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AR059075A1 - Bencesulfonil - cromano , tiocromano tetrahidronaftaleno e inhibidores de gamma secretasa relacionados - Google Patents

Bencesulfonil - cromano , tiocromano tetrahidronaftaleno e inhibidores de gamma secretasa relacionados

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Publication number
AR059075A1
AR059075A1 ARP070100225A ARP070100225A AR059075A1 AR 059075 A1 AR059075 A1 AR 059075A1 AR P070100225 A ARP070100225 A AR P070100225A AR P070100225 A ARP070100225 A AR P070100225A AR 059075 A1 AR059075 A1 AR 059075A1
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Argentina
Prior art keywords
alkylene
alkyl
independently selected
group
substituted
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ARP070100225A
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Schering Corp
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    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/22—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/94—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D313/02—Seven-membered rings
    • C07D313/06—Seven-membered rings condensed with carbocyclic rings or ring systems
    • C07D313/08—Seven-membered rings condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
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    • C07D335/00—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
    • C07D335/04—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
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    • 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
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    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
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    • 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
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
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    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/08—One of the condensed rings being a six-membered aromatic ring the other ring being five-membered, e.g. indane
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    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/10—One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline
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    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/12—One of the condensed rings being a six-membered aromatic ring the other ring being at least seven-membered

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  • Organic Chemistry (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
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  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Formulaciones que comprenden dichos compuestos, pueden ser utiles, por ejemplo en el tratamiento de la enfermedad de Alzheimer. Reivindicacion 1: Un compuesto de formula (1), o una sal, solvato, o éster del mismo farmacéuticamente aceptable, donde: X está seleccionado del grupo que consiste en -C(R1)2-, -O-, -S-, -S(O2)-, -NR1-, y -N(C(O)R1)-; cada R1 está seleccionado independientemente del grupo que consiste en H y alquilo; R2, R3, y R4 están cada uno