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    SUBSTITUTED TETRACYCLIC AZEPINE DERIVATIVES WHICH HAVE AFFINITY FOR 5-HT2 RECEPTORS
    31.
    发明专利
    SUBSTITUTED TETRACYCLIC AZEPINE DERIVATIVES WHICH HAVE AFFINITY FOR 5-HT2 RECEPTORS 未知

    公开(公告)号：GR3035680T3

    公开(公告)日：2001-06-29

    申请号：GR20010400530

    申请日：2001-03-30

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： SIPIDO VICTOR KAREL ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  ANDRES-GIL JOSE IGNACIO ,  MEERT THEO FRANS ,  GIL-LOPETEGUI PILAR

    IPC: A61K31/535 ,  A61K31/55 ,  A61P9/00 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/26 ,  C07D223/20 ,  C07D223/30 ,  C07D261/00 ,  C07D498/04

    Abstract: This invention concerns the compounds of formula (I), the pharmaceutically acceptable salts and stereoisomeric forms thereof, and also the N-oxide forms thereof. (I) wherein: R1 and R2 each independently are hydrogen; C1-6alkyl; C1-6alkylcarbonyl; trihalomethylcarbonyl; C1-6alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6alkylcarbonyloxy, C1-6alkyloxycarbonyl or aryl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R3, R4, R5, R6, R9, R10, R11 or R12 each independently are hydrogen, halo, cyano, hydroxy, trifluoromethyl, trifluoromethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)-amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)-aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl, C1-6alkyloxy-carbonyl; R7 and R8 are each independently hydrogen, hydroxy, C1-6alkyl, C1-6alkyloxy or R7 and R8 taken together may form mono- or di(cyano)methylene, or together with the carbon atom to which they are attached form a carbonyl or a spiro substituent; or R7 and R8 taken together may form methylene; R13 is hydrogen, C1-6alkyl, or trifluoromethyl; R14 is hydrogen, C1-6alkyl, cyano, or trifluoromethyl; n is zero to 6. These compounds were tested as mCPP-antagonists in rats. The compounds of formula (I) may be used as therapeutic agents in the treatment or the prevention of CNS disorders, cardiovascular disorders or gastrointestinal disorders.

    34.
    发明专利
    未知

    公开(公告)号：DE69520071D1

    公开(公告)日：2001-03-15

    申请号：DE69520071

    申请日：1995-10-25

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： FERNANDEZ-GADEA FRANCISCO JAVI ,  SIPIDO KAREL ,  ANDRES-GIL JOSE IGNACIO ,  MEERT FRANS

    IPC: A61K31/535 ,  A61K31/55 ,  A61K31/553 ,  A61K31/554 ,  A61P9/00 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/26 ,  C07D261/20 ,  C07D267/16 ,  C07D498/04 ,  C07D513/04

    Abstract: PCT No. PCT/EP95/04197 Sec. 371 Date Apr. 25, 1997 Sec. 102(e) Date Apr. 25, 1997 PCT Filed Oct. 25, 1995 PCT Pub. No. WO96/14321 PCT Pub. Date May 17, 1996This invention concerns the compounds of formula (I), the pharmaceutically acceptable salts and stereoisomeric forms thereof, and also the N-oxide forms thereof. (I) wherein: R1 and R2 each independently are hydrogen; C1-6alkyl; C1-6alkylcarbonyl; trihalomethylcarbonyl; C1-6alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6alkylcarbonyloxy, C1-6alkyloxycarbonyl or aryl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R3 to R10 each independently are hydrogen, halo, cyano, hydroxy, trifluoromethyl, trifluoromethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)-aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl; R11 is hydrogen, C1-6alkyl, or trifluoromethyl; R12 is hydrogen, C1-6alkyl, cyano, or trifluoromethyl; n is zero to 6; and X is O, S, S(=O) or S(=O)2. The compounds of formula (I) may be used as therapeutic agents in the treatment or the prevention of CNS disorders, cardiovascular disorders or gastrointestinal disorders.

    35.
    发明专利
    未知

    公开(公告)号：AT199087T

    公开(公告)日：2001-02-15

    申请号：AT95937006

    申请日：1995-10-25

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： SIPIDO VICTOR KAREL ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  ANDRES-GIL JOSE IGNACIO ,  MEERT THEO FRANS ,  GIL-LOPETEGUI PILAR

    IPC: A61K31/535 ,  A61K31/55 ,  A61P9/00 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/26 ,  C07D223/20 ,  C07D223/30 ,  C07D261/00 ,  C07D498/04 ,  C07D223/00

