AR075247A1 - Derivados de azaspiranil-alquilcarbamatos de heterociclos de 5 eslabones, su preparacion y su aplicacion en terapeutica - Google Patents

Derivados de azaspiranil-alquilcarbamatos de heterociclos de 5 eslabones, su preparacion y su aplicacion en terapeutica

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Publication number
AR075247A1
AR075247A1 ARP100100315A ARP100100315A AR075247A1 AR 075247 A1 AR075247 A1 AR 075247A1 AR P100100315 A ARP100100315 A AR P100100315A AR P100100315 A ARP100100315 A AR P100100315A AR 075247 A1 AR075247 A1 AR 075247A1
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Argentina
Prior art keywords
group
cycloalkyl
alkyl
cycle
alkylene
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ARP100100315A
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English (en)
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Philippe Yaiche
Nathalie Chereze
Alistair Lochead
Mourad Saady
Ahmed Abouabdellah
Julien Vache
Aude Fayol
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Sanofi Aventis
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Publication of AR075247A1 publication Critical patent/AR075247A1/es

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    • 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
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/438The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P13/00Drugs for disorders of the urinary system
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
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    • A61P25/20Hypnotics; Sedatives
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    • 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
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
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    • A61P35/00Antineoplastic agents
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    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00Drugs for disorders of the cardiovascular system
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    • A61P9/00Drugs for disorders of the cardiovascular system
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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Psychiatry (AREA)
  • Otolaryngology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Composicion farmacéutica, proceso de preparacion y uso como inhibidores de la enzima FAAH. Reivindicacion 1: Compuesto que responde a la formula (1) en la que R2 representa un átomo de hidrogeno, de fluor o un grupo hidroxilo, ciano, trifluorometilo, alquilo C1-6, alcoxi C1-6, NR8R9; rn, n, o y p representan, independientemente entre sí, un numero entero igual a 0, 1, 2 o 3; A representa un enlace covalente o un grupo alquileno C1-8; R1 representa un grupo R5 opcionalmente sustituido por uno o varios grupos R6 y/o R7; R5 representa un grupo elegido entre un fenilo, piridinilo, piridazinilo, pirimidinilo, pirazinilo, triazinilo, naftalenilo, quinolinilo, isoquinolinilo, ftalazinilo, quinazolinilo, quinoxalinilo, cinolinilo, naftiridinilo; R6 representa un átomo de halogeno, un grupo ciano, -CH2CN, nitro, hidroxilo, alquilo C1-6, alcoxi C1-6, tioalquilo C1-6, haloalquilo C1-6, haloalcoxi C1-6, halotioalquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquileno C1-3, cicloalquil C3-7-alquilen C1-3-O-, NR8R9, NR8COR9, NR8CO2R9, NR8SO2R9, NR8SO2NR8R9, COR8, CO2R8, CONR8R9, SO2R8, SO2NR8R9 u -O-alquilen C1-3-O-; R7 representa un grupo elegido entre un: furanilo, pirrolilo, tienilo, oxazolilo, isoxazolilo, tiazolilo, isotiazolilo, imidazolilo, pirazolilo, oxadiazol, tiadiazol, fenilo, piridinilo, piridazinilo, pirimidinilo, pirazinilo, triazina, naftalenilo, quinolinilo, isoquinolinilo, ftalazinilo, quinazolinilo, quinoxalinilo, cinnolinilo, naftiridinilo, imidazopirimidinilo, tienopirimidinilo, benzofuranilo, benzotienilo, bencimidazolilo, benzoxazolilo, bencisoxazolilo, benzotiazolilo, bencisotiazolilo, indolilo, isoindolilo, indazolilo, pirrolopiridinilo, furopiridinilo, tienopiridinilo, imidazopiridinilo, pirazolopiridinilo, oxazolopiridinilo, isoxazolopiridinilo, tiazolopiridinilo, feniloxi, benciloxi, pirimidinoxi; pudiendo estar el o los grupos R7 sustituidos por uno o varios grupos R6 idénticos o diferentes entre sí; R3 representa un átomo de hidrogeno, de fluor, un grupo alquilo C1-6 o un grupo trifluorometilo; R4 representa un grupo elegido entre un: furanilo, pirrolilo, tienilo, tiazolilo, isotiazolilo, oxazolilo, isoxazolilo, pirazolilo, oxadiazolilo, tiadiazolilo, imidazolilo, triazolilo, tetrazolilo; estando este grupo opcionalmente sustituido por uno o varios sustituyentes elegidos entre un átomo de halogeno, un grupo alquilo C1-6, haloalquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquileno C1-3, haloalcoxi C1-6, ciano, NR8R9, NR8COR9, NR8CO2R9, NR8SO2R9, NR8SO2NR8R9, COR8, CO2R8, CONR8R9, CON(R8)alquilen C1-3-NR10R11, SO2R8, SO2NR8R9 u -O-alquilen C1-3-O-; fenilo, feniloxi, benciloxi, piridinilo, pirazinilo, piridazinilo, triazinilo o pirimidinilo; pudiendo estar los grupos fenilo, feniloxi, benciloxi, piridinilo, pirazinilo, piridazinilo, triazinilo y pirimidinilo sustituidos por uno o varios sustituyentes elegidos entre un átomo de halogeno, un grupo ciano, nitro, alquilo C1-6, alcoxi C1-6, tioalquilo C1-6, haloalquilo C1-6, haloalcoxi C1-6, halotioalquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquileno C1-3; R8 y R9 representan, independientemente entre sí, un átomo de hidrogeno o un grupo alquilo C1-6, o forman con el o los átomos a los que están unidos, en el caso de NR8R9, un ciclo elegido entre los ciclos: azetidina, pirrolidina, piperidina, morfolina, tiomorfolina, azepina, oxazepina o piperazina, estando este ciclo opcionalmente sustituido por un grupo alquilo C1-6 o bencilo; en el caso de NR8COR9, un ciclo lactama; en el caso de NR8CO2R9, un ciclo oxazolidinona, oxazinona u oxazepinona; en el caso de NR8SO2R9, un ciclo sultame; en el caso de NR8SO2NR8R9, un ciclo dioxido de tiazolidina o dioxido de tiadiazinano; R10 y R11 representan, independientemente entre sí, un átomo de hidrogeno o un grupo alquilo C1-6 en el estado de base o de sal de adicion a un ácido.
ARP100100315A 2009-02-05 2010-02-05 Derivados de azaspiranil-alquilcarbamatos de heterociclos de 5 eslabones, su preparacion y su aplicacion en terapeutica AR075247A1 (es)

