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    Aminoalkyl furan derivatives
    11.
    发明授权
    Aminoalkyl furan derivatives 失效
    氨基烷基呋喃衍生物

    公开(公告)号：US4128658A

    公开(公告)日：1978-12-05

    申请号：US818762

    申请日：1977-07-25

    申请人： Barry J. Price ,  John W. Clitherow ,  John Bradshaw

    发明人： Barry J. Price ,  John W. Clitherow ,  John Bradshaw

    IPC分类号： C07C323/25 ,  A61K31/34 ,  A61K31/341 ,  A61P43/00 ,  C07C67/00 ,  C07C313/00 ,  C07D207/08 ,  C07D233/64 ,  C07D275/02 ,  C07D275/03 ,  C07D307/38 ,  C07D307/52 ,  C07D307/54 ,  C07D307/64 ,  C07D405/06 ,  C07D405/12 ,  C07D413/14 ,  A01N9/12 ,  A01N9/20

    CPC分类号： C07D275/03 ,  A61K31/34 ,  C07D207/08 ,  C07D307/38 ,  C07D307/52 ,  C07D307/64

    摘要： Compounds of the general formula I: ##STR1## and physiologically acceptable salts thereof and N-oxides and hydrates, in which R.sub.1 and R.sub.2 which may be the same or different represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group ##STR2## in which R.sub.4 represents hydrogen or lower alkyl or R.sub.1 and R.sub.2 may, together with the nitrogen atom to which they are attached, form a heterocyclic ring which may contain other heteroatoms selected from O and ##STR3## R.sub.3 is hydrogen, lower alkyl, lower alkenyl or alkoxyalkyl; X is --CH.sub.2 --, O or S;Y represents .dbd. S, .dbd. O, .dbd. NR.sub.5 or .dbd. CHR.sub.6 ;Alk denotes a straight or branched alkylene chain of 1 to 6 carbon atoms;R.sub.5 is H, nitro, cyano, lower alkyl, aryl, alkylsulphonyl, or arylsulphonyl;R.sub.6 represents nitro, arylsulphonyl or alkylsulphonyl;M is an integer from 2 to 4; andN is 1 or 2; or when X .dbd. S, or --CH.sub.2 --, n is zero, 1 or 2.These compounds have H.sub.2 -antagonist activity. Intermediates in the production thereof are also provided.

    摘要翻译： 通式I的化合物及其生理上可接受的盐和N-氧化物和水合物，其中可以相同或不同的R 1和R 2表示氢，低级烷基，环烷基，低级烯基，芳烷基或 被氧原子间隔的低级烷基或其中R 4表示氢或低级烷基或R 1和R 2的基团可以与它们所连接的氮原子一起形成杂环，该杂环可以含有选自O 且R 3为氢，低级烷基，低级烯基或烷氧基烷基; X是-CH 2 - ，O或S; Y表示= S，= O，= NR5或= CHR6; Alk表示1〜6个碳原子的直链或支链亚烷基链; R5是H，硝基，氰基，低级烷基，芳基，烷基磺酰基或芳基磺酰基; R6表示硝基，芳基磺酰基或烷基磺酰基; M是从2到4的整数; 和N是1或2; 或当X = S或-CH 2 - 时，n为0,1或2。

    Furan derivatives having selective action on histamine receptors
    12.
    发明授权
    Furan derivatives having selective action on histamine receptors 失效
    呋喃衍生物对组胺受体具有选择性作用

    公开(公告)号：US4255440A

    公开(公告)日：1981-03-10

    申请号：US951026

    申请日：1978-10-13

    申请人： Barry J. Price ,  John W. Clitherow ,  John Bradshaw

    发明人： Barry J. Price ,  John W. Clitherow ,  John Bradshaw

    IPC分类号： C07C323/25 ,  A61K31/34 ,  A61K31/341 ,  A61P43/00 ,  C07C67/00 ,  C07C313/00 ,  C07D207/08 ,  C07D233/64 ,  C07D275/02 ,  C07D275/03 ,  C07D307/38 ,  C07D307/52 ,  C07D307/54 ,  C07D307/64 ,  C07D405/06 ,  C07D405/12 ,  C07D413/14 ,  A61K31/40 ,  A61K31/535 ,  C07D413/06

