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1. 发明申请

WO2006090094A1 PYRIMIDOTHIOPHENE COMPOUNDS FOR USE AS HSP90 INHIBITORS 审中-公开
标题翻译：用作HSP90抑制剂的吡咯烷酮化合物
公开(公告)号：WO2006090094A1
公开(公告)日：2006-08-31
申请号：PCT/GB2005/000736
申请日：2005-02-28
申请人： VERNALIS R & D LTD , BROUGH, Paul, Andrew , BARRIL-ALONSO, Xavier , DRYSDALE, Martin, James
发明人： BROUGH, Paul, Andrew , BARRIL-ALONSO, Xavier , DRYSDALE, Martin, James
IPC分类号： C07D495/04 , A61K31/381 , A61K31/519 , A61P35/00
CPC分类号： C07D495/04
摘要： Certain specific compounds of formula (I) are inhibitors of HSP90 activity in vitro or in vivo, and of use in the treatment of inter alia , cancer: formula (I) wherein R 2 is a group of formula -(Ar 1 ) m -(Alk 1 ) P -(Z) r -(Alk 2 ) S -Q wherein Ar 1 is an optionally substituted aryl or heteroaryl radical, Alk 1 and Alk 2 are optionally substituted divalent C 1 -C 3 alkylene or C 2 -C 3 alkenylene radicals, m, p, r and s are independently 0 or 1, Z is -0-, -S-, -(C=0)-, -(C=S)-, -SO 2 -, -C(=0)O-, -C(=O)NR A - , -C(=S)NR A -, -SO 2 NR A -, -NR A C(=0)-, -NR A SO 2 - or -NR A -wherein R A is hydrogen or C 1 -C 6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R 3 is hydrogen, an optional substituent, or an optionally substituted (C 1 -C 6 )alkyl, aryl or heteroaryl radical; and R 4 is a carboxylic ester, carboxamide or sulfonamide group.
摘要翻译：式（I）的某些特定化合物是体外或体内HSP90活性的抑制剂，并且用于治疗其它癌症：式（I）其中R 2是式 - （AR ^{1 ）_{米 - （ALK ^{1 ）_{P - （Z）_{- [R 和Alk 2是任选取代的二价C 1 -C 3亚烷基或C 2 -C 3亚烷基， 3个亚烯基，m，p，r和s独立地为0或1，Z为-O - ， - S - ， - （C = O） - ， - （C = S） - ， -C（= O）O-，-C（= O）NR A - ， - C（= S）NR A - - ， - SO 2 - ， - NR A - ， - C（= O） - ， - NR A - SO 2 - 或-NR A - 其中R A是氢或C 1 -C 6 Q是氢或任选取代的碳环或杂环基; R 3是氢，任选的取代基或任选取代的（C 1 -C 6 -C 6）烷基，芳基或杂芳基; R 4是羧酸酯，羧酰胺或磺酰胺基。}}}}}

