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1. 发明申请

WO1994017054A1 OXIME DERIVATIVES 审中-公开
标题翻译： OXIME衍生物
公开(公告)号：WO1994017054A1
公开(公告)日：1994-08-04
申请号：PCT/EP1994000186
申请日：1994-01-25
申请人： ZENECA LIMITED , ZENECA-PHARMA S.A. , LARGE, Michael, Stewart
发明人： ZENECA LIMITED , ZENECA-PHARMA S.A.
IPC分类号： C07D309/10
CPC分类号： C07D409/04 , C07D309/10
摘要： The invention concerns oxime derivatives of formula (I) wherein R includes hydrogen, carboxy, carbamoyl and (1-4C)alkyl; R includes hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, (2-5C)alkanoyl and cyano-(1-4C)alkyl; Ar is optionally-substituted phenylene or a heteroaryl diradical; A is a direct link to X , or A is (1-4C)alkylene; X is oxy, thio, sulphinyl or sulphonyl; Ar includes optionally-substituted phenylene and thiophenediyl; R is hydrogen, (2-5C)alkanoyl or benzoyl; and R and R together form a group of the formula -A -X -A - which together with the carbon atom to which A and A are attached define a ring having 5 or 6 ring atoms, each of A and A is (1-3C)alkylene and X includes oxy; 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，氨基甲酰基和（1-4C）烷基; R 5包括氢，（1-4C）烷基，（3-4C）烯基，（3-4C）炔基，（2-5C）烷酰基和氰基 - （1-4C）烷基; Ar 1是任选取代的亚苯基或杂芳基双基; A 1是与X 1的直接键，或A 1是（1-4C）亚烷基; X 1是氧基，硫基，亚磺酰基或磺酰基; Ar 2包括任选取代的亚苯基和噻吩二基; R 1是氢，（2-5C）烷酰基或苯甲酰基; 并且R 2和R 3一起形成式-A 2 -X 2 -A 3的基团 - 与A 2和A 3的碳原子一起连接的环是具有5或6个环原子的环，A 2和A 3各自为（1-3C）亚烷基且X 2包括氧; 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。

2. 发明申请

WO1998007742A1 SULFONAMIDES 审中-公开
标题翻译：磺胺类药物
公开(公告)号：WO1998007742A1
公开(公告)日：1998-02-26
申请号：PCT/GB1997002222
申请日：1997-08-19
申请人： ZENECA LIMITED , ZENECA-PHARMA S.A. , BARLAAM, Bernard, Christophe
发明人： ZENECA LIMITED , ZENECA-PHARMA S.A.
IPC分类号： C07K05/06
CPC分类号： C07D213/70 , C07C311/19 , C07C311/29 , C07C311/42 , C07C311/46 , C07D209/34 , C07D215/36 , C07D217/02 , C07D233/84 , C07D239/88 , C07D261/10 , C07D271/12 , C07D277/54 , C07D333/34 , C07D409/04
摘要： Compounds of formula (I) wherein R is aryl, heterocyclyl or heteroaryl; R is hydrogen, C1-8alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, heteroaryl, heterocyclyl, arylC1-6alkyl, heteroarylC1-6alkyl, heterocyclylC1-6alkyl or C3-8cycloalkylC1-6alkyl; R is C1-6alkyl, C2-6alkenyl, aryl, C1-6alkyl, heteroarylC1-6alkyl or the side-chain of a naturally occurring amino acid; R is hydrogen, C1-6alkyl, C3-8cycloalkyl, C4-8cycloalkenyl, arylC1-6alkyl, heteroarylC1-6alkyl or heterocyclylC1-6alkyl; R is hydrogen or C1-6alkyl; or R and R together with the nitrogen atom to which they are joined form a heterocyclic ring; wherein any group or ring, in R -R , is optionally substituted; or pharmaceutically acceptable salts or in vivo hydrolysable esters thereof, are described as inhibitors of the production of Tumor Necrosis Factor and/or one or more matrix metalloproteinase enzymes. Compositions containing them and their preparation are also described.
摘要翻译：式（I）的化合物，其中R 1是芳基，杂环基或杂芳基; R 2是氢，C 1-8烷基，C 2-6烯基，C 2-6炔基，C 3-8环烷基，杂芳基，杂环基，芳基C 1-6烷基，杂芳基C 1-6烷基，杂环基C 1-6烷基或C 3-8环烷基C 1-6烷基; R 3是C 1-6烷基，C 2-6烯基，芳基，C 1-6烷基，杂芳基C 1-6烷基或天然存在的氨基酸的侧链; R 4是氢，C 1-6烷基，C 3-8环烷基，C 4-8环烯基，芳基C 1-6烷基，杂芳基C 1-6烷基或杂环基C 1-6烷基; R 5是氢或C 1-6烷基; 或R 4和R 5与它们所连接的氮原子一起形成杂环; 其中R 1 -R 5中的任何基团或环任选被取代; 或其药学上可接受的盐或体内可水解的酯被描述为产生肿瘤坏死因子和/或一种或多种基质金属蛋白酶的抑制剂。还描述了含有它们的组合物及其制备方法。

