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11. 发明公开

EP1121119A1 A NEW COMPOSITION 审中-公开
标题翻译：一种新的组合物
公开(公告)号：EP1121119A1
公开(公告)日：2001-08-08
申请号：EP99951320.3
申请日：1999-09-13
申请人： AstraZeneca AB
发明人： EVENDEN, John,AstraZeneca R&D Boston , THORBERG, Seth-Olov
IPC分类号： A61K31/35
CPC分类号： A61K31/35 , A61K31/44 , A61K2300/00
摘要： The invention relates to a composition comprising a first component (a) which is (R)-3-N,N-dicyclobutylamino-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide hydrogen (2R,3R)-tartrate monohydrate and a second component (b) which is 1-[3-(dimethylamino)propyl]-1-(p-fluorophenyl)-5-phthalancarbonitrile, as the racemate or an enantiomer thereof, in the form of the free base, or a pharmaceutically acceptable salt and/or solvate thereof, the preparation thereof, pharmaceutical formulations containing said composition, use of and a method of treatment of affective disorders such as mood disorders and anxiety disorders with said composition as well as a kit containing said composition.
摘要翻译：（R）-3-N，N-二环丁基氨基-8-氟-3,4-二氢-2H-1-苯并吡喃-5-甲酰胺氢的第一组分（a）（2R， 3R）酒石酸盐一水合物和作为外消旋体或其对映体的第二组分（b），其为1- [3-（二甲基氨基）丙基] -1-（对氟苯基）-5-邻苯二甲腈游离碱或其药学上可接受的盐和/或溶剂合物，其制备方法，含有所述组合物的药物制剂，用所述组合物治疗情感障碍如心境障碍和焦虑症的用途和方法，以及含有所述组合物。

12. 发明公开

EP1025095A1 SUBSTITUTED CHROMAN DERIVATIVES 有权
标题翻译：取代色
公开(公告)号：EP1025095A1
公开(公告)日：2000-08-09
申请号：EP98944377.5
申请日：1998-09-09
申请人： AstraZeneca AB
发明人： BERG, Stefan , NYLÖF, Martin , ROSS, Svante , THORBERG, Seth-Olov
IPC分类号： C07D311/58 , A61K31/495 , A61K31/535
CPC分类号： C07D405/12 , C07D311/58 , C07D407/12
摘要： The present invention relates to new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives compounds having formula (I) wherein X is N or CH; Y is NR2CH2, CH2NR2, NR2CO, CONR2, NR2SO2 or NR2CONR2 wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted with R4 and/or R5; and n is 0-4; as (R)-enantiomers, (S)-enantiomers or a racemate in the form of a free base or a pharmaceutically acceptable salt or solvate thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds.

13. 发明授权

EP1025096B1 SUBSTITUTED CHROMAN DERIVATIVES 有权
标题翻译：取代色
公开(公告)号：EP1025096B1
公开(公告)日：2003-11-26
申请号：EP98944378.3
申请日：1998-09-09
申请人： AstraZeneca AB
发明人： BERG, Stefan , LINDERBERG, Mats , ROSS, Svante , THORBERG, Seth-Olov , ULFF, Bengt
IPC分类号： C07D311/58 , A61K31/495 , A61K31/535
CPC分类号： C07D311/58
摘要： The present invention relates to new piperidinyl- or piperazinyl-substituted-3,4-dihydro-2H-1-benzopyran derivatives having formula (I) wherein X is N or CH; Y is NR2CH2, CH2NR2, NR2CO, CONR2 or NR2SO2 wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted; n is 0-4; R9 is C1-C6 alkyl, C3-C6 cycloalkyl, OCF3, OCHF2, OCH2F, halogen, CONR6R7, CN, CF3, OH, C1-C6 alkoxy, NR6R7, SO3CH3, SO3CF3, SO2NR6R7, an unsubstituted or substituted heterocyclic or heteroaromatic ring containing one or two heteroatoms selected from N and O, wherein the substituent(s) is(are) C1-C6 alkyl; or COR8; wherein R6, R7 and R8 are as defined above, as (R)-enantiomers, (S)-enantiomers or racemates in the form of a free base or pharmaceutically acceptable salts or solvates thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds in therapy.

