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1. 发明申请

US20090163490A1 Pyrrolopyrimidine Derivatives Used As HSP90 Inhibitors 审中-公开
标题翻译：用作HSP90抑制剂的吡咯并嘧啶衍生物
公开(公告)号：US20090163490A1
公开(公告)日：2009-06-25
申请号：US12282526
申请日：2007-03-09
申请人： Paul Andrew Brough , Martin James Drysdale , Nicholas Gareth Davies , Nicolas Noel Foloppe , Stephen Stokes
发明人： Paul Andrew Brough , Martin James Drysdale , Nicholas Gareth Davies , Nicolas Noel Foloppe , Stephen Stokes
IPC分类号： A61K31/5377 , C07D487/04 , A61P31/12 , A61K31/519
CPC分类号： C07D487/04
摘要： Compounds of formula (I) have HSP90 inhibitory activity and are therefore useful in the treatment of, inter alia, cancer: Formula (I) wherein Ri is hydrogen, fluoro, chloro, bromo, or a radical of formula -X-Alk1-(Z)m-(Alk2)n-Q wherein X is —O—, —S— —S(O)—, SO2—, or —NH—, Z is —O—, —S—, —(C═O)—, —(C═S)—, —S(O)—, —SO2—, —NRA—, or, in either orientation —C(═O)O—, —C(═O)NRA—, —C(═S)NRA—, —SO2NRA—, —NRAC(═O)—, or —NRASO2— wherein RA is hydrogen or C1-C6 alkyl AIk1 and AIk2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, n and p are independently 0 or 1, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R2 is a radical of formula —(Ar1)p-(Alk1)q-(Z)r-(Alk2)s-Q wherein Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1, Alk2, Z, and Q are as defined above, and p, q, r and s are independently 0 or 1; and R3 is cyano (—CN), fluoro, chloro, bromo, methyl in which in which one or more hydrogen atoms are optionally replaced by fluorine atoms, ethyl in which in which one or more hydrogen atoms are optionally replaced by fluorine atoms, cyclopropyl, —OH, —CH2OH, —C(O)NH2, —C(O)CH3, Or —NH2.
摘要翻译：式（I）化合物具有HSP90抑制活性，因此可用于治疗尤其是癌症：式（I）其中R 1是氢，氟，氯，溴或式-X-Alk1-（ Z）m-（Alk2）nQ其中X是-O - ， - S-S（O） - ，SO2-或-NH-，Z是-O - ， - S-， - （CO）（ - ） - ， - （ - O - ） - ， - （ - O - ） - ， - （ - - ， - SO 2 -NRA - ， - NRAC（-O） - 或-NRASO 2 - ，其中RA为氢或C 1 -C 6烷基，Alk 1和Alk 2为任选取代的二价C 1 -C 3亚烷基或C 2 -C 3亚烯基，m，n和p 独立地为0或1，并且Q为氢或任选取代的碳环或杂环基; R2是式 - （Ar1）p-（Alk1）q-（Z）r-（Alk2）sQ的基团，其中Ar1是任选取代的芳基或杂芳基，Alk1，Alk2，Z和Q如上定义，和p，q，r和s独立地为0或1; 并且R 3是氰基（-CN），氟，氯，溴，其中一个或多个氢原子任选被氟原子取代的甲基，其中一个或多个氢原子任选被氟原子取代的乙基，环丙基，-OH，-CH 2 OH，-C（O）NH 2，-C（O）CH 3或-NH 2。

