公开(公告)号：US4610984A

公开(公告)日：1986-09-09

申请号：US601637

申请日：1984-04-18

申请人： Karl Schonafinger ,  Rudi Beyerle ,  Ursula Schindler ,  Piero Martorana ,  Rolf-Eberhard Nitz

发明人： Karl Schonafinger ,  Rudi Beyerle ,  Ursula Schindler ,  Piero Martorana ,  Rolf-Eberhard Nitz

IPC分类号： C07D295/18 ,  A61K31/495 ,  A61P25/28 ,  C07D207/16 ,  C07D213/82 ,  C07D295/192 ,  C07D295/205 ,  C07D295/215 ,  C07D307/68 ,  C07D409/12 ,  C07D295/20

CPC分类号： C07D213/82 ,  C07D207/16 ,  C07D295/192 ,  C07D295/205 ,  C07D295/215 ,  C07D307/68 ,  C07D409/12

摘要： This invention relates to certain 4-acyl-piperazine-1-acetamides. These compounds are useful as memory and learning enhancers and for the treatment and prevention of cerebral insufficiency.

摘要翻译： 本发明涉及某些4-酰基哌嗪-1-乙酰胺。 这些化合物可用作记忆和学习增强剂以及治疗和预防脑功能不全。

公开(公告)号：US4305939A

公开(公告)日：1981-12-15

申请号：US166951

申请日：1980-07-08

申请人： Karl Schonafinger ,  Rudi Beyerle ,  Rolf-Eberhard Nitz ,  Piero A. Martorana ,  Volker Fiedler

发明人： Karl Schonafinger ,  Rudi Beyerle ,  Rolf-Eberhard Nitz ,  Piero A. Martorana ,  Volker Fiedler

IPC分类号： C07D413/04 ,  A61K31/4245 ,  A61K31/425 ,  A61K31/495 ,  A61K31/496 ,  A61K31/54 ,  A61P9/00 ,  A61P9/12 ,  C07D271/04 ,  C07D295/28 ,  C07D413/06 ,  C07D417/04 ,  A61K31/38 ,  A61K31/41 ,  C07D279/10

CPC分类号： C07D295/30 ,  C07D271/04

摘要： Physiologically-acceptable 3-aminosydnonimines of the formula ##STR1## and their pharmacologically-acceptable acid-addition salts, when formulated into medicament dosage forms, are useful for reducing systemic blood pressure, pulmonary artery pressure and left ventricular end diastolic pressure when orally administered to patients in need of such pressure reduction. These compounds are prepared by cyclizing a compound which, in its free-base state, is of the formula ##STR2## to a corresponding product which, in its free-base state, is of the formula ##STR3## and, when R.sup.2 is other than --H, acylating that product.

摘要翻译： 当配制成药物剂型时，式（I）的生理学上可接受的3-氨基亚氨基亚胺及其药理学上可接受的酸加成盐可用于降低全身血压，肺动脉压和左心室舒张末期压 口服给予需要减压的患者。 这些化合物通过将其游离碱状态为具有式（II）的化合物环化成相应的产物，其在其游离碱状态下具有式（Ia） 并且当R2不是-H时，酰化该产物。

公开(公告)号：US4020071A

公开(公告)日：1977-04-26

申请号：US531324

申请日：1974-12-10

申请人： Thomas Raabe ,  Otto Grawinger ,  Josef Scholtholt ,  Rolf-Eberhard Nitz ,  Eckhard Schraven

发明人： Thomas Raabe ,  Otto Grawinger ,  Josef Scholtholt ,  Rolf-Eberhard Nitz ,  Eckhard Schraven

