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US 6,838,558 B2Granted
Pyrazolobenzodiazepines
AssigneeHoffmann-La Roche Inc.
InventorsQingjie Ding, Jin-Jun Liu, Giacomo Pizzolato, Chung-Chen Wei, Peter Michael Wovkulich
Life of this patent
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Abstract
Disclosed are novel pyrazolobenzodiazepines having the formula These compounds are useful in the preparation of the pyrazolobenzodiazepines of formula I, which are useful in the treatment and control of solid tumors.
Claims26
A compound of formula
- wherein:
- R1 is selected from the group consisting of
- —H,
- —NO2,
- —CN,
- -halogen,
- -lower alkyl which is straight-chained and which optionally may be substituted by the group consisting of —OH and halogen,
- —OR5,
- —R6—OR7,
- —COOR7,
- —CONR8R9,
- —NR10R11,
- —NHCOR12, and
- —NHSO2R13;
- R2 and R4 are each independently selected from the group consisting of
- —H,
- -halogen,
- —NO2,
- —CF3, and
- —straight chained lower alkyl;
- R5 is selected from lower alkyl which optionally may be substituted by halogen;
- R6 is selected from —(CH2)1-6—;
- R7 is selected from the group consisting of —H and lower alkyl;
- R8 and R9 are each independently selected from the group consisting of —H and -lower alkyl which itself optionally may be substituted by —OH and —NH2;
- alternatively, R8 and R9 may form a 5- or 6-membered heterocycle which optionally may be substituted by the group consisting of —OH, —NH2, and lower alkyl;
- R10, R11 and R12 are each independently selected from the group consisting of —H and lower alkyl;
- R13 is selected from the group consisting of lower alkyl which optionally may be substituted by the group consisting of halogen and —NR14R15;
- and
- R14 and R15 are each independently selected from the group consisting of —H and lower alkyl which optionally may be substituted halogen, or alternatively, —NR14R15 is a heterocycle.
26 more elements
A compound of formula
- wherein:
- R1 is selected from the group consisting of
- —H,
- —NO2,
- —CN,
- -halogen,
- -lower alkyl which is straight-chained and which optionally may be substituted by the group consisting of —OH and halogen,
- —OR5,
- —R6—OR7,
- —COOR7,
- —CONR8R9,
- —NR10R11,
- —NHCOR12, and
- —NHSO2R13;
- R2 and R4 are each independently selected from the group consisting of
- —H,
- -halogen,
- —NO2,
- —CF3, and
- -straight chained lower alkyl;
- R3 is selected from the group consisting of
- —H,
- -lower alkyl which optionally may be substituted by —OH,
- —OR9, F, and aryl,
- -cycloalkyl,
- -aryl,
- -heterocycle,
- -heteroaryl,
- —COOR7
- —CN,
- -alkenyl,
- —CONR8R9, and
- -alkynyl;
- R5 is selected from lower alkyl which optionally may be substituted by halogen;
- R6 is selected from —(CH2)1-6—;
- R7 is selected from the group consisting of —H and lower alkyl;
- R8 and R9 are each independently selected from the group consisting of —H and —lower alkyl which itself optionally may be substituted by —OH and —NH2;
- alternatively, R8 and R9 may form a 5- or 6-membered heterocycle which optionally may be substituted by the group consisting of —OH, —NH2, and lower alkyl;
- R10, R11 and R12 are each independently selected from the group consisting of —H and lower alkyl;
- R13 is selected from the group consisting of lower alkyl which optionally may be substituted by the group consisting of halogen and —NR14R15;
- and
- R14 and R15 are each independently selected from the group consisting of —H and lower alkyl which optionally may be substituted halogen, or alternatively, —NR14R15 is a heterocycle.
39 more elements
Dependencies are inferred from the claim text.