AR094174A1 - Lactamas fusionadas de arilo y heteroarilo - Google Patents
Lactamas fusionadas de arilo y heteroariloInfo
- Publication number
- AR094174A1 AR094174A1 ARP130104902A ARP130104902A AR094174A1 AR 094174 A1 AR094174 A1 AR 094174A1 AR P130104902 A ARP130104902 A AR P130104902A AR P130104902 A ARP130104902 A AR P130104902A AR 094174 A1 AR094174 A1 AR 094174A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkoxy
- cycloalkyl
- aryl
- membered heteroaryl
- Prior art date
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Classifications
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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
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
-
- 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
- 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
Abstract
Composiciones farmacéuticas que comprenden dichos compuestos y sales, y a la utilización de esos compuestos, sales y composiciones para el tratamiento de crecimiento celular anormal, que incluye cáncer. Reivindicación 1: Un compuesto de la fórmula (1), o una sal farmacéuticamente aceptable del mismo, en donde: U es N o CR³; V es N o CR⁴; R¹ es alquilo C₁₋₈, alcoxi C₁₋₈, halo, -OH, -CN o -NR⁷R⁸, en donde cada alquilo C₁₋₈ o alcoxi C₁₋₈ es sustituido de manera opcional por uno o más R²¹; R² es seleccionado a partir del grupo que consta de H, alquilo C₁₋₈, alcoxi C₁₋₈, -OR⁶, -NR⁷R⁸, -C(O)NR⁷R⁸, -SO₂NR⁷R⁸, -NR⁷SO₂R⁸, cicloalquilo C₃₋₈, heterociclilo de 3 - 12 miembros, arilo C₆₋₁₂ y heteroarilo de 5 - 12 miembros, en donde cada alquilo C₁₋₈ o alcoxi C₁₋₈ es sustituido de manera opcional por uno o más R²², y cada cicloalquilo C₃₋₈, heterociclilo de 3 - 12 miembros, arilo C₆₋₁₂ o heteroarilo de 5 - 12 miembros es sustituido de manera opcional por uno o más R³²; R³ es H, alquilo C₁₋₈, alcoxi C₁₋₈, halo, -OH, -CN o -NR⁷R⁸, en donde cada alquilo C₁₋₈ o alcoxi C₁₋₈ es sustituido de manera opcional por uno o más R²³; R⁴ es seleccionado a partir del grupo que consta de H, halo, alquilo C₁₋₈, cicloalquilo C₃₋₈, heterociclilo de 3 - 12 miembros, arilo C₆₋₁₂, heteroarilo de 5 - 12 miembros, -(alquilo C₁₋₄)Rᶻ, -ORˣ, -CN, -C(O)Rˣ, -CO₂Rˣ, -C(O)NRˣRʸ, -SRˣ, -SORˣ, -SO₂Rˣ, -SO₂NRˣRʸ, -NO₂, -NRˣRʸ, -NRˣC(O)Rʸ, -NRˣC(O)NRˣRʸ, -NRˣC(O)ORʸ, -NRˣSO₂Rʸ, -NRˣSO₂NRˣRʸ, -OC(O)Rˣ y -OC(O)NRˣRʸ; cada Rˣ y Rʸ es seleccionado de manera independiente a partir del grupo que consta de H, alquilo C₁₋₈, cicloalquilo C₃₋₈, heterociclilo de 3 - 12 miembros, arilo C₆₋₁₂ y heteroarilo de 5 - 12 miembros; o Rˣ y Rʸ se pueden tomar junto con el átomo de N al cual se unen para formar un anillo heterociclilo de 3 - 12 miembros o heteroarilo de 5 - 12 miembros, cada uno que contiene de manera opcional 1, 2 ó 3 heteroátomos adicionales seleccionados a partir de O, N y S; cada Rᶻ es seleccionado de manera independiente a partir del grupo que consta de cicloalquilo C₃₋₈, heterociclilo de 3 - 12 miembros, arilo C₆₋₁₂ y heteroarilo de 5 - 12 miembros; y en donde cada alquilo C₁₋₈ en R⁴, Rˣ o Rʸ y cada alquilo C₁₋₄ en (alquilo C₁₋₄)Rᶻ es sustituido de manera opcional por uno o más R²⁴, y cada cicloalquilo C₃₋₈, heterociclilo de 3 - 12 miembros, arilo C₃₋₁₂, o heteroarilo