AR114168A1 - Compuestos y su uso en el tratamiento del cáncer - Google Patents
Compuestos y su uso en el tratamiento del cáncerInfo
- Publication number
- AR114168A1 AR114168A1 ARP180103831A ARP180103831A AR114168A1 AR 114168 A1 AR114168 A1 AR 114168A1 AR P180103831 A ARP180103831 A AR P180103831A AR P180103831 A ARP180103831 A AR P180103831A AR 114168 A1 AR114168 A1 AR 114168A1
- Authority
- AR
- Argentina
- Prior art keywords
- methyl
- compounds
- pharmaceutically acceptable
- independently selected
- treatment
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 206010028980 Neoplasm Diseases 0.000 title abstract 2
- 201000011510 cancer Diseases 0.000 title abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 7
- 125000004432 carbon atom Chemical group C* 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 125000005647 linker group Chemical group 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 2
- 239000000651 prodrug Substances 0.000 abstract 2
- 229940002612 prodrug Drugs 0.000 abstract 2
- XXJGBENTLXFVFI-UHFFFAOYSA-N 1-amino-methylene Chemical compound N[CH2] XXJGBENTLXFVFI-UHFFFAOYSA-N 0.000 abstract 1
- JNCMHMUGTWEVOZ-UHFFFAOYSA-N F[CH]F Chemical compound F[CH]F JNCMHMUGTWEVOZ-UHFFFAOYSA-N 0.000 abstract 1
- 108010081348 HRT1 protein Hairy Proteins 0.000 abstract 1
- 102100021881 Hairy/enhancer-of-split related with YRPW motif protein 1 Human genes 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
- 125000006222 dimethylaminomethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])* 0.000 abstract 1
- VUWZPRWSIVNGKG-UHFFFAOYSA-N fluoromethane Chemical compound F[CH2] VUWZPRWSIVNGKG-UHFFFAOYSA-N 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical compound O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 125000006533 methyl amino methyl group Chemical group [H]N(C([H])([H])[H])C([H])([H])* 0.000 abstract 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000003566 oxetanyl group Chemical group 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biophysics (AREA)
- General Health & Medical Sciences (AREA)
- Genetics & Genomics (AREA)
- Medicinal Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Biochemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Indole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
La memoria descriptiva se refiere en general a compuestos de fórmula (1), y sales y profármacos farmacéuticamente aceptables de los mismos, donde R¹, R⁴, R⁵, R⁶, R⁷, el Enlazador, X, Y, A, G, D y E tienen cualquiera de los significados definidos en el presente documento. Esta memoria descriptiva también se refiere al uso de dichos compuestos y sales y solvatos farmacéuticamente aceptables de los mismos en métodos para el tratamiento del cuerpo humano o animal, por ejemplo, en la prevención o tratamiento del cáncer. Esta memoria descriptiva también se refiere a procesos y compuestos intermedios implicados en la preparación de dichos compuestos y a composiciones farmacéuticas que los contienen. Reivindicación 1: Un compuesto de fórmula (1), o una sal o profármaco farmacéuticamente aceptable del mismo, en donde: R¹ representa H o metilo; A y G son independientemente CR² o N; R² se selecciona independientemente de H, F, Cl, CN, metilo o metoxi; D y E son independientemente CR³ o N; R³ se selecciona independientemente de H, F, Cl, o metilo; R⁴ representa H, metilo o F; R⁵ representa H, metilo o F; o R⁴ y R⁵ tomados junto con el átomo de carbono al que están unidos forman un anillo de ciclopropilo o un anillo de oxetanilo; R⁶ representa H, metilo, F, CH₂F, CHF₂, CF₃, CN, CH₂CN, CH₂OMe, CH₂OH, C(O)OH, C(O)OMe o SO₂Me; R⁷ representa H, metilo, -CH₂NHMe, -CH₂NMe₂ o CH₂NH₂; X representa -O-, -CH=CH-C(O)NH-, -NHC(O)-, -C(O)NH- o -pirrolidinil-NMeC(O)-; Y representa un enlace o -C(O)-; el Enlazador es un resto de unión opcionalmente sustituido que comprende una cadena ramificada o no ramificada, ciclada o no ciclada, saturada o insaturada de 4 a 20 átomos de carbono de longitud, en donde 1 a 6 de los átomos de carbono se reemplazan opcionalmente con un heteroátomo seleccionado independientemente de O, N y S.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762608847P | 2017-12-21 | 2017-12-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR114168A1 true AR114168A1 (es) | 2020-07-29 |
Family
ID=65276230
