C07J41/0044

NEUROACTIVE STEROIDS AND THEIR METHODS OF USE

Provided herein is a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R.sup.19, R.sup.5, R.sup.3a, R.sup.1a, R.sup.1b, R.sup.2a, R.sup.2b, R.sup.4a, R.sup.4b, R.sup.6a, R.sup.6b, R.sup.7a, R.sup.7b, R.sup.11a, R.sup.11b, R.sup.12a, R.sup.12b, R.sup.18, R.sup.D, and q are defined herein. L is selected from the group consisting of: wherein A indicates the point of attachment at C17 and wherein X is selected from the group consisting of —C(0)N(R.sup.55a)(R.sup.55b), —N(R.sup.55a)(R.sup.55b), —N(R.sup.55b)C(O)(R.sup.55a), and R.sup.55C wherein R.sup.55c is carbon-bound substituted or unsubstituted heteroaryl or substituted or unsubstituted aryl. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.

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MONOMERIC AND OLIGOMERIC COMPOUND EMBODIMENTS AS CONTRACEPTIVES AND THERAPIES AND METHODS OF MAKING AND USING THE SAME

Disclosed herein are monomeric and oligomeric compound embodiments for use as contraceptive agents. Monomeric compound embodiments disclosed herein comprise substituents that facilitate the ability of the compounds to exhibit progestogenic, androgenic, and estrogenic activity, which can prevent or inhibit bone density loss in subjects. Oligomeric compound embodiments disclosed herein provide the ability to control receptor activation and/or treatment by incorporating a tunable linker group which couples steroidal-based compounds to one another or with therapeutic agents and facilitates selective cleavage of the monomeric components of the oligomeric compound.

Hydroxysteroid compounds, their intermediates, process of preparation, composition and uses thereof

The present invention relates to novel steroidal compounds of formula (I), process for preparation of the same and composition comprising these compounds. ##STR00001##

Tripartite Androgen Receptor Eliminators, Methods and Uses Thereof
20230092979 · 2023-03-23 · ·

The present specification discloses tripartite androgen receptor eliminators (AREs), pharmaceutical compositions and medicaments comprising such AREs, methods and uses for such AREs and compositions and medicaments, and methods and uses for AREs and compositions and medicaments for treating an androgen receptor signaling-mediated condition, disease or disorder.

COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS

Provided herein is a compound of Formula (1-I): or a pharmaceutically acceptable salt thereof, wherein R.sup.2a, R.sup.2b, R.sup.3, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6a, R.sup.6b, R.sup.11a, R.sup.11b, R.sup.16a, R.sup.16b, R.sup.19, R.sup.18, X, q, r, s, t, u, and n are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (1-I) and methods of using the compounds, e.g, in the treatment of CNS-related disorders.

##STR00001##

Steroid derivative regulators, method for preparing the same, and uses thereof

Steroid derivative regulators, a method for preparing the same, and uses thereof are described. Specifically, a compound as shown in formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and uses thereof as a regulator of GABA .sub.A receptor for treating depression, convulsion, Parkinson's disease, and nervous system diseases are described, wherein the substituents of the formula (I) are as defined in the description. ##STR00001##

Therapeutically active steroidal derivatives

The invention relates to compounds of formula (II), ##STR00001##
and pharmaceutically acceptable salts thereof,
wherein R1 to R4 are as defined in the claims. The invention further relates to their use as inhibitors of 17β-HSD1 and in treatment or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17β-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. The present invention also relates to the preparation of the aforementioned compounds and pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds or pharmaceutically acceptable salts thereof.

COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS

Described herein are neuroactive steroids of the Formula (I):

##STR00001##

or a pharmaceutically acceptable salt thereof; wherein custom-character, A, R.sup.1, R.sup.2, and R.sup.3 are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use, e.g., for treating a subject suffering from a disease or disorder described herein.

Prodrug and profluorescent compounds for selective mitochondrial imaging and therapeutic targeting

The present invention relates to the use of prodrugs susceptible to nitroreductase (NTR) activation. In particular, provided herein are mitochondria-targeting prodrug compounds and probes, including profluorescent near-infrared (NIR) probes and non-fluorescent prodrugs, as well as to methods of using said prodrug compounds and probes for imaging mitochondria and for mitochondria-specific delivery of therapeutic agents.

3ALPHA, 5BETA-NEUROACTIVE STEROIDS FOR THE TREATMENT OF EPILEPSY AND SEIZURE DISEASES

3α5β-steroid compounds of general formula I is disclosed. These compounds are useful in the treatment of epilepsy or comorbidities associated with epilepsy or conditions associated with convulsions, such as seizures associated with hypoxia, seizures associated with traumatic brain damage, seizures associated with intoxication, pathological changes caused by hyperexcitation, or in treatment of conditions accompanying epilepsy, such as affective disorders, depression, post-traumatic stress disorder (PTSD) and stress-related diseases, anxiety, schizophrenia and psychotic disorders, related ischemic CNS damage, neurodegenerative changes and disorders, multiple sclerosis. The compounds of general formula I also show age-specific efficacy.