公开(公告)号：US5510350A

公开(公告)日：1996-04-23

申请号：US237297

申请日：1994-05-03

申请人： Alexander W. Oxford ,  William L. Mitchell ,  John Bradshaw ,  John W. Clitherow ,  Malcolm Carter

发明人： Alexander W. Oxford ,  William L. Mitchell ,  John Bradshaw ,  John W. Clitherow ,  Malcolm Carter

IPC分类号： A61K31/495 ,  A61K20060101 ,  A61K31/165 ,  A61K31/41 ,  A61K31/496 ,  A61K31/53 ,  A61P5/00 ,  A61P9/12 ,  A61P15/10 ,  A61P25/00 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  C07D20060101 ,  C07D249/04 ,  C07D249/06 ,  C07D249/08 ,  C07D249/14 ,  C07D271/06 ,  C07D271/07 ,  C07D271/08 ,  C07D271/10 ,  C07D271/107 ,  C07D285/06 ,  C07D285/08 ,  C07D285/10 ,  C07D285/12 ,  C07D285/125 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

CPC分类号： C07D249/08 ,  C07D249/06 ,  C07D271/06 ,  C07D271/07 ,  C07D271/107 ,  C07D285/06 ,  C07D285/08 ,  C07D285/12

摘要： The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt or solvate thereof wherein R.sup.1 represents a hydrogen atom or a halogen atom or a group selected from C.sub.1-6 alkyl and C.sub.1-6 alkoxy;R.sup.2 represents a phenyl group substituted by a group selected from ##STR2## and optionally further substituted by one or two substituents selected from halogen atoms, C.sub.1-6 alkoxy, hydroxy, and C.sub.1-6 alkyl;R.sup.3 represents the group ##STR3## R.sup.4 and R.sup.5, which may be the same or different, each independently represent a hydrogen atom or a halogen atom or a group selected from hydroxy, C.sub.1-6 alkoxy and C.sub.1-6 alkyl;R.sup.6 represents a hydrogen atom or a group selected from --NR.sup.9 R.sup.10 and a C.sub.1-6 alkyl group optionally substituted by one or two substituents selected from C.sub.1-6 alkoxy, hydroxy, C.sub.1-6 acyloxy and --SO.sub.2 R.sup.11 ;R.sup.7, R.sup.8 and R.sup.9, which may be the same or different, each independently represent a hydrogen atom or a C.sub.1-6 alkyl group;R.sup.10 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.1-6 acyl, benzoyl and --SO.sub.2 R.sup.11 ;R.sup.11 represents a C.sub.1-6 alkyl group or a phenyl group;Z represents an oxygen atom or a group selected from NR.sup.8 and S(O).sub.k ; andk represents zero, 1 or 2.The compounds may be used in the treatment or prophylaxis of depression and other CNS disorders.

摘要翻译： 本发明提供式（I）化合物：其中R 1表示氢原子或卤素原子或选自C 1-6烷基和C 1-6烷氧基的基团;或其生理学上可接受的盐或溶剂化物。 R 2表示被选自下列基团取代的苯基，并任选进一步被一个或两个选自卤素原子，C 1-6烷氧基，羟基和C 1-6烷基的取代基取代; R 3表示基团R 4和R 5可以相同或不同，各自独立地表示氢原子或卤素原子或选自羟基，C 1-6烷氧基和C 1-6烷基的基团。 R6表示氢原子或选自-NR9R10和任选被一个或两个选自C 1-6烷氧基，C 1-6酰氧基和-SO 2 R 11的取代基取代的C 1-6烷基的基团; R 7，R 8和R 9可以相同或不同，各自独立地表示氢原子或C 1-6烷基; R 10表示氢原子或选自C 1-6烷基，C 1-6酰基，苯甲酰基和-SO 2 R 11的基团; R11表示C1-6烷基或苯基; Z表示氧原子或选自NR8和S（O）k的基团; 并且k代表0,1或2.化合物可用于治疗或预防抑郁症和其它CNS疾病。

公开(公告)号：US4939144A

公开(公告)日：1990-07-03

申请号：US260680

申请日：1988-10-21

申请人： Ian H. Coates ,  David C. Humber ,  James A. Bell ,  George B. Ewan ,  Alexander W. Oxford ,  William L. Mitchell

发明人： Ian H. Coates ,  David C. Humber ,  James A. Bell ,  George B. Ewan ,  Alexander W. Oxford ,  William L. Mitchell

