公开(公告)号：PL208593B1

公开(公告)日：2011-05-31

申请号：PL36326402

申请日：2002-02-13

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANDRES-GIL JOSE IGNACIO ,  FERNANDEZ-GADEA FRANCISCO JAVIER ,  ALCAZAR-VACA MANUEL JESUS ,  CID-NUŇEZ JOSĒ MARIA ,  PASTOR-FERNANDEZ JOAQUIN ,  MEGENS ANTONIUS ADRIANUS HENDRIKUS PETRUS ,  HEYLEN GODELIEVE IRMA CHRISTINE MARIA ,  LANGLOIS XAVIER JEAN MICHEL ,  BAKKER MARGARETHA HENRICA MARIA ,  STECKLER THOMAS HORST WOLFGANG

IPC: C07D498/04 ,  A61K31/454 ,  A61K31/495 ,  A61K31/496 ,  A61K31/538 ,  A61P3/04 ,  A61P25/00 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  C07D261/20 ,  C07D498/14 ,  C07D519/00

公开(公告)号：CA2410233C

公开(公告)日：2011-01-25

申请号：CA2410233

申请日：2001-06-13

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： VAN EMELEN KRISTOF ,  DE BRUYN MARCEL FRANS LEOPOLD ,  ALCAZAR-VACA MANUEL JESUS ,  ANDRES-GIL JOSE IGNACIO ,  FERNANDEZ-GADEA FRANCISCO JAVIER ,  MATESANZ-BALLESTEROS MARIA ENCARNACION ,  BARTOLOME-NEBREDA JOSE MANUEL

IPC: C07D491/056 ,  C07D491/06 ,  A61K31/435 ,  A61K31/436 ,  A61K31/4545 ,  A61K31/513 ,  A61K31/5383 ,  A61P1/00 ,  A61P1/14 ,  C07D411/04 ,  C07D491/04 ,  C07D491/052 ,  C07D497/04 ,  C07D498/04

Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharma-ceutically acceptable acid addition salt thereof, wherein -a1=a2-a3=a4- is a bivalent radical wherein one or two of a1 to a4 are nitrogen and the remaining a1 to a4 are -CH=; -Z1-Z2- is a bivalent radical; -A- is a bivalent radical of formula -N(R6)-Alk2- or a 5, 6 or 7-membered saturated heterocycle containing one or two nitrogen atoms; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R5 is a radical of formula (d-1), (d-2), (d-3), (d-4), (d-5) wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or =NR9; Y2 is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to disturbed fundic accomodation.

公开(公告)号：PT2091938E

公开(公告)日：2011-01-20

申请号：PT07847833

申请日：2007-12-05

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BARTOLOME-NEBREDA JOSE MANUEL ,  JAMES MACDONALD GREGOR ,  ANDRES-GIL JOSE IGNACIO ,  KEYBUS FRANS ALFONS MARIA VAN DEN ,  GOOL MICHIEL LUC MARIA VAN

IPC: C07D401/12 ,  A61K31/501 ,  A61P25/18

公开(公告)号：DE602007010179D1

公开(公告)日：2010-12-09

申请号：DE602007010179

申请日：2007-12-05

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： MACDONALD GREGOR JAMES ,  ANDRES-GIL JOSE IGNACIO ,  VAN DEN KEYBUS FRANS ALFONS MARIA ,  BARTOLOME-NEBREDA JOSE MANUEL ,  VAN GOOL MICHIEL LUC MARIA

IPC: C07D401/12 ,  A61K31/501 ,  A61P25/18

公开(公告)号：AT486070T

公开(公告)日：2010-11-15

申请号：AT07847833

申请日：2007-12-05

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： MACDONALD GREGOR JAMES ,  ANDRES-GIL JOSE IGNACIO ,  VAN DEN KEYBUS FRANS ALFONS MARIA ,  BARTOLOME-NEBREDA JOSE MANUEL ,  VAN GOOL MICHIEL LUC MARIA

IPC: C07D401/12 ,  A61K31/501 ,  A61P25/18

Abstract: The present invention relates to 6-(piperidin-4-ylamino)pyridazin-3-carbonitriles of the general formula (I); or a pharmaceutically acceptable salt thereof, or a stereoisomeric form, that are fast dissociating dopamine 2 receptor antagonists, as well as processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.

