公开(公告)号：US08507480B2

公开(公告)日：2013-08-13

申请号：US12708686

申请日：2010-02-19

Applicant: Martin James Drysdale ,  Brian William Dymock ,  Harry Finch ,  Paul Webb ,  Edward McDonald ,  Karen Elizabeth James ,  Kwai Ming Cheung ,  Thomas Peter Matthews

Inventor： Martin James Drysdale ,  Brian William Dymock ,  Harry Finch ,  Paul Webb ,  Edward McDonald ,  Karen Elizabeth James ,  Kwai Ming Cheung ,  Thomas Peter Matthews

IPC: C07D261/08 ,  C07D261/10 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D495/04 ,  A61K31/422 ,  A61K31/42 ,  A61K31/4439 ,  A61K31/427 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/454 ,  A61K31/541 ,  A61P3/10 ,  A61P29/00

CPC classification number: A61K31/541 ,  A61K31/42 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5377 ,  C07D261/08 ,  C07D261/10 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D495/04

Abstract: Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C═O)—, —(C═S)—, —SO.sub.2-, —C(═O)O—, —C(═O)NRA—, —C(═S)NRA—, —SO2NRA—, —NRAC(═O)—, —NRASO2—or —NRA— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R2 is (i) a group of formula (IA) above or (ii) a carboxamide radical; or (iii) a non aromatic carbocyclic or heterocyclic ring wherein a ring carbon is optionally substituted, and/or a ring nitrogen is optionally substituted by a group of formula -(Alk1)p-(Z)r-(Alk2)s-Q wherein Q, Alk1, Alk2, Z, p, r and s are as defined above in relation to group (IA); and R3 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6 alkenyl, or C1-C6 alkynyl; or a carboxyl, carboxamide, or carboxyl ester group.

Abstract translation: 式（A）或（B）的异恶唑是HSP90活性的抑制剂，可用于治疗例如癌症：其中R1是式（IA）的基团：-Ar1-（Alk1）对（Z）r - （Alk2）sQ，其中在任何相容的组合中，Ar 1是任选取代的芳基或杂芳基，Alk1和Alk2是任选取代的二价C 1 -C 6亚烷基或C 2 -C 6亚烯基，p，r和s独立地为0或1， Z是-O - ， - S - ， - （C = O） - ， - （C = S） - ，-SO 2 - ， - C（= O） - ， - C（= S）NRA，-SO 2 NRRA-，-NRAC（= O） - ，-NRASO 2 - 或-NRA-，其中RA是氢或C 1 -C 6烷基，Q是氢或任选取代的碳环或 杂环基; R2是（i）上述式（IA）的基团或（ii）甲酰胺基团; 或（iii）非芳族碳环或杂环，其中环碳任选被取代，和/或环氮任选被式 - （Alk1）对（Z）r-（Alk2）sQ基团取代，其中Q ，Alk1，Alk2，Z，p，r和s如上文关于组（IA）所定义; 并且R 3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。

公开(公告)号：US08450310B2

公开(公告)日：2013-05-28

申请号：US13525409

申请日：2012-06-18

Applicant: Martin James Drysdale ,  Brian William Dymock ,  Harry Finch ,  Paul Webb ,  Edward McDonald ,  Karen Elizabeth James ,  Kwai Ming Cheung ,  Thomas Peter Matthews

Inventor： Martin James Drysdale ,  Brian William Dymock ,  Harry Finch ,  Paul Webb ,  Edward McDonald ,  Karen Elizabeth James ,  Kwai Ming Cheung ,  Thomas Peter Matthews

IPC: C07D261/08 ,  C07D261/10 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D495/04 ,  A61P35/00 ,  A61K31/42 ,  A61K31/5377 ,  A61K31/422 ,  A61K31/4439 ,  A61K31/427 ,  A61K31/496

CPC classification number: A61K31/541 ,  A61K31/42 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5377 ,  C07D261/08 ,  C07D261/10 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D495/04

Abstract: Isoxazoles of formula (A) or (B) wherein R1 is a group of formula (IB) The isoxazoles are inhibitors of HSP90 activity, and useful for the treatment of, for example, cancers.

