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1. 发明申请

WO2010142956A3 AROYLTHIOUREA AND ARYLTHIOCARBONYLUREA DERIVATIVES 审中-公开
标题翻译：阿魏酸和亚油酸衍生物
公开(公告)号：WO2010142956A3
公开(公告)日：2011-01-27
申请号：PCT/GB2010001136
申请日：2010-06-09
申请人： UNIV DUNDEE , UNIV ST ANDREWS , LAIN SONIA , WESTWOOD NICHOLAS JAMES , LANE DAVID PHILIP
发明人： LAIN SONIA , WESTWOOD NICHOLAS JAMES , LANE DAVID PHILIP
IPC分类号： C07C335/26 , A61K31/17 , A61P3/04 , A61P3/10 , A61P25/16 , A61P31/18 , A61P33/06 , A61P35/00 , C07C327/54
CPC分类号： C07C335/26 , C07C327/54
摘要： The invention provides compounds according to formula (I): (wherein X, Y, Z1 R1, R2, R3, Ar and Ar' are as dedfined herein), and physiologically acceptable salts, solvates, esters or amides thereof, pharmaceutical compositions comprising these compounds and the compounds for use in medicine, for example for the treatment or prophylaxis of diseases involving cell proliferation, such as cancer, and for the treatment or prophylaxis of other diseases.
摘要翻译：本发明提供了根据式（I）的化合物：其中X，Y，Z 1 R 1，R 2，R 3，Ar和Ar'如本文所述）和其生理上可接受的盐，溶剂合物，酯或酰胺，包含这些化合物和用于医药的化合物，例如用于治疗或预防涉及细胞增殖的疾病，例如癌症，以及用于治疗或预防其它疾病。

2. 发明申请

WO2005121096A3 A MULTICORE INDAZOLINONE LIBRARY 审中-公开
标题翻译：多米诺帝山地图书馆
公开(公告)号：WO2005121096A3
公开(公告)日：2006-11-23
申请号：PCT/GB2005002230
申请日：2005-06-08
申请人： UNIV ST ANDREWS , WESTWOOD NICHOLAS JAMES , ISAMBERT NICOLAS STANISLAS JEA
发明人： WESTWOOD NICHOLAS JAMES , ISAMBERT NICOLAS STANISLAS JEA
IPC分类号： C07D231/00 , C07D231/56
CPC分类号： C07D231/56
摘要： There is provided a method to convert O-functionalized indazolinone-derivatives to the corresponding N2-functinoalised indazolinone derivatives, by use of microwave energy or a transition metal catalyst. A preferred catalyst is palladium tetrakis. The method described allows the creation of a library of chemical compounds which can be screened for biological activity.
摘要翻译：提供了通过使用微波能量或过渡金属催化剂将O-官能化的吲唑啉酮衍生物转化成相应的N2-功能化吲哚啉酮衍生物的方法。优选的催化剂是四钯。所描述的方法允许创建可以筛选生物活性的化合物文库。

3. 发明申请

WO2010038043A1 PYRIMIDE DERIVATIVES AND THEIR PHARMACEUTICAL USE 审中-公开
标题翻译：吡嗪衍生物及其药物用途
公开(公告)号：WO2010038043A1
公开(公告)日：2010-04-08
申请号：PCT/GB2009/002367
申请日：2009-10-02
申请人： THE UNIVERSITY COURT OF THE UNIVERSITY OF DUNDEE , THE UNIVERSITY COURT OF THE UNIVERSITY OF ST ANDREWS , WESTWOOD, Nicholas, James , LAIN, Sonia , MEDDA, Federico
发明人： WESTWOOD, Nicholas, James , LAIN, Sonia , MEDDA, Federico
IPC分类号： C07D239/54 , C07D239/56 , A61P35/00
CPC分类号： C07D239/54 , C07D239/56
摘要： The invention provides a compound according to formula (I): wherein: X is O or S; Y is O or S; each Ar and Ar' is independently a mono-, bi- or tricyclic aryl or heteroaryl group optionally substituted with one or more substituents selected from halo, alkyl, aryl, heteroaryl, hydroxyl, nitro, amino, alkoxy, alkylthio, cyano, thio, ester, acyl and amido; each R 2 is independently hydrogen, halo, alkyl, aryl, heteroaryl, hydroxyl, nitro, amino, alkoxy, alkylthio, cyano and thio; and R 1 is as defined herein, or a physiologically acceptable salt, solvate, ester, amide or other physiologically functional derivative thereof.
摘要翻译：本发明提供式（I）化合物：其中：X为O或S; Y为O或S; 每个Ar和Ar'独立地是任选被一个或多个选自卤素，烷基，芳基，杂芳基，羟基，硝基，氨基，烷氧基，烷硫基，氰基，硫代，酯，酰基和酰氨基; 每个R 2独立地是氢，卤素，烷基，芳基，杂芳基，羟基，硝基，氨基，烷氧基，烷硫基，氰基和硫代; 和R1如本文所定义，或其生理学上可接受的盐，溶剂化物，酯，酰胺或其它生理功能衍生物。

