AR077301A1 - Derivados de 2-carboxamida-7-piperazinil-benzofurano como antagonistas de 5-ht1a y 5-ht1b - Google Patents

Derivados de 2-carboxamida-7-piperazinil-benzofurano como antagonistas de 5-ht1a y 5-ht1b

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Publication number
AR077301A1
AR077301A1 ARP100102339A ARP100102339A AR077301A1 AR 077301 A1 AR077301 A1 AR 077301A1 AR P100102339 A ARP100102339 A AR P100102339A AR P100102339 A ARP100102339 A AR P100102339A AR 077301 A1 AR077301 A1 AR 077301A1
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AR
Argentina
Prior art keywords
alkyl
heterocyclyl
heteroaryl
halogen
carbocyclyl
Prior art date
Application number
ARP100102339A
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English (en)
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Astrazeneca Ab
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Publication of AR077301A1 publication Critical patent/AR077301A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/82Benzo [b] furans; Hydrogenated benzo [b] furans 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 carbon atoms of the hetero ring
    • C07D307/84Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/82Benzo [b] furans; Hydrogenated benzo [b] furans 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 carbon atoms of the hetero ring
    • C07D307/84Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D307/85Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Medicinal Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Anesthesiology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Composiciones farmacéuticas que contienen dichos compuestos y al uso de dichos compuestos en terapia, por ejemplo, en el tratamiento de trastornos cognitivos. También se proveen intermediarios utiles en su preparacion. Reivindicacion 1: Un compuesto de formula (1), donde R1 es heteroarilo o heterociclilo, donde dicho heteroarilo o heterociclilo está opcionalmente sustituido con uno o más sustituyentes seleccionados entre alquilo C1-4, halogeno, CF3, CN, alcoxi C1-4, C(O)alquilo C1-4, N(alquil C1-4)C(O)-alquilo C1-4, NHC(O)alquilo C1-4, C(O)HN(alquilo C1-4) y C(O)N(alquilo C1-4)2; R2 es alquilo C1-4, heterociclilo, alquilarilo C1-4, alquilheteroarilo C1-4, carbociclilo, alquilheterociclilo C1-4, heterociclil-heteroarilo, aril-heterociclilo, carbociclil-heteroarilo, heterociclil-arilo, donde en dichos grupos el resto heterociclilo, arilo, heteroarilo o carbociclilo puede estar opcionalmente sustituido con uno o más sustituyentes seleccionados entre halogeno, alcoxi C1-4, C(O)alquilo C1-4, alquil C0-4SO2alquilo C1-4, ciano, hidroxi y alquilo C1-4; R3 es hidrogeno o alquilo C1-4, o R2 y R3 junto con el átomo de nitrogeno pueden formar un sistema de anillo saturado que contiene 4, 5 o 6 átomos constituyentes del anillo seleccionados entre carbono y nitrogeno, y donde dicho sistema de anillo está opcionalmente sustituido con uno o más sustituyentes seleccionados entre halogeno, alquilo C1-4 y alcoxi C1-4, O-heteroarilo; R4 es hidrogeno, halogeno, metilo o metoxi, o una sal farmacéuticamente aceptable de este. Reivindicacion 39: Un compuesto de acuerdo con la formula (7) donde R2 es alquilo C1-4, heterociclilo, alquilarilo C1-4, alquilheteroarilo C1-4, carbociclilo, alquilheterociclilo C1-4, heterociclil-heteroarilo, aril-heterociclilo, carbociclil-heteroarilo, heterociclil-arilo, donde en dichos grupos el resto heterociclilo, arilo, heteroarilo o carbociclilo puede estar opcionalmente sustituido con uno o más sustituyentes seleccionados entre halogeno, alcoxi C1-4, C(O)alquilo C1-4, alquil C0-4SO2alquilo C1-4, ciano, hidroxi y alquilo C1-4; R3 es hidrogeno o alquilo C1-4, o R2 y R3 junto con el átomo de nitrogeno pueden formar un sistema de anillo saturado que contiene 4, 5 o 6 átomos constituyentes del anillo seleccionados entre carbono y nitrogeno, y donde dicho sistema de anillo está opcionalmente sustituido con uno o más sustituyentes seleccionados entre halogeno, alquilo C1-4 y alcoxi C1-4, O-heteroarilo; R4 es hidrogeno, halogeno, metilo o metoxi.
ARP100102339A 2009-06-30 2010-06-30 Derivados de 2-carboxamida-7-piperazinil-benzofurano como antagonistas de 5-ht1a y 5-ht1b AR077301A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US22165709P 2009-06-30 2009-06-30