    CPC分类号： C07D275/03 ,  A61K31/34 ,  C07D207/08 ,  C07D307/38 ,  C07D307/52 ,  C07D307/64

    摘要： Compounds of the general formula I: ##STR1## and physiologically acceptable salts thereof and N-oxides and hydrates, in which R.sub.1 and R.sub.2 which may be the same or different represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group ##STR2## in which R.sub.4 represents hydrogen or lower alkyl or R.sub.1 and R.sub.2 may, together with the nitrogen atom to which they are attached, form a heterocyclic ring which may contain other heteroatoms selected from O and ##STR3## R.sub.3 is hydrogen, lower alkyl, lower alkenyl or alkoxyalkyl; X is --CH.sub.2 --, O-- or --S--;Y represents .dbd.S, .dbd.O, .dbd.NR.sub.5 or .dbd.CHR.sub.6 ;Alk denotes a straight or branched alkylene chain of 1 to 6 carbon atoms;R.sub.5 is H, nitro, cyano, lower alkyl, aryl, alkylsulphonyl, or arylsulphonyl;R.sub.6 represents nitro, arylsulphonyl or alkylsulphonyl;m is an integer from 2 to 4; andn is 1 or 2; or when X is --S-- or --CH.sub.2 --, n is zero, 1 or 2.These compounds have H.sub.2 -antagonist activity. Intermediates in the production thereof are also provided.

    摘要翻译： 通式I的化合物及其生理上可接受的盐和N-氧化物和水合物，其中可以相同或不同的R 1和R 2表示氢，低级烷基，环烷基，低级烯基，芳烷基或 被氧原子间隔的低级烷基或其中R 4表示氢或低级烷基或R 1和R 2的基团可以与它们所连接的氮原子一起形成杂环，该杂环可以含有选自O 且R 3为氢，低级烷基，低级烯基或烷氧基烷基; X是-CH 2 - ，O-或-S-; Y表示= S，= O，= NR5或= CHR6; Alk表示1〜6个碳原子的直链或支链亚烷基链; R5是H，硝基，氰基，低级烷基，芳基，烷基磺酰基或芳基磺酰基; R6表示硝基，芳基磺酰基或烷基磺酰基; m为2〜4的整数; n为1或2; 或当X为-S-或-CH 2 - 时，n为0,1或2.这些化合物具有H 2 - 拮抗剂活性。 还提供了其生产中的中间体。

    Substituted furan compounds and pharmaceutical compositions containing them
    13.
    发明授权
    Substituted furan compounds and pharmaceutical compositions containing them 失效
    取代的呋喃化合物和含有它们的药物组合物

