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1. 发明申请

WO1997030997A1 TROPANE-DERIVATIVES, THEIR PREPARATION AND USE 审中-公开
标题翻译： TROPANE-DERIVATIVES，他们的准备和使用
公开(公告)号：WO1997030997A1
公开(公告)日：1997-08-28
申请号：PCT/EP1997000850
申请日：1997-02-21
申请人： NEUROSEARCH A/S , SCHEEL-KRÜGER, Jorgen , MOLDT, Peter , WÄTJEN, Frank
发明人： NEUROSEARCH A/S
IPC分类号： C07D451/02
CPC分类号： C07D451/02 , C07D451/00
摘要： The present invention discloses compounds of formula (a), (b), (c) or (d), or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or 2-hydroxyethyl; R is -CH2-X-R', wherein X is O, S or NR", wherein R" is hydrogen, or alkyl and R' is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, or -CO-alkyl; R is phenyl which may be substitued one or more times with substituents selected from the group consisting of halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl; 3,4-methylenedioxyphenyl; benzyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl; heteroaryl which may be substitued one or more times with substituents selected from the group consisting of halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl; or naphthyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl. The compounds possess valuable pharmaceutical properties as monoamine neurotransmitter, i.e. dopamine, serotonin, noradrenaline, reuptake inhibitors.
摘要翻译：本发明公开了式（a），（b），（c）或（d）的化合物或其任何混合物或其药学上可接受的盐; 其中R是氢，烷基，烯基，炔基，环烷基，环烷基烷基或2-羟乙基; R 3是-CH 2 -X-R'，其中X是O，S或NR“，其中R”是氢或烷基，R'是烷基，烯基，炔基，环烷基，环烷基烷基或-CO-烷基 ; R 4是可以被选自卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基和芳基的取代基取代一次或多次的苯基; 3,4-亚甲二氧苯基; 可以被选自卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基和芳基的取代基取代一次或多次的苄基。可以用选自卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基和芳基的取代基取代一次或多次的杂芳基; 或萘基，其可以被选自卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基和芳基的取代基取代一次或多次。该化合物具有作为单胺神经递质（即多巴胺，5-羟色胺，去甲肾上腺素，再摄取抑制剂）的有价值的药物性质。

2. 发明申请

WO2005011694A1 2-METHOXYMETHYL-3-(3,4-DICHLOROPHENYL)-8-AZABICYCLO[3.2.1]OCTANE TARTRATE SALTS 审中-公开
标题翻译： 2-甲氧基甲基-3-（3,4-二氯苯基）-8-氮杂双环[3.2.1]十八烷酸钠盐
公开(公告)号：WO2005011694A1
公开(公告)日：2005-02-10
申请号：PCT/EP2004/051651
申请日：2004-07-29
申请人： NEUROSEARCH A/S , FRØSTRUP, Brian , WÄTJEN, Frank , JENSEN, Klaus, Snej
发明人： FRØSTRUP, Brian , WÄTJEN, Frank , JENSEN, Klaus, Snej
IPC分类号： A61K31/46
CPC分类号： C07D451/02
摘要： This invention relates to novel (1R,2R,3S,5S)-2-methoxymethyl-3-(3,4dichlorophenyl)-8-azabicyclo[3.2. 1 ]octane tartrate salts, such as L-tartrate monohydrates and anhydrates. The salts are useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these salts in a method for therapy and to pharmaceutical compositions comprising the salts of the invention.
摘要翻译：本发明涉及新的（1R，2R，3S，5S）-2-甲氧基甲基-3-（3,4-二氯苯基）-8-氮杂双环[3.2。 1]辛烷酒石酸盐，如L-酒石酸盐一水合物和水合物。这些盐可用作单胺神经递质再摄取抑制剂。在其它方面，本发明涉及这些盐在治疗方法中的用途以及包含本发明的盐的药物组合物。

3. 发明申请

WO1996008494A1 INDOLE-2,3-DIONE-3-OXIME DERIVATIVES, THEIR PREPARATION AND USE 审中-公开
标题翻译：吲哚-2,3-二酮-3-氧化物衍生物，其制备和使用
公开(公告)号：WO1996008494A1
公开(公告)日：1996-03-21
申请号：PCT/EP1995003593
申请日：1995-09-12
申请人： NEUROSEARCH A/S , MOLDT, Peter , WÄTJEN, Frank
发明人： NEUROSEARCH A/S
IPC分类号： C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The present patent application discloses compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R , X and R have the meanings set further in the specification. A is a ring of five to seven atoms fused with the benzo ring at the positions marked a and b. The compounds are useful in the treatment of cerebrovascular disorders for example.
摘要翻译：本专利申请公开了具有式（I）的化合物或其药学上可接受的盐，其中R 1，X和R 5具有在说明书中进一步设定的含义。 A是在标记a和b的位置与苯环稠合的5至7个原子的环。该化合物可用于治疗例如脑血管障碍。

