CA2989313A1 - Treatment of nut midline carcinoma - Google Patents
Treatment of nut midline carcinomaInfo
- Publication number
- CA2989313A1 CA2989313A1 CA2989313A CA2989313A CA2989313A1 CA 2989313 A1 CA2989313 A1 CA 2989313A1 CA 2989313 A CA2989313 A CA 2989313A CA 2989313 A CA2989313 A CA 2989313A CA 2989313 A1 CA2989313 A1 CA 2989313A1
- Authority
- CA
- Canada
- Prior art keywords
- alkyl
- alkylene
- cycloalkyl
- heterocycloalkyl
- aryl
- 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.)
- Abandoned
Links
- 201000004253 NUT midline carcinoma Diseases 0.000 title claims abstract description 67
- 238000011282 treatment Methods 0.000 title claims description 26
- 229940125763 bromodomain inhibitor Drugs 0.000 claims abstract description 77
- 238000000034 method Methods 0.000 claims abstract description 57
- 230000014509 gene expression Effects 0.000 claims abstract description 49
- 101001046686 Homo sapiens Integrin alpha-M Proteins 0.000 claims abstract description 48
- 102100022338 Integrin alpha-M Human genes 0.000 claims abstract description 47
- 101710137446 NUT family member 1 Proteins 0.000 claims abstract description 33
- 102100027086 NUT family member 1 Human genes 0.000 claims abstract description 31
- 238000011269 treatment regimen Methods 0.000 claims abstract description 30
- 201000009030 Carcinoma Diseases 0.000 claims abstract description 11
- 125000001424 substituent group Chemical group 0.000 claims description 153
- 125000003118 aryl group Chemical group 0.000 claims description 134
- 125000001072 heteroaryl group Chemical group 0.000 claims description 130
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 127
- 150000001875 compounds Chemical class 0.000 claims description 78
- 239000003814 drug Substances 0.000 claims description 75
- 229940079593 drug Drugs 0.000 claims description 65
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 54
- 150000003839 salts Chemical class 0.000 claims description 54
- 125000005275 alkylenearyl group Chemical group 0.000 claims description 29
- 125000005218 alkyleneheteroaryl group Chemical group 0.000 claims description 29
- 229910052736 halogen Inorganic materials 0.000 claims description 22
- 150000002367 halogens Chemical class 0.000 claims description 22
- 229910052757 nitrogen Inorganic materials 0.000 claims description 21
- 125000006652 (C3-C12) cycloalkyl group Chemical group 0.000 claims description 18
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 16
- 125000004429 atom Chemical group 0.000 claims description 16
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- 125000005843 halogen group Chemical group 0.000 claims description 12
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- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 9
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- 238000012544 monitoring process Methods 0.000 claims description 5
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims description 4
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims description 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 4
- 125000006707 (C3-C12) heterocycloalkyl group Chemical group 0.000 claims description 3
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- 230000004043 responsiveness Effects 0.000 abstract description 11
- 125000000217 alkyl group Chemical group 0.000 description 582
- -1 hydrocarbon radical Chemical class 0.000 description 83
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 70
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 46
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 38
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 32
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- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 32
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- 125000000753 cycloalkyl group Chemical group 0.000 description 28
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- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 24
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- 125000003545 alkoxy group Chemical group 0.000 description 20
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- PKQXLRYFPSZKDU-QFIPXVFZSA-N 2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]-N-[3-(4-methylpiperazin-1-yl)propyl]acetamide Chemical compound C1CN(C)CCN1CCCNC(=O)C[C@H]1C2=NN=C(C)N2C(SC(C)=C2C)=C2C(C=2C=CC(Cl)=CC=2)=N1 PKQXLRYFPSZKDU-QFIPXVFZSA-N 0.000 description 19
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- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 14
- 125000002950 monocyclic group Chemical group 0.000 description 14
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- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 description 10
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- 125000004356 hydroxy functional group Chemical group O* 0.000 description 7
- 125000001041 indolyl group Chemical group 0.000 description 7
- 102100033642 Bromodomain-containing protein 3 Human genes 0.000 description 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 6
- 101000871851 Homo sapiens Bromodomain-containing protein 3 Proteins 0.000 description 6
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical group C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 description 6
- 108010004729 Phycoerythrin Proteins 0.000 description 6
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical group C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 description 6
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 6
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical group C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 description 6
- 239000002253 acid Substances 0.000 description 6
- 238000009472 formulation Methods 0.000 description 6
- 125000000842 isoxazolyl group Chemical group 0.000 description 6
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- 125000000168 pyrrolyl group Chemical group 0.000 description 6
