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1. 发明公开

EP0385721A3 Process for the preparation of lactam derivatives 失效
标题翻译：制备乳酸衍生物的方法
公开(公告)号：EP0385721A3
公开(公告)日：1991-10-09
申请号：EP90302075.8
申请日：1990-02-27
申请人： GLAXO GROUP LIMITED
发明人： Coates, Ian Harold , Oxford, Alexander William , North, Peter, Charles , Miller, Thomas , Baxter, Anthony David , Hammond, Kevin Ian
IPC分类号： C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04 , Y02P20/55
摘要： The invention provides a process for the preparation of a compound of general formula (I):
wherein Im represents an imidazolyl group of the formula :
and R¹ represents a hydrogen atom or a group selected from C₁₋₆alkyl, C₃₋₆alkenyl, C₃₋₁₀alkynyl, C₃₋₇cycloalkyl, C₃₋₇cycloalkylC₁₋₄alkyl, phenyl, phenylC₁₋₃alkyl, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, -CO₂R⁵, -COR⁵, -CONR⁵R⁶ or -SO₂R⁵ (wherein R⁵ and R⁶, which may be the same or different, each represents a hydrogen atom, a C₁₋₆alkyl or C₃₋₇cycloalkyl group, or a phenyl or phenylC₁₋₄alkyl group, in which the phenyl group is optionally substituted by one or more C₁₋₄alkyl, C₁₋₄alkoxy or hydroxy groups or halogen atoms, with the proviso that R⁵ does not represent a hydrogen atom when R¹ represents a group -CO₂R⁵ or -SO₂R⁵);
one of the groups represented by R², R³ and R⁴ is a hydrogen atom or a C₁₋₆alkyl, C₃₋₇cycloalkyl, C₃₋₆alkenyl, phenyl or phenylC₁₋₃alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C₁₋₆alkyl group; and n represents 2 or 3;
which comprises reacting a compound of formula (II)
or a protected derivative thereof, with a compound of formula (III):
HOCH₂-Im (III)
or a salt thereof in the presence of an acid at an elevated temperature, followed where necessary by removal of any protecting groups.
摘要翻译：本发明提供了制备通式（I）的化合物的方法：其中Im表示下式的咪唑基：其中R 1表示氢原子或选自C1- C 1-6烷基，C 3-6烯基，C 3-10炔基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基，苯基C 1-3烷基，苯基甲氧基甲基，苯氧基乙基，苯氧基甲基，-CO 2 R 5，-COR 5，-CONR 5 R 6或-SO 2 R 5（其中R 5和R 6可以相同或不同，各自表示氢原子，C 1-6烷基或C 3-7环烷基，或苯基或苯基C 1 -4-烷基，其中苯基任选被一个或多个C 1-4烷基，C 1-4烷氧基或羟基或卤素原子取代，条件是R 5不表示氢原子，当R 1表示基团-CO 2 R 5或-SO 2 R 5）; 由R 2，R 3和R 4表示的基团之一是氢原子或C 1-6烷基，C 3-7环烷基，C 3-6烯基，苯基或苯基C 1-3烷基，其中每一个两个可以相同或不同的基团表示氢原子或C1-6烷基; n表示2或3; 其包括使式（II）化合物或其保护的衍生物与式（III）化合物：HOCH 2 -Im（III）或其盐在酸的存在下在升高的温度下反应，随后必要时通过去除任何保护基团。

2. 发明授权

EP0237678B1 Tryptamine derivatives, their synthesis and their use in pharmaceutical compositions 失效
标题翻译：三甲胺衍生物，其合成及其在药物组合物中的应用
公开(公告)号：EP0237678B1
公开(公告)日：1991-04-03
申请号：EP86309647.5
申请日：1986-12-11
申请人： GLAXO GROUP LIMITED
发明人： Oxford, William Alexander , Bays, David Edmund , Coates, Ian Harold , Webb, Colin Frederick
IPC分类号： C07D209/16 , A61K31/40
CPC分类号： C07D209/16

