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1. 发明申请

US20070275961A1 Triazolo ' 1, 5-A ! Pyrimidines and Their Use in Medicine 审中-公开
标题翻译： Triazolo'1，5-A！嘧啶及其在医学中的应用
公开(公告)号：US20070275961A1
公开(公告)日：2007-11-29
申请号：US10558694
申请日：2004-06-02
申请人： Justin Bower , Andrew Cansfield , Allan Jordan , Martin Parratt , Lee Walmsley , Douglas Williamson
发明人： Justin Bower , Andrew Cansfield , Allan Jordan , Martin Parratt , Lee Walmsley , Douglas Williamson
IPC分类号： A61K31/519 , A61K31/496 , A61K31/5377 , A61P17/06 , A61P35/00 , A61P9/00 , C07D413/14 , C07D487/04
CPC分类号： A61K31/519 , C07D487/04
摘要： Compounds of formula (IA) or (AB) are kinase inhibitors, especially of CDK2, and/or PDK1 and/or CHK1: wherein Ring A is an optionally substituted aryl, heteroaryl, carbocyclic or heterocyclic radical, Alk represents an optionally substituted clivaient C1-C6 alkylene radical; n is 0 or 1; Q represents a radical of formula -(Alk1)p-(X),(Alk2)s-Z wherein in any compatible combination Z is hydrogen or an optionally substituted carbocyclic or heterocyclic ring, p, r and s are 0 or 1, and Alk1, Alk2, X, are as described in the specification, and R1 represents a radical 3 4 3 (CYC)k-(Alk3)a-(Y)b-(Alk4)d-B wherein k, a, b and d are 0 or 1, and Cyc, Alk3, Alk4 and B are as described in the specification.
摘要翻译：式（IA）或（AB）的化合物是激酶抑制剂，特别是CDK2和/或PDK1和/或CHK1的激酶抑制剂：其中环A是任选取代的芳基，杂芳基，碳环或杂环基，Alk表示任选取代的亲水性C C 1 -C 6亚烷基; n为0或1; Q表示式 - （Alk-1）对 - （X），（Alk 2 O 3）-SZ的基团，其中以任何相容的组合 Z是氢或任选取代的碳环或杂环，p，r和s是0或1，并且Alk 1，Alk 2 X，如规格，R 1表示基团3 4 3（CYC）3 - （烷基）（Y）b - 其中k，a，b和d分别为0或1，并且Cyc，Alk 3号，3号，4号和B号如说明书中所述。

2. 发明申请

US20100305143A1 PYRROLOPYRIMIDINE COMPOUNDS 审中-公开
标题翻译：吡咯烷酮化合物
公开(公告)号：US20100305143A1
公开(公告)日：2010-12-02
申请号：US12677919
申请日：2008-09-19
申请人： Allan Jordan , Simon Bedford , Klenke Burkhard , Ian Yule , Karinne Poullennec
发明人： Allan Jordan , Simon Bedford , Klenke Burkhard , Ian Yule , Karinne Poullennec
IPC分类号： A61K31/519 , C07D487/04 , A61P29/00 , A61P3/10 , A61P35/00 , A61P11/06 , A61P11/00
CPC分类号： C07D487/04
摘要： Compounds of formula (I) are A2B receptor antagonists: wherein Ri is optionally substituted aryl or an optionally substituted monocyclic heteroaryl group having 5 or 6 ring atoms; R2 and R3 are independently selected from hydrogen, or optionally substituted C1-C6 alkyl, C1-C6 alkoxy-(C1-C6)-alkyl, C3-C8 cycloalkyl, aryl, heteroaryl, aryl-(C1-C6)-alkyl, or heteroaryl-(C1-C6)-alkyl; R4 and R5 are independently selected from hydrogen, optionally substituted C1-C6alkyl, optionally substituted aryl, aryl-(C1-C6)-alkyl optionally substituted in the ring part thereof, —NHR7—N(—R8)—R9, —NH—(C═O)—R10, —(C═O)—NH—R11, —(C═O)—O—R12, or halo; R6 is hydrogen, C1-C6 alkyl, aryl-(C1-C6)-alkyl, —(C═O)—NH—R13, —(C═O)—R14, aryl, heteroaryl, hydroxy-(C1-C6)-alkyl, or C3-C8 cycloalkyl-alkyl; and R7, R8, R9, R10, R11, R12, R13 and R14 are independently selected from C1-C6 alkyl, aryl, aryl-(C1-C6)-alkyl and heteroaryl.
摘要翻译：式（I）化合物是A2B受体拮抗剂：其中R 1是任选取代的芳基或具有5或6个环原子的任选取代的单环杂芳基; R 2和R 3独立地选自氢或任选取代的C 1 -C 6烷基，C 1 -C 6烷氧基 - （C 1 -C 6） - 烷基，C 3 -C 8环烷基，芳基，杂芳基，芳基 - （C 1 -C 6） - 烷基或杂芳基 - （C 1 -C 6） - 烷基; R 4和R 5独立地选自氢，任选取代的C 1 -C 6烷基，任选取代的芳基，在其环部任选取代的芳基 - （C 1 -C 6） - 烷基，-NHR 7 -N（-R 8）-R 9，-NH- （C = O）-R 10， - （C = O）-NH-R 11， - （C = O）-O-R 12或卤素; R6是氢，C1-C6烷基，芳基 - （C1-C6） - 烷基， - （C = O）-NH-R13， - （C = O）-R14，芳基，杂芳基，羟基 - （C1-C6） - 烷基或C 3 -C 8环烷基 - 烷基; 并且R 7，R 8，R 9，R 10，R 11，R 12，R 13和R 14独立地选自C 1 -C 6烷基，芳基，芳基 - （C 1 -C 6） - 烷基和杂芳基。

