Nothing Special   »   [go: up one dir, main page]

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

Links

Classifications

    • 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
    • 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
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/41—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
    • 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
    • A61K31/41—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
    • 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
    • A61K31/435—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
    • 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
    • A61K31/435—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
    • A61K31/444—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
    • 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
    • A61K31/435—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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • 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
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • 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
    • C07D209/52—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 condensed with a ring other than six-membered
    • 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
    • C07D401/02—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
    • 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
    • C07D401/10—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 aromatic rings
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D403/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D403/10—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 linked by a carbon chain containing aromatic 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • C07D413/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole 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.
ARP140103584A 2013-09-26 2014-09-26 Moduladores octahidro-ciclopenta[c]pirrol negativos de nr2b AR097794A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361883050P 2013-09-26 2013-09-26

Publications (1)

Publication Number Publication Date
AR097794A1 true AR097794A1 (es) 2016-04-13

Family

ID=52744524

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP140103584A AR097794A1 (es) 2013-09-26 2014-09-26 Moduladores octahidro-ciclopenta[c]pirrol negativos de nr2b

Country Status (9)

Country Link
US (4) US9540324B2 (es)
EP (2) EP3036221B1 (es)
JP (1) JP6546596B2 (es)
CN (1) CN105916843B (es)
AR (1) AR097794A1 (es)
ES (2) ES2707739T3 (es)
TW (1) TW201605791A (es)
UY (1) UY35750A (es)
WO (1) WO2015048507A1 (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR097794A1 (es) 2013-09-26 2016-04-13 Mnemosyne Pharmaceuticals Inc Moduladores octahidro-ciclopenta[c]pirrol negativos de nr2b
JO3579B1 (ar) * 2014-09-26 2020-07-05 Luc Therapeutics Inc مُعدِلات تفاغرية سالبة لمستقبل nr2b من المركب n-ألكيل أريل-5-أوكسي أريل-ثامن هيدرو-خماسي الحلقة [c] بيرول
CA2992820C (en) 2015-08-05 2022-08-16 Indivior Uk Limited Dopamine d3 receptor antagonists having a bicyclo moiety
WO2018232158A1 (en) * 2017-06-15 2018-12-20 Belite Bio, Inc. Methods of treating metabolic diseases with fused bicyclic pyrroles
CA3121850A1 (en) 2019-01-03 2020-07-09 Avive Solutions, Inc. Defibrillator communications architecture

