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Aminopyrimidines as Syk inhibitors
专利权人:
MERCK SHARP & DOHME CORP.;Merck Canada Inc.
发明人:
ALTMANN, Michael D.,ANDRESEN, Brian M.,ARRINGTON, Kenneth L.,CHILDERS, Kaleen Konrad,DI FRANCESCO, Maria Emilia,DONOFRIO, Anthony,ELLIS, John Michael,FISCHER, Christian,GUERIN, David Joseph,HAIDLE, An
申请号:
ES10801736
公开号:
ES2609040T3
申请日:
2010.12.15
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound of formula (I) or a pharmaceutically acceptable salt thereof: ** Formula ** in which p is 0 to 4; q is 0, 1 or 2; Cy is selected from C4-7 cycloalkyl, oxetanyl, pyrrolidinyl, piperidinyl and azepanyl; R1 is selected from H, C1-4 alkyl, C1-4 haloalkyl, C3-6 cycloalkyl and C1-4 Oalkyl; R4 is selected from H, C1-4 alkyl and C3-4 cycloalkyl; Ry (a) is aminomethyl, OH, OCH3, OCH2CH2OH, F, CN, CO2Ra (a), CONRb (a) Rc (a), NRa (a) Ra (a), NHC (O) C1-3 alkyl (optionally substituted with OH), NHC (O) NH2, NHSO2NH2, NHSO2 C1-3alkyl or NHSO2haloalkyl C1-3; Rz (a) is selected from (A) C1-4 alkyl optionally substituted with one to three groups independently selected from OH, NH2, CN, CO2Ra (a) and CONH2, (B) C1-3 fluoroalkyl, (C) halogen, (D) CN, (E) C1-4alkyl (optionally substituted with one or two groups independently selected from ORa (a), CN, CO2Ra (a), CONRa (a) Ra (a) and NRa (a) Ra ( a)), (F) CO-phenyl (optionally substituted with one or two groups independently selected from ethynyl, CO2Ra (a), CN, F and OH), (G) C3-6 CO-cycloalkyl (optionally substituted with OH or CO2Ra (a)), (H) C0-3-CO2Ra (a), (I) -C (O) NRb (a) Rc (a), (J) -ORa (a), (K) -OC (O) Ra (a), (L) -NRb (a) Rc (a), (M) -NHC (O) C1-4 alkyl (optionally substituted with one to three OH or a CONRa (a) Ra (a )), (N) -NHSO2 C1-3alkyl, (O) -NHSO2NH2, (P) oxo, (Q) 1,3,4-oxadiazol-2 (3H) -one, (R) 1,2,4- oxadiazol-5 (4H) -one, (S) SO2NH2, (T) SO2 C1-3alkyl, (U) SO2haloalkyl C1-3 and (V) SO2Ph; Ra (a) is H or C1-4 alkyl; Rb (a) and Rc (a) are independently selected from (A) H, (B) C3-6 cycloalkyl optionally substituted with OH, (C) heteroaryl selected from imidazolyl, pyridyl and indolyl, (D) tetrahydrofuranyl, (E) benzyl, (F) phenyl optionally substituted with one or two groups independently selected from (CH2) 0-2OH and F, (G1) C1-4 alkyl and (G2) C1-4 haloalkyl, wherein (G1) and (G2) are each optionally substituted with one to three groups independently selected from (i) OH, (ii) C3-6 cycloalkyl optional
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