AR096339A1 - Agonistas del receptor de somatostatina subtipo 4 (sstr4) - Google Patents

Agonistas del receptor de somatostatina subtipo 4 (sstr4)

Info

Publication number
AR096339A1
AR096339A1 ARP140101981A ARP140101981A AR096339A1 AR 096339 A1 AR096339 A1 AR 096339A1 AR P140101981 A ARP140101981 A AR P140101981A AR P140101981 A ARP140101981 A AR P140101981A AR 096339 A1 AR096339 A1 AR 096339A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
group
monocyclic
bicyclic
Prior art date
Application number
ARP140101981A
Other languages
English (en)
Inventor
Ferrara Marco
Just Stefan
Kuelzer Raimund
Lingard Iain
Mazzaferro Rocco
Rudolf Klaus
Giovannini Riccardo
Cui Yunhai
Doods Henri
Original Assignee
Boehringer Ingelheim Int
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 Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR096339A1 publication Critical patent/AR096339A1/es

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    • 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
    • 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
    • A61K31/41—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
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—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
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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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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    • A61K31/41—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
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    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • 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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    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/495—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
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    • A61K31/50—Pyridazines; Hydrogenated pyridazines
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
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    • 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
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    • 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
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    • 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
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • C07D487/04—Ortho-condensed systems

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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Peptides Or Proteins (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Derivados de la amida del ácido 3-aza-biciclo[3.1.0]hexan-6-carboxílico de la fórmula general (1), que son agonistas del receptor de somatostatina subtipo 4 (SSTR4), útiles para la prevención o el tratamiento de trastornos médicos relacionados con SSTR4. Además, procesos para preparar composiciones farmacéuticas, así como procesos para la fabricación de compuestos de acuerdo con la presente. Reivindicación 1: Compuestos caracterizados por la fórmula (1) en donde A se selecciona del grupo que consiste en H y alquilo C₁₋₆; R¹ y R² se seleccionan independientemente del grupo que consiste en H, alquilo C₁₋₆ y cicloalquilo C₃₋₆, en donde al menos uno de R¹ o R² es alquilo C₁₋₆ o cicloalquilo C₃₋₆, en donde alquilo C₁₋₆ o cicloalquilo C₃₋₆ se sustituyen opcionalmente con halógenos o MeO-, o en donde R¹ y R² juntos forman un puente de alquileno de 2 a 5 miembros opcionalmente sustituido con halógenos, que incorpora de 0 a 2 heteroátomos que se seleccionan independientemente del grupo que consiste en N, O y S; W se selecciona del grupo que consiste en arilo monocíclico o bicíclico, heteroarilo monocíclico o bicíclico, heterociclilo monocíclico o bicíclico, y cicloalquilo monocíclico o bicíclico, en donde cada uno de estos sistemas de anillos se sustituye opcionalmente con uno o más R³; y en donde el heteroarilo comprende hasta 4 heteroátomos y uno o dos anillos de 5 ó 6 miembros; R³ se selecciona independientemente del grupo que consiste en alquilo C₁₋₆, cicloalquilo C₃₋₈, alquil C₁₋₆-O-, bencilo, halógeno, HO-, NC-, heteroarilo monocíclico o bicíclico, y heterociclilo monocíclico de 5 ó 6 miembros que contiene un heteroátomo seleccionado del grupo que consiste en N, O ó S(O)ʳ, en donde el heteroarilo contiene hasta 4 heteroátomos y uno o dos anillos de 5 ó 6 miembros, y r es 0, 1 ó 2, en donde alquilo C₁₋₆, cicloalquilo C₃₋₈, alquil C₁₋₆-O-, bencilo, heteroarilo y heterociclilo se sustituyen opcionalmente con halógenos, HO-, acetilo, alquil C₁₋₆-O-, oxo, R⁴-S(O)₂-, en donde R⁴ es arilo, cicloalquilo C₃₋₆ y/o alquilo C₁₋₆; Y se selecciona del grupo que consiste en un enlace, -CH₂-, -CH₂CH₂- y -CH₂O-; o una sal de cualquiera de los compuestos mencionados anteriormente.
ARP140101981A 2013-05-17 2014-05-16 Agonistas del receptor de somatostatina subtipo 4 (sstr4) AR096339A1 (es)

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