AR050945A1 - Medicamentos que contienen compuestos de carbonilo y su uso - Google Patents

Medicamentos que contienen compuestos de carbonilo y su uso

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Publication number
AR050945A1
AR050945A1 ARP050103944A ARP050103944A AR050945A1 AR 050945 A1 AR050945 A1 AR 050945A1 AR P050103944 A ARP050103944 A AR P050103944A AR P050103944 A ARP050103944 A AR P050103944A AR 050945 A1 AR050945 A1 AR 050945A1
Authority
AR
Argentina
Prior art keywords
mono
atoms
hal
coor3
het
Prior art date
Application number
ARP050103944A
Other languages
English (en)
Inventor
Dieter Dorsch
Werner Mederski
Christos Tsaklakidis
Johannes Gleitz
Bertram Cezanne
Original Assignee
Merck Patent Gmbh
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Filing date
Publication date
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR050945A1 publication Critical patent/AR050945A1/es

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    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic 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
    • A61K31/5355Non-condensed oxazines and containing further heterocyclic 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
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

Landscapes

  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Uso de compuesto de la formula (1), en la que: R1, R2 son cada uno, de modo independiente entre sí, H, =O, Hal, A, etinilo, OR3, N(R3)2, NO2, CN, N3, COOR3, CON(R3)2, -[C(R4)2]n-Ar, -[C(R4)2]n-Het, -[C(R4)2]n-cicloalquilo, -OCOR3, -OCON(R3)2, NR3COA o NR3SO2A; R1 y R2 también son juntos un carbociclo o heterociclo de 3 a 7 miembros unidos de forma bicíclica o espirocíclica con 0 a 3 átomos de N, O y/o S; R3 es H, A, H-C:::C-CH2-, CH3-C:::C-CH2-, -CH2-CH(OH)-CH2OH, -CH2-CH(OH)-CH2NH2, -CH2- CH(OH)-CH2Het', -[C(R4)2]n-Ar', -[C(R4)2]n-Het', -[C(R4)2]n-cicloalquilo, -[C(R4)2]n-COOA o -[C(R4)2]nN(R4)2; R4 es H o A; W es N, CR3 o un átomo de C sp2 hibridado; E es junto con W un anillo carbocíclico o heterocíclico saturado de 3 a 7 miembros con 0 a 3 átomo de N, 0 a 2 átomo de O y/o 0 a 2 átomos de S, que puede contener un enlace doble; D es un carbociclo o heterociclo aromático mono- o bicíclico no sustituido o mono- o polisustituido con Hal, A, OR3, N(R3)2, NO2, CN, COOR3 o CON(R3)2, con 0 a 4 átomos de N, O y/o S; G es -[C(R4)2]n-, -[C(R4)2]nNR3, -[C(R4)2]nO-, -[C(R4)2]nS- o -[C(R4)=C(R4)]n-; X es -[C(R4)2]nCONR3[C(R4)2]n-, -[C(R4)2]nNR3CO[C(R4)2]n-; -[C(R4)2]nNR3[C(R4)2]n-, -[C(R4)2]nO[C(R4)2]n-, -[C(R4)2]nCO[C(R4)2]n- o - [C(R4)2]nCOO[C(R4)2]n-; Y es alquileno, cicloalquileno, Het-diílo o Ar-diílo; T es un carbociclo o heterociclo mono- o bicíclico saturado o insaturado con 0 a 4 átomos de N, O y/o S, que está mono- o disustituido con =O, =S, =NR3, =N-CN, =N-NO2, =NOR3, =NCOR3, =NCOOR3, =NOCOR3 y que también puede estar mono-, di- o trisustituido con R3, Hal, A, -[C(R4)2]n-Ar, -[C(R4)2]n-Het, -[C(R4)2]n-cicloalquilo, OR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3CON(R3)2, NR3SO2A, COR3, SO2NR3 y/o S(O)nA; A es alquilo no ramificado o ramificado con C1-10, en donde uno o dos grupos CH2 pueden estar reemplazados por átomos de O o S y/o por grupos -CH=CH y/o también 1-7 átomos de H pueden estar reemplazados por F; Ar es fenilo, naftilo o bifenilo no sustituido o mono-, di- o trisustituido con Hal, A, OR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3CON(R3)2, NR3SO2A, COR3, SO2N(R3)2, S(O)nA, -[C(R4)2]n-COOR3 u -O[C(R4)2]o-COOR3; Ar' es fenilo, naftilo o bifenilo no sustituido o mono-, di- o trisustituido con Hal, A, OR4, N(R4)2, NO2, CN, COOR4, CON(R4)2, NR4COA, NR4CON(R4)2, NR4SO2A, COR4, SO2N(R4)2, S(O)nA, -[C(R4)2]n-COOR4 u -O[C(R4)2]o-COOR4; Het es un heterociclo mono- o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede estar no sustituido o mono-, di- o trisustituido con Hal, A; -[C(R4)2]n-Ar, -[C(R4)2]n-Het', -[C(R4)2]n-cicloalquilo, OR3, N(R3)2, NR3CON(R3)2, NO2, CN, -[C(R4)2]n-COOR3, -[C(R4)2]n-CON(R3)2, NR3COA, NR3SO2A, COR3, SO2NR3, S(O)mA y/o el oxígeno del carbonilo; Het' es un heterociclo mono-, o bicíclico saturado, insaturado o aromático con 1 a 4 átomo de N, O y/o S, que puede estar no sustituido o mono- o disustituido con el oxígeno del carbonilo, =S, =N(R4)2, Hal, A, OR4, N(R4)2, NO2, CN, COOR4, CON(R4)2, NR4COA, NR4CON(R4)2, NR4SO2A, COR4, SO2NR4 y/o S(O)nA; Hal es F, Cl, Br o I; n es 0, 1 o 2; o es 1, 2 o 3; así como sus derivados, solvatos, sales y estereoisomeros de utilidad farmacéuticamente, incluyendo sus mezclas en todas las proporciones, para preparar un medicamento para la prevencion y el tratamiento de enfermedades tromboembolicas y/o trombosis como consecuencia de una intervencion quirurgica, enfermedades de origen genético con tendencia incrementada a la trombosis, enfermedades del sistema vascular arterial y venoso, insuficiencia cardíaca, fibrilacion atrial, trombofilia, tinnitus y/o sepsis.
ARP050103944A 2004-09-22 2005-09-21 Medicamentos que contienen compuestos de carbonilo y su uso AR050945A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102004045796A DE102004045796A1 (de) 2004-09-22 2004-09-22 Arzneimittel enthaltend Carbonylverbindungen sowie deren Verwendung

Publications (1)

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AR050945A1 true AR050945A1 (es) 2006-12-06

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Country Status (18)

Country Link
US (1) US20080003214A1 (es)
EP (1) EP1791597A2 (es)
JP (1) JP2008513387A (es)
KR (1) KR20070054210A (es)
CN (1) CN101102818A (es)
AR (1) AR050945A1 (es)
AU (1) AU2005287637A1 (es)
BR (1) BRPI0515592A (es)
CA (1) CA2581172A1 (es)
DE (1) DE102004045796A1 (es)
EC (1) ECSP077401A (es)
IL (1) IL181964A0 (es)
MX (1) MX2007003175A (es)
PE (1) PE20060527A1 (es)
RU (1) RU2007115157A (es)
TW (1) TW200612910A (es)
WO (1) WO2006032342A2 (es)
ZA (1) ZA200703272B (es)

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CN104619698B (zh) 2012-06-28 2016-08-31 诺华股份有限公司 吡咯烷衍生物及其作为补体途径调节剂的用途
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