公开(公告)号：US20060063782A1

公开(公告)日：2006-03-23

申请号：US10519922

申请日：2003-07-03

申请人： Christopher Murray ,  Michael Hartshorn ,  Martyn Frederickson ,  Miles Congreve ,  Alessandro Padova ,  Steven Woodhead ,  Adrian Gill ,  Andrew Woodhead

发明人： Christopher Murray ,  Michael Hartshorn ,  Martyn Frederickson ,  Miles Congreve ,  Alessandro Padova ,  Steven Woodhead ,  Adrian Gill ,  Andrew Woodhead

IPC分类号： A61K31/4965 ,  C07D213/63 ,  A61K31/44

CPC分类号： C07D213/73 ,  C07D213/65 ,  C07D213/74 ,  C07D213/81 ,  C07D241/18 ,  C07D241/20 ,  C07D241/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14 ,  C07D513/04

摘要： Compounds of the formula (I), wherein: —X═Y— is selected from —CR =CR — and —CR ═N—; R is selected from H, halo, NRR′, NHC(═O)R, NHC(═O)NRR′, NH2SO2R, and C(═O)NRR′; R and R (where present) are independently selected from H, optionally substituted C1-7 alkyl, optionally substituted C5-20 aryl, optionally substituted C3-20 heterocyclyl, halo, amino, amido, hydroxy, ether, thio, thioether, acylamido, ureido and sulfonamino; R is an optionally substituted C5-20 aryl or C5-20 heteroaryl group; and R is selected from R , halo, NHR , C(═O)NHR , OR , SR , NHC(═O)R , NHC(═O)NHR , NHS(═O)R , wherein R is H or C1-3 alkyl (optionally substituted by halo, NH2, OH, SH) are disclosed for use in therapy and for treating diseases ameliorated by inhibiting p38 MAP kinase.

摘要翻译： 式（I）的化合物，其中：-X-Y-选自-CR 2 = CR 3 - 和-CR 2 -N-; R 1选自H，卤素，NRR'，NHC（-O）R，NHC（-O）NRR'，NH 2 SO 2 R和C（-O）NRR'; R 2和R 3（如果存在）独立地选自H，任选取代的C 1-7烷基，任选取代的C 5-20芳基，任选取代的C 3-20杂环基，卤素，氨基，酰胺基，羟基，醚， 硫代，硫醚，酰氨基，脲基和磺氨基; R 4是任选取代的C 5-20芳基或C 5-20杂芳基; R 5选自R 5，卤素，NHR 5，C（O）NHR 5，OR 5，SR 5，NHC（-O） R 5，NHC（-O）NHR 5，NHS（-O）R 5，其中R 5'是H或C 1-3烷基（任选地被卤素，NH 2，OH ，SH）被公开用于治疗和治疗通过抑制p38 MAP激酶而改善的疾病。

公开(公告)号：US20070082898A1

公开(公告)日：2007-04-12

申请号：US10553361

申请日：2004-04-13

申请人： Adrian Gill ,  Steven Woodhead ,  Maria Carr

发明人： Adrian Gill ,  Steven Woodhead ,  Maria Carr

IPC分类号： A61K31/538 ,  A61K31/522 ,  A61K31/52 ,  A61K31/517 ,  A61K31/496 ,  A61K31/4745 ,  A61K31/4709 ,  A61K31/4178 ,  A61K31/416 ,  C07D417/02 ,  C07D413/02 ,  C07D409/02

CPC分类号： C07D409/12 ,  C07D333/38 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14

