公开(公告)号：AU652840B2

公开(公告)日：1994-09-08

申请号：AU1900192

申请日：1992-06-09

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: A61K31/55 ,  A61K33/06 ,  A61P37/08 ,  C07D235/00 ,  C07D487/04 ,  C07D519/00

Abstract: The present invention is concerned with novel imidazo[2,1-b][3]benzazepines of formula the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein each of the dotted lines independently represents an optional bond; R represents hydrogen, halo, C1-4alkyl or C1-4alkyloxy; R represents hydrogen, halo, C1-4alkyl or C1-4alkyloxy; R represents hydrogen, C1-4alkyl, ethenyl substituted with hydroxycarbonyl or C1-4alkyloxycarbonyl, C1-4alkyl substituted with hydroxycarbonyl or C1-4alkyloxycarbonyl, hydroxyC1-4alkyl, formyl or hydroxycarbonyl; R represents hydrogen, C1-4alkyl, hydroxyC1-4alkyl, phenyl or halo; R represents hydrogen, C1-4alkyl or halo; L represents hydrogen; C1-6alkyl; C1-6alkyl substituted with one substituent selected from the group consisting of hydroxy, halo, C1-4alkyloxy, hydroxycarbonyl, C1-4alkyloxycarbonyl, C1-4alkyloxycarbonyl-C1-4alkyloxy, hydroxycarbonylC1-4alkyloxy, C1-4alkyloxycarbonylamino, C1-4alkylaminocarbonyl, C1-4alkylaminocarbonylamino, C1-4alkylaminothiocarbonylamino, aryl, aryloxy and arylcarbonyl; C1-6alkyl substituted with both hydroxy and aryloxy; C3-6alkenyl; C3-6alkenyl substituted with aryl; or, L represents a radical of formula -Alk-Y-Het (a-1), -Alk-NH-CO-Het (a-2) or -Alk-Het (a-3); provided that 6,11-dihydro-11-(4-piperidinylidene)-5H-imidazo[2,1-b][3]benzazepine is ecxluded, which are useful antiallergic compounds. Compositions comprising said compounds, methods of using and processes for preparing the same.

公开(公告)号：HRP920155A2

公开(公告)日：1994-08-31

申请号：HRP920155

申请日：1992-06-10

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: A61K33/06 ,  A61K31/55 ,  A61P37/08 ,  C07D235/00 ,  C07D487/04 ,  C07D519/00 ,  C07D487/12

Abstract: The present invention is concerned with novel imidazo[2,1-b][3]benzazepines of formula the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein each of the dotted lines independently represents an optional bond; R represents hydrogen, halo, C1-4alkyl or C1-4alkyloxy; R represents hydrogen, halo, C1-4alkyl or C1-4alkyloxy; R represents hydrogen, C1-4alkyl, ethenyl substituted with hydroxycarbonyl or C1-4alkyloxycarbonyl, C1-4alkyl substituted with hydroxycarbonyl or C1-4alkyloxycarbonyl, hydroxyC1-4alkyl, formyl or hydroxycarbonyl; R represents hydrogen, C1-4alkyl, hydroxyC1-4alkyl, phenyl or halo; R represents hydrogen, C1-4alkyl or halo; L represents hydrogen; C1-6alkyl; C1-6alkyl substituted with one substituent selected from the group consisting of hydroxy, halo, C1-4alkyloxy, hydroxycarbonyl, C1-4alkyloxycarbonyl, C1-4alkyloxycarbonyl-C1-4alkyloxy, hydroxycarbonylC1-4alkyloxy, C1-4alkyloxycarbonylamino, C1-4alkylaminocarbonyl, C1-4alkylaminocarbonylamino, C1-4alkylaminothiocarbonylamino, aryl, aryloxy and arylcarbonyl; C1-6alkyl substituted with both hydroxy and aryloxy; C3-6alkenyl; C3-6alkenyl substituted with aryl; or, L represents a radical of formula -Alk-Y-Het (a-1), -Alk-NH-CO-Het (a-2) or -Alk-Het (a-3); provided that 6,11-dihydro-11-(4-piperidinylidene)-5H-imidazo[2,1-b][3]benzazepine is ecxluded, which are useful antiallergic compounds. Compositions comprising said compounds, methods of using and processes for preparing the same.

