AR112907A1 - Pirazoles inhibidores de monoacilglicerol lipasa (magl) - Google Patents

Pirazoles inhibidores de monoacilglicerol lipasa (magl)

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Publication number
AR112907A1
AR112907A1 ARP180101355A ARP180101355A AR112907A1 AR 112907 A1 AR112907 A1 AR 112907A1 AR P180101355 A ARP180101355 A AR P180101355A AR P180101355 A ARP180101355 A AR P180101355A AR 112907 A1 AR112907 A1 AR 112907A1
Authority
AR
Argentina
Prior art keywords
alkyl
heterocycloalkyl
halogen
haloalkyl
heteroaryl
Prior art date
Application number
ARP180101355A
Other languages
English (en)
Inventor
John J M Wiener
Katharine K Duncan
Olivia D Weber
Cheryl A Grice
Original Assignee
Abide Therapeutics 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 Abide Therapeutics Inc filed Critical Abide Therapeutics Inc
Publication of AR112907A1 publication Critical patent/AR112907A1/es

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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • 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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    • A61K31/435—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
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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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
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    • 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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    • C07D451/02—Heterocyclic 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
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  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Compuestos pirazol y composiciones que los comprenden. Los compuestos y composiciones son útiles como moduladores de la monoacilglicerol lipasa (MAGL). Además, son útiles para el tratamiento del dolor. Reivindicación 1: Un compuesto de fórmula (1); caracterizado porque: R¹ es -C(O)OR¹⁵ o -C(O)NR¹⁰R¹¹; R² es H, halógeno, C₁₋₆ alquilo, o C₁₋₆ haloalquilo; R³ es un compuesto seleccionado del grupo de fórmulas (2); A es N o C(H); X es -O-, -N(R¹⁶)-, o -CH₂N(R¹⁶)CH₂-; Y es -CH₂- o -C(O)-; Z es -S-, -O-, o -N(R¹⁸)-; R⁴ es H, halógeno, -OR⁷, C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₁₋₆ haloalquilo, -C(O)NR⁸R⁹, C₃₋₈ cicloalquilo, C₂₋₉ heterocicloalquilo, -C₁₋₆ alquil-C₂₋₉ heterocicloalquilo, C₆₋₁₀ arilo, o C₁₋₉ heteroarilo, donde el C₃₋₈ cicloalquilo, C₂₋₉ heterocicloalquilo, -C₁₋₆ alquil-C₂₋₉ heterocicloalquilo, C₆₋₁₀ arilo, o C₁₋₉ heteroarilo opcionalmente están sustituidos con 1 ó 2 R¹⁴; R⁵ es H, halógeno, C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₁₋₆ haloalcoxilo, o fenilo; R⁶ es H, halógeno o C₂₋₆ alquilo; R⁷ es H, C₁₋₆ alquilo, C₁₋₆ haloalquilo, -C₁₋₆ alquil-OH, C₂₋₉ heterocicloalquilo, C₆₋₁₀ arilo, o C₁₋₉ heteroarilo, donde el C₂₋₉ heterocicloalquilo, C₆₋₁₀ arilo, o C₁₋₉ heteroarilo opcionalmente están sustituidos con 1 ó 2 R¹⁴; cada R⁸ y cada R⁹ se seleccionan independientemente entre H y C₁₋₆ alquilo; o R⁸ y R⁹ junto con el nitrógeno al cual están unidos, se combinan para formar un anillo heterocicloalquilo; R¹⁰ y R¹¹ son independientemente entre sí H o C₁₋₆ alquilo; R¹² es H, halógeno, o C₁₋₆ alquilo; R¹³ es H o C₁₋₆ alquilo; cada R¹⁴ se selecciona independientemente entre halógeno, -OH, C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₁₋₆ alcoxilo, -C₁₋₆ alquil-OH, C₃₋₈ cicloalquilo, -C(O)OH, -C(O) NR⁸R⁹, -SO₂-C₁₋₆ alquilo, y -N(R¹⁷)C(O)-C₁₋₆ alquilo; R¹⁵ es H o C₁₋₆ alquilo; R¹⁶ es H, C₁₋₆ alquilo, -C(O)-C₁₋₆ alquilo, -C₁₋₆ alquil-OH, o -CH₂CO₂H; R¹⁷ es H o C₁₋₆ alquilo; R¹⁸ es H o C₁₋₆ alquilo; v es 0 ó 1; n es 0 ó 1; m es 0 ó 1; p es 0, 1 ó 2; y q es 0, 1 ó 2; o un solvato, hidrato, tautómero, N-óxido, estereoisómero, o una sal farmacéuticamente aceptable del mismo.
ARP180101355A 2017-05-23 2018-05-22 Pirazoles inhibidores de monoacilglicerol lipasa (magl) AR112907A1 (es)

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