AR086839A1 - Derivados de piridin-2-ona con actividad inhibitoria de ezh2 - Google Patents
Derivados de piridin-2-ona con actividad inhibitoria de ezh2Info
- Publication number
- AR086839A1 AR086839A1 ARP120101289A ARP120101289A AR086839A1 AR 086839 A1 AR086839 A1 AR 086839A1 AR P120101289 A ARP120101289 A AR P120101289A AR P120101289 A ARP120101289 A AR P120101289A AR 086839 A1 AR086839 A1 AR 086839A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- halo
- cyano
- cycloalkyl
- amino
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/62—Oxygen or sulfur atoms
- C07D213/63—One oxygen atom
- C07D213/64—One oxygen atom attached in position 2 or 6
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
-
- 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
- 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
- C07D401/12—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 chain containing hetero atoms as chain links
-
- 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
- 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
- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D407/02—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 two hetero rings
- C07D407/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D413/12—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 chain containing hetero atoms as chain links
-
- 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
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/113—Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyridine Compounds (AREA)
- Peptides Or Proteins (AREA)
Abstract
Derivados de 2-piridona, una composición farmacéutica que los comprende y su uso en el tratamiento del cáncer.Reivindicación 1: Un compuesto de la fórmula (1) o una de sus sales farmacéuticamente aceptables, en donde X1 es N o CR11; X2 es N o CR13; X3 es N o C y cuando X3 es N, R6 está ausente; Z es NR7R8, OR7, S(O)aR7 o CR7R8R14, en donde a es 0, 1 ó 2; cada uno de R1, R5, R9 y R10, de modo independiente, es H o alquilo C1-6 opcionalmente sustituido con uno o varios sustituyentes seleccionados del grupo que consiste en halo, hidroxilo, COOH, C(O)O-alquilo C1-6, ciano, alcoxilo C1-6, amino, mono-alquil C1-6-amino, di-alquil C1-6-amino, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros y heteroarilo de 5 ó 6 miembros; cada uno de R2, R3 y R4, de modo independiente, es -Q1-T1, en donde Q1 es un enlace o ligador de alquilo C1-3 opcionalmente sustituido con halo, ciano, hidroxilo o alcoxi C1-6 y T1 es H, halo, hidroxilo, COOH, ciano, azido o RS1, en donde RS1 es alquilo C1-3, alquenilo C2-6, alquinilo C2-6, alcoxilo C1-6, C(O)O-alquilo C1-6, cicloalquilo C3-8, arilo C6-10, amino, mono-alquil C1-6-amino, di-alquil C1-6-amino, heterocicloalquilo de 4 a 12 miembros o heteroarilo de 5 ó 6 miembros y RS1 está opcionalmente sustituido con uno o varios sustituyentes seleccionados del grupo que consiste en halo, hidroxilo, oxo, COOH, C(O)O-alquilo C1-6, ciano, alcoxilo C1-6, amino, mono-alquil C1-6-amino, di-alquil C1-6-amino, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros y heteroarilo de 5 ó 6 miembros; R6 es H, halo, ciano, azido, ORa, -NRaRb, -C(O)Ra, -C(O)ORa, -C(O)NRaRb, -NRbC(O)Ra, -S(O)bRa, -S(O)bNRaRb o RS2, en donde RS2 es alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8 o heterocicloalquilo de 4 a 12 miembros, b es 0, 1 ó 2, cada uno de Ra y Rb, de modo independiente es H o RS3 y RS3 es alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros o heteroarilo de 5 ó 6 miembros; o Ra y Rb, junto con el átomo de N al que están unidos, forman un anillo heterocicloalquilo de 4 a 12 miembros que tiene 0 ó 1 heteroátomos adicionales; y cada uno de RS2, RS3 y el anillo heterocicloalquilo de 4 a 12 miembros formado por Ra y Rb, está opcionalmente sustituido con uno o varios -Q2-T2, en donde Q2 es un enlace o ligador de alquilo C1-3 cada uno opcionalmente sustituido con halo, ciano, hidroxilo o alcoxi C1-6 y T2 es H, halo, ciano, -ORc, -NRcRd, -C(O)Rc, -C(O)ORc, -C(O)NRcRd, -NRdC(O)Rc, NRdC(O)ORc, -S(O)2Rc, -S(O)2NRcRd o RS4, en donde cada uno