IPC分类号： A61K31/415 ,  A61P1/00 ,  A61P1/08 ,  A61P25/00 ,  A61P25/04 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D521/00

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06

摘要： The invention relates to ketones of the general formula (I): ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## one of the groups represented by R.sup.1, R.sup.2 and R.sup.3 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenyl C.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;n represents 1, 2 or 3;Q represents a hydrogen atom, a halogen atom, or a hydroxy, C.sub.1-4 alkoxy, phenyl C.sub.1-3 alkoxy or C.sub.1-6 alkyl group, or a group --NR.sup.4 R.sup.5 or --CONR.sup.4 R.sup.5, (wherein R.sup.4 and R.sup.5, 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);and X represents an oxygen or a sulphur atom, or, when Im represents an imidazolyl group of formula (c) and n represents 1 or 3, X may also represent the group NR.sup.6, wherein R.sup.6 represents a hydrogen atom or a group selected from C.sub.1-10 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, phenyl, phenyl C.sub.1-3 alkyl, --CO.sub.2 R.sup.7, --COR.sup.7, --CONR.sup.7 R.sup.8 or --SO.sub.2 R.sup.7 (wherein R.sup.7 and R.sup.8, 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 phenyl C.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.7 does not represent a hydrogen atom when R.sup.6 represents a group --CO.sub.2 R.sup.7); and physiologically acceptable salts and solvates thereof.The compounds are potent and selective antagonists of the effect of 5-HT and 5-HT.sub.3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety, and nausea and vomiting.

公开(公告)号：US4324792A

公开(公告)日：1982-04-13

申请号：US193846

申请日：1980-10-03

申请人： John Bradshaw ,  Alexander W. Oxford ,  David I. C. Scopes

发明人： John Bradshaw ,  Alexander W. Oxford ,  David I. C. Scopes

IPC分类号： A61K31/415 ,  A61P43/00 ,  C07D231/12 ,  C07D233/54 ,  C07D233/64 ,  C07D403/06 ,  A61K31/445

CPC分类号： C07D233/64 ,  C07C255/00

摘要： The present invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts and bioprecursors thereof in which ##STR2## represents either ##STR3## R.sup.1 represents hydrogen, halogen, C.sub.1-4 alkoxy, hydroxy, alkyl, R.sup.4 CH(OH)--, cyano or R.sup.5 CONH--, R.sup.2 and R.sup.3, which may be the same or different, each represents a straight or branched chain alkyl group or alkenyl group or R.sup.2 and R.sup.3 may, together with the nitrogen atom to which they are attached, form a saturated heterocyclic ring containing from 5 to 7 members which may optionally contain an oxygen atom; R.sup.4 represents hydrogen or alkyl; and R.sup.5 represents hydrogen, alkyl or C.sub.1-4 alkoxy. The compounds have been shown to exhibit H.sub.1 -antagonist activity in standard pharmacological tests.

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和生物前体，其中R 1表示氢，卤素，C 1-4烷氧基，羟基，烷基，R 4 CH （OH） - ，氰基或R 5 CONH - ，R 2和R 3可以相同或不同，表示直链或支链烷基或烯基，或者R 2和R 3可以与它们所连接的氮原子一起 形成含有5至7个可任意含有氧原子的饱和杂环; R4表示氢或烷基; R5代表氢，烷基或C1-4烷氧基。 化合物已被证明在标准药理学试验中显示出H1拮抗剂活性。

公开(公告)号：US4316907A

公开(公告)日：1982-02-23

申请号：US163568

申请日：1980-06-27

申请人： Alexander W. Oxford ,  John Bradshaw ,  Ian H. Coates

发明人： Alexander W. Oxford ,  John Bradshaw ,  Ian H. Coates

IPC分类号： A61K31/38 ,  A61K31/381 ,  A61P9/12 ,  A61P25/02 ,  C07D333/38 ,  C07D333/24

CPC分类号： C07D333/38 ,  Y10S514/913

摘要： Thiophene carboxamides are described of general formula I ##STR1## in which the amide function is in the 2- or 3-position on the thiophene ring, R.sub.1 to R.sub.5 inclusive are hydrogen atoms or lower alkyl groups, X is --CH.sub.2 --, --O-- or --NR.sub.6 -- where R.sub.6 is hydrogen or a lower alkyl group, n is a number from 0 to 3 and Ar is an optionally substituted phenyl groupand their physiologically acceptable salts.The compounds have been found to lower blood pressure in animals and to exhibit a blocking action at .beta.-adrenoreceptors and their use is indicated for the treatment of cardiovascular disorders such as hypertension and angina. Some of the compounds also exhibit a blocking action on .alpha.-adrenoreceptors and their use is indicated for the treatment of hypertention.

