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    21.
    发明专利
    未知

    公开(公告)号：NO319531B1

    公开(公告)日：2005-08-29

    申请号：NO20004906

    申请日：2000-09-29

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： FREYNE EDDY JEAN EDGARD ,  DIELS GASTON STANISLAS MARCELL ,  DIAZ-MARTINEZ ADOLFO ,  MATESANZ-BALLESTEROS MARIA ENC

    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.

    PDE IV INHIBITING PYRIDINE DERIVATIVES
    23.
    发明专利
    PDE IV INHIBITING PYRIDINE DERIVATIVES 未知

    公开(公告)号：SI1068194T1

    公开(公告)日：2004-04-30

    申请号：SI9930470

    申请日：1999-03-24

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： FREYNE EDDY JEAN EDGARD ,  DIELS GASTON STANISLAS MARCELL ,  MATESANZ-BALLESTEROS ,  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.

    PDE IV inhibiting pyridine derivatives
    26.
    发明专利
    PDE IV inhibiting pyridine derivatives 未知

    公开(公告)号：NZ507022A

    公开(公告)日：2002-06-28

    申请号：NZ50702299

    申请日：1999-03-24

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： FREYNE EDDY JEAN EDGARD ,  MATESANZ-BALLESTEROS MARIA ENC ,  DIAZ-MARTINEZ ADOLFO ,  DIELS GASTON STANISLAS MARCELL

    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: A compound having the formula (I) wherein: L is hydrogen; C1-6alky or substituted with one or two substituents selected from the group consisting of hydroxy, C1-4alkyloxy, C1-4alkyloxycarbonyl, mono and di (C1-4alkyl) amino, aryl and Hert2; C3-6alkenyl; C3-6alkenyl substituted with aryl; C1-6alkylcarbonyl; C1-6alky! oxycarbonyl; piperidyl; piperidyl substituted with C1-4alkyl or arylC1 4alkyl; C1-6alkylsulfonyl or arylsulfonyl; -A-B-is a bivalent radical of formula:-CR4=CR5- (a-1); or- CHR4-CHR5- (a-2); D is O or NR6; Q is a radical of the formula (b-1), (b-2) or (b-3); R' is hydrogen or C1-4alkyl ; or R' and R2 together may form a bivalent radical of formula- (CH2)m- wherein m is 1, 2,3 or 4; R2 ís hydrogen; halo; C1-6alkyl; trifluoromethyl; C3-6cycloalkyl; carboxyl; C1-4alkyloxycarbonyl; C3-6cycloalkylaminocarbonyl; aryl; Het1 ; or C1-6alkyl substituted with cyano, amino, hydroxy, C1-4alkylcarbonylamino, aryl or Het1 ; or R2 is a radical of formula:-O-R9 (c-1); or-NH-R10 (c-2); R3 is hydrogen, halo, hydroxy, C1-6alkyl or C1-6alkyloxy; or R2 and R3 taken together may form a bivalent radical of formula : - (CH2)n-(d-1); -CH2-CH2-O-CH2-CH2- (d-2); -CH2-CH2-N (R11)-CH2-CH2- (d-3); or -CH2-CH=CH-CH2- (d-4); wherein n is 2,3,4 or 5. The compounds fine use in treating atopic or asthmatic diseases.

    PDE IV inhibiting pyridine derivatives
    27.
    发明专利
    PDE IV inhibiting pyridine derivatives 未知

    公开(公告)号：CZ20003338A3

    公开(公告)日：2001-02-14

    申请号：CZ20003338

    申请日：1999-03-24

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： FREYNE EDDY JEAN EDGARD ,  DIELS GASTON STANISLAS MARCELL ,  MATESANZ-BALLESTEROS MARIA ENC ,  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.

    28.
    发明专利
    未知

    公开(公告)号：TR200002801T2

    公开(公告)日：2000-12-21

    申请号：TR200002801

    申请日：1999-03-24

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： FREYNE EDDY JEAN EDGARD ,  DIELS GASTON STANISLAS MARCELL ,  MATESANZ-BALLESTEROS MARIA ENC ,  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.

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