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51. 发明专利

DE69826883T2 未知
公开(公告)号：DE69826883T2
公开(公告)日：2005-02-03
申请号：DE69826883
申请日：1998-10-27
申请人： NEUROSEARCH AS BALLERUP
发明人： PETERS DAN , OLSEN M , NIELSEN FELDBAEK , NIELSEN OSTERGAARD
IPC分类号： C07D217/22 , A61K31/4406 , A61K31/4418 , A61K31/4425 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/551 , A61P1/12 , A61P9/10 , A61P11/06 , A61P21/02 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/28 , A61P25/30 , A61P29/00 , C07D213/22 , C07D213/74 , C07D215/38 , C07D243/08 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D409/04 , C07D409/14 , C07D417/04 , C07D417/14
摘要： Heteroaryl diazacycloalkane derivatives (I) are new. Heteroaryl diazacycloalkane derivatives of formula (I) and their enantiomers or mixtures, isotopes and salts are new. [Image] n : 1-3 m : 0-2; R : H, alkyl, cycloalkyl, cycloalkylalkyl or aralkyl; R 1>aminophenyl; nitrophenyl; hydroxyphenyl; alkoxyphenyl; monocyclic 5-6 membered heterocyclyl (optionally substituted by alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, cycloalkoxy, alkenoxy, alkynoxy, methylenedioxy, halo, CF 3, OCF 3, CN, amino, NO 2, COOR 3, CONR 2R 3, NHCO 2R 2and/or OCONR 2R 3); aryl (optionally substituted by alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, cycloalkoxy, alkenoxy, alkynoxy, methylenedioxy, halo, CF 3, OCF 3, CN, amino and/or NO 2); X-alkyl-Y-alkyl (optionally alkyl substituted by alkoxy or thioalkoxy); X-(alkyl) o-aryl (optionally substituted by alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, cycloalkoxy, alkenoxy, alkynoxy, methylene-dioxy, halo, CF 3, OCF 3, CN, amino and/or NO 2); X-(alkyl) o-Z (optionally substituted by alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, cycloalkoxy, alkenoxy, alkynoxy, methylenedioxy, halo, CF 3, OCF 3, CN, amino and/or NO 2), monocyclic 5-6 membered heterocyclyl (optionally substituted by alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, cycloalkoxy, alkenoxy, alkynoxy, methylenedioxy, halo, CF 3, OCF 3, CN, amino and/or NO 2) (sic), bicyclic heterocyclyl comprising a 5-6 membered monocyclic heterocyclyl fused to a benzene ring (optionally substituted by alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, alkoxy-alkoxy, cycloalkoxy, alkenoxy, alkynoxy, methylenedioxy, halo, CF 3, OCF 3, CN, amino, NO 2, aryl optionally substituted by alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, cycloalkoxy, alkenoxy, alkynoxy, methylenedioxy, halo, CF 3, OCF 3, CN, amine and/or NO 2) or monocyclic 5-6 membered heterocyclyl (optionally substituted by alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, cycloalkoxy, alkenoxy, alkynoxy, methylenedioxy, halo, CF 3, OCF 3, CN, amino and/or NO 2); X, Y : O, S or NH, N-alkyl or Se; o : 0 or 1 and Z : 5-6 membered monocyclic heterocyclyl. ACTIVITY : Analgesic; Neuroprotective; Nootropic; Tranquilizer; Antiinflammatory; Antiaddictive; Antismoking; Anticonvulsant; Neuroleptic; Antidepressant; Antiasthmatic; Antianginal; Antimigraine. The affinity of 1-(6-chloro-5-methoxy-3-pyridyl)-homopiperazine fumaric acid salt for nicotinic Ach receptors was investigated in a test for in vitroinhibition of 3H-cytisine binding. The compound exhibited and IC 50value of 0.0007 mu M. MECHANISM OF ACTION : Nicotinic acetyl choline receptor ligand.

