公开(公告)号：US4876354A

公开(公告)日：1989-10-24

申请号：US191756

申请日：1988-05-03

申请人： Herbert Siegel ,  Klaus-Dieter Kampe ,  Hans G. Alpermann ,  Hermann J. Gerhards ,  Patricia Usinger ,  Ulrich Schacht ,  Margret Leven ,  Wolfgang Raether ,  Walter Dittmar ,  Burkhard Sachse

发明人： Herbert Siegel ,  Klaus-Dieter Kampe ,  Hans G. Alpermann ,  Hermann J. Gerhards ,  Patricia Usinger ,  Ulrich Schacht ,  Margret Leven ,  Wolfgang Raether ,  Walter Dittmar ,  Burkhard Sachse

IPC分类号： A61K31/41 ,  A61K31/415 ,  C07D233/60 ,  C07D233/64 ,  C07D249/08 ,  C07D521/00

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

摘要： Arylmethylazoles of the formula I ##STR1## in which Aryl is (substituted) phenyl or naphthyl;Z is CH or N;R.sup.1 and Q are H or alkyl;R.sup.2 is H, alk(en)yl or alkynyl;R.sup.3 and R.sup.4 are H, alkyl or other hydrocarbons; orR.sup.3 and R.sup.4 together are a --(CH.sub.2).sub.2-11 chain or a bridged --(CH.sub.2).sub.4-5 chain, and their acid addition salts, stereoisomers and optically active enantiomers possess outstanding antimycotic and antidepressant activity.They are obtained, inter alia, from arylmethylazoles II ##STR2## which are reacted with a strong base and then with a carbonyl compound III O.dbd.CR.sup.3 R.sup.4 ; thereafter, the product is reacted with the protic acid or with an alkyl halide IV R.sup.2 Hal.If desired, the products are converted to the acid addition salts, or the stereoisomers or optically active enantiomers are resolved.

摘要翻译： 芳基甲基唑，其中芳基是（取代的）苯基或萘基; Z是CH或N; R1和Q是H或烷基; R2是H，烷（烯）基或炔基; R3和R4是H，烷基或其他烃; 或R 3和R 4一起是 - （CH 2）2-11链或桥连 - （CH 2）4-5链，并且它们的酸加成盐，立体异构体和旋光对映异构体具有突出的抗真菌和抗抑郁活性。 它们特别由芳基甲基唑II II获得，它们与强碱反应，然后与羰基化合物III = CR 3 R 4反应; 此后，产物与质子酸或烷基卤IVR 2 Hal反应。 如果需要，将产物转化成酸加成盐，或者立体异构体或光学活性对映体被分解。

公开(公告)号：US4999352A

公开(公告)日：1991-03-12

申请号：US441200

申请日：1989-11-28

申请人： Klaus-Dieter Kampe ,  Patricia Usinger ,  Herbert Siegel ,  Hans G. Alpermann ,  Hermann J. Gerhards

发明人： Klaus-Dieter Kampe ,  Patricia Usinger ,  Herbert Siegel ,  Hans G. Alpermann ,  Hermann J. Gerhards

IPC分类号： A61K31/415 ,  A61P25/24 ,  A61P25/26 ,  A61P31/04 ,  C07D233/60 ,  C07D233/61 ,  C07D405/06 ,  C07D521/00

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

摘要： 1-(1-Aryl-2-hydroxyethyl)-imidazoles and salts thereof, processes for the preparation thereof, medicaments containing these compounds, and the use thereof.The invention relates to 1-(1-aryl-2-hydroxyethyl)-imidazoles of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, Q, W, X and Y have the meanings specified, and also to medicaments based on these compounds, in particular those having an antimycotic and an antidepressive action.

摘要翻译： 1-（1-芳基-2-羟乙基） - 咪唑及其盐，其制备方法，含有这些化合物的药物及其用途。 本发明涉及式Ⅰ的1-（1-芳基-2-羟乙基） - 咪唑，其中R1，R2，R3，Q，W，X和Y具有指定的含义，还涉及基于 对这些化合物，特别是具有抗真菌和抗抑郁作用的化合物。

公开(公告)号：US5023357A

公开(公告)日：1991-06-11

申请号：US411045

申请日：1989-09-21

申请人： Herbert Siegel ,  Klaus-Dieter Kampe ,  Hans-Georg Alpermann ,  Hermann J. Gerhards ,  Patricia Usinger ,  Ulrich Schacht ,  Margret Leven ,  Wolfgang Raether ,  Walter Dittmar ,  Burkhard Sachse

发明人： Herbert Siegel ,  Klaus-Dieter Kampe ,  Hans-Georg Alpermann ,  Hermann J. Gerhards ,  Patricia Usinger ,  Ulrich Schacht ,  Margret Leven ,  Wolfgang Raether ,  Walter Dittmar ,  Burkhard Sachse

