Patent classifications
C07J41/005
Bile acid derivatives as FXR agonists and methods of use thereof
The present invention provides compounds represented by Formula I, or pharmaceutically acceptable salts, prodrugs and esters thereof, ##STR00001##
The invention also provides pharmaceutical compositions comprising these compounds and methods of using this compounds for treating FXR-mediated or TGR5-mediated diseases or conditions.
CRYSTAL FORM OF 3-HYDROXY-5-PREGNANE-20-ONE DERIVATIVE, AND PREPARATION METHOD THEREFOR AND USE THEREOF
The present invention provides a crystal of a compound represented by formula I as a 3-hydroxy-5-pregnane-20-one derivative and a preparation method therefor. Specifically, the present invention provides novel crystal forms A-C of the compound represented by formula I and a preparation method therefor. The novel crystal forms of the compound represented by formula I of the present invention have excellent thermal stability and mechanical stability, the preparation process thereof is simple, and the novel crystal forms have an excellent industrial implementation potential.
##STR00001##
Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
The present invention provides compounds represented by Formula I, or pharmaceutically acceptable salts, stereoisomers, solvates, hydrates or combination thereof, ##STR00001##
The invention also provides pharmaceutical compositions comprising these compounds and methods of using this compounds for treating FXR-mediated or TGR5-mediated diseases or conditions.
Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
The present invention provides compounds represented by Formula I, or pharmaceutically acceptable salts, stereoisomers, solvates, hydrates or combination thereof, ##STR00001##
The invention also provides pharmaceutical compositions comprising these compounds and methods of using this compounds for treating FXR-mediated or TGR5-mediated diseases or conditions.
WATER-SOLUBLE ALLOPREGNENOLONE DERIVATIVE AND USE THEREOF
The present invention relates to the field of medicine, and particularly relates to a water-soluble allopregnenolone (3,5-tetrahydroprogesterone) derivative, a pharmaceutical composition comprising the same, and use thereof in prevention or treatment of central nervous system diseases, in sedation and hypnosis, in treatment of Alzheimer's disease, in treatment of epilepsy or in treatment of depression, especially postpartum depression.
##STR00001##
THIONYL TETRAFLUORIDE MODIFIED COMPOUNDS AND USES
Thionyl tetrafluoride gas reacts efficiently with primary amines to form reactive iminosulfur oxydifluoride compounds. These dual S.sup.VIF loaded iminosulfur oxydifluoride compounds, in turn, readily react with secondary amines or aryloxy silyl ethers (ArOSiR.sub.3), yielding the corresponding fused heteroatom-linked substrates. Iminosulfur oxyfluoride polymers also are provided by disclosed methods.
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##
PROGESTERONE ANALOGS AND USES RELATED THERETO
This disclosure relates to progesterone derivatives and uses related thereto. In certain embodiments, the disclosure relates to compounds disclosed herein and uses for managing inflammation resulting from traumatic brain injury or stroke.
C7, C12, and C16 substituted neuroactive steroids and their methods of use
Described herein are neuroactive steroids of Formula (I), Formula (V), or Formula (IX) or a pharmaceutically acceptable salt thereof; wherein each instance of R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.11a, R.sup.11b, R.sup.12, R.sup.16, R.sup.17, R.sup.19, and are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a compound described herein and methods of use and treatment, e.g., such as for inducing sedation and/or anesthesia. ##STR00001##
C17, C20, AND C21 SUBSTITUTED NEUROACTIVE STEROIDS AND THEIR METHODS OF USE
Described herein are neuroactive steroids or a pharmaceutically acceptable salt thereof. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a compound described herein and methods of use and treatment, e.g., such as for inducing sedation and/or anesthesia.