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1. 发明申请

WO2003029248A1 N-(4-(4-METHYLTHIAZOL-5-YL) PYRIMIDIN-2-YL) -N-PHENYLAMINES AS ANTIPROLIFERATIVE COMPOUNDS 审中-公开
标题翻译： N-（4-（4-甲基噻唑-5-基）吡啶基-2-YL）-N-苯甲酰胺作为抗生素化合物
公开(公告)号：WO2003029248A1
公开(公告)日：2003-04-10
申请号：PCT/GB2002/004383
申请日：2002-09-27
申请人： CYCLACEL LIMITED , WANG, Shudong , MEADES, Christopher , WOOD, Gavin , OSNOWSKI, Andrew , FISCHER, Peter, Martin
发明人： WANG, Shudong , MEADES, Christopher , WOOD, Gavin , OSNOWSKI, Andrew , FISCHER, Peter, Martin
IPC分类号： C07D417/04
CPC分类号： C07D417/04
摘要： The present invention relates to 2-substituted 4-heteroaryl-pyrimidines, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders such as cancer, leukaemia, psoriasis and the like.
摘要翻译：本发明涉及2-取代的4-杂芳基嘧啶，其制备方法，含有它们的药物组合物及其作为细胞周期蛋白依赖性激酶（CDK）抑制剂的用途，因此可用于治疗增殖性疾病如癌症，白血病，牛皮癣等。

2. 发明申请

WO2009118567A3 PYRIMIDINES, TRIAZINES AND THEIR USE AS KINASE INHIBITORS 审中-公开
标题翻译：哌嗪，三氮唑及其作为激酶抑制剂使用
公开(公告)号：WO2009118567A3
公开(公告)日：2010-03-11
申请号：PCT/GB2009050298
申请日：2009-03-26
申请人： UNIV NOTTINGHAM , WANG SHUDONG , SHI SHENHUA , ZAYTSEV ANDREY , FISCHER PETER MARTIN
发明人： WANG SHUDONG , SHI SHENHUA , ZAYTSEV ANDREY , FISCHER PETER MARTIN
IPC分类号： C07D251/18 , A61K31/506 , A61K31/53 , A61P35/00 , C07D417/04
CPC分类号： C07D417/04 , C07D251/18
摘要： A compound of formula (I) and its pharmaceutically acceptable salts or solvates and physiologically hydrolysable, solubilising or immobilisable derivatives wherein: Ar is a 5-membered heteroaryl ring wherein X1 and X2 are one or two heteroatoms or Ar is a 6-membered aromatic ring, wherein heteroatoms are selected from S, O, N, Se; Z is NH, NHCO, NHSO2, N-alkyl, CH2NH, CH2N-alkyl, CH2, CH2CH2, CH=CH, CH2CONH, SO2, or SO; Y is N or CR3; R1, R2, R5, R6, R7, R8 and R9 are each independently H, or a substituent; R3, when present, is selected from alkyl and a substituent, with the proviso that when Y is CR3, Ar is a 5- membered heterocycle comprising one or two N heteroatoms and Z is NH, then R3 is selected from C3+ alkyl and a substituent; R4 is selected from H, alkyl and R13 as hereinbefore defined, with the proviso that when R3 is absent, R4 is selected from alkyl and a substituent; processes for the preparation thereof, intermediates and precursors therefore and the use thereof as a medicament, and therapeutic compositions comprising the compound.
摘要翻译：式（I）化合物及其药学上可接受的盐或溶剂化物和生理上可水解，增溶或可固化的衍生物，其中：Ar是5元杂芳基环，其中X 1和X 2是一个或两个杂原子或Ar是6-元芳环其中杂原子选自S，O，N，Se; Z是NH，NHCO，NHSO 2，N-烷基，CH 2 NH，CH 2 N-烷基，CH 2，CH 2 CH 2，CH = CH，CH 2 CONH，SO 2或SO; Y为N或CR 3; R1，R2，R5，R6，R7，R8和R9各自独立地为H或取代基; 当存在时，R3选自烷基和取代基，条件是当Y为CR 3时，Ar为包含一个或两个N个杂原子且Z为NH的5-元杂环，则R3选自C3 +烷基和取代基 ; R 4选自如上文所定义的H，烷基和R 13，条件是当R 3不存在时，R 4选自烷基和取代基; 因此，其制备方法，中间体和前体及其作为药物的用途，以及包含该化合物的治疗组合物。

