公开(公告)号：JPH07215972A

公开(公告)日：1995-08-15

申请号：JP17037094

申请日：1994-06-30

Applicant: DUPHAR INT RES

Inventor： HARTOG JAN ,  VAN STEEN BARTHOLOMEUS J ,  MOS JOHANNES ,  SCHIPPER JACQUES

IPC: C07D405/14 ,  A61K31/495 ,  A61P25/00 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P43/00 ,  C07D209/00 ,  C07D275/00 ,  C07D295/00 ,  C07D319/00 ,  C07D405/12 ,  C07D417/12 ,  C07D417/14

公开(公告)号：NO318888B1

公开(公告)日：2005-05-18

申请号：NO20012339

申请日：2001-05-11

Applicant: DUPHAR INT RES

Inventor： MOS JOHANNES ,  FEENSTRA ROELOF W ,  LONG STEPHEN K ,  KRUSE CORNELIS GERRIT ,  VISSER GERBEN M ,  TOOROP GERRIT P

IPC: A61K31/40 ,  A61K31/4164 ,  A61K31/42 ,  A61K31/425 ,  A61K31/4439 ,  A61K31/496 ,  A61P25/00 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D209/34 ,  C07D235/26 ,  C07D263/58 ,  C07D277/68 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04

Abstract: The invention relates to a group of novel piperazine and piperidine derivatives of formula (I), wherein: S1 is hydrogen, halogen, alkyl (1-3C), CN, CF3, OCF3, SCF3, alkoxy (1-3C), amino or mono- or dialkyl (1-3C) substituted amino, or hydroxy; X represents NR3, S, CH2, O, SO or SO2, wherein R3 is H or alkyl (1-3C); . . . Z represents =C or -N; -R1 independently represent H or alkyl (1-3C), or R1 and R2 together can form a bridge 2 or 3 C-atoms; R4 is hydrogen or alkyl (1-3C); Q is methyl, ethyl, ethyl substituted with one or more fluorine atoms, cyclopropyl-methyl, optionally substituted with one or more fluorine atoms, and salts and prodrugs thereof. It has been found that these compounds have both partial dopamine D2-receptor agonism and partial serotonin 5-HT1A-receptor agonism mediated activities.

公开(公告)号：ES2217833T3

公开(公告)日：2004-11-01

申请号：ES99955980

申请日：1999-11-10

Applicant: DUPHAR INT RES

Inventor： TOOROP GERRIT P ,  FEENSTRA ROELOF W ,  VAN DER HEIJDEN JOHANNES A M ,  MOS JOHANNES ,  LONG STEPHEN K ,  VISSER GERBEN M

IPC: A61K31/40 ,  A61K31/4164 ,  A61K31/42 ,  A61K31/425 ,  A61K31/4439 ,  A61K31/496 ,  A61P25/00 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D209/34 ,  C07D235/26 ,  C07D263/58 ,  C07D277/68 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04

Abstract: The invention relates to a group of novel piperazine and piperidine derivatives of formula (I), wherein: S1 is hydrogen, halogen, alkyl (1-3C), CN, CF3, OCF3, SCF3, alkoxy (1-3C), amino or mono- or dialkyl (1-3C) substituted amino, or hydroxy; X represents NR3, S, CH2, O, SO or SO2, wherein R3 is H or alkyl (1-3C); . . . Z represents =C or -N; -R1 independently represent H or alkyl (1-3C), or R1 and R2 together can form a bridge 2 or 3 C-atoms; R4 is hydrogen or alkyl (1-3C); Q is methyl, ethyl, ethyl substituted with one or more fluorine atoms, cyclopropyl-methyl, optionally substituted with one or more fluorine atoms, and salts and prodrugs thereof. It has been found that these compounds have both partial dopamine D2-receptor agonism and partial serotonin 5-HT1A-receptor agonism mediated activities.

公开(公告)号：DE69428943T2

公开(公告)日：2002-08-01

申请号：DE69428943

申请日：1994-07-01

Applicant: DUPHAR INT RES

Inventor： HARTOG JAN ,  VAN STEEN B J ,  MOS JOHANNES ,  SCHIPPER JACQUES

IPC: C07D405/14 ,  A61K31/495 ,  A61P25/00 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P43/00 ,  C07D209/00 ,  C07D275/00 ,  C07D295/00 ,  C07D319/00 ,  C07D405/12 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention is concerned with compounds having 5-HT1A antagonistic activity useful in treating CNS disorders and having formula 2 wherein R1 is halogen, lower alkyl or alkoxy, hydroxy, trifluotomethyl or cyano, m has the value 1 or 2 and n has the value 0 or 1, A represents an alkylene chain containing 2-6 C-atoms which may be substituted with one or more lower alkyl groups or a monocyclic (hetero)aryl group, and B is methylene, ethylene, carbonyl, sulfinyl, sulfonyl or sulfur, and salts thereof.

公开(公告)号：AT208385T

公开(公告)日：2001-11-15

申请号：AT94201900

申请日：1994-07-01

Applicant: DUPHAR INT RES

Inventor： HARTOG JAN ,  VAN STEEN B J ,  MOS JOHANNES ,  SCHIPPER JACQUES

IPC: C07D405/14 ,  A61K31/495 ,  A61P25/00 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P43/00 ,  C07D209/00 ,  C07D275/00 ,  C07D295/00 ,  C07D319/00 ,  C07D405/12 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention is concerned with compounds having 5-HT1A antagonistic activity useful in treating CNS disorders and having formula 2 wherein R1 is halogen, lower alkyl or alkoxy, hydroxy, trifluotomethyl or cyano, m has the value 1 or 2 and n has the value 0 or 1, A represents an alkylene chain containing 2-6 C-atoms which may be substituted with one or more lower alkyl groups or a monocyclic (hetero)aryl group, and B is methylene, ethylene, carbonyl, sulfinyl, sulfonyl or sulfur, and salts thereof.

公开(公告)号：SK281681B6

公开(公告)日：2001-06-11

申请号：SK78894

申请日：1994-06-30

Applicant: DUPHAR INT RES

Inventor： HARTOG JAN ,  VAN STEEN BARTHOLOMEUS JOHANNE ,  MOS JOHANNES ,  SCHIPPER JACQUES

IPC: A61K31/495 ,  A61P25/00 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  C07D405/14 ,  A61P25/26 ,  A61P25/28 ,  A61P43/00 ,  C07D209/00 ,  C07D275/00 ,  C07D295/00 ,  C07D319/00 ,  C07D405/12 ,  C07D417/12 ,  C07D417/14 ,  C07D319/16

Abstract: The present invention is concerned with compounds having 5-HT1A antagonistic activity useful in treating CNS disorders and having formula 2 wherein R1 is halogen, lower alkyl or alkoxy, hydroxy, trifluotomethyl or cyano, m has the value 1 or 2 and n has the value 0 or 1, A represents an alkylene chain containing 2-6 C-atoms which may be substituted with one or more lower alkyl groups or a monocyclic (hetero)aryl group, and B is methylene, ethylene, carbonyl, sulfinyl, sulfonyl or sulfur, and salts thereof.

公开(公告)号：HUT75155A

公开(公告)日：1997-04-28

申请号：HU9401965

申请日：1994-06-30

Applicant: DUPHAR INT RES

Inventor： HARTOG JAN ,  MOS JOHANNES ,  SCHIPPER JACQUES ,  VAN STEEN BARTHOLOMEUS JOHANNE

IPC: A61K31/495 ,  A61P25/00 ,  A61P25/18 ,  C07D405/14 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P43/00 ,  C07D209/00 ,  C07D275/00 ,  C07D295/00 ,  C07D319/00 ,  C07D405/12 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention is concerned with compounds having 5-HT1A antagonistic activity useful in treating CNS disorders and having formula 2 wherein R1 is halogen, lower alkyl or alkoxy, hydroxy, trifluotomethyl or cyano, m has the value 1 or 2 and n has the value 0 or 1, A represents an alkylene chain containing 2-6 C-atoms which may be substituted with one or more lower alkyl groups or a monocyclic (hetero)aryl group, and B is methylene, ethylene, carbonyl, sulfinyl, sulfonyl or sulfur, and salts thereof.

公开(公告)号：SK78894A3

公开(公告)日：1995-03-08

申请号：SK78894

申请日：1994-06-30

Applicant: DUPHAR INT RES

Inventor： HARTOG JAN ,  VAN STEEN BARTHOLOMEUS J ,  MOS JOHANNES ,  SCHIPPER JACQUES

IPC: A61K31/495 ,  A61P25/00 ,  A61P25/18 ,  A61P25/20 ,  C07D405/14 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P43/00 ,  C07D209/00 ,  C07D275/00 ,  C07D295/00 ,  C07D319/00 ,  C07D405/12 ,  C07D417/12 ,  C07D417/14 ,  C07D319/16

Abstract: The present invention is concerned with compounds having 5-HT1A antagonistic activity useful in treating CNS disorders and having formula 2 wherein R1 is halogen, lower alkyl or alkoxy, hydroxy, trifluotomethyl or cyano, m has the value 1 or 2 and n has the value 0 or 1, A represents an alkylene chain containing 2 - 6 C-atoms which may be substituted with one or more lower alkyl groups or a monocyclic (hetero)aryl group, and B is methylene, ethylene, carbonyl, sulfinyl, sulfonyl or sulfur and salts thereof.

公开(公告)号：DK611489D0

公开(公告)日：1989-12-05

申请号：DK611489

申请日：1989-12-05

Applicant: DUPHAR INT RES

Inventor： HARTOG JAN ,  MOS JOHANNES

IPC: C07D209/08 ,  A61K31/495 ,  A61K31/496 ,  A61K31/55 ,  A61P1/08 ,  A61P25/00 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D209/30 ,  C07D215/40 ,  C07D241/04 ,  C07D241/42 ,  C07D241/44 ,  C07D249/18 ,  C07D261/20 ,  C07D263/56 ,  C07D263/58 ,  C07D265/36 ,  C07D277/64 ,  C07D277/82 ,  C07D295/12 ,  C07D295/13 ,  C07D307/79 ,  C07D311/14 ,  C07D311/18 ,  C07D311/58 ,  C07D317/62 ,  C07D317/66 ,  C07D319/08 ,  C07D319/18 ,  C07D319/20 ,  C07D321/10 ,  C07D327/06 ,  C07D333/50 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D521/00 ,  C07D319/16 ,  C07D311/08 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14

公开(公告)号：CZ299774B6

公开(公告)日：2008-11-19

申请号：CZ20011657

申请日：1999-11-10

Applicant: DUPHAR INT RES

Inventor： FEENSTRA ROELOF W ,  VAN DER HEIJDEN JOHANNES A M ,  MOS JOHANNES ,  LONG STEPHEN K ,  VISSER GERBEN M ,  KRUSE CORNELIS G ,  VAN SCHARRENBURG GUSTAAF J M ,  TOOROP GERRIT P

IPC: C07D401/04 ,  A61K31/40 ,  A61K31/4164 ,  A61K31/42 ,  A61K31/423 ,  A61K31/425 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/496 ,  A61P25/00 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D209/34 ,  C07D211/68 ,  C07D235/26 ,  C07D241/04 ,  C07D263/58 ,  C07D277/68 ,  C07D413/04 ,  C07D417/04

Abstract: Deriváty piperazinu a piperidinu vzorce I, kde S.sub.1.n. je vodík, halogen C.sub.1-3.n.alkyl, CN, CF.sub.3.n., OCF.sub.3.n., SCF.sub.3.n., C.sub.1-3.n.alkoxy, aminoskupina nebo aminoskupina substituovaná mono- nebo di-C.sub.1-3.n.alkylem, nebo hydroxyl; X je NR.sub.3.n., S, CH.sub.2.n., O, SO neboSO.sub.2.n., kde R.sub.3.n. je H nebo C.sub.1-3.n.alkyl; ...Z je H nebo C.sub.1-3.n.alkyl nebo R.sub.1.n. a R.sub.2.n. mohou spolecne tvorit mustek obsahující 2 až 3 atomy uhlíku; R.sub.4.n. je vodíknebo C.sub.1-3.n.alkyl; Q je methyl, ethyl, ethylsubstituovaný jedním nebo více fluory, cyklopropylmethyl, poprípade substituovaný jedním nebo více fluory a jejich soli. Mají aktivitu zprostredkovanou jak cástecným agonismem vuci receptoru dopaminuD.sub.2.n., tak cástecným agonismem vuci receptoru serotoninu 5-HT.sub.1A.n.. Jejich použití pri lécbe CNS, úzkosti, deprese a Parkinsonovy choroby.