MX9804108A - Derivados de quinolina-4-carboxamida, su preparacion y uso como antagonistas receptores de neuroquinina 3 (nk-3)- y neuroquinina 2 (kn-2). - Google Patents

Derivados de quinolina-4-carboxamida, su preparacion y uso como antagonistas receptores de neuroquinina 3 (nk-3)- y neuroquinina 2 (kn-2).

Info

Publication number
MX9804108A
MX9804108A MX9804108A MX9804108A MX9804108A MX 9804108 A MX9804108 A MX 9804108A MX 9804108 A MX9804108 A MX 9804108A MX 9804108 A MX9804108 A MX 9804108A MX 9804108 A MX9804108 A MX 9804108A
Authority
MX
Mexico
Prior art keywords
alkyl
optionally substituted
group
aryl
mono
Prior art date
Application number
MX9804108A
Other languages
English (en)
Inventor
Giuseppe Arnaldo Mari Giardina
Mario Grugni
Luca Francesco Raveglia
Carlo Farina
Original Assignee
Smithkline Beecham Spa
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 Spa filed Critical Smithkline Beecham Spa
Publication of MX9804108A publication Critical patent/MX9804108A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic 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
    • C07D231/12—Heterocyclic 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic 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
    • C07D215/16—Heterocyclic 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/233—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic 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
    • C07D215/16—Heterocyclic 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
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/50—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 4
    • C07D215/52—Carbon 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic 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
    • C07D233/56—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems

Abstract

Un compuesto de formula (Ver Formula) o una sal del mismo o un solvato del mismo, en la cual Ar es un arilo opcionalmente o un grupo cicloalcanodienilo de C5-7, o un grupo heterocíclico aromático de anillo sencillo o fundido, opcionalmente substituido; R es alquilo de C1-2, cicloalquilo de C3-7; (cicloalquilo de C3-7)-alquilo, fenil-(alquilo de C1-6) o alquilo de C1-6 opcionalmente fenil-substituido, un anillo heteroaromático de cinco miembros, opcionalmente substituido, hasta de cuatro heteroátomos, seleccionado entre O y N, hidroxi-(alquilo de C1-6), amino-(alquilo de C1-6), (alquilo de C1-6)-aminoalquilo, (dialquilo de C1-6)- aminoalquilo, acilaminoalquilo de C1-6, (alcoxi de C1-6)-alquilo, (alquilo de C1-6)-carbonilo, carboxi, (alcoxi de C1-6)-carbonilo, (alcoxi de C1-6)-carbonilo-(alquilo de C1-6), amino carbonilo, (alquilo de C1-6)-aminocarbonilo, (dialquilo de C1-6)-aminocarbonilo, halogeno-(alquilo de C1-6); o R es un grupo (CH2)p-en el cual P es 2 o 3, grupo que forma un anillo con un átomo de carbono de Ar; R3 representa hidrogeno o hasta cuatro substituyentes opcionales, seleccionados de la lista que consta de: alquilo de C1-6; alquenilo de C1-6, arilo, alcoxi de C1-6, hidroxi, halogeno, nitro, ciano, carboxamido, sulfonamido, (alcoxi de C1-6)-carbonilo, trifluorometilo, aciloxi, ftalimido, amino o mono- y di(alquilo de C1-6)-amino; R2 representa hidrogeno, alquilo de C1-6, hidroxi, halogeno, ciano, amino, mono- o di(alquilo de C1-6)-amino, alquilsulfonilamino, mono- o di(alcanoilo de C1-6)-amino en donde cualquier grupo alquilo es substituido opcionalmente con un grupo amino o con un grupo mono- o dialquilamino, o R3 es una porcion -X-(CH-2)n- Y en la cual X es un enlace o -O- y n es un numero entero en el intervalo de 1 a 5 siempre que cuando X es 0, n minuscula es solamente un numero entero de 2 a 5 e Y representa un grupo Ny1Y2 en el cual Y1 e Y2 seleccionan independientemente entre hidrogeno, alquilo de C1-3, alquenilo de C1-3, arilo o aril(alquilo de C1-6) o Y es hidroxi, halogeno o un grupo heterocíclico de anillo sencillo o fundido, enlazado con N, opcionalmente substituido, R3 es alquilo de C1-6 ramificado o lineal, cicloalquilo de C3-7, cicloalquilo de C4-7-alquilo, arilo opcionalmente substituido, o un grupo heterocíclico aromático de anillo sencillo o fundido, opcionalmente substituido; y R4 representa hidrogeno o alquilo de C1-6.
MX9804108A 1995-11-24 1998-05-22 Derivados de quinolina-4-carboxamida, su preparacion y uso como antagonistas receptores de neuroquinina 3 (nk-3)- y neuroquinina 2 (kn-2). MX9804108A (es)

