公开(公告)号：US06291474B1

公开(公告)日：2001-09-18

申请号：US09635879

申请日：2000-08-10

申请人： Christopher Ian Brightwell ,  Christopher Richard Ayles Godfrey ,  Christopher John Urch ,  Matthew Brian Hotson ,  Raymond Leo Sunley ,  Roger Salmon ,  Terence Lewis

发明人： Christopher Ian Brightwell ,  Christopher Richard Ayles Godfrey ,  Christopher John Urch ,  Matthew Brian Hotson ,  Raymond Leo Sunley ,  Roger Salmon ,  Terence Lewis

IPC分类号： A61K31435

CPC分类号： C07D451/02 ,  A01N43/90 ,  A01N47/16 ,  A01N47/18 ,  C07D451/04 ,  C07D451/06 ,  C07D451/14

摘要： The invention provides a compound of formula (I): wherein A is CH═CH; Ar is an optionally substituted 5-membered heterocyclic ring system containing from 1 to 3 heteroatoms individually selected from nitrogen, oxygen and sulfur atoms, and at least one unsaturation (double bond) between adjacent atoms in the ring, said heterocyclic ring being optionally fused to a benzene ring, and R′ is hydrogen, cyano, hydroxy, alkyl, alkoxy, amino, nitro, isocyanato, acylamino, hydroxyalkyl, optionally substituted heteroaryl, alkoxyalkyl, haloalkyl, halohydroxyalkyl, aralkyloxyalkyl, acyloxyalkyl, amidoximido, sulfonyloxyalkyl, aminoalkyl, alkoxycarbonylamino, acylaminoalkyl, cyanoalkyl, imino, formyl, acyl or carboxylic acid or an ester or amide thereof, or alkenyl or alkynyl either of which is optionally substituted by halogen, alkoxy, cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or cyano; or an acid addition salt, quaternary ammonium salt or N-oxide derived therefrom; an insecticidal, acaricidal or nematicidal composition comprising a compound of formula (I) and a suitable carrier or diluent therefor; a method of combating and controlling insect, acarine or nematode pests at a locus which comprises treating the pests or the locus of the pests with an effective amount of a compound of formula (I) or a composition as hereinbefore described.

摘要翻译： 本发明提供式（I）化合物：其中A为CH = CH; Ar是任选取代的5元杂环系统，其含有1-3个分别选自氮，氧和硫原子的杂原子，以及环中相邻原子之间的至少一个不饱和键（双键），所述杂环任选地与 苯环，R'是氢，氰基，羟基，烷基，烷氧基，氨基，硝基，异氰酸根合，酰氨基，羟基烷基，任选取代的杂芳基，烷氧基烷基，卤代烷基，卤代羟烷基，芳烷氧基烷基，酰氧基烷基，酰氨基亚氨基，磺酰氧基烷基，氨基烷基，烷氧基羰基氨基， 酰基氨基烷基，氰基烷基，亚氨基，甲酰基，酰基或羧酸或其酯或酰胺，或任选被卤素，烷氧基，环烷基，任选取代的芳基，任选取代的杂芳基或氰基取代的链烯基或炔基; 或由其衍生的酸加成盐，季铵盐或N-氧化物; 杀虫杀螨或杀线虫组合物，其包含式（I）化合物及其合适的载体或稀释剂; 一种防治昆虫，螨虫或线虫害虫的方法，包括用有效量的式（I）化合物或上述组合物处理害虫或害虫的场所。

公开(公告)号：US06177442B1

公开(公告)日：2001-01-23

申请号：US09357750

申请日：1999-07-21

申请人： Christopher John Urch ,  Terence Lewis ,  Raymond Leo Sunley ,  Roger Salmon ,  Christopher Richard Ayles Godfrey ,  Christopher Ian Brightwell ,  Matthew Brian Hotson

发明人： Christopher John Urch ,  Terence Lewis ,  Raymond Leo Sunley ,  Roger Salmon ,  Christopher Richard Ayles Godfrey ,  Christopher Ian Brightwell ,  Matthew Brian Hotson

