中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

492 records (took 0.026 seconds)

    51.
    发明专利
    未知

    公开(公告)号：BR0213325A

    公开(公告)日：2004-10-13

    申请号：BR0213325

    申请日：2002-10-10

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： JANSSENS FRANS EDUARD ,  LEENAERTS JOSEPH ELISABETH ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  GOMEZ-SANCHEZ ANTONIO ,  FLAMENG WILLEM ,  HERIJGERS PAUL JOANNES LUDOVIC ,  MEERT THEO FRANS ,  BORGERS MARCEL J M

    IPC: C07D401/04 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/506 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

    Abstract: The present invention relates to an agent for reducing ischaemic damage to an organ, in particular to a heart and a brain, pharmaceutical compositions comprising said agent and the use of said agent for the treatment of ischaemic diseases to the heart and the brain. The agent comprises a substituted 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivative according to Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof, the N-oxide forms thereof and the prodrugs thereof. In particular are claimed the compounds according to Formula (I) in which A=B is C-O or SO 2 , X is a covalent bond, R 1 is alkyloxy, alkyloxyalkyl, Ar or NR 9 R 10 , wherein R 9 and R 10 each independently are hydrogen or Ar; or A=B and R 1 together form a benzoxazolyl radical; p is zero, R 3 is benzyl optionally substituted with hydroxy, alkyl or alkyloxycarbonyl and R 4 and R 5 each are hydrogen. The use of said agents has important clinical ramifications with regard to the reduction of ischaemic damage to an organ in a mammal, in particular to a heart and/or a brain, the prevention of coronary artery diseases in a mammal by inducing a cardioprotective effect and the treatment and prevention of stroke.

    SUBSTITUTED 1-PIPERIDIN-4-YL-4-AZETIDIN-3-YL-PIPERAZINE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS
    53.
    发明专利
    SUBSTITUTED 1-PIPERIDIN-4-YL-4-AZETIDIN-3-YL-PIPERAZINE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS 未知

    公开(公告)号：AU2003299249A1

    公开(公告)日：2004-07-14

    申请号：AU2003299249

    申请日：2003-12-17

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： JANSSENS FRANS EDUARD ,  SOMMEN FRANCOIS MARIA ,  BOECK BENOIT CHRISTIAN ALBERT ,  LEENAERTS JOSEPH ELISABETH

    IPC: A61K31/495 ,  A61K31/506 ,  A61P11/06 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P29/00 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

    Abstract: The invention concerns substituted 1-piperidin-4-yl-4-azetidin-3-yl-piperazine having neurokinin antagonistic activity, in particular NK 1 and NK 1 /NK 3 -antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, emesis, anxiety, depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pain, neurogenic inflammation, asthma, micturition disorders such as urinary incontinence and nociception. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1. In view of their capability to antagonize the actions of tachykinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P by blocking the NK receptors, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of tachykinin-mediated conditions, such as, for instance CNS disorders, in particular depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality disorders, schizoaffective disorders, eating disorders, neurodegenerative diseases, addiction disorders, mood disorders, sexual dysfunction, pain and other CNS-related conditions; inflammation; allergic disorders; emesis; gastrointestinal disorders, in particular irritable bowel syndrome (IBS); skin disorders; vasospastic diseases; fibrosing and collagen diseases; disorders related to immune enhancement or suppression and rheumatic diseases and body weight control.

    55.
    发明专利
    未知

    公开(公告)号：ES2207632T3

    公开(公告)日：2004-06-01

    申请号：ES92911635

    申请日：1992-06-09

    Applicant: JANSSEN PHARMACEUTICA NV

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

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

    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.

    56.
    发明专利
    未知

    公开(公告)号：ES2204892T3

    公开(公告)日：2004-05-01

    申请号：ES92911643

    申请日：1992-06-09

    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

    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.

    58.
    发明专利
    未知

    公开(公告)号：PT588858E

    公开(公告)日：2004-02-27

    申请号：PT92911635

    申请日：1992-06-09

    Applicant: JANSSEN PHARMACEUTICA NV

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

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

    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.

Patent Agency Ranking