IPC分类号： A61K31/41 ,  A61K31/415 ,  C07D233/60 ,  C07D233/64 ,  C07D249/08 ,  C07D521/00

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

摘要： Arylmethylazoles of the formula I ##STR1## in which Aryl is (substituted) phenyl or naphthyl;Z is CH or N;R.sup.1 and Q are H or alkyl;R.sup.2 is H, alk(en)yl or alkynyl;R.sup.3 l and R.sup.4 are H, alkyl or other hydrocarbons; orR.sup.3 and R.sup.4 together are a --(CH.sub.2).sub.2-11 chain or a bridged --(CH.sub.2).sub.4-5 chain,and their acid addition salts, stereoisomers and optically active enantiomers possess outstanding antimycotic and antidepressant activity.They are obtained, inter alia, from arylmethylazoles II ##STR2## which are reacted with a strong base and then with a carbonyl compound III 0=CR.sup.3 R.sup.4 ; thereafter, the product is reacted with the protic acid or with an alkyl halide IV R.sup.2 Hal.If desired, the products are converted to the acid addition salts, or the stereoisomers or optically active enantiomers are resolved.

公开(公告)号：US5100890A

公开(公告)日：1992-03-31

申请号：US411256

申请日：1989-09-25

申请人： Herbert Siegel ,  Klaus-Dieter Kampe ,  Hans-Georg Alpermann ,  Hermann J. Gerhards ,  Patricia Usinger ,  Ulrich Schacht ,  Margret Leven ,  Wolfgang Raether ,  Walter Dittmar ,  Burkhard Sachse

发明人： Herbert Siegel ,  Klaus-Dieter Kampe ,  Hans-Georg Alpermann ,  Hermann J. Gerhards ,  Patricia Usinger ,  Ulrich Schacht ,  Margret Leven ,  Wolfgang Raether ,  Walter Dittmar ,  Burkhard Sachse

IPC分类号： A61K31/41 ,  A61K31/415 ,  C07D233/60 ,  C07D233/64 ,  C07D249/08 ,  C07D521/00

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

摘要： Arylmethylazoles of the formula I ##STR1## in which Aryl is (substituted) phenyl or naphthyl;Z is CH or N;R.sup.1 and Q are H or alkyl;R.sup.2 is H, alk(en)yl or alkynyl;R.sup.3 and R.sup.4 are H, alkyl or other hydrocarbons; orR.sup.3 and R.sup.4 together are a--(CH.sub.2).sub.2-11 chain or a bridged--(CH.sub.2).sub.4-5 chain,and their acid addition salts, stereoisomers and optically active enantiomers possess outstanding antimycotic and antidepressant activity.They are obtained, inter alia, from arylmethylazoles II ##STR2## which are reacted with a strong base and then with a carbonyl compound III O.dbd.CR.sup.3 R.sup.4 ; thereafter, the product is reacted with the protic acid or with an alkyl halide IV R.sup.2 Hal.If desired, the products are converted to the acid addition salts, or the stereoisomers or optically active enantiomes are resolved.

公开(公告)号：US5141937A

公开(公告)日：1992-08-25

申请号：US247968

申请日：1988-09-21

申请人： Herbert Siegel ,  Ernold Granzer

发明人： Herbert Siegel ,  Ernold Granzer

IPC分类号： C07C251/44 ,  A61K31/045 ,  A61K31/12 ,  A61K31/135 ,  A61K31/15 ,  A61K31/165 ,  A61K31/19 ,  A61K31/215 ,  A61K31/275 ,  A61K31/34 ,  A61K31/343 ,  A61K31/40 ,  A61K31/495 ,  A61K31/535 ,  A61K31/5375 ,  A61P3/06 ,  A61P9/10 ,  C07C45/00 ,  C07C49/643 ,  C07C61/39 ,  C07C61/40 ,  C07C62/32 ,  C07C67/00 ,  C07C209/00 ,  C07C209/40 ,  C07C209/50 ,  C07C211/29 ,  C07C213/00 ,  C07C217/74 ,  C07C217/76 ,  C07C217/80 ,  C07C227/00 ,  C07C227/18 ,  C07C229/46 ,  C07C231/00 ,  C07C231/02 ,  C07C233/58 ,  C07C235/40 ,  C07C237/24 ,  C07C239/00 ,  C07D209/76 ,  C07D295/06 ,  C07D295/073 ,  C07D295/18 ,  C07D295/185 ,  C07D307/93

CPC分类号： C07D295/185 ,  A61K31/045 ,  A61K31/12 ,  A61K31/19 ,  A61K31/215 ,  A61K31/275 ,  A61K31/34 ,  A61K31/40 ,  C07D295/073

摘要： Pharmaceutical products containing a 7-diphenylmethylenebicycloheptane or 7-diphenylmethylenebicycloheptene derivative of the formula I ##STR1## in which A, B, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the stated meanings, or a physiologically tolerated acid addition salt of these compounds, and the use thereof as hypolipidemics are described. In addition, new 7-diphenylmethylenebicycloheptane and -heptene derivatives of the formula Ia ##STR2## in which A, B, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the stated meanings, and the physiologically tolerated acid addition salts thereof, as well as processes for the preparation thereof, are described.

