公开(公告)号：ZA881660B

公开(公告)日：1989-11-29

申请号：ZA881660

申请日：1988-03-08

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  FRANS EDUARD JANSSENS ,  DIELS GASTON STANISLAS MARCELL ,  GASTON STANISLAS MARCELLA DIEL ,  TORREMANS JOSEPH LEO GHISLANUS ,  JOSEPH LEO GHISLANUS TORREMANS ,  SOMMEN FRANCOIS MARIA ,  FRANCOIS MARIA SOMMEN

IPC: C07D223/12 ,  A61K31/435 ,  A61K31/45 ,  A61K31/47 ,  A61K31/495 ,  A61K31/52 ,  A61K31/522 ,  A61P37/08 ,  A61P43/00 ,  C07D207/14 ,  C07D213/75 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D405/14 ,  C07D471/04 ,  C07D473/00 ,  C07D473/04 ,  C07D473/28 ,  C07D473/30 ,  C07D473/40 ,  C07D487/04 ,  C07D513/04 ,  C07D519/00 ,  A61K ,  C07D

Abstract: Novel 1-alkyl substituted benzimidazole derivatives of formula wherein -A =A -A =A - is a bivalent radical having the formula -CH=CH-CH=CH- (a-1), -N=CH-CH=CH- (a-2), -CH=N-CH=CH- (a-3), -CH=CH-N=CH- (a-4), -CH=CH-CH=N- (a-5), -N=CH-N=CH- (a-6), or -CH=N-CH=N- (a-7); B is NR , CH2, O, S, SO or SO2; L is hydrogen, C1-6alkylcarbonyl, C1-6alkylsulfonyl, C1-6alkyloxycarbonyl, Ar -C1-6alkyloxycarbonyl, Ar -carbonyl, Ar -sulfonyl, C3-6cycloalkyl, C2-6alkenyl optionally substituted with Ar , C1-12alkyl, a radical of formula -Alk-R (b-1), -Alk-Y-R (b-2), -Alk-Z -C(X)-Z -R (b-3), or -CH2-CHOH-CH2-O-R (b-4); the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, which compounds are anti-allergic agents; pharmaceutical compositions containing such compounds as an active ingredient and methods of preparing said compounds and pharmaceutical compositions.

公开(公告)号：ZA8801660B

公开(公告)日：1989-11-29

申请号：ZA8801660

申请日：1988-03-08

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  FRANS EDUARD JANSSENS ,  DIELS GASTON STANISLAS MARCELL ,  GASTON STANISLAS MARCELLA DIEL ,  TORREMANS JOSEPH LEO GHISLANUS ,  JOSEPH LEO GHISLANUS TORREMANS ,  SOMMEN FRANCOIS MARIA ,  FRANCOIS MARIA SOMMEN

IPC: C07D223/12 ,  A61K31/435 ,  A61K31/47 ,  A61K31/495 ,  A61K31/52 ,  A61K31/522 ,  A61P37/08 ,  A61P43/00 ,  C07D207/14 ,  C07D213/75 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D471/04 ,  C07D473/00 ,  C07D473/04 ,  C07D473/28 ,  C07D473/30 ,  C07D473/40 ,  C07D487/04 ,  C07D519/00 ,  A61K ,  C07D

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D471/04 ,  C07D473/00

公开(公告)号：ZA915654B

公开(公告)日：1993-03-31

申请号：ZA915654

申请日：1991-07-18

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  FRANS EDUARD JANSSENS ,  SOMMEN FRANCOIS MARIA ,  FRANCOIS MARIA SOMMEN ,  DIELS GASTON STANISLAS MARCELL ,  GASTON STANISLAS MARCELLA DIEL