de Rc y Rd, de modo independiente es H o RS5, cada uno de RS4 y RS5, de modo independiente, es alquilo C1-6, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros o heteroarilo de 5 ó 6 miembros o Rc y Rd, junto con el átomo de N al que están unidos, forman un anillo heterocicloalquilo de 4 a 12 miembros que tiene 0 ó 1 heteroátomos adicionales y cada uno de RS4, RS5 y el anillo heterocicloalquilo de 4 a 12 miembros formado por Rc y Rd, está opcionalmente sustituido con uno o varios -Q3-T3, en donde Q3 es un enlace o ligador de alquilo C1-3 cada uno opcionalmente sustituido con halo, ciano, hidroxilo o alcoxi C1-6 y T3 está seleccionado del grupo que consiste en halo, ciano, alquilo C1-6, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros, heteroarilo de 5 ó 6 miembros, ORe, COORe, -S(O)2Re, -NReRf y -C(O)NReRf, siendo cada uno de Re y Rf de modo independiente H o alquilo C1-6 o -Q3-T3 es oxo; o -Q2-T2 es oxo; R7 es -Q4-T4, en donde Q4 es un enlace, ligador de alquilo C1-4 o ligador de alquenilo C2-4, cada ligador opcionalmente sustituido con halo, ciano, hidroxilo o alcoxi C1-6 y T4 es H, halo, ciano, NRgRh, -ORg, -C(O)Rg, -C(O)ORg, -C(O)NRgRh, -C(O)NRgORh, -NRgC(O)Rh, S(O)2Rg o RS6, en donde cada uno de Rg y Rh, de modo independiente es H o RS7, cada uno de RS6 y RS7, de modo independiente es alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 14 miembros o heteroarilo de 5 ó 6 miembros y cada uno de RS6 y RS7 está opcionalmente sustituido con uno o varios -Q5-T5, en donde Q5 es un enlace, C(O), C(O)NRk, NRkC(O), S(O)2 o ligador de alquilo C1-3, siendo Rk H o alquilo C1-6 y T5 es H, halo, alquilo C1-6, hidroxilo, ciano, alcoxilo C1-6, amino, mono-alquil C1-6-amino, di-alquil C1-6-amino, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros, heteroarilo de 5 ó 6 miembros o S(O)qRq, en donde q es 0, 1 ó 2 y Rq es alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros o heteroarilo de 5 ó 6 miembros y T5 está opcionalmente sustituido con uno o varios sustituyentes seleccionados del grupo que consiste en halo, alquilo C1-6, hidroxilo, ciano, alcoxilo C1-6, amino, mono-alquil C1-6-amino, di-alquil C1-6-amino, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros y heteroarilo de 5 ó 6 miembros excepto cuando T5 es H, halo, hidroxilo o ciano; o -Q5-T5 es oxo; cada uno de R8, R11, R12 y R13, de modo independiente, es H, halo, hidroxilo, COOH, ciano, RS8, ORS8 o COORS8, en donde RS8 es alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, heterocicloalquilo de 4 a 12 miembros, amino, mono-alquil C1-6-amino o di-alquil C1-6-amino y RS8 está opcionalmente sustituido con uno o varios sustituyentes seleccionados del grupo que consiste en halo, hidroxilo, COOH, C(O)O-alquilo C1-6, ciano, alcoxilo C1-6, amino, mono-alquil C1-6-amino y di-alquil C1-6-amino; o R7 y R8, junto con el átomo de N al que están unidos, forman un anillo heterocicloalquilo de 4 a 12 miembros que tiene 0 a 2 heteroátomos adicionales o R7 y R8, junto con el átomo de C al que están unidos, forman cicloalquilo C3-8 o un anillo heterocicloalquilo de 4 a 12 miembros que tiene 1 a 3 heteroátomos y cada uno del anillo heterocicloalquilo de 4 a 12 miembros o cicloalquilo C3-8 formado R7 y R8 está opcionalmente sustituido con uno o varios -Q6-T6, en donde Q6 es un enlace, C(O), C(O)NRm, NRmC(O), S(O)2 o ligador de alquilo C1-3, siendo Rm H o alquilo C1-6 y T6 es H, halo, alquilo C1-6, hidroxilo, ciano, alcoxilo C1-6, amino, mono-alquil C1-6-amino, di-alquil C1-6- amino, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros, heteroarilo de 5 ó 6 miembros o S(O)pRp, en donde p es 0, 1 ó 2 y Rp es alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros o heteroarilo de 5 ó 6 miembros y T6 está opcionalmente sustituido con uno o varios sustituyentes seleccionados del grupo que consiste en halo, alquilo C1-6, hidroxilo, ciano, alcoxilo C1-6, amino, mono-alquil C1-6-amino, di-alquil C1-6-amino, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros y heteroarilo de 5 ó 6 miembros excepto cuando T6 es H, halo, hidroxilo o ciano; o -Q6-T6 es