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1. 发明授权

EP0462813B1 Bicyclic pyran derivatives and their use as inhibitors of 5-lipoxygenase 失效转让
标题翻译：双环吡喃衍生物及其作为5-脂氧合酶抑制剂的用途。
公开(公告)号：EP0462813B1
公开(公告)日：1995-10-25
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

2. 发明授权

EP0341990B1 Cephalosporins, process for their preparation and pharmaceutical compositions 有权
标题翻译：头孢菌素类，其制备方法和药物制剂。
公开(公告)号：EP0341990B1
公开(公告)日：1994-11-09
申请号：EP89304704.3
申请日：1989-05-09
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , ICI PHARMA
发明人： Siret, Patrice Jean , Jung, Frederick Henri , Bell, William
IPC分类号： C07D501/46 , A61K31/545
CPC分类号： C07D501/00

3. 发明授权

EP0304158B1 Cephalosporins, processes for their preparation and pharmaceutical compositions containing them 失效
标题翻译：头孢菌素类，它们的制备方法和含有它们的药物组合物。
公开(公告)号：EP0304158B1
公开(公告)日：1994-06-22
申请号：EP88306420.6
申请日：1988-07-13
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , ICI PHARMA
发明人： Arnould, Jean Claude , Jung, Frederick Henri , Boucherot, Dominique , Strawson, Colin John , Davies, David Huw
IPC分类号： C07D501/46 , C07D501/40
CPC分类号： C07D501/46 , C07D501/40

4. 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

5. 发明授权

EP0381375B1 Heterocyclic derivatives 失效
标题翻译：杂环衍生物
公开(公告)号：EP0381375B1
公开(公告)日：1992-11-11
申请号：EP90300780.5
申请日：1990-01-25
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , ICI PHARMA
发明人： Crawley, Graham Charles , Edwards, Martin Paul
IPC分类号： C07D417/12 , A61K31/435 , A61K31/495
CPC分类号： C07D417/12

6. 发明公开

EP0485111A2 The use of lipoxygenase and cyclooxygenase inhibitors as synergistic agents 失效
标题翻译：使用脂氧合酶和环氧合酶抑制剂作为协同剂
公开(公告)号：EP0485111A2
公开(公告)日：1992-05-13
申请号：EP91310059.0
申请日：1991-10-31
申请人： ZENECA LIMITED , ICI PHARMA
发明人： Foster, Stephen John
IPC分类号： A61K31/535 , A61K31/47 , A61K31/35
CPC分类号： A61K31/35 , A61K31/47 , A61K31/535 , A61K31/405 , A61K31/195 , A61K31/19 , A61K2300/00
摘要： The invention relates to synergistic agents for the treatment of inflammatory or arthritic conditions which comprise one of a selected group of inhibitors of the enzyme 5-lipoxygenase in conjunction or admixture with an inhibitor of the enzyme cyclooxygenase. Conveniently the 5-lipoxygenase inhibitor is, for example, 6-[(3-fluoro-5-[4-methoxy-3,4,5,6-tetrahydro-2 H -pyran-4-yl]phenoxy)methyl]-1-methyl-2-quinolone or 4-[5-fluoro-3-(4-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-7-ylthio)phenyl]-4-methoxytetrahydropyran and the cyclooxygenase inhibitor is selected from indomethacin, flurbiprofen and diclofenac. The invention also relates to a pharmaceutical composition containing said synergistic agent and to the use of said agent in the manufacture of a medicament for the synergistic treatment of inflammatory or arthritic disease.
摘要翻译：本发明涉及用于治疗炎性或关节炎病症的协同剂，其包含选择的5-脂氧合酶抑制剂中的一种与酶环加氧酶的抑制剂结合或混合。方便地，5-脂肪氧合酶抑制剂是例如6 - [（3-氟-5- [4-甲氧基-3,4,5,6-四氢-2H-吡喃-4-基]苯氧基）甲基] -1 2-甲基-2-喹啉酮或4- [5-氟-3-（4-甲基-3-氧代-2,3-二氢-4H-1,4-苯并恶嗪-7-基硫基）苯基] -4-甲氧基四氢吡喃和环加氧酶抑制剂选自吲哚美辛，氟比洛芬和双氯芬酸。本发明还涉及含有所述增效剂的药物组合物以及所述试剂在制备用于协同治疗炎症或关节炎疾病的药物中的用途。

7. 发明公开

EP0375452A3 Cycloalkane derivatives 失效
标题翻译：环烷基衍生物
公开(公告)号：EP0375452A3
公开(公告)日：1991-12-27
申请号：EP89313493.2
申请日：1989-12-21
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , ICI-PHARMA
发明人： Girodeau, Jean-Marc Marie Maurice
IPC分类号： C07C43/21 , A61K31/085 , C07C43/225 , C07C43/23 , C07C255/16
CPC分类号： C07C255/16 , C07C17/14 , C07C17/361 , C07C43/21 , C07C43/225 , C07C43/23 , C07C45/59 , C07C49/753 , C07C25/22
摘要： The invention concerns a cycloalkane 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 is hydrogen, (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;
or a pharmaceutically-acceptable salt thereof. The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.

8. 发明公开

EP0420511A3 Heterocyclic derivatives 失效转让
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.

9. 发明公开

EP0341990A3 Cephalosporins, process for their preparation and pharmaceutical compositions 有权
标题翻译： CEPHALOSPORINS，其制备和药物组合物的方法
公开(公告)号：EP0341990A3
公开(公告)日：1991-05-15
申请号：EP89304704.3
申请日：1989-05-09
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , ICI PHARMA
发明人： Siret, Patrice Jean , Jung, Frederick Henri , Bell, William
IPC分类号： C07D501/46 , A61K31/545
CPC分类号： C07D501/00
摘要： Cephalosporin antibiotics having a 3-position substituent of the formula:
are described, wherein R¹ is hydrogen or certain optionally substituted alkyl groups; X is a benzene ring or certain 5 or 6-membered heterocyclic ring and is fused to ring Y which is a nitrogen containing heteroaryl group; R² and R³ are independently hydroxy or an in vivo hydrolysable ester thereof, and ring system X-Y is optionally substituted. Processes for their preparation and use are described.

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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