C07J13/00

NEUROACTIVE 19-ALKOXY-17-SUBSTITUTED STEROIDS, PRODRUGS THEREOF, AND METHODS OF TREATMENT USING SAME
20200113916 · 2020-04-16 ·

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.

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Process for preparation of corticosteroids

The present invention discloses a process for the preparation of pregnadiene derivatives having formula I, their stereoisomer and intermediate thereof. Formula I wherein each substituent is independently, R.sub.1 and R.sub.2 is hydrogen or C.sub.1-C.sub.8 straight, branched alkyl chain, saturated or unsaturated cycloalkyl; R.sub.3 is hydrogen or wherein R.sub.5 represents C.sub.1-C.sub.8 straight, branched alkyl chain or cycloalkyl; R.sub.4 is hydrogen or halogen; R.sub.6 is hydrogen or halogen; ##STR00001##

ANTIBIOTICS WITH IMPROVED DRUG RESISTANCE PROFILE

Novel Fusidic Acid (FA) based compounds that have equivalent potency against clinical isolates of Staphylococcus aureus (S. aureus) and Enterococcus faecium (E. faecium) as well as an improved resistance profile in vitro when compared to FA. Importantly, the new compounds display efficacy against a FA-resistant strain of Staphylococcus aureus in a soft-tissue murine infection model. This disclosure delineates the structural features of FA necessary for potent antibiotic activity and demonstrates that the resistance profile can be improved for this scaffold and target.

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.

Methods for preparation of bile acids and derivatives thereof

The present application relates to a method of preparing compounds of Formula (I) or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, R.sub.1 is H, -OH, -OH, or an oxo group. ##STR00001##

19-nor neuroactive steroids and methods of use thereof

Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I): 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.

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Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same

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.

NOVEL PROCESS FOR PREPARATION OF CORTICOSTEROIDS

The present invention discloses a process for the preparation of pregnadiene derivatives having formula I, their stereoisomer and intermediate thereof. Formula I wherein each substituent is independently, R.sub.1 and R.sub.2 is hydrogen or C.sub.1-C.sub.8 straight, branched alkyl chain, saturated or unsaturated cycloalkyl; R.sub.3 is hydrogen or wherein R.sub.5 represents C.sub.1-C.sub.8 straight, branched alkyl chain or cycloalkyl; R.sub.4 is hydrogen or halogen; R.sub.6 is hydrogen or halogen;

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