Patent classifications
C07J71/00
PREPARATIONS OF HYDROPHOBIC THERAPEUTIC AGENTS, METHODS OF MANUFACTURE AND USE THEREOF
The present invention further provides method of preparing nanocrystals of a hydrophobic therapeutic gent such as fluticasone or triamcinolone, pharmaceutical compositions (e.g., topical or intranasal compositions) thereof and methods for treating and/or preventing the signs and/or symptoms of disorders such as blepharitis, Meibomian gland dysfuntion or skin inflammatiom or a respiratory disease (e.g., asthma).
Methods for the preparation of deoxycholic acid, and intermediates useful in the preparation of deoxycholic acid
The present invention relates to new and improved processes for the preparation of deoxycholic acid (DCA) and pharmaceutically acceptable salts thereof, as well as to novel intermediates useful for the preparation of DCA and pharmaceutically acceptable salts thereof. The starting compounds are steroids, sterols or fermented phytosterols of vegetable origin, being of formula SM: ##STR00001##
Process and intermediates for the synthesis of obeticholic acid and derivatives thereof
A process for the preparation of obeticholic acid and derivatives thereof by: (a) hydrogenation of the double bond and reductive opening of the epoxide of a compound of formula (II) or a salt or solvate thereof ##STR00001## to obtain a compound of formula (IIIa) and/or (IIIb), or salts or solvates thereof ##STR00002## and (b) conversion of a compound of formula (IIIa) and/or a compound of formula (IIIb), or a salt or solvate thereof, into a compound of formula (I), or a salt or solvate thereof ##STR00003##
Aqueous suspensions of ciclesonide for nebulisation
This invention relates to a method for the preparation of sterile aqueous suspensions of ciclesonide by sterilization with moist heat. The invention further relates to pharmaceutical compositions in particular to sterile aqueous suspensions of ciclesonide for administration by nebulization in the prophylaxis and/or treatment of respiratory diseases.
Aqueous suspensions of ciclesonide for nebulisation
This invention relates to a method for the preparation of sterile aqueous suspensions of ciclesonide by sterilization with moist heat. The invention further relates to pharmaceutical compositions in particular to sterile aqueous suspensions of ciclesonide for administration by nebulization in the prophylaxis and/or treatment of respiratory diseases.
COMPOUNDS, COMPOSITIONS, AND METHODS FOR TREATMENT OF ANDROGEN-MEDIATED DISEASE
Provided herein are steroid sulfatase inhibitor compounds and androgen receptor inhibitor compounds that can be useful in, for example, the treatment of cancers such as prostate cancer and breast cancer. Pharmaceutical compositions and kits including the compounds are described, as well as methods for the treatment of cancer such as prostate cancer and breast cancer.
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: , 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.
7-dehydrocholesterol derivatives and methods using same
The present invention provides, in certain aspects, novel 7-dehydrocholesterol (7DHC) derivatives that are useful in treating or preventing cancer, as well as in treating or preventing uncontrolled angiogenesis, in a subject. In certain embodiments of the present invention, the subject is a human. In other aspects, the present invention provides a method of preparing compounds of the invention, or a salt or solvate thereof.
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:, 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##