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1. 发明公开

EP2299996A1 5-LIPOXYGENASE INHIBITORS 审中-公开
标题翻译： 5-脂氧合酶抑制剂
公开(公告)号：EP2299996A1
公开(公告)日：2011-03-30
申请号：EP09757254.9
申请日：2009-06-01
申请人： Jackson, William Paul
发明人： Jackson, William Paul
IPC分类号： A61K31/18 , C07C311/21 , A61P35/00
CPC分类号： A61K31/18 , C07C311/21 , C07C311/46
摘要： The use of compounds of the formula (I) Ar
1 -L
1 -Ar
2 -L
2 -C(R
3 )(R
4 )N(OR
1 )C(=Y)-R
2 (I) where Y is selected from O or S; R
1 is H, a salt or readily hydrolysable substituent; R
2 is selected from H or CH
3 , CH
2 F, CF
2 H or CF
3 ; R
3 and R
4 are selected independently from H, C 1-4 alkyl or alkenyl, CF
3 , CH
2 F, CF
2 H and F, with the proviso that if either R
3 or R
4 is H, then the other is not H; L
1 is a linker group; L
2 is a linker group comprising an optionally substituted or unsubstituted unsaturated branched or straight chain alkyl group; Ar
1 is an optionally substituted or unsubstituted aryl or heterocyclic group; and Ar
2 is an optionally substituted or unsubstituted aryl or heterocyclic group, in the treatment of 5-lipoxygenase mediated cancer provide improved therapies due to the effective inhibition of 5- lipoxygenase and long duration of activity in vivo after oral administration.

2. 发明申请

WO2009146871A1 5-LIPOXYGENASE INHIBITORS 审中-公开
标题翻译： 5-LIPOXYGENASE抑制剂
公开(公告)号：WO2009146871A1
公开(公告)日：2009-12-10
申请号：PCT/EP2009/003906
申请日：2009-06-01
申请人： JACKSON, William Paul
发明人： JACKSON, William Paul
IPC分类号： A61K31/18 , C07C311/21 , A61P35/00
CPC分类号： A61K31/18 , C07C311/21 , C07C311/46
摘要： The use of compounds of the formula (I) Ar 1 -L 1 -Ar 2 -L 2 -C(R 3 )(R 4 )N(OR 1 )C(=Y)-R 2 (I) where Y is selected from O or S; R 1 is H, a salt or readily hydrolysable substituent; R 2 is selected from H or CH 3 , CH 2 F, CF 2 H or CF 3 ; R 3 and R 4 are selected independently from H, C 1-4 alkyl or alkenyl, CF 3 , CH 2 F, CF 2 H and F, with the proviso that if either R 3 or R 4 is H, then the other is not H; L 1 is a linker group; L 2 is a linker group comprising an optionally substituted or unsubstituted unsaturated branched or straight chain alkyl group; Ar 1 is an optionally substituted or unsubstituted aryl or heterocyclic group; and Ar 2 is an optionally substituted or unsubstituted aryl or heterocyclic group, in the treatment of 5-lipoxygenase mediated cancer provide improved therapies due to the effective inhibition of 5- lipoxygenase and long duration of activity in vivo after oral administration.
摘要翻译：使用式（I）Ar1-L1-Ar2-L2-C（R3）（R4）N（OR1）C（= Y）-R2（I）的化合物，其中Y选自O或S; R1是H，一种盐或易水解的取代基; R2选自H或CH3，CH2F，CF2H或CF3; R 3和R 4独立地选自H，C 1-4烷基或烯基，CF 3，CH 2 F，CF 2 H和F，条件是如果R 3或R 4是H，则另一个不是H; L1是连接基团; L2是包含任选取代或未取代的不饱和支链或直链烷基的连接基团; Ar 1是任选取代或未取代的芳基或杂环基; 并且Ar2是任选取代或未取代的芳基或杂环基，在5-脂氧合酶介导的癌症的治疗中，由于在口服给药后有效抑制5-脂氧合酶和长时间的活性，提供了改善的疗法。

3. 发明申请

WO1990001929A1 NEW MEDICAL USE 审中-公开
标题翻译：新医疗用途
公开(公告)号：WO1990001929A1
公开(公告)日：1990-03-08
申请号：PCT/GB1989000992
申请日：1989-08-25
申请人： THE WELLCOME FOUNDATION LIMITED , JACKSON, William, Paul , PETTIPHER, Eric, Roy
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： A61K31/19
CPC分类号： A61K31/19 , A61K31/15 , A61K31/16 , A61K31/165 , A61K31/60 , A61K2300/00
摘要： The present invention is concerned with combinations comprising a compound of formula (I): Ar-(L-Ar')q-(X)k-(Y)p-Q, which is a hydroxamic acid aryl derivative and a non-steroidal anti-inflammatory drug.
摘要翻译：本发明涉及包含式（I）的化合物：Ar-（L-Ar'）q-（X）k-（Y）pQ的组合，其是异羟肟酸芳基衍生物和非甾体抗 - 炎性药物。

