JP2017524668A5 - - Google Patents
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- JP2017524668A5 JP2017524668A5 JP2016573017A JP2016573017A JP2017524668A5 JP 2017524668 A5 JP2017524668 A5 JP 2017524668A5 JP 2016573017 A JP2016573017 A JP 2016573017A JP 2016573017 A JP2016573017 A JP 2016573017A JP 2017524668 A5 JP2017524668 A5 JP 2017524668A5
- Authority
- JP
- Japan
- Prior art keywords
- amino
- methoxy
- quinolyl
- substituents
- optionally substituted
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 125000001424 substituent group Chemical group 0.000 claims 21
- 229920006395 saturated elastomer Polymers 0.000 claims 15
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 8
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- 125000002837 carbocyclic group Chemical group 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 5
- 125000002619 bicyclic group Chemical group 0.000 claims 4
- 125000004122 cyclic group Chemical group 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 3
- -1 7-methoxy-2-phenyl-4-quinolyl Chemical group 0.000 claims 2
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 2
- 102100036279 DNA (cytosine-5)-methyltransferase 1 Human genes 0.000 claims 2
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 125000006413 ring segment Chemical group 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- KTUSPJLYLTVECJ-ZDUSSCGKSA-N (2s)-1-[(7-methoxy-2-phenylquinolin-4-yl)amino]propan-2-ol Chemical compound N=1C2=CC(OC)=CC=C2C(NC[C@H](C)O)=CC=1C1=CC=CC=C1 KTUSPJLYLTVECJ-ZDUSSCGKSA-N 0.000 claims 1
- DQHWTMWZCDUCCZ-ZOWNYOTGSA-N (2s)-1-[(7-methoxy-2-phenylquinolin-4-yl)amino]propan-2-ol;hydrochloride Chemical compound Cl.N=1C2=CC(OC)=CC=C2C(NC[C@H](C)O)=CC=1C1=CC=CC=C1 DQHWTMWZCDUCCZ-ZOWNYOTGSA-N 0.000 claims 1
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 claims 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000006711 (C2-C12) alkynyl group Chemical group 0.000 claims 1
- ACFVGTNISYIOJB-UHFFFAOYSA-N 1-[[2-(4-chlorophenyl)-7-methoxyquinolin-4-yl]amino]-3-(methylamino)propan-2-ol Chemical compound N=1C2=CC(OC)=CC=C2C(NCC(O)CNC)=CC=1C1=CC=C(Cl)C=C1 ACFVGTNISYIOJB-UHFFFAOYSA-N 0.000 claims 1
- HMQATFUGWORXRK-UHFFFAOYSA-N 1-[[2-(4-chlorophenyl)-7-methoxyquinolin-4-yl]amino]-3-(methylamino)propan-2-ol;hydrochloride Chemical compound Cl.N=1C2=CC(OC)=CC=C2C(NCC(O)CNC)=CC=1C1=CC=C(Cl)C=C1 HMQATFUGWORXRK-UHFFFAOYSA-N 0.000 claims 1
- ALGKSULFKHXVRC-UHFFFAOYSA-N 1-[[7-methoxy-2-(4-methylphenyl)quinolin-4-yl]amino]-3-(methylamino)propan-2-ol Chemical compound N=1C2=CC(OC)=CC=C2C(NCC(O)CNC)=CC=1C1=CC=C(C)C=C1 ALGKSULFKHXVRC-UHFFFAOYSA-N 0.000 claims 1
