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公开(公告)号:TR9800756T2
公开(公告)日:1998-07-21
申请号:TR9800756
申请日:1996-10-25
Applicant: JANSSEN PHARMACEUTICA NV
Inventor: JANSSENS FRANS EDUARD , SOMMEN FRANCOIS MARIA , SURLERAUX DOMINIQUE LOUIS NEST , LEENAERTS JOSEPH ELISABETH , ROOSBROECK YVES EMIEL MARIA VA
IPC: C07D401/04 , A61K31/00 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/498 , A61P1/08 , A61P23/00 , A61P29/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D211/58 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/14
CPC classification number: C07D401/12 , C07D211/58 , C07D405/12 , C07D413/14 , C07D417/12 , C07D471/04 , Y02P20/55
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公开(公告)号:TR199800756T2
公开(公告)日:1998-07-21
申请号:TR9800756
申请日:1996-10-25
Applicant: JANSSEN PHARMACEUTICA NV
Inventor: JANSSENS FRANS EDUARD , SOMMEN FRANCOIS MARIA , SURLERAUX DOMINIQUE LOUIS NEST , LEENAERTS JOSEPH ELISABETH , ROOSBROECK YVES EMIEL MARIA VA
IPC: C07D401/04 , A61K31/00 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/498 , A61P1/08 , A61P23/00 , A61P29/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D211/58 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/14
Abstract: This invention concerns the compounds of formulathe N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, as substance-P antagonists; their preparation, compositions containing them and their use as a medicine.
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公开(公告)号:ZA9610885B
公开(公告)日:1998-06-23
申请号:ZA9610885
申请日:1996-12-23
Applicant: JANSSEN PHARMACEUTICA NV
Inventor: JANSSENS FRANS EDUARD , SOMMEN FRANCOIS MARIA , SURLERAUX DOMINIQUE LOUIS NEST , ROOSBROECK YVES EMILE MARIA VA
IPC: A61K31/00 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/454 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/4965 , A61K31/497 , A61K31/498 , A61K31/505 , A61K31/506 , A61P43/00 , C07D211/44 , C07D211/46 , C07D211/52 , C07D211/58 , C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/10 , C07D491/10 , C07D491/113 , C07D , A61K
Abstract: The present invention concerns compounds of formulathe N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric 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 0, 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 of formula -O-CH2-CH2-O- or -O-CH2-CH2-CH2-O-; R2 is Ar2; Ar2C1-6alkyl; Het or HetC1-6alkyl; R3 is hydrogen or C1-6alkyl; R4 is hydrogen; C1-4alkyl; C1-4aklyloxyC1-4alkyl; hydroxyC1-4alkyl; carboxyl; C1-4aklyloxycarbonyl or Ar3; R5 is hydrogen; hydroxy; Ar3; Ar3C1-6alkyloxy; di(Ar3)C1-6alkyloxy; Ar3C1-6alkylthio; di(Ar3)C1-6alkylthio; Ar3C1-6alkylsulfoxy; di(Ar3)C1-6alkylsulfoxy; Ar3C1-6alkylsulfonyl; di(Ar3)C1-6alkylsulfonyl; -NR7R8; C1-6alkyl substituted with -NR7R8; or a radical of formula (a-1) or (a-2); R4 and R5 may also be taken together; R6 is hydrogen; hydroxy; C1-6alkyloxy; C1-6alkyl or Ar3C1-6alkyl; Ar1, Ar2 and Ar3 are phenyl or
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公开(公告)号:NO982404D0
公开(公告)日:1998-05-27
申请号:NO982404
申请日:1998-05-27
Applicant: JANSSEN PHARMACEUTICA NV
