公开(公告)号：US4672067A

公开(公告)日：1987-06-09

申请号：US625648

申请日：1984-06-28

申请人： Ian H. Coates ,  Keith Mills ,  Colin F. Webb ,  Michael D. Dowle ,  David E. Bays

发明人： Ian H. Coates ,  Keith Mills ,  Colin F. Webb ,  Michael D. Dowle ,  David E. Bays

IPC分类号： C07D209/14 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/404 ,  A61P9/00 ,  A61P25/04 ,  C07D209/16 ,  C07D209/48 ,  C07D471/04

CPC分类号： C07D209/16

摘要： Compounds are disclosed of formula (I) ##STR1## wherein R.sub.1 represents CHO, COR.sub.8, CO.sub.2 R.sub.8, CONR.sub.9 R.sub.10, CSNR.sub.9 R.sub.10 or SO.sub.2 NR.sub.9 R.sub.10, whereR.sub.8 represents alkyl, cycloalkyl, aryl or aralkyl,R.sub.9 represents hydrogen or alkyl, andR.sub.10 represents hydrogen or alkyl, cycloalkyl, aryl or aralkyl;R.sub.2, R.sub.3, R.sub.4, R.sub.6 and R.sub.7 each independently represents hydrogen or C.sub.1-3 alkyl;R.sub.5 represents hydrogen, or alkyl, cycloalkyl, alkenyl or aralkyl, orR.sub.4 and R.sub.5 together form an aralkylidene group or R.sub.4 and R.sub.5 together with the attached nitrogen atom form a saturated monocyclic 5- to 7-membered ring; andAlk represents C.sub.2-3 alkylene chain optionally substituted by not more than two C.sub.1-3 alkyl groups;and physiologically acceptable salts and solvates thereof. The compounds are potentially useful for the treatment of migraine and may be formulated as pharmaceutical compositions in conventional manner using pharmaceutically acceptable carriers or excipients. The compounds may be prepared by, for example, reaction of an aminoalkyl indole with an acid of formula R.sub.1 OH or an acylating agent corresponding thereto or with an inorganic cyanate or an organic isocyanate or isothiocyanate in order to introduce the desired R.sub.1 group at the 5-position on the indole nucleus.

摘要翻译： 公开了式（I）的化合物其中R 1表示CHO，COR8，CO 2 R 8，CONR 9 R 10，CSNR 9 R 10或SO 2 NR 9 R 10，其中R 8表示烷基，环烷基，芳基或芳烷基，R 9表示氢或烷基，R 10表示氢 或烷基，环烷基，芳基或芳烷基; R2，R3，R4，R6和R7各自独立地表示氢或C1-3烷基; R5表示氢或烷基，环烷基，烯基或芳烷基，或R4和R5一起形成芳烷叉基或R4和R5与连接的氮原子一起形成饱和的单环5-至7-元环; 并且Alk表示任选被不多于两个C 1-3烷基取代的C 2-3亚烷基链; 及其生理上可接受的盐和溶剂合物。 这些化合物潜在地可用于治疗偏头痛，并且可以使用药学上可接受的载体或赋形剂以常规方式配制成药物组合物。 化合物可以通过例如氨基烷基吲哚与式R1OH的酸或对应于其的酰化剂或与无机氰酸酯或有机异氰酸酯或异硫氰酸酯反应制备，以便在5- 在吲哚核上的位置。

公开(公告)号：US4636521A

公开(公告)日：1987-01-13

申请号：US626383

申请日：1984-06-29

申请人： Ian H. Coates ,  Keith Mills ,  Colin F. Webb ,  Michael D. Dowle ,  David E. Bays

发明人： Ian H. Coates ,  Keith Mills ,  Colin F. Webb ,  Michael D. Dowle ,  David E. Bays

IPC分类号： C07D209/14 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/404 ,  A61P9/00 ,  A61P25/04 ,  C07D209/16 ,  C07D209/48 ,  C07D471/04

