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 |
| US12083118B2 (en) | 2018-03-29 | 2024-09-10 | 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 |
| IL296984A (en) * | 2020-04-08 | 2022-12-01 | Rumi Scient Holdings Inc | Use of bromodomain inhibitors for treatment of huntington’s disease |
| AU2021255966A1 (en) * | 2020-04-17 | 2022-11-17 | Escient Pharmaceuticals, Inc. | Modulators of mas-related G-protein receptor X4 and related products and methods |
| US20240002378A1 (en) * | 2020-11-30 | 2024-01-04 | 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 |
| EP0052322B1 (de) | 1980-11-10 | 1985-03-27 | Gersonde, Klaus, Prof. Dr. | Verfahren zur Herstellung von Lipid-Vesikeln durch Ultraschallbehandlung, Anwendung des Verfahrens und Vorrichtung zur Durchführung des Verfahrens |
| 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 |
| DE3483949D1 (de) | 1983-09-26 | 1991-02-21 | Udo Dr Med Ehrenfeld | Mittel und erzeugnis fuer die diagnose und therapie von tumoren sowie zur behandlung von schwaechen der zelligen und humoralen immunabwehr. |
| DE3474511D1 (en) | 1983-11-01 | 1988-11-17 | Terumo Corp | 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 |
| NZ503464A (en) | 1997-09-29 | 2002-05-31 | Inhale Therapeutic Syst | Perforated microparticles containing a bioactive agent for pulmonary delivery |
| EP1071752B1 (en) | 1998-04-21 | 2003-07-09 | Micromet AG | CD19xCD3 SPECIFIC POLYPEPTIDES AND USES THEREOF |
| CA2382133C (en) | 2000-05-10 | 2010-11-23 | Alliance Pharmaceutical Corporation | Phospholipid-based powders for drug delivery |
| EP1458360B1 (en) | 2001-12-19 | 2011-05-11 | Novartis AG | 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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| AU2008345225A1 (en) * | 2007-12-21 | 2009-07-09 | 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 |
| CN102264723B (zh) | 2008-12-23 | 2014-12-10 | 霍夫曼-拉罗奇有限公司 | 作为p2x7调节剂的二氢吡啶酮酰胺 |
| WO2012174487A2 (en) | 2011-06-17 | 2012-12-20 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| WO2013027168A1 (en) | 2011-08-22 | 2013-02-28 | Pfizer Inc. | Novel heterocyclic compounds as bromodomain inhibitors |
| EP2780324B1 (en) | 2011-11-09 | 2017-05-17 | Abbvie Deutschland GmbH & Co. KG | Heterocyclic carboxamides useful as inhibitors of phosphodiesterase type 10a |
| US8940742B2 (en) * | 2012-04-10 | 2015-01-27 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
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| JP2016510039A (ja) | 2013-02-28 | 2016-04-04 | ワシントン・ユニバーシティＷａｓｈｉｎｇｔｏｎ Ｕｎｉｖｅｒｓｉｔｙ | ブロモドメイン阻害剤によるヒトサイトメガロウイルス感染および疾患の治療方法 |
| US8975417B2 (en) | 2013-05-27 | 2015-03-10 | Novartis Ag | Pyrazolopyrrolidine derivatives and their use in the treatment of disease |
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| 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 |
| KR102633122B1 (ko) * | 2014-08-01 | 2024-02-05 | 누에볼루션 에이/에스 | 브로모도메인에 대하여 활성을 갖는 화합물 |
-
2017
- 2017-02-15 EP EP17708985.1A patent/EP3416947A1/en not_active Withdrawn
- 2017-02-15 KR KR1020187026762A patent/KR20180134860A/ko not_active Withdrawn
- 2017-02-15 WO PCT/EP2017/053403 patent/WO2017140728A1/en not_active Ceased
- 2017-02-15 CA CA3013988A patent/CA3013988A1/en not_active Abandoned
- 2017-02-15 MX MX2018009870A patent/MX2018009870A/es unknown
- 2017-02-15 AU AU2017220611A patent/AU2017220611A1/en not_active Abandoned
- 2017-02-15 JP JP2018561082A patent/JP2019508496A/ja active Pending
- 2017-02-15 CN CN201780022602.9A patent/CN109153647A/zh active Pending
- 2017-02-15 US US16/077,913 patent/US10702518B2/en not_active Expired - Fee Related
-
2018
- 2018-08-08 IL IL261047A patent/IL261047A/en unknown