公开(公告)号：US4999370A

公开(公告)日：1991-03-12

申请号：US301297

申请日：1989-01-25

申请人： Wolfgang Ruger ,  Hansjorg Urbach ,  Rainer Henning ,  Jens Stechl ,  Patricia Usinger ,  Franz Hock

发明人： Wolfgang Ruger ,  Hansjorg Urbach ,  Rainer Henning ,  Jens Stechl ,  Patricia Usinger ,  Franz Hock

IPC分类号： C12N9/99 ,  A61K31/55 ,  A61K38/00 ,  A61K38/55 ,  A61K45/06 ,  A61P25/18 ,  A61P25/20 ,  C07D223/10 ,  C07D223/16 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04 ,  C07K1/06 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K14/81 ,  C07D209/02 ,  A61K31/40

CPC分类号： C07K5/0222 ,  A61K38/005

摘要： Compounds with a psychotropic action, agents containing them, and the use thereof for the treatment and prophylaxis of disorders of the central nervous system.The invention relates to the use of angiotensin converting enzyme inhibitors as pharmaceuticals with a psychotropic, especially anxiolytic, action, to agents containing them, and to the use thereof for the treatment or prophylaxis of disorders of the central nervous system, especially of anxiety states.The invention also relates to new compounds of the formula ##STR1## in which R.sup.2 denotes hydrogen or ethyl, and R.sup.3 denotes n-octyl, to processes for the preparation thereof, to agents containing them, and to the use thereof as pharmaceuticals.

摘要翻译： 具有精神作用的化合物，含有它们的药剂及其用于治疗和预防中枢神经系统疾病的用途。 本发明涉及血管紧张素转换酶抑制剂作为具有精神药物，特别是抗焦虑作用的药物对含有它们的药物的用途，以及其用于治疗或预防中枢神经系统疾病，特别是焦虑状态的用途。 本发明还涉及式IMA的新化合物，其中R2表示氢或乙基，R3表示正辛基，其制备方法，含有它们的试剂，以及作为药物的用途。

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：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：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：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.