This invention discloses method for preparing a non-radioactive standard β-CFT. Using cocaine hydrochloride as the starting material, and after a series of hydrolysis, dehydration, esterification and bonding reactions, a non-radioactive standard (2β-Carbomethoxy-3β-(4-fluoropenyl) tropane) is prepared. Furthermore, this preparation method has fewer steps, is easy to operate, and the purity of the product is as high as 97.97%. Therefore, the method for preparing a non-radioactive standard β-CFT can promote the development of positron imaging in the diagnosis of Parkinson's disease.

Compounds of Formula 1 and pharmaceutically acceptable compositions thereof are useful as TLR7/8 antagonists.

The invention provides methods for treating or preventing a condition mediated by the farnesoid X receptor (FXR), comprising administering tropifexor, a pharmaceutically acceptable salt, an amino acid conjugate or an acyl glucuronide conjugate thereof, at a dose of about 140 μg to about 250 μg, to a subject in need thereof.

Disclosed are compounds of Formula (I) or a salt thereof, wherein R.sub.1, R.sub.3, R.sub.4, R.sub.5, m, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases. ##STR00001##

Disclosed are compounds of Formula (I) or a salt thereof, wherein R.sub.1, R.sub.3, R.sub.4, R.sub.5, m, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases. ##STR00001##

The present invention relates to an improved synthesis of N-monofluoroalkyl tropanes using fluoroalkyl iodide. The invention also provides the use of such method to prepare the non-radioactive tropane intermediate FP-CIT, and its subsequent conversion to the .sup.123I-labelled radiopharmaceutical DaTSCAN™ (.sup.123I-ioflupane). Also provided is the use of fluoroalkyl iodide in the alkylation method of the invention.

The present invention relates to an improved synthesis of N-monofluoroalkyl tropanes using fluoroalkyl iodide. The invention also provides the use of such method to prepare the non-radioactive tropane intermediate FP-CIT, and its subsequent conversion to the .sup.123I-labelled radiopharmaceutical DaTSCAN™ (.sup.123I-ioflupane). Also provided is the use of fluoroalkyl iodide in the alkylation method of the invention.

Compounds of formula (I)

##STR00001##

wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.23, R.sub.24, L, A and B are as defined in claim 1, or pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as cytochrome P450 monooxygenase 11A1 (CYP11A1) inhibitors. The compounds are useful as medicaments in the treatment of steroid receptor, particularly androgen receptor, dependent diseases and conditions, such as prostate cancer.

Compounds of formula (I)

##STR00001##

wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.23, R.sub.24, L, A and B are as defined in claim 1, or pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as cytochrome P450 monooxygenase 11A1 (CYP11A1) inhibitors. The compounds are useful as medicaments in the treatment of steroid receptor, particularly androgen receptor, dependent diseases and conditions, such as prostate cancer.

The invention related to compounds of formula (I), ##STR00001##
and pharmaceutically acceptable salts thereof, wherein R.sup.1 to R.sup.2, A, Y and L are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.