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1. 发明申请

US20130012485A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：US20130012485A1
公开(公告)日：2013-01-10
申请号：US12520323
申请日：2007-12-20
申请人： Daniel Kaspar Bäschlin , Richard Sedrani , Stefanie Flohr , Kenji Namoto , Nils Ostermann , Finton Sirockin , François Gessier , Garry Fenton , Mandy Christine Beswick , David Edward Clark , Bohdan Waszkowycz
发明人： Daniel Kaspar Bäschlin , Richard Sedrani , Stefanie Flohr , Kenji Namoto , Nils Ostermann , Finton Sirockin , François Gessier , Garry Fenton , Mandy Christine Beswick , David Edward Clark , Bohdan Waszkowycz
IPC分类号： A61K31/135 , A61K31/568 , A61K31/565 , C07C217/52 , C07D487/04 , A61K31/4985 , C07D211/08 , A61K31/451 , C07D295/135 , A61K31/495 , C07D401/04 , A61K31/4545 , A61K31/454 , C07D243/08 , A61K31/551 , C07D223/04 , A61K31/55 , A61K31/501 , C07D237/14 , A61K31/50 , A61P3/10 , A61P19/02 , A61P3/04 , A61P19/10 , A61P9/04 , A61P25/28 , A61P13/12 , A61P3/06 , A61P9/10 , A61P29/00 , A61P25/00 , A61P35/04 , A61P9/12 , A61P25/22 , A61P5/00 , C07C215/42
CPC分类号： C07C215/42 , C07C211/29 , C07C211/31 , C07C211/40 , C07C215/14 , C07C217/16 , C07C217/52 , C07C229/16 , C07C233/41 , C07C237/10 , C07C237/24 , C07C237/36 , C07C255/24 , C07C271/20 , C07C311/07 , C07C311/08 , C07C311/20 , C07C311/29 , C07C317/32 , C07C317/44 , C07C2601/02 , C07C2601/14 , C07D207/404 , C07D211/14 , C07D211/60 , C07D213/64 , C07D213/81 , C07D213/82 , C07D233/36 , C07D237/14 , C07D237/24 , C07D239/10 , C07D239/90 , C07D263/20 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/14 , C07D409/04 , C07D471/04 , C07D487/04
摘要： Compounds of the formula (I) are provided: wherein V, W, X, Y, Z, R3, R4, R5, R6, R7 and m are as defined in the specification; and pharmaceutically acceptable salts and prodrugs thereof. The compounds may be useful in the treatment or prevention of various diseases and conditions in which dipeptidylpeptidase-IV (DPP-IV) is implicated.
摘要翻译：提供式（I）化合物：其中V，W，X，Y，Z，R 3，R 4，R 5，R 6，R 7和m如说明书中所定义; 及其药学上可接受的盐和前药。该化合物可用于治疗或预防涉及二肽基肽酶-IV（DPP-IV）的各种疾病和病症。

2. 发明授权

US07803831B2 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：US07803831B2
公开(公告)日：2010-09-28
申请号：US10536898
申请日：2003-12-04
申请人： Mandy Christine Beswick , Paul Andrew Brough , Martin James Drysdale , Brian William Dymock
发明人： Mandy Christine Beswick , Paul Andrew Brough , Martin James Drysdale , Brian William Dymock
IPC分类号： A61K31/415 , A61K31/4155 , C07D401/12 , C07D403/12
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）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为通过环碳连接并被2-位上的碳上的羟基取代的芳基或杂芳基，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 6链烯基或C 1 -C 6炔基; 或羧基，羧酰胺或羧基酯基团; 并且R 3是羧酰胺基。

