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1. 发明申请

WO2019154910A1 A TANNING COMPOSITION 审中-公开
公开(公告)号：WO2019154910A1
公开(公告)日：2019-08-15
申请号：PCT/EP2019/053004
申请日：2019-02-07
申请人： UBEAUTY GLOBAL
发明人： MONE, Rebecca
IPC分类号： A61K8/31 , A61K8/34 , A61K8/35 , A61K8/60 , A61Q19/04
摘要： The invention provides a tanning composition for oral administration by humans, the composition being a chewable pastille comprising: (i)a chewable base comprising a gelling agent and a sugar and/or sugar alcohol; and (ii)one or more skin colour-promoting agents. The sugar is typically a mixture of glucose and sucrose. The gelling agent may be is selected from gelatin, pectin, agar, alginate and carrageen an, and mixtures thereof. The skin colour-promoting agents may comprise one or more of the carotenoids β- carotene, lycopene, zeaxanthin, lutein and astaxanthin, tyrosine, PABA and copper.

2. 发明申请

WO2016170077A1 A SECURITY DEVICE 审中-公开
标题翻译：安全设备
公开(公告)号：WO2016170077A1
公开(公告)日：2016-10-27
申请号：PCT/EP2016/058937
申请日：2016-04-21
申请人： BRISE LIMITED
发明人： BRISE, Timothy Frank
IPC分类号： E05B73/00 , E05B67/00 , B66C1/18 , B62H5/00
CPC分类号： B62H5/003 , E05B15/16 , E05B15/1614 , E05B67/003
摘要： The invention provides a security device for tethering two or more objects together, the security device comprising a flexible strap having two ends; the two ends having means 104 for securing the ends to each other or to other objects; wherein the flexible strap is of layered construction and comprises a plurality of layers formed by separate flexible elongate flat strips 109.
摘要翻译：本发明提供了一种用于将两个或多个物体捆绑在一起的安全装置，该安全装置包括具有两端的柔性带; 两端具有用于将端部固定到彼此或其它物体的装置104; 其中柔性带是分层结构的，并且包括由单独的柔性细长扁平条109形成的多个层。

3. 发明申请

WO2009136166A1 A CONDENSATION APPARATUS 审中-公开
标题翻译：冷凝装置
公开(公告)号：WO2009136166A1
公开(公告)日：2009-11-12
申请号：PCT/GB2009/001147
申请日：2009-05-08
申请人： NANEUM LIMITED , GORBUNOV, Boris, Zachar , GNEWUCH, Harald, Wilhelm, Julius
发明人： GORBUNOV, Boris, Zachar , GNEWUCH, Harald, Wilhelm, Julius
IPC分类号： G01N15/06
CPC分类号： B05C3/005 , B01D5/0027 , B05C3/02 , G01N15/02 , G01N15/065 , G01N33/0011 , G01N2015/0046 , Y10T137/6416 , Y10T137/8593
摘要： The invention provides an apparatus for increasing the size of gas-entrained particles in order to render the gas-entrained particles detectable by a particle detector, the apparatus comprising an evaporation chamber (2) and a condenser (7); the evaporation chamber (2) having an inlet (1) for admitting gas into the evaporation chamber and an outlet through which vapour-laden gas may leave the evaporation chamber; the evaporation chamber (2) having disposed therein a heating element (3) and a porous support (6), the heating element being in direct contact with the porous support, wherein the porous support (6) carries thereon a vaporisable substance and the heating element (3) is heatable to vaporise the vaporisable substance to form vapour within the evaporation chamber (2); the condenser (2) being in fluid communication with the outlet of the evaporation chamber, and the condenser (7) having an outlet for connection to the particle detector the apparatus being configured so that vapour-laden gas from the evaporation chamber can flow into the condenser and condensation of the vaporisable substance onto gas-entrained particles in the condenser takes place to increase the size of the particles so that they are capable of being detected by a particle detector.
摘要翻译：本发明提供了一种用于增加气体夹带颗粒的尺寸的装置，以使由气体夹带的颗粒可被颗粒检测器检测到，该装置包括蒸发室（2）和冷凝器（7）; 蒸发室（2）具有用于将气体引入蒸发室的入口（1）和含蒸气的气体可通过该出口离开蒸发室; 所述蒸发室（2）在其中设置有加热元件（3）和多孔载体（6），所述加热元件与所述多孔载体直接接触，其中所述多孔载体（6）承载有可蒸发物质，并且所述加热元件元件（3）可加热以蒸发可蒸发物质以在蒸发室（2）内形成蒸气; 冷凝器（2）与蒸发室的出口流体连通，并且冷凝器（7）具有用于连接到颗粒检测器的出口，该装置被配置成使得来自蒸发室的含气体气体可以流入发生冷凝器和可冷凝物质在冷凝器中气体夹带的颗粒的冷凝，以增加颗粒的尺寸，使得它们能够被颗粒检测器检测。

