Estrene steroids as neurochemical initiators of change in human hypothalamic function and related pharmaceutical compositions
AssigneePherin Corporation
InventorsDavid L. Berliner, Nathan William Adams, Clive L. Jennings-White
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Abstract
The invention relates to a method of altering hypothalamic function in an individual. The method comprises nasally administering a human semiochemical, e.g. an Estrene steroid, or a pharmaceutical composition containing an Estrene steroid, such that the ligand semiochemical binds to a specific neuroepithelial receptor. The steroid is preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers. Other embodiments of the invention include pharmaceutical compositions containing the steroids.
Claims10
A pharmaceutical composition in a dosage unit form adapted for nasal administration in a human subject, said composition comprising per dosage unit, an effective amount of an Estrene steroid in a range to effect the nervous system through the vomeronasal organ but ineffective to have a systemic effect by absorption into the circulatory system and a pharmaceutically acceptable carrier, wherein said Estrene steroid has the formula ##STR73## wherein R.sub.1 is selected from the group consisting of one or two hydrogen atoms, methyl, methylene, and one or two halo atoms;
- R.sub.2 is absent or is selected from the group consisting of hydrogen and methyl;
- R.sub.3 is selected from the group consisting of oxo, hydroxy, lower alkoxy, lower acyloxy, benzoyl, cypionyl, glucouronide and sulfonyl;
- R.sub.4 is selected from the group consisting of hydrogen, hydroxy, lower alkoxy, lower acyloxy and halo;
- R.sub.5 is absent or is selected from the group consisting of hydrogen, hydroxy, lower alkoxy and lower acyloxy;
- R.sub.6 is a hydrogen or a halo;
- and "a" represents optional aromatic unsaturation of ring A of said steroid, or "b", "c", and "d" are each optional double bonds;
- and "e", "f", "g", "h", "i" and "j" are each optional double bonds;
- wherein:
- "h" and "i" are both double bonds;
- or "j" is a double bond;
- or "c" and "d" are double bonds;
- or "f" is a double bond.
A pharmaceutical composition in dosage unit form adapted for nasal administration in a human subject, said composition comprising per dosage unit, an effective amount of an Estrene steroid in a range to effect the nervous system through the vomeronasal organ but ineffective to have a systemic effect by absorption into the circulatory system and a pharmaceutically acceptable carrier, wherein said Estrene steroid is selected from the group consisting of Estra-1,3,5(10)-trien-3-ol;
- Estra-1,3,5(10),6-tetraen-3-ol;
- Estra-1,3,5(10),7-tetraen-3-ol;
- and 17-Methylene-estra-1,3,5(10),6,8(9)-hexaen-3-ol.
A pharmaceutical composition in a dosage unit form adapted for nasal administration in a human subject, said composition comprising per dosage unit, an effective amount of an Estrene steroid in a range to effect the nervous system through the vomeronasal organ but ineffective to have a systemic effect by absorption into the circulatory system and a pharmaceutically acceptable carrier, wherein said Estrene steroid has the formula:
- ##STR74## wherein R.sub.1 is selected from the group consisting of one or two hydrogen atoms, methyl, methylene, and one or two halo atoms;
- R.sub.2 is absent or is selected from the group consisting of hydrogen and methyl;
- R.sub.3 is selected from the group consisting of oxo, hydroxy, lower alkoxy, lower acyloxy, benzoyl, cypionyl, glucouronide and sulfonyl;
- R.sub.4 is selected from the group consisting of hydrogen, hydroxy, lower alkoxy, lower acyloxy and halo;
- R.sub.5 is absent or is selected from the group consisting of hydrogen, hydroxy, lower alkoxy and lower acyloxy;
- R.sub.6 is a hydrogen or a halo;
- and "a" represents optional aromatic unsaturation of ring A of said steroid, or "b", "c", and "d" are each optional double bonds;
- and "e", "f", "g", "h", "i" and "j" are each optional double bonds;
- wherein R.sub.1 is methylene or a single hydrogen.
Dependencies are inferred from the claim text.