公开(公告)号：HU9303553D0

公开(公告)日：1994-04-28

申请号：HU9303553

申请日：1992-06-09

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: A61K31/55 ,  A61K33/06 ,  A61P37/08 ,  C07D235/00 ,  C07D487/04 ,  C07D519/00

Abstract: The present invention is concerned with novel imidazo[2,1-b][3]benzazepines of formula the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein each of the dotted lines independently represents an optional bond; R represents hydrogen, halo, C1-4alkyl or C1-4alkyloxy; R represents hydrogen, halo, C1-4alkyl or C1-4alkyloxy; R represents hydrogen, C1-4alkyl, ethenyl substituted with hydroxycarbonyl or C1-4alkyloxycarbonyl, C1-4alkyl substituted with hydroxycarbonyl or C1-4alkyloxycarbonyl, hydroxyC1-4alkyl, formyl or hydroxycarbonyl; R represents hydrogen, C1-4alkyl, hydroxyC1-4alkyl, phenyl or halo; R represents hydrogen, C1-4alkyl or halo; L represents hydrogen; C1-6alkyl; C1-6alkyl substituted with one substituent selected from the group consisting of hydroxy, halo, C1-4alkyloxy, hydroxycarbonyl, C1-4alkyloxycarbonyl, C1-4alkyloxycarbonyl-C1-4alkyloxy, hydroxycarbonylC1-4alkyloxy, C1-4alkyloxycarbonylamino, C1-4alkylaminocarbonyl, C1-4alkylaminocarbonylamino, C1-4alkylaminothiocarbonylamino, aryl, aryloxy and arylcarbonyl; C1-6alkyl substituted with both hydroxy and aryloxy; C3-6alkenyl; C3-6alkenyl substituted with aryl; or, L represents a radical of formula -Alk-Y-Het (a-1), -Alk-NH-CO-Het (a-2) or -Alk-Het (a-3); provided that 6,11-dihydro-11-(4-piperidinylidene)-5H-imidazo[2,1-b][3]benzazepine is ecxluded, which are useful antiallergic compounds. Compositions comprising said compounds, methods of using and processes for preparing the same.

公开(公告)号：NO934493A

公开(公告)日：1994-01-04

申请号：NO934493

申请日：1993-12-09

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  DIELS GASTON STANISLAS MARCELL ,  LEENAERTS JOSEPH ELISABETH ,  COOYMANS LUDWIG PAUL

IPC: A61K31/55 ,  A61P37/08 ,  C07D235/00 ,  C07D487/14 ,  C07D491/14 ,  C07D491/147 ,  C07D495/14 ,  C07D519/00 ,  C07D

CPC classification number: C07D487/14 ,  C07D491/14 ,  C07D495/14

公开(公告)号：ZA924327B

公开(公告)日：1993-12-13

申请号：ZA924327

申请日：1992-06-12

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  DIELS GASTON STANISLAS MARCELL ,  LEENAERTS JOSEPH ELISABETH ,  COOYMANS LUDWIG PAUL

IPC: A61K31/55 ,  A61P37/08 ,  C07D235/00 ,  C07D487/14 ,  C07D491/14 ,  C07D491/147 ,  C07D495/14 ,  C07D519/00 ,  C07D ,  A61K ,  C07B

