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40 条记录 (耗时 0.021 秒)

    Novel derivatives of 2-(4-quinolinylamino)-5-fluoro-benzoic acids
    11.
    发明授权
    Novel derivatives of 2-(4-quinolinylamino)-5-fluoro-benzoic acids 失效
    2-（4-喹啉基氨基）-5-氟 - 苯甲酸的新衍生物

    公开(公告)号：US4233305A

    公开(公告)日：1980-11-11

    申请号：US966964

    申请日：1978-12-06

    申请人： Andre Allais ,  Jean Meier ,  Roger Deraedt

    发明人： Andre Allais ,  Jean Meier ,  Roger Deraedt

    IPC分类号： A61K31/47 ,  A61K31/495 ,  A61P25/04 ,  A61P29/02 ,  C07D215/44 ,  C07D401/12 ,  C07D405/12

    CPC分类号： C07D215/44

    摘要： Derivatives of 2-(4-quinolinylamino)-5-fluorobenzoic acid compounds of the formula ##STR1## wherein X is selected from the group consisting of chlorine and --CF.sub.3 in the 7- or 8-position and R is selected from the group consisting of hydrogen, an esterifying group, alkali metals, alkaline earth metals, ammonium and non-toxic, pharmaceutically acceptable organic amines and their non-toxic, pharmaceutically acceptable acid addition salts having remarkable analgesic properties and their preparation.

    摘要翻译： 式（I）的2-（4-喹啉基氨基）-5-氟苯甲酸化合物的衍生物，其中X选自7-或8-位的氯和-CF 3，R选自 由氢，酯化基团，碱金属，碱土金属，铵和无毒的药学上可接受的有机胺及其无毒的药学上可接受的酸加成盐组成，具有显着的镇痛特性及其制备。

    Steroids
    14.
    发明授权
    Steroids 失效
    新型类固醇

    公开(公告)号：US4395408A

    公开(公告)日：1983-07-26

    申请号：US292794

    申请日：1981-08-14

    申请人： Vesperto Torelli ,  Roger Deraedt ,  Lucien Nedelec

    发明人： Vesperto Torelli ,  Roger Deraedt ,  Lucien Nedelec

    IPC分类号： A61K31/56 ,  A61K31/57 ,  A61P35/00 ,  A61P37/00 ,  A61P37/04 ,  C07J13/00 ,  C07J41/00 ,  C07J5/00 ,  A01N45/00 ,  C07C117/00

    CPC分类号： C07J41/0027 ,  C07J13/007 ,  C07J41/0005 ,  Y10S514/885

    摘要： Novel 3-amino-steroids of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and methyl, W is selected from the group consisting of hydrogen and --OH and taken together with x forms ethylidene, X is selected from the group consisting of ethyl, ##STR2## and taken together with W forms ethylidene and the wavy lines signify that the substituents are in the .alpha. or .beta.-position with the proviso that when R.sub.1 is methyl and X is ethyl, ##STR3## W is --OH and their non-toxic, pharmaceutically acceptable acid addition salts and their preparation and intermediates therefore capable of stimulating immunitary activity.

    摘要翻译： 式（Ⅰ）的新型3-氨基类固醇，其中R 1选自氢和甲基，W选自氢和-OH，并与x一起形成亚乙基，X选自 由乙基组成的基团与W一起形成亚乙基，波浪线表示取代基在α或β-位，条件是当R 1是甲基且X是乙基时，W是 -OH及其无毒的药学上可接受的酸加成盐及其制备和中间体因此能够刺激免疫活性。

    Novel .DELTA..sup.4 -pregnenes
    16.
    发明授权
    Novel .DELTA..sup.4 -pregnenes 失效
    新型DELTA 4-孕烯

    公开(公告)号：US4189477A

    公开(公告)日：1980-02-19

    申请号：US903600

    申请日：1978-05-08

    申请人： Lucien Nedelec ,  Andre Pierdet ,  Roger Deraedt

    发明人： Lucien Nedelec ,  Andre Pierdet ,  Roger Deraedt

    IPC分类号： C07J5/00 ,  A61K31/57 ,  A61K31/573 ,  A61P29/00 ,  A61P37/08 ,  C07J41/00 ,  A61K31/56 ,  C07J1/00

    CPC分类号： C07J41/0016

    摘要： 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.

