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1. 发明申请

WO2004056818A1 OXAZOLIDINONE DERIVATIVES AS ANTIBACTERIAL 审中-公开
标题翻译：氧杂环丁酮衍生物作为抗生素
公开(公告)号：WO2004056818A1
公开(公告)日：2004-07-08
申请号：PCT/GB2003/005457
申请日：2003-12-15
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , GRAVESTOCK, Michael, Barry , HALES, Neil, James , TURNER, Paul
发明人： GRAVESTOCK, Michael, Barry , HALES, Neil, James , TURNER, Paul
IPC分类号： C07D413/14
CPC分类号： C07D413/14
摘要： A compound of the formula (I), or a pharmaceutically-acceptable salt, or in-vivo hydrolysable ester thereof : formula (I), wherein C is selected from D and E, formula (D), formula (E), R 2 a, R 6 a, and R 3 a are independently selected from for example H, CF 3 , Me and Et; R 2 b and R 6 b are independently selected from for example H, F, CF 3 , Me and Et; R 1 b is -X-Z wherein X is O or S and Z is a C-linked 5- or 6-membered heteroaryl ring; R 4 is for example an optionally substituted 5- or 6-membered heterocyclic ring system. Methods for making compounds of the formula (I), compositions containing them and their use as antibacterial agents are also described.
摘要翻译：式（I）化合物或其药学上可接受的盐或其体内可水解的酯：式（I），其中C选自D和E，式（D），式（E），R 2a， R6a和R3a独立地选自例如H，CF3，Me和Et; R2b和R6b独立地选自H，F，CF3，Me和Et; R1b是-X-Z，其中X是O或S，Z是C连接的5或6元杂芳基环; R4是例如任选取代的5元或6元杂环系。还描述了制备式（I）化合物，含有它们的组合物及其作为抗菌剂的用途的方法。

2. 发明申请

WO2004056816A1 ANTIBACTERIAL OXAZOLIDINONES 审中-公开
标题翻译：抗氧化亚油酸
公开(公告)号：WO2004056816A1
公开(公告)日：2004-07-08
申请号：PCT/GB2003/005444
申请日：2003-12-15
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , GRAVESTOCK, Michael, Barry , HALES, Neil, James , TURNER, Paul
发明人： GRAVESTOCK, Michael, Barry , HALES, Neil, James , TURNER, Paul
IPC分类号： C07D413/14
CPC分类号： C07D413/14 , C07D417/14
摘要： A compound of the formula (I), or a pharmaceutically-acceptable salt, or in-vivo hydrolysable ester thereof: formula (I)wherein C is selected from D and E, formula (II) R 2 a, R 6 a, and R 3 a are independently selected from for example H, CF 3 , Me and Et;R 2 b and R 6 b are independently selected from for example H, F, CF 3 , Me and Et; R 1 b is -NRz-Z wherein Rz is for example hydrogen and Z is a 5- or 6-membered heteroaryl ring;R 4 is for example an optionally substituted 5- or 6-membered heterocyclic ring system. Methods for making compounds of the formula (I), compositions containing them and their use as antibacterial agents are also described.
摘要翻译：式（I）化合物或其药学上可接受的盐或其体内可水解的酯：其中C选自D和E的式（I），式（II）R2a，R6a和R3a独立地选自例如H，CF 3，Me和Et; R 2b和R 6b独立地选自例如H，F，CF 3，Me和Et; R1b是-NRz-Z，其中Rz是例如氢，Z是5-或6-元杂芳基环; R4是例如任选取代的5元或6元杂环系。还描述了制备式（I）化合物，含有它们的组合物及其作为抗菌剂的用途的方法。

