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    1,3-dihydro-1-(phenylalkenyl)-2H-imidazol-2-one derivatives.
    41.
    发明专利
    1,3-dihydro-1-(phenylalkenyl)-2H-imidazol-2-one derivatives. 未知

    公开(公告)号：ZA962755B

    公开(公告)日：1997-10-06

    申请号：ZA962755

    申请日：1996-04-04

    Applicant: JANSSEN PHARMACEUTICA NV

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

    IPC: A61K31/415 ,  A61K31/4166 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P37/08 ,  C07D233/32 ,  C07D233/38 ,  C07D233/70 ,  C07D ,  A61K

    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.

    DERIVATIVES OF TETRACYCLIC SUBSTITUTED AZEPINES EXHIBITING AFFINITY IN RESPECT TO 5-HT2 RECEPTORS
    43.
    发明专利
    DERIVATIVES OF TETRACYCLIC SUBSTITUTED AZEPINES EXHIBITING AFFINITY IN RESPECT TO 5-HT2 RECEPTORS 未知

    公开(公告)号：PL319939A1

    公开(公告)日：1997-09-01

    申请号：PL31993995

    申请日：1995-10-25

    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.

    45.
    发明专利
    未知

    公开(公告)号：FI973245A0

    公开(公告)日：1997-08-06

    申请号：FI973245

    申请日：1997-08-06

    Applicant: JANSSEN PHARMACEUTICA NV

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

    IPC: A61K31/435 ,  A61P9/08 ,  A61P25/04 ,  A61P25/06 ,  C07D491/04 ,  C07D491/056 ,  C07D

    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.

    46.
    发明专利
    未知

    公开(公告)号：FI973245A

    公开(公告)日：1997-08-06

    申请号：FI973245

    申请日：1997-08-06

    Applicant: JANSSEN PHARMACEUTICA NV

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

    IPC: A61K31/435 ,  A61P9/08 ,  A61P25/04 ,  A61P25/06 ,  C07D491/04 ,  C07D491/056 ,  C07D

    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.

    48.
    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.

    49.
    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
    50.
    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.

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