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AR068657A1 - Derivados de piperidina y piperazina - Google Patents

Derivados de piperidina y piperazina

Info

Publication number
AR068657A1
AR068657A1 ARP080104328A ARP080104328A AR068657A1 AR 068657 A1 AR068657 A1 AR 068657A1 AR P080104328 A ARP080104328 A AR P080104328A AR P080104328 A ARP080104328 A AR P080104328A AR 068657 A1 AR068657 A1 AR 068657A1
Authority
AR
Argentina
Prior art keywords
nnr2
atoms
hal
nhet
mono
Prior art date
Application number
ARP080104328A
Other languages
English (en)
Inventor
Melanie Schultz
Kai Schiemann
Ingo Kober
Andree Blaukat
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR068657A1 publication Critical patent/AR068657A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58Benzoxazoles; Hydrogenated benzoxazoles 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 in position 2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/32Oxygen atoms
    • C07D209/34Oxygen atoms in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/26Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/16Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • C07D249/18Benzotriazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62Benzothiazoles
    • C07D277/68Benzothiazoles 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 in position 2
    • 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
    • C07D413/12Heterocyclic 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 chain containing hetero atoms as chain links
    • 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Indole Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Los compuestos de la formula (1), en donde R1 es un heterociclo insaturado o aromático bicíclico con 1 a 4 átomos de N, O y/o S, que puede no estar sustituido o que puede estar mono-, di- o trisustituido con A, Hal, NR2, (CR2)nCN, OR5 y/u =O (oxígeno del carbonilo); D es C o S; G es N o C, en caso de que G = N, R2 está ausente; en caso de que G = O, R2 es H o Ar1 o también junto con el átomo de C al que está unido el R2 y con E-W un radical espirocíclico seleccionado del grupo de formulas (2); Q es alquileno no ramificado o ramificado con 1, 2, 3 o 4 átomos de C, en donde 1-5 átomos de H pueden estar reemplazados por A, (CR2)n[X(CR2)n]p-Y, F y/o Cl; R3 es H, A, Ar, OR, SR, NR2, Hal, No2, CN, o (CR2)n[X(CR2)n]p-Y; X es O, NR o CR2; Y es OR o NR2; R5 es H o alquilo no ramificado o ramificado con 1, 2, 3, 4, 5 o 6 átomos de C, en donde 1-7 átomos de H pueden estar reemplazados por F y/o Cl; E es COO(CR2)n, COO(CRR4), CO(CR2)mO, CONH(CR2)n, C(=S)NH(CR2)n, S(O)qNH(CR2)n, S(O)q(CR2)n, CO(CR2)n, (CR2)n, CO(CR2)mO(CR2)n, CO(CR2)mNH(CR2)n, CO(CH2)nCO, COCHR6CHR7, C(=S)O(CR2)n, CO(CRR4)(CR2)n, COO(CRR4), (CRR4)(CR2)n, S(O)qCR=CR, COCR=CR, (CR2)mCO, CONH(CR2)mCRR4 O (CR2)mCONR; R4 es COOR5, Ar1, (CR2)nNR2, OH, NRCOOR8 o NRCOOA; R6, R7 son juntos (CH2)1-4; R8 es fenilo, naftilo o fluorenilo; R es H o alquilo no ramificado o ramificado con 1, 2, 3, 4, 5 o 6 átomos de carbono; W es Ar o Het; Ar es fenilo, indanilo, naftilo o bifenilo no sustituido o mono-, di-, tri-, tetra- o pentasustituido con Hal, A, (CR2)nOR, O(CR2)n, Ar1, (CR2)nNR2, SR, No2, CN, COOR, CONR2, NRCOA, NRSo2A, So2NR2, S(O)qA, CO-Het, (CR2)nHet, O(CR2)nNR2, O(CR2)nHet, NHCOOA, NHCONR2, NHCOO(CR2)nNR2, NHCOO(CR2)nHet, CR5=CR5Ar1, So2Het, NHCONH(CR2)nNR2, NHCONH(CR2)nHet, OCONH(CR2)nNR2, OCONH(CR2)nHet, CONR(CR2)nNR2, CONR(CR2)nHet y/o COA; Het es un heterociclo saturado, insaturado o aromático mono-, di- o tricíclico con 1 a 4 átomos de N, O y/o S, que puede no estar sustituido o que puede estar mono-, di- o trisustituido con Hal, A, (CR2)nAr1, O(CR2)nAr1, (CR2)nOR, (CR2)nNR2, SR, No2, CN, COOR, CONR2, NRCOA, NRSo2A, So2NR2, S(O)qA, CO-Het1, (CR2)nHet1, O(CR2)nNR2, O(CR2)nHet1, NHCOOA, NHCONR2, NHCOO(CR2)nNR2, NHCOO(CR2)nHet1, NHCONH(CR2)nNR2, NHCONH(CR2)nHet1, OCONH(CR2)nNR2, OCONH(CR2)nHet1, CO-Het1, CHO, COA, =S, =NH, =NA y/u =O (oxígeno del carbonilo); Het1 es un heterociclo saturado monocíclico con 1 a 2 N y/o átomos de O, que puede estar mono- o disustituido con A, OA, OH, Hal y/u =O (oxígeno del carbonilo); Ar1 es fenilo no sustituido o mono-, di-, tri-, tetra- o pentasustituido con Hal, CN, A y/o (CR2)nOR; A es alquilo no ramificado o ramificado con 1-10 átomos de C, en donde 1-7 átomos de H pueden estar reemplazados por OR, CN, NR2, F y/o Cl y/o en donde uno o dos grupos CH2 no adyacentes pueden estar reemplazados por O, NH, s, so, so2 y/o por grupos CH=CH, o alquilo cíclico con 3-7 átomos de C; m es 1, 2, 3, 4, 5 o 6; n es 0, 1, 2, 3, 4, 5, 6, 7 u 8; p es 1, 2, 3, 4, 5 o 6; q es 0, 1 o 2; Hal es F, Cl, Br o l; así como sus tautomeros, sales y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones, se pueden utilizar para el tratamiento de tumores. Medicamento en base al compuesto (y uso de este para preparar los medicamentos) y procedimiento de preparacion del compuesto.
ARP080104328A 2007-10-05 2008-10-03 Derivados de piperidina y piperazina AR068657A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102007047737A DE102007047737A1 (de) 2007-10-05 2007-10-05 Piperidin- und Piperazinderivate

