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1. 发明申请

US20060235058A1 Substituted 5-membered ring compounds and their use 失效
标题翻译：取代的5元环化合物及其用途
公开(公告)号：US20060235058A1
公开(公告)日：2006-10-19
申请号：US10561969
申请日：2004-06-24
申请人： Kwai Cheung , Brian Dymock , Edward McDonald , Martin Drysdale
发明人： Kwai Cheung , Brian Dymock , Edward McDonald , Martin Drysdale
IPC分类号： A61K31/4196 , A61K31/4192 , C07D249/04 , C07D249/08 , A61K31/41
CPC分类号： A61K31/4196 , A61K31/4192 , A61K31/427 , A61K31/433
摘要： Compound of a compound of formula (1) or a salt, N-oxide, hydrate or solvate thereof, in the preparation of a composition for inhibition of HSP90 activity: wherein ring A is an aromatic or non-aromatic carbocyclic or heterocyclic ring having 5 ring atoms, for example 1,2,3-triazolyl or a 1,2,4-triazolyl or a tetrazolyl ring; and R1 R2 R3 are as defined in the specification are inhibitors of HSP90 and therefore of use in the treatment of, for example, cancers, viral disease, inflammatory diseases such as rheumatoid arthritis, asthma, multiple sclerosis, Type I diabetes, lupus, psoriasis and inflammatory bowel disease; cystic fibrosis angiogenesis-related disease such as diabetic retinopathy, haemangiomas, and endometriosis; or for protection of normal cells against chemotherapy-induced toxicity; or diseases where failure to undergo apoptosis is an underlying factor, or protection from hypoxia-ischemic injury due to elevation of Hsp70 in the heart and brain; scrapie /CJD, Huntingdon's and Alzheimer's disease.
摘要翻译：式（1）化合物或其盐，N-氧化物，水合物或溶剂化物的化合物在制备抑制HSP90活性的组合物中的用途：其中环A是具有5个或更多个碳原子的芳族或非芳族碳环或杂环环原子，例如1,2,3-三唑基或1,2,4-三唑基或四唑基环; 和R 1 R 2 R 3 R 3如本说明书中所定义的是HSP90的抑制剂，因此用于治疗，例如，癌症，病毒性疾病，炎性疾病如类风湿性关节炎，哮喘，多发性硬化，I型糖尿病，狼疮，牛皮癣和炎症性肠病; 囊性纤维化血管生成相关疾病如糖尿病性视网膜病变，血管瘤和子宫内膜异位症; 或用于保护正常细胞免受化疗诱导的毒性; 或未能进行细胞凋亡的疾病是潜在的因素，或由于心脏和脑中Hsp70的升高而保护缺氧缺血性损伤; 瘙痒病/ CJD，亨廷顿氏症和阿尔茨海默病。

2. 发明申请

US20060241106A1 Isoxazole compounds as inhibitors of heat shock proteins 有权
公开(公告)号：US20060241106A1
公开(公告)日：2006-10-26
申请号：US10544443
申请日：2004-02-09
申请人： Martin Drysdale , Brian Dymock , Harry Finch , Paul Webb , Edward McDonald , Karen James , Kwai Cheung , Thomas Matthews
发明人： Martin Drysdale , Brian Dymock , Harry Finch , Paul Webb , Edward McDonald , Karen James , Kwai Cheung , Thomas Matthews
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/42
CPC分类号： A61K31/541 , A61K31/42 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/5377 , C07D261/08 , C07D261/10 , C07D413/04 , C07D413/10 , C07D417/04 , C07D495/04
摘要： Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: (A), (B) wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, —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; R2 is (i) a group of formula (IA) above or (ii) a carboxamide radical; or (iii) a non aromatic carbocyclic or heterocyclic ring wherein a ring carbon is optionally substituted, and/or a ring nitrogen is optionally substituted by a group of formula -(Alk1)p-(Z)r-(Alk2)s-Q wherein Q, Alk1, Alk2, Z, p, r and s are as defined above in relation to group (IA); and R3 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6 alkenyl, or C1-C6 alkynyl; or a carboxyl, carboxamide, or carboxyl ester group.

