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Inhibitors of Tyrosine Kinase (SYK) containing aminopiridina Spleen
专利权人:
MERCK SHARP & DOHME CORP.
发明人:
申请号:
ARP120101538
公开号:
AR086236A1
申请日:
2012.05.02
申请国别(地区):
AR
年份:
2013
代理人:
摘要:
It also provides Pharmaceutical compositions comprising these compounds and processes for using the compounds for treating diseases or conditions mediated by the Spleen Tyrosine Kinase (SYK).Claim 1: a compound of formula (1) or one of its pharmaceutically acceptable salts, in which: R1 is selected from the group consisting of: (i) c1-3 alkyl; (ii) fluoroalquilo; (iii) - ch2or1a A1A, which is selected from the group consisting of H and alkyl C1 - 6; (iv) - N (r1b) 2In which each occurrence of r1b is selected from the group consisting of H, alkyl or two r1b 3 C1 - together with the N Atom are United to form a group of formula (2), in which R is 1, 2, 3 or 4; (V) - or - (alkyl C1 3); (vi) - N (H) C (o) - (alkyl c1-3); (vii) Halo; (viii) and (IX) (H; ILO; R2 is - O - O - (c1-3 alkyl) - N (2, 2a)N (2a) - C (o) - R2B or - F; in the 2a is selected from the group consisting of H, alkyl c1-3 alkyl; and R2B is C1 - 6; R3 is co2r3a ch2co2r3a -, -, - ch2ch2co2r3a, tetrazol, - C (o) n (r3b) 2 - CH2OH, h, alkyl, Halo, C1 - 6 - Oh -, - or - (c1-3 alkyl) - N (r3b) 2, - CN, - C (o) n (H) s (OR) 2r3c, - C (o) - N (H) (R3D), - C (o) N (H) or (C R3A,)- P (o) (or3b) 2 or - B (OH) 2; where R3A is selected from the group which consists of H and alkyl C1 - 6; where each r3b is selected independently from the group consisting of H, alkyl c1-3; where R3C is selected from the group consisting of alkyl C1 - 3 - 3 fluoroalquilo cycloalkyl, C1, C3 - 6 And phenylWhere the phenyl is replaced without replacing or with one or two c1-3 alkyl; where R3D is selected from the group consisting of - CN, - or - (alkyl c1-3) and tetrazol; R4 is co2r4a ch2co2r4a ch2ch2co2r4a tetrazol,, -,, - C (o) n (r4b) 2 - CH2OH, h, alkyl, Halo, C1 - Oh, - 6, - or - (c1-3 alkyl) - N (r4b) 2 CN C (o) n (H) s (OR) 2r4c, - C (o) - N (H) (R4D), C (o) n (H) C (o) R4A,- P (o) (or4b) 2 or - B (OH) 2; where R4A is selected from the group consisting of H, alkyl and C1 - 6; where each r4b is selected independently among the group
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