de 5 - 12 miembros en R⁴, Rˣ, Rʸ, Rᶻ, o Rˣ y Rʸ tomados en conjunto es sustituido de manera opcional por uno o más R³⁴; cada R⁵ es seleccionado de manera independiente a partir del grupo que consta de halo, -OH, =O, alquilo C₁₋₄, alcoxi C₁₋₄, -CN, -NR⁹R¹⁰ y -C(O)NR⁹R¹⁰, en donde cada alquilo C₁₋₄ o alcoxi C₁₋₄ es sustituido de manera opcional con 1 a 3 sustituyentes seleccionados de modo independiente a partir del grupo que consta de halo, -OH, alcoxi C₁₋₄, -CN, -NR⁹R¹⁰ y -C(O)NR⁹R¹⁰; R⁶ es -(CR¹¹R¹²)ₙ-R¹³; cada R⁷ y R⁸ es seleccionado de manera independiente a partir del grupo que consta de H, alquilo C₁₋₈, cicloalquilo C₃₋₈, heterociclilo de 3 - 12 miembros, arilo C₆₋₁₂, y heteroarilo de 5 - 12 miembros; o R⁷ y R⁸ se pueden tomar junto con el átomo de N al cual se unen para formar un heterociclilo de 3 - 12 miembros o heteroarilo de 5 - 12 miembros, cada uno que contiene de manera opcional 1, 2 ó 3 heteroátomos adicionales seleccionados a partir de O, N y S; en donde cada alquilo C₁₋₈ en R⁷ o R⁸ es sustituido de manera opcional por uno o más R²⁷, y cada cicloalquilo C₃₋₈, heterociclilo de 3 - 12 miembros, arilo C₆₋₁₂, o heteroarilo de 5 - 12 miembros en R⁷, R⁸, o R⁷ y R⁸ tomados en conjunto es sustituido de manera opcional por uno o más R³⁷; cada R⁹ y R¹⁰ es de manera independiente H o alquilo C₁₋₄; o R⁹ y R¹⁰ se pueden tomar junto con el átomo de N al cual se unen para formar un heterociclilo de 3 - 12 miembros o heteroarilo de 5 - 12 miembros, cada uno que contiene de manera opcional 1, 2 ó 3 heteroátomos adicionales seleccionados a partir de O, N y S; en donde cada alquilo C₁₋₄ en R⁹ o R¹⁰, y cada heterociclilo de 3 - 12 miembros o heteroarilo de 5 - 12 miembros en R⁹ y R¹⁰ tomados en conjunto es sustituido de manera opcional por 1 a 3 sustituyentes seleccionados de modo independiente a partir del grupo que consta de halo, -OH, =O, alquilo C₁₋₄, alcoxi C₁₋₄, -CN, -NH₂, -NH(alquilo C₁₋₄) y -N(alquilo C₁₋₄)₂; cada R¹¹ y R¹² es de manera independiente H, halo o alquilo C₁₋₄, en donde cada alquilo C₁₋₄ es sustituido de manera opcional por uno o más R²²; R¹³ es seleccionado a partir del grupo que consta de cicloalquilo C₃₋₈, heterociclilo de 3 - 12 miembros, arilo C₆₋₁₂, y heteroarilo de 5 - 12 miembros, en donde cada cicloalquilo C₃₋₈, heterociclilo de 3 - 12 miembros, arilo C₆₋₁₂ o heteroarilo de 5 - 12 miembros es sustituido de manera opcional por uno o más R³²; m es 0 a 4; n es 0 a 4; cada R²¹, R²², R²³ y R²⁴ es seleccionado de manera independiente a partir del grupo que consta de halo, alquilo C₁₋₈, CN, =O, -C(O)Rᵉ, -CO₂Rᵉ, -C(O)NRᵉRᶠ, -ORᵉ, -SRᵉ, -SORᵉ, -SO₂Rᵉ, -SO₂NRᵉRᶠ, -NO₂, -NRᵉRᶠ, -NRᵉC(O)Rᶠ, -NRᵉC(O)NRᵉRᶠ, -NRᵉC(O)ORᶠ, -NRᵉSO₂Rᶠ, -NRᵉSO₂NRᵉRᶠ, -OC(O)Rᵉ, -OC(O)NRᵉRᶠ, cicloalquilo C₃₋₈, heterociclilo de 3 - 12 miembros, arilo C₆₋₁₂ y heteroarilo de 5 - 12 miembros; cada Rᵉ y Rᶠ es seleccionado de manera independiente a partir del grupo que consta de H, alquilo C₁₋₈, cicloalquilo C₃₋₈, heterociclilo de 3 - 12 miembros, arilo C₆₋₁₂ y heteroarilo de 5 - 12 miembros; o Rᵉ y Rᶠ se pueden tomar junto con el átomo de N al cual se unen para formar un anillo heterociclilo de 3 - 12 miembros o heteroarilo de 5 - 12 miembros, cada uno