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US 7,888,351 B2Granted
Organic compounds
AssigneeNovartis AG
InventorsDaniel Kaspar Baeschlin, Garry Fenton, Kenji Namoto, Nils Ostermann, Richard Sedrani, Finton Sirockin
Life of this patent
Estimating the term…
Abstract
The present invention relates to compounds of the formula; and their use in therapy.
Claims14
A compound of Formula (I):
- wherein
- the asterisk * designates a chiral centre of (R) or (S) configuration;
- V is absent or is ethylene;
- W is —C(O)— or —S(O)l—;
- X is a linker having 1 to 12 in-chain atoms and comprising one or more linkages selected from —O—, —C(O)—, —S(O)l—, —N(R9)— and hydrocarbylene optionally substituted with 1, 2, 3, 4 or 5 R11;
- Y is a linker selected from —O—, —N(R9)—, —C(O)—, —C(O)O—, —C(O)N(R9)—, —S(O)l— and S(O)lN(R9)—;
- R1 is selected from hydrogen;
- —N(R9)(R10) hydrocarbyl optionally substituted with 1, 2, 3, 4 or 5 R11;
- hydrocarbyloxy optionally substituted with 1, 2, 3, 4 or 5 R11;
- and
- —(CH2)k-heterocyclyl optionally substituted with 1, 2, 3, 4 or 5 R11;
- or, when Y is —N(R9)—, R1 and R9 taken together with the nitrogen atom to which they are attached may form a heterocycle, wherein said heterocycle is bound to X via said nitrogen atom and is optionally substituted with 1, 2, 3, 4 or 5 R11;
- R2 and R3 are each independently selected from R8, —OR8;
- —C(O)R8;
- —C(O)OR8 and —S(O)lR9;
- R4 and R5 are each independently selected from hydrogen, hydroxy, halogen and C1-6 alkyl optionally substituted with 1, 2, 3, 4 or 5 R11;
- R6 is aryl or heteroaryl, either of which is optionally-substituted with 1, 2, 3, 4 or 5 R11;
- R8 is selected from hydrogen;
- hydrocarbyl optionally substituted with 1, 2, 3, 4 or 5 R11;
- and —(CH2)k-heterocyclyl optionally substituted with 1, 2, 3, 4 or 5 R11;
- R9 and R10 are each independently selected from R8, —OR8, —C(O)R8, —C(O)OR8 and —S(O)lR8;
- or R9 and R10 taken together with a nitrogen atom to which they are attached form heterocyclyl optionally substituted with 1, 2, 3, 4 or 5 R11;
- each R11 is independently selected from R12;
- hydrocarbyl optionally substituted with 1, 2, 3, 4 or 5 R12;
- and —(CH2)k-heterocyclyl optionally substituted with 1, 2, 3, 4 or 5 R12;
- R12 is independently selected from halogen, trifluoromethyl, cyano, nitro, oxo, ═NR13, —OR13, —C(O)R13, —C(O)N(R13)R14, C(O)OR13, —OC(O)R13, —S(O)lR13, —S(O)lN(R13)R14, —N(R13)R14, —N(R13)N(R13)R14, —N(R13)C(O)R14 and —N(R13)S(O)lR13;
- R13 and R14 are each independently hydrogen or selected from hydrocarbyl and —(CH2)k-heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 substituents independently selected from oxo, halogen, cyano, amino, hydroxy, C1-6 alkyl and C1-6 alkoxy;
- k is 0, 1, 2, 3, 4, 5 or 6;
- and
- l is 0, 1 or 2;
- or a pharmaceutically acceptable salt or prodrug thereof.
28 more elements
Dependencies are inferred from the claim text.