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    Dihydropyridines, processes and intermediates for their production, and pharmaceutical formulations containing them
    2.
    发明公开
    Dihydropyridines, processes and intermediates for their production, and pharmaceutical formulations containing them 失效
    二氢吡啶，过程和它们的制备的中间体和包含它们的药物组合物。

    公开(公告)号：EP0174131A2

    公开(公告)日：1986-03-12

    申请号：EP85305930.1

    申请日：1985-08-21

    申请人： FISONS plc

    发明人： Baxter, Andrew John Gilby ,  Dixon, John ,  Gould, Kenneth John ,  Tinker, Alan Charles

    IPC分类号： C07D211/90 ,  C07D405/12 ,  C07D409/12 ,  C07D401/12 ,  C07D401/04 ,  C07D409/14 ,  C07D417/12 ,  C07D401/06 ,  A61K31/44

    CPC分类号： C07D209/48 ,  C07C45/00 ,  C07C47/55 ,  C07C47/575 ,  C07C205/44 ,  C07D231/12 ,  C07D231/20 ,  C07D233/56 ,  C07D249/08 ,  C07D305/08 ,  C07D331/04 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12

    摘要： There are described compounds of formula 1,

    in which R,, R 2 , R 3 , R s and R 6 are as defined in the specification and R 4 is a phenyl group carrying 3 or 4 substituents or is an unsaturated 5 membered heterocyclic group containing a single hetero-atom selected from oxygen, sulphur or nitrogen, R 4 being substituted by CF 3 , XR 22 , nitro, halogen, CN, alkyl C1 to 6, formyl dioxalanyl, -N(R 23 )COR 24 -CONR 25 R 26 , or amino which is optionally substituted by phenylsulphonyl or by trifluoroacetyl, and R 4 carries a substituent on the atom adjacent to the atom through which R 4 is connected to the remainder of the molecule,

    R 22 is phenyl or alkyl C1 to 6 optionally substituted by halogen,
    X is 0 or S(O) n ,
    n is 0, 1 or 2, and
    R 23 , R 24 , R 25 and R 26 , which may be the same or different, are each hydrogen or alkyl C1 to 6.

    There are also described methods for making the compounds, and their formulation and use as pharmaceuticals, eg for the treatment of cardiovascular conditions.
    There are further described compounds R 4 CHO which are useful in making compounds of formula I.

    摘要翻译： 中描述了式I的化合物，其中R1，R2，R3，R5和R6如说明书中所定义和R 4是承载3个或4个取代基的苯基或是包含单一的不饱和5元杂环基团 选自氧，硫或氮，R 4由CF 3，XR22，硝基，卤素，CN，烷基C1〜6，二氧戊环基甲酰基是substituiertem的杂原子，-N（R23）COR24 -CONR25R26，或氨基其是由苯磺酰OPTIONALLY substituiertem 或三氟乙酰基，和R 4进行的原子毗邻通过其中R 4被连接到分子的其余部分的原子的取代基，R 22是苯基或烷基C1至由卤素6 OPTIONALLY substituiertem，X是O或S（O）N 中，n为0，1或2，且R23，R24，R25和R26，其可以是相同或不同，各自为氢或烷基C1〜6有这样描述了用于制备该化合物的方法以及它们的配制和使用 作为药品，例如用于心血管疾病的治疗。 有进一步描述化合物中，R 4 CHO它们在制备式I化合物的有用

    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。

    Dihydropyridine derivatives, processes for their preparation and pharmaceutical compositions thereof
    8.
    发明公开
    Dihydropyridine derivatives, processes for their preparation and pharmaceutical compositions thereof 失效
    二氢吡啶衍生物，它们的制备方法和含有它们的药物组合物。

    公开(公告)号：EP0225175A2

    公开(公告)日：1987-06-10

    申请号：EP86309244.1

    申请日：1986-11-27

    申请人： FISONS plc

    发明人： Baxter, Andrew John Gilby ,  Dixon, John ,  McInally, Thomas ,  Tinker, Alan Charles

    IPC分类号： C07D211/90 ,  C07D401/06 ,  C07D401/12 ,  C07D409/12 ,  C07D409/04 ,  A61K31/445 ,  A61K31/505

    CPC分类号： C07D231/12 ,  C07D211/90 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/12 ,  C07D409/04 ,  C07D409/12

    摘要： There are described compounds of Formula I,
    in which R₁, R₂, R₃ and R₄ are as defined in the specification,
    R₅ is alkyl optionally interrupted by an amide group and optionally substituted by halogen or by a carboxy or a heterocyclic group,
    X is -O-, -NR-, -S(O) m₁ , or a bond,
    Z is hydrogen or together with R forms a bond,
    R is hydrogen, alkyl or together with Z forms a bond,
    R₆ is a 5 or 6 membered unsaturated nitrogen containing heterocyclic ring, optionally fused to a phenyl ring and optionally substituted by one or more of oxo, hydroxy, alkyl, -(CH₂) n₁ NH₂, alkoxy, phenyl or -COOH,
    and when X is -NR- or -S(O) m₁ -, R₆ may in addition be hydrogen or a group -CH₂CH₂NH₂, -CH₂CH₂-het. or NHC(=NH)NH₂,
    when X is -O-, R₆ may also be a group -NH₂, -C(=O) (CH₂) n NH₂, -CH₂CH₂NR₁₄R₁₅ or CH₂CH₂OCH₂CH₂NR₁₄R₁₅,
    when X is -NR-, -S(O) m₁ -, or a bond, R₆ may also be hydrogen or a group -C(=NR₁₂)NHR₁₃,
    R₁₃ and R₁₄ may be hydrogen or alkyl,
    R₁₂ is hydrogen, alkylcarbonyl, nitrile or hydroxy,
    R₁₅ is hydrogen or a group R₁₁,
    m and m₁ are each 0, 1 or 2,
    n is 0 or 1,
    n₁ is an integer from 0 to 6
    and pharmaceutically acceptable salts, esters, amides, analogues and protected derivatives thereof.

    摘要翻译： 中描述了I，其中R1，R2，R3和R4如说明书中所定义的式的化合物，R 5是烷基，其任选通过在酰胺基和任选substituiertem中断被卤素或由羧基或杂环基团， X是-O - ， - NR-，-S（O）M1，或一个键，Z为氢或一起为R形成键，R是氢，烷基或连同Z形成一个键，R 6是一个5或 6元杂环的不饱和含氮，由一个或多个氧代，羟基，烷基，任选稠合至苯环和任选substituiertem - （CH2）n1NH2，烷氧基，苯基或-COOH，并且当X是-NR-或 - S（O）M1，R 6可以另外是氢或基团-CH2CH2NH2，-CH2CH2-HET。 或NHC（= NH）NH 2，当X是-O-，R 6可以因此基团-NH 2，-C（= O）（CH 2）N NH 2，或-CH2CH2NR14R15 CH2CH2OCH2CH2NR14R15，当X为-NR - ， - S（ O）M1-，或键，R6因此可以是氢或基团-C（= NR 12）NHR13，R13和R14可以是氢或烷基，R 12为氢，烷基羰基，腈或羟基，R15是氢或基团 R11，m和M1各自为0，1或2，n是0或1，n1为0〜6及其可药用盐，酯，酰胺，受保护的类似物和衍生物的整数。

    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。