JP2019508496A5 - - Google Patents
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- JP2019508496A5 JP2019508496A5 JP2018561082A JP2018561082A JP2019508496A5 JP 2019508496 A5 JP2019508496 A5 JP 2019508496A5 JP 2018561082 A JP2018561082 A JP 2018561082A JP 2018561082 A JP2018561082 A JP 2018561082A JP 2019508496 A5 JP2019508496 A5 JP 2019508496A5
- Authority
- JP
- Japan
- Prior art keywords
- alkylene
- alkyl
- ring
- pharmaceutical composition
- composition according
- 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.)
- Pending
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- 125000002947 alkylene group Chemical group 0.000 claims 263
- 125000000217 alkyl group Chemical group 0.000 claims 216
- 239000008194 pharmaceutical composition Substances 0.000 claims 29
- -1 benzodioxanyl Chemical group 0.000 claims 22
- 150000001875 compounds Chemical class 0.000 claims 18
- 125000001188 haloalkyl group Chemical group 0.000 claims 18
- 229910052799 carbon Inorganic materials 0.000 claims 16
- 125000006413 ring segment Chemical group 0.000 claims 14
- 150000001721 carbon Chemical group 0.000 claims 12
- 229910052736 halogen Inorganic materials 0.000 claims 11
- 125000003342 alkenyl group Chemical group 0.000 claims 10
- 125000000304 alkynyl group Chemical group 0.000 claims 10
- 125000004122 cyclic group Chemical group 0.000 claims 10
- 125000001072 heteroaryl group Chemical group 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 8
- 239000000651 prodrug Substances 0.000 claims 8
- 229940002612 prodrug Drugs 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 239000012453 solvate Substances 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 239000003112 inhibitor Substances 0.000 claims 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- 125000003118 aryl group Chemical group 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 201000011510 cancer Diseases 0.000 claims 5
- 108091005625 BRD4 Proteins 0.000 claims 3
- 102100029895 Bromodomain-containing protein 4 Human genes 0.000 claims 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- 101000596093 Homo sapiens Transcription initiation factor TFIID subunit 1 Proteins 0.000 claims 3
- 102100035222 Transcription initiation factor TFIID subunit 1 Human genes 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 125000005877 1,4-benzodioxanyl group Chemical group 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- 201000004253 NUT midline carcinoma Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- QECMENZMDBOLDR-AWEZNQCLSA-N cpi 203 Chemical compound N([C@@H](CC(N)=O)C1=NN=C(N1C=1SC(C)=C(C)C=11)C)=C1C1=CC=C(Cl)C=C1 QECMENZMDBOLDR-AWEZNQCLSA-N 0.000 claims 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 208000005017 glioblastoma Diseases 0.000 claims 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 201000001514 prostate carcinoma Diseases 0.000 claims 2
- AAAQFGUYHFJNHI-SFHVURJKSA-N 2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide Chemical compound N([C@H](C1=NN=C(C)N1C1=CC=C(OC)C=C11)CC(=O)NCC)=C1C1=CC=C(Cl)C=C1 AAAQFGUYHFJNHI-SFHVURJKSA-N 0.000 claims 1
- GNMUEVRJHCWKTO-FQEVSTJZSA-N 6h-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-n-(4-hydroxyphenyl)-2,3,9-trimethyl-, (6s)- Chemical compound C([C@@H]1N=C(C2=C(N3C(C)=NN=C31)SC(=C2C)C)C=1C=CC(Cl)=CC=1)C(=O)NC1=CC=C(O)C=C1 GNMUEVRJHCWKTO-FQEVSTJZSA-N 0.000 claims 1