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5532243A (en) 1992-02-14 1996-07-02 The Dupont Merck Pharmaceutical Company Antipsychotic nitrogen-containing bicyclic compounds
US5262564A (en) 1992-10-30 1993-11-16 Octamer, Inc. Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents
DE4341403A1 (de) * 1993-12-04 1995-06-08 Basf Ag N-substituierte 3-Azabicycloalkan-Derivate, ihre Herstellung und Verwendung
US5541217A (en) * 1995-05-17 1996-07-30 Ortho Pharmaceutical Corporation 4-arylcyclopenta[c]pyrrole analgesics
US6369076B1 (en) * 1999-10-29 2002-04-09 Merck & Co. Inc. 5-benzyl-octahydroindole and 6-benzyl-decahydroquinoline NMDA/NR2B antagonists
CA2440803A1 (en) * 2001-03-07 2002-09-12 Pfizer Products Inc. Modulators of chemokine receptor activity
EP1391451B1 (en) 2001-04-19 2011-11-23 Eisai R&D Management Co., Ltd. 2-iminopyrrolidine derivates
CA2558211C (en) 2004-03-03 2013-09-03 Chemocentryx, Inc. Bicyclic and bridged nitrogen heterocycles
US7696241B2 (en) 2004-03-04 2010-04-13 Bristol-Myers Squibb Company Bicyclic compounds as modulators of androgen receptor function and method
CN101001860A (zh) * 2004-06-09 2007-07-18 霍夫曼-拉罗奇有限公司 杂环抗病毒化合物
EP1778688A1 (en) 2004-07-22 2007-05-02 Glaxo Group Limited Antibacterial agents
CA2603876A1 (en) 2005-04-19 2006-10-26 Merck & Co., Inc. N-alkyl-azacycloalkyl nmda/nr2b antagonists
EP1849772A1 (en) 2006-04-28 2007-10-31 Laboratorios Del Dr. Esteve, S.A. Bicyclic tetrahydropyrrole compounds
CA2640806A1 (en) 2006-04-28 2007-11-15 Laboratorios Del Dr. Esteve, S.A. Bicyclic tetrahydropyrrole compounds
CN101230058A (zh) 2007-01-23 2008-07-30 上海恒瑞医药有限公司 双环氮杂烷类衍生物、其制备方法及其在医药上的用途
TW200845977A (en) 2007-03-30 2008-12-01 Targacept Inc Sub-type selective azabicycloalkane derivatives
US8907095B2 (en) 2007-10-22 2014-12-09 Merck Sharp & Dohme Corp. Bicyclic heterocycle derivatives and their use as modulators of the activity of GPR119
EP2246347B1 (en) * 2008-01-23 2016-09-28 Shanghai Hengrui Pharmaceutical Co. Ltd. Dicycloazaalkane derivates, preparation processes and medical uses thereof
US8211933B2 (en) 2008-12-12 2012-07-03 Vanderbilt University 3.3.0 bicyclic GlyT1 inhibitors and methods of making and using same
FR2945533B1 (fr) * 2009-05-12 2011-05-27 Sanofi Aventis Derives de cyclopenta°c!pyrrolyl-alkylcarbamates d'heterocycles a 5 chainons, leur preparation et leur application en therapeutique
FR2945534B1 (fr) * 2009-05-12 2012-11-16 Sanofi Aventis DERIVES DE CYCLOPENTAL[c]PYRROLE-2-CARBOXYLATES, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE
BR112012016733A2 (pt) 2010-01-07 2015-09-01 Du Pont "composto, composição fungicida e método"
US8796470B2 (en) 2010-05-25 2014-08-05 Abbvie Inc. Substituted octahydrocyclopenta[c]pyrroles as calcium channel modulators
WO2011149995A1 (en) * 2010-05-25 2011-12-01 Abbott Laboratories Novel substituted octahydrocyclopenta [c]pyrrol-4-amines as calcium channel blockers
US8501768B2 (en) 2011-05-17 2013-08-06 Hoffmann-La Roche Inc. Hexahydrocyclopentapyrrolone, hexahydropyrrolopyrrolone, octahydropyrrolopyridinone and octahydropyridinone compounds
EP2721029B1 (en) * 2011-06-16 2018-07-18 Merck Sharp & Dohme Corp. Imidazopyridin-2-one derivatives
CN103732588B (zh) * 2011-07-27 2016-10-12 南京奥昭生物科技有限公司 螺环分子作为蛋白激酶抑制剂
JO3611B1 (ar) 2011-08-10 2020-08-27 Janssen Sciences Ireland Uc سايكلو بنتا (سي (بيرول 4,3 ثاني هيدرو 1 hمستبدله [8,1] نافثيريدينونات مضادة للجراثيم
WO2013091539A1 (zh) 2011-12-21 2013-06-27 江苏恒瑞医药股份有限公司 吡咯并六元杂芳环类衍生物、其制备方法及其在医药上的应用
AU2013322838B2 (en) * 2012-09-25 2018-02-01 F. Hoffmann-La Roche Ag New bicyclic derivatives
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
AR097794A1 (es) 2013-09-26 2016-04-13 Mnemosyne Pharmaceuticals Inc Moduladores octahidro-ciclopenta[c]pirrol negativos de nr2b
EA037928B1 (ru) 2014-03-26 2021-06-08 Ф. Хоффманн-Ля Рош Аг Бициклические соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa)

