Bismethylene-17A carbolactones and related uses
AssigneeEverstra, Inc.
InventorsKlaus Nickisch, Pemmaranu N. Rao, James W. Cessac, Anne Marie Simmons
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Abstract
Described herein are bismethylene-17α carbolactone derivatives having progestational and/or antimineralocorticoid and/or aldosterone antagonistic activity. Also described herein are methods of preparing and using these novel compounds.
Claims25
An antimineralocorticoid compound having the structure of formula (I):
- where:
- R1 is H or CH3;
- R2 is CH3 or CH2CH3;
- R3 and R4 are hydrogens;
- together form an α-CH2 bridge between carbons 15 and 16;
- or together form a β-CH2 bridge between carbons 15 and 16;
- and
- R5 and R6 together form an α-CH2 bridge between carbons 6 and 7 or a β-CH2 bridge between carbons 6 and 7.
A progestogen compound having the structure of formula (II):
- where:
- R3 and R4 together form an α-CH2 bridge between carbons 15 and 16 or a β-CH2 bridge between carbons 15 and 16;
- and
- R7 and R8 together form an α-CH2 bridge between carbons 1 and 2.
An oral dosage form comprising a progestogen compound and one or more pharmaceutically acceptable carriers suitable for oral delivery of the progestogen compound, the progestogen compound having the structure of formula (II):
- where:
- R3 and R4 together form an α-CH2 bridge between carbons 15 and 16 or a β-CH2 bridge between carbons 15 and 16;
- and
- R7 and R8 together form an α-CH2 bridge between carbons 1 and 2.
A method of producing a contraception comprising administering to a subject an effective amount of a progestogen compound, the progestogen compound having the structure of formula (II):
- where:
- R3 and R4 together form an α-CH2 bridge between carbons 15 and 16 or a β-CH2 bridge between carbons 15 and 16;
- and
- R7 and R8 together form an α-CH2 bridge between carbons 1 and 2.
Dependencies are inferred from the claim text.