    摘要翻译： 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。

    Analgesic compositions and method
    17.
    发明授权
    Analgesic compositions and method 失效
    止痛成分及方法

    公开(公告)号：US4760070A

    公开(公告)日：1988-07-26

    申请号：US930355

    申请日：1986-11-12

    申请人： Francoise Delevallee ,  Roger Deraedt

    发明人： Francoise Delevallee ,  Roger Deraedt

    IPC分类号： A61K31/485 ,  A61K31/52 ,  A61K31/535 ,  A61P25/04 ,  A61K31/44

    CPC分类号： A61K31/52 ,  A61K31/535

    摘要： An improved method of treating pain in warm-blooded animals, including humans, by administering a central analgesic and adenine simultaneously or successively at times of a few seconds up to two hours and novel analgesic compositions comprising an analgesically effective amount of a central analgesic and adenine free of side effects.

    摘要翻译： 一种治疗温血动物（包括人）疼痛的改进方法，通过在几秒至两小时的时间内同时或连续施用中枢镇痛剂和腺嘌呤，以及包含镇痛有效量的中枢镇痛药和腺嘌呤的新型止痛组合物 无副作用。

    Novel 11 beta-substituted-19-nor-steroids
    18.
    发明授权
    Novel 11 beta-substituted-19-nor-steroids 失效
    新型11型β-取代-19-去甲甾类

    公开(公告)号：US4634696A

    公开(公告)日：1987-01-06

    申请号：US760703

    申请日：1985-07-30

    申请人： Jean-Georges Teutsch ,  Vesperto Torelli ,  Roger Deraedt ,  Daniel Philibert

    发明人： Jean-Georges Teutsch ,  Vesperto Torelli ,  Roger Deraedt ,  Daniel Philibert

    IPC分类号： A61K31/565 ,  A61P5/38 ,  C07J1/00 ,  C07J21/00 ,  C07J41/00 ,  C07J43/00 ,  C07J71/00 ,  A61K31/56

    CPC分类号： C07J1/0088 ,  C07J1/0059 ,  C07J1/007 ,  C07J21/006 ,  C07J41/0077 ,  C07J41/0083 ,  C07J41/0094 ,  C07J43/003 ,  C07J71/0063

    摘要： Novel 19-nor-steroids of the formula ##STR1## wherein R.sub.1 is an organic group of 1 to 18 carbon atoms optionally containing at least one heteroatom with the atom immediately adjacent the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is the remainder of a pentagonal or hexagonal ring optionally substituted and optionally containing one unsaturated--bond, the A and B rings are selected from the group consisting of ##STR2## R' and R" are individually selected from the group consisting of hydrogen, --CN and alkyl of 1 to 4 carbon atoms with at least one being other than hydrogen, R.sub.x is selected from the group consisting of hydrogen and OR.sub.e, R.sub.e is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl, R.sub.a may be in the E or Z positions as indicated by the wavy line and is selected from the group consisting of ##STR3## and acyloxy, R.sub.a ' and R.sub.a " are alkyl of 1 to 4 carbon atoms or taken together with the nitrogen atom form a heterocycle of 5 to 6 chain members optionally containing another heteroatom with the proviso that when A and B are ##STR4## R.sub.1 contains at least one nitrogen, phosphorus or silicium atom and when A and B are ##STR5## R.sub.1 is not a linear alkyl and their non-toxic, pharmaceutically acceptable acid addition salts having a remarkable antigluococorticoid activity, their preparation and novel intermediates.

