AR119657A1 - Compuestos de pirimidina y composiciones farmacéuticas para prevenir o tratar cánceres que incluyen los mismos - Google Patents
Compuestos de pirimidina y composiciones farmacéuticas para prevenir o tratar cánceres que incluyen los mismosInfo
- Publication number
- AR119657A1 AR119657A1 ARP190102087A ARP190102087A AR119657A1 AR 119657 A1 AR119657 A1 AR 119657A1 AR P190102087 A ARP190102087 A AR P190102087A AR P190102087 A ARP190102087 A AR P190102087A AR 119657 A1 AR119657 A1 AR 119657A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- alkyl
- haloalkyl
- halogen
- formula
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title abstract 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical class C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 15
- 229910052739 hydrogen Inorganic materials 0.000 abstract 11
- 239000001257 hydrogen Substances 0.000 abstract 11
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 abstract 8
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 abstract 7
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 abstract 7
- 229910052736 halogen Inorganic materials 0.000 abstract 7
- 150000002367 halogens Chemical class 0.000 abstract 7
- 150000002431 hydrogen Chemical group 0.000 abstract 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 7
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 6
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 5
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 4
- 125000003277 amino group Chemical group 0.000 abstract 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 4
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 abstract 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 abstract 2
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 1
- 229910003827 NRaRb Inorganic materials 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 150000001602 bicycloalkyls Chemical group 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000005392 carboxamide group Chemical group NC(=O)* 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000005182 hydroxyalkylcarbonyl group Chemical group 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- -1 pyrimidine compound Chemical class 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000003396 thiol group Chemical group [H]S* 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Se proporcionan un compuesto de pirimidina representado por la fórmula (1), un método para preparar el compuesto, y un uso farmacéutico del compuesto para la prevención o el tratamiento del cáncer. Reivindicación 1: Un compuesto seleccionado entre un compuesto representado por la fórmula (1) y un estereoisómero, tautómero, solvato o sal farmacéuticamente aceptable del mismo, en donde, en la fórmula (1), R¹ es hidrógeno, un halógeno, un grupo hidroxi, un grupo alcoxi C₁₋₄ o -NRᵃRᵇ, en donde Rᵃ y Rᵇ son cada uno independientemente hidrógeno o un grupo alquilo C₁₋₄; R² es hidrógeno, un halógeno, un grupo ciano, un grupo nitro, un grupo amino, un grupo carboxamida, un grupo formilo, un grupo haloalquilo C₁₋₄ o un grupo alquilo C₁₋₄; R³ es hidrógeno, un halógeno, un grupo hidroxi, un grupo haloalquilo C₁₋₄, un grupo alquilo C₁₋₄, un grupo alquenilo C₂₋₄ o un grupo alquinilo C₂₋₄; cada R⁴ es independientemente hidrógeno, un halógeno, un grupo hidroxi, un grupo ciano, un grupo nitro, un grupo amino, -S(=O)ₗ-Rᶜ, un grupo haloalquilo C₁₋₄, un grupo alcoxi C₁₋₄, un grupo hidroxialquilo C₁₋₄, un grupo alquilo C₁₋₄, un grupo alquenilo C₂₋₄, un grupo alquinilo C₂₋₄, -NRᵈRᵉ, CO₂Rᵉ o -CO-NRᵈRᵉ, en donde Rᶜ es