2. 发明申请

WO2006008503A1 PYRIMIDOTHIOPHENE COMPOUNDS 审中-公开
标题翻译：吡咯烷酮化合物
公开(公告)号：WO2006008503A1
公开(公告)日：2006-01-26
申请号：PCT/GB2005/002816
申请日：2005-07-18
申请人： VERNALIS (CAMBRIDGE) LTD , CANCER RESEARCH TECHNOLOGY LTD , THE INSTITUTE OF CANCER RESEARCH , DYMOCK, Brian, William , BARRIL-ALONSO, Xavier , BROUGH, Paul, Andrew , DRYSDALE, Martin, James , WEBB, Paul
发明人： BARRIL-ALONSO, Xavier , BROUGH, Paul, Andrew , DRYSDALE, Martin, James , WEBB, Paul
IPC分类号： C07D495/04 , A61K31/519
CPC分类号： C07D495/04
摘要： Compounds of formula (I) are inhibitors of HSP90, and useful in the treatment of, for example, cancers: Formula (I) wherein R 2 is a group of formula (IA): -(Ar 1 ) m (Alk 1 ) P (Z) r (Alk 2 ) s - Q (1A) wherein in any compatible combination Ar 1 is an optionally substituted aryl or heteroaryl radical, Alk 1 and Alk 2 are optionally substituted divalent C 1 -C 3 alkylene or C 2 -C 3 alkenylene radicals, m, p, r and s are independently 0 or 1, Z is -0-, -S-, -(C=0)-, -(C=S)-, -SO 2 -, -C(=O)O-, -C(=O)NR A - , -C(=S)NR A -, -SO 2 NRA-, -NR A C(=0)-, -NR A S0 2 - or -NR A - wherein R A is hydrogen or C 1 -C 6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R 3 is hydrogen, an optional substituent, or an optionally substituted (C 1 -C 6 )alkyl, aryl or heteroaryl radical; and R 4 is (i) hydrogen, a -CN group, a nitro group -NO 2 , or a - C(=NOH)(NH 2 ) group, or(ii) an optionally substituted C 1 -C 6 alkyl, aryl, heterocyclic, aryl(C 1 -C 6 alkyl)-, or heterocyclic(C 1 -C 6 alkyl)- group, or (iii) a group of formula - C(=0)R 5 wherein R 5 is hydroxyl, optionally substituted C 1 -C 6 alkyl, C 1 -C 6 alkyoxy, aryl, aryloxy, heteroaryl, heteroaryloxy,aryl(C 1 -C 6 alkyl)-, aryl(C 1 -C 6 alkoxy)-, heteroaryl(C 1 -C 6 alkyl)-, or heteroaryl(C 1 -C 6 alkoxy)-, or (iv) a group of formula -C(=O)NHR 6 wherein R 6 is primary, secondary, tertiary or cyclic amino, or hydroxyl, optionally substituted C 1 -C 6 alkyl, C 1 -C 6 alkyoxy, aryl, aryloxy, heteroaryl, heteroaryloxy, aryl(C 1 -C 6 alkyl)-, aryl(C 1 -C 6 alkoxy)-, heteroaryl(C 1 -C 6 alkyl)-, or heteroaryl(C 1 -C 6 alkoxy)-.
摘要翻译：式（I）化合物是HSP90的抑制剂，可用于例如癌症的治疗：式（I）其中R

3. 发明申请

WO2007034185A1 PURINE COMPOUNDS AS HSP90 PROTEIN INHIBITORS FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：作为用于治疗癌症的HSP90蛋白抑制剂的嘌呤化合物
公开(公告)号：WO2007034185A1
公开(公告)日：2007-03-29
申请号：PCT/GB2006/003504
申请日：2006-09-20
申请人： VERNALIS (R & D) Ltd. , CANCER RESEARCH TECHNOLOGY LTD , THE INSTITUTE OF CANCER RESEARCH , BROUGH, Paul , DRYSDALE, Martin , BARRIL-ALONSO, Xavier
发明人： BROUGH, Paul , DRYSDALE, Martin , BARRIL-ALONSO, Xavier
IPC分类号： C07D473/40 , C07D473/36 , C07D473/28 , A61K31/52 , A61P35/00
CPC分类号： C07D473/40 , C07D473/30 , C07D473/36
摘要： Compounds of formula (I) are inhibitors of HSP90, and of utility in the treatment of, for example, cancers: wherein ring A is an aryl or heteroaryl ring or ring system; R 1 is hydrogen, fluoro, chloro, bromo, or a radical of formula (1A): -X-AIk 1 -(Z) m -(Alk 2 ) n -Q (IA) wherein X is a bond, -O-, -S- -S(O)-, -SO 2 -, or -NH-, Z is -O-, -S-, -(C=O)-, -(C=S)-, -S(O)-, -SO 2 -, -NR A -, or, in either orientation -C(=O)O-, -C(=O)NR A -, -C(=S)NR A -, -SO 2 NR A -, -NR A C(=O)-, or -NR A SO 2 - wherein R A is hydrogen or C 1 -C 6 alkyl in which one or more hydrogens is optionally substituted by fluorine; AIk 1 and AIk 2 are optionally substituted divalent C 1 -C 3 alkylene or C 2 -C 3 alkenylene radicals, m and n are independently 0 or 1 , and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R 2 is cyano (-CN), fluoro, chloro, bromo, methyl, ethyl, -OH, -CH 2 OH, -C(=O)NH 2 , -C(=O)H, -C(=O)CH 3 , or -NH 2 ; R 3 and R 4 are independently selected from hydrogen, fluoro, chloro, bromo, cyano (-CN), C 1 C 3 alkyl optionally substituted with one or more fluorine substituents, C 1 C 3 alkoxy optionally substituted with one or more fluorine substituents, -CH=CH 2 , -C=CH, cyclopropyl and -NH 2 , or R 3 and R 4 together represent a carbocyclic or heterocyclic ring fused to ring A, or methylenedioxy (-OCH 2 O-) or ethylenedioxy (-OCH 2 CH 2 O-) in either of which one or more hydrogens are optionally replaced by fluorine; Si is hydrogen, or a substituent as defined in the specification.
摘要翻译：式（I）化合物是HSP90的抑制剂，可用于治疗例如癌症：其中环A是芳基或杂芳基环或环系; R 1是氢，氟，氯，溴或式（1A）的基团：-X-Alk 1 - （Z）m