摘要翻译： 噻吩甲酰胺描述为通式I ，其中酰胺官能团位于噻吩环上的2-或3-位，R 1至R 5包括氢原子或低级烷基，X为-CH 2 - ， - O - 或-NR 6 - ，其中R 6是氢或低级烷基，n是0-3的数，Ar是任选取代的苯基及其生理上可接受的盐。 已经发现这些化合物降低动物血压并在β-肾上腺素受体上表现出阻断作用，并且它们用于治疗心血管疾病如高血压和心绞痛。 一些化合物还对α-肾上腺素受体表现出阻断作用，并且其用途用于治疗高血压。

公开(公告)号：US07528157B2

公开(公告)日：2009-05-05

申请号：US11615024

申请日：2006-12-22

申请人： Alexander W. Oxford ,  Richard J. Davis ,  Robert A. Coleman ,  Kenneth L. Clark ,  David E. Clark ,  Neil V. Harris ,  Garry Fenton ,  George Hynd ,  Keith A. J. Stuttle ,  Jonathan M. Sutton ,  Christopher G. Newton

发明人： Alexander W. Oxford ,  Richard J. Davis ,  Robert A. Coleman ,  Kenneth L. Clark ,  David E. Clark ,  Neil V. Harris ,  Garry Fenton ,  George Hynd ,  Keith A. J. Stuttle ,  Jonathan M. Sutton ,  Christopher G. Newton

IPC分类号： C07D307/68 ,  C07D405/10 ,  A61K31/34 ,  A61K31/443

CPC分类号： C07D307/54 ,  A61K31/34 ,  A61K31/341 ,  A61K31/4155 ,  A61K31/443 ,  C07D307/64 ,  C07D307/68 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

摘要： Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(═O), S(═O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(═O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.

摘要翻译： 式（I）化合物：其中：R2是H或任选取代的C 1-4烷基; Y是 - （CH 2）n X-，其中n是1或2，X是O，S，S（-O），S（-O）2或NRN1，其中RN1选自H或任选取代的C1- 4烷基或Y是-C（-O）NRN 2 - ，其中RN 2选自H，和任选取代的C 1-7烷基或C 5-20芳基; R3是与另外任意取代的C 6芳基连接的任意取代的C6芳基，其中如果两个C 6芳基都是苯环，则两个环之间可能有一个氧桥，与两个环上的连接相邻; A是单键或C1-3亚烷基; 并且R 5是：（i）羧基; （ii）式（II）的基团：（iii）式（III）的基团：其中R是任选取代的C 1-7烷基，C 5-20芳基或NRN 3 R N 4，其中RN 3和RN 4独立地选自任选取代的C 1 -4-烷基; （ⅳ）四唑-5-基。

公开(公告)号：US5618827A

公开(公告)日：1997-04-08

申请号：US307567

申请日：1994-09-21

申请人： Alexander W. Oxford

发明人： Alexander W. Oxford

IPC分类号： C07D413/12 ,  A61K31/445 ,  C07D413/10 ,  C07D417/10

CPC分类号： C07D413/12

摘要： Substituted phenylcarbamates and ureas of formula (I) ##STR1## wherein R.sup.1 represents a hydrogen or a halogen atom, or a C.sub.1-6 alkyl, C.sub.1-6 alkoxy or hydroxy group;R.sup.2 represents an oxadiazole or thiadiazole ring substituted by a group selected from C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, --CH.sub.2 C.sub.2-5 alkenyl, --CH.sub.2 C.sub.2-5 alkynyl, phenyl or benzyl;X represents NH or an oxygen atom;m represents zero, 1 or 2;R.sup.3 represents C.sub.1-6 alkyl, benzyl, --(CH.sub.2).sub.n R.sup.4 or ##STR2## R.sup.4 represents a group selected from cyano, hydroxyl, C.sub.1-6 alkoxy, phenoxy, C(O)C.sub.1-6 alkyl, C(O)C.sub.6 H.sub.5, --CONR.sup.6 R.sup.7, --NR.sup.6 COR.sup.7, --SO.sub.2 NR.sup.6 R.sup.7 or --NR.sup.6 SO.sub.2 R.sup.7 (wherein each of R.sup.6 and R.sup.7 independently represent a hydrogen atom, a C.sub.1-6 alkyl or phenyl group);n represents 2 or 3;R.sup.5 represents COR.sup.8 or SO.sub.2 R.sup.8 (wherein R.sup.8 represents a hydrogen atom, a C.sub.1-6 alkyl or phenyl group);and quaternary ammonium derivatives, piperidine N-oxides and pharmaceutically acceptable salts and solvates thereof; which compounds are potent and specific antagonists of 5-hydroxytryptamine (5HT; serotonin).

