- PPAR-SPARING COMPOUNDS FOR THE TREATMENT OF METABOLIC DISEASES
-
The present invention relates to hydroxamate compounds and pharmaceutical compositions that are useful for treating and/or preventing metabolic inflammation mediated diseases such as diabetes, obesity, hypertension, dyslipidemia, a neurodegenerative disorder (e.g., Alzheimer's disease, Parkinson's disease, or Huntington's disease), or any combination thereof. Moreover, the present invention also provides methods of treatment for these diseases or disorders.
- -
-
-
- PPAR-SPARING THIAZOLIDINEDIONES AND COMBINATIONS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
-
The present invention relates to PPARy- sparing compounds and pharmaceutical compositions formulated with such compounds that are useful for treating, delaying the onset of, or reducing the symptoms of a neurodegenerative disorder including Huntington's disease, epilepsy, AMS, and MS.
- -
-
-
- PPAR-SPARING COMPOUNDS FOR USE IN THE TREATMENT OF DIABETES AND OTHER METABOLIC DISEASES
-
The present invention relates to compounds and pharmaceutical compositions that are useful for treating and/or preventing diabetes or other metabolic diseases, optionally in combination with a second therapy such an active pharmaceutical agent or diet restriction or an increase in duration or exertion in physical activity.
- -
-
-
- 4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARα/γ agonists. Part I: Synthesis and pharmacological evaluation
-
Type-2 diabetes (T2D) is a complex metabolic disease characterized by insulin resistance in the liver and peripheral tissues accompanied by a defect in pancreatic β-cell. Since their discovery three subtypes of Peroxisomes Proliferators Activated Receptors were identified namely PPARα, PPARγ and PPARβ/(δ). We were interested in designing novel PPARγ selective agonists and/or dual PPARα/γ agonists. Based on the typical topology of synthetic PPAR agonists, we focused our design approach on 4,4-dimethyl-1,2,3,4-tetrahydroquinoline as novel cyclic tail.
- Parmenon, Cecile,Guillard, Jerome,Caignard, Daniel-Henri,Hennuyer, Nathalie,Staels, Bart,Audinot-Bouchez, Valerie,Boutin, Jean-Albert,Dacquet, Catherine,Ktorza, Alain,Viaud-Massuard, Marie-Claude
-
p. 1617 - 1622
(2008/09/19)
-
- PROCESS FOR PREPARING 3-ARYL-2-HYDROXY PROPANOIC ACID DERIVATIVES WITHOUT RESOLUTION
-
The present invention discloses an improve process for the preparation of S (-) and R (+) 3-aryl-2-hydroxy propanoic acid derivatives without any resolution involved.
- -
-
Page/Page column 20-21
(2010/02/11)
-
- Process development on the enantioselective enzymatic hydrolysis of S-ethyl 2-ethoxy-3-(4-hydroxyphenyl)propanoate
-
A novel biocatalytic approach for the large-scale production of S-2-ethoxy-3-(4-hydroxyphenyl)propanoic acid S-1 from its racemic ethylester rac-2 by enantioselective hydrolysis has been developed. S-1 is an important building block in the synthesis of PPARα and -γ agonists such as Ragaglitazar [NNC 61-0029 ((-)DRF2725)]. The development history comprises enzyme screening, biocatalyst and process optimization, and scale-up to pilot plant. The project was thereby highly interdisciplinary by combining biotechnology and chemistry technologies. The final process was successfully run on a 44-kg pilot scale in 43-48% yields and with high enantiomeric purities (98.4-99.6% ee).
- Deussen, Heinz-Josef,Zundel, Magali,Valdois, Marine,Lehmann, Soren Vig,Weil, Volker,Mailand Hjort, Carsten,stergaard, Peter Rahbek,Marcussen, Erik,Ebdrup, Soren
-
-