公开(公告)号：CA2437505C

公开(公告)日：2010-02-09

申请号：CA2437505

申请日：2002-02-13

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANDRES-GIL JOSE IGNACIO ,  FERNANDEZ-GADEA FRANCISCO JAVIER ,  ALCAZAR-VACA MANUEL JESUS ,  CID-NUNEZ JOSE MARIA ,  PASTOR-FERNANDEZ JOAQUIN ,  MEGENS ANTONIUS ADRIANUS HENDRIKUS PETRUS ,  HEYLEN GODELIEVE IRMA CHRISTINE MARIA ,  LANGLOIS XAVIER JEAN MICHEL ,  BAKKER MARGARETHA HENRICA MARIA ,  STECKLER THOMAS HORST WOLFGANG

IPC: C07D498/04 ,  A61K31/454 ,  A61K31/495 ,  A61K31/496 ,  A61K31/538 ,  A61P3/04 ,  A61P25/00 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  C07D261/20 ,  C07D498/14 ,  C07D519/00

Abstract: The invention concerns substituted isoxazolines derivatives according to Formula (I): wherein X = CH2#191, N-R7, S or O, R1, R2 and R3 are certain specific substituents, Pir is an optionally substituted piperidyl or piperazyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S ; a process for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for the treatment of depression and/of anxiety and disorders of body weight. The compounds according to the invention have surprisingly been shown to have a serotonine (5-HT) reuptake inhibitor activity in combination with additional .alpha.2-adrenoceptor antagonist activity and show a strong anti-depressant activity without being sedative. Compounds according to the invention are also suitable for treating patients with anxiety disorders and disorders of body weight. The invention also relates to novel combination of substituted isoxazolines derivatives having anti-depressant activity and/or anxiolytic activity and/or body weight control activity with antidepressants, anxiolytics and/or antipsychotics to improve efficacy and/or onset of action.

公开(公告)号：AU2003262573B2

公开(公告)日：2009-04-23

申请号：AU2003262573

申请日：2003-08-13

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： MEGENS ANTONIUS ADRIANUS HENDRIKUS PETRUS ,  ALCAZAR-VACA MANUEL JESUS ,  ANDRES-GIL JOSE IGNACIO ,  FERNANDEZ-GADEA FRANCISCO JAVIER ,  BAKKER MARGARETHA HENRICA MARIA ,  BARTOLOME-NEBREDA JOSE MANUEL

IPC: C07D498/14 ,  A61K31/42 ,  A61K31/424 ,  A61K31/437 ,  A61P1/14 ,  A61P3/04 ,  A61P15/10 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/32 ,  A61P25/36 ,  A61P43/00 ,  C07D498/12

Abstract: The invention concerns fused heterocyclic isoxazoline derivatives of Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof, more in particular, tetrahydropyranoisoxazole, hexahydroisoxazolopyridine, tetrahydrothiopyrano isoxazole and hexahydrobenzoisoxazole derivatives fused to a heterocyclic ring system via the 6-membered ring of the bicyclic moiety as well as processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for treating depression, anxiety, movement disorders, psychosis, Parkinson's disease and body weight disorders including anorexia nervosa and bulimia, wherein the variables are defined as in Claim 1. The compounds have surprisingly been shown to have selective serotonine (5-HT) reuptake inhibitor activity as well as alpha2-adrenoceptor antagonist activity, compounds according to the invention are also suitable for treatment and/or prophylaxis in diseases where either one of the activities alone or the combination of said activities may be of therapeutic use.

公开(公告)号：CA2216542C

公开(公告)日：2009-01-13

申请号：CA2216542

申请日：1996-03-28

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： FERNANDEZ-GADEA FRANCISCO JAVI ,  DIELS GASTON STANISLAS MARCELL ,  FREYNE EDDY JEAN EDGARD ,  ANDRES-GIL JOSE IGNACIO

IPC: C07D233/70 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4166 ,  A61K31/435 ,  A61K31/495 ,  A61K31/535 ,  A61K31/55 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P37/08 ,  C07D233/32 ,  C07D233/38 ,  C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D405/04 ,  C07D405/06 ,  C07D409/00 ,  C07D413/00 ,  C07D417/00