Publications (1)

Publication Number Publication Date
AR068657A1 true AR068657A1 (es) 2009-11-25

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Family Applications (1)

Application Number Title Priority Date Filing Date
ARP080104328A AR068657A1 (es) 2007-10-05 2008-10-03 Derivados de piperidina y piperazina

Country Status (22)

Country Link
US (2) US8791111B2 (es)
EP (2) EP2426106B1 (es)
JP (2) JP5597538B2 (es)
KR (1) KR20100075601A (es)
CN (1) CN101808988A (es)
AR (1) AR068657A1 (es)
AU (1) AU2008310067B2 (es)
BR (1) BRPI0817644A2 (es)
CA (1) CA2701519C (es)
CY (2) CY1113757T1 (es)
DE (1) DE102007047737A1 (es)
DK (2) DK2426106T3 (es)
EA (1) EA017787B1 (es)
ES (2) ES2392475T3 (es)
HR (2) HRP20120802T1 (es)
IL (1) IL204562A0 (es)
MX (1) MX2010003366A (es)
PL (2) PL2426106T3 (es)
PT (2) PT2193118E (es)
SI (2) SI2426106T1 (es)
WO (1) WO2009046841A2 (es)
ZA (1) ZA201003124B (es)

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AU2008310067B2 (en) 2013-09-26
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ES2429843T3 (es) 2013-11-18
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US8754097B2 (en) 2014-06-17
WO2009046841A3 (de) 2009-06-18
DK2426106T3 (da) 2013-11-04
JP5597538B2 (ja) 2014-10-01
CN101808988A (zh) 2010-08-18
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EA201000549A1 (ru) 2010-10-29
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US8791111B2 (en) 2014-07-29
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