2. 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。

3. 发明申请

US20070043024A1 Azacyclic compounds as inhibitors of sensory neurone specific channels 审中-公开
标题翻译：偶氮化合物作为感觉神经元特异性通道的抑制剂
公开(公告)号：US20070043024A1
公开(公告)日：2007-02-22
申请号：US10563561
申请日：2004-07-07
申请人： Richard Hamlyn , Michael Huckstep , Rosemary Lynch , Stephen Stokes , David Tickle , Lee Patient
发明人： Richard Hamlyn , Michael Huckstep , Rosemary Lynch , Stephen Stokes , David Tickle , Lee Patient
IPC分类号： A61L9/04 , A61K31/55 , A61K31/47 , A61K31/4745
CPC分类号： A61K31/47 , A61K31/4745 , A61K31/55
摘要： Compounds of the formula (I), and pharmaceutically acceptable salts thereof, are found to be antagonists of SNS sodium channels. They are therefore useful as analgesic and neuroprotective agents wherein: X is —N— or —CH—; n is from 0 to 3.
摘要翻译：发现式（I）化合物及其药学上可接受的盐是SNS钠通道的拮抗剂。因此它们可用作止痛剂和神经保护剂，其中：X是-N-或-CH-; n为0〜3。

4. 发明申请

US20060029340A1 Locatable dielectric optical fiber cable having easily removable locating element 有权
标题翻译：具有易拆卸定位元件的可定位电介质光缆
公开(公告)号：US20060029340A1
公开(公告)日：2006-02-09
申请号：US10914762
申请日：2004-08-09
申请人： Robert Andrews , Scott Chastain , Stephen Stokes , George Mackie
发明人： Robert Andrews , Scott Chastain , Stephen Stokes , George Mackie
IPC分类号： G02B6/44
CPC分类号： G02B6/447 , G02B6/4495
摘要： The present invention provides a dielectric optical fiber cable which is capable of being remotely detected while buried. Specifically, this invention incorporates a detectable and easily removable locating element which is attached to the optical fiber cable by a web defined by the jacket extending over both the optical fiber cable and the locating element. The web allows for the locating strand to be easily removed once separation of the locating element from the optical fiber cable is initiated. The web is designed to allow the initial tear to propagate into a precise longitudinal tear along a predetermined length of the optical fiber cable.
摘要翻译：本发明提供一种能够在埋藏时被远程检测的电介质光缆。具体地说，本发明结合了一种可检测且易于拆卸的定位元件，该定位元件由通过光纤电缆和定位元件两端延伸的护套限定的腹板连接到光纤电缆。一旦分离定位元件与光纤电缆分离就可以方便地拆下定位线。网被设计成允许初始撕裂沿着光纤缆线的预定长度传播到精确的纵向撕裂中。

5. 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。

6. 发明申请

US20080080820A1 Locatable dielectric optical fiber cable having easily removable locating element 有权
标题翻译：具有易拆卸定位元件的可定位电介质光缆
公开(公告)号：US20080080820A1
公开(公告)日：2008-04-03
申请号：US11980959
申请日：2007-10-31
申请人： Robert Andrews , Scott Chastain , Stephen Stokes , George Mackie
发明人： Robert Andrews , Scott Chastain , Stephen Stokes , George Mackie
IPC分类号： H01B11/22 , G02B6/44
CPC分类号： G02B6/447 , G02B6/4495
摘要： An optical fiber cable having a locating element and extending from a distribution enclosure to a premise is provided. The optic fiber cable includes a core having at least one optical fiber transmission medium disposed within a tubular member that has a jacket system disposed thereabout. A longitudinally extending detectable element is provided that does not function as a communications cable and that is detachably connected to said tubular member by the jacket system which is also disposed about the detectable element so as to define a web between the tubular member and the detectable element. The detectable element terminates before at least one of the distribution enclosure or the premise. The web defines a notch between the tubular member and the detectable element which serves as a shear plane to facilitate the propagation of a tear between the tubular member and the detectable element.
摘要翻译：提供了一种具有定位元件并从分配机壳延伸到前提的光缆。光纤电缆包括具有至少一个光纤传输介质的芯体，该光纤传输介质设置在管状部件内，该管状部件具有设置在其周围的护套系统。提供了一种纵向延伸的可检测元件，其不用作通信电缆，并且通过护套系统可拆卸地连接到所述管状构件，护套系统也围绕可检测元件设置，以便在管状构件和可检测元件之间限定腹板。可检测元件在分配封壳或前提中的至少一个之前终止。网状物在管状构件和可检测元件之间限定了一个凹口，其用作剪切平面以便于在管状构件和可检测元件之间传播泪液。

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