4. 发明申请

WO2010013011A1 P53 TUMOR SUPPRESSOR PROTEIN ACTIVATING 审中-公开
标题翻译： P53肿瘤抑制蛋白激活
公开(公告)号：WO2010013011A1
公开(公告)日：2010-02-04
申请号：PCT/GB2009/001884
申请日：2009-07-30
申请人： UNIVERSITY COURT OF THE UNIVERSITY OF DUNDEE , UNIVERSITY COURT OF THE UNIVERSITY OF ST ANDREWS , WESTWOOD, Nicholas, James , LAIN, Sonia , HOLLICK, Jonathan, James , LANE, David, Philip
发明人： WESTWOOD, Nicholas, James , LAIN, Sonia , HOLLICK, Jonathan, James , LANE, David, Philip
IPC分类号： C07D207/06 , A61K31/381 , A61P35/00
CPC分类号： C07D207/34
摘要： The invention provides a compound of formula (I), wherein X, L 1-4 and R 1-4 are as defined herein, with the proviso that the compound is not (i) 4-benzoyl-3,5-dimethyl-1 H -pyrrole-2-carboxylic acid ethyl ester; (ii) 4-(2,5-difluorobenzoyl)-3,5-dimethyl-1 H -pyrrole-2-carboxylic acid ethyl ester); (iii) 4-acetyl-3,5-dimethyl-1 H -pyrrole-2-carboxylic acid ethyl ester; or (iv) 4-(3-dimethylamino-acryloyl)-3,5-dimethyl-1 H -pyrrole-2-carboxylic acid ethyl ester, or a pharmaceutically acceptable derivative thereof.
摘要翻译：本发明提供式（I）化合物，其中X，L1-4和R1-4如本文所定义，条件是该化合物不是（i）4-苯甲酰基-3,5-二甲基-1H-吡咯 -2-羧酸乙酯; （ii）4-（2,5-二氟苯甲酰基）-3,5-二甲基-1H-吡咯-2-甲酸乙酯）; （iii）4-乙酰基-3,5-二甲基-1H-吡咯-2-甲酸乙酯; 或（iv）4-（3-二甲基氨基 - 丙烯酰基）-3,5-二甲基-1H-吡咯-2-甲酸乙酯或其药学上可接受的衍生物。

