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US 2017/0320867 A1Published application
Heteroaromatic compounds as btk inhibitors
AssigneeBoehringer Ingelheim International GmbH
InventorsJoerg Martin BENTZIEN, Angela Kay BERRY, Todd BOSANAC, Michael Jason BURKE, Darren Todd DISALVO, Joshua Courtney HORAN, Shuang LIANG, Can MAO, Wang MAO, Yue SHEN, Fariba SOLEYMANZADEH, Renee M. ZINDELL
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Abstract
The present invention encompasses compounds of the formula (I) wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.
Claims21
A compound of the formula (I)
- wherein
- A ring is:
- R1 is N(R3)2 or hydrogen;
- Cy is aryl or heteroaryl each is substituted by R2 and optionally substituted by halogen, halo C1 alkyl, C1-4 alkyl and C1-4 alkoxy;
- R2 is chosen from:
- L-Ar, C1-6 alkyl and C1-6 alkoxy, each Ar, C1-6 alkyl and C1-6 alkoxy are optionally substituted by halogen, halo C1-4 alkyl, C1 alkyl, R3—S(O)m—, —CN, —C(O)—N(R3)2 or C1-4 alkoxy;
- L is a linker chosen from a bond, O, >C(O), —(CH2)n—, —O—(CH2)n—, —N(R3)—, —N(R3)—(CH2)n—, —(CH2)n—N(R3)—, —C(O)—N(R3)—, —C(O)—N(R3)—(CH2)n—, —N(R3)—C(O)—N(R3)—, —N(R3)—C(O)—, —S(O)m—N(R3)— and —N(R3)—S(O)m—, wherein the —CH2— in each L can have 1-2 hydrogens replaced by C1-3 alkyl, said C1-3 alkyl groups can optionally cyclize to form a C3-6 cycloalkyl ring;
- Ar is carbocycle, heterocycyl or heteroaryl;
- X1 is a linker chosen from a bond, —(CH2)n—;
- Y is chosen from C7-C10 spirocycle optionally containing 0-1 ring nitrogen atoms, a nitrogen containing mono- or bi-cyclic heterocycle, carbocycle, aryl, each substituted by one R4;
- R4 is
- wherein R5 cannot be hydrogen,
- each n is independently 1-4;
- each m is independently 0-2;
- each R3 is independently chosen from hydrogen or C1-4 alkyl;
- each R5 is independently chosen from hydrogen, C1-4 alkyl, C1-4 alkoxy, C1-4 alkylC1-4 alkoxy, —(CH2)n-heterocycle and heterocycle each heterocycle optionally substituted by halogen, OH or R3—S(O)m—;
- each group defined above for Cy, R1-R5, X1 and Y can be where possible partially or fully halogenated;
- or a pharmaceutically acceptable salt thereof.
15 more elements
A compound chosen from:
- or the pharmaceutically acceptable salts thereof.
A compound chosen from:
- or the pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.