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1. 发明申请

US20030220495A1 Inhibitors of farnesyl protein transferase 审中-公开
标题翻译：法呢基蛋白转移酶抑制剂
公开(公告)号：US20030220495A1
公开(公告)日：2003-11-27
申请号：US10071098
申请日：2002-02-11
申请人： Zeneca Limited and Zeneca Pharma S.A.
发明人： Francis Thomas Boyle , Gareth Morse Davies , James Michael Wardleworth , Jean-Claude Arnould
IPC分类号： C07D265/30
CPC分类号： C07D233/64 , C07D231/12 , C07D233/56 , C07D249/08
摘要： The present invention relates to inhibitors of ras farnesylation of Formula (1), wherein T is of Formula (1) or (2) or (3), A is aryl or heteroaryl; B is aryl or heteroaryl; X and Y represent hydrogen, or both X and Y can represent a single bond (so as to form a double bond); R1 represents a group of Formula (II) or (III), the group of Formula (II) or Formula (III) (having L or D configuration at the chiral alpha carbon in the corresponding free amino acid); R2 represents hydrogen, aryl or heteroaryl; Z represents a direct bond, methylene, ethylene, vinylene, oxy, nullCH2nullOnull or nullOnullCH2null; and R3nullR4, p and r are as defined in the specification or a pharmaceutically-acceptable salt, prodrug or solvate thereof. Processes for their preparation, their use as therapeutic agents and pharmaceutical compositions containing them. A particular use is in cancer therapy.
摘要翻译：本发明涉及式（1）的ras法呢基化抑制剂，其中T为式（1）或（2）或（3），A为芳基或杂芳基; B是芳基或杂芳基; X和Y表示氢，或者X和Y可以表示单键（从而形成双键）; R 1表示式（II）或（III）的基团，式（II）或式（III）的基团（在相应的游离氨基酸中的手性α碳处具有L或D构型）; R 2表示氢，芳基或杂芳基; Z表示直接键，亚甲基，亚乙基，亚乙烯基，氧基，-CH 2 -O-或-O-CH 2 - ; 和R 3 -R 4，p和r如说明书中所定义或其药学上可接受的盐，前药或溶剂化物。其制备方法，用作治疗剂和含有它们的药物组合物。一个特别的用途是癌症治疗。

2. 发明申请

US20040242574A1 QUINAZOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 有权
标题翻译：喹诺酮衍生物和含有它们的药物组合物
公开(公告)号：US20040242574A1
公开(公告)日：2004-12-02
申请号：US10698388
申请日：2003-11-03
申请人： ZENECA LIMITED , ZENECA PHARMA S.A.
发明人： Andrew Peter Thomas , Craig Johnstone , Edward Clayton , Elaine Sophie Elizabeth Stokes , Jean-Jacques Marcel Lohmann , Laurent Francois Andre Hennequin
IPC分类号： A61K031/541 , A61K031/517 , C07D417/02 , C07D43/02
CPC分类号： C07D401/12 , A61F13/02 , A61F13/023 , A61F2013/00221 , A61F2013/8408 , A61K31/517 , A61K31/541 , C07D239/94 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The invention relates to quinazoline derivatives of formula (I) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or nullNR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl), R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro, X1 represents nullOnull, nullCH2null, nullSnull, nullSOnull, nullSO2null, nullNR7COnull, nullCONR8null, nullSO2NR9null, nullNR10SO2null or nullNR11null (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl); R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or hetrocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group selected from alkyl and a 5 or 6 membered saturated carbocyclic or heterocyclic group, and salts thereof; processes for their preparation, 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. 1
摘要翻译：本发明涉及式（I）的喹唑啉衍生物，其中m为1至2的整数; R 1表示氢，羟基，卤代，硝基，三氟甲基，氰基，C 1-3烷基，C 1-3烷氧基，C 1-3烷硫基或-NR 5 R 6（其中R 5和R 6），其可以相同或不同，各自表示氢或C 1-3烷基），R 2表示氢，羟基，卤代，甲氧基，氨基或硝基; R 3表示羟基，卤代，C 1-3烷基，C 1-3烷氧基，C 1-3烷酰氧基，三氟甲基，氰基，氨基或硝基，X 1表示-O-，-CH 2 - ， - S - ， - SO-， -SO 2 - ，-NR 7 CO - ， - CONR 8 - ， - SO 2 NR 9 - ，-NR 10 SO 2 - 或-NR 11 - （其中R 7，R 8 R 9，R 10和R 11各自独立地表示氢，C 1-3烷基或C 1-3烷氧基C 2-3 - 烷基）; R 4表示任选取代的5或6元饱和碳环或杂环基团或基团，其为烯基，炔基或任选取代的烷基，该烷基可以含有杂原子连接基团，该烯基，炔基或烷基可以携带选自烷基和5或6元饱和碳环或杂环基的末端任选取代的基团及其盐; 其制备方法，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。

