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    73.
    发明专利
    未知

    公开(公告)号：NO972017L

    公开(公告)日：1997-04-30

    申请号：NO972017

    申请日：1997-04-30

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： SIPIDO VICTOR KAREL ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  ANDRES-GIL JOSE IGNACIO ,  MEERT THEO FRANS ,  GIL-LOPETEGUI PILAR

    IPC: A61K31/535 ,  A61K31/55 ,  A61P9/00 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/26 ,  C07D223/20 ,  C07D223/30 ,  C07D261/00 ,  C07D498/04

    Abstract: This invention concerns the compounds of formula (I), the pharmaceutically acceptable salts and stereoisomeric forms thereof, and also the N-oxide forms thereof. (I) wherein: R1 and R2 each independently are hydrogen; C1-6alkyl; C1-6alkylcarbonyl; trihalomethylcarbonyl; C1-6alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6alkylcarbonyloxy, C1-6alkyloxycarbonyl or aryl; 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; R3, R4, R5, R6, R9, R10, R11 or R12 each independently are hydrogen, halo, cyano, hydroxy, trifluoromethyl, trifluoromethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)-amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)-aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl, C1-6alkyloxy-carbonyl; R7 and R8 are each independently hydrogen, hydroxy, C1-6alkyl, C1-6alkyloxy or R7 and R8 taken together may form mono- or di(cyano)methylene, or together with the carbon atom to which they are attached form a carbonyl or a spiro substituent; or R7 and R8 taken together may form methylene; R13 is hydrogen, C1-6alkyl, or trifluoromethyl; R14 is hydrogen, C1-6alkyl, cyano, or trifluoromethyl; n is zero to 6. These compounds were tested as mCPP-antagonists in rats. The compounds of formula (I) may be used as therapeutic agents in the treatment or the prevention of CNS disorders, cardiovascular disorders or gastrointestinal disorders.

    74.
    发明专利
    未知

    公开(公告)号：BR9407298A

    公开(公告)日：1996-10-01

    申请号：BR9407298

    申请日：1994-08-12

    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.

    Vasoconstrictive substituted 2,3-dihydro-1,4-dioxinopyridines
    75.
    发明专利
    Vasoconstrictive substituted 2,3-dihydro-1,4-dioxinopyridines 未知

    公开(公告)号：AU4785696A

    公开(公告)日：1996-08-27

    申请号：AU4785696

    申请日：1996-01-30

    Applicant: JANSSEN PHARMACEUTICA NV

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

    IPC: A61K31/435 ,  A61P9/08 ,  A61P25/04 ,  A61P25/06 ,  C07D491/04 ,  C07D491/056

    Abstract: PCT No. PCT/EP96/00396 Sec. 371 Date Aug. 6, 1997 Sec. 102(e) Date Aug. 6, 1997 PCT Filed Jan. 30, 1996 PCT Pub. No. WO96/24596 PCT Pub. Date Aug. 15, 1996The present invention is concerned with compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts 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 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 -C(NR5R6)=C-R4 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.

    78.
    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.

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