- SDIHVEKETFXXLR-UHFFFAOYSA-N 1-[[7-methoxy-2-(4-methylphenyl)quinolin-4-yl]amino]-3-(methylamino)propan-2-ol;hydrochloride Chemical compound Cl.N=1C2=CC(OC)=CC=C2C(NCC(O)CNC)=CC=1C1=CC=C(C)C=C1 SDIHVEKETFXXLR-UHFFFAOYSA-N 0.000 claims 1
- GAHMYSIDLLELAV-UHFFFAOYSA-N 1-amino-3-[(7-methoxy-2-phenylquinolin-4-yl)amino]propan-2-ol Chemical compound N=1C2=CC(OC)=CC=C2C(NCC(O)CN)=CC=1C1=CC=CC=C1 GAHMYSIDLLELAV-UHFFFAOYSA-N 0.000 claims 1
- KORZBOYMMXMUJI-UHFFFAOYSA-N 1-amino-3-[(7-methoxy-2-phenylquinolin-4-yl)amino]propan-2-ol;hydrochloride Chemical compound Cl.N=1C2=CC(OC)=CC=C2C(NCC(O)CN)=CC=1C1=CC=CC=C1 KORZBOYMMXMUJI-UHFFFAOYSA-N 0.000 claims 1
- JXZSAHFDPIEHEE-UHFFFAOYSA-N 1-amino-3-[[2-(3,4-dichlorophenyl)-7-methoxyquinolin-4-yl]amino]propan-2-ol Chemical compound N=1C2=CC(OC)=CC=C2C(NCC(O)CN)=CC=1C1=CC=C(Cl)C(Cl)=C1 JXZSAHFDPIEHEE-UHFFFAOYSA-N 0.000 claims 1
- BMEVVKJXVKFHJE-UHFFFAOYSA-N 1-amino-3-[[2-(3,4-dichlorophenyl)-7-methoxyquinolin-4-yl]amino]propan-2-ol;hydrochloride Chemical compound Cl.N=1C2=CC(OC)=CC=C2C(NCC(O)CN)=CC=1C1=CC=C(Cl)C(Cl)=C1 BMEVVKJXVKFHJE-UHFFFAOYSA-N 0.000 claims 1
- WMAHVHCZQZEWMF-UHFFFAOYSA-N 1-amino-3-[[2-(4-chlorophenyl)-7-methoxyquinolin-4-yl]amino]propan-2-ol Chemical compound N=1C2=CC(OC)=CC=C2C(NCC(O)CN)=CC=1C1=CC=C(Cl)C=C1 WMAHVHCZQZEWMF-UHFFFAOYSA-N 0.000 claims 1
- IUCBDZRZUGJFOS-UHFFFAOYSA-N 1-amino-3-[[2-(4-chlorophenyl)-7-methoxyquinolin-4-yl]amino]propan-2-ol;hydrochloride Chemical compound Cl.N=1C2=CC(OC)=CC=C2C(NCC(O)CN)=CC=1C1=CC=C(Cl)C=C1 IUCBDZRZUGJFOS-UHFFFAOYSA-N 0.000 claims 1
- GEKIARRHTXRYNN-UHFFFAOYSA-N 1-amino-3-[[7-methoxy-2-(4-methoxyphenyl)quinolin-4-yl]amino]propan-2-ol Chemical compound C1=CC(OC)=CC=C1C1=CC(NCC(O)CN)=C(C=CC(OC)=C2)C2=N1 GEKIARRHTXRYNN-UHFFFAOYSA-N 0.000 claims 1
- JZSQVVRZFIVUGZ-UHFFFAOYSA-N 1-amino-3-[[7-methoxy-2-(4-methoxyphenyl)quinolin-4-yl]amino]propan-2-ol;hydrochloride Chemical compound Cl.C1=CC(OC)=CC=C1C1=CC(NCC(O)CN)=C(C=CC(OC)=C2)C2=N1 JZSQVVRZFIVUGZ-UHFFFAOYSA-N 0.000 claims 1
- LFPSNZFRCSVPHA-UHFFFAOYSA-N 1-amino-3-[[7-methoxy-2-(4-methylphenyl)quinolin-4-yl]amino]propan-2-ol Chemical compound N=1C2=CC(OC)=CC=C2C(NCC(O)CN)=CC=1C1=CC=C(C)C=C1 LFPSNZFRCSVPHA-UHFFFAOYSA-N 0.000 claims 1
- UXUGTFZKFJOPMY-UHFFFAOYSA-N 1-amino-3-[[7-methoxy-2-(4-methylphenyl)quinolin-4-yl]amino]propan-2-ol;hydrochloride Chemical compound Cl.N=1C2=CC(OC)=CC=C2C(NCC(O)CN)=CC=1C1=CC=C(C)C=C1 UXUGTFZKFJOPMY-UHFFFAOYSA-N 0.000 claims 1
- BZGJTNMHBWLFNW-UHFFFAOYSA-N 1-n,1-n-diethyl-4-n-(7-methoxy-2-phenylquinolin-4-yl)pentane-1,4-diamine Chemical compound N=1C2=CC(OC)=CC=C2C(NC(C)CCCN(CC)CC)=CC=1C1=CC=CC=C1 BZGJTNMHBWLFNW-UHFFFAOYSA-N 0.000 claims 1
- KACALPZREZDOBE-UHFFFAOYSA-N 2-(2-chlorophenyl)-6,7-dimethoxy-N-pyridin-4-ylquinolin-4-amine Chemical compound ClC1=C(C=CC=C1)C1=NC2=CC(=C(C=C2C(=C1)NC1=CC=NC=C1)OC)OC KACALPZREZDOBE-UHFFFAOYSA-N 0.000 claims 1