3. 发明申请

US20060148817A1 Pyrazole compounds 失效
公开(公告)号：US20060148817A1
公开(公告)日：2006-07-06
申请号：US10536899
申请日：2003-12-18
申请人： Christine Beswick , Martin Drysdale , Brian Dymock , Edward McDonald
发明人： Christine Beswick , Martin Drysdale , Brian Dymock , Edward McDonald
IPC分类号： A61K31/496 , C07D403/02
CPC分类号： C07D231/38 , A61K31/415 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/10 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Compounds of formula (IA) or (IB) or a salt, N-oxide, hydrate or solvate thereof are inhibitors of HSP90, and are of value in the treatment of diseases responsive to HSP90 inhibition such as cancers. In the formulae, Ar is an aryl, aryl(C1-C6 alkyl), aryl(C1-C6 alkyl), heteroaryl, heteroarylaryl(C1-C6 alkyl), or heteroarylaryl(C1-C6 alkyl) group, any of which being optionally substituted in the aryl or heteroaryl part thereof; R1, is hydrogen or optionally substituted C1-C6 alkyl; R2 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6 alkenyl, or C1-C6 alkynyl; or a carboxyl, carboxamide or carboxyl ester group; and ring A is a non aromatic carbocyclic or heterocyclic ring wherein (i) a ring carbon is optionally substituted, and/or (ii) a ring nitrogen is optionally substituted by a group of formula -(Alk1)p (Cyc)n-(Alk3)m-(Z)r-(Alk2)s Q where Alk1, Alk2 and Alk3 are optionally substituted C1-C3 alkyl, Cyc is an optionally substituted carbocyclic or heterocyclic radical; m, n, p, r and s are independently 0 or 1, Z is —0—, —S—, —(C═O)—, —S02-, —C(═O)O—, —OC(═O)—, —NW—, —C(═O)NRA—, —NRAC(═O)—, —SO2NRA—, or —NRASO2— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical.

4. 发明申请

US20070072855A1 Pyrazole compounds as hsp90 inhibitors for the treatment of cancer 失效
标题翻译：吡唑类化合物作为治疗癌症的hsp90抑制剂
公开(公告)号：US20070072855A1
公开(公告)日：2007-03-29
申请号：US10553955
申请日：2004-04-23
申请人： Xavier Barrilalonso , Brian Dymock , Martin Drysdale
发明人： Xavier Barrilalonso , Brian Dymock , Martin Drysdale
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/4152 , C07D413/02 , C07D403/02
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 R1, R2 and R3 are as defined in the specification, and X is —OR4 or —NR4R5 wherein R4 and R5 independently represent hydrogen or optionally substituted C1-C6 alkyl, or R4 and R5 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R 1，R 2和R 3 本说明书中所定义，X为-OR 4或-NR 4 R 5，其中R 4 R 5和R 5独立地表示氢或任选取代的C 1 -C 6烷基或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

US20050222230A1 3,4-diarylpyrazoles and their use in the therapy of cancer 失效
标题翻译： 3,4-二芳基吡唑及其在癌症治疗中的应用
公开(公告)号：US20050222230A1
公开(公告)日：2005-10-06
申请号：US10499030
申请日：2002-12-19
申请人： Martin Drysdale , Brian Dymock , Xavier Barril-Alonso , Paul Workman , Laurence Pearl , Chrisostomos Prodromou , Edward Macdonald
发明人： Martin Drysdale , Brian Dymock , Xavier Barril-Alonso , Paul Workman , Laurence Pearl , Chrisostomos Prodromou , Edward Macdonald
IPC分类号： A61K31/415 , A61K31/4155 , A61K31/4178 , A61K31/4184 , A61K31/427 , A61K31/428 , A61K31/506 , A61P35/00 , A61P43/00 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/22 , C07D401/04 , C07D401/10 , C07D403/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D417/04 , A61K31/4152
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: Ar3 is independently: a C5-20aryl group, and is optionally substituted; Ar4 is independently: a C5-20aryl group, and is optionally substituted; R5 is independently: hydrogen; halo; hydroxy; ether; formyl; acyl; carboxy; ester, acyloxy; oxycarbonyloxy; amido; acylamido; aminocarbonyloxy; tetrazolyl; amino; nitro; cyano; azido; sulfhydryl; thioether; sulfonamido; C1-7alkyl; C3-20heterocycyl; or C5-20aryl; R N is independently: —H; C1-7alkyl; C3-20heterocycyl; or, C5-20aryl; 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（体外和体内）用于抑制热休克蛋白90（HSP90）的用途，以及用于治疗HSP90介导的病症，包括例如癌症; 其中：Ar 3独立地是C 5-20-20芳基，并且是任选被取代的; Ar 4独立地是C 5-20-20芳基，并且是任选被取代的; R 5独立地为氢; 光环; 羟基; 醚; 甲酰基酰基; 羧基; 酯，酰氧基; 氧羰氧基氨基酸酰氨基; 氨基羰基氧基; 四唑基; 氨基; 硝基氰基叠氮巯基硫醚磺酰胺 C 1-7烷基; C 3-20杂环基; 或C 5-20-20芳基; R N 独立地为：-H; C 1-7烷基; C 3-20杂环基; 或C 5-20-20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。