    Abstract: This invention concerns the compounds of formula (I), the pharmaceutically acceptable salts and stereoisomeric forms thereof, and also the N-oxide forms thereof. (I) wherein: R1 and R2 each independently are hydrogen; C1-6alkyl; C1-6alkylcarbonyl; trihalomethylcarbonyl; C1-6alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6alkylcarbonyloxy, C1-6alkyloxycarbonyl or aryl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R3, R4, R5, R6, R9, R10, R11 or R12 each independently are hydrogen, halo, cyano, hydroxy, trifluoromethyl, trifluoromethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)-amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)-aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl, C1-6alkyloxy-carbonyl; R7 and R8 are each independently hydrogen, hydroxy, C1-6alkyl, C1-6alkyloxy or R7 and R8 taken together may form mono- or di(cyano)methylene, or together with the carbon atom to which they are attached form a carbonyl or a spiro substituent; or R7 and R8 taken together may form methylene; R13 is hydrogen, C1-6alkyl, or trifluoromethyl; R14 is hydrogen, C1-6alkyl, cyano, or trifluoromethyl; n is zero to 6. These compounds were tested as mCPP-antagonists in rats. The compounds of formula (I) may be used as therapeutic agents in the treatment or the prevention of CNS disorders, cardiovascular disorders or gastrointestinal disorders.

    36.
    发明专利
    未知

    公开(公告)号：BR9712256A

    公开(公告)日：1999-08-24

    申请号：BR9712256

    申请日：1997-09-24

    Applicant: JANSSEN PHARMACEUTICA NV

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

    IPC: C07D233/44 ,  A61K31/00 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4168 ,  A61P11/00 ,  A61P11/06 ,  A61P29/00 ,  A61P37/00 ,  A61P37/08 ,  C07D233/48 ,  C07D233/88 ,  C07D405/12

    Abstract: PCT No. PCT/EP97/05322 Sec. 371 Date Mar. 19, 1999 Sec. 102(e) Date Mar. 19, 1999 PCT Filed Sep. 24, 1997 PCT Pub. No. WO98/14432 PCT Pub. Date Apr. 9, 1998The present invention concerns 2-cyanoiminoimidazole derivatives having the formula the N-oxide forms, the pharmaceutically acceptable 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; 6,7-dihydro-5H-cyclopentapyridinyl; 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; halo; C1-6alkyl; trifluoromethyl; C3-6cycloalkyl; carboxyl; C1-4alkyloxycarbonyl; C3-6cycloalkylaminocarbonyl; aryl; Het1; or substituted C1-6alkyl; or R4 is -O-R7 or -NH-R8; R5 is hydrogen, halo, hydroxy, C1-6alkyl or C1-6alkyloxy; R6 is a hydrogen or C1-4alkyl; or R4 and R6, or R4 and R5 taken together may form a bivalent radical; -A-B- is -CR10=CR11- or -CHR10-CHR11-; L is hydrogen; C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl; C3-6alkenyl; substituted C3-6alkenyl; piperidinyl; substituted piperidinyl; C1-6alkylsulfonyl or arylsulfonyl; having PDE IV and cytokine inhibiting activity. The invention also relates to processes for preparing the compounds of formula (I) and pharmaceutical compositions thereof.

    Substituted tetracyclic azepine derivatives which have affinity for 5-HT2 receptors
    38.
    发明专利
    Substituted tetracyclic azepine derivatives which have affinity for 5-HT2 receptors 未知

    公开(公告)号：AU704285B2

    公开(公告)日：1999-04-15

    申请号：AU3924995

    申请日：1995-10-25

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： SIPIDO VICTOR KAREL ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  ANDRES-GIL JOSE IGNACIO ,  MEERT THEO FRANS ,  GIL-LOPETEGUI PILAR

    IPC: A61K31/535 ,  A61K31/55 ,  A61P9/00 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/26 ,  C07D223/20 ,  C07D223/30 ,  C07D261/00 ,  C07D498/04

    Abstract: This invention concerns the compounds of formula (I), the pharmaceutically acceptable salts and stereoisomeric forms thereof, and also the N-oxide forms thereof. (I) wherein: R1 and R2 each independently are hydrogen; C1-6alkyl; C1-6alkylcarbonyl; trihalomethylcarbonyl; C1-6alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6alkylcarbonyloxy, C1-6alkyloxycarbonyl or aryl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R3, R4, R5, R6, R9, R10, R11 or R12 each independently are hydrogen, halo, cyano, hydroxy, trifluoromethyl, trifluoromethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)-amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)-aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl, C1-6alkyloxy-carbonyl; R7 and R8 are each independently hydrogen, hydroxy, C1-6alkyl, C1-6alkyloxy or R7 and R8 taken together may form mono- or di(cyano)methylene, or together with the carbon atom to which they are attached form a carbonyl or a spiro substituent; or R7 and R8 taken together may form methylene; R13 is hydrogen, C1-6alkyl, or trifluoromethyl; R14 is hydrogen, C1-6alkyl, cyano, or trifluoromethyl; n is zero to 6. These compounds were tested as mCPP-antagonists in rats. The compounds of formula (I) may be used as therapeutic agents in the treatment or the prevention of CNS disorders, cardiovascular disorders or gastrointestinal disorders.

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