14. 发明授权

EP1025095B1 SUBSTITUTED CHROMAN DERIVATIVES 有权
标题翻译：取代的色素衍生物
公开(公告)号：EP1025095B1
公开(公告)日：2003-11-26
申请号：EP98944377.5
申请日：1998-09-09
申请人： AstraZeneca AB
发明人： BERG, Stefan , NYLÖF, Martin , ROSS, Svante , THORBERG, Seth-Olov
IPC分类号： C07D311/58 , A61K31/495 , A61K31/535
CPC分类号： C07D405/12 , C07D311/58 , C07D407/12
摘要： The present invention relates to new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives compounds having formula (I) wherein X is N or CH; Y is NR2CH2, CH2NR2, NR2CO, CONR2, NR2SO2 or NR2CONR2 wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted with R4 and/or R5; and n is 0-4; as (R)-enantiomers, (S)-enantiomers or a racemate in the form of a free base or a pharmaceutically acceptable salt or solvate thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds.
摘要翻译：本发明涉及具有式（I）的新的哌啶基或哌嗪基取代的二氢-2H-1-苯并吡喃衍生物化合物，其中X是N或CH; Y是NR 2 CH 2，CH 2 NR 2，NR 2 CO，CONR 2，NR 2 SO 2或NR 2 CONR 2，其中R 2是H或C 1 -C 6烷基; R1是H，C1-C6烷基或C3-C6环烷基; R 3是C 1 -C 6烷基，C 3 -C 6环烷基或（CH 2）n - 芳基，其中芳基是苯基或含有一个或两个选自N，O和S的杂原子的杂芳族环，并且其可以单 - 或二 - 取代 R4和/或R5; 并且n是0-4; 作为（R） - 对映异构体，（S） - 对映异构体或游离碱形式的外消旋体或其药学上可接受的盐或溶剂合物，其制备方法，含有所述治疗活性化合物的药物组合物以及所述活性化合物。

15. 发明公开

EP1113792A1 A NEW COMPOSITION 审中-公开
标题翻译：一种新的组合物
公开(公告)号：EP1113792A1
公开(公告)日：2001-07-11
申请号：EP99951318.7
申请日：1999-09-13
申请人： AstraZeneca AB
发明人： EVENDEN, John , THORBERG, Seth-Olov
IPC分类号： A61K31/35
CPC分类号： A61K31/00 , A61K31/35 , A61K45/06 , A61K31/135 , A61K31/15 , A61K2300/00
摘要： The invention relates to a composition comprising a first component (a) which is (R)-3-N,N-dicyclobutylamino-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide hydrogen (2R,3R)-tartrate monohydrate and a second component (b) which is a 5-HT reuptake inhibitor excluding citalopram and paroxetine, the preparation thereof, pharmaceutical formulations containing said composition, use of and a method of treatment of affective disorders such as mood disorders and anxiety disorders with said composition as well as a kit containing said composition.
摘要翻译：（R）-3-N，N-二环丁基氨基-8-氟-3,4-二氢-2H-1-苯并吡喃-5-甲酰胺氢的第一组分（a）（2R， 3R） - 酒石酸盐一水合物和第二组分（b），其是不包括西酞普兰和帕罗西汀的5-HT重摄取抑制剂，其制备，含有所述组合物的药物制剂，治疗情感障碍例如情绪障碍和所述组合物的焦虑症以及含有所述组合物的药盒。

16. 发明公开

EP1021183A1 A COMBINATION OF A SELECTIVE 5-HT 1A? ANTAGONIST AND A SELECTIVE h5-HT 1B? ANTAGONIST OR PARTIAL AGONIST 有权
标题翻译：选择性5-HT1A拮抗剂结合和选择性H5-HT1B拮抗剂或部分激动剂
公开(公告)号：EP1021183A1
公开(公告)日：2000-07-26
申请号：EP98944374.2
申请日：1998-09-09
申请人： AstraZeneca AB
发明人： BERG, Stefan , ROSS, Svante , THORBERG, Seth-Olov
IPC分类号： A61K31/495 , A61K31/535 , A61K31/35
CPC分类号： A61K31/495 , A61K31/535 , A61K31/35 , A61K2300/00
摘要： The invention relates to a combination of a first component (a) which is a selective 5-HT1A receptor antagonist having formula (I), wherein R1 is n-propyl or cyclobutyl, R2 is isopropyl, tertiary butyl, cyclobutyl, cyclopentyl or cyclohexyl, R3 is hydrogen and R4 is hydrogen or methyl and being in the (R)-enantiomer form, with a second component (b) which is a selective h5-HT1B antagonist or partial agonist having formula (II), wherein X is CH2, O, Y is CONH, NHCO, R1 is H, C1-C6 alkyl, C3-C6 cycloalkyl, R2 is H, C1-C6 alkyl, C1-C6 alkoxy, halogen, R3 is (1), (2), (3), (4), (5); R4 and R5 independently are H or C1-C4 alkyl as racemate R-enantiomer or S-enantiomer, and said components (a) and (b) being in the form of free bases, solvates or pharmaceutically acceptable salts thereof, the preparation thereof, pharmaceutical formulations containing said combination, use of and method of treatment of affective disorders such as depression, anxiety and OCD with said combination as well as a kit containing said combination.

