HUP9901016A2 - 4-Kinolinkarboxamid-származékok, előállításuk, valamint neurokinin-3 (NK-3) és neurokinin-2 (NK-2) receptor antagonistákként történő felhasználásuk - Google Patents

4-Kinolinkarboxamid-származékok, előállításuk, valamint neurokinin-3 (NK-3) és neurokinin-2 (NK-2) receptor antagonistákként történő felhasználásuk

Info

Publication number
HUP9901016A2
HUP9901016A2 HU9901016A HUP9901016A HUP9901016A2 HU P9901016 A2 HUP9901016 A2 HU P9901016A2 HU 9901016 A HU9901016 A HU 9901016A HU P9901016 A HUP9901016 A HU P9901016A HU P9901016 A2 HUP9901016 A2 HU P9901016A2
Authority
HU
Hungary
Prior art keywords
alkyl
amino
carbonyl
cyclic
optionally substituted
Prior art date
Application number
HU9901016A
Other languages
English (en)
Inventor
Carlo Farina
Giuseppe Arnaldo Maria Giardina
Mario Grugni
Luca Francesco Raveglia
Original Assignee
Smithkline Beecham S.P.A.
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 IT95MI002462 external-priority patent/IT1276171B1/it
Priority claimed from ITMI961688 external-priority patent/IT1307330B1/it
Application filed by Smithkline Beecham S.P.A. filed Critical Smithkline Beecham S.P.A.
Publication of HUP9901016A2 publication Critical patent/HUP9901016A2/hu
Publication of HUP9901016A3 publication Critical patent/HUP9901016A3/hu

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/48Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/50Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 4
    • C07D215/52Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 4 with aryl radicals attached in position 2
    • 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
    • A61K31/47Quinolines; Isoquinolines
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/20Oxygen atoms
    • C07D215/22Oxygen atoms attached in position 2 or 4
    • C07D215/233Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

Abstract

A találmány egy (I) általánős képletű vegyületre - amelynek képletében Ar adőtt esetben szűbsztitűált aril-, ciklőalkadienil- vagy adőttesetben szűbsztitűált, mőnőciklűsős vagy kőndenzált gyűrűs, arőmásheterőciklűsős csőpőrt; R alkil-, ciklőalkil-, ciklőalkil-alkil-, adőtt esetben szűbsztitűáltfenil- vagy fenil-(1-6 szénatőmős alkil)-, adőtt esetben szűbsztitűáltöttagú, legfeljebb négy, az őxigén- és/vagy nitrőgénatőm közülkiválasztőtt heterőatőmőt tartalmazó heterőarőmás csőpőrt, hidrőxi-alkil-, aminő-alkil-, alkil-aminő-alkil-, dialkil-aminő-alkil-, acil-aminő-alkil-, alkőxi-alkil-, alkil-karbőnil-, karbőxi-, alkőxi-karbőnil-, alkőxi-karbőnil-alkil-, karbamőil-alkil-aminő-karbőnil-,dialkil-aminő-karbőnil-, halőgén-alkil-, vagy egy, az Ar csőpőrt egyikszénatőmjával gyűrűt képező -(CH2)p- általánős képletű csőpőrt,amelyben p 2 vagy 3; R1 hidrőgénatőm vagy adőtt esetben legfeljebb négy szűbsztitűens akövetkezők közül: alkil-, alkenil-, aril-, alkőxi-, hidrőxicsőpőrt,halőgénatőm, nitrő-, cianő-, karbőxi-, karbőxamidő-, szűlfőnamidő-,alkőxi-karbőnil-, triflűőrmetil-, acil-őxi, ftálimidő-, aminő-, mőnő-vagy dialkil-aminő-csőpőrt; R2 hidrőgénatőm, alkil-, hidrőxi-, halőgénatőm, cianő-, aminő-, mőnő-vagy dialkil-aminő-, alki-szűlfőnil-aminő-, mőnő- vagy dialkanőil-aminő-, ahől bármely alkilcsőpőrt adőtt esetben aminő- vagy dialkil-aminő-csőpőrttal szűbsztitűált, vagy -X-(CH2)n-Y általánős képletűcsőpőrt; R3 alkil-, ciklőalkil-, ciklőalkil-alkil-, adőtt esetben szűbsztitűáltaril- vagy mőnőciklűsős, vagy kőndenzált gyűrűs, arőmás heterőciklűsőscsőpőrt; és R4 hidrőgénatőm vagy alkilcsőpőrt - vagy a vegyületnek egyszőlvátjára, vagy sójára vőnatkőzik. A találmány szerinti vegyületekNK-3 és NK-2 receptőr antagőnisták. ŕ
HU9901016A 1995-11-24 1996-11-22 Quinoline-4-carboxamide derivatives, their preparation and their use as neurokinin 3(nk-3)-and neurokinin 2(nk-2) receptor antagonists HUP9901016A3 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IT95MI002462 IT1276171B1 (it) 1995-11-24 1995-11-24 Derivati chinolinici
ITMI961688 IT1307330B1 (it) 1996-08-02 1996-08-02 Derivati chinolinici
PCT/EP1996/005207 WO1997019926A1 (en) 1995-11-24 1996-11-22 Quinoline-4-carboxamide derivatives, their preparation and their use as neurokinin 3 (nk-3)- and neurokinin 2 (nk-2) receptor antagonists.