- ZYIISCAWNDQQKE-UHFFFAOYSA-N 2-[(7-methoxy-2-phenylquinolin-4-yl)amino]ethanol Chemical compound N=1C2=CC(OC)=CC=C2C(NCCO)=CC=1C1=CC=CC=C1 ZYIISCAWNDQQKE-UHFFFAOYSA-N 0.000 claims 1
- RWUJTEDOJAJPKI-UHFFFAOYSA-N 2-[(7-methoxy-2-phenylquinolin-4-yl)amino]ethanol;hydrochloride Chemical compound Cl.N=1C2=CC(OC)=CC=C2C(NCCO)=CC=1C1=CC=CC=C1 RWUJTEDOJAJPKI-UHFFFAOYSA-N 0.000 claims 1
- YXNJWCMKWPWUCE-UHFFFAOYSA-N 2-[[2-(3,4-dichlorophenyl)-7-methoxyquinolin-4-yl]amino]ethanol Chemical compound N=1C2=CC(OC)=CC=C2C(NCCO)=CC=1C1=CC=C(Cl)C(Cl)=C1 YXNJWCMKWPWUCE-UHFFFAOYSA-N 0.000 claims 1
- ULUPPQMTRQCRDB-UHFFFAOYSA-N 2-[[2-(3,4-dichlorophenyl)-7-methoxyquinolin-4-yl]amino]ethanol;hydrochloride Chemical compound Cl.N=1C2=CC(OC)=CC=C2C(NCCO)=CC=1C1=CC=C(Cl)C(Cl)=C1 ULUPPQMTRQCRDB-UHFFFAOYSA-N 0.000 claims 1
- PWZTVPNSLQBOQF-UHFFFAOYSA-N 2-[[2-(4-chlorophenyl)-7-methoxyquinolin-4-yl]amino]ethanol Chemical compound N=1C2=CC(OC)=CC=C2C(NCCO)=CC=1C1=CC=C(Cl)C=C1 PWZTVPNSLQBOQF-UHFFFAOYSA-N 0.000 claims 1
- IBBSBRWGALTPRP-UHFFFAOYSA-N 2-[[2-(4-chlorophenyl)-7-methoxyquinolin-4-yl]amino]ethanol;hydrochloride Chemical compound Cl.N=1C2=CC(OC)=CC=C2C(NCCO)=CC=1C1=CC=C(Cl)C=C1 IBBSBRWGALTPRP-UHFFFAOYSA-N 0.000 claims 1
- RVXYSGFHWJGYCX-UHFFFAOYSA-N 2-[[7-methoxy-2-(4-methoxyphenyl)quinolin-4-yl]amino]ethanol Chemical compound C1=CC(OC)=CC=C1C1=CC(NCCO)=C(C=CC(OC)=C2)C2=N1 RVXYSGFHWJGYCX-UHFFFAOYSA-N 0.000 claims 1
- OBEMUFMGIAPKDG-UHFFFAOYSA-N 2-[[7-methoxy-2-(4-methoxyphenyl)quinolin-4-yl]amino]ethanol;hydrochloride Chemical compound Cl.C1=CC(OC)=CC=C1C1=CC(NCCO)=C(C=CC(OC)=C2)C2=N1 OBEMUFMGIAPKDG-UHFFFAOYSA-N 0.000 claims 1
- FUFBESHOBRTCEC-UHFFFAOYSA-N 2-[[7-methoxy-2-(4-methylphenyl)quinolin-4-yl]amino]ethanol Chemical compound N=1C2=CC(OC)=CC=C2C(NCCO)=CC=1C1=CC=C(C)C=C1 FUFBESHOBRTCEC-UHFFFAOYSA-N 0.000 claims 1
- BZDXKAKEVDLBQF-UHFFFAOYSA-N 2-[[7-methoxy-2-(4-methylphenyl)quinolin-4-yl]amino]ethanol;hydrochloride Chemical compound Cl.N=1C2=CC(OC)=CC=C2C(NCCO)=CC=1C1=CC=C(C)C=C1 BZDXKAKEVDLBQF-UHFFFAOYSA-N 0.000 claims 1
- 125000004207 3-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(OC([H])([H])[H])=C1[H] 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- CYORHGWKIKCGTL-UHFFFAOYSA-N 5-[[[2-(4-chlorophenyl)-7-methoxyquinolin-4-yl]amino]methyl]-1,3-oxazolidin-2-one Chemical compound C=1C(C=2C=CC(Cl)=CC=2)=NC2=CC(OC)=CC=C2C=1NCC1CNC(=O)O1 CYORHGWKIKCGTL-UHFFFAOYSA-N 0.000 claims 1
- QTBATKXDYFVWDJ-UHFFFAOYSA-N 5-[[[7-methoxy-2-(4-methylphenyl)quinolin-4-yl]amino]methyl]-1,3-oxazolidin-2-one Chemical compound C=1C(C=2C=CC(C)=CC=2)=NC2=CC(OC)=CC=C2C=1NCC1CNC(=O)O1 QTBATKXDYFVWDJ-UHFFFAOYSA-N 0.000 claims 1