que contiene de manera opcional 1, 2 ó 3 heteroátomos adicionales seleccionados a partir de O, N y S; en donde cada alquilo C₁₋₈, cicloalquilo C₃₋₈, heterociclilo de 3 - 12 miembros, arilo C₆₋₁₂ o heteroarilo de 5 - 12 miembros en R²⁴, Rᵉ, Rᶠ, o Rᵉ y Rᶠ tomados en conjunto es sustituido de manera opcional por 1 a 3 sustituyentes seleccionados de modo independiente a partir del grupo que consta de halo, -OH, =O, alquilo C₁₋₄, alcoxi C₁₋₄, haloalquilo C₁₋₆, hidroxialquilo C₁₋₆, alcoxi C₁₋₄-alquilo C₁₋₆, -CN, -NH₂, -NH(alquilo C₁₋₄) y -N(alquilo C₁₋₄)₂; cada R²⁷ es seleccionado de manera independiente a partir del grupo que consta de halo, -OH, alcoxi C₁₋₄, -CN, -NR⁹R¹⁰, cicloalquilo C₃₋₈, heterociclilo de 3 - 12 miembros, arilo C₆₋₁₂ y heteroarilo de 5 - 12 miembros, en donde cada alcoxi C₁₋₄, cicloalquilo C₃₋₈, heterociclilo de 3 - 12 miembros, arilo C₆₋₁₂ o heteroarilo de 5 - 12 miembros es sustituido de manera opcional por 1 a 3 sustituyentes seleccionados de modo independiente a partir del grupo que consta de halo, -OH, =O, alquilo C₁₋₄, alcoxi C₁₋₄, haloalquilo C₁₋₆, hidroxialquilo C₁₋₆, alcoxi C₁₋₄-alquilo C₁₋₆, -CN, - NH₂, -NH(alquilo C₁₋₄) y -N(alquilo C₁₋₄)₂; cada R³², R³⁴ y R³⁷ es seleccionado de manera independiente a partir del grupo que consta de halo, alquilo C₁₋₈, -CN, =O, -C(O)Rᶜ, -CO₂Rᶜ, -C(O)NRᶜRᵈ, -ORᶜ, -SRᶜ, -SORᶜ, -SO₂Rᶜ, -SO₂NRᶜRᵈ, -NO₂, -NRᶜRᵈ,
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261740596P | 2012-12-21 | 2012-12-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR094174A1 true AR094174A1 (es) | 2015-07-15 |
Family
ID=49917684
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130104902A AR094174A1 (es) | 2012-12-21 | 2013-12-19 | Lactamas fusionadas de arilo y heteroarilo |
Country Status (46)
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2013075084A1 (en) | 2011-11-18 | 2013-05-23 | Constellation Pharmaceuticals | Modulators of methyl modifying enzymes, compositions and uses thereof |
| NZ628762A (en) | 2012-02-10 | 2016-07-29 | Constellation Pharmaceuticals Inc | Modulators of methyl modifying enzymes, compositions and uses thereof |
| AR092742A1 (es) | 2012-10-02 | 2015-04-29 | Intermune Inc | Piridinonas antifibroticas |
| UA111305C2 (uk) * | 2012-12-21 | 2016-04-11 | Пфайзер Інк. | Конденсовані лактами арилу та гетероарилу |
| KR102532198B1 (ko) | 2012-12-21 | 2023-05-11 | 얀센 바이오파마, 인코퍼레이트. | 치환된 뉴클레오사이드, 뉴클레오타이드 및 그것의 유사체 |
| EP2970305B1 (en) | 2013-03-15 | 2017-02-22 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| US9969716B2 (en) | 2013-08-15 | 2018-05-15 | Constellation Pharmaceuticals, Inc. | Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof |
| GEP20186933B (en) * | 2014-06-17 | 2018-12-10 | Pfizer | Substituted dihydroisoquinoline compounds |
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| AR102767A1 (es) | 2014-12-05 | 2017-03-22 | Lilly Co Eli | Inhibidores de ezh2 |
| EP3236962A2 (en) | 2014-12-23 | 2017-11-01 | University of Copenhagen | Treatment of cancer by inhibiting ezh2 activity |
| PT3274343T (pt) * | 2015-03-27 | 2020-05-07 | Syngenta Participations Ag | Derivados heterobicíclicos microbicidas |
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