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1. 发明授权

US06432881B1 2-benzoylcyclohexane-1,3-dione as herbicides 有权
标题翻译： 2-苯甲酰基环己烷-1,3-二酮作为除草剂
公开(公告)号：US06432881B1
公开(公告)日：2002-08-13
申请号：US09485231
申请日：2000-02-07
申请人： Stefan Engel , Joachim Rheinheimer , Ernst Baumann , Wolfgang von Deyn , Regina Luise Hill , Guido Mayer , Ulf Misslitz , Oliver Wagner , Matthias Witschel , Martina Otten , Helmut Walter , Karl-Otto Westphalen
发明人： Stefan Engel , Joachim Rheinheimer , Ernst Baumann , Wolfgang von Deyn , Regina Luise Hill , Guido Mayer , Ulf Misslitz , Oliver Wagner , Matthias Witschel , Martina Otten , Helmut Walter , Karl-Otto Westphalen
IPC分类号： C07D23112
CPC分类号： A01N43/56 , C07D207/20 , C07D303/22 , C07D305/06 , C07D307/28 , C07D333/16
摘要： 2-Benzoylcyclohexane-1,3-diones of formula I : where: R1 and R2 are each hydrogen, mercapto, nitro, halogen, cyano, thiocyanato, alkyl, haloalkyl, alkoxy, alkenyl, alkynyl, —OR3, —OCOR3, —OSO2R3, —S(O)nR3 (n=0, 1, 2), —SO2OR3, —SO2N(R3)2, —NR3SO2R3 or —NR3COR3; R3 is hydrogen or optionally substituted alkyl, haloalkyl, alkenyl, alkynyl, phenyl or phenylalkyl; Q is optionally substituted cyclohexane-2-yl-1,3-dione; X1 is optionally substituted alkylene, propenylene, alkenylene or alkynylene; R4 is hydrogen or optionally substituted alkyl, alkenyl, alkynyl, phenyl, phenylalkyl; Het is a three- to six-membered, optionally substituted heterocyclic or heteroaromatic group; and agriculturally useful salts thereof, processes and intermediates for preparing compounds of formula I, compositions comprising them, and the use of the compounds of formula I and the compositions comprising them for controlling harmful plants are described.
摘要翻译：式I的2-苯甲酰基环己烷-1,3-二酮其中：R1和R2各自为氢，巯基，硝基，卤素，氰基，氰硫基，烷基，卤代烷基，烷氧基，烯基，炔基，-OR3，-OCOR3，-OSO2R3 ，-S（O）n R 3（n = 0,1,2），-SO 2 OR 3，-SO 2 N（R 3）2，-NR 3 SO 2 R 3或-NR 3 COR 3; R 3是氢或任选取代的烷基，卤代烷基，烯基，炔基，苯基或苯基 Q是任选取代的环己烷-2-基-1,3-二酮; X 1是任选取代的亚烷基，亚丙烯基，亚烯基或亚炔基; R 4是氢或任选取代的烷基，烯基，炔基，苯基，苯基烷基; 至六元，任选取代的杂环或杂芳族基团;及其农业上有用的盐，制备式I化合物的方法和中间体，包含它们的组合物，以及式I化合物及其组合物用于控制有害植物的用途被描述。

2. 发明授权

US06770597B2 Benzohydrazide derivatives as herbicides and desiccant compositions containing them 失效
标题翻译：作为除草剂的苯甲酰肼衍生物和含有它们的干燥剂组合物
公开(公告)号：US06770597B2
公开(公告)日：2004-08-03
申请号：US10196220
申请日：2002-07-17
申请人： Masamitsu Tsukamoto , Mark Read
发明人： Masamitsu Tsukamoto , Mark Read
IPC分类号： C07D23112
CPC分类号： C07D239/54 , A01N43/54 , A01N43/56 , A01N43/58 , A01N43/60 , A01N43/653 , A01N47/24 , C07D231/14 , C07D231/18 , C07D231/20 , C07D239/56 , C07D249/12 , C07D401/12 , C07D403/12
摘要： The compound of the formula: wherein Y, X, Z, T and Q are defined in the specification,
摘要翻译：下式化合物其中Y，X，Z，T和Q在本说明书中定义，

3. 发明授权

US06239285B1 Process for making 5-lipoxygenase inhibitors having varied heterocyclic ring systems 失效
标题翻译：制备具有不同杂环体系的5-脂氧合酶抑制剂的方法
公开(公告)号：US06239285B1
公开(公告)日：2001-05-29
申请号：US09606318
申请日：2000-06-29
申请人： Timothy Norris , Megan E. Hnatow
发明人： Timothy Norris , Megan E. Hnatow
IPC分类号： C07D23112
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D309/08
摘要： A process is described for preparing a compound of Formula (1.3.0): comprising: establishing a reaction mixture consisting of in an aprotic solvent; in the presence of NaOH or KOH; optionally in the presence of a phase transfer catalyst, especially a quaternary ammonium salt or a phosphonium salt; followed by heating said reaction mixture under a nitrogen atmosphere.
摘要翻译：描述了制备式（1.3.0）化合物的方法：包括：建立由非质子溶剂组成的反应混合物; 在NaOH或KOH的存在下; 任选地在相转移催化剂，特别是季铵盐或鏻盐的存在下; 然后在氮气氛下加热所述反应混合物。

