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61. 发明公开

EP0055562A2 Cephalosporin derivatives 有权转让
标题翻译：头孢菌素。
公开(公告)号：EP0055562A2
公开(公告)日：1982-07-07
申请号：EP81305958.1
申请日：1981-12-18
申请人： ICI PHARMA , IMPERIAL CHEMICAL INDUSTRIES PLC
发明人： Jung, Frédéric Henri , Davies, Gareth Morse
IPC分类号： C07D501/18 , C07D498/04 , C07D487/04 , C07D471/04 , A61K31/545
CPC分类号： C07D209/48 , C07D207/34 , C07D463/20 , C07D463/22 , C07D487/04 , C07D505/00
摘要： A cephalosporin derivative of the formula :-
in which R 0 is a hydrogen atom or a methyl radical; R' is any one of the C-3 substituents from antibacterially-active cephalosporins known in the art; R 2 is any one of the C-4 substituents from antibacterially-active cephalosporins known in the art; R 3 is a hydrogen atom or a 1-6C alkoxy or 1-6C alkylthio radical; X 1 is a sulphur or oxygen atom, a CH 2 radical or a radical of the formula NR 7 in which R 7 is a hydrogen atom, a 1-6C alkyl, formyl or benzyl radical; X 2 is a nitrogen atom or a radical of the formula

R 4 and R 7 , and R 5 and R 6 are a variety of substituents which are described in the specification; and the pharmaceutically-acceptable acid- or base- addition salts thereof. Pharmaceutical compositions, manufacturing processes and intermediates are also described.

62. 发明授权

EP0490634B1 Quinolinium salts intermediates 失效
标题翻译：喹啉盐中间体
公开(公告)号：EP0490634B1
公开(公告)日：1997-06-18
申请号：EP91311468.2
申请日：1991-12-10
申请人： ZENECA LIMITED , ICI PHARMA
发明人： Hutton, Jonathan , Waterson, David
IPC分类号： C07D405/12
CPC分类号： C07D405/12

63. 发明授权

EP0269298B1 Cephalosporins, process for their preparation and pharmaceutical compositions 失效
标题翻译：头孢菌素，其制备方法和药物组合物
公开(公告)号：EP0269298B1
公开(公告)日：1994-10-19
申请号：EP87309852.9
申请日：1987-11-06
申请人： ICI PHARMA
发明人： Bertrandie, Alain Michel , Bird, Thomas Geoffrey Colerick , Jung, Frederic Henry
IPC分类号： C07D501/46 , C07D501/36 , C07D501/34 , C07D501/20 , A61K31/545 , C07D501/56
CPC分类号： A61K31/545

64. 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

65. 发明授权

EP0375457B1 Cyclic ether derivatives 失效
标题翻译： ZyklischeÄtherderivate。
公开(公告)号：EP0375457B1
公开(公告)日：1994-03-16
申请号：EP89313521.0
申请日：1989-12-22
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , ICI-PHARMA
发明人： Hammon, Annie
IPC分类号： C07D317/22 , A61K31/335
CPC分类号： C07D405/04 , C07D317/22 , C07D327/04

66. 发明授权

EP0284174B1 Therapeutic preparations 有权
标题翻译：治疗准备
公开(公告)号：EP0284174B1
公开(公告)日：1992-07-29
申请号：EP88300281.8
申请日：1988-01-14
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , ICI PHARMA
发明人： Bruneau, Pierre Andre Raymond , Carey, Frank , Delvare, Christian Robert Ernest , Gibson, Keith Hopkinson , McMillan, Rodger Martin
IPC分类号： C07D231/56 , C07D401/06 , C07D405/06 , C07D409/06 , C07D401/10 , C07D403/06 , C07D417/06 , C07D403/12 , C07D405/12 , C07D401/12 , C07D413/06
CPC分类号： C07D231/56 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D413/06 , C07D417/06