4. 发明申请

WO2009125230A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2009125230A1
公开(公告)日：2009-10-15
申请号：PCT/GB2009/050358
申请日：2009-04-09
申请人： ASTEX THERAPEUTICS LIMITED , WILLIAMS, Marian , FREDERICKSON, Martyn
发明人： FREDERICKSON, Martyn
IPC分类号： C07D209/44 , A61K31/4035 , A61P35/00
CPC分类号： C07D295/155 , C07D209/44
摘要： The invention provides a compound of the formula (1 ): or a salt, solvate, N-oxide or tautomer thereof; wherein either R 1 is R 1 a and R 2 is R 2a ; or R 1 is R 1b and R 2 is R 2b ; provided that in each case at least one of R 1 and R 2 is other than hydrogen; R 1a and R 2a are the same or different and each is selected from hydrogen, C 1-4 alkyl, C 2-4 alkenyl and C 2-4 alkynyl wherein the C 1-4 alkyl is optionally substituted by C 1-2 alkoxy; R 1b and R 2b are the same or different and are selected from hydrogen, C(O)NR 4 R 5 , C(O)R 6 and C(O)OR 6 where R 6 is C 1-4 alkyl, R 4 and R 5 are both C 1-4 alkyl, or NR 4 R 5 forms a 4 to 7 membered saturated heterocyclic ring optionally containing a second heteroatom ring member selected from O, N or S and oxidised forms of N and S, the heterocyclic ring being optionally substituted by one or two C 1-4 alkyl groups and/or one or two oxo groups; and R 3 is a group (D): wherein the asterisk denotes the point of attachment to the isoindoline ring; but excluding acetic acid 5-acetoxy-4-isopropyl-2-[5-(4-methyl-piperazin-1 -ylmethyl)-1,3- dihydro-isoindole-2-carbonyl]-phenyl ester.
摘要翻译：本发明提供式（1）化合物或其盐，溶剂合物，N-氧化物或其互变异构体; 其中R1是R1a，R2是R2a; 或R1为R1b且R2为R2b; 条件是在每种情况下，R 1和R 2中的至少一个不是氢; R1a和R2a相同或不同，各自选自氢，C 1-4烷基，C 2-4烯基和C 2-4炔基，其中C 1-4烷基任选被C 1-2烷氧基取代; R1b和R2b相同或不同，并且选自氢，C（O）NR4R5，C（O）R6和C（O）OR6，其中R6是C1-4烷基，R4和R5都是C1-4烷基或 NR4R5形成任选地含有选自O，N或S的第二杂原子环成员和氧化形式的N和S的4至7元饱和杂环，杂环任选被一个或两个C 1-4烷基和/或一个或两个氧代基团; 并且R 3是基团（D）：其中星号表示与异吲哚啉环的连接点; 但不包括乙酸5-乙酰氧基-4-异丙基-2- [5-（4-甲基 - 哌嗪-1-基甲基）-1,3-二氢 - 异吲哚-2-羰基] - 苯酯。

