Alkylated piperazine compounds
AssigneeGenentech, Inc.
InventorsJames John Crawford, Wendy B. Young
Life of this patent
Estimating the term…
Abstract
Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating cancer mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of cancer in mammalian cells, or associated pathological conditions, are disclosed.
Claims13
A method of treating cancer comprising administering a pharmaceutical composition, which comprises a therapeutically effective amount of a Formula I compound and a pharmaceutically acceptable carrier, glidant, diluent, or excipient, to a patient with cancer, wherein the Formula I compound has the structure:
- or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein:
- R1, R2 and R3 are independently selected from H, F, Cl, —NH2, —NHCH3, —N(CH3)2, —OH, —OCH3, —OCH2CH3, —OCH2CH2OH, and C1-C3 alkyl;
- R4 is selected from H, F, Cl, CN, —CH2OH, —CH(CH3)OH, —C(CH3)2OH, —CH(CF3)OH, —CH2F, —CHF2, —CH2CHF2, —CF3, —C(O)NH2, —C(O)NHCH3, —C(O)N(CH3)2, —NH2, —NHCH3, —N(CH3)2, —NHC(O)CH3, —OH, —OCH3, —OCH2CH3, —OCH2CH2OH, cyclopropyl, cyclopropylmethyl, 1-hydroxycyclopropyl, imidazolyl, pyrazolyl, 3-hydroxy-oxetan-3-yl, oxetan-3-yl, and azetidin-1-yl;
- R5 is selected from —CH3, and —CH2CH3;
- n is 1, 2, 3, or 4;
- R6 is selected from H, —CH3, —CH2CH3, —CH2CH2OH, —NH2, and —OH;
- R7 is selected from the structures:
- where the wavy line indicates the site of attachment;
- R8 is selected from —CH3, —S(O)2CH3, cyclopropyl, azetidin-3-yl, oxetan-3-yl, and morpholin-4-yl;
- X1 is CR9 or N, where R9 is selected from H, F, Cl, —CH3, —CH2CH3, —CH2CH2OH, —NH2, —NHCH3, —N(CH3)2, —OH, —OCH3, —OCH2CH3, and —OCH2CH2OH;
- X2 is CR10 or N, where R10 is selected from H, —CH3, —CH2CH3, and —CH2CH2OH;
- and
- Y1 and Y2 are independently selected from CH and N, where Y1 and Y2 are not each N;
- wherein the cancer is a hematological malignancy.
Dependencies are inferred from the claim text.