- VUVUVNZRUGEAHB-CYBMUJFWSA-N 7-(3,5-dimethyl-4-isoxazolyl)-8-methoxy-1-[(1R)-1-(2-pyridinyl)ethyl]-3H-imidazo[4,5-c]quinolin-2-one Chemical compound C1([C@@H](C)N2C3=C4C=C(C(=CC4=NC=C3NC2=O)C2=C(ON=C2C)C)OC)=CC=CC=N1 VUVUVNZRUGEAHB-CYBMUJFWSA-N 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- NETXMUIMUZJUTB-UHFFFAOYSA-N apabetalone Chemical compound C=1C(OC)=CC(OC)=C(C(N2)=O)C=1N=C2C1=CC(C)=C(OCCO)C(C)=C1 NETXMUIMUZJUTB-UHFFFAOYSA-N 0.000 claims 1
- BNBQRQQYDMDJAH-UHFFFAOYSA-N benzodioxan Chemical compound C1=CC=C2OCCOC2=C1 BNBQRQQYDMDJAH-UHFFFAOYSA-N 0.000 claims 1
- XQVVPGYIWAGRNI-JOCHJYFZSA-N bi-2536 Chemical compound N1([C@@H](C(N(C)C2=CN=C(NC=3C(=CC(=CC=3)C(=O)NC3CCN(C)CC3)OC)N=C21)=O)CC)C1CCCC1 XQVVPGYIWAGRNI-JOCHJYFZSA-N 0.000 claims 1
- 229950000080 birabresib Drugs 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- NCACTGQDGOLTBA-UHFFFAOYSA-N n-[2-(cyclohexen-1-yl)ethyl]-3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-6-amine Chemical group N=1N2C(C)=NN=C2C=CC=1NCCC1=CCCCC1 NCACTGQDGOLTBA-UHFFFAOYSA-N 0.000 claims 1
- GCWIQUVXWZWCLE-INIZCTEOSA-N pelabresib Chemical compound N([C@@H](CC(N)=O)C=1ON=C(C=1C1=CC=CC=C11)C)=C1C1=CC=C(Cl)C=C1 GCWIQUVXWZWCLE-INIZCTEOSA-N 0.000 claims 1
- PRZDOWJHTJFLIF-UHFFFAOYSA-N CC1=CC(C(CCC2)NC(c(cc3)ccc3OC(F)(F)F)=O)=C2N(C)C1=O Chemical compound CC1=CC(C(CCC2)NC(c(cc3)ccc3OC(F)(F)F)=O)=C2N(C)C1=O PRZDOWJHTJFLIF-UHFFFAOYSA-N 0.000 description 1
- HYAAYYCEQJOIOZ-UHFFFAOYSA-N CN(C(CCCC1NC(c(cc2)ccc2OC)=O)=C1C=C1)C1=O Chemical compound CN(C(CCCC1NC(c(cc2)ccc2OC)=O)=C1C=C1)C1=O HYAAYYCEQJOIOZ-UHFFFAOYSA-N 0.000 description 1
- RQINZRYJDPRIEE-UHFFFAOYSA-N CN1c2cccc(NC(c(cc3)ccc3OC)=O)c2C(C2)C2C1=O Chemical compound CN1c2cccc(NC(c(cc3)ccc3OC)=O)c2C(C2)C2C1=O RQINZRYJDPRIEE-UHFFFAOYSA-N 0.000 description 1
- ADPICLVTHDAYMC-ARLHGKGLSA-N C[N-](C(CCC1)=C(C=C2)/C1=N/C(C(C[C@H](C1)OC)=CC1OC)=O)C2=O Chemical compound C[N-](C(CCC1)=C(C=C2)/C1=N/C(C(C[C@H](C1)OC)=CC1OC)=O)C2=O ADPICLVTHDAYMC-ARLHGKGLSA-N 0.000 description 1
- GUDYUROMTNBASD-UHFFFAOYSA-N Cc1cc(NC(c2cc(OC)cc(OC)c2)=O)c(C=CC(N2C)=O)c2c1 Chemical compound Cc1cc(NC(c2cc(OC)cc(OC)c2)=O)c(C=CC(N2C)=O)c2c1 GUDYUROMTNBASD-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16155781 | 2016-02-15 | ||
| EP16155781.4 | 2016-02-15 | ||
| PCT/EP2017/053403 WO2017140728A1 (en) | 2016-02-15 | 2017-02-15 | Taf1 inhibitors for the therapy of cancer |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019508496A JP2019508496A (ja) | 2019-03-28 |
| JP2019508496A5 true JP2019508496A5 (enExample) | 2020-03-26 |
Family
ID=55359457
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018561082A Pending JP2019508496A (ja) | 2016-02-15 | 2017-02-15 | 癌の治療法のためのｔａｆ１阻害剤 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US10702518B2 (enExample) |
| EP (1) | EP3416947A1 (enExample) |
| JP (1) | JP2019508496A (enExample) |
| KR (1) | KR20180134860A (enExample) |
| CN (1) | CN109153647A (enExample) |
| AU (1) | AU2017220611A1 (enExample) |
| CA (1) | CA3013988A1 (enExample) |
| IL (1) | IL261047A (enExample) |
| MX (1) | MX2018009870A (enExample) |
| WO (1) | WO2017140728A1 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11130740B2 (en) | 2017-04-25 | 2021-09-28 | Arbutus Biopharma Corporation | Substituted 2,3-dihydro-1H-indene analogs and methods using same |