CPC分类号： C07D209/16

摘要： Compounds are disclosed of general formula (I) ##STR1## wherein R.sub.1 represents an alkyl, cycloalkyl, aryl or aralkyl group;R.sub.2, R.sub.3, R.sub.4, R.sub.6 and R.sub.7, which may be the same or different, each represents a hydrogen atom or a C.sub.1-3 alkyl group;R.sub.5 represents a hydrogen atom or an alkyl, cycloalkyl, alkenyl or an aralkyl group; or R.sub.4 and R.sub.5 together form an aralkylidene group or R.sub.4 and R.sub.5 together with the nitrogen atom to which they are attached form a saturated monocyclic 5- to 7-membered ring; Alk represents an alkylene chain containing two or three carbon atoms which may be unsubstituted or substituted by not more than two C.sub.1-3 alkyl groups; and physiologically acceptable salts, solvates and bioprecursors thereof. The compounds are described as potentially useful for the treatment of migraine and may be formulated as pharmaceutical compositions in conventional manner using one or more pharmaceutically acceptable carriers or excipients. Various processes for the preparation of the compounds are disclosed including, for example, a process involving reaction of an aminoalkyl indole with a sulphonylating agent in order to introduce the --SO.sub.2 -- group at the 5-position on the indole nucleus.

摘要翻译： 公开了通式（I）的化合物其中R 1表示烷基，环烷基，芳基或芳烷基; R 2，R 3，R 4，R 6和R 7可以相同或不同，各自表示氢原子或C 1-3烷基; R5表示氢原子或烷基，环烷基，烯基或芳烷基; 或R 4和R 5一起形成亚烷基或R 4和R 5与它们所连接的氮原子一起形成饱和的单环5-至7-元环; Alk表示含有两个或三个碳原子的亚烷基链，其可以是未取代的或被不多于两个C 1-3烷基取代; 和其生理上可接受的盐，溶剂化物和生物前体。 这些化合物被描述为潜在地可用于治疗偏头痛，并且可以使用一种或多种药学上可接受的载体或赋形剂以常规方式配制成药物组合物。 公开了制备化合物的各种方法，包括例如涉及氨基烷基吲哚与磺酰化剂反应的方法，以便在吲哚核上的5-位引入-SO 2 - 基团。

公开(公告)号：US4855314A

公开(公告)日：1989-08-08

申请号：US1469

申请日：1987-01-08

申请人： Alexander W. Oxford ,  Ian H. Coates ,  David E. Bays ,  Colin F. Webb ,  Michael D. Dowle ,  Keith Mills ,  Colin D. Eldred

发明人： Alexander W. Oxford ,  Ian H. Coates ,  David E. Bays ,  Colin F. Webb ,  Michael D. Dowle ,  Keith Mills ,  Colin D. Eldred

IPC分类号： C07D209/14 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/405 ,  A61P9/00 ,  A61P25/04 ,  C07D209/16

CPC分类号： C07D209/16

摘要： Compounds are disclosed of formula (I): ##STR1## wherein R.sub.1 is halogen, a C.sub.1-3 alkoxy, R.sub.6 R.sub.7 NCO(CH.sub.2).sub.p --, R.sub.6 CONH(CH.sub.2).sub.p --, R.sub.6 R.sub.7 NSO.sub.2 (CH.sub.2).sub.p --, or R.sub.8 SO.sub.2 NH(CH.sub.2).sub.p -- (where R.sub.6 and R.sub.7 each represents hydrogen or C.sub.1-3 alkyl, R.sub.8 represents C.sub.1-3 alkyl and p is zero or 1);R.sub.2 represents hydrogen or C.sub.1-3 alkyl; R.sub.3 represents hydrogen or C.sub.1-3 alkyl;R.sub.4 and R.sub.5 each represents hydrogen, C.sub.1-3 alkyl or 2-propenyl;A represents --CO-- or --SO.sub.2 --;n represents an integer from 2 to 5; and m represents zero or an integer from 1 to 4; and physiologically acceptable salts and solvates (e.g. hydrates) thereof.The compounds have potent and selective vasoconstrictor activity and are indicated as useful for the treatment of migraine. The compounds may be formulated as pharmaceutical compositions with physiologically acceptable carriers or excipients for administration by any convenient route. Various methods for the preparation of the compounds (I) are disclosed.

