AR036086A1 - Compuestos de {[ 2- morfonil-4-il]-2-oxoetil}-(2-oxopirrolidinil 3-il)naftalen-2-sulfonamida, composiciones farmaceuticas formuladas con dichos compuestos; uso de dichos compuestos en la manufactura de medicamentos para el tratamiento de condiciones susceptibles de mejoramiento mediante la inhibicio - Google Patents

Compuestos de {[ 2- morfonil-4-il]-2-oxoetil}-(2-oxopirrolidinil 3-il)naftalen-2-sulfonamida, composiciones farmaceuticas formuladas con dichos compuestos; uso de dichos compuestos en la manufactura de medicamentos para el tratamiento de condiciones susceptibles de mejoramiento mediante la inhibicio

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Publication number
AR036086A1
AR036086A1 ARP020102128A ARP020102128A AR036086A1 AR 036086 A1 AR036086 A1 AR 036086A1 AR P020102128 A ARP020102128 A AR P020102128A AR P020102128 A ARP020102128 A AR P020102128A AR 036086 A1 AR036086 A1 AR 036086A1
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AR
Argentina
Prior art keywords
alkyl
compounds
group
3alkyl
phenyl
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ARP020102128A
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English (en)
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Glaxo Group Ltd
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Publication of AR036086A1 publication Critical patent/AR036086A1/es

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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
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory 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
    • A61P25/28Drugs 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D207/12Oxygen or sulfur atoms
    • 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
    • C07D413/02Heterocyclic 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
    • C07D413/06Heterocyclic 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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Se describen y reivindican compuestos que posee propiedades inhibitorias del factor Xa de fórmula (1) donde R1 representa hidrógeno, -alquilo C1-6, alquenilo C3-6, -(alquil C2-3)NRbRc, -(alquil C2-3)NHCORb, fenilo o un grupo heterocíclico aromático de 5 o 6 miembros, estando el fenilo o el grupo heterocíclico aromático de 5 o 6 miembros opcionalmente sustituidos con halógeno, o R1 representa un grupo X-W, en el que X representa alquileno C1-3 y W representa -CN, -CO2H, -CONRbRc, -COalquilo C1-6, -CO2alquilo C1-6, fenilo o un grupo heterocíclico aromático o no aromático de 5 o 6 miembros que contiene al menos un heteroátomo seleccionado entre O, N o S, estando el fenilo o el grupo heterocíclico aromático opcionalmente sustituido con uno o más sustituyentes seleccionados entre: alquilo C1-3, -alcoxi C1-3, (alquil C1-3)OH, halógeno, -CN, -CF3, NH2, -CO2H y -OH; R2 y R3 representan independientemente hidrógeno, -alquilo C1-3 o -CF3 con la condición de que uno de R2 y R3 es alquilo- C1-3 o CF3 y el otro es hidrógeno; Rb y Rc representan independientemente hidrógeno o -alquilo C1-3; A representa un grupo seleccionado entre: el grupo de fórmulas (2); Z representa uno o dos sustituyentes opcionales seleccionados independientemente entre halógeno y OH, W representa un sustituyente opcional -alquilo C1-3, Alq representa alquileno C2-3 o alquenileno C2-3, T representa un heteroátomo seleccionado entre O, N o S; B representa uno o más sustituyentes opcionales sobre los átomos de carbono del anillo seleccionados entre (1) uno o más sustituyentes seleccionados entre -CF3, -F, -CO2H, -alquilo C1-6, -(alquil C1-6)OH, -(alquil C1-3)NRbRc y -(alquil C0-3)CONRbRc y -(alquil C0-3) CO2alquiloC1-3, -CONH(alquil C2-3)OH, -CH2NH(alquil C2-3)OH, -CH2Oalquilo C1-3 y -CH2SO2alquilo C1-3; (2) un grupo -Y -Re, Y representa -alquileno C1-3-, -CO-, -(alquil C1-3)NH-, -(alquil C1-3)NHCO-, -(alquil C1-3)NHSO2-, -CH2NHSO2CH2- o un enlace directo, Re representa fenilo, un cicloalquilo de 5 a 6i miembros o un heterociclo de 5 o 6 miembros que contiene al menos un heteroátomo seleccionado entre O, N o S, cada uno de los cuales está opcionalmente sustituido con uno o más sustituyentes seleccionados entre: -alquilo C1-3, -alcoxi C1-3, -(alquil C1-3)OH, halógeno, -CN, CF3, -NH2, -CO2H y -OH, o (3) un segundo anillo R1 que está condensado con el anillo heterocíclico en el que R1 representa fenilo, un grupo cicloalquilo de 5 o 6 miembros o un grupo heterocíclico aromático de 5 o 6 miembros que contiene al menos un heteroátomo seleccionado entre O, N o S, y el grupo bicíclico condensado está opcionalmente sustituido con uno o más sustituyentes seleccionados entre: -alquilo C1-3, -alcoxi C1-3, -(alquil C1-3)OH, halógeno, -CN, -CF3, -NH2, -CO2H y -OH, y sus derivados farmacéuticamente aceptables. Se describen y reivindican los objetos restantes mencionados en el título.
ARP020102128A 2001-06-08 2002-06-06 Compuestos de {[ 2- morfonil-4-il]-2-oxoetil}-(2-oxopirrolidinil 3-il)naftalen-2-sulfonamida, composiciones farmaceuticas formuladas con dichos compuestos; uso de dichos compuestos en la manufactura de medicamentos para el tratamiento de condiciones susceptibles de mejoramiento mediante la inhibicio AR036086A1 (es)