    公开(公告)号：US4288443A

    公开(公告)日：1981-09-08

    申请号：US124115

    申请日：1980-02-25

    申请人： Duncan B. Judd ,  John W. Clitherow ,  Barry J. Price ,  John Bradshaw

    发明人： Duncan B. Judd ,  John W. Clitherow ,  Barry J. Price ,  John Bradshaw

    IPC分类号： A61K31/34 ,  A61K31/341 ,  A61P1/04 ,  C07D307/52 ,  C07D307/56 ,  C07D307/68 ,  C07D307/54

    CPC分类号： C07D307/56 ,  C07D307/52 ,  C07D307/68

    摘要： The invention relates to compounds of the general formula ##STR1## and physiologically acceptable salts and N-oxides, hydrates and bioprecursors thereof, in which R.sub.1 and R.sub.2 which may be the same or different each represent hydrogen, C.sub.1-8 alkyl, C.sub.4-8 cycloalkyl, C.sub.3-6 alkenyl, aralkyl with 1 to 4 carbon atoms in the alkyl residue or C.sub.1-8 alkyl interrupted by an oxygen atom or a group ##STR2## in which R.sub.5 represents hydrogen or C.sub.1-8 alkyl, or R.sub.1 and R.sub.2 may together with the nitrogen atom to which they are attached, form a saturated monocyclic 5 to 7 membered heterocyclic ring which may additionally contain the heterofunction O or ##STR3## R.sub.3 represents straight or branched chain C.sub.1-8 alkyl, alkoxyalkyl with 1 to 8 carbon atoms in each alkyl residue, C.sub.1-8 hydroxyalkyl, C.sub.1-8 alkoxycarbonyl, alkyl thioalkyl with 1 to 8 carbon atoms in each alkyl residue, halogen or aryl;R.sub.4 represents hydrogen, C.sub.1-8 alkyl, C.sub.3-6 alkenyl or alkoxyalkyl with 1 to 8 carbon atoms in each alkyl residue;X represents --O-- or --S--;Y represents .dbd.S, .dbd.O, .dbd.NR.sub.6 or .dbd.CHNO.sub.2 where R.sub.6 represents hydrogen, nitro, cyano, C.sub.1-8 alkyl, aryl, C.sub.1-8 alkylsulphonyl or arylsulphonyl;m represents an integer from 2 to 4 inclusive; andn represents an integer which is 1 or 2, or additionally when X is --S-- n may also be zero.The invention also relates to processes for the production of such compounds, pharmaceutical compositions containing them and certain novel intermediates used in their production, i.e. amines of the formula ##STR4## and alcohols of the formula ##STR5## The compounds of formula (I) show pharmacological activity as selective histamine H.sub.2 -antagonists.

    摘要翻译： 本发明涉及通式为（I）的化合物及其生理上可接受的盐和N-氧化物，水合物和生物前体，其中可以相同或不同的R 1和R 2各自表示氢，C 1-8烷基， C4-8环烷基，C3-6烯基，在烷基中具有1至4个碳原子的芳烷基或被氧原子间断的C1-8烷基或其中R5表示氢或C1-8烷基的基团，或R1 并且R 2可以与它们所连接的氮原子一起形成饱和的单环5至7元杂环，其可另外含有杂官能O，或者R 3表示直链或支链C 1-8烷基，烷氧基烷基与1至 每个烷基残基中的8个碳原子，C 1-8羟基烷基，C 1-8烷氧基羰基，每个烷基残基中具有1至8个碳原子的烷基硫代烷基，卤素或芳基; R4表示氢，C1-8烷基，C3-6烯基或每个烷基残基具有1至8个碳原子的烷氧基烷基; X表示-O-或-S-; Y表示= S，= O，= NR6或= CHNO2，其中R6表示氢，硝基，氰基，C1-8烷基，芳基，C1-8烷基磺酰基或芳基磺酰基; m表示2〜4的整数， 并且n表示1或2的整数，或者当X是-S-n时也可以为零。 本发明还涉及生产这种化合物的方法，含有它们的药物组合物和它们生产中使用的某些新型中间体，即式（III）的胺和式的醇（VIII）。化合物 式（I）表示作为选择性组胺H2拮抗剂的药理学活性。

    Aminoalkyl furan derivatives
    16.
    发明授权
    Aminoalkyl furan derivatives 失效
    氨基烷基呋喃衍生物

    公开(公告)号：US4279819A

    公开(公告)日：1981-07-21

    申请号：US951025

    申请日：1978-10-13

    申请人： Barry J. Price ,  John W. Clitherow ,  John Bradshaw

    发明人： Barry J. Price ,  John W. Clitherow ,  John Bradshaw

    IPC分类号： C07C323/25 ,  A61K31/34 ,  A61K31/341 ,  A61P43/00 ,  C07C67/00 ,  C07C313/00 ,  C07D207/08 ,  C07D233/64 ,  C07D275/02 ,  C07D275/03 ,  C07D307/38 ,  C07D307/52 ,  C07D307/54 ,  C07D307/64 ,  C07D405/06 ,  C07D405/12 ,  C07D413/14

