公开(公告)号：US4051249A

公开(公告)日：1977-09-27

申请号：US650291

申请日：1976-01-19

申请人： Michel Hardy ,  Daniel Humbert

发明人： Michel Hardy ,  Daniel Humbert

IPC分类号： A61K31/426 ,  C07D277/24 ,  C07D277/56

CPC分类号： C07D277/56 ,  C07D277/24

摘要： Non-toxic, pharmaceutically acceptable acid addition salts of a compound of the formula ##STR1## wherein R is an alkyl of 2 to 12 carbon atoms and R' is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms and acyl of an organic carboxylic acid of 1 to 12 carbon atoms having antilipolytic activity and a very prolonged vasodilatatory activity.

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：US4100291A

公开(公告)日：1978-07-11

申请号：US791927

申请日：1977-04-28

申请人： Francois Clemence ,  Daniel Humbert

发明人： Francois Clemence ,  Daniel Humbert

IPC分类号： C07D405/14 ,  A61K31/335 ,  A61K31/4439 ,  A61P9/12 ,  C07D319/20 ,  C07D405/12

CPC分类号： C07D319/20

摘要： Novel 1,4-benzodioxanes of the formula ##STR1## wherein R' is selected from the group consisting of hydrogen, alkoxy of 1 to 5 carbon atoms, chlorine, bromine and fluorine, R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms and Y and Z are hydrogen or together form a double bond in the form of their racemic mixtures or optically active isomers and their non-toxic, pharmaceutically acceptable acid addition salts having antihypertensive activity and a novel process and novel intermediates for their preparation.

摘要翻译： 式I'的新型1,4-苯并二氧恶烷其中R'选自氢，1至5个碳原子的烷氧基，氯，溴和氟，R 1和R 2分别选自 的氢和1至5个碳原子的烷基，Y和Z是氢或一起形成其外消旋混合物或光学活性异构体形式的双键及其具有抗高血压活性的无毒的药学上可接受的酸加成盐和新颖的 工艺和新型中间体的制备。

公开(公告)号：US4078076A

公开(公告)日：1978-03-07

申请号：US690010

申请日：1976-05-26

申请人： Francois Clemence ,  Daniel Humbert ,  Robert Fournex

发明人： Francois Clemence ,  Daniel Humbert ,  Robert Fournex

IPC分类号： C07D309/04 ,  C07D309/06 ,  A61K31/35 ,  C07D309/22

CPC分类号： C07D309/04 ,  C07D309/06

摘要： Novel pyranic derivatives of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and cations of alkali metals, alkaline earth metals, aluminum, amines and ammonium R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms and X is selected from the group consisting of hydrogen, chlorine and bromine having hypolipemic activity and reducing the level of total lipids in plasma.

摘要翻译： 其中R选自氢，1至6个碳原子的烷基和碱金属，碱土金属，铝，胺和铵的阳离子的新颖的吡喃衍生物，其中R 1和R 2分别选自 由氢和1-4个碳原子的烷基组成的组，X选自具有降血脂活性的氢，氯和溴，并降低血浆中总脂质的含量。

公开(公告)号：US4988692A

公开(公告)日：1991-01-29

申请号：US457237

申请日：1989-12-27

申请人： Jean-Claude Gasc ,  Daniel Humbert

发明人： Jean-Claude Gasc ,  Daniel Humbert

IPC分类号： A61K31/55 ,  A61P3/04 ,  A61P25/18 ,  A61P43/00 ,  C07D243/12 ,  C07D403/12

CPC分类号： C07D403/12 ,  C07D243/12

摘要： A compound in all possible isomeric forms and mixtures thereof of the formula ##STR1## wherein X and X' are individually selected from the group consisting of hydrogen, halogen, cyano, --NO.sub.2, --CF.sub.3 and alkyl and alkoxy of 1 to 8 carbon atoms, R is hydrogen or alkyl of 1 to 8 carbon atoms and Ar is selected from the group consisting of an unsubstituted or substituted aryl of 6 to 14 carbon atoms, an unsubstituted or substituted aromatic heterocyclic or a heterocyclic united with an unsubstituted or substituted aryl having cholecystokinine antagonistic activity.

摘要翻译： 具有式I的所有可能的异构体形式的化合物及其混合物，其中X和X'分别选自氢，卤素，氰基，-NO 2，-CF 3和1至8碳的烷基和烷氧基 原子，R为氢或1至8个碳原子的烷基，Ar选自未取代或取代的6至14个碳原子的芳基，未取代或取代的芳族杂环或杂环与未取代或取代的芳基 具有胆囊收缩素拮抗作用。

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：US4281012A

公开(公告)日：1981-07-28

申请号：US034432

申请日：1979-04-30

申请人： Daniel Humbert ,  Francois Clemence ,  Michele Dagnaux

发明人： Daniel Humbert ,  Francois Clemence ,  Michele Dagnaux

IPC分类号： A61K31/335 ,  A61K31/357 ,  A61P3/04 ,  A61P9/00 ,  C07C39/17 ,  C07C39/28 ,  C07C39/367 ,  C07C39/373 ,  C07C39/42 ,  C07C41/30 ,  C07C43/23 ,  C07C45/46 ,  C07C49/83 ,  C07C49/84 ,  C07D319/08

