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N-bridged selective androgen receptor modulators and methods of use thereof
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An androgen receptor and selective technology, applied in diseases, pharmaceutical formulations, organic active ingredients, etc., can solve problems such as easy damage, weakened physical condition, and harmful personal health
Inactive Publication Date: 2008-12-31
UNIV OF TENNESSEE RES FOUND
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For example, changes that occur during sarcoid wasting can result in a weakened physical condition that is detrimental to the individual's health, leading to increased susceptibility to infection, poor performance status, and vulnerability to injury
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[0258] The preparation of pharmaceutical compositions containing active ingredients is known in the art. Typically, such compositions are formulated as polypeptide aerosols for administration to the nasopharynx, or as injectable solutions or suspensions. However, solid forms suitable for solution in, or suspension in, liquid prior to injection can also be prepared. The formulation may also be emulsified. The active therapeutic ingredient is usually mixed with excipients which are pharmaceutically acceptable and compatible with the active ingredient. Suitable excipients are, for example, water, saline, dextrose, glycerol, ethanol, etc. or combinations thereof.
[0259] In addition, the composition can contain minor amounts of auxiliary substances, such as wetting or emulsifying agents, pH buffering agents, which enhance the effectiveness of the active ingredients.
[0260] The active ingredients can be formulated into compositions in the form of neutral pharmaceutically acce...
Embodiment 1
[0267] Synthesis of N-bridged selective androgen modulator compounds
[0269] According to route 1 ( figure 1 ) to synthesize the N-bridged selective androgen modulator compound (SARM) of the present invention. First, the synthesis was carried out in two separate steps—isolating the epoxide (S)-5 and then opening the epoxide. These steps were combined into a two-step one-pot process, where after epoxide formation, the solvent was removed and the resulting residue was immediately subjected to an opening step. The first step proceeded cleanly and completely to the epoxide by TLC. The epoxide is opened with the appropriate substituted aniline in hexafluoroisopropanol. Aromatic amines are extremely non-nucleophilic; therefore the epoxide must be formed and opened in the presence of hexafluoroisopropanol, which increases the electrophilicity of the epoxide.
[0276] Using a competitive bindingassay as previously described (Kirkovsky, L. et al., Chiralnonsteroidal affinity ligands for tbe androgen receptor. Bicalutamide analogues bearing electrophilic groups in the B aromatic ring. J. Med. Chem. 2000, 43, 581-590 ) to determine AR binding affinity. Briefly, AR binding studies were performed as follows: increasing concentrations (10 -3 nM to 10000nM) of each ligand and cytosol, and the saturating concentration 3 H-Mibobolone (MIB) (1 nm) was incubated together at 4°C for 18 hours. The incubation also contained 1000 nM triamcinolone acetonide to block the interaction of MIB with the progesterone receptor. To determine non-specific binding, a separate experiment was performed by adding 1000 nM MIB to the incubation. Separation of bound and free radioactivity was achieved at the end of the incubation by the hydroxyapatit...
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[0001] This application is a divisional application of the Chinese patent application 03819545.3 with the title of "N-bridged selective androgen receptor modulator and its use" submitted on June 17, 2003. technical field [0002] The present invention relates to a new class of androgen receptor targeting agents (ARTAs) which exhibit androgenic and anabolic activity of non-steroidal ligands of the androgen receptor. This agent defines a new subclass of compounds, which are selective androgen receptor modulators (SARMs), for a) male contraception; b) treatment of a variety of hormone-related conditions, such as those associated with decreased androgen in aging men ( ADAM) related disorders; c) treatment of female androgen-decreased (ADIF) related disorders; d) treatment and / or prevention of acute and / or chronic musclewasting; e) prevention and / or treatment of dry eye; f) oral androgen replacement therapy; and / or g) reducing the incidence of prostatecancer, preventing prostate ...
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