AR072937A1 - Derivados de piridina y pirimidina sustituida y su uso en el tratamiento de infecciones virales - Google Patents
Derivados de piridina y pirimidina sustituida y su uso en el tratamiento de infecciones viralesInfo
- Publication number
- AR072937A1 AR072937A1 ARP090103181A ARP090103181A AR072937A1 AR 072937 A1 AR072937 A1 AR 072937A1 AR P090103181 A ARP090103181 A AR P090103181A AR P090103181 A ARP090103181 A AR P090103181A AR 072937 A1 AR072937 A1 AR 072937A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkenyl
- aryl
- heteroaryl
- haloalkyl
- Prior art date
Links
- 208000036142 Viral infection Diseases 0.000 title abstract 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 24
- 125000003118 aryl group Chemical group 0.000 abstract 21
- 125000001424 substituent group Chemical group 0.000 abstract 16
- 125000005843 halogen group Chemical group 0.000 abstract 15
- 101100240516 Caenorhabditis elegans nhr-10 gene Proteins 0.000 abstract 14
- 125000000304 alkynyl group Chemical group 0.000 abstract 14
- 125000000217 alkyl group Chemical group 0.000 abstract 12
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 10
- -1 or an isomer Chemical class 0.000 abstract 10
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 9
- 125000001188 haloalkyl group Chemical group 0.000 abstract 8
- 125000004404 heteroalkyl group Chemical group 0.000 abstract 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 8
- 125000004366 heterocycloalkenyl group Chemical group 0.000 abstract 7
- 150000001875 compounds Chemical class 0.000 abstract 6
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 abstract 5
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000001374 aryl-fused-cycloalkyl group Chemical group 0.000 abstract 2
- 125000000461 aryl-fused-heterocycloalkyl group Chemical group 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 150000002148 esters Chemical class 0.000 abstract 2
- 125000000455 heteroaryl-fused-cycloalkyl group Chemical group 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- 125000003003 spiro group Chemical group 0.000 abstract 2
- 125000003107 substituted aryl group Chemical group 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 241000700605 Viruses Species 0.000 abstract 1
- 230000006806 disease prevention Effects 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000000643 heteroaryl-fused-heterocycloalkyl group Chemical group 0.000 abstract 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 1
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
- 230000009385 viral infection Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- 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
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- 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
-
- 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
- C07D405/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D409/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- 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
- C07D417/02—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 two hetero rings
- C07D417/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
-
- 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
Abstract