3. 发明申请

WO1994025453A1 4-ARYL-4-HYDROXY-TETRAHYDROPYRANS AND 3-ARYL-3-HYDROXY-TETRAHYDROFURANS AS 5-LIPOXYGENASE INHIBITORS 审中-公开
标题翻译： 4-亚氨基-4-羟基四氢吡喃酮和3-氰基-3-羟基四氢呋喃作为5-LIPOXYGENASE抑制剂
公开(公告)号：WO1994025453A1
公开(公告)日：1994-11-10
申请号：PCT/EP1994001277
申请日：1994-04-25
申请人： ZENECA LIMITED , ZENECA-PHARMA S.A.
发明人： ZENECA LIMITED , ZENECA-PHARMA S.A. , BIRD, Thomas, Geoffrey, Colerick , CRAWLEY, Graham, Charles , LARGE, Michael, Stewart , PLE, Patrick
IPC分类号： C07D405/12
CPC分类号： C07D405/12 , C07D409/14 , C07D417/14 , C07D493/08
摘要： The invention concerns ether derivatives of the formula (I): Q -X-Ar-Q , wherein Q 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, oxazolediyl, thiadiazolediyl or oxadiazolediyl; and Q is selected from the groups of formulae (II) and (III), wherein R is hydrogen, (2-5C)alkanoyl or optionally substituted benzoyl; R is (1-4C)alkyl; and R is hydrogen or (1-4C)alkyl; or R and R 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）的醚衍生物：Q 1 -X-Ar -Q 2，其中Q 1是任选取代的9,10或11元双环杂环部分，其含有一个或多个两个氮杂原子和任选地含有另外的选自氮，氧和硫的杂原子; 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，噻二唑二基或恶二唑二基。和Q 2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; R 2是（1-4C）烷基; 和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。

4. 发明申请

WO1995004055A1 THIAZOLE DERIVATIVES AS LIPOXYGENASE INHIBITORS 审中-公开
标题翻译：噻唑衍生物作为LIPOXYGENASE抑制剂
公开(公告)号：WO1995004055A1
公开(公告)日：1995-02-09
申请号：PCT/EP1994002408
申请日：1994-07-21
申请人： ZENECA LIMITED , ZENECA-PHARMA S.A.
发明人： ZENECA LIMITED , ZENECA-PHARMA S.A. , BIRD, Thomas, Geoffrey, Colerick
IPC分类号： C07D417/14
CPC分类号： C07D417/14
摘要： The invention concerns a thiazole derivative of formula (I) 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 is thio, sulphinyl or sulphonyl; Ar is thiazolediyl; R is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; and R and R together form a group of the formula -A -X -A - which together with the carbon atom to which A and A are attached define a ring having 5 or 6 ring atoms, wherein A and A , which may be the same or different, each is (1-3C)alkylene and X 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是在氮上的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 1位a（1-4C）烷基取代基的原子; X 1是硫代，亚磺酰基或磺酰基; Ar是噻唑二基; R 1是（1-4C）烷基，（3-4C）烯基或（3-4C）炔基; 并且R 2和R 3一起形成式-A 2 -X 2 -A 3的基团 - 与A 2和A 3的碳原子一起连接的环是具有5或6个环原子的环，其中可以相同或不同的A 2和A 3各自为（1-3C）亚烷基且X 2为氧，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。