3. 发明申请

US20110118284A1 THIENOPYRIMIDINE COMPOUNDS 有权
标题翻译：噻吗啉化合物
公开(公告)号：US20110118284A1
公开(公告)日：2011-05-19
申请号：US12678378
申请日：2008-09-19
申请人： Allan Jordan , Simon Bedford , Klenke Burkhard , Ian Yule , Karine Poullennec
发明人： Allan Jordan , Simon Bedford , Klenke Burkhard , Ian Yule , Karine Poullennec
IPC分类号： A61K31/519 , C07D495/04 , A61P35/00 , A61P3/10 , A61P29/00 , A61P11/00 , A61P11/06
CPC分类号： C07D495/04 , A61K31/519 , C07D495/14
摘要： Compounds of formula (I) are A2B receptor antagonists, wherein R1 is optionally substituted aryl or an optionally substituted 5- or 6-membered heteroaryl ring; R2 and R3 are independently selected from hydrogen, C1-C6 alkyl, C3-C8 cycloalkyl, C3-C8 cycloalkyl-(C1-C6)-alkyl, aryl-(C1-C6)-alkyl optionally substituted in the ring part thereof, a 5- or 6-membered monocyclic heterocyclic group optionally linked via a C1-C6 alkylene chain and optionally substituted in the ring part thereof, benzimidazol-2-yl-methyl, pyrid-3-yl-carbonyl, or (1-methyl-piperidin-4-yl)-carbonyl-methyl; or R2 and R3 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R4 is C1-C3 alkyl, C2-C3 alkenyl, —N(—R5)—R6, or optionally substituted heteroarylmethylamino; and R5 and R6 are independently selected from hydrogen or C1-C3 alkyl; or R5 and R6 taken together with the nitrogen atom to which they are attached form an optionally substituted 4- to 6-membered saturated ring.
摘要翻译：式（I）化合物是A2B受体拮抗剂，其中R1是任选取代的芳基或任选取代的5或6元杂芳基环; R2和R3独立地选自氢，C1-C6烷基，C3-C8环烷基，C3-C8环烷基 - （C1-C6） - 烷基，在其环部分任意取代的芳基 - （C 1 -C 6） - 烷基，任选通过C1-C6亚烷基链连接并任选在其环部分取代的5-或6-元单环杂环基，苯并咪唑-2-基 - 甲基，吡啶-3-基 - 羰基或（1-甲基 - 哌啶 -4-基） - 羰基 - 甲基; 或者R 2和R 3与它们所连接的氮原子一起形成任选取代的5-或6-元环; R 4是C 1 -C 3烷基，C 2 -C 3烯基，-N（-R 5）-R 6或任选取代的杂芳基甲基氨基; 并且R 5和R 6独立地选自氢或C 1 -C 3烷基; 或者R 5和R 6与它们所连接的氮原子一起形成任选取代的4至6元饱和环。

