公开(公告)号：US4320061A

公开(公告)日：1982-03-16

申请号：US243745

申请日：1981-03-16

申请人： Heinrich-Wilhelm Ohlendorf ,  Klaus-Ullrich Wolf ,  Wilhelm Kaupmann ,  Henning Heinemann

发明人： Heinrich-Wilhelm Ohlendorf ,  Klaus-Ullrich Wolf ,  Wilhelm Kaupmann ,  Henning Heinemann

IPC分类号： A61K31/335 ,  A61K31/37 ,  A61P1/00 ,  A61P1/14 ,  C07D313/08

CPC分类号： C07D313/08

摘要： Novel, 3-amino-1-benzoxepin-5(2H)-one derivatives and methods for their production are disclosed. These derivatives correspond to the Formula I: ##STR1## wherein: R.sub.1 and R.sub.2 independently of one another are hydrogen,C.sub.1 -C.sub.3 alkyl,C.sub.1 -C.sub.5 alkyl substituted with a terminal phenyl, or a phenyl containing one or two halogens, methyl or methoxy groups, a 3,4-methylenedioxy or a 3,4 -ethylenedioxy group,C.sub.2 -C.sub.5 alkyl substituted with terminal hydroxy or methoxy or,C.sub.3 -C.sub.4 alkenyl; orone of R.sub.1 and R.sub.2 are hydrogen or a C.sub.1 -C.sub.5 alkyl and the other is a C.sub.2 -C.sub.5 alkyl substituted with a terminal NR.sub.5 R.sub.6 ;R.sub.5 and R.sub.6 independently of one another are hydrogen or C.sub.1 -C.sub.5 alkyl; orR.sub.5 and R.sub.6 are together a 5 or 7 member ring, orR.sub.5 and R.sub.6 are together a 5 to 7 member ring having heterogeneous oxygen, sulfur or nitrogen;R.sub.1 and R.sub.2 are together a 5 to 7 member ring, orR.sub.1 and R.sub.2 are together a 5 to 7 member ring having heterogeneous oxygen, sulfur or NR.sub.7 ;R.sub.7 is hydrogen, methyl, benzyl or phenyl;R.sub.3 and R.sub.4 are independently of one another are hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio; orone of R.sub.3 and R.sub.4 is trifluoromethyl or nitro and the other is hydrogen;and the acid addition salts thereof. These compounds have a favorable effect on the treatment of spasms of the stomach-intestinal tract and, therefore, constitute the active ingredient of pharmaceutical compositions and methods for the treatment of disorders of the stomach and intestinal tract. Processes for the preparation of the derivatives and their acid addition salts and intermediate products for their preparation are also described.

摘要翻译： 公开了3-氨基-1-苯并氧杂-5（2H） - 酮衍生物及其生产方法。 这些衍生物对应于式I：其中：R 1和R 2彼此独立地是氢，C 1 -C 3烷基，被末端苯基取代的C 1 -C 5烷基或含有一个或两个卤素的苯基，甲基或 甲氧基，3,4-亚甲二氧基或3,4-亚乙二氧基，被末端羟基或甲氧基取代的C2-C5烷基，或C3-C4烯基; 或R 1和R 2中的一个为氢或C 1 -C 5烷基，另一个为被末端NR 5 R 6取代的C 2 -C 5烷基; R 5和R 6彼此独立地是氢或C 1 -C 5烷基; 或R 5和R 6一起为5或7元环，或者R 5和R 6一起是具有异质氧，硫或氮的5至7元环; R 1和R 2一起为5至7元环，或者R 1和R 2一起为具有异质氧，硫或NR 7的5至7元环; R7是氢，甲基，苄基或苯基; R 3和R 4彼此独立地为氢，卤素，C 1 -C 4烷基，C 1 -C 4烷氧基或C 1 -C 4烷硫基; 或者R 3和R 4中的一个是三氟甲基或硝基，另一个是氢; 及其酸加成盐。 这些化合物对胃肠道痉挛的治疗具有有利的作用，因此构成了用于治疗胃肠道疾病的药物组合物和方法的活性成分。 还描述了制备衍生物及其酸加成盐和中间产物用于制备的方法。