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP180103831A AR114168A1 (es) | 2017-12-21 | 2018-12-21 | Compuestos y su uso en el tratamiento del cáncer |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US10519152B2 (es) |
| EP (1) | EP3727355A1 (es) |
| JP (1) | JP2021507888A (es) |
| CN (1) | CN111491623A (es) |
| AR (1) | AR114168A1 (es) |
| CA (1) | CA3085264A1 (es) |
| TW (1) | TW201938556A (es) |
| WO (1) | WO2019123367A1 (es) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019222272A1 (en) | 2018-05-14 | 2019-11-21 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
| JP7515175B2 (ja) | 2018-07-31 | 2024-07-12 | ファイメクス株式会社 | 複素環化合物 |
| CA3138197A1 (en) | 2019-05-14 | 2020-11-19 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
| EP4058464A1 (en) | 2019-11-13 | 2022-09-21 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
| AU2021205326A1 (en) * | 2020-01-10 | 2022-07-21 | Amgen Inc. | SMARCA2-VHL degraders |
| US20230099727A1 (en) * | 2020-01-13 | 2023-03-30 | January Therapeutics, Inc. | Nanoparticle compositions |
| US20230312639A1 (en) | 2020-04-23 | 2023-10-05 | University Of Iowa Research Foundation | Gper proteolytic targeting chimeras |
| US11839659B2 (en) | 2020-07-02 | 2023-12-12 | Northwestern University | Proteolysis-targeting chimeric molecules (PROTACs) that induce degradation of indoleamine 2,3-dioxygenase (IDO) protein |
| CN116744920A (zh) * | 2021-02-08 | 2023-09-12 | 贝达药业股份有限公司 | 杂芳基并哌啶类衍生物及其药物组合物和应用 |
| US11981678B2 (en) | 2021-04-29 | 2024-05-14 | Northwestern University | Substituted [1,2,4]triazolo[4,3-c]pyrimidin-5-amines and proteolysis-targeting chimeric derivatives thereof (PROTACs) that induce degradation of embryonic ectoderm development (EED) protein |
| US12042543B2 (en) | 2021-04-30 | 2024-07-23 | Northwestern University | Substituted 3-amino-5-phenylbenzamide compounds as covalent inhibitors of enhancer zeste homolog 2 (EZH2) and proteolysis-targeting chimeric derivatives thereof (PROTACs) that induce degradation of EZH2 |
| IL308104A (en) | 2021-05-03 | 2023-12-01 | Nuvation Bio Inc | Nuclear hormone receptor-targeted compounds against cancer |
| WO2023013757A1 (ja) * | 2021-08-05 | 2023-02-09 | 積水メディカル株式会社 | アルキルシリルオキシ置換ベンジル化合物の製造方法 |
| CN115991672A (zh) * | 2022-12-30 | 2023-04-21 | 苏州美诺医药科技有限公司 | 一种4-羟基吡啶-2-甲酸甲酯的制备方法 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2008239598A1 (en) * | 2007-04-13 | 2008-10-23 | Ptc Therapeutics, Inc. | Administration of carboline derivatives useful in the treatment of cancer and other diseases |
| GB201311910D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel Compounds |
| CA2911859A1 (en) | 2013-05-28 | 2014-12-04 | Astrazeneca Ab | Chemical compounds |
| GB201311891D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| GB201311888D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| US10071164B2 (en) | 2014-08-11 | 2018-09-11 | Yale University | Estrogen-related receptor alpha based protac compounds and associated methods of use |
| CN112375077A (zh) | 2014-12-18 | 2021-02-19 | 豪夫迈·罗氏有限公司 | 四氢-吡啶并[3,4-b]吲哚雌激素受体调节剂及其用途 |
| GB201504314D0 (en) | 2015-03-13 | 2015-04-29 | Univ Dundee | Small molecules |
| EP3270917A4 (en) | 2015-03-18 | 2018-08-08 | Arvinas, Inc. | Compounds and methods for the enhanced degradation of targeted proteins |
| CN106317052B (zh) | 2015-06-24 | 2019-02-22 | 首都医科大学 | 咔啉酰-Orn(ClCH2NH)-AA-苄胺，其合成，活性和应用 |
| WO2017030814A1 (en) | 2015-08-19 | 2017-02-23 | Arvinas, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
-
2018
- 2018-12-18 US US16/223,224 patent/US10519152B2/en not_active Expired - Fee Related
- 2018-12-19 TW TW107145976A patent/TW201938556A/zh unknown
- 2018-12-20 EP EP18842738.9A patent/EP3727355A1/en not_active Withdrawn
- 2018-12-20 CN CN201880081630.2A patent/CN111491623A/zh active Pending
- 2018-12-20 WO PCT/IB2018/060425 patent/WO2019123367A1/en not_active Ceased
- 2018-12-20 JP JP2020533224A patent/JP2021507888A/ja active Pending
- 2018-12-20 CA CA3085264A patent/CA3085264A1/en not_active Abandoned
- 2018-12-21 AR ARP180103831A patent/AR114168A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US10519152B2 (en) | 2019-12-31 |
| CN111491623A (zh) | 2020-08-04 |
| CA3085264A1 (en) | 2019-06-27 |
| EP3727355A1 (en) | 2020-10-28 |
| US20190194190A1 (en) | 2019-06-27 |
| JP2021507888A (ja) | 2021-02-25 |
| TW201938556A (zh) | 2019-10-01 |
| WO2019123367A1 (en) | 2019-06-27 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |