AR120855A1 - Derivados de pirazolilo útiles como agentes anticancerígenos - Google Patents
Derivados de pirazolilo útiles como agentes anticancerígenosInfo
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- AR120855A1 AR120855A1 ARP200103593A ARP200103593A AR120855A1 AR 120855 A1 AR120855 A1 AR 120855A1 AR P200103593 A ARP200103593 A AR P200103593A AR P200103593 A ARP200103593 A AR P200103593A AR 120855 A1 AR120855 A1 AR 120855A1
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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
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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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
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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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
- C07D403/02—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 two hetero rings
- C07D403/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
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- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Peptides Or Proteins (AREA)
Abstract
La presente proporciona un compuesto de fórmula (1) o un estereoisómero del mismo, o un atropisómero del mismo, o una sal farmacéuticamente aceptable del mismo, o una sal farmacéuticamente aceptable de un estereoisómero del mismo, o una sal farmacéuticamente aceptable de un atropisómero del mismo; un método para fabricar dicho compuesto y sus usos terapéuticos. La presente proporciona además una combinación de agentes farmacológicamente activos y una composición farmacéutica que comprende dicho compuesto. Reivindicación 1: Un compuesto de fórmula (1), en donde A se selecciona del grupo que consta de: (a) C₅₋₇-cicloalquileno que no está sustituido o está sustituido con uno o más, de modo preferente 1, 2 ó 3, sustituyentes seleccionados independientemente entre flúor y C₁₋₄-alquilo; (b) un heterociclilo insaturado de 5 - 7 miembros que contiene un doble enlace carbono-carbono y un átomo de oxígeno como miembro del anillo, en donde dicho heterociclilo no está sustituido o está sustituido con uno o más, de modo preferente 1, 2 ó 3, sustituyentes, seleccionados independientemente de flúor y C₁₋₄-alquilo, de modo preferente 1, 2 ó 3, C₁₋₄-alquilo; (c) arilo C₆₋₁₀ que no está sustituido o está sustituido con 1, 2 ó 3 RA²; (d) un anillo heteroarilo de 5 - 6 miembros que contiene 1, 2 ó 3 heteroátomos seleccionados independientemente entre N, O y S como miembros del anillo, en donde dicho anillo heteroarilo no está sustituido o está sustituido en uno o más (por ejemplo, 1, 2 ó 3) átomos de carbono con RA³, y en donde un átomo de nitrógeno, cuando está presente en el anillo heteroarilo, no está sustituido o está sustituido con un sustituyente seleccionado del grupo que consiste en: C₁₋₄-alquilo, -(CH₂)₁₋₂-C₃₋₄-cicloalquilo, C₃₋₆-cicloalquilo, hidroxi-C₁₋₄-alquilo, flúor-C₁₋₄-alquilo, C₁₋₄-alcoxi-C₁₋₄-alquilo, N(R⁹)(R¹⁰)-C₁₋₄-alquilo, -SO₂-C₁₋₄-alquilo, -SO₂-C₃₋₄-cicloalquilo, -(CH₂)ₚ-Hetᵖʸ, y -(CH₂)ₚ-N(R⁹)(R¹⁰); (e) un anillo heteroarilo de 8 - 10 miembros que contiene de 1 a 3 heteroátomos