17. 发明公开

EP1014985A1 A COMBINATION OF A 5-HT REUPTAKE INHIBITOR AND A h5-HT 1B ANTAGONIST OR PARTIAL AGONIST 有权
标题翻译：组合VAN 5-HT血清素再摄取抑制剂和H5-HT IB拮抗剂或部分激动剂
公开(公告)号：EP1014985A1
公开(公告)日：2000-07-05
申请号：EP98944375.9
申请日：1998-09-09
申请人： AstraZeneca AB
发明人： BERG, Stefan , ROSS, Svante , THORBERG, Seth-Olov
IPC分类号： A61K31/495 , A61K31/535
CPC分类号： A61K31/495 , A61K31/535 , A61K31/55 , A61K31/445 , A61K31/34 , A61K31/135 , A61K2300/00
摘要： The invention relates to a combination of a first component (a) which is a 5-HT reuptake inhibitor and a second component (b) which is selective h5-HT1B antagonist or partial agonist having formula (I) wherein X is CH2, O; Y is CONH, NHCO; R1 is H, C1-C6 alkyl, C3-C6 cycloalkyl; R2 is H, C1-C6 alkyl, C1-C6 alkoxy, halogen; R3 is (1), (2), (3), CF3; R4 and R5 independently are H, or C1-C4 alkyl, as racemate, R-enantiomer or S-enantiomer, and said components (a) and (b) being in the form of free bases, solvents or pharmaceutically acceptable salts thereof, the preparation thereof, pharmaceutical formulations containing said combinations, use of and method of treatment of affective disorders such as depression, anxiety and OCD with said combination as well as kit containing said combination.

18. 发明授权

EP1025094B1 SUBSTITUTED INDAN DERIVATIVES 有权
标题翻译：取代茚衍生物
公开(公告)号：EP1025094B1
公开(公告)日：2004-08-25
申请号：EP98944379.1
申请日：1998-09-09
申请人： AstraZeneca AB
发明人： BERG, Stefan , FLORVALL, Lennart , ROSS, Svante , THORBERG, Seth-Olov
IPC分类号： C07D295/135 , C07D295/155 , C07D211/26 , C07D211/34 , A61K31/495 , A61K31/445
CPC分类号： C07D295/135 , C07D295/155
摘要： The present invention relates to new piperidyl- or piperazinyl-substituted indan derivatives having formula (I) wherein X is N or CH; Y is NR2HC2, CH2NR2, NR2CO, CONR2 or NR2SO2, wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S which may be mono- or di-substituted; n is 0-4; R9 is H, C1-C6 alkyl, C3-C6 cycloalkyl OCF3, OCHF2, OCH2F, halogen, CN, CF3, OH, C1-C6 alcoxy, C1-C6 alcoxy-C1-C6 alkyl, NR6R7, SO3CH3, SO3CF3, SO2NR6R7, an unsubstituted or substituted heterocyclic or heteroaromatic ring containing one or two heteroatoms selected from N and O, wherein the substituent(s) is(are) C1-C6 alkyl; or COR8, wherein R6, R7 and R8 are as defined above, as R-enantiomers, S-enantiomers or racemates in the form of a free base or pharmaceutically acceptable salts or solvates thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds in therapy.

