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US 9,867,826 B2Granted
Heterocycles as modulators of kinase activity
AssigneeMerck Patent GmbH
InventorsRuoxi Lan, Xiaoling Chen, Yufang Xiao, Bayard R. Huck, Andreas Goutopoulos
Life of this patent
Estimating the term…
Abstract
The invention provides novel heterocyclic amines according to Formula (I) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
Claims12
A compound of Formula (I)
- wherein:
- RA and R1, together with the atoms to which each is attached, forms a 5-membered monocyclic heteroaryl ring having 1 nitrogen;
- which is optionally substituted;
- each R2 is independently Hal or A;
- A is unbranched or branched alkyl group having 1, 2, 3, 4, 5 of 6 C atoms in which 1-4 H atoms can be replaced, independently of each other, by Hal;
- R3 an unbranched or branched linear or mono- or bicyclic alkyl group having 1, 2, 3,4, 5, 6, 7, 8 or 9 C atoms, in which one or two CH2 groups may be replaced by an —O— or —NH— group, and/or in which one or two CH groups may be replaced by —N— and/or in which 1, 2 or 3 H atoms may be replaced by Hal or OH;
- or R3 is unbranched or branched alkyl group having 1, 2, 3, 4, 5 of 6 C atoms, which is substituted by a 3-6 membered heterocyclic ring, which may be further optionally substituted;
- R4 is C5-10 aryl, a 3-8 membered saturated or partially unsaturated carbocyclic ring, a 3-7 membered heterocylic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a 5-6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur;
- each of which is mono-, di- or trisubstituted by Hal, LA, OH, O(LA), NH2 and/or NH(LA), N(LA)2, NO2, CN, OCN, COOH, COO(LA), CONH2, CONH(LA), CON(LA)2, NHCO(LA), NHCONH(LA), NHCONH2, NHSO2(LA), CHO or CO(LA);
- LA is an unbranched or branched, saturated or partially unsaturated, linear hydrocarbon chain having 1, 2, 3 or 4 C atoms, wherein 1, 2 or 3 H atoms may be replaced by Hal;
- Hal is F, Cl, Br or I;
- and
- n is 1 or 2;
- or a pharmaceutically acceptable salt thereof.
11 more elements
Dependencies are inferred from the claim text.