Publications (1)

Publication Number Publication Date
AR077301A1 true AR077301A1 (es) 2011-08-17

Family

ID=43381415

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100102339A AR077301A1 (es) 2009-06-30 2010-06-30 Derivados de 2-carboxamida-7-piperazinil-benzofurano como antagonistas de 5-ht1a y 5-ht1b

Country Status (14)

Country Link
US (2) US8367676B2 (es)
EP (1) EP2448934B1 (es)
JP (1) JP5767211B2 (es)
KR (1) KR20120110000A (es)
CN (1) CN102482264B (es)
AR (1) AR077301A1 (es)
AU (1) AU2010266753B2 (es)
BR (1) BRPI1014222A2 (es)
CA (1) CA2765475A1 (es)
MX (1) MX2011013449A (es)
RU (1) RU2011152516A (es)
TW (1) TW201103922A (es)
UY (1) UY32744A (es)
WO (1) WO2011002405A1 (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8367676B2 (en) 2009-06-30 2013-02-05 Astrazeneca Ab 2-carboxamide-7-piperazinyl-benzofuran derivatives 774
WO2012087229A1 (en) 2010-12-20 2012-06-28 Astrazeneca Ab 2-carboxamide-4-piperazinyl-benzofuran derivative
CN102993186B (zh) * 2012-12-20 2015-11-18 北京海步国际医药科技发展有限公司 一种新型的哌嗪衍生物
EP2964654A4 (en) * 2013-03-07 2016-08-10 Glaxosmithkline Llc THIEN [3,2-D] PYRIMIDIN-6-CARBOXAMIDE AND ANALOGUE AS SIRTUIN MODULATORS
WO2020183011A1 (en) 2019-03-14 2020-09-17 Institut Curie Htr1d inhibitors and uses thereof in the treatment of cancer
US20230312577A1 (en) * 2020-06-05 2023-10-05 Monash University Dual kinase-bromodomain inhibitors
CN117430574B (zh) * 2023-12-20 2024-03-22 潍坊医学院 一种苯并呋喃衍生物及其制备方法、用途

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AR022303A1 (es) 1999-01-22 2002-09-04 Lundbeck & Co As H Derivados de piperidina, tetrahidropiridina y piperazina, su preparacion y utilizacion
BR0210411A (pt) 2001-06-15 2004-08-17 Hoffmann La Roche Derivados 4-piperazinilindol com afinidade para o receptor 5-ht6
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Also Published As

Publication number Publication date
US20130296296A1 (en) 2013-11-07
CA2765475A1 (en) 2011-01-06
AU2010266753A1 (en) 2012-01-19
BRPI1014222A2 (pt) 2017-05-16
JP5767211B2 (ja) 2015-08-19
US20100331341A1 (en) 2010-12-30
KR20120110000A (ko) 2012-10-09
UY32744A (es) 2011-01-31
AU2010266753B2 (en) 2013-08-08
US8367676B2 (en) 2013-02-05
EP2448934A4 (en) 2012-12-05
JP2012532125A (ja) 2012-12-13
EP2448934A1 (en) 2012-05-09
TW201103922A (en) 2011-02-01
US8859534B2 (en) 2014-10-14
CN102482264B (zh) 2015-10-07
CN102482264A (zh) 2012-05-30
WO2011002405A1 (en) 2011-01-06
RU2011152516A (ru) 2013-08-10
EP2448934B1 (en) 2014-05-21
MX2011013449A (es) 2012-02-13

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