5. 发明申请

WO2009022123A1 APPARATUS FOR STORING AND DISPENSING A WATER DISPERSIBLE SUBSTANCE AND RELATED METHOD 审中-公开
标题翻译：用于储存和分配水分散物质和相关方法的装置
公开(公告)号：WO2009022123A1
公开(公告)日：2009-02-19
申请号：PCT/GB2008/002722
申请日：2008-08-11
申请人： CONCENTRATED SOLUTIONS LIMITED , COLLINS, Mark
发明人： COLLINS, Mark
IPC分类号： B01F1/00 , B01F15/00 , B65D81/32 , B01F3/08 , B01F3/12
CPC分类号： B01F1/0033 , B01F15/00831 , B01F15/0085 , B65D81/3216 , B65D81/3272
摘要： The invention provides an apparatus for storing and dispensing a water dispersible substance, the apparatus comprising an outer container (2) and an inner container (10); wherein the outer container has an inlet and an outlet (8); the inner container has one or more openings through which water may pass and containing one or more dosage units comprising a water-swellable or water- soluble polymer, which polymer has encapsulated therein a water dispersible substance; and the outer and inner containers are configured such that in use, when the inner container is disposed inside the outer container, water may be passed through the outer and inner containers to elute the water dispersible substance from the polymer thereby to provide a solution of the substance.
摘要翻译：本发明提供一种用于储存和分配水分散物质的装置，该装置包括外部容器（2）和内部容器（10）; 其中所述外部容器具有入口和出口（8）; 内部容器具有一个或多个开口，水可通过该开口，并且包含一个或多个包含水溶胀性或水溶性聚合物的剂量单位，该聚合物在其中封装有水分散性物质; 外容器和内容器的构造使得在使用中，当内容器设置在外容器内时，水可以通过外容器和内容器以从聚合物中洗脱水分散物质，从而提供溶液物质。

6. 发明申请

WO2008139152A1 N-OXIDE-CONTAINING PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：含氧化氮的药物化合物
公开(公告)号：WO2008139152A1
公开(公告)日：2008-11-20
申请号：PCT/GB2008/001595
申请日：2008-05-09
申请人： SENTINEL ONCOLOGY LIMITED , BOYLE, Robert, George , TRAVERS, Stuart
发明人： BOYLE, Robert, George , TRAVERS, Stuart
IPC分类号： C07C291/04 , C07C311/32 , C07D401/12 , C07D403/14 , C07D417/14 , A61K31/13 , A61P35/00 , C07D413/14 , C07D417/12
CPC分类号： C07D401/12 , A61K9/0019 , A61K9/19 , A61K31/13 , C07C291/04 , C07C311/08 , C07C2603/26 , C07D403/14 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The invention provides a method of preparing a therapeutically active compound having reduced hERG activity, which method comprises: (a) selecting a non-N-oxide drug compound containing a basic tertiary amino group, wherein said non-N-oxide compound is known to have or is suspected of having a therapeutically unacceptable level of hERG inhibitory activity; (b) testing the non-N-oxide drug compound for hERG inhibitory activity; (c) reacting the non-N-oxide drug compound with an oxidising agent to form an N- oxide drug compound having an N-oxide at the basic tertiary amino group; (d) testing the N-oxide drug compound for hERG inhibitory activity; (e) testing the N-oxide drug compound for therapeutically useful activity; (f) comparing the hERG inhibitory activity of the N-oxide drug compound and non- N-oxide drug compound; and (g) when the N-oxide drug compound has therapeutically useful activity and has hERG activity which is at least ten fold less than the hERG inhibitory activity of the non-N-oxide drug compound, formulating the N-oxide drug compound for use in medicine. Also provided by the invention are novel compounds prepared by the aforementioned method and the use of the novel compounds in medicine.
摘要翻译：本发明提供了制备具有降低的hERG活性的治疗活性化合物的方法，该方法包括：（a）选择含有碱性叔氨基的非N-氧化物药物化合物，其中所述非N-氧化物化合物已知为有或怀疑具有治疗上不可接受的水平的hERG抑制活性; （b）测试非N-氧化物药物化合物的hERG抑制活性; （c）使非N-氧化物药物化合物与氧化剂反应形成具有碱性叔氨基的N-氧化物的N-氧化物药物化合物; （d）测试N-氧化物药物化合物的hERG抑制活性; （e）测试N-氧化物药物化合物用于治疗有用的活性; （f）比较N-氧化物药物化合物和非N-氧化物药物化合物的hERG抑制活性; 和（g）当N-氧化物药物化合物具有治疗有用的活性并且具有比非N-氧化物药物化合物的hERG抑制活性小至少十倍的hERG活性时，配制使用的N-氧化物药物化合物在医学上。本发明还提供了通过上述方法制备的新型化合物和该新型化合物在医药中的应用。

