公开(公告)号：US4588731A

公开(公告)日：1986-05-13

申请号：US747665

申请日：1985-06-21

申请人： Daniel Humbert ,  Jean-Claude Gasc ,  Peter F. Hunt

发明人： Daniel Humbert ,  Jean-Claude Gasc ,  Peter F. Hunt

IPC分类号： C07D215/56 ,  C07D498/04 ,  A61K31/42 ,  C07D215/00 ,  C07D498/02

CPC分类号： C07D215/56

摘要： Novel isoxazoloquinolinones of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, fluorine, chlorine, bromine, alkyl and alkoxy of 1 to 5 carbon atoms, --NO.sub.2 and CF.sub.3 -- and R.sub.1 is phenyl optionally substituted by at least one member selected from the group consisting of halogen and alkyl and alkoxy of 1 to 5 carbon atoms having anxiolytic activity and their preparation and novel intermediates.

摘要翻译： 新的式（I）的异恶唑啉喹啉酮，其中R选自氢，氟，氯，溴，1至5个碳原子的烷基和烷氧基，-NO 2和CF 3 - ，R 1是任选被至少取代的苯基 选自卤素和具有1-5个碳原子的烷基和烷氧基的一个成员具有抗焦虑活性及其制备和新的中间体。

公开(公告)号：US4591589A

公开(公告)日：1986-05-27

申请号：US692030

申请日：1985-01-16

申请人： Jean-Claude Gasc ,  Daniel Humbert ,  Peter F. Hunt

发明人： Jean-Claude Gasc ,  Daniel Humbert ,  Peter F. Hunt

IPC分类号： C07D487/04 ,  A61K31/50 ,  C07D487/02

CPC分类号： C07D487/04

摘要： Novel pyrazolo[4,3-c]cinnolin-3-one derivatives of the formula ##STR1## wherein R may be in the 7- or 8-position and is selected from the group consisting of hydrogen, halogen, alkyl and alkoxy of 1 to 5 carbon atoms, --NO.sub.2 and --CF.sub.3 and R' is hydrogen or R and R' taken together form an alkylenedioxy of 1 to 4 carbon atoms at the 7- or 8-positions and R.sub.1 is selected from the group consisting of phenyl, pyridyl, thiazolyl, dihydrothiazolyl and thienyl, all optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, halogen, mono-, di- and tri- halomethyl and aralkoxy of 7 to 12 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having anxiolytic properties and novel intermediates therefore.

摘要翻译： 新的吡唑并[4,3-c]噌啉-3-酮衍生物，其中R可以在7-或8-位，并且选自氢，卤素，烷基和烷氧基， 1至5个碳原子，-NO 2和-CF 3和R'是氢或R和R'在一起形成在7或8位上具有1至4个碳原子的亚烷基二氧基，并且R 1选自苯基 ，吡啶基，噻唑基，二氢噻唑基和噻吩基，其全部任选被至少一个由1至5个碳原子的烷基和烷氧基组成的组中的一个取代，卤素，7至12个碳原子的一，二和三卤代甲基和芳烷氧基 因此具有抗焦虑性质的原子及其无毒的药学上可接受的酸加成盐。

公开(公告)号：US4450166A

公开(公告)日：1984-05-22

申请号：US386597

申请日：1982-06-09

申请人： Francois Clemence ,  Peter F. Hunt ,  Odile Le Martret ,  Daniel Humbert

发明人： Francois Clemence ,  Peter F. Hunt ,  Odile Le Martret ,  Daniel Humbert

IPC分类号： C07D215/56 ,  C07D417/12 ,  A61K31/47

CPC分类号： C07D417/12 ,  C07D215/56

摘要： Novel N-(4,5-dihydro-thiazol-2-yl)-4-hydroxy-3-quinoline-carboxamides of the formula ##STR1## wherein R is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms and R.sub.1 is selected from the group consisting of hydrogen, halogen, linear alkyl of 1 to 4 carbon atoms, branched alkyl of 3 to 5 carbon atoms, alkoxy of 1 to 4 carbon atoms, CF.sub.3 --, CF.sub.3 O--, CF.sub.3 S-- and CH.sub.3 S-- in the 6- or 7-position and their non-toxic, pharmaceutically acceptable acid addition salts having a strong anxiolytic activity and a remarkable affinity for benzodiapines receptors and their preparation.

