公开(公告)号：US20110086851A1

公开(公告)日：2011-04-14

申请号：US12993007

申请日：2009-05-13

Applicant: Bernard Golding ,  Richard Franklin

Inventor： Bernard Golding ,  Richard Franklin

IPC: A61K31/519 ,  C07D487/10 ,  A61K31/527 ,  C07D487/20 ,  C07D487/04 ,  C07D498/20 ,  A61K31/5386 ,  C07D491/20 ,  C07D495/20 ,  A61P7/02 ,  A61P9/10

CPC classification number: C07D487/04

Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.

Abstract translation: 本发明涉及具有降低心血管副作用潜力的选择性血小板降低剂阿那格雷的取代类似物的发现，其应该导致改善的患者依从性和治疗骨髓增生性疾病的安全性。 更具体地，本发明涉及具有以下通式的某些咪唑并喹唑啉衍生物，其中取代基具有权利要求1中定义的含义，并且其在人体中可用作血小板降低剂。 本发明的化合物通过抑制巨核细胞吞噬作用并因此起血小板的形成的作用。

公开(公告)号：US20110065735A1

公开(公告)日：2011-03-17

申请号：US12993069

申请日：2009-05-13

Applicant: Bernard Golding ,  Richard Franklin ,  Peter Cicala

Inventor： Bernard Golding ,  Richard Franklin ,  Peter Cicala

IPC: A61K31/517 ,  C07D239/84 ,  A61P7/02

CPC classification number: C07D239/84

Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.

公开(公告)号：US20060106025A1

公开(公告)日：2006-05-18

申请号：US11231041

申请日：2005-09-20

Applicant: Graeme Smith ,  Niall Martin ,  Keith Menear ,  Marc Hummersone ,  Laurent Rigoreau ,  Roger Griffin ,  Bernard Golding ,  David Newell ,  Hilary Calvert ,  Nicola Curtin ,  Ian Hardcastle ,  Kappusamy Saravanan

Inventor： Graeme Smith ,  Niall Martin ,  Keith Menear ,  Marc Hummersone ,  Laurent Rigoreau ,  Roger Griffin ,  Bernard Golding ,  David Newell ,  Hilary Calvert ,  Nicola Curtin ,  Ian Hardcastle ,  Kappusamy Saravanan

IPC: A61K31/496 ,  C07D409/14

CPC classification number: C07D413/14 ,  C07D409/04 ,  C07D409/14

Abstract: A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R1 and R2 are independently selected from hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; Q is —NH—C(═O)— or —O—; Y is an optionally substituted C1-5 alkylene group; X is selected from SR3 or NR4R5, wherein, R3, or R4 and R5 are independently selected from hydrogen, optionally substituted C1-7 alkyl, C5-20 aryl, or C3-20 heterocyclyl groups, or R4 and R5 may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; if Q is —O—, X is additionally selected from —C(═O)—NR6R7, wherein R6 and R7 are independently selected from hydrogen, optionally substituted C1-7 alkyl, C5-20 aryl, or C3-20 heterocyclyl groups, or R6 and R7 may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; and if Q is —NH—C(═O)—, —Y—X may additionally be selected from C1-7 alkyl.

Abstract translation: 式I化合物及其异构体，盐，溶剂合物，化学保护形式及其前药，其中：R 1和R 2独立地选自氢，任选地 取代的C 1-7烷基，C 3-20杂环基或C 5-20-20芳基，或者可以一起形成 与它们所连接的氮原子一起形成具有4至8个环原子的任选取代的杂环; Q是-NH-C（-O） - 或-O-; Y是任选取代的C 1-5亚烷基; X选自SR 3或NR 4 R 5，其中R 3，R 3，R 3， 4和R 5独立地选自氢，任选取代的C 1-7 - 烷基，C 5-20-20芳基，或 C 3-20杂环基或R 4和R 5可以一起与它们所连接的氮原子一起形成一个 具有4至8个环原子的任选取代的杂环; 如果Q是-O-，X另外选自-C（-O）-NR 6 R 7，其中R 6和R 独立地选自氢，任选取代的C 1-7 - 烷基，C 5-20-20芳基或C 3-20 或者R 6和R 7可以与它们所连接的氮原子一起形成任选取代的杂环，其具有4个 至8个环原子; 并且如果Q是-NH-C（-O） - ，-Y-X可另外选自C 1-7烷基。

公开(公告)号：US20110130405A1

公开(公告)日：2011-06-02

申请号：US12992997

申请日：2009-05-13

Applicant: Bernard Golding ,  Richard Franklin ,  Kim Hirst

Inventor： Bernard Golding ,  Richard Franklin ,  Kim Hirst

IPC: A61K31/519 ,  C07D239/00 ,  A61P7/02

CPC classification number: C07D495/14 ,  C07D471/14 ,  C07D487/14 ,  C07D491/147

Abstract: This invention relates to the discovery of 3-and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula (I) shown below wherein the meanings of the substituents are defined in claim 1 and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.