Abstract translation: 式（A）或（B）的异恶唑其中R1是式（IB）的基团异恶唑是HSP90活性的抑制剂，可用于治疗例如癌症。

公开(公告)号：US08432601B2

公开(公告)日：2013-04-30

申请号：US12434379

申请日：2009-05-01

Applicant: Steven Paul Webb ,  Dennis Brestovansky ,  Craig Richard Berry ,  John Russell Kingery

Inventor： Steven Paul Webb ,  Dennis Brestovansky ,  Craig Richard Berry ,  John Russell Kingery

IPC: G02F1/15

CPC classification number: C08L71/02 ,  G02F1/1521 ,  G02F1/161 ,  G02F2001/1519

Abstract: An electrochromic display module employing a unique combination of architecture and electrochromic composition to provide an extended life to the module. The architecture may involve the use of an extended seal about a perimeter of a display portion where the composition is located. In this manner, the rate of solvent leakage from the composition may be substantially reduced. Additionally, the electrochromic composition itself may make use of particular low volatility solvents and constituent combinations so as to discourage the amount particle generation therein. Ultimately, an electrochromic display module having a useful life of more than about 3 years may be provided.

Abstract translation: 一种电致变色显示模块，采用独特的架构和电致变色组合结合，为模块提供延长的使用寿命。 该结构可以涉及围绕组合物所在的显示部分的周边使用延长的密封。 以这种方式，可以显着降低来自组合物的溶剂泄漏速率。 此外，电致变色组合物本身可以利用特定的低挥发性溶剂和组成组合，以便阻止其中的颗粒产生量。 最终，可以提供使用寿命大于3年的电致变色显示模块。

公开(公告)号：US20110021498A1

公开(公告)日：2011-01-27

申请号：US12812791

申请日：2009-01-20

Applicant: Stephen Stokes ,  Nicolas Foloppe ,  Andrea Fiumana ,  Martin Drysdale ,  Simon Bedford ,  Paul Webb

Inventor： Stephen Stokes ,  Nicolas Foloppe ,  Andrea Fiumana ,  Martin Drysdale ,  Simon Bedford ,  Paul Webb

IPC: A61K31/397 ,  A61P35/00 ,  A61P19/02 ,  C07D401/14 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  C07D413/14 ,  A61K31/5377

CPC classification number: C07D401/14 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  C07D413/14

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20100277788A1

公开(公告)日：2010-11-04

申请号：US12434379

申请日：2009-05-01

Applicant: Steven Paul Webb ,  Dennis Brestovansky ,  Craig Richard Berry ,  John Russell Kingery

Inventor： Steven Paul Webb ,  Dennis Brestovansky ,  Craig Richard Berry ,  John Russell Kingery

IPC: G02F1/161 ,  G02F1/153 ,  C08G65/04 ,  C08L63/00

CPC classification number: C08L71/02 ,  G02F1/1521 ,  G02F1/161 ,  G02F2001/1519

Abstract: An electrochromic display module employing a unique combination of architecture and electrochromic composition to provide an extended life to the module. The architecture may involve the use of an extended seal about a perimeter of a display portion where the composition is located. In this manner, the rate of solvent leakage from the composition may be substantially reduced. Additionally, the electrochromic composition itself may make use of particular low volatility solvents and constituent combinations so as to discourage the amount particle generation therein. Ultimately, an electrochromic display module having a useful life of more than about 3 years may be provided.