67. 发明公开

EP0462813A3 Bicyclic pyran derivatives and their use as inhibitors of 5-lipoxygenase 失效转让
标题翻译：双相PYRAN衍生物及其作为5-LIPOXYGENASE的抑制剂的用途
公开(公告)号：EP0462813A3
公开(公告)日：1992-01-22
申请号：EP91305532.3
申请日：1991-06-19
申请人： ZENECA LIMITED , ICI PHARMA
发明人： Bruneau, Pierre André Raymond , Crawley, Graham Charles, Chapel House
IPC分类号： C07D413/12 , C07D417/12 , C07D498/04 , A61K31/535 , A61K31/54
CPC分类号： C07D413/10 , C07D413/12 , C07D417/12
摘要： The invention concerns a bicyclic heterocyclic compound of the formula I, or a pharmaceutically-acceptable salt thereof. The invention concerns also processes for the manufacture of a bibyclic heterocyclic compound of the formula I, or a pharmaceutically-acceptable salt thereof, and pharmaceutical compositions containing said compound. Also included in the invention is a method of treating various inflammatory or allergic diseases using a bibyclic heterocyclic compound of the formula I, or a pharmaceutically-acceptable salt thereof, and the use of such a compound in the production of a new medicament for such use.

68. 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。

69. 发明公开

EP0375457A2 Cyclic ether derivatives 失效
标题翻译：环醚衍生物。
公开(公告)号：EP0375457A2
公开(公告)日：1990-06-27
申请号：EP89313521.0
申请日：1989-12-22
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , ICI-PHARMA
发明人： Hammon, Annie
IPC分类号： C07D317/22 , A61K31/335
CPC分类号： C07D405/04 , C07D317/22 , C07D327/04
摘要： The invention concerns a cyclic ether derivative of the formula I
wherein Ar¹ is optionally substituted phenyl or naphthyl;
A¹ is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo-(3-6C)alkylene;
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-X-A³- wherein each of A² and A³ is (1-6C)alkylene and X is oxy, thio, sulphinyl, sulphonyl or imino; and
R³ is (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl or substituted (1-4C)alkyl;
or a pharmaceutically-acceptable salt thereof.
The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.

70. 发明公开

EP0269298A3 Cephalosporins, process for their preparation and pharmaceutical compositions 失效
标题翻译： CEPHALOSPORINS，其制备和药物组合物的方法
公开(公告)号：EP0269298A3
公开(公告)日：1989-11-29
申请号：EP87309852.9
申请日：1987-11-06
申请人： ICI PHARMA
发明人： Bertrandie, Alain Michel , Bird, Thomas Geoffrey Colerick , Jung, Frederic Henry
IPC分类号： C07D501/46 , C07D501/36 , C07D501/34 , C07D501/20 , A61K31/545 , C07D501/56
CPC分类号： A61K31/545
摘要： Cephalosporin compounds having a 3-position substituent of the formula (I) are described:
-CH₂-Y-Q (I)
wherein Y is a bond or a linking group -NR⁴-Yʹ-, -O-Yʹ-, -S-Yʹ- wherein R⁴ is hydrogen, various optionally substituted alkyl groups, alkenyl, alkanoyl or alkanesulphonyl, and Yʹ is a bond or various optionally substituted alkylene groups; and Q is a benzene ring (optionally fused to a further benzene ring so forming a naphthyl group or optionally fused to a 5 or 6 membered heterocyclic aromatic group containing 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur), said benzene ring being substituted by groups R¹ and R² which are ortho with respect to one another, wherein R¹ is hydroxy or an in vivo hydrolysable ester thereof and R² is hydroxy, an in vivo hydrolysable ester thereof, carboxy, sulpho, hydroxymethyl, methanesulphonamido or ureido; or Q is a group of the formula (II) or (III):
wherein M is oxygen or a group NR³
wherein R³ is hydrogen or C 1-4 alkyl; ring Q being further optionally substituted. The use of such compounds as antibacterial agents is described as are processes for their preparation and intermediates therefor.

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