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1. 发明授权

US5202343A Tricyclic ketones useful as HT.sub.3 -receptor antagonists 失效
标题翻译： TRICYCLIC KETONES有用作为HT3受体拮抗剂
公开(公告)号：US5202343A
公开(公告)日：1993-04-13
申请号：US887607
申请日：1992-05-22
申请人： Ian H. Coates , John Bradshaw , James A. Bell , David C. Humber , George B. Ewan , William L. Mitchell , Barry J. Price
发明人： Ian H. Coates , John Bradshaw , James A. Bell , David C. Humber , George B. Ewan , William L. Mitchell , Barry J. Price
IPC分类号： C07D403/06
CPC分类号： C07D403/06
摘要： The invention relates to compounds of the general formula (I): ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, phenylC.sub.1-3 alkyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CONR.sup.5 R.sup.6 or --SO.sub.2 R.sup.5 ;R.sup.5 and R.sup.6, which may be the same or different, each represents a hydrogen atom, a C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl group, or a phenyl or phenylC.sub.1-4 alkyl group, in which the phenyl group is optionally substituted by one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy or hydroxy groups or halogen atoms, with the proviso that R.sup.5 does not represent a hydrogen atom when R.sup.1 represents a group --CO.sub.2 R.sup.5 or --SO.sub.2 R.sup.5 ;one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;Q represents a hydrogen or a halogen atom, or a hydroxy, C.sub.1-4 alkoxy, phenylC.sub.1-3 alkoxy or C.sub.1-6 alkyl group or a group --NR.sup.7 R.sup.8 or --CONR.sup.7 R.sup.8 ;R.sup.7 and R.sup.8, which may be the same or different, each represents a hydrogen atom or a C.sub.1-4 alkyl or C.sub.3-4 alkenyl group, or together with the nitrogen atom to which they are attached form a saturated 5 to 7 membered ring;n represents 1, 2 or 3; andA-B represents the group CH--CH.sub.2 or C.dbd.CH; and physiologically acceptable salts and solvates thereof.The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety, and nausea and vomiting.
摘要翻译：本发明涉及通式（I）的化合物：其中Im表示下式的咪唑基：R1表示氢原子或选自C1-6烷基，C3-6烯基， C 3-10炔基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基，苯基C 1-3烷基，-CO 2 R 5，-COR 5，-CONR 5 R 6或-SO 2 R 5; R 5和R 6可以相同或不同，表示氢原子，C 1-6烷基或C 3-7环烷基或苯基或苯基C 1-4烷基，其中苯基任选被一个或多个C 1 -4-烷基，C 1-4烷氧基或羟基或卤素原子，条件是当R 1表示-CO 2 R 5或-SO 2 R 5基团时，R 5不表示氢原子; 由R 2，R 3和R 4表示的基团之一是氢原子或C 1-6烷基，C 3-7环烷基，C 3-6烯基，苯基或苯基C 1-3烷基，其它两个基团可以相同或不同的是氢原子或C1-6烷基; Q表示氢或卤素原子，或羟基，C 1-4烷氧基，苯基C 1-3烷氧基或C 1-6烷基或基团-NR 7 R 8或-CONR 7 R 8; R 7和R 8可以相同或不同，各自表示氢原子或C 1-4烷基或C 3-4烯基，或与它们所连接的氮原子一起形成饱和的5至7元环; n表示1,2或3; A-B表示基团CH-CH 2或C = CH; 及其生理上可接受的盐和溶剂合物。这些化合物是5-HT在5-HT 3受体上的作用的有效和选择性拮抗剂，可用于治疗精神病，焦虑和恶心和呕吐。

2. 发明授权

US4481199A 1,2,4-Triazole-3-amine and 1,2,4 triazole-3,5-diamine compounds and their pharmaceutical use 失效
标题翻译： 1,2,4-三唑-3-胺和1,2,4-三唑-3,5-二胺化合物及其药物用途
公开(公告)号：US4481199A
公开(公告)日：1984-11-06
申请号：US511234
申请日：1983-07-06
申请人： Linda Carey , Barry J. Price , John W. Clitherow , John Bradshaw , Michael Martin-Smith , David E. Bays , Philip Blatcher
发明人： Linda Carey , Barry J. Price , John W. Clitherow , John Bradshaw , Michael Martin-Smith , David E. Bays , Philip Blatcher
IPC分类号： A61K31/41 , A61K31/443 , A61K31/445 , A61P1/04 , A61P43/00 , C07D249/12 , C07D249/14 , C07D295/096 , C07D307/52 , C07D405/12 , C07D471/04 , C07D405/14
CPC分类号： C07D295/096 , C07D249/14 , C07D471/04
摘要： The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in which the substituents are defined later.The compounds 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，其中取代基定义在后面。该化合物显示出作为选择性组胺H2拮抗剂的药理学活性。