3. 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。

4. 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。

5. 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。

6. 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。

7. 发明申请

WO1997032856A1 4-ANILINOQUINAZOLINE DERIVATIVES 审中-公开
标题翻译： 4-苯胺氮杂环丁烷衍生物
公开(公告)号：WO1997032856A1
公开(公告)日：1997-09-12
申请号：PCT/GB1997000550
申请日：1997-02-28
申请人： ZENECA LIMITED , ZENECA PHARMA S.A. , THOMAS, Andrew, Peter , HENNEQUIN, Laurent, François, André , JOHNSTONE, Craig
发明人： ZENECA LIMITED , ZENECA PHARMA S.A.
IPC分类号： C07D239/94
CPC分类号： C07D239/94
摘要： The invention relates to quinazoline derivatives of formula (I) (wherein: R represents hydrogen or methoxy; R represents methoxy, ethoxy, 2-methoxyethoxy, 3-methoxypropoxy, 2-ethoxyethoxy, trifluoromethoxy, 2,2,2-trifluoroethoxy, 2-hydroxyethoxy, 3-hydroxypropoxy, 2-(N,N-dimethylamino)ethoxy, 3-(N,N-dimethylamino)propoxy, 2-morpholinoethoxy, 3-morpholinopropoxy, 4-morpholinobutoxy, 2-piperidinoethoxy, 3-piperidinopropoxy, 4-piperidinobutoxy, 2-(piperazin-1-yl)ethoxy, 3-(piperazin-1-yl)propoxy, 4-(piperazin-1-yl)butoxy, 2-(4-methylpiperazin-1-yl)ethoxy, 3-(4-methylpiperazin-1-yl)propoxy or 4-(4-methylpiperazin-1-yl)butoxy; the phenyl group bearing (R )2 is selected from: 2-fluoro-5-hydroxyphenyl, 4-bromo-2-fluorophenyl, 2,4-difluorophenyl, 4-chloro-2-fluorophenyl, 2-fluoro-4-methylphenyl, 2-fluoro-4-methoxyphenyl, 4-bromo-3-hydroxyphenyl, 4-fluoro-3-hydroxyphenyl, 4-chloro-3-hydroxyphenyl, 3-hydroxy-4-methylphenyl, 3-hydroxy-4-methoxyphenyl and 4-cyano-2-fluorophenyl); 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：R 1表示氢或甲氧基; R 2表示甲氧基，乙氧基，2-甲氧基乙氧基，3-甲氧基丙氧基，2-乙氧基乙氧基，三氟甲氧基， 2-（N，N-二甲基氨基）乙氧基，3-（N，N-二甲氨基）丙氧基，2-吗啉代乙氧基，3-吗啉代丙氧基，4-吗啉代丁氧基，2-哌啶子基乙氧基， 3-哌啶基丁氧基，2-（哌嗪-1-基）乙氧基，3-（哌嗪-1-基）丙氧基，4-（哌嗪-1-基）丁氧基，2-（4-甲基哌嗪-1-基）乙氧基，3-（4-甲基哌嗪-1-基）丙氧基或4-（4-甲基哌嗪-1-基）丁氧基;带有（R 3）2的苯基选自：2-氟-5 4-羟基苯基，4-溴-2-氟苯基，2,4-二氟苯基，4-氯-2-氟苯基，2-氟-4-甲基苯基，2-氟-4-甲氧基苯基，4-溴-3-羟基苯基，4 4-氟-3-羟基苯基，3-羟基-4-甲基苯基，3-羟基-4-甲氧基苯基和4-氰基-2-氟苯基）。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。

8. 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。

9. 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。

10. 发明申请

WO1993019070A1 CARBAPENEM DERIVATIVES AS ANTIBIOTICS AND INTERMEDIATES THEREOF 审中-公开
标题翻译：卡巴因衍生物作为抗生素及其中间体
公开(公告)号：WO1993019070A1
公开(公告)日：1993-09-30
申请号：PCT/GB1993000603
申请日：1993-03-24
申请人： ZENECA LIMITED , ZENECA Pharma S.A. , JUNG, Frédéric, Henri
发明人： ZENECA LIMITED , ZENECA Pharma S.A.
IPC分类号： C07D477/00
CPC分类号： C07D477/20 , C07D409/12 , C07D409/14 , C07F9/568
摘要： The present invention relates to carbapenems and provides a compound of formula (I) wherein: R is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl; R is hydrogen or C1-4alkyl; R is hydrogen or C1-4alkyl; and the thienyl ring is optionally further substituted by one or two substituents selected from halo, cyano, C1-4alkyl, nitro, hydroxy, carboxy, C1-4alkoxy, trifluoromethyl, C1-4alkoxycarbonyl, amino, C1-4alkylamino, di-C1-4alkylamino, sulfonic acid, C1-4alkylS(O)n- (wherein n is 0-2), C1-4alkanoylamino, C1-4alkanoyl(N &cir& _-C1-4alkyl)amino, carbamoyl, C1-4alkylcarbamoyl, di-C1-4alkylcarbamoyl and N &cir& _-C1-4alkanesulfonamido; or by a tetramethylene group attached to adjacent carbon atoms on the thienyl ring; or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them are also described.
摘要翻译：本发明涉及碳青霉烯并提供式（I）化合物，其中：R 1是1-羟乙基，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; 噻吩基环任选被一个或两个选自卤素，氰基，C 1-4烷基，硝基，羟基，羧基，C 1-4烷氧基，三氟甲基，C 1-4烷氧基羰基，氨基，C 1-4烷基氨基，二-C 1-4烷基氨基，磺酸，C 1-4烷基S（O）n-（其中n为0-2），C 1-4烷酰基氨基，C 1-4烷酰基（N 1 -C 1-4烷基）氨基，氨基甲酰基，C 1-4烷基氨基甲酰基，和N和C 1-4烷基磺酰胺基; 或通过连接在噻吩环上相邻碳原子上的四亚甲基; 或其药学上可接受的盐或体内可水解的酯。还描述了其制备方法，其制备中的中间体，它们作为治疗剂的用途和含有它们的药物组合物。

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