摘要翻译： PCT No.PCT / EP93 / 00799 Sec。 371日期1994年9月21日 102（e）1994年9月21日PCT 1993年3月26日PCT公布。 WO93 / 20071 PCT出版物 日期：1993年10月14日式（I）的取代的苯基氨基甲酸酯和脲其中R 1表示氢或卤素原子，或C 1-6烷基，C 1-6烷氧基或羟基; R2代表被选自C1-6烷基，C3-7环烷基，-CH2C2-5烯基，-CH2C2-5炔基，苯基或苄基的基团取代的恶二唑或噻二唑环; X表示NH或氧原子; m表示0，1或2; R3代表C1-6烷基，苄基， - （CH2）nR4或R4代表选自氰基，羟基，C1-6烷氧基，苯氧基，C（O）C1-6烷基，C（O）C6H5，-CONR6R7， -NR6COR7，-SO2NR6R7或-NR6SO2R7（其中R6和R7各自独立地表示氢原子，C1-6烷基或苯基）; n表示2或3; R5表示COR8或SO2R8（其中R8表示氢原子，C1-6烷基或苯基）; 和季铵衍生物，哌啶N-氧化物及其药学上可接受的盐和溶剂合物; 哪些化合物是5-羟色胺（5HT; 5-羟色胺）的有效和特异性的拮抗剂。

公开(公告)号：US5221687A

公开(公告)日：1993-06-22

申请号：US934307

申请日：1992-08-25

申请人： Ian H. Coates ,  Alexander W. Oxford ,  Peter C. North ,  Michael B. Tyers

发明人： Ian H. Coates ,  Alexander W. Oxford ,  Peter C. North ,  Michael B. Tyers

IPC分类号： A61K31/00 ,  A61K31/445 ,  A61K31/55

CPC分类号： A61K31/00 ,  A61K31/445 ,  A61K31/55

摘要： The invention relates to the use of compounds of formula (I) ##STR1## wherein Im represents an imidazolyl group of formula: ##STR2## and 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, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CONR.sup.5 R.sup.6 or --SO.sub.2 R.sup.5 (wherein 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 R4 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;and n represents 2 or 3,and physiologically acceptable salts and solvates thereof for the manufacture of a medicament for the treatment of depression.

摘要翻译： 本发明涉及式（I）化合物其中Im表示下式的咪唑基，R1表示氢原子或选自C 1-6烷基，C 3-6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，苯基甲氧基甲基，苯氧基乙基，苯氧基甲基，-CO 2 R 5，-COR 5，-CONR 5 R 6或-SO 2 R 5（其中R 5和R 6可以相同或不同 各自表示氢原子，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，代表氢原子或C1-6烷基; 和n表示2或3，以及其生理上可接受的盐和溶剂合物，用于制备用于治疗抑郁症的药物。

公开(公告)号：US4739072A

公开(公告)日：1988-04-19

申请号：US888254

申请日：1986-07-23

申请人： Alexander W. Oxford ,  Colin D. Eldred ,  Ian H. Coates ,  James A. Bell ,  David C. Humber ,  George B. Ewan

发明人： Alexander W. Oxford ,  Colin D. Eldred ,  Ian H. Coates ,  James A. Bell ,  David C. Humber ,  George B. Ewan

IPC分类号： C07D403/06 ,  A61K31/415 ,  C07C221/00 ,  C07C225/14 ,  C07D233/60 ,  C07D233/61 ,  C07D521/00 ,  C07D403/00

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

摘要： The invention relates to a process for the preparation of a compound of general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-(C.sub.1-4)alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-(C.sub.1-3)alkyl group, and 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.2-6 alkenyl or phenyl-(C.sub.1-3)alkyl group and each of the other two groups, which may be the same or different, represent a hydrogen atom or a C.sub.1-6 alkyl group;or a salt or protected derivative thereof, by cyclization of a compound of general formula (II) ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined above, or a salt or a protected derivative thereof.The compounds of formula (I) are potent and selective antagonists at "neuronal" 5-hydroxytryptamine receptors.

