[go: up one dir, main page]

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

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

Info

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
Authority
AR
Argentina
Prior art keywords
alkylene
alkyl
independently selected
group
substituted
Prior art date
Application number
ARP070100225A
Other languages
English (en)
Original Assignee
Schering Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Schering Corp filed Critical Schering Corp
Publication of AR059075A1 publication Critical patent/AR059075A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • 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
    • C07D311/04—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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/14—Sulfones; Sulfoxides having sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/16—Sulfones; Sulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C317/20—Sulfones; Sulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of rings other than six-membered aromatic rings of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • 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
    • C07D311/78—Ring systems having three or more relevant rings
    • C07D311/80—Dibenzopyrans; Hydrogenated dibenzopyrans
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • 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
    • C07D311/78—Ring systems having three or more relevant rings
    • C07D311/92—Naphthopyrans; Hydrogenated naphthopyrans
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • 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
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D313/00—Heterocyclic compounds containing rings of more than six members having one oxygen atom as the only ring hetero atom
    • 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
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D335/06—Benzothiopyrans; Hydrogenated benzothiopyrans
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • 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
    • C07C2602/08—One of the condensed rings being a six-membered aromatic ring the other ring being five-membered, e.g. indane
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • 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
    • C07C2602/10—One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • 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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Medicinal Chemistry (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • 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)
  • Pyrane Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • 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
ARP070100225A 2006-01-20 2007-01-18 Bencesulfonil - cromano , tiocromano tetrahidronaftaleno e inhibidores de gamma secretasa relacionados AR059075A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US76084206P 2006-01-20 2006-01-20
US81487106P 2006-06-19 2006-06-19

Publications (1)

Publication Number Publication Date
AR059075A1 true AR059075A1 (es) 2008-03-12

Family

ID=38171604

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070100225A AR059075A1 (es) 2006-01-20 2007-01-18 Bencesulfonil - cromano , tiocromano tetrahidronaftaleno e inhibidores de gamma secretasa relacionados

Country Status (17)

Country Link
US (2) US8067621B2 (es)
EP (1) EP1976843B1 (es)
JP (1) JP5047992B2 (es)
KR (1) KR20080095885A (es)
CN (1) CN102702044A (es)
AR (1) AR059075A1 (es)
AU (1) AU2007207481B2 (es)
BR (1) BRPI0706685A2 (es)
CA (1) CA2637897A1 (es)
EC (1) ECSP088638A (es)
IL (1) IL192906A0 (es)
MX (1) MX2008009414A (es)
NO (1) NO20083598L (es)
PE (1) PE20071321A1 (es)
RU (1) RU2448964C2 (es)
TW (1) TW200738666A (es)
WO (1) WO2007084595A2 (es)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR049377A1 (es) * 2004-04-05 2006-07-26 Schering Corp Inhibidores de secretasa gamma
MX2007000040A (es) * 2004-06-30 2007-03-07 Schering Corp N-arilsulfonilaminas heterociclicas sustituidas como inhibidores de gamma-secretasas.
JP5047992B2 (ja) 2006-01-20 2012-10-10 シェーリング コーポレイション ガンマセクレターゼ阻害剤としての、炭素環および複素環アリールスルホン
AU2008275735B2 (en) * 2007-07-05 2014-03-27 Merck Sharp & Dohme Corp. Tetrahydropyranochromene gamma secretase inhibitors
CA2693216A1 (en) * 2007-07-17 2009-01-22 Schering Corporation Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors
US8486940B2 (en) 2009-09-11 2013-07-16 Probiodrug Ag Inhibitors
US20110190269A1 (en) * 2010-02-01 2011-08-04 Karlheinz Baumann Gamma secretase modulators
EP2691393B1 (en) * 2011-03-31 2016-09-14 Pfizer Inc Novel bicyclic pyridinones
US8933116B2 (en) * 2011-04-04 2015-01-13 Merck Sharp & Dohme Corp. Gamma secretase inhibitors
WO2013036464A1 (en) * 2011-09-09 2013-03-14 Merck Sharp & Dohme Corp. Gamma secretase inhibitors
UA110688C2 (uk) * 2012-09-21 2016-01-25 Пфайзер Інк. Біциклічні піридинони
WO2014085211A2 (en) * 2012-11-29 2014-06-05 Merck Sharp & Dohme Corp. Spirocyclic sulfones as gamma secretase inhibitors
EA028033B1 (ru) 2013-03-14 2017-09-29 Новартис Аг 3-пиримидин-4-ил-оксазолидин-2-оны в качестве ингибиторов мутантного idh
US9643947B2 (en) 2013-08-28 2017-05-09 Northwestern University 7-membered fused heterocycles and methods of their synthesis
TN2017000342A1 (en) 2015-02-03 2019-01-16 Pfizer Novel cyclopropabenzofuranyl pyridopyrazinediones
MA42049A (fr) * 2015-05-07 2021-03-17 Bristol Myers Squibb Co Sulfones tricycliques utiles commes modulateurs ror-gamma
US10787428B2 (en) * 2015-12-24 2020-09-29 Kyowa Kirin Co., Ltd. α,β-unsaturated amide compound
MA46461A (fr) * 2016-10-10 2021-04-07 Bristol Myers Squibb Co Sulfones tricycliques en tant que modulateurs de ror gamma
CN110049985B (zh) * 2016-10-13 2022-05-31 百时美施贵宝公司 作为RORγ调节剂的杂环砜类
AU2017356911A1 (en) * 2016-11-09 2019-06-20 Bristol-Myers Squibb Company Tricyclic sulfones as ROR gamma modulators
WO2018226992A1 (en) 2017-06-07 2018-12-13 Adrx, Inc. Tau aggregation inhibitors
SG11201912770SA (en) * 2017-06-23 2020-01-30 Kyowa Kirin Co Ltd a, ß-UNSATURATED AMIDE COMPOUND
EP3668886A2 (en) 2017-08-18 2020-06-24 Adrx, Inc. Tau aggregation peptide inhibitors
ES2812698T3 (es) 2017-09-29 2021-03-18 Probiodrug Ag Inhibidores de glutaminil ciclasa
WO2019222438A1 (en) * 2018-05-17 2019-11-21 Bristol-Myers Squibb Company Tricyclic sulfone compound as a ror gamma modulator

