Invention Grant
- Patent Title: Phenylanine derivatives
- Patent Title (中): 苯胺衍生物
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Application No.: US11749499Application Date: 2007-05-16
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Publication No.: US07825216B2Publication Date: 2010-11-02
- Inventor: Terrence R. Burke, Jr. , Yang Gao , Zhu-jun Yao , Dajun Yang
- Applicant: Terrence R. Burke, Jr. , Yang Gao , Zhu-jun Yao , Dajun Yang
- Applicant Address: US DC Washington US DC Washington
- Assignee: The United States of America as represented by the Department of Health and Human Services,Georgetown University
- Current Assignee: The United States of America as represented by the Department of Health and Human Services,Georgetown University
- Current Assignee Address: US DC Washington US DC Washington
- Agency: Leydig, Voit & Mayer, Ltd.
- Main IPC: C07K2/00
- IPC: C07K2/00

Abstract:
The present invention provides phenylalanine derivatives that inhibit SH2 domain binding with a phosphoprotein. These derivatives include compounds of the formula: W—Y-(AA)n-Z wherein n is 0 to 15; Y is a phenylalanyl radical having a phenyl ring, an amine end, and a carboxyl end, the phenyl ring having one or more substituents, e.g., hydroxyl, carboxyl, formyl, carboxyalkyl, carboxyalkyloxy, dicarboxyalkyl, dicarboxyalkyloxy, dicarboxyhaloalkyl, dicarboxyhaloalkyloxy, and phosphonoalkyl, or phosphonohaloalkyl; W is a moiety attached to the nitrogen of Y and is, e.g., alkylcarbonyl, oxalyl, alkylaminooxalyl, arylaminooxalyl, arylalkylaminooxalyl, or alkoxyoxalyl; AA is an amino acid, the amine end of which is attached to the carboxyl end of Y; and Z is an arylalkylamino or arylheterocyclyl alkylamino; or a salt thereof; with the proviso that W is not arylalkylamino when the phenyl ring of phenylalanyl contains a phosphonoalkyl or phosphonohaloalkyl substituent at a position para to the alkylamido group and the ortho and meta positions are unsubstituted. The present invention further provides precursors suitable for preparing the phenylalanine derivatives and a method for the preparation of the precursors. The present invention further provides conjugates comprising a precursor and a conjugant that are covalently linked. These conjugates have biological and/or pharmacological properties.
Public/Granted literature
- US20070219194A1 PHENYLALANINE DERIVATIVES Public/Granted day:2007-09-20
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