公开(公告)号：US4279904A

公开(公告)日：1981-07-21

申请号：US173075

申请日：1980-07-28

申请人： Heinrich-Wilhelm Ohlendorf ,  Klaus-Ullrich Wolf ,  Wilhelm Kaupmann ,  Henning Heinemann

发明人： Heinrich-Wilhelm Ohlendorf ,  Klaus-Ullrich Wolf ,  Wilhelm Kaupmann ,  Henning Heinemann

IPC分类号： A61K31/335 ,  A61K31/35 ,  A61K31/55 ,  A61P1/00 ,  A61P1/14 ,  C07D313/08

CPC分类号： C07D313/08

摘要： Novel 3-amino-1-benzoxepine derivatives and methods for their production are disclosed. These derivatives correspond to the Formula I ##STR1## wherein: R.sub.1 and R.sub.2 independently of one another arehydrogen,C.sub.1 -C.sub.5 alkyl,C.sub.1 -C.sub.5 alkyl substituted with a terminal phenyl, or a phenyl containing one or two halogens, methyl or methoxy groups, a 3,4-methylenedioxy or a 3,4-ethylenedioxy group,C.sub.2 -C.sub.5 alkyl substituted with terminal hydroxy or methoxy or,C.sub.3 -C.sub.4 alkenyl; orone of R.sub.1 and R.sub.2 are hydrogen or a C.sub.1 -C.sub.5 alkyl and the other is a C.sub.2 -C.sub.5 alkyl substituted with a terminal NR.sub.7 R.sub.8 ;R.sub.7 and R.sub.8 independently of one another are hydrogen or C.sub.1 -C.sub.5 alkyl; orR.sub.7 and R.sub.8 are together a 5 to 7 member ring or said ring having heterogeneous oxygen, sulfur or nitrogen, orR.sub.1 and R.sub.2 are together a 5 to 7 member ring or said ring having heterogeneous oxygen, sulfur or NR.sub.9 ;R.sub.9 is hydrogen, methyl, benzyl, or phenyl;one of R.sub.3 and R.sub.4 is hydrogen and the other hydroxy, orR.sub.3 and R.sub.4 together are oxygen;R.sub.5 and R.sub.6 independently of one another are hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio; orone of R.sub.5 and R.sub.6 is trifluoromethyl or nitro and the other is hydrogen; the stereo isomers and the acid addition salts thereof. These compounds have a favorable effect upon the motility of the gastro-intestinal tract and, therefore, constitute the active ingredient of pharmaceutical compositions and methods for the treatment of motility disorders.

摘要翻译： 公开了新的3-氨基-1-苯并恶庚因衍生物及其生产方法。 这些衍生物对应于式I其中：R1和R2彼此独立地是氢，C1-C5烷基，被末端苯基取代的C1-C5烷基或含有一个或两个卤素的苯基，甲基或甲氧基 基团，3,4-亚甲二氧基或3,4-亚乙二氧基，被末端羟基或甲氧基取代的C 2 -C 5烷基或C 3 -C 4烯基; 或R 1和R 2中的一个为氢或C 1 -C 5烷基，另一个为被末端NR 7 R 8取代的C 2 -C 5烷基; R 7和R 8彼此独立地是氢或C 1 -C 5烷基; 或R 7和R 8一起为5至7元环或所述具有异质氧，硫或氮的环，或R 1和R 2一起为5至7元环或所述具有异质的氧，硫或NR 9的环; R9是氢，甲基，苄基或苯基; R3和R4之一是氢，另一个羟基或R3和R4一起是氧; R 5和R 6彼此独立地是氢，卤素，C 1 -C 4烷基，C 1 -C 4烷氧基或C 1 -C 4烷硫基; 或者R 5和R 6中的一个是三氟甲基或硝基，另一个是氢; 立体异构体及其酸加成盐。 这些化合物对胃肠道的运动性具有有利的作用，因此构成用于治疗运动障碍的药物组合物和方法的活性成分。

