AR065393A1 - Derivados de indol como agonistas del receptor de canabinoides cb1, y su uso en el tratamiento del dolor - Google Patents

Derivados de indol como agonistas del receptor de canabinoides cb1, y su uso en el tratamiento del dolor

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Publication number
AR065393A1
AR065393A1 ARP080100681A ARP080100681A AR065393A1 AR 065393 A1 AR065393 A1 AR 065393A1 AR P080100681 A ARP080100681 A AR P080100681A AR P080100681 A ARP080100681 A AR P080100681A AR 065393 A1 AR065393 A1 AR 065393A1
Authority
AR
Argentina
Prior art keywords
alkyl
pain
hydrogen
optionally substituted
treatment
Prior art date
Application number
ARP080100681A
Other languages
English (en)
Inventor
Julia Adam
Original Assignee
Organon Nv
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.)
Filing date
Publication date
Application filed by Organon Nv filed Critical Organon Nv
Publication of AR065393A1 publication Critical patent/AR065393A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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
    • C07D417/02—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 two hetero rings
    • C07D417/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245—Oxadiazoles
    • 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
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory 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
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond

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

Abstract

Se refiere a un derivado de indol que tiene la formula general I donde A representa un anillo heterocíclico aromático de 5 miembros, donde X1, X2 y X3 son seleccionados independientemente entre N, O, S y CH; Y representa CH2, O, S o SO2; R1 es H,(Cl-4)alquilo, (C1-4)alquiloxi CN o halogeno; R2, R2', R3, R3', R4, R4', R5 y R5' son independientemente hidrogeno, (C1-4)alquilo (opcionalmente sustituido con OH) o CO-ORg; o un par de sustituyentes geminales R3 y R3', o R5 y R5'representan juntosun grupo ceto, y los otros son todos hidrogeno o (C1-4)alquilo; o R2 y R5 representan juntos un puente de metileno o de etileno, y R2', R3, R3', R4, R4' y R5' son hidrogeno; n es 1 o 2; R6 es H, (C1-4) alquilo (opcionalmente sustituido con OH), (C1-4)alquiloxi, CO-NR9R10, CO-OR11 o 1,2,4-oxadiazol-3-ilo), SO2NR12R13 o COOR14; R7 es H o halogeno; R8 es (C1-4)alquilo; R9 y R10 son independientemente hidrogeno, (C1-4)alquilo o (C3-7)cicloalquilo, estando los grupos alquilo opcionalmentesustituidos con OH o (C1-4)alquilo; R11 es H o (C1-4)alquilo; R12 y R13 son independientemente H o (C1-4)alquilo; R14 es (C1-6)alquilo; o una sal farmacéuticamente aceptable del mismo, como agonista del receptor de canabinoides CB1, que puede usarseen el tratamiento del dolor, por ejemplo dolor perioperatorio, dolor cronico, dolor neuropático, dolor de cáncer y dolor y espasticidad asociados con la esclerosis multiple.
ARP080100681A 2007-02-22 2008-02-20 Derivados de indol como agonistas del receptor de canabinoides cb1, y su uso en el tratamiento del dolor AR065393A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP07102870 2007-02-22

Publications (1)

Publication Number Publication Date
AR065393A1 true AR065393A1 (es) 2009-06-03

Family

ID=38283196

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP080100681A AR065393A1 (es) 2007-02-22 2008-02-20 Derivados de indol como agonistas del receptor de canabinoides cb1, y su uso en el tratamiento del dolor

Country Status (18)

