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    1.
    发明专利
    未知

    公开(公告)号：DE69635224T2

    公开(公告)日：2006-06-22

    申请号：DE69635224

    申请日：1996-03-28

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： FREYNE JEAN ,  DIELS STANISLAS ,  ANDRES-GIL IGNACIO ,  FERNANDEZ-GADEA JAVIER

    IPC: C07D233/70 ,  A61K31/415 ,  A61K31/4166 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P37/08 ,  C07D233/32 ,  C07D233/38 ,  C07D405/04 ,  C07D405/06

    Abstract: PCT No. PCT/EP96/01393 Sec. 371 Date Sep. 29, 1997 Sec. 102(e) Date Sep. 29, 1997 PCT Filed Mar. 28, 1996 PCT Pub. No. WO96/31487 PCT Pub. Date Oct. 10, 1996The 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 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 is a bivalent radical of formula 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; Het1 is morpholinyl or optionally substituted pyridinyl, -furanyl, -thienyl, -hydroxypyridinyl, -imidazolyl, -thiazolyl, -oxazolyl, -isoquinolinyl, -quinolinonyl, -piperidinyl, -piperazinyl; and Het2 is morpholinyl 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 formula (I) and pharmaceutical compositions thereof.

    2.
    发明专利
    未知

    公开(公告)号：DE69233161T2

    公开(公告)日：2004-05-27

    申请号：DE69233161

    申请日：1992-06-09

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： JANSSENS EDUARD ,  DIELS STANISLAS ,  LEENAERTS ELISABETH ,  COOYMANS 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.

    3.
    发明专利
    未知

    公开(公告)号：DE69619661D1

    公开(公告)日：2002-04-11

    申请号：DE69619661

    申请日：1996-03-28

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： FREYNE JEAN ,  DIELS STANISLAS ,  ANDRES GIL JOSE IGNACIO ,  FERNANDEZ GADEA FRANCISCO JAVI

    IPC: C07D233/32 ,  A61K31/415 ,  A61K31/4166 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P37/08 ,  C07D233/36 ,  C07D233/38 ,  C07D233/70 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12

    Abstract: The present invention describes the use of compounds for the manufacture of a medicament for treating warm-blooded animals suffering from disease states related to an abnormal enzymatic or catalytic activity of phosphodiesterase IV (PDE IV), and/or disease states related to a physiologically detrimental excess of cytokines, in particular allergic, atopic and inflammatory diseases, said compounds having the formula the N-oxide forms, the pharmaceutically 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; halo; optionally substituted C1-6alkyl; trifluoromethyl; C3-6cycloalkyl; carboxyl; C1-4alkyloxycarbonyl; C3-6cycloalkylaminocarbonyl; aryl; Het1; or R4 is a radical of formula: -O-R6; or -NH-R7; R5 is hydrogen, halo, hydroxy or C1-6alkyl; or R4 and R5 taken together may form a bivalent radical of formula: -(CH2)n-; -CH2-CH2-O-CH2-CH2-; -CH2-CH2-N(R8)-CH2-CH2-; or -CH2-CH=CH-CH2-; Y is a direct bond, haloC1-4alkanediyl or C1-4alkanediyl; -A-B- is a bivalent radical of formula: -CR9=CR10-; or -CHR9-CHR10-; and 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; Het1 <

    6.
    发明专利
    未知

    公开(公告)号：DE69619661T2

    公开(公告)日：2002-10-31

    申请号：DE69619661

    申请日：1996-03-28

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： FREYNE JEAN ,  DIELS STANISLAS ,  ANDRES GIL JOSE IGNACIO ,  FERNANDEZ GADEA FRANCISCO JAVI

    IPC: C07D233/32 ,  A61K31/415 ,  A61K31/4166 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P37/08 ,  C07D233/36 ,  C07D233/38 ,  C07D233/70 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12

    Abstract: The present invention describes the use of compounds for the manufacture of a medicament for treating warm-blooded animals suffering from disease states related to an abnormal enzymatic or catalytic activity of phosphodiesterase IV (PDE IV), and/or disease states related to a physiologically detrimental excess of cytokines, in particular allergic, atopic and inflammatory diseases, said compounds having the formula the N-oxide forms, the pharmaceutically 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; halo; optionally substituted C1-6alkyl; trifluoromethyl; C3-6cycloalkyl; carboxyl; C1-4alkyloxycarbonyl; C3-6cycloalkylaminocarbonyl; aryl; Het1; or R4 is a radical of formula: -O-R6; or -NH-R7; R5 is hydrogen, halo, hydroxy or C1-6alkyl; or R4 and R5 taken together may form a bivalent radical of formula: -(CH2)n-; -CH2-CH2-O-CH2-CH2-; -CH2-CH2-N(R8)-CH2-CH2-; or -CH2-CH=CH-CH2-; Y is a direct bond, haloC1-4alkanediyl or C1-4alkanediyl; -A-B- is a bivalent radical of formula: -CR9=CR10-; or -CHR9-CHR10-; and 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; Het1 <

    7.
    发明专利
    未知

    公开(公告)号：DE69912590D1

    公开(公告)日：2003-12-11

    申请号：DE69912590

    申请日：1999-03-24

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： FREYNE JEAN ,  DIELS STANISLAS ,  MATESANZ-BALLESTEROS CAMPO DE ,  DIAZ-MARTINEZ ADOLFO

    IPC: A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4439 ,  A61P11/06 ,  A61P17/00 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D401/06 ,  C07D405/14 ,  C07D407/14

    Abstract: The present invention concerns pyridine derivatives having the formulathe N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein L is hydrogen; C1-6alkyl; C1-6alkyl carbonyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl; C3-6alkenyl; substituted C3-6alkenyl; piperidyl; substituted piperidyl; C1-6alkylsulfonyl or arylsulfonyl; -A-B- is -CR =CR - or-CHR -CHR -; D is O or NR ; R is a hydrogen or C1-4alkyl; R is hydrogen; halo; C1-6alkyl; trifluoromethyl; C3-6cycloalkyl; carboxyl; C1-4alkyl oxycarbonyl; C3-6cycloalkylaminocarbonyl; aryl; Het ; or substituted C1-6alkyl; or R is -O-R or -NH-R ; R is hydrogen, halo, hydroxy, C1-6alkyl or C1-6alkyloxy; or R and R , or R and R taken together may form a bivalent radical; Q is disubstituted pyridine; R and R each independently are hydrogen; C1-6alkyl; difluoromethyl; trifluoromethyl; C3-6cyclo alkyl; a saturated 5-, 6- or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; 6,7-dihydro-5H-cyclopentapyridyl; bicyclo[2.2.1]-2-heptenyl; bicyclo[2.2.1]heptanyl; C1-6alkylsulfonyl; arylsulfonyl; or substituted C1-10alkyl; having PDE IV and cytokine inhibiting activity. The invention also relates to processes for preparing the compounds of formula (I), pharmaceutical compositions thereof and their use as a medicament.

    8.
    发明专利
    未知

    公开(公告)号：DE69233205D1

    公开(公告)日：2003-10-23

    申请号：DE69233205

    申请日：1992-06-09

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： JANSSENS EDUARD ,  DIELS STANISLAS ,  LEENAERTS ELISABETH

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

    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.

    9.
    发明专利
    未知

    公开(公告)号：DE69233161D1

    公开(公告)日：2003-09-18

    申请号：DE69233161

    申请日：1992-06-09

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： JANSSENS EDUARD ,  DIELS STANISLAS ,  LEENAERTS ELISABETH ,  COOYMANS 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.

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