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1. 发明申请

WO2012140170A2 AN APPARATUS FOR GENERATING HEAT 审中-公开
标题翻译：用于产生热量的装置
公开(公告)号：WO2012140170A2
公开(公告)日：2012-10-18
申请号：PCT/EP2012/056727
申请日：2012-04-12
申请人： COLLINS, Mark
发明人： COLLINS, Mark
IPC分类号： F24J1/00
CPC分类号： C01B3/08 , C01B3/06 , F24D15/00 , F24D2200/16 , F24V30/00 , Y02E60/36
摘要： The invention provides an apparatus for heating a heatable liquid, which apparatus comprises: (i) a first storage vessel containing (a) a slurry or suspension of a metal powder in water; (ii) a second storage vessel containing (b) a solution of an alkali metal hydroxide; (iii) a reaction vessel in fluid communication with (i) and (ii) and having at least one inlet through which (a) and (b) can be introduced into the reaction vessel so that they react to form reaction products, a first outlet for removal of a liquid reaction product stream containing reaction products of (a) and (b) and a second outlet for removal of gaseous materials generated by reaction of (a) and (b); (iv) a first heat exchanger disposed in or on the reaction vessel, the heatable liquid being arranged to flow through the first heat exchanger so that heat produced by reaction between (a) and (b) in the reaction vessel is transferred to the heatable liquid; (v) at least one ancillary heat exchanger disposed downstream of the first outlet for extracting heat from the liquid reaction product stream, wherein the ancillary heat exchanger is arranged to transfer heat to the heatable liquid or is arranged to pre-heat one or both of (a) and (b) prior to introduction into the reaction vessel; (vi) a separator, linked to the second outlet, for collecting hydrogen gas formed by the reaction of (a) with (b); (vii) a burner for the hydrogen gas; and (viii) a further heat exchanger associated with the burner for transferring heat obtained from combustion of the hydrogen gas to the heatable liquid.
摘要翻译：本发明提供了一种用于加热可加热液体的装置，该装置包括：（i）第一储存容器，其包含（a）金属粉末在水中的浆液或悬浮液; （ii）含有（b）碱金属氢氧化物溶液的第二储存容器; （iii）与（i）和（ii）流体连通并且具有至少一个入口的反应容器，其中（a）和（b）可以通过该入口引入反应容器中，使得它们反应以形成反应产物，第一用于除去含有（a）和（b）的反应产物的液体反应产物流的出口和用于除去由（a）和（b）反应产生的气态物质的第二出口; （iv）设置在反应容器内或上的第一热交换器，所述可加热液体被布置成流过第一热交换器，使得通过反应容器中的（a）和（b）之间的反应产生的热量被转移到可加热的液体; （v）设置在第一出口下游的至少一个辅助热交换器，用于从液体反应产物流中提取热量，其中辅助热交换器布置成将热量传递到可加热液体，或者被布置成预热一个或两个（a）和（b）在引入反应容器之前; （vi）连接到第二出口的用于收集由（a）与（b）的反应形成的氢气的分离器; （vii）用于氢气的燃烧器; 和（viii）与燃烧器相关联的另外的热交换器，用于将从氢气燃烧获得的热量传递到可加热液体。

