JP2017526675A5 - - Google Patents
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- JP2017526675A5 JP2017526675A5 JP2017510881A JP2017510881A JP2017526675A5 JP 2017526675 A5 JP2017526675 A5 JP 2017526675A5 JP 2017510881 A JP2017510881 A JP 2017510881A JP 2017510881 A JP2017510881 A JP 2017510881A JP 2017526675 A5 JP2017526675 A5 JP 2017526675A5
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- JP
- Japan
- Prior art keywords
- cycloalkyl
- solvate
- alkyl
- pharmaceutically acceptable
- acceptable salt
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims description 180
- 125000000217 alkyl group Chemical group 0.000 claims description 170
- 150000003839 salts Chemical class 0.000 claims description 121
- 239000012453 solvate Substances 0.000 claims description 119
- 125000000623 heterocyclic group Chemical group 0.000 claims description 104
- 125000000304 alkynyl group Chemical group 0.000 claims description 94
- 125000003342 alkenyl group Chemical group 0.000 claims description 93
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 88
- 229910052799 carbon Inorganic materials 0.000 claims description 87
- 125000001072 heteroaryl group Chemical group 0.000 claims description 78
- 125000003118 aryl group Chemical group 0.000 claims description 75
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims description 64
- 125000003709 fluoroalkyl group Chemical group 0.000 claims description 60
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims description 54
- 125000001424 substituent group Chemical group 0.000 claims description 42
- 125000004432 carbon atom Chemical group C* 0.000 claims description 33
- 229910052736 halogen Inorganic materials 0.000 claims description 32
- 150000002367 halogens Chemical class 0.000 claims description 32
- 125000003545 alkoxy group Chemical group 0.000 claims description 30
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 24
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 24
- 125000004104 aryloxy group Chemical group 0.000 claims description 24
- 125000005553 heteroaryloxy group Chemical group 0.000 claims description 22
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 20
- 125000004429 atom Chemical group 0.000 claims description 17
- 102100035864 Histone lysine demethylase PHF8 Human genes 0.000 claims description 16
- 101001000378 Homo sapiens Histone lysine demethylase PHF8 Proteins 0.000 claims description 16
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 16
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 14
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 12
- 125000002947 alkylene group Chemical group 0.000 claims description 10
- 230000001419 dependent effect Effects 0.000 claims description 10
- 201000010099 disease Diseases 0.000 claims description 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 10
- 239000008194 pharmaceutical composition Substances 0.000 claims description 10
- 101100073171 Drosophila melanogaster Kdm2 gene Proteins 0.000 claims description 8
- 101000614013 Homo sapiens Lysine-specific demethylase 2B Proteins 0.000 claims description 8
- 101001088893 Homo sapiens Lysine-specific demethylase 4C Proteins 0.000 claims description 8
- 101001088883 Homo sapiens Lysine-specific demethylase 5B Proteins 0.000 claims description 8
- 101001025967 Homo sapiens Lysine-specific demethylase 6A Proteins 0.000 claims description 8
- 102100040584 Lysine-specific demethylase 2B Human genes 0.000 claims description 8
- 102100033230 Lysine-specific demethylase 4C Human genes 0.000 claims description 8
- 102100033247 Lysine-specific demethylase 5B Human genes 0.000 claims description 8
- 102100037462 Lysine-specific demethylase 6A Human genes 0.000 claims description 8
- 102100037465 Lysine-specific demethylase 7A Human genes 0.000 claims description 8
- 230000005764 inhibitory process Effects 0.000 claims description 8
- 101150048064 kdm7a gene Proteins 0.000 claims description 8
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 8
- 125000004043 oxo group Chemical group O=* 0.000 claims description 8
- 125000002993 cycloalkylene group Chemical group 0.000 claims description 6
