Patent classifications
C07J41/0055
HYDROXYSTEROID COMPOUNDS
The present application discloses derivatives of hydroxysteroids, pharmaceutically acceptable salts, stereoisomers or tautomers thereof. The compounds and compositions described herein can be used in therapy.
Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
The present invention provides compounds of Formula I, ##STR00001##
pharmaceutical compositions comprising these compounds and methods of using these compounds to prevent or treat FXR-mediated or TGR5-mediated diseases or conditions.
Glucosamine derivatives for the prevention or treatment of joint disorders
There are provided compounds of Formula (A) and pharmaceutically acceptable salts and esters thereof, and pharmaceutical compositions thereof, used for the prevention or treatment in a mammal of joint and bone disorders such as arthritis and osteoporosis. ##STR00001##
CATIONIC STEROIDAL ANTIMICROBIAL COMPOUNDS WITH ENDOGENOUS GROUPS
Cationic steroidal antimicrobial (CSA) compounds having a structure of Formula I, II or III, or salt thereof, wherein at least one of R.sub.1-R.sub.18, (e.g., R.sub.18) includes a terpenyl group attached via an ester or amide linkage and at least one R.sub.1-R.sub.18, (e.g., R.sub.3, R.sub.7 and R.sub.12) is an amino acid linked to the steroidal backbone by an ester or amide linkage:
##STR00001## R.sub.18 has the following structure:
—R.sub.19—(C═O)—X—R.sub.20 where R.sub.19 is omitted or alkyl, alkenyl, alkynyl, or aryl, X is oxygen or nitrogen, and R.sub.20 is a terpenyl group. R.sub.3, R.sub.7 and R.sub.12 have the following structure:
R.sub.22R.sub.23N—R.sub.21—(C═O)—X— where R.sub.21 is substituted or unsubstituted alkyl, X is oxygen or nitrogen, and R.sub.22 and R.sub.23 are independently hydrogen, alkyl, alkenyl, alkynyl, or aryl.
NOVEL ANNULATION CATALYSTS VIA DIRECT C-H BOND AMINATION
Disclosed are compounds, methods, reagents, systems, and kits for the preparation and utilization of monomeric or polymeric metal-based compounds. These metal-based compounds are organometallic catalysts composed of substituted dipyrrin ligands bound to transition metals. C—H bond functionalization catalysis can be performed with the disclosed organometallic catalysts to yield C—N bonds to generate substituted bicyclic, spiro, and fused nitrogen-containing heterocycles, all common motifs in various pharmaceutical and bioactive molecules.
SYNTHETIC DERIVATIVES OF CHOLIC ACID 7-SULFATE AND USES THEREOF
The compositions and methods provided herein are related, in part, to the discovery of cholic acid 7-sulfate as a treatment for diabetes. Provided herein is a method for treating a metabolic disorder (e.g., diabetes, obesity), or an inflammatory disease (e.g., Crohn's disease, inflammatory bowel disease, ulcerative colitis, pancreatitis, hepatitis, appendicitis, gastritis, diverticulitis, celiac disease, food intolerance, enteritis, ulcer, gastroesophageal reflux disease (GERD), psoriatic arthritis, psoriasis, and rheumatoid arthritis) in a subject in need thereof comprising administering to a subject a compound of Formulae (I)-(XVII).
STEROL PURIFICATION
The invention relates to sterol esters and methods for producing purified sterols that can be utilized in methods for producing a lipid nanoparticle.
NEUROACTIVE STEROIDS AND THEIR METHODS OF USE
Provided herein is a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R.sup.19, R.sup.5, R.sup.3a, R.sup.1a, R.sup.1b, R.sup.2a, R.sup.2b, R.sup.4a, R.sup.4b, R.sup.6a, R.sup.6b, R.sup.7a, R.sup.7b, R.sup.11a, R.sup.11b, R.sup.12a, R.sup.12b, R.sup.18, R.sup.D, and q are defined herein. L is selected from the group consisting of: wherein A indicates the point of attachment at C17 and wherein X is selected from the group consisting of —C(0)N(R.sup.55a)(R.sup.55b), —N(R.sup.55a)(R.sup.55b), —N(R.sup.55b)C(O)(R.sup.55a), and R.sup.55C wherein R.sup.55c is carbon-bound substituted or unsubstituted heteroaryl or substituted or unsubstituted aryl. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.
##STR00001##
COMPOSITIONS FOR THE DELIVERY OF PAYLOAD MOLECULES TO AIRWAY EPITHELIUM
The present disclosure provides LNPs comprising payload molecules, e.g., mRNA therapeutics, for the treatment of diseases or disorders, which would benefit from delivery of payload molecules to airway cells.
COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS
Described herein are neuroactive steroids of the Formula (II): or a pharmaceutically acceptable salt thereof; wherein A, R.sup.1, R.sup.2a, R.sup.2b, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6 and are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e. g., such for inducing sedation and/or anesthesia.
##STR00001##