The invention relates to compounds of formula (I): ##STR00001## wherein R is ethyl, propyl or allyl, and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists.

The invention relates to compounds of formula (I): ##STR00001## wherein R is ethyl, propyl or allyl, and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists.

The present invention relates to a substance of formula (I), whereby R.sub.1 is an alkyl or alkenyl group having 6 to 20 carbon atoms; R.sub.2 is H or missing, whereby O is bound via a double bond, R.sub.3 is H or an acyl group -C(O)R.sub.5, whereby R.sub.5 is an alkyl or alkylene group having 1 to 10 carbon atoms, and R.sub.4 is H or a phosphate group for use as a medicament and for use in a method of preventing or treating a subject suffering from an autoimmune disease. The present invention further relates to a method for generating regulatory T cells (Treg cells) in vitro comprising the steps of providing precursor CD4.sup.+T cells, cultivating the precursor CD4.sup.+T cells provided in step 1) in the presence of the substance as defined herein, and, optionally, isolating the generated regulatory T cells (Treg cells).

The present invention relates to a substance of formula (I), whereby R.sub.1 is an alkyl or alkenyl group having 6 to 20 carbon atoms; R.sub.2 is H or missing, whereby O is bound via a double bond, R.sub.3 is H or an acyl group -C(O)R.sub.5, whereby R.sub.5 is an alkyl or alkylene group having 1 to 10 carbon atoms, and R.sub.4 is H or a phosphate group for use as a medicament and for use in a method of preventing or treating a subject suffering from an autoimmune disease. The present invention further relates to a method for generating regulatory T cells (Treg cells) in vitro comprising the steps of providing precursor CD4.sup.+T cells, cultivating the precursor CD4.sup.+T cells provided in step 1) in the presence of the substance as defined herein, and, optionally, isolating the generated regulatory T cells (Treg cells).

A compound of formula I

##STR00001##

or a pharmaceutical salt thereof of formula II,

##STR00002##

as well as a process to obtain said compound and a process to obtain said salt. Additionally, disclosed is the use of said compound of formula I or said pharmaceutical salt thereof of formula II as a medicament, in particular as a peroxisome proliferator-activated receptor gamma (PPARγ) agonist, for use in the treatment or prevention of a disease responsive to PPARγ agonists. Also disclosed is a pharmaceutical composition comprising said compound or said salt, as well as a method of treating or preventing a disease with said compound of formula I or said salt thereof of formula II, or with a composition comprising said compound or said salt.

The present invention relates to the technical field of medicine, and to derivatives represented by formula 1 and formula 2 in which a carboxylic acid group is introduced into the structure of Ginkgolide B by means of a hydroxyl group at the 10-position and ester derivatives of carboxylic acid groups, and pharmaceutically acceptable organic or inorganic salts. Ginkgolide B is used as a parent body and is prepared by means of chemical structure modification so as to achieve the goals of improving solubility, increasing bioavailability and enhancing healing efficacy. The prepared compound and carboxylate salts thereof have significant platelet activating factor antagonism, an anticoagulant effect and an anti-acute cerebral ischemia effect, and can be used for preparing a drug for preventing and treating ischemic stroke, thrombosis, angina pectoris, cardiopulmonary infarction, as well as inflammation, asthma and other diseases related to a platelet activating factor.

##STR00001##

This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. ##STR00001##
wherein: X is C or N with the proviso that when X is N, R.sup.1 does not exist; W is C or N with the proviso that when W is N, R.sup.2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of ##STR00002## Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. ##STR00003##
wherein: L and M are independently selected from the group consisting of C.sub.1-C.sub.6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.

This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. ##STR00001##
wherein: X is C or N with the proviso that when X is N, R.sup.1 does not exist; W is C or N with the proviso that when W is N, R.sup.2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of ##STR00002## Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. ##STR00003##
wherein: L and M are independently selected from the group consisting of C.sub.1-C.sub.6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.

Compounds are provided having the following structure: Formula (I) or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R, R.sup.1, R.sup.2, G.sup.1, G.sup.2 and n are as defined herein. Use of the compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, compositions comprising the compounds and methods for their use and preparation are also provided. ##STR00001##

A compound of formula (I) or a salt thereof are provided: ##STR00001##
wherein R.sup.1, X and R.sup.3 are defined in the specification, useful in the treatment of disorders mediated by KMO such as acute pancreatitis, chronic kidney disease, other conditions associated with systemic inflammatory response syndrome (SIRS), Huntington's disease, Alzheimer's disease, spinocerebellar ataxias, Parkinson's disease, AIDS-dementia complex, amylotrophic lateral sclerosis (ALS), depression, schizophrenia, sepsis, cardiovascular shock, severe trauma, acute lung injury, acute respiratory distress syndrome, acute cholecystitis, severe burns, pneumonia, extensive surgical procedures, ischemic bowel, severe acute hepatic disease, severe acute hepatic encephalopathy or acute renal failure.