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Zhou F.-W.,Southwest University | Lei H.-S.,Chongqing Pharmaceutical Research Institute Co. | Fan L.,Southwest University | Jiang L.,Schlumberger | And 9 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2014

Tuberculosis remains a global public health problem in recent years. To develop novel type of potential antitubercular agents, twelve novel dihydroartemisinin-fluoroquinolone (DHA-FQ) conjugates (three types of molecules) were gradually designed and conveniently synthesized. All the newly synthesized conjugates were well characterized and evaluated against different Mycobacterium tuberculosis strains in vitro. The screening results showed that five DHA-FQ conjugates were active toward M. tuberculosis H37Rv, and compound 3a exhibited the strongest inhibitory activity (MIC = 0.0625 μg/mL), which was comparable to the positive control Moxifloxacin and even stronger than Ofloxacin. Conjugates 2a and 3a also displayed comparable activities against various clinically isolated sensitive and resistant M. tuberculosis strains (MIC = 0.125-16 μg/mL) to Moxifloxacin. All target compounds possessed selective anti-M. tuberculosis ability. Preliminary structure-activity relationship demonstrated that short linker between DHA and FQ was favorable for strong antitubercular activity. This study provides a new clue for the development of novel antitubercular lead molecules. © 2014 Elsevier Ltd. All rights reserved.


Chen Y.-N.,Chongqing Medical University | Zhao X.-D.,Fochon Pharma Inc. | Deng J.,Chongqing Pharmaceutical Research Institute Co. | Li Q.-G.,Chongqing Medical University
Acta Crystallographica Section E: Structure Reports Online | Year: 2012

The title compound, C14H19N3O3, was synthesized by the reaction of 3-methoxy-propionitrile, tert-butyl bromo-acetate and eth-oxy-methyl-enemalononitrile. In the crystal, N - H⋯O hydrogen bonds link the molecules into chains propagating along the b axis. © Chen et al. 2012.


Wang N.-N.,Chongqing Medical University | Zhang D.-L.,Chongqing Pharmaceutical Research Institute Co. | Jiang X.-H.,Chongqing Medical University
Chirality | Year: 2015

A high-performance liquid chromatography (HPLC) method was established to detect Xeljanz enantiomers in active pharmaceutical ingredients (APIs) and tablets. The separation was achieved on a Chiralpak IC column using a mobile phase of hexane-ethanoldiethylamine (65:35:0.1, v/v). The detection wavelength was 289 nm. The peak areas and the enantiomer concentrations in the range of 0.15-2.25μg·mL-1 were in high linearity, with correlation coefficients higher than 0.999. The recoveries were 86.44% at the concentrations of 7.5, 18.75, and 37.5μg·mL-1. The limit of detection (LOD) and limit of quantification (LOQ) were 0.042 and 0.14μg·mL-1, respectively. This HPLC method is suitable for detecting the enantiomers of Xeljanz in its APIs and tablets. © 2014 Wiley Periodicals, Inc.


Zong T.,University of Sichuan | Zong T.,Chongqing Pharmaceutical Research Institute Company | Mei L.,University of Sichuan | Gao H.,University of Sichuan | And 6 more authors.
Journal of Pharmaceutical Sciences | Year: 2014

The development of a drug delivery strategy that can not only cross the blood-brain barrier (BBB) rapidly, but also target the glioma and reach the core of glioma is essential and important for glioma treatment. To achieve this goal, we established a dual-targeting liposomal system modified with TAT (AYGRKKRRQRRR) and T7 (HAIYPRH), in which the specific ligand T7 could target BBB and brain glioma tumor and the nonspecific ligand TAT could enhance the effect of passing through BBB, and elevate the penetration into the tumor. The dual-targeting effects were evaluated by both in vitro and in vivo experiments. To identify the targeting effect, in vitro cellular uptake and BBB model were performed. Tumor spheroid penetration was performed to evaluate the penetration characteristics of the dual-targeting liposomes. In vivo pharmacokinetic studies were utilized to evaluate the influence of T7 and TAT peptides on the behavior of nanoparticle drug delivery system, and tissue distribution was further utilized to evaluate the glioma-targeting efficiency of the dual-targeting liposomes. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association.