5. 发明申请

WO1994029297A1 2-OXO-1,2,3,4-TETRAHYDROQUINOLINE DERIVATIVES 审中-公开
标题翻译： 2-OXO-1,2,3,4-四氢喹啉衍生物
公开(公告)号：WO1994029297A1
公开(公告)日：1994-12-22
申请号：PCT/EP1994001807
申请日：1994-06-03
申请人： ZENECA LIMITED , ZENECA-PHARMA S.A. , BRUNEAU, Pierre, Andre, Raymond , EDWARDS, Philip, Neil
发明人： ZENECA LIMITED , ZENECA-PHARMA S.A.
IPC分类号： C07D405/12
CPC分类号： C07D405/12
摘要： The invention concerns a 2-oxo-1,2,3,4-tetrahydroquinoline derivative of formula (I) wherein Q is 2-oxo-1,2,3,4-tetrahydroquinolin-6-yl which bears on the nitrogen atom at the 1-position a (1-4C)alkyl substituent; X is thio, sulphinyl or sulphonyl; Ar is optionally-substituted 1,3-phenylene; R is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; and R and R together form a group of the formula -A -X -A - which together with the carbon atom to which A and A are attached define a ring having 5 or 6 ring atoms, wherein each of A and A is (1-3C)alkylene and X is oxy; 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2-氧代-1,2,3,4-四氢喹啉衍生物，其中Q是2-氧代-1,2,3,4-四氢喹啉-6-基，其在氮原子上 1位a（1-4C）烷基取代基; X 1是硫代，亚磺酰基或磺酰基; Ar是任选取代的1,3-亚苯基; R 1是（1-4C）烷基，（3-4C）烯基或（3-4C）炔基; 并且R 2和R 3一起形成式-A 2 -X 2 -A 3的基团 - 与A 2和A 3的碳原子一起连接的环是具有5或6个环原子的环，其中A 2和A 3各自为（1-3C）亚烷基且X 2为氧; 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。

6. 发明申请

WO1997022596A1 QUINAZOLINE DERIVATIVES 审中-公开
标题翻译：喹诺酮衍生物
公开(公告)号：WO1997022596A1
公开(公告)日：1997-06-26
申请号：PCT/GB1996003075
申请日：1996-12-13
申请人： ZENECA LIMITED , ZENECA-PHARMA S.A. , LOHMANN, Jean-Jacques, Marcel , HENNEQUIN, Laurent, François, André , THOMAS, Andrew, Peter
发明人： ZENECA LIMITED , ZENECA-PHARMA S.A.
IPC分类号： C07D239/94
CPC分类号： C07D403/12 , C07D239/88 , C07D239/94 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The invention relates to quinazoline derivatives of formula (I) [wherein: Y represents -O-, -S-, -CH2-, -SO-, -SO2-, -NR CO-, -CONR -, -SO2NR -, -NR SO2- or -NR - (wherein R , R , R , R and R each independently represents hydrogen, alkyl or alkoxyalkyl); R represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, alkyl, alkoxy, alkylthio, amino or alkylamino. R represents hydrogen, hydroxy, halogeno, alkyl, alkoxy, trifluoromethyl, cyano, amino or nitro; m is an integer from 1 to 5; R represents hydroxy, halogeno, alkyl, alkoxy, alkanoyloxy, trifluoromethyl, cyano, amino or nitro; R represents a group which is or which contains an optionally substituted pyridone, phenyl or aromatic heterocyclic group] and salts thereof; processes for their preparation and pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.
摘要翻译：本发明涉及式（I）的喹唑啉衍生物[其中：Y 1表示-O - ， - S - ， - CH 2 - ， - SO - ， - SO 2 - ， - NR 5 CO-，-CONR 6 - ， - SO 2 NR 7 - ，-NR 8 SO 2 - 或-NR 9 - （其中R 5，R 6，R 7，R 8和R 9 >各自独立地表示氢，烷基或烷氧基烷基）; R 1表示氢，羟基，卤代，硝基，三氟甲基，氰基，烷基，烷氧基，烷硫基，氨基或烷基氨基。 R 2表示氢，羟基，卤代，烷基，烷氧基，三氟甲基，氰基，氨基或硝基; m为1〜5的整数; R 3表示羟基，卤代，烷基，烷氧基，烷酰氧基，三氟甲基，氰基，氨基或硝基; R 4表示含有任选取代的吡啶酮，苯基或芳族杂环基团的基团及其盐; 其制备方法和含有式（I）化合物或其药学上可接受的盐作为活性成分的药物组合物。式（I）化合物及其药学上可接受的盐抑制VEGF的作用，其在治疗许多疾病状态（包括癌症和类风湿性关节炎）中是有价值的。

