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Extract from the Register of European Patents

EP About this file: EP4066896

EP4066896 - G9A INHIBITOR [Right-click to bookmark this link]
StatusRequest for examination was made
Status updated on  02.09.2022
Database last updated on 26.06.2024
FormerThe international publication has been made
Status updated on  04.06.2021
Most recent event   Tooltip28.02.2024Supplementary search reportpublished on 27.03.2024  [2024/13]
Applicant(s)For all designated states
RIKEN
2-1 Hirosawa
Wako-shi, Saitama 351-0198 / JP
For all designated states
Tokyo University of Pharmacy & Life Sciences
1432-1, Horinouchi
Hachioji-shi, Tokyo 192-0392 / JP
For all designated states
Microbial Chemistry Research Foundation
14-23, Kamiosaki 3-chome Shinagawa-ku
Tokyo 141-0021 / JP
[2022/40]
Inventor(s)01 / SUMIYA Tatsunobu
c/o Watarase Research Center, Kyorin
Pharmaceutical Co., Ltd.
1848, Nogi, Nogi-machi
Shimotsuga-gun, Tochigi 329-0114 / JP
02 / NISHIGAYA Yosuke
c/o Watarase Research Center, Kyorin
Pharmaceutical Co., Ltd.
1848, Nogi, Nogi-machi
Shimotsuga-gun, Tochigi 329-0114 / JP
03 / NAMIE Ryosuke
c/o Watarase Research Center, Kyorin
Pharmaceutical Co., Ltd.
1848, Nogi, Nogi-machi
Shimotsuga-gun, Tochigi 329-0114 / JP
04 / HASHIMOTO Noriaki
c/o Watarase Research Center, Kyorin
Pharmaceutical Co., Ltd.
1848, Nogi, Nogi-machi
Shimotsuga-gun, Tochigi 329-0114 / JP
05 / ITO Akihiro
c/o Tokyo University of Pharmacy and Life
Sciences
1432-1, Horinouchi
Hachioji-shi, Tokyo 192-0392 / JP
06 / SHIRAI Fumiyuki
c/o RIKEN
2-1, Hirosawa
Wako-shi, Saitama 351-0198 / JP
07 / KIKUZATO Ko
c/o RIKEN
2-1, Hirosawa
Wako-shi, Saitama 351-0198 / JP
08 / YOSHIDA Minoru
c/o RIKEN
2-1, Hirosawa
Wako-shi, Saitama 351-0198 / JP
 [2022/40]
Representative(s)J A Kemp LLP
80 Turnmill Street
London EC1M 5QU / GB
[2022/40]
Application number, filing date20893619.526.11.2020
[2022/40]
WO2020JP43966
Priority number, dateJP2019021399027.11.2019         Original published format: JP 2019213990
[2022/40]
Filing languageJA
Procedural languageEN
PublicationType: A1 Application with search report
No.:WO2021106988
Date:03.06.2021
Language:JA
[2021/22]
Type: A1 Application with search report 
No.:EP4066896
Date:05.10.2022
Language:EN
[2022/40]
Search report(s)International search report - published on:JP03.06.2021
(Supplementary) European search report - dispatched on:EP27.02.2024
ClassificationIPC:A61P7/00, A61P21/00, A61P25/00, A61P25/04, A61P29/00, A61P31/12, A61P33/06, A61P35/00, A61P35/02, A61P35/04, A61P43/00, C07D401/12, C07D401/14, C07D403/12, C07D405/12, C07D405/14, C07D417/12, C07D417/14, C07D471/04, C07D491/107, C07D209/42
[2022/40]
CPC:
A61P7/00 (EP); C07D209/42 (EP,US); A61P21/00 (EP);
A61P25/00 (EP); A61P25/04 (EP); A61P29/00 (EP);
A61P31/12 (EP); A61P33/06 (EP); A61P35/00 (EP);
A61P35/02 (EP); A61P35/04 (EP); A61P43/00 (EP);
C07D209/96 (EP); C07D213/74 (EP); C07D213/75 (EP);
C07D401/12 (EP,US); C07D401/14 (EP); C07D403/12 (EP,US);
C07D403/14 (EP); C07D405/12 (EP); C07D405/14 (EP);
C07D417/12 (EP); C07D417/14 (EP,US); C07D471/04 (EP,US);
C07D487/10 (EP); C07D491/107 (EP); Y02A50/30 (EP) (-)
Designated contracting statesAL,   AT,   BE,   BG,   CH,   CY,   CZ,   DE,   DK,   EE,   ES,   FI,   FR,   GB,   GR,   HR,   HU,   IE,   IS,   IT,   LI,   LT,   LU,   LV,   MC,   MK,   MT,   NL,   NO,   PL,   PT,   RO,   RS,   SE,   SI,   SK,   SM,   TR [2022/40]
TitleGerman:G9A-INHIBITOR[2022/40]
English:G9A INHIBITOR[2022/40]
French:INHIBITEUR DE G9A[2022/40]
Entry into regional phase15.06.2022Translation filed 
15.06.2022National basic fee paid 
15.06.2022Search fee paid 
15.06.2022Designation fee(s) paid 
15.06.2022Examination fee paid 