4. 发明授权

US06169086A Pyrazole derivatives 失效
标题翻译：吡唑衍生物
公开(公告)号：US06169086A
公开(公告)日：2001-01-02
申请号：US09359419
申请日：1999-07-23
申请人： Akio Ejima , Satoru Ohsuki , Hitoshi Ohki , Hiroyuki Naito
发明人： Akio Ejima , Satoru Ohsuki , Hitoshi Ohki , Hiroyuki Naito
IPC分类号： C07D23112
CPC分类号： C07D231/12 , C07D401/04 , C07D403/04 , C07D403/14 , C07D417/04 , C07D471/04 , C07D487/04
摘要： The present invention relates to cis- and trans-forms of pyrazole derivatives, salts thereof, or agents containing the same, and represented by the general formula (I): wherein G represents a nitrogen containing saturated heterocyclic structure represented by the following formula: These compounds exhibit anti-tumor activity on 5-FU-resistant tumors and effects on P glycoprotein expressing, multiple-drug resistant tumors. An example of a pyrazole derivative which demonstrates 50% inhibition of tumor cell growth is 3-[4-(3-chloro-5-fluorophenyl)-1 piperazinyl]-1-[1-(3-chloro-2-pyridyl)-5-methyl-4-pyrazolyl)-1-trans-propene hydrochloride. Synthesis of the compounds represented by formula (I) can be prepared by any one of various routes such as a Mannich reaction, a Wittig reaction, reductive amination or substitution by allylation.
摘要翻译：本发明涉及吡唑衍生物，其盐或含有该取代基的吡唑衍生物，其盐或其代表物的顺式和反式，其通式（I）表示：其中G表示由下式表示的含氮饱和杂环结构：这些化合物对5-FU抗性肿瘤表现出抗肿瘤活性，对P糖蛋白表达，多重耐药性肿瘤有影响。显示50％抑制肿瘤细胞生长的吡唑衍生物的实例是3- [4-（3-氯-5-氟苯基）-1-哌嗪基] -1- [1-（3-氯-2-吡啶基） - 5-甲基-4-吡唑基）-1-反丙烯盐酸盐。由式（I）表示的化合物的合成可以通过各种途径中的任何一种制备，例如曼尼希反应，维蒂希反应，还原胺化或烯丙基取代。

5. 发明授权

US06579988B2 Processes for the preparation of 1,5-diarylpyrazoles 失效
标题翻译：制备1,5-二芳基吡唑的方法
公开(公告)号：US06579988B2
公开(公告)日：2003-06-17
申请号：US10245949
申请日：2002-09-18
申请人： M. V. Ramana Reddy , Stanley C. Bell
发明人： M. V. Ramana Reddy , Stanley C. Bell
IPC分类号： C07D23112
CPC分类号： C07D231/12
摘要： Provided are processes for the preparation of the compound of the formula wherein R1, R3 and R4 are independently selected from the group consisting of hydrogen, halogen, hydroxyl, nitro, lower alkyl, lower alkoxy, carboxy, C1-C6 trihaloalkyl, and cyano; and R2 is amino or lower alkyl. Also provided are synthetic intermediates that are useful as intermediates in the preparation of the compound of the formula 1.
摘要翻译：提供制备式Ⅳ化合物的方法，R 3和R 4独立地选自氢，卤素，羟基，硝基，低级烷基，低级烷氧基，羧基，C 1 -C 6三卤代烷基和氰基; 并且R 2是氨基或低级烷基。还提供了合成中间体，其可用作制备式1化合物的中间体。

6. 发明授权

US06482956B2 Endothelin receptor antagonists 失效
标题翻译：内皮素受体拮抗剂
公开(公告)号：US06482956B2
公开(公告)日：2002-11-19
申请号：US10021461
申请日：2001-11-30
申请人： Juan Ignacio Luengo , John Duncan Elliott
发明人： Juan Ignacio Luengo , John Duncan Elliott
IPC分类号： C07D23112
CPC分类号： C07D231/12 , C07D405/06 , C07D405/14
摘要： Novel pyrroles, pyrazoles and triazoles, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.
摘要翻译：描述了新颖的吡咯，吡唑和三唑，含有这些化合物的药物组合物及其作为内皮素受体拮抗剂的用途。

7. 发明授权

US06353116B1 Endothelin receptor antagonists 失效
公开(公告)号：US06353116B1
公开(公告)日：2002-03-05
申请号：US09460487
申请日：1999-12-14
申请人： Juan Ignacio Luengo , John Duncan Elliott
发明人： Juan Ignacio Luengo , John Duncan Elliott
IPC分类号： C07D23112
CPC分类号： C07D231/12 , C07D405/06 , C07D405/14
摘要： Novel pyrroles, pyrazoles and triazoles, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.