3. 发明公开

EP0303506A3 Indole derivatives 失效
标题翻译：吲哚衍生物
公开(公告)号：EP0303506A3
公开(公告)日：1990-09-26
申请号：EP88307498.1
申请日：1988-08-12
申请人： GLAXO GROUP LIMITED
发明人： Oxford, Alexander William , Coates, Ian Harold , Butina, Darko
IPC分类号： C07D401/04 , A61K31/445
CPC分类号： C07D401/04
摘要： Compounds are disclosed of formula (I)
wherein
R₁ represents H or C₁₋₆ alkyl;
R₂ represents H, C₁₋6 alkyl, C₃₋₇ cycloalkyl, C₃₋₆ alkenyl, phenyl or phen(C₁₋₃)alkyl in which the phenyl ring is optionally substituted by halogen, C₁₋₄ alkoxy, hydroxy or C₁₋₃ alkyl;
R₃ represents H, C₁₋₃ alkyl, -CO₂R₅, -COR₅, -COCO₂R₅ or -CONHR₅ where
R₅ represents H, C₁₋₄ alkyl, C₃₋₇ cycloalkyl, C₂₋₄ alkenyl, aryl or ar(C₁₋₄)alkyl in which the aryl group is optionally substituted by halogen, C₁₋₄ alkoxy, C₁₋₄ alkyl or hydroxy) (provided that where R₃ represents -CO₂R₅, R₅ is other than H);
R₄ represents H, C₁₋₃ alkyl, C₃₋₆ alkenyl, phenyl or phen(C₁₋₃)alkyl;
A-B represents CH-CH₂- or C=CH-
D represents -CO- or -SO₂-
n represents 0, 1-5;
provided that when D represents -SO₂, n is 2, R₃ represents H and R₄ represents H or C₁₋₃ alkyl, R₂ is other than H or C₁₋₆ alkyl;
and pharmaceutically acceptable salts and solvates (for example hydrates) thereof. The compounds are indicated as useful for the treatment of migraine, cluster headache, chronic paroxysmal hemicrania and headache associated with vascular disorders. Processes and intermediates for their preparation and pharmaceutical compositions containing them are also disclosed.
摘要翻译：公开了式（Ⅰ）的化合物，其中R 1代表H或C 1-6烷基; R 2代表H，C 1-6烷基，C 3-8环烷基，C 3-6链烯基，苯基或苯基（C 1-3）烷基，其中苯环可被卤素，C 1-4烷氧基，羟基或C 1-3烷基 ; R 3代表H，C 1-3烷基，-CO 2 R 5，-COR 5，-COCO 2 R 5或-CONHR 5，其中R 5代表H，C 1-4烷基，C 3-8环烷基，C 2-4链烯基，芳基或芳基（C 1-4）（其中芳基可被卤素，C 1-4烷氧基，C 1-4烷基或羟基取代）（条件是其中R 3代表-CO 2 R 5，R 5不是H）。 R 4代表H，C 1-3烷基，C 3-6链烯基，苯基或苯（C 1-3）烷基; A-B代表CH-CH 2 - 或C = CH- D代表-CO-或-SO 2 - n代表0,1-5; 条件是当D代表-SO 2时，n是2，R 3代表H，R 4代表H或C 1-3烷基，R 2不是H或C 1-6烷基; 及其药学上可接受的盐和溶剂化物（例如水合物）。该化合物可用于治疗偏头痛，丛集性头痛，慢性阵发性偏头痛和与血管疾病相关的头痛。还公开了其制备方法和中间体以及含有它们的药物组合物。