3. 发明申请

WO2004005278A1 BISARYLSULFONAMIDE COMPOUNDS AND THEIR USE IN CANCER THERAPY 审中-公开
标题翻译： BISARYLSULFONAMIDE化合物及其在癌症治疗中的应用
公开(公告)号：WO2004005278A1
公开(公告)日：2004-01-15
申请号：PCT/GB2003/002923
申请日：2003-07-07
申请人： CYCLACEL LIMITED , WANG, Shudong , GIBSON, Darren , DUNCAN, Kenneth , BAILEY, Kevin , THOMAS, Mark , MacCALLUM, David , ZHELEVA, Daniella , TURNER, Nicholas, John , FISCHER, Peter, Martin
发明人： WANG, Shudong , GIBSON, Darren , DUNCAN, Kenneth , BAILEY, Kevin , THOMAS, Mark , MacCALLUM, David , ZHELEVA, Daniella , TURNER, Nicholas, John , FISCHER, Peter, Martin
IPC分类号： C07D333/42
CPC分类号： C07D213/70 , A61K31/43 , A61K31/4439 , A61K31/454 , A61K31/5377 , C07C311/21 , C07C311/29 , C07C311/44 , C07D207/34 , C07D207/36 , C07D209/14 , C07D209/16 , C07D213/71 , C07D231/12 , C07D235/30 , C07D263/32 , C07D277/36 , C07D277/56 , C07D285/06 , C07D285/10 , C07D295/185 , C07D319/18 , C07D333/34 , C07D333/42 , C07D333/62 , C07D409/04 , C07D409/12 , C07D413/04 , C07D513/04
摘要： The present invention relates to the use of bisarylsulfonamide compounds of formula (I) wherein W is a C I-5 branched or unbranched alkyl group or a C 2-5 alkenyl group; nis0or1; R 1 is H, a C, 1-8 branched or unbranched alkyl group, a C 2-8 alkenyl group, or an aryl or aralkyl group; Ar 1 is a substituted thienyl, furyl, pyrrolyl, imidazothiazolyl, thiazolyl, pyridyl or phenyl group; and Ar 2 is a substituted phenyl, indolyl or benzoimidazolyl group; in the preparation of a medicament for treating proliferative disorders. Further aspects of the invention relate to compounds of formula (I), pharmaceutical compositions thereof, and an assay for determining binding to HDM2.
摘要翻译：本发明涉及式（I）的双芳基磺酰胺化合物，其中W是C1-5支链或非支链烷基或C2-5烯基; nis0or1; R 1是H，C 1-8支链或非支链烷基，C 2-8烯基或芳基或芳烷基; Ar 1是取代的噻吩基，呋喃基，吡咯基，咪唑并噻唑基，噻唑基，吡啶基或苯基; Ar 2是取代的苯基，吲哚基或苯并咪唑基; 在制备用于治疗增殖性疾病的药物中。本发明的其它方面涉及式（I）化合物，其药物组合物和用于测定与HDM2结合的测定法。

4. 发明申请

WO2002079193A1 INHIBITORS OF CYCLIN DEPENDENT KINASES AS ANTI-CANCER AGENT 审中-公开
标题翻译：作为抗癌剂的CYCLIN依赖性激素的抑制剂
公开(公告)号：WO2002079193A1
公开(公告)日：2002-10-10
申请号：PCT/GB2002/001445
申请日：2002-03-26
申请人： CYCLACEL LIMITED , FISCHER, Peter, Martin , WANG, Shudong , WOOD, Gavin
发明人： FISCHER, Peter, Martin , WANG, Shudong , WOOD, Gavin
IPC分类号： C07D403/04
CPC分类号： C07D403/04
摘要： The present invention relates to 2-substituted 4-heteroaryl-pyrimidines, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferation disorders such as cancer, leukaemia, psoriasis and the like.
摘要翻译：本发明涉及2-取代的4-杂芳基嘧啶，其制备方法，含有它们的药物组合物及其作为细胞周期蛋白依赖性激酶（CDK）抑制剂的用途，因此其用于治疗增殖性疾病如癌症，白血病，牛皮癣等。

