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    SUBSTITUTED 4-(4-PIPERIDIN-4-YL-PIPERAZIN-1-YL)-AZEPANE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS
    14.
    发明专利
    SUBSTITUTED 4-(4-PIPERIDIN-4-YL-PIPERAZIN-1-YL)-AZEPANE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS 未知

    公开(公告)号：CA2509090C

    公开(公告)日：2012-01-24

    申请号：CA2509090

    申请日：2003-12-17

    Applicant: JANSSEN PHARMACEUTICA NV

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

    IPC: C07D401/14 ,  A61K31/55 ,  C07D401/12 ,  C07D405/14 ,  C07D413/14

    Abstract: The invention concerns substituted 4-(4-piperidin-4-yl-piperazin-1-yl)-azepane derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of pain, emesis, anxiety, depression and IBS. 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 and Neurokinin B by blocking the NK1, NK2 and NK3 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 schizoaffective disorders, depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality 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.

    15.
    发明专利
    未知

    公开(公告)号：NO331174B1

    公开(公告)日：2011-10-24

    申请号：NO20053569

    申请日：2005-07-21

    Applicant: JANSSEN PHARMACEUTICA NV

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

    IPC: A61K31/454 ,  A61P25/00 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D498/14 ,  A61K31/496

    Abstract: This invention concerns substituted I-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, anxiety, depression, emesis and IBS. 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 and Neurokinin B by blocking the NK1, NK2 and NK3 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 schizoaffective disorders, depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality 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.

    SUBSTITUTED 1,4-DI-PIPERIDIN-4-YL-PIPERAZINE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS
    16.
    发明专利
    SUBSTITUTED 1,4-DI-PIPERIDIN-4-YL-PIPERAZINE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS 未知

    公开(公告)号：CA2499903C

    公开(公告)日：2011-06-14

    申请号：CA2499903

    申请日：2003-10-07

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： JANSSENS FRANS EDUARD ,  SOMMEN FRANCOIS MARIA ,  DE BOECK BENOIT CHRISTIAN ALBERT GHISLAIN ,  LEENAERTS JOSEPH ELISABETH ,  VAN ROOSBROECK YVES EMIEL MARIA ,  DIELS GASTON STANISLAS MARCELLA

    IPC: C07D211/58 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

    Abstract: The invention concerns substituted 1,4-di-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of emesis, anxiety, depression, pain, pancreatitis and IBS. 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 neurokinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P by blocking the NK1 receptor, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of neurokinin-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.

    ANTIHISTAMINIC SPIRO COMPOUNDS
    19.
    发明专利
    ANTIHISTAMINIC SPIRO COMPOUNDS 未知

    公开(公告)号：CA2355939C

    公开(公告)日：2010-12-14

    申请号：CA2355939

    申请日：1999-12-15

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： JANSSENS FRANS EDUARD ,  LEENAERTS JOSEPH ELISABETH

    IPC: C07D471/20 ,  A61K31/438 ,  A61K31/55 ,  A61P11/06 ,  A61P17/00 ,  A61P17/04 ,  A61P27/14 ,  A61P27/16 ,  A61P37/00 ,  A61P37/08 ,  A61P43/00 ,  C07D209/00 ,  C07D221/00 ,  C07D223/00 ,  C07D235/00 ,  C07D333/00 ,  C07D487/20 ,  C07D495/22 ,  C07D498/20 ,  C07D519/00

    Abstract: This invention concerns the compounds of formula (I) a prodrug, a N-oxide, an addition salt, a quaternary amine or a stereochemically isomeric form thereof wherein R1 is hydrogen, C1-6alkyl, halo, formyl, carboxyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyl, N(R3R4)C(=O)-, N(R3R4)C(-O)N(R5)-, ethenyl substituted with carboxyl or C1-6alkyloxycarbonyl, or C1-6alkyl substituted with hydroxy, carboxyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, N(R3R4)C(=O)-, C1-6alkylC(=O)N(R5)-, C1-6alkylS(=O)2N(R5)- or N(R3R4)C(=O)N(R5)-wherein each R3 and each R4 independently are hydrogen or C1-4alkyl, and R5 is hydrogen or hydroxy; R2 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, N(R3R4)C(=O)-, aryl or halo; n is 1 or 2; -A-B- represents a bivalent radical of formula -Y-CH=CH-, -CH=CH-Y-, or -CH=CH-CH=CH-, wherein each hydrogen atom may independently be replaced by R6 wherein R6 is C1-6alkyl, halo, hydroxy, C1-6alkyloxy, ethenyl substituted with carboxyl or C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, formyl, carboxyl, or hydroxycarbonylC1-6alkyl, and each Y independently is a bivalent radical of formula -O-, --S- or -NR7-, wherein R7 is hydrogen, C1-6alkyl or C1-6alkylcarbonyl; Z is a bivalent radical of formula -(CH2)p-, -CH=CH-, -CH2-CHOH-, -CH2-O-, -CH2-C(=O), or -CH2-C(=NOH)-, provided that the bivalent radicals are connected to the nitrogen of the imidazole ring via their -CH2- moiety; and wherein p is 1, 2, 3 or 4; L is hydrogen; C1-6alkyl; C2-6alkenyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; C1-6alkyl substituted with hydroxy, carboxyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, aryl, aryloxy, cyano or R8HN- wherein R8 is hydrogen, C1-6alkyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyl; or L represents a radical of formula -Alk-Y-Het1, -Alk-NH-CO-Het2 or -Alk-Het3 wherein Alk represents C1-4alkanediyl; Y represents O, S or NH; Het1, Het2 and Het3 each represent an optionally substituted heterocycle; for use as a medicine.

    Substituted 1-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives and their use as neurokinin antagonists
    20.
    发明专利
    Substituted 1-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives and their use as neurokinin antagonists 未知

    公开(公告)号：AU2003302488B2

    公开(公告)日：2009-10-08

    申请号：AU2003302488

    申请日：2003-12-17

    Applicant: JANSSEN PHARMACEUTICA NV

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

    IPC: C07D401/14 ,  A61K31/454 ,  A61P25/00 ,  C07D401/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D498/14

    Abstract: This invention concerns substituted I-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, anxiety, depression, emesis and IBS. 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 and Neurokinin B by blocking the NK1, NK2 and NK3 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 schizoaffective disorders, depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality 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.

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