3. 发明授权

US4410523A Heterocyclic derivatives 失效
公开(公告)号：US4410523A
公开(公告)日：1983-10-18
申请号：US199522
申请日：1980-10-22
申请人： William D. Ollis , Barry J. Price , Linda Carey , Roger Hayes , John W. Clitherow , John Bradshaw , John W. M. Mackinnon
发明人： William D. Ollis , Barry J. Price , Linda Carey , Roger Hayes , John W. Clitherow , John Bradshaw , John W. M. Mackinnon
IPC分类号： C07D249/14 , A61K31/395 , C07D249/10
CPC分类号： C07D249/14 , Y10S514/927
摘要： The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichR.sub.1 and R.sub.2, which may be the same or different, each represent hydrogen, C.sub.1-10 alkyl, cycloalkyl, alkenyl, aralkyl, trifluoroalkyl, heteroaralkyl, or alkyl substituted by hydroxy, alkoxy, amino, alkylamino, dialkyamino or cycloalkyl, or R.sub.1 and R.sub.2 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 and is attached to the cyclohexadiene ring at either the 4- or 5- position;X represents --CH.sub.2 or --O--;m represents 2, 3, 4 or 5 and when X is --O-- the chain (CH.sub.2).sub.m may be interrupted by an oxygen atom provided that there are at least two methylene groups between any two heteroatoms in the moiety --X(CH.sub.2).sub.m NH--;R.sub.3 represents hydrogen, alkyl, alkenyl, aralkyl, or C.sub.2-6 alkyl substituted by hydroxy or alkoxy; andR.sub.4 represents hydrogen, alkyl, alkenyl, aralkyl, hydroxyalkyl, acyloxyalkyl, alkoxyalkyl, aryloxyalkyl, aralkyloxyalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, hydroxy or alkoxy or the group NR.sub.5 R.sub.6 whereR.sub.5 represents hydrogen, alkyl, alkyl substituted by hydroxy or C.sub.1-3 alkoxy, alkenyl, aralkyl or heteroaralkyl and R.sub.6 represents any of the groups defined for R.sub.5 or may represent the group COR.sub.7 where R.sub.7 represents hydrogen, alkyl, aryl, aralkyl, alkoxy, heteroaryl or monocyclic heteroaralkyl or R.sub.6 represents the group SO.sub.2 R.sub.8 where R.sub.8 represents alkyl or aryl, or R.sub.6 represents the group ##STR2## where Y is oxygen or sulphur and R.sub.9 represents hydrogen, alkyl, cycloalkyl, aryl or aralkyl,or R.sub.5 and R.sub.6 taken together may represent the group .dbd.CR.sub.10 R.sub.11 where R.sub.10 represents aryl or heteroaryl and R.sub.11 represents hydrogen or alkyl.The compounds show activity as selective histamine H.sub.2 -antagonists.

4. 发明授权

US4255440A Furan derivatives having selective action on histamine receptors 失效
标题翻译：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。

5. 发明授权

US4318913A 1,2,4-Triazole-3,5-diamine derivatives 失效
标题翻译： 1,2,4-三唑-3,5-二胺衍生物
公开(公告)号：US4318913A
公开(公告)日：1982-03-09
申请号：US33508
申请日：1979-04-26
申请人： John W. Clitherow , John Bradshaw , John W. M. Mackinnon , Barry J. Price , Michael Martin-Smith , Duncan B. Judd
发明人： John W. Clitherow , John Bradshaw , John W. M. Mackinnon , Barry J. Price , Michael Martin-Smith , Duncan B. Judd
IPC分类号： C07D209/48 , C07D249/14 , C07D307/52 , C07D317/12 , A61K31/445 , A61K31/41 , C07D403/12 , C07D403/14
CPC分类号： C07D209/48 , C07D249/14 , C07D307/52 , C07D317/12 , Y10S514/926 , Y10S514/927
摘要： The invention relates to compounds of the formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichR.sub.1 and R.sub.2 represent hydrogen, an aliphatic or cycloaliphatic group, or R.sub.1 and R.sub.2 together with the nitrogen atom form a 5 to 10 membered heterocyclic ring:Alk represents a straight or branched alkylene chain;Q represents furan, thiophen or benzene ring which is incorporated into the rest of the molecule;X represents --CH.sub.2 --, ##STR2## --O-- or --S-- whereR.sub.6 represents hydrogen or methyl;n represents zero, 1 or 2;m represents 2, 3 or 4;R.sub.3 represents hydrogen, a substituted or unsubstituted aliphatic or aryl group and;R.sub.4 and R.sub.5, which may be the same or different, each represent hydrogen, a substituted or unsubstituted aliphatic, aryl, or together with the nitrogen atom form a heterocyclic group.
摘要翻译：本发明涉及式（I）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表示氢，脂族或脂环族基团，或R 1和R 2与氮原子一起形成5至10元杂环：Alk表示直链或支链亚烷基链; Q表示呋喃，噻吩或苯环，其结合到分子的其余部分中; X表示-CH 2 - ， -O-或-S-，其中R 6表示氢或甲基; n表示0，1或2; m表示2,3或4; R 3表示氢，取代或未取代的脂族或芳基， R 4和R 5可以相同或不同，各自表示氢，取代或未取代的脂族基，芳基或与氮原子一起形成杂环基。

