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71. 发明授权

US5502027A Herbicidal glutarimides 失效
标题翻译：除草戊二酰
公开(公告)号：US5502027A
公开(公告)日：1996-03-26
申请号：US323292
申请日：1994-10-14
申请人： Barry C. Lange , John W. Ashmore , Jane Wissinger-Cornille , Colin M. Tice
发明人： Barry C. Lange , John W. Ashmore , Jane Wissinger-Cornille , Colin M. Tice
IPC分类号： A01N37/32 , A01N37/46 , A01N39/00 , A01N39/02 , A01N39/04 , A01N41/04 , A01N41/10 , A01N43/08 , A01N43/16 , A01N43/20 , A01N43/28 , A01N43/30 , A01N43/32 , A01N43/38 , A01N43/40 , A01N43/56 , A01N43/72 , A01N43/74 , A01N43/80 , A01N43/86 , A01N55/00 , C07D211/18 , C07D211/76 , C07D211/84 , C07D211/88 , C07D217/24 , C07D401/04 , C07D401/10 , C07D405/04 , C07D405/10 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07F7/08 , C07D265/36
CPC分类号： C07D401/04 , A01N37/32 , A01N37/46 , A01N39/00 , A01N39/02 , A01N39/04 , A01N41/04 , A01N41/10 , A01N43/08 , A01N43/16 , A01N43/20 , A01N43/28 , A01N43/30 , A01N43/32 , A01N43/38 , A01N43/40 , A01N43/56 , A01N43/72 , A01N43/74 , A01N43/80 , A01N43/86 , A01N55/00 , C07D211/18 , C07D211/76 , C07D211/84 , C07D211/88 , C07D217/24 , C07D401/10 , C07D405/04 , C07D405/10 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07F7/0812
摘要： This invention relates to glutarimide compounds exhibiting herbicidal activity having the structure ##STR1## wherein A is carbonyl, thiocarbonyl or methylene, Al is carbonyl or methylene, Q is O or (CH.sub.2).sub.n where n is 0 or 1, D is CH or N and R, R.sup.1, R.sup.2, T, X, Y and Z are as defined within, compositions containing these compounds and methods of using these compounds as herbicides and algicides.
摘要翻译：本发明涉及具有亚甲基结构，Al为羰基或亚甲基的除草活性的戊二酰亚胺化合物，Q为O或（CH2）n，其中n为0或1，D为CH或N，R，R1，R2，T，X ，Y和Z定义如下，含有这些化合物的组合物和使用这些化合物作为除草剂和杀藻剂的方法。

72. 发明授权

US4868181A 1,4-dihydropyridine derivatives with calcium agonist and alpha.sub.1 -antagonist activity 失效
标题翻译：具有钙激动剂和α1-拮抗剂活性的1,4-二氢吡啶衍生物
公开(公告)号：US4868181A
公开(公告)日：1989-09-19
申请号：US64361
申请日：1987-06-30
申请人： Alexander L. Johnson , Philip Ma , Petrus B. M. W. M. Timmermans , Ruth R. Wexler
发明人： Alexander L. Johnson , Philip Ma , Petrus B. M. W. M. Timmermans , Ruth R. Wexler
IPC分类号： C07D401/14 , A61K31/4422 , A61P9/04 , C07D211/84 , C07D211/90 , C07D213/63 , C07D239/26 , C07D241/04 , C07D295/033 , C07D401/04 , C07D401/12 , C07D491/04 , C07D491/048
CPC分类号： C07D401/04 , C07D211/84 , C07D211/90 , C07D401/12 , C07D491/04
摘要： 1,4-Dihydropyridine derivatives which combine both calcium agonist and alpha.sub.1 -antagonist activity are useful in treating congestive heart failure. These derivatives are compounds having the formula: ##STR1## wherein Ar, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are defined in the specification.
摘要翻译：结合钙激动剂和α1-拮抗剂活性的1,4-二氢吡啶衍生物可用于治疗充血性心力衰竭。这些衍生物是具有下式的化合物：其中Ar，R 3，R 4，R 5和R 6在本说明书中定义。