seleccionados independientemente del grupo que consiste en: (1) H, (2) alquilo, (3) -OR5, (4) alquileno-OR5, (5) -alquileno-R6, (6) -C(O)-alquilo, (7) -alquileno-C(O)-alquilo, (8) -C(O)-R6, (9) -alquileno-C(O)-R6, (10) -C(O)O-alquilo, (11) -alquileno-C(O)O-alquilo, (12) -C(O)NH- alquilo, (13) -alquileno-C(O)NH-alquilo, (14) -C(O)N(alquilo)2, (15) -alquileno-C(O)N(alquilo)2, (16) -R8, (17) -alquileno-R8, (18) -NHR5, (19) -N(R5)2, (20) -alquileno-NHR5 , (21) -alquileno-N(R5)2, (22) alquenilo, (23) -NH-R8, (24) -NH- CH(C(O)Oalquilo(C1-6))-alquileno-O-alquileno-R6, (25) -NCH(C(O)Oalquilo(C1-6))-alquileno-OH, (26) -NH-C(O)-alquenilo, y (27) -N alquilo(C1-6)C(O)-alquenilo; o R2 y R3, o R2 y un R4, o R3 y un R4, conjuntamente con los átomos a los cuales se muestra que están unidos forman un anillo cicloalquilo o heterocicloalquilo fusionado, donde dicho anillo cicloalquilo o heterocicloalquilo fusionado está no sustituido o sustituido con uno o más grupos L3; y con la condicion de que cuando X es -O- y m es 1, entonces por lo menos uno de R2, R3 o R4 no es H; Cada R5 está seleccionado independientemente del grupo que consiste en: (1) H, (2) alquilo(C1-6), (3) alquilo hidroxilo-sustituido, (4) R6, (5) R7, (6) -C(O)alquilo(C 1-6), (7) -C(O)- haloalquilo(C1-6), (8) -C(O)-R6, (9) -C(O)-R7, (10) -C(O)NH-alquilo(C1-6), (11) -C(O)N(alquilo(C1-C6))2 donde cada alquilo está seleccionado independientemente, (12) -S(O)2-alquilo(C1-6), (13) -S(O)2- haloalquilo(C1-6), (14) -S(O)2-R6, (15) -S(O)2- R7, (16) -S(O)2-R8, (17) -alquileno-C(O)-alquilo(C1-6), (18) -alquileno-C(O)-haloalquilo (C1-6), (19) -alquileno-C(O)R6, (20) -alquileno-C(O)-R7, (21) -alquileno-S(O)2-alquilo (C1-6), (22) -alquileno-S(O)2-haloalquilo(C1-6), (23) -alquileno-S(O)2- R6, (24) -alquileno-S(O)2-R7, (25) -alquileno-S(O)2-R8, (26) -alquileno-NHC(O)-alquilo(C1-6), (27) -alquileno-NHC(O)-haloalquilo (C1-6), (28) -alquileno-NHC(O)-R6, (29) -alquileno-NHC(O)-R7, (30) -alquileno-NHS(O)2-alquilo(C1-6), (31) -alquileno- NHS(O)2-haloalquilo (C1-6), (32) -alquileno-NHS(O)2-R6, (33) -alquileno-NHS(O)2-R7, (34) -alquileno- N(alquilo)C(O)-alquilo(C1-6), (35) -alquileno-N(alquilo)C(O)-haloalquilo(C1-6), (36) -alquileno-N(alquilo)C(O)-R6, (37) -alquileno-N(alquilo)C(O)- R7, (38) -alquileno-N(alquilo)S(O)2-alquilo(C1-6), (39) -alquileno-N(alquilo)S(O)2-haloalquilo(C1-6), (40)-alquileno-N(alquilo)S(O)2-R6, (41) -alquileno- N(alquilo)S(O)2-R7, (42) -alquileno-C(O)-NH-alquilo(C1-6), (43) -alquileno-C(O)-NHR6, (44) - alquileno-C(O)-NHR7, (45) -alquileno-S(O)2NH-alquilo(C1-6), (46) -alquileno-S(O)2NH-R6, (47) -alquileno-S(O)2NH-R7, (48) -alquileno-C(O)N(alquilo(C 1-6))2 donde cada grupo alquilo está seleccionado independientemente, (49) -alquileno-C(O)- N(alquilo)R6, (50) -alquileno-C(O)N(alquilo)R 7, (51) -alquileno-S(O)2N(alquilo(C1-6))2 donde cada grupo alquilo está seleccionado independientemente, (52) -alquileno-S(O)2N(alquilo)-R6, (53) -alquileno-S(O)2N(alquilo)-R7, (54) -alquileno-OH, (55) - alquileno-OC(O)-NH-alquilo, (56) -alquileno-OC(O)NH-R8, (57) -alquileno-CN, (58) -R8, (59) -alquileno-SH, (60) -alquileno-S(O)2-NH-R8, (61) -alquileno-S(O)2-alquileno-R6, (62) alquileno