IPC分类号： C07D239/26 ,  C07D303/22 ,  C07D303/24 ,  C07D239/06

CPC分类号： C07D303/22 ,  C07D239/26 ,  C07D303/24 ,  Y10S514/821

摘要： The present invention relates to new pharmacologically valuable derivatives of 1-phenoxy-3-amino-propan-2-ol having the formula ##STR1## and the aldehyde condensation products and acid addition salts thereof wherein X is selected from the group consisting of ##STR2## wherein the phenyl ring I may have attached to it up to three similar or different substituents selected from the group consisting of alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, alkoxy, alkenyloxy, alkinyloxy, benzyloxy, phenyl, halogen and --NR.sub.1 R.sub.2, wherein R.sub.1 is selected from alkyl and acyl, and R.sub.2 is selected from hydrogen and alkyl; and to the production thereof by a method selected from (A) reacting 1-phenoxy-3-amino-propan-2-ol having the formula ##STR3## with a compound having the formula Y-X, wherein X has the above-defined meaning and Y is selected from halogen, --OH, --OK or --ONa; (B) reacting a compound of the formula ##STR4## with a compound of the formula H.sub.2 N--X, wherein X has the above-defined meaning and Z is selected from ##STR5## and ##STR6## (C) reacting a phenol ##STR7## wherein X and Z have the meaning defined above.

摘要翻译： 本发明涉及具有下式的1-苯氧基-3-氨基 - 丙-2-醇的新药理学上有价值的衍生物及其醛缩合产物及其酸加成盐，其中X选自和，其中苯环I可以连接至多至三个相似或不同的选自烷基，烯基，炔基，环烷基，环烯基，烷氧基，烯氧基，烷氧基，苄氧基，苯基，卤素和 -NR1R2，其中R1选自烷基和酰基，R2选自氢和烷基; 并且通过选自（A）使具有式“IMAGE”的1-苯氧基-3-氨基 - 丙-2-醇与具有式YX的化合物反应的方法制备，其中X具有上述含义， Y选自卤素，-OH，-OK或-ONa; （B）使式“IMAGE”的化合物与式H2N-X的化合物反应，其中X具有上述含义并且Z选自和（C）使苯酚其中X和Z具有上述定义。

公开(公告)号：US3987036A

公开(公告)日：1976-10-19

申请号：US488578

申请日：1974-07-15

申请人： Heinz Bender ,  Otto Grawinger ,  Adolf Stachel, deceased ,  by Ingeburg Lydia Katharina Stachel, heiress ,  Rudi Beyerle ,  Josef Scholtholt ,  Rolf-Eberhard Nitz

发明人： Heinz Bender ,  Otto Grawinger ,  Adolf Stachel, deceased ,  by Ingeburg Lydia Katharina Stachel, heiress ,  Rudi Beyerle ,  Josef Scholtholt ,  Rolf-Eberhard Nitz

IPC分类号： C07D237/32 ,  C07C69/635 ,  C07D239/90 ,  C07D239/95 ,  C07D239/96 ,  C07D253/08 ,  C07D311/16 ,  C07D239/80 ,  C07D401/06

CPC分类号： C07D253/08 ,  C07D311/16

摘要： The present invention relates to new pharmacologically valuable, basically substituted heterocyclic compounds of the formula ##EQU1## wherein X represents--N=N----ch=n-- ##EQU2## R represents an aliphatic, cycloaliphatic, araliphatic or aromatic amine radical having 2 to 10 carbon atoms or the radical of a 5, 6 or 7 ring-membered heterocyclic amine optionally containing an additional N, O or S hetero atom, the radical being attached through the nitrogen atom,R.sub.1 and R.sub.2 represent alkoxy groups containing 1 - 4 C-atoms, R.sub.3 represents lower alkyl having 1 - 3 C-atoms and m and n are 1, 2 or 3.The above derivatives are produced by acylating heterocyclic derivatives having the formula ##STR1## with an alkoxycinnamic acid of the general formula ##STR2## OR A FUNCTIONAL DERIVATIVE OF THE LATTER, OPTIONALLY IN THE PRESENCE OF AN ACID-BINDING AGENT, THE RADICALS R, R.sub.1, R.sub.2, n and m having the meanings set out above.