73. 发明授权

US4812572A Process for preparation of fluoroaromatic or fluoroheterocyclic compounds 失效
标题翻译：氟代芳族化合物或氟代杂环化合物的制备方法
公开(公告)号：US4812572A
公开(公告)日：1989-03-14
申请号：US77875
申请日：1987-07-27
申请人： Michael S. Howarth , David M. Tomkinson
发明人： Michael S. Howarth , David M. Tomkinson
IPC分类号： C07B31/00 , C07B39/00 , C07C17/00 , C07C17/093 , C07C17/12 , C07C25/13 , C07C25/18 , C07C51/363 , C07C67/00 , C07C201/00 , C07C201/12 , C07C205/12 , C07D213/61 , C07D213/73 , C07D211/72 , C07D211/84 , C07D211/90 , C07D213/72
CPC分类号： C07D213/61 , C07B39/00 , C07C17/093 , C07C201/12 , C07C51/363
摘要： A process for the preparation of a fluoroaromatic or fluoroheterocyclic compound, which comprises diazotizing the corresponding amino-aromatic or amino-heterocyclic compound in hydrogen fluoride and decomposing the diazonium salt in the diazotization mixture so formed, characterized in that decomposition is carried out at super atmospheric pressure.

74. 发明授权

US4791122A Circulation active novel 5-aryldihydropyridines 失效
标题翻译：循环活性新型5-芳基二氢吡啶
公开(公告)号：US4791122A
公开(公告)日：1988-12-13
申请号：US816916
申请日：1986-01-08
申请人： Jurgen Stoltefuss , Rainer Gross , Matthias Schramm , Gunter Thomas , Michael Kayser , Bernd Pelster
发明人： Jurgen Stoltefuss , Rainer Gross , Matthias Schramm , Gunter Thomas , Michael Kayser , Bernd Pelster
IPC分类号： A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/451 , A61K31/455 , A61P3/00 , A61P3/08 , A61P9/04 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P43/00 , C07D211/84 , C07D211/90 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04 , A61K31/44
CPC分类号： C07D409/04 , C07D211/84 , C07D211/90
摘要： 5-Aryl-1,4-dihydropyridines of the formula ##STR1## in which Rrepresents cycloalkyl,heteroaryl oraryl which is optionally substituted by at least one substituent independently selected from the group consisting of halogen, nitro, hydroxyl, amino, carboxyl, alkoxycarbonyl, cyano, acyl, acyloxy, acylthio, by alkyl, alkyloxy, alkylthio or alkylsulphonyl, each of which is optionally substituted by one or more halogens, by aryl which is optionally substituted by alkyl, alkoxy, halogen or nitro, or optionally by the group --Z--CH.sub.2 --R.sup.4,whereZ represents oxygen or sulphur, andR.sup.4represents cycloalkyl,heteroaryl oraryl which is optionally substituted by halogen, cyano, nitro, hydroxyl, carboxyl, alkoxycarbonyl or by alkyl or alkoxy, each of which is optionally substituted by one or more halogens,R.sup.1 and R.sup.2are identical or different andrepresent straight-chain or branched alkyl which is optionally substituted by aryl, carboxyl, alkoxycarbonyl or by hydroxyl,R.sup.3represents nitro, cyano orthe group ##STR2## where A represents oxygen, sulphur or --N--R.sup.6,R.sup.6 represents hydrogen, phenyl or alkyl,and whereR.sup.5represents hydrogen,cycloalkyl ora hydrocarbon radical which is optionally interrupted in the chain by one or more carbonyl groups and/or sulphur and/or oxygen atoms and is optionally substituted by halogen, nitro, cyano, hydroxyl, mercapto, carboxyl, alkoxycarbonyl, aryl, acyloxy, acylthio, heteroaryl or by an amino group, the amino group carrying one or two identical or different substituents from the group comprising phenyl, alkyl or aralkyl,X and Yare identical or different andrepresent hydrogen,alkyl, alkoxy or alkoxycarbonyl,halogen, hydroxyl, nitro, carboxyl, cyano ortrifluoromethyl or trifluoromethoxy,or physiologically acceptable salts thereof, are active on the cardiovascular system.
摘要翻译：其中R代表环烷基，杂芳基或芳基，其任选被至少一个独立地选自卤素，硝基，羟基，氨基，羧基，氨基，烷氧基，酰氧基，酰氧基，酰硫基，烷基，烷氧基，烷硫基或烷基磺酰基，其各自任选被一个或多个卤素取代，任选被烷基，烷氧基，卤素或硝基取代的芳基，或任选地被基团-Z-CH2-R4，其中Z表示氧或硫，R4表示环烷基，杂芳基或芳基，其任选被卤素，氰基，硝基，羟基，羧基，烷氧基羰基或烷基或烷氧基取代，由一个或多个卤素取代，R 1和R 2相同或不同，表示任选被芳基，羧基，烷氧基羰基或羟基取代的直链或支链烷基，R 3表示硝基，氰基或t 其中A表示氧，硫或-N-R6，R6表示氢，苯基或烷基，R5表示氢，环烷基或烃基，其任选地在链中被一个或多个羰基中断，任选被卤素，硝基，氰基，羟基，巯基，羧基，烷氧基羰基，芳基，酰氧基，酰硫基，杂芳基或氨基取代，所述氨基含有一个或两个相同或不同的烷基或芳烷基，X和Y的取代基是相同或不同的，代表氢，烷基，烷氧基或烷氧基羰基，卤素，羟基，硝基，羧基，氰基或三氟甲基或三氟甲氧基或其生理学上可接受的盐是活性的对心血管系统。