摘要翻译： 含有其中A，B，R 1，R 2，R 3和R 4具有所述含义的式I的7-二苯基亚甲基双环庚烷或7-二苯基亚甲基双环庚烯衍生物或这些化合物的生理上耐受的酸加成盐， 描述其作为降血脂药物的用途。 此外，其中A，B，R 1，R 2，R 3和R 4具有所述含义的式Iaa Ia的新的7-二苯基亚甲基双环庚烷和庚烯衍生物及其生理上耐受的酸加成盐，以及方法 描述其制备方法。

公开(公告)号：US5114816A

公开(公告)日：1992-05-19

申请号：US431221

申请日：1989-11-03

申请人： Siegfried Scheler ,  Gerhard Buhr ,  Helmut Lenz ,  Klaus Bergmann ,  Herbert Siegel

发明人： Siegfried Scheler ,  Gerhard Buhr ,  Helmut Lenz ,  Klaus Bergmann ,  Herbert Siegel

IPC分类号： C07C309/26 ,  C07C309/52 ,  C07C309/73 ,  C07C311/37 ,  C07C323/66 ,  G03F7/022

CPC分类号： G03F7/022 ,  C07C309/26 ,  C07C2101/16

摘要： The invention relates to novel radiation-sensitive compounds which are esters or amides of a 1,2-naphthoquinone-(2)-diazide-4-sulfonic acid of the general formula ##STR1## in which R.sub.1 and R.sub.2 are identical or different and denote hydrogen, an alkyl group, an alkyl ether group or an alkyl thioether group whose carbon chains may be interrupted by ether oxygen atoms, an acylamino group, carboxylic acid ester group, sulfonic acid ester group or sulfonamide group,R.sub.1 and R.sub.2 not being hydrogen at the same time.The compounds are used as radiation-sensitive components in radiation-sensitive mixtures with which corresponding copying materials can be produced. The compounds have an absorption which is directed towards longer wavelengths matching the emission range of commercially available radiation sources. They also make it possible, in a reliable and practical manner, to carry out negativeworking image reversal processes.

摘要翻译： 本发明涉及新的辐射敏感化合物，它们是通式为（I）的1,2-萘醌 - （2） - 二叠氮-4-磺酸的酯或酰胺，其中R 1和R 2相同或 不同的表示氢，烷基，烷基醚基或其碳链可被醚氧原子间隔的烷基硫醚基，酰氨基，羧酸酯基，磺酸酯基或磺酰胺基，R1和R2不是 同时是氢。 这些化合物用作辐射敏感性混合物中的辐射敏感组分，可以制备相应的复印材料。 这些化合物具有吸收，该吸收指向与市售辐射源的发射范围匹配的较长波长。 它们也使得以可靠和实际的方式实现负面的图像反转过程成为可能。

公开(公告)号：US4855087A

公开(公告)日：1989-08-08

申请号：US127175

申请日：1987-12-01

申请人： Herbert Siegel

发明人： Herbert Siegel

IPC分类号： B01J31/02 ,  B01J31/00 ,  B01J31/26 ,  C07B61/00 ,  C07F9/42

CPC分类号： C07F9/42

摘要： The invention relates to a process for the preparation of 2-chloroethanephosphonyl dichloride by reaction of an ester of 2-chloroethanephosphonic acid of the formula ##STR1## or a mixture of the two esters with thionyl chloride at a temperature of 60.degree. to 160.degree. C. Phosphine oxides are employed as catalysts therein. The thionyl chloride is added to the initially introduced ester.