7. 发明申请

WO2008044034A1 HYDROBENZAMIDE DERIVATIVES AS INHIBITORS OF HSP90 审中-公开
标题翻译：盐酸衍生物作为HSP90的抑制剂
公开(公告)号：WO2008044034A1
公开(公告)日：2008-04-17
申请号：PCT/GB2007/003871
申请日：2007-10-12
申请人： ASTEX THERAPEUTICS LIMITED , FREDERICKSON, Martyn , LYONS, John, Francis , THOMPSON, Neil, Thomas , VINKOVIC, Mladen , WILLIAMS, Brian , WOODHEAD, Andrew James , WOOLFORD, Alison, Jo-Anne
发明人： FREDERICKSON, Martyn , LYONS, John, Francis , THOMPSON, Neil, Thomas , VINKOVIC, Mladen , WILLIAMS, Brian , WOODHEAD, Andrew James , WOOLFORD, Alison, Jo-Anne
IPC分类号： C07D209/44 , C07C65/05 , C07C69/02 , A61P35/00 , A61K31/496
CPC分类号： C07C67/317 , C07C59/08 , C07C67/313 , C07C69/92 , C07C235/60 , C07D209/44
摘要： The invention provides an acid addition salt of a compound of the formula (1) Also provided by the invention are processes for preparing the compound of formula (1) and alkyl analogues thereof, novel intermediates for use in the process and methods for preparing the intermediates. The invention also provides new medical uses of compounds of the formula (1) and its ethyl analogue.
摘要翻译：本发明提供式（1）化合物的酸加成盐本发明还提供了制备式（1）化合物及其烷基类似物的方法，用于该方法的新中间体和制备中间体的方法。本发明还提供式（1）化合物及其乙基类似物的新的医学用途。