halo-sustituido, (63) -C(O)OR8, (64) -C(O)Oalquilo(C1--6), (65) -C(O)R8, (66) -C(O)alquileno-O-(C1-6)alquiIo, (67) -C(O)NH2, (68) -alquileno-O-(C1-6)alquilo, (69) -alquileno-R8, (70) -S(O)2-haloalquilo(C1-6), (71) haloalquilo(C1-6) hidroxi sustituido, (72) -alquileno-NH2, (73) -alquileno-NH-S(O)2-R8, (74) - alquileno-NH-C(O)-R8, (75) -alquileno-NH-C(O)O-alquilo(C1-6), (76) -alquileno-O-C(O)-alquilo(C1-6), (77) -alquileno-O-S(O)2-alquilo(C1-6), (78) -alquileno-R6, (79) -alquileno-R7, (80) -alquileno-NH-C(O)-NH-alquilo(C1-6), (81) -alquileno- N(S(O)2haloalquilo(C1-6)2 donde cada resto -S(O)2haloalquilo(C1-6) está seleccionada independientemente, (82) -alquileno-N(alquilo(C1-6))S(O)2R8, (83) -alquileno-OC(O)-N(alquilo)2 donde cada alquilo está seleccionado independientemente, (84) - alquileno-NH-alquilo(C1-6), (85) -C(O)-alquileno-C(O)O-alquilo(C1-6), (86) -C(O)-C(O)-O-alquilo(C1-6), (87) -C(O)-alquileno-R6, (88) -C(O)-NH-R8, (89) -C(O)-NH-R6, (90) -C(O)-NH-alquileno-R6, (91) -C(O) alquileno-NH-S(O)2-haloalquilo(C1-6), (92) - C(O)-alquileno-NH-C(O)-O-alquilo(C1-6), (93) -C(O)-alquileno-NH2, (94) -C(O)-alquileno-NH-S(O)2-R8, (95) -C(O)-alquileno-NH-S(O)2-alquilo(C1-6), (96) -C(O)-alquileno-NH-C(O) alquilo(C1-6), (97) -C(O)-alquileno-N(S(O)2alquilo(C1-6))2 donde cada resto -S(O)2alquilo(C1-6) está seleccionada independientemente, (98) -C(O)alquileno-NH-C(O)-NH-alquilo(C 1-6), (99) -alquileno-O-R6, (100) -alquileno-R7, (101) -C(O)OH, (102) -alquileno-N(S(O)2alquilo(C1-6))2, (103) -alquileno-C(O)-O-alquilo(C1- 6), (104) haloalquilo, (105) halo, (106) -alquileno-C(O)-NH2, (107) =N-O-alquilo(C1-6), (108) =N-O-alquileno-R6, (109) =N-O-alquenilo, (110) =N-O-R6, (111) =N-NH-S(O)2-R6, (112) alquenilo, (113) =R8, (114) -alquileno-O-alquileno-Si(alquilo(C1-6))3 donde cada alquilo está seleccionado independientemente, (115) -alquileno-S(O)2-N(alquileno-R6)2 donde cada resto alquileno-R6 está seleccionado independientemente, (116) -alquileno-S(O)2-NH2, (117) -O-C(O)-R9, (118) -O-C(O)-alquilo(C1-6), (119) - S(O)2NH(alquilo(C1-6)), (120) -S(O)2N(alquilo(C1-6))2 donde cada alquilo está seleccionado independientemente, (121) -S(O)2NHR8, (122) -alquileno-C(O)OH, (123) -alquileno-Ç(O)NH(haloalquilo(C1-6)), (124) -alquileno-C(O)-NH-alquileno-R8, (125) - alquileno-C(O)-NH-alquileno-OH (por ejemplo, -CH2-C(O)-NH-CH2CH2- OH), (126) -C(O)O(haloalquilo C1-6), (127) -C(O)OR6, (128) -C(O)OR7, (129) -alquileno-NHSO2N(alquilo)2 donde cada alquilo está seleccionado independientemente, (130) -alquileno- NHSO2NHalquilo, (131) -alquileno-N(alquilo)-SO2N(alquilo)2 donde cada alquilo está seleccionado independientemente, (132) -alquileno-N(alquilo)-SO2NHalquilo donde cada alquilo está seleccionado independientemente, (133) -alquileno-O-SO2-alquilo, (134) -alquileno-NH-C(O)-N(alquilo)2 donde cada alquilo está seleccionado independientemente, (135) -alquileno-NH-C(O)-NHalquilo, (136) -alquileno-N(alquilo)-C(O)-N-(alquilo)2 donde cada alquilo está seleccionado independientemente, (137) -alquileno- N(alquilo)-C(O)-NHalquilo, (138) -CN, (139) -alquileno-P(O)(Oalquilo)2 donde cada alquilo está seleccionado independientemente, (140) -alquileno-CH(OH)-P(O)(Oalquilo)2 (por ejemplo, -alquileno-CH(OH)-P(O)(Oalquilo(C1-6))2 