52. 发明专利

DE69817214T2 未知
公开(公告)号：DE69817214T2
公开(公告)日：2004-06-09
申请号：DE69817214
申请日：1998-11-05
申请人： NEUROSEARCH AS BALLERUP
发明人： PETERS DAN , OLSEN M , NIELSEN FELDBAEK , NIELSEN OSTERGAARD
IPC分类号： A61K31/4427 , A61K31/4439 , A61K31/4545 , A61K31/55 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/28 , A61P25/30 , A61P29/00 , C07D401/12 , C07D403/12 , A61K31/44
摘要： The present invention discloses compounds represented by the general formula any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein m is 1,2 or 3 n is 1, 2 or 3; R represents hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R represents a monocyclic 5 to 6 membered heterocyclic group which may be substituted one or more times; R represents a bicyclic heterocyclic group, composed of a 5 to 6 membered monocyclic heterocyclic group fused to a benzene ring, and which may be substituted one or more times. The compounds of the invention are useful as nicotinic ACh receptor ligands.

53. 发明专利

DE60003911T2 未知
公开(公告)号：DE60003911T2
公开(公告)日：2004-05-27
申请号：DE60003911
申请日：2000-04-19
申请人： NEUROSEARCH AS BALLERUP
发明人： NIELSEN SIMON FELDB K , PETERS DAN , NIELSEN ELSEBET OSTERGAARD , OLSEN GUNNAR M
IPC分类号： C07D213/61 , A61K31/44 , A61K31/4427 , A61K31/496 , A61K31/501 , A61K31/551 , A61K51/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/16 , A61P25/28 , A61P25/30 , A61P25/34 , C07D213/65 , C07D213/74 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D417/04 , C07D405/04 , C07D409/04 , C07D409/14 , C07D417/14 , A61K31/495
摘要： The present invention relates to novel heteroaryl diazacycloalkane derivatives, which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neurodegeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

54. 发明专利

DE69332366T2 未知
公开(公告)号：DE69332366T2
公开(公告)日：2003-06-18
申请号：DE69332366
申请日：1993-12-20
申请人： NEUROSEARCH AS BALLERUP
发明人： MOLDT PETER , SCHEEL-KRUEGER JOERGEN , JENSEN LEIF HELTH
IPC分类号： A61K31/435 , A61K31/46 , A61P25/00 , A61P25/24 , A61P25/26 , A61P25/30 , C07D451/02

55. 发明专利

DE69332366D1 未知
公开(公告)号：DE69332366D1
公开(公告)日：2002-11-14
申请号：DE69332366
申请日：1993-12-20
申请人： NEUROSEARCH AS BALLERUP
发明人： MOLDT PETER , SCHEEL-KRUEGER JOERGEN , JENSEN LEIF HELTH
IPC分类号： A61K31/435 , A61K31/46 , A61P25/00 , A61P25/24 , A61P25/26 , A61P25/30 , C07D451/02

56. 发明专利

DE69903053D1 未知
公开(公告)号：DE69903053D1
公开(公告)日：2002-10-24
申请号：DE69903053
申请日：1999-09-27
申请人： NEUROSEARCH AS BALLERUP
发明人： DAHL BJARNE H , CHRISTOPHERSEN PALLE
IPC分类号： A61K31/136 , A61K31/41 , A61P1/04 , A61P1/12 , A61P7/00 , A61P7/10 , A61P9/12 , A61P19/10 , A61P27/06 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07C225/22 , C07C229/56 , C07D249/08 , C07D257/04 , C07C227/18 , A61K31/195
摘要： The invention relates to compounds having the formula (I) or a pharmaceutically acceptable salt thereof. In the formula (I), X represents a group having the structural formula (II), and Y represents O or S. The compounds of the invention can be used a chloride channel blockers.

57. 发明专利

DE60303825D1 未知
公开(公告)号：DE60303825D1
公开(公告)日：2006-04-27
申请号：DE60303825
申请日：2003-08-13
申请人： NEUROSEARCH AS BALLERUP
发明人： GOULIAEV HAAHR , BROWN DALBY , WAETJEN FRANK
IPC分类号： C07D471/04 , C07D307/20 , C07D487/04 , C12P17/04 , C12P41/00
摘要： The present invention is directed to a method of preparing enantiomers of indole-2,3-dione-3-oxime derivatives.