5. 发明申请

WO2009118567A2 PYRIMIDINES, TRIAZINES AND THEIR USE AS PHARMACEUTICAL AGENTS 审中-公开
标题翻译：吡咯嗪，三氮唑及其作为药物代用品
公开(公告)号：WO2009118567A2
公开(公告)日：2009-10-01
申请号：PCT/GB2009/050298
申请日：2009-03-26
申请人： THE UNIVERSITY OF NOTTINGHAM , FISCHER, Peter Martin , WANG, Shudong , ZAYTSEV, Andrey
发明人： FISCHER, Peter Martin , WANG, Shudong , ZAYTSEV, Andrey
IPC分类号： C07D251/18 , C07D417/04 , A61K31/506 , A61K31/53 , A61P35/00
CPC分类号： C07D417/04 , C07D251/18
摘要： A compound of formula (I) and its pharmaceutically acceptable salts or solvates and physiologically hydrolysable, solubilising or immobilisable derivatives wherein: Ar is a 5-membered heteroaryl ring wherein X 1 and X 2 are one or two heteroatoms or Ar is a 6-membered aromatic ring, wherein heteroatoms are selected from S, O, N, Se; Z is NH, NHCO, NHSO 2 , N-alkyl, CH 2 NH, CH 2 N-alkyl, CH 2 , CH 2 CH 2 , CH=CH, CH 2 CONH, SO 2 , or SO; Y is N or CR 3 ; R 1 , R 2 , R 5 , R 6 , R 7 , R 8 and R 9 are each independently H, or a substituent; R 3 , when present, is selected from alkyl and a substituent, with the proviso that when Y is CR 3 , Ar is a 5- membered heterocycle comprising one or two N heteroatoms and Z is NH, then R3 is selected from C 3+ alkyl and a substituent; R 4 is selected from H, alkyl and R 13 as hereinbefore defined, with the proviso that when R 3 is absent, R 4 is selected from alkyl and a substituent; processes for the preparation thereof, intermediates and precursors therefore and the use thereof as a medicament, and therapeutic compositions comprising the compound.
摘要翻译：式（I）化合物及其药学上可接受的盐或溶剂化物和生理上可水解，增溶或可固化的衍生物，其中：Ar是5元杂芳基环，其中X 1和X 2是一个或两个杂原子或Ar是6-元芳环其中杂原子选自S，O，N，Se; Z是NH，NHCO，NHSO 2，N-烷基，CH 2 NH，CH 2 N-烷基，CH 2，CH 2 CH 2，CH = CH，CH 2 CONH，SO 2或SO; Y为N或CR 3; R1，R2，R5，R6，R7，R8和R9各自独立地为H或取代基; 当存在时，R3选自烷基和取代基，条件是当Y为CR 3时，Ar为包含一个或两个N个杂原子且Z为NH的5-元杂环，则R3选自C3 +烷基和取代基 ; R 4选自如上文所定义的H，烷基和R 13，条件是当R 3不存在时，R 4选自烷基和取代基; 因此，其制备方法，中间体和前体及其作为药物的用途，以及包含该化合物的治疗组合物。

6. 发明申请

WO1994027627A1 HEMOREGULATORY PEPTIDES 审中-公开
标题翻译： HEMOREGULATORY PHEPTIDES
公开(公告)号：WO1994027627A1
公开(公告)日：1994-12-08
申请号：PCT/US1994005859
申请日：1994-05-24
申请人： SMITHKLINE BEECHAM CORPORATION , BHATNAGAR, Pradip, Kumar , HEERDING, Dirk , FISCHER, Peter, Martin
发明人： SMITHKLINE BEECHAM CORPORATION
IPC分类号： A61K37/00
CPC分类号： C07K5/0821 , A61K38/00 , C07K5/0202 , C07K5/021 , C07K5/06139
摘要： The invention provides compounds of the general formula (I): A -B -X -(CH2)m-(CON(R1))r-(CH2)s-Y -(CH2)s-(N(R1)CO)r-(CH2)n-X -B -A . The compounds of this invention are also illustrated by the formula (II): A -B -X -(CH2)m-(CON(R1))r-(CH2)s-Y -(CH2)s-(N(R1)CO)r-(CH2)n-X -B -A . The compounds of the invention have hemo-regulatory activity and can be used to stimulate haematopoiesis and can also be used for the treatment of certain symptoms caused by or arising out of viral, fungal and bacterial infectious diseases.
摘要翻译：本发明提供通式（I）的化合物：A 1 -B 1 -X 1 - （CH 2）m - （CON（R 1））r - （CH 2）s Y 1 - （CH 2 ）S-（N（R 1）CO）R-（CH 2）NX <1> -B <1> -A <1>。本发明的化合物也用式（II）表示：A 2 -B 2 -X 2 - （CH 2）m - （CON（R 1））r - （CH 2）s Y 2 - （CH 2）S - （N（R 1）CO）R-（CH 2）NX <2> -B <2> -A <2>。本发明的化合物具有血液调节活性并且可用于刺激造血作用，并且还可用于治疗由病毒，真菌和细菌感染性疾病引起或由其引起的某些症状。