3. 发明授权

US08168633B2 Thiazolopyrimidines and their use as inhibitors of phosphatidylinositol-3 kinase 有权
标题翻译：噻唑并嘧啶及其作为磷脂酰肌醇-3激酶抑制剂的用途
公开(公告)号：US08168633B2
公开(公告)日：2012-05-01
申请号：US12986317
申请日：2011-01-07
申请人： Timothy Colin Hancox , Neil Anthony Pegg , Mandy Christine Beswick , Toby Jonathan Blench , Elsa Amandine Dechaux , Jahusz Jozef Kulagowski , Alan John Nadin , Stephen Price
发明人： Timothy Colin Hancox , Neil Anthony Pegg , Mandy Christine Beswick , Toby Jonathan Blench , Elsa Amandine Dechaux , Jahusz Jozef Kulagowski , Alan John Nadin , Stephen Price
IPC分类号： A61K31/5377
CPC分类号： C07D513/04
摘要： Thiazolopyrimidine compounds of formula I, where W represents a thiazole ring, selectively inhibit the p110 delta subtype of PI3 Kinase (PI3K), and are useful for treating diseases and disorders arising from abnormal cell growth, function or behavior associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
摘要翻译：式I的噻唑并嘧啶化合物，其中W表示噻唑环，选择性地抑制PI3激酶（PI3K）的p110δ亚型，并且可用于治疗由与PI3激酶例如癌症相关的异常细胞生长，功能或行为引起的疾病和障碍，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌功能障碍和神经障碍。

4. 发明申请

US20100305065A1 USE OF 4-(PYRROLIDIN-1-YL)QUINOLINE COMPOUNDS TO KILL CLINICALLY LATENT MICROORGANISMS 有权
标题翻译：使用4-（吡咯烷-1-基）喹啉化合物杀死临床微生物
公开(公告)号：US20100305065A1
公开(公告)日：2010-12-02
申请号：US12600470
申请日：2008-05-16
申请人： Mandy Christine Beswick , Susan Mary Cramp , Yanmin Hu , Thomas David Pallin , Hazel Joan Dyke , Anthony Coates
发明人： Mandy Christine Beswick , Susan Mary Cramp , Yanmin Hu , Thomas David Pallin , Hazel Joan Dyke , Anthony Coates
IPC分类号： A61K31/7028 , C07D401/04 , A61K31/4709 , C07D403/14 , A61K31/497 , A61K31/65 , A61K31/665 , A61K31/56 , A61P31/04 , A61P31/00 , A61P31/06 , A61P17/10 , A61P1/04 , A61P17/02
CPC分类号： A61K31/4709 , A61K31/497 , A61K31/501 , A61K31/517 , C07D401/04 , C07D403/14 , Y02A50/401 , Y02A50/404 , Y02A50/406 , Y02A50/469 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/479 , Y02A50/481 , Y02A50/483
摘要： There is provided the use of compounds of formula wherein R1, R2, R3 and E have meanings given in the description, for the preparation of a medicament for killing clinically latent microorganisms. There is also provided the use of compounds of formula I for treating microbial infections, as well as certain compounds of formula (I) per se.
摘要翻译：提供了下式化合物的用途，其中R1，R2，R3和E具有描述中给出的含义，用于制备用于杀死临床潜在微生物的药物。还提供了式I化合物用于治疗微生物感染的用途，以及某些式（I）化合物本身。

5. 发明授权

US08759348B2 Use of 4-(pyrrolidin-1-yl)quinoline compounds to kill clinically latent microorganisms 有权
标题翻译：使用4-（吡咯烷-1-基）喹啉化合物杀死临床潜在的微生物
公开(公告)号：US08759348B2
公开(公告)日：2014-06-24
申请号：US12600470
申请日：2008-05-16
申请人： Mandy Christine Beswick , Susan Mary Cramp , Yanmin Hu , Thomas David Pallin , Hazel Joan Dyke , Anthony Coates
发明人： Mandy Christine Beswick , Susan Mary Cramp , Yanmin Hu , Thomas David Pallin , Hazel Joan Dyke , Anthony Coates
IPC分类号： A61K31/4709 , A61K31/497 , A61K31/501 , C07D401/14 , C07D403/14 , C07D401/04
CPC分类号： A61K31/4709 , A61K31/497 , A61K31/501 , A61K31/517 , C07D401/04 , C07D403/14 , Y02A50/401 , Y02A50/404 , Y02A50/406 , Y02A50/469 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/479 , Y02A50/481 , Y02A50/483
摘要： There is provided the use of compounds of formula wherein R1, R2, R3 and E have meanings given in the description, for the preparation of a medicament for killing clinically latent microorganisms. There is also provided the use of compounds of formula I for treating microbial infections, as well as certain compounds of formula (I) per se.
摘要翻译：提供了下式化合物的用途，其中R1，R2，R3和E具有描述中给出的含义，用于制备用于杀死临床潜在微生物的药物。还提供了式I化合物用于治疗微生物感染的用途，以及某些式（I）化合物本身。