6. 发明授权

US4128658A Aminoalkyl furan derivatives 失效
标题翻译：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。

7. 发明授权

US4764612A 3-[3-[1-piperidinylmethyl]phenoxy]propanamine 失效
标题翻译： 3- [3- [1-哌啶基甲基]苯氧基]丙胺
公开(公告)号：US4764612A
公开(公告)日：1988-08-16
申请号：US826832
申请日：1986-02-06
申请人： John W. Clitherow , John Bradshaw , John W. M. Mackinnon , Barry J. Price , Michael Martin-Smith , Duncan B. Judd
发明人： John W. Clitherow , John Bradshaw , John W. M. Mackinnon , Barry J. Price , Michael Martin-Smith , Duncan B. Judd
IPC分类号： C07D209/48 , C07D249/14 , C07D307/52 , C07D317/12 , C07D295/12
CPC分类号： C07D209/48 , C07D249/14 , C07D307/52 , C07D317/12 , Y10S514/926 , Y10S514/927
摘要： The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in which the variables are as defined in the specification.The compounds of formula (I) show pharmacological activity as selective histamine H.sub.2 -antagonists.Also disclosed are intermediates in the preparation of the compounds of the formula (I).
摘要翻译：本发明涉及通式（I）化合物（Ⅰ）及其生理上可接受的盐，水合物和生物前体，其中变量如说明书中所定义。式（I）化合物显示作为选择性组胺H2拮抗剂的药理活性。还公开了制备式（I）化合物的中间体。

8. 发明授权

US4536508A Triazoleamine derivatives having histamine H.sub.2 -antagonist properties 失效
标题翻译：具有组胺H2拮抗剂性质的三唑胺衍生物
公开(公告)号：US4536508A
公开(公告)日：1985-08-20
申请号：US467896
申请日：1983-02-18
申请人： John W. Clitherow , Barry J. Price , John Bradshaw , Michael Martin-Smith , John W. M. Mackinnon , Duncan B. Judd , Roger Hayes
发明人： John W. Clitherow , Barry J. Price , John Bradshaw , Michael Martin-Smith , John W. M. Mackinnon , Duncan B. Judd , Roger Hayes
IPC分类号： C07D249/08 , A61K31/41 , A61K31/435 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/535 , A61K31/55 , A61P43/00 , C07D249/14 , C07D295/096 , C07D307/52 , C07D317/22 , C07D333/36 , C07D401/12 , C07D405/12 , C07D409/12 , C07D521/00 , C07D401/10 , C07D413/10
CPC分类号： C07D295/096 , C07D249/14 , C07D307/52 , C07D317/22 , C07D333/36
摘要： The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, which show pharmacological activity as selective histamine H.sub.2 -antagonists.
摘要翻译：本发明涉及通式（I）的化合物及其生理学上可接受的盐，水合物和生物前体，其表现出作为选择性组胺H2拮抗剂的药理学活性。

9. 发明授权

US4485104A 1,2,4-Triazole-3-amines and their pharmaceutical use 失效
标题翻译： 1,2,4-三唑-3-胺及其药物用途
公开(公告)号：US4485104A
公开(公告)日：1984-11-27
申请号：US469231
申请日：1983-02-24
申请人： John W. Clitherow , Barry J. Price , Roger Hayes , David E. Bays
发明人： John W. Clitherow , Barry J. Price , Roger Hayes , David E. Bays
IPC分类号： C07D209/48 , C07D249/14 , C07D295/096 , C07D401/04 , C07D405/12 , C07D409/12 , C07D417/12 , A61K31/41 , C07D403/12 , C07D403/14
CPC分类号： C07D209/48 , C07D249/14 , C07D295/096 , C07D401/04 , C07D405/12 , C07D409/12 , C07D417/12
摘要： Compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof have been found to show pharmacological activity as selective histamine H.sub.2 -antagonists. The substituents in the compounds of formula (I) are defined in the main body of the disclosure.
摘要翻译：已经发现通式（I）的化合物（I）及其生理上可接受的盐，水合物和生物前体已显示出作为选择性组胺H2拮抗剂的药理学活性。式（I）化合物中的取代基在本公开的主体中定义。

10. 发明授权

US4382929A Thiophene derivatives and their pharmaceutical compositions and method of use 失效
标题翻译：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。

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