un grupo alquilo C₁₋₄ o -NRᵈRᵉ, cada uno de Rᵈ y Rᵉ es independientemente hidrógeno o un grupo alquilo C₁₋₄, ₗ es un número entero de 0 a 2, y k es un número entero de 0 a 4; R⁵ y R⁶ son cada uno independientemente hidrógeno, un halógeno, un grupo hidroxi, un grupo nitro, un grupo amino, un grupo alcoxi C₁₋₄ o un grupo alquilo C₁₋₄; R⁷ es un grupo hidroxialquilo C₁₋₄, un grupo alquilo C₁₋₄, un grupo alquenilo C₂₋₄, un grupo alquinilo C₂₋₄, un grupo cicloalquilo C₃₋₇ o un grupo heterocicloalquilo C₃₋₉, en donde el grupo cicloalquilo C₃₋₇ o el heterocicloalquilo C₃₋₉ están sin sustituir o sustituidos con un halógeno, un grupo alquilo C₁₋₄ o un grupo haloalquilo C₁₋₄; y X es H u OH; en donde, cuando X es OH, el compuesto representado por la fórmula (1) incluye una estructura tautomérica representada por la fórmula (2), R³, R⁴ y k en la fórmula (2) son iguales a como se describen junto con la fórmula (1); Y es -(CH₂)ₘ-, -(CH₂)ₘ-O-(CH₂)ₙ-, -(CH₂)ₘ-CO-(CH₂)ₙ-, (CH₂)ₘ-NR⁸-(CH₂)ₙ- o -(CH₂)ₘ-SO₂-(CH₂)ₙ-, en donde R⁸ es hidrógeno o un grupo alquilo C₁₋₄, ₘ ʸ ₙ ₛₒₙ ᶜₐᵈₐ ᵘₙₒ ⁱₙᵈₑₚₑₙᵈⁱₑₙₜₑₘₑₙₜₑ ᵘₙ ₙúₘₑʳₒ ₑₙₜₑʳₒ ᵈₑ ₀ ₐ ₂; ʸ Z ₛₑ ʳₑₚʳₑₛₑₙₜₐ ₘₑᵈⁱₐₙₜₑ ₗₐ ᶠóʳₘᵘₗₐ ₍₃₎; ₑₙ ᵈₒₙᵈₑ, ₑₙ ₗₐ ᶠóʳₘᵘₗₐ ₍₃₎, Aₙⁱₗₗₒ A ₑₛ ᵘₙ ᵍʳᵘₚₒ ᶜⁱᶜₗₒₐₗqᵘⁱₗₒ C₃₋₁₀ o un grupo heterocicloalquilo C₂₋₁₁; R⁹ es un halógeno, un grupo hidroxi, un grupo ciano, un grupo nitro, un grupo amino, un grupo tiol, un grupo formilo, un grupo haloalquilo C₁₋₄, un grupo alcoxi C₁₋₄, un grupo hidroxialquilo C₁₋₄ lineal o ramificado, un grupo alquilo C₁₋₄ lineal o ramificado, un grupo alquenilo C₂₋₄, un grupo alquinilo C₂₋₄, un grupo cicloalquilo C₃₋₁₀, un grupo heterocicloalquilo C₂₋₉, un grupo hidroxiheterocicloalquilo C₂₋₉, un grupo hidroxialquilcarbonilo C₁₋₄ lineal o ramificado, -NR¹⁰R¹¹, -COR¹², -COOR¹² o -SO₂R¹³, q es un número entero de 0 a 5, en donde, cuando el Anillo A es piperazina o piperidina, q no es 0, y en donde dos o más R⁹ se conectan o condensan con el Anillo A para formar un grupo bicicloalquilo de 7 a 12 miembros, grupo heterobicicloalquilo, grupo espirocicloalquilo o grupo espiroheterocicloalquilo; R¹⁰ y R¹¹ son cada uno independientemente hidrógeno, un grupo hidroxialquilo C₁₋₄, un grupo haloalquilo C₁₋₄, un grupo alquilo C₁₋₄, un grupo alquenilo C₂₋₄ o un grupo alquinilo C₂₋₄; R¹² es hidrógeno, un grupo hidroxi, un grupo hidroxialquilo C₁₋₄, un grupo haloalquilo C₁₋₄, un grupo alquilo C₁₋₄, un grupo alquenilo C₂₋₄, un grupo alquinilo C₂₋₄, un grupo cicloalquilo C₃₋₁₀ o un grupo heterocicloalquilo C₂₋₉; R¹³ es hidroxi, un grupo haloalquilo C₁₋₄, un grupo alquilo C₁₋₄, un grupo alquenilo C₂₋₄, un grupo alquinilo C₂₋₄, un grupo cicloalquilo C₃₋₁₀, un grupo heterocicloalquilo C₂₋₉, grupo arilo o -NRᶠRᵍ, y cada uno de Rᶠ y Rᵍ es independientemente hidrógeno o un grupo alquilo C₁₋₄.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR1020180086768A KR101954370B1 (ko) | 2018-07-25 | 2018-07-25 | 피리미딘 화합물 및 이를 포함하는 암의 예방 또는 치료용 약학 조성물 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR119657A1 true AR119657A1 (es) | 2022-01-05 |
Family
ID=65760263
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP190102087A AR119657A1 (es) | 2018-07-25 | 2019-07-24 | Compuestos de pirimidina y composiciones farmacéuticas para prevenir o tratar cánceres que incluyen los mismos |
Country Status (17)
| Country | Link |
|---|---|
| US (2) | US11292786B2 (es) |
| EP (1) | EP3810601A4 (es) |
| JP (1) | JP6806931B2 (es) |
| KR (1) | KR101954370B1 (es) |
| CN (2) | CN116693506B (es) |
| AR (1) | AR119657A1 (es) |
| BR (1) | BR112021001122A2 (es) |
| CA (1) | CA3106961A1 (es) |
