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    Amine derivatives, processes for their production and pharmaceutical compositions containing them
    1.
    发明公开
    Amine derivatives, processes for their production and pharmaceutical compositions containing them 失效
    胺衍生物，它们的生产和含有它们的药物组合物。

    公开(公告)号：EP0072061A1

    公开(公告)日：1983-02-16

    申请号：EP82200930.4

    申请日：1982-07-22

    申请人： FISONS plc

    发明人： Farmer, John Bates ,  Ince, Francis ,  Brown, Rodney Alan ,  Dixon, John

    IPC分类号： C07C91/28 ,  C07D295/12 ,  C07D223/16 ,  C07D213/38 ,  A61K31/135

    CPC分类号： C07D223/16 ,  C07D213/38 ,  C07D295/13 ,  C07D307/33

    摘要： There are described compounds of formula I,
    in which D, represents a group of formula II,
    where R, and R 5 , or H 3 and R 5 may form a chain -CH 2 CH 2 -, or R 4 and R 5 may form a chain -CH 2 -, or R 3 , R 4 and R 5 are each hydrogen, the remainder of R,, R 3 and R 4 , which may be the same or different, being hydrogen, alkyl or phenyl,
    none, one or two of R 6 , R 7 , R 8 and R, represent hydroxy and the remainder represent hydrogen,

    X represents a chain -(CH 2 ) n -, optionally substituted by hydroxy,
    n is an integer from 1 to 7 inclusive,
    D 2 represents hydrogen, alkyl, phenyl; alkyl substituted by one or more of hydroxy, pyridyl, phenyl; or alkyl substituted by phenyl which in turn is substituted by halogen, alkyl, amino, alkoxy or nitro,
    or D 2 represents a group of formula III,
    where R 2 and R 12 , or R, o and R 12 may form a chain -CH 2- CH 2- , or R 11 and R 12 may form a chain -CH 2 -, or R 10 , R,, and R 12 are each hydrogen,
    the remainder of R 2 , R 10 and R 11 , which may be the same or different being hydrogen, alkyl or phenyl,
    none, one or two of R 13 , R 14 , R 15 and R 16 represent hydroxy, and the remainder represent hydrogen,
    or R 2 and D 2 , together with the nitrogen atom to which they are attached, form a 5 or 6 membered heterocyclic ring,
    provided that when X is not substituted by hydroxy and

    i) when R 3 , R 4 and R 5 are hydrogen, R, and R 2 are both hydrogen or lower alkyl, and two of R 6 , R 7 , R 8 and R 9 are hydroxy, D 2 is not identical to D 1 , or
    ii) when R,, R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and R 9 are hydrogen, R 2 and D 2 do not each represent lower alkyl, or do not together with the nitrogen atom to which they are attached, form a 5 or 6 membered heterocyclic ring, or iii) when R,, R 4 , R 5 , R 6 , R 7 , R 8 and R 9 are hydrogen, and R 3 is alkyl, D 2 is not identical to D 1 , or
    iv) when R, is phenyl, R 3 and R 5 together form the chain -CH 2 CH 2 -, R 6 , R 7 , R 8 and R 9 are hydrogen, n is 1, D 2 and R 2 do not each represent hydrogen or alkyl, or do not together form a heterocyclic ring,

    and pharmaceutically acceptable derivatives thereof.

    There are also described methods for making the compounds and pharmaceutical, e.g. cardiac, compositions containing the compounds.

    3,4-Dihydroxyphenyl ethyl amine derivatives and pharmaceutical compositions containing them
    3.
    发明公开
    3,4-Dihydroxyphenyl ethyl amine derivatives and pharmaceutical compositions containing them 失效
    3,4-二羟基苯乙氨基 - 衍生物及其衍生物。

    公开(公告)号：EP0118974A1

    公开(公告)日：1984-09-19

    申请号：EP84300384.9

    申请日：1984-01-23

    申请人： FISONS plc

    发明人： Dixon, John ,  Ince, Francis

    IPC分类号： C07C91/32 ,  C07C93/04 ,  C07C149/24 ,  C07C147/02 ,  C07D333/20 ,  A61K31/135 ,  A61K31/38

    CPC分类号： C07C323/25 ,  C07C323/00 ,  C07D333/20

    摘要： There are described compounds of formula I,
    in which Z represents 0, S, S0 2 , CO, NR or a single bond, G represents a one or two ring, saturated or unsaturated carbocyclic or heterocyclic group optionally substituted by phenyl trihalomethyl or at least two groups selected from alkoxy C1 to 6 or halogen atoms, provided that when Z represents a single bond G does not represent phenyl, R represents hydrogen or alkyl C1-6, m and n each independently represent 2, 3 or 4, and q represents an integer from 1 to 3 inclusive, and pharmaceutically acceptable derivatives thereof.
    There are also described processes for producing the compounds and pharmaceutical, e.g. cardiac, compositions containing them.

