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1. 发明授权

US5478843A Thiazole derivatives 失效
标题翻译：噻唑衍生物
公开(公告)号：US5478843A
公开(公告)日：1995-12-26
申请号：US277890
申请日：1994-07-20
申请人： Thomas G. C. Bird
发明人： Thomas G. C. Bird
IPC分类号： C07D417/14 , C07D215/227 , A61K31/47 , C07D215/36 , C07D417/12
CPC分类号： C07D417/14
摘要： The invention concerns a thiazole derivative of the formula I ##STR1## wherein Q is 2-oxo-1,2,3,4-tetrahydroquinolin-6-yl or 2-oxo-1,2-dihydroquinolin-6-yl which bears on the nitrogen atom at the 1-position a (1-4C)alkyl substituent;X.sup.1 is thio, sulphinyl or sulphonyl;Ar is thiazolediyl;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which together with the carbon atom to which A.sup.2 and A.sup.3 are attached define a ring having 5 or 6 ring atoms, wherein A.sup.2 and A.sup.3, which may be the same or different, each is (1-3C)alkylene and X.sup.2 is oxy, and which ring may bear one or two (1-4C)alkyl substituents;or a pharmaceutically-acceptable salt thereof;processes for their preparation; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
摘要翻译：本发明涉及式I的噻唑衍生物，其中Q是2-氧代-1,2,3,4-四氢喹啉-6-基或2-氧代-1,2-二氢喹啉-6-基，其中带有在1-位上的氮原子a（1-4C）烷基取代基; X1是硫代，亚磺酰基或磺酰基; Ar是噻唑二基; R1是（1-4C）烷基，（3-4C）烯基或（3-4C）炔基; 并且R2和R3一起形成式-A2-X2-A3-的基团，其与A2和A3所连接的碳原子一起定义为具有5或6个环原子的环，其中A2和A3可以是相同或不同，各自为（1-3C）亚烷基，X2为氧基，并且该环可以带有一个或两个（1-4C）烷基取代基; 或其药学上可接受的盐; 其准备过程; 含有它们的药物组合物及其作为5-脂肪氧合酶抑制剂的用途。

2. 发明授权

US5217978A Substituted-optionally hydrogenated isoquinoline compounds, pharmaceutical compositions and pharmaceutical method of use 失效
标题翻译：取代的氢化异喹啉化合物，药物组合物和药物使用方法
公开(公告)号：US5217978A
公开(公告)日：1993-06-08
申请号：US717505
申请日：1991-06-19
申请人： Thomas G. C. Bird
发明人： Thomas G. C. Bird
IPC分类号： A61K31/35 , A61K31/015 , A61K31/341 , A61K31/38 , A61K31/47 , A61K31/535 , A61P11/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07D307/64 , C07D333/34 , C07D407/04 , C07D407/06 , C07D409/04 , C07D409/06 , C07D409/14 , C07D413/14 , C07D419/12
CPC分类号： C07D407/04 , C07D409/04 , C07D409/14 , C07D413/14
摘要： The invention concerns a heterocyclene derivative of the formula I ##STR1## wherein Ar.sup.1 is optionally substituted phenyl, naphthyl or a 9- or 10-membered bicyclic heterocyclic moiety;A.sup.1 is a direct link to X.sup.1 or (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar.sup.2 is optionally substituted 5-membered heterocyclene moiety;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl; or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.

3. 发明授权

US5089513A 5-lipoxygenase inhibitory thiazoles 失效
标题翻译： 5-LIPOXYGENASE抑制剂THIAZOLES
公开(公告)号：US5089513A
公开(公告)日：1992-02-18
申请号：US378163
申请日：1989-07-11
申请人： Thomas G. C. Bird , Graham C. Crawley , Martin P. Edwards , Philip N. Edwards , Jean-Marc M. M. Girodeau , John F. Kingston
发明人： Thomas G. C. Bird , Graham C. Crawley , Martin P. Edwards , Philip N. Edwards , Jean-Marc M. M. Girodeau , John F. Kingston
IPC分类号： C12N9/99 , A61K31/425 , A61K31/426 , A61K31/44 , A61P29/00 , A61P37/08 , A61P43/00 , C07D277/24 , C07D417/06
CPC分类号： C07D417/06 , C07D277/24
摘要： The invention concerns a thiazole of the formula I, ##STR1## wherein Ar.sup.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.sup.2 is optionally substituted phenylene, or a 6-membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 is hydrogen, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl or substituted (1-4C)alkyl;R.sup.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.

