公开(公告)号：US4772624A

公开(公告)日：1988-09-20

申请号：US779167

申请日：1985-09-23

申请人： Christopher J. Palmer ,  John E. Casida

发明人： Christopher J. Palmer ,  John E. Casida

IPC分类号： A01N43/90 ,  A01N55/00 ,  C07D493/08 ,  C07D497/08 ,  C07F7/08 ,  A01N43/32 ,  C07D323/04

CPC分类号： C07D493/08 ,  A01N43/90 ,  A01N55/00 ,  C07D497/08 ,  C07F7/0812 ,  C09K2019/3425

摘要： A compound of the formula ##STR1## wherein R is C.sub.3 -C.sub.10 normal- or branched- alkyl or cycloalkyl, C.sub.3 -C.sub.10 normal- or branched- alkyl or cycloalkyl having one or more halogen, cyano, C.sub.1 -C.sub.2 partially or completely halogenated alkyl, or C.sub.1 -C.sub.3 alkoxy or partially or completely halogenated alkoxy substituents, C.sub.3 -C.sub.10 cycloalkyl having C.sub.1 -C.sub.2 alkyl substituents, phenyl, or phenyl having one or more halogen, cyano, nitro, ethynl, C.sub.1 -C.sub.2 alkyl or partially or completely halogenated alkyl, or C.sub.1 -C.sub.3 alkoxy or partially or completely halogenated alkoxy substituents; wherein at least one of R.sub.2 -R.sub.6 is ethynyl; and wherein the remainder of R.sub.2 -R.sub.6 are independently either hydrogen, halogen, C.sub.1 -C.sub.2 alkyl, partially or completely halogenated C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.3 alkoxy, partially or completely halogenated C.sub.1 -C.sub.3 alkoxy, ethynyl, nitro, cyano, or azido. Such a compound is useful in killing pests, particularly insects.

摘要翻译： 其中R是具有一个或多个卤素，氰基，C 1 -C 2部分或完全卤代烷基的C 3 -C 10正或支链烷基或环烷基，C 3 -C 10正链或支链烷基或环烷基的化合物 ，或C 1 -C 3烷氧基或部分或完全卤化的烷氧基取代基，具有C 1 -C 2烷基取代基的C 3 -C 10环烷基，苯基或具有一个或多个卤素，氰基，硝基，乙炔基，C 1 -C 2烷基或部分或完全卤化的苯基 烷基或C 1 -C 3烷氧基或部分或完全卤化的烷氧基取代基; 其中R 2 -R 6中的至少一个是乙炔基; 部分或完全卤化的C 1 -C 2烷基，C 1 -C 3烷氧基，部分或完全卤化的C 1 -C 3烷氧基，乙炔基，硝基，氰基或 叠氮 这种化合物可用于杀死害虫，特别是昆虫。

公开(公告)号：US4876274A

公开(公告)日：1989-10-24

申请号：US902083

申请日：1986-08-27

申请人： Christopher J. Palmer ,  John E. Casida

发明人： Christopher J. Palmer ,  John E. Casida

IPC分类号： A01N43/90 ,  C07D493/08

CPC分类号： C07D493/08 ,  A01N43/90

摘要： A pesticidal composition comprising a compound having the formula R--C(CH.sub.2 O).sub.3 C--X wherein R and X are each organic substituents and wherein the compound has an LD.sub.50, in micrograms of compound per gram of body weight of a selected pest, of less than about 400 and/or an LD.sub.50 in the presence of synergist of less than about 20 is disclosed along with its use in killing pests. Pesticidal activity has been found against a broad range of types of insects. The pesticidal activity of the composition is strongly enhanced by the use of a selected synergist.

