公开(公告)号：US4211551A

公开(公告)日：1980-07-08

申请号：US850468

申请日：1977-11-10

申请人： Kurt Thiele ,  Quazi Ahmed ,  Walter Scharen ,  Jacques Meyer

发明人： Kurt Thiele ,  Quazi Ahmed ,  Walter Scharen ,  Jacques Meyer

IPC分类号： A01N39/04 ,  A01P13/00 ,  A01N9/24

CPC分类号： A01N39/04

摘要： Herbicidal compositions for selective weed control comprising 4-(4'-chlorobenzyl)-phenoxy acetic acid or a salt thereof and the novel salts of 4-(4'-chlorobenzyl)-phenoxy acetic acid.A method for selectively controlling weeds by applying to a crop area an effective amount of 4-(4'-chlorobenzyl)-phenoxy acetic acid or a salt of said acid.

摘要翻译： 用于选择性杂草控制的除草组合物包含4-（4'-氯苄基） - 苯氧基乙酸或其盐和4-（4'-氯苄基） - 苯氧基乙酸的新型盐。 通过向作物区域施加有效量的4-（4'-氯苄基） - 苯氧基乙酸或所述酸的盐来选择性地控制杂草的方法。

公开(公告)号：US4275068A

公开(公告)日：1981-06-23

申请号：US48536

申请日：1979-04-23

申请人： Kurt Thiele ,  Quazi Ahmed ,  Ulrich Jahn ,  Rudolf Adrian

发明人： Kurt Thiele ,  Quazi Ahmed ,  Ulrich Jahn ,  Rudolf Adrian

IPC分类号： C07D213/80 ,  A61K31/455 ,  A61K31/60 ,  C07C69/90

CPC分类号： C07D213/80

摘要： Novel alkylene glycol derivatives of the formula (1) ##STR1## in which R.sup.1 is the hydrogen atom, an alkyl group having 1-4 C-atoms or an aryl group, R.sup.2 is the hydrogen atom or an alkyl group having 1-4 C-atoms, R.sup.3 is the hydrogen atom or a group of the formula ##STR2## in which Z is an alkyl residue, an optionally substituted aryl residue or a heterocyclic residue and R.sup.4 is a residue of the formula ##STR3## in which R.sup.5 is the hydrogen atom or chlorine atom, or the methyl group, exhibit an advantageous activity in regard of lowering the cholesterol and triglyceride level in the blood. Production of the novel derivatives by reduction of the corresponding acids, or by reacting a phenol of the formula ##STR4## and an alcohol of the formula ##STR5## optionally with subsequent esterification, is described.

摘要翻译： 式（1）的新型亚烷基二醇衍生物其中R1是氢原子，具有1-4个碳原子的烷基或芳基，R2是氢原子或具有1个碳原子的烷基 -4个C原子，R3是氢原子或其中Z是烷基残基，任选取代的芳基残基或杂环残基的式“IMAGE”的基团，R4是式“IMAGE”的残基，其中 R5是氢原子或氯原子或甲基，在降低血液中的胆固醇和甘油三酯水平方面表现出有利的活性。 描述了通过还原相应的酸或通过使式（IMAGE）的酚与式（IMAGE）的醇任选地随后的酯化反应制备新衍生物。

公开(公告)号：US4214095A

公开(公告)日：1980-07-22

申请号：US6542

申请日：1979-01-25

申请人： Kurt Thiele ,  Quazi Ahmed ,  Rudolf Adrian ,  Ulrich Jahn

发明人： Kurt Thiele ,  Quazi Ahmed ,  Rudolf Adrian ,  Ulrich Jahn

IPC分类号： C07C69/712 ,  A61K31/19 ,  A61K31/195 ,  A61K31/215 ,  A61K31/22 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4418 ,  A61P3/06 ,  C07C51/00 ,  C07C59/125 ,  C07C59/68 ,  C07C67/00 ,  C07C69/612 ,  C07C201/00 ,  C07C205/37 ,  C07D213/30 ,  C07C69/76

CPC分类号： C07D213/30 ,  C07C205/37 ,  C07C59/68

摘要： Novel compounds of the formula (1) ##STR1## wherein R.sup.1 and R.sup.2 are different lower alkyls and R.sup.3 is a lower alkyl or a methyl pyridine group, and the acid addition salts of formula (1) compounds when R.sup.3 is methyl pyridine. The novel compounds have an asymmetric C-atom and may be in the form of the D,L racemates or the D or L stereoisomers.These compounds are useful in the treatment of hypercholesterolemia and hyperlipidemia because of their high effectiveness in reducing the level of cholesterol and lipids in the blood combined with very low general toxicities and substantially reduced hepatomegalitic effects.