oxo; y R14 está ausente, H o alquilo C1-6 opcionalmente sustituido con uno o varios sustituyentes seleccionados del grupo que consiste en halo, hidroxilo, COOH, C(O)O-alquilo C1-6, ciano, alcoxilo C1-6, amino, mono-alquil C1-6-amino, di-alquil C1-6-amino, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros y heteroarilo de 5 ó 6 miembros; siempre que el compuesto no sea N-(5-(((4,6-dimetil-2-oxo-1,2-dihidropiridin-3-il)metil)carbamoil)-2-metilfenil)furan-2-carboxamida, N,N’-(5-(((4,6-dimetil-2-oxo-1,2-dihidropiridin-3-il)metil)carbamoil)-1,3-fenilen)diacetamida, N-((4,6-dimetil-2-oxo-1,2-dihidropiridin-3-il)metil)-3-pivalamidobenzamida, 3-(3,4-dihidro-2H-benzo[b][1,4]dioxepin-7-sulfonamido)-N-((4,6-dimetil-2-oxo-1,2-dihidropiridin-3-il)metil)benzamida, N-((4,6-dimetil-2-oxo-1,2-dihidropiridin-3-il)metil)-3,5-dimetoxibenzamida, N-((4,6-dimetil-2-oxo-1,2-dihidropiridin-3-il)metil)-3,4,5-trimetoxibenzamida, 3-alil-N-((4,6-dimetil-2-oxo-1,2-dihidropiridin-3-il)metil)-4,5-dimetoxibenzamida, 4-(2-amino-2-oxoetoxi)-3-cloro-N-((4,6-dimetil-2-oxo-1,2-dihidropiridin-3-il)metil)-5-metoxibenzamida, 3-cloro-N-((4,6-dimetil-2-oxo-1,2-dihidropiridin-3-il)metil)-4-hidroxi-5-metoxibenzamida, o 3-bromo-N-((4,6-dimetil-2-oxo-1,2-dihidropiridin-3-il)metil)-5-metoxi-4-propoxibenzamida.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161474825P | 2011-04-13 | 2011-04-13 | |
| US201161505676P | 2011-07-08 | 2011-07-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR086839A1 true AR086839A1 (es) | 2014-01-29 |
Family
ID=46000399
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120101289A AR086839A1 (es) | 2011-04-13 | 2012-04-13 | Derivados de piridin-2-ona con actividad inhibitoria de ezh2 |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US9376422B2 (es) |
| EP (3) | EP3470396A1 (es) |
| JP (1) | JP2014513084A (es) |
| KR (1) | KR101975613B1 (es) |
| CN (1) | CN104066718B (es) |
| AR (1) | AR086839A1 (es) |
| AU (2) | AU2012242604B2 (es) |
| BR (1) | BR112013026308B1 (es) |
| CA (1) | CA2832846C (es) |
| DK (1) | DK2697198T3 (es) |
| ES (1) | ES2590489T3 (es) |
| HK (1) | HK1202534A1 (es) |
| HU (1) | HUE030722T2 (es) |
| IL (1) | IL228746B (es) |
| MX (1) | MX344530B (es) |
| PL (1) | PL2697198T3 (es) |
| PT (1) | PT2697198T (es) |
| RU (2) | RU2017126990A (es) |
| TW (2) | TW201733984A (es) |
| WO (1) | WO2012142513A1 (es) |
Families Citing this family (85)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20130102477A1 (en) | 2010-06-23 | 2013-04-25 | Ryan D. Morin | Biomarkers for non-hodgkin lymphomas and uses thereof |
| BR112013005806B1 (pt) | 2010-09-10 | 2022-05-10 | Epizyme, Inc | Métodos para detectar se um indivíduo é um candidato para o tratamento com ou responsivo a um inibidor de ezh2 e usos terapêuticos do dito inibidor de ezh2 |
| US9175331B2 (en) | 2010-09-10 | 2015-11-03 | Epizyme, Inc. | Inhibitors of human EZH2, and methods of use thereof |
| JO3438B1 (ar) | 2011-04-13 | 2019-10-20 | Epizyme Inc | مركبات بنزين مستبدلة بأريل أو أريل غير متجانس |
| WO2013075084A1 (en) * | 2011-11-18 | 2013-05-23 | Constellation Pharmaceuticals | Modulators of methyl modifying enzymes, compositions and uses thereof |
| CA2862289C (en) | 2012-02-10 | 2019-11-26 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| IL308807B2 (en) | 2012-04-13 | 2025-08-01 | Epizyme Inc | Combination therapy for treating cancer |
| PL2836491T3 (pl) | 2012-04-13 | 2017-08-31 | Epizyme, Inc. | Postać soli inhibitora ludzkiej metylotransferazy histonowej EZH2 |
| US9562041B2 (en) | 2012-05-16 | 2017-02-07 | Glaxosmithkline Llc | Enhancer of zeste homolog 2 inhibitors |
| CA2884848C (en) * | 2012-09-28 | 2017-08-22 | Pfizer Inc. | Benzamide and heterobenzamide compounds |
| IL308613A (en) * | 2012-10-15 | 2024-01-01 | Epizyme Inc | Cancer treatment methods |
| US9006242B2 (en) | 2012-10-15 | 2015-04-14 | Epizyme, Inc. | Substituted benzene compounds |
| TWI494424B (zh) * | 2012-11-20 | 2015-08-01 | Dow Global Technologies Llc | 可蒸餾燃料標記物 |
| RU2015127822A (ru) * | 2012-12-13 | 2017-01-16 | ГЛЭКСОСМИТКЛАЙН ЭлЭлСи | Ингибиторы энхансера гомолога 2 белка zeste |