4. 发明申请

US20070281936A1 Pyrimidine Compounds as Purine Receptor Antagonist 失效
标题翻译：嘧啶化合物作为嘌呤受体拮抗剂
公开(公告)号：US20070281936A1
公开(公告)日：2007-12-06
申请号：US10588757
申请日：2005-02-11
申请人： Roger Gillespie , Richard Todd , Gemma Stratton , Allan Jordan
发明人： Roger Gillespie , Richard Todd , Gemma Stratton , Allan Jordan
IPC分类号： A61K31/506 , A61K31/496 , A61K31/5377 , A61P25/14 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , C07D239/42 , C07D413/14
CPC分类号： C07D409/14 , C07D401/12 , C07D405/04 , C07D405/14 , C07D413/14 , C07D417/04 , C07D417/14
摘要： Compounds of formula (I); wherein R1 is H or NHZ; R2 is optionally substituted aryl or heteroaryl attached via a carbon atom; R3 is H; optionally substituted C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, or C3 C7 cycloalkyl, halogen; OH or OR, or R4 is H, optionally substituted C1-C6alkyl, C3 C6alkenyl, C3-C6alkynyl, C3-C7 cycloalkyl, aryl or heteroaryl, R5 is H or optionally substituted C1-C6alkyl, C3-C6alkenyl, C3-C6alkynyl, or C3-C7 cycloalkyl; or R4 and R5 together form a 5 or 6-membered heterocyclic ring; and R10 is optionally substituted C1-C6alkyl; are purine receptor, particularly adenosine receptor antagonists, useful for treatment of, inter alia, movement disorders such as Parkinsons disease.
摘要翻译：式（I）化合物; 其中R 1是H或NHZ; R 2是通过碳原子连接的任选取代的芳基或杂芳基; R 3是H; 任选取代的C 1 -C 6烷基，C 2 -C 6亚烯基，C 2 - 或者C 3 -C 7环烷基，卤素; C 1 -C 6烷基， OH或OR，或R 4是H，任选取代的C 1 -C 6烷基，C 3 C C 6链烯基，C 3 -C 6炔基，C 3 -C 7炔基，C 3 -C 6炔基，C 3 -C 6炔基，环烷基，芳基或杂芳基，R 5是H或任选取代的C 1 -C 6烷基，C 3 - -C 6亚烷基，C 3 -C 6炔基或C 3 -C 7炔基，环烷基; 或R 4和R 5一起形成5或6元杂环; 且R 10是任选取代的C 1 -C 6烷基; 是嘌呤受体，特别是腺苷受体拮抗剂，可用于治疗尤其是运动障碍如帕金森病。

5. 发明授权

US08642594B2 Substituted thieno[2,3-d]pyrimidines as HSP90 inhibitors 有权
标题翻译：取代噻吩并[2,3-d]嘧啶作为HSP90抑制剂
公开(公告)号：US08642594B2
公开(公告)日：2014-02-04
申请号：US12690983
申请日：2010-01-21
申请人： Brian William Dymock , Martin James Drysdale , Christofe Fromont , Allan Jordan , Xavier Barril-Alonso
发明人： Brian William Dymock , Martin James Drysdale , Christofe Fromont , Allan Jordan , Xavier Barril-Alonso
IPC分类号： A61K31/519 , A61K31/5377 , A61K31/497 , A61P25/28 , C07D487/04 , C07D295/04 , C07D295/104
CPC分类号： C07D495/04 , A61K31/519
摘要： Compounds of formula (1) are inhibitors of HSP90 activity in vitro or in vivo, and of use in the treatment of inter alia, cancer: wherein R2 is a group of formula —(Ar1)m-(Alk1)P-(Z)r-(Alk2)S-Q wherein Ar1 is an optionally substituted aryl or heteroaryl radical, Alk′ and Alk 2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, p, r and s are independently 0 or 1, Z is —O—, —S—, —(C═O)—, —(C═S)—, —SO2—, —C(═O)O—, —C(═O)NRA—, —C(═S)NRA—, —SO2NRA—, —NRAC(═O)—, —NRASO2— or —NRA— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group.
摘要翻译：式（1）化合物是体外或体内HSP90活性的抑制剂，尤其用于治疗癌症：其中R2是式 - （Ar1）m-（Alk1）P-（Z） r-（Alk2）SQ其中Ar1是任选取代的芳基或杂芳基，Alk'和Alk 2是任选取代的二价C 1 -C 3亚烷基或C 2 -C 3亚烯基，m，p，r和s独立地为0或1， Z是-O - ， - S - ， - （C = O） - ， - （C = S） - ， - SO 2 - ， - C（= O）（= S）NRA，-SO2NRA-，-NRAC（= O） - ，-NRASO2-或-NRA-，其中RA是氢或C1-C6烷基，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）烷基，芳基或杂芳基; 并且R 4是羧酸酯，羧酰胺或磺酰胺基。