6. 发明授权

US07612201B2 Pyrazole compounds 失效
标题翻译：吡唑化合物
公开(公告)号：US07612201B2
公开(公告)日：2009-11-03
申请号：US10536899
申请日：2003-12-18
申请人： Mandy Christine Beswick , Martin James Drysdale , Brian William Dymock , Edward McDonald
发明人： Mandy Christine Beswick , Martin James Drysdale , Brian William Dymock , Edward McDonald
IPC分类号： C07D231/38 , C07D401/04 , C07D403/04 , C07D405/12 , C07D409/12 , C07D417/12
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.
摘要翻译：式（IA）或（IB）化合物或其盐，N-氧化物，水合物或溶剂合物是HSP90的抑制剂，并且在治疗对HSP90抑制作用的疾病如癌症的治疗中具有价值。在式中，Ar是芳基，（C 1 -C 6烷基），芳基（C 1 -C 6烷基），杂芳基，杂芳基芳基（C 1 -C 6烷基）或杂芳基芳基（C 1 -C 6烷基）在其芳基或杂芳基部分取代; R1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 6烯基或C 1 -C 6炔基; 或羧基，羧酰胺或羧基酯基团; 环A是非芳族碳环或杂环，其中（i）环碳任选被取代，和/或（ii）环氮任选地被式 - （Alk1）p（Cyc）n-（ Alk3）m-（Z）r（Alk2）sQ其中Alk1，Alk2和Alk3是任选取代的C 1 -C 3烷基，Cyc是任选取代的碳环或杂环基; m，n，p，r和s独立地为0或1，Z为-O - ， - S - ， - （CO） - ， - SO2-，-C - ，-NW-， - C（ - O）NRA - ， - NRAC（-O） - ， - SO2NRA-或-NRASO2-，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。

7. 发明申请

US20110098270A1 THIAZOLOPYRIMIDINES AND THEIR USE AS INHIBITORS OF PHOSPHATIDYLINOSITOL-3 KINASE 有权
标题翻译：噻唑啉酮和它们作为磷脂酰肌醇-3激酶的抑制剂
公开(公告)号：US20110098270A1
公开(公告)日：2011-04-28
申请号：US12986317
申请日：2011-01-07
申请人： Timothy Colin Hancox , Neil Anthony Pegg , Mandy Christine Beswick , Toby Jonathan Blench , Elsa Amandine Dechaux , Jahusz Jozef Kulagowski , Alan John Nadin , Stephen Price
发明人： Timothy Colin Hancox , Neil Anthony Pegg , Mandy Christine Beswick , Toby Jonathan Blench , Elsa Amandine Dechaux , Jahusz Jozef Kulagowski , Alan John Nadin , Stephen Price
IPC分类号： A61K31/397 , A61K31/5377 , A61P35/00
CPC分类号： C07D513/04
摘要： Thiazolopyrimidine compounds of formula I, where W represents a thiazole ring, selectively inhibit the p110 delta subtype of PI3 Kinase (PI3K), and are useful for treating diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
摘要翻译：式I的噻唑并嘧啶化合物，其中W表示噻唑环，选择性地抑制PI3激酶（PI3K）的p110δ亚型，并且可用于治疗由与PI3激酶例如癌症相关的异常细胞生长，功能或行为引起的疾病和障碍，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌功能障碍和神经障碍。