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Application Number Priority Date Filing Date Title
GBGB0114005.2A GB0114005D0 (en) 2001-06-08 2001-06-08 Chemical compounds

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Publication Number Publication Date
AR036086A1 true AR036086A1 (es) 2004-08-11

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ARP020102128A AR036086A1 (es) 2001-06-08 2002-06-06 Compuestos de {[ 2- morfonil-4-il]-2-oxoetil}-(2-oxopirrolidinil 3-il)naftalen-2-sulfonamida, composiciones farmaceuticas formuladas con dichos compuestos; uso de dichos compuestos en la manufactura de medicamentos para el tratamiento de condiciones susceptibles de mejoramiento mediante la inhibicio

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Country Link
US (4) US7186717B2 (es)
EP (1) EP1395553B1 (es)
JP (1) JP4242274B2 (es)
KR (1) KR100877245B1 (es)
CN (1) CN1256324C (es)
AR (1) AR036086A1 (es)
AT (1) ATE289294T1 (es)
AU (1) AU2002311451B2 (es)
BR (1) BR0210207A (es)
CA (1) CA2449629A1 (es)
CO (1) CO5540285A2 (es)
CZ (1) CZ20033325A3 (es)
DE (1) DE60203006T2 (es)
DK (1) DK1395553T3 (es)
ES (1) ES2235050T3 (es)
GB (1) GB0114005D0 (es)
HK (1) HK1063471A1 (es)
HU (1) HUP0400156A3 (es)
IL (1) IL159195A0 (es)
MX (1) MXPA03011384A (es)
MY (1) MY136859A (es)
NO (1) NO326689B1 (es)
NZ (1) NZ530004A (es)
PL (1) PL368082A1 (es)
PT (1) PT1395553E (es)
SI (1) SI1395553T1 (es)
TW (1) TWI298719B (es)
WO (1) WO2002100830A1 (es)
ZA (1) ZA200309367B (es)

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GB0114005D0 (en) * 2001-06-08 2001-08-01 Glaxo Group Ltd Chemical compounds
GB0130705D0 (en) * 2001-12-21 2002-02-06 Glaxo Group Ltd Chemical compounds
GB0228533D0 (en) 2002-12-06 2003-01-15 Glaxo Group Ltd Crystalline form
GB0228552D0 (en) * 2002-12-06 2003-01-15 Glaxo Group Ltd Chemical compounds
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AU2005336535B2 (en) * 2005-09-22 2012-05-24 Trobio Ab Stabilized protease composition
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CN105143213B (zh) * 2013-04-26 2018-07-24 赛诺菲 5-氯-噻吩-2-甲酸[(s)-2-[甲基-3-(2-氧代-吡咯烷-1-基)-苯磺酰基氨基]-3-(4-甲基-哌嗪-1-基)-3-氧代-丙基]酰胺的酒石酸盐
DE102014108210A1 (de) 2014-06-11 2015-12-17 Dietrich Gulba Rodentizid
EP3078378B1 (en) 2015-04-08 2020-06-24 Vaiomer Use of factor xa inhibitors for regulating glycemia
EP4070658A1 (de) 2021-04-06 2022-10-12 BIORoxx GmbH Verwendung von blutgerinnungshemmenden verbindungen als rodentizide

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GB0228533D0 (en) * 2002-12-06 2003-01-15 Glaxo Group Ltd Crystalline form

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IL159195A0 (en) 2004-06-01
US7429587B2 (en) 2008-09-30
MXPA03011384A (es) 2004-04-05
DK1395553T3 (da) 2005-06-06
EP1395553B1 (en) 2005-02-16
US20070142375A1 (en) 2007-06-21
CZ20033325A3 (cs) 2004-08-18
AU2002311451B2 (en) 2006-03-02
PL368082A1 (en) 2005-03-21
CA2449629A1 (en) 2002-12-19
MY136859A (en) 2008-11-28
CO5540285A2 (es) 2005-07-29
NZ530004A (en) 2005-08-26
HK1063471A1 (en) 2004-12-31
US20070142374A1 (en) 2007-06-21
US20050107379A1 (en) 2005-05-19
DE60203006D1 (de) 2005-03-24
BR0210207A (pt) 2004-08-03
GB0114005D0 (en) 2001-08-01
JP4242274B2 (ja) 2009-03-25
HUP0400156A2 (hu) 2004-07-28
KR20040004706A (ko) 2004-01-13
DE60203006T2 (de) 2006-03-30
US7517879B2 (en) 2009-04-14
EP1395553A1 (en) 2004-03-10
NO20035440D0 (no) 2003-12-05
JP2004537530A (ja) 2004-12-16
CN1538955A (zh) 2004-10-20
US7186717B2 (en) 2007-03-06
PT1395553E (pt) 2005-06-30
CN1256324C (zh) 2006-05-17
KR100877245B1 (ko) 2009-01-07
TWI298719B (en) 2008-07-11
ZA200309367B (en) 2004-08-02
HUP0400156A3 (en) 2008-10-28
ATE289294T1 (de) 2005-03-15
SI1395553T1 (en) 2005-06-30
US20070155745A1 (en) 2007-07-05
ES2235050T3 (es) 2005-07-01
WO2002100830A1 (en) 2002-12-19
NO326689B1 (no) 2009-01-26
US7326785B2 (en) 2008-02-05

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