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1. 发明公开

EP0410661A3 Bicyclic derivatives 失效
标题翻译：双相衍生物
公开(公告)号：EP0410661A3
公开(公告)日：1991-07-24
申请号：EP90308023.2
申请日：1990-07-23
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , ICI PHARMA
发明人： Bird, Thomas Geoffrey Colerick , Kingston, John Francis, 24 Cornfield Close , Waterson, David
IPC分类号： C07D407/04 , C07D317/46 , A61K31/36
CPC分类号： C07D407/04 , C07D317/46
摘要： The invention concerns a bicyclic derivative of the formula I, or a pharmaceutically-acceptable salt thereof.
wherein Ar¹ is optionally substituted phenyl or naphthyl;
R¹ if (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl; and
R² and R³ together form a group of the formula -A¹-X-A²-, wherein each of A¹ and A² is (1-4C)alkylene and X is oxy, thio, sulphinyl, sulphonyl or imino. The invention also concerns processes for the manufacture of a bicyclic derivative of the formula I, or a pharmaceutically-acceptable salt thereof, and pharmaceutical compositions containing said bicyclic derivatives. The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.

2. 发明公开

EP0351194A3 Thiazole derivatives having a 5-lipoxygenase-inhibiting activity 失效
标题翻译：杂环化合物
公开(公告)号：EP0351194A3
公开(公告)日：1990-06-27
申请号：EP89307041.7
申请日：1989-07-11
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , ICI PHARMA
发明人： Bird, Thomas Geoffrey Colerick , Edwards, Philip Neil , Crawley, Graham Charles , Girodeau, Jean-Marc Marie Maurice , Edwards, Martin Paul , Kingston, John Francis
IPC分类号： C07D277/20 , A61K31/425 , C07D417/06 , C07D277/24 , A61K31/435
CPC分类号： C07D417/06 , C07D277/24
摘要： The invention concerns a thiazole of the formula 1,
wherein Ar 1 is optionally substituted aryl of up to 10 carbon atoms;
A is a direct link to X, or is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene; X is oxy, thio, sulphinyl, sulphonyl or imino; Ar 2 is optionally substituted phenylene,
or a 6-membered heterocyclene moiety containing up to three nitrogen atoms; R 1 is hydrogen, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl or substituted (1-4C)alkyl; R 2 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, substituted (1-4C)alkyl or (2-6C)alkanoyl; Q is optionally substituted thiazolyl; or a pharmaceutically-acceptable salt thereof. The invention also concerns processes for the manufacture of a thiazole of the formula I, or a pharmaceutically-acceptable salt thereof, and pharmaceutical compositions containing said thiazole.

3. 发明公开

EP0409414A1 Diaryl ether cycloalkanes 失效
标题翻译：二芳基醚环烷烃
公开(公告)号：EP0409414A1
公开(公告)日：1991-01-23
申请号：EP90306766.8
申请日：1990-06-20
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , ICI PHARMA
发明人： Edwards, Philip Neil , Bird, Thomas Geoffrey Colerick
IPC分类号： C07C323/18 , A61K31/10
CPC分类号： C07C323/18
摘要： The invention concerns a diaryl ether cycloalkane of the formula I, or a pharmaceutically-acceptable salt thereof,
wherein Ar¹ is optionally substituted phenyl or naphthyl;
X¹ is oxy, thio, sulphinyl or sulphonyl;
Ar² is optionally substituted phenylene, or a 6-membered heterocyclene moiety containing up to three nitrogen atoms;
R¹ is (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl; and
R² and R³ together form a (3-6C)alkylene group which defines an optionally substituted ring having 4 to 7 ring atoms.
The invention also concerns processes for the manufacture of a diaryl ether cycloalkane of the formula I, or a pharmaceutically-acceptable salt thereof, and pharmaceutical compositions containing said cycloalkane. The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.
摘要翻译：本发明涉及式I的二芳基醚环烷烃或其药学上可接受的盐，其中Ar 1是任选取代的苯基或萘基; X 1是氧，硫，亚磺酰基或磺酰基; Ar 2是任选取代的亚苯基或含有至多三个氮原子的6元杂环部分; （1-6C）烷基，（3-6C）烯基，（3-6C）炔基，氰基 - （1-4C）烷基或（2-4C）烷酰基或任选取代的苯甲酰基; 并且R 2和R 3一起形成一个（3-6C）亚烷基，它定义了一个任选取代的具有4至7个环原子的环。本发明还涉及制备式I的二芳基醚环烷烃或其药学上可接受的盐的方法和含有所述环烷烃的药物组合物。本发明的化合物是5-脂氧合酶的抑制剂。

