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1. 发明专利

DE69826883D1 未知
公开(公告)号：DE69826883D1
公开(公告)日：2004-11-11
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.

2. 发明专利

DE69810107T2 未知
公开(公告)号：DE69810107T2
公开(公告)日：2003-08-21
申请号：DE69810107
申请日：1998-05-29
申请人： NEUROSEARCH AS BALLERUP
发明人： PETERS DAN , OLSEN M , NIELSEN FELDBAEK , NIELSEN OSTERGAARD
IPC分类号： C07D223/04 , A61K31/395 , A61K31/4427 , A61K31/4709 , A61K31/55 , A61P21/00 , A61P25/00 , A61P25/16 , A61P25/28 , A61P25/34 , A61P29/00 , A61P43/00 , C07D223/06 , C07D225/02 , C07D401/04

3. 发明专利

DE60018312T2 未知
公开(公告)号：DE60018312T2
公开(公告)日：2005-08-18
申请号：DE60018312
申请日：2000-12-14
申请人： NEUROSEARCH AS BALLERUP
发明人： PETERS DAN , OLSEN M , NIELSEN ELSEBET OSTERGAARD , NIELSEN FELDBAEK , AHRING K , JORGENSEN TINO DYHRING
IPC分类号： A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K49/00 , A61K49/04 , A61K51/00 , A61P1/00 , A61P1/04 , A61P1/12 , A61P3/00 , A61P5/14 , A61P9/00 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/06 , A61P11/16 , A61P15/06 , A61P15/10 , A61P17/00 , A61P17/02 , A61P21/02 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/34 , A61P25/36 , A61P29/00 , A61P43/00 , C07D471/08 , C07D487/04 , C07D487/08 , A61K31/439 , A61K31/4995 , A61K31/55
摘要： The present invention relates to novel heteroaryl-diazabicycloalkanes 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.

4. 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.

5. 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.

6. 发明专利

DE60108639T2 未知
公开(公告)号：DE60108639T2
公开(公告)日：2005-07-07
申请号：DE60108639
申请日：2001-06-20
申请人： NEUROSEARCH AS BALLERUP
发明人： PETERS DAN , OLSEN GUNNAR M , NIELSEN ELSEBET OSTERGAARD , AHRING K , NIELSEN FELDBAEK , JORGENSEN DYHRING
IPC分类号： C07D487/04 , A61K31/551 , A61P1/04 , A61P1/12 , A61P3/04 , A61P5/16 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/06 , A61P15/00 , A61P15/10 , A61P17/10 , A61P21/00 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P25/36 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D471/04 , C07D487/08 , C07D471/08 , A61K31/395 , A61K31/439
摘要： The present invention relates to novel aryl and heteroaryl diazabicycloalkane derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. 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), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

7. 发明专利

DE60018312D1 未知
公开(公告)号：DE60018312D1
公开(公告)日：2005-03-31
申请号：DE60018312
申请日：2000-12-14
申请人： NEUROSEARCH AS BALLERUP
发明人： PETERS DAN , OLSEN M , NIELSEN ELSEBET OSTERGAARD , NIELSEN FELDBAEK , AHRING K , JORGENSEN TINO DYHRING
IPC分类号： A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K49/00 , A61K49/04 , A61K51/00 , A61P1/00 , A61P1/04 , A61P1/12 , A61P3/00 , A61P5/14 , A61P9/00 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/06 , A61P11/16 , A61P15/06 , A61P15/10 , A61P17/00 , A61P17/02 , A61P21/02 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/34 , A61P25/36 , A61P29/00 , A61P43/00 , C07D471/08 , C07D487/04 , C07D487/08 , A61K31/439 , A61K31/4995 , A61K31/55
摘要： The present invention relates to novel heteroaryl-diazabicycloalkanes 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.

8. 发明专利

DE60108639D1 未知
公开(公告)号：DE60108639D1
公开(公告)日：2005-03-03
申请号：DE60108639
申请日：2001-06-20
申请人： NEUROSEARCH AS BALLERUP
发明人： PETERS DAN , OLSEN GUNNAR M , NIELSEN ELSEBET OSTERGAARD , AHRING K , NIELSEN FELDBAEK , JORGENSEN DYHRING
IPC分类号： C07D487/04 , A61K31/551 , A61P1/04 , A61P1/12 , A61P3/04 , A61P5/16 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/06 , A61P15/00 , A61P15/10 , A61P17/10 , A61P21/00 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P25/36 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D471/04 , C07D487/08 , C07D471/08 , A61K31/395 , A61K31/439
摘要： The present invention relates to novel aryl and heteroaryl diazabicycloalkane derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. 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), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

9. 发明专利

DE69817214D1 未知
公开(公告)号：DE69817214D1
公开(公告)日：2003-09-18
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.

10. 发明专利

DE69810107D1 未知
公开(公告)号：DE69810107D1
公开(公告)日：2003-01-23
申请号：DE69810107
申请日：1998-05-29
申请人： NEUROSEARCH AS BALLERUP
发明人： PETERS DAN , PETERS, DAN , OLSEN, M.GUNNAR , NIELSEN, FELDBAEK SIMON , NIELSEN, OSTERGAARD ELSEBET , NIELSEN FELDBAEK , NIELSEN OSTERGAARD
IPC分类号： C07D223/04 , A61K31/395 , A61K31/4427 , A61K31/4709 , A61K31/55 , A61P21/00 , A61P25/00 , A61P25/16 , A61P25/28 , A61P25/34 , A61P29/00 , A61P43/00 , C07D223/06 , C07D225/02 , C07D401/04

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