Abstract translation: 一种电致变色显示模块，采用独特的架构和电致变色组合结合，为模块提供延长的使用寿命。 该结构可以涉及围绕组合物所在的显示部分的周边使用延长的密封。 以这种方式，可以显着降低来自组合物的溶剂泄漏速率。 此外，电致变色组合物本身可以利用特定的低挥发性溶剂和组成组合，以便阻止其中的颗粒产生量。 最终，可以提供使用寿命大于3年的电致变色显示模块。

公开(公告)号：US07823932B2

公开(公告)日：2010-11-02

申请号：US11737429

申请日：2007-04-19

Applicant: Steven Paul Webb ,  Alan Richard Glaze

Inventor： Steven Paul Webb ,  Alan Richard Glaze

IPC: F16L17/00

CPC classification number: F16L13/148 ,  F16L13/142

Abstract: A press fitting arrangement includes a sealing ring to be housed within a bead of a press fitting into which a tube is to be inserted. There is at least one gap between the press fitting together with the sealing ring and the tube which is closed by pressing at least one portion of the press fitting. The sealing ring has at least one first portion along the majority of its circumference. Each first portion of the sealing ring has an outside diameter (SOD1) prior to fitment into the press fitting bead which is larger than the inside bead diameter (BID) and an inside diameter (SID1) prior to the insertion of the tube which is less than the tube outside diameter (TOD). Additionally, the sealing ring has at least one pair of diametrically opposing second portions, each second portion of the sealing ring comprising a recess between the two projections.

Abstract translation: 按压配合装置包括密封环，该密封环容纳在要插入管的压配合件的胎圈内。 压力机与密封环配合在一起的至少一个间隙和通过按压压配件的至少一部分而封闭的管子。 密封环具有沿其大部分圆周的至少一个第一部分。 密封环的每个第一部分在装配到压入配料珠中之前具有大于内胎圈直径（BID）的外径（SOD1）和在插入管之前的内径（SID1）较小 比管外径（TOD）。 另外，密封环具有至少一对直径相对的第二部分，密封环的每个第二部分包括在两个突起之间的凹部。

公开(公告)号：US20100179138A1

公开(公告)日：2010-07-15

申请号：US12708686

申请日：2010-02-19

Applicant: Martin James Drysdale ,  Brian William Dymock ,  Harry Finch ,  Paul Webb ,  Edward McDonald ,  Karen Elizabeth James ,  Kwai Ming Cheung ,  Thomas Peter Matthews

Inventor： Martin James Drysdale ,  Brian William Dymock ,  Harry Finch ,  Paul Webb ,  Edward McDonald ,  Karen Elizabeth James ,  Kwai Ming Cheung ,  Thomas Peter Matthews

IPC: A61K31/422 ,  A61K31/42 ,  A61K31/4439 ,  A61K31/427 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/454 ,  A61K31/541 ,  A61P3/10 ,  A61P29/00 ,  C07D261/08 ,  C07D413/10 ,  C07D417/04 ,  C07D413/14

CPC classification number: A61K31/541 ,  A61K31/42 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5377 ,  C07D261/08 ,  C07D261/10 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D495/04

Abstract: Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C═O)—, —(C═S)—, —SO.sub.2-, —C(═O)O—, —C(═O)NRA—, —C(═S)NRA—, —SO2NRA—, —NRAC(═O)—, —NRASO2—or —NRA— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R2 is (i) a group of formula (IA) above or (ii) a carboxamide radical; or (iii) a non aromatic carbocyclic or heterocyclic ring wherein a ring carbon is optionally substituted, and/or a ring nitrogen is optionally substituted by a group of formula -(Alk1)p-(Z)r-(Alk2)s-Q wherein Q, Alk1, Alk2, Z, p, r and s are as defined above in relation to group (IA); and R3 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6 alkenyl, or C1-C6 alkynyl; or a carboxyl, carboxamide, or carboxyl ester group.