公开(公告)号：US3706739A

公开(公告)日：1972-12-19

申请号：US3706739D

申请日：1970-05-18

申请人： RUDI BEYERLE ,  ROLF EBERHARD NITZ ,  KLAUS RESAG ,  ECKHARD SCHRAVEN ,  ADOLF STACHEL

发明人： BEYERLE RUDI ,  NITZ ROLF-EBERHARD ,  RESAG KLAUS ,  SCHRAVEN ECKHARD ,  STACHEL ADOLF

IPC分类号： C07D253/08 ,  C07D87/36

CPC分类号： C07D253/08 ,  Y10S514/929

摘要： The present invention pertains to new, pharmacologically valuable basically substituted 1,2,3-benzotriazine-4(3H)-one derivatives having excellent coronary dilator properties and which have the structural formula

WHEREIN R'' is a radical selected from the group consisting of a secondary aliphatic, cycloaliphatic or araliphatic amine containing two to 10 carbon atoms; or of a 5, 6 or 7-membered heterocyclic nitrogen base, which contains in the nucleus in addition to the nitrogen atom a corresponding number of methylene groups as well as an additional member selected from the group consisting of a nitrogen, an oxygen or a sulfur atom, said radical being bound via a nitrogen atom; R1 is an alkoxy group having one to four carbon atoms, which may be in the 6,7 or 6,7,8-position; R2 is an alkoxy group having one to four carbon atoms; m is an integer selected from 1, 2 and 3; and n is an integer selected from 2 and 3; and to processes for producing said derivatives.

摘要翻译： 本发明涉及具有优异冠状动脉扩张剂性质的新的，药理学有价值的基本上取代的1,2,3-苯并三嗪-4（3H） - 酮衍生物，其结构式为：WHEREIN R'是选自以下的基团 含有2至10个碳原子的仲脂族，脂环族或芳脂族胺; 或5,6或7-元杂环氮碱，其在核中除了氮原子之外还含有相应数目的亚甲基以及另外的选自氮，氧或 硫原子，所述基团通过氮原子结合; R1是具有1-4个碳原子的烷氧基，其可以是6,7或6,7,8位; R2是具有1-4个碳原子的烷氧基; m是选自1,2和3的整数; n为选自2和3的整数; 以及制备所述衍生物的方法。

公开(公告)号：US4845091A

公开(公告)日：1989-07-04

申请号：US885081

申请日：1986-07-14

申请人： Karl Schonafinger ,  Rudi Beyerle ,  Helmut Bohn ,  Melitta Just ,  Piero Martorana ,  Rolf-Eberhard Nitz

发明人： Karl Schonafinger ,  Rudi Beyerle ,  Helmut Bohn ,  Melitta Just ,  Piero Martorana ,  Rolf-Eberhard Nitz

IPC分类号： A61K31/41 ,  A61K31/4245 ,  A61K31/445 ,  A61K31/495 ,  A61K31/496 ,  A61K31/535 ,  A61K31/5377 ,  A61K31/54 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D271/04 ,  C07D317/00 ,  C07D413/12 ,  C07D493/04

CPC分类号： C07D413/12 ,  C07D271/04 ,  C07D493/04

摘要： Optically active substituted 3-aminosydnonimines of the general formula I ##STR1## and their pharmacologically acceptable acid addition salts, wherein R.sup.1 denotes, for example, the radical R.sup.3 (R.sup.4)N-,R.sup.2 denotes the radical 1-methoxyethyl (--CH(CH.sub.3)OCH.sub.3), acetoxy-phenyl-methyl (--CH(C.sub.6 H.sub.5)O--COCH.sub.3), 1-(ethoxycarbonyl)-ethoxy (--O--CH.sub.3)CO.sub.2 C.sub.2 H.sub.5),R.sup.3 denotes alkyl(C.sub.1 -C.sub.4) andR.sup.4 denotes for example alkyl(C.sub.1 -C.sub.4),possess valuable pharmaceutical properties.