2. 发明申请

WO2006040569A1 THIOPHENE AMIDE COMPOUNDS FOR USE IN THE TREATMENT OR PROPHYLAXIS OF CANCERS 审中-公开
标题翻译：用于治疗或预防癌症的噻吩类化合物
公开(公告)号：WO2006040569A1
公开(公告)日：2006-04-20
申请号：PCT/GB2005/003957
申请日：2005-10-14
申请人： ASTEX THERAPEUTICS LIMITED , GILL, Adrian, Liam , LYONS, John, Francis , THOMPSON, Neil, Thomas
发明人： GILL, Adrian, Liam , LYONS, John, Francis , THOMPSON, Neil, Thomas
IPC分类号： A61K31/5386 , A61K31/4155 , A61K31/5377 , A61K31/496 , A61K31/4439 , A61P35/00
CPC分类号： A61K31/4155 , A61K31/4439 , A61K31/496 , A61K31/5377 , A61K31/5386
摘要： The invention provides the use of a compound for the manufacture of a medicament for the prophylaxis or treatment of a cancer or a para-neoplastic effect associated with a cancer, the para-neoplastic effect being other than cachexia, and the compound being a compound of the formula (I), or a salt, solvate or N-oxide thereof, wherein: R 1 and R 2 are the same or different and each is selected from hydrogen, C 1-4 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; R 3 is an aryl or heteroaryl group of 5 to 12 ring members optionally substituted by one or more substituent groups R 7 wherein R 7 is as defined in the claims; R 4 is a group YR 5 or a group R 6 ; Y is NH, O or S; R 5 is selected from (a) optionally substituted carbocyclic and heterocyclic groups having from 3 to 12 ring members; and (b) optionally substituted C 1-8 hydrocarbyl 20 groups; and R 6 is an optionally substituted heterocyclic group having from 4 to 12 ring members and containing at least one ring nitrogen atom through which R 6 is linked to the adjacent carbonyl group.
摘要翻译：本发明提供化合物在制备用于预防或治疗与癌症相关的癌症或副肿瘤作用的药物中的用途，所述副肿瘤作用不是恶病质，所述化合物是化合物式（I）或其盐，溶剂合物或N-氧化物，其中：R

3. 发明申请

WO2006038025A1 OSTOMY BAGS 审中-公开
标题翻译： OSTOMY包包
公开(公告)号：WO2006038025A1
公开(公告)日：2006-04-13
申请号：PCT/GB2005/003870
申请日：2005-10-07
申请人： WELLAND MEDICAL LIMITED , REIDER, Martina , FINN, Richard , SMITH, Rory, James, Maxwell
发明人： REIDER, Martina , FINN, Richard , SMITH, Rory, James, Maxwell
IPC分类号： A61F5/443
CPC分类号： A61F5/443 , A61F5/448 , A61F2013/00676 , A61F2013/00748
摘要： The invention provides an adhesive flange for securing an ostomy bag to the body of a patient about a stomal opening; the adhesive flange comprising a support member (2) having secured to one side thereof an ostomy bag (6) or means for connection to an ostomy bag, and having on the other side thereof a layer (4) of a water-degradable bioadhesive (e.g. a hydrocolloid adhesive or hydrogel adhesive) for securing the support member (2) to the body of the patient; the support member (2) and adhesive layer (4) having an aperture (8) for locating about the stomal opening and through which stomal waste can pass; characterized in that the aperture is lined with a water repellent material (10) selected from silicones and non-foamed polyurethane that prevents or inhibits lateral migration of water into the bioadhesive layer (4).
摘要翻译：本发明提供了一种用于将造口袋固定到患者身体关于气孔开口的粘合凸缘; 粘合剂法兰包括一个固定在其一侧的造口袋（6）的支撑件（2）或用于与造口袋连接的装置，并且在另一侧上具有可降解水的生物粘合剂层（4）例如水胶体粘合剂或水凝胶粘合剂），用于将支撑构件（2）固定到患者的身体; 所述支撑构件（2）和粘合剂层（4）具有用于围绕所述气孔开口定位并且通过所述孔口废物可以通过的孔（8）其特征在于，孔径衬有选自硅氧烷和非发泡聚氨酯的防水材料（10），其防止或抑制水进入生物粘附层（4）的侧向迁移。

4. 发明申请

WO2020074461A1 TYK2 KINASE INHIBITORS 审中-公开
公开(公告)号：WO2020074461A1
公开(公告)日：2020-04-16
申请号：PCT/EP2019/077118
申请日：2019-10-07
申请人： SAREUM LIMITED
发明人： READER, John Charles
IPC分类号： C07D263/48 , A61P29/00 , A61P37/00 , A61K31/541
摘要： The invention provides compounds of the formula (1): (1) or a salt or tautomer thereof; wherein R 1 is hydrogen or fluorine, pharmaceutical compositions containing the compounds and medical uses of the compounds (for example, in the treatment of inflammatory or immune disorders).