donde cada alquilo está seleccionado independientemente, (141) -alquileno-OC(O)N(alquilo C1-6)-R8, (142) -alquileno-S(O)2-N(alquilo C1-6)-R8, (143) -alquileno-N(alquilo C1-6)-S(O)2-R8, (144) -alquileno-N(alquilo C1-6)-C(O)-R8, (145) -alquileno-N(alquilo C1-6)-C(O)O- alquilo(C1-6) donde cada alquilo está seleccionado independientemente, (146) -alquileno-N(alquilo C1-6)-C(O)-NH-alquilo(C1-6) donde cada alquilo está seleccionado independientemente, (147) -alquileno-NH-C(O)-N(alquilo C1-6)2 donde cada alquilo está seleccionado independientemente, (148) -alquileno-N(alquilo C1-6)-C(O)-N(alquilo C1-6)2 donde cada alquilo está seleccionado independientemente, (149) -C(O)-N(alquilo C1-6)-R8, (150) -C(O)-N(alquilo C1-6)-R6, (151) -C(O)-N(alquilo C1-6)-alquileno- R6, (152) -C(O)-alquileno-N(alquilo C1-6)-S(O)2-haloalquilo(C1-6) donde cada alquilo está seleccionado independientemente, (153) -C(O)-alquileno-N(alquilo C1-6)-C(O)-O-alquilo(C1-C6) donde cada alquilo está seleccionado independientemente, (154) - C(O)alquileno-NH(alquilo C1-6), (155) -C(O)-alquileno-N(alquilo C1-6)2 donde cada alquilo está seleccionado independientemente, (156) -C(O)-alquileno-N(alquilo C1-6)-S(O)2-R8, (157) -C(O)-alquileno-N(alquilo C1-6)-S(O)2-alquilo(C1-6), (158) -C(O)- alquileno-N(alquilo C1-6)-C(O)-alquilo(C1-6), (159) -C(O)-alquileno-N(alquilo Ç1-6)-C(O)-NH-alquilo(C1-6) donde cada alquilo está seleccionado independientemente, (160) -C(O)-alquileno-NH-C(O)-N(alquilo(C1-6))2 donde cada alquilo está seleccionado independientemente, (161) -C(O)-alquileno-N(alquilo C1-6)-C(O)-N(alquilo(C1-6))2 donde cada alquilo está seleccionado independientemente, (162) -alquileno-C(O)-NH(alquilo C1-6), (163) -alquileno-C(O)-N(alquilo C1-6)2 donde cada alquilo está seleccionado independientemente, (164) =N-N(alquilo C1-6)-S(O)2-R6, (165) -S(O)2N(alquilo C1-6)R8, (166) -alquileno-C(O)N(alquilo C1-6)(haloalquilo(C1-6)) donde cada grupo alquilo está seleccionado independientemente, (167) -alquileno- C(O)N(haloalquilo(C1-6))2 donde cada grupo alquilo está seleccionado independientemente, (168) -alquileno-C(O)-N(alquilo C1-6)-alquileno-R8, (169) -alquileno-C(O)-N(alquilo C1-6)-alquileno-OH, y (170) -O-C(O)-R7; R6 está seleccionado del grupo que consiste en: arilo(C6-14) no sustituido, arilo(C6-14) sustituido con uno o más grupos L1, heteroarilo(C5-14) no sustituido, y heteroarilo(C5-14) sustituido con uno o más grupos L1; R7 está seleccionado del grupo que consiste en heterocicloalquilo no sustituido y heterocicloalquilo sustituido con uno o más grupos L2; R8 está seleccionado del grupo que consiste en cicloalquilo no sustituido y cicloalquilo sustituido con uno o más grupos L3; Ar está seleccionado del grupo que consiste en: (a) arilo no sustituido, (b) arilo sustituido con uno o más grupos L1, (c) heteroarilo no sustituido, y (d) heteroarilo sustituido, que está sustituido con uno o más grupos L1; R9 es un anillo heterocicloalquilo multicíclico unido con enlaces donde dicho resto R9 está no sustituido o dicho resto R9 está sustituido con uno o más grupos L2; cada L1 está seleccionado independientemente del grupo que consiste en: halo
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