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 6
- 230000002401 inhibitory effect Effects 0.000 claims description 6
- 229910052757 nitrogen Inorganic materials 0.000 claims description 6
- 238000002360 preparation method Methods 0.000 claims description 6
- 239000003814 drug Substances 0.000 claims description 5
- 125000002733 (C1-C6) fluoroalkyl group Chemical group 0.000 claims description 4
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 4
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims description 4
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims description 4
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 4
- 125000005429 oxyalkyl group Chemical group 0.000 claims description 4
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 4
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims description 2
- 108010033040 Histones Proteins 0.000 claims description 2
- 239000013543 active substance Substances 0.000 claims description 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 2
- 230000017858 demethylation Effects 0.000 claims description 2
- 238000010520 demethylation reaction Methods 0.000 claims description 2
- 125000002883 imidazolyl group Chemical group 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
- 125000001425 triazolyl group Chemical group 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 17
- 125000006546 (C4-C10) cycloalkyl group Chemical group 0.000 claims 4
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 4
- -1 alkeni R Chemical group 0.000 claims 3
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 2
- 238000006467 substitution reaction Methods 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 102000006947 Histones Human genes 0.000 claims 1
- 238000007792 addition Methods 0.000 claims 1
- 150000001408 amides Chemical group 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 150000003457 sulfones Chemical class 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 238000000034 method Methods 0.000 description 4
- 0 **N(*)C(*)c1nc(*)nc(O)c1 Chemical compound **N(*)C(*)c1nc(*)nc(O)c1 0.000 description 1
- RASVGFMDDLVZSK-UHFFFAOYSA-N CCc1cnc(CNCc2nc(C)cc(C(O)=O)c2)[n]1CCc1ccccc1 Chemical compound CCc1cnc(CNCc2nc(C)cc(C(O)=O)c2)[n]1CCc1ccccc1 RASVGFMDDLVZSK-UHFFFAOYSA-N 0.000 description 1
- ORTZUFGQPDXCIN-UHFFFAOYSA-N Cc1cc(C(O)=O)cc(CNCc2ncc(CC#CC)[n]2Cc(cc2)ccc2F)n1 Chemical compound Cc1cc(C(O)=O)cc(CNCc2ncc(CC#CC)[n]2Cc(cc2)ccc2F)n1 ORTZUFGQPDXCIN-UHFFFAOYSA-N 0.000 description 1
- DTDVJXFGJQBRLW-UHFFFAOYSA-N Cc1cc(C(O)=O)cc(CNCc2nnc[n]2CCc2cccc(Cl)c2)n1 Chemical compound Cc1cc(C(O)=O)cc(CNCc2nnc[n]2CCc2cccc(Cl)c2)n1 DTDVJXFGJQBRLW-UHFFFAOYSA-N 0.000 description 1
- XNAUNIHPQIPVLW-UHFFFAOYSA-N Cc1nc(CNCc2nnc(CNC3)[n]2C3c2ccccc2)cc(C(O)=O)c1 Chemical compound Cc1nc(CNCc2nnc(CNC3)[n]2C3c2ccccc2)cc(C(O)=O)c1 XNAUNIHPQIPVLW-UHFFFAOYSA-N 0.000 description 1
- HITBOZDUYVYOEN-UHFFFAOYSA-N OCc1cc(C(O)=O)cc(CNCc2nc(C=O)c[n]2Cc(cc2)ccc2F)n1 Chemical compound OCc1cc(C(O)=O)cc(CNCc2nc(C=O)c[n]2Cc(cc2)ccc2F)n1 HITBOZDUYVYOEN-UHFFFAOYSA-N 0.000 description 1
- CGFCQTHVWSBUDP-UHFFFAOYSA-N OCc1cc(C(O)=O)cc(CNCc2nnc[n]2CCc2cc(Cl)cc(Cl)c2)n1 Chemical compound OCc1cc(C(O)=O)cc(CNCc2nnc[n]2CCc2cc(Cl)cc(Cl)c2)n1 CGFCQTHVWSBUDP-UHFFFAOYSA-N 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 125000000565 sulfonamide group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462042717P | 2014-08-27 | 2014-08-27 | |
| US62/042,717 | 2014-08-27 | ||
| PCT/US2015/046921 WO2016033169A1 (en) | 2014-08-27 | 2015-08-26 | Compounds and methods for inhibiting histone demethylases |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017526675A JP2017526675A (ja) | 2017-09-14 |
| JP2017526675A5 true JP2017526675A5 (enExample) | 2018-09-27 |
Family
ID=54062822
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017510881A Withdrawn JP2017526675A (ja) | 2014-08-27 | 2015-08-26 | ヒストンデメチラーゼを阻害するための化合物および方法 |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US9802941B2 (enExample) |
| EP (1) | EP3186238A1 (enExample) |
| JP (1) | JP2017526675A (enExample) |
| KR (1) | KR20170040805A (enExample) |