摘要翻译： 本发明涉及一种制备2-氯乙烷膦酰基二氯化物的方法，该方法是将式（Ⅱ）所示的2-氯乙酰膦酸的酯与式（Ⅱ）的混合物与亚硫酰氯在60℃的温度下反应 DEG至160℃。使用氧化膦作为其中的催化剂。 将亚硫酰氯加入到初始引入的酯中。

公开(公告)号：US4761252A

公开(公告)日：1988-08-02

申请号：US90229

申请日：1987-08-27

申请人： Herbert Siegel ,  Erwin Weiss ,  Harald Berger

发明人： Herbert Siegel ,  Erwin Weiss ,  Harald Berger

IPC分类号： B01J27/08 ,  B01J27/138 ,  B01J31/00 ,  B01J31/02 ,  C07B61/00 ,  C07F9/42

CPC分类号： C07F9/42

摘要： The invention relates to a process for the preparation of vinylphosphonic dichloride, in which a 2-chloroethanephosphonate of the formula ##STR1## or a mixture of the two esters, is reacted with thionyl chloride at a temperature of 60.degree. to 160.degree. C. in the presence of a catalyst which contains tertiary phosphines, quaternary ammonium or phosphonium salts or alkali metal or alkaline-earth metal halides.During this reaction, any thionyl chloride which may be present is removed by distillation subsequent to this reaction, the mixture remaining is heated to 140.degree. to 200.degree. C., and the vinylphosphonic dichloride produced during this is removed by distillation.

摘要翻译： 本发明涉及一种制备乙烯基膦酸二氯化物的方法，其中将式（II）的2-氯乙基膦酸盐或两种酯的混合物与亚硫酰氯在60至160℃的温度下反应。 在含有叔膦，季铵或鏻盐或碱金属或碱土金属卤化物的催化剂的存在下。 在该反应中，在该反应之后，通过蒸馏除去可能存在的任何亚硫酰氯，将剩余的混合物加热至140℃至200℃，并通过蒸馏除去其中产生的乙烯基膦酰氯。

公开(公告)号：US4761251A

公开(公告)日：1988-08-02

申请号：US089964

申请日：1987-08-27

申请人： Herbert Siegel ,  Erwin Weiss ,  Harald Berger

发明人： Herbert Siegel ,  Erwin Weiss ,  Harald Berger

IPC分类号： B01J31/00 ,  C07B61/00 ,  C07F9/42

CPC分类号： C07F9/42

摘要： The invention relates to a process for the preparation of vinylphosphonic dichloride through elimination of hydrogen chloride from 2-chloroethanephosphonic dichloride in the presence of catalysts. The catalysts used are tertiary phosphines, quaternary ammonium or phosphonium salts or alkali metal or alkaline-earth metal halides. When triphenyl phosphine is used as the catalyst, the reaction is carried out under reduced pressure at a temperature of 130.degree. to 166.degree. C. and the vinylphosphonic dichloride produced is simultaneously removed by distillation under reduced pressure. When the other catalysts are used, the process can be carried out at atmospheric pressure or reduced pressure and at temperatures of about 130.degree. to 220.degree. C. and the vinylphosphonic dichloride produced can be removed by distillation simultaneously with or subsequent to the reaction.

摘要翻译： 本发明涉及通过在催化剂存在下从2-氯乙烷膦酸二氯中除去氯化氢来制备乙烯基膦酸二氯化物的方法。 所用的催化剂是叔膦，季铵或鏻盐或碱金属或碱土金属卤化物。 当使用三苯基膦作为催化剂时，反应在130〜166℃的温度下进行减压蒸馏，同时通过减压蒸馏同时除去生成的乙烯基膦酸二氯。 当使用其它催化剂时，该方法可以在大气压或低压下和在约130℃至220℃的温度下进行，并且所产生的乙烯基膦酸二氯化物可以在反应或反应后同时通过蒸馏除去。

公开(公告)号：US4749524A

公开(公告)日：1988-06-07

申请号：US89827

申请日：1987-08-27

申请人： Herbert Siegel ,  Erwin Weiss ,  Harald Berger

发明人： Herbert Siegel ,  Erwin Weiss ,  Harald Berger

IPC分类号： B01J27/00 ,  B01J27/08 ,  B01J27/138 ,  B01J31/00 ,  B01J31/02 ,  C07B61/00 ,  C07F9/42

CPC分类号： C07F9/42

摘要： The invention relates to a process for the preparation of 2-chloroethanephosphonic dichloride through reaction of a 2-chloroethanephosphonate of the formula ##STR1## or a mixture of the two esters, with thionyl chloride at a temperature of 60.degree. to 160.degree. C. In this reaction, tertiary phosphines, quaternary ammonium or phosphonium salts or alkali metal or alkaline-earth metal halides are employed as catalysts. The thionyl chloride is introduced into the initially introduced ester.

摘要翻译： 本发明涉及一种制备2-氯乙烷膦酸二氯化物的方法，该方法是将式（Ⅱ）所示的2-氯乙基膦酸酯与式（Ⅱ）的混合物与亚硫酰氯反应，温度为60℃至 160℃。在该反应中，使用叔膦，季铵或鏻盐或碱金属或碱土金属卤化物作为催化剂。 将亚硫酰氯引入初始引入的酯中。