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) |
Families Citing this family (54)
| Publication number | Priority date | Publication date | Assignee | Title |
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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 |
| BR102017010009A2 (pt) | 2016-05-27 | 2017-12-12 | Gilead Sciences, Inc. | Compounds for the treatment of hepatitis b virus infection |
| SG11201809893WA (en) | 2016-05-27 | 2018-12-28 | Gilead Sciences Inc | Methods for treating hepatitis b virus infections using ns5a, ns5b or ns3 inhibitors |
| JOP20190024A1 (ar) | 2016-08-26 | 2019-02-19 | Gilead Sciences Inc | مركبات بيروليزين بها استبدال واستخداماتها |
| AU2017318601B2 (en) | 2016-09-02 | 2020-09-03 | Gilead Sciences, Inc. | Toll like receptor modulator compounds |
| EP3507288B1 (en) | 2016-09-02 | 2020-08-26 | Gilead Sciences, Inc. | 4,6-diamino-pyrido[3,2-d]pyrimidine derivaties as toll like receptor modulators |
| US10662416B2 (en) | 2016-10-14 | 2020-05-26 | Precision Biosciences, Inc. | Engineered meganucleases specific for recognition sequences in the hepatitis B virus genome |
| TWI820984B (zh) | 2017-01-31 | 2023-11-01 | 美商基利科學股份有限公司 | 替諾福韋埃拉酚胺(tenofovir alafenamide)之晶型 |
| JOP20180008A1 (ar) | 2017-02-02 | 2019-01-30 | Gilead Sciences Inc | مركبات لعلاج إصابة بعدوى فيروس الالتهاب الكبدي b |
| JOP20180040A1 (ar) | 2017-04-20 | 2019-01-30 | Gilead Sciences Inc | مثبطات pd-1/pd-l1 |
| 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 |
| CN111511754B (zh) | 2017-12-20 | 2023-09-12 | 捷克共和国有机化学与生物化学研究所 | 活化sting转接蛋白的具有膦酸酯键的2’3’环状二核苷酸 |
| KR102492187B1 (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 3'3' 사이클릭 다이뉴클레오티드 |
| 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 |
| TWI796596B (zh) | 2018-02-13 | 2023-03-21 | 美商基利科學股份有限公司 | Pd‐1/pd‐l1抑制劑 |
| KR102526964B1 (ko) | 2018-02-26 | 2023-04-28 | 길리애드 사이언시즈, 인코포레이티드 | Hbv 복제 억제제로서의 치환된 피롤리진 화합물 |
| EP3774883A1 (en) | 2018-04-05 | 2021-02-17 | Gilead Sciences, Inc. | Antibodies and fragments thereof that bind hepatitis b virus protein x |
| 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 |
| TWI818007B (zh) | 2018-04-06 | 2023-10-11 | 捷克科學院有機化學與生物化學研究所 | 2'3'-環二核苷酸 |
| 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 |
| TW201945388A (zh) | 2018-04-12 | 2019-12-01 | 美商精密生物科學公司 | 對b型肝炎病毒基因體中之識別序列具有特異性之最佳化之經工程化巨核酸酶 |
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| JP7158577B2 (ja) | 2018-10-24 | 2022-10-21 | ギリアード サイエンシーズ， インコーポレイテッド | Ｐｄ－１／ｐｄ－ｌ１阻害剤 |
| KR102658602B1 (ko) | 2018-10-31 | 2024-04-19 | 길리애드 사이언시즈, 인코포레이티드 | Hpk1 억제 활성을 갖는 치환된 6-아자벤즈이미다졸 화합물 |
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| 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 |
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-
2015
- 2015-08-26 SG SG11201701182VA patent/SG11201701182VA/en unknown
- 2015-08-26 JP JP2017510881A patent/JP2017526675A/ja not_active Withdrawn
- 2015-08-26 BR BR112017003442A patent/BR112017003442A2/pt not_active Application Discontinuation
- 2015-08-26 AU AU2015306662A patent/AU2015306662A1/en not_active Abandoned
- 2015-08-26 MX MX2017002451A patent/MX2017002451A/es unknown
- 2015-08-26 CN CN201580046345.3A patent/CN107074807A/zh active Pending
- 2015-08-26 TW TW104127904A patent/TW201625536A/zh unknown
- 2015-08-26 US US14/836,397 patent/US9802941B2/en active Active
- 2015-08-26 WO PCT/US2015/046921 patent/WO2016033169A1/en not_active Ceased
- 2015-08-26 KR KR1020177006855A patent/KR20170040805A/ko not_active Withdrawn
- 2015-08-26 AR ARP150102728A patent/AR101692A1/es unknown
- 2015-08-26 EA EA201790154A patent/EA201790154A1/ru unknown
- 2015-08-26 EP EP15759595.0A patent/EP3186238A1/en not_active Withdrawn
- 2015-08-26 CA CA2957947A patent/CA2957947A1/en not_active Abandoned
- 2015-08-26 MA MA040470A patent/MA40470A/fr unknown
-
2017
- 2017-01-30 IL IL250355A patent/IL250355A0/en unknown
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