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Derivatives of N - (pyridin-2-yl) - pyrimidine - 4 containing an Amine Group sulphoximine
专利权人:
BAYER PHARMA AKTIENGESELLSCHAFT
发明人:
LÜCKING, ULRICH,BÖHNKE DR. NIELS,SCHOLZ, DR. ARNE,LIENAU, DR. PHILIP,SIEMEISTER, DR. GERHARD,BÖMER, DR. ULF,KOSEMUND, DR. DIRK,BOHLMANN, ROLF,ZORN, DR. LUDWING
申请号:
CU20150051
公开号:
CU20150051A7
申请日:
2015.05.15
申请国别(地区):
CU
年份:
2015
代理人:
摘要:
The invention relates to N - (pyridine-2-il) pyridine-4-amino sulfur dioxide derivative, which contains a group of sulfur, and proposes a general (I) formula,(f) Among them, R1, R2, R3, R4 and R5 are defined in the claim as drugs that can be used to treat and / or prevent high-risk disorders, viral infections and / or cardiovascular diseases. In addition, the invention relates to intermediate compounds of formulas (5) and (6),1. Formula compounds (I) that facilitate the preparation of R1, R2, R3, R4 and R5 as defined in the claim, and procedures for the preparation of these formula compounds or their salt solutions, salts and / or solutions in which a reaction of formula compound (5) occurs,1. Use trifluoroethane and 1,3-dibromo-5,5-dimethylhydrazine, and use an alkali salt as a formula compound in the cyclic ether as a solvent (6);Or oxidize a formula compound (6),An alkaline acid salt containing a C1-C2-C (O) -C1-C2- tar plasma as a solvent and, if such a three fluorine ethyl compound is present, removed to produce a formula compound (I),In the case where R5 is hydrogen (frumula gap) or a substitute, a formula compound (6) is oxidized in a solvent with peroxysulfuric acid based oxidant, selected from c1-c3-tar-oh, water and N, n-dicarboxylic acid amine, or a mixture of both, to form a formula (I) compound,Where R5 is hydrogen.La invención se relaciona con derivados de N-(piridin-2-il)pirimidin-4-amina disustituida que contienen un grupo sulfoximina y que presentan la fórmula general (I), (ESPACIO PARA LA FÓRMULA) donde R1, R2, R3, R4 y R5 son como se definen en las reivindicaciones, que son útiles como medicamentos para el tratamiento y/o la profilaxis de los trastornos hiperproliferativos, enfermedades infecciosas inducidas por virus y/o de las enfermedades cardiovasculares. Adicionalmente, la invención se refiere a compuestos intermediarios de fórmulas (5) y (6), útiles para preparar los compuestos de fórmula (I) (ESPACIO PARA LAS FÓRMULAS) donde R1, R2, R3, R
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