7. 发明申请

WO1994029291A1 ANILINE DERIVATIVES 审中-公开
标题翻译：苯胺衍生物
公开(公告)号：WO1994029291A1
公开(公告)日：1994-12-22
申请号：PCT/EP1994001808
申请日：1994-06-03
申请人： ZENECA LIMITED , ZENECA-PHARMA S.A. , EDWARDS, Philip, Neil
发明人： ZENECA LIMITED , ZENECA-PHARMA S.A.
IPC分类号： C07D309/10
CPC分类号： C07D405/12 , C07D309/10
摘要： The invention concerns an aniline derivative of formula (I) wherein R includes hydrogen and (1-4C)alkyl; R includes hydrogen and (1-4C)alkyl; R is hydrogen or (1-4C)alkyl; X includes a group of the formula CR R wherein R is hydrogen or (1-4C)alkyl and R is hydrogen or (1-4C)alkyl; A includes a direct link to X ; X includes thio and sulphonyl; Ar includes phenylene, which may be optionally substituted; R includes hydrogen and (1-4C)alkyl; and R and R together form a ring having 5 to 6 ring atoms including one oxygen atom, and which ring may bear one, two or three substituents, including methyl alpha to the oxygen atom; 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）的苯胺衍生物，其中R 4包括氢和（1-4C）烷基; R 5包括氢和（1-4C）烷基; R 6是氢或（1-4C）烷基; X 3包括式CR 7 R 8的基团，其中R 7是氢或（1-4C）烷基，R 8是氢或（1-4C）烷基; A <1>包括与X <1>的直接链接; X 1包括硫代和磺酰基; Ar包括可以任选取代的亚苯基; R 1包括氢和（1-4C）烷基; 并且R 2和R 3一起形成具有5至6个环原子的环，包括一个氧原子，并且该环可以带有一个，两个或三个取代基，包括氧原子的甲基α; 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。