4. 发明申请

WO1994029311A1 AMINO ACID ESTER OF NUCLEOSIDE ANALOGUES 审中-公开
标题翻译：氨基酸类似物的氨基酸
公开(公告)号：WO1994029311A1
公开(公告)日：1994-12-22
申请号：PCT/GB1994001245
申请日：1994-06-09
申请人： FARMHISPANIA SA , JACKSON, William, Paul
发明人： FARMHISPANIA SA
IPC分类号： C07D473/00
CPC分类号： C07D473/00
摘要： A process for the preparation of an amino acid ester of a nucleoside analogue, said process comprising reacting a nucleoside analogue having an esterifiable hydroxy group in its linear or cyclic ether moiety with a 2-oxa-4-aza-cycloalkane-1,3-dione, which process is economical, quick and simple to perform.
摘要翻译：一种制备核苷类似物的氨基酸酯的方法，所述方法包括使其直链或环状醚部分中具有可酯化羟基的核苷类似物与2-氧杂-4-氮杂 - 环烷烃-1,3- 二酮，哪个过程是经济，快速和简单的执行。

5. 发明申请

WO2008068170A1 HDAC INHIBITORS 审中-公开
标题翻译： HDAC抑制剂
公开(公告)号：WO2008068170A1
公开(公告)日：2008-06-12
申请号：PCT/EP2007/062914
申请日：2007-11-27
申请人： JACKSON, William Paul
发明人： JACKSON, William Paul
IPC分类号： C07C311/21 , A61K31/18 , A61P35/00
CPC分类号： C07C311/21
摘要： The use of compounds of the formula (I): Ar 1 -L 1 -Ar 2 -L 2 -C(R 3 )(R 4 )N(OR 1 )C(=Y)-R 2 where Y is selected from O or S; R 1 is H, a salt or readily hydrolysable substituent; R 2 is selected from H or CH 3 , CH 2 F, CF 2 H or CF 3 ; R 3 and R 4 are selected independently from H, C1-4 alkyl or alkenyl, CF 3 , CH 2 F, CF 2 H and F, with the proviso that if either R 3 or R 4 is H, then the other is not H; L 1 is a linker group; L 2 is a linker group comprising an optionally substituted or unsubstituted unsaturated branched or straight chain alkyl group; Ar 1 is an optionally substituted or unsubstituted aryl or heterocyclic group; and Ar 2 is an optionally substituted or unsubstituted aryl or heterocyclic group, in the treatment of HDAC mediated diseases or diseases provide improved therapies due to the potent inhibition of HDAC and long duration of activity in vivo after oral administration. They are potential useful in diseases in which HDAC has been implicated, e.g. psoriasis, cancer, Alzheimer's disease, Huntington's disease and HIV.
摘要翻译：使用式（I）的化合物：其中R 1，R 2，R 2，R 1，R 2， -C（R ^{3 ）（R ^{4 ）N（OR ^{1 ）C（= Y）-R ^{2 其中Y选自O或S; R 1是H，盐或易水解的取代基; R 2选自H或CH 3，CH 2，F，CF 2 H或CF 3， 3 ; R 3和R 4独立地选自H，C 1-4烷基或链烯基，CF 3，CH 2， F，CF 2 H和F，条件是如果R 3或R 4是H，则另一个不是H ; L 1是连接基团; L 2是包含任选取代或未取代的不饱和支链或直链烷基的连接基团; Ar 1是任选取代或未取代的芳基或杂环基; 和Ar 2是任选取代或未取代的芳基或杂环基，在治疗HDAC介导的疾病或疾病中由于HDAC的有效抑制和口服给药后体内活性长时间而提供改善的疗法。它们对于涉及HDAC的疾病具有潜在的用途。牛皮癣，癌症，阿尔茨海默病，亨廷顿病和艾滋病毒。}}}}

6. 发明申请

WO1987004152A1 NEW ARYL DERIVATIVES 审中-公开
标题翻译：新的ARYL衍生物
公开(公告)号：WO1987004152A1
公开(公告)日：1987-07-16
申请号：PCT/GB1986000791
申请日：1986-12-23
申请人： THE WELLCOME FOUNDATION LTD. , KNEEN, Geoffrey , JACKSON, William, Paul , ISLIP, Peter, John
发明人： THE WELLCOME FOUNDATION LTD.
IPC分类号： C07C83/10
CPC分类号： A61K31/185
摘要： Compounds of formula (I) where k is 0 or 1; one of m and n is 0 and the other is 1; Ar represents a phenyl or a naphthyl group, both of which optionally may be substituted by one or more substituents selected from C1-4 alkyl (which may itself optionally be substituted by one or more halogen atoms), C1-4 alkoxy, halo, nitro, amino, carboxy, C1-4 alkoxycarbonyl and hydroxy; X represents oxygen or sulphur; Y is C1-6 alkylene; and R and R are independently selected from hydrogen and C1-4 alkyl; and salts thereof for use in a method of treatment of the human or animal body by surgery or therapy or of diagnosis practised on the human or animal body have lipoxygenase and cyclooxygenase inhibiting properties.
摘要翻译：其中k为0或1的式（I）化合物; m和n之一是0，另一个是1; Ar表示苯基或萘基，它们都可以被一个或多个选自C 1-4烷基（其本身可任选被一个或多个卤素原子取代），C 1-4烷氧基，卤素，硝基，氨基，羧基，C 1-4烷氧基羰基和羟基; X表示氧或硫; Y是C 1-6亚烷基; R 1和R 2独立地选自氢和C 1-4烷基; 其盐用于通过手术或治疗或在人或动物体上进行的诊断来治疗人或动物体的方法具有脂氧合酶和环氧合酶抑制性质。

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