6. 发明授权

US07820658B2 Substituted thieno[2,3-d]pyrimidines as HSP90 inhibitors 有权
标题翻译：取代噻吩并[2,3-d]嘧啶作为HSP90抑制剂
公开(公告)号：US07820658B2
公开(公告)日：2010-10-26
申请号：US10569287
申请日：2004-08-26
申请人： Brian William Dymock , Martin James Drysdale , Christofe Fromont , Allan Jordan , Xavier Barril-Alonso
发明人： Brian William Dymock , Martin James Drysdale , Christofe Fromont , Allan Jordan , Xavier Barril-Alonso
IPC分类号： C07D487/04 , A61K31/519 , C07D295/04 , C07D295/104 , A61K31/5377 , A61K31/497 , A61P25/28
CPC分类号： C07D495/04 , A61K31/519
摘要： Compounds of formula (1) are inhibitors of HSP90 activity in vitro or in vivo, and of use in the treatment of inter alia, Cancer: wherein R2 is a group of formula —(Ar1)m-(Alk1)P-(Z)r-(Alk 2)S-Q wherein Ar1 is an optionally substituted aryl or heteroaryl radical, Alk′ and Alk 2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, p, r and s are independently 0 or 1, Z is —O—, —S—, —(C═O)—, —(C═S)—, —SO2—, —C(═O)O—, —C(═O)NRA—, —C(═S)NRA—, —SO2NRA—, —NRAC(═O)_, —NRASO2- or —NRA—wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group.
摘要翻译：式（1）的化合物是体外或体内的HSP90活性的抑制剂，并且用于治疗尤其是癌症：其中R2是式 - （Ar1）m-（Alk1）P-（Z） r-（Alk 2）SQ其中Ar1是任选取代的芳基或杂芳基，Alk'和Alk 2是任选取代的二价C 1 -C 3亚烷基或C 2 -C 3亚烯基，m，p，r和s独立地为0或1 ，Z为-O - ， - S - ， - （C = O） - ， - （C = S） - ， - SO 2 - ， - C（= O）其中RA是氢或C 1 -C 6烷基，Q是氢或任选取代的碳环或杂环基; C（= O）NR A - ， - SO 2 NRA-，-NRAC（= O） 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。

7. 发明授权

US08354415B2 Thienopyrimidine compounds and compositions 有权
标题翻译：噻吩并嘧啶化合物和组合物
公开(公告)号：US08354415B2
公开(公告)日：2013-01-15
申请号：US12678376
申请日：2008-09-19
申请人： Allan Jordan , Simon Bedford , Klenke Burkhard , Ian Yule , Karine Poullennec
发明人： Allan Jordan , Simon Bedford , Klenke Burkhard , Ian Yule , Karine Poullennec
IPC分类号： C07D495/04 , A61K31/519 , A61P11/06 , A61P11/08 , A61P29/00
CPC分类号： C07D495/04
摘要： Compounds of formula (I) are A2B wherein R1 and R2 are independently selected from hydrogen, or optionally substituted CrC6 alkyl, C1-C6alkoxy-(C1-C6)-alkyl, C3-C8 cycloalkyl, aryl, heteroaryl, aryl-(C1-C6)-alkyl, or heteroaryl-(C1-C6)-alkyl; or R−1 and R2 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R3 and R4 are independently selected from hydrogen, or optionally substituted C1-C6 alkyl, C1-C6 alkoxy-(C1-C6)-alkyl, C3-C8 cycloalkyl, aryl, heteroaryl, aryl-(C1-C6)-alkyl, or heteroaryl-C1-C6)-alkyl; or R3 and R4 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R5 and R6 are independently selected from hydrogen, C1-C6 alkyl, aryl, aryl-(C1-C6)-alkyl, —NHR7—N(—R8)—R9, —NH—(C═O)—R10, —(C═O)—NH—R11, —(C═O)—O—R12, or halo; and R7, R8, R9, R10, R−11, and R12 are independently selected from C1-C6 alkyl, aryl, aryl-(C1-C6)-alkyl and heteroaryl.
摘要翻译：式（I）化合物是其中R 1和R 2独立地选自氢或任选取代的C 1 -C 6烷基，C 1 -C 6烷氧基 - （C 1 -C 6） - 烷基，C 3 -C 8环烷基，芳基，杂芳基，芳基 - （C1- C6） - 烷基或杂芳基 - （C1-C6） - 烷基; 或R 1和R 2与它们所连接的氮原子一起形成任选取代的5或6元环; R 3和R 4独立地选自氢或任选取代的C 1 -C 6烷基，C 1 -C 6烷氧基 - （C 1 -C 6） - 烷基，C 3 -C 8环烷基，芳基，杂芳基，芳基 - （C 1 -C 6） - 烷基或杂芳基-C 1 -C 6） - 烷基; 或者R 3和R 4与它们所连接的氮原子一起形成任选取代的5或6元环; R 5和R 6独立地选自氢，C 1 -C 6烷基，芳基，芳基 - （C 1 -C 6） - 烷基，-NHR 7 -N（-R 8）-R 9，-NH-（C = O）-R 10， - （ C = O）-NH-R 11， - （C = O）-O-R 12或卤素; 并且R 7，R 8，R 9，R 10，R 11和R 12独立地选自C 1 -C 6烷基，芳基，芳基 - （C 1 -C 6） - 烷基和杂芳基。