    摘要翻译： 描述式I，...的化合物，其中Z代表O，SO2，CO，NR或单键，G表示一个或两个环，饱和或不饱和的碳环或杂环基团，任选被苯基三卤代甲基取代或 至少两个选自烷氧基C1至6或卤原子的基团，条件是当Z表示单键时，G不表示苯基，R表示氢或C1-6烷基，... m和n各自独立地表示2,3或4个 ，q表示1〜3的整数，及其药学上可接受的衍生物。 还描述了用于生产化合物和药物的方法，例如， 心脏，含有它们的组合物。

    2-(3,4-Dihydroxyphenyl ethyl amines, their preparation and use as pharmaceutical compounds
    5.
    发明公开
    2-(3,4-Dihydroxyphenyl ethyl amines, their preparation and use as pharmaceutical compounds 失效
    2-（3-4-二羟基苯基） - 甲胺，其中Herstellung und ihre Verwendung als Arzneimittel。

    公开(公告)号：EP0292202A1

    公开(公告)日：1988-11-23

    申请号：EP88304319.2

    申请日：1988-05-12

    申请人： FISONS plc

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

    IPC分类号： C07C215/52

    CPC分类号： C07C215/54

    摘要： There are described compounds of formula I,
        in which
        one of R₃₀ and R₄₀ represents a group Ra,
        and the other of R₃₀ and R₄₀ represents hydrogen or halogen,
        R₅₀ and R₆₀, which may be the same or different, each independently represent hydrogen or alkyl C 1 to C6; in addition R₆₀ may represent a group Rb,
        wherein X represents a C2 to C8 alkylene chain optionally interrupted by a double bond or by S(0) n , wherein n is 0, 1 or 2, Z represents a C 1 to C3 alkylene chain, each of X and Z being optionally substituted by OH or one or more alkyl C 1 to C6,
        R₇₀ represents hydrogen, alkyl C 1 to C6 or (CH₂) q R₁₁,
        R₁₀ and R₁₁ independently represent phenyl substituted by one or more substituents R₂₃, which may be the same or different; or R₁₀ represents a saturated carbocyclic group,
        R₁₅ represents hydrogen, alkyl C 1 to C6, or together with R₂₃ forms a (CH₂)p chain, wherein p represents 0, 1 or 2,
        R₂₀, R₂₁, R₂₂ and R₂₃ independently represent hydrogen, alkyl C 1 to C6, NHR₂₅, SH, NO₂, halogen, CF₃, SO₂R₂₆, CH₂₀H or OH, wherein R₂₅ represents hydrogen, alkyl C 1 to C6 or alkanoyl C 1 to C6 and R₂₆ represents alkyl C 1 to C6 or NH₂
        l represents 2, 3 or 4,
        q represents an integer from 1 to 6 inclusive,
        provided that when R₄₀, R₅₀ and R₇₀ each represent hydrogen and R₆₀ represents Rb,
        then Ra represents 2(3-hydroxyphenyl)ethyl, R₁₅ represents hydrogen and either

    a) X represents (CH₂) p , in which p is 3, 5, 7 or 8 or
    b) at least one of X and Z is substituted by either OH or one or more alkyl C 1 to C6,
        and pharmaceutically acceptable salts and solvates thereof.
    There are also described processes for the preparation of the compounds of formula I and pharmaceutical compositions containing them. The compounds of the invention may be used in the treatment or prophylaxis of renal failure or cardiovascular disorders.

    摘要翻译： 描述了式I的化合物，其中R30和R40中的一个代表基团Ra，，R30和R40中的另一个表示氢或卤素，R50和R60可以相同或不同， 各自独立地表示氢或C 1至C 6的烷基; 另外，R 60可以表示Rb，，其中X表示任选被双键中断的C 2〜C 8亚烷基链或S（O）n，其中n为0,1或2，Z表示C 1〜 C3亚烷基链，X和Z各自任选被OH或一个或多个C 1至C 6的烷基取代，R 70表示氢，烷基C 1至C 6或（CH 2）q R 11，R 10和R 11独立地表示被一个或多个 取代基R 23可以相同或不同; 或R 10表示饱和碳环基，R 15表示氢，C 1至C 6烷基，或与R 23一起形成（CH 2）p链，其中p表示0,1或2，R 20，R 21，R 22和R 23独立地表示氢， 烷基C 1至C 6，NHR 25，SH，NO 2，卤素，CF 3，SO 2 R 26，CH 2 OH或OH，其中R 25表示氢，C 1至C 6烷基或C 1至C 6烷酰基，R 26表示烷基C 1至C 6或NH 2 2,3或4，q表示1〜6的整数，其中R40，R50和R70各自表示氢，R60表示Rb，则Ra表示2（3-羟基苯基）乙基，R15表示氢，a） X表示（CH 2）p，其中p为3,5,7或8或b）X和Z中的至少一个被OH或一个或多个C 1 -C 6烷基取代，及其药学上可接受的盐和溶剂合物 。 还描述了制备式I化合物的方法和含有它们的药物组合物。 本发明的化合物可用于治疗或预防肾衰竭或心血管疾病。