    摘要翻译： 式（I）的新型19-去甲甾类化合物，其中R 1是任选地含有至少一个杂原子的碳原子数为1至18的有机基团，紧邻11个碳原子的原子是碳，R2是1的烃 至少8个碳原子，X是任选地被取代且任选地含有一个不饱和键的五边形或六边形环的剩余部分，A和B环选自由下列组成的组：（a） （c）＆lt; IMAGE＆gt;（d）和＆lt; IMAGE＆gt;（e）R'和R“分别选自氢，-CN和1至4个碳原子的烷基，其中至少一个是其它 R x选自氢和ORe，Re选自氢，任选取代的1至6个碳原子的烷基和酰基，R a可以在E或Z位置，如 波浪线，并且选自和酰氧基，Ra'和Ra“是烷基 1至4个碳原子或与氮原子一起形成任选含有另一个杂原子的5至6个链成员的杂环，条件是当A和B为至少一个氮，磷或硅原子时， A和B是，R1不是直链烷基及其无毒的药学上可接受的酸加成盐，具有显着的抗皮质激素活性，其制备和新型中间体。

    Novel 3 .alpha.-amino steroids
    19.
    发明授权
    Novel 3 .alpha.-amino steroids 失效
    新型3α-氨基类固醇

    公开(公告)号：US4424218A

    公开(公告)日：1984-01-03

    申请号：US292791

    申请日：1981-08-14

    申请人： Roger Deraedt ,  Vesperto Torelli ,  Jean Vacher ,  Josette Benzoni

    发明人： Roger Deraedt ,  Vesperto Torelli ,  Jean Vacher ,  Josette Benzoni

    IPC分类号： C07J13/00 ,  C07J41/00 ,  C07J43/00 ,  A01N45/00

    CPC分类号： C07J13/007 ,  C07J41/0005 ,  C07J41/0027 ,  C07J43/003 ,  Y10S514/885

    摘要： A 3-amino-steroid of the formula ##STR1## wherein W is selected from the group consisting of hydrogen and --OH and taken together with X is ethylidene, X is selected from the group consisting of ethyl, ##STR2## the wavy line indicates the substituent has the .alpha.- and .beta.-position, R.sub.1 is selected from the group consisting of hydrogen and --CH.sub.3, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and hydroxyalkyl of 2 to 5 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, hydroxyalkyl of 2 to 5 carbon atoms, acyl of organic acid of 2 to 8 carbon atoms, alkoxycarbonyl of 2 to 8 carbon atoms, acyl of an .alpha.-amino-carboxylic acid and a peptide of 2 to 3 .alpha.-amino-carboxylic acids and their non-toxic, pharmaceutically acceptable acid addition acids with the proviso that R.sub.2 and R.sub.3 are not both hydrogen and (i) when R.sub.1 is methyl, W and R.sub.2 are hydrogen and X is ##STR3## in the case R.sub.3 is not methyl, acetyl or derived from an anminocarboxylic acid, (ii) when R.sub.1 is --CH.sub.3, W is hydrogen, R.sub.2 is --CH.sub.3 and X is ##STR4## in the case R.sub.3 is not methyl or acetyl, (iii) when R.sub.1 is methyl, R.sub.2 and W are hydrogen, X is ##STR5## with the --OH having the (S) configuration and the amino group is in the .alpha.-position in the case R.sub.3 is not methyl (iiii) R.sub.2 and W are hydrogen, X is ##STR6## and the 3-amino is in the .alpha.-position in the case at least one of R.sub.1, R.sub.2 and R.sub.3 is not methyl and (iiiii) R.sub.2 and W are hydrogen, R.sub.1 is methyl, X is ##STR7## with the --OH having the (R) configuration and the 3-amino is in the .alpha.-position in the case R.sub.3 is not ethoxycarbonyl capable of stimulating the defenses of an organism, especially by potentializing the production of IgE (immunoglobulins E) and their preparation.

