公开(公告)号：US20100278835A1

公开(公告)日：2010-11-04

申请号：US12720094

申请日：2010-03-09

申请人： Helen Blade ,  Heather Marie Jackson ,  Gary Peter Tomkinson ,  Elisa Ann Carron ,  James Andrew Lumley ,  Christopher John Pilkington ,  Alexander James Floyd Thomas ,  Justin Warne

发明人： Helen Blade ,  Heather Marie Jackson ,  Gary Peter Tomkinson ,  Elisa Ann Carron ,  James Andrew Lumley ,  Christopher John Pilkington ,  Alexander James Floyd Thomas ,  Justin Warne

IPC分类号： A61K31/519 ,  C07D403/06 ,  A61K31/517 ,  C07D471/04 ,  A61P31/14 ,  A61P11/00 ,  A61K39/42

CPC分类号： C07D403/06 ,  C07D471/04

摘要： The invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are as defined in the specification, and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are useful in the treatment of respiratory syncytial virus (RSV).

摘要翻译： 本发明提供式（I）化合物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10，R 11和R 12如本说明书中所定义，及其旋光异构体，外消旋体和互变异构体， 其药学上可接受的盐; 以及其制备方法，含有它们的药物组合物及其在治疗中的用途。 该化合物可用于治疗呼吸道合胞病毒（RSV）。

公开(公告)号：US20090318427A1

公开(公告)日：2009-12-24

申请号：US12067318

申请日：2005-09-19

申请人： Helena Dennison ,  Justin Warne ,  Keith Spencer ,  George Cockerill ,  James Lumley

发明人： Helena Dennison ,  Justin Warne ,  Keith Spencer ,  George Cockerill ,  James Lumley

IPC分类号： A61K31/5513 ,  A61P31/12 ,  C07D243/24

CPC分类号： C07D243/24 ,  A61K31/5513

摘要： Use of a benzodiazepine of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in treating or preventing a hepatitis C infection, wherein: —R1 represents C1-6 alkyl, aryl or heteroaryl; —R2 represents hydrogen or C1-6 alkyl; —each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano, —CO2R′, —CONR′R″, —NH—C0-R′, —S(O)R′, —S(O)2R′, —NH—S(O)2R′, —S(O)NR′R″ or —S(O)2NR′R″, wherein each R′ and R″ is the same or different and represents hydrogen or C1-6 alkyl; —n is from 0 to 3; —R4 represents hydrogen or C1-6 alkyl; —R5 represents C1-6alkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 hydroxyalkyl)-, heteroaryl-(C1-6hydroxyalkyl)-, carbocyclyl-(C1-6 hydroxyalkyl)-, heterocyclyl-(C1-6hydroxyalkyl)-, aryl-C(O)—C(O)—, heteroaryl-C(O)—C(O)—, carbocyclyl-C(O)—C(O)—, heterocyclyl-C(O)—C(O)— or —XR6; —X represents —CO—, —S(O)— or —S(O)2—; and —R6 represents C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkylthio, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 alkyl)-O—, heteroaryl-(C1-6 alkyl)-O—, carbocyclyl-(C1-6 alkyl)-O—, heterocyclyl-(C1-6 alkyl)-O— or —NR′R″ wherein each R′ and R″ is the same or different and represents hydrogen, C1-6 alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)- or heterocyclyl-(C1-6 alkyl)-.

公开(公告)号：US20060089359A1

公开(公告)日：2006-04-27

申请号：US11233311

申请日：2005-09-23

申请人： Edward Boyd ,  Frederick Brookfield ,  Guy Georges ,  Bernhard Goller ,  Sabine Huensch ,  Petra Rueger ,  Matthias Rueth ,  Stefan Scheiblich ,  Christine Schuell ,  Wolfgang von der Saal ,  Justin Warne ,  Stefan Weigand

发明人： Edward Boyd ,  Frederick Brookfield ,  Guy Georges ,  Bernhard Goller ,  Sabine Huensch ,  Petra Rueger ,  Matthias Rueth ,  Stefan Scheiblich ,  Christine Schuell ,  Wolfgang von der Saal ,  Justin Warne ,  Stefan Weigand

IPC分类号： A61K31/502 ,  C07D403/02

CPC分类号： C07D403/12

摘要： Compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates are disclosed. Also disclosed are methods for the preparation of the above-mentioned compounds, pharmaceutical compositions containing them, as well as the use of the above-mentioned compounds in the treatment, control or prevention of illnesses such as cancer.