Inventor: JANSSENS FRANS EDUARD , SOMMEN FRANCOIS MARIA , SURLERAUX DOMINIQUE LOUIS NEST , ROOSBROECK YVES EMIEL MARIA VA
IPC: A61K31/00 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/454 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/4965 , A61K31/497 , A61K31/498 , A61K31/505 , A61K31/506 , A61P43/00 , C07D211/44 , C07D211/46 , C07D211/52 , C07D211/58 , C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/10 , C07D491/10 , C07D491/113 , C07D
Abstract: The present invention concerns compounds of formulathe N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric 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 0, 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 of formula -O-CH2-CH2-O- or -O-CH2-CH2-CH2-O-; R2 is Ar2; Ar2C1-6alkyl; Het or HetC1-6alkyl; R3 is hydrogen or C1-6alkyl; R4 is hydrogen; C1-4alkyl; C1-4aklyloxyC1-4alkyl; hydroxyC1-4alkyl; carboxyl; C1-4aklyloxycarbonyl or Ar3; R5 is hydrogen; hydroxy; Ar3; Ar3C1-6alkyloxy; di(Ar3)C1-6alkyloxy; Ar3C1-6alkylthio; di(Ar3)C1-6alkylthio; Ar3C1-6alkylsulfoxy; di(Ar3)C1-6alkylsulfoxy; Ar3C1-6alkylsulfonyl; di(Ar3)C1-6alkylsulfonyl; -NR7R8; C1-6alkyl substituted with -NR7R8; or a radical of formula (a-1) or (a-2); R4 and R5 may also be taken together; R6 is hydrogen; hydroxy; C1-6alkyloxy; C1-6alkyl or Ar3C1-6alkyl; Ar1, Ar2 and Ar3 are phenyl or
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公开(公告)号:NO982124D0
公开(公告)日:1998-05-11
申请号:NO982124
申请日:1998-05-11
Applicant: JANSSEN PHARMACEUTICA NV
Inventor: JANSSENS FRANS EDUARD , LEENAERTS JOSEPH ELISABETH , SOMMEN FRANCOIS MARIA , SURLERAUX DOMINIQUE LOUIS NEST
IPC: A61K31/00 , A61K31/445 , A61K31/47 , A61K31/4738 , A61K31/4745 , A61K31/5365 , A61K31/55 , A61K31/553 , A61K45/00 , A61P31/00 , A61P31/06 , A61P33/00 , A61P33/02 , A61P33/04 , A61P33/06 , A61P35/00 , A61P35/02 , A61P43/00 , C07D471/04 , C07D487/04 , C07D487/14 , C07D491/147 , C07D495/14 , C07D498/04 , C07D498/14 , C07D
Abstract: This invention concerns the compounds of formulathe N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dotted line is an optional bond; n is 1 or 2; R1 is hydrogen; halo; formyl; C1-4alkyl optionally substituted with hydroxy, C1-4alkyloxy, C1-4alkylcarbonyloxy, imidazolyl, thiazolyl or oxazolyl; or a radical of formula -X-COOR5, -X-CONR6R7 or -X-COR10 wherein -X- is a direct bond, C1-4alkanediyl or C2-6alkenediyl; R5 is hydrogen, C1-12alkyl, Ar, Het, C1-6alkyl substituted with C1-4alkyloxy, aryl or heteroaryl; R6 and R7 each independently are hydrogen or C1-4alkyl; R2 is hydrogen, halo, C1-4alkyl, hydroxyC1-4alkyl, C1-4alkyloxycarbonyl, carboxyl, formyl or phenyl; R3 is hydrogen, C1-4alkyl or C1-4alkyloxy; R4 is hydrogen, halo, C1-4alkyl, C1-4alkyloxy or haloC1-4alkyl; Z is -CH2-, -CH2-CH2-, -CH=CH-, -CHOH-CH2-, -O-CH2-, -C(=O)-CH2- or -C(=NOH)-CH2-; -A-B- is a bivalent radical; A1 is a direct bond, optionally substituted C1-6alkanediyl, C1-6alkanediyl-oxy-C1-6alkanediyl, carbonyl, C1-6alkanediylcarbonyl, optionally substituted C1-6alkanediyloxy; A2 is a direct bond or C1-6alkanediyl; and Q is aryl. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for inhibiting or reversing the effects of multidrug resistance.
