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1. 发明授权

US4226876A Arthropodicidal imidazoline derivatives 失效
标题翻译：节肢动物咪唑啉衍生物
公开(公告)号：US4226876A
公开(公告)日：1980-10-07
申请号：US968422
申请日：1978-12-11
申请人： Frederick C. Copp , Peter T. Roberts , Alexander D. Frenkel , David Collard
发明人： Frederick C. Copp , Peter T. Roberts , Alexander D. Frenkel , David Collard
IPC分类号： A01N43/50 , A01N47/16 , A01N47/22 , A01N47/38 , A01N47/42 , C07D233/22 , C07D233/24 , A61K31/415
CPC分类号： A01N47/38 , A01N43/50 , A01N47/16 , A01N47/22 , A01N47/42 , C07D233/22 , C07D233/24
摘要： Compounds of formula (I): ##STR1## wherein Ar is an unsubstituted or mono-, di or tri-substituted phenyl radical in which the substituents are the same or different and are selected from alkyl, alkoxy, halogen, hydroxy, cyano, amino, trifluoromethyl or nitro and in which any two adjacent carbon atoms on the phenyl ring may optionally be joined by a carbon chain having 3 or 4 carbon atoms;X.sup.1 is O or NH;R.sup.1 and R.sup.2 are the same or different and are hydrogen or alkyl; andZ is a group SO.sub.n R.sup.8 or a group ##STR2## in which X.sup.2 is O, S or NR.sup.4 ; R.sup.3 is alkyl, aryl, alkyloxy, aryloxy or NR.sup.5 R.sup.6 ;R.sup.4 is alkyl, aryl, alkyloxy, aryloxy, alkylthio, arylthio or NR.sup.5 R.sup.6 ;R.sup.5 and R.sup.6 are the same or different and are hydrogen, alkyl, aryl, COR.sup.7 or SO.sub.2 R.sup.7 ;R.sup.7 is alkyl, aryl, alkoxy or aryloxy;n is 1 or 2;R.sup.8 is alkyl, aryl or NR.sup.9 R.sup.10 ; andR.sup.9 and R.sup.10 are the same or different and are hydrogen, alkyl or aryl,provided that when Ar is unsubstituted phenyl, X.sup.1 is NH, R.sup.1 and R.sup.2 are H, Z is ##STR3## and X.sup.2 is 0, R.sup.3 is not methyl, methods of making such compounds, pesticidal formulations containing them and their use as pesticides are disclosed.
摘要翻译：式（I）的化合物：其中Ar是未取代的或单，二或三取代的苯基，其中取代基相同或不同，并且选自烷基，烷氧基，卤素，羟基，氰基，氨基，三氟甲基或硝基，并且其中苯环上任何两个相邻的碳原子可任选地被具有3或4个碳原子的碳链连接; X1是O或NH; R1和R2相同或不同，为氢或烷基; Z为X，O，S或NR4的基团SOnR8或基团; R3是烷基，芳基，烷氧基，芳氧基或NR5R6; R4是烷基，芳基，烷氧基，芳氧基，烷硫基，芳硫基或NR5R6; R5和R6相同或不同，为氢，烷基，芳基，COR7或SO2R7; R7是烷基，芳基，烷氧基或芳氧基; n为1或2; R8是烷基，芳基或NR9R10; 并且R 9和R 10相同或不同，为氢，烷基或芳基，条件是当Ar为未取代的苯基时，X 1为NH，R 1和R 2为H，Z为X，X 2为0，R 3不为甲基，公开了制备这些化合物的方法，含有它们的杀虫剂及其作为杀虫剂的用途。

2. 发明授权

US4414223A Pesticidal anilinomethylimidazolines 失效
标题翻译：杀虫剂苯胺基甲基咪唑
公开(公告)号：US4414223A
公开(公告)日：1983-11-08
申请号：US264305
申请日：1981-05-18
申请人： Frederick C. Copp , Peter T. Roberts , Alexander D. Frenkel , David Collard
发明人： Frederick C. Copp , Peter T. Roberts , Alexander D. Frenkel , David Collard
IPC分类号： A01N43/50 , A01N47/16 , A01N47/22 , A01N47/38 , A01N47/42 , C07D233/22 , C07D233/24
CPC分类号： C07D233/22 , A01N43/50 , A01N47/16 , A01N47/22 , A01N47/38 , A01N47/42 , C07D233/24
摘要： 1-Phenoxyalkyl- and 1-anilinoalkyl imidazolines, methods for the preparation thereof, the use thereof as intermediates and pesticides and pesticidal formulations containing such compounds.
摘要翻译： 1-苯氧基烷基和1-苯胺基烷基咪唑啉，其制备方法，其作为中间体的用途和农药以及含有这些化合物的杀虫剂。