公开(公告)号：US4279905A

公开(公告)日：1981-07-21

申请号：US173076

申请日：1980-07-28

申请人： Heinrich-Wilhelm Ohlendorf ,  Klaus-Ullrich Wolf ,  Wilhelm Kaupmann

发明人： Heinrich-Wilhelm Ohlendorf ,  Klaus-Ullrich Wolf ,  Wilhelm Kaupmann

IPC分类号： A61K31/335 ,  A61K31/37 ,  A61P1/00 ,  A61P1/14 ,  C07D313/08

CPC分类号： C07D313/08

摘要： Novel, 3-amino-1-benzoxepin-5 (2H)-one derivatives and methods for their production are disclosed. These derivatives correspond to the Formula I: ##STR1## wherein: R.sub.1 and R.sub.2 independently of one another arehydrogen,C.sub.1 -C.sub.5 alkyl,C.sub.1 -C.sub.5 alkyl substituted with a terminal phenyl, or a phenyl containing one or two halogens, methyl or methoxy groups, a 3,4-methylenedioxy or a 3,4-ethylenedioxy group,C.sub.2 -C.sub.5 alkyl substituted with terminal hydroxy or methoxy or,C.sub.3 -C.sub.4 alkenyl; orone of R.sub.1 and R.sub.2 are hydrogen or a C.sub.1 -C.sub.5 alkyl and the other is a C.sub.2 -C.sub.5 alkyl substituted with a terminal NR.sub.5 R.sub.6 ;R.sub.5 and R.sub.6 independently of one another are hydrogen or C.sub.1 -C.sub.5 alkyl; orR.sub.5 and R.sub.6 are together a 5 to 7 member ring, orR.sub.5 and R.sub.6 are together a 5 to 7 member ring having heterogeneous oxygen, sulfur or nitrogen;R.sub.1 and R.sub.2 are together a 5 to 7 member ring, orR.sub.1 and R.sub.2 are together a 5 to 7 member ring having heterogeneous oxygen, sulfur or NR.sub.7 ;R.sub.7 is hydrogen, methyl, benzyl or phenyl;R.sub.3 and R.sub.4 independently of one another are hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio; orone of R.sub.3 and R.sub.4 is trifluoromethyl or nitro and the other is hydrogen;and the acid addition salts thereof. These compounds have a favorable effect on the treatment of spasms of the stomach-intestinal tract and, therefore, constitute the active ingredient of pharmaceutical compositions and methods for the treatment of disorders of the stomach and intestinal tract. Processes for the preparation of the derivatives and their acid addition salts and intermediate products for their preparation are also descrived.

摘要翻译： 公开了3-氨基-1-苯并氧杂-5（2H） - 酮衍生物及其生产方法。 这些衍生物对应于式I：其中：R 1和R 2彼此独立地是氢，C 1 -C 5烷基，被末端苯基取代的C 1 -C 5烷基或含有一个或两个卤素的苯基，甲基或 甲氧基，3,4-亚甲二氧基或3,4-亚乙二氧基，被末端羟基或甲氧基取代的C 2 -C 5烷基或C 3 -C 4烯基; 或R 1和R 2中的一个为氢或C 1 -C 5烷基，另一个为被末端NR 5 R 6取代的C 2 -C 5烷基; R 5和R 6彼此独立地是氢或C 1 -C 5烷基; 或R 5和R 6一起为5至7元环，或者R 5和R 6一起为具有异质的氧，硫或氮的5至7元环; R 1和R 2一起为5至7元环，或者R 1和R 2一起为具有异质氧，硫或NR 7的5至7元环; R7是氢，甲基，苄基或苯基; R 3和R 4彼此独立地是氢，卤素，C 1 -C 4烷基，C 1 -C 4烷氧基或C 1 -C 4烷硫基; 或者R 3和R 4中的一个是三氟甲基或硝基，另一个是氢; 及其酸加成盐。 这些化合物对胃肠道痉挛的治疗具有有利的作用，因此构成了用于治疗胃肠道疾病的药物组合物和方法的活性成分。 还描述了制备衍生物及其酸加成盐和中间产物用于其制备的方法。

公开(公告)号：US4924004A

公开(公告)日：1990-05-08

申请号：US264049

申请日：1988-10-28

申请人： Heinrich-Wilhelm Ohlendorf ,  Wilhelm Kaupmann ,  Ulrich Kuehl ,  Gerd Buschmann ,  Stephen Magda

发明人： Heinrich-Wilhelm Ohlendorf ,  Wilhelm Kaupmann ,  Ulrich Kuehl ,  Gerd Buschmann ,  Stephen Magda

IPC分类号： C07D209/14 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P9/06 ,  C07D209/24 ,  C07D209/42