75. 发明授权

US4675328A Phenyl-pyridinium salts and use thereof in inhibiting intestinal resorption 失效
标题翻译：苯基吡啶鎓盐及其在抑制肠吸收中的应用
公开(公告)号：US4675328A
公开(公告)日：1987-06-23
申请号：US819187
申请日：1986-01-15
申请人： Jean-Marie Cassal , Albrecht Edenhofer , Henri Ramuz
发明人： Jean-Marie Cassal , Albrecht Edenhofer , Henri Ramuz
IPC分类号： A61K31/415 , A61K31/42 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4418 , A61K31/4425 , A61P1/00 , A61P3/04 , A61P3/06 , A61P9/10 , C07C49/84 , C07D211/72 , C07D213/04 , C07D213/20 , C07D233/60 , C07D239/26 , C07D277/22 , C07D303/22 , C07D303/34 , C07D303/36 , C07D317/22 , C07D211/84 , C07D213/69 , C07D213/78
CPC分类号： C07D213/20 , C07C205/45 , C07C49/84 , C07D303/22 , C07D303/34 , C07D303/36 , C07D317/22
摘要： Polycyclic salts of the formulaA-XN+CH.sub.2 --(Y).sub.n --(CH.sub.2).sub.p --(Z).sub.q --L--(T).sub.r --M IwhereinA.sup.- is the anion of a strong organic or inorganic acid;XN.sup.+ is pyridinium, pyrimidinium, thiazolium or imidazolium substituted by R.sup.1, R.sup.2 and R.sup.3 ;n, q and r individually are the integer 1 or 0 and p is an integer from 1 to 15;Y is CH.sub.2, C(H,OH) or C(O):Z is O, S, CH.sub.2, C(O), NQ.sup.1, SO.sub.2, C(O)O, OC(O), C(O)N(Q.sup.1) or N(Q.sup.1)C(O);L is p-phenylene substituted by R.sup.4 ; andM is phenyl substituted by R.sup.5 and R.sup.6,T has one of the meanings given above, for Z or is C(CH.sub.3).sub.2, C.sub.2 H.sub.4, C(Q.sup.2).dbd.C(Q.sup.3), C.tbd.C, CH.sub.2 C(O), C(O)CH.sub.2, CH.sub.2 O or OCH.sub.2,R.sup.1 is a group Ar, Ar-C.sub.1-4 -alkyl, ArO or ArC(O),Ar is phenyl substituted by R.sup.7, R.sup.8 and R.sup.9 ;R.sup.2 and R.sup.3 individually are H, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy or C.sub.6 H.sub.5,with the proviso that the N-atom in the 3-position of an imidazolium group XN.sup.