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International application No. Applicant's or agent's file reference
PCT/IB2020/054381 JBI6072WOPCT1
International filing date (day/month/year) (Earliest) Priority Date (day/month/year)
08 May 2020 10 May 2019
FOR FURTHER ACTION: See Form PCT/ISA/220 as well as, where applicable, item 5 below.
This international search report has been prepared by this International Searching Authority and is transmitted to the applicant according to Article 18. A copy is being transmitted to the International Bureau.
It is also accompanied by a copy of each prior art document cited in this report.
1. Basis of the report
a. With regard to the language, the international search was carried out on the basis of:
the international application in the language in which it was filed.
a translation of the international application into                                          which is the language of a translation furnished for the purposes of international search (Rules 12.3(a) and 23.1(b)).
This international search report has been established taking into account the rectification of an obvious mistake authorized by or notified to this Authority under Rule 91 (Rule 43.6bis(a)).
1. With regard to any nucleotide and/or amino acid sequence disclosed in the international application, the international search was carried out on the basis of a sequence listing:
a. forming part of the international application as filed:
in the form of an Annex C/ST.25 text file.
on paper or in the form of an image file.
b. furnished together with the international application under PCT Rule 13ter.1(a) for the purposes of international search only in the form of an Annex C/ST.25 text file.
c. furnished subsequent to the international filing date for the purposes of international search only:
in the form of an Annex C/ST.25 text file (Rule 13ter.1(a)).
on paper or in the form of an image file (Rule 13ter.1(b) and Administrative Instructions, Section 713).
In addition, in the case that more than one version or copy of a sequence listing has been filed or furnished, the required statements that the information in the subsequent or additional copies is identical to that forming part of the application as filed or does not go beyond the application as filed, as appropriate, were furnished.
Additional comments:
2. Certain claims were found unsearchable
This international search report has not been established in respect of certain claims under Article 17(2)(a) for the following reasons:
Claims Nos.:
because they relate to subject matter not required to be searched by this Authority, namely:
Claims Nos.: 3(completely); 1, 2, 4-9, 11-28(partially)
because they relate to parts of the international application that do not comply with the prescribed requirements to such an extent that no meaningful international search can be carried out, specifically:
The claims 1-9, 11-14, 16-17 and 20-28 relate to an extremely large number of possible compounds and their use all linked to chelators (I) (as defined in claim 1). Claims 1-9, 11-14, 16-17 and 19-28 also contain the terms "linker" and/or "nucleophilic moiety" and/or "electrophilic moiety" and/or "targeting ligand" whose exact scope cannot be readily determined in product claims and in claims using those products. This is an attempt to define products by desired properties rather than the more precise method of using purely structural definitions. Support and disclosure in the sense of Article 6 and 5 PCT is to be found however for only a very small proportion of the compounds or uses claimed. The only claim where the four contested terms are fully defined is claim 10.
The non-compliance with the substantive provisions is to such an extent, that the search was performed taking into consideration the non-compliance in determining the extent of the search of the claims. (PCT Guidelines 9.19 and 9.23). Accordingly only claim 10 has been fully searched. Subject matter based on a combination of claims 4 and 5-7 (where R11 is adequately defined) and 9 (where L1 is adequately defined) has also been fully searchable. There is currently no claim corresponding to this scope.
The search of claims 1-2, 4-9, 11-28 was restricted to those claimed compounds/uses which appear to be supported and a generalisation of their structural formulae, i.e. where the chelator is as defined in claim 10 or a combination of claims 4 + (5-7) + 9. The remaining subject matter of claims has not been searched. Claim 3 was not searched at all since the restricted scope of the search only covers compounds where both A and B are a pyridine ring.
The examination of the scope of the claims, particularly with reference to novelty, inventive step and Articles 5/6 PCT has been limited to the searched scope.
The applicant's attention is drawn to the fact that claims relating to inventions in respect of which no international search report has been established need not be the subject of an international preliminary examination (Rule 66.1(e) PCT). The applicant is advised that the EPO policy when acting as an International Preliminary Examining Authority is normally not to carry out a preliminary examination on matter which has not been searched. This is the case irrespective of whether or not the claims are amended following receipt of the search report or during any Chapter II procedure. If the application proceeds into the regional phase before the EPO, the applicant is reminded that a search may be carried out during examination before the EPO (see EPO Guidelines C-IV, 7.2), should the problems which led to the Article 17(2) declaration be overcome.
Claims Nos.:
because they are dependent claims and are not drafted in accordance with the second and third sentences of Rule 6.4(a).
3. Unity of invention is lacking
4. Title of the invention
The text is approved as submitted by the applicant.
The text has been established by this Authority to read as follows:
5. Abstract
The text is approved as submitted by the applicant.
The text has been established, according to Rule 38.2, by this Authority as it appears in Box No. IV. The applicant may, within one month from the date of mailing of this international search report, submit comments to this Authority.

