222555-05-7

Upstream product

• 482656-47-3 ethyl (2R)-3-[4-(benzyloxy)phenyl]-2-hydroxypropanoate 
• 222835-03-2 3-(4-benzyloxy-phenyl)-2-ethoxy-acrylic acid ethyl ester 
• 13676-06-7 ethyl 2-ethoxy-2-(diethylphosphono)acetate 
• 34006-60-5 ethyl 2-chloro-2-ethoxyacetate 
• 6065-82-3 Ethyl diethoxyacetate 
• 197299-16-4 ethyl 2-ethoxy-3-(4-hydroxy-phenyl)-propionate 
• 373368-68-4 (R)-3-[4-(benzyloxy)phenyl]-2-hydroxypropanoic acid 
• 847268-21-7 ethyl (2R)-3-[4-(benzyloxy)phenyl]-2-ethoxypropanoate 

Downstream Products

• 1416820-83-1 ethyl (2R)-2-ethoxy-3-{4-[2-(3-methoxyphenyl)-2-oxoethoxy]phenyl}propanoate 
• 1416820-84-2 (2R)-2-ethoxy-3-{4-[2-(3-methoxyphenyl)-2-oxoethoxy]phenyl}propanoic acid 
• 1416820-93-3 (R)-ethyl 2-ethoxy-3-(4-(2-(5-ethylpyridin-2-yl)-2-oxoethoxy)phenyl)propanoate 
• 1416820-94-4 (R)-2-ethoxy-3-(4-(2-(5-ethylpyridin-2-yl)-2-oxoethoxy)phenyl)propanoic acid 
• 1022149-28-5 C₃₃H₃₉NO₅ 
• 305827-61-6 (-)-ethyl 2-ethoxy-3-[4-[2-(2,3-dihydro-1,4-benzoxazin-4-yl)ethoxy]phenyl]propanoate 
• 305827-41-2 (-)-ethyl 2-ethoxy-3-[4-[2-(2,3-dihydro-1,4-benzothiazin-4-yl)ethoxy]phenyl]propanoate 

Relevant academic research and scientific papers

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.

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.

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).