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    53.
    发明专利
    未知

    公开(公告)号：NO960647D0

    公开(公告)日：1996-02-19

    申请号：NO960647

    申请日：1996-02-19

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： LOMMEN GUY ROSALIA EUGENE VAN ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  ANDRES-GIL JOSE IGNACIO ,  MATESANZ-BALLESTEROS MARIA ENC

    IPC: A61K31/35 ,  A61K31/436 ,  A61K31/44 ,  A61K31/453 ,  A61K31/505 ,  A61P9/02 ,  A61P9/08 ,  A61P25/04 ,  A61P25/06 ,  C07D405/12 ,  C07D491/04 ,  C07D491/052

    Abstract: PCT No. PCT/EP94/02700 Sec. 371 Date Jan. 24, 1996 Sec. 102(e) Date Jan. 24, 1996 PCT Filed Aug. 12, 1994 PCT Pub. No. WO95/05381 PCT Pub. Date Feb. 23, 1995The present invention is concerned with compounds of formula (I) the pharmaceutically acceptable acid addition salts thereof, the +E,uns N+EE -oxides thereof and the stereochemically isomeric forms thereof, wherein =a1-a2=a3-a4= is a bivalent radical of formula:=N-CH=CH-CH=(a),=CH-N=CH-CH=(b),=CH-CH=N-CH=(c),=CH-CH=CH-N=(d),wherein in said bivalent radicals one or two hydrogen atoms can be substituted by halo, hydroxy, C1-6alkyl or C1-6alkyloxy; R1 is hydrogen or C1-6alkyl; R2 is hydrogen or C1-6alkyl; R3 is hydrogen or C1-6alkyl; Alk1 is C1-5alkanediyl; Alk2 is C2-15alkanediyl; Q is a five- or six-membered heterocyclic ring containing at least one nitrogen atom or a radical of formula (aa) wherein R4 is hydrogen, cyano, aminocarbonyl or C1-6alkyl; R5 is hydrogen, C1-6alkyl, C3-6alkenyl or C3-6alkynyl; R6 is hydrogen or C1-6alkyl; or R5 and R6 taken together may form a bivalent radical of formula -(CH2)4- or -(CH2)5-. Pharmaceutical compositions, preparations and use as a medicine are described.

    59.
    发明专利
    未知

    公开(公告)号：AT380794T

    公开(公告)日：2007-12-15

    申请号：AT96909151

    申请日：1996-03-28

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： FREYNE EDDY ,  DIELS GASTON ,  ANDRES-GIL JOSE IGNACIO ,  FERNANDEZ-GADEA FRANCISCO JAVI

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

    Abstract: PCT No. PCT/EP96/01395 Sec. 371 Date Sep. 30, 1997 Sec. 102(e) Date Sep. 30, 1997 PCT Filed Mar. 28, 1996 PCT Pub. No. WO96/31486 PCT Pub. Date Oct. 10, 1996The present invention concerns the compounds of 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; cyano; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl or aryl; R5 is hydrogen; cyano; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl or aryl; Y is a direct bond or C1-3alkanediyl; -A-B- is a bivalent radical of formula -CR6=CR7- or -CHR6-CHR7-; L is hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; C1-6alkylsulfonyl or arylsulfonyl; aryl is optionally substituted phenyl; Het is morpholinyl or optionally substituted piperidinyl, -piperazinyl, -pyridinyl;, -furanyl or -thienyl; having PDE IV and cytokine inhibiting activity. Further, pharmaceutical compositions, preparations and use as a medicine are described.

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