摘要翻译： 式（1）的新型化合物其中R1和R2是不同的低级烷基，R3是低级烷基或甲基吡啶基，当式（1）的酸加成盐化合物当R3是甲基吡啶时 。 新化合物具有不对称C原子，并且可以是D，L外消旋物或D或L立体异构体的形式。 这些化合物可用于治疗高胆固醇血症和高脂血症，因为它们在降低血液中的胆固醇和脂质的水平方面具有很高的有效性，同时具有非常低的一般毒性和显着降低的肝母细胞效应。

公开(公告)号：US4115393A

公开(公告)日：1978-09-19

申请号：US773145

申请日：1977-03-01

申请人： Kurt Thiele ,  Quazi Ahmed ,  Rudolf Adrian ,  Ulrich Jahn

发明人： Kurt Thiele ,  Quazi Ahmed ,  Rudolf Adrian ,  Ulrich Jahn

IPC分类号： C07C59/68 ,  C07C59/70 ,  C07D211/46 ,  C07D213/55 ,  C07D473/08

CPC分类号： C07C321/00 ,  C07C59/68 ,  C07C59/70 ,  C07D211/46 ,  C07D473/08

摘要： Compounds of the formula ##STR1## WHEREIN R represents hydrogen, halogen, hydroxy or alkyl or alkoxy containing from 1 to 4 carbon atoms;X represents benzyl, benzyloxy or benzylthio, or benzyl, benzyloxy or benzylthio substituted by a said radical R;A.sup.1 and A.sup.2 which can be the same or different are hydrogen or alkyl radical containing up to 10 carbon atoms such that the total number of carbon atoms in A.sup.1 and A.sup.2 is not more than 10;n is an integer of from 1 to 3;m is 1 or 2;And pharmacologically acceptable salts thereof.These compounds have pharmaceutical utility by virtue of their ability to reduce the level of fatty substances in the blood.

摘要翻译： 式中的R 1表示氢，卤素，羟基或含有1至4个碳原子的烷基或烷氧基; X表示苄基，苄氧基或苄硫基，或被所述基团R取代的苄基，苄氧基或苄硫基; 可以相同或不同的A 1和A 2是氢或含有至多10个碳原子的烷基，使得A1和A2中的碳原子总数不大于10; N是1到3的整数; M IS 1 OR 2; 及其药理学上可接受的药物。

公开(公告)号：US4483999A

公开(公告)日：1984-11-20

申请号：US773148

申请日：1977-03-01

申请人： Kurt Thiele ,  Quazi Ahmed ,  Rudolf Adrian ,  Ulrich Jahn

发明人： Kurt Thiele ,  Quazi Ahmed ,  Rudolf Adrian ,  Ulrich Jahn

IPC分类号： C07C59/68 ,  C07C59/70 ,  C07C69/712 ,  C07D211/46 ,  C07D473/08 ,  C07C69/76

CPC分类号： C07C321/00 ,  C07C59/68 ,  C07C59/70 ,  C07D211/46 ,  C07D473/08

摘要： Novel compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, halogen, or alkyl or alkoxy containing from 1 to 4 carbon atoms,R.sup.2 is hydrogen, halogen, hydroxy or alkyl of alkoxy containing from 1 to 4 carbon atoms,n and m are integers such that the sum (n+m) lies in the range from 3 to 10 inclusive and n differs from m, andx is alkyl containing from 1 to 4 carbon atoms, hydrogen or a cation which is a metal cation of main Groups 1, 2 and 3 of the Periodic System of the Elements, an organic base cation or an ammonium ion. These compounds have pharmaceutical utility by virtue of their considerable ability to reduce the level of fatty substances in the blood.