8. 发明申请

WO1994027999A1 BICYCLIC ETHER DERIVATIVES AND THEIR USE AS 5-LIPOXYGENASE INHIBITORS 审中-公开
标题翻译：双相醚衍生物及其作为5-LIPOXYGENASE抑制剂的用途
公开(公告)号：WO1994027999A1
公开(公告)日：1994-12-08
申请号：PCT/EP1994001805
申请日：1994-06-03
申请人： ZENECA LIMITED , ZENECA-PHARMA S.A. , EDWARDS, Philip, Neil
发明人： ZENECA LIMITED , ZENECA-PHARMA S.A.
IPC分类号： C07D493/08
CPC分类号： C07D495/08
摘要： The invention concerns a bicyclic ether derivative of formula (I), wherein Ar is phenyl or naphthyl, or a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur; A is a direct link to the group X or A is (1-4C)alkylene; X is oxy, thio, sulphinyl or sulphonyl; Ar is phenylene, pyridinediyl, pyrimidinediyl, thiophendiyl, furandiyl or thiazolediyl; and R is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; 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）的双环醚衍生物，其中Ar 1是苯基或萘基，或含有一个或两个氮杂原子并任选地含有另外选自氮，氧和硫的杂原子的10元双环杂环部分 ; A是直接连接到X基团或A是（1-4C）亚烷基; X是氧基，硫基，亚磺酰基或磺酰基; Ar 2是亚苯基，吡啶二基，嘧啶二基，噻吩二基，呋喃二基或噻唑二基; 并且R 1是（1-4C）烷基，（3-4C）烯基或（3-4C）炔基; 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。

9. 发明申请

WO1993015078A1 CARBAPENEMS CONTAINING A CARBOXY SUBSTITUTED PHENYL GROUP, PROCESSES FOR THEIR PREPARATION, INTERMEDIATES AND USE AS ANTIBIOTICS 审中-公开
标题翻译：含有羧基取代苯基的碳水化合物，其制备方法，中间体和用作抗生素
公开(公告)号：WO1993015078A1
公开(公告)日：1993-08-05
申请号：PCT/GB1993000217
申请日：1993-02-02
申请人： ZENECA LIMITED , ZENECA-PHARMA S.A. , BETTS, Michael, John , DAVIES, Gareth, Morse , SWAIN, Michael, Lingard
发明人： ZENECA LIMITED , ZENECA-PHARMA S.A.
IPC分类号： C07D477/00
CPC分类号： C07D477/20 , A61K31/40 , A61K31/407 , A61K31/41 , C07D207/16 , C07D403/12 , C07F9/568
摘要： The present invention relates to carbapenems and provides a compound of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof wherein: R is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl; R is hydrogen or C1-4alkyl; R is hydrogen or C1-4alkyl; R and R are the same or different and are selected from hydrogen, halo, cyano, C1-4alkyl, nitro, hydroxy, carboxy, C1-4alkoxy, C1-4alkoxycarbonyl, aminosulphonyl, C1-4alkylaminosulphonyl, di-C1-4alkylaminosulphonyl, carbamoyl, C1-4alkylcarbamoyl, di-C1-4alkylcarbamoyl, trifluoromethyl, sulphonic acid, amino, C1-4alkylamino, di-C1-4alkylamino, C1-4alkanoylamino, C1-4alkanoyl(N-C1-4alkyl)amino, C1-4alkanesulphonamido and C1-4alkylS(O)n- wherein n is zero, one or two; with the proviso that there is no hydroxy or carboxy substituent in a position ortho to the link to -NR -. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.
摘要翻译：本发明涉及碳青霉烯并提供式（I）化合物或其药学上可接受的盐或体内可水解的酯，其中：R 1是1-羟基乙基，1-氟乙基或羟甲基; R 2是氢或C 1-4烷基; R 3是氢或C 1-4烷基; R 4和R 5相同或不同，选自氢，卤素，氰基，C 1-4烷基，硝基，羟基，羧基，C 1-4烷氧基，C 1-4烷氧基羰基，氨基磺酰基，C 1-4烷基氨基磺酰基， C 1-4烷基氨基磺酰基，氨基甲酰基，C 1-4烷基氨基甲酰基，二-C 1-4烷基氨基甲酰基，三氟甲基，磺酸，氨基，C 1-4烷基氨基，二-C 1-4烷基氨基，C 1-4烷酰基氨基，C 1-4烷酰基（N-C 1-4烷基）氨基，C 1 -4烷基磺酰氨基和C 1-4烷基S（O）n - ，其中n为0，一个或两个; 条件是在与-NR 3 - 的连接相邻的位置处不存在羟基或羧基取代基。其制备方法，制备中的中间体，作为治疗剂的用途和含有它们的药物组合物。

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