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1. 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。

2. 发明授权

US4323566A Triazole acylamines, pharmaceutical compositions thereof and method of use thereof 失效
公开(公告)号：US4323566A
公开(公告)日：1982-04-06
申请号：US125847
申请日：1980-02-29
申请人： John W. Clitherow , Barry J. Price , John Bradshaw , Michael Martin-Smith , John W. M. MacKinnon , Duncan B. Judd , Linda Carey
发明人： John W. Clitherow , Barry J. Price , John Bradshaw , Michael Martin-Smith , John W. M. MacKinnon , Duncan B. Judd , Linda Carey
IPC分类号： C07D249/14 , C07D295/096 , C07D307/52 , C07D317/22 , C07D333/36 , C07D403/12 , A61K31/41 , C07D403/14
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, in whichR.sub.1 and R.sub.2, which may be the same of different, each represent hydrogen, C.sub.1 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, trifluoroalkyl, or alkyl substituted by hydroxy, alkoxy, amino alkylamino dialkylamino 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 which is oxygen or sulphur;Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms,Q represents a furan or thiophene ring in which incorporation into the rest of the molecule is through bonds at the 2- and 5- positions, the furan ring optionally bearing a further substituent R.sub.6 adjacent to the group R.sub.1 R.sub.2 N-Alk, or Q represents 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;R.sub.6 represents halogen or C.sub.1-4 alkyl which may be substituted by hydroxy or C.sub.1-4 alkoxy;x represents --CH.sub.2 --, --O--, --S--or ##STR2## where R.sub.5 represents hydrogen or methyl; n represents zero, 1 or 2;m represents 2, 3 or 4;R.sub.3 represents hydrogen, alkyl, alkenyl, aralkyl, hydroxyalkyl with at least two carbon atoms, alkoxyalkyl, or aryl, andR.sub.4 represents hydrogen, alkyl, alkenyl or aralkyl and R.sub.7 represents the group COR.sub.8 where R.sub.8 represents hydrogen, alkyl, aryl, aralkyl, alkoxy, heteroaryl or monocyclic heteroarylalkyl or R.sub.7 represents the group SO.sub.2 R.sub.9 where R.sub.9 represents alkyl or aryl, or R.sub.7 represents the group ##STR3## where Y is oxygen or sulphur and R.sub.10 represents hydrogen, alkyl, cycloalkyl, aryl or aralkyl.The compounds of formula (I) show pharmacological activity as selective histamine H.sub.2 - antagonists.

3. 发明授权

US4442110A 1H-1,2,4-Triazole-3,5-diamine derivatives and use as selective histamine H.sub.2 -antagonists 失效
公开(公告)号：US4442110A
公开(公告)日：1984-04-10
申请号：US324440
申请日：1981-11-24
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 , A01N43/64
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 whichR.sub.1 and R.sub.2, which may be the same or different, each represent hydrogen, C.sub.1-10 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, trifluoroalkyl or alkyl substituted by hydroxy, alkoxy, amino, alkylamino, dialkylamino 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 alicyclic heterocyclic 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;Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms;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, the furan ring optionally bearing a further substituent R.sub.7 adjacent to the group R.sub.1 R.sub.2 N-Alk-, or Q represents 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;R.sub.7 represents halogen or C.sub.1-4 alkyl which may be substituted by hydroxy or C.sub.1-4 alkoxy;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, alkyl, alkenyl, aralkyl, hydroxyalkyl having at least two carbon atoms, alkoxyalkyl or aryl; andR.sub.4 and R.sub.5, which may be the same or different, each represent hydrogen, alkyl, alkyl substituted by hydroxy or C.sub.1-3 alkoxy, alkenyl, aralkyl or heteroaralkyl or R.sub.4 and R.sub.5 may together with the nitrogen atom to which they are attached form a 5 to 7-membered saturated heterocyclic ring which may contain another heteroatom, or the group ##STR3## or R.sub.4 and R.sub.5 taken together may represent the group .dbd.CR.sub.8 R.sub.9 where R.sub.8 represents aryl or heteroaryl and R.sub.9 represents hydrogen or alkyl.Preferably when X represents an oxygen atom or ##STR4## and n is zero, then Q only represents a benzene ring. The compounds of formula (I) show pharmacological activity as selective histamine H.sub.2 -antagonists.

