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1. 发明专利

CA2063314A1 ALKYLENEDIOXYPHENYL ETHER DERIVATIVES HAVING ANTI-ISCHAEMIC, MEMORY ENHANCING AND ANTI-CONVULSIVE ACTIVITY 未知
公开(公告)号：CA2063314A1
公开(公告)日：1992-09-21
申请号：CA2063314
申请日：1992-03-18
申请人： DUPHAR INT RES
发明人： LANGE JOSEPHUS H M , TOOROP GERRIT P , VAN WIJNGAARDEN INEKE , DEN HARTOG JACOBUS A J
IPC分类号： C07D317/64 , C07D319/18 , C07D405/06 , A61K31/36 , A61K31/445 , A61K31/495
摘要： DIR 0482 The invention relates to compounds having anti-ischaemic activity, memory enhancing activity and anti-convulsive activity of the formulae 1A and 1B (1A) (1B) wherein -R1 + R2 together form an alkylene group having 1-3 C-atoms which may be substituted with one or more alkyl group(s) having 13 C-atoms; -Z is methylene optionally substituted with one alkyl group having 1-3 C-atoms, or with one phenylalkyl group with 1-3 C-atoms in the alkyl group, which phenyl group may be substituted with a group (R5)p wherein. R6 is halogen, hydroxy, alkyl or hydroxyalkyl having 1-5 C-atoms, alkoxy having 1-3 C-atoms, S-alkyl, S(O)-alkyl or S(O)2-alkyl having 1-3 Catoms, amino, mono- or dialkylamino having 1-3 C-atoms per alkyl group, trifluoromethyl, trifluoromethoxy, a sulphonylamido group SO2NHR or a carbalkoxy group COOR wherein R is alkyl having 1-4 C-atoms, the group COOH, SO3H,CONH2, the amidino group or cyano group, and p has the value 0-3; -R3 and R4 independent of each other represent hydrogen, alkyl having 1-10 C-atoms, alkenyl or alkynyl having 3-10 Catoms, cycloalkyi having 3-8 C-atoms, cycloalkyl-alkyl having 3-8 ring atoms and 1-5 C-atoms in the alkyl group, phenylalkyl or heteroaryl-alkyl having 1-5 C-atoms in the alkyl group, phenylalkenyl, heteroaryl-alkenyl, phenylalkynyl or heteroaryl-alkynyl group having 3-5 C-atoms in the alkenyl group or alkynyl group, which groups R3 and R4 may be substituted with a group (R8)p wherein R6 and p have the above mentioned meanings, or wherein R3+R4 together with DIR 0482 the nitrogen atom form a saturated or unsaturated heterocyclic group of 5-7 ring atoms, which may contain a second hetero-atom from the group consisting of oxygen, sulphur and nitrogen, which ring may be substituted with a group (R5)p wherein R6 and p have the above mentioned meanings, or with phenylalkyl, heteroarylalkyl, phenylalkenyl, heteroaryl-alkenyl, phenylalkynyl or heteroaryl-alkynyl having at most 3 C-atoms in the alkyl, alkenyl or alkynyl part, which groups may be substituted with a group (R6)p wherein R6 and p have the above-mentioned meanings, or which ring may be annelated with a phenyl group; -R5 is alkyl having 1-12 C-atoms, alkenyl or alkynyl having 3-12 C-atoms, cycloalkyl having 3-8 C-atoms, cycloalkyl-alkyl having 3-8 ring atoms and 1-5 C-atoms in the alkyl group, phenylalkyl or heteroaryl-alkyl having 1-5 C-atoms in the alkyl sub-group, phenylalkenyl, heteroaryl-alkenyl, phenylalkynyl or heteroaryl-alkynyl having 3-5 C-atoms in the alkenyl subgroup or alkynyl sub-group, which groups may be substituted with a group (R6)p, wherein R6 and p have the abovementioned meanings, and which alkyl sub-groups, alkenyl sub-groups and alkynyl sub-groups may contain a group -O-, S- or CO, or a pharmacologically acceptable salt thereof

2. 发明专利

NO318888B1 未知
公开(公告)号：NO318888B1
公开(公告)日：2005-05-18
申请号：NO20012339
申请日：2001-05-11
申请人： DUPHAR INT RES
发明人： MOS JOHANNES , FEENSTRA ROELOF W , LONG STEPHEN K , KRUSE CORNELIS GERRIT , VISSER GERBEN M , TOOROP GERRIT P
IPC分类号： 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
摘要： 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.

3. 发明专利

ES2217833T3 未知
公开(公告)号：ES2217833T3
公开(公告)日：2004-11-01
申请号：ES99955980
申请日：1999-11-10
申请人： DUPHAR INT RES
发明人： TOOROP GERRIT P , FEENSTRA ROELOF W , VAN DER HEIJDEN JOHANNES A M , MOS JOHANNES , LONG STEPHEN K , VISSER GERBEN M
IPC分类号： 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
摘要： 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.

4. 发明专利

CZ299774B6 Nové piperazinové a piperidinové slouceniny, zpusob jejich prípravy a jejich použití 未知
公开(公告)号：CZ299774B6
公开(公告)日：2008-11-19
申请号：CZ20011657
申请日：1999-11-10
申请人： DUPHAR INT RES
发明人： 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分类号： 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
摘要： 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.

5. 发明专利

HK1039489A1 New piperazine and piperidine compounds. 未知
公开(公告)号：HK1039489A1
公开(公告)日：2002-04-26
申请号：HK02100871
申请日：2002-02-05
申请人： DUPHAR INT RES
发明人： FEENSTRA ROELOF W , HEIJDEN VAN DER JOHANNES A M , MOS JOHANNES , LONG STEPHEN K , VISSER GERBEN M , KRUSE CORNELIS G , SCHARRENBURG VAN GUSTAAF J M , TOOROP ANNE G , TOOROP GERRIT P
IPC分类号： 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 , C07D , A61K , A61P
摘要： 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.