摘要： The invention provides the use of a compound for the manufacture of a medicament for the prophylaxis or treatment of a disease state or condition mediated by a p38 MAP kinase; the compound being defined by formula (I): wherein: R1 and R2 are the same or different and each is selected from hydrogen, C1-4 hydrocarbyl, halogen and cyano; X is selected from C═O, C═S, C(═O)NH, C(═S)NH, C(═O)O, C(═O)S, C(═S)O and C(═S)S; R3 is selected from aryl and hetcroaryl groups each having from 5 to 12 ring members, the aryl and heteroaryl groups each being unsubstituted or substituted by one or more substituent groups R7 selected from halogen, hydroxy, trifluoromethyl, cyano, nitro, carboxy, amino, carbocyclic and heterocyclic groups having from 3 to 12 ring members; a group Ra—Rb wherein Ra is a bond, 0, CO, X1C(X2), C(X2)X1, X1C(X2)X1, S, SO, SO2, NRc, SO2NRc or NRcSO2; and Rb is selected from hydrogen, carbocyclic and heterocyclic groups having from 3 to 7 ring members, and a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from hydroxy, oxo, halogen, cyano, nitro, amino, mono- or di-C1-4 hydrocarbylamino, carbocyclic and heterocyclic groups having from 3 to 12 ring members and wherein one or more carbon atoms of the C1-8 hydrocarbyl group may optionally be replaced by O, S, SO, SO2, NRc, X1C(X2), C(X2)X1 or X1C(X2)X1; X1 is O, S or NRc and X2 is ═O, ═S or ═NRc; Rc is hydrogen or C1-4 hydrocarbyl; R4 is a group YR5 or a group R6; Y is is NH, O or S; R5 is selected from (a) carbocyclic and heterocyclic groups having from 3 to 12 ring members; and (b) C1-8 hydrocarbyl groups optionally substituted by one or more substituents selected from hydroxy, oxo, halogen, cyano, amino, mono- or di- C1-4 hydrocarbylamino, and carbocyclic and heterocyclic groups having from 3 to 12 ring members, wherein one or more carbon atoms of the C1-8 hydrocarbyl group may optionally be replaced by O, S, SO, SO2, NRc, X1C(X2), C(X2)X1 or X1C(X2)X1, provided that when Y is O, a carbon atom adjacent to the group Y is not replaced by O; and R6 is a heterocyclic group having from 4 to 12 ring members and containing at least one ring nitrogen atom through which R6 is linked to the adjacent carbonyl group; wherein the carbocyclic and heterocyclic groups of substituents R5 and R6 are each unsubstituted or substituted by one or more substituent groups R7 as hereinbefore defined. Also provided are novel compounds, pharmaceutical compositions containing the compounds and methods for their preparation.

公开(公告)号：US20110152244A1

公开(公告)日：2011-06-23

申请号：US13060154

申请日：2009-08-20

申请人： Gilbert Besong ,  Christopher Thomas Brain ,  Clinton A. Brooks ,  Miles Stuart Congreve ,  Claudio Dagostin ,  Guo He ,  Ying Huo ,  Steven Howard ,  Yue Li ,  Yipin Lu ,  Paul Morteson ,  Troy Smith ,  Moo Sung ,  Steven Woodhead ,  Wojciech Wrona

发明人： Gilbert Besong ,  Christopher Thomas Brain ,  Clinton A. Brooks ,  Miles Stuart Congreve ,  Claudio Dagostin ,  Guo He ,  Ying Huo ,  Steven Howard ,  Yue Li ,  Yipin Lu ,  Paul Morteson ,  Troy Smith ,  Moo Sung ,  Steven Woodhead ,  Wojciech Wrona

IPC分类号： C07D487/04 ,  A61K31/497 ,  A61K31/519 ,  A61K31/551 ,  A61K31/5377 ,  A61K31/501 ,  C12N9/99 ,  A61P35/04 ,  A61P29/00

CPC分类号： C07D487/04 ,  A61K31/519 ,  C07D487/08

摘要： The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.

摘要翻译： 所公开的化合物涉及蛋白激酶相关病症的治疗和疗法。 还需要可用于治疗或预防或改善癌症，移植排斥和自身免疫性疾病的一种或多种症状的化合物。 此外，需要使用本文提供的化合物调节蛋白激酶如CDK1，CDK2，CDK4，CDK5，CDK6，CDK7，CDK8和CDK9的活性的方法。

公开(公告)号：US20130247126A1

公开(公告)日：2013-09-19

申请号：US13988856

申请日：2010-11-26

申请人： Jeremy Bennett ,  Steven Woodhead

发明人： Jeremy Bennett ,  Steven Woodhead

IPC分类号： H04N21/236

CPC分类号： H04N21/23611 ,  H04L47/22 ,  H04L47/2408 ,  H04L47/29 ,  H04L47/30 ,  H04L65/602 ,  H04N21/23406 ,  H04N21/23614 ,  H04N21/23655

