Processes for stereoselective preparation of a chiral alcohol or a chiral amine are described. The processes include reacting a first prochiral reactant selected from the group consisting of a ketone, an aldehyde, and an imine, with a second reactant that includes a Grignard reagent, in the presence of a chiral trans-diamine of formula (1) as defined herein: ##STR00001##

The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.

Disclosed are 4-hydroxylphenyl substituted carbocycles and there use as selective agonists of the estrogen receptor beta isoform (ER). The disclosed compounds may be formulated as pharmaceutical compositions and administered to treat diseases associated with ER activity, such as proliferative diseases and disorders and/or psychiatric diseases or disorders.

The present disclosure relates to methods and intermediates useful for preparing a compound of formula I: ##STR00001## or a co-crystal, solvate, salt or combination thereof.

Disclosed is a cyclopropanation process comprising the step of reacting an alkene compound having at least one carbon-carbon double bond with at least one dihaloalkane. The reaction is carried out in the presence of (i) particulate metal Zn, (ii) catalytically effective amount of particulate metal Cu or a salt thereof, (iii) at least one haloalkylsilane, and (iv) at least one solvent.

Described herein are modified monoterpene TRPM8 activating compounds. In particular, provided herein are compounds that affect the function of ion channels in a cell, and are useful as therapeutic agents or with therapeutic agents. The compounds provided herein are useful in the treatment of a variety of diseases and conditions including inflammatory eye diseases such as uveitis, cardiovascular diseases, inflammatory diseases, and diseases characterized by abnormal growth, such as cancers.

The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, Formula (I), wherein, the group XY is NHSO.sub.2; Z is a monocyclic or polycyclic cycloalkyl group or a monocyclic or polycyclic heterocycloalkyl group, each of which is optionally substituted by one or more groups selected from haloalkyl, alkyl, alkenyl, alkynyl and (CR.sub.16R.sub.17).sub.mR.sub.18, where m is 0 to 6; L is a direct bond or a group (CR.sub.14R.sub.15).sub.n, where n is 1 or 2; R.sub.1 is H, CN, Cl or F or alkyl; R.sub.2 is selected from COOH and a tetrazolyl group; R.sub.3 is selected from H, halo, alkoxy and alkyl; R.sub.4 is selected from H and halo; R.sub.5 is selected from H, alkyl, haloalkyl, SO.sub.2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R.sub.6 is H; R.sub.7 is selected from H, CN, haloalkyl, halo, SO.sub.2-alkyl, SO.sub.2NR.sub.12R.sub.13, heteroaryl, CONR.sub.10R.sub.11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.9 is selected from H, alkyl and halo; Rio, R.sub.1, R.sub.12 and R.sub.13 are each independently H or alkyl; R.sub.14 and R.sub.15 are each independently H, halo or alkyl; R.sub.16 and R.sub.17 are each independently H, halo, haloalkyl or alkyl; and each R.sub.18 is independently selected from OH, CN, alkoxy and halo. Further aspects of the invention relate to such compounds for use in the field of immune-oncology and related applications.

##STR00001##

The present invention belongs to the field of pharmaceutical technology, more specifically relates to optically pure benzyl-4-chlorophenyl-C-glucoside derivatives represented by formulae (II) and (III), a process for preparing these compounds and intermediates thereof, a pharmaceutical formulation and a pharmaceutical composition containing these compounds, and the use of the optically pure benzyl-4-chlorophenyl-C-glucoside derivative as a sodium glucose co-transporter (SGLT) inhibitor in manufacture of a medicament for treating and/or preventing diabetes mellitus (including insulin-dependent diabetes mellitus and non-insulin-dependent diabetes mellitus) or diabetes-associated diseases (including insulin resistance disease and obesity) ##STR00001##

Compounds are provided having the following Structure (I):

##STR00001##

or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein R.sup.1, R.sup.1, L.sup.1, L.sup.2, L.sup.2a, L.sup.2b, and A are as defined herein. Use of the compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, compositions comprising the compounds and methods for their use and preparation are also provided.

The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.