    CPC分类号： C07D275/03 ,  A61K31/34 ,  C07D207/08 ,  C07D307/38 ,  C07D307/52 ,  C07D307/64

    摘要： Compounds of the general formula I: ##STR1## and physiologically acceptable salts thereof and N-oxides and hydrates, in which R.sub.1 and R.sub.2 which may be the same or different represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group ##STR2## in which R.sub.4 represents hydrogen or lower alkyl or R.sub.1 and R.sub.2 may, together with the nitrogen atom to which they are attached, form a heterocyclic ring which may contain other heteroatoms selected from O and ##STR3## R.sub.3 is hydrogen, lower alkyl, lower alkenyl or alkoxyalkyl; X is --CH.sub.2 --, O or S;Y represents .dbd.S, .dbd.O, .dbd.NR.sub.5 or .dbd.CHR.sub.6 ;Alk denotes a straight or branched alkylene chain of 1 to 6 carbon atoms;R.sub.5 is H, nitro, cyano, lower alkyl, aryl, alkylsulphonyl, or arylsulphonyl;R.sub.6 represents nitro, arylsulphonyl or alkylsulphonyl;m is an integer from 2 to 4; andn is 1 or 2; or when X.dbd.S, or --CH.sub.2 --, n is zero, 1 or 2.These compounds have H.sub.2 -antagonist activity. Intermediates in the production thereof are also provided.

    摘要翻译： 通式I的化合物及其生理上可接受的盐和N-氧化物和水合物，其中可以相同或不同的R 1和R 2表示氢，低级烷基，环烷基，低级烯基，芳烷基或 被氧原子间隔的低级烷基或其中R 4表示氢或低级烷基或R 1和R 2的基团可以与它们所连接的氮原子一起形成杂环，该杂环可以含有选自O 且R 3为氢，低级烷基，低级烯基或烷氧基烷基; X是-CH 2 - ，O或S; Y表示= S，= O，= NR5或= CHR6; Alk表示1〜6个碳原子的直链或支链亚烷基链; R5是H，硝基，氰基，低级烷基，芳基，烷基磺酰基或芳基磺酰基; R6表示硝基，芳基磺酰基或烷基磺酰基; m为2〜4的整数; n为1或2; 或当X = S或-CH 2 - 时，n为0,1或2.这些化合物具有H 2 - 拮抗剂活性。 还提供了其生产中的中间体。

    Thiophene derivatives and their pharmaceutical compositions and method of use
    19.
    发明授权
    Thiophene derivatives and their pharmaceutical compositions and method of use 失效
    噻吩衍生物及其药物组合物和使用方法