seleccionados independientemente entre nitrógeno, oxígeno y azufre, o un anillo heterobicíclico parcialmente saturado de 8 - 10 miembros que contiene de 1 a 3 heteroátomos o grupos de heteroátomos seleccionados independientemente de 0 - 3 átomos de nitrógeno, 0 - 2 átomos de oxígeno, 0 - 1 átomo de azufre y 0 - 1 grupo S(=O)₂ en el anillo heterobicíclico, en donde dicho anillo heteroarilo o anillo heterobicíclico no está sustituido o está sustituido en un átomo de carbono con 1, 2, 3, 4 ó 5 RA⁴, y en donde el anillo heteroarilo bicíclico está además opcionalmente sustituido en un átomo de carbono con oxo y en donde un átomo de nitrógeno, cuando está presente, está sin sustituir o sustituido con un sustituyente que es -(CO)-C₁₋₄-alquilo o C₁₋₄-alquilo, y en donde dicho C₁₋₄-alquilo está opcionalmente sustituido con 1 ó 2 sustituyentes seleccionados independientemente entre ciano, hidroxi, oxo, flúor, C₁₋₄-alcoxi, C₁₋₄-alcoxi-C₁₋₄-alquil-oxi, Hetᵇ y NR⁹R¹⁰; y en donde Hetᵇ es un anillo heterocíclico de 4 ó 5 ó 6 miembros que comprende 1 ó 2 heteroátomos o grupos seleccionados independientemente de N, O, S, SO y SO₂, en donde dicho anillo heterocíclico Hetᵇ no está sustituido o está sustituido en un átomo de carbono con uno o dos sustituyentes seleccionados independientemente de alquilo C₁₋₄, hidroxi, ciano, flúor, alcoxi C₁₋₄-hidroxi-alquilo C₁₋₄, hidroxi-alquilo C₁₋₄, alcoxi C₁₋₄, flúor-alcoxi C₁₋₄ y flúor-alquilo C₁₋₄, y donde dicho anillo heterocíclico Hetᵇ está además opcionalmente sustituido en un átomo de carbono con oxo, y donde el átomo de nitrógeno cuando está presente en Hetᵇ está opcionalmente sustituido adicionalmente con alquilo C₁₋₄ que está opcionalmente sustituido con 1 a 3 sustituyentes seleccionados independientemente de flúor, hidroxi y alcoxi C₁₋₄; en donde A está unido al resto del compuesto de fórmula (1) por un átomo de carbono en A que tiene hibridación sp²; en donde B se selecciona del grupo que consta de B¹ y B², en donde B¹ es arilo C₆₋₁₀ que no está sustituido o está sustituido con 1, 2, 3 ó 4 RBᵃ; B² es un heteroarilo de 6 - 13 miembros que comprende 1, 2 ó 3 átomos de nitrógeno, en donde B² no está sustituido o está sustituido con 1, 2, 3 ó 4 RBᵇ; C se selecciona del grupo que consiste en hidrógeno, alquilo C₁₋₃, cicloalquilo C₃₋₅, flúor-alquilo C₁₋₃, ciano, -CH₂-CN, -CH(CN)-CH₃, -CH₂-OH, -CH(OH)-CH₃ y halo; L se selecciona del grupo que consta de: los compuestos del grupo de fórmulas (2); en donde n es 1, 2 ó 3, RL se selecciona de hidrógeno, metilo, etilo, -CH₂-CN y -CH₂-OH, donde G* representa el punto de unión a G; G se selecciona del grupo que consta de los compuestos del grupo de fórmulas (3); en donde R² se selecciona de hidrógeno, alquilo C₁₋₃, -C(O)-alquilo C₁₋₃, y flúor; R³ es hidrógeno; R⁴ se selecciona de hidrógeno, metilo, -CH₂F, -CH₂-OCH₃ y -CH₂-N(CH₃)₂; R⁵ se selecciona de hidrógeno y metilo; R⁶ es hidrógeno; R⁷ se selecciona de hidrógeno y metilo; en donde RA² se selecciona independientemente del grupo que consiste en: NR⁹R¹⁰, ciano, -(CH₂)ₚ-CN, halo, OH, hidroxi-alquilo C₁₋₄, -(COOH), -(CH₂)ₚ-COOH, alquilo C₁₋₄, flúor-alquilo C₁₋₄, alcoxi C₁₋₄, alcoxi C₁₋₄-alquilo