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1. 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

2. 发明公开

EP0409412A3 Diaryl ether cyclic ethers 失效
标题翻译：二芳基醚环醚
公开(公告)号：EP0409412A3
公开(公告)日：1991-07-24
申请号：EP90306763.5
申请日：1990-06-20
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , ICI PHARMA
发明人： Edwards, Philip Neil , Bird, Thomad Geoffrey Colerick
IPC分类号： C07D317/18 , C07D317/22 , A61K31/335
CPC分类号： C07D317/22
摘要： The invention concerns a diaryl ether cyclic ether 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 and R² 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; and
R³ is (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl and substituted (1-4C)alkyl. The invention also concerns processes for the manufacture of a diaryl ether cyclic ether of the formula I, or a pharmaceutically-acceptable salt thereof, and pharmaceutical compositions containing said cyclic ether. The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.
摘要翻译：本发明涉及式I的二芳基醚环醚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; R 1和R 2一起形成式-A 2 -X 2 -A 3 - 的基团，其中A 2和A 3各自是（1-4C）亚烷基，X 2是氧，硫，亚磺酰基，磺酰基或亚氨基; （1-6C）烷基，（2-6C）链烯基，（2-6C）炔基和取代的（1-4C）烷基。本发明还涉及制备式I的二芳基醚环状醚或其药学上可接受的盐的方法，以及含有所述环状醚的药物组合物。本发明的化合物是5-脂氧合酶的抑制剂。

3. 发明授权

EP0124369B1 Phenol derivatives 失效
标题翻译：苯酚衍生物
公开(公告)号：EP0124369B1
公开(公告)日：1987-06-24
申请号：EP84302860.6
申请日：1984-04-27
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC
发明人： Crawley, Graham Charles , Edwards, Philip Neil , Hill, George Beresford , Pilgrim, William Robert , Tait, Brian Steele , Young, Derek William
IPC分类号： C07C149/36 , C07C147/14 , C07C147/10 , C07C103/76 , C07C103/737
CPC分类号： C07F9/6552 , C07C43/225 , C07C43/23 , C07C45/305 , C07C45/44 , C07C45/46 , C07C45/513 , C07C45/60 , C07C45/68 , C07C49/755 , C07C59/64 , C07C59/72 , C07C62/34 , C07C309/00 , C07C317/00 , C07C323/00 , C07C2602/08 , C07C2602/10 , C07D333/60 , C07F7/1852 , C07C47/277 , C07C49/84

4. 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。

5. 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。

6. 发明授权

EP0163416B1 Phenol derivatives 失效
标题翻译：苯酚衍生物
公开(公告)号：EP0163416B1
公开(公告)日：1989-05-31
申请号：EP85302881.9
申请日：1985-04-24
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC
发明人： Bowler, Jean , Glen, Alasdair Thomas , Crawley, Graham Charles , Large, Michael Stewart , Edwards, Philip Neil , Tait, Brian Steele
IPC分类号： C07C103/34 , C07C147/14 , C07C147/02 , C07C149/18 , C07C149/20 , C07C149/26 , C07C149/273 , A61K31/16 , A61K31/215 , A61K31/10
CPC分类号： C07C323/16 , C07C45/46 , C07C45/515 , C07C45/68 , C07C49/755 , C07C49/757 , C07C65/40 , C07C317/18 , C07C2602/10 , C07F7/1856 , C07F9/5031

