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1. 发明专利

DE69922997T2 未知
公开(公告)号：DE69922997T2
公开(公告)日：2005-12-15
申请号：DE69922997
申请日：1999-12-03
申请人： NEUROSEARCH AS BALLERUP
发明人： JENSEN BO SKAANING , JOERGENSEN TINO DYHRING , AHRING PHILIP K , CHRISTOPHERSEN PALLE , STROEBAEK DORTE , TEUBER LENE , OLESEN SOEREN PETER
IPC分类号： A61K31/404 , A61K31/403 , A61K31/496 , A61P1/00 , A61P1/04 , A61P1/12 , A61P3/10 , A61P5/48 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/00 , A61P13/10 , A61P13/12 , A61P15/00 , A61P15/12 , A61P17/14 , A61P21/00 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/28 , A61P27/16 , A61P35/00 , A61P37/06 , A61P43/00 , C07D209/60 , C07D209/40 , A61P11/08
摘要： The present invention relates to ion channel activating agents. More particularly, the present invention relates to a particular class of chemical compounds that has proven useful as openers of SKCa and IKCa channels. In further aspects, the present invention relates to the use of these SK/IK channel activating agents for the manufacture of medicaments and pharmaceutical compositions comprising the SK/IK channel activating agents. The SK/IK channel activating agents of the invention are useful for the treatment or alleviation of diseases and conditions associated with the SK/IK channels, in particular respiratory diseases such as asthma, cystic fibrosis, chronic obstructive pulmonary disease and rhinorrhea, convulsions, vascular spasms, coronary artery spasms, renal disorders, polycystic kidney disease, bladder spasms, urinary incontinence, bladder outflow obstruction, irritable bowel syndrome, gastrointestinal dysfunction, secretory diarrhea, ischaemia, cerebral ischaemia, ischaemic heart disease, angina pectoris, coronary heart disease, traumatic brain injury, psychosis, anxiety, depression, dementia, memory and attention deficits, Alzheimer's disease, dysmenorrhea, narcolepsy, Reynaud's disease, intermittent claudication, Sjorgren's syndrome, migraine, arrhythmia, hypertension, absence seizures, myotonic muscle dystrophia, xerostomi, diabetes type II, hyperinsulinemia, premature labor, baldness, cancer, and immune suppression.

2. 发明专利

DE60020556T2 未知
公开(公告)号：DE60020556T2
公开(公告)日：2005-10-27
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.

3. 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.

4. 发明专利

DE69922997D1 未知
公开(公告)号：DE69922997D1
公开(公告)日：2005-02-03
申请号：DE69922997
申请日：1999-12-03
申请人： NEUROSEARCH AS BALLERUP
发明人： JENSEN BO SKAANING , JOERGENSEN TINO DYHRING , AHRING PHILIP K , CHRISTOPHERSEN PALLE , STROEBAEK DORTE , TEUBER LENE , OLESEN SOEREN PETER
IPC分类号： A61K31/404 , A61K31/403 , A61K31/496 , A61P1/00 , A61P1/04 , A61P1/12 , A61P3/10 , A61P5/48 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/00 , A61P13/10 , A61P13/12 , A61P15/00 , A61P15/12 , A61P17/14 , A61P21/00 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/28 , A61P27/16 , A61P35/00 , A61P37/06 , A61P43/00 , C07D209/60 , C07D209/40 , A61P11/08
摘要： The present invention relates to ion channel activating agents. More particularly, the present invention relates to a particular class of chemical compounds that has proven useful as openers of SKCa and IKCa channels. In further aspects, the present invention relates to the use of these SK/IK channel activating agents for the manufacture of medicaments and pharmaceutical compositions comprising the SK/IK channel activating agents. The SK/IK channel activating agents of the invention are useful for the treatment or alleviation of diseases and conditions associated with the SK/IK channels, in particular respiratory diseases such as asthma, cystic fibrosis, chronic obstructive pulmonary disease and rhinorrhea, convulsions, vascular spasms, coronary artery spasms, renal disorders, polycystic kidney disease, bladder spasms, urinary incontinence, bladder outflow obstruction, irritable bowel syndrome, gastrointestinal dysfunction, secretory diarrhea, ischaemia, cerebral ischaemia, ischaemic heart disease, angina pectoris, coronary heart disease, traumatic brain injury, psychosis, anxiety, depression, dementia, memory and attention deficits, Alzheimer's disease, dysmenorrhea, narcolepsy, Reynaud's disease, intermittent claudication, Sjorgren's syndrome, migraine, arrhythmia, hypertension, absence seizures, myotonic muscle dystrophia, xerostomi, diabetes type II, hyperinsulinemia, premature labor, baldness, cancer, and immune suppression.

5. 发明专利

DE69922986D1 未知
公开(公告)号：DE69922986D1
公开(公告)日：2005-02-03
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.

