AR047812A1 - Compuestos de tetrazol y su uso como antagonistas del receptor de glutamato metabotropico - Google Patents

Compuestos de tetrazol y su uso como antagonistas del receptor de glutamato metabotropico

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Publication number
AR047812A1
AR047812A1 ARP050100615A ARP050100615A AR047812A1 AR 047812 A1 AR047812 A1 AR 047812A1 AR P050100615 A ARP050100615 A AR P050100615A AR P050100615 A ARP050100615 A AR P050100615A AR 047812 A1 AR047812 A1 AR 047812A1
Authority
AR
Argentina
Prior art keywords
6alkyl
4alkyl
nr5r6
ring
6alkylnr5
Prior art date
Application number
ARP050100615A
Other languages
English (en)
Original Assignee
Nps Pharma Inc
Astrazeneca Ab
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.)
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34886129&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR047812(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Nps Pharma Inc, Astrazeneca Ab filed Critical Nps Pharma Inc
Publication of AR047812A1 publication Critical patent/AR047812A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04—Five-membered rings
    • 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
    • A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • 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
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • 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
    • C07D403/06—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Procesos para su preparacion, composiciones farmacéuticas que contienen dichos compuestos y el uso terapéutico de los mismos. Reivindicacion 1: Un compuesto caracterizado porque responde a la formula (1), en donde: X3 y X4 se seleccionan entre N y C, de modo que cuando X3 es N, X4 es C y cuando X3 es C, X4 es N; P se selecciona entre arilo y heteroarilo; si m = 1 entonces R1 se une a P a través de un átomo de carbono en el anillo P en una meta-posicion del anillo P respecto del punto de union de P a X3, y si m = 2 entonces R1 se une a P vía carbon átomos en el anillo P en las posiciones 2 y 5 del anillo P; R1 se selecciona entre el grupo formado por hidroxi, halo, nitro, C1-6 alquilhalo, OC1-6alquilhalo, C1-6 alquilo, OC1-6alquilo, C2-6 alquenilo, OC2-6alquenilo, C2-6 alquinilo, OC2-6alquinilo, C0-6alquilC3-6cicloalquilo, OC0-6alquilC3-6cicloalquilo, C0-6 alquilarilo, OC0-6alquilarilo, CHO, (CO)R5, O(CO)R5, O(CO)OR5, O(CNR5)OR5, C1-6alquilOR5, OC2-6alquilOR5, C1-6alquil(CO)R5, OC1- 6alquil(CO)R5, C0-6alquilCO2R5, OC1-6alquilCO2R5, C0-6 alquilciano, OC2-6alquilciano, C0-6alquilNR5R6, OC2-6alquilNR5R6, C1-6alquil(CO)NR5R6, OC1-6alquil(CO)NR5R6, C0-6alquilNR5(CO)R6, OC2-6alquilNR5(CO)R6, C0-6alquilNR5(CO)NR5R6, C0-6alquilSR5, OC2- 6alquilSR5, C0-6alquil(SO)R5, OC2-6alquil(SO)R5, C0-6alquilSO2R5, OC2-6alquilSO2R5, C0-6alquil(SO2)NR5R6, OC2-6alquil(SO2)NR5R6, C0-6alquilNR5(SO2)R6, OC2-6alquilNR5(SO2)R6, C0-6alquilNR5(SO2)NR5R6, OC2-6alquilNR5(SO2)NR5R6, (CO)NR5R6, O(CO)NR5R6, NR5OR6, C0-6alquilNR5(CO)OR6, OC2-6alquilNR5(CO)OR6, SO3R5 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; X1 se seleccionan entre el grupo formado por C2-3 alquilo, C2-3 alquenilo, NR3, O, S, CR3R4, SO, SO2; X2 se seleccionan entre el grupo formado por un enlace CR3R4, O, S, NR3, SO, SO2; R3 y R4 se seleccionan en forma independiente entre un grupo formado por hidrogeno, hidroxi, C-6 alquilo, C0-6 alquilciano, oxo, =NR5, =NOR5, C1-4 