WO2015150921A3 - Methods for treating prostate cancer - Google Patents

Methods for treating prostate cancer Download PDF

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Publication number
WO2015150921A3
WO2015150921A3 PCT/IB2015/001187 IB2015001187W WO2015150921A3 WO 2015150921 A3 WO2015150921 A3 WO 2015150921A3 IB 2015001187 W IB2015001187 W IB 2015001187W WO 2015150921 A3 WO2015150921 A3 WO 2015150921A3
Authority
WO
WIPO (PCT)
Prior art keywords
prostate cancer
treating prostate
subject
androgen receptor
methods
Prior art date
Application number
PCT/IB2015/001187
Other languages
French (fr)
Other versions
WO2015150921A2 (en
Inventor
Xavier SALVATELLA
Eva DE MOL
Carlos W. BERTONCINI
Christopher T.W. PHANG
Iain J. MCEWAN
Antoni RIERA
Original Assignee
Fundacio Institut De Recerca Biomedica (Irb Barcelona)
Institucio Catalana De Recerca I Estudis Advancats
University Court Of The University Of Aberdeen
Unversitat De Barcelona
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Fundacio Institut De Recerca Biomedica (Irb Barcelona), Institucio Catalana De Recerca I Estudis Advancats, University Court Of The University Of Aberdeen, Unversitat De Barcelona filed Critical Fundacio Institut De Recerca Biomedica (Irb Barcelona)
Publication of WO2015150921A2 publication Critical patent/WO2015150921A2/en
Publication of WO2015150921A3 publication Critical patent/WO2015150921A3/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/433—Thidiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/574—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/57407—Specifically defined cancers
    • G01N33/57434—Specifically defined cancers of prostate
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/74—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving hormones or other non-cytokine intercellular protein regulatory factors such as growth factors, including receptors to hormones and growth factors
    • G01N33/743—Steroid hormones
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/705—Assays involving receptors, cell surface antigens or cell surface determinants
    • G01N2333/72—Assays involving receptors, cell surface antigens or cell surface determinants for hormones
    • G01N2333/723—Steroid/thyroid hormone superfamily, e.g. GR, EcR, androgen receptor, oestrogen receptor
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/10—Screening for compounds of potential therapeutic value involving cells

Abstract

A method for inhibiting activity of the human androgen receptor in a cell, and a method for treating prostate cancer in a subject in need thereof, using a molecule which specifically inhibits interaction of amino acids 433-438 of the N-terminal domain of the receptor with the RAP74 subunit of TFIIF. A method of inhibiting androgen receptor activity in a cell, and a method for treating prostate cancer in a subject in need thereof, using an inhibitor of the phosphorylation of one or more residues of the N-terminal domain of the androgen receptor selected from the group consisting of: Ser422, Ser424, Ser426, Ser430, Ser431, Ser432, Thr435 and Thr438. A method of diagnosing a subject having, or at risk of having, castration-resistant prostate cancer, comprising determining the phosphorylation status of one or more of residues Ser422, Ser424, Ser426, Ser430, Ser431, Ser432, Thr435 and Thr438.
PCT/IB2015/001187 2014-04-03 2015-04-03 Methods for treating prostate cancer WO2015150921A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201461974822P 2014-04-03 2014-04-03
US61/974,822 2014-04-03

Publications (2)

Publication Number Publication Date
WO2015150921A2 WO2015150921A2 (en) 2015-10-08
WO2015150921A3 true WO2015150921A3 (en) 2016-03-10

Family

ID=53761431

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2015/001187 WO2015150921A2 (en) 2014-04-03 2015-04-03 Methods for treating prostate cancer

Country Status (1)

Country Link
WO (1) WO2015150921A2 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019023654A2 (en) * 2017-07-28 2019-01-31 Massachusetts Institute Of Technology Discovery of small molecules that target the androgen receptor and uses thereof
WO2019023651A2 (en) 2017-07-28 2019-01-31 Massachusetts Institute Of Technology Small molecule modulators of the androgen receptor

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050054663A1 (en) * 2003-08-13 2005-03-10 Bennett Christina N. GSK-3 inhibitors
WO2006018633A1 (en) * 2004-08-17 2006-02-23 Imperial Innovations Limited Use of gsk-3 inhibitors for the treatment of prostate cancer

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050054663A1 (en) * 2003-08-13 2005-03-10 Bennett Christina N. GSK-3 inhibitors
WO2006018633A1 (en) * 2004-08-17 2006-02-23 Imperial Innovations Limited Use of gsk-3 inhibitors for the treatment of prostate cancer

Non-Patent Citations (7)

* Cited by examiner, † Cited by third party
Title
ALISON J. HOLE ET AL: "Comparative Structural and Functional Studies of 4-(Thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 Inhibitors Suggest the Basis for Isotype Selectivity", JOURNAL OF MEDICINAL CHEMISTRY, vol. 56, no. 3, 20 December 2012 (2012-12-20), US, pages 660 - 670, XP055145617, ISSN: 0022-2623, DOI: 10.1021/jm301495v *
E. A. MOSTAGHEL ET AL: "Molecular Pathways: Targeting Resistance in the Androgen Receptor for Therapeutic Benefit", CLINICAL CANCER RESEARCH, vol. 20, no. 4, 15 February 2014 (2014-02-15), US, pages 791 - 798, XP055220529, ISSN: 1078-0432, DOI: 10.1158/1078-0432.CCR-12-3601 *
MANUJ TANDON ET AL: "New Pyrazolopyrimidine Inhibitors of Protein Kinase D as Potent Anticancer Agents for Prostate Cancer Cells", PLOS ONE, vol. 8, no. 9, 23 September 2013 (2013-09-23), pages e75601, XP055222794, DOI: 10.1371/journal.pone.0075601 *
OUMATA N ET AL: "Roscovitine-Derived, Dual-Specificity Inhibitors of Cyclin-Dependent Kinases and Casein Kinases 1", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 51, no. 17, 11 September 2008 (2008-09-11), pages 5229 - 5242, XP002544873, ISSN: 0022-2623, [retrieved on 20080813], DOI: 10.1021/JM800109E *
QING ZHU ET AL: "Suppression of glycogen synthase kinase 3 activity reduces tumor growth of prostate cancer in vivo", PROSTATE., vol. 71, no. 8, 1 June 2011 (2011-06-01), US, pages 835 - 845, XP055222884, ISSN: 0270-4137, DOI: 10.1002/pros.21300 *
RAYMOND J. ANDERSEN ET AL: "Regression of Castrate-Recurrent Prostate Cancer by a Small-Molecule Inhibitor of the Amino-Terminus Domain of the Androgen Receptor", CANCER CELL, vol. 17, no. 6, 1 June 2010 (2010-06-01), US, pages 535 - 546, XP055223053, ISSN: 1535-6108, DOI: 10.1016/j.ccr.2010.04.027 *
TIMOTHY C. THOMPSON: "Grappling with the Androgen Receptor: A New Approach for Treating Advanced Prostate Cancer", CANCER CELL, vol. 17, no. 6, 1 June 2010 (2010-06-01), US, pages 525 - 526, XP055220515, ISSN: 1535-6108, DOI: 10.1016/j.ccr.2010.05.018 *

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