摘要翻译： 一种农药组合物，其包含具有式RC（CH 2 O）3 C-X的化合物，其中R和X各自是有机取代基，并且其中所述化合物具有LD50，以每克体重的所选有害生物的微克化合物的小于约 在小于约20的增效剂存在下，400和/或LD 50以及其在杀虫中的应用被公开。 针对广泛类型的昆虫已经发现杀虫活性。 组合物的杀虫活性通过使用所选择的增效剂强烈增强。

公开(公告)号：US5061726A

公开(公告)日：1991-10-29

申请号：US514011

申请日：1990-04-26

申请人： Christopher J. Palmer ,  John E. Casida ,  John P. Larkin

发明人： Christopher J. Palmer ,  John E. Casida ,  John P. Larkin

IPC分类号： A01N43/32 ,  C07D327/06

CPC分类号： C07D327/06 ,  A01N43/32

摘要： Pesticidally-active alkynylphenyl-substituted 1,3-oxathianes and related substituted compounds of the formula: ##STR1## and their use in controlling pests such as arthropods and helminths are described.

摘要翻译： 描述了农药活性炔基苯基取代的1,3-氧硫杂环己烷和下式的相关取代的化合物及其在控制害虫如节肢动物和蠕虫中的用途。

公开(公告)号：US4965257A

公开(公告)日：1990-10-23

申请号：US384067

申请日：1989-07-24

申请人： John E. Casida ,  Christopher J. Palmer ,  John P. Larkin ,  Ian H. Smith

发明人： John E. Casida ,  Christopher J. Palmer ,  John P. Larkin ,  Ian H. Smith

IPC分类号： A01N43/90 ,  A01N55/00 ,  C07D493/08 ,  C07D497/08 ,  C07F7/08

CPC分类号： C07D493/08 ,  A01N43/90 ,  A01N55/00 ,  C07D497/08 ,  C07F7/0812

摘要： Bicyclo-[2,2,1]-heptanes, bicyclo-[2,2,2]-octanes and bicyclo-[2,2,3]-nonanes, having 2 or 3 ring hetero atoms selected from O, S and N, substituted at the 1-position by a 4-alkynylphenyl group and at the 4-position and optionally at the 3 and/or 5-position are valuable pesticides, particularly insecticides and acaracides. The compounds may be prepared by reacting an alkyne with the corresponding 4-iodophenyl substituted compounds or by debromination of the corresponding 4-dibromomethylphenyl substituted compound.

摘要翻译： 具有2或3个选自O，S和N的环杂原子的双环 - [2,2,1]庚烷，双环 - [2,2,2] - 辛烷和双环 - [2,2,3] - 壬烷 在4-位被4-炔基苯基取代，在4位和任选在3位和/或5位被取代是有价值的农药，特别是杀虫剂和吖啶。 化合物可以通过使炔与相应的4-碘苯基取代的化合物反应或通过相应的4-二溴甲基苯基取代的化合物的脱溴来制备。

