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1. 发明申请

WO1998002438A1 BICYCLIC HETEROAROMATIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：双相异构化合物作为蛋白酪氨酸激酶抑制剂
公开(公告)号：WO1998002438A1
公开(公告)日：1998-01-22
申请号：PCT/EP1997003674
申请日：1997-07-11
申请人： GLAXO GROUP LIMITED , COCKERILL, George, Stuart , CARTER, Malcolm, Clive , GUNTRIP, Stephen, Barry , SMITH, Kathryn, Jane
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D471/04
CPC分类号： C07D493/08 , C07D209/08 , C07D231/56 , C07D235/08 , C07D401/06 , C07D407/12 , C07D471/04
摘要： Substituted heteroaromatic compounds, and in particular substituted bicyclic heteroaromatic compounds of formula (I), wherein X is N or CH; A represents a fused 5, 6 or 7-membered heterocyclic ring containing 1 to 5 heteroatoms which may be the same or different and which are selected from N, O or S(O)m, wherein m is as defined above, the heterocyclic ring containing a total of 1, 2 or 3 double bonds inclusive of the bond in the pyridine or pyrimidine ring to which it is fused, with the provisos that the heterocyclic ring does not form part of a purine and that the fused heterocyclic ring does not contain two adjacent O or S(O)m atoms. U represents a 5 to 10-membered mono or bicyclic ring system in which one or more of the carbon atoms is optionally replaced by a heteroatom independently selected from N, O and S(O)m, wherein m is 0,1 or 2 and wherein the ring system is substituted by at least one independently selected R group and is optionally substituted by at least one indepenently selected R group, with the proviso that U does not represent phenyl; are protein tyrosine kinase inhibitors. The compounds are described as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of cancer and psoriasis.
摘要翻译：取代的杂芳族化合物，特别是式（I）的取代的双环杂芳族化合物，其中X是N或CH; A表示稠合的5,6或7元杂环，其含有1至5个可以相同或不同的杂原子，并且其选自N，O或S（O）m，其中m如上定义，杂环包含总共1,2或3个双键，包括其所融合的吡啶或嘧啶环中的键，条件是杂环不形成嘌呤的一部分，并且稠合杂环不含两个相邻的O或S（O）m原子。 U表示5至10元单环或双环系，其中一个或多个碳原子任选被独立地选自N，O和S（O）m的杂原子取代，其中m为0,1或2，以及其中所述环系被至少一个独立选择的R 6基团取代，并且任选地被至少一个独立选择的R 4基团取代，条件是U不表示苯基; 是蛋白酪氨酸激酶抑制剂。这些化合物被描述为它们的制备方法，包括这些化合物的药物组合物及其在药物中的用途，例如治疗癌症和牛皮癣。