alquilhalo, halo, C1-4alquilC3-7cicloalquilo, C3-7 cicloalquilo, O(CO)C1-4alquilo, (CO)C1-4alquilo, C1-4alquil(SO)C0-4alquilo, C1-4alquil(SO2)C0-4alquilo, (SO)C0-4alquilo, (SO2)C0-4alquilo, OC1-4alquilo, C1- 4alquilOR5 y C0-4alquilNR5R6; Q es ya sea seleccionado entre triazol, piperazina, y imidazol, o bien Q es cualquier otro anillo heterocíclico de 4,5, 6 o 7 miembros que contienen uno o más heteroátomos seleccionados entre N, O y S y está fusionado a un anillo y triazol; R2 se selecciona entre el grupo formado por hidroxi, C0-6 alquilciano, =NR5, =O, =NOR5, C1-4 alquilhalo, halo, C1-6 alquilo, C3-6 cicloalquilo, C0-6 alquilarilo, C0-6 alquilheteroarilo, C0-6 alquilcicloalquilo, C0-6 alquilheterocicloalquilo, OC1-4alquilo, OC0-6alquilarilo, O(CO)C1-4alquilo, (CO)OC1-4alquilo, C0-4alquil(S)C0-4alquilo, C1-4alquil(SO)C0-4alquilo, C1-4alquil(SO2)C0-4alquilo, (SO)C0-4alquilo, (SO2)C0-4alquilo, C1-4alquilOR5, C0-4alquilNR5R6 y un anillo de 5 o 6 miembros que contiene uno o más átomos seleccionados en forma independiente entre C, N, O y S, y dicho anillo opcionalmente puede fusionarse con un anillo de 5 o 6 miembros que contiene uno o más átomos seleccionados en forma independiente entre el grupo formado por C, N y O y en donde dicho anillo y dicho anillo fusionado pueden sustituirse con uno o más A; y cualquier C1-6 alquilo, arilo o heteroarilo definido bajo R1, R2 y R3 puede sustituirse con uno o más A; y A se selecciona entre el grupo formado por hidrogeno, hidroxi, halo, nitro, oxo, C0-6 alquilciano, C0-4alquilC3-6cicloalquilo, C1-6 alquilo, -OC1-6alquilo, C1-6 alquilhalo, OC1-6alquilhalo, C2-6 alquenilo, C0-3 alquilarilo, C0-6alquilOR5, OC2-6alquilOR5, C1-6alquilSR5, OC2-6alquilSR5, (CO)R5, O(CO)R5, OC2-6alquilciano, OC1-6alquilCO2R5, O(CO)OR5, OC1-6alquil(CO)R5, C1-6alquil(CO)R5, NR5OR6, C0-6NR5R6, OC2-6alquilNR5R6, C0-6alquil(CO)NR5R6, OC1-6alquil(CO)NR5R6, OC2-6alquilNR5(CO)R6, C0- 6alquilNR5(CO)R6, C0-6alquilNR5(CO)NR5R6, O(CO)NR5R6, C0-6alquil(SO2)NR5R6, OC2-6alquil(SO2)NR5R6, C0-6alquilNR5(SO2)R6, OC2-6alquilNR5(SO2)R6, SO3R5, C1-6alquilNR5(SO2)NR5R6, OC2-6alquil(SO2)R5, C0-6alquil(SO2)R5, C0-6alquil(SO)R5, OC2- 6alquil(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; R5 y R6 se seleccionan en forma independiente entre H, C1-6 alquilo, C3-7 cicloalquilo y arilo; y sus sales e hidratos; m se selecciona entre 1 o 2; p se selecciona entre 0, 1, 2, 3 y 4, o una sal o hidrato del mismo; con la salvedad de que el compuesto no sea: 1-(2-benzotiazolil)-4-[[5-(5-metil-2-furanil)-2H-tetrazol-2-il]acetil-piperazina; 1- (4-acetilfenil)-4-[[5-(5-metil-2-furanil)-2H-tetrazol-2-il]acetil]-piperazina; o 5-(5-metil-2-furanil)-N-(2-fenil-2H-benzotriazol-5-il)-2H-tetrazol-2-acetamida.
ARP050100615A 2004-02-18 2005-02-18 Compuestos de tetrazol y su uso como antagonistas del receptor de glutamato metabotropico AR047812A1 (es)

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US (2) US20070197549A1 (es)
EP (1) EP1716125B1 (es)
JP (1) JP5084269B2 (es)
KR (1) KR20070027504A (es)
CN (2) CN1918137B (es)
AR (1) AR047812A1 (es)
AU (1) AU2005214379B2 (es)
BR (1) BRPI0507498A (es)
CA (1) CA2556263A1 (es)
IL (1) IL177056A0 (es)
MX (1) MXPA06009019A (es)
MY (1) MY145075A (es)
NO (1) NO20063470L (es)
RU (1) RU2372347C2 (es)
SG (1) SG150539A1 (es)
TW (1) TW200533664A (es)
UA (1) UA85576C2 (es)
UY (1) UY28763A1 (es)
WO (1) WO2005080356A1 (es)
ZA (1) ZA200606594B (es)

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