4. 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。

5. 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。

6. 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。

7. 发明授权

US4317819A Amine derivatives 失效
标题翻译：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。

8. 发明授权

US4524071A Pyrimidone derivatives 失效
标题翻译：嘧啶衍生物
公开(公告)号：US4524071A
公开(公告)日：1985-06-18
申请号：US58256
申请日：1979-07-17
申请人： Barry J. Price , John W. Clitherow , John Bradshaw , Michael Martin-Smith , Duncan B. Judd , Roger Hayes
发明人： Barry J. Price , John W. Clitherow , John Bradshaw , Michael Martin-Smith , Duncan B. Judd , Roger Hayes
IPC分类号： A61K31/505 , A61P27/16 , A61P29/00 , A61P37/08 , C07D213/65 , C07D215/12 , C07D239/46 , C07D239/47 , C07D239/56 , C07D307/52 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/12 , C07D405/14 , C07D409/14
CPC分类号： C07D239/47 , C07D213/65 , C07D215/12 , C07D239/56 , C07D307/52
摘要： Compounds of the formula (I) ##STR1## in which R.sub.1 and R.sub.2 each may represent hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, or alkyl, substituted by hydroxy, C.sub.1-3 alkoxy, amino, C.sub.1-3 alkylamino or di-C.sub.1-3 alkylamino or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form an alicyclic heterocyclic ring which 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 are described.Alk is a straight lower alkylene chain,Q is a furan or thiophen ring, the furan ring optionally bearing a further substituent R.sub.5 adjacent to the group R.sub.1 R.sub.2 NAlk-- or Q represents a benzene ring.R.sub.5 represents halogen or C.sub.1-3 alkyl which may be substituted by a hydroxy or C.sub.1-3 alkoxy group;X represents --CH.sub.2 --, --O-- or --S--;n represents zero or 1;m represents 2, 3 or 4;Y represents .dbd.O or .dbd.S;R.sub.3 represents hydrogen in which case R.sub.4 represents methyl or R.sub.3 represents --(CH.sub.2).sub.p V(CH.sub.2).sub.q Ar, phenyl, or alkyl in which case R.sub.4 represents hydrogen;V represents --CH.sub.2 --, --O--, or --S--;p represents zero, 1, 2 or 3;q represents zero, 1, 2 or 3;the sum of p+q being 3 or less;Ar represents an aromatic carbocyclic or heterocyclic ring being optionally substituted by at least one C.sub.1-3 alkyl, C.sub.1-3 alkoxy C.sub.1-3 alkyl, hydroxy, C.sub.1-3 alkoxy, methylenedioxy, halogen, trifluoromethyl or di-C.sub.1-3 alkylamino group;except that when n is zero and X is oxygen then Q represents a benzene or thiophen ring. The compounds of formula (I) have pharmacological activity as selective histamine H.sub.2 -antagonists.
摘要翻译：式（I）的化合物其中R 1和R 2各自可以表示被羟基，C 1-3烷氧基，氨基，C 1-3取代的氢，烷基，环烷基，烯基，炔基，芳烷基或烷基烷基氨基或二-C 1-3烷基氨基或R 1和R 2与它们所连接的氮原子一起形成脂环族杂环，其可以是未取代的或可以被一个或多个C 1-3烷基或羟基和/ 或可以含有另外的杂原子。 Al是直链亚烷基链，Q是呋喃或噻吩环，呋喃环任选带有与R1R2NAlk-基团相邻的另外的取代基R5，或Q表示苯环。 R5表示可被羟基或C1-3烷氧基取代的卤素或C1-3烷基; X表示-CH 2 - ， - O-或-S-; n表示0或1; m表示2,3或4; Y表示= O或= S; R 3表示氢，在这种情况下，R 4表示甲基或R 3表示 - （CH 2）p V（CH 2）qAr，苯基或烷基，在这种情况下，R 4表示氢; V表示-CH 2 - ， - O-或-S-; p代表零，1,2或3; q表示零，1,2或3; p + q的和为3以下; Ar表示任选被至少一个C 1-3烷基，C 1-3烷氧基C 1-3烷基，羟基，C 1-3烷氧基，亚甲二氧基，卤素，三氟甲基或二-C 1-3烷基氨基取代的芳族碳环或杂环; 除了当n为0且X为氧时，Q表示苯或噻吩环。式（I）化合物具有作为选择性组胺H2拮抗剂的药理学活性。