2. 发明申请

WO1997013771A1 BICYCLIC HETEROAROMATIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白酪氨酸激酶抑制剂的双相异构化合物
公开(公告)号：WO1997013771A1
公开(公告)日：1997-04-17
申请号：PCT/EP1996004399
申请日：1996-10-10
申请人： GLAXO GROUP LIMITED , COCKERILL, George, Stuart , GUNTRIP, Stephen, Barry , McKEOWN, Stephen, Carl , PAGE, Martin, John , SMITH, Kathryn, Jane , VILE, Sadie , HUDSON, Alan, Thomas , BARRACLOUGH, Paul , FRANZMANN, Karl, Witold
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D495/04
摘要： Substituted heteroaromatic compounds of formula (A) wherein X is N or CH; in which (a) represents a fused 5, 6 or 7-membered heterocyclic ring and R is a group ZR wherein Z is joined to R through a (CH2)p group in which p is 0, 1, or 2 and Z represents a group V(CH2), V(CF2), (CH2)V, (CF2)V, V(CRR'), V(CHR) or V where R and R' are each C1-4 alkyl and in which V is a hydrocarbyl group containing 0, 1 or 2 carbon atoms, carbonyl, dicarbonyl, CH(OH), CH(CN), sulphonamide, amide, O, S(O)m or NR where R is hydrogen or R is C1-4 alkyl; and R is an optionally substituted C3-6 cycloalkyl or an optionally substituted 5, 6, 7, 8, 9 or 10-membered carbocyclic or heterocyclic moiety; or R is a group ZR in which Z is NR , and NR and R together form an optionally substituted 5, 6, 7, 8, 9 or 10-membered carbocyclic or heterocyclic moiety, are protein tyrosine kinase inhibitors. The compounds are described, as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of psoriasis, fibrosis, atherosclerosis, restenosis, auto-immune disease, allergy, asthma, transplantation rejection, inflammation, thrombosis, nervous system diseases, and cancer.
摘要翻译：取代的式（A）的杂芳族化合物，其中X是N或CH; 其中（a）表示稠合的5,6或7元杂环，R 3是基团ZR 4，其中Z通过（CH 2）p基团与R 4连接，其中p为0 ，1或2，Z表示V（CH2），V（CF2），（CH2）V，（CF2）V，V（CRR'），V（CHR）或V，其中R和R' -4-烷基，其中V是含有0,1或2个碳原子的烃基，羰基，二羰基，CH（OH），CH（CN），磺酰胺，酰胺，O，S（O）其中R b是氢或R b是C 1-4烷基; 和R 4是任选取代的C 3-6环烷基或任选取代的5,6,7,8,9或10元碳环或杂环部分; 或R 3是Z Z 4，其中Z是NR b，NR b和R 4一起形成任选取代的5,6,7,8,9或10元碳环或杂环部分是蛋白质酪氨酸激酶抑制剂。描述了这些化合物，以及其制备方法，包括这些化合物的药物组合物及其在医学中的用途，例如治疗牛皮癣，纤维化，动脉粥样硬化，再狭窄，自身免疫疾病，过敏，哮喘，移植排斥，炎症，血栓形成，神经系统疾病和癌症。

3. 发明申请

WO2006079833A1 QUINAZOLINE DERIVATIVES AS ANTIVIRAL AGENTS 审中-公开
标题翻译：喹诺酮衍生物作为抗病毒剂
公开(公告)号：WO2006079833A1
公开(公告)日：2006-08-03
申请号：PCT/GB2006/000294
申请日：2006-01-30
申请人： ARROW THERAPEUTICS LIMITED , COCKERILL, George, Stuart , FLACK, Stephen, Sean , MATHEWS, Neil , SALTER, James, Iain
发明人： COCKERILL, George, Stuart , FLACK, Stephen, Sean , MATHEWS, Neil , SALTER, James, Iain
IPC分类号： C07C255/61 , C07D239/94 , C07D403/14 , A61P31/14 , A61K31/5377 , A61K31/517
CPC分类号： C07C255/61 , C07D239/94
摘要： Compounds of formula (I) are found to be active in inhibiting replication of flaviviridae Formula (I) wherein: X represents a direct bond or a moiety -L-NR-, wherein R is hydrogen or C 1 -C 4 alkyl, and L represents a C 1 -C 4 alkylene, C 6 -C 10 aryl or 5- to 10- membered heteroaryl moiety; either R 1 and R 2 , together with the N atom to which they are attached, form a 5- to 10- membered heterocyclyl group or a 5- to 10- membered heteroaryl group, or R 1 represents hydrogen, C 6 -C 10 aryl, C 1 -C 4 alkyl or C 1 -C 4 hydroxyalkyl and R 2 represents C 6 -C 10 aryl, C 1 -C 4 alkyl or C 1 -C 4 hydroxyalkyl; and R 3 represents a C 6 -C 10 aryl, C 3 -C 6 carbocyclyl, 5- to 10- membered heteroaryl or 5- to 10- membered heterocyclyl moiety, said aryl, carbocyclyl, heteroaryl and heterocyclyl groups being unsubstituted or substituted by 1, 2 or 3 substituents selected from halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, hydroxy, thiol, -NH 2 , C 1 -C 4 hydroxyalkyl, C 1 -C 4 thioalkyl and C 1 -C 4 aminoalkyl substituents.
摘要翻译：发现式（I）化合物在抑制黄病毒科（I）的复制中具有活性，其中：X表示直接键或部分-L-NR-，其中R为氢或C 1〜 -C 4烷基，L表示C 1 -C 4亚烷基，C 6 -C 3亚烷基 > 10个芳基或5-至10-元杂芳基部分; R 1和R 2 2与它们所连接的N原子一起形成5-至10-元杂环基或5-至10-元杂芳基或R 1代表氢，C 6 -C 10芳基，C 1 -C 3 > 4个C 1 -C 4烷基或C 1 -C 4羟基烷基，R 2表示C 6 -C C 1 -C 10芳基，C 1 -C 4烷基或C 1 -C 4烷基或C 1 -C 4 - 羟; 和R 3表示C 6 -C 10芳基，C 3 -C 6 - 所述芳基，碳环基，杂芳基和杂环基是未被取代的或被1,2或3个选自卤素，C 1 -C 6烷基的取代基取代的杂芳基或5-至10-元杂环基部分 C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 3亚烷基，C 1 -C 4烷基，C 1 -C 4烷基，C 1 -C 4烷基，卤代烷基，C 1 -C 4卤代烷氧基，羟基，硫醇，-NH 2，C 1， C 1 -C 4 - 羟基烷基，C 1 -C 4硫代烷基和C 1 -C 3 - 4个氨基烷基取代基。