CPC分类号： C07D209/42

摘要： New 1-phenyl-2-aminocarbonylindole compounds are described which have the general formula I ##STR1## where R.sub.1 is a hydrogen atom, or a lower alkyl, alkenyl, cycloalkyl or cycloalkylalkyl radical, R.sub.2 is a hydrogen atom or a lower alkyl radical, R.sub.3 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, R.sub.4 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, or, if R.sub.3 is a hydrogen atom, R.sub.4 may be a nitro or trifluoromethyl radical, or R.sub.3 and R.sub.4 together denote a methylenedioxy or ethylenedioxy radical, R.sub.5 has the meanings given for R.sub.3, R.sub.6 has the meanings given for R.sub.4, R.sub.7 is a hydrogen atom or, if R.sub.5 and R.sub.6 are lower alkoxy radicals, R.sub.7 may also be a lower alkoxy radical, R.sub.8 and R.sub.9 are each a hydrogen atom or a lower alkyl radical or, together with the nitrogen atom, form a heterocyclic group, and Z is a alkylene chain which is optionally substituted by hydroxyl. The compounds have pharmacological properties, in particular antiarrhythmic properties. The compounds may be in the form of the free base or acid addition salts. Pharmaceutical compositions containing these compounds are described as is a method of preparing them.Valuable intermediates for the production of these compounds and methods of preparing the intermediates are also described.

公开(公告)号：US4814345A

公开(公告)日：1989-03-21

申请号：US123201

申请日：1987-11-20

申请人： Heinrich-Wilhelm Ohlendorf ,  Wilhelm Kaupmann ,  Ulrich Kuhl ,  Gerd Buschmann ,  Stephen J. Magda

发明人： Heinrich-Wilhelm Ohlendorf ,  Wilhelm Kaupmann ,  Ulrich Kuhl ,  Gerd Buschmann ,  Stephen J. Magda

IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P9/06 ,  C07D209/42 ,  A61K31/405

CPC分类号： C07D209/42

摘要： Novel 1-phenyl-2-aminocarbonylindole compounds are disclosed having the general formula I ##STR1## wherein R.sub.1 is an aliphatic or aromatic acyl group or an optionally substituted benzyl group; R.sub.2 is hydrogen or a lower alkyl radical; R.sub.3 is a hydrogen, a halogen, a lower alkyl radical, or a lower alkoxy radical; R.sub.4 is hydrogen, a halogen, a lower alkyl radical, or a lower alkoxy radical; R.sub.5 has the significance given R.sub.3 ; R.sub.6 has the significance given for R.sub.4, or R.sub.6 is nitro or trifluoromethyl; R.sub.7 and R.sub.8 each represent hydrogen or a lower alkyl radical, or together with a nitrogen atom form a heterocyclic group; and Z signifies an alkylene chain optionally substituted by hydroxy or acyloxy. The compounds have pharmacological, in particular antiarrhythmic, properties.

摘要翻译： 公开了具有通式I的新型1-苯基-2-氨基羰基吲哚化合物，其中R 1是脂族或芳族酰基或任选取代的苄基; R2是氢或低级烷基; R3是氢，卤素，低级烷基或低级烷氧基; R4是氢，卤素，低级烷基或低级烷氧基; R5具有给定R3的意义; R6对R4具有重要意义，或R6是硝基或三氟甲基; R7和R8各自表示氢或低级烷基，或与氮原子一起形成杂环基; Z表示任选被羟基或酰氧基取代的亚烷基链。 这些化合物具有药理学，特别是抗心律不齐的特性。

公开(公告)号：US4803198A

公开(公告)日：1989-02-07

申请号：US885684

申请日：1986-07-15

申请人： Heinrich-Wilhelm Ohlendorf ,  Wilhelm Kaupmann ,  Ulrich Kuehl ,  Gerd Buschmann ,  Stephen J. Magda

发明人： Heinrich-Wilhelm Ohlendorf ,  Wilhelm Kaupmann ,  Ulrich Kuehl ,  Gerd Buschmann ,  Stephen J. Magda

IPC分类号： C07D209/14 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P9/06 ,  C07D209/24 ,  C07D209/42 ,  A61K31/55 ,  C07D403/12 ,  C07D403/14