IPC: A61K31/445 ,  A61K31/40 ,  A61K31/41 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/427 ,  A61K31/435 ,  A61K31/4427 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/52 ,  A61K31/542 ,  A61K31/55 ,  A61P37/08 ,  A61P43/00 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D417/14 ,  C07D471/04 ,  C07D473/00 ,  C07D473/30 ,  C07D473/40 ,  C07D487/04 ,  C07D513/04 ,  C07D519/00 ,  A61K ,  C07D

公开(公告)号：ZA8804696B

公开(公告)日：1990-03-28

申请号：ZA8804696

申请日：1988-06-30

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  FRANS EDUARD JANSSENS ,  DIELS GASTON STANISLAS MARCELL ,  GASTON STANISLAS MARCELLA DIEL ,  PILLE GEERT MARCEL ESTER ,  GEERT MARCEL ESTER PILLE

IPC: C07D401/12 ,  A61K31/415 ,  A61K31/425 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/55 ,  A61P11/00 ,  A61P27/16 ,  A61P37/08 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/00 ,  C07D519/00 ,  A61K ,  C07B ,  C07D

CPC classification number: C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/00

公开(公告)号：EE9900585A

公开(公告)日：2000-08-15

申请号：EEP9900585

申请日：1998-07-02

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： EDDY JEAN EDGARD FREYNE ,  GUSTAAF MARIA BOECKX ,  WAUWE JEAN PIERRE FRANS VAN ,  GASTON STANISLAS MARCELLA DIEL

IPC: C07D253/06 ,  A61K31/53 ,  A61K51/00 ,  A61K51/04 ,  A61P11/06 ,  A61P17/00 ,  A61P27/02 ,  A61P27/14 ,  A61P37/08 ,  A61P43/00 ,  C07D253/075 ,  C07D403/10 ,  C07D417/10

Abstract: The present invention is concerned with the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p represents 0, 1, 2 or 3; q represents 0, 1, 2, 3 or 4; R 1 represents hydrogen, C 1-6 alkyl, mono- or di(C 1-6 alkyl)aminoC 1-6 alkyloxy, mercapto, C 1-6 alkylthio, C 3-7 cycloalkyl, aryl or C 1-6 alkyl substituted with mono- or di(C 1-6 alkyl)amino, C 1-6 alkyloxy, aryl or Het; R 2 represents cyano or a radical of formula -C(-X)-Y-R 5 ; wherein X represents O or S; Y represents O, S, NR 6 or a direct bond; R 5 represents hydrogen; C 3-7 cycloalkyl; aryl or optionally substituted C 1-6 alkyl; and where Y is a direct bond, R 5 may also be halo or Het; R 3 and R 4 each independently represents halo, haloC 1-6 alkyl, C 1-6 alkyl, hydroxy, C 1-6 alkyloxy, C 1-6 alkylcarbonyloxy, mercapto, C 1-6 alkylthio, C 1-6 alkylsulfonyl, C 1-6 alkylsulfinyl, haloC 1-6 alkylsulfonyl, aryl, cyano, nitro, amino, mono- and di(C 1-6 alkyl)amino or (C 1-6 alkylcarbonyl)amino; aryl represents phenyl or substituted phenyl; and Het represents an optionally substituted heterocycle; in the manufacture of a medicament useful for treating eosinophil-dependent inflammatory diseases. The invention also relates to novel compounds, their preparation and compositions comprising them.

公开(公告)号：ZA884696B

公开(公告)日：1990-03-28

申请号：ZA884696

申请日：1988-06-30

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  FRANS EDUARD JANSSENS ,  DIELS GASTON STANISLAS MARCELL ,  GASTON STANISLAS MARCELLA DIEL ,  PILLE GEERT MARCEL ESTER ,  GEERT MARCEL ESTER PILLE

IPC: C07D401/12 ,  A61K31/415 ,  A61K31/425 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/52 ,  A61K31/55 ,  A61P11/00 ,  A61P27/16 ,  A61P37/08 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/00 ,  C07D473/26 ,  C07D519/00 ,  A61K ,  C07B ,  C07D

