Patent number: 9701678
Abstract: Hsp90 inhibitors having are provided having the formula: (I) with a 2?,4?,5?-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4? and 5? positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2-alkyl, COO-alkyl, KH2, OH, CN, SO2X5, NO2, NO, C?SR2NSO2X5, C?OR2, where X5 is F, NH2, alkyl or H, and R2 is alkyl, NH2, NH-alkyl or O-alkyl, C1 to C6 alkyl or alkoxy; or wherein X1 has the formula —O—(CH2)n—O—, wherein n is an integer from 0 to 2, preferably 1 or 2, and one of the oxygens is bonded at the 5?-position and the other at the 4?-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.
Type:
Grant
Filed:
April 18, 2014
Date of Patent:
July 11, 2017
Assignee:
Memorial Sloan Kettering Cancer Center
Inventors:
Gabriela Chiosis, Huazhong He, Laura Llauger-Bufi, Joungnam Kim, Steve M. Larson, Peter Smith-Jones
Publication number: 20140227183
Abstract: Hsp90 inhibitors having are provided having the formula: (I) with a 2?,4?,5?-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4? and 5? positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2alkyl, COO-alkyl, KH2, OH, CN, SO2X5, NO2, NO, C?SR2 NSO2X5, C?OR2, where X5 is F, NH2, alkyl or H, and R2 is alkyl, NH2, NH-alkyl or O-alkyl, C1 to C6 alkyl or alkoxy; or wherein X1 has the formula —O—(CH2)n—O—, wherein n is an integer from 0 to 2, preferably 1 or 2, and one of the oxygens is bonded at the 5?-position and the other at the 4?-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.
Type:
Application
Filed:
April 18, 2014
Publication date:
August 14, 2014
Applicant:
MEMORIAL SLOAN KETTERING CANCER CENTER
Inventors:
Gabriela Chiosis, Huazhong He, Laura Llauger-Bufi, Joungnam Kim, Steve M. Larson, Peter Smith-Jones
Patent number: 7834181
Abstract: Hsp90 inhibitors are provided having the formula: with a 2?,4?,5?-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4? and 5? positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2?alkyl, COO-alkyl, KH2, OH, CN, SO2X5, NO2, NO, C?SR2 NSO2X5, C?OR2, where X5 is F, NH2, alkyl or H, and R2 is alkyl, NH2, NH-alkyl or O-alkyl, C1 to C6 alkyl or alkoxy; or wherein X1 has the formula —O—(CH2)n—O—, wherein n is an integer from 0 to 2, preferably 1 or 2, and one of the oxygen is bonded at the 5?-position and the other at the 4?-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.
Type:
Grant
Filed:
February 1, 2006
Date of Patent:
November 16, 2010
Assignee:
Slaon-Kettering Institute for Cancer Research
Inventors:
Gabriela Chiosis, Huazhong He, Laura Llauger-Bufi, Joungnam Kim, Steve M. Larson, Peter Smith-Jones
Publication number: 20080253965
Abstract: Hsp90 inhibitors are provided having the formula: with a 2?,4?,5?-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4? and 5? positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2. alkyl, COO-alkyl, KH2, OH, CN, SO2X5, NO2, NO, C?SR2 NSO2X5, C?OR2, where X5 is F, NH2, alkyl or H, and R2 is alkyl, NH2, NH-alkyl or O-alkyl, C1 to C6 alkyl or alkoxy; or wherein X1 has the formula -0-(CH2)n-0-, wherein n is an integer from O to 2, preferably 1 or 2, and one of the oxygens is bonded at the 5?-position and the other at the 4?-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.
Type:
Application
Filed:
February 1, 2006
Publication date:
October 16, 2008
Applicant:
SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
Inventors:
Gabriela Chiosis, Huazhong He, Laura Llauger-Bufi, Joungnam Kim, Steve M. Larson, Peter Smith-Jones