公开(公告)号：US4942173A

公开(公告)日：1990-07-17

申请号：US315247

申请日：1989-02-24

申请人： John E. Casida ,  Christopher J. Palmer ,  John P. Larkin ,  Ian H. Smith

发明人： John E. Casida ,  Christopher J. Palmer ,  John P. Larkin ,  Ian H. Smith

IPC分类号： A01N43/90 ,  A01N55/00 ,  C07C43/13 ,  C07D493/08 ,  C07F7/08

CPC分类号： C07D493/08 ,  A01N43/90 ,  A01N55/00 ,  C07C43/13 ,  C07F7/0812

摘要： The present invention relates to a compound of the formula (I): ##STR1## wherein R is C.sub.2-10 alkyl, alkenyl or alkynyl, each optionally substituted by or methyl substituted by cyano, C.sub.3-4 cycloalkyl, halo, C.sub.1-4 alkoxy or a group S(O)m R.sup.4 where R.sup.4 is C.sub.1-4 alkyl and m is 0, 1 or 2, or Ris C.sub.3-10 cycloalkyl, C.sub.4-10 cycloalkenyl or phenyl, each optionally substituted by C.sub.1-4 alkoxy, C.sub.1-3 alkyl, C.sub.2-4 alkynyl, halo, cyano or a group S(O)m R.sup.4 as defined hereinbefore; R.sup.1 is halo, C.sub.1-3 alkyl, C.sub.2-3 alkenyl or alkynyl each optionally substituted by halo, cyano, C.sub.1-4 alkoxy, alkyl carbalkoxy containing up to 6 carbon atoms, a group S(O)m R.sup.4 as defined hereinbefore or alkynyl substituted by tri-C.sub.1-4 alkylsilyl, or R.sup.1 is cyano, spiro-cyclopropyl, gem dimethyl, gem dicyano, gem diethynyl, oxo or methylene optionally substituted by cyano of C.sub.1-3 alkyl optionally substituted by fluorine, or R.sup.1 and R and the carbon atoms to which they are attached form a C.sub.5-7 carbocyclic ring optionally substituted by halo, C.sub.1-3 alkyl or alkoxy or C.sub.2-3 alkenyl, R.sup.2 is phenyl substituted by an C.sub.2-3 alkynyl group or by a tri-C.sub.1-4 alkylsilylalkynyl group and R.sup.3 is hydrogen, C.sub.1-3 alkyl, C.sub.2-3 alkenyl or alkynyl each optionally substituted by cyano, C.sub.1-4 alkylthio, C.sub.1-4 alkoxy or halo, or R.sup.3 is cyano or halo, its use in medicine, pharmaceutical compositions containing it and its preparation.

摘要翻译： 本发明涉及式（I）的化合物：其中R为C 2-10烷基，烯基或炔基，各自任选被被氰基取代的甲基，C 3-4的环烷基，卤素，C 1 -4-烷氧基或基团S（O）m R 4，其中R 4是C 1-4烷基，m是0,1或2，或者R 3为C 3-10环烷基，C 4-10环烯基或苯基，各自任选被C 1-4烷氧基 ，C 1-3烷基，C 2-4炔基，卤素，氰基或如上所定义的基团S（O）m R 4; R 1为卤素，C 1-3烷基，任选被卤素，氰基，C 1-4烷氧基，含有至多6个碳原子的烷基烷氧基取代的C 2-3烯基或炔基，如上所定义的基团S（O）m R 4或炔基 被三-C 1-4烷基甲硅烷基取代，或R 1是氰基，螺环丙基，二甲基，双环戊二烯，偕二乙炔基，氧代或亚甲基，任选被氰基任选被氟取代的C 1-3烷基取代，或R 1和R， 它们连接的碳原子形成任选被卤素，C 1-3烷基或烷氧基或C 2-3烯基取代的C 5-7碳环，R 2是被C 2-3炔基取代的苯基或被三-C 1-4 烷基甲硅烷基炔基和R3是氢，C1-3烷基，C2-3烯基或炔基，各自任选被氰基，C1-4烷硫基，C1-4烷氧基或卤素取代，或R3是氰基或卤素，其用于医药，药物组合物 包含它及其准备。

公开(公告)号：US4622315A

公开(公告)日：1986-11-11

申请号：US465440

申请日：1983-02-10

申请人： Prem Dureja ,  John E. Casida ,  Luis O. Ruzo

发明人： Prem Dureja ,  John E. Casida ,  Luis O. Ruzo

IPC分类号： A01N25/22 ,  A01N53/00 ,  A01N65/00

CPC分类号： A01N25/22 ,  A01N53/00 ,  Y10S514/972

摘要： A number of pyrethroid insecticides are photolabile, thus limiting their use outdoors. The non-photolabile pyrethroids often have the disadvantage of lasting too long when used outdoors. Herein, certain toxicologically acceptable compounds are designated which stabilize the normally photolabile pyrethroids and allow them to be used for an extended time period out of doors. The stabilizers have an electron deficient .pi. system and serve to decrease the rate of the photochemical decomposition of the pyrethroid at a given light level.