    摘要翻译： 其中W选自氢和-OH并与X一起并与X一起形成的式（I）的3-氨基类固醇是亚乙基，X选自乙烯基，波浪线 表示取代基具有α-和β-位，R 1选自氢和-CH 3，R 2选自氢，1至5个碳原子的烷基和2至5个碳原子的羟烷基 R 3选自氢，1至5个碳原子的烷基，2至5个碳原子的羟基烷基，2至8个碳原子的有机酸酰基，2至8个碳原子的烷氧基羰基， - 氨基 - 羧酸和2至3个α-氨基 - 羧酸的肽及其无毒的药学上可接受的酸加成酸，条件是R2和R3不同时为氢和（i）当R1为甲基时，W 在R 3不是甲基的情况下，R 2是氢并且X是，乙酰基或 （ii）当R 1为-CH 3时，W为氢，R 2为-CH 3，X为不是甲基或乙酰基的情况下为X，（ⅲ）当R 1为甲基时，R 2和W为 是氢，X是具有（S）构型的-OH，而在R3不是甲基的情况下氨基位于α位置（iiii），R2和W是氢，X是＆lt; IMAGE＆gt;和 在R1，R2和R3中的至少一个不是甲基的情况下，3-氨基是α-位，并且（iiiii）R 2和W是氢，R 1是甲基，X是OH，其中-OH具有 （R）构型，并且在R3不是能够刺激生物体的防御性的乙氧基羰基的情况下，特别是通过潜在地产生IgE（免疫球蛋白E）及其制备，3-氨基是α-位。

    Novel 17 .alpha.-aryl-steroids
    20.
    发明授权
    Novel 17 .alpha.-aryl-steroids 失效
    新型17α-芳基类固醇

    公开(公告)号：US4203981A

    公开(公告)日：1980-05-20

    申请号：US692

    申请日：1979-01-03

    申请人： Andre Pierdet ,  Vesperto Torelli ,  Roger Deraedt

    发明人： Andre Pierdet ,  Vesperto Torelli ,  Roger Deraedt

    IPC分类号： A61K31/565 ,  A61K31/58 ,  A61P29/00 ,  C07J1/00 ,  C07J17/00 ,  C07J33/00 ,  C07J43/00 ,  C07J71/00 ,  A61K31/56

    CPC分类号： C07J43/003 ,  C07J1/0011 ,  C07J1/0033 ,  C07J17/00 ,  C07J33/002 ,  C07J71/0015

    摘要： Novel steroids of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and acyl of an organic carboxylic acid of 1 to 18 carbon atoms, R.sub.2 is selected from the group consisting of optionally substituted aryl of 6 to 12 carbon atoms and optionally substituted heterocyclic selected from the group consisting of furyl, thienyl, pyridyl and pyrimidyl, the optional substituents being selected from the group consisting of hydroxy, alkyl and alkoxy of 1 to 4 carbon atoms, halogens and --CF.sub.3, the dotted line in the A ring indicates an optional .DELTA..sup.1(2) - double bond and A may be oxo and B is hydrogen or A is .DELTA.--OH and B is hydrogen or halogen or A and B form a .DELTA..sup.9(10) - double bond having very good anti-inflammatory activity and their preparation and novel intermediates.

    摘要翻译： 式（Ⅰ）的新型类固醇，其中R 1选自氢和1至18个碳原子的有机羧酸的酰基，R 2选自任选取代的6至12个碳原子的芳基 和任选取代的杂环基，其选自呋喃基，噻吩基，吡啶基和嘧啶基，任选的取代基选自羟基，1至4个碳原子的烷基和烷氧基，卤素和-CF 3， 环表示可选的DELTA 1（2） - 双键，A可以是氧代，B是氢或A是DELTA -OH，B是氢或卤素，或A和B形成具有非常特异的DELTA 9（10） - 双键 良好的抗炎活性及其制备及新型中间体。