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    Pde iv inhibiting pyridine derivatives
    43.
    发明专利
    Pde iv inhibiting pyridine derivatives 未知

    公开(公告)号：AU3147499A

    公开(公告)日：1999-10-18

    申请号：AU3147499

    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.

    PDE IV INHIBITING PYRIDINE DERIVATIVES
    44.
    发明专利
    PDE IV INHIBITING PYRIDINE DERIVATIVES 未知

    公开(公告)号：CA2326045C

    公开(公告)日：2008-12-09

    申请号：CA2326045

    申请日：1999-03-24

    Applicant: JANSSEN PHARMACEUTICA NV

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

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

    Abstract: The present invention concerns pyridine derivatives having formula (I), the 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 -CR4-CR5- or -CHR4-CHR5-; D is O or NR6; R1 is a hydrogen or C1-4alkyl; R 2 is hydrogen; halo; C1-6alkyl; trifluoromethyl; C3-6cycloalkyl; carboxyl; C1-4alkyl oxycarbonyl; C3-6cycloalkylaminocarbonyl ; aryl; HET1; or substituted C1-6alkyl; or R2 is aR9 or NH-R10; R3 is hydrogen, halo, hydroxy, C1-6alkyl or C1-6alkyloxy; or R2 a nd Ri, or R2 and R3 taken together may form a bivalent radical; Q is disubstituted pyridine; R7 and R8 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.

    Derivát pyridinu, způsob jeho výroby a použití a farmaceutická kompozice s jeho obsahem
    45.
    发明专利
    Derivát pyridinu, způsob jeho výroby a použití a farmaceutická kompozice s jeho obsahem 未知

    公开(公告)号：CZ298747B6

    公开(公告)日：2008-01-16

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

    Abstract: Derivát pyridinu vzorce (I), kde -A-B- znamená dvojmocný zbytek vzorce -CR.sup.4.n.=CR.sup.5.n.-nebo -CHR.sup.4.n.=CHR.sup.5.n.-; D je O nebo NR.sup.6.n.; Q je substituovaný 2- nebo 3- pyridyl; R.sup.1.n. je H nebo C.sub.1-4.n.alkyl; R.sup.2.n.je H; halogen; C.sub.1-6.n.alkyl; trifluormethyl;C.sub.3-6.n.cykloalkyl; karboxyl; C.sub.1-4.n.alkyloxykarbonyl; C.sub.3-6.n.cykloalkylaminokarbonyl; aryl, Het.sup.1.n.; nebo C.sub.1-6.n.alkyl substituovaný kyanoskupinou, aminoskupinou, hydroxyskupinou, C.sub.1-4.n.alkylkarbonylaminoskupinou, arylskupinou nebo skupinou Het.sup.1.n.; nebo R.sup.2.n. je -O- R.sup.9.n. nebo -NH-R.sup.10.n.; R.sup.3.n. je H, halogen, hydroxy, C.sub.1-6.n.alkyl nebo C.sub.1-6.n.alkoxy; R.sup.4.n. a R.sup.5.n. je každý nezávisle H nebo C.sub.1-4.n.alkyl; R.sup.6.n. je H, C.sub.1-4.n.alkyl nebo kyano; R.sup.9.n. je H; C.sub.1-6.n.alkyl; C.sub.1-6.n.alkyl substituovaný hydroxyskupinou, karboxyskupinou, C.sub.1-4.n.alkyloxykarbonylskupinou, aminoskupinou, mono- nebo di(C.sub.1-4.n.alkyl)aminoskupinou, skupinou Het.sup.1.n. nebo arylskupinou; aryl znamená popřípadě substituovanou fenylovou skupinu; Het.sup.1.n. znamená popřípadě substituovanou heterocyklylskupinu; a jeho N-oxidová forma, farmaceuticky přijatelná adiční sůl s kyselinou nebo bází a stereochemicky izomerní forma. Tento derivát inhibuje PDE IV. Způsob jeho výroby a použití a farmaceutická kompozice s jeho obsahem.

    PDE IV INHIBITING PYRIDINE DERIVATIVES
    46.
    发明专利
    PDE IV INHIBITING PYRIDINE DERIVATIVES 未知

    公开(公告)号：PL196026B1

    公开(公告)日：2007-11-30

    申请号：PL34319499

    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: C07D401/06 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4439 ,  A61P11/06 ,  A61P17/00 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  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.

    47.
    发明专利
    未知

    公开(公告)号：EE04718B1

    公开(公告)日：2006-10-16

    申请号：EEP200000569

    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 ,  A61K31/435

    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
    49.
    发明专利
    PDE IV INHIBITING PYRIDINE DERIVATIVES 未知

    公开(公告)号：BG64705B1

    公开(公告)日：2005-12-30

    申请号：BG10471800

    申请日：2000-08-28

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： FREYNE EDDY JEAN ,  DIELS GASTON STANISLAS MARCELL ,  MATESANZ-BALLESTEROS MARIA ,  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 formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein L is hydrogen; C1-6alkyl, C1-6alkyl carbonyl; C1-6a; koxycarbonyl; substituted C1-6alkyl; C3-6alkenyl; substituted C3-6a;kenyl; piperidyl; substituted piperidyl; C1-6alkylsulfonyl or arylsulfonyl; -A-B-C3-6cycloalkyl; carboxyl; C14alkyl oxycarbonyl; C3-6cycloalkylaminocarbonyl; aryl, HET1; or substituted C1-6alkyl; or R2 is O-R9 or NH-R10; R3 is hydrogen, halo, hydroxy, C1-6alkyl or C1-6alkyloxy; or R2 andR1, or R2 and R3 taken together may form a bivalent radical; Q is disubstituted pyridine; R7 and R8 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; arylsuylfonyl; or substituted C1-10 alkyl; having PDE IV and citokine inhibiting activity. The invention also relates to processes for preparing the compounds of formula (I), pharmaceutical compositions thereof and their use as medicaments.

    50.
    发明专利
    未知

    公开(公告)号：PT1068194E

    公开(公告)日：2004-03-31

    申请号：PT99913302

    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.

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