摘要翻译： 新的式（I）的N-（4,5-二氢 - 噻唑-2-基）-4-羟基-3-喹啉 - 甲酰胺其中R选自氢和1至4个碳的烷基 原子和R 1选自氢，卤素，1至4个碳原子的直链烷基，3至5个碳原子的支链烷基，1至4个碳原子的烷氧基，CF 3 - ，CF 3 O-，CF 3 S-和CH 3 S - 6-或7-位及其无毒的药学上可接受的酸加成盐，其具有强的抗焦虑活性和对苯并二氮杂受体的显着亲和力及其制备。

公开(公告)号：US4450167A

公开(公告)日：1984-05-22

申请号：US398575

申请日：1982-07-15

申请人： Odile Le Martret ,  Daniel Humbert ,  Peter F. Hunt

发明人： Odile Le Martret ,  Daniel Humbert ,  Peter F. Hunt

IPC分类号： C07D215/48 ,  A61K31/47 ,  A61P25/20 ,  C07D215/54 ,  C07D215/56 ,  C07D401/12

CPC分类号： C07D401/12 ,  C07D215/54 ,  C07D215/56

摘要： Novel 3-quinoline-carboxamides of the formula ##STR1## wherein R is in 6 or 7-position and is selected from the group consisting of hydrogen, halogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, --CF.sub.3, --SCF.sub.3 and CH.sub.3 S--, R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, phenyl and benzyl, R.sub.2 is --NHR.sub.4, R.sub.4 is selected from the group consisting of alkyl of 2 to 6 carbon atoms, substituted aryl of 6 to 10 carbon atoms and substituted heterocycle of an aromatic character of 3 to 5 carbon atoms with the proviso that when R.sub.4 is a mono substituted aryl or heterocycle, the substituent is different from R of the quinoline when it is a halogen and R.sub.3 is selected from the group consisting of hydrogen and --OH and their non-toxic, pharmaceutically acceptable acid addition salts having remarkable anxiolytic properties capable of lessening emotional reactions and diminishing states of psychic tension and their preparation.

摘要翻译： 式（Ⅰ）的新型3-喹啉 - 甲酰胺其中R为6或7位，选自氢，卤素，1至6个碳原子的烷基，3至6个碳原子的环烷基， 1至6个碳原子的烷氧基，-CF 3，-SCF 3和CH 3 S - ，R 1选自氢，1至6个碳原子的烷基，苯基和苄基，R 2是-NHR 4，R 4选自 由2至6个碳原子的烷基，6至10个碳原子的取代的芳基和3至5个碳原子的芳族特征的取代杂环组成，条件是当R4是单取代的芳基或杂环时，取代基不同 当喹啉为卤素时，R 3选自氢和-OH，并且其无毒的药学上可接受的酸加成盐具有显着的抗焦虑性能，能够减轻情绪反应和心理紧张状态的降低， 准备 离子。

公开(公告)号：US4591461A

公开(公告)日：1986-05-27

申请号：US791773

申请日：1985-10-28

申请人： Alain Jouquey ,  Peter F. Hunt

发明人： Alain Jouquey ,  Peter F. Hunt

IPC分类号： C07J1/00 ,  C07C67/00 ,  C07C239/00 ,  C07C253/00 ,  C07C255/31 ,  C07C255/47 ,  C07C271/00 ,  C07J41/00 ,  C07J73/00 ,  C07J75/00 ,  C07C121/46 ,  C07C121/47

CPC分类号： C07J41/0016 ,  C07J73/005 ,  C07C2103/26

摘要： A novel process for the preparation of a 16-imino-17-aza-steroid of the formula ##STR1## wherein A is selected from the group consisting of hydrogen and tritium comprising reacting a compound of the formula ##STR2## wherein A has the above definition and R is an acyl of an organic carboxylic acid of 1 to 8 carbon atoms with an oximation agent to obtain a compound of the formula ##STR3## reacting the latter with an agent to form an acid chloride to obtain a compound of the formula ##STR4## reacting the latter with ammonia to obtain a compound of the formula ##STR5## reacting the latter with an alkali metal hypohalite in the presence of a base to obtain a compound of the formula ##STR6## wherein X is a halogen and reacting the latter with a base to obtain the desired compound and the novel compound of formula I wherein A is tritium and the novel intermediates of formulae III, IV, V and VI.

