Patent classifications
C07J41/0088
Androstane Derivatives with Activity as Pure or Predominantly Pure Stimulators of SERCA2a for the Treatment of Heart Failure.
Compounds and compositions for the activation of SERCA2a are disclosed. In particular, provided are compounds that act as predominantly pure or pure SERCA2a activators while only moderately inhibiting the Na.sup.+/K.sup.+ ATPase. In general, the disclosed compounds are derivatives of androstane having the formula (I). Also disclosed herein are pharmaceutical compositions comprising one or more of the compounds of formula (I) for use for the treatment of heart failure.
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Hydroxysteroid compounds, their intermediates, process of preparation, composition and uses thereof
The present invention relates to novel steroidal compounds of formula (I), process for preparation of the same and composition comprising these compounds. ##STR00001##
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.
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,
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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.
Methods for treating inflammation, autoimmune disorders and pain
Disclosed herein are methods of treating, reducing, or preventing a disease such as oral mucositis, gastric mucositis, or inflammatory fibrosis, comprising identifying a patient in need of treatment and administering a therapeutically effective amount of at least one cationic steroid antimicrobial (CSA), or a pharmaceutically acceptable salt thereof. Kits comprising such compositions and instructions on such methods are also contemplated herein.
INHIBITORS OF GLUCOCORTICOID RECEPTOR
The present invention relates generally to compositions and methods for treating cancer and hypercortisolism. Provided herein are substituted steroidal derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of glucocorticoid receptors. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.
METHODS FOR MODULATION OF LIPOPROTEIN LIPASE AND APOLIPOPROTEIN C2 EXPRESSION AND/OR ACTIVITY IN THE TREATMENT OF PERIPHERAL AND CENTRAL NERVOUS SYSTEM TISSUE DISEASE STATES
Methods for modulating lipoprotein lipase (LPL) and Apoliprotein C2 (ApoC2) expression and/or activity in the treatment of peripheral and central nervous system tissue disease states with C-6 substituted estradiol derivatives are presented herein.
Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid
The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I): ##STR00001##
wherein: , R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and Y are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.
Compounds for treating neurodegenerative disorders
The invention relates to compounds of formula (I), their method of synthesis as well as their use to treat neurodegenerative disorders. ##STR00001##
DEOXYCHOLIC ACID COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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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