4. 发明公开

EP0357415A3 Use of serotonin antagonists in the treatment of cognitive disorders 失效
标题翻译：使用丝氨酸拮抗剂治疗认知障碍
公开(公告)号：EP0357415A3
公开(公告)日：1990-08-08
申请号：EP89308805.4
申请日：1989-08-31
申请人： GLAXO GROUP LIMITED
发明人： Coates, Ian Harold , Oxford, Alexander William , North, Peter Charles , Tyers, Michael Brian
IPC分类号： A61K31/00 , A61K31/445 , A61K31/55
CPC分类号： A61K31/445 , A61K31/00 , A61K31/55
摘要： The invention relates to the use of compounds of formula
wherein Im represents an imidazolyl group of formula:
and R¹ represents a hydrogen atom or a group selected from C₁₋₆alkyl, C₃₋₆alkenyl, C₃₋₁₀alkynyl, C₃₋₇cycloalkyl,C₃₋₇cycloalkylC₁₋₄alkyl, phenyl, phenylC₁₋₃alkyl, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, -CO₂R⁵, -COR⁵, -CONR⁵R⁶ or -SO₂R⁵ (wherein R⁵ and R⁶, which may be the same or different, each represents a hydrogen atom, a C₁₋₆alkyl or C₃₋₇cycloalkyl group, or a phenyl or phenylC₁₋₄alkyl group, in which the phenyl group is optionally substituted by one or more C₁₋₄alkyl, C₁₋₄alkoxy or hydroxy groups or halogen atoms, with the proviso that R⁵ does not represent a hydrogen atom when R¹ represents a group -CO₂R⁵ or -SO₂R⁵);
one of the groups represented by R², R³ and R⁴ is a hydrogen atom or a C₁₋₆alkyl, C₃₋₇cycloalkyl, C₃₋₆alkenyl, phenyl or phenylC₁₋₃alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C₁₋₆ alkyl group;
and n represents 2 or 3,
and physiologically acceptable salts and solvates thereof for the manufacture of a medicament for the treatment of a cognitive disorder.

5. 发明公开

EP0357416A3 Use of serotonin antagonists in the treatment of drug addiction 失效
标题翻译：使用丝氨酸拮抗剂治疗药物治疗
公开(公告)号：EP0357416A3
公开(公告)日：1990-06-06
申请号：EP89308806.2
申请日：1989-08-31
申请人： GLAXO GROUP LIMITED
发明人： Coates, Ian Harold , Oxford, Alexander William , North, Peter Charles , Tyers, Michael Brian
IPC分类号： A61K31/00 , A61K31/445 , A61K31/55
CPC分类号： A61K31/00 , A61K31/445 , A61K31/55
摘要： The invention relates to the use of compounds of formula (I)
wherein Im represents an imidazolyl group of formula:
and R¹ represents a hydrogen atom or a group selected from C₁₋₆alkyl, C₃₋₆alkenyl, C₃₋₁₀alkynyl, C₃₋₇cycloalkyl, C₃₋₇cycloalkylC₁₋₄alkyl, phenyl, phenylC₁₋₃alkyl, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, -CO₂R⁵, -COR⁵, -CONR⁵R⁶ or -SO₂R⁵ (wherein R⁵ and R⁶, which may be the same or different, each represents a hydrogen atom, a C₁₋₆alkyl or C₃₋₇cycloalkyl group, or a phenyl or phenylC₁₋₄alkyl group, in which the phenyl group is optionally substituted by one or more C₁₋₄alkyl, C₁₋₄alkoxy or hydroxy groups or halogen atoms, with the proviso that R⁵ does not represent a hydrogen atom when R¹ represents a group -CO₂R⁵ or -SO₂R⁵);
one of the groups represented by R², R³ and R⁴ is a hydrogen atom or a C₁₋₆alkyl, C₃₋₇cycloalkyl, C₃₋₆alkenyl, phenyl or phenyl C₁₋₃alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C₁₋₆ alkyl group;
and n represents 2 or 3,
and physiologically acceptable salts and solvates thereof for the manufacture of a medicament for the relief or prevention of a withdrawal syndrome resulting from addiction to a drug of substance of abuse and/or for the suppression of dependence on drugs or substances of abuse.