4. 发明申请

WO2003033482A1 OXADIAZOLYL-BIPHENYLCARBOXAMIDES AND THEIR USE AS P38 KINASE INHIBITORS 审中-公开
标题翻译：氧化二苯乙烯消化酶及其作为P38激酶抑制剂的用途
公开(公告)号：WO2003033482A1
公开(公告)日：2003-04-24
申请号：PCT/EP2002/011574
申请日：2002-10-16
申请人： GLAXO GROUP LIMITED , ANGELL, Richard, Martyn , BAMBOROUGH, Paul , COCKERILL, George, Stuart , SMITH, Kathryn, Jane , WALKER, Ann, Louise
发明人： ANGELL, Richard, Martyn , BAMBOROUGH, Paul , COCKERILL, George, Stuart , SMITH, Kathryn, Jane , WALKER, Ann, Louise
IPC分类号： C07D271/10
CPC分类号： C07D271/10 , C07D231/12 , C07D233/56 , C07D249/08 , C07D413/12 , C07D417/12
摘要： Compounds of formula (I), wherein R 3 is the group; or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
摘要翻译：式（I）化合物，其中R 3是基团; 或其药学上可接受的盐或溶剂化物，以及它们作为药物的用途，特别是作为p38激酶抑制剂。

5. 发明申请

WO2003033457A1 BIPHENYL-DERIVATIVES AS P38-KINASE INHIBITORS 审中-公开
标题翻译：作为P38-激酶抑制剂的联苯衍生物
公开(公告)号：WO2003033457A1
公开(公告)日：2003-04-24
申请号：PCT/EP2002/011571
申请日：2002-10-16
申请人： GLAXO GROUP LIMITED , ANGELL, Richard, Martyn , ASTON, Nicola, Mary , BAMBOROUGH, Paul , BAMFORD, Mark, James , COCKERILL, George, Stuart , FLACK, Stephen, Sean , LAINE, Dramane, Ibrahim , WALKER, Ann, Louise
发明人： ANGELL, Richard, Martyn , ASTON, Nicola, Mary , BAMBOROUGH, Paul , BAMFORD, Mark, James , COCKERILL, George, Stuart , FLACK, Stephen, Sean , LAINE, Dramane, Ibrahim , WALKER, Ann, Louise
IPC分类号： C07C233/01
CPC分类号： C07D213/81 , C07D261/18 , C07D307/68 , C07D333/38 , C07D401/12
摘要： Compounds of formula (I), or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
摘要翻译：式（I）化合物或其药学上可接受的盐或溶剂化物，及其作为药物的用途，特别是作为p38激酶抑制剂。