C₁₋₄, N(R⁹)(R¹⁰)-alquilo C₁₋₄, N(R⁹)(R¹⁰)-alquilo C₁₋₄-oxi, N(R⁹)(R¹⁰)-C₁₋₄-alcoxi, alquilo C₁₋₄-carbonil-oxi-alquilo C₁₋₄-oxi, hidroxi-alquilo C₁₋₄-oxi, alcoxi C₁₋₄-alquilo C₁₋₄-oxi, alcoxi C₁₋₄-alquilo C₁₋₄-oxi-alquilo C₁₋₄, -SO₂-alquilo C₁₋₄, -SO₂-cicloalquilo C₃₋₄, -(CH₂)₁₋₂-cicloalquilo C₃₋₄, Hetᵖʸ, -(CH₂)ₚ-Hetᵖʸ, -C(=O)-NR⁹R¹⁰, -(CH₂)ₚ-C(=O)NR⁹R¹⁰; en donde RA³ se selecciona independientemente del grupo que consiste en oxo, NR⁹R¹⁰, ciano, -(CH₂)ₚ-CN, halo, OH, hidroxi-alquilo C₁₋₄, -(COOH), -(CH₂)ₚ-COOH, alquilo C₁₋₄, flúor-alquilo C₁₋₄, alcoxi C₁₋₄, alcoxi C₁₋₄-alquilo C₁₋₄, N(R⁹)(R¹⁰)-alquilo C₁₋₄, N(R⁹)(R¹⁰)-alquilo C₁₋₄-oxi, N(R⁹)(R¹⁰)-alcoxi C₁₋₄, alquilo C₁₋₄-carbonil-oxi-alquilo C₁₋₄-oxi, hidroxi-alquilo C₁₋₄-oxi, alcoxi C₁₋₄-alquilo C₁₋₄-oxi, alcoxi C₁₋₄-alquilo C₁₋₄-oxi-alquilo C₁₋₄, -SO₂-alquilo C₁₋₄, -SO₂-cicloalquilo C₃₋₄, -(CH₂)₁₋₂-cicloalquilo C₃₋₄, Hetᵖʸ, -(CH₂)ₚ-Hetᵖʸ, -C(=O)-NR⁹R¹⁰, -(CH₂)ₚ-C(=O)NR⁹R¹⁰, (CH₂)ₚ-NR⁹R¹⁰; en donde RA⁴ se selecciona independientemente del grupo que consiste en ciano, CO₂H, halo, alquilo C₁₋₄, flúor-alquilo C₁₋₄, hidroxi, hidroxi-alquilo C₁₋₄, hidroxi-alquilo C₁₋₄-oxi, alcoxi C₁₋₄, alcoxi C₁₋₄-alquilo C₁₋₄, alcoxi C₁₋₄-alquilo C₁₋₄-oxi, NR⁹R¹⁰, N(R⁹)(R¹⁰)-alquilo C₁₋₄, N(R⁹)(R¹⁰)-alquilo C₁₋₄-oxi, -(CO)-alquilo C₁₋₄, y R⁹R¹⁰N-alquilo C₁₋₄-oxi-(CO)-alquilo C₁₋₄; en donde p es 1 ó 2 ó 3; R⁹ se selecciona de hidrógeno y alquilo C₁₋₄; R¹⁰ se selecciona del grupo que consiste en hidrógeno, alquilo C₁₋₄, hidroxi-alquilo C₁₋₄, alcoxi C₁₋₄-alquilo C₁₋₄ y di-alquilo C₁₋₄-amino-alquilo C₁₋₄; Hetᵖʸ es un anillo heterocíclico saturado de 4, 5, 6 ó 7 miembros que comprende uno o dos heteroátomos seleccionados independientemente de O, N y S, o que comprende un grupo S-óxido (SO) o S-dióxido (SO₂), y donde dicho anillo heterocíclico está opcionalmente sustituido con oxo en un átomo de carbono, y donde dicho anillo heterocíclico está opcionalmente sustituido adicionalmente en uno o más átomos de carbono con 1, 2 ó 3 sustituyentes seleccionados independientemente de alcoxi C₁₋₄, halo, alquilo C₁₋₄, hidroxi-alquilo C₁₋₄ y flúor-alquilo C₁₋₄, y donde el átomo de nitrógeno, si está presente en dicho heterociclo, está opcionalmente sustituido adicionalmente con R¹⁰; o Hetᵖʸ es un anillo heteroarilo de 5 ó 6 miembros, que comprende 1, 2 ó 3 átomos de nitrógeno y en donde dicho anillo heteroarilo está opcionalmente sustituido con uno o más (por ejemplo, 1, 2 ó 3) sustituyentes seleccionados independientemente de NR⁹R¹⁰, -C(=O)-NR⁹R¹⁰, halo, alquilo C₁₋₄, hidroxi-alquilo C₁₋₄, flúor-alquilo C₁₋₄, ciano, OH, y alcoxi C₁₋₄; cada RBᵃ se selecciona independientemente del grupo que consiste en hidroxi, NH₂, alquilo C₁₋₄ y halo; cada RBᵇ se selecciona independientemente del grupo que consiste en alquilo C₁₋₄, ciclopropilo, flúor-alquilo C₁₋₃, ciano, halo, NH₂ y alcoxi C₁₋₃, o un estereoisómero del mismo, o un atropisómero del mismo, o una sal farmacéuticamente aceptable del mismo, o una sal farmacéuticamente aceptable de un estereoisómero del mismo, o una sal farmacéuticamente aceptable de un atropisómero del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962951400P | 2019-12-20 | 2019-12-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR120855A1 true AR120855A1 (es) | 2022-03-23 |