公开(公告)号：US5196534A

公开(公告)日：1993-03-23

申请号：US704099

申请日：1991-05-22

申请人： John W. F. Whitehead ,  Keith Mills ,  Ian H. Coates ,  Alexander W. Oxford ,  Peter C. North

发明人： John W. F. Whitehead ,  Keith Mills ,  Ian H. Coates ,  Alexander W. Oxford ,  Peter C. North

IPC分类号： C07B61/00 ,  C07D211/86 ,  C07D471/04

CPC分类号： C07D471/04 ,  C07D211/86

摘要： The invention relates to a process for the preparation of a compound of formula (I) ##STR1## wherein R represent a hydrogen atom or a methyl or ethyl group, which comprises cyclising a compound of formul (IV) ##STR2## Where R represents a hydrogen atom, the compound of formula (IV) may optionally be alkylated to produce a compound in whcich R is methyl or ethyl.The compound of formula (I) is useful as an intermediate in the preparation of 2,3,4,5-tetrahydro-2-[(imidazol-4(or 5)-yl)methyl]-1H-pyrido[4,3-b]indol-1-ones having 5-HT.sub.3 antagonist activity.

公开(公告)号：US20120231995A1

公开(公告)日：2012-09-13

申请号：US13473707

申请日：2012-05-17

申请人： Petra Helga Beck ,  Marc Barry Brown ,  David Edward Clark ,  Anthony Coates ,  Hazel Joan Dyke ,  Yanmin Hu ,  Derek John Londesbrough ,  Keith Mills ,  Thomas David Pallin ,  Gary Patrick Reid ,  Gerlinda Stoddart

发明人： Petra Helga Beck ,  Marc Barry Brown ,  David Edward Clark ,  Anthony Coates ,  Hazel Joan Dyke ,  Yanmin Hu ,  Derek John Londesbrough ,  Keith Mills ,  Thomas David Pallin ,  Gary Patrick Reid ,  Gerlinda Stoddart

IPC分类号： A61K31/4745 ,  A01N43/90 ,  A61K31/5377 ,  A61K31/497 ,  A61K31/496 ,  A61K31/43 ,  A61K31/7052 ,  A61K38/12 ,  A61K31/5383 ,  A61P31/00 ,  A01P1/00 ,  A61P31/06 ,  A61P31/04 ,  A61P17/10 ,  A61P1/04 ,  A61P11/08 ,  A61P17/02 ,  A61P29/00 ,  A61P1/02 ,  A61P11/00 ,  A61P27/02 ,  A61P15/02 ,  A61P1/00 ,  A61P15/00 ,  A61P31/08 ,  A61P1/16 ,  A61P15/14 ,  A61P25/00 ,  A61P13/00 ,  A61P1/18 ,  A61P13/08 ,  A61P17/00 ,  A61P31/10 ,  A61P33/02 ,  C07D471/04

CPC分类号： A61K31/4709 ,  A01N43/90 ,  A61K31/43 ,  A61K31/4439 ,  A61K31/4706 ,  A61K31/4725 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/497 ,  A61K31/546 ,  A61K31/7052 ,  A61L2/0088 ,  C07D471/04 ,  Y02A50/401 ,  Y02A50/404 ,  Y02A50/406 ,  Y02A50/411 ,  Y02A50/469 ,  Y02A50/473 ,  Y02A50/475 ,  Y02A50/478 ,  Y02A50/479 ,  Y02A50/481 ,  Y02A50/483

摘要： There is provided the use of compounds of formula I wherein R1, R2, R3 and X have meanings given in the description, for the preparation of a medicament for killing clinically latent microorganisms. There is also provided the use of compounds of formula I for treating microbial infections, as well as certain compounds of formula I per se.

