AR112907A1 - Pirazoles inhibidores de monoacilglicerol lipasa (magl) - Google Patents
Pirazoles inhibidores de monoacilglicerol lipasa (magl)Info
- 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
Links
- 150000003217 pyrazoles Chemical class 0.000 title abstract 2
- 102000004882 Lipase Human genes 0.000 title 1
- 108090001060 Lipase Proteins 0.000 title 1
- 239000004367 Lipase Substances 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 235000019421 lipase Nutrition 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 16
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 7
- 229910052736 halogen Inorganic materials 0.000 abstract 6
- 150000002367 halogens Chemical class 0.000 abstract 6
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 5
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- -1 -C (O) NR8R9 Chemical group 0.000 abstract 2
- 102000005398 Monoacylglycerol Lipase Human genes 0.000 abstract 2
- 108020002334 Monoacylglycerol lipase Proteins 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
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- 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
- A61K31/435—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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- 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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- 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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- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
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- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- 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.
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US201762510213P | 2017-05-23 | 2017-05-23 |
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ARP180101355A AR112907A1 (es) | 2017-05-23 | 2018-05-22 | Pirazoles inhibidores de monoacilglicerol lipasa (magl) |
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EP (2) | EP3630744B1 (es) |
JP (2) | JP7157771B2 (es) |
KR (2) | KR102643778B1 (es) |
CN (2) | CN110678456B (es) |
AR (1) | AR112907A1 (es) |
AU (1) | AU2018271876B2 (es) |
BR (1) | BR112019024566A2 (es) |
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CL (1) | CL2019003397A1 (es) |
CO (1) | CO2019013013A2 (es) |
CR (1) | CR20190536A (es) |
DK (1) | DK3630744T3 (es) |
DO (1) | DOP2019000283A (es) |
EA (1) | EA201992409A1 (es) |
EC (1) | ECSP19084085A (es) |
ES (1) | ES2940111T3 (es) |
FI (1) | FI3630744T3 (es) |
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PH (1) | PH12019502548A1 (es) |
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PT (1) | PT3630744T (es) |
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SA (1) | SA519410589B1 (es) |
SI (1) | SI3630744T1 (es) |
TW (1) | TWI786117B (es) |
UA (1) | UA124990C2 (es) |
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