CPC分类号： C07D209/42

摘要： New 1-phenyl-2-aminocarbonylindole compounds are described which have the general formula I ##STR1## where R.sub.1 is a hydrogen atom, or a lower alkyl, alkenyl, cycloalkylalkyl radical, R.sub.2 is a hydrogen atom or a lower alkyl radical, R.sub.3 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, R.sub.4 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, or, if R.sub.3 is a hydrogen atom, R.sub.4 may be a nitro or trifluoromethyl radical, or R.sub.3 and R.sub.4 together denote a methylenedioxy or ethylenedioxy radical, R.sub.5 has the meanings given for R.sub.3, R.sub.6 has the meanings given for R.sub.4, R.sub.7 is a hydrogen atom or, if R.sub.5 and R.sub.6 are lower alkoxy radicals, R.sub.7 may also be a lower alkoxy radical, R.sub.8 and R.sub.9 are each a hydrogen atom or a lower alkyl radical or, together with the nitrogen atom, form a heterocyclic group, and Z is an alkylene chain which is optionally substituted by hydroxyl. The compounds have pharmaceutical properties, in particular antiarrhythmic properties. The compounds may be in the form of the free bases or acid addition salts. Pharmaceutical compositions containing these compounds are described as is a method of preparing them.Valuable intermediates for the production of these compounds and methods of preparing the intermediates are also described.

摘要翻译： 描述了具有通式Ⅰ的新的1-苯基-2-氨基羰基吲哚化合物，其中R 1是氢原子，或低级烷基，烯基，环烷基烷基，R 2是氢原子或低级烷基，R 3 是氢或卤素原子，或低级烷基，羟基或低级烷氧基，R4是氢或卤素原子，或低级烷基，羟基或低级烷氧基，或者如果R3是氢原子，R4可以是 硝基或三氟甲基，或R 3和R 4一起表示亚甲二氧基或亚乙二氧基，R 5具有R 3的含义，R 6具有对R 4的定义，R 7是氢原子，或者如果R 5和R 6是低级烷氧基，则R 7 也可以是低级烷氧基，R 8和R 9各自为氢原子或低级烷基，或者与氮原子一起形成杂环基，Z为任选被羟基取代的亚烷基链。 这些化合物具有药物性质，特别是抗心律失常性质。 化合物可以是游离碱或酸加成盐的形式。 含有这些化合物的药物组合物被描述为制备它们的方法。 还描述了制备这些化合物的有价值的中间体和制备中间体的方法。

公开(公告)号：US4009184A

公开(公告)日：1977-02-22

申请号：US477091

申请日：1974-06-06

申请人： Wilhelm Kaupmann ,  Klaus-Wolf VON Eickstedt ,  Salah-Eldin Rahman

发明人： Wilhelm Kaupmann ,  Klaus-Wolf VON Eickstedt ,  Salah-Eldin Rahman

IPC分类号： C07D307/80 ,  C07D307/81

CPC分类号： C07D307/81 ,  C07D307/80

摘要： Compounds which are amino carbonyl derivatives of benzofurans which have the formula ##STR1## in which R is a hydrogen, halogen, or alkyl radical containing up to 4 carbon atoms, X is a phenyl, halophenyl, alkylphenyl, or alkoxyphenyl radical, the alkyl moieties of which contain up to 4 carbon atoms, and Y is a dialkylamino radical, the alkyl moieties of which contain up to 4 carbon atoms, or a pyrrolidino, piperidino, hexamethylenimino, morpholino, piperazino, 4-methylpiperazino, or 4-(2-hydroxyethyl)piperazino radical, and acid addition salts thereof, processes for their preparation, and pharmaceutical compositions containing these compounds.

摘要翻译： 作为具有式“IMAGE”的苯并呋喃的氨基羰基衍生物的化合物，其中R是含有至多4个碳原子的氢，卤素或烷基，X是苯基，卤代苯基，烷基苯基或烷氧基苯基，烷基部分 其中含有至多4个碳原子，Y是其烷基部分含有至多4个碳原子的二烷基氨基，或吡咯烷子基，哌啶子基，六亚甲基亚氨基，吗啉代，哌嗪基，4-甲基哌嗪基或4-（2- 羟乙基）哌嗪基及其酸加成盐，其制备方法和含有这些化合物的药物组合物。