公开(公告)号：NO310913B1

公开(公告)日：2001-09-17

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

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

公开(公告)号：GR3033154T3

公开(公告)日：2000-08-31

申请号：GR20000400847

申请日：2000-04-04

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

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.

公开(公告)号：EA000909B1

公开(公告)日：2000-06-26

申请号：EA199800404

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

公开(公告)号：ES2143238T3

公开(公告)日：2000-05-01

申请号：ES96937248

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

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.

公开(公告)号：AU709683B2

公开(公告)日：1999-09-02

申请号：AU2026997

申请日：1997-03-11

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

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.

公开(公告)号：HU9900415A2

公开(公告)日：1999-05-28

申请号：HU9900415

申请日：1997-03-11

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

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.

公开(公告)号：BR9611184A

公开(公告)日：1999-03-30

申请号：BR9611184

申请日：1996-10-25

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  SOMMEN FRANCOIS MARIA ,  SURLERAUX DOMINIQUE LOUIS NEST ,  ROOSBROECK YVES EMIEL MARIA VA ,  LEENAERTS JOSEPH ELISABETH

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.

公开(公告)号：PL327441A1

公开(公告)日：1998-12-07

申请号：PL32744196

申请日：1996-12-20

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  SOMMEN FRANCOIS MARIA ,  SURLERAUX DOMINIQUE LOUIS NEST ,  VAN ROOSBROECK YVES EMIEL MARI

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 ,  C07D211/00 ,  C07D401/00 ,  C07D417/00

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

公开(公告)号：TR199801191T2

公开(公告)日：1998-10-21

申请号：TR9801191

申请日：1997-03-11

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

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.

公开(公告)号：TR9801211T2

公开(公告)日：1998-09-21

申请号：TR9801211

申请日：1996-12-20

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

CPC classification number: C07D401/06 ,  C07D211/44 ,  C07D211/46 ,  C07D211/52 ,  C07D211/58 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/10 ,  C07D491/10