3. 发明授权

US4320142A N-[(phenyl(oxy or amino))thioacetyl]-1,2-diamine anthropodicides 失效
标题翻译： N - [（苯基（氧基或氨基））硫代乙酰] -1,2-二胺杀虫剂
公开(公告)号：US4320142A
公开(公告)日：1982-03-16
申请号：US150065
申请日：1980-05-15
申请人： Malcolm H. Black , Alexander D. Frenkel , Peter T. Roberts
发明人： Malcolm H. Black , Alexander D. Frenkel , Peter T. Roberts
IPC分类号： A01N39/02 , A01N39/04 , A01N47/12 , A01N47/28 , A01N47/30 , C07C327/40 , C07C157/09 , A01N47/10 , A01N47/22 , A01N47/40 , C07C153/063 , C07C155/02
CPC分类号： A01N39/04 , A01N39/02 , A01N47/12 , A01N47/28 , A01N47/30 , C07C327/40
摘要： Compounds of formula (I) are pesticides active against arthropods. ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 are H, alkyl, alkoxy, halo, CN or CF.sub.3 or two are linked to form a 3 or 4 carbon atom group;X is O or NA where A is H or alkyl;R is H or alkyl;R.sup.4 is H or optionally substituted alkyl, aryl, aralkyl, alkenyl or alkynyl; andR.sup.5 is --CB. R.sup.6 where B is O, S or NR.sup.7 where R.sup.7 is H, alkyl, alkoxy, or optionally substituted aryl or aralkyl;R.sup.6 is H, R.sup.8, OR.sup.8, SR.sup.8 or NR.sup.9 R.sup.10 where R.sup.8 is alkyl, alkenyl or optionally substituted aryl, aralkyl or aryloxyalkyl; and R.sup.9 and R.sup.10 are H, alkyl or optionally substituted aryl or aralkyl;The invention also comprises processes for the preparation of compounds (I), formulations containing them, and their use as pesticides.
摘要翻译：式（I）化合物是对节肢动物活性的农药。（I）其中R1，R2和R3是H，烷基，烷氧基，卤素，CN或CF3或两个连接形成3或4个碳原子基团; X是O或NA，其中A是H或烷基; R是H或烷基; R 4是H或任选取代的烷基，芳基，芳烷基，烯基或炔基; R5为-CB。 R6，其中B为O，S或NR7，其中R7为H，烷基，烷氧基或任选取代的芳基或芳烷基; R6是H，R8，OR8，SR8或NR9R10，其中R8是烷基，烯基或任选取代的芳基，芳烷基或芳氧基烷基; 且R 9和R 10为H，烷基或任选取代的芳基或芳烷基; 本发明还包括制备化合物（I），含有它们的制剂及其作为农药的用途的方法。