4. 发明公开

EP0409413A2 Diaryl ether heterocycles 失效
标题翻译： Diaryläther-Heterozyklen。
公开(公告)号：EP0409413A2
公开(公告)日：1991-01-23
申请号：EP90306765.0
申请日：1990-06-20
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , ICI PHARMA
发明人： Edwards, Philip Neil , Bird, Thomas Geoffrey Colerick
IPC分类号： C07D309/10 , C07D409/12 , A61K31/35
CPC分类号： C07D409/12 , C07D307/20 , C07D309/10
摘要： The invention concerns a diaryl ether heterocycle of the formula I, or a pharmaceutically-acceptable salt thereof,
wherein Ar¹ is optionally substituted phenyl or naphthyl;
X¹ is oxy, thio, sulphinyl or sulphonyl;
Ar² is optionally substituted phenylene, or a 6-membered heterocyclene moiety containing up to three nitrogen atoms;
R¹ is (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl; and
R² and R³ together form a group of the formula -A²-X²-A³- wherein each of A² and A³ is (1-4C)alkylene and X² is oxy, thio, sulphinyl, sulphonyl or imino.
The invention also concerns processes for the manufacture of a diaryl ether heterocycle of the formula I, or a pharmaceutically-acceptable salt thereof, and pharmaceutical compositions containing said heterocycle. The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.
摘要翻译：本发明涉及式I的二芳基醚杂环或其药学上可接受的盐，其中Ar 1是任选取代的苯基或萘基; X 1是氧基，硫基，亚磺酰基或磺酰基; Ar 2是任选取代的亚苯基，或含有至多三个氮原子的6-元杂环烯部分; （1-6C）烷基，（3-6C）烯基，（3-6C）炔基，氰基 - （1-4C）烷基或（2-4C）烷酰基或任选取代的苯甲酰基; 并且R 2和R 3一起形成式-A 2 -X 2 -A 3 - 的基团，其中A 2和A 3各自为（1-4C ）亚烷基，X 2是氧基，硫基，亚磺酰基，磺酰基或亚氨基。本发明还涉及制备式I的二芳基醚杂环或其药学上可接受的盐以及含有所述杂环的药物组合物的方法。本发明的化合物是5-脂氧合酶的抑制剂。

5. 发明授权

EP0410661B1 Bicyclic derivatives 失效
标题翻译： Bizyklische Derivate。
公开(公告)号：EP0410661B1
公开(公告)日：1994-06-15
申请号：EP90308023.2
申请日：1990-07-23
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , ICI PHARMA
发明人： Bird, Thomas Geoffrey Colerick , Kingston, John Francis, 24 Cornfield Close , Waterson, David
IPC分类号： C07D407/04 , C07D317/46 , A61K31/36
CPC分类号： C07D407/04 , C07D317/46

6. 发明授权

EP0351194B1 Thiazole derivatives having a 5-lipoxygenase-inhibiting activity 失效
标题翻译：噻唑衍生物具有5-脂氧合酶抑制活性。
公开(公告)号：EP0351194B1
公开(公告)日：1994-06-15
申请号：EP89307041.7
申请日：1989-07-11
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , ICI PHARMA
发明人： Bird, Thomas Geoffrey Colerick , Edwards, Philip Neil , Crawley, Graham Charles , Girodeau, Jean-Marc Marie Maurice , Edwards, Martin Paul , Kingston, John Francis
IPC分类号： C07D277/20 , A61K31/425 , C07D417/06 , C07D277/24 , A61K31/435
CPC分类号： C07D417/06 , C07D277/24