6. 发明专利

DE69817802T2 未知
公开(公告)号：DE69817802T2
公开(公告)日：2004-04-08
申请号：DE69817802
申请日：1998-04-21
申请人： NEUROSEARCH AS BALLERUP
发明人： CHRISTOPHERSEN PALLE , PEDERSEN OVE
IPC分类号： C07D249/12 , A61K31/41 , A61K31/4196 , A61K31/4245 , A61K31/4427 , A61P1/04 , A61P1/12 , A61P3/00 , A61P7/06 , A61P9/00 , A61P9/12 , A61P19/10 , A61P27/06 , A61P29/00 , A61P37/08 , C07C233/55 , C07C271/58 , C07C275/40 , C07C275/42 , C07C309/51 , C07C311/08 , C07C311/21 , C07C311/47 , C07C311/60 , C07C335/22 , C07D249/10 , C07D257/04 , C07D271/10 , C07D401/10 , C07D405/10 , C07D409/10
摘要： A compound having the formula (I) or a pharmaceutically acceptable salt thereof where the variables are defined in the specification are useful in the treatment of sickle-cell anemia.

7. 发明专利

DE69903053T2 未知
公开(公告)号：DE69903053T2
公开(公告)日：2003-05-22
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.

8. 发明专利

DE69716424D1 未知
公开(公告)号：DE69716424D1
公开(公告)日：2002-11-21
申请号：DE69716424
申请日：1997-05-26
申请人： NEUROSEARCH AS BALLERUP
发明人： CHRISTOPHERSEN PALLE , PEDERSEN OVE
IPC分类号： A61K31/245 , A61K31/00 , A61K31/155 , A61K31/17 , A61P1/00 , A61P1/12 , A61P7/00 , A61P7/06 , A61P27/00 , A61P27/06 , A61P29/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07C229/56 , C07C233/55 , C07C271/58 , C07C273/18 , C07C275/40 , C07C275/42 , C07C309/51 , C07C311/08 , C07C311/21 , C07C311/47 , C07C311/51 , C07C311/60 , C07C335/16 , C07C335/22 , C07C311/39 , A61K31/19 , A61K31/18
摘要： The present patent application relates to compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein one of R1, R2 and R3 is a non-cyclic acidic group having a pKa value below 8 or a group which is in vivo convertible to such a group; R4, R5 and the other two of the substituents R1, R2 and R3 are each independently selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro, amnino, and aryl, aralkyl, arylamino, aryloxy, aryl-CO-, or heteroaryl, wherein the aryl and heteroaryl groups may be substituted one or more times with substituents selected from alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, hydroxy, alkoxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro and amino; or R3 and R4 or R4 and R5 together form a fused 4- to 7-membered carbocyclic ring which may be unsaturated, or partially or fully saturated, while the other substituents R1, R2, R3, R4 and R5 are as defined above; Y is -CO-, -CS-, -SO2-, or -C(=N-R8)-, wherein R8 is hydrogen, alkyl, or cyano; X is -NH-, -CH2-NH-, or -SO2-NH-; Z is NR6, O, -CH=CH-, -C=C-, -N=CH-, or -CH=N-; wherein R6 is hydrogen, or alkyl; R11, R12, R13, R14 and R15 are each independently selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro, amino, -NHSO2-R7, -COOR7, -SO2N(R7)2, -SO2OR7 and -CO-R7, wherein R7 is hydrogen alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl or aralkyl; and aryl, aralkyl, arylamino, aryloxy, aryl-CO-, or heteroaryl, wherein the aryl and heteroaryl groups may be substituted one or more times with substituents selected from alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, hydroxy, alkoxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro and amino; or one of R11 and R12, R12 a

9. 发明专利

DE69920259T2 未知
公开(公告)号：DE69920259T2
公开(公告)日：2005-01-20
申请号：DE69920259
申请日：1999-12-03
申请人： NEUROSEARCH AS BALLERUP
发明人： JENSEN SKAANING , CHRISTOPHERSEN PALLE , STROBAEK DORTE , TEUBER LENE
IPC分类号： A61P1/00 , A61K31/15 , A61P3/10 , A61P9/00 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/02 , A61P13/10 , A61P13/12 , A61P15/00 , A61P17/02 , A61P17/14 , A61P21/00 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07C251/48 , C07C251/50
摘要： The present invention relates to ion channel modulating agents. More particularly, the present invention relates to a particular class of oxime derivatives 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.

10. 发明专利

DE69817802D1 未知
公开(公告)号：DE69817802D1
公开(公告)日：2003-10-09
申请号：DE69817802
申请日：1998-04-21
申请人： NEUROSEARCH AS BALLERUP
发明人： CHRISTOPHERSEN PALLE , PEDERSEN OVE
IPC分类号： C07D249/12 , A61K31/41 , A61K31/4196 , A61K31/4245 , A61K31/4427 , A61P1/04 , A61P1/12 , A61P3/00 , A61P7/06 , A61P9/00 , A61P9/12 , A61P19/10 , A61P27/06 , A61P29/00 , A61P37/08 , C07C233/55 , C07C271/58 , C07C275/40 , C07C275/42 , C07C309/51 , C07C311/08 , C07C311/21 , C07C311/47 , C07C311/60 , C07C335/22 , C07D249/10 , C07D257/04 , C07D271/10 , C07D401/10 , C07D405/10 , C07D409/10
摘要： A compound having the formula (I) or a pharmaceutically acceptable salt thereof where the variables are defined in the specification are useful in the treatment of sickle-cell anemia.

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