4. 发明授权

US07776867B2 Furanopyrimidines 有权
标题翻译：呋喃并嘧啶
公开(公告)号：US07776867B2
公开(公告)日：2010-08-17
申请号：US11169312
申请日：2005-06-29
申请人： John Laird Buchanan , William H. Buckner , Simon A. Burkitt , Erin F. DiMauro , Christopher N. Farthing , Alexander D. Frenkel , Martin J. Harrison , Frank Kayser , Jinqian Liu , Sarah E. Lively , Teresa L. Marshall , David C. McGowan , Rajiv Sharma , Stephen J. Shuttleworth , Xiaotian Zhu
发明人： John Laird Buchanan , William H. Buckner , Simon A. Burkitt , Erin F. DiMauro , Christopher N. Farthing , Alexander D. Frenkel , Martin J. Harrison , Frank Kayser , Jinqian Liu , Sarah E. Lively , Teresa L. Marshall , David C. McGowan , Rajiv Sharma , Stephen J. Shuttleworth , Xiaotian Zhu
IPC分类号： C07D495/04 , C07D243/08 , C07D519/00 , A61K31/519 , A61K31/4995 , A61K31/496 , A61K31/427 , A61K31/5513 , A61K31/5377 , A61K31/538 , A61K31/541 , A61P35/00
CPC分类号： C07D491/04 , C07D495/04
摘要： The present invention relates to furanopyrimidine compounds having the general Formula I: and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula I, methods of treating various diseases and conditions in a mammal, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma and thymoma, comprising administering to the mammal a therapeutically effective amount of a compound of Formula I. The invention also relates to methods of manufacturing medicaments, which comprise one or more compounds of Formula I.
摘要翻译：本发明涉及具有通式I的呋喃并嘧啶化合物及其立体异构体，互变异构体，溶剂合物，药用盐和衍生物及其前药。本发明还包括药物组合物，其包含式I化合物，治疗哺乳动物各种疾病和病症的方法，包括炎症，抑制T细胞活化，增殖，关节炎，器官移植，缺血或再灌注损伤，心肌梗塞，中风，多发性硬化，炎性肠病，克罗恩病，狼疮，超敏反应，1型糖尿病，牛皮癣，皮炎，桥本氏甲状腺炎，干燥综合征，自身免疫性甲状腺功能亢进，艾迪生病，自身免疫性疾病，肾小球性肾炎，过敏性疾病，哮喘，干草病，湿疹，结肠癌和胸腺瘤，包括向哺乳动物施用治疗有效量的式I化合物。本发明还涉及制备药物的方法，其包含一种或多种式I化合物。

5. 发明授权

US4238497A Imidazoline derivatives, salts thereof and their use as pesticides 失效
标题翻译：咪唑啉衍生物，其盐及其作为杀虫剂的用途
公开(公告)号：US4238497A
公开(公告)日：1980-12-09
申请号：US954745
申请日：1978-10-26
申请人： Malcolm H. Black , Alexander D. Frenkel , Peter T. Roberts
发明人： Malcolm H. Black , Alexander D. Frenkel , Peter T. Roberts
IPC分类号： A01N43/50 , A01N47/16 , A01N47/22 , A01N47/38 , A01N47/44 , C07D233/06 , C07D233/20 , C07D233/24 , A61K31/45
CPC分类号： C07C255/00 , A01N43/50 , A01N47/16 , A01N47/22 , A01N47/38 , A01N47/44 , C07D233/06 , C07D233/20 , C07D233/24
摘要： Imidazoline compounds of formula (I): ##STR1## wherein Ar is selected from a phenyl or a mono-, di- or tri-substituted phenyl radical in which the substituents are selected from alkyl, alkoxy, halogen, hydroxy, cyano, amino, trihalomethyl and nitro and in which any two adjacent carbon atoms of the phenyl ring may be joined by a carbon chain containing 3 or 4 carbon atoms;X.sup.1 is S, NR.sup.3 or NZ.sup.1 ;R.sup.1 and R.sup.2 are selected from hydrogen or alkyl;R.sup.3 is alkyl or aryl;m is 0 or 1; andZ.sup.1 and Z.sup.2 are a group SO.sub.n R.sup.9 or a group ##STR2## in which X.sup.2 is O, S or NR.sup.5 ; R.sup.4 is alkyl, aryl, alkoxy, aryloxy, amino or amido;R.sup.5 is alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, amino or amido;the alkyl or alkoxy radicals containing from 1 to 4 carbon atoms each; or an acid addition salt of the imidazoline compound.Methods of preparing the compounds are provided, as are pesticidal formulations containing them.The compounds are active against pests, especially arthropods of the Order Acarina.
摘要翻译：式（I）的咪唑啉化合物：其中Ar选自苯基或单取代，二取代或三取代的苯基，其中取代基选自烷基，烷氧基，卤素，羟基，氰基，氨基，三卤甲基和硝基，其中苯环的任何两个相邻碳原子可以通过含有3或4个碳原子的碳链连接; X1为S，NR3或NZ1; R1和R2选自氢或烷基; R3是烷基或芳基; m为0或1; 并且Z 1和Z 2是其中X 2是O，S或NR 5的基团SO n R 9或基团; R4是烷基，芳基，烷氧基，芳氧基，氨基或酰氨基; R5是烷基，芳基，烷氧基，芳氧基，烷硫基，芳硫基，氨基或酰氨基; 每个含有1至4个碳原子的烷基或烷氧基; 或咪唑啉化合物的酸加成盐。提供了制备化合物的方法，含有它们的杀虫剂也是如此。这些化合物对有害生物是有效的，尤其是蜱螨目的节肢动物。