6. 发明申请

WO2003032972A1 5’-CARBAMOYL-1,1-BIPHENYL-4-CARBOXAMIDE DERIVATIVES AND THEIR USE AS P38 KINASE INHIBITORS 审中-公开
标题翻译： 5'-CARBAMOYL-1,1-BIPHENYL-4-CARBOXAMIDE DERIVATIVES AND THE E Use as P38 KINASE INHIBITORS
公开(公告)号：WO2003032972A1
公开(公告)日：2003-04-24
申请号：PCT/EP2002/011577
申请日：2002-10-16
申请人： GLAXO GROUP LIMITED , ANGELL, Richard, Martyn , ASTON, Nicola, Mary , BAMBOROUGH, Paul , BAMFORD, Mark, James , COCKERILL, George, Stuart , MERRICK, Suzanne, Joy , SMITH, Kathryn, Jane , WALKER, Ann, Louise
发明人： ANGELL, Richard, Martyn , ASTON, Nicola, Mary , BAMBOROUGH, Paul , BAMFORD, Mark, James , COCKERILL, George, Stuart , MERRICK, Suzanne, Joy , SMITH, Kathryn, Jane , WALKER, Ann, Louise
IPC分类号： A61K31/166
CPC分类号： C07D213/40 , C07C233/65 , C07C233/69 , C07C233/78 , C07C237/22 , C07C237/42 , C07C311/05 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D215/12 , C07D231/40 , C07D277/46 , C07D285/135 , C07D417/04
摘要： Compounds of formula (I): wherein when m is 0 to 4 R 1 is selected from C 1-6 alkyl, C 3-7 cycloalkyl, C 2-6 alkenyl, -SO 2 NR 4 R 5 , -CONR 4 R 5 and -COOR 4 ; and when m is 2 to 4 R 1 is additionally selected from C 1-6 alkoxy, hydroxy, NR 4 R 5 , -NR 4 SO 2 R 5 , -NR 4 SOR 5 , -NR 4 COR 5 , and -NR 4 CONR 4 R 5 ; R 2 is selected from hydrogen, C 1-6 alkyl and -(CH 2 ) n -C 3-7 cycloalkyl; R 3 is the group -CO-NH-(CH 2 ) p -R 6 ; U is selected from methyl and halogen; W is selected from methyl and chlorine; V and Y are each selected independently from hydrogen, methyl and halogen; m is selected from 0, 1, 2, 3 and 4 wherein each carbon atom of the resulting carbon chain may be optionally substituted with one or two groups selected independently from C 1-6 alkyl; n is selected from 0, 1, 2 and 3; p and r are independently selected from 0, 1 and 2; s is selected from 0, 1 and 2; or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
摘要翻译：式（I）化合物：其中当m为0至4时，R 1为选自C 1-6烷基，C 3-7 - 环烷基，C 2-6烯基，-SO 3 S 2，NR 4，R 5，-CONR 4， R 5 和-COOR 4 ; 当m为2至4时，另外选自C 1-6烷氧基，羟基，NR 4 R 5， / sp>，-NR 4 S S S S sp 3，-NR 4，R 5，R 6，R 6，R 6， SP>; R 6选自氢，C 1-6烷基和 - （CH 2）n - （CH 3）n - sb> 3-7环烷基; R 3是基团-CO-NH-（CH 2）2，其中R 1和R 2分别是-CO-NH-（CH 2）2。 U选自甲基和卤素; W选自甲基和氯; V和Y各自独立地选自氢，甲基和卤素; m选自0,1,2,3和4，其中所得碳链的每个碳原子可以任选被一个或两个独立地选自C 1-6烷基的基团取代; n选自0,1,2和3; p和r独立地选自0,1和2; s选自0,1和2; 或其药学上可接受的盐或溶剂合物，以及它们作为药物的用途，特别是作为p38激酶抑制剂。

