Patent classifications
A61P15/16
Non-hormonal compositions and methods for male contraception
The present invention relates to non-hormonal compositions and methods for inducing a condition of aspermia, azoospermia, or severe oligozoospermia in the male subject such that these compositions and methods for administering the same may be used as male contraception. Embodiments of the present invention may comprise a composition comprising an alpha-1-adrenoreceptor antagonist, such as (R)-silodosin, for daily administration to a male subject. The compositions and related methods may further include pharmaceutically acceptable carriers. The present invention further includes formulations which allow for a delay such that delayed or missed dose(s) do not nullify the contraceptive effect of the treatment regimen. Such compositions and methods may also avoid the side effects associated with typical formulations of alpha-1-adrenoreceptor antagonists.
Non-hormonal compositions and methods for male contraception
The present invention relates to non-hormonal compositions and methods for inducing a condition of aspermia, azoospermia, or severe oligozoospermia in the male subject such that these compositions and methods for administering the same may be used as male contraception. Embodiments of the present invention may comprise a composition comprising an alpha-1-adrenoreceptor antagonist, such as (R)-silodosin, for daily administration to a male subject. The compositions and related methods may further include pharmaceutically acceptable carriers. The present invention further includes formulations which allow for a delay such that delayed or missed dose(s) do not nullify the contraceptive effect of the treatment regimen. Such compositions and methods may also avoid the side effects associated with typical formulations of alpha-1-adrenoreceptor antagonists.
Acetamide thienotriazolodiazepines and uses thereof
The present invention provides compounds of Formula (I), and pharmaceutically compositions thereof. Compounds of Formula (I) are binders of bromodomains and/or bromodomain-containing proteins (e.g., bromo and extra terminal (BET) proteins). Also provided are methods, uses, and kits using the compounds and pharmaceutical compositions for inhibiting the activity (e.g., increased activity) of bromodomains and/or bromodomain containing proteins and for treating and/or preventing in a subject diseases associated with bromodomains or bromodomain-containing proteins (e.g., proliferative diseases, cardiovascular diseases, viral infections, fibrotic diseases, metabolic diseases, endocrine diseases, and radiation poisoning). The compounds, pharmaceutical compositions, and kits are also useful for male contraception. ##STR00001##
SALT OF FUSED HETEROCYCLIC DERIVATIVE AND CRYSTAL THEREOF
The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyl-oxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid choline salt having excellent solubility and storage stability.
TETRAHYDROQUINOLINE COMPOSITIONS AS BET BROMODOMAIN INHIBITORS
The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula I:
##STR00001##
wherein W, X, Y, Z, R.sup.1, R.sup.2, R.sup.5, and R.sup.8 are as described herein.
SELECTIVE ANDROGEN RECEPTOR MODULATORS (SARMS) AND USES THEREOF
Provided herein are compounds that bind to androgen receptors and/or modulate activity of androgen receptors. Also provided are methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.
METHODS FOR IMPLANTING AND REVERSING STIMULI-RESPONSIVE IMPLANTS
Described are methods for reversible occlusion of a body lumen by way of degradation as a result of exposure to one or more stimuli such as light. The methods include administering one or more substance(s) into a body lumen of a subject and forming a stimuli-responsive polymer mass in the body lumen from the one or more substance(s). The mass is sufficient to occlude the body lumen in a manner that prevents transport of at least one material through the body lumen and is susceptible to on-command reversal in the body lumen upon exposure to one or more stimuli. The methods include administering one or more stimuli to a polymer mass in a body lumen for a time and intensity to cause the reverse the polymer mass. The methods are particular useful for applications in which it is desirable to temporarily occlude a body lumen, such as male and female contraception.
DENDRITIC CELLS-TARGETING VACCINE
The present disclosure relates to recombinant single chain fragment variable (ScFv) binding to DEC-205 of dendritic cells having amino acid sequence selected from a group consisting of SEQ ID NO: 1, SEQ ID NO: 2, SEQ ID NO: 3, SEQ ID NO: 4, SEQ ID NO: 5, SEQ ID NO: 6, SEQ ID NO: 7, SEQ ID NO: 8, and SEQ ID NO: 9. Also disclosed are ScFv-antigen complex, a method for inducing immune response in a subject using the ScFv-antigen complex and a vaccine composition comprising the ScFv-antigen complex. The ScFv-antigen complex as disclosed herein can be used as immuno-contraceptives for mammals.
Compositions and Methods for Ablating Niche Cells in Testis and Other Epithelial Cells and Methods Relating Thereto
The present disclosure relates to compositions and methods for ablating epithelial cells, in particular to methods for ablating Sertoli cells in testis, and methods related thereto. In particular, the present disclosure relates to methods for ablating Sertoli and other cells in the testis using benzalkonium chloride, to methods for rescuing endogenous spermatogenesis in a subject suffering from Sertoli cell dysfunction, to methods of reconstructing spermatogenesis, to methods of treating infertility, and to methods for the selective depletion of epithelial cells in a tissue and for the treatment of diseases or disorders associated with damaged epithelial cells.
Uses of diazepane derivatives
The present invention provides compounds of Formula (II) (e.g., compounds of Formula (I)), and pharmaceutically compositions thereof. Compounds of Formula (II) are believed to be binders of bromodomains and/or bromodomain-containing proteins (e.g., bromo and extra terminal (BET) proteins). Also provided are methods, uses, and kits using the compounds and pharmaceutical compositions for inhibiting the activity (e.g., increased activity) of bromodomains and/or bromodomain-containing proteins and for treating and/or preventing in a subject diseases associated with bromodomains or bromodomain-containing proteins (e.g., proliferative diseases, cardiovascular diseases, viral infections, fibrotic diseases, metabolic diseases, endocrine diseases, and radiation poisoning). The compounds, pharmaceutical compositions, and kits are also useful for male contraception. ##STR00001##