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.

6. Drawings
The figure of the drawings to be published with the abstract is Figure No. ____________
as suggested by the applicant.
as selected by this Authority, because the applicant failed to suggest a figure.
as selected by this Authority, because this figure better characterizes the invention.
none of the figures is to be published with the abstract.


     C07D 413/06 (2006.01)i; C07D 413/14 (2006.01)i; A61K 31/4427 (2006.01)i; A61K 51/04 (2006.01)i; A61K 51/10 (2006.01)i; A61P 35/00 (2006.01)i
According to International Patent Classification (IPC) or to both national classification and IPC


Minimum documentation searched (classification system followed by classification symbols):
Documentation searched other than minimum documentation to the extent that such documents are included in the fields searched:
Electronic data base consulted during the international search (name of data base and, where practicable, search terms used):
EPO-Internal, WPI Data


Category* Citation of document, with indication, where appropriate, of the relevant passages Relevant to claim No.
WO 2020106886 A1 (UNIV CORNELL [US]) 28 May 2020 (2020-05-28)
claim 1
WO 2018183906 A1 (UNIV CORNELL [US]) 04 October 2018 (2018-10-04)
cited in the application
claim 1
NIKKI A. THIELE ET AL, "An Eighteen-Membered Macrocyclic Ligand for Actinium-225 Targeted Alpha Therapy", ANGEWANDTE CHEMIE, INTERNATIONAL EDITION,Vol. 56, No. 46, 16 October 2017 (2017-10-16), page 14712-14717,
cited in the application
the whole document
WO 2018187631 A1 (UNIV CORNELL [US]) 11 October 2018 (2018-10-11)
paragraph [0170] - paragraph [0172]; claim 1
W. F. MAGUIRE ET AL, "Efficient 1-Step Radiolabeling of Monoclonal Antibodies to High Specific Activity with 225Ac for -Particle Radioimmunotherapy of Cancer", THE JOURNAL OF NUCLEAR MEDICINE,Vol. 55, No. 9, 30 June 2014 (2014-06-30), page 1492-1498,
the whole document
ADRIÁN ROCA-SABIO ET AL, "Macrocyclic Receptor Exhibiting Unprecedented Selectivity for Light Lanthanides", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY,Vol. 131, No. 9, 11 March 2009 (2009-03-11), page 3331-3341,
cited in the application
the whole document
Special categories of cited documents:
document defining the general state of the art which is not considered to be of particular relevance
document cited by the applicant in the international application
earlier application or patent but published on or after the international filing date
document which may throw doubts on priority claim(s) or which is cited to establish the publication date of another citation or other special reason (as specified)
document referring to an oral disclosure, use, exhibition or other means
document published prior to the international filing date but later than the priority date claimed
later document published after the international filing date or priority date and not in conflict with the application but cited to understand the principle or theory underlying the invention
document of particular relevance; the claimed invention cannot be considered novel or cannot be considered to involve an inventive step when the document is taken alone
document of particular relevance; the claimed invention cannot be considered to involve an inventive step when the document is combined with one or more other such documents, such combination being obvious to a person skilled in the art
document member of the same patent family


Patent document cited in search report Publication date
Patent family member(s) Publication date
WO 2020106886 A1
28 May 2020
US 2020157087 A1
WO 2020106886 A1
21 May 2020
28 May 2020
WO 2018183906 A1
04 October 2018
AU 2018243682 A1
CA 3058454 A1
CN 110573186 A
EP 3600452 A1
JP 2020515596 A
KR 20190139222 A
WO 2018183906 A1
17 October 2019
04 October 2018
13 December 2019
05 February 2020
28 May 2020
17 December 2019
04 October 2018
WO 2018187631 A1
11 October 2018
AU 2018249559 A1
CA 3058663 A1
CN 110612126 A
EP 3609541 A1
JP 2020516611 A
KR 20190129931 A
WO 2018187631 A1
31 October 2019
11 October 2018
24 December 2019
19 February 2020
11 June 2020
20 November 2019
11 October 2018
Name and mailing address of the ISA/:
European Patent Office
P.B. 5818, Patentlaan 2, 2280 HV Rijswijk,
Telephone No. (+31-70)340-2040
Facsimile No. (+31-70)340-3016
Date of the actual completion of the international search:
25 June 2020
Date of mailing of the international search report:
02 July 2020
Authorized officer:
Gettins, Marc
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