AR047068A1 - Tetrahidroquinolinas - Google Patents

Tetrahidroquinolinas

Info

Publication number
AR047068A1
AR047068A1 ARP040104789A ARP040104789A AR047068A1 AR 047068 A1 AR047068 A1 AR 047068A1 AR P040104789 A ARP040104789 A AR P040104789A AR P040104789 A ARP040104789 A AR P040104789A AR 047068 A1 AR047068 A1 AR 047068A1
Authority
AR
Argentina
Prior art keywords
nnr2
naryl
nheteroaryl
nxr
ncoor
Prior art date
Application number
ARP040104789A
Other languages
English (en)
Inventor
Helmut Reubold
Kai Dr Schiemann
Soheila Dr Anzali
Helga Dr Drosdat
Ulrich Dr Emde
Dirk Dr Finsinger
Johannes Dr Gleitz
Bjoern Dr Hock
Frank Dr Zenke
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
Priority claimed from DE10360154A external-priority patent/DE10360154A1/de
Priority claimed from DE102004026026A external-priority patent/DE102004026026A1/de
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR047068A1 publication Critical patent/AR047068A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom 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
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4706—4-Aminoquinolines; 8-Aminoquinolines, e.g. chloroquine, primaquine
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/12—Heterocyclic 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 three hetero rings
    • C07D491/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Compuestos de la formula (1) en donde W es CH o N; R1, R2, R3 son, de modo independiente entre sí, H, R, A, arilo, heteroarilo, Hal, -(CY2)n-SA, -(CY2)n-SCF3, -(CY2)n-SCN, -(CY2)n-CF3, -(CY2)n-OCF3, cicloalquilo, -SCH3, -SCN, -CF3, -OCF3, -OA, - (CY2)n-OH, -(CY2)n-CO2R, -(CY2)n-CN, -(CY2)n-Hal, -(CY2)nNR2, -(CY2)n-OA, -(CY2)n-OCOA, -SCF3, -(CY2)n-CONR2, -(CY2)n-NHCOA, -(CY2)n-NHSO2A, SF5, Si(CH3)3, CO-(CY2)n-CH3, -(CY2)n-N-pirrolidona, CH(CH2)nNRCOOR, CHNRCOOR, NCO, CH(CH2)nCOOR, NCOOR, CH(CH2)nOH, N(CH2)nOH, CHNH2, CH(CH2)nNR2, CH(CH2)nNR2, C(OH)R, CHNCOR, CH(CH2)narilo, CH(CH2)nheteroarilo, CH(CH2)nR1, N(CH2)nCOOR, CH(CH2)nX(CH2)narilo, CH(CH2)nX(CH2)nheteroarilo, N(CH2)nCONR2, XCONR(CH2)nNR2, N[(CH2)nXCOOR]CO(CH2)narilo, N[(CH2)nXR]CO(CH2)narilo, N[(CH2)nXR]CO(CH2)nXarilo, N[(CH2)nXR]SO2(CH2)narilo, N[(CH2)nNRCOOR]CO(CH2)narilo, N[(CH2)nNR2]CO(CH2)narilo, N[(CH2)nNR2]CO(CH2)nNRarilo, N[(CH2)nNR2]SO2(CH2)narilo, N[(CH2)nXR]CO(CH2)nheteroarilo, N[(CH2)nXR]CO(CH2)nXheteroarilo, N[(CH2)nXR]SO2(CH2)nheteroarilo, N[(CH2)nNRCOOR]CO(CH2)nheteroarilo, N[(CH2)nNR2]CO(CH2)nheteroarilo, N[(CH2)nNR2]CO(CH2)nNRheteroarilo, N[(CH2)nNR2]SO2(CH2)nheteroarilo, O(CH2)nNR2, X(CH2)nNR2, NCO(CH2)nNR2, R1 y R2 también son juntos -N-C(CF3)=N-, -N-CR=N-, -N-N=N-; Y es H, A, Hal; A es alquilo o cicloalquilo, en donde uno o varios átomos de H pueden estar reemplazados por H; Hal es F, Cl, Br, o I; R es H o A, en caso de radicales geminales R también son juntos (CH2)5-,-(CH2)4-,-(CH2)2-X-(CH2)2 o -(CH2)2-Z-(CH2)2; R4, R5 son, de modo independiente entre sí, H o un radical de N-pirrolidona insustituida o mono o polisustituida con OR, NO2, Hal, CF3, OCF3, CN, NR2 o SR, arilo o heteroarilo, -X- (CH2)2OR, -X-CO(CH2)nCH3, -X-(CH2)2NR2, R1, Sarilo, Oarilo, CH2Si(CH3)3, o juntos son -X(CR2)2, -X-(CR2)3-, X-(CHCH2OR) (CH2)2-, X-(CHCH2NR2)(CH2)2-, -X (CH2)2NR2, -(CR2)3-, -(CR2)4-. -CR=CR-CR=CR-, -XCHQ(CR2)2-, -XCHQCR2-, R-N-(C=X)-N-R, - XC[(CH2)nOR]2CH2CH2-; X es O, S o NR; Q es CH2Hal, CHO, CORa, CH2Ra, CH2OCORa, CH2NCOR1, CH2N(R1)2, CH2OR1, CH2OCON(R1)2, CH2OCOOR1, CH2NHCON(R1)2, CH2NHCOOR1, OR, NHR2, NR2, NR(CH2)narilo, NR(CH2)nOR, COOR, radical de N-pirrolidona, OCOR, NR(CH2)nNR2, N[(CH2)nNR2]CO(CH2)narilo, N[(CH2)nNHCOOR]COarilo, R1, N[CH2(CH2)nOR]2, NR(CH2)nNCOOR, X(CH2)nX(CH2)nXR, NR(CH2)nX(CH2)nOH, NR(CH2)nO(CH2)nOH, (CH2)nCOOR, O(CO)NR(CH2)nOR, O(CO) (CH2)nNR2, NR(CH2)nNR2, N[(CH2)nNR2]CO(CH2)narilo, N[(CH2)nXR]CO(CH2)narilo, N[(CH2)nXR]CO(CH2)nheteroarilo, N[(CH2)nNR2]CO(CH2)nheteroarilo, N[(CH2)nNR2]CO(CH2)nR1, N(R)(CH2)nN(R)COOR, XCOO(CH2)nNR2, OSO2A, OSO2CF3, OSO2Ar, OCONR2, OCH2(CH2)nNR2; Ra se selecciona del grupo de formulas (2); Z es CH2, X, CHCONH2, CH(CH2)nNRCOOR, CHNRCOOR, NCO, CH(CH2)nCOOR, NCOOR, CH(CH2)nOH, N(CH2)nOH, CHNH2, CH(CH2)nNR2, CH(CH2)nNR2, C(OH)R,CHNCOR, CH(CH2)narilo, CH(CH2)nheteroarilo, CH(CH2)nR1, N(CH2)nCOOR, CH(CH2)nX(CH2)narilo, CH(CH2)nX(CH2)nheteroarilo, N(CH2)nCONR2, XCONR(CH2)nNR2, N[(CH2)nXCOOR]CO(CH2)narilo, N[(CH2)nXR]CO(CH2)narilo, N[(CH2)nXR]CO(CH2)nXarilo, N[(CH2)nXR]SO2(CH2)narilo, N[(CH2)nNRCOOR]CO(CH2)narilo, N[(CH2)nNR2]CO(CH2)narilo, N[(CH2)nNR2]CO(CH2)nNRarilo, N[(CH2)nNR2]SO2(CH2)narilo, N[(CH2)nXR]CO(CH2)nheteroarilo, N[(CH2)nXR]CO(CH2)nXheteroarilo, N[(CH2)nXR]SO2(CH2)nheteroarilo, N[(CH2)nNRCOOR]CO(CH2)nheteroarilo, N[(CH2)nNR2]CO(CH2)nheteroarilo, N[(CH2)nNR2]CO(CH2)nNRheteroarilo, N[(CH2)nNR2]SO2(CH2)nheteroarilo, O(CH2)nNR2, X(CH2)nNR2, NCO(CH2)nNR2; R6 es arilo o heteroarilo insustituido o mono o polisustituido con arilo o heteroarilo, que puede estar sustituido con Hal, NO2, CN, A, OR, OCOR, COR, NR2, CF3, OCF3, OCH(CF3)2, Hal, NO2, CN, OR, A, -(CY2)nOR, -OCOR, -(CY2)n-CO2R, -(CY2)n-CN, -NCOR, -COR o -(CY2)n-NR2; R7 es (C=O)-R, (C=O)-NR2, (C=O)-OR, H o A, m es 0, 1 o 2; y n es 0, 1, 2, 3, 4, 5, 6 o 7, así como sus derivados, solvatos, tautomeros, sales y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones. Se pueden utilizar, entre otras cosas, para el tratamiento de tumores.
ARP040104789A 2003-12-20 2004-12-20 Tetrahidroquinolinas AR047068A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE10360154A DE10360154A1 (de) 2003-12-20 2003-12-20 Tetrahydrochinoline
US53996104P 2004-01-30 2004-01-30
DE102004026026A DE102004026026A1 (de) 2004-05-27 2004-05-27 Tetrahydrochinoline

Publications (1)

Publication Number Publication Date
AR047068A1 true AR047068A1 (es) 2006-01-04

Family

ID=34743228

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040104789A AR047068A1 (es) 2003-12-20 2004-12-20 Tetrahidroquinolinas

Country Status (6)

Country Link
KR (1) KR101211973B1 (es)
AR (1) AR047068A1 (es)
CY (2) CY1110467T1 (es)
DE (1) DE502004008434D1 (es)
HK (1) HK1096395A1 (es)
MX (1) MXPA06006714A (es)

Also Published As

Publication number Publication date
MXPA06006714A (es) 2006-08-18
CY1111704T1 (el) 2015-10-07
DE502004008434D1 (de) 2008-12-18
CY1110467T1 (el) 2015-04-29
KR101211973B1 (ko) 2012-12-13
KR20060127002A (ko) 2006-12-11
HK1096395A1 (en) 2007-06-01

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