    Pharmacologically active pyrrole and pyrazole derivatives
    7.
    发明公开
    Pharmacologically active pyrrole and pyrazole derivatives 失效
    Pharmakologisch aktive Pyrrol- und Pyrazolderivate。

    公开(公告)号：EP0230110A1

    公开(公告)日：1987-07-29

    申请号：EP86309235.9

    申请日：1986-11-26

    申请人： FISONS plc

    发明人： Baxter, Andrew John Gilby ,  Dixon, John ,  Ince, Francis ,  Springthorpe, Brian ,  Tinker, Alan Charles

    IPC分类号： C07D207/337 ,  C07D231/14 ,  C07D401/06 ,  C07D413/06 ,  A61K31/395

    CPC分类号： C07D207/325 ,  C07C59/56 ,  C07C59/88 ,  C07C323/00 ,  C07D207/335 ,  C07D207/34 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16

    摘要： There are described compounds of formula I,
    wherein

    either one of Y and Z (which may be the same or different) represents CH, CR 2 or C-COOR 21 , in which R 2 represents alkyl C 1 to C6 optionally substituted by halogen, hydroxy, amino, isothioureido or a group R 5 COO- in which R 5 represents alkyl C 1 to C6, R 2 being optionally interrupted by O or S, and R 21 represents alkyl C 1 to C6, and the other one of Y and Z represents CR 2 or C-COOR 21 ,
    or one of Y and Z represents N and the other CH, CR 2 or C-COOR 21 ,
    R 4 represents Ar 1 -B-(W) x , in which
    W represents C=O, S, SO, SO 2 or C=N-OH,
    x represents 0 or 1,
    B represents a single bond or (CH 2 )p in which p represents 1 or 2, the group (CH 2 )p being optionally substituted by alkyl C1 to
    Ar 1 represents phenyl, naphthyl or benzofurazanyl, Ar 1 being optionally substituted by one or more of X, CX 3 , OCH n X 3-n , hydroxy, alkyl C 1 to C6, Oalkyl C 1 to C6, nitro, amino, carboxy, -SCH 2 Ar 2 , -OCH 2 Ar 2 or -OCOAr 2 in which
    X represents halogen,
    n represents 0,1, 2 or 3, and
    Ar 2 represents phenyl or phenyl substituted by hydroxy, halogen, alkyl C 1 to C6 or Oalkyl C 1 to C6, and
    R 3 and R 1 are as defined in the specification.

    There are also described processes for the preparation of compounds of formula I and pharmaceutical, eg cardiovascular, compositions containing them.

    摘要翻译： 描述了式I，的化合物，其中Y和Z（其可以相同或不同）中的任一个表示CH，CR 2或C-COOR 21，其中R 2表示任选被卤素取代的C 1 -C 6烷基，羟基 ，氨基，异硫脲基或R5COO-基团，其中R5表示烷基C1至C6，R2任选被O或S间隔，R21表示烷基C1至C6，Y和Z中的另一个表示CR2或C-COOR21， 或者Y和Z中的一个表示N，另一个CH，CR 2或C-COOR 21，R 4表示Ar 1 -B-（W）x，其中W表示C = O，S，SO，SO 2或C = N-OH， x表示0或1，B表示单键或（CH 2）p，其中p表示1或2，基团（CH 2）p任选被C 1至C 6的烷基取代，Ar 1表示苯基，萘基或苯并呋咱基，Ar 1表示 任选地被X，CX 3，OCH n X 3-n，羟基，C 1 -C 6烷基，C 1至C 6的烷基，硝基，氨基，羧基，-SCH 2 Ar 2，-OCH 2 Ar 2或-OCOAr 2中的一个或多个取代，其中X表示卤素， s 0,1,2或3，并且Ar 2表示苯基或被羟基，卤素，C 1至C 6烷基或C 1至C 6烷基取代的苯基，R 3和R 1如本说明书中所定义。 还描述了制备式I化合物和药物，例如含有它们的心血管组合物的方法。

    Catecholamine derivatives, processes for their preparation and pharmaceutical compositions thereof
    8.
    发明公开
    Catecholamine derivatives, processes for their preparation and pharmaceutical compositions thereof 失效
    的儿茶酚胺衍生物，它们的制备方法和它们的药物组合物。

