C07C317/18

PROCESS FOR THE PREPARATION OF VITAMIN K2
20170283354 · 2017-10-05 ·

Using a combination of Kumada, Suzuki and Biellmann chemistry, various menaquinones can synthesised rapidly and with stereochemical integrity offering a new way of preparing these vitamin K2 components for the pharmaceutical market. In one embodiment a process for the preparation of a compound of formula (I)

##STR00001## is defined including a step in which (i) a compound of formula (II) is reacted with a compound of formula (III)

##STR00002## wherein R is an alkyl group; LG is a leaving group; m is an integer from 0 to 8; n is an integer of from 0 to 9; and X is hydrogen, halide, hydroxyl or protected hydroxyl; in the presence of a copper, nickel or palladium catalyst.

PROCESS FOR THE PREPARATION OF VITAMIN K2
20170283354 · 2017-10-05 ·

Using a combination of Kumada, Suzuki and Biellmann chemistry, various menaquinones can synthesised rapidly and with stereochemical integrity offering a new way of preparing these vitamin K2 components for the pharmaceutical market. In one embodiment a process for the preparation of a compound of formula (I)

##STR00001## is defined including a step in which (i) a compound of formula (II) is reacted with a compound of formula (III)

##STR00002## wherein R is an alkyl group; LG is a leaving group; m is an integer from 0 to 8; n is an integer of from 0 to 9; and X is hydrogen, halide, hydroxyl or protected hydroxyl; in the presence of a copper, nickel or palladium catalyst.

Polyanionic delivery of nucleic acids

Disclosed are dendritic anionic lipids which are compounds of Formula (I): wherein R and R.sup.1 are non-polar groups, L is a linking moiety, and Dm is a dendritic moiety of m generations, each as defined herein. These dendritic anionic lipids are useful for delivery and expression of m RNA and encoded protein, e.g., as a component of liposomal delivery vehicle, and accordingly can be useful for treating various diseases, disorders and conditions, such as those associated with deficiency of one or more proteins. ##STR00001##

Polyanionic delivery of nucleic acids

Disclosed are dendritic anionic lipids which are compounds of Formula (I): wherein R and R.sup.1 are non-polar groups, L is a linking moiety, and Dm is a dendritic moiety of m generations, each as defined herein. These dendritic anionic lipids are useful for delivery and expression of m RNA and encoded protein, e.g., as a component of liposomal delivery vehicle, and accordingly can be useful for treating various diseases, disorders and conditions, such as those associated with deficiency of one or more proteins. ##STR00001##

AGONISTS OF ROR GAMMAt

The present invention is directed to compounds of the formula (I) wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

##STR00001##

AGONISTS OF ROR GAMMAt

The present invention is directed to compounds of the formula (I) wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

##STR00001##

Fluorinated benzenesulfonamides as inhibitors of carbonic anhydrase

Novel fluorinated benzenesulfonamides compounds of general formula (I) ##STR00001##
can be used in biomedicine as active ingredients in pharmaceutical formulations, because they inhibit enzymes which participate in disease progression.

Fluorinated benzenesulfonamides as inhibitors of carbonic anhydrase

Novel fluorinated benzenesulfonamides compounds of general formula (I) ##STR00001##
can be used in biomedicine as active ingredients in pharmaceutical formulations, because they inhibit enzymes which participate in disease progression.

Hydrogels with biodegradable crosslinking

Hydrogels that degrade under appropriate conditions of pH and temperature by virtue of crosslinking compounds that cleave through an elimination reaction are described. The hydrogels may be used for delivery of various agents, such as pharmaceuticals.

Hydrogels with biodegradable crosslinking

Hydrogels that degrade under appropriate conditions of pH and temperature by virtue of crosslinking compounds that cleave through an elimination reaction are described. The hydrogels may be used for delivery of various agents, such as pharmaceuticals.