+ is substituted by Ar,Ar-C.sub.1-4 -alkyl or C.sub.1-4 -alkyl,R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 individually are H, halogen, CF.sub.3, NO.sub.2, CN, C.sub.1-4 - -(alkyl, alkoxy, alkylthio or alkylsulphonyl), SO.sub.2 N(R,Q), C(O)N(Q.sup.4,Q.sup.5), C(O)Q.sup.4, C(O)OQ.sup.4 or OC(O)Q.sup.4,R, Q, Q.sup.1, Q.sup.2 and Q.sup.3 individually are H orC.sub.1-4 -alkyl, andQ.sup.4 and Q.sup.5 individually are C.sub.1-4 -alkyl inhibit the intestinal resorption of cholesterol and of bile salts in the enterohepatic circulation. These salts containing a quaternary N-atom can be manufactured starting from corresponding amines.
摘要翻译：式A-XN + CH2-（Y）n-（CH2）p-（Z）q-L-（T）r-MⅠ的多环盐，其中A-是强有机或无机酸的阴离子; XN +是被R1，R2和R3取代的吡啶鎓，嘧啶鎓，噻唑鎓或咪唑鎓; n，q和r分别为整数1或0，p为1至15的整数; Y是CH 2，C（H，OH）或C（O）：Z是O，S，CH 2，C（O），NQ 1，SO 2，C（O）O，OC（O） Q1）或N（Q1）C（O）; L是被R4取代的对亚苯基; 并且M是被R 5和R 6取代的苯基，T具有以上给出的含义之一，对于Z或是C（CH 3）2，C 2 H 4，C（Q 2）= C（Q 3），C 3 D C，CH 2 C（O） C（O）CH 2，CH 2 O或OCH 2，R 1是Ar，Ar-C 1-4 - 烷基，ArO或ArC（O）基团，Ar是被R 7，R 8和R 9取代的苯基; R 2和R 3分别是H，C 1-4 - 烷基，C 1-4 - 烷氧基或C 6 H 5，条件是咪唑鎓基团XN +的3-位上的N-原子被Ar取代，Ar-C 1-4 - 烷基或C 1-4 - 烷基，R 4，R 5，R 6，R 7，R 8和R 9分别是H，卤素，CF 3，NO 2，CN，C 1-4 - （烷基，烷氧基，烷硫基或烷基磺酰基），SO 2 N（R， Q），C（O）N（Q4，Q5），C（O）Q4，C（O）OQ4或OC（O）Q4，R，Q，Q1，Q2和Q3分别为H或C1-4烷基，Q4和Q5分别为C1-4烷基，抑制肠肝循环中胆固醇和胆汁盐的肠道吸收。这些含有季氮原子的盐可以从相应的胺开始制备。

76. 发明授权

US4670045A Fungicidal control employing ester derivatives of 4,6-disubstituted 2-pyridinols 失效
标题翻译：使用4,6-二取代的2-吡啶醇的酯衍生物进行杀真菌对照
公开(公告)号：US4670045A
公开(公告)日：1987-06-02
申请号：US748796
申请日：1985-06-26
申请人： Robert J. Ehr , Helen K. Tobol , Lillian H. Troxell
发明人： Robert J. Ehr , Helen K. Tobol , Lillian H. Troxell
IPC分类号： A01N43/40 , A01N47/06 , A01N47/18 , A01N47/20 , C07D213/64 , C07D213/70 , C07D405/12 , C07D211/84
CPC分类号： C07D213/64 , A01N43/40 , A01N47/06 , A01N47/18 , A01N47/20 , C07D213/70 , C07D405/12
摘要： 6-Halo(or CF.sub.3)-4-((di- or tri)halomethyl)-2-pyridinyl esters of carboxylic, carbonic, carbamic, thiocarbamic, sulfonic, or sulfamic acids, exemplified by 6-chloro-4-(trichloromethyl)-2-pyridinyl pentanoate, 4-methylbenzenesulfonate or methylcarbamate, are novel and are useful in the protection of plants from attack by soil-borne fungi.
摘要翻译：羧酸，碳酸，氨基甲酸，硫代氨基甲酸，磺酸或氨基磺酸的6-卤代（或CF 3）-4 - （（二或三）卤代甲基）-2-吡啶基酯，例如6-氯-4-（三氯甲基） -2-吡啶基戊酸酯，4-甲基苯磺酸酯或甲基氨基甲酸酯是新颖的，可用于保护植物免受土壤真菌侵袭。