4. 发明授权

US5008258A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5008258A
公开(公告)日：1991-04-16
申请号：US221945
申请日：1988-07-18
申请人： Thomas G. C. Bird , Frederick H. Jung
发明人： Thomas G. C. Bird , Frederick H. Jung
IPC分类号： C07D501/56 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/04 , C07D501/46 , C07D501/48
CPC分类号： C07D501/46
摘要： Cephalosporin compounds having as a 3-substituent the group: ##STR1## wherein Y represents a bond, optionally substituted alkylene or --CH.sub.2 CH.sub.2 NHCO--, P is a benzene ring substituted by groups W and Z ortho with respect to one another wherein W is hydroxy or an in vivo hydrolyzable ester thereof, Z is hydroxy, an in vivo hydrolyzable ester thereof, carboxy, sulpho, hydroxymethyl, --NHSO.sub.2 CH.sub.3 or NHCONH.sub.2, Q is a mono- or bicyclic ring system substituted by R.sup.7 wherein R.sup.7 is hydrogen or a range of groups and ring Q is optionally further substituted; are described as antibacterial agents. Processes for their preparation and their methods of use are described.

5. 发明授权

US5137913A Diaryl ether cyclic ethers 失效
标题翻译：二芳基醚环醚
公开(公告)号：US5137913A
公开(公告)日：1992-08-11
申请号：US806775
申请日：1991-12-12
申请人： Thomas G. C. Bird , Philip N. Edwards
发明人： Thomas G. C. Bird , Philip N. Edwards
IPC分类号： A61K31/075 , A61K31/335 , A61K31/357 , A61K31/44 , A61P29/00 , A61P37/08 , A61P43/00 , C07D20060101 , C07D317/22
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, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl or naphthyl;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is optionally substituted phenylene, or a 6-membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 and R.sup.2 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- wherein each of A.sup.2 and A.sup.3 is (1-4C) alkylene and X.sup.2 is oxy, thio, sulphinyl, sulphonyl or imino; andR.sup.3 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; X1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; R1和R2一起形成式-A2-X2-A3-的基团，其中A2和A3各自为（1-4C）亚烷基，X2为氧基，硫基，亚磺酰基，磺酰基或亚氨基; （1-6C）烷基，（2-6C）烯基，（2-6C）炔基和取代的（1-4C）烷基。本发明还涉及制备式I的二芳基醚环醚或其药学上可接受的盐的方法和含有所述环醚的药物组合物。本发明的化合物是5-脂氧合酶的抑制剂。

6. 发明授权

US5126365A Bicyclic derivatives 失效
标题翻译：双相衍生物
公开(公告)号：US5126365A
公开(公告)日：1992-06-30
申请号：US557103
申请日：1990-07-25
申请人： Thomas G. C. Bird , John F. Kingston , David Waterson
发明人： Thomas G. C. Bird , John F. Kingston , David Waterson
IPC分类号： C07D405/04 , A61K31/335 , A61K31/38 , A61K31/40 , A61K31/443 , A61K31/4433 , A61K31/445 , A61P1/04 , A61P29/00 , A61P37/08 , A61P43/00 , C07D317/46 , C07D407/04 , C07D409/04
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, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl or naphthyl; R.sup.1 if (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.1 --X--A.sup.2 ---, wherein each of A.sup.1 and A.sup.2 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.