7. 发明申请

WO2012004549A1 PHENOXYPROPANOL DERIVATIVES AND THEIR USE IN TREATING CARDIAC AND CARDIOVASCULAR DISEASES 审中-公开
标题翻译：苯氧基丙酸衍生物及其在治疗心脏病和心血管疾病中的应用
公开(公告)号：WO2012004549A1
公开(公告)日：2012-01-12
申请号：PCT/GB2010/051106
申请日：2010-07-05
申请人： THE UNIVERSITY OF NOTTINGHAM , MISTRY, Shailesh , DARAS, Etienne , FROMONT, Christophe , JADHAV, Gopal , FISCHER, Peter Martin , KELLAM, Barrie , HILL, Stephen John , BAKER, Jillian Glenda
发明人： MISTRY, Shailesh , DARAS, Etienne , FROMONT, Christophe , JADHAV, Gopal , FISCHER, Peter Martin , KELLAM, Barrie , HILL, Stephen John , BAKER, Jillian Glenda
IPC分类号： C07C275/40 , C07C275/28 , C07C235/34 , C07C335/20 , A61K31/16 , A61K31/17 , A61P9/04
CPC分类号： C07C217/64 , C07C43/23 , C07C213/08 , C07C217/34 , C07C231/12 , C07C233/40 , C07C233/65 , C07C233/78 , C07C235/34 , C07C235/50 , C07C235/60 , C07C237/04 , C07C237/34 , C07C269/06 , C07C271/28 , C07C273/1854 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/36 , C07C275/40 , C07C275/42 , C07C303/40 , C07C311/13 , C07C335/16 , C07C335/20 , C07C2601/02 , C07C2601/08 , C07D303/24
摘要： A compound of formula I-0, and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: wherein Z 1 is C 1 -C 4 linear or branched alkyl or alkenyl; R 4 is selected from unsubstituted and substituted C 3 -C 8 cycloalkyl, C 1 -C 8 linear or branched alkyl, C 2-5 alkenyl, C 6 -C 10 heteroaryl or aryl, or C 3 -C 8 heterocyclyl which may be part unsaturated, and combinations thereof; is linear C 2-3 alkylene,; X 1 is selected from NH and O; X 2 is selected from unsaturated C and unsaturated S; and X 3 is selected from NH and CH 2 ; or one of X 1 and X 3 is a single bond; or X 1 is O and X 2 and X 3 together are a single bond; and R 7 is selected from oxo, F, Cl, Br, CN, NH 2 , NR 9 2 , NO 2 , CF 3 , OR 9 , COR 9 , OCOR 9 , COOR 9, NR 9 COR 9 , CONR 9 2 SO 2 NR 9 2 , NR 9 SO 2 R 9 ; and R 8 is selected from C 1-5 alkyl, C 1-5 alkoxyl, C 2-5 alkenyl or alkynyl, C 6-10 ) aryl and C 3-8 cycloalkyl and combinations thereof, which may be unsubstituted or f urther substituted by one or more F, Cl, Br, CN, NH 2 , NR 3 2 , NO 2 , CF 3 ; and R 9 is selected from H and a group R 8 as hereinbefore defined; n7 and n8 and the sum thereof are independently selected from zero and the whole number integer 1 to 4; processes for the preparation thereof, compositions and uses.
摘要翻译：式I-0的化合物及其药学上可接受的盐或盐和生理上可水解的游离形式或盐形式的衍生物：其中Z1是C1-C4直链或支链烷基或烯基; R4选自未取代和取代的C 3 -C 8环烷基，C 1 -C 8直链或支链烷基，C 2-5烯基，C 6 -C 10杂芳基或芳基，或可以是部分不饱和的C 3 -C 8杂环基，及其组合; 是直链C 2-3亚烷基; X1选自NH和O; X2选自不饱和C和不饱和S; 并且X 3选自NH和CH 2; 或者X1和X3中的一个是单键; 或X1为O，X2和X3一起为单键; 并且R 7选自氧代，F，Cl，Br，CN，NH 2，NR 9 2，NO 2，CF 3，OR 9，COR 9，OCOR 9，COOR 9，NR 9 COR 9，CONR 9 2 SO 2 NR 9 2，NR 9 SO 2 R 9; 并且R 8选自C 1-5烷基，C 1-5烷氧基，C 2-5烯基或炔基，C 6-10芳基和C 3-8环烷基及其组合，其可未被取代或被一个或多个F， Cl，Br，CN，NH 2，NR 3 2，NO 2，CF 3; 并且R 9选自H和上文定义的基团R 8; n7和n8，它们的和独立地选自零和整数1至4; 制备方法，组合物和用途。