摘要翻译： 公开了式I化合物的药学上可接受的盐，对映体形式，非对映异构体和外消旋体。 还公开了制备上述化合物的方法，含有它们的药物组合物，以及上述化合物在治疗，控制或预防诸如癌症等疾病中的用途。

公开(公告)号：US08039616B2

公开(公告)日：2011-10-18

申请号：US12067318

申请日：2005-09-19

申请人： Helena Dennison ,  Justin Warne ,  Keith Spencer ,  George Cockerill ,  James Lumley

发明人： Helena Dennison ,  Justin Warne ,  Keith Spencer ,  George Cockerill ,  James Lumley

IPC分类号： C07D243/12 ,  A61K31/55

CPC分类号： C07D243/24 ,  A61K31/5513

摘要： Use of a benzodiazepine of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in treating or preventing a hepatitis C infection, wherein: —R1 represents C1-6 alkyl, aryl or heteroaryl; —R2 represents hydrogen or C1-6 alkyl; —each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano, —CO2R′, —CONR′R″, —NH—CO—R′, —S(O)R′, —S(O)2R′, —NH—S(O)2R′, —S(O)NR′R″ or —S(O)2NR′R″, wherein each R′ and R″ is the same or different and represents hydrogen or C1-6 alkyl; —n is from 0 to 3; —R4 represents hydrogen or C1-6 alkyl; —R5 represents C1-6alkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 hydroxyalkyl)-, heteroaryl-(C1-6hydroxyalkyl)-, carbocyclyl-(C1-6 hydroxyalkyl)-, heterocyclyl-(C1-6hydroxyalkyl)-, aryl-C(O)—C(O)—, heteroaryl-C(O)—C(O)—, carbocyclyl-C(O)—C(O)—, heterocyclyl-C(O)—C(O)— or —XR6; —X represents —CO—, —S(O)— or —S(O)2—; and —R6 represents C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkylthio, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 alkyl)-O—, heteroaryl-(C1-6 alkyl)-O—, carbocyclyl-(C1-6 alkyl)-O—, heterocyclyl-(C1-6 alkyl)-O— or —NR′R″ wherein each R′ and R″ is the same or different and represents hydrogen, C1-6 alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)- or heterocyclyl-(C1-6 alkyl)-.

公开(公告)号：US07226923B2

公开(公告)日：2007-06-05

申请号：US11233311

申请日：2005-09-23

申请人： Edward Boyd ,  Frederick Brookfield ,  Guy Georges ,  Bernhard Goller ,  Sabine Huensch ,  Petra Rueger ,  Matthias Rueth ,  Stefan Scheiblich ,  Christine Schuell ,  Wolfgang von der Saal ,  Justin Warne ,  Stefan Weigand

发明人： Edward Boyd ,  Frederick Brookfield ,  Guy Georges ,  Bernhard Goller ,  Sabine Huensch ,  Petra Rueger ,  Matthias Rueth ,  Stefan Scheiblich ,  Christine Schuell ,  Wolfgang von der Saal ,  Justin Warne ,  Stefan Weigand

IPC分类号： C07D403/12 ,  C07D403/14 ,  A61K31/502

CPC分类号： C07D403/12

摘要： Compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates are disclosed. Also disclosed are methods for the preparation of the above-mentioned compounds, pharmaceutical compositions containing them, as well as the use of the above-mentioned compounds in the treatment, control or prevention of illnesses such as cancer.

摘要翻译： 公开了式I化合物的药学上可接受的盐，对映体形式，非对映异构体和外消旋体。 还公开了制备上述化合物的方法，含有它们的药物组合物，以及上述化合物在治疗，控制或预防诸如癌症等疾病中的用途。