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1. (WO1998052942) QUINOLINE-4-CARBOXAMIDE DERIVATIVES AS NK-2 AND NK-3 RECEPTOR ANTAGONISTS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1998/052942 International Application No.: PCT/EP1998/003014
Publication Date: 26.11.1998 International Filing Date: 18.05.1998
Chapter 2 Demand Filed: 25.11.1998
IPC:
C07D 251/52 (2006.01) ,C07D 401/06 (2006.01) ,C07D 491/10 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
251
Heterocyclic compounds containing 1,3,5-triazine rings
02
not condensed with other rings
12
having three double bonds between ring members or between ring members and non-ring members
26
with only hetero atoms directly attached to ring carbon atoms
40
Nitrogen atoms
48
Two nitrogen atoms
52
with an oxygen or sulfur atom attached to the third ring carbon atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
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
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
491
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/-C07D459/290
02
in which the condensed system contains two hetero rings
10
Spiro-condensed systems
Applicants:
SMITHKLINE BEECHAM S.P.A. [IT/IT]; Via Zambeletti I-20021 Baranzate di Bollate, IT (AllExceptUS)
GIARDINA, Giuseppe, Arnaldo, Maria [IT/IT]; IT (UsOnly)
GRUGNI, Mario [IT/IT]; IT (UsOnly)
GRAZIANI, Davide [IT/IT]; IT (UsOnly)
RAVEGLIA, Luca, Francesco [IT/IT]; IT (UsOnly)
Inventors:
GIARDINA, Giuseppe, Arnaldo, Maria; IT
GRUGNI, Mario; IT
GRAZIANI, Davide; IT
RAVEGLIA, Luca, Francesco; IT
Agent:
RUTTER, Keith; SmithKline Beecham plc Corporate Intellectual Property Two New Horizons Court Brentford, Middlesex TW8 9EP, GB
GIDDINGS, Peter, John; SmithKline_Beecham p.l.c. Corporate Intellectual Property Two New Horizons Court Brentford Middlesex TW8 9EP, GB
Priority Data:
9710750.223.05.1997GB
MI97A00235417.10.1997IT
MI97A00277516.12.1997IT
Title (EN) QUINOLINE-4-CARBOXAMIDE DERIVATIVES AS NK-2 AND NK-3 RECEPTOR ANTAGONISTS
(FR) NOUVEAUX COMPOSES
Abstract:
(EN) A compound, or a solvate or a salt thereof, of formula (I): wherein, Ar is an optionally substituted aryl or a C5-7 cycloalkdienyl group, or a C5-7 cycloalkyl group or an optionally substituted single or fused ring aromatic heterocyclic group; R is C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, optionally substituted phenyl or phenyl C1-6 alkyl, an optionally substituted five-membered heteroaromatic ring comprising up to four heteroatoms selected from O and N, hydroxy C1-6 alkyl, amino C1-6 alkyl, C1-6 alkylaminoalkyl, di C1-6 alkylaminoalkyl, C1-6 acylaminoalkyl, C1-6 alkoxyalkyl, C1-6 alkylcarbonyl, carboxy, C1-6 alkoxycarbonyl, C1-6 alkoxycarbonyl C1-6 alkyl, aminocarbonyl, C1-6 alkylaminocarbonyl, di C1-6 alkylaminocarbonyl, halogeno C1-6 alkyl; or R is a group -(CH2)p- wherein p is 2 or 3 which group forms a ring with a carbon atom of Ar; R1 represents hydrogen or up to four optional substituents selected from the list consisting of: C1-6 alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, phthalimido, amino or mono- and di-C1-6 alkylamino; R2 represents a moiety -(CH2)n-NY1Y2 wherein n is an integer in the range of from 1 to 9, Y1 and Y2 are independently selected from hydrogen; C1-6-alkyl; C1-6 alkyl substituted with hydroxy, C1-6 alkylamino or bis (C1-6 alkyl) amino; C1-6-alkenyl; aryl or aryl-C1-6-alkyl or Y1 and Y2 together with the nitrogen atom to which they are attached represent an optionally substituted N-linked single or fused ring heterocyclic group; R3 is branched or linear C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, optionally substituted aryl, or an optionally substituted single of fused ring aromatic heterocyclic group; and R4 represents hydrogen or C1-6 alkyl; a pharmaceutical composition comprising such a compound, process for preparing such a compound and the use of such a compound in medicine.