| EP2935264B1 (en) | 2012-12-21 | 2017-10-18 | Epizyme, Inc. | 1,4-pyridone bicyclic heteroaryl compounds |
| UA111305C2 (uk) * | 2012-12-21 | 2016-04-11 | Пфайзер Інк. | Конденсовані лактами арилу та гетероарилу |
| EP2935214B1 (en) | 2012-12-21 | 2019-02-20 | Epizyme, Inc. | 1,4-pyridone compounds |
| BR112015022785A2 (pt) | 2013-03-14 | 2017-07-18 | Epizyme Inc | composto; composição farmacêutica; kit ou artigo farmacêutico embalado; método de inibição de uma arginina metil transferase (rmt); método de modulação da expressão genética; método de modulação da transcrição; e método de tratamento de um distúrbio mediado por rmt |
| EP2970220A2 (en) | 2013-03-14 | 2016-01-20 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| US9447079B2 (en) | 2013-03-14 | 2016-09-20 | Epizyme, Inc. | PRMT1 inhibitors and uses thereof |
| US9023883B2 (en) | 2013-03-14 | 2015-05-05 | Epizyme, Inc. | PRMT1 inhibitors and uses thereof |
| US9120757B2 (en) | 2013-03-14 | 2015-09-01 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| CA2903264A1 (en) | 2013-03-14 | 2014-11-06 | Epizyme, Inc. | Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof |
| WO2014153208A1 (en) | 2013-03-14 | 2014-09-25 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| US9133189B2 (en) | 2013-03-14 | 2015-09-15 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| US9365527B2 (en) | 2013-03-14 | 2016-06-14 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| US20160039767A1 (en) | 2013-03-14 | 2016-02-11 | Epizyme, Inc. | Pyrazole derivatives as prmt1 inhibitors and uses thereof |
| WO2014144326A1 (en) | 2013-03-15 | 2014-09-18 | G1 Therapeutics, Inc. | Transient protection of normal cells during chemotherapy |
| US9745305B2 (en) | 2013-03-15 | 2017-08-29 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| EP2970281A4 (en) * | 2013-03-15 | 2016-08-03 | Epizyme Inc | SUBSTITUTED BENZOL COMPOUNDS |
| EA030196B1 (ru) * | 2013-04-30 | 2018-07-31 | Глэксосмитклайн Интеллекчуал Проперти (No.2) Лимитед | Ингибиторы энхансера zeste гомолога 2 |
| US9556157B2 (en) | 2013-07-10 | 2017-01-31 | Glaxosmithkline Intellectual Property (No.2) Limited | Enhancer of zeste homolog 2 inhibitors |
| US9624205B2 (en) | 2013-07-19 | 2017-04-18 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| US10150764B2 (en) | 2013-07-19 | 2018-12-11 | Epizyme, Inc. | Substituted benzene compounds |
| EP3033334A1 (en) | 2013-08-15 | 2016-06-22 | Constellation Pharmaceuticals, Inc. | Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof |
| EA038869B1 (ru) | 2013-10-16 | 2021-10-29 | Эпизим, Инк. | Кристаллические формы гидрохлорида n-((4,6-диметил-2-оксо-1,2-дигидропиридин-3-ил)метил)-5-(этил(тетрагидро-2h-пиран-4-ил)амино)-4-метил-4'-(морфолинометил)-[1,1'-бифенил]-3-карбоксамида, фармацевтические композиции на их основе и способы их применения |
| US9738630B2 (en) | 2013-11-19 | 2017-08-22 | Bristol-Myers Squibb Company | Inhibitors of lysine methyl transferase |
| WO2015077194A1 (en) * | 2013-11-22 | 2015-05-28 | Bristol-Myers Squibb Company | Inhibitors of lysine methyl transferase |
| CN116019921A (zh) | 2013-12-06 | 2023-04-28 | Epizyme股份有限公司 | 用于治疗癌症的组合疗法 |
| LT3157527T (lt) | 2014-06-17 | 2023-07-25 | Epizyme, Inc. | Ezh2 inhibitoriai, skirti limfomos gydymui |
| GEAP201814347A (en) * | 2014-06-17 | 2018-08-10 | Pfizer | Substituted dihydroisoquinoline compounds |
| WO2015200650A1 (en) | 2014-06-25 | 2015-12-30 | Epizyme, Inc. | Substituted benzene and 6,5-fused bicyclic heteroaryl compounds |
| CA2963149A1 (en) | 2014-10-16 | 2016-04-21 | Epizyme, Inc. | Method for treating cancer |
| CA2965729A1 (en) * | 2014-10-28 | 2016-05-06 | Glaxosmithkline Intellectual Property (No.2) Limited | Enhancer of zeste homolog 2 inhibitors |
| MX383484B (es) | 2014-11-17 | 2025-03-11 | Epizyme Inc | Método para tratar el cáncer. |
| AR102767A1 (es) | 2014-12-05 | 2017-03-22 | Lilly Co Eli | Inhibidores de ezh2 |
| US20180271857A1 (en) | 2014-12-23 | 2018-09-27 | University Of Copenhagen | Treatment of cancer by inhibiting ezh2 activity |
