Patent classifications
C07J5/00
ENZYMATIC PROCESS FOR OBTAINING 17 ALPHA-MONOESTERS OF CORTEXOLONE AND/OR ITS 9,11-DEHYDRODERIVATIVES
The present invention refers to a new enzymatic process for obtaining 17-monoesters of cortexolone and/or its 9,11-dehydroderivatives starting from the corresponding 17,21-diesters which comprises an enzymatic alcoholysis reaction. Furthermore, the present invention refers to now crystalline forms of cortexolone-17-propionate and 9,11-dehydro-cortexolone 17-butanoate.
ENCODED DESIGN INTEGRATED SYNTHESIS OF NUCLEIC ACIDS, AND PHOSPHOLIPIDS, AND RELATED PHARMACEUTICAL PRODUCTS
Provided herein are reactive aromatic molecules (e.g., substituted chrysene heterodimers) encodable as base-four sequences for the design and integrated synthesis of nucleic acids (e.g., DNA, RNA, hybrid DNA/RNA) and associated phospholipid bilayers (e.g., cellular membranes). For example, 3,6,9,12-tetrasubstituted chrysene is coupled with 6,12-disubstituted chrysene through -electron stacking to form a base-four heterodimer. The orientation of the ring structure of the tetrasubstituted chrysene in this heterodimer comprises a base-two (binary) structure and the relative alignment of the ring structure of the disubstituted chrysene to the tetrasubstituted chrysene comprises a second independent base-two (binary) structure. This collectively results in a base-four (quaternary) complex composed of four independent reaction environments. Methods of forming the heterodimers (and conjugated systems) include coupling sidechains of ethoxylated alcohol by phosphorylation. This may result in phosphodiester linkages at the 6,12 positions and/or uncoupled phosphorylated sidechains of ethoxylated alcohol at the 3,9 positions of the reactive aromatic molecules. The uncoupled phosphorylated sidechains may polymerize with adjacent tetrasubstituted chrysene through phosphodiester linkages. Various methods for initiating a reaction (e.g., oxidative cleavage) within the assembly of these -electron stacked heterodimers can be utilized to produce nucleic acid sequences from the stacked tetrasubstituted chrysenes along with an associated phospholipid structure from the coupled disubstituted chrysene. Also provided herein are encoding and decoding design relations that can be utilized to map the base-four substituted chrysene heterodimers to the base-four nucleic acids (e.g., DNA, RNA, hybrid DNA/RNA). The present disclosure also includes various methods of regulating the sequence of substituted heterodimers to produce a specific encoding type of nucleic acid (e.g., DNA, RNA, hybrid DNA/RNA) and direct the 5-3 polymerization direction. The present disclosure also includes polycyclic pharmaceutical molecular agents resultant from the structural correlations in deriving the base-four heterodimer for subsequent synthesis to a sequence of nucleic acids and phospholipids.
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.
LYMPH DIRECTING PRODRUGS
The present invention relates to compounds and their uses, in particular, compounds in the form of prodrugs that promote transport of a pharmaceutical agent to the lymphatic system and subsequently enhance release of the parent drug.
NEUROSTEROID COMPOUNDS AND METHODS FOR THEIR PREPARATION AND USE IN TREATING CENTRAL NERVOUS SYSTEM DISORDERS
Described herein is the chemical structure of neurosteroid derivative compounds, methods of synthesizing the derivatives, and their uses in treating disorders, including those of the central nervous system. These compounds are readily synthesized and have improved pharmaceutical properties, including water solubility, compared to known neurosteroids.