公开(公告)号：US5543419A

公开(公告)日：1996-08-06

申请号：US204260

申请日：1994-07-05

Applicant: Peter E. Cross ,  Alan Stobie

Inventor： Peter E. Cross ,  Alan Stobie

IPC: A61K31/435 ,  A61K31/00 ,  A61K31/439 ,  A61P11/00 ,  A61P11/06 ,  A61P11/08 ,  A61P25/30 ,  C07C317/44 ,  C07C317/46 ,  C07C323/56 ,  C07D333/06 ,  C07D333/24 ,  C07D453/02

CPC classification number: C07D333/24 ,  C07C317/44 ,  C07C323/56 ,  C07D453/02

Abstract: Compounds of formula (I) wherein X is either (a) a phenyl group optionally substituted by 1 or 2 substituents each independently selected from halo, CF.sub.3, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and hydroxy or (b) a thienyl group; and Y is of formula (Ya) or (Yb) where A and B are 0, 1 or 2, D and E are 0 or 1, F is 0-3 and D+E+F=1-3, Z is 0, 1 or 2, R.sub.1 and R.sub.2 are H or alkyl or form a ring, and R.sub.3 is C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.6 cycloalkyl or optionally substituted phenyl or benzyl, are antimuscarinic bronchodilators useful for treating chronic obstructive airways disease or asthma.

Abstract translation: PCT No.PCT / EP92 / 02067 Sec。 371日期：1994年7月5日 102（e）日期1994年7月5日PCT提交1992年9月3日PCT公布。 公开号WO93 / 06098 （Yb）式（I）化合物其中X为（a）任选被1或2个取代基任意取代的苯基，各自独立地选自 卤代，CF 3，C 1 -C 4烷基，C 1 -C 4烷氧基和羟基或（b）噻吩基; 并且Y为式（Ya）或（Yb），其中A和B为0,1或2，D和E为0或1，F为0-3，D + E + F = 1-3，Z为0 ，1或2，R1和R2是H或烷基或形成环，R3是C1-C4烷基，C3-C6环烷基或任选取代的苯基或苄基是可用于治疗慢性阻塞性气道疾病或哮喘的抗毒蕈碱性支气管扩张剂。

公开(公告)号：US20090239928A1

公开(公告)日：2009-09-24

申请号：US11721352

申请日：2005-12-02

Applicant: Paul Vincent Fish ,  Thomas Ryckmans ,  Alan Stobie ,  Florian Wakenhut

Inventor： Paul Vincent Fish ,  Thomas Ryckmans ,  Alan Stobie ,  Florian Wakenhut

IPC: A61K31/40 ,  C07D207/14 ,  A61P13/00

CPC classification number: C07D207/14

Abstract: A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein: R1 is H, C1-6alkyl, —C(A)D, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-8allkyl, C1-8alkoxy, OH, halo, CF3, OCHF2, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; A is S or O; D is H, C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl; R2 represents aryl1 or het1, each of which is substituted by at least one substituent independently selected from B, provided that when R2 is substituted by halo then it is also substituted with at least one other substituent independently selected from B other than halo; B represents aryl2, het2, Oaryl2, Ohet2, Sarl2, Shet2, SC1-6alkyl, halogen, CHF2, OCHF2, CF2CF3, CH2CF3, CF2CH3, aryl2-C1-4alkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl, C3-6cycloalkylC1-4alkoxy, C3-6cycloalkyl-O—C1-4 alkyl, C3-6cycloalkyl-C1-4alkoxy-C1-4alkyl, OC3-6cycloalkyl, SC3-6cycloalkyl; wherein the aryl2 and het2 groups are optionally substituted by at least one group selected from C1-6alkyl, C3-6cycloalkyl, C1-6alkoxy, OC3-6cycloalkyl, halo, CN, OH, CF3, CHF2, OCF3, OCHF2, hydroxyC1$alkyl, C1-4alkoxy-C1-4alkyl, SC1-6alkyl and SCF3; n is 1 or 2, provided that when n is 1, m is 0 or 1 and when n is 2, m is 0, wherein if m is 0, then * represents a chiral centre; R3 is H, C1-6alkyl, C3-8cycloalkyl, C3-8cycloalkylC1-6alkyl, aryl3, het3, aryl3-C1-4alkyl or het3-C1-4alkyl, wherein the C3-8cycloalkyl, aryl3 or het3 groups are optionally substituted by at least one substituent independently selected from C1-6alkyl, C1-6alkoxy, CN, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; at each occurrence aryl, aryl1, aryl2 and aryl3 independently represent phenyl, naphthyl, anthracyl or phenanthryl; het1 represents an aromatic 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to an aryl group; at each occurrence het, het2, and het3 independently represents an aromatic or non-aromatic 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6-membered carbocyclic group or a second 4-, 5- or 6membered heterocycle which contains at least one N, O or S heteroatom.

