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    • 3. 发明授权
    • 4(2-indolyl)2-amino-pentanedioic acids and cholecyostokinin use thereof
    • 4(2-吲哚基)2-氨基 - 戊二酸和其选择性丝氨酸蛋白酶
    • US5064853A
    • 1991-11-12
    • US478479
    • 1990-02-12
    • Jean-Claude GascDaniel HumbertMario Vekens
    • Jean-Claude GascDaniel HumbertMario Vekens
    • A61K31/00A61K31/195A61K31/198A61K31/225A61K31/403A61K31/404A61K31/405A61K31/44A61K31/4406A61K31/4427A61K31/445A61K31/47A61K31/495A61P1/00A61P25/00C07C233/45C07C235/12C07C237/22C07C253/16C07C255/27C07D209/42C07D211/60C07D213/82C07D215/54C07D401/12C07D417/12
    • C07D213/82C07C237/22C07D209/42C07D211/60C07D215/54C07D401/12C07C2103/32
    • 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.
    • 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。
    • 5. 发明授权
    • 2-aryl pyrazolo[4,3-c]cinnolin-3-ones
    • 2-芳基吡唑并[4,3-c]噌啉-3-酮
    • US4591589A
    • 1986-05-27
    • US692030
    • 1985-01-16
    • Jean-Claude GascDaniel HumbertPeter F. Hunt
    • Jean-Claude GascDaniel HumbertPeter F. Hunt
    • C07D487/04A61K31/50C07D487/02
    • C07D487/04
    • 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.
    • 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。
    • 7. 发明授权
    • 1,3-Benzodioxin derivatives
    • 1,3-苯并二恶英衍生物
    • US4294845A
    • 1981-10-13
    • US34431
    • 1979-04-30
    • Daniel HumbertFrancois ClemenceMichele Dagnaux
    • Daniel HumbertFrancois ClemenceMichele Dagnaux
    • A61K31/335A61K31/357A61P3/04A61P9/00C07C39/367C07D319/08
    • C07D319/08C07C39/367
    • Novel racemic mixtures or optically active isomers of 1,3-benzodioxins of the formula ##STR1## wherein R.sub.1 ' is selected from the group consisting of hydrogen, alkali metal, alkaline earth metal, --NH.sub.4, aluminum, non-toxic, pharmaceutically acceptable amines, alkyl of 1 to 5 carbon atoms, 2,3-dihydroxypropanyl, (2,2-dimethyl-1,3-dioxolan-4-yl)methyl and dialkylaminoalkyl with alkyls of 1 to 4 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and phenyl and R.sub.4 and R.sub.5 are individually selected from the group consisting of hydrogen and halogen, and the non-toxic, pharmaceutically acceptable acid addition salts where R.sub.1 ' is dialkylaminoalkyl, with the proviso that R.sub.2 and R.sub.3 are not hydrogen simultaneously having hypolipemic activity and their preparation.
    • 下式的1,3-苯并二恶英的新型外消旋混合物或光学活性异构体其中R1'选自氢,碱金属,碱土金属,-NH4,铝,无毒,药学上可接受的 胺,1至5个碳原子的烷基,2,3-二羟基丙酰基,(2,2-二甲基-1,3-二氧戊环-4-基)甲基和具有1至4个碳原子的烷基的二烷基氨基烷基,R2选自 由氢和1至5个碳原子的烷基组成的组,R3选自氢,1至5个碳原子的烷基和苯基,R4和R5分别选自氢和卤素,和 无毒,药学上可接受的酸加成盐,其中R1'是二烷基氨基烷基,条件是R2和R3不同时具有降血脂活性及其制备。