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    • 5. 发明授权
    • Indolobenzoxazines
    • 吲哚溴嗪
    • US4318910A
    • 1982-03-09
    • US246169
    • 1981-03-23
    • Lucien NedelecAndre PierdetClaude Dumont
    • Lucien NedelecAndre PierdetClaude Dumont
    • A61K31/535A61P9/12A61P25/00A61P43/00C07D209/90C07D498/06A01N43/84
    • C07D209/90
    • Novel indolobenzoxazines of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and optionally substituted aralkyl of 7 to 12 carbon atoms, R.sub.1 is selected from the group consisting of hydrogen, chlorine and bromine, R.sub.2 ' is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 5 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms, alkenyl and alkynyl of 3 to 7 carbon atoms and optionally substituted aralkyl of 7 to 12 carbon atoms and the dotted line between 5 and 5a indicates the optional presence of a double bond and their non-toxic, pharmaceutically acceptable acid addition salts having hypotensive, antihypertensive and dopaminergic agonist properties and a process for their preparation.
    • 式“IMAGE”I'的新型吲哚并恶嗪其中R选自氢,1至5个碳原子的烷基和任选取代的7至12个碳原子的芳烷基,R 1选自氢,氯 和溴,R 2'选自氢,任选取代的1至5个碳原子的烷基,4至7个碳原子的环烷基烷基,3至7个碳原子的链烯基和炔基,以及7-12个碳原子的任选取代的芳烷基 原子和5和5a之间的虚线表示任选存在双键及其无毒的药学上可接受的具有降压,抗高血压和多巴胺能激动剂性质的酸加成盐及其制备方法。
    • 6. 发明授权
    • Novel 17.alpha.-aryl-steroids
    • 新型17α-芳基类固醇
    • US4242335A
    • 1980-12-30
    • US955403
    • 1978-10-27
    • Genevieve AzadianDaniel PhilibertAndre Pierdet
    • Genevieve AzadianDaniel PhilibertAndre Pierdet
    • A61K31/565C07J1/00C07J21/00
    • C07J1/0088C07J21/006
    • Novel 17.alpha.-aryl-steroids of the formula ##STR1## wherein R.sub.1 is alkyl of 1 to 3 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 12 carbon atoms and acyl of an organic carboxylic acid of 1 to 18 carbon atoms, R.sub.3 is aryl of 6 to 12 carbon atoms optionally substituted with at least one substituent selected from the group consisting of --OH, halogen, alkoxy and alkyl of 1 to 4 carbon atoms and --CF.sub.3, the dotted line in the B ring indicating an optional double bond in the 9(10)-position, and A and B are hydrogen and when there is a double bond in the 9(10)-position, A and B form a double bond in the 11(12) position or B is hydrogen and A is an 11.beta.-hydroxy having progestomimetic activity activity without androgenic activity and a process for their preparation and novel intermediates produced therein.
    • 新型17α-芳基 - 类固醇,其中R 1为1至3个碳原子的烷基,R 2选自氢,1至12个碳原子的烷基和有机羧酸的酰基 1至18个碳原子,R3是任选被至少一个选自-OH,卤素,烷氧基和1至4个碳原子的烷基和-CF 3的取代基取代的6至12个碳原子的芳基,虚线在 B环表示9(10)位中任选的双键,A和B是氢,当在9(10)位具有双键时,A和B在11(10) - 位上形成双键, 12)位置或B是氢,A是具有没有雄激素活性的模拟活动活性的11β-羟基,其制备方法和其中产生的新的中间体。
    • 8. 发明授权
    • Novel .DELTA..sup.4 -pregnenes
    • 新型DELTA 4-孕烯
    • US4189477A
    • 1980-02-19
    • US903600
    • 1978-05-08
    • Lucien NedelecAndre PierdetRoger Deraedt
    • Lucien NedelecAndre PierdetRoger Deraedt
    • C07J5/00A61K31/57A61K31/573A61P29/00A61P37/08C07J41/00A61K31/56C07J1/00
    • C07J41/0016
    • Novel .DELTA..sup.4 -pregnenes of the formula ##STR1## wherein X.sub.1 is selected from the group consisting of .dbd.O and ##STR2## Y is selected from the group consisting of hydrogen and halogen, R.sub.1 is selected from the group consisting of hydrogen and acyl of an organic carboxylic acid of 1 to 18 carbon atoms, X.sub.2 is selected from the group consisting of hydrogen and --OH, R in the 16.alpha.- or .beta.-position is selected from the group consisting of hydrogen, --OH and methyl, Z is selected from the group consisting of (1) --OH, (2) alkoxy of 1 to 12 carbon atoms, (3) cycloalkoxy of 3 to 12 carbon atoms, (4) acyloxy of an organic carboxylic acid of 1 to 18 carbon atoms, (5) ##STR3## wherein W is a hydrocarbon of 1 to 12 carbon atoms, (6) ##STR4## wherein R.sub.2 is hydrogen or alkyl of 1 to 12 carbon atoms, (7) ##STR5## wherein R.sub.3 is a hydrocarbon of 1 to 12 carbon atoms and (8) ##STR6## the dotted line in the A ring indicates the optional presence of a double bond in the 1(2)-position and A and B are both hydrogen or A is methyl, chlorine or fluorine while B is hydrogen or A and B may form a double bond in the 6(7)-position with the proviso that if the A ring has a 1(2) double bond, A is hydrogen or fluorine, B is hydrogen, Y is hydrogen or fluorine, X.sub.2 is hydrogen or --OH, R is methyl and Z is not --OH having a very marked antiallergic activity with a reduced anti-inflammatory activity and a process for their preparation.
    • 式(I)其中X1选自= O和Y的新型DELTA 4-孕烯选自氢和卤素,R 1选自氢和酰基 的1至18个碳原子的有机羧酸,X 2选自氢和-OH,16个α-或β-位中的R选自氢,-OH和甲基,Z 选自(1)-OH,(2)1至12个碳原子的烷氧基,(3)3至12个碳原子的环烷氧基,(4)1至18个碳原子的有机羧酸的酰氧基 (5)其中W是1至12个碳原子的烃,(6)其中R 2是氢或1至12个碳原子的烷基,(7)其中R 3是 1至12个碳原子和(8)A环中的虚线表示在1(2)位中任选存在双键,A和B均为氢 基或A是甲基,氯或氟,而B是氢或A和B可以在6(7) - 位上形成双键,条件是如果A环具有1(2)双键,则A是氢 或氟,B是氢,Y是氢或氟,X2是氢或-OH,R是甲基,Z不是-OH,具有非常显着的抗过敏活性,抗炎活性降低及其制备方法。