| SG10201902664RA (en) | 2015-04-20 | 2019-04-29 | Epizyme Inc | Combination therapy for treating cancer |
| US20180133211A1 (en) * | 2015-05-19 | 2018-05-17 | Mayo Foundation For Medical Education And Research | Methods and materials for promoting bone formation |
| MX387885B (es) | 2015-06-10 | 2025-03-19 | Epizyme Inc | Inhibidores de ezh2 para tratar linfomas. |
| WO2017035234A1 (en) | 2015-08-24 | 2017-03-02 | Epizyme, Inc. | Method for treating cancer |
| TW201718598A (zh) | 2015-08-27 | 2017-06-01 | 美國禮來大藥廠 | Ezh2抑制劑 |
| WO2017040190A1 (en) | 2015-08-28 | 2017-03-09 | Constellation Pharmaceuticals, Inc. | Crystalline forms of (r)-n-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1h-indole-3-carboxamide |
| EP3378859B1 (en) | 2015-11-19 | 2019-10-30 | Jiangsu Hengrui Medicine Co., Ltd. | Benzofuran derivative, preparation method thereof and use thereof in medicine |
| TWI773657B (zh) | 2015-12-18 | 2022-08-11 | 美商亞德利克斯公司 | 作爲非全身tgr5促效劑之經取代之4-苯基吡啶化合物 |
| US12084472B2 (en) | 2015-12-18 | 2024-09-10 | Ardelyx, Inc. | Substituted 4-phenyl pyridine compounds as non-systemic TGR5 agonists |
| JP2019503391A (ja) | 2016-01-29 | 2019-02-07 | エピザイム,インコーポレイティド | 癌を処置するための併用療法 |
| CN109311859B (zh) * | 2016-04-14 | 2022-01-21 | 广州嘉越医药科技有限公司 | 用于治疗纤维化和炎性疾病的含杂原子环丁烷取代基的吡啶酮衍生物 |
| WO2017210395A1 (en) | 2016-06-01 | 2017-12-07 | Epizyme, Inc. | Use of ezh2 inhibitors for treating cancer |
| EP3471830A4 (en) | 2016-06-17 | 2020-02-26 | Epizyme Inc | EZH2 INHIBITORS TO TREAT CANCER |
| US10457640B2 (en) | 2016-10-19 | 2019-10-29 | Constellation Pharmaceuticals, Inc. | Synthesis of inhibitors of EZH2 |
| CN108314677B (zh) | 2017-01-17 | 2020-06-30 | 安徽中科拓苒药物科学研究有限公司 | 一种ezh2抑制剂及其用途 |
| US11214561B2 (en) | 2017-01-25 | 2022-01-04 | Ancureall Pharmaceutical (Shanghai) Co., Ltd. | Histone methyltransferase EZH2 inhibitor, preparation method and pharmaceutical use thereof |
| US11395821B2 (en) | 2017-01-30 | 2022-07-26 | G1 Therapeutics, Inc. | Treatment of EGFR-driven cancer with fewer side effects |
| US10266542B2 (en) | 2017-03-15 | 2019-04-23 | Mirati Therapeutics, Inc. | EZH2 inhibitors |
| WO2018183885A1 (en) | 2017-03-31 | 2018-10-04 | Epizyme, Inc. | Combination therapy for treating cancer |
| EP3612181A4 (en) * | 2017-04-21 | 2021-01-06 | Epizyme, Inc. | Combination therapies with ehmt2 inhibitors |
| TWI772424B (zh) | 2017-05-18 | 2022-08-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | 一種苯并呋喃類衍生物游離鹼的晶型及製備方法 |
| US11602529B2 (en) | 2017-06-02 | 2023-03-14 | Epizyme, Inc. | Use of EZH2 inhibitors for treating cancer |
| CN111093660A (zh) | 2017-09-05 | 2020-05-01 | Epizyme股份有限公司 | 用于治疗癌症的组合疗法 |
| AU2018363467B2 (en) | 2017-11-10 | 2023-09-07 | Jiangsu Hengrui Medicine Co., Ltd. | Method for preparing benzofuran derivative |
| JP7201400B2 (ja) | 2017-11-14 | 2023-01-10 | ファイザー・インク | Ezh2阻害剤組合せ療法 |
| BR112020015583B1 (pt) | 2018-01-31 | 2022-12-06 | Mirati Therapeutics, Inc | Composto, composição farmacêutica e seu uso para tratar câncer |
| EP3823671B1 (en) | 2018-07-09 | 2024-02-07 | Fondation Asile Des Aveugles | Inhibition of prc2 subunits to treat eye disorders |
| CA3106589A1 (en) | 2018-07-27 | 2020-01-30 | Suzhou Sinovent Pharma Co., Ltd. | Polysubstituted benzene compound and preparation method and use thereof |
| MX2021007536A (es) | 2018-12-21 | 2021-09-23 | Les Laboratoires Servier Sas | Formas de sal y cristalinas de un compuesto organico y composiciones farmaceuticas del mismo. |
| US12473298B2 (en) | 2019-03-25 | 2025-11-18 | Shanghai Synergy Pharmaceutical Sciences Co., Ltd. | Amide compounds, preparation method therefor, and use thereof in the medical field |
| WO2020219448A1 (en) | 2019-04-22 | 2020-10-29 | Mirati Therapeutics, Inc. | Naphthyridine derivatives as prc2 inhibitors |
| EP3980422A1 (en) | 2019-06-05 | 2022-04-13 | Mirati Therapeutics, Inc. | Imidazo[1,2-c]pyrimidine derivatives as prc2 inhibitors for treating cancer |
| GB201908453D0 (en) * | 2019-06-12 | 2019-07-24 | Enterprise Therapeutics Ltd | Compounds for treating respiratory disease |
| JP2022545467A (ja) | 2019-08-22 | 2022-10-27 | ジュノー セラピューティクス インコーポレイテッド | T細胞療法とzesteホモログ2エンハンサー(EZH2)阻害剤との併用療法および関連方法 |
