C07F9/572

Psilocin derivatives as serotonergic psychedelic agents for the treatment of CNS disorders
11427604 · 2022-08-30 · ·

The present application relates to psilocin derivatives of Formula (I), to processes for their preparation, to compositions comprising them and to their use in activation of a serotonin receptor in a cell, as well as to treating diseases, disorders or conditions by activation of a serotonin receptor in a cell. ##STR00001##

Synthesis of Phosphoramidates

A process for the preparation of a compound of formula (I) including all isomers, stereoisomers, enantiomers and diastereomers thereof (I), and salts thereof; the process comprising providing a mixture comprising a compound of formula (II) and a compound of formula (III) subjecting the mixture provided in a) to reaction conditions in the presence of one or more Lewis acids to the mixture provided in a), obtaining a mixture comprising the compound of formula (I).

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Synthesis of Phosphoramidates

A process for the preparation of a compound of formula (I) including all isomers, stereoisomers, enantiomers and diastereomers thereof (I), and salts thereof; the process comprising providing a mixture comprising a compound of formula (II) and a compound of formula (III) subjecting the mixture provided in a) to reaction conditions in the presence of one or more Lewis acids to the mixture provided in a), obtaining a mixture comprising the compound of formula (I).

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PRODUCTION METHOD FOR BIFURCATED LIPID-LINKED OLIGONUCLEOTIDE, AND INTERMEDIATE

Provided are production methods capable of controlling quality of a bifurcated lipid-linked oligonucleotide, and intermediates which is useful for the production method, has good stability, and is easy to manage and analyze. Specifically, it is a method for producing a bifurcated lipid-linked oligonucleotide including a step of reacting a compound of formula (II):

##STR00001## wherein Pro.sup.1 to Pro.sup.4 are each independently a protecting group; Pro.sup.1 and Pro.sup.2 or Pro.sup.3 and Pro.sup.4 may be taken together to form a protecting group; m, n and p are each independently an integer of 0 to 5; and Y is a group of a formula: —P(OC.sub.2H.sub.4CN)(N(i-Pr).sub.2), or the like, with an oligonucleotide.

FUNCTIONAL LIPID CONSTRUCTS

The invention relates to functional lipid constructs and their use in diagnostic and therapeutic applications, including serodiagnosis, where the functional moiety is carbohydrate, peptide, chemically reactive group, conjugator or fluorophore.

LOW MOLECULAR WEIGHT MODULATORS OF THE COLD MENTHOL RECEPTOR TRPM8 AND USE THEREOF

The invention relates to new types of modulators of the cold menthol receptor TRPM8, to methods of modulating the TRPM8 receptor using these modulators; and in particular the use of the modulators for inducing a sensation of coldness; and also the articles and compositions produced using these modulators.

STAT6 inhibitors

The present disclosure provides compounds that are useful for inhibiting the STAT6 pathway. Also provided are related pharmaceutical compositions and methods of using the compounds. In some embodiments, the compounds may be used to treat a disease such as, e.g., an allergic lung disease, allergic rhinitis, chronic pulmonary obstructive disease, or a cancer.

STAT6 inhibitors

The present disclosure provides compounds that are useful for inhibiting the STAT6 pathway. Also provided are related pharmaceutical compositions and methods of using the compounds. In some embodiments, the compounds may be used to treat a disease such as, e.g., an allergic lung disease, allergic rhinitis, chronic pulmonary obstructive disease, or a cancer.

USE OF PHOSPHOROUS-CONTAINING ORGANIC OXYIMIDES AS FLAME RETARDANTS AND/OR AS STABILIZERS FOR PLASTICS, FLAME-RETARDANT AND/OR STABILIZED PLASTIC COMPOSITIONS, METHOD FOR THE PRODUCTION THEREOF, MOULDED PART, PAINT AND COATINGS

The present invention relates to the use of phosphorous-containing organic oxyimides according to the general formula (I) as flame retardant for plastic materials, as radical generators in plastic materials and/or stabilisers for plastics. In addition, the present invention relates to a flame-retardant plastic material moulding compound in which the previously described phosphorous-containing organic oxyimides are integrated, and also to a method for the production of the previously mentioned plastic material composition. Furthermore, the present invention relates to a moulded article, a paint or a coating from the previously mentioned flame-retardant plastic material composition.

A COMPOUND FOR THE DETECTION OF HNO IN BIOLOGICAL SYSTEMS

The present invention disclosed a compound of formula (I), process for preparation thereof and use of compound of formula (I) for detecting HNO in biological systems.

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