6. 发明公开

EP0356098A2 Lactam derivatives 失效
标题翻译：内酰胺衍生物
公开(公告)号：EP0356098A2
公开(公告)日：1990-02-28
申请号：EP89308229.7
申请日：1989-08-14
申请人： GLAXO GROUP LIMITED
发明人： Coates, Ian Harold , Oxford, Alexander William , North, Peter Charles
IPC分类号： C07D471/04 , A61K31/435
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention provides tricyclic lactams of the general formula (I)
wherein Im represents an imidazolyl group of the formula :
and R¹ represents a hydrogen atom or a group selected from C₁₋₆alkyl, C₃₋₆alkenyl, C₃₋₁₀alkynyl, C₃₋₇cycloalkyl, C₃₋₇cycloalkylC₁₋₄alkyl, phenyl, phenylC₁₋₃alkyl, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, -CO₂R⁵, -COR⁵, -CONR⁵R⁶ or -SO₂R⁵ (wherein R⁵ and R⁶, which may be the same or different, each represents a hydrogen atom, a C₁₋₆alkyl or C₃₋₇cycloalkyl group, or a phenyl or phenylC₁₋₄alkyl group, in which the phenyl group is optionally substituted by one or more C₁₋₄ alkyl, C₁₋₄alkoxy or hydroxy groups or halogen atoms, with the proviso that R⁵ does not represent a hydrogen atom when R¹ represents a group -CO₂R⁵ or -SO₂R⁵);
one of the groups represented by R², R³ and R⁴ is a hydrogen atom or a C₁₋₆alkyl, C₃₋₇cycloalkyl, C₃₋₆alkenyl, phenyl or phenylC₁₋₃alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C₁₋₆alkyl group;
and physiologically acceptable salts and solvates thereof.
The compounds of formula (I) or potent and selective antagonists of 5-hydroxytryptamine at 5-HT₃ receptors and are useful, for example, in the treatment of psychotic disorders, anxiety and nausea and vomiting.
摘要翻译：本发明提供了通式（I）的三环内酰胺，其中Im代表下式的咪唑基：和R 1代表氢原子或选自C 1-6烷基，C 3-6链烯基，C 3-10炔基，C 3-8环烷基，C 3 苯基，苯基C 1-3烷基，苯基甲氧基甲基，苯氧基乙基，苯氧基甲基，-CO 2 R 5，-COR 5，-CONR 5 R 6或-SO 2 R 5（其中R 5和R 6可以相同或不同，各自代表氢原子，C 1 C 1-6烷基或C 3-8环烷基，或苯基或苯基C 1-4烷基，其中苯基可任意地被一个或多个C 1-4烷基，C 1-4烷氧基或羟基或卤素原子取代，前提条件是R 5确实当R 1代表基团-CO 2 R 5或-SO 2 R 5时不代表氢原子; 由R 2，R 3和R 4代表的基团之一是氢原子或C 1-6烷基，C 3-8环烷基，C 3-6链烯基，苯基或苯基C 1-3烷基，并且其它两个基团中的每一个可以相同，或者不同，代表氢原子或C 1-6烷基; 和其生理上可接受的盐和溶剂合物。式（Ⅰ）化合物或5-羟色胺在5-HT 3受体上的有效和选择性拮抗剂，可用于例如治疗精神病，焦虑和恶心和呕吐。

7. 发明公开

EP0240096A1 Indole derivatives having a selective vasoconstrictor activity 失效
标题翻译： Indolderivate mit selektiver Vasokonstriktor-Wirkung。
公开(公告)号：EP0240096A1
公开(公告)日：1987-10-07
申请号：EP87300166.3
申请日：1987-01-08
申请人： GLAXO GROUP LIMITED
发明人： Mills, Keith , Eldred, Colin David , Oxford, Alexander William , Dowle, Michael Dennis , Coates, Ian Harold , Bays, David Edmund , Webb, Colin Frederick
IPC分类号： C07D209/14 , A61K31/40
CPC分类号： C07D209/16
摘要： Compounds are disclosed of formula (I):
wherein

R, represents halogen, C 1 3 alkoxy, or a group
R 6 R 7 NCO(CH 2 ) p -, R 6 CONH(CH 2 ) P -, R 6 R 7 NSO 2 (CH 2 ) p -,
or R 8 SO 2 NH(CH 2 ) p - (where R 6 and R 7 , each independently represents hydrogen or C, 3 alkyl, R a represents C 1 3 alkyl and p is zero or 1);
R 2 represents hydrogen or C, 3 alkyl; R 3 represents hydrogen or C, 3 alkyl;
R 4 and R 5 each independently represents hydrogen,
a C 1 3 alkyl or a 2-propenyl group;
A represents -CO- or -SO 2 -;
n represents an integer from 2 to 5; an m represents zero or an integer from 1 to 4; and physiologically acceptable salts and solvates (e.g. hydrates) thereof.