摘要翻译： 式中，R 1为氢，卤素，含有1至4个碳原子的烷基或烷氧基，R2为氢，卤素，羟基或含有1至4个碳原子的烷氧基烷基，n和m的新型化合物 整数，使得和（n + m）在3〜10的范围内，n与m不同，x是含有1〜4个碳原子的烷基，氢或作为主体1的金属阳离子的阳离子 ，元素周期系统的2和3，有机碱性离子或铵离子。 这些化合物由于其相当的降低血液中脂肪物质含量的能力而具有药用效用。

公开(公告)号：US4153803A

公开(公告)日：1979-05-08

申请号：US773144

申请日：1977-03-01

申请人： Kurt Thiele ,  Quazi Ahmed ,  Rudolf Adrian ,  Ulrich Jahn

发明人： Kurt Thiele ,  Quazi Ahmed ,  Rudolf Adrian ,  Ulrich Jahn

IPC分类号： A61K31/22 ,  C07C59/68 ,  C07C59/70 ,  C07C69/712 ,  C07C69/736 ,  C07D211/46 ,  C07D213/30 ,  C07D473/08 ,  C07C69/76

CPC分类号： C07C321/00 ,  C07C59/68 ,  C07C59/70 ,  C07D211/46 ,  C07D473/08

摘要： Compounds possessing pharmaceutical activity as substances able to lower the level of fatty substances in the blood possess the following general formula: ##STR1## wherein R represents hydrogen, halogen, hydroxy or alkyl or alkoxy containing from 1 to 4 carbon atoms;A.sup.1 and A.sup.2 which can be the same or different are hydrogen or alkyl containing from 1 to 9 carbon atoms such that A.sup.1 and A.sup.2 contain together not more than 10 carbon atoms,Y is oxygen, in which case X is benzyl, benzyloxy or benzylthio or benzyl, benzyloxy or benzylthio substituted by R and Z is amine, azacyclohydrocarbyloxy cycloalkoxy containing from 3 to 6 ring carbon atoms or tertiary aminoalkoxy or pivaloyloxyalkoxy in which the alkoxy group contains from 1 to 3 carbon atoms, or X is hydrogen and Z is pivaloyloxyalkoxy in which the alkoxy group contains from 1 to 3 carbon atoms, orY is oxygen, X is benzyl, benzyloxy or benzylthio or benzyl, benzyloxy or benzylthio substituted by R and Z is alkoxy containing from 1 to 4 carbon atoms, hydroxy or O.sup.- M.sup.+, M being a metal cation of Main Groups I, II or III of the Periodic System of the Elements or an organic base cation or ammonium ion, A.sup.1 and A.sup.2 being the same and being as aforesaid or being different with one of A.sup.1 and A.sup.2 being hydrogen or both being hydrogen and X being a para substituent with respect to Y in the benzene ring in the same general formula,Y is oxygen, X is hydrogen and Z is amine, azacyclohydrocarbyloxy or pivaloyloxyalkoxy in which the alkoxy group contains from 1 to 3 carbon atoms,Or Y is sulphur, in which case X is hydrogen, benzyl, benzyloxy or benzylthio or benzyl, benzyloxy or benzylthio substituted by R and Z is amine, azacyclohydrocarbyloxy, alkoxy containing from 1 to 4 carbon atoms, hydroxy, O.sup.- M.sup.+ wherein M is a metal cation of Main Groups I, II or III of the Periodic System of The Elements or an organic base cation or ammonium ion, cycloalkoxy containing from 3 to 6 ring carbon atoms or tertiaryaminoalkoxy, pivaloyloxyalkoxy or pyridyl-C-alkoxy in which the alkoxy group contains from 1 to 3 carbon atoms, and pharmacologically acceptable acid addition and quaternary ammonium salts of compounds containing basic groups, and optical isomers of said compounds when A.sup.1 and A.sup.2 are different.