Zong T.,University of Sichuan | Zong T.,Chongqing Pharmaceutical Research Institute Co. | Mei L.,University of Sichuan | Gao H.,University of Sichuan | And 7 more authors.
Molecular Pharmaceutics | Year: 2014

Therapeutic outcome for the treatment of glioma was often limited due to low permeability of delivery systems across the blood-brain barrier (BBB) and poor penetration into the tumor tissue. In order to overcome these hurdles, we developed the dual-targeting doxorubicin liposomes conjugated with cell-penetrating peptide (TAT) and transferrin (T7) (DOX-T7-TAT-LIP) for transporting drugs across the BBB, then targeting brain glioma, and penetrating into the tumor. The dual-targeting effects were evaluated by both in vitro and in vivo experiments. In vitro cellular uptake and three-dimensional tumor spheroid penetration studies demonstrated that the system could not only target endothelial and tumor monolayer cells but also penetrate tumor to reach the core of the tumor spheroids and inhibit the growth of the tumor spheroids. In vivo imaging further demonstrated that T7-TAT-LIP provided the highest tumor distribution. The median survival time of tumor-bearing mice after administering DOX-T7-TAT-LIP was significantly longer than those of the single-ligand doxorubicin liposomes and free doxorubicin. In conclusion, the dual-ligand liposomes comodified with T7 and TAT possessed strong capability of synergistic targeted delivery of payload into tumor cells both in vitro and in vivo, and they were able to improve the therapeutic efficacy of brain glioma in animals. © 2014 American Chemical Society.


Patent
Chongqing Pharmaceutical Research Institute Co. | Date: 2011-08-03

Three new crystalline forms of pemetrexed diacid, preparation methods and uses thereof are disclosed. These preparation processes are simple and have better practicality.


Patent
Chongqing Pharmaceutical Research Institute Co . Ltd. | Date: 2010-01-20

A febuxostat which purity is not less than 99.0%, method for preparation thereof, and pharmaceutical composition thereof. The method for preparation includes recrystallizing febuxostat in a mixed solvent. The said pharmaceutical composition can be used in manufacture of medicaments for treating diseases associated with hyperuricemia.


Patent
Chongqing Pharmaceutical Research Institute Co. | Date: 2010-10-28

The present invention provides a stable composition of rasagiline comprising an effective dosage of rasagiline or its pharmaceutically acceptable salts and an antioxidant used as a stabilizer. The dosage forms of the composition are pharmaceutically common transdermal-drug delivery dosage form and mucoadhesive delivery dosage form, such as patch, gel, ointment, cream, cataplasm, film, spray and solution, etc. The composition can be used to prevent or treat mental disorders.


Patent
Chongqing Pharmaceutical Research Institute Co. | Date: 2010-08-04

A method of purifying a salt of pemetrexed have a structure of formula (III) by salting-out, wherein if M_(3)^(+) is H^(+), then each of M_(1)^(+) and M_(2)^(+) is independently H^(+), Li^(+), Na^(+) or K^(+), provided that both of them are not H^(+); if M_(3)^(+) is Li^(+), Na^(+) or K^(+), then each of M_(1)^(+) and M_(2)^(+) is independently Li^(+), Na^(+) or K^(+).


Patent
Chongqing Pharmaceutical Research Institute Co. | Date: 2012-09-05

The present invention provides a stable composition of rasagiline comprising an effective dosage of rasagiline or its pharmaceutically acceptable salts and an antioxidant used as a stabilizer. The dosage forms of the composition are pharmaceutically common transdermal-drug delivery dosage form and mucoadhesive delivery dosage form, such as patch, gel, ointment, cream, cataplasm, film, spray and solution, etc. The composition can be used to prevent or treat mental disorders.

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