8. 发明申请

WO02079193A8 INHIBITORS OF CYCLIN DEPENDENT KINASES AS ANTI-CANCER AGENT 审中-公开
标题翻译：作为抗癌剂的CYCLIN依赖性激素的抑制剂
公开(公告)号：WO02079193A8
公开(公告)日：2005-03-17
申请号：PCT/GB0201445
申请日：2002-03-26
申请人： CYCLACEL LTD , FISCHER PETER MARTIN , WANG SHUDONG , WOOD GAVIN
发明人： FISCHER PETER MARTIN , WANG SHUDONG , WOOD GAVIN
IPC分类号： A61K31/506 , A61K31/5377 , A61P35/00 , A61P35/02 , A61P43/00 , C07D403/04
CPC分类号： C07D403/04
摘要： The present invention relates to 2-substituted 4-heteroaryl-pyrimidines, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferation disorders such as cancer, leukaemia, psoriasis and the like.
摘要翻译：本发明涉及2-取代的4-杂芳基嘧啶，其制备方法，含有它们的药物组合物及其作为细胞周期蛋白依赖性激酶（CDK）抑制剂的用途，因此可用于治疗增殖性疾病如癌症，白血病，牛皮癣等。

9. 发明申请

WO2006075152A1 4- (1H-INDOL-3-YL) -PYRIMIDIN-2-YLAMINE DERIVATES AND THEIR USE IN THERAPY 审中-公开
标题翻译： 4-（1H-吲哚-3-基） - 嘧啶-2-基]胺衍生物及其在治疗中的用途
公开(公告)号：WO2006075152A1
公开(公告)日：2006-07-20
申请号：PCT/GB2006/000087
申请日：2006-01-11
申请人： CYCLACEL LIMITED , FISCHER, Peter, Martin , WANG, Shudong , MEADES, Christopher, Keith , ANDREWS, Martin, James, Inglis , GIBSON, Darren , DUNCAN, Kenneth
发明人： FISCHER, Peter, Martin , WANG, Shudong , MEADES, Christopher, Keith , ANDREWS, Martin, James, Inglis , GIBSON, Darren , DUNCAN, Kenneth
IPC分类号： C07D401/14 , C07D403/04 , C07D405/14 , A61K31/506 , A61K31/5377 , A61P5/48 , A61P9/00 , A61P9/04 , A61P17/14 , A61P25/00 , A61P29/00 , A61P31/00 , A61P33/00 , A61P35/00
CPC分类号： C07D401/14 , C07D403/04 , C07D405/14
摘要： The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts thereof. The present invention seeks to provide further substituted heteroaryl-substituted pyrimidine derivatives. More specifically, the invention relates to compounds that have broad therapeutic applications in the treatment of a number of different diseases and/or that are capable of inhibiting one or more protein kinases.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐。本发明寻求提供进一步取代的杂芳基取代的嘧啶衍生物。更具体地，本发明涉及在治疗许多不同疾病和/或能够抑制一种或多种蛋白激酶方面具有广泛治疗应用的化合物。

10. 发明申请

WO1997017985A1 HEMOREGULATORY COMPOUNDS 审中-公开
标题翻译：血液循环系统化合物
公开(公告)号：WO1997017985A1
公开(公告)日：1997-05-22
申请号：PCT/US1996018245
申请日：1996-11-12
申请人： SMITHKLINE BEECHAM CORPORATION , NYCOMED IMAGING AS , BHATNAGAR, Pradip, Kumar , FISCHER, Peter, Martin
发明人： SMITHKLINE BEECHAM CORPORATION , NYCOMED IMAGING AS
IPC分类号： A61K38/07
CPC分类号： C07K5/0215 , A61K38/00
摘要： Novel compounds of general formula (I) which have hemoregulatory activities and can be used to stimulate haematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases.
摘要翻译：本发明涉及通式（I）的新型化合物，具有血清活性，可用于刺激血细胞生成和治疗病毒，真菌和细菌感染性疾病。

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