8. 发明申请

WO2008044027A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2008044027A2
公开(公告)日：2008-04-17
申请号：PCT/GB2007/003860
申请日：2007-10-12
申请人： ASTEX THERAPEUTICS LIMITED , CONGREVE, Miles Stuart , FAZAL, Lyndsey Helen , FREDERICKSON, Martyn , MURRAY, Christopher William , O'BRIEN, Michael Alistair , WOODHEAD, Andrew James , LYONS, John, Francis , THOMPSON, Neil Thomas
发明人： CONGREVE, Miles Stuart , FAZAL, Lyndsey Helen , FREDERICKSON, Martyn , MURRAY, Christopher William , O'BRIEN, Michael Alistair , WOODHEAD, Andrew James , LYONS, John, Francis , THOMPSON, Neil Thomas
CPC分类号： C07D403/06 , C07D209/08 , C07D209/44 , C07D215/08 , C07D215/14 , C07D217/06 , C07D401/04 , C07D401/12 , C07D401/14 , C07D471/04 , C07D471/08 , C07D471/10 , C07D491/08 , C07D491/10 , C07D491/107 , C07D491/18
摘要： The invention provides a compound for use in medicine, the compound being a compound of the formula (Vl 0 ) or a salt, solvate, tautomer or N-oxide thereof: wherein the bicyclic group: is selected from the structures C1, C5 and C6: wherein n is 0, 1, 2 or 3; R 1 : is„ hydrogen, hydroxy, or O-R z; R 2a is hydroxy, methoxy or O-R z; provided that at least one of R 1 and R 2a is O-R z; R z is L p -R p1 ; SO 3 H; a glucuronide residue; a mono-, di- or tripeptide residue; or; L p is a bond, C=O, (C=O)O, (C=O)NR p1 or S(O) x NR p1 ; x is 1 or 2; R p1 is hydrogen or a an optionally substituted C 1-25 hydrocarbyl group containing 0, 1 or 2 carbocyclic rings and 0, 1, 2, 3, 4, 5 or 6 carbon-carbon multiple bonds, provided that R p1 is not hydrogen when L p is a bond, C=O or (C=O)O; and provided also that O-R z does not contain an 0-0 moiety; and excluding compounds wherein R1 is hydroxy and R2a is methoxy; Rp2 and Rp3 are the same or different and each is a group R p1; and R 3 , R 4a , R 8 and R 10 are defined in the claims. The compounds of formula (Vl0) are pro-drugs of parent compounds wherein R 1 and/or R 2a are hydroxy, wherein the parent compounds have Hsp90 inhibiting activity.
摘要翻译：本发明提供了一种用于医药的化合物，该化合物为下式化合物：其盐，溶剂化物，互变异构体或N-氧化物：其中双环基团选自：结构C1，C5和C6：其中n为0,1,2或3; R 1是氢，羟基或OR z; R 2是羟基，甲氧基或OR z; O / O >条件是R 1和R 2 2中的至少一个是OR z; R z是L SUP > p p> SO 3 H;葡糖苷酸残基;单 - ，二 - 或三肽残基;或●L < / SUP>是键，C = O，（C = O）O，（C = O）NR P1或S（O）x NR 6 x为1或2; R p1为氢或任选取代的含0,1或2个碳环的C 1-25烃基和0 ，1,2,3,4,5或6个碳 - 碳多重键，条件是当P = O时，R p2不是氢，C = O或（C = O）O;并且也提供OR 0不含0-0部分;并且不包括其中R 1是羟基并且R 2a是甲氧基的化合物; Rp2和Rp3相同或不同，每个是基团R p1; R 3和R 3，R 4a，R 8和R 10 是定义在权利要求中。式（V10）化合物是其中R 1和/或R 2a的羟基的母体化合物的前体药物，其中母体化合物具有Hsp90抑制活性。

9. 发明申请

WO2008015423A1 QUINOLINE AND QUINOXALINE N-OXIDES AS CHK-1 INHIBITORS 审中-公开
标题翻译：喹啉和喹喔啉N-氧化物作为CHK-1抑制剂
公开(公告)号：WO2008015423A1
公开(公告)日：2008-02-07
申请号：PCT/GB2007/002918
申请日：2007-08-01
申请人： SENTINEL ONCOLOGY LIMITED , BOYLE, Robert, George , TRAVERS, Stuart
发明人： BOYLE, Robert, George , TRAVERS, Stuart
IPC分类号： C07D241/52 , A61K31/498 , A61P35/00
CPC分类号： C07D241/52
摘要： The invention provides compounds of the formula (1) or salts, solvates or tautomers thereof; wherein Y 1 and Y 2 are both N + -O - or one of Y 1 and Y 2 is N and the other is N + -O - ; G is CH 2 , O, NH, NHCO or CONH; A is a group (CH 2 ) n where n is 1 to 4 provided that when G is O or NH, n is at least 2; Q is N or N + -O - ; V 2 is nitrogen or a group CR 5 ; V 3 is nitrogen or a group CR 5 ; V 4 is nitrogen or CH; provided that no more than two of V 2 , V 3 and V 4 are nitrogen; R 1 and R 2 are the same or different and each is hydrogen or a substituent R 6 ; R 3 and R 4 are the same or different and each is hydrogen or C 1-4 alkyl; or R 3 and R 4 together with the nitrogen atom to which they are attached form an azetidine, pyrrolidine, piperidine, piperazine, N-methylpiperazine or morpholine group; provided that when Q is N + -O - , then R 3 and R 4 are both other than hydrogen; R 5 is hydrogen or a substituent R 6 ; and R 6 is as defined in the claims. The compounds of formula (1) are reduced under hypoxic conditions such as those found in solid tumour cells to give compounds that inhibit or modulate Chk-1 kinase.
摘要翻译：本发明提供式（1）化合物或其盐，溶剂合物或互变异构体; 其中Y 1和Y 2都是N O - ， - O - O - 或Y 1 - / SUP>和Y 2是N，另一个是N + - O - O - G是CH 2，O，NH，NHCO或CONH; A是一个基团（CH 2）n n其中n是1至4，条件是当G是O或NH时，n至少为2; Q是N或N + O - - O - V 2是氮或基团CR 5; V 3是氮或基团CR 5; V 4是氮或CH; 条件是V 2，V 3和V 4中不超过2个为氮; R 1和R 2相同或不同，各自为氢或取代基R 6; R 3和R 4相同或不同，各自为氢或C 1-4烷基; 或R 3和R 4与它们所连接的氮原子一起形成氮杂环丁烷，吡咯烷，哌啶，哌嗪，N-甲基哌嗪或吗啉基团; 条件是当Q是N + O - O - 时，R 3和R 4都不是氢 ; R 5是氢或取代基R 6; 和R 6如权利要求中所定义。式（1）的化合物在例如在实体瘤细胞中发现的缺氧条件下被还原，得到抑制或调节Chk-1激酶的化合物。

