Patent classifications
C07J43/00
TGR5 modulators and methods of use thereof
The application relates to compounds of formula A: ##STR00001##
or a salt, solvate, ester, tautomer, amino acide conjugate, or metabolite thereof. The compounds of formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.
BIAMINOQUINOLINES AND NANOFORMULATIONS FOR CANCER TREATMENT
The present invention provides bisaminoquinoline compounds of Formula (I). The present invention also provides nanocarriers comprising compounds of the present invention, and methods of using the nanocarriers for treating diseases and imaging.
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.
##STR00001##
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(O)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.
##STR00001##
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(O)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.
##STR00001##
STEROIDAL COMPOSITIONS AND METHODS OF TREATING LIPOGENIC CANCERS
The invention describes novel steroidal compounds, compositions containing the same, and methods of using the same as SREBP inhibitors, as LXR agonists, or as dual modulators of SREBP and LXR, to treat SREBP and/or LXR mediated diseases.
SIRNA THERAPY FOR TRANSTHYRETIN (TTR) RELATED OCULAR AMYLOIDOSIS
The invention relates to a method of treating ocular amyloidosis by reducing TTR expression in a subject by administering a double-stranded ribonucleic acid (dsRNA) that targets a TTR gene to the retinal pigment epithelium of the subject.
SIRNA THERAPY FOR TRANSTHYRETIN (TTR) RELATED OCULAR AMYLOIDOSIS
The invention relates to a method of treating ocular amyloidosis by reducing TTR expression in a subject by administering a double-stranded ribonucleic acid (dsRNA) that targets a TTR gene to the retinal pigment epithelium of the subject.
CRYSTALLINE FORMS OF A NEUROACTIVE STEROID
This invention relates to crystalline forms of anhydrous Compound (1) and pharmaceutical compositions thereof. Also disclosed herein are methods of making crystalline solid forms of Compound (1), and methods of using the crystalline forms of Compound (1) and pharmaceutical compositions thereof for modulating GABA activity (e.g., positive allosteric modulation of GABA activity) and treating CNS-related disorders.
##STR00001##
Compositions and methods for treating CNS disorders
Described herein are neuroactive steroids of the Formula (I): ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein , 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.