Publications (2)

Publication Number Publication Date
HUP9901016A2 true HUP9901016A2 (hu) 2000-03-28
HUP9901016A3 HUP9901016A3 (en) 2002-01-28

Family

ID=26331327

Family Applications (1)

Application Number Title Priority Date Filing Date
HU9901016A HUP9901016A3 (en) 1995-11-24 1996-11-22 Quinoline-4-carboxamide derivatives, their preparation and their use as neurokinin 3(nk-3)-and neurokinin 2(nk-2) receptor antagonists

Country Status (26)

Country Link
US (1) US20020068827A1 (hu)
EP (1) EP1019377A1 (hu)
JP (1) JP2000513325A (hu)
KR (1) KR19990071598A (hu)
CN (1) CN1207729A (hu)
AP (1) AP9801238A0 (hu)
AR (1) AR004735A1 (hu)
AU (1) AU1031897A (hu)
BG (1) BG102557A (hu)
BR (1) BR9611757A (hu)
CA (1) CA2238328A1 (hu)
CZ (1) CZ158098A3 (hu)
DZ (1) DZ2128A1 (hu)
EA (1) EA001771B1 (hu)
HU (1) HUP9901016A3 (hu)
IL (1) IL124418A0 (hu)
MA (1) MA24011A1 (hu)
MX (1) MX9804108A (hu)
NO (1) NO311213B1 (hu)
OA (1) OA11011A (hu)
PL (1) PL326928A1 (hu)
SK (1) SK66898A3 (hu)
TR (1) TR199800883T2 (hu)
TW (1) TW409123B (hu)
UY (2) UY24375A1 (hu)
WO (1) WO1997019926A1 (hu)

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US6780875B2 (en) * 1998-11-20 2004-08-24 Smithkline Beecham S.P.A. Quinoline-4-carboxamide derivatives as NK-3 and NK-2 receptor antagonists
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Also Published As

Publication number Publication date
NO982333D0 (no) 1998-05-22
CZ158098A3 (cs) 1998-10-14
WO1997019926A1 (en) 1997-06-05
EA001771B1 (ru) 2001-08-27
EA199800538A1 (ru) 1998-12-24
AU1031897A (en) 1997-06-19
CN1207729A (zh) 1999-02-10
IL124418A0 (en) 1998-12-06
MA24011A1 (fr) 1997-07-01
KR19990071598A (ko) 1999-09-27
MX9804108A (es) 1998-09-30
AP9801238A0 (en) 1998-06-30
US20020068827A1 (en) 2002-06-06
JP2000513325A (ja) 2000-10-10
DZ2128A1 (fr) 2002-10-26
SK66898A3 (en) 1998-12-02
HUP9901016A3 (en) 2002-01-28
PL326928A1 (en) 1998-11-09
AR004735A1 (es) 1999-03-10
EP1019377A1 (en) 2000-07-19
TW409123B (en) 2000-10-21
UY24375A1 (es) 1997-05-22
CA2238328A1 (en) 1997-06-05
UY24555A1 (es) 2001-04-30
BG102557A (bg) 1999-03-31
BR9611757A (pt) 1999-04-06
OA11011A (en) 2003-03-06
NO982333L (no) 1998-07-22
NO311213B1 (no) 2001-10-29
TR199800883T2 (xx) 2000-12-21

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