C07J71/00

Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid

The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I): ##STR00001##
wherein: custom character, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and Y are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.

Sterol derivatives and preparation method and uses thereof

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##

Withanolides useful for the treatment of neurodegenerative diseases

Provided herein are synthetic analogs of withanolide natural products and their pharmaceutical uses in treating neurodegenerative diseases.

NEW TECHNOLOGY TO CONJUGATE THE TACCALONOLIDE MICROTUBULE STABILIZERS WITH LINKERS/PAYLOADS
20230061432 · 2023-03-02 ·

The present disclosure is concerned with taccalonolide analogs and conjugated taccalonolide analogs useful as cellular probes and in the treatment of, for example, hyperproliferative disorders such as cardiovascular diseases and cancer. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

TRITERPENOID COMPOUNDS, PHARMACEUTICAL COMPOSITIONS THEREOF, AND THEIR USE FOR TREATING A NUCLEAR RECEPTOR SUBFAMILY 4 GROUP A MEMBER 1-MEDIATED DISEASE

Disclosed herein are triterpenoid compounds, for example, a compound of Formula (I), and pharmaceutical compositions thereof. Also disclosed herein are methods of their use for treat.

##STR00001##

TRACELESS LINKERS AND PROTEIN-CONJUGATES THEREOF
20230119539 · 2023-04-20 ·

Provided herein are compounds, compounds including traceless linkers, protein conjugates thereof, and compositions thereof. Also provided herein are methods for the treatment of diseases, disorders, and conditions, and/or the management of the symptoms thereof, associated with inflammatory diseases and autoimmune disorders further associated with the glucocorticoid receptor, glucocorticoid binding, and/or glucocorticoid receptor signalling, including administration of the compounds or payloads via traceless linker-payloads, and protein conjugates thereof.

Betulastatin compounds

The present disclosure relates to Betulastatin compounds, pharmaceutical compositions and kits comprising such compounds, and methods for using such compounds or pharmaceutical compositions.

GLUCOCORTICOID RECEPTOR AGONISTS

The present invention provides a compound of Formula I:

##STR00001##

wherein R is H or

##STR00002##

R.sup.1 is H, halogen, C1-C3 alkyl, C3-C6 cycloalkyl, C1-C3 alkoxy, C2-C3 alkenyl, OCF.sub.3,

##STR00003##

R.sup.2 is H, halogen, C1-C3 alkyl, C1-C3 alkoxy, or C2-C4 alkenyl;
R.sup.3 is NH.sub.2, or CH.sub.2NH.sub.2; and
X is O, OCH.sub.2, OCH.sub.2CH.sub.2, OCH(CH.sub.3), CH.sub.2O, SCH.sub.2, CH.sub.2S, CH.sub.2, NHCH.sub.2, CH.sub.2NH, N(CH.sub.3)CH.sub.2, CH.sub.2CH.sub.2, C≡C, or a bond, wherein X is connected to phenyl ring A at the ortho or the meta position, 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 and rheumatoid arthritis.

BUDESONIDE 21-PHOSPHATE SALTS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

The present invention relates to salts of budesonide 21-phosphate with β2 adrenergic agonists, preferably with formoterol, pharmaceutical compositions containing the same and the use thereof in the treatment of respiratory inflammatory pathologies, obstructive pathologies and allergen-induced airway dysfunctions. The invention further relates to the process for preparing said salts.

HEXADECAHYDRO-1H-CYCLOPENTA[A]PHENANTHRENE DERIVATIVES USEFUL IN TREATING PAIN AND INFLAMMATION

Wherein, R.sup.1, R.sup.2, R.sup.3, R.sup.4a, R.sup.4b and R.sup.5 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds are useful in treating inflammation and/or pain. Compositions comprising a compound of the invention are also disclosed, as are methods of using the compounds to treat inflammation and/or pain.