3. 发明申请

WO2004048392A1 OXAZOLIDINONE AND / OR ISOXAZOLINE DERIVATIVES AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译：氧化氮和/或异恶唑衍生物作为抗菌剂
公开(公告)号：WO2004048392A1
公开(公告)日：2004-06-10
申请号：PCT/GB2003/005087
申请日：2003-11-24
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , CARCANAGUE, Daniel, Robert , GRAVESTOCK, Michael, Barry , HALES, Neil, James , HAUCK, Sheila, Irene , WEBER, Thomas, Peter
发明人： CARCANAGUE, Daniel, Robert , GRAVESTOCK, Michael, Barry , HALES, Neil, James , HAUCK, Sheila, Irene , WEBER, Thomas, Peter
IPC分类号： C07F7/18
CPC分类号： C07D413/14 , C07D413/10 , C07D417/14 , C07F9/653 , C07F9/65583
摘要： A compound of the formula (I), or a pharmaceutically-acceptable salt, or in-vivo hydrolysable ester thereof: formula (I) wherein in (I) C is for example formula (D), formula (E), formula (H) wherein A and B are independently selected from (i) formula (J) and (ii) formula (K) m is 1 or 2; R 2 b and R 6 b, R 2 a and R 6 a, R 3 a and R 5 a, are for example selected from H, F, OMe and Me; R 2 b' and R 6 b', R 2 a' and R 6 a', R 3 a', R 5 a' are for example selected from H, OMe and Me; R 1 a is for example optionally substituted (1-10C)alkyl; R 1 b is for example selected from -NR 5 C(=W)R 4 , formula (a) , or formula (b) wherein HET-1 is for example isoxazolyl and HET-2 is for example triazolyl or tetrazolyl. Methods for making compounds of the formula (I), compositions containing them and their use as antibacterial agents are also described.
摘要翻译：式（I）化合物或其药学上可接受的盐或其体内可水解的酯：式（I）其中（I）中的C为例如式（D），式（E），式）其中A和B独立地选自（i）式（J）和（ii）式（K）中m是1或2; R2b和R6b，R2a和R6a，R3a和R5a例如选自H，F，OMe和Me; R2b'和R6b'，R2a'和R6a'，R3a'，R5a'例如选自H，OMe和Me; R 1a是例如任选取代的（1-10C）烷基; R1b例如选自-NR5C（= W）R4，式（a）或式（b），其中HET-1为例如异恶唑基，HET-2为例如三唑基或四唑基。还描述了制备式（I）化合物，含有它们的组合物及其作为抗菌剂的用途的方法。

4. 发明申请

WO2003022824A1 OXAZOLIDINONE AND/OR ISOXAZOLINE AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译：奥沙利多和/或异山梨醇作为抗菌剂
公开(公告)号：WO2003022824A1
公开(公告)日：2003-03-20
申请号：PCT/GB2002/004120
申请日：2002-09-09
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , GRAVESTOCK, Michael, Barry , HALES, Neil, James , SWAIN, Michael, Lingard , HAUCK, Sheila, Irene , MILLS, Stuart, Dennett
发明人： GRAVESTOCK, Michael, Barry , HALES, Neil, James , SWAIN, Michael, Lingard , HAUCK, Sheila, Irene , MILLS, Stuart, Dennett
IPC分类号： C07D263/24
CPC分类号： C07D263/20 , C07D413/10 , C07D413/14
摘要： Compounds of Formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, and compounds as shown in Formula (I) wherein C is for example (D), (E), (F); wherein A and B are independently selected from (i) and (ii); R 2 a to R 3 b are independently selected from hydrogen and fluorine; R 1 a and R 1 b are independently selected from, for example, hydroxy, -NHC(=W)R 4 , (a) and (b); wherein W is O or S; R 4 is, for example, hydrogen, amino, (1-4C)alkyl; HET-1 is, for example, a C-linked 5-membered heteroaryl ring; HET-2 is, for example, an N-linked 5-membered, fully or partially unsaturated heterocyclic ring; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.
摘要翻译：式（I）化合物或其药学上可接受的盐或其体内可水解的酯，以及其中C为（D），（E），（F）的式（I）所示的化合物。其中A和B独立地选自（i）和（ii）; R2a至R3b独立地选自氢和氟; R1a和R1b独立地选自羟基，-NHC（= W）R4，（a）和（b）; 其中W是O或S; R4是例如氢，氨基，（1-4C）烷基; HET-1是例如C连接的5元杂芳基环; HET-2是例如N-连接的5元全部或部分不饱和杂环; 作为抗菌剂是有用的; 并描述了其制造方法和含有它们的药物组合物。

5. 发明申请

WO2004056819A1 OXAZOLIDINONE DERIVATIVES AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译：作为抗菌剂的奥昔洛芬衍生物
公开(公告)号：WO2004056819A1
公开(公告)日：2004-07-08
申请号：PCT/GB2003/005498
申请日：2003-12-15
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , GRAVESTOCK, Michael, Barry , HALES, Neil, James , RECK, Folkert , ZHOU, Fei
发明人： GRAVESTOCK, Michael, Barry , HALES, Neil, James , RECK, Folkert , ZHOU, Fei
IPC分类号： C07D413/14
CPC分类号： C07D413/14 , C07D413/10
摘要： A compound of the formula (I), or a pharmaceutically-acceptable salt, or in-vivo hydrolysable ester thereof: formula (I) wherein C is selected from D and E, formula (D), formula (E) R 2 a, R 6 a, and R 3 a are independently selected from for example H, CF 3 , Me and Et; R 2 b and R 6 b are independently selected from for example H, F, CF 3 , Me and Et; R 1 b is for example acetamido; R 4 is for example an optionally substituted 5- or 6- membered heterocyclic ring system. Methods for making compounds of the formula (I), compositions containing them and their use as antibacterial agents are also described.
摘要翻译：式（I）化合物或其药学上可接受的盐或其体内可水解的酯：式（I）其中C选自D和E，式（D），式（E）R 2a，R 6a，和R 3a独立地选自例如H，CF 3，Me和Et; R2b和R6b独立地选自H，F，CF3，Me和Et; R1b是例如乙酰氨基; R4是例如任选取代的5-或6-元杂环系统。还描述了制备式（I）化合物，含有它们的组合物及其作为抗菌剂的用途的方法。