7. 发明申请

WO2003032980A1 5'-CARBAMOYL-1,1'-BIPHENYL-4-CARBOXAMIDE DERIVATIVES AND THEIR USE AS P38 KINASE INHIBITORS 审中-公开
标题翻译： 5'-CARBAMOYL-1,1'-联苯-4-羧酰胺衍生物及其作为P38激酶抑制剂的用途
公开(公告)号：WO2003032980A1
公开(公告)日：2003-04-24
申请号：PCT/EP2002/011573
申请日：2002-10-16
申请人： GLAXO GROUP LIMITED , ANGELL, Richard, Martyn , ASTON, Nicola, Mary , BAMBOROUGH, Paul , BAMFORD, Mark, James , COCKERILL, George, Stuart , MERRICK, Suzanne, Joy , WALKER, Ann, Louise
发明人： ANGELL, Richard, Martyn , ASTON, Nicola, Mary , BAMBOROUGH, Paul , BAMFORD, Mark, James , COCKERILL, George, Stuart , MERRICK, Suzanne, Joy , WALKER, Ann, Louise
IPC分类号： A61K31/40
CPC分类号： C07D295/182 , C07D211/26 , C07D231/12 , C07D233/56 , C07D249/08 , C07D277/28 , C07D295/13 , C07D295/135 , C07D307/14 , C07D307/52
摘要： Compounds of formula (I): wherein X is a bond or a phenyl group which may be optionally substituted; R 1 is selected from an optionally substituted five- to seven-membered heterocyclic ring, an optionally substituted five- to seven-membered heteroaryl ring and an optionally substituted fused bicyclic ring; R 2 is selected from hydrogen, C 1-6 alkyl and -(CH 2 ) p -C 3-7 cycloalkyl; or when X is a bond and m and n are both zero R 1 and R 2 , together with the nitrogen atom to which they are bound, form a five- to six-membered heterocyclic ring optionally containing one additional heteroatom selected from oxygen and nitrogen, which can be optionally substituted by C 1-4 alkyl; R 3 is the group -CO-NH-(CH 2 ) q -R 4 ; U is selected from methyl and halogen; W is selected from methyl and chlorine; V and Y are each selected independently from hydrogen, methyl and halogen; Z is selected from -O- and a bond; m and n are independently selected from 0, 1 and 2, wherein each carbon atom of the resulting carbon chain may be optionally substituted with up to two groups selected independently from C 1-6 alkyl, and the sum of m+ n is from 0 to 4; p is selected from 0 and 1; q and s are selected from 0, 1 and 2; r is selected from 0, 1 and 2; or pharmaceutically acceptable salts or solvated thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
摘要翻译：式（I）的化合物：其中X是可以任意取代的键或苯基; R 6选自任选取代的五至七元杂环，任选取代的五元至七元杂芳基环和任选取代的稠合双环; R 2选自氢，C 1 -C 6烷基和 - （CH 2 b）2 s C 3 -C 7 - 环烷基; 或者当X是键并且m和n均为0时，与其结合的氮原子一起形成5至6个碳原子任选地含有一个选自氧和氮的另外的杂原子，其可以任选被C 1-4烷基取代; R 3是基团-CO-NH-（CH 2）2，其中R 1和R 2各自独立地为氢。 U选自甲基和卤素; W选自甲基和氯; V和Y各自独立地选自氢，甲基和卤素; Z选自-O-和键; m和n独立地选自0,1和2，其中所得碳链的每个碳原子可以任选被至多两个独立地选自C 1-6烷基的基团取代，并且总和 m + n为0〜4; p选自0和1; q和s选自0,1和2; r选自0,1和2; 或其药学上可接受的盐或溶剂合物，以及它们作为药物的用途，特别是作为p38激酶抑制剂。