77. 发明授权

US4539322A Dihydropyridine derivatives and their use in treating heart conditions and hypertension 失效
标题翻译：二氢吡啶衍生物及其在治疗心脏病和高血压中的应用
公开(公告)号：US4539322A
公开(公告)日：1985-09-03
申请号：US528507
申请日：1983-09-01
申请人： Simon F. Campbell , Peter E. Cross , John K. Stubbs
发明人： Simon F. Campbell , Peter E. Cross , John K. Stubbs
IPC分类号： C07D295/08 , A61K31/4422 , A61K31/4427 , A61K31/443 , A61K31/455 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P3/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , C07D211/84 , C07D211/90 , C07D295/088 , C07D401/02 , C07D401/12 , C07D405/12 , C07D407/12 , C07D417/04 , C07D417/12
CPC分类号： C07D295/088 , C07D211/90 , C07D401/12 , C07D407/12 , C07D417/12
摘要： 1,4-Dihydropyridine derivatives of the formula: ##STR1## and their pharmaceutically acceptable acid addition salts; where R is aryl or heteroaryl;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl or2-methoxyethyl;Y is --(CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 --, --CH.sub.2 CH(CH.sub.3)-- or --CH.sub.2 C(CH.sub.3).sub.2 --;R.sup.3 is hydrogen or an organic substituentare useful in treating or preventing heart conditions or hypertension.
摘要翻译：下式的1,4-二氢吡啶衍生物及其药学上可接受的酸加成盐; 其中R是芳基或杂芳基; R 1和R 2各自独立地为C 1 -C 4烷基或2-甲氧基乙基; Y是 - （CH 2）2 - ， - （CH 2）3 - ， - CH 2 CH（CH 3） - 或-CH 2 C（CH 3）2 - R3是氢或有机取代基可用于治疗或预防心脏病或高血压。

78. 发明授权

US4521603A Continuous process for the production of polybromopyridine compounds 失效
标题翻译：连续生产多溴吡啶化合物的方法
公开(公告)号：US4521603A
公开(公告)日：1985-06-04
申请号：US462845
申请日：1983-02-01
申请人： Max M. Boudakian
发明人： Max M. Boudakian
IPC分类号： C07D213/61 , C07D211/84 , C07D213/72 , C07D213/80
CPC分类号： C07D213/61
摘要： A continuous process for producing a polybromopyridine compound comprises admixing a polychloropyridine compound with an anhydrous water soluble solvent in a first reaction zone to form a solution of the polychloropyridine compound. Hydrogen bromide gas is introduced into the solution while maintaining the temperature in the range of from about 70.degree. to about 140.degree. C. to produce a solution of the polybromopyridine compound. The solution is cooled to a temperature in the range of from about 5.degree. to about 35.degree. C. to precipitate the polybromopyridine compound from the anhydrous solvent. The polybromopyridine compound is separated from the anhydrous solvent and the anhydrous solvent is returned to the first reaction zone. Polybromopyridine compounds of increased purity are produced in a process having reduced material, energy and operating costs. The process does not require the use of water or other co-solvents nor the distillation of the reaction product mixture.
摘要翻译：制备多溴吡啶化合物的连续方法包括在第一反应区中混合聚氯吡啶化合物与无水水溶性溶剂以形成聚氯吡啶化合物的溶液。将氢溴化物气体引入溶液中，同时将温度保持在约70℃至约140℃的范围内，以产生多溴吡啶化合物的溶液。将溶液冷却至约5℃至约35℃的温度，从无水溶剂中沉淀出多溴吡啶化合物。从无水溶剂中分离出多溴吡啶化合物，将无水溶剂返回到第一反应区。在具有降低的材料，能量和操作成本的方法中产生增加纯度的多溴吡啶化合物。该方法不需要使用水或其它助溶剂，也不需要蒸馏反应产物混合物。