8. 发明申请

US20100298349A1 THIENOPYRIMIDINE COMPOUNDS AND COMPOSITIONS 有权
标题翻译：噻吗啉化合物和组合物
公开(公告)号：US20100298349A1
公开(公告)日：2010-11-25
申请号：US12678376
申请日：2008-09-19
申请人： Allan Jordan , Simon Bedford , Klenke Burkhard , Ian Yule , Karinne Poullennec
发明人： Allan Jordan , Simon Bedford , Klenke Burkhard , Ian Yule , Karinne Poullennec
IPC分类号： A61K31/519 , C07D495/04 , A61P11/00 , A61P3/10 , A61P29/00 , A61P35/00
CPC分类号： C07D495/04
摘要： Compounds of formula (I) are A2B wherein R1 and R2 are independently selected from hydrogen, or optionally substituted CrC6 alkyl, C1-C6alkoxy-(C1-C6)-alkyl, C3-C8 cycloalkyl, aryl, heteroaryl, aryl-(C1-C6)-alkyl, or heteroaryl-(C1-C6) -alkyl; or R−1 and R2 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R3 and R4 are independently selected from hydrogen, or optionally substituted C1-C6 alkyl, C1-C6 alkoxy-(C1-C6)-alkyl, C3-C8 cycloalkyl, aryl, heteroaryl, aryl-(C1-C6)-alkyl, or heteroaryl-C1-C6)-alkyl; or R3 and R4 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R5 and R6 are independently selected from hydrogen, C1-C6 alkyl, aryl, aryl-(C1-C6)-alkyl, —NHR7—N(—R8)—R9, —NH—(C═O)—R10, —(C═O)—NH—R11, —(C═O)—O—R12, or halo; and R7, R8, R9, R10, R−11, and R12 are independently selected from C1-C6 alkyl, aryl, aryl-(C1-C6)-alkyl and heteroaryl.
摘要翻译：式（I）化合物是其中R 1和R 2独立地选自氢或任选取代的C 1 -C 6烷基，C 1 -C 6烷氧基 - （C 1 -C 6） - 烷基，C 3 -C 8环烷基，芳基，杂芳基，芳基 - （C1- C6） - 烷基或杂芳基 - （C1-C6） - 烷基; 或R 1和R 2与它们所连接的氮原子一起形成任选取代的5或6元环; R 3和R 4独立地选自氢或任选取代的C 1 -C 6烷基，C 1 -C 6烷氧基 - （C 1 -C 6） - 烷基，C 3 -C 8环烷基，芳基，杂芳基，芳基 - （C 1 -C 6） - 烷基或杂芳基-C 1 -C 6） - 烷基; 或者R 3和R 4与它们所连接的氮原子一起形成任选取代的5或6元环; R 5和R 6独立地选自氢，C 1 -C 6烷基，芳基，芳基 - （C 1 -C 6） - 烷基，-NHR 7 -N（-R 8）-R 9，-NH-（C = O）-R 10， - （ C = O）-NH-R 11， - （C = O）-O-R 12或卤素; 并且R 7，R 8，R 9，R 10，R 11和R 12独立地选自C 1 -C 6烷基，芳基，芳基 - （C 1 -C 6） - 烷基和杂芳基。