IPC分类号： A61K3146

CPC分类号： C07D451/02 ,  A01N43/90 ,  A01N47/16 ,  A01N47/18 ,  C07D451/04 ,  C07D451/06 ,  C07D451/14

摘要： The invention provides a compound of formula (I): wherein A represents a bidentate group of formula —CH2—X—CH2— (wherein X is methylene, sulfur or oxygen), X′C═CY or X′WC—CYZ (wherein X′, W, Y and Z are independently hydrogen, hydroxy, acyloxy, alkoxy, alkylsilyloxy, cyano or halogen, or X′ and W or Y and Z together with the carbon to which they are attached form a carbonyl group), provided that A is not CH2—CH2; Ar is an optionally substituted phenyl or 5- or 6-membered heterocyclic ring system containing from 1 to 3 heteroatoms individually selected from nitrogen, oxygen and sulfur atoms, and at least one unsaturation (double bond) between adjacent atoms in the ring, said heterocyclic ring being optionally fused to a benzene ring; aryl, heteroaryl, aralkyl, heteroarylalkyl, alkenyl, aralkenyl, alkynyl, alkoxycarbonyl, alkanesulfonyl, arenesulfonyl, alkanyloxycarbonyl, aralkyloxycarbonyl, aryloxycarbonyl, heterocyclylalkyl, carbamyl, dithiocarboxyl moieties of R, R3 and R4 comprise from 1 to 15 carbon atoms, and are optionally substituted with one or more substituents selected from, halogen, cyano, carboxyl, carboxylic acyl, carbamyl, alkoxycarbonyl, alkoxy, alkylenedioxy, hydroxy, nitro, haloalkyl, alkyl, amino, acylamino, imidate and phosphonato groups; or an acid addition salt, quaternary ammonium salt or N-oxide derived therefrom; an insecticidal, acaricidal or nematicidal composition comprising a compound of formula (I) and a suitable carrier or diluent therefor; a method of combating and controlling insect, acarine or nematode pests at a locus which comprises treating the pests or the locus of the pests with an effective amount of a compound of formula (I) or a composition as hereinbefore described.

摘要翻译： 本发明提供式（I）化合物：其中A表示式-CH 2 -X-CH 2 - （其中X为亚甲基，硫或氧），X'C = CY或X'WC-CYZ（其中 X'，W，Y和Z独立地为氢，羟基，酰氧基，烷氧基，烷基甲硅烷氧基，氰基或卤素，或X'和W或Y和Z与它们所连接的碳一起形成羰基） A不是CH2-CH2; Ar是任选取代的苯基或5-或6-元杂环体系，其含有1-3个分别选自氮，氧和硫原子的杂原子，以及环中相邻原子之间的至少一个不饱和键（双键），所述杂环 环任选地与苯环稠合; 芳基，杂芳基，芳烷基，杂芳基烷基，烯基，芳烯基，炔基，烷氧基羰基，链烷磺酰基，芳烃磺酰基，烷氧基羰基，芳烷氧基羰基，芳氧基羰基，杂环基烷基，氨基甲酰基，R，R3和R4的二硫代羧基部分包含1至15个碳原子， 具有一个或多个选自卤素，氰基，羧基，羧基酰基，氨基甲酰基，烷氧基羰基，烷氧基，亚烷基二氧基，羟基，硝基，卤代烷基，烷基，氨基，酰氨基，亚胺基和膦酸基的取代基。 或由其衍生的酸加成盐，季铵盐或N-氧化物; 杀虫杀螨或杀线虫组合物，其包含式（I）化合物及其合适的载体或稀释剂; 一种防治昆虫，螨虫或线虫害虫的方法，包括用有效量的式（I）化合物或上述组合物处理害虫或害虫的场所。

公开(公告)号：US06174894B1

公开(公告)日：2001-01-16

申请号：US09357749

申请日：1999-07-21

申请人： Christopher John Urch ,  Terence Lewis ,  Raymond Leo Sunley ,  Roger Salmon ,  Christopher Richard Ayles Godfrey ,  Christopher Ian Brightwell

发明人： Christopher John Urch ,  Terence Lewis ,  Raymond Leo Sunley ,  Roger Salmon ,  Christopher Richard Ayles Godfrey ,  Christopher Ian Brightwell