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4826967A (en) * 1987-06-16 1989-05-02 Naxcor Psoralen-nucleoside adducts and method for their preparation
FR2639349B1 (fr) * 1988-11-23 1991-02-22 Sanofi Sa Nouveaux derives du chromane actifs sur le systeme nerveux central, leur procede de preparation et les compositions pharmaceutiques en contenant
CA2009664A1 (en) * 1989-02-27 1990-08-27 Philip Thiam Shin Lau Tetrahydroquinolines and method of preparation
AU8854091A (en) * 1990-10-10 1992-05-20 Schering Corporation Bis-benzo cyclohepta piperidylidene, piperidine and piperazine compounds, compositions and methods of use
PL179448B1 (pl) * 1994-01-31 2000-09-29 Pfizer Neuroochronne zwiazki chromanoloweoraz kompozycje farmaceutyczne zawierajace te zwiazki PL PL PL PL PL
DE19533023B4 (de) * 1994-10-14 2007-05-16 Basf Ag Neue Carbonsäurederivate, ihre Herstellung und Verwendung
JP3810838B2 (ja) * 1994-12-12 2006-08-16 三共アグロ株式会社 除草性イソオキサゾリン誘導体
WO1999051587A1 (fr) * 1998-04-01 1999-10-14 Ono Pharmaceutical Co., Ltd. Derives de thiophene condenses et medicaments contenant ceux-ci comme principe actif
MXPA01008606A (es) 1999-02-26 2003-05-05 Merck & Co Inc Compuestos de sulfonamida novedosos y uso de los mismos.
MXPA04001014A (es) 2001-08-03 2004-05-27 Schering Corp Novedosos inhibidores de la gama secretasa.
GB0223039D0 (en) * 2002-10-04 2002-11-13 Merck Sharp & Dohme Therapeutic compounds
US7410964B2 (en) * 2003-05-16 2008-08-12 Merck Sharp & Dohme Ltd. Cyclohexyl sulphones as gamma-secretase inhibitors
EP1586561A1 (en) * 2004-04-13 2005-10-19 Cephalon, Inc. Bicyclic aromatic sulfinyl derivatives
MX2007000040A (es) * 2004-06-30 2007-03-07 Schering Corp N-arilsulfonilaminas heterociclicas sustituidas como inhibidores de gamma-secretasas.
JP5047992B2 (ja) 2006-01-20 2012-10-10 シェーリング コーポレイション ガンマセクレターゼ阻害剤としての、炭素環および複素環アリールスルホン
UY30377A1 (es) 2006-06-02 2008-01-02 Elan Pharm Inc Inhibidores triciclicos fusionados de sulfonamida de gama-secretasa
AU2008275735B2 (en) 2007-07-05 2014-03-27 Merck Sharp & Dohme Corp. Tetrahydropyranochromene gamma secretase inhibitors

