AR048065A1 - Compuestos de piperazina acetilinica y su uso como antagonistas del receptor de glutamato metabotropico - Google Patents

Compuestos de piperazina acetilinica y su uso como antagonistas del receptor de glutamato metabotropico

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Publication number
AR048065A1
AR048065A1 ARP050100613A ARP050100613A AR048065A1 AR 048065 A1 AR048065 A1 AR 048065A1 AR P050100613 A ARP050100613 A AR P050100613A AR P050100613 A ARP050100613 A AR P050100613A AR 048065 A1 AR048065 A1 AR 048065A1
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AR
Argentina
Prior art keywords
alkyl
nr5r6
group
6nr5r6
6alkyl
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ARP050100613A
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English (en)
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Nps Pharma Inc
Astrazeneca Ab
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Application filed by Nps Pharma Inc, Astrazeneca Ab filed Critical Nps Pharma Inc
Publication of AR048065A1 publication Critical patent/AR048065A1/es

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    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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    • 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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    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
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    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/38—Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
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    • C07—ORGANIC CHEMISTRY
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    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/61—Halogen atoms or nitro radicals
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    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/06—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals
    • C07D295/073—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals with the ring nitrogen atoms and the substituents separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
    • C07D295/205—Radicals derived from carbonic acid
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/14—Radicals substituted by singly bound hetero atoms other than halogen
    • C07D333/20—Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms

