29644-97-1Relevant academic research and scientific papers
Preparation process for indobufen intermediate
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Paragraph 0018-0025, (2019/10/01)
The invention belongs to the field of drug synthesis, and specifically discloses a preparation process for an indobufen intermediate. With the preparation process provided by the invention, hydrazinehydrate and iron oxyhydroxide are adopted to reduce 2-(4-nitrophenyl)butyric acid; and an obtained product reaches a purity of 99.5% or more and a yield of 99.0% or more. The preparation process provided by the invention only uses water as a reaction solvent, has simple synthesis process and post-treatment operation, is safe and environmentally-friendly, has low cost, improves the yield of a reaction and the purity of a product, and is applicable to industrial production.
Novel compounds that reverse the disease phenotype in Type 2 Gaucher disease patient-derived cells
Abou-Gharbia, Magid,Childers, Wayne,Colussi, Dennis J.,Fan, Rong,Gordon, John,Jacobson, Marlene A.,Liu, Yuxiao,Martinez, Rogelio,Melenski, Edward
supporting information, (2019/12/11)
Gaucher disease (GD) results from inherited mutations in the lysosomal enzyme β-glucocerobrosidase (GCase). Currently available treatment options for Type 1 GD are not efficacious for treating neuronopathic Type 2 and 3 GD due to their inability to cross the blood-brain barrier. In an effort to identify small molecules which could be optimized for CNS penetration we identified tamoxifen from a high throughput phenotypic screen on Type 2 GD patient-derived fibroblasts which reversed the disease phenotype. Structure activity studies around this scaffold led to novel molecules that displayed improved potency, efficacy and reduced estrogenic/antiestrogenic activity compared to the original hits. Here we present the design, synthesis and structure activity relationships that led to the lead molecule Compound 31.
NOVEL FUNCTIONALIZED N,N-DIALKYLAMINO PHENYL ETHERS AND THEIR METHOD OF USE
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Paragraph 0293, (2017/12/29)
Pharmaceutical compositions of the invention comprise functionalized N,N-dialkylamino phenyl ethers derivatives having a disease-modifying action in the treatment of diseases associated with lysosomal storage dysfunction that include Gaucher's disease, and any disease or condition involving lysosomal storage dysfunction.
Method for preparing indobufen
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Paragraph 0028; 0029; 0031; 0032; 0033, (2017/08/29)
The invention discloses a method for preparing indobufen; by optimizing the processes such as using a carbon-supported noble metal as a catalyst in hydrogenation reduction, using a suitable organic acid solvent in zinc powder reduction and introducing hydrogen chloride gas, the preparation method of indobufen is simple to perform and high in yield; the whole preparation method is good in safety, environmentally friendly, good for protecting the health of workers and suitable for industrial use, and the purity of prepared indobufen is high.
OXIDANT SENSITIVE AND INSENSITIVE AROMATIC ESTERS AS INHIBITORS OF HUMAN NEUTROPHIL ELASTASE
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, (2008/06/13)
2-Phenylalkanoate esters which are useful as inhibitors of human leukocyte elastase.