Also Published As

Publication number Publication date
UY35750A (es) 2015-04-30
TW201605791A (zh) 2016-02-16
US20150225342A1 (en) 2015-08-13
US11116749B2 (en) 2021-09-14
EP3461827B1 (en) 2022-02-23
ES2910848T3 (es) 2022-05-13
US20230012073A1 (en) 2023-01-12
CN105916843A (zh) 2016-08-31
US20180325868A1 (en) 2018-11-15
US20170071906A1 (en) 2017-03-16
EP3036221A4 (en) 2017-01-25
EP3461827A1 (en) 2019-04-03
CN105916843B (zh) 2019-09-20
WO2015048507A1 (en) 2015-04-02
JP2016536348A (ja) 2016-11-24
ES2707739T3 (es) 2019-04-04
US9540324B2 (en) 2017-01-10
US10052306B2 (en) 2018-08-21
EP3036221B1 (en) 2018-11-07
EP3036221A1 (en) 2016-06-29
JP6546596B2 (ja) 2019-07-17

Similar Documents

Publication Publication Date Title
AR103199A1 (es) N-alquilaril-5-oxiaril-octahidrociclopenta[c]pirrol moduladores alóstericos negativos de nr2b
AR103064A1 (es) Compuestos moduladores de fxr (nr1h4)
AR104176A1 (es) Inhibidores de ido (indolamina-2,3-dioxigenasa)
AR104884A1 (es) Compuestos de 4-hidroxi-3-(heteroaril)piridin-2-ona como agonistas de apj
AR105845A1 (es) Compuestos de heteroarilo bicíclicos fusionados como moduladores de la función irak4
AR099177A1 (es) Determinadas (2s)-n-[(1s)-1-ciano-2-feniletil]-1,4-oxazepan-2-carboxamidas como inhibidores de dipeptidil peptidasa 1
AR095326A1 (es) Heterociclos tricíclicos como inhibidores de la proteína bet
AR097082A1 (es) Compuestos terapéuticamente activos y sus métodos de uso
AR092742A1 (es) Piridinonas antifibroticas
AR091193A1 (es) HETEROCICLOS DE 5 MIEMBROS QUE CONTIENEN NITROGENO SUSTITUIDO POR CARBOXAMIDA O SULFONAMIDA COMO MODULADORES PARA EL RECEPTOR NUCLEAR HUERFANO RORg
AR090220A1 (es) Inhibidores de serina/treonina cinasa
AR097794A1 (es) Moduladores octahidro-ciclopenta[c]pirrol negativos de nr2b
AR103170A1 (es) Compuestos y composiciones farmacéuticas de los mismos para el tratamiento de desordenes inflamatorios y osteoartritis
AR107061A1 (es) Heteroarilhidroxipirimidinonas como agonistas del receptor de apj
AR090203A1 (es) Compuestos heterobiciclicos como inhibidores de pde10
AR101815A1 (es) Compuestos y composiciones como inhibidores de quinasa
AR096837A1 (es) Heterociclos tricíclicos como inhibidores de proteínas bet
EA201590581A1 (ru) Соединения бис-(фторалкил)-1,4-бензодиазепинона и их пролекарства
AR105575A1 (es) COMPUESTOS DE QUINOLINA COMO MODULADORES DE TNFa
AR091858A1 (es) INHIBIDORES DE CISTATIONIN-g-LIASA (CSE)
AR095426A1 (es) Inhibidores tripeptídicos de la epoxicetona proteasa
AR088781A1 (es) Compuestos antimicrobianos y metodos para prepararlos y utilizarlos
AR092869A1 (es) Alcoxipirazoles como activadores de guanilato ciclasa soluble
AR106865A1 (es) Piridinas sustituidas y métodos de uso
AR091490A1 (es) Antagonistas de iap

Legal Events

Date Code Title Description
FB Suspension of granting procedure