C07J41/0061

DEOXYCHOLIC ACID COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
20230146782 · 2023-05-11 ·

Disclosed are a deoxycholic acid compound and a pharmaceutical composition thereof, and use thereof in the preparation of drugs for treating liver diseases. The structure of the deoxycholic acid compound is as shown by Formula I, or pharmaceutically acceptable salts thereof. The compounds have significantly liver-targeting characteristics, and the compounds reduce the drug concentration in the circulatory system while improving the efficacy, thereby reducing the toxic side effects.

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COMPOUND WITH ANTI-SPORE ACTIVITY AND PHARMACEUTICAL COMPOSITION THEREOF

The present disclosure provides a compound represented by formula (I), or a salt or a stereoisomer thereof. The compound is capable of effectively inhibiting germination of Clostridium difficile spores with a significant bacteriostatic activity. The compound has an excellent prospect for use in preparation of a drug for preventing and/or treating a C. difficile-caused infectious disease, recurrence of the C. difficile-caused infectious disease, or a complication of the C. difficile-caused infectious disease.

TGR5 MODULATORS AND METHODS OF USE THEREOF

The application relates to compounds of formula A:

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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.

NOVEL DRUG DELIVERY CONJUGATED MOIETY FOR ORAL ADMINISTRATION OF DRUG UNSUITABLE FOR ORAL ADMINISTRATION AND PREPARATION METHOD THEREOF

The present invention provides a novel drug delivery conjugated moiety for oral administration of a drug that is not suitable for oral administration or a pharmaceutically acceptable salt thereof. When the drug delivery conjugated moiety of the present invention or a pharmaceutically acceptable salt thereof is combined with a drug, which is not suitable for oral administration, and is administered orally, it exhibits an excellent absorption rate without decreasing the biological activities of the drug. Moreover, the drug delivery conjugated moiety of the present invention or a pharmaceutically acceptable salt thereof can be easily prepared in a few steps, which is very advantageous in terms of mass production.

NEUROACTIVE STEROIDS AND METHODS OF USE THEREOF

Compounds are provided according to Formula (I):

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and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4, R.sup.5a, R.sup.5b, R.sup.6a, and R.sup.6b are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions.

METHODS OF MAKING CHOLIC ACID DERIVATIVES AND STARTING MATERIALS THEREFOR

Methods of making cholic acid derivatives, particularly ursodeoxycholic acid, tauroursodeoxycholic acid, 7-ketolithocholic acid, obeticholic acid, their carboxylate salts and carboxylate esters, and starting materials and intermediates therefor.

Steroid derivative FXR agonist

The present invention relates to a compound represented by formula (I), a tautomer thereof or a pharmaceutically acceptable salt thereof, and relates to applications thereof in the preparation of drugs for treating FXR related diseases. ##STR00001##

OXYSTEROLS AND METHODS OF USE THEREOF

Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R.sup.1, R.sup.2, and R.sup.3 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

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HETEROARYL CONTAINING BILE ACID ANALOGS AS FXR/TGR5 AGONISTS AND METHODS OF USE THEREOF
20170240587 · 2017-08-24 ·

The present invention provides compounds of Formula I,

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pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR and/or TGR5.

Benzoic Acid Derivatives of Bile Acid as FXR/TGR5 Agonists and Methods of Use Thereof
20170240586 · 2017-08-24 ·

The present invention provides compounds of Formula I:

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pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR and/or TGR5.