C07D305/14

Carbocyclic sulfone RORγ modulators

Described are RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders. ##STR00001##

Carbocyclic sulfone RORγ modulators

Described are RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders. ##STR00001##

Thermal extraction method and product

The present invention is related to a thermal extract of a plant material and methods of extraction thereof. The method of producing a thermal extract from a plant starting material by means of a thermal extraction of the starting material wherein the improvement consists in requiring smaller amounts of costly and/or toxic organic solvents for the extraction and partitioning steps.

Thermal extraction method and product

The present invention is related to a thermal extract of a plant material and methods of extraction thereof. The method of producing a thermal extract from a plant starting material by means of a thermal extraction of the starting material wherein the improvement consists in requiring smaller amounts of costly and/or toxic organic solvents for the extraction and partitioning steps.

INTEGRATED METHODS AND SYSTEMS FOR PRODUCING AMIDE AND NITRILE COMPOUNDS

Provided herein are integrated methods and systems for the production of acrylamide and acrylonitrile compounds and other compounds from at least beta-lactones and/or beta-hydroxy amides.

LIPID CONJUGATE PREPARED FROM SCAFFOLD MOIETY
20220226480 · 2022-07-21 ·

The application relates to a lipid conjugate of formula M-X1-L wherein M is a molecule of interest such as a drug moiety; X1 is a linker group such as ester, ether or carbamate; and L is a lipid scaffold represented by formula (IId): -L1-[L2(H)(X2R)]n-L3-[L4(H)(X2R)]p-L5-L6 and wherein L comprises 5 to 40 carbon atoms and 0 to 2 carbon-carbon double bonds. The lipid conjugate can p be formulated in a drug delivery vehicle such as a lipid nanoparticle (LNP).

THERAPEUTIC DENDRIMER
20210380765 · 2021-12-09 ·

Provided herein are dendrimers comprising: a core unit, five generations of building units which are lysine residues or analogues thereof, first terminal groups comprising a cabazitazel residue covalently attached to a diglycolyl linker group, and second terminal groups comprising a PEG group. Also provided herein are pharmaceutical compositions comprising the dendrimers, and methods and uses of the dendrimers in therapy of disorders such as cancers. Processes for making the dendrimers and intermediates are also provided.

CANNABINOID COMPOSITIONS AND USE THEREOF
20220151982 · 2022-05-19 ·

Methods of rapidly inhibiting efflux from a cell, sensitizing a drug-resistant cell to a drug and treating a subject with a drug-resistant pathology, by administering tetrahydrocannabinolic acid (THCa), cannabidiol (CBD) or a combination thereof are provided. Pharmaceutical compositions comprising THCa, CBD or a combination thereof and a drug are also provided.

ARTHROPOD CONTROLLING COMPOSITION
20220142157 · 2022-05-12 ·

Described herein are an arthropod controlling composition including a compound according to a formula (I), methods, and uses to control arthropods as well as arthropod controlling articles including the same.

LYMPHATIC MEDIATED TRANSPORT-BASED TRIGLYCERIDE PRODRUG, AND PREPARATION METHOD THEREFOR

In the field of medical technologies, there is a triglyceride prodrug based on lymphatic-mediated transport, particularly a triglyceride prodrug with different linking chains for lymphatic-mediated transport, and a method for preparing the same and use thereof in drug delivery. The prodrugs are linked by different linking bonds and methods for synthesizing the same. The structures of the prodrugs are as follows:

##STR00001##

wherein X, R.sub.1, R.sub.2, n, m are as described in the claims and specification. A mechanism of digestion and absorption of glycerol in the gastrointestinal tract is simulated by using a triglyceride-like structure, so as to promote the lymphatic transport of the drugs and avoid a first-pass effect. The prodrugs have targeting properties and can significantly increase or improve oral bioavailability.