58. 发明专利

DE69922936T2 未知
公开(公告)号：DE69922936T2
公开(公告)日：2005-12-08
申请号：DE69922936
申请日：1999-03-30
申请人： NEUROSEARCH AS BALLERUP
发明人： WAETJEN FRANK , DREJER JOERGEN
IPC分类号： C07D487/04 , A61K31/404 , A61K31/4738 , A61K31/5517 , A61P9/00 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/30 , A61P43/00 , C07D471/04 , A61K31/44 , A61K31/40 , A61K31/55
摘要： The present invention relates to the use of indole-2,3-dione-3-oxime derivatives in a method of combating diseases and disorders associated with or mediated by the release of excitatory amino acids.

59. 发明专利

DE69922986T2 未知
公开(公告)号：DE69922986T2
公开(公告)日：2005-07-07
申请号：DE69922986
申请日：1999-10-19
申请人： NEUROSEARCH AS BALLERUP
发明人： DAHL BJARNE H , CHRISTOPHERSEN PALLE
IPC分类号： C07D233/34 , A61K31/00 , A61K31/17 , A61K31/18 , A61K31/192 , A61K31/41 , A61K31/4166 , A61K31/4439 , A61K31/496 , A61P1/04 , A61P1/12 , A61P7/06 , A61P9/10 , A61P9/12 , A61P17/02 , A61P19/08 , A61P19/10 , A61P27/06 , A61P29/00 , A61P35/00 , A61P35/04 , A61P37/08 , A61P43/00 , C07C233/00 , C07C233/64 , C07C273/18 , C07C275/30 , C07C275/32 , C07C275/42 , C07C381/00 , C07C381/06 , C07D233/32 , C07D257/04 , C07D401/12 , A61K31/19
摘要： The present invention discloses compounds having the formula wherein one of R , R and R is a acidic functional group having a pKa value below 8 or a group which is convertible in vivo to such a group; and Y represents wherein R and R independently represents hydrogen or lower alkyl; X represents O or S. The compounds are useful as chloride channel blockers.

60. 发明专利

DE60020556D1 未知
公开(公告)号：DE60020556D1
公开(公告)日：2005-07-07
申请号：DE60020556
申请日：2000-05-12
申请人： NEUROSEARCH AS BALLERUP
发明人： JENSEN BO SKAANING , TEUBER LENE , STR B K DORTE , CHRISTOPHERSEN PALLE , OLESEN PETER NEUROSEARCH A S
IPC分类号： C07D277/82 , A61K31/4184 , A61K31/423 , A61K31/427 , A61K31/428 , A61K45/00 , A61P1/00 , A61P1/16 , A61P3/10 , A61P7/00 , A61P7/06 , A61P9/00 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/00 , A61P13/10 , A61P13/12 , A61P15/00 , A61P15/10 , A61P17/00 , A61P17/06 , A61P17/14 , A61P19/00 , A61P19/02 , A61P21/00 , A61P21/04 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/00 , A61P27/02 , A61P27/16 , A61P29/00 , A61P31/00 , A61P31/12 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/00 , A61P37/08 , C07D235/14 , C07D263/58 , C07D277/60 , C07D277/84
摘要： The present invention relates to ion channel modulating agents. More particularly, the present invention relates to a particular class of chemical compounds represented by general formula (I) that has proven useful as modulators of SKCa, IKCa and BKCa channels. In further aspects, the present invention relates to the use of these SK/IK/BK channel modulating agents for the manufacture of medicaments and pharmaceutical compositions comprising the SK/IK/BK channel modulating agents. The SK/IK/BK channel modulating agents of the invention are useful for the treatment or alleviation of diseases and conditions associated with the SK/IK/BK channels.

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