CPC分类号： C07D319/08 ,  C07C39/17 ,  C07C39/28 ,  C07C39/367 ,  C07C39/373 ,  C07C39/42 ,  C07C41/30 ,  C07C45/46 ,  C07C49/83 ,  C07C49/84 ,  C07C2101/14

摘要： Novel racemates and optically active isomers and mixtures of isomers of [4H]-1,3-benzodioxin-2-carboxylic acid compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, dialkylamino alkyl with alkyls of 1 to 5 carbon atoms, alkali metal, alkaline earth metal, aluminum, --NH.sub.4, non-toxic pharmaceutically acceptable amines, 2,3-dihydroxypropanyl and (2,2-dimethyl-1,3-dioxolan-4-yl)-methyl, R.sub.2 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, R.sub.3 and R.sub.6 are individually selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, ethenyl and cyclohexyl and taken together with the carbon atom to which they are attached form cyclohexyl, R.sub.5 is selected from the group consisting of hydrogen and halogen or R.sub.1 and R.sub.2 have the above definitions, R.sub.6 is ##STR2## R.sub.4 and R.sub.5 are individually selected from the group consisting of hydrogen, halogen, --CF.sub.3, cyclohexyl, alkoxy of 1 to 3 carbon atoms, alkyl of 1 to 3 carbon atoms and p-chlorophenoxy and R.sub.3 is selected from the group consisting of 2-propenyl, ethenyl, cyclohexyl, benzyl, hydrogen and alkyl of 1 to 5 carbon atoms with the proviso that when R.sub.3 is alkyl, at least one of R.sub.4 and R.sub.5 is no hydrogen or halogen and when R.sub.3 is hydrogen, at least one of R.sub.4 and R.sub.5 is not hydrogen, halogen or --CF.sub.3 and the non-toxic, pharmaceutically acceptable acid addition salts thereof when R.sub.1 is dialkylaminoalkyl which have a marked hypolipemiant activity and reduces the plasmatic level of lipids, triglycerides and cholestrol and their preparation.

摘要翻译： 新颖的外消旋物和光学活性异构体以及式[IMAGE] I的[4H] -1,3-苯并二恶英-2-羧酸化合物的异构体的混合物，其中R 1选自氢，1至5个碳的烷基 原子，具有1至5个碳原子的烷基的二烷基氨基烷基，碱金属，碱土金属，铝，-NH 4，无毒的药学上可接受的胺，2,3-二羟基丙酰基和（2,2-二甲基-1,3-二氧戊环） -4-基） - 甲基，R 2选自氢和1至5个碳原子的烷基，R 3和R 6分别选自氢，1至6个碳原子的烷基，乙烯基和环己基 并且与它们所连接的碳原子一起形成环己基，R 5选自氢和卤素，或者R 1和R 2具有上述定义，R 6和R 5各自独立地选自 的氢，卤素，-CF 3，环己基，1〜3个碳原子的烷氧基 在原子上具有1至3个碳原子的烷基和对氯苯氧基，R3选自2-丙烯基，乙烯基，环己基，苄基，氢和1至5个碳原子的烷基，条件是当R3为烷基 ，R 4和R 5中的至少一个不是氢或卤素，并且当R 3是氢时，当R 1是二烷基氨基烷基时，R 4和R 5中的至少一个不是氢，卤素或-CF 3及其无毒的药学上可接受的酸加成盐 其具有显着的降胆固醇活性并降低脂质，甘油三酯和胆甾醇的血浆水平及其制备。

公开(公告)号：US3971798A

公开(公告)日：1976-07-27

申请号：US485244

申请日：1974-07-02

申请人： Daniel Humbert ,  Roger Ratouis

发明人： Daniel Humbert ,  Roger Ratouis

IPC分类号： C07D213/30 ,  C07D213/24

CPC分类号： C07D213/30

摘要： There are provided 2-(p-chlorophenoxy) 2,2-dimethylacetate of /6'-(N-methylaminocarbonyloxymethyl) 2'-pyridyl/ methyl and its acid addition salts which have pharmacological properties particularly for regularizing metabolism, normalizing coagulation factors, combatting arteriosclerosis, chronic veinous insufficiencies and arterial hypertension. Also provided is a process for preparation of the compounds.

摘要翻译： 提供了具有特别用于规则化代谢，归一化凝血因子，对抗的药理学特性的2-（对氯苯氧基）2,2-二甲基乙酸酯/ 6' - （N-甲基氨基羰氧基甲基）2'-吡啶基/甲基及其酸加成盐 动脉硬化，慢性静脉功能不全和动脉高压。 还提供了制备化合物的方法。

公开(公告)号：US3957809A

公开(公告)日：1976-05-18

申请号：US495556

申请日：1974-08-08

申请人： Michel Hardy ,  Daniel Humbert

发明人： Michel Hardy ,  Daniel Humbert

IPC分类号： A61K31/425 ,  C07D277/24 ,  C07D277/56

CPC分类号： A61K31/425 ,  C07D277/24 ,  C07D277/56 ,  Y10S514/929

摘要： Novel thiazole derivatives of the formula ##EQU1## wherein R is alkyl of 2 to 12 carbon atoms and R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms and acyl of an organic carboxylic acid of 1 to 12 carbon atoms having hypolipemiant activity with a very prolonged vasodilatatory activity and their preparation.

