公开(公告)号：US4994483A

公开(公告)日：1991-02-19

申请号：US443874

申请日：1989-11-30

申请人： Alexander W. Oxford ,  Brian Evans ,  Michael D. Dowle ,  Ian H. Coates

发明人： Alexander W. Oxford ,  Brian Evans ,  Michael D. Dowle ,  Ian H. Coates

IPC分类号： C07D209/14 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P9/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/06 ,  C07C67/00 ,  C07C301/00 ,  C07C311/02 ,  C07C311/35 ,  C07D209/08 ,  C07D209/10 ,  C07D209/12 ,  C07D209/16 ,  C07D209/18 ,  C07D209/48

CPC分类号： C07D209/48 ,  C07C205/44 ,  C07C309/00 ,  C07D209/08 ,  C07D209/10 ,  C07D209/12 ,  C07D209/16 ,  C07D209/18 ,  Y10S514/93

摘要： Indole derivatives are disclosed of the general formula (I): ##STR1## wherein R.sub.1 is hydrogen, C.sub.1-6 alkyl or C.sub.3-6 alkenyl; R.sub.2 is a hydrogen, C.sub.1-3 alkyl, C.sub.3-6 alkenyl, phenyl, phen(C.sub.1-4)alkyl or C.sub.5-7 cycloalkyl; R.sub.3 and R.sub.4 are hydrogen, C.sub.1-3 alkyl or propenyl groups or together form an aralkylidene group; Alk is C.sub.2 -C.sub.3 alkylene chain and A is C.sub.2 -C.sub.5 alkylene chainand its physiologically acceptable salts and solvates.The compounds may be prepared, for example, by cyclization of a compound of general formula (II): ##STR2## where Q is the group NR.sub.3 R.sub.4 or a protected derivative thereof or a leaving group and R.sub.1 l, R.sub.2, R.sub.3, R.sub.4, A and Alk are as defined for formula (I).The compounds have a selective vosoconstrictor action and are useful in treating pain such as migraine. The compounds may be formulated as pharmaceutical compositions in conventional manner, preferably for oral administration.

摘要翻译： 公开了通式（I）的吲哚衍生物：其中R 1是氢，C 1-6烷基或C 3-6烯基; R 2是氢，C 1-3烷基，C 3-6烯基，苯基，苯基（C 1-4）烷基或C 5-7环烷​​基; R3和R4是氢，C1-3烷基或丙烯基或一起形成亚烷基; Alk是C2-C3亚烷基链，A是C2-C5亚烷基链及其生理上可接受的盐和溶剂合物。 化合物可以例如通过环化通式（II）的化合物来制备：其中Q是NR3R4基团或其保护的衍生物或离去基团，R1，R2，R3 ，R4，A和Alk如式（I）所定义。 该化合物具有选择性的血管收缩作用，并且可用于治疗疼痛如偏头痛。 化合物可以以常规方式配制成药物组合物，优选用于口服给药。

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：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：US4894387A

公开(公告)日：1990-01-16

申请号：US030235

申请日：1987-03-26

申请人： Darko Butina ,  Michael D. Dowle ,  Ian H. Coates

发明人： Darko Butina ,  Michael D. Dowle ,  Ian H. Coates

IPC分类号： C07D209/14 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P9/00 ,  A61P25/04 ,  C07C67/00 ,  C07C301/00 ,  C07C311/35 ,  C07D209/16 ,  C07D209/18

CPC分类号： C07D209/18 ,  C07D209/16

摘要： Compounds are disclosed of the general formula (I) ##STR1## wherein R.sub.1 represents halogen, alkyl, alkoxy or hydroxyl, or a group NR.sub.a R.sub.b or CON.sub.a R.sub.b, where R.sub.a and R.sub.b are hydrogen, alkyl or alkenyl or with the nitrogen atom form a saturated monocyclic 5 to 7-membered ring;R.sub.2 represents hydrogen or alkyl;R.sub.3 and R.sub.4 represent hydrogen, C.sub.1-3 alkyl or propenyl or R.sub.3 and R.sub.4 together form an aralkylidene group; Alk represents a C.sub.2-3 alkylene chain;n and m, are integers of 1 to 4 or n is zero, and their physiologically acceptable salts and solvates.The compounds are described as useful in treating pain originating from dilatation of the cranial vasculature in particular migraine and cluster headache and can be formulated in conventional manner as pharmaceutical compositions with carriers or excipients for administration by any convenient route.

摘要翻译： 公开了通式（I）的化合物其中R 1表示卤素，烷基，烷氧基或羟基，或NRaRb或CONaRb基团，其中R a和R b是氢，烷基或链烯基或氮原子形式 饱和单环5至7元环; R2代表氢或烷基; R3和R4代表氢，C1-3烷基或丙烯基或R3和R4一起形成亚烷基; Alk表示C2-3亚烷基链; n和m是1〜4的整数或n为0的整数，以及它们的生理上可接受的盐和溶剂合物。 描述了这些化合物可用于治疗源于颅血管扩张的疼痛，特别是偏头痛和丛集性头痛，并且可以以常规方式配制成具有载体或赋形剂的药物组合物，通过任何方便的途径给药。

公开(公告)号：US4816470A

公开(公告)日：1989-03-28

申请号：US789831

申请日：1985-11-15

申请人： Michael D. Dowle ,  Ian H. Coates

发明人： Michael D. Dowle ,  Ian H. Coates

IPC分类号： C07D209/14 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/404 ,  A61P9/00 ,  A61P25/04 ,  A61P25/06 ,  C07D209/10 ,  C07D209/16 ,  C07D209/18 ,  C07D209/24 ,  C07D209/48

CPC分类号： C07D209/48 ,  C07D209/10 ,  C07D209/16 ,  C07D209/18 ,  C07D209/24

摘要： Indole derivatives of the general formula (I) are disclosed: ##STR1## where R.sub.1 is H or an alkyl or alkenyl group, R.sub.2 is H, or an alkyl, alkenyl, aryl, aralkyl or cycloalkyl group;R.sub.3 is H or an alkyl group;R.sub.4 and R.sub.5 are independently H or an alkyl or propenyl group or together form an aralkylidene group; andAlk is an optionally substituted alkylene chain; and their physiologically acceptable salts and solutes.These compounds are potentially useful for the treatment of migraine and may be formulated as pharmaceutical compositions in conventional manner.Various methods for the production of the compounds are disclosed including a Fischer-indole cyclization process.

