公开(公告)号：EP0223598B1

公开(公告)日：1991-06-12

申请号：EP86309004.9

申请日：1986-11-18

申请人： FISONS plc

发明人： Dixon, John ,  Ince, Francis ,  Springthorpe, Brian

IPC分类号： C07C215/52 ,  C07D213/38 ,  C07C317/02 ,  C07C409/44 ,  A61K31/135 ,  A61K31/44

CPC分类号： C07C323/25 ,  C07D213/38 ,  Y10S514/821 ,  Y10S514/822 ,  Y10S514/824

公开(公告)号：EP0375668A3

公开(公告)日：1990-10-17

申请号：EP90200019.9

申请日：1984-10-17

申请人： FISONS plc

发明人： Dixon, John ,  Ince, Francis ,  Tinker, Alan Charles

IPC分类号： C07C215/52 ,  A61K31/135 ,  C07C323/25 ,  C07C217/16 ,  C07C275/28 ,  A61K31/17 ,  C07C233/40 ,  A61K31/16 ,  C07C237/06 ,  C07C229/14 ,  A61K31/195

CPC分类号： C07D215/227 ,  C07C43/174 ,  C07C43/23 ,  C07C45/515 ,  C07C65/24 ,  C07C215/52 ,  C07C215/80 ,  C07C217/10 ,  C07C217/16 ,  C07C229/14 ,  C07C233/13 ,  C07C233/40 ,  C07C237/06 ,  C07C275/28 ,  C07C311/08 ,  C07C317/28 ,  C07C323/25 ,  C07C2601/12 ,  C07C2601/14 ,  C07C2602/08 ,  C07D215/26 ,  C07D263/14 ,  C07D319/08 ,  C07C47/575

摘要： Compounds of formula I,
in which R₁ represents OH, NR₁₁R₂₁, CH₂R₁₂, or fluorine,
W represents a single bond, 1,2-,1,3- or 1,4-­phenylene; a -CH=CH-group or a 1,4-cyclohexanediyl group;
X represents NH, 0, S, SO₂, CO, CH₂, CONH or -COO;
Y represents inter alia (CH₂) q , CO, CS or SO₂
Z represents a single bond, NR₁₉, CH₂, 0, CO, S or SO₂,
and the other terms are as defined in the specification,
and pharmaceutically acceptable derivatives thereof,
possess useful pharmacological activity.

公开(公告)号：EP0289070A1

公开(公告)日：1988-11-02

申请号：EP88200648.9

申请日：1988-04-06

申请人： DUPHAR INTERNATIONAL RESEARCH B.V

发明人： Van Wijngaarden, Ineke ,  Den Hartog, Jacobus A. J. ,  Tulp, Martinus T. M. ,  Lobbezoo, Marinus W.

IPC分类号： C07C215/52 ,  C07C215/60 ,  C07C225/00 ,  C07C237/20 ,  C07D207/335 ,  C07D231/12 ,  A61K31/135 ,  A61K31/16 ,  A61K31/40 ,  A61K31/415

CPC分类号： C07D231/12

摘要： The invention relates to a group of tertiary arylethyl amine derivatives having opiate-antagonistic activity. The compounds have the general formula 1
wherein