| CN113248481B (zh) * | 2021-04-19 | 2023-03-24 | 中山大学 | Ezh2共价不可逆抑制剂、制备方法及其用途 |
| CN113292489B (zh) * | 2021-06-16 | 2022-08-30 | 泓博智源(开原)药业有限公司 | 二氯代二烷基烟腈的制备方法 |
| AU2023292893A1 (en) | 2022-06-13 | 2025-01-02 | Treeline Biosciences, Inc. | Quinolone bcl6 bifunctional degraders |
| IL317217A (en) | 2022-06-13 | 2025-01-01 | Treeline Biosciences Inc | BCL6 heterobifunctional 8,1-naphthyridin-2-one joints |
Family Cites Families (57)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4522811A (en) | 1982-07-08 | 1985-06-11 | Syntex (U.S.A.) Inc. | Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides |
| JPH0733729A (ja) | 1993-07-26 | 1995-02-03 | Kirin Brewery Co Ltd | N−シアノ−n′−置換−アリールカルボキシイミダミド化合物の製造法 |
| RU2128644C1 (ru) | 1993-12-27 | 1999-04-10 | Эйсай Ко., Лтд. | Производные антраниловой кислоты или их фармакологически приемлемые соли, промежуточные продукты для их получения и лекарственный препарат на их основе |
| DE19516776A1 (de) | 1995-05-10 | 1996-11-14 | Boehringer Ingelheim Int | Chromatin-Regulatorgene |
| US5741819A (en) | 1995-06-07 | 1998-04-21 | 3-Dimensional Pharmaceuticals, Inc. | Arylsulfonylaminobenzene derivatives and the use thereof as factor Xa inhibitors |
| US5763263A (en) | 1995-11-27 | 1998-06-09 | Dehlinger; Peter J. | Method and apparatus for producing position addressable combinatorial libraries |
| JP3906935B2 (ja) | 1995-12-18 | 2007-04-18 | 杏林製薬株式会社 | N−置換ジオキソチアゾリジルベンズアミド誘導体及びその製造法 |
| BR9914207A (pt) | 1998-09-30 | 2001-07-03 | Procter & Gamble | Ceto-amidas 2-substituìdas |
| UA71587C2 (uk) | 1998-11-10 | 2004-12-15 | Шерінг Акцієнгезелльшафт | Аміди антранілової кислоти та їхнє застосування як лікарських засобів |
| US6710058B2 (en) | 2000-11-06 | 2004-03-23 | Bristol-Myers Squibb Pharma Company | Monocyclic or bicyclic carbocycles and heterocycles as factor Xa inhibitors |
| DK1357111T3 (da) | 2000-12-28 | 2009-11-02 | Shionogi & Co | 2-pyridonderivater med affinitet for cannabinoid type 2-receptor |
| US7700293B2 (en) | 2001-08-02 | 2010-04-20 | The Regents Of The University Of Michigan | Expression profile of prostate cancer |
| US20050101590A1 (en) | 2002-02-19 | 2005-05-12 | Kiyoshi Yasui | Antipruritics |
| TW200306155A (en) | 2002-03-19 | 2003-11-16 | Du Pont | Benzamides and advantageous compositions thereof for use as fungicides |
| US7442685B2 (en) | 2003-06-13 | 2008-10-28 | The University Of North Carolina At Chapel Hill | DOT1 histone methyltransferases as a target for identifying therapeutic agents for leukemia |
| TWI324926B (en) * | 2004-04-23 | 2010-05-21 | Bristol Myers Squibb Co | Monocyclic heterocycles as kinase inhibitors |
| WO2005118796A2 (en) | 2004-06-01 | 2005-12-15 | The University Of North Carolina At Chapel Hill | Reconstituted histone methyltransferase complex and methods of identifying modulators thereof |
| JO2787B1 (en) | 2005-04-27 | 2014-03-15 | امجين إنك, | Alternative amide derivatives and methods of use |
| US7923219B2 (en) | 2005-06-02 | 2011-04-12 | The University Of North Carolina At Chapel Hill | Ubiquitin E3 ligase |
| FR2889526B1 (fr) | 2005-08-04 | 2012-02-17 | Aventis Pharma Sa | 7-aza-indazoles substitues, compositions les contenant, procede de fabrication et utilisation |
| EP1940821B1 (de) | 2005-10-19 | 2013-03-20 | Grünenthal GmbH | Neue vanilloid-rezeptor liganden und ihre verwendung zur herstellung von arzneimitteln |
| WO2007050347A1 (en) | 2005-10-21 | 2007-05-03 | Merck & Co., Inc. | Potassium channel inhibitors |
| EP1941060B1 (en) | 2005-10-28 | 2012-02-29 | The University of North Carolina At Chapel Hill | Protein demethylases comprising a jmjc domain |
| WO2007070818A1 (en) | 2005-12-14 | 2007-06-21 | Bristol-Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| WO2007087015A1 (en) | 2006-01-20 | 2007-08-02 | The University Of North Carolina At Chapel Hill | Diagnostic and therapeutic targets for leukemia |
| CN101443007A (zh) | 2006-05-15 | 2009-05-27 | Irm责任有限公司 | Terephthalamate化合物和组合物及其作为hiv整合酶抑制剂的用途 |