    公开(公告)号：EP0223598A2

    公开(公告)日：1987-05-27

    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

    摘要： There are described compounds of formula I,
    in which X represents a C2 to 8 alkylene chain optionally interrupted by a double bond or by S(O) n , wherein n is 0, 1 or 2;
    Y represents O or NH,
    l and m each independently represent 2, 3 or 4,
    R₁₀ represents phenyl substituted by one or more substituents R₂₃, which may be the same or different; or R₁₀ represents pyridyl, a saturated carbocyclic group, alkyl C 1 to 6 or hydrogen,
    R₁₅ represents hydrogen or together with R₂₃ forms a (CH₂) p chain, wherein p represents 0, 1 or 2;
    R₂₀, R₂₁, R₂₂ and R₂₃, which may be the same or different, independently represent hydrogen, alkyl C 1 to 6, NHR₂₅, SH, NO₂, halogen, CF₃, SO₂R₃₀, CH₂OH or OH, wherein R₂₅, represents hydrogen, alkyl C 1 to 6, alkanoyl C 1 to 6 or SO₂ alkyl C 1 to 6, and R₃₀ represents alkyl C 1 to 6 or NH₂,
    provided that when X represents an uninterrupted C4 alkylene chain, Y represents NH, m represents 2, l represents 2, R₁₀ represents phenyl, R₁₅ represents hydrogen, and R₂₁, R₂₂ and R₂₃ represent hydrogen, then R₂₀ does not represent hydrogen or 4-OH,
    and pharmaceutically acceptable salts and solvates thereof.
    There are also described processes for the preparation of the compounds of formula I and pharmaceutical compositions containing them. The compounds of the invention may be used in the treatment or prophylaxis of renal failure or cardiovascular disorders.

    Phenylethylamines, process for their preparation and compositions containing them
    9.
    发明公开
    Phenylethylamines, process for their preparation and compositions containing them 失效
    苯乙胺，其制备方法以及含有它们的组合物的方法。

    公开(公告)号：EP0142283A2

    公开(公告)日：1985-05-22

    申请号：EP84307102.8

    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： C07C215/30 ,  C07C215/22 ,  C07C323/01 ,  C07C275/28 ,  C07C233/64 ,  C07C237/02 ,  C07C317/02 ,  C07C215/46

    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： There are described compounds ofiformula I,
    in which R, represents OH, NR 11 R 12 , CH 2 R 12 or fluorine,

    R 2 , R 3 , R 11 , R 12 and R 2 , have various meanings as defined herein for example R 2 and R 3 may represent hydrogen, halogen, alkyl C1 to 6 or nitro;
    W represents a single bond, a disubstituted benzene or a 1,4-cyclohexanediyl group,
    X represents NH, 0, S, SO 2 , CO, CH 2 , CONH or-COO;
    Y, amongst other meanings defined herein, represents (CH 2 )q, CO, CS and SO 2 ,
    Z represents a single bond, NR 19 , CH 2 , O, CO, S or SO 2 , in which R 10 represents hydrogen or alkyl C1 to 6,
    n and m each independently represent an integer from 1 to 4 inclusive,
    q represents an integer from 1 to 3 inclusive,
    p represents 0 or an integer from 1 to 3 inclusive,
    R 10 represents hydrogen or chlorine,
    R 20 , amongst other meanings defined herein may represent hydrogen, with four provises as defined herein, and pharmaceutically acceptable derivatives thereof.

    There are also described the use of the compounds of formula 1 as pharmaceuticals, methods for making the compounds and pharmaceutical, e.g. cardiac, compositions containing the compounds.

    摘要翻译： 有式描述的化合物I，... ...其中R1 darstellt OH，NR 11 R 12，CH2R12或氟，... R2，R3，R11，R12和R21具有如对于实施例2和R 3定义可代表氢各种含义， 卤素，烷基C 1〜6或硝基; ... W表示单键，二取代苯或1,4-亚环己二基，... X darstellt NH，O，S，SO2，CO，CH 2，CONH或COO; ... Y 除了其他含义中所定义，darstellt（CH 2）q，CO，CS和SO2，... Z表示单键，NR 19，CH 2，O，CO，S或SO 2中哪R19 darstellt氢或烷基C1〜6，... N 和m各自独立地表示整数1〜4以下，。q darstellt到整数1至3个以下，。。。p darstellt 0或整数1至3个以下，... R10 darstellt氢或氯... R20，除其他含义 定义在可代表氢，...与如在定义了四个provises，以及它们的药学上可接受的衍生物。 ... 有这样描述了式I化合物作为药物，方法用于制备化合物和药物，E.G. 心脏，COMPOSITIONS CONTAINING的化合物。