4. 发明申请

WO2005040131A1 1,5,7-TRISUBSTITUTED BENZIMIDAZOLE DERIVATIVES AND THEIR USE FOR MODULATING THE GABAA RECEPTOR COMPLEX 审中-公开
标题翻译： 1,5,7-三唑并咪唑衍生物及其用于调节GABA A受体复合物的用途
公开(公告)号：WO2005040131A1
公开(公告)日：2005-05-06
申请号：PCT/EP2004/052582
申请日：2004-10-20
申请人： AKZO NOBEL N.V. , NEUROSEARCH A/S , HAMILTON, Niall, Morton , NAPIER, Susan, Elizabeth , EASSON, Morag, Ann, MacCall , COOKE, Andrew, John , TEUBER, Lene , MIRZA, Naheed , WÄTJEN, Frank
发明人： HAMILTON, Niall, Morton , NAPIER, Susan, Elizabeth , EASSON, Morag, Ann, MacCall , COOKE, Andrew, John , TEUBER, Lene , MIRZA, Naheed , WÄTJEN, Frank
IPC分类号： C07D235/06
CPC分类号： A61K31/4184 , C07D235/06 , C07D401/04 , C07D401/06 , C07D401/10 , C07D403/06 , C07D403/12 , C07D405/04
摘要： This invention relates to novel 1, 5, 7-trisubstituted benzimidazole derivatives of formula (I), pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABA A receptor complex.
摘要翻译：本发明涉及式（I）的新的1,5,7-三取代苯并咪唑衍生物，含有这些化合物的药物组合物及其处理方法。本发明的化合物可用于治疗对调节GABA A受体复合物有反应的中枢神经系统疾病和病症。

5. 发明申请

WO2004039778A1 NOVEL PIPERIDINE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS 审中-公开
标题翻译：新型哌啶衍生物及其作为单胺神经递质抑制剂的用途
公开(公告)号：WO2004039778A1
公开(公告)日：2004-05-13
申请号：PCT/DK2003/000734
申请日：2003-10-30
申请人： NEUROSEARCH A/S , WÄTJEN, Frank
发明人： WÄTJEN, Frank
IPC分类号： C07D211/22
CPC分类号： C07D211/22 , C07D211/60
摘要： This invention relates to novel piperidine derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
摘要翻译：本发明涉及用作单胺神经递质再摄取抑制剂的新型哌啶衍生物。在其它方面，本发明涉及这些化合物在治疗方法中的用途以及包含本发明化合物的药物组合物。

6. 发明申请

WO2004018466A2 A METHOD OF PREPARING ENANTIOMERS OF INDOLE-2,3-DIONE-3-OXIME DERIVATIVES 审中-公开
标题翻译：制备吲哚-2,3-二酮-3-氧肟衍生物对映体的方法
公开(公告)号：WO2004018466A2
公开(公告)日：2004-03-04
申请号：PCT/DK2003/000539
申请日：2003-08-13
申请人： NEUROSEARCH A/S , GOULIAEV, Alex, Haahr , BROWN, William, Dalby , WÄTJEN, Frank
发明人： GOULIAEV, Alex, Haahr , BROWN, William, Dalby , WÄTJEN, Frank
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C12P17/04 , C12P41/004
摘要： The present invention is directed to a method of preparing enantiomers of indole-2,3-dione-3-oxime derivatives.
摘要翻译：本发明涉及制备吲哚-2,3-二酮-3-肟衍生物的对映体的方法。