| CA3093851A1 (en) | 2018-03-29 | 2019-10-03 | Arbutus Biopharma Corporation | Substituted 1,1'-biphenyl compounds, analogues thereof, and methods using same |
| GB201913110D0 (en) * | 2019-09-11 | 2019-10-23 | Benevolentai Bio Ltd | New compounds and methods |
| WO2021074418A1 (en) * | 2019-10-16 | 2021-04-22 | Cemm - Forschungszentrum Für Molekulare Medizin Gmbh | Carbazole-type cullin ring ubiquitin ligase compounds and uses thereof |
| CN115666562B (zh) * | 2020-04-08 | 2026-03-27 | 鲁米科学控股股份有限公司 | 溴结构域抑制剂治疗亨廷顿病的用途 |
| CN115397412B (zh) * | 2020-04-17 | 2025-03-25 | 伊赛恩特制药公司 | Mas相关g蛋白受体x4的调节剂及相关产物和方法 |
| WO2022115753A1 (en) * | 2020-11-30 | 2022-06-02 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Merged scaffold taf1 inhibitors |
| JPWO2022138944A1 (enExample) * | 2020-12-25 | 2022-06-30 | ||
| US20240252662A1 (en) * | 2021-05-20 | 2024-08-01 | Case Western Reserve University | Peptide drug conjugates specific to fibronectin isotypes for cancer therapy |
| CN115710202B (zh) * | 2021-08-23 | 2024-05-03 | 江西同和药业股份有限公司 | 一种阿帕他酮关键中间体的制备方法及其应用 |
| IT202100022682A1 (it) * | 2021-09-01 | 2023-03-01 | Luigi Frati | Derivati pirimidinici e loro uso nel trattamento di tumori |
| WO2024206937A2 (en) * | 2023-03-30 | 2024-10-03 | Purdue Research Foundation | Bi-aryl methylated lactam derivatives and related compositions and method of use to inhibit the proliferation of cancerous cells |
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| US3773919A (en) | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
| US4263428A (en) | 1978-03-24 | 1981-04-21 | The Regents Of The University Of California | Bis-anthracycline nucleic acid function inhibitors and improved method for administering the same |
| DE3169595D1 (en) | 1980-11-10 | 1985-05-02 | Gersonde Klaus | Method of preparing lipid vesicles by ultrasonic treatment, the use of this method and apparatus for its application |
| US4485045A (en) | 1981-07-06 | 1984-11-27 | Research Corporation | Synthetic phosphatidyl cholines useful in forming liposomes |
| DE3374837D1 (en) | 1982-02-17 | 1988-01-21 | Ciba Geigy Ag | Lipids in the aqueous phase |
| DE3218121A1 (de) | 1982-05-14 | 1983-11-17 | Leskovar, Peter, Dr.-Ing., 8000 München | Arzneimittel zur tumorbehandlung |
| EP0102324A3 (de) | 1982-07-29 | 1984-11-07 | Ciba-Geigy Ag | Lipide und Tenside in wässriger Phase |
| US4544545A (en) | 1983-06-20 | 1985-10-01 | Trustees University Of Massachusetts | Liposomes containing modified cholesterol for organ targeting |
| HUT35524A (en) | 1983-08-02 | 1985-07-29 | Hoechst Ag | Process for preparing pharmaceutical compositions containing regulatory /regulative/ peptides providing for the retarded release of the active substance |
| ATE159858T1 (de) | 1983-09-26 | 1997-11-15 | Ehrenfeld Udo | Mittel und erzeugnis für die diagnose und therapie von tumoren sowie zur behandlung von schwächen der zelligen und humoralen immunabwehr |
| US4615885A (en) | 1983-11-01 | 1986-10-07 | Terumo Kabushiki Kaisha | Pharmaceutical composition containing urokinase |
| US6051256A (en) | 1994-03-07 | 2000-04-18 | Inhale Therapeutic Systems | Dispersible macromolecule compositions and methods for their preparation and use |
