RESUMEN
Pazopanib (trade name Votrient®) is a potent and selective multi-targeted tyrosine kinase inhibitor that blocks tumor growth and inhibits angiogenesis. Based on a recently reported procedure, we herein report the first synthesis of four potential process impurities generated in the production of pazopanib. The structure of these impurities were synthesized and characterized by 1H NMR, 13C NMR and HRMS data. The possible formation mechanisms of these impurities were also elucidated. These findings should be useful for the quality control of pazopanib in manufacture.
Asunto(s)
Inhibidores de la Angiogénesis/química , Contaminación de Medicamentos , Inhibidores de Proteínas Quinasas/química , Pirimidinas/química , Sulfonamidas/química , Indazoles , Espectroscopía de Resonancia Magnética/métodos , Control de CalidadRESUMEN
OBJECTIVE: To evaluate the therapeutic effects of laparoscopic Roux-en-Y gastric bypass (LRYGB) and laparoscopic duodenal-jejunal bypass with sleeve gastrectomy (SADJB-SG) in patients with type 2 diabetes mellitus and a low body mass index (BMI) of 25-27.5. METHODS: Thirty-one type 2 diabetic patients with a BMI of 25-27.5 underwent bariatric surgeries in the General Hospital of Guangzhou Military Command between August, 2013 and August, 2015. The patients receiving LRYGB (17 cases) and SADJB-SG (14 cases) were compared for physical indexes, glucose metabolism and of pancreatic islet function at 1 year after the surgeries. RESULTS: No mortality occurred in the patients after the operations. At 1 year after the operation, the patients in LRYGB group showed significant improvements in body weight, BMI, glycated hemoglobin (HbA1c), fasting plasma glucose (FPG), oral glucose tolerance test 2 h (OGTT2h), C-peptide, fasting insulin (FINS), and postprandial 2 hour insulin (2 hPINS) (P<0.05); in SADJB-SG group, significant improvements were observed in the body weigh, BMI, HbA1c, FPG, OGTT2h, and FINS after the operation (P<0.05). The postoperative improvements in body weigh, BMI, HbA1c, FPG, OGTT2h, C-peptide, and 2hPINS were comparable between SADJB-SG group and LRYGB group (P>0.05), but the incidence of postoperative anastomotic ulcer was lower in SADJB-SG group. CONCLUSION: SADJB-SG and LRYGB produce similar therapeutic effects in type 2 diabetic patients with a low BMI, but SADJB-SG is associated with a low incidence of postoperative complications and is therefore more suitable in such patients.