8. 发明授权

US06191283B1 Pyrazole intermediates in a method of preparation of &bgr;-amino acids 有权
标题翻译：吡唑中间体在制备β-氨基酸的方法中
公开(公告)号：US06191283B1
公开(公告)日：2001-02-20
申请号：US09404114
申请日：1999-09-23
申请人： Mukund Prahalada Rao Sibi , John Joseph Shay , Craig Peter Jasperse , Mei Liu
发明人： Mukund Prahalada Rao Sibi , John Joseph Shay , Craig Peter Jasperse , Mei Liu
IPC分类号： C07D23112
CPC分类号： C07D263/52 , C07D263/12
摘要： Pyrazole intermediates in a method for the preparation of &bgr;-amino acid compounds are provided. The method includes contacting an amine nucleophile with an &agr;,&bgr;-unsaturated amide compound in the presence of a chiral Lewis acid complex. The chiral Lewis acid complex is formed from an azophilic metal salt and a chiral bisoxazolinylmethane compound. The selective amidolysis of one enantiomer of the &bgr;-aminoamide product is also described.
摘要翻译：提供吡唑中间体制备β-氨基酸化合物的方法。该方法包括在手性路易斯酸络合物的存在下使胺亲核试剂与α，β-不饱和酰胺化合物接触。手性路易斯酸络合物由偶氮金属盐和手性双恶唑啉基甲烷化合物形成。还描述了β-氨基酰胺产物的一种对映异构体的选择性酰胺解。

9. 发明授权

US06495492B1 Substituted 3-aryl-pyrazoles 失效
标题翻译：取代的3-芳基 - 吡唑
公开(公告)号：US06495492B1
公开(公告)日：2002-12-17
申请号：US09763429
申请日：2001-02-20
申请人： Otto Schallner , Karl-Heinz Linker , Joachim Kluth , Mark Wilhelm Drewes , Dieter Feucht , Rolf Pontzen , Ingo Wetcholowsky
发明人： Otto Schallner , Karl-Heinz Linker , Joachim Kluth , Mark Wilhelm Drewes , Dieter Feucht , Rolf Pontzen , Ingo Wetcholowsky
IPC分类号： C07D23112
CPC分类号： C07D231/18 , A01N43/56 , C07D231/16 , C07D231/20
摘要： The invention relates to novel substituted 3-aryl-pyrazoles of the general formula (I) in which n, Q, R1, R2, R3, R4, R5 and X are each as defined in the description, and also to processes for their preparation and to their use as herbicides.
摘要翻译：本发明涉及通式（I）的新的取代的3-芳基吡唑，其中n，Q，R 1，R 2，R 3，R 4，R 5和X各自如说明书中所定义，并且其制备方法和用作除草剂。

10. 发明授权

US06410745B1 Process for preparing 1-guanylpyrazole acid adducts 失效
标题翻译：制备1-丙酰基吡唑加成物的方法
公开(公告)号：US06410745B1
公开(公告)日：2002-06-25
申请号：US09972897
申请日：2001-10-10
申请人： Guido Fries
发明人： Guido Fries
IPC分类号： C07D23112
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： 1-Guanylpyrazole acid adducts of the formula: wherein R1, R2 and R3 independently of one another are hydrogen, a branched or straight-chain C1-6-alkyl group, a C3-8-cycloalkyl group or a C6-12-aryl group which is unsubstituted or substituted by 1 to 6 alkyl groups; R4 is hydrogen or a straight-chain or branched C1-4-alkyl group; and X is Cl or Br, are prepared by a process which comprises: conducting the reaction of pyrazole or a derivative thereof with cyanamide or a derivative thereof and gaseous hydrogen chloride or hydrogen bromide in an aprotic solvent.
摘要翻译：具有下式的1-庚烷基吡唑酸加成物：其中R 1，R 2和R 3彼此独立地是氢，支链或直链C 1-6 - 烷基，C 3-8 - 环烷基或C 6-12 - 芳基其是未取代的或被1至6个烷基取代; R 4是氢或直链或支链C 1-4 - 烷基; 和X是Cl或Br的方法通过以下方法制备，所述方法包括：在非质子溶剂中进行吡唑或其衍生物与氰酰胺或其衍生物和气态氯化氢或溴化氢的反应。

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