摘要翻译： 许多拟除虫菊酯杀虫剂是光不稳定的，因此限制了它们在户外的使用。 非光不稳定的拟除虫菊酯通常具有在室外使用时持久时间长的缺点。 在这里，指定某些毒理学上可接受的化合物，其稳定通常光不稳定的拟除虫菊酯并允许它们在门外延长的时间段内使用。 稳定剂具有电子缺乏的pI系统，用于降低拟除虫菊酯在给定光照下的光化学分解速率。

公开(公告)号：US06303638B1

公开(公告)日：2001-10-16

申请号：US09372114

申请日：1999-08-20

申请人： Bachir Latli ,  John E. Casida

发明人： Bachir Latli ,  John E. Casida

IPC分类号： C07D41706

CPC分类号： C07D401/06 ,  C07D413/06 ,  C07D417/06

摘要： Novel compounds are provided that modulate the neuronal nicotinic acetylcholine receptor (nAChR), particularly the mammalian nAChR (m-nAChR). The compounds are substituted pyridine derivatives such as analogs of 1-[(6-chloro-3-pyridinyl)methyl]-2-imidazolidine and 1-[(6-chloro-3-pyridinyl)methyl]-2-iminothiazole. Methods of using the novel m-nAChR modulators are also provided, including methods of using the compounds as m-nAChR probes and as therapeutic agents to treat mammalian individuals suffering from conditions, disorders or diseases that are responsive to administration of an m-nAChR modulator. The compounds are useful in treating (1) CNS disorders such as Alzheimer's disease, AIDS-associated dementia, Tourette's Syndrome, attention deficit disorder, and attention deficit disorder, (2) inflammation and inflammatory diseases, (3) conditions caused by or associated with smooth muscle contractions, and (4) withdrawal symptoms associated with cessation of chemical substance abuse. The compounds are also useful as non-opiate analgesics, to treat mild, moderate or severe pain. Pharmaceutical formulations containing an m-nAChR modulator of the invention are provided as well.

摘要翻译： 提供调节神经元烟碱乙酰胆碱受体（nAChR），特别是哺乳动物nAChR（m-nAChR）的新型化合物。 化合物是取代的吡啶衍生物，例如1 - [（6-氯-3-吡啶基）甲基] -2-咪唑烷和1 - [（6-氯-3-吡啶基）甲基] -2-亚氨基噻唑的类似物。 还提供了使用新的m-nAChR调节剂的方法，包括使用化合物作为m-nAChR探针和作为治疗剂治疗患有对施用m-nAChR调节物的病症，病症或疾病的哺乳动物个体的方法 。 该化合物可用于治疗（1）中枢神经系统疾病如阿尔茨海默病，艾滋病相关性痴呆，图雷特综合征，注意缺陷障碍和注意力缺陷障碍，（2）炎症和炎性疾病，（3）由或由 平滑肌收缩，和（4）与化学物质滥用停止相关的戒断症状。 这些化合物也可用作非阿片类止痛药，用于治疗轻度，中度或重度疼痛。 还提供含有本发明的m-nAChR调节剂的药物制剂。

公开(公告)号：US5204333A

公开(公告)日：1993-04-20

申请号：US839685

申请日：1992-02-24

申请人： John P. Larkin ,  John B. Weston ,  Ian H. Smith ,  Christopher J. Palmer ,  John E. Casida

发明人： John P. Larkin ,  John B. Weston ,  Ian H. Smith ,  Christopher J. Palmer ,  John E. Casida

IPC分类号： A01N43/90 ,  A01N55/00 ,  C07D493/08 ,  C07D495/08 ,  C07D497/08

CPC分类号： C07D493/08 ,  A01N43/90 ,  A01N55/00 ,  C07D495/08 ,  C07D497/08

摘要： The present invention provides compounds of the formula (I): ##STR1## wherein R is a phenyl group, substituted fluorine atoms formulations containing them and their use in controlling pest infestation.

摘要翻译： 本发明提供式（I）化合物：其中R是苯基，含有它们的取代氟原子制剂及其在防治害虫侵袭中的用途。

公开(公告)号：US5057508A

公开(公告)日：1991-10-15

申请号：US481616

申请日：1990-02-20

申请人： John E. Casida ,  Christopher J. Palmer ,  John P. Larkin ,  Ian H. Smith

发明人： John E. Casida ,  Christopher J. Palmer ,  John P. Larkin ,  Ian H. Smith

IPC分类号： A01N43/90 ,  A01N55/00 ,  C07D493/08 ,  C07D497/08 ,  C07F7/08

CPC分类号： C07D493/08 ,  A01N43/90 ,  A01N55/00 ,  C07D497/08 ,  C07F7/0812

摘要： Bicyclo-[2,2,1]-heptanes, bicyclo-[2,2,2]-octanes and bicyclo[2,2,3]-nonanes having 2 or 3 ring hetero atoms selected from O, S and N, substituted at the 1-position by a 4-alkynylphenyl group and at the 4-position and optionally at the 3 and/or 5-position are valuable pesticides, particularly insecticides and acaracides. The compounds may be prepared by reacting an alkyne with the corresponding 4-iodophenyl substituted compound or by debromination of the corresponding 4-dibromomethylphenyl substituted compound.

