Patent classifications
C07J9/005
METHODS AND INTERMEDIATES FOR THE PREPARATION OF BILE ACID DERIVATIVES
The present disclosure relates to methods and novel intermediates useful in the preparation of a compound of formula I
##STR00001##
or pharmaceutically acceptable salt, hydrate, solvate or amino acid, sulfate or glucuronide conjugate, or prodrug thereof.
HYDROXYSTEROID COMPOUNDS
The present application discloses derivatives of hydroxysteroids, pharmaceutically acceptable salts, stereoisomers or tautomers thereof. The compounds and compositions described herein can be used in therapy.
Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
The present invention provides compounds of Formula I, ##STR00001##
pharmaceutical compositions comprising these compounds and methods of using these compounds to prevent or treat FXR-mediated or TGR5-mediated diseases or conditions.
Pleuromutilin ursodeoxycholic acid ester with antibacterial activity and a method of preparing the same
A compound with antibacterial activity having the following formula (I): ##STR00001##
is disclosed. A method of preparing the compound of formula (I) is also disclosed.
FRACTIONATION OF CRUDE TALL OIL
The present invention relates to fractionation of crude tall oil, which originates from the Kraft process black liquor. In the method, according to the present invention, simulated moving bed (SMB) chromatography is used to efficiently separate fractions from the crude tall oil.
Methods for Preparing Bile Acids
The present disclosure provides methods of preparing cholic acid, deoxycholic acid, or chenodeoxycholic acid, an ester thereof, or a pharmaceutically or cosmetically acceptable salt thereof, and novel and useful synthetic intermediates, for example, as described for methods 1, 1A, 1B, 2, 3, 3A, and 4. The method can start with a plant derived steroid as a starting material, such as dehydroepiandrosterone (DHEA) or Acetyl-dehydroepiandrosterone (Ac-DHEA). Also provided are pharmaceutical or cosmetic compositions and uses thereof, which comprise one or more of cholic acid, deoxycholic acid, or chenodeoxycholic acid, an ester thereof, or a pharmaceutically or cosmetically acceptable salt thereof, which is of high purity, for example, free of animal derived impurities.
CATIONIC STEROIDAL ANTIMICROBIAL COMPOUNDS WITH URETHANE LINKAGES
Cationic steroidal antimicrobial (CSA) compounds having a structure of Formula I, II or III, or salt thereof, wherein at least one of at least one of R.sub.1-R.sub.18, (e.g., R.sub.3, R.sub.7 and R.sub.12) is linked to the steroidal backbone by a urethane group:
##STR00001##
At least one of R.sub.1-R.sub.18, (e.g., R.sub.3, R.sub.7 and R.sub.12) has the following urethanyl structure:
—O—(C═O)—NR.sub.19R.sub.20
where R.sub.19 and R.sub.20 are independently hydrogen, alkyl, alkenyl, alkynyl, aryl, aminoalkyl, aminoalkenyl, aminoalkynyl, or aminoaryl, provided that at least one of R.sub.19 or R.sub.20 includes an amino group (e.g., R.sub.19 is hydrogen and R.sub.20 is (C.sub.2-C.sub.6)aminoalkyl).
R.sub.18 can have the following structure:
—R.sub.21—(C═O)—NR.sub.22R.sub.23
where R.sub.21 is omitted or alkyl, alkenyl, alkynyl, or aryl, and R.sub.22 and R.sub.23 are hydrogen, alkyl, alkenyl, alkynyl, or aryl, provided that at least one of R.sub.22 or R.sub.23 is not hydrogen.
STEROID COMPOUNDS AS TREG MODULATORS AND USES THEREOF
Steroid compounds are disclosed that have a formula represented by the following: (I) and wherein R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6a, R.sup.6b, R.sup.7, R.sup.8, and n are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for promoting differentiation of T regulatory (Treg) lymphocytes, and for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune disorders, and graft-versus-host disease.
##STR00001##
FLUORINATED AND ALKYLATED BILE ACIDS
The present invention relates to fluorinated and alkylated bile acids.
Amine salt of obeticholic acid
The present application relates to amine salt of obeticholic acid. Specifically, the present application relates to (S)-α-methylbenzylamine and diethylamine salt of obeticholic acid. The present application also relates to a process for preparation of amorphous form of obeticholic acid comprising converting amine salt of obeticholic acid to amorphous form of obeticholic acid.