| CL (1) | CL2021000175A1 (es) |
| DO (1) | DOP2021000017A (es) |
| MX (1) | MX2021000941A (es) |
| PE (1) | PE20210373A1 (es) |
| PH (1) | PH12021550124A1 (es) |
| SG (1) | SG11202100076RA (es) |
| TW (1) | TWI839363B (es) |
| WO (1) | WO2020022600A1 (es) |
| ZA (1) | ZA202100485B (es) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101954370B1 (ko) | 2018-07-25 | 2019-03-05 | 한미약품 주식회사 | 피리미딘 화합물 및 이를 포함하는 암의 예방 또는 치료용 약학 조성물 |
| PH12021551985A1 (en) * | 2019-02-22 | 2022-08-22 | Hanmi Pharmaceutical Co Ltd | Pharmaceutical composition comprising flt3 inhibitor and hypomethylating agent for treating acute myeloid leukemia |
| KR20210002015A (ko) * | 2019-06-27 | 2021-01-06 | 한미약품 주식회사 | Flt3 저해제 및 화학치료제를 포함하는 급성 골수성 백혈병 치료용 약학적 조성물 |
| WO2021066443A1 (ko) * | 2019-09-30 | 2021-04-08 | 한미약품 주식회사 | Flt3 저해제 및 mdm2 저해제를 포함하는 급성 골수성 백혈병 치료용 약학적 조성물 |
| WO2022098083A1 (ko) * | 2020-11-05 | 2022-05-12 | 한미약품 주식회사 | Flt3 억제제를 포함하는 백혈병 치료용 약학적 조성물 |
| MX2023009954A (es) * | 2021-02-26 | 2023-11-09 | Tyra Biosciences Inc | Compuestos de aminopirimidina y métodos de uso de estos. |
| CN117136184A (zh) * | 2021-02-26 | 2023-11-28 | 泰拉生物科学公司 | 氨基嘧啶化合物及其使用方法 |
| WO2022216098A1 (ko) * | 2021-04-08 | 2022-10-13 | 주식회사 스탠다임 | 신규한 lrrk2 억제제 |
| WO2023027966A1 (en) | 2021-08-24 | 2023-03-02 | Biomea Fusion, Inc. | Pyrazine compounds as irreversible inhibitors of flt3 |
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2018
- 2018-07-25 KR KR1020180086768A patent/KR101954370B1/ko active Active
-
2019
- 2019-02-13 JP JP2019566602A patent/JP6806931B2/ja active Active
- 2019-02-13 MX MX2021000941A patent/MX2021000941A/es unknown
- 2019-02-13 PE PE2021000090A patent/PE20210373A1/es unknown
- 2019-02-13 CN CN202310204523.7A patent/CN116693506B/zh active Active
- 2019-02-13 WO PCT/KR2019/001737 patent/WO2020022600A1/en not_active Ceased
- 2019-02-13 CN CN201980049569.8A patent/CN112469715B/zh active Active
- 2019-02-13 EP EP19841611.7A patent/EP3810601A4/en active Pending
- 2019-02-13 CA CA3106961A patent/CA3106961A1/en active Pending
- 2019-02-13 BR BR112021001122-6A patent/BR112021001122A2/pt active Search and Examination
- 2019-02-13 SG SG11202100076RA patent/SG11202100076RA/en unknown
- 2019-07-09 TW TW108124118A patent/TWI839363B/zh active
- 2019-07-24 AR ARP190102087A patent/AR119657A1/es unknown
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2020
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2021
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2022
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Also Published As
| Publication number | Publication date |
|---|---|
| TWI839363B (zh) | 2024-04-21 |
| CN116693506B (zh) | 2024-11-26 |
| US12325698B2 (en) | 2025-06-10 |
| WO2020022600A1 (en) | 2020-01-30 |
| CN116693506A (zh) | 2023-09-05 |
| ZA202100485B (en) | 2023-11-29 |
| KR101954370B1 (ko) | 2019-03-05 |
| JP2020527128A (ja) | 2020-09-03 |
| US11292786B2 (en) | 2022-04-05 |
| SG11202100076RA (en) | 2021-02-25 |
| DOP2021000017A (es) | 2021-04-15 |
| BR112021001122A2 (pt) | 2021-04-13 |
| EP3810601A1 (en) | 2021-04-28 |
| US20200255410A1 (en) | 2020-08-13 |
| NZ772028A (en) | 2024-09-27 |
| JP6806931B2 (ja) | 2021-01-06 |
| EP3810601A4 (en) | 2022-04-20 |
| TW202014417A (zh) | 2020-04-16 |
| MX2021000941A (es) | 2021-03-09 |
| CN112469715B (zh) | 2024-06-11 |
| CA3106961A1 (en) | 2020-01-30 |
| PE20210373A1 (es) | 2021-02-26 |
| CN112469715A (zh) | 2021-03-09 |
| US20230002358A1 (en) | 2023-01-05 |
| PH12021550124A1 (en) | 2021-09-27 |
| CL2021000175A1 (es) | 2021-07-02 |
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