摘要翻译： 一种用于制备式I的16亚氨基-17-氮杂类固醇的新方法，其中A选自氢和氚，包括使下式化合物II与式 上述定义，R为具有1至8个碳原子的有机羧酸的酰基与肟化剂反应，得到下式化合物，其中后者与试剂反应形成酰氯，得到化合物 IV使后者与氨反应，得到下式的化合物，其中R 1在碱的存在下与碱金属次卤酸盐反应，得到式VI的化合物，其中X为 卤素并使其与碱反应以获得所需化合物和式I的新型化合物，其中A是氚，以及式III，IV，V和VI的新型中间体。

公开(公告)号：US5111196A

公开(公告)日：1992-05-05

申请号：US28737

申请日：1987-03-23

申请人： Peter F. Hunt

发明人： Peter F. Hunt

IPC分类号： G08B5/00 ,  G06F3/147 ,  H01R13/66

CPC分类号： G06F3/147 ,  G09G2380/04

摘要： An independent, stand-alone, battery powered information display module to visually display computer generated, alpha-numeric information on one or more liquid crystal displays. The module has particular application for storing and displaying pricing and related information associated with a shelf item commonly offered for sale in a retail establishment, such as a grocery store, or the like. Pricing information is supplied by a computer to the price display module for storage and eventual display by way of a hand-held, portable data terminal. The portable data terminal is electrically connected to the display module by a multi-terminal connector, whereby electrical contact pins of the connector are aligned for engagement with respective electrical contact strips located at the face of the display module and connected to the memory thereof. A multi-conductor electrical cable extends from the contact pins of the connector to be coupled to the portable data terminal to permit the two-way transfer of information between the memory of the display module and the computer.

公开(公告)号：US4565876A

公开(公告)日：1986-01-21

申请号：US612606

申请日：1984-05-21

申请人： Alain Jouquey ,  Peter F. Hunt

发明人： Alain Jouquey ,  Peter F. Hunt

IPC分类号： C07J1/00 ,  C07C67/00 ,  C07C239/00 ,  C07C253/00 ,  C07C255/31 ,  C07C255/47 ,  C07C271/00 ,  C07J41/00 ,  C07J73/00 ,  C07J75/00 ,  C07D209/56

CPC分类号： C07J41/0016 ,  C07J73/005 ,  C07C2103/26

摘要： A novel process for the preparation of a 16-imino-17-aza-steroid of the formula ##STR1## wherein A is selected from the group consisting of hydrogen and tritium comprising reacting a compound of the formula ##STR2## wherein A has the above definition and R is an acyl of an organic carboxylic acid of 1 to 8 carbon atoms with an oximation agent to obtain a compound of the formula ##STR3## reacting the latter with an agent to form an acid chloride to obtain a compound of the formula ##STR4## reacting the latter with ammonia to obtain a compound of the formula ##STR5## reacting the latter with an alkali metal hypohalite in the presence of a base to obtain a compound of the formula ##STR6## wherein X is a halogen and reacting the latter with a base to obtain the desired compound and the novel compound of formula I wherein A is tritium and the novel intermediates of formulae III, IV, V and VI.

摘要翻译： 一种用于制备式I的16亚氨基-17-氮杂类固醇的新方法，其中A选自氢和氚，包括使下式化合物II与式 上述定义，R为具有1至8个碳原子的有机羧酸的酰基与肟化剂反应，得到下式化合物，其中后者与试剂反应形成酰氯，得到化合物 IV使后者与氨反应，得到下式的化合物，其中R 1在碱的存在下与碱金属次卤酸盐反应，得到式VI的化合物，其中X为 卤素并使其与碱反应以获得所需化合物和式I的新型化合物，其中A是氚，以及式III，IV，V和VI的新型中间体。