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1. US20180327368 - Heterocyclic compounds for cancer imaging and treatment and methods for their use

Office United States of America
Application Number 15543389
Application Date 13.01.2016
Publication Number 20180327368
Publication Date 15.11.2018
Grant Number 10654811
Grant Date 19.05.2020
Publication Kind B2
IPC
C07D 249/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
249Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
02not condensed with other rings
041,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07D 233/60
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
233Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54having two double bonds between ring members or between ring members and non-ring members
56with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
60with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
A61K 31/4164
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
41641,3-Diazoles
A61K 31/4192
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
41921,2,3-Triazoles
A61K 31/5375
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
53751,4-Oxazines, e.g. morpholine
CPC
A61K 31/4164
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
41641,3-Diazoles
C07D 249/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
249Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
02not condensed with other rings
041,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
A61K 31/4192
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
41921,2,3-Triazoles
A61K 31/5375
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
53751,4-Oxazines, e.g. morpholine
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 51/0453
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51Preparations containing radioactive substances for use in therapy or testing in vivo
02characterised by the carrier ; , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
04Organic compounds
041Heterocyclic compounds
044having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
0453having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
Applicants The University of British Columbia
British Columbia Cancer Agency Branch
Inventors Raymond John Andersen
Javier Garcia Fernandez
Kunzhong Jian
Marianne Dorothy Sadar
Nasrin R. Mawji
Carmen Adriana Banuelos
Agents Cooley LLP
Title
(EN) Heterocyclic compounds for cancer imaging and treatment and methods for their use
Abstract
(EN)

Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1, R2, R3, R11a, R11b, R11c, R11d, X, n1, n2, and n3 are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.

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