Examination procedure15.06.2022Examination requested  [2022/40]
09.12.2022Amendment by applicant (claims and/or description)
Fees paidRenewal fee
15.06.2022Renewal fee patent year 03
27.10.2023Renewal fee patent year 04
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Documents cited:Search[X]US5346907  (KERWIN JR JAMES F [US], et al) [X] 1-3,13-15 * abstract * * example 16 * * claims 1-16 *;
 [X]WO0024392  (SUMITOMO PHARMA [JP], et al) [X] 1-3,13-15 * abstract * * compounds 71-106 *; pages 93-95 * * claims 1-30 *;
 [X]WO0220530  (ASTRAZENECA AB [SE], et al) [X] 1-3,7,11,13,14 * abstract * * examples 6, 7, 11, 24, 25, 35, 42, 46, 53, 80, 82-88, 98-102 * * claims 1-9 *;
 [X]WO2004104001  (OSI PHARM INC [US], et al) [X] 1-3,7,11,13,14 * abstract * * examples 15, 20, 21, 26, 29-33, 38 * * examples 1-301 * * claims 1-31 *;
 [X]WO2009133348  (VANTIA LTD [GB], et al) [X] 1-3,13-15 * abstract * * examples 4-6, 9 * * compounds 15, 23, 55, 56, 63-66, 71-78 *; pages 93-99 * * compounds *; pages 100-105 * * examples 226-338 * * claims 1-15 *;
 [X]WO2011051673  (VANTIA LTD [GB], et al) [X] 1-3,13-15 * abstract * * examples 1-109 * * claims 1-20 *;
 [A]US2015274660  (PLIUSHCHEV MARINA A [US], et al) [A] 1-15 * abstract * * examples 1-27 * * claims 1-17 *;
 [A]WO2017181177  (EPIZYME INC [US]) [A] 1-15 * abstract * * compounds *; pages 60-258 ** claims 1-79 *;
 [A]WO2018005799  (UNIV GEORGIA STATE RES FOUND [US]) [A] 1-15 * abstract * * compounds *; pages 27-28 * * examples 1, 2 * * claims 1-19 *;
 [A]WO2019079607  (EPIZYME INC [US]) [A] 1-15 * abstract * * compounds *; pages 121-272 * * claims 1-218 *;
 [A]CN109824664  (UNIV GUANGZHOU CHINESE MEDICINE) [A] 1-15 * abstract * * examples 1-7 * * claims 1-8 *;
 [X]  - REGISTRY, CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US, (20160923), Database accession no. 1998710-51-2, URL: STN, XP002810946 [X] 1,2 * abstract *
 [X]  - REGISTRY, CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US, (20170727), Database accession no. 2103656-49-9, URL: STN, XP002810947 [X] 1-3 * abstract *
 [X]  - REGISTRY, CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US, (20120802), Database accession no. 1385476-54-9, URL: STN, XP002810948 [X] 1-3 * abstract *
 [X]  - REGISTRY, CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US, (20110410), Database accession no. 1277333-97-7, URL: STN, XP002810949 [X] 1-3,6 * abstract *
 [X]  - REGISTRY, CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US, (20110411), Database accession no. 1277271-40-5, URL: STN, XP002810950 [X] 1-3,6 * abstract *
 [X]  - REGISTRY, CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US, (20180321), Database accession no. 2195593-70-3, URL: STN, XP002810951 [X] 1-5 * abstract *
 [X]  - REGISTRY, CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US, (20180313), Database accession no. 21899-22-1, URL: STN, XP002810952 [X] 1-5 * abstract *
 [X]  - REGISTRY, CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US, (20180227), Database accession no. 2180285-90-7, URL: STN, XP002810953 [X] 1-4 * abstract *
 [X]  - REGISTRY, CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US, (20160715), Database accession no. 1952759-98-6, URL: STN, XP002810954 [X] 1-5 * abstract *
 [X]  - REGISTRY, CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US, (20110505), Database accession no. 1290503-95-5, URL: STN, XP002810955 [X] 1-4,7 * abstract *
 [X]  - BROWNE E J ET AL, "Preparation of amides derived from heterocyclic amines", JOURNAL OF THE CHEMICAL SOCIETY, SECTION C: ORGANIC CHEMISTRY.>6015C, CHEMICAL SOCIETY. LETCHWORTH, GB, (196801), vol. 1968, doi:10.1039/J39680002904, ISSN 0022-4952, page 2904, XP009092602 [X] 1,2,7,9,10 * abstract * * page 2905; table 1; compounds 5, 9 *