IPC分类号： A61K31435

CPC分类号： C07D451/02 ,  A01N43/90 ,  A01N47/16 ,  A01N47/18 ,  C07D451/04 ,  C07D451/06 ,  C07D451/14

摘要： The present invention provides a compound of Formula (I): wherein Ar is optionally substituted phenyl wherein the substutuents, if present, are selected from halogen atoms, cyano, alkyl, alkenyl, alkynyl, alkoxy, haloalkyl, haloalkenyl, alkylthio and alkyl amino groups; R represents hydrogen or cyano or a group selected from alkyl, aryl, heteroaryl, aralkyl, heteroarylalkyl, alkenyl, aralkenyl, alkynyl, alkoxycarbonyl, alkanesulfonyl, arenesulfonyl, alkenyloxycarbonyl, aralkyloxycarbonyl, aryloxycarbonyl, heterocyclylalkyl, carbamyl, dithiocarboxyl or XR3 (where X represents oxygen or a group NR4); R3 and R4 are, independently, hydrogen, alkyl, aryl, heteroaryl, aralkyl, heteroarylalkyl, alkenyl, aralkenyl, alkynyl, heterocyclylalkyl, alkoxycarbonyl or carboxylic acyl each of which may be optionally substituted; R1 represents hydrogen, hydroxy, alkyl, alkoxy, amino, nitro, isocyanato, acylamino, hydroxyalkyl, optionally substituted heteroaryl, alkoxyalkyl, haloalkyl, halohydroxyalkyl, aralkyloxyalkyl, acyloxyalkyl, amidoximido, sulfonyloxyalkyl, aminoalkyl, alkoxycarbonylamino, acylaminoalkyl, cyanoalkyl, imino, formyl, acyl or carboxylic acid or an ester or amide thereof, or alkenyl or alkynyl either of which is optionally substituted; or an acid addition salt, quaternary ammonium salt or N-oxide derived therefrom; an insecticidal, acaricidal or nematicidal composition comprising a compound of formula (I) and a suitable carrier or diluent therefor; and a method of combating and controlling insect, acarine or nematode pests at a locus which comprises treating the pests or the locus of the pests with an effective amount of a compound of formula (I) or a composition as hereinbefore described.

摘要翻译： 本发明提供式（I）的化合物：其中Ar是任选取代的苯基，其中如果存在这些取代基，则选自卤素原子，氰基，烷基，烯基，炔基，烷氧基，卤代烷基，卤代烯基，烷硫基和烷基氨基 ; R表示氢或氰基或选自烷基，芳基，杂芳基，芳烷基，杂芳基烷基，烯基，芳烯基，炔基，烷氧基羰基，链烷磺酰基，芳烃磺酰基，烯氧基羰基，芳烷氧基羰基，芳氧基羰基，杂环基烷基，氨基甲酰基，二硫代羧基或XR3（其中X表示氧 或NR4组）; R 3和R 4独立地是氢，烷基，芳基，杂芳基，芳烷基，杂芳基烷基，烯基，芳烯基，炔基，杂环基烷基，烷氧基羰基或羧酰基，各自可以任选被取代; R 1表示氢，羟基，烷基，烷氧基，氨基，硝基，异氰酸酯基，酰氨基，羟基烷基，任选取代的杂芳基，烷氧基烷基，卤代烷基，卤代羟烷基，芳烷氧基烷基，酰氧基烷基，酰氨基亚氨基，磺酰氧基烷基，氨基烷基，烷氧基羰基氨基，酰氨基烷基，氰基烷基，亚氨基，甲酰基， 酰基或羧酸或其酯或酰胺，或任选被取代的链烯基或炔基; 或由其衍生的酸加成盐，季铵盐或N-氧化物; 杀虫杀螨或杀线虫组合物，其包含式（I）化合物及其合适的载体或稀释剂; 以及一种防治昆虫，螨虫或线虫害虫的场所的方法，包括用有效量的式（I）化合物或上述组合物处理害虫或害虫的场所。

公开(公告)号：US5723464A

公开(公告)日：1998-03-03

申请号：US459205

申请日：1995-06-02

申请人： Christopher Ian Brightwell ,  Michael Gerard Kelly

发明人： Christopher Ian Brightwell ,  Michael Gerard Kelly

IPC分类号： A61K31/395 ,  A61K31/495 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P43/00 ,  C07D401/12 ,  C07D401/14

CPC分类号： C07D401/12

摘要： Compounds are disclosed which have the general formula A: ##STR1## where R.sup.a and R.sup.b are each hydrogen or methyl and R.sup.c is hydrogen, halo or C.sub.1-4 alkyl optionally in the form of a pharmaceutically acceptable acid addition salt. The compounds are useful in the treatment of CNS disorders.

