- Preparation process for indobufen intermediate
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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.
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Paragraph 0018-0025
(2019/10/01)
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- Novel compounds that reverse the disease phenotype in Type 2 Gaucher disease patient-derived cells
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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.
- Abou-Gharbia, Magid,Childers, Wayne,Colussi, Dennis J.,Fan, Rong,Gordon, John,Jacobson, Marlene A.,Liu, Yuxiao,Martinez, Rogelio,Melenski, Edward
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supporting information
(2019/12/11)
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- NOVEL FUNCTIONALIZED N,N-DIALKYLAMINO PHENYL ETHERS AND THEIR METHOD OF USE
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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.
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Paragraph 0293
(2017/12/29)
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- Method for preparing indobufen
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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.
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Paragraph 0028; 0029; 0031; 0032; 0033
(2017/08/29)
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- OXIDANT SENSITIVE AND INSENSITIVE AROMATIC ESTERS AS INHIBITORS OF HUMAN NEUTROPHIL ELASTASE
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2-Phenylalkanoate esters which are useful as inhibitors of human leukocyte elastase.
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