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Abstract

La presente se refiere a compuestos de piperazina acetilínca, procesos para la preparacion de los compuestos, composiciones farmacéuticas que contienen los compuestos, y uso de los compuestos en terapia. Reivindicacion 1: Un compuesto caracterizado porque responde a la formula (1) en donde: R1 se selecciona entre el grupo formado por hidroxi, halo, nitro, alquilhalo C1-6, Oalquilhalo C1-6, alquilo C1-6, Oalquilo C1-6, alquenilo C2-6, Oalquenilo C2-6, alquinilo C2-6, Oalquinilo C2-6, alquil C0- 6-cicloalquilo C3-6, Oalquil C0-6-cicloalquilo C3-6, alquilarilo C0-6, Oalquilarilo C0-6, CHO, (CO)R5, O(CO)R5, O(CO)OR5, O(CN)OR5, alquil C1-6-OR5, Oalquil C2-6-OR5, alquil C1-6(CO)R5, Oalquil C1-6(CO)R5, alquil C0-6CO2R5, Oalquil C1-6CO2R5, alquilciano C0-6, Oalquilciano C2-6, alquil C0-6NR5R6, Oalquil C2-6NR5R6, alquil C1-6(CO)NR5R6, Oalquil C1-6(CO)NR5R6, alquil C0-6NR5(CO)R6, Oalquil C2-6NR5(CO)R6, alquil C0-6NR5(CO)NR5R6, alquil C0-6SR5, Oalquil C2-6SR5, alquil C0-6(SO)R5, Oalquil C2-6(SO)R5, alquil C0-6SO2R5, Oalquil C2-6SO2R5, alquil C0-6(SO2)NR5R6, Oalquil C2-6(SO2)NR5R6, alquil C0-6NR5(SO2)R6, Oalquil C2-6NR5(SO2)R6, alquil C0-6NR5(SO2)NR5R6, Oalquil C2-6NR5(SO2)NR5R6, (CO)NR5R6, O(CO)NR5R6, NR5OR6, alquil C0-6NR5(CO)OR6, Oalquil C2-6NR5(CO)OR6, SO3R5 y un anillo de 5 o 6 miembros que contiene átomos seleccionados en forma independiente entre el grupo formado por C, N, O y S; R2 se selecciona entre el grupo formado por H, hidroxi, halo, nitro, alquilhalo C1-6, Oalquilhalo C1-6, alquilo C1-6, Oalquilo C1-6, alquenilo C2-6, Oalquenilo C2-6, alquinilo C2-6, Oalquinilo C2-6, alquil C0-6-cicloalquilo C3-6, Oalquil C0-6-cicloalquilo C3-6, alquilarilo C0-6, Oalquilarilo C0-6, CHO, (CO)R5, O(CO)R5, O(CO)OR5, O(CN)OR5, alquil C1-6-OR5, Oalquil C2-6OR5, alquil C1-6(CO)R5, Oalquil C1-6(CO)R5, alquil C0-6CO2R5, Oalquil C1-6CO2R5, alquilciano C0-6, Oalquilciano C2-6, alquil C0-6NR5R6, Oalquil C2-6NR5R6, alquil C1-6(CO)NR5R6, Oalquil C1-6(CO)NR5R6, alquil C0- 6NR5(CO)R6, Oalquil C2-6NR5(CO)R6, alquil C0-6NR5(CO)NR5R6, alquil C0-6SR5, Oalquil C2-6SR5, alquil C0-6(SO)R5, Oalquil C2-6(SO)R5, alquil C0-6SO2R5, Oalquil C2-6SO2R5, alquil C0-6(SO2)NR5R6, Oalquil C2-6(SO2)NR5R6, alquil C0-6NR5(SO2)R6, Oalquil C2- 6NR5(SO2)R6, alquil C0-6NR5(SO2)NR5R6, Oalquil C2-6NR5(SO2)NR5R6, (CO)NR5R6, O(CO)NR5R6, NR5OR6, alquil C0-6NR5(CO)OR6, Oalquil C2-6NR5(CO)OR6, SO3R5 y un anillo de 5 o 6 miembros que contiene átomos seleccionados en forma independiente entre el grupo formado por C, N, O y S; R3 se selecciona entre el grupo formado por: H, C(O)Oalquilhalo C1-6, C(O)Oalquilo C1-6, C(O)Oalquenilo C2-6, C(O)Oalquinilo C2-6, C(O)Oalquilo C0-6-cicloalquilo C3-6, C(O)O alquilarilo C0-6, C(O)Oalquil C1-6OR5, C(O)Oalquil C1-6(CO)R5, C(O)Oalquil C1-6CO2R5, C(O)Oalquilciano C1-6, C(O)Oalquil C0-6NR5R6, C(O)Oalquil C1-6(CO)NR5R6, C(O)Oalquil C2-6NR5(CO)R6, C(O)alquil C1-6NR5(CO)NR5R6, C(O)Oalquil C2-6SR5, C(O)Oalquil C1-6(SO)R5, C(O)Oalquil C1-6(SO2)R5, C(O)Oalquil C1-6(SO2)NR5R6, C(O)Oalquil C1-6NR5(SO2)R6, C(O)Oalquil C2-6NR5(SO2)NR5R6,(CO)NR5R6, C(O)Oalquil C1-6NR5(CO)OR6, C(S)Oalquilhalo C1-6, C(S)Oalquilo