También se proveen composiciones farmacéuticas que contienen tales compuestos. Estos compuestos son eficaces como inhibidores del VHC, y son utiles, solos o juntos con agentes terapéuticos, para el tratamiento o prevencion de enfermedades o trastornos tales como infecciones virales y trastornos relacionados con el virus. Reivindicacion 1: Un compuesto, o un isomero, éster, o tautomero de dicho compuesto, o una sal, solvato, o prodroga aceptable para uso farmacéutico de dicho compuesto, isomero, éster, o tautomero, dicho compuesto tiene la estructura general que se muestra en la formula (1), donde cada uno de R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18 y R19 y n se seleccionan independientemente y donde R se selecciona de alquilo, arilo, heteroarilo, cicloalquilo, cicloalquilo arilo-fusionado, cicloalquilo heteroarilo-fusionado, cicloalquenilo, cicloalquenilo arilo-fusionado, heterocicloalquenilo arilo-fusionado, heterocicloalquilo, heterocicloalquilo arilo-fusionado, y heterocicloalquilo heteroarilo-fusionado, donde cada uno de dicho alquilo, dicho arilo, dicho heteroarilo, dicho cicloalquilo, dicho cicloalquilo arilo-fusionado, dicho cicloalquilo heteroarilo-fusionado, dicho cicloalquenilo, dicho cicloalquenilo arilo-fusionado, dicho heterocicloalquenilo arilo-fusionado, dicho heterocicloalquilo, dicho heterocicloalquilo arilo-fusionado, y dicho heterocicloalquilo heteroarilo-fusionado, es no sustituido u opcional e independientemente sustituido con desde uno a cinco sustituyentes, los cuales son iguales o diferentes, cada sustituyente se selecciona independientemente de halo, -OH, -CN, oxo, alquilo, cicloalquilo, alquenilo, alquinilo, haloalquilo, heteroalquilo, heterohaloalquilo, -alquil-OH, -O-alquilo, -O-haloalquilo, -O-alquil-OH, arilo, -O-arilo, -S-arilo, -O-alquil-arilo, -S-alquil-arilo, heteroarilo, heteroariloalquil-, -O-heteroarilo, -S-heteroarilo, -O-alquil-heteroarilo, -S-alquil-heteroarilo, heterocicloalquilo, heterocicloalquiloalquil-, -C(O)-alquilo, -C(O)-haloalquilo, -C(O)-cicloalquilo, -C(O)-heterocicloalquilo, -C(O)H, -C(O)OH, -C(O)O-alquilo, -C(O)O-haloalquilo, -C(O)O-cicloalquilo, -C(O)O-heterocicloalquilo, -OC(O)-alquilo, -OC(O)-haloalquilo, -OC(O)-cicloalquilo, -OC(O)-heterocicloalquilo, -C(O)NH2, -C(O)NHR10, -C(O)NR10R11, -OC(O)NH2, -CO(O)NHR10, -CO(O)NR10R11, -NH2, -NHR10, -NR10R11, -NO2, -S(O)NHR10, -S(O)NR10R11, -S(O)R10, -S(O)2NH2, -S(O)2NHR10, -S(O)2NR10R11, -S(O)2R10, arilo sustituido, y heteroarilo sustituido, donde cada uno de dicho arilo sustituido y dicho heteroarilo sustituido contiene independientemente desde uno a tres sustituyentes, los cuales pueden ser iguales o diferentes, cada sustituyente se selecciona independientemente de halo, alquilo, -O-alquilo, y -C(O)O-alquilo; X e Y se seleccionan cada uno de ellos independientemente de N y CH, con la condicion que al menos uno de X o Y es N; Z = H, halo, -OH, -SH, -CN, alquilo, alquenilo, alquinilo, heteroalquilo, haloalquilo, heterohaloalquilo, -S-alquilo, -O-alquilo, -O-arilo, -O-heteroalquilo, -O-heteroarilo, -SH, -S-alquilo, -S-arilo, -S-heteroalquilo, -cicloalquilo, arilo, heteroarilo, -NH2, -NHR12, y-NR12R13; R1 se selecciona de H, halo, alquilo, haloalquilo, heteroalquilo, heterohaloalquilo, heteroarilo, -OH, -O-alquilo, -O-arilo, -O-heteroalquilo, -O-heteroarilo, -SH, -S-alquilo, -S-arilo, -S-heteroalquilo, -S-heteroarilo, -NH2, -NHR14, -NR14R15, -NO2, -S(O)NHR10, -S(O)NR10R11, -S(O)R10, -S(O)2NHR10, -S(O)2NR10R11, y -S(O)2R10; R2 (cuando R2 no esta unido con R9) se selecciona de H y alquilo; n = 0, 1 o 2; R3 se selecciona de H, -alquilo, -alquenilo, alquinilo, arilo, heteroarilo, y cicloalquilo, donde cada uno de dicho -alquilo, dicho -alquenilo, dicho alquinilo, dicho arilo, dicho heteroarilo, y dicho cicloalquilo, es no sustituido u opcional e independientemente sustituido con desde uno a tres sustituyentes, los cuales pueden ser iguales o diferentes, cada sustituyente se selecciona independientemente de halo, -OH, alquilo, -O-alquilo, -O-alquenilo, -O-haloalquilo, -O-haloalquenilo, -OC(O)-alquilo, -OC(O)-alquenilo, -OC(O)-haloalquilo, -OC(O)-haloalquenilo, -C(O)O-alquilo, -C(O)O-alquenilo, -C(O)O-haloalquilo, -C(O)O-haloalquenilo, arilo, heteroarilo, cicloalquilo, cicloalquenilo, heterocicloalquilo, y