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 metabotropicoInfo
- 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
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- nr5r6
- group
- 6nr5r6
- 6alkyl
- Prior art date
Links
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 title 1
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical class C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 229930195712 glutamate Natural products 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 105
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 30
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 8
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 7
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 7
- 229910052799 carbon Inorganic materials 0.000 abstract 5
- 125000004429 atom Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000001475 halogen functional group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 4
- 229910052757 nitrogen Inorganic materials 0.000 abstract 4
- 229910052760 oxygen Inorganic materials 0.000 abstract 4
- 229910052717 sulfur Inorganic materials 0.000 abstract 4
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 2
- -1 Oalkyl C2-6SO2R5 Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000004885 piperazines Chemical class 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
Classifications
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- 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
- C07D213/60—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
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- 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
- 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
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- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- 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
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- 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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- 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
- C07D213/60—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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- 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
- C07D295/04—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
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- 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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- C—CHEMISTRY; METALLURGY
- 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
- C07D307/52—Radicals substituted by nitrogen atoms not forming part of a nitro radical
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Compounds Containing Sulfur Atoms (AREA)
- Furan Compounds (AREA)
- Pyridine Compounds (AREA)
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.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US54529004P | 2004-02-18 | 2004-02-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR048065A1 true AR048065A1 (es) | 2006-03-29 |
Family
ID=34886128
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050100613A AR048065A1 (es) | 2004-02-18 | 2005-02-18 | Compuestos de piperazina acetilinica y su uso como antagonistas del receptor de glutamato metabotropico |
Country Status (15)
| Country | Link |
|---|---|
| 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) |
| UY (1) | UY28765A1 (es) |
| WO (1) | WO2005080363A1 (es) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY29796A1 (es) | 2005-09-29 | 2007-04-30 | Astrazeneca Ab | Nuevos compuestos para el tratamiento de trastornos neurológicos, psiquiátricos o del dolor |
| US8349852B2 (en) | 2009-01-13 | 2013-01-08 | Novartis Ag | Quinazolinone derivatives useful as vanilloid antagonists |
| AR080056A1 (es) | 2010-02-01 | 2012-03-07 | Novartis Ag | Derivados de ciclohexil-amida como antagonistas de los receptores de crf |
| EP2531510B1 (en) | 2010-02-01 | 2014-07-23 | Novartis AG | Pyrazolo[5,1b]oxazole derivatives as crf-1 receptor antagonists |
| US8835444B2 (en) | 2010-02-02 | 2014-09-16 | Novartis Ag | Cyclohexyl amide derivatives as CRF receptor antagonists |
| US8759382B2 (en) | 2010-09-29 | 2014-06-24 | Teva Pharmaceutical Industries Ltd. | Propargyl-trifluoromethoxy-aminobenzothiazole derivatives, their preparation and use |
| NZ627750A (en) | 2012-01-06 | 2016-11-25 | Abide Therapeutics Inc | Carbamate compounds and of making and using same |
| WO2016149401A2 (en) | 2015-03-18 | 2016-09-22 | Abide Therapeutics, Inc. | Piperazine carbamates and methods of making and using same |
| MX2017014344A (es) | 2015-05-11 | 2018-04-11 | Abide Therapeutics Inc | Metodos para el tratamiento de la inflacion o el dolor neuropatico. |
| WO2017143283A1 (en) | 2016-02-19 | 2017-08-24 | Abide Therapeutics, Inc. | Radiolabeled monoacylglycerol lipase occupancy probe |
| US10899737B2 (en) | 2016-09-19 | 2021-01-26 | Lundbeck La Jolla Research Center, 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 |
| KR20210010475A (ko) | 2018-05-15 | 2021-01-27 | 룬드벡 라 졸라 리서치 센터 인코포레이티드 | Magl 저해제 |
| KR20230004622A (ko) | 2020-04-21 | 2023-01-06 | 하. 룬드벡 아크티에셀스카브 | 모노아실글리세롤 리파제 억제제의 합성 |
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| 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 |
| JP2006506340A (ja) * | 2002-08-09 | 2006-02-23 | アストラゼネカ アクチボラグ | 代謝調節型グルタミン酸受容体5のモジュレーターとしてのオキサジアゾール |
-
2005
- 2005-02-17 RU RU2006128445/04A patent/RU2006128445A/ru not_active Application Discontinuation
- 2005-02-17 CN CNA2005800089014A patent/CN1934097A/zh active Pending
- 2005-02-17 WO PCT/US2005/005201 patent/WO2005080363A1/en not_active Ceased
- 2005-02-17 BR BRPI0507499-1A patent/BRPI0507499A/pt not_active Application Discontinuation
- 2005-02-17 AU AU2005214376A patent/AU2005214376A1/en not_active Abandoned
- 2005-02-17 JP JP2006554232A patent/JP2007523179A/ja active Pending
- 2005-02-17 KR KR1020067015942A patent/KR20070026382A/ko not_active Withdrawn
- 2005-02-17 TW TW094104644A patent/TW200531694A/zh unknown
- 2005-02-17 EP EP05723282A patent/EP1716130A1/en not_active Withdrawn
- 2005-02-17 CA CA002556268A patent/CA2556268A1/en not_active Abandoned
- 2005-02-18 UY UY28765A patent/UY28765A1/es unknown
- 2005-02-18 AR ARP050100613A patent/AR048065A1/es unknown
- 2005-08-17 US US11/060,470 patent/US20060235024A1/en not_active Abandoned
-
2006
- 2006-08-03 IL IL177292A patent/IL177292A0/en unknown
- 2006-08-08 NO NO20063597A patent/NO20063597L/no unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2007523179A (ja) | 2007-08-16 |
| AU2005214376A1 (en) | 2005-09-01 |
| IL177292A0 (en) | 2006-12-10 |
| TW200531694A (en) | 2005-10-01 |
| WO2005080363A1 (en) | 2005-09-01 |
| RU2006128445A (ru) | 2008-03-27 |
| BRPI0507499A (pt) | 2007-07-24 |
| US20060235024A1 (en) | 2006-10-19 |
| UY28765A1 (es) | 2005-06-30 |
| CN1934097A (zh) | 2007-03-21 |
| CA2556268A1 (en) | 2005-09-01 |
| KR20070026382A (ko) | 2007-03-08 |
| EP1716130A1 (en) | 2006-11-02 |
| NO20063597L (no) | 2006-10-10 |
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