PE20200293A1 - Inhibidores pirazolicos de magl - Google Patents

Inhibidores pirazolicos de magl

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Publication number
PE20200293A1
PE20200293A1 PE2019002453A PE2019002453A PE20200293A1 PE 20200293 A1 PE20200293 A1 PE 20200293A1 PE 2019002453 A PE2019002453 A PE 2019002453A PE 2019002453 A PE2019002453 A PE 2019002453A PE 20200293 A1 PE20200293 A1 PE 20200293A1
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PE
Peru
Prior art keywords
alkyl
magl
halogen
pyrazolic
inhibitors
Prior art date
Application number
PE2019002453A
Other languages
English (en)
Inventor
Cheryl A Grice
Olivia D Weber
Daniel J Buzard
Michael B Shaghafi
John J M Wiener
Justin S Cisar
Katharine K Duncan
Original Assignee
Lundbeck La Jolla Research Center Inc
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Application filed by Lundbeck La Jolla Research Center Inc filed Critical Lundbeck La Jolla Research Center Inc
Publication of PE20200293A1 publication Critical patent/PE20200293A1/es

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    • C07D471/00—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
    • 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
    • C07D471/10—Spiro-condensed systems
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • 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
    • A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive 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
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • C07D231/38—Nitrogen 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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    • 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
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    • 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
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    • 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
    • C07D413/12—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 chain containing hetero atoms as chain links
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    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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    • C07D451/00—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
    • 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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    • 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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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
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Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE PIRAZOL DE FORMULA (I) DONDE R1 ES -N(R2)C(O)R15 O -N(H)SO2R15; R2 ES H O ALQUILO C1-6; R3 ES UN COMPUESTO DE FORMULA (i), (ii), ENTRE OTROS, EN DONDE R4 ES H, HALOGENO, ALQUILO C1-6, ENTRE OTROS; R5 ES H, CN, HALOGENO, ENTRE OTROS; R6 Y R12 SON CADA UNO H, HALOGENO O ALQUILO C1-6; R10 ES -O-HALOALQUILO C1-6, -O-CICLOALQUILO C3-8, ENTRE OTROS; R13 ES H O ALQUILO C1-6; R15 ES ALQUILO C1-6 O CICLOALQUILO C3-8. SON COMPUESTOS PREFERIDOS: 5-(2-CLORO-5-((4-(3-(METILSULFONAMIDO)-1H-PIRAZOL-1-CARBONIL)PIPERAZIN-1-IL)METIL)FENIL)HEXAHIDROPIRROLO[3,4-C]PIRROL-2(1H)-CARBOXAMIDA; 4-((4-(3-(METILSULFONAMIDO)-1H-PIRAZOL-1-CARBONIL)PIPERAZIN-1-IL)METIL)-2-(TRIFLUOROMETIL)BENZAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DE LA MONOACILGLICEROL LIPASA (MAGL) SIENDO UTILES PARA EL TRATAMIENTO DEL DOLOR
PE2019002453A 2017-05-23 2018-05-22 Inhibidores pirazolicos de magl PE20200293A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762510223P 2017-05-23 2017-05-23
PCT/US2018/033964 WO2018217809A1 (en) 2017-05-23 2018-05-22 Pyrazole magl inhibitors

Publications (1)

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PE20200293A1 true PE20200293A1 (es) 2020-02-05

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US (1) US11149037B2 (es)
EP (1) EP3634404A4 (es)
JP (1) JP7162622B2 (es)
KR (1) KR20200010366A (es)
CN (1) CN110678177B (es)
AU (1) AU2018273888A1 (es)
BR (1) BR112019024488A2 (es)
CA (1) CA3065898A1 (es)
CL (1) CL2019003398A1 (es)
CO (1) CO2019013016A2 (es)
CR (1) CR20190537A (es)
DO (1) DOP2019000295A (es)
EA (1) EA201992504A1 (es)
EC (1) ECSP19083923A (es)
JO (1) JOP20190267A1 (es)
MA (1) MA50405A (es)
MX (1) MX2019014041A (es)
NI (1) NI201900120A (es)
PE (1) PE20200293A1 (es)
PH (1) PH12019502646A1 (es)
RU (1) RU2019137094A (es)
WO (1) WO2018217809A1 (es)

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PL3630744T3 (pl) 2017-05-23 2023-05-15 H. Lundbeck A/S Pirazolowe inhibitory magl
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JOP20190267A1 (ar) 2017-05-23 2019-11-18 Lundbeck La Jolla Research Center Inc مثبطات بيرازول magl
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