公开(公告)号：US07449462B2

公开(公告)日：2008-11-11

申请号：US10588876

申请日：2005-01-11

Applicant: Justin S. Bryans ,  Patrick S. Johnson ,  Thomas Ryckmans ,  Alan Stobie

Inventor： Justin S. Bryans ,  Patrick S. Johnson ,  Thomas Ryckmans ,  Alan Stobie

IPC: C07D401/14 ,  A61K31/5517

CPC classification number: C07D401/14

Abstract: Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: Het represents 2-pyridinyl or 2-pyrimidinyl; R1 represents H, C1-3 alkyl or a nitrogen-containing heterocyclic ring having 5 or 6 ring atoms; R2 represents H, benzyl or C1-3 alkyl; and R3 represents H, methyl, methoxy or chloro; are useful for treating anxiety, cardiovascular disease (including angina, atherosclerosis, hypertension, heart failure, edema, hypernatremia), dysmenorrhoea (primary and secondary), endometriosis, emesis (motion sickness), intrauterine growth retardation, inflammation (including rheumatoid arthritis), mittlesmerchz, preclampsia, premature ejaculation, premature (preterm) labor and Raynaud's disease.

Abstract translation: 式（I）化合物或其药学上可接受的衍生物，其中：Het表示2-吡啶基或2-嘧啶基; R 1表示H，C 1-3烷基或具有5或6个环原子的含氮杂环; R 2表示H，苄基或C 1-3烷基; R 3表示H，甲基，甲氧基或氯; （包括心绞痛，动脉粥样硬化，高血压，心力衰竭，水肿，高钠血症），痛经 早泄，过早（早产）劳动和雷诺氏病。

公开(公告)号：US07442795B2

公开(公告)日：2008-10-28

申请号：US11416498

申请日：2006-05-01

Applicant: Justin Stephen Bryans ,  Patrick Stephen Johnson ,  Thomas Ryckmans ,  Alan Stobie

Inventor： Justin Stephen Bryans ,  Patrick Stephen Johnson ,  Thomas Ryckmans ,  Alan Stobie

IPC: C07D401/14 ,  C07D413/14

CPC classification number: C07D401/04 ,  C07D413/14 ,  C07D487/04 ,  C07D513/04

Abstract: A compound of formula (I), or a pharmaceutically acceptable derivative, wherein A, B, V, W, X, Y, and Z are as defined herein; pharmaceutical compositions thereof; and uses thereof.

Abstract translation: 式（I）化合物或其药学上可接受的衍生物，其中A，B，V，W，X，Y和Z如本文所定义; 其药物组合物; 及其用途。

公开(公告)号：US20070225333A1

公开(公告)日：2007-09-27

申请号：US10598840

申请日：2005-04-18

Applicant: Justin Bryans ,  Patrick Johnson ,  Thomas Ryckmans ,  Alan Stobie

Inventor： Justin Bryans ,  Patrick Johnson ,  Thomas Ryckmans ,  Alan Stobie

IPC: C07D401/04 ,  C07D401/14 ,  C07D403/04

CPC classification number: C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14

Abstract: Compounds of formula (I): or a pharmaceutically acceptable derivative thereof, wherein R represents C1-6alkyl (optionally substituted by C1-6alkyloxy or Het) or C1-6alkyloxy; R1 and R2 independently represent hydrogen, halo or C1-6alkyl, ring A represents Het1; X represents O or NR3; R3 represents hydrogen or C1-6alkyl; ring B represents a phenyl group or Het2, either of which may be optionally substituted with one or more groups selected from halo, CN, C1-6alkyloxy, CF3, C1-6alkyl, NH2 and NO2; Het and Het1 independently represent a 5- or 6-membered saturated, partially unsaturated or aromatic heterocyclic group comprising either (a) 1 to 4 nitrogen atoms, (b) one oxygen or one sulphur atom or (c) 1 oxygen atom or 1 sulphur atoms and 1 or 2 nitrogen atoms are useful for treating anxiety, cardiovascular disease (including angina, atherosclerosis, hypertension, heart failure, edema, hypernatremia), dysmenorrhoea (primary and secondary), endometriosis, emesis (including motion sickness), intrauterine growth retardation, inflammation (including rheumatoid arthritis) mittlesmerchz, preclampsia, premature ejaculation, premature (preterm) labour and Raynaud's disease.