- 125000001960 7 membered carbocyclic group Chemical group 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 108010009540 DNA (Cytosine-5-)-Methyltransferase 1 Proteins 0.000 claims 1
- 102100024812 DNA (cytosine-5)-methyltransferase 3A Human genes 0.000 claims 1
- 102100024810 DNA (cytosine-5)-methyltransferase 3B Human genes 0.000 claims 1
- 101710123222 DNA (cytosine-5)-methyltransferase 3B Proteins 0.000 claims 1
- 108010024491 DNA Methyltransferase 3A Proteins 0.000 claims 1
- 102000011787 Histone Methyltransferases Human genes 0.000 claims 1
- 108010036115 Histone Methyltransferases Proteins 0.000 claims 1
- 101000931098 Homo sapiens DNA (cytosine-5)-methyltransferase 1 Proteins 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- CPEOJTVXNBACKS-UHFFFAOYSA-N n-benzyl-7-methoxy-2-phenylquinolin-4-amine Chemical compound C=1C(C=2C=CC=CC=2)=NC2=CC(OC)=CC=C2C=1NCC1=CC=CC=C1 CPEOJTVXNBACKS-UHFFFAOYSA-N 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14382230 | 2014-06-16 | ||
| EP14382230.2 | 2014-06-16 | ||
| PCT/EP2015/056860 WO2015192981A1 (en) | 2014-06-16 | 2015-03-30 | Novel compounds as dual inhibitors of histone methyltransferases and dna methyltransferases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017524668A JP2017524668A (ja) | 2017-08-31 |
| JP2017524668A5 true JP2017524668A5 (OSRAM) | 2018-04-12 |
| JP6527534B2 JP6527534B2 (ja) | 2019-06-05 |
Family
ID=51136403
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016573017A Active JP6527534B2 (ja) | 2014-06-16 | 2015-03-30 | ヒストンメチルトランスフェラーゼ及びｄｎａメチルトランスフェラーゼの二重阻害剤としての新規化合物 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US9840500B2 (OSRAM) |
| EP (1) | EP3154957B1 (OSRAM) |
| JP (1) | JP6527534B2 (OSRAM) |
| CN (1) | CN106536509B (OSRAM) |
| AU (1) | AU2015276537B2 (OSRAM) |
| CA (1) | CA2987978C (OSRAM) |
| DK (1) | DK3154957T3 (OSRAM) |
| ES (1) | ES2769648T3 (OSRAM) |
| WO (1) | WO2015192981A1 (OSRAM) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017102677A1 (en) * | 2015-12-14 | 2017-06-22 | Fundación Para La Investigación Médica Aplicada | 2,4,6,7-tetrasubstituted quinoline compounds as inhibitors of dna methyltransferases |
| KR20230130747A (ko) * | 2016-04-15 | 2023-09-12 | 에피자임, 인코포레이티드 | Ehmt1 및 ehmt2 저해제로서의 아민-치환된 아릴 또는 헤테로아릴 화합물 |
| TWI794171B (zh) | 2016-05-11 | 2023-03-01 | 美商滬亞生物國際有限公司 | Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療 |
| TWI808055B (zh) | 2016-05-11 | 2023-07-11 | 美商滬亞生物國際有限公司 | Hdac 抑制劑與 pd-1 抑制劑之組合治療 |
| US11278550B2 (en) | 2016-05-17 | 2022-03-22 | Duke University | Compositions and methods for the treatment of Prader-Willi syndrome |
| US11433068B2 (en) * | 2016-09-08 | 2022-09-06 | The General Hospital Corporation | Treatment of cancers having alterations within the SWI/SNF chromatin remodeling complex |