Abstract translation: 本发明涉及降低心血管副作用潜力的选择性血小板降低剂阿那格雷的3-取代类似物和5-取代的类似物，其应该导致改善的患者依从性和治疗骨髓增生性疾病的安全性。 更具体地，本发明涉及具有下面通式（I）的某些咪唑并喹唑啉衍生物，其中取代基的含义在权利要求1中定义，并且其在人体中可用作血小板降低剂。 本发明的化合物通过抑制巨核细胞吞噬作用并因此起血小板的形成的作用。

公开(公告)号：US20110071172A1

公开(公告)日：2011-03-24

申请号：US12993044

申请日：2009-05-13

Applicant: Bernard Golding ,  Richard Franklin

Inventor： Bernard Golding ,  Richard Franklin

IPC: A61K31/519 ,  C07D487/04 ,  C07D513/04 ,  A61P7/02 ,  A61P35/00 ,  A61P7/00

CPC classification number: C07D487/04 ,  C07D513/04

Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim (I): and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.

Abstract translation: 本发明涉及具有降低心血管副作用潜力的选择性血小板降低剂阿那格雷的取代类似物的发现，其应该导致改善的患者依从性和治疗骨髓增生性疾病的安全性。 更具体地说，本发明涉及具有下述通式的某些咪唑并喹唑啉衍生物，其中取代基具有权利要求（I）中定义的含义：并且其在人体中具有作为血小板降低剂的功效。 本发明的化合物通过抑制巨核细胞吞噬作用并因此起血小板的形成的作用。

公开(公告)号：US20110065714A1

公开(公告)日：2011-03-17

申请号：US12993033

申请日：2009-05-13

Applicant: Bernard Golding ,  Peter Cicala ,  Richard Franklin ,  Kim Hirst

Inventor： Bernard Golding ,  Peter Cicala ,  Richard Franklin ,  Kim Hirst

IPC: A61K31/519 ,  C07D471/04 ,  A61P7/02 ,  C07D491/048 ,  C07D487/04 ,  A61K31/5025 ,  C07D475/04

CPC classification number: C07D471/04 ,  C07D475/04 ,  C07D491/048 ,  C07D495/04

Abstract: This invention relates to the discovery of 3-and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.

Abstract translation: 本发明涉及降低心血管副作用潜力的选择性血小板降低剂阿那格雷的3-取代类似物和5-取代的类似物的发现，其应该导致改善的患者依从性和治疗骨髓增生性疾病的安全性。 更具体地，本发明涉及具有以下通式的某些咪唑并喹唑啉衍生物，其中取代基具有权利要求1中定义的含义，并且其在人体中可用作血小板降低剂。 本发明的化合物通过抑制巨核细胞吞噬作用并因此起血小板的形成的作用。

公开(公告)号：US20050107367A1

公开(公告)日：2005-05-19

申请号：US10486811

申请日：2002-08-14

Applicant: Niall Martin ,  Graeme Cameron Smith ,  Roger Griffin ,  Bernard Golding ,  Ian Hardcastle ,  Laurent Rigoreau ,  David Newell ,  Hilary Calvert ,  Nicola Curtin ,  Paul Workman ,  Florence Raynaud ,  Bernard Nutley

Inventor： Niall Martin ,  Graeme Cameron Smith ,  Roger Griffin ,  Bernard Golding ,  Ian Hardcastle ,  Laurent Rigoreau ,  David Newell ,  Hilary Calvert ,  Nicola Curtin ,  Paul Workman ,  Florence Raynaud ,  Bernard Nutley

IPC: C12N9/99 ,  A61K31/5377 ,  A61P31/12 ,  A61P35/00 ,  A61P43/00 ,  C07D335/02 ,  C07D409/10 ,  A61K31/541 ,  A61K31/496 ,  C07D413/04 ,  C07D417/04 ,  C07D49/04

