C07H17/02

MADRASIN-DERIVATIVE COMPOUNDS, COMPOSITION AND USES THEREOF FOR TREATING CANCER

The present invention relates to the fields of medicine and in particular cancer treatment. The invention more specifically relates to new compounds which are typically for use as a medicament. In particular, the invention relates to the use of these new compounds for increasing the presentation, typically the production and presentation, of Pioneer Translation Products (PTPs)-derived antigens by cells, in particular cancer cells, or changing the immunopeptidome, in a subject, and inducing or stimulating an immune response in the subject. The present disclosure also relates to uses of such compounds, in particular to prepare a pharmaceutical composition and/or to allow or improve the efficiency of a therapy in a subject in need thereof. The invention also discloses methods for treating a disease, in particular cancer, for preventing or treating cancer metastasis and/or cancer recurrence, in a subject. The present invention in addition provides kits suitable for preparing a composition according to the present invention and/or for implementing the herein described methods.

AROMATIC RING COMPOUND

A novel aromatic ring compound is represented by general formula (I). This compound, isomer, prodrug, solvate, pharmaceutically acceptable salt and pharmaceutical composition thereof are useful in preparing medicaments for treating depression and related symptoms.

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AROMATIC RING COMPOUND

A novel aromatic ring compound is represented by general formula (I). This compound, isomer, prodrug, solvate, pharmaceutically acceptable salt and pharmaceutical composition thereof are useful in preparing medicaments for treating depression and related symptoms.

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Modular synthesis of amphiphilic Janus glycodendrimers and their self-assembly into glycodendrimersomes

The invention concerns compounds of the formula (I) wherein: Y.sup.1 and Y.sup.2 are independently a monosaccharide or disaccharide; X.sup.1 and X.sup.2 are independently —(R.sup.9—O).sub.m—, —(R.sup.10).sub.p—, —O—(R.sup.11—O).sub.q—, —R.sup.16—O—R.sup.17—O— or a covalent bond; Q.sup.1 and Q.sup.2 are independently a nitrogen-containing heterocycle moiety; Z.sup.1 and Z.sup.2 are independently —(O—R.sup.7)—, —(O—C(═O)—R.sup.8)a-, —O—C(═O)—R.sup.12—C(=0)-R.sup.13—, —O—C(═O)—R.sup.14—C(═O)—R.sup.15 or a covalent bond; R.sup.7-R.sup.17 are each independently C.sub.1-C.sub.6 alkyl; R.sup.1-R.sup.6 are each independently a linear or branched alkyl group; b, c, d, e, f, and g are 0 or 1, provided b+c+d equals at least 2 and e+f+g equals at least 2; and a, m, p, and q are each an integer from 1-6. ##STR00001##

Modular synthesis of amphiphilic Janus glycodendrimers and their self-assembly into glycodendrimersomes

The invention concerns compounds of the formula (I) wherein: Y.sup.1 and Y.sup.2 are independently a monosaccharide or disaccharide; X.sup.1 and X.sup.2 are independently —(R.sup.9—O).sub.m—, —(R.sup.10).sub.p—, —O—(R.sup.11—O).sub.q—, —R.sup.16—O—R.sup.17—O— or a covalent bond; Q.sup.1 and Q.sup.2 are independently a nitrogen-containing heterocycle moiety; Z.sup.1 and Z.sup.2 are independently —(O—R.sup.7)—, —(O—C(═O)—R.sup.8)a-, —O—C(═O)—R.sup.12—C(=0)-R.sup.13—, —O—C(═O)—R.sup.14—C(═O)—R.sup.15 or a covalent bond; R.sup.7-R.sup.17 are each independently C.sub.1-C.sub.6 alkyl; R.sup.1-R.sup.6 are each independently a linear or branched alkyl group; b, c, d, e, f, and g are 0 or 1, provided b+c+d equals at least 2 and e+f+g equals at least 2; and a, m, p, and q are each an integer from 1-6. ##STR00001##

2' FLUORO SUBSTITUTED CARBA-NUCLEOSIDE ANALOGS FOR ANTIVIRAL TREATMENT

Provided are methods for treating Orthomyxoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula I:

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wherein R.sup.2 is halogen. The compounds, compositions, and methods provided are particularly useful for the treatment of Human Influenza virus infections.

5′-end derivatives

The present invention provides compounds of formula (1). Another aspect of the invention relates to a method of inhibiting the expression of a gene in call, the method comprising (a) contacting an oligonucleotide of the invention with the cell; and (b) maintaining the cell from step (a) for a time sufficient to obtain degradation of the mRNA of the target gene. ##STR00001##

5′-end derivatives

The present invention provides compounds of formula (1). Another aspect of the invention relates to a method of inhibiting the expression of a gene in call, the method comprising (a) contacting an oligonucleotide of the invention with the cell; and (b) maintaining the cell from step (a) for a time sufficient to obtain degradation of the mRNA of the target gene. ##STR00001##

Selective glycosidase inhibitors and uses thereof

The invention provides compounds of formula (I) with substituents as specified in claim 1 for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceuticals compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to over-expression of O-GlcNAcase or accumulation of O-GlcNac. ##STR00001##

Selective glycosidase inhibitors and uses thereof

The invention provides compounds of formula (I) with substituents as specified in claim 1 for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceuticals compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to over-expression of O-GlcNAcase or accumulation of O-GlcNac. ##STR00001##