摘要： The invention relates to a method and device for buffering data for multiplexing. The invention also relates to a method of multiplexing and to a multiplexer arrangement using the method and device for buffering data for multiplexing. In one embodiment the invention can be applied to the buffering of non-traffic data, such as firmware updates or other supplementary information, before multiplexing the non-traffic data with traffic data, such as television data of television channels, to form a satellite broadcast channel. In embodiments of the invention, non-traffic data for multiplexing is buffered and then read out again for multiplexing at a rate which is a function of buffer fullness. The non-traffic data may be multiplexed with at least one traffic data channel. A multiplexer can view the non-traffic data channel as another multiplexing input and can allocate the available bit rate between the traffic data channels and the non-traffic data accordingly.

摘要翻译： 本发明涉及用于缓冲多路复用数据的方法和装置。 本发明还涉及使用用于缓冲用于复用的数据的方法和装置的复用方法和多路复用器装置。 在一个实施例中，在将非业务数据与诸如电视频道的电视数据的业务数据复用之前，本发明可以应用于非业务数据的缓冲，例如固件更新或其他补充信息，以形成卫星广播 渠道。 在本发明的实施例中，用于多路复用的非业务数据被缓冲，然后再次读出以以缓冲器充满度的函数的复用。 非业务数据可以与至少一个业务数据信道多路复用。 多路复用器可以将非业务数据信道视为另一复用输入，并且可以相应地在业务数据信道和非业务数据之间分配可用比特率。

公开(公告)号：US09416136B2

公开(公告)日：2016-08-16

申请号：US14158358

申请日：2014-01-17

申请人： Gilbert Besong ,  Christopher Thomas Brain ,  Clinton A Brooks ,  Miles Stuart Congreve ,  Claudio Dagostin ,  Guo He ,  Ying Hou ,  Steven Howard ,  Yue Li ,  Yipin Lu ,  Paul Mortenson ,  Troy Smith ,  Moo Je Sung ,  Steven Woodhead ,  Wojciech Wrona ,  Bharat Lagu

发明人： Gilbert Besong ,  Christopher Thomas Brain ,  Clinton A Brooks ,  Miles Stuart Congreve ,  Claudio Dagostin ,  Guo He ,  Ying Hou ,  Steven Howard ,  Yue Li ,  Yipin Lu ,  Paul Mortenson ,  Troy Smith ,  Moo Je Sung ,  Steven Woodhead ,  Wojciech Wrona ,  Bharat Lagu

IPC分类号： A61K31/519 ,  A61P35/04 ,  C07D487/04 ,  C07D487/08

CPC分类号： C07D487/04 ,  A61K31/519 ,  C07D487/08

摘要： The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.

公开(公告)号：US09078017B2

公开(公告)日：2015-07-07

申请号：US13988856

申请日：2010-11-26

申请人： Jeremy Bennett ,  Steven Woodhead

发明人： Jeremy Bennett ,  Steven Woodhead

IPC分类号： H04L12/815 ,  H04L12/801 ,  H04L12/835 ,  H04L12/851 ,  H04L29/06 ,  H04N7/173 ,  H04N7/16 ,  H04J3/24 ,  H04N21/236 ,  H04N21/234 ,  H04N21/2365

CPC分类号： H04N21/23611 ,  H04L47/22 ,  H04L47/2408 ,  H04L47/29 ,  H04L47/30 ,  H04L65/602 ,  H04N21/23406 ,  H04N21/23614 ,  H04N21/23655

摘要： The invention relates to a method and device for buffering data for multiplexing. The invention also relates to a method of multiplexing and to a multiplexer arrangement using the method and device for buffering data for multiplexing. In one embodiment the invention can be applied to the buffering of non-traffic data, such as firmware updates or other supplementary information, before multiplexing the non-traffic data with traffic data, such as television data of television channels, to form a satellite broadcast channel. In embodiments of the invention, non-traffic data for multiplexing is buffered and then read out again for multiplexing at a rate which is a function of buffer fullness. The non-traffic data may be multiplexed with at least one traffic data channel. A multiplexer can view the non-traffic data channel as another multiplexing input and can allocate the available bit rate between the traffic data channels and the non-traffic data accordingly.