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公开(公告)号:ID16375A
公开(公告)日:1997-09-25
申请号:ID970888
申请日:1997-03-19
Applicant: JANSSEN PHARMACEUTICA NV
Inventor: JANSSENS FRANS EDUARD , LEENAERTS JOSEPH ELISABETH , SOMMEN FRANCOIS MARIA , SURLERAUX DOMINIQUE LOUIS NEST
IPC: A61K31/00 , A61K31/445 , A61K31/47 , A61K31/4738 , A61K31/4745 , A61K31/5365 , A61K31/55 , A61K31/553 , A61K45/00 , A61P31/00 , A61P31/06 , A61P33/00 , A61P33/02 , A61P33/04 , A61P33/06 , A61P35/00 , A61P35/02 , A61P43/00 , C07D471/04 , C07D487/04 , C07D487/14 , C07D491/147 , C07D495/14 , C07D498/04 , C07D498/14 , C07D235/02
Abstract: This invention concerns the compounds of formulathe N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dotted line is an optional bond; n is 1 or 2; R1 is hydrogen; halo; formyl; C1-4alkyl optionally substituted with hydroxy, C1-4alkyloxy, C1-4alkylcarbonyloxy, imidazolyl, thiazolyl or oxazolyl; or a radical of formula -X-COOR5, -X-CONR6R7 or -X-COR10 wherein -X- is a direct bond, C1-4alkanediyl or C2-6alkenediyl; R5 is hydrogen, C1-12alkyl, Ar, Het, C1-6alkyl substituted with C1-4alkyloxy, aryl or heteroaryl; R6 and R7 each independently are hydrogen or C1-4alkyl; R2 is hydrogen, halo, C1-4alkyl, hydroxyC1-4alkyl, C1-4alkyloxycarbonyl, carboxyl, formyl or phenyl; R3 is hydrogen, C1-4alkyl or C1-4alkyloxy; R4 is hydrogen, halo, C1-4alkyl, C1-4alkyloxy or haloC1-4alkyl; Z is -CH2-, -CH2-CH2-, -CH=CH-, -CHOH-CH2-, -O-CH2-, -C(=O)-CH2- or -C(=NOH)-CH2-; -A-B- is a bivalent radical; A1 is a direct bond, optionally substituted C1-6alkanediyl, C1-6alkanediyl-oxy-C1-6alkanediyl, carbonyl, C1-6alkanediylcarbonyl, optionally substituted C1-6alkanediyloxy; A2 is a direct bond or C1-6alkanediyl; and Q is aryl. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for inhibiting or reversing the effects of multidrug resistance.
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公开(公告)号:CA2234096C
公开(公告)日:2005-06-14
申请号:CA2234096
申请日:1996-10-25
Applicant: JANSSEN PHARMACEUTICA NV
Inventor: SOMMEN FRANCOIS MARIA , VAN ROOSBROECK YVES EMIEL MARI , JANSSENS FRANS EDUARD , LEENAERTS JOSEPH ELISABETH , SURLERAUX DOMINIQUE LOUIS NEST
IPC: C07D401/04 , A61K31/00 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/498 , A61P1/08 , A61P23/00 , A61P29/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D211/58 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/14 , C07D403/04 , C07D207/14 , C07D403/14 , A61K31/435 , A61K31/55
Abstract: This invention concerns the compounds of formula (I), the 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 substitut ed with 1 or 2 substituents selected from hydroxy, C1-6alkyloxy, Ar3, Ar3C1-6alkyloxy and Het2; C3-6alkenyl; Ar3C3-6alkenyl; di(Ar3)C3-6alken yl 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.
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公开(公告)号:CZ291794B6
公开(公告)日:2003-05-14
申请号:CZ132298
申请日:1996-10-25
Applicant: JANSSEN PHARMACEUTICA NV
Inventor: JANSSENS FRANS EDUARD , SOMMEN FRANCOIS MARIA , SURLERAUX DOMINIQUE LOUIS NEST , LEENAERTS JOSEPH ELISABETH , VAN ROOSBROECK YVES EMIEL MARI
IPC: C07D401/04 , A61K31/00 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/498 , A61P1/08 , A61P23/00 , A61P29/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D211/58 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/14 , A61K31/445 , A61K31/415 , A61P11/00 , A61P25/00 , A61P17/00
Abstract: In the present invention there are disclosed 1-(1,2-disubstituted piperidinyl)-4-substituted piperazine derivatives of the general formula I, their N-oxide forms, their pharmaceutically acceptable addition salts and their stereoisomeric forms, wherein n is 0, 1 or 2; m is 1 or 2, whereby when m is 2 then n is 1; p is 1 or 2; =Q represents =O or =NRe3; X represents a covalent bond or -O-, -S-, -NRe3-; Re1 denotes Are1, Are1alkyl having 1 to 6 carbon atoms or di(Are1)alkyl containing 1 to 6 carbon atoms, where each alkyl group containing 1 to 6 carbon atoms can be optionally substituted with a group comprising hydroxy, alkyloxy with 1 to 4 carbon atoms, oxo or a ketalyzed oxo substituent; Re2 represents Are2, Are2alkyl having 1 to 6 carbon atoms, Hete1 or Hete1alkyl having 1 to 6 carbon atoms; Re3 denotes hydrogen or alkyl containing 1 to 6 carbon atoms; L represents hydrogen, Are3, alkyl containing 1 to 6 carbon atoms, alkyl having 1 to 6 carbon atoms and being substituted with 1 or 2 substituents being selected from the group comprising hydroxy, alkyloxy having 1 to 6 carbon atoms, Are3, Are3alkyloxy having 1 to 6 carbon atoms and Hete2; alkenyl having 3 to 6 carbon atoms; Are3alkenyl having 3 to 6 carbon atoms, di(Are3)alkenyl having 3 to 6 carbon atoms or a radical of the general formula (a-1), (a-2), (a-3), (a-4) or (a-5); Are1, Are2 and Are3 each represent phenyl or a substituted phenyl; Hete1 and Hete2 each represent a monocyclic or bicyclic heterocycle. The above described compounds exhibit antagonistic activity on the substance-P. Claimed is also a process of their preparation, pharmaceutical compositions in which they are comprised and their use as medicaments.