C1-6, C(S)Oalquenilo C2-6, C(S)Oalquinilo C2-6, C(S)Oalquil C0-6-cicloalquilo C3-6, C(S)Oalquilarilo C0-6, C(S)Oalquil C1-6OR5, C(S)Oalquil C1-6(CO)R5, C(S)Oalquil C1-6CO2R5, C(S)Oalquilciano C1-6, C(S)Oalquil C0-6NR5R6, C(S)Oalquil C1-6(CO)NR5R6, C(S)Oalquil C2-6NR5(CO)R6, C(S)alquil C1-6NR5(CO)NR5R6, C(S)Oalquil C2-6SR5, C(S)Oalquil C1-6(SO)R5, C(S)Oalquil C1-6SO2R5, C(S)Oalquil C1-6(SO2)NR5R6, C(S)Oalquil C1-6NR5(SO2)R6, C(S)Oalquil C2-6NR5(SO2)NR5R6, (CO)NR5R6, y C(S)Oalquil C1-6NR5(CO)OR6; R4 se selecciona entre el grupo formado por hidroxi, halo, nitro, alquilhalo C1-6, Oalquilhalo C1-6, alquilo C1-6, Oalquilo C1-6, alquenilo C2-6, Oalquenilo C2-6, alquinilo C2-6, Oalquinilo C2-6, alquil C0-6-cicloalquilo C3-6, Oalquil C0-6-cicloalquilo C3-6, alquilarilo C0-6, Oalquilarilo C0-6, CHO, (CO)R5, O(CO)R5, O(CO)OR5, O(CN)OR5, alquil C1-6-OR5, Oalquil C2-6OR5, alquil C1-6(CO)R5, Oalquil C1-6(CO)R5, alquil C0-6CO2R5, Oalquil C1-6CO2R5, alquilciano C0-6, Oalquilciano C2-6, alquil C0-6NR5R6, Oalquil C2-6NR5R6, alquil C1-6(CO)NR5R6, Oalquil C1- 6(CO)NR5R6, alquil C0-6NR5(CO)R6, Oalquil C2-6NR5(CO)R6, alquil C0-6NR5(CO)NR5R6, alquil C0-6SR5, Oalquil C2-6SR5, alquil C0-6(SO)R5, Oalquil C2-6(SO)R5, alquil C0-6SO2R5, Oalquil C2-6SO2R5, alquil C0-6(SO2)NR5R6, Oalquil C2-6(SO2)NR5R6, alquil C0- 6NR5(SO2)R6, Oalquil C2-6NR5(SO2)R6, alquil C0-6NR5(SO2)NR5R6, Oalquil C2-6NR5(SO2)NR5R6, (CO)NR5R6, O(CO)NR5R6, NR5OR6, alquil C0-6NR5(CO)OR6, Oalquil C2-6NR5(CO)OR6, =NR5, =NOR5, =O, =S, SO3R5 y un anillo de 5 o 6 miembros que contiene átomos seleccionados en forma independiente entre el grupo formado por C, N, O y S; M se selecciona entre el grupo formado por =O, (CR5R6)m y (CR5R6)mC(O); R5 y R6 se seleccionan en forma independiente entre el grupo formado por H, alquilo C1-6, Oalquilo C1-6, cicloalquilo C3-7, Ocicloalquilo C3-7, alquilarilo C1-6, Oalquilarilo C1-6, arilo y heteroarilo; cualquier alquilo C1-6, arilo o heteroarilo definido bajo R1, R2, R3, R4, R5 y R6 puede sustituirse con uno o más A; A se selecciona entre el grupo formado por H, hidroxi, halo, nitro, oxo, alquilciano C0-6, alquil C0-4-cicloalquilo C3-6, alquilo C1-6, alquilhalo C1-6, Oalquilhalo C1-6, alquenilo C2-6, alquilarilo C0-3, alquil C0-6OR5, Oalquil C2-6OR5, alquil C1-6SR5, Oalquil C2-6SR5, (CO)R5, O(CO)R5, Oalquilciano C2-6, Oalquil C1-6CO2R5, O(CO)OR5, Oalquil C1-6(CO)R5, alquil C1-6(CO)R5, NR5OR6, alquil C1-6NR5R6, Oalquil C2-6NR5R6, alquil C0-6(CO)NR5R6, Oalquil C1-6(CO)NR5R6, Oalquil C2-6NR5(CO)R6, alquil C0-6NR5(CO)R6, alquil C0- 6NR5(CO)NR5R6, O(CO)NR5R6, alquil C0-6(SO2)NR5R6, Oalquil C2-6(SO2)NR5R6, alquil C0-6NR5(SO2)R6, Oalquil C2-6NR5(SO2)R6, SO3R5, alquil C1-6NR5(SO2)NR5R6, Oalquil C2-6(SO2)R5, alquil C0-6(SO2)R5, alquil C0-6(SO)R5, Oalquil C2-6(SO)R5 y un anillo de 5 o 6 miembros que contiene uno o más átomos seleccionados en forma independiente entre el grupo formado por C, N, O y S; m es 1, 2 o 3; n es un entero entre 0 y 8, inclusive; o una sal aceptable para uso farmacéutico o hidrato del mismo.
ARP050100613A 2004-02-18 2005-02-18 Compuestos de piperazina acetilinica y su uso como antagonistas del receptor de glutamato metabotropico AR048065A1 (es)