Abstract translation: 或式（I）化合物或其药学上可接受的衍生物，其中R表示C 1-6烷基（任选被C 1-6烷氧基或Het取代）或C 1-6烷基氧基; R 1和R 2独立地表示氢，卤素或C 1-6烷基，环A表示Het 1〜 ; X表示O或NR 3; R 3表示氢或C 1-6烷基; 环B表示苯基或Het 2，其中任一个可以任选被一个或多个选自卤素，CN，C 1-6烷氧基，CF 3， C 1〜C 6烷基，NH 2和NO 2; Het和Het 1独立地表示5-或6-元饱和，部分不饱和或芳族杂环基，其包含（a）1-4个氮原子，（b）一个氧或一个硫原子或（ c）1个氧原子或1个硫原子和1或2个氮原子可用于治疗焦虑症，心血管疾病（包括心绞痛，动脉粥样硬化，高血压，心力衰竭，水肿，高钠血症），痛经（原发性和继发性），子宫内膜异位症，呕吐 包括运动病），子宫内生长迟缓，炎症（包括类风湿性关节炎）手段，先兆子痫，早泄，早产（早产）劳动和雷诺病。

公开(公告)号：US07122683B2

公开(公告)日：2006-10-17

申请号：US11280128

申请日：2005-11-15

Applicant: Paul Vincent Fish ,  Thomas Ryckmans ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Alistair Whitlock

Inventor： Paul Vincent Fish ,  Thomas Ryckmans ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Alistair Whitlock

IPC: C07D207/14

CPC classification number: C07D207/14 ,  C07D405/12

Abstract: A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein: R1, R2, R3 and R20 are each independently H, Cl, Br, F, I, CF3, OCF3, Me or Et; R4 is het or C3-7 cycloalkyl optionally substituted by C1-4 alkyl, C1-4 alkoxy, alkoxyalkyl containing 2 to 4 carbon atoms or —S—(C1-4 alkyl); a is 0 or 1; and het is a non-aromatic 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6-membered carbocyclic group or a second 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, wherein the het group is optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; provided that at least one of R1, R2 and R3 are other than H. The compounds of the invention exhibit activity as both serotonin and noradrenaline re-uptake inhibitors and therefore have utility in a variety of therapeutic areas, for example urinary incontinence.

Abstract translation: 式（I）的化合物及其药学和/或兽医学上可接受的衍生物，其中：R 1，R 2，R 3和R 3 各自独立地为H，Cl，Br，F，I，CF 3，OCF 3，Me或Et; R 4是H或任选被C 1-4烷基取代的C 3-7环烷基，C 1-4 - 烷氧基，含有2至4个碳原子的烷氧基烷基或-S-（C 1-4烷基）; a是0或1; 并且它是非芳族的4-，5-或6-元杂环，其含有至少一个N，O或S杂原子，任选地与5或6元碳环基团或第二个4-，5-或 其含有至少一个N，O或S杂原子的6元杂环，其中所述基团任选地被至少一个独立地选自C 1-8烷基，C 1- 8个烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6 C 1-4烷基，C 1-4烷氧基-C 1-6烷基和C 1-4烷基-S SC 1 -4 烷基; 条件是R 1，R 2和R 3中的至少一个不是H.本发明的化合物表现出作为血清素的活性 和去甲肾上腺素再摄取抑制剂，因此可用于各种治疗领域，例如尿失禁。

公开(公告)号：US5292749A

公开(公告)日：1994-03-08

申请号：US852261

申请日：1992-06-05

Applicant: Alan Stobie

Inventor： Alan Stobie

IPC: A61K31/435 ,  A61K31/44 ,  A61K31/50 ,  A61K31/505 ,  A61P11/08 ,  A61P25/02 ,  C07D453/02 ,  C07D521/00 ,  C07D453/00

CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D453/02 ,  Y10S514/826

Abstract: ##STR1## 3-Quinuclidinyl butanoate and propanoate antimuscarinic bronchodilators, particularly useful in the treatment of chronic obstructive airways disease and asthma, of formula (1), and their pharmaceutically acceptable salts, wherein X is either (a) a phenyl group optionally substituted by one or two substituents each independently selected from halo. CF
3 , C
1 -C
4 alkyl, C
1 -C
4 alkoxy and hydroxy or (b) a thienyl group; and "Het" is either (a) a 5-membered nitrogen-containing heterocyclic group attached to the adjacent carbon atom either by a carbon or a ring nitrogen atom and which is selected from imidazolyl, pyrazolyl, triazolyl and tetrazolyl. (b) an oxadiazolyl or thiadiazolyl group attached to the adjacent carbon atom by a carbon atoms, or (c) a 6-membered nitrogen-containing heterocyclic group attached to the adjacent carbon atom by a carbon atom and selected from pyridinyl, pyrazinyl, pyrimidinyl and pyridazinyl, "Het" being optionally substituted by up to two substituents each independently selected from halo, CF
3 , C
1 -C
4 alkyl, C
1 -C
4 alkoxy, hydroxy, amino and azido; and m is 1 or 2.

Abstract translation: （I）3-喹喔啉基丁酸酯和丙酸酯抗毒蕈碱性支气管扩张剂，其特别可用于治疗式（1）的慢性阻塞性气道疾病和哮喘及其药学上可接受的盐，其中X为（a）苯基 任选被一个或两个独立地选自卤素的取代基取代。 CF 3，C 1 -C 4烷基，C 1 -C 4烷氧基和羟基或（b）噻吩基; 和“Het”是（a）通过碳或环氮原子连接在相邻碳原子上的5元含氮杂环基，其选自咪唑基，吡唑基，三唑基和四唑基。 （b）通过碳原子连接到相邻碳原子上的恶二唑基或噻二唑基，或（c）通过碳原子连接到相邻碳原子上的6元含氮杂环基，并且选自吡啶基，吡嗪基，嘧啶基 和哒嗪基，“Het”任选被至多两个独立地选自卤素，CF 3，C 1 -C 4烷基，C 1 -C 4烷氧基，羟基，氨基和叠氮基的取代基取代。 m为1或2。

公开(公告)号：US20100137316A1

公开(公告)日：2010-06-03

申请号：US12702383

申请日：2010-02-09

Applicant: Paul Vincent Fish ,  Malcolm Christian MacKenny ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Alistair Whitlock

Inventor： Paul Vincent Fish ,  Malcolm Christian MacKenny ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Alistair Whitlock

IPC: A61K31/5375 ,  C07D265/30

CPC classification number: C07D413/06 ,  A61K31/535 ,  C07D265/30 ,  C07D413/12

Abstract: The present invention provides compounds of Formula I wherein R1, R2, R3, and n have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of conditions including urinary disorders, pain, premature ejaculation, ADHD and fibromyalgia. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.

Abstract translation: 本发明提供式I化合物，其中R1，R2，R3和n具有说​​明书中定义的任何值及其药学上可接受的盐，其可用作治疗包括尿失禁，疼痛，过早 射精，ADHD和纤维肌痛。 还提供了包含一种或多种式I化合物的药物组合物。

公开(公告)号：US20090239929A1

公开(公告)日：2009-09-24

申请号：US11721359

申请日：2005-12-02

Applicant: Paul Vincent Fish ,  Thomas Ryckmans ,  Alan Stobie ,  Florian Wakenhut

Inventor： Paul Vincent Fish ,  Thomas Ryckmans ,  Alan Stobie ,  Florian Wakenhut

