Patents by Inventor Gabriela Chiosis

Gabriela Chiosis has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Publication number: 20140045867
    Abstract: The disclosure relates to Compounds of Formula (1) : and pharmaceutically acceptable salts thereof wherein Z1, Z2, Z3, Xa, Xb, Xc, Y, X2, and X4 are as defined herein, compositions comprising an effective amount of a Compound of Formula (1) or a pharmaceutically acceptable salt thereof, and methods to treat or prevent a condition, such as cancer which overexpresses Her-kinases, comprising administering to an patient in need thereof a therapeutically effective amount of a Compound of Formula (1) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 5, 2012
    Publication date: February 13, 2014
    Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
    Inventors: Tony Taldone, Gabriela Chiosis
  • Publication number: 20120252818
    Abstract: The present subject matter relates to a compound represented by the general formula (I) or (I?) or a pharmacologically acceptable salt thereof; pharmaceutical compositions containing at least one of these compounds; methods of making at least one of these compounds; methods of using at least one of these compounds for treating and/or preventing various cancers and/or proliferation disorders; methods of using at least one of these compounds for monitoring the effectiveness of an anticancer therapy against various cancers. In one embodiment, the subject matter relates to compounds that bind with a level of specificity to heat shock protein 70 (Hsp70). In another embodiment, the subject matter relates to compounds that bind with a level of specificity to inhibit both heat shock protein 70 (Hsp70) and heat shock cognate protein 70 (Hsc70).
    Type: Application
    Filed: August 17, 2010
    Publication date: October 4, 2012
    Applicant: MEMORIAL SLOAN-KETTERING CANCER CENTER
    Inventors: Gabriela Chiosis, Tony Taldone, Anna Rodina, Pallav Patel, Yanlong Kang
  • Publication number: 20120208806
    Abstract: The present application provides compounds useful in the inhibition of Hsp90, and hence in the treatment of disease.
    Type: Application
    Filed: October 7, 2010
    Publication date: August 16, 2012
    Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
    Inventors: Gabriela Chiosis, Tony Taldone, Weilin Sun
  • Publication number: 20110312980
    Abstract: Purine scaffold Hsp90 inhibitors are useful in therapeutic applications and as radioimaging ligands.
    Type: Application
    Filed: July 6, 2011
    Publication date: December 22, 2011
    Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
    Inventor: Gabriela Chiosis
  • Publication number: 20110104054
    Abstract: Hsp90 inhibitors having 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: November 4, 2010
    Publication date: May 5, 2011
    Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
    Inventors: Gabriela Chiosis, Huazhong He, Laura Llauger-bufi, Joungnam Kim, Steven 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 ā€”Oā€”(CH2)nā€”Oā€”, 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: 20090298857
    Abstract: Treatment of neurodegenerative diseases is achieved using small molecule purine scaffold compounds that inhibit Hsp90 and that possess the ability to cross the blood-brain barrier or are other wise delivered to the brain.
    Type: Application
    Filed: July 2, 2007
    Publication date: December 3, 2009
    Applicants: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH, THE ROCKEFELLER UNIVERSITY
    Inventors: Gabriela Chiosis, Paul Greengard, Fei Dou, Wenjie Luo
  • Patent number: 7439359
    Abstract: Structural differences in binding pockets of members of the HSP90 family can be exploited to achieve differential degradation of kinases and other signaling proteins through the use of designed small molecules which interact with the N-terminal binding pocket with an affinity which is greater than ADP and different from the ansamycin antibiotics for at least one species of the HSP90 family. Moreover, these small molecules can be designed to be soluble in aqueous media, thus providing a further advantage over the use of ansamycin antibiotics. Pharmaceutical compositions can be formulated containing a pharmaceutically acceptable carrier and a molecule that includes a binding moiety which binds to the N-terminal pocket of at least one member of the HSP90 family of proteins. Such binding moieties were found to have antiproliferative activity against tumor cells which are dependent on proteins requiring chaperones of the HSP90 family for their function.