6. 发明专利

AU9624198A Quinoline and quinazoline derivatives having corticotropin releasing factor (crf) antagonist activity 未知
公开(公告)号：AU9624198A
公开(公告)日：1999-03-29
申请号：AU9624198
申请日：1998-09-07
申请人： DUPHAR INT RES
发明人： HARTOG JACOBUS A J DEN , VISSER GERBEN M , TOOROP GERRIT P , JANSEN JOHANNES W C M , RONKEN ERIC , TULP MARTINUS T M , REINDERS JAN H
IPC分类号： A61K31/4375 , A61K31/47 , A61K31/4709 , A61K31/517 , A61K31/519 , A61P25/00 , A61P25/20 , A61P25/22 , A61P25/24 , A61P43/00 , C07D215/42 , C07D239/94 , C07D401/04 , C07D401/12 , C07D471/04 , C07D487/04
摘要： The present invention relates to novel compounds, to a method for the preparation of these novel compounds, to pharmaceutical compositions containing one or more of these compounds as an active component and to methods of using these in the treatment of stress-related disorders.

7. 发明专利

CA2270777A1 QUINOLINE AND QUINAZOLINE DERIVATIVES HAVING CORTICOTROPIN RELEASING FACTOR (CRF) ANTAGONIST ACTIVITY 未知
公开(公告)号：CA2270777A1
公开(公告)日：1999-03-18
申请号：CA2270777
申请日：1998-09-07
申请人： DUPHAR INT RES
发明人： RONKEN ERIC , TULP MARTINUS T M , REINDERS JAN H , JANSEN JOHANNES W C M , TOOROP GERRIT P , VISSER GERBEN M , DEN HARTOG JACOBUS A J
IPC分类号： A61K31/4375 , A61K31/47 , A61K31/4709 , A61K31/517 , A61K31/519 , A61P25/00 , A61P25/20 , A61P25/22 , A61P25/24 , A61P43/00 , C07D215/42 , C07D239/94 , C07D401/04 , C07D401/12 , C07D471/04 , C07D487/04
摘要： The invention relates to novel quinoline and quinazoline derivatives having corticotropin releasing factor (CRF) antagonist activity. It has been found that compounds having formula (I) wherein A is CH or N, ring Q is phenyl, pyridyl, pyrimidinyl or pyridazinyl, optionally substituted with one or two groups R4; ring Y is phenyl, pyridyl, pyrimidinyl, pyridazinyl or pyrazinyl; R1 and R2 are optionally branched C1-6-alkyl, C3-6-alkenyl, C3-6-alkynyl, C3-6-cycloalkyl-C1-4-alkyl, phenyl-C1-4-alkyl, 5- or 6-membered saturated or unsaturated heterocyclyl-C1-4-alkyl, which groups R1 and R2 can be substituted with OH, C1-3-alkoxy, C1-3-alkoxycarbonyl, optionally mono- or di-(C1-3-alkyl)substituted amino, halogen or cyano; R3 is H, C1-3-alkyl optionally substituted with one or more fluorine atoms, or R3 is halogen, methoxy or ethoxy; R4 is C1-3-alkyl optionally substituted with one or more fluorine atoms, or R4 is halogen, methoxy, ethoxy, amino, mono- or di-substituted amino, or cyano; R5 is halogen, optionally branched C1-6-alkyl, C3-6-alkenyl, C3-6-alkynyl, C3-6-cycloalkyl-C1-4-alkyl, O-(C1-6-alkyl), S-(C1-6-alkyl), SO2 (C1-6-alkyl), hydroxy, cyano, nitro, trifluoromethyl, SO2NH2, SO2N(mono- or diC1-4-alkyl), formyl, CO-(C1-6-alkyl), COOH, COO-(C1-6-alkyl), CONH2, CON(monoor di-C1-4-alkyl), amino, N(mono or di-C1-4-alkyl), NHCO(C1-6-alkyl), NHSO2 (C1-6-alkyl), which groups R5 can be identical or different; and n has the value 0 to 4; with the proviso that the group NR1R2 is not diethylamino, ethyl,n-propylamino or ethyl,n-butylamino, if A is CH, Q is unsubstituted phenyl, R3 is methyl, and substituent Y with the group(s) R5 is 2,4,6trimethylphenyl, and salts thereof have good CRF antagonist activity.

8. 发明专利

AT267183T 未知
公开(公告)号：AT267183T
公开(公告)日：2004-06-15
申请号：AT99955980
申请日：1999-11-10
申请人： DUPHAR INT RES
发明人： TOOROP GERRIT P , 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 ANNE G HF
IPC分类号： 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
摘要： 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.

9. 发明专利

SK6492001A3 NEW PIPERAZINE AND PIPERIDINE COMPOUNDS 未知
公开(公告)号：SK6492001A3
公开(公告)日：2001-10-08
申请号：SK6492001
申请日：1999-11-10
申请人： DUPHAR INT RES
发明人： 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分类号： 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
摘要： 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.

10. 发明专利

BR9915293A 未知
公开(公告)号：BR9915293A
公开(公告)日：2001-08-07
申请号：BR9915293
申请日：1999-11-10
申请人： DUPHAR INT RES
发明人： TOOROP GERRIT P , FEENSTRA ROELOF W , HEIJDEN JOHANNES A M VAN DER , MOS JOHANNES , LONG STEPHEN K , VISSER GERBEN M , KRUSE CORNELIS G , SCHARRENBURG GUSTAAF J M , TOOROP ANNE G
IPC分类号： 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
摘要： 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.

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