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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
Legal status (The legal status 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 status listed.)
Ceased
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
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Unversitat De Barcelona
Institucio Catalana de Recerca i Estudis Avancats ICREA
Fundacio Privada Institut de Recerca Biomedica IRB
University of Aberdeen
Original Assignee
Unversitat De Barcelona
Institucio Catalana de Recerca i Estudis Avancats ICREA
Fundacio Privada Institut de Recerca Biomedica IRB
University of Aberdeen
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 Unversitat De Barcelona, Institucio Catalana de Recerca i Estudis Avancats ICREA, Fundacio Privada Institut de Recerca Biomedica IRB, University of Aberdeen filed Critical Unversitat De Barcelona
Publication of WO2015150921A2 publication Critical patent/WO2015150921A2/en
Publication of WO2015150921A3 publication Critical patent/WO2015150921A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/433Thidiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/574Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/57407Specifically defined cancers
    • G01N33/57434Specifically defined cancers of prostate
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/74Chemical 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
    • G01N33/743Steroid hormones
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/705Assays involving receptors, cell surface antigens or cell surface determinants
    • G01N2333/72Assays involving receptors, cell surface antigens or cell surface determinants for hormones
    • G01N2333/723Steroid/thyroid hormone superfamily, e.g. GR, EcR, androgen receptor, oestrogen receptor
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00Screening for compounds of potential therapeutic value
    • G01N2500/10Screening for compounds of potential therapeutic value involving cells

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Public Health (AREA)
  • Biomedical Technology (AREA)
  • Veterinary Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Physics & Mathematics (AREA)
  • Microbiology (AREA)
  • Analytical Chemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Biotechnology (AREA)
  • Food Science & Technology (AREA)
  • Cell Biology (AREA)
  • Biochemistry (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

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 Ceased 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 Ceased 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
WO2019023651A2 (en) 2017-07-28 2019-01-31 Massachusetts Institute Of Technology Small molecule modulators of the androgen receptor
WO2019023654A2 (en) * 2017-07-28 2019-01-31 Massachusetts Institute Of Technology Discovery of small molecules that target the androgen receptor and uses thereof

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 *

Also Published As

Publication number Publication date
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