Abstract: The present invention is concerned with novel imidazo[1,2-a](pyrrolo, thieno or furano)[3,2-d]azepines of formula the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein each of the dotted lines independently represents an optional bond; R represents hydrogen, C1-4alkyl, halo, ethenyl substituted with hydroxycarbanyl or C1-4alkyloxycarbonyl, hydroxyC1-4alkyl, formyl, hydroxycarbonyl or hydroxycarbonylC1-4alkyl; R represents hydrogen, C1-4alkyl, ethenyl substituted with hydroxycarbonyl or C1-4alkyloxycarbonyl, C1-4alkyl substituted with hydroxycarbonyl or C1-4alkyloxycarbonyl, hydroxyC1-4alkyl, formyl or hydroxycarbonyl; R represents hydrogen, C1-4alkyl, hydroxyC1-4alkyl, phenyl or halo; L represents hydrogen; C1-6alkyl; C1-6alkyl substituted with one substituent selected from the group consisting of hydroxy, halo, C1-4alkyloxy, hydroxycarbonyl, C1-4alkyloxycarbonyl, C1-4alkyloxycarbonylC1-4alkyloxy, hydroxycarbonylC1-4alkyloxy, C1-4alkyloxycarbonylamino, C1-4alkylaminocarbonyl, C1-4alkylaminocarbonylamino, C1-4alkylaminothiocarbonylamino, aryl, aryloxy and arylcarbonyl; C1-6alkyl substituted with both hydroxy and aryloxy; C3-6alkenyl; C3-6alkenyl substituted with aryl; L represents a radical of formula -Alk-Y-Het (a-1), -Alk-NH-CO-Het (a-2) or -Alk-Het (a-3); which are useful antiallergic compounds. Compositions comprising said compounds, methods of using, and processes for preparing the same.

公开(公告)号：ZA924326B

公开(公告)日：1993-12-13

申请号：ZA924326

申请日：1992-06-12

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: A61K20060101 ,  C07B20060101 ,  C07D20060101 ,  C07D487/04 ,  C07D513/04 ,  C07D ,  A61K ,  C07B

公开(公告)号：FI935557A0

公开(公告)日：1993-12-10

申请号：FI935557

申请日：1993-12-10

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  DIELS GASTON STANISLAS MARCELL ,  LEENAERTS JOSEPH ELISABETH ,  COOYMANS LUDWIG PAUL

IPC: A61K31/55 ,  A61P37/08 ,  C07D235/00 ,  C07D487/14 ,  C07D491/14 ,  C07D491/147 ,  C07D495/14 ,  C07D519/00 ,  C07D

Abstract: The present invention is concerned with novel imidazo[1,2-a](pyrrolo, thieno or furano)[3,2-d]azepines of formula the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein each of the dotted lines independently represents an optional bond; R represents hydrogen, C1-4alkyl, halo, ethenyl substituted with hydroxycarbanyl or C1-4alkyloxycarbonyl, hydroxyC1-4alkyl, formyl, hydroxycarbonyl or hydroxycarbonylC1-4alkyl; R represents hydrogen, C1-4alkyl, ethenyl substituted with hydroxycarbonyl or C1-4alkyloxycarbonyl, C1-4alkyl substituted with hydroxycarbonyl or C1-4alkyloxycarbonyl, hydroxyC1-4alkyl, formyl or hydroxycarbonyl; R represents hydrogen, C1-4alkyl, hydroxyC1-4alkyl, phenyl or halo; L represents hydrogen; C1-6alkyl; C1-6alkyl substituted with one substituent selected from the group consisting of hydroxy, halo, C1-4alkyloxy, hydroxycarbonyl, C1-4alkyloxycarbonyl, C1-4alkyloxycarbonylC1-4alkyloxy, hydroxycarbonylC1-4alkyloxy, C1-4alkyloxycarbonylamino, C1-4alkylaminocarbonyl, C1-4alkylaminocarbonylamino, C1-4alkylaminothiocarbonylamino, aryl, aryloxy and arylcarbonyl; C1-6alkyl substituted with both hydroxy and aryloxy; C3-6alkenyl; C3-6alkenyl substituted with aryl; L represents a radical of formula -Alk-Y-Het (a-1), -Alk-NH-CO-Het (a-2) or -Alk-Het (a-3); which are useful antiallergic compounds. Compositions comprising said compounds, methods of using, and processes for preparing the same.