公开(公告)号：ZA8804346B

公开(公告)日：1990-02-28

申请号：ZA8804346

申请日：1988-06-17

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  FRANS EDUARD JANSSENS ,  TORREMANS JOSEPH LEO GHISLANUS ,  JOSEPH LEO GHISLANUS TORREMANS ,  DIELS GASTON STANISLAS MARCELL ,  GASTON STANISLAS MARCELLA DIEL

IPC: C07D401/12 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61P37/08 ,  A61P43/00 ,  C07D211/26 ,  C07D235/30 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/06 ,  C07D ,  A61K

CPC classification number: C07D401/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04

公开(公告)号：ZA9002664B

公开(公告)日：1991-12-24

申请号：ZA9002664

申请日：1990-04-05

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  FRANS EDUARD JANSSENS ,  DIELS GASTON STANISLAS MARCELL ,  GASTON STANISLAS MARCELLA DIEL ,  LEENAERTS JOSEPH ELISABETH ,  JOSEPH ELISABETH LEENAERTS

IPC: A61K31/341 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/4409 ,  A61K31/443 ,  A61K31/445 ,  A61K31/4523 ,  A61K31/495 ,  A61K31/55 ,  A61P37/08 ,  A61P43/00 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07D473/00 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00 ,  A61K ,  C07D

CPC classification number: C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07D473/00 ,  C07D513/04

公开(公告)号：ZA8804946B

公开(公告)日：1990-03-28

申请号：ZA8804946

申请日：1988-07-08

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  FRANS EDUARD JANSSENS ,  SOMMEN FRANCOIS MARIA ,  FRANCOIS MARIA SOMMEN ,  TORREMANS JOSEPH LEO GHISLANUS ,  JOSEPH LEO GHISLANUS TORREMANS ,  DIELS GASTON STANISLAS MARCELL ,  GASTON STANISLAS MARCELLA DIEL

IPC: A61K31/435 ,  A61K31/495 ,  A61K31/505 ,  A61K31/52 ,  A61K31/522 ,  A61K31/55 ,  A61P37/08 ,  C07D471/04 ,  C07D473/00 ,  C07D473/06 ,  C07D473/28 ,  C07D473/30 ,  C07D473/40 ,  C07D519/00 ,  A61K ,  C07D

CPC classification number: C07D471/04 ,  A61K31/495 ,  A61K31/505 ,  A61K31/55 ,  C07D473/00

公开(公告)号：ZA884346B

公开(公告)日：1990-02-28

申请号：ZA884346

申请日：1988-06-17

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  FRANS EDUARD JANSSENS ,  TORREMANS JOSEPH LEO GHISLANUS ,  JOSEPH LEO GHISLANUS TORREMANS ,  DIELS GASTON STANISLAS MARCELL ,  GASTON STANISLAS MARCELLA DIEL

IPC: C07D401/12 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61P37/08 ,  A61P43/00 ,  C07D211/26 ,  C07D235/30 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/06 ,  C07D ,  A61K

Abstract: Novel N-(4-piperidinyl) bicyclic condensed 2-imidazolamine derivatives of formula wherein: A =A -A =A is -CH=CH-CH=CH-, -N=CH-CH=CH-, -CH=N-CH=CH-, -CH=CH-N=CH or -CH=CH-CH=N-; R is hydrogen or C1-6alkyl; R is furanyl substituted with C1-6alkyl, pyrazinyl, thiazolyl, or imidazolyl optionally substituted with C1-6alkyl; L is C3-6alkenyl optionally substituted with Ar , or L is a radical of formula -Alk-R , -Alk-O-R , -Alk-N-(R )-R , -Alk-Z-C(=O)-R or -CH2-CH(OH)-CH2-O-R ; the pharmaceutically acceptable acid addition salts and possible stereochemically isomeric forms thereof, which compounds are anti-histaminic agents; pharmaceutical compositions containing such compounds as an active ingredient and methods of preparing said compounds and pharmaceutical compositions.