C07J21/00

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, R.sup.3a, R.sup.4a, R.sup.4b, R.sup.5, R.sup.7a, and R.sup.7b 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 and treatment, e.g., such for inducing sedation and/or anesthesia.

Neuroactive steroids and compositions thereof

Provided herein is a compound of Formula (I): ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R.sup.1a, R.sup.1b, 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.7a, R.sup.7a, R.sup.11a, R.sup.11b, R.sup.12a, R.sup.12b, R.sup.16a, R.sup.16b, R.sup.19, R.sup.11a, R.sup.22, R.sup.X, R.sup.Y and n are defined herein. 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.

Combination of estrogens plus antiprogestins with significant partial agonistic effect as an effective treatment of menopausal symptoms and for prevention of the occurrence of breast cancer

Described herein are compositions and methods for hormone replacement therapy that address the shortcomings of the existing methods. Described herein are pharmaceutically effective partial agonistic antiprogestins. The combined application of estrogens (such as estradiol, estriol and conjugated estrogens) and the disclosed partial agonistic antiprogestins can be used in hormone replacement therapy.

Combination of estrogens plus antiprogestins with significant partial agonistic effect as an effective treatment of menopausal symptoms and for prevention of the occurrence of breast cancer

Described herein are compositions and methods for hormone replacement therapy that address the shortcomings of the existing methods. Described herein are pharmaceutically effective partial agonistic antiprogestins. The combined application of estrogens (such as estradiol, estriol and conjugated estrogens) and the disclosed partial agonistic antiprogestins can be used in hormone replacement therapy.

NEUROACTIVE 19-ALKOXY-17-SUBSTITUTED STEROIDS, PRODRUGS THEREOF, AND METHODS OF TREATMENT USING SAME
20230190770 · 2023-06-22 ·

The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

NEUROACTIVE 19-ALKOXY-17-SUBSTITUTED STEROIDS, PRODRUGS THEREOF, AND METHODS OF TREATMENT USING SAME
20230190770 · 2023-06-22 ·

The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

19-NOR neuroactive steroids and methods of use thereof

Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (1): and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, tinnitus, and status epilepticus. ##STR00001##

19-NOR neuroactive steroids and methods of use thereof

Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (1): and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, tinnitus, and status epilepticus. ##STR00001##

Natural product analogs including an anti-inflammatory cyanoenone pharmacore and methods of use

This invention provides novel compounds comprising the following anti-inflammatory pharmacore: ##STR00001##
wherein X, R.sub.1 and R.sub.2 are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.

Method for preparing 6-alkylated steroidal derivatives and corresponding alkylated 5,6,7,8-tetrahydronaphthalene-2(4 alpha.H)-ones

The present invention concerns a method for preparing certain steroidal derivatives alkylated in position 6, comprising a step of alkylating the corresponding compound halogenated in position 6 with an organometallic alkylating agent.