摘要翻译： 本发明涉及一种制备通式（I）化合物的方法，其中R1表示氢原子或C1-10烷基，C3-7环烷基，C3-7环烷基 - （C1- 4）烷基，C 3-6烯基，C 3-10炔基，苯基或苯基 - （C 1-3）烷基，并且由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 2-6烯基或苯基 - （C 1-3）烷基，其它可以相同或不同的两个基团表示氢原子或C 1-6烷基; 或其盐或被保护的衍生物，通过使通式（II）化合物（II）其中R 1，R 2，R 3和R 4如上所定义的化合物或其盐或其保护的衍生物环化。 式（I）化合物是“神经元”5-羟色胺受体的有效和选择性拮抗剂。

公开(公告)号：US4140713A

公开(公告)日：1979-02-20

申请号：US873765

申请日：1978-01-31

申请人： Alexander W. Oxford ,  Ian H. Coates

发明人： Alexander W. Oxford ,  Ian H. Coates

IPC分类号： A61K31/165 ,  A61P25/02 ,  C07C67/00 ,  C07C231/00 ,  C07C231/02 ,  C07C231/06 ,  C07C231/12 ,  C07C237/30 ,  C07C301/00 ,  C07C303/40 ,  C07C311/08 ,  C07C313/00 ,  C07D295/112 ,  C07D295/135 ,  C07C91/06 ,  C07C143/78 ,  C07C143/80

CPC分类号： C07D295/112 ,  C07D295/135

摘要： Compounds of the general formula: ##STR1## and non-toxic physiologically acceptable salts thereof, in which R.sub.1 is a halogen atom or a group NR.sub.2 R.sub.3 ;R.sub.2 and R.sub.3, which may be the same or different, are hydrogen or (C.sub.1 -C.sub.6) straight or branched chain alkyl or R.sub.2 and R.sub.3 may, together with the nitrogen atom, form a 5 or 6 membered heterocyclic ring which may contain a further hetero atom selected from O, N or S; or R.sub.2 may be hydrogen and R.sub.3 may by group R.sub.4 CO or R.sub.4 SO.sub.2 where R.sub.4 is hydrogen or alkyl (C.sub.1-4);R.sub.5 is hydrogen or one or more halogen atoms or hydroxy or alkoxy (C.sub.1-4) groups; andX is CH.sub.2, O or a group NR.sub.6 where R.sub.6 is hydrogen or alkyl (C.sub.1-4). These compounds block .beta.-adrenoreceptors.

摘要翻译： 其中R 1为卤素原子或NR 2 R 3基团的通式为：其无毒生理学上可接受的盐; R2和R3可以相同或不同，是氢或（C1-C6）直链或支链烷基或R2和R3可以与氮原子一起形成5或6元杂环，其可以含有另外 选自O，N或S的杂原子; 或R 2可以是氢，R 3可以通过R4CO或R4SO2，其中R4是氢或烷基（C1-4）; R5是氢或一个或多个卤素原子或羟基或烷氧基（C1-4）基团; 并且X是CH 2，O或NR 6，其中R 6是氢或烷基（C 1-4）。 这些化合物阻断β-肾上腺素受体。

公开(公告)号：US07196089B2

公开(公告)日：2007-03-27

申请号：US10766030

申请日：2004-01-29

申请人： Alexander W. Oxford ,  Richard J. Davis ,  Robert A. Coleman ,  Kenneth L. Clark ,  David E. Clark ,  Neil V. Harris ,  Garry Fenton ,  George Hynd ,  Keith A. J. Stuttle ,  Jonathan M. Sutton ,  Christopher G. Newton

发明人： Alexander W. Oxford ,  Richard J. Davis ,  Robert A. Coleman ,  Kenneth L. Clark ,  David E. Clark ,  Neil V. Harris ,  Garry Fenton ,  George Hynd ,  Keith A. J. Stuttle ,  Jonathan M. Sutton ,  Christopher G. Newton

IPC分类号： A61K31/341 ,  A61K31/443 ,  A61K31/506 ,  C07D239/34 ,  C07D405/10 ,  C07D307/91 ,  C07D307/68

CPC分类号： C07D307/54 ,  A61K31/34 ,  A61K31/341 ,  A61K31/4155 ,  A61K31/443 ,  C07D307/64 ,  C07D307/68 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

摘要： Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(═O), S(═O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(═O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): or (iii) a group of formula (III):  wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.

摘要翻译： 式（I）的化合物：