7. 发明申请

WO1996033192A1 BENZIMIDAZOLE COMPOUNDS AND THEIR USE AS MODULATORS OF THE GABAA RECEPTOR COMPLEX 审中-公开
标题翻译：苯并咪唑化合物及其作为GABAA受体复合物的调节剂
公开(公告)号：WO1996033192A1
公开(公告)日：1996-10-24
申请号：PCT/EP1996001654
申请日：1996-04-19
申请人： NEUROSEARCH A/S , MEIJI SEIKA KAISHA, Ltd. , TEUBER, Lene , WÄTJEN, Frank
发明人： NEUROSEARCH A/S , MEIJI SEIKA KAISHA, Ltd.
IPC分类号： C07D401/14
CPC分类号： C07D235/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/10 , C07D403/10 , C07D405/10 , C07D405/14 , C07D409/10 , C07D413/14 , C07D417/10 , C07D417/14
摘要： The present patent application discloses compounds having formula (I) or a pharmaceutically acceptable salt thereof or an oxide thereof wherein R is formula (II), wherein A, B and D each is CH, or one or two of A, B and D is N and the others are CH; R is phenyl, benzimidazolyl, or monocyclic heteroaryl all of which may be substituted one or more times with substituents selected from alkyl, halogen, CF3, amino, nitro, cyano, acylamino, alkoxy, acyl, phenyl, and monocyclic heteroaryl, and one of R and R is hydrogen and the other is pyrrolyl which may be substituted one or more times with substituents selected from halogen, alkyl, phenyl, and alkoxy. The compounds are useful for the treatment of various central nervous system disorders such as epilepsy and other convulsive disorders, anxiety, sleep disorders and memory disorders.
摘要翻译：本专利申请公开了具有式（I）化合物或其药学上可接受的盐或其氧化物，其中R 3为式（II），其中A，B和D各自为CH，或A，B中的一种或两种 D为N，其余为CH; R 11是苯基，苯并咪唑基或单环杂芳基，其全部可以被选自烷基，卤素，CF 3，氨基，硝基，氰基，酰氨基，烷氧基，酰基，苯基和单环杂芳基的取代基取代一次或多次。 R 6和R 7中的一个是氢，另一个是可以被选自卤素，烷基，苯基和烷氧基的取代基取代一次或多次的吡咯基。该化合物可用于治疗各种中枢神经系统疾病如癫痫和其他惊厥性疾病，焦虑症，睡眠障碍和记忆障碍。

8. 发明申请

WO1994026747A1 AMPA ANTAGONISTS AND A METHOD OF TREATMENT THEREWITH 审中-公开
标题翻译： AMPA拮抗剂及其治疗方法
公开(公告)号：WO1994026747A1
公开(公告)日：1994-11-24
申请号：PCT/EP1994001492
申请日：1994-05-09
申请人： NEUROSEARCH A/S , WÄTJEN, Frank , DREJER, Jorgen
发明人： NEUROSEARCH A/S
IPC分类号： C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The present patent application discloses compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R is hydrogen, alkyl or benzyl; X is O or NOR , wherein R is hydrogen, alkyl or benzyl; Y is N-R wherein R is hydrogen, OH or alkyl; n is 0 or 1; R is phenyl, naphthyl, thienyl, pyridyl, all of which may be substituted one or more times with substituents selected from the group consisting of halogen; CF3, NO2, amino, alkyl, alkoxy and phenyl; A is a ring of five to seven atoms fused with the benzo ring at the positions marked a and b. The compounds are useful in the treatment of cerebrovascular disorders for example.
摘要翻译：本专利申请公开了具有式（I）的化合物或其药学上可接受的盐，其中R 1是氢，烷基或苄基; X是O或NOR 2，其中R 2是氢，烷基或苄基; Y是N-R 4，其中R 4是氢，OH或烷基; n为0或1; R 6是苯基，萘基，噻吩基，吡啶基，它们都可以被选自卤素的取代基取代一次或多次; CF 3，NO 2，氨基，烷基，烷氧基和苯基; A是在标记a和b的位置与苯环稠合的5至7个原子的环。该化合物可用于治疗例如脑血管障碍。

9. 发明申请

WO1998017651A1 1-PHENYL-BENZIMIDAZOLE COMPOUNDS AND THEIR USE AS BAGA-A RECEPTOR MODULATORS 审中-公开
标题翻译： 1-苯基 - 苯并咪唑化合物及其作为BAGA-A受体调节剂的用途
公开(公告)号：WO1998017651A1
公开(公告)日：1998-04-30
申请号：PCT/DK1997000462
申请日：1997-10-21
申请人： NEUROSEARCH A/S , TEUBER, Lene , WÄTJEN, Frank
发明人： NEUROSEARCH A/S
IPC分类号： C07D235/06
CPC分类号： C07D235/06 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D413/04
摘要： The present invention relates to novel benzimidazole compounds, represented by general formula (I) in which o is 0, 1, 2, or 3; R represents an alkyl group, a phenyl group, or a monocyclic heterocyclic group, which groups may be substituted one or more times with substituents selected from alkyl, cycloalkyl, cycloalkyl-alkyl, alkoxy, halogen, trifluoromethyl, cyano, amino, and nitro; or R represents a cyano group or a group of the formula -alkyl-CO2R , alkenyl-CO2R , -CO-R , -CO2(CH2)mR , or -C(R )=N-OR , R represents a group of formula -CO2-R , or R represents a group of general formula (II) in which n is 0, 1, 2 or 3; or R may represent a group of general formula (III), in which n is 0, 1, 2, or 3; the novel compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, such as for example anxiety, sleep disorders, anaestesia, memory disorders, and epilepsia or other convulsive disorders.
摘要翻译：本发明涉及由通式（I）表示的新的苯并咪唑化合物，其中o为0,1,2或3; R 1表示烷基，苯基或单环杂环基，该基团可以被选自烷基，环烷基，环烷基 - 烷基，烷氧基，卤素，三氟甲基，氰基，氨基，和硝基; 或R 1表示氰基或式 - 烷基-CO 2 R 2，烯基-CO 2 R 2，-CO-R 2，-CO 2（CH 2）m R 2或 - C（R 3）= N-OR 2，R 11表示式-CO 2 -R 9的基团，或R 11表示通式（II）的基团，其中n为 0,1,2或3; 或R 11可以表示通式（III）的基团，其中n为0,1,2或3; 本发明的新化合物可用于治疗对GABA A受体复合物的调节有反应的中枢神经系统疾病和病症，例如焦虑症，睡眠障碍，麻醉，记忆障碍和癫痫或其它惊厥性疾病。