R 1 is hydrogen, an optionally esterified hydroxyl group or mercapto group, a group -NHRs or -CONHR 9 , wherein R s is hydrogen, alkyl having 1-6 C-atoms or alkylcarbonyl having 1-7 C-atoms;
R 2 is hydrogen or, when R 1 is hydrogen, one of the other meanings of Ri, or
R 1 and R 2 together with the 2 carbon atoms of the benzene ring constitute a heterocyclic group which consists of five or six ring atoms and which comprises a group -NH-and, optionally may comprise an oxygen atom, sulphur atom or nitrogen atom as a second hetero atom;
R 3 is hydrogen, alkyl, alkoxy or alkylthio having 1-4 C-atoms, amino, mono-or dialkylamino having 1-4 C-atoms per alkyl group, hydroxyalkyl, alkyl-, alkylamino-or alkoxycarbonyl having 1-4 C-atoms in the alkyl group, nitro, cyano, halogen, trifluoromethyl, trifluoromethoxy, alkylsulphonyl having 1-4 C-atoms, or aminosulphonyl;
m has the value 1, 2 or 3;
R 4 is hydrogen, alkyl or alkoxy having 1-3 C-atoms, or hydroxyl;
R s is hydrogen; alkyl, phenylalkyl, hydroxyalkyl, methoxyalkyl, alkylcarbonyl, alkoxycarbonyl or alkylaminocarbonyl having 1-6 C-atoms in the optionally branched alkyl group;
R 6 is straight or branched alkyl, alkenyl or cycloalkylalkyl or cycloalkyl, having at most 8 C-atoms;
Y is a group R 7 -X-R 8 , wherein R 7 is a straight or branched alkylene chain having 3-8 C-atoms with at least 3 C-atoms between the nitrogen atom and group X; X is the carbonyl group or ketalised carbonyl group, or the group CHOH, CHC 6 H 5 , CH 2 , -CONH-or -CO-NCH 3 or an oxygen atom or sulphur atom; and R 8 is an alkyl group, cycloalkyl group or cycloalkylalkyl group having at most 10 C-atoms a phenyl group or phenylalkyl group having 1-4 C-atoms in the alkyl group, which groups Rs can be substituted with one or more groups R 3 ; or Y is a group of the formula 2a-2e

wherein R 10 may have the meanings given for R 3 .

摘要翻译： 本发明涉及具有阿片拮抗作用的一组叔芳基乙基胺衍生物。 该化合物具有通式1 其中R 1是氢，任意酯化的羟基或巯基，-NHR 9或-CONHR 9基团，其中R 9是氢，具有1-6个C原子的烷基或具有1- 7个C原子; R 2为氢或R 1为氢时，R 1，R 1和R 2与苯环的2个碳原子的其它含义之一构成由5或6个环原子组成的杂环基， NH-，并且任选地可以包含氧原子，硫原子或氮原子作为第二杂原子; R3是氢，烷基，烷氧基或具有1-4个C原子的烷硫基，氨基，每个烷基具有1-4个C原子的单或二烷基氨基，具有1-4个C原子的羟烷基，烷基 - ，烷基氨基或烷氧基羰基 在烷基中，硝基，氰基，卤素，三氟甲基，三氟甲氧基，具有1-4个C原子的烷基磺酰基，或氨基磺酰基; m的值为1,2或3; R4是氢，具有1-3个C原子的烷基或烷氧基，或羟基; R5是氢; 烷基，苯基烷基，羟基烷基，甲氧基烷基，烷基羰基，烷氧基羰基或具有1-6个C原子的烷基氨基羰基; R6是具有至多8个C原子的直链或支链烷基，烯基或环烷基烷基或环烷基; Y是R7-X-R8基团，其中R7是在氮原子和基团X之间具有3-8个碳原子和至少3个C原子的直链或支链亚烷基链; X是羰基或缩酮化羰基，或CHOH，CHC6H5，CH2，-CONH-或-CO-NCH3基团或氧原子或硫原子; R8是烷基中具有至多10个碳原子的烷基，环烷基或环烷基烷基，该烷基中具有1-4个C原子的苯基或苯基烷基，该基团R8可被一个或多个R 3基团取代; 或Y是式2a-2e 的基团，其中R 10可具有R3给出的含义。 一个

公开(公告)号：EP0187019A2

公开(公告)日：1986-07-09

申请号：EP85309216.1

申请日：1985-12-18

申请人： ELI LILLY AND COMPANY

发明人： Massey, Eddie Herman

IPC分类号： C07C215/52 ,  C07C59/01

CPC分类号： C07C215/54 ,  C07C59/06 ,  C07C59/10 ,  C07C59/105 ,  C07C59/255 ,  C07C59/285

摘要： Certain hydroxyalkanoic or alkandioic acid salts of dobutamine having desirable water solubility are useful in preparing intravenous solutions for treatment of cardiogenic shock.

摘要翻译： 具有所需水溶性的多巴酚丁胺的某些羟基链烷酸或链烷二酸盐可用于制备用于治疗心源性休克的静脉内溶液。