5. 发明申请

WO2005005430A3 PROCESS FOR THE PREPARATION OF FUROPYRROLES 审中-公开
标题翻译：制备氟化物的方法
公开(公告)号：WO2005005430A3
公开(公告)日：2005-06-16
申请号：PCT/EP2004051259
申请日：2004-06-28
申请人： CIBA SC HOLDING AG , RIGGS RICHARD LEWIS , WESTWOOD NICHOLAS JAMES , SMITH DAVID MACDONALD , MORTON COLIN
发明人： RIGGS RICHARD LEWIS , WESTWOOD NICHOLAS JAMES , SMITH DAVID MACDONALD , MORTON COLIN
IPC分类号： C07D487/04 , C07D491/04 , C07D491/048
CPC分类号： C07D487/04 , C07D491/04
摘要： The present invention relates to a process for the preparation of furopyrroles of the general formula (I), comprising (a) heating a compound of the formula (II) under microwave irradiation optionally in the presence of an inert solvent, wherein A and A are Cl-C18alkyl, C2-Cl8alkenyl, C2-Cl8alkynyl, C5-C8cycloalkyl, C5- C8cycloalkenyl, aryl or heteroaryl, A is hydrogen, C1-C18alkyl, cyanomethyl, Ar ,-CR R -(CH2 )m -Ar or Y- R , wherein R and R independently of each other stand for hydrogen or C1-C4alkyl, or phenyl which can be substituted up to three times with C1-C4alkyl, Ar stands for aryl, C5-C8 cloalkyl, C5-C8 cycloalkenyl or heteroaryl, which can be substituted one to three times with C1-C8alkyl, C1-C8alkoxy, halogen or phenyl, which can be substituted with C1-C8alkyI or C1-C8alkoxy one to three times, and m stands for 0, 1, 2, 3 or 4, R is C1-C18alkyl, in particular C1-C4alkyl, aryl, in particular phenyl, or aralkyl, in particular benzyl, which can be substituted one to three times with C1-C8alkyl, C1-C8alkoxy, or halogen, Y is -C(O)-, -C(O)O-, -C(O)NH-, -SO2NH- or -SO2- and R is C1-Cl8alkyl, Ar , or aralkyl. The furopyrroles of the general formula (I) can be obtained in high yield and high purity by the process of the present invention.
摘要翻译：本发明涉及一种制备通式（I）的呋喃并吡咯的方法，其包括（a）在微波辐射下任选地在惰性溶剂存在下加热式（II）化合物，其中A 1，和A 2是C 1 -C 18烷基，C 2 -C 18烯基，C 2 -C 18炔基，C 5 -C 8环烷基，C 5 -C 8环烯基，芳基或杂芳基，A 3是氢，C 1 -C 18烷基，氰甲基，Ar 3， R 31 - （CH 2）m -Ar 3或Y-R 32，其中R 30和R 31彼此独立地代表氢或C 1 -C 4烷基或可以被C 1 -C 4烷基取代三次的苯基，Ar 3代表芳基，C 5 -C 8烷基，C 5 -C 8环烯基或杂芳基，其可以被C 1 -C 8烷基，C 1 -C 8烷基取代一至三次 C 1-8烷氧基，卤素或苯基，其可以被C 1 -C 8烷基或C 1 -C 8烷氧基取代一至三次，m代表0,1,2,3或4，R是C 1 -C 18烷基，特别是C 1 -C 4烷基，芳基，特别是苯基或芳烷基，特别是苄基，可以用C 1 -C 8烷基，C 1 -C 8烷氧基或卤素取代一至三次，Y是-C（O） - ， - C（O）O-，-C（O）NH-，-SO 2 NH-或 - SO 2 - 和R 32是C 1 -C 8烷基，Ar 3或芳烷基。通过本发明的方法可以高产率和高纯度获得通式（I）的呋喃并吡咯。

