EA199800538A1 - Производные хинолин-4-карбоксамида, их получение и их применение в качестве антагонистов рецептора нейрокинина-3 (-к-3) и нейрокинина-2 (-к-2) - Google Patents

Производные хинолин-4-карбоксамида, их получение и их применение в качестве антагонистов рецептора нейрокинина-3 (-к-3) и нейрокинина-2 (-к-2)

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Publication number
EA199800538A1
EA199800538A1 EA199800538A EA199800538A EA199800538A1 EA 199800538 A1 EA199800538 A1 EA 199800538A1 EA 199800538 A EA199800538 A EA 199800538A EA 199800538 A EA199800538 A EA 199800538A EA 199800538 A1 EA199800538 A1 EA 199800538A1
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EA
Eurasian Patent Office
Prior art keywords
alkyl
group
optionally substituted
mono
amino
Prior art date
Application number
EA199800538A
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English (en)
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EA001771B1 (ru
Inventor
Джузеппе Арнальдо Мариа Гьярдина
Марио Груни
Лука Франческо Равелиа
Карло Фарина
Original Assignee
Смитклайн Бичам С.П.А.
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 IT96MI001688 external-priority patent/IT1307330B1/it
Application filed by Смитклайн Бичам С.П.А. filed Critical Смитклайн Бичам С.П.А.
Publication of EA199800538A1 publication Critical patent/EA199800538A1/ru
Publication of EA001771B1 publication Critical patent/EA001771B1/ru

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    • 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
    • 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
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

В настоящем изобретении предложено соединение формулы (I)или его соль, или его сольват, где Ar является необязательно замещенной арильной или C-циклоалкдиенильной группой или необязательно замещенной ароматической гетероциклической группой, содержащей одиночное или конденсированное кольцо; R является C-алкилом, C-циклоалкилом, C-циклоалкилалкилом, необязательно замещенным фенилом или фенил-C-алкилом, необязательно замещенным пятичленным гетероароматическим кольцом, содержащим до четырех гетероатомов, выбранных из O и N, гидрокси-C-алкилом, амино-C-алкилом, C-алкиламиноалкилом, ди-C-алкиламиноалкилом, C-ациламиноалкилом, C-алкоксилалкилом, C-алкилкарбонилом, карбокси, C-алкоксикарбонилом, C-алкоксикарбонил-C-алкилом, аминокарбонилом, C-алкиламинокарбонилом, ди-C-алкиламинокарбонилом, галоген-C-алкилом; или R является группой -(CH)-, где p равно 2 или 3, причем эта группа образует кольцо с атомом углерода Ar; Rпредставляет собой водород или до четырех необязательных заместителей, выбранных из списка, состоящего из C-алкила, C-алкенила, арила, C-алкокси, гидрокси, галогена, нитро, циано, карбокси, карбоксамидо, сульфонамидо, C-алкоксикарбонила, трифторметила, ацилокси, фталимидо, амино или моно- и ди-C-алкиламино; Rпредставляет собой водород, C-алкил, гидрокси, галоген, циано, амино, моно- или ди-C-алкиламино, алкилсульфониламино, моно- или ди-C-алканоиламино, где алкильная группа является необязательно замещенной аминогруппой или моно- или диалкиламиногруппой; или Rявляется группой -X-(CH)-Y, где X является связью или -O- и n представляет собой целое число в диапазоне от 1 до 5, при условии, что, когда X является -O-, тогда n представляет собой только целое число от 2 до 5, и Y представляет собой группу NYY, где Yи
EA199800538A 1995-11-24 1996-11-22 Производные хинолин-4-карбоксамида, их получение и их применение в качестве антагонистов рецептора нейрокинина-3 (-к-3) и нейрокинина-2 (-к-2) EA001771B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IT95MI002462 IT1276171B1 (it) 1995-11-24 1995-11-24 Derivati chinolinici
IT96MI001688 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
EA199800538A1 true EA199800538A1 (ru) 1998-12-24
EA001771B1 EA001771B1 (ru) 2001-08-27

Family

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Family Applications (1)

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EA199800538A EA001771B1 (ru) 1995-11-24 1996-11-22 Производные хинолин-4-карбоксамида, их получение и их применение в качестве антагонистов рецептора нейрокинина-3 (-к-3) и нейрокинина-2 (-к-2)

Country Status (26)

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

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PL326928A1 (en) 1998-11-09
KR19990071598A (ko) 1999-09-27
AR004735A1 (es) 1999-03-10
CN1207729A (zh) 1999-02-10
SK66898A3 (en) 1998-12-02
BG102557A (bg) 1999-03-31
UY24375A1 (es) 1997-05-22
AU1031897A (en) 1997-06-19
US20020068827A1 (en) 2002-06-06
NO311213B1 (no) 2001-10-29
UY24555A1 (es) 2001-04-30
CZ158098A3 (cs) 1998-10-14
NO982333D0 (no) 1998-05-22
EA001771B1 (ru) 2001-08-27
TR199800883T2 (xx) 2000-12-21
HUP9901016A3 (en) 2002-01-28
OA11011A (en) 2003-03-06
BR9611757A (pt) 1999-04-06
MX9804108A (es) 1998-09-30
AP9801238A0 (en) 1998-06-30
TW409123B (en) 2000-10-21
IL124418A0 (en) 1998-12-06
NO982333L (no) 1998-07-22
EP1019377A1 (en) 2000-07-19
HUP9901016A2 (hu) 2000-03-28
MA24011A1 (fr) 1997-07-01
DZ2128A1 (fr) 2002-10-26
CA2238328A1 (en) 1997-06-05
JP2000513325A (ja) 2000-10-10
WO1997019926A1 (en) 1997-06-05

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