AR111776A1 - Heteroarilos inhibidores de las proteínas ras mutantes de g12c - Google Patents
Heteroarilos inhibidores de las proteínas ras mutantes de g12cInfo
- Publication number
- AR111776A1 AR111776A1 ARP180101198A ARP180101198A AR111776A1 AR 111776 A1 AR111776 A1 AR 111776A1 AR P180101198 A ARP180101198 A AR P180101198A AR P180101198 A ARP180101198 A AR P180101198A AR 111776 A1 AR111776 A1 AR 111776A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- halo
- hydroxy
- heteroaryl
- alkoxy
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/14—Ortho-condensed systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Procesos e intermedios usados para su preparación, a composiciones farmacéuticas que los contienen y a su uso en el tratamiento de trastornos proliferativos celulares. Reivindicación 1: Un compuesto de fórmula (1), en donde: el Anillo A se selecciona de arilo, heteroarilo monocíclico y heteroarilo bicíclico; R¹ se selecciona independientemente de alquilo C₁₋₄, halo hidroxi, alcoxi C₁₋₄, fluoroalquilo C₁₋₃, fluoroalcoxi C₁₋₃, ciano, acetilenilo, NR⁷R⁸, C(O)NR⁹R¹⁰, CH₂R¹¹, N=S(O)Me₂, S(O)Me y SO₂R¹²; b es 0, 1, 2 ó 3; W es N o CR¹³; X es O ó NR¹⁴; Y es CR¹⁵R¹⁶, CR¹⁷R¹⁸CR¹⁹R²⁰, C=O, o C(O)CR²¹R²²; R² es H, ciano, halo, alquilo C₁₋₄, alcoxi C₁₋₄, fluoroalquilo C₁₋₃, NR²³R²⁴, acetilenilo o CH₂OR²⁵; R³ es H, fluoroalquilo C₁₋₃, OR²⁶, NR²⁷R²⁸, CH₂R²⁹, SR³⁰ o C(O)R³¹; R⁴ es H o Me; R⁵ es H o Me; R⁶ es H o CH₂NMe₂; R⁷ es H, alquilo C₁₋₄, C₍O₎ₐₗqᵘⁱₗₒ C₁₋₃ o CO₂-alquilo C₁₋₃; R¹¹ es hidroxi, ciano, heterociclilo, NR³²R³³, C(O)NR³⁴R³⁵ o SO₂-alquilo C₁₋₃; R¹² es alquilo C₁₋₃, fluoroalquilo C₁₋₃ o NR³⁶R³⁷; R¹³ es H, alquilo C₁₋₄, halo, fluoroalquilo C₁₋₃ o alcoxi C₁₋₄; R¹⁵, R¹⁶, R¹⁷ y R¹⁸ se seleccionan independientemente de H y alquilo C₁₋₃; R¹⁹, R²⁰, R²¹ y R²² se seleccionan independientemente de H, alquilo C₁₋₃, y flúor; R²⁶ se selecciona del grupo que consiste en: H; alquilo C₁₋₄ opcionalmente sustituido con 1 ó 2 sustituyentes seleccionados de hidroxi, alcoxi C₁₋₃, halo, NR³⁸R³⁹, C(O)NR⁴⁰R⁴¹, SO₂Me, heteroarilo, cicloalquilo C₃₋₇ o heterociclilo, en el que dicho heteroarilo o cicloalquilo C₃₋₇ está opcionalmente sustituido además con alquilo C₁₋₄, hidroxi, halo, ciano, o alcoxi C₁₋₄, y dicho heterociclilo está opcionalmente sustituido además con alquilo C₁₋₄, hidroxi, halo, C(O)Me, alcoxi C₁₋₃, fluoroalquilo C₁₋₃, cicloalquilo C₃₋₇, heterociclilo o heteroarilo; cicloalquilo C₃₋₇ opcionalmente sustituido con alquilo C₁₋₄, hidroxi o halo; heterociclilo opcionalmente sustituido con alquilo C₁₋₄, hidroxi, halo, C(O)Me, alcoxi C₁₋₃, fluoroalquilo C₁₋₃, cicloalquilo C₃₋₇, heterociclilo o heteroarilo; y heteroarilo opcionalmente sustituido con alquilo C₁₋₄, hidroxi, halo, ciano o alcoxi C₁₋₄; R²⁷ se selecciona del grupo que consiste en: H; C(O)R⁴²; alquilo C₁₋₄ opcionalmente sustituido con 1 ó 2 sustituyentes seleccionados de hidroxi, alcoxi C₁₋₃ halo, NR⁴³R⁴⁴, C(O)NR⁴⁵R⁴⁶, SO₂Me, heteroarilo, cicloalquilo