DOI:   http://dx.doi.org/10.1039/j39680002904
 [X]  - UTTAM KUMAR DAS ET AL, "Remarkable Shape-Sustaining, Load-Bearing, and Self-Healing Properties Displayed by a Supramolecular Gel Derived from a Bis-pyridyl-bis-amide of L-Phenyl Alanine", CHEMISTRY - AN ASIAN JOURNAL, WILEY-VCH, HOBOKEN, USA, (20140624), vol. 9, no. 9, doi:10.1002/ASIA.201402053, ISSN 1861-4728, pages 2475 - 2482, XP072422398 [X] 1,2,7,9,10 * abstract * * page 2476; figure 1 *

DOI:   http://dx.doi.org/10.1002/asia.201402053
 [X]  - BANERJEE SUBHABRATA ET AL, "Coordination Polymers in Selective Separation of Cations and Anions: A Series of Rarely Observed All Helical Three-Dimensional Coordination Polymers Derived from Various Chiral Amino Acid Based Bis-pyridyl-bis-amide Ligands", CRYSTAL GROWTH & DESIGN, US, (20111104), vol. 11, no. 12, doi:10.1021/cg201161q, ISSN 1528-7483, pages 5592 - 5597, XP093118152 [X] 1,2,7,9,10 * abstract * * scheme 1 *; page 5593 *

DOI:   http://dx.doi.org/10.1021/cg201161q
 [X]  - FOX SIDNEY W. ET AL, "Enzymic Synthesis of Peptide Bonds. VI. The Influence of Residue Type on Papaincatalyzed Reactions of Some Benzoylamino Acids with Some Amino Acid Anilides 1,2", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, (195311), vol. 75, no. 22, doi:10.1021/ja01118a021, ISSN 0002-7863, pages 5539 - 5542, XP093118201 [X] 1,2,7,8 * abstract * * page 5540; table II *

DOI:   http://dx.doi.org/10.1021/ja01118a021
 [X]  - REGISTRY, CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US, (20120801), Database accession no. 1385078-76-1, URL: STN, XP002810956 [X] 1,2,7,8 * abstract *
 [A]  - CAO YUE-PENG ET AL, "Inhibition of G9a by a small molecule inhibitor, UNC0642, induces apoptosis of human bladder cancer cells", ACTA PHARMACOLOGICA SINICA, NATURE PUBLISHING GROUP, GB, vol. 40, no. 8, doi:10.1038/S41401-018-0205-5, ISSN 1671-4083, (20190214), pages 1076 - 1084, (20190214), XP036994455 [A] 1-15 * abstract * * figures 1-6 *

DOI:   http://dx.doi.org/10.1038/s41401-018-0205-5
 [A]  - MILITE CIRO ET AL, "Discovery of a Novel Chemotype of Histone Lysine Methyltransferase EHMT1/2 (GLP/G9a) Inhibitors: Rational Design, Synthesis, Biological Evaluation, and Co-crystal Structure", JOURNAL OF MEDICINAL CHEMISTRY, US, (20190212), vol. 62, no. 5, doi:10.1021/acs.jmedchem.8b02008, ISSN 0022-2623, pages 2666 - 2689, XP055883905 [A] 1-15 * abstract * * chart 1 *; page 2667 * * page 2668; figure 1 * * page 2669; figure 2 * * page 2671; table 1 * * figures 6-11 *

DOI:   http://dx.doi.org/10.1021/acs.jmedchem.8b02008
International search[X]US3255202  (JOHNSON HERBERT E) [X] 1, 22 * claims, examples *;
 [X]WO2008135526  (BOEHRINGER INGELHEIM INT [DE], et al) [X] 1, 22, 27-30 * claims, examples *;
 [A]WO2012023285  (ONCOTHERAPY SCIENCE INC [JP], et al) [A] 1-30 * entire text *;
 [A]WO2013140148  (IMP INNOVATIONS LTD [GB], et al) [A] 1-30 * entire text *;
 [X]WO2015130964  (GILEAD SCIENCES INC [US]) [X] 1-2, 12-13, 27-30 * claims, examples *;
 [A]US2015274660  (PLIUSHCHEV MARINA A [US], et al) [A] 1-30* entire text *;
 [X]WO2017176962  (LYSOSOMAL THERAPEUTICS INC [US]) [X] 1, 22, 27-30 * claims, p. 137 *;
 [X]  - Database RECISTRY, (20180000), Database accession no. 2195593-70-3, URL: STN, XP055833093 [X] 1-6
 [X]  - Database RECISTRY, (20110000), Database accession no. 1277333-97-7, URL: STN, XP055833095 [X] 1-3, 10
 [X]  - Database RECISTRY, (20140000), Database accession no. 1385078-76-1, URL: STN, XP055833104 [X] 1-2, 12-13
 [X]  - Database RECISTRY, (20140000), Database accession no. 1581959-49-0, URL: STN, XP055833098 [X] 1-2, 12, 14-15,20-21 * entire text *
 [X]  - FOX, S. W. et al., "Enzymic synthesis of peptide bonds. VI. The influence of residue type on papain-catalyzed reactions of some benzoylamino acids with some amino acid anilides", Journal of the American Chemical Society, (19530000), vol. 75, doi:10.1021/ja01118a02 1, pages 5539 - 5542, XP055833108 [X] 1-2, 12-13 * tables II-III *
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