C07H15/08

Processes for the preparation of GalNAc acid derivatives
10597417 · 2020-03-24 · ·

The invention comprises a new process for the preparation of GalNAc derivatives of the formula I ##STR00001## wherein n is an integer between 0 and 10 and its salts, corresponding enantiomers and/or optical isomers thereof. The GalNAc acid derivative of formula I can be used for the preparation of therapeutically valuable GalNAc oligonucleotide conjugates.

Galnac cluster phosphoramidite
10590156 · 2020-03-17 · ·

The invention comprises GalNAc phosphoramidite derivatives of the formula I ##STR00001## wherein R.sup.1 is a hydroxy protecting group, n is an integer from 0 to 10 and m is an integer from 0 to 20 and its corresponding enantiomers and/or optical isomers thereof. The invention further comprises a process for the preparation of the GalNAc phosphoramidite derivatives of the formula I and its use in the preparation of therapeutically valuable GalNAc-cluster oligonucleotide conjugates.

Galnac cluster phosphoramidite
10590156 · 2020-03-17 · ·

The invention comprises GalNAc phosphoramidite derivatives of the formula I ##STR00001## wherein R.sup.1 is a hydroxy protecting group, n is an integer from 0 to 10 and m is an integer from 0 to 20 and its corresponding enantiomers and/or optical isomers thereof. The invention further comprises a process for the preparation of the GalNAc phosphoramidite derivatives of the formula I and its use in the preparation of therapeutically valuable GalNAc-cluster oligonucleotide conjugates.

CONJUGATED OLIGONUCLEOTIDE COMPOUNDS, METHODS OF MAKING AND USES THEREOF

The present invention relates to novel conjugated oligonucleotide compounds, which are suitable for therapeutic use. Additionally, the present invention provides methods of making these compounds, as well as methods of using such compounds for the treatment of various diseases and conditions.

CAPPED ALKOXYLATED ALCOHOLS
20240059973 · 2024-02-22 · ·

The invention relates to a composition comprising a mixture of C.sub.3-C.sub.22 alcohol alkoxylates which have a narrow weight distribution and are capped in the terminal portion by a group chosen from linear or branched alkyls comprising between 1 and 6 carbon atoms, the phenyl group, benzyl group and hydrocarbon groups having a carboxy function COO, and groups having a sugar unit. The invention also relates to the method for preparing said composition and to the uses thereof as a surfactant, in particular as a surfactant with low foaming power.

Targeted nucleic acid conjugate compositions

The invention provides conjugates that comprise a targeting moiety, a nucleic acid, and optional linking groups as well as synthetic intermediates and synthetic methods useful for preparing the conjugates. The conjugates are useful to target therapeutic nucleic acids to the liver and to treat liver diseases including hepatitis (e.g. hepatitis B and hepatitis D).

Targeted nucleic acid conjugate compositions

The invention provides conjugates that comprise a targeting moiety, a nucleic acid, and optional linking groups as well as synthetic intermediates and synthetic methods useful for preparing the conjugates. The conjugates are useful to target therapeutic nucleic acids to the liver and to treat liver diseases including hepatitis (e.g. hepatitis B and hepatitis D).

Vaccine against <i>Klebsiella pneumoniae</i>

The present invention relates to a synthetic oligosaccharide of general formula (I): T*-[(U.sub.x+4U.sub.x+3U.sub.x+2U.sub.x+1U.sub.x).sub.m(V.sub.x+2V.sub.x+1V.sub.x).sub.1-m-T-O-L-E that is related to Klebsiella pneumoniae serotype O3, O3b and/or O5 lipopolysaccharide and conjugate thereof. Said synthetic oligosaccharide, said conjugate and pharmaceutical composition containing said synthetic oligosaccharide or said conjugate are useful for prevention and/or treatment of diseases associated with Klebsiella pneumoniae. Furthermore, the synthetic oligosaccharide of general formula (I) is useful as marker in immunological assays for detection of antibodies against Klebsiella pneumoniae serotype O3, O3b and/or O5 bacteria.

Vaccine against <i>Klebsiella pneumoniae</i>

The present invention relates to a synthetic oligosaccharide of general formula (I): T*-[(U.sub.x+4U.sub.x+3U.sub.x+2U.sub.x+1U.sub.x).sub.m(V.sub.x+2V.sub.x+1V.sub.x).sub.1-m-T-O-L-E that is related to Klebsiella pneumoniae serotype O3, O3b and/or O5 lipopolysaccharide and conjugate thereof. Said synthetic oligosaccharide, said conjugate and pharmaceutical composition containing said synthetic oligosaccharide or said conjugate are useful for prevention and/or treatment of diseases associated with Klebsiella pneumoniae. Furthermore, the synthetic oligosaccharide of general formula (I) is useful as marker in immunological assays for detection of antibodies against Klebsiella pneumoniae serotype O3, O3b and/or O5 bacteria.

SUBSTITUTED-6,8-DIOXABICYCLO[3.2.1]OCTANE-2,3-DIOL COMPOUNDS AS TARGETING AGENTS OF ASGPR
20190321382 · 2019-10-24 · ·

Compounds of Formula (A) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by pharmaceutical compositions and the uses thereof as asialoglycoprotein receptor (ASGPR) targeting agents.

##STR00001##