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NZ784773B2 - G protein-coupled receptor (GPCR) modulation by imipridones - Google Patents
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NZ784773B2 - G protein-coupled receptor (GPCR) modulation by imipridones - Google Patents

G protein-coupled receptor (GPCR) modulation by imipridones

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Publication number
NZ784773B2
NZ784773B2 NZ784773A NZ78477317A NZ784773B2 NZ 784773 B2 NZ784773 B2 NZ 784773B2 NZ 784773 A NZ784773 A NZ 784773A NZ 78477317 A NZ78477317 A NZ 78477317A NZ 784773 B2 NZ784773 B2 NZ 784773B2
Authority
NZ
New Zealand
Prior art keywords
tumor
subject
use according
baseline
tumor burden
Prior art date
Application number
NZ784773A
Other versions
NZ784773A (en
Inventor
Joshua E Allen
Varun Vijay Prabhu
Martin Stogniew
Original Assignee
Oncoceutics Inc
Filing date
Publication date
Priority claimed from PCT/US2016/015817 external-priority patent/WO2016123571A1/en
Application filed by Oncoceutics Inc filed Critical Oncoceutics Inc
Priority claimed from NZ745425A external-priority patent/NZ745425A/en
Publication of NZ784773A publication Critical patent/NZ784773A/en
Publication of NZ784773B2 publication Critical patent/NZ784773B2/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • 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
    • A—HUMAN NECESSITIES
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    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—Ortho-condensed systems
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    • C12Q1/6876—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes
    • C12Q1/6883—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
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    • G01—MEASURING; TESTING
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    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
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    • G—PHYSICS
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    • 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
    • G01N33/68—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
    • G01N33/6872—Intracellular protein regulatory factors and their receptors, e.g. including ion channels

Abstract

Imipridones has been found to selectively modulate Class A G protein-coupled receptors (GPCRs), such as the D2-like subfamily of dopamine receptors, and to be useful for the treatment of conditions and disorders in need of such modulation, such as cancers, psychiatric disorders, and bacterial infections. In addition, methods of identifying whether a subject having these condition, is likely to be responsive to a treatment regimen, such as administration of an imipridone, are provided. Furthermore, methods of assessing the effectiveness of a treatment regimen, such as administration of an imipridone, monitoring, or providing a prognosis for a subject with these condition are also provided. In particular, the use of an imipridone (Formula I) in reducing tumor size relative to baseline of total tumor burden for a central nervous system cancer in a subject.

Claims (16)

1. A method of reducing tumor size relative to baseline of total tumor burden for a central s system cancer in a subject, said method comprising administering a compound of formula (1) or a pharmaceutically acceptable salt thereof to the subject, wherein the subject is a non-human.
2. Use of a compound of formula (1) or a pharmaceutically acceptable salt f in the manufacture of a medicament for reducing tumor size relative to baseline of total tumor burden for a central nervous system cancer in a human subject.
3. A method of reducing tumor burden relative to baseline of total tumor burden for a central nervous system cancer in a subject, said method comprising administering a compound of formula (1) or a pharmaceutically acceptable salt thereof to the subject, wherein the t is a non-human.
4. Use of a compound of a (1) 21625823_1 ters) P44343NZ01 or a ceutically acceptable salt thereof in the manufacture of a medicament for reducing tumor burden relative to baseline of total tumor burden for a l nervous system cancer in a human subject.
5. The method according to claim 1 or 3 or the use according to claim 2 or 4, wherein the tumor burden is ed by one or more of (a) reduction in tumor size relative to baseline of total tumor burden and (b) reduction in tumor volume relative to baseline.
6. The method or use ing to any one of claims 1 to 5, wherein the tumor burden and/or tumor size is measured with one or more of (a) CT scan and (b) MRI.
7. The method or use according to any one of claims 1 to 6, wherein the tumor burden and/or tumor size is measured after one or more treatment cycles.
8. The method or use according to any one of claims 1 to 7, wherein the tumor is meningioma, ependymoma, glioma, neuroblastoma or diffuse intrinsic e glioma.
9. The method or use according to any one of claims 1 to 8, wherein the tumor is a midline tumor.
10. The method or use according to any one of claims 1 to 9, wherein the tumor has a histone H3 mutation.
11. The method or use according to claim 10, wherein the histone H3 mutation is H3.3 K27M.
12. The method or use according to any one of claims 1 to 11, wherein the tumor is recurrent.
13. The method or use according to any one of claims 1 to 12, wherein the tumor is glioblastoma.
14. The method or use according to any one of claims 1, 2 or 5 to 13, wherein the tumor size is less than about 80%, less than about 60%, less than about 30%, less than about 20% or less than about 10% relative to baseline of total tumor burden in the subject.
15. The method or use according to any one of claims 1 to 14, wherein the pharmaceutically acceptable salt is a di-hydrochloride salt.
16. The method or use according to any one of claims 1 to 15, wherein the compound of formula (1), or a pharmaceutically acceptable salt f, is to be administered to the subject once every three weeks. 21625823_1 (GHMatters) P44343NZ01
NZ784773A 2017-01-30 G protein-coupled receptor (GPCR) modulation by imipridones NZ784773B2 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
PCT/US2016/015817 WO2016123571A1 (en) 2015-01-30 2016-01-29 7-benzyl-4-(2-methylbenzyl)-2,4,6,7,8,9-hexahydroimidazo [1,2-a]pyrido[3,4-e]pyrimidin-5(1h)-one, analogs and salts thereof and their use in therapy
US201662308325P 2016-03-15 2016-03-15
US201662425403P 2016-11-22 2016-11-22
NZ745425A NZ745425A (en) 2016-01-29 2017-01-30 G protein-coupled receptor (gpcr) modulation by imipridones

Publications (2)

Publication Number Publication Date
NZ784773A NZ784773A (en) 2025-05-02
NZ784773B2 true NZ784773B2 (en) 2025-08-05

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