Abstract: The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable acid or base addition salts and the stereochemically isomeric forms thereof, wherein RI and R2 each independently are hydrogen; CI-6alkyl; difluoromethyl; trifluoromethyl; C3-6cycloalkyl; a saturated 5-, 6- or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; bicyclo[2.2.1]-2--heptenyl; bicyclo[2.2.1]heptanyl; C1-6alkylsulfonyl; arylsulfonyl; or substituted C1-10alkyl; R3 is hydrogen, halo or CI-6alkyloxy; -C-X is a bivalent radical of formula =C=O; =C=CH-R4; =C=N-O-R5; or formula (a-4); Alk is C1-4alkanediyl; -A-B- is a bivalent radical of formula: --CR6=CR7- or -CHR6-CHR7-; L is hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C3-6alkenyl; optionally substituted piperidinyl; C1-6alkylsulfonyl or arylsulfonyl; aryl is optionally substituted phenyl; He t1 is morpholinyl or optionally substituted pyridinyl, -furanyl, -thienyl, -hydroxypyridinyl, -imidazolyl, -thiazolyl, -oxazolyl, - isoquinolinyl, -quinolinonyl, -piperidinyl, -piperazinyl; and Het2 is mor- pholinyl or optionally substituted piperidinyl, -piperazinyl, -pyridinyl, - furanyl or -thienyl; having PDE IV and cytokine inhibiting activity. The invention also relates to processes for preparing the compounds of formu la (I) and pharmaceutical compositions thereof.

公开(公告)号：CA2216546C

公开(公告)日：2009-01-06

申请号：CA2216546

申请日：1996-03-28

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANDRES-GIL JOSE IGNACIO ,  DIELS GASTON STANISLAS MARCELL ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  FREYNE EDDY JEAN EDGARD

IPC: C07D233/70 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4166 ,  A61K31/435 ,  A61K31/495 ,  A61K31/535 ,  A61K31/55 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P37/08 ,  C07D233/32 ,  C07D233/38 ,  C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  C07D413/00 ,  C07D417/00

Abstract: The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceuticlaly acceptable acid or base addition salts and the stereochemically isomeric forms thereof, wherein R1 and R2 each independently are hydrogen; C1-6alkyl; difluoromethyl; trifluoromethyl; C3-6cycloalkyl; a saturated 5-, 6- or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; bicyclo[2.2.1]-2-heptenyl; bicyclo[2.2.1]heptanyl; C1-6alkylsulfonyl; arylsulfonyl; or substituted C1-10alkyl; R3 is hydrogen, halo or C1- 6alkyloxy; R4 is hydrogen; cyano; optionally substituted C1-6alkyl; C1- 6alkyloxycarbonyl or aryl; R5 is hydrogen; cyano; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl or aryl; Y is a direct bond or C 1- 3alkanediyl; -A-B- is a bivalent radical of formula -CR6=CR7- or -CHR6-CHR7-; L is hydrogen; optionally substituted C1-6alkyl; C1- 6alkylcarbonyl; C1-6alkyloxycarbonyl; C1-6alkylsulfonyl or arylsulfonyl; aryl is optionally substituted phenyl; Het is morpholinyl or optionally substituted piperidinyl, -piperazinyl, -pyridinyl; -furanyl or -thienyl; having PDE IV and cytokine inhibiting acitivity. Further, pharmaceutical compositions, preparations and use as a medicine are described.

公开(公告)号：BRPI0516380A

公开(公告)日：2008-09-02

申请号：BRPI0516380

申请日：2005-12-20

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANDRES-GIL JOSE IGNACIO ,  ALCAZAR-VACA MANUEL JESUS ,  PASTOR-FERNANDEZ JOAQUIM ,  DRINKENBURG WILHELMUS HELENA IGNATIUS MARIA ,  LANGLOIS XAVIER JEAN MICHEL ,  SANTANARINA JULEN OYARZABAL ,  VEGA-RAMIRO JUAN-ANTONIO

IPC: C07D249/12 ,  A61K31/41 ,  A61K31/4166 ,  A61K31/4196 ,  A61P25/00 ,  C07D233/70 ,  C07D257/04 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D403/10

Abstract: The present invention concerns substituted triazolone, tetrazolone and imidazolone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1, having selective alpha2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.