AR044974A1 - Derivados duales de nk1/nk3, su uso, procedimiento de preparacion y medicamento para el tratamiento de la esquizofrenia - Google Patents

Derivados duales de nk1/nk3, su uso, procedimiento de preparacion y medicamento para el tratamiento de la esquizofrenia

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Publication number
AR044974A1
AR044974A1 ARP040102313A ARP040102313A AR044974A1 AR 044974 A1 AR044974 A1 AR 044974A1 AR P040102313 A ARP040102313 A AR P040102313A AR P040102313 A ARP040102313 A AR P040102313A AR 044974 A1 AR044974 A1 AR 044974A1
Authority
AR
Argentina
Prior art keywords
alkyl
unsubstituted
halogen
substituted
lower alkyl
Prior art date
Application number
ARP040102313A
Other languages
English (en)
Inventor
Torsten Hoffmann
Andreas Koblet
Jens-Uwe Peters
Patrick Schnider
Andrew Sleight
Heinz Stadler
Original Assignee
Hoffmann La Roche
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=33560750&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR044974(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR044974A1 publication Critical patent/AR044974A1/es

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/72Nitrogen atoms
    • C07D213/75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4418Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
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    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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    • A61K31/468-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
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    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/4995Pyrazines or piperazines forming part of bridged ring systems
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    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53861,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
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    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
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    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/547Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame spiro-condensed or forming part of bridged ring systems
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    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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    • A61K31/554Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
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    • C07D401/04Heterocyclic 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
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    • C07D417/00Heterocyclic 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
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    • C07D417/04Heterocyclic 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
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    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
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  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
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  • Pyridine Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Reivindicación 1: El uso de compuestos de la fórmula general (1), en donde: R1 es arilo, sin sustituir o sustituido por uno o más sustituyentes, seleccionados del grupo, consistente en alquilo inferior, alcoxilo inferior, halógeno, -(CH2)oOH, -C(O)H, CF3, CN, S-alquilo inferior, -S(O)-alquilo inferior, -C(O)NR'R'', -NR'R'', -NR'C(O)-alquilo inferior, -NR'S(O)2-alquilo inferior, o es heteroarilo, seleccionados de los grupos, consistentes en piridin-2- ó 3-ilo, imidazolilo u oxazolilo, sin sustituir o sustituido por alquilo inferior, halógeno o alcoxilo; R2 y R3 son independientemente el uno del otro hidrógeno, halógeno, alquilo, alcoxilo, OCHF2, OCH2F, OCF3 ó CF3; R4, R5 son independientemente el uno del otro hidrógeno, -(CR'R'')1-(CR'R'')1-(CR'R'')0,1-OH ó -(CR'R'')1-(CR'R'')1-(CR'R'')0,1-alquilo inferior, en donde R' y R'' en cada átomo de carbono puede ser el mismo o diferente el uno del otro, -C1,2-alquilo; -C(O)H; -(CH)2ocicloalquilo, sin sustituir o sustituido por hidroxilo; -(CH2)1,2,3NR'R''; -(CH2)1,2,3NR'C(O)-alquilo inferior; -(CH2)1,2,3NR'S(O)2-alquilo inferior; -(CH2)oS(O)-alquilo inferior; R' es hidrógeno, alquilo inferior, -(CH2)oOH, -C(O)H, -C(O)-alquilo inferior, -C(O)-cicloalquilo, -S(O)2-alquilo inferior; R'' es hidrógeno o alquilo inferior; o R4 y R5 forman junto con el átomo N al que están unidos un anillo con: -(CH2)3-5-, que está sin sustituir o sustituido por uno o más sustituyentes, seleccionados del grupo consistente en alquilo, halógeno, -(CR'R'')oOH, =O, -CHO, -NR'R'', en donde R' y R'' pueden formar junto con el átomo N al que están unidos un anillo con -(CH2)3-5, o mediante -(CH2)oNR'-C(O)-alquilo, -(CH2)o-C(O)-alquilo inferior, -(CH2)o-C(O)-cicloalquilo, -(CH2)oOC-(O)NR'R'', -(CH2)o-S(O)2-alquilo, -(CH2)o-S(O)-alquilo inferior, -(CH2)o-S-alquilo inferior, -(CH2)o-S(O)2-NR'R'', -(CH2)o-pirrolidinilo, o -C(O)NR'R'', o con -(CH2)1,2,3-NR'-(CH2)2-, que está sin sustituir o sustituido por uno o más sustituyentes, seleccionados del grupo consistente en alquilo inferior, halógeno, CF3, -(CR'R'')oOH, =O, -CHO, -NR'R'', en donde R' y R'' pueden formar junto con el átomo N al que están unidos un anillo con -(CH2)3-5, o mediante -(CH2)oNR'-C(O)-alquilo inferior, -(CH2)o-C(O)-alquilo inferior, -(CH2)o-C(O)-cicloalquilo, -(CH2)oOC(O)NR'R'', -(CH2)o-S(O)2-alquilo inferior, -(CH2)o-pirrolidinilo o -C(O)NR'R'', o con -(CH2)1,2,3-O-(CH2)2-, que está sin sustituir o sustituido por uno o más sustituyentes, seleccionados del grupo consistente en alquilo, halógeno, -(CR'R'')oOH, =O, -CHO, -NR'R'', en donde R' puede formar junto con el átomo N al que están unidos un anillo con -(CH2)3-5, o mediante -(CH2)oNR'-C(O)-alquilo inferior , -(CH2)o-C(O)-alquilo inferior, -(CH2)o-C(O)-cicloalquilo, -(CH2)oOC(O)NR'R'', -(CH2)o-S(O)2-alquilo inferior, -(CH2)o-pirrolidinilo o -C(O)NR'R'', o con -(CH2)1,2,3-S(O)0,1,2-(CH2)1,2,3-, que está sin sustituir o sustituido por uno o más sustituyentes, seleccionados del grupo consistente en alquilo inferior, halógeno, CF3, -(CR'R'')oOH, =O, -NR'R'', en donde R' y R'' pueden formar junto con el átomo N- al que están unidos un anillo con -(CH2)3-5, o -(CH2)oNR'-C(O)-alquilo inferior, -(CH2)o-C(O)-alquilo, -(CH2)o-C(O)-cicloalquilo, -(CH2)oOC(O)NR'R'', -(CH2)o-S(O)2-alquilo inferior, -(CH2)o-pirrolidi-nilo o -C(O)NR'R'', o con -CH2CH=CH-CH2-, que está sin sustituir o sustituido por uno o más sustituyentes, seleccionados del grupo consistente en alquilo, halógeno, -(CR'R'')oOH, =O, -CHO, -NR'R'', en donde R' y R'' pueden formar junto con el átomo N al que está unido un anillo con -(CH2)3-5, o mediante -(CH2)oNR'-C(O)-alquilo inferior, -(CH2)o-C(O)-alquilo inferior, -(CH2)o-C(O)-cicloalquilo, -(CH2)oOC(O)NR'R'', -(CH2)o-S(O)2-alquilo inferior, -(CH2)o-pirrolidinilo o -C(O)NR'R'', o es 0, 1, 2, ó 3 o sales de adición ácida farmacéuticamente activas de los mismos, para la preparación de medicamentos para el tratamiento de esquizofrenia.
ARP040102313A 2003-07-03 2004-07-01 Derivados duales de nk1/nk3, su uso, procedimiento de preparacion y medicamento para el tratamiento de la esquizofrenia AR044974A1 (es)

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IL172614A0 (en) 2006-04-10
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