摘要翻译： 本发明涉及用于缓冲多路复用数据的方法和装置。 本发明还涉及使用用于缓冲用于复用的数据的方法和装置的复用方法和多路复用器装置。 在一个实施例中，在将非业务数据与诸如电视频道的电视数据的业务数据复用之前，本发明可以应用于非业务数据的缓冲，例如固件更新或其他补充信息，以形成卫星广播 渠道。 在本发明的实施例中，用于多路复用的非业务数据被缓冲，然后再次读出以以缓冲器充满度的函数的复用。 非业务数据可以与至少一个业务数据信道多路复用。 多路复用器可以将非业务数据信道视为另一复用输入，并且可以相应地在业务数据信道和非业务数据之间分配可用比特率。

公开(公告)号：US20140135312A1

公开(公告)日：2014-05-15

申请号：US14158358

申请日：2014-01-17

申请人： Gilbert BESONG ,  Christopher Thomas Brain ,  Clinton A. Brooks ,  Miles Stuart Congreve ,  Claudio Dagostin ,  Guo He ,  Ying Huo ,  Steven Howard ,  Yue Ll ,  Yipin Lu ,  Paul Mortenston ,  Troy Smith ,  Moo Je Sung ,  Steven Woodhead ,  Wojciech Wrona ,  Bharat Lagu

发明人： Gilbert BESONG ,  Christopher Thomas Brain ,  Clinton A. Brooks ,  Miles Stuart Congreve ,  Claudio Dagostin ,  Guo He ,  Ying Huo ,  Steven Howard ,  Yue Ll ,  Yipin Lu ,  Paul Mortenston ,  Troy Smith ,  Moo Je Sung ,  Steven Woodhead ,  Wojciech Wrona ,  Bharat Lagu

IPC分类号： C07D487/08 ,  C07D487/04

CPC分类号： C07D487/04 ,  A61K31/519 ,  C07D487/08

摘要： The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.

摘要翻译： 所公开的化合物涉及蛋白激酶相关病症的治疗和疗法。 还需要可用于治疗或预防或改善癌症，移植排斥和自身免疫性疾病的一种或多种症状的化合物。 此外，需要使用本文提供的化合物调节蛋白激酶如CDK1，CDK2，CDK4，CDK5，CDK6，CDK7，CDK8和CDK9的活性的方法。

公开(公告)号：US20100105653A1

公开(公告)日：2010-04-29

申请号：US12545322

申请日：2009-08-21

申请人： Gilbert Besong ,  Christopher Thomas Brain ,  Clinton A. Brooks ,  Miles Stuart Congreve ,  Claudio Dagostin ,  Guo He ,  Ying Huo ,  Steven Howard ,  Yue Li ,  Yipin Lu ,  Paul Mortenson ,  Troy Smith ,  Moo Je Sung ,  Steven Woodhead ,  Wojciech Wrona

发明人： Gilbert Besong ,  Christopher Thomas Brain ,  Clinton A. Brooks ,  Miles Stuart Congreve ,  Claudio Dagostin ,  Guo He ,  Ying Huo ,  Steven Howard ,  Yue Li ,  Yipin Lu ,  Paul Mortenson ,  Troy Smith ,  Moo Je Sung ,  Steven Woodhead ,  Wojciech Wrona

IPC分类号： A61K31/519 ,  C07D487/04 ,  A61K31/551 ,  C12N5/00

CPC分类号： C07D487/04 ,  A61K31/519 ,  C07D487/08

摘要： The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.

摘要翻译： 所公开的化合物涉及蛋白激酶相关病症的治疗和疗法。 还需要可用于治疗或预防或改善癌症，移植排斥和自身免疫性疾病的一种或多种症状的化合物。 此外，需要使用本文提供的化合物调节蛋白激酶如CDK1，CDK2，CDK4，CDK5，CDK6，CDK7，CDK8和CDK9的活性的方法。