公开(公告)号：NO982406L

公开(公告)日：1998-08-24

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.

公开(公告)号：ZA9609090B

公开(公告)日：1998-04-29

申请号：ZA9609090

申请日：1996-10-29

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 ,  C07D ,  A61K

CPC classification number: C07D401/12 ,  C07D211/58 ,  C07D405/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  Y02P20/55

公开(公告)号：CA2237594A1

公开(公告)日：1997-09-25

申请号：CA2237594

申请日：1997-03-11

Applicant: JANSSEN PHARMACEUTICA NV

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

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 formula (I), the 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, C14alkyloxy, 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, C14alkyloxy 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 C16alkanediyloxy; 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：CA2238816A1

公开(公告)日：1997-07-10

申请号：CA2238816

申请日：1996-12-20

Applicant: JANSSEN PHARMACEUTICA NV

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

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: This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the 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; X is a covalent bond or a bivalent radical of formula -O-, -S-, NR3-; =Q is =O or =NR3; R1 is Ar1, Ar1C1-6alkyl or di(Ar1)C1-6alkyl wherein the C1-6alkyl group is optionally substituted; R2 is Ar2, Ar2C1-6alkyl, Het or HetC1-6alkyl; L is a benzimidazole or imidazopyridine derivative of formula (A) or (B); Ar1 is optionally substituted phenyl; Ar2 is naphtalenyl or optionally substituted phenyl; and Het is an optionally substituted monocyclic or bicyclic heterocycle; as substance P antagonists; their preparation, compositions containing them and their use as a medicine.

公开(公告)号：PL192397B1

公开(公告)日：2006-10-31

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: C07D211/44 ,  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 ,  C07D211/46 ,  C07D211/52 ,  C07D211/58 ,  C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/10 ,  C07D491/10 ,  C07D491/113

公开(公告)号：CZ294199B6

公开(公告)日：2004-10-13

申请号：CZ186698

申请日：1996-12-20

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 ,  A61K31/4355

Abstract: The present invention relates to tachykinin antagonists of the general formula I, N-oxide forms, 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; X is a covalent bond or a bivalent radical of the formula -O-, -S-, -NRe3-; =Q is =O or =NRe3; Re1 is Are1, Are1C1-6alkyl or di(Are1)C1-6alkyl wherein the alkyl group having 1 to 6 carbon atoms is an optionally substituted; Re2 represents Are2, Are2C1-6alkyl, Het or HetC1-6alkyl; L denotes a benzimidazole or imidazopyridine derivative of the general formula (A) or (B); Are1 represents optionally substituted phenyl; Are2 denotes naphthyl or optionally substituted phenyl; and Het represents an optionally substituted monocyclic or bicyclic heterocycle; as substance P antagonists; their preparation, compositions containing them and their use as a medicament.

公开(公告)号：CZ294060B6

公开(公告)日：2004-09-15

申请号：CZ152998

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: In the present invention, there is disclosed a condensed imidazole derivative of the general formula I being especially useful for inhibiting or reversing the effects of multidrug resistance.

公开(公告)号：NO310232B1

公开(公告)日：2001-06-11

申请号：NO981534

申请日：1998-04-03

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 ,  A61K31/395

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：PT862566E

公开(公告)日：2000-06-30

申请号：PT96937248

申请日：1996-10-25

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  SOMMEN FRANCOIS MARIA ,  LEENAERTS JOSEPH ELISABETH ,  SURLERAUX DOMINIQUE LOUIS NEST ,  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.

公开(公告)号：AT188691T

公开(公告)日：2000-01-15

申请号：AT96937248

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.