IPC: A61K31/40 ,  C07D207/14 ,  A61P13/00 ,  A61P25/24 ,  A61P25/00 ,  A61P15/12

CPC classification number: C07D207/14

Abstract: A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein: R1 is H, C1-6alkyl, —C(A)D, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted; A is S or O; D is H, C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl; aryl represents phenyl, naphthyl, anthracyl or phenanthryl; het represents an aromatic or non-aromatic 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6-membered carbocyclic group or a second 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom; R2 is aryl1 or het1, each optionally substituted; n is 1 or 2, provided that when n is 1, m is 0 or 1 and when n is 2, m is 0, wherein if m is 0, then * represents a chiral centre; R3 is (CH2)aE, wherein a is 0, 1 or 2 and E is a group selected from: Formula (i) wherein: X is O, S, NR12, (CH2)v or a bond; b is 1, 2, 3 or 4; c is 1, 2 or 3; v is 1 or 2; R10 and 11 are each independently H or C1-4 alkyl; and R12 is H, 1-6 alkyl, C(O)C1-6 alkyl, SO2—C1-6alkyl; and wherein one or more pairs of hydrogen atoms on adjacent carbon or nitrogen atoms may be replaced by a corresponding number of double bonds, provided the ring system is not aromatic; Formula (ii) a carbocyclic spiro group containing 6 to 12 carbon atoms; Formula (iii) wherein: d is 1, 2, 3 or 4; a is 1, 2 or 3; f is 1 or 2; and R30 is H or C1-4alkyl; and wherein one or more pairs of hydrogen atoms on adjacent carbon atoms may be replaced by a corresponding number of double bonds, provided the ring system is not aromatic; Formula (iv) wherein: g is 0, 1, 2 or 3; J is NR40; and R40 is C(O)C1-6 alkyl, S02-C1-6alkyl; Formula (v) wherein: h is 0, 1, 2 or 3; and R50 is H, C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; Formula (vi) —CH(cyclopropane)2; Formula (vii) C1-6alkyl, substituted by at least one substituent; and Formula (viii) C3-8cycloalkyl-C1-6alkyl; wherein the C1-6alkyl moiety is substituted at any point other than at the junction with the C3-8cycloalkyl moiety, by at least one substituent. The compounds exhibit activity as both serotonin and/or noradrenaline re-uptake inhibitors and therefore have utility in a variety of therapeutic areas, for example urinary incontinence.

公开(公告)号：US20080306123A1

公开(公告)日：2008-12-11

申请号：US12124755

申请日：2008-05-21

Applicant: Paul Vincent Fish ,  Michael Jonathan Fray ,  Deborah Jane Lovering ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Alistair Whitlock ,  Mark David Andrews ,  Alan Daniel Brown ,  Mark Ian Lansdell

Inventor： Paul Vincent Fish ,  Michael Jonathan Fray ,  Deborah Jane Lovering ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Alistair Whitlock ,  Mark David Andrews ,  Alan Daniel Brown ,  Mark Ian Lansdell

IPC: A61K31/4468 ,  A61P13/00 ,  A61P29/00 ,  A61P15/00 ,  A61P25/24

CPC classification number: C07D207/14

Abstract: A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein R1 is H, C1-6alkyl, —C(X)Y, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; R2 is aryl or heteroaryl, each optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; R3 is C1-6alkyl, C3-8cycloalkyl, C3-8cycloalkyl-C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-6alkyl, C1-6alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; X is S or O; Y is H, C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl; and n is 1 or 2, provided that when n is 1, m is 0 or 1 and when n is 2, m is 0, wherein if m is 0, then * represents a chiral center. The compounds of the invention exhibit activity as both serotonin and noradrenaline re-uptake inhibitors and therefore have utility in a variety of therapeutic areas, for example urinary incontinence.

Abstract translation: 式（I）化合物及其药学上和/或兽医学上可接受的衍生物，其中R 1是H，C 1-6烷基，-C（X）Y，C 3-8环烷基，芳基，het，芳基-C 1-4烷基或叔丁基 其中环烷基，芳基或苯基基团任选被至少一个独立地选自C 1-8烷基，C 1-8烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6烷基，C 1-4烷氧基 - C 1-6烷基和C 1-4烷基-S-C 1-4烷基; R 2是芳基或杂芳基，各自任选被至少一个独立地选自C 1-8烷基，C 1-8烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6烷基，C 1-4烷氧基-C 1-6烷基和C 1 -4-烷基-S-C 1-4烷基; R 3为C 1-6烷基，C 3-8环烷基，C 3-8环烷基-C 1-6烷基，芳基，杂环基，芳基-C 1-4烷基或叔-C 1-4烷基，其中环烷基，芳基或苯基基团任选被至少一个取代基取代 独立地选自C 1-6烷基，C 1-6烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6烷基，C 1-4烷氧基-C 1-6烷基和C 1-4烷基-S-C 1-4烷基; X是S或O; Y是H，C 1-6烷基，芳基，杂环基，芳基-C 1-4烷基或叔丁基C 1-4烷基; n为1或2，条件是当n为1时，m为0或1，当n为2时，m为0，其中如果m为0，则*表示手性中心。 本发明的化合物表现出5-羟色胺和去甲肾上腺素再摄取抑制剂的活性，因此可用于各种治疗领域，例如尿失禁。