| EP4063358B1 (en) * | 2016-12-22 | 2024-05-22 | Global Blood Therapeutics, Inc. | Histone methyltransferase inhibitors |
| WO2018119065A1 (en) | 2016-12-22 | 2018-06-28 | Asddr, Llc | Use of histone methyltransferase inhibitors and histone deacetylase inhibitors for therapy of phelan-mcdermid syndrome |
| US20200113901A1 (en) * | 2017-03-31 | 2020-04-16 | Epizyme, Inc. | Methods of using ehmt2 inhibitors |
| EP3612181A4 (en) | 2017-04-21 | 2021-01-06 | Epizyme, Inc. | Combination therapies with ehmt2 inhibitors |
| BR112019025770A2 (pt) | 2017-06-09 | 2020-06-23 | Global Blood Therapeutics, Inc. | Compostos de azaindol como inibidores de histona metiltransferase |
| WO2018229139A1 (en) | 2017-06-14 | 2018-12-20 | Fundación Para La Investigación Médica Aplicada | Novel compounds for use in cancer |
| WO2019036384A1 (en) | 2017-08-15 | 2019-02-21 | Global Blood Therapeutics, Inc. | TRICYCLIC COMPOUNDS AS HISTONE INHIBITORS METHYLTRANSFERASES |
| EP3668863B1 (en) | 2017-08-15 | 2025-03-19 | Global Blood Therapeutics, Inc. | Tricyclic compounds as histone methyl-transferase inhibitors |
| SG11202003225YA (en) * | 2017-10-18 | 2020-05-28 | Epizyme Inc | Amine-substituted heterocyclic compounds as ehmt2 inhibitors, salts thereof, and methods of synthesis thereof |
| WO2019079607A1 (en) * | 2017-10-18 | 2019-04-25 | Epizyme, Inc. | METHODS OF USING EHMT2 INHIBITORS IN THE TREATMENT OR PREVENTION OF BLOOD DISORDERS |
| EP3807248A4 (en) * | 2018-05-29 | 2021-10-27 | Council of Scientific and Industrial Research | BICYCLIC TOPOISOMERASE I INHIBITOR COMPOUNDS, THEIR PREPARATION AND USE |
| WO2019243236A1 (en) | 2018-06-18 | 2019-12-26 | Fundación Para La Investigación Médica Aplicada | New anticancer drug combinations |
| CN112390791B (zh) * | 2019-08-14 | 2023-08-01 | 复旦大学 | 一类dna甲基转移酶1荧光探针及其用途 |
| JP2023536634A (ja) * | 2020-08-07 | 2023-08-28 | アトス セラピューティクス，インコーポレイテッド | 自己免疫疾患および癌の処置のための小分子 |
| US11351149B2 (en) | 2020-09-03 | 2022-06-07 | Pfizer Inc. | Nitrile-containing antiviral compounds |
| CN115160294B (zh) * | 2022-06-27 | 2023-09-29 | 中山大学 | 一种G9a/GLP共价抑制剂及其制备方法及应用 |
| CN120965666A (zh) * | 2025-10-21 | 2025-11-18 | 四川大学华西医院 | 一种喹啉类化合物、制备方法和用途及其药物组合物 |
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| WO1999001154A1 (en) * | 1997-07-03 | 1999-01-14 | University Of Iowa Research Foundation | Method for inhibiting immunostimulatory dna associated responses |
| CA2412345A1 (en) * | 1999-06-16 | 2000-12-21 | University Of Iowa Research Foundation | Antagonism of immunostimulatory cpg-oligonucleotides by 4-aminoquinolines and other weak bases |
| EP1088818B1 (en) | 1999-10-01 | 2004-11-03 | F. Hoffmann-La Roche Ag | Quinolin-4-yl derivatives |