heterocicloalquenilo; R4 se selecciona de H, -OH, halo, -alquilo, -alquenilo, alquinilo, azido, arilo, heteroarilo, -O-alquilo,-O-alquenilo, -OC(O)-alquilo, -SH, -S-alquilo, -NH2, -NO2, -NHR10, -NR10R11, -C(O)OH, -C(O)OR10, -C(O)NH2, -C(O)NHR10, -C(O)NR10R11, -S(O)NHR10, -S(O)NR10R11, -S(O)R10, -S(O)2NHR10, -S(O)2NR10R11 y -S(O)2R10, donde cada uno de dicho -alquilo, dicho -alquenilo, dicho alquinilo, dicho arilo, dicho heteroarilo, dicho -O-alquilo, dicho -O-alquenilo, dicho -OC(O)-alquilo, y dicho -S-alquilo es no sustituido u opcional e independientemente sustituido con desde uno a tres sustituyentes, los cuales pueden ser iguales o diferentes, cada sustituyente se selecciona independientemente de halo, -OH, alquilo, haloalquilo, heteroalquilo, heterohaloalquilo, -O-alquilo, -O-alquenilo, -O-haloalquilo, -O-haloalquenilo, -OC(O)-alquilo, -OC(O)-alquenilo, -OC(O)-haloalquilo, -OC(O)-haloalquenilo, -C(O)O-alquilo, -C(O)O-alquenilo, -C(O)O-haloalquilo, -C(O)O-haloalquenilo, arilo, heteroarilo, cicloalquilo, cicloalquenilo, heterocicloalquilo, y heterocicloalquenilo; R5 se selecciona de H, -OH, halo, -alquilo, -alquenilo, alquinilo, azido, arilo, heteroarilo, -O-alquilo, -O-alquenilo, -OC(O)-alquilo, -SH, -S-alquilo, -NH2, -NO2, -NHR10, -NR10R11, -C(O)OH, -C(O)OR10, -C(O)NH2, -C(O)NHR10, -C(O)NR10R11, -S(O)NHR10, -S(O)NR10R11, -S(O)R10, -S(O)2NHR10, -S(O)2NR10R11, y -S(O)2R10 donde cada uno de dicho -alquilo, dicho -alquenilo, dicho alquinilo, dicho arilo, dicho heteroarilo, dicho -O-alquilo, dicho -O-alquenilo, dicho -OC(O)-alquilo, y dicho -S-alquilo es no sustituido u opcional e independientemente sustituido con desde uno a tres sustituyentes, los cuales pueden ser iguales o diferentes, cada sustituyente se selecciona independientemente de halo, -OH, alquilo, haloalquilo, heteroalquilo, heterohaloalquilo, -O-alquilo, -O-alquenilo, -O-haloalquilo, -O-haloalquenilo, -OC(O)-alquilo, -OC(O)-alquenilo, -OC(O)-haloalquilo, -OC(O)-haloalquenilo, -C(O)O-alquilo, -C(O)O-alquenilo, -C(O)O-haloalquilo, -C(O)O-haloalquenilo, arilo, heteroarilo, cicloalquilo, cicloalquenilo, heterocicloalquilo, y heterocicloalquenilo; o, en forma alternativa, R4 y R5 se toman juntos con el átomo de carbono al cual están éstos se muestran unidos para formar un anillo espirocicloalquilo de 3 a 7 miembros, saturado o parcialmente insaturado que contiene desde 0 a 3 heteroátomos del anillo espiro seleccionados de O, N, y S; R6 se selecciona de H, -OH, halo, -alquilo, -alquenilo, alquinilo, azido, arilo, heteroarilo, -O-alquilo,-O-alquenilo, -OC(O)-alquilo, -SH, -S-alquilo, -NH2, -NO2, -NHR10, -NR10R11, -C(O)OH, -C(O)OR10, -C(O)NH2, -C(O)NHR10, -C(O)NR10R11, -S(O)NHR10, -S(O)NR10R11, -S(O)R10, -S(O)2NHR10, -S(O)2NR10R11, y -S(O)2R10, donde cada uno de dicho -alquilo, dicho -alquenilo, dicho alquinilo, dicho arilo, dicho heteroarilo, dicho -O-alquilo, dicho -O-alquenilo, dicho -OC(O)-alquilo, y dicho S-alquilo es no sustituido u opcional o independientemente sustituido con desde uno a tres sustituyentes, los cuales pueden ser iguales o diferentes, cada sustituyente se selecciona independientemente de halo, -OH, alquilo, haloalquilo, heteroalquilo, heterohaloalquilo, -O-alquilo, -O-alquenilo, -O-haloalquilo, -O-haloalquenilo, -OC(O)-alquilo, -OC(O)-alquenilo, -OC(O)-haloalquilo, -OC(O)-haloalquenilo, -C(O)O-alquilo, -C(O)O-alquenilo, -C(O)O-haloalquilo, -C(O)O-haloalquenilo, arilo, heteroarilo, cicloalquilo, cicloalquenilo, heterocicloalquilo, y heterocicloalquenilo; o, en forma alternativa, R5 y R6 se toman