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    42.
    发明专利
    未知

    公开(公告)号：DE69914931D1

    公开(公告)日：2004-03-25

    申请号：DE69914931

    申请日：1999-10-07

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： FREYNE EDDY JEAN EDGARD ,  ANDRES-GIL JOSE IGNACIO ,  DEROOSE FREDERIK DIRK ,  PETIT DAVY PETRUS FRANCISCUS M ,  MATESANZ-BALLESTEROS MARIA E ,  ALVAREZ ESCOBAR ROSA MARIA

    IPC: C07D487/04 ,  A61K31/42 ,  A61K31/4427 ,  A61K31/4725 ,  A61K31/4738 ,  A61K31/496 ,  A61K31/506 ,  A61P3/12 ,  A61P9/10 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P29/00 ,  A61P31/12 ,  A61P35/00 ,  A61P37/00 ,  A61P37/06 ,  C07D261/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D498/04

    Abstract: The present invention is concerned with the compounds of formula wherein m, n and p are each independently 0 or 1 and q is 0, 1, 2, 3, 4 or 5; -A 1 =A 2 -A 3 =A 4 - is a pyridinylidene, pyridazinylidene, pyrimidinylidene, pyrazinylidene or phenylidene; B represents an amide, ketone or oxadiazole; D represents Ar or Het; Q represents a covalent direct bond or a ketone, -N-, -O-, -CR 5 R 6 -, amide, ethenyl, imine, sulfonyl, sulfinyl, 3-oxobutenyl, pyrazole, isoxazole or thiazole; L represents Ar or Het; R 1 represents hydrogen, halo, hydroxy, C (2-6) alkenyl, C (2-6) alkynyl, C (3-6) cycloalkyl, C (3-6) cycloalkenyl, cyano, guanidine, nitro, NR 17 R 18 , an optionally substituted C (1-6) alkyl or C (1-6) alkyloxy; R 2 and R 3 each independently represent hydrogen, halo, C (1-6) alkyloxy or an optionally substituted C (1-6) alkyl; R 5 and R 6 each independently represent hydrogen, hydroxy, halo, an optionally substituted C (1-6) alkyl, C (2-6) alkenyl, C (2-6) alkynyl, C (3-6) cycloalkyl, C (3-6) cycloalkenyl, C (1-6) alkyloxy, cyano, (C-O)R 25 , (C-O)OR 16 , (SO 2 )R 16 , aminocarbonyloxy, aminoC (1-6) alkyl, NR 17 R 18 , N 3 , Ar or Het; or R 5 and R 6 together with the carbon atom to which they are attached, form an Ar or Het; Ar represents an optionally substituted C (6-14) aryl; Het represents an optionally substituted C (1-14) heterocycle; or a N-oxide, pharmaceutically acceptable addition salt, quaternary amine or stereochemically isomeric form thereof; the processes for their preparation and compositions comprising them. It further relates to their use as a medicine.

    46.
    发明专利
    未知

    公开(公告)号：PT934280E

    公开(公告)日：2003-08-29

    申请号：PT97910380

    申请日：1997-09-24

    Applicant: JANSSEN PHARMACEUTICA NV

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

    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.

    47.
    发明专利
    未知

    公开(公告)号：DK0934280T3

    公开(公告)日：2003-07-21

    申请号：DK97910380

    申请日：1997-09-24

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： EDDY JEAN EDGARD FREYNE ,  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.

    50.
    发明专利
    未知

    公开(公告)号：DE69714980T2

    公开(公告)日：2003-04-10

    申请号：DE69714980

    申请日：1997-04-09

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： ANDRES-GIL JOSE IGNACIO ,  MARTINEZ-JIMENEZ PEDRO CAMPO D ,  FERNANDEZ-GADEA FRANCISCO CAMP ,  SIPIDO VICTOR KAREL

    IPC: A61K31/00 ,  A61K31/55 ,  A61K31/551 ,  A61K31/5513 ,  A61K31/553 ,  A61P1/00 ,  A61P9/00 ,  A61P9/12 ,  A61P25/06 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D237/30 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07D498/14 ,  C07D498/16

    Abstract: PCT No. PCT/EP97/01830 Sec. 371 Date Oct. 6, 1998 Sec. 102(e) Date Oct. 6, 1998 PCT Filed Apr. 9, 1997 PCT Pub. No. WO97/39001 PCT Pub. Date Oct. 23, 1997This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero to 6; p is zero to 3; q is zero to 3; r is zero to 3; R1 and R2 each independently are hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; trihalomethylcarbonyl; 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; each R3 and R4 independently are halo, cyano, hydroxy, trihalomethyl, trihalomethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)-aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl or C1-6alkyloxycarbonyl; each R5 independently is C1-6alkyl, cyano or trihalomethyl; X is CR6R7, NR8, O, S, S(=O) or S(=O)2; each independently represents a bivalent aromatic heterocycle wherein the heterocycle may be selected from the group consisting of pyrrole, pyrrazole, imidazole, triazole, furane, thiophene, isoxazole, oxazole, isothiazole, thiazole, pyridine, pyridazine, pyrimidine, pyrazine and triazine; or one of the two bivalent aromatic heterocycles in the compounds of formula (I) may be 1,2-benzenediyl; and aryl is optionally substituted phenyl; it further relates to compositions comprising thesae compounds, as well as their use as therapeutic agents in the treatment or the prevention of CNS disorders, cardiovascular disorders or gastrointestinal disorders.

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