19. 发明授权

EP1021183B1 A COMBINATION OF A SELECTIVE 5-HT1A ANTAGONIST AND A SELECTIVE h5-HT1B ANTAGONIST OR PARTIAL AGONIST 有权
标题翻译：选择性5-HT1A拮抗剂结合和选择性H5-HT1B拮抗剂或部分激动剂
公开(公告)号：EP1021183B1
公开(公告)日：2004-03-17
申请号：EP98944374.2
申请日：1998-09-09
申请人： AstraZeneca AB
发明人： BERG, Stefan , ROSS, Svante , THORBERG, Seth-Olov
IPC分类号： A61K31/495 , A61K31/535 , A61K31/35 , A61P25/24
CPC分类号： A61K31/495 , A61K31/535 , A61K31/35 , A61K2300/00
摘要： The invention relates to a combination of a first component (a) which is a selective 5-HT1A receptor antagonist having formula (I), wherein R1 is n-propyl or cyclobutyl, R2 is isopropyl, tertiary butyl, cyclobutyl, cyclopentyl or cyclohexyl, R3 is hydrogen and R4 is hydrogen or methyl and being in the (R)-enantiomer form, with a second component (b) which is a selective h5-HT1B antagonist or partial agonist having formula (II), wherein X is CH2, O, Y is CONH, NHCO, R1 is H, C1-C6 alkyl, C3-C6 cycloalkyl, R2 is H, C1-C6 alkyl, C1-C6 alkoxy, halogen, R3 is (1), (2), (3), (4), (5); R4 and R5 independently are H or C1-C4 alkyl as racemate R-enantiomer or S-enantiomer, and said components (a) and (b) being in the form of free bases, solvates or pharmaceutically acceptable salts thereof, the preparation thereof, pharmaceutical formulations containing said combination, use of and method of treatment of affective disorders such as depression, anxiety and OCD with said combination as well as a kit containing said combination.

20. 发明授权

EP1000048B1 SUBSTITUTED 1,2,3,4-TETRAHYDRONAPHTHALENE DERIVATIVES 失效
标题翻译：替代物1,2,3,4-四氢萘啶衍生物
公开(公告)号：EP1000048B1
公开(公告)日：2002-11-27
申请号：EP98934104.5
申请日：1998-07-15
申请人： AstraZeneca AB
发明人： BERG, Stefan , LINDERBERG, Mats , ROSS, Svante , THORBERG, Seth-Olov , ULFF, Bengt
IPC分类号： C07D295/135 , C07D295/155 , C07D211/26 , C07D211/34 , C07C237/24 , A61K31/495 , A61K31/445
CPC分类号： C07D295/192 , C07C237/24 , C07C2602/10 , C07D295/135 , C07D295/155 , C07D295/205
摘要： The present invention relates to new piperidyl-or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having formula (I) wherein X is N or CH; Y is NR2CH2, CH2-NR2, NR2-CO, CO-NR2 or NR2SO2 wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted, n is 0-4; R9 is C1-C6 alkyl, C3-C6 cycloalkyl, OCF3, OCHF2, OCH2F, halogen, CN, CF3, OH, C1-C6 alkoxy, C1-C6 alkoxy C1-C6 alkyl, NR6R7, SO3CH3, SO3CF3, SO2NR6R7, an unsubstituted or substituted heterocyclic or heteroaromatic ring containing one or two heteroatoms selected from N and O, wherein the substituent(s) is(are) C1-C6 alkyl; or COR8; wherein R6, R7 and R8 are as defined above, as (R)-enantiomers, (S)-enantiomers or racemates in the form of a free base or pharmaceutically acceptable salts thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds in therapy.
摘要翻译：本发明涉及具有式I的新的哌啶基或哌嗪基取代的-1,2,3,4-四氢萘衍生物，其中X是N或CH; Y是NR2CH2，CH2-NR2，NR2-CO，CO-NR2或NR2SO2，其中R2 是H或C 1 -C 6烷基; R 1是H，C 1 -C 6烷基或C 3 -C 6环烷基; R 3是C 1 -C 6烷基，C 3 -C 6环烷基或（CH 2）n - 芳基，其中芳基是苯基或含有一个或两个选自N，O和S的杂原子并且可被单取代或二取代的杂芳环是 0-4; R9是C1-C6烷基，C3-C6环烷基，OCF3，OCHF2，OCH2F，卤素，CN，CF3，OH，C1-C6烷氧基，C1-C6烷氧基-C1-C6烷基，NR6R7，SO3CH3，SO3CF3 ，SO 2 NR 6 R 7，含有一个或两个选自N和O的杂原子的未取代或取代的杂环或杂芳环，其中所述取代基为（C 1 -C 6）烷基; 或COR8; 其中R 6，R 7和R 8如上所定义，为游离碱形式的（R） - 对映异构体，（S） - 对映异构体或外消旋体或其药学上可接受的盐，其制备方法，含有所述治疗活性的药物组合物化合物和所述活性化合物在治疗中的用途。

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