Processing

Please wait...

Settings

Settings

Goto Application

1. WO2020229974 - MACROCYCLIC CHELATORS AND METHODS OF USE THEREOF

Publication Number WO/2020/229974
Publication Date 19.11.2020
International Application No. PCT/IB2020/054381
International Filing Date 08.05.2020
IPC
C07D 413/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
C07D 413/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
14containing three or more hetero rings
A61K 31/4427 2006.01
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
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
A61K 51/04 2006.01
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
04Organic compounds
A61K 51/10 2006.01
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
04Organic compounds
08Peptides, e.g. proteins
10Antibodies or immunoglobulins; Fragments thereof
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
CPC
A61K 51/025
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
025inorganic Tc complexes or compounds
A61K 51/0482
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
0474complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group
0482chelates from cyclic ligands, e.g. DOTA
A61K 51/1027
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
08Peptides, e.g. proteins ; , carriers being peptides, polyamino acids, proteins
10Antibodies or immunoglobulins; Fragments thereof ; , the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody
1027against receptors, cell-surface antigens or cell-surface determinants
A61K 51/1093
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
08Peptides, e.g. proteins ; , carriers being peptides, polyamino acids, proteins
10Antibodies or immunoglobulins; Fragments thereof ; , the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody
1093conjugates with carriers being antibodies
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07D 413/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
Applicants
  • JANSSEN BIOTECH, INC. [US]/[US]
Inventors
  • SALTER, Rhys
  • DUDKIN, Vadim
  • SONG, Fengbin
  • ZHANG, Wei
  • GOLDBERG, Shalom
  • KEITH, John
Agents
  • SHIRTZ, Joseph F.
  • HORNINGER, Lisa Mead
Priority Data
62/846,04410.05.2019US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) MACROCYCLIC CHELATORS AND METHODS OF USE THEREOF
(FR) CHÉLATEURS MACROCYCLIQUES ET LEURS PROCÉDÉS D'UTILISATION
Abstract
(EN)
Macrocyclic chelators (I) for chelation of alpha-emitting radiometal ions, such as actinium-225 are provided. Also provided are radiometal complexes containing an alpha-emitting radiometal ion bound to the macrocyclic chelator via coordinate bonding, and radioimmunoconjugates containing the radiometal complexes covalently linked to a targeting ligand, such as an antibody or antigen binding fragment thereof. The radioimmunoconjugates can be produced by click chemistry reactions. Methods of using the radiocomplexes and radioimmunoconjugates for selectively targeting neoplastic cells for radiotherapy and for treating neoplastic diseases and disorders are also described.
(FR)
L'invention concerne des chélateurs macrocycliques (I) pour la chélation d'ions radiométalliques à émission alpha, tels que l'actinium-225. L'invention concerne également des complexes radiométalliques contenant un ion radiométallique à émission alpha lié au chélateur macrocyclique par liaison de coordination, et des radioimmunoconjugués contenant les complexes radiométalliques liés de manière covalente à un ligand de ciblage, tel qu'un anticorps ou un fragment de liaison à l'antigène de celui-ci. Les radioimmunoconjugués peuvent être produits par des réactions de chimie click. L'invention concerne également des procédés d'utilisation des radiocomplexes et des radioimmunoconjugués pour cibler sélectivement des cellules néoplasiques pour la radiothérapie et pour traiter des maladies et des troubles néoplasiques.
Latest bibliographic data on file with the International Bureau