7. 发明授权

US5114933A Cephalosporin compounds 失效
标题翻译： CEPHALOSPORIN化合物
公开(公告)号：US5114933A
公开(公告)日：1992-05-19
申请号：US124213
申请日：1987-11-23
申请人： Alain M. Bertrandie , Thomas G. C. Bird , Frederic H. Jung
发明人： Alain M. Bertrandie , Thomas G. C. Bird , Frederic H. Jung
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D463/00 , C07D501/22 , C07D501/24 , C07D501/34 , C07D501/46 , C07D501/57 , C07D507/04 , C07D507/06 , C07D507/08
CPC分类号： A61K31/545
摘要： Cephalosporin compounds having a 3-position substituent of the formula (I) are described:--CH.sub.2 --Y--Q (I)wherein Y is a bond or a linking group --NR.sup.4 --Y'--, --O--Y'--, 13 S--Y'-- wherein R.sup.4 is hydrogen, various optionally substituted alkyl groups, alkenyl, alkanoyl or alkanesulphonyl, and Y' 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 R.sup.1 and R.sup.2 which are ortho with respect to one another, wherein R.sup.1 is hydroxy or an in vivo hydrolyzable ester thereof and R.sup.2 is hydroxy, and in vivo hydrolyzable ester thereof, carboxy, sulpho, hydroxymethyl, methanesulphonamido or ureido; or Q is a group of the formula (II) or (III): ##STR1## wherein M is oxygen or a group NR.sup.3 wherein R.sup.3 is hydrogen or C.sub.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.
摘要翻译：描述了具有式（I）的3-位取代基的头孢菌素化合物：其中Y是一个键的-CH 2 -YQ（I）或连接基-NR4-Y'，-Y-Y'，13 S- Y'-其中R 4是氢，各种任选取代的烷基，烯基，烷酰基或烷磺酰基，Y'是一个键或各种任选取代的亚烷基; 并且Q是苯环（任选地与另外的苯环稠合形成萘基或任选地与含有1,2或3个选自氮，氧和硫的杂原子的5或6元杂环芳族基团稠合），所述苯环其中R 1为羟基或其体内可水解的酯，R2为羟基，其体内可水解的酯，羧基，磺基，羟基甲基，甲磺酰氨基或脲基的基团R 1和R 2取代; 或Q是式（II）或（III）的基团：其中M是氧或NR 3，其中R 3是氢或C 1-4烷基; 环Q进一步任选被取代。这些化合物作为抗菌剂的使用被描述为它们的制备方法及其中间体。

8. 发明授权

US5484805A Heterocyclene derivatives 失效
标题翻译：杂环衍生物
公开(公告)号：US5484805A
公开(公告)日：1996-01-16
申请号：US271912
申请日：1994-07-08
申请人： Thomas G. C. Bird
发明人： Thomas G. C. Bird
IPC分类号： A61K31/35 , A61K31/015 , A61K31/341 , A61K31/38 , A61K31/47 , A61K31/535 , A61P11/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07D307/64 , C07D333/34 , C07D407/04 , C07D407/06 , C07D409/04 , C07D409/06 , C07D409/14 , C07D413/14 , C07D419/12 , A61K31/40 , C07D207/36 , C07D207/42
CPC分类号： C07D407/04 , C07D409/04 , C07D409/14 , C07D413/14
摘要： The invention concerns a heterocyclene derivative of the formula I ##STR1## wherein Ar.sup.1 is optionally substituted phenyl, naphthyl or a 9- or 10-membered bicyclic heterocyclic moiety;A.sup.1 is a direct link to X.sup.1 or (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar.sup.2 is optionally substituted 5-membered heterocyclene moiety;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sub.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.
摘要翻译：本发明涉及式I的杂环烯衍生物，其中Ar 1是任选取代的苯基，萘基或9-或10-元双环杂环部分; A1是与X1或（1-3C）亚烷基的直接键; X1是氧基，硫基，亚磺酰基，磺酰基或亚氨基; Ar 2是任选取代的5元杂环烯部分; R1是（1-4C）烷基，（3-4C）烯基或（3-4C）炔基; 并且R2和R3一起形成式-A2-X2-A3-的基团，其与A2和A3所连接的碳原子一起定义为具有5至7个环原子的环，其中A2和A3各自为（1-3C）亚烷基，X 2为氧基，硫基，亚磺酰基或磺酰基; 或其药学上可接受的盐。本发明的化合物是5-脂氧合酶的抑制剂。