公开(公告)号：ZA902664B

公开(公告)日：1991-12-24

申请号：ZA902664

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

Abstract: Hydroxylalkylfuranyl 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-, -CH=CH-CH=N-, -N=CH-N=CH- or -CH=N-CH=N- ; D is C1-4alkanediyl ; R is hydrogen, C1-6alkyl, arylC1-6alkyl or C1-6alkylcarbonyl ; R and R are hydrogen or C1-6alkyl ; n is 0, 1 or 2 ; B is NR , O, S, SO2 or CH2; R is hydrogen, C1-6alkyl, C3-6cycloalkyl or arylC1-6alkyl ; L is hydrogen, C1-12alkyl, C3-6cycloalkyl, C3-6alkenyl optionally substituted with aryl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, arylcarbonyl, arylC1-6alkyloxycarbonyl, C1-6alkylsulfonyl, arylsulfonyl, or a radical of formula -Alk-R , -Alk-Y-R , -Alk-Z -C(=X)-Z -R , or -CH2-CHOH-CH2-O-R , the acid addition salts and stereochemically isomeric forms thereof, said compounds having antiallergic activity. Pharmaceutical compositions containing such compounds as an active ingredient; methods of preparing said compounds and pharmaceutical compositions.

公开(公告)号：NZ233088A

公开(公告)日：1991-10-25

申请号：NZ23308890

申请日：1990-03-26

Applicant: JANSSEN PHARMACEUTICA NV

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

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 ,  C07D409/14 ,  C07D473/34 ,  A61K31/34 ,  A61K31/52 ,  A61K31/54 ,  A61K31/505

Abstract: Hydroxylalkylfuranyl 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-, -CH=CH-CH=N-, -N=CH-N=CH- or -CH=N-CH=N- ; D is C1-4alkanediyl ; R is hydrogen, C1-6alkyl, arylC1-6alkyl or C1-6alkylcarbonyl ; R and R are hydrogen or C1-6alkyl ; n is 0, 1 or 2 ; B is NR , O, S, SO2 or CH2; R is hydrogen, C1-6alkyl, C3-6cycloalkyl or arylC1-6alkyl ; L is hydrogen, C1-12alkyl, C3-6cycloalkyl, C3-6alkenyl optionally substituted with aryl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, arylcarbonyl, arylC1-6alkyloxycarbonyl, C1-6alkylsulfonyl, arylsulfonyl, or a radical of formula -Alk-R , -Alk-Y-R , -Alk-Z -C(=X)-Z -R , or -CH2-CHOH-CH2-O-R , the acid addition salts and stereochemically isomeric forms thereof, said compounds having antiallergic activity. Pharmaceutical compositions containing such compounds as an active ingredient; methods of preparing said compounds and pharmaceutical compositions.

公开(公告)号：HU902107D0

公开(公告)日：1990-07-28

申请号：HU210790

申请日：1990-04-06

Applicant: JANSSEN PHARMACEUTICA NV

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

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

Abstract: Hydroxylalkylfuranyl 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-, -CH=CH-CH=N-, -N=CH-N=CH- or -CH=N-CH=N- ; D is C1-4alkanediyl ; R is hydrogen, C1-6alkyl, arylC1-6alkyl or C1-6alkylcarbonyl ; R and R are hydrogen or C1-6alkyl ; n is 0, 1 or 2 ; B is NR , O, S, SO2 or CH2; R is hydrogen, C1-6alkyl, C3-6cycloalkyl or arylC1-6alkyl ; L is hydrogen, C1-12alkyl, C3-6cycloalkyl, C3-6alkenyl optionally substituted with aryl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, arylcarbonyl, arylC1-6alkyloxycarbonyl, C1-6alkylsulfonyl, arylsulfonyl, or a radical of formula -Alk-R , -Alk-Y-R , -Alk-Z -C(=X)-Z -R , or -CH2-CHOH-CH2-O-R , the acid addition salts and stereochemically isomeric forms thereof, said compounds having antiallergic activity. Pharmaceutical compositions containing such compounds as an active ingredient; methods of preparing said compounds and pharmaceutical compositions.