AR112803A2 - PIPERAZINE DERIVATIVES AS PYRUVATE KINASE M2 (PKM2) MODULATORS - Google Patents
PIPERAZINE DERIVATIVES AS PYRUVATE KINASE M2 (PKM2) MODULATORSInfo
- Publication number
- AR112803A2 AR112803A2 ARP180102600A ARP180102600A AR112803A2 AR 112803 A2 AR112803 A2 AR 112803A2 AR P180102600 A ARP180102600 A AR P180102600A AR P180102600 A ARP180102600 A AR P180102600A AR 112803 A2 AR112803 A2 AR 112803A2
- Authority
- AR
- Argentina
- Prior art keywords
- independently selected
- alkyl
- optionally substituted
- pkm2
- crcrc
- Prior art date
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La presente se refiere a compuestos y composiciones que comprenden compuestos que modulan a piruvato cinasa M2 (PKM2). También se describen métodos para usar los compuestos que modulan PKM2 en el tratamiento de cáncer. Reivindicación 1: Un compuesto de la fórmula (1), o una sal del mismo farmacéuticamente aceptable, caracterizado porque W, X, Y y Z son cada uno independientemente seleccionados a partir de CH o N; D y D¹ son independientemente seleccionados a partir de un enlace o NRᵇ; A es heteroarilo bicíclico opcionalmente sustituido; L es un enlace, -C(O)-, -(CRᶜRᶜ)ₘ-, -OC(O)-, -(CRᶜRᶜ)ₘ-OC(O)-, -(CRᶜRᶜ)ₘ-C(O)-, -NRᵇC(S)-, o -NRᵇC(O)-; R¹ se selecciona a partir de alquilo, cicloalquilo, arilo, heteroarilo, y heterociclilo; cada uno de los cuales es sustituido con 0 - 5 incidencias de Rᵈ; cada R³ se selecciona independientemente a partir de halo, haloalquilo, alquilo, hidroxilo y -ORᵃ o dos R³ adyacentes tomados junto con los átomos de carbono a los cuales están unidos, forman un ciclilo opcionalmente sustituido; cada Rᵃ se selecciona independientemente a partir de alquilo, acilo, hidroxialquilo y haloalquilo; cada Rᵇ se selecciona independientemente a partir de hidrógeno y alquilo; cada Rᶜ se selecciona independientemente a partir de hidrógeno, halo, alquilo, alcoxi y haloalcoxi o dos Rᶜ tomados junto con los átomos de carbono a los cuales están unidos, forman un cicloalquilo opcionalmente sustituido; cada Rᵈ se selecciona independientemente a partir de halo, haloalquilo, haloalcoxi, alquilo, alquinilo, nitro, ciano, hidroxilo, -C(O)Rᵃ, -OC(O)Rᵃ, -C(O)ORᵃ, -SRᵃ, -NRᵃRᵃ y -ORᵃ, o dos Rᵈ tomados junto con los átomos de carbono a los cuales están unidos, forman un heterociclilo opcionalmente sustituido; n es 0, 1, ó 2; m es 1, 2 ó 3; h es 0, 1, 2; y g es 0, 1 ó 2.This refers to compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2). Methods for using the compounds that modulate PKM2 in the treatment of cancer are also described. Claim 1: A compound of formula (1), or a pharmaceutically acceptable salt thereof, characterized in that W, X, Y and Z are each independently selected from CH or N; D and D¹ are independently selected from a bond or NRᵇ; A is optionally substituted bicyclic heteroaryl; L is a bond, -C (O) -, - (CRᶜRᶜ) ₘ-, -OC (O) -, - (CRᶜRᶜ) ₘ-OC (O) -, - (CRᶜRᶜ) ₘ-C (O) -, -NRᵇC (S) -, or -NRᵇC (O) -; R¹ is selected from alkyl, cycloalkyl, aryl, heteroaryl, and heterocyclyl; each of which is substituted with 0 - 5 occurrences of Rᵈ; Each R³ is independently selected from halo, haloalkyl, alkyl, hydroxyl, and -ORᵃ or two adjacent R³ taken together with the carbon atoms to which they are attached, form an optionally substituted cyclyl; each Rᵃ is independently selected from alkyl, acyl, hydroxyalkyl, and haloalkyl; each Rᵇ is independently selected from hydrogen and alkyl; each Rᶜ is independently selected from hydrogen, halo, alkyl, alkoxy, and haloalkoxy or two Rᶜ taken together with the carbon atoms to which they are attached, form an optionally substituted cycloalkyl; each Rᵈ is independently selected from halo, haloalkyl, haloalkoxy, alkyl, alkynyl, nitro, cyano, hydroxyl, -C (O) Rᵃ, -OC (O) Rᵃ, -C (O) ORᵃ, -SRᵃ, -NRᵃRᵃ and -ORᵃ, or two Rᵈ taken together with the carbon atoms to which they are attached, form an optionally substituted heterocyclyl; n is 0, 1, or 2; m is 1, 2, or 3; h is 0, 1, 2; and g is 0, 1, or 2.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US22143009P | 2009-06-29 | 2009-06-29 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR112803A2 true AR112803A2 (en) | 2019-12-11 |
Family
ID=69024790
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP180102600A AR112803A2 (en) | 2009-06-29 | 2018-09-13 | PIPERAZINE DERIVATIVES AS PYRUVATE KINASE M2 (PKM2) MODULATORS |
Country Status (1)
Country | Link |
---|---|
AR (1) | AR112803A2 (en) |
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2018
- 2018-09-13 AR ARP180102600A patent/AR112803A2/en unknown
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