公开(公告)号：US5064853A

公开(公告)日：1991-11-12

申请号：US478479

申请日：1990-02-12

申请人： Jean-Claude Gasc ,  Daniel Humbert ,  Mario Vekens

发明人： Jean-Claude Gasc ,  Daniel Humbert ,  Mario Vekens

IPC分类号： A61K31/00 ,  A61K31/195 ,  A61K31/198 ,  A61K31/225 ,  A61K31/403 ,  A61K31/404 ,  A61K31/405 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/47 ,  A61K31/495 ,  A61P1/00 ,  A61P25/00 ,  C07C233/45 ,  C07C235/12 ,  C07C237/22 ,  C07C253/16 ,  C07C255/27 ,  C07D209/42 ,  C07D211/60 ,  C07D213/82 ,  C07D215/54 ,  C07D401/12 ,  C07D417/12

CPC分类号： C07D213/82 ,  C07C237/22 ,  C07D209/42 ,  C07D211/60 ,  C07D215/54 ,  C07D401/12 ,  C07C2103/32

摘要： All possible isomeric forms and mixtures thereof of compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of indolyl, pyridyl, piperidinyl, quinolyl, thiazolyl and aryl of 6 to 14 carbon atoms and aralkyl of 7 to 18 carbon atoms with the latter two being unsubstituted or substituted with at least one member of the group consisting of halogen, alkyl and alkoxy of 1 to 8 carbon atoms, dialkylamino with alkyls of 1 to 8 carbon atoms, --CF.sub.3, --CN and --NO.sub.2, R.sub.2 is selected from the group consisting of ##STR2## Ar' are selected from the group consisting of pyridyl, indolyl, thiazolyl and aryl of 6 to 14 carbon atoms with the latter and the phenyl ring of b) being substituted or substrituted with at least one member of the group consisting of halogen, alkyl and alkoxy of 1 to 8 carbon atoms, dialkylamino with alkyls of 1 to 8 carbon atoms, --CF.sub.3, --CN and --NO.sub.2 and R.sub.3 is hydrogen or R.sub.2 and R.sub.3 together with the nitrogen to which they are attached form a 5 to 7 member hydrocarbyl ring optionally containing an oxygen or a second nitrogen unsubstituted or substituted with at least one member of the group consisting of alkyl of 1 to 8 carbon atoms, aryl of 6 to 14 carbon atoms and ##STR3## Ar and Ar' having the above definitions and R.sub.4 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, ##STR4## and aralkyl of 7 18 carbon atoms unsubstituted or substituted with at least one member of the group consisting of halogen, alkyl and alkoxy of 1 to 8 carbon atoms, dialkylamino with alkyls of 1 to 8 carbon atoms, --CF.sub.3, --CN and --NO.sub.2, Alk.sub.1 is an alkylene of 2 to 8 carbon atoms and alk.sub.2 and Alk.sub.3 are individually alkyl of 1 to 8 carbon atoms or cycloalkyl of 3 to 8 carbon atoms having cholecystokinin agonistic or antagonistic activity.

摘要翻译： 其中R 1选自吲哚基，吡啶基，哌啶基，喹啉基，噻唑基和6至14个碳原子的芳基和7至18个碳原子的芳烷基的所有可能的异构体形式及其混合物 后两者是未取代的或被至少一个由1至8个碳原子的烷基和烷氧基组成的组中的至少一个取代，二烷基氨基与1至8个碳原子的烷基，-CF 3，-CN和-NO 2，R 2 （a）（b）Ar'选自吡啶基，吲哚基，噻唑基和6至14个碳原子的芳基，后者为苯基，b为苯环 ）被至少一个由1至8个碳原子的烷基和烷氧基组成的组中的至少一个取代或取代，二烷基氨基与1至8个碳原子的烷基，-CF 3，-CN和-NO 2，R 3是氢或 R2和R3与它们所连接的氮一起形成5 至7元烃基环，任选地含有氧或未被取代或被至少一个由1至8个碳原子的烷基取代的第二个氮，或6-14个碳原子的芳基和具有 上述定义和R 4选自氢，1至8个碳原子的烷基，3至8个碳原子的环烷基，未取代的或未被至少一个成员取代的7-18个碳原子的芳烷基 由1至8个碳原子的卤素，烷基和烷氧基组成的基团，具有1至8个碳原子的烷基的二烷基氨基，-CF 3，-CN和-NO 2，Alk 1是2至8个碳原子的亚烷基，alk 2和Alk 3分别 具有1至8个碳原子的烷基或具有缩胆囊素激动或拮抗活性的3至8个碳原子的环烷基。