中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

18 records (took 0.022 seconds)

    DERIVADOS TETRACICLICOS DE OXAZEPINA Y TIAZEPINA SUSTITUIDOS CON AFINIDAD AL RECEPTOR DE 5-HT2.
    1.
    发明专利
    DERIVADOS TETRACICLICOS DE OXAZEPINA Y TIAZEPINA SUSTITUIDOS CON AFINIDAD AL RECEPTOR DE 5-HT2. 未知

    公开(公告)号：MX9703250A

    公开(公告)日：1997-07-31

    申请号：MX9703250

    申请日：1995-10-25

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： GADEA FRANCISCO JAVIER FERNAND ,  SIPIDO VICTOR KAREL ,  GIL JOSE IGNACIO ANDRES ,  MEERT THEO FRANS

    IPC: C07D498/04 ,  C07D513/04 ,  A61K31/535 ,  C07D261/00 ,  C07D267/00

    Abstract: Esta invencion se refiere a los compuestos de formula (I), las sales farmacéuticamente aceptables y las formas estereoisoméricas de las mismas, y también las formas de N-oxido de las mismas. En dicha formula, R1 y R2 son cada uno independientemente hidrogeno; C1-6 alquilo; C1-6 alquilcarbonilo; trihalometilcarbonilo; C1-6 alquilo sustituido con hidroxi, C1-6 alquiloxi, carboxilo, C1-6 alquilcarboniloxi, C1-6 alquiloxicarbonilo o arilo; o R1 y R2 considerados juntos con el átomo de nitrogeno al cual están unidos pueden formar un anillo de morfolinilo o un heterociclo sustituido opcionalmente; R3 y R10 son cada uno independientemente hidrogeno, halogeno, ciano, hidroxi, trifluorometilo, trifluorometoxi, carboxilo, nitro, amino, mono- o di(C1-6alquil)amino, C1-6 alquilcarbonilamino, aminosulfonilo, mono- o di(C1-6 alquil)-aminosulfonilo, C1-6 alquilo, C1-6 alquiloxi, C1-6 alquilcarbonilo, C1-6 alquiloxicarbonilo; R11 es hidrogeno, C1-6 alquilo o trifluorometilo; R12 es hidrogeno, C1-6 alquilo, ciano o trifluorometilo; n es 0 a 6; y X es 0,S,S(-O) o S(=O)2. Los compuestos de formula (I) pueden utilizarse como agentes terapéuticos en el tratamiento o la prevencion de trastornos del SNC, trastornos cardiovasculares o trastornos gastrointestinales.

    PDE IV inhibiting 2-cyanoiminoimidazole derivatives
    3.
    发明专利
    PDE IV inhibiting 2-cyanoiminoimidazole derivatives 未知

    公开(公告)号：AU719561B2

    公开(公告)日：2000-05-11

    申请号：AU4779297

    申请日：1997-09-24

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： FREYNE EDDY JEAN EDGARD ,  GADEA FRANCISCO JAVIER FERNAND ,  GIL JOSE IGNACIO ANDRES

    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.

    1,3-dihydro-1-(phenylalkyl)-2H-imidazol-2-one derivatives having PDEIV and cytokine activity
    4.
    发明专利
    1,3-dihydro-1-(phenylalkyl)-2H-imidazol-2-one derivatives having PDEIV and cytokine activity 未知

    公开(公告)号：AU702947B2

    公开(公告)日：1999-03-11

    申请号：AU5275596

    申请日：1996-03-28

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： FREYNE EDDY JEAN EDGARD ,  DIELS GASTON STANISLAS MARCELL ,  GIL JOSE IGNACIO ANDRES ,  GADEA FRANCISCO JAVIER FERNAND

    IPC: C07D233/32 ,  A61K31/415 ,  A61K31/4166 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P37/08 ,  C07D233/36 ,  C07D233/38 ,  C07D233/70 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12

    Abstract: The present invention describes the use of compounds for the manufacture of a medicament for treating warm-blooded animals suffering from disease states related to an abnormal enzymatic or catalytic activity of phosphodiesterase IV (PDE IV), and/or disease states related to a physiologically detrimental excess of cytokines, in particular allergic, atopic and inflammatory diseases, said compounds having the 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; halo; optionally substituted C1-6alkyl; trifluoromethyl; C3-6cycloalkyl; carboxyl; C1-4alkyloxycarbonyl; C3-6cycloalkylaminocarbonyl; aryl; Het1; or R4 is a radical of formula: -O-R6; or -NH-R7; R5 is hydrogen, halo, hydroxy or C1-6alkyl; or R4 and R5 taken together may form a bivalent radical of formula: -(CH2)n-; -CH2-CH2-O-CH2-CH2-; -CH2-CH2-N(R8)-CH2-CH2-; or -CH2-CH=CH-CH2-; Y is a direct bond, haloC1-4alkanediyl or C1-4alkanediyl; -A-B- is a bivalent radical of formula: -CR9=CR10-; or -CHR9-CHR10-; and L is hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C3-6alkenyl; optionally substituted piperidinyl; C1-6alkylsulfonyl or arylsulfonyl; aryl is optionally substituted phenyl; Het1 <

    Isoxazolidine derivatives
    5.
    发明专利
    Isoxazolidine derivatives 未知

    公开(公告)号：AU2385297A

    公开(公告)日：1997-11-07

    申请号：AU2385297

    申请日：1997-04-09

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： GIL JOSE IGNACIO ANDRES ,  MARTINEZ PEDRO ,  GADEA FRANCISCO JAVIER FERNAND ,  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.

    6.
    发明专利
    未知

    公开(公告)号：NO974602L

    公开(公告)日：1997-10-06

    申请号：NO974602

    申请日：1997-10-06

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： FREYNE EDDY JEAN EDGARD ,  DIELS GASTON STANISLAS MARCELL ,  GIL JOSE IGNACIO ANDRES ,  GADEA FRANCISCO JAVIER FERNAND

    IPC: A61K31/415 ,  A61K31/4166 ,  A61K31/44 ,  C07D233/32 ,  A61K31/4427 ,  A61K31/443 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P37/08 ,  C07D233/36 ,  C07D233/38 ,  C07D233/70 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12

    Abstract: The present invention describes the use of compounds for the manufacture of a medicament for treating warm-blooded animals suffering from disease states related to an abnormal enzymatic or catalytic activity of phosphodiesterase IV (PDE IV), and/or disease states related to a physiologically detrimental excess of cytokines, in particular allergic, atopic and inflammatory diseases, said compounds having the 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; halo; optionally substituted C1-6alkyl; trifluoromethyl; C3-6cycloalkyl; carboxyl; C1-4alkyloxycarbonyl; C3-6cycloalkylaminocarbonyl; aryl; Het1; or R4 is a radical of formula: -O-R6; or -NH-R7; R5 is hydrogen, halo, hydroxy or C1-6alkyl; or R4 and R5 taken together may form a bivalent radical of formula: -(CH2)n-; -CH2-CH2-O-CH2-CH2-; -CH2-CH2-N(R8)-CH2-CH2-; or -CH2-CH=CH-CH2-; Y is a direct bond, haloC1-4alkanediyl or C1-4alkanediyl; -A-B- is a bivalent radical of formula: -CR9=CR10-; or -CHR9-CHR10-; and L is hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C3-6alkenyl; optionally substituted piperidinyl; C1-6alkylsulfonyl or arylsulfonyl; aryl is optionally substituted phenyl; Het1 <

    7.
    发明专利
    未知

    公开(公告)号：NO974602D0

    公开(公告)日：1997-10-06

    申请号：NO974602

    申请日：1997-10-06

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： FREYNE EDDY JEAN EDGARD ,  DIELS GASTON STANISLAS MARCELL ,  GIL JOSE IGNACIO ANDRES ,  GADEA FRANCISCO JAVIER FERNAND

    IPC: A61K31/415 ,  A61K31/4166 ,  A61K31/44 ,  C07D233/32 ,  A61K31/4427 ,  A61K31/443 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P37/08 ,  C07D233/36 ,  C07D233/38 ,  C07D233/70 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12

    Abstract: The present invention describes the use of compounds for the manufacture of a medicament for treating warm-blooded animals suffering from disease states related to an abnormal enzymatic or catalytic activity of phosphodiesterase IV (PDE IV), and/or disease states related to a physiologically detrimental excess of cytokines, in particular allergic, atopic and inflammatory diseases, said compounds having the 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; halo; optionally substituted C1-6alkyl; trifluoromethyl; C3-6cycloalkyl; carboxyl; C1-4alkyloxycarbonyl; C3-6cycloalkylaminocarbonyl; aryl; Het1; or R4 is a radical of formula: -O-R6; or -NH-R7; R5 is hydrogen, halo, hydroxy or C1-6alkyl; or R4 and R5 taken together may form a bivalent radical of formula: -(CH2)n-; -CH2-CH2-O-CH2-CH2-; -CH2-CH2-N(R8)-CH2-CH2-; or -CH2-CH=CH-CH2-; Y is a direct bond, haloC1-4alkanediyl or C1-4alkanediyl; -A-B- is a bivalent radical of formula: -CR9=CR10-; or -CHR9-CHR10-; and L is hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C3-6alkenyl; optionally substituted piperidinyl; C1-6alkylsulfonyl or arylsulfonyl; aryl is optionally substituted phenyl; Het1 <

    1,3-dihydro-2h-imidazol-2-one derivatives having pde iv and cytokinin inhibiting activity
    8.
    发明专利
    1,3-dihydro-2h-imidazol-2-one derivatives having pde iv and cytokinin inhibiting activity 未知

    公开(公告)号：AU5497996A

    公开(公告)日：1996-10-23

    申请号：AU5497996

    申请日：1996-03-28

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： FREYNE EDDY JEAN EDGARD ,  DIELS GASTON STANISLAS MARCELL ,  GIL JOSE IGNACIO ANDRES ,  GADEA FRANCISCO JAVIER FERNAND

    IPC: A61K31/415 ,  A61K31/4166 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P37/08 ,  C07D233/32 ,  C07D233/38 ,  C07D233/70 ,  C07D405/04 ,  C07D405/06

    Abstract: PCT No. PCT/EP96/01393 Sec. 371 Date Sep. 29, 1997 Sec. 102(e) Date Sep. 29, 1997 PCT Filed Mar. 28, 1996 PCT Pub. No. WO96/31487 PCT Pub. Date Oct. 10, 1996The present invention concerns the compounds of formula (I) 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 is a bivalent radical of formula Alk is C1-4alkanediyl; -A-B- is a bivalent radical of formula: -CR6=CR7- or -CHR6-CHR7-; L is hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C3-6alkenyl; optionally substituted piperidinyl; C1-6alkylsulfonyl or arylsulfonyl; aryl is optionally substituted phenyl; Het1 is morpholinyl or optionally substituted pyridinyl, -furanyl, -thienyl, -hydroxypyridinyl, -imidazolyl, -thiazolyl, -oxazolyl, -isoquinolinyl, -quinolinonyl, -piperidinyl, -piperazinyl; and Het2 is morpholinyl or optionally substituted piperidinyl, -piperazinyl, -pyridinyl, -furanyl or -thienyl; having PDE IV and cytokine inhibiting activity. The invention also relates to processes for preparing the compounds of formula (I) and pharmaceutical compositions thereof.

Patent Agency Ranking