Abstract translation: 式（A）或（B）的异恶唑是HSP90活性的抑制剂，可用于治疗例如癌症：其中R1是式（IA）的基团：-Ar1-（Alk1）对（Z）r - （Alk2）sQ，其中在任何相容的组合中，Ar 1是任选取代的芳基或杂芳基，Alk1和Alk2是任选取代的二价C 1 -C 6亚烷基或C 2 -C 6亚烯基，p，r和s独立地为0或1， Z是-O - ， - S - ， - （C = O） - ， - （C = S） - ， - SO 2 - ， - C（= O） - ， - C（= S）NRA，-SO 2 NRRA - ，-NRAC（= O） - ， - NRASO 2 - 或-NRA-，其中RA是氢或C 1 -C 6烷基，Q是氢或任选取代的碳环或 杂环基; R2是（i）上述式（IA）的基团或（ii）甲酰胺基团; 或（iii）非芳族碳环或杂环，其中环碳任选被取代，和/或环氮任选被式 - （Alk1）对（Z）r-（Alk2）sQ基团取代，其中Q ，Alk1，Alk2，Z，p，r和s如上文关于组（IA）所定义; 并且R 3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。

公开(公告)号：US07561043B2

公开(公告)日：2009-07-14

申请号：US11607997

申请日：2006-12-04

Applicant: Ryusuke Hasegawa ,  John Paul Webb ,  Auburn Anthony Chestnut ,  Larry Hill ,  Ronald Joseph Martis

Inventor： Ryusuke Hasegawa ,  John Paul Webb ,  Auburn Anthony Chestnut ,  Larry Hill ,  Ronald Joseph Martis

IPC: G08B13/14

CPC classification number: G08B13/2434 ,  G08B13/2408 ,  G08B13/2442 ,  H01F1/15308 ,  H01F1/15391 ,  H01F41/0226

Abstract: A magnetomechanical resonance element or marker strip with facilitated performance based on an amorphous magnetostrictive alloy ribbon is utilized in an electronic article surveillance marker. A curvature along the element's length direction is introduced during ribbon fabrication with a different radius of curvature, which increases the resonance performance with minimal loss in the magneto-mechanical circuit, and more particularly, in a marker utilizing a plurality of resonating elements or marker strips. A marker is fabricated utilizing the resonance element or elements and is utilized in an electronic article surveillance system.

Abstract translation: 在电子物品监视标记中使用具有基于无定形磁致伸缩合金带的有利性能的磁力机械共振元件或标记条。 沿着元件长度方向的曲率在带状制造过程中引入了不同的曲率半径，这增加了磁 - 机械电路中损耗最小的谐振性能，更具体地说，在使用多个谐振元件或标记条的标记 。 使用谐振元件或元件制造标记，并用于电子物品监视系统。

公开(公告)号：US06156723A

公开(公告)日：2000-12-05

申请号：US930455

申请日：1998-01-12

Applicant: Peter Kushner ,  Paul Webb ,  Renee Williard ,  C. Anthony Hunt ,  Gabriella Lopez

Inventor： Peter Kushner ,  Paul Webb ,  Renee Williard ,  C. Anthony Hunt ,  Gabriella Lopez

IPC: A61K31/35 ,  A61K31/52 ,  A61K31/55 ,  C07K14/72 ,  C12Q1/68 ,  G01N33/74 ,  A61K31/00

CPC classification number: G01N33/743 ,  A61K31/35 ,  A61K31/52 ,  A61K31/55 ,  C07K14/721 ,  C12Q1/6897 ,  G01N2333/723 ,  G01N2500/00

Abstract: The present invention provides novel assay methods for identifying compounds that may have both estrogen agonist and antagonist properties. In particular, the assay use cells comprising promoters having an AP1 site linked to a reporter gene. Compounds capable of inducing or blocking expression of the reporter gene can thus be identified. The compounds may be further tested for the ability to modulate the standard estrogen response, as well.