摘要翻译： 通式Ⅰ的光学活性的取代的3-氨基二氨基亚胺及其药学上可接受的酸加成盐，其中R1表示例如基团R3（R4）N-，R2表示基团1-甲氧基乙基（-CH（ CH 3）OCH 3），乙酰氧基 - 苯基 - 甲基（-CH（C 6 H 5）O-COCH 3），1-（乙氧基羰基） - 乙氧基（-O-CH 3）CO 2 C 2 H 5），R 3表示烷基（C 1 -C 4） 烷基（C1-C4）具有有价值的药物性质。

公开(公告)号：US4760147A

公开(公告)日：1988-07-26

申请号：US941176

申请日：1986-12-12

申请人： Karl Schonafinger ,  Helmut Bohn ,  Piero Martorana ,  Rolf-Eberhard Nitz

发明人： Karl Schonafinger ,  Helmut Bohn ,  Piero Martorana ,  Rolf-Eberhard Nitz

IPC分类号： A61K31/44 ,  A61P3/00 ,  A61P3/14 ,  A61P9/00 ,  C07D211/90 ,  C07D413/04 ,  C07D493/04

CPC分类号： C07D413/04 ,  C07D211/90 ,  C07D493/04

摘要： Optically active substituted 1,4-dihydropyridines of the formula I having calcium antogonistic properties: ##STR1## wherein R denotes alkyl with 1 to 5 C atoms, alkoxy-alkyl with 1 to 4 C atoms, in the alkoxy part and 2 to 4 C atoms in the alkyl part, dialkylaminioalkyl with a total of 3 to 6 C atoms each of the alkyl groups as substituents on the amino group having 1 to 3 C atoms, or --CH(CH.sub.3)CO.sub.2 R.sup.5 in the optically active (R)-forms,R.sup.1 denotes phenyl which is monosubstituted by cyano, nitro or chlorine or is disubstituted by chlorine, R.sup.2 denotes oxadiazolyl, or an oxadiaxolyl which is substituted by methyl, ethyl, i-propyl, tert.-butyl, benzyl, methylthio, i-propylthio, aminocarbonylthio or methoxymethyl,R.sup.5 denotes alkyl with 1 to 4 C atoms, and acid-addition salts thereof, and acid addition salts thereof.

摘要翻译： 式I的光学活性取代的1,4-二氢吡啶具有钙非共轭性：其中R表示具有1至5个C原子的烷基，烷氧基 - 烷基，具有1至4个C原子，烷氧基部分和2 至烷基部分中的4个C原子，具有3至6个C原子的二烷基氨基烷基，每个烷基作为在具有1至3个C原子的氨基上的取代基，或光学活性的R（CH 3）CO 2 R 5 ）形式，R 1表示被氰基，硝基或氯单取代或被氯二取代的苯基，R 2表示恶二唑基，或被甲基，乙基，异丙基，叔丁基，苄基，甲硫基取代的恶二唑基， 异丙硫基，氨基羰硫基或甲氧基甲基，R5表示具有1-4个C原子的烷基，及其酸加成盐及其酸加成盐。

公开(公告)号：US3940406A

公开(公告)日：1976-02-24

申请号：US362567

申请日：1973-05-21

申请人： Thomas Raabe ,  Josef Scholtholt ,  Rolf-Eberhard Nitz

发明人： Thomas Raabe ,  Josef Scholtholt ,  Rolf-Eberhard Nitz

IPC分类号： C07D213/30 ,  A61K31/4406 ,  C07D213/38 ,  C07D213/50 ,  C07D303/24 ,  C07D413/06 ,  C07D213/36 ,  C07D213/40

CPC分类号： C07D303/24 ,  C07D213/38 ,  C07D213/50

摘要： The present invention relates to pharmacologically valuable new derivatives of 1-phenoxy-3-amino-propane-2-ol and process for their production. The new derivatives of 1-phenoxy-3-amino-propane-2-ol are suitable for the treatment and prophylaxis of diseases of the heart. Some possess pronounced .beta.-adrenalytic or anti-arythmic properties. These new derivatives have the structural formula ##SPC1##Wherein X signifies ##SPC2##And the phenyl nucleus I may be mono-, di- or trisubstituted by alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, alkoxy, alkenyloxy, phenyl, halogen or the radical --NR.sub.1 R.sub.2, in which R.sub.1 stands for alkyl or acyl and R.sub.2 for hydrogen or alkyl, together with their aldehyde condensation products and their acid addition salts.

