C07J71/00

NOVEL PROCESS FOR PREPARATION OF GLUCOCORTICOID STEROIDS

The present invention discloses a process for the preparation of 16, 17-acetals of pregnane derivatives having formula I

##STR00001##

wherein each substituent is independently selected from; R.sub.1 is H or CH.sub.3; R.sub.2 is C.sub.1-C.sub.6 linear or branched alkyl, alkynyl group or cycloalkyl group; aryl or heteroaryl group; or R.sub.1 and R.sub.2 combine to form saturated, unsaturated C.sub.3-C.sub.6 cyclic or heterocyclic ring; R.sub.3 and R.sub.4 are same or different and each independently represents H or halogen; R.sub.5 is —OH or —OCOR wherein R represents H or C.sub.1-C.sub.6 linear, branched or cyclic alkyl group that may be substituted.

Polymeric bile acid derivatives inhibit Hepatitis B and D virus and NTCP transport

The invention provides for treating HBV or HDV infection or inhibiting human sodium taurocholate co-transporting polypeptide (hNTCP) with a polymeric bile acid or salt thereof, and pharmaceutical compositions comprising a polymeric bile acid or salt thereof, and a second HBV or HDV medicament.

CARBOXY SUBSTITUTED GLUCOCORTICOID RECEPTOR AGONISTS
20230227493 · 2023-07-20 ·

The present invention provides a compound of Formula I:

##STR00001##

wherein R.sup.1 is H, halogen, C1-C3 alkyl, or C1-C3 alkoxy; R.sup.2 is H or halogen; and X is O, OCH.sub.2, or CH.sub.2, or a pharmaceutically acceptable salt thereof, wherein the compound of Formula I, or pharmaceutically acceptable salt thereof is useful for treating autoimmune and inflammatory diseases, such as atopic dermatitis, rheumatoid arthritis, and lupus nephritis.

STEROL ANALOGS AND USES THEREOF
20220402965 · 2022-12-22 ·

The invention relates to compositions and methods for the preparation, manufacture, and therapeutic use of compositions comprising mRNA and a lipid nanoparticle comprising a compound of the invention and an ionizable lipid.

STEROL DERIVATIVES AND PREPARATION METHOD AND USES THEREOF
20220389051 · 2022-12-08 ·

The present invention pertains to pharmaceutical chemical field, and relates to a sterol derivative as well as preparation method and uses thereof. Specifically, the present invention relates to a compound of Formula I, or a pharmaceutically acceptable salt, ester or ether thereof, wherein, R.sub.1 is selected from the group consisting of —OH, ═O(carbonyl), H, and C.sub.1-C.sub.3 alkyl; R.sub.2 is selected from the group consisting of —OH, H, and C.sub.1-C.sub.3 alkyl; R.sub.3 is selected from the group consisting of —OH, ═O, H, and C.sub.1-C.sub.3 alkyl; R.sub.4 is selected from the group consisting of —OH, H, and C.sub.1-C.sub.3 alkyl; and none, one, two, three or four of R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are —OH. The compound of the present invention can inhibit HMG-CoA reductase, tumor cells and lipase effectively, and is a potential drug for reducing blood-fat, antitumors, or for losing weight.

##STR00001##

HUMAN SQUALAMINE DERIVATIVES (ENT-06), RELATED COMPOSITIONS COMPRISING THE SAME, AND METHOD OF USING THE SAME
20220372066 · 2022-11-24 · ·

The present application relates generally to novel aminosterol compounds, compositions comprising the same, and methods of making and using the novel aminosterol compounds and compositions.

C4-modified oleanolic acid derivatives for inhibition of IL-17 and other uses

Disclosed herein are C4 modified oleanolic acid derivatives of the formula: Formula (X) or Formula (XII), as well as analogs thereof, wherein the variables are defined herein. In addition, disclosed herein are pharmaceutical compositions of these derivatives or analogs, methods for their manufacture, and methods for their use, including for the prevention and treatment of diseases or disorders associated with overproduction of IL-17. ##STR00001##

GLUCOCORTICOID RECEPTOR AGONIST AND IMMUNOCONJUGATES THEREOF

Provided herein are glucocorticoid receptor agonist immunoconjugates, glucocorticoid receptor agonists, and methods of using the same, e.g., to treat autoimmune or inflammatory diseases.

Natural and synthetic compounds for treating cancer and other diseases
11485755 · 2022-11-01 ·

This invention provides a method of synthesizing new active compounds for pharmaceutical uses including cancer treatment, wherein the cancers comprise breast, leukocytic, liver, ovarian, bladder, prostatic, skin, bone, brain, leukemia, lung, colon, CNS, melanoma, renal, cervical, esophageal, testicular, spleenic, kidney, lymphatic, pancreatic, stomach and thyroid cancers. This invention is an anti-adhesion therapy which uses the compound as a mediator or inhibitor of adhesion proteins and angiopoietins. It inhibits excess adhesion and inhibits cell attachment. It modulates angiogenesis. The compounds also use as mediator of cell adhesion receptor, cell circulating, cell moving and inflammatory diseases. The compounds are attached with angeloyl, acetyl, tigloyl, senecioyl, Crotonoyl, 3,3-Dimethylacryloyl, Cinnamoyl, Pentenoyl, Hexanoyl, benzoyl, Ethylbutyryl, benzoyl, dibenzoyl, alkanoyl, alkenoyl, benzoyl alkyl substituted alkanoyl, ethanoyl, propanoyl, propenoyl, butanoyl, butenoyl, pentanoyl, hexenoyl, heptanoyl, heptenoyl, octanoyl, octenoyl, nonanoyl, nonenoyl, decanoyl, decenoyl, propionyl, 2-propenoyl, 2-butenoyl, Isobutyryl, 2-methylpropanoyl, 2-ethylbutyryl, ethylbutanoyl, 2-ethylbutanoyl, butyryl, (E)-2,3-Dimethylacryloyl, (E)-2-Methylcrotonoyl, 3-cis-Methyl-methacryloyl, 3-Methyl-2-butenoyl, 3-Methylcrotonoyl, 4-Pentenoyl, (2E)-2-pentenoyl, Caproyl, 5-Hexenoyl, Capryloyl, Lauroyl, Dodecanoyl, Myristoyl, Tetradecanoyl, Oleoyl, O—C(2-18) Acyl.

Tripartite Androgen Receptor Eliminators, Methods and Uses Thereof
20230092979 · 2023-03-23 · ·

The present specification discloses tripartite androgen receptor eliminators (AREs), pharmaceutical compositions and medicaments comprising such AREs, methods and uses for such AREs and compositions and medicaments, and methods and uses for AREs and compositions and medicaments for treating an androgen receptor signaling-mediated condition, disease or disorder.