308348-93-8Relevant articles and documents
Synthesis method of copanlisib intermediate methyl 2-aminopyrimidine-5-carboxylate
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Paragraph 0016; 0022-0029, (2021/05/12)
The invention provides a synthetic method of a copanlisib intermediate methyl 2-aminopyrimidine-5-carboxylate, which comprises the following specific reaction steps: reacting sodium methoxide, ethyl formate and methyl 3,3-dimethoxypropionate in a methanol solvent at room temperature for 5 hours, then adding guanidine hydrochloride, conducting reacting at 50-55 DEG C for 2 hours, conducting cooling to room temperature after the reaction is completed, and conducting filtering and drying to obtain methyl 2-aminopyrimidine-5-carboxylate. The invention solves the problems of tedious reaction, high-risk raw material need, much waste liquid and waste water generated in the production process and the like in the existing reaction of the copanlisib intermediate methyl 2-aminopyrimidine-5-carboxylate, and provides a novel synthetic method of the copanlisib intermeidate methyl 2-aminopyrimidine-5-carboxylate, and the preparation method is simple, safe and controllable in reaction process, cheap and easily available in raw materials, high in yield, less in generated three wastes and the like.
COMBINATION THERAPY WITH A PHOSPHOINOSITIDE 3-KINASE INHIBITOR WITH A ZINC BINDING MOIETY
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Paragraph 0088; 0094, (2020/04/09)
The invention provides a method of treating cancer in a subject in need thereof, comprising administering to the subject: (a) a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein R is hydrogen or an acyl group; and (b) a PD-1 signaling inhibitor; wherein the compound of Formula I or pharmaceutically acceptable salt thereof and the PD-1 signaling inhibitor are administered in amounts which in combination are therapeutically effective. The invention further provides a pharmaceutical composition comprising a compound of Formula I or a pharmaceutically acceptable salt thereof, a PD-1 signaling inhibitor and a pharmaceutically acceptable carrier or excipient.
New tetrahydropyrido pyrimidinecarboxylic compound or salt thereof
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Paragraph 0171, (2016/10/08)
To provide a compound having an inhibitory activity for an androgen receptor. A tetrahydropyridopyrimidine compound represented by the following general formula (I) or a pharmaceutically acceptable thereof (in the formula, X and R are as defined in the specification).