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- 125000000335 thiazolyl group Chemical group 0.000 description 6
- 125000005032 thiofuranyl group Chemical group S1C(=CC=C1)* 0.000 description 6
- 125000001425 triazolyl group Chemical group 0.000 description 6
- 125000004606 5,6,7,8-tetrahydroisoquinolinyl group Chemical group C1(=NC=CC=2CCCCC12)* 0.000 description 5
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- 125000004122 cyclic group Chemical group 0.000 description 5
- LOKCTEFSRHRXRJ-UHFFFAOYSA-I dipotassium trisodium dihydrogen phosphate hydrogen phosphate dichloride Chemical compound P(=O)(O)(O)[O-].[K+].P(=O)(O)([O-])[O-].[Na+].[Na+].[Cl-].[K+].[Cl-].[Na+] LOKCTEFSRHRXRJ-UHFFFAOYSA-I 0.000 description 5
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- 238000007920 subcutaneous administration Methods 0.000 description 5
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Classifications
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
- G01N33/574—Immunoassay; Biospecific binding assay; Materials therefor for cancer
- G01N33/57407—Specifically defined cancers
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- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
- G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
- G01N2333/705—Assays involving receptors, cell surface antigens or cell surface determinants
- G01N2333/70546—Integrin superfamily, e.g. VLAs, leuCAM, GPIIb/GPIIIa, LPAM
- G01N2333/70553—Integrin beta2-subunit-containing molecules, e.g. CD11, CD18
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- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2800/00—Detection or diagnosis of diseases
- G01N2800/52—Predicting or monitoring the response to treatment, e.g. for selection of therapy based on assay results in personalised medicine; Prognosis
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- Chemical & Material Sciences (AREA)
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- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Investigating Or Analysing Biological Materials (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
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| PCT/US2016/039270 WO2016210275A1 (en) | 2015-06-26 | 2016-06-24 | Treatment of nut midline carcinoma |
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| CA2989313A1 true CA2989313A1 (en) | 2016-12-29 |
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| BR (1) | BR112017028178A2 (enExample) |
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| HUE031073T2 (en) | 2010-05-14 | 2017-06-28 | Dana Farber Cancer Inst Inc | Thieno triazolo-diazepine compounds for the treatment of neoplasia |
| RU2016122654A (ru) | 2013-11-08 | 2017-12-14 | Дана-Фарбер Кэнсер Инститьют, Инк. | Комбинированная терапия злокачественной опухоли с использованием ингибиторов бромодоменового и экстратерминального (вет) белка |
| CA2940472A1 (en) | 2014-02-28 | 2015-09-03 | Tensha Therapeutics, Inc. | Treatment of conditions associated with hyperinsulinaemia |
| EA033325B1 (ru) | 2014-10-27 | 2019-09-30 | Тэнша Терапеутикс, Инк. | Ингибиторы бромодомена |
| WO2024123929A1 (en) * | 2022-12-06 | 2024-06-13 | Bioventures, Llc | Development of potent dual hdac/brd4 inhibitors |
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| GB0919426D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| ES2652304T3 (es) | 2009-11-05 | 2018-02-01 | Glaxosmithkline Llc | Compuesto de benzodiacepina novedoso |
| HUE031073T2 (en) | 2010-05-14 | 2017-06-28 | Dana Farber Cancer Inst Inc | Thieno triazolo-diazepine compounds for the treatment of neoplasia |
| JP5715241B2 (ja) * | 2010-05-14 | 2015-05-07 | ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド | 新生物、炎症性疾患、およびその他の障害を治療するための組成物および方法 |
| WO2011161031A1 (en) | 2010-06-22 | 2011-12-29 | Glaxosmithkline Llc | Benzotriazolodiazepine compounds inhibitors of bromodomains |
| WO2012075456A1 (en) | 2010-12-02 | 2012-06-07 | Constellation Pharmaceuticals | Bromodomain inhibitors and uses thereof |
| AR084070A1 (es) | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| EP2705039B1 (en) | 2011-05-04 | 2017-07-26 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| EP2721031B1 (en) | 2011-06-17 | 2016-01-20 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| TWI602820B (zh) | 2012-06-06 | 2017-10-21 | 星宿藥物公司 | 溴域抑制劑及其用途 |
| CA2940472A1 (en) | 2014-02-28 | 2015-09-03 | Tensha Therapeutics, Inc. | Treatment of conditions associated with hyperinsulinaemia |
-
2016
- 2016-06-24 AU AU2016283020A patent/AU2016283020A1/en not_active Abandoned
- 2016-06-24 MA MA042249A patent/MA42249A/fr unknown
- 2016-06-24 CA CA2989313A patent/CA2989313A1/en not_active Abandoned
- 2016-06-24 HK HK18111394.9A patent/HK1252062A1/zh unknown
- 2016-06-24 JP JP2017563973A patent/JP2018520124A/ja active Pending
- 2016-06-24 EP EP16738292.8A patent/EP3314005A1/en not_active Withdrawn
- 2016-06-24 US US15/739,905 patent/US20180193350A1/en not_active Abandoned
- 2016-06-24 KR KR1020187000569A patent/KR20180035785A/ko not_active Withdrawn
- 2016-06-24 WO PCT/US2016/039270 patent/WO2016210275A1/en not_active Ceased
- 2016-06-24 AR ARP160101908A patent/AR105124A1/es unknown
- 2016-06-24 MX MX2017016337A patent/MX2017016337A/es unknown
- 2016-06-24 CN CN201680036201.4A patent/CN107787227A/zh active Pending
- 2016-06-24 BR BR112017028178A patent/BR112017028178A2/pt not_active Application Discontinuation
-
2017
- 2017-12-07 IL IL256186A patent/IL256186A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| BR112017028178A2 (pt) | 2018-08-28 |
| CN107787227A (zh) | 2018-03-09 |
| MX2017016337A (es) | 2018-11-22 |
| AU2016283020A1 (en) | 2018-01-04 |
| MA42249A (fr) | 2018-05-02 |
| KR20180035785A (ko) | 2018-04-06 |
| IL256186A (en) | 2018-02-28 |
| WO2016210275A1 (en) | 2016-12-29 |
| EP3314005A1 (en) | 2018-05-02 |
| US20180193350A1 (en) | 2018-07-12 |
| AR105124A1 (es) | 2017-09-06 |
| HK1252062A1 (zh) | 2019-05-10 |
| JP2018520124A (ja) | 2018-07-26 |
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