Patent classifications
C07J53/00
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.
DERIVATIVES OF BETULIN
The present invention relates to compounds characterized by having a structure according to the following Formula I:
##STR00001##
, or a pharmaceutically acceptable salt thereof. Compounds of the present invention are useful for the treatment or prevention of HIV.
CYCLOPENTANOPERHYDROPHENANTHRENE FRAMEWORK COMPOUNDS AND PREPARATION METHOD THEREFOR
The present invention pertains to the field of pharmaceutical chemistry, and relates to compounds having cyclopentanoperhydrophenanthrene skeletons and preparation methods therefore. The compounds have some physiological activity, and are useful as synthons/intermediates for further synthesizing some compounds having specific structures. These compounds and salts thereof are useful as lead compounds for synthesizing pharmaceuticals, pesticides and new materials. From this, further screen and preparation by chemical, biological and medical means offer new compounds that are more valuable and have important applications, achieving the object of inventing and creating new drugs.
Process for the preparation of drospirenone
A process is described wherein, by employing 17-(3-hydroxypropyl)-6,7;15,16-dimethylene-5-androstane-3,5,17-triol (II) as starting product, in a single stage reaction there is obtained drospirenone, (I), a synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic action, that is useful for preparing pharmaceutical compositions with contraceptive action. ##STR00001##
Betulinic acid proline derivatives as HIV inhibitors
The invention relates to novel betulinic acid derivatives and related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases.
Extended Triterpene Derivatives
The present invention concerns novel pharmaceutically active triterpene derivatives, pharmaceutical compositions containing the same, their use as medicaments, and the use of the compounds for the manufacture of specific medicaments. The present invention also concerns a method of treatment involving administration of the compounds. Specifically, the compounds are derivatives of betulinic acid having substitutions at one or more of the C-3, C2-8 and C-19 positions as further described herein. The novel compounds are useful as antiretroviral agents. In particular, the novel compounds are useful for the treatment of Human Immunodeficiency Virus (HIV).
Process for the preparation of drospirenone
A process is disclosed wherein, using either 17a-(3-hydroxypropyl)-6p,7p;15p,16p-dimethylene-5p-androstane-3p,5,17p-triol (II) or 3,5^I^^-6,7;15,16-dimethylene-5,17-pregnane-21,17-carbolactone (III) as starting material, through a single-step reaction it is obtained drospirenone (I), a synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic activity, useful for preparing pharmaceutical compositions with contraceptive action. ##STR00001##
N-acetyl amino acid ESTER derivatives of betulin and preparation method thereof
The present invention disclosed N-acetyl amino acid ester derivatives of betulin and the preparation method thereof, the method comprising the steps that in the presence of an alkaline substance, a catalyst and a racemization-inhibitor, the carboxyl group of N-acetyl amino acid is activated by a coupling agent; and then the activated N-acetyl amino acid is reacted with betulin via esterification reaction to obtain the N-acetyl amino acid ester derivative of betulin. The present invention provided a simple synthesis method to synthesize the N-acetyl amino acid ester derivatives of betulin by using betulin as a precursor compound and modifying the molecular structure of betulin. Such structural modification of betulin significantly enhances the anti-tumor activity of the betulin derivatives and therefore has important values.
METHOD AND APPARATUS FOR PROCESSING BIRCH BARK
The present disclosure relates to a method for processing birch bark. The present disclosure further relates to an arrangement for processing birch bark.
C17 polar-substituted heteroaromatic synthetic triterpenoids and methods of use thereof
Disclosed herein are compounds of the formula: ##STR00001##
wherein the variables are defined herein. Also provided are pharmaceutical compositions thereof. In some aspects, the compounds and compositions provided herein may be used as antioxidant inflammation modulators. In some aspects, the present disclosure provides methods wherein the compounds and composition described herein are used for the treatment of diseases and disorders, including those associated with inflammation and cancer.