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Heteroaryl compounds as inhibitors of BTK and Uses Thereof
专利权人:
MERCK PATENT GMBH
发明人:
申请号:
ARP140103948
公开号:
AR098136A1
申请日:
2014.10.21
申请国别(地区):
AR
年份:
2016
代理人:
摘要:
This refers to compounds of pyridine, pyrazine, pyrimidine, and pyridazine hydrochloride and pharmaceutically acceptable compositions thereof, useful as inhibitors of BTK. They are useful to treat ailments such as Asthma and Allergy.Claim 1: Compound of formula (1) or a pharmaceutically acceptable Salt thereof, in which the ring is a heteroaryl Ring of 6 members that have 1 or 2 nitrogens, selected from pyridine, pyrazine and pyrimidine; R u00b2, pyridazine hydrochloride, is selected from Halogen, - R, - haloal Chilo - or, -, - CN, - no u2082 so u2082r Sr., -, -, - C (o) - R, co u2082r, - C (o) n (R) - u2082, NRC (NRC) - R (o) n (R) - u2082, nrso u2082r,Or - N (R) u2082; r u00b3 is selected from Halogen, R -, or haloalquilo, -, -, - CN, - no u2082 so u2082r Sr., -, -, - C (o) - R, co u2082r, - C (o) n (R) - u2082, NRC (or R) NRC, - (o) n (R) u2082 nrso u2082r, -, or - N (R) u2082; at least one of R u00b2 or r u00b3 is - C (o) n (R) u2082, or CN; each R is independently Hydrogen, aliphatic c u2081 u208b u2086 c u2083 u208b u2081 u2080, aryl ring, a carboc u00edclico partially saturated or unsaturated 3 - 8 members,A Heterocyclic Ring of 3 - 7 members that have 1-4 heteroatoms selected irrespective of Nitrogen, Oxygen, sulfur, or a monocyclic heteroaryl Ring of 5 - 6 members that have 1-4 heteroatoms selected from Oxygen, nitrogen Regardless,Or Sulfur; each of which is optionally substituted; or two groups R on the same Atom are taken together with the Atom to which they are United to form a c u2083 u208b u2081 u2080 aryl ring, a carboc u00edclico partially saturated or unsaturated 3 - 8 members, a Heterocyclic Ring of 3 - 7 Members that have 1-4 heteroatoms selected irrespective of Nitrogen, Oxygen or SulfurMonocyclic heteroaryl Ring or a 5 - 6 members that have 1-4 heteroatoms selected irrespective of Nitrogen, Oxygen or Sulfur; each of which is optionally substituted; l is a divalent Group selected from c u2081 u208b u2086 c u2083 u208b u2081 u2080 aliphati
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