Also Published As

Publication number Publication date
RU2008133856A (ru) 2010-02-27
US20070197581A1 (en) 2007-08-23
IL192906A0 (en) 2009-02-11
AU2007207481A1 (en) 2007-07-26
JP2009528980A (ja) 2009-08-13
MX2008009414A (es) 2008-10-01
WO2007084595A2 (en) 2007-07-26
US20120264736A1 (en) 2012-10-18
US8067621B2 (en) 2011-11-29
PE20071321A1 (es) 2007-12-29
CN102702044A (zh) 2012-10-03
KR20080095885A (ko) 2008-10-29
BRPI0706685A2 (pt) 2011-04-05
TW200738666A (en) 2007-10-16
JP5047992B2 (ja) 2012-10-10
EP1976843B1 (en) 2013-09-04
AU2007207481B2 (en) 2012-08-23
US8569521B2 (en) 2013-10-29
CA2637897A1 (en) 2007-07-26
ECSP088638A (es) 2008-08-29
RU2448964C2 (ru) 2012-04-27
NO20083598L (no) 2008-10-20
EP1976843A2 (en) 2008-10-08
WO2007084595A3 (en) 2007-09-07

Similar Documents

Publication Publication Date Title
AR059075A1 (es) Bencesulfonil - cromano , tiocromano tetrahidronaftaleno e inhibidores de gamma secretasa relacionados
PE20090630A1 (es) Derivados de indol 2-carboxi sustituidos y metodos para su utilizacion
ES2552338T3 (es) Compuestos farmacéuticos
AR023260A1 (es) Peptidos macrociclicos activos frente al virus de la hepatitis c.
AR071617A1 (es) Bencenosulfonamidas de oxazol y tiazol, composiciones farmaceuticas que las contienen, proceso de preparacion y uso de las mismas como agentes anticancerigenos.
NO20065830L (no) Substituerte 2-kinolyloksazoler som er anvendbare som PDE4-inhibitorer.
AR061726A1 (es) Piperidinas sustituidas que aumentan la actividad de p53 y su uso
ES2284856T3 (es) Derivados de quinolil propil piperidina, su preparacion y las composiciones que los contienen.
AR070234A1 (es) Compuestos que comprenden un grupo ciclobutoxi
PE20080457A1 (es) Compuestos de oximilo macrociclico inhibidores de proteasas de hepatitis c
PE20070751A1 (es) Derivados de isoxazolidina como inhibidores de la interaccion de proteinas bcl
PE20141005A1 (es) 1,3-oxazinas como inhibidores de bace1 y/o bace2
AR054618A1 (es) Compuestos de azetidina y su uso como inhibidores de proteasas
WO2003059269A3 (en) Acridone inhibitors of impdh enzyme
ATE341590T1 (de) Milchsäurepolymerzusammensetzung und formkörper daraus
AR062361A1 (es) Compuestos heterociclicos de fosfonatos y fosfinatos, composiciones farmaceuticas que los contienen y usos como agentes antidiabeticos
CO6150179A2 (es) Derivados de n-(amino-heteroaril)-1h-hindol-2-carboxamidas su preparacion y su aplicacion en terapeutica
PE20071326A1 (es) Inhibidores de la polimerasa viral
PE20080072A1 (es) Compuestos heterociclicos como inhibidores de proteasas serinas
AR057980A1 (es) Derivados de la 1- amino-ftalazina sustituida, su preparacion y composicion farmaceutica
NO20072198L (no) Korrosjons- og gasshydratinhibitorer med foroket biologisk nedbrytbarhet og redusert toksisitet
CO4990946A1 (es) Antagonistas del receptor de trombina
PE20090548A1 (es) Compuestos aza-biciclohexano como inhibidores de trombina
CO5580782A2 (es) Antibioticos de glicopeptido-cefalosporina entrecruzados
ES2347133T3 (es) Procedimiento e intermedios para preparar acetales de acido aspartico sustituidos.

Legal Events

Date Code Title Description
FA Abandonment or withdrawal