7. 发明公开

EP0160508A3 Phenol derivatives 失效
标题翻译：苯酚衍生物
公开(公告)号：EP0160508A3
公开(公告)日：1986-10-08
申请号：EP85302882
申请日：1985-04-24
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC
发明人： Edwards, Philip Neil , Tait, Brian Steele
IPC分类号： C07C103/34 , C07C125/065 , C07C147/14 , C07C149/16 , C07C149/247 , C07C149/273 , C07D207/16 , A61K31/16 , A61K31/215 , A61K31/10
CPC分类号： C07D207/16 , C07C271/22 , C07C317/00 , C07C323/00
摘要： Mono- or bis-complex esters or ethers of a phenol derivative of the formula
wherein NU is a defined mono- or bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl;
hydroxyphenyl-hydroxyindanyl, hydroxyphenyl-hydroxy--benzothienyl or di-hydrdxyphenyl-ethylene or vinylene nucleus; wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages, wherein R'is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R' is joined to R 2 , and wherein X is -CONR 2 -, -CSNR 2 -,-NR 12 CO-, -NR 12 CS-, -NR 12 CONR 2 -,
-SO 2 NR 2 - or -CO-, or, when R 1 is not hydrogen, is -NR 12 COO-, -S-, -SO- or -S0 2 -, wherein R 2 is hydrogen or alkyl, or R 1 and R 2 together form alkylene; wherein R 12 is hydrogen or alkyl, and wherein R 22 is hydrogen, cyano or nitro; or a salt thereof when appropriate. The compounds possess antioestrogenic activity and may be used for the treatment of hormone-dependent breast tumours or of anovulatory infertility.
摘要翻译：下式的酚衍生物的单或双配位酯或醚，其中NU是定义的单酚或双酚核，包括羟苯基 - 羟基萘基; 羟基苯基 - 羟基茚基，羟基苯基 - 羟基 - 苯并噻吩基或二 - 羟基苯基 - 乙烯或亚乙烯基核; 其中A为亚烷基，亚烯基或亚炔基，其可被亚苯基或其它键中断，其中R'为氢或烷基，烯基，环烷基，卤代烷基，芳基或芳基烷基，或R'与R2连接，且其中X为 - CONR 2 - ， - CSNR 2 - ， - NR 12 CO - ， - NR 12 CS-，-NR 12 CONR 2 - ， - SO 2 NR 2 - 或-CO-，或者当R 1不为氢时为-NR 12 COO - - ，其中R 2是氢或烷基，或者R 1和R 2一起形成亚烷基; 其中R12是氢或烷基，并且其中R22是氢，氰基或硝基; 或适当的盐。该化合物具有抗雌激素活性，可用于治疗激素依赖性乳腺肿瘤或无排卵性不育症。

8. 发明授权

EP0037697B1 Dioxolane derivatives for use as chemical intermediates 失效
标题翻译：用作化学中间体的二氧化钛衍生物
公开(公告)号：EP0037697B1
公开(公告)日：1984-08-01
申请号：EP81301391.9
申请日：1981-03-31
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC
发明人： Edwards, Philip Neil , Martin, David Michael Glanville
IPC分类号： C07D317/34 , C07C59/66
CPC分类号： C07D317/34 , C07C45/49 , C07C59/66 , C07C47/55

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

EP0420511A3 Heterocyclic derivatives 失效
标题翻译：杂环衍生物
公开(公告)号：EP0420511A3
公开(公告)日：1991-08-28
申请号：EP90310332.3
申请日：1990-09-21
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , ICI PHARMA
发明人： Crawley, Graham Charles , Edwards, Philip Neil
IPC分类号： C07D405/12 , C07D409/12 , C07D401/12 , A61K31/47 , A61K31/50
CPC分类号： C07D409/12 , C07D401/12 , C07D405/12
摘要： The invention concerns a heterocyclic derivative of the formula I
wherein Q is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;
X¹ is oxy, thio, sulphinyl, sulphonyl or imino;
Ar is phenylene which may optionally bear one or two substituents or
Ar is an optionally substituted 6-membered heterocyclene moiety containing up to three nitrogen atoms;
R¹ is (1-6C)alkyl, (3-6C)alkenyl or (3-6C)alkynyl; and
R² and R³ together form a group of the formula -A²-X²-A³- which, together with the carbon atom to which A² and A³ are attached, defines a ring having 4 to 7 ring atoms, wherein A² and A³, which may be the same or different, each is (1-4C)alkylene and X² is oxy, thio, sulphinyl, sulphonyl or imino;
or a pharmaceutically-acceptable salt thereof. The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.

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