juntos para formar un enlace doble; R7 se selecciona de H, -OH, halo, -alquilo, -alquenilo, alquinilo, azido, arilo, heteroarilo, -O-alquilo,-O-alquenilo, -OC(O)-alquilo, -SH, -S-alquilo, -NH2, -NO2, -NHR10, -NR10R11, -C(O)OH, -C(O)OR10, -C(O)NH2, -C(O)NHR10, -C(O)NR10R11, -S(O)NHR10, -S(O)NR10R11, -S(O)R10, -S(O)2NHR10, -S(O)2NR10R11, y -S(O)2R10, donde cada uno de dicho -alquilo, dicho -alquenilo, dicho alquinilo, dicho arilo, dicho heteroarilo, dicho -O-alquilo, dicho -O-alquenilo, dicho -OC(O)-alquilo, y dicho S-alquilo es no sustituido u opcional o independientemente sustituido con desde uno a tres sustituyentes, los cuales pueden ser iguales o diferentes, cada sustituyente se selecciona independientemente de halo, -OH, alquilo, haloalquilo, heteroalquilo, heterohaloalquilo, -O-alquilo, -O-alquenilo, -O-haloalquilo, -O-haloalquenilo, -OC(O)-alquilo, -OC(O)-alquenilo, -OC(O)-haloalquilo, -OC(O)-haloalquenilo, -C(O)O-alquilo, -C(O)O-alquenilo, -C(O)O-haloalquilo, -C(O)O-haloalquenilo, arilo, heteroarilo, cicloalquilo, cicloalquenilo, heterocicloalquilo, y heterocicloalquenilo; o, en forma alternativa, R6 y R7 se toman juntos con el átomo de carbono al cual están éstos se muestran unidos para formar un anillo espirocicloalquilo de 3 a 7 miembros, saturado o parcialmente insaturado que contiene desde 0 a 3 heteroátomos del anillo espiro seleccionados de O, N, y S; R8 se selecciona de H, -OH, halo, -alquilo, -alquenilo, alquinilo, azido, arilo, heteroarilo, -O-alquilo, -O-alquenilo, -OC(O)-alquilo, -SH, -S-alquilo, -NH2, -NO2, -NHR10, -NR10R11, -C(O)OH, -C(O)OR10, -C(O)NH2, -C(O)NHR10, -C(O)NR10R11, -S(O)NHR10, -S(O)NR10R11, -S(O)R10, -S(O)2NHR10, -S(O)2NR10R11, y -S(O)2R10, donde cada uno de dicho -alquilo, dicho -alquenilo, dicho alquinilo, dicho arilo, dicho heteroarilo, dicho -O-alquilo, dicho -O-alquenilo, dicho -OC(O)-alquilo, y dicho S-alquilo es no sustituido u opcional o independientemente sustituido con desde uno a tres sustituyentes, los cuales pueden ser iguales o diferentes, cada sustituyente se selecciona independientemente de halo, -OH, alquilo, haloalquilo, heteroalquilo, heterohaloalquilo, -O-alquilo, -O-cicloalquilo, -O-
Applications Claiming Priority (1)
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EP (1) | EP2326627A1 (es) |
JP (2) | JP5731976B2 (es) |
AR (1) | AR072937A1 (es) |
AU (1) | AU2009282567B2 (es) |
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-
2009
- 2009-08-19 EP EP09741507A patent/EP2326627A1/en not_active Withdrawn
- 2009-08-19 TW TW098127908A patent/TWI409265B/zh not_active IP Right Cessation
- 2009-08-19 WO PCT/US2009/054264 patent/WO2010022121A1/en active Application Filing
- 2009-08-19 AR ARP090103181A patent/AR072937A1/es not_active Application Discontinuation
- 2009-08-19 JP JP2011523950A patent/JP5731976B2/ja not_active Expired - Fee Related
- 2009-08-19 US US13/059,193 patent/US8697694B2/en active Active
- 2009-08-19 AU AU2009282567A patent/AU2009282567B2/en not_active Ceased
- 2009-08-19 CA CA2734486A patent/CA2734486A1/en not_active Abandoned
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2015
- 2015-02-17 JP JP2015028549A patent/JP2015129153A/ja active Pending
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TWI409265B (zh) | 2013-09-21 |
TW201020255A (en) | 2010-06-01 |
AU2009282567A1 (en) | 2010-02-25 |
JP2012500278A (ja) | 2012-01-05 |
AU2009282567B2 (en) | 2014-10-02 |
US8697694B2 (en) | 2014-04-15 |
JP5731976B2 (ja) | 2015-06-10 |
CA2734486A1 (en) | 2010-02-25 |
EP2326627A1 (en) | 2011-06-01 |
WO2010022121A1 (en) | 2010-02-25 |
JP2015129153A (ja) | 2015-07-16 |
US20110318305A1 (en) | 2011-12-29 |
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