8. 发明申请

WO1997003069A1 HETEROCYCLIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：杂环化合物和含有它们的药物组合物
公开(公告)号：WO1997003069A1
公开(公告)日：1997-01-30
申请号：PCT/EP1996003026
申请日：1996-07-11
申请人： GLAXO GROUP LIMITED , COCKERILL, George, Stuart , CARTER, Malcolm, Clive , McKEOWN, Stephen, Karl , VILE, Sadie , PAGE, Martin, John , HUDSON, Alan, Thomas , BARRACLOUGH, Paul , FRANZMANN, Karl, Witold
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D403/12
CPC分类号： C07D401/14 , C07D403/12 , C07D405/14 , C07D491/04
摘要： The invention is directed toward substituted heteroaromatic compounds which are protein tyrosine kinase inhibitors, in particular to substituted quinolines and quinazolines. Methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of psoriasis, fibrosis, atherosclerosis, restenosis, auto-immune disease, allergy, asthma, transplantation rejection, inflammation, thrombosis, nervous system diseases, and cancer.
摘要翻译：本发明涉及取代的杂芳族化合物，其是蛋白质酪氨酸激酶抑制剂，特别是取代的喹啉和喹唑啉。其制备方法，包括这些化合物的药物组合物及其在医学中的应用，例如治疗牛皮癣，纤维化，动脉粥样硬化，再狭窄，自身免疫疾病，过敏，哮喘，移植排斥，炎症，血栓形成，神经系统疾病，和癌症。

9. 发明申请

WO1996004906A1 COMPOUNDS FOR THE TREATMENT OF RESTENOSIS 审中-公开
标题翻译：用于治疗抑郁症的化合物
公开(公告)号：WO1996004906A1
公开(公告)日：1996-02-22
申请号：PCT/GB1995001899
申请日：1995-08-11
申请人： THE WELLCOME FOUNDATION LIMITED , BONSER, Robert, William , SLATER, Martin, John , COCKERILL, George, Stuart
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： A61K31/40
CPC分类号： C07D487/14 , A61K31/407 , A61K31/437
摘要： The present invention is concerned with compounds of formula (I) having use in the prophylaxis or treatment of restenosis. In particular, the invention relates to the use of these compounds in the manufacture of medicaments for the prophylaxis or treatment of restenosis, to medicaments obtained thereby, and to a method for treatment to prevent or alleviate restenosis using the compounds of the invention or a medicament containing said compounds.
摘要翻译：本发明涉及用于预防或治疗再狭窄的式（I）化合物。特别地，本发明涉及这些化合物在制备用于预防或治疗再狭窄的药物中的用途，以及由此获得的药物的用途以及使用本发明的化合物或药物来预防或减轻再狭窄的治疗方法含有所述化合物。