C₃₋₇, o heterociclilo, en el que dicho heteroarilo o cicloalquilo C₃₋₇ está sustituido opcionalmente además con alquilo C₁₋₄, hidroxi, halo, ciano, o alcoxi C₁₋₄ y dicho heterociclilo está sustituido opcionalmente además con alquilo C₁₋₄, hidroxi, halo, C(O)Me, alcoxi C₁₋₃, fluoroalquilo C₁₋₃, cicloalquilo C₃₋₇, heterociclilo o heteroarilo; cicloalquilo C₃₋₇ opcionalmente sustituido con alquilo C₁₋₄, hidroxi o halo; heterociclilo opcionalmente sustituido con alquilo C₁₋₄, hidroxi, halo, C(O)Me, alcoxi C₁₋₃, fluoroalquilo C₁₋₃, cicloalquilo C₃₋₇, CH₂-ciclopropilo, heterociclilo o heteroarilo; y heteroarilo opcionalmente sustituido con alquilo C₁₋₄, hidroxi, halo, ciano o alcoxi C₁₋₄; R²⁸ es H o Me; o R²⁷ y R²⁸ tomados junto con el átomo de nitrógeno al que están unidos forman un anillo heterocíclico de 4, 5, 6 ó 7 miembros, en el que dicho anillo está opcionalmente sustituido con alquilo C₁₋₄, hidroxi, halo, C(O)Me, NR⁴⁷R⁴⁸, alcoxi C₁₋₃, fluoroalquilo C₁₋₃, cicloalquilo C₃₋₇, CH₂-ciclopropilo, heterociclilo o heteroarilo; R²⁹ se selecciona del grupo que consiste en: H; NR⁴⁹R⁵⁰; alquilo C₁₋₃ opcionalmente sustituido con 1 ó 2 sustituyentes seleccionados de hidroxi, alcoxi C₁₋₃, halo, NR⁵¹R⁵², C(O)NR⁵³R⁵⁴, SO₂Me, heteroarilo, cicloalquilo C₃₋₇ o heterociclilo, en el que dicho heteroarilo o cicloalquilo C₃₋₇ está sustituido opcionalmente además con alquilo C₁₋₄, hidroxi, halo, ciano, o alcoxi C₁₋₄ y dicho heterociclilo está sustituido opcionalmente además con alquilo C₁₋₄, hidroxi, halo, C(O)Me, alcoxi C₁₋₃, fluoroalquilo C₁₋₃, cicloalquilo C₃₋₇, heterociclilo o heteroarilo; cicloalquilo C₃₋₇ opcionalmente sustituido con alquilo C₁₋₄, hidroxi o halo; heterociclilo opcionalmente sustituido con alquilo C₁₋₄, hidroxi, halo, C(O)Me, alcoxi C₁₋₃, fluoroalquilo C₁₋₃, cicloalquilo C₃₋₇, CH₂-ciclopropilo, heterociclilo o heteroarilo; y heteroarilo opcionalmente sustituido con alquilo C₁₋₄, hidroxi, halo, ciano o alcoxi C₁₋₄; R³⁰ se selecciona del grupo que consiste en: alquilo C₁₋₄ opcionalmente sustituido con 1 ó 2 sustituyentes seleccionados de hidroxi, alcoxi C₁₋₃, halo, NR⁵⁵R⁵⁶, C(O)NR⁵⁷R⁵⁸, SO₂Me, heteroarilo, cicloalquilo C₃₋₇ o heterociclilo, en el que dicho heteroarilo o cicloalquilo C₃₋₇ está sustituido opcionalmente además con alquilo C₁₋₄, hidroxi, halo, ciano, o alcoxi C₁₋₄, y dicho heterociclilo está sustituido opcionalmente además con alquilo C₁₋₄, hidroxi, halo, C(O)Me, alcoxi C₁₋₃, fluoroalquilo C₁₋₃, cicloalquilo C₃₋₇, heterociclilo o heteroarilo; cicloalquilo C₃₋₇ opcionalmente sustituido con alquilo C₁₋₄, hidroxi o halo; heterociclilo opcionalmente sustituido con alquilo C₁₋₄, hidroxi, halo, C(O)Me, alcoxi C₁₋₃, fluoroalquilo C₁₋₃, cicloalquilo C₃₋₇, heterociclilo o heteroarilo; y heteroarilo opcionalmente sustituido con alquilo C₁₋₄, hidroxi, halo, ciano o alcoxi C₁₋₄; R³¹ es NR⁵⁹R⁶⁰; R⁴² es heteroarilo opcionalmente sustituido o alquilo C₁₋₄ opcionalmente