6. 发明申请

US20070043044A1 Pyrimidothiophene compounds 有权
标题翻译：嘧啶并噻吩化合物
公开(公告)号：US20070043044A1
公开(公告)日：2007-02-22
申请号：US10569287
申请日：2004-08-26
申请人： Brian Dymock , Martin Drysdale , Christofe Fromont , Allan Jordan , Xavier Barril-Alonso
发明人： Brian Dymock , Martin Drysdale , Christofe Fromont , Allan Jordan , Xavier Barril-Alonso
IPC分类号： A61K31/5377 , A61K31/519 , C07D498/02
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）的化合物是体外或体内的HSP90活性的抑制剂，并且用于特别是治疗癌症的用途，其中R 2 2是式 - （Ar 1） - （Z） - （Z） - （Alk＆lt; SUP＆gt; 其中Ar 1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 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 中，Z为-O - ， - S - ， - （CO） - ， - （CS） - ， - SO 2 - ， - C（ - -C（-S）NR a - ， - O 2 NR A - ， - O - C（-O） - ， - NR S - 2 - 或-NR A - ，其中R A是氢或C 1 -C 6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 -C 6）烷基，芳基或杂芳基; R 4是羧酸酯，羧酰胺或磺酰胺基。

7. 发明申请

US20070213328A1 Pyridothiophene Compounds 审中-公开
标题翻译：吡啶并噻吩化合物
公开(公告)号：US20070213328A1
公开(公告)日：2007-09-13
申请号：US10574788
申请日：2004-10-05
申请人： Martin Drysdale , Brian Dymock , Xavier Barril-Alonso
发明人： Martin Drysdale , Brian Dymock , Xavier Barril-Alonso
IPC分类号： A61K31/4365 , A61P35/00
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 R2 is a group of formula (IA): -(Ar1)m-(Alk1)p-(Z)r-(Alk2)s-Q (IA) Ar1, Alk1, Z, Alk2 and Q being as defined in the specification; m, p, r and s are independently 0 or 1; 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; 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R 2是式（IA）的基团： - （Z 1） - （Z 1） - （Z 1） - （Z 1） Z（Alk），（Z），Al（k）＆lt; SUP＆gt;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 -C 6）烷基，芳基或杂芳基; R 4是羧酸酯，羧酰胺或磺酰胺基; 或其盐，N-氧化物，水合物或溶剂合物。