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公开(公告)号:NO313291B1
公开(公告)日:2002-09-09
申请号:NO982406
申请日:1998-05-27
Applicant: JANSSEN PHARMACEUTICA NV
Inventor: JANSSENS FRANS EDUARD , SOMMEN FRANCOIS MARIA , SURLERAUX DOMINIQUE LOUIS NEST , LEENAERTS JOSEPH ELISABETH
IPC: A61K31/00 , A61K31/415 , A61K31/435 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/444 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/454 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/4965 , A61K31/497 , A61K31/498 , A61K31/55 , A61P1/00 , A61P9/00 , A61P11/00 , A61P17/00 , A61P25/00 , A61P25/04 , A61P29/00 , A61P35/00 , A61P37/00 , A61P43/00 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
Abstract: N-heterocyclic compounds of formula (I), and their N-oxides, salts and isomers, are new. n = 0, 1 or 2; m = 1 or 2, provided that when m is 2, then n is 1; X = a bond, O, S or NR3; Q = O or NR3; R1 = Ar1, Ar1(1-6C alkyl) or di(Ar1)(1-6C alkyl), where the 1-6C alkyl groups are optionally substituted by OH, TO, oxo or a ketalised oxo substituent of formula OCH2CH2O or OCH2CH2CH2O; R2 = Ar2, Ar2(1-6C alkyl), Het or Het(1-6C alkyl); L = a group of formula (i) or (ii); p = 0, 1 or 2; Y, depending on whether the optional second bond is present or not, is (i) a bivalent radical of formula CH2, CH(OH), C(O), O, S, SO, SO2, NR3, CH2NR3 or CONR3, or (ii) a trivalent radical of formula CH; A=B is a bivalent radical of formula CH=CH, N=CH or CH=N; R3 = H or R; R4 = H, R, 3-7C cycloalkyl, Alk-R7 or Alk-Z-R8; Alk = 1-6C alkanediyl; Z = O, S or NR3; R7 = Ph (optionally substituted by 1-2 halo, R or RO); furanyl (optionally substituted by 1-2 R or hydroxy(1-6C alkyl)); thienyl (optionally substituted by 1-2 halo or R); oxazolyl, thiazolyl or pyridinyl (all optionally substituted by 1-2 R); R8 = R (optionally substituted by OH, COOH or COOR); R5 = H, halo, OH or RO; R6 = H, R or Ar1(1-6 alkyl); Ar1 = Ph (optionally substituted by 1-3 halo, T, T', CN, CONH2, TO or T'O); Ar2 = naphthalenyl, or Ph (optionally substituted by 1-3 OH, halo, CN, NO2, NH2, NHT, N(T)2, T, T', TO, T'O, COOH, COOT, CONH2, CONHT or CON(T)2); Het = pyrrolyl, pyrazolyl, imidazolyl, furanyl, thienyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, quinolinyl, quinoxalinyl, indolyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl, benzisothiazolyl, benzofuranyl or benzothienyl (all optionally substituted on carbon by 1-2 halo, T or mono-, di- or tri(halo)methyl); T, T', R, = 1-4C alkyl, halo(1-4C alkyl), 1-6C alkyl respectively.
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公开(公告)号:CY2177B1
公开(公告)日:2002-08-23
申请号:CY0000030
申请日:2000-06-16
Applicant: JANSSEN PHARMACEUTICA NV
Inventor: JANSSENS FRANS EDUARD , SOMMEN FRANCOIS MARIA , SURLERAUX DOMINIQUE LOUIS NEST , LEENAERTS JOSEPH ELISABETH , ROOSBROECK VAN YVES EMIEL MARI
IPC: C07D401/04 , A61K31/00 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/498 , A61P1/08 , A61P23/00 , A61P29/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D211/58 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/14
Abstract: This invention concerns the compounds of formulathe N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, as substance-P antagonists; their preparation, compositions containing them and their use as a medicine.
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