摘要翻译： 公开了通式（I）的吲哚衍生物：其中R 1是H或烷基或烯基，R 2是H或烷基，烯基，芳基，芳烷基或环烷基; R3是H或烷基; R 4和R 5独立地为H或烷基或丙烯基或一起形成亚烷基; 并且Alk是任选取代的亚烷基链; 及其生理上可接受的盐和溶质。 这些化合物潜在地可用于治疗偏头痛，并且可以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，包括费 - 吲哚环化方法。

公开(公告)号：US5276050A

公开(公告)日：1994-01-04

申请号：US908329

申请日：1992-07-06

申请人： Steven J. Cooper ,  Ian H. Coates ,  Alexander W. Oxford ,  Peter C. North

发明人： Steven J. Cooper ,  Ian H. Coates ,  Alexander W. Oxford ,  Peter C. North

IPC分类号： A61K31/415

CPC分类号： A61K31/415

摘要： The invention relates to the use of compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof, in which 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 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;and n represents 2 or 3,for the treatment of a condition involving excessive eating, for example bulimia.

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和溶剂化物，其中Im表示下式的咪唑基：其中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 或更多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; n表示2或3，用于治疗涉及过度饮食的病症，例如贪食症。

公开(公告)号：US5066660A

公开(公告)日：1991-11-19

申请号：US570513

申请日：1990-08-21

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

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

IPC分类号： A61K31/4427 ,  A61K31/445 ,  A61P25/04 ,  A61P25/06 ,  C07D401/04

CPC分类号： C07D401/04

摘要： Compounds are disclosed of formula (I) ##STR1## wherein R.sub.1 represents H or C.sub.1-6 alkyl;R.sub.2 represents H, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phen(C.sub.1-3)alkyl in which the phenyl ring is optionally substituted by halogen, C.sub.1-4 alkoxy, hydroxy or C.sub.1-3 alkyl;R.sub.3 represents H, C.sub.1-3 alkyl, --CO.sub.2 R.sub.5, --COR.sub.5, --COCO.sub.2 R.sub.5 or --CONHR.sub.5 whereR.sub.5 represents H, C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-4 alkenyl, aryl or ar(C.sub.1-4)alkyl in which the aryl group is optionally substituted by halogen, C.sub.1-4 alkoxy, C.sub.1-4 alkyl or hydroxy) (provided that where R.sub.3 represents --CO.sub.2 R.sub.5, R.sub.5 is other than H);R.sub.4 represents H, C.sub.1-3 alkyl, C.sub.3-6 alkenyl, phenyl or phen (C.sub.1-3)alkyl;A-B represents CH--CH.sub.2 --or C.dbd.CH--D represents --CO-- or --SO.sub.2 --n represents 0, 1-5;provided that when D represents --SO.sub.2, n is 2, R.sub.3 represents H and R.sub.4 represents H or C.sub.1-3 alkyl, R.sub.2 is other than H or C.sub.1-6 alkyl; and pharmaceutically acceptable salts and solvates (for example hydrates) thereof.The compounds are indicated as useful for the treatment of migraine, cluster headache, chronic paroxysmal hemicrania and headache associated with vascular disorders.Processes and intermediates for their preparation and pharmaceutical compositions containing them are also disclosed.

公开(公告)号：US4997831A

公开(公告)日：1991-03-05

申请号：US401249

申请日：1989-08-31

申请人： David E. Bays ,  Ian H. Coates ,  Alexander W. Oxford ,  Peter C. North

发明人： David E. Bays ,  Ian H. Coates ,  Alexander W. Oxford ,  Peter C. North

IPC分类号： A61K31/415 ,  A61K31/435 ,  A61K31/495 ,  A61K31/535 ,  A61K31/55 ,  A61P1/00 ,  A61P1/04 ,  A61P1/08 ,  A61P3/06 ,  A61P25/04 ,  A61P25/06 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P43/00 ,  C07D471/16 ,  C07D487/16 ,  C07D495/16 ,  C07D498/16 ,  C07D513/16 ,  C07D471/04 ,  A61K31/475

CPC分类号： C07D471/16 ,  C07D487/16 ,  C07D498/16

摘要： The invention provides lactam derivatives of the general formula (I) ##STR1## wherein n represents 2 or 3; Im represents an imidazolyl group of the formula: ##STR2## wherein 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 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; Y represents a group --(CH.sub.2).sub.m --, wherein m represents 2, 3 or 4; or Y represents a group --X(CH.sub.2).sub.p --, wherein p represents 2 or 3, X represents an oxygen or a sulphur atom or a group NR.sup.4, where R.sup.4 is a C.sub.1-6 alkyl group, and X is attached to the benzene ring moiety of the molecule; and physiologically acceptable salts and solvates thereof.The compounds of formula (I) are potent and selective antagonists of 5-hydroxytryptamine at 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：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。