6. 发明申请

WO2004048350A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2004048350A2
公开(公告)日：2004-06-10
申请号：PCT/GB2003/005091
申请日：2003-11-24
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , GRAVESTOCK, Michael, Barry , HALES, Neil, James , RECK, Folkert , ZHOU, Fei
发明人： GRAVESTOCK, Michael, Barry , HALES, Neil, James , RECK, Folkert , ZHOU, Fei
IPC分类号： C07D263/00
CPC分类号： C07D413/14
摘要： A compound of the formula (I), or a pharmaceutically-acceptable salt, or in-vivo hydrolysable ester thereof: Wherein C is selected from (D) and (E), R 2 a, R 6 a, and R 3 a ar e independently selected from for example H, CF 3 , Me and Et; R 2 b and R6b are independently selected from for example H,F, CF 3 , Me and Et; R 1 b is for example optionally substituted diazolyl, triazolyl or tetrazolyl; R 4 is for example an optionally substituted 5- or 6-membered heterocyclic ring system. Methods for making compounds of the formula (I), compositions containing them and their use as antibacterial agents are also described.
摘要翻译：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C选自（D）和（E），R 2a，R 6a和R 3a独立地选自例如 H，CF 3，Me和Et; R2b和R6b独立地选自H，F，CF3，Me和Et; R 1b是例如任选取代的二唑基，三唑基或四唑基; R4是例如任选取代的5元或6元杂环系。还描述了制备式（I）化合物，含有它们的组合物及其作为抗菌剂的用途的方法。

7. 发明申请

WO2004083206A1 ANTIBACTERIAL OXALIDINONES 审中-公开
标题翻译：抗氧化剂
公开(公告)号：WO2004083206A1
公开(公告)日：2004-09-30
申请号：PCT/GB2004/001132
申请日：2004-03-16
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , GRAVESTOCK, Michael, Barry , HALES, Neil, James , HAUCK, Sheila, Irene
发明人： GRAVESTOCK, Michael, Barry , HALES, Neil, James , HAUCK, Sheila, Irene
IPC分类号： C07D413/14
CPC分类号： C07D413/14 , C07F9/65583
摘要： Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereo Formula (I): wherein: N-HET is for example triazolyl; Q is for example phenyl or pyridyl, substituted with T; T is for example selected from (TAa1 to TAa12) such as (TAa1) and (TAa5): R 4h , R 5h , R 6h are for example selected from hydrogen, (1-4C)alkyl, (1-4C)alkoxycarbonyl, (1-4C)alkanoyl and carbamoyl; processes for making them, compositions containing them and their use as antibacterial agents are described.
摘要翻译：式（I）化合物或其药学上可接受的盐或体内可水解的酯，其中式（I）：其中：N-HET是例如三唑基; Q为例如苯基或吡啶基，被T取代; T为例如（TAa1〜TAa12），例如（TAa1）和（TAa5）：R 4h，R 5h，R 6h为例如选自氢，（1-4C）烷基，（ 1-4C）烷氧基羰基，（1-4C）烷酰基和氨基甲酰基; 描述了制备它们的方法，含有它们的组合物及其作为抗菌剂的用途。

8. 发明申请

WO2004083205A1 ANTIBACTERIAL 1, 3- OXAZOLIDIN -2- ONE DERIVATIVES 审中-公开
标题翻译：抗真菌剂，3-氧杂环丁烷-2-酮衍生物
公开(公告)号：WO2004083205A1
公开(公告)日：2004-09-30
申请号：PCT/GB2004/001119
申请日：2004-03-16
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , GRAVESTOCK, Michael, Barry , HALES, Neil, James , HAUCK, Sheila, Irene
发明人： GRAVESTOCK, Michael, Barry , HALES, Neil, James , HAUCK, Sheila, Irene
IPC分类号： C07D413/14
CPC分类号： C07D413/14
摘要： Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereof, wherein: N-HET is for example triazolyl substituted with R 1 ; R 1 is for example optionally substituted (1-4C)alkyl; Q is for example phenyl or pyridyl, substituted with T; T is for example selected from (TAa1 to TAa12) such as (TAa1 and TAa5); formula (II): R 4h , R 5h , R 6h are for example selected from hydrogen, (1-4C)alkyl, (1-4C)alkoxycarbonyl, (1-4C)alkanoyl and carbamoyl; processes for making them, compositions containing them and their use as antibacterial agents are described.
摘要翻译：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：N-HET是例如被R 1取代的三唑基; R 1是例如任选取代的（1-4C）烷基; Q为例如苯基或吡啶基，被T取代; T例如选自（TAa1〜TAa12），例如（TAa1和TAa5）; 式（II）：R 4h，R 5h，R 6h是例如选自氢，（1-4C）烷基，（1-4C）烷氧基羰基，（1-4C）烷酰基和氨基甲酰基; 描述了制备它们的方法，含有它们的组合物及其作为抗菌剂的用途。

