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US 7,803,956 B2Granted
Benzofuran derivatives useful for treating hyper-proliferative disorders
AssigneeBayer Pharmaceuticals Corporation
InventorsChengzhi Zhang, Jacques Dumas, Gaetan H. Ladouceur, Qian Zhao, Martin F. Hentemann, Sharad K. Verma, Qingming Zhu, Rico C. Lavoie, Jianmei Fan, Barton Phillips
Life of this patent
Estimating the term…
Abstract
The invention relates to novel benzofuran derivatives, processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disorders.
Claims19
A method of treating a hyper-proliferative disorder in a mammal, comprising administering to a mammal in need thereof an effective amount of a compound of formula (I)
- wherein
- Ar1 is selected from benzodioxolyl, pyrrolidinyl, pyridyl or pyridyl N-oxide, each optionally mono-substituted with C(O)NH2, halo, (C1-C3)alkoxy, amino, hydroxy(C1-C3)alkyl, or (C1-C3)alkyl optionally substituted with aminocarbonyl or (C1-C3)alkylcarbonylamino,
- a five-membered aromatic heterocycle optionally substituted with 1 or 2 substituents each independently selected from (C1-C3)alkyl, C(O)H, C(O)(C1-C3)alkyl, and halo, and
- phenyl optionally substituted with 1 or 2 substituents each selected independently from OH, —OCF3, CF3, CN, halo, NO2, NR5R5, NHC(O)R6, NHS(O)2R5, NHS(O)2NR5R5, S(O)nR8, 1C(O)R10, C(O)NH(C1-C3)alkoxy-(C1-C3)alkyl, C(O )NH(C3-C6)cycloalkyl, pyrrolidinonyl, imidazolinyl, imidazolidinonyl, (C1—C3)alkoxy optionally substituted with 1 or 2 OH groups, and (C1-C3)alkyl optionally mono-substituted with CN, OH, NR5R5, NHC(O)R6, NHS(O)2(C1-C3) alkyl, C(O)NR5R5, oxazolidinonyl, imidazolidinonyl optionally mono-substituted with (C1-C3) alkyl, pyrrolidinonyl optionally mono-substituted with (C1-C3)alkyl, a five-membered N containing heterocycle optionally mono-substituted with (C1-C3)alkyl, piperazinyl optionally mono-substituted with (C1-C3)alkyl, pyridyl optionally mono-substituted with CF3 or (C1-C3) alkoxy, thienyl optionally mono-substituted with C(O)(C1-C3)alkyl, or pyrimidinyl optionally mono-substituted with NRC[(C1-C3)alkyl]2;
- Ar2 is selected from benzodioxolyl, phenyl optionally substituted with 1 or 2 substituents each selected independently from (C1-C3)alkyl, (C1-C3)alkoxy, OH, NO2, CN, halo, and CF3, and pyridyl mono-substituted with (C1-C3)alkyl or CF3;
- R1, R2, and R3 are hydrogen;
- R4 is selected from hydrogen, (C1-C3)alkyl, (C1-C3)alkoxy, CN, and C(O)NHR5, wherein (C1-C3)alkyl can optionally be substituted with halo, (C1-C3)alkoxy, hydroxyalkylamino, alkoxyalkylamino;
- R5 is selected from H, (C3-C6)cycloalkyl, and (C1-C3)alkyl optionally substituted with 1 or 2 OH groups or mono-substituted with (C1-C3)alkoxy, (C1-C3)alkylamino, S(O)2(C1-C3) alkyl, or C(O)R7;
- R6 is selected from H, (C3-C6)cycloalkyl, (C1-C3)alkoxy, (C2-C6)alkenyl, CHF2, CF3,NHR5, and (C1-C3)alkyl optionally substituted with one or more substituents selected from Cl and F, or optionally mono-substituted with NH2 or NHC(O)(C1-C3)alkyl;
- R7 is selected from (C1-C3)alkoxy, (C2-C6)alkenyl, CHF2, CF3, (C3-C6)cycloalkyl, NR7-1R7-1, and (C1-C3)alkyl optionally substituted with one or more substituents selected from Cl and F, or mono-substituted with NHC(O)(C1-C3)alkyl or NH2, wherein R7-1 is hydrogen or (C1-C3)alkyl;
- R8 is selected from (C1-C3)alkyl and NR9R9;
- R9 is selected from H and (C1-C3)alkyl optionally mono-substituted with (C1-C3)alkoxy, or aminocarbonyl, or substituted with 1 or 2 OH groups;
- R10 is selected from H, (C1-C3)alkoxy, NHR9, and (C1-C3)alkyl optionally mono-substituted with pyrrolidinyl, morpholinyl, pyridinyl, piperazinyl optionally substituted with (C1-C3)alkyl, or piperidinyl optionally substituted with (C1-C3)alkyl;
- n is 0, 1, or 2;
- or a pharmaceutically acceptable salt thereof.
12 more elements
Dependencies are inferred from the claim text.