79. 发明授权

US4483993A Production of polychlorinated pyridine mixtures by liquid phase chlorination of beta-picoline or beta-picoline hydrochloride 失效
标题翻译：通过液相氯化β-甲基吡啶或β-甲基吡啶盐酸盐生产多氯吡啶混合物
公开(公告)号：US4483993A
公开(公告)日：1984-11-20
申请号：US529603
申请日：1983-09-06
申请人： Michael J. Marinak , John L. Simonson
发明人： Michael J. Marinak , John L. Simonson
IPC分类号： B01J19/24 , C07D213/61 , C07D211/72 , C07D211/84
CPC分类号： B01J19/245 , C07D213/61 , B01J2219/00069 , B01J2219/00105 , B01J2219/00132 , B01J2219/00166 , B01J2219/00182 , B01J2219/00186 , B01J2219/1942
摘要： Preparation of high yields of mixtures rich in polychlorinated pyridines by maintaining a chlorine to beta-picoline weight ratio of greater than about 5:1 when reacting chlorine and beta-picoline or beta-picolie hydrochloride non-catalytically in the liquid phase at temperatures of at least about 190.degree. C., the reactants being contained in a well mixed diluent producing less than one mole of hydrogen chlorine per mole of diluent by reaction with the chlorine in the indicated temperature range. Chlorination of the beta-picoline or beta-picoline hydrochloride in a primary reactor is followed by selective further chlorination thereof in finishing reactor means at a temperature of at least about 190.degree. C. to obtain high yields of desired final products useful as intermediates in the formation of herbicides and the like. Like further chlorination to obtain such final products is also applicable to mixtures rich in monochloro-, dichloro-, and trichloro-3-trichloromethyl pyridines produced by other processes.
摘要翻译：通过在液相中将氯和β-甲基吡啶或β-吡啶甲酸盐在液相中反应时，通过保持大于约5:1的氯至β-甲基吡啶的重量比，制备高产率的富含多氯代吡啶的混合物至少约190℃，反应物被包含在充分混合的稀释剂中，通过在指示的温度范围内与氯反应，每摩尔稀释剂产生小于1摩尔的氢氯。在初级反应器中氯化β-甲基吡啶或β-甲基吡啶盐酸盐之后，在整个反应器装置中在至少约190℃的温度下进行选择性进一步氯化，以获得高产率的用作中间体的所需最终产物除草剂的形成等。像进一步氯化以获得这样的最终产物也适用于富含其它方法生产的一氯代，二氯和三氯-3-三氯甲基吡啶的混合物。

80. 发明授权

US4446325A 1,4-Dihydropyridine compounds 失效
标题翻译： 1,4-二氢吡啶化合物
公开(公告)号：US4446325A
公开(公告)日：1984-05-01
申请号：US435183
申请日：1982-10-19
申请人： Sachio Ohno , Kiyoshi Mizukoshi , Osamu Komatsu , Kenzi Ichihara , Takashi Morishima
发明人： Sachio Ohno , Kiyoshi Mizukoshi , Osamu Komatsu , Kenzi Ichihara , Takashi Morishima
IPC分类号： C07D211/84 , C07D211/90 , C07D317/24 , C07D405/12 , C07D409/12 , C07D213/55
CPC分类号： C07D405/12 , C07D211/90 , C07D317/24 , C07D409/12
摘要： 1,4-Dihydropyridine compounds having excellent coronary and vertebral vasodilation, blood pressure depression and anti-hypertensive activities are disclosed. These compounds are low toxic and stable to light, and are very useful for pharmaceutical agents.
摘要翻译：公开了具有优异的冠状和椎体血管舒张，血压抑制和抗高血压活性的1,4-二氢吡啶化合物。这些化合物具有低毒性和光稳定性，对于药剂非常有用。

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