Abstract translation: PCT No.PCT / US96 / 04104 Sec。 371日期：1998年1月12日 102（e）日期1998年1月12日PCT 1996年3月26日PCT公布。 公开号WO96 / 30505 PCT 日期1996年10月3日本发明提供了鉴定可具有雌激素激动剂和拮抗剂性质的化合物的新型测定方法。 特别地，该测定使用包含与报告基因连接的AP1位点的启动子的细胞。 因此可以鉴定能够诱导或阻断报道基因表达的化合物。 还可以进一步测试这些化合物调节标准雌激素反应的能力。

公开(公告)号：US4096108A

公开(公告)日：1978-06-20

申请号：US687132

申请日：1976-05-17

Applicant: Benton Paul Webb ,  Donald Louis Nelson

Inventor： Benton Paul Webb ,  Donald Louis Nelson

IPC: C08G16/02 ,  C08L61/10 ,  C08L61/34 ,  F16D69/02 ,  C08K3/34

CPC classification number: C08G16/0218 ,  C08L61/34 ,  F16D69/021

Abstract: Superior frictional materials are formed by heating under pressure in the presence of a filler, e.g., asbestos, and a source of formaldehyde, e.g., hexamethylenetetramine, the polymers formed by reacting (1) a mixture of compounds selected from the group having the formulaR.sub.1 --A--CH.sub.2 --OCH.sub.2 --.sub.y A--.sub.x CH.sub.2 --OCH.sub.2 --.sub.y R.sub.3wherein each A is an independently selected aromatic radical having the formula ##STR1## WHEREIN EACH R.sub.1 represents an independently selected radical from the group consisting of hydrogen, --CH.sub.2 --OCH.sub.2 --.sub.y R.sub.3 ; each R.sub.2 represents an independently selected radical selected from the group consisting of R.sub.1, halogen or an alkyl group of 1 to 10 carbon atoms; R.sub.3 represents a radical selected from the group consisting of hydrogen, methoxy, ethoxy, propoxy or --A--H; x represents an integer from 0 to 60; y represents an integer from 0 to 4; z represents an integer from 0 to 2; and B represents oxygen or sulfur; provided that if x is 0 and A is diphenyloxide, then y must be 1 or greater; which mixture may contain up to 50% by weight unreacted aromatic HAH; with (2) at least one monomeric reactant selected from the group ##STR2## WHEREIN R represents hydrogen, alkyl or aryl of 1 to 20 carbon atoms and ##STR3## M REPRESENTS AN INTEGER FROM 1 TO 3; O REPRESENTS AN INTEGER FROM 1 TO 5; P REPRESENTS AN INTEGER FROM 0 TO 3; B represents oxygen, sulfur or C.sub.1 to C.sub.3 alkylidene and q represents an integer from 0 to 1; and finally with (3) formaldehyde in the presence of an acid catalyst at a temperature of from between about 90.degree. C to about 190.degree. C for from several minutes to several hours.

Abstract translation: 优选的摩擦材料通过在填料（例如石棉）和甲醛源（例如六亚甲基四胺）的存在下加压而形成，所述聚合物通过使（1）选自具有式R1的化合物的混合物 -A-CH2-OCH2-yA-xCH2-OCH2-yR3，其中每个A是独立选择的具有下式的芳族基团：其中R 1表示独立选自下列基团：氢， CH2-OCH2-yR3; 每个R 2表示独立选自下组的基团：R1，卤素或1-10个碳原子的烷基; R3表示选自氢，甲氧基，乙氧基，丙氧基或-A-H的基团; x表示0〜60的整数， y表示0〜4的整数， z表示0〜2的整数， B表示氧或硫; 条件是如果x为0且A为二苯氧基，则y必须为1或更大; 该混合物可含有至多50重量％的未反应芳香族HAH; 其中（2）至少一种单体反应物，其选自基团R表示氢，1至20个碳原子的烷基或芳基和1至3的整数; O代表1到5的整数; P代表0到3的整数; B表示氧，硫或C1至C3亚烷基，q表示0至1的整数; 最后用（3）甲醛在酸催化剂存在下，在约90℃至约190℃的温度下进行几分钟至数小时。