The present invention relates to a process for preparing B-[(7?, 17?)-17-hydroxy-7-[9-[(4,4,5,5,5-pentafluoropentyl)sulfi nyl]estra-1, 3, 5(10)-trien-3-yl]-boronic acid, known as Fulvestrant-3-boronic acid or ZB716, whose structure is reported below: Formula (I) ZB716

##STR00001##

The invention relates inter alia to methods of producing sulfated oligosaccharide derivatives and intermediates thereof. The sulfated oligosaccharide derivatives may be represented by the following formula (I):

[X].sub.nY?ZR.sup.1R.sup.2Formula (I)

wherein: X and Y are any D- or L-hexose or pentose, wherein each hydroxyl group not involved in a glycosidic linkage is substituted by a group W, and Y has an anomeric carbon atom; W is SO.sub.3M, and M is any pharmaceutically acceptable cation; n is an integer from 2 to 6; Z is O, and is linked to the anomeric carbon atom of Y; and R.sup.1R.sup.2 together form a lipophilic moiety.

Described herein are new anti-cancer compounds and methods of using such compounds, acting through a new mechanism of action by simultaneous inhibition of leukemia inhibitory factor (LIF) and MDM2.

5-cholesten, 3, 25-diol, disulfate (25HCDS) has been found to be an authentic PPAR.sub. agonist and LXR antagonist, and is used for the therapy of lipid disorders and inflammatory diseases, including without limitation fatty liver, inflammatory bowel, and atherosclerotic diseases.

Methods and compositions are provided for the treatment of familial exudative vitreoretinopathy (FEVR) through the administration of a therapeutically effective amount of a sphingosine-1-phosphate receptor type 2 (S1PR2) antagonist. Also provided herein are compounds which contain bioisosteric replacements of the urea group of JTE-013 and analogs thereof, and their use in treating retinopathies and diseases characterized by insufficient angiogenesis.

The present invention relates to compounds and their uses, in particular, compounds in the form of prodrugs that promote transport of a pharmaceutical agent to the lymphatic system and subsequently enhance release of the parent drug.

The present invention relates to compounds and their uses, in particular, compounds in the form of prodrugs that promote transport of a pharmaceutical agent to the lymphatic system and subsequently enhance release of the parent drug.

Disclosed are inhibitors of the farnesoid X receptor, for example of formula (I), wherein R.sup.1, R.sup.2, R.sup.4, X, Y, Z, m, and n are as defined herein, which are useful in treating or preventing obesity, type 2 diabetes/insulin resistance and non-alcoholic fatty liver disease in a mammal in need thereof. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the invention, a method of method of inhibiting a farnesoid X receptor in a mammal, and a method of treating or preventing obesity in a mammal. ##STR00001##

The present disclosure relates to synthetic methods for preparing a 9-alpha-substituted or a 9-beta-substituted steroid-like compound. In particular, the disclosure relates to methods for generating a steroidal C9-C10 bond and establishing stereochemistry at C9 in such compounds. The methods provide high levels of stereoselection in the C9-C10 bond forming process. Compounds synthesized by such methods can be used as nuclear hormone receptor modulators.

The invention relates to an antagonist of CB1 receptor for use in the treatment of a pathologic condition or disorder selected from the group consisting of bladder and gastrointestinal disorders; inflammatory diseases; cardiovascular diseases; nephropathies; glaucoma; spasticity; cancer; osteoporosis; metabolic disorders; obesity; addiction, dependence, abuse and relapse related disorders; psychiatric and neurological disorders; neurodegenerative disorders; autoimmune hepatitis and encephalitis; pain; reproductive disorders and skin inflammatory and fibrotic diseases.