Abstract:
Tetrahydroquinoline derivatives of general formula (I) or salts thereof, having a specific and strong binding affinity for AR and exhibiting AR agonism or antagonism; and drug compositions containing the derivatives or the salts.
Abstract:
The invention provides chimeric molecules that are catalytic antagonists of a target molecule. The catalytic antagonists of this invention preferably comprise a targeting moiety attached to an enzyme that degrades the molecule specifically bound by the targeting moiety. The catalytic antagonists of this invention thus bind to a target recognized by the targeting moiety (e.g., a receptor) the enzyme component of the chimera then degrades all or part of the target. This typically results in a reduction or loss of activity of the target and release of the chimeric molecule. The chimeric molecule is then free to attack and degrade another target molecule.
Abstract:
Disclosed is a pharmaceutical formulation in the form of a capsule for oral administration comprising testosterone undecanoate as an active ingredient dissolved in a pharmaceutically acceptable liquid carrier, characterised in that the liquid carrier comprises at least 50 % by weight of castor oil. The choice of castor oil as the liquid carrier, in conjunction with the choice of testosterone undecanoate as the androgen, makes for a solution which can comprise about 200-250 mg/ml of TU. This is a novel achievement for any orally administerable solution of testosterone. The solution may also contain a lipophilic surfactant such as lauroglycol.
Abstract translation:公开了用于口服给药的胶囊形式的药物制剂,其包含溶解在药学上可接受的液体载体中的作为活性成分的十一酸睾酮,其特征在于,所述液体载体包含至少50重量%的蓖麻油。 作为液体载体的蓖麻油的选择,结合选择作为雄激素的十一酸睾酮,可以制备可包含约200-250mg / ml TU的溶液。 这是任何可口服给药的睾酮溶液的新成就。 该溶液还可以含有亲脂性表面活性剂,如青霉烯。
Abstract:
The invention deals with the transport of preferably large molecules across nasal mucosa by means of specially designed, highly adaptable carriers loaded with said molecules. One of the purposes of making such formulations is to achieve non-invasive systemic delivery of therapeutic polypeptides, proteins and other macromolecules; the other intent is to overcome circumstantially the blood-brain barrier by exploiting the nasal cavity to enter the body and then to get access to the brain. A third intent is to achieve successful protective or tolerogenic immunisation via nasal antigen or allergen administration.
Abstract:
A pharmaceutical composition for adapted for oral administration comprising at least 10 % w/w native testosterone, at least 36% w/w sesame oil, at least 28% w/w propylene glycol monolaurate, at least 9 % w/w ethanol and at least 14 % w/w benzyl alcohol. A dosage regimen for use in a human subject comprising administering at least a first and a second pharmaceutical compositions wherein, the first composition comprises between 2.5-7.5 % w/w native testosterone, sesame oil, propylene glycol monolaurate, ethanol and benzyl alcohol; and the second composition comprises at least 9% w/w native testosterone, sesame oil, propylene glycol monolaurate, ethanol and benzyl alcohol; wherein said first and second compositions are administered orally at least once in a 24- hour period to said human subject to normalise serum testosterone. A process to produce a composition comprising native testosterone comprising i) forming a homogeneous preparation comprising sesame oil, propylene glycol monolaurate, benzyl alcohol and ethanol; ii) adding native testosterone at a concentration of about 13% w/w to said homogeneous preparation to form a combined testosterone preparation; and iii) mixing the combined preparation to dissolve testosterone to form a substantially clear preparation.
Abstract:
The present disclosure concerns peptide compounds of formula (I) or (II) and combinations thereof that can be administered orally for promoting endogenous steroid, and particularly testosterone, production: A-Xaa 1 Xaa 2 -Xaa 3 -Xaa 4 -Xaa 5 -Xaa 6 -Xaa 7 -Xaa 8 -B (I) A-Xaa 1 -Xaa A -Xaa B -Xaa 2 -Xaa 3 -Xaa 4 -Xaa 5 -Xaa 6 -Xaa 7 -Xaa C -Xaa D -Xaa E -Xaa 8 -B (II)
Abstract:
A therapeutically effective amount of a combination of: (a) an inhibitor of CYP11B1; and (b) ACAT1 inhibitor N-(2,6-bis(l-methylethyl) phenyl)-N'-((l-(4-(dimethylamino)phenyl)cyclopentyl)-methyl) urea (ATR-101) or a salt thereof; or (a) an inhibitor of CYP11B1; (b) an inhibitor of CYP11B2; and (c) ACAT1 inhibitor N-(2,6-bis(1-methylethyl)phenyl)-N'-((1-(4-(dimethyl-lamino)phenyl)cyclopentyl) -methyl)urea or a salt thereof for use in a method for the treatment of disorders associated with excess Cortisol production, including treatment of Cushing's syndrome.
Abstract:
. Novel methods of improving or enhancing psychological, somatic, and sexual conditions in an aging male human subject, by administering fenugreek or fenugreek seeds, or an extract of fenugreek or fenugreek seeds, are described. Novel methods of reducing symptom severity of andropause, improving sexual functions, preventing further decline of sexual hormones, and/or improving sexual hormonal level in an aging male human subject, by administering fenugreek or fenugreek seeds, or an extract of fenugreek or fenugreek seeds, are also described.