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US 10,882,857 B2Granted
Bicyclic compounds as ATX inhibitors
AssigneeHoffmann-La Roche Inc.
InventorsJérôme Hert, Daniel Hunziker, Patrizio Mattei, Markus Rudolph, Petra Schmitz, Patrick Di Giorgio
Life of this patent
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Abstract
The invention provides novel compounds having the general formula (I) wherein R1, R2, Y, W, A, X, m and n are as defined herein, compositions including the compounds and methods of using the compounds.
Claims30
A compound of formula (II):
- wherein:
- R1 is selected from the group consisting of:
- i) phenyl substituted by R3, R4 and R5,
- ii) phenyl-C1-6-alkyl substituted by R3, R4 and R5,
- iii) phenoxy-C1-6-alkyl substituted by R3, R4 and R5,
- iv) phenyl-C2-6-alkenyl substituted by R3, R4 and R5,
- v) phenyl-C2-6-alkynyl substituted by R3, R4 and R5,
- vi) pyridinyl substituted by R3, R4 and R5,
- vii) pyridinyl-C1-6-alkyl substituted by R3, R4 and R5,
- viii) pyridinyl-C2-6-alkenyl substituted by R3, R4 and R5,
- ix) pyridinyl-C2-6-alkynyl substituted by R3, R4 and R5,
- x) thiophenyl substituted by R3, R4 and R5,
- xi) thiophenyl-C1-6-alkyl substituted by R3, R4 and R5,
- xii) thiophenyl-C2-6-alkenyl substituted by R3, R4 and R5, and
- xiii) thiophenyl-C2-6-alkynyl substituted by R3, R4 and R5;
- Y is selected from the group consisting of:
- x) C3-8-cycloalkyl-C1-6-alkyl,
- xi) C3-8-cycloalkyl-C1-6-alkoxy,
- xii) C3-8-cycloalkoxy,
- xiii) C3-8-cycloalkoxy-C1-6-alkyl,
- xiv) C1-6-alkylamino,
- xv) C1-6-alkylcarbonylamino,
- xvi) C3-8-cycloalkylcarbonylamino,
- xvii) C1-6-alkyltetrazolyl,
- xviii) C1-6-alkyltetrazolyl-C1-6-alkyl, and
- xix) heterocycloalkyl-C1-6-alkoxy;
- R4 and R5 are independently selected from the group consisting of:
- i) H,
- ii) halogen,
- iii) hydroxy,
- iv) cyano,
- v) C1-6-alkyl,
- vi) C1-6-alkoxy,
- vii) C1-6-alkoxy-C1-6-alkyl,
- viii) halo-C1-6-alkoxy,
- ix) halo-C1-6-alkyl,
- x) hydroxy-C1-6-alkyl,
- xi) C3-8-cycloalkyl,
- xii) C3-8-cycloalkyl-C1-6-alkyl,
- xiii) C3-8-cycloalkyl-C1-6-alkoxy,
- xiv) C3-8-cycloalkoxy,
- xv) C3-8-cycloalkoxy-C1-6-alkyl,
- xvi) C1-6-alkylcarbonylamino,
- xvii) C3-8-cycloalkylcarbonylamino,
- xviii) C1-6-alkyltetrazolyl,
- xix) C1-6-alkyltetrazolyl-C1-6-alkyl, and
- xx) heterocycloalkyl-C1-6-alkoxy;
- R6 is selected from the group consisting of:
- i) H,
- ii) C1-6-alkyl, and
- i) —OC(O)—, and
- ii) —C(O)—;
- A is selected from the group consisting of:
- i) —O—, and
- ii) —S—;
- X is selected from the group consisting of:
- i) —N—, and
- ii) —CH—;
- W is selected from the group consisting of:
- i) —C(O)—, and
- ii) —S(O)2—;
- R2 is selected from the ring systems O, AO, AW, AX, AY and AZ;
- R3 is selected from the group consisting of:
- i) halogen,
- ii) hydroxy,
- iii) cyano, C1-6-alkyl,
- iv) C1-6-alkoxy,
- v) C1-6-alkoxy-C1-6-alkyl,
- vi) halo-C1-6-alkoxy,
- vii) halo-C1-6-alkyl,
- viii) hydroxy-C1-6-alkyl,
- ix) C3-8-cycloalkyl,
- iii) C3-8-cycloalkyl;
- m is 1;
- n is 1 or 2;
- and
- r is 1, 2 or 3;
- or a pharmaceutically acceptable salt thereof.
75 more elements
Dependencies are inferred from the claim text.