl, R.sub.1 and R.sub.2 are the same or different and selected from C.sub.1 to C.sub.18 linear or branched alkyl, R.sub.3 and R.sub.4 are the same or different and selected from C.sub.1 to C.sub.4 linear or branched alkyl, CF.sub.3, OR.sub.5 where R.sub.5 is C.sub.1 to C.sub.8 linear or branched alkyl or polyethylene oxide, l is 1, 2, 3, 4, 5, 6, 7 or 8, m is 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16 or 17, n is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17 or 18, wherein the aryl groups of R may be substituted or unsubstituted, X=halogen, and Y=(III) wherein R.sub.6, R.sub.7, R.sub.8, R.sub.9 and R.sub.10 are the same or different and selected from C.sub.1 to C.sub.6 linear or branched alkyl and the benzophenone is selected from the group consisting of substituted benzophenone and unsubstituted benzophenone, process for preparing the compound and antimicrobial surface coating compositions of the compound.

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POLYAMINE SULFONAMIDES AND USES THEREOF

Cancer is a disease for which there remains a great unmet medical need, and therefore the discovery and development of new antineoplastic agents is critically important. The present invention relates in part to new therapeutic compounds with antineoplastic activity. Provided herein are polyamine sulfonamides such as compounds of Formula (I), or pharmaceutically acceptable salts thereof, which may be used in the treatment and/or prevention of diseases such as cancer. Also provided herein are pharmaceutical compositions and kits comprising the inventive compounds. Furthermore, the present invention provides methods of treating and/or preventing diseases (e.g., cancer) using compounds of Formula (I), or pharmaceutically acceptable salts thereof or pharmaceutical compositions thereof. Other methods provided include methods for inducing apoptosis of a cell, as well as methods for inhibiting alpha-enolase enzymatic activity in vivo and in vitro.

POLYAMINE SULFONAMIDES AND USES THEREOF

Cancer is a disease for which there remains a great unmet medical need, and therefore the discovery and development of new antineoplastic agents is critically important. The present invention relates in part to new therapeutic compounds with antineoplastic activity. Provided herein are polyamine sulfonamides such as compounds of Formula (I), or pharmaceutically acceptable salts thereof, which may be used in the treatment and/or prevention of diseases such as cancer. Also provided herein are pharmaceutical compositions and kits comprising the inventive compounds. Furthermore, the present invention provides methods of treating and/or preventing diseases (e.g., cancer) using compounds of Formula (I), or pharmaceutically acceptable salts thereof or pharmaceutical compositions thereof. Other methods provided include methods for inducing apoptosis of a cell, as well as methods for inhibiting alpha-enolase enzymatic activity in vivo and in vitro.

Process For Hydrogenating Ketones In The Presence Of RU(II) Catalysts

The present invention relates to a process for hydrogenating a substrate including a carbon-heteroatom double bond, the process including the step of reacting the substrate with hydrogen gas in the presence of a hydrogenation catalyst, wherein the hydrogenation catalyst is a complex of formula (I):

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R.sub.1-10, A and Hal are as defined in the specification. The present invention also provides processes for the preparation of the complex of formula (I) and intermediates thereof.

Process For Hydrogenating Ketones In The Presence Of RU(II) Catalysts

The present invention relates to a process for hydrogenating a substrate including a carbon-heteroatom double bond, the process including the step of reacting the substrate with hydrogen gas in the presence of a hydrogenation catalyst, wherein the hydrogenation catalyst is a complex of formula (I):

##STR00001##

R.sub.1-10, A and Hal are as defined in the specification. The present invention also provides processes for the preparation of the complex of formula (I) and intermediates thereof.

COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS
20180273467 · 2018-09-27 ·

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.

COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS
20180273467 · 2018-09-27 ·

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.

USE OF DUAL-CATION FLUOROCARBON SURFACTANT AS AMPHIPHOBIC WETTABILITY REVERSAL AGENT IN DRILLING FLUID

The present invention relates to the well drilling field in petrochemical industry, in particular to use of dual-cation fluorocarbon surfactant as amphiphobic wettability reversal agent in drilling fluid. The dual-cation fluorocarbon surfactant is a dual-cation fluorocarbon surfactant of which the cation part is represented by the following formula (1). The dual-cation fluorocarbon surfactant of the present invention can serve as wettability reversal agent when it is used for oil-gas drilling to enable rock amphiphobic, and is an amphiphobic wettability reversal agent which can cause rock surface to be non-hydrophilic and non-lipophilic. Using of dual-cation fluorocarbon surfactant, especially when drilling highly hydrous mud shale, can avoid permeation of water and oil into the rock effectively and thereby a capillary phenomenon can be prevented, and an effect of stabilizing the well wall and protecting the reservoir is attained.

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