7. 发明公开

EP0409413A3 Diaryl ether heterocycles 失效
标题翻译：二元醚等离子体
公开(公告)号：EP0409413A3
公开(公告)日：1991-07-17
申请号：EP90306765.0
申请日：1990-06-20
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , ICI PHARMA
发明人： Edwards, Philip Neil , Bird, Thomas Geoffrey Colerick
IPC分类号： C07D309/10 , C07D409/12 , A61K31/35
CPC分类号： C07D409/12 , C07D307/20 , C07D309/10
摘要： The invention concerns a diaryl ether heterocycle of the formula I, or a pharmaceutically-acceptable salt thereof,
wherein Ar¹ is optionally substituted phenyl or naphthyl;
X¹ is oxy, thio, sulphinyl or sulphonyl;
Ar² is optionally substituted phenylene, or a 6-membered heterocyclene moiety containing up to three nitrogen atoms;
R¹ is (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl; and
R² and R³ together form a group of the formula -A²-X²-A³- wherein each of A² and A³ is (1-4C)alkylene and X² is oxy, thio, sulphinyl, sulphonyl or imino. The invention also concerns processes for the manufacture of a diaryl ether heterocycle of the formula I, or a pharmaceutically-acceptable salt thereof, and pharmaceutical compositions containing said heterocycle. The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.

8. 发明授权

EP0409413B1 Diaryl ether heterocycles 失效
标题翻译： Diaryläther-Heterozyklen。
公开(公告)号：EP0409413B1
公开(公告)日：1994-08-03
申请号：EP90306765.0
申请日：1990-06-20
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , ICI PHARMA
发明人： Edwards, Philip Neil , Bird, Thomas Geoffrey Colerick
IPC分类号： C07D309/10 , C07D409/12 , A61K31/35
CPC分类号： C07D409/12 , C07D307/20 , C07D309/10

9. 发明授权

EP0409414B1 Diaryl ether cycloalkanes 失效
标题翻译： DIARYL循环圈
公开(公告)号：EP0409414B1
公开(公告)日：1993-09-29
申请号：EP90306766.8
申请日：1990-06-20
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , ICI PHARMA
发明人： Edwards, Philip Neil , Bird, Thomas Geoffrey Colerick
IPC分类号： C07C323/18 , A61K31/10
CPC分类号： C07C323/18

10. 发明公开

EP0410661A2 Bicyclic derivatives 失效
标题翻译： Bizyklische Derivate。
公开(公告)号：EP0410661A2
公开(公告)日：1991-01-30
申请号：EP90308023.2
申请日：1990-07-23
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , ICI PHARMA
发明人： Bird, Thomas Geoffrey Colerick , Kingston, John Francis, 24 Cornfield Close , Waterson, David
IPC分类号： C07D407/04 , C07D317/46 , A61K31/36
CPC分类号： C07D407/04 , C07D317/46
摘要： The invention concerns a bicyclic derivative of the formula I, or a pharmaceutically-acceptable salt thereof.
wherein Ar¹ is optionally substituted phenyl or naphthyl;
R¹ if (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl; and
R² and R³ together form a group of the formula -A¹-X-A²-, wherein each of A¹ and A² is (1-4C)alkylene and X is oxy, thio, sulphinyl, sulphonyl or imino.
The invention also concerns processes for the manufacture of a bicyclic derivative of the formula I, or a pharmaceutically-acceptable salt thereof, and pharmaceutical compositions containing said bicyclic derivatives. The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.
摘要翻译：本发明涉及式I的双环衍生物或其药学上可接受的盐。其中Ar 1是任选取代的苯基或萘基; （1-6C）烷基，（3-6C）烯基，（3-6C）炔基，氰基 - （1-4C）烷基或（2-4C）烷酰基或任选取代的苯甲酰基; 和R 2和R 3一起形成式-A 1 -XA 2 - 的基团，其中A 1和A 2各自为（1-4C）亚烷基和X 是氧基，硫基，亚磺酰基，磺酰基或亚氨基。本发明还涉及制备式I的双环衍生物或其药学上可接受的盐以及含有所述双环衍生物的药物组合物的方法。本发明的化合物是5-脂氧合酶的抑制剂。

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