摘要翻译： 具有2或3个选自O，S和N的环杂原子的双环 - [2,2,1] - 庚烷，双环 - [2,2,2] - 辛烷和双环[2,2,3] - 壬烷取代 在4-位炔基苯基在1-位，在4-位和任选地在3和/或5位上是有价值的农药，特别是杀虫剂和吖啶。 化合物可以通过使炔与相应的4-碘苯基取代的化合物反应或通过相应的4-二溴甲基苯基取代的化合物的脱溴来制备。

公开(公告)号：US4985411A

公开(公告)日：1991-01-15

申请号：US442629

申请日：1989-11-29

申请人： John E. Casida ,  Michael Elliott

发明人： John E. Casida ,  Michael Elliott

IPC分类号： A01N43/32 ,  C07D339/08 ,  C07F7/08

CPC分类号： C07D339/08 ,  A01N43/32

摘要： The present invention provides compounds of the formula (I): ##STR1## wherein m and n are independently selected from 0, 1 or 2, ##STR2## R is selected from hydrogen, methyl or ethyl; R.sup.1 is selected from C.sub.1-4 hydrocarbyl substituted by one to five halo atoms, and a group --C.tbd.C--R.sup.9 wherein R.sup.9 is a group S(O).sub.w --R.sup.10 wherein R.sup.10 is trifluoromethyl, methyl or ethyl and w is 0, 1 or 2 or R.sup.9 is a C.sub.3-5 aliphatic group or an aliphatic group containing up to 5 carbon atoms atoms substituted by C.sub.1-4 alkoxy, C.sub.2-6 alkoxyalkoxy, C.sub.1-8 acyloxy, halo or hydroxy, a group COR.sup.11 wherein R.sup.11 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or a group NR.sup.12 R.sup.13 wherein R.sup.12 and R.sup.13 are independently selected from hydrogen, methyl or ethyl, or R.sup.9 is SiR.sup.14 R.sup.15 R.sup.16 wherein R.sup.14 to R.sup.16 are the same or different and each is a C.sub.1-4 aliphatic group or R.sup.14 and R.sup.15 are C.sub.1-4 aliphatic groups and R.sup.16 is a phenyl group; R.sup.2, R.sup.3, R.sup.7 and R.sup.8 are independently selected from hydrogen, methyl or halo; R.sup.4a and R.sup.4b, R.sup.6a and R.sup.6b are independently selected from hydrogen, C.sub.1-3 alkyl, C.sub.2-3 alkenyl or alkynyl each being optionally substituted by halo, cyano or C.sub.1-4 alkoxy; cyano, halo or a group COR .sup.11a wherein R.sup.11a is hydrogen, C.sub.1-4 alkoxy, C.sub.1-4 alkyl or a group NR.sup.12a R.sup.13a wherein R.sup.12a and R.sup.13a are independently selected from hydrogen, methyl or ethyl; R.sup.5a is a non-aromatic hydrocarbyl group containing up to seven carbon atoms, or phenyl each optionally substituted by cyano, halo, C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, C.sub.3-4 cycloalkyl, C.sub.1-4 alkoxy or a group S(O).sub.q R.sup.17 wherein q is 0, 1 or 2 and R.sup.17 is methyl or ethyl and R.sup.5b is hydrogen, hydroxy or C.sub.1-4 alkyl optionally substituted by alkoxy; and represents --CH--CH-- or --C.dbd.C-- which are useful pesticides, processes for their preparation, pesticidal formulations containing them and their use in the control or prevention of pest infestation.