9. 发明授权

US5478842A Ether derivatives having 5-lipoxygenase inhibitory activity 失效
标题翻译：具有5-脂氧合酶抑制活性的醚衍生物
公开(公告)号：US5478842A
公开(公告)日：1995-12-26
申请号：US234148
申请日：1994-04-28
申请人： Thomas G. C. Bird , Graham C. Crawley , Michael S. Large , Patrick Ple
发明人： Thomas G. C. Bird , Graham C. Crawley , Michael S. Large , Patrick Ple
IPC分类号： A61K31/40 , A61K31/47 , A61K31/55 , A61P11/00 , A61P17/00 , A61P29/00 , A61P37/08 , C07D405/12 , C07D409/14 , C07D417/14 , C07D493/08 , C07D405/14
CPC分类号： C07D405/12 , C07D409/14 , C07D417/14 , C07D493/08
摘要： The invention concerns ether derivatives of the formula IQ.sup.1 --X--Ar--Q.sup.2 IwhereinQ.sup.1 is an optionally substituted 9-, 10- or 11-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;X is oxy, thio, sulphinyl or sulphonyl;Ar is optionally substituted phenylene, pyridinediyl, pyrimidinediyl, thiophenediyl, furandiyl, thiazolediyl, oxazoiediyl, thiadiazoiediyl or oxadiazolediyl; andQ.sup.2 is selected from the groups of the formulae II and III: ##STR1## wherein R.sup.1 is hydrogen, (2-5C)alkanoyl or optionally substituted benzoyl;R.sup.2 is (1-4C)alkyl; andR.sup.3 is hydrogen or (1-4C)alkyl;or R.sup.2 and R.sup.3 are linked to form a methylene, vinylene, ethylene or trimethylene group;or a pharmaceutically-acceptable salt thereof;processes for their preparation; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
摘要翻译：本发明涉及式I Q1-X-Ar-Q2I的醚衍生物，其中Q1是含有一个或两个氮杂原子的任选取代的9,10或11元双环杂环部分，并任选地含有另外的选自氮，氧和硫; X是氧基，硫基，亚磺酰基或磺酰基; Ar是任选取代的亚苯基，吡啶二基，嘧啶二基，噻吩二基，呋喃二基，噻唑二基，恶唑二基，噻二唑基或恶二唑二基。并且Q2选自式II和III的基团：其中R 1是氢，（2-5C）烷酰基或任选取代的苯甲酰基; R2是（1-4C）烷基; 并且R 3是氢或（1-4C）烷基; 或R 2和R 3连接形成亚甲基，亚乙烯基，亚乙基或三亚甲基; 或其药学上可接受的盐; 其准备过程; 含有它们的药物组合物及其作为5-脂肪氧合酶抑制剂的用途。

10. 发明授权

US5332757A Oxime derivatives 失效
标题翻译：肟衍生物
公开(公告)号：US5332757A
公开(公告)日：1994-07-26
申请号：US14564
申请日：1993-02-08
申请人： Thomas G. C. Bird , Patrick Ple
发明人： Thomas G. C. Bird , Patrick Ple
IPC分类号： A61K31/425 , A61K31/505 , A61P29/00 , A61P37/08 , A61P43/00 , C07D239/42 , C07D307/20 , C07D309/08 , C07D309/10 , C07D317/22 , C07D405/04 , C07D409/02 , C07D409/04 , C07D409/12 , C07D417/04 , C07D417/12 , A61K31/35 , A61K31/34
CPC分类号： C07D405/04 , C07D307/20 , C07D309/10 , C07D317/22 , C07D409/04 , C07D417/04
摘要： The invention concerns oxime derivatives of the formula I ##STR1## wherein R.sup.4 includes hydrogen, carboxy, carbamoyl, amino, cyano, trifluoromethyl, (1-4C)alkylamino, di-(1-4C)alkylamino and (1-4C)alkyl;R.sup.5 includes hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, (2-5C)alkanoyl, halogeno-(2-4C)alkyl and hydroxy-(2-4C)alkyl;Ar.sup.1 is phenylene or a heteroaryl diradical;A.sup.1 is a direct link to X.sup.1, or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene or a heteroaryl diradical;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula -A.sup.2 -X.sup.2 -A.sup.3 - which together with the carbon atom to which A.sup.2 and A.sup.3 are attached define a ring having 5 or 6 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl, sulphonyl or imino;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
摘要翻译：本发明涉及式I的肟衍生物，其中R 4包括氢，羧基，氨基甲酰基，氨基，氰基，三氟甲基，（1-4C）烷基氨基，二（1-4C）烷基氨基和（1-4C）烷基 ; R5包括氢，（1-4C）烷基，（3-4C）烯基，（3-4C）炔基，（2-5C）烷酰基，卤代 - （2-4C）烷基和羟基 - （2-4C）烷基; Ar1是亚苯基或杂芳基双基; A1是直接连接到X1，或A1是（1-4C）亚烷基; X1是氧基，硫基，亚磺酰基或磺酰基; Ar 2是亚苯基或杂芳基双基; R1是（1-4C）烷基，（3-4C）烯基或（3-4C）炔基; 并且R2和R3一起形成式-A2-X2-A3-的基团，其与A2和A3所连接的碳原子一起形成具有5或6个环原子的环，其中A2和A3各自为（1 -3C）亚烷基，X 2为氧基，硫基，亚磺酰基，磺酰基或亚氨基; 或其药学上可接受的盐; 制造过程; 含有它们的药物组合物及其作为5-脂肪氧合酶抑制剂的用途。

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