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51. 发明授权

US4366164A Amine derivatives 失效
标题翻译：胺衍生物
公开(公告)号：US4366164A
公开(公告)日：1982-12-28
申请号：US213407
申请日：1980-12-05
申请人： John W. Clitherow , Barry Price , John Bradshaw , Michael Martin-Smith
发明人： John W. Clitherow , Barry 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 , C07D333/38
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 from 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 andAlk 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R 4和R 5与它们所连接的氮原子一起可以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。并且R 2表示低级烷基或基团 - （CH 2）y E（CH 2）x G，其中y表示2,3或4，或当E是-CH 2 - 基团时可另外表示0或1; x表示零，1或2; E表示-CH 2 - ， - O-或-S-; G表示单环5或6元碳环或杂环芳环; 或G表示组，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。

52. 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.

53. 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.

54. 发明授权

US4210593A Process for preparing acetylsulfaguanidine 失效
标题翻译：制备乙酰氨基胍的方法
公开(公告)号：US4210593A
公开(公告)日：1980-07-01
申请号：US902597
申请日：1978-05-04
申请人： Imre A. Halmos
发明人： Imre A. Halmos
IPC分类号： C07C311/64 , C07C143/58
CPC分类号： C07C311/64
摘要： A method suitable for the continuous preparation of acetylsulfaguanidine is described which comprises exposing a thin layer of a concentrated aqueous solution of ammonium acetylsulfanilylcyanamide to microwave radiation until essentially anhydrous ammonium acetylsulfanilylcyanamide is obtained in the form of a glassy, non-crystalline sheet, and converting the dry ammonium acetylsulfanilylcyanamide to acetylsulfaguanidine by heating.
摘要翻译：描述了一种适用于连续制备乙酰氨基胍的方法，其包括将薄层的乙酰基磺酰氨基氰胺铵水溶液的薄层暴露于微波辐射，直至得到玻璃状非结晶片形式的基本上无水的乙酰基氨基磺酰氰胺，通过加热将乙酰磺酰基氰胺干燥至乙酰氨基胍。

55. 发明授权

US2426882A Sulfonyl dicyandiamides and methods for their preparation 失效
标题翻译：磺酰双氰胺及其制备方法
公开(公告)号：US2426882A
公开(公告)日：1947-09-02
申请号：US43857342
申请日：1942-04-11
申请人： AMERICAN CYANAMID CO
发明人： KAISER DONALD W , THURSTON JACK T
IPC分类号： C07C311/64
CPC分类号： C07C311/64

56. 发明授权

US2416995A Process for the manufacture of para-aminobenzene-sulfonyl-guanidine 失效
标题翻译：制备对氨基苯磺酰基胍的方法
公开(公告)号：US2416995A
公开(公告)日：1947-03-04
申请号：US46178642
申请日：1942-10-12
申请人： CIBA PHARM PROD INC
发明人： MAX HARTMANN , VON MEYENBURG HARALD
IPC分类号： C07C311/64
CPC分类号： C07C311/64

57. 发明授权

US2331375A Method of preparing a mono-(biguanido) benzene monosulphonamide 失效
标题翻译：制备单（双胍）苯单磺酰胺的方法
公开(公告)号：US2331375A
公开(公告)日：1943-10-12
申请号：US38067041
申请日：1941-02-26
申请人： GEN ELECTRIC
发明人： D ALELIO GAETANO F
IPC分类号： C07C311/64
CPC分类号： C07C311/64

58. 发明授权

US2295884A P-substituted-benzenesulphonyl biguanides and methods for their preparation 失效
标题翻译： P-取代苯磺酰双胍及其制备方法
公开(公告)号：US2295884A
公开(公告)日：1942-09-15
申请号：US38033641
申请日：1941-02-24
申请人： AMERICAN CYANAMID CO
发明人： STANLEY WINNEK PHILIP
IPC分类号： C07C311/64
CPC分类号： C07C311/64

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