Family
ID=76477081
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP200103593A AR120855A1 (es) | 2019-12-20 | 2020-12-21 | Derivados de pirazolilo útiles como agentes anticancerígenos |
Country Status (31)
| Country | Link |
|---|---|
| US (1) | US11702409B2 (es) |
| EP (2) | EP4076662B1 (es) |
| JP (3) | JP7726883B2 (es) |
| KR (1) | KR20220114064A (es) |
| AR (1) | AR120855A1 (es) |
| AU (1) | AU2020410531B2 (es) |
| CA (1) | CA3165148A1 (es) |
| CL (1) | CL2022001625A1 (es) |
| CO (1) | CO2022008344A2 (es) |
| CR (1) | CR20220281A (es) |
| DK (1) | DK4076662T3 (es) |
| DO (1) | DOP2022000124A (es) |
| EC (1) | ECSP22047876A (es) |
| ES (1) | ES2987196T3 (es) |
| FI (1) | FI4076662T3 (es) |
| HR (1) | HRP20240513T1 (es) |
| HU (1) | HUE066235T2 (es) |
| IL (1) | IL293893A (es) |
| JO (1) | JOP20220155A1 (es) |
| LT (1) | LT4076662T (es) |
| MA (1) | MA58004B1 (es) |
| MX (1) | MX2022007350A (es) |
| PE (1) | PE20221910A1 (es) |
| PH (1) | PH12022551454A1 (es) |
| PL (1) | PL4076662T3 (es) |
| PT (1) | PT4076662T (es) |
| RS (1) | RS65419B1 (es) |
| SI (1) | SI4076662T1 (es) |
| TW (1) | TW202136241A (es) |
| UY (1) | UY38990A (es) |
| WO (2) | WO2021120890A1 (es) |
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| TWI831855B (zh) | 2018-10-26 | 2024-02-11 | 日商大鵬藥品工業股份有限公司 | 新穎吲唑化合物或其鹽 |
| CA3158793A1 (en) | 2019-10-28 | 2021-05-06 | Merck Sharp & Dohme Corp. | Small molecule inhibitors of kras g12c mutant |
| WO2021106230A1 (ja) | 2019-11-29 | 2021-06-03 | 大鵬薬品工業株式会社 | 新規なフェノール化合物又はその塩 |
| US11685727B2 (en) | 2019-12-20 | 2023-06-27 | Nuevolution A/S | Compounds active towards nuclear receptors |
| AU2021285032A1 (en) | 2020-06-02 | 2022-12-08 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| UY39391A (es) * | 2020-08-24 | 2022-03-31 | Adama Makhteshim Ltd | Proceso para la preparación de pirazoles sustituidos |
| CA3187757A1 (en) | 2020-09-03 | 2022-03-24 | Ethan AHLER | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| US11690915B2 (en) | 2020-09-15 | 2023-07-04 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2022066805A1 (en) | 2020-09-23 | 2022-03-31 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| KR20230098252A (ko) * | 2020-10-30 | 2023-07-03 | 노파르티스 아게 | Kras g12c 억제제 화합물의 새로운 결정형 |
| WO2022133345A1 (en) | 2020-12-18 | 2022-06-23 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| AU2021408129A1 (en) * | 2020-12-22 | 2023-07-13 | Novartis Ag | Pharmaceutical combinations comprising a kras g12c inhibitor and uses of a kras g12c inhibitor for the treatment of cancers |
| WO2022133731A1 (en) * | 2020-12-22 | 2022-06-30 | Novartis Ag | Pharmaceutical combinations comprising a kras g12c inhibitor and uses of a kras g12c inhibitor and for the treatment of cancers |
| CN118561952A (zh) | 2021-05-05 | 2024-08-30 | 锐新医药公司 | Ras抑制剂 |
| CR20230558A (es) | 2021-05-05 | 2024-01-24 | Revolution Medicines Inc | Inhibidores de ras para el tratamiento del cáncer |
| EP4340883A1 (en) * | 2021-05-19 | 2024-03-27 | Genentech, Inc. | Combination therapy |
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