sustituido; R⁴⁹ y R⁵¹ se seleccionan independientemente de H, alquilo C₁₋₄, heterociclilo y heteroarilo; R⁵⁹ y R⁶⁰ se seleccionan independientemente de H y alquilo C₁₋₄; o R⁵⁹ y R⁶⁰ tomados junto con el átomo de nitrógeno al que están unidos forman un anillo heterocíclico de 4, 5 ó 6 miembros, en el que dicho anillo está opcionalmente sustituido con alquilo C₁₋₄, hidroxi, halo o C(O)Me; R⁸, R⁹, R¹⁰, R¹⁴, R²³, R²⁴, R²⁵, R³², R³³, R³⁴, R³⁵, R³⁶, R³⁷, R³⁸, R³⁹, R⁴⁰, R⁴¹, R⁴³, R⁴⁴, R⁴⁵, R⁴⁶, R⁴⁷, R⁴⁸, R⁵⁰, R⁵², R⁵³, R⁵⁴, R⁵⁵, R⁵⁶, R⁵⁷ y R⁵⁸ se seleccionan independientemente de H y alquilo C₁₋₄; o una de sus sales farmacéuticamente aceptables.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762504638P | 2017-05-11 | 2017-05-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR111776A1 true AR111776A1 (es) | 2019-08-21 |
Family
ID=62492577
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP180101198A AR111776A1 (es) | 2017-05-11 | 2018-05-08 | Heteroarilos inhibidores de las proteínas ras mutantes de g12c |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US20200109153A1 (es) |
| EP (1) | EP3621968A1 (es) |
| JP (1) | JP2020519589A (es) |
| CN (1) | CN110603258A (es) |
| AR (1) | AR111776A1 (es) |
| CA (1) | CA3061650A1 (es) |
| TW (1) | TW201906848A (es) |
| WO (1) | WO2018206539A1 (es) |
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| JP4691041B2 (ja) * | 2003-11-20 | 2011-06-01 | チルドレンズ ホスピタル メディカル センター | Ｇｔｐアーゼ阻害剤および使用方法 |
| WO2011121350A1 (en) * | 2010-04-01 | 2011-10-06 | Astrazeneca Ab | 4 -amino -7,8- dihydropyrimido [5, 4 - f] [1, 4] oxazepin- 5 ( 6h) - one based dgat1 inhibitors |
| BR112015022483A2 (pt) * | 2013-03-14 | 2017-07-18 | Novartis Ag | 3-pirimidin-4-il-oxazolidin-2-onas como inibidores de idh mutante |
| US9862701B2 (en) * | 2014-09-25 | 2018-01-09 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| US10730867B2 (en) * | 2015-09-28 | 2020-08-04 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
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- 2018-05-08 CA CA3061650A patent/CA3061650A1/en not_active Abandoned
- 2018-05-08 JP JP2019561278A patent/JP2020519589A/ja not_active Withdrawn
- 2018-05-08 AR ARP180101198A patent/AR111776A1/es unknown
- 2018-05-08 TW TW107115513A patent/TW201906848A/zh unknown
- 2018-05-08 WO PCT/EP2018/061787 patent/WO2018206539A1/en unknown
- 2018-05-08 CN CN201880030263.3A patent/CN110603258A/zh active Pending
- 2018-05-08 US US16/611,538 patent/US20200109153A1/en not_active Abandoned
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2021
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| US20200109153A1 (en) | 2020-04-09 |
| WO2018206539A1 (en) | 2018-11-15 |
| TW201906848A (zh) | 2019-02-16 |
| CA3061650A1 (en) | 2018-11-15 |
| US20220127281A1 (en) | 2022-04-28 |
| JP2020519589A (ja) | 2020-07-02 |
| CN110603258A (zh) | 2019-12-20 |
| EP3621968A1 (en) | 2020-03-18 |
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