5. 发明申请

WO2006046024A1 ORTHO- CONDENSED PYRIDINE AND PYRIMIDINE DERIVATIVES (E. G. PURINES) AS PROTEIN KINASES INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的ORTHO-浓缩的吡啶和吡嗪衍生物（E.G.PININES）
公开(公告)号：WO2006046024A1
公开(公告)日：2006-05-04
申请号：PCT/GB2005/004119
申请日：2005-10-25
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , BERDINI, Valerio , BOYLE, Robert, George , SAXTY, Gordon , WALKER, David, Winter , WOODHEAD, Steven, John , WYATT, Paul, Graham , CALDWELL, John , COLLINS, Ian , DA FONSECA, Tatiana, Faria
发明人： BERDINI, Valerio , BOYLE, Robert, George , SAXTY, Gordon , WALKER, David, Winter , WOODHEAD, Steven, John , WYATT, Paul, Graham , CALDWELL, John , COLLINS, Ian , DA FONSECA, Tatiana, Faria
IPC分类号： A61K31/52 , A61K31/519 , C07D473/34 , A61K31/437 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , A61K31/4545 , A61K31/519 , A61K31/52 , A61K31/522 , C07D473/34 , C07D487/04
摘要： The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR 5 ; J l -J 2 is N=C(R 6 ), (R 7 )C=N, (R 8 )N-C(O), (R 8 ) 2 C-C(O), N=N or (R 7 )C=C(R 6 ); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q 1 is a bond or a saturated C 1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONR q or NR q CO where R q is hydrogen or methyl, or R q is a C 1-4 alkylene chain linked to R 1 or a carbon atom of Q 1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q 1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q 2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group may optionally bear one or more substituents selected from fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the G group; and provided that when E is aryl or heteroaryl, then Q 2 is other than a bond; G is hydrogen, NR 2 R 3 , OH or SH provided that when E is aryl or heteroaryl and Q 2 is a bond, then G is hydrogen; R 1 is hydrogen or an aryl or heteroaryl group, with the proviso that when R 1 is hydrogen and G is NR 2 R 3 , then Q 2 is a bond; and R 2 , R 3 , R 4 , R 6 and R 8 are as defined in the claims.
摘要翻译：本发明提供了用作蛋白激酶B抑制剂的化合物，该化合物是式（I）化合物或其盐，溶剂合物，互变异构体或N-氧化物，其中T是N或CR 5 >; N = C（R 6），（R 7）C = N，（R 8）NC（O），（R 8）2 CC（O），N = N或（R 7））C = C（R ^{6 ）; E是5或6个环成员的单环碳环或杂环基，杂环基含有至多3个选自O，N和S的杂原子; Q 1是一个键或饱和的C 1-3烃连接基团，连接基团中的一个碳原子任选地被氧或氮原子代替，或相邻的一对碳原子可以被CONR Q或Q Q取代，其中R q是氢或甲基，或R 0 q是与R 1连接的C 1-4亚烷基链或Q 1的碳原子以形成环状的部分; 并且其中连接基团Q 1的碳原子可以任选地具有一个或多个选自氟和羟基的取代基; Q 2是含有1至3个碳原子的键或饱和烃连接基团，其中连接基团中的一个碳原子可以任选被氧或氮原子取代; 并且其中所述连接基团的碳原子可以任选地具有一个或多个选自氟和羟基的取代基，条件是当存在的羟基不相对于G基团位于碳原子a时; 并且条件是当E是芳基或杂芳基时，则Q 2不是键; G是氢，NR 2 R 3，OH或SH，条件是当E是芳基或杂芳基且Q 2是键时，则G 是氢; R 1是氢或芳基或杂芳基，条件是当R 1是氢并且G是NR 2 R 3 ，则Q 2是一个键; 和R 2，R 2，R 3，R 4，R 4， SUP＆gt;和R＆gt; 8如权利要求中所定义。}