6. 发明授权

US07358250B2 Pyrrolo[2,3-d]pyrimidines that modulate ACK1 activity 失效
标题翻译：吡咯并[2,3-d]嘧啶，其调节ACK1活性
公开(公告)号：US07358250B2
公开(公告)日：2008-04-15
申请号：US11169313
申请日：2005-06-29
申请人： Christopher N. Farthing , Paul Faulder , Alexander D. Frenkel , Martin J. Harrison , Xianyun Jiao , Frank Kayser , David J. Kopecky , Jinqian Liu , Sarah E. Lively , Rajiv Sharma , Stephen J. Shuttleworth
发明人： Christopher N. Farthing , Paul Faulder , Alexander D. Frenkel , Martin J. Harrison , Xianyun Jiao , Frank Kayser , David J. Kopecky , Jinqian Liu , Sarah E. Lively , Rajiv Sharma , Stephen J. Shuttleworth
IPC分类号： C07D487/04 , C07D413/10 , A61P35/04 , C07F9/02 , A61K31/519 , A61K31/5355 , A61K31/675
CPC分类号： C07D487/04
摘要： Compounds that modulate the action of ACK1 and LCK, and related compositions methods for treating ACK1- and LCK-mediated diseases are described. In one aspect, the compounds have the general structure: where the values of the substituents are provided herein.
摘要翻译：描述了调节ACK1和LCK的作用的化合物以及用于治疗ACK1和LCK介导的疾病的相关组合物方法。在一个方面，化合物具有一般结构：其中本文提供取代基的值。

7. 发明授权

US4863966A Pesticidal amines 失效
标题翻译：杀虫胺
公开(公告)号：US4863966A
公开(公告)日：1989-09-05
申请号：US234908
申请日：1981-02-17
申请人： Malcolm H. Black , Alexander D. Frenkel , Peter T. Roberts
发明人： Malcolm H. Black , Alexander D. Frenkel , Peter T. Roberts
IPC分类号： A61K31/165 , A01N37/20 , A01N37/44 , A01N39/02 , A01N39/04 , A61K31/396 , A61K31/40 , A61P17/00 , A61P33/00 , C07C67/00 , C07C325/00 , C07C327/42 , C07D203/12 , C07D295/13
CPC分类号： C07D295/13 , A01N37/44 , A01N39/02 , A01N39/04
摘要： Compounds of formula (I) are pesticides having activity against arthropods: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are H, alkyl, alkoxy, halo, cyano or trifluoromethyl, or two of R.sup.1, R.sup.2 and R.sup.3 are linked to form a 3 or 4 carbon atom group;X is O or NA where A is H or alkyl;R is H or alkyl; andR.sup.4 and R.sup.5 are H, alkenyl or haloalkenyl or optionally substituted alkyl, aryl or aralkyl, or NR.sup.4 R.sup.5 represents a heterocyclic ring; or an acid addition salt thereof.The invention further provides methods for the preparation of the compounds, pesticidal formulations containing them, and their use in controlling arthropod pests.
摘要翻译：式（I）化合物是具有抗节肢动物活性的农药：其中R 1，R 2和R 3是H，烷基，烷氧基，卤素，氰基或三氟甲基，或者R 1，R 2和R 3中的两个连接形成3或 4个碳原子团; X是O或NA，其中A是H或烷基; R是H或烷基; 和R 4和R 5是H，烯基或卤代烯基或任选取代的烷基，芳基或芳烷基，或NR 4 R 5表示杂环; 或其酸加成盐。本发明还提供了制备化合物的方法，含有它们的杀虫剂，以及它们在控制节肢动物害虫中的用途。

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