332013-26-0

Upstream product

• 332012-40-5 Telatinib 
• 75-75-2 methanesulfonic acid 
• 332013-42-0 ethyl 2-methylaminocarbonyl-4-picolinate 

Relevant academic research and scientific papers

Industrial production method tela for Nepal of methanesulfonic acid

The invention provides an industrial production method of telatinib mesylate. According to the method, 2-methylamino carbonyl-4-picolinic acid ethyl ester is used as a raw material, sodium borohydride is used as a reducing agent, or sodium borohydride and Lewis acid are selected for catalytic reduction, 2-methylamino carbonyl-4-pyridinemethanol is obtained after reduction in an organic solvent, an intermediate 2-methylamino carbonyl-4-pyridinemethanol hydrochloride monohydrate is obtained through salt formation, the 2-methylamino carbonyl-4-pyridinemethanol hydrochloride monohydrate and 4-chloro-anilino-7-chlorofuro[2,3-d]pyridazine have a condensation reaction under the action of potassium tert-butoxide to form telatinib free alkali, the telatinib free alkali reacts with methane sulfonic acid to form salt finally, and the telatinib mesylate is obtained through cooling and crystallization. The process operation is simple and safe, reaction conditions are mild, the obtained product is high in purity and meets the quality requirement, and the method is suitable for large-scale industrial production.

SUBSTITUTED PYRIDINES AND PYRIDAZINES WITH ANGIOGENESIS INHIBITING ACTIVITY

Substituted pyridines and pyridazines having angiogenesis inhibiting activity and generalized structural formula (I) wherein the ring containing A, B, D, E, and L is phenyl or a nitrogen-containing heterocycle; groups X and Y may be any of a variety of defined linking units; R and R may be defined independent substituents or together may be a ring-defining bridge; ring J may be an aryl, pyridyl, or cycloalkyl group; and G groups may be any of a variety of defined substituents. Pharmaceutical compositions containing these materials, and methods of treating a mammal having a condition characterized by abnormal angiogenesis or hyperpermeability processes using these materials are also disclosed.

COMPOUNDS FOR TREATING PULMONARY HYPERTENSION

The present invention relates to pharmaceutical compositions and combinations for treating, preventing or managing pulmonary hypertension comprising small molecule heterocyclic pharmaceuticals, and more particularly, substituted pyridines and pyridazines optionally combined with at least one additional therapeutic agent.

Substituted pyridines and pyridazines with angiogenesis inhibiting activity

Substituted pyridazines having angiogenesis inhibiting activity and the generalized structural formula wherein the ring containing A, B, D, E, and L is phenyl or a nitrogen-containing heterocycle; groups X and Y may be any of a variety of defined linking units; R1and R2may be defined independent substituents or together may be a ring-defining bridge; ring J may be an aryl, pyridyl, or cycloalkyl group; and G groups may be any of a variety of defined substituents. Pharmaceutical compositions containing these materials, and methods of treating a mammal having a condition characterized by abnormal angiogenesis or hyperpermiability processes using these materials are also disclosed.