6. 发明申请

WO2006046023A1 ORTHO- CONDENSED PYRIDINE AND PYRIMIDINE DERIVATIVES (E. G. PURINES) AS PROTEIN KINASES INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的ORTHO-浓缩的吡啶和吡嗪衍生物（E.G.PININES）
公开(公告)号：WO2006046023A1
公开(公告)日：2006-05-04
申请号：PCT/GB2005/004115
申请日：2005-10-25
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , BERDINI, Valerio , BOYLE, Robert, George , SAXTY, Gordon , VERDONK, Marinus, Leendert , WOODHEAD, Steven, John , WYATT, Paul, Graham , SORE, Hannah, Fiona , CALDWELL, John , COLLINS, Ian , DA FONSECA, Tatiana, Faria , DONALD, Alastair
发明人： BERDINI, Valerio , BOYLE, Robert, George , SAXTY, Gordon , VERDONK, Marinus, Leendert , WOODHEAD, Steven, John , WYATT, Paul, Graham , SORE, Hannah, Fiona , CALDWELL, John , COLLINS, Ian , DA FONSECA, Tatiana, Faria , DONALD, Alastair
IPC分类号： A61K31/52 , A61K31/519 , C07D473/34 , A61K31/437 , C07D471/04 , C07D487/04 , C07D473/00
CPC分类号： C07D471/04 , C07D473/00 , C07D473/34 , C07D487/04
摘要： The invention provides a compound for use in the prophylaxis or treatment of a disease state or condition mediated by protein kinase B, the compound having the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR 5 ; J 1 -J 2 is N=C(R 6 ), (R 7 )C=N, (R 8 )N-C(O), (R 8 ) 2 C-C(O), N=N or (R 7 )C=C(R 6 ); A is an optionally substituted saturated C 1-7 hydrocarbon linker group having a maximum chain length of 5 atoms extending between R 1 and NR 2 R 3 and a maximum chain length of 4 atoms extending between E and NR 2 R 3 , one of the carbon atoms in the linker group being optionally replaced by oxygen or nitrogen; E is a monocyclic or bicyclic carbocyclic or heterocyclic group or an acyclic group X-G wherein X is CH 2 , O, S or NH and G is a C 1-4 alkylene chain wherein one of the carbon atoms is optionally replaced by O, S or NH; R 1 is hydrogen or an aryl or heteroaryl group; R 2 and R 3 are each hydrogen, optionally substituted C 1-4 hydrocarbyl or optionally substituted C 1-4 acyl; or NR 2 R 3 forms an imidazole group or a saturated monocyclic heterocyclic group having 4-7 ring members; or NR 2 R 3 and A together form a saturated monocyclic heterocyclic group having 4-7 ring members which is optionally substituted by C 1-4 alkyl; or NR 2 R 3 and the adjacent carbon atom of linker group A together form a cyano group; or R 1 , A and NR 2 R 3 together form a cyano group; and R 4 , R 5 , R 6 , R 7 and R 8 are each independently selected from hydrogen and various substituents as defined in the claims.
摘要翻译：本发明提供了一种用于预防或治疗由蛋白激酶B介导的疾病状态或病症的化合物，其具有式（I）：或其盐，溶剂合物，互变异构体或N-氧化物，其中T为N或 CR ^{5 ; J 1是N = C（R 6），（R 7）C = N，（R 8）NC（O），（R 8）2 CC（O），N = N或（R 7））C = C（R ^{6 ）; A是在R 1和R 2之间延伸的最大链长为5个原子的任选取代的饱和C 1 -C 7烃连接基团连接基团中的一个碳原子是任选的，并且在E和NR 2 R 3之间延伸的最大链长为4个原子用氧或氮代替; E是单环或双环碳环或杂环基或非环基XG，其中X是CH 2，O，S或NH，G是C 1-4亚烷基链其中一个碳原子任选被O，S或NH取代; R 1是氢或芳基或杂芳基; R 2和R 3各自为氢，任选取代的C 1-4 - 烃基或任选取代的C 1-4 - >酰基; 或NR 2 R 3形成具有4-7个环成员的咪唑基或饱和单环杂环基; 或NR 2 R 3和A一起形成具有4-7个环成员的饱和单环杂环基，其任选被C 1-4烷基取代，烷基; 或NR 2 R 3和连接基团A的相邻碳原子一起形成氰基; 或R 1，A和NR 2 R 3一起形成氰基; 和R 4，R 5，R 6，R 7和R 8，各自独立地选自氢和权利要求中所定义的各种取代基。}}