4. 发明申请

WO2004096212A1 PYRAZOLE COMPOUNDS AS HSP90 INHIBITORS FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：作为HSP90抑制剂治疗癌症的吡唑化合物
公开(公告)号：WO2004096212A1
公开(公告)日：2004-11-11
申请号：PCT/GB2004/001740
申请日：2004-04-23
申请人： VERNALIS (CAMBRIDGE) LIMITED , CANCER RESEARCH TECHNOLOGY LTD , THE INSTITUTE OF CANCER RESEARCH , BARRIL-ALONSO, Xavier , DYMOCK, Brian, William , DRYSDALE, Martin, James
发明人： BARRIL-ALONSO, Xavier , DYMOCK, Brian, William , DRYSDALE, Martin, James
IPC分类号： A61K31/415
CPC分类号： C07K5/06139 , C07D231/14 , C07K5/06191
摘要： Compounds of formula (I) are inhibitors of HSP90 activity, and useful in the treatment of proliferative disease such as cancers: wherein R 1 , R 2 and R 3 are as defined in the specification, and X is -OR 4 or - NR 4 R 5 wherein R 4 and R 5 independently represent hydrogen or optionally substituted C 1 -C 6 alkyl, or R 4 and R 5 taken together with the nitrogen to which they are attached form an optionally substituted nitrogen-containing ring having 5-8 ring atoms.
摘要翻译：式（I）化合物是HSP90活性的抑制剂，可用于治疗增殖性疾病如癌症：其中R1，R2和R3如说明书中所定义，X为-OR4或-NR4R5，其中R4和R5独立地为代表氢或任选取代的C 1 -C 6烷基，或者R 4和R 5与它们所连接的氮一起形成任选取代的具有5-8个环原子的含氮环。

5. 发明申请

WO2005034950A1 PYRIDOTHIOPHENE COMPOUNDS 审中-公开
标题翻译：吡咯烷酮化合物
公开(公告)号：WO2005034950A1
公开(公告)日：2005-04-21
申请号：PCT/GB2004/004216
申请日：2004-10-05
申请人： VERNALIS (CAMBRIDGE) LIMITED , DRYSDALE, Martin, James , DYMOCK, Brian, William , BARRIL-ALONSO, Xavier
发明人： DRYSDALE, Martin, James , DYMOCK, Brian, William , BARRIL-ALONSO, Xavier
IPC分类号： A61K31/4365
CPC分类号： A61K31/4365
摘要： The use of compounds of formula (I) in therapy, particularly for the treatment of a disorder mediated by excessive or inappropriate HSP90 activity formula (I), wherein R 2 is a group of formula (IA): -(Ar l ) m -(Alk l ) p -(Z) r -(Alk 2 ) S -Q (IA) Ar l ,Alk 1 , Z, Alk 2 and Q being as defined in the specification; m, p, r and s are independently 0 or 1; R 3 is hydrogen, an optional substituent, or an optionally substituted (C l -C 6 )alkyl, aryl or heteroaryl radical; and R 4 is a carboxylic ester, carboxamide or sulfonamide group; or a salt, N-oxide, hydrate, or solvate thereof.
摘要翻译：式（I）化合物在治疗中的用途，特别是用于治疗由过量或不适当的HSP90活性式（I）介导的病症，其中R2是式（IA）的基团： - （Ar 1）m - （Alk1）对（Z）r-（Alk 2）SQ（IA）Ar 1，Alk 1，Z，Alk 2和Q如说明书中所定义; m，p，r和s独立地为0或1; R 3是氢，任选的取代基，或任选取代的（C 1 -C 6）烷基，芳基或杂芳基; 并且R 4是羧酸酯，羧酰胺或磺酰胺基团; 或其盐，N-氧化物，水合物或溶剂合物。