摘要翻译： 提供式I化合物的用途，其中R1，R2，R3和X具有描述中给出的含义，用于制备用于杀死临床潜在微生物的药物。 还提供了式I化合物用于治疗微生物感染的用途，以及式I本身的某些化合物。

公开(公告)号：US08207187B2

公开(公告)日：2012-06-26

申请号：US12092947

申请日：2006-11-08

申请人： Petra Helga Beck ,  Marc Barry Brown ,  David Edward Clark ,  Anthony Coates ,  Hazel Joan Dyke ,  Yanmin Hu ,  Derek John Londesbrough ,  Keith Mills ,  Thomas David Pallin ,  Gary Patrick Reid ,  Gerlinda Stoddart

发明人： Petra Helga Beck ,  Marc Barry Brown ,  David Edward Clark ,  Anthony Coates ,  Hazel Joan Dyke ,  Yanmin Hu ,  Derek John Londesbrough ,  Keith Mills ,  Thomas David Pallin ,  Gary Patrick Reid ,  Gerlinda Stoddart

IPC分类号： A61K31/4745 ,  A61P31/04 ,  C07D471/14 ,  C07D471/04

CPC分类号： A61K31/4709 ,  A01N43/90 ,  A61K31/43 ,  A61K31/4439 ,  A61K31/4706 ,  A61K31/4725 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/497 ,  A61K31/546 ,  A61K31/7052 ,  A61L2/0088 ,  C07D471/04 ,  Y02A50/401 ,  Y02A50/404 ,  Y02A50/406 ,  Y02A50/411 ,  Y02A50/469 ,  Y02A50/473 ,  Y02A50/475 ,  Y02A50/478 ,  Y02A50/479 ,  Y02A50/481 ,  Y02A50/483

摘要： There is provided the use of compounds of formula I wherein R1, R2, R3 and X have meanings given in the description, for the preparation of a medicament for killing clinically latent microorganisms. There is also provided the use of compounds of formula I for treating microbial infections, as well as certain compounds of formula I per se.

摘要翻译： 提供式I化合物的用途，其中R1，R2，R3和X具有描述中给出的含义，用于制备用于杀死临床潜在微生物的药物。 还提供了式I化合物用于治疗微生物感染的用途，以及式I本身的某些化合物。

公开(公告)号：US09694006B2

公开(公告)日：2017-07-04

申请号：US13473707

申请日：2012-05-17

申请人： Petra Helga Beck ,  Marc Barry Brown ,  David Edward Clark ,  Anthony Coates ,  Hazel Joan Dyke ,  Yanmin Hu ,  Derek John Londesbrough ,  Keith Mills ,  Thomas David Pallin ,  Gary Patrick Reid ,  Gerlinda Stoddart

发明人： Petra Helga Beck ,  Marc Barry Brown ,  David Edward Clark ,  Anthony Coates ,  Hazel Joan Dyke ,  Yanmin Hu ,  Derek John Londesbrough ,  Keith Mills ,  Thomas David Pallin ,  Gary Patrick Reid ,  Gerlinda Stoddart

IPC分类号： A61K31/4745 ,  A61K31/4439 ,  C07D471/04

CPC分类号： A61K31/4709 ,  A01N43/90 ,  A61K31/43 ,  A61K31/4439 ,  A61K31/4706 ,  A61K31/4725 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/497 ,  A61K31/546 ,  A61K31/7052 ,  A61L2/0088 ,  C07D471/04 ,  Y02A50/401 ,  Y02A50/404 ,  Y02A50/406 ,  Y02A50/411 ,  Y02A50/469 ,  Y02A50/473 ,  Y02A50/475 ,  Y02A50/478 ,  Y02A50/479 ,  Y02A50/481 ,  Y02A50/483

摘要： There is provided the use of compounds of formula I wherein R1, R2, R3 and X have meanings given in the description, for the preparation of a medicament for killing clinically latent microorganisms. There is also provided the use of compounds of formula I for treating microbial infections, as well as certain compounds of formula I per se.

