Some content of this application is unavailable at the moment.
If this situation persist, please contact us atFeedback&Contact
1. (WO1997016440) 1-(1,2-DISUBSTITUTED PIPERIDINYL)-4-SUBSTITUTED PIPERAZINE DERIVATIVES
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1997/016440 International Application No.: PCT/EP1996/004660
Publication Date: 09.05.1997 International Filing Date: 25.10.1996
Chapter 2 Demand Filed: 05.04.1997
IPC:
C07D 211/58 (2006.01) ,C07D 401/12 (2006.01) ,C07D 405/12 (2006.01) ,C07D 413/14 (2006.01) ,C07D 417/12 (2006.01) ,C07D 471/04 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
211
Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06
having no double bonds between ring members or between ring members and non-ring members
36
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
56
Nitrogen atoms
58
attached in position 4
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
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
Applicants:
JANSSEN PHARMACEUTICA N.V. [BE/BE]; Turnhoutseweg 30 B-2340 Beerse, BE (AllExceptUS)
JANSSENS, Frans, Eduard [BE/BE]; BE (UsOnly)
SOMMEN, François, Maria [BE/BE]; BE (UsOnly)
SURLERAUX, Dominique, Louis, Nestor, Ghislaine [BE/BE]; BE (UsOnly)
LEENAERTS, Joseph, Elisabeth [BE/BE]; BE (UsOnly)
VAN ROOSBROECK, Yves, Emiel, Maria [BE/BE]; BE (UsOnly)
Inventors:
JANSSENS, Frans, Eduard; BE
SOMMEN, François, Maria; BE
SURLERAUX, Dominique, Louis, Nestor, Ghislaine; BE
LEENAERTS, Joseph, Elisabeth; BE
VAN ROOSBROECK, Yves, Emiel, Maria; BE
Agent:
DE CORTE, Filip; Janssen Pharmaceutica N.V. Patent Dept. Turnhoutseweg 30 B-2340 Beerse, BE
Priority Data:
95202929.630.10.1995EP
Title (EN) 1-(1,2-DISUBSTITUTED PIPERIDINYL)-4-SUBSTITUTED PIPERAZINE DERIVATIVES
(FR) DERIVES DE PIPERAZINE A SUBSTITUTION EN POSITIONS 1-(DIPERIDINYLE A DISUBSTITUTION EN POSITIONS 1,2)-4
Abstract:
(EN) This invention concerns the compounds of formula (I), the $i(N)-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; p is 1 or 2; =Q is =O or =NR3; X is a covalent bond or a bivalent radical of formula -O-, -S-, -NR3-; R1 is Ar1, Ar1C1-6alkyl or di(Ar1)C1-6alkyl, wherein each C1-6alkyl group is optionally substituted with hydroxy, C1-4alkyloxy, oxo or a ketalized oxo substituent; R2 is Ar2, Ar2C1-6alkyl, Het1 or Het1C1-6alkyl; R3 is hydrogen or C1-6alkyl; L is hydrogen; Ar3; C1-6alkyl; C1-6alkyl substituted with 1 or 2 substituents selected from hydroxy, C1-6alkyloxy, Ar3, Ar3C1-6alkyloxy and Het2; C3-6alkenyl; Ar3C3-6alkenyl; di(Ar3)C3-6alkenyl or a radical of formula (a-1), (a-2), (a-3), (a-4) or (a-5); Ar1, Ar2 and Ar3 are each phenyl or substituted phenyl; Het1 and Het2 are each monocyclic or a bicyclic heterocycle; as substance-P antagonists; their preparation, compositions containing them and their use as a medicine.
(FR) L'invention concerne des composés de la formule (I), les formes N-oxyde de ceux-ci, les sels d'addition acceptables sur le plan pharmacologique ainsi que les formes stéréo-isomères de ces composés. Dans cette formule, n vaut 0, 1 ou 2; m vaut 1 ou 2, à condition que si m vaut 2, n vaille 1, p vaut 1 ou 2; =Q représente =O ou =NR3; X représente une liaison covalente ou un radical bivalent de formule -O-, -S-, -NR3-; R1 représente Ar1, Ar1alkyle C1-6 ou di(Ar1)alkyle C1-6, où chaque groupe alkyle C1-6 est éventuellement substitué par hydroxy, alkyloxy C1-4, oxo ou un substituant oxo cétalisé; R2 représente Ar2, Ar2alkyle C1-6, Het1 ou Het1alkyle C1-6; R3 représente hydrogène ou alkyle C1-6; L représente hydrogène; Ar3; alkyle C1-6; alkyle C1-6 substitué par un ou deux substituants choisis parmi hydroxy, alkyloxy C1-6, Ar3, Ar3alkyloxy C1-6 et Het2; alcényle C3-6; Ar3alcényle C3-6; di(Ar3)alcényle C3-6 ou un radical de la formule (a-1), (a-2), (a-3), (a-4) ou (a-5); Ar1, Ar2 et Ar3 représentent chacun phényle ou phényle substitué; Het1 et Het2 représentent chacun un hétérocycle monocyclique ou bicyclique. Ces composés constituent des antagonistes de la substance P. On décrit également leur préparation, des compositions les contenant ainsi que leur utilisation en tant que médicament.
Designated States: AL, AM, AU, BA, BB, BG, BR, CA, CN, CU, CZ, EE, GE, HU, IL, IS, JP, KG, KR, LC, LK, LR, LT, LV, MD, MG, MK, MN, MX, NO, NZ, PL, RO, SG, SI, SK, TR, TT, UA, US, UZ, VN
African Regional Intellectual Property Organization (ARIPO) (KE, LS, MW, SD, SZ, UG)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, 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:
CZPV1998-1322NO19981534TR1998/00756MXPA/a/1998/003407SG51984IL123962
EP0862566US6197772USRE037886US6521621JP3073238 JPH11514634
CN1205699CN1438220CA2234096EA199800404DE000069606196PT862566
KR1019990064178NZ321575AU1996074932ID014.632MYPI 96004500TH28678
IN1880/CAL/1996