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US (1) US20060235024A1 (es)
EP (1) EP1716130A1 (es)
JP (1) JP2007523179A (es)
KR (1) KR20070026382A (es)
CN (1) CN1934097A (es)
AR (1) AR048065A1 (es)
AU (1) AU2005214376A1 (es)
BR (1) BRPI0507499A (es)
CA (1) CA2556268A1 (es)
IL (1) IL177292A0 (es)
NO (1) NO20063597L (es)
RU (1) RU2006128445A (es)
TW (1) TW200531694A (es)
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AR058807A1 (es) 2005-09-29 2008-02-27 Astrazeneca Ab 5-(fenilisoxazoletoxi)-triazol-3-il piridinas sustituidas, para el tratamiento de trastornos mediados por el receptor mglur5
US8349852B2 (en) 2009-01-13 2013-01-08 Novartis Ag Quinazolinone derivatives useful as vanilloid antagonists
JP2013518085A (ja) 2010-02-01 2013-05-20 ノバルティス アーゲー ＣＲＦ−１受容体アンタゴニストとしてのピラゾロ［５，１ｂ］オキサゾール誘導体
AR080056A1 (es) 2010-02-01 2012-03-07 Novartis Ag Derivados de ciclohexil-amida como antagonistas de los receptores de crf
JP5748777B2 (ja) 2010-02-02 2015-07-15 ノバルティス アーゲー Ｃｒｆ受容体アンタゴニストとしてのシクロヘキシルアミド誘導体
EP2621490A4 (en) 2010-09-29 2014-04-02 Teva Pharma PROPARGYL-TRIFLUOROMETHOXY-AMINO-BENZOTHIAZOLE DERIVATIVES, PREPARATION THEREOF AND USE THEREOF
CN107982266B (zh) 2012-01-06 2021-07-30 H.隆德贝克有限公司 氨基甲酸酯化合物及其制备和使用方法
ES2878041T3 (es) 2015-03-18 2021-11-18 H Lundbeck As Carbamatos de piperazina y métodos para prepararlos y usarlos
CN113413387A (zh) 2015-05-11 2021-09-21 H.隆德贝克有限公司 治疗炎症或神经性疼痛的方法
US10463753B2 (en) 2016-02-19 2019-11-05 Lundbeck La Jolla Research Center, Inc. Radiolabeled monoacylglycerol lipase occupancy probe
WO2018053447A1 (en) 2016-09-19 2018-03-22 Abide Therapeutics, Inc. Piperazine carbamates and methods of making and using same
JOP20190105A1 (ar) 2016-11-16 2019-05-09 Lundbeck La Jolla Research Center Inc مثبطات أحادي أسيل جليسرول ليباز (magl)
JOP20190106A1 (ar) 2016-11-16 2019-05-09 Lundbeck La Jolla Research Center Inc مثبطات أحادي أسيل جليسرول ليباز (magl)
CN107043355B (zh) * 2017-05-12 2019-08-09 苏州正永生物医药有限公司 一种盐酸依美斯汀中间体化合物及其制备方法
BR112020000863A2 (pt) 2018-05-15 2020-12-08 Lundbeck La Jolla Research Center, Inc. Inibidores de magl
CN115427403A (zh) 2020-04-21 2022-12-02 H.隆德贝克有限公司 单酰基甘油脂肪酶抑制剂的合成

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003093236A1 (en) * 2002-05-02 2003-11-13 Euro-Celtique, S.A. 1-(pyrid-2-yl)-piperazine compounds as metabotropic glutamate receptor inhibitor
SE0201943D0 (sv) * 2002-06-20 2002-06-20 Astrazeneca Ab New use
TW200812986A (en) * 2002-08-09 2008-03-16 Nps Pharma Inc New compounds

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CA2556268A1 (en) 2005-09-01
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AU2005214376A1 (en) 2005-09-01
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