| CN (1) | CN107074807A (enExample) |
| AR (1) | AR101692A1 (enExample) |
| AU (1) | AU2015306662A1 (enExample) |
| BR (1) | BR112017003442A2 (enExample) |
| CA (1) | CA2957947A1 (enExample) |
| EA (1) | EA201790154A1 (enExample) |
| IL (1) | IL250355A0 (enExample) |
| MA (1) | MA40470A (enExample) |
| MX (1) | MX2017002451A (enExample) |
| SG (1) | SG11201701182VA (enExample) |
| TW (1) | TW201625536A (enExample) |
| WO (1) | WO2016033169A1 (enExample) |
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| WO2017198785A1 (en) * | 2016-05-18 | 2017-11-23 | Ieo - Istituto Europeo Di Oncologia S.R.L. | Oxime derivatives useful as inhibitors of histone demethylase kdm4c |
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| BR102017010009A2 (pt) | 2016-05-27 | 2017-12-12 | Gilead Sciences, Inc. | Compounds for the treatment of hepatitis b virus infection |
| JOP20190024A1 (ar) | 2016-08-26 | 2019-02-19 | Gilead Sciences Inc | مركبات بيروليزين بها استبدال واستخداماتها |
| US10640499B2 (en) | 2016-09-02 | 2020-05-05 | Gilead Sciences, Inc. | Toll like receptor modulator compounds |
| MA46093A (fr) | 2016-09-02 | 2021-05-19 | Gilead Sciences Inc | Composés modulateurs du recepteur de type toll |
| FI3526323T3 (fi) | 2016-10-14 | 2023-06-06 | Prec Biosciences Inc | Hepatiitti B -viruksen genomissa oleville tunnistussekvensseille spesifisiä muokattuja meganukleaaseja |
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| WO2018222831A1 (en) * | 2017-05-31 | 2018-12-06 | The Children's Medical Center Corporation | TARGETING LYSINE DEMETHYLASES (KDMs) AS A THERAPEUTIC STRATEGY FOR DIFFUSE LARGE B-CELL LYMPHOMA |
| KR102492115B1 (ko) | 2017-12-20 | 2023-01-27 | 인스티튜트 오브 오가닉 케미스트리 앤드 바이오케미스트리 에이에스 씨알 브이.브이.아이. | Sting 어댑터 단백질을 활성화하는 포스포네이트 결합을 가진 2'3' 사이클릭 다이뉴클레오티드 |
| CA3084569A1 (en) | 2017-12-20 | 2019-06-27 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein |
| WO2019154261A1 (zh) * | 2018-02-09 | 2019-08-15 | 南京明德新药研发股份有限公司 | 与kmd5通路相关的吡啶衍生物 |
| EP4227302A1 (en) | 2018-02-13 | 2023-08-16 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| US10836769B2 (en) | 2018-02-26 | 2020-11-17 | Gilead Sciences, Inc. | Substituted pyrrolizine compounds and uses thereof |
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| TWI833744B (zh) | 2018-04-06 | 2024-03-01 | 捷克科學院有機化學與生物化學研究所 | 3'3'-環二核苷酸 |
| TW202005654A (zh) | 2018-04-06 | 2020-02-01 | 捷克科學院有機化學與生物化學研究所 | ２，２，─環二核苷酸 |
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| EP3935066A1 (en) | 2019-03-07 | 2022-01-12 | Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. | 3'3'-cyclic dinucleotides and prodrugs thereof |
| WO2020178768A1 (en) | 2019-03-07 | 2020-09-10 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator |
| US12318403B2 (en) | 2019-03-07 | 2025-06-03 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 2′3′-cyclic dinucleotides and prodrugs thereof |
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-
2015
- 2015-08-26 EA EA201790154A patent/EA201790154A1/ru unknown
- 2015-08-26 SG SG11201701182VA patent/SG11201701182VA/en unknown
- 2015-08-26 AU AU2015306662A patent/AU2015306662A1/en not_active Abandoned
- 2015-08-26 CN CN201580046345.3A patent/CN107074807A/zh active Pending
- 2015-08-26 MX MX2017002451A patent/MX2017002451A/es unknown
- 2015-08-26 MA MA040470A patent/MA40470A/fr unknown
- 2015-08-26 KR KR1020177006855A patent/KR20170040805A/ko not_active Withdrawn
- 2015-08-26 BR BR112017003442A patent/BR112017003442A2/pt not_active Application Discontinuation
- 2015-08-26 AR ARP150102728A patent/AR101692A1/es unknown
- 2015-08-26 TW TW104127904A patent/TW201625536A/zh unknown
- 2015-08-26 CA CA2957947A patent/CA2957947A1/en not_active Abandoned
- 2015-08-26 JP JP2017510881A patent/JP2017526675A/ja not_active Withdrawn
- 2015-08-26 EP EP15759595.0A patent/EP3186238A1/en not_active Withdrawn
- 2015-08-26 WO PCT/US2015/046921 patent/WO2016033169A1/en not_active Ceased
- 2015-08-26 US US14/836,397 patent/US9802941B2/en active Active
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2017
- 2017-01-30 IL IL250355A patent/IL250355A0/en unknown
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