CPC classification number: C07D335/02

Abstract: The present invention provides compounds of formula (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein R1 and R2 are independently hydrogen, an option ally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; and R3 is an optionally substituted C3-20 heterocyclyl or C5-20 aryl group, and their use as pharmaceuticals, particularly in treating diseases which are retroviral mediated or ameliorated by the inhibition of DNA-PK,

Abstract translation: 本发明提供式（I）化合物及其异构体，盐，溶剂化物，化学保护形式及其前药，其中R 1和R 2独立地为氢， 选择性地取代C 1-7烷基，C 3-20杂环基或C 5-20-20芳基，或可一起形成 与它们所连接的氮原子一起形成具有4-8个环原子的任选取代的杂环; 并且R 3是任选取代的C 3-20杂环基或C 5-20芳基，并且它们作为药物的用途，特别是在治疗 通过抑制DNA-PK介导或改善的逆转录病毒的疾病，

公开(公告)号：US20110263850A1

公开(公告)日：2011-10-27

申请号：US13132001

申请日：2009-11-30

Applicant: Bernard Golding

Inventor： Bernard Golding

IPC: C07D487/04 ,  C07C227/18

CPC classification number: C07D487/04 ,  C07C201/08 ,  C07C201/12 ,  C07C227/16 ,  C07C227/18 ,  C07C303/28 ,  C07C309/66 ,  C07C229/14 ,  C07C205/44 ,  C07C205/26

Abstract: The present invention relates to a novel process for producing quinazoline compounds which are useful in therapy. More specifically, the compounds produced by the process of the invention are useful in the treatment of a number of cardiovascular diseases. The process of the invention provides 6,7-dichloro-1,5- dihydroimidazo [2,1 -b] quinazolin 2 (3H)-one, more commonly known as anagrelide and its analogues in a clean and efficient manner.

Abstract translation: 本发明涉及可用于治疗的喹唑啉化合物的新方法。 更具体地，通过本发明的方法生产的化合物可用于治疗许多心血管疾病。 本发明的方法以清洁和有效的方式提供了6,7-二氯-1,5-二氢咪唑并[2,1-b]喹唑啉2（3H） - 酮，更通常称为阿那格雷及其类似物。

公开(公告)号：US20110071174A1

公开(公告)日：2011-03-24

申请号：US12993064

申请日：2009-05-13

Applicant: Bernard Golding ,  Richard Franklin

Inventor： Bernard Golding ,  Richard Franklin

IPC: A61K31/519 ,  C07D239/00 ,  C07D471/04 ,  A61K31/437 ,  A61P7/02 ,  A61P35/00

CPC classification number: C07D487/04

Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.

Abstract translation: 本发明涉及具有降低心血管副作用潜力的选择性血小板降低剂阿那格雷的取代类似物的发现，其应该导致改善的患者依从性和治疗骨髓增生性疾病的安全性。 更具体地，本发明涉及具有以下通式的某些咪唑并喹唑啉衍生物，其中取代基具有权利要求1中定义的含义，并且其在人体中可用作血小板降低剂。 本发明的化合物通过抑制巨核细胞吞噬作用并因此起血小板的形成的作用。

公开(公告)号：US20060264623A1

公开(公告)日：2006-11-23

申请号：US11403763

申请日：2006-04-13

Applicant: Graeme Smith ,  Niall Martin ,  Keith Menear ,  Marc Hummersone ,  Xiao-ling Cockcroft ,  Mark Frigerio ,  Roger Griffin ,  Bernard Golding ,  Ian Hardcastle ,  David Newell ,  Hilary Calvert ,  Nicola Curtin ,  Marine Desage-El Murr

Inventor： Graeme Smith ,  Niall Martin ,  Keith Menear ,  Marc Hummersone ,  Xiao-ling Cockcroft ,  Mark Frigerio ,  Roger Griffin ,  Bernard Golding ,  Ian Hardcastle ,  David Newell ,  Hilary Calvert ,  Nicola Curtin ,  Marine Desage-El Murr

IPC: C07D413/00

CPC classification number: C07D413/00 ,  C07D401/14 ,  C07D405/04 ,  C07D407/04 ,  C07D407/14 ,  C07D409/04 ,  C07D471/04

Abstract: Compounds of formula l: wherein A, B and D are respectively selected from the group consisting of: (i) CH, NH, C; (ii) CH, N, N;and (iii) CH, O, C; are disclosed for use in inhibiting DNA-PK.

Abstract translation: 式I化合物：其中A，B和D分别选自：（i）CH，NH，C; （ii）CH，N，N;和（iii）CH，O，C; 被公开用于抑制DNA-PK。