(FR) L'invention concerne un composé, ou un solvate ou un sel de ce dernier, selon la formule (I). Dans cette dernière, Ar est un aryle éventuellement substitué ou un groupe cycloalkdienyl C5-7 ou un groupe cycloalkyl C5-7 ou un groupe hétérocyclique aromatique à noyau simple ou fondu, éventuellement substitué; R représente alkyle C1-6, cycloalkyle C3-7, cycloalkylalkyle C3-7, phényle éventuellement substitué ou phényle C1-6 alkyle, une chaine hétéroaromatique à cinq éléments éventuellement substituée, comprenant jusqu'à quatre hétéroatomes sélectionnés parmi O et N, hydroxy C1-6 alkyle, amino C1-6 alkyle, alkylaminoalkyle C1-6, di alkylaminoalkyle C1-6, acylamincoalkyle C1-6, alcoxyalkyle C1-6, alkylcarbonyle C1-6, carboxy, alcoxycarbonyle C1-6, alcoxycarbonyle C1-6 alkyle C1-6, aminocarbonyle, alkylaminocarbonyle C1-6, di alkylaminocarnobyle C1-6, halogéno alkyle C1-6; ou R est un groupe -(CH2)p- où p est 2 ou 3, lequel groupe forme un cycle avec un atome de carbone de Ar; R1 représente de l'hydrogène ou jusqu'à quatre substituants éventuels sélectionnés parmi alkyle C1-6, alkényle C1-6, aryle, alcoxy C1-6, hydroxy, halogène, nitro, cyano, carboxy, carboxamido, sulfamido, alcoxycarbonyle C1-6, trifluorométhyle, acyloxy, phthalimido, amino ou mono- et di-alkylamino C1-6. R2 représente une fraction -(CH2)n-NY1Y2 où n est un nombre entier compris entre 1 et 9, Y1 et Y2 sont indépendamment sélectionnés parmi de l'hydrogène, alkyle C1-6, alkyle C1-6 substitué par hydroxy, alkylamino C1-6 ou bis (C1-6alkyl)amino; alkényle C1-6, aryle ou aryl-C1-6-alkyle ou Y1 et Y2 ensemble avec l'atome d'azote auquel ils sont fixés représentent un groupe hétérocyclique à noyau simple ou fondu à liaison N, éventuellement substitué. R3 est un alkyl C1-6 linéaire ou ramifié, cycloalkyle C3-7, cycloalkylalkyle C4-7, aryle éventuellement substitué, ou un groupe hétérocyclique aromatique à noyau simple ou fondu, éventuellement substitué; et R4 représente hydrogène ou alkyle C1-6. L'invention traite aussi d'une composition pharmaceutique comprenant ce composé, un procédé de préparation de ce composé et l'utilisation de ce composé en médecine.
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Designated States: AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CU, CZ, DE, DK, EE, ES, FI, GB, GE, GH, GM, GW, HU, ID, IL, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, UA, UG, US, UZ, VN, YU, ZW
African Regional Intellectual Property Organization (ARIPO) (GH, GM, KE, LS, MW, SD, SZ, UG, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
CZPV1999-4161NO19995711NZ501073SK159299TR1999/02883MXPA/a/1999/010841
APAP/P/1999/001695KR1020010012823SG69007VN4222IL133036EP0983262
US20050159428US20060205735US20070197546JP2002500645 CN1264378CA2291111
EA199901062AU1998082098