9. 发明授权

US09120807B2 Thienopyrimidine compounds 有权
标题翻译：噻吩并嘧啶化合物
公开(公告)号：US09120807B2
公开(公告)日：2015-09-01
申请号：US12678378
申请日：2008-09-19
申请人： Allan Jordan , Simon Bedford , Klenke Burkhard , Ian Yule , Karine Poullennec
发明人： Allan Jordan , Simon Bedford , Klenke Burkhard , Ian Yule , Karine Poullennec
IPC分类号： C07D495/04 , A61K31/519
CPC分类号： C07D495/04 , A61K31/519 , C07D495/14
摘要： Compounds of formula (I) are A2B receptor antagonists, wherein R1 is optionally substituted aryl or an optionally substituted 5- or 6-membered heteroaryl ring; R2 and R3 are independently selected from hydrogen, C1-C6 alkyl, C3-C8 cycloalkyl, C3-C8 cycloalkyl-(C1-C6)-alkyl, aryl-(C1-C6)-alkyl optionally substituted in the ring part thereof, a 5- or 6-membered monocyclic heterocyclic group optionally linked via a C1-C6 alkylene chain and optionally substituted in the ring part thereof, benzimidazol-2-yl-methyl, pyrid-3-yl-carbonyl, or (1-methyl-piperidin-4-yl)-carbonyl-methyl; or R2 and R3 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R4 is C1-C3 alkyl, C2-C3 alkenyl, —N(—R5)—R6, or optionally substituted heteroarylmethylamino; and R5 and R6 are independently selected from hydrogen or C1-C3 alkyl; or R5 and R6 taken together with the nitrogen atom to which they are attached form an optionally substituted 4- to 6-membered saturated ring.
摘要翻译：式（I）化合物是A2B受体拮抗剂，其中R1是任选取代的芳基或任选取代的5或6元杂芳基环; R2和R3独立地选自氢，C1-C6烷基，C3-C8环烷基，C3-C8环烷基 - （C1-C6） - 烷基，在其环部分任意取代的芳基 - （C 1 -C 6） - 烷基，任选通过C1-C6亚烷基链连接并任选在其环部分取代的5-或6-元单环杂环基，苯并咪唑-2-基 - 甲基，吡啶-3-基 - 羰基或（1-甲基 - 哌啶 -4-基） - 羰基 - 甲基; 或者R 2和R 3与它们所连接的氮原子一起形成任选取代的5-或6-元环; R 4是C 1 -C 3烷基，C 2 -C 3烯基，-N（-R 5）-R 6或任选取代的杂芳基甲基氨基; 并且R 5和R 6独立地选自氢或C 1 -C 3烷基; 或者R 5和R 6与它们所连接的氮原子一起形成任选取代的4至6元饱和环。

10. 发明申请

US20100120767A1 Pyrimidothiophene Compounds 有权
标题翻译：嘧啶并噻吩化合物
公开(公告)号：US20100120767A1
公开(公告)日：2010-05-13
申请号：US12690983
申请日：2010-01-21
申请人： Brian William Dymock , Martin James Drysdale , Christofe Fromont , Allan Jordan , Xavier Barril-Alonso
发明人： Brian William Dymock , Martin James Drysdale , Christofe Fromont , Allan Jordan , Xavier Barril-Alonso
IPC分类号： A61K31/5377 , A61K31/519 , A61P29/00 , A61P19/02 , A61P11/06 , C07D495/04
CPC分类号： C07D495/04 , A61K31/519
摘要： Compounds of formula (1) are inhibitors of HSP90 activity in vitro or in vivo, and of use in the treatment of inter alia, cancer: wherein R2 is a group of formula —(Ar1)m-(Alk1)P-(Z)r-(Alk2)S-Q wherein Ar1 is an optionally substituted aryl or heteroaryl radical, Alk′ and Alk 2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C═O)—, —(C═S)—, -S02-, —C(═O)O—, —C(═O)NRA—, —C(═S)NRA—, -S02NRA—, —NRAC(═O)—, —NRAS02- or —NRA— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group.
摘要翻译：式（1）化合物是体外或体内HSP90活性的抑制剂，尤其用于治疗癌症：其中R2是式 - （Ar1）m-（Alk1）P-（Z） r-（Alk2）SQ其中Ar1是任选取代的芳基或杂芳基，Alk'和Alk 2是任选取代的二价C 1 -C 3亚烷基或C 2 -C 3亚烯基，m，p，r和s独立地为0或1， Z是-O - ， - S - ， - （C = O） - ， - （C = S） - ， - SO2-，-C（= O）O-，-C（= O）NRA，-C 其中RA是氢或C 1 -C 6烷基，Q是氢或任选取代的碳环或杂环基;（≡S）NRA-，-SO 2 NR-，-NRAC（= O） - ， - NRASO 2 - 或-NRA- 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。

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