6. 发明申请

WO2005005430A2 PROCESS FOR THE PREPARATION OF FUROPYRROLES 审中-公开
标题翻译：制备呋喃甲醇的方法
公开(公告)号：WO2005005430A2
公开(公告)日：2005-01-20
申请号：PCT/EP2004/051259
申请日：2004-06-28
申请人： CIBA SPECIALTY CHEMICALS HOLDING INC. , RIGGS, Richard Lewis , WESTWOOD, Nicholas James , SMITH, David Macdonald , MORTON, Colin
发明人： RIGGS, Richard Lewis , WESTWOOD, Nicholas James , SMITH, David Macdonald , MORTON, Colin
IPC分类号： C07D491/00
CPC分类号： C07D487/04 , C07D491/04
摘要： The present invention relates to a process for the preparation of furopyrroles of the general formula (I), comprising (a) heating a compound of the formula (II) under microwave irradiation optionally in the presence of an inert solvent, wherein A 1 and A 2 are C l -C 18 alkyl, C 2 -C l8 alkenyl, C 2 -C l8 alkynyl, C 5 -C 8 cycloalkyl, C 5- C 8 cycloalkenyl, aryl or heteroaryl, A 3 is hydrogen, C 1 -C 18 alkyl, cyanomethyl, Ar 3 ,-CR 30 R 31 -(CH 2 ) m -Ar 3 or Y- R 32 , wherein R 30 and R 31 independently of each other stand for hydrogen or C 1 -C 4 alkyl, or phenyl which can be substituted up to three times with C 1 -C 4 alkyl, Ar 3 stands for aryl, C 5 -C 8 cloalkyl, C 5 -C 8 cycloalkenyl or heteroaryl, which can be substituted one to three times with C 1 -C 8 alkyl, C 1 -C 8 alkoxy, halogen or phenyl, which can be substituted with C 1 -C 8 alkyI or C 1 -C 8 alkoxy one to three times, and m stands for 0, 1, 2, 3 or 4, R is C 1 -C 18 alkyl, in particular C 1 -C 4 alkyl, aryl, in particular phenyl, or aralkyl, in particular benzyl, which can be substituted one to three times with C 1 -C 8 alkyl, C 1 -C 8 alkoxy, or halogen, Y is -C(O)-, -C(O)O-, -C(O)NH-, -SO 2 NH- or -SO 2 - and R 32 is C 1 -C l8 alkyl, Ar 3 , or aralkyl. The furopyrroles of the general formula (I) can be obtained in high yield and high purity by the process of the present invention.
摘要翻译：本发明涉及制备通式（I）呋喃并呋喃的方法，其包括（a）在微波辐射下任选地在存在下式（II）的情况下加热式惰性溶剂，其中A 1和A 2是C 1 -C 18烷基，C≡2 -C≡C8烯基，C≡C12炔基，C≡C-sub C8-C8环烯基，芳基或杂芳基，A 3是氢，C 1 -C 8环烷基，C 5 -C 8环烯基，芳基或杂芳基，A 3是氢，C≡1 C18烷基，氰甲基，Ar 3，-CR 30 R 31 - （CH 3） - ， - CH 2），或者Y-R <32>，或者Y-R <32> 其中R 30和R 31彼此独立地代表氢或C 1 -C 4 - / - ，其中R 30和R 31彼此独立地代表氢或C 1 -C 4 - 烷基或可被C 1 -C 4烷基取代至多三次的苯基，Ar 3代表芳基，C 1 -C 4烷基，低于5-C 8 cloa C 1 -C 8 - 环烯基或杂芳基，其可以被C 1 -C 8取代1-3次， C 1-8烷基，C 1 -C 8烷氧基，卤素或可被C 1 -C 8取代的苯基烷基或C 1 -C 8烷氧基取代1-3次，m代表0,1,2,3或4，R是C

7. 发明申请

WO2008029096A8 P53 ACTIVATING BENZOYL UREA AND BENZOYL THIOUREA COMPOUNDS 审中-公开
标题翻译： P53活化苯甲酰脲和苯甲酰硫脲化合物
公开(公告)号：WO2008029096A8
公开(公告)日：2008-08-14
申请号：PCT/GB2007003302
申请日：2007-09-04
申请人： UNIV DUNDEE , UNIV ST ANDREWS , LAIN SONIA , LANE DAVID PHILLIP , STARK MICHAEL JOHN RAYMOND , MCCARTHY ANNA ROSE , HOLLICK JONATHAN JAMES , WESTWOOD NICHOLAS JAMES
发明人： LAIN SONIA , LANE DAVID PHILLIP , STARK MICHAEL JOHN RAYMOND , MCCARTHY ANNA ROSE , HOLLICK JONATHAN JAMES , WESTWOOD NICHOLAS JAMES
IPC分类号： A61K31/17
CPC分类号： C07D295/155 , C07C275/54 , C07C335/26 , C07D295/15
摘要： The present invention relates to compounds which acivate the p53 response, and find use in, for example, hyperproliferative diseases such as cancer treatment and potentially other diseases/conditions (involving sirtuin function).
摘要翻译：本发明涉及激活p53应答的化合物，并且可用于例如过度增殖性疾病如癌症治疗和潜在的其他疾病/病症（涉及瑟土因功能）。