Applications Claiming Priority (2)

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

Publications (1)

Publication Number Publication Date
MX9804108A true MX9804108A (es) 1998-09-30

Family

ID=26331327

Family Applications (1)

Application Number Title Priority Date Filing Date
MX9804108A MX9804108A (es) 1995-11-24 1998-05-22 Derivados de quinolina-4-carboxamida, su preparacion y uso como antagonistas receptores de neuroquinina 3 (nk-3)- y neuroquinina 2 (kn-2).

Country Status (26)

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

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WO1998052942A1 (en) * 1997-05-23 1998-11-26 Smithkline Beecham S.P.A. Quinoline-4-carboxamide derivatives as nk-2 and nk-3 receptor antagonists
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GB9825554D0 (en) 1998-11-20 1999-01-13 Smithkline Beecham Spa Novel Compounds
IL143137A0 (en) * 1998-11-20 2002-04-21 Smithkline Beecham Spa Quinoline-4-carboxamide derivatives as nk-3 and nk-2 receptor antagonists
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
DK1035115T3 (da) * 1999-02-24 2005-01-24 Hoffmann La Roche 4-phenylpyridinderivater og anvendelse deraf som NK-1-receptorantagonister
US7037922B1 (en) 2000-03-10 2006-05-02 Neurogen Corporation Aryl fused 2,4-disubstituted pyridines: NK3 receptor ligands
WO2000058307A2 (en) * 1999-03-11 2000-10-05 Neurogen Corporation Aryl fused 2,4-disubstituted pyridines: nk3 receptor ligands
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AU4802500A (en) * 1999-04-26 2000-11-10 Neurogen Corporation 2-aminoquinolinecarboxamides: neurokinin receptor ligands
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WO2002013825A1 (en) * 2000-08-11 2002-02-21 Smithkline Beecham P.L.C. Novel pharmaceutical use of quinnoline derivatives
WO2002038547A1 (en) * 2000-11-13 2002-05-16 Glaxosmithkline Spa Quinoline derivatives as nk-3 and nk-2 antagonists
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CN102924375B (zh) * 2012-06-21 2015-02-18 江苏恩华药业股份有限公司 Talnetant中间体及其制备方法和应用
US9475773B2 (en) 2013-04-19 2016-10-25 Astrazeneca Ab NK3 receptor antagonist compound (NK3RA) for use in a method for the treatment of polycystic ovary syndrome (PCOS)
EP3191452A1 (de) 2014-09-09 2017-07-19 Bayer Pharma Aktiengesellschaft Substituierte n,2-diarylchinolin-4-carboxamide und ihre anti-inflammatorische verwendung
EP3271334A1 (de) 2015-03-18 2018-01-24 Bayer Pharma Aktiengesellschaft Substituierte n-bicyclo-2-arylchinolin-4-carboxamide und ihre verwendung
WO2017072629A1 (en) 2015-10-29 2017-05-04 Cadila Healthcare Limited Pharmaceutical combination of nk3 receptor antagonist and biguanides
WO2017153235A1 (de) 2016-03-09 2017-09-14 Bayer Pharma Aktiengesellschaft Substituierte n-cyclo-3-aryl-1-naphthamide und ihre verwendung
WO2017153234A1 (de) 2016-03-09 2017-09-14 Bayer Pharma Aktiengesellschaft Substituierte n-cyclo-2-arylchinolin-4-carboxamide und ihre verwendung
WO2017153231A1 (de) 2016-03-09 2017-09-14 Bayer Pharma Aktiengesellschaft Substituierte n-cyclo-2-arylisochinolinon-4-carboxamide und ihre verwendung
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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
HUP9901016A2 (hu) 2000-03-28
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
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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