Country Link
US (1) US7655645B2 (es)
EP (1) EP2125795B1 (es)
JP (1) JP5324476B2 (es)
KR (1) KR20090113383A (es)
CN (1) CN101616914B (es)
AR (1) AR065393A1 (es)
AU (1) AU2008219226B2 (es)
BR (1) BRPI0807867A2 (es)
CA (1) CA2678147A1 (es)
CL (1) CL2008000514A1 (es)
EC (1) ECSP099593A (es)
IL (1) IL199848A0 (es)
MX (1) MX2009008316A (es)
PE (1) PE20090112A1 (es)
RU (1) RU2009135255A (es)
TW (1) TW200848417A (es)
WO (1) WO2008101995A1 (es)
ZA (1) ZA200905265B (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI330635B (en) 2004-03-05 2010-09-21 Organon Nv (indol-3-yl)-heterocycle derivatives
US7763732B2 (en) * 2005-08-24 2010-07-27 N.V. Organon Indole derivatives
TW200848417A (en) 2007-02-22 2008-12-16 Organon Nv Indole derivatives
AR073701A1 (es) * 2008-09-29 2010-11-24 Abbott Lab Derivados de indol y de indolicina, metodos para su preparacion, una composicion farmaceutica que los comprende y su uso en el tratamiento de enfermedades neurodegenerativas.
US9332757B2 (en) 2010-10-25 2016-05-10 Vanderbilt University Composition for inhibition of insect host sensing
EP3653054A1 (en) 2011-05-06 2020-05-20 Vanderbilt University Composition for inhibition of insect sensing
CN102757427A (zh) * 2012-07-09 2012-10-31 陕西科技大学 2-氨基-5-异二氢吲哚-1,3-二酮甲基1,3,4-噻二唑及其制备方法
EP3273779A4 (en) 2015-03-25 2018-09-05 Vanderbilt University Binary compositions as disruptors of orco-mediated odorant sensing

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4939138A (en) * 1988-12-29 1990-07-03 Sterling Drug Inc. 2- and 3-aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo(1,2,3-DE)-1,4-benzoxazines
TWI283577B (en) * 1999-10-11 2007-07-11 Sod Conseils Rech Applic Pharmaceutical composition of imidazole derivatives acting as modulators of sodium channels and the use thereof
WO2001058869A2 (en) 2000-02-11 2001-08-16 Bristol-Myers Squibb Company Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators in treating respiratory and non-respiratory diseases
AUPR118000A0 (en) 2000-11-02 2000-11-23 Amrad Operations Pty. Limited Therapeutic molecules and methods
DE60237431D1 (de) 2001-01-29 2010-10-07 Univ Connecticut Rezeptor-selektive cannabimimetische aminoalkylindole
TWI248438B (en) * 2001-04-10 2006-02-01 Sod Conseils Rech Applic Derivatives of heterocycles with 5 members, their preparation and their use as medicaments
TW200402417A (en) 2002-06-21 2004-02-16 Akzo Nobel Nv 1-[(Indol-3-yl)carbonyl]piperazine derivatives
CA2549147C (en) 2003-12-17 2012-04-10 Akzo Nobel N.V. Tricyclic 1-((3-indol-3-yl)carbonyl) piperazine derivatives as cannabinoid cb1 receptor agonists
TWI330635B (en) * 2004-03-05 2010-09-21 Organon Nv (indol-3-yl)-heterocycle derivatives
US20090029984A1 (en) * 2005-07-11 2009-01-29 N.V. Organon Synergistic combination for the treatment of pain (cannabinoid receptor agonist and opioid receptor agonist)
TW200745096A (en) 2005-08-23 2007-12-16 Organon Nv Indole derivatives
US7763732B2 (en) * 2005-08-24 2010-07-27 N.V. Organon Indole derivatives
TW200848417A (en) 2007-02-22 2008-12-16 Organon Nv Indole derivatives

Also Published As

Publication number Publication date
CN101616914B (zh) 2012-10-10
EP2125795A1 (en) 2009-12-02
RU2009135255A (ru) 2011-03-27
ECSP099593A (es) 2009-09-29
CL2008000514A1 (es) 2008-06-20
WO2008101995A1 (en) 2008-08-28
TW200848417A (en) 2008-12-16
MX2009008316A (es) 2009-08-12
AU2008219226A1 (en) 2008-08-28
US7655645B2 (en) 2010-02-02
CA2678147A1 (en) 2008-08-28
JP2010519278A (ja) 2010-06-03
JP5324476B2 (ja) 2013-10-23
PE20090112A1 (es) 2009-02-26
IL199848A0 (en) 2010-04-15
US20080207598A1 (en) 2008-08-28
EP2125795B1 (en) 2013-03-20
AU2008219226B2 (en) 2013-02-07
BRPI0807867A2 (pt) 2014-06-03
KR20090113383A (ko) 2009-10-30
CN101616914A (zh) 2009-12-30
ZA200905265B (en) 2010-04-28

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