摘要翻译： 本发明涉及1-苯氧基-3-氨基丙烷-2-醇的药理学有价值的新衍生物及其生产方法。 1-苯氧基-3-氨基 - 丙烷-2-醇的新衍生物适用于治疗和预防心脏疾病。 一些具有显着的β-去肾上腺素或抗-Arcional性质。 这些新衍生物具有结构式X表示，而苯基核I可以被烷基，烯基，炔基，环烷基，环烯基，烷氧基，烯氧基，苯基，卤素或基团-NR1R2单，二或三取代，其中 R1代表烷基或酰基，R2代表氢或烷基，以及它们的醛缩合产物及其酸加成盐。

公开(公告)号：US4785010A

公开(公告)日：1988-11-15

申请号：US797210

申请日：1985-11-12

申请人： Gerhard Zoller ,  Rudi Beyerle ,  Ursula Schindler ,  Rolf-Eberhard Nitz ,  Piero A. Martorana

发明人： Gerhard Zoller ,  Rudi Beyerle ,  Ursula Schindler ,  Rolf-Eberhard Nitz ,  Piero A. Martorana

IPC分类号： C07D207/32 ,  C07D207/335 ,  C07D209/48 ,  C07D401/12 ,  C07D403/06 ,  C07D403/14 ,  C07D417/06 ,  C07D471/04

CPC分类号： C07D207/335 ,  C07D209/48 ,  C07D401/12 ,  C07D403/06 ,  C07D403/14 ,  C07D417/06 ,  C07D471/04

摘要： 2-(Aminoalkyl)-pyrrole derivatives of the formula ##STR1## wherein R denotes hydrogen, alkyl or phenyl, R.sup.1 denotes, for example, hydrogen, alkyl, alkoxy-carbonyl, aryl, substituted aryl or heteroaryl, R.sup.2 and R.sup.3 denote, for example, hydrogen, alkyl, alkanoyl, arylcarbonyl, heteroarylcarbonyl or arylenedicarbonyl and n denotes 1, 2 or 3, and their acid addition salts, are used as pharmacological active compounds for combating cerebral aging processes.

摘要翻译： 其中R表示氢，烷基或苯基，R 1表示例如氢，烷基，烷氧基 - 羰基，芳基，取代的芳基或杂芳基，R2和R3表示用于 例如，氢，烷基，烷酰基，芳基羰基，杂芳基羰基或芳基二羰基，n表示1,2或3，并且它们的酸加成盐用作用于对抗脑衰老过程的药理活性化合物。

公开(公告)号：US4666902A

公开(公告)日：1987-05-19

申请号：US618526

申请日：1984-06-08

申请人： Gerhard Zoller ,  Rudi Beyerle ,  Melitta Just ,  Piero Martorana ,  Helmut Bohn ,  Rolf-Eberhard Nitz

发明人： Gerhard Zoller ,  Rudi Beyerle ,  Melitta Just ,  Piero Martorana ,  Helmut Bohn ,  Rolf-Eberhard Nitz

IPC分类号： C07C51/00 ,  C07C59/90 ,  C07D237/04 ,  C07D307/33 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D413/12 ,  C07D521/00 ,  C07D237/02 ,  A61K31/50

CPC分类号： C07D307/33 ,  C07C51/00 ,  C07C59/90 ,  C07D231/12 ,  C07D233/56 ,  C07D237/04 ,  C07D249/08 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D413/12

摘要： Tetrahydropyridazinones of the formula I ##STR1## wherein R denotes an optionally substituted carbocyclic or heterocyclic radical, R.sup.1 denotes hydrogen; alkyl; aralkyl, which is optionally substituted in the aryl part; or acyl, and R.sup.2 denotes hydrogen; alkyl, which can optionally be substituted; or optionally substituted phenyl; and their acid addition compounds, if these can be prepared.The tetrahydropyridazinone derivatives of the formula I according to the invention and their physiologically acceptable salts exhibit useful pharmacological actions.

摘要翻译： 式I的四氢哒嗪酮（I）其中R表示任选取代的碳环或杂环基，R 1表示氢; 烷基; 芳烷基，其任选在芳基部分被取代; 或酰基，并且R 2表示氢; 烷基，其可任选被取代; 或任选取代的苯基; 和它们的酸加成化合物，如果可以制备它们。 根据本发明的式I的四氢哒嗪酮衍生物及其生理学上可接受的盐表现出有用的药理作用。