9. 发明申请

WO2004048370A1 ANTIBACTERIAL COMPOUNDS 审中-公开
标题翻译：抗菌化合物
公开(公告)号：WO2004048370A1
公开(公告)日：2004-06-10
申请号：PCT/GB2003/005082
申请日：2003-11-24
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , GRAVESTOCK, Michael, Barry , HALES, Neil, James
发明人： GRAVESTOCK, Michael, Barry , HALES, Neil, James
IPC分类号： C07D413/14
CPC分类号： C07D413/14 , C07F7/1856
摘要： A compound of the formula (I), or a pharmaceutically-acceptable salt, or in-vivo hydrolysable ester thereof wherein in (I) C is for example formula (D), (E), (H) wherein A and B are independently selected from formulae (i) and (ii) and R 2 b and R 6 b, R 2 b and R 6 a, R 3 a and R 5 a, are for example selected from H, F, OMe and Me; R 2 b’ and R 6 b’, R 2 a’ and R 6 a’, R 3 a’, R 5 a’ are for example selected from H, OMe and Me; R 1 a and R 1 b are for example selected from hydroxy, -OSi(tri-(1-6C)alkyl), NR 5 C(=W) R 4 , formla (a), formula (b) wherein HET-1 is for example isoxazolyl and HET-2 is for example triazolyl or tetrazolyl. Methods for making compounds of the formula (I), compositions containing them and their use as antibacterial agents are also described.
摘要翻译：式（I）化合物或其药学上可接受的盐或其体内可水解的酯，其中在（I）中，C为例如式（D），（E），（H）其中A和B独立地为选自式（ⅰ）和（ⅱ）和R2b和R6b，R2b和R6a，R3a和R5a，例如选自H，F，OMe和Me; R2b'和R6b'，R2a'和R6a'，R3a'，R5a'例如选自H，OMe和Me; R1a和R1b例如选自羟基，-OSi（三（1-6C）烷基），NR5C（= W）R4，formla（a），式（b），其中HET-1是例如异恶唑基和HET- 2是例如三唑基或四唑基。还描述了制备式（I）化合物，含有它们的组合物及其作为抗菌剂的用途的方法。

10. 发明申请

WO2004078753A1 HYDROXYMETHYL SUBSTITUTED DIHYDROISOXAZOLE DERIVATIVES USEFUL AS ANTIBIOTIC AGENTS 审中-公开
标题翻译：用作抗生素的羟甲基取代的二氢吲哚酮衍生物
公开(公告)号：WO2004078753A1
公开(公告)日：2004-09-16
申请号：PCT/GB2004/000730
申请日：2004-02-24
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , GRAVESTOCK, Michael, Barry , HALES, Neil, James , CARCANAGUE, Daniel, Robert
发明人： GRAVESTOCK, Michael, Barry , HALES, Neil, James , CARCANAGUE, Daniel, Robert
IPC分类号： C07D413/14
CPC分类号： C07D413/14
摘要： Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, (I) R1a is NH(C=W)R 5 or (a); W is O or S; R 2 and R 3 are for example H or F; R 1 is for example hydrogen, or halogen; R 5 is selected from hydrogen, (2-6C)alkyl (optionally substituted); R 6 and R 7 are independently selected from hydrogen, and (1-4C)alkyl (optionally substituted); wherein R 4 is either a hydroxymethyl substituent on C-4' of the isoxazoline ring; or R 4 is a hydroxymethyl substituent on C-5' of the isoxazoline ring and the stereochemistry at C-5' of the isoxazoline ring and at C-5 of the oxazolidinone ring is selected, such that the compound of formula (I) is a single diastereomer; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.
摘要翻译：式（I）化合物或其药学上可接受的盐或其体内可水解的酯，（I）R 1a是NH（C = W）R 5或（a）; W为O或S; R2和R3例如为H或F; R1是例如氢或卤素; R5选自氢，（2-6C）烷基（任选取代的）; R6和R7独立地选自氢，和（1-4C）烷基（任选取代的）; 其中R4是异恶唑啉环的C-4'上的羟甲基取代基; 或R4是异恶唑啉环的C-5'上的羟甲基取代基，并且选择异恶唑啉环的C-5'和恶唑烷酮环的C-5的立体化学，使式（I）化合物为单一非对映异构体; 作为抗菌剂是有用的; 并描述了其制造方法和含有它们的药物组合物。

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