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FR0900493A FR2941696B1 (fr) 2009-02-05 2009-02-05 Derives d'azaspiranyl-alkylcarbamates d'heterocycles a 5 chainons, leur preparation et leur application en therapeutique

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US (1) US8889702B2 (es)
EP (1) EP2393809B1 (es)
JP (1) JP5586632B2 (es)
KR (1) KR20110117215A (es)
CN (1) CN102369200B (es)
AR (1) AR075247A1 (es)
AU (1) AU2010212235B2 (es)
BR (1) BRPI1007456A2 (es)
CA (1) CA2751481C (es)
CO (1) CO6362007A2 (es)
EA (1) EA201171000A1 (es)
FR (1) FR2941696B1 (es)
IL (1) IL214390A0 (es)
MA (1) MA33104B1 (es)
MX (1) MX2011008308A (es)
SG (1) SG173557A1 (es)
TN (1) TN2011000331A1 (es)
TW (1) TW201039823A (es)
UY (1) UY32423A (es)
WO (1) WO2010089510A2 (es)

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US8889702B2 (en) 2014-11-18
MA33104B1 (fr) 2012-03-01
EP2393809B1 (fr) 2014-04-30
WO2010089510A3 (fr) 2010-09-30
AU2010212235A1 (en) 2011-08-25
UY32423A (es) 2010-09-30
FR2941696B1 (fr) 2011-04-15
SG173557A1 (en) 2011-09-29
BRPI1007456A2 (pt) 2019-04-16
EP2393809A2 (fr) 2011-12-14
FR2941696A1 (fr) 2010-08-06
KR20110117215A (ko) 2011-10-26
CA2751481C (fr) 2017-05-23
EA201171000A1 (ru) 2012-02-28
CA2751481A1 (fr) 2010-08-12
TW201039823A (en) 2010-11-16
MX2011008308A (es) 2011-11-02
WO2010089510A2 (fr) 2010-08-12
CO6362007A2 (es) 2012-01-20
US20110319381A1 (en) 2011-12-29
CN102369200B (zh) 2015-05-20
CN102369200A (zh) 2012-03-07
AU2010212235B2 (en) 2016-06-09
JP2012516881A (ja) 2012-07-26
JP5586632B2 (ja) 2014-09-10
TN2011000331A1 (fr) 2013-03-27
IL214390A0 (en) 2011-09-27

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