7. 发明申请

WO2012168456A1 A METHOD OF FASTENING A WALL OR ROOFING PANEL 审中-公开
标题翻译：一种墙壁或屋面板的方法
公开(公告)号：WO2012168456A1
公开(公告)日：2012-12-13
申请号：PCT/EP2012/060936
申请日：2012-06-08
申请人： JACKSON, Patrick, Steven
发明人： JACKSON, Patrick, Steven
IPC分类号： E04D3/36 , F16B13/06 , E04F13/08
CPC分类号： E04F13/0837 , E04D3/3606 , F16B13/061
摘要： The invention provides a method of securing an external cladding panel to a building support member using a fastener, wherein the fastener comprises a tubular body (1) having a shaft (2) disposed therein, the shaft (2) having a compression member (4) mounted or formed on a distal end thereof and having at a proximal end thereof a rotatable member (7) which, when rotated, serves to draw the compression member (4) in a rearwards direction, the fastener having at least one deformable member (3b-3c-3d) which surrounds the shaft (2) and is disposed axially between the compression member (4) and the tubular body (1), and wherein the fastener is provided with engagement means for engaging the building support member; which method comprises: (a) identifying a fastening hole in the external cladding panel or, where there is no fastening hole, forming such a hole; (b) inserting the fastener into the hole from an internal side of the external cladding panel so that the compression member on the shaft and the deformable member protrude through the hole and beyond the external cladding panel and so that the engagement means of the fastener engages the building support member; (c) from a location on the internal side of the external cladding panel, rotating the rotatable member thereby to draw the compression member in a rearwards direction to compress and deform the deformable member so that it expands radially outwardly on an external side of the external cladding panel to a width greater than the hole thereby to secure the external cladding panel to the building support member. Also provided are fasteners for use in the method.
摘要翻译：本发明提供一种使用紧固件将外部包覆板固定到建筑支撑构件的方法，其中紧固件包括其中设置有轴（2）的管状体（1），轴（2）具有压缩构件（4））安装或形成在其远端上，并且在其近端处具有可旋转构件（7），所述可旋转构件（7）当旋转时用于沿向后方向拉动所述压缩构件（4），所述紧固件具有至少一个可变形构件包围所述轴（2）并且轴向地设置在所述压缩构件（4）和所述管状体（1）之间，并且其中所述紧固件设置有用于接合所述建筑物支撑构件的接合装置; 该方法包括：（a）识别外部包覆板中的紧固孔，或者在没有紧固孔的情况下形成这样的孔; （b）从外部包覆板的内侧将紧固件插入到孔中，使得轴上的压缩构件和可变形构件穿过孔突出并超出外部包覆面板，使得紧固件的接合装置接合建筑物支撑构件; （c）从外部包覆面板的内侧的位置旋转可旋转构件，从而沿着向后方向拉伸压缩构件，以使可变形构件压缩和变形，使得其在外部外侧径向向外扩张覆盖板的宽度大于孔的宽度，从而将外部包覆板固定到建筑支撑构件上。还提供了用于该方法的紧固件。