9. 发明授权

US4279911A Amine derivatives and pharmaceutical compositions containing them 失效
标题翻译：胺衍生物和含有它们的药物组合物
公开(公告)号：US4279911A
公开(公告)日：1981-07-21
申请号：US157203
申请日：1980-06-06
申请人： Michael Martin-Smith , Barry J. Price , John Bradshaw , John W. Clitherow
发明人： Michael Martin-Smith , Barry J. Price , John Bradshaw , John W. Clitherow
IPC分类号： A61K31/34 , A61K31/341 , A61K31/345 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/495 , A61K31/505 , A61P1/04 , C07C67/00 , C07C209/00 , C07C209/60 , C07C211/29 , C07C217/48 , C07C261/04 , C07C275/32 , C07C301/00 , C07C303/36 , C07C303/40 , C07C311/64 , C07C313/00 , C07C323/29 , C07C323/44 , C07C323/47 , C07C323/48 , C07C325/00 , C07C335/08 , C07D209/48 , C07D213/32 , C07D295/096 , C07D307/28 , C07D307/38 , C07D307/52 , C07D333/20 , C07D405/12 , C07D409/12 , A61K31/44 , C07D213/58 , C07D307/54
CPC分类号： C07D209/48 , C07D213/32 , C07D295/096 , C07D307/52 , C07D333/20 , Y10S514/826 , Y10S514/887 , Y10S514/925 , Y10S514/926 , Y10S514/927
摘要： The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, N-oxides, hydrates and bioprecursors thereof, in which Y represents .dbd.O, .dbd.S, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 represents hydrogen, nitro, cyano, lower alkyl, aryl, lower alkylsulphonyl or arylsulphonyl; R.sub.1 and R.sub.2, which may be the same or different, each represent hydrogen lower alkyl, cycloalkyl, lower alkenyl, aralkyl, hydroxy, lower trifluoroalkyl, lower alkyl substituted by hydroxy, lower alkoxy, amine, lower alkylamino or dialkylamino, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring which may contain other heteroatoms or the group ##STR2## where R.sub.4 represents hydrogen or lower alkyl;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, 1 or 2;m represents 2, 3 or 4;Alk represents a straight chain alkylene group of 1 to 3 carbon atoms; (except that n is not zero when X is oxygen and Q is a furan or thiophen ring system);q represents 2, 3 or 4 or can additionally represent zero or 1 when E is a --CH.sub.2 -group;p represents zero, 1 or 2;E represents --CH.sub.2 --, --O-- or --S--; andZ represents a monocyclic 5 or 6 membered carbocyclic or heterocyclic aromatic ring which may be optionally substituted by one or more groups or Z 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.5 and R.sub.6, which may be the same or different, each represent any of the groups defined for R.sub.1 and R.sub.2 ; (except that p is not zero when E is oxygen and Q' or Z is a furan or thiophen ring system).The compounds of formula (I) show pharmacological activity as selective histamine H.sub.2 -antagonists.

10. 发明授权

US4233302A Amine derivatives and pharmaceutical compositions containing them 失效
公开(公告)号：US4233302A
公开(公告)日：1980-11-11
申请号：US970534
申请日：1978-12-18
申请人： Michael Martin-Smith , Barry J. Price , John Bradshaw , John W. Clitherow
发明人： Michael Martin-Smith , Barry J. Price , John Bradshaw , John W. Clitherow
IPC分类号： A61K31/34 , A61K31/341 , A61K31/345 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/495 , A61K31/505 , A61P1/04 , C07C67/00 , C07C209/00 , C07C209/60 , C07C211/29 , C07C217/48 , C07C261/04 , C07C275/32 , C07C301/00 , C07C303/36 , C07C303/40 , C07C311/64 , C07C313/00 , C07C323/29 , C07C323/44 , C07C323/47 , C07C323/48 , C07C325/00 , C07C335/08 , C07D209/48 , C07D213/32 , C07D295/096 , C07D307/28 , C07D307/38 , C07D307/52 , C07D333/20 , C07D405/12 , C07D409/12 , A61K31/44 , C07D213/58 , C07D307/54
CPC分类号： C07D209/48 , C07D213/32 , C07D295/096 , C07D307/52 , C07D333/20 , Y10S514/826 , Y10S514/887 , Y10S514/925 , Y10S514/926 , Y10S514/927
摘要： The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, N-oxides, hydrates and bioprecursors thereof, in whichY represents .dbd.O, .dbd.S, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 represents hydrogen, nitro, cyano, lower alkyl, aryl, lower alkylsulphonyl or arylsulphonyl;R.sub.1 and R.sub.2, which may be the same or different, each represent hydrogen lower alkyl, cycloalkyl, lower alkenyl, aralkyl, hydroxy, lower trifluoroalkyl, lower alkyl substituted by hydroxy, lower alkoxy, amine, lower alkylamino or dialkylamino, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring which may contain other heteroatoms or the group ##STR2## where R.sub.4 represents hydrogen or lower alkyl; 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, 1 or 2;m represents 2, 3 or 4;Alk represents a straight chain alkylene group of 1 to 3 carbon atoms; (except that n is not zero when X is oxygen and Q is a furan or thiophen ring system)q represents 2, 3 or 4 or can additionally represent zero or 1 when E is a --CH.sub.2 -group;p represents zero, 1 or 2;E represents --CH.sub.2 --, --O-- or --S--; andZ represents a monocyclic 5 or 6 membered carbocyclic or heterocyclic aromatic ring which may be optionally substituted by one or more groups or Z represents the group ##STR3## where Q' represents any of the rings defined for Q; Alk' represents any of the groups defined for Alk; andR.sub.5 and R.sub.6, which may be the same or different, each represent any of the groups defined for R.sub.1 and R.sub.2 ; (except that p is not zero when E is oxygen and Q' or Z is a furan or thiophen ring system).The compounds of formula (I) show pharmacological activity as selective histamine H.sub.2 -antagonists.

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