8. 发明申请

US20070112192A1 3-(2-Hydroxy-phenyl)-1h-pyrazole-4-carboxylic acid amide derivatives as hsp90 inhibitors for the treatment of cancer 失效
标题翻译： 3-（2-羟基 - 苯基）-1H-吡唑-4-羧酸酰胺衍生物作为治疗癌症的hsp90抑制剂
公开(公告)号：US20070112192A1
公开(公告)日：2007-05-17
申请号：US10536898
申请日：2003-12-04
申请人： Mandy Beswick , Paul Brough , Martin Drysdale , Brian Dymock
发明人： Mandy Beswick , Paul Brough , Martin Drysdale , Brian Dymock
IPC分类号： C07D413/00
CPC分类号： C07D231/14 , C07D401/12 , C07D405/12 , C07D409/12
摘要： Compounds of formula (IA) or (IB) or salts, N-oxides. hydrates or solvates thereof are Inhibitors of HSP90, and useful in the treatment of, for example, cancer: formula (IA), formula (IB) wherein Ar is an aryl or heteroaryl radical which is linked via a ring carbon, and which is substituted by a hydroxy group on a carbon in the 2-position, and which is otherwise either unsubstituted or optionally substituted; R1 is hydrogen or optionally substituted C1-C6 alkyl; R2 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6alkenyl, or C1-C6 alkynyl; or a carboxyl, carboxamide or carboxyl ester group; and R3 is a carboxamide group.
摘要翻译：式（IA）或（IB）的化合物或其盐，N-氧化物。水合物或溶剂化物是HSP90的抑制剂，可用于治疗例如癌症：式（IA），式（IB）其中Ar是通过环碳连接且被取代的芳基或杂芳基通过2-位上的碳上的羟基，其另外是未取代的或任选被取代的; R 1是氢或任选取代的C 1 -C 6烷基; R 2是氢，任选取代的环烷基，环烯基，C 1 -C 6烷基，C 1 -C C 6链烯基或C 1 -C 6炔基; 或羧基，羧酰胺或羧基酯基团; R 3是甲酰胺基。

9. 发明授权

US08916591B2 Indolyl-pyridone derivatives having checkpoint kinase 1 inhibitory activity 有权
标题翻译：具有检查点激酶1抑制活性的吲哚基 - 吡啶酮衍生物
公开(公告)号：US08916591B2
公开(公告)日：2014-12-23
申请号：US12812791
申请日：2009-01-20
申请人： Stephen Stokes , Nicolas Foloppe , Andrea Fiumana , Martin Drysdale , Simon Bedford , Paul Webb
发明人： Stephen Stokes , Nicolas Foloppe , Andrea Fiumana , Martin Drysdale , Simon Bedford , Paul Webb
IPC分类号： A61K31/4439 , C07D401/14
CPC分类号： C07D401/14 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/5377 , C07D413/14
摘要： Compounds of formula (I) have checkpoint kinase 1 (CHK1) inhibitory activity: wherein R1, R2, R5 and R6 are independently selected from hydrogen, hydroxy, methyl, trifluoromethyl, hydroxymethyl, methoxy, trifluoromethoxy, methylamino and dimethylamino; R3, and R4 are independently selected from hydrogen, hydroxy, C1-C3 alkyl, fluoro-(C1-C3)-alkyl, hydroxy-(C1C3)-alkyl, C1-C3 alkoxy, fluoro-(C1-C3)-alkoxy, hydroxy-(C1-C3)-alkoxy, -AIk-N(R11)—R12, -0-AIk-N(R11)—R12, —C(═O)OH, carboxy-(C1-C3)-alkyl, or —C(═O)—NH—R13; AIk is a straight or branched chain divalent C1-C6 alkylene radical; R7 and R8 are independently selected from hydrogen, hydroxy, or C1-C3 alkoxy; X is a straight chain divalent C1-C3 alkylene radical, optionally substituted on one or more carbons by R9 and/or R10; W is selected from —C(═O)—N(—R16)— or —N(—R17)—C(═O)—; Y is hydrogen, C1-C3 alkyl, C1-C3 alkoxy, or halo; and Q is selected from optionally substituted phenyl, optionally substituted cyclohexyl, or an optionally substituted 6-membered monocyclic heteroaryl ring.
摘要翻译：式（I）化合物具有检测点激酶1（CHK1）抑制活性：其中R1，R2，R5和R6独立地选自氢，羟基，甲基，三氟甲基，羟甲基，甲氧基，三氟甲氧基，甲基氨基和二甲基氨基; R 3和R 4独立地选自氢，羟基，C 1 -C 3烷基，氟 - （C 1 -C 3） - 烷基，羟基 - （C 1 -C 3） - 烷基，C 1 -C 3烷氧基，氟 - （C 1 -C 3） - 烷氧基，羟基 - （C1-C3） - 烷氧基，-Ik-N（R11）-R12，-O-Alk-N（R11）-R12，-C（= O）OH，羧基 - （C1-C3） - 烷基，或-C（= O）-NH-R 13; Alk是直链或支链二价C1-C6亚烷基; R 7和R 8独立地选自氢，羟基或C 1 -C 3烷氧基; X是直链的二价C1-C3亚烷基，任选地被一个或多个碳上被R9和/或R10取代; W选自-C（= O）-N（-R 16） - 或-N（-R 17）-C（= O） - ; Y是氢，C 1 -C 3烷基，C 1 -C 3烷氧基或卤素; 并且Q选自任选取代的苯基，任选取代的环己基或任选取代的6元单环杂芳基环。