| CA2652634A1 (en) * | 2006-05-18 | 2007-11-29 | Amphora Discovery Corporation | Certain substituted quinolones, compositions, and uses thereof |
| EP2086318A4 (en) | 2006-10-10 | 2009-12-23 | Burnham Inst Medical Research | NEUROPROTECTIVE COMPOSITIONS AND CORRESPONDING METHODS |
| MX2009008531A (es) | 2007-02-16 | 2009-08-26 | Amgen Inc | Cetonas de heterociclilo que contienen nitrogeno y su uso como inhibidores de c-met. |
| US8338437B2 (en) | 2007-02-28 | 2012-12-25 | Methylgene Inc. | Amines as small molecule inhibitors |
| WO2008113006A1 (en) * | 2007-03-14 | 2008-09-18 | Xenon Pharmaceuticals Inc. | Methods of using quinolinone compounds in treating sodium channel-mediated diseases or conditions |
| DE102007017884A1 (de) | 2007-04-13 | 2008-10-16 | Grünethal GmbH | Neue Vanilloid-Rezeptor Liganden und ihre Verwendung zur Herstellung von Arzneimitteln |
| US20090012031A1 (en) | 2007-07-03 | 2009-01-08 | The Regents Of The University Of Michigan | EZH2 Cancer Markers |
| US8247401B2 (en) | 2007-10-31 | 2012-08-21 | Merck Sharp & Dohme Corp. | P2X3 receptor antagonists for treatment of pain |
| NZ586418A (en) | 2007-12-19 | 2012-09-28 | Cancer Rec Tech Ltd | Pyrido[2,3-b]pyrazine-8-substituted compounds and their use |
| KR101608096B1 (ko) | 2008-01-23 | 2016-03-31 | 브리스톨-마이어스 스큅 컴퍼니 | 4-피리디논 화합물 및 암을 위한 그의 용도 |
| WO2009124137A2 (en) | 2008-04-01 | 2009-10-08 | Mount Sinai School Of Medicine Of New York University | Method of suppressing gene transcription through histone lysine methylation |
| US20100113415A1 (en) | 2008-05-29 | 2010-05-06 | Rajapakse Hemaka A | Epha4 rtk inhibitors for treatment of neurological and neurodegenerative disorders and cancer |
| WO2010017355A2 (en) * | 2008-08-08 | 2010-02-11 | New York Blood Center | Small molecule inhibitors of retroviral assembly and maturation |
| FR2934995B1 (fr) | 2008-08-14 | 2010-08-27 | Sanofi Aventis | Composes d'azetidines polysubstitues, leur preparation et leur application en therapeutique |
| CA2738583A1 (en) | 2008-10-01 | 2010-04-08 | Ludwig Institute For Cancer Research | Methods for the treatment of cancer |
| US20120065247A1 (en) | 2009-03-27 | 2012-03-15 | Discoverybiomed, Inc. | Modulating ires-mediated translation |
| US20110021362A1 (en) | 2009-07-20 | 2011-01-27 | Constellation Pharmaceuticals | Agents for stimulating activity of methyl modifying enzymes and methods of use thereof |
| US8329149B2 (en) | 2009-12-30 | 2012-12-11 | Avon Products, Inc. | Topical lightening composition and uses thereof |
| CN102970869B (zh) | 2010-05-07 | 2014-07-16 | 葛兰素史密斯克莱有限责任公司 | 吲哚 |
| JP5889875B2 (ja) | 2010-05-07 | 2016-03-22 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーGlaxoSmithKline LLC | アザインダゾール |
| EP2566328B1 (en) | 2010-05-07 | 2015-03-04 | GlaxoSmithKline LLC | Indazoles |
| BR112013005806B1 (pt) | 2010-09-10 | 2022-05-10 | Epizyme, Inc | Métodos para detectar se um indivíduo é um candidato para o tratamento com ou responsivo a um inibidor de ezh2 e usos terapêuticos do dito inibidor de ezh2 |
| US9175331B2 (en) | 2010-09-10 | 2015-11-03 | Epizyme, Inc. | Inhibitors of human EZH2, and methods of use thereof |
| WO2012068589A2 (en) | 2010-11-19 | 2012-05-24 | Constellation Pharmaceuticals | Modulators of methyl modifying enzymes, compositions and uses thereof |
| WO2012075080A1 (en) | 2010-12-01 | 2012-06-07 | Glaxosmithkline Llc | Indoles |
| EP2646454B1 (en) | 2010-12-03 | 2015-07-08 | Epizyme, Inc. | 7-deazapurine modulators of histone methyltransferase, and methods of use thereof |
| WO2012118812A2 (en) | 2011-02-28 | 2012-09-07 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| JO3438B1 (ar) * | 2011-04-13 | 2019-10-20 | Epizyme Inc | مركبات بنزين مستبدلة بأريل أو أريل غير متجانس |
| WO2013003635A1 (en) | 2011-06-28 | 2013-01-03 | Stoplift, Inc. | Image processing to prevent access to private information |
| US9562041B2 (en) | 2012-05-16 | 2017-02-07 | Glaxosmithkline Llc | Enhancer of zeste homolog 2 inhibitors |
| US9006242B2 (en) | 2012-10-15 | 2015-04-14 | Epizyme, Inc. | Substituted benzene compounds |
-
2012
- 2012-04-12 TW TW106103833A patent/TW201733984A/zh unknown