摘要翻译： 公开了具有通式A（A）的化合物，其中R a和R b各自为氢或甲基，R c为氢，卤素或任选以药学上可接受的酸加成盐形式的C 1-4烷基。 该化合物可用于治疗CNS疾病。

公开(公告)号：US6133449A

公开(公告)日：2000-10-17

申请号：US12066

申请日：1998-01-22

申请人： Christopher Ian Brightwell ,  Robin Gerald Shepherd

发明人： Christopher Ian Brightwell ,  Robin Gerald Shepherd

IPC分类号： C07D213/74 ,  C07D401/12 ,  C07D419/04 ,  C07D213/42

CPC分类号： C07D213/74 ,  C07D401/12 ,  C07D419/04

摘要： Compounds having the formulaR.sup.5 O--A--NR.sup.4 --R.sup.2 (V)where R.sup.2 is a heteroaryl group linked to the remainder of the molecule via a carbon atom adjacent a nitrogen atom and R.sup.4 and R.sup.5 are both hydrogen atoms or together represent --SO-- or --SO.sub.2 -- and A is C.sub.2 -C.sub.4 alkylene optionally substituted by one or more lower alkyl groups are novel intermediates in the preparation of pharmaceutically useful piperazine derivatives as end compounds. The compounds having formula V where R.sup.4 and R.sup.5 are hydrogen may be prepared by a rearrangement of a compound having the formula (VI).R.sup.2 O--A--NH.sub.2 (VI)

摘要翻译： 具有式R 5 O-A-NR 4 -R 2（V）的化合物，其中R 2是通过与氮原子相邻的碳原子连接到分子的其余部分的杂芳基，R 4和R 5都是氢原子或一起表示-SO-或 - SO 2 - 和A是任选被一个或多个低级烷基取代的C 2 -C 4亚烷基，作为制备作为末端化合物的药学上可用的哌嗪衍生物的新中间体。 具有式V的化合物，其中R 4和R 5是氢可以通过具有式（VI）的化合物的重排来制备：R 2 O-A-NH 2（VI）

公开(公告)号：US06175012B1

公开(公告)日：2001-01-16

申请号：US09010741

申请日：1998-01-22

申请人： Christopher Ian Brightwell ,  Robin Gerald Shepherd

发明人： Christopher Ian Brightwell ,  Robin Gerald Shepherd

IPC分类号： C07D40112

CPC分类号： C07D213/74 ,  C07D401/12 ,  C07D419/04

摘要： Compounds having the formula R5O—A—NR4—R2  (V) where R2 is a heteroaryl group linked to the remainder of the molecule via a carbon atom adjacent a nitrogen atom and R4 and R5 are both hydrogen atoms or together represent —SO— or —SO2— and A is C2-C4 alkylene optionally substituted by one or more lower alkyl groups are novel intermediates in the preparation of pharmaceutically useful piperazine derivatives as end compounds. The compounds having formula V where R4 and R5 are hydrogen may be prepared by a rearrangement of a compound having the formula (VI). R2O—A—NH2  (VI)

摘要翻译： 具有通式R 2的化合物是通过与氮原子相邻的碳原子与分子的其余部分连接的杂芳基，并且R 4和R 5均为氢原子或一起代表-SO-或-SO 2 - 并且A为任选的C 2 -C 4亚烷基 被一个或多个低级烷基取代是制备药学上可用的哌嗪衍生物作为末端化合物的新中间体。 具有式V的化合物，其中R 4和R 5是氢可以通过具有式（VI）的化合物的重排来制备。

公开(公告)号：US06395902B1

公开(公告)日：2002-05-28

申请号：US09614792

申请日：2000-07-12

申请人： Christopher Ian Brightwell ,  Robin Gerald Shepherd

发明人： Christopher Ian Brightwell ,  Robin Gerald Shepherd

IPC分类号： C07D41904

CPC分类号： C07D213/74 ,  C07D401/12 ,  C07D419/04

摘要： Compounds having the formula R5O—A—NR4—R2  (V) where R2 is a heteroaryl group linked to the remainder of the molecule via a carbon atom adjacent a nitrogen atom and R4 and R5 are both hydrogen atoms or together represent —SO— or —SO2— and A is C2-C4 alkylene optionally substituted by one or more lower alkyl groups are novel intermediates in the preparation of pharmaceutically useful piperazine derivatives as end compounds. The compounds having formula V where R4 and R5 are hydrogen may be prepared by a rearrangement of a compound having the formula (VI). R2O—A—NH2  (VI)

摘要翻译： 具有通式R 2的化合物是通过与氮原子相邻的碳原子与分子的其余部分连接的杂芳基，并且R 4和R 5均为氢原子或一起代表-SO-或-SO 2 - 并且A为任选的C 2 -C 4亚烷基 被一个或多个低级烷基取代是制备药学上可用的哌嗪衍生物作为末端化合物的新中间体。 具有式V的化合物，其中R 4和R 5是氢可以通过具有式（VI）的化合物的重排来制备。