8. 发明申请

WO2006051290A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2006051290A2
公开(公告)日：2006-05-18
申请号：PCT/GB2005/004323
申请日：2005-11-09
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , BERDINI, Valerio , BOYLE, Robert, George , SAXTY, Gordon , VERDONK, Marinus, Leendert , WOODHEAD, Steven, John , WYATT, Paul, Graham , SORE, Hannah, Fiona , WALKER, David, Winter , CALDWELL, John , COLLINS, Ian
发明人： BERDINI, Valerio , BOYLE, Robert, George , SAXTY, Gordon , VERDONK, Marinus, Leendert , WOODHEAD, Steven, John , WYATT, Paul, Graham , SORE, Hannah, Fiona , WALKER, David, Winter , CALDWELL, John , COLLINS, Ian
IPC分类号： A61K31/505 , A61P35/00 , C07D239/88 , C07D401/12 , C07D401/04 , C07D401/06 , C07D403/12
CPC分类号： C07D403/12 , A61K31/505 , C07D239/88 , C07D239/91 , C07D239/96 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04
摘要： The invention provides a compound of the formula (I) or a salt, solvate, tautomer or N-oxide thereof for use in the treatment or prophylaxis of a disease state or condition mediated by protein kinase A and/or protein kinase B, wherein the ring Q is a benzene ring; J 2 -J 1 is N=CR 7 or R 1a N-CO; G is OH or NR 5 R 6 ; E is CONR 7 , NR 7 CO, C(R 8 )=C(R 8 ) or (X) m (CR 8 R 8a ) n where X is O, S or NR 7 ; provided that when J 2 -J 1 is R 1a N-CO, E is other than NR 7 CO; m and n are each 0 or 1, where m + n = 1 or 2; A is a bond and R 4 and R 4a are absent, or A is a saturated optionally substituted C 1-7 hydrocarbon linker group having a maximum chain length of 5 atoms extending between E and G, one carbon atom in the linker group A being optionally replaced by O or N; R 1 , R la , R 2 , and R 3 are each H; halogen; C 1-6 hydrocarbyl optionally substituted by halogen, OH or C 1-2 alkoxy; CN; CONHR 8 ; NH 2 ; NHCOR 10 or NHCONHR 10 ; R 4 is H or C 1-4 alkyl; R 4a is H, C 1-4 alkyl or a group R 9 ; R 5 and R 6 are each selected from H, R 9 and C 1-4 hydrocarbyl optionally substituted by halogen, C 1-2 alkoxy or R 9 ;or NR 5 R 6 forms a saturated 4-7 membered monocyclic heterocyclic group; R 7 is H or C 1-4 alkyl; R 8 and R 8a each H or saturated C 1-4 hydrocarbyl optionally substituted by fluorine; R 9 is a monocyclic or bicyclic carbocyclic or heterocyclic group containing up to 3 ring heteroatoms selected from N, O and S; or R 4 , R 4a and A together form a saturated monocyclic 4-7 membered heterocycle; or NR 5 R 6 , R 4 and A form a saturated 4-7 membered monocyclic heterocycle; or R 4 , together with R 7 or R 8 and A and E form a 4-7 membered saturated monocyclic heterocycle; or NR 5 R 6 and R 7 or R 8 together with A and E form a 4-7 membered saturated monocyclic heterocycle; and R 10 is optionally substituted phenyl or benzyl.
摘要翻译：本发明提供式（I）化合物或其盐，溶剂化物，互变异构体或N-氧化物，用于治疗或预防由蛋白激酶A和/或蛋白激酶B介导的疾病状态或病症，其中环Q是苯环; N 2是N = CR 7或R 1a N-CO; G是OH或NR 5 R 6; E是CONR 7，NR 7 CO，C（R 8）= C（R 8）或（R 8）其中X是O，S或NR 7（其中X是O，S或NR 7）其中X是O，S或NR 7 ; 条件是当J 2是-J 1，R 1是N-CO时，E不是NR 7 CO ; m和n各自为0或1，其中m + n = 1或2; A是键，R 4和R 4a不存在，或A是饱和的任选取代的C 1-7烃连接基团，其具有在E和G之间延伸的5个原子的最大链长度，连接基团A中的一个碳原子任选地被O或N取代; R 1，R 2，R 2，R 3和R 3各自为H; 卤素; 任选被卤素，OH或C 1-12烷氧基取代的C 1-6烷基; CN; CONHR ^{8 ; NH _{2 ; NHCOR 10或NHCONHR 10; R 4是H或C 1-4烷基; R 4a是H，C 1-4烷基或基团R 9; R 5和R 6各自选自H，R 9和C 1-4烃基，任选被卤素，C 1-2烷氧基或R 9或NR 5 R 6形成饱和的4-7 元环杂环基; R 7是H或C 1-4烷基; 每个H或任选被氟取代的饱和C 1-4烃基的R 8和R 8 8a; R 9是含有至多3个选自N，O和S的环杂原子的单环或双环碳环或杂环基; 或R 4，R 4a和A一起形成饱和单环4-7元杂环; 或NR 5 R 6，R 4和A形成饱和的4-7元单环杂环; 或R 4，...，以及R 7或R 8，A和E形成4-7元饱和单环杂环; 或NR 5 R 6和R 7或R 8与A和E一起形成4-7元环饱和单环杂环; R 10是任选取代的苯基或苄基。}}

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