Patent classifications
C07J63/008
NEUROACTIVE STEROIDS AND COMPOSITIONS THEREOF
Provided herein is a compound of the Formula (I) or a pharmaceutically acceptable salt thereof, wherein R.sup.2a, R.sup.2b, R.sup.3a, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6, R.sup.7, R.sup.11a, R.sup.11b, R.sup.15a, R.sup.15b, R.sup.16, R.sup.17, R.sup.19, R.sup.X, R.sup.Y, and t are defined herein. 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##
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.
Glycyrrhetinic acid derivatives for treating hyperkalemia
The present invention provides a compound of formula (I) or a salt thereof: (I) wherein X, L, V, R.sub.1, R.sub.2, R.sub.3 and R.sub.4, are as defined herein. These compounds are inhibitors of 11-hydroxysteroid dehydrogenase type 2 (11-HSD-2) and are used to treat hyperkalemia. ##STR00001##
COMPOUNDS WITH HIV MATURATION INHIBITORY ACTIVITY
The present invention relates to the mesylate (CH.sub.3SO.sub.2.sup.−) salt of the following compound:
##STR00001##
Saponin Conjugates
The current invention relates to an effector moiety capable of inducing an intracellular effect when present inside a mammalian cell, the effector moiety comprising a payload conjugated with at least one saponin. The invention also relates to an antibody-drug conjugate comprising the effector moiety according to the invention, or a ligand-drug conjugate comprising the effector moiety of the invention, the effector moiety comprising covalently coupled saponin. The invention also relates to a therapeutic combination comprising: (a) the effector moiety of the invention, comprising at least one saponin, and optionally a pharmaceutically acceptable excipient; and (b) an antibody-drug conjugate or a ligand-drug conjugate, and optionally a pharmaceutically acceptable excipient. Further, the invention relates to a pharmaceutical composition comprising the effector moiety of the invention or the antibody-drug conjugate of the invention or the ligand-drug conjugate of the invention, comprising at least one saponin covalently linked to the effector molecule, and optionally a pharmaceutically acceptable excipient. The invention also relates to the effector moiety of the invention or the antibody-drug conjugate of the invention or the therapeutic combination of the invention or the ligand-drug conjugate of the invention or the pharmaceutical composition of the invention, for use as a medicament. Finally, the invention also relates to the effector moiety of the invention or the antibody-drug conjugate of the invention or the therapeutic combination of the invention or the ligand-drug conjugate of the invention or the pharmaceutical composition of the invention, for use in the treatment or prevention of a cancer or an autoimmune disease.
METHODS AND COMPOUNDS FOR MODULATING THE SECRETION OR EXPRESSION OF ADHESION PROTEINS OR ANGIOPOIETINS OF CELLS
This invention provides methods, processes, compounds and compositions for modulating the gene expression or secretion of adhesion proteins, angiopoietins or their receptors to cure diseases, for anti-angiogenesis and for treating parasites, wherein the adhesion proteins or receptors comprise fibronectin, integrins family, myosin, vitronectin, collagen, laminin, glycosylation cell surface proteins, polyglycans, cadherin, heparin, tenascin, CD 54, CAM, elastin and FAK; wherein the angiopoietins comprise angiopoietin 1, angiopoietin 2, angiopoietin 3, angiopoietin 4, angiopoietin 5, angiopoietin 6, angiopoietin 7, angiopoietin-like 1, angiopoietin-like 2, angiopoietin-like 3, angiopoietin-like 4, angiopoietin-like 5, angiopoietin-like 6, and angiopoietin-like 7; wherein the cancers comprise breast cancer, leukocyte cancer, liver cancer, ovarian cancer, bladder cancer, prostate cancer, skin cancer, bone cancer, brain cancer, leukemia cancer, lung cancer, colon cancer, CNS cancer, melanoma cancer, renal cancer, cervical cancer, esophageal cancer, testicular cancer, spleenic cancer, kidney cancer, lymphatic cancer, pancreas cancer, stomach cancer and thyroid cancer.
TERPINOID DERIVATIVES AND USES THEREOF
Described herein are terpinoid derivatives as NRF2 inhibitors and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of inflammatory diseases.
2,2-DIFLUOROPROPIONAMIDE DERIVATIVES OF BARDOXOLONE METHYL, POLYMORPHIC FORMS AND METHODS OF USE THEREOF
The present invention relates generally to the compound: N-((4aS,6aR,6bS,8aR,12aS,14aR,14bS)-11-cyano-2,2,6a,6b,9,9,12a-heptamethyl-10,14-dioxo-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,12a,14,14a,14b-octadecahydropicen-4a-yl)-2,2-difluoropropanamide,
polymorphic forms thereof, methods for preparation and use thereof, pharmaceutical compositions thereof, and kits and articles of manufacture thereof.
COMPOUNDS WITH HIV MATURATION INHIBITORY ACTIVITY
The present invention relates to compound of Formula I or a pharmaceutically acceptable salt thereof
##STR00001## wherein R.sup.1 is
##STR00002##
where the squiggly line indicates the point of attachment to the rest of the molecule; R.sup.2 is F or
##STR00003##
where the squiggly line indicates the point of attachment to the rest of the molecule; R.sup.3 is H or CH.sub.3; Z is O or is absent; and R.sup.4 is —OC.sub.1-3alkyl, C.sub.1-30alkyl, or —N(CH.sub.3).sub.2.
FLUORINATED AND ALKYLATED BILE ACIDS
The present invention relates to fluorinated and alkylated bile acids.