    公开(公告)号：US4382929A

    公开(公告)日：1983-05-10

    申请号：US200007

    申请日：1980-10-23

    申请人： John Bradshaw ,  Duncan B. Judd ,  Barry J. Price ,  John W. Clitherow

    发明人： John Bradshaw ,  Duncan B. Judd ,  Barry J. Price ,  John W. Clitherow

    IPC分类号： C07D333/20 ,  C07D333/28 ,  C07D333/32 ,  C07D333/34 ,  C07D333/42 ,  C07D417/06 ,  A61K31/38

    CPC分类号： C07D333/42 ,  C07D333/20 ,  C07D333/28 ,  C07D333/32 ,  C07D333/34

    摘要： The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in which one of R.sub.1 and R.sub.2 represents hydrogen, halogen or a C.sub.1-4 alkyl group which may be optionally substituted by hydroxy or C.sub.1-4 alkoxy, and the other represents the group R.sub.4 R.sub.5 NAlk-- in which R.sub.4 represents hydrogen, C.sub.1-10 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, heteroaralkyl, trifluoroalkyl, or alkyl substituted by hydroxy, alkoxy, amino, alkylamino, dialkylamino or cycloalkyl, and R.sub.5 represents hydrogen or a C.sub.1-4 alkyl group or R.sub.4 and R.sub.5 may, together with the nitrogen atom to which they are attached, form a 5 to 10 membered ring which may be saturated or may contain at least one double bond, may be unsubstituted or may be substituted by one or more C.sub.1-3 alkyl groups or a hydroxy group and/or may contain another heteroatom selected from oxygen and sulphur;Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms;R.sub.3, which may be in either the 2 or 3-position, represents the group ##STR2## where X represents --CH.sub.2 --, --O-- or --S--; n represents zero, 1 or 2;m represents 2, 3 or 4; andwhere Y represents S, O, CHNO.sub.2 or NR.sub.7 where R.sub.7 is nitro, cyano, alkylsulphonyl or arylsulphonyl;R.sub.6 represents hydrogen, alkyl, alkenyl, alkynyl, alkoxyalkyl or aralkyl;with the provisos thatwhere R.sub.2 represents the group R.sub.4 R.sub.5 NAlk then R.sub.3 is in the 2-position; andwhere R.sub.2 represents hydrogen then R.sub.3 is in the 3-position.The compounds of formula (I) show pharmacological activity as selective histamine H.sub.2 -- antagonists.

    摘要翻译： 本发明提供了通式（I）的化合物及其生理学上可接受的盐，水合物和生物前体，其中R 1和R 2中的一个代表氢，卤素或任选被取代的C 1-4烷基 另一个代表R4R5NAlk-，其中R4代表氢，C1-10烷基，环烷基，烯基，炔基，芳烷基，杂芳烷基，三氟烷基或被羟基，烷氧基，氨基，烷基氨基取代的烷基 ，二烷基氨基或环烷基，R 5表示氢或C 1-4烷基或R 4和R 5可以与它们所连接的氮原子一起形成5至10元环，其可以是饱和的或可以含有至少一个 双键可以是未取代的或可以被一个或多个C 1-3烷基或羟基取代和/或可以含有另外选自氧和硫的杂原子; Alk表示1〜6个碳原子的直链或支链亚烷基链; R 3可以在2或3位，表示基团，其中X表示-CH 2 - ， - O-或-S-; n表示0，1或2; m表示2,3或4; 其中Y表示S，O，CHNO 2或NR 7，其中R 7是硝基，氰基，烷基磺酰基或芳基磺酰基; R6表示氢，烷基，烯基，炔基，烷氧基烷基或芳烷基; 条件是其中R2表示R4R5NAlk基团，则R3为2-位; 并且其中R 2表示氢，则R 3为3-位。 式（I）的化合物显示作为选择性组胺H2拮抗剂的药理活性。

    Amine derivatives
    20.
    发明授权
    Amine derivatives 失效
    胺衍生物

    公开(公告)号：US4317819A

    公开(公告)日：1982-03-02

    申请号：US213680

    申请日：1980-12-05

    申请人： John W. Clitherow ,  Barry J. Price ,  John Bradshaw ,  Michael Martin-Smith

    发明人： John W. Clitherow ,  Barry J. Price ,  John Bradshaw ,  Michael Martin-Smith

    IPC分类号： A61K31/155 ,  A61K31/335 ,  A61K31/38 ,  A61P1/00 ,  C07C67/00 ,  C07C209/00 ,  C07C211/27 ,  C07C213/00 ,  C07C217/48 ,  C07C239/00 ,  C07C275/12 ,  C07C279/04 ,  C07C279/28 ,  C07C301/00 ,  C07C311/64 ,  C07C325/00 ,  C07C335/08 ,  C07D233/64 ,  C07D295/096 ,  C07D307/38 ,  C07D307/42 ,  C07D307/52 ,  C07D333/14 ,  A61K31/17 ,  C07C127/17 ,  C07C129/12