    Type: Grant
    Filed: November 1, 2001
    Date of Patent: October 21, 2008
    Assignee: Sloan-Kettering Institute for Cancer Research
    Inventors: Gabriela Chiosis, Neal Rosen
  • 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
  • Publication number: 20070178537
    Abstract: A method for evaluation of molecules to identify those that can act as therapeutic inhibitors of Hsp90 makes use of a fluorescence polarization (FP) assay and a cell based assay, either individually or in combination. The FP assay uses a fluorescently-labeled Hsp90 binding agent and measure the degree of fluorescence polarization relative to the standard. A decrease in the degree of polarization indicates that fluorescently-labeled Hsp90 binding agent has been wholly or partially displaced by a candidate molecule, and identifies the molecule as having activity as an inhibitor of Hsp90. The cell based assay tests for decrease is an Hsp90-dependent activity of normal or tumor cells.
    Type: Application
    Filed: June 30, 2004
    Publication date: August 2, 2007
    Applicant: Sloan-Kettering Institute for Cancer Research
    Inventors: Gabriela Chiosis, Neal Rosen, Henri Huezo
  • Patent number: 6953861
    Abstract: The present invention relates to pyrrolidine compounds of the general structure: where n is an integer 1-6 and R is hydrogen or a C1 to C6 straight chain or branched alkyl group, and wherein when n=1, R=CH3 or H, useful for re-sensitizing vancomycin resistant Gram-positive bacteria in which resistance results from the conversion of an amide bond to an ester bond on the cell wall peptide precursors of the bacteria.
    Type: Grant
    Filed: March 18, 2004
    Date of Patent: October 11, 2005
    Assignees: The Trustees of Columbia University in the City of New York, The Rockefeller University
    Inventors: Gabriela Chiosis, Ivo G. Boneca, W. Clark Still
  • Publication number: 20040180814
    Abstract: The present invention relates a method for re-sensitizing vancomycin resistant Gram-positive bacteria in which resistance results from the conversion of an amide bond to an ester bond in the cell wall peptide precursors of the bacteria which comprises using an antibacterial amount of vancomycin or a homolog of vancomycin and an amount of an agent effective to selectively cleave the ester bond so as to thereby re-sensitize vancomycin resistant bacteria.
    Type: Application
    Filed: March 18, 2004
    Publication date: September 16, 2004
    Applicants: The Trustees of Columbia University in the of City of NewYork, The Rockefeller University
    Inventors: Gabriela Chiosis, Ivo G. Boneca, W. Clark Still
  • Publication number: 20040102458
    Abstract: Structural differences in binding pockets of members of the HSP90 family can be exploited to achieve differential degradation of kinases and other signaling proteins through the use of designed small molecules which interact with the N-terminal binding pocket with an affinity which is greater than ADP and different from the ansamycin antibiotics for at least one species of the HSP90 family. Moreover, these small molecules can be designed to be soluble in aqueous media, thus providing a further advantage over the use of ansamycin antibiotics. Pharmaceutical compositions can be formulated containing a pharmaceutically acceptable carrier and a molecule that includes a binding moiety which binds to the N-terminal pocket of at least one member of the HSP90 family of proteins. Such binding moieties were found to have antiproliferative activity against tumor cells which are dependent on proteins requiring chaperones of the HSP90 family for their function.
    Type: Application
    Filed: May 1, 2003
    Publication date: May 27, 2004
    Inventors: Gabriela Chiosis, Neal Rosen
  • Patent number: 6734165
    Abstract: The present invention relates a method for re-sensitizing vancomycin resistant Gram-positive bacteria in which resistance results from the conversion of an amide bond to an ester bond in the cell wall peptide precursors of the bacteria which comprises using an antibacterial amount of vancomycin or a homolog of vancomycin and an amount of an agent effective to selectively cleave the ester bond so as to thereby re-sensitize vancomycin resistant bacteria.
    Type: Grant
    Filed: August 23, 2001
    Date of Patent: May 11, 2004
    Assignees: The Trustees of Columbia University in the City of New York, The Rockefeller University
    Inventors: Gabriela Chiosis, Ivo G. Boneca, W. Clark Still
  • Publication number: 20030125372
    Abstract: The present invention relates a method for re-sensitizing vancomycin resistant Gram-positive bacteria in which resistance results from the conversion of an amide bond to an ester bond in the cell wall peptide precursors of the bacteria which comprises using an antibacterial amount of vancomycin or a homolog of vancomycin and an amount of an agent effective to selectively cleave the ester bond so as to thereby re-sensitize vancomycin resistant bacteria.
    Type: Application
    Filed: August 23, 2001
    Publication date: July 3, 2003
    Inventors: Gabriela Chiosis, Ivo G. Boneca, W. Clark Still