- 2012-04-12 TW TW101112996A patent/TWI598336B/zh active
- 2012-04-13 KR KR1020137029686A patent/KR101975613B1/ko active Active
- 2012-04-13 RU RU2017126990A patent/RU2017126990A/ru not_active Application Discontinuation
- 2012-04-13 JP JP2014505375A patent/JP2014513084A/ja active Pending
- 2012-04-13 EP EP18189032.8A patent/EP3470396A1/en not_active Withdrawn
- 2012-04-13 ES ES12716968.8T patent/ES2590489T3/es active Active
- 2012-04-13 EP EP16173275.5A patent/EP3165520B1/en not_active Not-in-force
- 2012-04-13 CN CN201280029120.3A patent/CN104066718B/zh active Active
- 2012-04-13 CA CA2832846A patent/CA2832846C/en active Active
- 2012-04-13 EP EP12716968.8A patent/EP2697198B1/en active Active
- 2012-04-13 PL PL12716968.8T patent/PL2697198T3/pl unknown
- 2012-04-13 PT PT127169688T patent/PT2697198T/pt unknown
- 2012-04-13 AR ARP120101289A patent/AR086839A1/es unknown
- 2012-04-13 US US14/110,873 patent/US9376422B2/en active Active
- 2012-04-13 HU HUE12716968A patent/HUE030722T2/en unknown
- 2012-04-13 DK DK12716968.8T patent/DK2697198T3/en active
- 2012-04-13 MX MX2013011922A patent/MX344530B/es active IP Right Grant
- 2012-04-13 HK HK15103015.8A patent/HK1202534A1/xx unknown
- 2012-04-13 WO PCT/US2012/033662 patent/WO2012142513A1/en not_active Ceased
- 2012-04-13 AU AU2012242604A patent/AU2012242604B2/en not_active Ceased
- 2012-04-13 RU RU2013150510A patent/RU2629118C2/ru active
- 2012-04-13 BR BR112013026308-3A patent/BR112013026308B1/pt active IP Right Grant
-
2013
- 2013-10-06 IL IL228746A patent/IL228746B/en active IP Right Grant
-
2016
- 2016-05-23 US US15/162,453 patent/US20160332969A1/en not_active Abandoned
-
2017
- 2017-08-21 AU AU2017218920A patent/AU2017218920A1/en not_active Abandoned
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR086839A1 (es) | Derivados de piridin-2-ona con actividad inhibitoria de ezh2 | |
| AR086008A1 (es) | Compuestos de benceno sustituidos con arilo o heteroarilo | |
| AR126406A2 (es) | Compuestos de tetrazolinona y su uso | |
| AR087760A1 (es) | Heterociclilaminas como inhibidores de pi3k | |
| AR101175A1 (es) | Imidazopiridinas e imidazopirazinas como inhibidores de lsd1 | |
| AR094410A1 (es) | Compuestos terapéuticos | |
| AR101600A1 (es) | COMPUESTOS DE SPIRO[3H-INDOL-3,2-PIRROLIDIN]-2(1H)-ONA Y DERIVADOS COMO INHIBIDORES DE MDM2-p53 | |
| RU2014114466A (ru) | ИНДАЗОЛ-3-КАРБОКСАМИДЫ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ СИГНАЛЬНОГО ПУТИ WNT/β-КАТЕНИНА | |
| AR085283A1 (es) | Antagonistas de hepcidina a base de sulfonaminoquinolina | |
| AR092108A1 (es) | Piridazina 1,4 disustituida, analogos de la misma y metodos para tratar las enfermedades relacionadas con deficiencia del smn | |
| AR080057A1 (es) | Piridinas disustituidas como anticancerigenos | |
| AR076066A1 (es) | Inhibidores de la tirosina-quinasa de bruton | |
| AR083933A1 (es) | Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak | |
| JP2016522172A5 (es) | ||
| AR081653A1 (es) | Inhibidores del virus de la hepatitis c | |
| AR105845A1 (es) | Compuestos de heteroarilo bicíclicos fusionados como moduladores de la función irak4 | |
| AR094816A2 (es) | Compuestos antivirales | |
| AR089776A1 (es) | 5,8-dihidro-6h-pirazolo[3,4-h]quinazolinas como inhibidores de igf-1r/ir | |
| AR082850A1 (es) | Aminopirazoloquinazolinas | |
| PE20170127A1 (es) | Indazol-3-carboxamidas 5-sustituidas y preparacion y uso de las mismas | |
| AR081848A1 (es) | Inhibidores de la proteina ns5a del vhc | |
| AR051342A1 (es) | Derivados de purina, purinona, deazapurina y deazapurinona como inhibidores de la actividad de la protein quinasa; metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en la elaboracion de un medicamento para el tratamiento de enfermedades mediadas por la protein quina | |
| AR059338A1 (es) | N-fenilbenzotriazolilo como inhibidores de c-kit | |
| AR084706A1 (es) | Derivados sustituidos de imidazoquinolinas como inhibidores de quinasa y proceso para su preparacion | |
| ES2620668T3 (es) | Derivados de amidas y sulfonamidas amido espirocíclicas |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |