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公开(公告)号：AU2925799A
公开(公告)日：1999-08-23
申请号：AU2925799
申请日：1999-02-05
Applicant: DUPHAR INT RES
Inventor： HARTOG JACOBUS A J DEN , VISSER GERBEN M , STEEN BARTHOLOMEUS J VAN , TULP MARTINUS T M , RONKEN ERIC , KRUSE CORNELIS G
IPC: A61K31/4709 , A61K31/496 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D201/00 , C07D215/38 , C07D401/12 , C07D405/12
Abstract: The present invention relates to a group of novel 2-aminoquinoline derivatives which are potent and selective agonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R1)n represents 1 or 2 substituents, which can be the same or different, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, and mono- or dialkyl (C1-2)amino, or two groups R1 at adjacent carbon atoms together with the benzene ring may form the benzdioxane group or benzofuran group, X represents nitrogen or carbon, and the dotted line may represent a double bond, (R2)p represents 0, 1 or 2 substituents, which can be the same or different, from the group methyl and ethyl, or (R2)p is a methylene bridge or ethylene bridge, R3 is hydrogen or methyl, and (R)m represents 0, 1, or 2 substituents, which can be the same or different and can be located at all available positions of the quinolyl group, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, and mono- or dialkyl (C1-2)amino, on the understanding that R1 cannot represent o-OCH3 when X is nitrogen, (R2)p and R3 are hydrogen, m is 0 and n is 1
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公开(公告)号：NO984380L
公开(公告)日：1999-03-25
申请号：NO984380
申请日：1998-09-21
Applicant: DUPHAR INT RES
Inventor： FEENSTRA ROELOF W , HARTOG JACOBUS A J DEN , KRUSE CORNELIS G , TULP MARTINUS T M , LONG STEPHEN K
IPC: C07D411/12 , A61K31/00 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/55 , A61K31/551 , A61K31/5513 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/14 , C07D411/14 , C07D413/04 , C07D413/12 , C07D413/14
Abstract: The invention relates to a group of new piperazine and piperidine compounds having interesting pharmacological properties. It has been found that compounds of the formula (a) wherein A represents a heterocyclic group of 5-7 ring atoms wherein 1 - 3 heteroatoms from the group O, N and S are present, R1 is hydrogen or fluoro, R2 is C1-4-alkyl, C1-4-alkoxy or an oxo group, and p is 0, 1 or 2, Z represents carbon or nitrogen, and the dotted line is a single bond when Z is nitrogen, and a single or double bond when Zis carbon, R3 and R4 independently are hydrogen or C1-4-alkyl, n has the value 1 or 2, R5 is 2-pyridyl, 3-pyridyl or 4-pyridyl substituted at the meta-position with respect to the methylene bridge with a group Y, and optionally substituted with (R6)q, Y is phenyl, furanyl or thienyl, which groups may be substituted with 1-3 substituents of the group hydroxy, halogen, CF3, C1-4-alkoxy, C1-4-alkyl, cyano, aminocarbonyl, mono- or di-C1-4-alkylaminocarbonyl, R6 is halogen, hydroxy, C1-4-alkoxy or C1-4-alkyl, and q is 0, 1, 2 or 3 and salts thereof, show affinities for both the dopamine D2-, D3-, D4- receptors and the serotonin 5-HT1A receptor.
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公开(公告)号：PT1054885E
公开(公告)日：2007-10-03
申请号：PT99914450
申请日：1999-02-05
Applicant: DUPHAR INT RES
Inventor： HARTOG JACOBUS A J DEN , VISSER GERBEN M , STEEN BARTHOLOMEUS J VAN , RONKEN ERIC , LANGE JOSEPHUS H M , TULP MARTINUS T M , KRUSE CORNELIS G
IPC: C07D413/14 , A61K31/445 , A61K31/454 , A61K31/55 , A61P25/00 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00
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公开(公告)号：NO312835B1
公开(公告)日：2002-07-08
申请号：NO984380
申请日：1998-09-21
Applicant: DUPHAR INT RES
Inventor： FEENSTRA ROELOF W , HARTOG JACOBUS A J DEN , KRUSE CORNELIS GERRIT , TULP MARTINUS THEODORUS MARIA , LONG STEPHEN K
IPC: C07D411/12 , A61K31/00 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/55 , A61K31/551 , A61K31/5513 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/14 , C07D411/14 , C07D413/04 , C07D413/12 , C07D413/14
Abstract: The invention relates to a group of new piperazine and piperidine compounds having interesting pharmacological properties. It has been found that compounds of the formula (a) wherein A represents a heterocyclic group of 5-7 ring atoms wherein 1 - 3 heteroatoms from the group O, N and S are present, R1 is hydrogen or fluoro, R2 is C1-4-alkyl, C1-4-alkoxy or an oxo group, and p is 0, 1 or 2, Z represents carbon or nitrogen, and the dotted line is a single bond when Z is nitrogen, and a single or double bond when Zis carbon, R3 and R4 independently are hydrogen or C1-4-alkyl, n has the value 1 or 2, R5 is 2-pyridyl, 3-pyridyl or 4-pyridyl substituted at the meta-position with respect to the methylene bridge with a group Y, and optionally substituted with (R6)q, Y is phenyl, furanyl or thienyl, which groups may be substituted with 1-3 substituents of the group hydroxy, halogen, CF3, C1-4-alkoxy, C1-4-alkyl, cyano, aminocarbonyl, mono- or di-C1-4-alkylaminocarbonyl, R6 is halogen, hydroxy, C1-4-alkoxy or C1-4-alkyl, and q is 0, 1, 2 or 3 and salts thereof, show affinities for both the dopamine D2-, D3-, D4- receptors and the serotonin 5-HT1A receptor.
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公开(公告)号：TR9801866A1
公开(公告)日：1999-04-21
申请号：TR9801866
申请日：1998-09-21
Applicant: DUPHAR INT RES
Inventor： TRA ROELOF W FEENS , HARTOG JACOBUS A J DEN , KRUSE CORNELIS G , TULP MARTINUS T M , LONG STEPHEN K
IPC: C07D411/12 , A61K31/00 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/55 , A61K31/551 , A61K31/5513 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/14 , C07D411/14 , C07D413/04 , C07D413/12 , C07D413/14
CPC classification number: C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12
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Patent Agency Ranking
公开(公告)号：TR199801866A1
公开(公告)日：1999-04-21
申请号：TR9801866
申请日：1998-09-21
Applicant: DUPHAR INT RES
Inventor： TRA ROELOF W FEENS , HARTOG JACOBUS A J DEN , KRUSE CORNELIS G , TULP MARTINUS T M , LONG STEPHEN K
IPC: C07D411/12 , A61K31/00 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/55 , A61K31/551 , A61K31/5513 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/14 , C07D411/14 , C07D413/04 , C07D413/12 , C07D413/14
Abstract: The invention relates to a group of new piperazine and piperidine compounds having interesting pharmacological properties. It has been found that compounds of the formula (a) wherein A represents a heterocyclic group of 5-7 ring atoms wherein 1 - 3 heteroatoms from the group O, N and S are present, R1 is hydrogen or fluoro, R2 is C1-4-alkyl, C1-4-alkoxy or an oxo group, and p is 0, 1 or 2, Z represents carbon or nitrogen, and the dotted line is a single bond when Z is nitrogen, and a single or double bond when Zis carbon, R3 and R4 independently are hydrogen or C1-4-alkyl, n has the value 1 or 2, R5 is 2-pyridyl, 3-pyridyl or 4-pyridyl substituted at the meta-position with respect to the methylene bridge with a group Y, and optionally substituted with (R6)q, Y is phenyl, furanyl or thienyl, which groups may be substituted with 1-3 substituents of the group hydroxy, halogen, CF3, C1-4-alkoxy, C1-4-alkyl, cyano, aminocarbonyl, mono- or di-C1-4-alkylaminocarbonyl, R6 is halogen, hydroxy, C1-4-alkoxy or C1-4-alkyl, and q is 0, 1, 2 or 3 and salts thereof, show affinities for both the dopamine D2-, D3-, D4- receptors and the serotonin 5-HT1A receptor.
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公开(公告)号：NO984380A
公开(公告)日：1999-03-25
申请号：NO984380
申请日：1998-09-21
Applicant: DUPHAR INT RES
Inventor： FEENSTRA ROELOF W , HARTOG JACOBUS A J DEN , KRUSE CORNELIS G , TULP MARTINUS T M , LONG STEPHEN K
IPC: C07D411/12 , A61K31/00 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/55 , A61K31/551 , A61K31/5513 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/14 , C07D411/14 , C07D413/04 , C07D413/12 , C07D413/14
CPC classification number: C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12
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公开(公告)号：ID20895A
公开(公告)日：1999-03-25
申请号：ID981269
申请日：1998-09-21
Applicant: DUPHAR INT RES
Inventor： FEENSTRA ROELOF W , HARTOG JACOBUS A J DEN , KRUSE CORNELIS G , TULP MARTINUS T M , LONG STEPHEN K
IPC: C07D411/12 , A61K31/00 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/55 , A61K31/551 , A61K31/5513 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/14 , C07D411/14 , C07D413/04 , C07D413/12 , C07D413/14
Abstract: The invention relates to a group of new piperazine and piperidine compounds having interesting pharmacological properties. It has been found that compounds of the formula (a) wherein A represents a heterocyclic group of 5-7 ring atoms wherein 1 - 3 heteroatoms from the group O, N and S are present, R1 is hydrogen or fluoro, R2 is C1-4-alkyl, C1-4-alkoxy or an oxo group, and p is 0, 1 or 2, Z represents carbon or nitrogen, and the dotted line is a single bond when Z is nitrogen, and a single or double bond when Zis carbon, R3 and R4 independently are hydrogen or C1-4-alkyl, n has the value 1 or 2, R5 is 2-pyridyl, 3-pyridyl or 4-pyridyl substituted at the meta-position with respect to the methylene bridge with a group Y, and optionally substituted with (R6)q, Y is phenyl, furanyl or thienyl, which groups may be substituted with 1-3 substituents of the group hydroxy, halogen, CF3, C1-4-alkoxy, C1-4-alkyl, cyano, aminocarbonyl, mono- or di-C1-4-alkylaminocarbonyl, R6 is halogen, hydroxy, C1-4-alkoxy or C1-4-alkyl, and q is 0, 1, 2 or 3 and salts thereof, show affinities for both the dopamine D2-, D3-, D4- receptors and the serotonin 5-HT1A receptor.
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公开(公告)号：ZA907493B
公开(公告)日：1992-01-29
申请号：ZA907493
申请日：1990-09-19
Applicant: DUPHAR INT RES
Inventor： WITIAK DONALD T , DONALD T WITIAK , WIJNGAARDEN INEKE VAN , INEKE VAN WIJNGAARDEN , NAIR RAGHUNATAN V , RAGHUNATAN V NAIR , LANGE JOSEPHUS H M , JOSEPHUS H M LANGE , HARTOG JACOBUS A J DEN , JACOBUS A J DEN HARTOG
IPC: A61K31/357 , A61K31/36 , A61K31/443 , A61K31/445 , A61K31/495 , A61K31/535 , A61P9/00 , A61P9/08 , A61P9/10 , C07C217/58 , C07D295/096 , C07D317/64 , C07D319/18 , C07D321/10 , C07D405/06 , C07D , A61K , C07C
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公开(公告)号：ZA9007493B
公开(公告)日：1992-01-29
申请号：ZA9007493
申请日：1990-09-19
Applicant: DUPHAR INT RES
Inventor： WITIAK DONALD T , DONALD T WITIAK , WIJNGAARDEN INEKE VAN , INEKE VAN WIJNGAARDEN , NAIR RAGHUNATAN V , RAGHUNATAN V NAIR , LANGE JOSEPHUS H M , JOSEPHUS H M LANGE , HARTOG JACOBUS A J DEN , JACOBUS A J DEN HARTOG
IPC: A61K31/357 , A61K31/36 , A61K31/443 , A61K31/445 , A61K31/495 , A61K31/535 , A61P9/00 , A61P9/08 , A61P9/10 , C07C217/58 , C07D295/096 , C07D317/64 , C07D319/18 , C07D321/10 , C07D405/06 , C07D , A61K , C07C
CPC classification number: C07D295/096 , C07C217/58 , C07D317/64 , C07D319/18 , C07D321/10
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