8. 发明申请

WO2005121096A2 A MULTICORE CHEMICAL COMPOUND LIBRARY 审中-公开
标题翻译：多元化学化合物图书馆
公开(公告)号：WO2005121096A2
公开(公告)日：2005-12-22
申请号：PCT/GB2005/002230
申请日：2005-06-08
申请人： THE UNIVERSITY COURT OF THE UNIVERSITY OF ST ANDREWS , WESTWOOD, Nicholas, James , ISAMBERT, Nicolas, Stanislas, Jean
发明人： WESTWOOD, Nicholas, James , ISAMBERT, Nicolas, Stanislas, Jean
IPC分类号： C07D231/00
CPC分类号： C07D231/56
摘要： There is provided a method to convert O-functionalized indazolinone-derivatives to the corresponding N2-functinoalised indazolinone derivatives, by use of microwave energy or a transition metal catalyst. A preferred catalyst is palladium tetrakis. The method described allows the creation of a library of chemical compounds which can be screened for biological activity.
摘要翻译：提供了通过使用微波能量或过渡金属催化剂将O-官能化的吲唑啉酮衍生物转化成相应的N2-功能化吲哚啉酮衍生物的方法。优选的催化剂是四钯。所描述的方法允许创建可以筛选生物活性的化合物文库。

9. 发明申请

WO2010142956A2 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2010142956A2
公开(公告)日：2010-12-16
申请号：PCT/GB2010/001136
申请日：2010-06-09
申请人： UNIVERSITY COURT OF THE UNIVERSITY OF DUNDEE , UNIVERSITY COURT OF THE UNIVERSITY OF ST ANDREWS , LAIN, Sonia , WESTWOOD, Nicholas, James , LANE, David, Philip
发明人： LAIN, Sonia , WESTWOOD, Nicholas, James , LANE, David, Philip
IPC分类号： C07C335/26
CPC分类号： C07C335/26 , C07C327/54
摘要： The invention provides compounds according to formula (I): (wherein X, Y, Z1 R1, R2, R3, Ar and Ar' are as dedfined herein), and physiologically acceptable salts, solvates, esters or amides thereof, pharmaceutical compositions comprising these compounds and the compounds for use in medicine, for example for the treatment or prophylaxis of diseases involving cell proliferation, such as cancer, and for the treatment or prophylaxis of other diseases.
摘要翻译：本发明提供了根据式（I）的化合物：其中X，Y，Z 1 R 1，R 2，R 3，Ar和Ar'如本文所述）和其生理上可接受的盐，溶剂合物，酯或酰胺，包含这些化合物和用于医药的化合物，例如用于治疗或预防涉及细胞增殖的疾病，例如癌症，以及用于治疗或预防其它疾病。

10. 发明申请

WO2008029096A3 P53 ACTIVATING BENZOYL UREA AND BENZOYL THIOUREA COMPOUNDS 审中-公开
公开(公告)号：WO2008029096A3
公开(公告)日：2008-03-13
申请号：PCT/GB2007/003302
申请日：2007-09-04
申请人： UNIVERSITY COURT OF THE UNIVERSITY OF DUNDEE , UNIVERSITY COURT OF THE UNIVERSITY OF ST. ANDREWS , LAIN, Sonia , LANE, David, Phillip , STARK, Michael, John, Raymond , MCCARTHY, Anna, Rose , HOLLICK, Jonathan, James , WESTWOOD, Nicholas, James
发明人： LAIN, Sonia , LANE, David, Phillip , STARK, Michael, John, Raymond , MCCARTHY, Anna, Rose , HOLLICK, Jonathan, James , WESTWOOD, Nicholas, James
IPC分类号： A61K31/17
摘要： The present invention relates to compounds which acivate the p53 response, and find use in, for example, hyperproliferative diseases such as cancer treatment and potentially other diseases/conditions (involving sirtuin function).

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