MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER HAFTUNG
发明人:
HENRY YU,LIZBETH CELESTE DESELM
申请号：
ARP130100516
公开号：
AR090103A1
申请日:
2013.02.21
申请国别(地区):
AR
年份:
2014
代理人:
摘要：
a. A is the compound of equation (1) of phenyl or 2,3-dihydro-indol-1,6-di Y L, each of which is not replaced by OA or is replaced by OA alone； X is Hal, and refers to the tar of 1,2,3 or 4 C atoms； l 1 is (ch832222) - 83451 NR o (ch.83222)；NH (CH₂) ₙ,OCH CHOH NHCO (CH)CO (CH) NRUh...(CH₂)ₙCONR¹,O (CH) CONRNR CONR CHR CONRSo8322； NR 1 (ch83222). - 8346conr 1 u (ch832222) - 8346nr 1； LZ means o (ch832222)(CH₂) ₙNR¹CO, O (CH₂) ₚNR¹CO, CHR⁵NR¹CO or CHR³NR⁴CO； R¹ denotes H or methyl； R² denotes piperidinyl, piperazinyl, pyrrolidinyl, morpholinyl, 2,3-dihydropyrazolyl, 1,2-dihydro-pyridyl or tetrahydropyranyl, each of which is unsubstituted or mono- or disubstituted with A and / or = O； R³ and R⁴ together denote an alkylene chain having 2, 3 or 4 CH₂ groups；R830909 refers to a or bencilo； a refers to unbundled tar or bulk material with 1-10 C atoms, wherein 1-7 H atoms can be replaced by F and / or 1 or 2 non adjacent CH and / or ch83222 groups can be replaced by O or N； Hal refers to F, Cl, Br or I； n refers to 0, 1, 2, 3 or 4； P refers to 1, 2, 3 or 4； and its solution, salt, 6. Acceptable Dow and stereoisomers of drugs, including mixtures in various proportions. They are Syk inhibitors that, among other things, can be used to treat rheumatoid arthritis.Compuestos de la fórmula (1) en donde el anillo A denota fenileno o 2,3-dihidro-indol-1,6-diílo, cada uno de los cuales no está sustituido o está monosustituido con OA； X denota Hal； Y denota alquilo que tiene 1, 2, 3 ó 4 átomos de C； L¹ denota (CH₂)ₙNR¹CO, (CH₂)ₙ, NH(CH₂)ₙ, OCH₂CHOH, NHCO(CH₂)ₙ, CO(CH₂)ₙNR¹, CONR², (CH₂)ₙCONR¹, O(CH₂)ₚCONR¹, NR¹CONR³CHR⁴CONR¹, SO₂NR¹(CH₂)ₚCONR¹ u O(CH₂)ₚNR¹CO； L² denota O(CH₂)ₚ, (CH₂)ₙNR¹CO, O(CH₂)ₚNR¹CO, CHR⁵NR¹CO o CHR³NR⁴CO； R¹ denota H o metilo； R² denota piperidinilo, piperazinilo, pirrolidinilo, morfolinilo, 2,3-dihidro-pirazolilo, 1,2-dihidro-piridilo o tetrahidropiranilo, cada uno de los cuales no está sustituido o está mono- o disustituido con A y/u =O； R³ y R⁴ denotan juntos
