TABLE 1 | Recent patent applications related to FXR and TGR5 receptor modulators
From the following article:
Charlotte Harrison
Nature Reviews Drug Discovery 7, 636-637 (August 2008)
doi:10.1038/nrd2651
| Patent number(s) | Assignee(s) | Subject |
|---|---|---|
| WO 2007140183 | Eli Lilly | Describes new pyrazole derivatives that are potent, efficacious and selective FXR agonists; useful for treating dyslipidaemia, coronary artery disease, obesity and hypertension. |
| WO 2007092751 | Eli Lilly | Describes new aryl-isoxazole derivatives that are FXR modulators that enhance the profile of lipid regulation; useful for treating dyslipidaemia, atherosclerosis and diabetes. |
| US 20080096921 WO 2008051942 | GlaxoSmithKline | These describe new 2-quinolinecarboxylic acid derivatives (preferably their potassium salts) that act as FXR agonists; useful for treating diabetes, obesity, metabolic syndrome and organ fibrosis. |
| WO 2007076260 | GlaxoSmithKline | Describes new substituted isoxazole compounds that are FXR agonists that improve the flux of bile acid from the liver to the intestine; useful for treating liver fibrosis, diabetes, metabolic syndrome and obesity. |
| WO 2007095174 | Intercept Pharmaceuticals | Describes new bile-acid compounds that are FXR modulators; useful for treating hypercholesterolaemia and hypertriglyceridaemia, and metabolic conditions such as insulin resistance, diabetes and obesity. |
| WO 2008002573 | Intercept Pharmaceuticals | Describes new 24-nor-5b-cholan-23-sulphonic acid derivatives that are selective FXR modulators; useful for treating gastrointestinal, renal, cardiovascular and metabolic diseases. |
| US 2008039435 | Intercept Pharmaceuticals | Describes new (R)-4-pentanoic acid derivatives that are FXR agonists; useful for increasing HDL-cholesterol, for lowering triglycerides, and for the treatment or prevention of arteriosclerosis, hypercholesterolaemia and hyperlipidaemia. |
| WO 2008067222 | Kalypsys | Describes new heterocyclic compounds as modulators of TGR5; useful for treating or preventing diabetes, obesity, fatty liver, liver fibrosis, kidney fibrosis, anorexia nervosa and bulimia nervosa. |
| WO 2008067219 | Kalypsys | Describes new quinazolinone compounds that are TGR5 modulators; useful for treating or preventing metabolic, cardiovascular and inflammatory diseases. |
| EP 1810689 | Mitsubishi Pharma | Deascribes a compound that suppresses FXR activity; useful for preventing and/or treating diabetes by suppressing hepatic glucose neogenesis or activating energy metabolism. |
| WO 2008025540 | Phenex Pharmaceuticals | Describes new heterocyclic compounds that are potent FXR agonists or partial agonists with improved physicochemical and pharmacokinetic properties; useful for the prophylaxis and treatment of obesity, dyslipidaemia and diabetes. |
| WO 2008000643 US 20080021027 | Roche et al. | These describe new benzimidazole derivatives that are selective FXR agonists; useful for treating dyslipidaemia, atherosclerosis, diabetes, metabolic syndrome and cholesterol gallstone disease. |
| JP 2008094826 | Takeda | Describes a heterocyclic amide compound that is an FXR inhibitor without side effects; useful as a preventive and/or therapeutic agent of hyperlipidaemia, cholesterolaemia and artherosclerosis disease. |
| JP 2007230909 | University of Tokyo | Describes novel substituted isoxazole derivatives that are FXR agonists or antagonists; useful for preventing and/or treating lipid metabolism disorders. |
| FXR, farnesoid X receptor; HDL, high-density lipoprotein; TGR5, also known as G-protein-coupled bile acid receptor 1 (GPBAR1). | ||
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