    CPC分类号： C07D295/096 ,  C07C279/28 ,  C07D307/38 ,  C07D307/42 ,  C07D307/52 ,  C07D333/14 ,  Y10S514/886 ,  Y10S514/926 ,  Y10S514/927

    摘要： The invention provides compounds of general formula ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichY and Z, which may be the same or different, each represent oxygen, sulphur, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 is hydrogen, nitro, cyano, lower alkyl, aryl, alkylsulphonyl or arylsulphonyl;p has a value from 2 to 12;R.sub.1 represents ##STR2## in which R.sub.4 and R.sub.5 which may be the same or different, each represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group >N-R.sub.6 in which R.sub.6 represents hydrogen or lower alkyl, or R.sub.4 and R.sub.5 together with the nitrogen atom to which they are attached form a 5 to 7-membered saturated heterocyclic ring which may contain an additional oxygen atom or the group >NR.sub.6 ;Q represents a furan or thiophen ring in which incorporation into the rest of the molecule is through bonds at the 2 and 5 positions, or a benzene ring in which incorporation into the rest of the molecule is through bonds at the 1 and 3 or 1 and 4 positions;X represents --CH.sub.2 --, --O-- or --S--;n represents zero or 1;m represents 2, 3 or 4 and Alk represents a straight chain alkylene group of 1 to 3 carbon atoms,andR.sub.2 represents lower alkyl or the group--(CH.sub.2).sub.y E(CH.sub.2).sub.x Gin whichy represents 2, 3 or 4 or can additionally represent zero or 1 when E is a --CH.sub.2 -- group, x represents zero, 1 or 2;E represents --CH.sub.2 --, --O-- or --S--; andG represents a monocyclic 5 or 6 membered carbocyclic or heterocyclic aromatic ring, or G represents the group ##STR3## where Q' represents any of the rings defined for Q; Alk' represents any of the groups defined for Alk; and R.sub.4 ' and R.sub.5 ' which may be the same or different represent any of the groups defined for R.sub.4 or R.sub.5.The compounds of formula (I) have pharmacological activity as selective histamine H.sub.2 -antagonists.

    摘要翻译： 本发明提供了通式（I）的化合物及其生理上可接受的盐，水合物和生物前体，其中Y和Z可以相同或不同，各自表示氧，硫，= CHNO 2或= NR 3，其中R 3 是氢，硝基，氰基，低级烷基，芳基，烷基磺酰基或芳基磺酰基; p的值为2到12; R 1表示其中可以相同或不同的R 4和R 5各自表示氢，低级烷基，环烷基，低级烯基，芳烷基或被氧原子间隔的低级烷基或基团> N-R6，其中R 6表示 氢或低级烷基，或R4和R5与它们所连接的氮原子一起形成可含有另外的氧原子或基团> NR 6的5至7元饱和杂环; Q表示呋喃或噻吩环，其中与分子的其余部分结合通过2和5位的键，或苯环，其中结合到分子的其余部分通过1和3或1的键和 4个职位; X表示-CH 2 - ， - O-或-S-; n表示0或1; m表示2,3或4，Alk表示1〜3个碳原子的直链亚烷基，R2表示低级烷基或 - （CH2）yE（CH2）xG，y表示2,3或4或可以 当E是-CH 2 - 基时，x代表0或1; E表示-CH 2 - ， - O-或-S-; 并且G表示单环5或6元碳环或杂环芳环，或G表示基团，其中Q'表示为Q定义的任何环; Alk'代表为Alk定义的任何组; 和可以相同或不同的R 4'和R 5'表示对于R 4或R 5定义的任何基团。 式（I）化合物具有作为选择性组胺H2拮抗剂的药理学活性。