| DE69813853T3 (de) | 1997-09-29 | 2011-05-12 | Novartis Ag | Perforierte mikroteilchen und deren verwendung |
| KR100508289B1 (ko) | 1998-04-21 | 2005-08-17 | 마이크로메트 에이지 | Ｃｄ１９×ｃｄ３ 특이 폴리펩티드 및 그의 용도 |
| US7442388B2 (en) | 2000-05-10 | 2008-10-28 | Weers Jeffry G | Phospholipid-based powders for drug delivery |
| US7368102B2 (en) | 2001-12-19 | 2008-05-06 | Nektar Therapeutics | Pulmonary delivery of aminoglycosides |
| JP2005060247A (ja) * | 2003-08-12 | 2005-03-10 | Takeda Chem Ind Ltd | イソキノリノン誘導体、その製造法および用途 |
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| TWI425945B (zh) * | 2007-05-28 | 2014-02-11 | Seldar Pharma Inc | 四氫異喹啉－１－酮衍生物或其鹽 |
| US8642660B2 (en) * | 2007-12-21 | 2014-02-04 | The University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
| CN101497584B (zh) * | 2008-01-29 | 2010-12-22 | 首都医科大学 | 异喹啉-3-甲酰氨基酸苄酯及其制备和应用 |
| JP5478637B2 (ja) | 2008-12-23 | 2014-04-23 | エフ．ホフマン−ラ ロシュ アーゲー | Ｐ２ｘ７モジュレーターとしてのジヒドロピリドンアミド |
| US9328117B2 (en) | 2011-06-17 | 2016-05-03 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| WO2013027168A1 (en) | 2011-08-22 | 2013-02-28 | Pfizer Inc. | Novel heterocyclic compounds as bromodomain inhibitors |
| BR112014011173A2 (pt) | 2011-11-09 | 2017-05-09 | Abbvie Deutschland | carboxamidas heterocíclicas úteis como inibidores de fosfodiesterase tipo 10a |
| US8940742B2 (en) * | 2012-04-10 | 2015-01-27 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
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| ES2857687T3 (es) | 2013-01-31 | 2021-09-29 | Vertex Pharma | Piridona amidas como moduladores de los canales de sodio |
| AU2014223990A1 (en) | 2013-02-28 | 2015-09-10 | Washington University | Methods of treatment of human cytomegalovirus infection and diseases with bromodomain inhibitors |
| US8975417B2 (en) | 2013-05-27 | 2015-03-10 | Novartis Ag | Pyrazolopyrrolidine derivatives and their use in the treatment of disease |
| CA2913697A1 (en) | 2013-05-27 | 2014-12-04 | Novartis Ag | Imidazopyrrolidinone derivatives and their use in the treatment of disease |
| CA2912986A1 (en) | 2013-05-28 | 2014-12-04 | Novartis Ag | Pyrazolo-pyrrolidin-4-one derivatives as bet inhibitors and their use in the treatment of disease |
| WO2015106272A1 (en) | 2014-01-13 | 2015-07-16 | Harki Daniel A | Small molecule inhibitors of apobec3g and apobec3b |
| WO2016004417A1 (en) | 2014-07-03 | 2016-01-07 | Board Of Regents, University Of Texas System | Gls1 inhibitors for treating disease |
| ES2896400T3 (es) | 2014-08-01 | 2022-02-24 | Nuevolution As | Compuestos activos frente a bromdominios |
-
2017
- 2017-02-15 MX MX2018009870A patent/MX2018009870A/es unknown
- 2017-02-15 JP JP2018561082A patent/JP2019508496A/ja active Pending
- 2017-02-15 AU AU2017220611A patent/AU2017220611A1/en not_active Abandoned
- 2017-02-15 CN CN201780022602.9A patent/CN109153647A/zh active Pending
- 2017-02-15 WO PCT/EP2017/053403 patent/WO2017140728A1/en not_active Ceased
- 2017-02-15 KR KR1020187026762A patent/KR20180134860A/ko not_active Withdrawn
- 2017-02-15 US US16/077,913 patent/US10702518B2/en not_active Expired - Fee Related
- 2017-02-15 EP EP17708985.1A patent/EP3416947A1/en not_active Withdrawn
- 2017-02-15 CA CA3013988A patent/CA3013988A1/en not_active Abandoned
-
2018
- 2018-08-08 IL IL261047A patent/IL261047A/en unknown