10. 发明申请

US20110021498A1 INDOLYL- PYRIDONE DERIVATIVES HAVING CHECKPOINT KINASE 1 INHIBITORY ACTIVITY 有权
标题翻译：具有检测点激酶1的吲哚基 - 吡啶酮衍生物1抑制活性
公开(公告)号：US20110021498A1
公开(公告)日：2011-01-27
申请号：US12812791
申请日：2009-01-20
申请人： Stephen Stokes , Nicolas Foloppe , Andrea Fiumana , Martin Drysdale , Simon Bedford , Paul Webb
发明人： Stephen Stokes , Nicolas Foloppe , Andrea Fiumana , Martin Drysdale , Simon Bedford , Paul Webb
IPC分类号： A61K31/397 , A61P35/00 , A61P19/02 , C07D401/14 , A61K31/4439 , A61K31/444 , A61K31/4545 , C07D413/14 , A61K31/5377
CPC分类号： C07D401/14 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/5377 , C07D413/14
摘要： Compounds of formula (I) have checkpoint kinase 1 (CHK1) inhibitory activity: wherein R1, R2, R5 and R6 are independently selected from hydrogen, hydroxy, methyl, trifluoromethyl, hydroxymethyl, methoxy, trifluoromethoxy, methylamino and dimethylamino; R3, and R4 are independently selected from hydrogen, hydroxy, C1-C3 alkyl, fluoro-(C1-C3)-alkyl, hydroxy-(C1C3)-alkyl, C1-C3 alkoxy, fluoro-(C1-C3)-alkoxy, hydroxy-(C1-C3)-alkoxy, -AIk-N(R11)—R12, -0-AIk-N(R11)—R12, —C(═O)OH, carboxy-(C1-C3)-alkyl, or —C(═O)—NH—R13; AIk is a straight or branched chain divalent C1-C6 alkylene radical; R7 and R8 are independently selected from hydrogen, hydroxy, or C1-C3 alkoxy; X is a straight chain divalent C1-C3 alkylene radical, optionally substituted on one or more carbons by R9 and/or R10; W is selected from —C(═O)—N(—R16)— or —N(—R17)—C(═O)—; Y is hydrogen, C1-C3 alkyl, C1-C3 alkoxy, or halo; and Q is selected from optionally substituted phenyl, optionally substituted cyclohexyl, or an optionally substituted 6-membered monocyclic heteroaryl ring.
摘要翻译：式（I）化合物具有检测点激酶1（CHK1）抑制活性：其中R1，R2，R5和R6独立地选自氢，羟基，甲基，三氟甲基，羟甲基，甲氧基，三氟甲氧基，甲基氨基和二甲基氨基; R 3和R 4独立地选自氢，羟基，C 1 -C 3烷基，氟 - （C 1 -C 3） - 烷基，羟基 - （C 1 -C 3） - 烷基，C 1 -C 3烷氧基，氟 - （C 1 -C 3） - 烷氧基，羟基 - （C1-C3） - 烷氧基，-Ik-N（R11）-R12，-O-Alk-N（R11）-R12，-C（= O）OH，羧基 - （C1-C3） - 烷基，或-C（= O）-NH-R 13; Alk是直链或支链二价C1-C6亚烷基; R 7和R 8独立地选自氢，羟基或C 1 -C 3烷氧基; X是直链的二价C1-C3亚烷基，任选地被一个或多个碳上被R9和/或R10取代; W选自-C（= O）-N（-R 16） - 或-N（-R 17）-C（= O） - ; Y是氢，C 1 -C 3烷基，C 1 -C 3烷氧基或卤素; 并且Q选自任选取代的苯基，任选取代的环己基或任选取代的6元单环杂芳基环。

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