10. 发明申请

WO1991016301A1 PESTICIDES 审中-公开
标题翻译：农药
公开(公告)号：WO1991016301A1
公开(公告)日：1991-10-31
申请号：PCT/GB1991000539
申请日：1991-04-08
申请人： THE WELLCOME FOUNDATION LIMITED , BLADE, Robert, John , COCKERILL, George, Stuart
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： C07C313/28
CPC分类号： A01N49/00 , C07C233/91 , C07C313/28 , C07C2601/02 , C07D213/71
摘要： The present application discloses pesticidally active compounds of the formula (I): QQ CR = CR CR = CR C(=X )NR R , or a salt thereof, wherein Q is a monocyclic aromatic ring, or fused bicyclic ring system of which at least one ring is aromatic containing 9 or 10 atoms of which one may be nitrogen and the rest carbon each ring system being optionally substituted, or Q is a dihalovinyl group or a group R -C=C- where R is C1-4 alkyl, tri C1-4 alkylsilyl, halogen or hydrogen; Q is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C1-3 alkyl, halo, C1-3 haloalkyl, alkynyl, or cyano; R , R , R and R are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C1-4 alkyl or C1-4 haloalkyl; X is oxygen or sulphur; R is C1-8 hydrocarbyl optionally substituted by dioxalanyl, halo, cyano, trifluoromethyl, trifluoromethylthio or C1-6 alkoxy; and R is selected from: (A) -Y=X -(R )a where X is O or S, Y is phosphorus or carbon, R is hydrogen, C1-4 alkyl, C1-4 alkoxy, C1-5 alkylcarbonyl or aryl or CO2R where R is a C1-4 alkyl or aryl, and a is 1 or 2, (B) -S(O)bR , where R is a C1-4 alkyl, aryl, aryloxy or C1-4 alkoxy, wherein the aryl ring may be substituted by one or more halo, nitro, cyano, C1-4 alkyl, C1-4 alkoxy groups each in turn optionally substituted by one or more halogens, or R is a group NR R wherein R is -COR where R is hydrogen, fluorine or C1-4 alkyl or R is a group CO.CO2R , SNR R or P(->O)R wherein 11 and 11 are the same or different and each is a group R and R , R and R as hereinbefore defined, or R is C1-4 alkyl substituted by C1-4 alkyl, C1-5 alkylcarbonyl or aryl, carboalkoxy or cyano, or R is a group CO2R where R is C1-4 alkyl or aryl, R is C1-4 alkyl, and b=0, 1 or 2; (C) -CR R X R where R and R are hydrogen or C1-4 alkyl, X is oxygen or sulphur and R is C1-4 alkyl, C1-5 alkylcarbonyl or aralkylcarbonyl R , R X may be linked to form a ring system; (D) -CR R X is a 5 or 6 membered heterocyclic ring containing an oxygen or sulphur atom optionally substituted by C1-4 alkyl, their preparation, pesticidal compositions containing them and their use against pests.
摘要翻译：本申请公开了式（I）的杀虫活性化合物：QQ <1> CR 1 = CR 2 CR 3 = CR 4 C（= X 1）NR 5 R 6>或其盐，其中Q是单环芳环，或稠合双环体系，其中至少一个芳环含有9或10个原子，其中一个可以是氮，其余的碳每个环系被任选取代或Q是二卤代乙烯基或基团R 7-C≡C，其中R 7是C 1-4烷基，三C 1-4烷基甲硅烷基，卤素或氢; Q 1是任选被一个或多个选自C 1-3烷基，卤素，C 1-3卤代烷基，炔基或氰基的基团取代的1,2-环丙基环; R 1，R 2，R 3和R 4相同或不同，至少一个为氢，其余独立地选自氢，卤素，C 1-4烷基或C 1-4卤代烷基 ; X 1是氧或硫; 卤代，氰基，三氟甲基，三氟甲硫基或C 1-6烷氧基取代的C 1-8烃基; 并且R 6选自：（A）-Y = X 2 - （R 8）a，其中X 2为O或S，Y为磷或碳，R 8为氢， C 1-4烷基，C 1-4烷氧基，C 1-5烷基羰基或芳基或CO 2 R 9，其中R 9是C 1-4烷基或芳基，a是1或2，（B）-S（O） b R 10，其中R 10是C 1-4烷基，芳基，芳氧基或C 1-4烷氧基，其中芳环可以被一个或多个卤素，硝基，氰基，C 1-4烷基， 4个烷氧基各自依次被一个或多个卤素取代，或R 10是NR 11基团，其中R 11是-COR 13，其中R 13是氢，氟或C 1-4烷基或R 13是CO CO 2 R 9，SNR 11a，R 11b或P - > O 8 R 8，其中11和11b是相同或不同，并且各自为如上文所定义的基团R 11和R 3，R 9和R 11，或R 11为被C 1-4烷基取代的C 1-4烷基，C 1 烷基羰基或芳基，烷氧羰基或氰基，或R 11是CO 2 R 14基团，其中R 14是C 1-4烷基或芳基，R 12是C 1-4烷基，b = 0， 1或2; （C）-CR 15 R 16 X 3 R 17其中R 15和R 16为氢或C 1-4烷基，X 3为氧或硫，R 17为 >为C 1-4烷基，C 1-5烷基羰基或芳烷基羰基R 17，R 15 X 3可以连接形成环系; （D）-CR 15 R 16 X 3是含有任选被C 1-4烷基取代的氧或硫原子的5或6元杂环，它们的制备方法，含有它们的杀虫组合物及其对害虫的用途。

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