The compounds have potent and selective vasoconstrictor activity and are indicated as useful for the treatment of migraine. The compounds may be formulated as pharmaceutical compositions with pharmaceutically acceptable carriers or excipients for administration by any suitable means. Various methods for the preparation of the compounds are disclosed.
摘要翻译：公开了式（I）化合物：其中R 1表示卤素，C 3烷氧基或基团R 6 R 7 NCO（CH 2）p - ，R 6 CONH（CH 2）p - ，R 6 R 7 NSO 2（CH 2）p - 或R 8 SO 2 NH（CH 2）对 - （其中R 6和R 7各自独立地表示氢或C 1-3烷基，R 8表示C 1-3烷基，p表示0或1）。 R 2表示氢或C 1-3烷基; R 3表示氢或C 1-3烷基; R 4和R 5各自独立地表示氢，C 1-3烷基或2-丙烯基; A表示-CO-或-SO 2 - ; n表示2〜5的整数， m表示0或1至4的整数; 和其生理上可接受的盐和溶剂合物（例如水合物）。这些化合物具有有效和选择性的血管收缩剂活性，并被用于治疗偏头痛。化合物可以配制成具有药学上可接受的载体或赋形剂的药物组合物，用于通过任何合适的方式给药。公开了制备化合物的各种方法。

8. 发明授权

EP0385721B1 Process for the preparation of lactam derivatives 失效
标题翻译： Verfahren zur Herstellung von Lactamderivaten。
公开(公告)号：EP0385721B1
公开(公告)日：1995-01-25
申请号：EP90302075.8
申请日：1990-02-27
申请人： GLAXO GROUP LIMITED
发明人： Coates, Ian Harold , Oxford, Alexander William , North, Peter, Charles , Miller, Thomas , Baxter, Anthony David , Hammond, Kevin Ian
IPC分类号： C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04 , Y02P20/55

9. 发明授权

EP0219193B1 Tetrahydrocarbazolone derivatives, processes for their preparation and pharmaceutical compositions containing them 失效
标题翻译：四氯化碳衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：EP0219193B1
公开(公告)日：1992-05-27
申请号：EP86305674.3
申请日：1986-07-23
申请人： GLAXO GROUP LIMITED
发明人： Coates, Ian Harold , Bell, James Angus , Humber, David Cedric , Ewan, George Blanch
IPC分类号： C07D403/06 , A61K31/415 , C07D209/88
CPC分类号： C07D231/12 , C07D209/88 , C07D233/56 , C07D249/08 , C07D403/06

10. 发明公开

EP0431443A3 Use of tetrahydrocarbazolone derivatives for the manufacture of medicaments 失效
标题翻译：四氯化碳激光衍生物用于制造药物的用途
公开(公告)号：EP0431443A3
公开(公告)日：1991-09-18
申请号：EP90122615.9
申请日：1986-06-24
申请人： GLAXO GROUP LIMITED
发明人： Tyers, Michael Brian , Coates, Ian Harold , Bell, James Angus , Humber, David Cedric , Ewan, George Blanch
IPC分类号： A61K31/415
CPC分类号： A61K31/415 , Y10S514/872 , Y10S514/917 , Y10S514/922 , A61K31/34 , A61K2300/00
摘要： The invention relates to the use of compounds of the general formula (I)
wherein
R¹ represents a hydrogen atom or a C₁₋₁₀ alkyl, C₃₋₇ cycloalkyl, C₃₋₇ cycloalkyl-(C₁₋₄) alkyl, C₃₋₆ alkenyl, C₃₋₁₀ alkynyl, phenyl or phenyl-C₁₋₃ alkyl group; and one of the groups represented by
R², R³, and R⁴ is a hydrogen atom or a C₁₋₆ alkyl, C₃₋₇cycloalkyl, C₂₋₆ alkenyl or phenyl - C₁₋₃ alkyl group and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C₁₋₆ alkyl group;
and physiologically acceptable salts and solvates thereof, for the relief of nausea and vomiting and/or the promotion of gastric emptying and for the manufacture of a medicament for this purpose. Promotion of gastric emptying may be for the relief of gastro-intestinal disorders associated with gastric stasis or may be of advantage in radiological examination procedures. The invention also relates to a product containing a therapeutic agent liable to induce nausea and vomiting, e.g. a cytostatic agent such as a cyclophosphamide, an alkylating agent or a platinum complex, and a compound of the general formula (I) as a combined preparation for simultaneous separate or sequential use in therapy.

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