10. 发明申请

WO2007125320A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2007125320A1
公开(公告)日：2007-11-08
申请号：PCT/GB2007/001517
申请日：2007-04-25
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESERARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , SAXTY, Gordon , VERDONK, Marinus, Leendert , CALDWELL, John , COLLINS, Ian , CHEUNG, Kwai-Ming , DA FONSECA MCHARDY, Tatiana, Faria
发明人： SAXTY, Gordon , VERDONK, Marinus, Leendert , CALDWELL, John , COLLINS, Ian , CHEUNG, Kwai-Ming , DA FONSECA MCHARDY, Tatiana, Faria
IPC分类号： C07D471/04 , C07D495/04 , C07D498/04 , A61K31/506 , A61P35/00
CPC分类号： C07D471/04 , C07D495/04
摘要： Compounds of the formula (I), and salts, solvates, tautomers and N-oxide thereof; wherein TG is selected from groups (1) and (2): wherein the asterisk (*) represents the point of attachment of the group E to the group X; R la is an optionally substituted aryl or heteroaryl group; R lb is hydrogen or a group Rla; X is an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 are heteroatoms selected from O, N and S; and A, E, R 2 , R 3 , R 4 , Q 1 and Q 2 are as defined in the claims; provided that when E is aryl or heteroaryl, then Q 2 is other than a bond; and further provided that the moiety (a) is other than a group (BG1) or (BG2); wherein (BGl) and (BG2) are each optionally substituted; T is N or CR Z ; J 1 -J 2 is selected from N=C(R Z ), (R Z )C=N, (R Z )N-C(O), (R Z ) 2 C-C(O), N=N and (R Z )C=C(R 6 ); J 4 - J 3 is a group N=C(R Z ) or a group (R Z )N-CO; and R Z is hydrogen or a substituent. The compounds of the formula (I) have PKA and PKB kinase inhibiting activity and are useful in the treatment of cancers.
摘要翻译：式（I）化合物及其盐，溶剂合物，互变异构体和N-氧化物; 其中TG选自基团（1）和（2）：其中星号（*）表示基团E与基团X的连接点; R 1是任选取代的芳基或杂芳基; R 1b是氢或基团R 1a; X是具有8至12个环成员的任选取代的双环杂环基，其中多达5个是选自O，N和S的杂原子; 和A，E，R 2，R 3，R 4，Q 1和Q 2 如权利要求中所定义; 条件是当E是芳基或杂芳基时，则Q 2不是键; 并且进一步规定部分（a）不是基团（BG1）或（BG2）; 其中（BG1）和（BG2）各自任选被取代; T是N或CR Z; J <1> 1 2 选自N = C（R Z），（R Z）Z = NC（O），（R）Z CC（O），N = N和（R O） >ž）C = C（R ^{6 ）; J 3 - N 3是基团N = C（R Z）或基团（R Z），的N- CO; 并且R Z是氢或取代基。式（I）化合物具有PKA和PKB激酶抑制活性，可用于治疗癌症。}

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