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US 2006/0154872 A1Published application
Hemiasterlin derivatives and uses thereof
AssigneeEisai Co., Ltd.
InventorsSilvio Campagna, Francis Fang, James Kowalczyk, Shawn Schiller, Boris Seletsky, Mark Spyvee, Hu Yang
Life of this patent
Estimating the term…
Abstract
The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1-R7, X1, X2, R, Q, and n are as defined herein.
Claims20
1-55. (canceled)
An intermediate having the structure:
- wherein g is 1, 2, 3 or 4;
- L is CRL1RL2, wherein each occurrence of RL1, RL2 and RL3 is independently hydrogen or an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl or heteroaryl moiety;
- each occurrence of RG1, RM1 and RM2 is each independently hydrogen or an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl or heteroaryl moiety;
- wherein any two adjacent RL1, RL2, RL3, RG1, RM1 or RM2 groups, taken together, form a substituted or unsubstituted alicyclic or heteroalicyclic moiety containing 3-6 atoms or an aryl or heteroaryl moiety;
- R2 is hydrogen, —(C═O)Rc or an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl or heteroaryl moiety;
- wherein each occurrence of RC is independently hydrogen, OH, ORD, or an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl or heteroaryl moiety;
- wherein RD is an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl or heteroaryl moiety;
- and
- R6 is hydrogen, —(C═O)RE or an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl or heteroaryl moiety, wherein each occurrence of RE is independently hydrogen, OH, ORF, or an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl or heteroaryl moiety;
- wherein RF is an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl or heteroaryl moiety;
- wherein at least one of R2, R6, RG1, RM1 and RM2 is not hydrogen or an aliphatic, alicyclic or aryl moiety.
8 more elements
An intermediate having the structure:
- wherein Rx1 and Rx2 are independently hydrogen, aliphatic, alicyclic or aryl;
- g is 1, 2, 3 or 4;
- L is CRL1RL2, wherein each occurrence of RL1, RL2 and RL3 is independently hydrogen or an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl or heteroaryl moiety;
- each occurrence of RG1, RM1 and RM2 is each independently hydrogen or an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl or heteroaryl moiety;
- wherein any two adjacent RL1, RL2, RL3, RG1, RM1 or RM2 groups, taken together, form a substituted or unsubstituted alicyclic or heteroalicyclic moiety containing 3-6 atoms or an aryl or heteroaryl moiety;
- R2 is hydrogen, —(C═O)RC or an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl or heteroaryl moiety;
- wherein each occurrence of RC is independently hydrogen, OH, ORD, or an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl or heteroaryl moiety;
- wherein RD is an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl or heteroaryl moiety;
- and
- R6 is hydrogen, —(C═O)RE or an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl or heteroaryl moiety, wherein each occurrence of RE is independently hydrogen, OH, ORF, or an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl or heteroaryl moiety;
- wherein RF is an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl or heteroaryl moiety;
- wherein at least one of R2, R6, RG1, Rx1, Rx2, RM1 and RM2 is not hydrogen or an aliphatic, alicyclic or aryl moiety.
9 more elements
Dependencies are inferred from the claim text.