公开(公告)号：US4554356A

公开(公告)日：1985-11-19

申请号：US692324

申请日：1985-01-16

申请人： Ludwig Zirngibl ,  Kurt Thiele

发明人： Ludwig Zirngibl ,  Kurt Thiele

IPC分类号： C07D233/00 ,  B01J31/02 ,  C07B61/00 ,  C07D233/60 ,  C07D233/68 ,  C07D233/70 ,  C07D233/91 ,  C07D333/00 ,  C07D401/00 ,  C07D409/00 ,  C07D521/00

CPC分类号： C07D231/12 ,  C07D249/08

摘要： A process for the manufacture of imidazolylvinyl ethers of the formula ##STR1## wherein Im represents the substituted or unsubstituted 1-H-imidazol-1-yl group and An, R and Y are defined hereinbelow by condensation of a corresponding ketone of the formulaAr--CO--CHR--Im (II)with the splitting-off of a Z group, with a condensable substance of the formulaZ--Y (III)in the aqueous solution of a strong inorganic base, preferably in concentrated aqueous soda lye. The reaction may also be carried out in the presence of a second liquid organic phase, preferably benzene or toluene, especially in the presence of a phase transfer catalyst in this case. Through careful crystallization of the product manufactured according to this method, it is possible to manufacture approximately pure E-isomers of the imidazolylvinyl ether of formula (I), without the requirement of chromatographic separation.

摘要翻译： PCT No.PCT / EP82 / 00010 Sec。 371日期1982年5月24日 102（e）日期1982年5月24日PCT提交1982年1月21日PCT公布。 出版物WO82 / 02552 日本1982年8月5日。一种制备式（I）的咪唑基乙烯基醚的方法，其中Im表示取代或未取代的1-H-咪唑-1-基，An，R和Y定义如下 通过将式Ar-CO-CHR-Im（II）的相应的酮与Z基团的分离与式ZY（III）的可冷凝物质在强无机碱的水溶液中缩合， 优选在浓缩的苏打碱液中。 反应也可以在第二液体有机相存在下进行，优选苯或甲苯，特别是在这种情况下在相转移催化剂存在下。 通过根据该方法制造的产品的仔细结晶，可以制备式（I）的咪唑基乙烯基醚的近似纯的E-异构体，而不需要色谱分离。

公开(公告)号：US4330545A

公开(公告)日：1982-05-18

申请号：US150964

申请日：1980-05-19

申请人： Ludwig Zirngibl ,  Johanna Fischer ,  Kurt Thiele

发明人： Ludwig Zirngibl ,  Johanna Fischer ,  Kurt Thiele

IPC分类号： A01N43/50 ,  C07C43/225 ,  A01N43/54 ,  A01N43/56 ,  C07D401/12 ,  C07D403/12 ,  C07D407/12 ,  C07D409/12

CPC分类号： C07C43/225 ,  A01N43/50

摘要： Aryl-imidazol-1-yl vinyl ethers and their acid addition salts are disclosed, wherein the imidazolyl vinyl ether has the formula: ##STR1## Ar in the formula represents a substituted or unsubstituted aryl or heterocyclic radical; R represents hydrogen or a C.sub.1 -C.sub.12 alkyl or cycloalkyl (saturated or unsaturated) or Ar as above; Im represents a 1-H-imidazol-1-yl group (unsubstituted or substituted); and Y represents a saturated or unsaturated C.sub.1 -C.sub.12 alkyl or a group --Z--Ar in which Ar has the above meaning and --Z-- is a saturated or unsaturated C.sub.1 -C.sub.12 alkylene wherein each of the alkyl and the alkylene may have a carbon chain once or twice interrupted by or, in the case of the alkylene, terminated on its Ar-end by oxy, thio, sulfinyl or sulfonyl bridges, always with the proviso that at least one of Ar and Y is a heterocyclic radical. These compounds are wide-spectrum fungicides and bactericides, and the preferred compounds among them are hydrophilic.