公开(公告)号：US08521506B2

公开(公告)日：2013-08-27

申请号：US11525231

申请日：2006-09-21

申请人： Mark Lancaster ,  Alastair Gordon ,  Keith Mills

发明人： Mark Lancaster ,  Alastair Gordon ,  Keith Mills

IPC分类号： G06F17/28

CPC分类号： G06F17/289 ,  G06F17/28 ,  G06F17/2827 ,  G06F17/2836

摘要： A computer-implemented method for use in natural language translation comprises performing in software processes, the steps of: comparing source material with stored material in a first natural language, said stored material having previously been translated from said first natural language to at least a second natural language, identifying at least a part of said source material which has a relationship with at least a part of said stored material, outputting said identified part of source material and said identified part of stored material in a form suitable for review by a user, and replacing said identified part of source material with said identified part of stored material to assist full translation of said source material from said first natural language to at least said second natural language.

摘要翻译： 用于自然语言翻译的计算机实现的方法包括在软件过程中执行以下步骤：将源材料与存储的材料以第一自然语言进行比较，所述存储的材料先前已经从所述第一自然语言翻译成至少第二自然语言 自然语言，识别与所述存储的材料的至少一部分具有关系的所述源材料的至少一部分，以适合用户审查的形式输出所述源材料的所述识别的部分和存储的材料的所述识别的部分， 以及用所述确定的所存储的材料部分替换源材料的所述识别的部分，以帮助所述源材料从所述第一自然语言到至少所述第二自然语言的完全翻译。

公开(公告)号：US20080077395A1

公开(公告)日：2008-03-27

申请号：US11525231

申请日：2006-09-21

申请人： Mark Lancaster ,  Alastair Gordon ,  Keith Mills

发明人： Mark Lancaster ,  Alastair Gordon ,  Keith Mills

IPC分类号： G06F17/27

CPC分类号： G06F17/289 ,  G06F17/28 ,  G06F17/2827 ,  G06F17/2836

摘要： A computer-implemented method for use in natural language translation comprises performing in software processes, the steps of: comparing source material with stored material in a first natural language, said stored material having previously been translated from said first natural language to at least a second natural language, identifying at least a part of said source material which has a relationship with at least a part of said stored material, outputting said identified part of source material and said identified part of stored material in a form suitable for review by a user, and replacing said identified part of source material with said identified part of stored material to assist full translation of said source material from said first natural language to at least said second natural language.

摘要翻译： 用于自然语言翻译的计算机实现的方法包括在软件过程中执行以下步骤：将源材料与存储的材料以第一自然语言进行比较，所述存储的材料先前已经从所述第一自然语言翻译成至少第二自然语言 自然语言，识别与所述存储的材料的至少一部分具有关系的所述源材料的至少一部分，以适合用户审查的形式输出所述源材料的所述识别的部分和存储的材料的所述识别的部分， 以及用所述确定的所存储的材料部分替换源材料的所述识别的部分，以帮助所述源材料从所述第一自然语言到至少所述第二自然语言的完全翻译。

公开(公告)号：US20130346062A1

公开(公告)日：2013-12-26

申请号：US13951451

申请日：2013-07-25

申请人： Mark Lancaster ,  Alistair Gordon ,  Keith Mills

发明人： Mark Lancaster ,  Alistair Gordon ,  Keith Mills

IPC分类号： G06F17/28

CPC分类号： G06F17/289 ,  G06F17/28 ,  G06F17/2827 ,  G06F17/2836

摘要： A computer-implemented method for use in natural language translation comprises performing in software processes, the steps of: comparing source material with stored material in a first natural language, said stored material having previously been translated from said first natural language to at least a second natural language, identifying at least a part of said source material which has a relationship with at least a part of said stored material, outputting said identified part of source material and said identified part of stored material in a form suitable for review by a user, and replacing said identified part of source material with said identified part of stored material to assist full translation of said source material from said first natural language to at least said second natural language.

摘要翻译： 用于自然语言翻译的计算机实现的方法包括在软件过程中执行以下步骤：将源材料与存储的材料以第一自然语言进行比较，所述存储的材料先前已经从所述第一自然语言翻译成至少第二自然语言 自然语言，识别与所述存储的材料的至少一部分具有关系的所述源材料的至少一部分，以适合用户审查的形式输出所述源材料的所述识别的部分和存储的材料的所述识别的部分， 以及用所述确定的所存储的材料部分替换源材料的所述识别的部分，以帮助所述源材料从所述第一自然语言到至少所述第二自然语言的完全翻译。