Modulators of sperm hypermotility and uses thereof
Inventors
Chong, Jayhong A. • Moran, Magdalene M.
Assignees
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Publication Number
US-9732050-B2
Publication Date
2017-08-15
Expiration Date
Abstract
The invention provides novel compositions and compounds that inhibit CatSper channel activity, that preferentially inhibits sperm hyperactivity over sperm motility, or both. The compounds of the invention are useful as contraceptive agents that may be adminstered to males, females, or concurrently to both sexual partners. The invention further provides methods of conducting drug discovery business and of conducting a reproductive medicine business. The invention also provides methods of identifying compounds that modulate sperm hypermotility.
Core Innovation
The invention relates to a birth control device that combines a condom with a compound represented by a formula having variable substituents W, X, Y, and R, and pharmaceutically acceptable salts. The disclosure includes specific structural options corresponding to the defined variables and selected illustrated compound structures.
The described compound class is used with the condom as a contraceptive component, and the disclosure further describes compound formulations for condoms and associated compositions, including lubricants and creams. It is also described as a control agent in sperm assays and as a contraceptive approach by modulating CatSper1 activity, including effects on Ca2+ influx and Ca2+ currents, and by selectively reducing sperm hyperactivation.
The disclosure further states that the approach can decrease CatSper1 activity while preserving motility and viability, and that it provides broader fertility reduction and contraceptive methods for male and female fertility. It describes competitive binding with CatSper1-binding agents, coadministration with other contraceptives, and reversible effects on infertility.
Claims Coverage
The independent claim coverage centers on a condom-based birth control device that includes a compound defined by a substituent-variable chemical formula, or pharmaceutically acceptable salts. Dependent claim information refines this by specifying particular values for W, X, and/or Y, optionally including specified functional ingredient types, and allowing selection from illustrated compound structures.
Condom with formula-defined compound
A birth control device comprising a condom and a compound represented by a formula wherein W is CR′ or N (R′ is a lower alkyl or a hydrogen), X is O or S, Y (independently for each occurrence) is C–O, C–S, or SO2, and R (independently for each occurrence) is alkyl, alkenyl, alkynyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aralkyl, heteroaralkyl, carbocyclylalkyl, or heterocyclylalkyl, or a pharmaceutically acceptable salt of said compound.
Narrowed W variable set to N
The birth control device of the formula-defined compound characterized by W equals N.
Narrowed X variable set to O
The birth control device of the formula-defined compound characterized by X equals O.
Constrained Y variable as C–O
The birth control device of the formula-defined compound wherein Y, independently for each occurrence, is C–O.
Functional ingredient types within the compound
A birth control device wherein the compound comprises one or more of a lubricant, a warming composition, a spermicidal agent, a desensitizer, or an erectogenic composition.
Selected illustrated compound structures or salts
A birth control device defined by including a compound selected from the illustrated structures or a pharmaceutically acceptable salt thereof.
Overall, the claim coverage centers on a condom-based birth control device that includes a compound defined by a substituent-variable chemical formula, or pharmaceutically acceptable salts, with dependent refinements that specify particular values for W, X, and/or Y, optionally include specified functional ingredient types, and allow selection from illustrated compound structures.
Stated Advantages
Preferentially suppress sperm hyperactivity and/or CatSper1 activity and Ca2+ influx while suppressing sperm motility and/or viability to a lesser extent, supporting reversible contraception.
CatSper1 is sperm-specific, and knockout leads to male sterility, supporting tissue selectivity and reduced side effects.
Selectively reduces sperm hyperactivity while decreasing CatSper1 activity and Ca2+ influx/Ca2+ currents.
Decreases CatSper1 activity while preserving sperm motility and viability.
Provides reversible infertility effects.
Documented Applications
A birth control device comprising a condom and a compound represented by the formula, including pharmaceutically acceptable salts.
Decreasing fertility in males and females, including contraception and joint fertility reduction.
Pharmaceutical compositions and dosage forms including injectables, transdermal patches, implants, and topical formats, as well as condom and birth-control device formats.
Screening and identifying compounds that inhibit or promote sperm hyperactivation via CatSper channel activity.
Using CatSper1/CatSper modulators as inhibitors/antagonists for sperm hyperactivity and Ca2+ influx suppression for reversible contraception.
Use in sperm assays as a control agent, including sperm motility/hyperactivation screening assays.
Fertility reduction and contraceptive methods for males and females using the disclosed compound class and multiple administration routes.
Drug discovery business methods involving screening workflows and assays related to sperm motility/hyperactivation.
Competitive binding context with CatSper1-binding agents and coadministration with other contraceptives.
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