摘要翻译： 公开了芳基 - 咪唑-1-基乙烯基醚及其酸加成盐，其中咪唑基乙烯基醚具有下式：下式中的Ar表示取代或未取代的芳基或杂环基; R代表氢或C1-C12烷基或环烷基（饱和或不饱和）或如上所述的Ar; Im表示1-H-咪唑-1-基（未取代或取代的）; 并且Y表示饱和或不饱和的C 1 -C 12烷基或基团-Z-Ar，其中Ar具有上述含义，-Z-是饱和或不饱和的C 1 -C 12亚烷基，其中烷基和亚烷基中的每一个可以具有碳 链中断一次或两次，或者在亚烷基的情况下，通过氧基，硫基，亚磺酰基或磺酰基桥接在其Ar末端上，条件是Ar和Y中的至少一个是杂环基。 这些化合物是广谱杀菌剂和杀菌剂，其中优选的化合物是亲水的。

公开(公告)号：US4603204A

公开(公告)日：1986-07-29

申请号：US474230

申请日：1983-03-11

申请人： Kurt Thiele ,  Felix Geissmann ,  Ludwig Zirngibl ,  Ulrich Jahn

发明人： Kurt Thiele ,  Felix Geissmann ,  Ludwig Zirngibl ,  Ulrich Jahn

IPC分类号： A61K31/52 ,  A61K31/522 ,  A61P25/02 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D295/22 ,  C07D307/02 ,  C07D473/08

CPC分类号： C07D473/08

摘要： New derivatives of theophylline having the formula ##STR1## in which R denotes hydrogen or OH, n the numbers 0 or 1, X either >CH-- or >N--, Y either --O-- or --CO-- and R a five membered or six membered aryl ring or hetero-aryl ring, that is substituted in given cases with halogen, short chain alkyl groups, alkoxy groups or halogen-alkyl, and exhibit in addition to other properties, histamine-, serotinine- bradykynine- antagonistic, anti-anaphylactic and -adrenergic stimulating effects.

摘要翻译： 具有式（I）的茶碱的新衍生物，其中R表示氢或OH，n为数字0或1，X或> CH-或> N-，Y为-O-或-CO-，R a 在给定的情况下被卤素，短链烷基，烷氧基或卤素 - 烷基取代的五元或六元芳基环或杂芳基环，并且除了其它性质外，还表现出组胺，血清素 - 卡那霉素拮抗剂 ，抗过敏和肾上腺素能刺激作用。

公开(公告)号：US4210657A

公开(公告)日：1980-07-01

申请号：US970330

申请日：1978-12-18

申请人： Ludwig Zirngibl ,  Johanna Fischer ,  Kurt Thiele

发明人： Ludwig Zirngibl ,  Johanna Fischer ,  Kurt Thiele

IPC分类号： A01N43/50 ,  A61K31/415 ,  A61P31/04 ,  C07C43/225 ,  C07D233/60 ,  C07D233/68 ,  C07D233/91 ,  C07D521/00

CPC分类号： C07D231/12 ,  A01N43/50 ,  C07C43/225 ,  C07D233/56 ,  C07D249/08

摘要： Aryl-imidazol-1-yl vinyl ethers and their acid addition salts are disclosed, wherein the imidazolyl vinyl ether has the formula: ##STR1## Ar in the formula represents a substituted or unsubstituted aryl or heterocyclic radical; R represents hydrogen or a C.sub.1 -C.sub.12 alkyl or cycloalkyl (saturated or unsaturated) or Ar as above; Im represents a 1-H-imidazol-1-yl group (unsubstituted or substituted); and Y represents a saturated or unsaturated, acyclic or cyclic C.sub.1 -C.sub.12 alkyl, or aryl or aralkyl, or an alkyl or alkylene residue directly bound to the ether oxygen and having a chain once or twice interrupted by --O--, --S--, --SO-- or --SO.sub.2 -- bridges. These compounds are effective wide spectrum fungicides and bactericides.

摘要翻译： 公开了芳基 - 咪唑-1-基乙烯基醚及其酸加成盐，其中咪唑基乙烯基醚具有下式：式中的Ar表示取代或未取代的芳基或杂环基; R代表氢或C1-C12烷基或环烷基（饱和或不饱和）或如上所述的Ar; Im表示1-H-咪唑-1-基（未取代或取代的）; 并且Y表示饱和或不饱和的无环或环状C 1 -C 12烷基或芳基或芳烷基，或直接键合到醚氧上并具有一个或两个被-O - ， - S - 间隔的链的烷基或亚烷基， -SO-或-SO 2 - 桥。 这些化合物是有效的广谱杀菌剂和杀菌剂。