| US6440995B1 (en) * | 1999-10-01 | 2002-08-27 | Hoffman-La Roche Inc. | Quinolin-4-yl derivatives |
| AU2002361846A1 (en) * | 2001-12-21 | 2003-07-15 | Bayer Pharmaceuticals Corporation | Quinazoline and quinoline derivative compounds as inhibitors of prolylpeptidase, inducers of apoptosis and cancer treatment agents |
| WO2004056352A1 (en) * | 2002-12-19 | 2004-07-08 | Scios, Inc. | TREATMENT OF OBESITY AND ASSOCIATED CONDITIONS WITH TGF-β INHIBITORS |
| US7314939B2 (en) * | 2003-06-17 | 2008-01-01 | Millennium Pharmaceuticals, Inc. | Compositions and methods for inhibiting TGF-β |
| CA2664631A1 (en) | 2006-10-12 | 2008-04-17 | David J. Bearss | Quinoline derivatives for modulating dna methylation |
| CN101535295A (zh) * | 2006-10-12 | 2009-09-16 | 休普基因公司 | 用于调节dna甲基化的喹啉衍生物 |
| US7790746B2 (en) | 2007-10-12 | 2010-09-07 | Supergen, Inc. | Quinoline derivatives for modulating DNA methylation |
| WO2010151791A1 (en) * | 2009-06-25 | 2010-12-29 | Amgen Inc. | Heterocyclic compounds and their uses |
| CA2770753C (en) * | 2009-08-12 | 2019-01-15 | Kyoto University | Method for inducing differentiation of pluripotent stem cells into neural precursor cells |
| WO2011054433A1 (en) * | 2009-11-07 | 2011-05-12 | Merck Patent Gmbh | Heteroarylaminoquinolines as tgf-beta receptor kinase inhibitors |
| EP2771012A4 (en) * | 2011-10-24 | 2015-06-24 | Glaxosmithkline Ip No 2 Ltd | NEW CONNECTIONS |
| EP2828250B1 (en) | 2012-03-19 | 2021-03-10 | Imperial College Innovations Limited | Quinazoline compounds and their use in therapy |
| EP2730558A1 (en) | 2012-11-08 | 2014-05-14 | Ikerchem, S.L. | Indole derivatives, pharmaceutical compositions containing such indoles and their use as DNA methylation modulators |
| EP2918014B1 (en) * | 2012-11-09 | 2018-10-31 | OCT Circuit Technologies International Limited | Analog to digital conversion method with offset tracking and correction and analog to digital converter implementing the same |
| JP6338601B2 (ja) * | 2013-03-01 | 2018-06-06 | フンダシオン パラ ラ インベスティガシオン メディカ アプリカダ | ホスホジエステラーゼとヒストンデアセチラーゼの二重阻害剤としての新規な化合物 |
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2015
- 2015-03-30 US US15/315,326 patent/US9840500B2/en active Active
- 2015-03-30 CN CN201580034131.4A patent/CN106536509B/zh active Active
- 2015-03-30 ES ES15714185T patent/ES2769648T3/es active Active
- 2015-03-30 WO PCT/EP2015/056860 patent/WO2015192981A1/en not_active Ceased
- 2015-03-30 AU AU2015276537A patent/AU2015276537B2/en active Active
- 2015-03-30 JP JP2016573017A patent/JP6527534B2/ja active Active
- 2015-03-30 DK DK15714185.4T patent/DK3154957T3/da active
- 2015-03-30 EP EP15714185.4A patent/EP3154957B1/en active Active
- 2015-03-30 CA CA2987978A patent/CA2987978C/en active Active
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