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AR097794A1 - Moduladores octahidro-ciclopenta[c]pirrol negativos de nr2b - Google Patents

Moduladores octahidro-ciclopenta[c]pirrol negativos de nr2b

Info

Publication number
AR097794A1
AR097794A1 ARP140103584A ARP140103584A AR097794A1 AR 097794 A1 AR097794 A1 AR 097794A1 AR P140103584 A ARP140103584 A AR P140103584A AR P140103584 A ARP140103584 A AR P140103584A AR 097794 A1 AR097794 A1 AR 097794A1
Authority
AR
Argentina
Prior art keywords
alkyl
group
alkylene
optionally substituted
substituents
Prior art date
Application number
ARP140103584A
Other languages
English (en)
Inventor
A Volkmann Robert
S Menniti Frank
R Anderson David
Original Assignee
Mnemosyne Pharmaceuticals Inc
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 Mnemosyne Pharmaceuticals Inc filed Critical Mnemosyne Pharmaceuticals Inc
Publication of AR097794A1 publication Critical patent/AR097794A1/es

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    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A—HUMAN NECESSITIES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4192—1,2,3-Triazoles
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/423—Oxazoles condensed with carbocyclic rings
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    • 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
    • A61K31/4439—Non 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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    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • 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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    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
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    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
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    • 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
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    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Indole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Se describen compuestos que modulan selectivamente de forma negativa los receptores de NMDA que contienen una subunidad NR1/NR2B, composiciones farmacéuticas que comprenden los compuestos y métodos para tratar una enfermedad usando los compuestos. Estos compuestos pueden utilizarse como terapia para mejorar la transmisión sináptica cerebral. Reivindicación 1: Un compuesto de la fórmula (1) o sal, profármaco, solvato, hidrato, tautómero o estereoisómero farmacéuticamente aceptable de este, donde: L¹ es alquilo C₂₋₄ lineal o ramificado opcionalmente sustituido con uno o más sustituyentes que se seleccionan del grupo que consiste en OH, D, OR¹⁰, NH₂, NHR¹⁰ y N(R¹⁰)(R¹⁰), con la condición de que no más de un oxígeno o nitrógeno se una a ningún carbono, o L¹ se selecciona del grupo que consiste en -CO-alquilenil C₁₋₂-, -S(O)₂-, -S(O)₂NH-, -C(O)NH-, -C(O)NR¹⁰-, -alquilenil C₁₋₃-C(O)-alquilenil C₁₋₃-, y un enlace, donde el alquilenil C₁₋₂ o alquilenil C₁₋₃ se sustituye opcionalmente con alquilo C₁₋₄; cada R¹⁰ Y R¹⁰ se selecciona independientemente del grupo que consiste en H; O-alquil C₁₋₅; alquilo C₁₋₆ opcionalmente sustituido con uno o más sustituyentes que se seleccionan del grupo que consiste en OH, O-alquil C₁₋₅, -OP(O)(OH)₂, OP(O)O₂⁻²M₂, -OC(O)alquilo, -OC(O)O-alquilo, arilo y heteroarilo; y cicloalquilo opcionalmente sustituido con uno o más sustituyentes que se seleccionan del grupo que consiste en OH y O-alquil C₁₋₅; con la condición de que no más de un oxígeno se una a ningún carbono de R¹⁰ y R¹⁰; M es un catión metálico monovalente; o R¹⁰ y R¹⁰, junto con el nitrógeno al cual están unidos, pueden formar un heterociclo; R¹ es arilo o heteroarilo, los cuales se sustituyen opcionalmente con uno o más sustituyentes que se seleccionan del grupo que consiste en OH, CN, halógeno, -O-R¹⁰, -OP(O)(OH)₂, OP(O)O₂⁻²M₂, -SH, -S-R¹⁰, alquilo C₁₋₅, alquilo ramificado, -haloalquil C₁₋₆, NH₂, NHR¹⁰, -hidroxialquil C₁₋₆, N(R¹⁰)(NR¹⁰), -NHS(O)₂R¹⁰, -O-alquilarilo, -O-(CH₂)ₙ-C(O)-arilo y NHCOR¹⁰; M es un catión metálico monovalente, o R¹ es cicloalquilo; X se selecciona del grupo que consiste en H, halógeno, OH, O-alquil C₁₋₆, O-alquilo ramificado, alquilo C₁₋₅ lineal y alquilo C₁₋₅ ramificado; Y e Y son independientemente H, F o metilo; L² es -(CH₂)ₙ- o -(CHR¹¹)ₙ-, o un enlace; cada R¹¹ se selecciona independientemente del grupo que consiste en H, -alquilenil C₁₋₅-, -C(O)-alquilenil C₁₋₅- y -alquilenil-CO-alquilenil-; R² es cicloalquil C₃₋₈; heterociclil C₃₋₈, fenilo, naftilo, heteroarilo o heteroarilo bicíclico, cada uno de los cuales se sustituye opcionalmente con uno o más sustituyentes que se seleccionan del grupo que consiste en halógeno, OH, alquil C₁₋₆, OR¹⁰, CN, NH₂, NHR¹⁰, N(R¹⁰)(R¹⁰), SH, SR¹⁰, SOR¹⁰, SO₂R¹⁰, SO₂NHR¹⁰, SO₂N(R¹⁰)(R¹⁰), CONH₂, CONR¹⁰ y CON(R¹⁰)(R¹⁰); y n es 1, 2 ó 3.
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