C07H9/04

SUBSTITUTED NUCLEOSIDES, NUCLEOTIDES AND ANALAOGS THEREOF
20200277321 · 2020-09-03 ·

Disclosed herein are compounds of the Formula (I) and pharmaceutically acceptable salts thereof: (I) where the variables in Formula (I) are described herein. Methods of synthesizing such compounds and methods of using them to treat diseases and/or conditions such as a Picornaviridae, Flaviviridae, Filoviridae, Pneumoviridae and/or Coronaviridae viral infections are also disclosed.

##STR00001##

Bis-diox(ol)ane compounds

The present invention relates to new bi-functional and polyfunctional bis-dioxolanes and bis-dioxanes. The present inventors have established that the bis-dioxolanes and bis-dioxanes of the invention are highly advantageous as building blocks, cross-linking and/or coupling agents in polymer engineering. They can be derived from biomass sources in a highly efficient manner. The production of the present bis-dioxolanes and bis-dioxanes from biomass has the particular advantage that it facilitates the introduction of desired functionality in a highly flexible manner. Hence, the present invention provides novel bi- or polyfunctional bis-dioxolanes and bis-dioxanes, their production from renewable (biomass) sources, as well as their use in the engineering of polymers.

Bis-diox(ol)ane compounds

The present invention relates to new bi-functional and polyfunctional bis-dioxolanes and bis-dioxanes. The present inventors have established that the bis-dioxolanes and bis-dioxanes of the invention are highly advantageous as building blocks, cross-linking and/or coupling agents in polymer engineering. They can be derived from biomass sources in a highly efficient manner. The production of the present bis-dioxolanes and bis-dioxanes from biomass has the particular advantage that it facilitates the introduction of desired functionality in a highly flexible manner. Hence, the present invention provides novel bi- or polyfunctional bis-dioxolanes and bis-dioxanes, their production from renewable (biomass) sources, as well as their use in the engineering of polymers.

5-azido-5-deoxy-2 :3-isopropylidene-D-arabinose compounds; their method of manufacture and their use for the synthesis of ARA-N3, KDO-N3 and 4EKDO-N3

Disclosed are new compounds of formulae: ##STR00001##
Wherein: R.sup.1 and R.sup.2 can be independently H; a C.sub.1 to C.sub.6 alkyl including methyl, ethyl, propyl, butyl; aryl including phenyl, para-methoxyphenyl; or R.sup.1,R.sup.2 together with the carbon C-6 can be a cyclopentylidene or cyclohexylidene; each of these groups being substituted or not; and R.sup.3 can be a C.sub.1 to C.sub.6 alkyl including methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl; or aryl including phenyl, methylphenyl, ethylphenyl, each of these groups being substituted or not. The invention also relates to their method of manufacture and their use for the synthesis of Ara-N.sub.3, Kdo-N.sub.3 and 4eKdo-N.sub.3.

5-azido-5-deoxy-2 :3-isopropylidene-D-arabinose compounds; their method of manufacture and their use for the synthesis of ARA-N3, KDO-N3 and 4EKDO-N3

Disclosed are new compounds of formulae: ##STR00001##
Wherein: R.sup.1 and R.sup.2 can be independently H; a C.sub.1 to C.sub.6 alkyl including methyl, ethyl, propyl, butyl; aryl including phenyl, para-methoxyphenyl; or R.sup.1,R.sup.2 together with the carbon C-6 can be a cyclopentylidene or cyclohexylidene; each of these groups being substituted or not; and R.sup.3 can be a C.sub.1 to C.sub.6 alkyl including methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl; or aryl including phenyl, methylphenyl, ethylphenyl, each of these groups being substituted or not. The invention also relates to their method of manufacture and their use for the synthesis of Ara-N.sub.3, Kdo-N.sub.3 and 4eKdo-N.sub.3.

Amine solvate of sodium-glucose linked transporter inhibitor, and preparation method and application thereof
10519183 · 2019-12-31 · ·

Disclosed are an amine solvate of a sodium-glucose linked transporter (SGLT) inhibitor, and a preparation method and application thereof. The SGLT inhibitor is (1S,2S,3S,4R,5S)-5-(3-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)methyl)-4-ethylbenzyl)-1-(hydroxymethyl)-6,8-dioxabicyclo[3.2.1]octane-2,3,4-triol. Further provided is a crystalline compound of the amine solvate, a pharmaceutical composition comprising the amine solvate, and an application of the amine solvate in preparing an SGLT-inhibiting pharmaceutical product.

Amine solvate of sodium-glucose linked transporter inhibitor, and preparation method and application thereof
10519183 · 2019-12-31 · ·

Disclosed are an amine solvate of a sodium-glucose linked transporter (SGLT) inhibitor, and a preparation method and application thereof. The SGLT inhibitor is (1S,2S,3S,4R,5S)-5-(3-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)methyl)-4-ethylbenzyl)-1-(hydroxymethyl)-6,8-dioxabicyclo[3.2.1]octane-2,3,4-triol. Further provided is a crystalline compound of the amine solvate, a pharmaceutical composition comprising the amine solvate, and an application of the amine solvate in preparing an SGLT-inhibiting pharmaceutical product.

ASGPR-BINDING COMPOUNDS FOR THE DEGRADATION OF EXTRACELLULAR PROTEINS

Compounds and compositions that have an asialoglycoprotein receptor (ASGPR) binding ligand bound to an extracellular protein binding ligand for the selective degradation of the target extracellular protein in vivo to treat disorders mediated by the extracellular protein are described.

Sugar derivatives and uses thereof to prepare novel senolytic agents

Provided herein are novel sugar derivatives which are intermediates for preparing senolytic agents that selectively kill senescent cells associated with numerous pathologies and diseases, including age-related pathologies and diseases.

Sugar derivatives and uses thereof to prepare novel senolytic agents

Provided herein are novel sugar derivatives which are intermediates for preparing senolytic agents that selectively kill senescent cells associated with numerous pathologies and diseases, including age-related pathologies and diseases.