10. 发明申请

WO1998014447A1 NOVEL INDOLE-2,3-DIONE-3-OXIME DERIVATIVES 审中-公开
标题翻译：新型吲哚-3,3-二酮-3-氧化物衍生物
公开(公告)号：WO1998014447A1
公开(公告)日：1998-04-09
申请号：PCT/DK1997000418
申请日：1997-10-01
申请人： NEUROSEARCH A/S , WÄTJEN, Frank , DREJER, Jorgen
发明人： NEUROSEARCH A/S
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention relates to novel indole-2,3-dione-3-oxime derivatives capable of antagonising the effect of excitatory amino acids, such as glutamate. More specifically the novel indole-2,3-dione-3-oxime derivatives of the invention may be described by general formula (I), wherein R represents "Het", or a group of formula (II), wherein "Het" represents a saturated or unsaturated, 4 to 7 membered, monocyclic, heterocyclic ring, at least one of R , R , and R independently represents hydrogen, alkyl, or hydroxyalkyl, and at least one of R , R , and R independently represents (CH2)nR ; wherein R represents hydroxy, carboxy, alkoxycarbonyl, alkenyloxycarbonyl, alkynyloxycarbonyl, cycloalkoxycarbonyl, cycloalkyl-alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, CONR R , or "Het"; wherein n is 0, 1, 2, or 3; and R represents phenyl, naphthyl, thienyl, or pyridyl, all of which may be substituted. "A" represents a ring of five to seven atoms fused with the benzo ring at the positions marked "a" and "b", and formed by the following bivalent radicals: a-NR -CH2-CH2-b; a-CH2-NR -CH2-b; a-CH2-CH2-NR -b; a-NR -CH2-CH2-CH2-b; a-CH2-NR -CH2-CH2-b; a-CH2-CH2-NR -CH2-b; a-CH2-CH2-CH2-NR -b; a-NR -CH2-CH2-CH2-CH2-b; a-CH2-NR -CH2-CH2-CH2-b; a-CH2-CH2-NR -CH2-CH2-b; a-CH2-CH2-CH2-NR -CH2-b; or a-CH2-CH2-CH2-CH2-NR -b; wherein R represents hydrogen, alkyl or CH2CH2OH; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及能够拮抗兴奋性氨基酸如谷氨酸的作用的新的吲哚-2,3-二酮-3-肟衍生物。更具体地，本发明的新的吲哚-2,3-二酮-3-肟衍生物可以由通式（I）描述，其中R 3表示“Het”，或式（II）的基团，其中“ Het“表示饱和或不饱和的4至7元单环杂环，R 31，R 32和R 33中的至少一个独立地表示氢，烷基或羟烷基，并且至少一个 R 31，R 32和R 33独立地表示（CH 2）n R 34; 其中R 34表示羟基，羧基，烷氧基羰基，烯氧基羰基，炔氧基羰基，环烷氧基羰基，环烷基 - 烷氧基羰基，芳氧基羰基，芳烷氧羰基，CONR 35 R 36或“Het”。其中n为0,1,2或3; 并且R 5代表苯基，萘基，噻吩基或吡啶基，它们都可被取代。 “A”表示在标记为“a”和“b”的位置与苯并环稠合的5至7个原子的环，由以下二价基团形成：a-NR 6 -CH 2 -CH 2 -B; 一个-CH2-NR <6> -CH2-B; 一个-CH2-CH2-NR <6> -b; 一个-NR <6> -CH2-CH2-CH2-B; 一个-CH2-NR <6> -CH2-CH2-B; 一个-CH2-CH2-NR <6> -CH2-B; 一个-CH2-CH2-CH2-NR <6> -b; 一个-NR <6> -CH2-CH2-CH2-CH2-B; 一个-CH2-NR <6> -CH2-CH2-CH2-B; 一个-CH2-CH2-NR <6> -CH2-CH2-B; 一个-CH2-CH2-CH2-NR <6> -CH2-B; 或a-CH2-CH2-CH2-CH2-NR6-b; 其中R 6表示氢，烷基或CH 2 CH 2 OH; 或其药学上可接受的盐。

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