8. 发明授权

US07893060B2 Thiazolopyrimidines and their use as inhibitors of phosphatidylinositol-3 kinase 有权
标题翻译：噻唑并嘧啶及其作为磷脂酰肌醇-3激酶抑制剂的用途
公开(公告)号：US07893060B2
公开(公告)日：2011-02-22
申请号：US12663823
申请日：2008-06-12
申请人： Timothy Colin Hancox , Neil Anthony Pegg , Mandy Christine Beswick , Toby Jonathan Blench , Elsa Amandine Dechaux , Janusz Jozef Kulagowski , Alan John Nadin , Stephen Price
发明人： Timothy Colin Hancox , Neil Anthony Pegg , Mandy Christine Beswick , Toby Jonathan Blench , Elsa Amandine Dechaux , Janusz Jozef Kulagowski , Alan John Nadin , Stephen Price
IPC分类号： A61K31/5377 , C07D413/14
CPC分类号： C07D513/04
摘要： Thiazolopyrimidines of formula (I): wherein W represents a thiazole ring; R1 and R2 form, together with the N atom to which they are attached, a group of the following formula (IIa): in which A is a ring system; m is 0, 1 or 2; R3 is H or C1-C6 alkyl; and R4 is an indole group which is unsubstituted or substituted; and the pharmaceutically acceptable salts thereof are inhibitors of PI3K and are selective for the p110δ isoform, which is a class Ia PD kinase, over both other class Ia and class Ib kinases. The compounds may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
摘要翻译：式（I）的噻唑并嘧啶：其中W表示噻唑环; R1和R2与它们所连接的N原子一起形成下式（IIa）的基团：其中A是环系; m为0,1或2; R3是H或C1-C6烷基; R4是未取代或取代的吲哚基; 其药学上可接受的盐是PI3K的抑制剂，并且对于其它1a类和1b类激酶对p110δ同种型是Ia Ia激酶的选择性。该化合物可用于治疗与PI3激酶例如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌功能障碍和神经障碍相关的异常细胞生长，功能或行为引起的疾病和障碍。

9. 发明申请

US20100190769A1 THIAZOLOPYRIMIDINES AND THEIR USE AS INHIBITORS OF PHOSPHATIDYLINOSITOL-3 KINASE 有权
标题翻译：噻唑啉酮和它们作为磷脂酰肌醇-3激酶的抑制剂
公开(公告)号：US20100190769A1
公开(公告)日：2010-07-29
申请号：US12663823
申请日：2008-06-12
申请人： Timothy Colin Hancox , Neil Anthony Pegg , Mandy Christine Beswick , Toby Jonathan Blench , Elsa Amandine Dechaux , Janusz Jozef Kulagowski , Alan John Nadin , Stephen Price
发明人： Timothy Colin Hancox , Neil Anthony Pegg , Mandy Christine Beswick , Toby Jonathan Blench , Elsa Amandine Dechaux , Janusz Jozef Kulagowski , Alan John Nadin , Stephen Price
IPC分类号： A61K31/5377 , C07D413/14 , A61P35/00 , A61P37/00 , A61P9/00 , A61P31/12 , A61P29/00 , A61P3/00 , A61P5/00 , A61P25/00
CPC分类号： C07D513/04
摘要： Thiazolopyrimidines of formula (I): wherein W represents a thiazole ring; R1 and R2 form, together with the N atom to which they are attached, a group of the following formula (IIa): in which A is a ring system; m is 0, 1 or 2; R is H or C1-C6 alkyl; and R is an indole group which is unsubstituted or substituted; and the pharmaceutically acceptable salts thereof are inhibitors of PI3K and are selective for the p110δ isoform, which is a class Ia PD kinase, over both other class Ia and class Ib kinases. The compounds may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
摘要翻译：式（I）的噻唑并嘧啶：其中W表示噻唑环; R1和R2与它们所连接的N原子一起形成下式（IIa）的基团：其中A是环系; m为0,1或2; R是H或C 1 -C 6烷基; 并且R是未取代或取代的吲哚基; 并且其药学上可接受的盐是PI3K的抑制剂，并且对于其它Ia类和1b类激酶对p110δ同种型是Ia Ia激酶的选择性。该化合物可用于治疗与PI3激酶例如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌功能障碍和神经障碍相关的异常细胞生长，功能或行为引起的疾病和障碍。

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