6. 发明申请

WO2003055860A1 3,4-DIARYLPYRAZOLES AND THEIR USE IN THE THERAPY OF CANCER 审中-公开
标题翻译： 3,4-DIARYLPYRAZOLES及其在癌症治疗中的应用
公开(公告)号：WO2003055860A1
公开(公告)日：2003-07-10
申请号：PCT/GB2002/005778
申请日：2002-12-19
申请人： RIBOTARGETS LIMITED , CANCER RESEARCH TECHNOLOGY LTD. , THE INSTITUTE OF CANCER RESEARCH , DRYSDALE, Martin, James , DYMOCK, Brian, William , BARRIL-ALONSO, Xavier , WORKMAN, Paul , PEARL, Laurence, Harris , PRODROMOU, Chrisostomos , MACDONALD, Edward
发明人： DRYSDALE, Martin, James , DYMOCK, Brian, William , BARRIL-ALONSO, Xavier , WORKMAN, Paul , PEARL, Laurence, Harris , PRODROMOU, Chrisostomos , MACDONALD, Edward
IPC分类号： C07D231/12
CPC分类号： C07D231/12 , A61K31/415 , C07D231/14 , C07D231/16 , C07D401/04 , C07D401/10 , C07D403/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D417/04
摘要： The present invention pertains to the use of certain 3,4-diarylpyrazoles of formula (I), both in vitro and in vivo , to inhibit heat shock protein 90 (HSP90), and in the treatment of conditions mediated by HSP90, including, for example, cancer; wherein: Ar 3 is independently: a C 5-20 aryl group, and is optionally substituted; Ar 4 is independently: a C 5-20 aryl group, and is optionally substituted; R 5 is independently: hydrogen; halo; hydroxy; ether; formyl; acyl; carboxy; ester; acyloxy; oxycarbonyloxy; amido; acylamido; aminocarbonyloxy; tetrazolyl; amino; nitro; cyano; azido; sulfhydryl; thioether; sulfonamido; C 1-7 alkyl; C 3-20 heterocycyl; or C 5-20 aryl; R N is independently: -H; C 1-7 alkyl; C 3-20 heterocycyl; or, C 5-20 aryl; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to such compounds, pharmaceutical compositions comprising such compounds, such compounds for medical use, such compounds for use in the treatment of conditions mediated by HSP90, including, for example, cancer, and use of such compounds in the preparation of medicaments for such treatments.
摘要翻译：本发明涉及式（I）的某些3,4-二芳基吡唑（体外和体外）均用于抑制热休克蛋白90（HSP90），以及治疗由HSP90介导的病症，包括例如癌症; 其中：Ar 3独立地为：C 5-20芳基，并且是任选取代的; Ar 4独立地是C 5-20芳基，并且任选被取代; R 5独立地为：氢; 光环; 羟基; 醚; 甲酰基; 酰基; 羧基; 酯; 酰氧基; 氧羰基氧; 酰胺基; 酰氨基; 羰基氨基; 四唑基; 氨基; 硝基; 氰基; 叠氮; 巯基; 硫醚; 磺酰; ç 1-7 烷基; ç 3-20 杂环基; 或C 15-20芳基; R N 独立地为：-H; ç 1-7 烷基; ç 3-20 杂环基; 或者C 15-20芳基; 和其药学上可接受的盐，溶剂合物，酰胺，酯，醚，化学保护形式及其前药。本发明还涉及这样的化合物，包含这种化合物的药物组合物，用于医疗用途的这种化合物，用于治疗由HSP90介导的病症包括例如癌症的化合物，以及这些化合物在制备药物用于治疗。

7. 发明授权

EP1675861B1 PYRIMIDOTHIOPHENE COMPOUNDS 有权
标题翻译：嘧啶并噻吩化合物
公开(公告)号：EP1675861B1
公开(公告)日：2015-12-23
申请号：EP04768197.8
申请日：2004-08-26
申请人： Vernalis (R&D) Ltd. , Cancer Research Technology Limited , The Institute of Cancer Research
发明人： DYMOCK, Brian William, Evotec OAI Ltd , DRYSDALE, Martin James, Vernalis (Cambridge) Ltd , FROMONT, Christofe, Vernalis (Cambridge) Ltd , JORDAN, Allan, Vernalis (Cambridge) Limited , BARRIL-ALONSO, Xavier
IPC分类号： C07D495/04 , A61K31/00 , A61P35/00
CPC分类号： C07D495/04 , A61K31/519

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